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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
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. [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]
| ID Source | ID |
|---|---|
| PubMed CID | 6918296 |
| CHEMBL ID | 1200969 |
| CHEBI ID | 521033 |
| SCHEMBL ID | 5903 |
| MeSH ID | M0281571 |
| Synonym |
|---|
| AB01274774-01 |
| avodart |
| dutasteride |
| gi-198745x |
| avidart |
| avolve |
| gg-745 |
| gi-198745 |
| duagen |
| 164656-23-9 |
| dutasteride (jan/usp/inn) |
| avodart (tn) |
| D03820 |
| 17beta-n-(2,5-bis(trifluoromethyl))phenyl-carbamoyl-4-aza-5alpha-androst-1-en-3-one |
| gi198745 |
| (5alpha,17beta)-n-(2,5-bis(trifluoromethyl)phenyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide |
| DB01126 |
| alpha,alpha,alpha,alpha',alpha',alpha'-hexafluoro-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxy-2',5'-xylidide |
| gi 198745 |
| 1h-indeno(5,4-f)quinoline-7-carboxamide, n-(2,5-bis(trifluoromethyl)phenyl)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4ar,4bs,6as,7s,9as,9bs,11ar)- |
| dutasteride [usan] |
| gg 745 |
| (5.alpha.,5 bis(trifluoromethyl)phenyl}-3-oxo-4-azaandrost-1-ene-17-carboxamide;dutasteride;avodart; |
| nsc-740477 |
| nsc740477 |
| duastride |
| nsc-759880 |
| CHEMBL1200969 , |
| (1s,3as,3bs,5ar,9ar,11as)-n-[2,5-bis(trifluoromethyl)phenyl]-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide |
| n-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide |
| chebi:521033 , |
| 4-azaandrost-1-ene-17-carboxamide, n-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-, (5a,17b)- |
| A810580 |
| (1s,3as,3bs,5ar,9ar,9bs,11as)-n-[2,5-bis(trifluoromethyl)phenyl]-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide |
| unii-o0j6xjn02i |
| nsc 759880 |
| dutasteride [usan:inn:ban] |
| nsc 740477 |
| o0j6xjn02i , |
| dtxsid8046452 , |
| dtxcid6026452 |
| tox21_112199 |
| cas-164656-23-9 |
| bdbm50340481 |
| BCP9000630 |
| AKOS015924431 |
| AKOS015920136 |
| BCPP000248 |
| dutasteride [usp-rs] |
| dutasteride [vandf] |
| jalyn component dutasteride |
| .alpha.,.alpha.,.alpha.,.alpha.',.alpha.',.alpha.'-hexafluoro-3-oxo-4-aza-5.alpha.-androst-1-ene-17.beta.-carboxy-2',5'-xylidide |
| dutasteride [inn] |
| dutasteride [mi] |
| dutasteride [usp monograph] |
| dutasteride [jan] |
| dutasteride [who-dd] |
| dutasteride [orange book] |
| dutasteride [ep monograph] |
| dutasteride component of jalyn |
| dutasteride [mart.] |
| (5.alpha.,17.beta.)-n-(2,5-bis(trifluoromethyl)phenyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide |
| S1202 |
| CS-1542 |
| HY-13613 |
| SCHEMBL5903 |
| gtpl7457 |
| (4ar,4bs,6as,7s,9as,9bs,11ar)-n-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxamide |
| Q-201052 |
| AB01274774_02 |
| (1s,2r,7r,10s,11s,14s,15s)-n-[2,5-bis(trifluoromethyl)phenyl]-2,15-dimethyl-5-oxo-6-azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxamide |
| mfcd00937869 |
| GS-3565 |
| dutasteride, united states pharmacopeia (usp) reference standard |
| dutasteride, european pharmacopoeia (ep) reference standard |
| dutasteride, >=98% (hplc) |
| dutasteride for system suitability, european pharmacopoeia (ep) reference standard |
| (5alpha,17beta)-n-{2,5-bis(trifluoromethyl)-phenyl}-3-oxo-4-azaandrost-1-ene-17-carboxamide |
| Q424760 |
| Z1558504346 |
| BCP02344 |
| BRD-K30373883-001-02-8 |
| 1h-indeno[5,4-f]quinoline-7-carboxamide, n-[2,5-bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4ar,4bs,6as,7s,9as,9bs,11ar)- |
| CCG-269904 |
| EX-A1952 |
| (4ar,4bs,6as,7s,9as,9bs,11ar)-n-[2,5-bis(trifluoromethyl)phenyl]-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-1h-indeno[5,4-f]quinoline-7-carboxamide |
| (5alpha,17beta)-n-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-azaandrost-1-ene-17-carboxamide |
| dutasteride for system suitability |
| dutasteride- bio-x |
| BD164398 |
| g04cb02 |
| dutasteridum |
| dutasterida |
| dutasteride (mart.) |
| dutasteride (usp monograph) |
| dutasteride (usp-rs) |
| dutasteride (ep monograph) |
| D5973 |
| EN300-124223 |
| (4ar,4bs,6as,7s,9as,9bs,11ar)-n-[2,5-bis(trifluoromethyl)phenyl]-4a,6a-dimethyl-2-oxo-1h,2h,4ah,4bh,5h,6h,6ah,7h,8h,9h,9ah,9bh,10h,11h,11ah-indeno[5,4-f]quinoline-7-carboxamide |
Dutasteride is a potent inhibitor of 5-alpha reductase enzymes that reduces concentrations of dihydrotestosterone to a greater extent than finasteride. The drug is an effective, safe and well-tolerated treatment either a monotherapy or a combination.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dutasteride is a specific and selective inhibitor of both 5α-reductase isoforms used mainly in benign prostatic hyperplasia and lower urinary tract symptoms. " | ( LC-MS/MS determination of dutasteride and its major metabolites in human plasma. Buś-Kwaśnik, K; Giebułtowicz, J; Gniazdowska, E; Kaza, M, 2021) | 2.36 |
| "The dutasteride add-on is a reasonable treatment option for male patients with LUTS who are not satisfied with tadalafil monotherapy." | ( Dutasteride add-on treatment to tadalafil for patients with benign prostatic enlargement is similarly effective as dutasteride add-on treatment to alpha blocker: a propensity-score matching analysis. Abe, N; Ishikawa, M; Kakizaki, H; Makino, S; Miyauchi, K; Wada, N, 2022) | 2.72 |
| "Dutasteride is a 5α-reductase inhibitor that is used for benign prostate hypertrophy and androgenetic alopecia." | ( Cerebral Venous Sinus Thrombosis Associated with Dutasteride Use. Cheon, K; Cho, BH; Choi, BK; Jung, JW; Lee, KY, 2020) | 1.53 |
| "Dutasteride is a 5alpha-reductase inhibitor in clinical use to treat endocrine conditions. " | ( Effect of the 5α-reductase enzyme inhibitor dutasteride in the brain of intact and parkinsonian mice. Caruso, D; Di Paolo, T; Litim, N; Melcangi, RC; Morissette, M, 2017) | 2.16 |
| "Dutasteride is a potent inhibitor of 5-alpha reductase enzymes that reduces concentrations of dihydrotestosterone to a greater extent than finasteride. " | ( A population-based study of the risk of osteoporosis and fracture with dutasteride and finasteride. Antoniou, T; Gomes, T; Ho, JM; Juurlink, DN; Macdonald, EM; Mamdani, MM; Tadrous, M; Yao, Z, 2018) | 2.16 |
| "Dutasteride is a pharmacologically important drug employed to treat prostate cancer. " | ( Deciphering the binding of dutasteride with human alpha-2-macroglobulin: Molecular docking and calorimetric approach. Ahsan, H; Ali, SS; Khan, FH; Siddiqui, T; Zia, MK, 2019) | 2.25 |
| "Dutasteride is a selective inhibitor of type 1 and type 2 isoforms of 5-α-reductase, an enzyme responsible for the conversion of testosterone to 5-α-dihydrotestosterone, approved as a treatment for symptomatic BPH." | ( Dutasteride for the treatment of benign prostatic hyperplasia. Kapoor, A; Wu, C, 2013) | 2.55 |
| "Dutasteride is an effective, safe and well-tolerated treatment either as monotherapy or in combination with an α-blocker, for the management of symptomatic BPH to improve symptoms, reduce the risk of acute urinary retention and risk for BPH-related surgery. " | ( Dutasteride for the treatment of benign prostatic hyperplasia. Kapoor, A; Wu, C, 2013) | 3.28 |
| "Dutasteride is suggestive to be an alternative treatment option to patients with AGA who do not clinically respond to finasteride in six months." | ( Effect of dutasteride 0.5 mg/d in men with androgenetic alopecia recalcitrant to finasteride. Choi, JW; Huh, CH; Jung, JY; Kim, BJ; Kwon, SH; Park, KC; Yeon, JH; Youn, SW, 2014) | 2.25 |
| "Dutasteride is a dual blocker of both the type-1 and type-2 isoform of SRD5A1 and is indicated in the treatment of benign prostate hyperplasia." | ( The anti-androgen drug dutasteride renders triple negative breast cancer cells more sensitive to chemotherapy via inhibition of HIF-1α-/VEGF-signaling. Bernemann, C; Götte, M; Hülsewig, C; Kiesel, L; Ruckert, C; von Wahlde, MK, 2015) | 1.45 |
| "Dutasteride is a 5-alpha reductase inhibitor used to treat benign prostatic hyperplasia. " | ( [CLINICOPATHOLOGICAL STUDY OF PROSTATE BIOPSY IN PATIENTS RECEIVING DUTASTERIDE FOR BENIGN PROSTATIC HYPERPLASIA]. Endo, T; Hiruta, N; Kamijima, S; Kamiya, N; Lee, FC; Nishimi, D; Oka, R; Suzuki, H; Takanami, M; Utsumi, T; Yano, M, 2015) | 2.1 |
| "Dutasteride is a new drug similar to finasteride, inhibits enzyme testosterone 5-alpha reductase, diminish symptoms of BPH, reduce risk of the complications and increases quality of life in patients with BPH." | ( Cost effectiveness comparison of dutasteride and finasteride in patients with benign prostatic hyperplasia--The Markov model based on data from Montenegro. Dabanović, V; Janković, S; Kostić, M, 2016) | 1.44 |
| "Dutasteride is a cost effective option for treating BPH comparing to finasteride. " | ( Cost effectiveness comparison of dutasteride and finasteride in patients with benign prostatic hyperplasia--The Markov model based on data from Montenegro. Dabanović, V; Janković, S; Kostić, M, 2016) | 2.16 |
| "Dutasteride is a 5 alpha-reductase (5AR) inhibitor currently being evaluated both for chemoprevention and treatment of prostate cancer." | ( Effects of the 5 alpha-reductase inhibitor dutasteride on gene expression in prostate cancer xenografts. Anderson, SK; Ballman, KV; Regan, KM; Schmidt, LJ; Sun, Z; Tindall, DJ, 2009) | 1.34 |
| "Dutasteride (Avodart) is a dual inhibitor of both type I and type II 5 alpha reductases, and thus inhibits conversion of testosterone to dihydrotestosterone, a key mediator of male pattern hair loss." | ( Efficacy, safety, and tolerability of dutasteride 0.5 mg once daily in male patients with male pattern hair loss: a randomized, double-blind, placebo-controlled, phase III study. Cho, HK; Eun, HC; Hong, SP; Ji, JH; Kim, BY; Kwon, OS; Lee, WS; Lew, BL; Park, HY; Ro, BI; Shin, HS; Sim, WY; Yeon, JH, 2010) | 2.07 |
| "Dutasteride is a dual inhibitor of type I and type II 5α-reductases and provides nearly complete suppression of dihydrotestosterone, which plays a key role in the aetiology and development of benign prostatic hyperplasia (BPH). " | ( Efficacy and safety of dutasteride in Chinese adults with symptomatic benign prostatic hyperplasia: a randomized, double-blind, parallel-group, placebo-controlled study with an open-label extension. Na, Y; Ye, Z; Zhang, S, 2012) | 2.13 |
| "Dutasteride has proved to be a safe and efficacious treatment for symptoms related to BPH. " | ( Dutasteride for the treatment of prostate-related conditions. Bubley, G; Dumas, C; Slater, S, 2012) | 3.26 |
| "Dutasteride is an inhibitor of 5α-reductase, an enzyme that is responsible for the conversion of testosterone to its active form dihydrotestosterone." | ( Dutasteride/tamsulosin fixed-dose combination for the treatment of benign prostatic enlargement. Hashim, H; Ismail, M, 2012) | 2.54 |
| "Dutasteride is a potent inhibitor of dihydrotestosterone production that is safe and effective in terms of the reduction of prostate volume and symptoms, flow rate improvement, and the reduction of the risk of acute urinary retention and surgery during a 24-month study period." | ( Efficacy and safety of a dual inhibitor of 5-alpha-reductase types 1 and 2 (dutasteride) in men with benign prostatic hyperplasia. Andriole, G; Boyle, P; Hoefner, K; Nickel, JC; Roehrborn, CG, 2002) | 1.99 |
| "Dutasteride is a new 5-alpha reductase inhibitor for the treatment of men with moderate to severe lower urinary tract symptoms secondary to benign prostatic hyperplasia. " | ( Dutasteride: a new 5-alpha reductase inhibitor for men with lower urinary tract symptoms secondary to benign prostatic hyperplasia. Brown, CT; Nuttall, MC, 2003) | 3.2 |
| "Dutasteride is a 5alpha-reductase inhibitor that inhibits both types 1 and 2 isozymes of 5alpha-reductase, the enzyme responsible for converting testosterone to dihydrotestosterone in the prostate and other tissues. " | ( Dutasteride: a potent dual inhibitor of 5-alpha-reductase for benign prostatic hyperplasia. Rabasseda, X, 2004) | 3.21 |
| "Dutasteride is a new dual 5alpha-reductase inhibitor for the treatment of benign prostatic hyperplasia. " | ( Dutasteride: a novel dual inhibitor of 5alpha-reductase for benign prostatic hyperplasia. Djavan, B; Fong, YK; Milani, S, 2005) | 3.21 |
| "Dutasteride is a specific selective inhibitor of the two isoenzymes, while finasteride is a selective inhibitor of type 2 -alpha-reductase." | ( [Effect of dutasteride on reduction of plasma DHT following finasteride therapy in patients with benign prostatic hyperplasia]. Botto, H; Comenducci, A; Lan, O; Poulain, JE, 2005) | 1.44 |
| "Dutasteride is a novel dual inhibitor of the 5 alpha-reductase enzymes and is currently in use both for treatment of benign prostate hyperplasia (BPH) and in the reduction by dutasteride of prostate cancer events (REDUCE) prostate cancer prevention trial." | ( Inhibition of fatty acid synthase activity in prostate cancer cells by dutasteride. Ballman, KV; Schmidt, LJ; Tindall, DJ, 2007) | 1.29 |
Dutasteride has a potential to improve BMD with elevation of serum testosterone in aging male patients with LUTS and prostatic enlargement. It has a role as an adjunct in the treatment of prostate cancer; but this is an area still under active investigation.
Dutasteride has been shown to increase expression of the prostate-specific membrane antigen (PSMA) in prostate cancer cells. It has been demonstrated to be effective in several randomized, double-blind, placebo controlled trials in androgenetic alopecia.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dutasteride has a potential to improve BMD with elevation of serum testosterone in aging male patients with LUTS and prostatic enlargement." | ( Dutasteride improves bone mineral density in male patients with lower urinary tract symptoms and prostatic enlargement: a preliminary study. Hashizume, K; Kakizaki, H; Matsumoto, S; Wada, N, 2016) | 3.32 |
| "Dutasteride has a role as an adjunct in the treatment of prostate cancer; however, this is an area still under active investigation." | ( Dutasteride for the treatment of prostate-related conditions. Bubley, G; Dumas, C; Slater, S, 2012) | 2.54 |
| "Dutasteride has been proposed as an effective therapy for frontal fibrosing alopecia (FFA)." | ( Effectiveness of dutasteride in a large series of patients with frontal fibrosing alopecia in real clinical practice. Hermosa-Gelbard, Á; Jaén-Olasolo, P; Moreno-Arrones, ÓM; Pindado-Ortega, C; Rodrigues-Barata, AR; Saceda-Corralo, D; Vañó-Galván, S, 2021) | 2.4 |
| "Dutasteride has been shown to increase expression of the prostate-specific membrane antigen (PSMA) in prostate cancer cells in previous in vitro studies. " | ( Impact of short-term Dutasteride treatment on prostate-specific membrane antigen expression in a mouse xenograft model. Burger, IA; Eberli, D; Kranzbühler, B; Prause, L; Rupp, NJ; Salemi, S; Sousa, R; Sulser, T, 2021) | 2.38 |
| "Dutasteride has been demonstrated to be effective in several randomized, double-blind, placebo controlled trials in androgenetic alopecia." | ( Dutasteride in Androgenetic Alopecia: An Update. Adil, M; Arif, T; Dorjay, K; Sami, M, 2017) | 2.62 |
| "Dutasteride has been shown to be more effective than finasteride in the treatment of AGA but is not yet a recommended therapy." | ( Androgens and hair loss. Alsantali, A; Shapiro, J, 2009) | 1.07 |
| "Dutasteride has been investigated in three multicenter studies involving 4325 men aged 50 years and above with benign prostatic hyperplasia." | ( Dutasteride: a potent dual inhibitor of 5-alpha-reductase for benign prostatic hyperplasia. Rabasseda, X, 2004) | 2.49 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Dutasteride can improve lower urinary tract symptoms by improving storage bladder function and relieving obstruction." | ( Urodynamic effects of dutasteride add-on therapy to alpha-adrenergic antagonist for patients with benign prostatic enlargement: prospective pressure-flow study. Hashizume, K; Kakizaki, H; Kita, M; Matsumoto, S; Wada, N, 2013) | 2.15 |
Dutasteride treatment significantly improved urinary symptoms and BMD in patients with low baseline serum TT and FT levels. The drug also reduced alcohol effects on the BAES sedation and SS anesthesia scales. Dutasterside treatment was associated with highly variable alterations in benign epithelial gene expression.
Dutasteride was well tolerated with no statistically significant increase in drug-related adverse events during the open-label extension. The adverse event profile was similar to that observed in the overall CombAT population.
In the presence or absence of tamsulosin, there were no apparent changes in dutasteride AUC and Cmax. Benign prostatic hyperplasia and prostate cancer can be treated with the 5α-reductase inhibitors, finasteride and dutasterside.
Curcumin combined with dutasteride suppressed proliferation and affected apoptosis of LNCaP cells.
| Excerpt | Reference | Relevance |
|---|---|---|
| "To evaluate the likelihood of alpha-adrenergic antagonist (alpha-blocker) discontinuation in combination with dutasteride or finasteride among patients aged > or =65 years with enlarged prostate." | ( Comparative analysis of alpha-blocker utilization in combination with 5-alpha reductase inhibitors for enlarged prostate in a managed care setting among Medicare-aged men. Davis, EA; Eaddy, MT; Issa, MM; Lin, PJ; Shah, MB, 2008) | 0.56 |
| "Curcumin combined with dutasteride suppressed proliferation and affected apoptosis of LNCaP cells." | ( Effects of Curcumin Combined With the 5-alpha Reductase Inhibitor Dutasteride on LNCaP Prostate Cancer Cells. Arai, G; Fukuda, K; Horie, S; Ide, H; Lu, Y; Nakayama, A; Okada, H; Osaka, A; Saito, K; Takei, A, ) | 0.68 |
Co-administration of the 5α-reductase inhibitor dutasteride increases the oral testosterone bioavailability in men with experimentally induced hypogonadism. Eudragit E nanoparticles containing a drug load of 5% showed an increase in bioavailability by 550% as compared to dutsasteride suspension.
The model derived from single dose data from healthy volunteers was considered to be valid for the prediction of DHT levels in the patient population. The preparation of a solid-supersaturatable SMEDDS with HPMC or Soluplus could be a promising formulation strategy to develop novel solid dosage forms of dutasteride.
| Role | Description |
|---|---|
| EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor | An EC 1.3.1.* (oxidoreductase acting on CH-CH group of donor, NAD(+) or NADP(+) as acceptor) inhibitor that interferes with the action of of 3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+)), EC 1.3.1.22, the enzyme which converts testosterone (CHEBI:17347) into the more potent androgen 5alpha-dihydrotestosterone. |
| antihyperplasia drug | A drug used for the treatment of hyperplasia (increaced cell production within an organ or tissue). |
| [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] | |
| Class | Description |
|---|---|
| aza-steroid | An aza-steroid is a steroid where in the carbon skeleton a carbon atom is replaced by nitrogen. |
| (trifluoromethyl)benzenes | An organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens. |
| delta-lactam | A lactam in which the amide bond is contained within a six-membered ring, which includes the amide nitrogen and the carbonyl carbon. |
| [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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| AR protein | Homo sapiens (human) | Potency | 18.4891 | 0.0002 | 21.2231 | 8,912.5098 | AID743040; AID743054 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 17.4159 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 5.5238 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743079; AID743080; AID743091 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 2.5119 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 3.3491 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 18.8336 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
| Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 29.8000 | 0.1100 | 7.1903 | 10.0000 | AID1473738 |
| 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0040 | 0.0017 | 0.4880 | 7.5000 | AID1573006 |
| 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Homo sapiens (human) | IC50 (µMol) | 0.0001 | 0.0001 | 0.5267 | 10.0000 | AID1573007 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glycine receptor subunit alpha-1 | Homo sapiens (human) | EC50 (µMol) | 0.3300 | 0.3200 | 1.4577 | 4.2000 | AID1203550 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1573006 | Inhibition of human type 1 5alpha reductase | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
| AID1473740 | Inhibition 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 assay | 2013 | Toxicological 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. |
| AID1272912 | Effect on organ weight in male wistar rat assessed as vas deferens tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=67.613+/-3.248 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1473741 | Inhibition 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 assay | 2013 | Toxicological 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. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1473739 | Inhibition 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 assay | 2013 | Toxicological 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. |
| AID1272908 | Effect on organ weight in male wistar rat assessed as dorsal prostate tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=50.325+/-7.519 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1473782 | Ratio of drug concentration at steady state in human at 0.5 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological 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. |
| AID1473781 | Drug concentration at steady state in human at 0.5 mg, po QD after 24 hrs | 2013 | Toxicological 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. |
| AID1203552 | Modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as effect on acetylcholine-induced currents at 10 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1203550 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1203549 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 1 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
| AID1272911 | Effect on organ weight in male wistar rat assessed as adrenal tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=14.762 +/-0.600 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1272905 | Increase in body weight gain in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=9.412+/-1.632g%) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug 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. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug 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. |
| AID1473738 | Inhibition 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 assay | 2013 | Toxicological 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. |
| AID1272913 | Effect on organ weight in male wistar rat assessed as epididymis tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=187.356+/- 5.961 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID591082 | Inhibition of Mycobacterium tuberculosis 3 beta hydroxysteriod dehydrogenase | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Inhibition of the M. tuberculosis 3β-hydroxysteroid dehydrogenase by azasteroids. |
| AID1272906 | Effect on organ weight in male wistar rat assessed as liver tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=2.994+/- 0.254 g/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
| AID1203551 | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents at 10 uM after 1 to 4 days by two-electrode voltage clamp assay relative to control | 2015 | Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7 | Ensemble-based virtual screening for cannabinoid-like potentiators of the human glycine receptor α1 for the treatment of pain. |
| AID1473780 | AUC in human at 0.5 mg, po QD after 24 hrs | 2013 | Toxicological 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. |
| AID1272907 | Effect on organ weight in male wistar rat assessed as ventral prostate tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=59.494+/- 4.733 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1272910 | Effect on organ weight in male wistar rat assessed testis tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=1054.099+/- 55.648 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1272909 | Effect on organ weight in male wistar rat assessed as seminal vesicles tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=175.439+/-12.833 mg/100g) | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors. |
| AID1573007 | Inhibition of human type 2 5alpha reductase | 2018 | Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14 | Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (0.72) | 18.2507 |
| 2000's | 173 (24.79) | 29.6817 |
| 2010's | 411 (58.88) | 24.3611 |
| 2020's | 109 (15.62) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (89.80) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 188 (25.82%) | 5.53% |
| Reviews | 131 (17.99%) | 6.00% |
| Case Studies | 16 (2.20%) | 4.05% |
| Observational | 8 (1.10%) | 0.25% |
| Other | 385 (52.88%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Randomized, Double-Blind, Placebo-Controlled Trial Assessing the Efficacy and Safety of Dutasteride in Extending the Time to Progression of Low-Risk, Localized Prostate Cancer in Men Who Are Candidates for or Undergoing Expectant Management [NCT00363311] | Phase 4 | 302 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| Drug Use Investigation for AVOLVE(BPH) [NCT01376284] | 1,000 participants (Actual) | Observational | 2010-12-31 | Completed | |||
| Establishing the Benefits of Adherence to Enlarged Prostate Treatment: A Validation Study Linking Adherence to Outcomes Using the Market Scan Database [NCT01381510] | 54,459 participants (Actual) | Observational | 2010-06-30 | Completed | |||
| A Biomarker Study of STA9090 in Castration-Resistant Prostate Cancer (CRPC) With Assessment of Androgen Receptor Pathway Signaling [NCT01368003] | Phase 2 | 0 participants (Actual) | Interventional | 2011-04-30 | Withdrawn(stopped due to Loss of funding.) | ||
| Biomarker Study Targeting Abiraterone Metabolites and Polymporphisms in Men With PSA Progression on Abiraterone for the Treatment of Castration Resistant or Castration Sensitive Prostate Cancer (The Bio-STAMP Study) [NCT05705700] | Phase 2 | 0 participants (Actual) | Interventional | 2023-02-28 | Withdrawn(stopped due to Feasibility) | ||
| A Phase II Neoadjuvant Study of Enzalutamide, Abiraterone Acetate, Dutasteride and Degarelix in Men With Localized Prostate Cancer Pre-prostatectomy [NCT02159690] | Phase 2 | 0 participants (Actual) | Interventional | 2014-09-30 | Withdrawn(stopped due to loss of funding) | ||
| Apoptosis and Expression of Neovascularization-related Factors in Human Prostate Tissue After Administration of Dutasteride [NCT00880672] | Phase 4 | 40 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| A Single-Dose, Randomised, Open-Label, Two-Period Crossover Study to Determine the Bioequivalence of the Second Generation Dutasteride and Tamsulosin HCl Combination Capsule in the Fed State in Healthy Adult Male Subjects [NCT02058576] | Phase 1 | 77 participants (Actual) | Interventional | 2014-02-11 | Completed | ||
| Mechanisms of Hormonal Control of Spermatogenesis in Man [NCT02147964] | Phase 2 | 0 participants (Actual) | Interventional | 2019-06-30 | Withdrawn(stopped due to No funding was obtained for this study.) | ||
| Economic Analyses Alongside the REDUCE Clinical Trial [NCT01337258] | 1 participants (Actual) | Observational | 2010-01-31 | Completed | |||
| Effect of 5α Reductase Inhibitor Dutasteride on the Prevention of the Prostate Cancer in Men With High Grade Intraepithelial Neoplasia of the Prostate [NCT00780754] | Phase 3 | 200 participants (Anticipated) | Interventional | 2007-04-30 | Completed | ||
| Benefits of Adherence to 5-alpha Reductase Inhibitor Treatment in Men With Enlarged Prostate: An Assessment of Medicare and Medicaid Patients Using the MarketScan Database [NCT01376258] | 28,903 participants (Actual) | Observational | 2010-10-31 | Completed | |||
| Dutasteride Treatment for Reducing Heavy Drinking in AUD: Predictors of Efficacy [NCT04098302] | Phase 2/Phase 3 | 180 participants (Actual) | Interventional | 2019-10-15 | Active, not recruiting | ||
| An Open-label, Randomized, Single Dose, Two-Period Crossover Study to Determine the Bioavailability of a Fixed Dose Combination Capsule Formulation of Dutasteride and Tamsulosin Hydrochloride (0.5mg/0.2mg) Relative to Co-administration of Dutasteride 0.5m [NCT01254071] | Phase 1 | 86 participants (Actual) | Interventional | 2010-09-10 | Completed | ||
| Single Site, Phase II, Double Blind, Randomized, Placebo Controlled Study of the Effect of Dutasteride (Avodart) 0.5mg on the Volume and Characteristics of Prostate Cancer, as Assessed by Multifunctional Magnetic Resonance Imaging (MRI) With Lower Risk Pr [NCT01193855] | Phase 2 | 42 participants (Anticipated) | Interventional | 2010-06-30 | Recruiting | ||
| A Pilot Study of MRI and Spectroscopy Imaging Changes With 6-months of Dutasteride in Patients With Symptomatic Benign Prostatic Hypertrophy and Low-risk Prostate Cancer on Watchful Waiting or Requiring Neoadjuvant Androgen Suppression Prior to Prostate B [NCT00706966] | 10 participants (Actual) | Interventional | 2005-06-30 | Completed | |||
| Comparative Efficacy of DuodartTM Versus Watchful Waiting With Step-up Therapy to Tamsulosin in the Management of Treatment naïve Men With Symptomatic BPH [NCT01294592] | Phase 4 | 742 participants (Actual) | Interventional | 2010-12-22 | Completed | ||
| Subjective and Physiological Effects of Alcohol: Role of Genetic Variation and Adrenal Hormones [NCT00734656] | 94 participants (Actual) | Interventional | 2007-03-31 | Completed | |||
| A Phase I/II Trial of Ketoconazole, Hydrocortisone, Dutasteride and Lapatinib (KHAD-L) in Castration Resistant Prostate Cancer With Pre- and Post-therapy Tumor Biopsies [NCT00953576] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2009-09-29 | Terminated(stopped due to The study terminated early due to concerns about drug toxicity.) | ||
| "Dutasteride in Men Receiving Testosterone Therapy: Impact on Serum PSA, Testosterone, DHT Levels and Prostate Volume: Implications for Prostate Safety" [NCT00752869] | Phase 4 | 24 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| An Open Label, Randomized, Repeat Dose, 3 Period Crossover Study to Determine the Bioequivalence of 3 Different Formulations of Tamsulosin at Steady State in Healthy Male Volunteers [NCT00609596] | Phase 1 | 24 participants (Actual) | Interventional | 2008-02-26 | Completed | ||
| Pharmacokinetic Study of Single Dose Dutasteride in Healthy Subjects [NCT00802321] | 40 participants (Actual) | Interventional | 2006-04-30 | Completed | |||
| [NCT02839122] | Phase 1 | 28 participants (Actual) | Interventional | 2016-05-31 | Completed | ||
| ARI103094-Follow-Up Study for REDUCE Study Subjects [NCT00883909] | 2,795 participants (Actual) | Observational | 2009-04-09 | Completed | |||
| A Single-Dose, Randomised, Open-Label, Two-Period Crossover Study to Determine the Bioequivalence of the Second Generation Dutasteride and Tamsulosin HCl Combination Capsule in the Fasted State in Healthy Adult Male Subjects [NCT02052713] | Phase 1 | 78 participants (Actual) | Interventional | 2014-02-19 | Completed | ||
| 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 1 | 36 participants (Actual) | Interventional | 2017-03-27 | Completed | ||
| A Long-term Extension Study of GI198745 in Subjects With Benign Prostatic Hyperplasia [NCT00969072] | Phase 2 | 121 participants (Actual) | Interventional | 2003-08-31 | Completed | ||
| A Randomized, Double-blind, Parallel Group Study to Investigate the Efficacy and Safety of Treatment With Dutasteride (0.5mg) and Tamsulosin (0.4mg), Administered Once Daily for 4 Years, Alone and Combination, on the Improvement of Symptoms and Clinical O [NCT00090103] | Phase 3 | 4,844 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
| A Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study of the Efficacy and Safety of Dutasteride 0.5 mg Administered Orally Once Daily for Four Years to Reduce the Risk of Biopsy-Detectable Prostate Cancer [NCT00056407] | Phase 3 | 8,231 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| A Randomized Phase II Trial on the Addition of Dutasteride to Combined Androgen Blockade Therapy Versus Combined Androgen Blockade Therapy Alone in Patients With Recurrent and/or Metastatic Salivary Duct Carcinoma - DUCT Study [NCT05513365] | Phase 2 | 98 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
| Effect of Dutasteride on Androgen-Response Gene Expression During the Tumor Regrowth Phase of Intermittent Androgen Ablation Therapy in Patients With Advanced Prostate Cancer [NCT00668642] | Phase 2 | 20 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
| A Randomized, Open-label, Single-dose, Crossover Study to Evaluate the Pharmacokinetics and Safety of AD-208 [NCT04214808] | Phase 1 | 24 participants (Actual) | Interventional | 2020-01-03 | Completed | ||
| Phase II Trial of Exogenous Testosterone Plus Dutasteride for the Treatment of Castrate Metastatic Prostate Cancer [NCT00853697] | Phase 2 | 6 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Exploratory Clinical Trial of Safety and Efficacy of Daily Application of Topical Dutasteride in Men With Androgenic Alopecia. [NCT05599243] | Phase 2 | 45 participants (Anticipated) | Interventional | 2022-09-29 | Active, not recruiting | ||
| Clinical Evaluation of Dutasteride in Benign Prostatic Hyperplasia: A Randomized, Double-Blind, Placebo-Controlled, Parallel Group Comparative Study of GI198745 (Dutasteride) in Subjects With Benign Prostatic Hyperplasia. [NCT00368979] | Phase 3 | 378 participants (Actual) | Interventional | 2006-02-17 | Completed | ||
| Switch Study: Are There Any Measurable Differences When Switching Patients on Finasteride Therapy to Dutasteride? [NCT00690950] | Phase 4 | 50 participants (Anticipated) | Interventional | 2008-05-31 | Enrolling by invitation | ||
| The Effect of Male Hormonal Contraceptive Regimens on Prostate Tissue In Normal Men [NCT00490555] | Phase 2/Phase 3 | 32 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Bioequivalence Study of Dutasteride Capsules-An Evaluation of the Bioequivalence of Dutasteride Capsule Manufactured at GSK Compared to Dutasteride Capsule Manufactured at Catalent in Healthy Japanese Male Subjects [NCT02578953] | Phase 1 | 36 participants (Actual) | Interventional | 2015-09-09 | Completed | ||
| Randomized, Double-Blind, Placebo-Controlled Trial Assessing The Efficacy And Safety Of Dutasteride At Improving Lower Urinary Tract Symptoms In Men With Clinically Localized Prostate Cancer Being Treated With Single-Dose Goserelin, Trans-Urethral Incisio [NCT00805701] | Phase 4 | 40 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Metabolic Effects of Testosterone Alone or in Combination With Dutasteride or Anastrazole in Obese Men [NCT00983554] | 57 participants (Actual) | Interventional | 2005-06-30 | Active, not recruiting | |||
| A Randomised, Double-Blind, Placebo-Controlled Trial Assessing the Efficacy and Safety of Dutasteride (AVODART™) 0.5 mg in Extending the Time to PSA Doubling in Men With Prostate Cancer and Biochemical Failure (PSA Increase) After Radical Therapy With Cur [NCT00558363] | Phase 2 | 294 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| A Feasibility Study of Oral Hormonal Therapy and Radiation for Non-metastatic, Intermediate or High Risk Prostate Cancer in Men 70 and Older or With Medical Comorbidities [NCT01342367] | 74 participants (Actual) | Interventional | 2010-12-17 | Active, not recruiting | |||
| Effect of Dutasteride on Bladder Wall Hypertrophy in Patients With Benign Prostatic Obstruction: A 24-Week Open-Label, Single-Arm Pilot Study [NCT00827814] | Phase 4 | 36 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| An Randomised, Double-blind, Placebo-controlled, Parallel Group Study to Assess the Efficacy and Safety of Dutasteride 0.5mg Once Daily for 6 Months in the Treatment of Male Subjects With Androgenetic Alopecia (Norwood-Hamilton Classification Type IIIv, I [NCT00441116] | Phase 3 | 153 participants (Actual) | Interventional | 2006-12-15 | Completed | ||
| Phase II Clinical Trial to Examine the Efficacy and Safety of Dutasteride in Patients With Kennedy's Disease (Spinal and Bulbar Muscular Atrophy) [NCT00303446] | Phase 2 | 57 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| [NCT01942551] | Phase 1 | 47 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
| Effects of Dutasteride on Intraprostatic Dihydrotestosterone (DHT) Levels [NCT00062790] | Phase 4 | 50 participants | Interventional | 2003-10-31 | Completed | ||
| An Open Label, Single Sequence, Three Period, Drug-Drug Interaction Study To Examine The Pharmacokinetics Of Dutasteride And Tamsulosin And Their Interactions In Chinese Male Healthy Volunteers [NCT01957189] | Phase 1 | 24 participants (Actual) | Interventional | 2013-10-25 | Completed | ||
| Oral Androgens in Man-4: Gonadotropin Suppression Medicated by Oral Testosterone Enanthate in Oil Plus Dutasteride (Short Title: Oral T-4) [NCT00399165] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Testosterone Replacement and Dutasteride Effectiveness (TRADE) [NCT00194675] | Phase 4 | 53 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| A Randomized Double-Blind Parallel Group Study Comparing Casodex (or Generic Equivalent) 50mg Plus Placebo to Casodex (or Generic Equivalent) 50mg Plus Dutasteride 3.5mg Administered for 18 Months to Men With Prostate Cancer Who Have Failed First-Line And [NCT00470834] | Phase 4 | 127 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
| A Randomized Double-blind Placebo-controlled Pilot Trial on the Effects of Testosterone Undecanoate Plus Dutasteride or Placebo on Muscle Strength, Body Composition and Metabolic Profile in Transmen [NCT04545450] | Phase 3 | 16 participants (Actual) | Interventional | 2008-11-04 | Completed | ||
| 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 3 | 667 participants (Actual) | Interventional | 2021-07-27 | Completed | ||
| An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance to Monitor the Safety and Effectiveness of AVODART® Administered in Korean Androgenetic Alopecia Patients According to the Prescribing Information [NCT01004809] | 712 participants (Actual) | Observational | 2010-04-29 | Completed | |||
| A Randomized, Double-blind, Placebo-controlled, Six-month Parallel-group Study to Assess Efficacy and Safety of Dutasteride 0.5mg Once Daily in Chinese Patients With Benign Prostatic Hyperplasia (BPH), Followed by a 12-month Open-label Treatment Phase [NCT00527605] | Phase 3 | 253 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
| A Study of the Efficacy and Safety of Multiple Doses of Dutasteride Versus Placebo and Finasteride in the Treatment of Male Subjects With Androgenetic Alopecia [NCT01231607] | Phase 3 | 917 participants (Actual) | Interventional | 2010-10-28 | Completed | ||
| Phase 4 Study of Dual Five Alpha Reductase Inhibition Combined With Alpha Blockade in Men With Refractory Urinary Retention Secondary to BPH [NCT00680680] | 20 participants (Anticipated) | Interventional | 2004-05-31 | Completed | |||
| Placebo Controlled Pilot Study of Dutasteride for the Reduction of Alcohol Use in Male Drinkers [NCT01262287] | Phase 4 | 47 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| An Open-label, Randomized, Single Dose, Four-Period Crossover Study to Compare the Bioavailability of Fixed Dose Combination Capsule Formulations of Dutasteride and Tamsulosin Hydrochloride (0.5 mg/0.2 mg) With 10% and 15% of Enteric Coated Pellets With H [NCT01471678] | Phase 1 | 27 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| An Open-label, Randomized, Single Dose, Multi-stage, Cross-over Study to Determine the Relative Bioavailability of Fixed Dose Combination Products Containing a 3-oblong Dutasteride Soft Gel Capsule and Tamsulosin (0.5 mg Dutasteride /0.2 mg Tamsulosin HCl [NCT01495026] | Phase 1 | 63 participants (Actual) | Interventional | 2011-11-06 | Completed | ||
| An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance to Monitor the Safety and/or Efficacy of AVODART(Dutasteride) Administered in Korean BPH(Benign Prostatic Hyperplasia) Patients According to the Prescribing Information [NCT01299571] | 3,977 participants (Actual) | Observational | 2004-12-31 | Completed | |||
| Multi Center Double Blind Study Comparing 0.5 mg Dutasteride vs Placebo Daily in Men Receiving Intermittent Androgen Ablation Therapy for Prostate Cancer [NCT00553878] | Phase 2/Phase 3 | 100 participants (Anticipated) | Interventional | 2007-03-31 | Completed | ||
| A Pivotal, Open-label Trial Assessing the Safety and Efficacy of the 0.5 mg Dutasteride and 0.4 mg Tamsulosin Combination Once Daily for Six Months in Patients With Benign Prostatic Hyperplasia [NCT01673490] | Phase 4 | 59 participants (Actual) | Interventional | 2012-06-29 | Terminated(stopped due to The sole investigative site refused to accept the amended protocol and declined to continue the study. There was no safety signal nor any other reason.) | ||
| A Pilot Investigation of Dutasteride (Avodart) After Failure of Finasteride (Proscar) In the Management of Symptomatic Prostatic Enlargement/Hypertrophy (BPE/H) [NCT00382356] | 20 participants (Actual) | Interventional | 2004-11-30 | Completed | |||
| A Randomized Trial of Tamsulosin and/or Dutasteride Versus Placebo to Relieve Urinary Symptoms After Brachytherapy for the Treatment of Localized Prostate Cancer [NCT00244309] | Phase 3 | 348 participants (Anticipated) | Interventional | 2005-11-30 | Completed | ||
| A Randomized, Placebo-Controlled, Double-Blind Study of the Use of Dutasteride for Improving Peri-Operative and Long-Term Outcomes of Photoselective Vaporization of the Prostate (DOP Study) [NCT00274417] | 60 participants | Interventional | 2006-01-31 | Active, not recruiting | |||
| The Effects of Dutasteride on Mood, HPA Axis, and Serum Allopregnanolone Levels in Women With Menstrual-Related Mood Disorders and Controls [NCT00082043] | Phase 1 | 34 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| Prostate Medication, Metabolism and Gut Microbiota [NCT06001619] | Phase 4 | 100 participants (Anticipated) | Interventional | 2022-12-01 | Recruiting | ||
| An Open Label Study to Evaluate the Impact of Novel Fixed-dose Testosterone/Dutasteride Combinations on the Relative Bioavailability of the Individual Dutasteride and Testosterone Components [NCT00400335] | Phase 1 | 60 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| The Role of 5-alpha Reductase in Mediating Testosterone Actions [NCT00493987] | Phase 4 | 184 participants (Anticipated) | Interventional | 2002-11-30 | Completed | ||
| Oral Androgens in Man-3: Pharmacokinetics of Oral Testosterone With Concomitant Inhibition of 5α-Reductase by Dutasteride Short Title: ORAL T-3 [NCT00161421] | Phase 2 | 18 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| A Randomized, Double-blind, Placebo-controlled, Study of Safety and Efficacy of Dutasteride in Combination With Tolterodine ER or Placebo in Men With Lower Urinary Tract Symptoms (LUTS) Including Urgency and Frequency [NCT00939120] | Phase 4 | 46 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| A Randomised, Double-Blind, Placebo-Controlled, Multicentre Phase IV Study to Evaluate the Efficacy and Safety of Dutasteride 0.5mg Administered Orally Daily for 24 Weeks to Reduce The Risk of Acute Urinary Retention Relapse Following Successful Trial Wit [NCT00421421] | Phase 4 | 276 participants | Interventional | 2007-03-31 | Terminated(stopped due to Incomplete information) | ||
| Assessment of Response of Patients on Surveillance for Favorable Risk Prostate Cancer to Dutasteride [NCT01525914] | 100 participants (Actual) | Observational | 2010-05-31 | Completed | |||
| Detection of Prostate Cancer With Contrast-Enhanced Ultrasound After Treatment With Dutasteride [NCT00398281] | Phase 3 | 450 participants (Anticipated) | Interventional | 2006-11-30 | Completed | ||
| A Phase II, 28-Day, Randomized, Parallel-Group, Open-Label Study Evaluating the Efficacy and Safety of Twice Daily Oral Doses of Testosterone (150-400mg) Co-administered With 0.25mg Dutasteride Compared With 400mg Testosterone Alone and 0.25mg Dutasteride [NCT00398580] | Phase 2 | 43 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| An Open-Label, Randomized, Single Dose Crossover Study to Determine the Bioequivalence of Duodart® 0.5mg/0.4mg (Capsule Formulation of Dutasteride 0.5mg and Tamsulosin Hydrochloride 0.4mg) Compared to Concomitant Dosing of Avodart® 0.5mg and Omnic® 0.4mg [NCT01657851] | Phase 1 | 35 participants (Actual) | Interventional | 2012-08-23 | Completed | ||
| Phase II Study of Dutasteride in Prostate Cancer Recurrent During Androgen Deprivation Therapy [NCT00403000] | Phase 2 | 27 participants (Actual) | Interventional | 2004-12-31 | Completed | ||
| Role of Testosterone and Its Metabolites Regarding Different Physiological Functions in Subjects Affected by Gender Identity Disorder (FtM Transsexuals) [NCT00146146] | Phase 3 | 15 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
| Early Antiandrogen Treatment (EAT) With Dutasteride for COVID-19 (EAT-DUTA AndroCoV Trial) [NCT04729491] | Phase 2/Phase 3 | 138 participants (Actual) | Interventional | 2020-06-30 | Completed | ||
| Phase II Trial of Abiraterone Acetate Combined With Dutasteride With Correlative Assessment of Tumor Androgen Levels and Androgen Receptor Sequence and Signaling at Baseline and at Progression [NCT01393730] | Phase 2 | 40 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| A Phase II Trial of Ketoconazole, Hydrocortisone and Dutasteride in Asymptomatic Hormone Refractory Prostate Cancer [NCT00673127] | Phase 2 | 57 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
| A Multi-center Randomized Placebo Controlled Trial Evaluating the Efficacy of JALYN in Improving Symptoms in Men Diagnosed With Benign Prostatic Hyperplasia (BPH) and Chronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS) [NCT01830829] | Phase 3 | 1 participants (Actual) | Interventional | 2013-04-30 | Terminated(stopped due to Difficulty in enrolling particpants) | ||
| Mechanisms of Testosterone-Driven Growth-Hormone (GH) Secretion in Aging Men: Modulation of GHRH, GHRP and Somatostatin Action by Estrogenic Versus Androgenic Steroids [NCT00309855] | Phase 1 | 80 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Demonstrating the Clinical and Economic Benefit of 5 Alpha Reductase Inhibitor Adherence in Benign Prostatic Hyperplasia [NCT01334723] | 35,032 participants (Actual) | Observational | 2010-04-30 | Completed | |||
| A Prospective Study of Sexual Function in Sexually Active Men Treated for BPH [NCT01777269] | Phase 4 | 489 participants (Actual) | Interventional | 2013-02-18 | Completed | ||
| A Randomized, Open-label, Parallel-group Study, to Assess the Pharmocodynamic Effect on Dihydrotestosterone Regulated Gene Expression, Longitudinally and in a Dose Dependent Manner, of 0.5mg and 3.5mg Dutasteride Administered Orally Once Daily, for One Ye [NCT00375765] | Phase 4 | 40 participants | Interventional | 2005-04-30 | Completed | ||
| Clinical Progression and Costs in Benign Prostatic Hyperplasia Patients Treated With Early Versus Delayed Combination Therapy [NCT01435954] | 13,551 participants (Actual) | Observational | 2010-08-31 | Completed | |||
| A Randomized, Double-blind, Parallel Group Study to Compare the Efficacy and Safety of Combination Treatment With Dutasteride (0.5mg) and Tamsulosin (0.2mg) With Tamsulosin (0.2mg) Monotherapy, Administered Once Daily for 2 Years, on the Improvement of Sy [NCT02058368] | Phase 3 | 607 participants (Actual) | Interventional | 2014-02-10 | Completed | ||
| A Phase II Study of Enzalutamide Plus Dutasteride/Finasteride as First Line Treatment for Vulnerable Patients ≥ 65 Years With Systemic Prostate Cancer [NCT02213107] | Phase 2 | 40 participants (Anticipated) | Interventional | 2014-09-30 | Active, not recruiting | ||
| An Open-label, Single Dose, Randomized, Two-period Crossover Study to Investigate the Bioavailability of a Novel Dosage Form of Dutasteride in Healthy Male Subjects [NCT01577693] | Phase 1 | 35 participants (Actual) | Interventional | 2011-05-12 | Completed | ||
| R01 CA155301: Validation of Digital Morphometry for Cancer Risk in Benign Prostate Biopsies [NCT01594502] | 139 participants (Actual) | Observational | 2011-09-30 | Completed | |||
| An Open Label Study of 5α-reductase Inhibition on the Regulation of Insulin Action and Metabolic Phenotype in Healthy Volunteers. [NCT01923090] | Phase 2 | 12 participants (Anticipated) | Interventional | 2012-08-31 | Recruiting | ||
| An Evaluation of the Bioequivalence of Five 0.1 mg GI198745/Dutasteride Soft Gelatin Capsules Compared to One 0.5 mg GI198745/Dutasteride Gelatin Capsules in Healthy Male Volunteers [NCT01929330] | Phase 1 | 36 participants (Actual) | Interventional | 2013-09-23 | Completed | ||
| Role of Dutasteride in Treatment of Category IIIB Chronic Prostatitis (A Placebo-Controlled Study) [NCT04756206] | Phase 2/Phase 3 | 50 participants (Actual) | Interventional | 2019-01-01 | Completed | ||
| Mechanisms of Control of the Intratesticular Hormonal Milieu in Man [NCT01215292] | Phase 1/Phase 2 | 46 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Prospective Study of Sexual Function in Men Taking Dutasteride for the Treatment of Androgenetic Alopecia [NCT02014584] | Phase 3 | 117 participants (Actual) | Interventional | 2014-07-02 | Completed | ||
| Maximal Suppression of the Androgen Axis in Clinically Localized Prostate Cancer [NCT00298155] | Phase 2 | 35 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| A Randomized, Open-label, Phase 2 Study Of Mdv3100 As A Neoadjuvant Therapy For Patients Undergoing Prostatectomy For Localized Prostate Cancer [NCT01547299] | Phase 2 | 52 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| A Phase I Study of PCUR-101 in Combination With Androgen Directed Therapy in the Treatment of Patients With Metastatic Castration-Resistant Prostate Cancer [NCT04677855] | Phase 1 | 48 participants (Anticipated) | Interventional | 2021-03-30 | Recruiting | ||
| 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 1 | 54 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
| A Randomized Placebo-Controlled Double-Blind Clinical Trial to Assess the Role of Dutasteride in Patients Undergoing 3D Mapping Biopsy in Early Stage Prostate Cancer [NCT00985738] | Phase 2 | 16 participants (Actual) | Interventional | 2009-09-30 | Terminated(stopped due to Low recruitment) | ||
| A Randomized, Placebo-Controlled, Double-Masked Clinical Trial Comparing Laser TURP With and Without Neo-Adjuvant Dutasteride [NCT00431626] | Phase 3 | 4 participants (Actual) | Interventional | 2006-10-31 | Terminated(stopped due to Low enrollment) | ||
| Dutasteride Treatment for the Reduction of Heavy Drinking [NCT01758523] | Phase 4 | 189 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| An Open-label, Randomized, Single Dose, Two-way Crossover Study to Determine the Bioavailability of One Fixed Dose Combination Capsule Formulation of Dutasteride and Tamsulosin Hydrochloride (0.5 mg/0.2 mg) Relative to Coadministration of One Dutasteride [NCT02509104] | Phase 1 | 56 participants (Actual) | Interventional | 2015-07-30 | Completed | ||
| Clinical and Economic Outcomes of Patients Utilizing Combination Therapy for Enlarged Prostates: A Henry Ford Database Assessment [NCT01386983] | 332 participants (Actual) | Observational | 2009-03-31 | Completed | |||
| Study ARI114264: A Long-Term Study of the Safety and Efficacy of Dutasteride in the Treatment of Male Subjects With Androgenetic Alopecia [NCT01831791] | Phase 3 | 120 participants (Actual) | Interventional | 2013-04-14 | Completed | ||
| Phase II Study of Bicalutamide and Dutasteride for Prostate Cytoreduction Prior to Permanent Implant I-125 Prostate Brachytherapy [NCT00866554] | Phase 2 | 60 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Molecular Mechanisms of Dutasteride and Dietary Interventions to Prevent Prostate Cancer and Reduce Its Progression [NCT01653925] | 120 participants (Actual) | Interventional | 2010-11-30 | Active, not recruiting | |||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
"The occurrence and quantity of high-grade prostatic intraepithelial neoplasia (HGPIN) and atypical small acinar proliferation (ASAP) at biopsy were measured. HGPIN and ASAP are considered precancerous conditions. A participant diagnosed with prostate cancer only (i.e., no HGPIN or ASAP) was counted in both the first category (HGPIN or prostate cancer diagnosis) and again in the last category (HGPIN, ASAP, or prostate cancer diagnosis)." (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| HGPIN or prostate cancer diagnosis | HGPIN and no prostate cancer | HGPIN and no ASAP and no prostate cancer | HGPIN or ASAP | HGPIN or ASAP and no prostate cancer | HGPIN, ASAP, or prostate cancer diagnosis | |
| Dutasteride 0.5 mg | 810 | 151 | 121 | 409 | 248 | 907 |
| Placebo | 1126 | 268 | 206 | 675 | 373 | 1231 |
Medication taken during the study, including alpha blockers, was recorded at each 6-month study visit and during phone calls that occurred 3 months after each visit. (NCT00056407)
Timeframe: Years 1-2, Overall (Years 1-4)
| Intervention | participants (Number) | |
|---|---|---|
| Years 1-2 | Overall | |
| Dutasteride 0.5 mg | 317 | 515 |
| Placebo | 425 | 770 |
Prostate volume was measured by transrectal ultrasound (TRUS) when biopsies were performed at Year 2 and Year 4. The investigator calculated the prostate volume using three prostate measurements (anteroposterior, cephalocaudal, and transverse diameters). Estimates are based on the adjusted means from the general linear model: log(Post-Baseline/Baseline value) = treatment and cluster and log (baseline value). (NCT00056407)
Timeframe: Baseline, Month 24, and Month 48
| Intervention | percent change (Mean) | |
|---|---|---|
| Month 24, n=3192, 3116 | Month 48, n=3289, 3194 | |
| Dutasteride 0.5 mg | -17.4 | -17.5 |
| Placebo | 13.0 | 19.7 |
Maximum urinary flow was measured at selected sites using a Dantec Uroflow meter with a Thompson filter. Change from baseline was calculated as Month 12, 24, 36, and 48 values minus the baseline value. Estimates are based on the adjusted means from the general linear model: change from baseline = baseline Qmax and treatment. This measurement was performed at selected centers. (NCT00056407)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | milliliters/second (Mean) | |||
|---|---|---|---|---|
| Month 12, n=1178, 1168 | Month 24, n=1337, 1295 | Month 36, n=1375, 1334 | Month 48, n=1390, 1359 | |
| Dutasteride 0.5 mg | 0.27 | 0.60 | 0.13 | 0.41 |
| Placebo | -0.55 | -0.63 | -0.74 | -0.90 |
The amount of prostate biopsy tissue with HGPIN was measured. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | cc*10^-3 (microliter) (Mean) |
|---|---|
| Placebo | 0.1105 |
| Dutasteride 0.5 mg | 0.0446 |
The average amount of cancer seen by the pathologist in the prostate tissue samples taken during the biopsy was measured. A core is a prostate biopsy sample. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | percentage of core (Mean) |
|---|---|
| Placebo | 13.4 |
| Dutasteride 0.5 mg | 12.2 |
Participants reported events of macroscopic hematuria (visible blood in the urine) throughout the study. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | participants (Number) |
|---|---|
| Placebo | 168 |
| Dutasteride 0.5 mg | 127 |
Testosterone, a male sex hormone, was measured by taking blood samples at screening and yearly thereafter. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | percent change (Mean) |
|---|---|
| Placebo | -0.1 |
| Dutasteride 0.5 mg | 20.0 |
The average number of prostate biopsy samples (cores) determined to be cancerous by the pathologist was measured. Normally, 10 cores were taken per biopsy for each participant. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | number of cores (Mean) |
|---|---|
| Placebo | 1.9 |
| Dutasteride 0.5 mg | 1.8 |
The NIH CSPI is a 9-item questionnaire that measures chronic prostatitis symptoms. The total score ranges from 0 to 43. A higher score indicates greater negative impact of prostatitis. Participants completed the questionnaire at Baseline and at each 6-month visit. Participants whose language did not have a validated translation of the questionnaire did not participate. Estimates are based on the adjusted means from the general linear model: change from Baseline = Baseline Value and Cluster and Treatment. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | 0.94 |
| Dutasteride 0.5 mg | -0.37 |
The PASSFI is a 3-item questionnaire that measures sexual function. Responses range from 0 (big problem) to 4 (no problem), with a total score of 12. A higher score indicates fewer problems with sexual functioning. Participants completed the questionnaire at Baseline and then yearly . Participants whose language did not have a validated translation of the questionnaire did not participate. Estimates are based on the adjusted means from the general linear model: change from baseline = baseline value and cluster and treatment. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | -0.82 |
| Dutasteride 0.5 mg | -1.5 |
Participants reported events of macroscopic hematospermia (visible blood in semen) throughout the study. (NCT00056407)
Timeframe: Baseline through Year 4
| Intervention | participants (Number) |
|---|---|
| Placebo | 78 |
| Dutasteride 0.5 mg | 53 |
The number of participants who received treatment for prostate cancer was measured. Prostate cancer interventions included surgical interventions (e.g., prostatectomy, adenomectomy, transurethral resection) and non-surgical interventions (e.g., chemotherapy, hormone therapy, radiation therapy). (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | participants (Number) | ||
|---|---|---|---|
| Any intervention | Any surgical intervention | Any non-surgical intervention | |
| Dutasteride 0.5 mg | 300 | 221 | 95 |
| Placebo | 438 | 304 | 172 |
The MOS Sleep-6S is a 6-item questionnaire measuring quality of sleep. Scores range from 1 (all of the time) to 6 (none of the time) and are converted to a 1-100 scale and then averaged; a higher score indicates greater negative impact, which indicates more sleep disturbance. Participants completed the questionnaire at Baseline and at each 6-month visit. Participants whose language did not have a validated translation of the questionnaire did not participate. Estimates are based on the adjusted means from the general linear model: change from baseline=baseline value and cluster and treatment. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | -0.03 |
| Dutasteride 0.5 mg | 0.02 |
The IPSS is a 7-item questionnaire that measures urinary symptoms. It measures the level of urinary symptoms (including incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia) reported as the total IPSS score. Each of the 7 questions has a 6-point response scale (0=none/not at all to 5=almost always) with a total score that can range from 0-35: mild (0-7), moderate (8-19), or severe (20-35). Estimates are based on adjusted means from the general linear model: change from baseline = baseline value and cluster and treatment. (NCT00056407)
Timeframe: Baseline to Year 4 (Month 48)
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | 1.35 |
| Dutasteride 0.5 mg | -0.46 |
The BII is a 4-item questionnaire that rates the level of BPH-related physical discomfort, worry, and interference with normal activities the participant has experienced. The total BII score ranges from 1 (no impact on symptoms) to 13 (major impact on symptoms). Participants completed the questionnaire at Baseline and at each 6-month visit. Participants whose language did not have a validated translation of the questionnaire did not participate. Estimates are based on the adjusted means from the general linear model:change from baseline = baseline value and cluster and treatment. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | 0.44 |
| Dutasteride 0.5 mg | -0.21 |
The QOL Q8 is the last question of the IPSS Questionnaire. It is a question about the participant's quality of life as it relates to prostate symptoms. Responses range from 0 (most positive) to 6 (most negative). A higher score indicates worse quality of life. Participants completed the questionnaire at Screening, Baseline, and at each 6-month visit. Estimates are based on the adjusted means from the general linear model: change from baseline = baseline value and cluster and treatment. (NCT00056407)
Timeframe: Baseline and Month 48
| Intervention | points on a scale (Mean) |
|---|---|
| Placebo | -0.06 |
| Dutasteride 0.5 mg | -0.33 |
A participant was considered to have AUR when he reported being unable to urinate and required catherization. Participants were asked to report any events of AUR during the study. (NCT00056407)
Timeframe: Years 1-2 and Overall (Years 1-4)
| Intervention | participants (Number) | |
|---|---|---|
| Years 1-2 | Overall | |
| Dutasteride 0.5 mg | 39 | 63 |
| Placebo | 150 | 272 |
A participant was considered to have a UTI if the investigator noted that the participant had UTI symptoms and had been prescribed antibiotics. Participants were asked to report any events of UTI during the study. (NCT00056407)
Timeframe: Years 1-2, Years 3-4, and Overall (Years 1-4)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Years 1-2, n=4073, 4049 | Years 3-4, n=3363, 3318 | Overall, n=4073, 4049 | |
| Dutasteride 0.5 mg | 131 | 83 | 214 |
| Placebo | 196 | 164 | 360 |
Study biopsies consisted of 10 biopsy samples (cores) in a pre-defined pattern. Biopsies were read at the central pathology laboratory (CPL, which processed the majority, 94%, of biopsies). Biopsy cases that were positive for prostate cancer or precancerous lesions (high-grade prostatic intraepithelial neoplasia[HGPIN] or typical small acinar proliferation [ASAP]) and prostate surgeries were reviewed by the lead pathologist. (NCT00056407)
Timeframe: Years 1-2, Years 3-4, and Overall (Years 1-4)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Years 1- 2, n=4073, 4049 | Years 3- 4, n=2815, 2844 | Overall, n=4073, 4049 | |
| Dutasteride 0.5 mg | 435 | 224 | 659 |
| Placebo | 578 | 280 | 858 |
Study biopsies (biop.) consisted of 10 biop. samples (cores) in a pre-defined pattern and were read at the central pathology laboratory. Biop. cases that were positive for prostate cancer or precancerous lesions (HGPIN or ASAP) and prostate surgeries were reviewed by the lead pathologist. Participants included in the risk sets at Years 1-2 and Years 3-4 included those with a positive biop. at Years 1-2 or a biop. after Months 18-24, and those with a positive biop. at Years 3-4 or a biop. after Month 42, respectively. Overall included participants with a positive biop. or biop. after Month 42. (NCT00056407)
Timeframe: Years 1-2, Years 3-4, and Overall (Years 1-4)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Years 1-2, n=3319, 3209 | Years 3-4, n=2325, 2434 | Overall, n=2903, 2869 | |
| Dutasteride 0.5 mg | 435 | 224 | 659 |
| Placebo | 578 | 280 | 858 |
Study biopsies consisted of 10 biopsy samples (cores) in a pre-defined pattern. Biopsies were read at the central pathology laboratory (which processed the majority, 94%, of biopsies). Biopsy cases that were positive for prostate cancer or precancerous lesions (HGPIN or ASAP) and prostate surgeries were reviewed by the lead pathologist. Participants included in the risk set at Years 1-2, Years 3-4, and Overall (Years 1-4) were those who had a biopsy during the specified time period. (NCT00056407)
Timeframe: Years 1-2, Years 3-4, and Overall (Years 1-4)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Years 1-2, n=3364, 3244 | Years 3- 4, n=2359, 2451 | Overall, n=3424, 3305 | |
| Dutasteride 0.5 mg | 435 | 224 | 659 |
| Placebo | 578 | 280 | 858 |
Gleason score was determined by examining prostate biopsies and surgical samples. The Gleason scoring system sums the two most common Gleason grade patterns in order to predict the likelihood of a participant doing well or badly with their cancer. Gleason grades range from 1 (normal) to 5 (advanced cancer). The lowest Gleason score is 2 (1+1), and the highest Gleason score is 10 (5+5). A Gleason score of 2-6 is a low-grade cancer; a Gleason score of 7-10 is high-grade cancer. The most severe high-grade cancers are the subset of Gleason scores 8-10. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | participants (Number) | ||
|---|---|---|---|
| Between 2 and 6 | Between 7 and 10 | Between 8 and 10 | |
| Dutasteride 0.5 mg | 437 | 220 | 29 |
| Placebo | 617 | 233 | 19 |
Number of participants whose DHT, the active form of the male sex hormone testosterone, was less than 0.555 nanomoles/liter and below the level of detection at Month 48 was measured. It was measured by taking blood samples at screening and yearly thereafter. (NCT00056407)
Timeframe: Month 48
| Intervention | participants (Number) | |
|---|---|---|
| <0.555 nanomoles/Liter | ||
| Dutasteride 0.5 mg | 3414 | 2210 |
| Placebo | 493 | 42 |
Overall survival is assessed as the number of deaths reported throughout the study. (NCT00056407)
Timeframe: From time informed consent is signed to 4-month Safety Follow-Up period
| Intervention | number of deaths (Number) | |
|---|---|---|
| Years 1-2 | Overall | |
| Dutasteride 0.5 mg | 32 | 70 |
| Placebo | 29 | 77 |
The treatment alteration score is a measure of the cellular changes due to treatment (effect of male hormone withdrawal) on the nucleus and cytoplasm of the prostate cancer cell. The treatment alteration score is the sum of two scores (the nuclear alteration score and the cytoplasmic architectural score), each ranging from 0 to 3, with 0 indicating no change and 3 indicating severe changes. (NCT00056407)
Timeframe: Baseline to Year 4
| Intervention | points on a scale (Mean) | ||
|---|---|---|---|
| Nuclear, n=3357, 3256 | Architectural, n=3357, 3258 | Total, n=3357, 3256 | |
| Dutasteride 0.5 mg | 0.019 | 0.023 | 0.041 |
| Placebo | 0.008 | 0.009 | 0.017 |
Prostate volume measurements were conducted annually using Transurethral ultrasound (TRUS). The anteroposterior, cephalocaudal, and transverse diameters of the prostate obtained by TRUS calculate the total prostate volume centimeters (cc). Percent change from baseline = [(post-baseline - baseline)/baseline value] x 100. Estimates were based on the adjusted (least squares) means from the general linear model: log(post-baseline/baseline value) + treatment + cluster + log(baseline value) and are reported as percent change from baseline. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12, n=1411, 1442, 1451 | Month 24, n= 1427, 1451, 1465 | Month 36, n= 1430, 1455, 1468 | Month 48, n= 1430, 1455, 1468 | |
| Dutasteride 0.5 mg | -25.2 | -28.0 | -28.8 | -28.0 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -24.1 | -26.9 | -27.6 | -27.3 |
| Tamsulosin 0.4 mg | -1.5 | 0.0 | 1.6 | 4.6 |
A participant was considered to have AUR when he was unable to urinate and required bladder catheterization. BPH is also known as an enlarged prostate. When symptoms of BPH become bothersome, surgery may be required. When events of AUR and BPH-related surgery were participant-reported or identified, they were recorded in the participants' clinic record. (NCT00090103)
Timeframe: Years 1, 2, 3, and 4
| Intervention | events (Number) | |||
|---|---|---|---|---|
| Year 1, n=1610, 1623, 1611 | Year 2, n=1457, 1484, 1464 | Year 3, n=1347, 1365, 1307 | Year 4, n=1274, 1277, 1176 | |
| Dutasteride 0.5 mg | 27 | 22 | 16 | 19 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 29 | 14 | 15 | 9 |
| Tamsulosin 0.4 mg | 40 | 62 | 44 | 45 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with BPH-related surgery. Responses to the following question were recorded: Would the participant have paid a visit to his general practitioner (GP)/Urologist regarding BPH-related surgery since the last study visit?. If the answer to the question was yes, the number of Yes responses was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | yes responses (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1564 | Month 6, n=1479, 1516, 1513 | Month 9, n=1438, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1380 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1166 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1034 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 34 | 23 | 10 | 10 | 9 | 12 | 9 | 7 | 9 | 9 | 7 | 5 | 8 | 8 | 8 | 3 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 16 | 20 | 12 | 5 | 9 | 13 | 10 | 4 | 9 | 7 | 5 | 3 | 7 | 9 | 6 | 1 |
| Tamsulosin 0.4 mg | 28 | 16 | 17 | 6 | 9 | 10 | 8 | 3 | 5 | 4 | 8 | 2 | 5 | 2 | 5 | 1 |
The time when the first symptom/event of BPH clinical progression has occurred (i.e. AUR, incontinence) was measured. Summaries are based on the first occuring event after treatment start. The time period is from treatment start to each participant's last treatment visit. The Year 4 events include all those that occur during the fourth year and beyond. (NCT00090103)
Timeframe: Years 1, 2, 3, and 4
| Intervention | events (Number) | |||
|---|---|---|---|---|
| Year 1, n=1610, 1623, 1611 | Year 2, n= 1264, 1240, 1262 | Year 3, n=1135, 1082, 1048 | Year 4, n= 1047, 959, 880 | |
| Dutasteride 0.5 mg | 184 | 54 | 29 | 22 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 126 | 31 | 30 | 16 |
| Tamsulosin 0.4 mg | 171 | 78 | 67 | 31 |
The number of participants (par.) with symptom deterioration of International Prostate Symptom Score (IPSS) ≥4 points on two consecutive visits post-baseline are presented. Data are based on the first occurrence of an event after treatment start. The year-4 events include all that occured during the 4th year and beyond. The IPSS is a 7-item questionnaire measuring the level of urinary symptoms reported as the total score. Each question has a 6-point response scale (0=none/not at all to 5=almost always), with a total score ranging from 0-35: mild (0-7), moderate (8-19), or severe (20-35). (NCT00090103)
Timeframe: Years 1, 2, 3, and 4 (from treatment start until each participant's last treatment-phase visit)
| Intervention | events (Number) | |||
|---|---|---|---|---|
| Year 1, n=1610, 1623, 1611 | Year 2, n=1286, 1278, 1296 | Year 3, n=1158, 1132, 1088 | Year 4, n=1083, 1001, 926 | |
| Dutasteride 0.5 mg | 138 | 38 | 23 | 13 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 91 | 23 | 14 | 11 |
| Tamsulosin 0.4 mg | 119 | 49 | 42 | 19 |
A participant was considered to have hematospermia when there was presence of blood in the semen. Hematospermia can occur from prostatitis (prostate infection), from cancer, or after a prostate biopsy. The event of hematospermia was either participant-reported or identified by the investigator during a clinic visit. Overall Crude Rate is the number of participants from the total number analyzed that experience experienced an incident of post-baseline BPH or Non-BPH related hematospermia. Participants may appear in both categories. (NCT00090103)
Timeframe: Baseline (Day 1) through Year 4
| Intervention | participants (Number) | ||
|---|---|---|---|
| Overall Crude Rate | Non-BPH-related Crude Rate | BPH-related Crude Rate | |
| Dutasteride 0.5 mg | 19 | 3 | 17 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 18 | 2 | 17 |
| Tamsulosin 0.4 mg | 20 | 9 | 11 |
A participant was considered to have macroscopic hematuria when there was presence of blood in the urine. The event of macroscopic hematuria was either participant-reported or identified by the investigator during a clinic visit. Overall Crude Rate is the number of participants from the total number analyzed that experience experienced an incident of post-baseline BPH or Non-BPH related macroscopic hematuria. Participants may appear in both categories. (NCT00090103)
Timeframe: Baseline (Day 1) through Year 4
| Intervention | participants (Number) | ||
|---|---|---|---|
| Overall crude rate | Non-BPH-related Crude Rate | BPH-Related Crude Rate | |
| Dutasteride 0.5 mg | 70 | 28 | 45 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 53 | 15 | 40 |
| Tamsulosin 0.4 mg | 81 | 25 | 56 |
A participant was considered to have AUR when he was unable to urinate and required bladder catheterization. BPH is also known as an enlarged prostate. When symptoms of BPH become bothersome, surgery may be required. When events of AUR and BPH-related surgery were participant reported or identified, they were recorded in the participants' clinic record. (NCT00090103)
Timeframe: Baseline (Day 1) through Year 4
| Intervention | participants (Number) | |
|---|---|---|
| AUR | BPH-related surgery | |
| Dutasteride 0.5 mg | 44 | 40 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 35 | 32 |
| Tamsulosin 0.4 mg | 109 | 82 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with unplanned visits to GP/Urologist. Responses to the following question were recorded: Has the participant had any unplanned GP/Urologist (outpatient) visits that would have taken place if a scheduled study visit had not been planned (this can include visits resulting from UTI, UI macroscopic haematuria, etc?. If the answer to the question was yes, the number of visits was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | visits (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1564 | Month 6, n=1479, 1517, 1514 | Month 9, n=1439, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1380 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1166 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1035 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 25 | 34 | 35 | 29 | 22 | 25 | 21 | 19 | 11 | 8 | 5 | 4 | 13 | 8 | 5 | 6 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 23 | 23 | 16 | 30 | 24 | 21 | 18 | 10 | 15 | 7 | 4 | 5 | 6 | 4 | 3 | 1 |
| Tamsulosin 0.4 mg | 26 | 22 | 22 | 34 | 27 | 26 | 14 | 21 | 14 | 10 | 10 | 7 | 19 | 12 | 6 | 5 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with unplanned visits to GP/Urologist. Responses to the following question were recorded: Does the participant have any unscheduled GP/Urologist (outpatients) visits planned, not relating to the study (this can include visits resulting from UTI, UI, macroscopic haematuria, etc.?. If the answer to the question was yes, the number of visits was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | visits (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1564 | Month 6, n=1479, 1516, 1514 | Month 9, n=1439, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1381 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1166 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1035 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 27 | 29 | 27 | 28 | 28 | 21 | 27 | 23 | 12 | 16 | 13 | 12 | 10 | 9 | 7 | 4 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 27 | 23 | 12 | 30 | 19 | 23 | 20 | 29 | 13 | 10 | 6 | 8 | 12 | 15 | 5 | 7 |
| Tamsulosin 0.4 mg | 30 | 33 | 26 | 29 | 32 | 34 | 26 | 26 | 16 | 10 | 20 | 18 | 18 | 15 | 8 | 8 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with an episode of AUR. Responses to the following question were recorded: Has the participant needed to make any unscheduled visits to his general practitioner (GP)/Urologist regarding AUR symptoms since the last study visit? If the answer to the question was yes, the number of visits was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | visits (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1565 | Month 6, n=1479, 1517, 1514 | Month 9, n=1439, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1380 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1166 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1035 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 6 | 4 | 3 | 3 | 6 | 4 | 3 | 2 | 6 | 2 | 4 | 1 | 2 | 2 | 2 | 2 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 8 | 2 | 4 | 3 | 3 | 3 | 3 | 2 | 1 | 3 | 3 | 2 | 2 | 3 | 1 | 1 |
| Tamsulosin 0.4 mg | 7 | 3 | 8 | 9 | 6 | 10 | 9 | 7 | 7 | 8 | 5 | 5 | 5 | 8 | 4 | 2 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with BPH-related surgery. Responses to the following question were recorded: Has the participant needed to visit his general practitioner (GP)/Urologist regarding BPH-related surgery since the last study visit?. If the answer to the question was yes, the number of visits was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | visits (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1564 | Month 6, n=1479, 1517, 1514 | Month 9, n=1439, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1380 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1165 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1035 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 3 | 1 | 2 | 2 | 5 | 0 | 0 | 0 | 3 | 1 | 1 | 2 | 3 | 2 | 3 | 2 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 0 | 2 | 2 | 1 | 2 | 4 | 1 | 2 | 3 | 0 | 0 | 2 | 1 | 1 | 0 | 0 |
| Tamsulosin 0.4 mg | 3 | 2 | 3 | 7 | 7 | 4 | 3 | 3 | 4 | 1 | 5 | 1 | 2 | 5 | 2 | 1 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Since you began taking the study medication, how has control of your urinary problems changed?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Improvement, n=1585, 1600, 1586 | BL, No Change/Any Worsening, n=1585, 1600, 1586 | Month (M) 12, Any Improvement, n=1576, 1593, 1581 | M12, No Change/Any Worsening, n=1576, 1593, 1581 | M24, Any Improvement, n=1576, 1593, 1581 | M24, No Change/Any Worsening, n=1576, 1593, 1581 | M36, Any Improvement, n=1576, 1593, 1581 | M36, No Change/Any Worsening, n=1576, 1593, 1581 | M48, Any Improvement, n=1576, 1593, 1581 | M48, No Change/Any Worsening, n=1576, 1593, 1581 | |
| Dutasteride 0.5 mg | 656 | 944 | 1171 | 422 | 1200 | 393 | 1203 | 390 | 1212 | 381 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 696 | 889 | 1281 | 295 | 1273 | 303 | 1268 | 308 | 1278 | 298 |
| Tamsulosin 0.4 mg | 706 | 880 | 1218 | 363 | 1195 | 386 | 1152 | 429 | 1138 | 443 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Overall, how satisfied are you with the study medication and it's effect on your urinary problems?. Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=1573, 1598, 1574 | BL, Neutral/Any Dissatisfact., n=1573, 1598, 1574 | Month (M) 12, Any Satisfact., n=1574, 1592, 1581 | M12, Neutral/Any Dissatisfact., n=1574, 1592, 1581 | M24, Any Satisfact., n=1574, 1592, 1581 | M24, Neutral/Any Dissatisfact., n=1574, 1592, 1581 | M36, Any Satisfact., n=1574, 1592, 1581 | M36, Neutral/Any Dissatisfact., n=1574, 1592, 1581 | M48, Any Satifact., n=1574, 1592, 1581 | M48, Neutral/Any Dissatisfact., n=1574, 1592, 1581 | |
| Dutasteride 0.5 mg | 683 | 915 | 1159 | 433 | 1188 | 404 | 1188 | 404 | 1182 | 410 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 717 | 856 | 150 | 324 | 1279 | 295 | 1270 | 304 | 1262 | 312 |
| Tamsulosin 0.4 mg | 699 | 875 | 1202 | 379 | 1163 | 418 | 1119 | 462 | 1097 | 484 |
"At each scheduled 13-week clinic visit post-randomization, the investigator was to record details of any health care utilization associated with an episode of AUR. Responses to the following question were recorded: Would the participant have paid a visit to his GP/Urologist regarding AUR symptoms if this study visit had not been planned?. If the answer to the question was yes, the number of Yes responses was recorded." (NCT00090103)
Timeframe: Every 3 months from Month 3 to Month 48
| Intervention | yes responses (Number) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3, n=1550, 1581, 1564 | Month 6, n=1479, 1516, 1513 | Month 9, n=1439, 1465, 1477 | Month 12, n=1400, 1431, 1434 | Month 15, n=1343, 1386, 1380 | Month 18, n=1318, 1350, 1328 | Month 21, n=1281, 1326, 1287 | Month 24, n=1263, 1293, 1244 | Month 27, n=1233, 1262, 1206 | Month 30, n=1222, 1221, 1166 | Month 33, n=1202, 1199, 1128 | Month 36, n=1187, 1174, 1095 | Month 39, n=1160, 1144, 1055 | Month 42, n=1149, 1126, 1035 | Month 45, n=1129, 1110, 1009 | Month 48, n=1113, 1093, 990 | |
| Dutasteride 0.5 mg | 32 | 26 | 14 | 13 | 15 | 13 | 15 | 9 | 11 | 9 | 10 | 4 | 9 | 8 | 8 | 9 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 31 | 21 | 18 | 8 | 9 | 17 | 10 | 5 | 9 | 7 | 9 | 5 | 7 | 6 | 7 | 2 |
| Tamsulosin 0.4 mg | 29 | 26 | 18 | 9 | 12 | 19 | 17 | 8 | 8 | 9 | 11 | 5 | 6 | 8 | 5 | 5 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Since you began taking the study medication, how has your pain during urination changed?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Improvement, n=852, 889, 822 | BL, No Change/Any Worsening, n=852, 889, 822 | Month (M) 12, Any Improvement, n=760, 781, 755 | M12, No Change/Any Worsening, n=760, 781, 755 | M24, Any Improvement, n=706, 760, 747 | M24, No Change/Any Worsening, n=706, 760, 747 | M36, Any Improvement, n=704, 741, 733 | M36, No Change/Any Worsening, n=704, 741, 733 | M48, No Change/Any Worsening, n=702, 739, 740 | M48, Any Improvement, n=702, 739, 740 | |
| Dutasteride 0.5 mg | 314 | 575 | 500 | 281 | 508 | 252 | 504 | 237 | 252 | 487 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 321 | 531 | 550 | 210 | 532 | 174 | 529 | 175 | 175 | 527 |
| Tamsulosin 0.4 mg | 319 | 503 | 529 | 226 | 519 | 228 | 491 | 242 | 257 | 483 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of How satisfied are you with the effect the study medication has on your pain prior to urinating?. Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=908, 932, 889 | BL, Neutral/Any Dissatisfact., n=908, 932, 889 | Month (M) 12, Any Satisfact., n=1022, 1088, 1019 | M12, Neutral/Any Dissatisfact., n=1022, 1088, 1019 | M24, Any Satisfact., n=1077, 1151, 1085 | M24, Neutral/Any Dissatisfact., n=1077, 1151, 1085 | M36, Any Satisfact., n=1115, 1200, 1135 | M36, Neutral/Any Dissatisfact., n=1115, 1200, 1135 | M48, Any Satisfact., n=1135, 1223, 1161 | M48, Neutral/Any Dissatisfact., n=1135, 1223, 1161 | |
| Dutasteride 0.5 mg | 351 | 581 | 672 | 416 | 740 | 411 | 785 | 415 | 792 | 431 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 375 | 533 | 712 | 310 | 764 | 313 | 799 | 316 | 810 | 325 |
| Tamsulosin 0.4 mg | 351 | 538 | 681 | 338 | 708 | 377 | 736 | 399 | 739 | 422 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Since you began taking the study medication, how has your pain prior to urinating changed?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Improvement, n=869, 901, 849 | BL, No Change/Any Worsening, n=869, 901, 849 | Month (M) 12, Any Improvement, n=769, 817, 771 | M12, No Change/Any Worsening, n=769, 817, 771 | M24, Any Improvement, n=720, 780, 771 | M24, No Change/Any Worsening, n=720, 780, 771 | M36, Any Improvement, n=714, 753, 748 | M36, No Change/Any Worsening, n=714, 753, 748 | M48, Any Improvement, n=709, 756, 751 | M48, No Change/Any Worsening, n=709, 756, 751 | |
| Dutasteride 0.5 mg | 331 | 570 | 526 | 291 | 526 | 254 | 514 | 239 | 510 | 246 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 337 | 532 | 556 | 213 | 537 | 183 | 540 | 174 | 531 | 178 |
| Tamsulosin 0.4 mg | 332 | 517 | 527 | 244 | 535 | 236 | 496 | 252 | 489 | 262 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of How satisfied are you with the effect of the study medication on the strength of your urinary stream?. Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=1583,1601,1582 | BL, Neutral/Any Dissatisfact., n=1583,1601,1582 | Month (M) 12, Any Satisfact., n=1576, 1593, 1581 | M12, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M24, Any Satisfact., n=1576, 1593, 1581 | M24, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M36, Any Satisfact., n=1576, 1593, 1581 | M36, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M48, Any Satisfact., n=1576, 1593, 1581 | M48, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | |
| Dutasteride 0.5 mg | 586 | 1015 | 1037 | 556 | 1072 | 521 | 1075 | 518 | 1089 | 504 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 632 | 951 | 1154 | 422 | 1203 | 373 | 1201 | 375 | 1208 | 368 |
| Tamsulosin 0.4 mg | 613 | 969 | 1097 | 484 | 1051 | 530 | 1039 | 542 | 1022 | 559 |
The five components measured were symptom deterioration, BPH-related AUR, BPH-related incontinence, recurrent BPH-related Urinary Tract Infection (UTI), and BPH-related renal insufficiency. (NCT00090103)
Timeframe: Baseline (Day 1) to Year 4
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Symptom deterioration | BPH-related AUR | BPH-related incontinence | Recurrent BPH-related UTI | BPH-related renal insufficiency | |
| Dutasteride 0.5 mg | 203 | 31 | 49 | 5 | 2 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 132 | 22 | 46 | 2 | 1 |
| Tamsulosin 0.4 mg | 221 | 64 | 56 | 3 | 5 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Since you began taking the study medication, how has the way your urinary problems interfere with your ability to go about your usual activities changed?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Improvement, n=1574, 1599, 1575 | BL, No Change/Any Worsening, n=1574, 1599, 1575 | Month (M) 12, Any Improvement, n=1575, 1593, 1580 | M12, No Change/Any Worsening, n=1575, 1593, 1580 | M24, Any Improvement, n=1575, 1593, 1580 | M24, No Change/Any Worsening, n=1575, 1593, 1580 | M36, Any Improvement, n=1575, 1593, 1580 | M36, No Change/Any Worsening, n=1575, 1593, 1580 | M48, Any Improvement, n=1575, 1593, 1580 | M48, No Change/Any Worsening, n=1575, 1593, 1580 | |
| Dutasteride 0.5 mg | 481 | 1118 | 1027 | 566 | 1053 | 540 | 1593 | 529 | 1063 | 530 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 509 | 1065 | 1124 | 451 | 1146 | 429 | 1575 | 412 | 1148 | 427 |
| Tamsulosin 0.4 mg | 494 | 1081 | 1084 | 496 | 1049 | 531 | 1580 | 553 | 1008 | 572 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of How satisfied are you with the effect the study medication has on your pain during urination?. Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=890, 925, 851 | BL, Neutral/Any Dissatisfact., n=890, 925, 851 | Month (M) 12, Any Satisfact., n=1022, 1088, 1011 | M12, Neutral/Any Dissatisfact., n=1022, 1088, 1011 | M24, Any Satisfact., n=1077, 1155, 1079 | M24, Neutral/Any Dissatisfact., n=1077, 1155, 1079 | M36, Any Satisfact., n=1121, 1206, 1131 | M36, Neutral/Any Dissatisfact., n=1121, 1206, 1131 | M48, Any Satsifact., n=1146,1224,1160 | M48, Neutral/Any Dissatisfact., n=1146, 1224, 1160 | |
| Dutasteride 0.5 mg | 348 | 577 | 655 | 433 | 730 | 425 | 784 | 422 | 785 | 439 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 354 | 536 | 712 | 310 | 763 | 314 | 807 | 314 | 827 | 319 |
| Tamsulosin 0.4 mg | 333 | 518 | 678 | 333 | 708 | 371 | 724 | 407 | 729 | 431 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Since you began taking the study medication, how has the strength of your urinary stream changed?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Improvement, n=1585, 1601, 1585 | BL, No Change/Any Worsening, n=1585, 1601, 1585 | Month (M) 12, Any Improvement, n=1576, 1593, 158 | M12, No Change/Any Worsening, n=1576, 1593, 1581 | M24, Any Improvement, n=1576, 1593, 1581 | M24, No Change/Any Worsening, n=1576, 1593, 1581 | M36, Any Improvement, n=1576, 1593, 1581 | M36, No Change/Any Worsening, n=1576, 1593, 1581 | M48, Any Improvement, n=1576, 1593, 1581 | M48, No Change/Any Worsening, n=1576, 1593, 1581 | |
| Dutasteride 0.5 mg | 602 | 999 | 1044 | 549 | 1070 | 523 | 1071 | 522 | 1086 | 507 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 629 | 956 | 1181 | 395 | 1215 | 361 | 1206 | 370 | 1202 | 374 |
| Tamsulosin 0.4 mg | 615 | 970 | 1105 | 476 | 1057 | 524 | 1023 | 558 | 1008 | 573 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of How satisfied are you with the effect of the study medication on control of your urinary problems? Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=1587, 1600, 1583 | BL, Neutral/Any Dissatisfact., n=1587, 1600, 1583 | Month (M) 12, Any Satisfact., n=1576, 1593, 1581 | M12, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M24, Any Satisfact., n=1576, 1593, 1581 | M24, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M36, Any Satisfact., n=1576, 1593, 1581 | M36, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | M48, Any Satisfact., n=1576, 1593, 1581 | M48, Neutral/Any Dissatisfact., n=1576, 1593, 1581 | |
| Dutasteride 0.5 mg | 652 | 948 | 1127 | 466 | 1166 | 427 | 1167 | 426 | 1172 | 421 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 707 | 880 | 1224 | 352 | 1261 | 315 | 1260 | 316 | 1267 | 309 |
| Tamsulosin 0.4 mg | 686 | 897 | 1178 | 403 | 1150 | 431 | 1120 | 461 | 1088 | 493 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of How satisfied are you with the effect the study medication has on your ability to go about your usual activities without interference from your urinary problems?. Satisfact., satisfaction." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline (BL), Any Satisfact., n=1574, 1600, 1576 | BL, Neutral /Any Dissatisfact., n=1574, 1600, 1576 | Month (M) 12, Any Satisfact., n=1575, 1593, 1580 | M12, Neutral/Any Dissatisfact., n=1575, 1593, 1580 | M24, Any Satisfact., n=1575, 1593, 1580 | M24, Neutral/Any Dissatisfact., n=1575, 1593, 1580 | M36, Any Satisfact., n=1575, 1593, 1580 | M36, Neutral/Any Dissatisfact., n=1575, 1593, 1580 | M48, Any Satisfact., n=1575, 1593, 1580 | M48, Neutral/Any Dissatisfact., n=1575, 1593, 1580 | |
| Dutasteride 0.5 mg | 565 | 1035 | 1073 | 520 | 1116 | 477 | 1098 | 495 | 1123 | 470 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 611 | 963 | 1176 | 399 | 1205 | 370 | 1210 | 365 | 1213 | 362 |
| Tamsulosin 0.4 mg | 584 | 992 | 1114 | 466 | 1088 | 492 | 1074 | 506 | 1043 | 537 |
"This 12-item questionnaire (PPSM) was developed by GlaxoSmithKline for use in this study and was designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms at baseline and Months 3, 6, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36, 39, 42, 45, and 48. Participants were asked to respond to the question of Would you ask your doctor for the medication you received in this study?." (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Baseline, Yes, n=1560, 1579, 1562 | Baseline, No/Not Sure, n=1560, 1579, 1562 | Month 12, Yes, n=1574, 1592, 1581 | Month 12, No/Not Sure, n=1574, 1592, 1581 | Month 24, Yes, n=1574, 1592, 1581 | Month 24, No/Not Sure, n=1574, 1592, 1581 | Month 36, Yes, n=1574, 1592, 1581 | Month 36, No/Not Sure, n=1574, 1592, 1581 | Month 48, Yes, n=1574, 1592, 1581 | Month 48, No/Not Sure, n=1574, 1592, 1581 | |
| Dutasteride 0.5 mg | 557 | 1022 | 920 | 671 | 955 | 636 | 956 | 636 | 918 | 674 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 587 | 973 | 972 | 602 | 1027 | 547 | 1031 | 543 | 1003 | 571 |
| Tamsulosin 0.4 mg | 582 | 980 | 970 | 611 | 952 | 629 | 915 | 666 | 874 | 707 |
The BII is a 4-item questionnaire, score range of 0 (best) to 12 (worst) for questions 1-3, and 0 (best) to 13 (worst) for question 4, that assesses the overall impact of BPH on a participant's general sense of well being and measures aspects of physical discomfort, worry, and bother, all of which can be affected by BPH and its symptoms. BII score = sum of questions 1-4. Change from baseline = Post-Baseline Value. Estimates are based on the adjusted (least squares) means from the general linear model: change from baseline BII = treatment + cluster + baseline BII. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | points on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12 | Month 24 | Month 36 | Month 48 | |
| Dutasteride 0.5 mg | -1.5 | -1.7 | -1.8 | -1.8 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -1.9 | -2.1 | -2.2 | -2.2 |
| Tamsulosin 0.4 mg | -1.6 | -1.5 | -1.3 | -1.2 |
The effect of study treatment on BHS was assessed by using three self-administered questionnaires: the International Prostate Symptom Score (IPSS), the BPH Impact Index (BII), and Patient Perception of Study Medication (PPSM). The BHS score was collected on the IPPS questionnaire and ranged from 0 (best) to 6 (worst). Percent change from baseline = [(post-baseline - baseline)/baseline value] x 100. Estimates were based on the adjusted (least squares) means from the general linear model: change from baseline BPH-related health status = treatment + cluster + baseline BPH-Related health status. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, 48
| Intervention | points on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12 | Month 24 | Month 36 | Month 48 | |
| Dutasteride 0.5 mg | -1.0 | -1.1 | -1.2 | -1.3 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -1.2 | -1.4 | -1.5 | -1.5 |
| Tamsulosin 0.4 mg | -1.0 | -1.1 | -1.1 | -1.1 |
The IPSS is a 7-item questionnaire that measures urinary symptoms. It measures the level of urinary symptoms (including incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia) reported as the total IPSS score. Each of the 7 questions has a 6-point response scale (0=none/not at all to 5=almost always) with a total score that can range from 0-35: mild (0-7), moderate (8-19), or severe (20-35). Estimates are based on adjusted (least squares) means from the general linear model: change from baseline IPSS = Treatment + Cluster + Baseline IPSS. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | points on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12 | Month 24 | Month 36 | Month 48 | |
| Dutasteride 0.5 mg | -4.2 | -4.9 | -5.2 | -5.3 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -5.6 | -6.2 | -6.3 | -6.3 |
| Tamsulosin 0.4 mg | -4.5 | -4.3 | -4.0 | -3.8 |
Prostate volume (PV) measurements were conducted annually using Transurethral ultrasound (TRUS). The anteroposterior, cephalocaudal, and transverse diameters of the prostate obtained by TRUS calculate the total PV in centimeters (cc). Results are for the transition zone measurements of the prostate in a small subset of participants. Percent change from baseline (BL) = [(post-BL - BL)/BL value] x 100. Estimates are based on the adjusted (least squares) means for the general linear model: log(post-BL/BL value) = treatment + cluster + log(BL value) and are reported as percent change from BL. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | percent change (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12, n= 150, 159, 160 | Month 24, n= 153, 164, 160 | Month 36, n= 155, 164, 162 | Month 48, n= 155, 164, 163 | |
| Dutasteride 0.5 mg | -15.6 | -22.8 | -26.7 | -26.5 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -17.2 | -23.4 | -20.9 | -17.9 |
| Tamsulosin 0.4 mg | 5.6 | 8.7 | 14.7 | 18.2 |
Peak maximum urinary flow (Qmax) of urinary flow using a Medtronic (formerly Dantec) Uroflow Meter (Urodyn 1000 or Duet models) with a Thompson filter was measured. Estimates are based on adjusted (least squares) means from the general linear model: Change from baseline Qmax = treatment + cluster + baseline Qmax. (NCT00090103)
Timeframe: Baseline and Months 12, 24, 36, and 48
| Intervention | milliliters (mL)/second (sec) (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 12, n=1477, 1482, 1510 | Month 24, n= 1492, 1501, 1519 | Month 36, n= 1495, 1504, 1521 | Month 48, n= 1495, 1505, 1523 | |
| Dutasteride 0.5 mg | 1.5 | 1.9 | 1.9 | 2.0 |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 2.0 | 2.4 | 2.6 | 2.4 |
| Tamsulosin 0.4 mg | 0.9 | 0.9 | 0.6 | 0.7 |
(NCT00194675)
Timeframe: Baseline, Month 6
| Intervention | cubic centimeters (Mean) | |
|---|---|---|
| Baseline, Day 0 | Month 6 | |
| Testosterone Gel + Oral Dutasteride | 44.4 | 38.6 |
| Testosterone Gel + Oral Placebo | 54.2 | 58.3 |
(NCT00194675)
Timeframe: Baseline, Month 6
| Intervention | ng/ ml (Mean) | |
|---|---|---|
| Baseline PSA | Month 6 PSA | |
| Testosterone Gel + Oral Dutasteride | 2.1 | 1.4 |
| Testosterone Gel + Oral Placebo | 2.8 | 3.1 |
(NCT00194675)
Timeframe: Baseline, 3-months, 6-months
| Intervention | ng/ dL (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Total testosterone, baseline | Total testosterone, month 3 | Total testosterone, month 6 | Free testosterone, baseline | Free testosterone, month 3 | Free testosterone, month 6 | Dihydrotestosterone (DHT), baseline | Dihydrotestosterone (DHT), month 3 | Dihydrotestosterone (DHT), month 6 | Dehydroepiandrosterone (DHEA), baseline | Dehydroepiandrosterone (DHEA), month 3 | Dehydroepiandrosterone (DHEA), month 6 | Androstenedione, baseline | Androstenedione, month 3 | Androstenedione, month 6 | |
| Testosterone Gel + Oral Dutasteride | 213 | 525 | 534 | 4.5 | 12.0 | 12.3 | 28 | 16 | 12 | 99 | 109 | 111 | 47 | 140 | 123 |
| Testosterone Gel + Oral Placebo | 206 | 494 | 481 | 4.2 | 11.3 | 11.4 | 47 | 145 | 134 | 72 | 98 | 97 | 45 | 99 | 100 |
(NCT00194675)
Timeframe: Baseline, 3-months, 6-months
| Intervention | cc (Mean) | ||
|---|---|---|---|
| Baseline Post Residual Volume (PVR) | 3 month Post Residual Volume | 6 month Post Residual Volume | |
| Testosterone Gel + Oral Dutasteride | 48 | 41 | 32 |
| Testosterone Gel + Oral Placebo | 43 | 36 | 39 |
(NCT00194675)
Timeframe: Baseline, 3-months, 6-months
| Intervention | cc/sec (Mean) | ||
|---|---|---|---|
| Baseline Uroflow, Baseline | Uroflow after 3 months of treatment | Uroflow after 6 months of treatment | |
| Testosterone Gel + Oral Dutasteride | 13.4 | 13.2 | 14.6 |
| Testosterone Gel + Oral Placebo | 13.8 | 12.7 | 13.8 |
International Prostate Symptom Score to assess lower urinary tract symptoms (LUTS) due to benign prostatic hyperplasia (BPH). Minimum score = 0, maximum score = 35; mildly symptomatic score = 0-7; moderately symptomatic score = 8-19; severely symptomatic score = 20-35; no subscales. (NCT00194675)
Timeframe: Baseline, Month 3, Month 6
| Intervention | score (Mean) | ||
|---|---|---|---|
| Baseline IPSS | Month 3- IPSS | Month 6 IPSS | |
| Testosterone Gel + Oral Dutasteride | 13.3 | 10.2 | 10.3 |
| Testosterone Gel + Oral Placebo | 13.5 | 11.6 | 11.1 |
Tissue dihydrotesterone (DHT) (NCT00298155)
Timeframe: After 12 weeks of neoadjuvant androgen deprivation
| Intervention | ng/g (Mean) |
|---|---|
| Group 1 | 0.03 |
| Group 2 | 0.06 |
| Group 3 | 0.03 |
Serum DHT (NCT00298155)
Timeframe: After 12 weeks of neoadjuvant androgen deprivation
| Intervention | ng/dL (Mean) |
|---|---|
| Group 1 | 4.2 |
| Group 2 | 3.6 |
| Group 3 | 5.7 |
Subjects rated their daily activity with a modified 9-question Activities of Daily Living (ADL) questionnaire (0-4, fully impaired to normal). (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Activities of Daily Living, Change at 12 months | Activities of Daily Living, Change at 24 months | |
| Dutasteride | 0.4 | 1.1 |
| Placebo | 0.4 | 1.2 |
The Adult Myopathy Assessment Tool rates physical function and muscle endurance, with higher scores indicating better performance; it includes 7 timed functional tasks and 6 endurance tasks (0=worst, 45=best). (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Adult Myopathy Assessment Tool, Change at 12 mos. | Adult Myopathy Assessment Tool, Change at 24 mos. | |
| Dutasteride | -0.7 | -1.5 |
| Placebo | -2.2 | -2.8 |
Serum creatine kinase was determined in venous blood samples analyzed at the Department of Laboratory Medicine of the NIH Clinical Center. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | Units/liter (Mean) | |
|---|---|---|
| Creatine kinase change at 12 months | Creatine kinase change at 24 months | |
| Dutasteride | -32 | -62 |
| Placebo | -36 | -19 |
The subjects did the 2-minute walk in a 50-foot (15.2-meter) corridor three times, and the average distance was calculated. The subjects were allowed to use an assistive device and rest between the trials. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | meters (Mean) | |
|---|---|---|
| Timed 2-minute Walk, Change at 12 months | Timed 2-minute Walk, Change at 24 months | |
| Dutasteride | -0.8 | -1.6 |
| Placebo | 8.1 | 2.2 |
Sexual function was rated using the International Index of Erectile Function (IIEF). The total IIEF score (5-75, worst-best) was reported as the percent maximum (0-100%). (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | percent of maximum score (Mean) | |
|---|---|---|
| IIEF, Change at 12 months | IIEF, Change at 24 months | |
| Dutasteride | -2.1 | -3.5 |
| Placebo | -2.4 | -0.3 |
Manual muscle testing was performed using a modified Medical Research Council (MRC) scale (0=worst, 5=best); the average muscle score was based on 22 muscle groups. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | MRC units on a scale (Mean) | |
|---|---|---|
| Manual Muscle Testing, Change at 12 months | Manual Muscle Testing, Change at 24 months | |
| Dutasteride | -0.25 | 0.01 |
| Placebo | 0.04 | 0.02 |
Nerve conduction studies were done on the median motor nerve, and the compound muscle action potential amplitude was determined. Loss of amplitude indicates impairment of conduction. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | mVolts (Mean) | |
|---|---|---|
| Median Motor Action Potential, Change at 12 months | Median Motor Action Potential, Change at 24 months | |
| Dutasteride | 0.52 | 0.24 |
| Placebo | 0.04 | -0.24 |
Subjects completed the Medical Outcomes Study Short Form Version 2 (SF-36v2), in which they rated their mental quality of life over the preceding 4 weeks. Raw SF-36v2 scores were converted to norm-based scales and component summaries using the scoring code provided by QualityMetric (mean=50, standard deviation (SD)=10), and percent change in the norm-based scale was calculated. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | percent change (Mean) | |
|---|---|---|
| SF-36v2 Mental Component Sum., Change at 12 mos. | SF-36v2 Mental Component Sum., Change at 24 mos. | |
| Dutasteride | 0.1 | -3.2 |
| Placebo | 0.6 | 3.3 |
Subjects completed the Medical Outcomes Study Short Form Version 2 (SF-36v2), in which they rated their physical quality of life over the preceding 4 weeks. Raw SF-36v2 scores were converted to norm-based scales and component summaries using the scoring code provided by QualityMetric (mean=50, standard deviation (SD)=10). (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | percent change (Mean) | |
|---|---|---|
| SF-36v2 Physical Component Sum., Change at 12 mos. | SF-36v2 Physical Component Sum., Change at 24 mos. | |
| Dutasteride | 2.5 | 2.1 |
| Placebo | -0.9 | -3.6 |
Motor unit number estimation (MUNE) was done with a statistical MUNE program, on the abductor pollicis brevis. All subjects were evaluated on the right side unless severe atrophy produced very low compound muscle action potentials; in this case, the left side was investigated or the abductor digiti minimi was substituted. A decrease in MUNE indicates a loss of motor units. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | motor unit number (Mean) | |
|---|---|---|
| Motor Unit Nerve Estimation, Change at 12 months | Motor Unit Nerve Estimation, Change at 24 months | |
| Dutasteride | -4.2 | -2.6 |
| Placebo | -4.2 | -2.2 |
Quantitative muscle assessment (QMA) was done with a fixed frame dynamometer, a strain gauge tensiometer, and a computer-aided acquisition system. Maximal voluntary isometric muscle contractions were measured twice, the average was calculated, and the results were summed over 22 muscle groups (11 on each side). The total force was scaled for body weight and expressed as percent change from baseline. Measurements were performed at 0, 12, and 24 months. The calculated percent changes at 12 and 24 months are shown. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | percent change (Mean) | |
|---|---|---|
| Muscle Strength Change From Baseline at 12 Months | Muscle Strength Change From Baseline at 24 Months | |
| Dutasteride | 3.1 | 1.3 |
| Placebo | -2.2 | -4.5 |
The Bulbar Rating Scale includes eight domains each rated on a 1-4 scale, abnormal to normal. The original 8-32 point scale was transformed to a 0-100% scale to represent the responses as percentages. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | percentage of maximum score (Mean) | |
|---|---|---|
| Bulbar Rating Scale, Change at 12 months | Bulbar Rating Scale, Change at 24 months | |
| Dutasteride | 2.6 | 3.9 |
| Placebo | 5.7 | 6.4 |
Nerve conduction studies were done on four sensory nerves (median, ulnar, radial, sural), and the amplitudes of the evoked responses were averaged. Loss of amplitude indicates impairment of conduction. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | microVolts (Mean) | |
|---|---|---|
| Sensory Nerve Action Potential, Change at 12 mos. | Sensory Nerve Action Potential, Change at 24 mos. | |
| Dutasteride | 0 | 0 |
| Placebo | 0 | 0 |
Modified barium swallow studies were done at 0, 12, and 24 months. Twenty-five domains were assessed, and six were chosen for final analysis based on the abnormal findings in subjects evaluated at baseline: vallecular pooling and repeated-swallow, each assessed with thin liquids, purees, and solids (rated 1-4, abnormal to normal). (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Swallow Score Average, Change at 12 months | Swallow Score Average, Change at 24 months | |
| Dutasteride | 0.06 | -0.14 |
| Placebo | -0.25 | -0.53 |
Nerve conduction studies were done on the peroneal nerve, and the compound muscle action potential amplitude was determined. Loss of amplitude indicates impairment of conduction. (NCT00303446)
Timeframe: 0, 12, and 24 months
| Intervention | mVolts (Mean) | |
|---|---|---|
| Peroneal Motor Action Potential, Change at 12 mos. | Peroneal Motor Action Potential, Change at 24 mos. | |
| Dutasteride | 0.02 | 0.04 |
| Placebo | 0.16 | 0.15 |
"The MAX-PC anxiety subscale consists of 3 questions related to PSA testing; I have been so anxious about my PSA test that I have thought about delaying it., I have been so worried about my PSA test result that I have thought about asking my doctor to repeat the test., I have been so concerned about my PSA test result that I have thought about having the test repeated at another laboratory to make sure the test results were accurate. A higher MAX-PC score indicates greater anxiety.Scores range from 0 to 3 for each question. The total score is the sum of the 3 question scores; 0 to 9." (NCT00363311)
Timeframe: Baseline and Months 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Month 3 | Month 6 | Month 12 | Month 18 | Month 18 Take-Home | Month 36 | Month 36 Take-Home | |
| Dutasteride 0.5 mg Once Daily | 0.3 | -0.3 | -0.6 | -0.8 | -0.1 | -0.7 | -1.0 |
| Matching Placebo 0.5 mg Once Daily | 0.7 | 0.1 | 0.1 | -0.2 | 0.3 | 0.4 | 0.5 |
"The MAX-PC fear of recurrence subscale consists of 4 questions related to fear of recurrence; Because cancer is unpredictable, I feel I cannot plan for the future., My fear of having my cancer getting worse gets in the way of my enjoying life., I am afraid of my cancer getting worse., I am more nervous since I was diagnosed with prostate cancer. A higher MAX-PC score indicates greater anxiety. Scores range from 0 to 3 for each question. The total score is the sum of the 4 question scores: 0 to 12." (NCT00363311)
Timeframe: Baseline and Months 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Month 3, n=146, 143 | Month 6, n= 148, 143 | Month 12, n=148, 143 | Month 18, n=148, 143 | Month 18 Take-Home, n=148, 143 | Month 36, n=148, 143 | Month 36 Take-Home, n=148, 143 | |
| Dutasteride 0.5 mg Once Daily | -0.0 | -0.5 | -0.7 | -0.7 | -0.3 | -0.6 | -0.7 |
| Matching Placebo 0.5 mg Once Daily | -0.2 | -0.2 | -0.1 | -0.1 | 0.0 | 0.0 | 0.0 |
"Prostate volume was determined at baseline, Year 1.5, and Year 3. The anteroposterior, cephalocaudal, and transverse diameters of the prostate were obtained by transrectal ultrasound (TRUS) to calculate the prostate volume using the following formula:~π/ 6 (anteroposterior width * cephalocaudal width * transverse width). Prostate volume calculated by pre-programmed equipment was unacceptable for the on-study prostate volume measurements." (NCT00363311)
Timeframe: Baseline and Years 1.5 and 3
| Intervention | cc (Mean) | |
|---|---|---|
| Year 1.5, n=117, 117 | Year 3, n=118, 118 | |
| Dutasteride 0.5 mg Once Daily | -9.5 | -8.6 |
| Matching Placebo 0.5 mg Once Daily | 0.7 | 3.3 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | millimeters (Mean) | ||
|---|---|---|---|
| Year 1.5, n= 87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 2.5 | 1.5 | 3.8 |
| Matching Placebo 0.5 mg Once Daily | 3.9 | 1.8 | 4.8 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. Change from baseline was calculated as the number of cancer-positive cores at post-baseline biopsy minus the number of cancer-positive cores at baseline. (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | cores (Mean) | ||
|---|---|---|---|
| Year 1.5, n= 87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 0.6 | 2.0 | 2.5 |
| Matching Placebo 0.5 mg Once Daily | 1.1 | 2.0 | 3.0 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. (100 * number of positive cores/number of evaluated cores). (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | percentage of cores (Mean) | ||
|---|---|---|---|
| Year 1.5, n= 87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 3.7 | 1.5 | 6.0 |
| Matching Placebo 0.5 mg Once Daily | 8.4 | 4.1 | 10.0 |
The FACT-P consists of a total of 39 questions. This scale is divided into five subscales: the Physical Well-Being Subscale (7 questions); the Social/Family Well-Being Subscale (7 questions); the Emotional Well-Being Subscale (6 questions); the Functional Well-Being Subscale (7 questions); and the Prostate Cancer Subscale (12 questions). The questionnaire was administered at baseline and at Months 18 and 36. The score for each of the 39 questions ranges from 0 to 4. The total FACT-P score thus ranges from 0 to156; a higher score indicates better QOL. (NCT00363311)
Timeframe: Baseline and Months 18 and 36
| Intervention | points on a scale (Mean) | |
|---|---|---|
| Month 18, n=144, 140 | Month 36, n=148, 140 | |
| Dutasteride 0.5 mg Once Daily | -1.2 | -2.3 |
| Matching Placebo 0.5 mg Once Daily | -4.2 | -3.7 |
The MAX-PC is a self-reported measure evaluating three aspects of PC-related anxiety: general anxiety related to PC/treatment, fear of recurrence, and anxiety related to PSA testing. The MAX-PC consists of 18 questions, each score ranging from 0 (least anxiety) to 3 (maximum anxiety). Total score is the sum of each question score, thus ranging from 0 to 54. A higher MAX-PC score indicates greater anxiety. At Months 18 and 36, participants were given an additional copy of the questionnaire and were asked to complete at home once they were notified of their PSA result and to send back to clinic. (NCT00363311)
Timeframe: Baseline and Months 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Month 3, n=146, 143 | Month 6, n=148, 143 | Month 12, n=148, 143 | Month 18, n=148, 143 | Month 18 Take-Home, n=148, 143 | Month 36, n=148, 143 | Month 36 Take-Home, n=148, 143 | |
| Dutasteride 0.5 mg Once Daily | 0.3 | -0.8 | -1.4 | -1.6 | -0.6 | -1.5 | -1.8 |
| Matching Placebo 0.5 mg Once Daily | 0.4 | -0.0 | -0.1 | -0.3 | 0.6 | 0.5 | 0.7 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. Tumor length is calculated as the number of cores (12) * total tumor length/number of evaluated cores. (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | millimeters (Mean) | |||
|---|---|---|---|---|
| Baseline, n= 155, 147 | Year 1.5, n=87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 2.1 | 4.8 | 3.8 | 6.1 |
| Matching Placebo 0.5 mg Once Daily | 2.0 | 6.2 | 3.7 | 7.0 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsies (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. The sum of cancer positive cores and the sum of evaluated cores were used to compute the percentage (100* number of positive cores/number of evaluated cores). (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | percentage of cores (Mean) | |||
|---|---|---|---|---|
| Baseline, n= 155, 147 | Year 1.5, n=87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 14.5 | 19.0 | 17.3 | 21.7 |
| Matching Placebo 0.5 mg Once Daily | 14.3 | 23.7 | 16.5 | 24.7 |
All on-study or for-cause biopsies were reviewed and analyzed by a central pathologist. The 2005 International Society of Urological Pathologists recommendations for clinical tumor staging were used. T1c = tumor identified by needle biopsy (e.g., because of elevated prostate-specific antigen [PSA]); T2 = tumor confined within the prostate; T2a = tumor involves one-half of one lobe, but not both lobes of the prostate. (NCT00363311)
Timeframe: Baseline
| Intervention | biopsies (Number) | ||
|---|---|---|---|
| T1c | T2a | T2c | |
| Dutasteride 0.5 mg Once Daily | 117 | 29 | 1 |
| Matching Placebo 0.5 mg Once Daily | 125 | 30 | 0 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. All biopsies were reviewed and analyzed by a central pathologist. . The final biopsy is defined as the latest post-baseline biopsy for which the results are available from the central pathology laboratory. (NCT00363311)
Timeframe: Baseline, Year 1.5, Year 3, Years 0-3 (Final biopsy)
| Intervention | cores (Mean) | |||
|---|---|---|---|---|
| Baseline, n=155, 147 | Year 1.5, n=87, 99 | Year 3, n=52, 54 | Years 0-3 (Final biopsy), n=105, 90 | |
| Dutasteride 0.5 mg Once Daily | 1.6 | 2.2 | 2.0 | 2.5 |
| Matching Placebo 0.5 mg Once Daily | 1.6 | 2.8 | 2.0 | 3.0 |
Pathological progression is defined as one of the following: >=4 cores involved; >=50% of any 1 core involved; or a Gleason pattern of >=4 as a result of any on-study/for-cause biopsy. The 2005 International Society of Urological Pathologists recommendations for Gleason scoring (GS) were used to grade tumors. A primary grade is assigned to the most common tumor pattern, and a second grade to the next most common tumor pattern. The two grades are added together to get a GS. The Gleason grade=1-5, with 5 having the worst prognosis. The Gleason score=2-10, with 10 having the worst prognosis. (NCT00363311)
Timeframe: Year 1.5 and Overall (Years 0-3)
| Intervention | participants (Number) | |
|---|---|---|
| Year 1.5, n= 136, 139 | Overall (Years 0-3) n=136, 140 | |
| Dutasteride 0.5 mg Once Daily | 27 | 43 |
| Matching Placebo 0.5 mg Once Daily | 39 | 51 |
PC progression (prog.) was defined as the earliest occurrence of primary therapy, also referred to as therapeutic prog., for PC (prostatectomy/radiation/hormonal therapy); or pathological prog., defined as 1 of the following: >=4 cores involved; >=50% of any 1 core involved; or a Gleason pattern of >=4 as a result of any on-study/for-cause biopsy. Primary Gleason grade is assigned to the most common tumor pattern; a second grade to the next most common tumor pattern. The two grades are added together to get a score. Gleason grade= 1-5; Gleason score=2-10; 5 and 10 indicate worst prognosis. (NCT00363311)
Timeframe: Year 1.5 and Overall (Years 0-3)
| Intervention | participants (Number) | |
|---|---|---|
| Year 1.5, n=144, 142 | Overall (Years 0-3), n= 155, 147 | |
| Dutasteride 0.5 mg Once Daily | 32 | 54 |
| Matching Placebo 0.5 mg Once Daily | 50 | 71 |
The 2005 International Society of Urological Pathologists recommendations for Gleason scoring were used to grade tumors. A primary grade is assigned to the most common tumor pattern (how the cancer cells look under a microscope), and a second grade to the next most common pattern. The two grades are added together to get a GS. Gleason grade range= 1-5; 5=worst prognosis. GS range=2-10; 10=worst prognosis. Improvement is defined as a decrease in GS from a baseline score of 6 (GS<=6; includes no cancer); worsening is defined as an increase in GS from a baseline score of 6 (GS >6). (NCT00363311)
Timeframe: Year 1.5
| Intervention | participants (Number) | ||
|---|---|---|---|
| Improvement | No change | Worsening | |
| Dutasteride 0.5 mg Once Daily | 21 | 58 | 21 |
| Matching Placebo 0.5 mg Once Daily | 6 | 51 | 24 |
The 2005 International Society of Urological Pathologists recommendations for Gleason scoring were used to grade tumors. A primary grade is assigned to the most common tumor pattern (how the cancer cells look under a microscope), and a second grade to the next most common pattern. The two grades are added together to get a GS. Gleason grade range= 1-5; 5=worst prognosis. GS range=2-10; 10=worst prognosis. Improvement is defined as a decrease in GS from a baseline score of 6 (GS<=6; includes no cancer); worsening is defined as an increase in GS from a baseline score of 6 (GS >6). (NCT00363311)
Timeframe: Years 0-3 (Final Biopsy)
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Improvement | No cancer, GS 0 | No change | Worsening | |
| Dutasteride 0.5 mg Once Daily | 50 | 50 | 71 | 19 |
| Matching Placebo 0.5 mg Once Daily | 31 | 31 | 83 | 22 |
All on-study or for-cause biopsies were reviewed and analyzed by a central pathologist. The 2005 International Society of Urological Pathologists recommendations for Gleason scoring were used to grade the tumor. A primary grade is assigned to the most common tumor pattern (how the cancer cells look under a microscope), and a secondary grade to the next most common tumor pattern. The two grades are added together to get a GS. The Gleason grade ranges from 1 to 5, with 5 having the worst prognosis. The Gleason score ranges from 2 to 10, with 10 having the worst prognosis. (NCT00363311)
Timeframe: Years 0-3 (Final Biopsy)
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Missing (No Cancer) | GS 5 | GS 6 | GS 7, 3 (primary grade) + 4 (secondary grade) | GS 7, 4 (primary grade) + 3 (secondary grade) | GS 8 | GS 9-10 | |
| Dutasteride 0.5 mg Once Daily | 50 | 0 | 71 | 13 | 4 | 2 | 0 |
| Matching Placebo 0.5 mg Once Daily | 31 | 0 | 83 | 15 | 4 | 3 | 0 |
"All on-study or for-cause biopsies were reviewed and analyzed by a central pathologist. The National Comprehensive Network (NCCN), 2005 clinical practices guidelines in Oncology-prostate cancer were used for clinical tumor staging. T0: no evidence of primary tumor; T1: clinically inapparent tumor, neither palpable nor visible by imaging; T2: tumor confined within the prostate; T3: tumor extends through the prostate capsule; T4: tumor is fixed or invades adjacent structures other than seminal vesicles. A clinical stage of T0 in post-baseline biopsies has been interpreted as No Worsening." (NCT00363311)
Timeframe: Months 0-18
| Intervention | biopsies (Number) | |
|---|---|---|
| No Worsening (same/lower stage) | Worsening (higher stage) | |
| Dutasteride 0.5 mg Once Daily | 53 | 5 |
| Matching Placebo 0.5 mg Once Daily | 53 | 13 |
All participants were required by protocol to undergo a transrectal ultrasound (TRUS)-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. If a for-cause biopsy occurred within 6 months prior to the protocol-mandated biopsy, the biopsy was counted as the protocol-mandated biopsy. All biopsies were reviewed and analyzed by a central pathologist. (NCT00363311)
Timeframe: Baseline to Month 18
| Intervention | participants (Number) | |
|---|---|---|
| Participants with a PCa diagnosis | Participants with no PCa diagnosis | |
| Dutasteride 0.5 mg Once Daily | 111 | 29 |
| Matching Placebo 0.5 mg Once Daily | 111 | 25 |
All participants were required by protocol to undergo a TRUS-guided 12-core prostate biopsy at 1.5 and 3 years or at the end of the study, if the participant discontinued the study early. Any for-cause biopsy (outside of protocol-mandated biopsies) 12 cores were obtained. If a for-cause biopsy occurred within 6 months prior to the protocol-mandated biopsy, the biopsy was counted as the protocol-mandated biopsy. The final biopsy is defined as the latest post-baseline biopsy for which the results are available from the central pathology laboratory. (NCT00363311)
Timeframe: Years 0-3
| Intervention | participants (Number) | |
|---|---|---|
| Participants with a PCa diagnosis | Participants with no PCa diagnosis | |
| Dutasteride 0.5 mg Once Daily | 90 | 50 |
| Matching Placebo 0.5 mg Once Daily | 105 | 31 |
"Prostate volume was determined at baseline, Year 1.5, and Year 3. The anteroposterior, cephalocaudal, and transverse diameters of the prostate were obtained by transrectal ultrasound (TRUS) to calculate the prostate volume using the following formula:~π/ 6 (anteroposterior width * cephalocaudal width * transverse width). Prostate volume calculated by pre-programmed equipment is unacceptable for the on-study prostate volume measurements." (NCT00363311)
Timeframe: Baseline and Years 1.5 and 3
| Intervention | percent change (Mean) | |
|---|---|---|
| Year 1.5, n=117, 117 | Year 3, n=118, 118 | |
| Dutasteride 0.5 mg Once Daily | -19.8 | -18.0 |
| Matching Placebo 0.5 mg Once Daily | 3.7 | 7.7 |
The FACT-P consists of a total of 39 questions. This scale is divided into five subscales: the Physical Well-Being Subscale (7 questions); the Social/Family Well-Being Subscale (7 questions); the Emotional Well-Being Subscale (6 questions); the Functional Well-Being Subscale (7 questions); and the Prostate Cancer Subscale (12 questions). The questionnaire was administered at baseline and at Months 18 and 36. The score for each of the 39 questions ranges from 0 to 4. The total FACT-P score thus ranges from 0 to156; a higher score indicates better QOL. (NCT00363311)
Timeframe: Baseline and Months 18 and 36
| Intervention | points on a scale (Mean) | |
|---|---|---|
| Month 18, n=144, 140 | Month 36, n=148, 140 | |
| Dutasteride 0.5 mg Once Daily | -0.2 | -1.0 |
| Matching Placebo 0.5 mg Once Daily | -2.8 | -1.8 |
"Prostate volume was determined at baseline, at Year 1.5, and at Year 3. The anteroposterior, cephalocaudal, and transverse diameters of the prostate were obtained by transrectal ultrasound (TRUS) to calculate the prostate volume using the following formula:~π/ 6 (anteroposterior width * cephalocaudal width * transverse width). Prostate volume calculated by pre-programmed equipment is unacceptable for the on-study prostate volume measurements." (NCT00363311)
Timeframe: Baseline and Years 1.5 and 3
| Intervention | cubic centimeters (cc) (Mean) | ||
|---|---|---|---|
| Baseline, n=133, 126 | Year 1.5, n=117, 117 | Year 3, n=118, 118 | |
| Dutasteride 0.5 mg Once Daily | 43.2 | 43.3 | 43.1 |
| Matching Placebo 0.5 mg Once Daily | 44.2 | 43.1 | 43.0 |
The FACT-P consists of a total of 39 questions. This scale is divided into five subscales: the Physical Well-Being Subscale (7 questions); the Social/Family Well-Being Subscale (7 questions); the Emotional Well-Being Subscale (6 questions); the Functional Well-Being Subscale (7 questions); and the Prostate Cancer Subscale (12 questions). The score for each of the 39 questions ranges from 0 to 4. The total FACT-P score thus ranges from 0 to156; a higher score indicates better quality of life. (NCT00363311)
Timeframe: Baseline and Months 18 and 36
| Intervention | points on a scale (Mean) | ||
|---|---|---|---|
| Baseline, n=154, 145 | Month 18, n=145, 140 | Month 36, n=149, 140 | |
| Dutasteride 0.5 mg Once Daily | 131.3 | 130.2 | 129.0 |
| Matching Placebo 0.5 mg Once Daily | 129.9 | 126.9 | 126.6 |
"The MAX-PC anxiety subscale consists of 3 questions related to PSA testing; I have been so anxious about my PSA test that I have thought about delaying it., I have been so worried about my PSA test result that I have thought about asking my doctor to repeat the test., I have been so concerned about my PSA test result that I have thought about having the test repeated at another laboratory to make sure the test results were accurate. A higher MAX-PC score indicates greater anxiety.Scores range from 0 to 3 for each question. The total score is the sum of the 3 question scores; 0 to 9." (NCT00363311)
Timeframe: Baseline and Months 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline, n=154, 147 | Month 3, n=152, 144 | Month 6, n=152, 144 | Month 12, n=152, 144 | Month 18, n=152, 144 | Month 18 Take-Home, n=152, 144 | Month 36, n=152,144 | Month 36 Take-Home, n=152, 144 | |
| Dutasteride 0.5 mg Once Daily | 7.3 | 7.5 | 6.9 | 6.6 | 6.4 | 7.1 | 6.5 | 6.2 |
| Matching Placebo 0.5 mg Once Daily | 7.1 | 7.5 | 7.0 | 7.0 | 6.7 | 7.2 | 7.3 | 7.4 |
"The MAX-PC fear of recurrence subscale consists of 4 questions related to fear of recurrence; Because cancer is unpredictable, I feel I cannot plan for the future., My fear of having my cancer getting worse gets in the way of my enjoying life., I am afraid of my cancer getting worse., I am more nervous since I was diagnosed with prostate cancer. A higher MAX-PC score indicates greater anxiety. Scores range from 0 to 3 for each question. The total score is the sum of the 4 question scores: 0 to 12." (NCT00363311)
Timeframe: Baseline and Months 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Baseline, n=151, 146 | Month 3, n=150, 144 | Month 6, n=152, 144 | Month 12, n=152, 144 | Month 18, n=152, 144 | Month 18 Take-Home, n=152, 144 | Month 36, n=152, 144 | |
| Dutasteride 0.5 mg Once Daily | 3.4 | 3.3 | 2.9 | 2.6 | 2.7 | 3.0 | 2.7 |
| Matching Placebo 0.5 mg Once Daily | 3.4 | 3.2 | 3.3 | 3.2 | 3.3 | 3.4 | 3.4 |
The MAX-PC is a self-reported measure evaluating three aspects of PC-related anxiety: general anxiety related to PC/treatment, fear of recurrence, and anxiety related to PSA testing. The MAX-PC consists of 18 questions, each score ranging from 0 (least anxiety) to 3 (maximum anxiety). Total score is the sum of each question score, thus ranging from 0 to 54. A higher MAX-PC score indicates greater anxiety. At Months 18 and 36, participants were given an additional copy of the questionnaire and were asked to complete at home once they were notified of their PSA result and to send back to clinic. (NCT00363311)
Timeframe: Baseline and Month 3, 6, 12, 18, and 36
| Intervention | points on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline, n=151, 146 | Month 3, n=150, 144 | Month 6, n=152, 144 | Month 12, n=152, 144 | Month 18, n=152, 144 | Month 18 Take-Home, n=152, 144 | Month 36, n=152, 144 | Month 36 Take-Home, n=152, 144 | |
| Dutasteride 0.5 mg Once Daily | 11.3 | 11.4 | 10.4 | 9.7 | 9.5 | 10.6 | 9.6 | 9.4 |
| Matching Placebo 0.5 mg Once Daily | 11.0 | 11.4 | 10.9 | 10.7 | 10.5 | 11.4 | 11.3 | 11.5 |
"The FACT-P Physical Well-Being subscale is divided into 7 questions, and the participants rated the outcome over the past 7 days; I have a lack of energy., I have nausea., Because of my physical condition, I have trouble meeting the needs of my family., I have pain., I am bothered by side effects of treatment., I feel ill., I am forced to spend time in bed. The score for each question ranges from 0 to 4; a lower score indicates better physical well-being. The total FACT-P score thus ranges from 0 to156; a higher score indicates a better quality of life." (NCT00363311)
Timeframe: Baseline and Months 18 and 36
| Intervention | points on a scale (Mean) | |
|---|---|---|
| Month 18, n=148, 140 | Month 36, n=149, 140 | |
| Dutasteride 0.5 mg Once Daily | -0.2 | -0.3 |
| Matching Placebo 0.5 mg Once Daily | -0.4 | -0.3 |
Primary therapy, also referred to as therapeutic progression, for prostate cancer can be one of the following: prostatectomy, radiation, or hormonal therapy. (NCT00363311)
Timeframe: Year 1.5 and Overall (Years 0-3)
| Intervention | participants (Number) | |
|---|---|---|
| Year 1.5 | Overall (Years 0-3) | |
| Dutasteride 0.5 mg Once Daily | 5 | 11 |
| Matching Placebo 0.5 mg Once Daily | 11 | 20 |
"The FACT-P Social Well-Being subscale is divided into 7 questions, and the participants rated the outcome over the past 7 days; I feel close to my friends., I get emotional support from my family., I get support from my friends., My family has accepted my illness., I am satisfied with family communication about my illness., I feel close to my partner (or the person who is my main support)., I am satisfied with my sex life. The score for each question ranges from 0 to 4; a higher score indicates better social well-being. The total FACT-P score thus ranges from 0 to 156." (NCT00363311)
Timeframe: Baseline and Months 18 and 36
| Intervention | points on a scale (Mean) | |
|---|---|---|
| Month 18, n=148, 140 | Month 36, n=149, 140 | |
| Dutasteride 0.5 mg Once Daily | -0.6 | -1.2 |
| Matching Placebo 0.5 mg Once Daily | -1.4 | -1.1 |
Improvement is defined as greater than or equal to a 2 point increase in participants total score on the I-PSS questionaire. (NCT00368979)
Timeframe: Baseline and Week 52
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Improvement >=2 Points | Improvement >=3 Points | Improvement >=4 Points | Improvement >=5 Points | Improvement >=6 Points | Improvement >=20% | Improvement >=25% | Improvement >=30% | Improvement >=40% | Improvement >=50% | Improvement >=75% | |
| Dutasteride | 139 | 128 | 115 | 94 | 82 | 122 | 114 | 106 | 86 | 67 | 17 |
| Placebo | 113 | 102 | 82 | 75 | 62 | 99 | 84 | 71 | 54 | 39 | 7 |
Improvement was defined as an increase in Qmax by greater than or equal to 1 mL/sec (NCT00368979)
Timeframe: Baseline and Week 52
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Improvement >=1 mL/sec | Improvement >=2 mL/sec | Improvement >=2.5 mL/sec | Improvement >=3 mL/sec | Improvement >=4 mL/sec | Improvement >=5 mL/sec | Improvement >=10 mL/sec | Improvement >=30% | |
| Dutasteride | 103 | 86 | 73 | 70 | 53 | 44 | 11 | 63 |
| Placebo | 79 | 56 | 45 | 44 | 29 | 22 | 4 | 41 |
The International Prostate Symptom Score (I-PSS) consists of 7 verified questions concerning urinary symptoms and one quality of life question scored from 0 to 5(0=Not at All, to 5=Almost Always). The total score can range from 0 to 35. Score of 1-7=Mild, 8-19=Moderate, 20-35=Severe. (NCT00368979)
Timeframe: Baseline and Week 52
| Intervention | score on a scale (Mean) |
|---|---|
| Placebo | -3.6 |
| Dutasteride | -5.5 |
Maximum Urine Flow Rate (Qmax) is the peak flow in milliliters per second. (NCT00368979)
Timeframe: Baseline and Week 52
| Intervention | milliliters per second (mL/sec) (Mean) |
|---|---|
| Placebo | 0.6 |
| Dutasteride | 2.2 |
Prostate volume measurements by transrectal ultrasound (TRUS). Average prostate volume (55cc). The Ultrasound scans the prostate in the transverse plane while moving in the cephalocaudal direction of the prostate. The height and width of the prostate section with the greatest surface area is recorded. (NCT00368979)
Timeframe: Baseline and Week 52
| Intervention | cubic centimeters (cc) (Mean) |
|---|---|
| Placebo | -8.9 |
| Dutasteride | -31.5 |
AUA symptoms index change is measured on a five level-scale: -2 (much worse), -1(worse) , 0 (no change), 1 (better), 2 (much better) (NCT00431626)
Timeframe: one year
| Intervention | units on a scale (Mean) |
|---|---|
| Laser TURP With Dutasteride | 1 |
GlaxoSmithKline - Hair Growth Index with Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions comparing photographs of their hair before treatment and concerning the last week and evaluated the change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Much less scalp (Month 3) | Moderately less scalp (Month 3) | Slightly less scalp (Month 3) | The same amount of scalp (Month 3) | Slightly more scalp (Month 3) | Moderately more scalp (Month 3) | Much more scalp (Month 3) | Much less scalp (Month 6) | Moderately less scalp (Month 6) | Slightly less scalp (Month 6) | The same amount of scalp (Month 6) | Slightly more scalp (Month 6) | Moderately more scalp (Month 6) | Much more scalp (Month 6) | |
| Dutasteride | 1 | 2 | 3 | 20 | 25 | 15 | 7 | 0 | 0 | 2 | 22 | 17 | 28 | 4 |
| Placebo | 1 | 3 | 14 | 24 | 23 | 7 | 3 | 2 | 5 | 21 | 28 | 17 | 1 | 1 |
GlaxoSmithKline - Hair Growth Index without Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions without photographs concerning their perception of Change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Much less hair (Month 3) | Moderately less hair (Month 3) | Slightly less hair (Month 3) | The same amount of hair (Month 3) | Slightly more hair (Month 3) | Moderately more hair (Month 3) | Much more hair (Month 3) | Much less hair (Month 6) | Moderately less hair (Month 6) | Slightly less hair (Month 6) | The same amount of hair (Month 6) | Slightly more hair (Month 6) | Moderately more hair (Month 6) | Much more hair (Month 6) | |
| Dutasteride | 5 | 8 | 26 | 32 | 1 | 1 | 0 | 9 | 13 | 24 | 25 | 2 | 0 | 0 |
| Placebo | 4 | 7 | 26 | 36 | 2 | 0 | 0 | 7 | 8 | 22 | 35 | 3 | 0 | 0 |
GlaxoSmithKline - Hair Growth Index without Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions without photographs concerning their perception of Change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| I strongly disagree (Month 3) | I disagree (Month 3) | No opinion either way (Month 3) | I agree(Month 3) | I strongly agree (Month 3) | I strongly disagree (Month 6) | I disagree (Month 6) | No opinion either way (Month 6) | I agree (Month 6) | I strongly agree(Month 6) | |
| Dutasteride | 0 | 4 | 5 | 62 | 2 | 0 | 3 | 3 | 60 | 7 |
| Placebo | 0 | 8 | 11 | 56 | 0 | 0 | 8 | 9 | 58 | 0 |
GlaxoSmithKline - Hair Growth Index without Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions without photographs concerning their perception of Change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Much worse (Month 3) | Moderately worse (Month 3) | Slightly worse (Month 3) | Not Changed (Month 3) | Slightly Better (Month 3) | Moderately Better (Month 3) | Much Better (Month 3) | Much worse (Month 6) | Moderately worse (Month 6) | Slightly worse (Month 6) | Not changed (Month 6) | Slightly Better (Month 6) | Moderately Better (Month 6) | Much Better (Month 6) | |
| Dutasteride | 0 | 0 | 1 | 36 | 25 | 7 | 4 | 0 | 1 | 2 | 23 | 26 | 11 | 10 |
| Placebo | 0 | 1 | 4 | 47 | 20 | 3 | 0 | 0 | 0 | 10 | 33 | 29 | 3 | 0 |
GlaxoSmithKline - Hair Growth Index without Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions without photographs concerning their perception of Change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| I strongly disagree (month 3) | I disagree (month 3) | No opinion either way (month 3) | I agree (month 3) | I strongly agree (month 3) | I strongly disagree (month 6) | I disagree (month 6) | No opinion either way (month 6) | I agree (month 6) | I strongly agree (month 6) | |
| Dutasteride | 0 | 18 | 20 | 34 | 1 | 0 | 18 | 12 | 40 | 3 |
| Placebo | 1 | 30 | 13 | 30 | 1 | 0 | 27 | 17 | 29 | 2 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 6
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small Problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Problem | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 53 | 6 | 3 | 1 | 0 | 2 | 0 | 2 | 1 | 0 | 2 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 52 | 5 | 3 | 0 | 0 | 3 | 3 | 0 | 0 | 0 | 1 | 1 | 4 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 6
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small Problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Problem | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 54 | 5 | 2 | 1 | 0 | 3 | 3 | 1 | 0 | 0 | 1 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 54 | 5 | 3 | 0 | 0 | 3 | 1 | 0 | 1 | 0 | 1 | 2 | 3 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 6
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small Problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Problem | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 53 | 6 | 2 | 1 | 0 | 0 | 0 | 3 | 1 | 0 | 3 | 1 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 52 | 4 | 4 | 0 | 0 | 4 | 0 | 1 | 0 | 0 | 1 | 2 | 3 | 2 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
The Macrophotographic hair count method marks a 1-inch diameter circular area at the anterior leading edge of the vertex thinning area and then photographed. The photographs are enlarged and converted into dot maps and the dot maps are converted into total hair counts by means of personal computer-based scanners and imaging software. (NCT00441116)
Timeframe: Baseline and 6 months
| Intervention | hair count per centimeters squared (Mean) | ||
|---|---|---|---|
| Baseline | Month 6 | Change from Baseline - Month 6 | |
| Dutasteride | 148.14 | 162.27 | 12.21 |
| Placebo | 144.27 | 149.57 | 4.67 |
Normal ranges: TSH, 0.25-3.50 µIU/mL; T4, 4.5-12.0 mg/dL; PSA, ≤4 ng/mL; DHT, males (m): prepuberty, <0.1, adult, 0.25-0.75; females (f): prepuberty, <0.03, premenopausal, 0.05-0.3, menopausal, <0.03 ng/mL; T, m: 2.36-9.96; f: 0.08-0.86 ng/mL; LH, m: 1-8; f: follicular, 4-12; periovulatory, >20; luteal 5-20; postmenopausal, >10 IU/L. (NCT00441116)
Timeframe: Baseline to Month 6 and Month 10
| Intervention | Participants (Number) | |||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| TSH - Baseline - Normal | TSH - Baseline - Abnormal | TSH - Month 6 - Normal | TSH - Month 6 - Abnormal | TSH - Month 10 - Normal | TSH - Month 10 - Abnormal | T4 - Baseline - Normal | T4 - Baseline - Abnormal | T4 - Month 6 - Normal | T4 - Month 6 - Abnormal | T4 - Month 10 - Normal | T4 - Month 10 - Abnormal | PSA - Screening - Normal | PSA - Screening - Abnormal | PSA - Month 6 - Normal | PSA - Month 6 - Abnormal | PSA - Month 10 - Normal | PSA - Month 10 - Abnormal | DHT - Screening - Normal | DHT - Screening - Abnormal | DHT - Month 6 - Normal | DHT - Month 6 - Abnormal | DHT - Month 10 - Normal | DHT - Month 10 - Abnormal | Testosterone - Screening - Normal | Testosterone - Screening - Abnormal | Testosterone - Month 6 - Normal | Testosterone - Month 6 - Abnormal | Testosterone - Month 10 - Normal | Testosterone - Month 10 - Abnormal | LH - Baseline - Normal | LH - Baseline - Abnormal | |
| Dutasteride | 70 | 3 | 70 | 0 | 71 | 1 | 73 | 0 | 70 | 0 | 72 | 0 | 73 | 0 | 70 | 0 | 72 | 0 | 72 | 1 | 69 | 1 | 70 | 2 | 73 | 0 | 67 | 3 | 69 | 3 | 67 | 6 |
| Placebo | 75 | 0 | 69 | 4 | 74 | 1 | 75 | 0 | 71 | 2 | 74 | 1 | 75 | 0 | 73 | 0 | 75 | 0 | 74 | 1 | 69 | 4 | 72 | 3 | 74 | 1 | 71 | 2 | 74 | 1 | 64 | 11 |
Improvement Distribution is based on the number of hairs per centimeters squared by macrophotographic conversion hair count. Score Range -3=greatly decreased to +3=greatly increased. 0=No change. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Greatly decreased (Month 3) | Moderately decreased (Month 3) | Slightly decreased (Month 3) | No Change (Month 3) | Slightly increased (Month 3) | Moderately increased (Month 3) | Greatly increased (Month 3) | Greatly decreased (Month 6) | Moderately decreased (Month 6) | Slightly decreased (Month 6) | No Change (Month 6) | Slightly increased (Month 6) | Moderately increased (Month 6) | Greatly increased (Month 6) | |
| Dutasteride | 0 | 1 | 0 | 28 | 35 | 8 | 1 | 0 | 0 | 4 | 24 | 31 | 12 | 2 |
| Placebo | 0 | 1 | 13 | 30 | 30 | 1 | 0 | 0 | 8 | 16 | 36 | 14 | 1 | 0 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 10
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small Problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Problem | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 57 | 5 | 0 | 0 | 0 | 2 | 1 | 1 | 0 | 0 | 3 | 1 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 55 | 3 | 0 | 2 | 0 | 4 | 0 | 1 | 0 | 0 | 1 | 3 | 3 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 10
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small Problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Problem | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 54 | 6 | 3 | 0 | 0 | 2 | 3 | 0 | 0 | 0 | 3 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 54 | 5 | 0 | 1 | 0 | 2 | 4 | 0 | 0 | 0 | 2 | 2 | 2 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
"In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? For example, No Problem shift to No Problem indicates that the participant experienced no problem at baseline and no problem at Month 6, respectively." (NCT00441116)
Timeframe: Baseline to Month 10
| Intervention | Participants (Number) | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No Problem shift to No Problem | No Problem shift to Very Small problem | No Problem shift to Small Problem | No Problem shift to Medium Problem | No Problem shift to Big Problem | Very Small Problem shift to No Problem | Very Small Problem shift to Very Small Problem | Very Small Problem shift to Small Problem | Very Small Problem shift to Medium Problem | Very Small Problem shift to Big Problem | Small Problem shift to No Problem | Small Problem shift to Very Small Problem | Small Problem shift to Small Problem | Small Problem shift to Medium Problem | Small Problem shift to Big Problem | Medium Problem shift to No Problem | Medium Problem shift to Very Small Problem | Medium Problem shift to Small Problem | Medium Problem shift to Medium Problem | Medium Problem shift to Big Problem | Big Problem shift to No Proble | Big Problem shift to Very Small Problem | Big Problem shift to Small Problem | Big Problem shift to Medium Problem | Big Problem shift to Big Problem | |
| Dutasteride | 56 | 2 | 3 | 0 | 1 | 2 | 5 | 0 | 0 | 0 | 2 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 56 | 6 | 0 | 0 | 0 | 3 | 1 | 0 | 1 | 0 | 2 | 3 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? (NCT00441116)
Timeframe: Screening
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sex Drive - No Problem | Sex Drive - Very Small Problem | Sex Drive - Small Problem | Sex Drive - Medium Problem | Sex Drive - Big Problem | Erection - No Problem | Erection - Very Small Problem | Erection - Small Problem | Erection - Medium Problem | Erection - Big Problem | Ejaculation - No Problem | Ejaculation - Very Small Problem | Ejaculation - Small Problem | Ejaculation - Medium Problem | Ejaculation - Big Problem | |
| Dutasteride | 60 | 5 | 4 | 4 | 0 | 62 | 7 | 4 | 0 | 0 | 64 | 6 | 3 | 0 | 0 |
| Placebo | 58 | 5 | 9 | 3 | 0 | 60 | 6 | 7 | 2 | 0 | 63 | 4 | 7 | 1 | 0 |
In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? (NCT00441116)
Timeframe: Month 6
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sex Drive - No Problem | Sex Drive - Very Small Problem | Sex Drive - Small Problem | Sex Drive - Medium Problem | Sex Drive - Big Problem | Erection - No Problem | Erection - Very Small Problem | Erection - Small Problem | Erection - Medium Problem | Erection - Big Problem | Ejaculation - No Problem | Ejaculation - Very Small Problem | Ejaculation - Small Problem | Ejaculation - Medium Problem | Ejaculation - Big Problem | |
| Dutasteride | 56 | 7 | 7 | 2 | 0 | 57 | 6 | 6 | 3 | 0 | 58 | 8 | 4 | 2 | 0 |
| Placebo | 59 | 6 | 8 | 2 | 0 | 58 | 9 | 7 | 1 | 0 | 59 | 8 | 6 | 2 | 0 |
In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? (NCT00441116)
Timeframe: Month 3
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sex Drive - No Problem | Sex Drive - Very small Problem | Sex Drive - Small Problem | Sex Drive - Medium Problem | Sex Drive - Big Problem | Erection - No Problem | Erection - Very Small Problem | Erection - Small Problem | Erection - Medium Problem | Erection - Big Problem | Ejaculation - No Problem | Ejaculation - Very Small Problem | Ejaculation - Small Problem | Ejaculation - Medium Problem | Ejaculation - Big Problem | |
| Dutasteride | 49 | 12 | 5 | 5 | 0 | 52 | 11 | 2 | 6 | 0 | 55 | 9 | 3 | 4 | 0 |
| Placebo | 59 | 8 | 5 | 0 | 1 | 56 | 10 | 3 | 3 | 1 | 59 | 8 | 3 | 2 | 1 |
In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? (NCT00441116)
Timeframe: Month 10
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sex Drive - No Problem | Sex Drive - Very Small Problem | Sex Drive - Small Problem | Sex Drive - Medium Problem | Sex Drive - Big Problem | Erection - No Problem | Erection - Very Small Problem | Erection - Small Problem | Erection - Medium Problem | Erection - Big Problem | Ejaculation - No Problem | Ejaculation - Very Small Problem | Ejaculation - Small Problem | Ejaculation - Medium Problem | Ejaculation - Big Problem | |
| Dutasteride | 62 | 7 | 2 | 1 | 0 | 59 | 9 | 4 | 0 | 0 | 60 | 7 | 4 | 0 | 1 |
| Placebo | 62 | 6 | 4 | 3 | 0 | 60 | 11 | 2 | 2 | 0 | 62 | 10 | 1 | 2 | 0 |
In the past 7 days, to what extent have you considered: a lack of sex drive to be a problem?, your ability to get and keep erections to be a problem? your ejaculation to be a problem? (NCT00441116)
Timeframe: Baseline
| Intervention | Participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sex Drive - No Problem | Sex Drive - Very small problem | Sex Drive - Small problem | Sex Drive - Medium problem | Sex Drive - Big problem | Erection - No Problem | Erection - Very small problem | Erection - Small problem | Erection - Medium problem | Erection - Big problem | Ejaculation - No Problem | Ejaculation - Very small problem | Ejaculation - Small problem | Ejaculation - Medium problem | Ejaculation - Big problem | |
| Dutasteride | 63 | 4 | 6 | 0 | 0 | 64 | 5 | 4 | 0 | 0 | 63 | 7 | 3 | 0 | 0 |
| Placebo | 60 | 5 | 8 | 1 | 0 | 60 | 6 | 7 | 1 | 0 | 62 | 5 | 7 | 0 | 0 |
"Improvement Distribution is based on the number of hairs per centimeters squared by macrophotographic conversion hair count.~Score Range -3=greatly decreased to +3=greatly increased. 0=No change." (NCT00441116)
Timeframe: Baseline to Month 3 and Baseline to Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Greatly decreased (Month 3) | Moderately decreased (Month 3) | Slightly decreased (Month 3) | No change (Month 3) | Slightly increased (Month 3) | Moderately increased (Month 3) | Greatly increased (Month 3) | Greatly decreased (Month 6) | Moderately decreased (Month 6) | Slightly decreased (Month 6) | No Change (Month 6) | Slightly increased (Month 6) | Moderately increased (Month 6) | Greatly increased (Month 6) | |
| Dutasteride | 0 | 1 | 3 | 28 | 33 | 8 | 0 | 0 | 0 | 6 | 40 | 20 | 5 | 2 |
| Placebo | 0 | 0 | 14 | 29 | 28 | 4 | 0 | 1 | 4 | 29 | 32 | 8 | 1 | 0 |
Glucose, Creatinine, Ferritine (ug/L) and Zinc (Hmol/L) (NCT00441116)
Timeframe: Baseline and Month 6
| Intervention | mg/dL (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Glucose - Baseline | Glucose - Month 6 | Creatinine - Baseline | Creatinine - Month 6 | Ferritine (ug/L) - Baseline | Ferritine (ug/L) - Month 6 | Zinc (Hmol/L) - Baseline | Zinc (Hmol/L) - Month 6 | |
| Dutasteride | 104.48 | 104.49 | 1.03 | 1.05 | 100.21 | 109.61 | 111.19 | 118.07 |
| Placebo | 101.56 | 106.31 | 1.03 | 1.06 | 131.91 | 132.36 | 112.66 | 113.87 |
sGOT (AST)- serum Glutamic-Oxaloacetic Transaminase, sGPT (ALT) - serum Glutamic-Pyruvic Transaminase, Alkaline Phosphatase, Bilirubin(mg/dL) and Albumin(g/dL) (NCT00441116)
Timeframe: Baseline and Month 6
| Intervention | IU/L (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| AST(SGOT) - Baseline | AST(SGOT) - Month 6 | ALT(SGPT) - Baseline | ALT(SGPT) - Month 6 | Alkaline Phosphatase - Baseline | Alkaline Phosphatase - Month 6 | Bilirubin (mg/dL) - Baseline | Bilirubin (mg/dL) - Month 6 | Albumin (g/dL) - Baseline | Albumin (g/dL) - Month 6 | |
| Dutasteride | 23.10 | 25.88 | 29.79 | 34.00 | 87.34 | 85.51 | 0.78 | 0.80 | 4.66 | 4.64 |
| Placebo | 22.80 | 25.11 | 26.91 | 30.47 | 85.79 | 84.24 | 0.71 | 0.79 | 4.60 | 4.60 |
Comparing Lab values and differences from Baseline to month 6 (NCT00441116)
Timeframe: Baseline and Month 6
| Intervention | thousands/microliter (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| WBC - Baseline | WBC - Month 6 | Neutrophils - Baseline | Neutrophils - Month 6 | Lymphocytes - Baseline | Lymphocytes - Month 6 | Monocytes - Baseline | Monocytes - Month 6 | Eosinophils - Baseline | Eosinophils - Month 6 | Basophils - Baseline | Basophils - Month 6 | Platelets - Baseline | Platelets - Month 6 | Hemoglobin (%)- Baseline | Hemoglobin (%) - Month 6 | MCV (fL)- Baseline | MCV (fL) - Month 6 | |
| Dutasteride | 6898.49 | 6463.61 | 53.46 | 52.47 | 35.96 | 36.96 | 7.03 | 7.08 | 2.81 | 2.75 | 0.48 | 0.50 | 249.63 | 243.69 | 15.44 | 15.41 | 92.12 | 91.57 |
| Placebo | 6336.93 | 6387.03 | 53.52 | 52.90 | 35.87 | 36.03 | 7.03 | 7.14 | 2.69 | 2.99 | 0.52 | 0.51 | 250.19 | 240.26 | 15.54 | 15.46 | 91.89 | 91.44 |
Sodium, Potassium (mEq/L), and Bicarbonate (NCT00441116)
Timeframe: Baseline and Month 6
| Intervention | mmol/L (Mean) | |||||
|---|---|---|---|---|---|---|
| Sodium - Baseline | Sodium - Month 6 | Potassium (mEq/L) - Baseline | Potassium (mEq/L) - Month 6 | Bicarbonate - Baseline | Bicarbonate - Month 6 | |
| Dutasteride | 141.23 | 141.54 | 4.22 | 4.25 | 27.66 | 26.61 |
| Placebo | 141.41 | 141.58 | 4.34 | 4.29 | 28.23 | 27.08 |
Mean percent change from Baseline for testosterone. Testosterone was measured in ng/ml. (NCT00441116)
Timeframe: Month 3, Month 6, and Month 10
| Intervention | Percent change (Mean) | ||
|---|---|---|---|
| % Change in Testosterone - Month 3 | % Change in Testosterone - Month 6 | % Change in Testosterone - Month 10 | |
| Dutasteride | 18.78 | 8.15 | 12.18 |
| Placebo | -5.27 | -6.59 | 0.99 |
Mean percent change from Baseline for DHT. DHT was measured in pg/ml. Change from baseline = Month 3, 6, and 10 values minus baseline value. (NCT00441116)
Timeframe: Month 3, Month 6 and Month 10
| Intervention | Percent change (Mean) | ||
|---|---|---|---|
| % Change in DHT - Month 3 | % Change in DHT - Month 6 | % Change in DHT - Month 10 | |
| Dutasteride | -16.92 | -4.30 | 3.85 |
| Placebo | -1.90 | 22.83 | 7.58 |
GlaxoSmithKline - Hair Growth Index with Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions comparing photographs of their hair before treatment and concerning the last week and evaluated the change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Much less scalp (month 3) | Moderately less scalp (month 3) | Slightly less scalp (month 3) | The same amount of scalp (month 3) | Slightly more scalp (month 3) | Moderately more scalp (month 3) | Much more scalp (month 3) | Much less scalp (month 6) | Moderately less scalp (month 6) | Slightly less scalp (month 6) | The same amount of scalp (month 6) | Slightly more scalp (month 6) | Moderately more scalp (month 6) | Much more scalp (month 6) | |
| Dutasteride | 10 | 17 | 25 | 14 | 3 | 1 | 3 | 9 | 16 | 26 | 20 | 1 | 1 | 0 |
| Placebo | 3 | 11 | 17 | 26 | 14 | 4 | 0 | 2 | 5 | 15 | 26 | 22 | 4 | 1 |
GlaxoSmithKline - Hair Growth Index with Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions comparing photographs of their hair before treatment and concerning the last week and evaluated the change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Greatly decreased (Month 3) | Moderately decreased (Month 3) | Slightly decreased (Month 3) | Stayed the same (Month 3) | Slightly increased (Month 3) | Moderately increased (Month 3) | Greatly increased (Month 3) | Greatly decreased (Month 6) | Moderately decreased (Month 6) | Slightly decreased (Month 6) | Stayed the same (Month 6) | Slightly increased (Month 6) | Moderately increased (Month 6) | Greatly increased (Month 6) | |
| Dutasteride | 0 | 2 | 7 | 17 | 26 | 15 | 6 | 0 | 0 | 0 | 22 | 22 | 23 | 6 |
| Placebo | 0 | 1 | 19 | 21 | 21 | 10 | 3 | 2 | 4 | 22 | 26 | 18 | 2 | 1 |
GlaxoSmithKline - Hair Growth Index with Photographs subject assessment of change in hair loss and overall appearance at 3 and 6 months. Subjects answered 4 questions comparing photographs of their hair before treatment and concerning the last week and evaluated the change in Hair Growth. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Much Worse (Month 3) | Moderately Worse (Month 3) | Slightly Worse (Month 3) | Not Changed (Month 3) | Slightly Better (Month 3) | Moderately Better (Month 3) | Much Better (Month 3) | Much Worse (Month 6) | Moderately Worse (Month 6) | Slightly Worse (Month 6) | Not Changed (Month 6) | Slightly Better (Month 6) | Moderately Better (Month 6) | Much Better (Month 6) | |
| Dutasteride | 0 | 2 | 2 | 16 | 28 | 14 | 11 | 0 | 0 | 0 | 21 | 24 | 19 | 9 |
| Placebo | 0 | 1 | 9 | 28 | 24 | 9 | 4 | 1 | 2 | 20 | 25 | 23 | 2 | 2 |
Improvement Distribution Score is based on the number of hairs per centimeters squared by macrophotographic conversion hair count. Score Range: -3 = greatly decreased to +3 = greatly increased. 0 = No change. (NCT00441116)
Timeframe: Month 3 and Month 6
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Month 3 Mean Score | Month 6 Mean Score | |
| Dutasteride | 0.78 | 0.88 |
| Placebo | 0.19 | -0.30 |
The Macrophotographic hair count method marks a 1-inch diameter circular area at the anterior leading edge of the vertex thinning area and then photographed. The photographs are enlarged and converted into dot maps and the dot maps are converted into total hair counts by means of personal computer-based scanners and imaging software. (NCT00441116)
Timeframe: Baseline and Month 3
| Intervention | hair count per centimeters squared (Mean) | ||
|---|---|---|---|
| Baseline | Month 3 | Change from Baseline - Month 3 | |
| Dutasteride | 148.14 | 160.19 | 7.58 |
| Placebo | 144.27 | 154.50 | 10.24 |
Time to disease progression (PD) is defined as the interval of time between the date of the start of treatment and the date of PD. PD is defined as prostate specific antigen (PSA) progression from Baseline (PSA value is 25% and at least 2 nanograms per milliliter [ng/mL] above Baseline, confirmed by a second PSA value); PSA progression from nadir, without a 50% decrease from Baseline (PSA value is 25% and at least 2 ng/mL above nadir, confirmed by a second PSA value); PSA progression from nadir, with a 50% or more decrease from Baseline (PSA value is 50% and at least 2 ng/mL above nadir, confirmed by a second PSA value); metastatic disease (radiographic evidence of metastatic disease); death due to prostate cancer; or the receipt of post-Baseline rescue medication. PSA confirmation was not required if no subsequent PSA values were available. Participants who did not experience an event were censored at the date of the latest follow-up information. (NCT00470834)
Timeframe: Interval of time between the date of the start of treatment and the date of disease progression (up to Study Month 42)
| Intervention | Days (Mean) |
|---|---|
| Bicalutamide 50 mg/Placebo | 376.9 |
| Bicalutamide 50 mg/Dutasteride 3.5 mg | 433.1 |
Time to treatment failure is defined as the interval of time between the date of the start of treatment and the date of treatment failure. Treatment failure is defined as PSA progression from Baseline (PSA value is 25% and at least 2 ng/mL above Baseline, confirmed by a second PSA value); metastatic disease (radiographic evidence of metastatic disease); death due to prostate cancer; or receipt of post-baseline rescue medications. PSA confirmation was not required if no subsequent PSA values were available. Participants who did not experience an event were censored at the date of the latest follow-up information. (NCT00470834)
Timeframe: Interval of time between the date of the start of treatment and the date of treatment failure (up to Study Month 42)
| Intervention | Days (Mean) |
|---|---|
| Bicalutamide 50 mg/Placebo | 368.4 |
| Bicalutamide 50 mg/Dutasteride 3.5 mg | 457.5 |
Metastatic disease is that evidenced by a radiographic assessment. The time of metastatic disease was the date of radiographic evidence. (NCT00470834)
Timeframe: Interval of time between the date of the start of treatment and the date of radiographic evidence of metastatic disease (up to Study Month 42)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Months 1-18, n=65, 62 | Months 19-42, n=26, 30 | Overall (Months 1-42), n=65, 62 | |
| Bicalutamide 50 mg/Dutasteride 3.5 mg | 5 | 1 | 6 |
| Bicalutamide 50 mg/Placebo | 8 | 1 | 9 |
PSA response is defined as a 50% or greater decrease in PSA from Baseline, confirmed by a second PSA measurement. The time of this response was the date of the first PSA measurement that showed a 50% or greater decrease from the Baseline PSA measurement. PSA confirmation was not required if no subsequent PSA values were available. (NCT00470834)
Timeframe: Time from Baseline PSA measurement until the first PSA measurement with a 50% or greater reduction in PSA values (up to Study Month 42)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Months 1-18, n=65, 62 | Months 19-42, n=4, 7 | Overall (Months 1-42), n=65, 62 | |
| Bicalutamide 50 mg/Dutasteride 3.5 mg | 38 | 0 | 38 |
| Bicalutamide 50 mg/Placebo | 37 | 0 | 37 |
Change from Baseline in total PSA was measured at each scheduled post-baseline visit using a general linear model with effects for treatment and Baseline total PSA. Analysis was done using the last observation carried forward (LOCF) approach, in which missing post-Baseline values were imputed with earlier non-missing values. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT00470834)
Timeframe: Baseline and Months 6, 12, 18, 21, and 42
| Intervention | Nanograms per milliliter (ng/mL) (Median) | ||||
|---|---|---|---|---|---|
| Month 6, n=62, 61 | Month 12, n=62, 61 | Month 18, n=62, 61 | Month 21, n=26, 30 | Month 42, n=26, 30 | |
| Bicalutamide 50 mg/Dutasteride 3.5 mg | -2.2 | -2.1 | -1.7 | -1.8 | 0.6 |
| Bicalutamide 50 mg/Placebo | -2.0 | -1.7 | -1.2 | -2.1 | -0.1 |
(NCT00490555)
Timeframe: 10 weeks
| Intervention | ng/mL (Median) |
|---|---|
| 1) Placebo | 0.9 |
| 2) Testosterone Gel | 0.9 |
| 3) T Gel +Dutasteride | 1.8 |
| 4) T Gel+ DMPA | 0.7 |
(NCT00490555)
Timeframe: 10 weeks
| Intervention | ng/mL (Median) |
|---|---|
| 1) Placebo | 4.3 |
| 2) Testosterone Gel | 3.5 |
| 3) T Gel +Dutasteride | 3.8 |
| 4) T Gel+ DMPA | 3.2 |
(NCT00490555)
Timeframe: 10 weeks
| Intervention | ng/mL (Median) |
|---|---|
| 1) Placebo | 0.5 |
| 2) Testosterone Gel | 1.8 |
| 3) T Gel +Dutasteride | 0.5 |
| 4) T Gel+ DMPA | 0.6 |
(NCT00490555)
Timeframe: 10 weeks
| Intervention | ng/mL (Median) |
|---|---|
| 1) Placebo | 4.0 |
| 2) Testosterone Gel | 4.4 |
| 3) T Gel +Dutasteride | 7.0 |
| 4) T Gel+ DMPA | 1.8 |
PSA level week 10 end of treatment (NCT00490555)
Timeframe: 10 weeks
| Intervention | ng/mL (Median) |
|---|---|
| 1) Placebo | 0.8 |
| 2) Testosterone Gel | 0.9 |
| 3) T Gel +Dutasteride | 0.7 |
| 4) T Gel+ DMPA | 0.4 |
Percent change from baseline was calculated as the prostate volume at Month 3 minus the volume at baseline, divided by the prostate volume at baseline and multiplied by 100. Prostate volume was measured by transrectal ultrasound. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | percent change in volume (Mean) |
|---|---|
| Dutasteride 0.5 mg | -12.02 |
| Placebo | -1.02 |
Percent change from baseline was calculated as the prostate volume at Month 6 minus the volume at baseline, divided by the prostate volume at baseline and multiplied by 100. Prostate volume was measured by transrectal ultrasound. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | percent change in volume (Mean) |
|---|---|
| Dutasteride 0.5 mg | -17.00 |
| Placebo | -2.77 |
Percent change from baseline was calculated as the DHT at Month 3 minus the value at baseline, divided by the baseline value and multiplied by 100. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | -59.15 |
| Placebo | 28.33 |
Percent change from baseline was calculated as serum DHT at month 6 minus the value at baseline ,divided by the baseline value and multiplied by 100. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | -52.53 |
| Placebo | 26.78 |
Change from baseline was calculated as Qmax at Month 3 minus Qmax at baseline. Qmax is the peak urinary flow measured by a uroflow meter. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | ml/s (Mean) |
|---|---|
| Dutasteride 0.5 mg | 0.93 |
| Placebo | 0.17 |
Change from baseline was calculated as Qmax at Month 6 minus Qmax at baseline. Qmax is the peak urinary flow measured by a uroflow meter. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | milliliters/second (ml/s) (Mean) |
|---|---|
| Dutasteride 0.5 mg | 0.75 |
| Placebo | 0.03 |
Change from baseline was calculated as the AUA-SI score at month 3 minus the baseline score. AUA-SI is a self-administered questionnaire that assesses the severity of benign prostate hyperplasia symptoms. Scores range from 0 to 35; mild, 0-7; moderate, 8-19; severe, 20-35. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | points on a scale (Mean) |
|---|---|
| Dutasteride 0.5 mg | -2.9 |
| Placebo | -2.4 |
Change from baseline was calculated as the AUS-SI score at month 6 minus the baseline score. AUA-SI is a self-administered questionnaire that assesses the severity of benign prostatic hyperplasia symptoms. Scores range from 0 to 35; mild, 0-7; moderate, 8-19; severe, 20-35. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | points on a scale (Mean) |
|---|---|
| Dutasteride 0.5 mg | -4.9 |
| Placebo | -4.1 |
Change from baseline was calculated as the prostate volume at Month 3 minus the volume at baseline. Prostate volume is measured by transrectal ultrasound. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | cubic centimeters (Mean) |
|---|---|
| Dutasteride 0.5 mg | -7.11 |
| Placebo | -1.06 |
Change from baseline was calculated as the prostate volume at Month 6 minus the volume at baseline. Prostate volume was measured by transrectal ultrasound. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | cubic centimeters (Mean) |
|---|---|
| Dutasteride 0.5 mg | -9.16 |
| Placebo | -1.20 |
Change from baseline was calculated as the value of DHT at Month 3 minus the baseline value. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | pg/ml (Mean) |
|---|---|
| Dutasteride 0.5 mg | -319.605 |
| Placebo | -34.400 |
Change from baseline was calculated as the value of DHT at Month 6 minus the baseline value. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | picograms/milliliter (pg/ml) (Mean) |
|---|---|
| Dutasteride 0.5 mg | -289.175 |
| Placebo | -46.099 |
Percent change from baseline was calculated as Qmax at Month 6 minus Qmax at baseline, divided by baseline Qmax and multiplied by 100. Qmax is the peak urinary flow measured by a uroflow meter. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | 16.14 |
| Placebo | 6.31 |
Percent change from baseline was calculated as Qmax at Month 3 minus Qmax at baseline, divided by baseline Qmax and multiplied by 100. Qmax is the peak urinary flow measured by a uroflow meter. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | 14.34 |
| Placebo | 5.85 |
Percent change from baseline is calculated as the AUA-SI score at month 6 minus the baseline AUA-SI score, divided by the baseline score and multiplied by 100. AUA-SI is a self-administered questionnaire that assesses the severity of benign prostatic hyperplasia symptoms. Scores range from 0 to 35; mild, 0-7; moderate, 8-19; severe, 20-35. (NCT00527605)
Timeframe: Baseline and Month 6
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | -26.48 |
| Placebo | -20.79 |
Percent change from baseline is calculated as the AUA-SI score at month 3 minus the baseline AUA-SI score, divided by the baseline score and multiplied by 100. AUA-SI is a self-administered questionnaire that assesses the severity of benign prostatic hyperplasia symptoms. Scores range from 0 to 35; mild, 0-7; moderate, 8-19; severe, 20-35. (NCT00527605)
Timeframe: Baseline and Month 3
| Intervention | percent change (Mean) |
|---|---|
| Dutasteride 0.5 mg | -15.64 |
| Placebo | -11.91 |
A participant was designated as having PSA progression if there existed a post-baseline PSA value (within treatment period, typically up to 24-month evaluations) that was >10 ng/ml if radical prostatectomy or >20 ng/ml if primary radiotherapy and PSA >=1.5 times the baseline PSA value, or 0
Timeframe: up to 28 months
| Intervention | days (Median) |
|---|---|
| Placebo | 368.0 |
| Dutasteride 0.5 mg | 368.0 |
A participant was designated as having a PSA progression if there existed a post-baseline PSA value (within treatment period, typically up to 24-month evaluations) that was (>10 ng/ml if radical prostatectomy or >20 ng/ml if primary radiotherapy) and PSA >=1.5 times the baseline PSA value), or 0
Timeframe: up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| With PSA progression | Without PSA progression | |
| Dutasteride 0.5 mg | 19 | 127 |
| Placebo | 25 | 119 |
Participants underwent a digital rectal examination to evaluate for focal abnormality of the prostate. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) |
|---|---|
| Placebo | 10 |
| Dutasteride 0.5 mg | 8 |
Participants with improvement included those whose PSADT at a specified visit was positive but more than the baseline PSADT, whose PSA at the visit was the same as the baseline PSA, or whose PSA at the visit was less than the baseline PSA. Participants with worsening included those whose PSADT at the visit was positive but less than the baseline PSADT. (NCT00558363)
Timeframe: Baseline; Month 12, Month 24, End-of-Treatment (up to 28 months)
| Intervention | participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Month 12, Worsening; n=110, 123 | Month 12, No change; n=110, 123 | Month 12, Improvement; n=110, 123 | Month 24, Worsening; n=76, 110 | Month 24, No change; n=76, 110 | Month 24, Improvement; n=76, 110 | End-of treatment, Worsening; n=144, 144 | End-of treatment, No change; n=144, 144 | End-of treatment, Improvement; n=144, 144 | |
| Dutasteride 0.5 mg | 7 | 0 | 116 | 3 | 0 | 107 | 19 | 0 | 125 |
| Placebo | 20 | 0 | 90 | 7 | 0 | 69 | 37 | 0 | 107 |
Threshold vital signs are defined as follows: < 80 mmHg or > 165 mmHg for systolic blood pressure; < 40 mmHg or > 105 mm Hg for diastolic blood pressure, < 40 beats per minute (bpm) or > 100 bpm for heart rate. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| Baseline | Any time post-baseline | |
| Dutasteride 0.5 mg | 15 | 36 |
| Placebo | 18 | 37 |
Percent change from nadir PSA at Month X = 100*(Month X PSA - nadir PSA)/Nadir PSA. Nadir PSA was reported by the site as the lowest historical PSA value after the radical therapy. A nadir value below the detection level was captured as 0.0. The missing PSA value for scheduled visits could have been replaced by non-missing PSA values within 30 days after the clinic visit date. If such replacement was not possible, the latest non-missing post-baseline PSA before the scheduled visit was used for the scheduled visit PSA (Last Observation Carried Forward). (NCT00558363)
Timeframe: Baseline; Months 12 and 24
| Intervention | percent change (Mean) | |
|---|---|---|
| Month 12 | Month 24 | |
| Dutasteride 0.5 mg | 2120.7 | 2927.2 |
| Placebo | 2810.3 | 4036.1 |
Percent change in PSA from baseline at Month X = 100*(Month X PSA - Baseline PSA)/Baseline PSA. The missing PSA value for scheduled visits could have been replaced by non-missing PSA values within 30 days after the clinic visit date. If such replacement was not possible, the latest non-missing post-baseline PSA before the scheduled visit was used for the scheduled visit PSA (Last Observation Carried Forward). (NCT00558363)
Timeframe: Baseline; Months 12 and 24
| Intervention | percent change (Mean) | |
|---|---|---|
| Month 12 | Month 24 | |
| Dutasteride 0.5 mg | 11.8 | 86.2 |
| Placebo | 93.1 | 197.3 |
A participant has a normal value for a laboratory parameter if the value is within the low and high range of normal provided by the laboratory. Each laboratory parameter is evaluated for shift from normal at baseline to abnormal any time post-baseline. A participant with any laboratory parameter showing this shift is counted. A participant is counted only once even if he had such a shift in more than one laboratory parameter or more than once among all post-baseline evaluations. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) |
|---|---|
| Placebo | 74 |
| Dutasteride 0.5 mg | 64 |
Time to disease progression is defined as the number of days between baseline and the first occurrence of any of the following: PSA doubling time (PSADT)<=91 days, PSA value is at least 50% more than baseline value (>20 nanogram/milliliter [ng/ml] for primary radiotherapy group or >10 ng/ml for radical prostatectomy group), rescue treatment, cancer-positive biopsy, cancer-positive bone scan. (Confirmation of PSA criteria is required in an immediate subsequent PSA, if available, and PSA values for consideration are restricted to treatment period, typically up to 24-month evaluations.) (NCT00558363)
Timeframe: up to 28 months
| Intervention | days (Median) |
|---|---|
| Placebo | 365.0 |
| Dutasteride 0.5 mg | 285.0 |
A participant was designated as having a PSA rise if there existed a post-baseline PSA value (within treatment period, typically up to 24-month evaluations) that was >1.15 times the baseline PSA value, and all subsequent PSA values were >1.15 times the baseline PSA value. The study day for the first PSA evaluation that qualified for analysis of PSA rise was used for time to PSA rise. If none of the post-baseline PSA values qualified for analysis of PSA rise during the study, time to PSA rise was censored at the last post-baseline PSA evaluation. (NCT00558363)
Timeframe: up to 28 months
| Intervention | days (Median) |
|---|---|
| Placebo | 100.0 |
| Dutasteride 0.5 mg | 279.0 |
Change from nadir PSA at Month X = Month X PSA - nadir PSA. Nadir PSA was reported by the site as the lowest historical PSA value after the radical therapy. A nadir value below the detection level was captured as 0.0. The missing PSA value for scheduled visits could have been replaced by non-missing PSA values within 30 days after the clinic visit date. If such replacement was not possible, the latest non-missing post-baseline PSA before the scheduled visit was used for the scheduled visit PSA (Last Observation Carried Forward). (NCT00558363)
Timeframe: Baseline; Months 12 and 24
| Intervention | ng/ml (Mean) | |
|---|---|---|
| Month 12 | Month 24 | |
| Dutasteride 0.5 mg | 3.5 | 4.9 |
| Placebo | 4.7 | 6.3 |
Change in PSA from baseline at Month X = Month X PSA - Baseline PSA. The missing PSA value for scheduled visits could have been replaced by non-missing PSA values within 30 days after the clinic visit date. If such replacement was not possible, the latest non-missing post-baseline PSA before the scheduled visit was used for the scheduled visit PSA (Last Observation Carried Forward). (NCT00558363)
Timeframe: Baseline; Months 12 and 24
| Intervention | nanograms/milliliter (ng/ml) (Mean) | |
|---|---|---|
| Month 12 | Month 24 | |
| Dutasteride 0.5 mg | 0.9 | 2.3 |
| Placebo | 2.3 | 3.9 |
MAX-PC is an 18-item, self-reported measure that evaluates prostate cancer-related anxiety. The score ranges from 0 to 54, and an increase in the score indicates a worsened anxiety level. Change from Baseline at Month X = Month X MAX-PC score - Baseline MAX-PC score. A missing post-baseline value is replaced by the last available post-baseline value (Last Observation Carried Forward(LOCF)). A general linear model controls for previous therapy, site cluster, and baseline MAX-PC score. (NCT00558363)
Timeframe: Baseline; Months 3, 6, 12, 18, and 24
| Intervention | scores on a scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 3, n=144, 141 | Month 6, n=144, 143 | Month 12, n=144, 143 | Month 18, n=144, 143 | Month 24, n=144, 143 | |
| Dutasteride 0.5 mg | -1.4 | -3.1 | -2.9 | -2.2 | -1.4 |
| Placebo | -1.6 | -2.2 | -0.8 | -1.1 | -0.4 |
Treatment responders at Month X were defined as participants (par.) with either a PSA decrease or an increase <=15% from baseline to Month X confirmed in all PSA measurements between baseline (BL) and Month X. (NCT00558363)
Timeframe: Months 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 3, n=141, 141 | Month 6, n=131, 135 | Month 9, n=121, 129 | Month 12, n=110, 124 | Month 15, n=100, 121 | Month 18, n=95, 120 | Month 21, n=83, 112 | Month 24, n=76, 110 | |
| Dutasteride 0.5 mg | 117 | 105 | 95 | 87 | 82 | 76 | 70 | 62 |
| Placebo | 64 | 36 | 22 | 13 | 10 | 8 | 7 | 6 |
A participant was designated as having a PSA rise if there existed a post-baseline PSA value (within treatment period, typically up to 24-month evluations) that was >1.15 times the baseline PSA value, and all subsequent PSA values were >1.15 times the baseline PSA value. (NCT00558363)
Timeframe: up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| With PSA rise | Without PSA rise | |
| Dutasteride 0.5 mg | 72 | 74 |
| Placebo | 127 | 17 |
Threshold laboratory values are defined in terms of a multiplicative factor of the testing laboratory's normal range, pre-specified in the analysis plan. A laboratory value that is above the upper limit factor multiplied by the upper limit of the normal range is considered a high threshold value. A laboratory value that is below the lower limit factor multiplied by the lower limit of the normal range is considered a low threshold value. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| Threshold at BL | Non-threshold at BL; threshold at any time post-BL | |
| Dutasteride 0.5 mg | 9 | 5 |
| Placebo | 5 | 11 |
Disease progression is defined as the first occurrence of any of the following: PSADT<=91 days, PSA value is at least 50% more than baseline value (>20 ng/ml for primary radiotherapy group or >10 ng/ml for radical prostatectomy group), rescue treatment, cancer-positive biopsy, cancer-positive bone scan. If one of the PSA criteria is qualifying (within treatment period, typically up to 24-month evaluations), an immediate subsequent PSA, if available, must confirm either criterion (or at least 85% of the qualifying value). (NCT00558363)
Timeframe: up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| With disease progression | Without disease progression | |
| Dutasteride 0.5 mg | 25 | 121 |
| Placebo | 49 | 95 |
Participants underwent clinical examination of the breasts, to evaluate for nipple tenderness. Clinical significance of the results was determined by subjective judgment of the clinical personnel performing the examination. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| BL; NT, n=147, 147 | BL; Clinically significant (CS) NT, n=0, 3 | No NT at BL, but NT at any time post-BL, n=147,147 | CS change in NT; BL to any time post-BL, n=8, 11 | |
| Dutasteride 0.5 mg | 3 | 0 | 11 | 1 |
| Placebo | 0 | 0 | 8 | 0 |
Time to PSA doubling is defined as the number of days between the baseline date and the study day of the first post-baseline PSA evaluation date (within treatment period, typically up to 24-month evaluations) on which the PSA value was at least twice as much as the baseline PSA value, and the immediate subsequent value, if available, was at least 85% of two times the baseline value. Participants who never achieved PSA doubling were censored at the last post-baseline, non-missing PSA evaluation. (NCT00558363)
Timeframe: up to 28 months
| Intervention | days (Median) | |
|---|---|---|
| Participants (par.) with PSA doubling; n=82, 41 | Par. without PSA doubling (censored); n=62, 105 | |
| Dutasteride 0.5 mg | 458.0 | NA |
| Placebo | 365.5 | NA |
Participants underwent clinical examination of the breasts, to evaluate for palpable breast tissue. Clinical significance of the results was determined by subjective judgment of the clinical personnel performing the examination. (NCT00558363)
Timeframe: Baseline; up to 28 months
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| BL; PBT, n=147, 147 | BL; Clinically significant (CS) PBT, n=6, 4 | No BL PBT, but PBT at any time post-BL, n=147,147 | CS change in PBT; BL to any time post-BL, n=10, 21 | |
| Dutasteride 0.5 mg | 4 | 0 | 21 | 4 |
| Placebo | 6 | 0 | 10 | 0 |
PSA doubling is defined as the first post-baseline PSA value (within treatment period, typically up to 24-month evaluations) that was at least twice as much as the baseline PSA value and was confirmed as such (at least 85% of two times the baseline PSA value) in the immediate subsequent PSA value if one is available. (NCT00558363)
Timeframe: up to 28 months
| Intervention | participants (Number) | |
|---|---|---|
| With PSA doubling | Without PSA doubling | |
| Dutasteride 0.5 mg | 41 | 105 |
| Placebo | 82 | 62 |
PSA doubling is defined as the first post-baseline PSA value (within treatment period, typically up to 12-month evaluations) that was at least twice as much as the baseline PSA value and was confirmed as such (at least 85% of two times the baseline PSA value) in the immediate subsequent PSA value if one is available. (NCT00558363)
Timeframe: up to 16 months
| Intervention | participants (Number) | |
|---|---|---|
| With PSA doubling | Without PSA doubling | |
| Dutasteride 0.5 mg | 15 | 131 |
| Placebo | 50 | 94 |
Time to PSA doubling is defined as the number of days between the baseline date and the study day of the first post-baseline PSA evaluation date within Year 1 (Y1; within treatment period, typically up to 12-month evaluations) on which the PSA value was at least twice as much as the baseline PSA value, and the immediate subsequent value, if available, was at least 85% of two times the baseline value. (NCT00558363)
Timeframe: up to 16 months
| Intervention | days (Median) | |
|---|---|---|
| Participants with PSA doubling in Y1; n=50, 15 | Participants without PSA doubling in Y1: n=94, 131 | |
| Dutasteride 0.5 mg | 183.0 | NA |
| Placebo | 273.5 | NA |
"Calculation of number of months when baseline PSA doubles compared between the 2 arms at the end of off-treatment cycle 1." (NCT00668642)
Timeframe: At month 9 and ongoing monthly until end of off-cycle 1 defined by when the testosterone level reaches normal (approximately 6 months)
| Intervention | Months (Mean) |
|---|---|
| A: Dutasteride During First Off-Cycle | 1.42 |
| B: Placebo During First Off-Cycle | 1.56 |
"Calculation of the level of gene expression of the U19 tumor suppressor gene compared between the 2 arms at the end of off-treatment cycle 1." (NCT00668642)
Timeframe: At the end of off-cycle 1 defined by when the testosterone level reaches normal (approximately 6 months)
| Intervention | Relative expression (Mean) |
|---|---|
| A: Dutasteride During First Off-Cycle | 0.24 |
| B: Placebo During First Off-Cycle | 0.28 |
PSA decline of 50% from baseline confirmed by a PSA at least 4 weeks later. (NCT00673127)
Timeframe: From treatment initiation until treatment cessation. Maximum 32 months. Median treament duration 8 months.
| Intervention | percentage of participants (Number) |
|---|---|
| KHAD | 56 |
Duration of time from treatment initiation until documented progression (PSA or Disease progression) (NCT00673127)
Timeframe: Duration of time from treatment initiation until documented progression. Maximum 32 months
| Intervention | months (Median) |
|---|---|
| KHAD | 14.5 |
(NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | ng/dL (Mean) |
|---|---|
| Dutasteride - Baseline | 33.5 |
| Dutasteride - 1 Month | 5.2 |
| Dutasteride - 3 Months | 2.5 |
| Dutasteride - 6 Months | 2.5 |
Functional Alterations due to Changes in Elimination (FACE) is a 14-item questionnaire designed to evaluate the effects of changes in urinary and bowel elimination on daily functioning. It is scored out of 56, with higher scores reflecting poorer HRQL. (NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | units on a scale (Mean) |
|---|---|
| Dutasteride - Baseline | 4.6 |
| Dutasteride - 1 Month | 4.7 |
| Dutasteride - 3 Months | 5.0 |
| Dutasteride - 6 Months | 4.8 |
The Spitzer Quality of Life Index (SQLI) is a validated five-item questionnaire evaluating global HRQL. Activity, daily living, health, support of family and friends, and outlook are each rated on a 3-point scale (0 to 2), with total score ranging from 0-10, with lower score indicating poorer HRQL. (NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | units on a scale (Mean) |
|---|---|
| Dutasteride - Baseline | 9.7 |
| Dutasteride - 1 Month | 9.9 |
| Dutasteride - 3 Months | 9.6 |
| Dutasteride - 6 Months | 9.9 |
The International Index of Erectile Function (IIEF-5) is an abridged five-item version of the original IIEF 15-item questionnaire designed to evaluate erectile function, based on a definition arrived at by the National Institutes of Health Consensus Panel. Each of 5 questions about erectile function over the past 6 months is scored by the patient from 1 (severe dysfunction) to 5 (little or no dysfunction). The IIEF-5 is scored from 5 to 25, with lower scores indicating erectile dysfunction: 22-25 = No erectile dysfunction; 17-21 = Mild erectile dysfunction; 12-16 = Mild to moderate erectile dysfunction; 8-11 = Moderate erectile dysfunction; 5-7 = Severe erectile dysfunction (NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | units on a scale (Mean) |
|---|---|
| Dutasteride - Baseline | 16.4 |
| Dutasteride - 1 Month | 17.0 |
| Dutasteride - 3 Months | 16.0 |
| Dutasteride - 6 Months | 15.3 |
IPSS (The International Prostate Symptom Score) is a symptom index based on seven questions concerning urinary symptoms (1 Incomplete emptying, 2 Frequency, 3 Intermittency, 4 Urgency, 5 Weak Stream, 6 Straining, 7 Nocturia) for which the patient chooses one out of six answers indicating increasing severity of the particular symptom, ranging from 0 (Not at all) to 5(Almost always). The total score can therefore range from 0 to 35 (asymptomatic to very symptomatic). Mild (symptom score less than of equal to 7); Moderate (symptom score range 8-19); Severe (symptom score range 20-35). (NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | units on a scale (Mean) |
|---|---|
| Dutasteride - Baseline | 8.8 |
| Dutasteride - 1 Month | 6.6 |
| Dutasteride - 3 Months | 7.9 |
| Dutasteride - 6 Months | 5.9 |
(NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | ng/mL (Mean) |
|---|---|
| Dutasteride - Baseline | 5.44 |
| Dutasteride - 1 Month | 4.33 |
| Dutasteride - 3 Months | 2.85 |
| Dutasteride - 6 Months | 2.59 |
Proportion of voxels consistent with prostate cancer as measured by magnetic resonance spectroscopy imaging (MRSI). MRSI spectra were examined and scored as healthy or cancerous. The change in cancerous volumes over time was evaluated. Because a significant decrease in citrate and polyamines on MRSI spectra was noted at 1 month compared with baseline, healthy tissue appeared to be more like cancer and thus created a false impression that the cancer had grown after 1 month. To reduce this bias, primary comparisons were made between the 1-month and 6-month scans. (NCT00706966)
Timeframe: 1 month, 6 months
| Intervention | participants (Number) | ||
|---|---|---|---|
| 30-45% Decrease | No change (95 - 100%) | 65-167% Increase | |
| Dutasteride | 3 | 2 | 4 |
(NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | ng/dL (Mean) |
|---|---|
| Dutasteride - Baseline | 356.5 |
| Dutasteride - 1 Month | 418.4 |
| Dutasteride - 3 Months | 443.2 |
| Dutasteride - 6 Months | 484.3 |
Toxicities from Dutasteride were recorded at each study visit and assessed by NCI-CTCAE v3.0. (NCT00706966)
Timeframe: Baseline, 1, 3, and 6 months
| Intervention | adverse events (Number) |
|---|---|
| Dutasteride | 5 |
Biphasic Alcohol Effects Scale (BAES) Sedation items - sum of subjective responses - 0(not at all)to 10 (extremely)- for 7 sedation related questions regarding effects of alcohol. Total BAES sedation subscale score 0-70 with higher numbers indicating greater sedative effects of alcohol. [Martin, C. S., M. Earleywine, R. E. Musty, M. W. Perrine and R. M. Swift (1993a). Development and validation of the Biphasic Alcohol Effects Scale. Alcohol Clin Exp Res 17(1): 140-6.] (NCT00734656)
Timeframe: 40, 80, 120, 160, 210 and 240 minutes after start of drinking
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo Medication + Placebo Alcohol | 0.7 |
| Placebo Medication + 0.8 gr/kg Ethanol | 8.9 |
| 4 mg Dutasteride + Placebo Alcohol | 1.5 |
| 4 mg Dutasteride + 0.8 mg/kg Ethanol | 7.4 |
Biphasic Alcohol Effects Scale (BAES)Simulation items - sum of subjective responses - 0(not at all)to 10 (extremely)- for 7 stimulation related questions regarding effects of alcohol. Total BAES stimulation subscale score 0-70 with higher numbers indicating greater stimulating effects of alcohol. [Martin, C. S., M. Earleywine, R. E. Musty, M. W. Perrine and R. M. Swift (1993a). Development and validation of the Biphasic Alcohol Effects Scale. Alcohol Clin Exp Res 17(1): 140-6.] (NCT00734656)
Timeframe: 40, 80, 120, 160, 210 and 240 minutes after start of drinking
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo Medication + Placebo Alcohol | 0.7 |
| Placebo Medication + 0.8 gr/kg Ethanol | 4.2 |
| 4 mg Dutasteride + Placebo Alcohol | 1.7 |
| 4 mg Dutasteride + 0.8 mg/kg Ethanol | 4.8 |
Breath Alcohol level (NCT00734656)
Timeframe: 40 minutes after beginning drink
| Intervention | gr/dL (Mean) |
|---|---|
| Placebo Medication + Placebo Alcohol | 0.001 |
| Placebo Medication + 0.8 gr/kg Ethanol | 0.075 |
| 4 mg Dutasteride + Placebo Alcohol | 0.001 |
| 4 mg Dutasteride + 0.8 mg/kg Ethanol | 0.071 |
Ratio of serum 3a-androstanediol drawn prior to alcohol administration (2-4 days after medication administration) compared to the baseline level prior to medication dose. The pharmacologic effect of dutasteride was measured by assay of serum 5a-androstan-3a,17b-diol,17-glucuronide (aka 3a-androstanediol glucuronide) as a biochemical measure of 5a-reductase enzyme inhibition. 3a-androstanediol glucuronide is the primary metabolic excretion product of 3a,5a-androstane neuroactive steroids. The (NCT00734656)
Timeframe: Baseline (pre medication administration) and 2-4 days post-medication (alcohol session)
| Intervention | ratio (Mean) |
|---|---|
| Placebo Medication + Placebo Alcohol | 1.04 |
| Placebo Medication + 0.8 gr/kg Ethanol | 1.11 |
| 4 mg Dutasteride + Placebo Alcohol | 0.31 |
| 4 mg Dutasteride + 0.8 mg/kg Ethanol | 0.31 |
To evaluate the safety of dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with symptoms of LUTS: post-voiding residual volume measured via ultrasound. (NCT00939120)
Timeframe: 12 months
| Intervention | mL (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 101.7 |
| Placebo + Dutasteride 0.5mg | 75.8 |
To evaluate the efficacy in men taking dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with LUTS including OAB symptoms: participant reported patient perception of bladder condition (PPBC), one question scored from 1-6, higher scores indicating more severe symptoms. (NCT00939120)
Timeframe: 12 months
| Intervention | units on a scale (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 3.6 |
| Placebo + Dutasteride 0.5mg | 3.0 |
To evaluate the efficacy in men taking dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with LUTS including OAB symptoms: overactive bladder questionnaire (OABq) - 33 questions scored via 1-6 (higher scores indicate more severe symptoms), thus values ranged from 33-198. (NCT00939120)
Timeframe: 12 months
| Intervention | units on a scale (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 80.2 |
| Placebo + Dutasteride 0.5mg | 67.7 |
To evaluate the efficacy in men taking dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with LUTS including OAB symptoms: voiding subscore of international prostate symptoms score (IPSS) - 4 questions scored from 0-5 (higher score indicating more severe symptoms), thus total scores ranged from 0-20. (NCT00939120)
Timeframe: 12 months
| Intervention | units on a scale (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 7.5 |
| Placebo + Dutasteride 0.5mg | 7.0 |
To evaluate the efficacy in men taking dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with LUTS including OAB symptoms: total international prostate symptoms score (IPSS) - 7 questions scored from 0-5 (higher score indicating more severe symptoms), thus total scores ranged from 0-35. (NCT00939120)
Timeframe: 12 months
| Intervention | units on a scale (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 15.4 |
| Placebo + Dutasteride 0.5mg | 14.5 |
To evaluate the efficacy in men taking dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with LUTS including OAB symptoms: storage subscore international prostate symptoms score (IPSS) - 3 questions scored from 0-5 (higher score indicating more severe symptoms), thus total scores ranged from 0-15. (NCT00939120)
Timeframe: 12 months
| Intervention | units on a scale (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 7.9 |
| Placebo + Dutasteride 0.5mg | 7.5 |
To evaluate the safety of dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with symptoms of LUTS: acute urinary attention (AUR) - inability to urinate requiring catheterization. (NCT00939120)
Timeframe: 12 months
| Intervention | participants (Number) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 0 |
| Placebo + Dutasteride 0.5mg | 0 |
To evaluate the safety of dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with symptoms of LUTS: maximum urine flow rate (Qmax) measured via uroflowmetry. (NCT00939120)
Timeframe: 12 months
| Intervention | mL/sec (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 11.7 |
| Placebo + Dutasteride 0.5mg | 12.9 |
To evaluate the safety of dutasteride 0.5 mg in combination with either tolterodine ER 4mg or placebo for the treatment of men with symptoms of LUTS: urine voided volume (voiding) measured by uroflowmetry. (NCT00939120)
Timeframe: 12 months
| Intervention | mL (Mean) |
|---|---|
| Tolterodine ER 4mg + Dutasteride 0.5mg | 219.9 |
| Placebo + Dutasteride 0.5mg | 232.9 |
"A DLT is defined as an adverse event (AE) occurring during the first cycle of KHLAD treatment that are determined to related to the Lapatinib or the combination as follows:~Any Grade 3 or greater non-hematological treatment related (possible, probable, or definite attribution) including diarrhea~Grade 4 or greater for hematological toxicities, regardless of attribution.~Grade 3 skin reactions, pulmonary reactions, regardless of attribution." (NCT00953576)
Timeframe: The evaluation for DLT occurred continuously through one cycle of treatment (28 days).
| Intervention | participants with DLT (Number) |
|---|---|
| Phase I Dose Level 1: KHAD+L (250 mg) | 0 |
| Phase I Dose Level 2: KHAD+L (500 mg) | 2 |
All grade 3-4 adverse events (AE) with treatment attribution of possibly, probably or definite based on CTCAEv4 as reported on case report forms were counted to calculate the proportion of participants experiencing at least one treatment-related grade 3 or 4 AE of any type on treatment. (NCT00953576)
Timeframe: Assessed each cycle throughout treatment. Treatment duration in months was a median (range) of 5.4 months (range 1 day-8.3 months). Thus, AEs were evaluated up to 8.3 months.
| Intervention | proportion of participants (Number) |
|---|---|
| Phase I Dose Level 1: KHAD+L (250 mg) | 0 |
| Phase I Dose Level 2: KHAD+L (500 mg) | 0.40 |
The MTD of lapatinib in combination with KHAD is determined by the number of participants who experience a dose limiting toxicity (DLT) at the various dose levels of lapatinib under evaluation. See subsequent primary outcome measure for the DLT definition. The MTD is defined as the lapatinib dose at which fewer than one-third of patients experience a DLT. If no DLTs are observed, the MTD is not reached and the Recommended Phase II Dose (RP2D) will be based on safety and pharmacokinetic results. (NCT00953576)
Timeframe: The evaluation for MTD occurred continuously through one cycle of KHLAD treatment (28 days).
| Intervention | mg 1x daily (Number) |
|---|---|
| All Phase I Participants KHAD+L | NA |
Plasma lapatinib levels were measured after day 28 of KHLAD treatment. Participants were instructed to fast prior to samples being taken. (NCT00953576)
Timeframe: After first 28 days of KHLAD treatment
| Intervention | ng/mL (Mean) |
|---|---|
| Phase I Dose Level 1: KHAD+L (250 mg) | 731 |
| Phase I Dose Level 2: KHAD+L (500 mg) | 1506 |
(NCT01215292)
Timeframe: 10 days
| Intervention | ng/mL (Median) |
|---|---|
| Acyline + Testosterone Gel + Placebo | 14 |
| Acyline + Tgel + Ketoconazole 400mg | 3.7 |
| Acyline + Tgel + Ketoconazole 800mg | 1.7 |
| Acyline & TGel & Dutasteride 2.5mg | 18.4 |
| Acyline & TGel & Anastrazole 1mg | 24.0 |
(NCT01215292)
Timeframe: 10 days
| Intervention | ng/mL (Median) |
|---|---|
| Acyline + Testosterone Gel (Tgel)+ Placebo | 3.17 |
| Acyline & TGel & Ketoconazole 400 mg | 2.08 |
| Acyline & TGel & Ketoconazole 800 mg | 1.46 |
| Acyline & TGel & Dutasteride | 0.12 |
| Acyline & TGel & Anastrazole | 3.63 |
(NCT01215292)
Timeframe: 10 days
| Intervention | ng/mL (Median) |
|---|---|
| Acyline + Testosterone Gel (Tgel)+ Placebo | .87 |
| Acyline + Tgel + Ketoconazole 400mg | 0.5 |
| Acyline + Tgel + Ketoconazole 800mg | 0.12 |
| Acyline & TGel & Dutasteride 2.5mg | 1.7 |
| Acyline & TGel & Anastrazole 1mg | 3.6 |
"Participant-perceived change in HG was assessed by 3 questions (each scored on a 7-point scale) on a health outcome questionnaire: Since the start of treatment, when I look at my thinning area, I can see..., Since the start of treatment, my hair now covers…, and Since the start of treatment, the appearance (thickness/quality/amount) of the thinning area on my head is… -3, Much less; -2, Moderately less; -1, Slightly less; 0, The same amount; 1, Slightly more; 2, Moderately more; 3, Much more scalp. The scores for the 3 questions were summed to obtain the HGI total score (-9 to 9)." (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 12, n=171, 171, 172, 166, 160 | Week 24, n=172, 174, 177, 167, 165 | |
| Dutasteride 0.02 mg | 0.9 | 1.1 |
| Dutasteride 0.1 mg | 1.7 | 2.8 |
| Dutasteride 0.5 mg | 2.0 | 3.2 |
| Finasteride 1 mg | 1.7 | 2.5 |
| Placebo | 1.2 | 1.1 |
The IPAQ was completed by the Investigator or designee by comparing the global photographs obtained at Baseline with those obtained at Week 12. This assessment was made separately based on the global photography of the vertex and frontal views. The change from Baseline in hair growth was assessed using the following 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. (NCT01231607)
Timeframe: Baseline and Week 12
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Vertex view | Frontal view | |
| Dutasteride 0.02 mg | 0.35 | 0.33 |
| Dutasteride 0.1 mg | 0.62 | 0.54 |
| Dutasteride 0.5 mg | 0.78 | 0.55 |
| Finasteride 1 mg | 0.70 | 0.55 |
| Placebo | 0.48 | 0.30 |
The IPAQ was completed by the Investigator or designee by comparing the global photographs obtained at Baseline with those obtained at Week 12. This assessment was made separately based on the global photography of the vertex and frontal views. The change from Baseline in hair growth was assessed using the following 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. (NCT01231607)
Timeframe: Baseline and Week 24
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Vertex view | Frontal view | |
| Dutasteride 0.02 mg | 0.37 | 0.28 |
| Dutasteride 0.1 mg | 1.03 | 0.78 |
| Dutasteride 0.5 mg | 1.30 | 1.11 |
| Finasteride 1 mg | 1.07 | 0.88 |
| Placebo | 0.36 | 0.30 |
The target area hair width was the sum of all nonvellus hairs (>=30 µm in width; thick and noticeable hair) within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). For the MT, hair was clipped before each photograph. A cosmetic ink dot was placed by tattoo at Baseline so that the same area could be identified at Baseline and post-Baseline. If the ink dot faded, it was re-done in exactly the same location to ensure it was visible for subsequent photographs. Change from Baseline was calculated as the Week 12 or Week 24 value minus the Baseline value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | millimeters (Least Squares Mean) | |
|---|---|---|
| Week 12, n=152, 154, 155, 149, 134 | Week 24, n=152, 158, 159, 152, 142 | |
| Dutasteride 0.02 mg | 0.1 | 0.1 |
| Dutasteride 0.1 mg | 0.7 | 0.8 |
| Dutasteride 0.5 mg | 0.9 | 1.2 |
| Finasteride 1 mg | 0.6 | 0.8 |
| Placebo | -0.1 | -0.2 |
The target area hair width was the sum of all nonvellus hairs (>=30 µm in width; thick and noticeable hair) within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). For the MT, hair was clipped before each photograph. A cosmetic ink dot was placed by tattoo at Baseline so that the same area could be identified at Baseline and post-Baseline. If the ink dot faded, it was re-done in exactly the same location to ensure it was visible for subsequent photographs. Change from Baseline was calculated as the Week 12 or Week 24 value minus the Baseline value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | millimeters (Least Squares Mean) | |
|---|---|---|
| Week 12, n=147, 144, 151, 145, 131 | Week 24, n=148, 155, 158, 150, 141 | |
| Dutasteride 0.02 mg | 0.3 | -0.0 |
| Dutasteride 0.1 mg | 3.1 | 3.9 |
| Dutasteride 0.5 mg | 4.7 | 5.8 |
| Finasteride 1 mg | 3.2 | 4.0 |
| Placebo | -0.7 | -0.9 |
The THC (thick, long, and dark hair) was the sum of all nonvellus hairs (>=60 μm in width; thick and noticeable hair) within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on the hair follicles in the photographs. Change from BL=Week 12/Week 24 value minus BL value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | Hair count (Least Squares Mean) | |
|---|---|---|
| Week 12, n=147, 144, 151, 145, 131 | Week 24, n=148, 155, 158, 150, 141 | |
| Dutasteride 0.02 mg | -13.4 | -15.7 |
| Dutasteride 0.1 mg | 18.3 | 29.4 |
| Dutasteride 0.5 mg | 29.3 | 46 |
| Finasteride 1 mg | 24.2 | 36.3 |
| Placebo | -11.5 | -17.5 |
The THC (thick, long, and dark hair) was the sum of all nonvellus hairs (>=60 μm in width; thick and noticeable hair) within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12/Week 24 value minus BL value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | Hair count (Least Squares Mean) | |
|---|---|---|
| Week 12, n=152, 154, 155, 149, 134 | Week 24, n=152, 158, 159, 152, 142 | |
| Dutasteride 0.02 mg | -2.7 | -2.8 |
| Dutasteride 0.1 mg | 4.0 | 6.0 |
| Dutasteride 0.5 mg | 5.9 | 9.3 |
| Finasteride 1 mg | 4.5 | 7.2 |
| Placebo | -1.1 | -3.0 |
Participant satisfaction with hair appearance/growth was assessed by 5 questions (each scored on a 7-point scale: How satisfied do you feel about: [1] The overall appearance of your hair; [2] The appearance of the thinning area[s] [TAs] on your head; [3] The amount of scalp that can be seen in the TAs; [4] The amount of hair in the TAs; [5] The growth of hair in the TAs): -3, Very dissatisfied (DS); -2, DS; -1, Somewhat DS; 0, Neutral (neither satisfied nor DS); 1, Somewhat satisfied (SA); 2, SA; 3, Very SA. The scores for the 5 questions were summed to obtain the HGSS total score (-15 to 15). (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Week 12, n=171, 174, 173, 170, 160 | Week 24, n=172, 176, 177, 170, 165 | |
| Dutasteride 0.02 mg | 7.9 | 8.3 |
| Dutasteride 0.1 mg | 9.8 | 11.5 |
| Dutasteride 0.5 mg | 8.4 | 12.5 |
| Finasteride 1 mg | 8.5 | 10.8 |
| Placebo | 8.5 | 9.3 |
A central panel of 3 dermatologists independently assessed change in hair growth from Baseline to Week 24 using a 7-point scale: greatly decreased (-3), moderately decreased (-2), slightly decreased (-1), no change (0), slightly increased (1), moderately increased (2), and greatly increased (3). The median score, across the 3 panel members, is summarized. This assessment was performed by comparing the global photographs obtained at Baseline with those subsequently obtained at Week 24. This assessment was made separately based on the global photography of the vertex and frontal views. (NCT01231607)
Timeframe: Baseline and Week 24
| Intervention | scores on a scale (Least Squares Mean) | |
|---|---|---|
| Vertex view, n=172, 174, 176, 167, 164 | Frontal/Superior view, n=171, 174, 176, 167, 165 | |
| Dutasteride 0.02 mg | -0.09 | -0.10 |
| Dutasteride 0.1 mg | 0.42 | 0.36 |
| Dutasteride 0.5 mg | 0.63 | 0.58 |
| Finasteride 1 mg | 0.49 | 0.34 |
| Placebo | -0.15 | -0.14 |
"The investigator/designee assessed the stage (Stage I to Stage VII) of AGA (i.e., male pattern baldness [MPB]) by utilizing the Norwood-Hamilton scale, used to measure the progression of MPB. Stage VII indicates worse balding than stage I. Assessment was made by direct visual examination (aided by pictures) of the participant at Baseline and Week 12 (W12). v, vertex; most of the hair loss (commonly seen with advancing age) is on the vertex. a, type a variant; major features are (1) the entire anterior hairline border recedes in unison; (2) there is no simultaneous balding of the vertex." (NCT01231607)
Timeframe: Baseline and Week 12
| Intervention | participants (Number) | |||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BL S IIIv to W12 S II, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S IIa, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S III, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S IIIa, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S IIIv, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S IV, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S IVa, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S V, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S Va, n=79, 70, 69, 72, 73 | BL S IIIv to W12 S VI, n=79, 70, 69, 72, 73 | BL S IV to W12 S II, n=52, 59, 58, 56, 53 | BL S IV to W12 S IIa, n=52, 59, 58, 56, 53 | BL S IV to W12 S III, n=52, 59, 58, 56, 53 | BL S IV to W12 S IIIa, n=52, 59, 58, 56, 53 | BL S IV to W12 S IIIv, n=52, 59, 58, 56, 53 | BL S IV to W12 S IV, n=52, 59, 58, 56, 53 | BL S IV to W12 S IVa, n=52, 59, 58, 56, 53 | BL S IV to W12 S V, n=52, 59, 58, 56, 53 | BL S IV to W12 S Va, n=52, 59, 58, 56, 53 | BL S IV to W12 S VI, n=52, 59, 58, 56, 53 | BL S V to W12 S II, n=41, 46, 46, 41, 35 | BL S V to W12 S IIa, n=41, 46, 46, 41, 35 | BL S V to W12 S III, n=41, 46, 46, 41, 35 | BL S V to W12 S IIIa, n=41, 46, 46, 41, 35 | BL S V to W12 S IIIv, n=41, 46, 46, 41, 35 | BL S V to W12 S IV, n=41, 46, 46, 41, 35 | BL S V to W12 S IVa, n=41, 46, 46, 41, 35 | BL S V to W12 S V, n=41, 46, 46, 41, 35 | BL S V to W12 S Va, n=41, 46, 46, 41, 35 | BL S V to W12 S VI, n=41, 46, 46, 41, 35 | |
| Dutasteride 0.02 mg | 1 | 0 | 8 | 0 | 59 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 4 | 0 | 3 | 50 | 0 | 2 | 0 | 0 | 0 | 0 | 1 | 0 | 1 | 4 | 0 | 40 | 0 | 0 |
| Dutasteride 0.1 mg | 0 | 0 | 11 | 1 | 55 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 8 | 44 | 1 | 4 | 0 | 0 | 0 | 0 | 0 | 0 | 3 | 5 | 0 | 38 | 0 | 0 |
| Dutasteride 0.5 mg | 1 | 0 | 10 | 0 | 59 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 4 | 0 | 5 | 47 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 1 | 5 | 0 | 33 | 0 | 1 |
| Finasteride 1 mg | 0 | 0 | 11 | 0 | 62 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 5 | 45 | 0 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 2 | 0 | 33 | 0 | 0 |
| Placebo | 1 | 0 | 4 | 0 | 71 | 2 | 0 | 1 | 0 | 0 | 0 | 0 | 2 | 0 | 2 | 45 | 1 | 2 | 0 | 0 | 0 | 0 | 2 | 0 | 0 | 4 | 0 | 35 | 0 | 0 |
"The investigator/designee assessed the stage (Stage I to Stage VII) of AGA (i.e., male pattern baldness [MPB]) by utilizing the Norwood-Hamilton scale, used to measure the progression of MPB. Stage VII indicates worse balding than stage I. Assessment was made by direct visual examination (aided by pictures) of the participant at Baseline and Week 24 (W24). v, vertex; most of the hair loss (commonly seen with advancing age) is on the vertex. a, type a variant; major features are (1) the entire anterior hairline border recedes in unison; (2) there is no simultaneous balding of the vertex." (NCT01231607)
Timeframe: Baseline and Week 24
| Intervention | participants (Number) | |||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BL S IIIv to W24 S II, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S IIa, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S III, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S IIIa, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S IIIv, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S IV, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S IVa, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S V, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S Va, n=80, 72, 72, 72, 76 | BL S IIIv to W24 S VI, n=80, 72, 72, 72, 76 | BL S IV to W24 S II, n=52, 59, 59, 56, 54 | BL S IV to W24 S IIa, n=52, 59, 59, 56, 54 | BL S IV to W24 S III, n=52, 59, 59, 56, 54 | BL S IV to W24 S IIIa, n=52, 59, 59, 56, 54 | BL S IV to W24 S IIIv, n=52, 59, 59, 56, 54 | BL S IV to W24 S IV, n=52, 59, 59, 56, 54 | BL S IV to W24 S IVa, n=52, 59, 59, 56, 54 | BL S IV to W24 S V, n=52, 59, 59, 56, 54 | BL S IV to W24 S Va, n=52, 59, 59, 56, 54 | BL S IV to W24 S VI, n=52, 59, 59, 56, 54 | BL S V to W24 S II, n=41, 46, 46, 41, 35 | BL S V to W12 S IIa, n=41, 46, 46, 41, 35 | BL S V to W24 S III, n=41, 46, 46, 41, 35 | BL S V to W24 S IIIa, n=41, 46, 46, 41, 35 | BL S V to W24 S IIIv, n=41, 46, 46, 41, 35 | BL S V to W24 S IV, n=41, 46, 46, 41, 35 | BL S V to W24 S IVa, n=41, 46, 46, 41, 35 | BL S V to W24 S V, n=41, 46, 46, 41, 35 | BL S V to W24 S Va, n=41, 46, 46, 41, 35 | BL S V to W24 S VI, n=41, 46, 46, 41, 35 | |
| Dutasteride 0.02 mg | 2 | 0 | 8 | 0 | 61 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 3 | 0 | 7 | 46 | 0 | 2 | 0 | 0 | 1 | 0 | 1 | 0 | 1 | 10 | 0 | 33 | 0 | 0 |
| Dutasteride 0.1 mg | 2 | 0 | 11 | 0 | 58 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 4 | 0 | 11 | 39 | 0 | 4 | 0 | 0 | 0 | 0 | 1 | 0 | 4 | 8 | 0 | 33 | 0 | 0 |
| Dutasteride 0.5 mg | 3 | 1 | 13 | 0 | 54 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 5 | 2 | 10 | 37 | 1 | 0 | 0 | 0 | 0 | 0 | 3 | 0 | 3 | 10 | 0 | 25 | 0 | 0 |
| Finasteride 1 mg | 2 | 1 | 13 | 0 | 59 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 4 | 0 | 13 | 36 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 0 | 1 | 8 | 1 | 24 | 0 | 0 |
| Placebo | 3 | 0 | 6 | 0 | 67 | 4 | 0 | 0 | 0 | 0 | 0 | 0 | 2 | 0 | 4 | 44 | 0 | 2 | 0 | 0 | 0 | 0 | 2 | 0 | 3 | 7 | 0 | 29 | 0 | 0 |
Serum concentrations of dutasteride were measured after 12 weeks and 24 weeks of study treatment and at follow-up (approximately 2 weeks after the last dose of study treatment). (NCT01231607)
Timeframe: Week 12, Week 24, and Week 26
| Intervention | nanograms per milliliter (ng/mL) (Mean) | ||
|---|---|---|---|
| Week 12, n=172, 172, 165 | Week 24, n=158, 158, 153 | Week 26, n=156, 154, 152 | |
| Dutasteride 0.02 mg | 0.2 | 0.0 | 0.1 |
| Dutasteride 0.1 mg | 2.1 | 2.0 | 0.3 |
| Dutasteride 0.5 mg | 33.2 | 36.1 | 21.1 |
Serum concentrations of DHT were measured after 12 weeks and 24 weeks of study treatment and at follow-up (approximately 2 weeks after the last dose of study treatment). (NCT01231607)
Timeframe: Week 12, Week 24, and Week 26
| Intervention | nanomoles per liter (nmol/L) (Mean) | ||
|---|---|---|---|
| Week 12, n=172, 174, 172, 170, 161 | Week 24, n=173, 177, 176, 170, 165 | Week 26, n=173, 177, 177, 171, 165 | |
| Dutasteride 0.02 mg | 0.88 | 1.01 | 1.11 |
| Dutasteride 0.1 mg | 0.39 | 0.49 | 0.77 |
| Dutasteride 0.5 mg | 0.31 | 0.31 | 0.37 |
| Finasteride 1 mg | 0.45 | 0.49 | 1.03 |
| Placebo | 1.17 | 1.16 | 1.21 |
The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 24 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 24
| Intervention | Hair count (Least Squares Mean) |
|---|---|
| Placebo | -4.9 |
| Dutasteride 0.02 mg | 17.1 |
| Dutasteride 0.1 mg | 63.0 |
| Dutasteride 0.5 mg | 89.6 |
| Finasteride 1 mg | 56.5 |
The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 24 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 24
| Intervention | Hair count (Least Squares Mean) |
|---|---|
| Placebo | -0.3 |
| Dutasteride 0.02 mg | 4.2 |
| Dutasteride 0.1 mg | 12.4 |
| Dutasteride 0.5 mg | 18.1 |
| Finasteride 1 mg | 12.1 |
The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 12
| Intervention | Hair count (Least Squares Mean) |
|---|---|
| Placebo | -0.4 |
| Dutasteride 0.02 mg | 5.1 |
| Dutasteride 0.1 mg | 12.8 |
| Dutasteride 0.5 mg | 17.1 |
| Finasteride 1 mg | 10.8 |
The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 12
| Intervention | Hair count (Least Squares Mean) |
|---|---|
| Placebo | -4.0 |
| Dutasteride 0.02 mg | 22.9 |
| Dutasteride 0.1 mg | 59.6 |
| Dutasteride 0.5 mg | 82.3 |
| Finasteride 1 mg | 50.9 |
Change in Average Standard Drinks (14 gr ethanol) per week: last 2 weeks of treatment (wk 7-8) minus baseline average drinking average from baseline 90 day drinking history (NCT01262287)
Timeframe: Baseline (average weekly drinking for 90 day period prior to screening) vs. End Point (average weekly drinking weeks 7 and 8 of treatment)
| Intervention | standard drinks per week (Mean) |
|---|---|
| Dutasteride | -26.2 |
| Placebo | -25.5 |
Moderation of primary outcome measure [change in standard drinks per week from baseline to end point (average weeks 7 and 8 of treatment)] by genetic variation rs12529 in neuroactive steroid biosynthetic enzyme gene AKR1C (AKR1C3*2 C-allele associated with alcohol use disorder) (NCT01262287)
Timeframe: Baseline (average weekly drinking for 90 day period prior to screening) vs. End Point (average weekly drinking weeks 7 and 8 of treatment)
| Intervention | standard drinks per week (Mean) |
|---|---|
| AKR1C3*2 C/C Genotype + Dutasteride | -32.4 |
| AKR1C3*2 C/C Genotype + Placebo | -31.2 |
| AKR1C3*2 G-carriers + Dutasteride | 21.8 |
| AKR1C3*2 G-carriers + Placebo | -22.3 |
"The PPST questionnaire consists of two questions (asked to determine how satisfied participants are with the treatment received) and was administered at Baseline and all post-Baseline visits. Question 2 was: Would you ask your doctor for the treatment you received in this study? There were three possible responses, including: Yes, No, and Not sure. Response categories included Yes and No or Not Sure, created by grouping together No and Not sure. The LOCF method involves bringing forward the last non-missing post-Baseline assessment for a participant with missing data and/or for a participant who discontinued from the study." (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Participants (Number) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline, Yes, n=315, 328 | Baseline, No or Not Sure, n=315, 328 | Month 1, Yes, n=358, 347 | Month 1, No or Not Sure, n=358, 347 | Month 3, Yes, n=359, 357 | Month 3, No or Not Sure, n=359, 357 | Month 6, Yes, n=359, 360 | Month 6, No or Not Sure, n=359, 360 | Month 9, Yes, n=359, 361 | Month 9, No or Not Sure, n=359, 361 | Month 12, Yes, n=359, 363 | Month 12, No or Not Sure, n=359, 363 | Month 15, Yes, n=359, 364 | Month 15, No or Not Sure, n=359, 364 | Month 18, Yes, n=359, 364 | Month 18, No or Not Sure, n=359, 364 | Month 21, Yes, n=359, 364 | Month 21, No or Not Sure, n=359, 364 | Month 24, Yes, n=359, 364 | Month 24, No or Not Sure, n=359, 364 | |
| Dutasteride Plus Tamsulosin | 109 | 206 | 224 | 134 | 232 | 127 | 232 | 127 | 238 | 121 | 240 | 119 | 246 | 113 | 235 | 124 | 249 | 110 | 243 | 116 |
| Watchful Waiting All: Escalated Yes and No | 103 | 225 | 166 | 181 | 207 | 150 | 227 | 133 | 231 | 130 | 229 | 134 | 239 | 125 | 236 | 128 | 234 | 130 | 236 | 128 |
Symptom improvement was assessed using IPSS categorical changes from Baseline. Change from Baseline categories were summarized by treatment group using five improvement levels: >=1 point through >=5 points. IPSS percent change from Baseline was summarized using seven improvement levels: >0 percent, >=10 percent, >=20 percent, >=25 percent, >=30 percent, >=40 percent, and >=50 percent. Change in IPSS from Baseline was analysed using the LOCF method and is summarized for the following categories: >=2 points, >=3 points, and percent change >=25. The 7 items in the IPSS questionnaire quantitatively measure the level of urinary symptoms reported as a total IPSS. The total IPSS (sum of the first 7 items) can range from 0 to 35: mild (0 to 7), moderate (8 to 19), or severe (20 to 35). (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Participants (Number) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 1, >=2 points, n=358, 367 | Month 1, >=3 points, n=358, 367 | Month 1, >=25 percent, n=358, 367 | Month 3, >=2 points, n=359, 368 | Month 3, >=3 points, n=359, 368 | Month 3, >=25 percent, n= 359, 368 | Month 6, >=2 points, n=359, 368 | Month 6, >=3 points, n=359, 368 | Month 6, >=25 percent, n=359, 368 | Month 9, >=2 points, n=359, 368 | Month 9, >=3 points, n=359, 368 | Month 9, >=25 percent, n=359, 368 | Month 12, >=2 points, n=359, 368 | Month 12, >=3 points, n=359, 368 | Month 12, >=25 percent, n= 359, 368 | Month 15, >=2 points, n=359, 368 | Month 15, >=3 points, n=359, 368 | Month 15, >=25 percent, n=359, 368 | Month 18, >=2 points, n=359, 368 | Month 18, >=3 points, n=359, 368 | Month 18, >=25 percent, 359, 368 | Month 21, >=2 points, n=359, 368 | Month 21, >=3 points, n=359, 368 | Month 21, >=25 percent, n= 359, 368 | Month 24, >=2 points, n=359, 368 | Month 24, >=3points, n=359, 368 | Month 24, >=25 percent, n= 359, 368 | |
| Dutasteride Plus Tamsulosin | 225 | 182 | 161 | 277 | 233 | 218 | 277 | 245 | 229 | 286 | 257 | 247 | 291 | 261 | 249 | 289 | 259 | 245 | 288 | 262 | 245 | 292 | 267 | 253 | 295 | 277 | 261 |
| Watchful Waiting All: Escalated Yes and No | 149 | 90 | 76 | 221 | 172 | 150 | 250 | 208 | 189 | 276 | 222 | 207 | 273 | 229 | 214 | 275 | 243 | 231 | 268 | 229 | 212 | 274 | 237 | 224 | 279 | 234 | 221 |
A post-randomization adverse event is defined as an event with an onset on or after the randomization date or with a missing onset date. An AE is defined as any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect. Medical or scientific judgment was exercised in deciding whether reporting was appropriate in other situations. Refer to the general non-serious AE/SAE module for a list of non-serious AEs (occurring at a frequency threshold of >=5%) and SAEs. (NCT01294592)
Timeframe: Up to 2 years
| Intervention | Participants (Number) | |
|---|---|---|
| Any AE | Any SAE | |
| Dutasteride Plus Tamsulosin | 190 | 38 |
| Watchful Waiting All: Escalated Yes and No | 119 | 25 |
| Watchful Waiting Escalated=Yes | 95 | 19 |
BPH-related surgery was summarized for events occurring on or after the date of randomization. The number of participants who had any BPH-related surgery, the indicated type of surgery, and multiple surgeries was summarized by treatment. Type of surgery data (cystoscopy, transurethral resection of the prostate [TURP], and prostatectomy) are presented in terms of the first-occurring BPH-related surgery after randomization. It was possible for a single participant to have multiple surgeries. (NCT01294592)
Timeframe: Up to Month 24
| Intervention | Participants (Number) | |||||
|---|---|---|---|---|---|---|
| Participants with any BPH-related surgery | Participants with cystoscopy | Participants with TURP | Participants with prostatectomy | Participants with 2 surgeries | Participants with >=3 surgeries | |
| Dutasteride Plus Tamsulosin | 6 | 5 | 2 | 0 | 1 | 0 |
| Watchful Waiting All: Escalated Yes and No | 3 | 1 | 1 | 1 | 0 | 0 |
The number of participants with the first occurrence of clinical progression (CP) of BPH occurring on or after the randomization date are summarized by treatment and year. Time is based on the date of the first-occurring CP event, and is relative to the randomization date. CP of BPH is a composite of five endpoints assessed through the end of the study, including: symptom deterioration by IPSS >=3 points from Baseline (Visit 2); acute urinary retention related to BPH; incontinence (overflow or urge) related to BPH; recurrent urinary tract infection (UTI) or urosepsis related to BPH; renal insufficiency related to BPH (a single >=50% rise from Baseline serum creatinine and a total value >=1.5 milligrams/deciliter). For components that required multiple episodes, the first of the multiple episodes was utilized in terms of timing. (NCT01294592)
Timeframe: Up to 2 years
| Intervention | Events (Number) | |
|---|---|---|
| Year 1, n=369, 373 | Year 2, n=276, 251 | |
| Dutasteride Plus Tamsulosin | 48 | 17 |
| Watchful Waiting All: Escalated Yes and No | 94 | 14 |
"Each participant was asked 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?. This response was rated from 0 (delighted) to 6 (terrible). Change from Baseline in the BHS score was summarized by treatment group using the LOCF approach at each scheduled post-Baseline assessment. LOCF analysis involves bringing forward the last non-missing post-Baseline assessment for a participant with missing data and/or for a participant who discontinued from the study. Estimates are based on the adjusted means from the general linear model: Change from Baseline =Treatment + Cluster + Baseline Value. Baseline is defined as the Visit 2 value if it exists; otherwise, it is the latest of all Screening values. Change from Baseline was calculated as the post-Baseline value minus the Baseline value." (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Scores on a scale (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Month 1, n=358, 367 | Month 3, n=359, 368 | Month 6, n=359, 368 | Month 9, n=359, 368 | Month 12, n=359, 368 | Month 15, n=359, 368 | Month 18, n=359, 368 | Month 21, n=359, 368 | Month 24, n=359, 368 | |
| Dutasteride Plus Tamsulosin | -0.8 | -1.1 | -1.2 | -1.3 | -1.3 | -1.4 | -1.4 | -1.5 | -1.5 |
| Watchful Waiting All: Escalated Yes and No | -0.3 | -0.7 | -0.9 | -1.0 | -1.1 | -1.1 | -1.1 | -1.1 | -1.1 |
The BII is a 4-item questionnaire covering physical discomfort, worry, bother, and impact on usual activities, with a minimum score of 0 (best) and a maximum score (worst) of 13 points. Individual missing questionnaire responses were imputed, as applicable. Change from Baseline in the BII score was summarized by treatment group using the LOCF approach at each scheduled post-Baseline assessment. LOCF analysis involves bringing forward the last non-missing post-Baseline assessment for a participant with missing data and/or for a participant who discontinued from the study. Estimates are based on the adjusted means from the general linear model: Change from Baseline =Treatment + Cluster + Baseline Value. Baseline is defined as the Visit 2 value if it exists; otherwise, it is the latest of all Screening values. Change from Baseline was calculated as the post-Baseline value minus the Baseline value. (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Scores on a scale (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Month 1, n=357, 366 | Month 3, n=359, 368 | Month 6, n=359, 368 | Month 9, n=359, 368 | Month 12, n=359, 368 | Month 15, n=359, 368 | Month 18, n=359, 368 | Month 21, n=359, 368 | Month 24, n=359, 368 | |
| Dutasteride Plus Tamsulosin | -1.3 | -1.8 | -1.9 | -2.1 | -2.1 | -2.2 | -2.2 | -2.4 | -2.4 |
| Watchful Waiting All: Escalated Yes and No | -0.4 | -1.0 | -1.3 | -1.5 | -1.5 | -1.5 | -1.4 | -1.6 | -1.6 |
Study drug exposure (days) = treatment stop date - treatment start date + 1. Participants in the Watchful Waiting Escalated=Yes subgroup could have been escalated to study drug at any time during the study. Therefore, it is possible that participants were exposed to tamsulosin for a shorter length of time than participants in the dutasteride plus tamsulosin group. (NCT01294592)
Timeframe: Up to 2 years
| Intervention | days (Mean) |
|---|---|
| Dutasteride Plus Tamsulosin | 639.8 |
| Watchful Waiting Escalated=Yes | 566.3 |
"The IPSS questionnaire is a 7-item self-administered questionnaire designed to quantify the following urinary symptoms: Question 1 (Q1), incomplete emptying; Q2, frequency; Q3, intermittency; Q4, urgency; Q5, weak stream; Q6, straining; Q7, nocturia. It has an additional, independent eighth question to assess change in BPH-related health status (BHS) and quality of life. BHS scores range from 0 to 6, where 0 indicates delighted and 6 indicates terrible. The 7 items in the IPSS questionnaire quantitatively measure the level of urinary symptoms reported as a total IPSS. The total IPSS (sum of the first 7 items) can range from 0 to 35: mild (0 to 7), moderate (8 to 19), or severe (20 to 35). Change from Baseline in IPSS total score was calculated as the Month 24 value minus the Baseline value. LOCF analysis involves bringing forward the last non-missing post-Baseline assessment for a participant with missing data and/or for a participant who discontinued from the study." (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Scores on a scale (Least Squares Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Month 1, n=358, 367 | Month 3, n=359, 368 | Month 6, n=359, 368 | Month 9, n=359, 368 | Month 12, n=359, 368 | Month 15, n=359, 368 | Month 18, n=359, 368 | Month 21, n=359, 368 | Month 24, n=359, 368 | |
| Dutasteride Plus Tamsulosin | -3.2 | -4.5 | -4.6 | -5.1 | -5.2 | -5.2 | -5.1 | -5.5 | -5.4 |
| Watchful Waiting All: Escalated Yes and No | -0.9 | -2.4 | -3.2 | -3.6 | -3.6 | -3.6 | -3.3 | -3.6 | -3.6 |
"CP of BPH is a composite of five endpoints assessed through the end of the study, including: symptom progression (symptom deterioration by IPSS >=3 points from Baseline [Visit 2]); acute urinary retention (AUR) related to BPH; incontinence (overflow or urge) related to BPH; recurrent urinary tract infection (UTI) or urosepsis related to BPH; renal insufficiency related to BPH (a single >=50% rise from Baseline serum creatinine and a total value >=1.5 milligrams/deciliter). The number of participants with CP of BPH, the number of participants with the indicated first-occurring component of CP of BPH, the number of participants with two simultaneously first-occurring components (Tied for first component), and the number of participants with multiple first-occurring components were summarized by treatment group." (NCT01294592)
Timeframe: Up to Month 24
| Intervention | Participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Participants with CP of BPH, n=369, 373 | BPH symptom progression, n=65, 108 | BPH-related AUR, n=65, 108 | BPH-related incontinence, n=65, 108 | Recurrent BPH-related UTI, n=65, 108 | BPH-related renal insufficiency, n=65, 108 | Tied for first component, n=65, 108 | Multiple components (2 components), n=65, 108 | Multiple components (3 components), n=65, 108 | Multiple components (>=4 components), n=65, 108 | |
| Dutasteride Plus Tamsulosin | 65 | 59 | 2 | 4 | 0 | 0 | 0 | 4 | 0 | 0 |
| Watchful Waiting All: Escalated Yes and No | 108 | 97 | 4 | 3 | 4 | 0 | 0 | 9 | 1 | 1 |
"The PPST questionnaire consists of two questions (asked to determine how satisfied participants are with the treatment received) and was administered at Baseline and all post-Baseline visits. Question 1 was: Overall, how satisfied are you with the treatment and its effect on your urinary problems? There were seven possible responses, including: very satisfied, satisfied, somewhat satisfied, neutral, somewhat dissatisfied, dissatisfied, and very dissatisfied. Response categories were created by grouping together very satisfied, satisfied, and somewhat satisfied responses into the category of Any Satisfaction (AS), and separately grouping neutral, somewhat dissatisfied, dissatisfied, and very dissatisfied responses into the category of Neutral or Any Dissatisfaction (N/AD). The LOCF method involves bringing forward the last non-missing post-Baseline assessment for a participant with missing data and/or for a participant who discontinued from the study." (NCT01294592)
Timeframe: Baseline and Months 1, 3, 6, 9, 12, 15, 18, 21, and 24
| Intervention | Participants (Number) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline, Any Satisfaction, n=315, 328 | Baseline, Neutral/Any Dissatisfaction, n=315, 328 | Month 1, Any Satisfaction, n=358, 349 | Month 1, Neutral/Any Dissatisfaction, n=358, 349 | Month 3, Any Satisfaction, n= 359, 359 | Month 3, Neutral/Any Dissatisfaction, n=359, 359 | Month 6, Any Satisfaction, n=359, 361 | Month 6, Neutral /Any Dissatisfaction, n=359, 361 | Month 9, Any Satisfaction, n=359, 361 | Month 9, Neutral/Any Dissatisfaction, n= 359, 361 | Month 12, Any Satisfaction, n=359, 363 | Month 12, Neutral/Any Dissatisfaction, n=359, 363 | Month 15, Any Satisfaction, n=359, 364 | Month 15, Neutral/Any Dissatisfaction, n=359, 364 | Month 18, Any Satisfaction, n=359, 364 | Month 18, Neutral/Any Dissatisfaction, n=359, 364 | Month 21, Any Satisfaction, n=359, 364 | Month 21, Neutral/Any Dissatisfaction, n=359, 364 | Month 24, Any Satisfaction, n=359, 364 | Month 24, Neutral/Any Dissatisfaction, n=359, 364 | |
| Dutasteride Plus Tamsulosin | 119 | 196 | 272 | 86 | 300 | 59 | 301 | 58 | 304 | 55 | 311 | 48 | 311 | 48 | 305 | 54 | 310 | 49 | 312 | 47 |
| Watchful Waiting All: Escalated Yes and No | 122 | 206 | 209 | 140 | 265 | 94 | 285 | 76 | 293 | 68 | 305 | 58 | 299 | 65 | 298 | 66 | 300 | 64 | 312 | 52 |
"A serious adverse event is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or results in prolongation of existing hospitalization, results in disability/incapacity, or is a congenital anomaly/birth defect. For a list of all serious adverse events occurring during the course of the study, see the table entitled Serious Adverse Events in the Adverse Event section of the results record." (NCT01299571)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Avodart 0.5 mg | 5 |
"An adverse event is any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. For a list of all adverse events occurring during the course of the study, see the table entitled Other (Non-Serious) Adverse Events in the Adverse Event section of the results record." (NCT01299571)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Avodart 0.5 mg | 146 |
An adverse event is any untoward medical occurrence in a participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Unexpected adverse events include those not listed in the approved product information and not described as precautions or warnings. (NCT01299571)
Timeframe: 6 months
| Intervention | participants (Number) | ||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Insomnia | Mouth Dry | Constipation | Abdominal Pain | Diarrhea | Vomiting | Colonic Polyp | Epigastric Discomfort | Gastroesophageal Reflux | Hemorrhoids | Asthenia | Fever | Chills | Pain | Spasms | Orofacial Dyskinesia | Embolism Pulmonary | Thrombosis Cerebral | Nose Congestion | Pneumonia | Lung Carcinoma | Skin Eruption | Thrombosis Venous Deep | |
| Avodart 0.5 mg | 2 | 3 | 2 | 2 | 2 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 | 1 |
In this analysis, we evaluated mean BPH-related costs for every 30 days of 5-ARI therapy. Mean costs were evaluated by month on therapy for BPH-related medical costs (defined as any claim with a primary ICD-9-CM code of 222.2 or 600.xx). (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | United States dollars per month (Mean) |
|---|---|
| Acute Urinary Retention Outcomes Cohort | 28.08 |
| Prostate Surgery Outcomes Cohort | 29.89 |
Claims-based definition of AUR and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR and surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 75%. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | participants (Number) | |
|---|---|---|
| Number of Participants with AUR and surgery | Number of Participants without AUR and surgery | |
| Acute Urinary Retention Outcomes Cohort, MPR <=75% | 2755 | 7658 |
| Acute Urinary Retention Outcomes Cohort, MPR >75% | 1277 | 5603 |
| Prostate Surgery Outcomes Cohort, MPR <=75% | 627 | 10480 |
| Prostate Surgery Outcomes Cohort, MPR >75% | 185 | 6447 |
In this analysis, we evaluated mean BPH-related costs per month for participants with an MPR of >=80% versus <80%. Mean costs were evaluated by month on therapy for BPH-related medical costs (defined as any claim with a primary ICD-9-CM code of 222.2 or 600.xx). (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | United States dollars per month (Mean) | |
|---|---|---|
| MPR >=80% | MPR <80% | |
| Acute Urinary Retention Outcomes Cohort | 24.24 | 30.83 |
| Prostate Surgery Outcomes Cohort | 23.02 | 33.95 |
Claims-based definition of AUR and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR and surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 80%. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | participants (Number) | |
|---|---|---|
| Number of Participants with AUR and surgery | Number of Participants without AUR and surgery | |
| Acute Urinary Retention Outcomes Cohort, MPR <=80% | 2812 | 8975 |
| Acute Urinary Retention Outcomes Cohort, MPR >80% | 915 | 4591 |
| Prostate Surgery Outcomes Cohort, MPR <=80% | 627 | 11326 |
| Prostate Surgery Outcomes Cohort, MPR >80% | 185 | 5601 |
In this analysis, we evaluated mean BPH-related costs per month for participants with an MPR of >=75% versus <75%. Mean costs were evaluated by month on therapy for BPH-related medical costs (defined as any claim with a primary ICD-9-CM code of 222.2 or 600.xx). (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | United States dollars per month (Mean) | |
|---|---|---|
| MPR >=75% | MPR <75% | |
| Acute Urinary Retention Outcomes Cohort | 27.12 | 29.64 |
| Prostate Surgery Outcomes Cohort | 27.14 | 32.37 |
In this analysis, we evaluated mean BPH-related costs per month for participants with an MPR of >=70% versus <70%. Mean costs were evaluated by month on therapy for BPH-related medical costs (defined as any claim with a primary ICD-9-CM code of 222.2 or 600.xx). (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | United States dollars per month (Mean) | |
|---|---|---|
| MPR >=70% | MPR <70% | |
| Acute Urinary Retention Outcomes Cohort | 23.56 | 35.25 |
| Prostate Surgery Outcomes Cohort | 24.40 | 38.59 |
In this analysis, we evaluated the association between 5-ARI length of therapy and risk of acute urinary retention and prostate surgery. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | days (Mean) |
|---|---|
| Acute Urinary Retention Outcomes Cohort | 276.8 |
| Prostate Surgery Outcomes Cohort | 289.5 |
Claims-based definition of acute urinary retention (AUR) and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR or surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 70%. (NCT01334723)
Timeframe: The 5 and a half year period from January 1, 2000 to June 30, 2006
| Intervention | participants (Number) | |
|---|---|---|
| Number of Participants with AUR and Surgery | Number of Participants without AUR and Surgery | |
| Acute Urinary Retention Outcomes Cohort, MPR <=70% | 2140 | 5511 |
| Acute Urinary Retention Outcomes Cohort, MPR >70% | 1587 | 8055 |
| Prostate Surgery Outcomes Cohort, MPR <=70% | 481 | 6905 |
| Prostate Surgery Outocomes Cohort, MPR >70% | 331 | 10022 |
Increase in prostate-specific antigen (PSA) measured over time. Freedom from biochemical failure (FFBF) was defined from the time of enrollment until PSA failure occurs as defined by the Phoenix definition of a rise to 2 ng/mL above the nadir PSA value. (NCT01342367)
Timeframe: 4 years
| Intervention | percentage of participants (Number) |
|---|---|
| SOC Cohort | 81 |
| Oral ADT Group | 88 |
"Questionnaires were completed in writing by the patient. Questionnaires were administered at 1-2 months after initiation of hormonal treatment (before RT), at 3-4 months (during RT), and at 6 months after initiation of study therapy. Patients also completed questionnaires at 12, 18, and 24 months after completion of radiation therapy. Of primary interest were the baseline and 6 month and 24 month timepoints which are reported here.~Scale scores could range from 0-100, with higher scores indicating better quality of life." (NCT01342367)
Timeframe: Baseline, 6 months, and 24 months
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Baseline | 6 month | 24 month | |
| Oral ADT Group | 89 | 88 | 84 |
| SOC Cohort | 92 | 81 | 83 |
EP-related charges were defined as medical claims submitted to The Health Alliance Plan (HAP), a Health Maintenance Organization (HMO) owned and operated by the Henry Ford Heath System (HFHS) for reimbursement and internal billing data that had a primary diagnosis of EP. Charges were assessed during months 5 to 12 of the variable follow-up period. Follow-up could end only due to end of continuous eligibility, end of study period, or end of 1-year follow-up. Charges were computed on a per-month basis due to differences in the length of follow-up in the sample. (NCT01386983)
Timeframe: 3 months prior to and 12 months following index date
| Intervention | dollars (Mean) |
|---|---|
| Early Cohort | 129.14 |
| Delayed Cohort | 254.51 |
Participants with clinical progression are defined as those with acute urinary retention and/or receiving prostate-related surgery. (NCT01386983)
Timeframe: 3 months prior to and 12 months following index date
| Intervention | participants (Number) |
|---|---|
| Early Cohort | 14 |
| Delayed Cohort | 5 |
Overall response (OR) rate was defined as achieving partial response (PR) or complete response (CR) based on RECIST 1.0 criteria on treatment. Per RECIST 1.0 for target lesions, CR is complete disappearance of all target lesions and PR is at least a 30% decrease in the sum of longest diameter (LD) of target lesions, taking as reference baseline sum LD. To be assigned a status of CR or PR, changes in tumor measurements must be confirmed by repeat assessments performed no fewer than 4 weeks after the response criteria are first met. PR or better overall response assumes at a minimum incomplete response/stable disease (SD) for the evaluation of non-target lesions and absence of new lesions. (NCT01393730)
Timeframe: Disease was evaluated radiologically at baseline and every 12 weeks cycles on treatment. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | Participants (Count of Participants) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 6 |
Serum androgen levels measured based on established methods. The change from baseline to progression was calculated for each participant. (NCT01393730)
Timeframe: Pairs of patients' samples for androgen analyses were obtained at baseline and at time of progression. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | ng/dl (Median) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 1.2 |
Serum testosterone levels were estimated based on established methods. The change from baseline to progression was calculated for each participant. (NCT01393730)
Timeframe: Samples for testosterone analyses were obtained at baseline and at time of progression. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | ng/dL (Median) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 0.25 |
AR related mutation was defined as presence of T878A mutation. Expression of T878A was measured by established methods. (NCT01393730)
Timeframe: Pairs of patients samples were evaluated at baseline and time of progression. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | Participants (Count of Participants) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 1 |
Presence of AR amplification was measured by established methods. (NCT01393730)
Timeframe: Patients' samples were evaluated at baseline and every 12 weeks on treatment. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | Participants (Count of Participants) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 10 |
PSA response was defined as decline of 50% from baseline confirmed by a PSA at least 4 weeks later based on Prostate-specific Antigen Working Group-2 (PSAWG-2) (2008) criteria. (NCT01393730)
Timeframe: PSA was measured at baseline and day 1 of every cycle on treatment. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | Participants (Count of Participants) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 34 |
TTP based on the Kaplan-Meier method is defined as the duration of time from study entry to documented first observation of progressive disease (PD). Per RECIST 1.0 for target lesions, PD is at least a 20% increase in sum LD of target lesions, taking as reference the smallest sum LD recorded since the treatment started or appearance of new lesions. For non-target lesions, PD is the appearance of one or more new lesions and/or unequivocal progression of existing non-target lesions. (NCT01393730)
Timeframe: Disease evaluation occurred every 12 weeks while patients were receiving treatment. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | Months (Median) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 11 |
Time to PSA progression based on the Kaplan-Meier method was defined as the time between registration and documented PSA progression. PSA progression based on Prostate-Specific Antigen Working Group-2 (PSAWG-2) (2008) criteria was an increase of >/=25% and >/= 2 ng/ml after 12 weeks for patients without a PSA decline from baseline and an increase of >/=25% and >/= 2 ng/ml above the nadir, confirmed by a 2nd value 3 weeks or later for patients with a PSA decline from baseline. PSA progression was reported not duration of response. (NCT01393730)
Timeframe: PSA was measured at baseline and day 1 of every cycle on treatment. In this study cohort, participants were followed up to 48 months for this endpoint.
| Intervention | months (Median) |
|---|---|
| Abiraterone + Prednisone + Dutasteride | 5 |
(NCT01547299)
Timeframe: Baseline
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 4.10 |
| Enzalutamide | 3.69 |
(NCT01547299)
Timeframe: Day 180
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.12 |
| Enzalutamide | 9.76 |
To determine the effects on PSA as measured by the time to the lowest post baseline PSA value prior to prostatectomy. Prostate-specific antigen (PSA) was a protein produced by normal, as well as malignant, cells of the prostate gland. The PSA nadir was the participant's lowest observed post baseline PSA value. (NCT01547299)
Timeframe: Day 195
| Intervention | days (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 5.09 |
| Enzalutamide | 6.01 |
The Twelve-Item Short Form Version 2 was HRQoL instrument that measured general health and well-being across physical and mental components. The general health domain score contained 1 item scored on a scale of 1 to 5 where 1=excellent to 5=poor health, where higher score indicated worse health status. Best change from baseline category in general health domain score ranged from worsened (decrease of at least 1 minimally important difference), stable (changed by less than 1 minimally important difference), or improved (increase of at least 1 minimally important difference). Minimally important difference was defined as one-half the standard deviation of the score of interest at baseline. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 5 | 6 | 7 |
| Enzalutamide + Leuprolide + Dutasteride | 5 | 9 | 2 |
EPIC Hormonal Domain was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's hormonal function. It was measured on a scale ranged from 0 (worst) to 100 (best) scale with higher scores representing better hormonal function. Best change from baseline category in EPIC hormonal domain summary score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 10 | 7 | 1 |
| Enzalutamide + Leuprolide + Dutasteride | 10 | 3 | 3 |
EPIC hormonal bother subscale score was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's hormonal function. EPIC hormonal bother subscale was a component of hormonal domain that was evaluated on a distinct set of questions. It was measured on a scale ranged from 0 (worst) to 100 (best) scale with higher scores representing less hormonal bothering. Best change from baseline category in EPIC hormonal bother subscale score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 6 | 11 | 1 |
| Enzalutamide + Leuprolide + Dutasteride | 9 | 5 | 2 |
To determine the effects of triplet therapy and enzalutamide alone on androgen receptor signaling in prostatectomy specimens. Androgen receptor (AR) was a type of nuclear receptor that was activated by binding either of the androgenic hormones, testosterone, or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Androgen receptor (AR) signaling represented the major therapeutic target for treating metastatic prostate cancer. Assessment of androgen receptor signaling was measured by intensity of androgen receptor IHC staining and were graded as 0 (absent), 1 (weak), 2 (moderate) and 3 (strong). Percentage of participants within each grade are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| 0 | 1 | 2 | 3 | |
| Enzalutamide | 0.0 | 0.0 | 5.3 | 94.7 |
| Enzalutamide + Leuprolide + Dutasteride | 0.0 | 5.6 | 27.8 | 66.7 |
To determine the percentage of participants with positive surgical margins at prostatectomy as assessed by the local and central pathologist. Surgical margin, also known as tumor free margin referred to the visible normal tissue or skin margin that was removed with the surgical excision of a tumor, growth, or malignancy. The margin was described as positive when the pathologist finds cancer cells at the edge of the tissue, suggesting that all of the cancer has not been removed. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Local pathologist | Central pathologist | |
| Enzalutamide | 12.0 | 16.0 |
| Enzalutamide + Leuprolide + Dutasteride | 4.3 | 21.7 |
To determine the percentage of participants with positive seminal vesicles at prostatectomy as assessed by the local and central pathologist. Seminal vesicles or seminal glands, were defined as a pair of simple tubular glands located within the pelvis. They secrete fluid that partly composes the semen. Seminal vesicles with cancer cells in them were called positive seminal vesicles. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Local pathologist | Central pathologist | |
| Enzalutamide | 36.0 | 36.0 |
| Enzalutamide + Leuprolide + Dutasteride | 30.4 | 30.4 |
To determine the percentage of participants with positive lymph nodes at prostatectomy as assessed by the local and central pathologist. Lymph nodes were small clumps of immune cells that act as filters for the lymphatic system. Lymph nodes with cancer cells in them were called positive lymph nodes. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Local pathologist | Central pathologist | |
| Enzalutamide | 4.0 | 4.0 |
| Enzalutamide + Leuprolide + Dutasteride | 26.1 | 26.1 |
The Twelve-Item Short Form Version 2 was HRQoL instrument that measured general health and well-being across physical and mental components. The mental health domain score had 2 items scored on a scale of 1 to 5 where for 1 item 1=all of the time person felt calm and peaceful to 5=none of the time person felt calm and peaceful. The score ranged from 1 to 5, where higher scores meant worse mental status. For other item 1=all of the time person felt downhearted and blue to 5=none of the time person felt downhearted and blue. The score ranged from 1 to 5, where higher scores meant better mental status. Best change from baseline category in mental component summary ranged from worsened (decrease of at least 1 minimally important difference), stable (changed by less than 1 minimally important difference), or improved (increase of at least 1 minimally important difference). Minimally important difference was defined as one-half the standard deviation of the score of interest at baseline. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 1 | 11 | 5 |
| Enzalutamide + Leuprolide + Dutasteride | 4 | 8 | 4 |
Pathologic complete response rate was defined as percentage of participants with pathologic complete response. Pathologic complete response rate following triplet therapy (enzalutamide in combination with leuprolide and dutasteride) and enzalutamide alone when administered as neoadjuvant therapy for 180 days prior to prostatectomy in participants with localized prostate cancer. Pathologic complete response was defined as the absence of morphologically identifiable carcinoma in the prostatectomy specimen, as assessed by the local and central pathologist. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Local pathologist | Central pathologist | |
| Enzalutamide | 0.0 | 0.0 |
| Enzalutamide + Leuprolide + Dutasteride | 8.7 | 4.3 |
An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. (NCT01547299)
Timeframe: From baseline up to 210 days
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Permanent Discontinuation of Enzalutamide | Temporary Interruption of Enzalutamide | Dose Reduction of Enzalutamide | Study Drug Discontinuation | |
| Enzalutamide | 0 | 0 | 0 | 0 |
| Enzalutamide + Leuprolide + Dutasteride | 0 | 3 | 0 | 0 |
To determine pharmacodynamic effects as measured by the amount of tissue DHT in prostatectomy specimens following radical prostatectomy. (NCT01547299)
Timeframe: Day 180
| Intervention | picogram per milligram (Mean) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.04 |
| Enzalutamide | 3.34 |
Assessment was performed to determine the effects of triplet therapy and enzalutamide alone on mitotic index. Mitotic index was defined as the ratio between the numbers of cells in a population undergoing mitosis to the number of cells in a population not undergoing mitosis in prostatectomy specimens. (NCT01547299)
Timeframe: Day 180
| Intervention | ratio (Mean) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.9 |
| Enzalutamide | 2.6 |
To determine the percentage of participants with extracapsular extension at prostatectomy as assessed by the local pathologist. Extracapsular extension was defined as prostate cancer cells when extended into the prostate capsule or outer lining of the prostate gland. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 26.1 |
| Enzalutamide | 36.0 |
To determine the percentage of participants with extracapsular extension at prostatectomy as assessed by the central pathologist. Extracapsular extension was defined as prostate cancer cells when extended into the prostate capsule or outer lining of the prostate gland. (NCT01547299)
Timeframe: Day 180
| Intervention | percentage of participants (Number) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 56.5 |
| Enzalutamide | 70.8 |
To determine serum hormone effects as measured by change in testosterone at baseline and at completion of therapy. (NCT01547299)
Timeframe: Day 180
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | -4.00 |
| Enzalutamide | 5.74 |
To determine serum hormone effects as measured by change in DHT values from baseline to the completion of therapy. (NCT01547299)
Timeframe: Day 180
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | -0.33 |
| Enzalutamide | 0.25 |
EPIC hormonal function subscale score was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's hormonal function. EPIC hormonal function subscale was a component of hormonal domain that was evaluated on a distinct set of questions. It was measured on a scale ranged from 0 (worst) to 100 (best) scale with higher scores representing better hormonal function. Best change from baseline category in EPIC hormonal function subscale score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 11 | 7 | 0 |
| Enzalutamide + Leuprolide + Dutasteride | 11 | 2 | 3 |
The Twelve-Item Short Form Version 2 was HRQoL instrument that measured general health and well-being across physical and mental components. The mental health domain score had 2 items scored on a scale of 1 to 5, where higher scores indicated worse mental status. The total score ranged from 1 to 10, where higher scores indicated worse mental status. Best change from baseline category in mental component summary ranged from worsened (decrease of at least 1 minimally important difference), stable (changed by less than 1 minimally important difference), or improved (increase of at least 1 minimally important difference). Minimally important difference was defined as one-half the standard deviation of the score of interest at baseline. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 1 | 10 | 7 |
| Enzalutamide + Leuprolide + Dutasteride | 3 | 9 | 4 |
To determine the effects on PSA as measured by the percentage of participants with PSA less than (<) 0.2 nanogram per milliliter (ng/mL), and a 50 percent (%) and 90% decrease in PSA value prior to prostatectomy. Prostate-specific antigen (PSA) was a protein produced by normal, as well as malignant, cells of the prostate gland. (NCT01547299)
Timeframe: Day 195
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| PSA < 0.2 ng/mL | 50% decrease in PSA | 90% decrease in PSA | |
| Enzalutamide | 29.6 | 100.0 | 63.0 |
| Enzalutamide + Leuprolide + Dutasteride | 92.0 | 100.0 | 100.0 |
To determine pharmacodynamic effects as measured by the amount of tissue testosterone in prostatectomy specimens following radical prostatectomy. (NCT01547299)
Timeframe: Day 180
| Intervention | picogram per milligram (Mean) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.18 |
| Enzalutamide | 0.90 |
EPIC sexual bother subscale was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's sexual function and sexual satisfaction. EPIC sexual bother subscale was a component of sexual domain that was evaluated on a distinct set of questions. It was measured on a scale ranged from 0 (worst) to 100 (best) with higher scores representing less sexual bother and difficulty. Best change from baseline category in EPIC sexual bother subscale score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation of baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 5 | 7 | 4 |
| Enzalutamide + Leuprolide + Dutasteride | 7 | 9 | 0 |
EPIC sexual function subscale was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's sexual function and sexual satisfaction. EPIC sexual function subscale was a component of sexual domain that was evaluated on a distinct set of questions. It was measured on a scale ranged from 0 (worst) to 100 (best) with higher scores representing better sexual function. Best change from baseline category in EPIC sexual function subscale score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation of baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 12 | 5 | 0 |
| Enzalutamide + Leuprolide + Dutasteride | 11 | 4 | 0 |
EPIC sexual domain was HRQoL instrument that measured the effects of prostate cancer treatment on a participant's sexual function and sexual satisfaction. Sexual domain summary score was measured on a scale ranged from 0 (worst) to 100 (best) with higher scores representing better sexual function and satisfaction. Best change from baseline category in EPIC sexual domain summary score ranged from worsened to improved where worsened indicated decrease of at least 1 minimally important difference, stable indicated changed by less than 1 minimally important difference and improved indicated increase of at least 1 minimally important difference. Minimally important difference was defined as one-half of the standard deviation of baseline score. Number of participants within each category are reported below. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 10 | 6 | 0 |
| Enzalutamide + Leuprolide + Dutasteride | 11 | 4 | 1 |
The Twelve-Item Short Form Version 2 was HRQoL instrument that measured general health and well-being across physical and mental components. The physical functioning domain score contained 2 items each scored on a scale of 1 to 5 where 1=excellent physical functioning to 5=poor physical functioning. Physical functioning domain total score ranged from 1 to 10, where higher scores indicated poor physical functioning. Best change from baseline category in physical functioning domain score ranged from worsened (decrease of at least 1 minimally important difference), stable (changed by less than 1 minimally important difference), or improved (increase of at least 1 minimally important difference). Minimally important difference was defined as one-half the standard deviation of the score of interest at baseline. (NCT01547299)
Timeframe: Day 180
| Intervention | participants (Number) | ||
|---|---|---|---|
| Worsened | Stable | Improved | |
| Enzalutamide | 2 | 15 | 1 |
| Enzalutamide + Leuprolide + Dutasteride | 3 | 12 | 1 |
To determine the effects on PSA as measured by the lowest post baseline PSA value prior to prostatectomy. Prostate-specific antigen (PSA) was a protein produced by normal, as well as malignant, cells of the prostate gland. The PSA nadir was the participant's lowest observed post baseline PSA value. (NCT01547299)
Timeframe: Day 195
| Intervention | microgram per liter (mcg/L) (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.04 |
| Enzalutamide | 0.51 |
(NCT01547299)
Timeframe: Baseline
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.34 |
| Enzalutamide | 0.29 |
(NCT01547299)
Timeframe: Day 180
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.01 |
| Enzalutamide | 0.51 |
The Qmax is used as an indicator for the diagnosis of enlarged prostate. A lower Qmax may indicate that the enlarged prostate. Qmax was assessed at Baseline (screening), Month 3 and Month 6. Change from Baseline was calculated as Qmax score at specified timepoint minus the Baseline Qmax score. (NCT01673490)
Timeframe: Baseline, Month 3 and Month 6
| Intervention | Mililiter/seconds (Mean) | |
|---|---|---|
| Month 3, n=54 | Month 6, n=52 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 2.77 | 2.01 |
The IPSS is a screening tool used to assess the symptoms of prostate related disease. The IPSS questionnaire consists of seven symptoms questions including feeling of incomplete bladder emptying, frequency, intermittency, urgency, weak stream, straining and nocturia, each referring to during the last month, and each involving assignment of a score from 0 to 5 (no symptoms to almost always symptoms) for a total of maximum 35 points. IPSS total is the sum of the scores of seven questions; therefore, the possible total score ranges from 0 to 35 (0-7: Mildly symptomatic; 8-19: Moderately symptomatic; 20-35: Severely symptomatic). IPSS was assessed at Baseline and Month 6. Change from Baseline was calculated as Month 6 IPSS score- minus Baseline IPSS score. (NCT01673490)
Timeframe: Baseline and Month 6
| Intervention | Scores on a scale (Mean) |
|---|---|
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -8.3 |
Blood samples were collected at Screening, Month 3 (Visit 3) and Month 6 (Visit 5) for hematology laboratory assessments. Hematology parameters included basophils, leukocytes, hemoglobin (HGB), eosinophils, erythrocytes (ery), ery mean Corpuscular HGB concentration, ery mean corpuscular HGB, ery distribution width, lymphocytes, hematocrit, monocytes, neutrophils and platelets. The number of participants with a shift from normal at Baseline to abnormal at any time post-Baseline for hematology parameters are summarized. (NCT01673490)
Timeframe: Screening, Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Basophils/Leukocytes, n=54 | Eosinophils/Leukocytes, n=46 | Ery Mean Corpuscular HGB Concentration, n=44 | Ery Mean Corpuscular Hemoglobin, n=36 | Ery Mean Corpuscular Volume, n=42 | Erythrocytes, n=49 | Erythrocytes Distribution Width, n=4 | Hematocrit, n=48 | Hemoglobin, n=49 | Leukocytes, n=47 | Lymphocytes/Leukocytes, n=53 | Monocytes/Leukocytes, n=52 | Neutrophils/Leukocytes, n=41 | Platelets, n=53 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 0 | 5 | 22 | 6 | 4 | 3 | 3 | 7 | 2 | 7 | 1 | 1 | 5 | 1 |
Serum sample was collected at Screening (Baseline for participants with Free to Total PSA ratio at Month 6), and Month 6 for assessment of free to total PSA ratio. PSA is a substance produced by prostate gland, and the elevated level of PSA indicates prostate cancer or any other non-cancerous condition related to prostate. Free to total PSA ratio at Baseline for participants with free to total PSA Ratio at Month 6 and free to total PSA ratio at month 6 are presented. (NCT01673490)
Timeframe: Baseline, Month 6
| Intervention | Ratio (Mean) | |
|---|---|---|
| Baseline, n=50 | Month 6, n=52 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 28.207 | 24.887 |
Serum sample was collected at Baseline, Month 3 and Month 6 for assesment of total PSA. PSA is a substance produced by prostate gland, and the elevated level of PSA indicates prostate cancer or any other non-cancerous condition related to prostate. Change from Baseline in total PSA at Month 3 and Month 6 was calculated as value at specified visist minus Baseline value. (NCT01673490)
Timeframe: Baseline, Month 3 and Month 6
| Intervention | Microgram per liter (ug/L) (Mean) | |
|---|---|---|
| Month 3, n=54 | Month 6, n=52 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | -1.499 | -1.824 |
Urine samples were collected at Screening (SC), Month 3 (3M) and Month 6 (6M) for urinalysis laboratory assesment. Final value (FV) is defined as the latest post-Baseline value available in the study for each parameter.Urinalysis parameters included erythrocytes, glucose, ketones, leukocytes and protein. Number of participants with a negative (NEG) or positive (POS) response at the indicated time points are summarized. (NCT01673490)
Timeframe: Screening, Month 3 and Month 6
| Intervention | Participants (Number) | |||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Erythrocytes, SC, POS, n=59 | Erythrocytes, SC, NEG, n=59 | Erythrocytes, 3M, POS, n=54 | Erythrocytes, 3M, NEG, n=54 | Erythrocytes, 6M, POS, n=52 | Erythrocytes, 6M, NEG, n=52 | Erythrocytes, FV, POS, n=54 | Erythrocytes, FV, NEG, n=54 | Glucose, SC, POS, n=59 | Glucose, SC, NEG, n=59 | Glucose, 3M, POS, n=54 | Glucose, 3M, NEG, n=54 | Glucose, 6M, POS, n=52 | Glucose, 6M, NEG, n=52 | Glucose, FV, POS, n=54 | Glucose, FV, NEG, n=54 | Ketones, SC, POS, n=59 | Ketones, SC, NEG, n=59 | Ketones, 3M, POS, n=54 | Ketones, 3M, NEG, n=54 | Ketones, 6M, POS, n=52 | Ketones, 6M, NEG, n=52 | Ketones, FV, POS, n=54 | Ketones, FV, NEG, n=54 | Leukocytes, SC, POS, n=59 | Leukocytes, SC, NEG, n=59 | Leukocytes, 3M, POS, n=54 | Leukocytes, 3M, NEG, n=54 | Leukocytes, 6M, POS, n=52 | Leukocytes, 6M, NEG, n=52 | Leukocytes, FV, POS, n=54 | Leukocytes, FV, NEG, n=54 | Protein, SC, POS, n=59 | Protein, SC, NEG, n=59 | Protein, 3M, POS, n=54 | Protein, 3M, NEG, n=54 | Protein, 6M, POS, n=52 | Protein, 6M, NEG, N=52 | Protein, FV, POS, n=54 | Protein, FV, NEG, n=54 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 4 | 55 | 6 | 48 | 6 | 46 | 7 | 47 | 3 | 56 | 1 | 53 | 0 | 52 | 0 | 54 | 0 | 59 | 2 | 52 | 1 | 51 | 1 | 53 | 3 | 56 | 0 | 54 | 6 | 46 | 6 | 48 | 9 | 50 | 6 | 48 | 7 | 45 | 8 | 46 |
Blood samples were collected at Screening, Month 1 (Visit 1), Month 3 (Visit 3) and Month 6 (Visit 5) for chemistry laboratory assessments. Clinical chemistry parameters included alanine aminotrasferase (ALT), aspartate aminotrasferase (AST), creatinine, glucose, potassium, protein, sodium and urea. The number of participants with a shift from normal at Baseline to abnormal at any time post-Baseline for a clinical chemistry parameter are summarized. (NCT01673490)
Timeframe: Screening, Month 1, Month 3 and Month 6
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| ALT, n=48 | AST, n=49 | Creatinine, n=51 | Glucose, n=47 | Potassium, n=52 | Protein, n=56 | Sodium, n=53 | Urea, n=54 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 9 | 6 | 9 | 8 | 1 | 4 | 0 | 7 |
An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product at any dose, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, is an important medical event that jeopardizes the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, and is associated with liver injury and impaired liver function. (NCT01673490)
Timeframe: From start of study medication until follow-up (up to 7 months)
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Any AE | Any SAE | Any treatment-related AE | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 2 | 1 | 1 |
An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product at any dose, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a medicinal product. An SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, is a congenital anomaly/birth defect, is an important medical event that jeopardizes the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, and is associated with liver injury and impaired liver function. (NCT01673490)
Timeframe: From start of study medication until follow-up (up to 7 months)
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Any AE | Any SAE | Any treatment-related AE | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 13 | 1 | 3 |
A 12 lead ECG was measured at Screening, Month 1 (Visit 1), Month 3 (Visit 3) and Month 6 (Visit 5). (NCT01673490)
Timeframe: Screening, Month 1, Month 3 and Month 6
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Screening, n=59 | Month 1, n=56 | Month 3, n=53 | Month 6, n=52 | |
| Dutasteride 0.5 mg Plus Tamsulosin 0.4 mg | 49 | 47 | 50 | 44 |
Carbohydrate-deficient transferrin (CDT) at end of treatment as percentage of baseline. Serum CDT is a biochemical measure of heavy alcohol use. (NCT01758523)
Timeframe: end of 12-week treatment vs. baseline
| Intervention | percentage of baseline CDT (Mean) |
|---|---|
| Dutasteride | 94 |
| Sugar Pill | 107 |
Total number of drinks aggregated by week (NCT01758523)
Timeframe: 12-week treatment period
| Intervention | drinks/week (Mean) |
|---|---|
| Dutasteride | 22.0 |
| Sugar Pill | 27.2 |
Change in Number of days / week with 5 or more drinks consumed contrasting AKR1C3*2 CC vs. G-carrier genotype and treatment group (NCT01758523)
Timeframe: 12-week treatment period
| Intervention | heavy drinking days/week (Mean) |
|---|---|
| Dutasteride - AKR1C3*2 CC | 1.06 |
| Sugar Pill - AKR1C3*2 CC | 2.9 |
| Dutasteride - AKR1C3*2 G-carrier | 2.05 |
| Sugar Pill - AKR1C3*2 G-carrier | 2.5 |
Number of days / study week with 5 or more drinks consumed (NCT01758523)
Timeframe: 12-week treatment period
| Intervention | heavy drinking days/week (Mean) |
|---|---|
| Dutasteride | 1.75 |
| Sugar Pill | 2.67 |
Number of participants with no hazardous drinking (not more than 4 drinks on one day and not more than 14 drinks per week) during the last 4 weeks of treatment. (NCT01758523)
Timeframe: Last 4 weeks of treatment
| Intervention | Participants (Count of Participants) |
|---|---|
| Dutasteride | 13 |
| Sugar Pill | 3 |
Number of participants with no heavy drinking days (days with 5 or more drinks) during the last 4 weeks of treatment. (NCT01758523)
Timeframe: Last 4 weeks of treatment
| Intervention | Participants (Count of Participants) |
|---|---|
| Dutasteride | 16 |
| Sugar Pill | 8 |
Participants with change from baseline in total MSHQ scores with good BPH symptomatic response (measured by improvement in IPSS)were analysed.Change from BL at the scheduled post-baseline time points were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 12 value(s) minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 12
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Placebo | -0.6 |
| Duodart | -8.3 |
Total MSHQ score is composed of 3 domain scores: Erection score(ES)=sum of score for Questions (Q) 1 to 3(ranges from 0 to 15), Ejaculation score(EjS)=sum of scores for Q5 to 11(ranges from 1 to 35), Satisfaction score(SS)=sum of scores for Q13 to 18(ranges from 6 to 30). Total MSHQ score=ES+EjS+SS. The total MSHQ score ranges from 7-80, with higher scores indicating greater sexual function. Change from BL at scheduled post-BL time points were analyzed using a mixed model repeated measures (MMRM) analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest double-blind (DB) treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 12 value(s) minus BL value(s) (NCT01777269)
Timeframe: Baseline and 12 months
| Intervention | Scores on a scale (Least Squares Mean) |
|---|---|
| Placebo | -0.7 |
| Duodart | -8.7 |
Ejaculation scale is a domain of MSHQ to assess ejaculatory dysfunction. EjS is the sum of score for questions 5 to 11. The score ranges from 1 (could not ejaculate) to 35 (strong ejaculation). Change from BL at the scheduled post-baseline time points were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 1, 3, 6, 9 and 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1, n=210, 208 | Month 3, n= 197, 196 | Month 6, n= 191, 179 | Month 9, n=177, 161 | Month 12, n= 173, 164 | |
| Duodart | -3.2 | -5.8 | -7.5 | -7.6 | -7.5 |
| Placebo | -0.3 | -0.5 | -0.7 | -0.5 | -0.6 |
"Participants reaching thresholds of change in total MSHQ were assessed. Threshold values are defined as multiplicative factor. Threshold included +10 points, +20 points, +25 points, -10 points, -20 points, -25 points; where + indicates improvement and -indicates worsening. Treatment comparisons were done based on categories defined by these thresholds using Mantel-Haenszel test" (NCT01777269)
Timeframe: Baseline and 12 months
| Intervention | Participants (Number) | |||||
|---|---|---|---|---|---|---|
| >= 25 | >= 20 | >= 10 | <= -25 | <= -20 | <= -10 | |
| Duodart | 1 | 3 | 8 | 13 | 20 | 61 |
| Placebo | 0 | 3 | 16 | 3 | 3 | 24 |
Total MSHQ score is composed of 3 domain scores: ES+EjS+SS and the score ranges from 7-80, with higher scores indicating greater sexual function. Par. with change from baseline in total MSHQ scores with good BPH symptomatic response (measured by improvement in IPSS)were analysed. Change from BL at the scheduled post-baseline time points were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 12 value(s) minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 12
| Intervention | Scores on a scale (Least Squares Mean) | |
|---|---|---|
| IPSS improvement of >=2, n=152, 142 | IPSS improvement of >=3, n=138,136 | |
| Duodart | -8.4 | -8.0 |
| Placebo | -0.6 | -0.6 |
Satisfaction scale is a domain of MSHQ to assess sexual relationship. SS is the sum of score for questions 13 to 18. The score ranges from 6 (extremely dissatisfied) to 30 (extremely satisfied). Change from BL at the scheduled post-baseline time points were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 1, 3, 6, 9 and 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Month 1, n=200, 197 | Month 3, n= 189, 182 | Month 6, n= 185, 168 | Month 9, n=173, 153 | Month 12, n= 169, 152 | |
| Duodart | -0.8 | -0.5 | -1.5 | -1.2 | -0.6 |
| Placebo | 0.1 | 0.4 | 0.2 | -0.0 | 0.3 |
The BPH Impact Index (BII) is a 4-item, self-administered questionnaire evaluating the 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. Change from BL were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the subject took at least one dose of DB study drug; change from BL was calculated as Week 2, Months 1, 3, 6, 9 and 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 2, n=226, 227 | Month1, n=216, 223 | Month 3, n=211, 217 | Month 6, n=201, 195 | Month 9, n=188, 179 | Month 12, n=183, 177 | |
| Duodart | -0.7 | -0.7 | -1.1 | -1.2 | -1.2 | -1.2 |
| Placebo | -0.3 | -0.7 | -0.9 | -0.6 | -0.7 | -0.6 |
Patient Perception of Study Medication (PPSM) is a 12-item questionnaire designed to quantify the participant's perceptions and satisfaction with the effect of study treatment on control of their urinary symptoms. The total PPSM score ranges from 7 to 49, with higher scores indicating lower satisfaction. Change from BL were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the subject took at least one dose of DB study drug; change from BL was calculated as Week 2, Months 1, 3, 6, 9, 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline, Week 2, Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 2, n=225, 227 | Month1, n=216, 223 | Month 3, n=211, 217 | Month 6, n=201, 195 | Month 9, n=188, 179 | Month 12, n=182, 177 | |
| Duodart | -3.4 | -3.4 | -3.8 | -3.6 | -2.9 | -4.6 |
| Placebo | -0.4 | -1.3 | -1.7 | -1.0 | -1.6 | -1.0 |
The IPSS questionnaire is a 7-item self-administered questionnaire designed to quantify urinary symptoms: Q1, incomplete emptying; Q2, frequency; Q3, intermittency; Q4, urgency; Q5, weak stream; Q6, straining; Q7, nocturia. The score can range from 0 to 35: mild (0 to 7), moderate (8 to 19), or severe (20 to 35). Change from BL were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Week 2, Months 1, 3, 6, 9 and 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Least Squares Mean) | |||||
|---|---|---|---|---|---|---|
| Week 2, n=232, 234 | Month1, n=222, 231 | Month 3, n=217, 224 | Month 6, n=206, 203 | Month 9, n=193, 185 | Month 12, n=187, 184 | |
| Duodart | -3.1 | -3.4 | -4.1 | -4.6 | -4.5 | -5.2 |
| Placebo | -1.5 | -2.8 | -2.8 | -2.9 | -3.2 | -3.2 |
Total MSHQ score is composed of 3 domain scores: ES=sum of score for Q 1 to 3(ranges from 0 to 15), EjS=sum of scores for Q5 to 11(ranges from 1 to 35), SS=sum of scores for Q13 to 18(ranges from 6 to 30). Total MSHQ score=ES+EjS+SS and the score ranges from 7-80, with higher scores indicating greater sexual function. Change from BL at scheduled post-BL time points were analysed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 1, 3, 6, 9 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, and 9
| Intervention | Scores on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Month 1, n=193, 192 | Month 3, n= 184, 181 | Month 6, n=179, 164 | Month 9, n=166, 146 | |
| Duodart | -4.6 | -6.9 | -9.9 | -9.6 |
| Placebo | -0.5 | -0.5 | -0.8 | -0.8 |
Erection scale is a domain of MSHQ to assess erectile dysfunction. ES is the sum of score for questions 1 to 3. The score ranges from 0 (no erection) to 15 (strong erection). Change from BL at the scheduled post-baseline time points were analyzed using MMRM analysis method with an Observed Cases approach. Values are expressed as adjusted mean along with standard error. The MMRM analysis included fixed categorical effects of treatment, visit and treatment by visit interaction and the continuous fixed covariates of BL total score and BL score by visit interaction. BL is defined as earliest DB treatment start date if the par. took at least one dose of DB study drug; change from BL was calculated as Month 1, 3, 6, 9 and 12 values minus BL value(s). Only those par with non-missing change from baseline data were analysed (presented as n=X,X in the category titles) (NCT01777269)
Timeframe: Baseline and Month 1, 3, 6, 9 and 12
| Intervention | Scores on a scale (Least Squares Mean) | ||||
|---|---|---|---|---|---|
| Month 1, n=209, 215 | Month 3, n= 202, 208 | Month 6, n= 193, 188 | Month 9, n=182, 169 | Month 12, n= 175, 168 | |
| Duodart | -0.5 | -0.7 | -1.0 | -1.2 | -1.0 |
| Placebo | -0.3 | -0.5 | -0.6 | -0.5 | -0.5 |
Blood samples for DHT analysis was collected at Baseline, Week 26 and Week 52. DHT values at a lower limit of quantification (LLQ) were imputed using 1/2 LLQ. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). The LOCF method for missing data was used by carrying forward the last non-missing post-Baseline assessment for participants with missing visit data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 26 and Week 52
| Intervention | nanomole per liter (nmol/L) (Mean) | ||
|---|---|---|---|
| Baseline, n=120 | Week 26 LOCF, n=118 | Week 52 LOCF, n=118 | |
| Dutasteride 0.5 mg | 1.55 | 0.19 | 0.17 |
The DLQI is a 10-item validated measure developed specifically to assess quality of life (QoL) in participants with dermatological conditions. It assesses six domains: symptoms and feelings, daily activities, leisure, work ⁄school, personal relationships, and treatment. The DLQI total is the sum of 10 questions, each ranging from 0 (unanswered/not relevant,not at all) to 3 (very much). The higher the score, the greater the impairment of (QoL). Change from Baseline in DLQI scores is defined as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). The LOCF method for missing data was used by carrying forward the last non-missing post-Baseline assessment for participants with missing data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 13, Week 26, Week 39, and Week 52
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| Week 13 LOCF | Week 26 LOCF | Week 39 LOCF | Week 52 LOCF | |
| Dutasteride 0.5 mg | -0.15 | -0.25 | -0.27 | -0.23 |
The Problem Assessment Scale of the Sexual Function Inventory (PAS SFI) questionnaire was used to assess participant-perceived problems in sexual function using 3 questions assessing problems with sex drive, erections and ejaculation. They are scored on a 5-point scale of 0 to 4 (0=big problem, 1= medium problem, 2=small problem, 3=very small problem, 4=no problem). Total scores range from 0-12. Change from Baseline in PAS SFI scores is defined as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). The LOCF method for missing data was used by carrying forward the last non-missing post-Baseline assessment for participants with missing data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 13, Week 26, Week 39 and Week 52
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| Week 13 LOCF | Week 26 LOCF | Week 39 LOCF | Week 52 LOCF | |
| Dutasteride 0.5 mg | -0.6 | -0.7 | -0.3 | -0.3 |
Target area hair count is based on the nonvellus hair(>= 30 micrometer[μm] in width) count within a target 2.54cm(1 inch) diameter circle at the vertex and was assessed by macrophotographic technique. A cosmetic ink dot was placed by means of a tattoo at BL on the scalp in the center of the circle as a marker to guide the placement of the hair count area at subsequent time points. If the ink dot faded between study visits, it was redone. For the macrophotography, hair was clipped before each photograph. Change from BL is defined as post-BL value minus BL value. The BL value is defined as the latest assessment on or before the BL date(latest non-missing value of either treatment start date or randomization date). The last observation carried forward(LOCF) method for missing data was used by carrying forward the last non-missing post-BL assessment value for participants with missing data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 26, and Week 52
| Intervention | Hair count (Mean) | |
|---|---|---|
| Week 26 LOCF | Week 52 LOCF | |
| Dutasteride 0.5 mg | 87.3 | 68.1 |
Target area hair width was based on the total width of the nonvellus hairs(>=30μm in width) within a target 2.54cm(1 inch) diameter circle at the vertex and was assessed by macrophotographic technique. A cosmetic ink dot was placed by means of a tattoo at BL on the scalp in the center of the circle as a marker to guide the placement of the hair count area at subsequent time points. If the ink dot faded between study visits, it was redone. For the macrophotography, hair was clipped before each photograph. Change from BL is defined as the post-BL value minus the BL value. The BL value of an assessment is defined as the latest assessment on or before the BL date(latest non-missing value of either the treatment start date or the randomization date). The LOCF method for missing data was used by carrying forward the last non-missing post-BL assessment value for participants with missing data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 26, and Week 52
| Intervention | microns x 10^-3 (Mean) | |
|---|---|---|
| Week 26 LOCF | Week 52 LOCF | |
| Dutasteride 0.5 mg | 6.7 | 6.5 |
Terminal hair count was based on the terminal hair(>=60 μm in width) count within a target 2.54cm(1 inch) diameter circle at the vertex and was assessed by macrophotographic technique. A cosmetic ink dot was placed by means of a tattoo at BL on the scalp in the center of the circle as a marker to guide the placement of the hair count area at subsequent time points. If the ink dot faded between study visits, it was redone. For the macrophotography, hair was clipped before each photograph. Change from BL is defined as the post-BL value minus the BL value. BL value of an assessment is defined as the latest assessment on or before the BL date(latest non-missing value of either the treatment start date or the randomization date). The LOCF method for missing data was used by carrying forward the last non-missing post-BL assessment for participants with missing data and/or for participants who discontinued from the study. (NCT01831791)
Timeframe: Baseline, Week 26 and Week 52
| Intervention | Hair count (Mean) | |
|---|---|---|
| Week 26 LOCF | Week 52 LOCF | |
| Dutasteride 0.5 mg | 60.8 | 76.9 |
Blood samples were collected for the measurement of ALT, ALP and AST at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the ALT, ALP and AST values are summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Units per liter (U/L) (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| ALT, Week 26, n=114 | ALT, Week 52, n=111 | ALT, Final value, n=118 | ALP, Week 26, n=114 | ALP, Week 52, n=111 | ALP, Final value, n=118 | AST, Week 26, n=113 | AST, Week 52, n=108 | AST, Final value, n=118 | |
| Dutasteride 0.5 mg | 5.58 | 1.51 | 1.14 | 0.30 | 0.24 | 0.24 | 4.81 | 1.85 | 1.71 |
Vital sign monitoring included heart rate measurement at the Screening visit, Baseline visit, Weeks 13, 26, 39, and 52 visits and the early withdrawal visit if applicable. Change from Baseline in heart rate is summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline visit, Weeks 13, 26, 39, and 52 visits and or early withdrawal visit
| Intervention | Beats per minute (Mean) | ||||
|---|---|---|---|---|---|
| Week 13, n=120 | Week 26, n=116 | Week 39, n=112 | Week 52, n=111 | Final value, n=120 | |
| Dutasteride 0.5 mg | 0.3 | 0.6 | 2.7 | -0.3 | -0.6 |
Blood samples were collected for the measurement of hematocrit at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the hematocrit value is summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Proportion of red blood cells in blood (Mean) | ||
|---|---|---|---|
| Week 26, n=114 | Week 52, n=111 | Final value, n=118 | |
| Dutasteride 0.5 mg | -0.01 | 0.00 | -0.00 |
Blood samples were collected for the measurement of hemoglobin, albumin and total protein at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the hemoglobin, albumin and total protein values are summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Grams per liter (g/L) (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Hemoglobin, Week 26, n=114 | Hemoglobin, Week 52, n=111 | Hemoglobin, Final value, n=118 | Albumin, Week 26, n=114 | Albumin, Week 52, n=111 | Albumin, Final value, n=118 | Total protein, Week 26, n=114 | Total protein, Week 52, n=111 | Total protein, Final value, n=118 | |
| Dutasteride 0.5 mg | 0.61 | -0.94 | -0.69 | -0.64 | -1.42 | -1.31 | -0.17 | -0.55 | -0.40 |
Blood samples were collected for the measurement of platelet count and white blood cell count at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the platelet count and white blood cell count values are summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | 10^9 cells/Liter (GI/L) (Mean) | |||||
|---|---|---|---|---|---|---|
| Platelet count, Week 26, n=114 | Platelet count,Week 52, n=109 | Platelet count,Final value, n=118 | White blood cells count, Week 26, n=114 | White blood cells count, Week 52, n=111 | White blood cells count, Final value, n=118 | |
| Dutasteride 0.5 mg | 3.41 | -1.48 | -1.12 | 0.05 | 0.17 | 0.13 |
Blood samples were collected for the measurement of potassium, sodium, glucose and urea/BUN at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the potassium, sodium, glucose and urea/BUN values are summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Millimoles per liter (mmol/L) (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Potassium, Week 26, n=113 | Potassium,, Week 52, n=108 | Potassium, Final value, n=118 | Sodium, Week 26, n=114 | Sodium, Week 52, n=111 | Sodium, Final value, n=118 | Glucose, Week 26, n=114 | Glucose, Week 52, n=111 | Glucose, Final value, n=118 | Urea/BUN , Week 26, n=114 | Urea/BUN , Week 52, n=111 | Urea/BUN , Final value, n=118 | |
| Dutasteride 0.5 mg | 0.08 | 0.02 | 0.02 | 1.22 | 1.01 | 1.02 | 0.48 | 0.44 | 0.45 | 0.05 | 0.02 | 0.00 |
Blood samples were collected for the measurement of prostate-specific antigen at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the prostate-specific antigen value is summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Microgram per liter (µg/L) (Mean) | ||
|---|---|---|---|
| Week 26, n=116 | Week 52, n=111 | Final value, n=118 | |
| Dutasteride 0.5 mg | -0.29 | -0.32 | -0.32 |
Blood samples were collected for the measurement of the red blood cell count at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the red blood cell count value is summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | 10^12 cells per liter (TI/L) (Mean) | ||
|---|---|---|---|
| Week 26, n=114 | Week 52, n=111 | Final value, n=118 | |
| Dutasteride 0.5 mg | -0.01 | 0.01 | 0.01 |
Blood pressure measurements were taken to observe vital signs and included systolic blood pressure (SBP) and diastolic blood pressure (DBP) at the Screening visit, Baseline visit, Weeks 13, 26, 39, and 52 visits and the early withdrawal visit if applicable. Change from Baseline in SBP and DBP is summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Weeks 13, 26, 39, and 52 visits and or early withdrawal visit
| Intervention | Millimeters of mercury (mmHg) (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| SBP, Week 13, n=120 | SBP, Week 26, n=116 | SBP, Week 39, n=112 | SBP, Week 52, n=111 | SBP, Final value, n=120 | DBP, Week 13, n=120 | DBP, Week 26, n=116 | DBP, Week 39, n=112 | DBP, Week 52, n=111 | DBP, Final value, n=120 | |
| Dutasteride 0.5 mg | -0.3 | 0.9 | 0.9 | -1.3 | -1.0 | -1.3 | 1.9 | 0.4 | -0.3 | -0.6 |
Blood samples were collected for the measurement of total bilirubin and creatinine at Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. Change from Baseline in the total bilirubin and creatinine values are summarized for each post-Baseline assessment as well as for the final assessment (the last post-Baseline value in the study [final value]). Change from Baseline was calculated as the post-Baseline value minus the Baseline value. The Baseline value of an assessment is defined as the latest assessment on or before the Baseline date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Micromoles per liter (µmol/L) (Mean) | |||||
|---|---|---|---|---|---|---|
| Total bilirubin, Week 26, n=114 | Total bilirubin,, Week 52, n=111 | Total bilirubin, Final value, n=118 | Creatinine, Week 26, n=114 | Creatinine, Week 52, n=111 | Creatinine, Final value, n=118 | |
| Dutasteride 0.5 mg | -0.99 | -0.23 | -0.26 | -1.14 | 1.73 | 1.29 |
A central panel of 3 dermatologists independently assessed change in hair growth from Baseline to Week 26 and Week 52 using a 7-point scale: greatly decreased (-3), moderately decreased (-2), slightly decreased (-1), no change (0), slightly increased (1), moderately increased (2), and greatly increased (3). The median score, across the 3 panel members, is summarized. This assessment was performed by comparing the global photographs obtained at Baseline (Screening) with those subsequently obtained at Week 26 and Week 52. This assessment was made separately based on the global photography of the vertex and frontal views. The LOCF method for missing data was used for the assessment, if a participants was missing the Week 26 global photograph, but has a global photograph from an earlier assessment (i.e., a withdrawal visit), then that photograph was assessed during the panel review. (NCT01831791)
Timeframe: Baseline, Week 26 and Week 52
| Intervention | Scores on a scale (Mean) | |||
|---|---|---|---|---|
| Week 26 LOCF, vertex view | Week 26 LOCF, frontal view | Week 52 LOCF, vertex view | Week 52 LOCF, frontal view | |
| Dutasteride 0.5 mg | 1.34 | 1.21 | 1.50 | 1.40 |
The C-SSRS captures occurrence, severity, and frequency of suicide-related thoughts and behaviors. The number of participants answering yes/no responses to questions about suicidal ideation (Question [Que] 1 and Que 2) at Baseline and post-Baseline (since last visit) and suicidal behaviors (Que 6 - Que 10) at post-Baseline (since last visit) are presented. Questions included the presence (yes) or absence (no) of the following: Que 1 - a wish to be dead; Que 2 - nonspecific (NS) active suicidal thoughts; Que 6 - preparatory acts or behavior; Que 7 - aborted attempt; Que 8 - interrupted attempt (int. att.); Que 9 - non-fatal actual suicide attempt; Que 10 - completed suicide and non-suicidal self-injurious behavior. Final assessment (FA) is the last post-Baseline measurement during the study. (NCT01831791)
Timeframe: Baseline, Week 26 and Week 52
| Intervention | Participants (Number) | |||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BL, wish to be dead, n=103 | BL, NS active suicidal thoughts, n=103 | Week 26, wish to be dead, n=116 | Week 26, NS active suicidal thoughts, n=116 | Week 26 preparatory acts or behavior, n=116 | Week 26, aborted attempt, n=116 | Week 26, int. att., n=116 | Week 26, non-fatal actual suicide attempt, n=116 | Week 26, completed suicide, n=116 | Week 26, non-suicidal self-injurious, n=116 | Week 52, wish to be dead, n=111 | Week 52, NS active suicidal thoughts, n=111 | Week 52 preparatory acts or behavior, n=111 | Week 52, aborted attempt, n=111 | Week 52, interrupted attempt n=111 | Week 52, non-fatal actual suicide attempt, n=111 | Week 52, completed suicide, n=111 | Week 52, non-suicidal self-injurious, n=111 | FA, wish to be dead, n=118 | FA, NS active suicidal thoughts, n=118 | FA preparatory acts or behavior, n=118 | FA, aborted attempt, n=118 | FA, int. att., n=118 | FA, non-fatal actual suicide attempt, n=118 | FA, completed suicide, n=118 | FA, non-suicidal self-injurious, n=118 | |
| Dutasteride 0.5 mg | 2 | 0 | 2 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 3 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
An AE is defined as any untoward medical occurrence in a participant temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. An AE can therefore be any unfavorable and unintended sign(including an abnormal laboratory finding), symptom, or disease(new or exacerbated) temporally associated with the use of a medicinal product. A SAE is defined as any untoward medical occurrence that, at any dose, results in death, is life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, a congenital anomaly/birth defect, important medical events that jeopardize the participants or may require medical or surgical intervention to prevent one of the other outcomes listed in the above definition, drug-induced liver injury, breast cancer in male participants, prostate cancer, spontaneous abortion in female partner of male participants (NCT01831791)
Timeframe: From Baseline (Week 0) until Week 52
| Intervention | Participants (Number) | |
|---|---|---|
| Any AE | Any SAE | |
| Dutasteride 0.5 mg | 64 | 2 |
Blood samples for the assessment of the indicated laboratory parameters were taken at the Baseline, Week 26 and Week 52 visits and the early withdrawal visit where applicable. The laboratory parameters included ALP, ALT, AST, total bilirubin, total protein, sodium, potassium, albumin, glucose, creatinine, urea/BUN, hemoglobin, hematocrit, red blood cell (RBC) count, platelet count, white blood cell (WBC) count, and prostate-specific antigen (PSA). A laboratory value (LV) that is within the normal range is considered normal. A LV that is above the upper limit of the normal range is considered high abnormal. A LV that is below the lower limit of the normal range is considered low abnormal. Number of participants with any LV shifts from BL at any time post-BL are presented for, normal at BL to abnormal; normal at BL to high; normal at BL to low; normal or low at BL to high; normal or high at BL to low. (NCT01831791)
Timeframe: Baseline, Week 26 and 52 visits and/or early withdrawal visit
| Intervention | Participants (Number) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Hemoglobin, normal at BL to abnormal, n=98 | Hematocrit, normal at BL to abnormal, n=95 | Platelet count, normal at BL to abnormal, n=118 | RBC count, normal at BL to abnormal, n=99 | WBC count, normal at BL to abnormal, n=117 | Albumin, normal at BL to abnormal, n=116 | ALP, normal at BL to abnormal, n=118 | ALT, normal at BL to abnormal, n=116 | AST, normal at BL to abnormal, n=118 | Total Bilirubin, normal at BL to abnormal, n=104 | Creatinine, normal at BL to abnormal, n=99 | Glucose, normal at BL to abnormal, n=116 | Potassium, normal at BL to abnormal, n=118 | Total Protein, normal at BL to abnormal, n=118 | Sodium, normal at BL to abnormal, n=118 | Urea/BUN, normal at BL to abnormal, n=116 | PSA, normal at BL to abnormal, n=118 | Hemoglobin, normal at BL to high, n=98 | Hematocrit, normal at BL to high, n=95 | Platelet count, normal at BL to high, n=118 | RBC count, normal at BL to high, n=99 | WBC count, normal at BL to high, n=117 | Albumin, normal at BL to high, n=116 | ALP, normal at BL to high, n=118 | ALT, normal at BL to high, n=116 | AST, normal at BL to high, n=118 | Total Bilirubin, normal at BL to high, n=104 | Creatinine, normal at BL to high, n=99 | Glucose, normal at BL to high, n=116 | Potassium, normal at BL to high, n=118 | Total Protein, normal at BL to high, n=118 | Sodium, normal at BL to high, n=118 | Urea/BUN, normal at BL to high, n=116 | PSA, normal at BL to high, n=118 | Hemoglobin, normal at BL to low, n=98 | Hematocrit, normal at BL to low, n=95 | Platelet count, normal at BL to low, n=118 | RBC count, normal at BL to low, n=99 | WBC count, normal at BL to low, n=117 | Albumin, normal at BL to low, n=116 | ALP, normal at BL to low, n=118 | ALT, normal at BL to low, n=116 | AST, normal at BL to low, n=118 | Total Bilirubin, normal at BL to low, n=104 | Creatinine, normal at BL to low, n=99 | Glucose, normal at BL to low, n=116 | Potassium, normal at BL to low, n=118 | Total Protein, normal at BL to low, n=118 | Sodium, normal at BL to low, n=118 | Urea/BUN, normal at BL to low, n=116 | PSA, normal at BL to low, n=118 | Hemoglobin, normal or low at BL to high, n=118 | Hematocrit, normal or low at BL to high, n=106 | Platelet count, normal or low at BL to high, n=118 | RBC count, normal or low at BL to high, n=118 | WBC count, normal or low at BL to high, n=118 | Albumin, normal or low at BL to high, n=116 | ALP, normal or low at BL to high, n=118 | ALT, normal or low at BL to high, n=116 | AST, normal or low at BL to high, n=118 | Total Bilirubin, normal or low at BL to high n=104 | Creatinine, normal or low at BL to high, n=118 | Glucose, normal or low at BL to high, n=117 | Potassium, normal or low at BL to high, n=118 | Total Protein, normal or low at BL to high, n=118 | Sodium, normal or low at BL to high, n=118 | Urea/BUN, normal or low at BL to high, n=117 | PSA, normal or low at BL to high, n=118 | Hemoglobin, normal or high at BL to low, n=98 | Hematocrit, normal or high at BL to low, n=107 | Platelet count, normal or high at BL to low, n=118 | RBC count, normal or high at BL to low, n=99 | WBC count, normal or high at BL to low, n=117 | Albumin, normal or high at BL to low, n=118 | ALP, normal or high at BL to low, n=118 | ALT, normal or high at BL to low, n=118 | AST, normal or high at BL to low, n=118 | Total Bilirubin, normal or high at BL to low,n=118 | Creatinine, normal or high at BL to low, n=99 | Glucose, normal or high at BL to low, n=117 | Potassium, normal or high at BL to low, n=118 | Total Protein, normal or high at BL to low, n=118 | Sodium, normal or high at BL to low, n=118 | Urea/BUN, normal or high at BL to low, n=117 | PSA, normal or high at BL to low, n=118 | |
| Dutasteride 0.5 mg | 8 | 8 | 0 | 11 | 3 | 0 | 1 | 7 | 6 | 5 | 10 | 14 | 0 | 2 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 3 | 0 | 1 | 7 | 6 | 5 | 0 | 14 | 0 | 0 | 1 | 0 | 1 | 8 | 8 | 0 | 11 | 0 | 0 | 0 | 0 | 0 | 0 | 10 | 0 | 0 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 3 | 0 | 1 | 7 | 6 | 5 | 0 | 14 | 0 | 0 | 1 | 0 | 1 | 8 | 8 | 0 | 11 | 0 | 0 | 0 | 0 | 0 | 0 | 10 | 0 | 0 | 2 | 0 | 0 | 0 |
A qualitative breast examination was performed at Baseline (Week 0), at the Week 26 Visit and at the Week 52 Visit (and at the early withdrawal visit, if applicable). Participants were assessed for presence (reported as yes) and absence (reported as no) of palpable breast tissue (PBT) or nipple tenderness (NT) and/or clinically significant (CS) PBT or NT at Baseline (BL), at each scheduled Post-BL assessment. Change from BL in breast examination results included the number of participants with change from 'no (N)' at BL to 'yes (Y)' at any Post-BL assessment for the presence of PBT or NT, and the number of participants with change from N at BL in CS to Y at any Post-BL assessment in CS for PBT and for NT. BL value of an assessment is defined as the latest assessment on or before the BL date (latest non-missing value of either the treatment start date or the randomization date). (NCT01831791)
Timeframe: Baseline to Week 52
| Intervention | Participants (Number) | |||||
|---|---|---|---|---|---|---|
| PBT, Change from N at BL to Y, n=120 | PBT, CS, Y (among change from N at BL to Y), n=0 | PBT, CS, N (among change from N at BL to Y), n=0 | NT, Change from N at BL to Y, n=120 | NT, CS, Y (among change from N at BL to Y), n=1 | NT, CS, N (among change from N at BL to Y), n=0 | |
| Dutasteride 0.5 mg | 0 | 0 | 0 | 1 | 1 | 0 |
An AE is considered drug-related if the relationship variable indicates so, or if the variable value is missing. Any AE with a start date on or after the treatment start date and on or before the last dose of treatment is considered on-treatment (treatment-emergent). This includes an AE with a missing onset date. Any AE which occurred, in the investigator's judgement and is possibly related to suicidality, is defined as possible suicidality-related adverse event (PSRAE). Suicidality was assessed by using the columbia-suicide severity rating scale (C-SSRS) as determined by the investigator. The C-SSRS captures occurrence, severity, and frequency of suicide-related thoughts and behaviors. (NCT01831791)
Timeframe: From Baseline (Week 0) until Week 52
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Any drug related AEs | Any treatment-emergent AEs | Any AE leading to study drug discontinuation | Any PSRAE | |
| Dutasteride 0.5 mg | 20 | 64 | 0 | 3 |
"The investigator/designee assessed the stage (Stage I to Stage VII) of AGA (i.e., male pattern baldness [MPB]) by utilizing the Norwood-Hamilton scale, used to measure the progression of MPB. Stage VII indicates worse balding than Stage I. Assessment was made by direct visual examination (aided by pictures) of the participant at Screening (Baseline), Week 26, and Week 52. v, vertex; most of the hair loss (commonly seen with advancing age) is on the vertex. a, type a variant; major features are (1) the entire anterior hairline border recedes in unison; (2) there is no simultaneous balding of the vertex. The number of participants with stage changes from Baseline are summarized. The LOCF method for missing data was used by carrying forward the last non-missing post-Baseline assessment for participants with missing data and/or for participants who discontinued from the study." (NCT01831791)
Timeframe: Baseline, Week 26 and Week 52
| Intervention | Participants (Number) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline BL Stage IIIv to W26 Stage I, n=53 | BL Stage IIIv to W26 Stage II, n=53 | BL Stage IIIv to W26 Stage IIa, n=53 | BL Stage IIIv to W26 Stage III, n=53 | BL Stage IIIv to W26 Stage IIIa, n=53 | BL Stage IIIv to W26 Stage IIIv, n=53 | BL Stage IIIv to W26 Stage IV, n=53 | BL Stage IIIv to W26 Stage IVa, n=53 | BL Stage IIIv to W26 Stage V, n=53 | BL Stage IIIv to W26 Stage Va, n=53 | BL Stage IIIv to W26 Stage VI, n=53 | BL Stage IV to W26 Stage I, n=46 | BL Stage IV to W26 Stage II, n=46 | BL Stage IV to W26 Stage IIa, n=46 | BL Stage IV to W26 Stage III, n=46 | BL Stage IV to W26 Stage IIIa, n=46 | BL Stage IV to W26 Stage IIIv, n=46 | BL Stage IV to W26 Stage IV, n=46 | BL Stage IV to W26 Stage IVa, n=46 | BL Stage IV to W26 Stage V, n=46 | BL Stage IV to W26 Stage Va, n=46 | BL Stage IV to W26 Stage VI, n=46 | BL Stage V to W26 Stage I, n=19 | BL Stage V to W26 Stage II, n=19 | BL Stage V to W26 Stage IIa, n=19 | BL Stage V to W26 Stage III, n=19 | BL Stage V to W26 Stage IIIa, n=19 | BL Stage V to W26 Stage IIIv, n=19 | BL Stage V to W26 Stage IV, n=19 | BL Stage V to W26 Stage IVa, n=19 | BL Stage V to W26 Stage V, n=19 | BL Stage V to W26 Stage Va, n=19 | BL Stage V to W26 Stage VI, n=19 | BL Stage IIIv to W52 Stage I, n=53 | BL Stage IIIv to W52 Stage II, n=53 | BL Stage IIIv to W52 Stage IIa, n=53 | BL Stage IIIv to W52 Stage III, n=53 | BL Stage IIIv to W52 Stage IIIa, n=53 | BL Stage IIIv to W52 Stage IIIv, n=53 | BL Stage IIIv to W52 Stage IV, n=53 | BL Stage IIIv to W52 Stage IVa, n=53 | BL Stage IIIv to W52 Stage V, n=53 | BL Stage IIIv to W52 Stage Va, n=53 | BL Stage IIIv to W52 Stage VI, n=53 | BL Stage IV to W52 Stage I, n=46 | BL Stage IV to W52 Stage II, n=46 | BL Stage IV to W52 Stage IIa, n=46 | BL Stage IV to W52 Stage III, n=46 | BL Stage IV to W52 Stage IIIa, n=46 | BL Stage IV to W52 Stage IIIv, n=46 | BL Stage IV to W52 Stage IV, n=46 | BL Stage IV to W52 Stage IVa, n=46 | BL Stage IV to W52 Stage V, n=46 | BL Stage IV to W52 Stage Va, n=46 | BL Stage IV to W52 Stage VI, n=46 | BL Stage V to W52 Stage I, n=19 | BL Stage V to W52 Stage II, n=19 | BL Stage V to W52 Stage IIa, n=19 | BL Stage V to W52 Stage III, n=19 | BL Stage V to W52 Stage IIIa, n=19 | BL Stage V to W52 Stage IIIv, n=19 | BL Stage V to W52 Stage IV, n=19 | BL Stage V to W52 Stage IVa, n=19 | BL Stage V to W52 Stage V, n=19 | BL Stage V to W52 Stage Va, n=19 | BL Stage V to W52 Stage VI, n=19 | |
| Dutasteride 0.5 mg | 0 | 0 | 2 | 4 | 0 | 45 | 2 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 15 | 29 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 1 | 0 | 3 | 10 | 0 | 5 | 0 | 0 | 1 | 2 | 4 | 14 | 0 | 28 | 4 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 19 | 26 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 2 | 0 | 4 | 10 | 0 | 3 | 0 | 0 |
Assessment of suicidality were done through use of the Columbia Suicide Severity Rating Scale (C-SSRS) for suicidal ideation with the ratings 1 to 5 (1. wish to be dead, 2. Non-specific suicidal thoughts, 3..without intent, 4. with intent but no plan, 5. with plan and intent) and for suicidal behavior with the ratings 6 to 9 (6.Prep acts/behavior, 7.aborted attempt, 8. interrupted attempt and 9. actual attempt). C-SSRS was administered at Day 1, Week 12, Week 24, and the early withdrawal visit if applicable . (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Wish to be dead | Non-specific suicidal thoughts | Without intent | With intent but no plan | With plan and intent | Prep acts/behavior | Aborted attempt | Interrupted attempt | Actual attempt | Non-suicidal self injury behavior | |
| Dutasteride 0.5 mg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Assessment of suicidality were done through use of the Columbia Suicide Severity Rating Scale (C-SSRS) for suicidal ideation with the ratings 1 to 5 (1. wish to be dead, 2. Non-specific suicidal thoughts, 3. without intent, 4. with intent but no plan, 5. with plan and intent) and for suicidal behavior with the ratings 6 to 9 (6.Prep acts/behavior, 7.aborted attempt, 8. interrupted attempt and 9. actual attempt). C-SSRS was administered at Day 1, Week 12, Week 24, and the early withdrawal visit if applicable . (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Wish to be dead | Non-specific suicidal thoughts | Without intent | With intent but no plan | With plan and intent | Prep acts/behavior | Aborted attempt | Interrupted attempt | Actual attempt | Non-suicidal self injury behavior | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
The Baseline blood presssure assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | millimeter of mercury (mmHg) (Mean) | |||
|---|---|---|---|---|
| SBP Week 12, n=59, 53 | SBP Week 24, n=57, 52 | DBP Week 12, n=59, 53 | DBP Week 24, n=57, 52 | |
| Dutasteride 0.5 mg | -0.1 | -2.0 | 1.6 | -1.5 |
| Placebo | 0.9 | -1.0 | 2.1 | -0.2 |
The HGSS assessed participants satisfaction with hair appearance and growth by scoring 5 questions on a 7-point scale ranging from 1=very dissatisfied to 7=very satisfied with a maximum score of 35. The Baseline assessment was defined as the latest assessment on or before the OL treatment start. Change from Baseline is post-Baseline value minus Baseline value. A decrease from Baseline indicates a worsening. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Scores on a Scale (Mean) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 4.5 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 4.5 |
The DLQI was a 10-item questionnaire designed to evaluate the effect of skin conditions (alopecia) on the participants quality of life. Each item was scored on a 4-point scale ranging from 0 to 3 with a maximum score of 30. Higher scores represent greater impairment in quality of life. The Baseline assessment was defined as the latest assessment on or before the OL treatment start. Change from Baseline is post-Baseline value minus Baseline value. (NCT02014584)
Timeframe: Baseline and Upto Week 24
| Intervention | Scores on a Scale (Mean) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -1.0 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -0.8 |
Participants were referred as premature discontinuations if they do not complete the double-blind period. The reasons for premature withdrawal were protocol deviation, lost to follow-up and withdrawal of consent by participants. (NCT02014584)
Timeframe: Week 24
| Intervention | Participants (Number) |
|---|---|
| Placebo | 2 |
| Dutasteride 0.5 mg | 6 |
Participants were referred as premature discontinuations if they do not complete the open-label treatment period. The reasons for premature withdrawal were protocol deviation, lost to follow-up and withdrawal of consent by participants. (NCT02014584)
Timeframe: Week 48
| Intervention | Participants (Number) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 5 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 1 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Participants (Number) |
|---|---|
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo | 0 |
| Dutasteride 0.5 mg | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo | 5 |
| Dutasteride 0.5 mg | 9 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Participants (Number) |
|---|---|
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 10 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 3 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 2 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Treatment related AE included events which the investigator classified as having a reasonable possibility of being caused by the investigational product or whose classification was missing. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Participants (Number) |
|---|---|
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 11 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Treatment related AE included events which the investigator classified as having a reasonable possibilty of being caused by the investigational product or whose classification was missing. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 4 |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 2 |
Clinical chemistry parameters included: albumin and total protein at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | G/L (Mean) | |||
|---|---|---|---|---|
| Albumin OL Week 24, n=44, 47 | Albumin Final Value, n=44, 47 | Total Protein OL Week 24, n=44, 47 | Total Protein Final Value, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -1.1 | -1.1 | -2.4 | -2.4 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -0.6 | -0.5 | -0.8 | -0.7 |
The Baseline heart rate assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | Beats per Minute (Mean) | |
|---|---|---|
| Week 12, n=59, 53 | Week 24, n=57, 52 | |
| Dutasteride 0.5 mg | -0.6 | -0.7 |
| Placebo | 0.3 | 0.6 |
Baseline heart rate assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | Beats per Minute (Mean) | |
|---|---|---|
| Week 12, n=46, 48 | Week 24, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 1.1 | 1.2 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -1.5 | -0.3 |
The HGSS assessed participants satisfaction with hair appearance and growth by scoring 5 questions on a 7-point scale ranging from 1=very dissatisfied to 7= very satisfied with a maximum score of 35. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. A decrease from Baseline indicates a worsening. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | Scores on a Scale (Least Squares Mean) | |
|---|---|---|
| DB Week 12, n= 58, 53 | DB Week 24, n=57, 52 | |
| Dutasteride 0.5 mg | 2.4 | 3.2 |
| Placebo | 1.3 | -0.1 |
The global assessment questions consist of 2 questions, recording how much the participant perceives his sexual life has changed and how he perceives his ability to achieve and maintain erections has changed, compared to how it was before he began receiving treatment in this study. The wording of these questions were based on the Patient Global Impression of Improvement questionnaire, which was validated for use in the assessment of improvement in stress urinary incontinence. The questions were scored on a 7-point scale.The Baseline assessment was defined as the latest assessment on or before the DB treatment start. (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline, Erection ability, Very Much Better | Baseline, Erection ability, Much Better | Baseline, Erection ability, A Little Better | Baseline, Erection ability, No change | Baseline, Erection ability, A Little Worse | Baseline, Erection ability, Much worse | Baseline, Erection ability, Very Much Worse | Baseline, Sexual life, Very Much Better | Baseline, sexual life, Much Better | Baseline, sexual life, A Little Better | Baseline, sexual life, No change | Baseline, sexual life, A Little Worse | Baseline, sexual life, Much worse | Baseline, sexual life, Very Much Worse | DB week 24, Erection ability, Very Much Better | DB week 24, Erection ability, Much Better | DB week 24, Erection ability, A Little Better | DB week 24, Erection ability, No change | DB week 24, Erection ability, A Little Worse | DB week 24, Erection ability, Much worse | DB week 24, Erection ability, Very Much Worse | DB week 24, Sexual life, Very Much Better | DB week 24, sexual life, Much Better | DB week 24, sexual life, A Little Better | DB week 24, sexual life, No change | DB week 24, sexual life, A Little Worse | DB week 24, sexual life, Much worse | DB week 24, sexual life, Very Much Worse | |
| Dutasteride 0.5 mg | 0 | 1 | 1 | 55 | 1 | 0 | 0 | 0 | 1 | 0 | 56 | 1 | 0 | 0 | 0 | 0 | 4 | 40 | 7 | 1 | 0 | 0 | 1 | 2 | 39 | 9 | 1 | 0 |
| Placebo | 0 | 1 | 1 | 54 | 3 | 0 | 0 | 0 | 1 | 1 | 55 | 2 | 0 | 0 | 1 | 0 | 2 | 49 | 5 | 0 | 0 | 1 | 0 | 3 | 47 | 6 | 0 | 0 |
The global assessment questions consist of 2 questions, recording how much the participant perceives his sexual life has changed and how he perceives his ability to achieve and maintain erections has changed, compared to how it was before he began receiving treatment in this study. The wording of these questions were based on the Patient Global Impression of Improvement questionnaire, which was validated for use in the assessment of improvement in stress urinary incontinence. The questions were scored on a 7-point scale.The Baseline assessment was defined as the latest assessment on or before the OL treatment start. (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| OL Baseline, Erection ability, Very Much Better | OL Baseline, Erection ability, Much Better | OL Baseline, Erection ability, A Little Better | OL Baseline, Erection ability, No change | OL Baseline, Erection ability, A Little Worse | OL Baseline, Erection ability, Much worse | OL Baseline, Erection ability, Very Much Worse | OL Baseline, Sexual life, Very Much Better | OL Baseline, sexual life, Much Better | OL Baseline, sexual life, A Little Better | OL Baseline, sexual life, No change | OL Baseline, sexual life, A Little Worse | OL Baseline, sexual life, Much worse | OL Baseline, sexual life, Very Much Worse | OL week 24, Erection ability, Very Much Better | OL week 24, Erection ability, Much Better | OL week 24, Erection ability, A Little Better | OL week 24, Erection ability, No change | OL week 24, Erection ability, A Little Worse | OL week 24, Erection ability, Much worse | OL week 24, Erection ability, Very Much Worse | OL week 24, Sexual life, Very Much Better | OL week 24, sexual life, Much Better | OL week 24, sexual life, A Little Better | OL week 24, sexual life, No change | OL week 24, sexual life, A Little Worse | OL week 24, sexual life, Much worse | OL week 24, sexual life, Very Much Worse | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 | 0 | 4 | 39 | 5 | 0 | 0 | 0 | 1 | 2 | 39 | 6 | 0 | 0 | 0 | 0 | 4 | 37 | 5 | 0 | 0 | 0 | 1 | 2 | 39 | 4 | 0 | 0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 1 | 0 | 1 | 42 | 5 | 0 | 0 | 1 | 0 | 2 | 40 | 6 | 0 | 0 | 0 | 2 | 1 | 35 | 6 | 0 | 0 | 0 | 2 | 1 | 37 | 4 | 0 | 0 |
Baseline blood presure assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | mmHg (Mean) | |||
|---|---|---|---|---|
| SBP Week 12, n=46, 48 | SBP Week 24, n=44, 47 | DBP Week 12, n=46, 48 | DBP Week 24, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0.1 | 0.4 | -0.6 | 0.9 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -0.9 | -0.7 | -0.8 | -1.4 |
Clinical chemistry parameters included: creatinine, direct bilirubin, total bilirubin at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | UMOL/L (Mean) | |||||
|---|---|---|---|---|---|---|
| Creatinine OL Week 24, n=44, 47 | Creatinine Final Value, n=44, 47 | Direct bilirubin OL Week 24, n=44, 47 | Direct bilirubin Final Value, n=44, 47 | Total bilirubin OL Week 24, n=44, 47 | Total bilirubin Final Value, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -0.2 | -0.2 | 0.1 | 0.1 | 0.4 | 0.4 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 1.1 | 1.2 | 0.1 | 0.1 | 0.9 | 1.0 |
Clinical chemistry parameters included: alanine aminotransferase (ALT), alkaline phosphatase (ALP), aspartate aminotransferase (AST) and gamma glutamyl transferase (GGT) at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | IU/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| ALT DB Week 24, n=57, 52 | ALT Final Value, n=58, 53 | ALP DB Week 24, n=57, 52 | ALP Final Value, n=58, 53 | AST DB Week 24, n=57, 51 | AST Final Value, n=58, 52 | GGT DB Week 24, n=57, 52 | GGT Final Value, n=58, 53 | |
| Dutasteride 0.5 mg | 4.0 | 3.5 | -4.1 | -4.5 | 0.5 | 0.3 | -1.1 | -1.1 |
| Placebo | 0.9 | 1.0 | -4.8 | -4.8 | 0.7 | 0.6 | -6.4 | -6.3 |
The Baseline blood presssure assessment was defined as the latest assessment on or before the open-label treatment start. The clinical concern range for vital signs was defined as: systolic blood pressure (lower: <80, upper: >165) and diastolic blood pressure: (lower: <40, upper: >105). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline SBP <80 mmHg | Baseline SBP >165 mmHg | Baseline DBP <40 mmHg | Baseline DBP >105 mmHg | Post Baseline SBP <80 mmHg | Post Baseline SBP >165 mmHg | Post Baseline DBP <40 mmHg | Post Baseline DBP >105 mmHg | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Clinical chemistry parameters included: albumin and total protein at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | G/L (Mean) | |||
|---|---|---|---|---|
| Albumin, DB Week 24, n=57, 52 | Albumin, Final Value, n=58, 53 | Total Protein, DB Week 24, n=57, 52 | Total Protein, Final Value, n=58, 53 | |
| Dutasteride 0.5 mg | -0.1 | -0.1 | -0.0 | 0.1 |
| Placebo | 0.2 | 0.2 | -0.1 | -0.1 |
Clinical chemistry parameters included: creatinine, direct bilirubin, total bilirubin at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | UMOL/L (Mean) | |||||
|---|---|---|---|---|---|---|
| Creatinine DB Week 24, n=57, 52 | Creatinine Final Value, n=58, 53 | Direct bilirubin DB Week 24, n=57, 52 | Direct bilirubin Final Value, n=58, 53 | Total bilirubin DB Week 24, n=57, 52 | Total bilirubin Final Value, n=58, 53 | |
| Dutasteride 0.5 mg | -0.7 | -0.8 | -0.3 | -0.2 | -1.1 | -1.0 |
| Placebo | 1.7 | 1.6 | -0.2 | -0.1 | -1.1 | -1.1 |
Clinical chemistry parameters included: glucose, potassium, sodium, and urea/BUN at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | MMOL/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Glucose DB Week 24, n=57, 52 | Glucose Final Value, n=58, 53 | Potassium DB Week 24, n=57, 51 | Potassium Final Value n=58, 52 | Sodium DB Week 24, n=57, 52 | Sodium Final Value, n=58, 53 | Urea/BUN Final Value, n=57, 52 | Urea/BUN Value, n=58, 53 | |
| Dutasteride 0.5 mg | 0.0 | 0.0 | 0.0 | 0.0 | 0.2 | 0.4 | 0.0 | 0.1 |
| Placebo | 0.1 | 0.1 | 0.0 | 0.0 | 0.5 | 0.5 | 0.2 | 0.2 |
Clinical chemistry parameters included: ALT, ALP, AST, and GGT at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | IU/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| ALT OL Week 24, n=44, 47 | ALT Final Value, n=44, 47 | ALP OL Week 24, n=44, 47 | ALP Final Value, n=44, 47 | AST OL Week 24, n=43, 47 | AST Final Value, n=44, 47 | GGT OL Week 24, n=44, 47 | GGT Final Value, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -1.7 | -1.7 | -3.3 | -3.3 | 0.1 | 0.1 | 0.6 | 0.6 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -1.4 | -1.3 | 0.0 | 0.0 | -0.2 | -0.5 | 3.7 | 3.7 |
Clinical chemistry parameters included: glucose, potassium, sodium, and urea/BUN at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | MMOL/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Glucose OL Week 24, n=44, 47 | Glucose Final Value, n=44, 47 | Potassium OL Week 24, n=43, 47 | Potassium Final Value, n=44, 47 | Sodium OL Week 24, n=44, 47 | Sodium Final Value, n=44, 47 | Urea/BUN OL Week 24, n=44, 47 | Urea/BUN Final Value, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0.2 | 0.2 | -0.0 | -0.0 | -0.6 | -0.6 | -0.1 | -0.1 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0.3 | 0.3 | -0.1 | -0.0 | -0.9 | -0.9 | 0.3 | 0.3 |
Hematology parameter included: hematocrit at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Proportion of RBCs (Mean) | |
|---|---|---|
| DB Week 24, n=55, 51 | Final Value, n=56, 52 | |
| Dutasteride 0.5 mg | 0.0 | 0.0 |
| Placebo | -0.0 | -0.0 |
Hematology parameter included: hemoglobin at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | G/L (Mean) | |
|---|---|---|
| DB Week 24, n=55, 51 | Final Value, n=56, 52 | |
| Dutasteride 0.5 mg | -0.8 | -0.8 |
| Placebo | -2.0 | -2.0 |
Hematology parameter included: RBC at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | T/L (Mean) | |
|---|---|---|
| DB Week 24, n=55, 51 | Final Value, n=56, 52 | |
| Dutasteride 0.5 mg | 0.0 | 0.0 |
| Placebo | -0.0 | -0.0 |
Hematology parameter included: hematocrit at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Proportion of RBCs (Mean) | |
|---|---|---|
| OL Week 24, n=43, 47 | Final Value, n=43, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0.0 | 0.0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0.0 | 0.0 |
Hematology parameters included: hemoglobin at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | G/L (Mean) | |
|---|---|---|
| OL Week 24, n=43, 47 | Final Value, n=43, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -1.4 | -1.4 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -1.5 | -1.5 |
Hematology parameter included: RBC at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | T/L (Mean) | |
|---|---|---|
| OL Week 24, n=43, 47 | Final Value, n=43, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -0.1 | -0.1 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | -0.1 | -0.1 |
Hematology parameters included: platelet count, white blood cell (WBC) count, basophils, eosinophils, lymphocytes, monocytes, segmented neutrophils and total neutrophils at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the double-blind treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Giga per Liter (GI/L) (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Platelet Count DB Week 24, n=54, 47 | Platelet Count Final Value, n=55, 48 | WBC DB Week 24, n=55, 51 | WBC Final Value, n=56, 52 | Basophils DB Week 24, n=50, 46 | Basophils Final Value, n=51, 47 | Eosinophils DB Week 24, n=50, 46 | Eosinophils Final Value, n=51, 47 | Lymphocytes DB Week 24, n=50, 46 | Lymphocytes Final Value, n=51, 47 | Monocytes DB Week 24, n=50, 46 | Monocytes Final Value, n=51, 47 | Segmented Neutrophils DB Week 24, n=50, 46 | Segmented Neutrophils Final Value, n=51, 47 | Total Neutrophils DB Week 24, n=50, 46 | Total Neutrophils Final Value, n=51, 47 | |
| Dutasteride 0.5 mg | 9.6 | 9.0 | 0.1 | 0.1 | -0.0 | -0.0 | -0.0 | -0.0 | -0.1 | -0.0 | -0.0 | -0.0 | 0.2 | 0.2 | 0.2 | 0.2 |
| Placebo | 2.2 | 2.3 | 0.1 | 0.1 | -0.0 | -0.0 | -0.0 | -0.0 | 0.0 | 0.1 | 0.0 | 0.0 | 0.1 | 0.1 | 0.1 | 0.1 |
Hematology parameters included: platelet count, white blood cell (WBC) count, basophils, eosinophils, lymphocytes, monocytes, segmented neutrophils, and total neutrophils at the indicated time points (Week 24 and final value). The Baseline assessment was defined as the latest assessment on or before the open-label treatment start. Change from Baseline is post-Baseline value minus Baseline value. A final value for each period is defined as the latest post-Baseline value available in the period. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Giga per Liter (GI/L) (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Platelet Count OL Week 24, n=42, 45 | Platelet Count Final Value, n=42, 45 | WBC OL Week 24, n=42, 47 | WBC Final Value, n=42, 47 | Basophils OL Week 24, n=39, 44 | Basophils Final Value, n=40, 44 | Eosinophils OL Week 24, n=39, 44 | Eosinophils Final Value, n=40, 44 | Lymphocytes OL Week 24, n=39, 44 | Lymphocytes Final Value, n=40, 44 | Monocytes OL Week 24, n=39, 44 | Monocytes Final Value, n=40, 44 | Segmented Neutrophils OL Week 24, n=39, 44 | Segmented Neutrophils Final Value, n=40, 44 | Total Neutrophils OL Week 24, n=39, 44 | Total Neutrophils Final Value, n=40, 44 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -2.5 | -3.4 | 0.2 | 0.1 | 0.0 | 0.0 | 0.0 | 0.0 | 0.1 | 0.1 | -0.0 | -0.0 | 0.0 | 0.0 | 0.0 | 0.0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 2.1 | 2.1 | 0.2 | 0.1 | -0.0 | -0.0 | -0.0 | -0.0 | -0.0 | -0.0 | -0.0 | -0.0 | 0.2 | 0.2 | 0.2 | 0.2 |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. Overall score range is 0-75. The erectile function score range is 0-30, intercourse satisfaction score range is 0-15, orgasmic function score range is 0-10, sexual desire score range is 0-10, overall satisfaction score range is 0-10. A decrease from Baseline indicates a worsening. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Scores on a Scale (Least Squares Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Erectile Function DB Week 4, n=56, 54 | Erectile Function DB Week 12, n= 59, 53 | Erectile Function DB Week 24, n=57, 52 | Intercourse satisfaction DB Week 4, n=56, 54 | Intercourse satisfaction DB Week 12, n=59, 53 | Intercourse satisfaction DB Week 24, n=57, 52 | Orgasmic function DB Week 4, n=56, 54 | Orgasmic function DB Week 12, n=59, 53 | Orgasmic function DB Week 24, n=57, 52 | Sexual desire DB Week 4, n=56, 54 | Sexual desire DB Week 12, n=59, 53 | Sexual desire DB Week 24, n=57, 52 | Overall sexual satisfaction DB Week 4, n=56, 54 | Overall sexual satisfaction DB Week 12, n=59, 53 | Overall sexual satisfaction DB Week 24, n=57, 51 | |
| Dutasteride 0.5 mg | -0.3 | -1.3 | -1.2 | 0.0 | -0.2 | -0.4 | 0.1 | -0.1 | -0.1 | -0.1 | -0.4 | -0.2 | 0.1 | -0.2 | -0.2 |
| Placebo | -0.5 | -0.5 | -0.5 | -0.3 | -0.1 | -0.3 | -0.0 | 0.0 | -0.0 | -0.4 | -0.2 | -0.2 | -0.1 | -0.1 | -0.1 |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. Overall score range is 0-75. The erectile function score range is 0-30, intercourse satisfaction score range is 0-15, orgasmic function score range is 0-10, sexual desire score range is 0-10, overall satisfaction score range is 0-10. A decrease from Baseline indicates a worsening. The Baseline assessment was defined as the latest assessment on or before the OL treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Scores on a Scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Erectile Function OL Week 4, n=47, 48 | Erectile Function OL Week 12, n= 46, 48 | Erectile Function OL Week 24, n=44, 47 | Intercourse satisfaction OL Week 4, n=47, 48 | Intercourse satisfaction OL Week 12, n= 46, 48 | Intercourse satisfaction OL Week 24, n=44, 47 | Orgasmic function OL Week 4, n=47, 48 | Orgasmic function OL Week 12, n= 46, 48 | Orgasmic function OL Week 24, n=44, 47 | Sexual desire OL Week 4, n=47, 48 | Sexual desire OL Week 12, n= 46, 48 | Sexual desire OL Week 24, n=44, 47 | Overall sexual satisfaction OL Week 4, n=47, 48 | Overall sexual satisfaction OL Week 12, n= 46, 48 | Overall sexual satisfaction OL Week 24, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | -0.1 | -0.3 | -1.4 | 0.0 | -0.1 | -0.5 | 0.1 | -0.1 | -0.4 | 0.0 | -0.1 | -0.1 | 0.1 | 0.2 | -0.1 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0.0 | -0.1 | 0.0 | 0.1 | -0.2 | -0.1 | 0.1 | 0.0 | 0.1 | 0.1 | -0.2 | -0.0 | 0.0 | -0.2 | -0.2 |
The DLQI was a 10-item questionnaire designed to evaluate the effect of skin conditions (alopecia) on the participants quality of life. Each item was scored on a 4-point scale ranging from 0 to 3 with a maximum score of 30. Higher scores represent greater impairment in quality of life. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 12 and Week 24
| Intervention | Scores on a Scale (Least Squares Mean) | |
|---|---|---|
| DB Week 12, n= 58, 53 | DB Week 24, n=57, 52 | |
| Dutasteride 0.5 mg | -0.4 | 0.2 |
| Placebo | 0.2 | 0.7 |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. Overall score range is 0-75. The erectile function score range is 0-30, intercourse satisfaction score range is 0-15, orgasmic function score range is 0-10, sexual desire score range is 0-10, overall satisfaction score range is 0-10. A decrease from Baseline indicates a worsening. The change from Baseline values are presented for Week 4, Week 12 and Week 24. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Scores on a Scale (Least Squares Mean) | ||
|---|---|---|---|
| DB Week 4, n=56, 54 | DB Week 12, n= 59, 53 | DB Week 24, n=57, 51 | |
| Dutasteride 0.5 mg | -0.0 | -2.2 | -1.2 |
| Placebo | -1.4 | -0.9 | -1.2 |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. Overall score range is 0-75. The erectile function score range is 0-30, intercourse satisfaction score range is 0-15, orgasmic function score range is 0-10, sexual desire score range is 0-10, overall satisfaction score range is 0-10. A decrease from Baseline indicates a worsening. The change from Baseline values are presented for Week 4, Week 12 and Week 24. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Scores on a Scale (Mean) | ||
|---|---|---|---|
| OL Week 4, n=47, 48 | OL Week 12, n=46, 48 | OL Week 24, n=44, 47 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0.2 | -0.3 | -2.6 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0.4 | -0.6 | -0.1 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. Duration is the total number of non-overlapping days for all events per subject. A duration is censored if there is at least one event with unknown start date or end date, in which case the censored duration is the minimum number of days that a subject has experienced any of these events. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). NA=not applicable. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Days (Mean) | ||
|---|---|---|---|
| Altered (decreased) libido n=1 | Impotence, n=8 | Ejaculation disorder, n=1 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 135.0 | 90.8 | 63.0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. Duration is the total number of non-overlapping days for all events per subject. A duration is censored if there is at least one event with unknown start date or end date, in which case the censored duration is the minimum number of days that a subject has experienced any of these events. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). NA=not applicable. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Days (Mean) | ||
|---|---|---|---|
| Altered (decreased) libido n=2,1 | Impotence, n=3, 7 | Ejaculation disorder, n=0, 1 | |
| Dutasteride 0.5 mg | 44.0 | 78.6 | 63.0 |
| Placebo | 88.5 | 68.3 | NA |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs related to sexual function are defined as: altered (decreased) libido, impotence, and ejaculation disorders. Duration is the total number of non-overlapping days for all events per subject. A duration is censored if there is at least one event with unknown start date or end date, in which case the censored duration is the minimum number of days that a subject has experienced any of these events. Only those participants available at the specified time points were analyzed (represented by n=X, X in the category titles). NA=not applicable. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Days (Mean) | ||
|---|---|---|---|
| Altered (decreased) libido n=2,1 | Impotence, n=1, 1 | Ejaculation disorder, n=0, 0 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 135.0 | 176.0 | NA |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 77.5 | 181.0 | NA |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. The erectile function domain of the IIEF (IIEF-EF) includes Questions 1 through 5 and Question 15 (maximum score of 30). A clinically meaningful gradient of severity of erectile dysfunction (ED) has been developed, indicating that a score of greater than 25 represents an individual without ED while men scoring <=25 may be classified as having ED. The values are presented for Week 4, Week 12 and Week 24. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Participants (Number) | ||
|---|---|---|---|
| OL Week 4 | OL Week 12 | OL Week 24 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 2 | 3 | 5 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 2 | 2 | 1 |
The IIEF is a validated 15-item questionnaire with individual items of the questionnaire assigned to five separate domains of sexual function (i.e., erectile function, orgasmic function, sexual desire, intercourse satisfaction, and overall satisfaction). The IIEF was employed to assess treatment-related changes in men with erectile dysfunction. The erectile function domain of the IIEF (IIEF-EF) includes Questions 1 through 5 and Question 15 (maximum score of 30). A clinically meaningful gradient of severity of erectile dysfunction (ED) has been developed, indicating that a score of greater than 25 represents an individual without ED while men scoring <=25 may be classified as having ED. The values are presented for Week 4, Week 12 and Week 24. The Baseline assessment was defined as the latest assessment on or before the DB treatment start. Change from Baseline is post-Baseline value minus Baseline value. (NCT02014584)
Timeframe: Baseline, Week 4, Week 12 and Week 24
| Intervention | Participants (Number) | ||
|---|---|---|---|
| DB Week 4 | DB Week 12 | DB Week 24 | |
| Dutasteride 0.5 mg | 1 | 7 | 6 |
| Placebo | 3 | 4 | 3 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs of special interest included those of sexual function: breast disorders (breast enlargement and breast tenderness), prostate cancer, cardiovascular events, and possible suicidality-related AEs (PSRAEs). Infrequent AEs of special interest included breast cancer, allergic reactions, depressed mood, hair changes, interference with formation of external genitalia in a male fetus, potential for decreased male fertility, and testicular pain and swelling. Special interest AEs are groups of MedDRA terms which have been defined in the analysis plan. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Altered (decreased libido) | Impotence | Ejaculation disorders | Breast disorder | Prostate cancer | Cardiovascular adverse event | Infrequent adverse events | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 1 | 8 | 1 | 0 | 0 | 0 | 2 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs of special interest included those of sexual function: breast disorders (breast enlargement and breast tenderness), prostate cancer, cardiovascular events, and possible suicidality-related AEs (PSRAEs). Infrequent AEs of special interest included breast cancer, allergic reactions, depressed mood, hair changes, interference with formation of external genitalia in a male fetus, potential for decreased male fertility, and testicular pain and swelling. Special interest AEs are groups of MedDRA terms which have been defined in the analysis plan. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Altered (decreased libido) | Impotence | Ejaculation disorders | Breast disorder | Prostate cancer | Cardiovascular adverse event | Infrequent adverse events | |
| Dutasteride 0.5 mg | 1 | 7 | 1 | 0 | 0 | 0 | 1 |
| Placebo | 2 | 3 | 0 | 0 | 0 | 0 | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. AEs of special interest included those of sexual function: breast disorders (breast enlargement and breast tenderness), prostate cancer, cardiovascular events, and possible suicidality-related AEs (PSRAEs). Infrequent AEs of special interest included breast cancer, allergic reactions, depressed mood, hair changes, interference with formation of external genitalia in a male fetus, potential for decreased male fertility, and testicular pain and swelling. Special interest AEs are groups of MedDRA terms which have been defined in the analysis plan. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Altered (decreased libido) | Impotence | Ejaculation disorders | Breast disorder | Prostate cancer | Cardiovascular adverse event | Infrequent adverse events | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 1 | 1 | 0 | 0 | 0 | 0 | 1 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 2 | 1 | 0 | 0 | 0 | 0 | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.. SAE is defined as 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, all events of possible drug-induced liver injury with hyperbilirubinemia, breast cancer in male participants, or spontaneous abortion in female partner of male participant. The PSRAE form was used in this study to collect detailed information on the circumstances of reported AEs which, in the investigator's opinion, were possibly suicidality-related. (NCT02014584)
Timeframe: 48 weeks
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Any AE | Any SAE | PSRAE | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 25 | 1 | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.. SAE is defined as 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, all events of possible drug-induced liver injury with hyperbilirubinemia, breast cancer in male participants, or spontaneous abortion in female partner of male participant. The PSRAE form was used in this study to collect detailed information on the circumstances of reported AEs which, in the investigator's opinion, were possibly suicidality-related. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Any AE | Any SAE | PSRAE | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 15 | 0 | 0 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 13 | 1 | 0 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. SAE is defined as 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, all events of possible drug-induced liver injury with hyperbilirubinemia, breast cancer in male participants, or spontaneous abortion in female partner of male participant. The PSRAE form was used in this study to collect detailed information on the circumstances of reported AEs which, in the investigator's opinion, were possibly suicidality-related. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Any AE | Any SAE | PSRAE | |
| Dutasteride 0.5 mg | 19 | 1 | 0 |
| Placebo | 18 | 1 | 0 |
The Baseline heart rate assessment was defined as the latest assessment on or before the double-blind treatment start. The clinical concern range for heart rate was defined as: (lower: <40, upper: >100). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Baseline <40 | Baseline >100 | Post- Baseline <40 | Post- Baseline >100 | |
| Dutasteride 0.5 mg | 0 | 1 | 0 | 2 |
| Placebo | 0 | 1 | 0 | 1 |
Baseline heart rate assessment was defined as the latest assessment on or before the open-label treatment start. The clinical concern range for heart rate was defined as: (lower: <40, upper: >100). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Baseline <40 | Baseline >100 | Post- Baseline <40 | Post- Baseline >100 | |
| Dutasteride 0.5 mg (DB)/Dutasteride 0.5 mg (OL) | 0 | 1 | 0 | 5 |
| Placebo (DB)/Dutasteride 0.5 mg (OL) | 0 | 1 | 0 | 3 |
The Baseline blood presssure assessment was defined as the latest assessment on or before the double-blind treatment start. The clinical concern range for vital signs was defined as: Systolic blood pressure (lower: <80, upper: >165) and diastolic blood pressure: (lower: <40, upper: >105). (NCT02014584)
Timeframe: Baseline and up to Week 24
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline SBP <80 mmHg | Baseline SBP >165 mmHg | Baseline DBP <40 mmHg | Baseline DBP >105 mmHg | Post Baseline SBP <80 mmHg | Post Baseline SBP >165 mmHg | Post Baseline DBP <40 mmHg | Post Baseline DBP >105 mmHg | |
| Dutasteride 0.5 mg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 2 |
| Placebo | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
An AE is defined as any untoward medical occurrence in a patient or clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Treatment related AE included events which the investigator classified as having a reasonable possibilty of being caused by the investigational product or whose classification was missing. (NCT02014584)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Placebo | 5 |
| Dutasteride 0.5 mg | 11 |
AUR is defined as condition when the participant is unable to urinate and requires bladder catheterization. AUR or BPH-related surgery event details per participant was summarized as first occurring of either AUR or BPH-related surgery. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| Overall | Year 1 subset | Year 2 subset | |
| Dut 0.5 mg + Tam 0.2 mg | 4 | 2 | 2 |
| Placebo + Tam 0.2mg | 15 | 8 | 7 |
BPH-related interventions were recorded. BPH-related interventions included adenomectomy, balloon dilatation, electroresection, thermotherapy (microwave or radiofrequency), laser resection, prostatectomy, prostatotomy, transurethral resection of the prostate, transurethral drainage of prostatic abscess, drainage of prostatic cysts, radioactive seeding of the prostate, prostatic urethral stenting, incision of periurethral stricture, ethanol injections into the prostate, transrectal high intensity focussed ultrasound, transurethral needle ablation and transurethral microwave thermotherapy. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| Overall | Year 1 subset | Year 2 subset | |
| Dut 0.5 mg + Tam 0.2 mg | 2 | 0 | 2 |
| Placebo + Tam 0.2mg | 3 | 0 | 3 |
Details of number of participants in different types of wards was recorded. Types of wards included general ward, recovery, intensive care unit, multiple ward types and others (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| General ward | Recovery | Other | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 1 | 0 |
| Placebo + Tam 0.2mg | 2 | 0 | 1 |
Improvement in IPSS was categorized as improvement, no change and worsening. Improvement defined as greater than or equal to 2 points, greater than or equal to 3 points and greater than or equal to 25 percent in participants at months 3,6,9,12,15,18,21 and 24 . Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline was reported based on the LOCF. Change from Baseline defined as difference between Post-Baseline value and Baseline value. (NCT02058368)
Timeframe: Baseline and 3, 6, 9,12,15,18,21 and 24 months
| Intervention | Participants (Number) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 3,>= 3 units, n=299, 296 | Month 3,>= 2 units, n=299,296 | Month 3,>= 25percent, n=299, 296 | Month 6,>= 3 units, n=300, 298 | Month 6,>= 2 units, n=300, 298 | Month 6,>= 25percent, n=300, 298 | Month 9,>= 3 units, n=300, 298 | Month 9,>= 2 units, n=300, 298 | Month 9,>= 25percent, n=300, 298 | Month 12,>= 3 units, n=300, 298 | Month 12,>= 2 units, n=300, 298 | Month 12,>= 25percent, n=300, 298 | Month 15,>= 3 units, n=300, 298 | Month 15,>= 2 units, n=300, 298 | Month 15,>= 25percent, n=300, 298 | Month 18,>= 3 units, n=300, 298 | Month 18,>= 2 units, n=300, 298 | Month 18,>= 25percent, n=300, 298 | Month 21,>= 3 units, n=300, 298 | Month 21,>= 2 units, n=300, 298 | Month 21,>= 25percent, n=300, 298 | Month 24,>= 3 units, n=300, 298 | Month 24,>= 2 units, n=300, 298 | Month 24,>= 25percent, n=300, 298 | |
| Dut 0.5 mg + Tam 0.2 mg | 157 | 176 | 123 | 156 | 176 | 133 | 177 | 193 | 150 | 171 | 191 | 154 | 186 | 203 | 160 | 171 | 187 | 148 | 178 | 194 | 161 | 184 | 197 | 169 |
| Placebo + Tam 0.2mg | 160 | 190 | 134 | 156 | 179 | 131 | 157 | 185 | 128 | 154 | 179 | 131 | 171 | 186 | 133 | 156 | 173 | 136 | 169 | 186 | 141 | 156 | 175 | 137 |
An adverse event is defined as any untoward medical occurrence in a subject or clinical investigation subject, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. A SAE is defined as resulting in death, life threatening, requires hospitalization or prolongation of hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation that is medically important, All events of possible drug-induced liver injury with hyperbilirubinaemia, male breast cancer and spontaneous abortion of a female partner of a male subject (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Any Non-serious AE | Any SAE | |
| Dut 0.5 mg + Tam 0.2 mg | 208 | 49 |
| Placebo + Tam 0.2mg | 203 | 52 |
BHS was collected as Question 8 the IPSS questionnaire regarding quality of life due to urinary symptom with scores values ranging from 0 (delightful) to 6 (terrible). Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from baseline BHS at each scheduled post-baseline assessment was compared in terms of combination treatment (Dut plus Tam) versus tamsulosin treatment using t-tests from a general linear model with effects for treatment, country, and Baseline BHS. (NCT02058368)
Timeframe: Baseline, 3, 6, 9, 12, 15, 18, 21 and 24 Months
| Intervention | Scores on scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 3, n=299, 296 | Month 6, n=300,298 | Month 9, n=300, 298 | Month 12, n=300, 298 | Month 15, n=300, 298 | Month 18, n=300, 298 | Month 21, n=300, 298 | Month 24, n=300, 298 | |
| Dut 0.5 mg + Tam 0.2 mg | -0.85 | -0.73 | -0.95 | -0.90 | -1.02 | -1.00 | -1.02 | -1.16 |
| Placebo + Tam 0.2mg | -0.88 | -0.89 | -1.08 | -0.87 | -0.93 | -0.92 | -1.08 | -1.00 |
Total serum PSA concentrations were assessed at pre-screening, month 6, 12 and 24. Change from baseline total PSA was compared in terms of combination treatment (Dut plus Tam) versus tamsulosin treatment at each scheduled post-baseline assessment using a general linear model with effects for treatment and baseline total PSA. Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline defined as difference between Post-Baseline value and Baseline value. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Baseline 6, 12 and 24 Months
| Intervention | nanogram/milliliter (ng/mL) (Mean) | ||
|---|---|---|---|
| Month 6, n=292, 294 | Month 12, n=293, 294 | Month 24, n=293, 295 | |
| Dut 0.5 mg + Tam 0.2 mg | -1.7 | -1.9 | -2.0 |
| Placebo + Tam 0.2mg | 0.2 | 0.2 | 0.7 |
PAS SFI consists of three questions each with a range of 0 (Big Problem) to 4 (No Problem). PAS SFI was administered at screening, Baseline and at each month 12 and 24. The total PSI is the sum of the three questions; the total score range is 0 to 12. Change from Baseline PAS SFI at each scheduled post-baseline assessment was compared in terms of combination treatment (Dut plus Tam) versus tamsulosin treatment using t-tests from a general linear model with effects for treatment, country, and Baseline PAS SFI. Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline defined as difference between Post-Baseline value and Baseline value. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Baseline, 12 and 24 Months
| Intervention | Scores on scale (Mean) | |
|---|---|---|
| Month 12, n=291, 293 | Month 24, n=291, 294 | |
| Dut 0.5 mg + Tam 0.2 mg | -0.91 | -0.82 |
| Placebo + Tam 0.2mg | 0.11 | -0.11 |
Post void residual volume was measured suprapubically by ultrasound (immediately following the urinary flow measurement). Post void residual volume change from Baseline distribution at each scheduled post-Baseline assessment was compared with combination treatment (Dut plus Tam) versus tamsulosin treatment using a nonparametric van Elteren test. Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline defined as difference between Post-Baseline value and Baseline value. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Baseline, 6, 12, 18 and 24 Months
| Intervention | mL (Mean) | |||
|---|---|---|---|---|
| Month 6, n=288, 290 | Month 12, n=291, 292 | Month 18, n=291, 292 | Month 24, n=291, 292 | |
| Dut 0.5 mg + Tam 0.2 mg | -3.0 | -1.4 | -1.3 | -2.6 |
| Placebo + Tam 0.2mg | -4.8 | 1.5 | -2.6 | 2.6 |
Qmax is defined as maximum urine flow. Qmax was measured with Uroflow meter (Urodyn 1000) at Screening, Baseline, and at Months 6,12,18 and 24. Change from Baseline Qmax at each scheduled post-Baseline assessment was compared in terms of combination treatment (Dut plus Tam) versus tamsulosin treatment using t-tests from a general linear model with effects for treatment, country, and Baseline Qmax. Baseline value was defined as the latest non-missing assessment either treatment start date or randomization date. Change from Baseline defined as difference between Post-Baseline value and Baseline value. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Baseline, 6, 12, 18 and 24 Months
| Intervention | milliliter per second (mL/sec) (Mean) | |||
|---|---|---|---|---|
| Month 6, n=270, 274 | Month 12, n=286, 287 | Month 18, n=287, 288 | Month 24, n=287,290 | |
| Dut 0.5 mg + Tam 0.2 mg | 1.54 | 1.62 | 2.36 | 2.27 |
| Placebo + Tam 0.2mg | 0.62 | 0.63 | 0.90 | 0.93 |
IPSS (also called IPSS total score) is the sum of the seven questions with each score ranging from 0 (best) to 5 (worst). IPSS was self administered at screening, Baseline and each time-point of Month 3, 6, 9, 12, 15, 18, 21 and 24. Seven questions included are incomplete emptying, frequency, intermittency, urgency, weak stream, straining and nocturia. The total IPSS score can range from 0-35 with severity catagories of mild (0 to 7), moderate (8 to 19) or severe (20 to 35). LOCF is defined as carrying forward the last non-missing post-Baseline assessment for participants with missing visit data and/or for participants who discontinued from the study. Baseline value is defined as the latest non-missing assessment of either treatment start date or randomization date. Month 24 is the primary timepoint and earlier timepoints are considered secondary. Change from Baseline defined as difference between Post-Baseline value and Baseline value. (NCT02058368)
Timeframe: Baseline and 3, 6, 9, 12, 15, 18, 21 and 24 months
| Intervention | Score on scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 3, n=299, 296 | Month 6, n=300, 298 | Month 9, n=300, 298 | Month 12,n= 300, 298 | Month 15, n=300, 298 | Month 18, n=300, 298 | Month 21, n=300, 298 | Month 24, n=300, 298 | |
| Dut 0.5 mg + Tam 0.2 mg | -3.28 | -3.36 | -4.28 | -4.30 | -4.90 | -4.54 | -4.66 | -4.96 |
| Placebo + Tam 0.2mg | -4.07 | -3.73 | -4.14 | -3.93 | -3.95 | -3.84 | -3.94 | -3.53 |
The BII consists of four questions and BII total score is the sum of four questions. Total score range is 0 (no problem) to 13 (worst value). Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline BII at each scheduled post-baseline assessment was compared in terms of combination treatment (Dut plus Tam) versus tamsulosin treatment using t-tests from a general linear model with effects for treatment, country, and Baseline BII. Change from Baseline was summarized using LOCF approaches. (NCT02058368)
Timeframe: Baseline 3, 6, 9, 12, 15, 18, 21 and 24 Months
| Intervention | Scores on scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 3, n=299, 296 | Month 6, n=300, 298 | Month 9, n=300, 298 | Month 12, n=300, 298 | Month 15, n=300, 298 | Month 18, n=300, 298 | Month 21, n=300, 298 | Month 24, n=300, 298 | |
| Dut 0.5 mg + Tam 0.2 mg | -1.23 | -1.08 | -1.26 | -1.24 | -1.41 | -1.28 | -1.27 | -1.48 |
| Placebo + Tam 0.2mg | -1.48 | -1.28 | -1.55 | -1.39 | -1.30 | -1.16 | -1.12 | -1.02 |
Duration of hospitalization days due to AUR or BPH-related surgery was recorded. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Days (Median) |
|---|---|
| Placebo + Tam 0.2mg | 10.0 |
| Dut 0.5 mg + Tam 0.2 mg | 9.0 |
Qmax change from Baseline was presented using six improvement levels: >0 milliliter per second (mL/sec) and >=1 mL/sec through >=5mL/sec. Qmax percentage change from Baseline was presented using six improvement levels: >0%, >=10%, >=20%, >=30%, >=40%, and >=50%. Here, Qmax improvement of >= 3 mL/sec and Qmax percentage of >= 30 % for 24 Months has been summarized. Baseline value is defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline defined as difference between Post-Baseline value and Baseline value. Baseline value is defined as the latest non-missing assessment of either treatment start date or randomization date. (NCT02058368)
Timeframe: Baseline 6, 12, 18 and 24 Months
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 6, >= 3 mL/sec, n=270, 274 | Month 6, >= 3 %, n=270, 274 | Month 12, >= 3 mL/sec, n=286, 287 | Month 12, >= 3 %, n=286, 287 | Month 18, >= 3 mL/sec, n=287, 288 | Month 18, >= 3 %, n= 287, 288 | Month 24, >= 3 mL/sec, n=287, 290 | Month 24, >= 30 %, n=287, 290 | |
| Dut 0.5 mg + Tam 0.2 mg | 86 | 86 | 102 | 107 | 115 | 111 | 121 | 119 |
| Placebo + Tam 0.2mg | 69 | 70 | 64 | 73 | 80 | 81 | 77 | 71 |
Suicidality was assessed utilizing the Columbia Suicide Severity Rating Scale (C-SSRS). It included tabular summaries of suicidal ideation and suicidal behavior questions that were administered. Assessments were carried out at Screening, Month 6, Month 12, and Month 24 (or end of treatment) visits. C-SSRS included Question1-2 were for suicidal ideation Question 1: Passive: wish to be dead, Question 2: Active: Non-specific (no method, intent or plan). Questions 6-10 were for suicidal behavior, Question 6: Preparatory Acts or Behavior, Question 7: any aborted attempt, Question 8: Any interrupted attempts, Question 9: Any non-fatal actual suicide attempt, Question 10: Completed suicide. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: 6, 12, 18 , 24 months and final assessment
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 6, Suicidal ideation, Q1, n=289, 285 | Month 6, Suicidal ideation, Q2, n=289, 285 | Month 6, Suicidal behavior, Q6, n=289, 285 | Month 6, Suicidal behavior, Q7, n=289, 285 | Month 6, Suicidal behavior, Q8, n=289, 285 | Month 6, Suicidal behavior, Q9, n=289, 285 | Month 6, Suicidal behavior, Q10, n=289, 285 | Month 12, Suicidal ideation, Q1, n=279, 273 | Month 12, Suicidal ideation, Q2, n=279, 273 | Month 12, Suicidal behavior, Q6, n=279, 273 | Month 12, Suicidal behavior, Q7, n=279, 273 | Month 12, Suicidal behavior, Q8, n=279, 273 | Month 12, Suicidal behavior, Q9, n=279, 273 | Month 12, Suicidal behavior, Q10, n=279, 273 | Month 24, Suicidal ideation, Q1, n=261, 251 | Month 24, Suicidal ideation, Q2, n=261, 251 | Month 12, Suicidal behavior, Q6, n=261, 251 | Month 12, Suicidal behavior, Q7, n=261, 251 | Month 12, Suicidal behavior, Q8, n=261, 251 | Month 12, Suicidal behavior, Q9, n=261, 251 | Month 12, Suicidal behavior, Q10, n=261, 251 | Final assessment, Suicidal ideation,Q1, n=288, 285 | Final assessment, Suicidal ideation,Q2, n=288, 285 | Final assessment, Suicidal behavior,Q6, n=288, 285 | Final assessment, Suicidal behavior,Q7, n=288, 285 | Final assessment, Suicidal behavior,Q8, n=288, 285 | Final assessment, Suicidal behavior,Q9, n=288, 285 | Final assessment, Suicidal behavior,Q10,n=288, 285 | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo + Tam 0.2mg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Clinical chemistry laboratory parameters assessed included albumin, alanine aminotransferase (ALT), alkaline phosphatase (ALP), aspartate aminotransferase (AST), creatinine, glucose, potassium, sodium, total bilirubin, total protein and urea/blood urea nitrogen (BUN). Threshold factors are in the below table. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| albumin, <0.90 X LLN, n=289, 292 | albumin, >1.20 X ULN, n=289, 292 | ALT, >3.00 X ULN, n=289, 292 | ALP, > 1.50 X ULN, n=289, 292 | AST, >3.00 X ULN, n=288, 292 | creatinine, <0.50 X LLN, n=289, 292 | creatinine, >3.00 X ULN, n=289, 292 | glucose, <0.70 X LLN, n=288, 292 | glucose, >1.75 X ULN, n=280, 285 | potassium, <0.75 X LLN, n=288, 292 | potassium, >1.40 X ULN, n=288, 292 | sodium, <0.90 X LLN, n=289, 292 | sodium, >1.15 X ULN, n=289, 292 | total bilirubin, >2.50 X ULN, n=289, 292 | total protein, <0.80 X LLN, n=289, 292 | total protein, >1.15 X ULN, n=289, 292 | Urea/BUN, <0.50 X LLN, n=289, 292 | Urea/BUN, >2.00 X ULN, n=289, 292 | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 13 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo + Tam 0.2mg | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 13 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
The threshold laboratory values are defined in terms of a multiplicative factor of the testing laboratory's normal range. A laboratory value that is above the upper limit factor multiplied by the upper limit of the normal (ULN) range is considered a high threshold value. A laboratory value that is below the lower limit factor multiplied by the lower limit of the normal (LLN) range is considered a low threshold value. Hematology laboratory parameters assessed included hemoglobin (Hgb), platelet count, white blood cell count (WBC) and red blood cell (RBC) count. Threshold factors are in the below table. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| Hgb, <0.75 X LLN, n=287, 291 | Platelet count, <0.75 X LLN, n=284, 283 | Platelet count, >1.50 X ULN, n=285, 285 | RBC, <0.50 X LLN, n=287, 291 | WBC, <0.50 X LLN, n=287, 291 | WBC, >3.00 X ULN, n=287, 291 | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 1 | 0 | 0 | 0 | 0 |
| Placebo + Tam 0.2mg | 0 | 6 | 0 | 0 | 0 | 0 |
Vital signs included assessment of systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate. Threshold ranges for SBP ranged from < 80 mmHg (millimeter of mercury) (lower) to > 165 mmHg (upper); for DBP ranged from < 40 mmHg (lower) to > 105 mmHg (upper) and heart rate < 40 beats per minute (bpm) (lower) to > 100 bpm (upper). (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| SBP, < 80 mmHg | SBP, > 165 mmHg | SBP, either threshold | DBP, < 40 mmHg | DBP, > 105 mmHg | DBP, either threshold | Heart rate, < 40 bpm | Heart rate, > 100 bpm | Heart rate, either threshold | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 13 | 13 | 0 | 2 | 2 | 0 | 14 | 14 |
| Placebo + Tam 0.2mg | 0 | 10 | 10 | 0 | 6 | 6 | 0 | 11 | 11 |
Details of participants who were admitted to hospitals related to AUR or BPH-Related surgery has been recorded. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Out-patient | In-patient | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 3 |
| Placebo + Tam 0.2mg | 5 | 6 |
AUR is defined as condition when the participant is unable to urinate and requires bladder catheterization. (NCT02058368)
Timeframe: Up to 24 Months
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| Overall | Year 1 subset | Year 2 subset | |
| Dut 0.5 mg + Tam 0.2 mg | 2 | 2 | 0 |
| Placebo + Tam 0.2mg | 13 | 8 | 5 |
Prostate Volume measurements were conducted annually using Transrectal ultrasound (TRUS). The following calculation was utilized to assess the prostate volume (cc): pi/6 (Anteroposterior Width multiplied by Cephalocaudal Width multiplied by Transverse Width). Post-Baseline prostate volume was calculated at 12 and 24 months. Baseline value was defined as the latest non-missing assessment of either treatment start date or randomization date. Change from Baseline was reported based on the LOCF. Change from Baseline defined as difference between Post-Baseline value and Baseline value and reported as a percentage. (NCT02058368)
Timeframe: Baseline,12 and 24 months
| Intervention | Cubic centimeters (cc) (Mean) | |
|---|---|---|
| Month 12, n=287, 286 | Month 24, n=287, 286 | |
| Dut 0.5 mg + Tam 0.2 mg | -22.8 | -24.8 |
| Placebo + Tam 0.2mg | 0.2 | 3.6 |
DRE evaluation was carried out from normal/diffusely enlarged at Baseline to focal abnormalities at any time post-Baseline. DRE was assessed at screening visit, Month 6, 12, 18 , 24 and final assessment is the latest post-Baseline evaluation that was available. Here, participants with focal abnormalities are summarized. Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: 6, 12, 18 , 24 months and final assessment
| Intervention | Participants (Count of Participants) | ||||
|---|---|---|---|---|---|
| Month 6, n=287, 285 | Month 12, n=279, 272 | Month 18, n=267, 258 | Month 24, n=261, 252 | Final Assessment, n=296, 295 | |
| Dut 0.5 mg + Tam 0.2 mg | 9 | 11 | 12 | 13 | 15 |
| Placebo + Tam 0.2mg | 11 | 10 | 6 | 10 | 10 |
Qualitative breast examination included palpable breast tissue and nipple tenderness. Here, participants with clinically significant abnormalities for palpable breast tissue and nipple tenderness are summarized. Qualitative breast examination was done at screening visit, Month 6, 12, 18 , 24 and final assessment (latest post-Baseline evaluation that was available). Only those participants available at the specified time points (represented by n=X in the category titles) were analyzed. (NCT02058368)
Timeframe: 6, 12, 18 , 24 months and final assessment
| Intervention | Participants (Count of Participants) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Palpable breast tissue, Month 6, n=289, 284 | Nipple tenderness,Month 6, n=289, 284 | Palpable breast tissue, Month 12, n=279, 273 | Nipple tenderness,Month 12, n=279, 273 | Palpable breast tissue, Month 18, n=267, 258 | Nipple tenderness,Month 18, n=267, 258 | Palpable breast tissue, Month 24, n=262, 252 | Nipple tenderness, Month 24, n=262, 252 | Palpable breast tissue,final assessment, n=296,296 | Nipple tenderness,final assessment, n=296, 296 | |
| Dut 0.5 mg + Tam 0.2 mg | 0 | 0 | 2 | 1 | 0 | 0 | 0 | 0 | 0 | 0 |
| Placebo + Tam 0.2mg | 0 | 0 | 1 | 0 | 1 | 0 | 0 | 0 | 0 | 0 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| adenine [no description available] | 2.31 | 1 | 0 | 6-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. | 3.23 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| salicylic acid Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL). | 5.68 | 5 | 1 | monohydroxybenzoic acid | algal metabolite; antifungal agent; antiinfective agent; EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor; keratolytic drug; plant hormone; plant metabolite |
| 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. | 3.23 | 1 | 0 | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| 3,4-dihydroxyphenylacetic acid 3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents. | 2.11 | 1 | 0 | catechols; dihydroxyphenylacetic acid | human metabolite |
| 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. | 3.23 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| 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. | 2.05 | 1 | 0 | 2-hydroxy monocarboxylic acid | algal metabolite; Daphnia magna metabolite |
| formaldehyde paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy | 2.15 | 1 | 0 | aldehyde; one-carbon compound | allergen; carcinogenic agent; disinfectant; EC 3.5.1.4 (amidase) inhibitor; environmental contaminant; Escherichia coli metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| methanol Methanol: A colorless, flammable liquid used in the manufacture of FORMALDEHYDE and ACETIC ACID, in chemical synthesis, antifreeze, and as a solvent. Ingestion of methanol is toxic and may cause blindness.. primary alcohol : A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it.. methanol : The primary alcohol that is the simplest aliphatic alcohol, comprising a methyl and an alcohol group. | 2.06 | 1 | 0 | alkyl alcohol; one-carbon compound; primary alcohol; volatile organic compound | amphiprotic solvent; Escherichia coli metabolite; fuel; human metabolite; mouse metabolite; Mycoplasma genitalium metabolite |
| melatonin [no description available] | 2.08 | 1 | 0 | acetamides; tryptamines | anticonvulsant; central nervous system depressant; geroprotector; hormone; human metabolite; immunological adjuvant; mouse metabolite; radical scavenger |
| 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. | 3.23 | 1 | 0 | pyridine 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 |
| 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. | 3.61 | 2 | 0 | monocarboxylic 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). | 3.23 | 1 | 0 | hydroxymethylpyridine; 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. | 3.23 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| 2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors. | 2.06 | 1 | 0 | non-proteinogenic alpha-amino acid | NMDA receptor antagonist |
| pk 11195 PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine | 2.13 | 1 | 0 | aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes | antineoplastic agent |
| 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. | 2.08 | 1 | 0 | monochlorobenzenes; N-arylpiperazine | drug metabolite; environmental contaminant; serotonergic agonist; xenobiotic |
| 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine: A dopaminergic neurotoxic compound which produces irreversible clinical, chemical, and pathological alterations that mimic those found in Parkinson disease.. 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine : A tetrahydropyridine that is 1,2,3,6-tetrahydropyridine substituted by a methyl group at position 1 and a phenyl group at position 4. | 2.31 | 1 | 0 | methylpyridines; phenylpyridine; tetrahydropyridine | neurotoxin |
| homovanillic acid Homovanillic Acid: A 3-O-methyl ETHER of (3,4-dihydroxyphenyl)acetic acid.. homovanillate : A hydroxy monocarboxylic acid anion which is obtained by deprotonation of the carboxy group of homovanillic acid.. homovanillic acid : A monocarboxylic acid that is the 3-O-methyl ether of (3,4-dihydroxyphenyl)acetic acid. It is a catecholamine metabolite. | 2.11 | 1 | 0 | guaiacols; monocarboxylic acid | human metabolite; mouse metabolite |
| phenytoin [no description available] | 3.57 | 2 | 0 | imidazolidine-2,4-dione | anticonvulsant; 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. | 2.08 | 1 | 0 | acridines; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.86 | 3 | 0 | acetamides; 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) | 3.61 | 2 | 0 | monocarboxylic 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. | 3.23 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| alaproclate alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer | 3.23 | 1 | 0 | alpha-amino acid ester | |
| albendazole [no description available] | 3.61 | 2 | 0 | aryl 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). | 3.61 | 2 | 0 | phenols; 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. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| alfuzosin alfuzosin: structure given in first source | 5.41 | 7 | 0 | monocarboxylic 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. | 3.57 | 2 | 0 | imidazoles; 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. | 3.23 | 1 | 0 | organochlorine 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. | 2.08 | 1 | 0 | secondary 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. | 3.23 | 1 | 0 | triamino-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 | 3.23 | 1 | 0 | adamantanes; 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. | 3.23 | 1 | 0 | quaternary ammonium ion | EC 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. | 3.61 | 2 | 0 | acetamides; 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. | 3.23 | 1 | 0 | diamine; 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. | 2.08 | 1 | 0 | dicarboximide; 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. | 3.23 | 1 | 0 | N-acylglycine | Daphnia magna metabolite |
| theophylline [no description available] | 3.86 | 3 | 0 | dimethylxanthine | adenosine 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. | 3.86 | 3 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| dan 2163 [no description available] | 2.08 | 1 | 0 | aromatic 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. | 3.61 | 2 | 0 | carbotricyclic 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. | 2.08 | 1 | 0 | monocarboxylic 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. | 3.88 | 3 | 0 | dihydropyridine; 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. | 3.61 | 2 | 0 | dibenzooxazepine | adrenergic 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. | 2.08 | 1 | 0 | acridines; aromatic ether; sulfonamide | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| anastrozole [no description available] | 5.48 | 4 | 1 | nitrile; 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. | 2.08 | 1 | 0 | anthracenes | antipsoriatic |
| 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. | 2.08 | 1 | 0 | pyrazolone | antipyretic; 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. | 5.48 | 4 | 1 | benzoic 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. | 2.5 | 2 | 0 | benzimidazoles; 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. | 3.61 | 2 | 0 | ethanolamines; 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. | 3.61 | 2 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| baclofen [no description available] | 3.61 | 2 | 0 | amino 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. | 3.23 | 1 | 0 | indazoles; 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. | 3.23 | 1 | 0 | benzothiadiazine; 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. | 3.61 | 2 | 0 | 1-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. | 2.08 | 1 | 0 | benzoate ester; substituted aniline | allergen; antipruritic drug; sensitiser; topical anaesthetic |
| betaxolol [no description available] | 3.23 | 1 | 0 | propanolamine | antihypertensive 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. | 3.23 | 1 | 0 | carbamate 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. | 8.05 | 7 | 4 | (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. | 2.08 | 1 | 0 | biphenyls; 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. | 3.23 | 1 | 0 | piperidines; 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) | 3.61 | 2 | 0 | diarylmethane | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 3.23 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bromopride bromopride: RN given refers to parent cpd; structure | 2.08 | 1 | 0 | benzamides | |
| bronopol [no description available] | 2.08 | 1 | 0 | nitro compound | |
| bumetanide [no description available] | 3.86 | 3 | 0 | amino 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. | 3.23 | 1 | 0 | azaspiro 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] | 3.86 | 3 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| secbutabarbital secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital | 3.23 | 1 | 0 | barbiturates | |
| caffeine [no description available] | 3.86 | 3 | 0 | purine 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. | 3.61 | 2 | 0 | aromatic 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. | 3.57 | 2 | 0 | benzimidazolecarboxylic 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. | 3.86 | 3 | 0 | dibenzoazepine; 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. | 3.23 | 1 | 0 | monochlorobenzenes; 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. | 3.23 | 1 | 0 | carbamate ester | muscle 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. | 2.08 | 1 | 0 | N-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. | 2.08 | 1 | 0 | carbazoles; organochlorine compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug; photosensitizing agent |
| carvedilol [no description available] | 3.61 | 2 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 3.61 | 2 | 0 | organofluorine 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. | 3.23 | 1 | 0 | ether; 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. | 3.86 | 3 | 0 | aromatic 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 | 3.23 | 1 | 0 | diarylmethane | |
| 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. | 3.61 | 2 | 0 | benzodiazepine | |
| 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. | 3.23 | 1 | 0 | 1,3-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. | 3.61 | 2 | 0 | aminoquinoline; 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. | 3.23 | 1 | 0 | benzothiadiazine | antihypertensive 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. | 3.61 | 2 | 0 | monochlorobenzenes; 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. | 3.86 | 3 | 0 | organochlorine 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. | 3.61 | 2 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 3.61 | 2 | 0 | isoindoles; 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. | 3.61 | 2 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cifenline [no description available] | 2.08 | 1 | 0 | diarylmethane | |
| ciclopirox [no description available] | 2.08 | 1 | 0 | cyclic 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. | 2.08 | 1 | 0 | aromatic ether; thiazolidinone | antineoplastic agent; insulin-sensitizing drug |
| cilostazol [no description available] | 3.61 | 2 | 0 | lactam; 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. | 3.86 | 3 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofibrate [no description available] | 2.08 | 1 | 0 | cyclopropanes; 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. | 3.86 | 3 | 0 | aminoquinoline; 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 |
| 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. | 3.61 | 2 | 0 | 2-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. | 3.35 | 1 | 0 | amino 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. | 2.08 | 1 | 0 | monohydroxyquinoline; 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. | 2.08 | 1 | 0 | 1,4-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. | 2.08 | 1 | 0 | monochlorobenzenes; phenazines | dye; leprostatic drug; non-steroidal anti-inflammatory drug |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 3.86 | 3 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 3.61 | 2 | 0 | tertiary amine | estrogen 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. | 3.61 | 2 | 0 | dibenzoazepine | anticoronaviral 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. | 3.57 | 2 | 0 | 1,4-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. | 3.57 | 2 | 0 | clonidine; imidazoline | |
| 4-chloro-N-(2,6-dimethyl-1-piperidinyl)-3-sulfamoylbenzamide [no description available] | 2.08 | 1 | 0 | sulfonamide | |
| 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. | 3.23 | 1 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 3.23 | 1 | 0 | conazole 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. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant; 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. | 3.23 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| dapsone [no description available] | 3.86 | 3 | 0 | substituted 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. | 3.23 | 1 | 0 | acyclic desferrioxamine | bacterial 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. | 3.61 | 2 | 0 | dibenzoazepine; 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. | 3.23 | 1 | 0 | primary 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. | 3.86 | 3 | 0 | 1,4-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. | 3.61 | 2 | 0 | benzothiadiazine; 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. | 3.23 | 1 | 0 | amino 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. | 3.23 | 1 | 0 | dichlorobenzene; 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. | 3.23 | 1 | 0 | carboxylic 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. | 3.23 | 1 | 0 | pentacarboxylic acid | copper 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. | 3.57 | 2 | 0 | monohydroxybenzoic 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. | 3.23 | 1 | 0 | dithiol; 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. | 3.57 | 2 | 0 | ether; 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. | 3.61 | 2 | 0 | piperidines; 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. | 3.61 | 2 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 3.61 | 2 | 0 | organic 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. | 3.57 | 2 | 0 | branched-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. | 2.46 | 2 | 0 | benzimidazoles; 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. | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | morpholines; 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. | 7.52 | 12 | 1 | aromatic 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. | 3.61 | 2 | 0 | dibenzooxepine; 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. | 3.23 | 1 | 0 | pyridines; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| ebastine [no description available] | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | phenols; 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. | 2.08 | 1 | 0 | 1,8-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. | 3.23 | 1 | 0 | triazoles; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA modulator |
| 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. | 3.61 | 2 | 0 | aromatic 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. | 3.61 | 2 | 0 | dicarboximide; 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. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| 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. | 3.23 | 1 | 0 | 1,1-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. | 3.23 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 3.86 | 3 | 0 | 2-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. | 3.23 | 1 | 0 | carbamate ester | anticonvulsant; 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. | 2.08 | 1 | 0 | biphenyls; 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. | 3.61 | 2 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenfluramine Fenfluramine: A centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release.. fenfluramine : A secondary amino compound that is 1-phenyl-propan-2-amine in which one of the meta-hydrogens is substituted by trifluoromethyl, and one of the hydrogens attached to the nitrogen is substituted by an ethyl group. It binds to the serotonin reuptake pump, causing inhbition of serotonin uptake and release of serotonin. The resulting increased levels of serotonin lead to greater serotonin receptor activation which in turn lead to enhancement of serotoninergic transmission in the centres of feeding behavior located in the hypothalamus. This suppresses the appetite for carbohydrates. Fenfluramine was used as the hydrochloride for treatment of diabetes and obesity. It was withdrawn worldwide after reports of heart valve disease and pulmonary hypertension. | 3.47 | 1 | 1 | (trifluoromethyl)benzenes; secondary amino compound | appetite depressant; serotonergic agonist; serotonin uptake inhibitor |
| 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 | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | benzazepine | alpha-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. | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid. | 3.27 | 1 | 0 | anilide; monocarboxylic acid amide; piperidines | adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| 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. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fipexide fipexide: regulates dopaminergic systems at macromolecular level | 3.23 | 1 | 0 | benzodioxoles | |
| 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. | 3.23 | 1 | 0 | carboxylic 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). | 3.23 | 1 | 0 | aromatic 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. | 2.08 | 1 | 0 | difluorobenzene; 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. | 3.61 | 2 | 0 | conazole 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. | 3.86 | 3 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 3.57 | 2 | 0 | N-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. | 3.61 | 2 | 0 | ethyl 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. | 3.61 | 2 | 0 | benzoic 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. | 3.61 | 2 | 0 | nucleobase 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. | 3.61 | 2 | 0 | (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. | 3.23 | 1 | 0 | 1,4-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. | 3.23 | 1 | 0 | fluorobiphenyl; monocarboxylic acid | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fluspirilene Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia. | 2.11 | 1 | 0 | diarylmethane | |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 5.17 | 5 | 0 | (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. | 3.23 | 1 | 0 | pyrazoles | antidote; 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. | 3.23 | 1 | 0 | carboxylic 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. | 3.61 | 2 | 0 | chlorobenzoic 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. | 3.57 | 2 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 3.61 | 2 | 0 | aromatic ether | antilipemic 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. | 3.23 | 1 | 0 | aminoquinoline; 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. | 2.08 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; insulin secretagogue; radical scavenger |
| glimepiride glimepiride: structure given in first source | 3.86 | 3 | 0 | sulfonamide | |
| 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. | 3.86 | 3 | 0 | aromatic 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. | 3.86 | 3 | 0 | monochlorobenzenes; 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] | 3.23 | 1 | 0 | benzenes | |
| granisetron [no description available] | 3.57 | 2 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 3.23 | 1 | 0 | methoxybenzenes | |
| 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. | 3.23 | 1 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 3.61 | 2 | 0 | acetamides | |
| 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. | 3.23 | 1 | 0 | carboxamidine; 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. | 3.86 | 3 | 0 | aromatic 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. | 3.23 | 1 | 0 | azaarene; 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. | 4.08 | 4 | 0 | benzothiadiazine; 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. | 3.61 | 2 | 0 | benzothiadiazine; 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. | 3.61 | 2 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 3.61 | 2 | 0 | one-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. | 3.23 | 1 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; 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. | 3.23 | 1 | 0 | primary 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. | 3.61 | 2 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 3.61 | 2 | 0 | ifosfamides | alkylating 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. | 3.86 | 3 | 0 | dibenzoazepine | adrenergic 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. | 3.61 | 2 | 0 | bipyridines | EC 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. | 3.61 | 2 | 0 | indoles; 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. | 3.61 | 2 | 0 | aromatic 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. | 2.08 | 1 | 0 | benzenedicarboxamide; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| ioversol [no description available] | 3.23 | 1 | 0 | amidobenzoic acid | |
| iproniazid [no description available] | 3.61 | 2 | 0 | carbohydrazide; 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. | 3.86 | 3 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| 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) | 3.23 | 1 | 0 | benzenes | |
| 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). | 3.61 | 2 | 0 | carbohydrazide | antitubercular 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. | 3.23 | 1 | 0 | catechols; 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. | 3.23 | 1 | 0 | alkylbenzene | |
| 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. | 3.61 | 2 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 3.86 | 3 | 0 | piperazines | |
| 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. | 3.61 | 2 | 0 | cyclohexanones; 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. | 2.08 | 1 | 0 | aromatic 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. | 9.29 | 9 | 2 | dichlorobenzene; 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. | 3.23 | 1 | 0 | benzophenones; 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. | 3.23 | 1 | 0 | amino 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. | 3.23 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 3.61 | 2 | 0 | 1,2,4-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. | 3.86 | 3 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| 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. | 3.61 | 2 | 0 | (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] | 11.37 | 6 | 2 | nitrile; 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. | 2.08 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antimicrobial agent; antitubercular agent; photosensitizing agent |
| lomustine [no description available] | 3.61 | 2 | 0 | N-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. | 3.23 | 1 | 0 | monocarboxylic 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. | 3.61 | 2 | 0 | benzocycloheptapyridine; 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. | 3.23 | 1 | 0 | benzodiazepine | |
| 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 | 3.57 | 2 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| loxapine Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. | 3.23 | 1 | 0 | dibenzooxazepine | antipsychotic agent; dopaminergic antagonist |
| 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. | 3.61 | 2 | 0 | anthracenes | |
| 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. | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | primary aliphatic amine | |
| mechlorethamine nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR. | 3.23 | 1 | 0 | nitrogen 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. | 3.23 | 1 | 0 | diarylmethane | |
| 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. | 3.23 | 1 | 0 | aminobenzoic 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. | 3.61 | 2 | 0 | aminobenzoic 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 |
| mefloquine hydrochloride [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4. | 2.11 | 1 | 0 | organofluorine compound; piperidines; quinolines; secondary alcohol | |
| memantine [no description available] | 3.23 | 1 | 0 | adamantanes; 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 | 3.23 | 1 | 0 | diarylmethane | |
| 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. | 3.23 | 1 | 0 | ethyl 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. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| 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. | 3.23 | 1 | 0 | piperidinecarboxamide | drug 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) | 3.23 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | amino 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. | 3.23 | 1 | 0 | phenothiazines; 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. | 3.23 | 1 | 0 | aralkylamino 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. | 3.85 | 3 | 0 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| 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. | 3.23 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 3.23 | 1 | 0 | sulfonamide; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | aromatic 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) | 3.23 | 1 | 0 | benzothiadiazine | |
| 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. | 3.23 | 1 | 0 | beta-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. | 3.86 | 3 | 0 | benzamides; 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. | 3.23 | 1 | 0 | organochlorine 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. | 3.61 | 2 | 0 | aromatic 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. | 3.61 | 2 | 0 | C-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. | 3.23 | 1 | 0 | aromatic ketone | antimetabolite; 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. | 3.61 | 2 | 0 | aromatic 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. | 3.86 | 3 | 0 | imidazobenzodiazepine; 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. | 3.23 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 3.57 | 2 | 0 | bipyridines; 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. | 11.18 | 24 | 1 | dialkylarylamine; 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. | 3.61 | 2 | 0 | benzazepine; 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. | 3.23 | 1 | 0 | diarylmethane | |
| 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. | 3.23 | 1 | 0 | dihydroxyanthraquinone | analgesic; 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. | 2.08 | 1 | 0 | benzamides; 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. | 3.23 | 1 | 0 | monocarboxylic 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) | 3.23 | 1 | 0 | monoterpenoid | |
| 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. | 2.08 | 1 | 0 | acetamides; 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. | 3.23 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nadolol [no description available] | 3.61 | 2 | 0 | tetralins | |
| nalidixic acid [no description available] | 3.61 | 2 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| naratriptan naratriptan: structure given in first source | 3.57 | 2 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 3.61 | 2 | 0 | aromatic 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. | 2.08 | 1 | 0 | benzoxazocine; 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. | 2.08 | 1 | 0 | quaternary ammonium ion | antidote 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. | 3.86 | 3 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 3.23 | 1 | 0 | organonitrogen 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. | 3.61 | 2 | 0 | benzenes; C-nitro compound; diester; dihydropyridine; methyl ester; tertiary amino compound | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 3.86 | 3 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 3.23 | 1 | 0 | (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. | 3.61 | 2 | 0 | aromatic 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. | 3.86 | 3 | 0 | 2-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. | 3.61 | 2 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| 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). | 2.46 | 2 | 0 | 1,4-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. | 2.08 | 1 | 0 | C-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. | 3.23 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 3.57 | 2 | 0 | 1,3-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. | 3.23 | 1 | 0 | isoquinolines | dopamine 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. | 3.61 | 2 | 0 | fluoroquinolone 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. | 3.61 | 2 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| 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. | 3.61 | 2 | 0 | 3-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. | 3.61 | 2 | 0 | aromatic 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. | 3.61 | 2 | 0 | carbazoles | |
| 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. | 3.23 | 1 | 0 | ether; 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. | 3.61 | 2 | 0 | 1,3-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. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease). | 2.6 | 1 | 0 | benzenetriol; catecholamine; primary amino compound | drug metabolite; human metabolite; neurotoxin |
| 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. | 3.9 | 3 | 0 | acetylenic 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. | 3.23 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pamidronate [no description available] | 3.23 | 1 | 0 | phosphonoacetic 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. | 3.57 | 2 | 0 | aromatic 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. | 3.61 | 2 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| 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. | 3.61 | 2 | 0 | 1,3-oxazoles | central 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. | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 3.61 | 2 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 3.23 | 1 | 0 | piperidines | cardiovascular 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. | 3.61 | 2 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenacetin Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione | 2.08 | 1 | 0 | acetamides; 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. | 3.57 | 2 | 0 | barbiturates | anticonvulsant; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | primary amine | adrenergic 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. | 3.23 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| 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. | 3.61 | 2 | 0 | indoles; 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. | 3.61 | 2 | 0 | aromatic 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. | 2.08 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| 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. | 2.08 | 1 | 0 | N-arylpiperazine | |
| polythiazide [no description available] | 3.23 | 1 | 0 | benzothiadiazine | |
| duodote duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents | 3.23 | 1 | 0 | pyridinium ion | antidote to organophosphate poisoning; antidote to sarin poisoning; cholinergic drug; cholinesterase reactivator |
| ono 1078 pranlukast: SRS-A antagonist; leukotriene D4 receptor antagonist | 2.08 | 1 | 0 | chromones | |
| pyranoprofen pyranoprofen: RN given refers to unlabled parent cpd; structure given in first source | 2.08 | 1 | 0 | pyridochromene | |
| praziquantel azinox: Russian drug | 3.9 | 3 | 0 | isoquinolines | |
| 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. | 4.91 | 6 | 0 | aromatic 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. | 3.61 | 2 | 0 | aminoquinoline; 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. | 3.86 | 3 | 0 | pyrimidone | anticonvulsant; 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. | 3.61 | 2 | 0 | benzoic 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. | 3.86 | 3 | 0 | benzamides | anti-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. | 3.23 | 1 | 0 | benzamides; 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. | 3.61 | 2 | 0 | N-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. | 3.61 | 2 | 0 | pyrrolidines; 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. | 3.61 | 2 | 0 | phenothiazines; 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. | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | xanthenes | |
| 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. | 3.23 | 1 | 0 | phenols | anticonvulsant; 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. | 3.61 | 2 | 0 | naphthalenes; 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. | 3.57 | 2 | 0 | carbotricyclic compound | antidepressant |
| pyridostigmine [no description available] | 3.23 | 1 | 0 | pyridinium ion | |
| pyrimethamine Maloprim: contains above 2 cpds | 3.23 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| sch 16134 quazepam: structure given in first source | 3.23 | 1 | 0 | benzodiazepine | |
| quetiapine [no description available] | 3.23 | 1 | 0 | dibenzothiazepine; 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. | 3.23 | 1 | 0 | benzimidazoles; 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. | 3.57 | 2 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| ranitidine [no description available] | 2.08 | 1 | 0 | aralkylamine | |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 3.61 | 2 | 0 | benzothiazoles | |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 3.23 | 1 | 0 | alkylamine | |
| 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. | 4.1 | 4 | 0 | 1,2-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 |
| rizatriptan rizatriptan: structure given in first source; RN given refers to benzoate | 3.57 | 2 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rofecoxib [no description available] | 2.46 | 2 | 0 | butenolide; sulfone | analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| ropinirole [no description available] | 3.57 | 2 | 0 | indolones; tertiary amine | antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist |
| saccharin Saccharin: Flavoring agent and non-nutritive sweetener.. saccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent. | 2.03 | 1 | 0 | 1,2-benzisothiazole; N-sulfonylcarboxamide | environmental contaminant; sweetening agent; xenobiotic |
| 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. | 3.23 | 1 | 0 | benzoate 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. | 3.23 | 1 | 0 | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 3.23 | 1 | 0 | organochlorine 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. | 3.61 | 2 | 0 | pyrimidines; 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. | 3.23 | 1 | 0 | pyridines | |
| 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. | 3.61 | 2 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 3.61 | 2 | 0 | aromatic 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). | 3.61 | 2 | 0 | dicarboxylic 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. | 3.23 | 1 | 0 | quaternary 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. | 3.23 | 1 | 0 | sulfonamide 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. | 2.08 | 1 | 0 | isoxazoles; 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] | 2.08 | 1 | 0 | sulfonamide | |
| 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. | 3.61 | 2 | 0 | ||
| 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. | 3.23 | 1 | 0 | 1,3-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. | 2.08 | 1 | 0 | isoxazoles; sulfonamide antibiotic; sulfonamide | antibacterial drug; drug allergen |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| 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. | 3.61 | 2 | 0 | sulfonamide; 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. | 2.08 | 1 | 0 | N-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. | 2.08 | 1 | 0 | acetylenic compound; ethyl ester; pyridines; retinoid; thiochromane | keratolytic drug; prodrug; teratogenic agent |
| telenzepine telenzepine: structure given in first source | 2.03 | 1 | 0 | benzodiazepine | |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 3.23 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 3.61 | 2 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia | 4.76 | 5 | 0 | furans; 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. | 3.61 | 2 | 0 | phenylethanolamines; 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. | 2.08 | 1 | 0 | diarylmethane | |
| 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. | 3.23 | 1 | 0 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 3.23 | 1 | 0 | 1,3-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. | 3.23 | 1 | 0 | phenothiazines; 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). | 3.61 | 2 | 0 | aziridines | |
| tiapride [no description available] | 2.08 | 1 | 0 | benzamides | |
| 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. | 3.23 | 1 | 0 | monochlorobenzenes; 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. | 2.08 | 1 | 0 | aromatic 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. | 3.61 | 2 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 3.23 | 1 | 0 | N-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. | 3.61 | 2 | 0 | benzothiadiazole; 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) | 2.08 | 1 | 0 | pyridinecarboxamide | |
| 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. | 3.23 | 1 | 0 | N-sulfonylurea | hypoglycemic 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. | 3.86 | 3 | 0 | N-sulfonylurea | human 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. | 3.23 | 1 | 0 | aromatic ketone; monocarboxylic acid; pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| tolnaftate [no description available] | 2.08 | 1 | 0 | monothiocarbamic ester | antifungal 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. | 3.57 | 2 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 3.23 | 1 | 0 | amino 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. | 3.61 | 2 | 0 | monochlorobenzenes; 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. | 3.86 | 3 | 0 | pteridines | diuretic; 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. | 3.57 | 2 | 0 | triazolobenzodiazepine | sedative |
| trifluoperazine [no description available] | 3.23 | 1 | 0 | N-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 |
| 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. | 3.23 | 1 | 0 | amine | |
| 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. | 3.23 | 1 | 0 | oxazolidinone | anticonvulsant; 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. | 3.23 | 1 | 0 | benzamides; 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. | 3.86 | 3 | 0 | aminopyrimidine; 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. | 3.23 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | dibenzoazepine; 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. | 3.61 | 2 | 0 | chromanes; 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. | 2.08 | 1 | 0 | ||
| tyramine [no description available] | 3.23 | 1 | 0 | monoamine 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. | 3.57 | 2 | 0 | aminopyridine; 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. | 2.08 | 1 | 0 | undecenoic acid | antifungal drug; plant metabolite |
| urapidil [no description available] | 2.08 | 1 | 0 | piperazines | |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 3.61 | 2 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 3.61 | 2 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| pirinixic acid pirinixic acid: structure | 2.08 | 1 | 0 | aryl sulfide; organochlorine compound; pyrimidines | |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 3.61 | 2 | 0 | carbamate 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. | 3.86 | 3 | 0 | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| 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. | 3.57 | 2 | 0 | imidazopyridine | central 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. | 3.61 | 2 | 0 | 1,2-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. | 2.08 | 1 | 0 | monochloropyridine; 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. | 3.23 | 1 | 0 | corticosteroid 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. | 3.23 | 1 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| 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. | 5.31 | 3 | 1 | 11beta-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. | 3.61 | 2 | 0 | alkaloid 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. | 3.23 | 1 | 0 | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| sorbitol D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol). | 3.23 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| 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. | 3.23 | 1 | 0 | 2-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. | 3.23 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| 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. | 5.88 | 7 | 0 | 3-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. | 3.61 | 2 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| cysteine [no description available] | 3.23 | 1 | 0 | cysteine 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 |
| 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. | 3.57 | 2 | 0 | 11-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 |
| estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens. | 3.66 | 2 | 0 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| androsterone [no description available] | 6.52 | 4 | 4 | 17-oxo steroid; 3alpha-hydroxy steroid; androstanoid; C19-steroid | androgen; anticonvulsant; human blood serum metabolite; human metabolite; human urinary metabolite; mouse metabolite; pheromone |
| etiocholanolone Etiocholanolone: The 5-beta-reduced isomer of ANDROSTERONE. Etiocholanolone is a major metabolite of TESTOSTERONE and ANDROSTENEDIONE in many mammalian species including humans. It is excreted in the URINE.. 3alpha-hydroxy-5beta-androstan-17-one : An androstanoid that is 5beta-androstane substituted by an alpha-hydroxy group at position 3 and an oxo group at position 17. It is a metabolite of testosterone in mammals. | 3.56 | 1 | 1 | 17-oxo steroid; 3alpha-hydroxy steroid; androstanoid | human metabolite; mouse metabolite |
| dehydroepiandrosterone Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.. dehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands. | 2.1 | 1 | 0 | 17-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; androstanoid | androgen; human metabolite; mouse metabolite |
| 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. | 3.57 | 2 | 0 | penicillin 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. | 3.23 | 1 | 0 | pilocarpine | antiglaucoma drug |
| 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. | 3.23 | 1 | 0 | 2-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. | 2.08 | 1 | 0 | chlorocarbon; chloromethanes | hepatotoxic agent; refrigerant |
| cantharidin Cantharidin: A toxic compound, isolated from the Spanish fly or blistering beetle (Lytta (Cantharis) vesicatoria) and other insects. It is a potent and specific inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A). This compound can produce severe skin inflammation, and is extremely toxic if ingested orally.. cantharidin : A monoterpenoid with an epoxy-bridged cyclic dicarboxylic anhydride structure secreted by many species of blister beetle, and most notably by the Spanish fly, Lytta vesicatoria. Natural toxin inhibitor of protein phosphatases 1 and 2A. | 7.03 | 1 | 0 | cyclic dicarboxylic anhydride; monoterpenoid | EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; herbicide |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 3.86 | 3 | 0 | C-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. | 3.23 | 1 | 0 | amino 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] | 3.23 | 1 | 0 | acetate 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. | 3.57 | 2 | 0 | carbamate 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. | 2.46 | 2 | 0 | 17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound | xenoestrogen |
| testosterone propionate Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors. | 2.31 | 1 | 0 | steroid ester | |
| 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. | 2.08 | 1 | 0 | bisbenzylisoquinoline alkaloid | drug 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. | 3.61 | 2 | 0 | aporphine alkaloid | alpha-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. | 3.23 | 1 | 0 | 17beta-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. | 3.23 | 1 | 0 | benzoquinolizine; 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. | 3.61 | 2 | 0 | kanamycins | bacterial metabolite |
| 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 | 2.58 | 2 | 0 | amino 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. | 3.23 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| 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. | 3.23 | 1 | 0 | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| acetylcholine chloride acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug. | 3.23 | 1 | 0 | quaternary 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. | 3.23 | 1 | 0 | phenothiazines | |
| 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. | 3.57 | 2 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| 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. | 3.23 | 1 | 0 | calcium salt | chelator |
| androstenedione Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads. | 2.11 | 1 | 0 | 17-oxo steroid; 3-oxo-Delta(4) steroid; androstanoid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
| 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. | 3.23 | 1 | 0 | aspartate 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. | 3.61 | 2 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| mebanazine mebanazine: RN given refers to parent cpd without isomeric designation; structure | 3.23 | 1 | 0 | benzenes | |
| 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. | 3.23 | 1 | 0 | penicillin | antibacterial agent; antibacterial drug |
| triamcinolone diacetate triamcinolone diacetate: lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone | 2.08 | 1 | 0 | corticosteroid hormone | |
| norethindrone Norethindrone: A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.. norethisterone : A 17beta-hydroxy steroid that is testosterone in which the hydrogen at position 17 is replaced by an ethynyl group and in which the methyl group attached to position 10 is replaced by hydrogen. | 2.03 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound; tertiary alcohol | progestin; synthetic oral contraceptive |
| 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). | 3.23 | 1 | 0 | 4-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) | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 3.23 | 1 | 0 | mannitol | allergen; 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] | 3.61 | 2 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| medroxyprogesterone acetate [no description available] | 2.08 | 1 | 0 | 20-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 |
| 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. | 3.23 | 1 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| 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. | 3.23 | 1 | 0 | fluoroalkane; 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. | 2.49 | 2 | 0 | 11beta-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. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
| phencyclidine Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.. phencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects. | 2.03 | 1 | 0 | benzenes; piperidines | anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug |
| 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 | 3.23 | 1 | 0 | organic 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) | 3.23 | 1 | 0 | primary amino compound; triol | buffer |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 3.86 | 3 | 0 | 6-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. | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | organobromine 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. | 3.23 | 1 | 0 | penicillin 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. | 3.23 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| n-vinyl-2-pyrrolidinone N-vinyl-2-pyrrolidinone: monomer of POVIDONE; structure given in first source | 2.49 | 2 | 0 | pyrrolidin-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. | 3.23 | 1 | 0 | phenylethanolamines; 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. | 3.23 | 1 | 0 | aromatic ketone; tertiary amine | appetite depressant |
| quinuclidines Quinuclidines: A class of organic compounds which contain two rings that share a pair of bridgehead carbon atoms and contains an amine group. | 2.11 | 1 | 0 | quinuclidines; 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. | 3.23 | 1 | 0 | benzoate ester; secondary amino compound; substituted aniline | anaesthetic; antitussive |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 3.23 | 1 | 0 | ergoline 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. | 2.08 | 1 | 0 | biguanides | antineoplastic agent; geroprotector; hypoglycemic agent |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 3.23 | 1 | 0 | quinolines | |
| pregnenolone [no description available] | 4.17 | 3 | 1 | 20-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; C21-steroid | human metabolite; mouse metabolite |
| 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. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| potassium cyanide [no description available] | 2.04 | 1 | 0 | cyanide salt; one-carbon compound; potassium salt | EC 1.15.1.1 (superoxide dismutase) inhibitor; EC 1.9.3.1 (cytochrome c oxidase) inhibitor; neurotoxin |
| 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. | 3.23 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| fluocortolone Fluocortolone: A glucocorticoid with anti-inflammatory activity used topically for various skin disorders. | 2.03 | 1 | 0 | 21-hydroxy steroid | |
| 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. | 4.93 | 6 | 0 | azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines | |
| thiazoles [no description available] | 2.75 | 3 | 0 | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| 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. | 3.23 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| chlormadinone acetate Chlormadinone Acetate: An orally active synthetic progestational hormone used often in combinations as an oral contraceptive (CONTRACEPTIVES, ORAL). | 7.5 | 2 | 0 | corticosteroid hormone | |
| testosterone enanthate [no description available] | 9.31 | 9 | 8 | heptanoate 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. | 3.61 | 2 | 0 | mixture | bronchodilator 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. | 3.23 | 1 | 0 | N-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. | 3.61 | 2 | 0 | benzazepine 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. | 3.23 | 1 | 0 | steroid 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. | 2.08 | 1 | 0 | hydrochloride | antineoplastic 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) | 2.08 | 1 | 0 | 11beta-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 |
| cyproterone acetate [no description available] | 3.21 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; chlorinated steroid; steroid ester | androgen antagonist; geroprotector; progestin |
| nandrolone Nandrolone: C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position.. nandrolone : A 3-oxo Delta(4)-steroid that is estr-4-en-3-one substituted by a beta-hydroxy group at position 17. | 2.04 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid | human metabolite |
| 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. | 3.23 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-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. | 3.23 | 1 | 0 | bile 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. | 2.08 | 1 | 0 | isoquinoline alkaloid; pyridoisoquinoline | antiamoebic agent; anticoronaviral agent; antiinfective agent; antimalarial; antineoplastic agent; antiprotozoal drug; antiviral agent; autophagy inhibitor; emetic; expectorant; plant metabolite; protein synthesis inhibitor |
| phenylpropanolamine Phenylpropanolamine: A sympathomimetic that acts mainly by causing release of NOREPINEPHRINE but also has direct agonist activity at some adrenergic receptors. It is most commonly used as a nasal vasoconstrictor and an appetite depressant.. phenylpropanolamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group. A decongestant and appetite suppressant, it is commonly used in prescription and over-the-counter cough and cold preparations.. (-)-norephedrine : An amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1R,2S-stereoisomer). It is a plant alkaloid. | 2.97 | 1 | 0 | amphetamines; phenethylamine alkaloid | plant metabolite |
| 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. | 3.23 | 1 | 0 | 4-hydroxy monocarboxylic acid; hydroxybutyric acid | general anaesthetic; GHB receptor agonist; neurotoxin; sedative |
| 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. | 3.23 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| medroxyprogesterone [no description available] | 3.23 | 1 | 0 | 17alpha-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. | 16.17 | 59 | 27 | 17beta-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 | 3.61 | 2 | 0 | diarylmethane | |
| 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. | 3.23 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| levocarnitine (R)-carnitine : The (R)-enantiomer of carnitine. | 3.23 | 1 | 0 | carnitine | antilipemic drug; nootropic agent; nutraceutical; Saccharomyces cerevisiae metabolite; water-soluble vitamin (role) |
| senecioic acid senecioic acid: structure. 3-methylbut-2-enoic acid : A methyl-branched fatty acid that is but-2-enoic acid bearing a methyl substituent at position 3. | 3.27 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; methyl-branched fatty acid; monounsaturated fatty acid; short-chain fatty acid | plant metabolite |
| sulfanilylurea sulfanilylurea: antimicrobial agent; structure | 3.23 | 1 | 0 | benzenes; 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. | 2.08 | 1 | 0 | isothiocyanate | insecticide |
| lactulose [no description available] | 3.23 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| megestrol acetate [no description available] | 2.08 | 1 | 0 | 20-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] | 3.23 | 1 | 0 | ||
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 3.23 | 1 | 0 | acetylcysteine; 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. | 3.86 | 3 | 0 | cyclic ketone; erythromycin | |
| hydroxychloroquine sulfate [no description available] | 2.08 | 1 | 0 | ||
| 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. | 6.21 | 5 | 2 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| boldenone boldenone: RN given refers to (17beta)-isomer. boldenone : An 3-oxo-Delta(1),Delta(4)-steroid substituted by an oxo group at position 3 and a beta-hydroxy group at position 17. It is an anabolic androgenic steroid that has been developed for veterinary use. | 4.37 | 1 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; anabolic androgenic steroid | |
| 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. | 3.23 | 1 | 0 | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
| estradiol valerate [no description available] | 2.03 | 1 | 0 | steroid ester | |
| 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. | 2.08 | 1 | 0 | hydrochloride | antitubercular 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. | 3.57 | 2 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| antimycin a [no description available] | 2.08 | 1 | 0 | benzamides; 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. | 3.23 | 1 | 0 | glycopeptide | antibacterial 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. | 6.6 | 9 | 0 | alpha-tocopherol | algal 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. | 2.08 | 1 | 0 | aliphatic 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. | 3.23 | 1 | 0 | monocarboxylic acid | EC 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 | 2.08 | 1 | 0 | aromatic ketone | |
| metaxalone [no description available] | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | cyclic 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. | 3.87 | 3 | 0 | benzochromene; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.87 | 3 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| 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. | 3.23 | 1 | 0 | brompheniramine | anti-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 | 3.86 | 3 | 0 | dihydrofuran; 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. | 3.61 | 2 | 0 | dichlorobenzene; 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. | 3.23 | 1 | 0 | 17alpha-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] | 3.23 | 1 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| cladribine [no description available] | 3.61 | 2 | 0 | organochlorine 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. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| metocurine metocurine: from Chinese herb Cyclea hainanensis Mrr | 2.08 | 1 | 0 | isoquinolines | |
| floxacillin Floxacillin: Antibiotic analog of CLOXACILLIN.. flucloxacillin : A penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain. | 2.03 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| clomacran clomacran: RN given refers to parent cpd; structure | 3.23 | 1 | 0 | acridines | |
| methenamine hippurate methenamine hippurate: both parts of molecule contribute to its antibacterial action | 3.23 | 1 | 0 | N-acylglycine | |
| levomethadone levomethadone : A 6-(dimethylamino)-4,4-diphenylheptan-3-one that has (R)-configuration. It is the active enantiomer of methadone and its hydrochloride salt is used to treat adults who are addicted to drugs such as heroin and morphine. | 2.03 | 1 | 0 | 6-(dimethylamino)-4,4-diphenylheptan-3-one | antitussive; mu-opioid receptor agonist; NMDA receptor antagonist; opioid analgesic |
| 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. | 3.23 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| n-methylaspartate N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration. | 2.46 | 2 | 0 | amino dicarboxylic acid; D-alpha-amino acid; D-aspartic acid derivative; secondary amino compound | neurotransmitter agent |
| phenylethylmalonamide Phenylethylmalonamide: A metabolite of primidone. | 2.03 | 1 | 0 | amine | |
| 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. | 2.08 | 1 | 0 | organic sodium salt | antineoplastic agent; bone density conservation agent; chelator |
| lutetium Lutetium: An element of the rare earth family of metals. It has the atomic symbol Lu, atomic number 71, and atomic weight 175. | 2.21 | 1 | 0 | d-block element atom; lanthanoid atom | |
| holmium Holmium: An element of the rare earth family of metals. It has the atomic symbol Ho, atomic number 67, and atomic weight 164.93. | 8.64 | 1 | 1 | f-block element atom; lanthanoid atom | |
| 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. | 2.08 | 1 | 0 | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source | 2.08 | 1 | 0 | delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite |
| 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. | 3.23 | 1 | 0 | inorganic sodium salt | antidote to cyanide poisoning; antifungal drug; nephroprotective agent |
| mafenide acetate [no description available] | 2.08 | 1 | 0 | carboxylic 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; | 2.08 | 1 | 0 | anthraquinone | |
| metopimazine metopimazine: RN given refers to parent cpd; structure | 2.03 | 1 | 0 | phenothiazines | |
| 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. | 3.23 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| selegiline hydrochloride, (r)-isomer [no description available] | 2.08 | 1 | 0 | hydrochloride; terminal acetylenic compound | antiparkinson drug; dopaminergic agent; EC 1.4.3.4 (monoamine oxidase) inhibitor |
| 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. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpyrrolidine | anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic antagonist |
| thiamphenicol [no description available] | 2.08 | 1 | 0 | monocarboxylic acid amide; sulfone | antimicrobial agent; immunosuppressive agent |
| pancuronium bromide pancuronium bromide : A bromide salt consisting of two bromide ions and one pancuronium dication. | 2.08 | 1 | 0 | bromide salt | cholinergic 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. | 3.57 | 2 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| 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. | 2.08 | 1 | 0 | C-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. | 3.61 | 2 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| metergoline Metergoline: A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.. metergoline : An ergoline alkaloid that is the N-benzyloxycarbonyl derivative of lysergamine. A 5-HT2 antagonist. Also 5-HT1 antagonist and 5-HT1D ligand. Has moderate affinity for 5-HT6 and high affinity for 5-HT7. | 2.03 | 1 | 0 | carbamate ester; ergoline alkaloid | dopamine agonist; geroprotector; serotonergic antagonist |
| 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 | 3.23 | 1 | 0 | ||
| laxagetten 4,4'-diacetoxydiphenylpyridylemethane [no description available] | 3.23 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | aminoglycoside 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. | 3.61 | 2 | 0 | nucleoside 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. | 3.23 | 1 | 0 | aromatic 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. | 3.57 | 2 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| 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. | 2.06 | 1 | 0 | chloride salt; organic chloride salt | antiseptic drug; surfactant |
| triamcinolone Triamcinolone: A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739). triamcinolone : A C21-steroid hormone that is 1,4-pregnadiene-3,20-dione carrying four hydroxy substituents at positions 11beta, 16alpha, 17alpha and 21 as well as a fluoro substituent at position 9. Used in the form of its 16,17-acetonide to treat various skin infections. | 2.25 | 1 | 0 | 11beta-hydroxy steroid; 16alpha-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | anti-allergic agent; anti-inflammatory drug |
| oxyphenisatin [no description available] | 3.23 | 1 | 0 | indoles | |
| fludrocortisone Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity. | 3.23 | 1 | 0 | 11beta-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. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| pregnanolone Pregnanolone: A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.. 3alpha-hydroxy-5beta-pregnan-20-one : The 3alpha-stereoisomer of 3-hydroxy-5beta-pregnan-20-one. | 3.92 | 2 | 1 | 3-hydroxy-5beta-pregnan-20-one; 3alpha-hydroxy steroid | human metabolite; intravenous anaesthetic; sedative |
| 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. | 2.08 | 1 | 0 | C-nitro compound; imidazoles; monocarboxylic acid amide | antiprotozoal drug |
| androstane-3,17-diol Androstane-3,17-diol: The unspecified form of the steroid, normally a major metabolite of TESTOSTERONE with androgenic activity. It has been implicated as a regulator of gonadotropin secretion. | 3.48 | 1 | 1 | 17-hydroxy steroid; 3-hydroxy steroid; androstanoid | |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 3.23 | 1 | 0 | chlorphenamine | |
| clometacin clometacin: structure | 3.23 | 1 | 0 | N-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. | 3.57 | 2 | 0 | beta-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. | 3.61 | 2 | 0 | penicillin 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. | 3.61 | 2 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| indoramin Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent. | 2.08 | 1 | 0 | tryptamines | |
| 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. | 3.61 | 2 | 0 | cyclic 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. | 3.61 | 2 | 0 | catechols; 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. | 3.23 | 1 | 0 | carbamate 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. | 3.23 | 1 | 0 | amino 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. | 3.86 | 3 | 0 | azide; 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) | 2.08 | 1 | 0 | organic molecular entity | |
| pirprofen pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure | 3.23 | 1 | 0 | pyrroline | |
| 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. | 2.08 | 1 | 0 | amino cyclitol glycoside | antibacterial 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). | 3.9 | 3 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 3.61 | 2 | 0 | beta-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. | 3.23 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| penbutolol Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent. | 3.23 | 1 | 0 | ethanolamines | |
| ribavirin Rebetron: Rebetron is tradename | 3.86 | 3 | 0 | 1-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. | 3.61 | 2 | 0 | alpha-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. | 3.23 | 1 | 0 | beta-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. | 3.23 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | L-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. | 3.86 | 3 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive 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. | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | acetate ester; androstane; quaternary ammonium ion | drug allergen; muscle relaxant; neuromuscular agent; nicotinic antagonist |
| dexibuprofen dexibuprofen: structure in first source | 2.03 | 1 | 0 | ibuprofen | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| 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. | 3.23 | 1 | 0 | 1,3-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] | 3.23 | 1 | 0 | benzophenones | |
| 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. | 3.23 | 1 | 0 | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | antimalarial |
| 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 | 3.61 | 2 | 0 | benzamides; 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. | 3.23 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| acarbose [no description available] | 3.61 | 2 | 0 | tetrasaccharide derivative | EC 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. | 3.57 | 2 | 0 | aminopyridine; 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. | 3.23 | 1 | 0 | aminoglycoside; 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] | 2.08 | 1 | 0 | acetamides | |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 3.57 | 2 | 0 | anthracycline 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. | 3.23 | 1 | 0 | penicillin 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. | 3.23 | 1 | 0 | aromatic 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. | 3.61 | 2 | 0 | alkanethiol; 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. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| staurosporine [no description available] | 2.08 | 1 | 0 | indolocarbazole 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. | 2.08 | 1 | 0 | one-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. | 3.23 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| atracurium besylate atracurium besylate : The bisbenzenesulfonate salt of atracurium. | 2.08 | 1 | 0 | organosulfonate 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. | 2.08 | 1 | 0 | nitrate ester; pyridinecarboxamide | potassium channel opener; vasodilator agent |
| endralazine BQ 22-708: RN given refers to parent cpd | 2.03 | 1 | 0 | benzamides | |
| 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. | 3.23 | 1 | 0 | diamine; 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. | 2.08 | 1 | 0 | methanesulfonate salt | antiparkinson drug; dopamine agonist; geroprotector |
| 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. | 3.61 | 2 | 0 | cephalosporin | antibacterial drug |
| talniflumate talniflumate: an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma | 2.08 | 1 | 0 | benzofurans | |
| fenoldopam mesylate [no description available] | 2.08 | 1 | 0 | benzazepine | |
| fialuridine [no description available] | 3.23 | 1 | 0 | ||
| 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. | 3.86 | 3 | 0 | cephalosporin | antibacterial 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. | 2.08 | 1 | 0 | fluoroquinolone antibiotic; monocarboxylic acid; N-alkylpiperazine; N-arylpiperazine; quinolone antibiotic; quinolone | antibacterial drug; antiinfective agent; DNA synthesis inhibitor |
| pirazolac [no description available] | 2.03 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 3.23 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| haloperidol decanoate [no description available] | 3.23 | 1 | 0 | organic 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. | 3.61 | 2 | 0 | ||
| 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). | 9.12 | 4 | 0 | delta-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 | 2.08 | 1 | 0 | aminopyridine | |
| tolrestat tolrestat: RN & structure given in first source | 3.23 | 1 | 0 | naphthalenes | EC 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. | 2.46 | 2 | 0 | aromatic ketone | |
| stepronin [no description available] | 2.08 | 1 | 0 | N-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. | 3.86 | 3 | 0 | delta-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. | 2.08 | 1 | 0 | benzodioxine; 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. | 2.08 | 1 | 0 | dimethoxybenzene | |
| 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. | 3.23 | 1 | 0 | ||
| 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. | 3.57 | 2 | 0 | 3-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. | 3.61 | 2 | 0 | N-acylurea | antineoplastic 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. | 2.08 | 1 | 0 | hydrochloride | adrenergic uptake inhibitor; antidepressant |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 3.57 | 2 | 0 | aromatic 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. | 3.61 | 2 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| alpidem [no description available] | 3.23 | 1 | 0 | imidazoles | |
| eproxindine eproxindine: structure given in first source | 2.03 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| (S)-nomifensine (S)-nomifensine : The S enantiomer of nomifensine. | 2.03 | 1 | 0 | nomifensine | |
| fosphenytoin fosphenytoin: structure given in first & second source | 3.23 | 1 | 0 | imidazolidine-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. | 2.08 | 1 | 0 | naphthoic 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. | 3.23 | 1 | 0 | aromatic 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. | 18.73 | 250 | 18 | 3-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. | 2.08 | 1 | 0 | imidazoquinoline | antineoplastic 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. | 3.23 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| (2S)-2-[[oxo-(4-propan-2-ylcyclohexyl)methyl]amino]-3-phenylpropanoic acid [no description available] | 2.03 | 1 | 0 | phenylalanine derivative | |
| 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. | 2.08 | 1 | 0 | heteroarylpiperidine; 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. | 2.5 | 2 | 0 | adamantanes; 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. | 3.23 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| aromasil [no description available] | 3.61 | 2 | 0 | 17-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] | 2.08 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | |
| zileuton [no description available] | 3.61 | 2 | 0 | 1-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. | 3.23 | 1 | 0 | methyl 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. | 3.61 | 2 | 0 | phosphonic 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. | 3.57 | 2 | 0 | beta-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. | 3.57 | 2 | 0 | pyranoindolizinoquinoline | antineoplastic 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. | 3.61 | 2 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gemcitabine hydrochloride [no description available] | 2.08 | 1 | 0 | hydrochloride; 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. | 3.23 | 1 | 0 | organofluorine 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 | 3.23 | 1 | 0 | benzenes; 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. | 3.61 | 2 | 0 | aromatic 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. | 3.23 | 1 | 0 | alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester | intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative |
| atorvastatin calcium anhydrous [no description available] | 2.08 | 1 | 0 | organic calcium salt | |
| atorvastatin [no description available] | 3.57 | 2 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 3.86 | 3 | 0 | monothioacetal; 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. | 2.08 | 1 | 0 | duloxetine hydrochloride | antidepressant |
| duloxetine [no description available] | 3.23 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 3.23 | 1 | 0 | carbamate 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. | 3.61 | 2 | 0 | biphenylyltetrazole; 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. | 3.23 | 1 | 0 | ||
| 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. | 3.57 | 2 | 0 | 1,2-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. | 3.86 | 3 | 0 | oxazolidinone; 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. | 2.08 | 1 | 0 | 6-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. | 3.86 | 3 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| tasosartan tasosartan: angiotensin II antagonist; structure given in first source | 3.23 | 1 | 0 | biphenyls | |
| 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 | 3.23 | 1 | 0 | organochlorine 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. | 3.23 | 1 | 0 | L-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. | 3.23 | 1 | 0 | carbamate 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 | 3.65 | 2 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| caloreen caloreen: glucose polymer with average length of five glucose units for dietary energy supplement. dextrin : Glucans produced by the hydrolysis of starch or glycogen. They are mixtures of polymers of D-glucose units linked by alpha(1->4) or alpha(1->6) glycosidic bonds. | 2.1 | 1 | 0 | ||
| pipothiazine pipothiazine: was heading 1975-94 (see under PHENOTHIAZINE TRANQUILIZERS 1975-90); use PHENOTHIAZINES to search PIPOTHIAZINE 1975-94; a member of the family of phenothiazine tranquilizers | 2.03 | 1 | 0 | ||
| paroxetine hydrochloride paroxetine hydrochloride : The hydrochloride salt of paroxetine. It is an antidepressant drug. | 2.08 | 1 | 0 | hydrochloride | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| bupropion hydrochloride [no description available] | 2.08 | 1 | 0 | aromatic 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. | 2.08 | 1 | 0 | hydrochloride | adrenergic 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. | 3.23 | 1 | 0 | ||
| cefprozil [no description available] | 3.23 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| doxazosin mesylate Cardura: Trade name in United States. | 2.08 | 1 | 0 | methanesulfonate salt | geroprotector |
| 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. | 3.61 | 2 | 0 | acetylenic 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. | 3.61 | 2 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| 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. | 2.08 | 1 | 0 | 2-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. | 2.08 | 1 | 0 | hydrochloride; 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. | 3.23 | 1 | 0 | aromatic 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. | 3.61 | 2 | 0 | azacycloalkane; 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] | 3.61 | 2 | 0 | carbamate 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. | 3.57 | 2 | 0 | acetamides; 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] | 5.07 | 3 | 3 | steroid ester | |
| ticlopidine hydrochloride [no description available] | 2.08 | 1 | 0 | hydrochloride | |
| epirubicin hydrochloride [no description available] | 2.08 | 1 | 0 | ||
| histamine phosphate histamine phosphate : A phosphate salt that is the diphosphate salt of histamine. | 3.23 | 1 | 0 | phosphate salt | histamine agonist |
| tilbroquinol [no description available] | 3.23 | 1 | 0 | organohalogen compound; quinolines | |
| bendamustine [no description available] | 3.23 | 1 | 0 | benzimidazoles | |
| 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. | 3.23 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| ebrotidine ebrotidine: an H2-receptor antagonist and gastric mucosa protector | 3.23 | 1 | 0 | sulfonamide | |
| pazufloxacin [no description available] | 2.08 | 1 | 0 | quinolines | |
| repaglinide [no description available] | 3.86 | 3 | 0 | piperidines | |
| 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. | 3.9 | 3 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| dexfenfluramine Dexfenfluramine: The S-isomer of FENFLURAMINE. It is a serotonin agonist and is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity.. (S)-fenfluramine : The S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects. | 2.03 | 1 | 0 | fenfluramine | appetite depressant; serotonergic agonist; serotonin uptake inhibitor |
| 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. | 5.29 | 4 | 3 | 1,2,3-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. | 2.08 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | dichlorobenzene; 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. | 3.61 | 2 | 0 | 1,1-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. | 3.62 | 2 | 0 | organic peroxide; sesquiterpene lactone | antimalarial; plant metabolite |
| brinzolamide brinzolamide: an antiglaucoma agent | 2.08 | 1 | 0 | sulfonamide; 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 | 2.46 | 2 | 0 | 3-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. | 2.08 | 1 | 0 | artemisinin derivative; cyclic acetal; organic peroxide; semisynthetic derivative; sesquiterpenoid | antimalarial |
| fenflumizole fenflumizole: structure in first source | 2.03 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | acetamides; organosulfonic acid | environmental contaminant; neurotransmitter agent; xenobiotic |
| isaxonine isaxonine: promotes nerve growth | 3.23 | 1 | 0 | aminopyrimidine | |
| 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. | 3.23 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 3.61 | 2 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| 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. | 3.61 | 2 | 0 | 1,2-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. | 3.23 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| loxapine succinate [no description available] | 2.08 | 1 | 0 | succinate salt | geroprotector |
| fenoxypropazine [no description available] | 3.23 | 1 | 0 | aromatic 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. | 3.61 | 2 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| betamipron [no description available] | 2.08 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| uroxatral [no description available] | 2.08 | 1 | 0 | hydrochloride | |
| aceclofenac [no description available] | 3.61 | 2 | 0 | amino 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] | 3.23 | 1 | 0 | imidazoles | |
| thiocolchicoside [no description available] | 2.08 | 1 | 0 | glycoside | |
| prednisolone phosphate prednisolone phosphate: RN given refers to (11 beta)-isomer. prednisolone phosphate : A synthetic glucocorticoid resulting from the formal condensation of the 21-hydroxy group of prednisolone with one of the hydroxy groups of phosphoric acid. It is a prodrug for prednisolone that is activated in vivo by phosphatases. | 2.03 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid; glucocorticoid; steroid phosphate; tertiary alpha-hydroxy ketone | anti-inflammatory agent; antineoplastic agent; glucocorticoid receptor agonist; prodrug |
| (S)-flurbiprofen [no description available] | 2.03 | 1 | 0 | flurbiprofen | |
| methanesulfonamide [no description available] | 3.27 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | carbapenems | |
| 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. | 3.57 | 2 | 0 | hydroxy-1,2-naphthoquinone | |
| rivastigmine [no description available] | 3.23 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 3.23 | 1 | 0 | carbazoles | |
| 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. | 3.57 | 2 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 3.61 | 2 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| tamiflu [no description available] | 2.08 | 1 | 0 | phosphate salt | |
| trifluoromethylsulfonamide trifluoromethylsulfonamide: RN given refers to parent | 3.27 | 1 | 0 | ||
| bexarotene [no description available] | 3.61 | 2 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic agent |
| s20098 [no description available] | 2.08 | 1 | 0 | acetamides | |
| flunisolide flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones | 2.46 | 2 | 0 | 11beta-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 |
| 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. | 2.08 | 1 | 0 | organoammonium salt | analgesic; 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. | 3.86 | 3 | 0 | macrolide antibiotic | antibacterial 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. | 2.08 | 1 | 0 | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic 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] | 3.57 | 2 | 0 | peptide | |
| gliquidone gliquidone: structure; RN given refers to parent cpd | 2.08 | 1 | 0 | isoquinolines | |
| lekoptin (S)-verapamil : A 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile that has S configuration. | 2.03 | 1 | 0 | 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile | |
| tarenflurbil tarenflurbil: R-enantiomer of flurbiprofen but not a COX inhibitor; modulates NF-kB, gamma-secretase, amyloid beta-protein; | 2.03 | 1 | 0 | flurbiprofen | |
| mci 9038 [no description available] | 3.23 | 1 | 0 | peptide | |
| lopinavir [no description available] | 2.08 | 1 | 0 | amphetamines; dicarboxylic acid diamide | anticoronaviral agent; antiviral drug; HIV protease inhibitor |
| 16-dehydropregnenolone 16,17-didehydropregnenolone : A 3beta-hydroxy-Delta(5)-steroid that is pregnenolone with a double bond between positions 16 and 17. | 2.04 | 1 | 0 | 20-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; enone | |
| moxifloxacin hydrochloride moxifloxacin hydrochloride : A hydrochloride comprising equimolar amounts of moxifloxacin and hydrogen chloride. | 2.08 | 1 | 0 | hydrochloride | antibacterial 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. | 3.91 | 3 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| mizoribine [no description available] | 2.08 | 1 | 0 | imidazoles | anticoronaviral agent |
| sr141716 [no description available] | 2.08 | 1 | 0 | amidopiperidine; 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. | 3.86 | 3 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| eudragit-e Eudragit-E: a cationic polymer, used as a embolic material for arteriovenous malformations and as a taste masker | 2.48 | 2 | 0 | ||
| racecadotril racecadotril: parenterally active enkephalinase inhibitor | 2.08 | 1 | 0 | N-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 | 3.23 | 1 | 0 | alpha-amino acid ester; dicarboxylic acid monoester; ethyl ester; organic heterobicyclic compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| tadalafil [no description available] | 6.07 | 7 | 1 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| ibuprofen, (r)-isomer [no description available] | 2.03 | 1 | 0 | ibuprofen | |
| 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. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
| nitisinone [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| plavix [no description available] | 2.08 | 1 | 0 | azaheterocycle sulfate salt; organoammonium sulfate salt | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| clofarabine [no description available] | 3.61 | 2 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| 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. | 3.86 | 3 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 3.61 | 2 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| 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. | 3.57 | 2 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| mk 0663 [no description available] | 2.08 | 1 | 0 | bipyridines; organochlorine compound; sulfone | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| gefitinib [no description available] | 3.86 | 3 | 0 | aromatic 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. | 3.61 | 2 | 0 | benzocycloheptapyridine | anti-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. | 3.23 | 1 | 0 | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
| methotrexate [no description available] | 4.09 | 4 | 0 | dicarboxylic 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] | 17.27 | 82 | 35 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| rufinamide rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source | 3.23 | 1 | 0 | aromatic amide; heteroarene | |
| sulbactam [no description available] | 2.08 | 1 | 0 | penicillanic acids | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 3.61 | 2 | 0 | biphenyls | |
| dexpanthenol dexpanthenol: The alcohol of pantothenic acid | 3.23 | 1 | 0 | amino 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. | 3.23 | 1 | 0 | sulfonamide | prodrug |
| abiraterone [no description available] | 8.65 | 9 | 5 | 3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor |
| fce 28260 (22RS-N-1,1,1-trifluoro-2-phenylprop-2-yl)-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide: structure given in first source | 3.27 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| 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. | 3.57 | 2 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| lexapro Lexapro: Trade name of escitalopram, the active S-enantiomer of the racemic citalopram. | 2.08 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | N-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. | 3.61 | 2 | 0 | secondary 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). | 3.23 | 1 | 0 | carbohydrazide | antiviral 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. | 3.86 | 3 | 0 | 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; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV 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). | 3.61 | 2 | 0 | azetidines; 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. | 3.23 | 1 | 0 | carbapenemcarboxylic 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. | 3.61 | 2 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| 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). | 3.62 | 2 | 0 | benzazepine | aquaretic; 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. | 3.57 | 2 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| pralnacasan pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source | 3.23 | 1 | 0 | ||
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 3.23 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 3.23 | 1 | 0 | isoquinolines | |
| 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. | 3.23 | 1 | 0 | methyl phenyl(piperidin-2-yl)acetate | adrenergic agent |
| xamoterol Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist. | 2.08 | 1 | 0 | morpholines | |
| disopyramide, (s)-isomer [no description available] | 2.03 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | methoxynaphthalene; 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. | 3.62 | 2 | 0 | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| lubiprostone [no description available] | 3.23 | 1 | 0 | ||
| isradipine, (s)-isomer [no description available] | 2.03 | 1 | 0 | ||
| olmesartan olmesartan: an active metabolite of CS 866 | 2.03 | 1 | 0 | biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent |
| telbivudine [no description available] | 3.61 | 2 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) 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. | 3.23 | 1 | 0 | amino 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. | 3.23 | 1 | 0 | antibiotic 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. | 3.23 | 1 | 0 | corticosteroid 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. | 3.23 | 1 | 0 | ||
| 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). | 2.02 | 1 | 0 | amino acid zwitterion; angiotensin II | human metabolite |
| fiduxosin fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source | 3.23 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | ||
| erlotinib [no description available] | 3.23 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| ketoprofen [no description available] | 2.03 | 1 | 0 | ||
| etravirine [no description available] | 3.23 | 1 | 0 | aminopyrimidine; 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. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 3.61 | 2 | 0 | indanes | |
| lapatinib [no description available] | 3.23 | 1 | 0 | furans; 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. | 3.23 | 1 | 0 | carbamate 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. | 3.61 | 2 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| bms204352 BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source | 2.08 | 1 | 0 | ||
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 3.61 | 2 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 3.61 | 2 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| sorafenib [no description available] | 3.23 | 1 | 0 | (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] | 3.61 | 2 | 0 | aromatic 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. | 4.24 | 3 | 1 | isoquinolines | |
| regadenoson [no description available] | 3.23 | 1 | 0 | purine 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. | 3.61 | 2 | 0 | N-acyl-amino acid | |
| vincaleukoblastine [no description available] | 3.61 | 2 | 0 | acetate 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] | 2.08 | 1 | 0 | organic sulfate salt | antineoplastic agent; geroprotector |
| mibolerone mibolerone: prevents estrus in animals & prevents experimental lymphoid leukosis; minor descriptor (80-83); on-line & Index Medicus search NANDROLONE/AA (80-83); RN given refers to (7alpha,17beta)-isomer; structure. mibolerone : An androgen that is nalandrone carrying two methyl substituents at positions 7alpha and 17. | 2.04 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid | anabolic agent; androgen |
| benzarone benzarone: antihemorrhagic agent; structure | 3.23 | 1 | 0 | 1-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. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| pnu 120596 1-(5-chloro-2,4-dimethoxyphenyl)-3-(5-methylisoxazol-3-yl)urea: an alpha7nAChR agonist; structure in first source | 2.11 | 1 | 0 | ureas | |
| wortmannin [no description available] | 2.08 | 1 | 0 | acetate 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] | 3.61 | 2 | 0 | amino 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. | 3.61 | 2 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| 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. | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | oxytocic; vasodilator agent |
| 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. | 3.61 | 2 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| 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. | 3.86 | 3 | 0 | cinchona alkaloid | alpha-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. | 3.61 | 2 | 0 | alpha,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. | 3.23 | 1 | 0 | 1-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. | 3.23 | 1 | 0 | beta-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. | 2.46 | 2 | 0 | cardenolide glycoside | EC 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. | 3.86 | 3 | 0 | L-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. | 3.23 | 1 | 0 | acetate 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. | 3.57 | 2 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| perindopril erbumine [no description available] | 2.08 | 1 | 0 | addition compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| miglitol [no description available] | 3.61 | 2 | 0 | piperidines | |
| 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. | 3.23 | 1 | 0 | L-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. | 2.08 | 1 | 0 | organic bromide salt; quaternary ammonium salt | muscle relaxant; neuromuscular agent |
| linezolid [no description available] | 3.86 | 3 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| chloramphenicol palmitate chloramphenicol palmitate: RN given refers to ((R-(R*,R*))-isomer) | 2.03 | 1 | 0 | hexadecanoate ester | |
| clindamycin phosphate [no description available] | 3.23 | 1 | 0 | ||
| pemirolast potassium salt [no description available] | 2.08 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | 3-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] | 3.23 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| ao 128 AO 128: alpha-glucosidase inhibitor; structure given in first source | 2.08 | 1 | 0 | organic 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. | 2.08 | 1 | 0 | 11beta-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. | 3.23 | 1 | 0 | 1-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. | 2.08 | 1 | 0 | 11beta-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. | 2.48 | 2 | 0 | cyclodextrin | |
| 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. | 5.51 | 4 | 0 | retinoic 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). | 3.23 | 1 | 0 | retinol; 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. | 4.27 | 5 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| 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). | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; 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. | 3.57 | 2 | 0 | 2-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. | 2.08 | 1 | 0 | alpha,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. | 3.59 | 2 | 0 | ||
| lycopene [no description available] | 5.16 | 4 | 0 | acyclic carotene | antioxidant; plant metabolite |
| fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus. | 3.23 | 1 | 0 | epoxide; 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. | 3.61 | 2 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| octreotide [no description available] | 3.23 | 1 | 0 | ||
| eptifibatide [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| decitabine [no description available] | 3.61 | 2 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 3.61 | 2 | 0 | aromatic 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] | 2.08 | 1 | 0 | anthracycline; 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) | 3.23 | 1 | 0 | actinomycin | mutagen |
| 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. | 3.86 | 3 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| enkephalin, leucine Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties. | 3.27 | 1 | 0 | pentapeptide; peptide zwitterion | analgesic; delta-opioid receptor agonist; human metabolite; mu-opioid receptor agonist; neurotransmitter; rat metabolite |
| 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. | 3.23 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 3.61 | 2 | 0 | aromatic 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. | 2.08 | 1 | 0 | C-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. | 3.23 | 1 | 0 | antibiotic 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). | 3.23 | 1 | 0 | flavin; 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. | 3.23 | 1 | 0 | one-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. | 3.23 | 1 | 0 | arsenic oxide | antineoplastic agent; insecticide |
| bromochloroacetic acid Keratins: A class of fibrous proteins or scleroproteins that represents the principal constituent of EPIDERMIS; HAIR; NAILS; horny tissues, and the organic matrix of tooth ENAMEL. Two major conformational groups have been characterized, alpha-keratin, whose peptide backbone forms a coiled-coil alpha helical structure consisting of TYPE I KERATIN and a TYPE II KERATIN, and beta-keratin, whose backbone forms a zigzag or pleated sheet structure. alpha-Keratins have been classified into at least 20 subtypes. In addition multiple isoforms of subtypes have been found which may be due to GENE DUPLICATION.. bromochloroacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by bromine while a second is replaced by chlorine. A low-melting (27.5-31.5degreeC), hygroscopic crystalline solid, it can be formed during the disinfection (by chlorination) of water that contains bromide ions and organic matter, so can occur in drinking water as a byproduct of the disinfection process. | 2.03 | 1 | 0 | 2-bromocarboxylic acid; monocarboxylic acid; organochlorine compound | |
| sr 90107 fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux. | 3.23 | 1 | 0 | ||
| meglumine iodipamide [no description available] | 3.23 | 1 | 0 | organoammonium salt | radioopaque 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. | 3.23 | 1 | 0 | peptide hormone; tripeptide | human metabolite |
| chloroquine diphosphate [no description available] | 2.03 | 1 | 0 | chloroquine | |
| dextromethadone D-methadone: an NMDA receptor antagonist analgesic that lacks opioid activity. dextromethadone : A 6-(dimethylamino)-4,4-diphenylheptan-3-one that has (S)-configuration. It is the less active enantiomer of methadone and has very little activity on opioid receptors and mainly responsible for the inhibition of hERG K+ channels and thus for cardiac toxicity. The drug is currently under clinical development for the treatment of major depressive disorder. | 2.03 | 1 | 0 | 6-(dimethylamino)-4,4-diphenylheptan-3-one | NMDA receptor antagonist; opioid analgesic |
| 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. | 3.61 | 2 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| s 1033 [no description available] | 3.23 | 1 | 0 | (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. | 2.08 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; androstanoid; epoxy steroid; nitrile | abortifacient; antineoplastic agent; EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor |
| 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. | 2.08 | 1 | 0 | acetate salt | antineoplastic agent; gonadotropin releasing hormone agonist |
| leuprolide Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty. | 4.58 | 2 | 0 | oligopeptide | anti-estrogen; antineoplastic 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. | 3.86 | 3 | 0 | pyrimidinethione | antidote 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. | 3.23 | 1 | 0 | ethyl 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. | 3.61 | 2 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| dexketoprofen dexketoprofen : A monocarboxylic acid that is (S)-hydratropic acid substituted at position 3 on the phenyl ring by a benzoyl group. A cyclooxygenase inhibitor, it is used to relieve short-term pain, such as muscular pain, dental pain and dysmenorrhoea. | 2.03 | 1 | 0 | benzophenones; monocarboxylic acid | cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| 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). | 2.08 | 1 | 0 | sulpiride | antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist |
| caffeic acid trans-caffeic acid : The trans-isomer of caffeic acid. | 2.41 | 1 | 0 | caffeic acid | geroprotector; mouse metabolite |
| ondansetron, (s)-isomer [no description available] | 2.03 | 1 | 0 | ||
| 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'. | 3.23 | 1 | 0 | 1,4,5,6-tetrahydropyrimidines; carboxamidine; thiophenes | antinematodal drug |
| thiothixene [no description available] | 3.23 | 1 | 0 | N-methylpiperazine | anticoronaviral 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. | 3.86 | 3 | 0 | zopiclone | central 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. | 3.18 | 1 | 0 | aromatic 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. | 3.23 | 1 | 0 | diarylmethane | |
| 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. | 3.86 | 3 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid 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. | 2.08 | 1 | 0 | diarylmethane; 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. | 3.9 | 3 | 0 | monocarboxylic 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] | 3.23 | 1 | 0 | acetylenic 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. | 2.08 | 1 | 0 | monocarboxylic acid; thiazolidines | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| drotaverin drotaverin: Hungarian drug; RN given refers to parent cpd; structure | 2.08 | 1 | 0 | isoquinolines | |
| 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. | 3.23 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic 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. | 3.23 | 1 | 0 | dicarboxylic 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. | 3.57 | 2 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| streptozocin [no description available] | 3.23 | 1 | 0 | ||
| tamoxifen [no description available] | 3.61 | 2 | 0 | stilbenoid; 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 |
| nadp [no description available] | 2.25 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 3.23 | 1 | 0 | ||
| 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. | 2.08 | 1 | 0 | 11alpha-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. | 3.23 | 1 | 0 | carbohydrate-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. | 2.08 | 1 | 0 | cyclodepsipeptide; 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. | 3.23 | 1 | 0 | C-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 | 3.23 | 1 | 0 | ||
| hmr 3647 [no description available] | 3.86 | 3 | 0 | ||
| latoconazole latoconazole: RN refers to cpd without isomeric designation; latoconazole is (E)-isomer; structure given in first source | 2.08 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug | |
| maraviroc [no description available] | 3.61 | 2 | 0 | tropane alkaloid | |
| toremifene citrate [no description available] | 2.08 | 1 | 0 | stilbenoid | anticoronaviral 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. | 4.09 | 2 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| 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). | 3.61 | 2 | 0 | beta-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. | 3.23 | 1 | 0 | amino disaccharide; glycosylgalactose derivative; iduronic acids; oligosaccharide sulfate | |
| dolasetron [no description available] | 3.23 | 1 | 0 | indolyl carboxylic acid | |
| gestodene Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer | 2.08 | 1 | 0 | steroid | estrogen |
| 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. | 3.61 | 2 | 0 | beta-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] | 3.61 | 2 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| fospropofol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| azilect [no description available] | 2.08 | 1 | 0 | ||
| rasagiline [no description available] | 3.23 | 1 | 0 | indanes; 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). | 3.61 | 2 | 0 | 1,3-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 |
| tocainide, (s)-isomer [no description available] | 2.03 | 1 | 0 | ||
| sodium dodecyl sulfate Sodium Dodecyl Sulfate: An anionic surfactant, usually a mixture of sodium alkyl sulfates, mainly the lauryl; lowers surface tension of aqueous solutions; used as fat emulsifier, wetting agent, detergent in cosmetics, pharmaceuticals and toothpastes; also as research tool in protein biochemistry.. sodium dodecyl sulfate : An organic sodium salt that is the sodium salt of dodecyl hydrogen sulfate. | 2.08 | 1 | 0 | organic sodium salt | detergent; protein denaturant |
| 17-ketosteroids 17-Ketosteroids: Steroids that contain a ketone group at position 17.. 17-oxo steroid : Any oxo steroid carrying the oxo group at position 17. | 2.13 | 1 | 0 | ||
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 3.61 | 2 | 0 | triazolopyrazine; 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. | 3.61 | 2 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| quercetin [no description available] | 2.08 | 1 | 0 | 7-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 |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 3.86 | 3 | 0 | D3 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] | 2.08 | 1 | 0 | prostaglandins E | anticoagulant; 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. | 3.61 | 2 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| cholecalciferol Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.. calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone. | 2.11 | 1 | 0 | D3 vitamins; hydroxy seco-steroid; seco-cholestane; secondary alcohol; steroid hormone | geroprotector; human metabolite |
| genistein [no description available] | 3.18 | 1 | 0 | 7-hydroxyisoflavones | antineoplastic 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. | 3.23 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| clavulanic acid Clavulanic Acid: A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.. clavulanate : The conjugate base of clavulanic acid.. clavulanic acid : Antibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes. | 2.03 | 1 | 0 | oxapenam | antibacterial drug; anxiolytic drug; bacterial metabolite; EC 3.5.2.6 (beta-lactamase) inhibitor |
| 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. | 3.86 | 3 | 0 | 11beta-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. | 3.61 | 2 | 0 | ||
| 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. | 3.61 | 2 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 3.57 | 2 | 0 | aliphatic 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. | 3.23 | 1 | 0 | isoquinolines | |
| 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. | 2.08 | 1 | 0 | maleate salt | anti-allergic agent |
| dexchlorpheniramine maleate [no description available] | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | ||
| 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. | 3.61 | 2 | 0 | carboxylic 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. | 3.61 | 2 | 0 | 2-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] | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| morin morin: a light yellowish pigment found in the wood of old fustic (Chlorophora tinctoria). morin : A pentahydroxyflavone that is 7-hydroxyflavonol bearing three additional hydroxy substituents at positions 2' 4' and 5. | 7.25 | 1 | 0 | 7-hydroxyflavonol; pentahydroxyflavone | angiogenesis modulating agent; anti-inflammatory agent; antibacterial agent; antihypertensive agent; antineoplastic agent; antioxidant; EC 5.99.1.2 (DNA topoisomerase) inhibitor; hepatoprotective agent; metabolite; neuroprotective agent |
| l 660,711 [no description available] | 2.08 | 1 | 0 | quinolines | |
| 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. | 2.08 | 1 | 0 | (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. | 2.08 | 1 | 0 | amidobenzoic 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. | 3.23 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| imipenem [no description available] | 2.08 | 1 | 0 | carbapenems | |
| etretinate retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof. | 2.08 | 1 | 0 | enoate 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. | 3.61 | 2 | 0 | retinoic acid | antineoplastic 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. | 2.08 | 1 | 0 | organoammonium salt | anti-asthmatic drug; H1-receptor antagonist |
| epoprostenol [no description available] | 3.23 | 1 | 0 | prostaglandins I | mouse metabolite |
| indocyanine green [no description available] | 3.23 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| dinoprost tromethamine [no description available] | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | N-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. | 3.23 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| rosuvastatin calcium S 4522: structure in first source | 2.08 | 1 | 0 | N-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. | 2.08 | 1 | 0 | allylamine antifungal drug; hydrochloride | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor |
| ethamolin monoethanolamine oleate: used for treatment of pyogenic granuloma | 3.23 | 1 | 0 | long-chain fatty acid | |
| alatrofloxacin mesylate [no description available] | 3.23 | 1 | 0 | ||
| codeine [no description available] | 3.57 | 2 | 0 | morphinane 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 | 3.61 | 2 | 0 | homodetic cyclic peptide | anti-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] | 2.08 | 1 | 0 | antibiotic 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. | 3.61 | 2 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| estropipate estropipate: used therapeutically in menopausal patients | 3.23 | 1 | 0 | piperazinium 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. | 3.57 | 2 | 0 | morphinane 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. | 3.61 | 2 | 0 | pyrrolidin-2-ones | anticonvulsant; 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. | 3.23 | 1 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nabilone nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure | 3.23 | 1 | 0 | ||
| nalmefene nalmefene: RN given refers to 5-alpha isomer | 2.08 | 1 | 0 | morphinane 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. | 3.86 | 3 | 0 | morphinane 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. | 3.23 | 1 | 0 | organic 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) | 3.23 | 1 | 0 | morphinane 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. | 3.23 | 1 | 0 | phylloquinones; vitamin K | cofactor; human metabolite; plant metabolite |
| proscillaridin Proscillaridin: A cardiotonic glycoside isolated from Scilla maritima var. alba (Squill). | 2.03 | 1 | 0 | organic molecular entity | |
| 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. | 8.84 | 3 | 0 | antibiotic 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. | 3.86 | 3 | 0 | cyclic 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. | 3.23 | 1 | 0 | ||
| 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. | 3.57 | 2 | 0 | morphinane 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] | 2.08 | 1 | 0 | ||
| acipimox acipimox: lipolysis inhibitor | 2.08 | 1 | 0 | pyrazinecarboxylic acid | |
| atosiban [no description available] | 2.08 | 1 | 0 | oligopeptide | |
| 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. | 3.23 | 1 | 0 | amphetamines; 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. | 2.08 | 1 | 0 | monocarboxylic acid amide | antiglaucoma drug; antihypertensive agent |
| clobetasol Clobetasol: A derivative of PREDNISOLONE with high glucocorticoid activity and low mineralocorticoid activity. Absorbed through the skin faster than FLUOCINONIDE, it is used topically in treatment of PSORIASIS but may cause marked adrenocortical suppression.. clobetasol : A 3-oxo-Delta(1),Delta(4)-steroid that is 16beta-methylpregna-1,4-diene-3,20-dione bearing hydroxy groups at the 11beta and 17alpha positions, fluorine at position 9, and a chlorine substituent at position 21. It is used as its 17alpha-propionate ester to treat various skin disorders, including exzema and psoriasis. | 2.55 | 2 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid; chlorinated steroid; fluorinated steroid; glucocorticoid; tertiary alpha-hydroxy ketone | anti-inflammatory drug; SMO receptor agonist |
| 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. | 3.23 | 1 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 3.23 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| fluticasone Fluticasone: A STEROID with GLUCOCORTICOID RECEPTOR activity that is used to manage the symptoms of ASTHMA; ALLERGIC RHINITIS, and ATOPIC DERMATITIS.. fluticasone : A trifluorinated corticosteroid used in the form of its propionate ester for treatment of allergic rhinitis. | 2.03 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 3-oxo-Delta(4) steroid; corticosteroid; fluorinated steroid; thioester | anti-allergic agent; anti-asthmatic drug |
| 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. | 5.92 | 2 | 1 | organic molecular entity | |
| 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. | 2.08 | 1 | 0 | isopropyl ester; prostaglandins Falpha; triol | antiglaucoma drug; antihypertensive agent; EC 4.2.1.1 (carbonic anhydrase) inhibitor; prodrug |
| 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. | 3.57 | 2 | 0 | organic heteropentacyclic compound | mu-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. | 3.61 | 2 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 3.23 | 1 | 0 | acetate 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 | 6.13 | 4 | 2 | indolecarboxamide | |
| 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. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 3.23 | 1 | 0 | monocarboxylic 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 |
| (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. | 3.86 | 3 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| molsidomine [no description available] | 2.08 | 1 | 0 | ethyl ester; morpholines; oxadiazole; zwitterion | antioxidant; apoptosis inhibitor; cardioprotective agent; nitric oxide donor; vasodilator agent |
| levorphanol Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. | 3.23 | 1 | 0 | morphinane 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. | 3.57 | 2 | 0 | cyclopropanes; 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. | 3.23 | 1 | 0 | 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene | antitussive; 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. | 3.61 | 2 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 3.61 | 2 | 0 | cephalosporin | antibacterial 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. | 3.61 | 2 | 0 | dipeptide | EC 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. | 3.23 | 1 | 0 | benzazepine; 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. | 3.61 | 2 | 0 | azabicycloalkane; 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. | 3.23 | 1 | 0 | ||
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 3.61 | 2 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| 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) | 3.23 | 1 | 0 | styrenes | |
| 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. | 2.08 | 1 | 0 | maleate salt | antihypertensive 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). | 3.57 | 2 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| trientine hydrochloride [no description available] | 3.23 | 1 | 0 | ||
| n-methylscopolamine bromide scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. | 3.23 | 1 | 0 | ||
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic 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. | 3.61 | 2 | 0 | dicarboxylic 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. | 3.23 | 1 | 0 | amidoxime; 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] | 3.23 | 1 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 3.23 | 1 | 0 | 1,2,4-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. | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| pafuramidine pafuramidine: a prodrug of furamidine | 3.23 | 1 | 0 | ||
| ceftazidime [no description available] | 3.23 | 1 | 0 | cephalosporin; 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. | 3.86 | 3 | 0 | dicarboxylic 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. | 3.61 | 2 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 3.61 | 2 | 0 | peptide | |
| 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. | 3.23 | 1 | 0 | monocarboxylic acid amide; monomethoxybenzene | antihypertensive agent |
| famotidine [no description available] | 3.61 | 2 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| 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. | 3.23 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| (R)-citalopram (R)-citalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has R-configuration at the chiral centre. It is the inactive enantiomer of citalopram. | 2.03 | 1 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | |
| cci 15641 [no description available] | 2.08 | 1 | 0 | cephalosporin | |
| selenium Selenium: An element with the atomic symbol Se, atomic number 34, and atomic weight 78.97. It is an essential micronutrient for mammals and other animals but is toxic in large amounts. Selenium protects intracellular structures against oxidative damage. It is an essential component of GLUTATHIONE PEROXIDASE. | 5.87 | 6 | 0 | chalcogen; nonmetal atom | micronutrient |
| cefpodoxime [no description available] | 3.23 | 1 | 0 | carboxylic 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. | 3.23 | 1 | 0 | azabicycloalkane; 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. | 2.08 | 1 | 0 | fumarate salt | antiviral drug; HIV-1 reverse transcriptase inhibitor; prodrug |
| imidafenacin imidafenacin: structure in first source | 5.2 | 3 | 3 | diarylmethane | |
| 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. | 2.08 | 1 | 0 | brompheniramine maleate | anti-allergic agent; H1-receptor antagonist |
| rifaximin [no description available] | 3.61 | 2 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 3.61 | 2 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| rosiglitazone-metformin combination rosiglitazone-metformin combination: a combination of metformin and rosiglitazone used for treating type 2 diabetes | 2.01 | 1 | 0 | ||
| 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. | 2.08 | 1 | 0 | carboxylic acid; carboxylic ester; cephalosporin | antibacterial drug; prodrug |
| ceftizoxime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 3.57 | 2 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| fluphenazine [no description available] | 2.08 | 1 | 0 | ||
| 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. | 3.86 | 3 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| dantrolene [no description available] | 3.23 | 1 | 0 | ||
| roxithromycin (E)-roxithromycin : A major geometrical isomer of roxithromycin. | 2.08 | 1 | 0 | roxithromycin | environmental contaminant; xenobiotic |
| cefdinir [no description available] | 3.61 | 2 | 0 | cephalosporin; ketoxime | antibacterial drug |
| etonogestrel [no description available] | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| bisoprolol, fumarate (1:1) salt [no description available] | 2.08 | 1 | 0 | ||
| artesunate artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether | 2.08 | 1 | 0 | artemisinin derivative; cyclic acetal; dicarboxylic acid monoester; hemisuccinate; semisynthetic derivative; sesquiterpenoid | antimalarial; antineoplastic agent; ferroptosis inducer |
| etoposide phosphate [no description available] | 2.08 | 1 | 0 | furonaphthodioxole | |
| ciclesonide ciclesonide: nasal spray approved for seasonal and perennial allergic rhinitis | 2.08 | 1 | 0 | organic molecular entity | |
| temsirolimus [no description available] | 3.61 | 2 | 0 | macrolide lactam | |
| vilazodone vilazodone : A 1-benzofuran that is 5-(piperazin-1-yl}-1-benzofuran-2-carboxamide having a (5-cyanoindol-3-yl)butyl group attached at position N-4 on the piperazine ring. Used for the treatment of major depressive disorder. | 3.27 | 1 | 0 | 1-benzofurans; indoles; monocarboxylic acid amide; N-alkylpiperazine; N-arylpiperazine; nitrile | antidepressant; serotonergic agonist; serotonin uptake inhibitor |
| tekturna [no description available] | 2.08 | 1 | 0 | fumarate salt | antihypertensive agent |
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 3.23 | 1 | 0 | diarylmethane | |
| bibx 1382bs BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001 | 3.23 | 1 | 0 | substituted aniline | |
| vildagliptin [no description available] | 2.08 | 1 | 0 | amino acid amide | |
| fesoterodine fesoterodine: a muscarinic antagonist for treatment of overactive bladder | 3.23 | 1 | 0 | diarylmethane | |
| sgd 301-76 [no description available] | 2.08 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; organic nitrate salt | antiinfective agent |
| fluvoxamine maleate [no description available] | 2.08 | 1 | 0 | (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. | 2.08 | 1 | 0 | ||
| 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. | 3.57 | 2 | 0 | 1,8-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. | 3.61 | 2 | 0 | benzimidazoles; sulfoxide | |
| gemifloxacin mesylate gemifloxacin mesylate : The mesylate salt of gemifloxacin. | 2.08 | 1 | 0 | methanesulfonate salt | antimicrobial agent; topoisomerase IV inhibitor |
| fosinopril [no description available] | 3.23 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | 2-[(diphenylmethyl)sulfinyl]acetamide | central nervous system stimulant; eugeroic |
| norfenfluramine Dexnorfenfluramine: D-isomer of Norfenfluramine | 2.03 | 1 | 0 | amphetamines | |
| abiraterone acetate Abiraterone Acetate: An androstene derivative that inhibits STEROID 17-ALPHA-HYDROXYLASE and is used as an ANTINEOPLASTIC AGENT in the treatment of metastatic castration-resistant PROSTATE CANCER.. abiraterone acetate : A sterol ester obtained by formal condensation of the 3-hydroxy group of abiraterone with the carboxy group of acetic acid. A prodrug that is converted in vivo into abiraterone. Used for treatment of metastatic castrate-resistant prostate cancer. | 4.02 | 2 | 1 | pyridines; sterol ester | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug |
| 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. | 3.23 | 1 | 0 | oligopeptide | |
| 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. | 3.23 | 1 | 0 | alkylbenzene | |
| 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. | 3.23 | 1 | 0 | organic molecular entity | |
| 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. | 7.52 | 2 | 0 | 1,3-thiazoles; aromatic amide; ethanolamines; monocarboxylic acid amide | beta-adrenergic agonist |
| 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. | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| 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. | 2.08 | 1 | 0 | aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes | anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor |
| mk 386 4,7beta-dimethyl-4-azacholestan-3-one: structure given in first source | 2.04 | 1 | 0 | ||
| dpc 423 [no description available] | 3.27 | 1 | 0 | ||
| hki 272 [no description available] | 2.08 | 1 | 0 | nitrile; 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. | 2.08 | 1 | 0 | N-acylpiperidine; nitrile; pyrrolopyrimidine; tertiary amino compound | antirheumatic drug; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor |
| samarium sphingomyelin 16:0 : A sphingomyelin in which the total number of carbons contained in the sphingoid base and fatty acyl groups is 16 with zero double bonds.. sphingomyelin d18:1/16:0 : A sphingomyelin d18:1 in which the fatty acyl group contains 16 carbons and is fully saturated.. N-hexadecanoylsphingosine-1-phosphocholine : A sphingomyelin 34:1 in which the N-acyl group and sphingoid base are specified as hexadecanoyl and sphingosine respectively. | 3.27 | 1 | 0 | sphingomyelin d18:1/16:0 | mouse metabolite |
| 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. | 3.61 | 2 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| 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. | 3.23 | 1 | 0 | ||
| amg 009 AMG 009: an anti-inflammatory agent; structure in first source | 2.08 | 1 | 0 | ||
| cefotaxime sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| baci-im [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| acebutolol alpha-D-glucosyl-(1->4)-alpha-D-mannose : An alpha-D-glucosyl-(1->4)-D-mannopyranose in which the anomeric hydroxy group has alpha configuration. | 2.11 | 1 | 0 | alpha-D-glucosyl-(1->4)-D-mannopyranose | |
| regorafenib [no description available] | 2.11 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; monofluorobenzenes; phenylureas; pyridinecarboxamide | antineoplastic agent; hepatotoxic agent; tyrosine kinase inhibitor |
| bms 477118 [no description available] | 3.23 | 1 | 0 | adamantanes; 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. | 3.23 | 1 | 0 | nystatins | |
| ch 4987655 [no description available] | 3.27 | 1 | 0 | ||
| milnacipran [no description available] | 3.57 | 2 | 0 | acetamides | |
| 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. | 2.08 | 1 | 0 | ||
| pristinamycin iib virginiamycin M2: structure in first source | 3.27 | 1 | 0 | ||
| scopolamine hydrobromide [no description available] | 3.23 | 1 | 0 | ||
| 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. | 2.08 | 1 | 0 | imidazoquinoline; nitrile; quinolines; ring assembly; ureas | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor |
| rabeprazole sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| mdv 3100 [no description available] | 2.11 | 1 | 0 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent |
| 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. | 3.61 | 2 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| somatostatin [no description available] | 2.08 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | |
| 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. | 3.23 | 1 | 0 | ||
| ganirelix [no description available] | 3.23 | 1 | 0 | polypeptide | |
| teriparatide [no description available] | 3.23 | 1 | 0 | polypeptide | |
| salmon calcitonin [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone; polypeptide | bone density conservation agent; metabolite |
| ly-146032 [no description available] | 3.61 | 2 | 0 | heterodetic 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 | 3.23 | 1 | 0 | polypeptide | |
| acyline [no description available] | 3.51 | 1 | 1 | ||
| exenatide [no description available] | 3.23 | 1 | 0 | ||
| 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. | 2.08 | 1 | 0 | ||
| cellulose DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications. | 2.49 | 2 | 0 | glycoside | |
| phosphatidylcholines Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety. | 2.06 | 1 | 0 | 1,2-diacyl-sn-glycero-3-phosphocholine | |
| 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. | 2.08 | 1 | 0 | organic sodium salt; statin (semi-synthetic) | anticholesteremic drug |
| alendronate sodium [no description available] | 2.08 | 1 | 0 | ||
| sl 80.0750 [no description available] | 2.08 | 1 | 0 | ||
| chitosan [no description available] | 7.25 | 1 | 0 | ||
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 3.61 | 2 | 0 | organosulfonic acid | |
| 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. | 2.08 | 1 | 0 | potassium salt | antibacterial 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. | 3.23 | 1 | 0 | lactate salt; organic sodium salt | food acidity regulator; food preservative |
| piperacillin sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| sodium iothalamate [no description available] | 3.23 | 1 | 0 | ||
| oxacillin sodium [no description available] | 2.08 | 1 | 0 | organic 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. | 2.08 | 1 | 0 | organic sodium salt | |
| azlocillin sodium [no description available] | 2.08 | 1 | 0 | organic sodium salt | |
| ethyl cellulose [no description available] | 2.1 | 1 | 0 | glycoside | |
| 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. | 3.23 | 1 | 0 | oligopeptide | antineoplastic agent; GnRH antagonist |
| tolterodine tartrate Tolterodine Tartrate: An ANTIMUSCARINIC AGENT selective for the MUSCARINIC RECEPTORS of the BLADDER that is used in the treatment of URINARY INCONTINENCE and URINARY URGE INCONTINENCE. | 2.97 | 1 | 0 | tartrate salt | |
| methylcellulose Methylcellulose: Methylester of cellulose. Methylcellulose is used as an emulsifying and suspending agent in cosmetics, pharmaceutics and the chemical industry. It is used therapeutically as a bulk laxative. | 2.07 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| raltegravir [no description available] | 3.23 | 1 | 0 | 1,2,4-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. | 3.86 | 3 | 0 | ||
| chlortetracycline Chlortetracycline: A TETRACYCLINE with a 7-chloro substitution.. chlortetracycline : A member of the class of tetracyclines with formula C22H23ClN2O8 isolated from Streptomyces aureofaciens. | 2.03 | 1 | 0 | ||
| 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. | 3.57 | 2 | 0 | ||
| 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. | 3.86 | 3 | 0 | ||
| methacycline Methacycline: A broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period.. methacycline : A tetracycline that is the 6-methylene analogue of oxytetracycline, obtained by formal dehydration at position 6. | 2.03 | 1 | 0 | ||
| piroxicam [no description available] | 3.86 | 3 | 0 | benzothiazine; 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 | 2.08 | 1 | 0 | aromatic amide | |
| 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. | 3.61 | 2 | 0 | 1,3-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. | 2.08 | 1 | 0 | heteroaryl 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. | 2.08 | 1 | 0 | benzothiazine; 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. | 3.23 | 1 | 0 | benzenes; 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. | 3.23 | 1 | 0 | ||
| 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. | 3.23 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| minocycline hydrochloride [no description available] | 2.08 | 1 | 0 | ||
| tigecycline [no description available] | 3.61 | 2 | 0 | ||
| (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). | 2.03 | 1 | 0 | 4-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. | 2.08 | 1 | 0 | heteroaryl hydroxy compound; monocarboxylic acid amide; organochlorine compound; pyridines; thienothiazine | antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fertinex [no description available] | 3.23 | 1 | 0 | ||
| psma-617 PSMA-617: inhibits prostate-specific membrane antigen; structure in first source | 2.21 | 1 | 0 | ||
| silybin Silybin: The major active component of silymarin flavonoids extracted from seeds of the MILK THISTLE, Silybum marianum; it is used in the treatment of HEPATITIS; LIVER CIRRHOSIS; and CHEMICAL AND DRUG INDUCED LIVER INJURY, and has antineoplastic activity; silybins A and B are diastereomers. | 3.18 | 1 | 0 | ||
| technetium tc 99m medronate Technetium Tc 99m Medronate: A gamma-emitting radionuclide imaging agent used primarily in skeletal scintigraphy. Because of its absorption by a variety of tumors, it is useful for the detection of neoplasms. | 5.83 | 2 | 2 | ||
| 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. | 3.61 | 2 | 0 | 2-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. | 3.61 | 2 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| 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. | 3.23 | 1 | 0 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| 3-methyladenine N3-methyladenine: structure in first source | 2.31 | 1 | 0 | ||
| 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) | 3.86 | 3 | 0 | cyclic 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. | 3.86 | 3 | 0 | benzodiazepine; 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. | 3.61 | 2 | 0 | dacarbazine | |
| 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. | 3.61 | 2 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 3.61 | 2 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valtrex [no description available] | 2.08 | 1 | 0 | organic 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. | 3.23 | 1 | 0 | L-valyl ester | antiviral 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. | 3.57 | 2 | 0 | piperazines; 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. | 3.61 | 2 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| raltitrexed [no description available] | 2.08 | 1 | 0 | N-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. | 3.57 | 2 | 0 | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| 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. | 3.61 | 2 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 3.61 | 2 | 0 | tetrahydrofolic acid | |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 3.23 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 3.61 | 2 | 0 | N-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. | 3.23 | 1 | 0 | imidazoquinazoline | anticoagulant; 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 | 3.23 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| 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). | 3.23 | 1 | 0 | N-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. | 2.54 | 2 | 0 | citrate salt | EC 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. | 3.23 | 1 | 0 | L-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. | 3.86 | 3 | 0 | (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. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; phosphoramide; triazoles | antiemetic; neurokinin-1 receptor antagonist; prodrug |
| tegaserod maleate [no description available] | 2.08 | 1 | 0 | maleate salt | serotonergic agonist |
| rifabutin [no description available] | 3.61 | 2 | 0 | ||
| levomefolate calcium levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid. | 3.23 | 1 | 0 | organic calcium salt | antidepressant |
| ferric carboxymaltose ferric carboxymaltose: effective for treatment of postpartum anemia | 2.11 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 3.7 | 3 | 0 |
| Adverse Drug Event [description not available] | 0 | 5.67 | 6 | 1 |
| 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. | 0 | 3.7 | 3 | 0 |
| 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. | 0 | 5.67 | 6 | 1 |
| Ache [description not available] | 0 | 2.87 | 3 | 0 |
| Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. | 0 | 7.87 | 3 | 0 |
| Disease Exacerbation [description not available] | 0 | 14.89 | 45 | 21 |
| Asymptomatic Conditions [description not available] | 0 | 6.07 | 3 | 3 |
| Lower Urinary Tract Symptom [description not available] | 0 | 12.17 | 55 | 19 |
| Adenoma, Prostatic [description not available] | 0 | 21.76 | 341 | 110 |
| Cancer of Prostate [description not available] | 0 | 20.21 | 222 | 70 |
| 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. | 1 | 23.76 | 341 | 110 |
| Prostatic Neoplasms Tumors or cancer of the PROSTATE. | 1 | 24.96 | 444 | 140 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 4.96 | 13 | 0 |
| Idiopathic Parkinson Disease [description not available] | 0 | 4.02 | 3 | 0 |
| 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) | 0 | 4.02 | 3 | 0 |
| Alopecia Cicatrisata [description not available] | 0 | 14.73 | 72 | 7 |
| Alopecia Absence of hair from areas where it is normally present. | 1 | 19.4 | 144 | 14 |
| Impotence [description not available] | 0 | 13.99 | 38 | 11 |
| Erectile Dysfunction The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction. | 0 | 13.99 | 38 | 11 |
| 2019 Novel Coronavirus Disease [description not available] | 0 | 2.76 | 2 | 0 |
| Urinary Retention Inability to empty the URINARY BLADDER with voiding (URINATION). | 0 | 12.66 | 33 | 13 |
| Bladder, Overactive [description not available] | 0 | 8.14 | 12 | 5 |
| 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. | 0 | 8.14 | 12 | 5 |
| Bladder Cancer [description not available] | 0 | 8.21 | 4 | 0 |
| Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER. | 0 | 3.21 | 4 | 0 |
| Androgen-Independent Prostatic Cancer [description not available] | 0 | 10.32 | 17 | 11 |
| Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE. | 1 | 12.32 | 17 | 11 |
| Acute Confusional Senile Dementia [description not available] | 0 | 2.41 | 1 | 0 |
| Acute Onset Vascular Dementia [description not available] | 0 | 2.41 | 1 | 0 |
| 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) | 0 | 2.41 | 1 | 0 |
| Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders. | 0 | 5.15 | 6 | 0 |
| 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) | 0 | 2.41 | 1 | 0 |
| Degenerative Diseases, Central Nervous System [description not available] | 0 | 3.33 | 1 | 0 |
| Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures. | 0 | 3.33 | 1 | 0 |
| 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. | 0 | 7.6 | 1 | 0 |
| Dyskinesia, Medication-Induced [description not available] | 0 | 2.6 | 1 | 0 |
| Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199) | 0 | 2.6 | 1 | 0 |
| Suicidal Ideation A risk factor for suicide attempts and completions, it is the most common of all suicidal behavior, but only a minority of ideators engage in overt self-harm. | 0 | 2.66 | 2 | 0 |
| Margins of Excision The edges of tissue removed in a surgery for assessment of the effectiveness of a surgical procedure in achieving the local control of a neoplasm and the adequacy of tumor removal. When the margin is negative or not involved by tumor (e.g., CANCER) it suggests all of the tumor has been removed by the surgery. | 0 | 2.21 | 1 | 0 |
| Invasiveness, Neoplasm [description not available] | 0 | 5.17 | 3 | 1 |
| Carcinoma, Transitional Cell A malignant neoplasm derived from TRANSITIONAL EPITHELIAL CELLS, occurring chiefly in the URINARY BLADDER; URETERS; or RENAL PELVIS. | 0 | 2.63 | 2 | 0 |
| Genetic Predisposition [description not available] | 0 | 7.48 | 7 | 1 |
| 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) | 0 | 4.7 | 6 | 1 |
| Complication, Postoperative [description not available] | 0 | 5.29 | 6 | 2 |
| Urination Disorders Abnormalities in the process of URINE voiding, including bladder control, frequency of URINATION, as well as the volume and composition of URINE. | 0 | 12.3 | 18 | 11 |
| 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. | 0 | 10.29 | 6 | 2 |
| Astrocytoma, Grade IV [description not available] | 0 | 2.66 | 2 | 0 |
| 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. | 0 | 2.66 | 2 | 0 |
| 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. | 0 | 5.84 | 4 | 1 |
| 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. | 0 | 5.84 | 4 | 1 |
| Blood Loss, Surgical Loss of blood during a surgical procedure. | 0 | 9.26 | 16 | 9 |
| Actinic Reticuloid Syndrome [description not available] | 0 | 2.25 | 1 | 0 |
| Cirrhosis [description not available] | 0 | 4.44 | 7 | 0 |
| Innate Inflammatory Response [description not available] | 0 | 6.25 | 4 | 1 |
| Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury. | 0 | 4.44 | 7 | 0 |
| 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. | 0 | 6.25 | 4 | 1 |
| Sex Disorders [description not available] | 0 | 10.74 | 19 | 4 |
| Sexual Dysfunction, Physiological Physiological disturbances in normal sexual performance in either the male or the female. | 0 | 10.74 | 19 | 4 |
| Allergic Contact Dermatitis [description not available] | 0 | 2.25 | 1 | 0 |
| Angioneurotic Edema [description not available] | 0 | 2.52 | 2 | 0 |
| Angioedema Swelling involving the deep DERMIS, subcutaneous, or submucosal tissues, representing localized EDEMA. Angioedema often occurs in the face, lips, tongue, and larynx. | 0 | 2.52 | 2 | 0 |
| Dermatitis, Allergic Contact A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure. | 0 | 2.25 | 1 | 0 |
| Cranial Sinus Thrombosis [description not available] | 0 | 2.25 | 1 | 0 |
| Carcinoma, Anaplastic [description not available] | 0 | 4.22 | 3 | 1 |
| Local Neoplasm Recurrence [description not available] | 0 | 6.41 | 5 | 3 |
| 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. | 0 | 4.22 | 3 | 1 |
| Atrophy, Muscular, Spinobulbar [description not available] | 0 | 6.01 | 3 | 1 |
| Bulbo-Spinal Atrophy, X-Linked An X-linked recessive form of spinal muscular atrophy. It is due to a mutation of the gene encoding the ANDROGEN RECEPTOR. | 1 | 8.01 | 3 | 1 |
| Acute Bacterial Prostatitis [description not available] | 0 | 7.75 | 8 | 5 |
| 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. | 1 | 14.75 | 8 | 5 |
| Dermatitis Medicamentosa [description not available] | 0 | 2.25 | 1 | 0 |
| Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes. | 0 | 2.25 | 1 | 0 |
| Benign Neoplasms, Brain [description not available] | 0 | 2.25 | 1 | 0 |
| 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. | 0 | 2.25 | 1 | 0 |
| Acute Disease Disease having a short and relatively severe course. | 0 | 6.43 | 11 | 4 |
| Nycturia [description not available] | 0 | 5.13 | 3 | 3 |
| Nocturia Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS). | 0 | 5.13 | 3 | 3 |
| Kahler Disease [description not available] | 0 | 2.31 | 1 | 0 |
| 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. | 0 | 2.31 | 1 | 0 |
| Lichen Ruber Planus [description not available] | 0 | 2.55 | 2 | 0 |
| Lichen Planus An inflammatory, pruritic disease of the skin and mucous membranes, which can be either generalized or localized. It is characterized by distinctive purplish, flat-topped papules having a predilection for the trunk and flexor surfaces. The lesions may be discrete or coalesce to form plaques. Histologically, there is a saw-tooth pattern of epidermal hyperplasia and vacuolar alteration of the basal layer of the epidermis along with an intense upper dermal inflammatory infiltrate composed predominantly of T-cells. Etiology is unknown. | 0 | 2.55 | 2 | 0 |
| Depression, Endogenous [description not available] | 0 | 2.15 | 1 | 0 |
| Depressive Disorder An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent. | 0 | 2.15 | 1 | 0 |
| Adenocarcinoma Of Kidney [description not available] | 0 | 3.56 | 1 | 1 |
| Cancer of Kidney [description not available] | 0 | 3.56 | 1 | 1 |
| Cancer of Lung [description not available] | 0 | 3.56 | 1 | 1 |
| Cancer of Ovary [description not available] | 0 | 3.56 | 1 | 1 |
| Colorectal Cancer [description not available] | 0 | 3.56 | 1 | 1 |
| Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma. | 0 | 3.56 | 1 | 1 |
| Kidney Neoplasms Tumors or cancers of the KIDNEY. | 0 | 3.56 | 1 | 1 |
| Lung Neoplasms Tumors or cancer of the LUNG. | 0 | 3.56 | 1 | 1 |
| Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS. | 0 | 3.56 | 1 | 1 |
| 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. | 0 | 3.56 | 1 | 1 |
| Intraepithelial Prostatic Neoplasia [description not available] | 0 | 6.39 | 5 | 3 |
| Prostatic Intraepithelial Neoplasia A premalignant change arising in the prostatic epithelium, regarded as the most important and most likely precursor of prostatic adenocarcinoma. The neoplasia takes the form of an intra-acinar or ductal proliferation of secretory cells with unequivocal nuclear anaplasia, which corresponds to nuclear grade 2 and 3 invasive prostate cancer. | 0 | 11.39 | 5 | 3 |
| Urinary Tract Infections Inflammatory responses of the epithelium of the URINARY TRACT to microbial invasions. They are often bacterial infections with associated BACTERIURIA and PYURIA. | 0 | 7.26 | 4 | 2 |
| Frigidity [description not available] | 0 | 7.27 | 4 | 2 |
| 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) | 0 | 7.27 | 4 | 2 |
| Bladder Neck Obstruction [description not available] | 0 | 5.9 | 8 | 1 |
| Hematuria Presence of blood in the urine. | 0 | 3.71 | 3 | 0 |
| Anterior Urethral Stricture [description not available] | 0 | 2.15 | 1 | 0 |
| Contracture Prolonged shortening of the muscle or other soft tissue around a joint, preventing movement of the joint. | 0 | 2.15 | 1 | 0 |
| Urethral Stricture Narrowing of any part of the URETHRA. It is characterized by decreased urinary stream and often other obstructive voiding symptoms. | 0 | 2.15 | 1 | 0 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 1 | 12.8 | 5 | 0 |
| MPTP Neurotoxicity Syndrome [description not available] | 0 | 2.53 | 2 | 0 |
| Amentia [description not available] | 0 | 2.17 | 1 | 0 |
| Dementia An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness. | 0 | 2.17 | 1 | 0 |
| Idiopathic Inflammatory Myopathies [description not available] | 0 | 2.17 | 1 | 0 |
| Myositis Inflammation of a muscle or muscle tissue. | 0 | 2.17 | 1 | 0 |
| Rhabdomyolysis Necrosis or disintegration of skeletal muscle often followed by myoglobinuria. | 0 | 2.17 | 1 | 0 |
| Acne Inversa [description not available] | 0 | 3.06 | 1 | 0 |
| Hidradenitis Suppurativa A chronic suppurative and cicatricial disease of the apocrine glands occurring chiefly in the axillae in women and in the groin and anal regions in men. It is characterized by poral occlusion with secondary bacterial infection, evolving into abscesses which eventually rupture. As the disease becomes chronic, ulcers appear, sinus tracts enlarge, fistulas develop, and fibrosis and scarring become evident. | 0 | 3.06 | 1 | 0 |
| Breast Cancer [description not available] | 0 | 5.76 | 4 | 1 |
| Breast Neoplasms Tumors or cancer of the human BREAST. | 0 | 5.76 | 4 | 1 |
| Adenocarcinoma, Basal Cell [description not available] | 0 | 6.93 | 5 | 2 |
| Lymph Node Metastasis [description not available] | 0 | 2.78 | 3 | 0 |
| Adenocarcinoma A malignant epithelial tumor with a glandular organization. | 0 | 6.93 | 5 | 2 |
| Age-Related Osteoporosis [description not available] | 0 | 2.55 | 2 | 0 |
| 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. | 0 | 7.55 | 2 | 0 |
| Osteoporotic Fractures Breaks in bones resulting from low bone mass and microarchitectural deterioration characteristic of OSTEOPOROSIS. | 0 | 2.17 | 1 | 0 |
| Hematospermia [description not available] | 0 | 2.17 | 1 | 0 |
| Sterility, Male [description not available] | 0 | 3.47 | 2 | 0 |
| 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. | 0 | 3.47 | 2 | 0 |
| Condition, Preneoplastic [description not available] | 0 | 2.48 | 2 | 0 |
| Precancerous Conditions Pathological conditions that tend eventually to become malignant. | 0 | 2.48 | 2 | 0 |
| Acne [description not available] | 0 | 3.4 | 2 | 0 |
| Congenital Adrenal Hyperplasia [description not available] | 0 | 3.12 | 1 | 0 |
| Hirsutism A condition observed in WOMEN and CHILDREN when there is excess coarse body hair of an adult male distribution pattern, such as facial and chest areas. It is the result of elevated ANDROGENS from the OVARIES, the ADRENAL GLANDS, or exogenous sources. The concept does not include HYPERTRICHOSIS, which is an androgen-independent excessive hair growth. | 0 | 3.12 | 1 | 0 |
| Polycystic Ovarian Syndrome [description not available] | 0 | 3.12 | 1 | 0 |
| Acne Vulgaris A chronic disorder of the pilosebaceous apparatus associated with an increase in sebum secretion. It is characterized by open comedones (blackheads), closed comedones (whiteheads), and pustular nodules. The cause is unknown, but heredity and age are predisposing factors. | 0 | 3.4 | 2 | 0 |
| Adrenal Hyperplasia, Congenital A group of inherited disorders of the ADRENAL GLANDS, caused by enzyme defects in the synthesis of cortisol (HYDROCORTISONE) and/or ALDOSTERONE leading to accumulation of precursors for ANDROGENS. Depending on the hormone imbalance, congenital adrenal hyperplasia can be classified as salt-wasting, hypertensive, virilizing, or feminizing. Defects in STEROID 21-HYDROXYLASE; STEROID 11-BETA-HYDROXYLASE; STEROID 17-ALPHA-HYDROXYLASE; 3-beta-hydroxysteroid dehydrogenase (3-HYDROXYSTEROID DEHYDROGENASES); TESTOSTERONE 5-ALPHA-REDUCTASE; or steroidogenic acute regulatory protein; among others, underlie these disorders. | 0 | 3.12 | 1 | 0 |
| Polycystic Ovary Syndrome A complex disorder characterized by infertility, HIRSUTISM; OBESITY; and various menstrual disturbances such as OLIGOMENORRHEA; AMENORRHEA; ANOVULATION. Polycystic ovary syndrome is usually associated with bilateral enlarged ovaries studded with atretic follicles, not with cysts. The term, polycystic ovary, is misleading. | 0 | 3.12 | 1 | 0 |
| Chronic Illness [description not available] | 0 | 5.63 | 3 | 2 |
| 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). | 0 | 5.63 | 3 | 2 |
| Dyslipidemia [description not available] | 0 | 4.88 | 2 | 1 |
| Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE. | 0 | 4.53 | 3 | 0 |
| 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. | 0 | 4.88 | 2 | 1 |
| Diabetes Mellitus, Adult-Onset [description not available] | 0 | 2.21 | 1 | 0 |
| 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. | 0 | 2.21 | 1 | 0 |
| Insulin Sensitivity [description not available] | 0 | 11.59 | 6 | 3 |
| 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. | 0 | 6.59 | 6 | 3 |
| Aggression Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism. | 0 | 3.47 | 1 | 1 |
| 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). | 0 | 12.25 | 4 | 2 |
| Breast Cancer, Male [description not available] | 0 | 2.49 | 2 | 0 |
| Breast Neoplasms, Male Any neoplasms of the male breast. These occur infrequently in males in developed countries, the incidence being about 1% of that in females. | 0 | 2.49 | 2 | 0 |
| Symptom Cluster [description not available] | 0 | 2.07 | 1 | 0 |
| Syndrome A characteristic symptom complex. | 0 | 2.07 | 1 | 0 |
| Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM. | 0 | 3.84 | 2 | 0 |
| Prostatic Diseases Pathological processes involving the PROSTATE or its component tissues. | 0 | 3 | 1 | 0 |
| Prostatism Lower urinary tract symptom, such as slow urinary stream, associated with PROSTATIC HYPERPLASIA in older men. | 0 | 10.21 | 13 | 10 |
| Hypergonadotropic Hypogonadism [description not available] | 0 | 6.38 | 5 | 3 |
| 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). | 1 | 13.38 | 5 | 3 |
| Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. | 0 | 4.37 | 4 | 1 |
| Alcohol Drinking Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking. | 0 | 5.09 | 3 | 3 |
| Alcohol Abuse [description not available] | 0 | 3.48 | 1 | 1 |
| Alcoholism A primary, chronic disease with genetic, psychosocial, and environmental factors influencing its development and manifestations. The disease is often progressive and fatal. It is characterized by impaired control over drinking, preoccupation with the drug alcohol, use of alcohol despite adverse consequences, and distortions in thinking, most notably denial. Each of these symptoms may be continuous or periodic. (Morse & Flavin for the Joint Commission of the National Council on Alcoholism and Drug Dependence and the American Society of Addiction Medicine to Study the Definition and Criteria for the Diagnosis of Alcoholism: in JAMA 1992;268:1012-4) | 0 | 3.48 | 1 | 1 |
| Bone Cancer [description not available] | 0 | 7.69 | 5 | 4 |
| Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES. | 0 | 7.69 | 5 | 4 |
| Metastase [description not available] | 0 | 4.83 | 2 | 1 |
| Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site. | 0 | 4.83 | 2 | 1 |
| ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available] | 0 | 2.11 | 1 | 0 |
| Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN. | 0 | 2.11 | 1 | 0 |
| 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. | 0 | 3.01 | 1 | 0 |
| 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. | 0 | 2.11 | 1 | 0 |
| Acute Coronary Syndrome An episode of MYOCARDIAL ISCHEMIA that generally lasts longer than a transient anginal episode that ultimately may lead to MYOCARDIAL INFARCTION. | 0 | 2.11 | 1 | 0 |
| Urinary Tract Diseases [description not available] | 0 | 2.11 | 1 | 0 |
| 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. | 0 | 6.42 | 3 | 3 |
| Bladder Calculi [description not available] | 0 | 2.11 | 1 | 0 |
| Premenstrual Dysphoric Disorder A condition in which a woman suffers from severe depression, irritability, and tension before MENSTRUATION. Premenstrual dysphoric disorder (PMDD) may involve a wide range of physical or emotional symptoms, which are more severe and debilitating than those seen with premenstrual syndrome (PMS), and which include at least one mood-related symptom. Symptoms usually stop when, or shortly after, menstruation begins. | 0 | 3.51 | 1 | 1 |
| Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment. | 0 | 3.03 | 1 | 0 |
| Psychoses, Drug [description not available] | 0 | 3.03 | 1 | 0 |
| 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. | 0 | 8.5 | 1 | 1 |
| Adverse Effects, Long Term [description not available] | 0 | 4.43 | 1 | 1 |
| Sycosis [description not available] | 0 | 2.15 | 1 | 0 |
| Folliculitis Inflammation of follicles, primarily hair follicles. | 0 | 2.15 | 1 | 0 |
| Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. | 0 | 2.54 | 2 | 0 |
| Abnormalities, Drug-Induced Congenital abnormalities caused by medicinal substances or drugs of abuse given to or taken by the mother, or to which she is inadvertently exposed during the manufacture of such substances. The concept excludes abnormalities resulting from exposure to non-medicinal chemicals in the environment. | 0 | 2.46 | 2 | 0 |
| 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) | 0 | 2.13 | 1 | 0 |
| Apoplexy [description not available] | 0 | 2.15 | 1 | 0 |
| Cardiac Failure [description not available] | 0 | 7.68 | 5 | 4 |
| Cardiovascular Stroke [description not available] | 0 | 2.15 | 1 | 0 |
| 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. | 0 | 7.68 | 5 | 4 |
| Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION). | 0 | 2.15 | 1 | 0 |
| 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) | 0 | 2.15 | 1 | 0 |
| Hyperidrosis [description not available] | 0 | 3.87 | 1 | 0 |
| Hyperhidrosis Excessive sweating. In the localized type, the most frequent sites are the palms, soles, axillae, inguinal folds, and the perineal area. Its chief cause is thought to be emotional. Generalized hyperhidrosis may be induced by a hot, humid environment, by fever, or by vigorous exercise. | 0 | 3.87 | 1 | 0 |
| Intertrochanteric Fractures [description not available] | 0 | 2.04 | 1 | 0 |
| Hip Fractures Fractures of the FEMUR HEAD; the FEMUR NECK; (FEMORAL NECK FRACTURES); the trochanters; or the inter- or subtrochanteric region. Excludes fractures of the acetabulum and fractures of the femoral shaft below the subtrochanteric region (FEMORAL FRACTURES). | 0 | 2.04 | 1 | 0 |
| Hormone-Dependent Neoplasms [description not available] | 0 | 7.44 | 7 | 1 |
| Bone Fractures [description not available] | 0 | 4.37 | 1 | 1 |
| Fractures, Bone Breaks in bones. | 0 | 4.37 | 1 | 1 |
| Benign Neoplasms [description not available] | 0 | 3.67 | 3 | 0 |
| 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. | 0 | 3.67 | 3 | 0 |
| Adolescent Gynecomastia [description not available] | 0 | 6.31 | 8 | 5 |
| Blood Pressure, High [description not available] | 0 | 3.45 | 1 | 1 |
| Gynecomastia Enlargement of the BREAST in the males, caused by an excess of ESTROGENS. Physiological gynecomastia is normally observed in NEWBORNS; ADOLESCENT; and AGING males. | 0 | 6.31 | 8 | 5 |
| 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. | 0 | 3.45 | 1 | 1 |
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 4.37 | 1 | 1 |
| Long Sleeper Syndrome [description not available] | 0 | 2.07 | 1 | 0 |
| Sleep Wake Disorders Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle. | 0 | 2.07 | 1 | 0 |
| 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. | 0 | 2.08 | 1 | 0 |
| Bone Loss, Perimenopausal [description not available] | 0 | 2.08 | 1 | 0 |
| Cicatrix The fibrous tissue that replaces normal tissue during the process of WOUND HEALING. | 0 | 2.08 | 1 | 0 |
| Osteoporosis, Postmenopausal Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency. | 0 | 2.08 | 1 | 0 |
| ENT Diseases [description not available] | 0 | 4.31 | 1 | 1 |
| Angiogenesis, Pathologic [description not available] | 0 | 4.32 | 1 | 1 |
| Molluscum Contagiosum A common, benign, usually self-limited viral infection of the skin and occasionally the conjunctivae by a poxvirus (MOLLUSCUM CONTAGIOSUM VIRUS). (Dorland, 27th ed) | 0 | 2.03 | 1 | 0 |
| Cholera Infantum [description not available] | 0 | 3.41 | 1 | 1 |
| Pelvic Pain Pain in the pelvic region of genital and non-genital origin. | 0 | 2.03 | 1 | 0 |
| Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill. | 0 | 2.03 | 1 | 0 |
| Hyperactivity, Motor [description not available] | 0 | 2.04 | 1 | 0 |
| Psychoses [description not available] | 0 | 2.04 | 1 | 0 |
| Psychotic Disorders Disorders in which there is a loss of ego boundaries or a gross impairment in reality testing with delusions or prominent hallucinations. (From DSM-IV, 1994) | 0 | 2.04 | 1 | 0 |
| Amyloid Deposits [description not available] | 0 | 2.04 | 1 | 0 |
| Brain Disorders [description not available] | 0 | 2.04 | 1 | 0 |
| Amyloidosis A group of sporadic, familial and/or inherited, degenerative, and infectious disease processes, linked by the common theme of abnormal protein folding and deposition of AMYLOID. As the amyloid deposits enlarge they displace normal tissue structures, causing disruption of function. Various signs and symptoms depend on the location and size of the deposits. | 0 | 2.04 | 1 | 0 |
| Brain Diseases Pathologic conditions affecting the BRAIN, which is composed of the intracranial components of the CENTRAL NERVOUS SYSTEM. This includes (but is not limited to) the CEREBRAL CORTEX; intracranial white matter; BASAL GANGLIA; THALAMUS; HYPOTHALAMUS; BRAIN STEM; and CEREBELLUM. | 0 | 2.04 | 1 | 0 |