Compounds > tadalafil
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tadalafil

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Cross-References

ID SourceID
PubMed CID110635
CHEMBL ID779
CHEBI ID71940
SCHEMBL ID33333
MeSH IDM0431130

Synonyms (144)

Synonym
AB00639969-08
ly-450190
cialis
adcirca
ic-351
gf-196960
CIA ,
6-benzo[1,3]dioxol-5-yl-2-methyl-2,3,6,7,12,12a-hexahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
MLS001424132
tadalafil ,
MLS000759426
smr000466321
1XOZ
DB00820
(6r,12ar)-2,3,6,7,12,12a-hexahydro-2-methyl-6-(3,4-(methylenedioxy)phenyl) pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione
(6r-trans)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione
cialis (tn)
D02008
171596-29-5
adcirca (tn)
zalutia (tn)
tadalafil (jan/usp/inn)
pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6r-trans)-
ic 351
ic351
tadalafil [usan]
icos 351
pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6r,12ar)-
(6r,12ar)-2,3,6,7,12,12a-hexahydro-2-methyl-6-(3,4-methylenedioxyphenyl)pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione
hsdb 7303
gf 196960
(2r,8r)-2-(2h-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione
(6r,12ar)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1,2,1,6]pyrido[3,4-b]indole-1,4-dione
chembl779 ,
bdbm14777
MLS001165782
MLS001195644
HMS2051N17
chebi:71940 ,
tadalafil mylan
nsc-750236
nsc-759172
ly450190
trans-tadalafil
nsc750236
pyrazino[1',6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12ahexahydro-2-methyl-, (6r,12ar)-
(6r,3,6,7,12,12a-hexahydro-2-methyl-6-[3,4-(methylenedioxy)phenyl]pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
(6r,12ar)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
A23556
dtxcid7026786
dtxsid9046786 ,
tox21_112642
cas-171596-29-5
nsc759172
pharmakon1600-01505639
HMS2235L21
(6r,12ar)-6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
CCG-100973
tadanafil
CS-1414
1,3-benzodioxol-5-yl(methyl)[?]dione
nsc 750236
tadalafil [usan:inn:ban]
742sxx0ict ,
unii-742sxx0ict
nsc 759172
tadalafil lilly
S1512
AKOS015892559
(6r,12ar)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6h,7h)-dione
gtpl7299
pyrazino(1',2':1,6)pyrido(3,4-b)indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6r-12ar)-
tadalafil [hsdb]
tadalafil [orange book]
tadalafil [vandf]
entadfi component tadalafil
tadalafil [mi]
tadalafil [ep monograph]
tadalafil [usp monograph]
tadalafil component of entadfi
tadalafil [who-dd]
tadalafil [usp-rs]
tadalafil [jan]
tadalafil [ema epar]
tadalafil [inn]
tadalafil [mart.]
HY-90009A
MLS006010126
AB42193
NC00223
SCHEMBL33333
tox21_112642_1
NCGC00263909-02
KS-1117 ,
cialis, tadalafil
(6r,12ar) 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
(6r,12 ar)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
(6r,12ar) 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino [1',2':1,6] pyrido[3,4-b]indole-1,4-dione
WOXKDUGGOYFFRN-IIBYNOLFSA-N
zalutia
(6r,12ar)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
tadalafil(cialis)
AB00639969_10
AB00639969_09
(2r,8r)-2-(2h-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11,13,15-tetraene-4,7-dione
(2r,8r)-2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
mfcd07771966
SR-05000001940-1
sr-05000001940
gf196960
tadalafil 1.0 mg/ml in acetonitrile
SW197603-2
tadalafil; cialis
Q424156
rel-(6r,12ar)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6h,7h)-dione
171488-03-2
tadalafilo
tadalafila
tadalafil (cialis)
EX-A2644
1242099-07-5
AMY10321
BRD-K93645900-001-04-8
AR-270/43507798
6-(1,3-benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydropyrazino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione
HMS3884G19
(6r,12ar)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1,2:1,6]pyrido[3,4-b]indole-1,4-dione
tadalafil specified impurity a
tadalafil (6r ,12as)- lilly
(-)-tadalafil (6r ,12as) diastereomer
(-)-tadalafil (6r)
tadalafil 100 microg/ml in acetonitrile
tadalafil- bio-x
BT164435
tadalafil (usp-rs)
tadalafil (ep monograph)
tadalafilum
g04be08
tadalafil (mart.)
tadliq
alyq
pyrazino
tadalafil (usp monograph)
Z1501485354

Research Excerpts

Overview

Tadalafil is a PDE5I which has been licensed for the treatment of erectile dysfunction (ED) since 2003, is effective from 30 minutes after administration and its efficacy is maintained for up to 36 hours. It is an illegal additive in antifatigue supplements.

ExcerptReferenceRelevance
"Tadalafil is a potential drug for reducing CDDP-induced spermatogenic dysfunction. "( Protective effects of tadalafil against cisplatin-induced spermatogenic dysfunction.
Chiba, K; Fujisawa, M; Ishida, T; Kaku, Y; Okada, K; Onishi, A; Sato, K, 2022)		2.48
"Tadalafil is a selective phosphodiesterase type-5 (PDE5) inhibitor that is approved for the treatment of men with erectile dysfunction (ED) and/or benign prostate hyperplasia (BPH) -associated symptoms. "( Tadalafil and Steroid Hormones Interactions in Adipose, Bone and Prostate Tissues: Focus on Translational Perspectives.
Antinozzi, C; Aversa, A; Di Luigi, L; Greco, EA; Sgrò, P, 2022)		3.61
"Tadalafil is an illegal additive in antifatigue supplements. "( Terahertz spectroscopic detection of antifatigue illegal additives in health care product matrices.
Li, H; Li, Y; Liu, B; Pan, W; Xiao, H; Yang, L; Zhang, B, 2022)		2.16
"Tadalafil is a PDE5I which has been licensed for the treatment of erectile dysfunction (ED) since 2003, is effective from 30 minutes after administration and its efficacy is maintained for up to 36 hours. "( Tadalafil Once a Day for Men with Erectile Dysfunction: Is It Superior than On-Demand Administration?
Fadhly, SF; Felizio, J; Mantiri, BJ; Prasetyo, DT; Rahardjo, HE; Raharja, PAR; Rahman, IA; Ringoringo, DRL; Tambunan, MP, 2019)		3.4
"Tadalafil (TDF), is a long-acting phosphodiesterase-5 (PDE5) inhibitor commonly used as treatment for erectile dysfunction."( Tadalafil alleviates cisplatin-induced reproductive toxicity through the activation of the Nrf2/HO-1 pathway and the inhibition of oxidative stress and apoptosis in male rats.
Abdel-Wahab, BA; Alkahtani, SA; Elagab, EAM, 2020)		2.72
"Tadalafil is considered to be a promising drug for PE."( Effect and mechanism of prophylactic use of tadalafil during pregnancy on l-NAME-induced preeclampsia-like rats.
Cai, W; Chen, S; Li, Y; Niu, X; Wang, B; Yang, N, 2020)		1.54
"Tadalafil (TDL) is an illegal additive drug found in drinks and functional foods that could threaten public health. "( Fluorescence based immunochromatographic sensor for rapid and sensitive detection of tadalafil and comparison with a gold lateral flow immunoassay.
Cui, G; Kuang, H; Liu, L; Suryoprabowo, S; Xu, C, 2021)		2.29
"Tadalafil is an effective, reversible, and competitive phosphodiesterase 5 inhibitor mainly used to treat erectile dysfunction. "( Pharmacokinetic and Bioequivalence Evaluation of 2 Tadalafil Tablets in Healthy Male Chinese Subjects Under Fasting and Fed Conditions.
Chen, JL; Hu, Y; Jiang, B; Lou, HG; Ruan, ZR; Shao, R; Yang, DD, 2022)		2.42
"Tadalafil is a widely prescribed phosphodiesterase-5 inhibitor that increases blood flow in other vascular territories."( Perfusion by Arterial Spin labelling following Single dose Tadalafil In Small vessel disease (PASTIS): study protocol for a randomised controlled trial.
Barrick, TR; Betteridge, S; Clarke, N; Haig, CE; Hainsworth, AH; Howe, FA; Isaacs, JD; Khan, U; Kruuse, C; Madigan, JB; Moynihan, B; Pauls, MMH; Pereira, AC; Rolfe, D; Rostrup, E; Trippier, S, 2017)		1.42
"Tadalafil therapy is an effective therapeutic option in patients with ESRD who undergo HD, not only for the treatment of ED, but also for ejaculatory function, with acceptable adverse effects."( The efficacy of low-dose tadalafil in patients undergoing hemodialysis with end-stage renal disease.
Akdeniz, E; Aşcı, R; Bolat, MS; Cinar, O; Özer, İ, 2017)		2.2
"Tadalafil is a promising phosphodiesterase (PDE) 5 inhibitor prescribed for erectile dysfunction (ED). "( Administration of daily 5 mg tadalafil improves endothelial function in patients with benign prostatic hyperplasia.
Amano, T; Earle, C; Imao, T; Kishikage, T; Matsumoto, Y, 2018)		2.21
"Tadalafil is a selective phosphodiesterase 5 inhibitor that dilates the maternal blood sinuses in the placenta, thereby facilitating the growth of the fetus."( Tadalafil treatment in mice for preeclampsia with fetal growth restriction has neuro-benefic effects in offspring through modulating prenatal hypoxic conditions.
Endoh, M; Furuhashi, F; Hosoda, H; Ikeda, T; Ikemura, K; Kamimoto, Y; Kaneda, MK; Kato, I; Kimura, T; Kondo, E; Ma, N; Magawa, S; Maki, S; Miyoshi, T; Nii, M; Okuda, M; Owa, T; Shimada, K; Tachibana, R; Tanaka, H; Tanaka, K; Tsuji, M; Umekawa, T; Yoshikawa, K, 2019)		2.68
"Tadalafil is a safe and tolerable therapy and unlike α1- adrenoceptors and 5-alpha reductase inhibitors, which can cause sexual dysfunctions, tadalafil improves sexual function."( Tadalafil for the treatment of benign prostatic hyperplasia.
De Nucci, G; Mónica, FZ, 2019)		2.68
"Tadalafil is a clinically relevant drug that blocks phosphodiesterase 5 with high specificity and is used to treat erectile dysfunction."( Phosphodiesterase 5 inhibition improves contractile function and restores transverse tubule loss and catecholamine responsiveness in heart failure.
Becker, LK; Caldwell, JL; Church, SJ; Dibb, KM; Eisner, DA; Hutchings, DC; Kirkwood, GJ; Lawless, M; Madders, GWP; Pearman, CM; Radcliffe, EJ; Smith, CER; Taylor, RF; Trafford, AW; Unwin, RD; Woods, LS, 2019)		1.24
"Tadalafil is a phosphodiesterase (PDE)-5 inhibitor that induces an increase in uterine blood flow by dilatation of blood vessels in cases of FGR with placental dysfunction, which improves FGR."( Phase-1 clinical study of tadalafil administered for selective fetal growth restriction in twin pregnancy.
Furuhashi, F; Ikeda, T; Kondo, E; Kubo, M; Magawa, S; Maki, S; Nii, M; Tanaka, H; Tanaka, K, 2021)		1.64
"Tadalafil is a drug from the phosphodiesterase-5 inhibitors (PDE-5) group, which is used to treat erectile dysfunction (ED), lower urinary tract symptoms (LUTS) caused by benign prostatic hyperplasia (BPH) and ED with LUTS in patients with BPH. "( [Safety of tadalafil in patients with cardiovascular comorbidities].
Bulygin, KV; Galimov, SN; Galimova, EF; Gaysina, GG; Nikitina, IL; Pavlov, VN, 2019)		2.35
"Tadalafil is a phosphodiesterase (PDE)-5 inhibitor recently approved by the United States Food and Drug Administration for lower urinary tracts symptoms (LUTS) associated with benign prostatic hyperplasia (BPH). "( Tadalafil: a phosphodiesterase-5 inhibitor for benign prostatic hyperplasia.
Baye, J; Cantrell, MA; Vouri, SM, 2013)		3.28
"Tadalafil is a phosphodiesterase type-5 (PDE5) inhibitor licensed for the treatment of erectile dysfunction (ED) in adult males (Cialis-Lilly) and for the management of pulmonary arterial hypertension (Adcirca-Lilly).(1) The 5mg tablet was licensed in November 2012 for the treatment of the signs and symptoms of benign prostatic hyperplasia (BPH) in adult males (Cialis 5mg-Lilly).(2) In this article, we consider the evidence for tadalafil and how its use fits with current management strategies for BPH. "( Tadalafil for benign prostatic hyperplasia.
, 2013)		3.28
"Tadalafil is a potent and selective phosphodiesterase type 5 inhibitor that provides effective treatment for erectile dysfunction (ED). "( Regional cerebral blood flow following single-dose and continuous-dose tadalafil after stroke.
Lampl, Y; Lorberboym, M; Makhline, E, 2014)		2.08
"Tadalafil is a long-acting and highly specific PDE5 inhibitor, which makes it the most attractive in its class for long-term management of patients with heart failure."( Tadalafil prevents acute heart failure with reduced ejection fraction in mice.
Chau, VQ; Hoke, NN; Kukreja, RC; Salloum, FN, 2014)		2.57
"Tadalafil once daily is a viable alternative to as-needed PDE5I therapy in men with ED. "( Comparative efficacy of tadalafil once daily in men with erectile dysfunction who demonstrated previous partial responses to as-needed sildenafil, tadalafil, or vardenafil.
Baygani, S; Burns, P; Goldfischer, E; Kim, E; Seftel, A, 2015)		2.17
"Tadalafil is a selective Phosphodiesterase-5 inhibitor that has been reported to have vasodilatory and antiproliferative effects on the pulmonary artery. "( Oral Tadalafil in Children with Pulmonary Arterial Hypertension.
Ala, S; Babazadeh, K; Rafati, M; Saeedi, M; Shiran, M; Shiva, A; Zamani, H, 2016)		2.39
"Tadalafil is a phosphodiesterase-5 inhibitor indicated for the treatment of erectile dysfunction. "( Tadalafil-loaded nanostructured lipid carriers using permeation enhancers.
Baek, JS; Cho, CW; Myung, CS; Pham, CV, 2015)		3.3
"Tadalafil (TDF) is a Biopharmaceutics Classification System (BCS) class II drug; the efficacy thereof is critically limited by inherent poor water solubility. "( Design of PVP/VA S-630 based tadalafil solid dispersion to enhance the dissolution rate.
Choi, JS; Park, JS, 2017)		2.19
"Tadalafil is a phosphodiesterase 5 (PDE5) inhibitor that is used to treat male erectile dysfunction. "( Pulmonary embolism after tadalafil ingestion.
Chen, HC; Chuang, SH; Wang, CS; Wang, CY, 2008)		2.09
"Tadalafil (Cialis)is a long-acting phosphodiesterase type-5 (PDE-5) inhibitor used to treat erectile dysfunction."( Tadalafil improves short-term memory by suppressing ischemia-induced apoptosis of hippocampal neuronal cells in gerbils.
Cho, HJ; Kim, BK; Kim, CJ; Kim, KH; Kim, SC; Kim, SE; Kim, SH; Kim, TS; Ko, IG; Shin, DH; Shin, MC; Shin, MS; Sung, YH, 2009)		2.52
"Tadalafil is a selective phosphodiesterase type 5 (PDE-5) inhibitor approved for the treatment of erectile dysfunction. "( EEG abnormalities during treatment with tadalafil, a phosphodiesterase type 5 inhibitor.
Akcin, S; Duman, T; Gorur, S; Guven, O; Melek, IM; Okuyucu, EE; Yilmazer, S, 2009)		2.06
"Tadalafil is a long-acting, selective inhibitor of phosphodiesterase 5 that has been shown to be effective at treating men with ED."( Evaluation of patient expectations and treatment satisfaction after 1-year tadalafil therapy for erectile dysfunction: the DETECT study.
Belger, M; Heidler, H; Perimenis, P; Roos, E; Roumeguere, T; Schmitt, H, 2009)		1.3
"Tadalafil is a long acting PDE-5 inhibitor largely unexplored for the treatment of iPAH."( Combination of sitaxentan and tadalafil for idiopathic pulmonary arterial hypertension following relapse on bosentan.
Faruqi, S; Fathi, H; Morice, AH, 2010)		1.37
"Tadalafil is a novel long-acting inhibitor of phosphodiesterase-5. "( Phosphodiesterase-5 inhibitor, tadalafil, protects against myocardial ischemia/reperfusion through protein-kinase g-dependent generation of hydrogen sulfide.
Abbate, A; Chau, VQ; Hoke, NN; Kukreja, RC; Ockaili, RA; Salloum, FN; Toldo, S; Varma, A, 2009)		2.08
"Tadalafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). "( Protective effects of tadalafil on experimental spinal cord injury in rats.
Güven, EO; Oktar, S; Ozgiray, E; Serarslan, Y; Söğüt, S; Yilmaz, N; Yönden, Z; Yurtseven, T, 2010)		2.12
"Tadalafil is a selective cyclic guanosine monophosphate-specific phosphodiesterase type 5 inhibitor that is effective in improving exercise ability, the time to clinical worsening and health-related quality of life (HR-QOL) scores in patients with pulmonary arterial hypertension (PAH). "( Tadalafil: in pulmonary arterial hypertension.
Croxtall, JD; Lyseng-Williamson, KA, 2010)		3.25
"Tadalafil is an effective and safe treatment for males with MS suffering from ED. "( Efficacy and safety of tadalafil for erectile dysfunction in patients with multiple sclerosis.
Del Popolo, G; Lombardi, G; Macchiarella, A, 2010)		2.11
"Tadalafil is a phosphodiesterase-5 inhibitor that is characterized by low solubility and high permeability. "( In sight into tadalafil - block copolymer binary solid dispersion: Mechanistic investigation of dissolution enhancement.
Mehanna, MM; Motawaa, AM; Samaha, MW, 2010)		2.16
"tadalafil). Rimonabant is a drug that was, at one time, approved for weight loss in Europe (although approval has been retracted), but not in the United States."( Identification of amino-tadalafil and rimonabant in electronic cigarette products using high pressure liquid chromatography with diode array and tandem mass spectrometric detection.
Allgire, J; Hadwiger, ME; Moore, T; Trehy, ML; Westenberger, B; Ye, W, 2010)		1.39
"Tadalafil is an efficient drug used to treat erectile dysfunction characterized by poor water solubility, which has a negative influence on its bioavailability. "( Tadalafil inclusion in microporous silica as effective dissolution enhancer: optimization of loading procedure and molecular state characterization.
Mehanna, MM; Motawaa, AM; Samaha, MW, 2011)		3.25
"Tadalafil is a selective inhibitor of phosphodiesterase type-5 (PDE-5) that was originally developed for the treatment of male erectile dysfunction and recently approved for the treatment of pulmonary arterial hypertension (PAH). "( Tadalafil for the treatment of pulmonary arterial hypertension.
Klinger, JR, 2011)		3.25
"Tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor and it is used in the treatment of pulmonary arterial hypertension and erectile dysfunction. "( Development and validation of a GC/MS method for the determination of tadalafil in whole blood.
Alevisopoulos, G; Athanaselis, S; Khraiwesh, A; Nikolaou, P; Papoutsis, I; Pistos, C; Spiliopoulou, C, 2011)		2.05
"Tadalafil is a phosphodiesterase-5 (PDE-5) inhibitor that was approved by the US Food and Drug Administration (FDA) in 2009 for the treatment of pulmonary arterial hypertension (PAH)."( Tadalafil: a long-acting phosphodiesterase-5 inhibitor for the treatment of pulmonary arterial hypertension.
Arif, SA; Poon, H, 2011)		3.25
"Tadalafil (Cialis) is a potent phosphodiesterase type 5 inhibitor that is widely used to treat erectile dysfunction. "( Optical coherence tomography in tadalafil-associated retinal toxicity.
Bandello, F; Coscas, F; Coscas, G; Soubrane, G; Souïed, E; Zucchiatti, I, )		1.86
"Tadalafil is an efficacious drug with a favorable side-effect profile and convenient mode of administration. "( Tadalafil for the treatment of pulmonary arterial hypertension.
Frey, MK; Lang, I, 2012)		3.26
"Tadalafil is an oral phosphodiesterase-5 inhibitor approved for PAH treatment. "( Tadalafil for the treatment of pulmonary arterial hypertension: a double-blind 52-week uncontrolled extension study.
Barst, RJ; Beardsworth, A; Botros, FT; Brundage, BH; Chan, M; Galiè, N; Ghofrani, HA; Oudiz, RJ; Simonneau, G, 2012)		3.26
"Tadalafil is a selective cyclic guanosine monophosphate-specific phosphodiesterase type 5 inhibitor. "( Tadalafil: in the treatment of signs and symptoms of benign prostatic hyperplasia with or without erectile dysfunction.
Curran, MP, 2012)		3.26
"Tadalafil appears to be an effective and a safe treatment option for patients with PAH."( Tadalafil as monotherapy and in combination regimens for the treatment of pulmonary arterial hypertension.
Schwarz, ER; Udeoji, DU, 2013)		2.55
"Tadalafil is a phosphodiesterase type 5 inhibitor in development by Lilly ICOS for the potential treatment of erectile dysfunction. "( Tadalafil Lilly ICOS.
Rotella, DP, 2003)		3.2
"Tadalafil (Cialis) is a new agent that has been studied in different patient populations."( Tadalafil: a new agent for erectile dysfunction.
Brock, GB, 2003)		2.48
"Tadalafil is a long-acting PDE-5 inhibitor, which is effective for up to 36 hr in the majority of men."( PDE-5 inhibition and sexual response: pharmacological mechanisms and clinical outcomes.
McKenna, KE; Rosen, RC, 2002)		1.04
"Tadalafil 20 mg is an effective and well-tolerated treatment for ED that has a period of responsiveness of up to 36 hours."( Efficacy of tadalafil for the treatment of erectile dysfunction at 24 and 36 hours after dosing: a randomized controlled trial.
Anglin, G; Giuliano, F; Padma-Nathan, H; Porst, H; Rosen, R; Varanese, L, 2003)		2.14
"Tadalafil appears to be a safe and effective treatment for men with ED."( Efficacy and tolerability of tadalafil, a novel phosphodiesterase 5 inhibitor, in treatment of erectile dysfunction.
Padma-Nathan, H, 2003)		1.33
"Tadalafil is a potent, selective, reversible phosphodiesterase 5 inhibitor under investigation for the treatment of erectile dysfunction (ED). "( Cardiovascular effects of tadalafil in patients on common antihypertensive therapies.
Emmick, JT; Kloner, RA; Mitchell, M, 2003)		2.06
"Tadalafil is a phosphodiesterase 5 (PDE5) inhibitor approved in >30 countries for the treatment of erectile dysfunction (ED). "( A multicenter, randomized, double-blind, crossover study of patient preference for tadalafil 20 mg or sildenafil citrate 50 mg during initiation of treatment for erectile dysfunction.
Ahuja, S; Denne, J; Govier, F; Kaufman, J; Kovalenko, P; Potempa, AJ, 2003)		1.99
"Tadalafil (Cialis) is an inhibitor of phosphodiesterase type 5, which mediates relaxation of vascular smooth muscle in the corpus cavernosum thus facilitating erection. "( Efficacy and treatment satisfaction with on-demand tadalafil (Cialis) in men with erectile dysfunction.
Basson, BR; Breza, J; Calomfirescu, N; Chen, J; Kopernicky, V; Kula, K; Skoumal, R, 2004)		2.02
"Tadalafil (TAD) is a new PDE5 inhibitor with a long half life that allows alternate day administration."( Chronic treatment with tadalafil improves endothelial function in men with increased cardiovascular risk.
Aversa, A; Fabbri, A; Fini, M; Rosano, GM; Spera, G; Vitale, C, 2005)		1.36
"Tadalafil is a potent reversible phosphodiesterase-5 inhibitor used for the treatment of erectile dysfunction. "( Determination of tadalafil in small volumes of plasma by high-performance liquid chromatography with UV detection.
Cheng, CL; Chou, CH, 2005)		2.11
"Tadalafil is a phosphodiesterase 5 (PDE5) inhibitor used for the treatment of erectile dysfunction (ED). "( Determining the earliest time within 30 minutes to erectogenic effect after tadalafil 10 and 20 mg: a multicenter, randomized, double-blind, placebo-controlled, at-home study.
Padma-Nathan, H; Pullman, W; Rosen, RC; Saikali, K; Shabsigh, R; Watkins, V, 2004)		2
"Tadalafil is a phosphodiesterase type 5 inhibitor for the treatment of erectile dysfunction (ED). "( Efficacy and safety of on-demand oral tadalafil in the treatment of men with erectile dysfunction in Taiwan: a randomized, double-blind, parallel, placebo-controlled clinical study.
Chen, KK; Costigan, TM; Emmick, JT; Huang, ST; Jiann, BP; Ju-Ton, H; Lee, SS; Lin, JS; Su, CK; Wang, CJ, 2004)		2.04
"Tadalafil is an inhibitor of phosphodiesterase type 5 used for the treatment of erectile dysfunction (ED). "( Efficacy and safety of on-demand tadalafil for the treatment of erectile dysfunction in South-East Asian men.
Chan, M; Cheong, NF; Ding, Q; Guo, YL; Lim, E; Pan, TM; Shen, W; Venugopalan, M; Wang, YX; Zhu, JC, 2006)		2.06
"Tadalafil is an effective treatment for erectile dysfunction after 3DCRT for prostatic carcinoma with successful intercourse reported in almost 50% of the patients, and it is well tolerated."( A randomized, double-blind, placebo-controlled, cross-over study to assess the efficacy of tadalafil (Cialis) in the treatment of erectile dysfunction following three-dimensional conformal external-beam radiotherapy for prostatic carcinoma.
Hop, WC; Incrocci, L; Slagter, C; Slob, AK, 2006)		2
"Tadalafil is a phosphodiesterase type 5 inhibitor with documented efficacy in the treatment of erectile dysfunction (ED)."( A comparison of the efficacy and tolerability of tadalafil 10 mg and 20 mg in Japanese patients with severe erectile dysfunction.
Fujimoto, K; Imaoka, T; Marumo, K; McGill, J; Stothard, D; Watts, S, 2007)		2.04
"Tadalafil (Cialis) is a known oral selective phosphodiesterase-5 inhibitor used widely in the management of erectile dysfunction. "( Tadalafil as an in vitro sperm motility stimulant.
Mostafa, T, 2007)		3.23
"Tadalafil is an effective drug in treating erectile dysfunction (ED), and its clinical efficacy has been confirmed by a great many researches. "( [Efficacy of tadalafil for erectile dysfunction: an updated review].
Bai, WJ, 2007)		2.15
"Tadalafil is an effective tool for treating ED in diabetes patients. "( Effect of tadalafil on erectile dysfunction in male patients with diabetes mellitus.
Antonijević, N; Dabetić, M; Dimitrijević-Srecković, V; Dordević, P; Gostiljac, D; Matanović, D; Milić, G; Nale, D; Nisić, T; Popović, S; Vujović, S, 2007)		2.18
"Tadalafil is an inhibitor of phosphodiesterase 5, approved for the treatment of erectile dysfunction. "( The cardiovascular safety of tadalafil.
Kieback, A; Kloner, RA; Reffelmann, T, 2008)		2.08
"Tadalafil is a phosphodiesterase V inhibitor that is used for treatment of erectile dysfunction by enhancing vascular smooth muscle relaxation."( The effects of tadalafil on axial-pattern skin flap survival in rats.
Chang, H; Minn, KW; Oh, M, 2008)		1.42
"Tadalafil is an effective treatment for ED in routine clinical practice. "( Therapeutic response after first month of tadalafil treatment predicts 12 months treatment continuation in patients with erectile dysfunction: results from the DETECT study.
Arver, S; Belger, M; Bitton, A; Roumeguère, T; Schmitt, H; Verheyden, B, 2008)		2.05
"Tadalafil is a new and clinically available phosphodiesterase-5 inhibitor that, aside from causing pulmonary vasodilation, has been shown to increase cardiac output in pulmonary hypertensive adults."( Tadalafil improves oxygenation in a model of newborn pulmonary hypertension.
Belik, J; Colvero, M; Fiori, H; Fiori, RM; Tessler, RB; Zadinello, M, 2008)		2.51
"Tadalafil is an oral phosphodiesterase type-5 inhibitor for male erectile dysfunction (ED). "( [Evaluation of tadalafil for the treatment of erectile dysfunction].
Liu, ZY; Sun, YH, 2008)		2.14
"Tadalafil is an inhibitor of phosphodiesterase type 5, and is currently undergoing regulatory review in the US and in Europe. "( Tadalafil (Cialis) for men with erectile dysfunction.
Cartledge, J; Eardley, I, 2002)		3.2

Effects

Tadalafil has a potentially preventive effect in treatment of cerebral vasospasm following subarachnoid bleeding. It has a higher stone expulsion rate than tamsulosin as a medical expulsive therapy for patients with distal stones from 5 to 10 mm without differences in side effects. Tadalafill has a potential for inhibiting neutrophil infiltration in renal IRI.

Tadalafil has been reported to exhibit antioxidant effects and is widely used in clinical practice to treat benign prostatic hyperplasia and erectile dysfunction. The drug has a higher stone expulsion rate than tamsulosin as a medical expulsive therapy for patients with distal stones.

ExcerptReferenceRelevance
"Tadalafil has a higher stone expulsion rate than tamsulosin as a medical expulsive therapy for patients with distal stones from 5 to 10 mm without differences in side effects."( Tamsulosin vs. Tadalafil as medical expulsive therapy for distal ureteral stones: a systematic review and meta-analysis.
Artifon, ELA; Belkovsky, M; da Cruz, JAS; Otoch, JP; Passerotti, CC; Zogaib, GV, )		1.93
"Tadalafil has a potential for inhibiting neutrophil infiltration in renal IRI."( Evaluation of Neutrophil Dynamics Change by Protective Effect of Tadalafil After Renal Ischemia/Reperfusion Using In Vivo Real-time Imaging.
Araki, M; Kashihara, N; Kidokoro, K; Maruyama, Y; Mitsui, Y; Nasu, Y; Sadahira, T; Sogawa, Y; Wada, K; Watanabe, M; Watanabe, T; Yoshinaga, K, 2022)		1.68
"Tadalafil has a manageable safety profile up to an MTD of 40 mg/d."( Phase-1 clinical study of tadalafil administered for selective fetal growth restriction in twin pregnancy.
Furuhashi, F; Ikeda, T; Kondo, E; Kubo, M; Magawa, S; Maki, S; Nii, M; Tanaka, H; Tanaka, K, 2021)		2.36
"Tadalafil has a significantly higher stone expulsion rate than tamsulosin when used as a medical expulsive therapy for distal ureteral stones sized 5-10 mm. "( Tamsulosin versus tadalafil as a medical expulsive therapy for distal ureteral stones: A prospective randomized study.
Acharya, GB; Basnet, RB; Kc, HB; Shah, AK; Shrestha, A; Shrestha, PM, 2016)		2.21
"Tadalafil has a lowering affect on RI and PI in experimentally created PUUO."( Effect of tadalafil on renal resistivity and pulsatility index in partial ureteral obstruction.
Akgul, T; Aklan, Z; Ayyildiz, A; Bumin, A; Germiyanoğlu, C; Karaguzel, E; Kaya, M, 2009)		2.2
"tadalafil has a potentially preventive effect in treatment of cerebral vasospasm following subarachnoid bleeding."( The effect of phosphodiesterase inhibitor tadalafil on vasospasm following subarachnoid hemorrhage in an experimental rabbit model.
Akalan, N; Bilginer, B; Isikay, AI; Narin, F; Onal, MB; Soylemezoglu, F, 2011)		2.08
"Tadalafil has a greater affinity (10,000-fold) for PDE-5 compared with the other PDE inhibitors and has a t(½) of 17.5 hours."( Tadalafil: a long-acting phosphodiesterase-5 inhibitor for the treatment of pulmonary arterial hypertension.
Arif, SA; Poon, H, 2011)		2.53
"Tadalafil has a longer duration of action than sildenafil and vardenafil."( Comparison of clinical trials with sildenafil, vardenafil and tadalafil in erectile dysfunction.
Doggrell, SA, 2005)		1.29
"Tadalafil has a longer half-life than sildenafil or vardenafil, and a longer duration of action than sildenafil and vardenafil."( Do vardenafil and tadalafil have advantages over sildenafil in the treatment of erectile dysfunction?
Doggrell, S, )		1.19
"Tadalafil has been reported to exhibit antioxidant effects and is widely used in clinical practice to treat benign prostatic hyperplasia and erectile dysfunction."( Protective effects of tadalafil against cisplatin-induced spermatogenic dysfunction.
Chiba, K; Fujisawa, M; Ishida, T; Kaku, Y; Okada, K; Onishi, A; Sato, K, 2022)		1.76
"Tadalafil has positive effects on neurodevelopment and antioxidant defense system, but there is no information for its possible role during gestation on reflexive motor behavior in offspring. "( Parental exposure of Tadalafil has beneficial effect on reflexive motor behaviors in mice offspring.
Asghari, A; Hassanpour, S; Imani, MH; Khaksar, E, 2022)		2.48
"Tadalafil has been demonstrated to improve vascular parameters."( Tadalafil Improves Haemodynamics and Arterial Stiffness but Not Flow- Mediated Dilation in Grade 1 Obesity. A Single-dose, Placebo-controlled Clinical Trial.
Barocio-Pantoja, M; Cardona-Müller, D; Cardona-Muñoz, EG; González-Radillo, OI; Grover-Páez, F; Larios-Cárdenas, M; Trujillo-Quirós, J, 2022)		2.89
"Tadalafil has a higher stone expulsion rate than tamsulosin as a medical expulsive therapy for patients with distal stones from 5 to 10 mm without differences in side effects."( Tamsulosin vs. Tadalafil as medical expulsive therapy for distal ureteral stones: a systematic review and meta-analysis.
Artifon, ELA; Belkovsky, M; da Cruz, JAS; Otoch, JP; Passerotti, CC; Zogaib, GV, )		1.93
"As tadalafil has the potential to improve atherosclerosis, we evaluated the relationship between LUTS and endothelial function using FMD, and the effects of tadalafil."( [EVALUATING THE RELATIONSHIP BETWEEN LOWER URINARY TRACT SYMPTOMS AND ENDOTHELIAL FUNCTION USING FLOW-MEDIATED DILATION, AND THE EFFECTS OF TADALAFIL].
Higashi, Y; Kuwahara, Y; Nakamura, K; Shimura, H; Takeda, M; Tsukamoto, T; Watanabe, N, 2020)		1.27
"Tadalafil has a potential for inhibiting neutrophil infiltration in renal IRI."( Evaluation of Neutrophil Dynamics Change by Protective Effect of Tadalafil After Renal Ischemia/Reperfusion Using In Vivo Real-time Imaging.
Araki, M; Kashihara, N; Kidokoro, K; Maruyama, Y; Mitsui, Y; Nasu, Y; Sadahira, T; Sogawa, Y; Wada, K; Watanabe, M; Watanabe, T; Yoshinaga, K, 2022)		1.68
"Tadalafil has been recently seen to also play a role in the treatment of urinary symptoms caused by benign prostatic hyperplasia."( Effectiveness of the addition of tadalafil to tamsulosin in the treatment of acute urinary retention in patients with benign prostatic hyperplasia: A randomized clinical trial.
Ameli, M; Ameli, Z; Baghani Aval, H, 2018)		1.48
"Tadalafil has a manageable safety profile up to an MTD of 40 mg/d."( Phase-1 clinical study of tadalafil administered for selective fetal growth restriction in twin pregnancy.
Furuhashi, F; Ikeda, T; Kondo, E; Kubo, M; Magawa, S; Maki, S; Nii, M; Tanaka, H; Tanaka, K, 2021)		2.36
"Tadalafil has demonstrated efficacy in treating both conditions."( Effects of tadalafil on lower urinary tract symptoms secondary to benign prostatic hyperplasia and on erectile dysfunction in sexually active men with both conditions: analyses of pooled data from four randomized, placebo-controlled tadalafil clinical stu
Esler, A; Porst, H; Roehrborn, CG; Secrest, RJ; Viktrup, L, 2013)		1.5
"Tadalafil has regulatory approval for the treatment of men with signs/symptoms of benign prostatic hyperplasia with and without erectile dysfunction. "( Direct effects of tadalafil on lower urinary tract symptoms versus indirect effects mediated through erectile dysfunction symptom improvement: integrated data analyses from 4 placebo controlled clinical studies.
Brock, GB; Donatucci, C; McVary, KT; Ni, X; Roehrborn, CG; Viktrup, L; Watts, S; Wong, DG, 2014)		2.18
"Tadalafil has modest symptomatic efficacy at best."( Tadalafil and benign prostatic hypertrophy. Too risky.
, 2014)		2.57
"Tadalafil has a significantly higher stone expulsion rate than tamsulosin when used as a medical expulsive therapy for distal ureteral stones sized 5-10 mm. "( Tamsulosin versus tadalafil as a medical expulsive therapy for distal ureteral stones: A prospective randomized study.
Acharya, GB; Basnet, RB; Kc, HB; Shah, AK; Shrestha, A; Shrestha, PM, 2016)		2.21
"Tadalafil has a lowering affect on RI and PI in experimentally created PUUO."( Effect of tadalafil on renal resistivity and pulsatility index in partial ureteral obstruction.
Akgul, T; Aklan, Z; Ayyildiz, A; Bumin, A; Germiyanoğlu, C; Karaguzel, E; Kaya, M, 2009)		2.2
"tadalafil has a potentially preventive effect in treatment of cerebral vasospasm following subarachnoid bleeding."( The effect of phosphodiesterase inhibitor tadalafil on vasospasm following subarachnoid hemorrhage in an experimental rabbit model.
Akalan, N; Bilginer, B; Isikay, AI; Narin, F; Onal, MB; Soylemezoglu, F, 2011)		2.08
"Tadalafil has a greater affinity (10,000-fold) for PDE-5 compared with the other PDE inhibitors and has a t(½) of 17.5 hours."( Tadalafil: a long-acting phosphodiesterase-5 inhibitor for the treatment of pulmonary arterial hypertension.
Arif, SA; Poon, H, 2011)		2.53
"Tadalafil has been well tolerated."( Efficacy and tolerability of tadalafil, a novel phosphodiesterase 5 inhibitor, in treatment of erectile dysfunction.
Padma-Nathan, H, 2003)		1.33
"Tadalafil has a longer duration of action than sildenafil and vardenafil."( Comparison of clinical trials with sildenafil, vardenafil and tadalafil in erectile dysfunction.
Doggrell, SA, 2005)		1.29
"Tadalafil has the longest duration of action (up to 36 hours); this feature can be both beneficial (greater sexual spontaneity) or possibly detrimental (greater exposure to drug, delayed adverse events)."( Clinical monograph for drug formulary review: erectile dysfunction agents.
Campbell, HE, 2005)		1.05
"Tadalafil has not been investigated in a large clinical trial with a South-east Asian population."( Efficacy and safety of on-demand oral tadalafil in the treatment of men with erectile dysfunction in Taiwan: a randomized, double-blind, parallel, placebo-controlled clinical study.
Chen, KK; Costigan, TM; Emmick, JT; Huang, ST; Jiann, BP; Ju-Ton, H; Lee, SS; Lin, JS; Su, CK; Wang, CJ, 2004)		1.32
"Tadalafil has a longer half-life than sildenafil or vardenafil, and a longer duration of action than sildenafil and vardenafil."( Do vardenafil and tadalafil have advantages over sildenafil in the treatment of erectile dysfunction?
Doggrell, S, )		1.19

Actions

Tadalafil therapy may enhance erectile function, improve anxiety, depression and quality of life. It is well tolerated by men with cirrhosis (CTP score < 10) and ED. The drug might inhibit kidney injury progression by preventing damage to podocytes and dysfunction of the glomerular filtration barrier.

ExcerptReferenceRelevance
"Tadalafil therapy may enhance erectile function, improve anxiety, depression and quality of life; and is well tolerated by men with cirrhosis (CTP score < 10) and ED. "( Tadalafil improves erectile dysfunction and quality of life in men with cirrhosis: a randomized double blind placebo controlled trial.
Arora, V; Benjamin, J; Bhardwaj, A; Choudhary, A; Jagdish, RK; Jindal, A; Kamaal, A; Kumar, G; Kumar, M; Maiwall, R; Rajan, V; Sarin, SK; Shasthry, SM, 2023)		3.8
"Tadalafil led to an increase in the NO levels, but a statistically significant NO release increase was found only at the highest dose and highest CPP."( Tadalafil in Increasing Doses: The Influence on Coronary Blood Flow and Oxidative Stress in Isolated Rat Hearts.
Banjac, NM; Jakovljević, VL; Prodanović, DV; Stilinović, NP; Tomas Petrović, AD; Vasović, LV; Vasović, VM, 2022)		2.89
"Tadalafil might inhibit kidney injury progression by preventing damage to podocytes and dysfunction of the glomerular filtration barrier."( Protective effects of tadalafil on damaged podocytes in an adriamycin-induced nephrotic syndrome model.
Furukawa-Hibi, Y; Hotta, Y; Kataoka, T; Kimura, K; Naiki-Ito, A; Sanagawa, A; Takahashi, S; Tomita, N, 2022)		1.76
"Tadalafil significantly promotes functional recovery after renal IR injury and effectively inhibits the induction of pro-inflammatory and inflammatory mediators. "( The Association of Phosphodiesterase 5 Inhibitor on Ischemia-Reperfusion Induced Kidney Injury in Rats.
Chung, MK; Kim, JH; Nam, JK; Park, SW, 2020)		2
"Tadalafil improves lower urinary tract symptoms (LUTS) including nocturia. "( Tadalafil Improves Nocturia and Nocturia-Related Quality of Life in Patients with Benign Prostatic Hyperplasia (KYU-PRO Study).
Eto, M; Mimata, H; Miyazato, M; Nishii, H; Oshiro, T; Saito, S; Sumino, Y; Takahashi, R; Yoshida, M, 2020)		3.44
"Tadalafil did not inhibit spontaneous seminal emission or electrical field stimulation-induced seminal vesicle contraction in normal rats. "( Comparison of the Effects of Tadalafil and α
Fujimura, M; Fukui, T; Oka, M; Oyama, T; Yoshifuji, M; Yoshinaga, R, 2019)		2.25
"Tadalafil displays important neuroprotective effects in experimental models of neurodegenerative diseases, however its mechanisms of action remain poorly understood. "( Tadalafil restores long-term memory and synaptic plasticity in mice with hepatic encephalopathy.
Araújo, SMR; Duarte-Silva, E; França, MER; Lós, DB; Oliveira, WH; Peixoto, CA; Ramos, RKLG, 2019)		3.4
"Tadalafil can enhance Rituximab treatment efficacy by improving the microvascular permeability in mice brain lymphoma."( Phosphodiesterase type 5 inhibitor Tadalafil increases Rituximab treatment efficacy in a mouse brain lymphoma model.
Chen, W; Liu, Y; Mao, Y; Meng, K; Qiao, X; Wang, R; Zhang, Q, 2015)		1.42
"Tadalafil did not produce any significant change in MAP, whereas tempol led to a significant fall (p < 0.01) in MAP."( Long-acting phosphodiesterase 5 inhibitor, tadalafil, and superoxide dismutase mimetic, tempol, protect against acute hypoxia-induced pulmonary hypertension in rats.
Fahim, M; Kotwani, A; Rashid, M, 2012)		1.36
"Tadalafil improved lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH; LUTS/BPH) in clinical studies but has not been evaluated together with an active control in an international clinical study."( Monotherapy with tadalafil or tamsulosin similarly improved lower urinary tract symptoms suggestive of benign prostatic hyperplasia in an international, randomised, parallel, placebo-controlled clinical trial.
Cox, D; Giuliano, F; Mirone, V; Oelke, M; Viktrup, L; Xu, L, 2012)		2.16
"Tadalafil group had lower rates of severe HAI compared with controls (4% vs 26%, p = 0.03), mostly because of decreased high-altitude pulmonary edema rates (4% vs 22%, p = 0.06)."( Tadalafil and acetazolamide versus acetazolamide for the prevention of severe high-altitude illness.
Caine, Y; Hermesh, H; Leshem, E; Maaravi, Y; Rosenberg, E; Schwartz, E, )		2.3
"Tadalafil did not increase the rate of MI or cardiac mortality compared with reported rates from epidemiological studies."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		1.34
"Tadalafil promotes a mobilization of PCs and improves endothelial function in ED patients."( Circulating endothelial progenitor cells and endothelial function after chronic Tadalafil treatment in subjects with erectile dysfunction.
Caretta, N; De Toni, L; Ferlin, A; Foresta, C; Galan, A; Lana, A; Vinanzi, C, )		1.08
"Tadalafil did not increase baseline flux (81.0+/-73.0 vs 91.3+/-114.0 arbitrary unit (AU), P=0.57), E(max) (280.0+/-107.6 vs 279.5+/-119.8 AU, P=0.94), ET(50) (25.4+/-4.4 vs 26.6+/-5.7 degrees C, P=0.62), or ET(90) (21.2+/-3.9 vs 21.8+/-5.0 degrees C, P=0.78), (cycle 1 values presented)."( The effects of tadalafil on cold-induced vasoconstriction in patients with Raynaud's phenomenon.
Friedman, EA; Harris, PA; Kurnik, D; Stein, CM; Wood, AJ, 2007)		1.41

Treatment

Tadalafil treatment normalized the low response to papaverine and high drop rate in the intracavernosal pressure measured by cavernosometry after CNR. Treatment significantly improved all domains of the IIEF from baseline, including the erectile function domain (change = 8.8, end point = 21.6; P < 0.001)

ExcerptReferenceRelevance
"Tadalafil treatment was able to decrease in hypertrophy and improve the LV function restoring cardiac function."( Tadalafil treatment improves cardiac, renal and lower urinary tract dysfunctions in rats with heart failure.
Andrade, DR; Claudino, MA; Goncalves, TT; Janussi, SC; Krikorian, K; Mora, AG; Priviero, FBM, 2022)		2.89
"The tadalafil-treated groups were orally administered 10 mg/kg tadalafil for 2 weeks."( Protective effects of tadalafil on damaged podocytes in an adriamycin-induced nephrotic syndrome model.
Furukawa-Hibi, Y; Hotta, Y; Kataoka, T; Kimura, K; Naiki-Ito, A; Sanagawa, A; Takahashi, S; Tomita, N, 2022)		1.52
"TheTADAlafil treatment for Fetuses with early-onset growth Restriction: multicentrer, randomizsed, phase II trial (TADAFER II) study showed the possibility of prolonging the pregnancy period in cases of early-onset fetal growth restriction; however, it was an open-label study. "( Tadalafil treatment for fetuses with early-onset growth restriction: a protocol for a multicentre, randomised, placebo-controlled, double-blind phase II trial (TADAFER IIb).
Aoki, S; Aoki, Y; Endo, M; Ikeda, T; Kasai, M; Kawamura, H; Kikuchi, N; Kinjo, T; Kotani, T; Kotera, M; Maegawa, Y; Maki, S; Nagao, K; Nakamura, K; Nakata, M; Nii, M; Nishimura, Y; Ogura, T; Sekizawa, A; Suga, S; Takakura, S; Takano, M; Tamaru, S; Tanaka, H; Tanaka, K; Tanaka, Y; Ushida, T; Yasuhi, I; Yasui, O; Yoshida, Y, 2022)		2.79
"Tadalafil treatment improves OAB symptoms and urodynamic parameters by decreasing oxidative stress level."( Efficacy of Tadalafil Therapy and Changes in Oxidative Stress Levels in Male Patients with Lower Urinary Tract Symptoms and Overactive Bladder.
Araki, K; Matsuo, T; Miyata, Y; Mukae, Y; Ohba, K; Otsubo, A; Sakai, H, 2020)		2.38
"The tadalafil treatment was only protective for cellular degeneration (p = 0.140)."( Comparison of the protective effects of sildenafil, vardenafil and tadalafil treatments in ischemia-reperfusion injury in rat ovary.
Akalın, EE; Anğın, AD; Basak, K; Cikman, MS; Kaptanagasi, AO; Sakin, O, 2019)		1.23
"Tadalafil treatment is safe for pregnant women with HDP. "( Tadalafil treatment for preeclampsia (medication in preeclampsia; MIE): a multicenter phase II clinical trial.
Endoh, M; Furuhashi, F; Ikeda, T; Kaneda, MK; Kimura, T; Kotani, T; Magawa, S; Maki, S; Nii, M; Nishimura, Y; Ogura, T; Sekizawa, A; Tanaka, H; Tanaka, K; Tsuji, M, 2021)		3.51
"Tadalafil 5mg daily treatment for 3 months did not result in significant modifications to VPS and AS. "( [Effect of tadalafil 5mg daily treatment on penile haemodynamics in patients with erectile dysfunction].
Gasanz, C; Moreno-Mendoza, D; Peraza, MF; Ruiz-Castañé, E; Sánchez-Curbelo, J; Sarquella, J; Villegas, JF, )		1.96
"Tadalafil treatment significantly suppressed the severity of the lesions."( Effect of tadalafil on chronic pelvic pain and prostatic inflammation in a rat model of experimental autoimmune prostatitis.
Kurita, M; Numakura, Y; Oka, M; Okamoto, K; Yamaguchi, H, 2018)		1.6
"Tadalafil treatment for PE with FGR reduced the expression of hypoxia-inducible factor-2α in the placenta and in the brain of the FGR fetus."( Tadalafil treatment in mice for preeclampsia with fetal growth restriction has neuro-benefic effects in offspring through modulating prenatal hypoxic conditions.
Endoh, M; Furuhashi, F; Hosoda, H; Ikeda, T; Ikemura, K; Kamimoto, Y; Kaneda, MK; Kato, I; Kimura, T; Kondo, E; Ma, N; Magawa, S; Maki, S; Miyoshi, T; Nii, M; Okuda, M; Owa, T; Shimada, K; Tachibana, R; Tanaka, H; Tanaka, K; Tsuji, M; Umekawa, T; Yoshikawa, K, 2019)		2.68
"Tadalafil can be a treatment option in cases where there is concern about negative effects on seminal emission."( Comparison of the Effects of Tadalafil and α
Fujimura, M; Fukui, T; Oka, M; Oyama, T; Yoshifuji, M; Yoshinaga, R, 2019)		2.25
"Tadalafil treatment increased bladder blood flow, and nicotine-treated rats had increased voiding interval and micturition volume."( Nicotine-induced hypoxia in rat urothelium deteriorates bladder storage functions.
Domen, T; Imamura, T; Ishizuka, O; Minagawa, T; Nagai, T; Ogawa, T; Suzuki, T; Ueno, M, 2019)		1.24
"Tadalafil treatment regulated the inflammation signaling pathways restoring learning and spatial memory."( Tadalafil restores long-term memory and synaptic plasticity in mice with hepatic encephalopathy.
Araújo, SMR; Duarte-Silva, E; França, MER; Lós, DB; Oliveira, WH; Peixoto, CA; Ramos, RKLG, 2019)		2.68
"Tadalafil treated bladders measured lower collagen content towards the end of the study, indicating an antifibrotic effect."( Urodynamic improvements following oral medical therapy for partial bladder outlet obstruction in an animal model.
Maciejewski, CC; Metcalfe, PD; Tredget, EE, 2015)		1.14
"Tadalafil treatment in this setting appears to have an antifibrotic effect."( Urodynamic improvements following oral medical therapy for partial bladder outlet obstruction in an animal model.
Maciejewski, CC; Metcalfe, PD; Tredget, EE, 2015)		1.14
"The tadalafil treatment improved erectile function (P = 0.0028), but had no effect on the inhibitory effects of serum from ED patients on the CACs and CFUs derived from healthy men."( Tadalafil treatment had a modest effect on endothelial cell damage and repair ability markers in men with erectile dysfunction and vascular risk.
Amicarelli, F; Barbonetti, A; D'Andrea, S; D'Angeli, A; Falone, S; Francavilla, F; Francavilla, S; Necozione, S; Pelliccione, F; Pezzella, A, )		2.05
"Tadalafil treatment reversed this effect."( The effect of methamphetamine on an animal model of erectile function.
Davies, KP; Martinez, LR; Nosanchuk, JD; Tar, MT, 2014)		1.12
"Tadalafil-treated diabetic mice demonstrated significantly improved left ventricular function, which is associated with increased cardiac SIRT1 activity."( Chronic inhibition of phosphodiesterase 5 with tadalafil attenuates mitochondrial dysfunction in type 2 diabetic hearts: potential role of NO/SIRT1/PGC-1α signaling.
Aluri, HS; Koka, S; Kukreja, RC; Lesnefsky, EJ; Xi, L, 2014)		1.38
"Tadalafil treatment was well tolerated and significantly reduced both MDSCs and Treg concentrations in the blood and in the tumor (P < 0.05)."( Tadalafil reduces myeloid-derived suppressor cells and regulatory T cells and promotes tumor immunity in patients with head and neck squamous cell carcinoma.
Borrello, I; Califano, J; De la Fuente, AC; Gomez, C; Nazarian, R; Reis, IM; Sargi, Z; Serafini, P; Vella, JL; Weed, DT, 2015)		2.58
"AI-tadalafil rats were treated with tadalafil (2 mg/kg/day) orally for 8 weeks after AI."( Protective effect of tadalafil on the functional and structural changes of the rat ventral prostate caused by chronic pelvic ischemia.
Andersson, KE; Nomiya, M; Sawada, N; Zarifpour, M, 2015)		1.25
"Tadalafil treated mice traveled less distance in the center and the mean speed of tadalafil treated aged mice was significantly lower than the tadalafil treated young mice in open field test."( Tadalafil enhances working memory, and reduces hippocampal oxidative stress in both young and aged mice.
Al-Amin, MM; Alam, MA; Alam, T; Didar, RR; Hasan, AT; Hasan, SM; Hossain, I; Rahman, MM, 2014)		2.57
"In tadalafil-treated podocytes, we examined the interaction between H2S and nitric oxide (NO)."( Tadalafil Integrates Nitric Oxide-Hydrogen Sulfide Signaling to Inhibit High Glucose-induced Matrix Protein Synthesis in Podocytes.
Choudhury, GG; Feliers, D; Gorin, Y; Kasinath, BS; Lee, HJ; Mariappan, MM; Sataranatarajan, K, 2015)		2.37
"Tadalafil treatment resulted in greater IPSS improvements in men with lower baseline estradiol-17β versus those with higher baseline estradiol-17β."( Do baseline estrogen and testosterone affect lower urinary tract symptoms (LUTS) prior to or after pharmacologic treatment with tadalafil?
Egan, KB; McVary, K; Miner, MM; Ni, X; Roehrborn, CG; Rosen, RC; Suh, M; Wittert, G; Wong, DG, 2015)		1.34
"Tadalafil-treated men had 2.8 times significantly increased adjusted odds of being combined responders vs non-responders (P < 0.001)."( Erectile dysfunction and lower urinary tract symptoms associated with benign prostatic hyperplasia (LUTS/BPH) combined responders to tadalafil after 12 weeks of treatment.
Egan, KB; Miner, MM; Ni, X; Roehrborn, CG; Rosen, RC; Wong, DG, 2016)		1.36
"Tadalafil treatment had a protective effect against the formation of urethral stricture in rabbit model. "( Effect of Tadalafil on Prevention of Urethral Stricture After Urethral Injury: An Experimental Study.
Aktas, C; Bozdemir, Y; Kurt, O; Ozcaglayan, O; Yazici, CM; Yesildag, E, 2016)		2.28
"Tadalafil treatment also markedly increased local blood flow and the density of FITC-dextran perfused vessels in the sciatic nerve concomitantly with increased intraepidermal nerve fiber density."( Tadalafil Promotes the Recovery of Peripheral Neuropathy in Type II Diabetic Mice.
Chopp, M; Jia, L; Lu, M; Lu, X; Szalad, A; Wang, L; Zhang, RL; Zhang, ZG, 2016)		2.6
"Tadalafil treatment improved golden retriever muscular dystrophy histopathological features, decreased levels of the cation channel TRPC6, increased total threonine phosphorylation status of TRPC6, decreased m-calpain levels and indicators of calpain target proteolysis, and elevated levels of utrophin."( Tadalafil Treatment Delays the Onset of Cardiomyopathy in Dystrophin-Deficient Hearts.
Forbes, SC; Hammers, DW; Shima, A; Sleeper, MM; Sweeney, HL; Walter, GA, 2016)		2.6
"Tadalafil treatment reduced the upregulation of mRNA levels of fibrosis markers, the decrease of bladder compliance and the increase of collagen concentration at the late phase of SCI."( Effects of an alpha1A/D-adrenoceptor antagonist, naftopidil, and a phosphodiesterase type 5 inhibitor, tadalafil, on urinary bladder remodeling in rats with spinal cord injury.
Kadekawa, K; Kawamorita, N; Majima, T; Mori, K; Okada, H; Sugaya, K; Tyagi, P; Yoshimura, N; Yoshizawa, T, 2017)		1.39
"Tadalafil treatment significantly attenuated these effects."( Erectile dysfunction in a murine model of sleep apnea.
Gozal, D; Lei, Z; Nozdrachev, AD; Rao, CV; Shah, ZA; Soukhova-O'Hare, GK, 2008)		1.07
"Tadalafil treatment improved short-term memory by suppressing ischemia-induced apoptotic neuronal cell death in the hippocampal CA1 region, and decreased cGMP level."( Tadalafil improves short-term memory by suppressing ischemia-induced apoptosis of hippocampal neuronal cells in gerbils.
Cho, HJ; Kim, BK; Kim, CJ; Kim, KH; Kim, SC; Kim, SE; Kim, SH; Kim, TS; Ko, IG; Shin, DH; Shin, MC; Shin, MS; Sung, YH, 2009)		2.52
"Tadalafil-treated animals exhibited greater Pao(2) throughout the course of reperfusion (P = .001) Mean pulmonary artery pressure was lower in tadalafil-treated animals (22 vs 40 mm Hg; P = .04)."( Long-acting oral phosphodiesterase inhibition preconditions against reperfusion injury in an experimental lung transplantation model.
Baumgartner, WA; Champion, HC; Shah, AS; Weiss, ES; Williams, JA, 2009)		1.07
"Tadalafil treatment accelerated Akt phosphorylation in cardiac tissue and decreased myocyte apoptosis."( Long-acting phosphodiesterase-5 inhibitor, tadalafil, induces sustained cardioprotection against lethal ischemic injury.
Ahmad, N; Ali, AK; Ashraf, M; Wang, Y, 2009)		1.34
"tadalafil treatment across four distinct geographies: Asia, Australia/New Zealand (ANZ), Central Eastern Europe/Middle East (CEE/ME), and Latin America (LA)."( Timing of dose relative to sexual intercourse attempt in previous sildenafil citrate users treated with tadalafil: a geographical comparison from a single arm, open-label study.
Abdo, CH; Gallagher, GL; Glina, S; Hernandez-Serrano, R; Lenero, E; Rampazzo, C; Rubio-Aurioles, E; Sotomayor, M; West, TM, 2009)		1.29
"Tadalafil treatment significantly improved the IPSS obstructive subscores (tadalafil 2.5, 5, 10, 20 mg with percentage changes of 24%, 31%, 33%, 33%, respectively) vs placebo (13%)."( Changes in peak urinary flow and voiding efficiency in men with signs and symptoms of benign prostatic hyperplasia during once daily tadalafil treatment.
Auerbach, SM; Elion-Mboussa, A; Kaminetsky, JC; Montelongo, RM; Roehrborn, CG; Viktrup, L, 2010)		1.29
"Tadalafil treatment was found effective."( [Treatment of erectile dysfunction of neurogenic genesis with inhibitors of phosphodiesterase of type 5 in patients with diabetes mellitus].
Kurbatov, DG; Rozhivanov, RV, )		0.85
"Tadalafil treatment improved the anastomotic bursting pressure and the hydroxyproline concentration in both normal and ischemic small intestine anastomosis."( The effect of tadalafil on anastomotic healing in ischemic small intestine in rats.
Ayhan, S; Coskun, T; Kara, E; Kaya, Y; Sakarya, A; Var, A, 2010)		2.16
"Tadalafil treatment significantly improved IIEF-5 score, SEP2 and SEP3 of both groups of the patients (P < 0.01). "( [Nocturnal penile tumescence and the effect of tadalafil on erectile dysfunction].
Bai, WJ; Gu, XE; Wang, XF; Xiao, F; Yan, ZA, 2010)		2.06
"Tadalafil 20-mg treatment significantly improved sexual function in patients who were taking serotonin reuptake inhibitors for depression, with mild to moderate, well-tolerable adverse events."( Efficacy and tolerability of tadalafil for treatment of erectile dysfunction in men taking serotonin reuptake inhibitors.
Alma, E; Evliyaoğlu, Y; Kobaner, M; Saygılı, M; Yelsel, K, 2011)		2.1
"Both tadalafil and tempol pretreatment partially prevented (p < 0.01) the rise in CO due to hypoxia."( Long-acting phosphodiesterase 5 inhibitor, tadalafil, and superoxide dismutase mimetic, tempol, protect against acute hypoxia-induced pulmonary hypertension in rats.
Fahim, M; Kotwani, A; Rashid, M, 2012)		1.1
"Tadalafil treatment was associated with significant improvements in ejaculatory function, orgasmic function and sexual satisfaction. "( Effects of 12 weeks of tadalafil treatment on ejaculatory and orgasmic dysfunction and sexual satisfaction in patients with mild to severe erectile dysfunction: integrated analysis of 17 placebo-controlled studies.
Bolyakov, A; Paduch, DA; Polzer, PK; Watts, SD, 2013)		2.14
"Tadalafil treatment improved the metabolic status and reduced infarct size compared to the untreated db/db mice (21.2±1.8% vs 45.8±2.8%; p<0.01)."( Phosphodiesterase-5 inhibitor tadalafil attenuates oxidative stress and protects against myocardial ischemia/reperfusion injury in type 2 diabetic mice.
Das, A; Koka, S; Kukreja, RC; Salloum, FN, 2013)		1.4
"Tadalafil-treated patients had a significantly greater positive response rate on the GAQ in all subpopulations analyzed compared with placebo-treated patients (P<0.03) except for the tadalafil 10 mg cardiovascular subpopulation (placebo, 46.8%; tadalafil 10 mg, 71.0%; P=0.127)."( The efficacy of tadalafil in clinical populations.
Ahuja, S; Eardley, I; Lewis, RW; O'Leary, M; Sadovsky, R; Seftel, A; Shen, W; Walker, DJ; Wang, WC; Wong, DG, 2005)		1.4
"Tadalafil treatment significantly improved SEP3 and IIEF EF domain scores. "( Tolerance to the therapeutic effect of tadalafil does not occur during 6 months of treatment: A randomized, double-blind, placebo-controlled study in men with erectile dysfunction.
Bradley, JD; Carson, CC; Fischer, CJ; Florio, VA; McMahon, CG; Wang, WC, 2006)		2.05
"Tadalafil-treated patients reported a significantly greater improvement in the mean percentage of successful penetrations (tadalafil: 34.5 +/- 4.1; placebo: -4.6 +/- 8.1) and successful intercourse attempts (tadalafil: 52.2 +/- 3.8; placebo: 16.8 +/- 7.8) than placebo-treated patients as measured by the Sexual Encounter Profile."( Efficacy of tadalafil in Egyptian and Turkish men with erectile dysfunction.
Beheiry, A; Esen, A; Kadioglu, A; Khalaf, I; Kopernicky, V; Saylan, M; Shoair, KZ; Wang, WC, 2006)		1.43
"Tadalafil treatment normalized the low response to papaverine and high drop rate in the intracavernosal pressure measured by cavernosometry after CNR compared with sham-operated rats. "( Chronic daily tadalafil prevents the corporal fibrosis and veno-occlusive dysfunction that occurs after cavernosal nerve resection.
Ferrini, MG; Gonzalez-Cadavid, N; Kovanecz, I; Rajfer, J; Rambhatla, A; Sanchez, S; Vernet, D, 2008)		2.15
"Tadalafil treatment significantly improved all domains of the IIEF from baseline, including the erectile function (EF) domain (change = 8.8, end point = 21.6; P < 0.001). "( Tadalafil is efficacious and well tolerated in the treatment of erectile dysfunction (ED) in men over 65 years of age: results from Multiple Observations in Men with ED in National Tadalafil Study in the United States.
Goldfischer, E; Hakim, LS; Natanegara, F; Sharlip, ID; Shumaker, BP; Wong, DG, 2008)		3.23
"Cotreatment with tadalafil and JQ-1 synergistically reduced YAP/TAZ protein expression, suppressed proliferation and induced G0-G1 arrest of cultured HCC cells."( Tadalafil enhances the therapeutic efficacy of BET inhibitors in hepatocellular carcinoma through activating Hippo pathway.
Gong, W; Jiang, Y; Kong, D; Liu, H; Miao, X; Wu, Z, 2021)		2.39
"Treatment with tadalafil improved these adverse effects."( Protective effects of tadalafil against cisplatin-induced spermatogenic dysfunction.
Chiba, K; Fujisawa, M; Ishida, T; Kaku, Y; Okada, K; Onishi, A; Sato, K, 2022)		1.38
"Treatment with tadalafil significantly improved their nocturia after 4 weeks, and these improvements were maintained for the 12-week treatment period."( Tadalafil Improves Nocturia and Nocturia-Related Quality of Life in Patients with Benign Prostatic Hyperplasia (KYU-PRO Study).
Eto, M; Mimata, H; Miyazato, M; Nishii, H; Oshiro, T; Saito, S; Sumino, Y; Takahashi, R; Yoshida, M, 2020)		2.34
"Treatment with tadalafil decreased prostate weight and PBR in a dose-dependent manner, and improved prostatic blood flow and tissue levels of MDA, IL-6, TGF-β1, and bFGF in SHRs, without affecting the blood pressure."( Protective effects of tadalafil on prostatic hyperplasia in spontaneously hypertensive rats.
Higashi, Y; Kamada, S; Kataoka, T; Nagao, Y; Saito, M; Shimizu, S; Shimizu, T, 2020)		1.21
"The treatment with tadalafil inhibited the excessive proliferation of IPAH-PASMCs in a concentration-dependent manner with an IC"( Tadalafil induces antiproliferation, apoptosis, and phosphodiesterase type 5 downregulation in idiopathic pulmonary arterial hypertension in vitro.
Fujitomi, E; Ohara, N; Sato, M; Tsukamoto, K; Yamamura, A; Yamamura, H, 2017)		2.22
"Treatment with tadalafil, an inhibitor of type 5 phosphodiesterase, by oral gavage 1 hour post-exposure and then once daily thereafter, attenuated systemic blood pressures, decreased inflammation, ameliorated pulmonary and cardiac injury, and improved maternal survival (from 36% to 80%) and fetal growth."( Mechanisms and Treatment of Halogen Inhalation-Induced Pulmonary and Systemic Injuries in Pregnant Mice.
Aggarwal, S; Ambalavanan, N; Bradley, WE; Carlisle, MA; Dell'Italia, L; Doran, S; Ford, DA; Jilling, T; Lam, A; Lambert, JA; Matalon, S; Patel, RP; Ren, C, 2017)		0.79
"The treatment with tadalafil 2 hours after the micro-neurosurgical lesions reduced the experimental MOFS lesions development, in a highly significant level (P<0.01) of 58.75%."( Tadalafil: Protective Action against the Development of Multiple Organ Failure Syndrome.
Bian, K; Botelho, PHH; Murad, F; Oliveira, GG; Oliveira, MAB; Oliveira, SAH, )		1.89
"Treatment with tadalafil 5 mg once daily effectively relieves lower urinary tract symptoms based on objective improvement of storage and voiding function, such as detrusor overactivity and bladder outlet obstruction, in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia."( Effects of tadalafil on storage and voiding function in patients with male lower urinary tract symptoms suggestive of benign prostatic hyperplasia: A urodynamic-based study.
Funahashi, Y; Gotoh, M; Kato, M; Majima, T; Matsukawa, Y; Matsuo, K; Yamamoto, T, 2018)		1.22
"Treatment with tadalafil and verapamil decreased the MDA level in treatment groups and also observed a significant change in sperm parameters between Sham and other groups."( Protective effect of tadalafil and verapamil on testicular function and oxidative stress after torsion/detorsion in adult male rat.
Ameli, M; Hashemi, MS; Moghimian, M; Shokoohi, M, 2018)		1.14
"Pretreatment with tadalafil protected against TAA-induced liver fibrosis, in a dose-dependent manner, as proved by the alleviation of inflammatory and fibrotic biomarkers."( The anti-inflammatory and anti-fibrotic effects of tadalafil in thioacetamide-induced liver fibrosis in rats.
Abdel-Salam, RM; Ahmed, NA; Mansour, HM; Salama, AAA; Yassen, NN; Zaki, HF, 2018)		1.06
"Treatment with tadalafil or vardenafil significantly suppressed oxLDL receptor (LOX-1) expression."( PDE5 inhibitors blunt inflammation in human BPH: a potential mechanism of action for PDE5 inhibitors in LUTS.
Carini, M; Cellai, I; Comeglio, P; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Nesi, G; Santi, R; Sebastianelli, A; Serni, S; Vignozzi, L, 2013)		0.73
"Treatment with tadalafil once daily significantly improved erectile function in men with mild to mild-moderate impairments in erectile function following PRN PDE5 inhibitor treatment."( A return to normal erectile function with tadalafil once daily after an incomplete response to as-needed PDE5 inhibitor therapy.
Burns, PR; Goldfischer, ER; Kim, ED; Ni, X; Seftel, AD, 2014)		1.02
"Pretreatment of tadalafil significantly attenuated the above effects of ischemia-reperfusion injury."( Neuroprotective effect of tadalafil, a PDE-5 inhibitor, and its modulation by L-NAME in mouse model of ischemia-reperfusion injury.
Gulati, P; Singh, N, 2014)		1.04
"Treatment with tadalafil 2.5mg or 5mg once daily was well tolerated and resulted in clinically important improvements in patients with mild (54.3% and 74.8%, respectively), moderate (51.3% and 63.1%, respectively), or severe (33.7% and 44.5%, respectively) ED."( Tadalafil once daily in men with erectile dysfunction: an integrated analysis of data obtained from 1913 patients from six randomized, double-blind, placebo-controlled, clinical studies.
Boess, F; Büttner, H; Gacci, M; Henneges, C; Porst, H, 2014)		2.2
"Pre-treatment with tadalafil inhibited both basal and PDGF-induced migration of bladder smooth muscle cells."( Tadalafil effect on metabolic syndrome-associated bladder alterations: an experimental study in a rabbit model.
Carini, M; Cellai, I; Comeglio, P; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Sarchielli, E; Vannelli, GB; Vignozzi, L, 2014)		2.16
"Pretreatment with tadalafil mimicked the neuroprotective effects of iPoCo."( Tadalafil enhances the neuroprotective effects of ischemic postconditioning in mice, probably in a nitric oxide associated manner.
Gulati, P; Singh, N, 2014)		2.17
"Co-treatment with tadalafil decreased the number of VT (0.85 ± 0.53) and MC (0.76 ± 0.22) compared with L-NAME group."( Effects of chronic administration of tamsulosin and tadalafil, alone or in combination, in rats with bladder outlet obstruction induced by chronic nitric oxide deficiency.
Cerqueira, JB; Gonzaga-Silva, LF; Jamacaru, FV; Moraes, MO; Regadas, RP; Reges, R; Sucupira, DG, )		0.71
"Treatment with tadalafil in aged mice improves working memory than the corresponding tadalafil treated young mice in radial arm maze test."( Tadalafil enhances working memory, and reduces hippocampal oxidative stress in both young and aged mice.
Al-Amin, MM; Alam, MA; Alam, T; Didar, RR; Hasan, AT; Hasan, SM; Hossain, I; Rahman, MM, 2014)		2.18
"Pretreatment with tadalafil reduced the absolute urinary excretion of KIM-1, but not of NGAL."( Effects of phosphodiesterase-5 inhibitor on ischemic kidney injury during nephron sparing surgery: quantitative assessment by NGAL and KIM-1.
Abassi, Z; Awad, H; Hussein, O; Khamaisi, M; Lahoud, Y; Matar, I; Nativ, O; Shalabi, A, 2015)		0.74
"Treatment with tadalafil reduced pulse pressure (P=0.0179), systolic blood pressure (P=0.001) and diastolic blood pressure (P=0.054) and increased aortic distensibility (P=0.001) and aortic strain (P=0.003) in the ED group."( Evaluation of arterial stiffness and cardiac function in patients with vascular erectile dysfunction: acute effects of phosphodiesterase-5 inhibitor tadalafil.
Aydinlar, A; Baran, I; Güllülü, S; Keçebaş, M; Kiliçarslan, H; Özdabakoğlu, O; Sağ, S; Şentürk, T; Tütüncü, A, 2017)		0.99
"Treatment with tadalafil resulted in significant improvements in International Prostate Symptom Score (mean difference between treatments -4.2, p < 0.001)."( Urodynamic effects of once daily tadalafil in men with lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia: a randomized, placebo controlled 12-week clinical trial.
Dmochowski, R; Kaminetsky, J; Klise, S; Kraus, S; Roehrborn, C; Xu, L, 2010)		0.98
"Treatment with tadalafil once daily for lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia showed no negative impact on bladder function as measured by detrusor pressure at maximum urinary flow rate or on any other urodynamic parameter assessed. "( Urodynamic effects of once daily tadalafil in men with lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia: a randomized, placebo controlled 12-week clinical trial.
Dmochowski, R; Kaminetsky, J; Klise, S; Kraus, S; Roehrborn, C; Xu, L, 2010)		0.99
"Treatment with tadalafil was generally well tolerated, with adverse events that were transient in nature and of mild to moderate intensity."( Tadalafil: in pulmonary arterial hypertension.
Croxtall, JD; Lyseng-Williamson, KA, 2010)		2.14
"Treatment with tadalafil increased significantly EPCs in both responders and poor responders."( New immunophenotype of circulating endothelial progenitor cells and endothelial microparticles in patients with erectile dysfunction and metabolic syndrome: effects of tadalafil administration.
La Vignera, S, 2011)		0.9
"Pretreatment with tadalafil significantly inhibited the acrolein-induced hyperactivity of both fibres."( Inhibitory effects of phosphodiesterase 5 inhibitor, tadalafil, on mechanosensitive bladder afferent nerve activities of the rat, and on acrolein-induced hyperactivity of these nerves.
Aizawa, N; Igawa, Y; Minagawa, T; Wyndaele, JJ, 2012)		0.95
"Treatment with tadalafil resulted in significant improvements in International Prostate Symptom Score (mean difference between treatments -4.2, p <0.001)."( Urodynamic effects of once daily tadalafil in men with lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia: a randomized, placebo controlled 12-week clinical trial.
Dmochowski, R; Kaminetsky, J; Klise, S; Kraus, S; Roehrborn, C; Xu, L, 2013)		1.01
"Treatment with tadalafil once daily for lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia showed no negative impact on bladder function as measured by detrusor pressure at maximum urinary flow rate or on any other urodynamic parameter assessed. "( Urodynamic effects of once daily tadalafil in men with lower urinary tract symptoms secondary to clinical benign prostatic hyperplasia: a randomized, placebo controlled 12-week clinical trial.
Dmochowski, R; Kaminetsky, J; Klise, S; Kraus, S; Roehrborn, C; Xu, L, 2013)		1.02
"Treatment with tadalafil 10 or 20 mg was associated with significant increases in ejaculatory and orgasmic function (vs placebo) across all baseline ED, EjD, and OD severity strata."( Effects of 12 weeks of tadalafil treatment on ejaculatory and orgasmic dysfunction and sexual satisfaction in patients with mild to severe erectile dysfunction: integrated analysis of 17 placebo-controlled studies.
Bolyakov, A; Paduch, DA; Polzer, PK; Watts, SD, 2013)		1.04
"Treatment with tadalafil significantly improved all primary efficacy variables, regardless of baseline HbA(1c) level."( Effects of tadalafil on erectile dysfunction in men with diabetes.
Anglin, G; Emmick, JT; Knight, JR; Sáenz de Tejada, I, 2002)		1.04
"Men treated with tadalafil compared with placebo reported greater mean changes from baseline on the erectile function domain score (9.3 vs 0.3 with placebo, p <0.001) and on the mean per patient percentage of successful penetration (SEP question 2, 31.6% vs 2.3% with placebo, p <0.001) and successful intercourse attempts (SEP question 3, 43.6% vs 3.5% with placebo, p <0.001). "( The efficacy and safety of tadalafil in United States and Puerto Rican men with erectile dysfunction.
Ahuja, S; Knapp, PM; Seftel, AD; Shin, J; Wang, WC; Wilson, SK, 2004)		0.96
"Treatment with Tadalafil determined a significant increase in PCs (P < 0.001) and FMD (P < 0.001) with respect to basal level."( Circulating endothelial progenitor cells and endothelial function after chronic Tadalafil treatment in subjects with erectile dysfunction.
Caretta, N; De Toni, L; Ferlin, A; Foresta, C; Galan, A; Lana, A; Vinanzi, C, )		0.7
"Treatment with tadalafil at a dose of 2 or 10 mg/kg significantly improved neurological functional recovery compared with saline-treated rats."( Tadalafil, a long-acting type 5 phosphodiesterase isoenzyme inhibitor, improves neurological functional recovery in a rat model of embolic stroke.
Chopp, M; Cui, Y; LaPointe, MC; Silver, B; Zhang, L; Zhang, RL; Zhang, Z, 2006)		2.12
"Treatment with tadalafil decreased the number of apoptotic cells and increased the phosphorylation of the 2 survival associated kinases Akt and extracellular signal-regulated kinase 1/2."( Tadalafil increases Akt and extracellular signal-regulated kinase 1/2 activation, and prevents apoptotic cell death in the penis following denervation.
Klausner, AP; Lysiak, JJ; Son, H; Steers, WD; Tuttle, JB; Yang, SK, 2008)		2.13

Toxicity

Tadalafil was well tolerated, and headache and dyspepsia were the most frequent adverse events. Maternal adverse events in all doses were recorded as at least one grade 1 adverse event. The main treatment-emergent adverse events are mild or moderate in severity, transient and reversible, which may disappear without drug withdrawal.

ExcerptReferenceRelevance
" Tadalafil was well tolerated, and headache and dyspepsia were the most frequent adverse events."( Efficacy and safety of tadalafil for the treatment of erectile dysfunction: results of integrated analyses.
Anglin, G; Brock, GB; Chen, KK; Costigan, T; McMahon, CG; Shen, W; Watkins, V; Whitaker, S, 2002)		1.54
" - The development of the PDE-5 inhibitors vardenafil and tadalafil prompts the question of whether and how these three substances differ in terms of their efficacy and adverse effects."( Erectile dysfunction: comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil--review of the literature.
Gleiter, CH; Gresser, U, 2002)		0.77
" In the present trial, the starting 10mg dose of tadalafil could be increased to 20mg if the patient could not achieve satisfactory intercourse or reduced to 5mg for an adverse event that was persistent, intolerable and judged by the investigator to be related to tadalafil."( Long-term safety and tolerability of tadalafil in the treatment of erectile dysfunction.
Casabé, A; Denne, J; Jünemann, KP; Knight, J; Meuleman, E; Moncada, I; Montorsi, F; Pacheco, C; Segal, S; Valiquette, L; Verheyden, B; Watkins, VS, 2004)		0.85
" Tadalafil was safe and well tolerated."( Long-term safety and tolerability of tadalafil in the treatment of erectile dysfunction.
Casabé, A; Denne, J; Jünemann, KP; Knight, J; Meuleman, E; Moncada, I; Montorsi, F; Pacheco, C; Segal, S; Valiquette, L; Verheyden, B; Watkins, VS, 2004)		1.51
"Tadalafil at doses of 5, 10, or 20mg taken as needed up to once daily for 18 to 24 months was safe and well tolerated."( Long-term safety and tolerability of tadalafil in the treatment of erectile dysfunction.
Casabé, A; Denne, J; Jünemann, KP; Knight, J; Meuleman, E; Moncada, I; Montorsi, F; Pacheco, C; Segal, S; Valiquette, L; Verheyden, B; Watkins, VS, 2004)		2.04
" The most frequent adverse events were headache, dyspepsia, back pain and myalgia."( The efficacy and safety of tadalafil: an update.
Carrier, S; Carson, CC; Cordell, WH; Denne, JS; Eardley, I; Rajfer, J; Shen, W; Walker, DJ, 2004)		0.62
" The most common treatment emergent adverse events were headache (15."( The efficacy and safety of tadalafil in United States and Puerto Rican men with erectile dysfunction.
Ahuja, S; Knapp, PM; Seftel, AD; Shin, J; Wang, WC; Wilson, SK, 2004)		0.62
" The most common treatment-emergent adverse events more frequent (>2%) with tadalafil than placebo were headache, dyspepsia, flushing, back pain, pain in limb and myalgia."( Efficacy and safety of tadalafil in a Western European population of men with erectile dysfunction.
Austoni, E; Beardsworth, A; Eardley, I; Gentile, V; Hackett, G; Lembo, D; Wang, C, 2004)		0.86
" Efficacy was assessed by the International Index of Erectile Function (IIEF), Sexual Encounter Profile (SEP), and Global Assessment Question (GAQ); patient and partner treatment satisfaction by the Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) and SEP; and safety by adverse events, laboratory values, and vital signs."( Efficacy, safety, and treatment satisfaction of tadalafil versus placebo in patients with erectile dysfunction evaluated at tertiary-care academic centers.
Carson, C; Fredlund, P; Kuepfer, C; Murphy, A; Segal, S; Shabsigh, R, 2005)		0.58
" Mild or moderate headache, dyspepsia, and myalgia were the most frequent treatment-emergent adverse events reported."( Efficacy, safety, and treatment satisfaction of tadalafil versus placebo in patients with erectile dysfunction evaluated at tertiary-care academic centers.
Carson, C; Fredlund, P; Kuepfer, C; Murphy, A; Segal, S; Shabsigh, R, 2005)		0.58
" The most common treatment-emergent adverse events--headache and dyspepsia--were generally mild or moderate."( A 6-month study of the efficacy and safety of tadalafil in the treatment of erectile dysfunction: a randomised, double-blind, parallel-group, placebo-controlled study in Australian men.
Fredlund, P; Jesudason, DR; Lording, DW; Lowy, MP; McMahon, CG; Murphy, A; Palmer, NR; Shin, J; Stuckey, BG; Sutherland, PD; Wittert, GA, 2005)		0.59
" Those safe and effective agents were originally developed for their cardiovascular effects and were incidentally found to enhance erections."( Cardiac safety in clinical trials of phosphodiesterase 5 inhibitors.
Carson, CC, 2005)		0.33
" Treatment-emergent adverse events were generally mild or moderate."( Efficacy and safety of oral tadalafil in the treatment of men in Canada with erectile dysfunction: a randomized, double-blind, parallel, placebo-controlled clinical trial.
Anglin, G; Beasley, CM; Brock, GB; Carrier, S; Pommerville, PJ; Shin, J; Whitaker, S, 2005)		0.62
" Treatment with on-demand tadalafil or daily tadalafil was well tolerated, and headaches, facial flushing, and dyspepsia were the most frequently observed adverse events."( Comparison of efficacy, safety, and tolerability of on-demand tadalafil and daily dosed tadalafil for the treatment of erectile dysfunction.
McMahon, C, 2005)		0.87
" Daily tadalafil was well tolerated with headache, dyspepsia, and facial flushing as the most frequent adverse events."( Efficacy and safety of daily tadalafil in men with erectile dysfunction previously unresponsive to on-demand tadalafil.
McMahon, C, 2004)		1.07
" Therefore, men with ED may be at increased risk for cardiovascular adverse events."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		0.61
"The aim of this retrospective analysis was to evaluate the cardiovascular adverse events in clinical trials of tadalafil, an effective medication for the treatment of ED."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		0.83
"An integrated analysis of cardiovascular adverse events was performed on a database from 35 controlled clinical trials (placebo [N = 2,118] and tadalafil [N = 5,228]) and eight open-label trials of tadalafil (tadalafil [N = 6,939])."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		0.82
"In 35 controlled tadalafil clinical trials, the incidence of cardiovascular adverse events was low and comparable in tadalafil- and placebo-treated patients."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		0.95
"In tadalafil clinical trials, the incidence of cardiovascular adverse events in patients receiving tadalafil was low and comparable to placebo."( Update on clinical trials of tadalafil demonstrates no increased risk of cardiovascular adverse events.
Costigan, TM; Emmick, JT; Jackson, G; Kloner, RA; Warner, MR, 2004)		1.24
" Most treatment-emergent adverse events were mild or moderate."( Efficacy and safety of on-demand oral tadalafil in the treatment of men with erectile dysfunction in Taiwan: a randomized, double-blind, parallel, placebo-controlled clinical study.
Chen, KK; Costigan, TM; Emmick, JT; Huang, ST; Jiann, BP; Ju-Ton, H; Lee, SS; Lin, JS; Su, CK; Wang, CJ, 2004)		0.59
" The most common treatment-emergent adverse events reported by patients in all eight groups were headache, nasal congestion, dyspepsia, flushing, and back pain."( Efficacy and safety of tadalafil across ethnic groups and various risk factors in men with erectile dysfunction: Use of a novel noninferiority study design.
Ahuja, S; Barada, J; Donatucci, C; Garcia, CS; Morgentaler, A; Natanegara, F; Niederberger, C; Wong, DG, 2006)		0.64
" Tadalafil was well tolerated, with dyspepsia and headache as the most frequent adverse events reported."( Efficacy and safety of two dosing regimens of tadalafil and patterns of sexual activity in men with diabetes mellitus and erectile dysfunction: Scheduled use vs. on-demand regimen evaluation (SURE) study in 14 European countries.
Buvat, J; Chan, M; Kuepfer, C; Schmitt, H; van Ahlen, H; Varanese, L, 2006)		1.5
"Tadalafil, when taken on demand or three times per week, is efficacious and safe in men with diabetes and ED."( Efficacy and safety of two dosing regimens of tadalafil and patterns of sexual activity in men with diabetes mellitus and erectile dysfunction: Scheduled use vs. on-demand regimen evaluation (SURE) study in 14 European countries.
Buvat, J; Chan, M; Kuepfer, C; Schmitt, H; van Ahlen, H; Varanese, L, 2006)		2.03
" All adverse events (11 cases of headache and dizziness, 8 cases of digestive canal unwell, 5 cases of flushing, 2 cases of back muscle pain) associated with tadalafil were mild and recovered without any treatment."( [Observation of safety and efficacy of tadalafil for men with erectile dysfunction].
Fang, JJ; Li, FY; Zhu, XW, 2006)		0.8
" Adverse reactions are generally transient and mild to moderate in nature."( [Observation of safety and efficacy of tadalafil for men with erectile dysfunction].
Fang, JJ; Li, FY; Zhu, XW, 2006)		0.6
" This retrospective analysis evaluated serious cardiovascular treatment-emergent adverse events (CVTEAEs) reported in 36 clinical trials of tadalafil, a phosphodiesterase-5 inhibitor used for the treatment of erectile dysfunction."( Cardiovascular safety update of Tadalafil: retrospective analysis of data from placebo-controlled and open-label clinical trials of Tadalafil with as needed, three times-per-week or once-a-day dosing.
Chan, M; Costigan, TM; Hutter, AM; Jackson, G; Kloner, RA; Mittleman, MA; Vail, GM; Warner, MR, 2006)		0.82
" Adverse events that occurred in at least 5% of patients were dyspepsia, headache, back pain, upper abdominal pain, and myalgia; nine patients (3."( Evaluation of the efficacy and safety of once-a-day dosing of tadalafil 5mg and 10mg in the treatment of erectile dysfunction: results of a multicenter, randomized, double-blind, placebo-controlled trial.
Casabé, AR; Elion-Mboussa, A; Giuliano, F; Glina, S; Porst, H; Ralph, D; Shen, W; Whitaker, JS, 2006)		0.57
" The most common adverse events reported by patients were headache, back pain, dyspepsia, and dizziness."( Efficacy and safety of on-demand tadalafil for the treatment of erectile dysfunction in South-East Asian men.
Chan, M; Cheong, NF; Ding, Q; Guo, YL; Lim, E; Pan, TM; Shen, W; Venugopalan, M; Wang, YX; Zhu, JC, 2006)		0.62
" Most (= or < 3%) treatment emergent adverse events were mild or moderate."( Efficacy and safety of on demand tadalafil in the treatment of East and Southeast Asian men with erectile dysfunction: a randomized double-blind, parallel, placebo-controlled clinical study.
Chiang, HS; Kopernicky, V; Li, MK; Mendoza, JB; Tan, HM; Wang, WC; Yip, WC, 2006)		0.62
" Most (98%) treatment-emergent adverse events were mild or moderate in severity."( Efficacy and safety of tadalafil 5, 10, and 20 mg in Japanese men with erectile dysfunction: results of a multicenter, randomized, double-blind, placebo-controlled study.
Ishii, N; Kamidono, S; Kimoto, Y; Marumo, K; Nagao, K; Tsujimura, A; Vail, GM; Watts, S, 2006)		0.64
" Treatment-emergent adverse events and vital signs were collected at each visit."( Efficacy and safety of tadalafil in men with erectile dysfunction following spinal cord injury.
Casariego, J; Cruz, N; Dahl, P; Del Popolo, G; Elion-Mboussa, A; Giuliano, F; Leriche, A; Löchner-Ernst, D; Lombardi, G; Reichert, S; Sanchez-Ramos, A, 2007)		0.65
" The 2 most common treatment-emergent adverse events in the tadalafil group compared with placebo were headache (8."( Efficacy and safety of tadalafil in men with erectile dysfunction following spinal cord injury.
Casariego, J; Cruz, N; Dahl, P; Del Popolo, G; Elion-Mboussa, A; Giuliano, F; Leriche, A; Löchner-Ernst, D; Lombardi, G; Reichert, S; Sanchez-Ramos, A, 2007)		0.89
" Adverse events (AEs) reported by all enrolled patients were collected."( Efficacy and safety of tadalafil in the treatment of Latin American men with erectile dysfunction: results of integrated analyses.
Casabé, A; Filimon, I; Glina, S; Kopernicky, V; Leñero, E; Quinzaños, L; Rubio-Aurioles, E; Torres, LO, 2008)		0.66
"Safety measures included adverse events, electrocardiograms, and clinical laboratory measures."( Long-term safety and efficacy of tadalafil 5 mg dosed once daily in men with erectile dysfunction.
Casabé, A; Esler, A; Feldman, R; Klise, SR; Porst, H; Rajfer, J; Ralph, D; Vieiralves, LF; Wolka, AM, 2008)		0.63
" No study drug-related serious adverse events were observed."( Long-term safety and efficacy of tadalafil 5 mg dosed once daily in men with erectile dysfunction.
Casabé, A; Esler, A; Feldman, R; Klise, SR; Porst, H; Rajfer, J; Ralph, D; Vieiralves, LF; Wolka, AM, 2008)		0.63
" The most frequently reported adverse clinical events were in keeping with clinical trial data and include headache, dyspepsia and back pain."( The safety profile of tadalafil as prescribed in general practice in England: results from a prescription-event monitoring study involving 16 129 patients.
Cornelius, V; Hazell, L; Shakir, SA; Wilton, LV, 2009)		0.67
" The profile of treatment-emergent adverse events with tadalafil once daily was similar to that previously reported with as-needed treatment; the most common adverse events with tadalafil (dyspepsia, nasopharyngitis, headaches) were reported in ( Efficacy and safety of tadalafil once daily: considerations for the practical application of a daily dosing option.
Donatucci, CF; Dowsett, SA; Giuliano, F; Glina, S; Sorsaburu, S; Watts, S; Wong, DG, 2008)		0.9
"Tadalafil represents an effective and safe long-term option for SCI patients with ED."( Efficacy and safety of medium and long-term tadalafil use in spinal cord patients with erectile dysfunction.
Cecconi, F; Del Popolo, G; Lombardi, G; Macchiarella, A, 2009)		2.06
"To identify the patient demographic factors, comorbidities, and concomitant medications associated with a change in the likelihood of tadalafil-associated adverse events (AEs) in men with erectile dysfunction."( Likelihood of tadalafil-associated adverse events in integrated multiclinical trial database: classification tree analysis in men with erectile dysfunction.
Brock, G; Glina, S; Kopernicky, V; Moncada, I; Watts, S; Wolka, A; Xu, L, 2009)		0.92
" In addition to its outstanding efficacy that lasts 36 hours, tadalafil shows an excellent safety and tolerance, with only a few transient mild to moderate adverse events."( [Tadalafil for erectile dysfunction: excellent safety and tolerance].
Bai, WJ, 2009)		1.5
" Headache and back pain were the most frequently reported adverse events."( Efficacy and safety of tadalafil taken as needed for the treatment of erectile dysfunction in Asian men: results of an integrated analysis.
Chiang, HS; Choi, HK; Guo, YL; Kopernicky, V; Shen, W; Viswanathan, VP; Yip, AW, 2009)		0.66
"Consistent with pharmacokinetic predictions, data from clinical trials indicate that once-daily use of low-dose tadalafil is a safe and effective treatment for men with ED."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.79
" The main treatment-emergent adverse events, chiefly induced by the interactions of tadalafil with PDE5 and isoforms, are mild or moderate in severity, transient and reversible, which may disappear without drug withdrawal."( [Safety and tolerance of tadalafil in the treatment of erectile dysfunction].
He, XY, 2009)		0.88
"Tadalafil is an effective and safe treatment for males with MS suffering from ED."( Efficacy and safety of tadalafil for erectile dysfunction in patients with multiple sclerosis.
Del Popolo, G; Lombardi, G; Macchiarella, A, 2010)		2.11
" The most common adverse events (AEs) in tadalafil-treated subjects were back pain, nasopharyngitis, dyspepsia, headache, and myalgia."( A randomized, double-blind, placebo-controlled, parallel study to assess the efficacy and safety of once-a-day tadalafil in men with erectile dysfunction who are naïve to PDE5 inhibitors.
Aversa, A; Barker, C; Moncada, I; Montorsi, F; Perimenis, P; Porst, H; Shane, MA; Sorsaburu, S, 2011)		0.85
" No serious adverse events were observed, except some common ones, such as rubeosis (11."( [Efficacy and safety of long-term small-dose tadalafil in the treatment of erectile dysfunction].
Ji, JT; Liu, ZY; Lu, X; Piao, SG; Sheng, X; Xu, CL; Xu, WD; Ye, HM, 2011)		0.63
" Categoric efficacy variables were analyzed with the Cochran-Mantel-Haenszel test, and between-group differences in treatment-emergent adverse events (TEAEs) were assessed using the Fisher exact test."( Efficacy and safety of tadalafil once daily in the treatment of men with lower urinary tract symptoms suggestive of benign prostatic hyperplasia: results of an international randomized, double-blind, placebo-controlled trial.
Casabé, AR; Kim, ED; Mirone, V; Porst, H; Secrest, RJ; Sundin, DP; Viktrup, L; Xu, L, 2011)		0.68
" The adverse event profile was consistent with that previously reported in men with ED."( Efficacy and safety of tadalafil once daily in the treatment of men with lower urinary tract symptoms suggestive of benign prostatic hyperplasia: results of an international randomized, double-blind, placebo-controlled trial.
Casabé, AR; Kim, ED; Mirone, V; Porst, H; Secrest, RJ; Sundin, DP; Viktrup, L; Xu, L, 2011)		0.68
" Phosphodiesterase type-5 inhibitors (PDE5-i) are generally regarded as safe and effective."( 10-Year analysis of adverse event reports to the Food and Drug Administration for phosphodiesterase type-5 inhibitors.
Costabile, RA; Lowe, G, 2012)		0.38
"Summarized reports of adverse events (AEs) for each PDE5-i were requested from the Center for Drug Evaluation and Research within the FDA."( 10-Year analysis of adverse event reports to the Food and Drug Administration for phosphodiesterase type-5 inhibitors.
Costabile, RA; Lowe, G, 2012)		0.38
" 10-year analysis of adverse event reports to the Food and Drug Administration for phosphodiesterase type-5 inhibitors."( 10-Year analysis of adverse event reports to the Food and Drug Administration for phosphodiesterase type-5 inhibitors.
Costabile, RA; Lowe, G, 2012)		0.38
"A low incidence of some PDE-related adverse events may be reflected by the high selectivity of avanafil against non-PDE5 isozymes."( Selectivity of avanafil, a PDE5 inhibitor for the treatment of erectile dysfunction: implications for clinical safety and improved tolerability.
Burnett, AL; Day, WW; DiDonato, K; Heller, WH; Kikkawa, K; Kotera, J; Omori, K; Peterson, CA; Wang, R; Yee, S, 2012)		0.38
" Lower selectivity against PDE1, PDE6, and PDE11 is consistent with results from randomized, placebo-controlled, phase 3 trials in which musculoskeletal and hemodynamic adverse events were reported in <2% of patients and no color vision-related abnormalities were reported with avanafil doses up to 200 mg once daily."( Selectivity of avanafil, a PDE5 inhibitor for the treatment of erectile dysfunction: implications for clinical safety and improved tolerability.
Burnett, AL; Day, WW; DiDonato, K; Heller, WH; Kikkawa, K; Kotera, J; Omori, K; Peterson, CA; Wang, R; Yee, S, 2012)		0.38
"Data suggest that avanafil may confer a safety benefit, in terms of a lower incidence of specific adverse events, by virtue of its high specificity to PDE5 and its overall selectivity against other PDE isozymes."( Selectivity of avanafil, a PDE5 inhibitor for the treatment of erectile dysfunction: implications for clinical safety and improved tolerability.
Burnett, AL; Day, WW; DiDonato, K; Heller, WH; Kikkawa, K; Kotera, J; Omori, K; Peterson, CA; Wang, R; Yee, S, 2012)		0.38
" Both doses of tadalafil were generally well tolerated, with adverse event rates similar to placebo."( Efficacy and safety of once-daily tadalafil in men with erectile dysfunction who reported no successful intercourse attempts at baseline.
Burns, PR; Kim, ED; Ni, X; Seftel, AD; Shabsigh, R, 2013)		1.02
" PDE5-Is are generally safe and well tolerated, and there is no major difference on the safety profile."( Comparative effectiveness and safety of oral phosphodiesterase type 5 inhibitors for erectile dysfunction: a systematic review and network meta-analysis.
Chen, Q; Ding, H; Lee, J; Liu, Y; Mao, C; Qin, X; Ren, Z; Tang, J; Tian, J; Yang, Z; Yuan, J; Zhang, R, 2013)		0.39
" Patient-reported adverse events included headache (4%) and heartburn (2%)."( Safety, tolerability, and efficacy of overnight switching from sildenafil to tadalafil in patients with pulmonary arterial hypertension.
Doran, AK; Hill, W; Shapiro, S; Traiger, G; Zhang, L, 2013)		0.62
" Changes in total International Prostate Symptom Score (IPSS), IPSS-quality of life index, and BPH impact index were examined overall, and changes in IPSS or adverse events (AEs) were examined across subgroups of interest."( Efficacy and safety of tadalafil 5 mg once daily for lower urinary tract symptoms suggestive of benign prostatic hyperplasia: subgroup analyses of pooled data from 4 multinational, randomized, placebo-controlled clinical studies.
Cox, D; Dey, D; Goldfischer, ER; Oelke, M; Porst, H; Viktrup, L; Watts, S, 2013)		0.7
" Changes in lower urinary tract symptoms secondary to benign prostatic hyperplasia were assessed with the I-PSS, erectile dysfunction improvements were assessed with the IIEF-EF (International Index of Erectile Function-Erectile Function) in sexually active men and safety was assessed by evaluating adverse events."( Efficacy and safety of the coadministration of tadalafil once daily with finasteride for 6 months in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia.
Casabé, A; Da Pozzo, LF; Henderson, RJ; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L; Wong, DG; Zepeda, S, 2014)		0.66
" Tadalafil/finasteride coadministration was well tolerated and most adverse events were mild/moderate."( Efficacy and safety of the coadministration of tadalafil once daily with finasteride for 6 months in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia.
Casabé, A; Da Pozzo, LF; Henderson, RJ; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L; Wong, DG; Zepeda, S, 2014)		1.57
" Safety assessment included laboratory tests and patient's reporting of adverse event."( A comparative randomized prospective study to evaluate efficacy and safety of combination of tamsulosin and tadalafil vs. tamsulosin or tadalafil alone in patients with lower urinary tract symptoms due to benign prostatic hyperplasia.
Mandal, AK; Mete, UK; Singh, DV; Singh, SK, 2014)		0.62
" Tadalafil may be a safe drug to treat children and young adults with PAH."( Comparison of the therapeutic and side effects of tadalafil and sildenafil in children and adolescents with pulmonary arterial hypertension.
Beheshtian, E; Sabri, MR, 2014)		1.57
" The safety was assessed by observing drug tolerability and adverse events."( Efficacy and safety of long-term tadalafil 5 mg once daily combined with sildenafil 50 mg as needed at the early stage of treatment for patients with erectile dysfunction.
Cui, H; Deng, Y; Fang, J; Liu, B; Song, Z; Wang, H; Wang, Z; Zhang, S, 2015)		0.7
"L-carnitine combined with tadalafil is safe and effective for the treatment of LOH with ED."( [Safety and efficacy of L-carnitine and tadalafil for late-onset hypogonadism with ED: a randomized controlled multicenter clinical trial].
Cai, ZK; Dai, JC; Li, P; Li, Z; Wang, YX; Wang, Z; Zhang, W; Zheng, JH, 2014)		0.97
"The present studies examined the toxic interaction between the non-coxib celecoxib derivative OSU-03012 and phosphodiesterase 5 (PDE5) inhibitors, and also determined the roles of endoplasmic reticulum stress response regulators in cell survival."( Regulation of OSU-03012 toxicity by ER stress proteins and ER stress-inducing drugs.
Booth, L; Cruickshanks, N; Dent, P; Grant, S; Poklepovic, A; Roberts, JL, 2014)		0.4
" It has not yet been observed if transition from sildenafil to tadalafil is beneficial in patients suffering from adverse reactions."( Safety and long-term efficacy of transition from sildenafil to tadalafil due to side effects in patients with pulmonary arterial hypertension.
Egenlauf, B; Ehlken, N; Grünig, E; Harzheim, D; Lichtblau, M; Marra, A; Pinado, FP, 2015)		0.9
"A retrospective analysis of PAH-patients who were stable on sildenafil for >3 months and transitioned to tadalafil due to adverse events was performed."( Safety and long-term efficacy of transition from sildenafil to tadalafil due to side effects in patients with pulmonary arterial hypertension.
Egenlauf, B; Ehlken, N; Grünig, E; Harzheim, D; Lichtblau, M; Marra, A; Pinado, FP, 2015)		0.87
"5 %) adverse events occurred under tadalafil as well and therapy with PDE-5 inhibitors was discontinued."( Safety and long-term efficacy of transition from sildenafil to tadalafil due to side effects in patients with pulmonary arterial hypertension.
Egenlauf, B; Ehlken, N; Grünig, E; Harzheim, D; Lichtblau, M; Marra, A; Pinado, FP, 2015)		0.93
" Specific adverse events with PDE5 inhibitors included headache (12."( Efficacy and safety of phosphodiesterase type 5 (PDE5) inhibitors in treating erectile dysfunction after bilateral nerve-sparing radical prostatectomy.
Cui, Y; Gao, Z; Liu, X; Shi, L, 2016)		0.43
" These products represent a major safety threat for the consumers in Egypt and the Middle East, especially; the target audience is mostly affected with heart and blood pressure problems seeking natural and safe alternatives to the well-established Phosphodiesterase 5 Inhibitors (PDE-5Is)."( Male enhancement Nutraceuticals in the Middle East market: Claim, pharmaceutical quality and safety assessments.
ElAgouri, G; ElAmrawy, F; ElYazbi, A; Eshra, A; Nounou, MI, 2015)		0.42
" Safety measurements included treatment-emergent adverse events (TEAEs), adverse events (AEs) leading to discontinuation, serious AEs (SAEs), and cardiovascular AEs."( Efficacy and safety of tadalafil 5 mg once daily in the treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia in men aged ≥75 years: integrated analyses of pooled data from multinational, randomized, placebo-controlled cli
Büttner, H; Oelke, M; Takita, Y; Viktrup, L; Wagg, A, 2017)		0.77
"Meta-analyses are frequently performed on adverse event data and are primarily used for improving statistical power to detect safety signals."( A Bayesian meta-analytic approach for safety signal detection in randomized clinical trials.
Fukimbara, S; Odani, M; Sato, T, 2017)		0.46
" We applied the proposed Bayesian meta-analysis models to published adverse event data from three premarketing randomized clinical trials of tadalafil and to a simulation study motivated by the case example to evaluate the characteristics of three alternative models."( A Bayesian meta-analytic approach for safety signal detection in randomized clinical trials.
Fukimbara, S; Odani, M; Sato, T, 2017)		0.66
"Comparison of the results from the Bayesian meta-analysis model with those from Fisher's exact test after simple pooling showed that 6 out of 10 adverse events were the same within a top 10 ranking of individual adverse events with regard to association with treatment."( A Bayesian meta-analytic approach for safety signal detection in randomized clinical trials.
Fukimbara, S; Odani, M; Sato, T, 2017)		0.46
"Adverse events under the same body system were not necessarily positively related when we used "system organ class" and "preferred term" in the Medical Dictionary for Regulatory Activities as a hierarchical structure of adverse events."( A Bayesian meta-analytic approach for safety signal detection in randomized clinical trials.
Fukimbara, S; Odani, M; Sato, T, 2017)		0.46
"Our proposed meta-analysis models considered trial effects to avoid confounding by trial and borrowed strength from both within and across body systems to obtain reasonable and stable estimates of an effect measure by considering a hierarchical structure of adverse events."( A Bayesian meta-analytic approach for safety signal detection in randomized clinical trials.
Fukimbara, S; Odani, M; Sato, T, 2017)		0.46
" Safety was assessed by analyzing the frequency of adverse drug reactions (ADRs), discontinuations due to adverse events (AEs), and serious adverse drug reactions (SADRs)."( Safety and effectiveness of tadalafil in patients with pulmonary arterial hypertension: Japanese post-marketing surveillance data.
Kobayashi, N; Murakami, M; Tajima, K; Taketsuna, M; Yamazaki, H, 2017)		0.75
" The meta-analyses of adverse events showed no significant differences."( Efficacy and Safety of Tadalafil Once-a-Day versus Tadalafil On-Demand in Patients with Erectile Dysfunction: A Systematic Review and Meta-Analyses.
Dong, Q; Liu, L; Peng, Z; Wei, Q; Yang, B; Yang, L, 2017)		0.77
" Safety was assessed from the frequency of adverse drug reactions (ADRs), discontinuations due to adverse events (AEs), and serious adverse drug reactions (SADRs)."( Safety and effectiveness of tadalafil in pediatric patients with pulmonary arterial hypertension: a sub-group analysis based on Japan post-marketing surveillance.
Kobayashi, N; Murakami, M; Suzuki, N; Tajima, K; Taketsuna, M; Yamazaki, H, 2017)		0.75
"Three cases were initially commenced on 10 mg/day and monitored for major adverse events."( Safety and dose-finding trial of tadalafil administered for fetal growth restriction: A phase-1 clinical study.
Ikeda, T; Kamimoto, Y; Kondo, E; Kubo, M; Maki, S; Murabayashi, N; Nii, M; Osato, K; Tanaka, H; Umekawa, T, 2017)		0.74
" Maternal adverse events in all doses were recorded as least one grade 1 adverse events, as tadalafil was considered acceptable from the viewpoint of the mothers."( Safety and dose-finding trial of tadalafil administered for fetal growth restriction: A phase-1 clinical study.
Ikeda, T; Kamimoto, Y; Kondo, E; Kubo, M; Maki, S; Murabayashi, N; Nii, M; Osato, K; Tanaka, H; Umekawa, T, 2017)		0.96
" The safety assessments were adverse reactions, laboratory test results, and vital signs at week 24."( Efficacy and Safety of a Fixed-Dose Combination Therapy of Tamsulosin and Tadalafil for Patients With Lower Urinary Tract Symptoms and Erectile Dysfunction: Results of a Randomized, Double-Blinded, Active-Controlled Trial.
Ahn, TY; Hyun, JS; Jung, J; Kim, SW; Lee, SW; Min, KS; Moon, DG; Moon, KH; Park, JK; Park, K; Park, NC; Ryu, JK; Son, H; Yang, DY; Yang, SK, 2017)		0.69
" No clinically significant adverse events regarding the investigational products were observed during the 24-week period."( Efficacy and Safety of a Fixed-Dose Combination Therapy of Tamsulosin and Tadalafil for Patients With Lower Urinary Tract Symptoms and Erectile Dysfunction: Results of a Randomized, Double-Blinded, Active-Controlled Trial.
Ahn, TY; Hyun, JS; Jung, J; Kim, SW; Lee, SW; Min, KS; Moon, DG; Moon, KH; Park, JK; Park, K; Park, NC; Ryu, JK; Son, H; Yang, DY; Yang, SK, 2017)		0.69
" The primary endpoint of the study was safety at 12 months as assessed by the proportion of patients experiencing at least one treatment-emergent adverse event (serious or nonserious)."( Evaluation of the long-term safety and effectiveness of tadalafil once daily in Chinese men with erectile dysfunction: interim results of a multicenter, randomized, open-label trial.
Dai, YT; Jiang, H; Li, FB; Lin, HC; Liu, JH; Lou, Y; Luo, JD; Yan, S; Zhang, ZC; Zhao, LM; Zhu, ZH, )		0.38
" The following outcome measures were obtained at baseline and at 4 and 8 weeks of tadalafil treatment: physical examination, adverse effects, Short Form 12 Health Survey (SF-12) score, International Index of Erectile Function (IIEF-5) score, bioelectrical impedance analysis (BIA), and free radical testing."( Evaluation of the effectiveness and safety of a daily dose of 5 mg of tadalafil, over an 8-week period, for improving quality of life among Korean men with andropause symptoms, including erectile dysfunction: A pilot study.
Han, CH; Kim, BD; Lee, JG; Lee, KK; Yum, KS, 2018)		0.94
" No adverse effects were noted."( Evaluation of the effectiveness and safety of a daily dose of 5 mg of tadalafil, over an 8-week period, for improving quality of life among Korean men with andropause symptoms, including erectile dysfunction: A pilot study.
Han, CH; Kim, BD; Lee, JG; Lee, KK; Yum, KS, 2018)		0.71
"Tadalafil (5 mg dose, once daily) is a safe and effective treatment to improve ED, and overall QoL, among Korean men with andropause symptoms, including ED."( Evaluation of the effectiveness and safety of a daily dose of 5 mg of tadalafil, over an 8-week period, for improving quality of life among Korean men with andropause symptoms, including erectile dysfunction: A pilot study.
Han, CH; Kim, BD; Lee, JG; Lee, KK; Yum, KS, 2018)		2.16
" We concluded that tadalafil is well tolerated and safe in patients with cardiovascular comorbidities and, in addition, has a beneficial effect on the cardiovascular system."( [Safety of tadalafil in patients with cardiovascular comorbidities].
Bulygin, KV; Galimov, SN; Galimova, EF; Gaysina, GG; Nikitina, IL; Pavlov, VN, 2019)		1.23
" However, the least side effect was observed in the tadalafil + aspirin group."( Efficacy and safety of combination of tadalafil and aspirin versus tadalafil or aspirin alone in patients with vascular erectile dysfunction: a comparative randomized prospective study.
Albayrak, S; Bayraktar, Z, 2019)		1.04
" For safety, combination-therapy had a higher incidence rate of any adverse events (AEs) and discontinuation due to AEs than monotherapy with the exception of pain."( Meta-Analysis of Efficacy and Safety of Tadalafil Plus Tamsulosin Compared with Tadalafil Alone in Treating Men with Benign Prostatic Hyperplasia and Erectile Dysfunction.
Cui, Y; Gao, Z; Wu, J; Xu, Z; Zheng, X; Zhou, Z, )		0.4
" Then we recorded the IIEF-5 score and penile erection hardness score (EHS) and adverse reactions and compared them among the three groups of patients."( [Efficacy and safety of regular use of sildenafil in the treatment of penile erectile dysfunction].
Jia, DH; Li, R; Wang, CL; Wang, R; Yang, F; Zhang, TB; Zhang, WX; Zheng, T, 2019)		0.51
"Regular use of sildenafil has a therapeutic effect similar to that of tadalafil but better than that of sildenafil on-demand, without more adverse effects."( [Efficacy and safety of regular use of sildenafil in the treatment of penile erectile dysfunction].
Jia, DH; Li, R; Wang, CL; Wang, R; Yang, F; Zhang, TB; Zhang, WX; Zheng, T, 2019)		0.75
" (Conclusion) Tadalafil is considered to be a highly effective and safe drug in very elderly patients with LUTS."( [EFFECTIVENESS AND SAFETY OF TADALAFIL IN VERY ELDERLY PATIENTS WITH LOWER URINARY TRACT SYMPTOMS].
Fukagai, T; Hayashi, K; Hirayama, K; Igarashi, A; Ishikawa, K; Koshikiya, A; Morita, M; Noguchi, T; Ogawa, Y; Sasaki, H, 2019)		1.17
"The adverse effects were minor and were managed symptomatically without any drug discontinuity."( Efficacy and safety of tadalafil vs tamsulosin in lower urinary tract symptoms (LUTS) as a result of benign prostate hyperplasia (BPH)-open label randomised controlled study.
Gupta, S; Singh, I; Tk, A, 2020)		0.87
"Male reproductive toxicity is a well-known adverse effect of cisplatin (CIS), an important antineoplastic agent used to control several types of cancers."( Tadalafil alleviates cisplatin-induced reproductive toxicity through the activation of the Nrf2/HO-1 pathway and the inhibition of oxidative stress and apoptosis in male rats.
Abdel-Wahab, BA; Alkahtani, SA; Elagab, EAM, 2020)		2
" An analysis of safety outcomes revealed extremely high adverse events (AEs) and pain in the combination group."( Efficacy and Safety of Combination Comprising Tamsulosin and PDE5-Is, Relative to Monotherapies, in Treating Lower Urinary Tract Symptoms and Erectile Dysfunction Associated With Benign Prostatic Hyperplasia: A Meta-Analysis.
Sun, F; Sun, K; Wang, J; Wang, T; Wu, G; Wu, J; Yao, H; Zhang, D, )		0.13
"To study the efficacy of phosphodiesterase-5 inhibitor tadalafil in attenuating adverse events after low-dose-rate brachytherapy for prostate cancer."( Impact of low-dose tadalafil on adverse events after low-dose-rate brachytherapy for prostate cancer: A bi-center randomized open-label trial.
Fukazawa, A; Hashida, I; Iijima, K; Ishizuka, O; Kato, H; Koiwai, K; Minagawa, T; Ogawa, T; Oguchi, T; Saitou, T, 2021)		1.2
"To describe the otorhinolaryngological adverse effects of the main drugs used in urological practice."( Otorhinolaryngological adverse effects of urological drugs.
Ganança, FF; Lopes, KC; Maia, NPD, )		0.13
"A review of the scientific literature was performed using a combination of specific descriptors (side effect, adverse effect, scopolamine, sildenafil, tadalafil, vardenafil, oxybutynin, tolterodine, spironolactone, furosemide, hydrochlorothiazide, doxazosin, alfuzosin, terazosin, prazosin, tamsulosin, desmopressin) contained in publications until April 2020."( Otorhinolaryngological adverse effects of urological drugs.
Ganança, FF; Lopes, KC; Maia, NPD, )		0.33
"The main drugs used in Urology may cause several otorhinolaryngological adverse effects."( Otorhinolaryngological adverse effects of urological drugs.
Ganança, FF; Lopes, KC; Maia, NPD, )		0.13
"Most of the drugs used in urological practice have otorhinolaryngological adverse effects."( Otorhinolaryngological adverse effects of urological drugs.
Ganança, FF; Lopes, KC; Maia, NPD, )		0.13
" Demographics, symptoms, and adverse effects were collected."( Safety and tolerability of combination therapy with ambrisentan and tadalafil for the treatment of pulmonary arterial hypertension in children: Real-world experience.
Crook, S; Dorn, ML; Frank, B; Hite, MD; Issapour, A; Ivy, DD; Krishnan, US; Rosenzweig, EB, 2022)		0.96
"This pooled safety analysis assessed the incidence of hypotension-related treatment-emergent adverse events (TEAEs) and major adverse cardiovascular events (MACEs) in patients with concomitant use of tadalafil and antihypertensive medications."( Analysis of integrated clinical safety data of tadalafil in patients receiving concomitant antihypertensive medications.
Gupta, A; Kloner, RA; Kostis, JB; McGraw, TP; Qiu, C, 2022)		1.17
"RCTs reporting obstetric or perinatal outcomes or maternal adverse outcomes in women taking PDE5i in pregnancy."( Phosphodiesterase-5 inhibitors in pregnancy: Systematic review and meta-analysis of maternal and perinatal safety and clinical outcomes.
Deprest, J; Kumar, S; Mol, BW; Russo, F; Turner, JM, 2022)		0.72
" Adverse events occurred in two cases."( Efficacy and safety of dutasteride with tadalafil add-on therapy in patients with lower urinary tract symptoms secondary to benign prostatic hyperplasia.
Fujimoto, K; Gotoh, D; Hori, S; Miyake, M; Morizawa, Y; Nakai, Y; Torimoto, K, 2022)		0.99

Pharmacokinetics

Tadalafil was absorbed rapidly with mean Cmax (378 microg l-1 for 20 mg) observed at 2 h. concentrations declined nearly monoexponentially with a mean (5th, 95th percentiles) t1/2 of 17.

ExcerptReferenceRelevance
" The method is suitable in pharmacokinetic investigation and monitoring tadalafil concentration."( Determination of tadalafil in small volumes of plasma by high-performance liquid chromatography with UV detection.
Cheng, CL; Chou, CH, 2005)		0.9
" This review comparatively discusses the major characteristics of the pharmacokinetic profile of all 3 PDE5 inhibitors, including bioavailability and rate of absorption, Biopharmaceutical Classification System categorization, elimination mechanisms, and metabolic profile including active metabolites, as well as the drug-drug interaction potential and modification of pharmacokinetic properties under selected physiologic and pathophysiologic conditions."( The clinical pharmacokinetics of phosphodiesterase-5 inhibitors for erectile dysfunction.
Gupta, M; Kovar, A; Meibohm, B, 2005)		0.33
"Potential pharmacokinetic interactions between dapoxetine, a serotonin transporter inhibitor developed for the treatment of premature ejaculation (PE), and the phosphodiesterase-5 inhibitors tadalafil and sildenafil, agents used in the treatment of erectile dysfunction (ED), were investigated in an open-label, randomized, crossover study (n=24 men) comparing dapoxetine 60 mg, dapoxetine 60 mg+tadalafil 20 mg, and dapoxetine 60 mg+sildenafil 100 mg."( Dapoxetine, a novel treatment for premature ejaculation, does not have pharmacokinetic interactions with phosphodiesterase-5 inhibitors.
Desai, D; Dresser, MJ; Gidwani, S; Modi, NB; Seftel, AD, )		0.32
"Tadalafil was absorbed rapidly with mean Cmax (378 microg l-1 for 20 mg) observed at 2 h; thereafter, concentrations declined nearly monoexponentially with a mean (5th, 95th percentiles) t1/2 of 17."( Tadalafil pharmacokinetics in healthy subjects.
Bedding, AW; Forgue, ST; Mitchell, MI; Patterson, BE; Payne, CD; Phillips, DL; Wrishko, RE, 2006)		3.22
" Tadalafil is mainly metabolized by cytochrome P450 (CYP) 3A4, and as bosentan induces CYP2C9 and CYP3A4, a pharmacokinetic interaction is possible between these agents."( Pharmacokinetic interaction between tadalafil and bosentan in healthy male subjects.
Darstein, C; Dingemanse, J; Mitchell, MI; Phillips, DL; Wrishko, RE; Yu, A, 2008)		1.53
"Based upon pharmacodynamic and pharmacokinetic data, once-daily doses of tadalafil 5 mg were predicted to provide therapeutic concentrations that would be maintained throughout the 24-hour dosing interval."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.81
"Consistent with pharmacokinetic predictions, data from clinical trials indicate that once-daily use of low-dose tadalafil is a safe and effective treatment for men with ED."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.79
" Due to the potential combination use, the pharmacokinetic (PK) interactions between these two drugs were assessed in a crossover study in 26 healthy adults."( No clinically relevant pharmacokinetic and safety interactions of ambrisentan in combination with tadalafil in healthy volunteers.
Boinpally, R; Dufton, C; Harrison, B; Mandagere, A; Spence, R, 2009)		0.57
" Pharmacokinetic parameters were determined in a noncompartmental analysis."( Effect of tipranavir/ritonavir combination on the pharmacokinetics of tadalafil in healthy volunteers.
Dellamonica, P; Durant, J; Ferrando, S; Garraffo, R; Lavrut, T; MacGregor, TR; Rouyrre, N; Sabo, JP, 2011)		0.6
" These findings have potential therapeutic implications for predicting the pharmacokinetic responses of humans to hyperlipidemia."( Effects of experimental hyperlipidemia on the pharmacokinetics of tadalafil in rats.
Lee, JH; Lee, YJ; Oh, JH, 2012)		0.62
"For both drugs, the peak plasma concentration was lower and the half-life was shorter than the known values in adults."( Pharmacokinetics of drugs for pediatric pulmonary hypertension.
Azuma, H; Kajihama, A; Kajino, H; Kamiyama, N; Maeda, J; Nakau, K; Oka, H; Sugimoto, M; Tasaki, Y; Yamagishi, H, 2016)		0.43
" Geometric mean ratios (GMRs) of the ODF to FCT formulations and their 90% CIs for the pharmacokinetic parameters were estimated."( Comparison of tadalafil pharmacokinetics after administration of a new orodispersible film versus a film-coated tablet.
Chang, S; Heo, SH; Hong, JH; Jin, EH; Kim, G; Kim, J; Kim, MG; Lee, S; Park, SI; Song, KH, 2018)		0.84
" Among them, compound 15 (TPN171) with subnanomolar potency for PDE5 and good selectivity over PDE6 was finally recognized as a potential drug candidate, and its pharmacokinetic profiles in rats and dogs are significantly improved compared to the starting compound (3)."( Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Aisa, HA; Gong, X; He, Y; Jiang, H; Jiang, X; Li, J; Liu, Z; Shen, J; Shi, J; Suo, J; Tian, G; Wang, Y; Wang, Z; Wu, C; Wu, J; Xu, Y; Xu, Z; Yang, R; Yang, X; Zhang, R; Zhang, X; Zhu, W; Zou, X, 2019)		0.51
" Pharmacodynamic study was performed via biochemical analysis of cyclic guanosine monophosphate (cGMP) in rat penis 2-h post-treatment and compared with oral suspension of Cialis® tablets."( Intranasal Tadalafil nanoemulsions: formulation, characterization and pharmacodynamic evaluation.
Abdelmonsif, DA; Boraie, N; Elbardisy, B; Galal, S, 2019)		0.9
" To investigate and potentially fulfill an unmet need in pediatric patients with PAH, pharmacokinetic (PK) data were explored in a pediatric phase Ib/II study and pooled with prior phase III (pulmonary arterial hypertension and response to tadalafil [PHIRST-1]) adult data to develop the first population PK model for tadalafil in pediatric patients with PAH."( Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Ferguson-Sells, L; Li, B; Small, D; Velez de Mendizabal, N, 2022)		1.19
" Pharmacokinetic parameters were calculated using noncompartmental analysis."( Pharmacokinetic and Bioequivalence Evaluation of 2 Tadalafil Tablets in Healthy Male Chinese Subjects Under Fasting and Fed Conditions.
Chen, JL; Hu, Y; Jiang, B; Lou, HG; Ruan, ZR; Shao, R; Yang, DD, 2022)		0.97
" This study aimed to examine the pharmacokinetic drug interaction between tadalafil and amlodipine and the tolerability of their combined administration in healthy male subjects."( Pharmacokinetic Drug Interaction Between Amlodipine and Tadalafil: An Open-Label, Randomized, Multiple-Dose Crossover Study in Healthy Male Volunteers.
Hong, S; Jung, J; Kim, H; Lee, SH; Lim, HS, 2022)		1.2
" Pharmacokinetic parameters were calculated using non-compartmental analysis."( Pharmacokinetic Drug Interaction Between Amlodipine and Tadalafil: An Open-Label, Randomized, Multiple-Dose Crossover Study in Healthy Male Volunteers.
Hong, S; Jung, J; Kim, H; Lee, SH; Lim, HS, 2022)		0.97
"A substantial pharmacokinetic drug interaction between tadalafil and amlodipine was observed with respect to the concentration of tadalafil when administered concomitantly."( Pharmacokinetic Drug Interaction Between Amlodipine and Tadalafil: An Open-Label, Randomized, Multiple-Dose Crossover Study in Healthy Male Volunteers.
Hong, S; Jung, J; Kim, H; Lee, SH; Lim, HS, 2022)		1.21
" Tadalafil and canagliflozin were determined simultaneously in real human plasma using the described procedure and the method was applied for in vivo pharmacokinetic drug interaction study between the studied drugs, which proved significant interaction between them when administered simultaneously."( Cytochrome P450 3A4-mediated pharmacokinetic interaction study between tadalafil and canagliflozin using high-performance thin-layer chromatography.
Abdel-Aal, FAM; Ali, ABH; Mohamed, AI; Rageh, AH, 2022)		1.86

Compound-Compound Interactions

Oral-appliance combined with tadalafil can improve erectile function in patients with severe OSAHS-induced ED, with a better efficacy than either of them used alone.Iloprost combined with low dose tadalfil regimen can effectively reduce PVR, increase 6MWD, and improve cardiopulmonary function in adults CHD patients with PAH.

ExcerptReferenceRelevance
"Perform a systematic review and meta-analysis of available prospective and cross-sectional studies on the use of PDE5-Is alone or in combination with α1-adrenergic blockers in patients with LUTS/benign prostatic hyperplasia (BPH)."( A systematic review and meta-analysis on the use of phosphodiesterase 5 inhibitors alone or in combination with α-blockers for lower urinary tract symptoms due to benign prostatic hyperplasia.
Carini, M; Corona, G; Gacci, M; Kaplan, SA; Maggi, M; McVary, KT; Mirone, V; Roehrborn, CG; Salvi, M; Serni, S; Vignozzi, L, 2012)		0.38
"To study the effect of Tadalafil combined with behavior therapy in helping obtain semen from infertile men in whom masturbation has failed."( [Tadalafil combined with behavior therapy for semen collection from infertile males in whom masturbation fails].
Gao, L; Hong, K; Jiang, H; Liu, DF; Ma, LL; Mao, JM; Qiao, J; Tang, WH; Yang, Y; Zhang, J; Zhao, LM, 2013)		1.61
"Sixty male infertile patients from whom masturbation had failed to obtain semen were equally assigned to receive Tadalafil combined with behavior therapy (combination group) or Tadalafil only (control group)."( [Tadalafil combined with behavior therapy for semen collection from infertile males in whom masturbation fails].
Gao, L; Hong, K; Jiang, H; Liu, DF; Ma, LL; Mao, JM; Qiao, J; Tang, WH; Yang, Y; Zhang, J; Zhao, LM, 2013)		1.51
"By training the patients and establishing a conditioned response to masturbation, Tadalafil combined with behavior therapy can significantly increase the success rate of semen collection from the male infertile patients in whom masturbation fails."( [Tadalafil combined with behavior therapy for semen collection from infertile males in whom masturbation fails].
Gao, L; Hong, K; Jiang, H; Liu, DF; Ma, LL; Mao, JM; Qiao, J; Tang, WH; Yang, Y; Zhang, J; Zhao, LM, 2013)		1.53
"To observe the clinical effect of low-dose testosterone undecanoate capsules combined with tadalafil on late-onset hypogonadism (LOH) accompanied with ED."( [Low-dose testosterone undecanoate capsules combined with tadalafil for late-onset hypogonadism accompanied with ED].
Huang, CC; Li, GY; Liang, JH; Liang, SK; Meng, ZB; Shen, SL; Song, WR; Wei, GQ; Zhang, X; Zhu, CH, 2013)		0.85
"Ninety cases of LOH accompanied with ED who met the inclusion criteria were randomly divided into a control group and a combination therapy group, the former treated with tadalafil and the latter with low-dose testosterone undecanoate capsules combined with tadalafil."( [Low-dose testosterone undecanoate capsules combined with tadalafil for late-onset hypogonadism accompanied with ED].
Huang, CC; Li, GY; Liang, JH; Liang, SK; Meng, ZB; Shen, SL; Song, WR; Wei, GQ; Zhang, X; Zhu, CH, 2013)		0.83
"Low-dose testosterone undecanoate capsules combined with tadalafil has a definite clinical effect and no obvious adverse reactions in the treatment of LOH accompanied with ED."( [Low-dose testosterone undecanoate capsules combined with tadalafil for late-onset hypogonadism accompanied with ED].
Huang, CC; Li, GY; Liang, JH; Liang, SK; Meng, ZB; Shen, SL; Song, WR; Wei, GQ; Zhang, X; Zhu, CH, 2013)		0.88
"This study aimed to evaluate the efficacy and safety of long-term and low-dose tadalafil combined with sildenafil as needed at the early stage of treatment for erectile dysfunction (ED)."( Efficacy and safety of long-term tadalafil 5 mg once daily combined with sildenafil 50 mg as needed at the early stage of treatment for patients with erectile dysfunction.
Cui, H; Deng, Y; Fang, J; Liu, B; Song, Z; Wang, H; Wang, Z; Zhang, S, 2015)		0.93
"To observe the clinical effect of low-dose once-daily tadalafil combined with Shuganyiyang Capsules in the treatment of mild-to-moderate erectile dysfunction (ED)."( [Low-dose tadalafil combined with Shuganyiyang capsules for mild-to-moderate erectile dysfunction].
Chen, G; Fu, J; Huang, XJ; Lü, BD; Yang, KB; Zhang, SG, 2014)		1.05
"Low-dose once-daily tadalafil combined with Shuganyiyang Capsules is obviously effective in the treatment of mild-to-moderate ED, which not only improves the patients'erectile function, sexual self-confidence and sexual spontaneity, but also reduces their time concerns."( [Low-dose tadalafil combined with Shuganyiyang capsules for mild-to-moderate erectile dysfunction].
Chen, G; Fu, J; Huang, XJ; Lü, BD; Yang, KB; Zhang, SG, 2014)		1.13
"To evaluate the therapy efficacy of iloprost combined with low dose tadalafil in adult congenital heart disease (CHD) patients with severe pulmonary arterial hypertension (PAH)."( [Effects of iloprost combined with low dose tadalafil in adult congenital heart disease patients with severe pulmonary arterial hypertension: a single-center, open-label controlled study].
Chen, J; Huang, T; Huang, X; Huang, Y; Wu, S; Xia, C; Yao, H; Zhang, C; Zhang, G; Zhuang, J, 2014)		0.9
"Adult CHD patients with severe PAH were included and divided into the sequential combination therapy group [iloprost: 10 µg/inhalation, 6 times per day for 6 months, and then add oral tadalafil (5 mg/d) till 12 months, n = 32] and upfront combination therapy group [iloprost: 10 µg/inhalation, 6 times per day combined with oral tadalafil (5 mg) for 12 months, n = 36]."( [Effects of iloprost combined with low dose tadalafil in adult congenital heart disease patients with severe pulmonary arterial hypertension: a single-center, open-label controlled study].
Chen, J; Huang, T; Huang, X; Huang, Y; Wu, S; Xia, C; Yao, H; Zhang, C; Zhang, G; Zhuang, J, 2014)		0.85
"Iloprost combined with low dose tadalafil regimen can effectively reduce PVR, increase 6MWD, and improve cardiopulmonary function in adults CHD patients with severe PAH."( [Effects of iloprost combined with low dose tadalafil in adult congenital heart disease patients with severe pulmonary arterial hypertension: a single-center, open-label controlled study].
Chen, J; Huang, T; Huang, X; Huang, Y; Wu, S; Xia, C; Yao, H; Zhang, C; Zhang, G; Zhuang, J, 2014)		0.95
"To investigate a possible relation between penile Doppler ultrasound examination (PDUE) parameters and efficacy of chronic therapy with tadalafil (TAD) combined with a protocol of aerobic physical activity (PA) in patients with late onset hypogonadism (LOH)."( Effects of tadalafil treatment combined with physical activity in patients with low onset hypogonadism: results from a not-randomized single arm phase 2 study.
Calogero, AE; Condorelli, RA; Di Mauro, M; La Vignera, S; Mongioì, LM; Morgia, G; Russo, GI, 2016)		1.03
"To compare the effectiveness of the phosphodiesterase type 5 inhibitor (PDE-5i) tadalafil alone and in combination with a biologically active dietary supplement (BADS) NeyroDoz, containing the precursors of serotonin in patients with erectile dysfunction (ED) associated with secondary premature ejaculation (SPE)."( [New data on the effectiveness of Tadalafil alone and in combination with NeyroDoz in treating erectile dysfunction associated with secondary premature ejaculation].
Akhvlediani, ND; Matyukhov, IP, 2016)		0.94
"To evaluate the effect of the oral-appliance combined with tadalafil in the treatment of erectile dysfunction (ED) induced by severe obstructive sleep apnea-hypopnea syndrome (OSAHS)."( [Oral-appliance combined with tadalafil for erectile dysfunction induced by severe obstructive sleep apneahypopnea syndrome].
Li, WB; Pan, MA; Zhang, T, 2016)		0.97
"Oral-appliance combined with tadalafil can improve erectile function in patients with severe OSAHS-induced ED, with a better efficacy than either of them used alone."( [Oral-appliance combined with tadalafil for erectile dysfunction induced by severe obstructive sleep apneahypopnea syndrome].
Li, WB; Pan, MA; Zhang, T, 2016)		1.01
" This article aims to provide the latest evidence for the efficacy and safety of traditional Chinese medicine (TCM) combined with tadalafil in treatment of erectile dysfunction."( Chinese herbal medicine combined with tadalafil for erectile dysfunction: a systematic review and meta-analysis.
Geng, LG; He, CB; Wang, YL; Yuan, SY, 2020)		1.03
"All randomized controlled trials that Chinese herbal medicine combined with tadalafil for erectile dysfunction were included in databases of China National Knowledge Infrastructure (CNKI), Wanfang, Weip Database, China Biology Medicine disc (CBM), MEDLINE, EMBASE, and Cochrane Library."( Chinese herbal medicine combined with tadalafil for erectile dysfunction: a systematic review and meta-analysis.
Geng, LG; He, CB; Wang, YL; Yuan, SY, 2020)		1.06
" Compared with tadalafil alone, meta-analysis suggests there were statistically significant differences in International Index of Erectile Function-5 (IIEF-5), effective rate, Sexual Encounter Profile questions 2 and 3 (SEP-Q2, SEP-Q3) between traditional Chinese medicine combined with tadalafil, and no statistically significant differences in side effects between the two groups."( Chinese herbal medicine combined with tadalafil for erectile dysfunction: a systematic review and meta-analysis.
Geng, LG; He, CB; Wang, YL; Yuan, SY, 2020)		1.18
"Traditional Chinese medicine combined with tadalafil has significant efficacy in the treatment of ED with no increase in side effects."( Chinese herbal medicine combined with tadalafil for erectile dysfunction: a systematic review and meta-analysis.
Geng, LG; He, CB; Wang, YL; Yuan, SY, 2020)		1.09
"Aim of our systematic review is to evaluate and summarize the efficacy and safety of tadalafil alone or in combination with tamsulosin for the management of lower urinary tract symptoms (LUTS)/benign prostatic hyperplasia (BPH) and erectile dysfunction (ED)."( Tadalafil Alone or in Combination with Tamsulosin for the Management for LUTS/BPH and ED.
Chapple, C; Gacci, M; Gravas, S; Kaplan, S; McVary, KT; Morselli, S; Sebastianelli, A; Serni, S; Spatafora, P; Vignozzi, L, 2020)		2.22
"To explore the clinical value of phosphodiesterase type-5 inhibitors (PDE-5i) combined with RigiScan-based audiovisual sexual stimulation (AVSS) test in comparison with that of nocturnal penile tumescence (NPT) test in evaluation of erectile function."( [PDE-5i combined with RigiScan-based audiovisual sexual stimulation test versus nocturnal penile tumescence test in evaluation of erectile function].
Ashok, R; Dai, YT; Gao, QQ; Song, T; Sun, GH; Sun, XL; Xu, ZP; Yu, W, 2020)		0.56
"Compared with NPT test, PDE -5i combined with RigiScan-based AVSS test is simple, inexpensive, practical and with a high sensitivity and specificity, and therefore can be used as the first-choice strategy for etiological diagnosis of ED."( [PDE-5i combined with RigiScan-based audiovisual sexual stimulation test versus nocturnal penile tumescence test in evaluation of erectile function].
Ashok, R; Dai, YT; Gao, QQ; Song, T; Sun, GH; Sun, XL; Xu, ZP; Yu, W, 2020)		0.56
" In this study, we validated a discriminant analysis using an ultra-compact, portable, and low-cost Raman scattering spectrometer combined with multivariate analysis."( Detection Method of Falsified Medicines by Using a Low-Cost Raman Scattering Spectrometer Combined with Soft Independent Modeling of Class Analogy and Partial Least Squares Discriminant Analysis.
Kimura, K; Sanada, T; Tsuboi, H; Yoshida, N, 2021)		0.62
"To investigate the clinical effect of tadalafil combined with behavioral therapy and psychological counseling in the treatment of erectile dysfunction (ED)."( [Tadalafil combined with behavioral therapy and psychological counseling for erectile dysfunction].
Liu, X; Zhu, ZM, 2021)		1.8
"We collected the clinical data on 338 cases of ED treated in our andrology clinic with tadalafil combined with behavioral therapy and psychological counseling (the trial group, n = 159) or with tadalafil alone (the control group, n = 179) from January to December 2019."( [Tadalafil combined with behavioral therapy and psychological counseling for erectile dysfunction].
Liu, X; Zhu, ZM, 2021)		1.75
"Tadalafil combined with behavior therapy and psychological counseling is superior to oral tadalafil alone in the treatment of ED, which affords greater satisfaction with the therapeutic effect, higher quality of sexual life, and better relationship between the partners."( [Tadalafil combined with behavioral therapy and psychological counseling for erectile dysfunction].
Liu, X; Zhu, ZM, 2021)		2.97
"To observe the clinical effect and safety of Shanhaidan Granules (SHDG) combined with tadalafil tablets (TT) in the treatment of ED."( [Effect of Shanhaidan Granules combined with tadalafil on erectile dysfunction: A multi-center clinical trial].
Chen, L; Chen, WJ; Cheng, HJ; Huang, YP; Li, L; Lu, MJ; Peng, Y; Wu, ZM; Yang, NQ, 2021)		1.1
"Shanhaidan Granules combined with tadalafil can significantly improve the erectile function and reduce TCM syndromes in ED patients, and therefore can be applied effectively and safely in clinical practice."( [Effect of Shanhaidan Granules combined with tadalafil on erectile dysfunction: A multi-center clinical trial].
Chen, L; Chen, WJ; Cheng, HJ; Huang, YP; Li, L; Lu, MJ; Peng, Y; Wu, ZM; Yang, NQ, 2021)		1.16
"We examined the discontinuation rates of tadalafil alone and in combination with a-blockers (ABs) for the treatment of male lower urinary tract symptoms (LUTS), with or without erectile dysfunction (ED)."( Discontinuation Rates of Tadalafil Alone and in Combination with a-Blockers in the Treatment of Male Lower Urinary Tract Symptoms with or without Coexisting Erectile Dysfunction: A Systematic Review and Meta-Analysis.
Chen, Q; Mao, Y; Tang, S; Zhou, H, 2022)		1.29
"The discontinuation rate of tadalafil alone or in combination with ABs for LUTS with or without ED was relatively low and varied according to the study type."( Discontinuation Rates of Tadalafil Alone and in Combination with a-Blockers in the Treatment of Male Lower Urinary Tract Symptoms with or without Coexisting Erectile Dysfunction: A Systematic Review and Meta-Analysis.
Chen, Q; Mao, Y; Tang, S; Zhou, H, 2022)		1.32
"The study explored the clinical efficacy of a type 5 phosphodiesterase inhibitor (PDE5i) combined with Ziyin Baihuo granules in the treatment of patients suffering from erectile dysfunction (ED) with yin deficiency and fire-hyperactivity syndrome."( Analyzing the Clinical Efficacy of a Type 5 Phosphodiesterase Inhibitor Combined With Ziyin Baihuo Granules in the Treatment of Erectile Dysfunction.
Lv, KL; Nan, YH; Sun, WG; Wang, R; Zhang, TB; Zhang, WX; Zheng, T, )		0.13
"To investigate the clinical effect of dumai (governor meridian) moxibustion combined with low-dose tadalafil in the treatment of ED with decline of vital gate fire."( [Dumai moxibustion combined with low-dose tadalafil for erectile dysfunction: Evaluation of therapeutic effect].
DU, JG; Li, PC; Sun, ZX; Wei, XX; Zhang, XH; Zhang, ZG, 2023)		1.39
"Dumai moxibustion combined with low-dose tadalafil can improve erectile function, increase penile blood flow velocity and alleviate clinical symptoms in ED patients with decline of vital gate fire, with definite clinical effect and safety."( [Dumai moxibustion combined with low-dose tadalafil for erectile dysfunction: Evaluation of therapeutic effect].
DU, JG; Li, PC; Sun, ZX; Wei, XX; Zhang, XH; Zhang, ZG, 2023)		1.44

Bioavailability

This study aims at improving the bioavailability of a poorly soluble phosphodiesterase-5 inhibitor; tadalafil (TD) via developing intranasal (IN) nanoemulsions (NEs)

ExcerptReferenceRelevance
" It is as efficacious as sildenafil in in vitro and in vivo PDE5 inhibition models, and it is orally bioavailable in rats and dogs."( Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Adam, L; Beyer, B; Chong, S; Ferrer, P; He, B; Henwood, A; Humphrey, WG; Krupinski, J; Macor, JE; Mason, H; Normandin, D; Pongrac, R; Seliger, L; Wang, J; Wu, X; Yu, G; Zhang, R, 2003)		0.32
" The validated method has been successfully used to analyze human plasma samples for application in pharmacokinetic, bioavailability or bioequivalence studies."( Quantitation of tadalafil in human plasma by liquid chromatography-tandem mass spectrometry with electrospray ionization.
Chidambara, J; Koteshwara, M; Manoj, S; Puran, S; Ramakrishna, NV; Santosh, M; Sumatha, B; Vishwottam, KN; Wishu, S, 2004)		0.67
" Unfortunately, the low aqueous solubility and poor oral bioavailability rendered them undesirable development candidates."( Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
Bhattacharjee, S; Guan, J; Haynes-Johnson, D; Jiang, W; John, TM; Kraft, P; Lundeen, S; Macielag, MJ; Qiu, Y; Sui, Z; Zhang, S, 2005)		0.33
" This review comparatively discusses the major characteristics of the pharmacokinetic profile of all 3 PDE5 inhibitors, including bioavailability and rate of absorption, Biopharmaceutical Classification System categorization, elimination mechanisms, and metabolic profile including active metabolites, as well as the drug-drug interaction potential and modification of pharmacokinetic properties under selected physiologic and pathophysiologic conditions."( The clinical pharmacokinetics of phosphodiesterase-5 inhibitors for erectile dysfunction.
Gupta, M; Kovar, A; Meibohm, B, 2005)		0.33
" Food had negligible effects on bioavailability as assessed by 90% confidence intervals for Cmax and AUC mean ratios."( Tadalafil pharmacokinetics in healthy subjects.
Bedding, AW; Forgue, ST; Mitchell, MI; Patterson, BE; Payne, CD; Phillips, DL; Wrishko, RE, 2006)		1.78
"High-altitude pulmonary edema (HAPE) is caused by exaggerated hypoxic pulmonary vasoconstriction associated with decreased bioavailability of nitric oxide in the lungs and by impaired reabsorption of alveolar fluid."( Both tadalafil and dexamethasone may reduce the incidence of high-altitude pulmonary edema: a randomized trial.
Bärtsch, P; Bernheim, A; Bloch, KE; Böhm, T; Brunner-La Rocca, HP; Dehnert, C; Fischler, M; Kiencke, S; Lehmann, T; Maggiorini, M; Mairbäurl, H; Naeije, R; Peth, S, 2006)		0.85
" The absorption rate was rapid (1."( Tadalafil population pharmacokinetics in patients with erectile dysfunction.
Forgue, ST; Rapado, J; Staab, A; Tillmann, C; Trocóniz, IF, 2007)		1.78
" There is increasing evidence suggesting that dysfunction of the vascular endothelium with reduced bioavailability of nitric oxide (NO) may be the pathogenetic link between ED and cardiovascular disease."( [Chronic PDE-5 inhibition in patients with erectile dysfunction: new treatment approach using once daily Tadalafil].
Büttner, H; Hell-Momeni, K; Porst, H, 2009)		0.57
" Solid dispersion approach represents a promising carrier system for effective enhancement of dissolution and oral bioavailability of poorly soluble drugs."( In sight into tadalafil - block copolymer binary solid dispersion: Mechanistic investigation of dissolution enhancement.
Mehanna, MM; Motawaa, AM; Samaha, MW, 2010)		0.72
"Insulin resistance impairs nitric oxide (NO) bioavailability and obesity promotes a state of chronic inflammation and damages the vascular endothelium."( Anti-inflammatory and cardioprotective effects of tadalafil in diabetic mice.
Das, A; Durrant, DE; Hoke, NN; Kukreja, RC; Salloum, FN; Varma, A, 2012)		0.63
" Solid dispersion (SD) techniques are widely used to improve the bioavailability of drugs that are poorly water-soluble."( Design of PVP/VA S-630 based tadalafil solid dispersion to enhance the dissolution rate.
Choi, JS; Park, JS, 2017)		0.75
"The purpose of this study is to improve the solubility, in vitro dissolution, and oral bioavailability in rats of tadalafil (TDF) by using SD technique with a weak acid and a copolymer."( Use of acidifier and solubilizer in tadalafil solid dispersion to enhance the in vitro dissolution and oral bioavailability in rats.
Byeon, JC; Choi, JS; Jang, WS; Jeong, HM; Kwon, SH; Lee, SE; Park, JS, 2017)		0.94
" Importantly, the bioavailability of this poorly water-soluble drug could be substantially increased with the proposed formulations, and the in vitro and in vivo release rates could be effectively adjusted by choosing the appropriate type of carrier material: Whereas mannitol-based ground hot-melt extrudates rapidly released the drug and led to an early rise in drug plasma concentrations, Soluplus-based systems released tadalafil more slowly, resulting in delayed plasma peaks."( In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release.
Cantin, O; Jachowicz, R; Krupa, A; Siepmann, J; Strach, B; Tabor, Z; Wróbel, A; Wyska, E, 2017)		0.89
"Here, solid dispersion (SD) techniques were utilized to improve the oral bioavailability of tadalafil (TDF)."( Tadalafil solid dispersion formulations based on PVP/VA S-630: Improving oral bioavailability in rats.
Byeon, JC; Choi, JS; Jang, WS; Lee, SE; Park, JS, 2017)		2.12
" One way to increase the bioavailability of these drugs is to use a supersaturating drug delivery strategy."( Development of a Video-Microscopic Tool To Evaluate the Precipitation Kinetics of Poorly Water Soluble Drugs: A Case Study with Tadalafil and HPMC.
Andersen, K; Christfort, JF; Madsen, CM; Müllertz, A; Nielsen, LH; Plum, J; Rades, T; Sandau, M, 2017)		0.66
"Co-amorphous drug delivery systems are a promising approach to improve the dissolution rate and therefore potentially the oral bioavailability of poorly-water soluble drugs."( Aspartame as a co-former in co-amorphous systems.
Grohganz, H; Knuhtsen, A; Löbmann, K; Pedersen, DS; Rades, T; Schnitzkewitz, J; Wu, W, 2018)		0.48
"The ability to increase the bioavailability and dissolution of poorly soluble hydrophobic drugs has been a major challenge for pharmaceutical development."( Enhancement of the apparent solubility and bioavailability of Tadalafil nanoparticles via antisolvent precipitation.
Guan, S; Huang, D; Li, Q; Liu, Y; Lu, T; Luo, D; Pan, P; Qiu, Z; Rao, Q; Zhang, L; Zhang, ZJ, 2019)		0.75
" More importantly, the samples prepared by such strategy exhibited a substantially improved bioavailability compared to the samples that were prepared by either spray-dried or hot-melt extruded processes."( Hot melt extrusion of heat-sensitive and high melting point drug: Inhibit the recrystallization of the prepared amorphous drug during extrusion to improve the bioavailability.
Guan, S; Huang, D; Li, Q; Liamas, E; Lu, M; Pan, P; Rao, Q; Xie, Z; Zhang, ZJ, 2019)		0.51
" In part 2, granulation size was found to not affect the relative bioavailability of the selected formulation."( A Phase I Study to Show the Relative Bioavailability and Bioequivalence of Fixed-Dose Combinations of Ambrisentan and Tadalafil in Healthy Subjects.
Berni, A; Chen, G; Khindri, S; Okour, M; Port, K; Puri, A; Schneider, I; Tenero, D, 2019)		0.72
"This study aims at improving the bioavailability of a poorly soluble phosphodiesterase-5 inhibitor; tadalafil (TD) via developing intranasal (IN) nanoemulsions (NEs)."( Intranasal Tadalafil nanoemulsions: formulation, characterization and pharmacodynamic evaluation.
Abdelmonsif, DA; Boraie, N; Elbardisy, B; Galal, S, 2019)		1.12
" Other covariate effects were that bosentan increased CL/F, V/F decreased with decreasing body weight, and bioavailability (F) decreased with increasing dose and decreasing age."( Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Ferguson-Sells, L; Li, B; Small, D; Velez de Mendizabal, N, 2022)		1.01
"A one-compartment model parameterized in terms of F, absorption rate constant, CL/F, and V/F described the data well."( Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Ferguson-Sells, L; Li, B; Small, D; Velez de Mendizabal, N, 2022)		1.01
" The oral bioavailability of this formulation is higher than that of the parent drug."( Lodenafil.
Al-Majed, AA; Alshehri, YM; Attwa, MW; Bakheit, AH, 2022)		0.72

Dosage Studied

Chronic dosing of tadalafil improves QoL of patients post-nsRP. A recent randomised, controlled Phase II trial revealed that tadalfil dosed once daily was well tolerated. The percentage of patients who achieved a normal EF domain score depended on the severity of erectile dysfunction.

ExcerptRelevanceReference
" The efficacy and safety of on-demand dosing of IC351 in men with erectile dysfunction was assessed in a multicenter, double-blind, placebo-controlled study."( On-demand IC351 (Cialis) enhances erectile function in patients with erectile dysfunction.
Ferguson, KM; McMurray, JG; Padma-Nathan, H; Pullman, WE; Rosen, RC; Saoud, JB; Whitaker, JS, 2001)		0.31
" After a 10- to 21-day washout period, subjects crossed over to either placebo or tadalafil, and nitrate dosing was repeated."( Time course of the interaction between tadalafil and nitrates.
Denne, J; Emmick, JT; Hutter, AM; Jackson, G; Kloner, RA; Mitchell, MI, 2003)		0.81
" Although the study sought to mimic the experience of actual patients receiving treatment for ED, the results are subject to potential limitations due to the design of the study, which included differences in dosing instructions and dosages for sildenafil and tadalafil."( Switching patients with erectile dysfunction from sildenafil citrate to tadalafil: results of a European multicenter, open-label study of patient preference.
Costigan, T; Murphy, A; Ströberg, P, 2003)		0.73
"To assess patient preference for erectile dysfunction treatment between either sildenafil or tadalafil, each administered with their respective dosing instructions, and to evaluate preference for either sildenafil or tadalafil dosing instructions during tadalafil therapy."( A multicenter, randomized, double-blind, crossover study to evaluate patient preference between tadalafil and sildenafil.
Beasley, CM; Costigan, T; Denne, J; Emmick, JT; Lockhart, D; Murphy, A; Rajfer, J; Segal, S; von Keitz, A, 2004)		0.76
" Because the dosing instructions for sildenafil and tadalafil are different, a unique methodology using sham placebo arms was employed to maintain the blind."( A multicenter, randomized, double-blind, crossover study to evaluate patient preference between tadalafil and sildenafil.
Beasley, CM; Costigan, T; Denne, J; Emmick, JT; Lockhart, D; Murphy, A; Rajfer, J; Segal, S; von Keitz, A, 2004)		0.79
"In the doses utilized in this study, 73% of patients preferred tadalafil with tadalafil dosing instructions for the treatment of their erectile dysfunction over sildenafil with sildenafil dosing instructions."( A multicenter, randomized, double-blind, crossover study to evaluate patient preference between tadalafil and sildenafil.
Beasley, CM; Costigan, T; Denne, J; Emmick, JT; Lockhart, D; Murphy, A; Rajfer, J; Segal, S; von Keitz, A, 2004)		0.78
" Tadalafil was effective up to 36 h after dosing and was effective regardless of disease severity and causes, and in patients of all ages."( The efficacy and safety of tadalafil: an update.
Carrier, S; Carson, CC; Cordell, WH; Denne, JS; Eardley, I; Rajfer, J; Shen, W; Walker, DJ, 2004)		1.53
"To determine the population dose-response relationship for tadalafil during on-demand (as-needed) administration for treatment of erectile dysfunction (ED)."( Population dose-response model for tadalafil in the treatment of male erectile dysfunction.
Allerheiligen, SR; Forgue, ST; Mackie, A; Rapado, J; Staab, A; Tillmann, C; Trocóniz, IF, 2004)		0.84
"The dose-response relationship for each efficacy variable was best described with an Emax model, in which maximum effect increased with ED severity at baseline."( Population dose-response model for tadalafil in the treatment of male erectile dysfunction.
Allerheiligen, SR; Forgue, ST; Mackie, A; Rapado, J; Staab, A; Tillmann, C; Trocóniz, IF, 2004)		0.6
"Population dose-response modeling of all five oucome measures indicated that efficacy in all ED severity groups in the studied population generally increased across the 2 to 25 mg tadalafil dose range."( Population dose-response model for tadalafil in the treatment of male erectile dysfunction.
Allerheiligen, SR; Forgue, ST; Mackie, A; Rapado, J; Staab, A; Tillmann, C; Trocóniz, IF, 2004)		0.79
" Blood pressure (BP) and heart rate were recorded before dosing and for 24 hours after dosing."( Interaction between the phosphodiesterase 5 inhibitor, tadalafil and 2 alpha-blockers, doxazosin and tamsulosin in healthy normotensive men.
Bedding, A; Emmick, JT; Jackson, G; Kloner, RA; Mitchell, MI; Pereira, A; Warner, MR, 2004)		0.57
"To examine the preference for 2 dosing regimens (on demand or 3 times/week) for tadalafil, a phosphodiesterase 5 inhibitor with a duration of effectiveness up to 36 hours in men with erectile dysfunction (ED)."( An evaluation of an alternative dosing regimen with tadalafil, 3 times/week, for men with erectile dysfunction: SURE study in 14 European countries.
Chan, M; Cordell, WH; Costa, P; Damber, JE; Holmes, S; Lembo, D; Mirone, V; Moncada, I; Van Ahlen, H; Varanese, L; Wespes, E, 2005)		0.81
" The two regimens provide additional treatment options by giving men with erectile dysfunction unique flexibility in dosing with tadalafil."( An evaluation of an alternative dosing regimen with tadalafil, 3 times/week, for men with erectile dysfunction: SURE study in 14 European countries.
Chan, M; Cordell, WH; Costa, P; Damber, JE; Holmes, S; Lembo, D; Mirone, V; Moncada, I; Van Ahlen, H; Varanese, L; Wespes, E, 2005)		0.78
" The review is aimed at providing comparative clinical pharmacology data to allow for scientifically rational, evidence-based prescribing and dosing decisions regarding the clinical use of these medications for the treatment of erectile dysfunction."( The clinical pharmacokinetics of phosphodiesterase-5 inhibitors for erectile dysfunction.
Gupta, M; Kovar, A; Meibohm, B, 2005)		0.33
" A post hoc analysis was used to determine the proportion of men with ED who attempted sexual intercourse during various intervals (>0 to < or = 1, >1 to < or = 4, and >4 to < or = 36, including >12 to < or = 36 h) after dosing with tadalafil or placebo over a 12-week period."( Time from dosing to sexual intercourse attempts in men taking tadalafil in clinical trials.
Ahuja, S; Burnett, AL; Eardley, I; Ellsworth, PI; Garcia, CS; Natanegara, F; Shabsigh, R; Sharlip, ID, 2005)		0.75
"To describe the pattern of sexual attempts by men with erectile dysfunction (ED) taking tadalafil 20 mg on demand or on an alternative dosing regimen, 3 times/week, and to assess changes in sexual behavior when the patients were exposed to the alternative regimen."( Sexual intercourse attempt patterns with two dosing regimens of tadalafil in men with erectile dysfunction: results from the SURE study in 14 European countries.
Casariego, J; Chan, M; Damber, JE; Mirone, V; Moncada, I; Varanese, L; Wespes, E, 2005)		0.79
"Patients on tadalafil changed their sexual behavior significantly when on an alternative dosing regimen (3 times/week) and had sexual attempts distributed over a wide period of time post dosing."( Sexual intercourse attempt patterns with two dosing regimens of tadalafil in men with erectile dysfunction: results from the SURE study in 14 European countries.
Casariego, J; Chan, M; Damber, JE; Mirone, V; Moncada, I; Varanese, L; Wespes, E, 2005)		0.95
"Compared with pretreatment and on-demand tadalafil baseline, daily dosed tadalafil significantly enhanced all efficacy outcome variables."( Efficacy and safety of daily tadalafil in men with erectile dysfunction previously unresponsive to on-demand tadalafil.
McMahon, C, 2004)		0.88
" Using a stopwatch, couples recorded in Sexual Encounter Profile diaries the earliest time within 30 minutes after dosing to the first erection adequate for vaginal penetration, and whether the erection led to successful intercourse."( Determining the earliest time within 30 minutes to erectogenic effect after tadalafil 10 and 20 mg: a multicenter, randomized, double-blind, placebo-controlled, at-home study.
Padma-Nathan, H; Pullman, W; Rosen, RC; Saikali, K; Shabsigh, R; Watkins, V, 2004)		0.55
"This stopwatch-based study demonstrated a pharmacodynamic effect within 30 minutes after dosing for tadalafil 10 and 20 mg."( Determining the earliest time within 30 minutes to erectogenic effect after tadalafil 10 and 20 mg: a multicenter, randomized, double-blind, placebo-controlled, at-home study.
Padma-Nathan, H; Pullman, W; Rosen, RC; Saikali, K; Shabsigh, R; Watkins, V, 2004)		0.77
" Fifty-nine percent of intercourse attempts were within 4 hours of dosing when patients were treated with tadalafil (88% with sildenafil)."( Timing of dose relative to sexual intercourse attempt in previous sildenafil citrate users treated with tadalafil.
Dyachkova, Y; Gatchalian, E; Glina, S; Kopernicky, V; Markey, C; Sotomayor, M; Yaman, O, 2006)		0.76
"Following the dosing instructions reflecting tadalafil's extended period of effectiveness, men with a history of established sildenafil use changed their dose-attempt behavior when treated with tadalafil."( Timing of dose relative to sexual intercourse attempt in previous sildenafil citrate users treated with tadalafil.
Dyachkova, Y; Gatchalian, E; Glina, S; Kopernicky, V; Markey, C; Sotomayor, M; Yaman, O, 2006)		0.81
" Phase 2: true non-responders were given new instructions based on drugs' pharmacologic profiles: TGs were dosed at least 2 h before intercourse; VGs were dosed only in fasted state."( Treatment strategy for "non-responders" to tadalafil and vardenafil: a real-life study.
Bekos, A; Hatzichristou, D; Hatzimouratidis, K; Ioannidis, E; Moysidis, K; Tsimtsiou, Z, 2006)		0.6
" Phase 2, 22 of 88 (25%) responded to dosing in a fasted state."( Treatment strategy for "non-responders" to tadalafil and vardenafil: a real-life study.
Bekos, A; Hatzichristou, D; Hatzimouratidis, K; Ioannidis, E; Moysidis, K; Tsimtsiou, Z, 2006)		0.6
" tadalafil and for their respective dosing instructions in a cohort of Spanish patients with erectile dysfunction (ED)."( [Tadalafil vs sildenafil patient preference in Spanish men with erectile dysfunction: results from an International Multicentric Study].
Casariego, J; Cassinello, A; Lledó García, E; Mo, D; Rajmil, O; Rodríguez Vela, L, 2006)		2.15
" Similarly, to evaluate preference for their respective dosing instructions, 30 patients were randomized to one of the 2 arms treated with tadalafil: one with sildenafil (S) dosing instructions and the other with tadalafil (T) dosing instructions."( [Tadalafil vs sildenafil patient preference in Spanish men with erectile dysfunction: results from an International Multicentric Study].
Casariego, J; Cassinello, A; Lledó García, E; Mo, D; Rajmil, O; Rodríguez Vela, L, 2006)		1.45
" Correspondingly, 73% of 13 evaluating each drug dosing instructions preferred T dosing instructions (p>0."( [Tadalafil vs sildenafil patient preference in Spanish men with erectile dysfunction: results from an International Multicentric Study].
Casariego, J; Cassinello, A; Lledó García, E; Mo, D; Rajmil, O; Rodríguez Vela, L, 2006)		1.24
"In this study, 7 out of 10 patients preferred tadalafil and its dosing instructions to sildenafil, for the treatment of their ED."( [Tadalafil vs sildenafil patient preference in Spanish men with erectile dysfunction: results from an International Multicentric Study].
Casariego, J; Cassinello, A; Lledó García, E; Mo, D; Rajmil, O; Rodríguez Vela, L, 2006)		1.5
"5-h half-life of tadalafil enables therapeutic plasma levels to be sustained with daily administration, tadalafil is a good candidate for once daily dosing therapy."( Evaluation of the efficacy and safety of once-a-day dosing of tadalafil 5mg and 10mg in the treatment of erectile dysfunction: results of a multicenter, randomized, double-blind, placebo-controlled trial.
Casabé, AR; Elion-Mboussa, A; Giuliano, F; Glina, S; Porst, H; Ralph, D; Shen, W; Whitaker, JS, 2006)		0.91
" A recent randomised, controlled Phase II trial of tadalafil versus placebo for the treatment of symptomatic BPH revealed that tadalafil dosed once daily was well tolerated and demonstrated statistically significant and clinically meaningful efficacy in the treatment of LUTS secondary to BPH and improved erectile function in men with both LUTS and ED."( Tadalafil for the treatment of lower urinary tract symptoms in men with benign prostatic hyperplasia.
Gonzalez, RR; Kaplan, SA, 2006)		2.03
"The efficacy and safety of tadalafil, dosed once a day for the treatment of erectile dysfunction, was assessed in a randomized, double-blind, placebo-controlled, parallel-design study at 15 US centers."( Tadalafil dosed once a day in men with erectile dysfunction: a randomized, double-blind, placebo-controlled study in the US.
Aliotta, PJ; Fitch, WP; Rajfer, J; Steidle, CP; Yu, A; Zhao, Y, )		1.87
"To determine whether patient characteristics influence the efficacy of two tadalafil dosage regimens and to identify prognostic factors predictive of tadalafil efficacy."( Predictors of tadalafil efficacy in men with erectile dysfunction: the SURE study comparing two dosing regimens.
Buvat, J; Costa, P; Hamidi, K; Holmes, S; Petto, H; Varanese, L; Weitckus, S, 2006)		0.92
" The percentage of patients who achieved a normal EF domain score and the percentages reporting positive responses to SEP3 and SEP5 depended on the severity of erectile dysfunction and the presence of certain comorbidities, irrespective of the tadalafil dosage regimen."( Predictors of tadalafil efficacy in men with erectile dysfunction: the SURE study comparing two dosing regimens.
Buvat, J; Costa, P; Hamidi, K; Holmes, S; Petto, H; Varanese, L; Weitckus, S, 2006)		0.88
"On-demand and three-times-per-week dosage regimens of tadalafil 20 mg were equally efficacious in men with erectile dysfunction."( Predictors of tadalafil efficacy in men with erectile dysfunction: the SURE study comparing two dosing regimens.
Buvat, J; Costa, P; Hamidi, K; Holmes, S; Petto, H; Varanese, L; Weitckus, S, 2006)		0.94
"To evaluate whether patterns of sexual activity and efficacy over time to two dosing regimens of tadalafil differ with ageing in men with erectile dysfunction (ED)."( The influence of age on treatment outcomes in men with erectile dysfunction treated with two regimens of tadalafil: results of the SURE study.
Chan, M; Jungwirth, A; Moncada, I; Schmitt, H; Varanese, L; Wespes, E, 2007)		0.77
" A high percentage of attempts occurred >4 h after dosing for all age groups ( approximately 70% for men taking tadalafil three times per week and approximately 50% for men taking tadalafil on-demand)."( The influence of age on treatment outcomes in men with erectile dysfunction treated with two regimens of tadalafil: results of the SURE study.
Chan, M; Jungwirth, A; Moncada, I; Schmitt, H; Varanese, L; Wespes, E, 2007)		0.76
" Tadalafil was effective up to 36 h after dosing for all age groups."( The influence of age on treatment outcomes in men with erectile dysfunction treated with two regimens of tadalafil: results of the SURE study.
Chan, M; Jungwirth, A; Moncada, I; Schmitt, H; Varanese, L; Wespes, E, 2007)		1.46
"We assessed the efficacy and safety of tadalafil dosed once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia."( Tadalafil relieves lower urinary tract symptoms secondary to benign prostatic hyperplasia.
Auerbach, SM; Denes, BS; Esler, A; Kaminetsky, JC; McVary, KT; Roehrborn, CG; Sides, GD; Wachs, B; Young, JM, 2007)		2.05
"To examine the preference for two dosing regimens of 20 mg of tadalafil, on demand or three times per week, in men affected with erectile dysfunction (ED) in Italy."( Evaluation of an alternative dosing regimen with tadalafil, three times per week, for men with erectile dysfunction: SURE study in Italy.
Fusco, F; Imbimbo, C; Longo, N; Mirone, V; Rossi, A; Sicuteri, R; Valle, D, 2007)		0.83
"In an open-label, crossover study of sildenafil (25, 50 or 100 mg) and tadalafil (10 or 20 mg), dosed as needed, after a 4-week baseline assessment, 367 men with ED were randomly assigned to sildenafil followed by tadalafil or vice versa (8-week dose optimization and 4-week assessment phase for each treatment period)."( Factors associated with preference for sildenafil citrate and tadalafil for treating erectile dysfunction in men naïve to phosphodiesterase 5 inhibitor therapy: post hoc analysis of data from a multicentre, randomized, open-label, crossover study.
Beardsworth, A; Chan, ML; Eardley, I; Jackson, G; Loughney, K; Mirone, V; Montorsi, F; Vail, GM, 2007)		0.81
" Dosage choice, reductions in the PAIRS time concerns domain, IIEF intercourse satisfaction domain improvements, smaller side-effect severity scores, more sexual attempts, and increased SEP4 scores (satisfaction with erection hardness) during the tadalafil or sildenafil treatment periods were all significantly associated with preference for tadalafil or sildenafil."( Factors associated with preference for sildenafil citrate and tadalafil for treating erectile dysfunction in men naïve to phosphodiesterase 5 inhibitor therapy: post hoc analysis of data from a multicentre, randomized, open-label, crossover study.
Beardsworth, A; Chan, ML; Eardley, I; Jackson, G; Loughney, K; Mirone, V; Montorsi, F; Vail, GM, 2007)		0.76
" Patient differences in time concerns, dosage choice, intercourse satisfaction, treatment tolerability, number of sexual attempts and satisfaction with erection hardness were the set of factors most significantly associated with treatment preference, and the preference observed for tadalafil (71%) or sildenafil (29%) might be substantially accounted for by differences in these factors during the tadalafil and sildenafil treatment periods."( Factors associated with preference for sildenafil citrate and tadalafil for treating erectile dysfunction in men naïve to phosphodiesterase 5 inhibitor therapy: post hoc analysis of data from a multicentre, randomized, open-label, crossover study.
Beardsworth, A; Chan, ML; Eardley, I; Jackson, G; Loughney, K; Mirone, V; Montorsi, F; Vail, GM, 2007)		0.76
" The incidence of hypotension was low in healthy men given increasing doses of doxazosin with chronically dosed tadalafil or placebo."( Hemodynamic interaction between a daily dosed phosphodiesterase 5 inhibitor, tadalafil, and the alpha-adrenergic blockers, doxazosin and tamsulosin, in middle-aged healthy male subjects.
Darstein, C; Guillaume, M; Jimenez, MC; Lonsdale, F; Mitchell, MI, 2007)		0.78
"5 hours) and its prolonged period of responsiveness (36-hours), constitute an ideal pharmacokinetic profile for once-a-day dosing and makes it an ideal candidate for rehabilitative therapy in DM patients, whereas a poor compliance with on-demand schedule is reported."( Redefining the role of long-acting phosphodiesterase inhibitor tadalafil in the treatment of diabetic erectile dysfunction.
Aversa, A; Bruzziches, R; Francomano, D; Greco, EA; Pili, M; Spera, G, 2008)		0.59
"With once-daily administration of tadalafil, dosing and sexual activity would no longer need to be temporally linked for patients with erectile dysfunction (ED)."( Long-term safety and efficacy of tadalafil 5 mg dosed once daily in men with erectile dysfunction.
Casabé, A; Esler, A; Feldman, R; Klise, SR; Porst, H; Rajfer, J; Ralph, D; Vieiralves, LF; Wolka, AM, 2008)		0.91
"To evaluate long-term safety and efficacy of tadalafil 5 mg dosed once daily for the treatment of ED."( Long-term safety and efficacy of tadalafil 5 mg dosed once daily in men with erectile dysfunction.
Casabé, A; Esler, A; Feldman, R; Klise, SR; Porst, H; Rajfer, J; Ralph, D; Vieiralves, LF; Wolka, AM, 2008)		0.89
"In these long-term, open-label, once-daily dosing studies, tadalafil 5 mg was well tolerated and effective, making it a viable alternative to the current on-demand dosing of tadalafil for men with ED."( Long-term safety and efficacy of tadalafil 5 mg dosed once daily in men with erectile dysfunction.
Casabé, A; Esler, A; Feldman, R; Klise, SR; Porst, H; Rajfer, J; Ralph, D; Vieiralves, LF; Wolka, AM, 2008)		0.87
" International Prostate Symptom Score improvements at 4, 8 and 12 weeks were significant for all tadalafil doses and they demonstrated a dose-response relationship."( Tadalafil administered once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia: a dose finding study.
Elion-Mboussa, A; McVary, KT; Roehrborn, CG; Viktrup, L, 2008)		2.01
" In a multicenter, open-label study, 1911 men received tadalafil 20 mg dosed as needed (up to once daily), for 12 weeks following a 4-week treatment-free run-in period."( Response to treatment with tadalafil in men with erectile dysfunction who reported no successful intercourse attempts at baseline.
Kim, ED; Muram, D; Natanegara, F; Rosen, RC; Shabsigh, R; Shinghal, R; Wong, DG, )		0.68
" Tadalafil is well-tolerated, consistent with the principle of safely, effectiveness and convenient dosing and is becoming the favorite choice of ED patients and their partners."( [Tadalafil for erectile dysfunction: outstanding efficacy for 36 hours].
Deng, SM, 2008)		2.17
" Findings from an integrated analysis of trials of tadalafil 10 and 20 mg as needed are presented to provide context for the daily dosing regime."( Efficacy and safety of tadalafil once daily: considerations for the practical application of a daily dosing option.
Donatucci, CF; Dowsett, SA; Giuliano, F; Glina, S; Sorsaburu, S; Watts, S; Wong, DG, 2008)		0.91
" For patients with a score lower than 26 in the erectile domain of the International Index of Erectile Function (IIEF15) and with total unsuccessful sexual attempts of more than 25% according to the Sexual Encounter Profile questions 2 and 3 (SEP2-3), the dosage of tadalafil was increased to 20 mg."( Efficacy and safety of medium and long-term tadalafil use in spinal cord patients with erectile dysfunction.
Cecconi, F; Del Popolo, G; Lombardi, G; Macchiarella, A, 2009)		0.79
" Development of the first once-daily alternative dosing regimen with a PDE5 inhibitor was motivated by the behavioral complexities associated with sexual intimacy."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.58
"To provide an alternative dosing option for certain men who may benefit from the removal of the temporal linkage between administration of an ED therapy and sexual intimacy or for men and their partners who anticipate at least twice-weekly sexual activity."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.58
"Based upon pharmacodynamic and pharmacokinetic data, once-daily doses of tadalafil 5 mg were predicted to provide therapeutic concentrations that would be maintained throughout the 24-hour dosing interval."( Safety, efficacy, and pharmacokinetic overview of low-dose daily administration of tadalafil.
McGill, J; Sorsaburu, S; Strawbridge, A; Wong, D; Wrishko, R, 2009)		0.81
" Dosing instructions were provided."( Timing of dose relative to sexual intercourse attempt in previous sildenafil citrate users treated with tadalafil: a geographical comparison from a single arm, open-label study.
Abdo, CH; Gallagher, GL; Glina, S; Hernandez-Serrano, R; Lenero, E; Rampazzo, C; Rubio-Aurioles, E; Sotomayor, M; West, TM, 2009)		0.57
" However, the extent to which sexual behavior alters is not uniform across geographical regions, suggesting that dosing instructions and duration of drug effectiveness, in combination with personal and cultural preferences, may determine sexual behavior with PDE5 inhibitor use."( Timing of dose relative to sexual intercourse attempt in previous sildenafil citrate users treated with tadalafil: a geographical comparison from a single arm, open-label study.
Abdo, CH; Gallagher, GL; Glina, S; Hernandez-Serrano, R; Lenero, E; Rampazzo, C; Rubio-Aurioles, E; Sotomayor, M; West, TM, 2009)		0.57
" Daily dosing may be useful in some men; however, the other available PDE5I continue to show excellent efficacy in the management of erectile dysfunction (ED)."( 2009 update on phosphodiesterase type 5 inhibitor therapy part 2: updates on optimal utilization for sexual concerns and rare toxicities in this class.
Shindel, AW, 2009)		0.35
" Interestingly in a pilot study of on-demand versus chronic administration of Tadalafil for 4 weeks, only regular dosing improved several markers of endothelial function."( [Chronic PDE-5 inhibition in patients with erectile dysfunction: new treatment approach using once daily Tadalafil].
Büttner, H; Hell-Momeni, K; Porst, H, 2009)		0.8
" Although the tablets contained efficacious amounts of PDE-5 inhibitors, neither the active ingredient nor the dosage corresponded to the description on the blister."( The identification of (-)-trans-tadalafil, tadalafil, and sildenafil in counterfeit Cialis and the optical purity of tadalafil stereoisomers.
de Kaste, D; Venhuis, BJ; Vredenbregt, MJ; Zomer, G, 2010)		0.64
" As the second PDE-5 inhibitor to gain approval for PAH, clinical properties such as its long half-life leading to once-daily dosing and possibly improved compliance, as well as potential cost benefit, may distinguish tadalafil from sildenafil in the widespread treatment of PAH."( Tadalafil for the treatment of pulmonary arterial hypertension.
Rosenzweig, EB, 2010)		1.99
"There were significant improvements in edema, glomerular filtration rate (GFR), weight, and loop diuretic dosage required, while strong trends were seen in urine output per day and urine output per unit loop diuretic per day."( The successful use of phosphodiesterase type 5 inhibitors to treat the syndrome of cor pulmonale and prerenal azotemia with diuresis of anasarca (CorPRADA).
Berez, PB, 2010)		0.36
" Those with a score lower than 26 on the International Index of Erectile Function (IIEF-15) and with less than 75% of total successful sexual attempts assessed by the Sexual Encounter Profile Questions 2 and 3 (SEP2-3) had their dosage of tadalafil increased to 20 mg, whereas responding subjects continued with 10 mg."( Efficacy and safety of tadalafil for erectile dysfunction in patients with multiple sclerosis.
Del Popolo, G; Lombardi, G; Macchiarella, A, 2010)		0.85
"A simple and accurate method to determine tadalafil (TAD) in pure powder and tablet dosage form was developed and validated using HPLC."( Determination of tadalafil in pure powder and tablet dosage form by high-performance liquid chromatography.
Barot, TG; Patel, PK, )		0.74
"The maximal beneficial effects of OAD dosing with 10 mg tadalafil may occur only after as many as 12 weeks."( Hypogonadal men nonresponders to the PDE5 inhibitor tadalafil benefit from normalization of testosterone levels with a 1% hydroalcoholic testosterone gel in the treatment of erectile dysfunction (TADTEST study).
Buvat, J; Colson, MH; Cuzin, B; Dean, JD; Eardley, I; Kaipia, A; Maggi, M; Martin-Morales, A; Meuleman, E; Moncada, I; Montorsi, F; Porst, H; Shabsigh, R; Yassin, A, 2011)		0.87
" The prolonged half-life of tadalafil lends itself well to this dosing regimen and conveys the advantage of separating medication from sexual interactions; lower dose therapy also carries the theoretical benefit of lower incidence of side effects."( A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy.
Shindel, AW; Washington, SL, 2010)		0.97
" Seventeen healthy male volunteers received sequential dosing of the studied product: TAD (day 1) alone in a single dose for 7 days followed by TAD (day 8) in a single dose with TPV/r (500/200 mg twice daily, days 8-18)."( Effect of tipranavir/ritonavir combination on the pharmacokinetics of tadalafil in healthy volunteers.
Dellamonica, P; Durant, J; Ferrando, S; Garraffo, R; Lavrut, T; MacGregor, TR; Rouyrre, N; Sabo, JP, 2011)		0.6
" The 405 patients enrolled in the single pivotal trial give this drug the largest initial placebo-controlled dataset of any of the oral PAH therapies; its once-daily dosing and excellent safety profile make it the most convenient of the therapies by a significant margin."( Novel therapeutic approaches in pulmonary arterial hypertension: focus on tadalafil.
Levin, YD; White, RJ, 2011)		0.6
" The longer half-life of tadalafil allows for once-daily dosing as compared with three-times daily dosing for sildenafil, the only other PDE-5 inhibitor currently approved for treatment of PAH."( Tadalafil for the treatment of pulmonary arterial hypertension.
Klinger, JR, 2011)		2.12
"To compare the efficacy and safety of on-demand 20-mg tadalafil (arm A) with the newly released tadalafil 5-mg once-a-day dosing (arm B) in patients with ED following radiotherapy for prostate cancer (PC)."( Efficacy and safety of tadalafil 20 mg on demand vs. tadalafil 5 mg once-a-day in the treatment of post-radiotherapy erectile dysfunction in prostate cancer men: a randomized phase II trial.
Badellino, S; Ciammella, P; Filippi, AR; Gontero, P; Guarneri, A; Moretto, F; Munoz, F; Ragona, R; Ricardi, U; Rondi, N; Tizzani, A; Valentino, F, 2010)		0.92
" The once-a-day 5-mg dosing showed higher compliance and marginally reduced side effects, thus making it an attractive alternative to on-demand therapy for ED in post-radiotherapy PC patients."( Efficacy and safety of tadalafil 20 mg on demand vs. tadalafil 5 mg once-a-day in the treatment of post-radiotherapy erectile dysfunction in prostate cancer men: a randomized phase II trial.
Badellino, S; Ciammella, P; Filippi, AR; Gontero, P; Guarneri, A; Moretto, F; Munoz, F; Ragona, R; Ricardi, U; Rondi, N; Tizzani, A; Valentino, F, 2010)		0.67
" Giving ED patients the opportunity to try all the three inhibitors can greatly improve the treatment compliance of the patient, whereas the majority of ED patients prefer one specific drug to the others, frequently tadalafil, irrespective of the severity and etiology of the disease, dosing sequence, age of the patient, or dose of medication."( [ED patients and their female partners prefer tadalafil].
Gong, BS, 2011)		0.81
"The purpose of this review is to evaluate the pharmacology, pharmacokinetic properties, clinical efficacy, adverse effects, drug interactions, and dosage and administration of tadalafil in patients with PAH."( Tadalafil: a long-acting phosphodiesterase-5 inhibitor for the treatment of pulmonary arterial hypertension.
Arif, SA; Poon, H, 2011)		2
"Tadalafil once-daily provides efficacy comparable to on-demand dosing regimens with PDE-5 inhibitors, is well tolerated and allows patients and their partners to disconnect the administration of medication from sexual activity, thereby enabling them to return to the sex-life they had before the onset of erectile dysfunction."( Chronic PDE-5 inhibition in patients with erectile dysfunction - a treatment approach using tadalafil once-daily.
Büttner, H; Hell-Momeni, K; Porst, H, 2012)		2.04
" There is level 5 evidence (expert opinion) that combination therapy of PDE5 inhibitors + L-arginine or daily dosing of tadalafil + short-acting PDE5 inhibitors pro re nata may rescue PDE5 inhibitor monotherapy failures."( SOP conservative (medical and mechanical) treatment of erectile dysfunction.
Brock, G; Burnett, A; Ghanem, H; Giuliano, F; Glina, S; Hellstrom, W; Martin-Morales, A; Porst, H; Salonia, A; Sharlip, I, 2013)		0.6
"To assess persistence/adherence rates of phosphodiesterase type-5 inhibitor (PDE5I) on-demand dosing in Latin American men with erectile dysfunction (ED), and explore patient characteristics and treatment factors that may be predictive for PDE5I persistence and adherence."( A 6 month, prospective, observational study of PDE5 inhibitor treatment persistence and adherence in Latin American men with erectile dysfunction.
Borregales, L; Cairoli, C; Reyes, LA; Rubio-Aurioles, E; Sorsaburu, S, 2013)		0.39
"Men from Brazil, Mexico, and Venezuela with ED who were naïve to PDE5Is were prescribed sildenafil, tadalafil, vardenafil, or lodenafil on-demand dosing and asked to provide information about PDE5I use at baseline and at 1, 3, and 6 months."( A 6 month, prospective, observational study of PDE5 inhibitor treatment persistence and adherence in Latin American men with erectile dysfunction.
Borregales, L; Cairoli, C; Reyes, LA; Rubio-Aurioles, E; Sorsaburu, S, 2013)		0.61
" Persistence was defined as use of ≥1 dose during the prior 4 weeks, adherence as compliance with dosing instructions during the most recent dose."( A 6-month, prospective, observational study of PDE5 inhibitor treatment persistence and adherence in Middle Eastern and North African men with erectile dysfunction.
Al-Mitwalli, K; El-Meliegy, A; Gurbuz, S; Hussein, T; Istarabadi, M; Lei, Y; Mostafa, T; Rabah, D, 2013)		0.39
" Both dosing schedules were well tolerated and no significant differences were observed in safety between the two groups."( [On-demand versus on-time dosing of tadalafil for erectile dysfunction: a prospective multi-center study].
Huang, YR; Jiang, ZX; Li, P; Li, Z; Liu, YF; Ma, M; Shen, ZJ; Tian, RH; Wang, GM; Wang, JL; Wang, YX; Wu, M; Yang, NQ; Zhong, S; Zhou, W, 2014)		0.68
"On-time dosing of tadalafil is efficacious and well tolerated in the treatment of ED, and has an even better effect than on-demand dosing at 8 weeks of medication and 1 month after withdrawal."( [On-demand versus on-time dosing of tadalafil for erectile dysfunction: a prospective multi-center study].
Huang, YR; Jiang, ZX; Li, P; Li, Z; Liu, YF; Ma, M; Shen, ZJ; Tian, RH; Wang, GM; Wang, JL; Wang, YX; Wu, M; Yang, NQ; Zhong, S; Zhou, W, 2014)		1.01
"This study investigated the effects of tadalafil dosing on RhoA/ROCK signaling in bladder, in a rabbit model of high-fat diet (HFD)-induced MetS."( Tadalafil effect on metabolic syndrome-associated bladder alterations: an experimental study in a rabbit model.
Carini, M; Cellai, I; Comeglio, P; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Sarchielli, E; Vannelli, GB; Vignozzi, L, 2014)		2.11
" Tadalafil dosing normalized HFD-induced bladder hypersensitivity to Y-27632, by reducing RhoA membrane translocation and ROCK overexpression."( Tadalafil effect on metabolic syndrome-associated bladder alterations: an experimental study in a rabbit model.
Carini, M; Cellai, I; Comeglio, P; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Sarchielli, E; Vannelli, GB; Vignozzi, L, 2014)		2.76
"Tadalafil dosing reduced RhoA/ROCK signaling and smooth muscle overactivity in an animal model of MetS-associated bladder alterations."( Tadalafil effect on metabolic syndrome-associated bladder alterations: an experimental study in a rabbit model.
Carini, M; Cellai, I; Comeglio, P; Filippi, S; Gacci, M; Maggi, M; Maneschi, E; Morelli, A; Sarchielli, E; Vannelli, GB; Vignozzi, L, 2014)		3.29
"A novel, precise, rapid and sensitive reverse phase high performance liquid chromatographic method has been developed for the validated estimation of Tadalafil in bulk and tablet dosage form."( Validation and method development of Tadalafil in bulk and tablet dosage form by RP-HPLC.
Bojanapu, A; Chennakesavalu, J; Dhanapal, K; Jayaprakash, V; Munusamy, J; Sellappan, M; Subramaniam, AT, 2015)		0.89
" Persistence was defined as using ≥ 1 dose during the previous 4 - weeks, and adherence as following dosing instructions for the most recent dose, assessed using the Persistence and Adherence Questionnaire."( PDE5 inhibitor treatment persistence and adherence in Brazilian men: post-hoc analyses from a 6-month, prospective, observational study.
Cairoli, C; Henneges, C; Reyes, LA; Sorsaburu, S, )		0.13
" Together, these results uncover a hitherto uncharacterized role of PDE5/cGMP/PKG signaling in bone homeostasis and provide the evidence that long-term treatment with PDE5 inhibitors at a high dosage may potentially cause bone catabolism."( Inhibition of phosphodiesterase 5 reduces bone mass by suppression of canonical Wnt signaling.
Chen, HX; Gong, Y; Hong, D; Hu, XH; Ji, X; Shi, W; Wang, HB; Wang, JR; Wu, XM; Xu, CY, 2014)		0.4
" Sildenafil (SIL) and vardenafil (VAR) are approved for as-needed (PRN) dosing; tadalafil (TAD) is approved for both PRN and once-a-day (OaD) dosing for ED."( Comparative efficacy of tadalafil once daily in men with erectile dysfunction who demonstrated previous partial responses to as-needed sildenafil, tadalafil, or vardenafil.
Baygani, S; Burns, P; Goldfischer, E; Kim, E; Seftel, A, 2015)		0.95
" The aim of this study was to compare the efficacies of two dosing regimens of 20 mg tadalafil (on-demand and 3 times per week) and to assess the role of tadalafil in recovery of erectile function and continence after BNSRP."( Effects of three-times-per-week versus on-demand tadalafil treatment on erectile function and continence recovery following bilateral nerve sparing radical prostatectomy: results of a prospective, randomized, and single-center study.
Atış, G; Canat, L; Çaşkurlu, T; Güner, B; Gürbüz, C, 2015)		0.9
" More recently, tadalafil has been introduced allowing once daily dosing with apparently similar efficacy to sildenafil in children."( Risk-benefit considerations when prescribing phosphodiesterase-5 inhibitors in children.
Bentley, S; Magee, AG; Makhecha, S, 2015)		0.76
"025); scores were not significantly different between treatments for satisfaction with dosing or side-effects (both P ≥ 0."( Treatment satisfaction and clinically meaningful symptom improvement in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia: Secondary results from a 6-month, randomized, double-blind study comparing f
Casabé, A; Glina, S; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L, 2015)		0.42
"These results suggest that chronic dosing of tadalafil improves QoL of patients post-nsRP."( Effects of tadalafil treatment after bilateral nerve-sparing radical prostatectomy: quality of life, psychosocial outcomes, and treatment satisfaction results from a randomized, placebo-controlled phase IV study.
Andrianne, R; Barry, J; Branicka, J; Büttner, H; Chadwick, D; Cuzin, B; Hell-Momeni, K; Henneges, C; Ilo, D; Patel, HR; Shah, N, 2015)		1.07
"A valid, sensitive and rapid spectrofluorimetric method has been developed and validated for determination of both tadalafil (TAD) and vardenafil (VAR) either in their pure form, in their tablet dosage forms or spiked in human plasma."( Validated spectrofluorimetric method for determination of two phosphodiesterase inhibitors tadalafil and vardenafil in pharmaceutical preparations and spiked human plasma.
Abu El-Enin, MA; Al-Ghaffar Hammouda, Mel-S; El-Ashry, SM; El-Sherbiny, DT; El-Wasseef, DR, 2016)		0.86
" Therefore, a novel, accurate, specific and sensitive reversed-phase high performance liquid chromatographic method with fluorescence detection was developed and validated for their separation and quantitation in dosage form and human plasma using avanafil as an internal standard (IS)."( A novel liquid chromatographic method with fluorescence detection for quantitation of tadalafil and dapoxetine hydrochloride in pharmaceutical dosage form and human plasma.
Ahmed Emad, el G; Amira, K; Maha, H; Mohamed, A, 2015)		0.64
"Oral dosing with bosentan and tadalafil in children may not achieve therapeutic blood concentration."( Pharmacokinetics of drugs for pediatric pulmonary hypertension.
Azuma, H; Kajihama, A; Kajino, H; Kamiyama, N; Maeda, J; Nakau, K; Oka, H; Sugimoto, M; Tasaki, Y; Yamagishi, H, 2016)		0.72
"To provide a descriptive comparison of erectile function response for tadalafil on-demand (PRN) and once-daily (OAD) dosing regimens in patients with common comorbid conditions, treatments, or risk factors that can be considered when treating ED."( Efficacy of Continuous Dosing of Tadalafil Once Daily vs Tadalafil On Demand in Clinical Subgroups of Men With Erectile Dysfunction: A Descriptive Comparison Using the Integrated Tadalafil Databases.
Barry, J; Brock, G; D'Souza, D; Mulhall, J; Ni, X; Oelke, M; Rosenberg, M; Seftel, A, 2016)		0.95
"Pharmacological advances in erectile dysfunction (ED) treatment have aroused growing interest among health professionals towards sexual dysfunction, generating an increasing demand for dosage forms and drug delivery systems, including tadalafil."( Technological Device for Manufacturing Transdermal Films: Possible Applications to the Individualized Treatment for Erectile Dysfunction.
Brandão, MAF; Ferreira, A; Polonini, HC; Raposo, FJ; Raposo, NRB, 2017)		0.64
"PAH patients receiving a stable combination treatment with ERA and PDE-5i with targeted dosage for at least 1 month were routinely assessed, including clinical parameters and plasma drug concentrations."( Plasma Drug Concentrations in Patients with Pulmonary Arterial Hypertension on Combination Treatment.
Benjamin, N; Burhenne, J; Egenlauf, B; Enderle, Y; Fischer, C; Grünig, E; Haefeli, WE; Harutyunova, S; Huppertz, A; Klose, H; Ohnesorge, J, 2017)		0.46
"To compare the efficacy and safety between tadalafil once-a-day and tadalafil on-demand dosing regimen in patients with ED."( Efficacy and Safety of Tadalafil Once-a-Day versus Tadalafil On-Demand in Patients with Erectile Dysfunction: A Systematic Review and Meta-Analyses.
Dong, Q; Liu, L; Peng, Z; Wei, Q; Yang, B; Yang, L, 2017)		1.03
"A systematic search of Medline, Embase, and Cochrane Library was performed to identify all randomized controlled trials (RCTs) that compared tadalafil used a once-a-day with an on-demand dosing regimen for erectile dysfunction."( Efficacy and Safety of Tadalafil Once-a-Day versus Tadalafil On-Demand in Patients with Erectile Dysfunction: A Systematic Review and Meta-Analyses.
Dong, Q; Liu, L; Peng, Z; Wei, Q; Yang, B; Yang, L, 2017)		0.97
" Meta-analyses of Sexual Encounter Profile questions 2 and 3 (SEP-2 and SEP-3) showed that the once-a-day dosing regimen was superior to the on-demand regimen with statistical significance."( Efficacy and Safety of Tadalafil Once-a-Day versus Tadalafil On-Demand in Patients with Erectile Dysfunction: A Systematic Review and Meta-Analyses.
Dong, Q; Liu, L; Peng, Z; Wei, Q; Yang, B; Yang, L, 2017)		0.77
" The 40-mg/day dosage was tried in six cases as the dosage was considered to be high."( Safety and dose-finding trial of tadalafil administered for fetal growth restriction: A phase-1 clinical study.
Ikeda, T; Kamimoto, Y; Kondo, E; Kubo, M; Maki, S; Murabayashi, N; Nii, M; Osato, K; Tanaka, H; Umekawa, T, 2017)		0.74
" Eight studies that examined the desired dosing regimens were identified."( The Efficacy of Tadalafil Daily vs on Demand in the Treatment of Erectile Dysfunction: A Systematic Review and Meta-analysis.
Bansal, UK; Fuller, TW; Jackman, SV; Jones, C; Wessel, C, 2018)		0.83
"Sildenafil and tadalafil are widely-used phosphodiesterase 5 (PDE5) inhibitors for which no clear dose-response relationship could be established."( Cyclic guanosine monophosphate modulates accumulation of phosphodiesterase 5 inhibitors in human platelets.
Bajraktari, G; Bugert, P; Burhenne, J; Haefeli, WE; Weiss, J, 2017)		0.81
" Because various PDE5Is vary in their duration of action and dosage regimen, this may be an important consideration in selecting the optimal agent for the ED patient."( Sexual habits of men with ED who take phosphodiesterase 5 inhibitors: a survey conducted in 7 countries.
Hassan, TA; Mulhall, JP; Rienow, J, 2018)		0.48
" The time to sexual intercourse after dosing was ≤1 hour for 70% and ≤4 hours for 96% of men."( Sexual habits of men with ED who take phosphodiesterase 5 inhibitors: a survey conducted in 7 countries.
Hassan, TA; Mulhall, JP; Rienow, J, 2018)		0.48
" The two models were applied on the dosage forms and statistically compared with the published HPLC method with no significant difference regarding accuracy and precision."( Linear Support Vector Regression and Partial Least-Squares for Determination of Dapoxetine Hydrochloride and Tadalafil in Binary Pharmaceutical Mixtures.
Abdelhamid, NS; Anwar, BH; Magdy, MA; Naguib, IA, 2020)		0.77
" Furthermore, the methods were successfully applied for the quantification of the two drugs in their combined dosage form."( Smart spectrophotometric assessment of tamsulosin hydrochloride and tadalafil in their new pharmaceutical formulation for treatment of benign prostatic hyperplasia and erectile dysfunction.
Rezk, MR; Tantawy, MA; Wadie, M; Weshahy, SA, 2020)		0.79
" The presented study is using previously analyzed pharmaceutical mixtures of Dapoxetine Hydrochloride (DAP) and Tadalafil (TAD) as a case study, whether in pure forms or in dosage form, where the study uses two datasets for analysis, the first aims to include COA and the second dataset avoids it, then a statistical comparison is conducted for training sets, test sets and dosage form datasets to see how far COA may interfere with analysis results."( Ultraviolet cutoff area and predictive ability of partial least squares regression method: A pharmaceutical case study.
Abdallah, FF; Naguib, IA, 2020)		0.77
"A rapid, smart and sensitive first derivative spectrofluorimetric method has been carried out for the simultaneous estimation of avanafil and tadalafil either in their pure form, tablet dosage form or spiked human plasma."( D-optimal design as a useful tool response surface methodology for the optimization of signals from synchronous fluorescence prior to simultaneous determination of avanafil and tadalafil.
Abdel-Raoof, AM; Abdelzaher, AM; El-Desouky, EA; Emara, MS; Hasan, MA; Osman, AE; Said, RAM, 2020)		0.95
" A sensitive, efficient and rapid assay was selected satisfactorily and applied for simultaneous determination of citalopram and tadalafil either in their pure forms, in tablet dosage forms or in spiked human plasma."( Simultaneous determination of citalopram and tadalafil by the second derivative synchronous fluorescence method in biological fluids; application of Box-Behnken optimization design.
Abdel-Fattah, A; Abdel-Raoof, AM; Eissa, MS; Hasan, MA; Madkour, AW, 2021)		1.09
" PK data from the studies were pooled to develop a pediatric population PK model for tadalafil that characterized relationships among dose, exposure, and the effects of covariates with an aim to develop a population PK model that could simulate concentration-time profiles and assess exposure-matched dosing strategies in a pediatric PAH population."( Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Ferguson-Sells, L; Li, B; Small, D; Velez de Mendizabal, N, 2022)		1.23
" The model demonstrated that plasma tadalafil concentrations in pediatric patients aged 2 to < 18 years were similar to those in adults at similar doses, and confirmed that dosing of 40 mg once daily in pediatric patients with a bodyweight ≥ 40 kg, and a dose of 20 mg once daily in patients with a body weight < 40 kg and aged ≥ 2 years are suitable for phase III evaluation."( Population Pharmacokinetics of Tadalafil in Pediatric Patients with Pulmonary Arterial Hypertension: A Combined Adult/Pediatric Model.
Ferguson-Sells, L; Li, B; Small, D; Velez de Mendizabal, N, 2022)		1.28
" This study is the first to develop and optimize a synchronous spectrofluorimetric method coupled with derivative and derivative ratio mathematical tools for the determination of tamsulosin andtadalafil in their newly released dosage form."( Assay of new combination of tamsulosin and tadalafil using synchronous spectrofluorimetric method coupled with mathematical tools.
Abdelhafez, AM; Gawad, DA; Hassan, EM; M Youssef, R, 2022)		1.17
" To detect treatment effects may require different dosing regimens."( The PASTIS trial: Testing tadalafil for possible use in vascular cognitive impairment.
Barrick, TR; Benjamin, P; Betteridge, S; Binnie, LR; Clarke, B; Dhillon, MK; Ghatala, R; Hainsworth, AH; Hainsworth, FAH; Howe, FA; Isaacs, JD; Khan, U; Kruuse, C; Madigan, JB; Moynihan, B; Patel, B; Pauls, MMH; Pereira, AC; Rostrup, E; Shtaya, ABY; Spilling, CA; Trippier, S; Williams, R; Young, R, 2022)		1.02
"In this study, the drug kinetics of tadalafil were compared between pregnant and non-pregnant women to determine the ideal dosage to promote uterine blood flow."( Maternal blood concentration of tadalafil in pregnancy: Comparison of pregnant and non-pregnant women.
Enomoto, N; Ikeda, T; Katsuragi, S; Maki, S; Takakura, S; Tanaka, H; Tanaka, K, 2022)		1.28
" The article also discusses the methods for preparation of lodenafil, its physical-chemical properties, analytical methods for its determination, pharmacological-toxicological properties, and dosing information."( Lodenafil.
Al-Majed, AA; Alshehri, YM; Attwa, MW; Bakheit, AH, 2022)		0.72
" That approach was utilized to estimation of the cited drugs in dosage forms, simultaneously with %recoveries for tadalafil and finasteride of 99."( Synchronous fluorescence as a green and selective method for the simultaneous determination of finasteride and tadalafil in dosage form and spiked human plasma.
Abdelaziz, A; Batekh, AE; Emad, N; Galal, M; Hussien, M; Karem, M; Moukhtar, DA; Salem, H, 2023)		1.33
" Between May 2020 and December 2022, we retrospectively analyzed the records of 126 ED patients who underwent Li-ESWT post unsuccessful PDE5is trials, defined as inadequate response following at least 6 consistent trials with correct dosage (preference given to 20 mg tadalafil)."( Non-invasive alternative for phosphodiesterase inhibitor-refractory erectile dysfunction: Real-life experience with low-intensity extracorporeal shockwave therapy.
Bayraktar, N, 2023)		1.09
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitorAn EC 3.1.4.* (phosphoric diester hydrolase) inhibitor that blocks the action of 3',5'-cyclic-GMP phosphodiesterase (EC 3.1.4.35).
vasodilator agentA drug used to cause dilation of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
pyrazinopyridoindole
benzodioxoles
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (83)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency39.81070.044717.8581100.0000AID485341
acetylcholinesteraseHomo sapiens (human)Potency20.67160.002541.796015,848.9004AID1347395; AID1347398
USP1 protein, partialHomo sapiens (human)Potency89.12510.031637.5844354.8130AID743255
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency16.57470.001022.650876.6163AID1224838; AID1224893
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68250.01237.983543.2770AID1346984; AID1645841
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency26.60320.003041.611522,387.1992AID1159553
pregnane X nuclear receptorHomo sapiens (human)Potency7.94330.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency22.42090.000229.305416,493.5996AID743080; AID743091
GVesicular stomatitis virusPotency19.49710.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency24.54540.00108.379861.1304AID1645840
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.79430.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency26.60320.000723.06741,258.9301AID743085
importin subunit beta-1 isoform 1Homo sapiens (human)Potency20.59625.804836.130665.1308AID540253
mitogen-activated protein kinase 1Homo sapiens (human)Potency3.98110.039816.784239.8107AID1454
snurportin-1Homo sapiens (human)Potency20.59625.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency20.59625.804816.996225.9290AID540253
Interferon betaHomo sapiens (human)Potency19.49710.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency1.41250.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency19.49710.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain B, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)0.00120.00001.947220.0000AID977608
Phosphodiesterase Bos taurus (cattle)IC50 (µMol)10.00000.10005.88009.9000AID159197
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)64.45070.00001.77679.2000AID1421855; AID159061; AID1598436; AID1797296; AID240958; AID735486
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)IC50 (µMol)2.92800.00051.13535.2000AID158129; AID1872578; AID240763; AID240962; AID735483
cGMP-specific 3',5'-cyclic phosphodiesteraseRattus norvegicus (Norway rat)Ki0.00500.00180.00390.0050AID239083
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)IC50 (µMol)72.22940.00001.85239.2000AID1421862; AID1598441; AID1797296; AID735481
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)37.74140.00001.18439.6140AID1321699; AID1380124; AID1380338; AID1384205; AID1421852; AID1555534; AID157949; AID157951; AID1598427; AID1659411; AID1797296; AID240961; AID366091; AID477863; AID566802; AID735487
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki0.00760.00071.07978.5000AID1421850; AID238296
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)IC50 (µMol)10.00000.00801.16175.6000AID1421863; AID1598442; AID240504; AID735479
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)IC50 (µMol)5.10000.01980.75935.1000AID158123
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaBos taurus (cattle)IC50 (µMol)4.05000.01980.93945.1000AID158123; AID454866
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50 (µMol)10.00000.40002.23759.9000AID158753
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC50 (µMol)204.83900.12004.048010.0000AID1207388; AID1207415
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)IC50 (µMol)2.92800.00051.22825.2000AID158129; AID1872578; AID240763; AID240962; AID735483
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Bos taurus (cattle)IC50 (µMol)5.10000.01980.66855.1000AID158123
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)IC50 (µMol)2.92800.00051.22825.2000AID158129; AID1872578; AID240763; AID240962; AID735483
Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)IC50 (µMol)5.10000.01980.75935.1000AID158123
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)IC50 (µMol)5.10000.01980.75935.1000AID158123
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)9.84000.00001.068010.0000AID1421857; AID159782; AID1598438; AID240960; AID735484
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)IC50 (µMol)2.92800.00051.22825.2000AID158129; AID1872578; AID240763; AID240962; AID735483
AcetylcholinesteraseRattus norvegicus (Norway rat)IC50 (µMol)26.15900.00020.52597.2000AID1555532
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)IC50 (µMol)3.57740.00050.90595.2000AID1421858; AID158129; AID1598439; AID1872578; AID240763; AID240962; AID735483
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC50 (µMol)204.83900.12004.048010.0000AID1207388; AID1207415
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC50 (µMol)10.00000.23002.510510.0000AID1421854; AID1598435; AID240957; AID735477
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)IC50 (µMol)10.00000.40002.23759.9000AID158753
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50 (µMol)72.22940.00002.14179.2000AID1598435; AID1797296; AID240957; AID735477
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.01200.00100.01460.1000AID410413
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)66.90070.00001.104010.0000AID159782; AID1598438; AID1797296; AID240960; AID566805; AID735484
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)9.80000.00001.465110.0000AID159782; AID1598438; AID240960; AID735484
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)68.02740.00001.146310.0000AID159782; AID1598438; AID1797296; AID240960; AID735484
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)101.33140.00091.901410.0000AID1207482; AID1207509; AID1207542; AID392051
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)IC50 (µMol)65.95360.00002.072410.0000AID1421856; AID1598437; AID1797296; AID240959; AID566803; AID566804; AID735485
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)398.10700.00032.25459.6000AID1207295
High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)IC50 (µMol)10.00000.09001.63104.6900AID1421861; AID1598440; AID240963; AID735482
Retinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)IC50 (µMol)2.92800.00051.22825.2000AID158129; AID1872578; AID240763; AID240962; AID735483
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC50 (µMol)10.00000.23001.98149.0000AID1598435; AID240957; AID735477
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)IC50 (µMol)10.00000.00031.990110.0000AID1598437; AID240959; AID735485
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)142.19100.00033.64849.2000AID1207328; AID1207355
cGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)IC50 (µMol)0.00750.00331.624010.0000AID157928; AID305334; AID410413; AID454868; AID659075
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)IC50 (µMol)5.10000.01980.75935.1000AID158123
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)IC50 (µMol)49.63290.00001.97009.2000AID1421860; AID159035; AID1598444; AID1797296; AID240764; AID241009; AID410415; AID454867; AID566806; AID566807; AID735478
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)IC50 (µMol)72.22940.00002.05139.2000AID1598440; AID1797296; AID240963; AID735482
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)IC50 (µMol)68.08070.00001.49049.2000AID1421864; AID1598443; AID1797296; AID241008; AID735480
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-specific 3',5'-cyclic phosphodiesteraseRattus norvegicus (Norway rat)EC50 (µMol)0.07800.07803.69279.0000AID1421871
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)EC50 (µMol)5.81001.00003.40505.8100AID1750322
Nuclear receptor subfamily 2 group E member 1Homo sapiens (human)EC50 (µMol)5.00005.00005.00005.0000AID1810681
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (340)

Processvia Protein(s)Taxonomy
negative regulation of cell adhesionPhosphodiesterase Bos taurus (cattle)
negative regulation of angiogenesisPhosphodiesterase Bos taurus (cattle)
negative regulation of lipid catabolic processPhosphodiesterase Bos taurus (cattle)
heart valve developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
ventricular septum developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
aorta developmentcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of inflammatory responsecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
establishment of endothelial barriercGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to mechanical stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cAMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to cGMPcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cellular response to 2,3,7,8-tetrachlorodibenzodioxinecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of gene expressioncGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cGMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of mitochondrion organizationcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
visual perceptionRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
regulation of DNA-templated transcriptionHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cellular response to epidermal growth factor stimulusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
signal transductionHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP metabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cGMP catabolic processHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
positive regulation of long-term synaptic potentiationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
negative regulation of neural precursor cell proliferationHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
behavioral fear responseHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
visual learningHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
operant conditioningHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
neuromuscular process controlling balanceHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
negative regulation of steroid hormone biosynthetic processHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
visual perceptionRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
visual perceptionRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaBos taurus (cattle)
cholesterol biosynthetic processCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
vesicle docking involved in exocytosisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
bicarbonate transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cholesterol transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
response to endoplasmic reticulum stressCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
transepithelial water transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of exocytosisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
sperm capacitationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
multicellular organismal-level water homeostasisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
intracellular pH elevationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
establishment of localization in cellCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
transmembrane transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
membrane hyperpolarizationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of enamel mineralizationCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cellular response to cAMPCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
amelogenesisCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of cyclic nucleotide-gated ion channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride transmembrane transportCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
positive regulation of voltage-gated chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cellular response to forskolinCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
epithelial cell maturationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
male gonad developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
vestibular nucleus developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
secretory granule organizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to acidic pHPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to light stimulusPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell action potential involved in contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of protein targeting to membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
visual perceptionRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
retina development in camera-type eyeRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
cAMP-mediated signalingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
visual perceptionRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of MAPK cascadeRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
visual perceptionRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
visual perceptionRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)
entrainment of circadian clock by photoperiodRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
sensory perception of smellcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of protein kinase A signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
visual perceptionRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
phototransduction, visible lightRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
entrainment of circadian clock by photoperiodRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
retinal cell apoptotic processRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
retina development in camera-type eyeRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
cAMP-mediated signalingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
phototransduction, visible lightCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
retinal cone cell developmentCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
cAMP-mediated signalingCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
visual perceptionCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
gastrin-induced gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
glucose metabolic processPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
heart developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
rhythmic behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of blood pressurePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of heart ratePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
iodide transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
erythrocyte differentiationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intracellular chloride ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
response to insulinPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
social behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
corticosterone secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear morphogenesisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intestinal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
auditory receptor cell developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
stomach developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal sodium ion absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to epinephrine stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
adrenergic receptor signaling pathwayPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cochlea developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
non-motile cilium assemblyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of smooth muscle cell apoptotic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cGMP catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
regulation of smooth muscle cell proliferationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
response to amphetamineCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
locomotory behaviorCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
visual learningCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
monocyte differentiationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
dopamine catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
serotonin metabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
neutrophil homeostasiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
neutrophil chemotaxiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
leukocyte migrationcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to lipopolysaccharidecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-5 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of heart contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
establishment of endothelial barriercAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesioncGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of angiogenesiscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cellular response to insulin stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of cell adhesion mediated by integrincGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of lipid catabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cAMP catabolic processHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
cAMP-mediated signalingHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
visual perceptionRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of MAPK cascadeRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
oocyte maturationcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
lipid metabolic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
response to xenobiotic stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of meiotic nuclear divisioncGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of apoptotic processcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of vascular permeabilitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
steroid hormone mediated signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of cAMP-mediated signalingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
positive regulation of oocyte developmentcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of ribonuclease activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to cGMPcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cellular response to transforming growth factor beta stimuluscGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
apoptotic signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
visual perceptionRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
signal transductionDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
negative regulation of cGMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
negative regulation of cAMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cAMP-mediated signalingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
chemical synaptic transmissioncAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cAMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP catabolic processcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
negative regulation of cGMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP-mediated signalingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
behavioral fear responseNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of neuroblast proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
aggressive behaviorNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
apoptotic processNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nervous system developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
neuroblast proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
visual perceptionNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
dentate gyrus developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
amygdala developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
olfactory bulb developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
layer formation in cerebral cortexNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
forebrain generation of neuronsNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cerebral cortex neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
anterior commissure morphogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
extracellular matrix organizationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
somatic stem cell population maintenanceNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
social behaviorNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of apoptotic processNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
steroid hormone mediated signaling pathwayNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
astrocyte cell migrationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cell fate commitmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of cell cycleNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group E member 1Homo sapiens (human)
astrocyte differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of astrocyte differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of dendrite morphogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
retina development in camera-type eyeNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of timing of neuron differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
long-term synaptic potentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
regulation of cell migration involved in sprouting angiogenesisNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of neural precursor cell proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
positive regulation of stem cell proliferationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
anatomical structure developmentNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group E member 1Homo sapiens (human)
cell differentiationNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (127)

Processvia Protein(s)Taxonomy
metal ion bindingPhosphodiesterase Bos taurus (cattle)
magnesium ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
zinc ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
TPR domain bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
phosphate ion bindingcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein homodimerization activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
GTPase inhibitor activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
protein bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
small GTPase bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
kinase bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
protein kinase activator activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
protein bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
metal ion bindingHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
zinc ion bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
cGMP bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
molecular adaptor activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
metal ion bindingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaBos taurus (cattle)
chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
intracellularly ATP-gated chloride channel activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATP bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
bicarbonate transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
isomerase activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATP hydrolysis activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel regulator activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel inhibitor activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
enzyme bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
PDZ domain bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein-folding chaperone bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
Sec61 translocon complex bindingCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ABC-type transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
ATPase-coupled transmembrane transporter activityCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium channel regulator activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
telethonin bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein-containing complex bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
metal ion bindingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
cGMP bindingCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Bos taurus (cattle)
metal ion bindingCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Bos taurus (cattle)
enzyme inhibitor activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
protein bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
spectrin bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
cGMP bindingRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
cGMP bindingRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
metal ion bindingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
cGMP bindingCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
metal ion bindingCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
calmodulin bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein phosphatase 1 bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
outward rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A catalytic subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A regulatory subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in atrial cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
enzyme bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
signaling receptor regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
beta-2 adrenergic receptor bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
ATPase bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
scaffold protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
heterocyclic compound bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
protein kinase B bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
metal ion bindingHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
enzyme inhibitor activityRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
protein bindingRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
cGMP bindingRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cGMP-inhibited cyclic-nucleotide phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
protein bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
nuclear estrogen receptor activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
metal ion bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
estrogen bindingcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseBos taurus (cattle)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
GTPase inhibitor activityRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cGMP bindingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
metal ion bindingDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP-stimulated cyclic-nucleotide phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cAMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
cGMP bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
metal ion bindingcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nuclear steroid receptor activityNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
protein bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
histone deacetylase bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (89)

Processvia Protein(s)Taxonomy
membranePhosphodiesterase Bos taurus (cattle)
guanyl-nucleotide exchange factor complexPhosphodiesterase Bos taurus (cattle)
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
endoplasmic reticulumcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
Golgi apparatuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
plasma membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
presynaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleuscGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial inner membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
perinuclear region of cytoplasmcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial outer membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
synaptic membranecGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
mitochondrial matrixcGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
cytosolRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cytoskeletonRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
ciliumRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cytoplasmic vesicle membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cytoplasmic vesicleRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cytoplasmRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
extracellular exosomeHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
nucleusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
nucleoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
endoplasmic reticulumHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
Golgi apparatusHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cytosolHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
plasma membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
ruffle membraneHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
sarcolemmaHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perikaryonHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AHomo sapiens (human)
cellular_componentHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
nucleusHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
cytosolHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8BHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
photoreceptor disc membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
photoreceptor outer segment membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaBos taurus (cattle)
photoreceptor disc membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaBos taurus (cattle)
photoreceptor outer segment membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaBos taurus (cattle)
nucleusCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytoplasmCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
lysosomal membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
early endosomeCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
endoplasmic reticulum membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytosolCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cell surfaceCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
apical plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
Golgi-associated vesicle membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
early endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
recycling endosomeCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
recycling endosome membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
protein-containing complexCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
chloride channel complexCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
cytosolCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
apical plasma membraneCystic fibrosis transmembrane conductance regulatorHomo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
Z discPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
plasma membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
photoreceptor disc membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
photoreceptor outer segment membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alphaHomo sapiens (human)
plasma membraneCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Bos taurus (cattle)
plasma membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
photoreceptor disc membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
photoreceptor outer segment membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
photoreceptor disc membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)
photoreceptor outer segment membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaBos taurus (cattle)
nucleoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
ruffle membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
photoreceptor disc membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
photoreceptor outer segment membraneRod cGMP-specific 3',5'-cyclic phosphodiesterase subunit betaHomo sapiens (human)
plasma membraneCone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
late endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transport vesiclePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmic vesicle membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuron projectionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuronal cell bodyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ciliary basePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lumenal side of membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral part of cellPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
monoatomic ion channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
synaptic vesiclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
postsynaptic densitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
Z disccAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
dendritic spinecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
excitatory synapsecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
extracellular spacecAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
ciliumcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
apical plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
endoplasmic reticulumcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
Golgi apparatuscGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
guanyl-nucleotide exchange factor complexcGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cytosolHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
perinuclear region of cytoplasmHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
nucleusHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
cytosolHigh affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7AHomo sapiens (human)
photoreceptor outer segment membraneRetinal cone rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit gammaHomo sapiens (human)
lysosomeCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
membranecGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
cytosolcGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cytosolRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
cytoskeletonRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
cytoplasmic vesicle membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
cytoplasmic vesicleRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
photoreceptor outer segment membraneRetinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit deltaBos taurus (cattle)
cellular_componentDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cytosolDual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
synapsecAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)
cytosolcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)
nucleoplasmNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
chromatinNuclear receptor subfamily 2 group E member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (260)

Assay IDTitleYearJournalArticle
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1384235Effective permeability of the compound at 50 uM after 18 hrs by UV spectroscopy based PAMPA2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1598435Inhibition of N-terminal GST-tagged human PDE1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1555534Inhibition of PDE5A1 (unknown origin) by immobilized metal ion affinity-based fluorescence polarization2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID1421865Selectivity index, ratio of IC50 for inhibition of full length recombinant human N-terminal GST-tagged PDE11A4 expressed in baculovirus infected sf9 cells to IC50 for inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in ba2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1384224Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1207448Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform
AID735472Selectivity ratio of IC50 for PDE6 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID735475Selectivity ratio of IC50 for PDE1 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID503318Antiproliferative activity against human PC3 cells at 1 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID735471Selectivity ratio of IC50 for PDE8 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID239083Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID29943Volume of distribution of compound was determined in rats2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1421864Inhibition of recombinant human N-terminal GST-tagged PDE10A1 (2 to 789 residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID1810681Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
AID410413Inhibition of bovine PDE52008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
AID454867Inhibition of human recombinant PDE112010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
AID1321729Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 after 2 hrs by Western blot analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1321733Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 100 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1321734Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1386237Selectivity ratio of IC50 for PDE11A catalytic domain (588 to 911 residues) (unknown origin) to IC50 for human PDE5A1 catalytic domain (535 to 860 residues)2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
AID305335Aqueous solubility in PBS at pH 7.42007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
AID158123Inhibition of bovine retina PDE6 (Phosphodiesterase 6)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1872578Inhibition of PDE6 (unknown origin)2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1872577Inhibition of PDE5 (unknown origin)2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID735483Inhibition of PDE6 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID454866Inhibition of bovine retina PDE62010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
AID477861Growth inhibition of human HT-29 cells after 72 hrs by cell titer glo assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
AID1207482Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform
AID1421860Inhibition of full length recombinant human N-terminal GST-tagged PDE11A4 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID240959Inhibition of human phosphodiesterase 32005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID158753Inhibition of bovine aorta PDE1 (Phosphodiesterase 1)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID735478Inhibition of PDE11 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID229980Relative inhibition of bovine aorta PDE5 and bovine retina PDE62003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID244234Ratio of inhibitory constant against phosphodiesterase 2 and phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID240958Inhibition of human phosphodiesterase 22005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1598437Inhibition of N-terminal GST-tagged human PDE3 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1380124Inhibition of PDE5A (unknown origin)2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.
AID1384225Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1421855Inhibition of recombinant human N-terminal FLAG-tagged PDE2A (2 to 941 residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID655406Inhibition of Trypanosoma brucei PDEB1 using cAMP as substrate at 100 uM preincubated for 10 mins prior substrate addition by spectrophotometry2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. Part 2. Tadalafil analogs.
AID1810682Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as remaining activity measured after 14 hrs by luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12
Propranolol Activates the Orphan Nuclear Receptor TLX to Counteract Proliferation and Migration of Glioblastoma Cells.
AID1872580Drug concentration in C57B6 mouse brain at 15 mg/kg, po via gavage measured after 90 mins by HPLC-MS analysis2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID566808Selectivity ratio of IC50 for human recombinant PDE11A-mediated hydrolysis of cGMP to IC50 for human recombinant PDE5A-mediated hydrolysis of cGMP2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID477863Inhibition of human recombinant PDE5 after 1.5 hrs by fluorescent polarization assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
AID1872579Permeability of compound in BBB assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.
AID1659411Inhibition of PDE5A (unknown origin)2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.
AID1421856Inhibition of recombinant human N-terminal GST-tagged PDE3B (592 to end residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID175661Effective concentration against rat aortic smooth muscle cell2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID566802Inhibition of human recombinant PDE5A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1555532Inhibition of AChE from rat cortex by Ellman's method2019European journal of medicinal chemistry, Aug-15, Volume: 176Multi-target design strategies for the improved treatment of Alzheimer's disease.
AID240763Inhibition of human phosphodiesterase 62005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
AID1222793Dissociation constant, pKa of the compound2013Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 41, Issue:5
Which metabolites circulate?
AID1598441Inhibition of N-terminal GST-tagged full length human PDE8A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1598427Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID240963Inhibition of human phosphodiesterase 72005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1321738Inhibition of PDE5A in human SH-SY5Y cells assessed as increase in CREB phosphorylation at Ser133 residue at 500 nM after 30 mins by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1750322Inhibition of PDE5A in HEK293 cells stably transfected with cGMP biosensor assessed as increase in SNP-induced intracellular cGMP level measured after 90 mins by luminescence assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID735473Selectivity ratio of IC50 for PDE4 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1321731Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1598489Volume of distribution at steady state in iv dosed rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID29807Oral bioavailability in rat was determined2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1384227Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 100 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1173629Selectivity for PDE5 (unknown origin) over PDE6 (unknown origin)2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.
AID566806Inhibition of human recombinant PDE11A-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID1598444Inhibition of N-terminal GST-tagged human PDE11A4 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1598488Clearance in iv dosed rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID237680Half-life was observed2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
AID1598438Inhibition of N-terminal GST-tagged human PDE4 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1598443Inhibition of N-terminal GST-tagged human PDE10A expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID735482Inhibition of PDE7 (unknown origin) using FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID238296Inhibition of human phosphodiesterase 52005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
AID477860Growth inhibition of human HT-29 cells at 100 uM after 72 hrs by cell titer glo assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
AID735470Selectivity ratio of IC50 for PDE7 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID477862Inhibition of human recombinant PDE5 at 100 uM after 1.5 hrs by fluorescent polarization assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
AID240504Inhibition of Phosphodiesterase 92005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID240764Inhibitory concentration against phosphodiesterase-112005Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
AID1321730Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 100 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID454872Inhibition of erectile dysfunction in New Zealand white rabbit assessed as induction of SNP-potentiated penile erection at 3 mg/kg, po after 2 hrs2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
AID1207328Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID1384230Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1598490Oral bioavailability in rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID159197Inhibition of bovine aorta PDE3 (Phosphodiesterase 3)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID566803Inhibition of human recombinant PDE3B-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID159061Inhibition of Human recombinant PDE2 (Phosphodiesterase 2)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID241009Inhibition of human phosphodiesterase 112005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID735480Inhibition of PDE10 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1421862Inhibition of full length recombinant human N-terminal GST-tagged PDE8A1 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID566805Inhibition of human recombinant PDE4B-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID240964Inhibitory concentration against human phosphodiesterase 8 activity2005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1598451Selectivity ratio of IC50 for N-terminal GST-tagged human PDE9A2 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1321735Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in alpha-tubulin acetylation at Lys 40 residue at 1000 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID411793Metabolic stability in human liver microsomes assessed as intrinsic clearance per mg of protein2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Metabolic soft spot identification and compound optimization in early discovery phases using MetaSite and LC-MS/MS validation.
AID229356Relative inhibition of PDE2 from rat kidney and PDE5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID659075Inhibition of bovine PDE5 after 24 hrs by time-resolved fluorescence resonance energy transfer assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.
AID1421857Inhibition of full length recombinant human N-terminal GST-tagged PDE4A1A expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID1321723Cytotoxicity against human THLE2 cells assessed as reduction in cell viability after 72 hrs by ATP Vialight assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1598446Selectivity ratio of IC50 for N-terminal GST-tagged human PDE2A1 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID241008Inhibitory concentration against human phosphodiesterase 102005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1421859Selectivity index, ratio of IC50 for inhibition of full length recombinant human N-terminal GST-tagged PDE6C expressed in baculovirus infected sf9 cells to IC50 for inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in bacu2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID240960Inhibition of human phosphodiesterase 42005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1598442Inhibition of N-terminal GST-tagged full length human PDE9A2 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1761536Binding affinity to sensorchip-immobilized human His-tagged CFTR F508 deletion mutant by surface plasmon resonance analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213In silico drug repositioning on F508del-CFTR: A proof-of-concept study on the AIFA library.
AID659072Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum GHA infected in human erythrocytes after 72 hrs using malstat staining by spectrophotometry2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.
AID1598450Selectivity ratio of IC50 for N-terminal GST-tagged human PDE8A1 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1421861Inhibition of recombinant human N-terminal GST-tagged PDE7A (122 to end residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID30201Half life in rat2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1384229Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 100 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1321699Inhibition of recombinant human PDE5A2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID240957Inhibition of human phosphodiesterase 12005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1598453Selectivity ratio of IC50 for N-terminal GST-tagged human PDE11A4 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1421854Inhibition of full length recombinant human N-terminal GST-tagged PDE1A expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID1598449Selectivity ratio of IC50 for N-terminal GST-tagged human PDE7 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID159035Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression2003Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
AID410415Inhibition of human recombinant PDE112008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1598429Selectivity ratio of IC50 for N-terminal GST-tagged human PDE6C to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1598445Selectivity ratio of IC50 for N-terminal GST-tagged human PDE1 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1421851Selectivity ratio of Ki for PDE6 (unknown origin) to Ki for PDE5 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID305334Inhibition of bovine PDE5 after 24 hrs by HTRF2007Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
AID1207268Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform
AID342571Vasorelaxation activity against noradrenaline-induced hypertonic contraction in Wistar rat aorta strips at 5 mM2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Methyl (11aS)-1,2,3,5,11,11a-hexahydro-3,3-dimethyl-1-oxo-6H-imidazo-[3',4':1,2]pyridin[3,4-b]indol-2-substituted acetates: synthesis and three-dimensional quantitative structure-activity relationship investigation as a class of novel vasodilators.
AID1635442Aqueous solubility of compound in water at 37 degC after 48 hrs by HPLC analysis2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID410414Inhibition of bovine PDE62008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
AID1598436Inhibition of human PDE2A1 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1421850Inhibition of PDE5 (unknown origin)2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID392051Inhibition of human ERG channel in HEK293 cells by voltage-clamp method2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Identification of "toxicophoric" features for predicting drug-induced QT interval prolongation.
AID229979Relative inhibition of bovine aorta PDE1 and PDE52003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID244235Ratio of inhibitory constant against phosphodiesterase 3 and phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID366091Inhibition of PDE52008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
AID1321724Cytotoxicity against mouse primary glial cells assessed as reduction in cell viability after 72 hrs by luminescence based ATPlite assay2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1598448Selectivity ratio of IC50 for N-terminal GST-tagged human PDE4 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1598440Inhibition of N-terminal GST-tagged human PDE7 expressed in baculovirus infected sf9 cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1598439Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1207542Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay
AID566804Inhibition of human recombinant PDE3B-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID366092Octanol-water partition coefficient, log P of the compound2008Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
AID566807Inhibition of human recombinant PDE11A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID23905The total clearance time in plasma in rat was determined2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1598447Selectivity ratio of IC50 for N-terminal GST-tagged human PDE3 to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID735476Selectivity ratio of IC50 for PDE2 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1321698Selectivity ratio of pLC50 for mouse primary glial cells to pLC50 for human THLE2 cells2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID157951Inhibition of Phosphodiesterase 5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID158129Inhibitory activity against phosphodiesterase 6 (PDE6) obtained from canine or bovine retina2003Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
AID735477Inhibition of PDE1 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID229359Relative inhibition of PDE6 from bovine retina and PDE5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID1384234Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID735486Inhibition of PDE2 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID229357Relative inhibition of PDE3 and PDE5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID597189Cytotoxicity against human MRC5 SV2 cells after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Drug to genome to drug: discovery of new antiplasmodial compounds.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1380338Inhibition of PDE5 (unknown origin)2018Journal of medicinal chemistry, 08-09, Volume: 61, Issue:15
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
AID1421863Inhibition of full length recombinant human N-terminal GST-tagged PDE9A2 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID1321739Inhibition of PDE5A in human SH-SY5Y cells assessed as increase in CREB phosphorylation at Ser133 residue at 500 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1421852Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-GMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID157949Inhibitory activity against phosphodiesterase 5 (PDE5) obtained from human corpus cavernosum tissue2003Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
AID1421871Inhibition of PDE5 in Wistar rat mesentric arteries assessed as inhibition of phenylephrine-induced contraction by measuring increase in acetylcholine-induced vasorelaxation by pressure myographic method2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1384231Inhibition of class-1 HDAC in human SH-SY5Y cells assessed as induction of AcH3K9 level at 1000 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID229355Relative inhibition of PDE1 from bovine heart and PDE5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID735474Selectivity ratio of IC50 for PDE3 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID159782Inhibition of Human recombinant PDE4 (Phosphodiesterase 4)2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1207355Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID1384228Inhibition of HDAC6 in human SH-SY5Y cells assessed as induction of tubulin K-40 acetylation level at 1000 nM after 2 hrs by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID229358Relative inhibition of PDE4 from rat kidney and PDE5 from human platelets2003Journal of medicinal chemistry, Feb-13, Volume: 46, Issue:4
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
AID1321728Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation after 2 hrs by Western blot analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID659073Cytotoxicity against human MRC5 SV2 cells after 72 hrs using resazurin by fluorimetry2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID244248Ratio of inhibitory constant against cone phosphodiesterase 6 and phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID1384205Inhibition of PDE5A (unknown origin)2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID1207509Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform
AID735468Selectivity ratio of IC50 for PDE11 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID735469Selectivity ratio of IC50 for PDE9 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID735479Inhibition of PDE9 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID244238Ratio of inhibitory constant against phosphodiesterase 1 and phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID597188Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum GHA strain infected in human erythrocytes after 72 hrs by spectrophotometry2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Drug to genome to drug: discovery of new antiplasmodial compounds.
AID244236Ratio of inhibitory constant against phosphodiesterase 4 and phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1193734Antimalarial activity against MRA-150, chloroquine, pyrimethamine, mefloquine-resistant asexual blood stage Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies.
AID1207415Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform
AID735487Inhibition of PDE5 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID240961Inhibition of human phosphodiesterase 52005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID1207388Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform
AID735484Inhibition of PDE4 (unknown origin) using FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1207295Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform
AID1173630Selectivity for PDE5 (unknown origin) over PDE11 (unknown origin)2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.
AID454868Inhibition of bovine platelet PDE52010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
AID240962Inhibition of human phosphodiesterase 62005Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID735481Inhibition of PDE8 (unknown origin) using FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1384233Inhibition of PDE5 in human SH-SY5Y cells assessed as induction of phosphorylated CREB level at 500 nM after 30 mins by Western blot analysis relative to control2018European journal of medicinal chemistry, Apr-25, Volume: 150Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
AID735485Inhibition of PDE3 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1598452Selectivity ratio of IC50 for N-terminal GST-tagged human PDE10A to IC50 for N-terminal GST-tagged human PDE5A12019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID735467Selectivity ratio of IC50 for PDE10 (unknown origin) to IC50 for PDE5 (unknown origin)2013European journal of medicinal chemistry, Feb, Volume: 60Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
AID1321732Inhibition of class 1 histone deacetylase in human SH-SY5Y cells assessed as increase in histone H3K9 acetylation at 1000 nM after 2 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1421858Inhibition of full length recombinant human N-terminal GST-tagged PDE6C expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
AID157928In vitro inhibitory activity against bovine phosphodiesterase 52003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
AID1598487Half-life in iv dosed rat2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
AID1321725Passive membrane permeability of the compound at 50 uM after 18 hrs by PAMPA2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
AID1345264Human phosphodiesterase 5A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID1345221Human phosphodiesterase 11A (Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs))2011Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
AID1797296Phosphodiesterase (PDE) Inhibition Assay from Article 10.1016/j.str.2004.10.004: \\Structural basis for the activity of drugs that inhibit phosphodiesterases.\\2004Structure (London, England : 1993), Dec, Volume: 12, Issue:12
Structural basis for the activity of drugs that inhibit phosphodiesterases.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2004Structure (London, England : 1993), Dec, Volume: 12, Issue:12
Structural basis for the activity of drugs that inhibit phosphodiesterases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,613)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's443 (27.46)29.6817
2010's862 (53.44)24.3611
2020's308 (19.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.18

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index62.18 (24.57)
Research Supply Index7.67 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index132.11 (26.88)
Search Engine Supply Index2.43 (0.95)

This Compound (62.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials392 (22.50%)5.53%
Reviews239 (13.72%)6.00%
Case Studies111 (6.37%)4.05%
Observational18 (1.03%)0.25%
Other982 (56.37%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (212)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized Control Trial to Assess the Efficacy of Tadalafil in Raynaud's Phenomenon in Scleroderma: A Double Blind, Parallel Group, Multicentric Study [NCT01117298]Phase 366 participants (Actual)Interventional2009-11-30Completed
Acute and Subacute Effect of Tadalafil Administration on Vasodilatation Mediated by Flow in Patients With Obesity Grade I-ii and Erectil Dysfunction [NCT03905018]Phase 380 participants (Anticipated)Interventional2019-05-01Recruiting
A Prospective, Open-label, Platform Study for Long-term Follow-up of Participants Using Study Intervention in Pulmonary Hypertension Parent Studies [NCT05179876]Phase 3230 participants (Anticipated)Interventional2022-05-04Recruiting
Functional Muscle Ischemia and PDE5A Inhibition in Duchenne Muscular Dystrophy [NCT01359670]Early Phase 130 participants (Actual)Interventional2011-05-31Completed
Efficacy and Safety of Focused Shockwave Therapy Plus Tadalafil vs Tadalafil Alone in Patient With Erectile Dysfunction: Randomized Controlled Trial [NCT05823506]36 participants (Anticipated)Interventional2023-02-01Recruiting
Clinical Efficacy of Phosphodiesterase-5 Inhibitor Tadalafil in Eisenmenger Syndrome - A Randomised, Placebo Controlled, Double Blind, Crossover Study [NCT01200732]Phase 228 participants (Actual)Interventional2008-02-29Completed
"Effect of Tadalafil, Sildenafil and Pentoxyfylline on Endometrial Thickness and Frozen Embryo Transfer Outcomes" [NCT05971667]Phase 2/Phase 3200 participants (Anticipated)Interventional2023-07-30Not yet recruiting
Evaluation of the Effects of a Daily Dose of 5 mg of Tadalafil on Lymphocyte to Monocyte Ratio and Monocyte to High-Density Lipoprotein Ratio in Patients With Erectile Dysfunction [NCT03918993]62 participants (Actual)Observational2019-02-14Completed
A Randomized Placebo Controlled Trial of Tadalafil for Erectile Dysfunction in Patients With Cirrhosis [NCT03566914]140 participants (Actual)Interventional2018-06-30Completed
PDE5 Inhibition for Obesity-Related Cardiometabolic Dysfunction [NCT02819440]Phase 2141 participants (Actual)Interventional2016-07-31Completed
A Randomized Controlled Double-Blind Trial for Prevention of Recurrent Ischemic Priapism in Men With Sickle Cell Disease: A Pilot Study [NCT05142254]Phase 264 participants (Actual)Interventional2022-04-01Active, not recruiting
[NCT03246880]Phase 3455 participants (Actual)Interventional2015-09-30Completed
Raising the Bars in the Treatment of Pulmonary Arterial Hypertension: Goal Oriented Strategy to Preserve Ejection Fraction Trial [NCT03236818]Phase 430 participants (Anticipated)Interventional2013-05-31Active, not recruiting
Multi-center, Randomized，Placebo and Positive Controlled Clinical Study of TPN171H Tablets on Acute Haemodynamics in Patients With Pulmonary Arterial Hypertension [NCT04483115]Phase 260 participants (Actual)Interventional2020-11-16Completed
An Open-label, Randomized, Multiple-dose Crossover Study to Evaluate a Pharmacokinetic Drug Interaction Between Tadalafil and Tamsulosin in Healthy Male Volunteers [NCT02239484]Phase 130 participants (Actual)Interventional2014-03-31Completed
Assessment of Single-dose Oral Tadalafil Pharmacokinetic Characteristics When Simultaneously Co-administered With Single-dose and Steady-state Tipranavir/Ritonavir 500 mg/200 mg to Healthy Male Volunteers [NCT02253862]Phase 117 participants (Actual)Interventional2005-12-31Completed
A Prospective, Randomized, 3-arm Parallel Trial to Evaluate the Safety and Clinical Effectiveness of 2 Lower Dose Combined PDE5i's vs. Single Maximal Dose PDE5i Treatment [NCT01364701]Phase 430 participants (Anticipated)Interventional2011-06-30Not yet recruiting
Comparison of the Efficacy and Safety of Low Intensity Extracorporeal Shock Wave Therapy Versus On-demand Tadalafil for Erectile Dysfunction [NCT05199727]50 participants (Anticipated)Interventional2021-09-01Recruiting
[NCT02839122]Phase 128 participants (Actual)Interventional2016-05-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Multicenter Study to Evaluate the Urodynamic Effects of Tadalafil Once a Day for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT00386009]Phase 2200 participants (Actual)Interventional2006-10-31Completed
Tadalafil as an Adjuvant to Therapy for Duchenne Muscular Dystrophy [NCT05195775]Phase 2/Phase 325 participants (Anticipated)Interventional2021-12-14Recruiting
A Pilot Study to Investigate the Effect of Phosphodiesterase Inhibitors on Chorioretinal Blood Flow Using Optical Coherence Tomography Angiography. [NCT04052269]Phase 330 participants (Anticipated)Interventional2019-06-21Suspended(stopped due to suspended due to COVID)
A Single-center, Open-label, Single-dose, Randomized, 2-way Crossover Phase 1 Study in Healthy Adult Participants to Assess the Relative Oral Bioavailability of the Combination of Macitentan/Tadalafil (10 mg/20 mg) Administered a Fixed-dose Combination Fo [NCT04540744]Phase 118 participants (Actual)Interventional2021-04-30Completed
Tadalafil and Acetazolamide Versus Acetazolamide in Acute Mountain Sickness Prevention [NCT01060969]55 participants (Actual)Interventional2006-01-31Completed
Prospective, Multi-center, Double-blind, Randomized, Active-controlled, Triple-dummy, Parallel-group, Group-sequential, Adaptive Phase 3 Clinical Study to Compare the Efficacy and Safety of Macitentan and Tadalafil Monotherapies With the Corresponding Fix [NCT03904693]Phase 3187 participants (Actual)Interventional2019-07-29Active, not recruiting
Effect of PDE5 Inhibitor on Respiratory Symptoms in COPD Complicated by Pulmonary Hypertension [NCT05937854]Phase 2126 participants (Anticipated)Interventional2024-01-15Not yet recruiting
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, 5-Group, Multinational Study to Evaluate the Efficacy, Dose Response, and Safety of Tadalafil Once-a-Day Dosing for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT00384930]Phase 2/Phase 31,058 participants (Actual)Interventional2006-08-31Completed
Investigational and Comparative Study to Assess Safety and Effectiveness of Tadalafil and Pentoxifyllin in the Management of Diabetic Nephropathy [NCT05487755]Phase 390 participants (Actual)Interventional2022-01-01Active, not recruiting
Double-blind, Placebo-controlled Study on Men With Lower Urinary Tract Symptoms to Assess Changes in Pressure Flow Study and in Molecular Profile of Prostatic Tissue After 12 Weeks Treatment With Tadalafil. [NCT02252367]Phase 486 participants (Actual)Interventional2015-12-31Completed
A Study Evaluating the Therapeutic Efficacy of Tamsulosin and Tadalafil Compared to Placebo in the Treatment and Prevention of Urinary Disorders After Transperineal Prostate Biopsy [NCT05537272]Phase 4120 participants (Anticipated)Interventional2022-09-01Enrolling by invitation
The Effect of Selective PDE-5 Inhibition on Capillary Recruitment, Glucose Uptake and Endothelial Function Following a Mixed Meal in Patients With Type 2 Diabetes Patients. [NCT01238224]Phase 122 participants (Actual)Interventional2009-11-30Terminated(stopped due to Durability of study medications could not be guaranteed after the expire date.)
An Open-label Trial of Oral Selegiline 5 or 10 mg and Tadalafil 2.5mg Co-administration to Male Patients With Parkinson's Disease and Moderate Erectile Dysfunction. [NCT02225548]Phase 410 participants (Anticipated)Interventional2014-09-30Recruiting
PERIOP-04 Phase Ib Trial of Perioperative Tadalafil and Influenza Vaccination in Cancer Patients Undergoing Major Surgical Resection of a Primary Abdominal Malignancy [NCT02998736]Phase 128 participants (Actual)Interventional2017-11-21Completed
The Effect of Tadalafil on Cerebral Large Arteries in Stroke Patients [NCT02801032]Phase 220 participants (Actual)Interventional2016-11-29Completed
The Phosphodiesterase Inhibitor Tadalafil as an Adjunct to Antidepressants in Major Depressive Disorder Patients: Randomized, Double-Blind, Placebo-Controlled Trial [NCT05030623]Phase 1/Phase 2100 participants (Anticipated)Interventional2021-08-01Recruiting
Effect of Tadalafil on Exercise Capacity in Pediatric Fontan Patients [NCT01291069]Phase 120 participants (Actual)Interventional2011-09-30Completed
A Prospective Case-crossover Study to Evaluate the Possible Association Between the Use of PDE5 Inhibitors and the Risk of Acute Nonarteritic Anterior Ischemic Optic Neuropathy (NAION) [NCT01131104]345 participants (Actual)Observational2010-05-31Completed
Do Phosphodiesterase 5A Inhibitors Improve Exercise Capacity in Patients With Chronic Obstructive Pulmonary Disease and Pulmonary Hypertension? [NCT01197469]Phase 2120 participants (Actual)Interventional2010-09-30Completed
The Effects of Mirabegron and Tadalafil on Glucose Tolerance in Prediabetics [NCT05051436]Phase 496 participants (Anticipated)Interventional2021-12-13Recruiting
A Randomized, Double-Blind, Parallel, Placebo-Controlled Study in Men With Erectile Dysfunction to Evaluate the Efficacy and Safety of Tadalafil When Sexual Attempts Occur at Specific Time Points After Dosing [NCT00547508]Phase 3485 participants (Actual)Interventional2002-10-31Completed
Non Ablative Erbium:YAG Laser Transurethral Treatment for Chronic Prostatitis/Chronic Pelvic Pain Syndrome in Younger Patients: a Prospective Comparative Study [NCT04446598]36 participants (Actual)Interventional2017-03-13Completed
Exploratory Trial of Immunochemoradiotherapy for Locally Advanced Pancreatic Adenocarcinoma [NCT01342224]Phase 111 participants (Actual)Interventional2011-01-31Completed
Investigator Sponsored Research Proposal : Efficacy and Safety of Combination Ambrisentan and TadaLafil in PATiEnts With PortoPulmonary Hypertension (ESCALATE-PPH) [NCT03309592]Phase 40 participants (Actual)Interventional2017-10-12Withdrawn(stopped due to Lack of eligible participants and failure to meeting study enrollment.)
Study on New Insights in Remodeling of Endocrine Cardiomyopathies: Intramyocardial, Molecular and Neuroendocrine Assessment in Response to Chronic Inhibition of Cyclic GMP Phosphodiesterase 5A in Cushing's Syndrome [NCT02611258]Phase 218 participants (Actual)Interventional2016-07-31Completed
Skeletal Muscle Blood Flow in Becker Muscular Dystrophy [NCT02653833]Early Phase 16 participants (Actual)Interventional2017-11-01Terminated(stopped due to PI passed away)
Effects of Daily Tadalafil on Body Composition in Men With Sexual Distress [NCT02554045]Phase 420 participants (Actual)Interventional2015-01-31Completed
An Open-label, Multicenter Study of Ambrisentan and a Phosphodiesterase Type-5 Inhibitor Combination Therapy in Subjects With Pulmonary Arterial Hypertension Who Have Demonstrated a Sub-Optimal Response to a Phosphodiesterase Type-5 Inhibitor [NCT00617305]Phase 438 participants (Actual)Interventional2008-04-30Completed
A Phase 1 Study to Demonstrate the Relative Bioavailability of Fixed Dose Combinations of Ambrisentan and Tadalafil in Healthy Subjects [NCT02688387]Phase 1112 participants (Actual)Interventional2016-03-18Completed
The Safety of Dapoxetine/Tadalafil Combination Therapy in Treatment of Men With Premature Ejaculation and Erectile Dysfunction [NCT03177746]Phase 440 participants (Anticipated)Interventional2022-12-31Not yet recruiting
Low Dose Tadalafil 5mg for Treatment of Female Overactive Bladder Syndrome :6 Months Follow up [NCT04500860]Phase 190 participants (Actual)Interventional2020-12-01Completed
The Effect of Combination Therapy Using Li-ESWT (Low Intensity Extracorporeal Shockwave Therapy) and PDE-5 Inhibitor in Patients With Erectile Dysfunction [NCT05043896]30 participants (Actual)Interventional2019-12-10Completed
A Prospective, Randomized, International, Multicenter, Double-arm, Controlled, Open-label Study of Riociguat in Patients With Pulmonary Arterial Hypertension (PAH) Who Are on a Stable Dose of Phosphodiesterase-5 Inhibitors (PDE-5i) With or Without Endothe [NCT02891850]Phase 4225 participants (Actual)Interventional2017-01-11Completed
The Use of Tadalafil in Confirmed COVID-19 Pneumonia. [NCT04946162]Phase 40 participants (Actual)Interventional2020-04-20Withdrawn(stopped due to The investigators never completed the IRB application due to decrease in need to conduct the study.)
A Randomized, Open Label, Single Dose, Two-way Crossover Clinical Trial to Investigate the Pharmacokinetics and Safety/Tolerability of YY-201 in Comparison to Dutasteride and Tadalafil Administered in Healthy Male Volunteer [NCT03240939]Phase 136 participants (Actual)Interventional2017-03-27Completed
A Phase II Study of Tadalafil and Pembrolizumab in Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma [NCT03993353]Phase 26 participants (Actual)Interventional2020-04-07Active, not recruiting
A Phase III, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy of Tadalafil Versus Placebo in Improving Hemodynamics and End-Organ Dysfunction in Fontan Physiology (TRIUMPH Trial) [NCT05206955]Phase 380 participants (Anticipated)Interventional2022-09-16Recruiting
An Extension Study to Evaluate the Long-Term Safety and Efficacy of the Phosphodiesterase Type 5 (PDE5) Inhibitor Tadalafil in the Treatment of Patients With Pulmonary Arterial Hypertension [NCT00549302]Phase 3357 participants (Actual)Interventional2005-12-31Completed
Tadalafil 5 mg Once a Day Compared to Placebo in Improving Erectile Dysfunction and Sexual Quality of Life [NCT00422734]Phase 3342 participants (Actual)Interventional2006-11-30Completed
Single-center, Open-label, Single-dose, 2-period, Randomized, Crossover Phase 1 Study to Demonstrate Bioequivalence of Tadalafil Administered as a Fixed Dose Combination Formulation of Macitentan/Tadalafil (10 mg/40 mg) and as the Free Combination of 10 m [NCT04235270]Phase 162 participants (Actual)Interventional2020-01-17Completed
A Randomized, Open-label, Multi-center, Parallel Group Study to Investigate the Efficacy and Safety of Vardenafil in Comparison to Tadalafil in Males With Erectile Dysfunction and a Diagnosis of Diabetes, Hypertension or Hyperlipidemia [NCT00668109]Phase 3614 participants (Actual)Interventional2003-12-31Completed
A Phase II Trial of Tadalafil in Patients With Squamous Cell Carcinoma of the Upper Aero Digestive Tract [NCT00894413]Phase 245 participants (Actual)Interventional2007-05-08Completed
Efficacy of Phosphodiesterase Type 5 Inhibitors in Severe Pulmonary Hypertension Due to Chronic Obstructive Pulmonary Disease [NCT05844462]Phase 3200 participants (Anticipated)Interventional2024-01-31Not yet recruiting
A Randomized, Double-Blind, Placebo-Controlled, Parallel Design, Multinational Study to Evaluate the Efficacy and Safety of Tadalafil 2.5 and 5 mg Once Daily Dosing for 12 Weeks for the Treatment of Erectile Dysfunction and Signs and Symptoms of Benign Pr [NCT00855582]Phase 3606 participants (Actual)Interventional2009-03-31Completed
Obesity-induced ED Response to Combined Effect of Tadalafil Drug in Addition to Interval and Continuous Training [NCT04623840]60 participants (Anticipated)Interventional2020-10-12Recruiting
A Randomized, Double-Blind, Parallel-Design, Placebo-Controlled Study to Evaluate the Effects of 5 mg Tadalafil (IC351, LY450190) and 50 mg Sildenafil Administered Once Daily for 6 Months on Visual Function in Healthy Subjects or Subjects With Mild Erecti [NCT00333281]Phase 4198 participants Interventional2005-06-30Completed
Pilot Study of Phosphodiesterase-5 Inhibitor Tadalafil (Cialis) as an Immunomodulator in Patients With Oral Cavity and Oropharyngeal Squamous Cell Carcinoma. [NCT00843635]35 participants (Actual)Interventional2008-09-30Completed
[NCT00705588]Phase 430 participants (Anticipated)Interventional2008-08-31Not yet recruiting
A Comparison of Psychosocial Outcomes Following Tadalafil Once a Day or PDE5 Inhibitor As Needed in Men With Erectile Dysfunction. [NCT00734604]Phase 3378 participants (Actual)Interventional2008-08-31Completed
A Postmarketing Observational Study to Assess Respiratory Tract Adverse Events in Pulmonary Arterial Hypertension Patients Treated With Tyvaso® (Treprostinil) Inhalation Solution [NCT01266265]1,333 participants (Actual)Observational2010-12-31Completed
Renin Angiotensin Aldosterone System (RAAS) and Fibrinolysis in Humans: ACEi [NCT00750308]27 participants (Actual)Interventional2006-12-31Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design Study to Evaluate the Safety and Efficacy of Daily Tadalafil for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia on Concomitant Alpha1-Adrenergic Blocker Ther [NCT00848081]Phase 3318 participants (Actual)Interventional2009-03-31Completed
[NCT02862483]Phase 3330 participants (Anticipated)Interventional2016-03-31Recruiting
Tadalafil Once Daily Following As-Needed Phosphodiesterase Type 5 Inhibitor Treatment, an Assessment of Return to Normal Erectile Function [NCT01130532]Phase 4623 participants (Actual)Interventional2010-08-31Completed
Impact of Tadalafil (LY450190) Once a Day or Tadalafil on Demand Compared to Sildenafil Citrate on Demand on Treatment Discontinuation in Patients With Erectile Dysfunction Who Are naïve to PDE5 Inhibitors [NCT01122264]Phase 4770 participants (Actual)Interventional2010-05-31Completed
National, Multicenter, Randomized, Double-blind, Double-dummy, Phase III Clinical Trial to Evaluate the Efficacy and Safety of Toronto Association in the Treatment of Erectile Dysfunction and Premature Ejaculation [NCT05052879]Phase 3232 participants (Anticipated)Interventional2024-07-31Not yet recruiting
Evaluation of Retinal and Choriocapillary Vascular Changes Using Optical Coherence Tomography Angiography in Patients Undergoing Tadalafil 20mg on Alternative Days: a Single-centre Prospective-control [NCT04164355]40 participants (Actual)Observational2020-07-04Completed
PDE5 Inhibition Via Tadalafil (Cialis®) to Enhance Anti-Tumor MUC1 Vaccine Efficacy in Patients With Resectable, and Recurrent or Second Primary Head and Neck Squamous Cell Carcinoma (HNSCC): A Phase I/II Clinical Trial [NCT02544880]Phase 116 participants (Actual)Interventional2016-04-25Completed
A Phase 3, Randomized, Double Blind, Placebo and Tamsulosin Controlled, Parallel Design, Multinational Study to Evaluate the Efficacy and Safety of Tadalafil Once a Day Dosing for 12 Weeks in Asian Men With Signs and Symptoms of Benign Prostatic Hyperplas [NCT00861757]Phase 3612 participants (Actual)Interventional2009-03-31Completed
Switching From Sildenafil Citrate to Tadalafil in Treatment of Erectile Dysfunction: Assessment of Treatment Preference [NCT00547352]Phase 4160 participants (Actual)Interventional2004-06-30Completed
A Multicenter, Parallel-Arm, Placebo-Controlled, Double-Blind Study to Evaluate the Efficacy and Safety of Tadalafil Administered Once Daily to Men With Lower Urinary Tract Symptoms Secondary to Benign Prostatic Hyperplasia [NCT00547625]Phase 2275 participants (Actual)Interventional2004-10-31Completed
A Randomized Controlled Trial to Examine the Utility of Tadalafil (5mg) For Treatment of Early Storage Symptoms and Erectile Dysfunction After Anatomical Endoscopic Enucleation of Prostate (AEEP) [NCT05955001]Phase 2/Phase 3110 participants (Anticipated)Interventional2023-04-01Active, not recruiting
Study on New Insights in Remodeling of Endocrine Cardiomyopathies: ASsessmentt of Intramyocardial, Molecular and NeUroendocrine Parameters in Response to Chronic Inhibition of Cyclic GMP Phosphodiesterase 5A in AcroMegaly [NCT02611336]Phase 215 participants (Actual)Interventional2016-07-31Completed
Effect of PDE5 Inhibition on Adipose Metabolism in Humans [NCT04684589]Phase 2100 participants (Anticipated)Interventional2021-03-16Recruiting
A Randomised, Double-Blind, Placebo-Controlled Study to Evaluate the Effect on Unassisted Erectile Function of the Early Use of Tadalafil 5 mg Once a Day and Tadalafil 20 mg On Demand Treatment for 9 Months in Subjects Undergoing Bilateral Nerve-Sparing R [NCT01026818]Phase 4583 participants (Actual)Interventional2009-11-30Completed
Effects on Insulin Resistance With the Phosphodiesterase-5 Inhibitor Tadalafil in Type 2 Diabetes - a Double-blind, Placebo-controlled Crossover Study [NCT02601989]Phase 223 participants (Actual)Interventional2015-11-30Completed
"An Open-Label Study to Evaluate the Efficacy and Safety of Tadalafil Administered On Demand to Men of Various Populations With Erectile Dysfunction" [NCT00547417]Phase 31,933 participants (Actual)Interventional2003-07-31Completed
"A Multinational, Randomized, Double-Blind, Parallel, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Tadalafil Administered On Demand to Asian Men With Erectile Dysfunction" [NCT00547573]Phase 3367 participants (Actual)Interventional2003-04-30Completed
Safety and Effectiveness of Adcirca (Tadalafil) in Japanese Patients With Pulmonary Arterial Hypertension: Open-label, Non-interventional Observational Study in Japan [NCT01066845]1,809 participants (Actual)Observational2010-01-31Completed
A Randomized, Double-blind, Placebo-controlled Cross-over Trial Assessing the Effect of Tadalafil (Cialis) on the Cardiovascular System in Men With Complete Spinal Cord Injury (SCI) at or Above the Sixth Thoracic Level [NCT01067391]Phase 420 participants (Actual)Interventional2009-10-31Completed
Functional Muscle Ischemia and PDE5A Inhibition in Becker Muscular Dystrophy [NCT01070511]Phase 448 participants (Anticipated)Interventional2010-01-31Completed
Daily Tadalafil and Gastric Emptying Time in Diabetic Gastroparesis [NCT01326117]Phase 40 participants (Actual)Interventional2011-04-30Withdrawn(stopped due to lack of patients who meet inclusion criteria; there was one screen failure)
Can Tadalafil (Cialis)® Maintain Erectile Function In Patients Treated With External-beam Radiotherapy For Prostate Cancer? A Randomized, Double-blind, Placebo-controlled Study [NCT00215631]Phase 3100 participants Interventional2005-10-31Terminated(stopped due to slow recruitment)
Phase I Trial of Chemoimmunotherapy and Hypofractionated Radiation Therapy for Borderline Resectable and Locally Advanced Pancreatic Adenocarcinoma. [NCT01903083]Phase 110 participants (Actual)Interventional2013-07-31Completed
[NCT01942551]Phase 147 participants (Actual)Interventional2013-09-30Completed
Improving Cerebral Blood Flow and Cognition in Patients With Cerebral Small Vessel Disease. The ETLAS-2 Trial [NCT05173896]Phase 2100 participants (Anticipated)Interventional2022-05-31Recruiting
Phosphodiesterase Type 5 Inhibition With Tadalafil Changes Outcomes in Heart Failure: Extent of Renal Damage (PITCH-ER) [NCT01960153]Phase 30 participants (Actual)Interventional2013-10-31Withdrawn(stopped due to Award was ended by NIH for parent study)
AMBITION: A Randomised, Multicenter Study of First-Line Ambrisentan and Tadalafil Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH) [NCT01178073]Phase 3610 participants (Actual)Interventional2010-10-01Completed
Phase II Study of Nivolumab (Anti-PD1), Tadalafil and Oral Vancomycin in Patients With Refractory Primary Hepatocellular Carcinoma or Liver Dominant Metastatic Cancer From Colorectal or Pancreatic Cancers [NCT03785210]Phase 222 participants (Actual)Interventional2019-06-05Completed
A Randomized, Double Blind, Placebo-controlled Study to Evaluate the Effect of Tadalafil Once Daily for 8 Weeks on Prostatic Blood Flow and Perfusion Parameters in Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT01152190]Phase 397 participants (Actual)Interventional2010-09-30Completed
Safety and Efficacy of Tadalafil vs. Tadalafil With Sildosin in the Management of Moderately and Severely Symptomatic Patients of Prostatic Hyperplasia [NCT04577040]400 participants (Anticipated)Observational2020-10-01Not yet recruiting
A Multi-centre, Randomised, Open-label, Home Use, Parallel Group, Clinical Investigation of Topically-applied MED3000 Gel and Oral Tadalafil (5 mg) Tablets for the Treatment of Erectile Dysfunction (ED) Over a 24 Week Period [NCT04984993]Phase 3116 participants (Actual)Interventional2021-09-14Completed
A Multi-center, Randomized, Double-blinded, Double-dummy, Parallel Group, 48-week, Phase III Clinical Trial to Evaluate the Efficacy and Safety of DKF-313 in Patients With Benign Prostatic Hyperplasia [NCT04947631]Phase 3667 participants (Actual)Interventional2021-07-27Completed
Randomised Control Trial to Assess the Efficacy of Tadalafil in Raynaud's Phenomenon in Scleroderma [NCT00626665]Phase 325 participants (Actual)Interventional2007-12-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Study to Assess the Efficacy and Safety of Tadalafil (LY450190) Once a Day in Subjects With Erectile Dysfunction Who Are Naïve to PDE5 Inhibitors [NCT00836693]Phase 3217 participants (Actual)Interventional2009-01-31Completed
An Open-Label, Phase II Single-Arm, Window Trial of Tadalafil Effect + Chemotherapy in Patients With Resectable Gastric/GEJ Adenocarcinoma [NCT05709574]Phase 210 participants (Anticipated)Interventional2023-03-03Recruiting
A Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Pilot Study to Evaluate the Efficacy and Safety of Tadalafil and Tamsulosin Once-a-Day Dosing for 12 Weeks in Asian Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT00540124]Phase 2151 participants (Actual)Interventional2007-10-31Completed
Randomized, Placebo-Controlled, Double-Blind, Cross-Over Trial of the Efficacy and Safety of IC351 in Female Patients With Raynaud Phenomenon and Female Sexual Dysfunction Secondary to Systemic Sclerosis [NCT00707187]Phase 2120 participants (Actual)Interventional2001-07-31Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Study to Assess Efficacy and Safety of Tadalafil (LY450190) in Subjects With Erectile Dysfunction Caused by Spinal Cord Injury [NCT00421083]Phase 3180 participants Interventional2004-09-30Completed
A Randomized, Double-blind, Placebo-controlled Phase III Trial to Evaluate the Effectiveness of a Phosphodiesterase 5 Inhibitor, Tadalafil, in Prevention of Erectile Dysfunction in Patients Treated With Radiotherapy for Prostate Cancer [NCT00931528]Phase 3242 participants (Actual)Interventional2009-11-30Completed
A Randomized, Open-Label, Crossover, Multicenter, Single Dose Comparator Study Evaluating Onset Of Penile Rigidity In Men With Erectile Dysfunction Who Are Treated With Viagra (Sildenafil Citrate) And Cialis (Tadalafil) [NCT00644956]Phase 456 participants (Actual)Interventional2003-06-30Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Global Multicenter Study to Evaluate the Efficacy and Safety of Tadalafil Once Daily Dosing for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT00970632]Phase 3511 participants (Actual)Interventional2009-10-31Completed
A Randomised, Double-blind, Double-dummy, Parallel-group, Active-controlled Study Evaluating the Efficacy of Vardenafil Versus Tadalafil When Intercourse is Attempted Within 45 Minutes of Administration in Subjects With Erectile Dysfunction [NCT00663130]Phase 4759 participants (Actual)Interventional2004-04-30Completed
A Phase 3b, Randomized, Double-blind, Placebo-controlled Parallel-design Study to Evaluate the Efficacy and Safety of Tadalafil Co-administered With Finasteride for 6 Months in Men With Lower Urinary Tract Symptoms and Prostatic Enlargement Secondary to B [NCT01139762]Phase 3696 participants (Actual)Interventional2010-09-30Completed
Multi-center, Randomized, Double-blind, Placebo/Active-controlled, Phase II Clinical Trial to Assess the Safety and Efficacy of YHD1023 in Patients With Erectile Dysfunction [NCT01423370]Phase 2104 participants (Anticipated)Interventional2011-11-30Completed
A Randomized, Open-label, Oral Single Dosing, Two-way Crossover Clinical Trial to Evaluate the Effects of Food on the Bioavailability of CKD-397 After a Single Oral Dose in Healthy Male Subjects [NCT02615782]Phase 116 participants (Actual)Interventional2015-12-31Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Multinational Study to Evaluate the Efficacy and Safety of Daily Tadalafil for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT00827242]Phase 3325 participants (Actual)Interventional2009-01-31Completed
Tadalafil 2.5 mg and 5 mg Once a Day Compared to Placebo in Day of Onset of Efficacy [NCT00833638]Phase 4372 participants (Actual)Interventional2009-02-28Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design Study to Evaluate the Efficacy and Safety of Tadalafil Once-a-Day Dosing for 12 Weeks Followed by an Open-Label Extension to Evaluate the Long-Term Safety and Efficacy of Tadalafil i [NCT00783094]Phase 2422 participants (Actual)Interventional2008-11-30Completed
Assessment of Efficacy of Mirabegron, Solifenacin, Tadalafil 5mg and Combination Therapy in Female Patients With Overactive Bladder: A Double Blinded Prospective Randomized Placebo -Controlled Trial [NCT06184334]300 participants (Actual)Interventional2022-09-14Completed
Prospective Observational Trial of Combination Therapy of Tadalafil 5mg Plus Tamsulosinmg for Men With Lower Urinary Tract Symptoms and Erectile Dysfunction [NCT04383093]75 participants (Actual)Observational2017-01-01Completed
A Phase 1, Open Label, Randomized, Four Period, Crossover, Multiple Dose Study To Assess The Pharmacokinetic Interaction Between Sitaxsentan and Tadalafil and The Effect Of Sildenafil On Sitaxsentan PK In Healthy Subjects [NCT01244620]Phase 116 participants (Actual)Interventional2010-11-30Terminated(stopped due to Safety Issue: The trial was prematurely terminated on Dec 9, 2010, due to safety concerns, specifically new emerging evidence of hepatic injury.)
Define in Preclinical Diastolic Dysfunction (PDD) With Renal Dysfunction, the Cardiorenal and Humoral Actions of Chronic Type V Phosphodiesterase (PDEV) Inhibition [NCT02058095]Phase 1/Phase 222 participants (Actual)Interventional2014-03-31Completed
To Define the Role of PDEV in Mediating the Decreased GFR and Attenuated Renal Sodium and cGMP Excretory Response to Acute Saline Volume Expansion in PSD and PDD With Renal Dysfunction. [NCT01544998]Phase 1/Phase 243 participants (Actual)Interventional2012-02-29Completed
A Double Blind Randomized Control Trial of Tadalafil in Interstitial Lung Disease of Scleroderma [NCT01553981]Phase 340 participants (Actual)Interventional2012-03-31Completed
Tadalafil for Sarcoidosis Associated Pulmonary Hypertension [NCT01324999]Phase 2/Phase 312 participants (Actual)Interventional2011-03-31Completed
Functional Muscle Ischemia and PDE5 Inhibition in Duchenne Muscular Dystrophy: Acute Dosing Study [NCT01580501]Phase 112 participants (Anticipated)Interventional2012-03-31Completed
Observational Study to Evaluate the Effect of Tadalafil 5mg Once Daily on Erectile Dysfunction and QOL in Andropause Patients With Erectile Dysfunction [NCT02943356]Phase 440 participants (Anticipated)Interventional2016-07-31Recruiting
A Phase 2 Study of the Safety, Efficacy, and Immune Response of CRS-207, Pembrolizumab, Ipilimumab, and Tadalafil in Patients With Previously Treated Metastatic Pancreatic Adenocarcinoma [NCT05014776]Phase 220 participants (Anticipated)Interventional2022-08-22Recruiting
Comparing The Effect of Tadalafil 5 mg/Day to Sildenafil 25 mg/Day on Neutrophil-Lymphocyte and Platelet-Lymphocyte Ratios in Erectile Dysfunction Patients; and Comparison of Clinical Response [NCT05466695]Early Phase 174 participants (Anticipated)Interventional2022-08-01Not yet recruiting
A Multicenter Open-Label Study to Determine Treatment Preference of Tadalafil (IC351, LY450190) or Sildenafil Citrate in the Oral Treatment of Erectile Dysfunction [NCT00547092]Phase 4386 participants (Actual)Interventional2003-10-31Completed
Switching From Sildenafil Citrate to Tadalafil in Treatment of Erectile Dysfunction: Multinational Assessment of Treatment Preference [NCT00547287]Phase 32,760 participants (Actual)Interventional2002-11-30Completed
Does Presence of Distress Due to Erectile Dysfunction Affect the Effect of Tadalafil on Sexual Life and Life Satisfaction? [NCT00547599]Phase 4659 participants (Actual)Interventional2003-04-30Completed
The Pharmacological Basis for the Increase in Visual Time Constants Induced by Single Oral Doses of Sildenafil [NCT00463957]12 participants Interventional2006-08-31Active, not recruiting
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Study to Evaluate the Efficacy and Safety of Tadalafil Once-a-day Dosing for 12 Weeks in Asian Men With Signs and Symptoms of Benign Prostatic Hyperplasia [NCT01460342]Phase 3610 participants (Actual)Interventional2011-12-31Completed
Randomized Placebo Controlled Trial of Treprostinil Infusion Combined With Oral Tadalafil or Placebo in Pulmonary Arterial Hypertension [NCT01302444]Phase 41 participants (Actual)Interventional2011-03-31Terminated(stopped due to One subject enrolled and completed this study. The study was stopped due to poor recruitment.)
A Phase II Trial of Tadalafil in Patients With Squamous Cell Carcinoma of the Upper Aero Digestive Tract [NCT01697800]Phase 240 participants (Actual)Interventional2012-09-30Completed
A Randomized, Double-Blind, Parallel, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Tadalafil (2.5mg and 5mg) Administered Once Daily to Men With Erectile Dysfunction [NCT00381732]Phase 3280 participants (Actual)Interventional2003-10-31Completed
A Clinical Trial of Ambrisentan and Tadalafil in Pulmonary Arterial Hypertension Associated With Systemic Sclerosis [NCT01042158]Phase 425 participants (Actual)Interventional2010-01-31Completed
A Study to Assess the Efficacy of Tadalafil to Treat Erectile Dysfunction After Radiotherapy of Prostate Cancer [NCT00122499]Phase 30 participants Interventional2003-02-28Completed
Efficiency of Tadalafil for Management of Female Sexual Dysfunction in Females With Genital Mutilation [NCT05266651]Phase 2/Phase 324 participants (Anticipated)Interventional2022-03-10Not yet recruiting
Efficacy and Safety of Tadalafil 20mg for the Treatment of Erectile Dysfunction in Chronic Renal Patients in Hemodialysis. [NCT00334477]Phase 260 participants InterventionalNot yet recruiting
Pilot Study to Investigate the Effect of Tadalafil on Secondary Pulmonary Hypertension in Chronic Obstructive Pulmonary Disease [NCT00506701]0 participants (Actual)Interventional2008-02-29Withdrawn(stopped due to due to lack of finance)
A Randomized, Double-Blind, Parallel Group, Placebo-Controlled Study Evaluating the Efficacy and Safety of Tadalafil (5mg and 20mg) Administered Once Daily to Subjects With Mild to Moderate Hypertension [NCT00157326]Phase 2180 participants (Actual)Interventional2005-09-30Completed
Low-intensity Shockwaves Therapy Co-administered With Tadalafil 5mg for the Treatment of Severe, Vasculogenic Erectile Dysfunction:Validation of an Evidence Based Protocol in a Randomized, Sham-controlled Trial [NCT03642366]51 participants (Anticipated)Interventional2018-08-27Recruiting
Tadalafil for the Treatment of Secondary Raynaud's Phenomenon [NCT00822354]10 participants (Actual)Interventional2008-09-30Completed
A Study to Evaluate the Pharmacokinetics of Tadalafil Administered Once Daily in Japanese and Non-Japanese Subjects With Benign Prostatic Hyperplasia [NCT01183650]Phase 124 participants (Actual)Interventional2010-07-31Completed
CombinatiON Up-FRON t Therapy for PAH - A Phase 4, Randomized, Multicenter Study of Inhaled Treprostinil in Treatment naïve Pulmonary Arterial Hypertension Patients Starting on Tadalafil [NCT01305252]Phase 421 participants (Actual)Interventional2010-07-31Completed
A Double Blind, Placebo Controlled, Parallel Group, Multicenter Study To Assess The Duration Of Action, Safety And Toleration Of Differing Doses and Combinations Of Immediate and Modified Release Formulations Of UK-369,003 and Cialis Compared To Placebo I [NCT00174486]Phase 2300 participants Interventional2005-02-28Completed
Tadalafil for Treatment of Priapism in Men With Sickle Cell Anemia [NCT00538564]Phase 20 participants (Actual)Interventional2006-11-30Withdrawn(stopped due to Trial closed just prior to study receiving Investigational Review Board approval)
A Randomized, Double-Blind, Parallel-Design, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Tadalafil (2.5 mg and 5 mg) Administered Once Daily to Men With Diabetes Mellitus and Erectile Dysfunction [NCT00547183]Phase 3298 participants (Actual)Interventional2004-10-31Completed
"A Randomized, Double-Blind, Placebo-Controlled Study of the Efficacy and Safety of Tadalafil Administered On Demand to Patients With Erectile Dysfunction" [NCT00547495]Phase 3343 participants (Actual)Interventional2004-03-31Completed
PHIRST-1: Randomized, Double-Blind, Placebo-Controlled Phase 3 Study of the Phosphodiesterase Type 5 (PDE5) Inhibitor Tadalafil in the Treatment in Patients With Pulmonary Arterial Hypertension [NCT00125918]Phase 3406 participants (Actual)Interventional2005-08-31Completed
A Study of LY900010 (LY2452473 + Tadalafil) in the Treatment of Men With Erectile Dysfunction [NCT01160289]Phase 2410 participants (Actual)Interventional2010-10-31Completed
Impact of Tadalafil 5 mg on Post-micturition Dribble in Young-age Men With no/Mild Lower Urinary Tract Symptoms: a Randomized Controlled Trial [NCT05146674]80 participants (Anticipated)Interventional2022-01-01Not yet recruiting
An Evaluation of Semen Characteristics After 40 Weeks Daily Dosing With 20 mg Tadalafil [NCT00382135]Phase 4282 participants (Actual)Interventional2003-11-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel Study of IC351 (LY450190) in Patients With Diabetic Gastroparesis [NCT00050609]Phase 22 participants (Actual)Interventional2003-02-28Completed
"Low-intensity Shockwave Therapy (LiST) for the Treatment of Mild and Mild-to-moderate Vasculogenic Erectile Dysfunction: a Randomized Placebo Controlled Two-parallel Arms Trial, Comparing 6 Sessions, With Daily Tadalafil 5mg vs Placebo" [NCT03641846]50 participants (Actual)Interventional2018-08-28Completed
Window of Opportunity Trial of Nivolumab and Tadalafil in Patients With Squamous Cell Carcinoma of the Head and Neck [NCT03238365]Early Phase 150 participants (Actual)Interventional2017-08-10Completed
Prospective, Multicenter, Open-label Study Evaluating the Effects of First-line Oral Combination Therapy of Macitentan and Tadalafil in Patients With Newly Diagnosed Pulmonary Arterial Hypertension (OPTIMA). [NCT02968901]Phase 446 participants (Actual)Interventional2015-09-01Terminated
Use of a Phosphodiesterase Type 5 Inhibitor to Improve Anabolic Resistance in Older Adults [NCT05458232]0 participants (Actual)Observational2023-01-20Withdrawn(stopped due to No subjects enrolled)
A Randomized, Open-label, Single-dose, 2-treatment, 2-way, 2-period Crossover Study to Evaluate the Safety and the Pharmacokinetic Characteristics of DKF-313 in Healthy Male Volunteers [NCT02352311]Phase 154 participants (Actual)Interventional2015-01-31Completed
Phase 2 Clinical Trial to Evaluate Safety and Efficacy of BZ371A In A Gel Applied in Patients That Performed Radical Prostatectomy [NCT05558007]Phase 272 participants (Anticipated)Interventional2023-11-30Recruiting
Phase 3 Randomized Trial of Tadalafil and Glycemic Traits [NCT01444651]Phase 373 participants (Actual)Interventional2011-08-31Completed
Effect of Tadalafil on the Quality of Life and Sexual Life in Erectile Dysfunction (ED) Patients Previously Treated With Other Oral ED Therapy [NCT00422578]Phase 4200 participants Interventional2004-10-31Completed
Effect of Tadalafil on Insulin Secretion and Insulin Sensitivity in Obese Men. [NCT02595684]Phase 418 participants (Actual)Interventional2015-08-31Completed
A Randomized Controlled Trial of the Effects of Tadalafil and Dexamethasone Versus Placebo on Pulmonary Edema Formation and Cerebral Blood Flow Autoregulation in High Altitude Newcomers With a Previous History of High Altitude Pulmonary Edema [NCT00274430]Phase 1/Phase 230 participants Interventional2003-07-31Completed
Single-center, Open-label, Single-dose, Two-period, Randomized, Crossover, Phase I Study to Demonstrate Bioequivalence Between a Fixed Dose Combination Product Formulation of Macitentan/Tadalafil (10 mg/40 mg) and the Free Combination of 10 mg Macitentan [NCT03215966]Phase 138 participants (Actual)Interventional2017-08-07Completed
A Double-Blind Efficacy and Safety Study of the Phosphodiesterase Type 5 Inhibitor Tadalafil in Pediatric Patients With Pulmonary Arterial Hypertension [NCT01824290]Phase 335 participants (Actual)Interventional2014-02-05Completed
Perfusion by Arterial Spin Labelling Following Single Dose Tadalafil in Small Vessel Disease (PASTIS) Trial [NCT02450253]Phase 255 participants (Actual)Interventional2015-09-30Completed
Evaluation of Retinal and Choriocapillary Vascular Changes Using Optical Coherence Tomography Angiography in Patients Undergoing Tadalafil 20mg on Alternative Days for More Than 6 Months: a Single-centre Prospective-control [NCT04491773]54 participants (Actual)Observational2019-11-01Completed
A Phase 2a, Open-Label, Multi-Center Study to Assess the Efficacy and Safety of Marrow Infiltrating Lymphocytes - Non-Small Cell Lung Cancer (MILs™ - NSCLC) Alone or in Combination With Nivolumab With or Without Tadalafil in Subjects With Locally Advanced [NCT04069936]Phase 219 participants (Actual)Interventional2019-10-15Terminated(stopped due to Resourcing)
Phosphodiesterase-5 Inhibitor (Tadalafil) Two Weeks Administration Period Effects in Left Ventricle Diastolic Dysfunction and BNP Levels in Resistant Hypertensive Patients [NCT01743911]20 participants (Actual)Interventional2010-09-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial of Tadalafil for Duchenne Muscular Dystrophy [NCT01865084]Phase 3331 participants (Actual)Interventional2013-09-30Terminated(stopped due to The study is being terminated for lack of efficacy)
Phase IV Study on New Insights in Remodeling of Diabetic Cardiomyopathy: Gender Difference in Intramyocardial, Molecular and Neuroendocrine Assessment in Response to Chronic Inhibition of Cyclic GMP Phosphodiesterase 5A [NCT01803828]Phase 4120 participants (Actual)Interventional2014-05-31Completed
A Randomized, Open-label, Multiple Dosing, 2-way Crossover Study to Evaluate the Pharmacokinetic Effect of Tamsulosin on Tadalafil in Healthy Male Volunteers [NCT02247518]Phase 116 participants (Actual)Interventional2014-09-30Completed
Effect of Phosphodiesterase-5 Inhibition With Tadalafil on SystEmic Right VEntricular Size and Function - a Multi-center, Double-blind, Randomized, Placebo-controlled Clinical Trial - SERVE Trial [NCT03049540]Phase 3100 participants (Actual)Interventional2017-10-25Completed
Comparative Study Between Tadalafil Versus Tamsulosin as a Medical Expulsive Therapy for Lower Ureteric Stones [NCT04641507]Phase 4166 participants (Actual)Interventional2020-01-01Active, not recruiting
Efficacy of Silodosin, Tadalafil Alone Versus Silodosin Plus Tadalafil as Medical Expulsive Therapy for Lower Ureteric Stones: A Prospective Randomized Placebo Controlled Study [NCT05789732]168 participants (Actual)Interventional2022-03-30Completed
LY2452473 Formulation Exploratory Bioavailability Study [NCT01401543]Phase 124 participants (Actual)Interventional2011-07-31Completed
Multicenter Study of the Efficacy and Safety of Dapoxetine Combined With Tadalafil in Men With Premature Ejaculation and Concomitant Erectile Dysfunction [NCT04361305]Phase 3150 participants (Anticipated)Interventional2020-06-03Not yet recruiting
Effectiveness and Tolerability of the On-demand Use of Combined Dapoxetine With Tadalafil and Combined Dapoxetine With Lidocaine 5% Spray in Treatment of Patients With Lifelong Premature Ejaculation and Non-responding to Dapoxetine Alone. [NCT04703127]Phase 360 participants (Anticipated)Interventional2020-03-30Recruiting
Aortic Stenosis and PhosphodiEsterase iNhibition With Aortic Valve Replacement (ASPEN-AVR): A Pilot Study [NCT01272388]Phase 41 participants (Actual)Interventional2011-01-31Terminated(stopped due to We designed a different pilot trial based on data obtained after this study started - the 2 studies were too overlapping to continue both.)
The Efficacy and Safety of Initial Triple Versus Initial Dual Oral Combination Therapy in Patients With Newly Diagnosed Pulmonary Arterial Hypertension: A Multi-center, Double-blind, Placebo-controlled, Phase 3b Study [NCT02558231]Phase 3247 participants (Actual)Interventional2016-05-01Completed
A Study to Determine the Effect of CYP3A Inhibition on the Pharmacokinetics of LY2623091 and the Effect of LY2623091 on the Pharmacokinetics of CYP3A Substrates in Healthy Subjects [NCT02300259]Phase 148 participants (Actual)Interventional2014-11-30Completed
A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Parallel-Design, Multicenter Study to Evaluate the Efficacy and Safety of Tadalafil Once-Daily Dosing for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia and Erectile Dysfunc [NCT01937871]Phase 3909 participants (Actual)Interventional2013-09-30Completed
Assessment of Serum YKL-40 Level and Platelets Indices Among Patients With Diabetic Erectile Dysfunction [NCT05446493]Phase 460 participants (Actual)Interventional2019-04-01Completed
A Single Dose Randomized Five-Way Crossover Pharmacokinetics (PK) Study of Tadalafil Semi-Chewable (Gummy) Formulations in Healthy Volunteers [NCT04762082]Phase 130 participants (Anticipated)Interventional2023-09-01Not yet recruiting
A Post-Marketing Clinical Study of LY450190 (Combined With Alpha1 Blocker Treatment) [NCT02431754]Phase 4171 participants (Actual)Interventional2015-04-30Completed
A Multiple Ascending Dose Study of Tadalafil to Assess the Pharmacokinetics and Safety in a Pediatric Population With Pulmonary Arterial Hypertension [NCT01484431]Phase 1/Phase 220 participants (Actual)Interventional2012-07-17Completed
Randomized, Double-blind, Two-arms Study With Parallel Groups to Determine the Effect of a Phosphodiesterase Inhibitor for 14 Weeks of Treatment Versus Placebo in Women With FSIAD. [NCT04433559]Phase 380 participants (Anticipated)Interventional2020-08-31Not yet recruiting
Medication Facilitated Ureteral Access Sheath Deployment During Ureteroscopy and Endoscopic-Guided Percutaneous Nephrolithotomy: A Randomized Double-Blind Placebo Controlled Trial of Tadalafil, Tamsulosin and Combination [NCT03229889]Phase 4220 participants (Anticipated)Interventional2017-06-07Enrolling by invitation
Efficacy of Tadalafil and Solifenacin Versus Tamsulosin and Solifenacin Combination Therapy for the Treatment of Benign Prostatic Hyperplasia With Overactive Bladder: A Randomized Controlled Trial [NCT05494567]Phase 460 participants (Anticipated)Interventional2021-11-08Active, not recruiting
Hookah Smoking, Carbon Monoxide, and Coronary Endothelial Function [NCT03166787]Phase 160 participants (Actual)Interventional2017-08-15Terminated(stopped due to Due to the Pandemic and the nature of this study we decided to terminate this study.)
The Effect of Sildenafil and Tadalafil on Skeletal Muscle and Perceptual Fatigue. [NCT01661595]30 participants (Actual)Interventional2012-11-30Completed
Endocan Level in Patients With Erectile Dysfunction and Relationship With Tadalafil Treatment [NCT05109377]90 participants (Anticipated)Interventional2021-06-24Recruiting
Administration of an Oral PDE5 Inhibitor, Tadalafil in Conjunction With Lenalidomide and Dexamethasone in Patients With Multiple Myeloma [NCT01374217]Phase 214 participants (Actual)Interventional2012-04-30Terminated(stopped due to early stopping rule)
Population Pharmacokinetics and Dosage Individualization of Bosentan, Sildenafil and Tadalafil in Persistent Pulmonary Hypertension of the Newborn [NCT04379180]500 participants (Anticipated)Observational2020-04-26Not yet recruiting
Comparison Between Tamsulosin and Tadalafil in Management of Benign Prostatic Hyperplasia A Randomised Trial [NCT05818670]Phase 4160 participants (Actual)Interventional2020-11-11Completed
Daily Oral L-arginine Plus Tadalafil in Diabetic Patients With Erectile Dysfunction: A Double-blinded Randomized Controlled Clinical Trial [NCT03834610]108 participants (Actual)Interventional2017-10-01Completed
A Phase IB Study to Use Tadalafil to Overcome Immunosuppression During Chemoradiotherapy for IDH-wildtype Grade III-IV Astrocytoma [NCT04757662]Phase 118 participants (Actual)Interventional2021-05-14Completed
A Randomized, Open-label, Multiple Dosing, 2-way Crossover Study to Evaluate the Pharmacokinetic Effect of Tadalafil on Tamsulosin in Healthy Male Volunteers [NCT02247505]Phase 129 participants (Actual)Interventional2014-09-30Completed
Comparative Study Between Fixed Dose Monotherapy (Phosphodiesterase 5 Inhibitors or Alpha Blockers) Versus Combined Therapy in Benign Prostatic Hyperplasia Patients With Lower Urinary Tract Symptoms [NCT05236634]120 participants (Anticipated)Interventional2022-05-01Not yet recruiting
Phosphodiesterase Type 5 Inhibition With Tadalafil Changes Outcomes in Heart Failure [NCT01910389]Phase 323 participants (Actual)Interventional2013-11-30Terminated(stopped due to terminated by funding agency)
Tadalafil for Pulmonary Hypertension Associated With Chronic Lung Disease [NCT01862536]Phase 244 participants (Actual)Interventional2013-10-01Completed
Define in Preclinical Systolic Dysfunction (PSD) With Renal Dysfunction, the Cardiorenal and Humoral Actions of Chronic Type V Phosphodiesterase (PDEV) Inhibition [NCT01970176]Phase 1/Phase 220 participants (Actual)Interventional2014-01-09Completed
An Evaluation of Tadalafil and Sildenafil Treatment in Men With Erectile Dysfunction in China [NCT01352507]Phase 4383 participants (Actual)Interventional2011-06-30Completed
Effects of Single Dose Tadalafil on Urethral and Anal Closure Function and on Urinary Flow in Healthy Females: A Randomised, Controlled, Double-blinded, Two-period Cross-over Study [NCT05095077]Phase 124 participants (Actual)Interventional2021-08-01Completed
Postmarketing Surveillance Study: A Randomized, Open-Label, 3-Month Interventional Study of Tadalafil Effectiveness (2.5 mg and 5 mg) and Long-Term Safety Administered Once Daily in Chinese Men With Erectile Dysfunction [NCT02224846]Phase 4635 participants (Actual)Interventional2014-10-31Completed
A Single-center, Open-label, Single-dose, Randomized, 3-way Crossover Phase 1 Study in Healthy Adult Participants to Assess the Bioequivalence of the Combination of Macitentan/Tadalafil (10 mg/20 mg) Administered as a Fixed Dose Combination Formulation Co [NCT05236231]Phase 140 participants (Actual)Interventional2022-02-04Completed
A Multicenter Observational Pilot Study on the Use of Tadalafil Delivra Cream in the Treatment of Raynaud's Phenomenon and Pain Associated With Digital Ulcers [NCT03393325]0 participants (Actual)Observational2018-10-31Withdrawn(stopped due to Sponsor decision. The study is not anticipated to start)
Aortic Stenosis and PhosphodiEsterase Type 5 iNhibition (ASPEN): A Pilot Study [NCT01275339]Phase 410 participants (Actual)Interventional2012-12-31Terminated(stopped due to Difficulty enrolling patients and PI moved institutions.)
A Randomized, Placebo-Controlled, Double-Blinded, Parallel, Phase 2a Study to Evaluate the Safety and Efficacy of LY2623091 in Patients With Primary Hypertension [NCT02194465]Phase 2304 participants (Actual)Interventional2014-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00384930 (10) [back to overview]Change From Baseline to Week 12 in International Prostate Symptom Score (IPSS): Supportive Analysis
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Benign Prostatic Hyperplasia Impact Index (BII)
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF) EF Domain
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) (Irritative) Subscore
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Question 7 (Nocturia)
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS): Primary Analysis
NCT00384930 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Peak Urinary Flow
NCT00384930 (10) [back to overview]"Number of Participants Who Answer Yes to the Lower Urinary Tract Symptoms (LUTS) Global Assessment Question (LUTS-GAQ)"
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Postvoid Residual Volume (PVRcath) Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Clinically Adverse and Statistically Significant Changes From Baseline to 12 Week Endpoint in Laboratory Tests
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Bladder Contractility Index (BCI) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Bladder Outlet Obstruction Index (BOOI) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Bladder Voiding Efficiency (BVE) Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Bladder Volume at First Involuntary Detrusor Contraction
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Detrusor Pressure at Peak Urinary Flow Rate (PdetQmax)
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Total Score
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Maximum Detrusor Pressure (Max Pdet) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Mean Urinary Flow Rate (Qave) Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Mean Urinary Flow Rate (Qave) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Peak Urinary Flow Rate (Qmax) Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Peak Urinary Flow Rate (Qmax) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Total Bladder Capacity Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Volume of Voided Urine (Vcomp) Measured During Free-Flow Studies
NCT00386009 (17) [back to overview]Change From Baseline to 12 Week Endpoint in Volume of Voided Urine (Vcomp) Measured During Pressure-Flow Studies
NCT00386009 (17) [back to overview]Presence of Involuntary Detrusor Contractions During Bladder Filling
NCT00422734 (14) [back to overview]Improvement in the Sexual Quality of Life in the Subject and His Study Partner as Measured by the Sexual Quality of Life (SQoL) Domain of the Sexual Life Quality Questionnaire (SLQQ)
NCT00422734 (14) [back to overview]Sexual Life Quality Questionnaire (SLQQ) Treatment Satisfaction Domain
NCT00422734 (14) [back to overview]"Percent of Subjects With Yes Responses to Global Assessment Questionnaire (GAQ) - Subject Response"
NCT00422734 (14) [back to overview]"Percent of Partners With Yes Responses to Global Assessment Questionnaire (GAQ) - Partner Response"
NCT00422734 (14) [back to overview]"Change From Baseline to Endpoint in the Percent of Yes Responses to Sexual Encounter Profile (SEP) Diary Questions 2 (SEP2) and 3 (SEP3)."
NCT00422734 (14) [back to overview]"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Partner-Sexual Encounter Profile (SEP) Questions 1 and 2 - Partner Response"
NCT00422734 (14) [back to overview]Change From Baseline to Week 12 Endpoint in the International Index of Erectile Function - Intercourse Satisfaction Domain - Subject Response
NCT00422734 (14) [back to overview]"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Sexual Encounter Profile (SEP) Questions 4 and 5 - Subject Response"
NCT00422734 (14) [back to overview]Change From Baseline to Endpoint in the International Index of Erectile Function (IIEF)- Erectile Function Domain Score (Sum of IIEF Questions 1-5 and 15)
NCT00422734 (14) [back to overview]Change From Baseline to 12 Week Endpoint in the Satisfaction Domain of the Female Sexual Function Index (FSFI) - Partner Response
NCT00422734 (14) [back to overview]Change From Baseline to 12 Week Endpoint in Overall Satisfaction Domain of the International Index of Erectile Function (IIEF-OS) - Subject Response
NCT00422734 (14) [back to overview]"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Partner-Sexual Encounter Profile (SEP) Question 3 - Partner Response"
NCT00422734 (14) [back to overview]Change From Baseline to 12 Week Endpoint in the Self-Esteem and Relationship (SEAR) Questionnaire
NCT00422734 (14) [back to overview]Change From Baseline to 12 Week Endpoint in the Self-Esteem and Relationship (SEAR) Questionnaire - Confidence Domain Subscales
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Uroflowmetry Parameters - Peak Urine Flow Rate (Qmax) and Mean Urine Flow Rate (Qmean)
NCT00540124 (13) [back to overview]Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Nocturia Subscore
NCT00540124 (13) [back to overview]Clinician Global Impression of Improvement (CGI-I) Combined Categories - Frequencies
NCT00540124 (13) [back to overview]Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Obstructive Subscore
NCT00540124 (13) [back to overview]Patient Global Impression of Improvement (PGI-I) Combined Categories - Frequencies
NCT00540124 (13) [back to overview]Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Irritative Subscore
NCT00540124 (13) [back to overview]Change From Baseline to 4 Week and 8 Week Endpoints in International Prostate Symptom Score (IPSS) Total Score
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Voids With Terminal Micturition Dribble and Post Micturition Dribble Per Week Based on Median as Reported by Patient Voiding Dribble Diary
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Uroflowmetry Parameters - Voided Urine Volume (Vcomp)
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Total, Waking, and Sleeping Voids (Average Number Per Week) Based on Median as Reported in Patient Voiding Dribble Diary
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Total Urinary Incontinence Episodes Per Week Based on Median as Reported in Patient Voiding Dribble Diary
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Total Score
NCT00540124 (13) [back to overview]Change From Baseline to 12 Week Endpoint in Benign Prostatic Hyperplasia Impact Index (BPH-II)
NCT00549302 (4) [back to overview]Probability of No Pulmonary Arterial Hypertension (PAH) Deterioration at Weeks 16, 28, 40 and up to 52
NCT00549302 (4) [back to overview]Number of Participants With Adverse Events (AEs)
NCT00549302 (4) [back to overview]6-Minute Walk Distance (6MWD) at Baseline and Weeks 16, 28, 40 and 52
NCT00549302 (4) [back to overview]Borg Dyspnea Assessment at Baseline and Weeks 16, 28, 40 and 52
NCT00617305 (11) [back to overview]Change From Baseline in Log-transformed N-terminal Pro-B-type Natriuretic Peptide (NT-proBNP) Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in Mean Pulmonary Artery Pressure (mPAP) (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in Mean Right Atrial Pressure (mRAP) (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in Pulmonary Vascular Resistance (PVR), Last Observation Carried Forward (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in Six Minute Walk Distance (6MWD) Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)
NCT00617305 (11) [back to overview]Overall Survival, Evaluated at Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, and After Week 48
NCT00617305 (11) [back to overview]Time to Clinical Worsening of PAH, Evaluated at Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, and After Week 48
NCT00617305 (11) [back to overview]Change From Baseline in Cardiac Output (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in the Cambridge Pulmonary Hypertension Outcome Review (CAMPHOR) Quality of Life (QOL) Survey Overall Score Measured at Weeks 12, 24, 36 and 48 (LOCF)
NCT00617305 (11) [back to overview]Change From Baseline in World Health Organization (WHO) Functional Class (LOCF) Measured at Weeks 4, 12, 24, 36 and 48.
NCT00617305 (11) [back to overview]Change in Dyspnea Index Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Intercourse Satisfaction (IS) Domain of the IIEF
NCT00734604 (15) [back to overview]"Question 4 I Felt Like a Whole Man Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"
NCT00734604 (15) [back to overview]"Question 2 I Felt in Control of my Sex Life Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Overall Satisfaction (OS) Domain of the IIEF
NCT00734604 (15) [back to overview]Change From Baseline Between Tadalafil Once a Day (OaD) and Tadalafil as Needed (PRN) in Sexual Self-Confidence Domain of Psychological and Interpersonal Relationship Scales (PAIRS)
NCT00734604 (15) [back to overview]Change From Baseline Between Tadalafil Once a Day (OaD) and Sildenafil as Needed (PRN) in Sexual Self-Confidence Domain of Psychological and Interpersonal Relationship Scales (PAIRS)
NCT00734604 (15) [back to overview]Number of Participants With at Least One Serious Adverse Event
NCT00734604 (15) [back to overview]"Question 3 I Felt the Drug Was in Control of my Erections Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Time Concerns Domain of PAIRS
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Erectile Function Domain of the International Index of Erectile Function (IIEF)
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Spontaneity Domain of PAIRS
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Self-Esteem And Relationship (SEAR) Questionnaire Transformed Total Score
NCT00734604 (15) [back to overview]Change From Baseline to Endpoint in the Proportion of Days With at Least One Morning Erection
NCT00734604 (15) [back to overview]Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Score at Endpoint
NCT00734604 (15) [back to overview]"Question 1 I Felt as if I Did Not Have ED Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"
NCT00750308 (2) [back to overview]Beta Cell Function
NCT00750308 (2) [back to overview]Insulin Sensitivity
NCT00783094 (23) [back to overview]Change From Baseline in Postvoid Residual Volume (PVR) at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Postvoid Residual Volume (PVR) at 12-Week Endpoint
NCT00783094 (23) [back to overview]Tadalafil Pharmacokinetics in Japanese Men: Plasma Concentration Measurement
NCT00783094 (23) [back to overview]Number of Participants With Adverse Events During 42 Weeks of Open-Label Treatment
NCT00783094 (23) [back to overview]Number of Participants With Adverse Events During 12 Weeks of the Study
NCT00783094 (23) [back to overview]Change From Baseline in Blood Pressure During at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Blood Pressure at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in the International Prostate Symptom Score (IPSS) Total Score at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Sitting Heart Rate at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Overactive Bladder Symptom Score (OABSS) at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in IPSS Quality of Life (QoL) Index at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in IPSS Quality of Life (QoL) Index at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Total Score at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Overactive Bladder Symptom Score (OABSS) at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Sitting Heart Rate at 12-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Prostate Specific Antigen (PSA) at 54-Week Endpoint
NCT00783094 (23) [back to overview]Change From Baseline in Prostate Specific Antigen (PSA) at 12-Week Endpoint
NCT00822354 (6) [back to overview]Raynaud's Condition Score (RCS) Visual Analog Scale (VAS)
NCT00822354 (6) [back to overview]Raynaud Severity Visual Analog Score (VAS)
NCT00822354 (6) [back to overview]Number of Raynaud's Phenomenon Attacks Per Day
NCT00822354 (6) [back to overview]Duration of Raynaud's Phenomenon Attacks
NCT00822354 (6) [back to overview]Digital Blood Pressure
NCT00822354 (6) [back to overview]Capillary Diameter
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Index of Erectile Function (IIEF)- Erectile Function (EF) Domain Scores
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, Postvoid Residual (PVR) Volume
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, Peak Flow Rate (Qmax) by Uroflowmetry
NCT00827242 (16) [back to overview]Clinical Global Impression of Improvement (CGI-I), Number of Participants in 7 Response Categories
NCT00827242 (16) [back to overview]Patient Global Impression of Improvement (PGI-I), Number of Participants in 7 Response Categories
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS)
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Nocturia Question
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, Mean Flow Rate (Qmean) by Uroflowmetry
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, Benign Prostatic Hyperplasia (BPH) Impact Index
NCT00827242 (16) [back to overview]Change From Baseline to 12 Weeks, Voided Volume (Vcomp) by Uroflowmetry
NCT00827242 (16) [back to overview]Change From Baseline to 4 Weeks, Benign Prostatic Hyperplasia (BPH) Impact Index
NCT00827242 (16) [back to overview]Change From Baseline to 4 Weeks, International Prostate Symptom Score (IPSS)
NCT00827242 (16) [back to overview]Change From Baseline to 1 Week, International Prostate Symptom Score (IPSS)
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question Number 1, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question Number 2, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question Number 3, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question Number 4, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses
NCT00833638 (12) [back to overview]Earliest Onset Day Measured by Cumulative Percentage of Participants With Yes Response to Sexual Encounter Profile Diary Question 3
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, Daily Cumulative Percentage of Successful Intercourse Attempts
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question Number 5, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses in the Double-blind Period and the Open-label Period for Participants Who Were Assigned to Tadalafil 5 mg in the Double-blind Treatment Period
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses in the Double-blind Period and the Open-label Period for Participants Who Were Assigned to Tadalafil 2.5 mg in the Double-blind Treatment Period
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses During the Double-blind and Open-label Periods for Participants Who Were Assigned to Placebo in the Double-blind Treatment Period
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses During the Double-blind Period and the Open-label Period for Participants Who Didn't Respond to Tadalafil 2.5 mg During Double-blind Period
NCT00833638 (12) [back to overview]Sexual Encounter Profile Diary Question 3, the Overall Distribution of Time to Onset by Yes Responses
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in Total and Subdomain Scores of the Self-Esteem and Relationship (SEAR) Questionnaire
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Percentage Volumetric Change
NCT00836693 (18) [back to overview]The Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire at 12 Week Endpoint
NCT00836693 (18) [back to overview]"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 1 Percentage of Yes Responses"
NCT00836693 (18) [back to overview]"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 4 Percentage of Yes Responses"
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in the Frequency of Spontaneous Morning Erections Captured by Patient Diary
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Number of Erectile Events Per Night
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Duration of Erectile Events Per Night
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Sexual Desire (SD)
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Overall Satisfaction (OS)
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Orgasmic Functions (OF)
NCT00836693 (18) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Intercourse Satisfaction (IS)
NCT00836693 (18) [back to overview]Change From Baseline in the International Index of Erectile Function - Erectile Function Domain (IIEF-EF) at Week 12
NCT00836693 (18) [back to overview]Change From Baseline in Question 2 of the Patient Sexual Encounter Profile (SEP) Diary at Week 12 in Percentage of Yes Responses
NCT00836693 (18) [back to overview]Sexual Encounter Profile (SEP) Diary, Question 3 Change From Baseline to Week 12 in Percentage of Yes Responses
NCT00836693 (18) [back to overview]"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 5 Percentage of Yes Responses"
NCT00836693 (18) [back to overview]Global Assessment Question (GAQ) Question 2 at 12 Week Endpoint
NCT00836693 (18) [back to overview]Global Assessment Question (GAQ) Question 1 at 12 Week Endpoint
NCT00843635 (4) [back to overview]Number of Participants Experiencing Adverse Events
NCT00843635 (4) [back to overview]Ratio of MDSC Concentration in the Blood
NCT00843635 (4) [back to overview]Ratio of T-reg Cell Concentration in the Blood
NCT00843635 (4) [back to overview]Ratio of Tumor-specific T-cell Concentration in the Blood
NCT00848081 (5) [back to overview]International Prostate Symptom Score (IPSS) Change From Baseline
NCT00848081 (5) [back to overview]Number of Participants With Positive Orthostatic Vital Signs Test; Shift From Any Pre-Randomization to Any Post-Randomization Visit
NCT00848081 (5) [back to overview]Postvoid Residual Volume (PVR) Change From Baseline
NCT00848081 (5) [back to overview]Uroflowmetry (Qmax) Change From Baseline
NCT00848081 (5) [back to overview]Number of Men With Treatment-emergent Dizziness
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function - Overall Satisfaction Domain at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Prostate Symptom Score Nocturia Question at Week 12
NCT00855582 (30) [back to overview]Change From Baseline in Uroflowmetry Parameters - Peak Urine Flow Rate (Qmax) at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function Question 3 at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function - Intercourse Satisfaction Domain at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score at Week 12 Endpoint (5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 5
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 4 at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function Question 4 at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 12 Endpoint (5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 2 at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in Uroflowmetry Parameters - Voided Volume (Vcomp) at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score at Week 12 Endpoint (2.5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in BPH Impact Index (BII) at Week 12 Endpoint (2.5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Benign Prostatic Hyperplasia (BPH) Impact Index (BII) at Week 12 Endpoint (5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 12 Endpoint (2.5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain at Week 4 and Week 8 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in Uroflowmetry Parameters - Mean Urine Flow Rate (Qmean) at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12 Endpoint (5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12 Endpoint (2.5 mg)
NCT00855582 (30) [back to overview]Change From Baseline in Modified IPSS (mIPSS) at Week 2 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Prostate Symptom Score Voiding (Obstructive) Subscore at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Prostate Symptom Score Storage (Irritative) Subscore at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Prostate Symptom Score Quality of Life (QoL) at Week 12 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in BPH Impact Index (BII) at Week 4 and 8 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) at Week 4 and Week 8 Endpoint
NCT00855582 (30) [back to overview]Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 4 and Week 8 Endpoint
NCT00855582 (30) [back to overview]Clinician Global Impression of Improvement (CGI-I) at Week 12 Endpoint
NCT00855582 (30) [back to overview]Erectile Function General Assessment Questionnaire (EF-GAQ)
NCT00855582 (30) [back to overview]Patient Global Impression of Improvement (PGI-I) at Week 12 Endpoint
NCT00861757 (12) [back to overview]Change From Baseline to 12 Weeks in International Prostate Symptom Score (IPSS) Subscore (Storage [Irritative] and Voiding [Obstructive])
NCT00861757 (12) [back to overview]Clinician Global Impression of Improvement (CGI-I) at Week 12
NCT00861757 (12) [back to overview]Patient Global Impression of Improvement (PGI-I) at Week 12
NCT00861757 (12) [back to overview]Change From Baseline in Benign Prostatic Hyperplasia (PBH) Impact Index (BII) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Blood Pressure (Sitting) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Quality of Life (QoL) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Postvoid Residual Volume (PVR) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Prostate Specific Antigen (PSA) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Sitting Heart Rate (HR) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 12 Weeks
NCT00861757 (12) [back to overview]Change From Baseline in Blood Pressure (Standing) at 12 Weeks
NCT00894413 (1) [back to overview]Change in Immune Response After Tadalafil Administration
NCT00931528 (7) [back to overview]Overall Sexual Function as Measured by Change From Baseline in the International Index of Erectile Function (IIEF)
NCT00931528 (7) [back to overview]Partner Marital Adjustment as Measured by the Locke's Marital Adjustment Test
NCT00931528 (7) [back to overview]Percentage of Patients Maintaining Spontaneous (Off-drug) Erectile Function (EF) at Weeks 28-30 After Initiation of Radiation Therapy (RT)
NCT00931528 (7) [back to overview]Patient Marital Adjustment as Measured by the Locke's Marital Adjustment Test
NCT00931528 (7) [back to overview]Percentage of Patients Maintaining Spontaneous (Off-drug) EF at Years 1 and 2 After Initiation of RT
NCT00931528 (7) [back to overview]Overall Patient Sexual Satisfaction as Measured by Change From Baseline in the Sexual Adjustment Questionnaire (SAQ) Score
NCT00931528 (7) [back to overview]Overall Partner Sexual Satisfaction as Measured by Change From Baseline in the Sexual Adjustment Questionnaire-Partner (SAQ-P) Score
NCT00970632 (17) [back to overview]Change From Baseline in Modified International Prostate Symptom Score (mIPSS) at 1 Week
NCT00970632 (17) [back to overview]Change From Baseline in Peak Urine Flow Rate (Q-Max) at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Postvoid Residual Volume (PVR) at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Total International Prostate Symptom Score (IPSS) at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Total International Prostate Symptom Score (IPSS) at 4 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Volume of Voided Urine (V-Comp) at 12 Weeks
NCT00970632 (17) [back to overview]Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 12 Weeks: Overall
NCT00970632 (17) [back to overview]Clinician Global Impression of Improvement (CGI-I) at 12 Weeks
NCT00970632 (17) [back to overview]Patient Global Impression of Improvement (PGI-I) at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Benign Prostatic Hyperplasia Impact Index (BII) at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Nocturia Question at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 12 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in Benign Prostatic Hyperplasia Impact Index (BII) at 4 Weeks
NCT00970632 (17) [back to overview]Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 12 Weeks.
NCT00970632 (17) [back to overview]Change From Baseline in Mean Urine Flow Rate (Q-Mean) at 12 Weeks
NCT01026818 (23) [back to overview]Change From Baseline in 'Yes' Answers to Morning Erections
NCT01026818 (23) [back to overview]Percentage of Participants With a Score of Greater Than or Equal to 22 in the International Index of Erectile Function- Erectile Function (IIEF-EF) Domain
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Month 10.5
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Month 13.5
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Month 2
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Month 5
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Month 9
NCT01026818 (23) [back to overview]Standardized Morning Erections Question (SMEQ) Score at Month 13.5
NCT01026818 (23) [back to overview]Standardized Morning Erections Question (SMEQ) Score at Month 2
NCT01026818 (23) [back to overview]Standardized Morning Erections Question (SMEQ) Score at Month 9
NCT01026818 (23) [back to overview]Residual Erectile Function (REF) at Baseline
NCT01026818 (23) [back to overview]Global Assessment Questions (GAQ) Question 1 at Month 9
NCT01026818 (23) [back to overview]Global Assessment Question (GAQ) Question 2 at Month 9
NCT01026818 (23) [back to overview]Global Assessment Question (GAQ) Question 2 at Month 13.5
NCT01026818 (23) [back to overview]Global Assessment Question (GAQ) Question 1 at Month 13.5
NCT01026818 (23) [back to overview]Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire Mean Score
NCT01026818 (23) [back to overview]Change in Penile Length and Girth
NCT01026818 (23) [back to overview]Change From Baseline to Endpoint in the International Index of Erectile Function- Erectile Function (IIEF-EF) Total Score
NCT01026818 (23) [back to overview]Change From Baseline to Endpoint in the International Index of Erectile Function (IIEF) Domains (Intercourse Satisfaction Domain, Orgasmic Function Domain, Sexual Desire Domain, Overall Satisfaction Domain)
NCT01026818 (23) [back to overview]Change From Baseline in Self Esteem and Relationship (SEAR) Questionnaire Score
NCT01026818 (23) [back to overview]Change From Baseline in 26-item Expanded Prostate Cancer Index Composite (EPIC-26) Questionnaire Score
NCT01026818 (23) [back to overview]Change From Baseline in 'Yes' Answers to Questions 1 to 5 of the Sexual Encounter Profile (SEP)
NCT01026818 (23) [back to overview]Percentage of Participants With a Score of Greater Than or Equal to 22 in the Erectile Function (EF) Domain of the International Index of Erectile Function (IIEF) Questionnaire
NCT01042158 (4) [back to overview]6-minute Walk Distance
NCT01042158 (4) [back to overview]Pulmonary Vascular Resistance (PVR)
NCT01042158 (4) [back to overview]Right Ventricular (RV) Mass
NCT01042158 (4) [back to overview]Tricuspid Annular Plane Systolic Excursion (TAPSE)
NCT01122264 (18) [back to overview]Reasons for Discontinuation of Randomized Erectile Dysfunction Treatment
NCT01122264 (18) [back to overview]Patterns of Erectile Dysfunction Treatment Change
NCT01122264 (18) [back to overview]Global Assessment Questions (GAQ)
NCT01122264 (18) [back to overview]Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire at 4, 8, 16, and 24 Weeks
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16, and 24 Weeks of the Sexual Relationship Domain of the Self-Esteem and Relationship (SEAR) Questionnaire
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16, and 24 Weeks of the Self Esteem Domain of the Self-Esteem and Relationship (SEAR) Questionnaire
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16, and 24 Weeks of the Overall Relationship Domain of the Self-Esteem and Relationship (SEAR) Questionnaire
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the Sexual Encounter Profile (SEP)
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Sexual Desire Domain
NCT01122264 (18) [back to overview]Time to Discontinuation of Randomized Treatment
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Overall Satisfaction Domain
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Orgasmic Function Domain
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16, and 24 Weeks of the Confidence Domain of the Self-Esteem and Relationship (SEAR) Questionnaire
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Intercourse Satisfaction Domain
NCT01122264 (18) [back to overview]Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Erectile Function (EF) Domain
NCT01122264 (18) [back to overview]Change From Baseline to 24 Week Endpoint of the Sexual Self-Confidence, Spontaneity, and Time Concerns Domains (23-items) of the Psychological and Interpersonal Relationships Scale (PAIRS)
NCT01122264 (18) [back to overview]Number of Days From the 8-Week Study Visit to the Time the Participant Discontinues From All Phosphodiesterase Type 5 (PDE5) Inhibitor Treatments
NCT01122264 (18) [back to overview]Number of Treatment Switches
NCT01130532 (13) [back to overview]Treatment Satisfaction Scale (TSS) - Partner Satisfaction With Medication Score at Week 12 Endpoint
NCT01130532 (13) [back to overview]Treatment Satisfaction Scale (TSS) - Patient Satisfaction With Medication Score at Week 12 Endpoint
NCT01130532 (13) [back to overview]"Change From Baseline to 12-Week in Percentage of Yes Responses to Sexual Encounter Profile (SEP) Questions 1-5"
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score
NCT01130532 (13) [back to overview]Change From 12 Weeks to 16 Weeks in Participant's International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in Treatment Satisfaction Scale (TSS) - Partner
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in Treatment Satisfaction Scale (TSS) - Patient
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Intercourse Satisfaction (IIEF-IS) Domain Score
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Overall Satisfaction (IIEF-OS) Domain Score
NCT01130532 (13) [back to overview]Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function (IIEF) Question 15 (Sexual Confidence)
NCT01130532 (13) [back to overview]Percentage of Participants Having an International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score Greater Than or Equal to 26 Through 12-Week Endpoint (Double-Blind Treatment Period)
NCT01130532 (13) [back to overview]Percentage of Participants Having International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score Greater Than or Equal to 26 From 12 to 16 Weeks
NCT01130532 (13) [back to overview]"Change From Week 12 to Week 16 Percentage of Yes Responses to Sexual Encounter Profile (SEP) Questions 3"
NCT01131104 (1) [back to overview]30-Day Person Time Analysis Risk of NAION Associated With PDE5 Inhibitor Use
NCT01139762 (14) [back to overview]Patient Global Impression of Improvement (PGI-I) at 26 Weeks
NCT01139762 (14) [back to overview]Clinician Global Impression of Improvement (CGI-I) at 26 Weeks
NCT01139762 (14) [back to overview]Change in Total International Prostate Symptom Score (IPSS) From Baseline to 4 and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Prostate Symptom Score (IPSS) Subscores Index From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Prostate Symptom Score (IPSS) Quality of Life Index From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) Question 3 and 4 Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Sexual Desire Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Overall Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Orgasmic Function Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Intercourse Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Erectile Function Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 26 Weeks
NCT01139762 (14) [back to overview]Change in Post Void Residual (PVR) Volume From Baseline to 26 Weeks
NCT01139762 (14) [back to overview]Change in Total International Prostate Symptom Score (IPSS) From Baseline to 12 Weeks
NCT01152190 (4) [back to overview]Change From Baseline to 4 and 8 Weeks in Arterial Resistive Index (RI) in the Prostate Peripheral Zone and Bladder Neck
NCT01152190 (4) [back to overview]Change From Baseline to 8-Week Endpoint in Arterial Resistive Index (RI) in the Prostate Transition Zone
NCT01152190 (4) [back to overview]Change From Baseline to 4-Week Endpoint in Arterial Resistive Index (RI) in the Prostate Transition Zone
NCT01152190 (4) [back to overview]Change From Baseline to 4 and 8 Weeks in Color Pixel Intensity (CPI) in the Prostate Transition Zone, Peripheral Zone, and Bladder Neck
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Total Cholesterol and Triglycerides
NCT01160289 (10) [back to overview]Percent Change From Baseline to 12 Week Endpoint in High-Density Lipoprotein Cholesterol (HDL-C) and Low-Density Lipoprotein Cholesterol (LDL-C)
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in IIEF EF Domain Score Reported by Testosterone Concentration Subgroups
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in IIEF Domain Scores (Intercourse Satisfaction, Orgasmic Function, Sexual Desire, and Overall Satisfaction)
NCT01160289 (10) [back to overview]"Change From Baseline to 12 Week Endpoint in the Percentage of Yes Responses on the Sexual Encounter Profile (SEP) Diary"
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Prostate-Specific Antigen (PSA)
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Insulin
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain Score
NCT01160289 (10) [back to overview]25)"-NCT01160289">"Change From Baseline to 12 Week Endpoint in the Percentage of Participants Who Return to Normal on the International Index of Erectile Function (IIEF) Scale (EF>25)"
NCT01160289 (10) [back to overview]Change From Baseline to 12 Week Endpoint in Fasting Glucose
NCT01178073 (6) [back to overview]Change From Baseline in Borg Dyspnea Index at Week 24
NCT01178073 (6) [back to overview]Number of Participants With First Adjudicated Clinical Failure (CF) Event, Death, Hospitalisation for Worsening PAH, Disease Progression, Unsatisfactory Long-term Clinical Response, All Through FAV
NCT01178073 (6) [back to overview]Percentage of Participants With a Satisfactory Clinical Response at Week 24
NCT01178073 (6) [back to overview]Change From Baseline in the 6 Minute Walk Distance Test at Week 24
NCT01178073 (6) [back to overview]Change From Baseline in the World Health Organization Functional Class at Week 24
NCT01178073 (6) [back to overview]Percent Change From Baseline in the N-Terminal Pro-B-Type Natriuretic Peptide at Week 24
NCT01183650 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) for Tadalafil and Metabolite IC710
NCT01183650 (3) [back to overview]Pharmacokinetics: Concentration Maximum (Cmax) of Tadalafil and Metabolite IC710
NCT01183650 (3) [back to overview]Pharmacokinetics: Time to Concentration Maximum (Tmax) of Tadalafil and Metabolite IC710
NCT01266265 (1) [back to overview]Prevalence of Respiratory Tract-Related Adverse Events of Interest
NCT01272388 (2) [back to overview]6 Minute Walk Distance
NCT01272388 (2) [back to overview]Quality of Life as Assessed by the Kansas City Cardiomyopathy Questionnaire (KCCQ)
NCT01275339 (1) [back to overview]Diastolic Function as Measured by Tissue Doppler e'
NCT01305252 (5) [back to overview]Change in NYHA/WHO Class
NCT01305252 (5) [back to overview]Change in Right Ventricular Ejection Fraction
NCT01305252 (5) [back to overview]N-terminal Pro B-type Natriuretic Peptide (NT-proBNP)
NCT01305252 (5) [back to overview]B-type Natriuretic Peptide (BNP)
NCT01305252 (5) [back to overview]6 Minute Walk Distance
NCT01324999 (8) [back to overview]Short Form-36 Global Score
NCT01324999 (8) [back to overview]Resting Oxygen Saturation
NCT01324999 (8) [back to overview]Oxygen Desaturation During 6 Minute Walk Test
NCT01324999 (8) [back to overview]Number of Participants With Change in WHO Functional Class (WHO FC)
NCT01324999 (8) [back to overview]Maximum Borg Dyspnea Score During 6 Minute Walk Test
NCT01324999 (8) [back to overview]Brain Natriuretic Peptide Level
NCT01324999 (8) [back to overview]St. George's Respiratory Questionnaire (SGRQ) Score
NCT01324999 (8) [back to overview]6 Minute Walk Distance
NCT01352507 (13) [back to overview]Change in PAIRS Spontaneity Domain
NCT01352507 (13) [back to overview]Change in International Index of Erectile Function (IIEF) Erectile Function Domain
NCT01352507 (13) [back to overview]Change in International Index of Erectile Function (IIEF) Intercourse Satisfaction Domain
NCT01352507 (13) [back to overview]Change in International Index of Erectile Function (IIEF) Orgasmic Function Domain
NCT01352507 (13) [back to overview]Change in International Index of Erectile Function (IIEF) Overall Satisfaction Domain
NCT01352507 (13) [back to overview]Change in International Index of Erectile Function (IIEF) Sexual Desire Domain
NCT01352507 (13) [back to overview]"Percentage of Participants Preferring Tadalafil Over Sildenafil Measured at Week 18 Using Question 1 of the Phosphodiesterase 5 Inhibitor Treatment Preference Questionnaire (PITPQ)"
NCT01352507 (13) [back to overview]Change in PAIRS Time Concerns Domain
NCT01352507 (13) [back to overview]Change in Psychosocial and Interpersonal Relationship Scale (PAIRS) Sexual Self-Confidence Domain
NCT01352507 (13) [back to overview]Change in Sexual Encounter Profile (SEP) Question 2
NCT01352507 (13) [back to overview]Change in Sexual Encounter Profile (SEP) Question 3
NCT01352507 (13) [back to overview]Drug Attributes Questionnaire (DRAQ) at Week 18
NCT01352507 (13) [back to overview]Percentage of Participants Moderately or Strongly Preferring the Selected Treatment at Week 18 Using Question 2 of the PITPQ
NCT01374217 (4) [back to overview]Duration of Response
NCT01374217 (4) [back to overview]Response Rate
NCT01374217 (4) [back to overview]Time to Progression
NCT01374217 (4) [back to overview]Quality of Life Scores
NCT01401543 (4) [back to overview]Pharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473
NCT01401543 (4) [back to overview]Pharmacokinetics: AUC(0-∞) of Tadalafil
NCT01401543 (4) [back to overview]Pharmacokinetics: Cmax of Tadalafil
NCT01401543 (4) [back to overview]Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473
NCT01444651 (6) [back to overview]Change in Insulin Resistance From Baseline to 3 Months, as Measured by HOMA-IR
NCT01444651 (6) [back to overview]Baseline to 3 Month Change in Composite of Insulin Resistance and Sensitivity, as Measured by the Oral Disposition Index
NCT01444651 (6) [back to overview]Baseline to 3-month Change in Endothelial Function Measured by EndoPAT
NCT01444651 (6) [back to overview]Baseline to 3-month Change in Insulin Sensitivity, as Measured by the Matsuda Index
NCT01444651 (6) [back to overview]Baseline to 3-month Change in Matsuda Disposition Index
NCT01444651 (6) [back to overview]Insulinogenic Index
NCT01460342 (8) [back to overview]Change From Baseline in Total Score of International Prostate Symptom Score (IPSS) at 12 Weeks
NCT01460342 (8) [back to overview]Change From Baseline in the International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index
NCT01460342 (8) [back to overview]Change From Baseline in the International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore
NCT01460342 (8) [back to overview]Change From Baseline in the International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore
NCT01460342 (8) [back to overview]Patient Global Impression of Improvement (PGI-I) Scale at 12 Weeks
NCT01460342 (8) [back to overview]Change From Baseline in Total Score of International Prostate Symptom Score (IPSS)
NCT01460342 (8) [back to overview]Clinician Global Impression of Improvement (CGI-I) Scale at 12 Weeks
NCT01460342 (8) [back to overview]Change From Baseline in Modified International Prostate Symptom Score (mIPSS) Score at 2 Weeks
NCT01484431 (4) [back to overview]Number of Participants With Palatability of the Tadalafil Suspension
NCT01484431 (4) [back to overview]Population Pharmacokinetics: Area Under the Concentration Curve Versus Time at a Dosing Interval at Steady State (AUCtau) for Tadalafil
NCT01484431 (4) [back to overview]Population Pharmacokinetics: Average Concentration (Cmean,ss) of for Tadalafil at Steady-State.
NCT01484431 (4) [back to overview]Percentage of Participants With Clinical Worsening
NCT01544998 (6) [back to overview]Change in Glomerular Filtration Rate (GFR) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group
NCT01544998 (6) [back to overview]Change in Natriuresis (Urinary Sodium Excretion) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group
NCT01544998 (6) [back to overview]Change in Natriuresis (Urinary Sodium Excretion) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group
NCT01544998 (6) [back to overview]Change in Glomerular Filtration Rate (GFR) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group
NCT01544998 (6) [back to overview]Change in Urinary Cyclic Guanosine Monophosphate (cGMP) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group
NCT01544998 (6) [back to overview]Change in Urinary Cyclic Guanosine Monophosphate (cGMP) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group
NCT01661595 (25) [back to overview]Exercised Induced Fatigability as Measured by Fatigue Rating Scale After 4 Weeks of Active Drug
NCT01661595 (25) [back to overview]Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 0.
NCT01661595 (25) [back to overview]Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 4.
NCT01661595 (25) [back to overview]Exercised Induced Fatigability as Measured by Fatigue Rating Scale After 4 Weeks of Placebo
NCT01661595 (25) [back to overview]Hemoglobin Level at Week 0
NCT01661595 (25) [back to overview]Hematocrit Level Was Measured at 4 Weeks
NCT01661595 (25) [back to overview]Hematocrit Level Measured at Week 0
NCT01661595 (25) [back to overview]Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 8.
NCT01661595 (25) [back to overview]Hematocrit Level Measured at Week 8
NCT01661595 (25) [back to overview]Walking Distance at 100% Effort as Measured by Walking Test After 4 Weeks of Placebo
NCT01661595 (25) [back to overview]Walking Distance at 100% Effort as Measured by Walking Test After 4 Weeks of Active Drug
NCT01661595 (25) [back to overview]Skeletal Muscle Fatigue as Measured by Biodex 4 Pro After 4 Weeks of Placebo
NCT01661595 (25) [back to overview]Skeletal Muscle Fatigue as Measured by Biodex 4 Pro After 4 Weeks of Active Drug
NCT01661595 (25) [back to overview]Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 8
NCT01661595 (25) [back to overview]Hemoglobin Level Measured at Week 4
NCT01661595 (25) [back to overview]Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 0
NCT01661595 (25) [back to overview]Maximum Peak Isometric Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Placebo
NCT01661595 (25) [back to overview]Maximum Peak Isometric Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Active Drug.
NCT01661595 (25) [back to overview]Maximum Peak Isokinetic Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Placebo.
NCT01661595 (25) [back to overview]Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 4
NCT01661595 (25) [back to overview]Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 8.
NCT01661595 (25) [back to overview]Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 4.
NCT01661595 (25) [back to overview]Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 0.
NCT01661595 (25) [back to overview]Hemoglobin Level Measured at Week 8
NCT01661595 (25) [back to overview]Maximum Peak Isokinetic Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Active Drug
NCT01824290 (7) [back to overview]Period 1: Change From Baseline to Week 24 in a 6 Minute Walk (MW) Distance in Meters
NCT01824290 (7) [back to overview]Period 1: Percentage of Participants Who Experience CW
NCT01824290 (7) [back to overview]Period 1: Time to Adjudicated Clinical Worsening (CW)
NCT01824290 (7) [back to overview]Period 2: Percentage of Participants Who Experience CW
NCT01824290 (7) [back to overview]Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at Steady-state
NCT01824290 (7) [back to overview]Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at Steady-state
NCT01824290 (7) [back to overview]Period 2: Time to First Occurrence of CW
NCT01862536 (7) [back to overview]Pulmonary Vascular Resistance
NCT01862536 (7) [back to overview]Change in 6 Minute Walk Test
NCT01862536 (7) [back to overview]Tricuspid Annular Plane Excursion (TAPSE)
NCT01862536 (7) [back to overview]St. George's Respiratory Questionnaire, Dyspnea and Health Related Quality of Life
NCT01862536 (7) [back to overview]Maximum VO2
NCT01862536 (7) [back to overview]Mean Pulmonary Artery Pressure
NCT01862536 (7) [back to overview]N-type Brain Natriuretic Peptide (BNP) Concentration
NCT01865084 (7) [back to overview]Change From Baseline in Six Minute Walk Distance (6MWD) in Meters
NCT01865084 (7) [back to overview]Change From Baseline in the North Star Ambulatory Assessment (NSAA) Global Score
NCT01865084 (7) [back to overview]Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil
NCT01865084 (7) [back to overview]Time to Persistent 10% Worsening in 6MWD
NCT01865084 (7) [back to overview]Change From Baseline in Pediatric Outcomes Data Collection Instrument (PODCI) Scores
NCT01865084 (7) [back to overview]Change From Baseline in Timed Function Tests in Seconds
NCT01865084 (7) [back to overview]Time to Persistent 10% Worsening in Timed Function Tests (TFT)
NCT01937871 (22) [back to overview]Change From Baseline in Yes Responses to Question 2 of the Sexual Encounter Profile (SEP) Questionnaire at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IIEF Intercourse Satisfaction at Week 12
NCT01937871 (22) [back to overview]Number of Participants With Clinician Global Impression of Improvement (CGI-I) at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Yes Responses to Question 3 of the SEP Questionnaire at Week 4 and Week 8
NCT01937871 (22) [back to overview]Change From Baseline in Yes Responses to Question 2 of the SEP Questionnaire at Week 4 and Week 8
NCT01937871 (22) [back to overview]Change From Baseline in IIEF EF at Week 4 and Week 8
NCT01937871 (22) [back to overview]Change From Baseline in Yes Responses to Question 3 of the SEP Questionnaire at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Total IPSS at Week 4 and Week 8
NCT01937871 (22) [back to overview]Change From Baseline in IIEF Subscores at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Postvoid Residual Volume (PVR) at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Modified International Prostate Symptom Score (mIPSS) at Week 2
NCT01937871 (22) [back to overview]Change From Baseline in IPSS Voiding (Obstructive) Subscore at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IPSS Storage (Irritative) Subscore at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in Uroflowmetry Measures at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IPSS Quality of Life (QoL) Index at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IIEF Sexual Desire at Week 12
NCT01937871 (22) [back to overview]Number of Participants With Patient Global Impression of Improvement (PGI-I) at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IPSS at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IIEF Overall Satisfaction (OS) at Week 12
NCT01937871 (22) [back to overview]Change From Baseline in IIEF Orgasmic Function at Week 12
NCT01970176 (3) [back to overview]Change in Glomerular Filtration Rate (GFR)
NCT01970176 (3) [back to overview]Change in Urinary Cyclic Guanosine 3',5'-Monophosphate (cGMP) Hormone Excretion
NCT01970176 (3) [back to overview]Change in Urinary Sodium Excretion
NCT02058095 (3) [back to overview]Change in Urinary Sodium Excretion
NCT02058095 (3) [back to overview]Change in Glomerular Filtration Rate (GFR)
NCT02058095 (3) [back to overview]Change in Urinary Cyclic Guanosine 3',5'-Monophosphate (cGMP) Hormone Excretion
NCT02194465 (5) [back to overview]Change From Baseline to 4 Weeks in 24 Hour Ambulatory Blood Pressure Monitoring (ABPM)
NCT02194465 (5) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of LY2623091
NCT02194465 (5) [back to overview]Change From Baseline to 4 Weeks in Seated Diastolic Blood Pressure (DBP)
NCT02194465 (5) [back to overview]Change From Baseline to 4 Weeks in Seated Systolic Blood Pressure (SBP)
NCT02194465 (5) [back to overview]Change From Baseline to 4 Weeks in Serum Potassium
NCT02224846 (8) [back to overview]Percentage of Participants Experiencing at Least One Adverse Event Leading to Discontinuation
NCT02224846 (8) [back to overview]Percentage of Participants Experiencing at Least One Treatment Emergent Adverse Event (Serious or Non-Serious)
NCT02224846 (8) [back to overview]"Percentage of Participants With Yes Responses to Global Assessment Questions (GAQ)1 and GAQ2"
NCT02224846 (8) [back to overview]"Percentage of Participants With Yes Responses to Sexual Encounter Profile (SEP) Diary"
NCT02224846 (8) [back to overview]Change From Baseline in the IIEF-EF Domain Questionnaire Score of 5 mg Tadalafil Treatments
NCT02224846 (8) [back to overview]Percentage of Participants Achieving Normal Erectile Functioning
NCT02224846 (8) [back to overview]Percentage of Participants Achieving Normal Erectile Functioning of 5 mg Tadalafil Treatments
NCT02224846 (8) [back to overview]Change From Baseline in the International Index of Erectile Function- Erectile Function (IIEF-EF) Domain Questionnaire Score
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Simvastatin and Simvastatin Acid
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Simvastatin and Simvastatin Acid
NCT02300259 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of LY2623091
NCT02300259 (6) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of Simvastatin and Simvastatin Acid
NCT02431754 (7) [back to overview]Percentage of Participants With PGI-I (Drug Attributes Questionnaire) on 8 Symptoms for BPH-Lower Urinary Tract Symptoms Improvement
NCT02431754 (7) [back to overview]Change From Baseline on the IPSS Quality of Life Score (IPSS QoL )
NCT02431754 (7) [back to overview]Change From Baseline on the International Prostate Symptom Score (IPSS) Total Score
NCT02431754 (7) [back to overview]Change From Baseline on the IPSS Storage (Irritative) Subscore
NCT02431754 (7) [back to overview]Change From Baseline on the IPSS Voiding (Obstructive) Subscore
NCT02431754 (7) [back to overview]Percentage of Participants With Global Impression of Improvement (PGI-I)
NCT02431754 (7) [back to overview]Percentage of Participants Preferring Combination Therapy Over Alpha Blocker Alone on the Treatment Preference Questionnaire (TPQ)
NCT02558231 (10) [back to overview]Percentage of Participants With Absence of Worsening From Baseline to Week 26 in World Health Organization (WHO) Functional Class (FC)
NCT02558231 (10) [back to overview]Number of Participants With Disease Progression Event
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in 6-minute Walk Distance (6MWD)
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Cardiac Index
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Mean Pulmonary Arterial Pressure (mPAP)
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Mean Right Atrial Pressure (mRAP)
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in N-terminal Pro B-type Natriuretic Peptide (NT-proBNP) Levels
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Pulmonary Vascular Resistance (PVR)
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Total Pulmonary Resistance
NCT02558231 (10) [back to overview]Change From Baseline to Week 26 in Venous Oxygen Saturation (%)
NCT02595684 (17) [back to overview]Body Fat
NCT02595684 (17) [back to overview]Area Under the Curve (AUC) Glucose
NCT02595684 (17) [back to overview]Diastolic Blood Pressure
NCT02595684 (17) [back to overview]Body Mass Index
NCT02595684 (17) [back to overview]Body Weight
NCT02595684 (17) [back to overview]Fasting Glucose
NCT02595684 (17) [back to overview]First Phase of Insulin Secretion
NCT02595684 (17) [back to overview]High Density Lipoprotein Cholesterol (HDL-c)
NCT02595684 (17) [back to overview]Insulin Sensitivity
NCT02595684 (17) [back to overview]Low Density Lipoprotein Cholesterol (LDL-c)
NCT02595684 (17) [back to overview]Postprandial Glucose
NCT02595684 (17) [back to overview]Systolic Blood Pressure
NCT02595684 (17) [back to overview]Total Cholesterol
NCT02595684 (17) [back to overview]Total Insulin Secretion
NCT02595684 (17) [back to overview]Triglycerides
NCT02595684 (17) [back to overview]Waist Circumference
NCT02595684 (17) [back to overview]Area Under the Curve (AUC) Insulin
NCT02688387 (59) [back to overview]Number of Participants With Clinical Chemistry Values of PCI- Part 2
NCT02688387 (59) [back to overview]Number of Participants With Abnormal Urinalysis Results by Dipstick Method-Part 1
NCT02688387 (59) [back to overview]Maximum Observed Concentration (Cmax) of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 1
NCT02688387 (59) [back to overview]Cmax of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 2
NCT02688387 (59) [back to overview]Cmax for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-Part 3A
NCT02688387 (59) [back to overview]Change From Baseline in Vital- Temperature, Part 2
NCT02688387 (59) [back to overview]Cmax for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B
NCT02688387 (59) [back to overview]Cmax for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions-3B
NCT02688387 (59) [back to overview]Change From Baseline in Vital- Temperature, Part 3B
NCT02688387 (59) [back to overview]Change From Baseline in Vital- Temperature, Part 3A
NCT02688387 (59) [back to overview]Change From Baseline in Vital- Temperature, Part 1
NCT02688387 (59) [back to overview]Change From Baseline in Vital- Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP), Part 1
NCT02688387 (59) [back to overview]Change From Baseline in Vital- SBP and DBP, Part 3B
NCT02688387 (59) [back to overview]Change From Baseline in Vital- SBP and DBP, Part 3A
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Respiratory Rate, Part 3A
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Respiratory Rate, Part 3-B
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Respiratory Rate, Part 2
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Respiratory Rate, Part 1
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Heart Rate, Part 3B
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Heart Rate, Part 3A
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Heart Rate, Part 2
NCT02688387 (59) [back to overview]Change From Baseline in Vital Signs-Heart Rate, Part 1
NCT02688387 (59) [back to overview]AUC From Time of Dose to Last Measurable Concentration (AUC [0-t]), in FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 1
NCT02688387 (59) [back to overview]AUC (0-t) for FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 2
NCT02688387 (59) [back to overview]AUC (0-t) for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-Part 3A
NCT02688387 (59) [back to overview]AUC (0-t) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B
NCT02688387 (59) [back to overview]Change From Baseline in Vital- SBP and DBP, Part 2
NCT02688387 (59) [back to overview]AUC (0-inf) for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-3A
NCT02688387 (59) [back to overview]AUC (0-inf) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B
NCT02688387 (59) [back to overview]AUC (0-inf) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions-3B
NCT02688387 (59) [back to overview]AUC (0 - Inf) for FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 2
NCT02688387 (59) [back to overview]Area Under the Plasma Concentration Time Curve (AUC) From Time Zero to Infinite (Inf) Time, AUC (0-inf) of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 1
NCT02688387 (59) [back to overview]Number of Participants With Abnormal Electrocardiogram (ECG) Findings, -Part 1
NCT02688387 (59) [back to overview]Number of Participants With Abnormal ECG Findings, -Part 3B
NCT02688387 (59) [back to overview]Number of Participants With Abnormal ECG Findings, -Part 3A
NCT02688387 (59) [back to overview]Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 3B
NCT02688387 (59) [back to overview]Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 3A
NCT02688387 (59) [back to overview]AUC (0-t) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions- Part 3B
NCT02688387 (59) [back to overview]Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 2
NCT02688387 (59) [back to overview]Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 1
NCT02688387 (59) [back to overview]Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 3B
NCT02688387 (59) [back to overview]Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 3A
NCT02688387 (59) [back to overview]Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 2
NCT02688387 (59) [back to overview]Plasma Half Life (t1/2) for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part1
NCT02688387 (59) [back to overview]Number of Participants With Urinalysis Results by Dipstick Analysis-Part 3B
NCT02688387 (59) [back to overview]Number of Participants With Urinalysis Results by Dipstick Analysis-Part 3A
NCT02688387 (59) [back to overview]Number of Participants With Urinalysis Results by Dipstick Analysis-Part 2
NCT02688387 (59) [back to overview]Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)-Part 1
NCT02688387 (59) [back to overview]Number of Participants With SAEs and AEs-Part 3B
NCT02688387 (59) [back to overview]Number of Participants With Abnormal ECG Findings, -Part 2
NCT02688387 (59) [back to overview]Number of Participants With SAEs and AEs-Part 3A
NCT02688387 (59) [back to overview]Number of Participants With SAEs and AEs-Part 2
NCT02688387 (59) [back to overview]Number of Participants With Hematology Values of Potential Clinical Importance (PCI)- Part1
NCT02688387 (59) [back to overview]Number of Participants With Hematology Values of PCI - Part 3B
NCT02688387 (59) [back to overview]Number of Participants With Hematology Values of PCI - Part 3A
NCT02688387 (59) [back to overview]Number of Participants With Hematology Values of PCI - Part 2
NCT02688387 (59) [back to overview]Number of Participants With Clinical Chemistry Values of PCI- Part1
NCT02688387 (59) [back to overview]Number of Participants With Clinical Chemistry Values of PCI- Part 3B
NCT02688387 (59) [back to overview]Number of Participants With Clinical Chemistry Values of PCI- Part 3A
NCT02819440 (8) [back to overview]Insulin Sensitivity After 12 Weeks of Drug Therapy
NCT02819440 (8) [back to overview]Sexual Function
NCT02819440 (8) [back to overview]Dual Energy X-Ray Absorptiometry (DEXA) (g)
NCT02819440 (8) [back to overview]Resting Energy Expenditure After 12 Weeks of Drug Therapy (kcal/Day)
NCT02819440 (8) [back to overview]Quality of Life Using the Medical Outcomes Study Short-Form Health Survey (SF-36) Physical Component Score
NCT02819440 (8) [back to overview]Physical Activity-induced Energy Expenditure (kcal/Day)
NCT02819440 (8) [back to overview]Maximal Oxygen Consumption
NCT02819440 (8) [back to overview]Maximal Exercise Energy Expenditure (kcal/Day)
NCT02891850 (5) [back to overview]Number of Participants With Satisfactory Clinical Response at Week 24
NCT02891850 (5) [back to overview]Number of Participants With Adjudicated Clinical Worsening at Week 24
NCT02891850 (5) [back to overview]Change in World Health Organization Functional Class (WHO FC) With Last Observation Carried Forward From Baseline to Week 24
NCT02891850 (5) [back to overview]Change in 6 Minute Walking Distance (6MWD) With Last Observation Carried Forward From Baseline to 24 Weeks
NCT02891850 (5) [back to overview]Change in N-terminal Pro-Brain Natriuretic Peptide (NT-proBNP) With Last Observation Carried Forward at Week 24
NCT03785210 (4) [back to overview]Best Overall Response (BOR)
NCT03785210 (4) [back to overview]Serious Adverse Events Possibly, Probably, and/or Definitely Related to Treatment
NCT03785210 (4) [back to overview]Overall Survival (OS) of Nivolumab Combined With Oral Vancomycin and Tadalafil in Participants With Refractory Hepatocellular Carcinoma (HCC) or Liver Dominant Metastatic Cancer From Colorectal Cancer or Pancreatic Ductal Adenocarcinoma (PDAC)
NCT03785210 (4) [back to overview]Number of Participants With Serious and/or Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0)
NCT03904693 (1) [back to overview]Change in Pulmonary Vascular Resistance (PVR) Expressed as the Ratio of Geometric Means of End of Double-blind Treatment (EDBT) to Baseline
NCT04984993 (3) [back to overview]Percentage of Uses Per Patient That Led to an Onset of Erection Within a Certain Period of Time in Patients Randomised to MED3000.
NCT04984993 (3) [back to overview]Percentage of Uses Per Patient That Led to an Onset of Action Within a Certain Period of Time in Patients Randomised to MED3000.
NCT04984993 (3) [back to overview]Change From Baseline in the Erectile Function (EF) Domain of the International Index of Erectile Function (IIEF) Questionnaire, in Patients Randomised to MED3000, at Week 24

Change From Baseline to Week 12 in International Prostate Symptom Score (IPSS): Supportive Analysis

Assesses the severity of BPH-LUTS and the response to therapy. The total score was derived by summing the scores of the responses to the 7 component questions. Scores range from 0 to 35; 0-7 Mildly symptomatic; 8-19 moderately symptomatic; 20-35 severely symptomatic. (NCT00384930)
Timeframe: Baseline and 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-2.23
2.5 mg Tadalafil-3.81
5 mg Tadalafil-4.83
10 mg Tadalafil-5.13
20 mg Tadalafil-5.17

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Change From Baseline to 12 Week Endpoint in Benign Prostatic Hyperplasia Impact Index (BII)

Measures the impact that symptoms of BPH has on the patients well being. This questionnaire has 4 questions assessing the level of urinary discomfort and it's impact on the patients. Three questions range from 0 (no impact) to 4 (high impact); one question ranges from 0 (low impact) to 4 (high impact). The BII score ranges from 0 to 16. (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil4.86-1.31
2.5 mg Tadalafil4.73-0.83
20 mg Tadalafil4.75-1.34
5 mg Tadalafil4.66-1.25
Placebo4.94-0.79

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF) EF Domain

Measures erectile function over the past 4 weeks on Questions 1-5 and 15 (6 questions) of the International Index of Erecile Function (IIEF) questionnaire. Scores range from 0 (low/no erectile function) to 5 (high erectile function), thus the 6 questions of the IIEF-EF domain range from 0 to 30. (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil17.226.64
2.5 mg Tadalafil17.423.97
20 mg Tadalafil16.287.44
5 mg Tadalafil15.296.56
Placebo17.260.78

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) (Irritative) Subscore

Measures irritative symptoms over the past 4 weeks of the IPSS. IPSS irritative subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores range from 1 (few irritative symptoms) to 5 (frequent irritative symptoms), thus the 3 questions of the irritative subscore range from 0 to 15. (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil7.88-2.04
2.5 mg Tadalafil7.78-1.62
20 mg Tadalafil7.53-2.05
5 mg Tadalafil7.65-1.91
Placebo7.58-0.99

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index

Assessment of quality of life (QOL) by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible). (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil3.55-0.98
2.5 mg Tadalafil3.69-0.86
20 mg Tadalafil3.59-0.97
5.0 mg Tadalafil3.54-0.92
Placebo3.57-0.56

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Question 7 (Nocturia)

Measures nocturia (the need to get up at night to urinate) over the past 4 weeks. Scores range from 1 (few episodes of nocturia) to 5 (frequent episodes of nocturia). (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil2.36-0.43
2.5 mg Tadalafil2.37-0.43
20 mg Tadalafil2.20-0.54
5 mg Tadalafil2.36-0.49
Placebo2.36-0.36

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore

Measures obstructive symptoms over the past 4 weeks of the IPSS. IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 1 (few obstructive symptoms) to 5 (frequent obstructive symptoms), thus the 4 questions of the obstructive score range from 0 to 20. (NCT00384930)
Timeframe: 12 weeks

,,,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
10 mg Tadalafil9.88-3.29
2.5 mg Tadalafil9.71-2.31
20 mg Tadalafil9.57-3.17
5 mg Tadalafil9.65-3.00
Placebo9.51-1.27

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS): Primary Analysis

Assesses the severity of BPH-LUTS and the response to therapy. The total score was derived by summing the scores of the responses to the 7 component questions. Scores range from 0 to 35; 0-7 Mildly symptomatic; 8-19 moderately symptomatic; 20-35 severely symptomatic. (NCT00384930)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
5 mg Tadalafil17.30-4.92
Placebo17.08-2.25

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Change From Baseline to 12 Week Endpoint in Peak Urinary Flow

Measures the maximum flow rate of urine (measured in mL/s). This is a continuous parameter with positive numeric values. (NCT00384930)
Timeframe: baseline and 12 weeks

,,,,
Interventionmilliliter per second (Mean)
BaselineChange from Baseline
10 mg Tadalafil9.931.69
2.5 mg Tadalafil9.971.50
20 mg Tadalafil9.822.15
5 mg Tadalafil10.371.61
Placebo10.311.23

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"Number of Participants Who Answer Yes to the Lower Urinary Tract Symptoms (LUTS) Global Assessment Question (LUTS-GAQ)"

LUTS-GAQ Question asks the participant if the treatment they have been on has improved their uninary symptoms. (NCT00384930)
Timeframe: 12 weeks

Interventionparticipants (Number)
Placebo109
2.5 mg Tadalafil120
5 mg Tadalafil139
10 mg Tadalafil146
20 mg Tadalafil138

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Change From Baseline to 12 Week Endpoint in Postvoid Residual Volume (PVRcath) Measured During Free-Flow Studies

PVRcath is the volume of urine remaining int he bladder after voiding, measured by catheterization. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo59.62-1.85
Tadalafil48.99-9.13

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Clinically Adverse and Statistically Significant Changes From Baseline to 12 Week Endpoint in Laboratory Tests

Laboratory tests that were statistically significant and clinically adverse would be reported for safety. (NCT00386009)
Timeframe: Baseline and 12 weeks

Interventionsignificant and clinically adverse labs (Number)
Placebo0
Tadalafil0

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Change From Baseline to 12 Week Endpoint in Bladder Contractility Index (BCI) Measured During Pressure-Flow Studies

BCI was derived from the equation PdetQmax + 5Qmax. Scores: <100 means weak, 100-150 menas normal, >150 means strong. A decrease means a decrease in contractility of the bladder. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a nomogram (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo102.284.43
Tadalafil108.32-1.04

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Change From Baseline to 12 Week Endpoint in Bladder Outlet Obstruction Index (BOOI) Measured During Pressure-Flow Studies

BOOI, formerly known as the Abrams-Griffith number, was derived from the equation PdetQmax - 2Qmax. Scores: <20 means unobstructed, 20-40 means equivocol, >40 means obstructed. An increase means worsening of obstruction, a decreased means lessening of obstruction (improvement). (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a nomogram (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo35.840.92
Tadalafil36.28-3.71

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Change From Baseline to 12 Week Endpoint in Bladder Voiding Efficiency (BVE) Measured During Free-Flow Studies

Bladder voiding efficiency was defined as (Vcomp/total bladder capacity) X 100 (obtained when the bladder was full). (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo84.01-0.52
Tadalafil85.851.85

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Change From Baseline to 12 Week Endpoint in Bladder Volume at First Involuntary Detrusor Contraction

Assessed in participants with involuntary detrusor contractions during the bladder filling at both baseline and endpoint. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo120.5527.86
Tadalafil164.0028.56

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Change From Baseline to 12 Week Endpoint in Detrusor Pressure at Peak Urinary Flow Rate (PdetQmax)

(NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventioncentimeters of water (cm H20) (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo54.831.92
Tadalafil56.87-2.95

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Total Score

The IPSS Total Score is obtained by combining the scores of the responses to the 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00386009)
Timeframe: 12 weeks

,
Interventionunits on a scale (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo22.01-5.04
Tadalafil21.46-9.13

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Change From Baseline to 12 Week Endpoint in Maximum Detrusor Pressure (Max Pdet) Measured During Pressure-Flow Studies

Max Pdet was defined as the maximum detrusor pressure observed during voiding. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventioncentimeters of water (cm H20) (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo67.13-0.48
Tadalafil72.20-2.11

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Change From Baseline to 12 Week Endpoint in Mean Urinary Flow Rate (Qave) Measured During Free-Flow Studies

Qave was measured during free-flow tests using a standard calibrated flow meter. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmillilters per second (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo7.10-0.01
Tadalafil7.231.00

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Change From Baseline to 12 Week Endpoint in Mean Urinary Flow Rate (Qave) Measured During Pressure-Flow Studies

Qave was measured during pressure-flow tests. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters per second (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo4.670.45
Tadalafil5.500.58

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Change From Baseline to 12 Week Endpoint in Peak Urinary Flow Rate (Qmax) Measured During Free-Flow Studies

Qmax was measured during free-flow tests using a standard calibrated flow meter. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters per second (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo13.030.52
Tadalafil14.750.01

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Change From Baseline to 12 Week Endpoint in Peak Urinary Flow Rate (Qmax) Measured During Pressure-Flow Studies

Qmax was measured duirng pressure-flow tests. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters per second (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo9.490.50
Tadalafil10.290.38

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Change From Baseline to 12 Week Endpoint in Total Bladder Capacity Measured During Free-Flow Studies

Total bladder capacity was defined as Vcomp + PVRcath (obtained when the bladder was full). (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo327.95-17.53
Tadalafil316.79-14.88

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Change From Baseline to 12 Week Endpoint in Volume of Voided Urine (Vcomp) Measured During Free-Flow Studies

(NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo258.56-4.10
Tadalafil268.22-5.17

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Change From Baseline to 12 Week Endpoint in Volume of Voided Urine (Vcomp) Measured During Pressure-Flow Studies

Vcomp was defined as the volume of voided urine measured during pressure-flow tests. (NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionmilliliters (Mean)
BaselineChange from Baseline to 12 Week Endpoint
Placebo294.103.31
Tadalafil296.6413.51

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Presence of Involuntary Detrusor Contractions During Bladder Filling

(NCT00386009)
Timeframe: Baseline and 12 weeks

,
Interventionparticipants (Number)
Present at BaselineNot Present at BaselinePresent at EndpointNot Present at EndpointPresent at Both Baseline and EndpointPresent at Baseline OnlyPresent at Endpoint OnlyPresent at Neither Baseline nor Endpoint
Placebo3358365522111444
Tadalafil2856315318101343

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Improvement in the Sexual Quality of Life in the Subject and His Study Partner as Measured by the Sexual Quality of Life (SQoL) Domain of the Sexual Life Quality Questionnaire (SLQQ)

The original item scores (-4 to 4 range) were converted to 0 to 8 scale score by adding 4 to each recorded responses. Each transformed score was multiplied by 12.5 for a total range of 0 to 100. Higher scores are indicative of a higher sexual quality of life. (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
SQoL - Subject (change from baseline)SQoL-Partner (change from baseline) (n=70, n=238)
Placebo12.597.93
Tadalafil39.3732.87

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Sexual Life Quality Questionnaire (SLQQ) Treatment Satisfaction Domain

The 6 SLQQ-treatment satisfaction questions were answered by subject and partner at Visit 4/Final Visit. Original item scores (1 to 6 range) were converted to 0 to 5 scale by subtracting 1 to each recorded responses. Each transformed score was multiplied by 20. Total range of scores: 0 (low satisfaction) to 100 (high satisfaction). (NCT00422734)
Timeframe: 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
SLQQ - Subject (n=72, n=244)SLQQ - Partner (n=70, n=238)
Placebo51.5855.25
Tadalafil75.0473.42

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"Percent of Subjects With Yes Responses to Global Assessment Questionnaire (GAQ) - Subject Response"

"Percent of subjects with Yes responses to Question 1 (Improvement in Erections) and Question 2 (Improvement in the Ability to Engage in Sexual Activity)" (NCT00422734)
Timeframe: 12 weeks

,
Interventionpercentage of subjects answering Yes (Number)
GAQ Question 1GAQ Question 2
Placebo2622
Tadalafil8179

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"Percent of Partners With Yes Responses to Global Assessment Questionnaire (GAQ) - Partner Response"

"Percent of Partners with Yes responses to Question 1 (Improvement in Erections) and Question 2 (Improvement in the Ability to Engage in Sexual Activity)" (NCT00422734)
Timeframe: 12 weeks

,
Interventionpercentage of partners answering Yes (Number)
GAQ Question 1GAQ Question 2
Placebo3024
Tadalafil7976

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"Change From Baseline to Endpoint in the Percent of Yes Responses to Sexual Encounter Profile (SEP) Diary Questions 2 (SEP2) and 3 (SEP3)."

"The baseline and endpoint score for each SEP question 2 (Insert penis into vagina) and 3 (Successful intercourse) are the subject's percentage of yes responses to those questions during the run-in period and postbaseline period, respectively." (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionpercent (Least Squares Mean)
"Question 2 change from baseline in percent yes""Question 3 change from baseline in percent yes"
Placebo2.1910.80
Tadalafil28.8046.46

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"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Partner-Sexual Encounter Profile (SEP) Questions 1 and 2 - Partner Response"

"The baseline and endpoint score for each SEP question 1 (Achieve some erection) and 2 (Insert penis into vagina) are the partner's percentage of yes responses to those questions during the run-in period and postbaseline period, respectively." (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionpercent (Least Squares Mean)
"Question 1 change from baseline in percent Yes""Question 2 change from baseline in percent Yes"
Placebo1.256.97
Tadalafil18.3430.69

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Change From Baseline to Week 12 Endpoint in the International Index of Erectile Function - Intercourse Satisfaction Domain - Subject Response

Self-reported intercourse satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 3 questions of the IIEF-IS domain range from 0 to 15. (NCT00422734)
Timeframe: Baseline and 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo0.09
Tadalafil2.74

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"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Sexual Encounter Profile (SEP) Questions 4 and 5 - Subject Response"

"The baseline and endpoint score for each SEP question 4 (Satisfied with hardness) and 5 (Satisfied overall) are the subject's percentage of yes responses to those questions during the run-in period and postbaseline period, respectively." (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionpercent (Least Squares Mean)
"Question 4 change from baseline in percent Yes""Question 5 change from baseline in percent Yes"
Placebo12.0811.47
Tadalafil50.0548.78

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Change From Baseline to Endpoint in the International Index of Erectile Function (IIEF)- Erectile Function Domain Score (Sum of IIEF Questions 1-5 and 15)

Measures erectile function over the past 4 weeks on Questions 1-5 and 15 (6 questions) of the International Index of Erecile Function (IIEF) questionnaire. Scores range from 0 (low/no erectile function) to 5 (high erectile function), thus the 6 questions of the IIEF-EF domain range from 0 to 30. (NCT00422734)
Timeframe: Baseline and 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo0.49
Tadalafil8.03

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Change From Baseline to 12 Week Endpoint in the Satisfaction Domain of the Female Sexual Function Index (FSFI) - Partner Response

The FSFI Satisfaction Domain (items 14-16) measures satisfaction with emotional closeness, sexual relationship, and overall sexual life. Each question is scored on a 0/1 to 5 scale and domain score is calculated by multiplying the total points by 0.4, for a total score range of 0.8 to 6, with higher scores indicating greater satisfaction. (NCT00422734)
Timeframe: Baseline and 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.40
Tadalafil0.32

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Change From Baseline to 12 Week Endpoint in Overall Satisfaction Domain of the International Index of Erectile Function (IIEF-OS) - Subject Response

Self-reported overall satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 2 questions of the IIEF-OS domain range from 0 to 10. (NCT00422734)
Timeframe: Baseline and 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo0.44
Tadalafil2.57

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"Change From Baseline to 12 Week Endpoint in Percent of Yes Responses to Partner-Sexual Encounter Profile (SEP) Question 3 - Partner Response"

"The baseline and endpoint score for partner SEP question 3 (Satisfied overall) are the partner's percentage of yes responses to the question during the run-in period and postbaseline period, respectively." (NCT00422734)
Timeframe: Baseline and 12 weeks

Interventionpercent (Least Squares Mean)
Placebo10.21
Tadalafil43.16

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Change From Baseline to 12 Week Endpoint in the Self-Esteem and Relationship (SEAR) Questionnaire

Measures improvement in self-esteem and relationship satisfaction. Questionnaire consists of two domains, Sexual Relationship (items 1-8) and Confidence (items 9-14). Overall score is transformed onto a 0 (least favorable) to 100 (most favorable) scale. Overall score was calculated from two domains and subscales scores. (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
Total Score change from baselineSexual Relationship change from baselineConfidence change from baseline
Placebo3.074.610.91
Tadalafil30.4434.2825.35

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Change From Baseline to 12 Week Endpoint in the Self-Esteem and Relationship (SEAR) Questionnaire - Confidence Domain Subscales

Measures improvement in confidence (items 9-14). Confidence domain consists of two subscales (Self-Esteem, items 9-12; Overall Relationship, items 13 and 14). Each domain score, subscale score, and overall score are transformed onto a 0 (least favorable) to 100 (most favorable) scale. (NCT00422734)
Timeframe: Baseline and 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
Self-Esteem change from baselineOverall Relationship change from baseline
Placebo3.26-4.04
Tadalafil29.5616.97

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Change From Baseline to 12 Week Endpoint in Uroflowmetry Parameters - Peak Urine Flow Rate (Qmax) and Mean Urine Flow Rate (Qmean)

Qmax: defined as the peak urine flow rate (measured in milliliters per second [mL/second] using a standard calibrated flowmeter); and Qmean, defined as the mean urine flow rate (measured in mL/second using a standard calibrated flowmeter). (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionmilliliters per second (Mean)
Baseline Qmax12 Week Change QmaxBaseline Qmean12 Week Change Qmean
Placebo10.52.85.72.0
Tadalafil11.42.46.11.5
Tamsulosin11.71.96.21.0

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Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Nocturia Subscore

IPSS Question 7 is used to assess the frequency of nocturia. Scores range from 0 (low frequency of nocturia) to 5 (high frequency of nocturia). (NCT00540124)
Timeframe: baseline, 4, 8, and 12 weeks

,,
Interventionunits on a scale (Mean)
Baseline (n=50, n=50, n=49)4 Week Change (n=50, n=49, n=49)8 Week Change (n=47, n=50, n=48)12 Week Change (n=47, n=48, n=48)
Placebo2.0-0.3-0.4-0.5
Tadalafil1.8-0.4-0.4-0.5
Tamsulosin1.7-0.3-0.4-0.5

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Clinician Global Impression of Improvement (CGI-I) Combined Categories - Frequencies

"Measures clinician's perception of patient improvement of illness at the time of assessment compared with start of treatment. Scores range from 1 (very much better) to 7 (very much worse). Scores were combined to provide number of participants whose clinician indicated they were worse (scores of 5, 6, or 7), no change (score of 4), or better (scores of 1, 2, or 3)." (NCT00540124)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
WorseNo ChangeBetter
Placebo0543
Tadalafil0841
Tamsulosin4440

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Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Obstructive Subscore

The IPSS voiding (obstructive) subscore is defined as sum of scores for Questions 1, 3, 5, and 6 of the IPSS. If scores for any of these questions are missing for a visit, the IPSS voiding subscore will be reported as missing for that visit. Subscore totals range from 0 to 20; higher scores are indicative of greater obstruction. (NCT00540124)
Timeframe: baseline, 4, 8, and 12 weeks

,,
Interventionunits on a scale (Mean)
Baseline (n=50, n=50, n=49)4 Week Change (n=50, n=49, n=49)8 Week Change (n=47, n=50, n=48)12 Week Change (n=47, n=48, n=48)
Placebo10.6-2.0-2.3-2.7
Tadalafil10.4-2.6-3.1-3.6
Tamsulosin11.2-2.4-3.1-3.9

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Patient Global Impression of Improvement (PGI-I) Combined Categories - Frequencies

"A scale that measures the patient's perception of improvement at the time of assessment compared with the start of treatment. The score ranges from 1 (very much better) to 7 (very much worse). Scores were combined to provide number of participants who indicated they were worse (scores of 5, 6, or 7), no change (score of 4), or better (scores of 1, 2, or 3)." (NCT00540124)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
WorseNo ChangeBetter
Placebo11037
Tadalafil1543
Tamsulosin3738

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Change From Baseline to 4, 8, and 12 Week Endpoints in International Prostate Symptom Score (IPSS) - Irritative Subscore

The IPSS storage (irritative) subscore is defined as sum of scores for Questions 2, 4, and 7 of the IPSS. If scores for any of these questions are missing for a visit, the IPSS storage subscore will be reported as missing for that visit. Subscore totals range from 0 to 15; higher scores are indicative of greater irritation. (NCT00540124)
Timeframe: baseline, 4, 8, and 12 weeks

,,
Interventionunits on a scale (Mean)
Baseline (n=50, n=50, n=49)4 Week Change (n=50, n=49, n=49)8 Week Change (n=47, n=50, n=48)12 Week Change (n=47, n=48, n=48)
Placebo6.7-0.8-0.9-1.6
Tadalafil6.7-1.4-1.6-2.2
Tamsulosin6.5-1.7-1.9-1.8

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Change From Baseline to 4 Week and 8 Week Endpoints in International Prostate Symptom Score (IPSS) Total Score

The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00540124)
Timeframe: baseline, 4 and 8 weeks

,,
Interventionunits on a scale (Least Squares Mean)
4 Week Change (n=50, n=49, n=49)8 Week Change (n=47, n=50, n=48)
Placebo-2.8-3.3
Tadalafil-4.0-4.8
Tamsulosin-4.0-4.8

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Change From Baseline to 12 Week Endpoint in Voids With Terminal Micturition Dribble and Post Micturition Dribble Per Week Based on Median as Reported by Patient Voiding Dribble Diary

A patient-completed diary that measures terminal dribble (dribble in the end of urination) and post-micturition dribble (dribble after urination). (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionaverage number per week (Mean)
Baseline Terminal Micturation Dribble12 Week Change Terminal Micturation DribbleBaseline Post Micturation Dribble12 Week Change Post Micturation Dribble
Placebo68.7-11.714.3-0.8
Tadalafil69.81.617.8-4.8
Tamsulosin77.5-8.525.5-7.6

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Change From Baseline to 12 Week Endpoint in Uroflowmetry Parameters - Voided Urine Volume (Vcomp)

Vcomp, defined as the volume of voided urine (measured in milliliters [mL]). (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionmilliliters (Mean)
Baseline12 Week Change
Placebo220.021.4
Tadalafil233.219.7
Tamsulosin236.623.9

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Change From Baseline to 12 Week Endpoint in Total, Waking, and Sleeping Voids (Average Number Per Week) Based on Median as Reported in Patient Voiding Dribble Diary

Patient-completed diary that measures daytime frequency (waking voids) and nocturia (sleeping voids). Average number of waking voids per week, average number of sleeping voids per week, and average number of total voids (sleeping+waking) per week are reported. (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionaverage number per week (Mean)
Baseline Waking Voids12 Week Change Waking VoidsBaseline Sleeping Voids12 Week Change Sleeping VoidsBaseline Total Voids12 Week Change Total Voids
Placebo48.2-0.310.3-1.358.6-1.6
Tadalafil46.9-2.19.8-2.356.7-4.4
Tamsulosin48.4-1.37.9-1.456.3-2.7

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Change From Baseline to 12 Week Endpoint in Total Urinary Incontinence Episodes Per Week Based on Median as Reported in Patient Voiding Dribble Diary

A patient-completed diary that measures urinary incontinence (UI) (leaks). Number of UI leaks per week are reported. (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionaverage number per week (Mean)
Baseline12 Week Change
Placebo0.8-0.3
Tadalafil1.10.7
Tamsulosin1.6-0.3

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Change From Baseline to 12 Week Endpoint in International Prostate Symptom Score (IPSS) Total Score

The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Week Change
Placebo17.3-4.2
Tadalafil17.1-5.8
Tamsulosin17.7-5.6

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Change From Baseline to 12 Week Endpoint in Benign Prostatic Hyperplasia Impact Index (BPH-II)

The BPH-BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range of 0 to 13; higher scores represent increased perceived impact of BPH-LUTS on overall health. If scores for any component question were missing for a visit, BPH-BII was reported as missing for that visit. (NCT00540124)
Timeframe: baseline, 12 weeks

,,
Interventionunits on a scale (Mean)
Baseline12 Week Change
Placebo6.2-2.0
Tadalafil6.1-2.2
Tamsulosin6.2-1.7

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Probability of No Pulmonary Arterial Hypertension (PAH) Deterioration at Weeks 16, 28, 40 and up to 52

World Health Organization Functional Classification Assessment (WHO FC) is a method of classifying disease severity in PAH. The classes are: Class I: pulmonary hypertension (PH) but without resulting limitation of physical activity, Class II: PH resulting in slight limitation of physical activity, Class III: PH resulting in marked limitation of physical activity, Class IV: PH with inability to carry out any physical activity without symptoms. Deterioration of WHO FC is defined as moving to a higher WHO FC within one visit. Results are presented as Kaplan-Meier estimates (% probability) of remaining free from WHO FC deterioration after a given time. (NCT00549302)
Timeframe: Baseline and Weeks 16, 28, 40 and 52

,
Interventionprobability (%) no PAH deterioration (Number)
Week 16 (n=57, 262)Week 28 (n=50, 238)Week 40 (n=45, 222)Week 52 (n=33,136)
Tadalafil 20 Milligrams (mg) Double-Blind95888181
Tadalafil 40 mg Double-Blind96908885

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Number of Participants With Adverse Events (AEs)

A summary of serious and all other non-serious AEs, which include adverse events reported for laboratory tests and vital signs, is located in the Reported Adverse Event module. (NCT00549302)
Timeframe: Baseline (Double-Blind Period) up to Week 243 (End of Open-Label Period)

Interventionparticipants (Number)
Serious AEsOther Non-Serious AEs
Tadalafil 20 mg or 40 mg Double-Blind and 40 mg Open-Label184334

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6-Minute Walk Distance (6MWD) at Baseline and Weeks 16, 28, 40 and 52

6MWD measured the distance a participant was able to walk unassisted in 6 minutes. (NCT00549302)
Timeframe: Baseline and Weeks 16, 28, 40 and 52

,
Interventionmeters (m) (Mean)
Distance walked at Baseline (n=63, 287Distance walked at Week 16 (n=58, 272)Distance walked at Week 28 (n=55, 250)Distance walked at Week 40 (n=51, 241)Distance walked at Week 52 (n=51, 235)Endpoint-Week 52 or LOCF (n=60,281)
Tadalafil 20 Milligrams (mg) Double-Blind397.74396.37406.41411.81415.31401.52
Tadalafil 40 mg Double-Blind375.38381.47384.97386.57394.00379.80

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Borg Dyspnea Assessment at Baseline and Weeks 16, 28, 40 and 52

Borg dyspnea score is a participant rated measure of their greatest degree of shortness of breath during exertion (6-minute walk test). Score ranged from 0 (nothing at all) to 10 (very, very severe [maximal]). (NCT00549302)
Timeframe: Baseline and Weeks 16, 28, 40 and 52

,
Interventionunits on a scale (Mean)
Score at Baseline (n=62, 287)Score at Week 16 (n=58, 271)Score at Week 28 (n=54,249)Score at Week 40 (n=51, 240)Score at Week 52 (n=51,235)Endpoint-Week 52 or LOCF (n=60,281)
Tadalafil 40 mg3.653.513.443.383.293.54
Tadalalfil 20 Milligrams (mg)3.413.413.463.213.683.75

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Change From Baseline in Log-transformed N-terminal Pro-B-type Natriuretic Peptide (NT-proBNP) Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)

The primary analysis of this secondary outcome measure is mean percent change from Baseline to Week 24. The changes from Baseline to Weeks 4, 12, 36, and 48 were also evaluated. A decrease in log-transformed measurement value (pg/mL) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 48

,,,,
Interventionpg/mL (log-transformed) (Mean)
BaselineWeek 4Week 12Week 24Week 36Week 48
Ambrisentan Only6.15.75.75.75.75.6
Any Ambrisentan6.25.75.85.75.75.7
Any Placebo6.76.76.86.46.36.7
Placebo Only0.07.57.67.68.08.0
Placebo/Ambrisentan6.76.26.36.05.96.4

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Change From Baseline in Mean Pulmonary Artery Pressure (mPAP) (LOCF)

This secondary hemodynamic outcome is supportive of the primary outcome. A decrease in measurement value (mmHg) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 24

,,,
InterventionmmHg (Mean)
BaselineWeek 24
Ambrisentan Only49.944.4
Any Ambrisentan50.443.8
Any Placebo52.838.8
Placebo/Ambrisentan54.538.8

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Change From Baseline in Mean Right Atrial Pressure (mRAP) (LOCF)

This secondary hemodynamic outcome is supportive of the primary outcome. A decrease in measurement value (mmHg) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 24

,,,
InterventionmmHg (Mean)
BaselineWeek 24
Ambrisentan Only8.58.4
Any Ambrisentan8.78.1
Any Placebo11.16.3
Placebo/Ambrisentan10.36.3

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Change From Baseline in Pulmonary Vascular Resistance (PVR), Last Observation Carried Forward (LOCF)

The primary objective of this study is to evaluate the change from baseline in PVR, and other hemodynamic parameters, following the addition of ambrisentan to background PDE-5i therapy in subjects with PAH who have demonstrated a sub-optimal response to PDE-5i monotherapy. A decrease in measurement value (dynes sec/cm^5) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 24

,,,
Interventiondynes sec/cm^5 (Mean)
BaselineWeek 24
Ambrisentan Only761.2518.8
Any Ambrisentan758.0509.8
Any Placebo703.6439.8
Placebo/Ambrisentan731.6439.8

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Change From Baseline in Six Minute Walk Distance (6MWD) Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)

The primary analysis of this secondary outcome measure is mean change from Baseline to Week 24. The changes from Baseline to Weeks 4, 12, 36, and 48 were also evaluated. An increase in measurement value (meters walked) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 48

,,,,
Interventionmeters walked (Mean)
BaselineWeek 4Week 12Week 24Week 36Week 48
Ambrisentan Only361.9376.5377.9382.4366.5378.9
Any Ambrisentan369.6383.7384.3387.0370.2379.4
Any Placebo413.6441.2433.0423.4399.8387.2
Placebo Only335.0442.0422.0422.0402.0402.0
Placebo/Ambrisentan433.3441.0435.8423.8399.3383.5

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Overall Survival, Evaluated at Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, and After Week 48

Overall survival was defined as the time from initiation of active treatment to death. Results are presented as the Kaplan-Meier estimate (% probability) of death after a given time. (NCT00617305)
Timeframe: Baseline to Week 48+

,
InterventionProbability of death occurring (%) (Number)
At Week 4At Week 8At Week 12At Week 16At Week 20At Week 24At Week 28At Week 32At Week 36At Week 40At Week 44At Week 48After Week 48
Ambrisentan Only0000000004444
Any Ambrisentan0000000003333

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Time to Clinical Worsening of PAH, Evaluated at Weeks 4, 8, 12, 16, 20, 24, 28, 32, 36, 40, 44, 48, and After Week 48

The time to clinical worsening was defined as the time from enrollment to the first occurrence of death, lung transplantation, hospitalization for PAH, atrial septostomy, or initiation of chronic parenteral prostanoid therapy. Results are presented as the Kaplan-Meier estimate (% probability) of having clinical worsening after a given time. (NCT00617305)
Timeframe: Baseline to Week 48+

,
InterventionProbability of clinical worsening (%) (Number)
At Week 4At Week 8At Week 12At Week 16At Week 20At Week 24At Week 28At Week 32At Week 36At Week 40At Week 44At Week 48After Week 48
Ambrisentan Only0000336161620202020
Any Ambrisentan0000336141417171717

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Change From Baseline in Cardiac Output (LOCF)

This secondary hemodynamic outcome is supportive of the primary outcome. An increase in measurement value (L/min) indicates improvement for this patient population. (NCT00617305)
Timeframe: Baseline to Week 24

,,,
InterventionL/min (Mean)
BaselineWeek 24
Ambrisentan Only4.45.2
Any Ambrisentan4.45.2
Any Placebo4.85.2
Placebo/Ambrisentan4.85.2

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Change From Baseline in the Cambridge Pulmonary Hypertension Outcome Review (CAMPHOR) Quality of Life (QOL) Survey Overall Score Measured at Weeks 12, 24, 36 and 48 (LOCF)

The primary analysis of this secondary outcome measure is mean change from Baseline to Week 24. The changes from Baseline to Weeks 12, 36, and 48 were also evaluated. Lower scores and decreases from baseline represent improved functioning and QOL. The CAMPHOR survey was not assessed at Week 4. The total CAMPHOR score scale ranges from 0 (good) to 25 (poor). A reduction in score over time represents improvement in this patient population. (NCT00617305)
Timeframe: Baseline to Week 48

,,,,
Interventionunits on a scale (Mean)
BaselineWeek 12Week 24Week 36Week48
Ambrisentan Only8.26.87.27.77.6
Any Ambrisentan7.76.76.77.27.1
Any Placebo4.24.82.83.43.6
Placebo Only4.02.02.03.03.0
Placebo/Ambrisentan4.35.53.03.53.8

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Change From Baseline in World Health Organization (WHO) Functional Class (LOCF) Measured at Weeks 4, 12, 24, 36 and 48.

The primary analysis of this secondary outcome measure is change from Baseline to Week 24. The changes from Baseline to Weeks 4, 12, 36, and 48 were also evaluated. WHO categories are 1 to 4 with the worst category being 4. Improvement is represented by a change in category to a lower number (for example, change from category 3 to 2), and deterioration is represented by a change in category to a higher number (for example, change from category 2 to 4). No change is represented by no change in category (for example, category 2 which remains 2). (NCT00617305)
Timeframe: Baseline to Week 48

,,,,
Interventionparticipants (Number)
Week 4 - ImprovementWeek 4 - No ChangeWeek 4 - DeteriorationWeek 4 - Missing DataWeek 12 - ImprovementWeek 12 - No ChangeWeek 12 - DeteriorationWeek 12 - Missing DataWeek 24 - ImprovementWeek 24 - No ChangeWeek 24 - DeteriorationWeek 24 - Missing DataWeek 36 - ImprovementWeek 36 - No ChangeWeek 36 - DeteriorationWeek 36 - Missing DataWeek 48 - ImprovementWeek 48 - No ChangeWeek 48 - DeteriorationWeek 48 - Missing Data
Ambrisentan Only3290182401121911171411141711
Any Ambrisentan3330192701142111191611152011
Any Placebo14002300320032002300
Placebo Only10001000100010001000
Placebo/Ambrisentan04001300220022001300

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Change in Dyspnea Index Measured at Weeks 4, 12, 24, 36 and 48 (LOCF)

The primary analysis of this secondary outcome measure is mean change from Baseline to Week 24. The changes from Baseline to Weeks 4, 12, 36, and 48 were also evaluated. The dyspnea index measures the degree of breathlessness after completion of the 6MWT using a scale of 0 to 10, with 0 indicating no breathlessness and 10 indicating maximum breathlessness. (NCT00617305)
Timeframe: Baseline to Week 48

,,,,
Interventionunits on a scale (Mean)
BaselineWeek 4Week 12Week 24Week 36Week 48
Ambrisentan Only3.73.23.22.93.23.1
Any Ambrisentan3.63.23.32.83.23.1
Any Placebo2.63.03.82.13.43.4
Placebo Only3.02.03.03.03.03.0
Placebo/Ambrisentan2.53.34.01.93.53.5

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Change From Baseline to Endpoint in the Intercourse Satisfaction (IS) Domain of the IIEF

Self-reported intercourse satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 3 questions of the IIEF-IS domain range from 0 to 15. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]8.343.99
Tadalafil as Needed [T(PRN)]8.373.83
Tadalafil Once a Day [T(OaD)]8.353.33

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"Question 4 I Felt Like a Whole Man Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"

Scores for Question 4 range from 0 (not at all) to 4 (extremely). (NCT00734604)
Timeframe: 8 weeks of each treatment

Interventionunits on a scale (Mean)
Tadalafil Once a Day [T(OaD)]2.53
Sildenafil as Needed [S(PRN)]2.57
Tadalafil as Needed [T(PRN)]2.44

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"Question 2 I Felt in Control of my Sex Life Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"

Scores for Question 2 range from 0 (not at all) to 4 (extremely). (NCT00734604)
Timeframe: 8 weeks of each treatment

Interventionunits on a scale (Mean)
Tadalafil Once a Day [T(OaD)]2.33
Sildenafil as Needed [S(PRN)]2.14
Tadalafil as Needed [T(PRN)]2.36

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Change From Baseline to Endpoint in the Overall Satisfaction (OS) Domain of the IIEF

Self-reported overall satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 2 questions of the IIEF-OS domain range from 0 to 10. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]5.222.87
Tadalafil as Needed [T(PRN)]5.272.84
Tadalafil Once a Day [T(OaD)]5.262.60

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Change From Baseline Between Tadalafil Once a Day (OaD) and Tadalafil as Needed (PRN) in Sexual Self-Confidence Domain of Psychological and Interpersonal Relationship Scales (PAIRS)

The PAIRS is a self-administed scale that assesses the broader psychological and interpersonal outcomes associated with erectile dysfunction and its treatment. Sexual Self-Confidence score is the average of responses on 6 PAIRS item scores. Sexual Self-Confidence scores range from 1 (strongly disagree) to 4 (strongly agree). Higher scores are indicative of greater sexual self-confidence. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Tadalafil as Needed [T(PRN)]2.240.50
Tadalafil Once a Day [T(OaD)]2.240.50

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Change From Baseline Between Tadalafil Once a Day (OaD) and Sildenafil as Needed (PRN) in Sexual Self-Confidence Domain of Psychological and Interpersonal Relationship Scales (PAIRS)

The PAIRS is a self-administed scale that assesses the broader psychological and interpersonal outcomes associated with erectile dysfunction and its treatment. Sexual Self-Confidence score is the average of responses on 6 PAIRS item scores. Sexual Self-Confidence scores range from 1 (strongly disagree) to 4 (strongly agree). Higher scores are indicative of greater sexual self-confidence. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]2.230.39
Tadalafil Once a Day [T(OaD)]2.240.50

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Number of Participants With at Least One Serious Adverse Event

Serious adverse events are listed in the Reported Adverse Event module. (NCT00734604)
Timeframe: baseline through 26 weeks (including two washout periods of 1 week each)

Interventionparticipants (Number)
Tadalafil Once a Day [T(OaD)]4
Sildenafil as Needed [S(PRN)]5
Tadalafil as Needed [T(PRN)]2

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"Question 3 I Felt the Drug Was in Control of my Erections Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"

Scores for Question 3 range from 0 (not at all) to 4 (extremely). (NCT00734604)
Timeframe: 8 weeks of each treatment

Interventionunits on a scale (Mean)
Tadalafil Once a Day [T(OaD)]1.99
Sildenafil as Needed [S(PRN)]2.28
Tadalafil as Needed [T(PRN)]2.50

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Change From Baseline to Endpoint in the Time Concerns Domain of PAIRS

The PAIRS is a self-administed scale that assesses the broader psychological and interpersonal outcomes associated with erectile dysfunction and its treatment. Time Concerns score is the average of responses on 8 PAIRS item scores. Time Concerns scores range from 1 (strongly disagree) to 4 (strongly agree). Higher scores are indicative of greater sexual self-confidence. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]2.420.00
Tadalafil as Needed [T(PRN)]2.42-0.17
Tadalafil Once a Day [T(OaD)]2.43-0.30

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Change From Baseline to Endpoint in the Erectile Function Domain of the International Index of Erectile Function (IIEF)

Self-reported erectile function over the past 4 weeks. Scores range from 0 (low or no erectile function) to 5 (high erectile function) on 6 questions (1-5, 15 of the IIEF). Total Erectile Function Domain scores range from 0 to 30. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]15.409.70
Tadalafil as Needed [T(PRN)]15.559.54
Tadalafil Once a Day [T(OaD)]15.608.68

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Change From Baseline to Endpoint in the Spontaneity Domain of PAIRS

The PAIRS is a self-administed scale that assesses the broader psychological and interpersonal outcomes associated with erectile dysfunction and its treatment. Spontaneity score is the average of responses on 9 PAIRS item scores. Spontaneity scores range from 1 (strongly disagree) to 4 (strongly agree). Higher scores are indicative of greater spontaneity. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]3.07-0.05
Tadalafil as Needed [T(PRN)]3.070.07
Tadalafil Once a Day [T(OaD)]3.060.10

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Change From Baseline to Endpoint in the Self-Esteem And Relationship (SEAR) Questionnaire Transformed Total Score

Measures improvement in self-esteem and relationship satisfaction. Questionnaire consists of two domains, Sexual Relationship (items 1-8) and Confidence (items 9-14). Overall score is transformed onto a 0 (least favorable) to 100 (most favorable) scale. Overall score was calculated from two domains and subscales scores. (NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]50.5022.87
Tadalafil as Needed [T(PRN)]50.6924.13
Tadalafil Once a Day [T(OaD)]50.2822.94

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Change From Baseline to Endpoint in the Proportion of Days With at Least One Morning Erection

(NCT00734604)
Timeframe: baseline, 8 weeks of each treatment

,,
Interventionproportion of days (Mean)
BaselineChange from Baseline
Sildenafil as Needed [S(PRN)]0.270.11
Tadalafil as Needed [T(PRN)]0.280.20
Tadalafil Once a Day [T(OaD)]0.280.26

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Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Score at Endpoint

EDITS is a questionnaire-based inventory capturing a participant's subjective evaluation of treatment for the participant's erection problems. All items on the 11-item Patient EDITS were scored from zero (no satisfaction or dissatisfaction) to four (high satisfaction). The EDITS Summary Score (transformed) is obtained by adding each individual score for all questions, dividing by the number of questions, and multiplying by 25, so that EDITS scores could range from a low of 0 (extremely low treatment satisfaction) to a high of 100 (extremely high treatment satisfaction). (NCT00734604)
Timeframe: 8 weeks of each treatment

Interventionunits on a scale (Mean)
Tadalafil Once a Day [T(OaD)]75.81
Sildenafil as Needed [S(PRN)]75.68
Tadalafil as Needed [T(PRN)]79.50

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"Question 1 I Felt as if I Did Not Have ED Score of the Patient Perception and Feelings Questions (PPF-Q) at Endpoint"

Scores for Question 1 range from 0 (not at all) to 4 (extremely). (NCT00734604)
Timeframe: 8 weeks of each treatment

Interventionunits on a scale (Mean)
Tadalafil Once a Day [T(OaD)]1.83
Sildenafil as Needed [S(PRN)]1.78
Tadalafil as Needed [T(PRN)]1.77

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Beta Cell Function

Beta cell function as measured during a frequently sampled IV glucose tolerance test (NCT00750308)
Timeframe: 3 hours

InterventionmicroU/mM (Mean)
Placeb Treatment241.2
Ramipril Treatment232.3
Tadalafil Treatment292.1
Combination Treatment287.6

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Insulin Sensitivity

As assessed using IV glucose tolerance test and calculated using Min Mod units mU/mm (NCT00750308)
Timeframe: three weeks

Intervention(mU/L)-1x(min)-1xL (Mean)
Placebo Treatment2.21
Ramipril Treatment1.76
Tadalafil Treatment1.88
Combination Treatment1.76

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Change From Baseline in Postvoid Residual Volume (PVR) at 54-Week Endpoint

Post residual volume (PVR) is measured by ultrasound at regular intervals. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionmilliliter (Mean)
Tadalafil 2.5 mg-5.7
Tadalafil 5 mg-1.9
Placebo-5.5

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Change From Baseline in Postvoid Residual Volume (PVR) at 12-Week Endpoint

Postvoid residual volume (PVR) is measured by ultrasound at regular intervals. (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionmilliliters (Mean)
Tadalafil 2.5 mg-9.41
Tadalafil 5 mg-5.15
Placebo-4.72

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Tadalafil Pharmacokinetics in Japanese Men: Plasma Concentration Measurement

Plasma from participants in the tadalafil treatment groups were assayed using a validated liquid chromatographic/mass spectrometric (LC/MS) method. (NCT00783094)
Timeframe: Baseline, 12 weeks

,
Interventionnanogram/milliliter (Geometric Mean)
0-6 hours (n=225, 200)6-12 hours (n=72, 72)12-24 hours (n=102, 106)24-48 hours (n=11, 8)
Tadalafil 2.5 mg86.068.757.543.5
Tadalafil 5 mg16914093.675.2

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Number of Participants With Adverse Events During 42 Weeks of Open-Label Treatment

A listing of Adverse Events are reported in the Reported Adverse Event Section. (NCT00783094)
Timeframe: End of 12 weeks of double-blind through 54 weeks

,,
Interventionparticipants (Number)
Serious Adverse EventsNon-Serious Adverse Events
Placebo494
Tadalafil 2.5 mg381
Tadalafil 5 mg481

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Number of Participants With Adverse Events During 12 Weeks of the Study

A listing of Adverse Events are reported in the Reported Adverse Event Section. (NCT00783094)
Timeframe: Baseline through 12 weeks

,,
Interventionparticipants (Number)
Serious Adverse EventsNon-Serious Adverse Events
Placebo153
Tadalafil 2.5 mg252
Tadalafil 5 mg254

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Change From Baseline in Blood Pressure During at 54-Week Endpoint

(NCT00783094)
Timeframe: Baseline, 54 weeks

,,
Interventionmillimeters of mercury (mmHg) (Mean)
Systolic blood pressureDiastolic blood pressure
Placebo-0.5-1.3
Tadalafil 2.5 mg-2.1-1.6
Tadalafil 5 mg-1.2-2.9

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Change From Baseline in Blood Pressure at 12-Week Endpoint

(NCT00783094)
Timeframe: Baseline, 12 weeks

,,
InterventionmmHg (Mean)
Systolic Blood PressureDiastolic Blood Pressure
Placebo-0.5-0.9
Tadalafil 2.5 mg-2.0-0.7
Tadalafil 5 mg-3.4-2.9

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Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 12-Week Endpoint

Uroflowmetry was assessed by Qmax, defined as the peak urine flow rate (measured in mL/second using a standard calibrated flowmeter). (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionmilliliters per second (Least Squares Mean)
Tadalafil 2.5 mg0.7
Tadalafil 5 mg0.6
Placebo1.4

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Change From Baseline in the International Prostate Symptom Score (IPSS) Total Score at 54-Week Endpoint

The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg-5.2
Tadalafil 5 mg-5.4
Placebo-6.2

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Change From Baseline in Sitting Heart Rate at 54-Week Endpoint

(NCT00783094)
Timeframe: Baseline, 54-weeks

Interventionbeats per minute (bpm) (Mean)
Tadalafil 2.5 mg1.4
Tadalafil 5 mg0.4
Placebo2.1

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Change From Baseline in Overactive Bladder Symptom Score (OABSS) at 12-Week Endpoint

The OABSS is a four-symptom questionnaire to assess overactive bladder (OAB) symptoms: daytime frequency, nighttime frequency, urgency, and urgency incontinence. Scores range from 0 - 15, with higher scores indicating more severe OAB symptoms. (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-0.7
Tadalafil 5 mg-0.8
Placebo-0.7

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Change From Baseline in IPSS Quality of Life (QoL) Index at 54-Week Endpoint

Assessment of quality of life (QOL) by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible). (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg-0.8
Tadalafil 5 mg-1.0
Placebo-0.9

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Change From Baseline in IPSS Quality of Life (QoL) Index at 12-Week Endpoint

Assessment of quality of life (QOL) by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible). (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-0.5
Tadalafil 5 mg-0.7
Placebo-0.4

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Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 54-Week Endpoint

IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (not at all) to 5 (frequent obstructive symptoms), thus the 4 questions of the obstructive score range from 0 to 20. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg-3.4
Tadalafil 5 mg-3.7
Placebo-4.3

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Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 12-Week Endpoint

IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (not at all) to 5 (frequent obstructive symptoms), thus the 4 questions of the obstructive score range from 0 to 20. (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-2.9
Tadalafil 5 mg-3.3
Placebo-2.4

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Change From Baseline in International Prostate Symptom Score (IPSS) Total Score at 12-Week Endpoint

The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-4.5
Tadalafil 5 mg-4.9
Placebo-3.8

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Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 54-Week Endpoint

IPSS storage (irritative) subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores range from 0 (not at all) to 5 (frequent irritative symptoms), thus the 3 questions of the irritative subscore range from 0 to 15. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg-1.9
Tadalafil 5 mg-1.6
Placebo-1.8

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Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 12-Week Endpoint

IPSS storage (irritative) subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores range from 0 (not at all) to 5 (frequent irritative symptoms), thus the 3 questions of the irritative subscore range from 0 to 15. (NCT00783094)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-1.6
Tadalafil 5 mg-1.6
Placebo-1.4

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Change From Baseline in Overactive Bladder Symptom Score (OABSS) at 54-Week Endpoint

The OABSS is a four-symptom questionnaire to assess overactive bladder (OAB) symptoms: daytime frequency, nighttime frequency, urgency, and urgency incontinence. Scores range from 0 - 15, with higher scores indicating more severe OAB symptoms. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg-0.9
Tadalafil 5 mg-1.0
Placebo-0.9

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Change From Baseline in Sitting Heart Rate at 12-Week Endpoint

(NCT00783094)
Timeframe: Baseline, 12 Weeks

Interventionbeats per minute (Mean)
Tadalafil 2.5 mg-0.7
Tadalafil 5 mg-1.2
Placebo0.0

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Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 54-Week Endpoint

Uroflowmetry was assessed by Qmax, defined as the peak urine flow rate (measured in mL/second using a standard calibrated flowmeter). (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionunits on a scale (Mean)
Tadalafil 2.5 mg2.29
Tadalafil 5 mg1.51
Placebo2.01

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Change From Baseline in Prostate Specific Antigen (PSA) at 54-Week Endpoint

Measurement of nanograms of PSA per milliliter (ng/mL) of blood. (NCT00783094)
Timeframe: Baseline, 54 weeks

Interventionmicrogram/liter (Mean)
Tadalafil 2.5 mg0.4
Tadalafil 5 mg0.3
Placebo0.3

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Change From Baseline in Prostate Specific Antigen (PSA) at 12-Week Endpoint

Measurement of nanograms of PSA per milliliter (ng/mL) of blood. (NCT00783094)
Timeframe: Baseline, 12 weeks

InterventionMicrograms per liter (Mean)
Tadalafil 2.5 mg0.26
Tadalafil 5 mg0.09
Placebo0.14

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Raynaud's Condition Score (RCS) Visual Analog Scale (VAS)

The VAS is a 100 millimeter (mm) line where 0 mm (left boundary) represents no difficulty with Raynaud's disease, and 100 mm (right boundary) represents extreme difficulty with Raynaud's disease. The subject makes a vertical mark on the VAS to indicate difficulty experienced that day with Raynaud's disease. The RCS is the distance from the left boundary to the vertical mark in mm. Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

Interventionmillimeters (Median)
Pre-treatment38.5
Week 4 of Treatment9
Pre-placebo35
Week 4 of Placebo26

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Raynaud Severity Visual Analog Score (VAS)

The VAS is a 100 millimeter (mm) line where 0 mm (left boundary) represents Raynaud's disease of low severity, and 100 mm (right boundary) represents extremely severe Raynaud's disease. The subject makes a vertical mark on the VAS to indicate the severity of Raynaud's disease over the past two weeks. The Raynaud's severity score is the distance from the left boundary to the vertical mark in mm. Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

Interventionmillimeters (Median)
Pre-treatment39
Week 4 of Treatment16.5
Pre-placebo51.5
Week 4 of Placebo37

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Number of Raynaud's Phenomenon Attacks Per Day

Subjects kept a daily record of the number of Raynaud's phenomenon attacks they experienced per day. Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

InterventionRaynaud's attacks per day (Median)
Pre-treatment2.4
Week 4 of Treatment1.1
Pre-placebo2.0
Week 4 of Placebo2.3

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Duration of Raynaud's Phenomenon Attacks

Subjects kept a daily record of the number of Raynaud's phenomenon attacks they experienced per day and the duration of each attack. Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

Interventionminutes (Median)
Pre-treatment5.7
Week 4 of Treatment11.4
Pre-placebo1.2
Week 4 of Placebo14.2

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Digital Blood Pressure

Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

Interventionmm Hg (Median)
Pre-treatment97
Week 4 of Treatment80
Pre-placebo84
Week 4 of Placebo80

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Capillary Diameter

Results are reported from data collected at Baseline/Week 0, Week 4, Week 5, and Week 9 visits. In subjects receiving tadalafil followed by placebo: Baseline/Week 0 data is Pre-treatment, Week 4 data corresponds to Week 4 of treatment, Week 5 data is Pre-placebo, and Week 9 data corresponds to Week 4 of placebo. In subjects receiving placebo followed by tadalafil: Baseline/Week 0 data is Pre-placebo, Week 4 data corresponds to Week 4 of placebo, Week 5 data is Pre-treatment, and Week 9 data corresponds to Week 4 of treatment. (NCT00822354)
Timeframe: 9 weeks

Interventionmicrometers (Median)
Pre-treatment9.3
Week 4 of Treatment10
Pre-placebo10.7
Week 4 of Placebo10

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Change From Baseline to 12 Weeks, International Index of Erectile Function (IIEF)- Erectile Function (EF) Domain Scores

Self-reported EF. Scores range from 0 (low or no EF) to 5 (high EF) on 6 questions (1-5, 15 of the IIEF). EF Domain scores range from 0 to 30. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil6.7
Placebo2.0

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Change From Baseline to 12 Weeks, Postvoid Residual (PVR) Volume

The amount of urine remaining in the bladder after void completion. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionmL (Mean)
Tadalafil8.8
Placebo4.5

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Change From Baseline to 12 Weeks, Peak Flow Rate (Qmax) by Uroflowmetry

Qmax was defined as the peak urine flow rate (measured in milliliters per second [mL/sec] using standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 milliliters (mL) and the voided volume (Vcomp) was >=125 mL. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionmL/sec (Mean)
Tadalafil1.6
Placebo1.1

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Clinical Global Impression of Improvement (CGI-I), Number of Participants in 7 Response Categories

Measures clinician's perception of patient improvement at the time of assessment compared with the start of treatment. Scores range from 1 (very much better) to 7 (very much worse). (NCT00827242)
Timeframe: 12 weeks

,
InterventionParticipants (Number)
7-Very Much Worse6-Much Worse5-A Little Worse4-No Change3-A Little Better2-Much Better1-Very Much Better
Placebo02105955257
Tadalafil05436583913

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Patient Global Impression of Improvement (PGI-I), Number of Participants in 7 Response Categories

A scale that measures the patient's perception of improvement at the time of assessment compared with the start of treatment. The score ranges from 1 (very much better) to 7 (very much worse). (NCT00827242)
Timeframe: 12 weeks

,
InterventionParticipants (Number)
7-Very Much Worse6-Much Worse5-A Little Worse4-No Change3-A Little Better2-Much Better1-Very Much Better
Placebo0645753326
Tadalafil15430574612

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Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS)

The IPSS Total Score is obtained by combining the scores of the responses to Question 1 through Question 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-5.6
Placebo-3.6

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Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Nocturia Question

Measures nocturia (the need to get up at night to urinate). Scores range from 0 (few episodes of nocturia) to 5 (frequent episodes of nocturia). LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-0.5
Placebo-0.4

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Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore

IPSS irritative subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores range from 0 (few irritative symptoms) to 5 (frequent irritative symptoms), thus the 3 questions of the irritative subscore range from 0 to 15. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-2.3
Placebo-1.3

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Change From Baseline to 12 Weeks, Mean Flow Rate (Qmean) by Uroflowmetry

Qmean was defined as the mean urine flow rate (measured in mL/sec using standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 mL and the Vcomp was >=125 mL. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionmL/sec (Mean)
Tadalafil0.6
Placebo0.5

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Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore

IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (few obstructive symptoms) to 5 (frequent obstructive symptoms), thus the 4 questions of the obstructive score range from 0 to 20. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-3.3
Placebo-2.3

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Change From Baseline to 12 Weeks, International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index

Assessment of QoL by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible). LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-1.0
Placebo-0.7

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Change From Baseline to 12 Weeks, Benign Prostatic Hyperplasia (BPH) Impact Index

The BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-1.8
Placebo-1.3

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Change From Baseline to 12 Weeks, Voided Volume (Vcomp) by Uroflowmetry

Vcomp was defined as the volume of urine voided (measured in mL using standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 mL and the Vcomp was >=125 mL. (NCT00827242)
Timeframe: Baseline, 12 weeks

InterventionmL (Mean)
Tadalafil16.9
Placebo3.9

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Change From Baseline to 4 Weeks, Benign Prostatic Hyperplasia (BPH) Impact Index

The BPH Impact Index (BII) is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 4 weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-1.8
Placebo-1.2

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Change From Baseline to 4 Weeks, International Prostate Symptom Score (IPSS)

The IPSS Total Score is obtained by combining the scores of the responses to Question 1 through Question 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 4 Weeks

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-5.3
Placebo-3.5

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Change From Baseline to 1 Week, International Prostate Symptom Score (IPSS)

The IPSS Total Score is obtained by combining the scores of the responses to Question 1 through Question 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. LS mean of change from baseline to endpoint is from an ANCOVA. The model includes terms for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction and treatment-by-region interaction. (NCT00827242)
Timeframe: Baseline, 1 week

InterventionUnits on a Scale (Least Squares Mean)
Tadalafil-3.4
Placebo-2.7

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Sexual Encounter Profile Diary Question Number 1, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of yes responses to the Sexual Encounter Profile Diary question number 1: Were you able to achieve at least some erection (some enlargement of the penis)? Data are presented as the mean percentage of participants who answered yes." (NCT00833638)
Timeframe: Baseline and 14 days double-blind period

Interventionpercentage of participants (Least Squares Mean)
Tadalafil 2.5 mg1.97
Tadalafil 5 mg2.74
Placebo-10.06

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Sexual Encounter Profile Diary Question Number 2, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of yes responses to the Sexual Encounter Profile Diary question number 2: Were you able insert your penis into your partner's vagina? Data are presented as the mean percentage of participants who answered yes." (NCT00833638)
Timeframe: Baseline and 14 days double-blind period

Interventionpercentage of participants (Least Squares Mean)
Tadalafil 2.5 mg8.11
Tadalafil 5 mg13.12
Placebo-7.29

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Sexual Encounter Profile Diary Question Number 3, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of yes responses to the Sexual Encounter Profile Diary question number 3: Did your erection last long enough for you to have successful intercourse? Data are presented as the mean percentage of participants who answered yes." (NCT00833638)
Timeframe: Baseline and 14 days double-blind period

Interventionpercentage of participants (Least Squares Mean)
Tadalafil 2.5 mg15.67
Tadalafil 5 mg21.94
Placebo1.40

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Sexual Encounter Profile Diary Question Number 4, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of yes responses to the Sexual Encounter Profile Diary question number 4: Were you satisfied with the hardness of your erection? Data are presented as the mean percentage of participants who answered yes." (NCT00833638)
Timeframe: Baseline and 14 days double-blind period

Interventionpercentage of participants (Least Squares Mean)
Tadalafil 2.5 mg20.94
Tadalafil 5 mg28.50
Placebo6.70

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Earliest Onset Day Measured by Cumulative Percentage of Participants With Yes Response to Sexual Encounter Profile Diary Question 3

"Cumulative percentage of participants achieving successful intercourse, as measured by yes responses to Sexual Encounter Profile diary question 3 (SEP3). SEP3 asks if the participant's erection lasted long enough to have successful intercourse." (NCT00833638)
Timeframe: 4 days during double-blind period

,,
Interventioncumulative percentage of participants (Number)
<= day 4<= day 3<= day 2<= day 1
Placebo47.242.336.628.5
Tadalafil 2.5 mg54.549.142.028.6
Tadalafil 5 mg62.255.048.625.2

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Sexual Encounter Profile Diary Question 3, Daily Cumulative Percentage of Successful Intercourse Attempts

"Assessed was the cumulative precentage of successful intercourse attempts (successful attempts relative to the total number of intercourse attempts) over the 14-day double-blind treatment period. A successful attempt was defined by a yes response to the sexual encounter profile diary question #3: Did your erection last long enough for you to have successful intercourse? Data are presented as the proportion of intercourse attempts for which participants answered yes relative to the total number of intercourse attempts. Total number of attempts = TNA." (NCT00833638)
Timeframe: 14 days during double-blind period

,,
Interventionpercentage of total number of attempts (Number)
<=day14 (TNA: n=905; n=813; n=781)<=day13 (TNA: n=877; n=777; n=755)<=day12 (TNA: n=827; n=730; n=711)<=day11 (TNA: n=774; n=678; n=668)<=day10 (TNA: n=726; n=626; n=625)<=day9 (TNA: n=668; n=574; n=572)<=day8 (TNA: n=608; n=534; n=523)<=day7 (TNA: n=563; n=483; n=481)<=day6 (TNA: n=505; n=439; n=435)<=day5 (TNA: n=464; n=402; n=396)<=day4 (TNA: n=412; n=350; n=352)<=day3 (TNA: n=324; n=265; n=262)<=day2 (TNA: n=214; n=179; n=175)<=day1 (TNA: n=109; n=83; n=83)
Placebo30.931.230.830.730.629.829.628.827.927.426.227.228.032.1
Tadalafil 2.5 mg45.144.544.043.241.940.239.538.737.436.637.135.535.838.6
Tadalafil 5 mg46.646.245.944.944.243.742.842.441.641.440.938.538.933.7

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Sexual Encounter Profile Diary Question Number 5, Change From Baseline to Post Baseline During the Double-blind Period in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of yes responses to the Sexual Encounter Profile Diary question number 5: Were you satisfied overall with this sexual experience? Data are presented as the mean percentage of participants who answered yes." (NCT00833638)
Timeframe: Baseline and 14 days double-blind period

Interventionpercentage of participants (Least Squares Mean)
Tadalafil 2.5 mg20.45
Tadalafil 5 mg25.60
Placebo6.52

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Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses in the Double-blind Period and the Open-label Period for Participants Who Were Assigned to Tadalafil 5 mg in the Double-blind Treatment Period

"Assessed were percentages of successful intercourse attempts relative to the total number of intercourse attempts over the 14-day open-label treatment period compared with the 14-day double-blind treatment period by dose group during the double-blind treatment period. A successful attempt was defined by a yes response to the sexual encounter profile diary question #3: Did your erection last long enough for you to have successful intercourse?" (NCT00833638)
Timeframe: 14-day double-blind and 14-day open-label

Interventionpercentage successful attempts (Mean)
Tadalafil 5 mg Double-blind49.54
Tadalafil 5 mg Open-label67.70

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Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses in the Double-blind Period and the Open-label Period for Participants Who Were Assigned to Tadalafil 2.5 mg in the Double-blind Treatment Period

"Assessed were percentages of successful intercourse attempts relative to the total number of intercourse attempts over the 14-day open-label treatment period compared with the 14-day double-blind treatment period by dose group during the double-blind treatment period. A successful attempt was defined by a yes response to the sexual encounter profile diary question #3: Did your erection last long enough for you to have successful intercourse?" (NCT00833638)
Timeframe: 14-day double-blind and 14-day open-label

Interventionpercentage successful attempts (Mean)
Tadalafil 2.5 mg Double-blind46.11
Tadalafil 5 mg Open-label68.33

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Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses During the Double-blind and Open-label Periods for Participants Who Were Assigned to Placebo in the Double-blind Treatment Period

"Assessed were percentages of successful intercourse attempts relative to the total number of intercourse attempts over the 14-day open-label treatment period compared with the 14-day double-blind treatment period by dose group during the double-blind treatment period. A successful attempt was defined by a yes response to the sexual encounter profile diary question #3: Did your erection last long enough for you to have successful intercourse?" (NCT00833638)
Timeframe: 14 days double-blind and 14 days open-label

Interventionpercentage successful attempts (Mean)
Placebo Double-blind32.21
Tadalafil 5 mg Open-label68.27

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Sexual Encounter Profile Diary Question 3, Percentages of Yes Responses During the Double-blind Period and the Open-label Period for Participants Who Didn't Respond to Tadalafil 2.5 mg During Double-blind Period

"Assessed were percentages of successful intercourse attempts relative to the total number of intercourse attempts in both treatment periods. A successful attempt was defined by a yes response to the sexual encounter profile diary question #3: Did your erection last long enough for you to have successful intercourse?" (NCT00833638)
Timeframe: 14 days double-blind and 14 days open-label

Interventionpercentage successful attempts (Mean)
Tadalafil 2.5 mg Double-blind32.51
Tadalafil 5 mg Open-label57.62

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Sexual Encounter Profile Diary Question 3, the Overall Distribution of Time to Onset by Yes Responses

"Assessed was the median time to onset of efficacy (day when 50% of participants have had at least 1 successful intercourse attempt) within the first 4 days of therapy based on a yes response to the sexual encounter profile diary question 3: Did your erection last long enough for you to have successful intercourse? Data are based on participants who responded yes. For the placebo group, onset of efficacy was not reached within the first 4 days of therapy, therefore, the analysis timeframe was expanded for this group to determine the median time to onset of efficacy." (NCT00833638)
Timeframe: 4 days double-blind period

Interventiondays (Median)
Tadalafil 2.5 mg4.0
Tadalafil 5 mg3.0
Placebo6.0

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Change From Baseline to 12 Week Endpoint in Total and Subdomain Scores of the Self-Esteem and Relationship (SEAR) Questionnaire

SEAR measures improvement in self-esteem and relationship satisfaction. Questionnaire consists of two domains, Sexual Relationship (items 1-8) and Confidence (items 9-14). All questions except negatively worded questions 8 and 11 are scored from 1=almost never/never to 5=almost always/always. Questions 8 and 11 were reverse scored, thus a higher score signifies a more favorable response for all 14 items. Overall score is transformed into a 0 (least favorable) to 100 (most favorable) scale. (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionunits on a scale (Mean)
Total (Baseline)Total (Change)Sexual Relationship Domain (Baseline)Sexual Relationship Domain (Change)Confidence Domain (Baseline)Confidence Domain (Change)Self-Esteem Domain (Baseline)Self-Esteem Domain (Change)Overall Relationship Domain (Baseline)Overall Relationship Domain (Change)
Placebo47.98.343.99.753.16.548.59.362.30.9
Tadalafil47.320.443.023.453.116.550.519.258.211.0

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Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Percentage Volumetric Change

NPT was measured using electrobioimpedance volumetric assessment (NEVA). The NEVA device measures a man's erections during the night. The percent of volume change of the penis during erections is measured and recorded for each erection. Data presented are mean percentage of volumetric change from baseline to Week 12. (NCT00836693)
Timeframe: Baseline, Week 12

Interventionpercent of volumetric change (Mean)
Tadalafil-5.96
Placebo-50.30

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The Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire at 12 Week Endpoint

The subject questionnaire consists of 11 questions. Each question is rated on a scale of 0 (extremely low treatment satisfaction) to 4 (extremely high treatment satisfaction). The EDITS summary score will be obtained by adding each individual result for all questions, dividing by the number of questions answered (mean satisfaction score), and multiplying by 25, thus obtaining a score that ranges from 0 (extremely low treatment satisfaction) to 100 (extremely high satisfaction). (NCT00836693)
Timeframe: Week 12

Interventionunits on a scale (Mean)
Tadalafil72.8
Placebo52.7

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"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 1 Percentage of Yes Responses"

"Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Question 1. Were you able to achieve at least some erection (some enlargement of the penis)? Data are presented as the mean percentage of yes responses per participant." (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionpercentage of yes responses (Mean)
BaselineWeek 12 Change
Placebo74.29.5
Tadalafil80.812.5

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"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 4 Percentage of Yes Responses"

"Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Question 4. Were you satisfied with the hardness of your erection? Data are presented as the mean percentage of yes responses per participant." (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionpercentage of yes responses (Mean)
BaselineWeek 12 Change
Placebo14.618.3
Tadalafil11.744.1

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Change From Baseline to 12 Week Endpoint in the Frequency of Spontaneous Morning Erections Captured by Patient Diary

The morning erection diary allows the participant to record whether he experienced an erection on waking. The participant is to complete the morning erection diary every morning during the run-in, treatment and follow-up periods. The percentage of mornings the participant reported an erection is analysed. (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionpercent (Mean)
Baseline (n=145, n=67)Week 12 Change (n=145, n=66)
Placebo28.911.9
Tadalafil31.027.5

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Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Number of Erectile Events Per Night

NPT was measured using electrobioimpedance volumetric assessment (NEVA). The NEVA device measures a man's erections during the night. The man wears the device for three nights prior to visit 2 (baseline), visit 5 (end of randomised treatment) and visit 6 (end of follow-up). Data are entered for the 2 nights prior to the visit. During the night the man may have multiple erections. The number of erections is recorded. (NCT00836693)
Timeframe: Baseline, Week 12

,
InterventionNumber of events per night (Mean)
Baseline (n=122, n=63)Week 12 Change (n=96, n=49)
Placebo2.44-0.09
Tadalafil2.75-0.11

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Change From Baseline to 12 Week Endpoint in Nocturnal Penile Tumescence (NPT) Pattern: Duration of Erectile Events Per Night

NPT was measured using electrobioimpedance volumetric assessment (NEVA). The NEVA device measures a man's erections during the night. The duration of erections are measured and recorded. Data presented are the duration of erectile events at baseline and the change from baseline to Week 12. (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionminutes (Mean)
Baseline (n=104, n=56)Week 12 Change (n=65, n=33)
Placebo26.372-0.398
Tadalafil28.487-1.553

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Sexual Desire (SD)

Self-reported overall satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 2 questions of the IIEF-SD domain range from 0 to 10. (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionunits on a scale (Mean)
BaselineWeek 12 Change
Placebo6.6-0.1
Tadalafil6.70.5

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Overall Satisfaction (OS)

Self-reported overall satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction to 5 (high satisfaction), thus the 2 questions of the IIEF-OS domain range from 0 to 10. (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionunits on a scale (Mean)
BaselineWeek 12 Change
Placebo5.10.8
Tadalafil5.22.0

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Orgasmic Functions (OF)

Self-reported overall satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction) to 5 (high satisfaction), thus the 2 questions of the IIEF-OF domain range from 0 to 10. (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionunits on a scale (Mean)
BaselineWeek 12 Change
Placebo7.20.5
Tadalafil6.52.0

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF), Intercourse Satisfaction (IS)

Self-reported intercourse satisfaction over the past 4 weeks. Scores range from 0 (low/no satisfaction) to 5 (high satisfaction), thus the 3 questions of the IIEF-IS domain range from 0 to 15. (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionunits on a scale (Mean)
BaselineWeek 12 Change
Placebo7.61.5
Tadalafil8.22.1

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Change From Baseline in the International Index of Erectile Function - Erectile Function Domain (IIEF-EF) at Week 12

Self-reported erectile function over the past 4 weeks. Scores range from 0 (low or no erectile function) to 5 (high erectile function) on 6 questions (1-5, 15 of the IIEF). Total Erectile Function Domain scores range from 0 to 30. (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionunits on a scale (Mean)
BaselineWeek 12 Change
Placebo16.03.3
Tadalafil15.57.3

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Change From Baseline in Question 2 of the Patient Sexual Encounter Profile (SEP) Diary at Week 12 in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Question 2. Were you able to insert your penis into your partner's vagina? Data are presented as the mean percentage of yes responses per participant." (NCT00836693)
Timeframe: Baseline, Week 12

,
Interventionpercentage of yes responses (Mean)
BaselineWeek 12 Change
Placebo59.911.6
Tadalafil60.123.2

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Sexual Encounter Profile (SEP) Diary, Question 3 Change From Baseline to Week 12 in Percentage of Yes Responses

"Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Question 3. Did your erection last long enough for you to have successful intercourse? Data are presented as the mean percentage of yes responses per participant." (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionpercentage of yes responses (Mean)
BaselineWeek 12 Change
Placebo32.219.3
Tadalafil28.239.4

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"Change From Baseline to 12 Week Endpoint in Sexual Encounter Profile (SEP) Question 5 Percentage of Yes Responses"

"Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Question 5. Were you satisfied overall with this sexual experience? Data are presented as the mean percentage of yes responses per participant." (NCT00836693)
Timeframe: Baseline, 12 weeks

,
Interventionpercentage of yes responses (Mean)
BaselineWeek 12 Change
Placebo12.918.5
Tadalafil10.343.2

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Global Assessment Question (GAQ) Question 2 at 12 Week Endpoint

GAQ Question 2: Choose the one number which best describes how you perceive your sexual life is now, compared to how it was before you began taking medication in this study. Responses range from 1=very much better to 7=very much worse. (NCT00836693)
Timeframe: Week 12

,
Interventionparticipants (Number)
Very Much BetterMuch BetterLittle BetterNo ChangeA Little WorseMuch WorseVery Much WorseMissing
Placebo51117274302
Tadalafil404928173414

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Global Assessment Question (GAQ) Question 1 at 12 Week Endpoint

GAQ Question 1: Choose the one number which best describes how you perceive your ability to achieve and maintain your erections now, compared to how it was before you began taking medication in this study. Responses range from 1=very much better to 7=very much worse. (NCT00836693)
Timeframe: Week 12

,
Interventionparticipants (Number)
Very Much BetterMuch BetterLittle BetterNo ChangeA Little WorseMuch WorseVery Much WorseMissing
Placebo7819245312
Tadalafil494129145424

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Number of Participants Experiencing Adverse Events

Assessment of Treatment-related Side Effects. Number of participants experiencing adverse events (NCT00843635)
Timeframe: From Day 1 to Day 20

Interventionparticipants (Number)
Arm A - 10mg4
Arm B - Tadalafil 20mg10
Arm C - Placebo3

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Ratio of MDSC Concentration in the Blood

Ratio of the number of Myeloid Derived Suppressor Cells (MDSC) in the Blood, per treatment group, from Baseline to End of Treatment at Time of Surgery. (NCT00843635)
Timeframe: Baseline, End of Treatment at time of Surgery

Interventionratio from baseline (Median)
Arm A - Tadalafil 10mg0.7680
Arm B - Tadalafil 20mg0.7919
Arm C - Placebo0.9876

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Ratio of T-reg Cell Concentration in the Blood

Ratio of the number of regulatory T cells in the blood, per treatment group, from Baseline to End of Treatment at Time of Surgery.. (NCT00843635)
Timeframe: Baseline, End of Treatment at Time of Surgery

Interventionratio from baseline (Median)
Arm A - Tadalafil 10mg0.7776
Arm B - Tadalafil 20mg0.6789
Arm C - Placebo0.8421

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Ratio of Tumor-specific T-cell Concentration in the Blood

Ratio of the number of tumor specific T cells in the blood, per treatment group, from Baseline to End of Treatment at Time of Surgery. (NCT00843635)
Timeframe: Baseline, End of Treatment at Time of Surgery

Interventionratio from baseline (Median)
Arm A - Tadalafil 10mg1.7401
Arm B - Tadalafil 20mg1.9020
Arm C - Placebo1.0933

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International Prostate Symptom Score (IPSS) Change From Baseline

Change from baseline to endpoint in IPSS Score. The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT00848081)
Timeframe: Baseline, 12 Weeks

,
Interventionunits on a scale (Mean)
BaselineChange from Baseline
Placebo13.3-1.49
Tadalafil13.87-2.28

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Number of Participants With Positive Orthostatic Vital Signs Test; Shift From Any Pre-Randomization to Any Post-Randomization Visit

A positive orthostatic test is defined as at least one of the following 4 criteria being met at any pre-randomization or post-randomization visit: (1) reduction in systolic blood pressure of >= 20 mmHg from the supine to standing position;(2)reduction in diastolic blood pressure of >=10 mmHg from the supine to standing position;(3)increase in heart rate of >= 20 bpm from the supine to standing position; or (4)Unable to remain standing. A negative orthostatic test is defined as none of the above 4 criteria (1, 2, 3, or 4) being met at any pre-randomization or post-randomization visit. (NCT00848081)
Timeframe: Baseline through 12 Weeks

,
InterventionParticipants (Number)
Positive Pre-Random. to Negative Post-Random.Negative Pre-Random. to Positive Post-Random.Positive Pre-Random. to Positive Post-Random.Negative Pre-Random. to Negative Post-Random.
Placebo222114101
Tadalafil151916106

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Postvoid Residual Volume (PVR) Change From Baseline

Change from baseline to endpoint in PVR volume. PVR is obtained by measuring with ultrasound the remaining urine in the bladder after urination. (NCT00848081)
Timeframe: Baseline, 12 Weeks

,
Interventionmilliliters (Mean)
Baseline valuesChange from Baseline
Placebo70.7-1.9
Tadalafil80.3-8.1

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Uroflowmetry (Qmax) Change From Baseline

Change from baseline to endpoint in Qmax. Qmax is defined as the peak urine flow rate (measured in milliliters per second [mL/second] using standard calibrated flowmeter). (NCT00848081)
Timeframe: Baseline, 12 Weeks

,
Interventionmilliliters per second (Mean)
BaselineChange from Baseline
Placebo12.80.6
Tadalafil11.80.6

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Number of Men With Treatment-emergent Dizziness

The primary safety measure is the proportion (reported in numbers) of subjects experiencing treatment-emergent dizziness to include the Medical Dictionary for Regulatory Activities (MedDRA) preferred terms of dizziness, dizziness postural, and procedural dizziness. Treatment-emergent dizziness is defined as any of the predefined terms of dizziness that is first reported or worsens in severity after baseline. (NCT00848081)
Timeframe: Baseline through 12 Weeks

InterventionParticipants (Number)
Placebo9
Tadalafil11

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Change From Baseline in International Index of Erectile Function - Overall Satisfaction Domain at Week 12 Endpoint

Self-reported overall satisfaction over the past 4 weeks. Calculated as the sum of IIEF Questions 13 and 14. Each question is scored from 1 through 5, with a possible total score of 2 through 10. Higher scores represent greater satisfaction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg1.8
Tadalafil 5 mg2.4
Placebo0.5

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Change From Baseline in International Prostate Symptom Score Nocturia Question at Week 12

The IPSS Nocturia question (Question 7) measures the number of times needed to get up at night to urinate. Scores range from 0 (none) to 5 (5 or more times). Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-0.5
Tadalafil 5 mg-0.6
Placebo-0.5

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Change From Baseline in Uroflowmetry Parameters - Peak Urine Flow Rate (Qmax) at Week 12 Endpoint

Qmax is defined as the peak urine flow rate (measured in milliliters per second [mL/sec] using standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 milliliters (mL) and the voided volume (Vcomp) was >= 125 mL. (NCT00855582)
Timeframe: Baseline, 12 weeks

InterventionmL/sec (Mean)
Tadalafil 2.5 mg1.7
Tadalafil 5 mg1.6
Placebo1.2

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Change From Baseline in International Index of Erectile Function Question 3 at Week 12 Endpoint

IIEF Question 3 asks how often a subject was able to penetrate his partner over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg0.9
Tadalafil 5 mg1.1
Placebo0.2

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Change From Baseline in International Index of Erectile Function - Intercourse Satisfaction Domain at Week 12 Endpoint

Self-reported intercourse satisfaction over the past 4 weeks. Calculated as the sum of IIEF Questions 6, 7 and 8. Each question is scored from 0 through 5 with a possible total score of 0 through 15. Higher score represent greater satisfaction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg1.6
Tadalafil 5 mg2.0
Placebo0.2

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Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score at Week 12 Endpoint (5 mg)

Self-reported erectile function over the past 4 weeks. Questions 1-5 were scored from 0-5, and Question 15 from 1 to 5. Erectile Function Domain scores range from 1 to 30; lower numerical scores represent greater severity of erectile dysfunction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 5 mg6.5
Placebo1.8

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 5

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 5, Were you satisfied overall with this sexual experience? Data are presented as the mean percentage of yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionpercentage of yes responses (Least Squares Mean)
Tadalafil 2.5 mg23.7
Tadalafil 5 mg38.2
Placebo9.9

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 4 at Week 12 Endpoint

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 4, Were you satisfied with the hardness of your erection? Data are presented as the mean percentage of yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionpercentage of yes responses (Least Squares Mean)
Tadalafil 2.5 mg26.6
Tadalafil 5 mg39.4
Placebo9.6

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Change From Baseline in International Index of Erectile Function Question 4 at Week 12 Endpoint

IIEF Question 4 asks whether how often a subject was able to maintain an erection after penetration over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg0.9
Tadalafil 5 mg1.3
Placebo0.4

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 12 Endpoint (5 mg)

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 3, Did your erection last long enough for you to have successful intercourse? Data are presented as the mean percentage of Yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionpercentage of Yes responses (Least Squares Mean)
Tadalafil 5 mg31.7
Placebo12.0

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 2 at Week 12 Endpoint

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 2, Were you able to insert your penis into your partner's vagina? Data are presented as the mean percentage of yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionpercentage of yes responses (Least Squares Mean)
Tadalafil 2.5 mg21.4
Tadalafil 5 mg25.1
Placebo9.3

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Change From Baseline in Uroflowmetry Parameters - Voided Volume (Vcomp) at Week 12 Endpoint

Vcomp is defined as the volume of urine voided (measures in mL using a standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 milliliters (mL) and the voided volume (Vcomp) was >= 125 mL. (NCT00855582)
Timeframe: Baseline, 12 weeks

InterventionmL (Mean)
Tadalafil 2.5 mg18.5
Tadalafil 5 mg13.3
Placebo11.4

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Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score at Week 12 Endpoint (2.5 mg)

Self-reported erectile function over the past 4 weeks. Questions 1-5 were scored from 0-5, and Question 15 from 1 to 5. Erectile Function Domain scores range from 1 to 30; lower numerical scores represent greater severity of erectile dysfunction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg5.2
Placebo1.8

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Change From Baseline in BPH Impact Index (BII) at Week 12 Endpoint (2.5 mg)

The BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-1.6
Placebo-1.2

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Change From Baseline in Benign Prostatic Hyperplasia (BPH) Impact Index (BII) at Week 12 Endpoint (5 mg)

The BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on scale (Least Squares Mean)
Tadalafil 5 mg-2.1
Placebo-1.2

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 12 Endpoint (2.5 mg)

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 3, Did your erection last long enough for you to have successful intercourse? Data are presented as the mean percentage of yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionpercentage of yes responses (Least Squares Mean)
Tadalafil 2.5 mg24.6
Placebo12.0

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Change From Baseline in International Index of Erectile Function - Erectile Function (IIEF-EF) Domain at Week 4 and Week 8 Endpoint

Self-reported erectile function over the past 4 weeks. Questions 1-5 were scored from 0-5, and Question 15 from 1 to 5. Erectile Function Domain scores range from 1 to 30; lower numerical scores represent greater severity of erectile dysfunction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 4 weeks, 8 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Week 4 Change (n=186, 197, 183)Week 8 Change (n=176, 192, 178)
Placebo1.01.8
Tadalafil 2.5 mg4.24.9
Tadalafil 5 mg6.16.6

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Change From Baseline in Uroflowmetry Parameters - Mean Urine Flow Rate (Qmean) at Week 12 Endpoint

Qmean is defined as the average urine flow rate (measured in milliliters per second [mL/second] using standard calibrated flowmeter). At each visit, a uroflowmetry assessment was considered valid and the data were included in the statistical analyses only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 milliliters (mL) and the voided volume (Vcomp) was >= 125 mL. (NCT00855582)
Timeframe: Baseline, 12 weeks

InterventionmL/sec (Mean)
Tadalafil 2.5 mg1.0
Tadalafil 5 mg0.9
Placebo0.6

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Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12 Endpoint (5 mg)

The total IPSS is obtained by combining the scores of the responses to component questions 1 through 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 5 mg-6.1
Placebo-3.8

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Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12 Endpoint (2.5 mg)

The total IPSS is obtained by combining the scores of the responses to component questions 1 through 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-4.6
Placebo-3.8

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Change From Baseline in Modified IPSS (mIPSS) at Week 2 Endpoint

The Modified IPSS is the total IPSS collected at 2 weeks post-baseline. The total IPSS is obtained by combining the scores of the responses to component questions 1 through 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from ANCOVA. The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 2 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-2.8
Tadalafil 5 mg-4.0
Placebo-2.2

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Change From Baseline in International Prostate Symptom Score Voiding (Obstructive) Subscore at Week 12 Endpoint

IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. The obstructive subscore ranges from 0 to 20 with a higher score representing greater obstruction. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-2.7
Tadalafil 5 mg-3.6
Placebo-2.2

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Change From Baseline in International Prostate Symptom Score Storage (Irritative) Subscore at Week 12 Endpoint

IPSS irritative subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. The irritative subscore ranges from 0 to 15 with a higher score representing more irritative symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-1.9
Tadalafil 5 mg-2.5
Placebo-1.6

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Change From Baseline in International Prostate Symptom Score Quality of Life (QoL) at Week 12 Endpoint

Assessment of quality of life (QoL) by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible). Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil 2.5 mg-0.9
Tadalafil 5 mg-1.0
Placebo-0.8

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Change From Baseline in BPH Impact Index (BII) at Week 4 and 8 Endpoint

The BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 4 weeks, 8 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Week 4 Change (n=186, 197, 183)Week 8 Change (n=175, 192, 177)
Placebo-0.7-1.2
Tadalafil 2.5 mg-1.0-1.4
Tadalafil 5 mg-1.5-1.8

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Change From Baseline in International Prostate Symptom Score (IPSS) at Week 4 and Week 8 Endpoint

The total IPSS is obtained by combining the scores of the responses to component questions 1 through 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction. (NCT00855582)
Timeframe: Baseline, 4 weeks, 8 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Week 4 Change (n=184, 197, 183)Week 8 Change (n=174, 192, 178)
Placebo-2.6-3.8
Tadalafil 2.5 mg-3.4-4.5
Tadalafil 5 mg-5.5-5.8

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Change From Baseline in Yes Responses to Sexual Encounter Profile (SEP) Diary Question 3 at Week 4 and Week 8 Endpoint

"Assessed as the mean change from baseline in the percentage of Yes responses to the SEP diary Question 3, Did your erection last long enough for you to have successful intercourse? Data are presented as the mean percentage of yes responses per the number of sexual attempts for a participant during a study period. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment group, region, baseline covariate, baseline-by-treatment interaction and treatment-by-region interaction." (NCT00855582)
Timeframe: Baseline, 4 weeks, 8 weeks

,,
Interventionpercentage of yes responses (Least Squares Mean)
Week 4 Change (n=180, 190, 180)Week 8 Change (n=172, 187, 171)
Placebo6.210.9
Tadalafil 2.5 mg22.322.9
Tadalafil 5 mg30.731.7

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Clinician Global Impression of Improvement (CGI-I) at Week 12 Endpoint

A scale that measures clinician's rating of the total change in the patient's urinary symptoms at endpoint compared with the start of treatment. Scores range from 1 (very much better) to 7 (very much worse).The data are presented as the number of participants in each of the seven categories: very much better (1); much better (2); a little better (3); no change (4); a little worse (5); much worse (6); very much worse (7). (NCT00855582)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
Placebo1496458453
Tadalafil 2.5 mg0284167567
Tadalafil 5 mg01242607814

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Erectile Function General Assessment Questionnaire (EF-GAQ)

The EF-GAQ consisted of two questions: (1) Has the treatment you have been taking during this study improved your erections? and (2) If yes, has the treatment improved your ability to engage in sexual activity? Each question has a Yes/No response. (NCT00855582)
Timeframe: 12 weeks

,,
Interventionparticipants with yes response (Number)
Question 1Question 2
Placebo7467
Tadalafil 2.5 mg135126
Tadalafil 5 mg155146

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Patient Global Impression of Improvement (PGI-I) at Week 12 Endpoint

A scale that measures the patient's perception of urinary symptoms at endpoint compared with the start of treatment. The score ranges from 1 (very much better) to 7 (very much worse). The data are presented as the number of participants in each of the seven categories: very much better (1); much better (2); a little better (3); no change (4); a little worse (5); much worse (6); very much worse (7). (NCT00855582)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
Placebo14136163376
Tadalafil 2.5 mg031234665713
Tadalafil 5 mg02334796019

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Change From Baseline to 12 Weeks in International Prostate Symptom Score (IPSS) Subscore (Storage [Irritative] and Voiding [Obstructive])

IPSS obstructive subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (few obstructive symptoms) to 5 (frequent obstructive symptoms); 4 questions of the obstructive score range from 0 to 20. IPSS irritative subscore is the sum of Questions 2, 4 and 7 of IPSS questionnaire. Scores range from 0 (no irritative symptoms) to 5 (frequent irritative symptoms); 3 questions of the irritative subscore range from 0 to 15. Least Squares Mean values were controlled for prior alpha blocker use (yes/no), country (Japan/Korea/Taiwan), and baseline value. (NCT00861757)
Timeframe: baseline, 12 weeks

,,,
Interventionunits on a scale (Least Squares Mean)
Voiding (Obstructive) Score (N = 154,151,155,152)Storage (Irritative) Score (N = 154,151,155,152)
0.2 mg Tamsulosin-3.8-1.7
2.5 mg Tadalafil-3.3-1.5
5.0 mg Tadalafil-3.0-1.7
Placebo-1.9-1.1

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Clinician Global Impression of Improvement (CGI-I) at Week 12

The CGI-I measures clinician's perception of patient improvement at the time of assessment compared with the start of treatment. There are 7 categories with scores ranging from 1 (very much better) to 7 (very much worse). The data are presented as the number of participants in each of the 7 categories: very much better (1); much better (2); a little better (3); no change (4); a little worse (5); much worse (6); very much worse (7). (NCT00861757)
Timeframe: 12 weeks

,,,
Interventionparticipants (Number)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
0.2 mg Tamsulosin01319684712
2.5 mg Tadalafil23421673911
5.0 mg Tadalafil01329624810
Placebo0384460307

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Patient Global Impression of Improvement (PGI-I) at Week 12

The PGI-I measures the patient's perception of improvement at the time of assessment compared with the start of treatment. There are 7 categories with scores ranging from 1 (very much better) to 7 (very much worse). The data are presented as the number of participants in each of the 7 categories: very much better (1); much better (2); a little better (3); no change (4); a little worse (5); much worse (6); very much worse (7). (NCT00861757)
Timeframe: 12 weeks

,,,
InterventionParticipants (Number)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
0.2 mg Tamsulosin0142558539
2.5 mg Tadalafil1142662449
5.0 mg Tadalafil10523744010
Placebo23124554324

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Change From Baseline in Benign Prostatic Hyperplasia (PBH) Impact Index (BII) at 12 Weeks

The BII is a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores range from 0 to 13; higher scores represent increased perceived impact of benign prostatic hyperplasia-lower urinary tract symptoms on overall health. Least Squares Mean values were controlled for BPH severity (moderate/severe), prior alpha blocker use (yes/no), country (Japan/Korea/Taiwan) and baseline value. (NCT00861757)
Timeframe: baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.8
2.5 mg Tadalafil-1.1
5.0 mg Tadalafil-1.0
0.2 mg Tamsulosin-1.6

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Change From Baseline in Blood Pressure (Sitting) at 12 Weeks

(NCT00861757)
Timeframe: baseline, 12 weeks

,,,
Interventionmm Hg (Mean)
Systolic Blood PressureDiastolic Blood Pressure
0.2 mg Tamsulosin0.2-0.6
2.5 mg Tadalafil-2.3-2.5
5.0 mg Tadalafil-0.5-1.4
Placebo0.9-0.3

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Change From Baseline in International Prostate Symptom Score (IPSS) Quality of Life (QoL) at 12 Weeks

"Assessment of QoL by urinary symptoms, with scores ranging from 0 (delighted) to 6 (terrible).~Least Squares Mean values were controlled for Benign Prostatic Hyperplasia severity (moderate/severe), prior alpha blocker use (yes/no), country (Japan/Korea/Taiwan), and baseline value." (NCT00861757)
Timeframe: baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.5
2.5 mg Tadalafil-0.8
5.0 mg Tadalafil-0.8
0.2 mg Tamsulosin-1.1

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Change From Baseline in International Prostate Symptom Score (IPSS) at 12 Weeks

"The IPSS Total Score is obtained by combining the scores of the responses to 1 through 7 component questions. Each question is scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms.~Least Squares Mean values were controlled for prior alpha blocker use (yes/no), country (Japan/Korea/Taiwan) and baseline value." (NCT00861757)
Timeframe: baseline, 12 weeks

InterventionUnits on a scale (Least Squares Mean)
Placebo-3.0
2.5 mg Tadalafil-4.8
5 mg Tadalafil-4.7
0.2 mg Tamsulosin-5.5

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Change From Baseline in Postvoid Residual Volume (PVR) at 12 Weeks

The PVR is defined as the volume of urine remaining in the bladder after voiding, estimated by ultrasound. (NCT00861757)
Timeframe: baseline, 12 weeks

Interventionmilliliter (mL) (Mean)
Placebo-1.20
2.5 mg Tadalafil-0.09
5.0 mg Tadalafil-2.90
0.2 mg Tamsulosin-5.67

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Change From Baseline in Prostate Specific Antigen (PSA) at 12 Weeks

Nanograms of PSA per milliliter (ng/mL) of blood. (NCT00861757)
Timeframe: baseline, 12 weeks

Interventionmicrogram/Liter (Mean)
Placebo-0.03
2.5 mg Tadalafil0.04
5.0 mg Tadalafil0.13
0.2 mg Tamsulosin-0.06

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Change From Baseline in Sitting Heart Rate (HR) at 12 Weeks

(NCT00861757)
Timeframe: baseline, 12 weeks

Interventionbeats per minute (bpm) (Mean)
Placebo-0.3
2.5 mg Tadalafil0.7
5.0 mg Tadalafil0.6
0.2 mg Tamsulosin0.6

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Change From Baseline in Uroflowmetry Parameter: Peak Flow Rate (Qmax) at 12 Weeks

"Qmax: defined as the peak urine flow rate (measured in milliliters per second [mL/second] using standard calibrated flowmeter).~Least Squares Mean values were controlled for Benign Prostatic Hyperplasia (BPH) severity (moderate/severe), prior alpha blocker use (yes/no), country (Japan/Korea/Taiwan), and baseline value." (NCT00861757)
Timeframe: baseline, 12 weeks

Interventionmilliliter per second (mL/sec) (Least Squares Mean)
Placebo2.1
2.5 mg Tadalafil1.6
5.0 mg Tadalafil1.3
0.2 mg Tamsulosin2.1

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Change From Baseline in Blood Pressure (Standing) at 12 Weeks

(NCT00861757)
Timeframe: baseline, 12 weeks

,,,
Interventionmm Hg (Mean)
Systolic Blood PressureDiastolic Blood Pressure
0.2 mg Tamsulosin-0.9-1.0
2.5 mg Tadalafil-2.9-2.3
5.0 mg Tadalafil0.6-1.7
Placebo0.80.4

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Change in Immune Response After Tadalafil Administration

Median fold-change in immune response of T-cell expansion, delayed-type hypersensitivity reactions, CD4/CD69, CD8/CD69. A positive value indicates an increase in immune response. (NCT00894413)
Timeframe: Change from baseline to up to 14 days post-intervention

,
Interventionfold change (Median)
T-cell expansionDTH areaCD4/CD69CD8/CD69
Placebo1.131.140.900.93
Tadalafil1.594.741.291.14

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Overall Sexual Function as Measured by Change From Baseline in the International Index of Erectile Function (IIEF)

The IIEF is a validated 15-item for measuring patient-reported erectile function. A score of 0-5 is given to each of the 15 questions that examine 5 main domains of male sexual function: erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction. Domain scores are the sum of each item. The erectile function domain has 5 items with a score range of 1-30, orgasmic function has 2 items with a score range of 0-10, sexual desire has 2 items with a score range of 0-10, intercourse satisfaction has 3 items with a score range of 0-15, and overall satisfaction has 2 items with a score range of 2-10. Total score ranges from 0-70, with higher scores indicated better functioning. Change from baseline is calculated by subtracting baseline score from score at the time point of interest. (NCT00931528)
Timeframe: Baseline, week 30, and years 1 and 2 from start of treatment

,
Interventionchange in total IIEF (Mean)
Week 30Year 1Year 2
Placebo-9.0-10.5-14.1
Tadalafil-8.2-9.5-9.7

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Partner Marital Adjustment as Measured by the Locke's Marital Adjustment Test

The Locke Marital Adjustment Test (LMAT) is a 16-item questionnaire with scores ranging from 48 to 138 for participants. Higher scores indicate greater sexual function, sexual wellbeing, or marital adjustment. The change in LMAT score is calculated by subtracting the baseline score from the follow-up score. (NCT00931528)
Timeframe: Baseline, week 30 and years 1 and 2 after the start of treatment

,
Interventionchange in LMAT score (Mean)
Week 30Year 1Year 2
Placebo-2.61.2-4.7
Tadalafil-1.5-2.3-2.8

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Percentage of Patients Maintaining Spontaneous (Off-drug) Erectile Function (EF) at Weeks 28-30 After Initiation of Radiation Therapy (RT)

"EF is measured by Question 1 of the International Index of Erectile Function (IIEF). The IIEF is a validated 15-item for measuring patient-reported erectile function. Question 1 asks How often were you able to get an erection during sexual activity? Responses ranged from 0=no sexual activity, to 5=Almost always or always. Higher scores indicated better functioning. All patients have erectile function prior to initiation of RT, indicated by a score of 3, 4, or 5 on IIEF Q1. Patients with a lower IIEF Q1 score at weeks 28-30 than at baseline will have less erectile function and be categorized as nonresponders. Patients with similar or improved erectile function will be categorized as responders (maintaining). Patient-related predictors of at erectile function at this time point are also reported with this outcome measure." (NCT00931528)
Timeframe: Baseline and 30 weeks from the start of radiation therapy

Interventionpercentage of participants (Number)
Tadalafil79
Placebo74

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Patient Marital Adjustment as Measured by the Locke's Marital Adjustment Test

The Locke Marital Adjustment Test (LMAT) is a 16-item questionnaire with scores ranging from 48 to 138 for participants. Higher scores indicate greater sexual function, sexual wellbeing, or marital adjustment. The change in LMAT score is calculated by subtracting the baseline score from the follow-up score. (NCT00931528)
Timeframe: Baseline, week 30 and years 1 and 2 after the start of treatment

,
Interventionchange in LMAT score (Mean)
Week 30Year 1Year 2
Placebo-2.6-1.9-1.4
Tadalafil-3.5-1.9-1.3

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Percentage of Patients Maintaining Spontaneous (Off-drug) EF at Years 1 and 2 After Initiation of RT

"The International Index of Erectile Function (IIEF) is a validated 15-item for measuring patient-reported erectile function. Question 1 asks How often were you able to get an erection during sexual activity? Responses ranged from 0=no sexual activity, to 5=Almost always or always. Higher scores indicated better functioning. All patients have erectile function prior to initiation of RT, indicated by a score of 3, 4, or 5. Patients with a lower IIEF Q1 score at weeks 28-30 than at baseline will have less erectile function and be categorized as nonresponders. Patients with similar or improved erectile function will be categorized as responders (maintaining). Patient-related predictors of at erectile function at Years 1 and 2 are also reported with this outcome measure." (NCT00931528)
Timeframe: Baseline, 1 and 2 years from the start of tadalafil or placebo

,
Interventionpercentage of participants (Number)
Year 1Year 2
Placebo71.463.3
Tadalafil72.268.4

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Overall Patient Sexual Satisfaction as Measured by Change From Baseline in the Sexual Adjustment Questionnaire (SAQ) Score

The Sexual Adjustment Questionnaire (SAQ) is a 20-item questionnaire with an overall score range between 8 and 100 including the following domains: desire, ranging between 5 and 30; dysfunction, 0 and 25; activity, 0 and 10; satisfaction, 1 and 10; and fatigue, 1 and 5. The change in SAQ score is calculated by subtracting the baseline score from the follow-up score. A positive change indicates an improvement in sexual well-being. (NCT00931528)
Timeframe: Baseline, week 30 and years 1 and 2 after the start of treatment

,
Interventionchange in SAQ score (Mean)
Week 30Year 1Year 2
Placebo-2.9-4.9-4.6
Tadalafil-2.0-3.7-3.4

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Overall Partner Sexual Satisfaction as Measured by Change From Baseline in the Sexual Adjustment Questionnaire-Partner (SAQ-P) Score

The SAQ-P is an 18-item questionnaire with an overall score range between 0 and 90 including the following domains: desire, dysfunction, activity, satisfaction, and fatigue. The change in SAQ score is calculated by subtracting the baseline score from the follow-up score. A positive change indicates an improvement in sexual well-being. (NCT00931528)
Timeframe: Baseline, week 30 and years 1 and 2 after the start of treatment

,
Interventionchange in SAQ score (Mean)
Week 30Year 1Year 2
Placebo-1.8-2.55.1
Tadalafil-4.9-3.91.5

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Change From Baseline in Modified International Prostate Symptom Score (mIPSS) at 1 Week

The mIPSS Total Score covered a time period of 1 week and was obtained by combining scores of responses to Component Questions 1-7. Each question was scored from 0-5 for an mIPSS range of 0-35 points; higher numerical scores represented greater severity of symptoms. Least Squares (LS) Mean of change from baseline to endpoint (Week 1 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 1 week

Interventionunits on a scale (Least Squares Mean)
Placebo-2.5
Tadalafil 5 mg-4.0
Tamsulosin 0.4 mg-4.0

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Change From Baseline in Peak Urine Flow Rate (Q-Max) at 12 Weeks

Q-max (peak urine flow rate) was measured in milliliters per second (mL/sec) using a standard calibrated flowmeter. At each visit, a uroflowmetry assessment was considered valid and data were included in the analyses only if the prevoid total bladder volume (assessed by ultrasound) was ≥150 to ≤550 mL and the voided volume (V-comp) was ≥125 mL. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionmilliliters per second (mL/sec) (Median)
Placebo0.3
Tadalafil 5 mg1.6
Tamsulosin 0.4 mg1.6

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Change From Baseline in Postvoid Residual Volume (PVR) at 12 Weeks

PVR was the amount of urine remaining in the bladder after void completion. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionmilliliter (mL) (Median)
Placebo0.0
Tadalafil 5 mg-1.0
Tamsulosin 0.4 mg-5.5

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Change From Baseline in Total International Prostate Symptom Score (IPSS) at 12 Weeks

The IPSS Total Score was obtained by combining the scores of the responses to Component Questions 1-7. Each question was scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represented greater severity of symptoms. Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-4.2
Tadalafil 5 mg-6.3
Tamsulosin 0.4 mg-5.7

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Change From Baseline in Total International Prostate Symptom Score (IPSS) at 4 Weeks

The IPSS Total Score was obtained by combining the scores of the responses to Component Questions 1-7. Each question was scored from 0-5 for an IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represented greater severity of symptoms. Least Squares (LS) Mean of change from baseline to endpoint (Week 4 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 4 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-3.3
Tadalafil 5 mg-5.5
Tamsulosin 0.4 mg-5.7

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Change From Baseline in Volume of Voided Urine (V-Comp) at 12 Weeks

V-comp (volume of urine voided) was measured in milliliters (mL) using a standard calibrated flowmeter. At each visit, a uroflowmetry assessment was considered valid and data were included in the analyses only if the prevoid total bladder volume (assessed by ultrasound) was ≥150 to ≤550 mL and V-comp was ≥125 mL. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionmilliliter (mL) (Median)
Placebo0.0
Tadalafil 5 mg11.0
Tamsulosin 0.4 mg16.0

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Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 12 Weeks: Overall

The TSS-BPH was a validated participant-rated instrument that measured participant satisfaction with treatment based on a 13-item questionnaire. The overall TSS-BPH score was converted to a percentage of the maximum value possible (percent ranged from 0-100) with lower scores indicating greater satisfaction. (NCT00970632)
Timeframe: 12 weeks

Interventionunits on a scale (Median)
Placebo28.9
Tadalafil 5 mg22.2
Tamsulosin 0.4 mg28.9

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Clinician Global Impression of Improvement (CGI-I) at 12 Weeks

"The CGI-I was an investigator-rated instrument that measured improvement or worsening of the participant's symptoms based on a 7-point scale. A score of 1=participant felt symptoms were very much better; score of 2=participant felt symptoms were much better; score of 3=participant felt symptoms were a little better; score of 4=participant felt no change in symptoms; score of 5=participant felt symptoms were a little worse; score of 6=participant felt symptoms were much worse; score of 7=participant felt symptoms were very much worse." (NCT00970632)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
Very much worseMuch worseA little worseNo changeA little betterMuch betterVery much better
Placebo1265157349
Tadalafil 5 mg02532585016
Tamsulosin 0.4 mg0174065386

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Patient Global Impression of Improvement (PGI-I) at 12 Weeks

"The PGI-I was a participant-rated instrument that measured the improvement or worsening of the participant's symptoms based on a 7-point scale at Week 12. A score of 1=participant felt symptoms were very much better; score of 2=participant felt symptoms were much better; score of 3=participant felt symptoms were a little better; score of 4=participant felt no change in symptoms; score of 5=participant felt symptoms were a little worse; score of 6=participant felt symptoms were much worse; score of 7=participant felt symptoms were very much worse." (NCT00970632)
Timeframe: 12 weeks

,,
Interventionparticipants (Number)
Very much worseMuch worseA little worseNo changeA little betterMuch betterVery much better
Placebo22451533611
Tadalafil 5 mg01628525617
Tamsulosin 0.4 mg00836554810

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Change From Baseline in Benign Prostatic Hyperplasia Impact Index (BII) at 12 Weeks

BII was a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores ranged from 0-13; higher scores represented increased perceived impact of BPH-lower urinary tract symptoms (LUTS) on overall health. Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.9
Tadalafil 5 mg-1.7
Tamsulosin 0.4 mg-1.5

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Change From Baseline in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain at 12 Weeks

IIEF measured self-reported EF over the past 4 weeks. Scores ranged from 0 (low or no EF)-5 (high EF) on 6 questions (1-5, 15 of the IIEF). Total EF Domain scores ranged from 1-30. Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo2.1
Tadalafil 5 mg6.0
Tamsulosin 0.4 mg1.7

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Change From Baseline in International Prostate Symptom Score (IPSS) Nocturia Question at 12 Weeks

The IPSS nocturia question (Component Question 7) measured nocturia (need to urinate at night) over the past 4 weeks. Scores ranged from 0 (no episodes of nocturia)-5 (5 or more episodes of nocturia). Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.3
Tadalafil 5 mg-0.5
Tamsulosin 0.4 mg-0.5

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Change From Baseline in International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index at 12 Weeks

IPSS QoL assessed QoL by urinary symptoms, with scores ranging from 0 (delighted)-6 (terrible). Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-1.0
Tadalafil 5 mg-1.3
Tamsulosin 0.4 mg-1.1

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Change From Baseline in International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore at 12 Weeks

IPSS storage (irritative) subscore was the sum of Component Questions 2, 4 and 7 of the IPSS questionnaire. Scores ranged from 0 (no irritative symptoms) to 5 (frequent irritative symptoms); therefore, the 3 questions of the irritative subscore ranged from 0 to 15. Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-1.6
Tadalafil 5 mg-2.2
Tamsulosin 0.4 mg-2.2

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Change From Baseline in Benign Prostatic Hyperplasia Impact Index (BII) at 4 Weeks

BII was a 4-item, self-administered questionnaire evaluating impact of urinary problems on overall health and activity. Total scores ranged from 0-13; higher scores represented increased perceived impact of BPH-lower urinary tract symptoms (LUTS) on overall health. Least Squares (LS) Mean of change from baseline to endpoint (Week 4 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 4 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-0.4
Tadalafil 5 mg-1.2
Tamsulosin 0.4 mg-1.3

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Change From Baseline in International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore at 12 Weeks.

IPSS voiding (obstructive) subscore was the sum of Component Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores ranged from 0 (no obstructive symptoms)-5 (frequent obstructive symptoms); therefore, the 4 questions of the obstructive score ranged from 0-20. Least Squares (LS) Mean of change from baseline to endpoint (Week 12 or last post-baseline value carried forward) was from an analysis of covariance (ANCOVA) and adjusted for treatment group, region, centered-baseline covariate, centered-baseline-by-treatment interaction, and treatment-by-region interaction. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-2.6
Tadalafil 5 mg-4.1
Tamsulosin 0.4 mg-3.5

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Change From Baseline in Mean Urine Flow Rate (Q-Mean) at 12 Weeks

Q-mean (mean urine flow rate) was measured in milliliters per second (mL/sec) using a standard calibrated flowmeter. At each visit, a uroflowmetry assessment was considered valid and data were included in the analyses only if the prevoid total bladder volume (assessed by ultrasound) was ≥150 to ≤550 mL and the voided volume (V-comp) was >=125 mL. (NCT00970632)
Timeframe: Baseline, 12 weeks

Interventionmilliliters per second (mL/sec) (Median)
Placebo0.10
Tadalafil 5 mg1.25
Tamsulosin 0.4 mg0.70

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Change From Baseline in 'Yes' Answers to Morning Erections

"The participants were asked to complete the morning erections diary every morning during the 4-week period before randomization and during the 6-week, Drug-Free, Washout Period. Data presented are the changes in the participant's percentage of yes responses relative to the number of days the question was answered during treatment. The analysis of covariance (ANCOVA) was used to calculate Least Square (LS) mean and 95% confidence interval (CI). LS mean values are adjusted for treatment, baseline morning erections frequency, age group and country." (NCT01026818)
Timeframe: Randomization (Baseline), Month 10.5

Intervention"percentage of yes response" (Least Squares Mean)
Tadalafil 5 mg OaD8.92
Tadalafil 20 mg PRN12.16
Placebo14.04

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Percentage of Participants With a Score of Greater Than or Equal to 22 in the International Index of Erectile Function- Erectile Function (IIEF-EF) Domain

Self-reported erectile function during the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (no sexual activity for Question 1, no sexual stimulation for Question 2 and did not attempt intercourse for Questions 3-5) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Data presented are the percentage of participants with an IIEF-EF Total Score greater than or equal to (≥) 22. (NCT01026818)
Timeframe: Month 9 and Month 13.5

,,
Interventionpercentage of participants (Number)
Month 9Month 13.5
Placebo14.227.0
Tadalafil 20 mg PRN19.733.1
Tadalafil 5 mg OaD25.232.4

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Residual Erectile Function (REF) at Month 10.5

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Month 10.5

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo22291922142
Tadalafil 20 mg PRN17302331106
Tadalafil 5 mg OaD13292522124

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Residual Erectile Function (REF) at Month 13.5

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Month 13.5

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo11251528243
Tadalafil 20 mg PRN8202034284
Tadalafil 5 mg OaD5191734214

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Residual Erectile Function (REF) at Month 2

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Month 2

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo38531915511
Tadalafil 20 mg PRN2751282358
Tadalafil 5 mg OaD28382625913

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Residual Erectile Function (REF) at Month 5

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Month 5

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo2735271969
Tadalafil 20 mg PRN2139213467
Tadalafil 5 mg OaD12371932158

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Residual Erectile Function (REF) at Month 9

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Month 9

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo23352318106
Tadalafil 20 mg PRN17283027155
Tadalafil 5 mg OaD112522232013

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Standardized Morning Erections Question (SMEQ) Score at Month 13.5

"Participants evaluated the frequency of their morning erections during the past 3-month period by answering the SMEQ (Do you ever wake up with an erection) using a 4-point grading system ranging from 0 (Yes, regularly) to 3 (never)." (NCT01026818)
Timeframe: Month 13.5

,,
Interventionparticipants (Number)
Yes, regularlyLess frequently than in the pastOnly occasionallyNeverMissing
Placebo131827426
Tadalafil 20 mg PRN152430405
Tadalafil 5 mg OaD132231322

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Standardized Morning Erections Question (SMEQ) Score at Month 2

"Participants evaluated the frequency of their morning erections during the past 3-month period by answering the SMEQ (Do you ever wake up with an erection) using a 4-point grading system ranging from 0 (Yes, regularly) to 3 (never)." (NCT01026818)
Timeframe: Month 2

,,
Interventionparticipants (Number)
Yes, regularlyLess frequently than in the pastOnly occasionallyNeverMissing
Placebo710268711
Tadalafil 20 mg PRN71531809
Tadalafil 5 mg OaD48417313

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Standardized Morning Erections Question (SMEQ) Score at Month 9

"Participants evaluated the frequency of their morning erections during the past 3-month period by answering the SMEQ (Do you ever wake up with an erection) using a 4-point grading system ranging from 0 (Yes, regularly) to 3 (never)." (NCT01026818)
Timeframe: Month 9

,,
Interventionparticipants (Number)
Yes, regularlyLess frequently than in the pastOnly occasionallyNeverMissing
Placebo7927657
Tadalafil 20 mg PRN91926617
Tadalafil 5 mg OaD721363911

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Residual Erectile Function (REF) at Baseline

The participant is asked to rate the hardness of his erection using a 5-point grading system, with 0 (penis does not enlarge), 1 (penis is larger but not hard), 2 (penis is hard but not enough for penetration), 3 (penis is hard enough for penetration but not completely hard), 4 (penis is completely hard and fully rigid.) (NCT01026818)
Timeframe: Baseline

,,
Interventionparticipants (Number)
REF = 0REF = 1REF = 2REF = 3REF = 4Missing
Placebo6447171300
Tadalafil 20 mg PRN6248171122
Tadalafil 5 mg OaD6146181202

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Global Assessment Questions (GAQ) Question 1 at Month 9

GAQ Question 1: Choose the one number which best describes how you perceive your ability to achieve and maintain your erections now, compared to how it was before you began taking medication in this study. Responses range from very much better (1) to very much worse (7). (NCT01026818)
Timeframe: Month 9

,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterNo changeA little worseMuch worseVery much worseMissing
Placebo49224836149
Tadalafil 20 mg PRN1022322858116
Tadalafil 5 mg OaD912333146811

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Global Assessment Question (GAQ) Question 2 at Month 9

GAQ Question 2: Choose the one number which best describes how you perceive your sexual life is now, compared to how it was before you began taking medication in this study. Responses range from very much better (1) to very much worse (7). (NCT01026818)
Timeframe: Month 9

,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterNo changeA little worseMuch worseVery much worseMissing
Placebo3111849410119
Tadalafil 20 mg PRN7252627101098
Tadalafil 5 mg OaD712303187910

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Global Assessment Question (GAQ) Question 2 at Month 13.5

GAQ Question 2: Choose the one number which best describes how you perceive your sexual life is now, compared to how it was before you began taking medication in this study. Responses range from very much better (1) to very much worse (7). (NCT01026818)
Timeframe: Month 13.5

,,
Interventionparticipants (Number)
Very much betterMuch betterA little betterNo changeA little worseMuch worseVery much worseMissing
Placebo142124265745
Tadalafil 20 mg PRN202326245367
Tadalafil 5 mg OaD92920254454

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Global Assessment Question (GAQ) Question 1 at Month 13.5

GAQ Question 1: Choose the one number which best describes how you perceive your ability to achieve and maintain your erections now, compared to how it was before you began taking medication in this study. Responses range from very much better (1) to very much worse (7). (NCT01026818)
Timeframe: Month 13.5

,,
Interventionparticipants (Number)
Very much betterMuch betterA little BetterNo ChangeA little worseMuch worseVery much worseMissing
Placebo161828262565
Tadalafil 20 mg PRN192527234367
Tadalafil 5 mg OaD132428194354

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Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire Mean Score

The EDITS questionnaire is a validated questionnaire consisting of 11 questions evaluating self-reported satisfaction with the erectile dysfunction (ED) treatment. Responses were based on the experiences during the previous 4 weeks. Each question is rated on a scale of 0 (extremely low treatment satisfaction) to 4 (extremely high treatment satisfaction). The EDITS mean score was obtained by adding each individual result for all questions, dividing by the number of questions answered. The mean scores range from 0 (extremely low treatment satisfaction) to 4 (extremely high satisfaction). The Mixed Model for Repeated Measures (MMRM) analysis was used to calculate Least Squares (LS) mean and 95% Confidence Interval (CI). LS mean values are adjusted for treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Months 9 and 13.5

,,
Interventionunits on a scale (Least Squares Mean)
Month 9Month 13.5
Placebo1.882.25
Tadalafil 20 mg PRN2.112.38
Tadalafil 5 mg OaD2.212.54

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Change in Penile Length and Girth

Measurements were performed with the penis in the flaccid state. The stretched penile length was measured from the tip of the glans to the pubopenile skin junction while applying tension to maximally stretch the penis. The penile circumference at midshaft was measured. All measurements were taken with a paper ruler to the nearest 0.5 centimeter (cm). The analysis of covariance (ANCOVA) was used to calculate Least Square (LS) mean and 95% confidence interval (CI). LS mean values are adjusted for treatment, baseline, age group and country. (NCT01026818)
Timeframe: Randomization (Baseline), Month 9

,,
Interventionmillimeter (mm) (Least Squares Mean)
LengthGirth
Placebo-5.73-2.34
Tadalafil 20 mg PRN-7.260.82
Tadalafil 5 mg OaD-1.530.03

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Change From Baseline to Endpoint in the International Index of Erectile Function- Erectile Function (IIEF-EF) Total Score

Self-reported erectile function during the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (no sexual activity for Question 1, no sexual stimulation for Question 2 and did not attempt intercourse for Questions 3-5) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. The Mixed Model for Repeated Measures (MMRM) analysis was used to calculate Least Squares (LS) mean and 95% confidence interval (CI). LS mean values are adjusted for baseline score, treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Randomization (Baseline), Months 9 and 10.5 and 13.5

,,
Interventionunits on a scale (Least Squares Mean)
Month 9Month 10.5Month 13.5
Placebo4.935.988.97
Tadalafil 20 mg PRN6.535.769.78
Tadalafil 5 mg OaD7.736.2410.60

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Change From Baseline to Endpoint in the International Index of Erectile Function (IIEF) Domains (Intercourse Satisfaction Domain, Orgasmic Function Domain, Sexual Desire Domain, Overall Satisfaction Domain)

Self-reported overall satisfaction during past 4 weeks. Orgasmic function score is sum of Questions (Q)9 and 10 of IIEF. Scores range from 0 (no sexual stimulation or intercourse) to 5 (high orgasm) for each Q, total 0 to 10. Sexual desire score is sum of Q11 and 12 of IIEF. Scores range from 1 (low/no desire) to 5 (high desire) for each Q, total 2 to 10. Intercourse satisfaction score is sum of Q6, 7 and 8 of IIEF. Scores range from 0 (no attempts for Q6, did not attempt intercourse for Q7 and no intercourse for Q8) to 5 (high satisfaction) for each Q, total 0 to 15. Overall satisfaction score is sum of Q13 and 14 of IIEF. Scores range from 1 (low/no satisfaction) to 5 (high satisfaction) for each Q, total 2 to 10. Higher total scores for each domain indicate higher function. MMRM analysis was used to calculate LS mean and 95% CI. LS mean values are adjusted for baseline, treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Randomization (Baseline), Months 9 and 10.5 and 13.5

,,
Interventionunits on a scale (Least Squares Mean)
Orgasmic function - Month 9Orgasmic function - Month 10.5Orgasmic function - Month 13.5Sexual desire - Month 9Sexual desire - Month 10.5Sexual desire - Month 13.5Intercourse satisfaction - Month 9Intercourse satisfaction - Month 10.5Intercourse satisfaction - Month 13.5Overall satisfaction - Month 9Overall satisfaction - Month 10.5Overall satisfaction - Month 13.5
Placebo2.392.483.420.630.550.952.962.724.140.780.721.52
Tadalafil 20 mg PRN2.482.482.900.650.650.893.502.814.080.930.481.57
Tadalafil 5 mg OaD2.762.943.570.650.611.043.893.214.700.970.641.50

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Change From Baseline in Self Esteem and Relationship (SEAR) Questionnaire Score

The SEAR questionnaire is a participant-reported measure of psychosocial outcomes in men with erectile dysfunction (ED). It consists of 14 items. Sexual Relationship domain consists of 8 items (items 1-8). Items 2-8 are rated on a scale of 1 (Never) to 5 (Always), whereas item 1 is reverse scored (1=Always and 5=Never). The total scores for sexual relationship domain range from 8-40 with higher scores indicating better relationship. Self-Esteem subdomain contains items 9 through 12 rated on a scale of 1 (no/low self-esteem) to 5 (high self-esteem). Total scores for Self-Esteem subscale range from 4-20 with higher scores indicating higher self-esteem. The Mixed Model for Repeated Measures (MMRM) analysis was used to calculate Least Squares (LS) mean and 95% Confidence Interval (CI). LS mean values are adjusted for baseline domain score, treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Randomization (Baseline), Months 9 and 13.5

,,
Interventionunits on a scale (Least Squares Mean)
Sexual relationship - Month 9Sexual relationship - Month 13.5Self-esteem - Month 9Self-esteem - Month 13.5
Placebo3.026.720.511.62
Tadalafil 20 mg PRN3.506.680.791.72
Tadalafil 5 mg OaD4.786.900.781.67

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Change From Baseline in 26-item Expanded Prostate Cancer Index Composite (EPIC-26) Questionnaire Score

EPIC-26 (participants) contains 26 items and 5 domains: Urinary Incontinence (Items 1-4), Urinary Irritative/Obstructive (Items 5-8), Bowel (Items 10-15), Sexual (Items 16-21), and Hormonal (Items 22-26). Response options for each EPIC item form a Likert scale, and multi-item scale scores are transformed linearly to a 0 to 100 scale for each domain, with higher scores representing better health-related quality of life. Responses are based on experiences during the previous 4 weeks. The Mixed Model for Repeated Measures (MMRM) analysis was used to calculate Least Squares (LS) mean and 95% confidence interval (CI). LS mean values are adjusted for baseline domain score, treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Randomization (Baseline), Months 9 and 13.5

,,
Interventionunits on a scale (Least Squares Mean)
Urinary Incontinence - Month 9Urinary Incontinence - Month 13.5Urinary Irritative/Obstructive - Month 9Urinary Irritative/Obstructive - Month 13.5Bowel - Month 9Bowel - Month 13.5Sexual - Month 9Sexual - Month 13.5Hormonal - Month 9Hormonal - Month 13.5
Placebo30.5935.4412.2612.306.486.7817.9833.37-0.183.01
Tadalafil 20 mg PRN31.1235.5413.2813.826.276.4920.6632.582.722.92
Tadalafil 5 mg OaD34.0837.4113.8313.865.946.8727.5336.551.722.48

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Change From Baseline in 'Yes' Answers to Questions 1 to 5 of the Sexual Encounter Profile (SEP)

Participant-assessed diary has 5 questions: Question (Q)1: erection achievement, Q2: successful penetration, Q3: successful intercourse, Q4: satisfied with erection, and Q5: satisfied with sexual experience) for each sexual encounter made over a specified period of time. SEP Q1-Q5 scores were determined as the percentage of 'Yes' responses to each of the 5 questions out of all sexual attempts recorded during the time period. The Mixed Model for Repeated Measures (MMRM) analysis was used to calculate Least Squares (LS) mean and 95% confidence interval (CI). LS mean values are adjusted for treatment, country, visit, visit-by-treatment, age group, and age group-by-treatment (if significant at p<0.10). (NCT01026818)
Timeframe: Randomization (Baseline), Months 9 and 10.5 and 13.5

,,
Intervention"percentage of yes responses" (Least Squares Mean)
Q1 - Month 9Q1 - Month 10.5Q1 - Month 13.5Q2 - Month 9Q2 - Month 10.5Q2 - Month 13.5Q3 - Month 9Q3 - Month 10.5Q3 - Month 13.5Q4 - Month 9Q4 - Month 10.5Q4 - Month 13.5Q5 - Month 9Q5 - Month 10.5Q5 - Month 13.5
Placebo52.5458.8675.2727.6736.2650.1121.6128.5240.7514.3018.8830.5614.0419.1129.38
Tadalafil 20 mg PRN63.8864.2479.7934.2934.9956.0724.0923.0145.8318.1511.7435.6217.7310.5234.96
Tadalafil 5 mg OaD67.4167.7886.1644.0040.8163.4833.6728.7552.4126.1716.9442.0825.4216.2640.81

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Percentage of Participants With a Score of Greater Than or Equal to 22 in the Erectile Function (EF) Domain of the International Index of Erectile Function (IIEF) Questionnaire

Self-reported erectile function during the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (no sexual activity for Question 1, no sexual stimulation for Question 2 and did not attempt intercourse for Questions 3-5) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Data presented are the percentage of participants with an IIEF-EF Total Score greater than or equal to (≥) 22. (NCT01026818)
Timeframe: Month 10.5

Interventionpercentage of participants (Number)
Tadalafil 5 mg OaD20.9
Tadalafil 20 mg PRN16.9
Placebo19.1

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6-minute Walk Distance

patients were made to take a walk of normal speed to cover a distance in 6 minutes and distance covered was recorded. This was done at baseline (week o) and then repeated t 36 weeks. (NCT01042158)
Timeframe: baseline and 36 weeks

Interventionmeters (Mean)
Baseline (week 0)Week 36
Tadalafil and Ambrisentan Upfront Therapy343395

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Pulmonary Vascular Resistance (PVR)

Change in Pulmonary Vascular Resistance (PVR) was ascertained via Right Heart Catheterization (RHC) measurement of the difference between the PVR at baseline and 36 weeks (NCT01042158)
Timeframe: baseline 36 weeks

InterventionWood units (Median)
BaselineAt 36 weeks
Tadalafil and Ambrisentan Upfront Therapy6.93.1

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Right Ventricular (RV) Mass

Assessment of change in Right ventricular mass was done via standard volumetric cine images of the right heart at baseline and comparing it to that at the end of 36 weeks using Cardiac Magnetic Resonance Imaging studies. (NCT01042158)
Timeframe: baseline and 36 weeks

Interventiongrams (Median)
BaselineAt 36 weeks
Tadalafil and Ambrisentan Upfront Therapy32.528.0

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Tricuspid Annular Plane Systolic Excursion (TAPSE)

The extent of displacement of the tricuspid valves, termed as Tricuspid Annular Plane Systolic Excursion (TAPSE) was measured using a trans-thoracic echocardiogram following Right heart catheterization. (NCT01042158)
Timeframe: baseline and 36 weeks

Interventioncm (Mean)
Baseline at week 0week 36
Tadalafil and Ambrisentan Upfront Therapy2.21.65

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Reasons for Discontinuation of Randomized Erectile Dysfunction Treatment

The reported reasons for a decision to discontinue from initial randomized treatment prior to Week 24 are reported. Discontinuation of randomized treatment was defined as switching between the 3 study treatments (tadalafil on demand, tadalafil once a day, or sildenafil citrate on demand) or discontinuing from all treatments. A change of dose within the same treatment was not considered as switching of treatment. (NCT01122264)
Timeframe: Baseline through 24 weeks

,,
Interventionparticipants (Number)
Slow onset of actionCompleted treatmentLack of efficacy (hardness of erection)Lack of efficacy (duration of erection)Lack of confidence in medication working each timeAdverse eventFeel medication controls my sexual lifeNon-desired spontaneous erectionsTime constraints due to short drug action windowPartner's requestDon't want to take a pill every dayPrefer a pill every day, not on demandParticipant discontinuation from the trialParticipant did not take any study drugParticipants without discontinuation event
Sildenafil Citrate On Demand10155242167011302814189
Tadalafil On Demand51467371210020112146
Tadalafil Once a Day9155115100402270110122

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Patterns of Erectile Dysfunction Treatment Change

Results are reported as the number of participants per sequence of study medications (tadalafil on demand, tadalafil once a day, or sildenafil citrate on demand) that were taken as a result of switching treatments. The Other Treatment Sequence reports the number of participants per sequence of study medications that were taken as a result of switching treatments more than once. The number of participants who did not switch is also reported. (NCT01122264)
Timeframe: Baseline through 24 weeks

Interventionparticipants (Number)
No Treatment IntakeNo SwitchFrom Once a Day to Any On DemandFrom Any On Demand to Once a DayFrom Any On Demand to Any On DemandReturning Back to Randomized TreatmentOther Treatment Sequence
Entire Study Population34099584973547

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Global Assessment Questions (GAQ)

The GAQ consists of 2 Yes/No/No Response (No Respo) questions. GAQ Question (Q)1: Has the treatment you have been taking during this study improved your erections? GAQ Q2: Has the treatment improved your ability to engage in sexual activity? (NCT01122264)
Timeframe: 24 weeks

,,
Interventionparticipants (Number)
Q1:Treatment improved erections? YesQ1:Treatment improved erections? NoQ1: Treatment improved erections? No ResponseQ2:Treatment improved ability to engage? YesQ2:Treatment improved ability to engage? NoQ2: Treatment improved ability to engage? No Respo
Sildenafil Citrate On Demand2033424204849
Tadalafil On Demand21820142091429
Tadalafil Once a Day2192315214736

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Erectile Dysfunction Inventory of Treatment Satisfaction (EDITS) Questionnaire at 4, 8, 16, and 24 Weeks

The participant questionnaire consists of 11 questions. Each question is rated on a scale of 0 (extremely low treatment satisfaction) to 4 (extremely high treatment satisfaction). The EDITS summary score was obtained by adding each individual result for all questions, dividing by the number of questions answered (mean satisfaction score), then multiplying by 25, thus obtaining a score range from 0 (extremely low treatment satisfaction) to 100 (extremely high satisfaction). Least Squares Mean changes were adjusted for treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
EDITS at Week 4EDITS at Week 8 (n=231, 235, 231)EDITS at Week 16 (n=168, 147, 100)EDITS at Week 24 (n=141, 118, 80)
Sildenafil Citrate On Demand71.9872.7476.6477.98
Tadalafil On Demand72.3675.2879.6481.01
Tadalafil Once a Day75.2076.6477.6678.75

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Change From Baseline to 4, 8, 16, and 24 Weeks of the Sexual Relationship Domain of the Self-Esteem and Relationship (SEAR) Questionnaire

SEAR assesses psychosocial outcomes in men with erectile dysfunction. Sexual Relationship domain consists of 8 items (items 1-8). Items 2-8 are rated on a scale of 1 (Never) to 5 (Always), whereas item 1 is reverse scored (1=Always and 5=Never). The domain score was computed by summing its respective items, then transforming it into a 0 (least favorable) to 100 (most favorable) scale. Transformed score = 100 x [(actual raw score - lowest possible raw score)/possible raw score range]. Least Squares Mean changes adjusted for baseline score, treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=230, 232, 231)Change from Baseline to Week 16 (n=167, 146, 101)Change from Baseline to Week 24 (n=140, 117, 81)
Sildenafil Citrate On Demand29.5031.1537.3237.46
Tadalafil On Demand27.6531.4237.5939.37
Tadalafil Once a Day29.2631.0732.9034.96

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Change From Baseline to 4, 8, 16, and 24 Weeks of the Self Esteem Domain of the Self-Esteem and Relationship (SEAR) Questionnaire

SEAR assesses psychosocial outcomes in men with erectile dysfunction. The Self-Esteem domain consists of 4 items (items 9-12), each rated on a scale of 1 (Never) to 5 (Always). Item 11 is reverse scored (1=Always and 5=Never). The domain score was computed by summing its respective items, then transforming it into a 0 (least favorable) to 100 (most favorable) scale. The transformed score = 100 x [(actual raw score - lowest possible raw score)/possible raw score range]. Least Squares Mean changes were adjusted for baseline score, treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to 4 WeeksChange from Baseline to 8 Weeks (n=230, 233, 233)Change from Baseline to 16 Weeks (n=167, 147, 100)Change from Baseline to 24 Weeks (n=140, 116, 81)
Sildenafil Citrate On Demand26.5928.9233.8533.52
Tadalafil On Demand25.1829.1435.2335.86
Tadalafil Once a Day24.1027.8029.4631.14

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Change From Baseline to 4, 8, 16, and 24 Weeks of the Overall Relationship Domain of the Self-Esteem and Relationship (SEAR) Questionnaire

SEAR assesses psychosocial outcomes in men with erectile dysfunction. The Overall Relationship domain consists of 2 items (items 13-14), each rated on a scale of 1 (Never) to 5 (Always). The domain score was computed by summing its respective items, then transforming it into a 0 (least favorable) to 100 (most favorable) scale. The transformed score = 100 x [(actual raw score - lowest possible raw score)/possible raw score range]. Least Squares Mean changes were adjusted for baseline score, treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=229, 232, 232)Change from Baseline to Week 16 (n=166, 147, 100)Change from Baseline to Week 24 (n=139, 116, 81)
Sildenafil Citrate On Demand22.0023.7428.5728.74
Tadalafil On Demand19.9222.7529.6330.28
Tadalafil Once a Day21.1022.9626.9629.93

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Change From Baseline to 4, 8, 16 and 24 Weeks of the Sexual Encounter Profile (SEP)

Participant-assessed diary. Has 5 questions (Question[Q]1:erection achievement, Q2:successful penetration, Q3:successful intercourse, Q4:satisfied with erection, and Q5:satisfied with sexual experience) for each sexual encounter made over specified period of time. SEP Q1-Q5 scores determined as percentage of 'Yes' responses to each of 5 questions out of all sexual attempts recorded during the time period. Least Squares Mean changes from baseline to endpoint for each visit from a repeated measures analysis included terms for baseline score, treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Intervention"percentage of yes responses" (Least Squares Mean)
Q1:Change from Baseline to 4 WeeksQ1:Change from Baseline to 8 Weeks (n=224,231,229)Q1:Change from Baseline to 16 Weeks (n=166,146,99)Q1:Change from Baseline to 24 Weeks (n=139,115,81)Q2:Change from Baseline to 4 WeeksQ2:Change from Baseline to 8 Weeks (n=224,231,229)Q2:Change from Baseline to 16 Weeks (n=166,146,99)Q2:Change from Baseline to 24 Weeks (n=139,115,81)Q3:Change from Baseline to 4 WeeksQ3:Change from Baseline to 8 Weeks (n=224,231,229)Q3:Change from Baseline to 16 Weeks (n=166,146,99)Q3:Change from Baseline to 24 Weeks (n=139,115,81)Q4:Change from Baseline to 4 WeeksQ4:Change from Baseline to 8 Weeks (n=224,231,229)Q4:Change from Baseline to 16 Weeks (n=166,146,99)Q4:Change from Baseline to 24 Weeks (n=139,115,81)Q5:Change from Baseline to 4 WeeksQ5:Change from Baseline to 8 Weeks (n=224,231,229)Q5:Change from Baseline to 16 Weeks (n=166,146,99)Q5:Change from Baseline to 24 Weeks (n=139,115,81)
Sildenafil Citrate On Demand18.4120.4120.5820.3429.6434.0836.0735.9344.4552.1156.9656.2851.4559.2866.4869.0449.6355.7362.4066.57
Tadalafil On Demand14.5016.6218.4619.9727.4831.1632.7635.8341.5247.4554.2656.3949.5960.8666.1772.6746.1253.9261.5765.45
Tadalafil Once a Day18.4919.8819.1919.6028.5631.6632.7634.7041.7644.5850.6253.8351.7855.5963.0068.0645.7150.0654.5662.17

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Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Sexual Desire Domain

Self-reported sexual desire on IIEF over past 4 weeks; comprises 2 questions (items 11 and 12). Each question rated on a scale from 1 (almost never or low/no sexual desire) to 5 (almost always or very high sexual desire). Total scores range: 2 to 10; lower numerical scores denote lower sexual desire. Least Squares Mean changes from baseline to endpoint for each visit from repeated measures analysis and included terms for baseline score, treatment group, country, baseline*treatment (if p<0.10), visit, and visit*treatment. Correlation matrix for repeated observations assumed to be unstructured. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to 4 WeeksChange from Baseline to 8 Weeks (n=230, 232, 232)Change from Baseline to 16 Weeks (n=167, 146, 101)Change from Baseline to 24 Weeks (n=140, 117, 81)
Sildenafil Citrate On Demand0.690.871.071.29
Tadalafil On Demand0.770.961.151.19
Tadalafil Once a Day0.750.900.870.78

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Time to Discontinuation of Randomized Treatment

Time to discontinuation of randomized treatment was defined as the number of days from randomization until the day the participant discontinued the randomized treatment. Discontinuation of randomized treatment was defined as switching between the 3 study treatments (tadalafil on demand, tadalafil once a day, or sildenafil citrate on demand) or discontinuing from all treatments. A change of dose within the same treatment was not considered switching of treatment. This outcome measure was estimated using the Kaplan-Meier product-limit method. (NCT01122264)
Timeframe: Baseline up to 334 days

Interventiondays (Median)
Tadalafil On DemandNA
Tadalafil Once a Day130
Sildenafil Citrate On Demand67

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Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Overall Satisfaction Domain

Self-reported overall satisfaction on the IIEF over past 4 weeks and consists of 2 questions (items 13 and 14), each rated on a scale from 1 (very dissatisfied) to 5 (very satisfied). Total scores range from 2 to 10; lower numerical scores represent lower overall satisfaction. Least Squares Mean changes from baseline to endpoint for each visit were from a repeated measures analysis and included terms for baseline score, treatment group, country, baseline*treatment (if p<0.10), visit, and visit*treatment. The correlation matrix for the repeated observations was assumed to be unstructured. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=230, 231, 233)Change from Baseline to Week 16 (n=167, 145, 101)Change from Baseline to Week 24 (n=141, 116, 81)
Sildenafil Citrate On Demand2.722.983.483.41
Tadalafil On Demand2.462.803.343.50
Tadalafil Once a Day2.582.853.093.24

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Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Orgasmic Function Domain

Self-reported orgasmic function on the IIEF over past 4 weeks and consists of 2 questions (items 9 and 10). Each question is rated on a scale from 0 (no sexual stimulation) to 5 (almost always/always). Total scores range from 0 to 10; lower scores represent lower orgasmic function. Least Squares Mean changes from baseline to endpoint for each visit were from a repeated measures analysis and included terms for baseline score, treatment group, country, baseline*treatment (if p<0.10), visit, and visit*treatment. The correlation matrix for the repeated observations was assumed to be unstructured. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=231, 232, 232)Change from Baseline to Week 16 (n=167, 146, 101)Change from Baseline to Week 24 (n=141, 116, 81)
Sildenafil Citrate On Demand1.922.262.662.62
Tadalafil On Demand1.641.772.372.55
Tadalafil Once a Day1.752.082.252.48

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Change From Baseline to 4, 8, 16, and 24 Weeks of the Confidence Domain of the Self-Esteem and Relationship (SEAR) Questionnaire

SEAR assesses psychosocial outcomes in men with erectile dysfunction. Confidence domain measures improvement in confidence; 2 subscales (6 items: Self-Esteem [items 9-12]; Overall Relationship [items 13-14]). Each item range: 1 (Never) to 5 (Always); item 11 reverse scored. Domain score=sum of domain's respective items, then transformed into 0 (least favorable) to 100 (most favorable) scale. Transformed score=100x[(actual raw score-lowest possible raw score)/possible raw score range]. Least Squares Mean change adjusted for baseline score, treatment group, country, visit, and visit*treatment. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=230, 233, 232)Change from Baseline to Week 16 (n=167, 147, 100)Change from Baseline to Week 24 (n=140, 116, 81)
Sildenafil Citrate On Demand25.0327.1431.8631.66
Tadalafil On Demand23.4326.9733.1533.74
Tadalafil Once a Day23.0426.1028.3330.42

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Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Intercourse Satisfaction Domain

Self-reported intercourse satisfaction score over past 4 weeks (1 intercourse attempt item, 2 intercourse satisfaction items). Each item range: 0 (no intercourse attempts/no satisfaction) to 5 (more attempts/high satisfaction). Total scores range: 0-15; lower scores=lower intercourse satisfaction. Least Squares Mean changes from baseline to endpoint for each visit from repeated measures analysis and included terms for baseline score, treatment group, country, baseline*treatment (if p<0.10), visit, and visit*treatment. Correlation matrix for repeated observations assumed to be unstructured. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=231, 232, 232)Change from Baseline to Week 16 (n=167, 146, 101)Change from Baseline to Week 24 (n=141, 116, 81)
Sildenafil Citrate On Demand3.533.954.414.70
Tadalafil On Demand3.213.694.384.48
Tadalafil Once a Day3.223.153.603.71

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Change From Baseline to 4, 8, 16 and 24 Weeks of the International Index of Erectile Function (IIEF) Erectile Function (EF) Domain

Self-reported EF score over past 4 weeks. Items 1-5 scores range from 0 (no sexual activity) to 5 (high EF). Item 15 score ranges from 1 (very low confidence to get/keep erection) to 5 (very high confidence). Total scores range from 1 to 30; lower scores denote greater erectile dysfunction severity. Least Squares Mean changes from baseline to endpoint for each visit from repeated measures analysis included terms for baseline score, treatment group, country, baseline*treatment (if p<0.10), visit, and visit*treatment. Correlation matrix for repeated observations assumed to be unstructured. (NCT01122264)
Timeframe: Baseline, 4, 8, 16, and 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Change from Baseline to Week 4Change from Baseline to Week 8 (n=231, 232, 232)Change from Baseline to Week 16 (n=167, 146, 101)Change from Baseline to Week 24 (n=141, 116, 81)
Sildenafil Citrate On Demand8.869.7010.5611.05
Tadalafil On Demand7.928.9810.6010.70
Tadalafil Once a Day8.609.089.9310.01

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Change From Baseline to 24 Week Endpoint of the Sexual Self-Confidence, Spontaneity, and Time Concerns Domains (23-items) of the Psychological and Interpersonal Relationships Scale (PAIRS)

The PAIRS is a 23-item scale that assesses broader psychological/interpersonal outcomes associated with erectile dysfunction and its treatment. Each question is rated on a Likert scale from 1 (strongly disagree) to 4 (strongly agree). The scale consists of 3 domains: Sexual Self-Confidence (items 1-6), Spontaneity domain (items 7-15), and Time Concerns (items 16-23). The average domain score for each domain was calculated by adding the nonmissing items for the respective domain, then dividing by the number of nonmissing items for the respective domain. Each average domain score ranged from 1 to 4. Higher scores represent the following: greater sexual self-confidence (better outcome); greater spontaneity (better outcome); higher time concerns (worse outcome). The Least Squares Mean changes were adjusted for treatment group, country, baseline IIEF-EF severity, baseline domain score, and baseline domain score*treatment (if p<0.10). (NCT01122264)
Timeframe: Baseline, 24 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Sexual Self-Confidence Domain (n=196, 203, 185)Spontaneity Domain (n=197, 202, 186)Time Concerns Domain (n=196, 200, 184)
Sildenafil Citrate On Demand0.730.020.04
Tadalafil On Demand0.930.13-0.08
Tadalafil Once a Day0.900.11-0.20

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Number of Days From the 8-Week Study Visit to the Time the Participant Discontinues From All Phosphodiesterase Type 5 (PDE5) Inhibitor Treatments

The differences in time between the 8-week time point and the discontinuation of all study treatments (that is, discontinuation from the study and not switching to another treatment) are reported by the median (95% confidence interval). Duration was measured as the number of days from Week 8 to the date of the last dose of the study drug. This outcome measure was estimated using the Kaplan-Meier product-limit method. (NCT01122264)
Timeframe: 8 weeks up to 334 days

Interventiondays (Median)
Tadalafil On DemandNA
Tadalafil Once a DayNA
Sildenafil Citrate On Demand187

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Number of Treatment Switches

The number of times participants switched erectile dysfunction medication within the 3 treatments being studied (tadalafil on demand, tadalafil once a day, or sildenafil citrate on demand). (NCT01122264)
Timeframe: Baseline through 24 weeks

Interventionnumber of treatment switches (Mean)
Tadalafil On Demand1.2
Tadalafil Once a Day1.2
Sildenafil Citrate On Demand1.3

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Treatment Satisfaction Scale (TSS) - Partner Satisfaction With Medication Score at Week 12 Endpoint

The TSS - partner satisfaction with medication measured participant's partner satisfaction with treatment based on a 13-item questionnaire. The overall score was converted to a 0-100 scale with higher numbers on the scale indicating greater satisfaction. Satisfaction with medication was analyzed using analysis of covariance (ANOVA). The model included factors of study, treatment group, and pooled site within study. (NCT01130532)
Timeframe: Week 12

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)52.5
5 mg Tadalafil (Period III)55.7
Placebo (Period III)27.5

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Treatment Satisfaction Scale (TSS) - Patient Satisfaction With Medication Score at Week 12 Endpoint

The TSS - patient satisfaction with medication measured participant satisfaction with treatment based on a 13-item questionnaire. The overall score was converted to a 0-100 scale with higher numbers on the scale indicating greater satisfaction. Satisfaction with medication was analyzed using analysis of covariance (ANOVA). The model included factors of study, treatment group, and pooled site within study. (NCT01130532)
Timeframe: Week 12

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)53.7
5 mg Tadalafil (Period III)55.9
Placebo (Period III)24.8

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"Change From Baseline to 12-Week in Percentage of Yes Responses to Sexual Encounter Profile (SEP) Questions 1-5"

Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Questions 1-5. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

,,
Intervention"percentage of yes responses" (Least Squares Mean)
Question 1: Able to Achieve ErectionQuestion 2: Able to InsertQuestion 3: Successful IntercourseQuestion 4: Satisfied with HardnessQuestion 5: Overall Satisfaction with Experience
2.5 mg Titrated to 5 mg Tadalafil (Period III)12.226.237.344.243.6
5 mg Tadalafil (Period III)11.426.139.442.841.2
Placebo (Period III)1.86.912.611.510.6

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Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)7.9
5 mg Tadalafil (Period III)8.1
Placebo (Period III)1.8

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Change From 12 Weeks to 16 Weeks in Participant's International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. (NCT01130532)
Timeframe: 12 weeks and 16 weeks

,,
Interventionunits on a scale (Mean)
End of Week 12End of Week 16
2.5 mg Titrated to 5 mg Tadalafil (Period IV)22.424.1
5 mg Tadalafil (Period IV)22.524.2
Placebo (Period IV)16.024.4

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Change From Baseline to 12-Week Endpoint in Treatment Satisfaction Scale (TSS) - Partner

The TSS measured participant's partner satisfaction with treatment based on a 13-item questionnaire. The overall score for each of five TSS domains (confidence to complete sexual activity, ease of erection, pleasure from sexual activity, erectile function satisfaction, and satisfaction with orgasm) was converted to a 0-100 scale with higher numbers on the scale indicating greater satisfaction. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Confidence to complete sexual activityEase of erectionPleasure from sexual activityErectile function satisfactionSatisfaction with orgasm
2.5 mg Titrated to 5 mg Tadalafil (Period III)23.723.118.228.618.7
5 mg Tadalafil (Period III)27.225.318.528.521.0
Placebo (Period III)2.00.71.33.43.6

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Change From Baseline to 12-Week Endpoint in Treatment Satisfaction Scale (TSS) - Patient

The TSS measured participant satisfaction with treatment based on a 13-item questionnaire. The overall score for each of five TSS domains (confidence to complete sexual activity, ease of erection, pleasure from sexual activity, erectile function satisfaction, and satisfaction with orgasm) was converted to a 0-100 scale with higher numbers on the scale indicating greater satisfaction. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

,,
Interventionunits on a scale (Least Squares Mean)
Confidence to complete sexual activityEase of erectionPleasure from sexual activityErectile function satisfactionSatisfaction with orgasm
2.5 mg Titrated to 5 mg Tadalafil (Period III)27.024.022.631.025.6
5 mg Tadalafil (Period III)29.224.722.733.626.3
Placebo (Period III)3.84.13.34.96.2

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Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Intercourse Satisfaction (IIEF-IS) Domain Score

Self-reported intercourse satisfaction over the past 4 weeks. IIEF-IS is the sum of Questions 6, 7 and 8 of the IIEF. Scores range from 0 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 3 questions of 0 to 15. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)2.8
5 mg Tadalafil (Period III)2.6
Placebo (Period III)0.6

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Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function - Overall Satisfaction (IIEF-OS) Domain Score

Self-reported overall satisfaction over the past 4 weeks. IIEF-OS is the sum of Questions 13 and 14; each question scored as 1 (low/no satisfaction) through 5 (high satisfaction) with total subscore for the 2 questions of 2 to 10. Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)2.4
5 mg Tadalafil (Period III)2.4
Placebo (Period III)0.6

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Change From Baseline to 12-Week Endpoint in the International Index of Erectile Function (IIEF) Question 15 (Sexual Confidence)

Self-reported erectile function over the past 4 weeks. Question 15, confidence in the ability to get an erection, is scored from 1 (very low confidence) to 5 (very high confidence). Least Squares (LS) mean of the change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model included centered-baseline as a covariate and factors of study, treatment group, and pooled site within study, and centered-baseline-by-treatment-group interaction. (NCT01130532)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
2.5 mg Titrated to 5 mg Tadalafil (Period III)1.2
5 mg Tadalafil (Period III)1.3
Placebo (Period III)0.3

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Percentage of Participants Having an International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score Greater Than or Equal to 26 Through 12-Week Endpoint (Double-Blind Treatment Period)

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Data presented are the percentage of participants who return to normal erectile function (IIEF-EF domain score ≥26) at end of double-blind treatment period (Period III). (NCT01130532)
Timeframe: Baseline through 12 weeks

Interventionpercentage of participants (Number)
2.5 mg Titrated to 5 mg Tadalafil (Period III)38.7
5 mg Tadalafil (Period III)39.6
Placebo (Period III)12.1

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Percentage of Participants Having International Index of Erectile Function - Erectile Function (IIEF-EF) Domain Score Greater Than or Equal to 26 From 12 to 16 Weeks

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Data presented are the percentage of participants who return to normal erectile function (IIEF-EF domain score ≥26) at end of open-label extension treatment period (Period IV). (NCT01130532)
Timeframe: 12 weeks through 16 weeks

Interventionpercentage of participants (Number)
2.5 mg Titrated to 5 mg Tadalafil (Period IV)54.5
5 mg Tadalafil (Period IV)59.8
Placebo (Period IV)62.8

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"Change From Week 12 to Week 16 Percentage of Yes Responses to Sexual Encounter Profile (SEP) Questions 3"

"Assessed the percentage of Yes responses to the SEP diary Question 3 Did your erection last long enough for you to have successful intercourse? from Week 12 (end of double-Blind treatment) to Week 16 (end of open-label treatment)." (NCT01130532)
Timeframe: 12 weeks and 16 weeks

,,
Intervention"percentage of yes responses" (Mean)
End of Week 12End of Week 16
2.5 mg Titrated to 5 mg Tadalafil (Period IV)68.375.0
5 mg Tadalafil (Period IV)69.075.5
Placebo (Period IV)43.180.0

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30-Day Person Time Analysis Risk of NAION Associated With PDE5 Inhibitor Use

Total participant days of PDE5 inhibitor exposure within 30 days prior to onset of NAION. (NCT01131104)
Timeframe: 30 days prior to NAION onset

InterventionRelative risk of exposure (Number)
Cohort 12.27

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Patient Global Impression of Improvement (PGI-I) at 26 Weeks

Patient Global Impression of Improvement (PGI-I) measures the participant's perception of improvement at the time of assessment compared with the start of treatment. Number of participants is reported by the categorized score ranging from 1 (very much better) to 7 (very much worse). (NCT01139762)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
1 = Very much better2 = Much better3 = Little better4 = No change5 = A little worse6 = Much worse7 = Very much worse
Placebo298211252571
Tadalafil21124102491021

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Clinician Global Impression of Improvement (CGI-I) at 26 Weeks

Clinician Global Impression of Improvement (CGI-I) measures clinician's perception of participant improvement at the time of assessment compared with the start of treatment. Number of participants is reported by the categorized score ranging from 1 (very much better) to 7 (very much worse). (NCT01139762)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
1 = Very much improved2 = Much improved3 = Minimally improved4 = No change5 = Minimally worse6 = Much worse7 = Very much worse
Placebo2297106481061
Tadalafil231299847550

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Change in Total International Prostate Symptom Score (IPSS) From Baseline to 4 and 26 Weeks

The International Prostate Symptom Score (IPSS) is a rating scale for severity of lower urinary tract symptoms (LUTS). The IPSS has a 7-component questionnaire. Each question is scored on a scale from 0 (none/no symptoms) to 5 (frequent symptoms), for a total score range of 0 to 35. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks26 weeks
Placebo-2.29-4.47
Tadalafil-3.95-5.51

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Change in International Prostate Symptom Score (IPSS) Subscores Index From Baseline to 4, 12, and 26 Weeks

IPSS storage (irritative) subscore is the sum of Questions 2, 4 and 7 of the 7-component IPSS questionnaire. Scores range from 0 (no irritative symptoms) to 5 (frequent irritative symptoms), with total subscore of the 3 questions for irritative subscore range from 0 to 15. IPSS voiding (obstructive) subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (no obstructive symptoms) to 5 (frequent obstructive symptoms), with total subscore of the 4 questions of the obstructive score range from 0 to 20. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
IPSS storage (irritative) subscore - 4 weeksIPSS storage (irritative) subscore - 12 weeksIPSS storage (irritative) subscore - 26 weeksIPSS voiding (obstructive) subscore - 4 weeksIPSS voiding (obstructive) subscore - 12 weeksIPSS voiding (obstructive) subscore - 26 weeks
Placebo-0.76-1.34-1.66-1.47-2.37-2.77
Tadalafil-1.27-1.74-2.00-2.65-3.41-3.50

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Change in International Prostate Symptom Score (IPSS) Quality of Life Index From Baseline to 4, 12, and 26 Weeks

"IPSS Quality of Life Index assesses participant response to the following question: If you were to spend the rest of your life with your urinary condition just the way it is now, how would you feel about that? Response options are Delighted (0); Pleased (1); Mostly satisfied (2); Mixed-about equally satisfied and dissatisfied (3); Mostly dissatisfied (4); Unhappy (5); Terrible (6), with a total range of 0-6. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction." (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.32-0.76-0.92
Tadalafil-0.63-0.95-1.10

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Change in International Index of Erectile Function (IIEF) Question 3 and 4 Scores From Baseline to 4, 12, and 26 Weeks

IIEF Question 3 asks how often a participant was able to penetrate his partner over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). IIEF Question 4 asks whether/how often a participant was able to maintain an erection after penetration over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
Question 3 - 4 weeksQuestion 3 - 12 weeksQuestion 3 - 26 weeksQuestion 4 - 4 weeksQuestion 4 - 12 weeksQuestion 4 - 26 weeks
Placebo-0.320.04-0.07-0.210.130.06
Tadalafil0.420.720.680.490.740.68

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Change in International Index of Erectile Function (IIEF) - Sexual Desire Domain Scores From Baseline to 4, 12, and 26 Weeks

Sexual desire domain scores is the sum of Questions 11 and 12 from the IIEF questionnaire. Scores range from 1 (low/no desire) to 5 (high desire) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Higher total scores indicate higher desire. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.47-0.23-0.05
Tadalafil0.460.560.71

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Change in International Index of Erectile Function (IIEF) - Overall Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported overall satisfaction over the past 4 weeks. IIEF-Overall Satisfaction is the sum of Questions 13 and 14 of IIEF questionnaire. Scores range from 1 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Higher total scores indicate higher satisfaction. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.100.310.40
Tadalafil0.911.381.61

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Change in International Index of Erectile Function (IIEF) - Orgasmic Function Domain Scores From Baseline to 4, 12, and 26 Weeks

Orgasmic Function domain scores is the sum of Questions 9 and 10 from the IIEF questionnaire. Scores range from 0 (low/no orgasm) to 5 (high orgasm) for each question, with the total possible score for the 2 questions ranging from 0 to 10. Higher total scores indicate higher orgasm. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.630.18-0.18
Tadalafil0.901.080.89

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Change in International Index of Erectile Function (IIEF) - Intercourse Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported intercourse satisfaction over the past 4 weeks. IIEF-intercourse satisfaction is the sum of Questions 6, 7 and 8 of the IIEF. Scores range from 0 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 3 questions of 0 to 15. Higher total scores indicate higher satisfaction. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.460.08-0.26
Tadalafil1.361.681.72

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Change in International Index of Erectile Function (IIEF) - Erectile Function Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-1.140.63-0.02
Tadalafil3.714.714.71

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Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 26 Weeks

The TSS-BPH was a validated participant-rated instrument that measured participant satisfaction with treatment based on a 13-item questionnaire. It consists of 10 items on a Likert-like scale with scores ranging from 1 (higher satisfaction) to 5 (lower satisfaction), 1 item with score ranging from 0 (higher satisfaction) to 5 (lower satisfaction), and 2 yes/no questions. The mean score for each participant ranges from 0.9 (higher satisfaction) to 5.0 (lower satisfaction). Data presented are the average of mean scores for each treatment group. (NCT01139762)
Timeframe: 26 weeks

Interventionunits on a scale (Mean)
Tadalafil2.0
Placebo2.1

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Change in Post Void Residual (PVR) Volume From Baseline to 26 Weeks

Postvoid Residual Volume (PVR) is determined using a portable, calibrated ultrasound device. It consists of the average of a minimum of 3 scans where the residual bladder volume was calculated by averaging the most accurate of the 3 imaging attempts. (NCT01139762)
Timeframe: Baseline, 26 weeks

Interventionmilliliters (mL) (Mean)
Tadalafil-24.8
Placebo-23.1

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Change in Total International Prostate Symptom Score (IPSS) From Baseline to 12 Weeks

The International Prostate Symptom Score (IPSS) is a rating scale for severity of lower urinary tract symptoms (LUTS). The IPSS has a 7-component questionnaire. Each question is scored on a scale from 0 (none/no symptoms) to 5 (frequent symptoms), for a total score range of 0 to 35. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil-5.18
Placebo-3.76

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Change From Baseline to 4 and 8 Weeks in Arterial Resistive Index (RI) in the Prostate Peripheral Zone and Bladder Neck

Arterial RI was a measure of vascular resistance using Doppler ultrasound. RI was the ratio of (peak systolic velocity - end diastolic velocity)/peak systolic velocity, and increased as resistance to flow increased. The least squares (LS) mean was estimated from a mixed-effects model with repeated measures (MMRM) that included fixed effects for treatment, region, visit, and treatment-by-visit interaction, baseline as a covariate, a random effect of participant within treatment, and an unstructured covariance matrix. (NCT01152190)
Timeframe: Baseline, Week 4 and Week 8

,
Interventionratio (Least Squares Mean)
Week 4 Change, Prostate Peripheral Zone (n=45, 43)Week 8 Change, Prostate Peripheral Zone (n=43, 38)Week 4 Change, Bladder Neck (n=30, 30)Week 8 Change, Bladder Neck (n=32, 26)
Placebo0.00-0.01-0.010.01
Tadalafil0.010.010.010.02

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Change From Baseline to 8-Week Endpoint in Arterial Resistive Index (RI) in the Prostate Transition Zone

Arterial RI was a measure of vascular resistance using Doppler ultrasound. RI was the ratio of (peak systolic velocity - end diastolic velocity)/peak systolic velocity, and increased as resistance to blood flow increased. The least squares (LS) mean was estimated from a mixed-effects model with repeated measures (MMRM) that included fixed effects for treatment, region, visit, and treatment-by-visit interaction, baseline as a covariate, a random effect of participant within treatment, and an unstructured covariance matrix. (NCT01152190)
Timeframe: Baseline, Week 8

Interventionratio (Least Squares Mean)
Placebo-0.01
Tadalafil0.00

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Change From Baseline to 4-Week Endpoint in Arterial Resistive Index (RI) in the Prostate Transition Zone

Arterial RI was a measure of vascular resistance using Doppler ultrasound. RI was the ratio of (peak systolic velocity - end diastolic velocity)/peak systolic velocity, and increased as resistance to flow increased. The least squares (LS) mean was estimated from a mixed-effects model with repeated measures (MMRM) that included fixed effects for treatment, region, visit, and treatment-by-visit interaction, baseline as a covariate, a random effect of participant within treatment, and an unstructured covariance matrix. (NCT01152190)
Timeframe: Baseline, Week 4

Interventionratio (Least Squares Mean)
Placebo0.00
Tadalafil0.01

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Change From Baseline to 4 and 8 Weeks in Color Pixel Intensity (CPI) in the Prostate Transition Zone, Peripheral Zone, and Bladder Neck

CPI quantified blood flow in a pre-specified region of interest by using color Doppler imaging. CPI was the mean color pixel intensity in the region of interest and scores could range from 0 to 160. An increase in CPI reflected an increase in blood flow. The least squares (LS) mean was estimated from a mixed-effects model with repeated measures (MMRM) that included fixed effects for treatment, region, visit, and treatment-by-visit interaction, baseline as a covariate, a random effect of participant within treatment, and an unstructured covariance matrix. (NCT01152190)
Timeframe: Baseline, Week 4 and Week 8

,
Interventionunits on a scale (Least Squares Mean)
Week 4 Change, Prostate Transition Zone (n=44, 43)Week 8 Change, Prostate Transition Zone (n=43, 38)Week 4 Change, Prostate Peripheral Zone (n=44, 43)Week 8 Change, Prostate Peripheral Zone (n=43, 38)Week 4 Change, Bladder Neck (n=42, 40)Week 8 Change, Bladder Neck (n=38, 36)
Placebo-2.212.02-1.483.117.37-0.13
Tadalafil0.422.531.992.553.177.81

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Change From Baseline to 12 Week Endpoint in Total Cholesterol and Triglycerides

The least squares (LS) mean was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

,,,,
Interventionmillimoles per Liter (mmol/L) (Least Squares Mean)
Total CholesterolTriglycerides
1 mg LY2452473 and 5 mg Tadalafil-0.210-0.155
10 mg Tadalafil-0.086-0.139
5 mg LY2452473-0.282-0.067
5 mg LY2452473 and 5 mg Tadalafil-0.275-0.171
5 mg Tadalafil-0.0590.056

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Percent Change From Baseline to 12 Week Endpoint in High-Density Lipoprotein Cholesterol (HDL-C) and Low-Density Lipoprotein Cholesterol (LDL-C)

The least squares (LS) was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

,,,,
Interventionpercent change (Least Squares Mean)
HDL-CLDL-C
1 mg LY2452473 and 5 mg Tadalafil-7.440-1.695
10 mg Tadalafil1.776-0.066
5 mg LY2452473-22.230-3.424
5 mg LY2452473 and 5 mg Tadalafil-16.9740.062
5 mg Tadalafil1.573-0.718

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Change From Baseline to 12 Week Endpoint in IIEF EF Domain Score Reported by Testosterone Concentration Subgroups

The International Index of Erectile Function (IIEF) EF was the sum of Questions (Q) 1 to Q5 and Q15 of the IIEF Self-reported questionnaire. Q1 to Q5 were rated 0 (low/no erectile function) to 5 (high erectile function) and Q15 was rated 1 (no/low confidence) to 5 (high confidence). IIEF EF domain scores ranged from 1 to 30. Higher scores denoted better EF. Testosterone concentration subgroups were based on optimal baseline testosterone levels (<340 nanograms per deciliter [ng/dL] or ≥340 ng/dL). The least squares (LS) mean was estimated from an analysis of covariance (ANCOVA) model that included terms for treatment group, baseline, and baseline*treatment interaction (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

,,,,
Interventionunits on a scale (Least Squares Mean)
Testosterone <340 ng/dLTestosterone ≥340 ng/dL
1 mg LY2452473 and 5 mg Tadalafil2.5231.077
10 mg Tadalafil4.1722.217
5 mg LY2452473-1.055-0.714
5 mg LY2452473 and 5 mg Tadalafil1.0123.416
5 mg Tadalafil1.9351.703

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Change From Baseline to 12 Week Endpoint in IIEF Domain Scores (Intercourse Satisfaction, Orgasmic Function, Sexual Desire, and Overall Satisfaction)

Intercourse Satisfaction (IS) domain score: sum of Questions (Q) 6, Q7, and Q8, each rated 0 (low/no satisfaction) to 5 (high satisfaction). IS domain score range: 0 to 15; lower scores denoted lower satisfaction. Orgasmic Function (OF) domain score: sum of Q9 and Q10, each rated 0 (no sexual stimulation) to 5 (almost always/always). OF domain score range: 0 to 10; lower scores denoted lower OF. Sexual Desire (SD) domain score: sum of Q11 and Q12, each rated 1 (almost never or low/no sexual desire) to 5 (almost always or very high sexual desire). SD domain score range: 2 to 10; lower scores denoted lower SD. Overall Satisfaction (OS) domain score: sum of Q13 and Q14, each rated 1 (low/no satisfaction) to 5 (high satisfaction). OS domain score range: 2 to 10; lower scores denoted lower OS. Least squares (LS) mean estimated from repeated measures analysis of variance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

,,,,
Interventionunits on a scale (Least Squares Mean)
Intercourse SatisfactionOrgasmic FunctionSexual DesireOverall Satisfaction
1 mg LY2452473 and 5 mg Tadalafil0.4750.5100.0920.477
10 mg Tadalafil1.1270.6780.3921.206
5 mg LY2452473-0.6720.160-0.201-0.378
5 mg LY2452473 and 5 mg Tadalafil0.5140.1170.0010.258
5 mg Tadalafil0.5540.7330.1800.826

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"Change From Baseline to 12 Week Endpoint in the Percentage of Yes Responses on the Sexual Encounter Profile (SEP) Diary"

"The SEP diary was a participant-assessed diary with 5 questions (Q): Q1 (erection achievement), Q2 (successful penetration), Q3 (successful intercourse), Q4 (satisfied with erection), and Q5 (satisfied with sexual experience) for each sexual encounter made over a specified period of time. SEP Q1 to Q5 scores were determined as a percentage of Yes responses to each of the 5 questions out of all sexual attempts recorded during the time period. A higher percentage of Yes responses indicated better EF. Assessed was the mean change from baseline in the percentage of Yes responses to the SEP diary Q1 to Q5. The least squares (LS) mean was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value <0.25)." (NCT01160289)
Timeframe: Baseline, Week 12

,,,,
Intervention"percentage of yes responses" (Least Squares Mean)
Question 1Question 2Question 3Question 4Question 5
1 mg LY2452473 and 5 mg Tadalafil-0.2473.1759.29612.93513.602
10 mg Tadalafil4.42710.26714.64524.20222.410
5 mg LY2452473-10.711-7.849-3.800-1.570-1.956
5 mg LY2452473 and 5 mg Tadalafil-2.9763.68911.75213.91015.196
5 mg Tadalafil-1.4251.8442.5938.8579.400

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Change From Baseline to 12 Week Endpoint in Prostate-Specific Antigen (PSA)

The least squares (LS) mean was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

Interventionnanograms per milliliter (ng/mL) (Least Squares Mean)
1 mg LY2452473 and 5 mg Tadalafil0.162
5 mg LY2452473 and 5 mg Tadalafil-0.088
5 mg LY24524730.265
10 mg Tadalafil0.246
5 mg Tadalafil0.032

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Change From Baseline to 12 Week Endpoint in Fasting Insulin

Change from baseline to 12 Week endpoint in fasting blood insulin concentration. The least squares (LS) mean was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

Interventionmilliunits per Liter (mU/L) (Least Squares Mean)
1 mg LY2452473 and 5 mg Tadalafil3.756
5 mg LY2452473 and 5 mg Tadalafil-4.501
5 mg LY2452473-0.717
10 mg Tadalafil-3.300
5 mg Tadalafil-1.276

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Change From Baseline to 12 Week Endpoint in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain Score

The IIEF EF domain score was the sum of Questions (Q) 1 to Q5 and Q15 of the IIEF self-reported questionnaire. Q1 to Q5 were rated 0 (low/no EF) to 5 (high EF) and Q15 was rated 1 (no/low confidence) to 5 (high confidence). IIEF EF domain scores ranged from 1 to 30. Higher scores denoted better EF. (NCT01160289)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Mean)
1 mg LY2452473 and 5 mg Tadalafil2.515
5 mg LY2452473 and 5 mg Tadalafil2.405
5 mg LY2452473-0.971
10 mg Tadalafil3.530
5 mg Tadalafil2.054

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25)"-NCT01160289">

"Change From Baseline to 12 Week Endpoint in the Percentage of Participants Who Return to Normal on the International Index of Erectile Function (IIEF) Scale (EF>25)"

The percentage of participants whose IIEF Erectile Function (EF) domain scores changed from ≤25 at baseline to >25 (normal) at Week 12. The IIEF EF domain score was the sum of IIEF Question (Q) 1 to Q5 and Q15. Q1 to Q5 were rated 0 (low/no EF) to 5 (high EF) and Q15 was rated 1 (no/low confidence) to 5 (high confidence). IIEF EF domain scores ranged from 1 to 30. Higher scores denoted better EF. (NCT01160289)
Timeframe: Baseline, Week 12

Interventionpercentage of participants (Number)
1 mg LY2452473 and 5 mg Tadalafil24.7
5 mg LY2452473 and 5 mg Tadalafil27.8
5 mg LY245247313.5
10 mg Tadalafil30.3
5 mg Tadalafil27.6

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Change From Baseline to 12 Week Endpoint in Fasting Glucose

The least squares (LS) mean was estimated from a repeated measures analysis of covariance model that included terms for treatment, visit, treatment*visit, baseline, baseline*treatment (if p-value<0.25). (NCT01160289)
Timeframe: Baseline, Week 12

Interventionmillimoles per Liter (mmol/L) (Least Squares Mean)
1 mg LY2452473 and 5 mg Tadalafil0.153
5 mg LY2452473 and 5 mg Tadalafil-0.306
5 mg LY24524730.070
10 mg Tadalafil-0.234
5 mg Tadalafil0.158

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Change From Baseline in Borg Dyspnea Index at Week 24

Borg Dyspnea Index (BDI) indicates the degree of breathlessness after completion of the 6 minute walk test. The BDI was calculated by using the Borg category (C) ratio (R) CR10 scale which starts at 0 (nothing at all) and has no upper limit (extremely strong). Change from BL was calculated as the Week 24 values minus the BL value. The BDI scale was assessed by each participant. The BL BDI score is the average of the two BDI values obtained following the two 6MWD tests used in determining the BL 6MWD. A negative change from BL in the BDI score represented an improvement for the participant. The analysis was performed based on the last observation carried forward data, except in the case of an adjudicated clinical failure event of death or hospitalization preceding the missing data observation. In this case, the missing observation was assigned the worst-rank score relative to those actually observed and was assigned rank reflecting the relative order of the actual event times. (NCT01178073)
Timeframe: Baseline (BL) and Week 24

InterventionScores on a scale (Median)
Combination Therapy: Ambrisentan + Tadalafil-1.00
Monotherapy Pooled: Ambrisentan or Tadalafil-0.50
Ambrisentan Monotherapy-0.50
Tadalafil Monotherapy-0.50

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Number of Participants With First Adjudicated Clinical Failure (CF) Event, Death, Hospitalisation for Worsening PAH, Disease Progression, Unsatisfactory Long-term Clinical Response, All Through FAV

Time to the first adjudicated CF event (death, hospitalization for worsening pulmonary arterial hypertension [PAH], disease progression, or unsatisfactory long-term clinical response) after initiating either first-line combination therapy with AMB and TAD or first-line monotherapy with either drug (AMB or TAD) in par. with PAH was assessed. If data was not available for some par. following a loss to follow-up, their event times were treated as censored at their last assessment time for the statistical analyses. FAV occurred approximately 4 weeks after the predicted 105th adjudicated first CF event was reached. Par. who had an FAV, and who had no adjudicated events or whose first adjudicated event occurred after their FAV, were censored at their individual FAV. Modified Intent-to-Treat (mITT) Population: all randomized par. who met the PAH diagnosis and inclusion/exclusion criteria defined in protocol amendment 2 and who also received at least one dose of investigational product (IP). (NCT01178073)
Timeframe: From Baseline up to the Final Assessment Visit (FAV) (average of 609 days)

,,,
InterventionParticipants (Number)
First adjudicated clinical failure eventDeath (all-cause)Hospitalization for worsening PAHDisease progressionUnsatisfactory long-term clinical response
Ambrisentan Monotherapy432181211
Combination Therapy: Ambrisentan + Tadalafil469101017
Monotherapy Pooled: Ambrisentan or Tadalafil778301623
Tadalafil Monotherapy34612412

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Percentage of Participants With a Satisfactory Clinical Response at Week 24

A satisfactory clinical response at Week 24 is defined as a participant who meets all of the following criteria: 10% improvement in 6MWD compared with Baseline; improvement to or maintenance of World Health Organization (WHO) class I or II symptoms; no events of clinical worsening prior to or at the Week 24 visit. Clinical worsening events included: death, hospitalization for pulmonary arterial hypertension (PAH), and disease progression. Participants without an event of clinical worsening prior to or at the Week 24 visit who did not have a 6MWD value or a WHO functional class value at Week 24 were excluded from the analysis. (NCT01178073)
Timeframe: Baseline and Week 24

InterventionPercentage of participants (Number)
Combination Therapy: Ambrisentan + Tadalafil39
Monotherapy Pooled: Ambrisentan or Tadalafil29
Ambrisentan Monotherapy31
Tadalafil Monotherapy27

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Change From Baseline in the 6 Minute Walk Distance Test at Week 24

The 6-minute walk distance (6MWD) test measures the distance that a participant can walk in a period of 6 minutes. Change from Baseline was calculated as the Week 24 value minus the Baseline value. The analysis was performed based on last observation carried forward data, except in the case of an adjudicated clinical failure event of death or hospitalization preceding the missing data observation. In this case, the missing observation was assigned the worst-rank score relative to those actually observed and was assigned a rank reflecting the relative order of the actual event times. Baseline 6MWD comprised of an average of the last two consecutive measurements prior to randomization that varied by no greater than 10%. If only one measurement was available, that measurement was used. If no two consecutive measures vary by no greater than 10% then Baseline was based on the last two consecutive measures for a participant. (NCT01178073)
Timeframe: Baseline and Week 24

InterventionMeters (Median)
Combination Therapy: Ambrisentan + Tadalafil48.98
Monotherapy Pooled: Ambrisentan or Tadalafil23.80
Ambrisentan Monotherapy27.00
Tadalafil Monotherapy22.70

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Change From Baseline in the World Health Organization Functional Class at Week 24

The WHO Functional Class (FC) indicates the severity of PAH and is an adaptation of the New York Heart Association classification. It was assessed by the investigator. There are four grades for WHO FC based on severity of symptoms (Class I = none, Class IV = most severe). Baseline WHO FC is the latest assessment prior to dosing (i.e., at Randomization or Screening). Change from Baseline at Week 24 was calculated as the Week 24 value minus the Baseline value. The analysis was performed based on the last observation carried forward data, except in the case of an adjudicated clinical failure event of death or hospitalization preceding the missing data observation. In this case, the missing observations was assigned the worst-rank score relative to those actually observed and was assigned rank reflecting the relative order of the actual event times. (NCT01178073)
Timeframe: Baseline and Week 24

InterventionScores on a scale (Median)
Combination Therapy: Ambrisentan + Tadalafil0.0
Monotherapy Pooled: Ambrisentan or Tadalafil0.0
Ambrisentan Monotherapy0.0
Tadalafil Monotherapy0.0

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Percent Change From Baseline in the N-Terminal Pro-B-Type Natriuretic Peptide at Week 24

N-Terminal Pro-B-Type Natriuretic Peptide (NT-proBNP) is a surrogate marker of heart failure. The data were log-transformed. The geometric mean was calculated (based on the log-transformed data). The geometric mean ratio was calculated as the ratio between the Week 24 value and the Baseline value (based on the log-transformed data) and presented as percent change = 100 * (geometric mean ratio - 1). The Baseline value is the last value prior to administration of study drug; this may be prior to or on the day of study drug initiation. No imputation was performed for missing data. The secondary endpoints were analyzed according to a pre-specified hierarchical testing procedure. (NCT01178073)
Timeframe: Baseline and Week 24

InterventionPercent change (Mean)
Combination Therapy: Ambrisentan + Tadalafil-67.15
Monotherapy Pooled: Ambrisentan or Tadalafil-50.37
Ambrisentan Monotherapy-56.15
Tadalafil Monotherapy-43.83

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Pharmacokinetics: Area Under the Concentration Curve (AUC) for Tadalafil and Metabolite IC710

AUC for Day 1 is reported as AUC(tau [t], day 1), which is AUC from time zero to 24 hours (t) postdose on Day 1. AUC for Day 10 is reported as AUC(t,steady state [ss]), which is AUC during one 24-hour dosing interval at steady-state. (NCT01183650)
Timeframe: 1 day and 10 days

,
Interventionnanograms*hour/milliliter (ng*hr/mL) (Geometric Mean)
Day 1 TadalafilDay 10 TadalafilDay 1 Metabolite IC710Day 10 Metabolite IC710
Caucasian Participants134034103992290
Japanese Participants141027105252270

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Pharmacokinetics: Concentration Maximum (Cmax) of Tadalafil and Metabolite IC710

(NCT01183650)
Timeframe: 1 day and 10 days

,
Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Day 1 TadalafilDay 10 TadalafilDay 1 Metabolite IC710Day 10 Metabolite IC710
Caucasian Participants10421524.0102
Japanese Participants10217332.1105

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Pharmacokinetics: Time to Concentration Maximum (Tmax) of Tadalafil and Metabolite IC710

(NCT01183650)
Timeframe: 1 day and 10 days

,
Interventionhours (Median)
Day 1 TadalafilDay 10 TadalafilDay 1 Metabolite IC710Day 10 Metabolite IC710
Caucasian Participants2.002.5324.008.00
Japanese Participants4.003.0023.834.00

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6 Minute Walk Distance

How far the subject walked in 6 minutes. (NCT01272388)
Timeframe: Baseline and 4 weeks

Interventionfeet (Number)
Baseline4 weeks
Tadalafil1080860

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Quality of Life as Assessed by the Kansas City Cardiomyopathy Questionnaire (KCCQ)

KCCQ overall summary score is reported. Scale is 0-100 (higher value is better). (NCT01272388)
Timeframe: Baseline and 4 weeks

Interventionunits on a scale (Number)
Baseline4 weeks
Tadalafil8781.25

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Diastolic Function as Measured by Tissue Doppler e'

Measurement of e' (average of septal and lateral) on echo at each of the time points specified. (NCT01275339)
Timeframe: Baseline, 12 weeks, and 6 months

,,
Interventioncm/sec (Mean)
Baseline12 weeks6 months
Placebo in Non-Diabetic Cohort5.284.885.33
Tadalafil in Diabetic Cohort4.593.754.63
Tadalafil in Non-Diabetic Cohort5.976.446.16

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Change in NYHA/WHO Class

"At 48 week,WHO/NYHA functional class was assessed for change in WHO/NYHA functional class.Change NYHA is measured as decrease or increase in NYHA class in the subjects compared with baseline.~NYHA /WHO functional class is described below:~NYHA functional class I:no symptoms and no limitation in ordinary physical activity NYHA functional class II:Mild symptoms (mild shortness of breath and/or angina) and slight limitation during ordinary activity NYHA functional class III:Marked limitation in activity due to symptoms, even during less-than-ordinary activity NYHA functional class IV:Severe limitations. Experiences symptoms even while at rest A higher functional class represent worse symptoms." (NCT01305252)
Timeframe: Baseline and 48 week

Interventionparticipants (Number)
Tadalafil Alone6
Tadalafil and Treprostinil Inhalations11

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Change in Right Ventricular Ejection Fraction

Effect of dual-upfront therapies versus mono-therapy on percent change of right ventricular function assesed by cardiac MRI (cMRI) at 24 weeks compared with the baseline. (NCT01305252)
Timeframe: Basline and 24 weeks

Interventionpercent change (Mean)
Tadalafil and Treprostinil Inhalations7.45
Tadalafil Alone2.8

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N-terminal Pro B-type Natriuretic Peptide (NT-proBNP)

Change from baseline in N-terminal Pro B-type Natriuretic Peptide (NT-proBNP) (NCT01305252)
Timeframe: Baseline and 24 weeks

Interventionpg/mL (Mean)
Tadalafil and Treprostinil Inhalations1239
Tadalafil Alone988.4

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B-type Natriuretic Peptide (BNP)

B-type Natriuretic peptide measures the percent change from baseline. (NCT01305252)
Timeframe: Baseline and 24 weeks

Interventionpercent change (Mean)
Tadalafil Alone374
Tadalafil and Treprostinil Inhalations295.6

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6 Minute Walk Distance

Change in 6MWD during 24 week period compared between Tada and Tada+iTre. (NCT01305252)
Timeframe: Baseline and 24 weeks

Interventionmeters (Mean)
Tadalafil Alone82.63
Tadalafil and Treprostinil Inhalations87.69

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Short Form-36 Global Score

SF- 36 investigates the standard of quality of life through a general health assessment and not specific to a particular disease, age or treatment group. It is a 36-item questionnaire measuring 8 domains (physical functioning, role physical, bodily pain, general health, vitality, social functioning, role emotional, and mental health). Each domain score ranges from 0 (worst) to 100 (best), with higher scores reflecting better health-related functional status. The global score is determined by taking an average of the individual domain scores. The global score range is from 0 (worst) to 100 (best). (NCT01324999)
Timeframe: Baseline, Week 8, Week 16, Week 24

Interventionunits on a scale (Mean)
BaselineWeek 8Week 16Week 24
Tadalafil38.537.739.238.9

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Resting Oxygen Saturation

Percent oxygen saturation of hemoglobin as measured by pulse oximetry in the resting state. (NCT01324999)
Timeframe: Baseline, Week 24

Interventionpercent (Mean)
BaselineWeek 24
Tadalafil96.595.2

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Oxygen Desaturation During 6 Minute Walk Test

Change (decrease) in oxygen saturation from start of 6 minute walk to nadir during the 6 minute walk test (NCT01324999)
Timeframe: Baseline, Week 24

Interventionoxygen saturation percentage points (Mean)
BaselineWeek 24
Tadalafil99

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Number of Participants With Change in WHO Functional Class (WHO FC)

The WHO functional classification ranges from I (patient's disease does not affect daily activities) to IV (patient's disease causes severe impairment). Higher scores indicate more severe impairment. (NCT01324999)
Timeframe: Baseline, Week 24

Interventionparticipants (Number)
Number of participants that improved to WHO FC INumber of participants that improved to WHO FC IINumber of participants that improved to WHO FC III
Tadalafil100

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Maximum Borg Dyspnea Score During 6 Minute Walk Test

The modified Borg scale consists of a vertical scale labelled 0 to10 with corresponding verbal expressions of progressively increasing sensation (shortness of breath) intensity. 0 represents no dyspnea, and 10 is the highest level of perceived dyspnea. (NCT01324999)
Timeframe: Baseline, Week 8, Week 16, Week 24

Interventionunits on a scale (Mean)
BaselineWeek 8Week 16Week 24
Tadalafil4.85.05.36.3

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Brain Natriuretic Peptide Level

(NCT01324999)
Timeframe: Baseline, Week 8, Week 16, Week 24

Interventionpg/mL (Mean)
BaselineWeek 8Week 16Week 24
Tadalafil58.832.337.542.6

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St. George's Respiratory Questionnaire (SGRQ) Score

The SGRQ ranges from 0 (no impairment of quality of life) to 100 (highest impairment of quality of life) (NCT01324999)
Timeframe: Baseline, Week 8, Week 16, Week 24

Interventionunits on a scale (Mean)
BaselineWeek 8Week 16Week 24
Tadalafil64.565.164.371.1

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6 Minute Walk Distance

(NCT01324999)
Timeframe: Baseline, Week 8, Week 16, Week 24

Interventionmeters (Mean)
BaselineWeek 8Week 16Week 24
Tadalafil419.1418.1436.5377.1

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Change in PAIRS Spontaneity Domain

PAIRS was a self-administered, 29-item scale that assessed the broader psychological and interpersonal outcomes associated with ED and its treatment. Each question was rated on a Likert scale that ranged from 1 (strongly disagree) to 4 (strongly agree). The spontaneity domain score was the average score for Items 3, 12, 13, 16, 17, 19, 21, 22, and 28. Spontaneity domain scores ranged from 1 (strongly disagree) to 4 (strongly agree). Change was defined as endpoint minus baseline domain score. Change in PAIRS spontaneity domain at Week 8 and Week 18 were averaged to produce an overall change in PAIRS spontaneity domain score. Higher scores were indicative of greater spontaneity. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil0.33
Sildenafil0.20

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Change in International Index of Erectile Function (IIEF) Erectile Function Domain

Self-reported erectile function over the past 4 weeks. IIEF erectile function was the sum of Q1 through Q5 and Q15 of the IIEF. Q1 through Q5 were scored 0 (low/no erectile function) to 5 (high erectile function) and Q15 was scored 1 (no/low confidence) to 5 (high confidence). IIEF erectile function domain scores ranged from 1 to 30. Change was defined as endpoint minus baseline domain score. Change in IIEF erectile function domain at Week 8 and Week 18 were averaged to produce an overall change in IIEF EF domain score. Higher scores were indicative of better erectile function. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil12.03
Sildenafil11.86

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Change in International Index of Erectile Function (IIEF) Intercourse Satisfaction Domain

Self-reported intercourse satisfaction over the past 4 weeks. IIEF intercourse satisfaction was the sum of Q6, Q7, and Q8 of the IIEF. Scores ranged from 0 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 3 questions ranging from 0 to 15. Change was defined as endpoint minus baseline domain score. Change in IIEF intercourse satisfaction domain at Week 8 and Week 18 were averaged to produce an overall change in IIEF intercourse satisfaction domain score. Higher scores were indicative of an increase in intercourse satisfaction. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil5.88
Sildenafil5.91

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Change in International Index of Erectile Function (IIEF) Orgasmic Function Domain

Self-reported orgasmic function over the past 4 weeks. IIEF orgasmic function was the sum of Q9 and Q10 of the IIEF. Scores ranged from 0 (no stimulation) to 5 (almost always) for each question, with the total possible score for the 2 questions ranging from 0 to 10. Change was defined as endpoint minus baseline domain score. Change in IIEF orgasmic function domain at Week 8 and Week 18 were averaged to produce an overall change in IIEF orgasmic function domain score. Higher scores were indicative of better orgasmic function. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil3.70
Sildenafil3.71

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Change in International Index of Erectile Function (IIEF) Overall Satisfaction Domain

Self-reported overall satisfaction over the past 4 weeks. IIEF overall satisfaction was the sum of Q13 and Q14. Scores ranged from 1 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Change was defined as endpoint minus baseline domain score. Change in IIEF overall satisfaction domain at Week 8 and Week 18 were averaged to produce an overall change in IIEF overall satisfaction domain score. Higher IIEF overall satisfaction domain scores were indicative of greater overall satisfaction. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil3.74
Sildenafil3.71

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Change in International Index of Erectile Function (IIEF) Sexual Desire Domain

Self-reported sexual desire over the past 4 weeks. IIEF sexual desire was the sum of Q11 and Q12. Scores ranged from 1 (low/almost never) to 5 (very high/almost always) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Change was defined as endpoint minus baseline domain score. Change in IIEF sexual desire domain at Week 8 and Week 18 were averaged to produce an overall change in IIEF sexual desire domain score. Higher scores were indicative of increased sexual desire. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil2.55
Sildenafil2.60

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"Percentage of Participants Preferring Tadalafil Over Sildenafil Measured at Week 18 Using Question 1 of the Phosphodiesterase 5 Inhibitor Treatment Preference Questionnaire (PITPQ)"

PITPQ Question (Q) 1 was a dichotomous outcome measure in which the participant selected his preferred study treatment (tadalafil or sildenafil) to receive during the Extension Phase. (NCT01352507)
Timeframe: Week 18

Interventionpercentage of participants (Number)
All Randomized Participants69.1

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Change in PAIRS Time Concerns Domain

PAIRS was a self-administered, 29-item scale that assessed the broader psychological and interpersonal outcomes associated with ED and its treatment. Each question was rated on a Likert scale that ranged from 1 (strongly disagree) to 4 (strongly agree). The time concerns domain score was the average score for Items 1, 2, 6, 7, 8, 20, 24, and 25. Time concern domain scores ranged from 1 (strongly disagree) to 4 (strongly agree). Change was defined as endpoint minus baseline domain score. Change in PAIRS time concerns at Week 8 and Week 18 were averaged to produce an overall change in PAIRS time concerns domain score. Higher scores were indicative of more time concerns. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil-0.28
Sildenafil-0.14

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Change in Psychosocial and Interpersonal Relationship Scale (PAIRS) Sexual Self-Confidence Domain

PAIRS was a self-administered, 29-item scale that assessed the broader psychological and interpersonal outcomes associated with ED and its treatment. Each question was rated on a Likert scale that ranged from 1 (strongly disagree) to 4 (strongly agree). The sexual self-confidence domain score was the average score for Items 5, 10, 15, 23, 27, and 29. Sexual self-confidence domain scores ranged from 1 (strongly disagree) to 4 (strongly agree). Change was defined as endpoint minus baseline domain score. Change in PAIRS sexual self-confidence domain scores at Week 8 and Week 18 were averaged to produce an overall change in PAIRS sexual self-confidence domain score. Higher scores were indicative of greater sexual self-confidence. (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Interventionunits on a scale (Mean)
Tadalafil0.75
Sildenafil0.72

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Change in Sexual Encounter Profile (SEP) Question 2

"Participant-assessed diary that assessed the mean change from baseline in the percentage of yes responses to SEP Q2, Were you able to insert your penis into your partner's vagina?. The SEP Q2 score was determined as the percentage of yes responses to SEP Q2 out of all sexual attempts recorded during the time period. Change was defined as the percentage of yes responses at endpoint minus the percentage of yes responses at baseline. Change in percentage of yes responses to SEP Q2 at Week 8 and Week 18 were averaged to produce an overall change in SEP Q2." (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Intervention"percentage of yes responses" (Mean)
Tadalafil45.28
Sildenafil44.94

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Change in Sexual Encounter Profile (SEP) Question 3

"Participant-assessed diary that assessed the mean change from baseline in the percentage of yes responses to SEP Q3, Did your erection last long enough for you to have successful intercourse?. The SEP Q3 score was determined as the percentage of yes responses to SEP Q3 out of all sexual attempts recorded during the time period. Change was defined as the percentage of yes responses at endpoint minus percentage of yes responses at baseline. Change in the percentage of yes responses to SEP Q3 at Week 8 and Week 18 were averaged to produce an overall change in SEP Q3." (NCT01352507)
Timeframe: Baseline, Week 8, and Week 18

Intervention"percentage of yes responses" (Mean)
Tadalafil64.53
Sildenafil63.72

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Drug Attributes Questionnaire (DRAQ) at Week 18

DRAQ was a questionnaire used to record explanations for why participants preferred a drug. Participants identified their first and second reasons for drug preference from a choice of 7 reasons. Each reason for drug preference includes participants who selected that reason as their first or second reason. (NCT01352507)
Timeframe: Week 18

,
Interventionpercentage of participants (Number)
Time between drug and first erection was shortWas able to get an erection long after having drugHad erections the next morningThe firmness of erectionsWas able to get an erection every timeHad few side effectsPartner preferred this treatment
Sildenafil35.211.111.151.956.525.97.4
Tadalafil10.355.024.036.437.623.610.7

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Percentage of Participants Moderately or Strongly Preferring the Selected Treatment at Week 18 Using Question 2 of the PITPQ

"PITPQ Q2 was a measure of the degree of treatment preference based on the participant's opinion. The question was, For the treatment preference you selected in Q1, what is your degree of preference?. Choices were moderate or strong." (NCT01352507)
Timeframe: Week 18

,
Interventionpercentage of participants (Number)
Strong preferenceModerate preference
Sildenafil34.365.7
Tadalafil38.062.0

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Duration of Response

Median length of response in months. (NCT01374217)
Timeframe: Up to 6 months

Interventionmonths (Median)
Tadalafil2.3

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Response Rate

Percentage of participants who responded to the addition of tadalafil. Response is defined as a complete remission (CR), very good partial remission (VGPR), partial remission (PR), or stable disease (SD) by International Uniform Response criteria. (NCT01374217)
Timeframe: Up to 6 months

InterventionParticipants (Count of Participants)
Tadalafil5

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Time to Progression

Median time to progression of disease in days. (NCT01374217)
Timeframe: Up to 71 days

Interventiondays (Median)
Tadalafil48

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Quality of Life Scores

Median change in symptom scores. Scale is the EORTC QLQ-C30. There are three domains: symptom scale (score range 7-14); past week (score range 21-82); and global health status (score range 2-14). Higher or increasing scores mean worse outcomes; lower or decreasing scores mean better outcomes. (NCT01374217)
Timeframe: 3 months (M3) and 6 months (M6)

Interventionchange in score on a scale (Median)
Symptoms (M3)Past week (M3)Global health status (M3)Symptoms (M6)Past week (M6)Global health status (M6)
Tadalafil05-1.516-1

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Pharmacokinetics: Area Under the Concentration-Time Curve From Time Zero to Infinity [AUC(0-∞)] of LY2452473

(NCT01401543)
Timeframe: Predose up to 96 hours postdose for each of the 4 treatment periods

Interventionnanograms*hours per milliliter (ng*h/mL) (Mean)
5 mg LY2452473 and 5 mg Tadalafil514
LY900010 (Particle Size #1)495
LY900010 (Particle Size #2)453
LY900010 (Particle Size #3)463

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Pharmacokinetics: AUC(0-∞) of Tadalafil

(NCT01401543)
Timeframe: Predose up to 96 hours postdose for each of the 4 treatment periods

Interventionnanograms*hours per milliliter (ng*h/mL) (Mean)
5 mg LY2452473 and 5 mg Tadalafil2410
LY900010 (Particle Size #1)2400
LY900010 (Particle Size #2)2240
LY900010 (Particle Size #3)2290

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Pharmacokinetics: Cmax of Tadalafil

(NCT01401543)
Timeframe: Predose up to 96 hours postdose for each of the 4 treatment periods

Interventionnanograms per milliliter (ng/mL) (Mean)
5 mg LY2452473 and 5 mg Tadalafil102
LY900010 (Particle Size #1)74.4
LY900010 (Particle Size #2)72.4
LY900010 (Particle Size #3)70.0

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Pharmacokinetics: Maximum Plasma Concentration (Cmax) of LY2452473

(NCT01401543)
Timeframe: Predose up to 96 hours postdose for each of the 4 treatment periods

Interventionnanograms per milliliter (ng/mL) (Mean)
5 mg LY2452473 and 5 mg Tadalafil32.5
LY900010 (Particle Size #1)27.1
LY900010 (Particle Size #2)25.6
LY900010 (Particle Size #3)24.7

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Change in Insulin Resistance From Baseline to 3 Months, as Measured by HOMA-IR

The primary endpoint is defined as the treatment group difference in the change in insulin resistance (baseline HOMA-IR minus 3-month HOMA-IR). HOMA-IR = [fasting glucose * fasting insulin]/405 (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionmg*microunits/dL*mL (Mean)
Baseline3 months
Placebo3.845.06
Tadalafil3.573.81

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Baseline to 3 Month Change in Composite of Insulin Resistance and Sensitivity, as Measured by the Oral Disposition Index

The secondary endpoint is defined as the treatment group difference in the change in oral disposition index (baseline minus 3-month). This is thought to reflect a composite of both insulin resistance and secretion. Oral disposition index = insulinogenic index / fasting insulin (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionunitless index (Mean)
Baseline3-month
Placebo2.870.58
Tadalafil1.744.48

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Baseline to 3-month Change in Endothelial Function Measured by EndoPAT

Endothelial function was measured using the reactive hyperemia index, acquired using EndoPAT device. Peripheral arterial tonometry probes were placed on both index fingers. After a 5 min equilibration period, a blood pressure cuff was inflated to 200 mmHg and kept inflated for 5 min. The cuff was then rapidly deflated and the reactive hyperemic response pulse volume recorded, where RHI = ratio of hyperemic finger pulse volume (post-cuff inflation / pre-cuff inflation) to control finger pulse volume (post-cuff inflation / pre-cuff inflation) (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionunitless index (Mean)
Baseline3-month
Placebo2.32.2
Tadalafil2.12.1

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Baseline to 3-month Change in Insulin Sensitivity, as Measured by the Matsuda Index

The secondary endpoint is defined as the treatment group difference in the change in Matsuda Index (baseline minus 3-month). This index is a measure of insulin resistance derived from a frequently sampled oral glucose tolerance test, obtaining glucose and insulin levels in the fasting state, as well as 30, 60, 90, and 120 min after administration of oral glucose load. Matsuda index = 10,000/SQRT [fasting glucose*fasting insulin* (mean glucose from time 30, 60, 90, 120 min) * (mean insulin at time 30, 60, 90, and 120 min)] (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionunitless index (Mean)
Baseline3 months
Placebo3.513.28
Tadalafil3.604.27

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Baseline to 3-month Change in Matsuda Disposition Index

Change in disposition index from baseline to 3 months. This index is a composite measure thought to reflect insulin resistance and secretion. Matsuda disposition index = [Matsuda sensitivity index * insulinogenic index] (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionunitless index (Mean)
Baseline3-month
Placebo6.670.19
Tadalafil2.239.22

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Insulinogenic Index

The secondary endpoint is defined as the treatment group difference in the change in insulinogenic index (baseline minus 3-month). This index is thought to reflect insulin secretion, and is derived from fasting and 30 min-post oral glucose tolerance testing glucose and insulin values. Insulinogenic index = [fasting insulin - insulin at time 30 min] / [fasting glucose - glucose at time 30 min] (NCT01444651)
Timeframe: Baseline and 3 months

,
Interventionunitless index (Mean)
Baseline3-month
Placebo2.171.04
Tadalafil0.392.62

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Change From Baseline in Total Score of International Prostate Symptom Score (IPSS) at 12 Weeks

The IPSS Total Score was the sum of Questions 1 through 7 in the IPSS questionnaire. Each question was based on the participant's urination experiences and prostate symptoms during the last month. Scores ranged from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score that ranged from 0 to 35; higher numerical scores represented a greater severity of symptoms. Least squares (LS) mean was based on the mixed-effect model repeated measures (MMRM) model analysis with participants as random effects, treatment, prior alpha-blocker use (yes/no), country (Japan/Korea), visit, and treatment-by-visit interaction as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates. (NCT01460342)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-4.5
Tadalafil-6.0

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Change From Baseline in the International Prostate Symptom Score (IPSS) Quality of Life (QoL) Index

"The IPSS QoL Index assessed the participant's response to the following question, If you were to spend the rest of your life with your urinary condition just the way it is now, how would you feel about that?. Response options were 0 (Delighted), 1 (Pleased), 2 (Mostly satisfied), 3 (Mixed, about equally satisfied and dissatisfied), 4 (Mostly dissatisfied), 5 (Unhappy), and 6 (Terrible), for a QoL Index Score that ranged from 0 to 6. Least squares (LS) mean was based on the mixed-effect model repeated measures (MMRM) model analysis with participants as random effects, treatment, prior alpha-blocker use (yes/no), country (Japan/Korea), visit, and treatment-by-visit interaction as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates." (NCT01460342)
Timeframe: Baseline, 4 weeks, 8 weeks, 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
Change at Week 4Change at Week 8Change at Week 12
Placebo-0.5-0.7-0.9
Tadalafil-0.6-0.8-1.1

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Change From Baseline in the International Prostate Symptom Score (IPSS) Storage (Irritative) Subscore

The IPSS Storage (Irritative) Subscore was the sum of Questions 2, 4, and 7 in the IPSS questionnaire. Each question was scored from 0 (no irritative symptoms) to 5 (frequent irritative symptoms) for an IPSS Storage (Irritative) Subscore that ranged from 0 to 15; higher numerical scores represented a greater severity of symptoms. Least squares (LS) mean was based on the mixed-effect model repeated measures (MMRM) model analysis with participants as random effects, treatment, prior alpha-blocker use (yes/no), country (Japan/Korea), visit, and treatment-by-visit interaction as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates. (NCT01460342)
Timeframe: Baseline, 4 weeks, 8 weeks, 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
Change at 4 WeeksChange at 8 WeeksChange at 12 Weeks
Placebo-0.9-1.3-1.4
Tadalafil-1.2-1.7-2.0

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Change From Baseline in the International Prostate Symptom Score (IPSS) Voiding (Obstructive) Subscore

The IPSS Voiding (Obstructive) Subscore was the sum of Questions 1, 3, 5, and 6 in the IPSS questionnaire. Each question was scored from 0 (no obstructive symptoms) to 5 (frequent obstructive symptoms) for an IPSS Voiding (Obstructive) Subscore that ranged from 0 to 20; higher numerical scores represented a greater severity of symptoms. Least squares (LS) mean was based on the mixed-effect model repeated measures (MMRM) model analysis with participants as random effects, treatment, prior alpha-blocker use (yes/no), country (Japan/Korea), visit, and treatment-by-visit interaction as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates. (NCT01460342)
Timeframe: Baseline, 4 weeks, 8 weeks, 12 weeks

,
Interventionunits on a scale (Least Squares Mean)
Change at Week 4Change at Week 8Change at Week 12
Placebo-1.8-2.6-3.1
Tadalafil-2.8-3.4-4.0

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Patient Global Impression of Improvement (PGI-I) Scale at 12 Weeks

The PGI-I scale measured the participant's perception of improvement at the time of assessment compared with the start of treatment. Scores were 1 (Very much better), 2 (Much improved), 3 (Minimally improved), 4 (No change), 5 (Minimally worse), 6 (Much worse), and 7 (Very much worse). (NCT01460342)
Timeframe: 12 Weeks

,
Interventionparticipants (Number)
Very Much BetterMuch BetterA Little BetterNo ChangeA Little WorseMuch WorseVery Much WorseMissing
Placebo955138907023
Tadalafil1879148552004

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Change From Baseline in Total Score of International Prostate Symptom Score (IPSS)

The IPSS Total Score was the sum of Questions 1 through 7 in the IPSS questionnaire. Each question was based on the participant's urination experiences and prostate symptoms during the last month. Scores ranged from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score that ranged from 0 to 35; higher numerical scores represented a greater severity of symptoms. Least squares (LS) mean was based on the mixed-effect model repeated measures (MMRM) model analysis with participants as random effects, treatment, prior alpha-blocker use (yes/no), country (Japan/Korea), visit, and treatment-by-visit interaction as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates. (NCT01460342)
Timeframe: Baseline, 4 weeks, 8 weeks

,
Interventionunits on a scale (Least Squares Mean)
Change at Week 4Change at Week 8
Placebo-2.8-4.0
Tadalafil-4.0-5.2

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Clinician Global Impression of Improvement (CGI-I) Scale at 12 Weeks

The CGI-I measured the clinician's perception of participant improvement at the time of assessment compared with the start of treatment. Scores were 1 (Very much better), 2 (Much improved), 3 (Minimally improved), 4 (No change), 5 (Minimally worse), 6 (Much worse), and 7 (Very much worse). (NCT01460342)
Timeframe: 12 Weeks

,
Interventionparticipants (Number)
Very Much ImprovedMuch ImprovedMinimally ImprovedNo ChangeMinimally WorseMuch WorseVery Much WorseMissing
Placebo1074115938013
Tadalafil14103125591004

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Change From Baseline in Modified International Prostate Symptom Score (mIPSS) Score at 2 Weeks

The mIPSS Total Score was the sum of Questions 1 through 7 in the mIPSS questionnaire, which was a modified version of the IPSS questionnaire. Questions about the participant's urination experiences and prostate symptoms in the IPSS questionnaire were modified to obtain responses based on time since the last visit rather than during the last month. Each question was scored from 0 (none/no symptoms) to 5 (frequent symptoms) for an mIPSS Total Score that ranged from 0 to 35; higher numerical scores represented a greater severity of symptoms. Least squares (LS) mean was based on the analysis of covariance (ANCOVA) model with treatment, prior alpha-blocker use (yes/no), and country (Japan/Korea) as fixed effects, and baseline value and placebo lead-in total IPSS change as fixed covariates. (NCT01460342)
Timeframe: Baseline, 2 weeks

Interventionunits on a scale (Least Squares Mean)
Placebo-2.1
Tadalafil-2.7

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Number of Participants With Palatability of the Tadalafil Suspension

"The Taste Assessment Questionnaire (TAQ) questions were:~TAQRES1: Please rate the bitterness level. TAQRES2: Please rate the sweetness level. TAQRES3: Please rate the aftertaste. TAQRES4: Please rate the overall acceptability of the taste for daily use." (NCT01484431)
Timeframe: Day 35 (high dose)

InterventionParticipants (Count of Participants)
TAQRES1: Extremely bitterTAQRES1: Very bitterTAQRES1: Moderately bitterTAQRES1: Slightly bitterTAQRES1: Not bitterTAQRES2: Extremely sweetTAQRES2: Very sweetTAQRES2: Moderately sweetTAQRES2: Slightly sweetTAQRES2: Not sweetTAQRES3: Extreme aftertasteTAQRES3: Strong aftertasteTAQRES3: Moderate aftertasteTAQRES3:Slight aftertasteTAQRES3:No aftertasteTAQRES4: Not acceptableTAQRES4: Slightly acceptableTAQRES4: AcceptableTAQRES4: Very acceptable
Light Weight: <25 kg0000310110010020021

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Population Pharmacokinetics: Area Under the Concentration Curve Versus Time at a Dosing Interval at Steady State (AUCtau) for Tadalafil

"Population Pharmacokinetics: Area Under the Concentration Curve Versus Time at a Dosing Interval at Steady State (AUCtau) for Tadalafil.~The measure of dispersion reported is 90% Prediction Intervals and not Confidence Intervals." (NCT01484431)
Timeframe: Period 1: Pre Dose and 2, 4, 8, 12, and 24 Hours Post Dose on Days 1, 14 and 49; with single dose measures on Day 1 and steady-state measurements on Days 14 and 49

,,
Interventionnanograms* hour per milliliter(ng*hr/mL) (Median)
Not Taking BosentanTaking Concomitant Bosentan
20 mg Light Weight: <25 kg81704550
20 mg Middle Weight: 25 kg to <40 kg83905000
40 mg Heavy Weight: ≥40 kg152008990

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Population Pharmacokinetics: Average Concentration (Cmean,ss) of for Tadalafil at Steady-State.

"Population Pharmacokinetics: Average Concentration (Cmean,ss) of for tadalafil at steady-state.~The measure of dispersion reported is 90% Prediction Intervals and not Confidence Intervals." (NCT01484431)
Timeframe: Period 1: Pre Dose and 2, 4, 8, 12, and 24 Hours Post Dose on Days 1, 14 and 49; with single dose measures on Day 1 and steady-state measurements on Days 14 and 49

,,
Interventionnanograms per milliliter (ng/mL) (Median)
Not Taking BosentanTaking Concomitant Bosentan
20 mg Light Weight <25 kg340190
20 mg Middle Weight: 25 kg to <40 kg350209
40 mg Heavy Weight: ≥40 kg633375

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Percentage of Participants With Clinical Worsening

Clinical worsening was defined as any of the following: death, lung or heart transplantation, atrial septostomy or Potts' shunt, hospitalization for Pulmonary Arterial Hypertension (PAH) progression, new onset syncope, initiation of new PAH therapy (including increase in the dose of existing PAH specific concomitant therapy, such as endothelin receptor agonist or beraprost medication), or increase of 1 or more in World Health Organization(WHO) Functional Class (except for participants already in Class IV; only for participants unable to perform the 6 minute walk (6MW) test; worsening of WHO functional class by 1 or more for participants who can perform a 6 minute walk (6MW) test and who have a decrease of ≥ 20% in the 6 minute walk distance (for those participants who are ≥6 years of age). (NCT01484431)
Timeframe: Baseline Up to 27 Months

Interventionpercentage of participants (Number)
Light Weight <25 kg50.00
Middle Weight: 25 kg to <40 kg28.57
Heavy Weight: ≥40 kg33.33

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Change in Glomerular Filtration Rate (GFR) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

InterventionmL/min/1.73 m^2 (Mean)
Tadalafil Plus Nesiritide-5.3
Tadalafil Plus Placebo3.9

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Change in Natriuresis (Urinary Sodium Excretion) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

InterventionmEq/min (Mean)
Tadalafil Plus Nesiritide41.8
Tadalafil Plus Placebo88.9

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Change in Natriuresis (Urinary Sodium Excretion) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

InterventionmEq/min (Mean)
Tadalafil Plus Nesiritide92.5
Tadalafil Plus Placebo97.0

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Change in Glomerular Filtration Rate (GFR) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

InterventionmL/min/1.73 m^2 (Mean)
Tadalafil Plus Nesiritide-12.7
Tadalafil Plus Placebo9.4

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Change in Urinary Cyclic Guanosine Monophosphate (cGMP) at 60 Minutes for Preclinical Systolic Dysfunction (PSD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

Interventionpmol/min (Mean)
Tadalafil Plus Nesiritide2566.9
Tadalafil Plus Placebo34.2

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Change in Urinary Cyclic Guanosine Monophosphate (cGMP) at 60 Minutes for Preclinical Diastolic Dysfunction (PDD) Reporting Group

Value at 60 minutes minus value at baseline. (NCT01544998)
Timeframe: Baseline, 60 minutes after saline load

Interventionpmol/min (Mean)
Tadalafil Plus Nesiritide1851
Tadalafil Plus Placebo173.4

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Exercised Induced Fatigability as Measured by Fatigue Rating Scale After 4 Weeks of Active Drug

The fatigue rating scale is a scale from 0 to 10 with 0 being no fatigue at all and 10 being the worst fatigue the subject can imagine. The subject is asked to rate their level of fatigue in their leg. This test was performed before and immedicately after the Biodex leg fatigue test. Data is presented as change in scale from pre fatigue test to post fatigue test, with a higher score indicating a greater level of fatigue. (NCT01661595)
Timeframe: after 4 weeks of active drug

Interventionunits on a scale (Mean)
Sildenafil / Placebo4.5
Tadalafil / Placebo3.5
Placebo / Sildenafil5.25
Placebo / Tadalafil6.0

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Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 0.

Fat Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 0

Interventionkilograms (Mean)
Sildenafil, Then Placebo32.35
Tadalfil, Then Placebo37.21
Placebo, Then Sildenafil32.72
Placebo, Then Tadalafil32.10

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Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 4.

Fat Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 4

Interventionkilograms (Mean)
Sildenafil, Then Placebo33.16
Tadalfil, Then Placebo37.12
Placebo, Then Sildenafil32.30
Placebo, Then Tadalafil32.47

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Exercised Induced Fatigability as Measured by Fatigue Rating Scale After 4 Weeks of Placebo

The fatigue rating scale is a scale from 0 to 10 with 0 being no fatigue at all and 10 being the worst fatigue the subject can imagine. The subject is asked to rate their level of fatigue in their leg. This test was performed before and immedicately after the Biodex leg fatigue test after 4 weeks of placebo. Data is presented as change in scale from pre fatigue test to post fatigue test, with a higher score indicating a greater level of fatigue. (NCT01661595)
Timeframe: after 4 weeks of placebo

Interventionunits on a scale (Mean)
Sildenafil / Placebo4.33
Tadalafil / Placebo2.5
Placebo / Sildenafil7.0
Placebo / Tadalafil4.75

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Hemoglobin Level at Week 0

Hemoglobin was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 11.6 - 15.0 g/dL. (NCT01661595)
Timeframe: week 0

Interventiong/dL (Mean)
Sildenafil, Then Placebo13.42
Tadalfil, Then Placebo12.78
Placebo, Then Sildenafil12.4
Placebo, Then Tadalafil13.05

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Hematocrit Level Was Measured at 4 Weeks

Hematocrit was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 35.7 - 45.2%. (NCT01661595)
Timeframe: 4 weeks

Interventionpercent of red blood cells (Mean)
Sildenafil, Then Placebo39.08
Tadalfil, Then Placebo37.38
Placebo, Then Sildenafil38.13
Placebo, Then Tadalafil39.1

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Hematocrit Level Measured at Week 0

Hematocrit was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 35.7 - 45.2%. (NCT01661595)
Timeframe: week 0

Interventionpercent of red blood cells (Mean)
Sildenafil, Then Placebo39.53
Tadalfil, Then Placebo38.55
Placebo, Then Sildenafil37.25
Placebo, Then Tadalafil31.88

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Fat Mass as Measured by Dual Energy X-ray Absorptiometry at Week 8.

Fat Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 8

Interventionkilograms (Mean)
Sildenafil, Then Placebo33.60
Tadalfil, Then Placebo37.02
Placebo, Then Sildenafil32.40
Placebo, Then Tadalafil32.79

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Hematocrit Level Measured at Week 8

Hematocrit was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 35.7 - 45.2%. (NCT01661595)
Timeframe: week 8

Interventionpercent of red blood cells (Mean)
Sildenafil, Then Placebo40.38
Tadalfil, Then Placebo36.6
Placebo, Then Sildenafil38.1
Placebo, Then Tadalafil38.4

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Walking Distance at 100% Effort as Measured by Walking Test After 4 Weeks of Placebo

Walking performance will be assessed during 2 minutes of walking in long corridor hallways. Subjects will be asked to walk at 100% effort (as quickly as they can safely walk without running) for 2 minutes. Distance traveled for the 2 minutes will be recorded. The walking test will be completed at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of placebo

Interventionmeters (Mean)
Sildenafil, Then Placebo203.82
Tadalfil, Then Placebo189.79
Placebo, Then Sildenafil198.41
Placebo, Then Tadalafil202.80

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Walking Distance at 100% Effort as Measured by Walking Test After 4 Weeks of Active Drug

Walking performance will be assessed during 2 minutes of walking in long corridor hallways. Subjects will be asked to walk at 100% effort (as quickly as they can safely walk without running) for 2 minutes. Distance traveled for the 2 minutes will be recorded. The walking test will be completed at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of active drug

Interventionmeter (Mean)
Sildenafil, Then Placebo197.01
Tadalfil, Then Placebo178.56
Placebo, Then Sildenafil200.19
Placebo, Then Tadalafil203.46

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Skeletal Muscle Fatigue as Measured by Biodex 4 Pro After 4 Weeks of Placebo

Isokinetic Fatigue Measure (knee extension) is measured on a Biodex System Pro 4 within a 75 degree range of motion. Subjects performed concentric contractions at a fixed speed of 120 degree/sec. 50 contractions were performed at 100% force, one contraction every second. Isokinetic fatigue will be measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. Data is presented as mean maximum force over all 50 kicks. (NCT01661595)
Timeframe: after 4 weeks of placebo

InterventionNewton-Meters (Mean)
Sildenafil, Then Placebo59.69
Tadalafil, Then Placebo42.07
Placebo, Then Sildenafil67.17
Placebo, Then Tadalafil63.24

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Skeletal Muscle Fatigue as Measured by Biodex 4 Pro After 4 Weeks of Active Drug

Isokinetic Fatigue Measure (knee extension) is measured on a Biodex System Pro 4 within a 75 degree range of motion. Subjects performed concentric contractions at a fixed speed of 120 degree/sec. 50 contractions were performed at 100% force, one contraction every second. Isokinetic fatigue will be measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. Data is presented as mean maximum force over all 50 kicks. (NCT01661595)
Timeframe: after 4 weeks of active drug

InterventionNewton-Meters (Mean)
Sildenafil / Placebo60.90
Tadalafil / Placebo42.48
Placebo / Sildenafil62.68
Placebo / Tadalafil63.25

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Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 8

Fatigue symptoms will be measured using the 30-item Multidimensional Fatigue Symptom Inventory - Short Form, a validated measure that yields one overall score of total fatigue calculated using five sub scales (general, physical, emotional, mental, vigor). With the exception of the vigor sub scale, higher scores indicate greater fatigue. Total fatigue score is calculated by summing the sub categories (general, physical, emotional and mental) and subtracting vigor. Total scores range from -24 to 96, with a higher score indicating more fatigue. (NCT01661595)
Timeframe: week 8

Interventionscores on a scale (Mean)
Sildenafil, Then Placebo9.67
Tadalfil, Then Placebo3.25
Placebo, Then Sildenafil-9.67
Placebo, Then Tadalafil-9.25

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Hemoglobin Level Measured at Week 4

Hemoglobin was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 11.6 - 15.0 g/dL. (NCT01661595)
Timeframe: week 4

Interventiong/dL (Mean)
Sildenafil, Then Placebo13.05
Tadalfil, Then Placebo12.03
Placebo, Then Sildenafil12.6
Placebo, Then Tadalafil13.2

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Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 0

Fatigue symptoms will be measured using the 30-item Multidimensional Fatigue Symptom Inventory - Short Form, a validated measure that yields one overall score of total fatigue calculated using five sub scales (general, physical, emotional, mental, vigor). With the exception of the vigor sub scale, higher scores indicate greater fatigue. Total fatigue score is calculated by summing the sub categories (general, physical, emotional and mental) and subtracting vigor. Total scores range from -24 to 96, with a higher score indicating more fatigue. (NCT01661595)
Timeframe: Week 0

Interventionscores on a scale (Mean)
Sildenafil, Then Placebo9.66
Tadalfil, Then Placebo-7.5
Placebo, Then Sildenafil-8
Placebo, Then Tadalafil-3.75

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Maximum Peak Isometric Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Placebo

Peak isometric strength is measured on a Biodex System 4 Pro. This test is isolated to the quadricep muscle of one leg. Isometric test is performed at 90 degrees with 5 seconds of force production for each contraction and 15 seconds of rest. 1 set of 3 contractions at 100% force performed. Isometric strength was measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of placebo

InterventionNewton-Meters (Mean)
Sildenafil, Then Placebo145.86
Tadalfil, Then Placebo104.17
Placebo, Then Sildenafil149.14
Placebo, Then Tadalafil148.34

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Maximum Peak Isometric Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Active Drug.

Peak isometric strength is measured on a Biodex System 4 Pro. This test is isolated to the quadricep muscle of one leg. Isometric test is performed at 90 degrees with 5 seconds of force production for each contraction and 15 seconds of rest. 1 set of 3 contractions at 100% force performed. Isometric strength was measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of active drug

InterventionNewton-Meters (Mean)
Sildenafil, Then Placebo140.09
Tadalfil, Then Placebo110.39
Placebo, Then Sildenafil133.81
Placebo, Then Tadalafil139.96

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Maximum Peak Isokinetic Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Placebo.

Isokinetic strength (knee extension) is measured on a Biodex System Pro 4 within a 75 degree range of motion. Subjects performed concentric contractions at a fixed speed of 120 degree/sec. 1 set of 3 contractions were performed at 100% force. Isokinetic strength will be measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of placebo

InterventionNewton-Meters (Mean)
Sildenafil, Then Placebo105.15
Tadalfil, Then Placebo78.59
Placebo, Then Sildenafil117.71
Placebo, Then Tadalafil111.67

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Perceptual Fatigue as Measured by Multidimensional Fatigue Symptom Inventory - Short Form Total Score at Week 4

Fatigue symptoms will be measured using the 30-item Multidimensional Fatigue Symptom Inventory - Short Form, a validated measure that yields one overall score of total fatigue calculated using five sub scales (general, physical, emotional, mental, vigor). With the exception of the vigor sub scale, higher scores indicate greater fatigue. Total fatigue score is calculated by summing the sub categories (general, physical, emotional and mental) and subtracting vigor. Total scores range from -24 to 96, with a higher score indicating more fatigue. (NCT01661595)
Timeframe: week 4

Interventionscores on a scale (Mean)
Sildenafil, Then Placebo6.33
Tadalfil, Then Placebo-3.33
Placebo, Then Sildenafil-6.33
Placebo, Then Tadalafil-3.5

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Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 8.

Lean Body Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 8

Interventionkilograms (Mean)
Sildenafil, Then Placebo46.22
Tadalfil, Then Placebo40.76
Placebo, Then Sildenafil52.09
Placebo, Then Tadalafil55.10

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Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 4.

Lean Body Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 4

Interventionkilograms (Mean)
Sildenafil, Then Placebo46.29
Tadalfil, Then Placebo41.02
Placebo, Then Sildenafil50.61
Placebo, Then Tadalafil54.85

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Lean Body Mass as Measured by Dual Energy X-ray Absorptiometry at Week 0.

Lean Body Mass is calculated from a whole body scan measured on a dual energy x-ray absorptiometry. (NCT01661595)
Timeframe: week 0

Interventionkilograms (Mean)
Sildenafil, Then Placebo44.60
Tadalfil, Then Placebo41.43
Placebo, Then Sildenafil49.93
Placebo, Then Tadalafil54.45

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Hemoglobin Level Measured at Week 8

Hemoglobin was measured by University of Texas Medical Branch Clinical Laboratory. Normal ranges are 11.6 - 15.0 g/dL. (NCT01661595)
Timeframe: week 8

Interventiong/dL (Mean)
Sildenafil, Then Placebo13.55
Tadalfil, Then Placebo11.97
Placebo, Then Sildenafil12.5
Placebo, Then Tadalafil12.95

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Maximum Peak Isokinetic Leg Strength as Measured by Biodex Pro4 After 4 Weeks of Active Drug

Isokinetic strength (knee extension) is measured on a Biodex System Pro 4 within a 75 degree range of motion. Subjects performed concentric contractions at a fixed speed of 120 degree/sec. 1 set of 3 contractions were performed at 100% force. Isokinetic strength will be measured at week 4 and week 8. Depending on grouping, the week 4 and week 8 measures may be placebo or active drug. Data will be reported as after 4 weeks of placebo or after 4 weeks of active drug. (NCT01661595)
Timeframe: after 4 weeks of active drug

InterventionNewton-Meters (Mean)
Sildenafil, Then Placebo106.79
Tadalfil, Then Placebo79.33
Placebo, Then Sildenafil116.48
Placebo, Then Tadalafil114.75

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Period 1: Change From Baseline to Week 24 in a 6 Minute Walk (MW) Distance in Meters

6MWD in meters assessed in a subset of participants who are ≥6 to <18 years of age who are developmentally capable of performing a 6MW test. Change from baseline was derived using mixed model repeated measures (MMRM) with terms for treatment group, visit, baseline 6MWD, and treatment-by-visit interaction. (NCT01824290)
Timeframe: Baseline, Week 24

InterventionMeters (Least Squares Mean)
Placebo36.60
Tadalafil60.48

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Period 1: Percentage of Participants Who Experience CW

Clinical worsening was defined as any of the following: death,lung or heart transplantation,atrial septostomy or Potts' shunt,hospitalization for Pulmonary Arterial Hypertension(PAH) progression,new onset syncope, initiation of new PAH therapy(including increase in the dose of existing PAH specific concomitant therapy,such as endothelin receptor agonist or beraprost medication),or increase of 1 or more in World Health Organization(WHO) Functional Class(except for participants already in Class IV; only for participants unable to perform the 6 minute walk(6MW) test;worsening of WHO functional class by 1 or more for participants who can perform a 6 minute walk(6MW) test and who have a decrease of ≥ 20% in the 6 minute walk distance(for those participants who are ≥6 years of age).Criteria for CW(from Period 1) were adjudicated by an independent,blinded study-specific Clinical Endpoint Committee(CEC).This adjudication was used for data analysis, and was not used to guide subject treatment. (NCT01824290)
Timeframe: Baseline through Week 24

Interventionpercentage of participants (Number)
Placebo0
Tadalafil0

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Period 1: Time to Adjudicated Clinical Worsening (CW)

Clinical worsening was defined as any of the following: death,lung or heart transplantation,atrial septostomy or Potts' shunt,hospitalization for Pulmonary Arterial Hypertension(PAH) progression,new onset syncope,initiation of new PAH therapy(including increase in the dose of existing PAH specific concomitant therapy,such as endothelin receptor agonist or beraprost medication), or increase of 1 or more in World Health Organization(WHO) Functional Class(except for participants already in Class IV;only for participants unable to perform the 6 minute walk(6MW) test;worsening of WHO functional class by 1 or more for participants who can perform a 6 minute walk(6MW) test and who have a decrease of ≥ 20% in the 6 minute walk distance(for those participants who are ≥6 years of age). Criteria for CW(from Period 1) were adjudicated by an independent,blinded study-specific Clinical Endpoint Committee(CEC).This adjudication was used for data analysis, and was not used to guide subject treatment. (NCT01824290)
Timeframe: Baseline through Week 24

InterventionWeeks (Median)
PlaceboNA
TadalafilNA

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Period 2: Percentage of Participants Who Experience CW

Clinical worsening was defined as any of the following: death, lung or heart transplantation, atrial septostomy or Potts' shunt, hospitalization for Pulmonary Arterial Hypertension (PAH) progression, new onset syncope, initiation of new PAH therapy (including increase in the dose of existing PAH specific concomitant therapy, such as endothelin receptor agonist or beraprost medication), or increase of 1 or more in World Health Organization(WHO) Functional Class (except for participants already in Class IV; only for participants unable to perform the 6 minute walk (6MW) test; worsening of WHO functional class by 1 or more for participants who can perform a 6 minute walk (6MW) test and who have a decrease of ≥ 20% in the 6 minute walk distance (for those participants who are ≥6 years of age). (NCT01824290)
Timeframe: Period 2 Baseline through Study Completion (Up to 24 Months)

Interventionpercentage of participants (Number)
Placebo/Tadalafil - Open-Label Treatment12.5
Tadalafil/Tadalafil - Open-Label Treatment18.8

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Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at Steady-state

Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at steady-state (NCT01824290)
Timeframe: Week 2, Week 4, Week 16 and Week 24

InterventionLiter Per Hour (L/hr) (Geometric Mean)
With concomitant bosentan
40 mg Tadalafil4.49

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Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at Steady-state

Period 1: Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil at steady-state (NCT01824290)
Timeframe: Week 2, Week 4, Week 16 and Week 24

InterventionLiter Per Hour (L/hr) (Geometric Mean)
With concomitant bosentanNo bosentan (ERA: Macitentan)
20 mg Tadalafil3.63NA

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Period 2: Time to First Occurrence of CW

Clinical worsening was defined as any of the following: death, lung or heart transplantation, atrial septostomy or Potts' shunt, hospitalization for Pulmonary Arterial Hypertension (PAH) progression, new onset syncope, initiation of new PAH therapy (including increase in the dose of existing PAH specific concomitant therapy, such as endothelin receptor agonist or beraprost medication), or increase of 1 or more in World Health Organization(WHO) Functional Class (except for participants already in Class IV; only for participants unable to perform the 6 minute walk (6MW) test; worsening of WHO functional class by 1 or more for participants who can perform a 6 minute walk (6MW) test and who have a decrease of ≥ 20% in the 6 minute walk distance (for those participants who are ≥6 years of age). (NCT01824290)
Timeframe: Period 2 Baseline through Study Completion (Up to 24 Months)

InterventionMonths (Median)
Placebo/Tadalafil - Open-Label TreatmentNA
Tadalafil/Tadalafil - Open-Label TreatmentNA

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Pulmonary Vascular Resistance

Pulmonary vascular resistance assessed on right heart catheterization is a hemodynamic measurement of pulmonary vascular remodeling. (NCT01862536)
Timeframe: 6 months

InterventionmmHg (Median)
Placebo4.26
Tadalafil2.69

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Change in 6 Minute Walk Test

Change from baseline in distance walked in 6 minutes. (NCT01862536)
Timeframe: The change in distance walked when assessed at 3 months following trial initiation as compared to baseline, similarly at 6 months compared to baseline, at 9 months compared to baseline and at 12 months compared to baseline.

,
InterventionMeters walked in 6 minutes (Median)
Change in 6 MWT from baseline to 3 monthsChange in 6 MWT from baseline to 6 monthsChange in 6 MWT from baseline to 9 monthsChange in 6 MWT from baseline to 12 months
Placebo7.0016.00-18.0021.00
Tadalafil16.604.908.9316.76

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Tricuspid Annular Plane Excursion (TAPSE)

The tricuspid annular plane excursion is an echocardiographic measurement of right ventricular systolic dysfunction. (NCT01862536)
Timeframe: 12 months

Interventionmm (Median)
Placebo2.08
Tadalafil2.12

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Maximum VO2

Measure of aerobic fitness on exercise assessed by cardiopulmonary exercise test. (NCT01862536)
Timeframe: 12 months

InterventionmL/kg/min (Median)
Tadalafil13.6

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Mean Pulmonary Artery Pressure

Mean pulmonary artery pressure assessed by right heart catheterization is a hemodynamic measurement of pulmonary hypertension severity. (NCT01862536)
Timeframe: 6 months

InterventionWood units (Median)
Placebo33.00
Tadalafil29.00

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N-type Brain Natriuretic Peptide (BNP) Concentration

Plasma BNP concentration is a biochemical marker that correlates positively with pulmonary hypertension severity. (NCT01862536)
Timeframe: 12 months

Interventionpg/mL (Median)
Placebo37.50
Tadalafil47.81

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Change From Baseline in Six Minute Walk Distance (6MWD) in Meters

"6MWD measured the distance in meters a participant was able to walk in 6 minutes. The study used 6MWD procedure modified specifically for use in boys with Duchenne muscular dystrophy (DMD), including standardized verbal encouragement at specific intervals to maintain attention to the test, and use of a safety chaser to walk behind the participant during testing (McDonald et al., 2010a). The LS mean (LSM) change from baseline, standard error was derived using mixed model repeated measures (MMRM) methodology with factors for pooled country, treatment, visit, treatment-by-visit interaction and baseline 6MWD as a covariate." (NCT01865084)
Timeframe: Baseline, Week 48

InterventionMeters (Least Squares Mean)
Placebo-50.99
0.3 mg/kg Tadalafil-64.71
0.6 mg/kg Tadalafil-59.08

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Change From Baseline in the North Star Ambulatory Assessment (NSAA) Global Score

The NSAA is a functional scale specifically designed for ambulant boys with DMD that can provide additional information on motor functions important in maintaining normal ambulation and other activities important to everyday life. The NSAA is a 17-item evaluation of standing, ability to transition from lying to sitting, sitting to standing, and other mobility assessments. Each of the 17 items is evaluated on an ordinal scale of 0, 1, or 2, with higher scores reflecting better performance on the assessment, for a total maximum score of 34. This score was transformed to a 0 to 100 scale for the key analysis (referred to as linearized), with higher transformed scores reflecting better performance.The LS mean (LSM) change from baseline standard error was derived using mixed model repeated measures methodology (MMRM) with factors for pooled country, treatment, visit, treatment-by-visit interaction and Day 1 value as baseline covariate. (NCT01865084)
Timeframe: Baseline, Week 48

InterventionUnits on a scale (Least Squares Mean)
Placebo-8.80
0.3 mg/kg Tadalafil-9.31
0.6 mg/kg Tadalafil-8.96

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Pharmacokinetics (PK): Apparent Clearance (CL/F) of Tadalafil

The data reported are population estimate and inter-patient variability. (NCT01865084)
Timeframe: Weeks 4, 12, 24 and 36: -1 Hour up to 24 Hours Postdose

InterventionLiter per hour (L/hr) (Geometric Mean)
0.3 mg/kg Tadalafil and 0.6 mg/kg Tadalafil1.79

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Time to Persistent 10% Worsening in 6MWD

Time on study until the 6MWD becomes 10% less than the baseline 6MWD and continues at that level or lower until the end of study. (NCT01865084)
Timeframe: Baseline through Week 48

InterventionDays (Median)
PlaceboNA
0.3 mg/kg TadalafilNA
0.6 mg/kg TadalafilNA

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Change From Baseline in Pediatric Outcomes Data Collection Instrument (PODCI) Scores

"PODCI includes a Global Functioning Scale and 5 core scales:Upper Extremity and Physical Function,Transfer/Basic Mobility, Sports/Physical Functioning, Pain/Comfort,and Happiness.The Global Functioning Scale is the mean of the mean scores from 4 of the 5 core scales (all except the happiness core scale).The following PODCI scores were prespecified in the protocol for analysis: Global Functioning, Upper Extremity and Physical Function,Transfer/Basic Mobility, and Sports/Physical Functioning. The Global Functioning Scale and each of the core scales were standardized so that a score of 0 represents a poor outcome/worse health, while 100 is the best possible outcome/best health (i.e., complete range of each score is 0 to 100, with higher scores representing better functioning). The LS mean (LSM) change from baseline,standard error was derived using MMRM with factors for pooled country, treatment, visit, treatment-by-visit interaction and baseline PODC scale as covariate." (NCT01865084)
Timeframe: Baseline, Week 48

,,
InterventionUnits on a scale (Least Squares Mean)
Global Functioning Scale (n=41,34,34)Upper Extremity & Physical FunctionTransfer/Basic Mobility Core ScaleSports/Physical Functioning Core Scale
0.3 mg/kg Tadalafil-7.36-3.73-12.50-11.98
0.6 mg/kg Tadalafil-7.34-2.47-12.78-7.88
Placebo-8.81-5.47-14.26-12.47

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Change From Baseline in Timed Function Tests in Seconds

Timed function tests included time it took to rise from floor, walk 10 meters, ascend 4 stairs, and descend 4 stairs.The lower the time in seconds taken, the better the performance. The LS mean change from baseline, standard error, was derived using mixed model repeated measures methodology (MMRM) with factors for pooled country, treatment, visit, treatment-by-visit interaction and Day 1 value as baseline covariate. (NCT01865084)
Timeframe: Baseline, Week 48

,,
InterventionSeconds (Least Squares Mean)
Rise from the Floor(n=92,75,89)10 Meter Walk/Run(n=105,90,100)Stair Climb (n=116,96,110)Stair Descend(n=115,95,110)
0.3 mg/kg Tadalafil3.600.954.102.07
0.6 mg/kg Tadalafil4.811.125.823.27
Placebo4.161.113.963.19

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Time to Persistent 10% Worsening in Timed Function Tests (TFT)

"Time on study until the TFT becomes 10% worse than the baseline TFT and continues at that level or lower until the end of study. The time to persistent 10% worsening is the observed time after baseline until the first observed timepoint where their time used for the TFTs is >110% of the baseline time and all the time values observed afterward are also >110% of baseline. If the participant discontinues prior to experiencing persistent worsening, this outcome for the participant is censored at the date of discontinuation of the double-blind period.~Only participants with complete evaluable data were analyzed. Complete evaluable data was defined as having baseline measurement, complete dates at evaluable visits and a post-baseline measurement at each evaluable visit." (NCT01865084)
Timeframe: Baseline through Week 48

,,
InterventionDays (Median)
Rise from the Floor (n=81,67,77)Stair Climb (n=112,91,107)10 Meter Walk/Run (n=98,83,91)Stair Descend (n=110,91,108)
0.3 mg/kg TadalafilNA259.0NANA
0.6 mg/kg TadalafilNA253.0NANA
Placebo253.0255.0NANA

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Change From Baseline in Yes Responses to Question 2 of the Sexual Encounter Profile (SEP) Questionnaire at Week 12

"Participant-assessed diary assesses the mean change from baseline in the percentage of yes responses to SEP Q2, Were you able to insert your penis into your partner's vagina?. The SEP Q2 score was determined as the percentage of yes responses to SEP Q2 out of all sexual attempts recorded during the time period. Change is defined as the percentage of yes responses at endpoint minus the percentage of yes responses at baseline. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment, country/region, baseline ED severity (mild/moderate/severe), centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), the centered baseline-by-treatment and the treatment-by-country/region interactions. The interaction terms are removed if p >= 0.10." (NCT01937871)
Timeframe: Baseline, Week 12

Intervention"percentage of yes responses" (Least Squares Mean)
Placebo10.90
5 mg Tadalafil23.87
0.2 mg Tamsulosin6.84

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Change From Baseline in IIEF Intercourse Satisfaction at Week 12

IIEF is a 15 item self-reported questionnaire used to assess overall erectile function and satisfaction during the past 4 weeks. IIEF-IS is the sum of Questions 6,7 and 8 of the IIEF. Scores range from 0(low/no satisfaction) to 5(high satisfaction) for each question, with the total possible score for the 3 questions ranging from 0 to 15.Higher scores were indicative of an increase in intercourse satisfaction. Least squares (LS) mean of change from baseline to endpoint is from MMRM. The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction,centered baseline value(defined as the baseline value for a participant- the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-0.05
5 mg Tadalafil1.08
0.2 mg Tamsulosin0.41

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Number of Participants With Clinician Global Impression of Improvement (CGI-I) at Week 12

CGI-I measures clinician's perception of participant improvement at the time of assessment (compared with the start of treatment) with scores ranging from 1 (very much better) to 7 (very much worse). (NCT01937871)
Timeframe: Week 12

,,
InterventionParticipants (Count of Participants)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
0.2 mg Tamsulosin00139854110
5 mg Tadalafil1056614012021
Placebo0212911309216

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Change From Baseline in Yes Responses to Question 3 of the SEP Questionnaire at Week 4 and Week 8

"Participant-assessed diary assesses the mean change from baseline in the percentage of yes responses to SEP Q3, Did your erection last long enough for you to have successful intercourse?. The SEP Q3 score is determined as the percentage of yes responses to SEP Q3 out of all sexual attempts recorded during the time period. Change was defined as the percentage of yes responses at endpoint minus percentage of yes responses at baseline. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment, country/region, baseline ED severity (mild/moderate/severe), centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), the centered baseline-by-treatment and the treatment-by-country/region interactions. The interaction terms are removed if p >= 0.10." (NCT01937871)
Timeframe: Baseline, Week 4; Baseline, Week 8

,,
Intervention"percentage of yes responses" (Least Squares Mean)
Week 4Week 8
0.2 mg Tamsulosin9.5714.98
5 mg Tadalafil23.3832.27
Placebo7.4114.08

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Change From Baseline in Yes Responses to Question 2 of the SEP Questionnaire at Week 4 and Week 8

"Participant-assessed diary assesses the mean change from baseline in the percentage of yes responses to SEP Q2, Were you able to insert your penis into your partner's vagina?. The SEP Q2 score is determined as the percentage of yes responses to SEP Q2 out of all sexual attempts recorded during the time period. Change was defined as the percentage of yes responses at endpoint minus the percentage of yes responses at baseline. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment, country/region, baseline ED severity (mild/moderate/severe), centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), the centered baseline-by-treatment and the treatment-by-country/region interactions. The interaction terms are removed if p >= 0.10." (NCT01937871)
Timeframe: Baseline, Week 4; Baseline, Week 8

,,
Intervention"percentage of yes responses" (Least Squares Mean)
Week 4Week 8
0.2 mg Tamsulosin6.217.42
5 mg Tadalafil20.5323.22
Placebo5.4310.79

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Change From Baseline in IIEF EF at Week 4 and Week 8

IIEF is a 15 item self-reported questionnaire used to assess overall erectile function and satisfaction during the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 were scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 was scored 1 (very low confidence) to 5 (very high confidence) with a total score ranging from 1 to 30. Higher scores represent better erectile function. LS mean of change from baseline to endpoint is from MMRM. The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 4; Baseline, Week 8

,,
Interventionunits on a scale (Least Squares Mean)
Week 4Week 8
0.2 mg Tamsulosin1.432.19
5 mg Tadalafil4.504.77
Placebo1.231.51

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Change From Baseline in Yes Responses to Question 3 of the SEP Questionnaire at Week 12

"Participant-assessed diary assesses the mean change from baseline in the percentage of yes responses to SEP Q3, Did your erection last long enough for you to have successful intercourse?.The SEP Q3 score is determined as the percentage of yes responses to SEP Q3 out of all sexual attempts recorded during the time period. Change was defined as the percentage of yes responses at endpoint minus percentage of yes responses at baseline. Least squares (LS) mean of change from baseline to endpoint is from an analysis of covariance (ANCOVA). The model includes terms for treatment, country/region, baseline ED severity (mild/moderate/severe), centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), the centered baseline-by-treatment and the treatment-by-country/region interactions. The interaction terms are removed if p >= 0.10." (NCT01937871)
Timeframe: Baseline, Week 12

Intervention"percentage of yes responses" (Least Squares Mean)
Placebo15.96
5 mg Tadalafil36.62
0.2 mg Tamsulosin17.42

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Change From Baseline in Total IPSS at Week 4 and Week 8

IPSS Total Score is the sum of Questions 1 through 7 of the IPSS questionnaire. Each question is scored from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score ranging from 0 to 35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM). The model includes effects for treatment, country/region, prior alpha-blocker therapy, baseline ED severity (mild/moderate/severe),visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 4; Baseline, Week 8

,,
Interventionunits on a scale (Least Squares Mean)
Week 4Week 8
0.2 mg Tamsulosin-3.92-4.44
5 mg Tadalafil-4.10-4.85
Placebo-2.99-3.50

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Change From Baseline in IIEF Subscores at Week 12

IIEF Question 3 asks how often a participant was able to penetrate his partner over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). IIEF Question 4 asks whether/how often a participant was able to maintain an erection after penetration over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). Least squares (LS) mean of change from baseline to endpoint is from MMRM. The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

,,
Interventionunits on a scale (Least Squares Mean)
IIEF Question 3IIEF Question 4
0.2 mg Tamsulosin0.390.50
5 mg Tadalafil0.870.87
Placebo0.280.30

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Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12

IPSS Total Score is the sum of Questions 1 through 7 of the IPSS questionnaire. Each question was scored from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score ranging from 0 to 35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM).The model includes effects for treatment, country/region, prior alpha-blocker therapy, baseline Erectile dysfunction (ED) severity (mild/moderate/severe),visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment.The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-4.08
5 mg Tadalafil-5.49
0.2 mg Tamsulosin-4.92

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Change From Baseline in Postvoid Residual Volume (PVR) at Week 12

The amount of urine remaining in the bladder after void completion. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionmilliliters (mL) (Mean)
Placebo-6.3
5 mg Tadalafil-3.8
0.2 mg Tamsulosin-9.5

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Change From Baseline in Modified International Prostate Symptom Score (mIPSS) at Week 2

The modified IPSS is the total IPSS collected at 2 weeks post-baseline.The total IPSS is obtained by combining the scores of the responses to component questions 1 through 7. Each question is scored from 0-5 for a total IPSS range of 0-35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from ANCOVA. The model includes terms for treatment, country/region, prior alpha-blocker use and baseline ED severity (mild/moderate/severe), centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), the centered baseline-by-treatment and the treatment-by-country/region interactions. The interaction terms are removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 2

Interventionunits on a scale (Least Squares Mean)
Placebo-2.19
5 mg Tadalafil-3.40
0.2 mg Tamsulosin-3.20

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Change From Baseline in IPSS Voiding (Obstructive) Subscore at Week 12

IPSS voiding (obstructive) subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores ranged from 0 (no obstructive symptoms) to 5 (frequent obstructive symptoms), with total subscore of the 4 questions of the obstructive score ranging from 0 to 20; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM). The model includes effects for treatment, country/region, prior alpha-blocker therapy, baseline ED severity (mild/moderate/severe),visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-2.42
5 mg Tadalafil-3.49
0.2 mg Tamsulosin-3.07

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Change From Baseline in IPSS Storage (Irritative) Subscore at Week 12

IPSS Storage (Irritative) subscore is the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores ranged from 0 (no irritative symptoms) to 5 (frequent irritative symptoms), with total subscore of the 3 questions for irritative subscore ranging from 0 to 15; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM). The model includes effects for treatment, country/region, prior alpha-blocker therapy, baseline ED severity (mild/moderate/severe), visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-1.68
5 mg Tadalafil-2.01
0.2 mg Tamsulosin-1.90

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Change From Baseline in Uroflowmetry Measures at Week 12

"Qmax is defined as the peak urine flow rate (measured in milliliters per second [mL/sec] using standard calibrated flowmeter).~At each visit, a uroflowmetry assessment was considered valid and the data were included only if the prevoid total bladder volume (assessed by ultrasound) was >=150 to <=550 milliliters (mL) and the voided volume (Vcomp) was >=125 mL. Changes in Qmax from baseline to endpoint in the double-blind treatment period were analyzed using Type III sums of squares ANOVA on rank-transformed data with a term for treatment group." (NCT01937871)
Timeframe: Baseline, Week 12

InterventionMilliliters/seconds (mL/sec) (Mean)
Placebo1.5
5 mg Tadalafil1.9
0.2 mg Tamsulosin2.0

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Change From Baseline in IPSS Quality of Life (QoL) Index at Week 12

"IPSS QoL assess participant response to the following question:If you were to spend the rest of your life with your urinary condition just the way it is now, how would you feel about that?. Response options are Delighted(0),Pleased(1);Mostly satisfied(2);mixed about equally satisfied and dissatisfied(3);Mostly dissatisfied(4);Unhappy(5);Terrible(6),with a total ranging from 0 to 6; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares(LS) mean of change from baseline(bl) to endpoint is from MMRM.The model includes effects for treatment,country/region, prior alpha-blocker therapy,baseline ED severity (mild/moderate/severe),visit, treatment-by-visit interaction, centered bl value (defined as the bl value for a participant -the overall bl mean value),placebo lead-in total IPSS change(change from Visit 2 at Visit 3),centered bl-by-treatment and treatment-by-country/region interactions." (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-0.85
5 mg Tadalafil-0.98
0.2 mg Tamsulosin-1.00

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Change From Baseline in IIEF Sexual Desire at Week 12

IIEF is a 15 item self-reported questionnaire used to assess overall erectile function and satisfaction during the past 4 weeks. IIEF sexual desire is the sum of Q11 and Q12. Scores ranged from 1 (low/almost never) to 5 (very high/almost always) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Higher scores were indicative of increased sexual desire. Least squares (LS) mean of change from baseline to endpoint is from MMRM. The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo0.46
5 mg Tadalafil1.12
0.2 mg Tamsulosin0.28

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Number of Participants With Patient Global Impression of Improvement (PGI-I) at Week 12

PGI-I measures a participant's perception of improvement at the time of assessment compared with the start of treatment. Score ranges from 1 (very much better) to 7 (very much worse). (NCT01937871)
Timeframe: Week 12

,,
InterventionParticipants (Count of Participants)
Very Much WorseMuch WorseA Little WorseNo ChangeA Little BetterMuch BetterVery Much Better
0.2 mg Tamsulosin0013793396
5 mg Tadalafil0225316411913
Placebo03587169735

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Change From Baseline in IPSS at Week 12

IPSS Total Score is the sum of Questions 1 through 7 of the IPSS questionnaire. Each question is scored from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score ranging from 0 to 35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM).The model includes effects for treatment, country/region, prior alpha-blocker therapy, baseline Erectile dysfunction (ED) severity (mild/moderate/severe),visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo-4.08
5 mg Tadalafil-5.49
0.2 mg Tamsulosin-4.92

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Change From Baseline in International Index of Erectile Function (IIEF) Erectile Function (EF) Domain at Week 12

IIEF is a 15 item self-reported questionnaire to assess overall erectile function and satisfaction during the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0(low/no erectile function) to 5(high erectile function) and Question 15 is scored 1(very low confidence) to 5(very high confidence) with a total score ranging from 1 to 30.Higher scores represent better erectile function.LS mean of change from baseline to endpoint is from MMRM.The model includes effects for treatment,country/region,baseline lower urinary tract symptoms(LUTS) severity (moderate/severe),visit,treatment-by-visit interaction,centered baseline value(defined as the baseline value for a participant-the overall baseline mean value), placebo lead-in total IPSS change(change from Visit 2 at Visit 3),centered baseline-by-treatment and treatment-by-country/region interactions.The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo1.88
5 mg Tadalafil5.24
0.2 mg Tamsulosin2.64

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Change From Baseline in IIEF Overall Satisfaction (OS) at Week 12

IIEF is a 15 item self-reported questionnaire used to assess overall erectile function and satisfaction during the past 4 weeks. IIEF-OS is the sum of Questions 13 and 14. Scores range from 1 (low/no satisfaction) to 5 (high satisfaction) for each question, with a total subscore ranging from 2 to 10;higher scores represent better erectile function. Least squares (LS) mean of change from baseline to endpoint is from an analysis mixed model for repeated measures (MMRM). The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction,centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo0.62
5 mg Tadalafil1.54
0.2 mg Tamsulosin0.71

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Change From Baseline in IIEF Orgasmic Function at Week 12

IIEF is a 15 item self-reported questionnaire used to assess overall erectile function and satisfaction during the past 4 weeks. IIEF orgasmic function is the sum of Q9 and Q10 of the IIEF. Scores ranged from 0 (no stimulation) to 5 (almost always) for each question, with the total possible score for the 2 questions ranging from 0 to 10. Higher scores were indicative of better orgasmic function. Least squares (LS) mean of change from baseline to endpoint is from MMRM. The model includes effects for treatment, country/region, baseline LUTS severity (moderate/severe), visit, treatment-by-visit interaction, centered baseline value (defined as the baseline value for a participant - the overall baseline mean value), placebo lead-in total IPSS change (change from Visit 2 at Visit 3), centered baseline-by-treatment and treatment-by-country/region interactions. The centered baseline-by-treatment and treatment-by-country interactions was removed if p >= 0.10. (NCT01937871)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
Placebo0.28
5 mg Tadalafil1.31
0.2 mg Tamsulosin0.57

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Change in Glomerular Filtration Rate (GFR)

Change in total GFR as measured by ml/1.72m2 (NCT01970176)
Timeframe: Baseline, 12 weeks

Interventionml/1.72m2 (Median)
Tadalafil-6.2
Placebo4.5

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Change in Urinary Cyclic Guanosine 3',5'-Monophosphate (cGMP) Hormone Excretion

Change in total urinary cGMP hormone excretion as measured by pmol/min (NCT01970176)
Timeframe: Baseline, 12 weeks

Interventionpmol/min (Median)
Tadalafil-71.1
Placebo51.6

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Change in Urinary Sodium Excretion

Change in total urinary sodium excretion as measured by MEq/min (NCT01970176)
Timeframe: Baseline, 12 weeks

InterventionMEq/min (Median)
Tadalafil29.5
Placebo25.1

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Change in Urinary Sodium Excretion

Change in total urinary sodium excretion as measured by MEq/min (NCT02058095)
Timeframe: Baseline, 12 weeks

InterventionMEq/min (Median)
Tadalafil74.43
Placebo29.11

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Change in Glomerular Filtration Rate (GFR)

Change in total GFR as measured by ml/1.72m2 (NCT02058095)
Timeframe: Baseline, 12 weeks

Interventionml/1.72 m2 (Median)
Tadalafil7
Placebo-9

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Change in Urinary Cyclic Guanosine 3',5'-Monophosphate (cGMP) Hormone Excretion

Change in total urinary cGMP hormone excretion as measured by pmol/min (NCT02058095)
Timeframe: Baseline, 12 weeks

Interventionpmol/min (Median)
Tadalafil450
Placebo-130.6

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Change From Baseline to 4 Weeks in 24 Hour Ambulatory Blood Pressure Monitoring (ABPM)

The LS mean change in blood pressure is calculated after adjusting for baseline, treatment and race using an analysis of covariance (ANCOVA). (NCT02194465)
Timeframe: Baseline, 4 Weeks

,,,,,,
InterventionmmHg (Least Squares Mean)
SBPDBP
13 mg LY2623091-11.1-4.7
13 mg LY2623091 + 20 mg Tadalafil-10.4-6.2
20 mg Tadalafil-6.3-5.6
24.5 mg LY2623091-10.4-3.4
6 mg LY2623091-4.9-1.7
Placebo0.31.0
Spironolactone-6.4-2.0

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of LY2623091

(NCT02194465)
Timeframe: 2 hours post-dose at 4 Weeks

Interventionnanogram/milliliter (ng/ml) (Geometric Mean)
6 mg LY2623091122
13 mg LY2623091228
24.5 mg LY2623091379
13 mg LY2623091 + 20 mg Tadalafil206

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Change From Baseline to 4 Weeks in Seated Diastolic Blood Pressure (DBP)

Change from baseline in DBP as measured by a cuff. LS mean change from baseline was calculated using a MMRM with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT02194465)
Timeframe: Baseline, 4 Weeks

InterventionmmHg (Least Squares Mean)
Placebo0.5
6 mg LY2623091-5.6
13 mg LY2623091-4.8
24.5 mg LY2623091-7.1
13 mg LY2623091 + 20 mg Tadalafil-6.8
20 mg Tadalafil-6.6
Spironolactone-1.2

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Change From Baseline to 4 Weeks in Seated Systolic Blood Pressure (SBP)

Change from baseline in SBP as measured by a cuff. Least squares (LS) mean change from baseline was calculated using a mixed model repeating measures (MMRM) with treatment, country, visit, and treatment-by-visit interaction as fixed effects and baseline as a covariate. (NCT02194465)
Timeframe: Baseline, 4 Weeks

Interventionmillimeter of mercury (mmHg) (Least Squares Mean)
Placebo-0.5
6 mg LY2623091-13.1
13 mg LY2623091-14.6
24.5 mg LY2623091-14.3
13 mg LY2623091 + 20 mg Tadalafil-11.8
20 mg Tadalafil-7.1
Spironolactone-15.4

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Change From Baseline to 4 Weeks in Serum Potassium

Potassium measurement as measured by standard laboratory tests. The LS mean change in potassium is calculated using MMRM with adjustment for baseline, treatment, visit, treatment*visit and race. (NCT02194465)
Timeframe: Baseline, 4 Weeks

Interventionmillimoles/L (mmol/L) (Least Squares Mean)
Placebo-0.04
6 mg LY26230910.10
13 mg LY26230910.11
24.5 mg LY26230910.25
13 mg LY2623091 + 20 mg Tadalafil0.10
20 mg Tadalafil-0.06
Spironolactone0.30

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Percentage of Participants Experiencing at Least One Adverse Event Leading to Discontinuation

Data presented are the number of participants who experienced 1 or more AEs (all causalities and drug-related) and serious AEs (SAEs) that lead to discontinuation. A summary of serious and other non-serious adverse events, regardless of causality, is located in the Reported Adverse Events module. (NCT02224846)
Timeframe: Baseline through Month 12

Interventionpercentage of participants (Number)
2.5 mg/5 mg Tadalafil1.4
5 mg Tadalafil0.7

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Percentage of Participants Experiencing at Least One Treatment Emergent Adverse Event (Serious or Non-Serious)

A Treatment Emergent Adverse Event (TEAE) was defined as an event that first occurs or worsens (increases in severity) after baseline, regardless of causality or severity. The percentage of participants with TEAEs was calculated by dividing the number of participants with at least 1 TEAE over the 12-Month treatment period by the total number of participants analyzed, multiplied by 100%. A summary of serious and other non-serious adverse events, regardless of causality, is located in the Reported Adverse Events module. (NCT02224846)
Timeframe: Baseline through Month 12

InterventionPercentage of participants (Number)
2.5 mg/5 mg Tadalafil33.8
5 mg Tadalafil35.9

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"Percentage of Participants With Yes Responses to Global Assessment Questions (GAQ)1 and GAQ2"

"Participants with yes responses to GAQ Question 1 (GAQ1) and GAQ Question 2 (GAQ2) of the GAQ questionnaire at Month 3 and Month 12.~GAQ1: Has the treatment you have been taking during this study improved your erections? GAQ2: If yes, has the treatment improved your ability to engage in sexual activity?" (NCT02224846)
Timeframe: Month 3, Month12, Month 24

,
Interventionpercentage of participants (Number)
Month 3: GAQ1Month 12: GAQ1Month 24: GAQ1Month 3: GAQ2Month 12: GAQ2Month 24: GAQ2
2.5 mg/5 mg Tadalafil89.696.696.886.595.596.2
5 mg Tadalafil95.797.595.792.196.194.5

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"Percentage of Participants With Yes Responses to Sexual Encounter Profile (SEP) Diary"

Participant-assessed diary has 5 questions(QI-Q5): 4 of the 5 questions were analyzed. Q2: successful penetration, Q3: successful intercourse, Q4: satisfied with erection, and Q5: satisfied with sexual experience) for each sexual encounter made over a specified period of time. SEP Q1-Q5 scores were determined as the percentage of 'Yes' responses to each of the 5 questions out of all sexual attempts recorded during the time period. (NCT02224846)
Timeframe: Month 1, Month 3

,
InterventionPercentage of participants (Mean)
Q2: successful penetration,Month 1Q2: successful penetration,Month 3Q3: successful intercourse,Month 1Q3: successful intercourse,Month 3Q4: satisfied with erection, Month 1Q4: satisfied with erection, Month 3Q5: satisfied with sexual experience,Month 1Q5: satisfied with sexual experience,Month 3
2.5 mg/5 mg Tadalafil81.388.241.255.724.839.920.435.7
5 mg Tadalafil86.791.749.560.135.543.531.139.2

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Change From Baseline in the IIEF-EF Domain Questionnaire Score of 5 mg Tadalafil Treatments

IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (no sexual activity for Question 1, no sexual stimulation for Question 2 and did not attempt intercourse for Questions 3-5) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Least Squares (LS) mean of the change from baseline is from Mixed effect Model Repeat Measurement (MMRM) model. The model included covariates baseline + visit + pooled investigator + baseline*visit, where participant is a random effect. (NCT02224846)
Timeframe: Baseline, Month 6; Baseline, Month 12;Baseline, Month 18; Baseline, Month 24

,
Interventionunits on a scale (Least Squares Mean)
Month 6Month 12Month 18Month 24
2.5 mg/5 mg Tadalafil8.28.18.68.6
5 mg Tadalafil7.97.98.38.5

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Percentage of Participants Achieving Normal Erectile Functioning

Participants achieving a normal erectile functioning (defined as having an IIEF-EF Domain score of >=26) at Month 1 and Month 3. (NCT02224846)
Timeframe: Month 1, Month 3

,
InterventionPercentage of partcipants (Number)
Month 1Month 3
2.5 mg/5 mg Tadalafil22.231.6
5 mg Tadalafil30.937.6

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Percentage of Participants Achieving Normal Erectile Functioning of 5 mg Tadalafil Treatments

Participants achieving a normal erectile functioning (defined as having an IIEF-EF Domain score of >=26) at Month 6 and Month 12. (NCT02224846)
Timeframe: Month 6, Month 12, Month 18, Month 24

,
InterventionPercentage of participants (Number)
Month 6Month 12Month 18Month 24
2.5 mg/5 mg Tadalafil38.244.144.645.5
5 mg Tadalafil42.343.543.748.2

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Change From Baseline in the International Index of Erectile Function- Erectile Function (IIEF-EF) Domain Questionnaire Score

IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (no sexual activity for Question 1, no sexual stimulation for Question 2 and did not attempt intercourse for Questions 3-5) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Least Squares (LS) mean of the change from baseline is from Mixed effect Model Repeat Measurement (MMRM) model. The model included covariates baseline + visit + pooled investigator + baseline*visit, where participant is a random effect. (NCT02224846)
Timeframe: Baseline, Month 1; Baseline, Month 3

,
Interventionunits on a scale (Least Squares Mean)
Month 1Month 3
2.5 mg/5 mg Tadalafil4.56.1
5 mg Tadalafil6.27.4

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
LY2623091 (Group 1)2540
Itraconazole + LY2623091 (Group 1)5660
LY2623091 (Group 4)2390
Diltiazem + LY2623091 (Group 4)3360

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Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
LY2623091 (Group 1)61.9
Itraconazole + LY2623091 (Group 1)66.9
LY2623091 (Group 4)61.8
Diltiazem + LY2623091 (Group 4)64.2

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng*hr/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin23.06.87
Simvastatin (Group 2)16.55.42

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Zero to Infinity (AUC[0-infinity]) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng*h/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin24.18.88
Simvastatin (Group 2)17.47.15

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Time T, Where T is the Last Time Point With a Measurable Concentration (AUC[0-tlast]) of LY2623091

(NCT02300259)
Timeframe: Group 1 (Days 1 and 6) Group 4 (Days 1 and 4): Predose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216, 240 hours (hr) postdose; additionally for Group 1 (Day 6): 264, 288, 312, 336, 360 hr postdose

Interventionng*hr/mL (Geometric Mean)
LY2623091 (Group 1)2480
Itraconazole + LY2623091 (Group 1)5240
LY2623091 (Group 4)2340
Diltiazem + LY2623091 (Group 4)3130

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Pharmacokinetics: Maximum Drug Concentration (Cmax) of Simvastatin and Simvastatin Acid

(NCT02300259)
Timeframe: Days 1 and 12: Predose, 0.5, 1, 2, 3, 4, 6, 8, 12 hours postdose

,
Interventionng/mL (Geometric Mean)
SimvastatinSimvastatin Acid
LY2623091 + Simvastatin (Group 2)9.890.877
Simvastatin (Group 2)7.780.720

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Percentage of Participants With PGI-I (Drug Attributes Questionnaire) on 8 Symptoms for BPH-Lower Urinary Tract Symptoms Improvement

PGI-I (Drug Attributes Questionnaire [DRAQ]) on 8 Symptoms for BPH-Lower Urinary Tract Symptoms.The DRAQ includes the following urinary symptoms: 1. Difficulty to void; 2. Frequent nighttime voiding; 3. Feeling of incomplete emptying; 4. Frequent daytime voiding; 5. Urinary urgency; 6. Taking a long time to urinate; 7. Need abdominal pressure to void; 8. Dribbling, leakage, and/or accidents. Each urinary symptom in the DRAQ will be evaluated by a participant using the PGI-I (discrete variables with seven categories) at the end of each treatment period, compared with how the symptom was before the participant's began taking medication in this study. The percentage of participants who reported a PGI-I (Drug Attributes Questionnaire) score of 1 to 3 are presented in the table below. (NCT02431754)
Timeframe: Week 8

,
Interventionpercentage of participants (Number)
Difficulty to void -Frequent nighttime voidingFeeling of incomplete emptyingFrequent daytime voidingUrinary urgencyTaking a long time to urinateNeed abdominal pressure to voidDribbling, leakage, and/or accidents
Placebo37.942.934.837.931.732.933.527.3
Tadalafil44.948.548.542.537.142.533.526.9

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Change From Baseline on the IPSS Quality of Life Score (IPSS QoL )

"IPSS QoL assess participant response to the following question: If you were to spend the rest of your life with your urinary condition just the way it is now, how would you feel about that?. Response options are Delighted (0), Pleased (1); Mostly satisfied (2); mixed about equally satisfied and dissatisfied (3); Mostly dissatisfied (4); Unhappy (5); Terrible (6), with a total ranging from 0 to 6 with higher numerical score representing worse Quality of Life from BPH symptom." (NCT02431754)
Timeframe: Baseline, Week 8

Interventionunits on a scale (Mean)
Tadalafil-0.4
Placebo-0.4

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Change From Baseline on the International Prostate Symptom Score (IPSS) Total Score

IPSS Total Score is the sum of Questions 1 through 7 of the IPSS questionnaire. Each question was scored from 0 (none/no symptoms) to 5 (frequent symptoms) for an IPSS Total Score ranging from 0 to 35 points; higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT02431754)
Timeframe: Baseline, Week 8

Interventionunits on a scale (Mean)
Tadalafil-2.5
Placebo-1.8

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Change From Baseline on the IPSS Storage (Irritative) Subscore

IPSS Storage (Irritative) subscore was the sum of Questions 2, 4 and 7 of the IPSS questionnaire. Scores ranged from 0 (no irritative symptoms) to 5 (frequent irritative symptoms), with total subscore of the 3 questions for irritative subscore ranging from 0 to 15. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT02431754)
Timeframe: Baseline,Week 8

Interventionunits on a scale (Mean)
Tadalafil-0.6
Placebo-0.5

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Change From Baseline on the IPSS Voiding (Obstructive) Subscore

IPSS voiding (obstructive) subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores ranged from 0 (no obstructive symptoms) to 5 (frequent obstructive symptoms), with total subscore of the 4 questions of the obstructive score ranging from 0 to 20. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. (NCT02431754)
Timeframe: Baseline, Week 8

Interventionunits on a scale (Mean)
Tadalafil-2.0
Placebo-1.3

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Percentage of Participants With Global Impression of Improvement (PGI-I)

"The PGI I is a participant rated instrument that measures the improvement or worsening of the subject's symptoms based on a 7 point scale. A score of 1 indicates that the subject feels his symptoms are very much better. A score of 4 indicates that the subjects feels no change in his symptoms and a score of 7 indicates that the subject feels his symptoms are very much worse. The percentage of participants who reported a PGI-I score of 1 to 3 are presented in the table below." (NCT02431754)
Timeframe: Week 8

Interventionpercentage of participants (Number)
Tadalafil61.1
Placebo53.4

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Percentage of Participants Preferring Combination Therapy Over Alpha Blocker Alone on the Treatment Preference Questionnaire (TPQ)

TPQ was used to investigate participant's preference between alpha1 blocker monotherapy and combination therapy with alpha1 blocker plus tadalafil. At the end of Treatment Period 2 (or discontinuation), participants were asked to choose a preferred treatment between the two treatments given in Treatment Period 1 and Treatment Period 2. (NCT02431754)
Timeframe: Week 20

,
Interventionpercentage of participants (Number)
Prefer therapy tadalafil + a1 blockerPrefer therapy placebo + a1 blocker
Placebo/Tadalafil68.331.7
Tadalafil/Placebo44.056.0

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Percentage of Participants With Absence of Worsening From Baseline to Week 26 in World Health Organization (WHO) Functional Class (FC)

WHO FC is a classification graded from Class I to IV which reflects disease severity based on symptoms. Worsening was defined as death or hospitalization due to PAH. Class I: No limitation of activity; Class II: slight limitation with ordinary activities; Class III: may not have symptoms at rest but greatly limited activities; Class IV: symptoms at rest and inability to carry out any physical activity without symptoms. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Week 26

Interventionpercentage of participants (Number)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)99.2
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)97.5

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Number of Participants With Disease Progression Event

Number of participants with disease progression event were reported. Disease progression event as adjudicated by the CEC, defined as any of the following: a. Death (all causes; adjudicated for PAH relationship); b. Hospitalization for worsening PAH; c. Initiation of prostacyclin, a prostacyclin analog, or a prostacyclin receptor agonist for worsening PAH; d. Clinical worsening defined as a post-baseline decrease in 6MWD by more than (>) 15 percent (%) from the highest 6MWD obtained at or after baseline, accompanied by WHO FC III or IV (both conditions confirmed at two consecutive post-baseline visits separated by 1-21 days). (NCT02558231)
Timeframe: Week 26, Month 12, Month 18, Month 24, Month 30, and End of Analysis Period (up to 40 months)

,
InterventionParticipants (Count of Participants)
Week 26Month 12Month 18Month 24Month 30End of Analysis Period (up to 40 months)
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)132023252727
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)81315151616

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Change From Baseline to Week 26 in 6-minute Walk Distance (6MWD)

The change from baseline to Week 26 in 6MWD was calculated as Week 26 minus baseline. The test measures the distance an individual is able to walk over a total of six minutes on a hard, flat surface. The goal is for the individual to walk as far as possible in six minutes. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionmeter (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)54.96
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)56.39

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Change From Baseline to Week 26 in Cardiac Index

Change from baseline to Week 26 in cardiac index was measured. Cardiac index is the amount of blood pumped by the heart, per minute, per meter square of body surface area. Re-calculated values were used for analysis and missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionliters per minute per meter square (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)0.97
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)0.84

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Change From Baseline to Week 26 in Mean Pulmonary Arterial Pressure (mPAP)

Change from baseline to Week 26 in mean Pulmonary Arterial Pressure (mPAP) was measured. The pulmonary artery pressure is a measure of the blood pressure found in the main pulmonary artery. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionmillimeters of mercury (mmHg) (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)-12.92
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)-12.20

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Change From Baseline to Week 26 in Mean Right Atrial Pressure (mRAP)

Change from baseline to Week 26 in mean Right Atrial Pressure (mRAP) was measured. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

InterventionmmHg (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)-1.78
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)-1.69

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Change From Baseline to Week 26 in N-terminal Pro B-type Natriuretic Peptide (NT-proBNP) Levels

The change from baseline to Week 26 in NT-proBNP was expressed as the ratio of Week 26 to baseline NT-proBNP (Week 26 divided by baseline). A geometric least square mean ratio of Week 26 to baseline NT-proBNP <1 corresponds to a reduction in NT-proBNP from baseline. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionratio (Geometric Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)0.26
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)0.25

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Change From Baseline to Week 26 in Pulmonary Vascular Resistance (PVR)

Change from baseline to Week 26 in PVR was expressed as the ratio of Week 26 to baseline PVR value (Week 26 divided by baseline) using re-calculated PVR. PVR was determined by right heart catheterization (RHC). A geometric least square mean ratio of Week 26 to baseline PVR less than (<) 1 corresponds to a reduction in PVR from baseline. Missing values were imputed using a last observation carried forward (LOCF) approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionratio (Geometric Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)0.46
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)0.48

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Change From Baseline to Week 26 in Total Pulmonary Resistance

Change from baseline to Week 26 in total pulmonary resistance was measured. Total pulmonary resistance was calculated as mPAP/CO*80, where CO is cardiac output. Re-calculated values were used for analysis and missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventiondynes*second per centimeter^5 (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)-511.88
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)-514.28

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Change From Baseline to Week 26 in Venous Oxygen Saturation (%)

Change from baseline to Week 26 in venous oxygen saturation was measured. Missing values were imputed using a LOCF approach. (NCT02558231)
Timeframe: Baseline, Week 26

Interventionpercentage of oxygen saturation (Least Squares Mean)
Triple Oral Therapy (Macitentan, Tadalafil, and Selexipag)5.59
Double Oral Therapy (Macitentan, Tadalafil, and Placebo)6.79

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Body Fat

The body fat will be measured at baseline and Day 28 by Electrical bioimpedance in % (NCT02595684)
Timeframe: Body fat at Day 28

Interventionpercentage of fat (Mean)
Tadalafil33.7
Placebo33.1

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Area Under the Curve (AUC) Glucose

Area under the curve of glucose measured at baseline and Day 28. The area under the curve (AUC) of glucose, (0.5 * glucose (G) 0´ + (G 30´+G 60´ + G 90´) + 0.5 * G 120´) * 30; has been widely used for calculating the glycemic index and for evaluating the efficacy of medications for postprandial hyperglycemia. (NCT02595684)
Timeframe: AUC at Day 28

Interventionmmol*h/L (Mean)
Tadalafil503
Placebo522

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Diastolic Blood Pressure

(NCT02595684)
Timeframe: Diastolic Blood Pressure at Day 28

InterventionmmHg (Mean)
Tadalafil77
Placebo73

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Body Mass Index

The Body Mass Index will be measured at baseline and Day 28 by Quetelet Index Formula. (NCT02595684)
Timeframe: Body Mass Index at Day 28

Interventionkg/m^2 (Mean)
Tadalafil33.7
Placebo33.1

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Body Weight

The body weight will be measured at baseline and Day 28 by Electrical bioimpedance. (NCT02595684)
Timeframe: Body Weight at Day 28

Interventionkg (Mean)
Tadalafil99.1
Placebo98.2

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Fasting Glucose

Fasting glucose will be evaluated at baseline and Day 28 with enzymatic-colorimetric. (NCT02595684)
Timeframe: Fasting glucose at Day 28

Interventionmmol/L (Mean)
Tadalafil4.8
Placebo5.0

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First Phase of Insulin Secretion

"First phase of insulin secretion will be calculated at baseline and Day 28 with Stumvoll Index.~Human studies support the critical physiologic role of the first-phase of insulin secretion in the maintenance of postmeal glucose homeostasis.~First phase of insulin secretion was estimated using the Stumvoll index (1283+ 1.829 x insulin 30' - 138.7 x glucose 30' + 3.772 x insulin 0'), the entered values reflect the first phase of insulin secretion" (NCT02595684)
Timeframe: First phase of insulin secretion at Day 28

Interventionindex (Mean)
Tadalafil1602
Placebo1194

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High Density Lipoprotein Cholesterol (HDL-c)

High density lipoprotein cholesterol (HDL-c) levels will be evaluated at baseline and Day 28 with enzymatic-colorimetric techniques. (NCT02595684)
Timeframe: HDL-c levels at Day 28

Interventionmmol/L (Mean)
Tadalafil1.1
Placebo1.1

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Insulin Sensitivity

"Insulin sensitivity will be calculated at baseline and Day 28 with Matsuda Index.~Matsuda Index value is used to indicate insulin resistance on diabetes. Insulin sensitivity was calculated with Matsuda index [10,000 / √glucose 0' x insulin 0') (mean glucose oral glucose tolerance test (OGTT) x mean insulin OGTT)]. The entered values reflect the insulin sensitivity" (NCT02595684)
Timeframe: Insulin sensitivity at Day 28

Interventionindex (Mean)
Tadalafil4.8
Placebo4.9

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Low Density Lipoprotein Cholesterol (LDL-c)

Low density lipoprotein cholesterol (LDL-c) levels will be evaluated at baseline and Day 28 with Friedewald formula. (NCT02595684)
Timeframe: LDL-c levels at Day 28

Interventionmmol/L (Mean)
Tadalafil2.3
Placebo2.2

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Postprandial Glucose

Postprandial glucose will be evaluated at baseline and Day 28 after a oral glucose. tolerance test with enzymatic-colorimetric techniques. (NCT02595684)
Timeframe: Postprandial glucose at Day 28

Interventionmmol/L (Mean)
Tadalafil6.3
Placebo6.5

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Systolic Blood Pressure

The systolic blood pressure was evaluated at baseline and Day 28 with a digital sphygmomanometer. (NCT02595684)
Timeframe: Systolic Blood Pressure at Day 28

InterventionmmHg (Mean)
Tadalafil120
Placebo115

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Total Cholesterol

Total cholesterol levels will be evaluated at baseline and Day 28 with enzymatic-colorimetric techniques. (NCT02595684)
Timeframe: Total cholesterol levels at Day 28

Interventionmmol/L (Mean)
Tadalafil4.4
Placebo4.3

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Total Insulin Secretion

"Total insulin secretion will be calculated at baseline and Day 28 with Insulinogenic Index.~The insulinogenic index is a ratio that relates enhancement of circulating insulin to the magnitude of the corresponding glycemic stimulus.~Total insulin secretion was calculated with the insulinogenic index (ΔAUC insulin/ΔAUC glucose), the entered values reflect the total insulin secretion" (NCT02595684)
Timeframe: Total insulin secretion at Day 28

Interventionindex (Mean)
Tadalafil0.52
Placebo0.61

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Triglycerides

Triglycerides levels will be evaluated at baseline and Day 28 with enzymatic-colorimetric techniques. (NCT02595684)
Timeframe: Triglycerides levels at Day 28

Interventionmmol/L (Mean)
Tadalafil2.3
Placebo2.4

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Waist Circumference

Waist circumference was evaluated at baseline and at Day 28 with a flexible tape. (NCT02595684)
Timeframe: Waist circumference at Day 28

Interventioncm (Mean)
Tadalafil112
Placebo112

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Area Under the Curve (AUC) Insulin

Area under the curve of insulin measured at baseline and Day 28. The Area Under the Curve (AUC) of insulin, (0.5 * Insulin (I) 0´ + (I 30´+I 60´ + I 90´) + 0.5 * I 120´) * 30; has been widely used for calculating the glycemic index and for evaluating the efficacy of medications for postprandial hyperinsulinemia. (NCT02595684)
Timeframe: AUC at Day 28

Interventionpmol*h/L (Mean)
Tadalafil291
Placebo262

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Number of Participants With Clinical Chemistry Values of PCI- Part 2

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of clinical chemistry parameters like glucose, calcium, albumin, sodium and potassium. It was collected at Day 2 (48 hour). The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Glucose, lowGlucose, highAlbumin, lowAlbumin, highCalcium, lowCalcium, highPotassium, lowPotassium, highSodium, lowSodium, high
Part 2, Treatment FG10000000000
Part 2, Treatment FG20000000000
Part 2, Treatment FG30000000000
Part 2, Treatment R0000000000

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Number of Participants With Abnormal Urinalysis Results by Dipstick Method-Part 1

Urine samples were collected at Day -1 (Baseline) and 48 hour, from the participants for urinalysis, by standard dipstick method. The parameters analyzed were ketones, glucose, occult blood, and protein. The number of participants with parameters detected as trace-lysed, trace-intact, trace, 2+ and 1+ was reported. Safety Population was used for analysis. (NCT02688387)
Timeframe: Up to Day 2

,,,,
InterventionParticipants (Number)
Ketone, trace-lysed, Day -1Ketone, trace-intact, Day -1Ketone, trace, Day -1Ketone, 2+, Day -1Ketone 1+, Day -1Ketone, trace-lysed, 48 hourKetone, trace-intact, 48 hourKetone, trace, 48 hourKetone, 2+, 48 hourKetone 1+, 48 hourGlucose, trace-lysed, Day -1Glucose, trace-Intact, Day -1Glucose, trace, Day -1Glucose, 2+, Day -1Glucose, 1+, Day -1Glucose, trace-lysed, 48 hourGlucose, trace-Intact, 48 hourGlucose, trace, 48 hourGlucose, 2+, 48 hourGlucose, 1+, 48 hourOccult blood, trace-lysed, Day -1Occult blood, trace-Intact, Day -1Occult blood, trace, Day -1Occult blood, 2+, Day -1Occult blood, 1+, Day -1Occult blood, trace-lysed, 48 hourOccult blood, trace-Intact, 48 hourOccult blood, trace, 48 hourOccult blood, 2+, 48 hourOccult blood, 1+, 48 hourProtein, trace-lysed, Day -1Protein, trace-Intact, Day -1Protein, trace, Day -1Protein, 2+, Day -1Protein, 1+, Day -1Protein, trace-lysed, 48 hourProtein, trace-Intact, 48 hourProtein, trace, 48 hourProtein, 2+, 48 hourProtein, 1+, 48 hour
Part 1, Treatment R0010000000000000000001001030000001000100
Part 1,Treatment F10020000000000000000000000100020010100000
Part 1,Treatment F20000000100000000000011001100010000000000
Part 1,Treatment F30000000000000000000000001020000000100000
Part 1,Treatment F40000000000000000000011000110000000100000

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Maximum Observed Concentration (Cmax) of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 1

Cmax is defined as the maximum (or peak) plasma concentration that the drug achieves, after the drug has been administered. Blood samples were collected at the indicated time points for analysis of ambrisentan and tadafil. The analysis was done under fasting condition post single dose. There is no formal hypotheses tested for Part 1 of the study. The analysis was performed on Pharmacokinetic (PK) parameter population, which included all participants who provided PK parameter data. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,,
InterventionNanogram per milliliter (Geometric Mean)
Ambrisentan, CmaxTadalafil, Cmax
Part 1, Treatment R755.37567.62
Part 1,Treatment F1766.29581.41
Part 1,Treatment F2685.33595.47
Part 1,Treatment F3738.49588.11
Part 1,Treatment F4722.57590.36

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Cmax of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 2

Cmax is defined as the maximum (or peak) plasma concentration that the drug achieves, after the drug has been administered. Blood samples were collected at the indicated time-points, of Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. There is no formal hypotheses tested for Part 2 of the study. Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionNanogram per milliliter (Geometric Mean)
Ambrisentan, (n=21,20,20,20)Tadalafil, (n=20,20,20,20)
Part 2, Treatment FG1720.79561.60
Part 2, Treatment FG2748.63550.78
Part 2, Treatment FG3726.15553.31
Part 2, Treatment R710.90537.80

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Cmax for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-Part 3A

Cmax is defined as the maximum (or peak) plasma concentration that the drug achieves, after the drug has been administered. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3A, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fed and fasting condition post single dose. PK parameter population was used. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionNanogram per milliliter (Geometric Mean)
Ambrisentan, CmaxTadalafil, Cmax
Part 3A,Treatment R1515.61533.67
Part 3A,Treatment R2728.32520.62
Part 3A,Treatment X1550.02525.10
Part 3A,Treatment X2756.60508.72

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Change From Baseline in Vital- Temperature, Part 2

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for temperature. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. Safety population included all the participants enrolled into the study who received atleast one dose of investigational product. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionDegree celsius (Mean)
Temperature, 0.5 hourTemperature, 1 hourTemperature, 2 hourTemperature, 4 hourTemperature, 8 hourTemperature, 12 hourTemperature, 24 hourTemperature, 48 hourTemperature, 72 hour
Part 2, Treatment FG1-0.02-0.11-0.17-0.06-0.080.04-0.02-0.06-0.13
Part 2, Treatment FG2-0.05-0.01-0.030.030.050.090.240.030.05
Part 2, Treatment FG3-0.14-0.04-0.23-0.190.030.100.07-0.110.06
Part 2, Treatment R-0.07-0.13-0.12-0.010.020.20-0.06-0.06-0.09

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Cmax for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B

Cmax is defined as the maximum (or peak) plasma concentration that the drug achieves, after the drug has been administered. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionNanogram per milliliter (Geometric Mean)
Ambrisentan, CmaxTadalafil, Cmax
Part 3B,Treatment R3380.47511.80
Part 3B,Treatment Y1375.87488.36

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Cmax for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions-3B

Cmax is defined as the maximum (or peak) plasma concentration that the drug achieves, after the drug has been administered. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. PK parameter population was used. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionNanogram per milliliter (Geometric Mean)
Ambrisentan, CmaxTadalafil, Cmax
Part 3B,Treatment R4358.89303.74
Part 3B,Treatment Y2405.89340.63

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Change From Baseline in Vital- Temperature, Part 3B

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for temperature. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionDegree Celsius (Mean)
Temperature, 0.5 hour (n=30,31,32,30)Temperature, 1 hour (n=30,31,32,30)Temperature, 2 hour (n=29,31,32,30)Temperature, 4 hour(n=30,31,32,30)Temperature, 8 hour (n=30,31,32,30)Temperature, 12 hour (n=30,31,32,30)Temperature, 24 hour (n=30,31,32,30)Temperature, 48 hour (n=30,31,32,30)Temperature, 72 hour (n=30,31,31,30)
Part 3B,Treatment R30.110.100.090.070.230.320.230.160.14
Part 3B,Treatment R40.050.090.040.090.170.450.190.220.08
Part 3B,Treatment Y10.060.060.050.100.290.310.340.190.33
Part 3B,Treatment Y20.130.070.070.050.220.390.120.130.26

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Change From Baseline in Vital- Temperature, Part 3A

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for temperature. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionDegree Celsius (Mean)
Temperature, 0.5 hourTemperature, 1 hourTemperature, 2 hourTemperature, 4 hourTemperature, 8 hourTemperature, 12 hourTemperature, 24 hourTemperature, 48 hourTemperature, 72 hour
Part 3A,Treatment R10.150.120.100.160.150.090.060.120.10
Part 3A,Treatment R20.120.040.07-0.010.150.270.160.320.18
Part 3A,Treatment X10.210.180.260.180.210.220.290.340.18
Part 3A,Treatment X20.010.070.050.150.120.270.250.280.20

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Change From Baseline in Vital- Temperature, Part 1

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for temperature. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,,
InterventionDegree celsius (Mean)
Temperature, 0.5 hourTemperature, 1 hourTemperature, 2 hourTemperature, 4 hourTemperature, 8 hourTemperature, 12 hourTemperature, 24 hourTemperature, 48 hourTemperature, 72 hour
Part 1, Treatment R-0.03-0.12-0.14-0.100.020.020.070.160.02
Part 1,Treatment F1-0.20-0.15-0.14-0.28-0.040.09-0.04-0.010.12
Part 1,Treatment F2-0.05-0.09-0.16-0.080.030.160.030.180.03
Part 1,Treatment F3-0.12-0.07-0.23-0.17-0.08-0.030.140.01-0.02
Part 1,Treatment F4-0.18-0.06-0.04-0.030.080.080.130.050.10

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Change From Baseline in Vital- Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP), Part 1

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for SBP and DBP. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. Safety population included all the participants enrolled into the study who received atleast one dose of investigational product. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,,
InterventionMilliliters of Mercury (Mean)
DBP, 0.5 hourDBP, 1 hourDBP, 2 hourDBP, 4 hourDBP, 8 hourDBP, 12 hourDBP, 24 hourDBP, 48 hourDBP, 72 hourSBP, 0.5 hourSBP, 1 hourSBP, 2 hourSBP, 4 hourSBP, 8 hourSBP, 12 hourSBP, 24 hourSBP, 48 hourSBP, 72 hour
Part 1, Treatment R-2.79-4.40-5.83-5.21-7.83-5.60-3.55-0.74-0.15-3.36-3.74-5.40-5.36-8.40-3.60-1.79-0.313.00
Part 1,Treatment F1-3.33-5.33-5.24-4.29-9.10-4.76-5.86-2.380.76-1.10-2.76-6.05-3.90-6.100.14-1.481.526.95
Part 1,Treatment F2-3.54-4.72-5.28-5.72-6.67-6.16-4.50-1.02-0.67-3.22-4.13-5.39-7.30-5.48-0.84-3.172.393.52
Part 1,Treatment F3-4.20-5.63-5.98-6.07-6.50-5.72-4.07-4.020.20-1.59-2.54-3.11-5.50-4.020.540.022.503.37
Part 1,Treatment F4-2.86-5.73-7.27-7.09-9.68-8.18-5.59-4.18-1.73-3.68-6.00-6.91-6.59-10.55-4.77-3.82-0.644.18

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Change From Baseline in Vital- SBP and DBP, Part 3B

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for SBP and DBP. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionMilliliters of Mercury (Mean)
DBP, 0.5 hourDBP, 1 hourDBP, 2 hourDBP, 4 hourDBP, 8 hourDBP, 12 hourDBP, 24 hourDBP, 48 hourDBP, 72 hourSBP, 0.5 hourSBP, 1 hourSBP, 2 hourSBP, 4 hourSBP, 8 hourSBP, 12 hourSBP, 24 hourSBP, 48 hourSBP, 72 hour
Part 3B,Treatment R3-2.53-3.41-5.00-6.56-7.81-5.88-3.31-0.41-0.470.30-0.20-1.98-3.14-3.050.450.363.452.76
Part 3B,Treatment R4-1.53-3.73-5.70-6.80-7.23-7.57-4.90-1.50-0.930.430.17-1.10-5.60-5.03-1.03-1.771.871.70
Part 3B,Treatment Y1-1.42-3.92-6.52-5.02-4.38-3.38-1.62-0.650.850.77-1.27-0.57-4.17-2.872.17-0.135.332.80
Part 3B,Treatment Y2-2.15-3.31-5.92-6.85-6.56-5.15-4.05-0.400.31-0.920.11-4.34-3.92-2.950.11-2.560.501.76

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Change From Baseline in Vital- SBP and DBP, Part 3A

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for SBP, DBP. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionMilliliters of Mercury (Mean)
DBP, 0.5 hourDBP, 1 hourDBP, 2 hourDBP, 4 hourDBP, 8 hourDBP, 12 hourDBP, 24 hourDBP, 48 hourDBP, 72 hourSBP, 0.5 hourSBP, 1 hourSBP, 2 hourSBP, 4 hourSBP, 8 hourSBP, 12 hourSBP, 24 hourSBP, 48 hourSBP, 72 hour
Part 3A,Treatment R1-3.02-5.86-6.89-10.30-6.45-7.67-4.77-1.89-1.524.552.86-0.08-4.30-5.23-1.05-2.481.363.86
Part 3A,Treatment R2-1.45-5.36-6.05-6.27-8.20-7.36-5.89-1.770.800.17-1.95-3.95-4.77-5.27-1.58-2.080.803.52
Part 3A,Treatment X1-3.47-6.69-8.97-8.75-8.41-7.25-7.25-2.41-1.565.752.880.28-1.72-5.06-0.03-0.782.721.81
Part 3A,Treatment X2-0.36-4.73-6.03-6.24-7.76-6.18-4.27-0.791.24-0.32-4.14-2.05-4.35-5.32-0.47-1.081.683.14

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Change From Baseline in Vital Signs-Respiratory Rate, Part 3A

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Respiratory rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBreaths per minute (Mean)
Respiratory rate, 0.5 hourRespiratory rate, 1 hourRespiratory rate, 2 hourRespiratory rate, 4 hourRespiratory rate, 8 hourRespiratory rate, 12 hourRespiratory rate, 24 hourRespiratory rate, 48 hourRespiratory rate, 72 hour
Part 3A,Treatment R11.50.80.61.10.50.60.20.60.8
Part 3A,Treatment R2-0.2-0.70.20.1-0.30.4-1.3-0.70.1
Part 3A,Treatment X10.40.90.70.60.10.9-0.50.00.6
Part 3A,Treatment X20.80.20.70.20.10.50.1-0.10.3

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Change From Baseline in Vital Signs-Respiratory Rate, Part 3-B

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Respiratory rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBreaths per minute (Mean)
Respiratory rate, 0.5 hour (n=30,31,32,30)Respiratory rate, 1 hour (n=30,31,32,30)Respiratory rate, 2 hour (n=30,31,32,30)Respiratory rate, 4 hour (n=30,31,32,30)Respiratory rate, 8 hour(n=30,31,32,30)Respiratory rate, 12 hour (n=30,31,32,30)Respiratory rate, 24 hour(n=30,31,32,30)Respiratory rate, 48 hour(n=30,31,32,30)Respiratory rate, 72 hour (n=30,31,31,30)
Part 3B,Treatment R3-0.8-0.1-0.1-0.40.00.2-0.6-0.10.2
Part 3B,Treatment R40.80.20.60.50.51.10.11.20.6
Part 3B,Treatment Y1-0.3-0.6-0.20.30.4-0.8-1.3-0.8-0.1
Part 3B,Treatment Y20.4-0.70.60.10.9-0.3-0.7-0.0-0.0

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Change From Baseline in Vital Signs-Respiratory Rate, Part 2

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Respiratory rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBreaths per minute (Mean)
Respiratory rate, 0.5 hourRespiratory rate, 1 hourRespiratory rate, 2 hourRespiratory rate, 4 hourRespiratory rate, 8 hourRespiratory rate, 12 hourRespiratory rate, 24 hourRespiratory rate, 48 hourRespiratory rate, 72 hour
Part 2, Treatment FG1-0.7-0.4-1.2-0.10.50.2-0.3-0.20.6
Part 2, Treatment FG20.30.30.4-0.10.40.81.30.70.6
Part 2, Treatment FG3-1.1-0.7-1.1-1.0-0.5-0.50.4-0.60.6
Part 2, Treatment R0.7-0.9-0.6-0.10.10.8-0.1-0.50.2

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Change From Baseline in Vital Signs-Respiratory Rate, Part 1

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Respiratory rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,,
InterventionBreaths per minute (Mean)
Respiratory rate, 0.5 hourRespiratory rate, 1 hourRespiratory rate, 2 hourRespiratory rate, 4 hourRespiratory rate, 8 hourRespiratory rate, 12 hourRespiratory rate, 24 hourRespiratory rate, 48 hourRespiratory rate, 72 hour
Part 1, Treatment R1.10.60.50.40.61.71.00.30.8
Part 1,Treatment F1-0.5-0.5-0.0-1.00.10.5-0.50.2-0.8
Part 1,Treatment F2-0.7-1.0-1.0-0.80.20.4-0.7-0.6-0.1
Part 1,Treatment F3-0.10.0-0.2-0.50.00.3-0.40.40.7
Part 1,Treatment F40.30.60.40.20.60.9-0.1-0.01.0

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Change From Baseline in Vital Signs-Heart Rate, Part 3B

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for HR. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBeats per minute (Mean)
HR, 0.5 hourHR, 1 hourHR, 2 hourHR, 4 hourHR, 8 hourHR, 12 hourHR, 24 hourHR, 48 hourHR, 72 hour
Part 3B,Treatment R32.615.705.674.957.2313.897.778.087.37
Part 3B,Treatment R42.785.485.586.228.7816.627.7210.159.62
Part 3B,Treatment Y13.056.056.084.859.6515.858.029.7210.78
Part 3B,Treatment Y23.504.923.763.697.3415.506.928.189.18

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Change From Baseline in Vital Signs-Heart Rate, Part 3A

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Heart rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBeats per minute (Mean)
HR, 0.5 hourHR, 1 hourHR, 2 hourHR, 4 hourHR, 8 hourHR, 12 hourHR, 24 hourHR, 48 hourHR, 72 hour
Part 3A,Treatment R110.6612.9711.4110.9110.1614.387.009.479.59
Part 3A,Treatment R22.814.664.164.448.5616.387.288.0310.03
Part 3A,Treatment X18.2810.2811.0610.169.0615.288.728.509.19
Part 3A,Treatment X22.645.524.615.0610.7915.918.739.4510.91

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Change From Baseline in Vital Signs-Heart Rate, Part 2

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Heart rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. Safety population included all the participants enrolled into the study who received atleast one dose of investigational product. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionBeats per minute (Mean)
HR, 0.5 hourHR, 1 hourHR, 2 hourHR, 4 hourHR, 8 hourHR, 12 hourHR, 24 hourHR, 48 hourHR, 72 hour
Part 2, Treatment FG12.853.853.755.458.3014.808.805.707.90
Part 2, Treatment FG21.955.102.753.206.5515.508.005.107.80
Part 2, Treatment FG32.205.356.456.008.3016.458.705.909.30
Part 2, Treatment R1.453.123.213.369.3617.216.746.799.40

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Change From Baseline in Vital Signs-Heart Rate, Part 1

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for Heart rate. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,,
InterventionBeats per minute (Mean)
HR, 0.5 hourHR, 1 hourHR, 2 hourHR, 4 hourHR, 8 hourHR, 12 hourHR, 24 hourHR, 48 hourHR, 72 hour
Part 1, Treatment R3.744.172.832.127.5510.836.747.695.03
Part 1,Treatment F12.983.793.693.268.2610.406.179.216.21
Part 1,Treatment F22.894.114.413.637.9312.757.028.677.54
Part 1,Treatment F31.132.481.911.527.1710.486.527.576.57
Part 1,Treatment F42.983.302.483.166.1111.115.616.485.57

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AUC From Time of Dose to Last Measurable Concentration (AUC [0-t]), in FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 1

AUC (0-t), was defined as, the AUC measured from the time of dose to the last measurable concentration. Blood samples of 2.7 mL and 2 mL, were collected for ambrisentan and tadafil respectively. The plasma samples at Part 1, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours. The analysis was done under fasting condition post single dose. The PK Parameter Population was used for analysis. There is no formal hypotheses tested for Part 1 of the study. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, (AUC 0- t)Tadalafil, (AUC 0- t)
Part 1, Treatment R5605.5812805.01
Part 1,Treatment F15418.0312469.86
Part 1,Treatment F25434.8813307.95
Part 1,Treatment F35655.7513376.86
Part 1,Treatment F45858.1813238.89

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AUC (0-t) for FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 2

AUC (0-t), was defined as, the AUC measured from the time of dose to the last measurable concentration. Blood samples of 2.7 mL and 2 mL, were collected for ambrisentan and tadafil respectively. The plasma samples for Part 2, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours. The analysis was done under fasting condition post single dose. PK parameter Population was used for analysis. There is no formal hypotheses tested for Part 2 of the study. Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, (n=21,20,20,20)Tadalafil, (n=20,20,20,20)
Part 2, Treatment FG16016.6213149.19
Part 2, Treatment FG26051.8313305.50
Part 2, Treatment FG36015.1113275.08
Part 2, Treatment R5893.7412832.91

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AUC (0-t) for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-Part 3A

AUC (0-t), was defined as, the AUC measured from the time of dose to the last measurable concentration. Blood samples of 2.7 mL and 2 mL, were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3A, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fed and fasting condition post single dose. PK parameter population was used. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, AUC (0-t)Tadalafil, AUC (0-t)
Part 3A,Treatment R15766.7114946.32
Part 3A,Treatment R26012.5113114.00
Part 3A,Treatment X15926.8714366.73
Part 3A,Treatment X26090.7413320.79

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AUC (0-t) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B

AUC (0-t), was defined as, the AUC measured from the time of dose to the last measurable concentration. Blood samples of 2.7 mL and 2 mL, were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. PK parameter population was used for analysis. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, AUC (0-t)Tadalafil, AUC (0-t)
Part 3B,Treatment R33190.5113325.63
Part 3B,Treatment Y13297.1613119.89

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Change From Baseline in Vital- SBP and DBP, Part 2

Vital signs were measured in semi-supine position after 5 minutes rest and were assessed for SBP and DBP. Change from Baseline, was defined as value at post-Baseline visit minus the Baseline value. Baseline, was defined as Day 1. (NCT02688387)
Timeframe: Baseline and Up to Day 3

,,,
InterventionMilliliters of Mercury (Mean)
DBP, 0.5 hourDBP, 1 hourDBP, 2 hourDBP, 4 hourDBP, 8 hourDBP, 12 hourDBP, 24 hourDBP, 48 hourDBP, 72 hourSBP, 0.5 hourSBP, 1 hourSBP, 2 hourSBP, 4 hourSBP, 8 hourSBP, 12 hourSBP, 24 hourSBP, 48 hourSBP, 72 hour
Part 2, Treatment FG10.28-4.23-4.98-3.53-2.58-3.18-1.032.483.231.63-3.93-2.48-2.13-3.984.38-0.684.785.13
Part 2, Treatment FG2-0.25-4.55-5.85-3.90-5.15-2.25-2.001.352.052.90-2.05-1.45-2.45-2.352.00-0.300.855.00
Part 2, Treatment FG3-1.00-4.35-7.05-5.10-5.65-4.35-5.251.401.50-0.33-1.98-7.33-5.58-6.380.83-1.682.083.48
Part 2, Treatment R-2.29-4.71-5.67-4.10-4.43-3.76-3.00-3.290.95-1.57-4.43-5.52-3.05-5.43-0.05-2.95-2.004.14

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AUC (0-inf) for Ambrisentan and Tadalafil, Following Candidate FDC (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fed and Fasted Conditions-3A

AUC (0- inf), is defined as area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity for ambrisentan and tadafil. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3A, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 48 and 72 hours post-dose. The analysis, was done under fed and fasting conditions post single dose. PK parameter population was used. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, AUC (0-inf)Tadalafil, AUC (0-inf)
Part 3A,Treatment R15898.7216596.18
Part 3A,Treatment R26155.6014612.84
Part 3A,Treatment X16075.5116086.66
Part 3A,Treatment X26231.4814856.32

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AUC (0-inf) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 40 mg) Under Fasted Conditions-3B

AUC (0- inf), is defined as area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity for ambrisentan and tadafil. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36,48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. PK Parameter Population was used for analysis. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionHour nanogram per milliliter (Geometric Mean)
Ambrisentan AUC (0-inf)Tadalafil, AUC (0-inf)
Part 3B,Treatment R33277.8114938.29
Part 3B,Treatment Y13397.5114724.34

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AUC (0-inf) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions-3B

AUC (0- inf), is defined as area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity for ambrisentan and tadafil. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis, was done under fasting conditions post single dose. PK parameter population was used for analysis. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan AUC (0-inf)Tadalafil, AUC (0-inf)
Part 3B,Treatment R43205.517748.47
Part 3B,Treatment Y23347.767962.14

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AUC (0 - Inf) for FDC, (Ambrisentan 10 mg + Tadalafil 40 mg) Relative to Reference Monotherapies Tested (Ambrisentan 10 mg & Tadalafil 40 mg), Under Fasting- Part 2

AUC (0- inf), is defined as area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity for ambrisentan and tadafil. Blood samples of 2.7 mL and 2 mL were collected for ambrisentan and tadafil respectively. The plasma samples for Part 2, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis, was done under fasting condition post single dose. PK parameter Populatio was used for analysis. There is no formal hypotheses tested for Part 2 of the study. Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, AUC (0-inf) (n=21,20,20,20)Tadalafil, AUC ( 0 - inf) (n=20,20,20,20)
Part 2, Treatment FG16179.4114443.86
Part 2, Treatment FG26189.2214502.37
Part 2, Treatment FG36201.4014457.33
Part 2, Treatment R6029.1914006.59

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Area Under the Plasma Concentration Time Curve (AUC) From Time Zero to Infinite (Inf) Time, AUC (0-inf) of Ambrisentan and Tadalafil in FDC (Ambrisentan 10 mg + Tadalafil 40 mg) and Montherapies (Ambrisentan 10 mg & Tadalafil 40 mg) - Part 1

AUC (0- inf), is defined as area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity for ambrisentan and tadafil. Blood samples were collected at the indicated time-points. The analysis was done under fasting condition post single dose. There is no formal hypothesis tested for Part 1 of the study. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan, (AUC 0 - inf)Tadalafil, (AUC 0 - inf)
Part 1, Treatment R5746.7313955.85
Part 1,Treatment F15566.0613408.30
Part 1,Treatment F25556.4414415.47
Part 1,Treatment F35788.9114545.28
Part 1,Treatment F46007.5714418.35

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Number of Participants With Abnormal Electrocardiogram (ECG) Findings, -Part 1

12-lead ECG, was measured in semi-supine position after 5 minutes rest. The data for worst case post-baseline has been reported. Data values for the participants with abnormal clinically significant values are reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to Day 3

InterventionParticipants (Number)
Part 1,Treatment F10
Part 1,Treatment F20
Part 1,Treatment F30
Part 1,Treatment F40
Part 1, Treatment R0

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Number of Participants With Abnormal ECG Findings, -Part 3B

12-lead ECG, were measured in semi-supine position after 5 minutes rest. It was conducted as triplicate at screen and baseline, whereas single measure at other times, unless out of range then triplicates were performed. The data for worst case post-baseline has been reported. Data values for the participants with abnormal clinically significant values are reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to Day 3

InterventionParticipants (Number)
Part 3B,Treatment Y10
Part 3B,Treatment Y20
Part 3B,Treatment R30
Part 3B,Treatment R40

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Number of Participants With Abnormal ECG Findings, -Part 3A

12-lead ECG, were measured in semi-supine position after 5 minutes rest. It was conducted as triplicate at screen and baseline, whereas single measure at other times, unless out of range then triplicates were performed. The data for worst case post-baseline has been reported. Data values for the participants with abnormal clinically significant values are reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to Day 3

InterventionParticipants (Number)
Part 3A,Treatment X10
Part 3A,Treatment X20
Part 3A,Treatment R10
Part 3A,Treatment R20

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Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 3B

Serial blood samples were collected at the indicated time-points. In Part 3B, tmax was determined for ambrisentan and tadalafil when administered in FDC (10mg/40mg) under fed state and fasted state and as reference monotherapies (ambrisentan 10 mg and tadalafil 40 mg). PK parameter population was used to measure the tmax. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour (Median)
Ambrisentan, TmaxTadafil, Tmax
Part 3B,Treatment R32.0002.500
Part 3B,Treatment R41.7582.008
Part 3B,Treatment Y11.7672.500
Part 3B,Treatment Y21.5001.500

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Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 3A

Serial blood samples were collected at the indicated time-points. In Part 3A, tmax was determined for ambrisentan and tadalafil when administered in FDC (10mg/40mg) under fed state and fasted state and as reference monotherapies (ambrisentan 10 mg and tadalafil 40 mg). PK parameter population was used to measure the tmax. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour (Median)
Ambrisentan, TmaxTadafil, Tmax
Part 3A,Treatment R14.008.000
Part 3A,Treatment R22.0002.258
Part 3A,Treatment X14.008.000
Part 3A,Treatment X21.5002.500

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AUC (0-t) for Ambrisentan and Tadalafil, FDCs (Ambrisentan 5 mg + Tadalafil 20 mg) Relative to Reference Monotherapies Tested (Ambrisentan 5 mg & Tadalafil 20 mg) Under Fasted Conditions- Part 3B

AUC (0-t), was defined as, the AUC measured from the time of dose to the last measurable concentration. Blood samples of 2.7 mL and 2 mL, were collected for ambrisentan and tadafil respectively. The plasma samples for Part 3B, were collected at the time-points pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48 and 72 hours post-dose. The analysis was done under fasting condition post single dose. PK parameter population was used for analysis. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,
InterventionHour*nanogram per milliliter (Geometric Mean)
Ambrisentan AUC (0-t)Tadalafil, AUC (0-t)
Part 3B,Treatment R43116.107076.48
Part 3B,Treatment Y23254.707264.28

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Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 2

Serial blood samples were collected at the indicated time-points. In Part 3A, tmax was determined for ambrisentan and tadalafil when administered in FDC (10mg/40mg) under fed state and fasted state and as reference monotherapies (ambrisentan 10 mg and tadalafil 40 mg). PK parameter population was used to measure the tmax. Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
Interventionhour (Median)
Ambrisentan, Tmax (n=21,20,20,20)Tadafil, Tmax (n=20,20,20,20)
Part 2, Treatment FG11.5001.750
Part 2, Treatment FG21.5002.000
Part 2, Treatment FG31.5082.000
Part 2, Treatment R1.5002.017

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Time Taken to Reach Maximum Concentration (Tmax) for Ambrisentan and Tadalafil in FDC and Reference Treatment - Part 1

Serial blood samples were collected at the indicated time-points. In Part 3A, tmax was determined for ambrisentan and tadalafil when administered in FDC (10mg/40mg) under fed state and fasted state and as reference monotherapies (ambrisentan 10 mg and tadalafil 40 mg). PK parameter population was used to measure the tmax. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,,
InterventionHour (Median)
Ambrisentan, TmaxTadafil, Tmax
Part 1, Treatment R1.5001.500
Part 1,Treatment F11.0001.500
Part 1,Treatment F21.5002.000
Part 1,Treatment F31.5002.000
Part 1,Treatment F41.5002.000

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Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 3B

t1/2 is defined as the time required by the concentration of the drug to reach half of its original value. The serial blood samples were assessed at specified timepoints. (NCT02688387)
Timeframe: Pre-dose, 0.5 hours, 1, 1.5, 2, 2.5, 4, 8, 12, 24, 36, 48, and 72 hours postdose

,,,
InterventionHour (Geometric Mean)
Ambrisentan, t1/2Tadalafil, t1/2
Part 3B,Treatment R316.1520.34
Part 3B,Treatment R416.0018.95
Part 3B,Treatment Y116.3920.27
Part 3B,Treatment Y216.4219.01

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Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 3A

t1/2 is defined as the time required by the concentration of the drug to reach half of its original value. The serial blood samples were assessed at specified timepoints. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour (Geometric Mean)
Ambrisentan, t1/2Tadalafil, t1/2
Part 3A,Treatment R114.6619.29
Part 3A,Treatment R215.6319.86
Part 3A,Treatment X115.6520.09
Part 3A,Treatment X215.4219.85

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Plasma t1/2 for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part 2

t1/2 is defined as the time required by the concentration of the drug to reach half of its original value. Only those participants available at the specified time points were analyzed (represented by n=X in the category titles). (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,
InterventionHour (Geometric Mean)
Ambrisentan, t1/2 (n=21,20,20,20)Tadalafil, t1/2, (n=20,20,20,20)
Part 2, Treatment FG115.7618.63
Part 2, Treatment FG215.3918.22
Part 2, Treatment FG316.6017.98
Part 2, Treatment R15.1918.58

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Plasma Half Life (t1/2) for Ambrisentan and Tadalafil in FDC and Reference Treatment Under Fed and Fasted Condition- Part1

t1/2 is defined as the time required by the concentration of the drug to reach half of its original value. (NCT02688387)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 2.5, 4, 8, 12, 18, 24, 36, 48 and 72 hours post-dose

,,,,
InterventionHour (Geometric Mean)
Ambrisentan, t1/2Tadalafil, t1/2
Part 1, Treatment R16.0818.04
Part 1,Treatment F116.7417.08
Part 1,Treatment F215.2517.76
Part 1,Treatment F315.7618.38
Part 1,Treatment F415.2518.48

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Number of Participants With Urinalysis Results by Dipstick Analysis-Part 3B

Urine samples were collected at Day -1 (Baseline) and 48 hour, from the participants for urinalysis, by standard dipstick method. The parameters analyzed were ketones, glucose, occult blood, and protein. The number of participants with parameters detected as trace-lysed, trace-intact, trace, 2+ and 1+ was reported. Safety Population was used for analysis. (NCT02688387)
Timeframe: Up to Day 2

,,,
InterventionParticipants (Number)
Ketone, trace-lysed, Day -1Ketone, trace-intact, Day -1Ketone, trace, Day -1Ketone, 3+, Day -1Ketone, trace-lysed, 48 hourKetone, trace-intact, 48 hourKetone, trace, 48 hourKetone, 3+, 48 hourGlucose, trace-lysed, Day -1Glucose, trace-Intact, Day -1Glucose, trace, Day -1Glucose, 3+, Day -1Glucose, trace-lysed, 48 hourGlucose, trace-Intact, 48 hourGlucose, trace, 48 hourGlucose, 3+, 48 hourOccult blood, trace-lysed, Day -1Occult blood, trace-Intact, Day -1Occult blood, trace, Day -1Occult blood, 3+, Day -1Occult blood, trace-lysed, 48 hourOccult blood, trace-Intact, 48 hourOccult blood, trace, 48 hourOccult blood, 3+, 48 hourProtein, trace-lysed, Day -1Protein, trace-Intact, Day -1Protein, trace, Day -1Protein, 3+, Day -1Protein, trace-lysed, 48 hourProtein, trace-Intact, 48 hourProtein, trace, 48 hourProtein, 3+, 48 hour
Part 3B,Treatment R300400010000000000300000000100000
Part 3B,Treatment R400100020000000000100010000200010
Part 3B,Treatment Y100100010000000002000000100000020
Part 3B,Treatment Y200410000000000000100000000100010

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Number of Participants With Urinalysis Results by Dipstick Analysis-Part 3A

Urine samples were collected at Day -1 (Baseline) and 48 hour, from the participants for urinalysis, by standard dipstick method. The parameters analyzed were ketones, glucose, occult blood, and protein. The number of participants with parameters detected as trace-lysed, trace-intact, trace, 2+ and 1+ was reported. Safety Population was used for analysis. (NCT02688387)
Timeframe: Up to Day 2

,,,
InterventionParticipants (Number)
Ketone, trace-lysed, Day -1Ketone, trace-intact, Day -1Ketone, trace, Day -1Ketone, 2+, Day -1Ketone 1+, Day -1Ketone, trace-lysed, 48 hourKetone, trace-intact, 48 hourKetone, trace, 48 hourKetone, 2+, 48 hourKetone 1+, 48 hourGlucose, trace-lysed, Day -1Glucose, trace-Intact, Day -1Glucose, trace, Day -1Glucose, 2+, Day -1Glucose, 1+, Day -1Glucose, trace-lysed, 48 hourGlucose, trace-Intact, 48 hourGlucose, trace, 48 hourGlucose, 2+, 48 hourGlucose, 1+, 48 hourOccult blood, trace-lysed, Day -1Occult blood, trace-Intact, Day -1Occult blood, trace, Day -1Occult blood, 2+, Day -1Occult blood, 1+, Day -1Occult blood, trace-lysed, 48 hourOccult blood, trace-Intact, 48 hourOccult blood, trace, 48 hourOccult blood, 2+, 48 hourOccult blood, 1+, 48 hourProtein, trace-lysed, Day -1Protein, trace-Intact, Day -1Protein, trace, Day -1Protein, 2+, Day -1Protein, 1+, Day -1Protein, trace-lysed, 48 hourProtein, trace-Intact, 48 hourProtein, trace, 48 hourProtein, 2+, 48 hourProtein, 1+, 48 hour
Part 3A,Treatment R10040100100000000000041020210010000000000
Part 3A,Treatment R20040000300000000000031000200010020000200
Part 3A,Treatment X10040000200000000000034000130000010000200
Part 3A,Treatment X20030000100000000000062010500000000000000

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Number of Participants With Urinalysis Results by Dipstick Analysis-Part 2

Urine samples were collected at Day -1 (Baseline) and 48 hour, from the participants for urinalysis, by standard dipstick method. The parameters analyzed were ketones, glucose, occult blood, and protein. The number of participants with parameters detected as trace-lysed, trace-intact, trace, 2+ and 1+ was reported. Safety Population was used for analysis (NCT02688387)
Timeframe: Up to Day 2

,,,
InterventionParticipants (Number)
Ketone, trace-intact, Day -1Ketone, trace, Day -1Ketone, 2+, Day -1Ketone, trace-intact, 48 hourKetone, trace, 48 hourKetone, 2+, 48 hourGlucose, trace-Intact, Day -1Glucose, trace, Day -1Glucose, 2+, Day -1Glucose, trace-Intact, 48 hourGlucose, trace, 48 hourGlucose, 2+, 48 hourOccult blood, trace-Intact, Day -1Occult blood, trace, Day -1Occult blood, 2+, Day -1Occult blood, trace-Intact, 48 hourOccult blood, trace, 48 hourOccult blood, 2+, 48 hourProtein, trace-Intact, Day -1Protein, trace, Day -1Protein, 2+, Day -1Protein, trace-Intact, 48 hourProtein, trace, 48 hourProtein, 2+, 48 hour
Part 2, Treatment FG1020000000000100000020010
Part 2, Treatment FG2020010000000000000020030
Part 2, Treatment FG3010001000000100100000030
Part 2, Treatment R010010000000000000010031

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Number of Participants With Serious Adverse Events (SAEs) and Adverse Events (AEs)-Part 1

An AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or is associated with liver injury and impaired liver function. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to 42 days

,,,,
InterventionParticipants (Number)
Any SAEAny AE
Part 1, Treatment R012
Part 1,Treatment F1012
Part 1,Treatment F2013
Part 1,Treatment F3013
Part 1,Treatment F4015

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Number of Participants With SAEs and AEs-Part 3B

An AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or is associated with liver injury and impaired liver function. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to 44 days

,,,
InterventionParticipants (Number)
Any SAEAny AE
Part 3B,Treatment R3024
Part 3B,Treatment R4015
Part 3B,Treatment Y1020
Part 3B,Treatment Y2018

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Number of Participants With Abnormal ECG Findings, -Part 2

12-lead ECG, were measured in semi-supine position after 5 minutes rest. It was conducted as triplicate at screen and baseline, whereas single measure at other times, unless out of range then triplicates were performed. The data for worst case post-baseline has been reported. Data values for the participants with abnormal clinically significant values are reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to Day 3

InterventionParticipants (Number)
Part 2, Treatment R0
Part 2, Treatment FG10
Part 2, Treatment FG20
Part 2, Treatment FG30

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Number of Participants With SAEs and AEs-Part 3A

An AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or is associated with liver injury and impaired liver function. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to 44 days

,,,
InterventionParticipants (Number)
Any SAEAny AE
Part 3A,Treatment R1025
Part 3A,Treatment R2023
Part 3A,Treatment X1024
Part 3A,Treatment X2021

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Number of Participants With SAEs and AEs-Part 2

An AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or is associated with liver injury and impaired liver function. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to 35 days

,,,
InterventionParticipants (Number)
Any SAEAny AE
Part 2, Treatment FG1012
Part 2, Treatment FG2014
Part 2, Treatment FG3012
Part 2, Treatment R013

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Number of Participants With Hematology Values of Potential Clinical Importance (PCI)- Part1

Blood samples were collected from the participants for analysis of hematology parameters like hematocrit, hemoglobin, lymphocytes, neutrophils, platelets and leukocytes. The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Up to Day 3

,,,,
InterventionParticipants (Number)
Hematocrit, lowHematocrit, highHemoglobin, lowHemoglobin, highLymphocytes, lowLymphocyte, highNeutrophils, lowNeutrophils, highPlatelets, lowPlatelets, highLeukocytes, lowLeukocytes, high
Part 1, Treatment R000100100010
Part 1,Treatment F1000000000000
Part 1,Treatment F2000010000020
Part 1,Treatment F3000000100010
Part 1,Treatment F4000000100010

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Number of Participants With Hematology Values of PCI - Part 3B

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of hematology parameters like hematocrit, hemoglobin, lymphocytes, neutrophils, platelets and leukocytes. It was conducted at Day 2 (48 hour). The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Hematocrit, lowHematocrit, highHemoglobin, lowHemoglobin, highLymphocytes, lowLymphocytes, highNeutrophils, lowNeutrophils, highPlatelets, lowPlatelets, highLeukocytes, lowLeukocytes, high
Part 3B,Treatment R3000000100000
Part 3B,Treatment R4000000200010
Part 3B,Treatment Y1000000000010
Part 3B,Treatment Y2000000200010

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Number of Participants With Hematology Values of PCI - Part 3A

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of hematology parameters like hematocrit, hemoglobin, lymphocytes, neutrophils, platelets and leukocytes. It was conducted at Day 2 (48 hours). The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Hematocrit, lowHematocrit, highHemoglobin, lowHemoglobin, highLymphocytes, lowLymphocytes, highNeutrophils, lowNeutrophils, highPlatelets, lowPlatelets, highLeukocytes, lowLeukocytes, high
Part 3A,Treatment R1000000000000
Part 3A,Treatment R2000000100010
Part 3A,Treatment X1000010000000
Part 3A,Treatment X2000010200010

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Number of Participants With Hematology Values of PCI - Part 2

Blood samples were collected from the participants for analysis of hematology parameters like hematocrit, hemoglobin, lymphocytes, neutrophils, platelets and leukocytes. The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Hematocrit, lowHematocrit, highHemoglobin, lowHemoglobin, highLymphocytes, lowLymphocytes, highNeutrophils, lowNeutrophils, highPlatelets, lowPlatelets, highLeukocytes, lowLeukocytes, high
Part 2, Treatment FG1000000100000
Part 2, Treatment FG2000000000000
Part 2, Treatment FG30000001000000
Part 2, Treatment R000000101000

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Number of Participants With Clinical Chemistry Values of PCI- Part1

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of clinical chemistry parameters like glucose, calcium, albumin, sodium and potassium. The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,,
InterventionParticipants (Number)
Glucose, lowGlucose, highAlbumin, lowAlbumin, highCalcium, lowCalcium, highPotassium, lowPotassium, highSodium, lowSodium, high
Part 1, Treatment R0000000000
Part 1,Treatment F10000000000
Part 1,Treatment F20000000000
Part 1,Treatment F30000000000
Part 1,Treatment F40000000000

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Number of Participants With Clinical Chemistry Values of PCI- Part 3B

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of clinical chemistry parameters like glucose, calcium, albumin, sodium and potassium. It was collected at Day 2 (48 hour). The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Glucose, lowGlucose, highAlbumin, lowAlbumin, highCalcium, lowCalcium, highPotassium, lowPotassium, highSodium, lowSodium, high
Part 3B,Treatment R30000000000
Part 3B,Treatment R40000000000
Part 3B,Treatment Y10000000100
Part 3B,Treatment Y20000000000

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Number of Participants With Clinical Chemistry Values of PCI- Part 3A

Blood samples of 2 mL, via a cannula for were collected from the participants for analysis of clinical chemistry parameters like glucose, calcium, albumin, sodium and potassium. It was collected at (48 hour). The data for number of participants, with low and high values of PCI have been reported. Safety population was used for analysis. (NCT02688387)
Timeframe: Day 2

,,,
InterventionParticipants (Number)
Glucose, lowGlucose, highAlbumin, lowAlbumin, highCalcium, lowCalcium, highPotassium, lowPotassium, highSodium, lowSodium, high
Part 3A,Treatment R10000000000
Part 3A,Treatment R20000000000
Part 3A,Treatment X10000000000
Part 3A,Treatment X20000000000

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Insulin Sensitivity After 12 Weeks of Drug Therapy

Subjects will undergo an insulin modified fasting intravenous glucose tolerance test (FS-IVGTT) protocol at 12 weeks adjusted statistically for the baseline measurement. (NCT02819440)
Timeframe: 12 weeks

Interventionml/kg/min/μIU ml (Median)
Tadalafil1.4
Placebo1.5

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Sexual Function

The Female Sexual Function Index will be used to measure sexual function in women with a range from 2-36 with higher scores indicating better sexual function. (NCT02819440)
Timeframe: 12 weeks

Interventionscore on a scale (Mean)
Tadalafil23.9
Placebo19.8

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Dual Energy X-Ray Absorptiometry (DEXA) (g)

fat mass at 12 weeks. (NCT02819440)
Timeframe: 12 weeks

Interventiongrams (Mean)
Tadalafil47
Placebo50

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Resting Energy Expenditure After 12 Weeks of Drug Therapy (kcal/Day)

Subjects will undergo a metabolic chamber protocol to measure resting exercise energy expenditure (kcal/min) at 12 weeks adjusted statistically for the baseline measurement. (NCT02819440)
Timeframe: 12 weeks

Interventionkcal/day (Mean)
Tadalafil1267
Placebo1268

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Quality of Life Using the Medical Outcomes Study Short-Form Health Survey (SF-36) Physical Component Score

Quality of life will be assessed using the Medical Outcomes Study Short-Form Health Survey (SF-36). The SF-36 is a 36 question survey with a total score range from 0-100; higher scores indicate better quality of life. (NCT02819440)
Timeframe: 12 weeks

Interventionscore on a scale (Mean)
Tadalafil52.7
Placebo51.0

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Physical Activity-induced Energy Expenditure (kcal/Day)

During the metabolic chamber protocol, conducted at baseline and at 12 weeks, the cardiopulmonary exercise test protocol will be conducted. The Energy Expenditure (EE) related to physical activity will be calculated as peak EE above the resting level while performing the exercise test. (NCT02819440)
Timeframe: 12 weeks

Interventionkcal/day (Mean)
Tadalafil3320
Placebo3269

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Maximal Oxygen Consumption

Subjects will undergo a symptom-limited cardiopulmonary exercise test to measure peak oxygen consumption (VO2 max). Maximal oxygen consumption will be measured as 'mL/min'. (NCT02819440)
Timeframe: 12 weeks

InterventionmL/min (Mean)
Tadalafil883
Placebo893

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Maximal Exercise Energy Expenditure (kcal/Day)

"Subjects will undergo a metabolic chamber protocol to measure maximal exercise energy expenditure (kcal/min) at 12 weeks adjusted statistically for the baseline measurement. Maximal Exercise Energy Expenditure will be measured as kcal/day" (NCT02819440)
Timeframe: 12 weeks

Interventionkcal/day (Mean)
Tadalafil4535
Placebo4588

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Number of Participants With Satisfactory Clinical Response at Week 24

"The treatment is assessed as efficient (participants with satisfactory clinical response) in case at least 2 out of the following 3 criteria were fulfilled~6 Minute Walking Distance increase by ≥ 10% or ≥ 30 m from baseline to Week 24~World Health Organization Functional Class (WHO FC) I or II at Week 24~N-terminal pro-brain natriuretic peptide (NT-proBNP) reduction ≥ 30% from baseline to Week 24 (NT-proBNP ratio Week 24/baseline ≤ 0.7) and in absence of the defined criteria of clinical worsening" (NCT02891850)
Timeframe: At Week 24

,
InterventionParticipants (Count of Participants)
With satisfactory clinical responseWithout satisfactory clinical response
PDE-5i2390
Riociguat4566

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Number of Participants With Adjudicated Clinical Worsening at Week 24

Clinical worsening was defined as death of any cause, hospitalization due to worsening pulmonary arterial hypertension (PAH) (adjudicated) or disease progression (adjudicated). (NCT02891850)
Timeframe: Up to 24 weeks

InterventionParticipants (Count of Participants)
Riociguat1
PDE-5i10

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Change in World Health Organization Functional Class (WHO FC) With Last Observation Carried Forward From Baseline to Week 24

The participant's functional class was determined by using the WHO classification. Possible classes range from I (patients with pulmonary hypertension (PH) but without resulting limitation of physical activity) to IV (patients with PH with inability to carry out any physical activity without symptoms). (NCT02891850)
Timeframe: From baseline and up to 24 weeks

Interventionclass (Mean)
Riociguat-0.5
PDE-5i-0.2

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Change in 6 Minute Walking Distance (6MWD) With Last Observation Carried Forward From Baseline to 24 Weeks

Six-minute walk distance (6MWD) was conducted to test the physical limitations of the participant by assessing the participant's exercise capacity. The distance walked by the participant in 6 minutes was measured. (NCT02891850)
Timeframe: From baseline and up to 24 weeks

Interventionmeters (m) (Mean)
Riociguat36.448
PDE-5i13.884

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Change in N-terminal Pro-Brain Natriuretic Peptide (NT-proBNP) With Last Observation Carried Forward at Week 24

N-terminal pro-brain natriuretic peptide (NT-proBNP) levels in the blood are used for screening, diagnosis of acute congestive heart failure (CHF) and may be useful to establish prognosis in heart failure. (NCT02891850)
Timeframe: From baseline and up to 24 weeks

Interventionpicograms per milliliter (pg/mL) (Mean)
Riociguat-88.234
PDE-5i81.414

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Best Overall Response (BOR)

Best overall response is defined as the best response recorded from the start of the treatment until disease progression/recurrence (taking as reference for progressive disease the smallest measurements recorded since the treatment started) assessed by the Response Evaluation Criteria in Solid Tumors (RECIST)v1.1. Complete Response (CR) is disappearance of all target lesions. Partial Response (PR) is at least a 30% decrease in the sum of the diameters of target lesions, taking as reference the baseline sum of diameters. Progressive Disease (PD) is at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). The appearance of one or more new lesions is also considered progressions). Stable Disease (SD) is neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference the smallest sum of diameters while on study. (NCT03785210)
Timeframe: Every 2 months and then every 6 months after discontinuation of treatment, for survival purposes, up to 3 years

,
InterventionParticipants (Count of Participants)
Complete ResponsePartial ResponseStable DiseaseProgressive DiseaseNot Evaluable
Cohort 1, Arm 1, Treatment Assignment Code 1, Participants With Hepatocellular Carcinoma00141
Cohort 2, Arm 1, Treatment Assignment Code 1, Participants With Liver Metastases00196

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Overall Survival (OS) of Nivolumab Combined With Oral Vancomycin and Tadalafil in Participants With Refractory Hepatocellular Carcinoma (HCC) or Liver Dominant Metastatic Cancer From Colorectal Cancer or Pancreatic Ductal Adenocarcinoma (PDAC)

Overall survival is calculated from the on-study date to the day of death using the Kaplan-Meier method. (NCT03785210)
Timeframe: Participants were followed from the on-study date to post discontinuation of treatment until the day of death, an average of 8 months.

InterventionMonths (Median)
Cohort 1, Arm 1, Treatment Assignment Code 1, Participants With Hepatocellular Carcinoma9.4
Cohort 2, Arm 1, Treatment Assignment Code 1, Participants With Liver Metastases3.4

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Number of Participants With Serious and/or Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0)

Here is the number of participants with serious and/or non-serious adverse events assessed by the Common Terminology Criteria for Adverse Events (CTCAE v5.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT03785210)
Timeframe: Date treatment consent signed to date off study, approximately 41 months/11 days and 36 months/22 days for the first and second group respectively.

InterventionParticipants (Count of Participants)
Cohort 1, Arm 1, Treatment Assignment Code 1, Participants With Hepatocellular Carcinoma6
Cohort 2, Arm 1, Treatment Assignment Code 1, Participants With Liver Metastases16

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Change in Pulmonary Vascular Resistance (PVR) Expressed as the Ratio of Geometric Means of End of Double-blind Treatment (EDBT) to Baseline

Change in PVR expressed as the ratio of geometric means of EDBT to baseline were reported. (NCT03904693)
Timeframe: Baseline, EDBT (up to 16 weeks)

InterventionRatio (Geometric Mean)
Treatment-naive And Prior ERA Strata: Macitentan 10 Milligrams (mg)0.77
Treatment-naive And Prior ERA Strata: M/T FDC0.55
Treatment-naive And Prior PDE-5i Strata: Tadalafil 20 mg0.78
Treatment-naive And Prior PDE-5i Strata: M/T FDC0.56

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Percentage of Uses Per Patient That Led to an Onset of Erection Within a Certain Period of Time in Patients Randomised to MED3000.

"Demonstrate a speed of onset of action from application of MED3000 gel to the time when patient notices their erection starting.~Percentage of MED3000 uses per patient that resulted in the patient noticing their erection starting within certain period of time, out of the total number of intercourse attempts made using the product during the 24-week treatment period. The certain periods of time are within 15 minutes, 10 minutes and 5 minutes. Percentage of uses is calculated with the denominator equal to the total number of intercourse attempts made using the product during the 24-week treatment period and the numerator equal to the total number of times that the response to the onset of action question 1 indicated a time of 5 (10, 15) minutes or less.~Question 1 of the Onset of Action questionnaire:~- After application of the gel/taking medication, when did you begin to notice your erection starting?" (NCT04984993)
Timeframe: 24 weeks

Interventionpercentage of uses per patient (Mean)
15 minutes10 minutes5 minutes
MED300062.5947.8124.01

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Percentage of Uses Per Patient That Led to an Onset of Action Within a Certain Period of Time in Patients Randomised to MED3000.

"Demonstrate a speed of onset of action from application of MED3000 gel to the time when the patients is able to have penetrative sex.~Percentage of MED3000 uses per patient that resulted in the patient being able to have penetrative sex within certain period of time, out of the total number of intercourse attempts made using the product during the 24-week treatment period. The certain periods of time are within 15 minutes, 10 minutes and 5 minutes. Percentage of uses is calculated with the denominator equal to the total number of intercourse attempts made using the product during the 24-week treatment period and the numerator equal to the total number of times that the response to the onset of action question 2 indicated a time of 5 (10, 15) minutes or less.~Question 2 of the Onset of Action questionnaire:~- After application of the gel/taking medication, when were you able to have penetrative sex?" (NCT04984993)
Timeframe: 24 weeks

Interventionpercentage of uses per patient (Mean)
15 minutes10 minutes5 minutes
MED300055.7031.9113.72

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Change From Baseline in the Erectile Function (EF) Domain of the International Index of Erectile Function (IIEF) Questionnaire, in Patients Randomised to MED3000, at Week 24

"Co-primary objectives:~Demonstrate an improvement compared to baseline of erectile function, in patients randomised to receive MED3000, using the IIEF-EF patient reported outcome instrument.~Observe a mean change from baseline of the IIEF-EF, in patients randomised to MED3000, greater or equal to the minimal clinically importance difference of 4.~The IIEF is a validated questionnaire, consisting of 15 questions, for detecting treatment changes in EF. The EF domain of IIEF is derived using questions 1, 2, 3, 4, 5 and 15. A score of 0 to 5 is awarded to each of questions 1 to 5 and a score of 1 to 5 is awarded to question 15. Higher scores indicate better sexual function. Domain score is computed by summing the scores for individual questions. The minimum and maximum possible scores are 1 and 30 respectively. Patients with a score of 21 or less are considered to have ED. Change from baseline = Week 24 score - Baseline score." (NCT04984993)
Timeframe: Baseline and Week 24

InterventionScore on a scale (Mean)
MED30005.73

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
acetone
methyl ketone : A ketone of formula RC(=O)CH3 (R =/= H).		7.1110ketone body;
methyl ketone;
propanones;
volatile organic compound		EC 3.5.1.4 (amidase) inhibitor;
human metabolite;
polar aprotic solvent
adenine
[no description available]		7.49206-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
betaine
glycine betaine : The amino acid betaine derived from glycine.		3.2310amino-acid betaine;
glycine derivative		fundamental metabolite
formic acid
formic acid: RN given refers to parent cpd. formic acid : The simplest carboxylic acid, containing a single carbon. Occurs naturally in various sources including the venom of bee and ant stings, and is a useful organic synthetic reagent. Principally used as a preservative and antibacterial agent in livestock feed. Induces severe metabolic acidosis and ocular injury in human subjects.		2.7830monocarboxylic acidantibacterial agent;
astringent;
metabolite;
protic solvent;
solvent
carnitine
[no description available]		4.4922amino-acid betainehuman metabolite;
mouse metabolite
choline
[no description available]		2.610cholinesallergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter;
nutrient;
plant metabolite;
Saccharomyces cerevisiae metabolite
hydrogen sulfide
Hydrogen Sulfide: A flammable, poisonous gas with a characteristic odor of rotten eggs. It is used in the manufacture of chemicals, in metallurgy, and as an analytical reagent. (From Merck Index, 11th ed). hydrogen sulfide : A sulfur hydride consisting of a single sulfur atom bonded to two hydrogen atoms. A highly poisonous, flammable gas with a characteristic odour of rotten eggs, it is often produced by bacterial decomposition of organic matter in the absence of oxygen.. thiol : An organosulfur compound in which a thiol group, -SH, is attached to a carbon atom of any aliphatic or aromatic moiety.		3.0540gas molecular entity;
hydracid;
mononuclear parent hydride;
sulfur hydride		Escherichia coli metabolite;
genotoxin;
metabolite;
signalling molecule;
toxin;
vasodilator agent
bupropion
Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring.		4.430aromatic ketone;
monochlorobenzenes;
secondary amino compound		antidepressant;
environmental contaminant;
xenobiotic
aminocaproic acid
Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator.		3.2310amino acid zwitterion;
epsilon-amino acid;
omega-amino fatty acid		antifibrinolytic drug;
hematologic agent;
metabolite
fosmidomycin
fosmidomycin: from Streptomyces lavendulae; RN given refers to parent cpd; structure in second source. fosmidomycin : Propylphosphonic acid in which one of the hydrogens at position 3 is substituted by a formyl(hydroxy)amino group. An antibiotic obtained from Streptomyces lavendulae, it specifically inhibits DXP reductoisomerase (EC 1.1.1.267), a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis.		2.1110hydroxamic acid;
phosphonic acids		antimicrobial agent;
bacterial metabolite;
EC 1.1.1.267 (1-deoxy-D-xylulose-5-phosphate reductoisomerase) inhibitor
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		4.95422-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
dimethyl sulfoxide
Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents.		2.4110sulfoxide;
volatile organic compound		alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger
glycerol
Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.		3.9421alditol;
triol		algal metabolite;
detergent;
Escherichia coli metabolite;
geroprotector;
human metabolite;
mouse metabolite;
osmolyte;
Saccharomyces cerevisiae metabolite;
solvent
hydrogen
Hydrogen: The first chemical element in the periodic table with atomic symbol H, and atomic number 1. Protium (atomic weight 1) is by far the most common hydrogen isotope. Hydrogen also exists as the stable isotope DEUTERIUM (atomic weight 2) and the radioactive isotope TRITIUM (atomic weight 3). Hydrogen forms into a diatomic molecule at room temperature and appears as a highly flammable colorless and odorless gas.. dihydrogen : An elemental molecule consisting of two hydrogens joined by a single bond.		7.2510elemental hydrogen;
elemental molecule;
gas molecular entity		antioxidant;
electron donor;
food packaging gas;
fuel;
human metabolite
melatonin
[no description available]		7.4920acetamides;
tryptamines		anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
nickel
Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.. nickel ion : A nickel atom having a net electric charge.. nickel atom : Chemical element (nickel group element atom) with atomic number 28.		7.1510metal allergen;
nickel group element atom		epitope;
micronutrient
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		2.1310pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		3.2310pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
nitrates
Nitrates: Inorganic or organic salts and esters of nitric acid. These compounds contain the NO3- radical.		9.8371monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species
nitrites
Nitrites: Salts of nitrous acid or compounds containing the group NO2-. The inorganic nitrites of the type MNO2 (where M=metal) are all insoluble, except the alkali nitrites. The organic nitrites may be isomeric, but not identical with the corresponding nitro compounds. (Grant & Hackh's Chemical Dictionary, 5th ed)		4.541monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species		human metabolite
pyrazinamide
pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis.		3.6120monocarboxylic acid amide;
N-acylammonia;
pyrazines		antitubercular agent;
prodrug
pyridoxine
4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms).		3.2310hydroxymethylpyridine;
methylpyridines;
monohydroxypyridine;
vitamin B6		cofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
thiamine
thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively.		3.2310primary alcohol;
vitamin B1		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
urea
pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives.		2.1110isourea;
monocarboxylic acid amide;
one-carbon compound		Daphnia magna metabolite;
Escherichia coli metabolite;
fertilizer;
flour treatment agent;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
8-hydroxy-2-(di-n-propylamino)tetralin
8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively		2.0410phenols;
tertiary amino compound;
tetralins		serotonergic antagonist
1-(3-chlorophenyl)piperazine
1-(3-chlorophenyl)piperazine: supposed metabolite of TRAZODONE; RN given refers to parent cpd; structure. 1-(3-chlorophenyl)piperazine : A N-arylpiperazine that is piperazine carrying a 3-chlorophenyl substituent at position 1. It is a metabolite of the antidepressant drug trazodone.		2.0810monochlorobenzenes;
N-arylpiperazine		drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic
1h-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one: structure given in first source; inhibits guanylyl cyclase. 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one : A member of the class of oxadiazoloquinoxalines that is 1H-[1,2,4]oxadiazolo[4,3-a]quinoxaline substituted at position 1 by an oxo group.		3.1450oxadiazoloquinoxalineEC 4.6.1.2 (guanylate cyclase) inhibitor
4-aminopyridine
[no description available]		2.2110aminopyridine;
aromatic amine		avicide;
orphan drug;
potassium channel blocker
phenytoin
[no description available]		3.2310imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
tacrine
Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.		2.0810acridines;
aromatic amine		EC 3.1.1.7 (acetylcholinesterase) inhibitor
acebutolol
Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.		3.6920aromatic amide;
ethanolamines;
ether;
monocarboxylic acid amide;
propanolamine;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympathomimetic agent
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		4.1640acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		4.9940monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
acetohydroxamic acid
acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group.		3.2310acetohydroxamic acids;
carbohydroximic acid		algal metabolite;
EC 3.5.1.5 (urease) inhibitor
ag-1296
6,7-dimethoxy-3-phenylquinoxaline: ATP-competitive inhibitor of receptor kinase		2.0310quinoxaline derivative
alaproclate
alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer		3.2310alpha-amino acid ester
albendazole
[no description available]		3.6120aryl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
albuterol
Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).		540phenols;
phenylethanolamines;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
environmental contaminant;
xenobiotic
alendronate
alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.		3.23101,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
alfuzosin
alfuzosin: structure given in first source		772monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
alosetron
alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.		3.2310imidazoles;
pyridoindole		antiemetic;
gastrointestinal drug;
serotonergic antagonist
alprazolam
Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug.		3.2310organochlorine compound;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA agonist;
muscle relaxant;
sedative;
xenobiotic
alprenolol
Alprenolol: One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.. alprenolol : A secondary alcohol that is propan-2-ol substituted by a 2-allylphenoxy group at position 1 and an isopropylamino group at position 3. It is a beta-adrenergic antagonist used as a antihypertensive, anti-arrhythmia and a sympatholytic agent.		2.0810secondary alcohol;
secondary amino compound		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
altretamine
Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.		3.2310triamino-1,3,5-triazine
amantadine
amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source		3.2310adamantanes;
primary aliphatic amine		analgesic;
antiparkinson drug;
antiviral drug;
dopaminergic agent;
NMDA receptor antagonist;
non-narcotic analgesic
ambenonium
ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens.		3.2310quaternary ammonium ionEC 3.1.1.8 (cholinesterase) inhibitor
diatrizoic acid
Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography.		3.6120acetamides;
benzoic acids;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
amifostine anhydrous
Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy.		3.2310diamine;
organic thiophosphate		antioxidant;
prodrug;
radiation protective agent
aminoglutethimide
Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position.		2.4620dicarboximide;
piperidones;
substituted aniline		adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
p-aminohippuric acid
p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow.		3.2310N-acylglycineDaphnia magna metabolite
theophylline
[no description available]		3.8930dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		3.89301-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
dan 2163
[no description available]		2.0810aromatic amide;
aromatic amine;
benzamides;
pyrrolidines;
sulfone		environmental contaminant;
second generation antipsychotic;
xenobiotic
amitriptyline
Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5.		3.6120carbotricyclic compound;
tertiary amine		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
tropomyosin-related kinase B receptor agonist;
xenobiotic
amlexanox
amlexanox: SRA-A antagonist;structure given in first source. amlexanox : A pyridochromene-derived monocarboxylic acid having an amino substituent at the 2-position, an oxo substituent at the 5-position and an isopropyl substituent at the 7-position.		2.0810monocarboxylic acid;
pyridochromene		anti-allergic agent;
anti-ulcer drug;
non-steroidal anti-inflammatory drug
amlodipine
Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.		10.3331dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound		antihypertensive agent;
calcium channel blocker;
vasodilator agent
amoxapine
Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position.		3.8930dibenzooxazepineadrenergic uptake inhibitor;
antidepressant;
dopaminergic antagonist;
geroprotector;
serotonin uptake inhibitor
amsacrine
Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity.		2.0810acridines;
aromatic ether;
sulfonamide		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
anastrozole
[no description available]		3.6120nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
anthralin
Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9.		2.0810anthracenesantipsoriatic
antipyrine
Antipyrine: An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29). antipyrine : A pyrazolone derivative that is 1,2-dihydropyrazol-3-one substituted with methyl groups at N-1 and C-5 and with a phenyl group at N-2.		2.0810pyrazoloneantipyretic;
cyclooxygenase 3 inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		6.2451benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
astemizole
Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects.. astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position.		2.7630benzimidazoles;
piperidines		anti-allergic agent;
anticoronaviral agent;
H1-receptor antagonist
atenolol
Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent.		3.9330ethanolamines;
monocarboxylic acid amide;
propanolamine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
sympatholytic agent;
xenobiotic
azathioprine
Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS.		3.6120aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine		antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug
baclofen
[no description available]		3.6120amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound		central nervous system depressant;
GABA agonist;
muscle relaxant
bendazac
bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts.		3.2310indazoles;
monocarboxylic acid		non-steroidal anti-inflammatory drug;
radical scavenger
bendroflumethiazide
Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group.		3.2310benzothiadiazine;
sulfonamide		antihypertensive agent;
diuretic
benzbromarone
Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication.		3.61201-benzofurans;
aromatic ketone		uricosuric drug
benzocaine
Benzocaine: A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.. dextran sulfate sodium : An organic sodium salt of dextran sulfate. It induces colitis in mice.. benzocaine : A benzoate ester having 4-aminobenzoic acid as the acid component and ethanol as the alcohol component. A surface anaesthetic, it is used to suppress the gag reflex, and as a lubricant and topical anaesthetic on the larynx, mouth, nasal cavity, respiratory tract, oesophagus, rectum, urinary tract, and vagina.		2.0810benzoate ester;
substituted aniline		allergen;
antipruritic drug;
sensitiser;
topical anaesthetic
bepridil
Bepridil: A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.. bepridil : A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl.		2.0510pyrrolidines;
tertiary amine		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
5-methoxypsoralen
5-Methoxypsoralen: A linear furanocoumarin that has phototoxic and anti-inflammatory properties, with effects similar to METHOXSALEN. It is used in PUVA THERAPY for the treatment of PSORIASIS.. 5-methoxypsoralen : A 5-methoxyfurocoumarin that is psoralen substituted by a methoxy group at position 5.		2.31105-methoxyfurocoumarin;
organic heterotricyclic compound;
psoralens		hepatoprotective agent;
plant metabolite
betaxolol
[no description available]		3.2310propanolamineantihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bethanechol
Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention.		3.2310carbamate ester;
quaternary ammonium ion		muscarinic agonist
bicalutamide
bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.		3.8630(trifluoromethyl)benzenes;
monocarboxylic acid amide;
monofluorobenzenes;
nitrile;
sulfone;
tertiary alcohol
bay h 4502
bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1.		2.0810biphenyls;
imidazoles
biperiden
Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease.		3.2310piperidines;
tertiary alcohol;
tertiary amino compound		antidote to sarin poisoning;
antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist;
parasympatholytic
bisacodyl
Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871)		3.6120diarylmethane
bisoprolol
Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS.		3.2310secondary alcohol;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent
bromhexine
Bromhexine: A mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p744). bromhexine : A substituted aniline that is 2,4-dibromoaniline which is substituted at position 6 by a [cyclohexyl(methyl)amino]methyl group. It is used (as the monohydrochloride salt) as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum).		2.0810organobromine compound;
substituted aniline;
tertiary amino compound		mucolytic
bromopride
bromopride: RN given refers to parent cpd; structure		2.0810benzamides
bronopol
[no description available]		2.0810nitro compound
bumetanide
[no description available]		3.6120amino acid;
benzoic acids;
sulfonamide		diuretic;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor
buspirone
Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position.		3.6120azaspiro compound;
N-alkylpiperazine;
N-arylpiperazine;
organic heteropolycyclic compound;
piperidones;
pyrimidines		anxiolytic drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
sedative;
serotonergic agonist
busulfan
[no description available]		3.6120methanesulfonate esteralkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent
secbutabarbital
secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital		3.2310barbiturates
caffeine
[no description available]		4.0940purine alkaloid;
trimethylxanthine		adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
verapamil
Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.		9.140aromatic ether;
nitrile;
polyether;
tertiary amino compound
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		3.2310benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		3.6120dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
carbinoxamine
carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease.		3.2310monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist
carisoprodol
Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.		3.2310carbamate estermuscle relaxant
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.0810N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
carprofen
carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs.		2.0810carbazoles;
organochlorine compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug;
photosensitizing agent
carvedilol
[no description available]		3.8730carbazoles;
secondary alcohol;
secondary amino compound		alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent
celecoxib
[no description available]		4.4560organofluorine compound;
pyrazoles;
sulfonamide;
toluenes		cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
cetirizine
Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.		3.2310ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines		anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		3.6120aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
chlorcyclizine
chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness		3.2310diarylmethane
chlordiazepoxide
Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2.		3.6120benzodiazepine
chlormezanone
Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions.		3.23101,3-thiazine;
lactam;
monochlorobenzenes;
sulfone		antipsychotic agent;
anxiolytic drug;
muscle relaxant
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		3.8830aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
chlorothiazide
Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension.		3.2310benzothiadiazineantihypertensive agent;
diuretic
chlorpheniramine
Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma.		3.6120monochlorobenzenes;
pyridines;
tertiary amino compound		anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor
chlorpromazine
Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.		4.140organochlorine compound;
phenothiazines;
tertiary amine		anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
phenothiazine antipsychotic drug
chlorpropamide
Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification.		3.6120monochlorobenzenes;
N-sulfonylurea		hypoglycemic agent;
insulin secretagogue
chlorthalidone
Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic.		3.6120isoindoles;
monochlorobenzenes;
sulfonamide
chlorzoxazone
Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm.		3.61201,3-benzoxazoles;
heteroaryl hydroxy compound;
organochlorine compound		muscle relaxant;
sedative
cifenline
[no description available]		2.4720diarylmethane
ciclopirox
[no description available]		2.0810cyclic hydroxamic acid;
hydroxypyridone antifungal drug;
pyridone		antibacterial agent;
antiseborrheic
ciglitazone
ciglitazone: structure given in second source; PPAR agonist used for type II diabetes. ciglitazone : An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist.		2.4620aromatic ether;
thiazolidinone		antineoplastic agent;
insulin-sensitizing drug
cilostamide
cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure		3.1210quinolines
cilostazol
[no description available]		5.460lactam;
tetrazoles		anticoagulant;
bronchodilator agent;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
fibrin modulating drug;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		3.6120aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
ciprofibrate
[no description available]		2.4620cyclopropanes;
monocarboxylic acid;
organochlorine compound		antilipemic drug
ciprofloxacin
Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.		3.6120aminoquinoline;
cyclopropanes;
fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone;
zwitterion		antibacterial drug;
antiinfective agent;
antimicrobial agent;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
environmental contaminant;
topoisomerase IV inhibitor;
xenobiotic
cisapride
Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.		2.0410benzamides
citalopram
Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group.		9.12402-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound
clenbuterol
Clenbuterol: A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma.. clenbuterol : A substituted aniline that is 2,6-dichloroaniline in which the hydrogen at position 4 has been replaced by a 2-(tert-butylamino)-1-hydroxyethyl group.		2.0310amino alcohol;
dichlorobenzene;
ethanolamines;
primary arylamine;
secondary amino compound;
substituted aniline		beta-adrenergic agonist;
bronchodilator agent;
sympathomimetic agent
clioquinol
Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease.		2.0810monohydroxyquinoline;
organochlorine compound;
organoiodine compound		antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antiprotozoal drug;
chelator;
copper chelator
clobazam
Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics.		2.08101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
GABA modulator
clofazimine
Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients.		2.0810monochlorobenzenes;
phenazines		dye;
leprostatic drug;
non-steroidal anti-inflammatory drug
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		3.8630aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clomiphene
[no description available]		3.6120tertiary amineestrogen antagonist;
estrogen receptor modulator
clomipramine
Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias.		3.6120dibenzoazepineanticoronaviral agent;
antidepressant;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
serotonergic antagonist;
serotonergic drug;
serotonin uptake inhibitor
clonazepam
Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation.		3.23101,4-benzodiazepinone;
monochlorobenzenes		anticonvulsant;
anxiolytic drug;
GABA modulator
clonidine
Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.		4.1420clonidine;
imidazoline
4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide
[no description available]		2.0810sulfonamide
chlorazepate
clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively.		3.23101,4-benzodiazepinoneanticonvulsant;
anxiolytic drug;
GABA modulator;
prodrug
clotrimazole
[no description available]		3.5720conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
cyclobenzaprine
cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm.		3.2310carbotricyclic compoundantidepressant;
muscle relaxant;
tranquilizing drug
cyclofenil
Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE.		3.2310organic molecular entity
cyproheptadine
Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.		3.2310piperidines;
tertiary amine		anti-allergic agent;
antipruritic drug;
gastrointestinal drug;
H1-receptor antagonist;
serotonergic antagonist
dapsone
[no description available]		3.6120substituted aniline;
sulfone		anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug
deferoxamine
Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator.		3.2310acyclic desferrioxaminebacterial metabolite;
ferroptosis inhibitor;
iron chelator;
siderophore
desipramine
Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.		3.8930dibenzoazepine;
secondary amino compound		adrenergic uptake inhibitor;
alpha-adrenergic antagonist;
antidepressant;
cholinergic antagonist;
drug allergen;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
serotonin uptake inhibitor
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		3.2310primary amine
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		3.95301,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
diazoxide
Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies.		3.6120benzothiadiazine;
organochlorine compound;
sulfone		antihypertensive agent;
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
diuretic;
K-ATP channel agonist;
sodium channel blocker;
sympathomimetic agent;
vasodilator agent
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		5.0221amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
dichlorphenamide
Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma.		3.2310dichlorobenzene;
sulfonamide		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
ophthalmology drug
dicyclomine
Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome.		3.2310carboxylic ester;
tertiary amine		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
pentetic acid
Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium.		3.2310pentacarboxylic acidcopper chelator
diflunisal
Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position.		3.2310monohydroxybenzoic acid;
organofluorine compound		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
dimercaprol
Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury.		3.2310dithiol;
primary alcohol		chelator
diphenhydramine
Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.		3.2310ether;
tertiary amino compound		anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative
dipyridamole
Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots.		4.7850piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol		adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
disopyramide
Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug.		3.6120monocarboxylic acid amide;
pyridines;
tertiary amino compound		anti-arrhythmia drug
disulfiram
[no description available]		3.6120organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
valproic acid
Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem.		3.2310branched-chain fatty acid;
branched-chain saturated fatty acid		anticonvulsant;
antimanic drug;
EC 3.5.1.98 (histone deacetylase) inhibitor;
GABA agent;
neuroprotective agent;
psychotropic drug;
teratogenic agent
domperidone
Domperidone: A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.. domperidone : 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used as an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet preparations.		2.4620benzimidazoles;
heteroarylpiperidine		antiemetic;
dopaminergic antagonist
donepezil
Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.		3.9330aromatic ether;
indanones;
piperidines;
racemate		EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent
doxapram
Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering.		3.2310morpholines;
pyrrolidin-2-ones		central nervous system stimulant
doxazosin
Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.		7.4853aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines		alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent
doxepin
Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug.		3.6120dibenzooxepine;
tertiary amino compound		antidepressant
doxylamine
Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM.		3.2310pyridines;
tertiary amine		anti-allergic agent;
antiemetic;
antitussive;
cholinergic antagonist;
H1-receptor antagonist;
histamine antagonist;
sedative
droperidol
Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon.		3.5820aromatic ketone;
benzimidazoles;
organofluorine compound		anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic
dyphylline
Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs.		3.2310oxopurine;
propane-1,2-diols		bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
muscle relaxant;
vasodilator agent
e 4031
E 4031: class III anti-arrhythmia agent; structure given in UD		2.0410sulfonamide
ebastine
[no description available]		2.0810organic molecular entity
edrophonium
Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.		3.2310phenols;
quaternary ammonium ion		antidote;
diagnostic agent;
EC 3.1.1.8 (cholinesterase) inhibitor
enoxacin
Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea.		2.08101,8-naphthyridine derivative;
amino acid;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-arylpiperazine;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor
estazolam
Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.		3.2310triazoles;
triazolobenzodiazepine		anticonvulsant;
anxiolytic drug;
GABA modulator
etazolate
Etazolate: A potent phosphodiesterase inhibitor proposed as an antipsychotic agent.. etazolate : A pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties.		3.2710ethyl ester;
hydrazone;
pyrazolopyridine		alpha-secretase activator;
antidepressant;
antipsychotic agent;
anxiolytic drug;
GABA agent;
neuroprotective agent;
phosphodiesterase IV inhibitor
ethacrynic acid
Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor.		3.6120aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid		EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic
ethosuximide
Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures.		3.6120dicarboximide;
pyrrolidinone		anticonvulsant;
geroprotector;
T-type calcium channel blocker
ethotoin
ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective.		3.2310imidazolidine-2,4-dioneanticonvulsant
etidronate
Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces.		3.23101,1-bis(phosphonic acid)antineoplastic agent;
bone density conservation agent;
chelator
etodolac
Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active.		3.2310monocarboxylic acid;
organic heterotricyclic compound		antipyretic;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
brl 42810
[no description available]		3.61202-aminopurines;
acetate ester		antiviral drug;
prodrug
felbamate
Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy.		3.2310carbamate esteranticonvulsant;
neuroprotective agent
4-biphenylylacetic acid
biphenyl-4-ylacetic acid : A monocarboxylic acid in which one of the alpha-hydrogens is substituted by a biphenyl-4-yl group. An active metabolite of fenbufen, it is used as a topical medicine to treat muscle inflammation and arthritis.		2.0810biphenyls;
monocarboxylic acid		non-steroidal anti-inflammatory drug
felodipine
Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris.		3.6120dichlorobenzene;
dihydropyridine;
ethyl ester;
methyl ester		anti-arrhythmia drug;
antihypertensive agent;
calcium channel blocker;
vasodilator agent
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		3.8630aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
fenoldopam
Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.		3.2310benzazepinealpha-adrenergic agonist;
antihypertensive agent;
dopamine agonist;
dopaminergic antagonist;
vasodilator agent
fenoprofen
Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding.		3.2310monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
fexofenadine
fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound.		3.2310piperidines;
tertiary amine		anti-allergic agent;
H1-receptor antagonist
fipexide
fipexide: regulates dopaminergic systems at macromolecular level		3.2310benzodioxoles
flavoxate
Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol.		3.2310carboxylic ester;
flavones;
piperidines;
tertiary amino compound		antispasmodic drug;
muscarinic antagonist;
parasympatholytic
flecainide
Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart).		3.6120aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines		anti-arrhythmia drug
fleroxacin
Fleroxacin: A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE.. fleroxacin : A fluoroquinolone antibiotic that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6, 7 and 8 by 2-fluoroethyl, carboxy, fluoro, 4-methylpiperazin-1-yl and fluoro groups, respectively. It is active against many Gram-positive and Gram-negative bacteria.		2.0810difluorobenzene;
fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
quinolines		antibacterial drug;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
fluconazole
Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis.		9.1240conazole antifungal drug;
difluorobenzene;
tertiary alcohol;
triazole antifungal drug		environmental contaminant;
P450 inhibitor;
xenobiotic
flucytosine
Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections.		3.6120aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone		prodrug
fluphenazine
[no description available]		3.2310N-alkylpiperazine;
organofluorine compound;
phenothiazines		anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug
flumazenil
Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose.		3.6120ethyl ester;
imidazobenzodiazepine;
organofluorine compound		antidote to benzodiazepine poisoning;
GABA antagonist
fluorescite
fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer.		3.6120benzoic acids;
cyclic ketone;
hydroxy monocarboxylic acid;
organic heterotricyclic compound;
phenols;
xanthene dye		fluorescent dye;
radioopaque medium
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		3.6120nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
fluoxetine
Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group.		10.6451(trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound
flurazepam
Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia.		3.23101,4-benzodiazepinone;
monofluorobenzenes;
organochlorine compound;
tertiary amino compound		anticonvulsant;
anxiolytic drug;
GABAA receptor agonist;
sedative
flurbiprofen
Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain.		3.2310fluorobiphenyl;
monocarboxylic acid		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
flutamide
Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species.		3.8930(trifluoromethyl)benzenes;
monocarboxylic acid amide		androgen antagonist;
antineoplastic agent
fomepizole
Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4.		3.2310pyrazolesantidote;
EC 1.1.1.1 (alcohol dehydrogenase) inhibitor;
protective agent
foscarnet
Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		3.2310carboxylic acid;
one-carbon compound;
phosphonic acids		antiviral drug;
geroprotector;
HIV-1 reverse transcriptase inhibitor;
sodium-dependent Pi-transporter inhibitor
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		8.9430chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
gabapentin
Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.		4.1520gamma-amino acidanticonvulsant;
calcium channel blocker;
environmental contaminant;
xenobiotic
vanoxerine
vanoxerine: structure given in first source. vanoxerine : An N-alkylpiperazine that consists of piperazine bearing 2-bis(4-fluorophenyl)methoxy]ethyl and 3-phenylpropyl groups at positions 1 and 4 respectively. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration.		3.2310ether;
N-alkylpiperazine;
organofluorine compound;
tertiary amino compound		dopamine uptake inhibitor
gemfibrozil
[no description available]		3.8630aromatic etherantilipemic drug
glafenine
Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market.		3.2310aminoquinoline;
carboxylic ester;
glycol;
organochlorine compound;
secondary amino compound		inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gliclazide
Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.		2.0810N-sulfonylureahypoglycemic agent;
insulin secretagogue;
radical scavenger
glimepiride
glimepiride: structure given in first source		3.6120sulfonamide
glipizide
Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus.		3.6120aromatic amide;
monocarboxylic acid amide;
N-sulfonylurea;
pyrazines		EC 2.7.1.33 (pantothenate kinase) inhibitor;
hypoglycemic agent;
insulin secretagogue
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		4.1140monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester
[no description available]		3.2310benzenes
go 6976
[no description available]		2.0310indolocarbazole;
organic heterohexacyclic compound		EC 2.7.11.13 (protein kinase C) inhibitor
granisetron
[no description available]		3.6120aromatic amide;
indazoles
guaifenesin
Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations.		3.2310methoxybenzenes
guanethidine
Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid.		3.2310azocanes;
guanidines		adrenergic antagonist;
antihypertensive agent;
sympatholytic agent
guanfacine
Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.		3.6120acetamides
guanidine
Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines.		3.2310carboxamidine;
guanidines;
one-carbon compound
haloperidol
Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.		4.0940aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol		antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist
hydralazine
Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent.		3.2310azaarene;
hydrazines;
ortho-fused heteroarene;
phthalazines		antihypertensive agent;
vasodilator agent
hydrochlorothiazide
Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure.		3.6120benzothiadiazine;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
hydroflumethiazide
Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide.		3.6120benzothiadiazine;
thiazide		antihypertensive agent;
diuretic
hydroxychloroquine
Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.		4.2420aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug
hydroxyurea
[no description available]		3.6120one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
hydroxyzine
Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively.		3.2310hydroxyether;
monochlorobenzenes;
N-alkylpiperazine		anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		3.2310monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
phenelzine
Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC.		3.2310primary amine
lidocaine
Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline.		10.4941benzenes;
monocarboxylic acid amide;
tertiary amino compound		anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic
ifosfamide
[no description available]		3.6120ifosfamidesalkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		4.1440dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
amrinone
Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure.		3.6120bipyridinesEC 3.1.4.* (phosphoric diester hydrolase) inhibitor
indapamide
Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine.		3.6120indoles;
organochlorine compound;
sulfonamide		antihypertensive agent;
diuretic
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		4.3850aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
iohexol
Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position.		2.0810benzenedicarboxamide;
organoiodine compound		environmental contaminant;
radioopaque medium;
xenobiotic
ioversol
[no description available]		3.2310amidobenzoic acid
iproniazid
[no description available]		3.6120carbohydrazide;
pyridines
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		3.6120azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
1-methyl-3-isobutylxanthine
1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES. 3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively.		3.53203-isobutyl-1-methylxanthine
isocarboxazid
Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311)		3.2310benzenes
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		3.6120carbohydrazideantitubercular agent;
drug allergen
isoproterenol
Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.		3.8430catechols;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
isoxsuprine
Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.		3.2310alkylbenzene
isradipine
Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.		3.6120benzoxadiazole;
dihydropyridine;
isopropyl ester;
methyl ester
itraconazole
[no description available]		3.8930piperazines
ketamine
Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.		3.8730cyclohexanones;
monochlorobenzenes;
secondary amino compound		analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic
ketanserin
Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group.		2.4920aromatic ketone;
organofluorine compound;
piperidines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		3.8630dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
ketoprofen
Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2.		10.0821benzophenones;
oxo monocarboxylic acid		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
ketorolac
Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively.		3.2310amino acid;
aromatic ketone;
monocarboxylic acid;
pyrrolizines;
racemate		analgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
labetalol
Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5.		3.2310benzamides;
benzenes;
phenols;
primary carboxamide;
salicylamides;
secondary alcohol;
secondary amino compound
lamotrigine
[no description available]		3.87301,2,4-triazines;
dichlorobenzene;
primary arylamine		anticonvulsant;
antidepressant;
antimanic drug;
calcium channel blocker;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
excitatory amino acid antagonist;
geroprotector;
non-narcotic analgesic;
xenobiotic
lansoprazole
Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.		3.8930benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
beta-lapachone
beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities.		2.0310benzochromenone;
orthoquinones		anti-inflammatory agent;
antineoplastic agent;
plant metabolite
leflunomide
Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide.		3.6120(trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide		antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor
letrozole
[no description available]		3.8630nitrile;
triazoles		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor
lofepramine
Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.		2.0810aromatic ketone;
dibenzoazepine;
monochlorobenzenes;
tertiary amino compound		antidepressant
lomefloxacin
lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery.		3.2310fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antimicrobial agent;
antitubercular agent;
photosensitizing agent
lomustine
[no description available]		3.6120N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
loperamide
Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.		3.2310monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol		anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist
loratadine
Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.		3.9430benzocycloheptapyridine;
ethyl ester;
N-acylpiperidine;
organochlorine compound;
tertiary carboxamide		anti-allergic agent;
cholinergic antagonist;
geroprotector;
H1-receptor antagonist
lorazepam
Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent.		3.2310benzodiazepine
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		3.2310biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
loxapine
Loxapine: An antipsychotic agent used in SCHIZOPHRENIA.		3.6120dibenzooxazepineantipsychotic agent;
dopaminergic antagonist
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		2.0310chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
6-anilino-5,8-quinolinedione
6-anilino-5,8-quinolinedione: structure given in first source; SRS-A & guanylate cyclase antagonist. 6-anilino-5,8-quinolinedione : A quinolone that is quinoline-5,8-dione in which the hydrogen at position 6 is replaced by an anilino group.		2.0510aminoquinoline;
aromatic amine;
p-quinones;
quinolone		antineoplastic agent;
EC 4.6.1.2 (guanylate cyclase) inhibitor
maprotiline
Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.		3.8730anthracenes
mebendazole
Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5.		3.9130aromatic ketone;
benzimidazoles;
carbamate ester		antinematodal drug;
microtubule-destabilising agent;
tubulin modulator
mecamylamine
Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool.		3.2310primary aliphatic amine
mechlorethamine
nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.		3.2310nitrogen mustard;
organochlorine compound		alkylating agent
meclizine
Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.		3.2310diarylmethane
meclofenamic acid
Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.		3.2310aminobenzoic acid;
organochlorine compound;
secondary amino compound		analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		3.6120aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
memantine
[no description available]		4.1820adamantanes;
primary aliphatic amine		antidepressant;
antiparkinson drug;
dopaminergic agent;
neuroprotective agent;
NMDA receptor antagonist
mepenzolate
mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure		3.2310diarylmethane
meperidine
Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain.		3.5820ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound		antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
mephenytoin
Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism.		3.2310imidazolidine-2,4-dioneanticonvulsant
mepivacaine
Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic.		3.2310piperidinecarboxamidedrug allergen;
local anaesthetic
meprobamate
Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603)		3.2310organic molecular entity
mesalamine
Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position.		3.2310amino acid;
aromatic amine;
monocarboxylic acid;
monohydroxybenzoic acid;
phenols		non-steroidal anti-inflammatory drug
mesoridazine
Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group.		3.2310phenothiazines;
sulfoxide;
tertiary amino compound		dopaminergic antagonist;
first generation antipsychotic
metaproterenol
Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself.		3.2310aralkylamino compound;
phenylethanolamines;
resorcinols;
secondary alcohol;
secondary amino compound
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		4.6940guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
methacrylic acid
methacrylic acid: RN given refers to parent cpd. methacrylic acid : An alpha,beta-unsaturated monocarboxylic acid that is acrylic acid in which the hydrogen at position 2 is substituted by a methyl group.		2.0610alpha,beta-unsaturated monocarboxylic acid
methadone
Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.		3.2310benzenes;
diarylmethane;
ketone;
tertiary amino compound
methazolamide
Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.		3.2310sulfonamide;
thiadiazoles
methocarbamol
Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester.		3.2310aromatic ether;
carbamate ester;
secondary alcohol
methoxsalen
Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis.		3.2310aromatic ether;
psoralens		antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite
methyclothiazide
Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825)		3.2310benzothiadiazine
methylphenidate
Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group.		3.2310beta-amino acid ester;
methyl ester;
piperidines
metoclopramide
Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.		3.6120benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound		antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic
metolazone
Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics.		3.2310organochlorine compound;
quinazolines;
sulfonamide		antihypertensive agent;
diuretic;
ion transport inhibitor
metoprolol
Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1.		5.4841aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound		antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		3.6120C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
metyrapone
Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency.		3.2310aromatic ketoneantimetabolite;
diagnostic agent;
EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor
mexiletine
Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol.		3.6120aromatic ether;
primary amino compound		anti-arrhythmia drug
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		11.3762imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
midodrine
Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine.		3.2310amino acid amide;
aromatic ether;
secondary alcohol		alpha-adrenergic agonist;
prodrug;
sympathomimetic agent;
vasoconstrictor agent
milrinone
[no description available]		4.3530bipyridines;
nitrile;
pyridone		cardiotonic drug;
EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent
minoxidil
Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6.		3.6120dialkylarylamine;
tertiary amino compound
mirtazapine
Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders.		3.6120benzazepine;
tetracyclic antidepressant		alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist
mitotane
Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.		3.2310diarylmethane
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		3.2310dihydroxyanthraquinoneanalgesic;
antineoplastic agent
moclobemide
Moclobemide: A reversible inhibitor of monoamine oxidase type A; (RIMA); (see MONOAMINE OXIDASE INHIBITORS) that has antidepressive properties.. moclobemide : A member of the class of benzamides that is benzamide substituted by a chloro group at position 4 and a 2-(morpholin-4-yl)ethyl group at the nitrogen atom. It acts as a reversible monoamine oxidase inhibitor and is used in the treatment of depression.		2.0810benzamides;
monochlorobenzenes;
morpholines		antidepressant;
environmental contaminant;
xenobiotic
modafinil
Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.		3.2310monocarboxylic acid amide;
sulfoxide
moxisylyte
Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312)		3.2310monoterpenoid
acecainide
Acecainide: A major metabolite of PROCAINAMIDE. Its anti-arrhythmic action may cause cardiac toxicity in kidney failure.. N-acetylprocainamide : A benzamide obtained via formal condensation of 4-acetamidobenzoic acid and 2-(diethylamino)ethylamine.		2.0810acetamides;
benzamides		anti-arrhythmia drug
nabumetone
Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs.		3.2310methoxynaphthalene;
methyl ketone		cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
nadolol
[no description available]		3.6120tetralins
naftopidil
[no description available]		7.5820piperazines
nalidixic acid
[no description available]		3.89301,8-naphthyridine derivative;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
DNA synthesis inhibitor
naratriptan
naratriptan: structure given in first source		3.2310heteroarylpiperidine;
sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
nefazodone
nefazodone: may be useful as an opiate adjunct		3.8930aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles		alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor
nefopam
Nefopam: Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26). nefopam : A racemate comprising equal amounts of (R)- and (S)-nefopam. The hydrochloride is a centrally acting non-opiate analgesic commonly used for the treatment of moderate to severe pain.. 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine : A member of the class of benzoxazocines that is 3,4,5,6-tetrahydro-1H-2,5-benzoxazocine substituted by phenyl and methyl groups at positions 1 and 5 respectively.		2.0810benzoxazocine;
tertiary amino compound
neostigmine
Neostigmine: A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.. neostigmine : A quaternary ammonium ion comprising an anilinium ion core having three methyl substituents on the aniline nitrogen, and a 3-[(dimethylcarbamoyl)oxy] substituent at position 3. It is a parasympathomimetic which acts as a reversible acetylcholinesterase inhibitor.		2.0810quaternary ammonium ionantidote to curare poisoning;
EC 3.1.1.7 (acetylcholinesterase) inhibitor
nevirapine
Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection.		3.6120cyclopropanes;
dipyridodiazepine		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nialamide
Nialamide: An MAO inhibitor that is used as an antidepressive agent.		3.2310organonitrogen compound;
organooxygen compound
nicardipine
Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively.		3.6120benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound
niclosamide
Niclosamide: An antihelmintic that is active against most tapeworms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p48). niclosamide : A secondary carboxamide resulting from the formal condensation of the carboxy group of 5-chlorosalicylic acid with the amino group of 2-chloro-4-nitroaniline. It is an oral anthelmintic drug approved for use against tapeworm infections.		2.0310benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide		anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor
nifedipine
Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.		5.1950C-nitro compound;
dihydropyridine;
methyl ester		calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent
nilutamide
[no description available]		3.2310(trifluoromethyl)benzenes;
C-nitro compound;
imidazolidinone		androgen antagonist;
antineoplastic agent
nimesulide
nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.		3.6120aromatic ether;
C-nitro compound;
sulfonamide		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
nimodipine
Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm.		8.95302-methoxyethyl ester;
C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
isopropyl ester		antihypertensive agent;
calcium channel blocker;
cardiovascular drug;
vasodilator agent
nisoldipine
Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris.		3.6120C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
methyl ester
nisoxetine
nisoxetine: potent inhibitor for norepinephrine uptake into rat brain synaptosomes & brain; NM refers to (+-)-isomer; RN given refers to parent cpd; structure. nisoxetine : A secondary amino compound that is N-methyl-3-phenylpropan-1-amine substituted at position 3 by a 2-methoxyphenoxy group.		2.0410aromatic ether;
secondary amino compound		adrenergic uptake inhibitor;
antidepressant
nitrazepam
Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome).		2.08101,4-benzodiazepinone;
C-nitro compound		anticonvulsant;
antispasmodic drug;
drug metabolite;
GABA modulator;
sedative
nitrendipine
Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension.		3.8521C-nitro compound;
dicarboxylic acids and O-substituted derivatives;
diester;
dihydropyridine;
ethyl ester;
methyl ester		antihypertensive agent;
calcium channel blocker;
geroprotector;
vasodilator agent
nitroglycerin
Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain.		7.1381nitroglycerolexplosive;
muscle relaxant;
nitric oxide donor;
prodrug;
tocolytic agent;
vasodilator agent;
xenobiotic
nizatidine
[no description available]		3.23101,3-thiazoles;
C-nitro compound;
carboxamidine;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
cholinergic drug;
H2-receptor antagonist
nomifensine
Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.		3.2310isoquinolinesdopamine uptake inhibitor
norfloxacin
Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase.		3.6120fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug;
DNA synthesis inhibitor;
environmental contaminant;
xenobiotic
nortriptyline
Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline.		3.8930organic tricyclic compound;
secondary amine		adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite
ns 1619
NS 1619: structure given in first source. NS 1619 : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca).		2.0810(trifluoromethyl)benzenes;
benzimidazoles;
phenols		potassium channel opener
ofloxacin
Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.		3.61203-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		3.8930aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
ondansetron
Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.		3.6120carbazoles
orphenadrine
Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol.		3.2310ether;
tertiary amino compound		antidyskinesia agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic
oxaprozin
Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis.		3.61201,3-oxazoles;
monocarboxylic acid		analgesic;
non-steroidal anti-inflammatory drug
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		3.23101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
oxybutynin
oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder.		3.930acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound		antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic
aminosalicylic acid
Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4.		3.2310aminobenzoic acid;
phenols		antitubercular agent
pamidronate
[no description available]		3.2310phosphonoacetic acid
pantoprazole
Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2.		3.6120aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic
papaverine
Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum.		6.4851benzylisoquinoline alkaloid;
dimethoxybenzene;
isoquinolines		antispasmodic drug;
vasodilator agent
patulin
Patulin: 4-Hydroxy-4H-furo(3,2-c)pyran-2(6H)-one. A mycotoxin produced by several species of Aspergillus and Penicillium. It is found in unfermented apple and grape juice and field crops. It has antibiotic properties and has been shown to be carcinogenic and mutagenic and causes chromosome damage in biological systems.. patulin : A furopyran and lactone that is (2H-pyran-3(6H)-ylidene)acetic acid which is substituted by hydroxy groups at positions 2 and 4 and in which the hydroxy group at position 4 has condensed with the carboxy group to give the corresponding bicyclic lactone. A mycotoxin produced by several species of Aspergillus and Penicillium, it has antibiotic properties but has been shown to be carcinogenic and mutagenic.		2.0310furopyran;
gamma-lactone;
lactol		antimicrobial agent;
Aspergillus metabolite;
carcinogenic agent;
mutagen;
mycotoxin;
Penicillium metabolite
pd 153035
4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline: structure given in first source. PD-153035 : A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.		2.0310aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
pd 158780
[no description available]		2.0310aromatic amine;
bromobenzenes;
diamine;
pyridopyrimidine;
secondary amino compound		antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
pd 98059
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one: inhibits MAP kinase kinase (MEK) activity, p42 MAPK and p44 MAPK; structure in first source. 2-(2-amino-3-methoxyphenyl)chromen-4-one : A member of the class of monomethoxyflavones that is 3'-methoxyflavone bearing an additional amino substituent at position 2'.		2.0310aromatic amine;
monomethoxyflavone		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector
pemoline
Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity.		3.61201,3-oxazolescentral nervous system stimulant
pentamidine
Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease.		3.6120aromatic ether;
carboxamidine;
diether		anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic
pentobarbital
Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		3.2310barbituratesGABAA receptor agonist
pentoxifylline
[no description available]		6.2191oxopurine
perhexiline
Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis.		3.2310piperidinescardiovascular drug
perphenazine
Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.		3.6120N-(2-hydroxyethyl)piperazine;
N-alkylpiperazine;
organochlorine compound;
phenothiazines		antiemetic;
dopaminergic antagonist;
phenothiazine antipsychotic drug
phenacetin
Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione		2.0810acetamides;
aromatic ether		cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		3.9130barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
phenoxybenzamine
Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator.		3.2310aromatic amine
phentermine
Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity.		3.2310primary amineadrenergic agent;
appetite depressant;
central nervous system drug;
central nervous system stimulant;
dopaminergic agent;
sympathomimetic agent
4-phenylbutyric acid
4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation.		3.2310monocarboxylic acidantineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug
pilsicainide
pilsicainide: structure given in first source. pilsicainide : A secondary carboxamide resulting from the formal condensation of the amino group of 2,6-dimethylaniline with the carboxy group of (tetrahydro-1H-pyrrolizin-7a(5H)-yl)acetic acid. It is a sodium channel blocker which is used as an antiarrhythmic drug for the management of atrial tachyarrhythmias in Japan.		2.0410organic heterobicyclic compound;
secondary carboxamide		anti-arrhythmia drug;
sodium channel blocker
pinacidil
Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)		3.1110pyridines
pindolol
Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.		3.6120indoles;
secondary amine		antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist;
serotonergic antagonist;
vasodilator agent
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		4.0940aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
piracetam
Piracetam: A compound suggested to be both a nootropic and a neuroprotective agent.		2.5120organonitrogen compound;
organooxygen compound
pirenperone
[no description available]		2.0410aromatic ketone
piribedil
Piribedil: A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist.		2.0810N-arylpiperazine
polythiazide
[no description available]		3.2310benzothiadiazine
potassium chloride
Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.		4.4330inorganic chloride;
inorganic potassium salt;
potassium salt		fertilizer
duodote
duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents		3.2310pyridinium ionantidote to organophosphate poisoning;
antidote to sarin poisoning;
cholinergic drug;
cholinesterase reactivator
ono 1078
pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist		2.0810chromones
pyranoprofen
pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source		2.0810pyridochromene
praziquantel
azinox: Russian drug		3.8930isoquinolines
prazosin
Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.		3.6120aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		3.6120aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
primidone
Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures.		3.6120pyrimidoneanticonvulsant;
environmental contaminant;
xenobiotic
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		3.6120benzoic acids;
sulfonamide		uricosuric drug
procainamide
Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias.		3.6120benzamidesanti-arrhythmia drug;
platelet aggregation inhibitor;
sodium channel blocker
procarbazine
Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		3.2310benzamides;
hydrazines		antineoplastic agent
prochlorperazine
Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.		3.6120N-alkylpiperazine;
N-methylpiperazine;
organochlorine compound;
phenothiazines		alpha-adrenergic antagonist;
antiemetic;
cholinergic antagonist;
dopamine receptor D2 antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic
procyclidine
Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3.		3.6120pyrrolidines;
tertiary alcohol		antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist
promethazine
Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety.		3.6120phenothiazines;
tertiary amine		anti-allergic agent;
anticoronaviral agent;
antiemetic;
antipruritic drug;
H1-receptor antagonist;
local anaesthetic;
sedative
propafenone
Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias.		4.1440aromatic ketone;
secondary alcohol;
secondary amino compound		anti-arrhythmia drug
propantheline
Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.		3.2310xanthenes
propofol
Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.		3.2310phenolsanticonvulsant;
antiemetic;
intravenous anaesthetic;
radical scavenger;
sedative
propranolol
Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3.		4.5870naphthalenes;
propanolamine;
secondary amine		anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic
protriptyline
Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation.		3.2310carbotricyclic compoundantidepressant
pyridostigmine
[no description available]		3.2310pyridinium ion
pyrimethamine
Maloprim: contains above 2 cpds		3.2310aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sch 16134
quazepam: structure given in first source		3.2310benzodiazepine
quetiapine
[no description available]		3.8630dibenzothiazepine;
N-alkylpiperazine;
N-arylpiperazine		adrenergic antagonist;
dopaminergic antagonist;
histamine antagonist;
second generation antipsychotic;
serotonergic antagonist
rabeprazole
Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.		3.2310benzimidazoles;
pyridines;
sulfoxide		anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
raloxifene
raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively.		3.57201-benzothiophenes;
aromatic ketone;
N-oxyethylpiperidine;
phenols		bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
ranitidine
[no description available]		2.0810aralkylamine
riluzole
Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.		3.6120benzothiazoles
rimantadine
Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza.		3.2310alkylamine
risperidone
Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.		4.09401,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist
ritanserin
Ritanserin: A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.. ritanserin : A thiazolopyrimidine that is 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one which is substituted at position 7 by a methyl group and at position 6 by a 2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl group. A potent and long-acting seratonin (5-hydroxytryptamine, 5-HT) antagonist of the subtype 5-HT2 (Ki = 0.39 nM), it is used in the treatment of a variety of disorders including anxiety, depression and schizophrenia. It has little sedative action.		2.0410organofluorine compound;
piperidines;
thiazolopyrimidine		antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist
rizatriptan
rizatriptan: structure given in first source; RN given refers to benzoate		3.2310tryptaminesanti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rofecoxib
[no description available]		2.4620butenolide;
sulfone		analgesic;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
rolipram
[no description available]		5.470pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
ropinirole
[no description available]		3.2310indolones;
tertiary amine		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
dopamine agonist
salicylsalicylic acid
salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes.		3.2310benzoate ester;
benzoic acids;
phenols;
salicylates		antineoplastic agent;
antirheumatic drug;
EC 3.5.2.6 (beta-lactamase) inhibitor;
hypoglycemic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
secobarbital
Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups.		3.2310barbituratesanaesthesia adjuvant;
GABA modulator;
sedative
sibutramine
sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride		8.8730organochlorine compound;
tertiary amino compound		anti-obesity agent;
serotonin uptake inhibitor
sulfadiazine
Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines.		3.6120pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
antimicrobial agent;
antiprotozoal drug;
coccidiostat;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
risedronic acid
Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION.		3.2310pyridines
sotalol
Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.		4.1240ethanolamines;
secondary alcohol;
secondary amino compound;
sulfonamide		anti-arrhythmia drug;
beta-adrenergic antagonist;
environmental contaminant;
xenobiotic
spiperone
Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.		2.0410aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound		alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist
imatinib
[no description available]		3.8630aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		4.1440dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
succinylcholine
Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid.		3.2310quaternary ammonium ion;
succinate ester		drug allergen;
muscle relaxant;
neuromuscular agent
sulfamethizole
Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2.		3.2310sulfonamide antibiotic;
sulfonamide;
thiadiazoles		antiinfective agent;
antimicrobial agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor
sulfamethoxazole
Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position.		2.0810isoxazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial agent;
antiinfective agent;
antimicrobial agent;
drug allergen;
EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
epitope;
P450 inhibitor;
xenobiotic
sulfanitran
[no description available]		2.0810sulfonamide
sulfasalazine
Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position.		3.6120
sulfathiazole
Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position.		3.23101,3-thiazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antiinfective agent;
drug allergen;
EC 2.5.1.15 (dihydropteroate synthase) inhibitor;
environmental contaminant;
xenobiotic
sulfisoxazole
Sulfisoxazole: A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms.. sulfisoxazole : A sulfonamide antibacterial with an oxazole substituent. It has antibiotic activity against a wide range of gram-negative and gram-positive organisms.		2.0810isoxazoles;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
drug allergen
2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol
[no description available]		3.2310alkylbenzene
sumatriptan
Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults.		3.6120sulfonamide;
tryptamines		serotonergic agonist;
vasoconstrictor agent
gatifloxacin
Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.		2.0810N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
tazarotene
tazarotene: a topical acetylenic retinoid; a topical kerytolytic. tazarotene : The ethyl ester of tazarotenic acid. A prodrug for tazarotenic acid, it is used for the treatment of psoriasis, acne, and sun-damaged skin.		2.0810acetylenic compound;
ethyl ester;
pyridines;
retinoid;
thiochromane		keratolytic drug;
prodrug;
teratogenic agent
temazepam
Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent.		3.2310benzodiazepine
temozolomide
[no description available]		3.6120imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
terazosin
Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia		3.6120furans;
piperazines;
primary amino compound;
quinazolines		alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent
terbutaline
Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group.		3.6120phenylethanolamines;
resorcinols		anti-asthmatic drug;
beta-adrenergic agonist;
bronchodilator agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hypoglycemic agent;
sympathomimetic agent;
tocolytic agent
terfenadine
Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME.		340diarylmethane
tetracaine
Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia.. tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia.		2.0410benzoate ester;
tertiary amino compound		local anaesthetic
thalidomide
Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group.		3.8630phthalimides;
piperidones
thiabendazole
Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate		3.23101,3-thiazoles;
benzimidazole fungicide;
benzimidazoles		antifungal agrochemical;
antinematodal drug
thioridazine
Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position.		3.2310phenothiazines;
piperidines		alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
thiotepa
Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed).		3.6120aziridines
tiapride
[no description available]		2.0810benzamides
ticlopidine
Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group.		3.2310monochlorobenzenes;
thienopyridine		anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
tilorone
Tilorone: An antiviral agent used as its hydrochloride. It is the first recognized synthetic, low-molecular-weight compound that is an orally active interferon inducer, and is also reported to have antineoplastic and anti-inflammatory actions.. tilorone : A member of the class of fluoren-9-ones that is 9H-fluoren-9-one which is substituted by a 2-(diethylamino)ethoxy group at positions 2 and 7. It is an interferon inducer and a selective alpha7 nicotinic acetylcholine receptor (alpha7 nAChR) agonist. Its hydrochloride salt is used as an antiviral drug.		2.0810aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound		anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist
tinidazole
Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent.		3.6120imidazolesantiamoebic agent;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
tiopronin
Tiopronin: Sulfhydryl acylated derivative of GLYCINE.		3.2310N-acyl-amino acid
tizanidine
tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites.		3.6120benzothiadiazole;
imidazoles		alpha-adrenergic agonist;
muscle relaxant
nikethamide
Nikethamide: A central nervous system stimulant. It was formerly used in the treatment of barbiturate overdose but is now considered to be of no value for such purposes and may be dangerous. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1229)		2.0810pyridinecarboxamide
tolazamide
Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.		3.2310N-sulfonylureahypoglycemic agent;
potassium channel blocker
tolbutamide
Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position.		3.6120N-sulfonylureahuman metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker
tolmetin
Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug.		3.2310aromatic ketone;
monocarboxylic acid;
pyrroles		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
tolnaftate
[no description available]		2.0810monothiocarbamic esterantifungal drug
ultram
2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively.		3.6120aromatic ether;
tertiary alcohol;
tertiary amino compound
tranexamic acid
Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage.		3.2310amino acid
trazodone
Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.		3.6120monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine		adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
triamterene
Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema.		3.6120pteridinesdiuretic;
sodium channel blocker
triazolam
Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries.		3.2310triazolobenzodiazepinesedative
trifluoperazine
[no description available]		3.2310N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines		antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug
trifluperidol
Trifluperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in the treatment of PSYCHOSES including MANIA and SCHIZOPHRENIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p621)		2.0410aromatic ketone
trihexyphenidyl
Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic.		3.2310amine
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		3.2310oxazolidinoneanticonvulsant;
geroprotector
trimethobenzamide
trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans.		3.2310benzamides;
tertiary amino compound		antiemetic
trimethoprim
Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.		3.6120aminopyrimidine;
methoxybenzenes		antibacterial drug;
diuretic;
drug allergen;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
environmental contaminant;
xenobiotic
trimetrexate
Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect.		3.2310
trimipramine
Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant.		3.2310dibenzoazepine;
tertiary amino compound		antidepressant;
environmental contaminant;
xenobiotic
troglitazone
Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity.		3.8630chromanes;
thiazolidinone		anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent
thenoyltrifluoroacetone
Thenoyltrifluoroacetone: Chelating agent and inhibitor of cellular respiration.		2.0810
tyramine
[no description available]		3.2310monoamine molecular messenger;
primary amino compound;
tyramines		EC 3.1.1.8 (cholinesterase) inhibitor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
neurotransmitter
delavirdine
Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.		3.2310aminopyridine;
indolecarboxamide;
N-acylpiperazine;
sulfonamide		antiviral drug;
HIV-1 reverse transcriptase inhibitor
undecylenic acid
undecylenic acid: a fatty acid with a terminal double bond. 10-undecenoic acid : An undecenoic acid having its double bond in the 10-position. It is derived from castor oil and is used for the treatment of skin problems.. undecenoic acid : A C11, straight-chain fatty acid carrying a C=C double bond at any position.		2.0810undecenoic acidantifungal drug;
plant metabolite
urapidil
[no description available]		2.0810piperazines
venlafaxine
venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.		4.140cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound		adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic
vigabatrin
[no description available]		3.6120gamma-amino acidanticonvulsant;
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor
pirinixic acid
pirinixic acid: structure		2.0810aryl sulfide;
organochlorine compound;
pyrimidines
ici 204,219
zafirlukast: a leukotriene D4 receptor antagonist		3.6120carbamate ester;
indoles;
N-sulfonylcarboxamide		anti-asthmatic agent;
leukotriene antagonist
zaleplon
zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position.		3.6120nitrile;
pyrazolopyrimidine		anticonvulsant;
anxiolytic drug;
central nervous system depressant;
sedative
zardaverine
zardaverine: structure given in first source. zardaverine : A pyridazinone derivative in which pyridazin-3(2H)-one is substituted at C-6 with a 4-(difluoromethoxy)-3-methoxyphenyl group. It is a phosphodiesterase inhibitor, selective for PDE3 and 4.		2.0210organofluorine compound;
pyridazinone		anti-asthmatic drug;
bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
peripheral nervous system drug
zm 336372
N-(5-(3-dimethylaminobenzamido)-2-methylphenyl)-4-hydroxybenzamide: an inhibitor of c-Raf; activates Raf-1; structure in first source		2.0310benzamides
zolpidem
Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.		3.2310imidazopyridinecentral nervous system depressant;
GABA agonist;
sedative
zonisamide
Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position.		3.86301,2-benzoxazoles;
sulfonamide		anticonvulsant;
antioxidant;
central nervous system drug;
protective agent;
T-type calcium channel blocker
zopiclone
zopiclone: S(+)-enantiomer of racemic zopiclone; azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position.		2.0810monochloropyridine;
pyrrolopyrazine		central nervous system depressant;
sedative
cortisone acetate
Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders.		3.2310corticosteroid hormone
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		3.2310mitomycinalkylating agent;
antineoplastic agent
corticosterone
[no description available]		3.481111beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone		human metabolite;
mouse metabolite
prednisolone
Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.		3.612011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic
reserpine
Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria.		3.6120alkaloid ester;
methyl ester;
yohimban alkaloid		adrenergic uptake inhibitor;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
first generation antipsychotic;
plant metabolite;
xenobiotic
phentolamine
Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.		4.6830imidazoles;
phenols;
substituted aniline;
tertiary amino compound		alpha-adrenergic antagonist;
vasodilator agent
sorbitol
D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol).		3.2310glucitolcathartic;
Escherichia coli metabolite;
food humectant;
human metabolite;
laxative;
metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite;
sweetening agent
hydroxyproline
Hydroxyproline: A hydroxylated form of the imino acid proline. A deficiency in ASCORBIC ACID can result in impaired hydroxyproline formation.. hydroxyproline : A proline derivative that is proline substituted by at least one hydroxy group.		2.17104-hydroxyproline;
L-alpha-amino acid zwitterion		human metabolite;
mouse metabolite;
plant metabolite
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		3.63202-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
dextroamphetamine
Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.		3.23101-phenylpropan-2-amineadrenergic agent;
adrenergic uptake inhibitor;
dopamine uptake inhibitor;
dopaminergic agent;
neurotoxin;
sympathomimetic agent
carbachol
Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.		2.7630ammonium salt;
carbamate ester		cardiotonic drug;
miotic;
muscarinic agonist;
nicotinic acetylcholine receptor agonist;
non-narcotic analgesic
spironolactone
Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7.		3.23103-oxo-Delta(4) steroid;
oxaspiro compound;
steroid lactone;
thioester		aldosterone antagonist;
antihypertensive agent;
diuretic;
environmental contaminant;
xenobiotic
penicillamine
Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group.		3.6120non-proteinogenic alpha-amino acid;
penicillamine		antirheumatic drug;
chelator;
copper chelator;
drug allergen
cysteine
[no description available]		3.2310cysteine zwitterion;
cysteine;
L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid		EC 4.3.1.3 (histidine ammonia-lyase) inhibitor;
flour treatment agent;
human metabolite
tetrahydrocortisol
[no description available]		3.481111beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3alpha-hydroxy steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
prednisone
Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid.		3.231011-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
tetrahydrocortisone
[no description available]		3.481121-hydroxy steroid
estrone
Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens.		3.231017-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols		antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
methylprednisolone acetate
Methylprednisolone Acetate: Methylprednisolone derivative that is used as an anti-inflammatory agent for the treatment of ALLERGY and ALLERGIC RHINITIS; ASTHMA; and BURSITIS; and for the treatment of ADRENAL INSUFFICIENCY.. methylprednisolone acetate : An acetate ester resulting from the formal condensation of the 21-hydroxy function of 6alpha-methylprednisolone compound with acetic acid.		2.051011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
acetate ester;
glucocorticoid;
steroid ester;
tertiary alpha-hydroxy ketone		anti-inflammatory drug
oxandrolone
Oxandrolone: A synthetic hormone with anabolic and androgenic properties.		3.231017beta-hydroxy steroid;
3-oxo steroid;
anabolic androgenic steroid;
oxa-steroid		anabolic agent;
androgen
penicillin g
Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.		3.2310penicillin allergen;
penicillin		antibacterial drug;
drug allergen;
epitope
pilocarpine
Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.		3.2310pilocarpineantiglaucoma drug
pentylenetetrazole
Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis.		2.6920organic heterobicyclic compound;
organonitrogen heterocyclic compound
triiodothyronine
Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.		3.23102-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine		human metabolite;
mouse metabolite;
thyroid hormone
carbon tetrachloride
Carbon Tetrachloride: A solvent for oils, fats, lacquers, varnishes, rubber waxes, and resins, and a starting material in the manufacturing of organic compounds. Poisoning by inhalation, ingestion or skin absorption is possible and may be fatal. (Merck Index, 11th ed). tetrachloromethane : A chlorocarbon that is methane in which all the hydrogens have been replaced by chloro groups.		2.0810chlorocarbon;
chloromethanes		hepatotoxic agent;
refrigerant
chloramphenicol
Amphenicol: Chloramphenicol and its derivatives.		3.6120C-nitro compound;
carboxamide;
diol;
organochlorine compound		antibacterial drug;
antimicrobial agent;
Escherichia coli metabolite;
geroprotector;
Mycoplasma genitalium metabolite;
protein synthesis inhibitor
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		3.8830amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
vincristine
[no description available]		3.2310acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
physostigmine
Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity.		3.2310carbamate ester;
indole alkaloid		antidote to curare poisoning;
EC 3.1.1.8 (cholinesterase) inhibitor;
miotic
ethinyl estradiol
Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration.		2.081017-hydroxy steroid;
3-hydroxy steroid;
terminal acetylenic compound		xenoestrogen
tubocurarine
Tubocurarine: A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.. tubocurarine : A benzylisoquinoline alkaloid muscle relaxant which constitutes the active component of curare.. isoquinoline alkaloid : Any alkaloid that has a structure based on an isoquinoline nucleus. They are derived from the amino acids like tyrosine and phenylalanine.		2.0810bisbenzylisoquinoline alkaloiddrug allergen;
muscle relaxant;
nicotinic antagonist
apomorphine
Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.		6.45100aporphine alkaloidalpha-adrenergic drug;
antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
emetic;
serotonergic drug
methyltestosterone
Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position.		3.231017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
enone		anabolic agent;
androgen;
antineoplastic agent
tetrabenazine
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7.		3.2310benzoquinolizine;
cyclic ketone;
tertiary amino compound
kanamycin a
Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components.		3.6120kanamycinsbacterial metabolite
bromodeoxyuridine
Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors.		2.4620pyrimidine 2'-deoxyribonucleosideantimetabolite;
antineoplastic agent
phenylephrine
Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.		2.7530phenols;
phenylethanolamines;
secondary amino compound		alpha-adrenergic agonist;
cardiotonic drug;
mydriatic agent;
nasal decongestant;
protective agent;
sympathomimetic agent;
vasoconstrictor agent
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		2.0810amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
edetic acid
Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.		3.2310ethylenediamine derivative;
polyamino carboxylic acid;
tetracarboxylic acid		anticoagulant;
antidote;
chelator;
copper chelator;
geroprotector
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.0310amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
cysteamine
Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2.		3.2310amine;
thiol		geroprotector;
human metabolite;
mouse metabolite;
radiation protective agent
acetylcholine chloride
acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug.		3.2310quaternary ammonium salt
mepazine
mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position.		3.2310phenothiazines
papaverine hydrochloride
[no description available]		3.5110
cloxacillin
Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6.		3.2310penicillin allergen;
penicillin;
semisynthetic derivative		antibacterial agent;
antibacterial drug
leucine
Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.		2.1710amino acid zwitterion;
L-alpha-amino acid;
leucine;
proteinogenic amino acid;
pyruvate family amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
calcium acetate
calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces.		3.2310calcium saltchelator
lactose
Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose.		2.0810lactose
methionine
Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4.		3.7120aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid		antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		3.6120alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
mebanazine
mebanazine: RN given refers to parent cpd without isomeric designation; structure		3.2310benzenes
oxacillin
Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.		3.2310penicillinantibacterial agent;
antibacterial drug
triamcinolone diacetate
triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone		2.0810corticosteroid hormone
cycloserine
Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis).		3.23104-amino-1,2-oxazolidin-3-one;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic;
zwitterion		antiinfective agent;
antimetabolite;
antitubercular agent;
metabolite;
NMDA receptor agonist
benziodarone
benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74)		3.2310aromatic ketone
ampicillin
Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.		3.2310beta-lactam antibiotic;
penicillin allergen;
penicillin		antibacterial drug
mannitol
[no description available]		3.2310mannitolallergen;
antiglaucoma drug;
compatible osmolytes;
Escherichia coli metabolite;
food anticaking agent;
food bulking agent;
food humectant;
food stabiliser;
food thickening agent;
hapten;
metabolite;
osmotic diuretic;
sweetening agent
cytarabine
[no description available]		3.6120beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
histidine
Histidine: An essential amino acid that is required for the production of HISTAMINE.. L-histidine : The L-enantiomer of the amino acid histidine.. histidine : An alpha-amino acid that is propanoic acid bearing an amino substituent at position 2 and a 1H-imidazol-4-yl group at position 3.		2.0310amino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
medroxyprogesterone acetate
[no description available]		2.081020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester		adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive
tryptophan
Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3.		2.1310erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan		antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		7.6693arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
acetonitrile
acetonitrile: RN given refers to unlabeled cpd. acetonitrile : A nitrile that is hydrogen cyanide in which the hydrogen has been replaced by a methyl group.		8.0140aliphatic nitrile;
volatile organic compound		EC 3.5.1.4 (amidase) inhibitor;
NMR chemical shift reference compound;
polar aprotic solvent
perflutren
Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines.		3.2310fluoroalkane;
fluorocarbon
triamcinolone acetonide
Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections.		2.081011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
cyclic ketal;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone		anti-allergic agent;
anti-inflammatory drug
fluoxymesterone
Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women.		3.231011beta-hydroxy steroid;
17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
anabolic androgenic steroid;
fluorinated steroid		anabolic agent;
antineoplastic agent
gibberellic acid
gibberellic acid: RN given refers to (1alpha,2beta,4aalpha,4bbeta,10beta)-isomer; structure. gibberellin A3 : A C19-gibberellin that is a pentacyclic diterpenoid responsible for promoting growth and elongation of cells in plants. Initially identified in Gibberella fujikuroi,it differs from gibberellin A1 in the presence of a double bond between C-3 and C-4.		2.0510C19-gibberellin;
gibberellin monocarboxylic acid;
lactone;
organic heteropentacyclic compound		mouse metabolite;
plant metabolite
methsuximide
methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation		3.2310organic molecular entity
tromethamine
Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)		5.0821primary amino compound;
triol		buffer
methylethyl ketone
methylethyl ketone: solvent; colorless synthetic resins, smokeless powders; may be irritating to eyes, mucous membranes; may be toxic in high concentrations; structure. butanone : Any ketone that is butane substituted by an oxo group at unspecified position.. butan-2-one : A dialkyl ketone that is a four-carbon ketone carrying a single keto- group at position C-2.		2.1110butanone;
dialkyl ketone;
methyl ketone;
volatile organic compound		bacterial metabolite;
polar aprotic solvent
acrylic acid
acrylic acid: RN given refers to parent cpd. acrylic acid : A alpha,beta-unsaturated monocarboxylic acid that is ethene substituted by a carboxy group.		2.0610alpha,beta-unsaturated monocarboxylic acidmetabolite
methylprednisolone
Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone.		4.13406-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic
rotenone
Derris: A plant genus of the family FABACEAE. The root is a source of rotenoids (ROTENONE) and flavonoids. Some species of Pongamia have been reclassified to this genus and some to MILLETTIA. Some species of Deguelia have been reclassified to this genus.. rotenoid : Members of the class of tetrahydrochromenochromene that consists of a cis-fused tetrahydrochromeno[3,4-b]chromene skeleton and its substituted derivatives. The term was originally restricted to natural products, but is now also used to describe semi-synthetic and fully synthetic compounds.		2.4620organic heteropentacyclic compound;
rotenones		antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin
brompheniramine
Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310organobromine compound;
pyridines		anti-allergic agent;
H1-receptor antagonist
penicillin v
Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain.		3.2310penicillin allergen;
penicillin
isosorbide dinitrate
Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action.		4.0720glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
n-vinyl-2-pyrrolidinone
N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source		2.8220pyrrolidin-2-ones
pseudoephedrine
Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group.		3.2310phenylethanolamines;
secondary alcohol;
secondary amino compound		anti-asthmatic drug;
bronchodilator agent;
central nervous system drug;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
diethylpropion
Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity.		3.6320aromatic ketone;
tertiary amine		appetite depressant
quinoxalines
quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.		3.1450mancude organic heterobicyclic parent;
naphthyridine;
ortho-fused heteroarene
quinuclidines
Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group.		3.4511quinuclidines;
saturated organic heterobicyclic parent
benzonatate
benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant.		3.2310benzoate ester;
secondary amino compound;
substituted aniline		anaesthetic;
antitussive
acrolein
[no description available]		7.0710enalherbicide;
human xenobiotic metabolite;
toxin
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		3.4611pyrrole;
secondary amine
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.0510mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
isopropyl myristate
isopropyl myristate: used for microemulsions; structure		2.0510fatty acid ester
methylergonovine
Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed)		3.2310ergoline alkaloid
phenformin
Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis.		2.0810biguanidesantineoplastic agent;
geroprotector;
hypoglycemic agent
meglumine
Meglumine: 1-Deoxy-1-(methylamino)-D-glucitol. A derivative of sorbitol in which the hydroxyl group in position 1 is replaced by a methylamino group. Often used in conjunction with iodinated organic compounds as contrast medium.. N-methylglucamine : A hexosamine that is D-glucitol in which the hydroxy group at position 1 is substituted by the nitrogen of a methylamino group. A crystalline base, it is used in preparing salts of certain acids for use as diagnostic radiopaque media, while its antimonate is used as an antiprotozoal in the treatment of leishmaniasis.		2.1510hexosamine;
secondary amino compound
cinchophen
cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94		3.2310quinolines
ethyl acetate
ethyl acetate : The acetate ester formed between acetic acid and ethanol.		2.2510acetate ester;
ethyl ester;
volatile organic compound		EC 3.4.19.3 (pyroglutamyl-peptidase I) inhibitor;
metabolite;
polar aprotic solvent;
Saccharomyces cerevisiae metabolite
yohimbine
Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.		11.0250methyl 17-hydroxy-20xi-yohimban-16-carboxylatealpha-adrenergic antagonist;
dopamine receptor D2 antagonist;
serotonergic antagonist
nafcillin
Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group.		3.2310penicillin allergen;
penicillin		antibacterial drug
methohexital
Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups.		3.2310acetylenic compound;
barbiturates		drug allergen;
intravenous anaesthetic
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		6.3562azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		2.1310adamantanes;
polycyclic alkane
isoxazoles
Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.		2.0510isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		6.21311,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		5.8132diazine;
pyrazines		Daphnia magna metabolite
ephedrine
Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively.		3.2310phenethylamine alkaloid;
phenylethanolamines		bacterial metabolite;
environmental contaminant;
nasal decongestant;
plant metabolite;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
norchlorcyclizine
norchlorcyclizine: RN given refers to parent cpd		2.3110
monocrotaline
Monocrotaline: A pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes are noted after oral magnesium treatment.		3.0340pyrrolizidine alkaloid
testosterone enanthate
[no description available]		8.9221heptanoate ester;
sterol ester		androgen
aminophylline
Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio.		3.6120mixturebronchodilator agent;
cardiotonic drug
azacitidine
Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia.		3.2310N-glycosyl-1,3,5-triazine;
nucleoside analogue		antineoplastic agent
galantamine
Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils.		3.6120benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound		antidote to curare poisoning;
cholinergic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant metabolite
nandrolone decanoate
Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS.		3.2310steroid ester
procarbazine hydrochloride
procarbazine hydrochloride : A hydrochloride obtained by combining procarbazine with one equivalent of hydrochloric acid. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands.		2.0810hydrochlorideantineoplastic agent
betamethasone
Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)		2.081011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		anti-asthmatic agent;
anti-inflammatory drug;
immunosuppressive agent
silicon carbide
silicon carbide: fibers used for reinforcement of porcelain crowns; a feldspathic body (gingival) porcelain; used to coat titanium hip prostheses		2.1110organosilicon compound
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		2.7230imidazolidine-2,4-dione
dextropropoxyphene
Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene.		3.23101-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoatemu-opioid receptor agonist;
opioid analgesic
chenodeoxycholic acid
Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3.		3.2310bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
emetine
Emetine: The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS.. emetine : A pyridoisoquinoline comprising emetam having methoxy substituents at the 6'-, 7'-, 10- and 11-positions. It is an antiprotozoal agent and emetic. It inhibits SARS-CoV2, Zika and Ebola virus replication and displays antimalarial, antineoplastic and antiamoebic properties.		2.0810isoquinoline alkaloid;
pyridoisoquinoline		antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor
4-hydroxybutyric acid
4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group.		3.23104-hydroxy monocarboxylic acid;
hydroxybutyric acid		general anaesthetic;
GHB receptor agonist;
neurotoxin;
sedative
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		3.1440
dihydroergotamine
Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension.		3.2310ergot alkaloid;
semisynthetic derivative		dopamine agonist;
non-narcotic analgesic;
serotonergic agonist;
sympatholytic agent;
vasoconstrictor agent
medroxyprogesterone
[no description available]		3.642017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		contraceptive drug;
progestin;
synthetic oral contraceptive
dihydrotestosterone
Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.		4.022117beta-hydroxy steroid;
17beta-hydroxyandrostan-3-one;
3-oxo-5alpha-steroid		androgen;
Daphnia magna metabolite;
human metabolite;
mouse metabolite
dimenhydrinate
gravinol: has antioxidant and ant-inflammatory activities; structure in first source		3.6120diarylmethane
methamphetamine
Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.		3.6120amphetamines;
secondary amine		central nervous system stimulant;
environmental contaminant;
neurotoxin;
psychotropic drug;
xenobiotic
levocarnitine
(R)-carnitine : The (R)-enantiomer of carnitine.		3.2310carnitineantilipemic drug;
nootropic agent;
nutraceutical;
Saccharomyces cerevisiae metabolite;
water-soluble vitamin (role)
malondialdehyde
Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form.		5.94221dialdehydebiomarker
sulfanilylurea
sulfanilylurea: antimicrobial agent; structure		3.2310benzenes;
sulfonamide
1-naphthylisothiocyanate
1-Naphthylisothiocyanate: A tool for the study of liver damage which causes bile stasis and hyperbilirubinemia acutely and bile duct hyperplasia and biliary cirrhosis chronically, with changes in hepatocyte function. It may cause skin and kidney damage.		2.0810isothiocyanateinsecticide
lactulose
[no description available]		3.2310glycosylfructosegastrointestinal drug;
laxative
megestrol acetate
[no description available]		2.081020-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
pamabrom
[no description available]		3.2310
acetylcysteine
N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine.		3.9730acetylcysteine;
L-cysteine derivative;
N-acetyl-L-amino acid		antidote to paracetamol poisoning;
antiinfective agent;
antioxidant;
antiviral drug;
ferroptosis inhibitor;
geroprotector;
human metabolite;
mucolytic;
radical scavenger;
vulnerary
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		3.6120cyclic ketone;
erythromycin
dehydroepiandrosterone sulfate
Dehydroepiandrosterone Sulfate: The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.. dehydroepiandrosterone sulfate : A steroid sulfate that is the 3-sulfooxy derivative of dehydroepiandrosterone.		3.431117-oxo steroid;
steroid sulfate		EC 2.7.1.33 (pantothenate kinase) inhibitor;
human metabolite;
mouse metabolite
methylnitrosourea
Methylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-methyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.		2.2110N-nitrosoureasalkylating agent;
carcinogenic agent;
mutagen;
teratogenic agent
hydroxychloroquine sulfate
[no description available]		2.0810
levonorgestrel
Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis.		3.612017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin;
synthetic oral contraceptive
diphenoxylate
Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin.		3.2310ethyl ester;
nitrile;
piperidinecarboxylate ester;
tertiary amine		antidiarrhoeal drug
ethambutol hydrochloride
ethambutol dihydrochloride : The dihydrchloride salt of ethambutol. A bacteriostatic antimycobacterial drug, it is effective against Mycobacterium tuberculosis and some other mycobacteria. It is used in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol dihydrochloride is used alone.		2.0810hydrochlorideantitubercular agent
ethambutol
Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone.		3.2310ethanolamines;
ethylenediamine derivative		antitubercular agent;
environmental contaminant;
xenobiotic
antimycin a
[no description available]		2.0810benzamides;
formamides;
macrodiolide;
phenols		antifungal agent;
mitochondrial respiratory-chain inhibitor;
piscicide
vancomycin
Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.		3.2310glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
d-alpha tocopherol
Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.		3.6420alpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
pregnenolone carbonitrile
Pregnenolone Carbonitrile: A catatoxic steroid and microsomal enzyme inducer having significant effects on the induction of cytochrome P450. It has also demonstrated the potential for protective capability against acetaminophen-induced liver damage.		2.0810aliphatic nitrile
ibufenac
ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects.		3.2310monocarboxylic acidEC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
metylperon
metylperon: RN given refers to parent cpd		2.0810aromatic ketone
methyl tert-butyl ether
methyl tert-butyl ether: used to dissolve gallstones; gasoline additive. methyl tert-butyl ether : An ether having methyl and tert-butyl as the two alkyl components.		2.0810etherfuel additive;
metabolite;
non-polar solvent
metaxalone
[no description available]		3.2310aromatic ether
spectinomycin
Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis.		3.2310cyclic acetal;
cyclic hemiketal;
cyclic ketone;
pyranobenzodioxin;
secondary alcohol;
secondary amino compound		antibacterial drug;
antimicrobial agent;
bacterial metabolite
dronabinol
Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.		3.2310benzochromene;
diterpenoid;
phytocannabinoid;
polyketide		cannabinoid receptor agonist;
epitope;
hallucinogen;
metabolite;
non-narcotic analgesic
amiloride
Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.		3.2310aromatic amine;
guanidines;
organochlorine compound;
pyrazines		diuretic;
sodium channel blocker
pimozide
Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group.		3.5820benzimidazoles;
heteroarylpiperidine;
organofluorine compound		antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist
7-hydroxychlorpromazine
7-hydroxychlorpromazine: RN given refers to parent cpd		2.0810phenothiazines
dexbrompheniramine
dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		3.2310brompheniramineanti-allergic agent;
H1-receptor antagonist
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		3.6120dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
dicloxacillin
Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group.		3.6120dichlorobenzene;
penicillin		antibacterial drug
megestrol
Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17.		3.231017alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone		antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive
streptomycin
[no description available]		3.2310antibiotic antifungal drug;
antibiotic fungicide;
streptomycins		antibacterial drug;
antifungal agrochemical;
antimicrobial agent;
antimicrobial drug;
bacterial metabolite;
protein synthesis inhibitor
carbonates
Carbonates: Salts or ions of the theoretical carbonic acid, containing the radical CO2(3-). Carbonates are readily decomposed by acids. The carbonates of the alkali metals are water-soluble; all others are insoluble. (From Grant & Hackh's Chemical Dictionary, 5th ed). carbonates : Organooxygen compounds that are salts or esters of carbonic acid, H2CO3.		2.0810carbon oxoanion
cladribine
[no description available]		3.6120organochlorine compound;
purine 2'-deoxyribonucleoside		antineoplastic agent;
immunosuppressive agent
carbenicillin
Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain.		3.2310penicillin allergen;
penicillin		antibacterial drug
dexpropranolol
[no description available]		2.3110propranolol
metocurine
metocurine: from Chinese herb Cyclea hainanensis Mrr		2.0810isoquinolines
clomacran
clomacran: RN given refers to parent cpd; structure		3.2310acridines
methenamine hippurate
methenamine hippurate: both parts of molecule contribute to its antibacterial action		3.2310N-acylglycine
limonene
Limonene: A naturally-occurring class of MONOTERPENES which occur as a clear colorless liquid at room temperature. Limonene is the major component in the oil of oranges which has many uses, including as flavor and fragrance. It is recognized as safe in food by the Food and Drug Administration (FDA).. limonene : A monoterpene that is cyclohex-1-ene substituted by a methyl group at position 1 and a prop-1-en-2-yl group at position 4 respectively.		7.2510cycloalkene;
p-menthadiene		human metabolite
olsalazine
olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease.		3.2310azobenzenes;
dicarboxylic acid		non-steroidal anti-inflammatory drug;
prodrug
etidronate disodium
etidronate disodium : An organic sodium salt resulting from the replacement of two protons from etidronic acid (one from from each of the phosphonic acid groups) by sodium ions.		2.0810organic sodium saltantineoplastic agent;
bone density conservation agent;
chelator
platinum
Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.		2.1710elemental platinum;
nickel group element atom;
platinum group metal atom
gold
Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.		7.5820copper group element atom;
elemental gold
zalcitabine
Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.		2.0810pyrimidine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
acetylglucosamine
Acetylglucosamine: The N-acetyl derivative of glucosamine.. N-acetyl-beta-D-glucosamine : An N-acetyl-D-glucosamine having beta-configuration at the anomeric centre.		3.4611N-acetyl-D-glucosamineepitope
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.4620delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
bromine
Bromine: A halogen with the atomic symbol Br, atomic number 35, and atomic weight 79.904. It is a volatile reddish-brown liquid that gives off suffocating vapors, is corrosive to the skin, and may cause severe gastroenteritis if ingested.		2.1510diatomic bromine
sodium thiosulfate
sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio.		3.2310inorganic sodium saltantidote to cyanide poisoning;
antifungal drug;
nephroprotective agent
mafenide acetate
[no description available]		2.0810carboxylic acid
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		2.0810anthraquinone
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		3.2310selegiline;
terminal acetylenic compound		geroprotector
selegiline hydrochloride, (r)-isomer
[no description available]		2.0810hydrochloride;
terminal acetylenic compound		antiparkinson drug;
dopaminergic agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor
levamisole
Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.		2.03106-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazoleantinematodal drug;
antirheumatic drug;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
immunological adjuvant;
immunomodulator
clemastine
Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		3.2310monochlorobenzenes;
N-alkylpyrrolidine		anti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
thiamphenicol
[no description available]		2.0810monocarboxylic acid amide;
sulfone		antimicrobial agent;
immunosuppressive agent
pancuronium bromide
pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication.		2.0810bromide saltcholinergic antagonist;
muscle relaxant;
nicotinic antagonist
cephalexin
Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
semisynthetic derivative		antibacterial drug
isosorbide-5-mononitrate
isosorbide-5-mononitrate: for prevention of angina pectoris; structure given in first source; a Russian drug		3.1210glucitol derivative;
nitrate ester		nitric oxide donor;
vasodilator agent
ornidazole
Ornidazole: A nitroimidazole antiprotozoal agent used in ameba and trichomonas infections. It is partially plasma-bound and also has radiation-sensitizing action.. ornidazole : A C-nitro compound that is 5-nitroimidazole in which the hydrogens at positions 1 and 2 are replaced by 3-chloro-2-hydroxypropyl and methyl groups, respectively. It is used in the treatment of susceptible protozoal infections and for the treatment of anaerobic bacterial infections.		2.0810C-nitro compound;
imidazoles;
organochlorine compound;
secondary alcohol		antiamoebic agent;
antibacterial drug;
antiinfective agent;
antiprotozoal drug;
antitrichomonal drug;
epitope
danazol
Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.		3.93017beta-hydroxy steroid;
terminal acetylenic compound		anti-estrogen;
estrogen antagonist;
geroprotector
fenclozic acid
fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd		3.2310
laxagetten 4,4'-diacetoxydiphenylpyridylemethane
[no description available]		3.2310
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		3.2310aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
fludarabine phosphate
fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas.		3.6120nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate		antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug
alclofenac
alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash.		3.2310aromatic ether;
monocarboxylic acid;
monochlorobenzenes		drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
bromocriptine
Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion.		4.1420indole alkaloidantidyskinesia agent;
antiparkinson drug;
dopamine agonist;
hormone antagonist
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		2.2510benzenes;
phenyl acetates
cetylpyridinium chloride anhydrous
tserigel: according to first source contains polyvinylbutyral & cetylpyridinium chloride; UD only lists cetylpyridinium chloride as constituent. cetylpyridinium chloride : A pyridinium salt that has N-hexadecylpyridinium as the cation and chloride as the anion. It has antiseptic properties and is used in solutions or lozenges for the treatment of minor infections of the mouth and throat.		3.4311chloride salt;
organic chloride salt		antiseptic drug;
surfactant
oxyphenisatin
[no description available]		3.2310indoles
fludrocortisone
Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity.		3.231011beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
fluorinated steroid;
mineralocorticoid		adrenergic agent;
anti-inflammatory drug
ursodeoxycholic acid
Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		3.2310bile acid;
C24-steroid;
dihydroxy-5beta-cholanic acid		human metabolite;
mouse metabolite
benzonidazole
benzonidazole: used in treatment of Chagas' disease. benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease.		2.0810C-nitro compound;
imidazoles;
monocarboxylic acid amide		antiprotozoal drug
dexchlorpheniramine
dexchlorpheniramine: RN given refers to parent cpd(S)-isomer		3.2310chlorphenamine
clometacin
clometacin: structure		3.2310N-acylindole
cefazolin
Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
tetrazoles;
thiadiazoles		antibacterial drug
amoxicillin
Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.		3.6120penicillin allergen;
penicillin		antibacterial drug
timolol
(S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine.		3.6120timololanti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist
indoramin
Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.		2.0810tryptamines
tramadol
Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer.		2.15102-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanoladrenergic uptake inhibitor;
antitussive;
capsaicin receptor antagonist;
delta-opioid receptor agonist;
kappa-opioid receptor agonist;
metabolite;
mu-opioid receptor agonist;
muscarinic antagonist;
nicotinic antagonist;
NMDA receptor antagonist;
opioid analgesic;
serotonergic antagonist;
serotonin uptake inhibitor
oxcarbazepine
Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy.		3.6120cyclic ketone;
dibenzoazepine		anticonvulsant;
drug allergen
carbidopa
carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		3.6120catechols;
hydrazines;
monocarboxylic acid		antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
moricizine
Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group.		3.2310carbamate ester;
morpholines;
phenothiazines		anti-arrhythmia drug
amineptin
amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne.		3.2310amino acid;
carbocyclic fatty acid;
carbotricyclic compound;
secondary amino compound		antidepressant;
dopamine uptake inhibitor
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		3.6120azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
feprazone
Feprazone: A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15)		2.0810organic molecular entity
pirprofen
pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure		3.2310pyrroline
tobramycin
Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.		2.0810amino cyclitol glycosideantibacterial agent;
antimicrobial agent;
toxin
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		3.8630taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		3.6120beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
dobutamine
Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure.		4.9521catecholamine;
secondary amine		beta-adrenergic agonist;
cardiotonic drug;
sympathomimetic agent
penbutolol
Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent.		3.2310ethanolamines
ribavirin
Rebetron: Rebetron is tradename		3.61201-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
amikacin
Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group.		3.6120alpha-D-glucoside;
amino cyclitol glycoside;
aminoglycoside;
carboxamide		antibacterial drug;
antimicrobial agent;
nephrotoxin
cephradine
Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton.		3.2310beta-lactam antibiotic allergen;
cephalosporin		antibacterial drug
ticrynafen
Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis.		3.2310aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid;
thiophenes		antihypertensive agent;
hepatotoxic agent;
loop diuretic
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		3.2310L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
diltiazem
Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension.		4.31505-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetateantihypertensive agent;
calcium channel blocker;
vasodilator agent
vecuronium bromide
Vecuronium Bromide: Monoquaternary homolog of PANCURONIUM. A non-depolarizing neuromuscular blocking agent with shorter duration of action than pancuronium. Its lack of significant cardiovascular effects and lack of dependence on good kidney function for elimination as well as its short duration of action and easy reversibility provide advantages over, or alternatives to, other established neuromuscular blocking agents.. vecuronium bromide : The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent;
nicotinic antagonist
vecuronium
vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents.		3.2310acetate ester;
androstane;
quaternary ammonium ion		drug allergen;
muscle relaxant;
neuromuscular agent;
nicotinic antagonist
ng-nitroarginine methyl ester
NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.		9.36180alpha-amino acid ester;
L-arginine derivative;
methyl ester;
N-nitro compound		EC 1.14.13.39 (nitric oxide synthase) inhibitor
benoxaprofen
benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals.		3.23101,3-benzoxazoles;
monocarboxylic acid;
monochlorobenzenes		antipsoriatic;
antipyretic;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
hepatotoxic agent;
nephrotoxin;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
protein kinase C agonist
exifone
[no description available]		3.2310benzophenones
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		3.2310[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
nitazoxanide
nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug		3.6120benzamides;
carboxylic ester
sufentanil
Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid.		3.2310anilide;
ether;
piperidines;
thiophenes		anaesthesia adjuvant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic
acarbose
[no description available]		3.6120tetrasaccharide derivativeEC 3.2.1.1 (alpha-amylase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
geroprotector;
hypoglycemic agent
torsemide
Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure.		3.2310aminopyridine;
N-sulfonylurea;
secondary amino compound		antihypertensive agent;
loop diuretic
epirubicin
Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA.		3.2310aminoglycoside;
anthracycline antibiotic;
anthracycline;
deoxy hexoside;
monosaccharide derivative;
p-quinones;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		antimicrobial agent;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
lorcainide
[no description available]		2.0810acetamides
idarubicin
Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.		3.2310anthracycline antibiotic;
deoxy hexoside;
monosaccharide derivative
piperacillin
Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group.		3.2310penicillin allergen;
penicillin		antibacterial drug
paroxetine
Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo.		6.4262aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines		antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
captopril
Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.		3.6120alkanethiol;
L-proline derivative;
N-acylpyrrolidine;
pyrrolidinemonocarboxylic acid		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
cefoperazone
Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance.		3.2310cephalosporinantibacterial drug
staurosporine
[no description available]		2.0810indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
foscarnet sodium
trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity.		2.0810one-carbon compound;
organic sodium salt		antiviral drug
atracurium
Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups.		3.2310diester;
quaternary ammonium ion		muscle relaxant;
nicotinic antagonist
atracurium besylate
atracurium besylate : The bisbenzenesulfonate salt of atracurium.		2.0810organosulfonate salt;
quaternary ammonium salt		muscle relaxant;
nicotinic antagonist
nicorandil
Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris.		2.0810nitrate ester;
pyridinecarboxamide		potassium channel opener;
vasodilator agent
pergolide
Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		3.2310diamine;
methyl sulfide;
organic heterotetracyclic compound		antiparkinson drug;
dopamine agonist
pergolide mesylate
pergolide mesylate : A methanesulfonate salt obtained from pergolide by mixing eqimolar amount of pergolide and methanesulfonic acid. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction.		2.0810methanesulfonate saltantiparkinson drug;
dopamine agonist;
geroprotector
colforsin
Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.		2.0310acetate ester;
cyclic ketone;
labdane diterpenoid;
organic heterotricyclic compound;
tertiary alpha-hydroxy ketone;
triol		adenylate cyclase agonist;
anti-HIV agent;
antihypertensive agent;
plant metabolite;
platelet aggregation inhibitor;
protein kinase A agonist
cefadroxil anhydrous
Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.6120cephalosporinantibacterial drug
encainide
Encainide: One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.. encainide : 4-Methoxy-N-phenylbenzamide in which the hydrogen at the 2 position of the phenyl group is substituted by a 2-(1-methylpiperidin-2-yl)ethyl group. A class Ic antiarrhythmic, the hydrochloride was used for the treatment of severe or life-threatening ventricular arrhythmias, but it was associated with increased death rates in patients who had asymptomatic heart rhythm abnormalities after a recent heart attack and was withdrawn from the market.		2.0810benzamides;
piperidines		anti-arrhythmia drug;
sodium channel blocker
talniflumate
talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma		2.0810benzofurans
fenoldopam mesylate
[no description available]		2.0810benzazepine
fialuridine
[no description available]		3.2310
cefaclor anhydrous
Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.6120cephalosporinantibacterial drug;
drug allergen
pefloxacin
Pefloxacin: A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria.. pefloxacin : A quinolone that is 4-oxo-1,4-dihydroquinoline which is substituted at positions 1, 3, 6 and 7 by ethyl, carboxy, fluorine, and 4-methylpiperazin-1-yl groups, respectively.		2.4720fluoroquinolone antibiotic;
monocarboxylic acid;
N-alkylpiperazine;
N-arylpiperazine;
quinolone antibiotic;
quinolone		antibacterial drug;
antiinfective agent;
DNA synthesis inhibitor
alfentanil
Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position.		3.2310monocarboxylic acid amide;
piperidines		central nervous system depressant;
intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
peripheral nervous system drug
fomesafen
fomesafen: a protoporphyrinogen oxidase-inhibiting herbicide. fomesafen : An N-sulfonylcarboxamide that is N-(methylsulfonyl)benzamide in which the phenyl ring is substituted by a nitro group at position 2 and a 2-chloro-4-(trifluoromethyl)phenoxy group at position 5. A protoporphyrinogen oxidase inhibitor, it was specially developed for use (generally as the corresponding sodium salt, fomesafen-sodium) for post-emergence control of broad-leaf weeds in soya.		2.5520aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-sulfonylcarboxamide;
organofluorine compound;
phenols		agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide
miglustat
miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group.		3.2310piperidines;
tertiary amino compound		anti-HIV agent;
EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor
haloperidol decanoate
[no description available]		3.2310organic molecular entity
cefotetan
Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms.		3.6120
lovastatin
Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).		5.4641delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug
flupirtine
flupirtine: RN given refers to parent cpd without isomeric designation		2.0810aminopyridine
tolrestat
tolrestat: RN & structure given in first source		3.2310naphthalenesEC 1.1.1.21 (aldehyde reductase) inhibitor
enoximone
Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.		2.0810aromatic ketone
stepronin
[no description available]		2.0810N-acyl-amino acid
simvastatin
Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.		9.2750delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)		EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug
idazoxan
Idazoxan: A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.. idazoxan : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine in which one of the hydrogens at position 2 has been replaced by a 4,5-dihydro-1H-imidazol-2-yl group.		2.0810benzodioxine;
imidazolines		alpha-adrenergic antagonist
remoxipride
Remoxipride: An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia.		2.0810dimethoxybenzene
balsalazide
balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond.		3.2310
pravastatin
Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		3.86303-hydroxy carboxylic acid;
carbobicyclic compound;
carboxylic ester;
hydroxy monocarboxylic acid;
secondary alcohol;
statin (semi-synthetic)		anticholesteremic drug;
environmental contaminant;
metabolite;
xenobiotic
cabergoline
Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.		3.6120N-acylureaantineoplastic agent;
antiparkinson drug;
dopamine agonist
atomoxetine hydrochloride
Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine.		2.0810hydrochlorideadrenergic uptake inhibitor;
antidepressant
atomoxetine
atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents.		3.6120aromatic ether;
secondary amino compound;
toluenes		adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic
quinapril
Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure.		3.6120dicarboxylic acid monoester;
ethyl ester;
isoquinolines;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
alpidem
[no description available]		3.2310imidazoles
raloxifene hydrochloride
Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.		2.1310hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		3.61203-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
itraconazole
Itraconazole: A triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes required for ERGOSTEROL synthesis.. itraconazole : An N-arylpiperazine that is cis-ketoconazole in which the imidazol-1-yl group is replaced by a 1,2,4-triazol-1-yl group and in which the actyl group attached to the piperazine moiety is replaced by a p-[(+-)1-sec-butyl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl]phenyl group. A potent P-glycoprotein and CYP3A4 inhibitor, it is used as an antifungal drug for the treatment of various fungal infections, including aspergillosis, blastomycosis, candidiasis, chromoblastomycosis, coccidioidomycosis, cryptococcosis, histoplasmosis, and sporotrichosis.		7.0210aromatic ether;
conazole antifungal drug;
cyclic ketal;
dichlorobenzene;
dioxolane;
N-arylpiperazine;
triazole antifungal drug;
triazoles		EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
Hedgehog signaling pathway inhibitor;
P450 inhibitor
fosphenytoin
fosphenytoin: structure given in first & second source		3.2310imidazolidine-2,4-dione
salmeterol xinafoate
Salmeterol Xinafoate: A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE.		3.3920naphthoic acid
ranolazine
Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina.		3.6120aromatic amide;
monocarboxylic acid amide;
monomethoxybenzene;
N-alkylpiperazine;
secondary alcohol
finasteride
Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.		8.411333-oxo steroid;
aza-steroid;
delta-lactam		androgen antagonist;
antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
imiquimod
Imiquimod: A topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial CARCINOMA, BASAL CELL; and ACTINIC KERATOSIS.. imiquimod : An imidazoquinoline fused [4,5-c] carrying isobutyl and amino substituents at N-1 and C-4 respectively. A prescription medication, it acts as an immune response modifier and is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis.		2.0810imidazoquinolineantineoplastic agent;
interferon inducer
esmolol
methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure.		3.2310aromatic ether;
ethanolamines;
methyl ester;
secondary alcohol;
secondary amino compound
sertindole
sertindole : A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-oxoimidazolidin-1-yl)ethyl group.		2.0810heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole		alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist
adapalene
Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE.. adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether.		2.0810adamantanes;
monocarboxylic acid;
naphthoic acid		dermatologic drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
non-steroidal anti-inflammatory drug
adefovir
adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection.		3.23106-aminopurines;
ether;
phosphonic acids		antiviral drug;
DNA synthesis inhibitor;
drug metabolite;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent
aromasil
[no description available]		3.863017-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid		antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor;
environmental contaminant;
xenobiotic
sparfloxacin
[no description available]		2.0810fluoroquinolone antibiotic;
N-arylpiperazine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone
zileuton
[no description available]		3.61201-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
clopidogrel
Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks.		3.2310methyl ester;
monochlorobenzenes;
thienopyridine		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
cidofovir anhydrous
Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients.		3.6120phosphonic acids;
pyrimidone		anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent
tiagabine
Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy.		3.2310beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes		anticonvulsant;
GABA reuptake inhibitor
topotecan
Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.		3.2310pyranoindolizinoquinolineantineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor
bromfenac
bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure.		3.6120aromatic amino acid;
benzophenones;
organobromine compound;
substituted aniline		non-narcotic analgesic;
non-steroidal anti-inflammatory drug
gemcitabine hydrochloride
[no description available]		2.0810hydrochloride;
organofluorine compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		3.2310organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
ibutilide
ibutilide: RN & structure in first source; RN refers to the fumarate salt		10.2231benzenes;
organic amino compound
aripiprazole
Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders.		3.6120aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone		drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist
remifentanil
Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline.		3.2310alpha-amino acid ester;
anilide;
monocarboxylic acid amide;
piperidinecarboxylate ester		intravenous anaesthetic;
mu-opioid receptor agonist;
opioid analgesic;
sedative
atorvastatin calcium anhydrous
[no description available]		2.0810organic calcium salt
atorvastatin
[no description available]		10.6751aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
lamivudine
[no description available]		3.6120monothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol		allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
duloxetine hydrochloride
Duloxetine Hydrochloride: A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.. (S)-duloxetine hydrochloride : A duloxetine hydrochloride in which the duloxetine moiety has S configuration.		2.0810duloxetine hydrochlorideantidepressant
duloxetine
[no description available]		3.6120duloxetine
irinotecan
[no description available]		3.2310carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		3.6120biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
ibandronic acid
Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS.		3.2310
ziprasidone
ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.		3.57201,2-benzisothiazole;
indolones;
organochlorine compound;
piperazines		antipsychotic agent;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
psychotropic drug;
serotonergic antagonist
zolmitriptan
zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine.		3.6120oxazolidinone;
tryptamines		anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
adefovir dipivoxil
bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection.		2.08106-aminopurines;
carbonate ester;
ether;
organic phosphonate		antiviral drug;
DNA synthesis inhibitor;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent;
prodrug
emtricitabine
Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection.		3.6120monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone		antiviral drug;
HIV-1 reverse transcriptase inhibitor
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		3.2310biphenyls
tiludronic acid
tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source		3.2310organochlorine compound
tirofiban
Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.		3.2310L-tyrosine derivative;
piperidines;
sulfonamide		anticoagulant;
fibrin modulating drug;
platelet glycoprotein-IIb/IIIa receptor antagonist
capecitabine
Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.		3.2310carbamate ester;
cytidines;
organofluorine compound		antimetabolite;
antineoplastic agent;
prodrug
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		4.9521adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
paroxetine hydrochloride
paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug.		2.0810hydrochlorideantidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor
bupropion hydrochloride
[no description available]		2.0810aromatic ketone
trazodone hydrochloride
Triticum: A plant genus of the family POACEAE that is the source of EDIBLE GRAIN. A hybrid with rye (SECALE CEREALE) is called TRITICALE. The seed is ground into FLOUR and used to make BREAD, and is the source of WHEAT GERM AGGLUTININS.. trazodone hydrochloride : A hydrochloride salt prepared from equimolar amounts of trazodone and hydrogen chloride.		2.0810hydrochlorideadrenergic antagonist;
antidepressant;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor
trovafloxacin
trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure.		3.2310
cefprozil
[no description available]		3.2310cephalosporin;
semisynthetic derivative		antibacterial drug
doxazosin mesylate
Cardura: Trade name in United States.		2.0810methanesulfonate saltgeroprotector
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		3.8930acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
nelfinavir
Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.		3.8930aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound		antineoplastic agent;
HIV protease inhibitor
glucose, (beta-d)-isomer
beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages.		2.0610D-glucopyranoseepitope;
mouse metabolite
mevastatin
mevastatin: antifungal metabolite from Penicillium brevicopactum; potent inhibitory activity to sterol synthesis; structure. mevastatin : A carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.		2.46202-pyranones;
carboxylic ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring)		antifungal agent;
apoptosis inducer;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
fungal metabolite;
Penicillium metabolite
bupivacaine hydrochloride
bupivacaine hydrochloride (anhydrous) : A racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride : A hydrochloride obtained by combining 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide with one molar equivalent of hydrochloric acid.		2.0810hydrochloride;
racemate		adrenergic antagonist;
amphiphile;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor;
local anaesthetic
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		3.2310aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
plerixafor
plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma.		3.8730azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound		anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant
amprenavir
[no description available]		3.6120carbamate ester;
sulfonamide;
tetrahydrofuryl ester		antiviral drug;
HIV protease inhibitor
oseltamivir
Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza.		3.2310acetamides;
amino acid ester;
cyclohexenecarboxylate ester;
primary amino compound		antiviral drug;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
environmental contaminant;
prodrug;
xenobiotic
testosterone undecanoate
[no description available]		5.0833steroid ester
ticlopidine hydrochloride
[no description available]		2.0810hydrochloride
epirubicin hydrochloride
[no description available]		2.0810
histamine phosphate
histamine phosphate : A phosphate salt that is the diphosphate salt of histamine.		3.2310phosphate salthistamine agonist
tilbroquinol
[no description available]		3.2310organohalogen compound;
quinolines
bendamustine
[no description available]		3.2310benzimidazoles
droxicam
droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis.		3.2310organic heterotricyclic compound;
pyridines		cyclooxygenase 1 inhibitor;
hepatotoxic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor;
prodrug
rutecarpine
rutacarpine: from Evodia rutaecarpa; an ingredient in zhuyu hewei zhitong capsules		2.2510beta-carbolines
ebrotidine
ebrotidine: an H2-receptor antagonist and gastric mucosa protector		3.2310sulfonamide
pazufloxacin
[no description available]		2.0810quinolines
repaglinide
[no description available]		3.8930piperidines
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		3.9330benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		2.52201,2,3-triazole
miconazole nitrate
miconazole nitrate : A racemate composed of equimolar amounts of (R)- and (S)-miconazole nitrate. An antifungal used for the treatment of athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes.		2.0810
sertraline
Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder.		3.5720dichlorobenzene;
secondary amino compound;
tetralins		antidepressant;
serotonin uptake inhibitor
zoledronic acid
Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position.		3.61201,1-bis(phosphonic acid);
imidazoles		bone density conservation agent
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
brinzolamide
brinzolamide: an antiglaucoma agent		2.0810sulfonamide;
thienothiazine		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
drospirenone
drospirenone: a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source		2.08103-oxo-Delta(4) steroid;
steroid lactone		aldosterone antagonist;
contraceptive drug;
progestin
artemether
Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		2.0810artemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid		antimalarial
acamprosate
Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3.		3.2310acetamides;
organosulfonic acid		environmental contaminant;
neurotransmitter agent;
xenobiotic
isaxonine
isaxonine: promotes nerve growth		3.2310aminopyrimidine
nebivolol
2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group.		3.2310chromanes;
diol;
organofluorine compound;
secondary alcohol;
secondary amino compound
uk 68798
[no description available]		3.8730aromatic ether;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
potassium channel blocker
dapoxetine
[no description available]		4.8361naphthalenes
hp 873
iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.		3.61201,2-benzoxazoles;
aromatic ether;
aromatic ketone;
methyl ketone;
monoamine;
organofluorine compound;
piperidines;
tertiary amino compound		dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist
dexrazoxane
Dexrazoxane: The (+)-enantiomorph of razoxane.		3.2310razoxaneantineoplastic agent;
cardiovascular drug;
chelator;
immunosuppressive agent
loxapine succinate
[no description available]		2.0810succinate saltgeroprotector
tocophersolan
tocophersolan: RN given refers to parent cpd		2.1510tocol
fenoxypropazine
[no description available]		3.2310aromatic ether
voriconazole
Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.		3.6120conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug		P450 inhibitor
betamipron
[no description available]		2.0810organonitrogen compound;
organooxygen compound
bufuralol
bufuralol: RN given refers to cpd without isomeric designation; structure		2.0810benzofurans
uroxatral
[no description available]		2.0810hydrochloride
aceclofenac
[no description available]		5.2931amino acid;
carboxylic ester;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
nitrefazole
[no description available]		3.2310imidazoles
thiocolchicoside
[no description available]		2.0810glycoside
doripenem
Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.		3.6120carbapenems
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		3.2310hydroxy-1,2-naphthoquinone
rivastigmine
[no description available]		3.2310carbamate ester;
tertiary amino compound		cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent
frovatriptan
[no description available]		3.2310carbazoles
eletriptan
eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group.		3.2310indoles;
N-alkylpyrrolidine;
sulfone		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
rosiglitazone
[no description available]		4.0940aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
tamiflu
[no description available]		2.0810phosphate salt
1-methylxanthine
1-methylxanthine: urinary metabolite of caffeine. 1-methylxanthine : A monomethylxanthine having the methyl group located at the 1-position. It is a metabolite of caffeine in humans.. 1-methyl-7H-xanthine : A 1-methylxanthine tautomer where the imidazole proton is located at the 7-position.		2.31101-methylxanthinemouse metabolite
bexarotene
[no description available]		3.6120benzoic acids;
naphthalenes;
retinoid		antineoplastic agent
s20098
[no description available]		2.0810acetamides
flunisolide
flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones		2.081011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic ketal;
fluorinated steroid;
primary alpha-hydroxy ketone		anti-asthmatic drug;
anti-inflammatory drug;
immunosuppressive agent
leucyl-leucyl-leucine
leucyl-leucyl-leucine: RN given refers to (L-Leu-L-Leu-L-Leu)-isomer. Leu-Leu-Leu : A tripeptide formed from three L-leucine residues.		210tripeptidemetabolite
ketorolac tromethamine
Ketorolac Tromethamine: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity.. ketorolac tromethamine : An organoammonium salt resulting from the mixture of equimolar amounts of ketorolac and tromethamine (tris). It has potent non-sedating analgesic and moderate anti-inflammatory effects. It is used in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis.		2.0810organoammonium saltanalgesic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor
clarithromycin
Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.		4.1140macrolide antibioticantibacterial drug;
environmental contaminant;
protein synthesis inhibitor;
xenobiotic
nicotine
(S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.		2.78303-(1-methylpyrrolidin-2-yl)pyridineanxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic
moexipril
[no description available]		3.2310peptide
4-hydroxypropranolol
4-hydroxypropranolol: metabolite of propanolol; RN given refers to parent cpd without isomeric designation		2.0810naphthols
gliquidone
gliquidone: structure; RN given refers to parent cpd		2.0810isoquinolines
melanotan-ii
melanotan-II: synthetic cyclic heptapeptide, an analog of alpha-melanotropin (4,10); capable of stimulating melanin synthesis & promoting rapid tanning of skin; currently in trials for use in the prevention of sunlight-induced skin cancer		3.1110organic molecular entity
mci 9038
[no description available]		3.2310peptide
lopinavir
[no description available]		2.0810amphetamines;
dicarboxylic acid diamide		anticoronaviral agent;
antiviral drug;
HIV protease inhibitor
moxifloxacin hydrochloride
moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride.		2.0810hydrochlorideantibacterial drug
fulvestrant
Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.		3.863017beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide		antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist
mizoribine
[no description available]		2.0810imidazolesanticoronaviral agent
sr141716
[no description available]		2.4720amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist
bosentan anhydrous
Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.		13.52379primary alcohol;
pyrimidines;
sulfonamide		antihypertensive agent;
endothelin receptor antagonist
beta-carboline-3-carboxylic acid ethyl ester
beta-carboline-3-carboxylic acid ethyl ester: isolated from brain tissue & urine; extremely potent displacer of diazepam from brain benzodiazepam receptors; structure in first source		3.2710beta-carbolines
racecadotril
racecadotril: parenterally active enkephalinase inhibitor		2.0810N-acyl-amino acid
perindopril
Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline		3.2310alpha-amino acid ester;
dicarboxylic acid monoester;
ethyl ester;
organic heterobicyclic compound		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
tryptoline
tryptoline: neurotoxic factor that may be involved in development of Parkinson's disease; enzymatic prep from human brain converts tryptamine to tryptoline; RN given refers to parent cpd; structure		2.5320beta-carbolines
n-monodemethyldiltiazem
N-monodemethyldiltiazem: RN given refers to (cis)-isomer; structure given in first source		2.0810benzothiazepine
paliperidone
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia.		3.23101,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol
nitisinone
[no description available]		3.2310(trifluoromethyl)benzenes;
C-nitro compound;
cyclohexanones;
mesotrione		EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor
plavix
[no description available]		2.0810azaheterocycle sulfate salt;
organoammonium sulfate salt		anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor
clofarabine
[no description available]		3.6120adenosines;
organofluorine compound		antimetabolite;
antineoplastic agent
anhydroecgonine methyl ester
anhydroecgonine methyl ester: structure given in first source		2.0410N-alkylpyrrolidine
pramipexole
Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively.		3.6120benzothiazoles;
diamine		antidyskinesia agent;
antiparkinson drug;
dopamine agonist;
radical scavenger
valdecoxib
[no description available]		4.0940isoxazoles;
sulfonamide		antipyretic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
yohimbane
yohimbane: from Gelsemium elegans; structure in first source		2.1110indole alkaloid fundamental parent;
indole alkaloid;
yohimban alkaloid
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		2.2510methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
almotriptan
almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position.		3.2310indoles;
sulfonamide;
tertiary amine		non-steroidal anti-inflammatory drug;
serotonergic agonist;
vasoconstrictor agent
tecastemizole
[no description available]		2.0410
mk 0663
[no description available]		2.0810bipyridines;
organochlorine compound;
sulfone		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
gefitinib
[no description available]		3.8930aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
desloratadine
desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.		4.1440benzocycloheptapyridineanti-allergic agent;
cholinergic antagonist;
drug metabolite;
H1-receptor antagonist
desvenlafaxine
O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine.		3.2310cyclohexanols;
phenols;
tertiary amino compound		antidepressant;
drug metabolite;
marine xenobiotic metabolite
methotrexate
[no description available]		3.6120dicarboxylic acid;
monocarboxylic acid amide;
pteridines		abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent
tamsulosin
[no description available]		14.9349245-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamidealpha-adrenergic antagonist;
antineoplastic agent
rufinamide
rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source		3.2310aromatic amide;
heteroarene
sulbactam
[no description available]		2.0810penicillanic acids
olmesartan medoxomil
Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION.		3.6120biphenyls
dexpanthenol
dexpanthenol: The alcohol of pantothenic acid		3.2310amino alcohol;
monocarboxylic acid amide		cholinergic drug;
provitamin
fosamprenavir
fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir.		3.2310sulfonamideprodrug
pagoclone
RP 59037: a partial benzodiazepine receptor agonist; a cyclopyrrolone that induces hypothermia		2.0810
abiraterone
[no description available]		2.08103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines		antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
febuxostat
Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout.		3.61201,3-thiazolemonocarboxylic acid;
aromatic ether;
nitrile		EC 1.17.3.2 (xanthine oxidase) inhibitor
aspartame
[no description available]		2.1710carboxylic acid;
dipeptide zwitterion;
dipeptide;
methyl ester		apoptosis inhibitor;
EC 3.1.3.1 (alkaline phosphatase) inhibitor;
environmental contaminant;
micronutrient;
nutraceutical;
sweetening agent;
xenobiotic
escitalopram
Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram.		3.23101-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrileantidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
lexapro
Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram.		2.0810
10-propargyl-10-deazaaminopterin
10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.		3.2310N-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
docetaxel anhydrous
Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.		3.6120secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
atazanavir
atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).		3.2310carbohydrazideantiviral drug;
HIV protease inhibitor
levofloxacin
Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.		3.61209-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid;
fluoroquinolone antibiotic;
quinolone antibiotic		antibacterial drug;
DNA synthesis inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
topoisomerase IV inhibitor
9-(2-hydroxy-3-nonyl)adenine
(2R,3S)-EHNA : EHNA of absolute configuration 2R,3S. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase.		3.1210EHNAEC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor
ezetimibe
Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).		3.6120azetidines;
beta-lactam;
organofluorine compound		anticholesteremic drug;
antilipemic drug;
antimetabolite
ertapenem
Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.		3.2310carbapenemcarboxylic acid;
pyrrolidinecarboxamide		antibacterial drug
cox 189
lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity.		3.6120amino acid;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
secondary amino compound		cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
cilomilast
[no description available]		3.5220methoxybenzenes
conivaptan
conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH).		3.2310benzazepineaquaretic;
vasopressin receptor antagonist
moxifloxacin
Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.		3.2310aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone		antibacterial drug
pralnacasan
pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source		3.2310
clevidipine
clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source		3.2310dihydropyridine
solifenacin
[no description available]		3.2310isoquinolines
dexmethylphenidate
dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate.		3.2310methyl phenyl(piperidin-2-yl)acetateadrenergic agent
rp 73401
piclamilast: an antiasthmatic agent and phosphodiesterase 4 inhibitor; structure in first source. piclamilast : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 3-(cyclopentyloxy)-4-methoxybenzoic acid with the primary amino group of 3,5-dichloropyridin-4-amine.		2.7430aromatic ether;
benzamides;
chloropyridine;
monocarboxylic acid amide		anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
phosphodiesterase IV inhibitor
xamoterol
Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist.		2.0810morpholines
desmethylastemizole
desmethylastemizole: astemizole metabolite in dog plasma; structure given in first source		2.0410benzimidazoles
naproxen
Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes.		3.9130methoxynaphthalene;
monocarboxylic acid		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
cinacalcet
cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group.		3.2310(trifluoromethyl)benzenes;
naphthalenes;
secondary amino compound		calcimimetic;
P450 inhibitor
birb 796
[no description available]		3.2710aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator
lubiprostone
[no description available]		3.2310
atazanavir sulfate
Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.		2.0210organic sulfate salt
(+)-rolipram
(+)-rolipram : The (S)-enantiomer of rolipram.		2.0210rolipram
telbivudine
[no description available]		3.6120pyrimidine 2'-deoxyribonucleosideantiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
n-desisopropylpropranolol
N-desisopropylpropranolol: RN given refers to parent cpd		2.3110
perlolyrine
perlolyrine: structure given in first source		2.1710organic molecular entitymetabolite
cyc 202
seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.		2.03102,6-diaminopurinesantiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
paromomycin
Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis.		3.2310amino cyclitol glycoside;
aminoglycoside antibiotic		anthelminthic drug;
antibacterial drug;
antiparasitic agent;
antiprotozoal drug
anidulafungin
Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis.		3.2310antibiotic antifungal drug;
azamacrocycle;
echinocandin;
heterodetic cyclic peptide;
semisynthetic derivative
17 alpha-hydroxyprogesterone caproate
17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS.		3.2310corticosteroid hormone
varenicline
Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking.		3.2310
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		2.4220amino acid zwitterion;
angiotensin II		human metabolite
fiduxosin
fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source		3.2310
atropine
tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.		3.8730
sb 203580
[no description available]		2.0310imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide		EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent
erlotinib
[no description available]		3.6120aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		2.0210divalent inorganic anion;
phosphite ion
dexketoprofen trometamol
dexketoprofen trometamol: a water-soluble tromethamine salt of the racemic ketoprofen, rac(+-)-ketoprofen		3.711
aflatoxin b1
Aflatoxin B1: A potent hepatotoxic and hepatocarcinogenic mycotoxin produced by the Aspergillus flavus group of fungi. It is also mutagenic, teratogenic, and causes immunosuppression in animals. It is found as a contaminant in peanuts, cottonseed meal, corn, and other grains. The mycotoxin requires epoxidation to aflatoxin B1 2,3-oxide for activation. Microsomal monooxygenases biotransform the toxin to the less toxic metabolites aflatoxin M1 and Q1.. aflatoxin B1 : An aflatoxin having a tetrahydrocyclopenta[c]furo[3',2':4,5]furo[2,3-h]chromene skeleton with oxygen functionality at positions 1, 4 and 11.		7.7620aflatoxin;
aromatic ether;
aromatic ketone		carcinogenic agent;
human metabolite
etravirine
[no description available]		3.2310aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound		antiviral agent;
HIV-1 reverse transcriptase inhibitor
dronedarone
Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias.		3.23101-benzofurans;
aromatic ether;
aromatic ketone;
sulfonamide;
tertiary amino compound		anti-arrhythmia drug;
environmental contaminant;
xenobiotic
ramelteon
ramelteon: melatonin MT1/MT2 receptor agonist		3.6120indanes
lapatinib
[no description available]		3.2310furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
darunavir
Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.		3.2310carbamate ester;
furofuran;
sulfonamide		antiviral drug;
HIV protease inhibitor
deferasirox
Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions.		3.6120benzoic acids;
monocarboxylic acid;
phenols;
triazoles		iron chelator
bms204352
BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source		2.0810
tbc-11251
sitaxsentan: endothelin A receptor antagonist; structure in first source		3.8730benzodioxoles
tolvaptan
[no description available]		3.6120benzazepine;
benzenedicarboxamide		aquaretic;
vasopressin receptor antagonist
sorafenib
[no description available]		8.6320(trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide		angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor
lenalidomide
[no description available]		4.1540aromatic amine;
dicarboximide;
isoindoles;
piperidones		angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
solifenacin succinate
Solifenacin Succinate: A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.		7.6863isoquinolines
regadenoson
[no description available]		3.2310purine nucleoside
lacosamide
Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES.		3.6120N-acyl-amino acid
estradiol 3-benzoate
17beta-estradiol 3-benzoate : A benzoate ester resulting from the formal condensation of benzoic acid with the phenolic hydroxy group of 17beta-estradiol.		3.591117beta-hydroxy steroid;
benzoate ester		estrogen receptor agonist;
xenoestrogen
cortisone
[no description available]		3.481111-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone		human metabolite;
mouse metabolite
2-aminoquinoxaline
2-aminoquinoxaline: structure in first source		2.3110
vincaleukoblastine
[no description available]		3.6120acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
vincristine sulfate
[no description available]		2.0810organic sulfate saltantineoplastic agent;
geroprotector
benzarone
benzarone: antihemorrhagic agent; structure		3.23101-benzofurans
estramustine
Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid.		3.231017beta-hydroxy steroid;
carbamate ester;
organochlorine compound		alkylating agent;
antineoplastic agent;
radiation protective agent
wortmannin
[no description available]		2.4620acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
bortezomib
[no description available]		3.6120amino acid amide;
L-phenylalanine derivative;
pyrazines		antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
ritonavir
Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.		5.48411,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas		antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic
fibrin
Fibrin: A protein derived from FIBRINOGEN in the presence of THROMBIN, which forms part of the blood clot.		2.3110peptide
glucosamine
D-glucosamine : An amino sugar whose structure comprises D-glucose having an amino substituent at position 2.. 2-amino-2-deoxy-D-glucopyranose : A D-glucosamine whose structure comprises D-glucopyranose having an amino substituent at position 2.		3.4611D-glucosamineEscherichia coli metabolite;
geroprotector;
mouse metabolite
oxytocin
Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour.		3.2310heterodetic cyclic peptide;
peptide hormone		oxytocic;
vasodilator agent
tartaric acid
tartaric acid: RN given refers to cpd with unspecified isomeric designation. D-tartaric acid : The D-enantiomer of tartaric acid.		7.8830tartaric acidEscherichia coli metabolite
pentostatin
Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia.		3.6120coformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
nitroarginine
Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.		2.4110guanidines;
L-arginine derivative;
N-nitro compound;
non-proteinogenic L-alpha-amino acid
inositol 3-phosphate
inositol 3-phosphate: RN given refers to (myo)-isomer		2.3110
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		4.350cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
meropenem
Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.		3.6120alpha,beta-unsaturated monocarboxylic acid;
carbapenemcarboxylic acid;
organic sulfide;
pyrrolidinecarboxamide		antibacterial agent;
antibacterial drug;
drug allergen
griseofulvin
Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment.		3.6201-benzofurans;
antibiotic antifungal drug;
benzofuran antifungal drug;
organochlorine compound;
oxaspiro compound		antibacterial agent;
Penicillium metabolite
cefoxitin
Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase.		3.2310beta-lactam antibiotic allergen;
cephalosporin;
cephamycin;
semisynthetic derivative		antibacterial drug
digitoxin
Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain.		2.0810cardenolide glycosideEC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor
saquinavir
Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.		3.6120L-asparagine derivative;
quinolines		antiviral drug;
HIV protease inhibitor
pancuronium
Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant.		3.2310acetate ester;
steroid ester		cholinergic antagonist;
muscle relaxant;
nicotinic antagonist
abacavir
abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection.		3.23102,6-diaminopurinesantiviral drug;
drug allergen;
HIV-1 reverse transcriptase inhibitor
perindopril erbumine
[no description available]		2.0810addition compoundantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
miglitol
[no description available]		3.6120piperidines
metyrosine
alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma.		3.2310L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		antihypertensive agent;
EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor
rocuronium bromide
rocuronium bromide : The organic bromide salt of a 5alpha androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents.		2.0810organic bromide salt;
quaternary ammonium salt		muscle relaxant;
neuromuscular agent
linezolid
[no description available]		3.6120acetamides;
morpholines;
organofluorine compound;
oxazolidinone		antibacterial drug;
protein synthesis inhibitor
acetylleucyl-leucyl-norleucinal
acetylleucyl-leucyl-norleucinal: a proteasome inhibitor. acetylleucyl-leucyl-norleucinal : A tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence.		2.0310aldehyde;
tripeptide		cysteine protease inhibitor
clindamycin phosphate
[no description available]		3.2310
pemirolast potassium salt
[no description available]		2.0810
eplerenone
Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION.		3.61203-oxo-Delta(4) steroid;
epoxy steroid;
gamma-lactone;
methyl ester;
organic heteropentacyclic compound;
oxaspiro compound;
steroid acid ester		aldosterone antagonist;
antihypertensive agent
tolterodine
[no description available]		3.6120tertiary amineantispasmodic drug;
muscarinic antagonist;
muscle relaxant
vinpocetine
vinpocetine: whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation		4.7530alkaloidgeroprotector
tibolone
tibolone: used in prevention of postmenopausal osteoporosis. tibolone : Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormone receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis.		2.081017beta-hydroxy steroid;
terminal acetylenic compound		bone density conservation agent;
hormone agonist
ao 128
AO 128: alpha-glucosidase inhibitor; structure given in first source		2.0810organic molecular entity
loteprednol etabonate
Loteprednol Etabonate: An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
etabonate ester;
organochlorine compound;
steroid acid ester;
steroid ester		anti-inflammatory drug
darifenacin
darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence.		3.61201-benzofurans;
monocarboxylic acid amide;
pyrrolidines		antispasmodic drug;
muscarinic antagonist
fluticasone propionate
fluticasone propionate : A trifluorinated corticosteroid that consists of 6alpha,9-difluoro-11beta,17alpha-dihydroxy-17beta-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a propionyl substituent at position 17; has anti-inflammatory, anti-asthmatic and anti-allergic activity.		2.081011beta-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
corticosteroid;
fluorinated steroid;
propanoate ester;
steroid ester;
thioester		adrenergic agent;
anti-allergic agent;
anti-asthmatic drug;
anti-inflammatory drug;
bronchodilator agent;
dermatologic drug
betadex
beta-Cyclodextrins: Cyclic GLUCANS consisting of seven (7) glucopyranose units linked by 1,4-glycosidic bonds.		3.0140cyclodextrin
trichostatin a
trichostatin A: chelates zinc ion in the active site of histone deacetylases, resulting in preventing histone unpacking so DNA is less available for transcription; do not confuse with TRICHOSANTHIN which is a protein; found in STREPTOMYCES		2.7630antibiotic antifungal agent;
hydroxamic acid;
trichostatin		bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector
tretinoin
Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.		3.8630retinoic acid;
vitamin A		anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule
retinol
Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).		3.2310retinol;
vitamin A		human metabolite;
mouse metabolite;
plant metabolite
tacrolimus
Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis.		3.6120macrolide lactambacterial metabolite;
immunosuppressive agent
cerivastatin
cerivastatin: cerivastatin is the ((E)-(+))-isomer; structure given in first source. cerivastatin : (3R,5S)-3,5-dihydroxyhept-6-enoic acid in which the (7E)-hydrogen is substituted by a 4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl group. Formerly used (as its sodium salt) to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.		2.4620dihydroxy monocarboxylic acid;
pyridines;
statin (synthetic)
rosuvastatin
rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer).		3.5720dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrimidines;
statin (synthetic);
sulfonamide		anti-inflammatory agent;
antilipemic drug;
cardioprotective agent;
CETP inhibitor;
environmental contaminant;
xenobiotic
cocaine
Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca.		2.1510benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic
mycophenolic acid
Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.		3.23102-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols		anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic
mupirocin
Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.		2.0810alpha,beta-unsaturated carboxylic ester;
epoxide;
monocarboxylic acid;
oxanes;
secondary alcohol;
triol		antibacterial drug;
bacterial metabolite;
protein synthesis inhibitor
clindamycin
Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.		3.2310
1-(3-tert-butyl-1-methylpyrazol-5-yl)-3-(4-chlorophenyl)urea
1-(3-tert-butyl-1-methylpyrazol-5-yl)-3-(4-chlorophenyl)urea : A member of the class of phenylureas that is urea which is substituted at position 1 by a 3-tert-butyl-1-methylpyrazol-5-yl group and at position 3 by a p-chlorophenyl group.		3.2710monochlorobenzenes;
phenylureas;
pyrazoles		EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
fosfomycin
Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus.		3.2310epoxide;
phosphonic acids		antimicrobial agent;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		3.6120macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
y 27632
Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.		2.4620aromatic amide
octreotide
[no description available]		3.2310
epothilone a
Epothilones: A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).		2.0310epothilone;
epoxide		antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator
eptifibatide
[no description available]		3.2310homodetic cyclic peptide;
macrocycle;
organic disulfide		anticoagulant;
platelet aggregation inhibitor
mesopram
mesopram: a potent & selective type IV phosphodiesterase inhibitor		2.0210
roflumilast
[no description available]		5.5880aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound		anti-asthmatic drug;
phosphodiesterase IV inhibitor
h 89
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.		2.4920N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
decitabine
[no description available]		3.61202'-deoxyribonucleoside
teniposide
[no description available]		3.6120aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes		antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
valrubicin
[no description available]		2.0810anthracycline;
trifluoroacetamide
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		3.2310actinomycinmutagen
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		3.6120L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
benzyloxycarbonylleucyl-leucyl-leucine aldehyde
benzyloxycarbonylleucyl-leucyl-leucine aldehyde: proteasome inhibitor. N-benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal : A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is protected as its benzyloxycarbonyl derivative.		2.0310amino aldehyde;
carbamate ester;
tripeptide		proteasome inhibitor
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		3.5620nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
posaconazole
[no description available]		3.6120aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles		trypanocidal drug
rubitecan
rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin.		2.0810C-nitro compound;
delta-lactone;
pyranoindolizinoquinoline;
semisynthetic derivative;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
micafungin
Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy.		3.2310antibiotic antifungal drug;
echinocandin		antiinfective agent
riboflavin
vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms).		3.2310flavin;
vitamin B2		anti-inflammatory agent;
antioxidant;
cofactor;
Escherichia coli metabolite;
food colouring;
fundamental metabolite;
human urinary metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite
sodium bicarbonate
Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.		3.2310one-carbon compound;
organic sodium salt		antacid;
food anticaking agent
arsenic trioxide
Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius.		3.2310arsenic oxideantineoplastic agent;
insecticide
2-(trifluoromethyl)acrylic acid
[no description available]		2.0610
sr 90107
fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux.		3.2310
meglumine iodipamide
[no description available]		3.2310organoammonium saltradioopaque medium
thyrotropin-releasing hormone
PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence.		3.2310peptide hormone;
tripeptide		human metabolite
arginine vasopressin
Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6.		3.6120vasopressincardiovascular drug;
hematologic agent;
mitogen
s 1033
[no description available]		3.2310(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
trilostane
trilostane: inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome. trilostane : An epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions.		2.081017beta-hydroxy steroid;
3-hydroxy steroid;
androstanoid;
epoxy steroid;
nitrile		abortifacient;
antineoplastic agent;
EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor
tropisetron
Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.		2.0510indolyl carboxylic acid
leuprolide acetate
leuprolide acetate : An acetate salt obtained by combining the nonapeptide leuprolide with acetic acid. A long lasting GnRH analog, LH-Rh agonist. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.		2.0810acetate saltantineoplastic agent;
gonadotropin releasing hormone agonist
propylthiouracil
Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.		3.6120pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
etomidate
Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.		3.2310ethyl ester;
imidazoles		intravenous anaesthetic;
sedative
mercaptopurine
Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis.		3.6120aryl thiol;
purines;
thiocarbonyl compound		anticoronaviral agent;
antimetabolite;
antineoplastic agent
levosulpiride
(S)-(-)-sulpiride : An optically active form of sulpiride having (S)-configuration. The active enantiomer of the racemic drug sulpiride. Selective D2-like dopamine antagonist (Ki values are ~ 0.015. ~ 0.013, 1, ~ 45 and ~ 77 muM at D2, D3, D4, D1 and D5 receptors respectively).		2.0810sulpirideantidepressant;
antiemetic;
antipsychotic agent;
dopaminergic antagonist
pyrantel
Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'.		3.23101,4,5,6-tetrahydropyrimidines;
carboxamidine;
thiophenes		antinematodal drug
1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone
1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone: structure in first source		2.3110
thiothixene
[no description available]		3.2310N-methylpiperazineanticoronaviral agent
eszopiclone
Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use.		3.6120zopiclonecentral nervous system depressant;
sedative
curcumin
Curcumin: A yellow-orange dye obtained from tumeric, the powdered root of CURCUMA longa. It is used in the preparation of curcuma paper and the detection of boron. Curcumin appears to possess a spectrum of pharmacological properties, due primarily to its inhibitory effects on metabolic enzymes.. curcumin : A beta-diketone that is methane in which two of the hydrogens are substituted by feruloyl groups. A natural dyestuff found in the root of Curcuma longa.		7.1110aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol		anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger
benztropine
Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.		3.2310diarylmethane
methimazole
Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen.		3.61201,3-dihydroimidazole-2-thionesantithyroid drug
cinnarizine
Cinnarizine: A piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.		2.4620diarylmethane;
N-alkylpiperazine;
olefinic compound		anti-allergic agent;
antiemetic;
calcium channel blocker;
geroprotector;
H1-receptor antagonist;
histamine antagonist;
muscarinic antagonist
sulindac
Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions.		3.8930monocarboxylic acid;
organofluorine compound;
sulfoxide		analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent
terbinafine
[no description available]		3.2310acetylenic compound;
allylamine antifungal drug;
enyne;
naphthalenes;
tertiary amine		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor;
sterol biosynthesis inhibitor
epalrestat
epalrestat : A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.		2.0810monocarboxylic acid;
thiazolidines		EC 1.1.1.21 (aldehyde reductase) inhibitor
drotaverin
drotaverin: Hungarian drug; RN given refers to parent cpd; structure		2.0810isoquinolines
thioguanine anhydrous
Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.		3.23102-aminopurinesanticoronaviral agent;
antimetabolite;
antineoplastic agent
thiourea
Thiourea: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.. thiourea : The simplest member of the thiourea class, consisting of urea with the oxygen atom substituted by sulfur.		2.1710one-carbon compound;
thioureas;
ureas		antioxidant;
chromophore
thioacetamide
Thioacetamide: A crystalline compound used as a laboratory reagent in place of HYDROGEN SULFIDE. It is a potent hepatocarcinogen.. thioacetamide : A thiocarboxamide consiting of acetamide having the oxygen replaced by sulfur.		7.5920thiocarboxamidehepatotoxic agent
succimer
Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning.		3.2310dicarboxylic acid;
dithiol;
sulfur-containing carboxylic acid		chelator
digoxin
Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small.		3.2310cardenolide glycoside;
steroid saponin		anti-arrhythmia drug;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
epitope
streptozocin
[no description available]		3.2310
tamoxifen
[no description available]		4.350stilbenoid;
tertiary amino compound		angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		3.2310pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
cancidas
[no description available]		3.2310
3-(n,n-dimethylsulfonamido)-4-methyl-nitrobenzene
BRL-50481 : A C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM).		3.5110C-nitro compound;
sulfonamide;
toluenes		bone density conservation agent;
EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor;
geroprotector
fusidic acid
Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.		2.081011alpha-hydroxy steroid;
3alpha-hydroxy steroid;
alpha,beta-unsaturated monocarboxylic acid;
steroid acid;
steroid antibiotic;
sterol ester		EC 2.7.1.33 (pantothenate kinase) inhibitor;
Escherichia coli metabolite;
protein synthesis inhibitor
lincomycin
Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis.		3.2310carbohydrate-containing antibiotic;
L-proline derivative;
monocarboxylic acid amide;
pyrrolidinecarboxamide;
S-glycosyl compound		antimicrobial agent;
bacterial metabolite
valinomycin
Valinomycin: A cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins. It is composed of 3 moles each of L-valine, D-alpha-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring. (From Merck Index, 11th ed) Valinomycin is a potassium selective ionophore and is commonly used as a tool in biochemical studies.. valinomycin : A twelve-membered cyclodepsipeptide composed of three repeating D-alpha-hydroxyisovaleryl-D-valyl-L-lactoyl-L-valyl units joined in sequence. An antibiotic found in several Streptomyces strains.		2.0810cyclodepsipeptide;
macrocycle		antimicrobial agent;
antiviral agent;
bacterial metabolite;
potassium ionophore
ranitidine
Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease.		3.2310C-nitro compound;
furans;
organic sulfide;
tertiary amino compound		anti-ulcer drug;
drug allergen;
environmental contaminant;
H2-receptor antagonist;
xenobiotic
aplaviroc
aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source		3.2310
hmr 3647
[no description available]		3.6120
latoconazole
latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source		2.0810conazole antifungal drug;
imidazole antifungal drug
maraviroc
[no description available]		3.6120tropane alkaloid
toremifene citrate
[no description available]		2.0810stilbenoidanticoronaviral agent
toremifene
Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue.		4.0940aromatic ether;
organochlorine compound;
tertiary amine		antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
telaprevir
[no description available]		3.2710cyclopentapyrrole;
cyclopropanes;
oligopeptide;
pyrazines		antiviral drug;
hepatitis C protease inhibitor;
peptidomimetic
nelarabine
nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G).		3.6120beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside		antineoplastic agent;
DNA synthesis inhibitor;
prodrug
dermatan sulfate
Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units.		3.2310amino disaccharide;
glycosylgalactose derivative;
iduronic acids;
oligosaccharide sulfate
dolasetron
[no description available]		3.6120indolyl carboxylic acid
gestodene
Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer		2.0810steroidestrogen
orlistat
Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug.		3.6120beta-lactone;
carboxylic ester;
formamides;
L-leucine derivative		anti-obesity agent;
bacterial metabolite;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor
quinine
[no description available]		3.6120cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
fospropofol
[no description available]		3.2310alkylbenzene
azilect
[no description available]		2.0810
rasagiline
[no description available]		3.6120indanes;
secondary amine;
terminal acetylenic compound		EC 1.4.3.4 (monoamine oxidase) inhibitor;
neuroprotective agent
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		3.61201,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
calixarenes
Calixarenes: Phenolic metacyclophanes derived from condensation of PHENOLS and ALDEHYDES. The name derives from the vase-like molecular structures. A bracketed [n] indicates the number of aromatic rings.. calixarenes : Originally macrocyclic compounds capable of assuming a basket (or "calix") shaped conformation. They are formed from p-hydrocarbyl phenols and formaldehyde. The term now applies to a variety of derivatives by substitution of the hydrocarbon cyclo{oligo[(1,3-phenylene)methylene]}.. calixarene : A macrocycle composed of 1,3-phenylene groups linked by methylene groups. The number of 1,3-phenylene units in the macrocycle is denoted by the "n" in calix[n]arene name.		2.5220
ovalbumin
Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.		7.1510
sc 560
SC560 : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-methoxyphenyl, trifluoromethyl and 4-chlorophenyl groups, respectively. Unlike many members of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors, SC-560 is selective for COX-1.		2.0310aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles		angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		3.6120triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		3.61202-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
jtk-303
[no description available]		3.2710aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone		HIV-1 integrase inhibitor
quercetin
[no description available]		2.55207-hydroxyflavonol;
pentahydroxyflavone		antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		2.3110prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
apigenin
Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia.		2.0310trihydroxyflavoneantineoplastic agent;
metabolite
calcitriol
dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes		3.6120D3 vitamins;
hydroxycalciol;
triol		antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical
alprostadil
[no description available]		9.77142prostaglandins Eanticoagulant;
human metabolite;
platelet aggregation inhibitor;
vasodilator agent
vitamin d 2
Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa.		3.6120hydroxy seco-steroid;
seco-ergostane;
vitamin D		bone density conservation agent;
nutraceutical;
plant metabolite;
rodenticide
rutin
Hydroxyethylrutoside: Monohydroxyethyl derivative of rutin. Peripheral circulation stimulant used in treatment of venous disorders.		2.3110disaccharide derivative;
quercetin O-glucoside;
rutinoside;
tetrahydroxyflavone		antioxidant;
metabolite
kaempferol
[no description available]		2.05107-hydroxyflavonol;
flavonols;
tetrahydroxyflavone		antibacterial agent;
geroprotector;
human blood serum metabolite;
human urinary metabolite;
human xenobiotic metabolite;
plant metabolite
genistein
[no description available]		2.03107-hydroxyisoflavonesantineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor
amphotericin b
Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.		3.2310antibiotic antifungal drug;
macrolide antibiotic;
polyene antibiotic		antiamoebic agent;
antiprotozoal drug;
bacterial metabolite
pulmicort
Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis.		3.612011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
cyclic acetal;
glucocorticoid;
primary alpha-hydroxy ketone		anti-inflammatory drug;
bronchodilator agent;
drug allergen
oxymetholone
Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects.		3.6120
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		3.6120dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
montelukast
montelukast: a leukotriene D4 receptor antagonist		3.6120aliphatic sulfide;
monocarboxylic acid;
quinolines		anti-arrhythmia drug;
anti-asthmatic drug;
leukotriene antagonist
mivacurium
Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent.		3.2310isoquinolines
brompheniramine maleate
brompheniramine maleate : The maleic acid salt of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810maleate saltanti-allergic agent
dexchlorpheniramine maleate
[no description available]		2.0810organic molecular entity
hemabate
carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy.		3.2310
mycophenolate mofetil
mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases.		3.6120carboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound		anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug
entacapone
entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.		3.61202-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
paricalcitol
[no description available]		3.2310hydroxy seco-steroid;
seco-cholestane		antiparathyroid drug
l 660,711
[no description available]		2.0810quinolines
travoprost
Travoprost: A cloprostenol derivative that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.. travoprost : The isopropyl ester of prostaglandin F2alpha in which the pentyl group is replaced by a 3-(trifluoromethyl)phenoxymethyl group. A synthetic analogue of prostaglandin F2alpha, ophthalmic solutions of travoprost are used as a topical medication for controlling the progression of open-angle glaucoma and ocular hypertension, by reducing intraocular pressure. It is a pro-drug; the isopropyl ester group is hydrolysed by esterases in the cornea to the biologically active free acid, fluprostenol.		2.0810(trifluoromethyl)benzenes;
isopropyl ester;
prostaglandins Falpha		antiglaucoma drug;
antihypertensive agent;
ophthalmology drug;
prodrug;
prostaglandin receptor agonist
tranilast
tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group.		2.0810amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide		anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent
7432 s
Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections.		3.2310cephalosporin;
dicarboxylic acid		antibacterial drug
imipenem
[no description available]		2.0810carbapenems
etretinate
retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.		2.0810enoate ester;
ethyl ester;
retinoid		keratolytic drug
isotretinoin
Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases.		3.6120retinoic acidantineoplastic agent;
keratolytic drug;
teratogenic agent
ketotifen fumarate
ketotifen fumarate : An organoammonium salt consisting of equimolar amounts of ketotifen(1+) and fumarate(1-) ions. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is a non-bronchodilator anti-asthmatic drug.		2.0810organoammonium saltanti-asthmatic drug;
H1-receptor antagonist
epoprostenol
[no description available]		3.2310prostaglandins Imouse metabolite
indocyanine green
[no description available]		3.23101,1-diunsubstituted alkanesulfonate;
benzoindole;
cyanine dye
dinoprost tromethamine
[no description available]		2.0810organic molecular entity
triprolidine
Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders.		3.2310N-alkylpyrrolidine;
olefinic compound;
pyridines		H1-receptor antagonist
pitavastatin
pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise.		3.2310cyclopropanes;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
quinolines;
statin (synthetic)		antioxidant
rosuvastatin calcium
S 4522: structure in first source		2.0810N-acyl-15-methylhexadecasphinganine-1-phosphoethanolamine;
organic calcium salt		anti-inflammatory agent;
cardioprotective agent;
CETP inhibitor
terbinafine hydrochloride
terbinafine hydrochloride : A hydrochloride obtained by reaction of terbinafine with one molar equivalent of hydrogen chloride.		2.0810allylamine antifungal drug;
hydrochloride		EC 1.14.13.132 (squalene monooxygenase) inhibitor;
P450 inhibitor
ethamolin
monoethanolamine oleate: used for treatment of pyogenic granuloma		3.2310long-chain fatty acid
alatrofloxacin mesylate
[no description available]		3.2310
codeine
[no description available]		3.6120morphinane alkaloid;
organic heteropentacyclic compound		antitussive;
drug allergen;
environmental contaminant;
opioid analgesic;
opioid receptor agonist;
prodrug;
xenobiotic
cyclosporine
ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF		3.6120homodetic cyclic peptideanti-asthmatic drug;
anticoronaviral agent;
antifungal agent;
antirheumatic drug;
carcinogenic agent;
dermatologic drug;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
geroprotector;
immunosuppressive agent;
metabolite
natamycin
[no description available]		2.0810antibiotic antifungal drug;
dicarboxylic acid monoester;
epoxide;
macrolide antibiotic;
monosaccharide derivative;
polyene antibiotic		antifungal agrochemical;
antimicrobial food preservative;
apoptosis inducer;
bacterial metabolite;
ophthalmology drug
acitretin
Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9.		3.6120acitretin;
alpha,beta-unsaturated monocarboxylic acid;
retinoid		keratolytic drug
estropipate
estropipate: used therapeutically in menopausal patients		3.2310piperazinium salt;
steroid sulfate
hydromorphone
Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class.		3.2310morphinane alkaloid;
organic heteropentacyclic compound		mu-opioid receptor agonist;
opioid analgesic
levetiracetam
Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine.		3.930pyrrolidin-2-onesanticonvulsant;
environmental contaminant;
xenobiotic
ly 163892
loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria.		3.2310carbacephem;
zwitterion		antibacterial drug;
antimicrobial agent
nabilone
nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure		3.2310
nalmefene
nalmefene: RN given refers to 5-alpha isomer		2.0810morphinane alkaloid
naloxone
Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.		3.8830morphinane alkaloid;
organic heteropentacyclic compound;
tertiary alcohol		antidote to opioid poisoning;
central nervous system depressant;
mu-opioid receptor antagonist
oxycodone
Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain.		3.2310organic heteropentacyclic compound;
semisynthetic derivative		antitussive;
mu-opioid receptor agonist;
opioid analgesic
oxymorphone
Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092)		3.2310morphinane alkaloid
vitamin k 1
Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones.		3.2310phylloquinones;
vitamin K		cofactor;
human metabolite;
plant metabolite
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		4.1140antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
topiramate
Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine.		3.6120cyclic ketal;
ketohexose derivative;
sulfamate ester		anticonvulsant;
sodium channel blocker
trospium chloride
trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder.		3.2310
brefeldin a
[no description available]		2.0310macrolide antibioticPenicillium metabolite
geldanamycin
[no description available]		2.03101,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound		antimicrobial agent;
antineoplastic agent;
antiviral agent;
cysteine protease inhibitor;
Hsp90 inhibitor
morphine
Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.		3.2310morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound		anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic
demycarosylturimycin h
[no description available]		2.0810
acipimox
acipimox: lipolysis inhibitor		2.0810pyrazinecarboxylic acid
atosiban
[no description available]		2.0810oligopeptide
benzphetamine
Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity.		3.2310amphetamines;
tertiary amine		adrenergic uptake inhibitor;
appetite depressant;
dopamine uptake inhibitor;
sympathomimetic agent
bimatoprost
Bimatoprost: A cloprostenol-derived amide that is used as an ANTIHYPERTENSIVE AGENT in the treatment of OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.		2.0810monocarboxylic acid amideantiglaucoma drug;
antihypertensive agent
deamino arginine vasopressin
Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR.		3.2310heterodetic cyclic peptidediagnostic agent;
renal agent;
vasopressin receptor agonist
dexmedetomidine
[no description available]		3.2310medetomidinealpha-adrenergic agonist;
analgesic;
non-narcotic analgesic;
sedative
kallidin
Kallidin: A decapeptide bradykinin homolog cleaved from kininogen by kallikreins. It is a smooth-muscle stimulant and hypotensive agent that acts by vasodilatation.		2.0410peptide
goserelin
Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer.		3.2310organic molecular entity
iloprost
Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.. iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension.		6.3661carbobicyclic compound;
monocarboxylic acid;
secondary alcohol		platelet aggregation inhibitor;
vasodilator agent
latanoprost
Latanoprost: A prostaglandin F analog used to treat OCULAR HYPERTENSION in patients with GLAUCOMA.. latanoprost : A prostaglandin Falpha that is the isopropyl ester prodrug of latanoprost free acid. Used in the treatment of open-angle glaucoma and ocular hypertension.		2.0810isopropyl ester;
prostaglandins Falpha;
triol		antiglaucoma drug;
antihypertensive agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
prodrug
lysophosphatidic acid
lysophosphatidic acid: RN given refers to parent cpd. 1-oleoyl-sn-glycerol 3-phosphate : A 1-acyl-sn-glycerol 3-phosphate having oleoyl as the 1-O-acyl group.. lysophosphatidic acid : A member of the class of lysophosphatidic acids obtained by hydrolytic removal of one of the two acyl groups of any phosphatidic acid. A 'closed' class.		2.03101-acyl-sn-glycerol 3-phosphate
nalbuphine
Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.		3.2310organic heteropentacyclic compoundmu-opioid receptor antagonist;
opioid analgesic
nateglinide
Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.		3.6120phenylalanine derivative
vinorelbine
[no description available]		3.2310acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
silodosin
silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source		9.08136indolecarboxamide
fluvoxamine
Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder.		3.2310(trifluoromethyl)benzenes;
5-methoxyvalerophenone O-(2-aminoethyl)oxime		antidepressant;
anxiolytic drug;
serotonin uptake inhibitor
su 11248
[no description available]		3.2310monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
sulindac sulfide
sulindac sulfide: sulfated analog of indomethacin & inhibitor of prostaglandin synthesis in vitro; RN given refers to cpd without isomeric designation; structure given in first source. sulindac sulfide : An aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity.		2.0810aryl sulfide;
monocarboxylic acid;
organofluorine compound		antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug
bay 11-7082
(E)-3-tosylacrylonitrile : A nitrile that is acrylonitrile in which the hydrogen located beta,trans to the cyano group is replaced by a tosyl group. It is an inhibitor of cytokine-induced IkappaB-alpha phosphorylation in cells.		2.0310nitrile;
sulfone		apoptosis inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
non-steroidal anti-inflammatory drug;
platelet aggregation inhibitor
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.		3.8630dihydroxy monocarboxylic acid;
indoles;
organofluorine compound
molsidomine
[no description available]		2.0810ethyl ester;
morpholines;
oxadiazole;
zwitterion		antioxidant;
apoptosis inhibitor;
cardioprotective agent;
nitric oxide donor;
vasodilator agent
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid: A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)		3.4811
levorphanol
Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.		3.2310morphinane alkaloid
naltrexone
Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence.		3.6120cyclopropanes;
morphinane-like compound;
organic heteropentacyclic compound		antidote to opioid poisoning;
central nervous system depressant;
environmental contaminant;
mu-opioid receptor antagonist;
xenobiotic
dextromethorphan
Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.		3.61206-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
butorphanol
Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain.		3.6120morphinane alkaloidantitussive;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic
cefixime
[no description available]		3.6120cephalosporinantibacterial drug;
drug allergen
lisinopril
Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.		3.6120dipeptideEC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
benazepril
benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure.		3.2310benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam		EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
ramipril
Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles.		5.4941azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester		bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug
verteporfin
(2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid.		3.2310
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		3.6120dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
ethyl oleate
[no description available]		2.0510long-chain fatty acid ethyl esteracaricide;
plant metabolite
zimeldine
Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385)		3.2310styrenes
enalapril maleate
enalapril maleate : The maleic acid salt of enalapril. It contains one molecule of maleic acid for each molecule of enalapril. Following oral administration, the ethyl ester group of enalapril is hydrolysed to afford the corresponding carboxylic acid, enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor. Enalapril is thus a prodrug for enalaprilat (which, unlike enalapril, is not absorbed by mouth), and its maleate is used in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients.		2.0810maleate saltantihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		3.2310dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
trientine hydrochloride
[no description available]		3.2310
n-methylscopolamine bromide
scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide.		3.2310
bleomycin
[no description available]		3.2310bleomycinantineoplastic agent;
metabolite
enalaprilat anhydrous
Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.		3.6120dicarboxylic acid;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ximelagatran
ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage.		3.2310amidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide		anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor
cefuroxime
[no description available]		3.23103-(carbamoyloxymethyl)cephalosporin;
furans;
oxime O-ether		drug allergen
ceftriaxone
[no description available]		3.23101,2,4-triazines;
1,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 3.5.2.6 (beta-lactamase) inhibitor
cefepime
Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton.		3.2310cephalosporin;
oxime O-ether		antibacterial drug
pafuramidine
pafuramidine: a prodrug of furamidine		3.2310
ceftazidime
[no description available]		3.2310cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
trandolapril
trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension.		3.6120dicarboxylic acid monoester;
dipeptide;
ethyl ester;
organic heterobicyclic compound;
secondary amino compound;
tertiary carboxamide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug
pregabalin
Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues.		3.9130gamma-amino acidanticonvulsant;
calcium channel blocker
alvimopan anhydrous
alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain		3.6120peptide
baohuoside i
baohuoside I: structure given in first source; isolated from the herb Epimedium davidii		3.3110glycosyloxyflavoneanti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite
aliskiren
aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.		3.2310monocarboxylic acid amide;
monomethoxybenzene		antihypertensive agent
famotidine
[no description available]		3.61201,3-thiazoles;
guanidines;
sulfonamide		anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
abscisic acid
Abscisic Acid: Abscission-accelerating plant growth substance isolated from young cotton fruit, leaves of sycamore, birch, and other plants, and from potatoes, lemons, avocados, and other fruits.. (S)-2-trans-abscisic acid : A 2-trans-abscisic acid with (S)-configuration at the chiral centre.. (+)-abscisic acid : The naturally occurring (1'S)-(+) enantiomer of abscisic acid. It is an important sesquiterpenoid plant hormone which acts as a regulator of plant responses to environmental stresses such as drought and cold.		2.05102-trans-abscisic acid
cefotaxime
Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.		3.23101,3-thiazoles;
cephalosporin;
oxime O-ether		antibacterial drug;
drug allergen
aztreonam
[no description available]		3.2310beta-lactam antibiotic allergen;
monobactam		antibacterial drug;
drug allergen;
EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor
cci 15641
[no description available]		2.0810cephalosporin
tetrodotoxin
Tetrodotoxin: An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.. tetrodotoxin : A quinazoline alkaloid that is a marine toxin isolated from fish such as puffer fish. It has been shown to exhibit potential neutotoxicity due to its ability to block voltage-gated sodium channels.		2.4520azatetracycloalkane;
oxatetracycloalkane;
quinazoline alkaloid		animal metabolite;
bacterial metabolite;
marine metabolite;
neurotoxin;
voltage-gated sodium channel blocker
cefpodoxime
[no description available]		3.2310carboxylic acid;
cephalosporin		antibacterial drug
palonosetron
Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.		3.2310azabicycloalkane;
delta-lactam;
organic heterotricyclic compound		antiemetic;
serotonergic antagonist
tenofovir disoproxil fumarate
tenofovir disoproxil fumarate : A fumarate salt prepared from equimolar amounts of tenofovir disoproxil and fumaric acid. It is used in combination therapy for the treatment of HIV infection.		2.0810fumarate saltantiviral drug;
HIV-1 reverse transcriptase inhibitor;
prodrug
dexbrompheniramine maleate
dexbrompheniramine maleate : The maleic acid salt of the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis.		2.0810brompheniramine maleateanti-allergic agent;
H1-receptor antagonist
rifaximin
[no description available]		3.6120acetate ester;
cyclic ketal;
lactam;
macrocycle;
organic heterohexacyclic compound;
rifamycins;
semisynthetic derivative		antimicrobial agent;
gastrointestinal drug;
orphan drug
everolimus
[no description available]		3.6120cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol		anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
ixabepilone
[no description available]		3.23101,3-thiazoles;
beta-hydroxy ketone;
epoxide;
lactam;
macrocycle		antineoplastic agent;
microtubule-destabilising agent
rilpivirine
[no description available]		8.5111aminopyrimidine;
nitrile		EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor
tanespimycin
CP 127374: analog of herbimycin A		2.03101,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound;
secondary amino compound		antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor
gw 1929
GW 1929: activates peroxisome proliferator-activated receptor-gamma; structure in first source		2.0310benzophenones
cefpodoxime proxetil
cefpodoxime proxetil: structure given in first source; prodrug for cefpodoxime. cefpodoxime proxetil : The 1-[(isopropoxycarbonyl)oxy]ethyl (proxetil) ester prodrug of cefpodoxime. After swallowing, hydrolysis of the ester group occurs in the intestinal epithelium, to release active cefpodoxime in the bloodstream. It is used to treat acute otitis media, pharyngitis, and sinusitis.		2.0810carboxylic acid;
carboxylic ester;
cephalosporin		antibacterial drug;
prodrug
ceftizoxime
[no description available]		3.2310cephalosporinantibacterial drug
2-[(3-iodophenyl)methylthio]-5-pyridin-4-yl-1,3,4-oxadiazole
[no description available]		2.0310aryl sulfide
1-methyl-d-lysergic acid butanolamide
[no description available]		3.2310ergot alkaloid;
monocarboxylic acid amide		serotonergic antagonist;
sympatholytic agent;
vasoconstrictor agent
paclobutrazol
paclobutrazol: RN given refers to (R*,R*)-(+-)-isomer. paclobutrazol : A racemate comprising equimolar amounts of (2R,3R)- and (2S,3S)-1-(4-chlorophenyl)-4,4-dimethyl-2-(1H-1,2,4-triazol-1-yl)pentan-3-ol. It acts as a plant-growth retardant and fungicide via inhibition of gibberellin biosynthesis.		2.0510
fluphenazine
[no description available]		2.0810
nitrofurantoin
Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA.		3.6120imidazolidine-2,4-dione;
nitrofuran antibiotic;
organonitrogen heterocyclic antibiotic;
organooxygen heterocyclic antibiotic		antibacterial drug;
antiinfective agent;
hepatotoxic agent
tubacin
tubacin: inhibits histone deacetylase 6; structure in first source		2.17101,3-oxazoles
butylscopolammonium bromide
Butylscopolammonium Bromide: Antimuscarinic quaternary ammonium derivative of scopolamine used to treat cramps in gastrointestinal, urinary, uterine, and biliary tracts, and to facilitate radiologic visualization of the gastrointestinal tract.		4.4330
dantrolene
[no description available]		3.2310
roxithromycin
(E)-roxithromycin : A major geometrical isomer of roxithromycin.		2.0810roxithromycinenvironmental contaminant;
xenobiotic
cefdinir
[no description available]		3.6120cephalosporin;
ketoxime		antibacterial drug
etonogestrel
[no description available]		3.231017beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
terminal acetylenic compound		contraceptive drug;
female contraceptive drug;
progestin
bisoprolol, fumarate (1:1) salt
[no description available]		2.0810
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		2.0810artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
ci 940
leptomycin : A complex, very long chain, polyunsaturated fatty acid whose core structure comprises 8-oxononadeca-2,10,12,16,18-pentaenoic acid having methyl substituents at positions 3, 5, 7, 9, 11 and 15 and a 3,6-dihydropyran-6-one-2-yl group at position 19.		2.0310hydroxy polyunsaturated fatty acid;
leptomycin		antifungal agent;
bacterial metabolite
beraprost
beraprost: stable prostacyclin analog; structure given in first source. beraprost : An organic heterotricyclic compound that is (3aS,8bS)-2,3,3a,8b-tetrahydro-1H-benzo[b]cyclopenta[d]furan in which the hydrogens at positions 1R, 2R and 5 are replaced by (3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl, hydroxy and 3-carboxypropyl groups, respectively. It is a prostaglandin receptor agonist which is approved to treat pulmonary arterial hypertension in Asia.		4.3150enyne;
monocarboxylic acid;
organic heterotricyclic compound;
secondary alcohol;
secondary allylic alcohol		anti-inflammatory agent;
antihypertensive agent;
platelet aggregation inhibitor;
prostaglandin receptor agonist;
vasodilator agent
etoposide phosphate
[no description available]		2.0810furonaphthodioxole
u 62840
U 62840: stereoisomeric benzindene prostaglandin analog; structure given in first source		7.27111carbotricyclic compound;
carboxylic acid		antihypertensive agent;
cardiovascular drug;
human blood serum metabolite;
platelet aggregation inhibitor;
vasodilator agent;
vitamin K antagonist
ciclesonide
ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis		2.0810organic molecular entity
flibanserin
[no description available]		7.110benzimidazoles;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound		antidepressant;
serotonergic agonist;
serotonergic antagonist
temsirolimus
[no description available]		3.6120macrolide lactam
dutasteride
Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland.		6.0771(trifluoromethyl)benzenes;
aza-steroid;
delta-lactam		antihyperplasia drug;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
tekturna
[no description available]		2.0810fumarate saltantihypertensive agent
lu 208075
ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension		14.854816diarylmethane
bibx 1382bs
BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001		3.2310substituted aniline
vildagliptin
[no description available]		2.0810amino acid amide
indacaterol
indacaterol: a beta2 adrenoceptor agonist; indacaterol is the (R)-isomer; structure in first source. indacaterol : A monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary disease.		2.0810indanes;
monohydroxyquinoline;
quinolone;
secondary alcohol;
secondary amino compound		beta-adrenergic agonist;
bronchodilator agent
fesoterodine
fesoterodine: a muscarinic antagonist for treatment of overactive bladder		10.0121diarylmethane
panobinostat
Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA.. panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma.		2.1310cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound		angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
sgd 301-76
[no description available]		2.0810conazole antifungal drug;
imidazole antifungal drug;
organic nitrate salt		antiinfective agent
fluvoxamine maleate
[no description available]		2.0810(trifluoromethyl)benzenes
thioacetazone
Thioacetazone: A thiosemicarbazone that is used in association with other antimycobacterial agents in the initial and continuation phases of antituberculosis regimens. Thiacetazone containing regimens are less effective than the short-course regimen recommended by the International Union Against Tuberculosis and are used in some developing countries to reduce drug costs. (From Martindale, The Extra Pharmacopoeia, 30th ed, p217). thiosemicarbazone : A hydrazone resulting from the formal condensation of an aldehyde or ketone with the non-thioacylated nitrogen of thiosemicarbazide or its substituted derivatives.		2.0810
gemifloxacin
Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position.		3.23101,8-naphthyridine derivative;
fluoroquinolone antibiotic;
monocarboxylic acid;
quinolone antibiotic		antibacterial drug;
antimicrobial agent;
topoisomerase IV inhibitor
dexlansoprazole
Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE.		3.6120benzimidazoles;
sulfoxide
gemifloxacin mesylate
gemifloxacin mesylate : The mesylate salt of gemifloxacin.		2.0810methanesulfonate saltantimicrobial agent;
topoisomerase IV inhibitor
fosinopril
[no description available]		3.2310
armodafinil
armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.		3.23102-[(diphenylmethyl)sulfinyl]acetamidecentral nervous system stimulant;
eugeroic
bay 58-2667
BAY 58-2667: activates guanylyl cyclase; structure in first source. cinaciguat : A benzoic acid that is 4-(aminomethyl)benzoic acid in which the amino group is substituted by 4-carboxybutyl and 2-(2-{[4-(2-phenylethyl)benzyl]oxy}phenyl)ethyl groups. It is a soluble guanylate cyclase activator, used for the treatment of acute decompensated heart failure.		2.9830aromatic ether;
benzoic acids;
dicarboxylic acid;
tertiary amino compound		antihypertensive agent;
soluble guanylate cyclase activator;
vasodilator agent
sincalide
Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.		3.2310oligopeptide
tapentadol
Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES.		3.2310alkylbenzene
brl 37344
BRL 37344: SB 206606 is the (R,R)-isomer		2.5920monocarboxylic acid
pentagastrin
Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.		3.2310organic molecular entity
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		2.7930aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
mirabegron
mirabegron: a beta3-adrenergic receptor agonist; structure in first source. mirabegron : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2-amino-1,3-thiazol-4-ylacetic acid with the anilino group of (1R)-2-{[2-(4-aminophenyl)ethyl]amino}-1-phenylethanol. Used for the treatment of overactive bladder syndrome.		7.03421,3-thiazoles;
aromatic amide;
ethanolamines;
monocarboxylic acid amide		beta-adrenergic agonist
avanafil
[no description available]		5.09120aromatic amide;
monocarboxylic acid amide;
organochlorine compound;
prolinols;
pyrimidines		EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
cefditoren
cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections.		3.2310carboxylic acid;
cephalosporin		antibacterial drug
scio-469
SCIO-469: a small-molecule p38 mitogen-activated protein (MAP) kinase inhibitor for potential oral therapy for inflammatory disorders; in phase lib clinical trials for rheumatoid arthritis 4/2004. talmapimod : An indolecarboxamide obtained by formal condensation of the carboxy group of 6-chloro-3-[(dimethylamino)(oxo)acetyl]-1-methylindole-5-carboxylic acid with the secondary amino group of (2S,5R)-1-[(4-fluorophenyl)methyl]-2,5-dimethylpiperazine. It is a potent inhibitor of MAPK and exhibits anti-cancer properties.		3.2710aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
ticagrelor
Ticagrelor: An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION.. ticagrelor : A triazolopyrimidine that is an adenosine isostere; the cyclopentane ring is similar to ribose and the nitrogen-rich [1,2,3]triazolo[4,5-d]pyrimidine moiety resembles the nucleobase adenine. A platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome.		2.0810aryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines		P2Y12 receptor antagonist;
platelet aggregation inhibitor
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		2.0810aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
selexipag
selexipag: prostacyclin receptor agonist. selexipag : A member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid).		5.8132aromatic amine;
ether;
monocarboxylic acid amide;
N-sulfonylcarboxamide;
pyrazines;
tertiary amino compound		orphan drug;
platelet aggregation inhibitor;
prodrug;
prostacyclin receptor agonist;
vasodilator agent
hki 272
[no description available]		2.0810nitrile;
quinolines		antineoplastic agent;
tyrosine kinase inhibitor
tofacitinib
tofacitinib : A pyrrolopyrimidine that is pyrrolo[2,3-d]pyrimidine substituted at position 4 by an N-methyl,N-(1-cyanoacetyl-4-methylpiperidin-3-yl)amino moiety. Used as its citrate salt to treat moderately to severely active rheumatoid arthritis.		2.0810N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound		antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
pifithrin-alpha
[no description available]		2.0310
l 706000
L 706000: a spirobenzopyran piperidine; structure given in first source		2.0410
roflumilast n-oxide
roflumilast N-oxide: an oral, once-daily phosphodiesterase 4 inhibitor; active metabolite of roflumilast		7.1710
osu 03012
OSU 03012: a PDK-1 inhibitor; structure in first source		2.5120antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles		antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
pazopanib
pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.		3.6120aminopyrimidine;
indazoles;
sulfonamide		angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
tribulus
Tribulus: A plant genus of the family ZYGOPHYLLACEAE. Members contain steroidal saponins. Ingestion by grazing animals causes PHOTOSENSITIVITY DISORDERS called geeldikkop (yellow thick head) in South Africa.		3.4611
prasugrel hydrochloride
Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels.		3.2310
heptakis(2,6-o-dimethyl)beta-cyclodextrin
heptakis(2,6-O-dimethyl)beta-cyclodextrin: stimulant for Bordetella pertussis Phase I		2.0410
aminotadalafil
aminotadalafil: structure in first source		2.9840
apixaban
[no description available]		2.0810aromatic ether;
lactam;
piperidones;
pyrazolopyridine		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
amg 009
AMG 009: an anti-inflammatory agent; structure in first source		2.0810
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		3.1450
cefotaxime sodium
[no description available]		2.0810organic sodium salt
baci-im
[no description available]		3.2310homodetic cyclic peptide;
polypeptide;
zwitterion		antibacterial agent;
antimicrobial agent
n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide
N-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide: MK-0364 is the (1S,2S)-isomer; a cannabinoid-1 receptor inverse agonist; structure in first source		2.0810stilbenoid
bms 477118
[no description available]		3.2310adamantanes;
azabicycloalkane;
monocarboxylic acid amide;
nitrile;
tertiary alcohol		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent
nystatin a1
Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.		3.2310nystatins
bay 63-2521
riociguat: guanylate cyclase stimulator; structure in first source. riociguat : A carbamate ester that is the methyl ester of {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamic acid. It is used for treatment of chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension		2.5720aminopyrimidine;
carbamate ester;
organofluorine compound;
pyrazolopyridine		antihypertensive agent;
soluble guanylate cyclase activator
quisinostat
[no description available]		2.1310indoles
apremilast
[no description available]		2.0810aromatic ether;
N-acetylarylamine;
phthalimides;
sulfone		non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor
pf-2545920
[no description available]		3.5110
milnacipran
[no description available]		3.2310acetamides
losartan potassium
Erythropoietin: Glycoprotein hormone, secreted chiefly by the KIDNEY in the adult and the LIVER in the FETUS, that acts on erythroid stem cells of the BONE MARROW to stimulate proliferation and differentiation.		2.5120
technetium tc 99m exametazime
Technetium Tc 99m Exametazime: A gamma-emitting RADIONUCLIDE IMAGING agent used in the evaluation of regional cerebral blood flow and in non-invasive dynamic biodistribution studies and MYOCARDIAL PERFUSION IMAGING. It has also been used to label leukocytes in the investigation of INFLAMMATORY BOWEL DISEASES.		3.4811
(2R,3S)-EHNA hydrochloride
(2R,3S)-EHNA hydrochloride : A hydrochloride salt obtained by reaction of (2R,3S)-EHNA with one equivalent of hydrochloric acid. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase.		3.5110hydrochlorideEC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor
scopolamine hydrobromide
[no description available]		4.2440
dactolisib
dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.		2.0810imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas		antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor
rabeprazole sodium
[no description available]		2.0810organic sodium salt
macitentan
[no description available]		9.46133aromatic ether;
organobromine compound;
pyrimidines;
ring assembly;
sulfamides		antihypertensive agent;
endothelin receptor antagonist;
orphan drug
bivalirudin
bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant.		3.6120polypeptideanticoagulant;
EC 3.4.21.5 (thrombin) inhibitor
somatostatin
[no description available]		2.0810heterodetic cyclic peptide;
peptide hormone
atrial natriuretic factor
Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.		2.1310polypeptide
enfuvirtide
Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes.		3.2310
ganirelix
[no description available]		3.2310polypeptide
glucagon
Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.		2.110peptide hormone
neuropeptide y
Neuropeptide Y: A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones.		2.1310
teriparatide
[no description available]		3.2310polypeptide
salmon calcitonin
[no description available]		3.2310heterodetic cyclic peptide;
peptide hormone;
polypeptide		bone density conservation agent;
metabolite
irl 1620
sovateltide: a potent, specific ligand for the endothelin-B receptor		2.0310
ly-146032
[no description available]		3.6120heterodetic cyclic peptide;
lipopeptide antibiotic;
lipopeptide;
macrocycle;
macrolide		antibacterial drug;
bacterial metabolite;
calcium-dependent antibiotics
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide
acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt		3.2310polypeptide
exenatide
[no description available]		3.2310
natriuretic peptide, c-type
Natriuretic Peptide, C-Type: A PEPTIDE of 22 amino acids, derived mainly from cells of VASCULAR ENDOTHELIUM. It is also found in the BRAIN, major endocrine glands, and other tissues. It shares structural homology with ATRIAL NATRIURETIC FACTOR. It has vasorelaxant activity thus is important in the regulation of vascular tone and blood flow. Several high molecular weight forms containing the 22 amino acids have been identified.		3.9521
warfarin sodium
warfarin sodium : A racemate comprising equal amounts of (R)- and (S)-warfarin sodium. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.		2.0810
endothelin-1
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)		4.3541
lumacaftor
lumacaftor: a corrector of CF transmembrane conductance regulator (CTFR); structure in first source. lumacaftor : An aromatic amide obtained by formal condensation of the carboxy group of 1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropane-1-carboxylic acid with the aromatic amino group of 3-(6-amino-3-methylpyridin-2-yl)benzoic acid. Used for the treatment of cystic fibrosis.		2.3110aromatic amide;
benzodioxoles;
benzoic acids;
cyclopropanes;
organofluorine compound;
pyridines		CFTR potentiator;
orphan drug
pravastatin sodium
pravastatin sodium : An organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.		2.0810organic sodium salt;
statin (semi-synthetic)		anticholesteremic drug
alendronate sodium
[no description available]		2.0810
sl 80.0750
[no description available]		2.0810
chitosan
[no description available]		9.0221
mesna
Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE.		3.6120organosulfonic acid
sodium oxybate
Sodium Oxybate: The sodium salt of 4-hydroxybutyric acid. It is used for both induction and maintenance of ANESTHESIA.		2.2110
clavulanate potassium
potassium clavulanate : A potassium salt having clavulanate as the counterion. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes and has only weak anitbiotic activity when administered alone. However it can be used in combination with amoxicillin trihydrate (under the trade name Augmentin) for treatment of a variety of bacterial infections, where it prevents antibiotic inactivation by microbial lactamases.		2.0810potassium saltantibacterial drug;
antimicrobial agent;
EC 3.5.2.6 (beta-lactamase) inhibitor
sodium lactate
Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion.		3.2310lactate salt;
organic sodium salt		food acidity regulator;
food preservative
piperacillin sodium
[no description available]		2.0810organic sodium salt
sodium iothalamate
[no description available]		3.2310
oxacillin sodium
[no description available]		2.0810organic sodium salt
cefazolin sodium
cefazolin sodium : A cephalosporin organic sodium salt having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups.		2.0810organic sodium salt
ro13-9904
Ceftriaxone: A broad-spectrum cephalosporin antibiotic and cefotaxime derivative with a very long half-life and high penetrability to meninges, eyes and inner ears.. ceftriaxone : A third-generation cephalosporin compound having 2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetylamino and [(2-methyl-5,6-dioxo-1,2,5,6-tetrahydro-1,2,4-triazin-3-yl)sulfanyl]methyl side-groups.		2.0610
azlocillin sodium
[no description available]		2.0810organic sodium salt
canagliflozin
canagliflozin hydrate : A hydrate that is the hemihydrate form of canagliflozin. Used for treatment of type II diabetes via inhibition of sodium-glucose transport protein subtype 2.		7.4110C-glycosyl compound;
organofluorine compound;
thiophenes		hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor
cardiovascular agents
Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.		2.4620
cetrorelix
cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast.		3.2310oligopeptideantineoplastic agent;
GnRH antagonist
incb-018424
[no description available]		2.0810nitrile;
pyrazoles;
pyrrolopyrimidine		antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
bms-790052
daclatasvir: an HCV NS5A inhibitor. daclatasvir : A member of the class of biphenyls that is a potent inhibitor of nonstructural protein 5A and is used (as its hydrochloride salt) for treatment of hepatitis C.		3.2710biphenyls;
carbamate ester;
carboxamide;
imidazoles;
valine derivative		antiviral drug;
nonstructural protein 5A inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		2.0510
interleukin-8
Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.		4.4622
azd3839
AZD3839: a BACE1 inhibitor; structure in first source		3.2710
abt-199
venetoclax: A BCL-2 inhibitor with antineoplastic activity that is used in the treatment of CHRONIC LYMPHOCYTIC LEUKEMIA associated with chromosome 17p deletion; structure in first source.. venetoclax : A member of the class of pyrrolopyridines that is a potent inhibitor of the antiapoptotic protein B-cell lymphoma 2. It is used for treamtment of chronic lymphocytic leukemia with 17p deletion.		3.2710aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine		antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor
tubastatin a
[no description available]		2.1710hydroxamic acid;
pyridoindole;
tertiary amino compound		EC 3.5.1.98 (histone deacetylase) inhibitor
natriuretic peptide, brain
Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.		9.25126polypeptide
acy-1215
ricolinostat: an HDAC6 inhibitor; structure in first source		2.1710pyrimidinecarboxylic acid
ass234
[no description available]		3.3110
ascorbic acid
Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.		3.2310ascorbic acid;
vitamin C		coenzyme;
cofactor;
flour treatment agent;
food antioxidant;
food colour retention agent;
geroprotector;
plant metabolite;
skin lightening agent
raltegravir
[no description available]		4.16201,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide		antiviral drug;
HIV-1 integrase inhibitor
tetracycline
Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.		3.6120
oxytetracycline, anhydrous
Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae.		3.2310
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		3.2310
piroxicam
[no description available]		3.9130benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
roquinimex
roquinimex: structure in first source		2.0810aromatic amide
acenocoumarol
Acenocoumarol: A coumarin that is used as an anticoagulant. Its actions and uses are similar to those of WARFARIN. (From Martindale, The Extra Pharmacopoeia, 30th ed, p233). acenocoumarol : A hydroxycoumarin that is warfarin in which the hydrogen at position 4 of the phenyl substituent is replaced by a nitro group.		2.0510C-nitro compound;
hydroxycoumarin;
methyl ketone		anticoagulant;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor
mobic
Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis.		3.61201,3-thiazoles;
benzothiazine;
monocarboxylic acid amide		analgesic;
antirheumatic drug;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
mobiflex
tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries.		2.0810heteroaryl hydroxy compound;
monocarboxylic acid amide;
pyridines;
thienothiazine		antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
isoxicam
isoxicam : A monocarboxylic acid amide that is piroxicam in which the pyrid-2-yl group is replaced by a 5-methyl-1,2-oxazol-3-yl group. A non-steroidal anti-inflammatory drug, it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome.		2.0810benzothiazine;
isoxazoles;
monocarboxylic acid amide		antirheumatic drug;
non-steroidal anti-inflammatory drug
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		4.4430benzenes;
hydroxycoumarin;
methyl ketone
demeclocycline
Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective.		3.2310
tipranavir
tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor.		9.9821sulfonamideantiviral drug;
HIV protease inhibitor
minocycline hydrochloride
[no description available]		2.0810
tigecycline
[no description available]		3.6120
(S)-warfarin
(S)-warfarin : A 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-1-benzopyran-2-one that has (S)-configuration (the racemate is warfarin, an anticoagulant drug and rodenticide).		2.08104-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one
lornoxicam
lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations.		2.0810heteroaryl hydroxy compound;
monocarboxylic acid amide;
organochlorine compound;
pyridines;
thienothiazine		antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug
a 769662
[no description available]		3.2710biphenyls
dolutegravir
[no description available]		3.2710difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide		HIV-1 integrase inhibitor
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		4.5260
d159687
[no description available]		3.2710
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.0810
fertinex
[no description available]		3.2310
hyaluronoglucosaminidase
Hyaluronoglucosaminidase: An enzyme that catalyzes the random hydrolysis of 1,4-linkages between N-acetyl-beta-D-glucosamine and D-glucuronate residues in hyaluronate. (From Enzyme Nomenclature, 1992) There has been use as ANTINEOPLASTIC AGENTS to limit NEOPLASM METASTASIS.		2.3110
gibberellins
[no description available]		2.0510
carboxymethyl-beta-cyclodextrin
[no description available]		2.1110
entecavir
entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B.		3.61202-aminopurines;
oxopurine;
primary alcohol;
secondary alcohol		antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
acyclovir
Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.		3.61202-aminopurines;
oxopurine		antimetabolite;
antiviral drug
cyclic gmp
Cyclic GMP: Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed). 3',5'-cyclic GMP : A 3',5'-cyclic purine nucleotide in which the purine nucleobase is specified as guanidine.		18.428763',5'-cyclic purine nucleotide;
guanyl ribonucleotide		Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
guanosine monophosphate
Guanosine Monophosphate: A guanine nucleotide containing one phosphate group esterified to the sugar moiety and found widely in nature.. guanosine 5'-monophosphate : A purine ribonucleoside 5'-monophosphate having guanine as the nucleobase.		4.4320guanosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate		biomarker;
Escherichia coli metabolite;
metabolite;
mouse metabolite
folic acid
folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin.		10.8331folic acids;
N-acyl-amino acid		human metabolite;
mouse metabolite;
nutrient
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		3.6120cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
clozapine
Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.		4.0940benzodiazepine;
N-arylpiperazine;
N-methylpiperazine;
organochlorine compound		adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
environmental contaminant;
GABA antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
xenobiotic
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		3.6120dacarbazine
didanosine
Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS.		3.6120purine 2',3'-dideoxyribonucleosideantimetabolite;
antiviral drug;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor;
geroprotector;
HIV-1 reverse transcriptase inhibitor
ganciclovir
[no description available]		3.61202-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
valtrex
[no description available]		2.0810organic molecular entity
valacyclovir
Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES.		3.2310L-valyl esterantiviral drug
sildenafil
sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position.		12240piperazines;
pyrazolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
olanzapine
Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.		3.8630benzodiazepine;
N-arylpiperazine;
N-methylpiperazine		antiemetic;
dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
second generation antipsychotic;
serotonergic antagonist;
serotonin uptake inhibitor
zaprinast
zaprinast: anaphylaxis inhibitor; structure		5.990triazolopyrimidines
raltitrexed
[no description available]		2.0810N-acyl-amino acid
vardenafil
vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine.		10.95130imidazotriazine;
N-alkylpiperazine;
N-sulfonylpiperazine		EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
Imidazosagatriazinone
[no description available]		2.0410pyrazolopyrimidine
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		4.4130nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
citrovorum factor
[no description available]		3.6120tetrahydrofolic acid
leucovorin
5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5.		3.2310formyltetrahydrofolic acidEscherichia coli metabolite;
mouse metabolite
rifapentine
rifapentine: cyclopentyl derivative of rifampicin		3.6120N-alkylpiperazine;
N-iminopiperazine;
rifamycins		antitubercular agent;
leprostatic drug
bl 4162a
anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions.		3.2310imidazoquinazolineanticoagulant;
antifibrinolytic drug;
cardiovascular drug;
platelet aggregation inhibitor
tegaserod
tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source		3.2310carboxamidine;
guanidines;
hydrazines;
indoles		gastrointestinal drug;
serotonergic agonist
norclozapine
norclozapine: structure given in first source. N-desmethylclozapine : A dibenzodoazepine substituted with chloro and piperazino groups which is a major metabolite of clozapine; a potent and selective 5-HT2C serotonin receptor antagonist.		2.0810dibenzodiazepine;
organochlorine compound;
piperazines		delta-opioid receptor agonist;
metabolite;
serotonergic antagonist
pemetrexed
pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT).		3.2310N-acyl-L-glutamic acid;
pyrrolopyrimidine		antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
sildenafil citrate
Sildenafil Citrate: A PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.. sildenafil citrate : The citrate salt of sildenafil.		20.9343438citrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
valganciclovir
Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine.		3.2310L-valyl ester;
purines		antiviral drug;
prodrug
aprepitant
Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors.		3.6120(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
triazoles		antidepressant;
antiemetic;
neurokinin-1 receptor antagonist;
peripheral nervous system drug;
substance P receptor antagonist
fosaprepitant
fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid.		3.2310(trifluoromethyl)benzenes;
cyclic acetal;
morpholines;
phosphoramide;
triazoles		antiemetic;
neurokinin-1 receptor antagonist;
prodrug
tegaserod maleate
[no description available]		2.0810maleate saltserotonergic agonist
da 8159
udenafil: a pyrazolo-pyrimidinone similar to sildenafil; phosphodiesterase type 5 inhibitor;		8.6471sulfonamide
vardenafil dihydrochloride
Vardenafil Dihydrochloride: A piperazine derivative, PHOSPHODIESTERASE 5 INHIBITOR and VASODILATOR AGENT that is used as a UROLOGICAL AGENT in the treatment of ERECTILE DYSFUNCTION.		18.4925612
rifabutin
[no description available]		3.6120
lodenafil carbonate
lodenafil carbonate: structure in first source		2.0810
8-hydroxy-2'-deoxyguanosine
8-Hydroxy-2'-Deoxyguanosine: Common oxidized form of deoxyguanosine in which C-8 position of guanine base has a carbonyl group.. 8-hydroxy-2'-deoxyguanosine : Guanosine substituted at the purine 8-position by a hydroxy group. It is used as a biomarker of oxidative DNA damage.		3.6411guanosinesbiomarker
desmethylolanzapine
desmethylolanzapine: structure in first source		2.0410benzodiazepine
mirodenafil
mirodenafil: an erectogenic agent; structure in first source. mirodenafil : A member of the class of pyrrolopyrimidines that is 3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one having a 5-{[4-(2-hydroxyethyl)piperazin-1-yl]sulfonyl}-2-propoxyphenyl group at positon 2, ethyl group at position 5, and a propyl group at position 7. It is a phosphodiesterase type 5 inhibitor which is used for the treatment of erectile dysfunction.		3.1610aromatic ether;
N-alkylpiperazine;
primary alcohol;
pyrrolopyrimidine;
sulfonamide		EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
levomefolate calcium
levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid.		3.2310organic calcium saltantidepressant
6-((3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo(3,4-d)pyrimidin-4-one
[no description available]		3.5110
bay 60-7550
[no description available]		4.120
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		3.8330
ConditionIndicatedRelationship StrengthStudiesTrials
Impotence
[description not available]		030.03747190
Erectile Dysfunction
The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.		129.81,494380
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		03.91120
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		09.2852
Cancer of Colon
[description not available]		02.830
Colonic Neoplasms
Tumors or cancer of the COLON.		02.830
Innate Inflammatory Response
[description not available]		06.23113
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		011.23113
Acute Liver Injury, Drug-Induced
[description not available]		03.730
Adverse Drug Event
[description not available]		06.993
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		03.730
Drug-Related Side Effects and Adverse Reactions
Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.		06.993
Acute Confusional Senile Dementia
[description not available]		06.63220
Alzheimer Disease
A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)		06.63220
Anemia, Fanconi
[description not available]		02.1310
Fanconi Anemia
Congenital disorder affecting all bone marrow elements, resulting in ANEMIA; LEUKOPENIA; and THROMBOPENIA, and associated with cardiac, renal, and limb malformations as well as dermal pigmentary changes. Spontaneous CHROMOSOME BREAKAGE is a feature of this disease along with predisposition to LEUKEMIA. There are at least 7 complementation groups in Fanconi anemia: FANCA, FANCB, FANCC, FANCD1, FANCD2, FANCE, FANCF, FANCG, and FANCL. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227650, August 20, 2004)		02.1310
Cancer of Prostate
[description not available]		012.723316
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		012.723316
Pulmonary Hypertension
[description not available]		018.8116139
Hypertension, Pulmonary
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.		123.5632278
Cognitive Decline
[description not available]		04.641
Cognitive Dysfunction
Diminished or impaired mental and/or intellectual function.		09.641
Congenital Zika Syndrome
[description not available]		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Astrocytoma, Grade IV
[description not available]		02.9130
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		14.9130
Hepatocellular Carcinoma
[description not available]		03.4350
Cancer of Liver
[description not available]		03.2540
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		03.4350
Liver Neoplasms
Tumors or cancer of the LIVER.		03.2540
Pulmonary Arterial Hypertension
A progressive rare pulmonary disease characterized by high blood pressure in the PULMONARY ARTERY.		115.593413
2019 Novel Coronavirus Disease
[description not available]		06.2531
Lower Urinary Tract Symptom
[description not available]		019.0914359
Adenoma, Prostatic
[description not available]		019.6317876
Nycturia
[description not available]		04.2731
Prostatic Hyperplasia
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.		121.6317876
Nocturia
Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS).		04.2731
Pulmonary Veno Occlusive Disease
[description not available]		03.4320
Pulmonary Veno-Occlusive Disease
Pathological process resulting in the fibrous obstruction of the small- and medium-sized PULMONARY VEINS and PULMONARY HYPERTENSION. Veno-occlusion can arise from fibrous proliferation of the VASCULAR INTIMA and VASCULAR MEDIA; THROMBOSIS; or a combination of both.		03.4320
Ejaculatio Praecox
[description not available]		06.2584
Premature Ejaculation
The emission of SEMEN and seminal fluid during the act of preparation for sexual intercourse, i.e. before there is penetration, or shortly after penetration.		06.2584
Cirrhosis, Liver
[description not available]		05.5751
Liver Cirrhosis
Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.		05.5751
Blood Pressure, High
[description not available]		011.15295
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		113.15295
HPV Infection
[description not available]		04.7211
Carcinoma, Squamous Cell of Head and Neck
[description not available]		07.0743
Cancer of Head
[description not available]		07.2753
Squamous Cell Carcinoma of Head and Neck
The most common type of head and neck carcinoma that originates from cells on the surface of the NASAL CAVITY; MOUTH; PARANASAL SINUSES, SALIVARY GLANDS, and LARYNX. Mutations in TNFRSF10B, PTEN, and ING1 genes are associated with this cancer.		07.0743
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		19.2753
Papillomavirus Infections
Neoplasms of the skin and mucous membranes caused by papillomaviruses. They are usually benign but some have a high risk for malignant progression.		04.7211
Symptom Cluster
[description not available]		05.1652
Syndrome
A characteristic symptom complex.		010.1652
Heritable Pulmonary Arterial Hypertension
[description not available]		016.3282
Familial Primary Pulmonary Hypertension
Familial or idiopathic hypertension in the PULMONARY CIRCULATION which is not secondary to other disease.		011.3282
Cardiac Failure
[description not available]		09.51152
Heart Failure
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.		111.51152
Anasarca
[description not available]		05.341
Peripheral Nerve Diseases
[description not available]		02.930
Drop Attack
[description not available]		02.4110
Weight Reduction
[description not available]		02.4110
Crow-Fukase Syndrome
[description not available]		02.4110
Neoplasms, Plasma Cell
Neoplasms associated with a proliferation of a single clone of PLASMA CELLS and characterized by the secretion of PARAPROTEINS.		02.4110
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		010.341
Peripheral Nervous System Diseases
Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.		02.930
Syncope
A transient loss of consciousness and postural tone caused by diminished blood flow to the brain (i.e., BRAIN ISCHEMIA). Presyncope refers to the sensation of lightheadedness and loss of strength that precedes a syncopal event or accompanies an incomplete syncope. (From Adams et al., Principles of Neurology, 6th ed, pp367-9)		02.4110
Weight Loss
Decrease in existing BODY WEIGHT.		02.4110
POEMS Syndrome
A multisystemic disorder characterized by a sensorimotor polyneuropathy (POLYNEUROPATHIES), organomegaly, endocrinopathy, monoclonal gammopathy, and pigmentary skin changes. Other clinical features which may be present include EDEMA; CACHEXIA; microangiopathic glomerulopathy; pulmonary hypertension (HYPERTENSION, PULMONARY); cutaneous necrosis; THROMBOCYTOSIS; and POLYCYTHEMIA. This disorder is frequently associated with osteosclerotic myeloma. (From Adams et al., Principles of Neurology, 6th ed, p1335; Rev Med Interne 1997;18(7):553-62)		02.4110
Fetal Growth Restriction
[description not available]		09.01226
Edema-Proteinuria-Hypertension Gestosis
[description not available]		05.181
Fetal Growth Retardation
Failure of a FETUS to attain expected GROWTH.		09.01226
Pre-Eclampsia
A complication of PREGNANCY, characterized by a complex of symptoms including maternal HYPERTENSION and PROTEINURIA with or without pathological EDEMA. Symptoms may range between mild and severe. Pre-eclampsia usually occurs after the 20th week of gestation, but may develop before this time in the presence of trophoblastic disease.		05.181
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		09.52286
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		08.04210
Breast Cancer
[description not available]		07.8220
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.8220
Cancer of Testis
[description not available]		02.4110
Atrophy
Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.		02.8130
Testicular Neoplasms
Tumors or cancer of the TESTIS. Germ cell tumors (GERMINOMA) of the testis constitute 95% of all testicular neoplasms.		02.4110
Diabetes Mellitus
A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.		09.36124
Fetal Distress
A nonreassuring fetal status (NRFS) indicating that the FETUS is compromised (American College of Obstetricians and Gynecologists 1988). It can be identified by sub-optimal values in FETAL HEART RATE; oxygenation of FETAL BLOOD; and other parameters.		03.3310
Alloxan Diabetes
[description not available]		05.12150
Diabetes Mellitus, Adult-Onset
[description not available]		09.76168
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		111.76168
Weight Gain
Increase in BODY WEIGHT over existing weight.		02.6620
Cirrhosis
[description not available]		04.7360
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		09.7360
Thromboembolism, Venous
[description not available]		02.4110
Venous Thromboembolism
Obstruction of a vein or VEINS (embolism) by a blood clot (THROMBUS) in the blood stream.		07.4110
Delayed Effects, Prenatal Exposure
[description not available]		02.7620
Nephrotic Syndrome
A condition characterized by severe PROTEINURIA, greater than 3.5 g/day in an average adult. The substantial loss of protein in the urine results in complications such as HYPOPROTEINEMIA; generalized EDEMA; HYPERTENSION; and HYPERLIPIDEMIAS. Diseases associated with nephrotic syndrome generally cause chronic kidney dysfunction.		07.4110
Proteinuria
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.		02.9330
Retinal Pigment Epithelial Detachment
[description not available]		02.4110
Retinal Detachment
Separation of the inner layers of the retina (neural retina) from the pigment epithelium. Retinal detachment occurs more commonly in men than in women, in eyes with degenerative myopia, in aging and in aphakia. It may occur after an uncomplicated cataract extraction, but it is seen more often if vitreous humor has been lost during surgery. (Dorland, 27th ed; Newell, Ophthalmology: Principles and Concepts, 7th ed, p310-12).		07.4110
Gastric Ulcer
[description not available]		03.0130
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		03.0130
Ulcer
A lesion on the surface of the skin or a mucous surface, produced by the sloughing of inflammatory necrotic tissue.		07.7220
Hyperoxia
An abnormal increase in the amount of oxygen in the tissues and organs.		03.6550
Active Hyperemia
[description not available]		02.9430
Hyperemia
The presence of an increased amount of blood in a body part or an organ leading to congestion or engorgement of blood vessels. Hyperemia can be due to increase of blood flow into the area (active or arterial), or due to obstruction of outflow of blood from the area (passive or venous).		02.9430
Plasmodium falciparum Malaria
[description not available]		02.4110
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.4110
Cardiac Remodeling, Ventricular
[description not available]		06.8381
Chronic Illness
[description not available]		05.3162
Pain, Chronic
[description not available]		05.6251
Acute Bacterial Prostatitis
[description not available]		07.54142
Pelvic Pain
Pain in the pelvic region of genital and non-genital origin.		06.86112
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		05.3162
Prostatitis
Infiltration of inflammatory cells into the parenchyma of PROSTATE. The subtypes are classified by their varied laboratory analysis, clinical presentation and response to treatment.		07.54142
Chronic Pain
Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain.		05.6251
Chronic Kidney Diseases
[description not available]		04.3531
Chronic Kidney Failure
[description not available]		04.2231
Kidney Failure, Chronic
The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.		04.2231
Renal Insufficiency, Chronic
Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)		04.3531
Bladder, Overactive
[description not available]		09.55195
Urinary Bladder, Overactive
Symptom of overactive detrusor muscle of the URINARY BLADDER that contracts with abnormally high frequency and urgency. Overactive bladder is characterized by the frequent feeling of needing to urinate during the day, during the night, or both. URINARY INCONTINENCE may or may not be present.		09.55195
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		05.2331
Insulin Sensitivity
[description not available]		012.5963
Cardiovascular Stroke
[description not available]		07.54160
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		05.2331
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		19.5963
Myocardial Infarction
NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION).		07.54160
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		114.0274
Complications of Diabetes Mellitus
[description not available]		09.06136
Fish Diseases
Diseases of freshwater, marine, hatchery or aquarium fish. This term includes diseases of both teleosts (true fish) and elasmobranchs (sharks, rays and skates).		02.4110
Age-Related Memory Disorders
[description not available]		03.4460
Memory Disorders
Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.		03.4460
Libman-Sacks Disease
[description not available]		06.6531
Sclerosis, Systemic
[description not available]		010.56145
Sex Disorders
[description not available]		09.57165
Lupus Erythematosus, Systemic
A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.		06.6531
Scleroderma, Systemic
A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.		112.56145
Sexual Dysfunction, Physiological
Physiological disturbances in normal sexual performance in either the male or the female.		111.57165
Diffuse Parenchymal Lung Disease
[description not available]		02.8930
Lung Diseases, Interstitial
A diverse group of lung diseases that affect the lung parenchyma. They are characterized by an initial inflammation of PULMONARY ALVEOLI that extends to the interstitium and beyond leading to diffuse PULMONARY FIBROSIS. Interstitial lung diseases are classified by their etiology (known or unknown causes), and radiological-pathological features.		14.8930
Acute Kidney Failure
[description not available]		05.47121
Acute Kidney Injury
Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.		05.47121
Lymphocytopenia
[description not available]		02.610
Lymphopenia
Reduction in the number of lymphocytes.		02.610
Diabetic Glomerulosclerosis
[description not available]		02.6120
Diabetic Nephropathies
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.		02.6120
Cardiac Output, Low
A state of subnormal or depressed cardiac output at rest or during stress. It is a characteristic of CARDIOVASCULAR DISEASES, including congenital, valvular, rheumatic, hypertensive, coronary, and cardiomyopathic. The serious form of low cardiac output is characterized by marked reduction in STROKE VOLUME, and systemic vasoconstriction resulting in cold, pale, and sometimes cyanotic extremities.		03.520
Cicatrization
The formation of fibrous tissue in the place of normal tissue during the process of WOUND HEALING. It includes scar tissue formation occurring in healing internal organs as well as in the skin after surface injuries.		02.610
Burns
Injuries to tissues caused by contact with heat, steam, chemicals (BURNS, CHEMICAL), electricity (BURNS, ELECTRIC), or the like.		08.1140
Cicatrix
The fibrous tissue that replaces normal tissue during the process of WOUND HEALING.		02.610
Dysplastic Nevus Syndrome, Hereditary
[description not available]		03.9320
Malignant Melanoma
[description not available]		03.7730
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		08.7730
Priapism
A prolonged painful erection that may lasts hours and is not associated with sexual activity. It is seen in patients with SICKLE CELL ANEMIA, advanced malignancy, spinal trauma; and certain drug treatments.		16.690
Ureteral Calculi
Stones in the URETER that are formed in the KIDNEY. They are rarely more than 5 mm in diameter for larger renal stones cannot enter ureters. They are often lodged at the ureteral narrowing and can cause excruciating renal colic.		015.3126
Achalasia
[description not available]		03.5210
Esophageal Achalasia
A motility disorder of the ESOPHAGUS in which the LOWER ESOPHAGEAL SPHINCTER (near the CARDIA) fails to relax resulting in functional obstruction of the esophagus, and DYSPHAGIA. Achalasia is characterized by a grossly contorted and dilated esophagus (megaesophagus).		03.5210
Urinary Retention
Inability to empty the URINARY BLADDER with voiding (URINATION).		011.5244
Dextro-Looped Transposition of the Great Arteries
[description not available]		05.9922
Transposition of Great Vessels
A congenital cardiovascular malformation in which the AORTA arises entirely from the RIGHT VENTRICLE, and the PULMONARY ARTERY arises from the LEFT VENTRICLE. Consequently, the pulmonary and the systemic circulations are parallel and not sequential, so that the venous return from the peripheral circulation is re-circulated by the right ventricle via aorta to the systemic circulation without being oxygenated in the lungs. This is a potentially lethal form of heart disease in newborns and infants.		17.9922
Angiospasm, Intracranial
[description not available]		02.830
Hemorrhage, Subarachnoid
[description not available]		03.0140
Subarachnoid Hemorrhage
Bleeding into the intracranial or spinal SUBARACHNOID SPACE, most resulting from INTRACRANIAL ANEURYSM rupture. It can occur after traumatic injuries (SUBARACHNOID HEMORRHAGE, TRAUMATIC). Clinical features include HEADACHE; NAUSEA; VOMITING, nuchal rigidity, variable neurological deficits and reduced mental status.		03.0140
Vasospasm, Intracranial
Constriction of arteries in the SKULL due to sudden, sharp, and often persistent smooth muscle contraction in blood vessels. Intracranial vasospasm results in reduced vessel lumen caliber, restricted blood flow to the brain, and BRAIN ISCHEMIA that may lead to hypoxic-ischemic brain injury (HYPOXIA-ISCHEMIA, BRAIN).		02.830
Ache
[description not available]		06.2743
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		011.2743
Preterm Birth
[description not available]		04.9621
Fetal Death
Death of the developing young in utero. BIRTH of a dead FETUS is STILLBIRTH.		04.9621
Premature Birth
CHILDBIRTH before 37 weeks of PREGNANCY (259 days from the first day of the mother's last menstrual period, or 245 days after FERTILIZATION).		04.9621
Hyperlipemia
[description not available]		06.241
Hyperlipidemias
Conditions with excess LIPIDS in the blood.		06.241
Cavernitis, Fibrous
[description not available]		05.1552
Penile Induration
A condition characterized by hardening of the PENIS due to the formation of fibrous plaques on the dorsolateral aspect of the PENIS, usually involving the membrane (tunica albuginea) surrounding the erectile tissue (corpus cavernosum penis). This may eventually cause a painful deformity of the shaft or constriction of the urethra, or both.		05.1552
Rupture
Forcible or traumatic tear or break of an organ or other soft part of the body.		02.610
Aseptic Necrosis of Femur Head
[description not available]		02.610
Cancer of Skin
[description not available]		03.8120
Skin Neoplasms
Tumors or cancer of the SKIN.		03.8120
Absence Seizure
[description not available]		04.3160
Seizures
Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.		09.3160
Canine Diseases
[description not available]		05.3543
Bloch-Siemens Syndrome
[description not available]		02.2510
Chemical Dependence
[description not available]		03.4320
Substance-Related Disorders
Disorders related to substance use or abuse.		03.4320
Atrial Remodeling
Long-term changes in the electrophysiological parameters and/or anatomical structures of the HEART ATRIA that result from prolonged changes in atrial rate, often associated with ATRIAL FIBRILLATION or long periods of intense EXERCISE.		02.2510
Ovarian Diseases
Pathological processes of the OVARY.		02.2110
Injury, Ischemia-Reperfusion
[description not available]		04.55220
Abnormality, Torsion
[description not available]		02.2110
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		04.55220
Left Ventricular Dysfunction
[description not available]		011.773
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		020.24221
Ventricular Dysfunction, Left
A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall.		06.773
Carcinogenesis
The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.		03.4820
Experimental Mammary Neoplasms
[description not available]		02.2110
Vascular Injuries
[description not available]		02.2110
Chronic Infantile Neurologic, Cutaneous, and Articular Syndrome
[description not available]		02.2110
Cryopyrin-Associated Periodic Syndromes
A group of rare autosomal dominant diseases, commonly characterized by atypical URTICARIA (hives) with systemic symptoms that develop into end-organ damage. The atypical hives do not involve T-cell or autoantibody. Cryopyrin-associated periodic syndrome includes three previously distinct disorders: Familial cold autoinflammatory syndrome; Muckle-Wells Syndrome; and CINCA Syndrome, that are now considered to represent a disease continuum, all caused by NLRP3 PROTEIN mutations.		02.2110
Acute Edematous Pancreatitis
[description not available]		02.2510
Pancreatitis
INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis.		07.2510
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		04.6151
Peripheral Nerve Injury
[description not available]		03.0840
Peripheral Nerve Injuries
Injuries to the PERIPHERAL NERVES.		03.0840
Urinary Incontinence
Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE.		06.8764
Cold Fingers, Hereditary
[description not available]		08.0673
Raynaud Disease
An idiopathic vascular disorder characterized by bilateral Raynaud phenomenon, the abrupt onset of digital paleness or CYANOSIS in response to cold exposure or stress.		110.0673
Crush Fractures
[description not available]		02.2510
Bladder, Underactive
[description not available]		02.6920
Bladder Disorder, Neurogenic
[description not available]		02.5420
Urinary Bladder, Neurogenic
Dysfunction of the URINARY BLADDER due to disease of the central or peripheral nervous system pathways involved in the control of URINATION. This is often associated with SPINAL CORD DISEASES, but may also be caused by BRAIN DISEASES or PERIPHERAL NERVE DISEASES.		02.5420
Bladder Neck Obstruction
[description not available]		05.79102
Connective Tissue Diseases
A heterogeneous group of disorders, some hereditary, others acquired, characterized by abnormal structure or function of one or more of the elements of connective tissue, i.e., collagen, elastin, or the mucopolysaccharides.		05.7232
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		07.04103
Dyslipidemia
[description not available]		02.5220
Injury, Myocardial Reperfusion
[description not available]		03.3460
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		07.04103
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		02.5220
Arteriosclerosis, Coronary
[description not available]		07.5562
Fibromuscular Dysplasia
An idiopathic, segmental, nonatheromatous disease of the musculature of arterial walls, leading to STENOSIS of small and medium-sized arteries. There is true proliferation of SMOOTH MUSCLE CELLS and fibrous tissue. Fibromuscular dysplasia lesions are smooth stenosis and occur most often in the renal and carotid arteries. They may also occur in other peripheral arteries of the extremity.		02.2510
Vascular Fistula
An abnormal passage between two or more BLOOD VESSELS, between ARTERIES; VEINS; or between an artery and a vein.		02.2510
Coronary Artery Disease
Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause.		07.5562
Urinary Tract Diseases
[description not available]		07.3461
Hyperplasia
An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells.		03.4620
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		07.18220
Depression
Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.		04.761
Age-Related Osteoporosis
[description not available]		02.5920
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		04.8770
Osteoporosis
Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.		02.5920
Osteoporotic Fractures
Breaks in bones resulting from low bone mass and microarchitectural deterioration characteristic of OSTEOPOROSIS.		02.2510
Colitis, Mucous
[description not available]		02.2510
Colonic Inertia
Symptom characterized by the passage of stool once a week or less.		02.2510
Constipation
Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.		07.2510
Irritable Bowel Syndrome
A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION.		07.2510
Disease Exacerbation
[description not available]		011.731813
Becker Muscular Dystrophy
[description not available]		012.3364
Muscular Dystrophy, Duchenne
An X-linked recessive muscle disease caused by an inability to synthesize DYSTROPHIN, which is involved with maintaining the integrity of the sarcolemma. Muscle fibers undergo a process that features degeneration and regeneration. Clinical manifestations include proximal weakness in the first few years of life, pseudohypertrophy, cardiomyopathy (see MYOCARDIAL DISEASES), and an increased incidence of impaired mentation. Becker muscular dystrophy is a closely related condition featuring a later onset of disease (usually adolescence) and a slowly progressive course. (Adams et al., Principles of Neurology, 6th ed, p1415)		19.3364
Colorectal Cancer
[description not available]		02.2510
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.2510
Infections, Coronavirus
[description not available]		02.2510
Cytokine Release Syndrome
A severe immune reaction characterized by excessive release of CYTOKINES. Symptoms include DYSPNEA; FEVER; HEADACHE; HYPOTENSION; NAUSEA; RASH; TACHYCARDIA; HYPOXIA; HYPERFERRITINEMIA, and MULTIPLE ORGAN FAILURE. It is associated with viral infections, SEPSIS; AUTOIMMUNE DISEASES and a variety of factors used in IMMUNOTHERAPY.		02.2510
Pneumonia, Viral
Inflammation of the lung parenchyma that is caused by a viral infection.		02.2510
Coronavirus Infections
Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).		02.2510
Cardiac Hypertrophy
Enlargement of the HEART due to chamber HYPERTROPHY, an increase in wall thickness without an increase in the number of cells (MYOCYTES, CARDIAC). It is the result of increase in myocyte size, mitochondrial and myofibrillar mass, as well as changes in extracellular matrix.		02.8330
Anemia, Splenic
[description not available]		02.2510
Cardiomegaly
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.		02.8330
Vascular Malformations
A spectrum of congenital, inherited, or acquired abnormalities in BLOOD VESSELS that can adversely affect the normal blood flow in ARTERIES or VEINS. Most are congenital defects such as abnormal communications between blood vessels (fistula), shunting of arterial blood directly into veins bypassing the CAPILLARIES (arteriovenous malformations), formation of large dilated blood blood-filled vessels (cavernous angioma), and swollen capillaries (capillary telangiectases). In rare cases, vascular malformations can result from trauma or diseases.		02.2510
Hyperhomocysteinemia
Condition in which the plasma levels of homocysteine and related metabolites are elevated (		07.4110
Acute Onset Vascular Dementia
[description not available]		02.4110
Dementia, Vascular
An imprecise term referring to dementia associated with CEREBROVASCULAR DISORDERS, including CEREBRAL INFARCTION (single or multiple), and conditions associated with chronic BRAIN ISCHEMIA. Diffuse, cortical, and subcortical subtypes have been described. (From Gerontol Geriatr 1998 Feb;31(1):36-44)		14.4110
Alveolitis, Fibrosing
[description not available]		03.0640
Pulmonary Fibrosis
A process in which normal lung tissues are progressively replaced by FIBROBLASTS and COLLAGEN causing an irreversible loss of the ability to transfer oxygen into the bloodstream via PULMONARY ALVEOLI. Patients show progressive DYSPNEA finally resulting in death.		08.0640
Pulmonary Sarcoidosis
[description not available]		02.2510
Sarcoidosis, Pulmonary
Sarcoidosis affecting predominantly the lungs, the site most frequently involved and most commonly causing morbidity and mortality in sarcoidosis. Pulmonary sarcoidosis is characterized by sharply circumscribed granulomas in the alveolar, bronchial, and vascular walls, composed of tightly packed cells derived from the mononuclear phagocyte system. The clinical symptoms when present are dyspnea upon exertion, nonproductive cough, and wheezing. (Cecil Textbook of Medicine, 19th ed, p431)		02.2510
ACD-MPV
[description not available]		03.1710
Persistent Fetal Circulation Syndrome
A syndrome of persistent PULMONARY HYPERTENSION in the newborn infant (INFANT, NEWBORN) without demonstrable HEART DISEASES. This neonatal condition can be caused by severe pulmonary vasoconstriction (reactive type), hypertrophy of pulmonary arterial muscle (hypertrophic type), or abnormally developed pulmonary arterioles (hypoplastic type). The newborn patient exhibits CYANOSIS and ACIDOSIS due to the persistence of fetal circulatory pattern of right-to-left shunting of blood through a patent ductus arteriosus (DUCTUS ARTERIOSUS, PATENT) and at times a patent foramen ovale (FORAMEN OVALE, PATENT).		03.1710
Experimental Hepatoma
[description not available]		02.3110
Cardiac Arrest, Sudden
[description not available]		02.3110
Death, Sudden, Cardiac
Unexpected rapid natural death due to cardiovascular collapse within one hour of initial symptoms. It is usually caused by the worsening of existing heart diseases. The sudden onset of symptoms, such as CHEST PAIN and CARDIAC ARRHYTHMIAS, particularly VENTRICULAR TACHYCARDIA, can lead to the loss of consciousness and cardiac arrest followed by biological death. (from Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine, 7th ed., 2005)		02.3110
Acute Myelogenous Leukemia
[description not available]		02.3110
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.3110
Hypergonadotropic Hypogonadism
[description not available]		08.0875
Hypogonadism
Condition resulting from deficient gonadal functions, such as GAMETOGENESIS and the production of GONADAL STEROID HORMONES. It is characterized by delay in GROWTH, germ cell maturation, and development of secondary sex characteristics. Hypogonadism can be due to a deficiency of GONADOTROPINS (hypogonadotropic hypogonadism) or due to primary gonadal failure (hypergonadotropic hypogonadism).		08.0875
Anoxemia
[description not available]		03.7190
Hypoxia
Sub-optimal OXYGEN levels in the ambient air of living organisms.		03.7190
Cardiomyopathies, Primary
[description not available]		03.4870
Experimental Radiation Injuries
[description not available]		02.3110
Cardiomyopathies
A group of diseases in which the dominant feature is the involvement of the CARDIAC MUSCLE itself. Cardiomyopathies are classified according to their predominant pathophysiological features (DILATED CARDIOMYOPATHY; HYPERTROPHIC CARDIOMYOPATHY; RESTRICTIVE CARDIOMYOPATHY) or their etiological/pathological factors (CARDIOMYOPATHY, ALCOHOLIC; ENDOCARDIAL FIBROELASTOSIS).		03.4870
Fatty Liver, Nonalcoholic
[description not available]		02.3110
Hypertrophy
General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).		08.4620
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		07.3110
Benign Neoplasms
[description not available]		02.3110
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		14.7220
Deficiency, Vitamin D
[description not available]		02.3110
Vitamin D Deficiency
A nutritional condition produced by a deficiency of VITAMIN D in the diet, insufficient production of vitamin D in the skin, inadequate absorption of vitamin D from the diet, or abnormal conversion of vitamin D to its bioactive metabolites. It is manifested clinically as RICKETS in children and OSTEOMALACIA in adults. (From Cecil Textbook of Medicine, 19th ed, p1406)		07.3110
Arterial Obstructive Diseases
[description not available]		03.8721
Arterial Occlusive Diseases
Pathological processes which result in the partial or complete obstruction of ARTERIES. They are characterized by greatly reduced or absence of blood flow through these vessels. They are also known as arterial insufficiency.		03.8721
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		08.2250
Ischemia
A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION.		07.33143
Anterior Urethral Stricture
[description not available]		02.5920
Urethral Stricture
Narrowing of any part of the URETHRA. It is characterized by decreased urinary stream and often other obstructive voiding symptoms.		07.5920
Carcinoma, Epidermoid
[description not available]		06.3942
Blood Loss, Surgical
Loss of blood during a surgical procedure.		02.3110
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		18.3942
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		08.0974
Diastolic Heart Failure
[description not available]		05.821
Heart Failure, Diastolic
Heart failure caused by abnormal myocardial relaxation during DIASTOLE leading to defective cardiac filling.		05.821
Menopause
The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age.		03.0610
Brain Thrombosis
[description not available]		02.1510
Anti-Phospholipid Antibody Syndrome
[description not available]		02.5320
Antiphospholipid Syndrome
The presence of antibodies directed against phospholipids (ANTIBODIES, ANTIPHOSPHOLIPID). The condition is associated with a variety of diseases, notably systemic lupus erythematosus and other connective tissue diseases, thrombopenia, and arterial or venous thromboses. In pregnancy it can cause abortion. Of the phospholipids, the cardiolipins show markedly elevated levels of anticardiolipin antibodies (ANTIBODIES, ANTICARDIOLIPIN). Present also are high levels of lupus anticoagulant (LUPUS COAGULATION INHIBITOR).		07.5320
Cerebral Microangiopathies
[description not available]		03.5311
Cerebral Small Vessel Diseases
Pathological processes or diseases where cerebral MICROVESSELS show abnormalities. They are often associated with aging, hypertension and risk factors for lacunar infarcts (see LACUNAR INFARCTION); LEUKOARAIOSIS; and CEREBRAL HEMORRHAGE.		03.5311
Inflammatory Response Syndrome, Systemic
[description not available]		02.1510
Chronic Lung Injury
[description not available]		02.1510
Systemic Inflammatory Response Syndrome
A systemic inflammatory response to a variety of clinical insults, characterized by two or more of the following conditions: (1) fever		02.1510
Limited Scleroderma
[description not available]		03.5611
Right Ventricular Dysfunction
[description not available]		04.2931
Scleroderma, Limited
The least progressive form of SYSTEMIC SCLERODERMA with skin thickening restricted to the face, neck and areas distal to the elbows and/or knees, sparing the trunk. The CREST SYNDROME is a form of limited scleroderma.		03.5611
Complication, Postoperative
[description not available]		07.5384
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		07.5384
Muscle Pain
[description not available]		04.8421
Back Ache
[description not available]		07.9163
Back Pain
Acute or chronic pain located in the posterior regions of the THORAX; LUMBOSACRAL REGION; or the adjacent regions.		07.9163
Flushing
A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress.		05.0631
Myalgia
Painful sensation in the muscles.		04.8421
Recrudescence
[description not available]		03.3160
Abnormality, Heart
[description not available]		05.6963
Intraventricular Septal Defects
[description not available]		03.5311
Heart Defects, Congenital
Developmental abnormalities involving structures of the heart. These defects are present at birth but may be discovered later in life.		17.6963
Heart Septal Defects, Ventricular
Developmental abnormalities in any portion of the VENTRICULAR SEPTUM resulting in abnormal communications between the two lower chambers of the heart. Classification of ventricular septal defects is based on location of the communication, such as perimembranous, inlet, outlet (infundibular), central muscular, marginal muscular, or apical muscular defect.		03.5311
Apnea, Obstructive Sleep
[description not available]		02.4820
Sleep Apnea, Obstructive
A disorder characterized by recurrent apneas during sleep despite persistent respiratory efforts. It is due to upper airway obstruction. The respiratory pauses may induce HYPERCAPNIA or HYPOXIA. Cardiac arrhythmias and elevation of systemic and pulmonary arterial pressures may occur. Frequent partial arousals occur throughout sleep, resulting in relative SLEEP DEPRIVATION and daytime tiredness. Associated conditions include OBESITY; ACROMEGALY; MYXEDEMA; micrognathia; MYOTONIC DYSTROPHY; adenotonsilar dystrophy; and NEUROMUSCULAR DISEASES. (From Adams et al., Principles of Neurology, 6th ed, p395)		02.4820
Central Serous Retinopathy
[description not available]		04.3870
Central Serous Chorioretinopathy
A visual impairment characterized by the accumulation of fluid under the retina through a defect in the retinal pigment epithelium.		04.3870
Arrhythmia
[description not available]		02.1710
Arrhythmias, Cardiac
Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.		02.1710
Hypoventilation
A reduction in the amount of air entering the pulmonary alveoli.		02.1710
Hyperkyphosis
[description not available]		02.1710
Airway Hyper-Responsiveness
[description not available]		07.1510
Autoimmune Chronic Hepatitis
[description not available]		02.1710
Esophageal Varices
[description not available]		02.1710
Hematochezia
The passage of bright red blood from the rectum. The blood may or may not be mixed with formed stool in the form of blood, blood clots, bloody stool or diarrhea.		02.1710
Cruveilhier-Baumgarten Syndrome
Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS.		03.0140
Cholangiitis, Sclerosing
[description not available]		02.1710
Esophageal and Gastric Varices
Dilated blood vessels in the ESOPHAGUS or GASTRIC FUNDUS that shunt blood from the portal circulation (PORTAL SYSTEM) to the systemic venous circulation. Often they are observed in individuals with portal hypertension (HYPERTENSION, PORTAL).		02.1710
Gastrointestinal Hemorrhage
Bleeding in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM.		02.1710
Hypertension, Portal
Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN.		03.0140
Cholangitis, Sclerosing
Chronic inflammatory disease of the BILIARY TRACT. It is characterized by fibrosis and hardening of the intrahepatic and extrahepatic biliary ductal systems leading to bile duct strictures, CHOLESTASIS, and eventual BILIARY CIRRHOSIS.		02.1710
Hepatitis, Autoimmune
A chronic self-perpetuating hepatocellular INFLAMMATION of unknown cause, usually with HYPERGAMMAGLOBULINEMIA and serum AUTOANTIBODIES.		02.1710
Dyskinesia Syndromes
[description not available]		02.1710
Movement Disorders
Syndromes which feature DYSKINESIAS as a cardinal manifestation of the disease process. Included in this category are degenerative, hereditary, post-infectious, medication-induced, post-inflammatory, and post-traumatic conditions.		02.1710
Embolism, Pulmonary
[description not available]		02.830
Pulmonary Embolism
Blocking of the PULMONARY ARTERY or one of its branches by an EMBOLUS.		07.830
Autoimmune Disease
[description not available]		02.8830
Autoimmune Diseases
Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.		02.8830
Nociceptive Pain
Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.		02.1710
Diabetic Angiopathies
VASCULAR DISEASES that are associated with DIABETES MELLITUS.		07.1475
Spermatic Cord Torsion
The twisting of the SPERMATIC CORD due to an anatomical abnormality that left the TESTIS mobile and dangling in the SCROTUM. The initial effect of testicular torsion is obstruction of venous return. Depending on the duration and degree of cord rotation, testicular symptoms range from EDEMA to interrupted arterial flow and testicular pain. If blood flow to testis is absent for 4 to 6 h, SPERMATOGENESIS may be permanently lost.		02.5420
Prostatism
Lower urinary tract symptom, such as slow urinary stream, associated with PROSTATIC HYPERPLASIA in older men.		010.32111
Breathlessness
[description not available]		02.8330
MS (Multiple Sclerosis)
[description not available]		05.4951
Dyspnea
Difficult or labored breathing.		02.8330
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		05.4951
Flank Pain
Pain emanating from below the RIBS and above the ILIUM.		02.1710
Inguinal Hernia
[description not available]		02.1710
Ecchymosis
Extravasation of blood into the skin, resulting in a nonelevated, rounded or irregular, blue or purplish patch, larger than a petechia.		02.1710
Hernia, Inguinal
An abdominal hernia with an external bulge in the GROIN region. It can be classified by the location of herniation. Indirect inguinal hernias occur through the internal inguinal ring. Direct inguinal hernias occur through defects in the ABDOMINAL WALL (transversalis fascia) in Hesselbach's triangle. The former type is commonly seen in children and young adults; the latter in adults.		02.1710
Acute Disease
Disease having a short and relatively severe course.		05.4951
Endolymphatic Hydrops
An accumulation of ENDOLYMPH in the inner ear (LABYRINTH) leading to buildup of pressure and distortion of intralabyrinthine structures, such as COCHLEA and SEMICIRCULAR CANALS. It is characterized by SENSORINEURAL HEARING LOSS; TINNITUS; and sometimes VERTIGO.		02.1710
Cochlear Hearing Loss
[description not available]		02.5220
Deafness, Sudden
Complete sensorineural hearing loss which develops suddenly over a period of hours or a few days.		02.4920
Hearing Loss, Sensorineural
Hearing loss resulting from damage to the COCHLEA and the sensorineural elements which lie internally beyond the oval and round windows. These elements include the AUDITORY NERVE and its connections in the BRAINSTEM.		02.5220
Glaucoma
An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)		02.2110
Retinal Degeneration
A retrogressive pathological change in the retina, focal or generalized, caused by genetic defects, inflammation, trauma, vascular disease, or aging. Degeneration affecting predominantly the macula lutea of the retina is MACULAR DEGENERATION. (Newell, Ophthalmology: Principles and Concepts, 7th ed, p304)		02.2110
Achromatopsia
Severely deficient color perception, typically with monochromacy and reduced visual acuity. The atypical form can include normal visual acuity with pseudomonochromacy.		02.2110
Color Vision Defects
Defects of color vision are mainly hereditary traits but can be secondary to acquired or developmental abnormalities in the CONES (RETINA). Severity of hereditary defects of color vision depends on the degree of mutation of the ROD OPSINS genes (on X CHROMOSOME and CHROMOSOME 3) that code the photopigments for red, green and blue.		02.2110
Anus Prolapse
[description not available]		02.2110
Agenesis of Hemidiaphragm
[description not available]		02.5420
Bronchopulmonary Dysplasia
A chronic lung disease developed after OXYGEN INHALATION THERAPY or mechanical ventilation (VENTILATION, MECHANICAL) usually occurring in certain premature infants (INFANT, PREMATURE) or newborn infants with respiratory distress syndrome (RESPIRATORY DISTRESS SYNDROME, NEWBORN). Histologically, it is characterized by the unusual abnormalities of the bronchioles, such as METAPLASIA, decrease in alveolar number, and formation of CYSTS.		02.2110
Hernias, Diaphragmatic, Congenital
Protrusion of abdominal structures into the THORAX as a result of embryologic defects in the DIAPHRAGM often present in the neonatal period. It can be isolated, syndromic, non-syndromic or be a part of chromosome abnormality. Associated pulmonary hypoplasia and PULMONARY HYPERTENSION can further complicate stabilization and surgical intervention.		02.5420
Bone Fractures
[description not available]		04.1931
Fractures, Bone
Breaks in bones.		04.1931
Enteropathy, Exudative
[description not available]		02.2110
Protein-Losing Enteropathies
Pathological conditions in the INTESTINES that are characterized by the gastrointestinal loss of serum proteins, including SERUM ALBUMIN; IMMUNOGLOBULINS; and at times LYMPHOCYTES. Severe condition can result in HYPOGAMMAGLOBULINEMIA or LYMPHOPENIA. Protein-losing enteropathies are associated with a number of diseases including INTESTINAL LYMPHANGIECTASIS; WHIPPLE'S DISEASE; and NEOPLASMS of the SMALL INTESTINE.		02.2110
Impotence, Arteriogenic
[description not available]		09.34216
Frigidity
[description not available]		07.56113
Autoimmune Diabetes
[description not available]		05.7254
Diabetes Mellitus, Type 1
A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.		05.7254
Sexual Dysfunctions, Psychological
Disturbances in sexual desire and the psychophysiologic changes that characterize the sexual response cycle and cause marked distress and interpersonal difficulty. (APA, DSM-IV, 1994)		07.56113
Ureteral Obstruction
Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy.		07.7830
Asthma, Bronchial
[description not available]		02.2110
Asthma
A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).		07.2110
Acquired Vocal Cord Palsy
[description not available]		02.2110
Hoarseness
An unnaturally deep or rough quality of voice.		02.2110
Vocal Cord Paralysis
Congenital or acquired paralysis of one or both VOCAL CORDS. This condition is caused by defects in the CENTRAL NERVOUS SYSTEM, the VAGUS NERVE and branches of LARYNGEAL NERVES. Common symptoms are VOICE DISORDERS including HOARSENESS or APHONIA.		02.2110
Dermatomyositis, Adult Type
[description not available]		02.2110
Pleural Diseases
Diseases involving the PLEURA.		02.2110
Dermatomyositis
A subacute or chronic inflammatory disease of muscle and skin, marked by proximal muscle weakness and a characteristic skin rash. The illness occurs with approximately equal frequency in children and adults. The skin lesions usually take the form of a purplish rash (or less often an exfoliative dermatitis) involving the nose, cheeks, forehead, upper trunk, and arms. The disease is associated with a complement mediated intramuscular microangiopathy, leading to loss of capillaries, muscle ischemia, muscle-fiber necrosis, and perifascicular atrophy. The childhood form of this disease tends to evolve into a systemic vasculitis. Dermatomyositis may occur in association with malignant neoplasms. (From Adams et al., Principles of Neurology, 6th ed, pp1405-6)		02.2110
Chronic Hepatitis C
[description not available]		02.2510
Tricuspid Incompetence
[description not available]		02.2510
Hepatitis C, Chronic
INFLAMMATION of the LIVER in humans that is caused by HEPATITIS C VIRUS lasting six months or more. Chronic hepatitis C can lead to LIVER CIRRHOSIS.		02.2510
Hypertrophy, Right Ventricular
Enlargement of the RIGHT VENTRICLE of the heart. This increase in ventricular mass is often attributed to PULMONARY HYPERTENSION and is a contributor to cardiovascular morbidity and mortality.		03.0240
Pulmonary Arterial Remodeling
[description not available]		02.2110
Encephalopathy, Hepatic
[description not available]		02.2110
Hepatic Encephalopathy
A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5)		07.2110
Sterility, Male
[description not available]		05.2562
Infertility, Male
The inability of the male to effect FERTILIZATION of an OVUM after a specified period of unprotected intercourse. Male sterility is permanent infertility.		05.2562
Asymmetric Diabetic Proximal Motor Neuropathy
[description not available]		05.2841
Diabetic Neuropathies
Peripheral, autonomic, and cranial nerve disorders that are associated with DIABETES MELLITUS. These conditions usually result from diabetic microvascular injury involving small blood vessels that supply nerves (VASA NERVORUM). Relatively common conditions which may be associated with diabetic neuropathy include third nerve palsy (see OCULOMOTOR NERVE DISEASES); MONONEUROPATHY; mononeuropathy multiplex; diabetic amyotrophy; a painful POLYNEUROPATHY; autonomic neuropathy; and thoracoabdominal neuropathy. (From Adams et al., Principles of Neurology, 6th ed, p1325)		05.2841
Anterior Ischemic Optic Neuropathy
[description not available]		09.74110
Optic Neuropathy, Ischemic
Ischemic injury to the OPTIC NERVE which usually affects the OPTIC DISK (optic neuropathy, anterior ischemic) and less frequently the retrobulbar portion of the nerve (optic neuropathy, posterior ischemic). The injury results from occlusion of arterial blood supply which may result from TEMPORAL ARTERITIS; ATHEROSCLEROSIS; COLLAGEN DISEASES; EMBOLISM; DIABETES MELLITUS; and other conditions. The disease primarily occurs in the sixth decade or later and presents with the sudden onset of painless and usually severe monocular visual loss. Anterior ischemic optic neuropathy also features optic disk edema with microhemorrhages. The optic disk appears normal in posterior ischemic optic neuropathy. (Glaser, Neuro-Ophthalmology, 2nd ed, p135)		04.74110
Astheno Teratozoospermia
[description not available]		02.110
Complication, Intraoperative
[description not available]		03.4220
Panic Attacks
[description not available]		02.0810
Prosthesis Durability
[description not available]		02.0810
Foreign-Body Migration
Migration of a foreign body from its original location to some other location in the body.		02.0810
Panic Disorder
A type of anxiety disorder characterized by unexpected panic attacks that last minutes or, rarely, hours. Panic attacks begin with intense apprehension, fear or terror and, often, a feeling of impending doom. Symptoms experienced during a panic attack include dyspnea or sensations of being smothered; dizziness, loss of balance or faintness; choking sensations; palpitations or accelerated heart rate; shakiness; sweating; nausea or other form of abdominal distress; depersonalization or derealization; paresthesias; hot flashes or chills; chest discomfort or pain; fear of dying and fear of not being in control of oneself or going crazy. Agoraphobia may also develop. Similar to other anxiety disorders, it may be inherited as an autosomal dominant trait.		02.0810
Sexually Transmitted Diseases
Diseases due to or propagated by sexual contact.		02.0810
Injuries, Spinal Cord
[description not available]		07.77143
Spinal Cord Injuries
Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).		07.77143
Anal Fissure
[description not available]		07.0810
Fissure in Ano
A painful linear tear at the margin of the anus. It appears as a crack or slit in the mucous membrane of the anus and is very painful and difficult to heal.		02.0810
Indigestion
[description not available]		05.9533
Bilateral Headache
[description not available]		08.4284
Nasopharyngitis
Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands.		04.3911
Dyspepsia
Impaired digestion, especially after eating.		05.9533
Headache
The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.		08.4284
Cerebral Ischemia
[description not available]		02.9940
Brain Ischemia
Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.		02.9940
E coli Infections
[description not available]		02.110
Necrotizing Pyelonephritis
[description not available]		02.110
Escherichia coli Infections
Infections with bacteria of the species ESCHERICHIA COLI.		02.110
Pyelonephritis
Inflammation of the KIDNEY involving the renal parenchyma (the NEPHRONS); KIDNEY PELVIS; and KIDNEY CALICES. It is characterized by ABDOMINAL PAIN; FEVER; NAUSEA; VOMITING; and occasionally DIARRHEA.		02.110
Anterior Choroidal Artery Infarction
[description not available]		02.520
Cerebral Infarction
The formation of an area of NECROSIS in the CEREBRUM caused by an insufficiency of arterial or venous blood flow. Infarcts of the cerebrum are generally classified by hemisphere (i.e., left vs. right), lobe (e.g., frontal lobe infarction), arterial distribution (e.g., INFARCTION, ANTERIOR CEREBRAL ARTERY), and etiology (e.g., embolic infarction).		02.520
Cystitis
Inflammation of the URINARY BLADDER, either from bacterial or non-bacterial causes. Cystitis is usually associated with painful urination (dysuria), increased frequency, urgency, and suprapubic pain.		07.110
HbS Disease
[description not available]		02.4620
Choked Disk
[description not available]		02.0810
Branch Retinal Artery Occlusion
[description not available]		02.5120
Anemia, Sickle Cell
A disease characterized by chronic hemolytic anemia, episodic painful crises, and pathologic involvement of many organs. It is the clinical expression of homozygosity for hemoglobin S.		02.4620
Papilledema
Swelling of the OPTIC DISK, usually in association with increased intracranial pressure, characterized by hyperemia, blurring of the disk margins, microhemorrhages, blind spot enlargement, and engorgement of retinal veins. Chronic papilledema may cause OPTIC ATROPHY and visual loss. (Miller et al., Clinical Neuro-Ophthalmology, 4th ed, p175)		02.0810
Retinal Artery Occlusion
Sudden ISCHEMIA in the RETINA due to blocked blood flow through the CENTRAL RETINAL ARTERY or its branches leading to sudden complete or partial loss of vision, respectively, in the eye.		07.5120
Benign Neonatal Sleep Myoclonus
[description not available]		0310
Apnea, Sleep
[description not available]		0310
Sleep Apnea Syndromes
Disorders characterized by multiple cessations of respirations during sleep that induce partial arousals and interfere with the maintenance of sleep. Sleep apnea syndromes are divided into central (see SLEEP APNEA, CENTRAL), obstructive (see SLEEP APNEA, OBSTRUCTIVE), and mixed central-obstructive types.		0310
Adenocarcinoma, Basal Cell
[description not available]		07.3463
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		07.3463
Joint Pain
[description not available]		02.4820
Arthralgia
Pain in the joint.		02.4820
Left Ventricular Hypertrophy
[description not available]		03.921
Hypertrophy, Left Ventricular
Enlargement of the LEFT VENTRICLE of the heart. This increase in ventricular mass is attributed to sustained abnormal pressure or volume loads and is a contributor to cardiovascular morbidity and mortality.		03.921
Embryopathies
[description not available]		02.110
Diaphragmatic Hernia
[description not available]		02.110
Bladder Diseases
[description not available]		02.110
Injuries, Radiation
[description not available]		05.3422
Airflow Obstruction, Chronic
[description not available]		06.3851
Pulmonary Disease, Chronic Obstructive
A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.		06.3851
Dementia Praecox
[description not available]		03.4811
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		03.4811
Amputation, Traumatic
Loss of a limb or other bodily appendage by accidental injury.		02.110
Ataxia
Impairment of the ability to perform smoothly coordinated voluntary movements. This condition may affect the limbs, trunk, eyes, pharynx, larynx, and other structures. Ataxia may result from impaired sensory or motor function. Sensory ataxia may result from posterior column injury or PERIPHERAL NERVE DISEASES. Motor ataxia may be associated with CEREBELLAR DISEASES; CEREBRAL CORTEX diseases; THALAMIC DISEASES; BASAL GANGLIA DISEASES; injury to the RED NUCLEUS; and other conditions.		02.4620
Kahler Disease
[description not available]		02.110
Multiple Myeloma
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.		14.110
Acute Renal Colic
[description not available]		05.3822
Renal Colic
A severe intermittent and spasmodic pain in the lower back radiating to the groin, scrotum, and labia which is most commonly caused by a kidney stone (RENAL CALCULUS) passing through the URETER or by other urinary track blockage. It is often associated with nausea, vomiting, fever, restlessness, dull pain, frequent urination, and HEMATURIA.		05.3822
Besnier-Boeck Disease
[description not available]		02.1110
Sarcoidosis
An idiopathic systemic inflammatory granulomatous disorder comprised of epithelioid and multinucleated giant cells with little necrosis. It usually invades the lungs with fibrosis and may also involve lymph nodes, skin, liver, spleen, eyes, phalangeal bones, and parotid glands.		02.1110
Urethral Diseases
Pathological processes involving the URETHRA.		02.110
Urinary Incontinence, Stress
Involuntary discharge of URINE as a result of physical activities that increase abdominal pressure on the URINARY BLADDER without detrusor contraction or overdistended bladder. The subtypes are classified by the degree of leakage, descent and opening of the bladder neck and URETHRA without bladder contraction, and sphincter deficiency.		02.110
Cardiovascular Pregnancy Complications
[description not available]		03.0110
Apoplexy
[description not available]		04.3741
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		16.3741
Local Neoplasm Recurrence
[description not available]		04.4111
Edema, Pulmonary
[description not available]		08.24126
Pulmonary Edema
Excessive accumulation of extravascular fluid in the lung, an indication of a serious underlying disease or disorder. Pulmonary edema prevents efficient PULMONARY GAS EXCHANGE in the PULMONARY ALVEOLI, and can be life-threatening.		08.24126
Colitis, Ischemic
Inflammation of the COLON due to colonic ISCHEMIA resulting from alterations in systemic circulation or local vasculature.		02.110
Benign Neoplasms, Brain
[description not available]		02.1110
Germinoblastoma
[description not available]		02.1110
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		02.1110
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		07.1110
Altitude Hypoxia
Low ambient oxygen tension associated with ALTITUDE.		07.9105
Altitude Sickness
Multiple symptoms associated with reduced oxygen at high ALTITUDE.		07.9105
Experimental Neoplasms
[description not available]		02.1110
Foot Injuries
General or unspecified injuries involving the foot.		02.1110
Foot Ulcer
Lesion on the surface of the skin of the foot, usually accompanied by inflammation. The lesion may become infected or necrotic and is frequently associated with diabetes or leprosy.		02.1110
Familial Nonmedullary Thyroid Cancer
[description not available]		02.1110
Carcinoma, Anaplastic
[description not available]		03.921
Carcinoma, Papillary
A malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. (Stedman, 25th ed)		02.1110
Cancer of the Thyroid
[description not available]		02.1110
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		03.921
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		02.1110
Kidney Failure
A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism.		02.7930
Renal Insufficiency
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE.		02.7930
Hematuria
Presence of blood in the urine.		02.1110
Pain, Intractable
Persistent pain that is refractory to some or all forms of treatment.		02.1110
Cancer of Kidney
[description not available]		03.511
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		03.511
Centriacinar Emphysema
[description not available]		02.1110
Allodynia
[description not available]		02.1110
Femoral Fractures
Fractures of the femur.		02.1110
Cranial Nerve Diseases
Disorders of one or more of the twelve cranial nerves. With the exception of the optic and olfactory nerves, this includes disorders of the brain stem nuclei from which the cranial nerves originate or terminate.		02.1110
Amaurosis
[description not available]		02.4620
Drug Withdrawal Symptoms
[description not available]		02.1310
Blindness
The inability to see or the loss or absence of perception of visual stimuli. This condition may be the result of EYE DISEASES; OPTIC NERVE DISEASES; OPTIC CHIASM diseases; or BRAIN DISEASES affecting the VISUAL PATHWAYS or OCCIPITAL LOBE.		02.4620
Substance Withdrawal Syndrome
Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug.		02.1310
Eunuchism
The state of being a eunuch, a male without TESTES or whose testes failed to develop. It is characterized by the lack of mature male GERM CELLS and TESTICULAR HORMONES.		03.5111
Adult-Onset Still Disease
[description not available]		02.1310
Still's Disease, Adult-Onset
Systemic-onset rheumatoid arthritis in adults. It differs from classical rheumatoid arthritis in that it is more often marked by acute febrile onset, and generalized lymphadenopathy and hepatosplenomegaly are more prominent.		02.1310
Axonotmesis
[description not available]		03.7130
Trauma, Nervous System
Traumatic injuries to the brain, cranial nerves, spinal cord, autonomic nervous system, or neuromuscular system, including iatrogenic injuries induced by surgical procedures.		03.7130
Dermatitis Medicamentosa
[description not available]		02.1310
Penile Diseases
Pathological processes involving the PENIS or its component tissues.		02.4820
Orphan Diseases
Rare diseases that have not been well studied.		02.1510
Experimental Lung Inflammation
Inflammation of any part, segment or lobe, of the lung parenchyma.		02.520
Pneumonia
Infection of the lung often accompanied by inflammation.		02.520
Silicosis
A form of pneumoconiosis resulting from inhalation of dust containing crystalline form of SILICON DIOXIDE, usually in the form of quartz. Amorphous silica is relatively nontoxic.		07.1310
Bronchial Hyperreactivity
Tendency of the smooth muscle of the tracheobronchial tree to contract more intensely in response to a given stimulus than it does in the response seen in normal individuals. This condition is present in virtually all symptomatic patients with asthma. The most prominent manifestation of this smooth muscle contraction is a decrease in airway caliber that can be readily measured in the pulmonary function laboratory.		02.1310
Oligohydramnios
A condition of abnormally low AMNIOTIC FLUID volume. Principal causes include malformations of fetal URINARY TRACT; FETAL GROWTH RETARDATION; GESTATIONAL HYPERTENSION; nicotine poisoning; and PROLONGED PREGNANCY.		02.1310
Branch Vein Occlusion
[description not available]		02.1310
Retinal Vein Occlusion
Blockage of the RETINAL VEIN. Those at high risk for this condition include patients with HYPERTENSION; DIABETES MELLITUS; ATHEROSCLEROSIS; and other CARDIOVASCULAR DISEASES.		02.1310
Birth Weight
The mass or quantity of heaviness of an individual at BIRTH. It is expressed by units of pounds or kilograms.		02.1510
Anemia, Cooley's
[description not available]		03.5311
beta-Thalassemia
A disorder characterized by reduced synthesis of the beta chains of hemoglobin. There is retardation of hemoglobin A synthesis in the heterozygous form (thalassemia minor), which is asymptomatic, while in the homozygous form (thalassemia major, Cooley's anemia, Mediterranean anemia, erythroblastic anemia), which can result in severe complications and even death, hemoglobin A synthesis is absent.		03.5311
Connective Tissue Disease, Mixed
[description not available]		04.4511
Chronic Paroxysmal Hemicrania
[description not available]		02.1510
Neuralgia, Pudendal
[description not available]		02.1510
Cardiac Toxicity
[description not available]		02.1510
Cardiotoxicity
Damage to the HEART or its function secondary to exposure to toxic substances such as drugs used in CHEMOTHERAPY; IMMUNOTHERAPY; or RADIATION.		02.1510
Amnesia, Transient Global
A syndrome characterized by a transient loss of the ability to form new memories. It primarily occurs in middle aged or elderly individuals, and episodes may last from minutes to hours. During the period of amnesia, immediate and recent memory abilities are impaired, but the level of consciousness and ability to perform other intellectual tasks are preserved. The condition is related to bilateral dysfunction of the medial portions of each TEMPORAL LOBE. Complete recovery normally occurs, and recurrences are unusual. (From Adams et al., Principles of Neurology, 6th ed, pp429-30)		02.4520
Deafness, Transitory
[description not available]		02.0410
Day Blindness
[description not available]		03.1450
Hearing Loss
A general term for the complete or partial loss of the ability to hear from one or both ears.		02.0410
Urination Disorders
Abnormalities in the process of URINE voiding, including bladder control, frequency of URINATION, as well as the volume and composition of URINE.		06.9963
Eisenmenger Syndrome
[description not available]		05.2121
Eisenmenger Complex
A condition associated with VENTRICULAR SEPTAL DEFECT and other congenital heart defects that allow the mixing of pulmonary and systemic circulation, increase blood flow into the lung, and subsequent responses to low oxygen in blood. This complex is characterized by progressive PULMONARY HYPERTENSION; HYPERTROPHY of the RIGHT VENTRICLE; CYANOSIS; and ERYTHROCYTOSIS.		17.2121
Complex Regional Pain Syndrome
[description not available]		08.4311
Complex Regional Pain Syndromes
Conditions characterized by pain involving an extremity or other body region, HYPERESTHESIA, and localized autonomic dysfunction following injury to soft tissue or nerve. The pain is usually associated with ERYTHEMA; SKIN TEMPERATURE changes, abnormal sudomotor activity (i.e., changes in sweating due to altered sympathetic innervation) or edema. The degree of pain and other manifestations is out of proportion to that expected from the inciting event. Two subtypes of this condition have been described: type I; (REFLEX SYMPATHETIC DYSTROPHY) and type II; (CAUSALGIA). (From Pain 1995 Oct;63(1):127-33)		03.4311
Heart Disease, Ischemic
[description not available]		04.3441
Myocardial Ischemia
A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).		04.3441
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		02.0510
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		02.0510
Petechiae
Pinhead size (3 mm) skin discolorization due to hemorrhage.		02.0510
Angiitis
[description not available]		02.0510
Purpura
Purplish or brownish red discoloration, easily visible through the epidermis, caused by hemorrhage into the tissues. When the size of the discolorization is		07.0510
Vasculitis
Inflammation of any one of the blood vessels, including the ARTERIES; VEINS; and rest of the vasculature system in the body.		02.0510
Lymphangitis
A lymphatic disease characterized by INFLAMMATION of LYMPHATIC VESSELS.		07.0510
Sclerosis
A pathological process consisting of hardening or fibrosis of an anatomical structure, often a vessel or a nerve.		02.0510
Distorted Hearing
[description not available]		02.4620
Azotaemia
[description not available]		02.0510
Cor Pulmonale
[description not available]		02.0510
Intraocular Pressure
The pressure of the fluids in the eye.		07.0510
Acute Lymphoid Leukemia
[description not available]		02.0510
Bone Marrow Diseases
Diseases involving the BONE MARROW.		02.0510
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		02.0510
Brain Swelling
[description not available]		03.3620
Brain Edema
Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)		03.3620
HIV Coinfection
[description not available]		02.4420
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		02.4420
Hereditary Optic Neuroretinopathy
[description not available]		02.0610
Optic Atrophy, Hereditary, Leber
A maternally linked genetic disorder that presents in mid-life as acute or subacute central vision loss leading to central scotoma and blindness. The disease has been associated with missense mutations in the mtDNA, in genes for Complex I, III, and IV polypeptides, that can act autonomously or in association with each other to cause the disease. (from Online Mendelian Inheritance in Man, http://www.ncbi.nlm.nih.gov/Omim/, MIM#535000 (April 17, 2001))		02.0610
Adjuvant Arthritis
[description not available]		02.0610
Arthritis, Degenerative
[description not available]		02.0610
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		02.0610
Brachial Paresis
[description not available]		02.0710
Adhesions, Tissue
[description not available]		02.0710
Emergencies
Situations or conditions requiring immediate intervention to avoid serious adverse results.		02.0710
Aneurysm, Thoracic Aortic
[description not available]		02.0710
Aortic Dissection
[description not available]		07.0710
Hemothorax
Hemorrhage within the pleural cavity.		02.0710
Circulatory Collapse
[description not available]		02.0710
Aortic Aneurysm, Ruptured
[description not available]		02.0710
Shock
A pathological condition manifested by failure to perfuse or oxygenate vital organs.		02.0710
Aortic Aneurysm, Thoracic
An abnormal balloon- or sac-like dilatation in the wall of the THORACIC AORTA. This proximal descending portion of aorta gives rise to the visceral and the parietal branches above the aortic hiatus at the diaphragm.		02.0710
Central Nervous System Disease
[description not available]		02.9910
Idiopathic Parkinson Disease
[description not available]		02.9910
Cleft Spine
[description not available]		02.9910
Central Nervous System Diseases
Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.		02.9910
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		02.9910
Anxiety Neuroses
[description not available]		02.0710
Anxiety Disorders
Persistent and disabling ANXIETY.		02.0710
Vascular Diseases
Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.		02.0710
Diathesis
[description not available]		02.0710
Fournier Disease
[description not available]		02.0710
Abdominal Compartment Syndrome
[description not available]		02.0710
Cardio-Renal Syndrome
Condition where a primary dysfunction of either heart or kidney results in failure of the other organ (e.g., HEART FAILURE with worsening RENAL INSUFFICIENCY).		02.0710
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		02.0810
Cardiomyopathy, Congestive
[description not available]		02.9910
Cardiomyopathy, Dilated
A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.		02.9910
Genital Diseases, Male
Pathological processes involving the male reproductive tract (GENITALIA, MALE).		02.0810
Angiogenesis, Pathologic
[description not available]		03.4711
Neointima
The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.		07.0810
Cardiac Diseases
[description not available]		02.0110
Heart Diseases
Pathological conditions involving the HEART including its structural and functional abnormalities.		02.0110
Sexual and Gender Disorders
Mental disorders related to sexual dysfunction, paraphilias, and gender identity disorders.		02.9310
Angor Pectoris
[description not available]		04.6632
Blood Pressure, Low
[description not available]		06.2742
Angina Pectoris
The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION.		04.6632
Hypotension
Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.		06.2742
Tachyarrhythmia
[description not available]		02.9310
Tachycardia
Abnormally rapid heartbeat, usually with a HEART RATE above 100 beats per minute for adults. Tachycardia accompanied by disturbance in the cardiac depolarization (cardiac arrhythmia) is called tachyarrhythmia.		02.9310
Atrioventricular Nodal Re-Entrant Tachycardia
[description not available]		02.0210
Ventricular Fibrillation
A potentially lethal cardiac arrhythmia that is characterized by uncoordinated extremely rapid firing of electrical impulses (400-600/min) in HEART VENTRICLES. Such asynchronous ventricular quivering or fibrillation prevents any effective cardiac output and results in unconsciousness (SYNCOPE). It is one of the major electrocardiographic patterns seen with CARDIAC ARREST.		02.0210
Tachycardia, Ventricular
An abnormally rapid ventricular rhythm usually in excess of 150 beats per minute. It is generated within the ventricle below the BUNDLE OF HIS, either as autonomic impulse formation or reentrant impulse conduction. Depending on the etiology, onset of ventricular tachycardia can be paroxysmal (sudden) or nonparoxysmal, its wide QRS complexes can be uniform or polymorphic, and the ventricular beating may be independent of the atrial beating (AV dissociation).		02.0210
Coronary Heart Disease
[description not available]		03.8120
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		02.9310
Coronary Disease
An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels.		03.8120
Depression, Involutional
Form of depression in those MIDDLE AGE with feelings of ANXIETY.		02.0210
Depressive Disorder, Major
Disorder in which five (or more) of the following symptoms have been present during the same 2-week period and represent a change from previous functioning; at least one of the symptoms is either (1) depressed mood or (2) loss of interest or pleasure. Symptoms include: depressed mood most of the day, nearly every daily; markedly diminished interest or pleasure in activities most of the day, nearly every day; significant weight loss when not dieting or weight gain; Insomnia or hypersomnia nearly every day; psychomotor agitation or retardation nearly every day; fatigue or loss of energy nearly every day; feelings of worthlessness or excessive or inappropriate guilt; diminished ability to think or concentrate, or indecisiveness, nearly every day; or recurrent thoughts of death, recurrent suicidal ideation without a specific plan, or a suicide attempt. (DSM-5)		14.0210
Nasal Bleeding
[description not available]		02.0210
Epistaxis
Bleeding from the nose.		07.0210
Carotid Artery Narrowing
[description not available]		02.0210
Carotid Stenosis
Narrowing or stricture of any part of the CAROTID ARTERIES, most often due to atherosclerotic plaque formation. Ulcerations may form in atherosclerotic plaques and induce THROMBUS formation. Platelet or cholesterol emboli may arise from stenotic carotid lesions and induce a TRANSIENT ISCHEMIC ATTACK; CEREBROVASCULAR ACCIDENT; or temporary blindness (AMAUROSIS FUGAX). (From Adams et al., Principles of Neurology, 6th ed, pp 822-3)		02.0210
Electrocardiogram QT Prolonged
[description not available]		03.4111
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		03.4111
Nervous System Disorders
[description not available]		03.3520
Nervous System Diseases
Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.		03.3520
Esophageal Dysmotility
[description not available]		02.0210
Nasal Catarrh
[description not available]		03.4111
Rhinitis
Inflammation of the NASAL MUCOSA, the mucous membrane lining the NASAL CAVITIES.		03.4111
Hemorrhage, Retinal
[description not available]		02.0310
Choroid Hemorrhage
Hemorrhage from the vessels of the choroid.		02.0310
Uveal Neoplasms
Tumors or cancer of the UVEA.		02.0310
Liver Dysfunction
[description not available]		02.0310
Liver Diseases
Pathological processes of the LIVER.		02.0310
Atherogenesis
[description not available]		02.0310
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		02.0310
Brain Emboli
[description not available]		02.0310
Acute Onset Aura Migraine
[description not available]		02.0310
Auricular Fibrillation
[description not available]		02.0310
Atrial Fibrillation
Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation.		02.0310
Migraine with Aura
A subtype of migraine disorder, characterized by recurrent attacks of reversible neurological symptoms (aura) that precede or accompany the headache. Aura may include a combination of sensory disturbances, such as blurred VISION; HALLUCINATIONS; VERTIGO; NUMBNESS; and difficulty in concentrating and speaking. Aura is usually followed by features of the COMMON MIGRAINE, such as PHOTOPHOBIA; PHONOPHOBIA; and NAUSEA. (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)		02.0310
Periphlebitis
Periphlebitis is inflammation of the outer coat of a vein or of tissues surrounding the vein.		02.0310
Phlebitis
Inflammation of a vein, often a vein in the leg. Phlebitis associated with a blood clot is called (THROMBOPHLEBITIS).		07.0310
Abdominal Cramps
[description not available]		02.0310
Ureteral Diseases
Pathological processes involving the URETERS.		02.0310
Muscular Dystrophy, Animal
MUSCULAR DYSTROPHY that occurs in VERTEBRATE animals.		02.0310
Scotoma
A localized defect in the visual field bordered by an area of normal vision. This occurs with a variety of EYE DISEASES (e.g., RETINAL DISEASES and GLAUCOMA); OPTIC NERVE DISEASES, and other conditions.		02.0410
Lassitude
[description not available]		04.3411
Fatigue
The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.		04.3411
Brain Hemorrhage, Cerebral
[description not available]		02.0410
Cerebral Hemorrhage
Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA.		07.0410
Drug Overdose
Accidental or deliberate use of a medication or street drug in excess of normal dosage.		02.0410
Rheumatoid Arthritis
[description not available]		0210
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		0210