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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
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. [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 | 657181 |
| CHEMBL ID | 1201199 |
| CHEBI ID | 6427 |
| SCHEMBL ID | 4585 |
| MeSH ID | M0025473 |
| Synonym |
|---|
| CHEMBL1201199 |
| leuporelin |
| (-)-leuprolide |
| tap-144 free base |
| ckd-841 |
| abbott-43818 free base |
| leuprorelin slow release |
| chebi:6427 , |
| gtpl1175 |
| fensolvi (leuprolide acetate injectable suspension) |
| (d-leu(sup 6),des-gly-nh2(sup 10),pro-ethylamide(sup 9))-lhrh |
| (d-leu(sup 6),des-gly-nh2(sup 10),pro-ethylamide(sup 9))-gnrh |
| leuprorelina [inn-spanish] |
| leuprorelinum [inn-latin] |
| nsc 377526 |
| hsdb 6518 |
| leuproreline [inn-french] |
| nsc-377526 |
| leuprolide |
| leuprorelin , |
| leuprolide acetate salt, >=98% (hplc) |
| DB00007 |
| bdbm50369395 |
| leuprorelina |
| leuproreline |
| unii-efy6w0m8tg |
| efy6w0m8tg , |
| leuprorelinum |
| leuprorelin [inn:ban] |
| ccris 8462 |
| leuprolide acetate salt |
| pglu-his-trp-ser-tyr-d-leu-leu-arg-pro-nhc2h5 |
| 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-leucyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
| l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-leucyl-l-leucyl-l-arginyl-l-proline ethylamide |
| pglu-his-trp-ser-tyr-d-leu-leu-arg-pro-nhet |
| leuprolide [hsdb] |
| 5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tryosyl-d-leucyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide |
| leuprorelin [ep monograph] |
| leuprorelin [inn] |
| leuprolide [mi] |
| leuprorelin [mart.] |
| leuprolide [vandf] |
| leuprorelin [who-dd] |
| AKOS015892744 |
| GFIJNRVAKGFPGQ-LIJARHBVSA-N |
| SCHEMBL4585 |
| HS-2016 |
| CS-4947 |
| HY-12553 |
| mfcd00167544 |
| AKOS030213246 |
| leuprolide acetate, united states pharmacopeia (usp) reference standard |
| leuprolide acetate (usan) |
| leuprorelin acetate (jan) |
| NCGC00485984-01 |
| (s)-n-ethyl-1-(((s)-5-oxopyrrolidine-2-carbonyl)-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-leucyl-l-leucyl-l-arginyl)pyrrolidine-2-carboxamide |
| DTXSID50872411 , |
| Q907160 |
| bisphenola-(3-chloro-2-hydroxypropyl)-& |
| CCG-270656 |
| C75519 |
| AKOS037515838 |
| EN300-7481165 |
| (2s)-1-[(2s)-5-carbamimidamido-2-[(2s)-2-[(2r)-2-[(2s)-2-[(2s)-3-hydroxy-2-[(2s)-2-[(2s)-3-(1h-imidazol-4-yl)-2-{[(2s)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1h-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]-4-methylpentanamid |
| 6-d-leucine-9-(n-ethyl-l-prolinamide)-1-9-luteinizing hormone-releasing factor (pig) |
| leuproreline (inn-french) |
| leuprorelin (mart.) |
| l02ae02 |
| leuprorelina (inn-spanish) |
| dtxcid00820063 |
| leuprorelinum (inn-latin) |
| leuprorelin (ep monograph) |
| 6-d-leucine-9-(n-ethyl-l-prolinamide)-10-deglycinamide luteinizing hormone-releasing factor (pig) |
Leuprolide is a synthetic nonapeptide drug (pyroGlu-His-Trp-Ser-Tyr-d-Leu- Leu-Arg-Pro-NHEt) that acts as a gonadotropin-releasing hormone agonist. It inhibits gonadotropic hormone secretion by down-regulating pituitary GnRH receptor when administered continuously at therapeutic doses.
Leuprolide acetate has been used to decrease uterine size and shrink leiomyomata. It is currently also being evaluated in phase II clinical trials for the treatment of Alzheimer's disease.
Leuprolide acetate-treated endometriotic tissue showed downregulated genes associated with the biological functions of steroid hormone regulation, cell proliferation, inflammation, and intracellular signaling. Leuprolides did not improve glucose intolerance, insulin level, insulin sensitivity indices, sex hormone levels, lipid profile, and estrus cycle.
The case highlights the potential side effect of lipodystrophy secondary to leuprolide acetate injections. The study was terminated prematurely because of the smaller than planned number of participants and events. No difference in major adverse cardiovascular events at 1 year between patients assigned to degarelix or le uprolide was observed.
Leuprolide is a gonadotropin-releasing hormone (GnRH) agonist widely used in androgen deprivation therapy for the treatment of advanced prostate cancer. The results of a pharmacokinetic study in male Sprague-Dawley rats showed improved transport of le uprolide from thiolated NPs.
Bioavailability of leuprolide acetate in healthy human male volunteers ranged from 4% to 18% and agreed well with particle size data. Relative oral bioavailability could be increased by nanoparticulate tablets up to 4.5 mg.
| Excerpt | Reference | Relevance |
|---|---|---|
| " bioavailability in rats was significantly increased by alpha-cyclodextrin (CD), EDTA, and solution volume." | ( Bioavailability of leuprolide acetate following nasal and inhalation delivery to rats and healthy humans. Adjei, A; Chun, A; Miller, J; Sundberg, D, 1992) | 0.61 |
| " Absolute bioavailability of leuprolide acetate in healthy human male volunteers ranged from 4% to 18% and agreed well with particle size data." | ( Pulmonary delivery of peptide drugs: effect of particle size on bioavailability of leuprolide acetate in healthy male volunteers. Adjei, A; Garren, J, 1990) | 0.8 |
| " The absolute bioavailability after vaginal administration of the 5% citric acid solution was 16." | ( Vaginal absorption of a potent luteinizing hormone-releasing hormone analogue (leuprolide) in rats II: mechanism of absorption enhancement with organic acids. Mima, H; Okada, H; Yamazaki, I; Yashiki, T, 1983) | 0.49 |
| " After vaginal administration, the fraction of the dose that reached the systemic circulation, the F value, was very high but the rate of absorption was very low; consequently there was a low peak level and persistence of serum level." | ( Serum concentration patterns of an LHRH agonist, gonadotrophins and sex steroids after subcutaneous, vaginal, rectal and nasal administration of the agonist to pregnant rats. Yamazaki, I, 1984) | 0.27 |
| " The vaginal absorption was enhanced by organic acids: citric, succinic, tartaric, and glycocholic; the absolute bioavailability increased to approximately 20%." | ( Vaginal absorption of a potent luteinizing hormone-releasing hormone analog (leuprolide) in rats I: absorption by various routes and absorption enhancement. Hirai, S; Mima, H; Ogawa, Y; Okada, H; Yamazaki, I; Yashiki, T, 1982) | 0.49 |
| "To determine the difference in FSH bioavailability from IM and SC injection sites." | ( Differences in serum follicle-stimulating hormone uptake after intramuscular and subcutaneous human menopausal gonadotropin injection. Dobbs, KE; Dumesic, DA; Dumesic, JA; Shapiro, SS, 1994) | 0.29 |
| " Computed absorption rate constants for FSH after IM and SC injection differed significantly." | ( Differences in serum follicle-stimulating hormone uptake after intramuscular and subcutaneous human menopausal gonadotropin injection. Dobbs, KE; Dumesic, DA; Dumesic, JA; Shapiro, SS, 1994) | 0.29 |
| " Absolute bioavailability of the drug in typical emulsion systems ranged from approximately 3 to 10% and represent an improvement of about 100 fold in gastrointestinal bioavailability of this peptide." | ( Effect of formulation adjuvants on gastrointestinal absorption of leuprolide acetate. Adjei, A; Bush, E; Diaz, G; Greer, J; Haviv, F; Johnson, E; Love, S, 1993) | 0.52 |
| " One key facet of this study was to attempt to understand the distribution and ultimate bioavailability of the peptide dispersed in an inert polymer matrix." | ( XPS and TOF-SIMS microanalysis of a peptide/polymer drug delivery device. Annapragada, A; Fu Lu, MY; John, CM; Odom, RW; Salvati, L, 1995) | 0.29 |
| " It was found that the extent and rate of absorption were similar between humans and monkeys following sublingual dosing of leuprolide formulations." | ( Sublingual absorption of leuprolide: comparison between human and animal models. Johnson, HW; Lu, MY; Qiu, Y; Reiland, TL, 1999) | 0.81 |
| " Additional in vivo studies using conscious rats showed that the bioavailability of leuprolide was less than 1% for both ileal and colonic administration." | ( Permeability and absorption of leuprolide from various intestinal regions in rabbits and rats. Hoffman, D; Lu, MF; Qiu, Y; Reiland, TL; Zheng, Y, 1999) | 0.81 |
| "In order to develop nasal powder preparations with higher bioavailability for peptide delivery, the effect of a combination of hydroxypropyl cellulose (HPC) and microcrystalline cellulose (MCC) used as base materials and microenvironment for the drugs in the preparations was examined." | ( Mucosal drug delivery using cellulose derivatives as a functional polymer. Makino, Y; Suzuki, Y, 1999) | 0.3 |
| " In tracheostomized dogs, both formulations showed comparable pharmacokinetic parameters including Cmax, Tmax, AUC0-12 and bioavailability (F%), indicating that the taste-masking excipients do not have an effect on lung absorption of leuprolide acetate." | ( Pulmonary peptide delivery: effect of taste-masking excipients on leuprolide suspension metered-dose inhalers. Adjei, AL; Barber, TE; Fulu, MY; Lee, DY; Zheng, JY, 2001) | 0.73 |
| "5 mg, a new depot formulation of leuprolide acetate that uses the Atrigel drug delivery system, causing an increase in bioavailability and optimising testosterone suppression - two key features of depot hormone suppression." | ( A subcutaneous delivery system for the extended release of leuprolide acetate for the treatment of prostate cancer. Perez-Marrero, R; Tyler, RC, 2004) | 0.85 |
| "The purpose of this study was to investigate the transport mechanisms and causes of low bioavailability of leuprolide." | ( Transport of leuprolide across rat intestine, rabbit intestine and Caco-2 cell monolayer. Dong, J; Feng, L; Guo, J; Jiang, G; Li, C; Li, Z; Ping, Q; Qi, S, 2004) | 0.91 |
| " Relative percentage of bioavailability (F) for nasal treatments was calculated from plasma concentration vs time plots." | ( Preliminary investigation of the nasal delivery of liposomal leuprorelin acetate for contraception in rats. Misra, A; Shahiwala, A, 2006) | 0.33 |
| " Starting with the thienopyridin-4-one derivative 26d (T-98475) an optimization study was performed, which resulted in the identification of a highly potent and orally bioavailable LHRH receptor antagonist, 3-(N-benzyl-N-methylaminomethyl)-7-(2,6-difluorobenzyl)-4,7-dihydro-2-[4-(1-hydroxy-1-cyclopropanecarboxamido)phenyl]-5-isobutyryl-4-oxothieno[2,3-b]pyridine (33c)." | ( Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. Cho, N; Endo, S; Furuya, S; Harada, M; Hayase, Y; Imada, T; Imaeda, T; Kasai, S; Matsumoto, H; Sasaki, S; Suzuki, N, 2006) | 0.33 |
| "The objective of this review is to critically discuss the formulations currently available on the market for leuprolide optimization and to consider how drug delivery plays an important role in improving the bioavailability of this compound." | ( Leuprolide acetate: pharmaceutical use and delivery potentials. Montanari, S; Ponchel, G; Teutonico, D, 2012) | 2.03 |
| "The purpose of this study was to develop thiolated nanoparticles to enhance the bioavailability for the nasal application of leuprolide." | ( Thiolated chitosan nanoparticles for the nasal administration of leuprolide: bioavailability and pharmacokinetic characterization. Augustijns, P; Barthelmes, J; Bernkop-Schnürch, A; Dünnhaput, S; Iqbal, J; Laffleur, F; Perera, G; Rahmat, D; Schlocker, W; Shahnaz, G; Vetter, A, 2012) | 0.82 |
| "2-fold improved oral bioavailability of leuprolide oleate SMEDDS compared to a leuprolide acetate control solution." | ( In vivo evaluation of an oral self-microemulsifying drug delivery system (SMEDDS) for leuprorelin. Bernkop-Schnürch, A; Hauptstein, S; Hintzen, F; Laffleur, F; Müller, C; Perera, G, 2014) | 0.67 |
| " Bioavailability of leuprolide following pulmonary administration was 75% higher compared to subcutaneously administered leuprolide." | ( Effect of protease inhibitors on pulmonary bioavailability of therapeutic proteins and peptides in the rat. Amancha, KP; Hussain, A, 2015) | 0.74 |
| " The bioavailability of leuprolide from PLGA-TG18 hybrid MPs was approximately four times higher than that from TG18 MP and PLGA MP alone using the same dose of leuprolide (6 mg/kg)." | ( In vivo evaluation of solid lipid microparticles and hybrid polymer-lipid microparticles for sustained delivery of leuprolide. Baldursdottir, SG; Luo, X; Mu, H; Sun, X; Wu, C; Yang, M, 2019) | 1.03 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| " This study suggests that mucoadhesive buccal tablets containing self-assembled LON may effectively increase the medication adherence for pediatric and geriatric patients by improving the bioavailability and permeation rate of LEU." | ( Mucoadhesive buccal tablet of leuprolide and its fatty acid conjugate: Design, in vitro evaluation and formulation strategies. Jin, H; Lee, BJ; Ngo, HV; Park, C, 2023) | 1.2 |
One hundred premenopausal women with uterine leiomyomas were treated with leuprolide acetate depot at a dosage of 3. It was found that the extent and rate of absorption were similar between humans and monkeys following sublingual dosing.
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| gonadotropin releasing hormone agonist | Any drug which binds to gonadotropin-releasing hormone receptors and triggers a response. |
| anti-estrogen | A drug which acts to reduce estrogenic activity in the body, either by reducing the amount of estrogen or by reducing the activity of whatever estrogen is present. |
| [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 |
|---|---|
| oligopeptide | A peptide containing a relatively small number of amino acids. |
| [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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | Homo sapiens (human) | IC50 (µMol) | 0.0005 | 0.0001 | 0.1289 | 5.2000 | AID102819; AID267082; AID267085 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0006 | 0.0003 | 0.1542 | 2.0000 | AID102815; AID102947; AID267084 |
| Gonadotropin-releasing hormone receptor | Rattus norvegicus (Norway rat) | Ki | 5,370,319,732,736,000.0000 | 0.0038 | 3.5186 | 6.5000 | AID102938 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| gonadotropin secretion | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| cellular response to gonadotropin-releasing hormone | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| G protein-coupled receptor signaling pathway | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| cellular response to hormone stimulus | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| peptide binding | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| gonadotropin-releasing hormone receptor activity | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| plasma membrane | Gonadotropin-releasing hormone receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693376 | Metabolic stability in mouse renal epithelial cell membranes assessed as compound remaining at 10 nM measured at 30 mins | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID1145199 | Induction of FSH release in ovariectomized estrogen/progesterone-treated rat at 100 ng, sc measured after 15 mins to 60 hrs post dose by RIA relative to LH-RH | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6. |
| AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693380 | Tmax in overnight fasted C57BL/6N mouse at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID693381 | Half life in overnight fasted C57BL/6N mouse at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID267087 | Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID267086 | Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
| AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID693378 | Metabolic stability in overnight fasted C57BL/6N mouse plasma at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID693379 | Cmax in overnight fasted C57BL/6N mouse at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693391 | Agonist activity at LHRH1 receptor in C57BL/6N mouse assessed as release of testosterone in plasma at 1 ug/kg, ip in presence of cetrorelix | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID693387 | Agonist activity at LHRH1 receptor in C57BL/6N mouse assessed as testosterone AUC (1 to 6 hrs) at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693390 | Agonist activity at LHRH1 receptor in C57BL/6N mouse assessed as release of testosterone in plasma at 1 ug/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID102947 | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. |
| AID16102 | Clearance in rat after iv dose (100 ug/kg) | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
| AID693383 | Clearance in overnight fasted C57BL/6N mouse at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID102819 | The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. |
| AID267082 | Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693375 | Displacement of [125I]-Tyr6, His5 from human LHRH1 receptor expressed in HEK 293 cells after 16 to 19 hrs by gamma counter | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID693382 | AUC in overnight fasted C57BL/6N mouse at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID678721 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID189942 | Intestinal stability against rat jejunum sac, activity is expressed as T1/2 | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
| AID693386 | Metabolic stability in overnight fasted C57BL/6N mouse plasma assessed as compound remaining at 50 ng/mL, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID197342 | Tested in vitro for LH release from cultured rat pituitary cells, activity is expressed as pD2 value | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID693384 | Drug excretion in overnight fasted C57BL/6N mouse assessed as elimination rate constant at 1 mg/kg, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1145197 | Induction of luteinizing hormone release in ovariectomized estrogen/progesterone-treated rat at 100 ng, sc measured after 15 mins to 60 hrs post dose by RIA relative to LH-RH | 1976 | Journal of medicinal chemistry, Mar, Volume: 19, Issue:3 | Analogs of luteinizing hormone-releasing hormone with increased biological activity produced by D-amino acid substitutions in position 6. |
| AID1535409 | Suppression of plasma testosterone level in Crl:CD(SD) rat at 2 nmol/hr administered via subcutaneous osmotic pumps measured after 6 days by radioimmunoassay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4 | A new class of pentapeptide KISS1 receptor agonists with hypothalamic-pituitary-gonadal axis activation. |
| AID102938 | In vitro binding affinity for rat pituitary LHRH receptor, activity is expressed as pKI value | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID24472 | Chymotrypsin degradation half-life was determined | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
| AID267084 | Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID693385 | Metabolic stability in overnight fasted C57BL/6N mouse plasma assessed as compound remaining at 5 ng/mL, ip | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Rationally designed cyclic analogues of luteinizing hormone-releasing hormone: enhanced enzymatic stability and biological properties. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID102815 | The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor. |
| AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID409956 | Inhibition of mouse brain MAOB | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21 | Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID267085 | Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor | 2006 | Journal of medicinal chemistry, Jun-29, Volume: 49, Issue:13 | Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
| AID1755775 | In vivo agonist activity at GnRH-R in C57BL6/N mouse assessed as release of testosterone in blood at 483.6 ug/kg, ip measured after 2 hrs by LC-MS/MS analysis | |||
| 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. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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. |
| AID1346012 | Rat GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 1994 | Endocrinology, Jul, Volume: 135, Issue:1 | Stable transfection of GH3 cells with rat gonadotropin-releasing hormone receptor complementary deoxyribonucleic acid results in expression of a receptor coupled to cyclic adenosine 3',5'-monophosphate-dependent prolactin release via a G-protein. |
| AID1346002 | Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 2007 | Endocrinology, Feb, Volume: 148, Issue:2 | Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 195 (6.64) | 18.7374 |
| 1990's | 981 (33.41) | 18.2507 |
| 2000's | 909 (30.96) | 29.6817 |
| 2010's | 679 (23.13) | 24.3611 |
| 2020's | 172 (5.86) | 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 (90.83) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 777 (25.21%) | 5.53% |
| Reviews | 249 (8.08%) | 6.00% |
| Case Studies | 466 (15.12%) | 4.05% |
| Observational | 15 (0.49%) | 0.25% |
| Other | 1,575 (51.10%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Intermittent Hormonal Therapy With Leuprorelin (3.75 mg SR) and Flutamide in the Treatment of Stage D2 or Tx Nx M1 ≠ M1a Metastatic Cancer of the Prostate [NCT00817739] | Phase 2 | 341 participants (Actual) | Interventional | 1996-12-31 | Completed | ||
| "Special Drug Use Surveillance of Leuplin PRO for Injection Kit 22.5 mg in Premenopausal Breast Cancer" [NCT03209518] | 312 participants (Actual) | Observational | 2016-03-18 | Completed | |||
| A Randomized Three Arm Phase II Study of (1) Everolimus, (2) Estrogen Deprivation Therapy (EDT) With Leuprolide + Letrozole and (3) Everolimus + EDT in Patients With Unresectable Fibrolamellar Hepatocellular Carcinoma (FLL-HCC) [NCT01642186] | Phase 2 | 28 participants (Actual) | Interventional | 2012-07-12 | Completed | ||
| Randomized Clinical Trial of the Pharmacodynamics of Lorelin Depot 3.75Mg (Leuprorelin Acetate) Produced by Laboratório Químico Farmacêutico Bergamo LTDA. Compared to Lupron Depot ® 3.75 Mg Produced by Abbott in Healthy Subjects [NCT01071005] | Phase 1 | 58 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| A Phase 2 Study of Darolutamide in Combination With Leuprolide Acetate in Hormone-Therapy Naive Recurrent and/or Metastatic Androgen Receptor (AR) Positive Salivary Gland Cancer [NCT05669664] | Phase 2 | 20 participants (Anticipated) | Interventional | 2023-07-20 | Recruiting | ||
| Vascular Mechanisms for the Effects of Loss of Ovarian Hormone Function on Cognition in Women [NCT02122198] | 17 participants (Actual) | Interventional | 2014-09-08 | Completed | |||
| A Phase 1/2, Open Label Study in Men With Prostate Cancer to Assess the Safety. Pharmacokinetics and Testosterone-Lowering Efficacy of TAK-448, Administered as a 1-Month Depot, Including a Randomized Portion With a Group Administered Leuprorelin [NCT01132404] | Phase 1/Phase 2 | 9 participants (Actual) | Interventional | 2010-11-30 | Terminated(stopped due to Developing new formulation of study drug. New study to open next year under a new protocol.) | ||
| Influence of Male Hormones on Regional Fat Metabolism [NCT01160328] | Phase 1 | 39 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| A Phase II Trial of GnRH Agonist for the Preservation of Ovarian Function After Hematopoietic Cell Transplantation (HCT) [NCT01343368] | Phase 2 | 19 participants (Actual) | Interventional | 2011-07-31 | Terminated | ||
| A Phase IV Interventional Safety Study of ELIGARD® in Prostate Cancer Patients in Asia (ELIGANT) [NCT03035032] | Phase 4 | 107 participants (Actual) | Interventional | 2017-06-23 | Completed | ||
| An Observational, Retrospective Study to Evaluate the Long Term Safety and Effectiveness of Leuprorelin in the Treatment of Central Precocious Puberty [NCT02993926] | 108 participants (Actual) | Observational | 2017-06-24 | Completed | |||
| Radiation Therapy and Androgen Deprivation Therapy in Treating Patients Who Have Undergone Surgery for Prostate Cancer (RADICALS) [NCT00541047] | Phase 3 | 4,236 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| A Double Blinded Randomized Crossover Phase III Study of Oral Thalidomide Versus Placebo in Patients With Stage D0 Androgen Dependent Prostate Cancer Following Limited Hormonal Ablation [NCT00004635] | Phase 3 | 159 participants (Actual) | Interventional | 2000-03-01 | Completed | ||
| A Phase III Randomized Prospective Trial of Adjuvant Hormonal Therapy in Surgically Treated Prostate Cancer Patients at High Risk for Recurrence [NCT00003645] | Phase 3 | 64 participants (Actual) | Interventional | 1999-06-14 | Terminated(stopped due to Per PI request) | ||
| Regulation of Cervical Mucus Secretion [NCT02969590] | Phase 4 | 5 participants (Actual) | Interventional | 2015-03-29 | Completed | ||
| Clinical Trial to Investigate the Safety and Pharmacokinetics/Pharmacodynamics of CKD-841 After Subcutaneous Injection in Postmenopausal Female [NCT03233932] | Phase 1 | 13 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
| Psychological Impact of Amenorrhea in Women With Endometriosis: Perspective Randomized Study [NCT02393482] | Phase 4 | 50 participants (Anticipated) | Interventional | 2021-06-30 | Not yet recruiting | ||
| HERO: A Multinational Phase 3 Randomized, Open-label, Parallel Group Study to Evaluate the Safety and Efficacy of Relugolix in Men With Advanced Prostate Cancer [NCT03085095] | Phase 3 | 1,134 participants (Actual) | Interventional | 2017-04-18 | Completed | ||
| Evaluation of the Testosterone Suppressive Effect in Healthy Male Volunteers of a Novel Leuprolide Acetate 3.75mg Depot (Lutrate) VS Market Reference Leuprolide Acetate 3.75mg Depot (Enantone) [NCT03662958] | 48 participants (Anticipated) | Interventional | 2018-08-01 | Recruiting | |||
| Comparison of the Operation and Medical Treatment of Endometriosis and Adenomyosis [NCT03778359] | 5,000 participants (Actual) | Observational | 2005-01-01 | Completed | |||
| Phase II Trial of Zometa on Bone Mineral Density on Patients With Stage D Prostate Cancer Undergoing Androgen Ablation Therapy [NCT00582556] | Phase 2 | 44 participants (Actual) | Interventional | 2003-04-30 | Completed | ||
| Prospective Multicenter Observational Program for Evaluation of Efficacy and Tolerability of the 6-month Depot Eligard 45 mg in Patients With Advanced Prostate Carcinoma in Routine Clinical Practice of Uro-Oncologists in the Russian Federation [NCT02128334] | 645 participants (Actual) | Observational | 2013-09-30 | Completed | |||
| Real-life Observational Study of Patients After 3-months of Leuprorelin 5mg Implant and Evaluation of Coping Strategies Among Patients With Prostate Cancer: LEPTO STUDY [NCT03990194] | 800 participants (Anticipated) | Observational | 2021-03-30 | Not yet recruiting | |||
| Phase II Study Evaluating HSV-tk + Valacyclovir Gene Therapy in Combination With Androgen Deprivation Therapy, Brachytherapy, External Beam Radiotherapy, and Prostatectomy for High-Risk Prostate Cancer [NCT03541928] | Phase 2 | 60 participants (Anticipated) | Interventional | 2018-08-02 | Recruiting | ||
| An Open-label, Single Arm, Multicenter, Phase III Study on the Efficacy, Safety, and Pharmacokinetics of FP-001 42 mg Controlled Release in Patients With Central (Gonadotropin-Dependent) Precocious Puberty (Casppian Study) [NCT05493709] | Phase 3 | 93 participants (Anticipated) | Interventional | 2023-06-02 | Recruiting | ||
| Comparative Study Between ICSI Results in Transvaginal Ultrasound Guided Embryo Transfer and Transabdominal Ultrasound Guided Embryo Transfer [NCT03683043] | Phase 4 | 120 participants (Anticipated) | Interventional | 2018-09-30 | Not yet recruiting | ||
| Evidence-based Medical Research on the Treatment of Children's Rapid Progressive Central Precocious Puberty With Integrative Chinese and Western Medicine [NCT03963752] | Phase 4 | 164 participants (Anticipated) | Interventional | 2019-08-15 | Recruiting | ||
| The Impact of Adjuvant Androgen Deprivation Following Radical Prostatectomy on Prostate Cancer Recurrence [NCT05169112] | Phase 3 | 40 participants (Anticipated) | Interventional | 2023-03-06 | Recruiting | ||
| A Phase 3 Study of Androgen Annihilation in High-Risk Biochemically Relapsed Prostate Cancer [NCT03009981] | Phase 3 | 504 participants (Anticipated) | Interventional | 2017-03-06 | Active, not recruiting | ||
| A Phase 2 Trial of Radium Ra 223 Dichloride in Combination With Androgen Deprivation Therapy and Stereotactic Body Radiation Therapy for Patients With Oligometastatic Castration Sensitive Prostate Cancer [NCT03361735] | Phase 2 | 25 participants (Actual) | Interventional | 2018-08-29 | Active, not recruiting | ||
| A Phase I/II Study of High-Dose-Rate Brachytherapy as Monotherapy for Prostate Cancer [NCT02346253] | 163 participants (Anticipated) | Interventional | 2015-01-13 | Active, not recruiting | |||
| A Single-Arm, Open-Label, Phase II Study of Systemic and Tumor Directed Therapy for Recurrent Oligometastatic M1 Prostate Cancer [NCT03902951] | Phase 2 | 28 participants (Actual) | Interventional | 2021-03-17 | Active, not recruiting | ||
| Phase III Study of Image Guided Radiation Therapy With or Without Androgen Suppression for Intermediate Risk Adenocarcinoma of the Prostate [NCT01492972] | Phase 3 | 192 participants (Anticipated) | Interventional | 2012-01-31 | Recruiting | ||
| Ovarian Suppression Plus Letrozole Plus Everolimus for Hormone Receptor-Positive, Tamoxifen and Ovarian Suppression Pretreated, Premenopausal Women With Recurrent or Metastatic Breast Cancer[LEO] [NCT02344550] | Phase 2 | 137 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| Efficacy of Recombinant FSH/GnRH Antagonist Protocol With and Without LH Adjunct and GnRH Agonist Trigger for Egg Bank Donation [NCT02069808] | Phase 4 | 38 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| A Prospective Randomised Controlled Trial of GnRH Agonist and Progesterone Versus Progesterone Only for Luteal Phase Support in Antagonist Cycles [NCT02262416] | Phase 3 | 200 participants (Anticipated) | Interventional | 2015-01-31 | Not yet recruiting | ||
| Phase II Study of Neo-adjuvant Chemotherapy With Letrozole in Patients With Estrogen Receptor Positive/HER-2 Negative Breast Cancer [NCT03497702] | Phase 2 | 114 participants (Anticipated) | Interventional | 2017-05-08 | Recruiting | ||
| Multi-Institutional Prospective Pilot Study of Lupron to Enhance Lymphocyte Immune Reconstitution Following Allogeneic Bone Marrow Transplantation in Post-Pubertal Children and Adults With Molecular Imaging Evaluation [NCT01338987] | Phase 2 | 76 participants (Actual) | Interventional | 2011-04-19 | Completed | ||
| A Phase 1/2 Study of Darolutamide and Abemaciclib in High-Risk Prostate Cancer [NCT05617885] | Phase 1/Phase 2 | 93 participants (Anticipated) | Interventional | 2023-08-09 | Recruiting | ||
| A Single Dose lead-in PK Followed by a Randomized, Double-blinded, Controlled, Multiple Dose Study of the Selective Progesterone Receptor Modulator Progenta (CDB-4124) in Pre-menopausal Women With Symptomatic Leiomyomata [NCT01069094] | Phase 1/Phase 2 | 29 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
| Phase III Trial of Dose Escalated Radiation Therapy and Standard Androgen Deprivation Therapy (ADT) With a GNRH Agonist vs. Dose Escalated Radiation Therapy and Enhanced ADT With a GNRH Agonist and TAK-700 For Men With High Risk Prostate Cancer [NCT01546987] | Phase 3 | 239 participants (Actual) | Interventional | 2012-05-31 | Active, not recruiting | ||
| Effects of the Levonorgestrel-releasing Intrauterine System Compared With the Leuprolide Acetate in Patients With Endometriosis: a Randomized Trial [NCT02158845] | Phase 4 | 44 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| Testosterone Regulation of the Natriuretic Peptide System [NCT02269072] | 0 participants (Actual) | Interventional | 2015-02-28 | Withdrawn(stopped due to Lack of funding) | |||
| "Special Drug Use Surveillance of Leuplin PRO for Injection Kit 22.5 mg for Prostate Cancer" [NCT03209492] | 333 participants (Actual) | Observational | 2016-04-01 | Completed | |||
| A Phase 3, Open-Label, Multi-Center, Safety And Efficacy Study of Oakwood Laboratories' Leuprolide Acetate For Injectable Suspension 22.5 mg In Patients With Prostate Cancer [NCT00598312] | Phase 3 | 201 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| COMPLEEMENT-1: An Open-label, Multicenter, Phase IIIb Study to Assess the Safety and Efficacy of Ribociclib (LEE011) in Combination With Letrozole for the Treatment of Men and Pre/Postmenopausal Women With Hormone Receptor-positive (HR+) HER2-negative (HE [NCT02941926] | Phase 3 | 3,246 participants (Actual) | Interventional | 2016-11-30 | Completed | ||
| A Phase 3, Randomized, Efficacy and Safety Study of Enzalutamide Plus Leuprolide, Enzalutamide Monotherapy, and Placebo Plus Leuprolide in Men With High-Risk Nonmetastatic Prostate Cancer Progressing After Definitive Therapy [NCT02319837] | Phase 3 | 1,068 participants (Actual) | Interventional | 2014-12-17 | Active, not recruiting | ||
| Comparative Efficacy and Safety of Combined Radiotherapy and Adjuvant Hormone Therapy (Leuprorelin SR 11.25 mg) and Hormone Therapy Alone (Leuprorelin SR 11.25 mg) in Locally Advanced Prostate Cancer (T3-T4 or pT3 on Biopsy, N0, M0) [NCT01122121] | Phase 3 | 273 participants (Actual) | Interventional | 2000-03-31 | Completed | ||
| Phase III Clinical Study to Evaluate Efficacy and Safety of TAK-385 40 mg Compared With Leuprorelin in Patients With Endometriosis [NCT03931915] | Phase 3 | 335 participants (Actual) | Interventional | 2019-05-08 | Completed | ||
| Relugolix Versus Leuprolide in Patients With Prostate Cancer: A Randomized, Open-Label Study to Assess Major Adverse Cardiovascular Events (REPLACE-CV) [NCT05605964] | Phase 3 | 2,250 participants (Anticipated) | Interventional | 2023-01-25 | Recruiting | ||
| A Phase II Study Comparing Salvage Radiotherapy in Combination With 6 Months of Androgen-deprivation Therapy Versus Anti-androgen Therapy With Apalutamide in Patients With Biochemical Progression After Radical Prostatectomy [NCT03899077] | Phase 2 | 202 participants (Anticipated) | Interventional | 2019-04-05 | Recruiting | ||
| Phase II Evaluation of Early Oral Estramustine, Oral Etoposide and Intravenous Paclitaxel in Combination With Hormone Therapy in Patients With High-Risk Metastatic Adenocarinoma of the Prostate [NCT00028769] | Phase 2 | 41 participants (Actual) | Interventional | 2001-12-31 | Completed | ||
| A PHASE III TRIAL OF THE STUDY OF ENDOCRINE THERAPY USED AS A CYTOREDUCTIVE AND CYTOSTATIC AGENT PRIOR TO RADIATION THERAPY IN GOOD PROGNOSIS LOCALLY CONFINED ADENOCARCINOMA OF THE PROSTATE [NCT00002597] | Phase 3 | 2,028 participants (Actual) | Interventional | 1994-10-31 | Completed | ||
| The Effects of GnRH-a on Angiogenesis of Endometriosis [NCT06106932] | 60 participants (Actual) | Interventional | 2015-09-30 | Completed | |||
| Initiation of Androgen Deprivation Therapy for the Treatment of Prostate Cancer Using Degarelix Acetate Followed by Leuprolide Acetate [NCT01344564] | 50 participants (Actual) | Interventional | 2011-04-30 | Completed | |||
| Phase II Trial of Radiation With Androgen Deprivation: Abiraterone Acetate, Prednisone and Luteinizing Hormone Releasing Hormone Agonist Prior to Radiation Therapy [NCT01023061] | Phase 2 | 24 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| CLASSICAL ANTAGONIST PROTOCOL IN COMPARISON WITH AGONIST STOP PROTOCOL IN Polycystic Ovary Symdrome WOMEN UNDERGOING Intra-cytoplasmic Injection TRIAL: a Randomized Controlled Trial [NCT04094467] | Phase 4 | 150 participants (Anticipated) | Interventional | 2019-12-07 | Recruiting | ||
| Phase I/II Study of Radioimmunoguided Intensity Modulated Radiotherapy (IMRT) for Prostate Cancer [NCT00653757] | Phase 1/Phase 2 | 100 participants (Anticipated) | Interventional | 2002-03-31 | Completed | ||
| A Phase II Study of Advanced Salivary Gland Carcinoma Based on Molecular Typing [NCT05924256] | Phase 2 | 66 participants (Anticipated) | Interventional | 2023-07-26 | Recruiting | ||
| Estrogen Deficiency and Mechanisms of Fat Accumulation [NCT00687739] | Phase 3 | 79 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| A Multi-center, Active Controlled, Pharmacokinetic, Safety and Efficacy Study of Proellex in Pre-Menopausal Women With Symptomatic Uterine Fibroids to Assess Persistence of Response [NCT00683917] | Phase 2 | 10 participants (Actual) | Interventional | 2008-05-31 | Terminated(stopped due to Repros stopped the study for safety and FDA put the study on hold for safety.) | ||
| A Multi-Center, Randomized, Open-Label Evaluation of MENOPUR® Versus FOLLISTIM® in Polycystic Ovarian Syndrome (PCOS) Patients [NCT00805935] | Phase 4 | 110 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| A Phase III Study of Neoadjuvant Docetaxel and Androgen Suppression Plus Radiation Therapy Versus Androgen Suppression Alone Plus Radiation Therapy for High-Risk Localized Adenocarcinoma of the Prostate [NCT00651326] | Phase 3 | 48 participants (Actual) | Interventional | 2008-06-02 | Terminated(stopped due to Poor accrual) | ||
| Does a GnRH Agonist Given at Embryo Transfer Improve Clinical Pregnancy and Live Birth Rates of Women Undergoing In-Vitro Fertilization? [NCT03544073] | Phase 3 | 0 participants (Actual) | Interventional | 2019-04-15 | Withdrawn(stopped due to The investigators were not able to get grant funding for this study.) | ||
| The LUCINDA Trial: LeUprolide Plus Cholinesterase Inhibition to Reduce Neurological Decline in Alzheimer's [NCT03649724] | Phase 2 | 180 participants (Anticipated) | Interventional | 2020-11-27 | Recruiting | ||
| "Specified Drug-Use Survey of Leuprorelin Acetate Injection Kit 11.25 mg All-Case Investigation: Spinal and Bulbar Muscular Atrophy (SBMA)" [NCT03555578] | 300 participants (Anticipated) | Observational | 2017-11-02 | Recruiting | |||
| The Association Between HSD3B1 Genotype and Steroid Metabolism in Normal and Prostate Cancer Tissue of Men With Intermediate and High-risk Prostate Cancer Undergoing Radical Prostatectomy After Treatment With Apalutamide and Leuprolide [NCT02770391] | Phase 2 | 54 participants (Actual) | Interventional | 2016-10-17 | Completed | ||
| Down-regulated Hormonally Controlled Cycles for Vitrification-warmed Blastocyst Transfers: Reduces Time to Transfer and Cycle Cancellation [NCT02238431] | 0 participants (Actual) | Interventional | 2014-12-31 | Withdrawn(stopped due to no patient uptake) | |||
| Efficacy, Safety, and Pharmaco-kinetics of Leuprolide Acetate for Injection 3.75mg (Depot) (Leuprorelin) Administered in Subjects With Advanced Adenocarcinoma of Prostate: A Randomized, Active Controlled, Comparative, Open-Label, Multi-Center, Phase 3 Stu [NCT04914195] | Phase 3 | 155 participants (Actual) | Interventional | 2021-07-01 | Completed | ||
| A Randomized Study of Finite Androgen Ablation vs. Finite Androgen Ablation in Combination With Abiraterone Acetate and Prednisone in Patients With Prostate Cancer Who Have PSA Progression After Prostatectomy and/or Radiotherapy [NCT01786265] | Phase 2 | 310 participants (Anticipated) | Interventional | 2013-02-05 | Active, not recruiting | ||
| An Open Label, Multicenter Study to Assess the Safety and Efficacy of Leuprorelin in the Treatment of Central Precocious Puberty [NCT02427958] | Phase 4 | 307 participants (Actual) | Interventional | 2015-08-07 | Completed | ||
| A Randomized, Open-label, Parallel-group, Active-control PK/PD Study of Three Doses of Leuprolide Oral Tablets in Comparison to an IM Dose of Leuprolide in Healthy Female Volunteers [NCT02807363] | Phase 2 | 35 participants (Actual) | Interventional | 2017-08-23 | Completed | ||
| Randomized, Open-label, Parallel-group, Multi-centre Phase II Clinical Trial of Active Cellular Immunotherapy With Preparation DCVAC/PCa in Combination With Hormone Therapy in Patients With Metastatic Prostate Cancer [NCT02107391] | Phase 2 | 63 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| To Evaluate the Effect of GnRH Agonist Administered in the Luteal Phase on ART Cycle Outcomes in Both GnRH Agonist and GnRH Antagonist Treated Ovarian Stimulation Protocols [NCT02114645] | 100 participants (Anticipated) | Interventional | 2014-04-30 | Not yet recruiting | |||
| Menopausal Sleep Fragmentation: Impact on Body Fat Gain Biomarkers in Women [NCT03047330] | Phase 4 | 125 participants (Actual) | Interventional | 2017-07-15 | Completed | ||
| A Phase I Trial to Evaluate Acute and Late Toxicities of Concurrent Treatment With Everolimus (RAD001) and Radio-Hormonotherapy in High-risk Prostate Cancer.(RHOMUS) [NCT00943956] | Phase 1 | 30 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
| Immediate or Early Salvage Post-operative External Radiotherapy Combined With Concomitant and Adjuvant Hormonal Treatment Versus Immediate or Early Salvage Postoperative External Radiotherapy Alone in pT3a-b R0-1 cN0M0 / pT2R1 cN0M0, Gleason Score 5-10 Pr [NCT00949962] | Phase 3 | 87 participants (Actual) | Interventional | 2009-10-31 | Terminated(stopped due to Poorly recruiting) | ||
| Long-term Effects of Enhanced Systemic Therapy and Tumor-directed Therapy for Newly Diagnosed Oligometastatic Prostate Cancer Confirmed by Conventional Imaging Modality: a Prospective, Single-arm Study. [NCT05212857] | Phase 2 | 160 participants (Anticipated) | Interventional | 2022-04-30 | Recruiting | ||
| Follicle-Stimulating Hormone (FSH) and the Onset of Puberty [NCT00734279] | Early Phase 1 | 11 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| A Randomized, Open Label, Multicenter, Phase III, 2-Arm Study of Androgen Deprivation With Leuprolide, +/- Docetaxel for Clinically Asymptomatic Prostate Cancer Subjects With a Rising PSA Following Definitive Local Therapy [NCT00514917] | Phase 3 | 413 participants (Actual) | Interventional | 2007-07-31 | Terminated(stopped due to Company decision to discontinue the study, not due to any safety or efficacy concerns) | ||
| Autonomic and Renal Contributions to Hypertension With Androgen Deprivation Therapy [NCT05700903] | Phase 4 | 228 participants (Anticipated) | Interventional | 2023-09-20 | Recruiting | ||
| A Randomized, Phase II Study of GW786034 (Pazopanib) in Stage D0 Relapsed Androgen Sensitive Prostate Cancer Following Limited GnRH Agonist Therapy [NCT00454571] | Phase 2 | 37 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Postoperative Hypofractionated Radiation Therapy and Hormonal Therapy in Patients With Prostate Cancer: A Phase II Trial [NCT04249154] | Phase 2 | 77 participants (Anticipated) | Interventional | 2019-09-03 | Recruiting | ||
| Ulipristal Acetate Versus GnRH Analogue Treatment Before Hysteroscopic Resection of Uterine Leiomyoma [NCT02361879] | Phase 4 | 146 participants (Anticipated) | Interventional | 2015-02-28 | Recruiting | ||
| Phase II-III Trial of Adjuvant Radiotherapy Following Radical Prostatectomy With or Without Adjuvant Docetaxel [NCT03070886] | Phase 2/Phase 3 | 175 participants (Actual) | Interventional | 2017-01-16 | Active, not recruiting | ||
| A Randomized Controlled Trial of Pre-retrieval Triggering Methods in in Vitro Fertilization Patients Classified as Low, Normal or High Responder [NCT02715336] | Phase 4 | 666 participants (Anticipated) | Interventional | 2015-10-31 | Recruiting | ||
| Anti-Androgens and Cabazitaxel in Defining Complete Response in Prostatectomy (ACDC-RP Trial): A Randomized, Open-label, Multi-centre Phase-2 Study Evaluating the Pathological Complete Response (pCR) Rate Following Neoadjuvant Therapy in Participants With [NCT02543255] | Phase 2 | 76 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
| Phase II Trial of Abraxane Plus Hormonal Therapy as Initial Treatment of Unresectable or Metastatic Adenocarcinoma of the Prostate [NCT00521781] | Phase 2 | 14 participants (Actual) | Interventional | 2007-08-31 | Terminated(stopped due to Sponsor decision) | ||
| Apalutamide Plus Intermittent Hormone Therapy (IHT) Versus IHT Alone in Prostate Cancer Patients With Biochemical Recurrence [NCT02811809] | Phase 2 | 0 participants (Actual) | Interventional | 2020-12-31 | Withdrawn(stopped due to Withdrawn due to operational issues. The study was withdrawn early, before enrolling its first participant.) | ||
| A Controlled Trial on Adenomyosis Treatment Comparing Aromatase Inhibitor Plus GnRH Analogue Versus GnRH Analog Alone [NCT03421639] | Phase 4 | 300 participants (Anticipated) | Interventional | 2017-12-01 | Recruiting | ||
| An Open Label, Multicenter, Single-arm and Prospective Study to Assess the Efficacy and Safety of Leuprorelin 3M in the Treatment of Central Precocious Puberty (CPP) [NCT05341115] | Phase 4 | 80 participants (Anticipated) | Interventional | 2023-03-14 | Recruiting | ||
| PCOS, Sleep Apnea and Metabolic Risk in Women [NCT00696111] | 80 participants (Anticipated) | Interventional | 2007-12-31 | Active, not recruiting | |||
| "A Phase IIA Study of Sequential (First Strike, Second Strike) Therapies, Modeled on Evolutionary Dynamics of Anthropocene Extinctions, for High Risk Metastatic Castration Sensitive Prostate Cancer" [NCT05189457] | Phase 2 | 31 participants (Anticipated) | Interventional | 2022-01-25 | Recruiting | ||
| A Phase II Neoadjuvant Trial of Sunitinib Malate (SU011248) Plus Hormonal Ablation for Patients Who Have High Risk Localized Prostate Cancer and Will Undergo Prostatectomy [NCT00329043] | Phase 2 | 64 participants (Anticipated) | Interventional | 2006-05-31 | Active, not recruiting | ||
| Phase II, Multicenter, Single Arm Trial to Assess the Feasibility of First Line Ribociclib in Combination With a Non Steroidal Aromatase Inhibitor in Elderly Patients With Hormone Receptor Positive/HER2 Negative Advanced Breast Cancer [NCT03944434] | Phase 2 | 116 participants (Actual) | Interventional | 2018-12-27 | Active, not recruiting | ||
| Efficacy and Safety of Somatropin in Combination With Leuprorelin Compared to Somatropin Alone in Pubertal Children With Idiopathic Short Stature [NCT00355030] | Phase 3 | 91 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| An Open-label, Multi-Centre, Randomized, Parallel-group Study, Investigating the Efficacy and Safety of Degarelix One Month Dosing Regimens; 160 mg (40 mg/ml) and 80 mg (20mg/ml), in Comparison to LUPRON DEPOT® 7.5 mg in Patients With Prostate Cancer Requ [NCT00295750] | Phase 3 | 620 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| Efficacy and Tolerance of Cyproterone Acetate Versus Medroxyprogesterone Acetate Versus Venlafaxine LP in the Treatment of Hot Flushes Caused by Leuprorelin 11.25 mg in Patients Treated for a Prostate Adenocarcinoma [NCT01011751] | Phase 3 | 311 participants (Actual) | Interventional | 2004-04-30 | Completed | ||
| Neoadjuvant Androgen Depletion in Combination With Vorinostat Followed by Radical Prostatectomy for Localized Prostate Cancer: Total Androgen-Receptor Gene Expression Targeted Therapy (TARGET) [NCT00589472] | Phase 2 | 19 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| 3 Months, Open-Label, Parallel-Group Study of the Pharmacodynamics, Pharmacokinetics and Safety of TAP-144SR 1-month Depot Gelatin-Free vs. Gelatin-Containing Formulation in Female Patients With Uterine Fibroids [NCT00776074] | Phase 2 | 80 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Phase II Interstitial Brachytherapy Combined With Androgen Deprivation Therapy for Locally Recurrent Prostate Cancer After Prior External Beam Irradiation [NCT00684905] | Phase 2 | 50 participants (Anticipated) | Interventional | 2000-04-30 | Completed | ||
| Study of Lupron Depot In The Treatment of Central Precocious Puberty [NCT00660010] | Phase 3 | 55 participants (Actual) | Interventional | 1991-01-31 | Completed | ||
| A Phase II, Randomized, Double-Blind, Placebo- and Active-Controlled Study to Assess the Efficacy and Safety of NBI-56418 in Subjects With Endometriosis [NCT00797225] | Phase 2 | 174 participants (Actual) | Interventional | 2008-11-26 | Completed | ||
| Monitoring Tolerance, Safety and Acceptance of Depo-Eligard® in an Open Label, Retrospective, Non-interventional Clinical Trial [NCT00811876] | 140 participants (Actual) | Observational | 2008-09-30 | Completed | |||
| The Effect of Elagolix in Comparison to Leuprolide Acetate on in Vitro Fertilization (IVF) Cycle Outcomes After a Transfer of Euploid Embryos to Patients With Surgically Diagnosed Endometriosis: A Pilot Trial [NCT04445025] | Early Phase 1 | 30 participants (Anticipated) | Interventional | 2020-09-01 | Recruiting | ||
| A Phase II Randomized Study of Palbociclib in Combination With Exemestane Plus GnRH Versus Capecitabine in Premenopausal Women With Hormone Receptor-Positive Metastatic Breast Cancer [NCT02592746] | Phase 2 | 182 participants (Anticipated) | Interventional | 2016-06-30 | Active, not recruiting | ||
| Phase II Trial of Temporary Androgen Deprivation Therapy in High Risk Prostate Cancer Following Radical Prostatectomy [NCT00937768] | Phase 2 | 16 participants (Actual) | Interventional | 2009-07-31 | Terminated | ||
| The Role of Stereotactic Body Radiotherapy in the Management of Castration-Resistant Prostate Cancer With Oligometastases: An Adaptive Phase II/III Randomized Trial. [NCT02685397] | Phase 2/Phase 3 | 130 participants (Anticipated) | Interventional | 2016-10-31 | Recruiting | ||
| Androgen Deprivation and Localized Radiotherapy to Metastases in Patients With Oligometastatic Hormone - Sensitive Prostate Cancer [NCT00544830] | Phase 2 | 29 participants (Actual) | Interventional | 2006-07-18 | Active, not recruiting | ||
| Utility of Exosomal microRNAs to Predict Response to Androgen Deprivation Therapy in Prostate Cancer Patients [NCT02366494] | 60 participants (Anticipated) | Observational | 2015-04-29 | Active, not recruiting | |||
| Comparing the Safety and Efficacy in the Use of Dienogest, Leuprolide Acetate, DMPA and Combined Oral Contraceptive Pills (Microgynon) on Endometriosis Patients After Conservative Surgery [NCT06145438] | Phase 3 | 100 participants (Anticipated) | Interventional | 2023-09-04 | Recruiting | ||
| A Randomized Controlled Trial of Treatment Protocols to Optimize Outcomes in Poor Responder In Vitro Fertilization (IVF) Patients: E2 Patch/Antagonist Protocol Versus OCP/Microdose Lupron Protocol [NCT00826839] | Phase 4 | 0 participants (Actual) | Interventional | 2009-01-31 | Withdrawn(stopped due to poor enrollment) | ||
| A Multicenter Open-label Clinical Study on the Prevention of Premature Ovarian Failure After Hematopoietic Stem Cell Transplantation [NCT05667428] | 200 participants (Anticipated) | Interventional | 2023-03-01 | Not yet recruiting | |||
| Sunitinib, Hormonal Ablation and External Beam Radiation Therapy for High-Risk and Locally Advanced Prostate Cancer [NCT00631527] | Phase 1 | 19 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Antigonadotropin-Leuprolide in Alzheimer's Disease Drug INvestigation (ALADDIN) VP 104 Study [NCT00076440] | Phase 2 | 90 participants | Interventional | 2003-12-31 | Completed | ||
| Effect of Short Term Ovarian Suppression on Androgen Overproduction in Overweight Girls With Androgen Excess (CBS007) [NCT01422096] | Early Phase 1 | 0 participants (Actual) | Interventional | 2018-06-01 | Withdrawn(stopped due to The study team decided not to pursue this study.) | ||
| Neoadjuvant Hormonal Ablation, Imatinib Mesylate and Docetaxel Followed by Radical Prostatectomy for High-Risk Localized Prostate Cancer [NCT00500110] | Phase 2 | 39 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
| The Central Nervous System Effects of Pharmacologically Induced Hypogonadotropic Hypogonadism With and Without Estrogen and Progesterone Replacement [NCT00001322] | Phase 1/Phase 2 | 100 participants (Actual) | Interventional | 1994-06-09 | Completed | ||
| A Phase II Study of Neoadjuvant Dasatinib Plus LHRH Analogue Therapy in High-Risk Localized Prostate Cancer [NCT00860158] | Phase 2 | 1 participants (Actual) | Interventional | 2009-03-31 | Terminated(stopped due to Slow accrual; closed by funder) | ||
| A Phase I/II Trial of Post-Prostatectomy Radiation Therapy, Hormonal Therapy and Concurrent Docetaxel for High Risk Pathologic T2-T3NO (Tumor-3, Node-0) Prostate Cancer [NCT00669162] | Phase 1/Phase 2 | 27 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| A 36 Month, Multi-Center, Open-Label Extension Study to Evaluate the Safety of Leuprolide Acetate 11.25 mg and 30 mg Formulations in Children With Central Precocious Puberty [NCT00667446] | Phase 3 | 72 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| A Randomized, Controlled, Open-Label Study Investigating the Safety and Efficacy of Degarelix Given Intermittently vs Continuous Androgen Deprivation Therapy With Lupron or Degarelix in Patients With Prostate Cancer With Prior Treatment Failure After Loca [NCT00928434] | Phase 3 | 409 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| The Impact of Continuous Versus Intermittent Androgen Deprivation Therapy on Bone Mineral Density Change in Prostate Cancer Patients: A Multicenter, Randomized Clinical Trial [NCT04248621] | Phase 4 | 164 participants (Anticipated) | Interventional | 2020-01-23 | Recruiting | ||
| A Prospective Randomized Study Comparing the Use of hCG or GnRH Agonist to Trigger Final Oocyte Maturation in High Responders Undergoing in-Vitro Fertilization Treatment [NCT00349258] | Phase 4 | 66 participants | Interventional | 2004-08-31 | Completed | ||
| OMPCa-Shanghai: An Open-label, Randomized Prospective Phase II Trial of Androgen Deprivation Therapy or Androgen Deprivation Therapy Plus Definitive Treatment (Radiation or Surgery) of the Primary Tumor in Oligometastatic Prostate Cancer [NCT02742675] | Phase 2 | 200 participants (Anticipated) | Interventional | 2015-09-30 | Active, not recruiting | ||
| Treatment of Uterine Fibroids With Magnetic Resonance Guided High Intensity Focused Ultrasound [NCT02736435] | Phase 3 | 0 participants (Actual) | Interventional | 2018-01-18 | Withdrawn(stopped due to Lengthy delays and inadequate support to proceed.) | ||
| An Exploratory, Open Label, Single-arm Study to Evaluate the Effect of Eligard® 6-month on Biomarkers of Disease in Patients With Metastatic Prostate Cancer [NCT01933022] | Phase 4 | 1 participants (Actual) | Interventional | 2014-08-31 | Terminated(stopped due to Termination due to high current screen rate failure and unreliable PSA mRNA assay.) | ||
| Understanding Experimentally Induced Hot Flushes and Their Impact on Sleep and Mood [NCT00455689] | Phase 4 | 20 participants (Actual) | Interventional | 2005-11-28 | Completed | ||
| Phase Ib Study of Limited Androgen Ablation and Two Dose Levels of Temsirolimus (NSC#683864) in Patients With Prostate Cancer Who Have a Biochemical Relapse After Prostatectomy and/or Radiotherapy [NCT00512668] | Phase 1 | 24 participants (Actual) | Interventional | 2007-09-30 | Terminated | ||
| An Open-Label, Multi-Centre, Extension Study, Evaluating the Long-Term Safety and Tolerability of Degarelix One-Month Dosing Regimen in Patients With Prostate Cancer Requiring Androgen Ablation Therapy [NCT00451958] | Phase 3 | 386 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
| Phase II Study of GnRH Analogue for Ovarian Function Preservation in Hematopoietic Stem Cell Transplantation Patients [NCT00429494] | Phase 2 | 60 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
| A Phase II Study of Androgen Receptor (AR) Inhibition by Darolutamide in Combination With Leuprolide Acetate and Exemestane in Recurrent Adult-Type Ovarian Granulosa Cell Tumor [NCT06169124] | Phase 2 | 37 participants (Anticipated) | Interventional | 2023-12-15 | Not yet recruiting | ||
| Study of the Modulatory Activity of an LHRH-Agonist (Leuprolide) on Melanoma Peptide Vaccines as Adjuvant Therapy in Melanoma Patients [NCT00254397] | Phase 2 | 98 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
| BASH-PC: Bariatric Arterial Embolization for Men Starting Hormones for Prostate Cancer [NCT04331717] | Phase 2 | 0 participants (Actual) | Interventional | 2020-11-16 | Withdrawn(stopped due to accrual on hold) | ||
| A Multicenter, Open-Label, Randomized, Phase III Trial Comparing Immediate Adjuvant Hormonal Therapy (ELIGARD®- Leuprolide Acetate) in Combination With TAXOTERE® (Docetaxel) Administered Every Three Weeks Versus Hormonal Therapy Alone Versus Deferred Ther [NCT00283062] | Phase 3 | 228 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Leuprolide Acetate to Enhance Immune Function Post-Autologous Stem Cell Transplantation [NCT00275262] | Phase 2 | 25 participants (Actual) | Interventional | 2006-02-28 | Terminated | ||
| A Randomised Trial Investigating the Effect on Biochemical (PSA) Control and Survival of Different Durations of Adjuvant Androgen Deprivation in Association With Definitive Radiation Treatment for Localised Carcinoma of the Prostate. [NCT00193856] | Phase 3 | 1,071 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
| A Post-Marketing Observational Study to Document Treatment Patterns and to Evaluate Leuprolide and Alternative Therapeutic Approaches to the Treatment of Advanced Prostate Cancer [NCT01081873] | 2,717 participants (Actual) | Observational | 2004-06-30 | Completed | |||
| An Evolutionary Double Bind Phase II Neoadjuvant Study of Abiraterone Acetate, Leuprolide Acetate, and Belzutifan in Men With Regional Prostate Cancer Eligible for Prostatectomy [NCT05574712] | Phase 2 | 30 participants (Anticipated) | Interventional | 2024-01-01 | Not yet recruiting | ||
| [NCT00004311] | Phase 2 | 0 participants | Interventional | 1989-07-31 | Completed | ||
| An Open Label, Randomized, Phase II Trial of Metabolic Complications in Patients Treated With Enzalutamide vs Standard ADT for the Treatment of Hormone Sensitive Prostate Cancer [NCT02278185] | Phase 2 | 19 participants (Actual) | Interventional | 2015-11-11 | Active, not recruiting | ||
| A Randomized, Phase II Trial of Brief Androgen-Ablation Combined With Cell-based CG1940/CG8711 Immunotherapy For Prostate Cancer in Patients With Non-Metastatic, Biochemically Relapsed Prostate Cancer [NCT00771017] | Phase 2 | 0 participants (Actual) | Interventional | 2008-07-31 | Withdrawn | ||
| A reAl-World Evidence Study Using Alberta Population Based Data to Describe Treatment Patterns for Metastatic castRation sENsitivE proState Cancer patientS (AWARENESS) [NCT05149131] | 400 participants (Anticipated) | Observational | 2022-01-17 | Active, not recruiting | |||
| Phase II Study of Talazoparib With Androgen Deprivation Therapy and Abiraterone in Castration Sensitive Prostate Cancer [NCT04734730] | Phase 2 | 70 participants (Anticipated) | Interventional | 2021-05-04 | Recruiting | ||
| Multicentric Phase II Trial of Salvage Radiotherapy Combined With Hormonotherapy in Oligometastatic Pelvic Node Relapses of Prostate Cancer (OLIGOPELVIS / GETUG P07) [NCT02274779] | Phase 2 | 70 participants (Anticipated) | Interventional | 2014-08-20 | Active, not recruiting | ||
| Sleep, Metabolic, and Cardiovascular Dysfunction in Polycystic Ovary Syndrome [NCT00203996] | Phase 4 | 37 participants (Actual) | Interventional | 2003-09-30 | Terminated(stopped due to Did not meet target patient accrual goals) | ||
| Phase 2 Response Evaluation of Finite Systemic Therapy With Advanced Androgen Signaling Inhibition and Radiation Therapy for Oligorecurrent Prostate Cancer (RESTART) [NCT04585932] | Phase 2 | 0 participants (Actual) | Interventional | 2020-11-24 | Withdrawn(stopped due to At the request of the ad interim Department Chairman due to PI is no longer at institution.) | ||
| A Randomized, Open-Label, Neoadjuvant Prostate Cancer Trial of Abiraterone Acetate Plus LHRHa Versus LHRHa Alone [NCT01088529] | Phase 2 | 66 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
| An Open Label Randomized Phase 2 Study To Evaluate The Activity, Tolerability, And Toxicity Of Combined Neoadjuvant Anti-angiogenesis and Androgen Ablation Therapy in Men Undergoing Radical Prostatectomy [NCT00244920] | Phase 2 | 0 participants (Actual) | Interventional | 2002-01-31 | Withdrawn(stopped due to Sponsor withdrew drug.) | ||
| A Phase III Confirmatory Study of KLH-2109 in Uterine Fibroids Patient With Menorrhagia [NCT05440383] | Phase 3 | 264 participants (Anticipated) | Interventional | 2022-10-11 | Active, not recruiting | ||
| Parallel Phase III Randomized Trials of Genomic-Risk Stratified Unfavorable Intermediate Risk Prostate Cancer: De-Intensification and Intensification Clinical Trial Evaluation (GUIDANCE) [NCT05050084] | Phase 3 | 2,050 participants (Anticipated) | Interventional | 2021-11-03 | Recruiting | ||
| Parallel Phase III Randomized Trials for High Risk Prostate Cancer Evaluating De-Intensification for Lower Genomic Risk and Intensification of Concurrent Therapy for Higher Genomic Risk With Radiation (PREDICT-RT*) [NCT04513717] | Phase 3 | 2,478 participants (Anticipated) | Interventional | 2020-12-15 | Recruiting | ||
| Strength, Aging, and Memory in Prostate Cancer: A Prospective Study of the Effects of Androgen Deprivation on Neurocognition and Frailty [NCT04852224] | 20 participants (Actual) | Observational | 2021-10-01 | Completed | |||
| Phase II Study of Neoadjuvant Hormonal Therapy Plus Docetaxel Followed by Radical Prostatectomy for Men With Proven or Suspected Node-positive Prostate Cancer [NCT01076335] | Phase 2 | 40 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
| A Phase 2 Study of Neoadjuvant PARP Inhibition Followed by Radical Prostatectomy in Patients With Unfavorable Intermediate-Risk or High-Risk Prostate Cancer With BRCA1/2 Gene Alterations (NePtune) [NCT05498272] | Phase 2 | 32 participants (Anticipated) | Interventional | 2023-02-01 | Recruiting | ||
| Phase III Study of Local or Systemic Therapy INtensification DIrected by PET in Prostate CAncer Patients With Post-ProstaTEctomy Biochemical Recurrence (INDICATE) [NCT04423211] | Phase 3 | 804 participants (Anticipated) | Interventional | 2020-10-08 | Recruiting | ||
| Lucrin® Depot Efficacy and Safety Monitoring Study in Patients With Advanced Prostate Cancer and Lower Urinary Tract Symptoms. International, Multicenter Post-marketing Observational Study. [NCT01078545] | 729 participants (Actual) | Observational | 2008-09-30 | Completed | |||
| A Phase II Study of NEOADjuvant Aromatase Inhibitor and Pertuzumab/Trastuzumab (NEOADAPT) [NCT02689921] | Phase 2 | 7 participants (Actual) | Interventional | 2016-04-30 | Active, not recruiting | ||
| A Phase II Randomized Study of Enzalutamide+Leuprolide Versus Enzalutamide+Leuprolide+Abiraterone Acetate+Prednisone as Neoadjuvant Therapy for HIgh-Risk Prostate Cancer Undergoing Prostatectomy [NCT02268175] | Phase 2 | 75 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
| [NCT02778919] | Phase 2 | 0 participants | Interventional | 2016-05-09 | Completed | ||
| A Novel Approach to Endometrial Preparation in Recipients of Donor Cycles [NCT01424618] | 20 participants (Anticipated) | Interventional | 2006-01-31 | Recruiting | |||
| Neoadjuvant Estradiol or Androgen Deprivation in Clinically Localized Prostate Cancer [NCT00167648] | Phase 2 | 17 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| BYLieve: A Phase II, Multicenter, Open-label, Three-cohort, Non- Comparative Study to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant or Letrozole in Patients With PIK3CA Mutant, Hormone Receptor (HR) Positive, HER2-negative Advanced Breast C [NCT03056755] | Phase 2 | 383 participants (Actual) | Interventional | 2017-08-14 | Active, not recruiting | ||
| Leuprolide Acetate Suppresses Pedophilic Urges and Arousability [NCT00220350] | Phase 2/Phase 3 | 10 participants | Interventional | 2001-10-31 | Active, not recruiting | ||
| A Phase IIIb Randomized Study of Intermittent Versus Continuous Androgen Deprivation Therapy Using ELIGARD 22.5 mg 3-month Depot in Subjects With Relapsing and Locally Advanced Prostate Cancer Who Are Responsive to Such Therapy [NCT00378690] | Phase 3 | 706 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| The ELDORADO (Eligard®, Docetaxel and Radiotherapy) Study: A Phase II Study of Chemo - Hormonal Therapy and Radiation in High Risk Prostate Cancer [NCT00452556] | Phase 2 | 86 participants (Anticipated) | Interventional | 2007-05-31 | Active, not recruiting | ||
| Comparative Controlled Clinical Trial of Two Pharmacological Treatments of Pedophilia [NCT00601276] | Phase 3 | 48 participants (Anticipated) | Interventional | 2007-12-31 | Terminated | ||
| CASPAR - A Phase III Trial of Enzalutamide and Rucaparib as a Novel Therapy in First-Line Metastatic Castration-Resistant Prostate Cancer [NCT04455750] | Phase 3 | 61 participants (Actual) | Interventional | 2021-02-19 | Active, not recruiting | ||
| The Impact of Estrogen Status on the Biological Function of Brown Adipose Tissue in Women Measured Using Quantitative PET/CT [NCT02927392] | 72 participants (Anticipated) | Interventional | 2017-01-01 | Completed | |||
| [NCT00505817] | Phase 4 | 0 participants | Interventional | Completed | |||
| Multi-site Study of Comprehensive Treatment for Children Precocious Puberty [NCT02920515] | Phase 4 | 740 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| Generation of Positive Biological Samples to Leuprolide Acetate for Doping Control [NCT02920359] | Phase 1 | 5 participants (Actual) | Interventional | 2016-11-17 | Completed | ||
| A Phase III Clinical Trial to Evaluate the Efficacy and Safety of DWJ108J in Patients With Central Precocious Puberty : A Single-arm, Open-label, Multi-center, Prospective Study [NCT06025409] | Phase 3 | 79 participants (Anticipated) | Interventional | 2023-08-01 | Recruiting | ||
| Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for OligoRecurrenT Prostate Cancer (VA STARPORT) [NCT04787744] | Phase 2/Phase 3 | 464 participants (Anticipated) | Interventional | 2021-07-01 | Recruiting | ||
| A Phase IIIb Study to Characterize the Effectiveness and Safety of ADJUVANT Ribociclib in Broad Real-World patIent Populations in Stage II anD Stage III HR+/HER2- Early Breast canceR (ADJUVANT WIDER) [NCT05827081] | Phase 3 | 2,500 participants (Anticipated) | Interventional | 2024-01-16 | Not yet recruiting | ||
| PROTOCOL FOR THE SCOTTISH PREMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002580] | Phase 3 | 1,000 participants (Anticipated) | Interventional | 1993-06-30 | Completed | ||
| [NCT00004344] | 4 participants | Observational | 1997-01-31 | Completed | |||
| PROtecting Ovaries and Fertility During Chemotherapy - The PROOF Trial: A Randomized Controlled Trial of Gonadotropin Releasing Hormone Agonist (GnRHa) for Fertility Preservation in Oncology Patients [NCT00380406] | Phase 3 | 30 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A Phase III Prospective Randomized Trial of Dose-Escalated Radiotherapy With or Without Short-Term Androgen Deprivation Therapy for Patients With Intermediate-Risk Prostate Cancer [NCT00936390] | Phase 3 | 1,538 participants (Actual) | Interventional | 2009-09-30 | Active, not recruiting | ||
| A Randomized, Open-Label, Phase 2 Trial Examining the Sequencing of Sipuleucel-T and Androgen Deprivation Therapy in Men With Non-metastatic Prostate Cancer and a Rising Serum Prostate Specific Antigen After Primary Therapy [NCT01431391] | Phase 2 | 68 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Oral Contraceptives Versus Depot-Leuprolide Taken After Surgery for Endometriosis-Associated Pelvic Pain [NCT00229996] | Phase 3 | 194 participants (Anticipated) | Interventional | 2004-07-31 | Completed | ||
| PROGNOSTIC SIGNIFICANCE OF ENDORECTAL MRI IN PREDICTING OUTCOME AFTER COMBINED RADIATION AND ANDROGEN SUPPRESSION FOR PROSTATE CANCER: A PROSPECTIVE PHASE II STUDY [NCT00002889] | Phase 2 | 180 participants (Actual) | Interventional | 1997-05-31 | Completed | ||
| Phase II, Randomized, Open-label, International, Multicenter Study to Compare Efficacy of Standard Chemotherapy vs. Letrozole Plus Abemaciclib as Neoadjuvant Therapy in HR-positive/HER2-negative High/Intermediate Risk Breast Cancer Patients [NCT04293393] | Phase 2 | 200 participants (Actual) | Interventional | 2020-10-02 | Active, not recruiting | ||
| Phase I Trial of Concurrent Taxotere With Radiation Therapy and Hormonal Therapy For Clinically Localized High Risk Prostate Cancer [NCT00099086] | Phase 1 | 20 participants (Actual) | Interventional | 2007-01-16 | Active, not recruiting | ||
| A Phase III Trial of Short Term Androgen Deprivation With Pelvic Lymph Node or Prostate Bed Only Radiotherapy (SPPORT) in Prostate Cancer Patients With a Rising PSA After Radical Prostatectomy [NCT00567580] | Phase 3 | 1,792 participants (Actual) | Interventional | 2008-02-29 | Active, not recruiting | ||
| Analysis of Genetic and Environmental Parameters Influencing Growth Rate of Precocious Puberty Children [NCT00438217] | Phase 4 | 100 participants | Interventional | Recruiting | |||
| Treatment of Endometriosis With Norethindrone Acetate ( NA) VS. Gonadotropin- Releasing Hormone (GnRH) Agonist (Lupron Depot 11.25 mg) [NCT00458458] | Phase 3 | 112 participants (Anticipated) | Interventional | 2004-08-31 | Active, not recruiting | ||
| RecoverPC: A Phase 2 Study of RElugolix Versus GnRH Agonist Quality of Life (QOL) and Testosterone reCOVERy in Men With Prostate Cancer [NCT05765500] | Phase 2 | 110 participants (Anticipated) | Interventional | 2024-01-31 | Not yet recruiting | ||
| Phase II Pilot of Aromatase Inhibitor Therapy With Femara® (Letrozole) and Ovarian Suppression in Premenopausal Estrogen Receptor Positive Women With Stage IV Carcinoma of the Breast [NCT00498901] | Phase 2 | 1 participants (Actual) | Interventional | 2007-02-28 | Terminated | ||
| 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 Phase I Trial for the Evaluation of the Two-way Pharmacokinetic-pharmacodynamic (PD) Interaction of Gender Affirming Exogenous Estrogen (With Testosterone Suppression) on TDF/FTC PrEP in Transgender Women (TGW) [NCT04760691] | Phase 1 | 20 participants (Anticipated) | Interventional | 2021-03-01 | Recruiting | ||
| Extended Endocrine Therapy for Premenopausal Women With Breast Cancer [NCT00903162] | Phase 2 | 17 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| A Randomized Phase II Study of Androgen Deprivation Combined With IMC-A12 Versus Androgen Deprivation Alone for Patients With New Hormone Sensitive Metastatic Prostate Cancer [NCT01120236] | Phase 2 | 211 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| A 12 Month Open Label Study of Serum Testosterone Recovery and PSA After Neo-Adjuvant Treatment With Eligard(TM) 22.5mg Used With Radiation Therapy in Patients With Early Prostate Cancer [NCT01136226] | Phase 4 | 42 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
| A Randomized Prospective Trial of Dual Trigger Ovulation in Oocyte Donors [NCT01443546] | Phase 4 | 26 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to Unable to complete accrual) | ||
| A Six-Month, Open-Label, Crossover Study Of the Maintenance Of Serum Testosterone And PSA Suppression After Switching Between Lupron 22.5 Mg And Eligard 22.5 Mg Or Zoladex 10.8 Mg And Eligard 22.5 Mg In Patients With Advanced Prostate Cancer [NCT00220194] | Phase 4 | 100 participants | Interventional | 2003-04-30 | Completed | ||
| Real World Evidence Study on Metastatic Prostate Cancer Patient Characteristics, Treatment Patterns and Outcomes in the Pirkanmaa Hospital District in Finland [NCT05701007] | 1 participants (Actual) | Observational | 2023-02-13 | Completed | |||
| Phase III Randomized, Placebo-Controlled Clinical Trial Evaluating the Use of Adjuvant Endocrine Therapy +/- One Year of Everolimus in Patients With High-Risk, Hormone Receptor-Positive and HER2/Neu Negative Breast Cancer [NCT01674140] | Phase 3 | 1,939 participants (Actual) | Interventional | 2013-09-12 | Active, not recruiting | ||
| Assisted Reproductive Technology (ART) and Pregnancy Outcomes in Women With Adenomyosis (Internal Endometriosis) According to Stimulation Protocol in Relation to Immunological and Endometrial Features: a Prospective, Randomized Study [NCT05937490] | Phase 4 | 500 participants (Anticipated) | Interventional | 2023-03-27 | Recruiting | ||
| A Phase 2 Open-Label, Randomized, Multi-center Study of Neoadjuvant Abiraterone Acetate (CB7630) Plus Leuprolide Acetate and Prednisone Versus Leuprolide Acetate Alone in Men With Localized High Risk Prostate Cancer [NCT00924469] | Phase 2 | 58 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Ultralong Administration of GnRH-a Before in Vitro Fertilization Improves Fertilization Rate But Not Pregnancy Rate in Women With Endometriosis. A Prospective, Randomized, Controlled Trial. [NCT01269125] | 180 participants (Actual) | Interventional | 2004-05-31 | Completed | |||
| Regulation of Cortisol Metabolism and Fat Patterning [NCT00694733] | 140 participants (Actual) | Interventional | 2005-05-31 | Active, not recruiting | |||
| Exploratory Study of Molecular Profile-Associated Evidence Guided Precision Therapy for Salivary Gland Cancer [NCT05087706] | 182 participants (Anticipated) | Observational [Patient Registry] | 2021-07-30 | Recruiting | |||
| Phase II, Open-label, Single-center Study Evaluating Safety and Activity of Androgen Deprivation Therapy Followed by Chemoimmunotherapy for Newly Metastatic Hormone-sensitive Prostate Cancer (mHSPC) [NCT03951831] | Phase 2 | 20 participants (Anticipated) | Interventional | 2019-05-16 | Active, not recruiting | ||
| Non-comparative, Opened Multicenter Study to Assess the Efficacy and Safety of ELIGARD 22.5mg in the Treatment of Subjects With Prostate Cancer [NCT01511874] | Phase 4 | 42 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Phase I Study Of SU5416 With Androgen Ablation And Radiation In Patients With Intermediate and Advanced Stage Prostate Cancer [NCT00026377] | Phase 1 | 3 participants (Actual) | Interventional | 2001-11-30 | Completed | ||
| A Pilot Study of Pembrolizumab and Exemestane/ Leuprolide in Premenopausal Hormone Receptor Positive/ HER2 Negative Locally Advanced or Metastatic Breast Cancer [NCT02990845] | Phase 1/Phase 2 | 16 participants (Actual) | Interventional | 2017-09-15 | Terminated(stopped due to The enrolment became difficult, as most of the premenopausal women decided to receive ovarian ablation for health insurance reimbursement for CDK4/6 inhibitor for the first-line treatment, making them ineligible for joining the study.) | ||
| Antigonadotropin-Leuprolide in Alzheimer's Disease Drug INvestigation (ALADDIN) [NCT00063310] | Phase 2 | 90 participants | Interventional | 2003-03-31 | Completed | ||
| [NCT00076531] | Phase 3 | 0 participants | Interventional | 2003-12-31 | Completed | ||
| Efficacy and Safety of a New Leuprolide Acetate 3.75 mg Depot Formulation, GP-Pharm S.A., When Given as Palliative Treatment to Prostate Cancer Patients [NCT00128531] | Phase 3 | 120 participants | Interventional | 2005-09-30 | Completed | ||
| A Phase 1, Open Label, Non-Randomized, Dose Escalation Study to Evaluate the Safety of CP-675,206 in Combination With Neoadjuvant Androgen Ablation and a Phase 2, Open Label, Randomized Study to Evaluate the Efficacy of CP-675,206 in Combination With Neoa [NCT00075192] | Phase 1/Phase 2 | 8 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| A Randomized Phase III Study Comparing Androgen Suppression and Elective Pelvic Nodal Irradiation Followed by High Dose 3-D Conformal Boost Versus Androgen Suppression and Elective Pelvic Nodal Irradiation Followed by 125-Iodine Brachytherapy Implant Boos [NCT00175396] | Phase 3 | 400 participants (Anticipated) | Interventional | 2004-05-31 | Active, not recruiting | ||
| Pharmacokinetic, Safety and Efficacy Study of a Six-Month Depot Formulation of Leuprolide in Subjects With Prostatic Carcinoma [NCT00056654] | 164 participants (Actual) | Interventional | 2003-03-31 | Completed | |||
| An Open-Labeled, Singled-Arm Study of the Safety, Efficacy, and Pharmacokinetic Behavior of Leuprolide Mesylate for Injectable Suspension (LMIS 50 mg) in Subjects With Advanced Prostate Carcinoma [NCT02234115] | Phase 3 | 137 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| Phase IV, Non-interventional, Prospective, Open Label, Non Comparative Real Life Data Collection of Depo-Eligard® 7.5 mg, 22.5 mg and 45 mg in Male Prostate Cancer Patients [NCT01793077] | 259 participants (Actual) | Observational | 2011-12-31 | Completed | |||
| A Phase 3, Multi-Center, Open-Label, Trial to Evaluate the Efficacy, Safety and Pharmacokinetics of Two 6-Month Leuprolide Formulations, in Subjects With Prostatic Adenocarcinoma [NCT00626431] | Phase 3 | 310 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| Randomized Trial of Concomitant Hypofractionated IMRT Boost Versus Conventional Fractionated IMRT Boost for Localized High Risk Prostate Cancer [NCT04239599] | 178 participants (Actual) | Interventional | 2011-03-31 | Active, not recruiting | |||
| Do Endometrial Implantation Markers Predict in Vitro Fertilization-embryo Transfer Cycle Outcomes in Endometriosis Patients Pretreated With Leuprolide Acetate in Depot Suspension? [NCT00621179] | Phase 4 | 37 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
| A Phase III, Randomised, Parallel Group, Double-blind, Double-dummy, Active Comparator-controlled, Multicenter Study to Assess the Efficacy and Safety of PGL4001 vs GnRH-agonist for Pre-operative Ttt of Symptomatic Uterine Myomas [NCT00740831] | Phase 3 | 301 participants (Actual) | Interventional | 2008-08-31 | Completed | ||
| A Phase II Study of Bipolar Androgen-based Therapy for Men With Androgen Ablation NaÃ-ve Recurrent Prostate Cancer [NCT01750398] | Phase 2 | 33 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Phase 2 Study of Enzalutamide and GnRH Agonist Before, During and After Radiation Therapy in Treatment of Patients With High-risk Localized Prostate Cancer [NCT02064582] | Phase 2 | 7 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Phase II Trial of Definitive Radiotherapy With Leuprolide and Enzalutamide in High Risk Prostate Cancer [NCT02508636] | Phase 2 | 11 participants (Actual) | Interventional | 2015-12-22 | Terminated(stopped due to Low Accrual) | ||
| Short Versus Long-term Androgen Deprivation Therapy Combined With Salvage Radiotherapy in Prostate Cancer Patients With Biochemical Recurrence After Prostatectomy: a Multicentre Phase III Randomised Controlled Trial [NCT05781217] | Phase 3 | 534 participants (Anticipated) | Interventional | 2023-03-14 | Recruiting | ||
| 20-347 NCT Number Title A Single Arm Phase II Study of ADjuvant Endocrine Therapy, Pertuzumab, and Trastuzumab for Patients With Anatomic Stage I Hormone Receptor-positive, HER2-positive Breast Cancer (ADEPT) [NCT04569747] | Phase 2 | 375 participants (Anticipated) | Interventional | 2021-01-11 | Recruiting | ||
| A Prospective, Randomized, Multicenter, Open-label Comparison of Pre-surgical Combination of Trastuzumab and Pertuzumab With Concurrent Taxane Chemotherapy or Endocrine Therapy Given for Twelve Weeks With a Quality of Life Assessment of Trastuzumab, Pertu [NCT03272477] | Phase 2 | 257 participants (Actual) | Interventional | 2017-10-05 | Active, not recruiting | ||
| Phase I/II Study of Weekly Intravenous Estramustine Phosphate in Combination With Paclitaxel and Carboplatin in Patients With Advanced Prostate Cancer [NCT00003394] | Phase 1/Phase 2 | 18 participants (Anticipated) | Interventional | 1998-04-30 | Completed | ||
| Study of Leuprolide in Adults With Hypogonadotropism [NCT00004438] | 45 participants (Anticipated) | Interventional | 1997-09-30 | Completed | |||
| Impact of Experimentally Induced Hot Flashes on Sleep and Mood Disturbance [NCT01116401] | Phase 4 | 29 participants (Actual) | Interventional | 2009-11-03 | Completed | ||
| The Phase 4 Clinical Trial to Evaluate the Efficacy and Safety of Luphere Depot Inj. 3.75mg(Leuprolide Acetate 3.75mg) in Patients With Precocious Puberty; A Single, Open, Multi-center, Prospective Study [NCT01634321] | Phase 4 | 63 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
| Effect of GnRH Antagonist Protocol vs Agonist Long Protocol During Controlled Hyperstimulation (COH)for Assisted Reproduction on IVF Outcome, Peak Estradiol Level, and Duration of Stimulation. [NCT01669291] | 43 participants (Actual) | Interventional | 2012-07-31 | Completed | |||
| An Open-label Dose-finding Study to Evaluate the Pharmacodynamic (PD) Profiles and Efficacy of Different Dosing Regimens of Leuprolide Oral Tablets (Ovarest®) in Women With Endometriosis [NCT05096065] | Phase 2 | 16 participants (Anticipated) | Interventional | 2022-03-18 | Recruiting | ||
| A Multi-Center, Randomized, Assessor-Blind, Controlled Trial Comparing the Occurrence of Major Adverse Cardiovascular Events (MACEs) in Patients With Prostate Cancer and Cardiovascular Disease Receiving Degarelix (Gonadotropin-Releasing Hormone (GnRH) Rec [NCT02663908] | Phase 3 | 545 participants (Actual) | Interventional | 2016-04-19 | Terminated(stopped due to Recruitment rate; a lower than anticipated observed cardiovascular event rate. The Sponsor decision to stop the trial was not based on any safety concerns or any knowledge of the results, or influenced by issues imposed by the COVID-19 pandemic.) | ||
| Ulipristal Acetate Versus GnRH Analogue for Myometrial Preservation in Patients With Submucosal Uterine Leiomyoma G2 [NCT02357563] | Phase 4 | 110 participants (Anticipated) | Interventional | 2015-02-28 | Recruiting | ||
| Gonadal Steroid Regulation of the Natriuretic Peptide System [NCT01763541] | Early Phase 1 | 0 participants (Actual) | Interventional | 2014-06-30 | Withdrawn | ||
| A Randomized, Double-blind, Placebo-controlled, Phase 2 Study to Assess the Efficacy, Safety, and Dose-Response Relationship of ASP1707 in Subjects With Endometriosis Associated Pelvic Pain for 12 Weeks, Followed by a 12-Week Double-blind Extension Withou [NCT01767090] | Phase 2 | 912 participants (Actual) | Interventional | 2012-12-04 | Completed | ||
| A Phase 3, Multi-center, Randomized, Open-label, Parallel-group, Comparative Study of TAP-144-SR (3M) to Evaluate Hormone Dynamics, Pharmacokinetics, Safety and Efficacy of TAP-144-SR (6M) 22.5 mg Subcutaneous Injection for 48 Weeks in Prostate Cancer Pat [NCT01546623] | Phase 3 | 160 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| A Randomized, Open-label, Single-dosing, 2x2 Crossover Phase 1 Study to Compare the Safety and Pharmacokinetics of PT105 With PT105R in Healthy Postmenopausal Female Volunteers [NCT04783636] | Phase 1 | 40 participants (Anticipated) | Interventional | 2021-03-11 | Not yet recruiting | ||
| Efficacy and Safety of a New Leuprolide Acetate 22.5 mg Depot Formulation in the Treatment of Prostate Cancer [NCT01415960] | Phase 3 | 163 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Identification of the Menstrual Cycle-Associated Factors That Modulate Circulating Lipid Levels in Premenopausal Women [NCT01546454] | 5 participants (Actual) | Interventional | 2012-02-29 | Completed | |||
| Feasibility of Cytoreductive Prostatectomy in Men Newly Diagnosed With Metastatic Prostate Cancer [NCT02458716] | Phase 1 | 26 participants (Actual) | Interventional | 2015-03-06 | Completed | ||
| Advantages of Ulipristal Acetate for the Preoperative Treatment of Hypoechoic Cellular Leiomyomas [NCT02361905] | Phase 4 | 42 participants (Anticipated) | Interventional | 2015-02-28 | Recruiting | ||
| An Open-Label, Single-Arm Study of The Efficacy, Safety, and Pharmacokinetic Behavior of Leuprolide Mesylate Injectable Suspension (LMIS 25 mg) in Subjects With Prostate Cancer [NCT03261999] | Phase 3 | 144 participants (Actual) | Interventional | 2017-09-26 | Completed | ||
| Salvage Therapeutic Radiation With Enzalutamide and ADT in Men With Recurrent Prostate Cancer (STREAM) [NCT02057939] | Phase 2 | 38 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| Phase I/II Study of Sorafenib Concurrent With Androgen Deprivation and Radiotherapy in the Treatment of Intermediate- and High-Risk Localized Prostate Cancer [NCT00924807] | Phase 1/Phase 2 | 4 participants (Actual) | Interventional | 2008-09-30 | Terminated(stopped due to Sponsor closed the trial) | ||
| A Phase 3, Multicenter, Open-Label, Two-Part Study to Evaluate the Safety, Efficacy, Pharmacokinetics, and Pharmacodynamics of Leuprolide Acetate 45 mg 6-Month Depot Formulation in Children With Central Precocious Puberty (CPP) [NCT03695237] | Phase 3 | 45 participants (Actual) | Interventional | 2018-10-24 | Completed | ||
| THE EFFICACY OF PREOPERATIVE USAGE OF GONADOTROPINE-RELEASING HORMONE AGONIST IN PATIENTS UNDERGOING TOTAL LAPAROSCOPIC HYSTERECTOMY DUE TO UTERIN FIBROIDS [NCT04192812] | 100 participants (Anticipated) | Interventional | 2020-12-30 | Not yet recruiting | |||
| ARN-509+Abiraterone Acetate+Leuprolide With Stereotactic, Ultra-Hypofractionated Radiation (AASUR) in Very High Risk Prostate Cancer: A Single Arm, Phase II Study [NCT02772588] | Phase 2 | 64 participants (Actual) | Interventional | 2016-05-31 | Active, not recruiting | ||
| Phase III Randomised Trial to Evaluate the Benefit of Adjuvant Hormonal Treatment With Leuprorelin Acetate (Eligard® 45 mg) for 24 Months After Radical Prostatectomy in Patients With High Risk of Recurrence. [NCT01442246] | Phase 3 | 700 participants (Anticipated) | Interventional | 2011-07-31 | Active, not recruiting | ||
| A Randomized Phase II Study of Androgen Deprivation Therapy With or Without Palbociclib in RB-Positive Metastatic Hormone-Sensitive Prostate Cancer [NCT02059213] | Phase 2 | 72 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
| Prediction of the PRONOUNCE Prostate Cancer Trial in Healthcare Claims Data [NCT04897958] | 14,417 participants (Actual) | Observational | 2019-09-21 | Completed | |||
| A Phase 2 Multicohort Study of Nivolumab in Combination With Docetaxel and Androgen Deprivation Therapy in Metastatic Hormone Sensitive Prostate Cancer Patients With DNA Damage Repair Defects or Inflamed Tumors [NCT04126070] | Phase 2 | 60 participants (Anticipated) | Interventional | 2020-05-11 | Recruiting | ||
| Multi-institutional Study to Increase Breast Conserving Surgery (BCS) Rate With Personalized Neoadjuvant Strategy in ER Positive and HER2 Negative Breast Cancer Patients for Whom BCS is Not Feasible [NCT03900637] | Phase 2 | 122 participants (Anticipated) | Interventional | 2019-11-08 | Active, not recruiting | ||
| DETECT V / CHEVENDO A Multicenter, Randomized Phase III Study to Compare Chemo- Versus Endocrine Therapy in Combination With Dual HER2-targeted Therapy of Herceptin® (Trastuzumab) and Perjeta® (Pertuzumab) Plus Kisqali® (Ribociclib) in Patients With HER2 [NCT02344472] | Phase 3 | 270 participants (Anticipated) | Interventional | 2015-09-30 | Recruiting | ||
| A Phase II, Open Label, Active Control, Multi-National, Multi-Centre, Randomized, Parallel Group Study Assessing Pharmacokinetics, Pharmacodynamics, Efficacy and Safety of CAM2032 (Leuprolide Acetate FluidCrystal® Injection Depot Once Monthly) After Repea [NCT02212197] | Phase 2 | 51 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| Androgen Deprivation Therapy for Oligo-recurrent Prostate Cancer in Addition to radioTherapy [NCT04302454] | Phase 3 | 280 participants (Anticipated) | Interventional | 2020-03-19 | Recruiting | ||
| Phase II Trial of Maximal Androgen Deprivation Followed by Conformal External Beam Radiotherapy With Continued Androgen Deprivation for Clinically Localized Prostate Cancer [NCT00003124] | Phase 2 | 105 participants (Anticipated) | Interventional | 1997-05-31 | Completed | ||
| Systemic and Tumor-Directed Therapy for Oligometastatic Prostate Cancer [NCT03298087] | Phase 2 | 28 participants (Actual) | Interventional | 2018-07-01 | Active, not recruiting | ||
| Study of Gonadotropin Releasing Hormone Agonist Test Using Leuprolide Acetate in Patients With Gonadotropin Deficiency [NCT00004426] | 90 participants (Anticipated) | Interventional | 1994-08-31 | Completed | |||
| Insulin Resistance and Testosterone in Non-Diabetic Postmenopausal Women [NCT00123110] | Phase 2 | 35 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
| Randomized Phase II Screening Trial of Enzalutamide/MDV-3100 and LHRH Analogue vs Combined Androgen Deprivation (LHRH Analogue + Bicalutamide) in Metastatic Hormone Sensitive Prostate Cancer [NCT02058706] | Phase 2 | 71 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Efficacy and Safety of a New Leuprolide Acetate 17 mg Depot Formulation, GP-Pharm S.A., When Given as Palliative Treatment to Prostate Cancer Patients [NCT00630799] | Phase 3 | 20 participants (Actual) | Interventional | 2008-05-31 | Terminated | ||
| A Phase II, Multicenter, Long-term Extension Study to Compare the Safety and Efficacy of TAK-385 (10, 20, and 40 mg) Following Oral Administration for 12 Weeks or More in the Treatment of Endometriosis [NCT01452685] | Phase 2 | 397 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| A Phase II, Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Study of the Efficacy and Safety of TAK-385 10, 20, and 40 mg (p.o.) in the Treatment of Endometriosis [NCT01458301] | Phase 2 | 487 participants (Actual) | Interventional | 2011-10-31 | Completed | ||
| A Randomized Controlled Study to Evaluate the Efficacy and Safety of Endocrine Therapy Plus Chemotherapy Versus Chemotherapy Alone as the Neoadjuvant Therapy in the Treatment of ER-positive, HER2-negative Breast Cancer (IIa-IIIc) [NCT02980965] | Phase 3 | 249 participants (Actual) | Interventional | 2013-05-31 | Completed | ||
| Phase II Study Of Neo-Adjuvant Paclitaxel, Estramustine And Carboplatin (TEC) Plus Androgen Ablation Prior To Radiation Therapy In Patients With Poor Prognosis Localized Prostate Cancer [NCT00016913] | Phase 2 | 34 participants (Actual) | Interventional | 2001-05-31 | Completed | ||
| A Prospective Study of Intermittent Androgen Suppression (IAS) in Men With Localized Prostate Cancer Who Have Biochemical Relapse After Radiation Therapy or Radical Prostatectomy [NCT00223665] | Phase 2 | 102 participants (Actual) | Interventional | 1997-01-08 | Completed | ||
| A Multidisciplinary Team-Based Approach to Mitigate the Impact of Androgen Deprivation Therapy in Prostate Cancer: A Randomized Phase 2 [NCT02168062] | Phase 2 | 57 participants (Actual) | Interventional | 2014-06-16 | Terminated(stopped due to Funding) | ||
| Analysis of Body Mass Index in Central Precocious Puberty(CPP) Patients Treated With Leuprolide Acetate [NCT02974270] | Phase 4 | 100 participants (Anticipated) | Interventional | 2016-06-30 | Recruiting | ||
| A GnRH Agonist IN Pre-menopausal Women STudy to Treat Severe Polycystic Liver Disease [NCT05478083] | Phase 2 | 36 participants (Anticipated) | Interventional | 2022-06-01 | Recruiting | ||
| Role of Suppression of Endometriosis With Progestins Before IVF-ET: a Non-inferiority Randomized Controlled Trial [NCT04500743] | 134 participants (Actual) | Interventional | 2018-08-01 | Completed | |||
| Adjuvant Ovarian Suppression Plus Aromatase Inhibitor or Tamoxifen for Hormone Receptor-Positive Breast Cancer in Women Younger Than 35: A Multicenter Randomized Clinical Trial [NCT02914158] | Phase 3 | 680 participants (Anticipated) | Interventional | 2016-03-30 | Recruiting | ||
| A Phase II Study of Definitive Therapy for Newly Diagnosed Men With Oligometastatic Prostate Cancer [NCT02716974] | Phase 2 | 26 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
| Bevacizumab Plus Paclitaxel Optimization Study With Interventional Maintenance Endocrine Therapy in Advanced or Metastatic ER-positive HER2-negative Breast Cancer -BOOSTER Trial, a Multicenter Randomized Phase II Study- [NCT01989780] | Phase 2 | 160 participants (Actual) | Interventional | 2014-01-31 | Completed | ||
| A Randomized Phase III Study of Neo-Adjuvant Docetaxel and Androgen Deprivation Prior to Radical Prostatectomy Versus Immediate Radical Prostatectomy in Patients With High-Risk, Clinically Localized Prostate Cancer [NCT00430183] | Phase 3 | 788 participants (Actual) | Interventional | 2007-05-08 | Active, not recruiting | ||
| A Phase I/II Study of Concurrent Weekly Docetaxel (Taxotere®), Androgen Ablation, and Adaptive External Beam Radiotherapy for Localized High-Risk Adenocarcinoma of the Prostate [NCT00225420] | Phase 1/Phase 2 | 23 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
| GnRH-a for Ovarian Protection During CYC Therapy for Rheumatic Diseases [NCT01257802] | Phase 3 | 14 participants (Actual) | Interventional | 2011-05-31 | Terminated | ||
| A Phase 2, Randomized, Open-label, Parallel Group Study to Evaluate the Safety and Efficacy of the Oral GnRH Antagonist TAK-385, Together With a Leuprorelin Observational Cohort, in Patients With Prostate Cancer [NCT02083185] | Phase 2 | 136 participants (Actual) | Interventional | 2014-03-26 | Completed | ||
| UKCCCR RANDOMISED TRIAL OF ADJUVANT ENDOCRINE THERAPY AND CHEMOTHERAPY IN WOMEN WITH EARLY BREAST CANCER, THE ADJUVANT BREAST CANCER (ABC) TRIAL [NCT00002582] | Phase 3 | 6,000 participants (Anticipated) | Interventional | 1993-06-30 | Completed | ||
| An Open Label, Randomized, Phase III Study, Evaluating the Efficacy of a Combination of Apalutamide With Radiotherapy and LHRH Agonist in High-risk Postprostatectomy Biochemically Relapsed Prostate Cancer Patients [NCT04181203] | Phase 3 | 490 participants (Anticipated) | Interventional | 2020-01-09 | Recruiting | ||
| [NCT00004436] | 30 participants | Interventional | 1993-07-31 | Completed | |||
| "Leuprorelin Acetate SR 11.25 mg Injection Kit Specified Drug-use Survey Long-term Use Survey in Prostate Cancer Patients (96 Weeks)" [NCT02167893] | 11,288 participants (Actual) | Observational | 2005-10-31 | Completed | |||
| Phase II Study of Antineoplastons A10 and AS2-1 Capsules With Total Androgen Blockade in Patients With Stage III or IV Adenocarcinoma of the Prostate [NCT00003517] | Phase 2 | 0 participants (Actual) | Interventional | Withdrawn | |||
| [NCT00004771] | Phase 2 | 40 participants | Interventional | 1992-10-31 | Completed | ||
| An Open-Label, Multicenter, Phase III Study to Assess the Impact of Transient Androgenic Deprivation With Enantone LP 11.25 Mg (Leuprorelin) on the Histological Progression of Indolent Prostate Cancer [NCT02085252] | Phase 3 | 116 participants (Actual) | Interventional | 2013-06-03 | Completed | ||
| A Prospective Comparison of Transcriptional Profiling of Luteal Phase Endometrial Biopsies After Induction of Oocyte Maturation With a Gonadotropin Releasing Hormone (GnRH) Agonist or Human Chorionic Gonadotropins (hCG) [NCT01606709] | Phase 4 | 7 participants (Actual) | Interventional | 2012-04-30 | Terminated(stopped due to Difficult to recruit patients) | ||
| Phase III Randomized Trial Comparing Total Androgen Blockade Versus Total Androgen Blockade Plus Pelvic Irradiation in Clinical Stage T3-4, N0, M0 Adenocarcinoma of the Prostate [NCT00002633] | Phase 3 | 361 participants (Actual) | Interventional | 1995-02-08 | Completed | ||
| An Open-label, Single Arm, Multicenter Study on the Efficacy, Safety, and Pharmacokinetics of Leuprolide Acetate 45 mg for Injectable Suspension Controlled Release in Subjects With Central (Gonadotropin-Dependent) Precocious Puberty [NCT02452931] | Phase 3 | 64 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
| A Randomized Phase II Study Of Bone-Targeted Therapy In Advanced Androgen-Dependent Prostate Cancer [NCT00081159] | Phase 2 | 80 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
| An Open Label, Randomized, Single Dose, Parallel-group, Phase 1 Study to Evaluate the Pharmacokinetics and Safety Following Subcutaneous Administration of DWJ108J in Patients With Prostate Cancer [NCT03029533] | Phase 1 | 44 participants (Anticipated) | Interventional | 2017-02-28 | Not yet recruiting | ||
| A Multi-Center Trial of Androgen Suppression With Abiraterone aCetate, LEuprolide, PARP Inhibition and Stereotactic Body Radiotherapy (ASCLEPIuS): A Phase I/2 Trial in High Risk and Node Positive Prostate Cancer [NCT04194554] | Phase 1/Phase 2 | 100 participants (Anticipated) | Interventional | 2020-11-06 | Recruiting | ||
| A Phase II Study of Definitive Therapy for Newly Diagnosed Men With Oligometastatic Prostate Cancer After Prostatectomy [NCT03043807] | Phase 2 | 26 participants (Actual) | Interventional | 2017-02-22 | Completed | ||
| A Phase 2 Study of Docetaxel Plus Apalutamide in Castration-Resistant Prostate Cancer Patients Post Abiraterone Acetate [NCT03093272] | Phase 2 | 9 participants (Actual) | Interventional | 2017-06-23 | Terminated(stopped due to Safety concerns) | ||
| A Randomized Phase Ib/II Study of Preoperative GDC-0449 and Androgen Ablation Compared to Androgen Ablation Alone Followed by Radical Prostatectomy for Select Patients With Locally Advanced Adenocarcinoma of the Prostate [NCT01163084] | Phase 1/Phase 2 | 10 participants (Actual) | Interventional | 2010-07-09 | Terminated | ||
| [NCT01546649] | Phase 3 | 167 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
| Neoadjuvant Chemohormonal Therapy Followed by Salvage Surgery for High Risk PSA Failure With Biopsy Proven Local Recurrence After Initial Definitive Radiotherapy [NCT01531205] | Phase 2 | 2 participants (Actual) | Interventional | 2012-05-31 | Terminated(stopped due to low accrual) | ||
| 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 | ||
| Ovarian Hormones, Reward Response, and Binge Eating in Bulimia Nervosa: An Experimental Design [NCT04225221] | Phase 2 | 10 participants (Actual) | Interventional | 2020-02-24 | Completed | ||
| PHASE III TRIAL OF ORCHIECTOMY/LHRH ANALOG + FLUTAMIDE + SURAMIN + HYDROCORTISONE VS ORCHIECTOMY/LHRH ANALOG + FLUTAMIDE IN PATIENTS WITH METASTATIC PROSTATE CANCER [NCT00002881] | Phase 3 | 0 participants | Interventional | 1996-10-31 | Completed | ||
| A Randomized, Double-blind, Double-dummy, Parallel- Group, Multi-center Phase IIb Study to Assess the Efficacy and Safety of Different Dose Combinations of an Aromatase Inhibitor and a Progestin in an Intravaginal Ring Versus Placebo and Leuprorelin / Leu [NCT02203331] | Phase 2 | 319 participants (Actual) | Interventional | 2014-10-16 | Completed | ||
| Phase III Randomized Trial of Standard Systemic Therapy (SST) Versus Standard Systemic Therapy Plus Definitive Treatment (Surgery or Radiation) of the Primary Tumor in Metastatic Prostate Cancer [NCT03678025] | Phase 3 | 1,273 participants (Anticipated) | Interventional | 2018-09-24 | Recruiting | ||
| A Phase III Double Blinded Study of Early Intervention After RADICAl ProstaTEctomy With Androgen Deprivation Therapy With or Without Darolutamide vs. Placebo in Men at Highest Risk of Prostate Cancer Metastasis by Genomic Stratification (ERADICATE) [NCT04484818] | Phase 3 | 27 participants (Actual) | Interventional | 2021-03-01 | Active, not recruiting | ||
| Phase II, Open Label, Dose Finding Study of the Effect of GTx-758 on Total and Free Testosterone Levels in Men With Prostate Cancer Compared to a Luteinizing Hormone Releasing Hormone Agonist [NCT01326312] | Phase 2 | 159 participants (Actual) | Interventional | 2011-06-30 | Terminated(stopped due to FDA Clinical Hold) | ||
| A Phase 3, Randomized, Multi-Center, Open-Label Study to Evaluate the Efficacy and Safety of Leuprolide Acetate 11.25 and 30 mg Formulations in Children With Central Precocious Puberty [NCT00635817] | Phase 3 | 84 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Randomized Crossover Trial to Assess the Tolerability of GnRH Analogue Administration in Patients With Advanced Prostate Cancer [NCT01161563] | Phase 4 | 118 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Randomised Phase II Study of Neoadjuvant TAK-700 and Leuprorelin Acetate Followed by Surgery Versus Surgery Alone in Intermediate and High Risk Clinically Localized Prostate Cancer [NCT03211052] | Phase 2 | 16 participants (Actual) | Interventional | 2013-02-18 | Terminated(stopped due to IMP no longer available) | ||
| Phase 2 Trial Pembrolizumab or Pembrolizumab in Combination With Intratumoral SD-101 Therapy in Patients With Hormone-Naïve Oligometastatic Prostate Cancer Receiving Stereotactic Body Radiation Therapy and Intermittent Androgen Deprivation Therapy [NCT03007732] | Phase 2 | 23 participants (Actual) | Interventional | 2017-05-17 | Active, not recruiting | ||
| "Leuplin SR 11.25 mg Injection Kit Specified Drug-use Survey: QOL Survey in Premenopausal Breast Cancer Patients" [NCT02134977] | 2,816 participants (Actual) | Observational | 2011-09-30 | Completed | |||
| Phase II Randomized Study Of Neoadjuvant And Adjuvant Abiraterone Acetate + Apalutamide For Intermediate-High Risk Prostate Cancer Undergoing Prostatectomy [NCT02903368] | Phase 2 | 118 participants (Actual) | Interventional | 2016-10-19 | Active, not recruiting | ||
| Randomized Trial of External Beam Radiation With or Without Short-Course Hormonal Therapy in Intermediate Risk Prostate Cancer Patients [NCT00388804] | Phase 3 | 39 participants (Actual) | Interventional | 2005-02-28 | Terminated(stopped due to Slow accrual.) | ||
| A Phase II Study of Ipilimumab PLUS Androgen Depravation Therapy in Castrate Sensitive Prostate Carcinoma [NCT01377389] | Phase 2 | 30 participants (Actual) | Interventional | 2011-06-17 | Terminated(stopped due to Due to adverse events) | ||
| A Neoadjuvant Phase IIa Study of Ipilimumab {Formerly Known as MDX-010 (BMS-734016)} Plus Hormone Ablation in Men With Prostate Cancer Followed by Radical Prostatectomy. [NCT01194271] | Phase 2 | 19 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Multicenter, Open, Prospective Study to Evaluate the Safety and Efficacy of Leuprorelin Acetate DPS (Leuplin DPS) Treatment Quarterly in Patients With Central Precocious Puberty [NCT03316482] | Phase 4 | 58 participants (Actual) | Interventional | 2015-06-11 | Completed | ||
| STEEL: A Randomized Phase II Trial of Salvage Radiotherapy With Standard vs Enhanced Androgen Deprivation Therapy (With Enzalutamide) in Patients With Post-Prostatectomy PSA Recurrences With Aggressive Disease Features [NCT03809000] | Phase 2 | 188 participants (Actual) | Interventional | 2019-04-15 | Active, not recruiting | ||
| PRospective, Multicenter Study to Evaluate Safety and Efficacy of Switching Treatments of Prostate Cancer Patients, Initially on Use of Monthly or Quarterly Goserelin Acetate (Zoladex®), to Semiannually Leuprorelin Acetate (Eligard®) [NCT05304169] | Phase 4 | 48 participants (Actual) | Interventional | 2017-11-14 | Completed | ||
| Phase Ib Trial of Enzalutamide in Combination With Radiation Therapy and LHRH Agonist Therapy in the Management of Intermediate and High-Risk Prostate Cancer [NCT02023463] | Phase 1 | 25 participants (Actual) | Interventional | 2014-04-02 | Active, not recruiting | ||
| The Relation of GnRH Treatment to QTc Interval in Transgender Female Youth: A Time Series Study [NCT03078829] | 3 participants (Actual) | Observational | 2017-05-01 | Terminated(stopped due to investigator has left UCSF) | |||
| The Treatment of Menstrually-Related Mood Disorders With the Gonadotropin Releasing Hormone (GnRH) Agonist, Depot Leuprolide Acetate (Lupron) [NCT00001259] | Phase 1 | 60 participants (Actual) | Interventional | 1992-08-11 | Completed | ||
| [NCT00004763] | Phase 2 | 45 participants | Interventional | 1993-01-31 | Completed | ||
| A Phase III Randomized Trial Comparing Intermittent Versus Continuous Androgen Suppression for Patients With Prostate-Specific-Antigen Progression in the Clinical Absence of Distant Metastases Following Radiotherapy for Prostate Cancer [NCT00003653] | Phase 3 | 1,386 participants (Actual) | Interventional | 1999-01-05 | Completed | ||
| Mechanism and Predictors of Cardiotoxicity After Prostate Cancer Treatment: A Parallel Cohort and Randomized Trial Comparing Radiation Alone, Radiation Plus Leuprolide, and Radiation Plus Relugolix [NCT05320406] | Phase 4 | 94 participants (Anticipated) | Interventional | 2022-06-06 | Recruiting | ||
| A Randomized, Single-blinded, Parallel Design Phase I Clinical Trial to Investigate the Safety and Pharmacokinetics/Pharmacodynamics of CKD-841 A-1, CKD-841 D or Leuplin Inj. After Subcutaneous Injection in Postmenopausal Female [NCT04840745] | Phase 1 | 32 participants (Anticipated) | Interventional | 2021-04-30 | Not yet recruiting | ||
| Whole-Pelvic Radiotherapy With a Stereotactic Body Radiotherapy Boost and Long-Term Androgen Deprivation for Unfavorable-Intermediate and High Risk Localized Adenocarcinoma of the Prostate. [NCT02064036] | Phase 1 | 17 participants (Actual) | Interventional | 2013-06-06 | Completed | ||
| Bioenergetic and Metabolic Consequences of the Loss of Ovarian Function in Women [NCT01712230] | 47 participants (Actual) | Interventional | 2012-10-31 | Completed | |||
| Maximal Stimulation and Delayed Fertilization for Diminished Ovarian Reserve: a Randomized Pilot Study [NCT01921166] | Phase 4 | 23 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| Neurophysiology of Postpartum Depression in an Experimental Model of Pregnancy and Parturition [NCT01762943] | 36 participants (Actual) | Interventional | 2013-08-31 | Completed | |||
| A Multi-institutional Phase I and Biomarker Study of Everolimus Added to Combined Hormonal and Radiation Therapy for High Risk Prostate Cancer [NCT01642732] | Phase 1 | 1 participants (Actual) | Interventional | 2012-10-31 | Terminated(stopped due to Lack of accrual and funding expires in June, 2014.) | ||
| A Multicenter, Randomized, Double-Blind, Parallel-Group, Phase 3 Study to Evaluate the Efficacy and Safety of Oral TAK-385 40 mg Compared With Leuprorelin in the Treatment of Uterine Fibroids [NCT02655237] | Phase 3 | 281 participants (Actual) | Interventional | 2016-03-05 | Completed | ||
| QoL and Treatment Compliance for Pre-menopausal Patients With HR+ Breast Cancer Using GnRHa as Ovarian Function Suppression(OFS) Treatment in the Chinese Population: a Real-world Observational Investigation [NCT05122377] | 500 participants (Anticipated) | Observational | 2021-11-30 | Not yet recruiting | |||
| Docetaxel With Rapid Hormonal Cycling as a Treatment for Patients With Prostate Cancer [NCT00587431] | Phase 2 | 102 participants (Actual) | Interventional | 2003-07-31 | Completed | ||
| Characterizing the Neural Substrates of Irritability in Women: an Experimental Neuroendocrine Model [NCT04051320] | Phase 2 | 23 participants (Actual) | Interventional | 2020-01-02 | Completed | ||
| A Phase II Immunotherapeutic Trial: Combination Androgen Ablative Therapy and CTLA-4 Blockade as a Treatment for Advanced Prostate Cancer [NCT00170157] | Phase 2 | 112 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
| Endometrial Receptivity Profile in Patients With Endometrial Proliferation Defects [NCT02406690] | 1 participants (Actual) | Observational | 2015-07-31 | Completed | |||
| Comparison of the Therapeutic Effects of Vaginal Repair With Leuprorelin and Vaginal Repair in the Treatment of Cesarean Section Scar Defect [NCT05206682] | 94 participants (Anticipated) | Interventional | 2023-05-01 | Not yet recruiting | |||
| "Leuplin SR 11.25 mg for Injection Specified Drug-use Survey Long-term Use Survey on Premenopausal Breast Cancer Patients (96 Weeks)" [NCT02154139] | 651 participants (Actual) | Observational | 2005-12-31 | Completed | |||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
"The Beck Depression Inventory (BDI) is a 21-item, self-report rating inventory that measures the severity of symptoms accompanying depression. Each item has a minimum score of 0 and a maximum score of 3, with higher numbers consistent with more severe symptoms. The score of each item is summed to amount the overall BDI score, with a minimum score of 0 and a maximum score of 63. Higher BDI scores are consistent with more severe depression. Score of 16 or greater is consistent with clinical depression.~Each participant completed the BDI every 2 weeks during each of the study phases throughout the 6-month study. Outcome measures reported consist of the average of two BDI scores from each phase of the study: the last 4 weeks of the GnRH agonist alone; weeks 6 and 8 of placebo alone; during the 4-week long estradiol phase (weeks 2 and 4 of estradiol) and the 4-week long progesterone phase (weeks 2 and 4 of progesterone)." (NCT00001259)
Timeframe: Placebo: Weeks 6 and 8 of Placebo; Lupron only: Weeks 6 and 8 or 10 and 12; Estradiol or progesterone: Weeks 2 and 4
| Intervention | score on a scale (Mean) |
|---|---|
| Placebo | 2.6 |
| GnRH Agonist Injections (Lupron-L Only) | 3.0 |
| Estradiol | 5.3 |
| Progesterone | 3.6 |
"The Beck Depression Inventory (BDI) is a 21-item, self-report rating inventory that measures the severity of symptoms accompanying depression. Each item has a minimum score of 0 and a maximum score of 3, with higher numbers consistent with more severe symptoms. The score of each item is summed to amount the overall BDI score, with a minimum score of 0 and a maximum score of 63. Higher BDI scores are consistent with more severe depression. Score of 16 or greater is consistent with clinical depression.~Each participant completed the BDI every 2 weeks during each of the study phases (i.e., GnRH agonist alone, estradiol and progesterone) throughout the 6-month study. Outcome measures reported consist of the average of two BDI scores from each phase of the study: the last 4 weeks of the GnRH agonist alone (phase 1), during the 4-week long estradiol phase (phase 2: weeks 2 and 4 of estradiol) and the 4-week long progesterone phase (phase 2: weeks 2 and 4 of progesterone)." (NCT00001322)
Timeframe: Phase 1: Weeks 6 and 8 or 10 and 12; Phase 2: Weeks 2 and 4 of estradiol or progesterone
| Intervention | Units on a scale (Mean) |
|---|---|
| Phase 1 - Lupron | 1.4 |
| Phase 2 - Estradiol | 1 |
| Phase 2 - Progesterone | 1.1 |
Disease-specific failure is defined as death certified as due to prostate cancer (by central review), death due to complications of treatment (irrespective of malignancy status), death from unknown causes with active malignancy, or death from unknown causes with previously documented relapse (either clinical or biochemical). Survival rates were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 95.7 |
| Radiation Therapy Alone | 92.6 |
Failure is defined as documented metastatic disease. Failure rates were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 5.5 |
| Radiation Therapy Alone | 8.0 |
The Phoenix definition of biochemical failure was used - an increase in the prostate-specific antigen (PSA) level of >2 ng per milliliter above the nadir. Failure rates were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 26.3 |
| Radiation Therapy Alone | 41.1 |
Clinical relapse is defined as local progression or distant metastases. Failure rates were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 15.0 |
| Radiation Therapy Alone | 21.7 |
Disease-free failure is defined as documentation of progression (local progression, distant failure, and biochemical failure) or death from any cause. Disease-free survival rates were estimated by the Kaplan-Meier method. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 51.7 |
| Radiation Therapy Alone | 39.5 |
Local progression defined as documented local progression as determined by clinical exam . Failure rates were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 10.9 |
| Radiation Therapy Alone | 16.1 |
Overall survival (OS) was calculated from randomization to the date of death from any cause and overall survival rates were estimated by the Kaplan-Meier method. (NCT00002597)
Timeframe: From date of randomization to 10 years
| Intervention | percentage of patients (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 61.9 |
| Radiation Therapy Alone | 56.8 |
The rate of prostate rebiopsy at two years is defined as the proportion of patients whose results are positive among all eligible patients who had a repeat biopsy at two years. The rate was estimated separately in each arm. (NCT00002597)
Timeframe: From registration to two years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 20.2 |
| Radiation Therapy Alone | 38.9 |
Second biochemical relapse is as defined as follows (after initiation of salvage hormone therapy): A rise in PSA on at least two consecutive cases above the nadir (after initiation of salvage hormone therapy), with the rises in PSA exceeding 1 ng/ml above the nadir; or failure to reach 4 ng/L or less at 18 months. The rates of second biochemical relapse were estimated by means of cumulative incidence functions. (NCT00002597)
Timeframe: From registration to 10 years
| Intervention | percentage of participants (Number) |
|---|---|
| Hormone Therapy + Radiation Therapy | 2.7 |
| Radiation Therapy Alone | 6.1 |
To determine the impact of one year of total androgen ablation on quality of life mentally, physically and sexual function. The following questionnaires were completed by patients in the clinic setting and used to assess HRQoL: Medical Outcomes Study 36-Item Short Form (SF-36) and University of California-Los Angeles Sexual Function Scale (UCLA-SFS). To score the SF-36, scales are standardized with a scoring algorithm or by the SF-36v2 scoring software to obtain a score ranging from 0 to 100. Higher scores indicate better quality of life. (NCT00003645)
Timeframe: 1 year
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Mental | Physical | Sexual Function | |
| Arm I - Leuprolide + Flutamide | 55 | 49 | 5 |
| Arm II - No Treatment | 54 | 49 | 28 |
To measure the differences in quality of life between wives of participants in the androgen ablation condition compared to wives of patients in the control condition by using quality of life assessments. The following questionnaires were completed in the clinic setting and used to assess Health related (HRQoL): Medical Outcomes Study 36-Item Short Form (SF-36), University of California-Los Angeles Sexual Function Scale (UCLA-SFS), and Southwest Oncology Group Treatment-Specific Symptoms Scale (SWOG-TSSS). The SF-36 was analysed using a composite score for each of physical health and mental health. SF-36, UCLA-SFS, SWOGTSSS were combined to classify participants' quality of life. (NCT00003645)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A | 19 |
| Arm B | 24 |
Here are the total number of participants with adverse events. For the detailed list of adverse events see the adverse event module. (NCT00004635)
Timeframe: Date treatment consent signed to date off study, approximately 60 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Thalidomide | 117 |
| Placebo | 98 |
Time to progression is defined as follows: if the PSA returns to baseline (defined as the PSA value prior to starting leuprolide or goserelin) or increases to the absolute value of 5 ng/ml. (NCT00004635)
Timeframe: 36 months
| Intervention | months (Median) |
|---|---|
| Thalidomide | 15 |
| Placebo | 9.6 |
Patients were evaluated for acute toxicities defined as grade 3 or greater cardiovascular (including venous thrombosis), gastrointestinal, or genitourinary toxicity occurring during the period starting from treatment initiation until 90 days or less after the completion of radiotherapy. The same toxicity measures were monitored at >90 days after the completion of radiotherapy. (NCT00016913)
Timeframe: 90 days and 1 year post treatment
| Intervention | Events (Number) | |
|---|---|---|
| Grade 3+ Toxicity <=90 days post radiotherapy | Grade 3+ Toxicity >90 days post radiotherapy | |
| Neo-Adj ChemoTx + Ablation Prior to RT | 2 | 0 |
PSA progression was defined in 2 ways. The CALGB PSA progression was defined as 2 consecutive rises in PSA with a rise of at least 0.2 ng/mL and above 1.0 ng/mL after radiation therapy; the date of PSA failure is taken as the midpoint between the last PSA before the rise and the first of the 2 PSAs that documented the rise. In addition, PSA progression was used according to the American Society for Therapeutic Radiology and Oncology 1996 (ASTRO) criteria and defined as 3 consecutive rises in PSA after radiation therapy. The date of PSA failure was taken as the midpoint between the time of the lowest PSA measure after irradiation and the first of the 3 consecutive rises. (NCT00016913)
Timeframe: PSA was measured every 4 weeks during chemotherapy, at least every 12 weeks post radiation for 2 years, and every 6 months thereafter until PSA failure date (Up to 5.5 years).
| Intervention | months (Median) | |
|---|---|---|
| CALGB criteria | ASTRO criteria | |
| Neo-Adj ChemoTx + Ablation Prior to RT | 17.1 | 12.1 |
PFS was defined as the time between treatment initiation and the date of disease progression (PSA, bone, tumor) or death, whichever occurred first. PSA progression is defined as 2 consecutive rising PSAs (a rise of at least 0.2 ng/mL) above 1.0 ng/mL. (NCT00016913)
Timeframe: registration to progression, up to 5.5 years from registration
| Intervention | months (Median) |
|---|---|
| Neo-Adj ChemoTx + Ablation Prior to RT | 12.1 |
Overall survival is defined from the date of registration to date of death from any cause (NCT00028769)
Timeframe: 0-5 years
| Intervention | months (Median) |
|---|---|
| CAD + Chemo | 38 |
Measured from time of registration to time of first documentation of progression determined from the prostate-specific antigen (PSA) level, clinical criteria, or symptomatic deterioration. PSA progression is defined as a 25% increase greater than baseline. If the patient's PSA level had decrease during the study, a 25% increase from the nadir PSA level, with absolute value of >=5 ng/mL is considered progression. CLinical progress is defined as the appearance of any new lesion at any site or death without documented progression. Symptomatic deterioration is defined as a global deterioration of the health status requiring discontinuation of treatment without objective evidence of progression. (NCT00028769)
Timeframe: 0-5 years (assessed every 3 months if no progression when the chemotherapy had been finished. Once off chemotherapy, assessed every 3 months until progression)
| Intervention | months (Median) |
|---|---|
| CAD + Chemo | 13 |
Adverse Events (AEs) are reported by the NCI Common Terminology Criteria for Adverse Events (CTCAE) version 2.0. For each patient, worst grade of each event type is reported. Grade 3 = Severe, Grade 4 = Life-threatening, Grade 5 = Fatal. (NCT00028769)
Timeframe: up to 5 years after registration
| Intervention | Participants (Number) | ||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Alkaline phosphatase increase | Anemia | Bilirubin increase | Cardiac ischemia/infarction | Confusion | Constipation/bowel obstruction | Edema | Erectile impotence | Fatigue/malaise/lethargy | GI-other | Hyperglycemia | Infection w/o 3-4 neutropenia | Infection with 3-4 neutropenia | Leukopenia | Lymphopenia | Neutropenia/granulocytopenia | PRBC transfusion | Pain-other | Prothrombin time increase | Renal failure | Second primary | Thrombocytopenia | Thrombosis/embolism | |
| CAD + Chemo | 1 | 1 | 1 | 1 | 1 | 1 | 2 | 3 | 2 | 1 | 2 | 1 | 2 | 9 | 2 | 9 | 2 | 1 | 1 | 1 | 1 | 1 | 4 |
Study's primary endpoint of PFS duration/time to progression was defined as the time from the date of randomization to the date of first evidence of disease progression or patient death. Prostate-specific antigen (PSA) progression is usually the first evidence of progression. PSA progression is defined as a 25% increase over the baseline or the nadir provided that the increase is a minimum of 1 ng/ml. (NCT00081159)
Timeframe: Up to 90 months with evaulation in 4 week intervals for up to 6 months of treatment, then follow up until disease progression
| Intervention | Months (Median) |
|---|---|
| HAT, Doxorubicin, Zoledronate + Strontium Chloride | 12.9 |
| HAT, Doxorubicin + Zoledronate | 18.5 |
Overall Survival defined as the length of time from the start of treatment till time that participants are still alive. (NCT00081159)
Timeframe: Up to 90 months
| Intervention | Months (Median) |
|---|---|
| HAT, Doxorubicin, Zoledronate + Strontium Chloride | 47.4 |
| HAT, Doxorubicin + Zoledronate | 53.5 |
Bone scan performed at baseline and at Week 13 provided if baseline scan was positive for metastases. A major bone scan response was considered with a substantial resolution of participant bone metastases on the bone scans, i.e. complete resolution of the osseous metastases on the bone scan. (NCT00081159)
Timeframe: Week 13
| Intervention | participants (Number) |
|---|---|
| HAT, Doxorubicin, Zoledronate + Strontium Chloride | 0 |
| HAT, Doxorubicin + Zoledronate | 0 |
Insulin resistance calculated from homeostasis model assessment of insulin resistance (HOMA-IR) equation: fasting insulin x fasting glucose / 405. Higher values indicate more insulin resistance. (NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Mean) |
|---|---|
| Metformin | -31.0 |
| Leuprolide | -8.18 |
| Placebo | 4.67 |
(NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Median) |
|---|---|
| Metformin | 4.6 |
| Leuprolide | -96.5 |
| Placebo | -1.2 |
(NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Mean) |
|---|---|
| Metformin | -4.2 |
| Leuprolide | 4.0 |
| Placebo | -0.3 |
(NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Median) |
|---|---|
| Metformin | 2.6 |
| Leuprolide | 0.9 |
| Placebo | -2.9 |
(NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Mean) |
|---|---|
| Metformin | -10.8 |
| Leuprolide | 5.3 |
| Placebo | 25.3 |
Percent change in free T by equilibrium dialysis between baseline and 12 weeks (NCT00123110)
Timeframe: Baseline to 12 weeks
| Intervention | percent change (Mean) |
|---|---|
| Metformin | -6.9 |
| Leuprolide | -35.8 |
| Placebo | 12.1 |
(NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | percent change (Mean) |
|---|---|
| Metformin | -1.3 |
| Leuprolide | 0.1 |
| Placebo | 0.3 |
Change in insulin sensitivity (mg/kg/min) calculated from hyperinsulinemic euglycemic clamp (NCT00123110)
Timeframe: baseline and 12 weeks
| Intervention | mg/kg/min (Mean) |
|---|---|
| Metformin | 0.44 |
| Leuprolide | 0.04 |
| Placebo | -0.08 |
PSA progression is defined as a rise in PSA to >4.0 ng/mL demonstrated twice in measurements taken two weeks apart. (NCT00170157)
Timeframe: 18 months from the start of AA therapy
| Intervention | participants (Number) |
|---|---|
| Entire Study Population | 0 |
Percent of participants who had undetectable PSA at 3 months on the initially assigned treatment arm (prior to crossing over). (NCT00170157)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Androgen Ablative (AA) Therapy + MDX-010 | 55 |
| Androgen Ablative (AA) Then AA Therapy + MDX-010 | 39 |
This outcome is defined as the average concentration of leptin (a hormone produced by the fat cells that affects feeding behavior and appetite) in the blood, measured repeatedly over a 24 hour period in each patient individually. (NCT00203996)
Timeframe: 15 minutes over a period of 24 hours
| Intervention | nanogram/milliliter (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 67.6 |
| Aim 2: Matched Controls With CPAP | 56.9 |
Insulin sensitivity Index (SI) is the increase in net fractional glucose clearance rate per unit change in plasma insulin concentration after an intravenous glucose load. SI quantifies the capacity of insulin to promote glucose disposal. (NCT00203996)
Timeframe: Baseline
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 3: SWS Suppression | 8.42 |
This outcome is defined as the average concentration of leptin (a hormone produced by the fat cells that affects feeding behavior and appetite) in the blood, measured repeatedly over a 24 hour period in each patient individually. (NCT00203996)
Timeframe: 15 minutes over a period of 24 hours
| Intervention | nanogram/milliliter (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 65.8 |
| Aim 2: Matched Controls With CPAP | 57.4 |
This outcome is defined as the average concentration of cortisol (a glucocorticoid produced by the adrenal gland) in the blood, measured repeatedly over a 24 hour period in each patient individually. (NCT00203996)
Timeframe: 10 minutes, over a period of 24 hours
| Intervention | microgram/deciliter (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 8.6 |
| Aim 2: Matched Controls With CPAP | 6.1 |
Insulin sensitivity Index (SI) is the increase in net fractional glucose clearance rate per unit change in plasma insulin concentration after an intravenous glucose load. SI quantifies the capacity of insulin to promote glucose disposal. (NCT00203996)
Timeframe: 3 nights
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 3: SWS Suppression | 5.87 |
Insulin sensitivity Index (SI) is the increase in net fractional glucose clearance rate per unit change in plasma insulin concentration after an intravenous glucose load. SI quantifies the capacity of insulin to promote glucose disposal. (NCT00203996)
Timeframe: 8 weeks
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 0.93 |
| Aim 2: Matched Controls With CPAP | 2.57 |
Acute insulin resistance to intravenous glucose (AIRg) is a measure of the secretion of insulin during the first 10 minutes after an intravenous glucose load. AIRg addresses adequacy of insulin secretion. (NCT00203996)
Timeframe: baseline (0 weeks)
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 1711 |
| Aim 2: Matched Controls With CPAP | 695 |
Acute insulin resistance to intravenous glucose (AIRg) is a measure of the secretion of insulin during the first 10 minutes after an intravenous glucose load. AIRg addresses adequacy of insulin secretion. (NCT00203996)
Timeframe: 8 weeks
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 1614 |
| Aim 2: Matched Controls With CPAP | 722 |
This outcome is defined as the average concentration of cortisol (a glucocorticoid produced by the adrenal gland) in the blood, measured repeatedly over a 24 hour period in each patient individually. (NCT00203996)
Timeframe: 10 minutes, over a period of 24 hours
| Intervention | microgram/deciliter (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 7.8 |
| Aim 2: Matched Controls With CPAP | 6.5 |
Insulin sensitivity Index (SI) is the increase in net fractional glucose clearance rate per unit change in plasma insulin concentration after an intravenous glucose load. SI quantifies the capacity of insulin to promote glucose disposal. (NCT00203996)
Timeframe: baseline (0 weeks)
| Intervention | mU/(liter x min) (Mean) |
|---|---|
| Aim 2: PCOS + SDB With CPAP | 0.87 |
| Aim 2: Matched Controls With CPAP | 3.67 |
Dual-energy x-ray absorptiometry (DEXA) scans were performed prior to first cycle of ADT, after completion of the first cycle of ADT, and prior to the start of the second cycle of ADT. Bone Mineral Density (BMD) was a assessed in g/cm^2 as a indicator of bone health. Percent change was assess for each patient at each time point. (NCT00223665)
Timeframe: From screening prior to first dose of ADT through the start of the second cycle of ADT.
| Intervention | Percent change of BMD (Number) | |
|---|---|---|
| Post Cycle 1 versus Baseline | Pre Cycle 2 versus Post Cycle 1 | |
| Intermittent Androgen Suppression (IAS) | -1.2 | -0.2 |
Spatial Memory was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT using the Puget Sound Route Learning Test. This test measured the ability to navigate a short route within a room. Three trials were administered followed by three trials of a new route using pictures placed on the floor as landmarks. A delayed recall is administered after twenty minutes. Performance was assessed based on number of correctly recalled sequences after a delay. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | number of correctly recalled sequences (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 19.50 | 22.00 | 23.76 | 24.12 |
Verbal Ability/Fluency was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. Participants were asked to verbally generate as many words beginning with a particular letter (e.g. P) within a 60 second period. Two trials were administered with two different letters. The total number of words generated was recorded for each letter and summed and analyzed. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | Number of words generated (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 24.65 | 26.15 | 26.29 | 25.70 |
Verbal Memory was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT via the Proactive Interference (PI) task. The PI task involves participants listening to a list of 10 words from the same semantic category (e.g., articles of clothing), and then recalling as many of these words as possible.The procedure is repeated for a total of 4 trials. Assessment is based on the total number of words recalled. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | Number of correctly recalled words (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 21.31 | 22.90 | 22.70 | 22.70 |
Dual-energy x-ray absorptiometry (DEXA) scans were performed prior to first cycle of ADT, after completion of the first cycle of ADT, and prior to the start of the second cycle of ADT. Bone Mineral Density (BMD) was a assessed in g/cm^2 as a indicator of bone health for each patient at each time point. This measure was defined as the percentage of participants with normal BMD scores at baseline who developed Osteopenia after the first cycle of ADT. (NCT00223665)
Timeframe: From screening prior to first dose of ADT through the start of the second cycle of ADT.
| Intervention | percent of participants (Number) |
|---|---|
| Intermittent Androgen Suppression (IAS) | 13.2 |
Assessment of overall survival measured as median time from completion of first full cycle of IAS until date of death from any cause. (NCT00223665)
Timeframe: From date of first treatment until the date of death or study withdrawal, whichever came first, assessed up to 16 years.
| Intervention | years (Median) |
|---|---|
| Intermittent Androgen Suppression (IAS) | 6.6 |
Monthly Prostate-Specific Antigen (PSA) testing to assess the point at which each patient's disease stops responding to Androgen Deprivation Therapy (ADT). Androgen Independence (AI), also know as Castrate Resistance (CR), was defined as 2 serial rises in PSA while on ADT with Testosterone levels <50 ng/dL. (NCT00223665)
Timeframe: From date of first treatment until the date of development of CR, metastatic progression, or study withdrawal, whichever came first, assessed up to 16 years.
| Intervention | years (Median) |
|---|---|
| Intermittent Androgen Suppression (IAS) | 4.0 |
Verbal Memory was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT via Story Recall. This task is based on the well known Wechsler Memory Scale -Revised Logical Memory task. Participants listened to two brief narratives (stories) and were asked to recall as much as possible immediately after hearing each story and following a 20-minute delay. Assessment was based on number of correctly recalled pieces of information after a delay. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | number of correctly recalled data points (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 35.06 | 37.86 | 39.38 | 41.16 |
Dual-energy x-ray absorptiometry (DEXA) scans were performed prior to first cycle of ADT, after completion of the first cycle of ADT, and prior to the start of the second cycle of ADT. Bone Mineral Density (BMD) was a assessed in g/cm^2 as a indicator of bone health for each patient at each time point. (NCT00223665)
Timeframe: From screening prior to first dose of ADT through the start of the second cycle of ADT.
| Intervention | Percent change in BMD (Number) | |
|---|---|---|
| Post Cycle 1 versus Baseline | Pre Cycle 2 versus Post Cycle 1 | |
| Intermittent Androgen Suppression (IAS) | -3.4 | 1.4 |
Estradiol was measured at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | pg/ml (Mean) | |||
|---|---|---|---|---|
| Baseline | Measurement at Month 3 | Measurement at Month 9 | Measurement at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 33.60 | 23.12 | 22.76 | 24.35 |
Executive Function was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. This assessment was based on the Stroop Color Word Interference Task. Subjects are asked to read 100 color words (red, green, blue), followed by identification of color blocks followed by reading the color of the ink and ignoring the word (e.g., the word 'blue' printed in green letters). Assessment was based on the amount of time needed to time to complete the assessment. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | minutes to complete the assessment (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 51.00 | 55.52 | 47.58 | 48.82 |
Spatial Ability was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. This assessment was based on the Wechsler Adult Intelligence Scale-Revised, Block Design sub-test and measures participants' ability to analyze and construct abstract figures from their component parts. The test allows a time limit of 3 minutes per design, for a total of nine designs. Score is based on total number of designs completed (max 9, min 0). (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | Number of correctly completed designs (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Combined Androgen Blockade | 8.65 | 7.20 | 8.82 | 8.47 |
Spatial Ability (Mental Rotation) was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. This assessment was based on the Vandenberg & Kuse (1978) Mental Rotation Test. Subjects are presented with line drawings of complex, three dimensional cubes on a computer screen. The subject must compare the two drawings and decide if they match. Score is based on number of correctly identified figures. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | Number of correctly identified figures (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 16.12 | 13.00 | 16.52 | 15.53 |
Visual Working Memory was assessed at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. This task is based on the Subject Ordered Pointing Task (SOPT). The participant is shown a grid array of 10, 12 or 16 abstract designs and they must choose a new design with each refresh of the screen. Assessment is based on total number of errors. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | total number of errors (Mean) | |||
|---|---|---|---|---|
| Baseline | Score at Month 3 | Score at Month 9 | Score at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 13.22 | 15.66 | 12.35 | 14.00 |
Testosterone was measured at baseline, and at Month 3, Month 9, and Month 12 after the start of the first cycle of ADT. (NCT00223665)
Timeframe: Baseline, Month 3, Month 9, and Month 12
| Intervention | ng/ml (Mean) | |||
|---|---|---|---|---|
| Baseline | Measurement at Month 3 | Measurement at Month 9 | Measurement at Month 12 | |
| Intermittent Androgen Suppression (IAS) | 406 | 0.28 | 0.20 | 2.45 |
Measure of the activity of a treatment on a disease. In this study it is measured from the date of enrollment to the date on which the prostate cancer progresses or the date the patient dies. Survival curves were estimated using the Kaplan-Meier technique. Biochemical (PSA) failure is defined, in accordance to the American Society for Therapeutic Radiology and Oncology consensus definition, as three consecutive rise in PSA. The date of biochemical failure is considered to be the midpoint between the last non-rising PSA and the first rising PSA. (NCT00225420)
Timeframe: Average follow up of 2 years
| Intervention | percentage of patients (Mean) |
|---|---|
| Single Arm | 94 |
Determine the number of patients experiencing dose-limiting toxicities (DLT) at each dose level. DLT was defined as grade 3-4 non-haematological or grade 4 haematological toxicity, using the Common Terminology Criteria for Adverse Events, version 3.0. (NCT00225420)
Timeframe: Average follow up of 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Docetaxel at 10 mg/m2 | 1 |
| Docetaxel 15 mg/m2 | 1 |
| Docetaxel 20 mg/m2 | 0 |
Summary of adverse events( AE) collected during vaccine treatment period using Common Terminology Criteria for Adverse Events v3.0 (CTCAE). Grade 0-Sign/symptom within normal limits, Grade 1-Mild AE, Grade 2-Moderate AE, Grade 3-Severe AE, Grade 4- Life threatening or disabling AE. (NCT00254397)
Timeframe: Baseline up to 48 weeks during vaccine treatment
| Intervention | occurences (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Grade 4, Unspecified Relationship | Grade 3, Possible | Grade 3, Probable | Grade 3, Unrelated | Grade 3, Unspecified Relationship | Grade 2, Definite | Grade 2, Possible | Grade 2, Probable | Grade 2, Unlikely | Grade 2, Unrelated | Grade 2, Unspecified Relationship | Grade 1, Definite | Grade 1, Possible | Grade 1, Probable | Grade 1, Unlikely | Grade 1, Unrelated | Grade 1, Unspecified Relationship | Grade 0, Possible | Grade 0, Probable | Grade 0, Unlikely | Grade 0, Unrelated | Grade 0, Unspecified Relationship | |
| gp100 - No Leuprolide | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 1 | 1 | 4 | 6 | 3 | 4 | 3 | 7 | 0 | 0 | 0 | 0 | 0 |
| gp100 + Leuprolide | 0 | 1 | 1 | 0 | 0 | 5 | 3 | 5 | 0 | 3 | 8 | 21 | 22 | 13 | 16 | 15 | 29 | 1 | 2 | 0 | 0 | 2 |
| gp100 + MAGE-3 - No Leuprolide | 0 | 1 | 0 | 1 | 1 | 0 | 3 | 1 | 3 | 4 | 7 | 50 | 74 | 56 | 38 | 36 | 37 | 0 | 0 | 0 | 0 | 13 |
| gp100 + MAGE-3 + Leuprolide | 1 | 0 | 0 | 0 | 0 | 11 | 19 | 3 | 2 | 1 | 16 | 61 | 103 | 53 | 25 | 45 | 61 | 0 | 0 | 2 | 0 | 5 |
"Reactivity to the gp100 peptide in each participant defined as >10 tetramer positive cells per 10^4 CD8+ T-cells as determined by the tetramer analysis at 3 months following initial vaccine. Number of participants with response as defined reported.~The primary end point of this clinical study was the comparison of tumor-specific immune responses to melanoma-specific peptide vaccines, gp100 and MAGE-3 in the presence or absence of Leuprolide.~Gp209-2M/HLA-A*0201 tetramers that are commercially available employed to analyze levels of gp209-2M specific CD8+ cytolytic T cells. The levels of peptide/ HLA-A*0201 tetramer between participants' peripheral blood mononuclear cells (PBMCs) with Leuprolide injection and without Leuprolide injection compared." (NCT00254397)
Timeframe: At 3 months following initial vaccine.
| Intervention | Participants (Count of Participants) |
|---|---|
| gp100 + Leuprolide | 6 |
| gp100 - No Leuprolide | 1 |
| gp100 + MAGE-3 + Leuprolide | 12 |
| gp100 + MAGE-3 - No Leuprolide | 19 |
Summary of most frequent adverse events collected study wide during vaccine treatment period using Common Terminology Criteria for Adverse Events v3.0 (CTCAE). (NCT00254397)
Timeframe: Baseline up to 48 weeks during vaccine treatment
| Intervention | occurences (Number) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Elevated Creatinine | Hyperglycemia | Cardiac troponin T | Cardiac Ischema | Fatigue | Hypotension | Ruptured lumbar disc | Possible Metastatic Lung Nodule | Cellulitis | Cerebral Ischemia | Cardiac Ischemia/stent | Atrial fibrillation | Multiple Allergic Reactions | |
| gp100 + Leuprolide | 1 | 1 | 1 | 1 | 15 | 1 | 1 | 1 | 1 | 1 | 1 | 2 | 1 |
| gp100 + No Leuprolide | 0 | 0 | 0 | 0 | 7 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Maximum Grade reported for participant adverse events. collected study wide during vaccine treatment period using Common Terminology Criteria for Adverse Events v3.0 (CTCAE). (NCT00254397)
Timeframe: Baseline up to 48 weeks during vaccine treatment
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Grade 4-Life threatening or disabling | Grade 3-Severe | Grade 2-Moderate | Grade 1-Mild | |
| gp100 - No Leuprolide | 0 | 0 | 2 | 2 |
| gp100 + Leuprolide | 0 | 2 | 5 | 2 |
| gp100 + MAGE-3 - No Leuprolide | 0 | 3 | 10 | 24 |
| gp100 + MAGE-3 + Leuprolide | 1 | 0 | 21 | 7 |
"CD8+ cells are a type of T cell. T cells are produced in the thymus and thymic function can be determined by TREC. By counting the number of TRECs present (only 1 copy per cell) within a population of CD8+ cells, an assessment of T cell recovery and immune response is obtained. Mayo Medical Clinic. http://www.mayomedicallaboratories.com/test-catalog/Clinical+and+Interpretive/87959. Accessed 17 MARCH 2010~The change from baseline is defined as posttransplant TREC/100,000 CD8+ cells minus pretransplant TREC /100,000 CD8+ cells." (NCT00275262)
Timeframe: Pretransplant and posttransplant (Month 12)
| Intervention | TREC /100,000 CD8+ cells (Mean) | |
|---|---|---|
| Baseline mean for TREC per 100,000 CD8+ cells | Mean change in TREC from baseline to final visit | |
| Leuprolide Acetate Depot (LAD) 11.25 mg 3 Month | 181.673 | -10.811 |
| Placebo | 364.414 | -184.084 |
"CD4+ cells are a type of T cell. T cells are produced in the thymus and thymic function can be determined by TREC. By counting the number of TRECs present (only 1 copy per cell) within a population of CD4 cells, an assessment of T cell recovery and immune response is obtained. Mayo Medical Clinic. http://www.mayomedicallaboratories.com/test-catalog/Clinical+and+Interpretive/87959. Accessed 17 MARCH 2010~The change from baseline is defined as posttransplant TREC/100,000 CD4+ cells minus pretransplant TREC /100,000 CD4+ cells." (NCT00275262)
Timeframe: Pretransplant and posttransplant (Month 12)
| Intervention | TREC /100,000 CD4+ cells (Mean) | |
|---|---|---|
| Baseline TREC per 100,000 CD4+ cells | Mean change in TREC from baseline to final visit | |
| Leuprolide Acetate Depot (LAD) 11.25 mg 3 Month | 67.524 | 522.321 |
| Placebo | 173.712 | -63.950 |
Patients received a subcutaneous injection of KLH vaccine 1 month after subjects received the third injection of LAD or placebo. Interferon gamma was determined by enzyme-linked immunosorbent spot-forming cell (ELISpot). Baseline is defined as the interferon gamma concentration obtained before the KLH vaccination. Change from baseline was calculated as the interferon gamma value postvaccination minus the interferon gamma value at baseline. (NCT00275262)
Timeframe: Month 6 prevaccination (baseline) and Month 7 postvaccination
| Intervention | spots/1 million cells (Mean) | |
|---|---|---|
| Mean interferon gamma at baseline | Mean interferon gamma change from baseline | |
| Leuprolide Acetate Depot (LAD) 11.25 mg 3 Month | 0.2 | 2.09 |
| Placebo | -1.4 | 10.25 |
Patients received a subcutaneous injection of KLH vaccine 1 month after subjects received the third injection of LAD or placebo. Serum immunoglobulin IgM antibodies were determined by enzyme-linked immunosorbent assay (ELISA). Baseline is defined as the IgM concentration before the KLH vaccination. Change from baseline was calculated as the IgM value postvaccination minus the IgM value at prevaccination. (NCT00275262)
Timeframe: Month 6 prevaccination (baseline) and Month 7 postvaccination
| Intervention | mcg/mL (Mean) | |
|---|---|---|
| Mean IgM at baseline (mcg/mL) | Mean IgM change from baseline (mcg/mL) | |
| Leuprolide Acetate Depot (LAD) 11.25 mg 3 Month | 4.0 | 2.91 |
| Placebo | 3.0 | 0.57 |
Patients received a subcutaneous injection of KLH vaccine 1 month after subjects received the third injection of LAD or placebo. Serum immunoglobulin IgG1 antibodies were determined by enzyme-linked immunosorbent assay (ELISA). Baseline is defined as the IgG1 concentration before the KLH vaccination. Change from baseline was calculated as the IgG1 value postvaccination minus the IgG1 value at baseline. (NCT00275262)
Timeframe: Month 6 prevaccination (baseline) and Month 7 postvaccination
| Intervention | mcg/mL (Mean) | |
|---|---|---|
| Mean IgG1 at baseline (mcg/mL) | Mean IgG1 change from baseline (mcg/mL) | |
| Leuprolide Acetate Depot (LAD) 11.25 mg 3 Month | 8.6 | 46.16 |
| Placebo | 10.8 | 16.76 |
"PFS is the interval from the date of surgery to date of progression. The date of progression was the earlier of~first PSA increase to ≥ 0.4 ng/mL confirmed within two weeks~date of the nadir, if PSA nadir did not reach < 0.4 ng/mL (for deferred arm)~first radiological/ histological evidence of tumor progression~death. Median PFS was to be estimated using Kaplan-Meier curves. However, enrollment was not met, and meaningful conclusions for efficacy or QoL could not be drawn. Median PFS could not be estimated. Reported is the number of participants with disease progression." (NCT00283062)
Timeframe: from the date of surgery up to 3 years after randomization of the last participant
| Intervention | participants (Number) |
|---|---|
| Docetaxel / Leuprolide Acetate - Immediate Treatment (I-CHT) | 10 |
| Leuprolide Acetate - Immediate Treatment (I-HT) | 14 |
| Docetaxel / Leuprolide Acetate - Deferred Treatment (D-CHT) | 9 |
| Leuprolide Acetate - Deferred Treatment (D-HT) | 8 |
"Overall survival (OS) was the time interval from the date of surgery to the date of death due to any cause.~Median OS was to be estimated using Kaplan-Meier Curves. However, enrollment was not met, and meaningful conclusions for efficacy or QoL could not be drawn. Moreover, median OS could not be estimated. Reported is the number of participants who died from any cause." (NCT00283062)
Timeframe: from the date of surgery up to 3 years after randomization of the last participant
| Intervention | participants (Number) |
|---|---|
| Docetaxel / Leuprolide Acetate - Immediate Treatment (I-CHT) | 0 |
| Leuprolide Acetate - Immediate Treatment (I-HT) | 2 |
| Docetaxel / Leuprolide Acetate - Deferred Treatment (D-CHT) | 1 |
| Leuprolide Acetate - Deferred Treatment (D-HT) | 1 |
"The FACT-P is a 39-item participant questionnaire which assesses physical well-being (7 items), social/family well-being (7 items), emotional well-being (6 items), functional well-being (7 items), and additional prostate cancer specific concerns (12 items). All items are scored from 0 (not at all) to 4 (very much). The total FACT-P score ranges from 0-156, with higher scores representing a better QoL with fewer symptoms. A score of 156 represents the best outcome.~Note: Enrollment was not met, and meaningful conclusions for efficacy or QoL could not be drawn due to the low sample size." (NCT00283062)
Timeframe: from 30 days before randomization (baseline) and 18 months after treatment initiation (for change from baseline)
| Intervention | score on a scale (Mean) | |
|---|---|---|
| Baseline | Change from Baseline (N=33, N=41, N=12, N=10) | |
| Docetaxel / Leuprolide Acetate - Deferred Treatment (D-CHT) | 114.7 | 6.7 |
| Docetaxel / Leuprolide Acetate - Immediate Treatment (I-CHT) | 124.0 | 0.7 |
| Leuprolide Acetate - Deferred Treatment (D-HT) | 119.7 | 6.1 |
| Leuprolide Acetate - Immediate Treatment (I-HT) | 121.5 | 1.7 |
Number of participants with treatment-emergent adverse events (TEAE). A TEAE was as any adverse event that occurred or worsened during the on-treatment period, which was the period from the day of first infusion of study treatment until 30 days after the last infusion of study treatment. (NCT00283062)
Timeframe: from treatment initiation up to 19 months after treatment initiation
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| with any adverse event (AE) | with any serious adverse event (SAE) | with an SAE resulting in death | with a drug-related AE | with a drug-related SAE | with AE leading to discontinue all study therapy | with AE leading to chemotherapy discontinuation | with AE leading to chemotherapy dose reduction | |
| Docetaxel / Leuprolide Acetate - Deferred Treatment (D-CHT) | 19 | 5 | 0 | 18 | 2 | 1 | 1 | 2 |
| Docetaxel / Leuprolide Acetate - Immediate Treatment (I-CHT) | 47 | 12 | 0 | 47 | 6 | 2 | 1 | 5 |
| Leuprolide Acetate - Deferred Treatment (D-HT) | 14 | 2 | 0 | 10 | 0 | 0 | NA | NA |
| Leuprolide Acetate - Immediate Treatment (I-HT) | 48 | 8 | 0 | 43 | 0 | 0 | NA | NA |
This outcome measure presents the testosterone levels 3 days after the initial dose of trial medication. (NCT00295750)
Timeframe: 3 days
| Intervention | percentage of patients (Mean) |
|---|---|
| Degarelix 240/160 mg | 95.5 |
| Degarelix 240/80 mg | 96.1 |
| Leuprolide 7.5 mg | 0 |
Kaplan-Maier estimates of the cumulative probabilities of testosterone <=0.5 ng/mL from Day 28 to Day 364. The degarelix response rate estimation determined whether the lower bound of the 95% confidence interval for the cumulative probability of testosterone <=0.5 ng/mL from Day 28 to Day 364 was no lower than 90%. (NCT00295750)
Timeframe: 12 months
| Intervention | percentage of patients (Mean) |
|---|---|
| Degarelix 240/160 mg | 98.3 |
| Degarelix 240/80 mg | 97.2 |
| Leuprolide 7.5 mg | 96.4 |
The QTc interval results are calculated with Fridericia's correction. QTc intervals are a standard evaluation of an electrocardiogram and help measure the risk of developing ventricular arrhythmias. (NCT00295750)
Timeframe: 12 months
| Intervention | milliseconds (Mean) | ||
|---|---|---|---|
| Baseline Day 0 (n=202, 207, 201) | Day 3 (n=195, 204, 197) | End of study 12 months (n=202, 207, 201) | |
| Degarelix 240/160 mg | 403 | 404 | 415 |
| Degarelix 240/80 mg | 407 | 411 | 420 |
| Leuprolide 7.5 mg | 404 | 405 | 419 |
Percentage change from Baseline to Day 14 and Day 28 in prostate-specific antigen, which is a clinically important biological marker for treatment effect and prostate cancer progression. (NCT00295750)
Timeframe: Days 14 and 28
| Intervention | percent change (Median) | |
|---|---|---|
| Day 14 | Day 28 | |
| Degarelix 240/160 mg | -64.6 | -82.3 |
| Degarelix 240/80 mg | -63.4 | -84.9 |
| Leuprolide 7.5 mg | -17.9 | -66.7 |
Vital signs and body weight included incidence of markedly abnormal changes from baseline to the end of the study in blood pressure (systolic and diastolic), pulse, and body weight at the end of trial as compared to baseline. The table presents the number of patients in each group with normal baseline and markedly abnormal value post-baseline. (NCT00295750)
Timeframe: 12 months
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Systolic blood pressure <=90 and decrease >=20 | Systolic blood pressure >=180 and increase >=20 | Diastolic blood pressure <=50 and decrease >=15 | Diastolic blood pressure >=105 and increase >=15 | Heart rate <=50 and decrease >=15 | Heart rate >=120 and increase >=15 | Body weight decrease of >=7 percent | Body weight increase of >=7 percent | |
| Degarelix 240/160 mg | 12 | 20 | 12 | 5 | 8 | 1 | 5 | 24 |
| Degarelix 240/80 mg | 8 | 16 | 10 | 13 | 7 | 0 | 6 | 15 |
| Leuprolide 7.5 mg | 6 | 23 | 9 | 8 | 9 | 1 | 10 | 23 |
Criteria for lab values changes from baseline to the end of the study considered markedly abnormal were set for each lab test. If 20% of patients reached that value, the results were reported. (NCT00295750)
Timeframe: Baseline to Day 364
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Haematocrit (<=0.37 ratio) | Haemoglobin (<=115 g/L) | Serum Urea Nitrogen (>=10.7 mmol/L) | Urine Protein (>=2 units from baseline) | Urine Bacteria (0 at baseline and >0 on treatment) | |
| Degarelix 240/160 mg | 73 | 32 | 48 | 65 | 96 |
| Degarelix 240/80 mg | 80 | 45 | 41 | 64 | 105 |
| Leuprolide 7.5 mg | 73 | 38 | 50 | 63 | 107 |
The time to prostate specific antigen failure was defined as the days from first dosing (scheduled dosing days) where an increase in serum prostate specific antigen of ≥50% from nadir and a least 5 ng/mL measured on two consecutive occasions at least two weeks apart was noted. (NCT00295750)
Timeframe: 12 months
| Intervention | participants (Number) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 0-28 (patients at risk=193, 201, 194) | Day 0-56 (patients at risk=192, 197, 192) | Day 0-84 (patients at risk=190, 193, 190) | Day 0-112 (patients at risk=190, 189, 188) | Day 0-140 (patients at risk=187, 187, 182) | Day 0-168 (patients at risk=179, 185, 180) | Day 0-196 (patients at risk=173, 181, 175) | Day 0-224 (patients at risk=168, 175, 173) | Day 0-252 (patients at risk=165, 169, 168) | Day 0-280 (patients at risk=157, 165, 163) | Day 0-308 (patients at risk=153, 161, 156) | Day 0-336 (patients at risk=149, 156, 150) | Day 0-364 (patients at risk=149, 155, 148) | |
| Degarelix 240/160 mg | 1 | 1 | 1 | 1 | 2 | 7 | 11 | 14 | 16 | 20 | 23 | 26 | 26 |
| Degarelix 240/80 mg | 0 | 0 | 0 | 1 | 2 | 4 | 4 | 7 | 9 | 11 | 12 | 15 | 16 |
| Leuprolide 7.5 mg | 1 | 1 | 1 | 3 | 7 | 9 | 11 | 12 | 14 | 18 | 21 | 24 | 26 |
Testosterone increases on Day 255 and/or on Day 259 (highest value of Day 255 and Day 259 was used) were compared with Day 252 values. Patients were categorised with shifts of <=-0.25, >-0.25-0, >0-0.25, >0.25-0.5 and >0.5 ng/mL from mean testosterone levels on Day 252. (NCT00295750)
Timeframe: Day 252, Day 255, and Day 259
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| <=-0.25 ng/mL | >-0.25-0 ng/mL | >0-0.25 ng/mL | >0.25-0.5 ng/mL | >0.5 ng/mL | |
| Degarelix 240/160 mg | 1 | 84 | 91 | 0 | 0 |
| Degarelix 240/80 mg | 3 | 85 | 90 | 0 | 0 |
| Leuprolide 7.5 mg | 0 | 49 | 122 | 5 | 3 |
A patient was defined as having a testosterone surge if the testosterone level exceeded baseline by >=15% on any two days during the first two weeks of treatment (i.e. two of Study Days 1, 3, 7 and 14). (NCT00295750)
Timeframe: 2 weeks
| Intervention | percentage of patients (Mean) |
|---|---|
| Degarelix 240/160 mg | 0.5 |
| Degarelix 240/80 mg | 0.0 |
| Leuprolide 7.5 mg | 80.1 |
A drug-related AE was an AE that occurred postdose or was present predose and became more severe postdose and was considered to be related to study treatment. A summary of other nonserious AEs, and all SAE's, regardless of causality, is located in the Reported Adverse Events section. (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | participants (Number) | |
|---|---|---|
| Study Period 1 (n=46, 45) | Study Period 2 (n=20, 19) | |
| Somatropin | 38 | 9 |
| Somatropin and Leuprorelin | 42 | 11 |
Bone age measured using the X-Ray of left hand and wrist. (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | years (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Randomization (n=45, 43) | Month 12 (n=40, 41) | Month 24 (n=34, 37) | Month 36 (n=18, 18) | Month 48 (n=7, 8) | Safety follow up 6 months (n=16, 7) | Safety follow up 18 months (n=12, 3) | Safety follow up 36 months (n=5, 0) | Safety follow up 12 months (final height)(n=18,14) | |
| Somatropin | 11.0 | 12.1 | 13.4 | 14.5 | 15.4 | 14.9 | 17.0 | 0 | 16.3 |
| Somatropin and Leuprorelin | 10.8 | 11.7 | 12.4 | 13.3 | 14.8 | 14.1 | 15.2 | 15.7 | 19.6 |
The height of the participants were measured barefoot using a standard wall-mounted Harpenden stadiometer. SDS report the number of standard deviations from the mean for age and sex for an individual measurement (normal range: -2 to +2 SDS). Height SDS is derived by subtracting the population mean from individual's height value and then dividing that difference by the population standard deviation. Greater height SDS values indicate greater height. (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | standard deviation score (Mean) |
|---|---|
| Somatropin and Leuprorelin | -1.8 |
| Somatropin | -1.9 |
"This is the difference between the gender, age and country matched standard deviation score of adult height and standard deviation score of baseline height for particular participant.~The height of the participants were measured barefoot using a standard wall-mounted Harpenden stadiometer. SDS report the number of standard deviations from the mean for age and sex for an individual measurement (normal range: -2 to +2 SDS). Height SDS is derived by subtracting the population mean from individual's height value and then dividing that difference by the population standard deviation. Greater height SDS values indicate greater height." (NCT00355030)
Timeframe: Baseline through End up Study (up to 9 years)
| Intervention | standard deviation score (Mean) |
|---|---|
| Somatropin and Leuprorelin | 0.6 |
| Somatropin | 0.6 |
"This is the difference between the gender, age and country matched standard deviation score of adult height and standard deviation score of baseline predicted height [calculated using the Bayley-Pinneau method based on height and bone age] for particular participant.~The height of the participants were measured barefoot using a standard wall-mounted Harpenden stadiometer. SDS report the number of standard deviations from the mean for age and sex for an individual measurement (normal range: -2 to +2 SDS). Height SDS is derived by subtracting the population mean from individual's height value and then dividing that difference by the population standard deviation. Greater height SDS values indicate greater height." (NCT00355030)
Timeframe: Baseline through End up Study (up to 9 years)
| Intervention | standard deviation score (Mean) |
|---|---|
| Somatropin and Leuprorelin | 1.1 |
| Somatropin | 1.2 |
"This is the difference between the gender, age and country matched standard deviation score of adult height and standard deviation score of target height [calculated as (mother's height (SDS) + father's height (SDS))/2] for particular participant.~The height of the participants were measured barefoot using a standard wall-mounted Harpenden stadiometer. SDS report the number of standard deviations from the mean for age and sex for an individual measurement (normal range: -2 to +2 SDS). Height SDS is derived by subtracting the population mean from individual's height value and then dividing that difference by the population standard deviation. Greater height SDS values indicate greater height." (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | standard deviation score (Mean) |
|---|---|
| Somatropin and Leuprorelin | -0.6 |
| Somatropin | -1.2 |
Percentage of children with normal adult height SDS (greater than -2 SDS and less than +2 SDS) (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | percentage of participants (Number) |
|---|---|
| Somatropin and Leuprorelin | 26.7 |
| Somatropin | 25.6 |
SDS report the number of standard deviations from the mean for age and sex for an individual measurement (normal range: -2 to +2 SDS). Height SDS is derived by subtracting the population mean from individual's height value and then dividing that difference by the population standard deviation. Greater height SDS values indicate greater height. (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | standard deviation score (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Randomization (n=45, 43) | Month 3 (n=45, 43) | Month 6 (n=45, 42) | Month 12 (n=44, 42) | Month 18 (n=42, 42) | Month 24 (n=37, 41) | Month 30 (n=25, 25) | Month 36 (n=18, 19) | Month 42 (n=13, 14) | Month 48 (n=7, 8) | Month 54 (n=1, 1) | Safety follow up 6 months (n=16, 9) | Safety follow up 12 months(n=15, 8) | Safety follow up 18 months (n=12, 4) | Safety follow up 24 months (n=9, 1) | Safety follow up 36 months (n=5, 0) | Safety follow up 42 months (n=2, 0) | Safety follow up 12 months (final height)(n=18,14) | Safety follow up 24 months (final height) (n=7,10) | Safety follow up 36 months (final height) (n=3,7) | |
| Somatropin | -2.5 | -2.4 | -2.2 | -2.0 | -1.9 | -1.8 | -2.0 | -2.0 | -1.9 | -1.9 | -1.7 | -1.7 | -1.7 | -1.9 | -1.2 | 0 | 0 | -1.8 | -2.0 | -2.2 |
| Somatropin and Leuprorelin | -2.5 | -2.4 | -2.3 | -2.2 | -2.2 | -2.3 | -2.2 | -2.0 | -1.8 | -1.6 | -1.0 | -2.1 | -1.9 | -1.9 | -1.9 | -1.9 | -2.4 | -1.9 | -1.6 | -1.2 |
Height velocity is the difference between 2 height measurements, divided by years elapsed between measurements. (NCT00355030)
Timeframe: Baseline through End of Study (up to 9 years)
| Intervention | centimeter per year (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Randomization (n=45, 43) | Month 3 (n=45, 43) | Month 6 (n=45, 42) | Month 12 (n=44, 42) | Month 18 (n=42, 42) | Month 24 (n=37, 41) | Month 30 (n=25, 25) | Month 36 (n=18, 19) | Month 42 (n=13, 14) | Month 48 (n=7, 8) | Month 54 (n=1, 1) | Safety follow up 6 months (n=16, 9) | Safety follow up 12 months(n=15, 8) | Safety follow up 18 months (n=12, 4) | Safety follow up 24 months (n=9, 1) | Safety follow up 36 months (n=5, 0) | Safety follow up 42 months (n=2, 0) | Safety follow up 12 months (final height)(n=18,14) | Safety follow up 24 months (final height) (n=7,10) | Safety follow up 36 months (final height) (n=3,7) | |
| Somatropin | 7.4 | 10.6 | 9.7 | 8.8 | 8.4 | 7.8 | 5.8 | 3.5 | 3.7 | 2.9 | 7.1 | 4.5 | 2.3 | 1.2 | 2.5 | 0 | 0 | 0.8 | 0.3 | 0.3 |
| Somatropin and Leuprorelin | 7.8 | 9.9 | 8.1 | 7.0 | 6.6 | 4.9 | 6.2 | 6.6 | 5.7 | 5.4 | 6.3 | 4.6 | 2.9 | 3.3 | 2.0 | 1.3 | 2.1 | 0.5 | 0.3 | 0.9 |
Baseline + Post-radiation PSA levels at three month intervals for initial two years then every 6 months thereafter. Participants with a rising PSA and no evidence of local or distant recurrence considered PSA failures. (NCT00388804)
Timeframe: 3 months up to 2 years
| Intervention | participants (Number) |
|---|---|
| RT Group 1 | 0 |
| RT Group 2 + Hormone Therapy | 0 |
Hormonal profile blood tests including follicle-stimulating hormone (FSH) test, luteinizing hormone (LH) and estradiol levels done every two months with menstruation questionnaire, starting three months after the injection of the second dose of leuprolide until the restoration of spontaneous menstruation or the presence of ovarian failure. Any unexpected vaginal bleeding or side effects during the period covered by leuprolide injection, which is 6 months, is recorded by participants in a monitoring checklist sheet given to them. (NCT00429494)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Leuprolide Acetate | 37 |
Proportion of participants surviving 5 years from randomization without biochemical progression or death. (NCT00430183)
Timeframe: 5 years
| Intervention | Proportion of participants (Number) |
|---|---|
| Arm A: Docetaxel + LHRH Agonist + Surgical Intervention | 0.81 |
| Arm B: Surgical Intervention | 0.74 |
Proportion of participants surviving 3 years from randomization without biochemical progression or death. bPFS was defined as the time from randomization to the date of the first documented biochemical progression or death. Progression will be defined as having experienced either of the following: a serum PSA level > 0.2 ng/mL that increases on 2 consecutive occasions each of which is at least 3 months apart or death occurs. The time of biochemical failure is measured from the date of randomization to the date of the first PSA level > 0.2 ng/mL. (NCT00430183)
Timeframe: Up to 3 years
| Intervention | proportion of patients (Number) |
|---|---|
| Arm A: Docetaxel + LHRH Agonist + Surgical Intervention | 0.89 |
| Arm B: Surgical Intervention | 0.84 |
This outcome measure included incidence of markedly abnormal changes in safety laboratory values. The table presents the number of participants with normal baseline (from main CS21 trial, NCT00295750) and at least one post-baseline markedly abnormal value during CS21A. Only the laboratory variables that had at least five percentages of participants in either group with abnormal value are presented, more variables were included in the study. ULN=Upper limit of normal. (NCT00451958)
Timeframe: Up to 4 years of treatment
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| S-Potassium (mmol/L) >=5.8 | S-Alanine aminotransferase (IU/L) >3xULN | S-Alkaline phosphatase (IU/L) >3xULN+25% increase | S-Creatinine (µmol/L) >=177 | S-Urea nitrogen (mmol/L) >=10.7 | B-Haematocrit (Ratio) <=0.37 | B-Haemoglobin (g/L) <=115 | B-Red blood cell count (10^12/L) <=3.5 | B-Eosinophils (%) >=10 | B-Lymphocytes (%) <=10 | |
| Degarelix 160 mg / Degarelix 160 mg | 9 | 6 | 5 | 7 | 9 | 47 | 20 | 15 | 7 | 9 |
| Degarelix 80 mg / Degarelix 80 mg | 11 | 1 | 4 | 12 | 6 | 40 | 12 | 10 | 6 | 8 |
| Leuprolide 7.5 mg / Degarelix 160 mg | 5 | 0 | 2 | 2 | 5 | 17 | 6 | 3 | 1 | 5 |
| Leuprolide 7.5 mg / Degarelix 80 mg | 6 | 1 | 4 | 5 | 5 | 22 | 9 | 5 | 1 | 10 |
(NCT00451958)
Timeframe: From time of switch to Day 56
| Intervention | International units/Liter (IU/L) (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Day 3 | Day 7 | Day 14 | Day 28 | Day 56 | |
| Leuprolide 7.5 mg/ Degarelix 240/160 mg | 0.035 | 0.035 | 0.035 | 0.035 | 0.035 | 0.035 |
| Leuprolide 7.5 mg/ Degarelix 240/80 mg | 0.035 | 0.035 | 0.035 | 0.035 | 0.035 | 0.035 |
(NCT00451958)
Timeframe: From time of switch to Day 56
| Intervention | ng/mL (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Day 3 | Day 7 | Day 14 | Day 28 | Day 56 | |
| Leuprolide 7.5 mg/ Degarelix 240/160 mg | 0.074 | 0.068 | 0.066 | 0.073 | 0.074 | 0.077 |
| Leuprolide 7.5 mg/ Degarelix 240/80 mg | 0.076 | 0.084 | 0.076 | 0.085 | 0.074 | 0.080 |
This outcome measure included incidence of markedly abnormal changes in blood pressure (systolic and diastolic), pulse, and body weight. The table presents the number of participants with normal baseline (from main CS21 study, NCT00295750) and at least one post-baseline markedly abnormal value during CS21A. (NCT00451958)
Timeframe: Up to 4 years of treatment
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Diastolic blood pressure <=50 and decrease >=15 | Diastolic blood pressure >=105 and increase >=15 | Systolic blood pressure <=90 and decrease >=20 | Systolic blood pressure >=180 and increase >=20 | Heart rate <=50 and decrease >=15 | Heart rate >=120 and increase >=15 | Body weight decrease of >=7 percent | Body weight increase of >=7 percent | |
| Degarelix 160 mg / Degarelix 160 mg | 6 | 6 | 4 | 13 | 3 | 1 | 24 | 14 |
| Degarelix 80 mg / Degarelix 80 mg | 3 | 3 | 4 | 7 | 4 | 1 | 15 | 25 |
| Leuprolide 7.5 mg / Degarelix 160 mg | 6 | 0 | 3 | 4 | 2 | 3 | 8 | 5 |
| Leuprolide 7.5 mg / Degarelix 80 mg | 3 | 4 | 5 | 7 | 7 | 1 | 21 | 4 |
PSA progression was defined as two consecutive increases of 50%, and at least 5 ng/mL, compared to nadir (obtained in either CS21, NCT00295750, or CS21A). The figures below present the percentage of participants with no PSA progression at each of the selected time points (there were more time points in the study) along with corresponding 95% confidence intervals (CI). (NCT00451958)
Timeframe: Until all participants have received at least 5 years of treatment and at a frequency of every 3 months
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Day 28 | Day 364 | Day 1960 | |
| Degarelix 160 mg / Degarelix 160 mg | 99.5 | 85.8 | 58.7 |
| Degarelix 80 mg / Degarelix 80 mg | 100 | 91.1 | 61.0 |
| Leuprolide 7.5 mg / Degarelix 160 mg | 100 | 87.9 | 73.8 |
| Leuprolide 7.5 mg / Degarelix 80 mg | 98.6 | 82.6 | 50.7 |
"The results below present the percentage of participants of having testosterone <=0.5 ng/mL at each of the selected time points (there were more time points in the study) from Day 28 in CS21 (NCT00295750) until the end of the CS21A study.~In all treatment groups approximately 3% per year of the participants had at least one testosterone >0.5 ng/mL during the study." (NCT00451958)
Timeframe: Until all participants have received at least 5 years of treatment and at a frequency of every 6 months
| Intervention | percentage (Number) | ||
|---|---|---|---|
| Day 84 | Day 364 | Day 1876 | |
| Degarelix 160 mg / Degarelix 160 mg | 100 | 98.3 | 87.7 |
| Degarelix 80 mg / Degarelix 80 mg | 99.5 | 97.2 | 82.0 |
| Leuprolide 7.5 mg / Degarelix 160 mg | 97.6 | 96.0 | 88.4 |
| Leuprolide 7.5 mg / Degarelix 80 mg | 98.6 | 97. | 84.1 |
(NCT00451958)
Timeframe: From time of switch to Day 56
| Intervention | International units/Liter (IU/L) (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Day 3 | Day 7 | Day 14 | Day 28 | Day 56 | |
| Leuprolide 7.5 mg/ Degarelix 240/160 mg | 4.4 | 2.8 | 2.6 | 2.3 | 1.7 | 1.55 |
| Leuprolide 7.5 mg/ Degarelix 240/80 mg | 4.8 | 2.7 | 2.6 | 2.2 | 1.8 | 1.3 |
(NCT00451958)
Timeframe: From time of switch to Day 56
| Intervention | ng/mL (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Day 3 | Day 7 | Day 14 | Day 28 | Day 56 | |
| Leuprolide 7.5 mg/ Degarelix 240/160 mg | 0.4 | 0.3 | 0.4 | 0.3 | 0.5 | 0.4 |
| Leuprolide 7.5 mg/ Degarelix 240/80 mg | 0.4 | 0.4 | 0.35 | 0.4 | 0.4 | 0.35 |
Sleep quality was measured using the Pittsburgh Sleep Quality Index (PSQI; range 0-21, higher score indicates poorer quality sleep), which was administered both before and four weeks after receiving the intervention. (NCT00455689)
Timeframe: baseline (before receiving intervention) and 4 weeks after receiving intervention
| Intervention | units on a scale (Median) |
|---|---|
| Developed Hot Flashes | 2.5 |
| Did Not Develop Hot Flashes | 1.0 |
Objective sleep efficiency was measured using actigraphy. Sleep efficiency (percent of time spent asleep between bedtime and wake time) was calculated and averaged over 2 consecutive nights both before and 4 weeks after receiving the intervention. (NCT00455689)
Timeframe: baseline (before receiving intervention) and 4 weeks after receiving intervention
| Intervention | percent change (Median) |
|---|---|
| Developed Hot Flashes | -2.6 |
| Did Not Develop Hot Flashes | 4.2 |
Probability of response, defined as pathological complete remission based on tissue obtained at surgery. Pathological Complete Response (pCR): Patients without gross or microscopic evidence of residual disease at Radical Prostatectomy defined as pCR. (NCT00500110)
Timeframe: Every 3 months for 1 year, then every 6 months until disease progression or death
| Intervention | participants (Number) |
|---|---|
| Treatment | 0 |
FACT-P is a 39-item participant questionnaire which assesses physical well-being (7 items), social/family well-being (7 items), emotional well-being (6 items), functional well-being (7 items), and additional prostate cancer specific concerns (12 items). All items are scored from 0 (not at all) to 4 (very much). The total FACT-P score ranges from 0-156, with higher scores representing a better quality of life with fewer symptoms. A score of 156 represents the best outcome. (NCT00514917)
Timeframe: Baseline, EOT (up to Month 18)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline (n=206, 205) | Change at EOT (n=186, 184) | |
| Docetaxel+Leuprolide+Bicalutamide | 121.4 | -4.9 |
| Leuprolide+Bicalutamide | 119.6 | -3.4 |
EF-IIEF is a 6-item erectile function domain of IIEF. It consists of Question 1, 2, 3, 4, 5, and 15 of IIEF questionnaire. 5 questions are scored from 0 (no activity) to 5 (very high activity) and 1 question is scored from 1 (very low activity) to 5 (very high activity). Total EF-IIEF score ranges from 1 to 30, where higher score indicates high activity. (NCT00514917)
Timeframe: Baseline, EOT (up to Month 18)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline (n=201, 205) | Change at EOT (n=180, 186) | |
| Docetaxel+Leuprolide+Bicalutamide | 6.4 | -3.1 |
| Leuprolide+Bicalutamide | 6.8 | -3.3 |
TEAE: any adverse event (AE) that occurred or worsened during the on-treatment period, which was the period from first administration of study treatment until 30 days after last administration of study treatment. AE: any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. Serious AE: an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly, or medically important. Drug-related AEs were any untoward medical occurrences attributed to study drug in a participant who received study drug. National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 3.0 Grade 3 (severe) and Grade 4 (life threatening/disabling) TEAEs were also reported. (NCT00514917)
Timeframe: From first administration of study treatment until 30 days after the last administration of study treatment
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Any TEAE | Any Serious AE | Any TEAE Resulting in Death | Any TEAE Leading to any Treatment Discontinuation | Any Grade 3-4 TEAE | Docetaxel Related TEAE | Leuprolide Related TEAE | Bicalutamide Related TEAE | Any Treatment Related TEAE | Any Grade 3-4 Serious TEAE | Any TEAE Leading to Interruption of any Treatment | |
| Docetaxel+Leuprolide+Bicalutamide | 188 | 49 | 0 | 35 | 94 | 183 | 109 | 52 | 184 | 43 | 77 |
| Leuprolide+Bicalutamide | 163 | 20 | 1 | 1 | 22 | NA | 136 | 74 | 136 | 14 | 1 |
PFS rate at Month 36 was defined as probability of being progression-free at Month 36. PFS rate was estimated using the Kaplan-Meier method. (NCT00514917)
Timeframe: Month 36
| Intervention | percent chance of being progression-free (Number) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 15.8 |
| Leuprolide+Bicalutamide | 9.1 |
PFS rate at Month 36 was defined as probability of being progression-free at Month 36. PFS rate was estimated using the Kaplan-Meier method. (NCT00514917)
Timeframe: Month 36
| Intervention | percent chance of being progression-free (Number) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 15.5 |
| Leuprolide+Bicalutamide | 8.6 |
The OS was the time interval from the date of randomization to the date of death due to any cause. OS was to be analyzed using the Kaplan-Meier method. However, the analysis was not performed due to insufficient number of events. Reported is the number of participants who died from any cause. (NCT00514917)
Timeframe: Randomization until death due to any cause, assessed up to Month 60
| Intervention | participants (Number) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 4 |
| Leuprolide+Bicalutamide | 11 |
PFS was the time from randomization to the date of first documented PSA progression, or radiographic progression, or death due to prostate cancer in the absence of previous documentation of disease progression, whichever occurred first. Median PFS was estimated using the Kaplan-Meier method. (NCT00514917)
Timeframe: Randomization until PSA progression or radiographic progression or death due to prostate cancer, assessed up to Month 60
| Intervention | months (Median) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 25.7 |
| Leuprolide+Bicalutamide | 24.7 |
MAF scale consists of 16-items to measure 4 dimensions of fatigue during past week: severity (Item 1-2), distress (Item 3), degree of interference in activities of daily living (Item 4-14), and timing (Item 15-16). Item 1-14 are scored on a numeric rating scale from 1 to 10, where higher score indicate more severity/distress/interference. Item 15-16 had multiple choice responses (4 responses each). Scale Index was calculated using Item 1-15, in following steps: 1) Item 15 score converted to 1-10 scale by multiplying the score with 2.5; 2) Average score was calculated from Item 4-14; 3) Finally scale index was calculated by adding Items 1, 2, 3 scores with average score from step 2 and converted score of Item 15 from step 1. Total MAF scale index score ranges 1 (no fatigue) to 50 (severe fatigue). (NCT00514917)
Timeframe: Baseline, EOT (up to Month 18)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline (n=168, 171) | Change at EOT (n=127, 144) | |
| Docetaxel+Leuprolide+Bicalutamide | 16.4 | 4.0 |
| Leuprolide+Bicalutamide | 16.6 | 2.6 |
PFS was the time from randomization to the date of first documented prostate specific antigen (PSA) progression, or radiographic progression, or death due to prostate cancer in the absence of previous documentation of disease progression, whichever occurred first. PSA progression was determined as: a) During treatment period: a 50 percent (%) increase from baseline, which was confirmed by a second value; b) During follow-up: detectable PSA (defined as PSA greater than or equal to 0.05 nanogram per millimeter [ng/mL]), which was confirmed by consecutive observation (not less than 2 weeks apart). Median PFS was estimated using the Kaplan-Meier method. (NCT00514917)
Timeframe: Randomization until PSA progression or radiographic progression or death due to prostate cancer, assessed up to Month 60
| Intervention | months (Median) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 25.4 |
| Leuprolide+Bicalutamide | 23.3 |
The cancer-specific survival was the time from the date of randomization to the date of death due to prostate cancer. Cancer-specific survival was to be analyzed using the Kaplan-Meier method. However, the analysis was not performed due to insufficient number of events. Reported is the number of participants who died from prostate cancer. (NCT00514917)
Timeframe: Randomization until death due to prostate cancer, assessed up to Month 60
| Intervention | participants (Number) |
|---|---|
| Docetaxel+Leuprolide+Bicalutamide | 2 |
| Leuprolide+Bicalutamide | 3 |
Physical well-being, functional well-being, and prostate cancer concerns sub-scales of the FACT-P questionnaire were combined to calculate TOI. Total TOI score ranges from 0 to 104, with higher scores representing a better quality of life with fewer symptoms. (NCT00514917)
Timeframe: Baseline, EOT (up to Month 18)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Baseline (n=206, 206) | Change at EOT (n=187, 187) | |
| Docetaxel+Leuprolide+Bicalutamide | 82.1 | -5.4 |
| Leuprolide+Bicalutamide | 80.4 | -3.1 |
Treatment failures: Count and percent of patients NOT reaching PSA concentration in serum either below 4 ng/dl or below baseline before LHRH treatment . (NCT00544830)
Timeframe: Off-treatment PSA measurement date minus on-study PSA measurement date, up to 36 weeks.
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 15 |
Time from the date of the last dose of bicalutamide or the last day of radiation therapy (whichever comes later) until the date criteria are met for PSA relapse. PSA relapse after completion of initial 36 weeks of androgen deprivation therapy is defined as an increase in PSA value to above pre-therapy level, or to > 10, whichever is smaller. For example, a patient with pre-treatment PSA level of 40 will resume androgen deprivation therapy when PSA level is > 10, while a patient with pre-treatment PSA level of 3 will resume androgen deprivation therapy when PSA level is > 3. (NCT00544830)
Timeframe: End-of-therapy until PSA reached pre-treatment level or 10 (whichever was lower)
| Intervention | month (Median) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 16.5 |
Patients who remained off of therapy, in remission, out of the number of patients with metastases limited to pelvic lymph nodes. (NCT00544830)
Timeframe: after 36 week LHRH treatment window.
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 7 |
Number of patients remaining in complete remission without androgen deprivation therapy in patients with metastases limited to pelvic lymph nodes. (NCT00544830)
Timeframe: after 36 weeks of LHRH therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 4 |
Length of follow-up of the 8 patients with metastases limited to pelvic lymph nodes, months. Patients are followed on day one of each of three 12-week periods. After completion of therapy, patients are followed every four weeks until PSA relapse, up to 46.4 months. (NCT00544830)
Timeframe: Patients are followed on day one of each of three 12-week periods. After completion of therapy, patients are followed every four weeks until PSA relapse, up to 46.4 months.
| Intervention | month (Median) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 14.7 |
Length of follow-up in weeks to off-study date. Patients are treated for 36 weeks (+/- 2 weeks) with androgen deprivation therapy. Patients are evaluated for disease on day 1 of each of three 12-week cycles. After the last cycle of anti-androgen therapy, patients are assessed every four weeks until PSA relapse occurs, up to 264.8 weeks (61.4 months; 5.1 years). Patients will remain off-treatment until they meet the criteria for re-treatment with androgen deprivation therapy, whereupon they will be taken off of the protocol. After patients are taken off protocol, we will do a chart review for long-term outcomes. (NCT00544830)
Timeframe: Patients are evaluated for disease on day 1 of each of three 12-week cycles. After the last cycle of anti-androgen therapy, patients are assessed every four weeks until PSA relapse occurs, up to 61.4 months
| Intervention | week (Median) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 111.4 |
Number of Patients who achieved PSA nadir of < 0.2 at 36 weeks. (NCT00544830)
Timeframe: During the time period between on-study PSA to off-study PSA, up to 36 weeks.
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Androgen Therapy, Radiation Therapy) | 25 |
Cause-specific mortality (failure) is defined as death due to prostate cancer or complications of protocol treatment (centrally reviewed), or death following disease progression (clinical or biochemical) in the absence of or after the initiation of any salvage therapy. [Biochemical progression is indicated by any rise in PSA.] Failure time is defined as time from randomization to the date of failure, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but the data monitoring committee decided to release results after the third interim analysis. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 2.7 |
| PBRT + STAD | 1.1 |
| PLNRT + PBRT + STAD | 0.8 |
Progression is defined as the first occurrence of the following events: biochemical failure by the Phoenix definition (prostate-specific antigen [PSA] ≥ 2 ng/ml over the nadir PSA), clinical failure (local, regional or distant), or death from any cause. The initiation of second salvage therapy before progression was a protocol violation and resulted in censoring. Progression time is defined as time from randomization to the date of progression, second salvage therapy (censored), or last known follow-up (censored). Freedom from progression rates are estimated using the Kaplan-Meier method. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but results were reported early. See Limitations and Caveats section. (NCT00567580)
Timeframe: From randomization to five years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 70.3 |
| PBRT + STAD | 81.3 |
| PLNRT + PBRT + STAD | 87.4 |
Hormone-refractory disease (failure) is defined as three rises in PSA after the start of second salvage androgen deprivation therapy. Failure time is defined as time from randomization to the date of failure, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but the data monitoring committee decided to release results after the third interim analysis. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 2.9 |
| PBRT + STAD | 2.4 |
| PLNRT + PBRT + STAD | 1.2 |
Survival time is defined as time from randomization to the date of death from any cause or last known follow-up (censored). Survival rates are estimated by the Kaplan-Meier method. Pairwise comparisons of the overall distributions of failure times are reported in statistical analysis section, with five-year rates reported here. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but the data monitoring committee decided to release results after the third interim analysis. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 93.9 |
| PBRT + STAD | 96.1 |
| PLNRT + PBRT + STAD | 95.7 |
Local failure is defined as first occurrence of local clinical progression. Failure time is defined as time from randomization to the date of failure, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but the data monitoring committee decided to release results after the third interim analysis. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 3.1 |
| PBRT + STAD | 1.2 |
| PLNRT + PBRT + STAD | 0.4 |
Common Terminology Criteria for Adverse Events (version 3.0) grades adverse event severity from 1=mild to 5=death. Summary data is provided in this outcome measure; see Adverse Events Module for specific adverse event data. Pairwise comparisons of Arm 2 vs Arm 1 and Arm 3 vs. Arm 2 are reported in the statistical analysis. (NCT00567580)
Timeframe: From randomization to 90 days after completion of radiotherapy (approximately 7-8 weeks).
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Grade 2+ | Grade 3+ | |
| PBRT + STAD | 36.3 | 8.7 |
| PBRT Alone | 18.8 | 4.4 |
| PLNRT + PBRT + STAD | 43.6 | 12.2 |
Distant metastasis (failure) is defined as the occurrence of distant metastasis determined by imaging. Failure time is defined as time from randomization to the date of failure, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but the data monitoring committee decided to release results after the third interim analysis. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 8.3 |
| PBRT + STAD | 5.9 |
| PLNRT + PBRT + STAD | 4.7 |
Common Terminology Criteria for Adverse Events (version 3.0) grades adverse event severity from 1=mild to 5=death. Late adverse events (AE) are defined as occurring > 90 days from the completion of RT. Failure time is defined as time from randomization to the date of first late grade 2 or grade 3 adverse event, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times between Arm 2 and Arm 1 and between Arm 3 and Arm 2, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. (NCT00567580)
Timeframe: AE: from 91 days after completion of RT (approximately 7-8 weeks) to last follow-up. Vital status: from randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Grade 2+ | Grade 3+ | |
| PBRT + STAD | 54.8 | 11.4 |
| PBRT Alone | 52.8 | 10.3 |
| PLNRT + PBRT + STAD | 58.6 | 14.4 |
Secondary biochemical (failure) is defined as either of two occurrences: 1. For detectable post-baseline PSA values (≥ 0.1), the first occurrence of a PSA value that is both ≥ 0.4 and a second rise above nadir; 2.The start of second salvage therapy. Failure time is defined as time from randomization to the date of failure, death (competing risk), or last known follow-up (censored). Failure rates for data summary are estimated using the cumulative incidence method, with 5-year rates provided here. Pairwise comparisons of the distributions of failure times, reported in the statistical analysis section, use cause-specific hazard rates for which deaths are censored. The study was designed for the final analysis to occur after all participants had been on study for at least 5 years, but results were reported early. See Limitations and Caveats section. (NCT00567580)
Timeframe: From randomization to last follow-up. Maximum follow-up at time of analysis was 10.5 years.
| Intervention | percentage of participants (Number) |
|---|---|
| PBRT Alone | 35.7 |
| PBRT + STAD | 22.3 |
| PLNRT + PBRT + STAD | 14.5 |
Immune markers were measured by isolating gamma-delta T cells one month after treatment with zoledronic acid. (NCT00582556)
Timeframe: 2 Years
| Intervention | participants (Number) |
|---|---|
| Zometa Given 7 Days Prior to Beginning ADT | 0 |
| Zometa Given at Month 6 | 0 |
| Zometa Given Monthly, Months 6-11 | 0 |
"PSA response was measured by observing the serum PSA one week after beginning zoledronic acid and prior to beginning androgen deprivation therapy.~Arm 2 and Arm 3 were not able to be assessed for this endpoint as all subjects were on androgen deprivation prior to receiving zoledronic acid." (NCT00582556)
Timeframe: 2 Years
| Intervention | participants (Number) |
|---|---|
| Zometa Given 7 Days Prior to Beginning ADT | 0 |
Serum bone-specific alkaline phosphatase was collected as the blood marker of bone turnover. (NCT00582556)
Timeframe: 2 years
| Intervention | participants (Number) |
|---|---|
| Zometa Given 7 Days Prior to Beginning ADT | 0 |
| Zometa Given at Month 6 | 0 |
| Zometa Given Monthly, Months 6-11 | 0 |
Effects on bone mineral density were measured at four locations at six month intervals for 24 months. (NCT00582556)
Timeframe: 2 years
| Intervention | participants (Number) |
|---|---|
| Zometa Given 7 Days Prior to Beginning ADT | 14 |
| Zometa Given at Month 6 | 15 |
| Zometa Given Monthly, Months 6-11 | 15 |
Docetaxel Pharmacokinetic parameters for cycles 1 and 2. (NCT00587431)
Timeframe: at Cycle 1 and 2
| Intervention | L/hr (Mean) | |
|---|---|---|
| Docetaxel clearance (Cycle 1) | Docetaxel clearance (Cycle 2) | |
| All Participants | 23.9 | 23.6 |
(NCT00587431)
Timeframe: Conclusion of the study (at 6 months then at 18 months post-treatment)
| Intervention | participants (Number) | |
|---|---|---|
| at 6 months post-treatment | at 18 months post-treatment | |
| Lupron + Docetaxel (70 mg/m2) + Testosterone (Metastatic) | 12 | 2 |
| Lupron + Docetaxel (75mg/m2) + Testosterone for (Metastatic) | 14 | 0 |
| Lupron + Docetaxel (75mg/m2) +Testosterone (RISING PSA) | 9 | 0 |
| Lupron +Docetaxel (70 mg/m2) +Testosterone (RISING PSA) | 13 | 3 |
A Gleason score is the sum of two numbers. Pathologist determines where the cancer is most prominent and assigns the primary grade, the secondary grade is assigned based on where the cancer is next most prominent. A score from one to five is assigned for each area based on how aggressive the tumor appears. A tumor with cell that appear close to normal is assigned a low Gleason score (six or below). A tumor with cells that appear clearly different from those of a normal prostate is assigned a high Gleason score (seven or above). A system of grading prostate cancer tissue based on how it looks under a microscope. Gleason scores range from 2 to 10 and indicate how likely it is that a tumor will spread. A low Gleason score means the cancer tissue is similar to normal prostate tissue and the tumor is less likely to spread; a high Gleason score means the cancer tissue is very different from normal and the tumor is more likely to spread. (NCT00589472)
Timeframe: Baseline
| Intervention | units on a scale (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 8 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 256 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | mcg/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 90 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 24 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/mL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 9.44 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 319 |
Number of patients who responded to controlled ovarian stimulation as evidenced by implantation of embryo. Implantation confirmed by ultrasound at 6 1/2 weeks of pregnancy. (NCT00621179)
Timeframe: Evaluated at 6 1/2 weeks of pregnancy which is 4 weeks post embryo transfer.
| Intervention | Participants (Count of Participants) |
|---|---|
| Group 1 | 7 |
| Group 2 | 5 |
| Group 3 | 3 |
| Group 4 | 5 |
The adjusted percentage of subjects with testosterone suppression (<= 50 ng/dL) from Week 4 to Week 48 was calculated by the Kaplan-Meier method for right-censored observations. The primary efficacy analysis was adjusted to censor subjects who received an anti-androgen at the last testosterone measurement before use of the anti-androgen. One additional subject was censored because of a laboratory error, at the last measurement before the error. The adjusted 90% 2-sided confidence interval was calculated from Kaplan-Meier estimates. (NCT00626431)
Timeframe: Week 4 to Week 48
| Intervention | Percent Suppressed (Number) |
|---|---|
| Leuprolide Acetate - Formulation A | 93.4 |
The percentage of subjects with testosterone suppression (<= 50 ng/dL) from Week 4 to Week 48 was calculated by the Kaplan-Meier method for right-censored observations. Subjects who failed testosterone suppression were considered failures on the first day of a testosterone measurement (>50 ng/dL). Subjects who prematurely discontinued without escaping and those who were successfully suppressed through Week 48 were censored at their last measured testosterone value (Day 337 to Day 340 at Week 48). The 90% 2-sided confidence interval was calculated from Kaplan-Meier estimates. (NCT00626431)
Timeframe: Week 4 to Week 48
| Intervention | Percent suppressed (Number) |
|---|---|
| Leuprolide Acetate - Formulation B | 86.9 |
The acute-on-chronic effect is an agonistic stimulation of luteinizing hormone after the second depot injection of Formulation A. The mean +/- standard error changes were measured to assess this effect from just before to 2 weeks after the second injection. (NCT00626431)
Timeframe: Week 24 before the second injection until 2 weeks after Week 24 (2 h, 4 h, 8 h, 1 d, 2 d, 3-10 d, and 11-17 d postdose)
| Intervention | ng/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Testosterone concentration at 2 hours postdose | Testosterone concentration at 4 hours postdose | Testosterone concentration at 8 hours postdose | Testosterone concentration at Day 1 postdose | Testosterone concentration at Day 2 postdose | Testosterone concentration at Days 3-10 postdose | Testosterone concentration at Days 11-17 postdose | |
| Leuprolide Acetate - Formulation A | 0.2 | 0.2 | 0.2 | 0.2 | 0.1 | 0.1 | 0.1 |
Baseline was the last measurement before the first dose of Formulation B. The mean +/- standard error was calculated at each visit. The final visit occurred at Week 48 unless the subject prematurely discontinued the study. (NCT00626431)
Timeframe: Baseline, Days 2 and 8, Weeks 2, 4, 8, 14, 20, 24, 26, 30, 34, 40, 46, 48, and Final Visit
| Intervention | ng/dL (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Testosterone concentration at baseline | Testosterone concentration at Day 2 | Testosterone concentration at Day 8 | Testosterone concentration at Week 2 | Testosterone concentration at Week 4 | Testosterone concentration at Week 8 | Testosterone concentration at Week 14 | Testosterone concentration at Week 20 | Testosterone concentration at Week 24 | Testosterone concentration at Week 26 | Testosterone concentration at Week 30 | Testosterone concentration at Week 34 | Testosterone concentration at Week 40 | Testosterone concentration at Week 46 | Testosterone concentration at Week 48/Final Visit | |
| Leuprolide Acetate - Formulation B | 414.0 | 578.0 | 466.9 | 127.4 | 15.3 | 9.1 | 8.9 | 9.6 | 28.0 | 15.6 | 9.4 | 9.7 | 9.5 | 9.4 | 13.8 |
The acute-on-chronic effect is an agonistic stimulation of luteinizing hormone after the second depot injection of Formulation B. The mean +/- standard error changes were measured to assess this effect from just before to 2 weeks after the second injection. (NCT00626431)
Timeframe: Week 24 before the second injection until 2 weeks after Week 24 (2 h, 4 h, 8 h, 1 d, 2 d, 3-10 d, and 11-17 d postdose)
| Intervention | ng/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Testosterone concentration at 2 hours postdose | Testosterone concentration at 4 hours postdose | Testosterone concentration at 8 hours postdose | Testosterone concentration at Day 1 postdose | Testosterone concentration at Day 2 postdose | Testosterone concentration at Days 3-10 postdose | Testosterone concentration at Days 11-17 postdose | |
| Leuprolide Acetate - Formulation B | 0.4 | 0.5 | 0.4 | 0.4 | 0.2 | 0.1 | -0.1 |
The acute-on-chronic effect is an agonistic stimulation of serum testosterone after the second depot injection of Formulation A. The mean +/- standard error changes were measured to assess this effect from just before to 2 weeks after the second injection. (NCT00626431)
Timeframe: Week 24 before the second injection until 2 weeks after Week 24 (2 hours [h], 4 h, 8 h, 1 day [d], 2 d, 3-10 d, and 11-17 d postdose)
| Intervention | ng/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Testosterone concentration at 2 hours postdose | Testosterone concentration at 4 hours postdose | Testosterone concentration at 8 hours postdose | Testosterone concentration at Day 1 postdose | Testosterone concentration at Day 2 postdose | Testosterone concentration at Days 3-10 postdose | Testosterone concentration at Days 11-17 postdose | |
| Leuprolide Acetate - Formulation A | -1.9 | -1.2 | -1.3 | -0.1 | -0.1 | -1.0 | -2.1 |
The acute-on-chronic effect is an agonistic stimulation of serum testosterone after the second depot injection of Formulation B. The mean +/- standard error changes were measured to assess this effect from just before to 2 weeks after the second injection. (NCT00626431)
Timeframe: Week 24 before the second injection until 2 weeks after Week 24 (2 h, 4 h, 8 h, 1 d, 2 d, 3-10 d, and 11-17 d postdose)
| Intervention | ng/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Testosterone concentration at 2 hours postdose | Testosterone concentration at 4 hours postdose | Testosterone concentration at 8 hours postdose | Testosterone concentration at Day 1 postdose | Testosterone concentration at Day 2 postdose | Testosterone concentration at Days 3-10 postdose | Testosterone concentration at Day 11-17 postdose | |
| Leuprolide Acetate - Formulation B | -0.7 | 1.6 | 3.6 | 8.0 | 7.8 | 4.5 | -4.2 |
PSA levels were measured at baseline and each treatment visit for Formulation A. The mean (+/- standard error) was calculated at each visit. The final visit occurred at Week 48 unless the subject prematurely discontinued the study. (NCT00626431)
Timeframe: Baseline, Day 8, Week 14, Week 24, Week 30, Week 40, Week 48, and the Final Visit
| Intervention | ng/mL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| PSA concentration at baseline | PSA Concentration at Day 8 | PSA Concentration at Week 14 | PSA Concentration at Week 24 | PSA Concentration at Week 30 | PSA Concentration at Week 40 | PSA Concentration at Week 48/Final Visit | |
| Leuprolide Acetate - Formulation A | 35.0 | 40.4 | 2.4 | 2.9 | 1.6 | 2.2 | 3.7 |
PSA levels were measured at baseline and each treatment visit for Formulation B. The mean (+/- standard error) was calculated at each visit. The final visit occurred at Week 48 unless the subject prematurely discontinued the study. (NCT00626431)
Timeframe: Baseline, Day 8, Week 14, Week 24, Week 30, Week 40, Week 48, and the Final Visit
| Intervention | ng/mL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| PSA concentration at baseline | PSA Concentration at Day 8 | PSA Concentration at Week 14 | PSA Concentration at Week 24 | PSA Concentration at Week 30 | PSA Concentration at Week 40 | PSA Concentration at Week 48/Final Visit | |
| Leuprolide Acetate - Formulation B | 20.5 | 23.1 | 2.4 | 2.5 | 2.7 | 2.5 | 6.2 |
Baseline was the last measurement before the first dose of Formulation A. The mean +/- standard error was calculated at each visit. The final visit occurred at Week 48 unless the subject prematurely discontinued the study. (NCT00626431)
Timeframe: Baseline, Days 2 and 8, Weeks 2, 4, 8, 14, 20, 24, 26, 30, 34, 40, 46, 48, and Final Visit
| Intervention | ng/dL (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Testosterone concentration at baseline | Testosterone concentration at Day 2 | Testosterone concentration at Day 8 | Testosterone concentration at Week 2 | Testosterone concentration at Week 4 | Testosterone concentration at Week 8 | Testosterone concentration at Week 14 | Testosterone concentration at Week 20 | Testosterone concentration at Week 24 | Testosterone concentration at Week 26 | Testosterone concentration at Week 30 | Testosterone concentration at Week 34 | Testosterone concentration at Week 40 | Testosterone concentration at Week 46 | Testosterone concentration at Week 48/Final Visit | |
| Leuprolide Acetate - Formulation A | 432.9 | 613.1 | 468.2 | 127.1 | 16.0 | 9.6 | 9.2 | 8.5 | 14.3 | 9.0 | 9.9 | 13.0 | 8.8 | 8.8 | 13.3 |
The percentage of subjects with testosterone suppression (<= 50 ng/dL) from Week 4 to Week 48 was calculated by the Kaplan-Meier method for right-censored observations. Subjects who failed testosterone suppression were considered failures on the first day of a testosterone measurement (>50 ng/dL). Subjects who prematurely discontinued without escaping and those who were successfully suppressed through Week 48 were censored at their last measured testosterone value (Day 337 to Day 340 at Week 48). The 90% 2-sided confidence interval was calculated from Kaplan-Meier estimates. (NCT00626431)
Timeframe: Week 4 to Week 48
| Intervention | Percent Suppressed (Number) |
|---|---|
| Leuprolide Acetate - Formulation A | 93.6 |
Percentage of participants with suppression of testosterone, out of the number of boys with at least 1 testosterone measurement at each visit (n/N%). Only boys are analyzed in this outcome measure. Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Month 1, 2, 3 and 6
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| Mo 1 (Arm A N=2, B N=1, C N=2, D N=3) | Mo 2 (Arm A N=2, B N=1, C N=2, D N=3) | Mo 3 (Arm A N=2, B N=1, C N=2, D N=3) | Mo 6 (Arm A N=1, B N=1, C N=2, D N=3) | |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 100 | 100 | 100 | 100 |
| Leuprolide Acetate 11.25 mg - Treatment Naive | 50.0 | 50.0 | 50.0 | 100 |
| Leuprolide Acetate 30 mg - Previous Treatment | 100 | 100 | 100 | 100 |
| Leuprolide Acetate 30 mg - Treatment Naive | 100 | 100 | 100 | 100 |
Percentage of participants with suppression of estradiol, out of the number of girls with at least 1 estradiol measurement at each visit (n/N%). Only girls are analyzed in this outcome measure. Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Month 1, 2, 3 and 6
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| Mo 1 (Arm A N=17, B N=18, C N=19, D N=16) | Mo 2 (Arm A N=19, B N=14, C N=19, D N=14) | Mo 3 (Arm A N=15, B N=18, C N=17, D N=18) | Mo 6 (Arm A N=12, B N=16, C N=15, D N=17) | |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 100 | 100 | 100 | 93.8 |
| Leuprolide Acetate 11.25 mg - Treatment Naive | 100 | 94.7 | 100 | 100 |
| Leuprolide Acetate 30 mg - Previous Treatment | 100 | 100 | 100 | 100 |
| Leuprolide Acetate 30 mg - Treatment Naive | 100 | 100 | 100 | 100 |
Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Baseline, Month 1, 2, 3 and 6
| Intervention | mIU/mL (Mean) | ||||
|---|---|---|---|---|---|
| Baseline (Arm A N=21, B N=21, C N=21, D N=21) | Mo 1 (Arm A N=21, B N=21, C N=21, D N=21) | Mo 2 (Arm A N=21, B N=20, C N=21, D N=20) | Mo 3 (Arm A N=16, B N=20, C N=20, D N=21) | Mo 6 (Arm A N=15, B N=18, C N=18, D N=21) | |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 1.8 | 1.7 | 2.0 | 1.8 | 2.5 |
| Leuprolide Acetate 11.25 mg - Treatment Naive | 45.9 | 4.4 | 4.5 | 2.3 | 2.0 |
| Leuprolide Acetate 30 mg - Previous Treatment | 1.7 | 1.4 | 1.5 | 1.5 | 1.5 |
| Leuprolide Acetate 30 mg - Treatment Naive | 23.5 | 1.9 | 2.0 | 1.4 | 1.6 |
The growth rate at baseline was the growth rate during the last year before the start of treatment and was calculated with the measurement closest to Day -336 (before Day -30) and the measurement up to Day 1. Growth rate at Month 6 was defined as the ratio of the change in height from Day 1 to the change in chronological age, with an approximate 6-month interval between the 2 height measurements. Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Baseline and Month 6
| Intervention | cm/year (Mean) | |
|---|---|---|
| Baseline (Arm A N=20, B N=21, C N=21, D N=21) | Mo 6 (Arm A N=14, B N=19, C N=19, D N=21) | |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 6.58 | -0.98 |
| Leuprolide Acetate 11.25 mg - Treatment Naive | 7.25 | -2.51 |
| Leuprolide Acetate 30 mg - Previous Treatment | 6.05 | -0.91 |
| Leuprolide Acetate 30 mg - Treatment Naive | 7.83 | -2.34 |
The ratio at Month 6 was calculated as (bone age at Month 6 - bone age at baseline)/(chronological age at Month 6 - chronological age at baseline). Observed data were used with no imputation for missing data. Baseline bone-age radiograph was performed at or within 3 months of the Screening Visit. (NCT00635817)
Timeframe: Baseline to Month 6
| Intervention | Ratio (Mean) |
|---|---|
| Leuprolide Acetate 11.25 mg - Treatment Naive | 0.59 |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 0.50 |
| Leuprolide Acetate 30 mg - Treatment Naive | 1.00 |
| Leuprolide Acetate 30 mg - Previous Treatment | 1.07 |
Percentage of participants with suppression of genital development and testicular volume, out of the number of boys with pubertal staging of genital development or testicular volume (n/N%). Only boys are analyzed in this outcome measure. External genital development (testes and penis) was rated from Stage 1 (early development) through Stage 5 (full development) according to a Tanner Staging pictogram. Boys entering the study with fully developed genitals (Stage 5) were excluded from this analysis. Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Month 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprolide Acetate 11.25 mg - Treatment Naive | 100 |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 0 |
| Leuprolide Acetate 30 mg - Treatment Naive | 50 |
| Leuprolide Acetate 30 mg - Previous Treatment | 33.3 |
Percentage of participants with suppression of breast development, out of the number of girls with pubertal staging of breast development (n/N%). Only girls are analyzed in this outcome measure. Breast development was rated from Stage 1 (early development) through Stage 5 (full development) according to a Tanner Staging pictogram. Girls entering the study with fully developed breasts (Stage 5) were excluded from this analysis. Observed data were used with no imputation for missing data. (NCT00635817)
Timeframe: Month 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprolide Acetate 11.25 mg - Treatment Naive | 92.9 |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 88.9 |
| Leuprolide Acetate 30 mg - Treatment Naive | 82.4 |
| Leuprolide Acetate 30 mg - Previous Treatment | 82.4 |
Percentage of participants with suppression of peak stimulated luteinizing hormone that was measured after a gonadotropin-releasing hormone agonist (GnRHa) stimulation test at Month (Mo) 2, 3, and 6. The analysis was performed according to a life table method. Subjects who withdrew without peak-stimulated luteinizing hormone >= 4 mIU/mL were censored at their last measurement of peak-stimulated luteinizing hormone. (NCT00635817)
Timeframe: Month 2 through 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprolide Acetate 11.25 mg - Treatment Naive | 76.2 |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 80.7 |
| Leuprolide Acetate 30 mg - Treatment Naive | 90.5 |
| Leuprolide Acetate 30 mg - Previous Treatment | 100 |
The ratio at baseline or Month 6 was calculated as bone age at baseline or Month 6/chronological age at baseline or Month 6. The percentage of participants with a decrease in the ratio was calculated as a simple percentage for each dose group. Observed data were used with no imputation for missing data. The baseline time frame was increased from the secondary outcome in this analysis to include all participants with a bone age radiograph at screening. This analysis was performed after the clinical study report was completed & is included to match the FDA package insert. (NCT00635817)
Timeframe: Baseline to Month 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprolide Acetate 11.25 mg | 87.9 |
| Leuprolide Acetate 30 mg | 75.0 |
Percentage of participants with suppression of peak stimulated luteinizing hormone that was measured after a GnRHa stimulation test at Mo 2, 3, and 6. A simple percentage and binomial exact confidence intervals were used in this analysis. Participants who withdrew with luteinizing hormone that remained suppressed were counted as a success. This analysis was performed after the clinical study report was completed and is included to match the FDA package insert. (NCT00635817)
Timeframe: Month 2 through 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprolide Acetate 11.25 mg - Treatment Naive | 76.2 |
| Leuprolide Acetate 11.25 mg - Previous Treatment | 81.0 |
| Leuprolide Acetate 30 mg - Treatment Naive | 90.5 |
| Leuprolide Acetate 30 mg - Previous Treatment | 100.0 |
Mean stimulated testosterone concentrations were assessed according to the DELFIA (registered trademark) assay. The final visit for measurement of testosterone occurred at a mean age +/- SD of 12.34 +/- 1.16 (range, 11.14 to 14.07) years. (NCT00660010)
Timeframe: Baseline, Weeks 4, 12, 24, 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | ng/dL (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Mean stimulated testosterone at baseline N=6 | Mean stimulated testosterone at Week 4 N=6 | Mean stimulated testosterone at Week 12 N=6 | Mean stimulated testosterone at Week 24 N=6 | Mean stimulated testosterone at Week 48 N=6 | Mean stimulated testosterone at Week 96 N=6 | Mean stimulated testosterone at Week 144 N=5 | Mean stimulated testosterone at Week 192 N=4 | Mean stimulated testosterone at Week 240 N=3 | Mean stimulated testosterone at Final Visit N=6 | |
| Leuprolide Acetate 1 Month Depot | 347.7 | 18.0 | 14.2 | 13.8 | 17.3 | 24.8 | 21.6 | 24.0 | 25.3 | 24.2 |
Regular menses was defined as 3 or more consecutive days of menstrual-like bleeding and was defined by the investigator's clinical judgment. (NCT00660010)
Timeframe: Posttreatment during the follow-up period (subjects observed every 6 months until physical and laboratory observations are at pubertal levels)
| Intervention | years (Mean) | |
|---|---|---|
| Time to regular menses | Age at regular menses | |
| Leuprolide Acetate 1 Month Depot | 1.5 | 12.9 |
Subjects were required to complete final adult questionnaire to provide information on adult reproductive function. Regular menses was defined as 3 or more consecutive days of menstrual-like bleeding. (NCT00660010)
Timeframe: Posttreatment data were collected from the final adult questionnaire (subjects >= 18 years of age)
| Intervention | Subjects (Number) | |
|---|---|---|
| No. of subjects with regular menses as adults | No. of subjects without regular menses as adults | |
| Leuprolide Acetate 1 Month Depot | 16 | 4 |
The final questionnaire was completed by 20 female subjects who were at least 18 years of age. The total number of pregnancies were reported. (NCT00660010)
Timeframe: Posttreatment data were collected from the final adult questionnaire (subjects >= 18 years of age)
| Intervention | Pregnancies (Number) | ||
|---|---|---|---|
| Number of pregnancies | Number of live births | Number of miscarriages | |
| Leuprolide Acetate 1 Month Depot | 12 | 6 | 5 |
The final questionnaire was completed by 20 females who were at least 18 years of age. The subjects reported on total number of pregnancies resulting in live births or number of miscarriages (spontaneous or elective) and whether the subject was currently pregnant. (NCT00660010)
Timeframe: Posttreatment data were collected from the final adult questionnaire (subjects >= 18 years of age)
| Intervention | Subjects (Number) | |
|---|---|---|
| Number of subjects who reported being pregnant | Number of subjects who were currently pregnant | |
| Leuprolide Acetate 1 Month Depot | 7 | 1 |
Suppression of clinical sexual characteristics was defined as regression (improvement) or no progression of breast development in females. Tanner staging is a scale of physical development that defines primary and secondary sex characteristics including size of breasts. The final visit occurred at a mean age +/- SD of 11.05 +/- 1.14 years (range, 6.96 to 12.95 years). (NCT00660010)
Timeframe: Week 4, Week 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | Percentage of subjects (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Breast development suppression - Week 4 N=44 | Breast development suppression-Week 48 N=47 | Breast development suppression -Week 96 N=41 | Breast development suppression-Week 144 N=29 | Breast development suppression - Week 192 N=18 | Breast development suppression -Week 240 N=13 | Breast development suppression-Final Visit N=48 | |
| Leuprolide Acetate 1 Month Depot | 81.8 | 80.9 | 87.8 | 82.8 | 66.7 | 76.9 | 77.1 |
Suppression of clinical sexual characteristics was defined as regression (improvement) or no progression of genital development in males. Tanner staging is a scale of physical development that defines primary and secondary sex characteristics including size of genitals. The final visit occurred at a mean age +/- SD of 12.35 +/-1.35 years (range, 10.71 to 14.07 years). (NCT00660010)
Timeframe: Week 4, Week 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | Percentage of subjects (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Genital development suppression - Week 4 N=5 | Genital development suppression - Week 48 N=6 | Genital development suppression - Week 96 N=6 | Genital development suppression - Week 144 N=4 | Genital development suppression - Week 192 N=4 | Genital development suppression - Week 240 N=3 | Genital development suppression - Final Visit N=6 | |
| Leuprolide Acetate 1 Month Depot | 80.0 | 83.3 | 83.3 | 75.0 | 75.0 | 66.7 | 83.3 |
Height was measured by stadiometer and was standardized for age according to standard growth charts. A standardized score of 0 indicated a mean ht. equivalent to mean of a standard population from 2000 CDC standardized ht. charts. Height gain was calculated as ht. - predicted ht. from the Bayley-Pinneau method on the basis of bone age at baseline. Final adult ht. was determined by measurement at final adult ht., if available, or by ht. collected during the follow-up period associated with a growth velocity <1 cm/year or a bone age >14 yrs in females or >15 yrs in males. (NCT00660010)
Timeframe: Final ht. (measured or provided for final questionnaire in subjects >= 18 years of age) or near final adult ht. (<1 cm/year or bone age > 14 years for females or > 15 years for males)
| Intervention | cm (Mean) | |||
|---|---|---|---|---|
| Near final adult ht. standardized score N=33 | Near final ht.gain from predicted ht. at BL N=29 | Final adult ht.standardized score N=19 | Final adult ht.gain from predicted ht. at BL N=17 | |
| Leuprolide Acetate 1 Month Depot | -0.2 | 3.2 | 0.0 | 3.9 |
Mean peak stimulated visit LH and FSH concentrations were assessed according to the DELFIA (registered trademark) assay. The final visit for measurement of both hormone concentrations occurred at a mean age +/- SD of 11.13 +/- 1.23 (range, 6.73 to 14.07) years. (NCT00660010)
Timeframe: Baseline, Weeks 4, 12, 24, 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | mIU/mL (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Peak stimulated LH at Baseline N=55 | Peak stimulated LH at Week 4 N = 55 | Peak stimulated LH at Week 12 N = 54 | Peak stimulated LH at Week 24 N = 53 | Peak stimulated LH at Week 48 N = 54 | Peak stimulated LH at Week 96 N = 46 | Peak stimulated LH at Week 144 N = 36 | Peak stimulated LH at Week 192 N = 20 | Peak stimulated LH at Week 240 N = 17 | Peak stimulated LH at Final Visit N = 55 | Peak stimulated FSH at Baseline N=55 | Peak stimulated FSH at Week 4 N = 55 | Peak stimulated FSH at Week 12 N = 54 | Peak stimulated FSH at Week 24 N = 53 | Peak stimulated FSH at Week 48 N = 54 | Peak stimulated FSH at Week 96 N = 46 | Peak stimulated FSH at Week 144 N = 36 | Peak stimulated FSH at Week 192 N = 20 | Peak stimulated FSH at Week 240 N = 17 | Peak stimulated FSH at Final Visit N = 55 | |
| Leuprolide Acetate 1 Month Depot | 35.0 | 0.8 | 1.1 | 0.8 | 0.6 | 0.4 | 0.4 | 0.4 | 0.4 | 0.8 | 13.3 | 0.9 | 1.1 | 1.2 | 1.2 | 1.4 | 1.4 | 1.3 | 1.4 | 1.7 |
Bone age was determined by radiography of the wrist according to the Fels Method. The mean ratio of bone age to chronological age provides information about the slowing of bone age progression. A score = 1 indicates that bone age is equal to chronological age. (NCT00660010)
Timeframe: Week 24 and Week 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | ratio (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Ratio at Baseline N=53 | Ratio at Week 24 N=53 | Ratio at Week 48 N=51 | Ratio at Week 96 N=44 | Ratio at Week 144 N=31 | Ratio at Week 192 N=26 | Ratio at Week 240 N=16 | Ratio at Final Visit N=53 | |
| Leuprolide Acetate 1 Month Depot | 1.5 | 1.5 | 1.4 | 1.3 | 1.2 | 1.2 | 1.2 | 1.2 |
Mean estradiol concentrations were assessed according to the DELFIA (registered trademark) assay. The lower limit of quantitation for estradiol is 5 pg/mL and measurements below this limit are given a value of 5 pg/mL. The final visit for measurement estradiol concentrations occurred at a mean age +/- SD of 10.93 +/- 1.27 (range, 5.59 to 13.24) years. (NCT00660010)
Timeframe: Baseline, Weeks 4, 12, 24, 48 (Year 1), yearly for 5 years (Week 240), and Final Visit
| Intervention | pg/mL (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Mean stimulated estradiol at baseline N=49 | Mean stimulated estradiol at Week 4 N=48 | Mean stimulated estradiol at Week 12 N=47 | Mean stimulated estradiol at Week 24 N=47 | Mean stimulated estradiol at Week 48 N=47 | Mean stimulated estradiol at Week 96 N=39 | Mean stimulated estradiol at Week 144 N=31 | Mean stimulated estradiol at Week 192 N=15 | Mean stimulated estradiol at Week 240 N=13 | Mean stimulated estradiol at Final Visit N=49 | |
| Leuprolide Acetate 1 Month Depot | 15.3 | 5.0 | 6.0 | 5.0 | 5.0 | 5.0 | 5.0 | 5.0 | 5.0 | 5.0 |
Baseline growth rate was the growth rate in the one year prior to Day 1 of the lead-in study L-CP07-167. Growth rates were calculated as the ratio of the change in height to the change in chronological age with an approximate 6-month interval for Day 1, Months 6, 12, 18, 24, 30, 36 and the Final Treatment Visit. (NCT00667446)
Timeframe: Baseline (the 1 year prior to the start of treatment in the lead-in study), and Day 1, Months 6, 12, 18, 24, 30, and 36
| Intervention | cm/year (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline [N=32, 38] | Change from Baseline at Day 1 [N=32, 38] | Change from Baseline at Month 6 [N=32, 37] | Change from Baseline at Month 12 [N=28, 32] | Change from Baseline at Month 18 [N=18, 23] | Change from Baseline at Month 24 [N=15, 19] | Change from Baseline at Month 30 [N=11, 17] | Change from Baseline at Month 36 [N=8, 13] | Change from Baseline at Final Visit [N=32, 38] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 7.2 | -1.67 | -1.66 | -1.99 | -2.21 | -2.36 | -1.86 | -2.64 | -2.27 |
| Leuprolide Acetate 3M Depot 30 mg | 7.53 | -1.65 | -2.04 | -2.28 | -2.06 | -1.59 | -2.13 | -2.19 | -2.64 |
Peak-stimulated luteinizing hormone refers to the maximum luteinizing hormone concentration measured 30 and 60 minutes after a gonadotropin-releasing hormone agonist (GnRHa) stimulation test. Final visit is the participant's last visit closest to Month 36. (NCT00667446)
Timeframe: Baseline of the lead-in study L-CP07-167, Day 1, Months 6, 12, 24, and 36
| Intervention | mIU/mL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Baseline [N=33, 38] | Day 1 [N=32, 37] | Month 6 [N=32, 36] | Month 12 [N=31, 32] | Month 24 [N=14, 18] | Month 36 [N=7, 11] | Final Visit [N=33, 36] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 21.89 | 2.00 | 2.22 | 2.24 | 1.67 | 1.51 | 1.81 |
| Leuprolide Acetate 3M Depot 30 mg | 10.16 | 1.49 | 1.62 | 1.58 | 0.88 | 0.91 | 1.15 |
"The percentage of female participants with suppression of basal estradiol to prepubertal levels, defined as estradiol < 20 pg/mL.~The estradiol assay was changed in June of 2010, and the lower limit of quantitation (LLOQ) was increased from 1 pg/mL to 10 pg/mL. This outcome measure reports data for assays performed before this change occurred, with an LLOQ of 1 pg/mL. Final visit is the participant's last visit closest to Month 36." (NCT00667446)
Timeframe: Day 1, Months 3, 6, 9, 12, and 24
| Intervention | percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Day 1 [N=28, 30] | Month 3 [N=29, 33] | Month 6 [N=26, 25] | Month 9 [N=18, 18] | Month 12 [N=10, 12] | Month 24 [N=1, 0] | Final Visit [N=31, 33] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 96.4 | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 |
| Leuprolide Acetate 3M Depot 30 mg | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 | NA | 100.0 |
"The percentage of female participants with suppression of basal estradiol to prepubertal levels, defined as estradiol < 20 pg/mL.~The estradiol assay was changed in June of 2010, and the lower limit of quantitation (LLOQ) was increased from 1 pg/mL to 10 pg/mL. This outcome measure reports data for assays performed after this change occurred, with an LLOQ of 10 pg/mL. Final visit is the participant's last visit closest to Month 36." (NCT00667446)
Timeframe: Months 6, 9, 12, 24, 30, and 36
| Intervention | percentage of participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Month 6 [N=4, 6] | Month 9 [N=13, 10] | Month 12 [N=20, 15] | Month 24 [N=14, 15] | Month 30 [N=9, 15] | Month 36 [N=7, 11] | Final Visit [N=24, 26] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 100.0 | 61.5 | 45.0 | 50.0 | 33.3 | 28.6 | 29.2 |
| Leuprolide Acetate 3M Depot 30 mg | 83.3 | 40.0 | 60.0 | 53.3 | 26.7 | 36.4 | 30.8 |
The percentage of female participants with suppression of breast development. Breast development was rated from Stage 1 (early development) through Stage 5 (full development) according to a modified Tanner Staging pictogram. Suppression of breast development is defined as regression or no progression of breast development from Baseline (of the lead-in study L-CP07-167) according to pubertal staging. Girls entering the study with fully developed breasts (Stage 5) were excluded from this analysis. Final visit is the participant's last visit closest to Month 36. (NCT00667446)
Timeframe: Baseline (of the lead-in study L-CP07-167), Day 1, Months 3, 6, 9, 12, 18, 24, 30, and 36
| Intervention | percentage of participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Day 1 [N= 31, 31] | Month 3 [N=29, 31] | Month 6 [N=31, 30] | Month 9 [N=31, 28] | Month 12 [N=28, 26] | Month 18 [N=17, 20] | Month 24 [N=14, 16] | Month 30 [N=10, 16] | Month 36 [N=8, 12] | Final Visit [N=31, 31] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 90.3 | 86.2 | 90.3 | 87.1 | 85.7 | 82.4 | 78.6 | 90.0 | 87.5 | 83.9 |
| Leuprolide Acetate 3M Depot 30 mg | 83.9 | 87.1 | 80.0 | 75.0 | 80.8 | 75.0 | 75.0 | 68.8 | 66.7 | 71.0 |
The percentage of male participants with suppression of basal testosterone to prepubertal levels, defined as testosterone < 30 ng/dL. Final visit is the participant's last visit closest to Month 36. (NCT00667446)
Timeframe: Day 1, Months 3, 6, 9, 12, 24, 30, and 36
| Intervention | percentage of participants (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Day 1 [N= 2, 5] | Month 3 [N=2, 5] | Month 6 [N=2, 5] | Month 9 [N=2, 5] | Month 12 [N=1, 5] | Month 24 [N=1, 3] | Month 30 [N=0, 1] | Month 36 [N=0, 1] | Final Visit [N=2, 5] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 | NA | NA | 100.0 |
| Leuprolide Acetate 3M Depot 30 mg | 100.0 | 100.0 | 80.0 | 80.0 | 100.0 | 66.7 | 100.0 | 100.0 | 100.0 |
"Bone age was determined by left hand/wrist bone age radiographs that were evaluated using the Fels Method by a central reader. The ratio of change from Baseline in bone age (BA)/change from Baseline in chronological age (CA) was calculated using the following formula:~(BA at Post-baseline Treatment Visit - BA at Baseline) / (CA at Post-baseline Treatment Visit - CA at Baseline)." (NCT00667446)
Timeframe: Baseline (of the lead-in study L-CP07-167), and Day 1, Months 12, 24, and 36
| Intervention | ratio (Mean) | ||||
|---|---|---|---|---|---|
| Day 1 [N=32, 37] | Month 12 [N=32, 32] | Month 24 [N=14, 17] | Month 36 [N=5, 11] | Final Visit [N=33, 32] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 0.51 | 0.52 | 0.53 | 0.43 | 0.48 |
| Leuprolide Acetate 3M Depot 30 mg | 1.02 | 0.62 | 0.72 | 0.64 | 0.56 |
Luteinizing Hormone (LH) suppression is defined as peak-stimulated LH < 4 mIU/mL. Peak-stimulated LH refers to the maximum LH concentration measured 30 and 60 minutes after a gonadotropin-releasing hormone agonist (GnRHa) stimulation test. Participants who failed suppression at previous visit and prematurely discontinued were counted as having failed future visits also. Final visit is the participant's last visit closest to Month 36. (NCT00667446)
Timeframe: Day 1, Months 6, 12, 24, and 36
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Day 1 [N= 32, 37] | Month 6 [N=32, 36] | Month 12 [N=31, 32] | Month 24 [N=16, 18] | Month 36 [N=9, 11] | Final Visit [N=33, 36] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 96.9 | 93.8 | 90.3 | 87.5 | 77.8 | 93.9 |
| Leuprolide Acetate 3M Depot 30 mg | 100.0 | 100.0 | 96.9 | 100.0 | 100.0 | 100.0 |
The percentage of male participants with suppression of testicular volume and genital staging. Testicular volume was calculated from the length, width and height of each testicle measured by ultrasound. External genital development (testes and penis) was rated from Stage 1 (early development) through Stage 5 (full development) according to a modified Tanner Staging pictogram. Suppression is defined as regression or no progression in both testicular volume and genital staging from Baseline (of the lead-in study L-CP07-167) according to pubertal staging. Boys entering the study with fully developed genitals (Stage 5) were excluded from this analysis. Final visit is the participant's last visit closest to Month 36. (NCT00667446)
Timeframe: Baseline (of the lead-in study L-CP07-167), Day 1, Months 3, 6, 9, 12, 18, 24, 30, and 36
| Intervention | percentage of participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Day 1 [N= 2, 5] | Month 3 [N=2, 5] | Month 6 [N=2, 5] | Month 9 [N=2, 5] | Month 12 [N=1, 5] | Month 18 [N=1, 3] | Month 24 [N=1, 3] | Month 30 [N=1, 1] | Month 36 [N=0, 1] | Final Visit [N=2, 5] | |
| Leuprolide Acetate 3M Depot 11.25 mg | 50.0 | 50.0 | 50.0 | 50.0 | 100.0 | 100.0 | 100.0 | 100.0 | NA | 50.0 |
| Leuprolide Acetate 3M Depot 30 mg | 40.0 | 60.0 | 60.0 | 40.0 | 60.0 | 100.0 | 33.3 | 100.0 | 100.0 | 20.0 |
Defined as percentage of patients that complete full dose of Radiation Therapy (RT) (NCT00669162)
Timeframe: 8 Months
| Intervention | percentage of participants (Number) |
|---|---|
| RT, Docetaxel, Hormonal Therapy | 26 |
Total body fat mass measured by DXA (NCT00687739)
Timeframe: Before and after 5 months of treatment
| Intervention | kg (Mean) |
|---|---|
| GnRHag+PL | 0.5 |
| GnRHag+PL+ex | -0.6 |
| GnRHag+E2 | 0.4 |
| GnRHag+E2+ex | -0.8 |
Total body fat-free mass measured by DXA (NCT00687739)
Timeframe: Before and after 5 months of treatment
| Intervention | kg (Mean) |
|---|---|
| GnRHag+PL | -1.0 |
| GnRHag+PL+ex | 0.1 |
| GnRHag+E2 | 0.0 |
| GnRHag+E2+ex | 1.0 |
Resting energy expenditure measured by indirect calorimeter at baseline and after 5 months of treatment. (NCT00687739)
Timeframe: Before and after 5 months of treatment
| Intervention | kcal/d (Mean) |
|---|---|
| GnRHag+PL | -37.8 |
| GnRHag+PL+ex | -87.2 |
| GnRHag+E2 | 14.6 |
| GnRHag+E2+ex | -19.3 |
24-hour energy expenditure measured by indirect calorimetry in a room calorimeter (NCT00687739)
Timeframe: Before and after 5 months of treatment
| Intervention | kcal/d (Mean) |
|---|---|
| GnRHag+PL | -108.8 |
| GnRHag+PL+ex | -166.5 |
| GnRHag+E2 | -92.7 |
| GnRHag+E2+Ex | -107.4 |
Cortisol response to corticotropin releasing hormone (CRH) during dexamethasone (DEX) suppression; DEX/CRH stimulation test (NCT00687739)
Timeframe: Before and after 5 months of treatment
| Intervention | ng/mL x min (Mean) |
|---|---|
| GnRHag+PL | 189 |
| GnRHag+E2 | -3115 |
"Uterine bleeding was assessed with the use of the PBAC, a validated self-reporting method to estimate menstrual blood loss.~Patients recorded daily the number of tampons and towels used and the degree to which individual items were soiled with blood (plus small or large clots). Monthly scores range from 0 (amenorrhea) to more than 500, with higher numbers indicating more bleeding.~A slightly stained tampon/towel scores 1, a partially stained tampon/towel scores 5, a completely saturated tampon scores 10 and a completely saturated towel scores 20. Small clots/flooding (2cm) score 1. Large clots/flooding (3cm) score 5.~Menorrhagia is defined as a PBAC > 100 during one menstrual period which approximates to a blood loss of > 80 mL. A PBAC of 400 corresponds to a blood loss of around 300 mL or approximately 80 tampons/towels used.~The week 13 PBAC score was calculated using the last 28 days of treatment." (NCT00740831)
Timeframe: 3 months
| Intervention | percentage of patients (Number) |
|---|---|
| A (PGL4001 5mg) | 90.3 |
| B (PGL4001 10mg) | 97.9 |
| C (GnRH-agonist) | 89.1 |
"Assessment of PGL4001 capacity to decrease volume of the three largest myomas was performed at each center by means of ultrasonography at baseline and at week 13.~The total volume of the three largest myomas assessed at screening and at end-of-treatment visit (Week 13) was analysed on a logarithm transformed scale (to base 10)." (NCT00740831)
Timeframe: 3 months
| Intervention | Log 10 (Log cm3) Total volume (Mean) |
|---|---|
| A (PGL4001 5mg) | -0.179 |
| B (PGL4001 10mg) | -0.220 |
| C (GnRH-agonist) | -0.268 |
"Difference in percentage of subjects reporting moderate or severe hot flushes:~Frequency and severity of this adverse event(as spontaneously reported by patients or elicited by nonleading questions) were recorded on standard forms at every visit up to week 17." (NCT00740831)
Timeframe: Up to week 17
| Intervention | percentage of patients (Number) |
|---|---|
| A (PGL4001 5mg) | 11.3 |
| B (PGL4001 10mg) | 9.7 |
| C (GnRH-agonist) | 39.6 |
Measured by log 10 (log pg/ml) transformed values for estradiol (E2) in blood samples (NCT00740831)
Timeframe: Week 13 visit
| Intervention | log 10 (log pg/ml) E2 (Mean) |
|---|---|
| A (PGL4001 5mg) | 1.897 |
| B (PGL4001 10mg) | 1.843 |
| C (GnRH-agonist) | 1.381 |
"The CPSSS consists of 5 components that address dysmenorrhea, dyspareunia, non-menstrual pelvic pain, pelvic tenderness, and pelvic induration.~To assess non-menstrual pelvic pain, participants were asked to select the best description of pelvic pain over the past 28 days using the following response categories:~0 = Absent; No discomfort.~1 = Mild; Occasional pelvic discomfort that can be treated with NSAIDs.~2 = Moderate; Noticeable discomfort or pain for most of cycle requiring regular use of NSAID or weak opiate.~3 = Severe; Pain persisting during the cycle or pain requiring strong analgesics." (NCT00797225)
Timeframe: Baseline and Week 12
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Placebo | -0.60 |
| Elagolix 150 mg | -0.58 |
| Elagolix 250 mg | -0.48 |
| Leuprorelin | -0.79 |
Blood samples to determine N-telopeptide concentrations were analyzed by a central laboratory using an enzyme-linked immunosorbent assay (ELISA). (NCT00797225)
Timeframe: Baseline and week 12
| Intervention | nM bone collagen equivalents (BCE) (Mean) |
|---|---|
| Placebo | 0.62 |
| Elagolix 150 mg | 0.77 |
| Elagolix 250 mg | 2.04 |
| Leuprorelin | 3.18 |
Defined as the number of days from the last dose of study drug until the start date of the first post-treatment menses. (NCT00797225)
Timeframe: From last day of study drug up to 6 weeks after the last dose.
| Intervention | days (Median) |
|---|---|
| Elagolix 150 mg | 22.5 |
| Elagolix 250 mg | 26.0 |
| Placebo / Elagolix 150 mg | 26.0 |
| Placebo / Elagolix 250 mg | 27.0 |
| Leuprorelin / Elagolix 150 mg | 29.0 |
| Leuprorelin / Elagolix 250 mg | 28.0 |
Bone mineral density (BMD) of the femur (total hip) was measured by dual-energy X-ray absorptiometry (DXA). (NCT00797225)
Timeframe: Baseline and week 12
| Intervention | percent change (Mean) |
|---|---|
| Placebo | -0.90 |
| Elagolix 150 mg | -0.342 |
| Elagolix 250 mg | -0.5623 |
| Leuprorelin | -1.122 |
Bone mineral density (BMD) of the femur (total hip) was measured by dual-energy X-ray absorptiometry (DXA). (NCT00797225)
Timeframe: Baseline and Week 24
| Intervention | percent change (Mean) |
|---|---|
| Elagolix 150 mg | -0.549 |
| Elagolix 250 mg | -0.699 |
| Placebo / Elagolix 150 mg | -0.126 |
| Placebo / Elagolix 250 mg | -0.573 |
| Leuprorelin / Elagolix 150 mg | -1.784 |
| Leuprorelin / Elagolix 250 mg | -1.783 |
Bone mineral density (BMD) of the spine was measured by dual-energy X-ray absorptiometry (DXA). (NCT00797225)
Timeframe: Baseline and week 12
| Intervention | percent change (Mean) |
|---|---|
| Placebo | 0.106 |
| Elagolix 150 mg | -1.053 |
| Elagolix 250 mg | -0.799 |
| Leuprorelin | -1.633 |
Bone mineral density (BMD) of the spine was measured by dual-energy X-ray absorptiometry (DXA). (NCT00797225)
Timeframe: Baseline and Week 24
| Intervention | percent change (Mean) |
|---|---|
| Elagolix 150 mg | -1.288 |
| Elagolix 250 mg | -1.855 |
| Placebo / Elagolix 150 mg | -0.990 |
| Placebo / Elagolix 250 mg | -0.648 |
| Leuprorelin / Elagolix 150 mg | -2.899 |
| Leuprorelin / Elagolix 250 mg | -4.378 |
"Hot flashes, if any, were reported daily by participants during the study using the e-Diary.~The average number of hot flashes per day was calculated for each participant as the total number of hot flashes divided by total days in the phase." (NCT00797225)
Timeframe: Screening (8 weeks prior to day 1), Treatment phase (weeks 1 to 12 for participants in the placebo and leuprorelin treatment groups and weeks 1 to 24 for participants in the elagolix treatment groups)
| Intervention | hot flashes per day (Median) | |
|---|---|---|
| Screening | Treatment Phase | |
| Elagolix 150 mg | 0.00 | 0.22 |
| Elagolix 250 mg | 0.00 | 1.10 |
| Leuprorelin | 0.00 | 1.73 |
| Placebo | 0.00 | 0.11 |
"The CPSSS consists of 5 components that address dysmenorrhea, dyspareunia, non-menstrual pelvic pain, pelvic tenderness, and pelvic induration.~To assess dyspareunia (painful intercourse) participants were asked to select the best description of pain during sexual intercourse over the past 28 days using the following response categories:~0 = Absent; No discomfort during sexual intercourse.~1 = Mild; I can tolerate the discomfort during sexual intercourse.~2 = Moderate; Intercourse is sometime interrupted due to pain.~3 = Severe; I prefer to avoid intercourse because of pain.~Not applicable. I am not sexually active for reasons other than my endometriosis symptoms." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.46 | -0.68 | -0.84 |
| Elagolix 250 mg | -0.49 | -0.77 | -0.89 |
| Leuprorelin | -0.55 | -0.76 | -1.04 |
| Placebo | -0.33 | -0.72 | -0.60 |
"Participants assessed dysmenorrhea (pain during menstruation) and its impact on their daily activities at approximately the same time each day of their period in an e-Diary according to the following response options:~Subject is not having her period~0 = No pain related to period~1 = Mild pain related to period; subject could not do some of the things she usually does~2 = Moderate pain related to period; subject could not do many of the things she usually does~3 = Severe pain related to period; subject could not do most of or all of the things she usually does.~The monthly mean dysmenorrhea score is the average of the daily values reported during the 4 weeks prior to each visit." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.64 | -0.86 | -0.76 |
| Elagolix 250 mg | -0.67 | -1.04 | -0.87 |
| Leuprorelin | -0.65 | -1.22 | -1.14 |
| Placebo | -0.17 | -0.40 | -0.35 |
"Participants assessed their pelvic pain not related to menses and its impact on their daily activities at approximately the same time every day in an e-Diary according to the following response options:~0 = No pelvic pain~1 = Mild pelvic pain; subject could not do some of the things she usually does~2 = Moderate pelvic pain; subject could not do many of the things she usually does~3 = Severe pelvic pain; subject could not do most or all of the things she usually does.~The monthly mean non-menstrual pelvic pain score is the average of the daily values reported during the 4 weeks prior to each visit." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.22 | -0.34 | -0.35 |
| Elagolix 250 mg | -0.21 | -0.36 | -0.34 |
| Leuprorelin | -0.27 | -0.46 | -0.55 |
| Placebo | -0.05 | -0.18 | -0.30 |
"The NRS is an 11-point scale used to measure endometriosis pain and was completed at approximately the same time each day using an electronic diary (e-Diary). Participants were instructed to select a single number between 0 (No pain) and 10 (Worst pain ever) that best described their endometriosis pain at its worst over the past day.~The monthly mean NRS is the average of the daily values reported during the 4 weeks prior to each visit." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.84 | -1.25 | -1.34 |
| Elagolix 250 mg | -1.00 | -1.57 | -1.47 |
| Leuprorelin | -0.94 | -1.55 | -1.81 |
| Placebo | -0.35 | -0.93 | -1.22 |
"Participants assessed dysmenorrhea and pelvic pain not related to menses and their impact on daily activities at approximately the same time every day on a 4-point scale (0 = none, 1 = mild, 2 = moderate, and 3 = severe) in an e-Diary. The dysmenorrhea scale included an option for participants who were not having their period.~The sum of the dysmenorrhea and non-menstrual pelvic pain scores on each day were calculated to create a daily total score. On days the participant was not having her period, the dysmenorrhea score was not defined; hence, the total score was equal to the non-menstrual pelvic pain score (range 0 to 3). On days where the participant recorded menstruation the total score ranged from 0 to 6, where higher scores indicate more severe pain. The monthly mean sum of dysmenorrhea and non-menstrual pelvic pain scores is the average of the daily values reported during the 4 weeks prior to each visit." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.43 | -0.58 | -0.55 |
| Elagolix 250 mg | -0.44 | -0.67 | -0.63 |
| Leuprorelin | -0.50 | -0.78 | -0.87 |
| Placebo | -0.12 | -0.24 | -0.40 |
"The NRS is an 11-point scale used to measure endometriosis pain and was completed at approximately the same time each day using an electronic diary (e-Diary). Participants were instructed to select a single number between 0 (No pain) and 10 (Worst pain ever) that best described their endometriosis pain at its worst over the past day.~The monthly peak NRS is the maximum of the daily values reported during the 4 weeks prior to each visit." (NCT00797225)
Timeframe: Baseline and Weeks 4, 8, and 12
| Intervention | units on a scale (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -1.82 | -2.23 | -2.62 |
| Elagolix 250 mg | -1.83 | -2.96 | -3.05 |
| Leuprorelin | -1.48 | -3.62 | -3.99 |
| Placebo | -0.20 | -0.89 | -1.67 |
"The daily use of endometriosis analgesics was reported by participants daily using the e-Diary. Participants reported whether the medication was over-the-counter (OTC) or prescription, and, if prescription, whether the medication was a narcotic.~The percentage of days of any analgesic use is defined as the number of days in the 4 weeks prior to each study visit that the participant reported the use of an analgesic, divided by the number of study days in the interval that the participant provided an e-Diary report regarding the use of endometriosis analgesics (including a response of none)." (NCT00797225)
Timeframe: Baseline, Weeks 4, 8 and 12
| Intervention | percentage of days (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -1.1 | -3.4 | -4.4 |
| Elagolix 250 mg | -8.4 | -9.1 | -8.3 |
| Leuprorelin | -8.7 | -10.2 | -10.5 |
| Placebo | -5.2 | -6.2 | -6.2 |
"The daily use of endometriosis analgesics was reported by participants daily using the e-Diary. Participants reported whether the medication was over-the-counter (OTC) or prescription, and, if prescription, whether the medication was a narcotic.~The percentage of days of narcotic analgesic use is defined as the number of days in the 4 weeks prior to each study visit that the participant reported the use of a narcotic analgesic, divided by the number of study days in the interval that the participant provided an e-Diary report regarding the use of endometriosis analgesics (including a response of none)." (NCT00797225)
Timeframe: Baseline, Weeks 4, 8 and 12
| Intervention | percentage of days (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | -0.1 | -0.1 | 0.1 |
| Elagolix 250 mg | 0.0 | -0.1 | 0.1 |
| Leuprorelin | -0.1 | -0.1 | 0.3 |
| Placebo | 0.0 | -0.1 | 0.0 |
"The daily use of endometriosis analgesics was reported by participants daily using the e-Diary. Participants reported whether the medication was over-the-counter (OTC) or prescription, and, if prescription, whether the medication was a narcotic.~The percentage of days of prescription analgesic use is defined as the number of days in the 4 weeks prior to each study visit that the participant reported the use of a prescription analgesic, divided by the number of study days in the interval that the participant provided an e-Diary report regarding the use of endometriosis analgesics (including a response of none)." (NCT00797225)
Timeframe: Baseline, Weeks 4, 8 and 12
| Intervention | percentage of days (Least Squares Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | 3.4 | 1.3 | 0.7 |
| Elagolix 250 mg | -1.2 | -2.8 | -1.9 |
| Leuprorelin | -2.5 | -2.6 | -2.8 |
| Placebo | -0.3 | -1.3 | -1.8 |
The concentration of serum estradiol (E2) was quantified using liquid chromatography with tandem mass spectrophotometry (LC/MS/MS). Serum estradiol concentrations below the limit of quantification (BLQ) were set equal to the lower limit of quantification (2.5 pg/mL). (NCT00797225)
Timeframe: Baseline and Weeks 4, 8 and 12
| Intervention | pg/mL (Median) | |||
|---|---|---|---|---|
| Baseline | Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | 43.40 | 36.40 | 36.90 | 36.70 |
| Elagolix 250 mg | 47.50 | 22.00 | 23.65 | 26.20 |
| Leuprorelin | 46.20 | 3.63 | 4.36 | 6.38 |
| Placebo | 39.10 | 49.50 | 61.00 | 87.90 |
"The Patient Global Impression of Change (PGIC) is a questionnaire-based assessment of the change in endometriosis pain since the initiation of study drug. The participant was asked to select from one of seven response categories:~Very Much Improved~Much Improved~Minimally Improved~Not Changed~Minimally Worse~Much Worse~Very Much Worse" (NCT00797225)
Timeframe: Weeks 4, 8 and 12
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | 3.0 | 2.5 | 2.4 |
| Elagolix 250 mg | 2.9 | 2.2 | 2.2 |
| Leuprorelin | 3.3 | 2.3 | 2.1 |
| Placebo | 3.4 | 2.8 | 2.6 |
"Uterine bleeding was reported daily by participants during the study using the e-Diary.~The percentage of days a participant reported any bleeding was calculated as the total number of days the participant reported any bleeding ( light, moderate, or heavy) divided by the total number of days the participant had a non-missing eDiary report of vaginal bleeding in the phase." (NCT00797225)
Timeframe: Screening (8 weeks prior to day 1), Treatment phase (weeks 1 to 12 for participants in the placebo and leuprorelin treatment groups and weeks 1 to 24 for participants in the elagolix treatment groups)
| Intervention | percentage of days (Mean) | |
|---|---|---|
| Screening | Treatment Phase | |
| Elagolix 150 mg | 18.32 | 10.78 |
| Elagolix 250 mg | 22.32 | 9.54 |
| Leuprorelin | 21.05 | 11.04 |
| Placebo | 21.10 | 21.46 |
"The PGIC is a questionnaire-based assessment of the change in endometriosis pain since the initiation of study drug. The participant was asked to select from one of seven response categories:~Very Much Improved~Much Improved~Minimally Improved~Not Changed~Minimally Worse~Much Worse~Very Much Worse" (NCT00797225)
Timeframe: Weeks 4, 8 and 12
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | 74.4 | 81.4 | 88.1 |
| Elagolix 250 mg | 65.1 | 90.7 | 88.4 |
| Leuprorelin | 50.0 | 88.6 | 93.2 |
| Placebo | 56.1 | 75.6 | 80.5 |
"The PGIC is a questionnaire-based assessment of the change in endometriosis pain since the initiation of study drug. The participant was asked to select from one of seven response categories:~Very Much Improved~Much Improved~Minimally Improved~Not Changed~Minimally Worse~Much Worse~Very Much Worse" (NCT00797225)
Timeframe: Weeks 4, 8 and 12
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Elagolix 150 mg | 25.6 | 53.5 | 54.8 |
| Elagolix 250 mg | 32.6 | 72.1 | 67.4 |
| Leuprorelin | 27.3 | 54.5 | 70.5 |
| Placebo | 7.3 | 36.6 | 53.7 |
"The EHP-5 is an instrument to measure health-related quality of life in women with endometriosis. The EHP-5 consists of two parts:~A core questionnaire consisting of five questions that measure the areas of pain, control and powerlessness, emotional well-being, social support, and self-image with five response categories for each item (Never, Rarely, Sometimes, Often, Always)~A supplemental questionnaire consisting of six additional questions which assess the areas of work, relationship with children, sexual intercourse, feelings about the medical profession, treatment, and infertility with the same five response categories plus an additional response category of Not Relevant which was not scored.~The scores associated with each possible outcome category are as follows: never (0), rarely (25), sometimes (50), often (75), and always (100). A negative change from baseline score indicates improvement in quality of life." (NCT00797225)
Timeframe: Baseline and week 12
| Intervention | units on a scale (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Pain | Control and Powerlessness | Emotional Wellbeing | Social Support | Self-image | Work | Relationship with Children | Sexual Intercourse | Medical Profession | Frustration with Treatment | Concerns with Infertility | |
| Elagolix 150 mg | -19.0 | -17.9 | -10.7 | -16.1 | -7.7 | -21.5 | -15.3 | -21.2 | -5.5 | -10.9 | -24.0 |
| Elagolix 250 mg | -25.0 | -20.9 | -12.8 | -18.6 | -5.8 | -29.9 | -25.0 | -30.6 | -7.6 | -7.6 | -13.8 |
| Leuprorelin | -31.8 | -23.9 | -13.6 | -15.3 | -8.5 | -38.6 | -22.9 | -28.9 | -6.3 | -12.5 | -13.3 |
| Placebo | -14.0 | -18.3 | -14.6 | -22.0 | -12.2 | -23.7 | -11.5 | -32.2 | -5.3 | -11.4 | -19.7 |
"The CPSSS consists of 5 components that address dysmenorrhea, dyspareunia, non-menstrual pelvic pain, pelvic tenderness, and pelvic induration.~To assess dysmenorrhea (pain during menstruation), participants were asked to select the best description of painful menstruation over the past 28 days using the following response categories:~0 = Absent; Amenorrhea (no bleeding) or no discomfort.~1 = Mild; Some loss of work efficiency; occasional use of analgesics.~2 = Moderate; In bed part of one day, occasional loss of work; regular use of analgesics.~3 = Severe; In bed ≥ 1 day, incapacitation; requirement for strong analgesics." (NCT00797225)
Timeframe: Baseline and Week 12
| Intervention | units on a scale (Least Squares Mean) |
|---|---|
| Placebo | -1.03 |
| Elagolix 150 mg | -1.29 |
| Elagolix 250 mg | -1.47 |
| Leuprorelin | -1.75 |
The fertilization rate for each participant was the percentage of the number of oocytes inseminated of the total number of oocytes retrieved. (NCT00805935)
Timeframe: approximately day 19
| Intervention | Percentage of oocytes retrieved (Number) |
|---|---|
| Menotropin | 17.1 |
| Follitropin Beta | 24.8 |
The mean number of follicles observed in both ovaries at the last transvaginal ultrasound in the stimulation phase. (NCT00805935)
Timeframe: approximately day 15
| Intervention | Follicles (Mean) |
|---|---|
| Menotropin | 27.7 |
| Follitropin Beta | 30.5 |
The mean number of oocytes retrieved approximately 36 hours after hCG (Novarel®) administration and fertilized (by insemination or intra cytoplasmic sperm injection (ICSI)) according to site-specific procedures. (NCT00805935)
Timeframe: approximately day 18
| Intervention | Oocytes (Mean) |
|---|---|
| Menotropin | 13.0 |
| Follitropin Beta | 15.6 |
"Number of participants with adverse events (AEs) that started after first treatment. Severity used a three point scale:~mild=awareness of signs/symptoms, but no disruption of usual activity moderate=event sufficient to affect usual activity (disturbing) severe=event causes inability to work or perform usual activities (unacceptable) Relatedness to study treatment used a four point scale: unrelated, unlikely, possible, probable.~Seriousness refers to death, hospitalization, a life-threatening experience, persistent or significant disability/incapacity, or congenital anomaly." (NCT00805935)
Timeframe: Week 1 to week12
| Intervention | Participants (Number) | |||||
|---|---|---|---|---|---|---|
| With at least one adverse event | With at least one mild or moderate adverse event | With at least one severe adverse event | With at least one serious adverse event | With at least one unrelated or unlikely AE | With at least one possibly or probably related AE | |
| Follitropin Beta/Progesterone in Oil | 14 | 14 | 0 | 0 | 13 | 6 |
| Follitropin Beta/Progesterone Vaginal Insert | 15 | 15 | 1 | 0 | 12 | 8 |
| Menotropin/Progesterone in Oil | 12 | 11 | 2 | 1 | 11 | 7 |
| Menotropin/Progesterone Vaginal Insert | 9 | 9 | 0 | 0 | 8 | 3 |
A count of participants whose discontinuation was clearly documented on the study completion/termination form as cycle cancellation for risk of ovarian hyperstimulation syndrome (OHSS). (NCT00805935)
Timeframe: weeks 1-3
| Intervention | Participants (Number) | |
|---|---|---|
| Yes | No | |
| Follitropin Beta/Progesterone in Oil | 0 | 30 |
| Follitropin Beta/Progesterone Vaginal Insert | 1 | 27 |
| Menotropin/Progesterone in Oil | 0 | 27 |
| Menotropin/Progesterone Vaginal Insert | 1 | 24 |
"The number of embryos, morulas and blastocysts transferred to the study participant on either day 3 or day 5 following fertilization. Embryos represent the earliest development stage and contain 2-8 cells.~Morulas, the next stage, continued cellular cleavage results in a 16-30 cell solid sphere. Morula further develop into blastocyst, which contains 70-100 cells in a hollow spherical shape." (NCT00805935)
Timeframe: approximately day 24
| Intervention | Embryos (Mean) | ||
|---|---|---|---|
| Number of embryos transferred | Number of morula transferred | Number of blastocyst transferred | |
| Follitropin Beta | 2.0 | 0.1 | 1.1 |
| Menotropin | 2.0 | 0.0 | 0.8 |
Clinical pregnancy is the confirmation of the presence of intrauterine gestational sacs on pregnancy ultrasound examination. (NCT00805935)
Timeframe: approximately Day 65
| Intervention | Percentage of participants (Number) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 48.0 |
| Menotropin/Progesterone in Oil | 33.3 |
| Follitropin Beta/Progesterone Vaginal Insert | 46.4 |
| Follitropin Beta/Progesterone in Oil | 63.3 |
Blood tests were sent to a central laboratory to obtain progesterone levels. (NCT00805935)
Timeframe: approximately day 16
| Intervention | ng/mL (Mean) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 1.3 |
| Menotropin/Progesterone in Oil | 1.1 |
| Follitropin Beta/Progesterone Vaginal Insert | 1.7 |
| Follitropin Beta/Progesterone in Oil | 1.3 |
Biochemical pregnancy is a positive β-hCG pregnancy test 12-14 days post embryo transfer. (NCT00805935)
Timeframe: approximately day 38 (Day 14 post embryo transfer)
| Intervention | Percentage of participants (Number) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 60.0 |
| Menotropin/Progesterone in Oil | 55.6 |
| Follitropin Beta/Progesterone Vaginal Insert | 60.7 |
| Follitropin Beta/Progesterone in Oil | 73.3 |
Estradiol monitoring during fertility therapy assesses follicular growth and is useful in monitoring the treatment. Blood tests sent to a central laboratory to obtain estradiol levels. (NCT00805935)
Timeframe: Day 6
| Intervention | pg/mL (Mean) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 354.6 |
| Menotropin/Progesterone in Oil | 268.2 |
| Follitropin Beta/Progesterone Vaginal Insert | 617.5 |
| Follitropin Beta/Progesterone in Oil | 550.5 |
Blood tests were sent to a central laboratory to obtain hCG levels. (NCT00805935)
Timeframe: Day 6
| Intervention | mIU/ml (Mean) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 1.0 |
| Menotropin/Progesterone in Oil | 1.0 |
| Follitropin Beta/Progesterone Vaginal Insert | 1.0 |
| Follitropin Beta/Progesterone in Oil | 1.0 |
The number of embryos that were not transferred but instead were frozen for future use. (NCT00805935)
Timeframe: approximately day 24
| Intervention | Embryos (Mean) |
|---|---|
| Menotropin | 1.9 |
| Follitropin Beta | 1.9 |
Clinical pregnancy is the confirmation of the presence of intrauterine gestational sacs on pregnancy ultrasound examination. (NCT00805935)
Timeframe: approximately Day 52
| Intervention | Percentage of participants (Number) |
|---|---|
| Menotropin/Progesterone Vaginal Insert | 56.0 |
| Menotropin/Progesterone in Oil | 33.3 |
| Follitropin Beta/Progesterone Vaginal Insert | 46.4 |
| Follitropin Beta/Progesterone in Oil | 66.7 |
The tolerability at one year of ovarian function suppression (OFS) using leuprolide and letrozole in this patient population. Specifically, the number of patients who discontinued treatment prior to one year due to toxicity. (NCT00903162)
Timeframe: 1 year
| Intervention | participants (Number) |
|---|---|
| Letrozole-Leuprolide | 4 |
Androstenedione is a steroid (a group of polycyclic compounds closely related biochemically to terpenes, for example, cholesterol, numerous hormones), that is produced in the testis, ovary and the adrenal cortex, and depending on the tissue type, androstenedione can serve as a precursor to testosterone, estrone and estradiol. The DHEA is a major steroid produced by the adrenal cortex. It is also produced in small quantities in the testis and the ovary. Androstenedione and DHEA concentration was measured in prostate tissues at Week 12 and 24. (NCT00924469)
Timeframe: Week 12 and 24
| Intervention | Picogram per milligram (pg/mg) (Mean) | |||
|---|---|---|---|---|
| Androstenedione: Week 12 (n=28,27) | Androstenedione: Week 24 (n=28,26) | DHEA: Week 12 (n=28,27) | DHEA: Week 24 (n=28,26) | |
| Abiraterone Plus Leuprolide Plus Prednisone | 0.082 | 0.090 | 1.994 | 3.138 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 0.277 | 0.070 | 29.241 | 2.170 |
The PSA response was evaluated according to Response Evaluation Criteria in Solid Tumors (RECIST) criterion which is, percentage of participants with PSA less than or equal to 0.2 nanogram/milliliter at Weeks 12 and 24 after androgen deprivation. (NCT00924469)
Timeframe: Weeks 12 and 24
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Week 12 | Week 24 | |
| Abiraterone Plus Leuprolide Plus Prednisone | 86.7 | 86.7 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 3.6 | 82.1 |
Serum concentrations of testosterone, DHT, androsterone, DHEA, DHEA-Sulfate, DHEA-Glucuronide and delta-4-androstenedione were measured at Weeks 12 and 24. (NCT00924469)
Timeframe: Week 12 and 24
| Intervention | Nanogram per deciliter (ng/dL) (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Testosterone: Week 12 (n=28,28) | Testosterone: Week 24 (n=25,25) | DHT: Week 12 (n=28,28) | DHT: Week 24 (n=26,26) | Androsterone: Week 12 (n=28,28) | Androsterone: Week 24 (26,26) | DHEA: Week 12 (n=28,28) | DHEA: Week 24 (n=26,26) | DHEA-Glucuronide: Week 12 (n=29,28) | DHEA-Glucuronide: Week 24 (n=27,27) | DHEA-Sulfate: Week 12 (n=28,28) | DHEA-Sulfate: Week 24 (n=26,26) | Delta-4-Androstenedione:Week 12(n=28,28) | Delta-4-Androstenedione:Week 24(n=26,26) | |
| Abiraterone Plus Leuprolide Plus Prednisone | 1.049 | 0.648 | 6.143 | 5.932 | 0.619 | 1.752 | 10.684 | 20.922 | 69.724 | 51.675 | 7156.270 | 9047.406 | 3.315 | 5.192 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 10.014 | 3.122 | 5.797 | 6.730 | 3.100 | 0.500 | 180.307 | 7.617 | 583.036 | 51.759 | 133338.875 | 9207.345 | 33.330 | 2.831 |
Testosterone is a potent androgen (a hormone that promotes the development and maintenance of male characteristics) and major product secreted by cells in the testis and produced in the adrenal glands and by prostate cancers. Dihydrotestosterone (DHT) is a potent androgenic metabolite of testosterone. Testosterone and DHT concentration was measured in prostate tissues after exposure to study treatments at Week 24. (NCT00924469)
Timeframe: Week 24
| Intervention | Picogram per milligram (pg/mg) (Mean) | |
|---|---|---|
| Testosterone | DHT | |
| Abiraterone Plus Leuprolide Plus Prednisone | 0.216 | 1.340 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 0.062 | 2.456 |
The DHT is a potent androgenic metabolite of testosterone and the concentration of DHT was measured in prostate tissues after exposure to study treatments at Week 12. (NCT00924469)
Timeframe: Week 12
| Intervention | Picogram per milligram (pg/mg) (Mean) |
|---|---|
| Abiraterone Plus Leuprolide Plus Prednisone | 4.311 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 2.170 |
Complete response is defined as a disappearance of all target lesions and was assessed by the Response Evaluation Criteria in Solid Tumors (RECIST) criterion. (NCT00924469)
Timeframe: Week 24
| Intervention | Percentage of participants (Number) |
|---|---|
| Abiraterone Plus Leuprolide Plus Prednisone | 10.3 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 3.7 |
Testosterone is a potent androgen (a hormone that promotes the development and maintenance of male characteristics) and major product secreted by cells in the testis and produced in the adrenal glands and by prostate cancers. Abiraterone acetate affects sources of testosterone in the body (ie, adrendal gland and prostate tumor). Testosterone concentration was measured in prostate tissues after exposure to study treatments at Week 12. (NCT00924469)
Timeframe: Week 12
| Intervention | Picogram per milligram (pg/mg) (Mean) |
|---|---|
| Abiraterone Plus Leuprolide Plus Prednisone | 0.089 |
| Leuprolide Then Abiraterone Plus Leuprolide Plus Prednisone | 0.228 |
"The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function.~Ejaculation domain consist of 2 questions and are scored on a scale of 0-4 (0=minimum, 4=maximum). Total score for the ejaculation domain ranges from 0 to 8. A higher scores represent better sexual function." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.90 | -0.80 | -1.06 | -1.24 | -1.07 | -1.17 |
| DI (Degarelix Intermittent) | -1.04 | -1.23 | -1.24 | -0.94 | -0.89 | -0.79 |
| LC (Leuprolide Continuous) | -0.87 | -1.08 | -0.94 | -0.93 | -1.12 | -0.97 |
| Total Continuous | -0.88 | -1.02 | -0.97 | -1.00 | -1.11 | -1.01 |
"The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function.~Sexual drive domain consist of 2 questions and are scored on a scale of 0-4 (0=minimum, 4=maximum). Total score for the sexual drive domain ranges from 0 to 8. A higher scores represent better sexual function." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -1.57 | -1.39 | -1.51 | -1.52 | -1.55 | -1.65 |
| DI (Degarelix Intermittent) | -1.57 | -1.71 | -1.72 | -1.59 | -1.44 | -1.30 |
| LC (Leuprolide Continuous) | -1.27 | -1.67 | -1.62 | -1.65 | -1.72 | -1.72 |
| Total Continuous | -1.33 | -1.61 | -1.60 | -1.63 | -1.69 | -1.71 |
"The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score.~Physical well-being consist of 7 items and scored on a scale of 0-4 (0=Not at all; 1=A little bit; 2=Somewhat; 3=Quite a bit; 4=Very much). Total score for the physical well-being sub scale ranges from 0 to 28. Higher scores represent better QoL." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -1.63 | -1.48 | -1.92 | -1.85 | -2.08 | -1.77 | -1.62 | -2.10 | -1.90 |
| DI (Degarelix Intermittent) | -1.47 | -1.41 | -0.96 | -1.24 | -1.05 | -1.00 | -0.91 | -1.00 | -1.04 |
| LC (Leuprolide Continuous) | -1.41 | -1.67 | -1.74 | -1.77 | -1.68 | -1.53 | -1.32 | -1.40 | -1.45 |
| Total Continuous | -1.46 | -1.63 | -1.78 | -1.79 | -1.76 | -1.58 | -1.39 | -1.55 | -1.55 |
The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score. Total FACT-P scores ranges from 0 to 156. Higher scores represent better QoL. (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -1.89 | -2.64 | -3.12 | -3.49 | -4.56 | -3.27 | -3.97 | -5.62 | -4.28 |
| DI (Degarelix Intermittent) | -1.86 | -2.03 | -1.75 | -1.61 | -0.89 | -1.18 | -0.95 | -1.74 | -1.36 |
| LC (Leuprolide Continuous) | -1.23 | -2.38 | -1.69 | -2.84 | -3.16 | -2.48 | -1.60 | -1.85 | -1.65 |
| Total Continuous | -1.37 | -2.43 | -1.99 | -2.98 | -3.45 | -2.65 | -2.09 | -2.64 | -2.20 |
"The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score.~Social well-being consist of 7 items and scored on a scale of 0-4 (0=Not at all; 1=A little bit; 2=Somewhat; 3=Quite a bit; 4=Very much). Total score for the social well-being sub scale ranges from 0 to 28. Higher scores represent better QoL." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.06 | -0.30 | -0.52 | -0.95 | -1.00 | -1.09 | -1.34 | -1.35 | -0.68 |
| DI (Degarelix Intermittent) | -0.18 | 0.00 | -0.33 | -0.02 | 0.36 | 0.20 | -0.16 | -0.02 | 0.28 |
| LC (Leuprolide Continuous) | -0.36 | -0.46 | -0.41 | -1.10 | -1.15 | -0.83 | -0.85 | -0.72 | -0.55 |
| Total Continuous | -0.30 | -0.43 | -0.43 | -1.07 | -1.12 | -0.88 | -0.95 | -0.85 | -0.58 |
"The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score.~Functional well-being consist of 7 items and scored on a scale of 0-4 (0=Not at all; 1=A little bit; 2=Somewhat; 3=Quite a bit; 4=Very much). Total score for the functional well-being sub scale ranges from 0 to 28. Higher scores represent better QoL." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.88 | -0.78 | -1.08 | -1.07 | -0.89 | -0.80 | -1.49 | -2.22 | -1.95 |
| DI (Degarelix Intermittent) | -0.96 | -1.41 | -1.18 | -1.14 | -1.35 | -1.25 | -0.92 | -1.49 | -1.02 |
| LC (Leuprolide Continuous) | -0.29 | -1.24 | -0.73 | -1.23 | -1.42 | -1.24 | -0.73 | -0.96 | -0.84 |
| Total Continuous | -0.42 | -1.15 | -0.80 | -1.20 | -1.31 | -1.15 | -0.89 | -1.22 | -1.07 |
Absolute change from Baseline in serum PSA levels during the study period was measured. (NCT00928434)
Timeframe: Phase A Visit 1-8 and Phase B Visit 9-15.
| Intervention | ng/mL (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase A, Visit 1 (Day 0) | Phase A, Visit 2 (Month 1) | Phase A, Visit 3 (Month 2) | Phase A, Visit 4 (Month 3) | Phase A, Visit 5 (Month 4) | Phase A, Visit 6 (Month 5) | Phase A, Visit 7 (Month 6) | Phase A, Visit 8 (Month 7) | Phase B, Visit 9 (Month 8) | Phase B, Visit 10 (Month 9) | Phase B, Visit 11 (Month 10) | Phase B, Visit 12 (Month 11) | Phase B, Visit 13 (Month 12) | Phase B, Visit 14 (Month 13) | Phase B, Visit 15 (Month 14) | |
| DC (Degarelix Continuous) | -0.91 | -14.3 | -14.8 | -15 | -15.1 | -15.1 | -15.1 | -15.1 | -15 | -15 | -14.9 | -14.9 | -14.8 | -14.8 | -14.8 |
| DI (Degarelix Intermittent) | NA | -6.39 | -6.94 | -7.07 | -7.16 | -7.19 | -7.21 | -7.24 | -7.25 | -7.18 | -7.07 | -6.96 | -6.81 | -6.79 | -6.74 |
| LC (Leuprolide Continuous) | NA | -6.38 | -8.12 | -8.44 | -8.51 | -8.59 | -8.64 | -8.64 | -8.64 | -8.64 | -8.63 | -8.64 | -8.64 | -8.59 | -8.6 |
The time to testosterone >0.5 ng/mL level in the DI group was counted from the start of Phase B at Day 196 (i.e. 28 days after last injection of degarelix) (NCT00928434)
Timeframe: During Phase B
| Intervention | Days (Median) |
|---|---|
| DI (Degarelix Intermittent) | 112.0 |
"The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function.~Problem assessment domain consist of 2 questions and are scored on a scale of 0-4 (0=minimum, 4=maximum). Total score for the problem assessment domain ranges from 0 to 8. A higher scores represent better sexual function." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.58 | -0.88 | -0.71 | -0.53 | -1.63 | -1.68 |
| DI (Degarelix Intermittent) | -0.26 | -0.90 | -0.56 | 0.09 | -0.15 | -0.31 |
| LC (Leuprolide Continuous) | -0.36 | -0.57 | -0.64 | -0.98 | -1.07 | -0.89 |
| Total Continuous | -0.40 | -0.63 | -0.66 | -0.89 | -1.19 | -1.05 |
Absolute Change From Baseline in Serum Testosterone Levels was measured. (NCT00928434)
Timeframe: Phase A Visit 1-8 and Phase B Visit 9-15.
| Intervention | ng/mL (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase A, Visit 1 (Day 0) | Phase A, Visit 2 (Month 1) | Phase A, Visit 3 (Month 2) | Phase A, Visit 4 (Month 3) | Phase A, Visit 5 (Month 4) | Phase A, Visit 6 (Month 5) | Phase A, Visit 7 (Month 6) | Phase A, Visit 8 (Month 7) | Phase B, Visit 9 (Month 8) | Phase B, Visit 10 (Month 9) | Phase B, Visit 11 (Month 10) | Phase B, Visit 12 (Month 11) | Phase B, Visit 13 (Month 12) | Phase B, Visit 14 (Month 13) | Phase B, Visit 15 (Month 14) | |
| DC (Degarelix Continuous) | -2.97 | -3.77 | -3.77 | -3.78 | -3.78 | -3.78 | -3.77 | -3.78 | -3.76 | -3.76 | -3.75 | -3.74 | -3.72 | -3.73 | -3.71 |
| DI (Degarelix Intermittent) | NA | -3.64 | -3.67 | -3.68 | -3.67 | -3.67 | -3.66 | -3.66 | -3.63 | -3.41 | -3.0 | -2.57 | -2.18 | -2.1 | -1.77 |
| LC (Leuprolide Continuous) | NA | -3.7 | -3.77 | -3.77 | -3.74 | -3.78 | -3.77 | -3.78 | -3.78 | -3.78 | -3.77 | -3.78 | -3.78 | -3.77 | -3.78 |
"The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score.~Additional concerns consist of 12 items and scored on a scale of 0-4 (0=Not at all; 1=A little bit; 2=Somewhat; 3=Quite a bit; 4=Very much). Total score for the additional concerns ranges from 0 to 48. Higher scores represent better QoL." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.92 | -1.34 | -1.03 | -1.64 | -0.80 | -0.56 | -1.20 | -0.96 | -0.67 |
| DI (Degarelix Intermittent) | -1.14 | -0.89 | -1.29 | -0.97 | -0.86 | -0.80 | -0.75 | -0.91 | -0.81 |
| LC (Leuprolide Continuous) | -0.51 | -1.03 | -0.63 | -0.90 | -0.70 | -0.58 | -0.75 | -0.86 | -0.27 |
| Total Continuous | -0.60 | -1.10 | -0.72 | -1.06 | -0.72 | -0.57 | -0.84 | -0.88 | -0.35 |
"The FACT-P is a multidimensional, self-report quality of life (QoL) instrument specifically designed for use with prostate cancer patients. It consists of 27 core items which assess patient function in four domains: Physical, Social/Family, Emotional, and Functional well-being, which is further supplemented by 12 site specific items to assess for prostate related symptoms. Each question is rated on a scale from 0 to 4, and then combined to produce sub-scale scores for each domain, as well as a global QoL score.~Emotional well-being consist of 6 items and scored on a scale of 0-4 (0=Not at all; 1=A little bit; 2=Somewhat; 3=Quite a bit; 4=Very much). Total score for the emotional well-being sub scale ranges from 0 to 24. Higher scores represent better QoL.Higher scores represent better QoL." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 8 | Phase B, Month 9 | Phase B, Month 10 | Phase B, Month 11 | Phase B, Month 12 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | 1.31 | 0.57 | 0.95 | 1.11 | 0.00 | 0.94 | 1.07 | 0.52 | 0.86 |
| DI (Degarelix Intermittent) | 0.69 | 0.67 | 0.65 | 0.75 | 1.09 | 0.82 | 0.99 | 0.74 | 0.40 |
| LC (Leuprolide Continuous) | 0.76 | 0.90 | 1.11 | 1.16 | 0.98 | 1.05 | 1.23 | 1.14 | 1.12 |
| Total Continuous | 0.88 | 0.83 | 1.08 | 1.15 | 0.77 | 1.03 | 1.20 | 1.01 | 1.06 |
The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function. Total SFI score ranges from 0 to 44. A higher scores represent better sexual function. (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -3.93 | -4.28 | -4.35 | -4.62 | -5.59 | -5.93 |
| DI (Degarelix Intermittent) | -4.07 | -5.20 | -4.97 | -3.56 | -3.37 | -3.27 |
| LC (Leuprolide Continuous) | -3.69 | -4.57 | -4.62 | -4.74 | -5.15 | -4.68 |
| Total Continuous | -3.74 | -4.51 | -4.56 | -4.71 | -5.24 | -4.94 |
"The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function.~Overall satisfaction domain consist of single question and is scored on a scale of 0-4 (0=minimum, 4=maximum). A higher score represent better sexual function." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.18 | -0.37 | -0.34 | -0.47 | -0.57 | -0.70 |
| DI (Degarelix Intermittent) | -0.32 | -0.28 | -0.33 | -0.15 | -0.11 | -0.12 |
| LC (Leuprolide Continuous) | -0.27 | -0.40 | -0.41 | -0.41 | -0.42 | -0.37 |
| Total Continuous | -0.25 | -0.39 | -0.39 | -0.42 | -0.45 | -0.44 |
"The SFI is a multidimensional, self-report instrument specifically designed to evaluate sexual function and satisfaction of men on treatment or with conditions that may affect sexual function. It consists of 11 questions which assess patient function in four domains: Sexual drive, Erection, Ejaculation, and Problem assessment, and a question in regards to overall assessment of sexual function.~Erection domain consist of 3 questions and are scored on a scale of 0-4 (0=minimum, 4=maximum). Total score for the erection domain ranges from 0 to 12. A higher scores represent better sexual function." (NCT00928434)
Timeframe: During 14 months
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Phase A, Month 3 | Phase A, Month 7 | Phase B, Month 9 | Phase B, Month 11 | Phase B, Month 13 | Phase B, Month 14 | |
| DC (Degarelix Continuous) | -0.91 | -1.06 | -1.07 | -1.34 | -1.36 | -1.43 |
| DI (Degarelix Intermittent) | -1.32 | -1.43 | -1.52 | -1.15 | -0.97 | -0.90 |
| LC (Leuprolide Continuous) | -1.21 | -1.34 | -1.46 | -1.28 | -1.33 | -1.26 |
| Total Continuous | -1.14 | -1.28 | -1.38 | -1.30 | -1.34 | -1.29 |
Percent change from Baseline in serum testosterone levels was measured. (NCT00928434)
Timeframe: Phase A Visit 1-8 and Phase B Visit 9-15.
| Intervention | Percent change (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase A, Visit 1 (Day 0) | Phase A, Visit 2 (Month 1) | Phase A, Visit 3 (Month 2) | Phase A, Visit 4 (Month 3) | Phase A, Visit 5 (Month 4) | Phase A, Visit 6 (Month 5) | Phase A, Visit 7 (Month 6) | Phase A, Visit 8 (Month 7) | Phase B, Visit 9 (Month 8) | Phase B, Visit 10 (Month 9) | Phase B, Visit 11 (Month 10) | Phase B, Visit 12 (Month 11) | Phase B, Visit 13 (Month 12) | Phase B, Visit 14 (Month 13) | Phase B, Visit 15 (Month 14) | |
| DC (Degarelix Continuous) | -95.8 | -97.4 | -97.5 | -97.8 | -97.7 | -97.6 | -97.6 | -97.5 | -97.1 | -97 | -97 | -96.7 | -96 | -96.5 | -95.8 |
| DI (Degarelix Intermittent) | NA | -96.4 | -97.3 | -97.5 | -97.2 | -97.3 | -96.8 | -96.9 | -95.6 | -88.7 | -77 | -65.4 | -54.7 | -51.9 | -44 |
| LC (Leuprolide Continuous) | NA | -95.5 | -97.7 | -97.5 | -96.2 | -97.8 | -97.9 | -97.7 | -97.8 | -97.7 | -97.5 | -97.9 | -97.8 | -97.4 | -97.7 |
Percentage of patients with serum PSA levels ≤4.0 ng/mL at 14 month was presented. (NCT00928434)
Timeframe: At 14 month
| Intervention | Percentage of patients (Number) |
|---|---|
| DI (Degarelix Intermittent) | 100 |
| Total Continuous | 98.4 |
Percentage of Subjects With a Serum PSA Level ≤4.0 ng/mL was measured during the study period. (NCT00928434)
Timeframe: At 14 months
| Intervention | Percentage of patients (Number) |
|---|---|
| DI (Degarelix Intermittent) | 100 |
| DC (Degarelix Continuous) | 97.6 |
| LC (Leuprolide Continuous) | 98.7 |
The time to return to normal range (≥1.5 ng/mL) or Baseline testosterone level in the DI group was counted from the start of Phase B at Day 196 (i.e. 28 days after last injection of degarelix). (NCT00928434)
Timeframe: During Phase B
| Intervention | Days (Median) |
|---|---|
| DI (Degarelix Intermittent) | 168 |
Percent change from Baseline in serum PSA levels during the study period was measured. (NCT00928434)
Timeframe: Phase A Visit 1-8 and Phase B Visit 9-15.
| Intervention | Percent change (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Phase A, Visit 1 (Day 0) | Phase A, Visit 2 (Month 1) | Phase A, Visit 3 (Month 2) | Phase A, Visit 4 (Month 3) | Phase A, Visit 5 (Month 4) | Phase A, Visit 6 (Month 5) | Phase A, Visit 7 (Month 6) | Phase A, Visit 8 (Month 7) | Phase B, Visit 9 (Month 8) | Phase B, Visit 10 (Month 9) | Phase B, Visit 11 (Month 10) | Phase B, Visit 12 (Month 11) | Phase B, Visit 13 (Month 12) | Phase B, Visit 14 (Month 13) | Phase B, Visit 15 (Month 14) | |
| DC (Degarelix Continuous) | -39.6 | -84.5 | -92.4 | -94.5 | -95.5 | -95.7 | -95.8 | -95.4 | -95.5 | -95.6 | -95.7 | -95.1 | -95.1 | -95.1 | -94.4 |
| DI (Degarelix Intermittent) | NA | -80.8 | -90.4 | -92.8 | -94.1 | -94.2 | -94.8 | -95.4 | -95.7 | -93.6 | -91.9 | -88 | -84.2 | -82.8 | -80.8 |
| LC (Leuprolide Continuous) | NA | -62.8 | -87.3 | -92.3 | -93.4 | -94.5 | -95.3 | -95.5 | -95.2 | -94.3 | -93.1 | -94.4 | -94.5 | -93.1 | -93.7 |
The EPIC assesses disease-specific aspects of prostate cancer and it's therapies and consists of four summary domains (bowel, urinary, sexual, and hormonal), each ranging from 0-100, with higher scores representing better health-related quality of life. Change is calculated as time point value - baseline value, such that a positive change indicates improvement. (NCT00936390)
Timeframe: Last week of RT (approximately 9 and 17 weeks from start of protocol treatment for Arm 1 and 2, respectively), then 6 months, 1 year and 5 years from end of RT.
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| End of RT | Six months post-RT | One year post-RT | Five years post-RT | |
| Dose-Escalated Radiation Therapy Alone | -1.8 | -0.7 | -0.8 | -0.3 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | -18.4 | -13.7 | -7.8 | -2.7 |
Common Terminology Criteria for Adverse Events (version 4.0) grades adverse event severity from 1=mild to 5=death. Summary data is provided in this outcome measure; see Adverse Events Module for specific adverse event data. Late adverse events are defined as occurring more than 30 days after the end of radiation therapy. Failure is defined as grade 3 or higher late adverse event. Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 12.8 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 15.2 |
Non-prostate cancer specific mortality is defined as a death without evidence of prostate cancer or a complication from treatment. . Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 9.1 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 9.0 |
Overall survival time is defined as time from randomization to the date of death from any cause or last known follow-up (censored). Overall survival rates are estimated by the Kaplan-Meier method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 90.0 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 91.0 |
Summary data is provided in this outcome measure; see Adverse Events Module for specific adverse event data. Acute adverse events are defined as occuring within 30 days of completion of radiation therapy. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years.
| Intervention | Participants (Count of Participants) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 152 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 504 |
Failure is defined as biochemical failure, local failure, or distant metastasis. Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 14.8 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 7.9 |
Salvage (non-protocol) ADT administration is defined as the first administration of subsequent ADT (either LHRH agonist or anti-androgen) Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Salvage ADT rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of salvage ADT times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 6.1 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 4.2 |
Prostate cancer specific mortality (failure) is defined as death due to prostate cancer or a complication from treatment. Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 0.90 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 0 |
"Distant metastasis (failure) is defined as metastatic disease documented by any method. If diagnosed on diagnostic imaging prompted by biochemical failure, then the event date will be the date of biochemical progression.~Failure time is defined as time from randomization to the date of first failure, last known follow-up (competing risk), or death without failure (censored). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported." (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 3.1 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 0.6 |
Local recurrence (failure) is defined as clinical (palpable) suspicion of local recurrence [this date is used] confirmed by biopsy. Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 2.6 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 0.6 |
The EPIC assesses disease-specific aspects of prostate cancer and it's therapies and consists of four summary domains (bowel, urinary, sexual, and hormonal), each ranging from 0-100, with higher scores representing better health-related quality of life. Change is calculated as time point value - baseline value, such that a positive change indicates improvement. (NCT00936390)
Timeframe: Last week of RT (approximately 9 and 17 weeks from start of protocol treatment for Arm 1 and 2, respectively), then 6 months, 1 year and 5 years from end of RT.
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| End of RT | Six months post-RT | One year post-RT | Five years post-RT | |
| Dose-Escalated Radiation Therapy Alone | -9.7 | -2.6 | -4.0 | -2.7 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | -10.5 | -3.8 | -5.2 | -2.9 |
The EPIC assesses disease-specific aspects of prostate cancer and it's therapies and consists of four summary domains (bowel, urinary, sexual, and hormonal), each ranging from 0-100, with higher scores representing better health-related quality of life. Change is calculated as time point value - baseline value, such that a positive change indicates improvement. (NCT00936390)
Timeframe: Last week of RT (approximately 9 and 17 weeks from start of protocol treatment for Arm 1 and 2, respectively), then 6 months, 1 year and 5 years from end of RT.
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| End of RT | Six months post-RT | One year post-RT | Five years post-RT | |
| Dose-Escalated Radiation Therapy Alone | -6.7 | -7.9 | -8.5 | -10.0 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | -22.6 | -19.9 | -16.6 | -9.6 |
The EPIC assesses disease-specific aspects of prostate cancer and it's therapies and consists of four summary domains (bowel, urinary, sexual, and hormonal), each ranging from 0-100, with higher scores representing better health-related quality of life. Change is calculated as time point value - baseline value, such that a positive change indicates improvement. (NCT00936390)
Timeframe: Last week of RT (approximately 9 and 17 weeks from start of protocol treatment for Arm 1 and 2, respectively), then 6 months, 1 year and 5 years from end of RT.
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| End of RT | Six months post-RT | One year post-RT | Five years post-RT | |
| Dose-Escalated Radiation Therapy Alone (Arm 1) | -12.4 | -0.1 | -1.9 | -0.4 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation (Arm 2) | -13.8 | -3.6 | -1.6 | 0.3 |
The PROMIS Fatigue short form 8a contains 8 questions, each with 5 responses ranging from 1 to 5, evaluating self-reported fatigue symptoms over the past 7 days. The total score is the sum of all questions which is then converted into a pro-rated T-score with a mean of 50 and standard deviation of 10, with a possible range of 33.1 to 77.8. Higher scores indicate more fatigue. Change is defined as value at one year - value at baseline. Positive change from baseline indicates increased fatigue at one year. (NCT00936390)
Timeframe: Last week of RT (approximately 9 and 17 weeks from start of protocol treatment for Arm 1 and 2, respectively), then 6 months, 1 year and 5 years from end of RT.
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| End of RT | Six months post-RT | One year post_RT | Five years post-RT | |
| Dose-Escalated Radiation Therapy Alone | 0.80 | 1.09 | 0.99 | 0.97 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 1.84 | 1.21 | 0.86 | 0.80 |
Overall survival time is defined as time from randomization to the date of death from any cause or last known follow-up (censored). Overall survival rates are estimated by the Kaplan-Meier method. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| EBRT | EBRT +LDR Brachytherapy Boost | EBRT +HDR Brachytherapy Boost | |
| Dose-Escalated Radiation Therapy Alone | 89.4 | 100 | 91.7 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 90.3 | 97.2 | 100 |
Biochemical failure is defined as an increase of at least 2 ng/ml above the nadir PSA. Failure time is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. Five-year rates are provided here. Analysis was planned to occur after 218 deaths were reported. (NCT00936390)
Timeframe: From randomization to last follow-up. Follow-up schedule: end of RT (2nd arm only), then every 3 months for a year, every 4 months for 4 years, then yearly. Maximum follow-up at time of analysis was 10.3 years. Five-year rates reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| Dose-Escalated Radiation Therapy Alone | 13.9 |
| Dose-Escalated Radiation Therapy and Short-Term Androgen-Deprivation | 7.7 |
Percentage of Participants with Grade 3 or Higher Adverse Events regardless of attribution per NCI CTCAE Version 3 (NCT00937768)
Timeframe: 2 years
| Intervention | percentage of patients (Number) |
|---|---|
| Androgen Deprivation Therapy | 100 |
| No Androgen Deprivation Therapy | 37.5 |
The number of deaths due to any cause are reported below. (NCT00937768)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Androgen Deprivation Therapy | 0 |
| No Androgen Deprivation Therapy | 0 |
The overall FACT-P Total Score at Baseline and months 3 and 6 mean and standard deviations are reported below. The FACT-P is a multidimensional, self-reported quality of life instrument consisting of 27 core items that assess participant function in 4 domains: physical, social/family, emotional, functional well-being, and supplemented by 12 site-specific items to assess for prostate-related symptoms. Each item is rated on a 0 to 4 Likert-type scale, and then combined to produce subscale scores for each domain, as well as a global quality of life score which is the sum of all 5 domain scores and ranges from 0 to 156 where higher scores represent better quality of life. (NCT00937768)
Timeframe: Baseline and months 3 and 6
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Baseline | Month 3 | Month 6 | |
| Androgen Deprivation Therapy | 122.7 | 118.6 | 109.4 |
| No Androgen Deprivation Therapy | 114.8 | 117.8 | 136.8 |
LASA Overall Quality of Life at Baseline, Months 3 and 6. Quality of Life (QOL) was measured using the single-item Linear Analogue Self Assessment (LASA) on a 0-10 scale, with 0=as bad as it can be and 10=as good as it can be. The average and standard deviation of the LASA overall quality of life score are reported below at baseline, months 3 and 6. (NCT00937768)
Timeframe: Baseline to Months 3 and 6
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Baseline | Month 3 | Month 6 | |
| Androgen Deprivation Therapy | 8.8 | 1.0 | 6.2 |
| No Androgen Deprivation Therapy | 6.9 | 7.0 | 8.7 |
Incidence of acute and chronic grade 3 or greater toxicity as evaluated using the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) version 3.0he distribution of time to late adverse events (observed severities of adverse events over time) will be estimated using the Kaplan-Meier method. (NCT01023061)
Timeframe: Up to 24 months after initiation of radiation therapy
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Antihormone Therapy and Radiation Therapy) | 6 |
Defined as the date of an increase of 2ng/mL or more above the Prostate specific antigen nadir achieved after completion of radiation with the date of progression defined as the date on which that value was measured. Distribution of time-to-event variables will be estimated using the Kaplan-Meier product-limit method. Estimated with two-sided 95% confidence intervals. (NCT01023061)
Timeframe: 6 months
| Intervention | years (Mean) |
|---|---|
| Treatment (Antihormone Therapy and Radiation Therapy) | 5 |
The levels from patients treated in this study will be compared to a control set of biopsies acquired from a separate but similar population of men with intermediate and high risk prostate cancer treated with three months of combined Luteinizing hormone releasing hormone agonist and bicalutamide as part of standard of care. (NCT01023061)
Timeframe: Week 12
| Intervention | pg/mg (Median) |
|---|---|
| Treatment (Antihormone Therapy and Radiation Therapy) | 0.050 |
Participants prostatic specific antigen (PSA) progression-free or event-free survival (that is, freedom from treatment failure) 1 year postoperatively. Treatment failure defined as objective tumor progression during therapy or in year after surgery, confirmed postoperative PSA ⩾1 ngml - 1, or any postoperative radiation, hormonal or other systemic therapy. Participants who did not undergo surgery within 8 weeks of completing 1 year of therapy on protocol (for any reason, including participant refusal) were counted as treatment failure, as were participants whose surgery was begun and aborted. (NCT01076335)
Timeframe: 1 Year
| Intervention | participants (Number) |
|---|---|
| Neoadjuvant Hormones + Docetaxel | 13 |
The International Prostate Symptom Score (IPSS) is used to assess the severity of lower urinary tract symptoms (LUTS) and to monitor disease progression. The IPSS is calculated from 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, and straining [rated as 0 (not at all) to 5 (almost always)], as well as how many times on average a participant has to get up to urinate at night (0=none to 5=5 times or more). The total score is classified as follows: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT01078545)
Timeframe: Baseline to 3, 6, 9, and 12 months.
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| IPSS at Baseline (n=727) | IPSS at month 3 (n=724) | IPSS at month 6 (n=717) | IPSS at month 9 (n=702) | IPSS at month 12 (n=699) | |
| Advanced PCa Patients With LUTS Treated With GnRH Analogue | 17.8 | 14.0 | 12.3 | 10.9 | 10.0 |
The International Prostate Symptom Score (IPSS) is used to assess the severity of lower urinary tract symptoms (LUTS) and to monitor disease progression. The IPSS is calculated from 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, and straining [rated as 0 (not at all) to 5 (almost always)], as well as how many times on average a participant has to get up to urinate at night (0=none to 5=5 times or more). The total score is classified as follows: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT01078545)
Timeframe: Baseline to 12 months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| IPSS at Baseline (n=727) | IPSS at 12 months (n=699) | |
| Advanced PCa Patients With LUTS Treated With GnRH Analogue | 17.8 | 10.0 |
Changes in the intensity of the following symptoms connected with prostate cancer: hematospermia (blood in the sperm), lower abdominal pain, urine incontinence, erectile dysfunction, crotch pain, anal pain or bleeding, lumbar/back pain, bone pain, spinal compression symptoms, peripheral lymph node enlargement, and lymphatic oedema of lower extremities. The intensity of each symptom was rated by the participant from 1 (minimum) to 7 (maximum). Zero indicates that the symptom was not present. (NCT01078545)
Timeframe: Baseline to 3, 6, 9, and 12 months.
| Intervention | Units on a scale (Median) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Hematospermia (Baseline; n=729) | Lower abdominal pain (Baseline; n=729) | >Month 3 (n=726) | Urinary incontinence (Baseline; n=729) | Erectile dysfunction (Baseline; n=729) | Crotch pain (Baseline; n=729) | Anal pain or bleeding (Baseline; n=729) | Lumbar/back pain (Baseline n=729) | Bone pain (Baseline; n=729) | >Month 9 (n=704) | >Month 12 (n=703) | Spinal compression symptoms (Baseline; n=729) | Periph. lymph node enlargement (Baseline; n=729) | Lymphatic oedema, lower extrem. (Baseline; n=729) | >Month 6 (n=719) | |||||||||||||||||||||||||||||||||||||||||
| Advanced PCa Patients With LUTS Treated With GnRH Analogue | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 4 | 5 | 5 | 6 | 6 | 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 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Percentage of participants at baseline with one of the following symptoms connected with prostate cancer: hematospermia (blood in the sperm), lower abdominal pain, urine incontinence, erectile dysfunction, crotch pain, anal pain or bleeding, lumbar/back pain, bone pain, spinal compression symptoms, peripheral lymph node enlargement, and lymphatic oedema of lower extremities. The intensity of each symptom was rated by the participant from 1 (minimum) to 7 (maximum). Zero indicates that the symptom was not present. (NCT01078545)
Timeframe: Baseline
| Intervention | Percentage of participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Hematospermia | Lower abdominal pain | Urine incontinence | Erectile dysfunction | Crotch pain | Anal pain or bleeding | Lumbar/back pain | Bone pain | Spinal compression symptoms | Peripheral lymph node enlargement | Lymphatic oedema of the lower extremities | |
| Advanced PCa Patients With LUTS Treated With GnRH Analogue | 3 | 31 | 13 | 62 | 24 | 2 | 15 | 17 | 1 | 2 | 6 |
Adverse events (AEs) were collected during the course of the study from the first visit (Baseline) through the last visit (12 months). The number of participants experiencing a non-serious or serious adverse event or both types of events are summarized. See the Reported Adverse Event section for details. (NCT01078545)
Timeframe: Baseline to 12 months
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Experienced a serious AE | Experienced a non-serious AE | Experienced both a serious AE and non-serious AE | |
| Advanced PCa Patients With LUTS Treated With GnRH Analogue | 5 | 3 | 1 |
In this case, a CT or MRI is considered positive when lymph nodes are detectable. A CT or MRI is considered negative when lymph nodes are not detectable. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | |
|---|---|---|
| Positive at baseline | Negative at baseline | |
| Advanced Prostate Cancer Participants | 374 | 1212 |
The number of participants by race at baseline is presented. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Black | Caucasian | Other | |
| Advanced Prostate Cancer Participants | 59 | 2154 | 4 |
The mean PSA in ng/mL to screen and assess for the recurrence of prostate cancer at each visit is presented. (NCT01081873)
Timeframe: time 0 (Baseline), month 3, and every 3 months until disease progression or up to 24 months, whichever came first
| Intervention | ng/mL (Mean) |
|---|---|
| Advanced Prostate Cancer Participants at Baseline | 62.16 |
| Advanced Prostate Cancer Participants at Month 3 | 12.95 |
| Advanced Prostate Cancer Participants at Month 6 | 6.23 |
| Advanced Prostate Cancer Participants at Month 9 | 8.01 |
| Advanced Prostate Cancer Participants at Month 12 | 8.41 |
| Advanced Prostate Cancer Participants at Month 15 | 8.88 |
| Advanced Prostate Cancer Participants at Month 18 | 9.57 |
| Advanced Prostate Cancer Participants at Month 21 | 23.02 |
| Advanced Prostate Cancer Participants at Month 24 | 15.29 |
| Advanced Prostate Cancer Participants - Last Available Record | 30.32 |
The number of participants with tumor stages T0, T1, T2, T3, and T4 as reported by the physician or pathologist is summarized. T0: no evidence of primary tumor. T1: histologic tumor confined to prostate; clinically unapparent tumor, undetectable by digital rectal examination or by ultrasound. T2: tumor is confined to prostrate and can be detected by digital rectal examination. T3: tumor extends through the prostate capsule but has not spread to other organs. T4: tumor has invaded adjacent structures/organs other than seminal vesicles. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| T0 stage | T1 stage | T2 stage | T3 stage | T4 stage | |
| Advanced Prostate Cancer Participants | 30 | 223 | 614 | 1215 | 220 |
Among those participants with a positive biopsy at baseline, the number of participants with adenocarcinoma tissue or other tissue type is summarized. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | ||
|---|---|---|---|
| Adenocarcinoma | Other | Not done | |
| Advanced Prostate Cancer Participants at Baseline | 2269 | 9 | 1 |
Prostate cancer treatment for all participants is summarized by the number of participants at each visit who took any Lucrin/Lucrin Tridepot, LHRH agonist, anti-androgens, or other drug treatments, or who had any type of surgery or radiotherapy (external radiation or brachytherapy). (NCT01081873)
Timeframe: time 0 (Baseline), month 3, and every 3 months until disease progression or up to 24 months, whichever came first
| Intervention | participants (Number) | ||||||
|---|---|---|---|---|---|---|---|
| Any Lucrin or Lucrin Tridepot used at each visit | Any LHRH agonist treatments used at each visit | Any anti-androgen treatments used at each visit | Other drug treatments used at each visit | Any surgery performed any time up to the visit | External radiation performed any time up to visit | Brachytherapy performed any time up to the visit | |
| Advanced Prostate Cancer Participants - Use at Any Visit | 2384 | 2392 | 1021 | 86 | 281 | 228 | 26 |
| Advanced Prostate Cancer Participants at Baseline | 2028 | 2034 | 841 | 31 | 244 | 129 | 13 |
| Advanced Prostate Cancer Participants at Month 12 | 969 | 973 | 397 | 31 | 127 | 79 | 10 |
| Advanced Prostate Cancer Participants at Month 15 | 540 | 545 | 223 | 27 | 92 | 43 | 9 |
| Advanced Prostate Cancer Participants at Month 18 | 629 | 636 | 261 | 24 | 94 | 56 | 9 |
| Advanced Prostate Cancer Participants at Month 21 | 450 | 452 | 182 | 23 | 80 | 33 | 8 |
| Advanced Prostate Cancer Participants at Month 24 | 1628 | 1635 | 603 | 57 | 192 | 133 | 21 |
| Advanced Prostate Cancer Participants at Month 3 | 1011 | 1015 | 388 | 22 | 145 | 84 | 10 |
| Advanced Prostate Cancer Participants at Month 6 | 817 | 821 | 303 | 21 | 103 | 76 | 10 |
| Advanced Prostate Cancer Participants at Month 9 | 640 | 643 | 243 | 24 | 97 | 73 | 11 |
The prognosis for participants is summarized for each visit by the number of participants at each visit with a survival prognosis of 10 years, 5 - 10 years, 1 - 5 years, 6 - 12 months, and < 6 months. Methods for determining survival prognosis were not prespecified, but were based on the judgement of each Investigator. (NCT01081873)
Timeframe: time 0 (Baseline), month 3, and every 3 months thereafter until disease progression or up to 24 months, whichever came first
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| > 10 years | 5 - 10 years | 1 - 5 years | 6 - 12 months | < 6 months | |
| Advanced Prostate Cancer Participants - Last Available Record | 331 | 1173 | 735 | 93 | 33 |
| Advanced Prostate Cancer Participants at Baseline | 395 | 1041 | 663 | 26 | 3 |
| Advanced Prostate Cancer Participants at Month 12 | 113 | 479 | 268 | 18 | 3 |
| Advanced Prostate Cancer Participants at Month 15 | 75 | 276 | 140 | 15 | 3 |
| Advanced Prostate Cancer Participants at Month 18 | 82 | 309 | 182 | 13 | 7 |
| Advanced Prostate Cancer Participants at Month 21 | 66 | 225 | 117 | 12 | 6 |
| Advanced Prostate Cancer Participants at Month 24 | 206 | 805 | 420 | 48 | 16 |
| Advanced Prostate Cancer Participants at Month 3 | 132 | 476 | 312 | 15 | 6 |
| Advanced Prostate Cancer Participants at Month 6 | 100 | 402 | 237 | 10 | 3 |
| Advanced Prostate Cancer Participants at Month 9 | 91 | 320 | 180 | 11 | 2 |
The number of participants at baseline who were positive or negative for tumors via a rectal examination, prostate biopsy, echograph of the hyperechogenic zones, or MRI are provided. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | |
|---|---|---|
| Positive at baseline | Negative at baseline | |
| Advanced Prostate Cancer Participants - Echograph | 1806 | 446 |
| Advanced Prostate Cancer Participants - MRI | 102 | 85 |
| Advanced Prostate Cancer Participants - Prostate Biopsy | 2355 | 9 |
| Advanced Prostate Cancer Participants - Rectal Examination | 2045 | 439 |
The number of participants with metastases that are absent, local tumor, single metastases, multiple metastases in 1 organ, and multiple metastases in multiple organs at each visit is summarized. (NCT01081873)
Timeframe: time 0 (Baseline), month 3, and every 3 months until disease progression or up to 24 months, whichever came first
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Absent | Local tumor | Single metastases | Multiple metastases in 1 organ | Multiple metastases in multiple organs | |
| Advanced Prostate Cancer Participants - Last Available Record | 870 | 64 | 100 | 268 | 109 |
| Advanced Prostate Cancer Participants at Baseline | 782 | 64 | 108 | 233 | 75 |
| Advanced Prostate Cancer Participants at Month 12 | 74 | 2 | 3 | 18 | 12 |
| Advanced Prostate Cancer Participants at Month 15 | 33 | 1 | 2 | 13 | 5 |
| Advanced Prostate Cancer Participants at Month 18 | 44 | 0 | 3 | 10 | 7 |
| Advanced Prostate Cancer Participants at Month 21 | 29 | 3 | 2 | 13 | 5 |
| Advanced Prostate Cancer Participants at Month 24 | 188 | 10 | 15 | 63 | 34 |
| Advanced Prostate Cancer Participants at Month 3 | 59 | 10 | 8 | 27 | 15 |
| Advanced Prostate Cancer Participants at Month 6 | 45 | 3 | 3 | 18 | 4 |
| Advanced Prostate Cancer Participants at Month 9 | 28 | 3 | 2 | 13 | 10 |
Response to treatment is summarized by the number of participants at each visit with a complete or partial response, stable disease, or progressive disease. Disease status determination was not predefined, but was based on the judgement of each Investigator. (NCT01081873)
Timeframe: month 3, and every 3 months until disease progression or up to 24 months, whichever came first
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Complete response | Partial response | Stable disease | Progressive disease | |
| Advanced Prostate Cancer Participants - Last Available Record | 1420 | 284 | 224 | 282 |
| Advanced Prostate Cancer Participants at Month 12 | 668 | 181 | 97 | 85 |
| Advanced Prostate Cancer Participants at Month 15 | 347 | 97 | 69 | 52 |
| Advanced Prostate Cancer Participants at Month 18 | 401 | 98 | 102 | 78 |
| Advanced Prostate Cancer Participants at Month 21 | 276 | 59 | 73 | 67 |
| Advanced Prostate Cancer Participants at Month 24 | 1181 | 199 | 200 | 184 |
| Advanced Prostate Cancer Participants at Month 3 | 525 | 379 | 97 | 37 |
| Advanced Prostate Cancer Participants at Month 6 | 496 | 231 | 89 | 37 |
| Advanced Prostate Cancer Participants at Month 9 | 402 | 139 | 83 | 46 |
The number of participants at baseline with a positive or negative bone scan was summarized. Determination of bone scan status was based on the interpretation of the Investigator or radiologist. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | |
|---|---|---|
| Positive at baseline | Negative at baseline | |
| Advanced Prostate Cancer Participants | 497 | 1353 |
The mean weight of all participants at baseline is provided. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | kg (Mean) |
|---|---|
| Advanced Prostate Cancer Participants | 77.36 |
The number of participants experiencing a serious adverse event during the course of the study is summarized. See the Reported Adverse Event section for details. (NCT01081873)
Timeframe: Baseline to disease progression or 24 months, whichever came first
| Intervention | participants (Number) |
|---|---|
| Advanced Prostate Cancer Participants | 121 |
The median, minimum, and maximum PSA values in ng/mL at baseline are provided. The mean PSA at baseline is reported in the Primary Outcome Measure section above. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | ng/mL (Median) |
|---|---|
| Advanced Prostate Cancer Participants | 13.66 |
The mean age of all participants at baseline is provided. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | years (Mean) |
|---|---|
| Advanced Prostate Cancer Participants | 75.39 |
The number of participants at baseline reported to be in metastasis stage M0 or M1 is summarized. M0: no distant metastasis. M1: metastasis to distant organs beyond regional lymph nodes. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | |
|---|---|---|
| M0 stage | M1 stage | |
| Advanced Prostate Cancer Participants | 1373 | 501 |
N0: tumor cells absent from regional lymph nodes. N1: regional lymph node metastasis present. (NCT01081873)
Timeframe: at time 0 (Baseline)
| Intervention | participants (Number) | |
|---|---|---|
| N0 stage | N1 stage | |
| Advanced Prostate Cancer Participants | 1296 | 360 |
The table below shows number of participants in each treatment group with a pathology tumor stage less than or equal to pT2. (NCT01088529)
Timeframe: At the end of Cycle 3 (at radical prostatectomy)
| Intervention | participants (Number) |
|---|---|
| AA+LHRHa | 24 |
| LHRHa | 8 |
The table below shows number of participants in each treatment group who had positive surgical margins. A positive surgical margin is defined as tumor extending to the inked-surface or margin of the prostate. (NCT01088529)
Timeframe: At the end of Cycle 3 (at radical prostatectomy)
| Intervention | participants (Number) |
|---|---|
| AA+LHRHa | 6 |
| LHRHa | 6 |
The table below shows number of participants in each treatment group who achieved a prostate-specific antigen (PSA) response defined as a drop in PSA value to less than or equal to 0.2 ng/mL. (NCT01088529)
Timeframe: Cycle 3 Day 1
| Intervention | participants (Number) |
|---|---|
| AA+LHRHa | 32 |
| LHRHa | 0 |
Wake after sleep onset (WASO) is calculated by averaging the number of minutes spent awake after initiating sleep each night from the two ambulatory polysomnography studies conducted at baseline and the two ambulatory polysomnography studies conducted four weeks after the GnRHa injection. (NCT01116401)
Timeframe: baseline and 4 weeks
| Intervention | percent change (Number) |
|---|---|
| GnRH Agonist Injection | 62 |
The Montgomery-Åsberg Depression Rating Scale is a widely used 10-item clinician-rated scale that describes the severity of depressive symptoms. It has a range of 0-60 with higher scores indicating greater symptom burden. Participants were assessed at baseline and four weeks after the GnRHa injection in order to calculate the change in MADRS score. (NCT01116401)
Timeframe: baseline and 4 weeks
| Intervention | units on a scale (Mean) |
|---|---|
| GnRH Agonist Injection | 3.1 |
The Friedman test will be used to evaluate correlations between microRNA measures (CT) and 28-week PSA response. (NCT01120236)
Timeframe: Baseline to 28 weeks
| Intervention | Cycle Threshold (CT) (Median) | ||||
|---|---|---|---|---|---|
| miR-141 | miR-200a | miR-200b | miR-210 | miR-375 | |
| PSA Complete Response | 32.6 | 34.5 | 33.6 | 32.5 | 33.0 |
| PSA Non-Responders | 31.5 | 33.8 | 32.6 | 32.3 | 29.5 |
| PSA Partial Response | 32.0 | 33.8 | 33.6 | 32.1 | 32.6 |
Undetectable PSA rate (<= 0.2 ng/mL) after seven cycles (28 weeks) of protocol treatment (NCT01120236)
Timeframe: 7 months
| Intervention | participants (Number) |
|---|---|
| Arm I (Androgen Deprivation and Cixutumumab) | 42 |
| Arm II (Androgen Deprivation Therapy) | 34 |
Only adverse events that are possibly, probably or definitely related to study drug are reported. (NCT01120236)
Timeframe: Up to 28 weeks
| Intervention | Participants (Number) | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Alanine aminotransferase increased | Anemia | Anxiety | Aspartate aminotransferase increased | Cognitive disturbance | Depression | Erectile dysfunction | Exostosis | Glucose intolerance | Hot flashes | Hypercalcemia | Hyperglycemia | Hypertension | Hypertriglyceridemia | Left ventricular systolic dysfunction | Nausea | Obesity | Soft tissue infection | Urinary tract infection | Urinary tract obstruction | Vomiting | |
| Arm I (Androgen Deprivation and Cixutumumab) | 1 | 1 | 0 | 1 | 1 | 0 | 1 | 1 | 0 | 1 | 2 | 8 | 2 | 1 | 1 | 1 | 1 | 1 | 1 | 0 | 1 |
| Arm II (Androgen Deprivation Therapy) | 0 | 1 | 1 | 0 | 0 | 1 | 0 | 0 | 1 | 1 | 0 | 0 | 2 | 0 | 0 | 0 | 1 | 0 | 0 | 1 | 0 |
The Friedman test will be used to evaluate correlations between microRNA measures (CT) and Baseline CTCs. (NCT01120236)
Timeframe: Baseline
| Intervention | Cycle Threshold (CT) (Median) | ||||
|---|---|---|---|---|---|
| miR-141 | miR-200a | miR-200b | miR-210 | miR-375 | |
| CTC= 1-4 | 32.7 | 34.7 | 33.2 | 32.7 | 32.7 |
| CTC= 5+ | 31.9 | 33.0 | 33.6 | 32.1 | 30.2 |
| CTC=0 | 33.0 | 34.4 | 33.4 | 32.5 | 32.8 |
A partial PSA response is considered <= 4 ng/mL (NCT01120236)
Timeframe: Up to 5 years
| Intervention | participants (Number) |
|---|---|
| Arm I (Androgen Deprivation and Cixutumumab) | 46 |
| Arm II (Androgen Deprivation Therapy) | 56 |
Serum samples and peripheral blood mononuclear cells (PBMNC) for pharmacodynamic activity with potential biomarkers for IMC-A12 (including, but not limited to: IGFBP2, IGFBP3 and Growth Hormone) obtained from optional blood specimens both before initiation of androgen deprivation therapy and twelve weeks after initiation of combined therapy. Results are reported as the difference between baseline and 12 weeks after start of therapy. (NCT01120236)
Timeframe: Baseline to 12 weeks
| Intervention | pg/mL (Mean) | ||
|---|---|---|---|
| IGFBP-I | IGFBP-III | GH | |
| Arm I (Androgen Deprivation and Cixutumumab) | -946 | 13893 | 66 |
| Arm II (Androgen Deprivation Therapy) | -904 | 291 | -25 |
Serum samples and peripheral blood mononuclear cells (PBMNC) for pharmacodynamic activity with potential biomarkers for IMC-A12 (including, but not limited to: IGF-I, free IGF-I and C-peptide) obtained from optional blood specimens both before initiation of androgen deprivation therapy and twelve weeks after initiation of combined therapy. Results are reported as the difference between baseline and 12 weeks after start of therapy. (NCT01120236)
Timeframe: Baseline to 12 weeks
| Intervention | ng/mL (Mean) | ||
|---|---|---|---|
| C-peptide | IGF-I | IGF-II | |
| Arm I (Androgen Deprivation and Cixutumumab) | -7 | 0 | 10 |
| Arm II (Androgen Deprivation Therapy) | 3 | 1 | -6 |
Serum samples and peripheral blood mononuclear cells (PBMNC) for pharmacodynamic activity with potential biomarkers for IMC-A12 (insulin) obtained from optional blood specimens both before initiation of androgen deprivation therapy and twelve weeks after initiation of combined therapy. Results are reported as the difference between baseline and 12 weeks after start of therapy. (NCT01120236)
Timeframe: Baseline to 12 weeks
| Intervention | ulU/mL (Mean) |
|---|---|
| Arm I (Androgen Deprivation and Cixutumumab) | 0 |
| Arm II (Androgen Deprivation Therapy) | 0 |
To Evaluate the time to testosterone recovery, which is defined as a return to with in 90% of pretreatment level, after 6 months of neo-adjuvant treatment with Eligard 22.5mg with Radiation Therapy in patients with early prostate Cancer (NCT01136226)
Timeframe: 6 mos
| Intervention | Months (Mean) |
|---|---|
| Single Arm- Eligard | 6 |
Questionnaire responses recorded on a Visual Analog Scale (VAS), which has a range of 0-100 mm, assessed approximately 15 minutes post-injection (NCT01161563)
Timeframe: 15 minutes
| Intervention | units on a scale (Mean) |
|---|---|
| Leuprolide Acetate | 20.53 |
| Triptorelin Pamoate | 5.88 |
Questionnaire responses recorded on a Visual Analog Scale (VAS), which has a range of 0-100 mm, assessed approximately 15 minutes post-injection (NCT01161563)
Timeframe: 15 minutes
| Intervention | units on a scale (Mean) |
|---|---|
| Leuprolide Acetate | 23.87 |
| Triptorelin Pamoate | 5.84 |
Immunological response assays were measured at several time points starting at baseline until the eighth week after starting the medicine for each participant. The immunological responses measured were Cluster of Differentiation 4 (CD4), Cluster of Differentiation 8 (CD8) and Inducible T-cell Costimulatory (ICOS) markers. T-cells with the CD4 marker help coordinate the immune system response to an invader. Killer T-cells have the CD8 marker and are responsible for killing the invader. ICOS is a molecule which stimulates the activity of the immune response of the killer T-Cells and memory T cells. Participants with at least a 2 fold increase in the presence of CD4, CD8, or ICOS markers from the participant's baseline measure were considered a responder for that marker. (NCT01194271)
Timeframe: Baseline to Week 8
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| CD4 | CD8 | ICOS | |
| Neoadjuvant Ipilimumab | 12 | 7 | 9 |
AMH level ≤1.0 predicts onset of menopause within 5 years in normal women (NCT01257802)
Timeframe: baseline and 6 months
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Baseline AMH level ≤1.0 ng/ml | Baseline AMH level >1 ng/ml | 6 Month AMH level ≤1.0 ng/ml | 6 Month AMH level >1 ng/ml | |
| LUPRON | 3 | 3 | 4 | 1 |
| PLACEBO | 6 | 1 | 1 | 0 |
Mean antral follicle count (AFC) is the average number of follicles counted in each of 2 ovaries (NCT01257802)
Timeframe: baseline and 6 months
| Intervention | # of ovarian follicles (Mean) | |
|---|---|---|
| Baseline Mean antral follicle count (AFC) | 6 Month Mean antral follicle count (AFC) | |
| LUPRON | 10.3 | 2.5 |
| PLACEBO | 14.4 | 17.7 |
Mean ovarian volume reflects the preservation of ovarian tissue despite exposure to cyclophosphamide; reduced ovarian size is documented in cyclophosphamide treated patients (NCT01257802)
Timeframe: baseline and 6 months
| Intervention | cubic centimeters (Mean) | |
|---|---|---|
| Baseline mean ovarian volume | 6 Month mean ovarian volume | |
| LUPRON | 9.59 | 4.26 |
| PLACEBO | 7.68 | 6.97 |
AMH was quantified in vitro a commercially available enzyme linked immunosorbent assay (ELISA) (Beckman Coulter; Marseille, France) was used for in vitro quantitative measurement of serum AMH. (NCT01257802)
Timeframe: Day 0 to 6-month post-intervention visit
| Intervention | ng/ml (Mean) | |
|---|---|---|
| Baseline AMH (ng/ml) | 6 month AMH (ng/ml) | |
| LUPRON | 2.07 | 0.72 |
| Placebo | 3.87 | 0.24 |
An AMH level of >1 ng/ml and/or an antral follicle count of >4 in either ovary is a strong predictor of residual ovarian function (NCT01257802)
Timeframe: baseline and 6 months
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Baseline AMH >1 ng/ml or AFC>4 | 6 Month AMH >1 ng/ml or AFC>4 | |
| LUPRON | 4 | 1 |
| PLACEBO | 6 | 0 |
Clinical pregnancy was confirmed by observing fetal cardiac activity on transvaginal ultrasound four weeks after a positive pregnancy test. (NCT01269125)
Timeframe: June 2004-August 2010
| Intervention | percentage (Mean) |
|---|---|
| Endometriosis, GnRH-a Treatment, IVF | 28.3 |
| Endometriosis, IVF | 25.4 |
| Tubal Infertility, IVF | 33.3 |
The fertilization rate was estimated for every woman 24 hours after oocyte retrieval (NCT01269125)
Timeframe: June 2004-August 2010
| Intervention | percentage (Mean) |
|---|---|
| Endometriosis, GnRH-a Treatment, IVF | 73.7 |
| Endometriosis, IVF | 62.7 |
| Tubal Infertility, IVF | 75.7 |
TNF-a was measured in the FF of all women (secondary outcome measures). To prevent any cytokine alterations, only blood-free samples were used. (NCT01269125)
Timeframe: June 2004-August 2010
| Intervention | pg/ml (Mean) | ||||
|---|---|---|---|---|---|
| TNF-a | IL-1β | IL-6 | IL-8 | IL-1-ra | |
| Endometriosis, GnRH-a Treatment, IVF | 21.4 | 3.1 | 16.7 | 238.1 | 166.6 |
| Endometriosis, IVF | 38.6 | 9.3 | 32.1 | 347.8 | 183 |
| Tubal Infertility, IVF | 22.5 | 2.9 | 14.7 | 241 | 151.7 |
Embryo development was evaluated 2 days after oocyte pick-up. The number of blastomeres and the proportion of embryo volume occupied by fragments were used for the evaluation. Embryos with < 10%, < 10-20%, < 20-30% and >30% fragments were estimated as grade 1,2,3 and 4, respectively. (NCT01269125)
Timeframe: June 2004-August 2010
| Intervention | Percentage of grade 1 embryos (Mean) |
|---|---|
| Endometriosis, GnRH-a Treatment, IVF | 25.5 |
| Endometriosis, IVF | 22.6 |
| Tubal Infertility, IVF | 27.0 |
Clinical pregnancy rate was confirmed by observing fetal cardiac activity on transvaginal ultrasound four weeks after a positive pregnancy test. (NCT01269125)
Timeframe: 4 weeks after a positive pregnancy test
| Intervention | Percentage (Mean) |
|---|---|
| Endometriosis, GnRH-a Treatment, IVF | 28.3 |
| Endometriosis, IVF | 25.4 |
| Tubal Infertility, IVF | 33.3 |
(NCT01326312)
Timeframe: 60 days
| Intervention | participants (Number) |
|---|---|
| GTx- 758 1000mg | 19 |
| GTx-758 2000mg | 34 |
| Lupron Depot | 43 |
(NCT01326312)
Timeframe: 12 months
| Intervention | Participants (Count of Participants) |
|---|---|
| GTx- 758 1000mg | 0 |
| GTx-758 2000mg | 3 |
| Lupron Depot | 9 |
Median time to castration was summarized using the Kaplan-Meier method. (NCT01326312)
Timeframe: 60 days
| Intervention | days (Median) |
|---|---|
| GTx-758 1000mg | 29 |
| GTx-758 2000mg | 21 |
| Lupron Depot | 21 |
18F-FLT imaging was performed serially on patients post transplant to identify the level of uptake of 18F-FLT at a day +5 to +12 scan and the day at which neutrophils recover to >500 (i.e., subclinical bone-marrow recovery within 5 days of Bone Marrow Transplantation (BMT infusion)). On each image for each patient, the region of interest was drawn within each thoracic medullary space (n=12), generating the SUV for each space. The mean of these was calculated for each scan. The analysis was the median of the means of the SUV of the thorax values of the day 5-12 scan (averaged the SUV of the thorax for each patient and then took the medians of these). (NCT01338987)
Timeframe: 18F FLT scan done between days +5 to +12 and then time from that scan to engraftment measured
| Intervention | Days (Median) | |
|---|---|---|
| Patients with SUV 1.4 or greater | Patients with SUV less than 1.4 | |
| Transplant Recipient | 5 | 15 |
B cell percentage is defined as the percentage of lymphocytes that are B cells. (NCT01338987)
Timeframe: after first Bone Marrow Transplant, approximately 12 months post-transplant
| Intervention | percentage of cells (Median) | ||
|---|---|---|---|
| Males that received leuprolide | Males that did not receive leuprolide | Females who all received leuprolide | |
| Transplant Recipient | 22.1 | 21.9 | 14.3 |
Serious and non-serious adverse events were assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT01338987)
Timeframe: 12 months after second BMT
| Intervention | Adverse Events (Number) |
|---|---|
| Transplant Recipient - 2nd Bone Marrow Transplant | 0 |
Here is the count of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria in Adverse Events (CTCAE v4.0). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT01338987)
Timeframe: Date treatment consent signed to date off study, approximately 79 months and 11 days.
| Intervention | Participants (Count of Participants) |
|---|---|
| Males That Did Not Receive Leuprolide for 1st Transplant | 10 |
| Males Randomized to Receive Leuprolide for 1st Transplant | 8 |
| Females That Received Leuprolide for 1st Transplant | 20 |
| Matched Related Donors for Transplant | 4 |
| Recipients of 2nd Transplant | 2 |
Comparison of treatment arms; interventional versus observational average LH levels during study. (NCT01343368)
Timeframe: Baseline
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 19.8 |
| Observational Arm | 6.8 |
Comparison of treatment arms; interventional versus observational average FSH levels. (NCT01343368)
Timeframe: Baseline
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 9.3 |
| Observational Arm | 4.4 |
Comparison of treatment arms; interventional versus observational average FSH levels. (NCT01343368)
Timeframe: 2 years
| Intervention | IU/L (Mean) |
|---|---|
| Observational Arm | 7.1 |
Comparison of treatment arms; interventional versus observational average AMH levels after receiving transplant. (NCT01343368)
Timeframe: Day Prior to Transplant
| Intervention | ng/ml (Mean) |
|---|---|
| Interventional - Received Leuprolide | 0.6 |
| Observational Arm | 6.4 |
Comparison of treatment arms; interventional versus observational average AMH levels after receiving transplant. (NCT01343368)
Timeframe: Day 180 after Transplant
| Intervention | ng/ml (Mean) |
|---|---|
| Interventional - Received Leuprolide | 0.08 |
Comparison of treatment arms; interventional versus observational. Ovarian failure rate is based on FSH measured at 180 days after HCT; to determine the effect of GnRH agonists on the incidence of ovarian failure (i.e. FSH >40 IU/L) after transplant. (NCT01343368)
Timeframe: Through Day 180 Post Transplant
| Intervention | Participants (Count of Participants) |
|---|---|
| Interventional - Received Leuprolide | 3 |
| Observational Arm | 1 |
Comparison of treatment arms; interventional versus observational average FSH levels. (NCT01343368)
Timeframe: 1 year
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 61.5 |
| Observational Arm | 48.8 |
Comparison of treatment arms; interventional versus observational. Count of patients who stopped menstrual bleeding; to determine how the effect of GnRH agonists are at suppressing menses during hematopoietic cell transplant (NCT01343368)
Timeframe: From Baseline Through Day 365
| Intervention | Participants (Count of Participants) |
|---|---|
| Interventional - Received Leuprolide | 2 |
| Observational Arm | 0 |
Comparison of treatment arms; interventional versus observational. Count of patients who resumed menses after hematopoietic cell transplant (NCT01343368)
Timeframe: Day 365 Post Transplant
| Intervention | Participants (Count of Participants) |
|---|---|
| Interventional - Received Leuprolide | 2 |
| Observational Arm | 4 |
Comparison of treatment arms; interventional versus observational average LH levels during study. (NCT01343368)
Timeframe: Day 180
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 31.1 |
| Observational Arm | 4.3 |
Comparison of treatment arms; interventional versus observational average LH levels during study. (NCT01343368)
Timeframe: Day 100
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 2.4 |
| Observational Arm | 6.4 |
Comparison of treatment arms; interventional versus observational average LH levels during study. (NCT01343368)
Timeframe: 1 year
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 31.9 |
| Observational Arm | 27.8 |
Comparison of treatment arms; interventional versus observational average LH levels during study. (NCT01343368)
Timeframe: 2 years
| Intervention | IU/L (Mean) |
|---|---|
| Observational Arm | 5.6 |
Comparison of treatment arms; interventional versus observational average FSH levels. (NCT01343368)
Timeframe: Day 180
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 47.0 |
| Observational Arm | 4.7 |
Comparison of treatment arms; interventional versus observational average FSH levels. (NCT01343368)
Timeframe: Day 100
| Intervention | IU/L (Mean) |
|---|---|
| Interventional - Received Leuprolide | 18.4 |
| Observational Arm | 9.1 |
"CD8 T-cells are known as cytotoxic T-cells or killer T-cells. When the resting CD8 T-cells are activated, the activated CD8 T-cells multiple to fight a specific target so creating a group of specifically activated T-cells. This test measured the minimal number of clonal expansions of CD8 T-cells that always preceded an adverse response to treatment that was due to increased activity in the immune system itself. The minimal number of clonal expansion points to what this increased activity in the immune system might look like." (NCT01377389)
Timeframe: Each evaluable patient was followed from the time of their first dose until 30 days after their last dose of study drug
| Intervention | clonal expansions (Number) |
|---|---|
| Ipilimumab and Androgen Depravation | 55 |
The number of months after the last ADT dose until the PSA progression (NCT01377389)
Timeframe: 2 to 45 months
| Intervention | months (Mean) |
|---|---|
| Ipilimumab and Androgen Depravation | 8.0 |
Overall survival of patients treated with intermittent ADT and ipilimumab in months. (NCT01377389)
Timeframe: From the date of randomization until the date of first documented progression or date of death from any case, whichever came first, assessed up to 70 months.
| Intervention | months (Mean) |
|---|---|
| Ipilimumab and Androgen Depravation | 36 |
The presence of testosterone was followed in each patient from the start of treatment until the testosterone lab test was found to be at a value greater than 50ng/mL. (NCT01377389)
Timeframe: 1 month up to 7 months.
| Intervention | months (Mean) |
|---|---|
| Ipilimumab and Androgen Depravation | 3.4 |
Anti-tumor activity assessed through serial PSA measurements (blood tests) at 7 months on treatment. Progression defined as two consecutive PSA values increasing by at least 20% or more from the lowest PSA value for each patient. (NCT01377389)
Timeframe: at the end of 7 months on treatment
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| PSA progression at 7 months | No PSA progression at 7 months | |
| Ipilimumab and Androgen Depravation | 6 | 18 |
The total number of adverse events which were related to one of the study drugs. Grade 1- Mild, asymptomatic of mild symptoms; clinical or diagnostic observation only; intervention not indicated. Grade 2- Moderate, minimal, local or noninvasive intervention indicated; limiting age-appropriate instrumental (daily living activities). Grate 3- Severe or medically significant but not immediately life-threatening; hospitalization or prolongation of hospitalization indicated; disabling; limiting self care of daily life activities. (NCT01377389)
Timeframe: From the first dose to the last follow-up, up to 60 months
| Intervention | related events (Number) | ||
|---|---|---|---|
| Grade 1 | Grade 2 | Grade 3 | |
| Ipilimumab and Androgen Depravation | 113 | 55 | 25 |
"For purposes of calculating summary statistics, any concentration values Below Limit Quantification (BLQ) were to be assigned ½ the Low Limit Quantification (LLOQ) (LLOQ=0.36). If the calculated mean, median or minimum value at a time point was less than LLOQ, BLQ is presented. In addition, since a high proportion of BLQ values may affect the Standard Deviation (SD); if more than 50% of values were imputed, then no mean or median was calculated for that time point." (NCT01415960)
Timeframe: 168 days
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Baseline | Day 168 | |
| Leuprolide Acetate 22.5 mg Depot | 44.36 | 2.37 |
"For purposes of calculating summary statistics, any concentration values Below Limit of Quantification (BLQ) were to be assigned ½ the Low Limit of Quantification (LLOQ) (LLOQ=3.66). If the calculated mean, median or minimum value at a time point was less than LLOQ, BLQ is presented. In addition, since a high proportion of BLQ values may affect the Standard Deviation (SD); if more than 50% of values were imputed, then no mean or median was to be calculated for that time point." (NCT01415960)
Timeframe: 168 days
| Intervention | mIU/mL (Mean) | ||
|---|---|---|---|
| Baseline | Day 28 | Day 168 | |
| Leuprolide Acetate 22.5 mg Depot | 15.14 | 1 | 5.80 |
"For purposes of calculating summary statistics, any concentration values Below Limit of Quantification (BLQ) were to be assigned ½ the Low Limit of Quantification (LLOQ) (LLOQ=2.00). If the calculated mean, median or minimum value at a time point was less than LLOQ, BLQ is presented. In addition, since a high proportion of BLQ values may affect the Standard Deviation (SD); if more than 50% of values were imputed, then no mean or median was calculated for that time point." (NCT01415960)
Timeframe: 168 days
| Intervention | mIU/mL (Mean) | ||
|---|---|---|---|
| Baseline | Day 28 | Day 168 | |
| Leuprolide Acetate 22.5 mg Depot | 7.24 | 1 | 1 |
"The WHO/ECOG, bone pain, urinary pain and urinary symptoms data reported are the most frequent percentage at the assessment time.~The WHO/ECOG performance status was summarized using the 0 to 4 WHO/ECOG performance status scale. (0= fully active, able to carry on all pre-disease performances without restriction).~Bone pain, urinary pain and urinary symptoms were determined using a 10-point scale (1= no pain/symptoms, 10= worst pain/symptom imaginable)." (NCT01415960)
Timeframe: 168 Days
| Intervention | percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline WHO/ECOG Score 0 (n=161) | Day 168 WHO/ECOG Scores 0 (n=152) | Baseline Bone Pain score 1 (n=161) | Day 168 Bone Pain score 1 (n=152) | Baseline Urinary Pain score 1 (n=161) | Day 168 Urinary Pain Score 1 (n=152) | Baseline Urinary Symptoms score 1 (n=161) | Day 168 Urinary Symptoms score 1 (n=152) | |
| Leuprolide Acetate 22.5 mg Depot | 83.9 | 82.9 | 95.0 | 94.1 | 98.8 | 97.4 | 87.6 | 89.5 |
The primary endpoint was testosterone ≤ 0.5 ng/mL assessed on Days 28, 84, and 168. Thereby, maintenance of castration was to be demonstrated through Day 168 with no missing data at these key time points, unless the missing data were due to an event unrelated to the study drug (ITT patients). (NCT01415960)
Timeframe: 168 days
| Intervention | percentage of participants (Number) |
|---|---|
| Leuprolide Acetate 22.5 mg Depot | 98.1 |
Leuprolide Pharmacokinetic Parameters (PK Population). (NCT01415960)
Timeframe: 84 days
| Intervention | day (Mean) | |
|---|---|---|
| Day 0/Dose 1 Tmax | Day 84/Dose 2 Tmax | |
| Leuprolide Acetate 22.5 mg Depot | 0.07 | 0.08 |
Leuprolide Pharmacokinetic Parameters (PK Population). (NCT01415960)
Timeframe: Cmax1: 0, 1 and 4 hours post-dose on Day 0 and once on Days 2, 14, 28, 56; Cmax2: 0, 1 and 4 hours post-dose on Day 84 and once on Days 86, 112 and 168.
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Day 0/Dose 1 Cmax | Day 84/Dose 2 Cmax | |
| Leuprolide Acetate 22.5 mg Depot | 46.79 | 48.30 |
Immune response at month 24 as evaluated by IFN-γ ELISPOT specific for PA2024 following sipuleucel-T/ADT treatment regimens to determine if order of administration impacted immune response. (NCT01431391)
Timeframe: PA2024 ELISPOT counts at Month 24
| Intervention | IFN-γ ELISPOT (per 300,000 PBMC) (Mean) |
|---|---|
| Arm 1: Sipuleucel-T Followed by ADT | 81.0 |
| Arm 2: ADT Followed by Sipuleucel-T | 61.1 |
A participant was considered to have an immune response it the post-baseline PA2024-specific IFN-g ELISPOT count was >18 (NCT01431391)
Timeframe: Month 24
| Intervention | percentage of participants (Number) |
|---|---|
| Arm 1:Sipuleucel-T Followed by ADT | 88 |
| Arm 2: ADT Followed by Sipuleucel-T | 85 |
Any donor having a serious complication such as severe hyperstimulation syndrome, ovarian torsion, infection or peritoneal bleeding will be recorded (NCT01443546)
Timeframe: 1 month
| Intervention | participants (Number) |
|---|---|
| hCG Trigger | 0 |
| Dual Trigger | 1 |
| Lupron Trigger | 0 |
To determine the feasibility of detecting circulating tumor cells in this patient population. CTC results per patient in milliliters. (NCT01531205)
Timeframe: One Year
| Intervention | CTC/mL (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline CTC/mL | 1 Month CTC/mL | 3 Month CTC/mL | Baseline CTC Clusters/mL | 1 Month CTC Clusters/mL | 3 Month CTC Clusters/mL | Baseline Apop/mL | 1 Month Apop/mL | 3 Month Apop/mL | Baseline Small Cells/mL | 1 Month Small Cells/mL | 3 Month Small Cells/mL | Baseline CK-CTC/mL | 1 Month CK-CTC/mL | 3 Month CK-CTC/mL | |
| Participant One | 2 | 1 | 27 | 1 | 0 | 28 | 1 | 1 | 1 | 0 | 0 | 0 | 3 | 0 | 18 |
| Participant Two | 1 | 6 | NA | 0 | 2 | NA | 1 | 4 | NA | 0 | 0 | NA | 0 | 1 | NA |
Number of events. To access the perioperative and postoperative morbidity with salvage surgery after neoadjuvant hormonal ablation and Cabazitaxel. (NCT01531205)
Timeframe: One Year
| Intervention | events (Number) |
|---|---|
| Experimental: Drug and Hormonal Therapy With Salvage Surgery | 0 |
Percentage of participants with stable (has not increased) or undetectable PSA post surgery. To assess Prostate-specific antigen(PSA)-progression free survival and prostate cancer specific survival for patients treated by chemohormonal therapy followed by salvage surgery for biopsy proven androgen-dependent high-risk locally recurrent prostate cancer following radiation therapy. (NCT01531205)
Timeframe: Four Months
| Intervention | percentage of participants (Number) |
|---|---|
| Experimental: Drug and Hormonal Therapy With Salvage Surgery | 0 |
Percentage of participants with CR post surgery. To evaluate the pathological complete response rate to androgen ablation plus Cabazitaxel in patients with locally recurrent prostate cancer following radiation therapy. Pathological Complete Response (pCR): Participants with no residual cancer in the local resection specimen and pelvic lymph nodes will be considered pCR. (NCT01531205)
Timeframe: One Year
| Intervention | percentage of participants (Number) |
|---|---|
| Experimental: Drug and Hormonal Therapy With Salvage Surgery | 0 |
Post surgery percentage of participants with negative surgical margin. To determine the surgical margin negative rate in patients who have undergone chemohormonal therapy followed by surgery for biopsy proven androgen-dependent high risk locally recurrent prostate cancer following primary radiation therapy. Margin: The edge or border of the tissue removed in cancer surgery. The margin is described as negative or clean when the pathologist finds no cancer cells at the edge of the tissue, suggesting that all of the cancer has been removed. The margin is described as positive or involved when the pathologist finds cancer cells at the edge of the tissue, suggesting that all of the cancer has not been removed. (NCT01531205)
Timeframe: One Year
| Intervention | percentage of participants (Number) |
|---|---|
| Experimental: Drug and Hormonal Therapy With Salvage Surgery | 100 |
(NCT01546454)
Timeframe: Entire Study
| Intervention | Total to HDL Cholesterol Ratio (Mean) |
|---|---|
| Non-steroidal Effects | 0.146 |
| Contraceptive Effects | 0.148 |
| Steroid Effects | -0.89 |
(NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | mIU/mL (Median) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Week 1 | Week 2 | Week 4 | Week 8 | Week 12 | Week 16 | Week 20 | Week 24 | Week 25 | Week 26 | Week 28 | Week 32 | Week 36 | Week 40 | Week 44 | Week 48 | |
| TAP-144-SR(3M) | 4.780 | 4.810 | 4.710 | 4.950 | 5.240 | 5.110 | 5.370 | 5.260 | 5.150 | 4.970 | 5.020 | 5.070 | 5.030 | 4.970 | 4.910 | 4.990 | 4.820 |
| TAP-144-SR(6M) | 5.120 | 5.430 | 4.890 | 4.625 | 5.225 | 5.340 | 5.300 | 5.030 | 4.990 | 5.210 | 5.010 | 5.060 | 5.210 | 5.585 | 5.100 | 5.150 | 5.110 |
(NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | mIU/mL (Median) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Week 1 | Week 2 | Week 4 | Week 8 | Week 12 | Week 16 | Week 20 | Week 24 | Week 25 | Week 26 | Week 28 | Week 32 | Week 36 | Week 40 | Week 44 | Week 48 | |
| TAP-144-SR(3M) | 0.000 | 0.220 | 0.150 | 0.110 | 0.000 | 0.110 | 0.055 | 0.110 | 0.000 | 0.185 | 0.130 | 0.000 | 0.000 | 0.000 | 0.000 | 0.000 | 0.000 |
| TAP-144-SR(6M) | 0.000 | 0.160 | 0.180 | 0.120 | 0.000 | 0.000 | 0.000 | 0.000 | 0.000 | 0.150 | 0.170 | 0.110 | 0.000 | 0.000 | 0.000 | 0.000 | 0.000 |
(NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | ng/dL (Median) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Week 1 | Week 2 | Week 4 | Week 8 | Week 12 | Week 16 | Week 20 | Week 24 | Week 25 | Week 26 | Week 28 | Week 32 | Week 36 | Week 40 | Week 44 | Week 48 | |
| TAP-144-SR(3M) | 7.0 | 7.0 | 6.0 | 8.0 | 8.0 | 8.0 | 7.5 | 6.0 | 6.0 | 5.5 | 4.0 | 6.0 | 8.0 | 7.0 | 8.0 | 8.0 | 6.0 |
| TAP-144-SR(6M) | 8.0 | 6.0 | 7.0 | 7.0 | 7.5 | 7.0 | 7.0 | 8.0 | 7.0 | 6.0 | 5.0 | 8.0 | 9.0 | 8.0 | 8.0 | 7.0 | 9.0 |
"Evaluation according to the Criteria for therapeutic effect from the General Rule for Clinical Pathological Studies on Prostate Cancer, 4th edition (determination of therapeutic effect by PSA)" (NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Presence of disesase progression: Yes | Presence of disesase progression: No | |
| TAP-144-SR(3M) | 92.5 | 93.5 |
| TAP-144-SR(6M) | 7.5 | 6.5 |
(NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | ng/dL (Mean) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline | Week 1 | Week 2 | Week 4 | Week 8 | Week 12 | Week 16 | Week 20 | Week 24 | Week 25 | Week 26 | Week 28 | Week 32 | Week 36 | Week 40 | Week 44 | Week 48 | |
| TAP-144-SR(3M) | 0.06188 | 0.1869 | 0.1335 | 0.1132 | 0.08374 | 0.08039 | 0.1220 | 0.08450 | 0.07437 | 0.1978 | 0.1418 | 0.1067 | 0.08236 | 0.08407 | 0.1086 | 0.08639 | 0.07945 |
| TAP-144-SR(6M) | 0.07113 | 0.1304 | 0.3085 | 0.8845 | 0.1792 | 0.1256 | 0.1024 | 0.06957 | 0.05167 | 0.1353 | 0.4318 | 0.7622 | 0.1524 | 0.1091 | 0.09118 | 0.06958 | 0.04596 |
"Assessment in accordance with the criteria for therapeutic effect from the General Rule for Clinical Pathological Studies on Prostate Cancer, 4th edition. Soft tissue response was evaluated in accordance with the Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1) for target lesions and assessed by CT or MRI: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR." (NCT01546623)
Timeframe: At week 48
| Intervention | Percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| Complete response | Partial Response | Stable Disease | Progressive Disease | Not Evaluable | |
| TAP-144-SR(3M) | 0.0 | 0.0 | 11.8 | 2.6 | 85.5 |
| TAP-144-SR(6M) | 0.0 | 0.0 | 13.9 | 0.0 | 86.1 |
(NCT01546623)
Timeframe: At 1 hour, week 24, and week 48 after administration
| Intervention | msec (Mean) | |||
|---|---|---|---|---|
| QTcF interval measurement at Basline | QTcF interval measurement at 1 hour | QTcF interval measurement at Week 24 | QTcF interval measurement at Week 48 | |
| TAP-144-SR(3M) | 436.2 | 432.2 | 433.4 | 431.7 |
| TAP-144-SR(6M) | 429.0 | 422.2 | 425.0 | 428.1 |
"Evaluation according to the Criteria for therapeutic effect from the General Rule for Clinical Pathological Studies on Prostate Cancer, 4th edition (determination of therapeutic effect by PSA)" (NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | percent change (Median) |
|---|---|
| TAP-144-SR(6M) | -86.225 |
| TAP-144-SR(3M) | -67.030 |
"Partially revised assessment based on the criteria for therapeutic effect from the General Rule for Clinical and Pathological Studies on Prostate Canter, 4th edition. Response is measured using bone scintigraphy. Increase in new (2 or more) bone lesion is considered as progression" (NCT01546623)
Timeframe: At Week 48
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Presence of disesase progression: New lesions ≥ 2 | Presence of disesase progression: New lesions < 1 | |
| TAP-144-SR(3M) | 1.3 | 98.7 |
| TAP-144-SR(6M) | 1.3 | 98.7 |
"Evaluation according to the Criteria for therapeutic effect from the General Rule for Clinical Pathological Studies on Prostate Cancer, 4th edition (determination of therapeutic effect by prostate-specific antigen [PSA])" (NCT01546623)
Timeframe: From baseline to Week 48
| Intervention | percent change (Median) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 4 | Week 8 | Week 12 | Week 16 | Week 20 | Week 24 | Week 28 | Week 32 | Week 36 | Week 40 | Week44 | Week 48 | |
| TAP-144-SR(3M) | -10.000 | -15.880 | -21.130 | -20.650 | -39.970 | -31.110 | -45.875 | -40.745 | -50.520 | -58.520 | -54.585 | -59.400 |
| TAP-144-SR(6M) | -7.930 | -14.255 | -20.810 | -19.720 | -44.740 | -49.270 | -56.705 | -57.690 | -60.710 | -80.610 | -74.105 | -72.900 |
Comparison of the proportion of patients maintained at castration level (≤100 ng/dL) (NCT01546623)
Timeframe: From the start of study drug administration through Week 48
| Intervention | Participants (Number) | |
|---|---|---|
| Number of participants maintained | Number of participants who did not maintain | |
| TAP-144-SR(3M) | 78 | 1 |
| TAP-144-SR(6M) | 81 | 0 |
This measure indicates serum LH concentration at baseline and post-baseline time points. It was measured in milli-international units per milliliter (mIU/mL). (NCT01546649)
Timeframe: Baseline, Hour 1, 3, 6 on Day 1, Day 2, 3, 4, 8, 15, 22, 29, 57, 85, 113, 141, 169, 176, 183, 197, 225, 253, 281, 309, 337, 421, 505, 589 and 673
| Intervention | mIU/mL (Median) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline [N=83;84] | Day1 (1hr) [N=82;84] | Day1 (3hr) [N=24;21] | Day1 (6hr) [N=24;21] | Day2 [N=83;84] | Day3 [N=83;84] | Day4 [N=83;84] | Week 1 (Day8) [N=83;84] | Week 2 (Day15) [N=83;84] | Week 3 (Day22) [N=83;84] | Week 4 (Day29) [N=83;84] | Week 8 (Day57) [N=83;84] | Week 12 (Day85) [N=83;83] | Week 16 (Day113) [N=82;82] | Week 20 (Day141) [N=81;82] | Week 24 (Day169) [N=80;81] | Week 25 (Day176) [N=79;80] | Week 26 (Day183) [N=79;80] | Week 28 (Day197) [N=75;77] | Week 32 (Day225) [N=78;80] | Week 36 (Day253) [N=79;80] | Week 40 (Day281) [N=78;80] | Week 44 (Day309) [N=77;80] | Week 48 (Day337) [N=77;80] | Week 60 (Day421) [N=77;79] | Week 72 (Day505) [N=77;78] | Week 84 (Day589) [N=76;77] | Week 96 (Day673) [N=75;75] | |
| TAP-144-SR (3M) | 4.490 | 30.585 | 63.260 | 61.210 | 19.755 | 10.500 | 9.375 | 4.475 | 1.990 | 1.085 | 0.845 | 0.570 | 0.520 | 0.430 | 0.405 | 0.460 | 0.455 | 0.405 | 0.410 | 0.440 | 0.395 | 0.390 | 0.385 | 0.415 | 0.440 | 0.420 | 0.410 | 0.360 |
| TAP-144-SR (6M) | 4.250 | 27.730 | 88.020 | 64.750 | 14.990 | 7.310 | 5.830 | 3.190 | 2.460 | 1.020 | 0.540 | 0.270 | 0.220 | 0.245 | 0.240 | 0.290 | 0.450 | 0.410 | 0.270 | 0.280 | 0.250 | 0.240 | 0.250 | 0.250 | 0.250 | 0.260 | 0.230 | 0.210 |
DFS is defined as time from randomization to earliest day of onset the events, recurrence [including recurrence in the ipsilateral breast], secondary cancer [including breast cancer in the contralateral breast] and death. DFS at Week 96 was defined as the percentage, calculated with Kaplan-Meier method, of participants did not experience any events at Week 96 since the randomization. (NCT01546649)
Timeframe: Week 96
| Intervention | percentage of participants (Number) |
|---|---|
| TAP-144-SR (6M) | 97.3 |
| TAP-144-SR (3M) | 97.5 |
DDFS is defined as time from randomization to earliest day of onset the events, distant recurrence, secondary cancer [including breast cancer in the contralateral breast] and death. DDFS at week 96 was defined as the percentage calculated with Kaplan-Meier method, of participants did not experience any events at week 96 since the randomization. (NCT01546649)
Timeframe: Week 96
| Intervention | percentage of participants (Number) |
|---|---|
| TAP-144-SR (6M) | 98.5 |
| TAP-144-SR (3M) | 98.8 |
This measure indicates serum FSH concentration at baseline and post-baseline time points. (NCT01546649)
Timeframe: Baseline, Hour 1, 3, 6 on Day 1, Day 2, 3, 4, 8, 15, 22, 29, 57, 85, 113, 141, 169, 176, 183, 197, 225, 253, 281, 309, 337, 421, 505, 589 and 673
| Intervention | mIU/mL (Median) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline [N=83;84] | Day1 (1hr) [N=82;84] | Day1 (3hr) [N=24;21] | Day1 (6hr) [N=24;21] | Day2 [N=83;84] | Day3 [N=83;84] | Day4 [N=83;84] | Week 1 (Day8) [N=83;84] | Week 2 (Day15) [N=83;84] | Week 3 (Day22) [N=83;84] | Week 4 (Day29) [N=83;84] | Week 8 (Day57) [N=83;84] | Week 12 (Day85) [N=83;83] | Week 16 (Day113) [N=82;82] | Week 20 (Day141) [N=81;82] | Week 24 (Day169) [N=80;81] | Week 25 (Day176) [N=79;80] | Week 26 (Day183) [N=79;80] | Week 28 (Day197) [N=75;77] | Week 32 (Day225) [N=78;80] | Week 36 (Day253) [N=79;80] | Week 40 (Day281) [N=78;80] | Week 44 (Day309) [N=77;80] | Week 48 (Day337) [N=77;80] | Week 60 (Day421) [N=77;79] | Week 72 (Day505) [N=77;78] | Week 84 (Day589) [N=76;77] | Week 96 (Day673) [N=75;75] | |
| TAP-144-SR (3M) | 5.605 | 10.000 | 19.950 | 25.340 | 12.515 | 6.780 | 5.585 | 3.035 | 1.705 | 1.570 | 2.015 | 2.345 | 2.240 | 1.830 | 1.905 | 2.000 | 1.600 | 1.700 | 1.690 | 1.980 | 2.035 | 1.710 | 1.825 | 1.885 | 1.910 | 1.920 | 1.840 | 1.740 |
| TAP-144-SR (6M) | 5.070 | 9.520 | 23.325 | 27.460 | 10.080 | 6.180 | 6.100 | 3.920 | 1.820 | 1.220 | 1.200 | 1.390 | 1.490 | 1.635 | 1.780 | 2.060 | 1.940 | 1.560 | 1.310 | 1.595 | 1.660 | 1.735 | 1.930 | 1.920 | 1.530 | 1.730 | 1.500 | 1.620 |
The measure indicates serum E2 concentration at baseline and post-baseline time points. (NCT01546649)
Timeframe: Baseline, Hour (hr) 1, 3, 6 on Day 1, Day 2, 3, 4, 8, 15, 22, 29, 57, 85, 113, 141, 169, 176, 183, 197, 225, 253, 281, 309, 337, 421, 505, 589 and 673
| Intervention | pg/mL (Median) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline [N=83;84] | Day1 (1hr) [N=82;84] | Day1 (3hr) [N=24;21] | Day1 (6hr) [N=24;21] | Day2 [N=83;84] | Day3 [N=83;84] | Day4 [N=83;84] | Week 1 (Day8) [N=83;84] | Week 2 (Day15) [N=83;84] | Week 3 (Day22) [N=83;84] | Week 4 (Day29) [N=83;84] | Week 8 (Day57) [N=83;84] | Week 12 (Day85) [N=83;83] | Week 16 (Day113) [N=82;82] | Week 20 (Day141) [N=81;82] | Week 24 (Day169) [N=80;81] | Week 25 (Day176) [N=79;80] | Week 26 (Day183) [N=79;80] | Week 28 (Day197) [N=75;77] | Week 32 (Day225) [N=78;80] | Week 36 (Day253) [N=79;80] | Week 40 (Day281) [N=78;80] | Week 44 (Day309) [N=77;80] | Week 48 (Day337) [N=77;80] | Week 60 (Day421) [N=77;79] | Week 72 (Day505) [N=77;78] | Week 84 (Day589) [N=76;77] | Week 96 (Day673) [N=75;75] | |
| TAP-144-SR (3M) | 99 | 110.5 | 64.0 | 99.0 | 115.5 | 87.5 | 110.0 | 112.0 | 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 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 |
| TAP-144-SR (6M) | 95 | 94.5 | 102.0 | 153.5 | 146.0 | 100.0 | 108.0 | 56.0 | 13.0 | 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 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 |
12-lead electrocardiography measurement was performed in supine position after 5 minutes at rest. Each measurement was recorded continuously for 10 seconds at the recording speed of 25 millimeter/second (mm/second). (NCT01546649)
Timeframe: Baseline, Hour 1, 3, 6 on Day 1, Day 29, 85, 169 and 337
| Intervention | millisecond (msec) (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline [N=83;84] | Day1 (1hr) [N=83;84] | Day1 (3hr) [N=24;21] | Day1 (6hr) [N=24;21] | Week 4 (Day29) [N=83;84] | Week 12 (Day85) [N=83;84] | Week 24 (Day169) [N=81;82] | Week 48 (Day337) [N=77;80] | |
| TAP-144-SR (3M) | 420.9 | 417.1 | 423.7 | 424.1 | 432.3 | 432.3 | 429.0 | 431.4 |
| TAP-144-SR (6M) | 421.5 | 417.8 | 416.8 | 415.8 | 431.2 | 433.3 | 431.0 | 430.0 |
This measure indicates the unchanged TAP-144 level in serum. (NCT01546649)
Timeframe: Baseline, Hour 1, 3, 6 on Day 1, Day 2, 3, 4, 8, 15, 22, 29, 57, 85, 113, 141, 169, 176, 183, 197, 225, 253, 281, 309 and 337
| Intervention | nanogram per deciliter (ng/dL) (Mean) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline [N=83;84] | Day1 (1hr) [N=82;84] | Day1 (3hr) [N=24;19] | Day1 (6hr) [N=24;21] | Day2 [N=83;84] | Day3 [N=83;84] | Day4 [N=83;84] | Week 1 (Day8) [N=82;83] | Week 2 (Day15) [N=82;84] | Week 3 (Day22) [N=83;84] | Week 4 (Day29) [N=83;83] | Week 8 (Day57) [N=83;83] | Week 12 (Day85) [N=83;83] | Week 16 (Day113) [N=82;82] | Week 20 (Day141) [N=81;82] | Week 24 (Day169) [N=80;81] | Week 25 (Day176) [N=79;80] | Week 26 (Day183) [N=79;80] | Week 28 (Day197) [N=80;80] | Week 32 (Day225) [N=78;80] | Week 36 (Day253) [N=79;80] | Week 40 (Day281) [N=79;80] | Week 44 (Day309) [N=77;80] | Week 48 (Day337) [N=77;80] | |
| TAP-144-SR (3M) | 0.000 | 28.45 | 20.27 | 8.037 | 0.4749 | 0.2492 | 0.2273 | 0.1050 | 0.08867 | 0.06471 | 0.04971 | 0.04744 | 0.06028 | 0.09347 | 0.07165 | 0.07634 | 0.1583 | 0.1109 | 0.08468 | 0.06881 | 0.06259 | 0.08163 | 0.06479 | 0.06313 |
| TAP-144-SR (6M) | 0.000 | 5.293 | 2.538 | 1.039 | 0.1401 | 0.02889 | 0.02380 | 0.09115 | 0.3702 | 0.7285 | 0.3442 | 0.1146 | 0.08051 | 0.05775 | 0.03941 | 0.02931 | 0.1128 | 0.3327 | 0.4687 | 0.1377 | 0.08521 | 0.06073 | 0.4339 | 0.02957 |
Comparison of both the treatment groups was done by assessing the suppressive effect on serum E2 concentration maintained at menopausal level (=<30pg/mL). Suppression rate was calculated as proportion of participants maintained at menopausal level. (NCT01546649)
Timeframe: Week 4 up to Week 48
| Intervention | percentage of participants (Number) |
|---|---|
| TAP-144-SR (6M) | 97.6 |
| TAP-144-SR (3M) | 96.4 |
Note, the revised protocol (see Limitations and Caveats) changed this outcome measure from secondary (original protocol) to primary. Biochemical failure will be defined by the Phoenix definition (PSA ≥ 2 ng/ml over the nadir PSA, the presence of local, regional, or distant recurrence, or the initiation of salvage androgen deprivation therapy. Time to failure is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method, while treatment effect comparisons are based on cause-specific hazards (deaths censored). Five-year rates are provided here. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 17.3 |
| TAK-700 + ADT + RT | 12.8 |
Time to prostate cancer death is defined as time from randomization to the date of death due to prostate cancer, last known follow-up (censored), or death due to other causes (competing risk). Failure rates were to be estimated using the cumulative incidence method. If too few events occur for meaningful estimates, then only counts of events will be reported. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | Participants (Count of Participants) |
|---|---|
| ADT + RT | 1 |
| TAK-700 + ADT + RT | 0 |
Distant metastases (failure) is defined as imaging or biopsy demonstrated evidence for systemic recurrence. Biopsy was not required, however it was encouraged in absence of a rising PSA. Time to failure is defined as time from randomization to the date of first failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method, while treatment effect comparisons are based on cause-specific hazards (deaths censored). Five-year rates are provided here. Note, the protocol lists this endpoint as regional or distant metastasis, but regional progression data was not collected. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 6.8 |
| TAK-700 + ADT + RT | 2.9 |
General clinical treatment failure (GCTF) is defined as: PSA > 25 ng/ml, documented local disease progression, regional or distant metastasis, or initiation of salvage androgen deprivation therapy. Failure time is defined as time from registration to the date of failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method, while treatment effect comparisons are based on cause-specific hazards (deaths censored). Five-year rates are provided here. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 12.5 |
| TAK-700 + ADT + RT | 6.8 |
Time to grade 3 or higher adverse event (event) is defined as time from randomization to the date of first event, last known follow-up (censored), or death without failure (competing risk). Event rates are estimated using the cumulative incidence method, while treatment effect comparisons are based on cause-specific hazards (deaths censored). Five-year rates are provided here. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 34.9 |
| TAK-700 + ADT + RT | 58.9 |
Local recurrence (failure) is defined as biopsy proven recurrence within the prostate gland. Time to failure is defined as time from randomization to the date of failure, last known follow-up (censored), or death without failure (competing risk). Failure rates are estimated using the cumulative incidence method, while treatment effect comparisons are based on cause-specific hazards (deaths censored). Five-year rates are provided here. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates reported.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 2.9 |
| TAK-700 + ADT + RT | 0.0 |
Note, the revised protocol (see Limitations and Caveats) changed this outcome measure from primary (original protocol) to secondary. Overall survival time is defined as time from randomization to the date of death from any cause or last known follow-up (censored). Overall survival rates are estimated by the Kaplan-Meier method. The protocol specifies that the distributions of failure times be compared between the arms, which is reported in the statistical analysis results. 5-year rates are provided. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | percentage of participants (Number) |
|---|---|
| ADT + RT | 89.4 |
| TAK-700 + ADT + RT | 88.1 |
Body Mass Index (BMI) is a person's weight in kilograms (or pounds) divided by the square of height in meters (or feet). Change from baseline = time point value - baseline value. (NCT01546987)
Timeframe: Baseline and yearly to five years.
| Intervention | kg/m^2 (Mean) | ||||
|---|---|---|---|---|---|
| 1 year | 2 years | 3 years | 4 years | 5 years | |
| ADT + RT | 0.64 | 0.67 | 0.75 | -0.02 | -0.52 |
| TAK-700 + ADT + RT | -0.84 | -0.34 | 0.25 | 0.46 | 0.15 |
The EPIC-Short Form is a 26-item, validated self-administered tool to assess disease-specific aspects of prostate cancer and its therapies consisting of five summary domains (bowel, urinary incontinence, urinary irritation/obstruction, sexual, and hormonal function). Responses for each item form a Likert scale which are transformed to a 0-100 scale. A domain score is the average of the transformed domain item scores, ranging from 0-100 with higher scores representing better health-related quality of life (HRQOL). Change at one year is defined as one-year value - baseline value. Positive change at one year indicates improved quality of life. (NCT01546987)
Timeframe: Baseline, one year
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| Bowel domain | Urinary domain | Sexual domain | Hormonal domain | |
| ADT + RT | -5.45 | -1.67 | -24.18 | -17.31 |
| TAK-700 + ADT + RT | -7.04 | -5.31 | -27.26 | -17.45 |
(NCT01546987)
Timeframe: Baseline, 12 months, 24 months
| Intervention | mg/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 98.99 | 102.27 | 104.24 |
| TAK-700 + ADT + RT | 100.52 | 117.39 | 105.51 |
(NCT01546987)
Timeframe: Baseline, 12 months, 24 months
| Intervention | mg/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 149.71 | 160.27 | 163.20 |
| TAK-700 + ADT + RT | 154.20 | 154.74 | 160.61 |
(NCT01546987)
Timeframe: Baseline, 12 months, 24 months
| Intervention | g/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 6.12 | 6.33 | 6.30 |
| TAK-700 + ADT + RT | 6.01 | 5.95 | 6.04 |
Common Terminology Criteria for Adverse Events (version 4.0) grades adverse event severity from 1=mild to 5=death. Summary data is provided in this outcome measure; see Adverse Events Module for specific adverse event data (NCT01546987)
Timeframe: From registration to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | Participants (Count of Participants) | ||||
|---|---|---|---|---|---|
| Grade 1 | Grade 2 | Grade 3 | Garde 4 | Grade 5 | |
| ADT + RT | 17 | 54 | 31 | 4 | 3 |
| TAK-700 + ADT + RT | 2 | 45 | 55 | 9 | 1 |
"Clinical survivorship events are defined as the following newly diagnosed non-fatal cardiovascular events or other clinical endpoints relevant to prostate cancer survivorship:~type 2 diabetes, coronary artery disease, myocardial infarction, stroke, pulmonary embolism, deep vein thrombosis, and osteoporotic fracture." (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | Participants (Count of Participants) | ||||||
|---|---|---|---|---|---|---|---|
| Type 2 diabetes | Coronary artery disease | Myocardial infarction | Stroke | Pulmonary embolism | Deep vein thrombosis | Osteoporotic fracture | |
| ADT + RT | 30 | 16 | 6 | 5 | 10 | 8 | 6 |
| TAK-700 + ADT + RT | 18 | 14 | 8 | 6 | 5 | 7 | 1 |
(NCT01546987)
Timeframe: Baseline, 12 months, 24 months
| Intervention | mg/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 40.91 | 44.94 | 42.16 |
| TAK-700 + ADT + RT | 41.32 | 44.50 | 44.85 |
(NCT01546987)
Timeframe: Baseline, 12 months, 24 months
| Intervention | mg/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 88.78 | 86.18 | 81.35 |
| TAK-700 + ADT + RT | 87.85 | 83.73 | 95.34 |
(NCT01546987)
Timeframe: Baseline,12 months, 24 months
| Intervention | ng/dL (Mean) | ||
|---|---|---|---|
| Baseline | 12 months | 24 months | |
| ADT + RT | 355.75 | 35.68 | 86.47 |
| TAK-700 + ADT + RT | 357.73 | 25.22 | 17.36 |
Testosterone recovery is defined as testosterone level after treatment greater than 230 ng/dL. Time to testosterone recovery is defined as time from randomization to the date of testosterone recovery, biochemical, local, or distant failure (competing risk), salvage therapy (competing risk), death (competing risk), or last known follow-up (censored). Testosterone recovery rates are estimated using the cumulative incidence method. (NCT01546987)
Timeframe: From registration to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years.
| Intervention | percentage of participants (Number) | |
|---|---|---|
| 12 months | 24 months | |
| ADT + RT | 19.4 | 32.9 |
| TAK-700 + ADT + RT | 12.5 | 17.4 |
Testosterone recovery is defined as testosterone level after treatment greater than 230 ng/dL. Testosterone recovery rates are estimated using the Kaplan-Meier method, censoring for biochemical, local, or distant failure, salvage therapy, death, and otherwise alive without event. Testosterone recovery time is defined as time from randomization to testosterone recovery or censoring. (NCT01546987)
Timeframe: From randomization to last follow-up. Follow-up schedule: every 3 months from start of treatment for 2 years, then every 6 months for 3 years, then yearly. Maximum follow-up at time of analysis was 9.1 years. Five-year rates are reported here.
| Intervention | years (Median) |
|---|---|
| ADT + RT | NA |
| TAK-700 + ADT + RT | NA |
The PROMIS Fatigue short form 8a contains 8 questions, each with 5 responses ranging from 1 to 5, evaluating self-reported fatigue symptoms over the past 7 days. The total score is the sum of all questions which is then converted into a pro-rated T-score with a mean of 50 and standard deviation of 10, with a possible range of 33.1 to 77.8. Higher scores indicate more fatigue. Change is defined as value at one year - value at baseline. Positive change from baseline indicates increased fatigue at one year. (NCT01546987)
Timeframe: Baseline, one year
| Intervention | T-score (Mean) |
|---|---|
| ADT + RT | 2.78 |
| TAK-700 + ADT + RT | 3.16 |
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 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 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 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 |
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 |
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 |
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 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 |
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 |
(NCT01547299)
Timeframe: Day 180
| Intervention | ng/mL (Median) |
|---|---|
| Enzalutamide + Leuprolide + Dutasteride | 0.01 |
| Enzalutamide | 0.51 |
(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 |
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 |
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 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 |
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 |
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 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 |
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 |
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 |
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 |
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 |
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 |
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 |
Kaplan-Meier OS will be measured from the date that study therapy was commenced until the date of death. (NCT01642186)
Timeframe: From date of randomization until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 100 months
| Intervention | months (Median) |
|---|---|
| Arm A Everolimus | 12.5 |
| Arm B Letrozole Plus Leuprolide | 14.0 |
| Arm C Combination Everolimus, Letrozole and Leuprolide | 10.6 |
Kaplan-Meier PFS will be measured from the date that study therapy is initiated until the date of first evidence of radiographic disease progression, global clinical deterioration as determined by study investigators, or death. (NCT01642186)
Timeframe: 2 years
| Intervention | months (Median) |
|---|---|
| Arm A Everolimus | 2.6 |
| Arm B Letrozole Plus Leuprolide | 2.7 |
| Arm C Combination Everolimus, Letrozole and Leuprolide | 2.4 |
Adverse events/toxicity will be monitored and recorded using the CTCAE version 4.0 and summarized descriptively. (NCT01642186)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A Everolimus | 9 |
| Arm B Letrozole Plus Leuprolide | 9 |
| Arm C Combination Everolimus, Letrozole and Leuprolide | 10 |
Objective responses will be reported using RECIST guidelines (version 1.1). Objective response will be estimated using binomial proportions and exact 95% CIs will be provided. Stable Disease is defined as neither sufficient shrinkage (compared to baseline) to qualify for Partial Reponse nor sufficient increase (taking as reference the smallest sum diameters while on study) to qualify for Progressive Disease. (NCT01642186)
Timeframe: 2 years
| Intervention | Percentage of pts with stable disease (Number) |
|---|---|
| Arm A Everolimus | 55 |
| Arm B Letrozole Plus Leuprolide | 37 |
| Arm C Combination Everolimus, Letrozole and Leuprolide | 11 |
Associations between baseline tissue biomarkers and PFS6 will be assessed using Fisher's exact test for categorical biomarkers, trend tests for ordinal biomarkers and Wilcoxon rank-sum test for continuous biomarkers. For patients undergoing surgery, changes in tissue biomarkers from baseline to surgery will be summarized descriptively in an exploratory fashion. (NCT01642186)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A Everolimus | 9 |
| Arm B Letrozole Plus Leuprolide | 9 |
| Arm C Combination Everolimus, Letrozole and Leuprolide | 10 |
Time from date of registration to date of first invasive recurrence (local, regional or distant), second invasive primary cancer (breast or not), or death due to any cause. Patients last known to be alive who have not experienced recurrence or second primary cancer are censored at their last contact date. The results were presented as 5-year IDFS estimate. (NCT01674140)
Timeframe: Up to 5 years post registration
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 74.4 |
| Everolimus | 74.9 |
Time from date of registration to date of invasive distant disease recurrence, second invasive primary cancer (breast or not) or death due to any cause. Patients last known to be alive who have not experienced distant recurrence, or second primary cancer are censored at their last contact date. The results were presented as 5-year DRFS estimate. (NCT01674140)
Timeframe: 5 years after last accrual
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 75.7 |
| Everolimus | 76.9 |
Toxicity based on Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. Only adverse events that are possibly, probably, or definitely related to study drug are reported. (NCT01674140)
Timeframe: Every 6 weeks while on protocol therapy. Adverse events (AEs) that occurred during follow up after protocol treatment were reported as late AEs, for every 6 months for the first 2 years and then yearly until 10 years after registration.
| Intervention | Participants (Number) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Abdominal pain | Alanine aminotransferase increased | Allergic reaction | Anemia | Anxiety | Appendicitis | Appendicitis perforated | Arthralgia | Ascites | Aspartate aminotransferase increased | Back pain | Bone pain | Breast infection | Cardiac arrest | Cholecystitis | Cholesterol high | Colitis | Cough | Dehydration | Depression | Diarrhea | Dizziness | Dyspnea | Edema face | Edema limbs | Eye disorders - Other, specify | Eye infection | Fatigue | Fever | Gallbladder infection | Gallbladder perforation | Gastrointestinal disorders - Other, specify | General disorders and admin site conditions - Other | Generalized muscle weakness | Headache | Heart failure | Hip fracture | Hot flashes | Hyperglycemia | Hyperhidrosis | Hyperkalemia | Hypertension | Hypertriglyceridemia | Hypokalemia | Hyponatremia | Hypophosphatemia | Hypoxia | Immune system disorders - Other, specify | Infections and infestations - Other, specify | Infusion related reaction | Insomnia | Investigations - Other, specify | Irregular menstruation | Joint infection | Kidney infection | Left ventricular systolic dysfunction | Lipase increased | Lung infection | Lymphedema | Lymphocyte count decreased | Menorrhagia | Mucositis oral | Muscle weakness lower limb | Muscle weakness upper limb | Musculoskeletal and connective tiss disorder - Other | Myalgia | Nasal congestion | Nausea | Neck pain | Nervous system disorders - Other, specify | Neuralgia | Neutrophil count decreased | Obesity | Otitis media | Pain | Pain in extremity | Papulopustular rash | Paroxysmal atrial tachycardia | Periorbital edema | Peripheral sensory neuropathy | Platelet count decreased | Pleural effusion | Pneumonitis | Portal vein thrombosis | Postoperative hemorrhage | Productive cough | Pruritus | Psychiatric disorders - Other, specify | Pulmonary edema | Radiation recall reaction (dermatologic) | Rash acneiform | Rash maculo-papular | Rash pustular | Respiratory failure | Sepsis | Seroma | Skin and subcutaneous tissue disorders - Other | Skin infection | Skin ulceration | Soft tissue infection | Sore throat | Suicidal ideation | Suicide attempt | Thromboembolic event | Tooth infection | Upper respiratory infection | Urinary tract infection | Vascular access complication | Vomiting | Weight gain | Weight loss | White blood cell decreased | Wound complication | Wound dehiscence | Wound infection | |
| Everolimus | 7 | 4 | 2 | 10 | 0 | 1 | 2 | 5 | 1 | 6 | 0 | 1 | 6 | 0 | 1 | 9 | 1 | 2 | 3 | 2 | 13 | 2 | 7 | 1 | 1 | 1 | 1 | 23 | 1 | 1 | 1 | 2 | 1 | 1 | 4 | 4 | 1 | 0 | 33 | 2 | 1 | 15 | 35 | 5 | 2 | 1 | 2 | 1 | 5 | 1 | 3 | 1 | 1 | 1 | 2 | 2 | 0 | 6 | 1 | 36 | 0 | 60 | 1 | 0 | 1 | 2 | 1 | 2 | 1 | 0 | 1 | 22 | 0 | 1 | 0 | 0 | 1 | 0 | 2 | 2 | 4 | 2 | 7 | 1 | 1 | 1 | 2 | 0 | 1 | 2 | 1 | 4 | 2 | 0 | 7 | 1 | 3 | 8 | 2 | 2 | 1 | 1 | 1 | 5 | 1 | 1 | 2 | 1 | 1 | 0 | 2 | 20 | 5 | 4 | 6 |
| Placebo | 1 | 1 | 0 | 0 | 1 | 2 | 0 | 1 | 0 | 1 | 1 | 0 | 1 | 1 | 0 | 0 | 1 | 0 | 0 | 0 | 3 | 0 | 2 | 0 | 0 | 0 | 0 | 6 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 2 | 1 | 0 | 0 | 6 | 4 | 0 | 0 | 0 | 0 | 0 | 4 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 1 | 2 | 0 | 5 | 1 | 2 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 3 | 1 | 0 | 1 | 1 | 0 | 1 | 0 | 1 | 1 | 0 | 1 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 3 | 0 | 0 | 0 | 0 | 0 | 3 | 0 | 0 | 1 | 0 | 1 | 2 | 0 | 2 | 0 | 1 | 0 |
Time from date of registration to date of death due to any cause. Patients last known to be alive are censored at their last contact date. The results were presented as 5-year OS estimate. (NCT01674140)
Timeframe: 5 years after last accrual
| Intervention | percentage of participants (Number) |
|---|---|
| Placebo | 85.8 |
| Everolimus | 88.1 |
Total Fat mass as measured by DXA (NCT01712230)
Timeframe: Change over 6 months
| Intervention | kg (Mean) |
|---|---|
| Placebo | 0.73 |
| GnRH Agonist | 1.66 |
| GnRH Agonist + Exercise | 0.89 |
Total Fat Free Mass as measured by DXA (NCT01712230)
Timeframe: Change over 6 months
| Intervention | kg (Mean) |
|---|---|
| Placebo | 0.1 |
| GnRH Agonist | -0.69 |
| GnRH Agonist + Exercise | -0.66 |
PAEE will be calculated as: TEE - REE - TEF, where TEE is total energy expenditure (measured by doubly-labeled water), REE is resting energy expenditure (measured by indirect calorimetry), and TEF is the thermic effect of feeding (estimated using a constant). (NCT01712230)
Timeframe: Change from baseline to 6 months
| Intervention | kcal/day (Mean) |
|---|---|
| Placebo | 74.5 |
| GnRH Agonist | -10.2 |
| GnRH Agonist + Exercise | 61.0 |
Change in c-telopeptides following Round 1 of BAT (9 months) compared to the timepoint immediately following the ADT Lead-In (6 months) (NCT01750398)
Timeframe: 6 months and 9 months
| Intervention | pg/ml (Mean) |
|---|---|
| ADT Plus IM Testosterone | -159.77 |
To determine the clinical effects of BAT in men with recurrent prostate cancer as first line therapy. This will be accomplished by assessing the number of patients achieving a PSA <4 ng/ml at the end of the trial. (NCT01750398)
Timeframe: 18 months
| Intervention | participants (Number) |
|---|---|
| ADT Plus IM Testosterone | 17 |
(NCT01750398)
Timeframe: Bseline, 6 months and 9 months.
| Intervention | cm (Mean) | |
|---|---|---|
| Following ADT lead in | Following round 1 of BAT | |
| ADT Plus IM Testosterone | 3.9 | -1.09 |
Change in weight is measured from baseline to 6 months (i.e. following ADT lead in) and from 6 months to 9 months (i.e. from post-ADT to the end of cycle 1 of BAT). (NCT01750398)
Timeframe: Baseline, 6 months and 9 months.
| Intervention | kg (Mean) | |
|---|---|---|
| Following ADT lead in | Following round 1 of BAT | |
| ADT Plus IM Testosterone | 2.08 | 1.21 |
To evaluate the number of patients who achieve a complete PSA response (i.e. serum PSA <0.2 ng/ml) at the end of the study (NCT01750398)
Timeframe: 18 months
| Intervention | participants (Number) | |
|---|---|---|
| Patients with PSA <0.2 ng/ml | Patients with PSA ≥0.2 ng/ml | |
| ADT Plus IM Testosterone | 3 | 26 |
To evaluate the number of men treated per the bipolar androgen therapy phase of the trial who developed radiographic or clinical progression. Radiographic progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. Clinical progression was defined as new symptoms that can be attributed to progressive prostate cancer (e.g. new/worsening pain, urinary obstruction, cord compression, bone fractures). (NCT01750398)
Timeframe: 18 months
| Intervention | participants (Number) | |
|---|---|---|
| Patients with radiographic/clinical progression | Patients without radiographic/clinical progression | |
| ADT Plus IM Testosterone | 6 | 23 |
"To measure quality of life through the RAND-SF36 (short-form 36 questionnaire) Quality of Life Survey, the Functional Assessment of Cancer Therapy - Prostate Cancer (FACT-P), the International Index of Erectile Function (IIEF), the International Prostate Symptom Score (IPSS) and a visual pain scale. Note that for all scales, higher scores indicate better quality of life/function, with the exception being the visual pain scale, where a higher score indicates more pain.~RAND-SF36: SF-36 is a set of generic, coherent, and easily administered quality-of-life measures. Range is from 0 to 100.~FACT-P: A tool used for assessing the health-related quality of life in men with prostate cancer. Range is from 0 to 156.~IIEF: Is a measure of erectile function. Range is from 5 to 25. IPSS: A tool used to measure symptoms related to prostatic disease. Range is from 0 to 35.~Visual pain scale: A tool used to track pain level. Range is from 0 to 10." (NCT01750398)
Timeframe: 3 months
| Intervention | units on a scale (Median) | |||
|---|---|---|---|---|
| Change in SF-36 after round 1 of BAT | Change in FACT-P after round 1 of BAT | Change in IIEF after round 1 of BAT | Change in IPSS after round 1 of BAT | |
| ADT Plus IM Testosterone | 3.2 | 3.5 | 10 | 0 |
"The IDAS Dysphoria Scale consists of 10 items and uses a 5-point Likert-type scale, ranging from 1 to 5 with 1 indicating not at all and 5 indicating extremely. As such, the range of possible scores is 10 to 50. The Dysphoria scale includes items assessing feelings of depression, inadequacy, psychomotor agitation, guilt, discouragement, anhedonia, poor concentration, difficulty with decision-making, psychomotor retardation, and worry. Higher scores indicate greater dysphoria." (NCT01762943)
Timeframe: Assessed at baseline and post-treatment
| Intervention | units on a scale (Mean) | |
|---|---|---|
| IDAS Dysphoria Baseline | IDAS Dysphoria Withdrawal | |
| Women With a History of Postpartum Depression (PPD) | 11.4 | 15.7 |
| Women Without Any Psychiatric History (Control) | 12.7 | 11.1 |
The primary outcome measure was functional magnetic resonance imaging (fMRI) data collected during a Monetary Incentive Delay (MID) Task. The BOLD response was examined within the nucleus accumbens, a brain region that responds to monetary rewards. The z statistic represents the maximum contrast between win versus non-win outcomes during the MID task in the nucleus accumbens, averaged across the participants in each group. The mean BOLD response ranged from z=1.7 to 2.3; higher z scores indicate greater activation of the nucleus accumbens during reward. Individual z scores were generated using the Oxford Centre for Functional Magnetic Resonance Imaging of the Brain (FMRIB) software library (FSL), which is a library of brain imaging analysis tools for fMRI. (NCT01762943)
Timeframe: baseline and hormone withdrawal
| Intervention | z score (Mean) | |||
|---|---|---|---|---|
| Left Nucleus Acc Baseline | Left Nucleus Acc Withdrawal | Right Nucleus Acc Baseline | Right Nucleus Acc Withdrawal | |
| Women With a History of Postpartum Depression (PPD) | 2.3 | 2.1 | 2.2 | 2.3 |
| Women Without Any Psychiatric History (Control) | 2.0 | 1.7 | 2.0 | 2.0 |
Number of oocytes retrieved (NCT01921166)
Timeframe: up to 24 months
| Intervention | oocytes (Number) |
|---|---|
| Clomiphene Plus Gonadotropins | 19 |
| Leuprolide Flare | 47 |
(NCT01921166)
Timeframe: up to 24 months
| Intervention | oocytes (Number) |
|---|---|
| Clomiphene Plus Gonadotropins | 19 |
| Leuprolide Flare | 47 |
Percentage of patients with recovering testosterone to > 100 at 1, 2, and 3 years. (NCT02057939)
Timeframe: 3 years
| Intervention | percentage (Number) | ||
|---|---|---|---|
| 1 year | 2 year | 3 year | |
| Enzalutamide | 94.6 | 100 | 100 |
Percentage of patients surviving 2 and 3 years from the start of study treatment without progression of disease. Biochemical PFS was defined as the time from the date of study treatment initiation to the date of first documented progression or death due to any cause. Progression-free was defined as being without one of the following: serum PSA value of 0.2 ng/mL or more above post-radiotherapy PSA nadir that continues to increase 4 weeks later OR if no nadir is experienced, two rising PSA values over 4 or more weeks (NCT02057939)
Timeframe: 3 years
| Intervention | percentage (Number) | |
|---|---|---|
| 2 year bPFS | 3 year bPFS | |
| Enzalutamide | 64.9 | 53.2 |
Safety and tolerability will be assessed using CTCAE v4.0 (NCT02057939)
Timeframe: 3 years
| Intervention | participants (Number) |
|---|---|
| Enzalutamide | 36 |
Median PSA nadir post-radiation therapy (NCT02057939)
Timeframe: 8 weeks
| Intervention | ng/ml (Median) |
|---|---|
| Enzalutamide | 0 |
Percentage of patients surviving 3 years from the start of study treatment without progression of disease. PFS was defined as the time from the date of study treatment initiation to the date of first documented progression or death due to any cause. Progression-free was defined as being without one of the following: serum PSA value of 0.2 ng/mL or more above post-radiotherapy PSA nadir that continues to increase 4 weeks later OR if no nadir is experienced, two rising PSA values over 4 or more weeks OR evidence of clinical progression or initiation of systemic therapy for progressive disease (NCT02057939)
Timeframe: 3 years
| Intervention | percentage (Number) |
|---|---|
| Enzalutamide | 53.2 |
Percentage of patients surviving 2 years from the start of study treatment without progression of disease. PFS was defined as the time from the date of study treatment initiation to the date of first documented progression or death due to any cause. Progression-free was defined as being without one of the following: serum PSA value of 0.2 ng/mL or more above post-radiotherapy PSA nadir that continues to increase 4 weeks later OR if no nadir is experienced, two rising PSA values over 4 or more weeks OR evidence of clinical progression or initiation of systemic therapy for progressive disease (NCT02057939)
Timeframe: 2 years
| Intervention | percentage (Number) |
|---|---|
| Enzalutamide | 64.9 |
The percentage of men with PSA less than 0.1 ng/mL and testosterone greater than 100 (NCT02057939)
Timeframe: every year, up to 3 years
| Intervention | percentage (Number) | ||
|---|---|---|---|
| 1 year | 2 year | 3 year | |
| Enzalutamide | 75.7 | 48.6 | 32.4 |
Will be summarized with point estimates (occurrence rates). A CTC response is defined as any level of CTC < 5 that is maintained or any level of CTC that is reduced from baseline. (NCT02058706)
Timeframe: Up to month 1
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 17 |
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 22 |
Point estimates will be calculated and CI estimates will be derived from the Wilcoxon method using STATA software. (NCT02058706)
Timeframe: 6 months
| Intervention | percentage of response at 6 months (Number) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 86 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 79 |
Percentage of patients with bone metastases Progression free at six months using the Kaplan-Meier method. (NCT02058706)
Timeframe: assessed at six months
| Intervention | percentage not progressed at 6 months (Number) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 91 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 33 |
Overall Survival will be measured from date of registration to death or last follow up. OS will be estimated with standard K-M methodology. Point and CI estimates of the 2-year rate will derived from the K-M life table. (NCT02058706)
Timeframe: Assessed at 2 years
| Intervention | percentage alive at 2 years (Number) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 82 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 54 |
Time to Treatment Failure from date of first treatment to date off treatment or date patient is taken off study for any reason. TTF will be estimated with standard K-M methodology. Point and CI estimates of the median and various time point-specific rates will be derived from the K-M life table. (NCT02058706)
Timeframe: Assessed up to 6 years.
| Intervention | months (Median) |
|---|---|
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 8.2 |
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 20.6 |
Will be estimated with standard K-M methodology. Point and CI estimates of the six-month rate will be derived from the K-M life table. (NCT02058706)
Timeframe: From registration to PSA progression defined by PCWG II criteria or measurable disease by RECIST 1.1, assessed at 6 months
| Intervention | percentage progression-free at 6 months (Number) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 92 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 45 |
Percentage of patients progression free at one year using the Kaplan-Meier method. (NCT02058706)
Timeframe: assessed at 1 year
| Intervention | % participants not progressed at 1 year (Number) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 84 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 34 |
Number of Participants with PSA Remission Assessed Using the Prostate Cancer Clinical Trials Working Group (PCWG2) Criteria specifically at the 7 month time point. The binary endpoint (yes/no) will be summarized with its point estimate (an occurrence rate), and 2-sided Wilson type 95% confidence interval (CI). PSA response rates will be compared by treatment arm in a stratified logistic regression model. (NCT02058706)
Timeframe: Month 7
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 29 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 16 |
Will be summarized with point estimates (occurrence rates), and 2-sided Wilson type 95% CIs. (NCT02058706)
Timeframe: Up to 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 30 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 17 |
The number of participants with Measurable disease response per RECIST v1.1. (NCT02058706)
Timeframe: Up to 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm A (Enzalutamide and LHRH Analogue Therapy) | 17 |
| Arm B (Bicalutamide and LHRH Analogue Therapy) | 17 |
Treatment delays will be reported to describe tolerability within each arm. (NCT02059213)
Timeframe: Up to 54 months
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| No Treatment delay of Bicalutamide | Treatment Delay of Bicalutamide | No Treatment Delay of Palbociclib | Treatment Delay of Palbociclib | |
| ADT + Ibrance® | 35 | 5 | 21 | 19 |
| ADT Alone | 19 | 1 | 0 | 0 |
Dose modifications will be reported to describe tolerability for arm 2 only (Ibrance®) (NCT02059213)
Timeframe: Up to 54 months
| Intervention | participants (Number) | ||
|---|---|---|---|
| No Dose Reduction (Palbociclib 125mg/day) | 1 Dose Reduction, to Palbociclib 100mg/day | 2 Dose Reductions, to Palbociclib 75mg/day | |
| ADT + Ibrance® | 28 | 5 | 7 |
The primary analysis will be assessment of the proportion of patients who achieve a (Prostate-specific antigen) PSA < 4ng/mL after seven months of protocol treatment in each arm. (NCT02059213)
Timeframe: 28 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| ADT Alone | 16 |
| ADT + Ibrance® | 32 |
12-month clinical progression-free survival rate will begin from treatment start until the event of biochemical (PSA) progression or death, whichever occurs first. Described by arm using Kaplan-Meier methods. (NCT02059213)
Timeframe: Up to 54 months
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| 12-month | 22-month (time of last event in Arm 1) | 32-month (time of last event in Arm 2) | |
| ADT + Ibrance® | 83.8 | 77.7 | 58.5 |
| ADT Alone | 77.7 | 64.8 | 64.8 |
12-month biochemical progression-free survival rate will begin from treatment start until the event of biochemical (PSA) progression or death, whichever occurs first. Described by arm using Kaplan-Meier methods. (NCT02059213)
Timeframe: Up to 54 months
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| 12-month | 26-month (time of last event in Arm 1) | 43-month (time of last event in Arm 2) | |
| ADT + Ibrance® | 76.5 | 59.4 | 33.9 |
| ADT Alone | 74.7 | 45.8 | 45.8 |
(NCT02059213)
Timeframe: Up to 54 months
| Intervention | Participants (Count of Participants) |
|---|---|
| ADT Alone | 13 |
| ADT + Ibrance® | 22 |
Grade >=3 adverse events that are possibly, probably or definitely related to study treatment, reported by number of participants affected in each arm (NCT02059213)
Timeframe: Up to 54 months
| Intervention | participants (Number) |
|---|---|
| ADT Alone | 0 |
| ADT + Ibrance® | 23 |
Duration of therapy will be reported to describe tolerability within each arm. (NCT02059213)
Timeframe: Up to 54 months
| Intervention | months (Mean) |
|---|---|
| ADT Alone | 22.4 |
| ADT + Ibrance® | 22.0 |
Assessment will number of participants who experience adverse events greater than or equal to Grade 3, as defined by NCI Common terminology criteria for adverse events(CTCAE) v4.0 (NCT02064582)
Timeframe: 12 months following initiation of treatment with enzalutamide plus GnRH agonist
| Intervention | Participants (Count of Participants) |
|---|---|
| Enzalutamide, Leuprolide, Radiation | 0 |
Fold change of Intra-tumoral Androgen Regulated Gene Expression (PSA, FKBP5, TMPRSS2, and NDRG1) will be measure at 12 months post therapy. (NCT02064582)
Timeframe: 12 months
| Intervention | Fold change (Median) | |||
|---|---|---|---|---|
| Fold change in PSA | Fold change in FKBP5 | Fold change in TMPRSS2 | Fold change in NDRG1 | |
| Enzalutamide, Leuprolide, Radiation | 0.54 | 2.2 | 0.65 | 0.36 |
Blood was collected and serum concentrations of SHBG were obtained using a validated laboratory test at a central laboratory facility. (NCT02083185)
Timeframe: Day 1 of Weeks 2, 5, 13, 25, 49, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | nanomoles per liter (nmol/L) (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 2, Day 1 | Week 5, Day 1 | Week 13, Day 1 | Week 25, Day 1 | Week 49, Day 1 | EOT | Follow-Up | End of Study | |
| Relugolix 120 mg | 48.594 | 49.185 | 50.538 | 50.774 | 54.022 | 54.105 | 60.250 | 51.063 |
| Relugolix 80 mg | 50.811 | 49.641 | 49.210 | 47.998 | 50.607 | 50.013 | 45.433 | 51.103 |
(NCT02083185)
Timeframe: During Weeks 1 to 24
| Intervention | days (Median) | |
|---|---|---|
| Time to Castration (< 50 ng/dL) | Time to Profound Castration (< 20 ng/dL) | |
| Leuprorelin 22.5 mg | 29 | 29 |
| Relugolix 120 mg | 4 | 15 |
| Relugolix 80 mg | 4 | 15 |
A single 12-lead ECG was performed. ECGs were read and interpreted locally and reviewed if indicated by the study monitor. ECG abnormalities were reported as AEs. (NCT02083185)
Timeframe: From first dose of study drug to 30 days after last dose of study drug up to 106.7 weeks
| Intervention | participants (Number) |
|---|---|
| Relugolix 80 mg | 0 |
| Relugolix 120 mg | 0 |
| Leuprorelin 22.5 mg | 0 |
EORTC QLQ-PR25 is an EORTC module designed to supplement the QLQ-C30 for any application in prostate cancer consisting of 25 questions distributed on 6 domains: urinary symptoms (8 items), incontinence aid (1 item), bowel symptoms (4 items), hormonal treatment-related symptoms (HTRS) (6 items), sexual activity (2 items), and sexual functioning (4 items). Questions use are answered using a 4-point scale: 1=Not at all to 4 =Very much. All raw domain scores are linearly transformed to a 0 to 100 scale, with higher scores reflecting either more symptoms (urinary, bowel, hormonal treatment-related symptoms) or higher levels of activity or functioning (sexual). A positive change from Baseline in activity or functioning scales and negative change from Baseline in symptom scales indicates improvement. (NCT02083185)
Timeframe: Baseline and Day 1 of Weeks 5,13, 25, 37 and 49, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | score on a scale (Mean) | |||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sexual Activity: Week 5, Day 1 | Sexual Activity: Week 13, Day 1 | Sexual Activity: Week 25, Day 1 | Sexual Activity: Week 37, Day 1 | Sexual Activity: Week 49, Day 1 | Sexual Activity: EOT | Sexual Activity: Follow-up | Sexual Activity: End of Study | Sexual Functioning: Week 5, Day 1 | Sexual Functioning: Week 13, Day 1 | Sexual Functioning: Week 25, Day 1 | Sexual Functioning: Week 37, Day 1 | Sexual Functioning: Week 49, Day 1 | Sexual Functioning: EOT | Sexual Functioning: Follow-up | Sexual Functioning: End of Study | Urinary Symptoms: Week 5, Day 1 | Urinary Symptoms: Week 13, Day 1 | Urinary Symptoms: Week 25, Day 1 | Urinary Symptoms: Week 37, Day 1 | Urinary Symptoms: Week 49, Day 1 | Urinary Symptoms: EOT | Urinary Symptoms: Follow-up | Urinary Symptoms: End of study | Bowel Symptoms: Week 5, Day 1 | Bowel Symptoms: Week 13, Day 1 | Bowel Symptoms: Week 25, Day 1 | Bowel Symptoms: Week 37, Day 1 | Bowel Symptoms: Week 49, Day 1 | Bowel Symptoms: EOT | Bowel Symptoms: Follow-up | Bowel Symptoms: End of Study | HTRS: Week 5, Day 1 | HTRS: Week 13, Day 1 | HTRS: Week 25, Day 1 | HTRS: Week 37, Day 1 | HTRS: Week 49, Day 1 | HTRS: EOT | HTRS: Follow-up | HTRS: End of Study | Incontinence Aid: Week 5, Day 1 | Incontinence Aid: Week 13, Day 1 | Incontinence Aid: Week 25, Day 1 | Incontinence Aid: Week 37, Day 1 | Incontinence Aid: Week 49, Day 1 | Incontinence Aid: EOT | Incontinence Aid: Follow-up | Incontinence Aid: End of Study | |
| Leuprorelin 22.5 mg | -7.6 | -11.1 | -18.8 | -14.3 | -17.5 | -30.8 | -14.3 | -21.9 | -4.2 | 0.8 | -16.7 | -19.8 | 6.0 | 37.5 | 2.1 | -13.9 | 4.2 | 6.8 | 7.2 | 12.9 | 9.9 | 9.0 | 9.8 | 6.8 | 0.3 | 2.4 | 1.1 | 3.2 | 2.4 | 2.6 | 2.4 | 1.0 | 3.5 | 7.2 | 10.9 | 13.2 | 15.9 | 17.9 | 15.9 | 12.5 | -16.7 | -16.7 | -16.7 | -16.7 | -22.2 | -16.7 | -33.3 | -33.3 |
| Relugolix 120 mg | -14.4 | -17.3 | -19.8 | -14.4 | -19.1 | -18.1 | -24.6 | -15.5 | -2.0 | -1.4 | -12.5 | -12.8 | -13.9 | -10.7 | -10.4 | -4.2 | 1.8 | 3.8 | 5.1 | 4.2 | 6.5 | 7.1 | 5.9 | 4.5 | 1.1 | 1.8 | 0.3 | 1.5 | 0.0 | 2.4 | 2.2 | -0.3 | 5.0 | 10.8 | 11.3 | 12.2 | 9.6 | 14.0 | 6.1 | 9.8 | -1.9 | -1.8 | 0.0 | -1.8 | -2.2 | 6.1 | -8.3 | -4.8 |
| Relugolix 80 mg | -6.0 | -9.3 | -9.4 | -12.0 | -13.0 | -15.7 | -9.2 | -7.9 | -9.9 | -8.3 | -4.7 | -10.7 | -16.7 | -16.7 | 3.1 | -11.5 | 2.0 | 1.9 | 3.6 | 3.4 | 4.0 | 3.3 | -1.0 | 2.2 | 1.9 | 1.0 | 3.1 | 3.8 | 3.0 | 2.1 | 0.0 | 2.1 | 5.6 | 9.2 | 11.7 | 13.3 | 14.4 | 12.9 | 7.5 | 10.8 | 0.0 | 0.0 | 3.5 | 8.3 | 7.0 | 6.1 | 0.0 | 0.0 |
Effective Castration rate is defined as the observed percentage of participants who have testosterone concentrations less than (<) 50 nanogram per deciliter (ng/dL) (1.73 nanomole per liter [nmol/L]) at all scheduled visits beginning after 4 weeks of treatment. (NCT02083185)
Timeframe: Day 1 of Week 5 to Day 1 of Week 25
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix 80 mg | 91 |
| Relugolix 120 mg | 91 |
| Leuprorelin 22.5 mg | 96 |
PSA nadir is the lowest PSA achieved after treatment. (NCT02083185)
Timeframe: During Weeks 1 to 24
| Intervention | micrograms per liter (µg/L) (Mean) |
|---|---|
| Relugolix 80 mg | 1.8 |
| Relugolix 120 mg | 5.2 |
| Leuprorelin 22.5 mg | 0.6 |
(NCT02083185)
Timeframe: Day 1 of Weeks 1, 2, 3, 5, 9, 13, 17, 25, 37, 49 pre-dose; Day 4 of Week 1 pre-dose; Day 1 of Weeks 5, 13, 2 hrs post-dose
| Intervention | nanograms per milliliter (ng/mL) (Mean) | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 1, Day 1 pre-dose | Week 1, Day 4 pre-dose | Week 2, Day 1 pre-dose | Week 3, Day 1 pre-dose | Week 5, Day 1 pre-dose | Week 5, Day 1, 2 hours post-dose | Week 9, Day 1 pre-dose | Week 13, Day 1 pre-dose | Week 13, Day 1, 2 hours post-dose | Week 17, Day 1 pre-dose | Week 25, Day 1 pre-dose | Week 37, Day 1 pre-dose | Week 49, Day 1 pre-dose | |
| Relugolix 120 mg | 0 | 14.2 | 8.7 | 10.3 | 8.4 | 45.4 | 8.0 | 9.0 | 42.2 | 8.9 | 11.5 | 10.9 | 9.4 |
| Relugolix 80 mg | 0 | 9.9 | 6.3 | 5.4 | 5.2 | 25.3 | 4.9 | 5.5 | 24.1 | 6.3 | 7.3 | 6.3 | 5.9 |
The EORTC QLQ-C30 included 30 questions comprising 9 multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social), 3 symptom scales (fatigue, pain, nausea/vomiting), single items (dyspnoea, appetite loss, insomnia, constipation/diarrhea and financial difficulties) and a global health and QOL scale. Most questions used a 4-point scale (1=Not at all to 4=Very much); 2 questions used a 7-point scale (1= Very poor to 7=Excellent). All domain scores were calculated as an average of item scores and transformed to 0 to 100 score range. A high score for a functional scale represents a high / healthy level of functioning, a high score for the global health status/quality of life (QoL) represents a high QoL, but a high score for a symptom scale/item represents a high level of symptomatology/problem. A positive change from Baseline in quality og life or functioning scales and negative change from Baseline in symptom or difficulties scales indicates improvement. (NCT02083185)
Timeframe: Day 1 of Weeks 5, 13, 25, 37, 49, 73, 97, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | score on a scale (Mean) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Quality of Life: Week 5, Day 1 | Quality of Life: Week 13, Day 1 | Quality of Life: Week 25, Day 1 | Quality of Life: Week 37, Day 1 | Quality of Life: Week 49, Day 1 | Quality of Life: EOT | Quality of Life: Follow-Up | Quality of Life: End of Study | Physical Functioning: Week 5, Day 1 | Physical Functioning: Week 13, Day 1 | Physical Functioning: Week 25, Day 1 | Physical Functioning: Week 37, Day 1 | Physical Functioning: Week 49, Day 1 | Physical Functioning: EOT | Physical Functioning: Follow-Up | Physical Functioning: End of Study | Role Functioning: Week 5, Day 1 | Role Functioning: Week 13, Day 1 | Role Functioning: Week 25, Day 1 | Role Functioning: Week 37, Day 1 | Role Functioning: Week 49, Day 1 | Role Functioning: EOT | Role Functioning: Follow-Up | Role Functioning: End of Study | Emotional Functioning: Week 5, Day 1 | Emotional Functioning: Week 13, Day 1 | Emotional Functioning: Week 37, Day 1 | Emotional Functioning: Week 49, Day 1 | Emotional Functioning: EOT | Emotional Functioning: Follow-Up | Emotional Functioning: End of Study | Cognitive Functioning: Week 5, Day 1 | Cognitive Functioning: Week 13, Day 1 | Cognitive Functioning: Week 25, Day 1 | Cognitive Functioning: Week 37, Day 1 | Cognitive Functioning: Week 49, Day 1 | Cognitive Functioning: EOT | Cognitive Functioning: Follow-Up | Cognitive Functioning: End of Study | Social Functioning: Week 5, Day 1 | Social Functioning: Week 13, Day 1 | Social Functioning: Week 25, Day 1 | Social Functioning: Week 37, Day 1 | Social Functioning: Week 49, Day 1 | Social Functioning: EOT | Social Functioning: Follow-Up | Social Functioning: End of Study | Fatigue: Week 5, Day 1 | Fatigue: Week 13, Day 1 | Fatigue: Week 25, Day 1 | Fatigue: Week 37, Day 1 | Fatigue: Week 49, Day 1 | Fatigue: EOT | Fatigue: Follow-up | Fatigue: End of study | Nausea and Vomiting: Week 5, Day 1 | Nausea and Vomiting: Week 13, Day 1 | Nausea and Vomiting: Week 25, Day 1 | Nausea and Vomiting: Week 37, Day 1 | Nausea and Vomiting: Week 49, Day 1 | Nausea and Vomiting: Week EOT | Nausea and Vomiting: Follow-Up | Nausea and Vomiting: End of Study | Pain: Week 5, Day 1 | Pain: Week 13, Day 1 | Pain: Week 25, Day 1 | Pain: Week 37, Day 1 | Pain: Week 49, Day 1 | Pain: EOT | Pain: Follow-Up | Pain: End of Study | Dyspnea: Week 5, Day 1 | Dyspnea: Week 13, Day 1 | Dyspnea: Week 25, Day 1 | Dyspnea: Week 37, Day 1 | Dyspnea: Week 49, Day 1 | Dyspnea: EOT | Dyspnea: Follow-Up | Dyspnea: End of Study | Insomnia: Week 5, Day 1 | Insomnia: Week 13, Day 1 | Insomnia: Week 25, Day 1 | Insomnia: Week 37, Day 1 | Insomnia: Week 49, Day 1 | Insomnia: EOT | Insomnia: Follow-Up | Insomnia: End of Study | Appetite Loss: Week 5, Day 1 | Appetite Loss: Week 13, Day 1 | Appetite Loss: Week 25, Day 1 | Appetite Loss: Week 37, Day 1 | Appetite Loss: Week 49, Day 1 | Appetite Loss: EOT | Appetite Loss: Follow-Up | Appetite Loss: End of Study | Constipation: Week 5, Day 1 | Constipation: Week 13, Day 1 | Constipation: Week 25, Day 1 | Constipation: Week 37, Day 1 | Constipation: Week 49, Day 1 | Constipation: EOT | Constipation: Follow-Up | Constipation: End Of Study | Diarrhea: Week 5, Day 1 | Diarrhea: Week 13, Day 1 | Diarrhea: Week 25, Day 1 | Diarrhea: Week 37, Day 1 | Diarrhea: Week 49, Day 1 | Diarrhea: EOT | Diarrhea: Follow-Up | Diarrhea: End Of Study | Financial Difficulties:Week 5, Day 1 | Financial Difficulties:Week 13, Day 1 | Financial Difficulties:Week 25, Day 1 | Financial Difficulties:Week 37, Day 1 | Financial Difficulties:Week 49, Day 1 | Financial Difficulties: EOT | Financial Difficulties: Follow-Up | Financial Difficulties: End of Study | |
| Leuprorelin 22.5 mg | -5.2 | -7.3 | -6.9 | -11.7 | -8.3 | -13.5 | -13.7 | -10.9 | -0.8 | -0.3 | -2.0 | -4.2 | -7.0 | -2.6 | -3.8 | -2.9 | 2.8 | 1.4 | -2.2 | -4.5 | -7.1 | -5.1 | -7.1 | -1.0 | 1.7 | -1.4 | -9.8 | -4.4 | -14.1 | -8.9 | -8.3 | -2.8 | -5.6 | -2.9 | -9.8 | -11.9 | -12.8 | -10.7 | -3.1 | 4.2 | -0.7 | -202 | -7.6 | -8.7 | -6.4 | -4.8 | 0.0 | 3.2 | 8.3 | 13.5 | 16.7 | 20.1 | 20.5 | 13.5 | 8.3 | 3.5 | 1.4 | 2.9 | 4.5 | 4.8 | 7.7 | 0.0 | 0.0 | 3.5 | 4.2 | 2.9 | 11.4 | 7.9 | 6.4 | 1.2 | -2.1 | 5.6 | 8.3 | 8.7 | 22.7 | 17.5 | 20.5 | 14.3 | 8.3 | 1.4 | 6.9 | 8.7 | 18.2 | 6.3 | 7.7 | 4.8 | 10.4 | 2.8 | 0.0 | 2.9 | 0.0 | 4.8 | 2.6 | -2.4 | 0.0 | 1.4 | 5.6 | 1.4 | 1.5 | 1.6 | 0.0 | 0.0 | 0.0 | 1.4 | 0.0 | 2.9 | 6.1 | 1.6 | 5.1 | 4.8 | 2.1 | -1.4 | 2.8 | 4.3 | 7.6 | 3.2 | 2.6 | 11.9 | 0.0 |
The EORTC QLQ-C30 included 30 questions comprising 9 multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social), 3 symptom scales (fatigue, pain, nausea/vomiting), single items (dyspnoea, appetite loss, insomnia, constipation/diarrhea and financial difficulties) and a global health and QOL scale. Most questions used a 4-point scale (1=Not at all to 4=Very much); 2 questions used a 7-point scale (1= Very poor to 7=Excellent). All domain scores were calculated as an average of item scores and transformed to 0 to 100 score range. A high score for a functional scale represents a high / healthy level of functioning, a high score for the global health status/quality of life (QoL) represents a high QoL, but a high score for a symptom scale/item represents a high level of symptomatology/problem. A positive change from Baseline in quality og life or functioning scales and negative change from Baseline in symptom or difficulties scales indicates improvement. (NCT02083185)
Timeframe: Day 1 of Weeks 5, 13, 25, 37, 49, 73, 97, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | score on a scale (Mean) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Quality of Life: Week 5, Day 1 | Quality of Life: Week 13, Day 1 | Quality of Life: Week 25, Day 1 | Quality of Life: Week 37, Day 1 | Quality of Life: Week 49, Day 1 | Quality of Life: Week 73, Day 1 | Quality of Life: Week 97, Day 1 | Quality of Life: EOT | Quality of Life: Follow-Up | Quality of Life: End of Study | Physical Functioning: Week 5, Day 1 | Physical Functioning: Week 13, Day 1 | Physical Functioning: Week 25, Day 1 | Physical Functioning: Week 37, Day 1 | Physical Functioning: Week 49, Day 1 | Physical Functioning: Week 73, Day 1 | Physical Functioning: Week 97, Day 1 | Physical Functioning: EOT | Physical Functioning: Follow-Up | Physical Functioning: End of Study | Role Functioning: Week 5, Day 1 | Role Functioning: Week 13, Day 1 | Role Functioning: Week 25, Day 1 | Role Functioning: Week 37, Day 1 | Role Functioning: Week 49, Day 1 | Role Functioning: Week 73, Day 1 | Role Functioning: Week 97, Day 1 | Role Functioning: EOT | Role Functioning: Follow-Up | Role Functioning: End of Study | Emotional Functioning: Week 5, Day 1 | Emotional Functioning: Week 13, Day 1 | Emotional Functioning: Week 37, Day 1 | Emotional Functioning: Week 49, Day 1 | Emotional Functioning: Week 73, Day 1 | Emotional Functioning: Week 97, Day 1 | Emotional Functioning: EOT | Emotional Functioning: Follow-Up | Emotional Functioning: End of Study | Cognitive Functioning: Week 5, Day 1 | Cognitive Functioning: Week 13, Day 1 | Cognitive Functioning: Week 25, Day 1 | Cognitive Functioning: Week 37, Day 1 | Cognitive Functioning: Week 49, Day 1 | Cognitive Functioning: Week 73, Day 1 | Cognitive Functioning: Week 97, Day 1 | Cognitive Functioning: EOT | Cognitive Functioning: Follow-Up | Cognitive Functioning: End of Study | Social Functioning: Week 5, Day 1 | Social Functioning: Week 13, Day 1 | Social Functioning: Week 25, Day 1 | Social Functioning: Week 37, Day 1 | Social Functioning: Week 49, Day 1 | Social Functioning: Week 73, Day 1 | Social Functioning: Week 97, Day 1 | Social Functioning: EOT | Social Functioning: Follow-Up | Social Functioning: End of Study | Fatigue: Week 5, Day 1 | Fatigue: Week 13, Day 1 | Fatigue: Week 25, Day 1 | Fatigue: Week 37, Day 1 | Fatigue: Week 49, Day 1 | Fatigue: Week 73, Day 1 | Fatigue: Week 97, Day 1 | Fatigue: EOT | Fatigue: Follow-up | Fatigue: End of study | Nausea and Vomiting: Week 5, Day 1 | Nausea and Vomiting: Week 13, Day 1 | Nausea and Vomiting: Week 25, Day 1 | Nausea and Vomiting: Week 37, Day 1 | Nausea and Vomiting: Week 49, Day 1 | Nausea and Vomiting: Week 73, Day 1 | Nausea and Vomiting: Week 97, Day 1 | Nausea and Vomiting: Week EOT | Nausea and Vomiting: Follow-Up | Nausea and Vomiting: End of Study | Pain: Week 5, Day 1 | Pain: Week 13, Day 1 | Pain: Week 25, Day 1 | Pain: Week 37, Day 1 | Pain: Week 49, Day 1 | Pain: Week 73, Day 1 | Pain: Week 97, Day 1 | Pain: EOT | Pain: Follow-Up | Pain: End of Study | Dyspnea: Week 5, Day 1 | Dyspnea: Week 13, Day 1 | Dyspnea: Week 25, Day 1 | Dyspnea: Week 37, Day 1 | Dyspnea: Week 49, Day 1 | Dyspnea: Week 73, Day 1 | Dyspnea: Week 97, Day 1 | Dyspnea: EOT | Dyspnea: Follow-Up | Dyspnea: End of Study | Insomnia: Week 5, Day 1 | Insomnia: Week 13, Day 1 | Insomnia: Week 25, Day 1 | Insomnia: Week 37, Day 1 | Insomnia: Week 49, Day 1 | Insomnia: Week 73, Day 1 | Insomnia: Week 97, Day 1 | Insomnia: EOT | Insomnia: Follow-Up | Insomnia: End of Study | Appetite Loss: Week 5, Day 1 | Appetite Loss: Week 13, Day 1 | Appetite Loss: Week 25, Day 1 | Appetite Loss: Week 37, Day 1 | Appetite Loss: Week 49, Day 1 | Appetite Loss: Week 73, Day 1 | Appetite Loss: Week 97, Day 1 | Appetite Loss: EOT | Appetite Loss: Follow-Up | Appetite Loss: End of Study | Constipation: Week 5, Day 1 | Constipation: Week 13, Day 1 | Constipation: Week 25, Day 1 | Constipation: Week 37, Day 1 | Constipation: Week 49, Day 1 | Constipation: Week 73, Day 1 | Constipation: Week 97, Day 1 | Constipation: EOT | Constipation: Follow-Up | Constipation: End Of Study | Diarrhea: Week 5, Day 1 | Diarrhea: Week 13, Day 1 | Diarrhea: Week 25, Day 1 | Diarrhea: Week 37, Day 1 | Diarrhea: Week 49, Day 1 | Diarrhea: Week 73, Day 1 | Diarrhea: Week 97, Day 1 | Diarrhea: EOT | Diarrhea: Follow-Up | Diarrhea: End Of Study | Financial Difficulties:Week 5, Day 1 | Financial Difficulties:Week 13, Day 1 | Financial Difficulties:Week 25, Day 1 | Financial Difficulties:Week 37, Day 1 | Financial Difficulties:Week 49, Day 1 | Financial Difficulties:Week 73, Day 1 | Financial Difficulties: Week 97, Day 1 | Financial Difficulties: EOT | Financial Difficulties: Follow-Up | Financial Difficulties: End of Study | |
| Relugolix 120 mg | -4.0 | -2.0 | -2.3 | -7.4 | -7.3 | -12.0 | -2.2 | -7.1 | -8.8 | -10.1 | -0.9 | -4.4 | -5.3 | -6.2 | -5.2 | -8.5 | -6.0 | -9.3 | -6.3 | -9.0 | -0.3 | -3.6 | -6.3 | -10.0 | -8.9 | -6.7 | -4.4 | -8.6 | -10.5 | -13.2 | 0.3 | -1.1 | -1.7 | -1.4 | -2.3 | 2.6 | -7.4 | -1.3 | -0.6 | -4.2 | -7.5 | -3.8 | -5.6 | -6.1 | -7.3 | -7.0 | -10.0 | -7.0 | -7.5 | -1.3 | -3.3 | -6.3 | -5.9 | -9.8 | -6.0 | -4.4 | -10.0 | -8.8 | -9.2 | 4.3 | 8.9 | 13.2 | 14.1 | 11.1 | 14.7 | 9.9 | 15.9 | 6.4 | 12.3 | 0.6 | 0.7 | 0.0 | 1.1 | 0.8 | 0.7 | 1.8 | 1.9 | 0.9 | -1.1 | 0.6 | 3.3 | 2.8 | 5.9 | 6.5 | 7.3 | 0.0 | 6.7 | 10.5 | 6.9 | 2.6 | 6.5 | 8.3 | 11.1 | 9.8 | 9.3 | 8.8 | 14.3 | 8.8 | 14.9 | 3.2 | 9.8 | 12.5 | 8.1 | 7.3 | 10.7 | 10.5 | 7.6 | 0.0 | 5.7 | 0.6 | -0.7 | 0.0 | 2.2 | 0.8 | 5.3 | 3.5 | 8.6 | 3.5 | 3.4 | 1.9 | 5.2 | 6.3 | 8.1 | 7.3 | 1.3 | 3.5 | 1.9 | 10.5 | 5.7 | 1.9 | 2.0 | 5.6 | 0.7 | -1.6 | 1.3 | 0.0 | 2.9 | 0.0 | -1.1 | 2.6 | -0.7 | 0.7 | 1.5 | 0.8 | 2.7 | 1.8 | 5.7 | 1.8 | 3.4 |
| Relugolix 80 mg | -2.7 | -2.3 | -6.4 | -6.0 | -7.2 | -3.4 | -6.6 | -4.8 | -5.4 | -7.9 | 0.9 | 0.3 | -2.8 | -4.8 | -4.3 | -5.1 | -8.1 | -3.4 | -4.0 | -8.9 | 0.3 | -1.0 | -4.9 | -10.9 | -8.1 | -8.0 | -8.8 | -9.5 | -10.0 | -10.6 | 1.9 | -0.7 | -4.3 | -3.0 | -2.0 | -2.6 | -3.6 | -3.3 | -5.3 | -0.9 | -1.0 | -0.7 | -5.8 | -2.6 | -5.7 | -6.1 | -2.9 | -0.8 | -2.3 | 0.3 | 1.6 | -1.0 | -2.5 | -3.7 | -2.9 | -5.3 | -5.2 | -3.3 | -3.7 | 1.9 | 6.1 | 6.3 | 9.7 | 10.9 | 10.0 | 5.8 | 12.1 | 7.2 | 11.4 | -1.3 | 0.7 | 0.0 | 0.4 | -1.9 | 0.0 | 5.3 | -0.5 | 3.3 | 1.4 | -1.6 | -1.0 | 0.3 | 2.9 | 3.3 | 6.9 | 5.3 | -0.5 | 9.2 | 6.5 | -0.6 | 5.9 | 4.2 | 6.5 | 6.7 | 8.0 | 10.5 | 7.6 | 11.7 | 11.1 | -1.3 | 2.6 | 6.3 | 2.2 | 6.7 | 2.3 | 10.5 | 6.7 | 5.0 | 1.9 | -3.8 | -0.7 | -3.5 | -0.7 | -0.7 | -2.3 | 0.0 | -3.8 | 0.0 | -1.9 | 0.6 | 3.9 | 2.8 | 5.8 | 2.2 | 1.1 | 1.8 | 3.8 | 5.0 | 3.7 | -1.9 | 3.9 | 2.8 | 3.6 | 3.0 | 4.6 | 7.0 | 4.8 | 3.3 | 1.9 | -1.3 | -2.0 | -3.5 | -2.9 | -5.2 | 0.0 | 5.3 | -3.8 | 5.0 | -2.8 |
An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. A SAE is any AE that results in death, is life threatening, requires hospitalization, results in persistent or significant disability or incapacity, is a congenital anomaly/birth defect or is a medically important event. (NCT02083185)
Timeframe: From first dose of study drug to 30 days after last dose of study drug up to 106.7 weeks
| Intervention | participants (Number) | |
|---|---|---|
| Any Adverse Event | SAEs | |
| Leuprorelin 22.5 mg | 23 | 2 |
| Relugolix 120 mg | 53 | 7 |
| Relugolix 80 mg | 53 | 10 |
Abnormal clinical laboratory values (serum chemistry and hematology) were reported as AEs if they were considered by the investigator to be a clinically significant change from Baseline or led to premature discontinuation of study treatment, dose modification, or other therapeutic intervention. (NCT02083185)
Timeframe: From first dose of study drug to 30 days after last dose of study drug up to 106.7 weeks
| Intervention | participants (Number) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Alanine aminotransferase increased | Aspartate aminotransferase increased | Gamma-glutamyltransferase increased | Blood triglycerides increased | Blood bilirubin increased | Hepatic enzyme increased | Prostatic specific antigen increased | Blood cholesterol increased | Low density lipoprotein increased | Blood glucose increased | Glycosylated haemoglobin increased | Blood creatinine increased | Blood lactate dehydrogenase increased | Blood alkaline phosphatase increased | Blood phosphorus increased | Blood potassium increased | Blood thyroid stimulating hormone increased | Blood testosterone increased | |
| Leuprorelin 22.5 mg | 4 | 3 | 2 | 1 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 |
| Relugolix 120 mg | 3 | 1 | 1 | 0 | 0 | 1 | 1 | 2 | 0 | 1 | 1 | 1 | 0 | 0 | 0 | 0 | 1 | 0 |
| Relugolix 80 mg | 7 | 6 | 3 | 3 | 1 | 0 | 1 | 0 | 1 | 1 | 0 | 0 | 2 | 1 | 1 | 1 | 0 | 0 |
Physical examination consists of examinations of the following body systems: (1) eyes; (2) ears, nose, throat; (3) cardiovascular system; (4) respiratory system; (5) gastrointestinal system; (6) dermatologic system; (7) extremities; (8) musculoskeletal system; (9) nervous system; (10) lymph nodes; and (11) physical examinations other than body systems described in (1) to (10) including slit lamp examination of the anterior eye. Any TEAEs Related to physical examination were reported. (NCT02083185)
Timeframe: From first dose of study drug to 30 days after last dose of study drug up to 106.7 weeks
| Intervention | participants (Number) | ||
|---|---|---|---|
| Weight increased | Weight decreased | Ophthalmological examination abnormal | |
| Leuprorelin 22.5 mg | 0 | 2 | 0 |
| Relugolix 120 mg | 2 | 0 | 0 |
| Relugolix 80 mg | 4 | 1 | 1 |
Vital signs included oral temperature, pulse rate, supine systolic and diastolic blood pressure, standing systolic and diastolic blood pressure, and weight. Any TEAEs that were associated with vital signs were reported. (NCT02083185)
Timeframe: From first dose of study drug to 30 days after last dose of study drug up to 106.7 weeks
| Intervention | participants (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Syncope | Hypertension | Hypotension | Arrhythmia | Bradycardia | Tachycardia | Heart rate irregular | Weight increased | Weight decreased | Pyrexia | |
| Leuprorelin 22.5 mg | 0 | 1 | 0 | 0 | 0 | 1 | 0 | 0 | 2 | 0 |
| Relugolix 120 mg | 2 | 4 | 2 | 1 | 0 | 1 | 0 | 2 | 0 | 0 |
| Relugolix 80 mg | 3 | 1 | 1 | 0 | 2 | 1 | 1 | 4 | 1 | 3 |
AMS scale is a self-administered questionnaire used to: 1) assess symptoms of aging (independent from those that are disease related) between groups of males under different conditions; 2) evaluate the severity of symptoms over time; and 3) measure changes before and after androgen therapy. Each question was answered between 1=none to 5=extremely severe for 17 items from psychological (5 items), somatic (7 items), and sexual (5 items) categories. Total score is sum of all the item scores and range from 17 (minimum) to 85 (maximum), where high score indicated high level of symptoms. (NCT02083185)
Timeframe: Baseline and Day 1 of Weeks 5,13, 25, 37 and 49, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | percent change (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 5, Day 1 | Week 13, Day 1 | Week 25, Day 1 | Week 37, Day 1 | Week 49, Day 1 | EOT | Follow-Up | End of Study | |
| Leuprorelin 22.5 mg | 10.083 | 21.887 | 46.995 | 49.422 | 59.971 | 60.952 | 53.834 | 49.879 |
| Relugolix 120 mg | 10.872 | 17.259 | 20.353 | 24.466 | 24.377 | 28.644 | 13.031 | 21.304 |
| Relugolix 80 mg | 3.914 | 14.781 | 20.272 | 24.136 | 30.122 | 18.857 | 15.754 | 16.270 |
PSA Response is defined as a reduction in PSA from Baseline and is reported for 2 categories: ≥ 50% reduction and ≥ 90% reduction. (NCT02083185)
Timeframe: Week 5, Day 1
| Intervention | percentage of participants (Number) | |
|---|---|---|
| ≥ 50% PSA reduction | ≥ 90% PSA reduction | |
| Leuprorelin 22.5 mg | 17 | 0 |
| Relugolix 120 mg | 83 | 6 |
| Relugolix 80 mg | 75 | 13 |
Blood was collected and serum concentrations of LH in milli international units per milliliters (mIU/mL) were obtained using a validated laboratory test at a central laboratory facility. (NCT02083185)
Timeframe: Baseline and Day 4 of Week 1, Day 1 of Weeks 2, 3, 5,13, 25 and 49, End of Treatment (EOT - 106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | mIU/mL (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 1, Day 4 | Week 2, Day 1 | Week 3, Day 1 | Week 5, Day 1 | Week 13, Day 1 | Week 25, Day 1 | Week 49, Day 1 | EOT | Follow-Up | End of Study | |
| Leuprorelin 22.5 mg | 17.551 | 8.279 | 3.171 | 0.508 | 0.277 | 0.134 | 0.138 | 0.585 | 0.525 | 1.394 |
| Relugolix 120 mg | 0.595 | 0.638 | 0.388 | 0.203 | 0.183 | 0.175 | 0.288 | 2.704 | 9.510 | 9.306 |
| Relugolix 80 mg | 0.665 | 0.548 | 0.341 | 0.424 | 0.229 | 0.195 | 0.341 | 3.189 | 8.624 | 7.182 |
Blood was collected and serum concentrations of PSA were obtained using a validated laboratory test at a central laboratory facility. (NCT02083185)
Timeframe: Day 1 of Weeks 13 and 25
| Intervention | μg/L (Mean) | |
|---|---|---|
| Week 13, Day 1 | Week 25, Day 1 | |
| Leuprorelin 22.5 mg | 0.916 | 0.624 |
| Relugolix 120 mg | 5.786 | 2.360 |
| Relugolix 80 mg | 2.651 | 1.936 |
Blood was collected and serum concentrations of SHBG were obtained using a validated laboratory test at a central laboratory facility. (NCT02083185)
Timeframe: Day 1 of Weeks 2, 5, 13, 25, 49, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | nanomoles per liter (nmol/L) (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Week 2, Day 1 | Week 5, Day 1 | Week 13, Day 1 | Week 25, Day 1 | Week 49, Day 1 | EOT | End of Study | |
| Leuprorelin 22.5 mg | 39.029 | 43.786 | 41.858 | 40.839 | 38.237 | 23.000 | 39.014 |
Blood was collected and serum concentrations of FSH were obtained using a validated laboratory test at a central laboratory facility. (NCT02083185)
Timeframe: Day 1 of Weeks 2, 5, 13, 25, 49, EOT (106.4 Weeks), Follow-up (110.4 Weeks) and End of Study (114.4 Weeks)
| Intervention | IU/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 2, Day 1 | Week 5, Day 1 | Week 13, Day 1 | Week 25, Day 1 | Week 49, Day 1 | EOT | Follow-Up | End of Study | |
| Leuprorelin 22.5 mg | 7.650 | 2.946 | 4.625 | 5.043 | 5.145 | 5.250 | 9.200 | 5.943 |
| Relugolix 120 mg | 3.183 | 1.035 | 0.908 | 1.344 | 1.938 | 5.691 | 14.610 | 15.768 |
| Relugolix 80 mg | 3.112 | 1.248 | 1.137 | 1.090 | 1.802 | 5.377 | 16.160 | 11.441 |
Staging biopsy of at least 12 cores were sampled and analyzed according to a centralized biopsy procedure which confirm the results of the first biopsy [presence of positive cores, the absence of core with tumor length > 3 millimeters (mm), and absence Grade 4 cells (Gleason score < 7)]. The Gleason score grades prostate cancer tissue, based on its appearance under a microscope. Scores range from 2 to 10, with a higher score meaning that the cancer tissue is more likely to spread. (NCT02085252)
Timeframe: Month 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Leuprorelin 11.25 mg | 28 |
| Active Surveillance | 17 |
The HADS is a 14-item scale that measures anxiety (7-items) and depression (7-items) over the previous week. Each question is answered on a scale of 0 (best) to 3 (worst) for a total possible score of 0 to 42, with higher scores indicating more anxiety and depression. A negative change from baseline indicates improvement. An ANCOVA model fitted with baseline HADS score and age as covariates was used for analyses. (NCT02085252)
Timeframe: Baseline and Months 3, 6, 9 and 12
| Intervention | score on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Change at Month 3 | Change at Month 6 | Change at Month 9 | Change at Month 12 | |
| Active Surveillance | -1.20 | -1.58 | -1.76 | -1.95 |
| Leuprorelin 11.25 mg | -0.83 | -1.44 | -2.06 | -1.87 |
Gleason score grades prostate cancer tissue, based on its appearance under a microscope. Scores range from 2 to 10, with a higher score meaning that the cancer tissue is more likely to spread. (NCT02085252)
Timeframe: Month 12
| Intervention | Participants (Count of Participants) |
|---|---|
| Leuprorelin 11.25 mg | 1 |
| Active Surveillance | 3 |
The IIEF-5, a 5 question patient completed questionnaire, is a measure of erectile dysfunction over the past 6 months. Each question is answered on a scale of 1 (worst) to 5 (best). Total score ranges from 5 to 25 with higher scores indicating better function (5-7: severe; 8-11: moderate; 12-16: mild to moderate;17-21: mild; 22-25: none). A positive change from baseline indicates improvement. A negative change from baseline indicates a worsening. An ANCOVA model fitted with baseline IIEF-5 score and age as covariates was used for analyses. (NCT02085252)
Timeframe: Baseline and Months 3, 6, 9 and 12
| Intervention | score on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Change at Month 3 | Change at Month 6 | Change at Month 9 | Change at Month 12 | |
| Active Surveillance | 0.00 | 0.01 | -0.38 | -0.02 |
| Leuprorelin 11.25 mg | -7.40 | -5.87 | -1.94 | -1.68 |
The I-PSS is an 8-question tool used to measure prostate symptoms (≤7: mildly symptomatic; 8-19 moderately symptomatic; 20-35 severely symptomatic). The first 7 symptom questions answered on a scale of 0 (never) to 5 (almost always) are used to determine the I-PSS Total S Score for a total possible score of 0 to 35. The 8th question is quality of life and is not reported here. A negative change from baseline indicates improvement. An Analysis of Covariance (ANCOVA) model fitted with baseline I-PSS total score and age as covariates was used for analysis. (NCT02085252)
Timeframe: Baseline and Months 3, 6, 9 and 12
| Intervention | score on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Change at Month 3 | Change at Month 6 | Change at Month 9 | Change at Month 12 | |
| Active Surveillance | 1.03 | 0.32 | 0.64 | 0.93 |
| Leuprorelin 11.25 mg | 0.37 | -0.38 | -1.13 | -0.48 |
MRI is an imaging technique used to investigate the anatomy and function of the body. Measurements were taken to determine the diameter of the lesions in millimeters (mm). (NCT02085252)
Timeframe: Baseline and Month 12
| Intervention | mm (Mean) | |
|---|---|---|
| Baseline | Month 12 | |
| Active Surveillance | 7.78 | 7.69 |
| Leuprorelin 11.25 mg | 6.39 | 6.25 |
MRI is an imaging technique used to investigate the anatomy and function of the body. Measurements were taken to calculate the prostatic volume in cubic millimeters (mm^3). (NCT02085252)
Timeframe: Baseline and Month 12
| Intervention | mm^3 (Mean) | |
|---|---|---|
| Baseline | Month 12 | |
| Active Surveillance | 49.44 | 48.33 |
| Leuprorelin 11.25 mg | 48.48 | 51.47 |
Blood was collected and sent to a central laboratory for analysis of PSA reported in milligrams/milliliter (mg/mL). A negative change from baseline indicates improvement. An ANCOVA model fitted with baseline PSA Level and age as covariates was used for analyses. (NCT02085252)
Timeframe: Baseline and Months 3, 6, 9 and 12
| Intervention | mg/mL (Least Squares Mean) | |||
|---|---|---|---|---|
| Change at Month 3 | Change at Month 6 | Change at Month 9 | Change at Month 12 | |
| Active Surveillance | 0.22 | 0.85 | 0.71 | 0.76 |
| Leuprorelin 11.25 mg | -4.61 | -3.27 | -1.46 | 0.17 |
Change in score on the Digit Span Test between baseline and 6 month. Raw scores on the Digit Span test range from 0-16 (Digits Forward) and 0-10 (Digits Backward) with higher scores indicating better performance. A positive change score indicates improved performance. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | number of correct trials (Mean) | |
|---|---|---|
| Digits Forward (trials correct) | Digits Backward (trials correct) | |
| GnRH Agonist | -0.88 | 0.00 |
| Placebo | 1.00 | -0.67 |
Changes in patterns of brain activation in the prefrontal cortex using functional magnetic resonance imaging (fMRI) during a task of working memory will be measured at baseline, 6 months, and 9 months (GnRH agonist arm only). Beta weight is the percent signal change on the FMRI from one condition to another. The FMRI is measuring blood oxygen levels and blood flow in different regions of the brain and using that to determine activity changes in the brain. A positive number/increase indicates more blood flow and brain activity in that area. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | beta-weight (Mean) | ||
|---|---|---|---|
| Frontal Pole (L) | Frontal Orbital Cortex (L) | Superior Frontal Gyrus (R) | |
| GnRH Agonist | -27.15 | -88.87 | -77.23 |
"Change in Rey Auditory Verbal Learning Test from baseline to 9 months.~Score is the change in the number of items correct on delayed recall trial. Scores on the RAVLT range from 0-15 with higher scores indicating better performance. A positive change indicates improvement in recall." (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | number of items recalled (Mean) |
|---|---|
| GnRH Agonist | 0 |
"Change in Rey Auditory Verbal Learning Test from baseline to 6 months.~Score is the change in the number of items correct on delayed recall trial. Scores on the RAVLT range from 0-15 with higher scores indicating better performance. A positive change indicates improvement in recall." (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | number of items recalled (Mean) |
|---|---|
| Placebo | -1.00 |
| GnRH Agonist | -1.38 |
Change in sum of scores on 3 COWAT trials (letters, F, A, and S) between baseline and 9 months. Participants are given one minute to think up as many words as they can associated with each letter (F, A, or S). Raw scores are the total number of words generated across all trials. Higher scores indicate more words generated and better performance. Positive change score indicates an increase in words generated, or improved performance. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | words generated (Mean) |
|---|---|
| GnRH Agonist | 7.33 |
Change in sum of scores on 3 COWAT trials (letters, F, A, and S) between baseline and 6 months. Participants are given one minute to think up as many words as they can associated with each letter (F, A, or S). Raw scores are the total number of words generated across all trials. Higher scores indicate more words generated and better performance. Positive change score indicates an increase in words generated, or improved performance. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | words generated (Mean) |
|---|---|
| Placebo | -5.33 |
| GnRH Agonist | 0.25 |
Changes in carotid artery compliance will be measured using ultrasound in at baseline, 9 months. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | mm^2/mmhgx10^-1 (Mean) |
|---|---|
| GnRH Agonist | -0.002 |
Changes in carotid artery compliance will be measured using ultrasound in at baseline, 6 months. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | mm^2/mmhgx10^-1 (Mean) |
|---|---|
| Placebo | -0.048 |
| GnRH Agonist | -0.095 |
Changes in patterns of brain activation in the prefrontal cortex using functional magnetic resonance imaging (fMRI) during a task of working memory will be measured at baseline, 6 months, and 9 months (GnRH agonist arm only). Beta weight is the percent signal change on the FMRI from one condition to another. The FMRI is measuring blood oxygen levels and blood flow in different regions of the brain and using that to determine activity changes in the brain. A positive number/increase indicates more blood flow and brain activity in that area. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | beta-weight (Mean) | ||
|---|---|---|---|
| Frontal Pole (L) | Frontal Orbital Cortex (L) | Superior Frontal Gyrus (R) | |
| GnRH Agonist | -62.20 | -79.04 | -53.05 |
| Placebo | 90.64 | 28.07 | 92.45 |
Change in number of correct responses in one minute on Stroop Color Word Interference test between baseline and 6 months. A positive number indicates more items correct indicating better performance. There is no maximum score because the test measures how many correct responses a participant can return within one minute (minimum = 0), however 40 or fewer is considered low. The change in the number of correct responses is reported, and so a positive number indicates more correct responses and better/improved cognitive function. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | number correct in one minute (Mean) |
|---|---|
| Placebo | -0.67 |
| GnRH Agonist | 0.25 |
Change in number of correct responses in one minute on Stroop Color Word Interference test between baseline and 9 months. Positive number indicates more items correct indicating better performance. There is no maximum score because the test measures how many correct responses a participant can return within one minute (minimum = 0), however 40 or fewer is considered low. The change in the number of correct responses is reported, and so a positive number indicates more correct responses and better/improved cognitive function. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | number correct in one minute (Mean) |
|---|---|
| GnRH Agonist | 7.33 |
Change in time (seconds) to complete Trails A test between baseline and 6 months. Negative value indicates faster time (better performance) at 6 months compared to baseline. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | seconds (Mean) |
|---|---|
| Placebo | 2.79 |
| GnRH Agonist | -5.82 |
Change in time (seconds) to complete Trails A test between baseline and 9 months. Negative value indicates faster time (better performance) at 9 months compared to baseline. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | time (seconds) (Mean) |
|---|---|
| GnRH Agonist | -5.46 |
Change in time (seconds) to complete Trails B test between baseline and 6 months. Negative value indicates faster time (better performance) at 6 months compared to baseline. (NCT02122198)
Timeframe: Baseline, 6 months
| Intervention | time (seconds) (Mean) |
|---|---|
| Placebo | 14.23 |
| GnRH Agonist | -4.32 |
Change in score on the Digit Span Test between baseline and 9 months. Raw scores on the Digit Span test range from 0-16 (Digits Forward) and 0-10 (Digits Backward) with higher scores indicating better performance. A positive change score indicates improved performance. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | number of trials correct (Mean) | |
|---|---|---|
| Digits Forward (trials correct) | Digits Backward (trials correct) | |
| GnRH Agonist | 1.00 | 1.0 |
Change in time (seconds) to complete Trails B test between baseline and 9 months. Negative value indicates faster time (better performance) at 9 months compared to baseline. (NCT02122198)
Timeframe: Baseline, 9 months
| Intervention | time (seconds) (Mean) |
|---|---|
| GnRH Agonist | 14.14 |
QOL-ACD score is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. It includes 4 subscale domains: Daily Activities, Physical Condition, Social Activities, Mental and Psychological Status. Total and subscale scores are calculated as sum of items within each subscale: Daily Activity (items 1-6), Physical Condition (7-11), Psychological Condition (12-16), Social Attitude (17-21) and total (1-22). Face scale: 5-point score for 1 item (22). Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Score range for total score is 22 to 110 and subscale score range for daily activity is 6 to 30, and for physical condition, psychological condition, and social attitude is 5 to 25. Less total/subscale scores reflect greater symptom severity and symptom impact on health-related QOL. (NCT02134977)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Total score (n=2174) | Daily activity (n=2178) | Physical condition (n=2178) | Psychological condition (n=2178) | Social relationships (n=2177) | |
| Leuprorelin Acetate | 88.9 | 28.0 | 21.9 | 19.1 | 16.0 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). QOL-ACD is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Total score for QOL-ACD-B is calculated as a sum of 18 items, score range: 18 to 90 where less scores reflect greater symptom severity and symptom impact on health-related quality of life. Means and standard deviations were calculated for the total score and score of each subscale from questionnaire items 1 to 18. (NCT02134977)
Timeframe: Week 12
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Total score: (n=2025) | Physical condition and pain: (n=2031) | Health-care and illness satisfaction: (n=2029) | |
| Leuprorelin Acetate | 71.0 | 73.1 | 85.2 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). QOL-ACD is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Total score for QOL-ACD-B is calculated as a sum of 18 items, score range: 18 to 90 where less scores reflect greater symptom severity and symptom impact on health-related quality of life. Means and standard deviations were calculated for the total score and score of each subscale from questionnaire items 1 to 18. (NCT02134977)
Timeframe: Week 48
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Total score (n=1651) | Physical condition and pain (n=1659) | Healthcare and illness satisfaction (n=1656) | |
| Leuprorelin Acetate | 71.9 | 74.8 | 84.9 |
"The question was with regard to the assessment of convenience associated with the changes in agents, The change in agents reduced the frequency of injections by one third; for this reason, did you feel relief from physical and emotional burden? and the answers were categorized as felt extreme relief, felt slight relief, no feeling either way, felt little relief, felt no relief." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Felt extreme relief | Felt slight relief | No feeling either way | Felt little relief | Felt no relief | Not determined | |
| Leuprorelin Acetate | 34.8 | 31.6 | 17.8 | 7.1 | 4.8 | 3.9 |
"The question was with regard to the assessment of convenience associated with the changes in agents, The change in agents reduced the frequency of injections by one third; for this reason, did you worry about the effect? and the options of the answers were not at all worried, not too worried, no thought either way, somewhat worried, and very worried." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Not at all worried | Not too worried | No thought either way | Somewhat worried | Very worried | Not determined | |
| Leuprorelin Acetate | 29.7 | 33.8 | 22.4 | 9.8 | 0.8 | 3.5 |
"The question was with regard to the assessment of convenience associated with the changes in agents, Was there a change in adverse drug reactions (e.g., menopausal-like symptoms such as hot flushes, injection-site abnormalities) due to the change in agents? and the options of the answers were events became much less severe, events became less severe, whether or not the events became severe cannot be determined, events became slightly more severe, and events became very severe." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Events became much less severe | Events became less severe | Cannot be determined | Events became slightly more severe | Events became very severe | Not determined | |
| Leuprorelin Acetate | 1.4 | 5.5 | 68.5 | 17.0 | 3.9 | 3.7 |
"The question was with regard to the assessment of convenience associated with the changes in agents, Was there a change in pain at the time of injection due to the change in agents? and the options of the answers were significantly relieved, slightly relieved, whether or not the pain worsened or was relieved cannot be determined, worsened slightly, and worsened significantly." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Significantly relieved | Slightly relieved | Cannot be determined | Worsened slightly | Worsened significantly | Not determined | |
| Leuprorelin Acetate | 4.7 | 10.4 | 64.9 | 14.4 | 2.1 | 3.5 |
"The question was with regard to the assessment of convenience associated with the changes in agents, Was the change in agents good? and the options of the answers were very good, somewhat good, whether or not the change in agents was good cannot be determined, somewhat bad, very bad." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Very good | Somewhat good | Cannot be determined | Somewhat bad | Very bad | Not determined | |
| Leuprorelin Acetate | 32.0 | 36.5 | 26.0 | 1.3 | 0.5 | 3.7 |
"The question was with regard to the assessment of convenience associated with the changes in agents, Did the change in agents reduce the frequency of your medical visits? and the answers were categorized as very much reduced, somewhat reduced, unchanged. Change in medicinal agents means participants with a historical diagnosis of premenopausal breast cancer who switched to leuprorelin acetate sustained-release 11.25 mg injection kit from a 4-week adjuvant therapy with a LH-RHa 1 month depot preparation as part of daily medical practice." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Very much reduced | Somewhat reduced | Unchanged | Not determined | |
| Leuprorelin Acetate | 67.7 | 10.1 | 16.9 | 5.3 |
"The question was with regard to the assessment of convenience associated with the changes in agents, Did you feel relief from financial burden (example, 3 months' drug costs and transportation fee) due to the change in agents? and the answers were categorized as felt extreme relief, felt slight relief, no feeling either way, felt little relief, felt no relief. The sum of all the categories is not 100% because of rounding error." (NCT02134977)
Timeframe: Week 48
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Felt extreme relief | Felt slight relief | No feeling either way | Felt little relief | Felt no relief | Not determined | |
| Leuprorelin Acetate | 22.2 | 41.0 | 21.2 | 9.5 | 2.4 | 3.6 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). QOL-ACD is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Total score was calculated over score range 0-100 for item 1 to 18 as ((a sum of 18 items)/18-1)*25). Score for physical condition and pain was calculated over score range 0-100 for item 1 to 6 as ((a sum of 6 items)/6-1)*25)). Score for health-care and illness satisfaction was calculated over score range 0-100 for item 7 to 10 as ((a sum of 4 items)/4-1)*25)), where less scores reflect greater symptom severity and symptom impact on health-related quality of life. Means and standard deviations were calculated for the total score and score of each subscale from questionnaire items 1 to 18. (NCT02134977)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Total score (n=2172) | Physical condition and pain (n=2175) | Health-care and illness satisfaction (n=2176) | |
| Leuprorelin Acetate | 70.4 | 72.3 | 85.1 |
QOL-ACD score is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. It includes 4 subscale domains: Daily Activities, Physical Condition, Social Activities, Mental and Psychological Status. Total and subscale scores are calculated as sum of items within each subscale: Daily Activity (items 1-6), Physical Condition (7-11), Psychological Condition (12-16), Social Attitude (17-21) and total (1-22). Face scale:5-point score for 1 item (22). Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Score range for total score is 22 to 110 and subscale score range for daily activity is 6 to 30, and for physical condition, psychological condition, and social attitude is 5 to 25. Less total/subscale scores reflect greater symptom severity and symptom impact on health-related QOL. (NCT02134977)
Timeframe: Week 12
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Total score (n=2031) | Daily activity (n=2034) | Physical condition (n=2034) | Psychological condition (n=2035) | Social relationships (n=2034) | |
| Leuprorelin Acetate | 88.7 | 27.9 | 21.8 | 18.8 | 16.3 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). For questionnaire item 19 (Did you feel inferior to your child when you interact with him/her? [due to the impact of illness and treatment]), item 20 (Did you worry about child rearing? [due to the impact of illness and treatment]), and item 21 (Do you worry about pregnancy or delivery? [due to the impact of illness and treatment]), the calculation was based on the score of each item. Each item was scored on a 5-point scale, where 1 was the worst response and 5 was the best. (NCT02134977)
Timeframe: Baseline
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Item 19: (n=631) | Item 20: (n=624) | Item 21: (n=203) | |
| Leuprorelin Acetate | 3.3 | 2.9 | 1.7 |
QOL-ACD score is a score used for cancer participants treated with anti-cancer drug and is a 22-item self-reported instrument assessing differences in symptom severity and health-related QOL. It includes 4 subscale domains: Daily Activities, Physical Condition, Social Activities, Mental and Psychological Status. Total and subscale scores are calculated as sum of items within each subscale: Daily Activity (items 1-6), Physical Condition (7-11), Psychological Condition (12-16), Social Attitude (17-21) and total (1-22). Face scale: 5-point score for 1 item (22). Participants answer each question on a 5-point scale (1: not at all [worst response] to 5: very much [best response]). Score range for total score is 22 to 110 and subscale score range for daily activity is 6 to 30, and for physical condition, psychological condition, and social attitude is 5 to 25. Less total/subscale scores reflect greater symptom severity and symptom impact on health-related QOL. (NCT02134977)
Timeframe: Week 48
| Intervention | units on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Total score (n=1658) | Daily activity (n=1662) | Physical condition (n=1662) | Psychological condition (n=1662) | Social relationships (n=1662) | |
| Leuprorelin Acetate | 89.9 | 28.1 | 22.2 | 19.1 | 16.6 |
Adverse drug reactions are defined as adverse events (AE) which are in the investigator's opinion of causal relationship to the study treatment. AE are defined as any unfavorable and unintended signs, symptoms or diseases temporally associated with the use of a medicinal product reported from the first dose of study drug to the last dose of study drug. (NCT02134977)
Timeframe: Baseline up to Week 48
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 427 |
Serious adverse drug reactions are defined as serious adverse events (SAE) which are in the investigator's opinion of causal relationship to the study treatment. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. The event was occurred in breast cancer female. (NCT02134977)
Timeframe: Baseline up to Week 48
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 8 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). For questionnaire item 19 (Did you feel inferior to your child when you interact with him/her? [due to the impact of illness and treatment]), item 20 (Did you worry about child rearing? [due to the impact of illness and treatment]), and item 21 (Do you worry about pregnancy or delivery? [due to the impact of illness and treatment]), the calculation was based on the score of each item. Each item was scored on a 5-point scale, where 1 was the worst response and 5 was the best. (NCT02134977)
Timeframe: Week 12
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Item 19 (n=574) | Item 20 (n=566) | Item 21 (n=180) | |
| Leuprorelin Acetate | 3.5 | 3.3 | 1.8 |
QOL-ACD-B is a part of QOL-ACD (using questionnaire items 1 to 18). For questionnaire item 19 (Did you feel inferior to your child when you interact with him/her? [due to the impact of illness and treatment]), item 20 (Did you worry about child rearing? [due to the impact of illness and treatment]), and item 21 (Do you worry about pregnancy or delivery? [due to the impact of illness and treatment]), the calculation was based on the score of each item. Each item was scored on a 5-point scale, where 1 was the worst response and 5 was the best. (NCT02134977)
Timeframe: Week 48
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Item 19 (n=443) | Item 20 (n=441) | Item 21 (n=129) | |
| Leuprorelin Acetate | 3.5 | 3.2 | 1.7 |
Adverse drug reactions are defined as adverse events (AE) which are in the investigator's opinion of causal relationship to the study treatment. AE are defined as any unfavorable and unintended signs, symptoms or diseases temporally associated with the use of a medicinal product reported from the first dose of study drug to the last dose of study drug. (NCT02154139)
Timeframe: Baseline up to 96 weeks
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 128 |
Serious adverse drug reactions are defined as serious adverse events (SAE) which are in the investigator's opinion of causal relationship to the study treatment. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. The event occurred was breast cancer female (NCT02154139)
Timeframe: Baseline up to 96 weeks
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 1 |
Progression-free survival (PFS) was defined as the time from the first day of study treatment to documented disease progression or death on study (ie, death from any cause within 30 days of the last dose of study drug), whichever occurred first. Disease progression was at least a 20% increase in the sum of the longest diameter of target lesions, taking as reference the smallest sum longest diameter recorded since the treatment started or the appearance of 1 or more new lesions or the appearance of 1 or more new lesions and/or unequivocal progression of existing non-target lesions. For patients who experienced no disease progression and did not die while on study, data were censored at the date of the last tumor assessment. Kaplan-Meier methodology was used to estimate PFS. (NCT02154139)
Timeframe: Baseline up to 96 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Leuprorelin Acetate | 49.68 |
Recurrence-free survival was determined in participants who were treated with the drug as adjuvant therapy, and tabulated, based on the date recurrence is confirmed, the presence or absence of recurrence, continued survival or death, and the date of death. (NCT02154139)
Timeframe: Baseline up to 96 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Leuprorelin Acetate | 95.37 |
Best overall response for a participant is the best observed post-baseline disease response as per Response Evaluation Criteria in Solid Tumors (RECIST) 1.0 criteria. Objective response was defined as a complete response (CR) or partial response (PR) determined on 2 consecutive occasions greater than or equal to (>=) 4 weeks apart, using Response Evaluation Criteria in Solid Tumors (RECIST). CR: The disappearance of all target lesions and all non-target lesions, normalization of tumor marker level, and no new lesions. PR: Disappearance of all target lesions and persistence of >= 1 non-target lesions and/or the maintenance of tumor marker level above the normal limits, or, at least a 30 percent (%) decrease in the sum of the longest diameter of target lesions, and no new lesions or unequivocal progression of existing non-target lesions. (NCT02154139)
Timeframe: Week 24, 48,96
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| Week 24 | Week 48 | Week 96 | |
| Leuprorelin Acetate | 10.34 | 12.00 | 15.00 |
PFS was defined as the time from the first day of study treatment to documented disease progression or death on study. For participants who experienced no disease progression and did not die while on study, data were censored at the date of the last tumor assessment. Kaplan-Meier methodology was used to estimate PFS. TNM classification based on tumor size, if cancer cells had spread to nearby lymph nodes (LN), or distant metastasis. Stages included: stage 0(no evidence of cancer cells),stage 1(T1N0M0), stage IIA(T0N1M0, T1N1M0, T2N0M0), stage IIB(T2N1M0, T3N0M0), stage IIIA(T0N2M0, T1N2M0, T2N3M0, T3N1orN2M0),stage IIIb( T4 anyNM0, any TN3M0),stage IIIC(any TN3M0), stage IV(any T any NM1), where T0=early form of tumor, T1=<2 centimeter (cm), T2=2-5 cm, T3=>2 cm, T4=large sized, N0=not spread to LN, N1=spread to 1 to 3,N2=spread to 4 to 9,N3=spread >10 axillary LN, M0=no metastasis, M1= Metastasis. (NCT02167893)
Timeframe: Baseline up to 96 weeks
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Stage I (N=467) | Stage II (N=4852) | Stage III (N=1926) | Stage IV (N=2446) | |
| Leuprorelin Acetate | 94.2 | 92.0 | 86.9 | 55.4 |
Adverse drug reactions are defined as adverse events (AEs) which are in the investigator's opinion of causal relationship to the study treatment. AEs are defined as any unfavorable and unintended signs, symptoms or diseases temporally associated with the use of a medicinal product reported from the first dose of study drug to the last dose of study drug. (NCT02167893)
Timeframe: Baseline up to Week 96
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 2052 |
OS was defined as the duration from randomization to death (due to any cause). Probability of OS was reported using Kaplan-Meier method. TNM classification based on tumor size, if cancer cells had spread to nearby lymph nodes (LN), or distant metastasis. Stages included: stage 0(no evidence of cancer cells),stage 1(T1N0M0), stage IIA(T0N1M0, T1N1M0, T2N0M0), stage IIB(T2N1M0, T3N0M0), stage IIIA(T0N2M0, T1N2M0, T2N3M0, T3N1orN2M0),stage IIIb( T4 anyNM0, any TN3M0),stage IIIC(any TN3M0), stage IV(any T any NM1), where T0=early form of tumor, T1=<2 centimeter (cm), T2=2-5 cm, T3=>2 cm, T4=large sized, N0=not spread to LN, N1=spread to 1 to 3,N2=spread to 4 to 9,N3=spread >10 axillary LN, M0=no metastasis, M1= Metastasis. (NCT02167893)
Timeframe: Baseline up to 96 weeks or death (which ever occurs first)
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Stage I (N=466) | Stage II (N=4852) | Stage III (N=1927) | Stage IV (N=2443) | |
| Leuprorelin Acetate | 96.9 | 97.4 | 97.6 | 88.5 |
Serious adverse drug reactions are defined as serious adverse events (SAE) which are in the investigator's opinion of causal relationship to the study treatment. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. (NCT02167893)
Timeframe: Baseline up to Week 96
| Intervention | participants (Number) |
|---|---|
| Leuprorelin Acetate | 188 |
The absolute change in score by group from baseline up to month 12 on the International Prostate Symptom Score (IPSS) was used to measure the severity of lower urinary tract symptoms and erectile function with lower numbers indicating less change in symptoms. Seven questions with scores ranging from 1-5 are summed to create a total score. Scores of 1-7 indicate mild symptoms, scores of 8-19 indicate moderate symptoms, and scores of 20-35 indicate severe symptoms. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 2 |
| Arm II (STAND Clinic) | -2 |
The absolute change in score by group from baseline up to month 12 on the International Prostate Symptom Score (IPSS) was used to measure the severity of lower urinary tract symptoms and erectile function. The last question on the IPSS can be looked at separately from the total score as it asks the participants to rate the overall quality of life due to their existing urinary symptoms on a scale of 0-6, with lower scores indicating a better quality of life. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 0 |
| Arm II (STAND Clinic) | 0 |
"The absolute change in scores on the Patient Health Questionnaire-9 (PHQ-9) from baseline after 12 months of study participation for participants was used to measure depression symptoms with a higher number indicating a greater percentage of change in scores. The total Patient Health Questionnaire-9 (PHQ-9) score is calculated by combining the responses of the participant on questions addressing how bothered the participant has been by various problems over the past 2 weeks. Each of the 9 items is scored on a scale of 0 (Not bothered at all) to 4 (Nearly every day). A total score of 5-9='Mild Depression Symptoms, 10-4=Minor Depression, Major Depression (mild), or Dysthymia, 15-19=Major Depression, moderately severe, and >20=Major Depression.~Between group comparisons were performed using the Wilcoxon-rank-sum test." (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 0 |
| Arm II (STAND Clinic) | .50 |
The absolute change from baseline in percentage body fat after 12 months of study participation for participants in the randomized cohort was measured using a bioelectrical impedance analyzer and between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | percentage of body fat mass (Median) |
|---|---|
| Arm I (Standard of Care) | -1 |
| Arm II (STAND Clinic) | 6.8 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in percentage of body fat from the baseline to the month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | percentage of body fat (Median) |
|---|---|
| Arm I (Standard of Care) | -1 |
| Arm II (STAND Clinic) | 6.8 |
The absolute change in bone health parameters as measured by the serum 25-(OH) vitamin D level from the baseline to the month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | nanograms per milliliter (ng/mL) (Median) |
|---|---|
| Arm I (Standard of Care) | 3.60 |
| Arm II (STAND Clinic) | 8.10 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in waist circumference from the baseline to the month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | centimeters (Median) |
|---|---|
| Arm I (Standard of Care) | 5 |
| Arm II (STAND Clinic) | 1.7 |
The percentage of participants in the pilot, non-randomized cohort who completed clinic visits for Supportive Therapy in Androgen Deprivation (STAND) will be reported to assess feasibility. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Non-Randomized Pilot Cohort | 62.5 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in systolic and diastolic blood pressure from the baseline to month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | mmHg (Median) | |
|---|---|---|
| Systolic Blood Pressure | Diastolic Blood Pressure | |
| Arm I (Standard of Care) | 10 | 2 |
| Arm II (STAND Clinic) | 9 | -3 |
The absolute change in bone density t-scores from the baseline to the month 12 assessment for participants in the randomized cohort was measured using bone density at the lumbar spine, bone density at the femoral neck, and bone density at the total hip. A T-score of -1.0 or above is normal bone density. A T-score between -1.0 and -2.5 indicates low bone density or osteopenia. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | t-score (Median) | ||
|---|---|---|---|
| Bone density at the lumbar spine | Bone density at the femoral neck | Bone density of total hip | |
| Arm I (Standard of Care) | -2.0 | -0.25 | -0.20 |
| Arm II (STAND Clinic) | -0.40 | -0.20 | -0.10 |
The EPIC-26 was measured at baseline and month 12 to determine the impact of quality of life issues across 5 prostate cancer specific domains: Urinary incontinence, Urinary irritation, Bowel function, Sexual function, and Hormonal function and overall total quality of life. Response options for each EPIC item form a Likert scale, and the raw score of each item is then transformed linearly to a 0-100 scale. Multiple items are combined and then averaged to form the domain scores and total score at each time point also ranging from 0-100, with higher scores representing better health related quality of life (HRQOL). Between group comparisons were performed using the Wilcoxon-rank-sum test (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) | |||||
|---|---|---|---|---|---|---|
| Total | Urinary incontinence | Urinary irritation | Bowel function | Sexual function | Hormonal Function | |
| Arm I (Standard of Care) | -4.91 | 0 | -5.00 | 0 | -12.50 | 0 |
| Arm II (STAND Clinic) | -3.85 | 0 | 5.00 | -4.17 | -2.08 | -17.50 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in fasting lipids which includes total cholesterol, low density lipoprotein, High density lipoprotein, and triglycerides levels from the baseline to the month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | milligram per deciliter (mg/dL) (Median) | |||
|---|---|---|---|---|
| Total Cholesterol | Low density lipoprotein | High density lipoprotein | Triglycerides | |
| Arm I (Standard of Care) | 4 | -4 | 5 | 19 |
| Arm II (STAND Clinic) | -1 | -4 | 7 | -3 |
Metabolic impact for participants from baseline to 12 months was measured using an exercise pattern questionnaire. The questionnaire measured self-reported average total time per week over the past year the participant participated in various physical activities such as walking, tennis, yoga, swimming, etc. Twelve response options for each activity are as follows: None, 1-4 minutes (min), 5-19 min, 20-39 min, 40-89 min, 1.5 hours, 2-3 hours, 4-6 hours, 7-10 hours, 11-20 hours, 21-30 hours, 31-40 hours, 40+ hours. The amount of time per week spent on each activity was converted to a hourly scale and the absolute change between baseline and month 12 times were calculated for each participant. The median absolute change in hours per week were compared for each of the 6 activity categories: non-vigorous, moderate, moderate-vigorous, vigorous, and total physical activity and total moderate and vigorous activity combined. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | hours per week (Median) | ||||
|---|---|---|---|---|---|
| Non-vigorous physical activity | Moderate physical activity | Vigorous physical activity | Total physical activity | Total Moderate-Vigorous physical activity (MVPA) | |
| Arm I (Standard of Care) | -0.62 | 0.00 | -0.20 | -.30 | -0.30 |
| Arm II (STAND Clinic) | -1.03 | 0.00 | -0.02 | -.90 | -0.08 |
"The absolute change in Lee Fatigue Scale from baseline to month 12 was used to measure the impact of Fatigue on a participants quality of life. The scale consists of 18 items relating to the subjective experience of fatigue. Each item asks respondents to place an X representing how they currently feel, along a visual analogue line that extends between two extremes (e.g., from not at all tired to extremely tired). Each line is 100 mm in length - thus, scores fall between 0 and 100. The instrument also possesses two subscales: fatigue (items 1-5 and 11-18) and energy (items 6-10). The fatigue subscale score is calculated as the mean of the 13 fatigue items, and the energy subscale score is the mean of the 5 energy items. Higher scores on the fatigue subscale represent greater fatigue severity, and higher scores on the energy subscale indicate higher levels of energy. Between group comparisons were performed using the Wilcoxon-rank-sum test." (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) | |
|---|---|---|
| Fatigue Scale | Energy Scale | |
| Arm I (Standard of Care) | 5.68 | -0.10 |
| Arm II (STAND Clinic) | 3.15 | 1.30 |
The SF-12 is a 12-item questionnaire used to assess generic health outcomes from the patient's perspective. The SF-12 consists of a subset of 12 items from the SF-36® Health Survey (SF-36) and measures two composite outcomes assessing mental health composite score (MCS) and physical health composite scores (PCS). The PCS & MCS are computed using the scores of twelve questions and range from 0 to 100, where a zero score indicates the lowest level of health measured by the scales and 100 indicates the highest level of health. The absolute change in item score by group from baseline up to 12 months was used to assess the quality of life/psychosocial impact on the patients with a larger scores indicating a greater degree of change on physical and mental health. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) | |
|---|---|---|
| Mental Composite Score | Physical Composite Score | |
| Arm I (Standard of Care) | 4.81 | -2.90 |
| Arm II (STAND Clinic) | -2.37 | -1.60 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in percentage hemoglobin A1c from the baseline to the month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | percentage (Median) |
|---|---|
| Arm I (Standard of Care) | -0.1 |
| Arm II (STAND Clinic) | -0.1 |
The AFI measures a participants perceived effectiveness in functioning at time of assessment. Each of the 16 items consists of a 100 mm horizontal line anchored with opposite phrases from not at all (0 mm) to extremely well or a great deal (100 mm). Subjects are asked to place a mark on the line that best describes functioning in relation to specific activity. Scores for each item are determined by measuring distance from lower end of scale in millimeters. The total score on the instrument is computed by obtaining an average of 16 scales. The absolute change in score by group from baseline up to month 12 in Attention Function Index was used to measure perceived effectiveness in common activities requiring attention and working memory in daily life with a higher number indicating a greater absolute change in scores. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 2.31 |
| Arm II (STAND Clinic) | -4 |
"Metabolic impact for participants in each group from baseline to 12 months was measured by using an ambulatory accelerometer worn by participants around their waist for 7 consecutive days. Participants were required at least 3 days of valid wear time, defined as >= 10 hours of wear per day. The accelerometer measured movement intensity and recorded vertical acceleration as counts, providing an indication of the intensity of physical activity associated with locomotion. Non-wear time was identified using Troiano 2007 default settings in the ActiLife v6.13.3 software. The amount of time participants were engaged in moderate to vigorous physical activities (MVPA) was measured by accelerometer as counts per minute (moderate activity = 2020-5998 counts per minute, and vigorous activity = 5999 or more counts per minute). Counts are then transformed into minutes per day with a total range of 0-1440 minutes. The median absolute change in average MVPA was compared between the two groups." (NCT02168062)
Timeframe: Up to 12 months
| Intervention | minutes per day (Median) |
|---|---|
| Arm I (Standard of Care) | -18.40 |
| Arm II (STAND Clinic) | -2.36 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in body weight from the baseline to month 12 assessment. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | kilograms (Median) |
|---|---|
| Arm I (Standard of Care) | 0.8 |
| Arm II (STAND Clinic) | 2.6 |
The absolute change in Hot Flash Related Daily Interference Scale from baseline to month 12 was used to measure the impact of occurrence of hot flashes on daily activities with higher numbers indicating a greater change in the interference of hot flashes with participant's quality of life. The HFRDIS is a 10-item scale measuring the degree hot flashes interfere with nine daily activities; the tenth item measures the degree hot flashes interfere with overall quality of life. The HFRDIS was developed to include daily life activities specific to impact of hot flashes. Participants rate degree to which hot flashes have interfered with each item during previous week using a 0 (do not interfere) to 10 (completely interfere) point scale, with total score ranging from 0-100. Higher scores indicate higher interference and thus, greater impact on quality of life. Women without hot flashes are asked to mark 0 for each item. Group comparisons performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 13 |
| Arm II (STAND Clinic) | 4.5 |
Metabolic and cardiac impact for participants in the randomized cohort was measured by calculating the absolute change in insulin resistance scores from the baseline to the month 12 assessment. Insulin resistance scores were calculated using the Homeostatic Model Assessment of Insulin Resistance (HOMA-IR). This calculation marks for both the presence and extent of any insulin resistance that participants might currently express. The HOMA-IR is an assessment using insulin and glucose lab values to generate an insulin resistance score. A healthy score range is 1.0 (0.5-1.4). A score of less than 1.0 means you are insulin-sensitive which is optimal. A score above 1.9 indicates early insulin resistance. A score above 2.9 indicates significant insulin resistance. Between group comparisons were performed using the Wilcoxon-rank-sum test. (NCT02168062)
Timeframe: Up to 12 months
| Intervention | score on a scale (Median) |
|---|---|
| Arm I (Standard of Care) | 0 |
| Arm II (STAND Clinic) | -0.5 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The percentage of days with pain >=4 within a 28-day window was calculated as 100 divided by the number of non-missing days within that 28-day window multiplied by the number of days within that window where Item 1 of the ESD was >=4. Here, number of subjects 'n' signifies evaluable subjects for the respective category. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), Cycle 1 (Treatment 1), Cycle 2 (Treatment 2), and Cycle 3 (Treatment 3)
| Intervention | percentage of days (Mean) | ||
|---|---|---|---|
| Change at Treatment 1 | Change at Treatment 2 | Change at Treatment 3 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | -15.1947 | -33.2423 | -35.1119 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | -15.4147 | -26.8462 | -27.4770 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | -15.1334 | -26.4468 | -32.2600 |
| LNG 40 mcg IVR + Placebo Injection | -12.8228 | -22.4950 | -23.5498 |
| Placebo IVR + Leuprorelin Injection | -21.4331 | -37.7330 | -53.4266 |
| Placebo IVR + Placebo Injection | -14.5323 | -30.9527 | -33.3421 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The percentage of days with pain >=7 within a 28-day window was calculated as 100 divided by the number of non-missing days within that 28-day window multiplied by the number of days within that 28-day window where item 1 of the ESD was >=7. Here, number of subjects 'n' signifies evaluable subjects for the respective category. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), Cycle 1 (Treatment 1), Cycle 2 (Treatment 2), and Cycle 3 (Treatment 3)
| Intervention | percentage of days (Mean) | ||
|---|---|---|---|
| Change at Treatment 1 | Change at Treatment 2 | Change at Treatment 3 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | -13.3722 | -22.3713 | -22.9682 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | -12.5862 | -17.2826 | -20.8529 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | -15.0341 | -20.6791 | -25.3052 |
| LNG 40 mcg IVR + Placebo Injection | -13.6756 | -24.1404 | -26.4197 |
| Placebo IVR + Leuprorelin Injection | -19.8898 | -36.3540 | -39.9516 |
| Placebo IVR + Placebo Injection | -16.0105 | -26.9979 | -28.4273 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The percentage of days with pain >=4 within a 28-day window was calculated as 100 divided by the number of non-missing days within that 28-day window multiplied by the number of days within that window where Item 1 of the ESD was >=4. Here, number of subjects 'n' signifies evaluable subjects for the respective category. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), Cycle 1 (Treatment 1), Cycle 2 (Treatment 2), and Cycle 3 (Treatment 3)
| Intervention | percentage of days (Mean) | ||
|---|---|---|---|
| Treatment 1 | Treatment 2 | Treatment 3 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | 70.6504 | 52.6028 | 50.7332 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | 69.3092 | 57.8777 | 57.0171 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | 73.8956 | 62.5822 | 56.7691 |
| LNG 40 mcg IVR + Placebo Injection | 71.8037 | 61.8199 | 60.2902 |
| Placebo IVR + Leuprorelin Injection | 70.2066 | 54.0965 | 38.6986 |
| Placebo IVR + Placebo Injection | 65.9074 | 49.487 | 47.0976 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The percentage of days with pain >=7 within a 28-day window was calculated as 100 divided by the number of non-missing days within that 28-day window multiplied by the number of days within that 28-day window where item 1 of the ESD was >=7. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), Cycle 1 (Treatment 1), Cycle 2 (Treatment 2), and Cycle 3 (Treatment 3)
| Intervention | percentage of days (Mean) | ||
|---|---|---|---|
| Treatment 1 | Treatment 2 | Treatment 3 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | 23.9322 | 14.9331 | 14.3362 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | 27.5659 | 22.8695 | 19.9332 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | 40.0813 | 34.4364 | 29.8103 |
| LNG 40 mcg IVR + Placebo Injection | 35.6034 | 25.6257 | 23.1293 |
| Placebo IVR + Leuprorelin Injection | 28.2015 | 12.1320 | 8.5351 |
| Placebo IVR + Placebo Injection | 25.1742 | 14.1869 | 12.7574 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The mean pain of the 7 days with worst EAPP within a 28-day window was calculated as the sum of ESD item 1 on 7 days with worst EAPP within that 28-day window divided by 7. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), first cycle (Treatment 1) (Day 1-28), second cycle (Treatment 2) (Day 29-56)
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Change at Treatment 1 | Change at Treatment 2 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | -1.0000 | -1.9959 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | -0.6849 | -1.5126 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | -1.1463 | -2.1224 |
| LNG 40 mcg IVR + Placebo Injection | -0.7582 | -1.6447 |
| Placebo IVR + Leuprorelin Injection | -1.2071 | -2.8607 |
| Placebo IVR + Placebo Injection | -0.9048 | -1.8022 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, subjects were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The mean pain within a 28-day window was calculated as the sum of ESD item 1 within that 28-day window divided by the number with non-missing days within that 28-day window. Here, number of subjects 'n' signifies evaluable subjects for the respective category. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), first cycle (Treatment 1) (Day 1-28), second cycle (Treatment 2) (Day 29-56), and third cycle (Treatment 3) (last 28 days of the treatment period, Day 57-84)
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Baseline | Change at Treatment 1 | Change at Treatment 2 | Change at Treatment 3 | |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | 5.7128 | -1.1257 | -1.9615 | -2.1268 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | 5.7409 | -0.9009 | -1.5068 | -1.6411 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | 6.3694 | -1.0931 | -1.7349 | -2.0112 |
| LNG 40 mcg IVR + Placebo Injection | 6.0938 | -0.8472 | -1.5774 | -1.8001 |
| Placebo IVR + Leuprorelin Injection | 6.3962 | -1.5315 | -2.6855 | -3.502 |
| Placebo IVR + Placebo Injection | 5.6399 | -0.9777 | -1.8994 | -2.2228 |
Pain intensity was assessed on 11-point (0-10) NRS by question 1. In question 1, participants were asked to rate the pain in the target area during the past 24 hours, where 0= no pain and 10= worst imaginable pain and responses were recorded in ESD. The mean pain of the 7 days with worst EAPP within a 28-day window was calculated as the sum of ESD item 1 on 7 days with worst EAPP within that 28-day window divided by 7. (NCT02203331)
Timeframe: Baseline (last 28 days before randomization), end of treatment (Treatment 3) (last 28 days of the treatment period, Day 57-84)
| Intervention | units on a scale (Mean) |
|---|---|
| LNG 40 mcg IVR + Placebo Injection | -1.8974 |
| ATZ 300 mcg / LNG 40 mcg IVR + Placebo Injection | -1.6061 |
| ATZ 600 mcg / LNG 40 mcg IVR + Placebo Injection | -2.4014 |
| ATZ 1050 mcg / LNG 40 mcg IVR + Placebo Injection | -2.2653 |
| Placebo IVR + Leuprorelin Injection | -3.7679 |
| Placebo IVR + Placebo Injection | -2.293 |
The PD effects of leuprolide were assessed by measuring serum testosterone concentrations during the trial. The following PD variable was analyzed: The profiles of testosterone concentration (ng/dL) following injections of the IMP. Blood samples for analyses of serum testosterone concentrations were collected at Screening and on Days 0 to 126. (NCT02212197)
Timeframe: Days 0-126
| Intervention | ng/dL (Median) | ||||
|---|---|---|---|---|---|
| Day 0 (predose) | Day 28 (predose) | Day 56 (predose) | Day 84 | Day 126 | |
| CAM2032 3.75 mg | 443 | 20.9 | 14.6 | 14.8 | 423 |
| CAM2032 7.5 mg | 321 | 24.5 | 13.8 | 10.6 | 278 |
| Eligard 7.5 mg | 350 | 18.1 | 12 | 12.4 | 85.8 |
Blood samples for analysis of serum leuprolide concentrations were collected at pre-determined time points throughout the trial (with full PK profiles after Dose 1 and Dose 3). The PK parameter, Cmax was derived for Doses 1 and 3 of the investigational medicinal product (IMP). (NCT02212197)
Timeframe: 84 days
| Intervention | ng/mL (Geometric Mean) | |
|---|---|---|
| Dose 1 | Dose 3 | |
| CAM2032 3.75 mg | 6.14 | 5.36 |
| CAM2032 7.5 mg | 9.66 | 11.3 |
| Eligard 7.5 mg | 13.6 | 12.1 |
The PD effects of leuprolide were assessed by measuring serum PSA concentrations during the trial. The following PD variable was analyzed: PSA (ng/mL) response to IMP. Blood samples for analyses of plasma PSA concentrations were collected at Screening and on Days 0 to 126. (NCT02212197)
Timeframe: Days 0-126
| Intervention | ng/mL (Median) | ||||
|---|---|---|---|---|---|
| Day 0 (predose) | Day 28 (predose) | Day 56 (predose) | Day 84 | Day 126 | |
| CAM2032 3.75 mg | 14.9 | 9 | 3.6 | 2.3 | 4.7 |
| CAM2032 7.5 mg | 18.8 | 8.3 | 5.8 | 2.6 | 3.1 |
| Eligard 7.5 mg | 14.6 | 4.6 | 2.1 | 1.6 | 1.6 |
Blood samples for analysis of serum leuprolide concentrations were collected at pre-determined time points throughout the trial (with full PK profiles after Dose 1 and Dose 3). The PK parameter, AUCtau was derived for Doses 1 and 3 of the IMP. (NCT02212197)
Timeframe: Days 0-28 and Days 56-84 (0-672 hours after Doses 1 and 3)
| Intervention | h*ng/mL (Geometric Mean) | |
|---|---|---|
| Dose 1 | Dose 3 | |
| CAM2032 3.75 mg | 329 | 343 |
| CAM2032 7.5 mg | 622 | 757 |
| Eligard 7.5 mg | 397 | 460 |
Blood samples for analysis of serum leuprolide concentrations were collected at pre-determined time points throughout the trial (with full PK profiles after Dose 1 and Dose 3). The PK parameter, t1/2 was derived for Doses 1 and 3 of the IMP. (NCT02212197)
Timeframe: Days 0-28 and Days 56-84
| Intervention | hour (Mean) | |
|---|---|---|
| Dose 1 | Dose 3 | |
| CAM2032 3.75 mg | 205 | 299 |
| CAM2032 7.5 mg | 231 | 434 |
| Eligard 7.5 mg | 743 | 378 |
The pharmacodynamic (PD) effects of leuprolide were assessed by measuring serum testosterone during the trial. Time to testosterone recovery after last dose of the IMP. Blood samples for analyses of serum testosterone concentrations were collected at Screening and on Days 0 to 126. (NCT02212197)
Timeframe: Days 56-126
| Intervention | days (Mean) |
|---|---|
| CAM2032 3.75 mg | 46.2 |
| CAM2032 7.5 mg | 52.3 |
| Eligard 7.5 mg | 65 |
The percentage of subjects with a serum testosterone concentration suppressed to castrate levels (≤ 50 ng/dL) following the first injection of LMIS 50 mg from Day 28 through Day 336 (remaining duration of the study). (NCT02234115)
Timeframe: baseline to 28 days, 28 days to 336 days
| Intervention | percentage of participants (Mean) |
|---|---|
| Leuprolide Mesylate 50mg | 97.0 |
Safety analysis was based on the safety information from the laboratory evaluations, AEs, and SAEs. (NCT02234115)
Timeframe: 336 days
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| TEAE | Drug-related AEs | SAE | |
| Leuprolide Mesylate 50mg | 114 | 85 | 20 |
RCB was analyzed using radical prostatectomy (RP) tissue. The largest area of tumor was measured by ruler and the longest tumor dimension in this area was used as the dimension for calculation. (NCT02268175)
Timeframe: after RP approximately 24 weeks from study entry
| Intervention | cm (Median) |
|---|---|
| ARM 1 | 0.03 |
| ARM 2 | 0.05 |
pCR is defined as the absence of morphologically identifiable carcinoma in the radical prostatectomy (RP) specimen. MRD is defined as the largest cross-sectional dimension of residual tumor measuring NCT02268175)
Timeframe: after RP approximately 24 weeks from study entry
| Intervention | percentage of participants (Number) |
|---|---|
| ARM 1 | 30 |
| ARM 2 | 16 |
pCR is defined as the absence of morphologically identifiable carcinoma in the radical prostatectomy (RP) specimen. (NCT02268175)
Timeframe: after RP approximately 24 weeks from study entry
| Intervention | Participants (Count of Participants) |
|---|---|
| ARM 1 | 5 |
| ARM 2 | 2 |
PSA nadir is the lowest PSA level recorded during neoadjuvant therapy. (NCT02268175)
Timeframe: PSA was assessed at baseline and every cycle during neoadjuvant therapy (up to 24 weeks).
| Intervention | ng/mL (Median) |
|---|---|
| ARM 1 | 0.03 |
| ARM 2 | 0.02 |
"The FACT-P is the Functional Assessment of Cancer Therapy - Prostate and measures physical/emotional quality of life in prostate cancer patients.~NUMBER OF ITEMS:39 PATIENT POPULATION:Prostate cancer patients 18 years and older RECALL PERIOD:Past 7 days RESPONSE SCALE:5 point Likert-type scale~SUBSCALE DOMAINS:~Physical Well-Being (PWB), Social/Family Well-Being (SWB), Emotional Well-Being (EWB), Functional Well-Being (FWB), Prostate Cancer Subscale (PCS)~SCORING:~Scores range from 0-158. In general, the higher the score, the better the quality of life.~Sexual Health in Men (SHIM). 5 item measure of erectile function. Total score is 1-25 with a higher score indicating better sexual health. Scores: no ED (SHIM total score, 22-25), mild (17-21), mild to moderate (12-16), moderate (8-11), and severe ED (1-7)." (NCT02278185)
Timeframe: Baseline to up to 7 months
| Intervention | score on a scale (Mean) | |
|---|---|---|
| SHIM | FACT-P | |
| Arm I (Enzalutamide) | -3.71 | -4.5 |
| Arm II (ADT) | -3.4 | -1.93 |
Log rank test will be used to compare the distributions of above variables between the group treated with enzalutamide to the group on standard ADT. (NCT02278185)
Timeframe: Time from randomization to the earliest objective evidence of radiographic progression as defined per protocol, assessed up to 30 days after the last dose of study drug
| Intervention | Months (Mean) |
|---|---|
| Arm I (Enzalutamide) | NA |
| Arm II (ADT) | 11.474 |
PSA progression as defined by an increase in >= 50% from nadir and an absolute increase of at least 2 ng/mL above the nadir, occurring at least 12 weeks after start of therapy that is confirmed by two consecutive increases taken at least 2 weeks apart. Log rank test will be used to compare the distributions of above variables between the group treated with enzalutamide to the group on standard ADT. (NCT02278185)
Timeframe: Time from randomization to the earliest objective evidence of PSA progression as defined per protocol, assessed up to 30 days after the last dose of study drug
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm I (Enzalutamide) | 0 |
| Arm II (ADT) | 1 |
Metabolic syndrome will be assessed at the beginning of each course and defined by the presence of 3 of the following five traits: abdominal obesity, defined as a waist circumference > 102 cm (> 40 in); serum triglycerides >= 150 mg/dL (1.7 mmol/L) or drug treatment for elevated triglycerides; serum HDL cholesterol < 40 mg/dL (1 mmol/L) or drug treatment for low HDL; blood pressure >= 130/>= 85 mmHg or drug treatment for elevated blood pressure; and FPG >= 100 mg/dL (5.6 mmol/L) or drug treatment for elevated blood glucose. (NCT02278185)
Timeframe: Within the first 6 months of therapy
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm I (Enzalutamide) | 4 |
| Arm II (ADT) | 0 |
Metabolic syndrome will be assessed at the beginning of each course and defined by the presence of 3 of the following five traits: abdominal obesity, defined as a waist circumference > 102 cm (> 40 in); serum triglycerides >= 150 mg/dL (1.7 mmol/L) or drug treatment for elevated triglycerides; serum high density lipoprotein (HDL) cholesterol < 40 mg/dL (1 mmol/L) or drug treatment for low HDL; blood pressure >= 130/>= 85 mmHg or drug treatment for elevated blood pressure; and fasting plasma glucose (FPG) >= 100 mg/dL (5.6 mmol/L) or drug treatment for elevated blood glucose. (NCT02278185)
Timeframe: Within the first 12 months of therapy
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm I (Enzalutamide) | 5 |
| Arm II (ADT) | 3 |
The incidence of adverse events has been reported in the adverse events log for clinicaltrials.gov (NCT02278185)
Timeframe: Up to 30 days after the last dose of study drug
| Intervention | Participants (Count of Participants) |
|---|---|
| Enzalutamide | 10 |
| Androgen Deprivation Therapy | 9 |
The Short SPPB incorporates 3 validated portions to assess a patient's balance and mobility. SPPB scores range from zero to 12 possible points. SPPB score of 3-9 points in persons with no mobility disability indicates frailty; SPPB score of 10 or greater for persons with no sarcopenia and no mobility disability indicates robustness. The higher the score, the better the physical function. Will be measured as a continuous outcome. (NCT02278185)
Timeframe: Difference between baseline and 12 months.
| Intervention | score on a scale (Mean) |
|---|---|
| Arm I (Enzalutamide) | 10.58 |
| Arm II (ADT) | 10.94 |
Mean change in available samples from baseline to 12 months, presented in mg/dL (NCT02278185)
Timeframe: Difference between baseline and 12 months.
| Intervention | mg/dL (Mean) |
|---|---|
| Arm I (Enzalutamide) | 0.87 |
| Arm II (ADT) | 6.42 |
Will be assessed for each treatment group. Measurements will be taken at day 1 of each course. A paired t-test will test within an arm as to whether the change from baseline to 12 months is significantly different from zero. (NCT02278185)
Timeframe: Baseline and month 12
| Intervention | microgram/L (Mean) |
|---|---|
| Arm I (Enzalutamide) | -18.55 |
| Arm II (ADT) | -58.14 |
Will be assessed for each treatment group. Measurements will be taken at day 1 of each course. A paired t-test within an arm as to whether the change from baseline to 12 months is significantly different from zero. N-Telopeptide units - nM Bone Collagen Equivalent (BCE). (NCT02278185)
Timeframe: Baseline and 12 months
| Intervention | nM BCE (Mean) |
|---|---|
| Arm I (Enzalutamide) | -3.05 |
| Arm II (ADT) | 1.73 |
"We will measure bone density via a DXA scanner, Left Femur and Right femur T scores will be added to a composite score. A paired t-test will test within an arm as to whether the change from baseline to twelve months is significantly different from zero.~The T-score is the standard deviation of how much bone density differs from the bone mass of an average healthy 30 year old. A score of 0 indicates no deviation from average. The following ranges are used:~T-score of -1.0 or above = normal bone density~T-score between -1.0 and -2.5 = low bone density, or osteopenia~T-score of -2.5 or lower = osteoporosis" (NCT02278185)
Timeframe: Baseline to 12 months
| Intervention | score on a scale (Mean) |
|---|---|
| Enzalutamide | -0.23 |
| Androgen Deprivation Therapy | 0 |
Tanner assessment score was used to document the stage of development of puberty through the assessment of secondary sexual characteristics. Female pubertal development staged by pubic hair development and breast size; male pubertal development staged by size of the genitalia and development of pubic hair. Rated in 5 stages: stage 1 (no development) to 5 (adult-like development in quantity and size). Regression or no progression was defined as negative change (improvement) or no change in Tanner score at Week 96 compared to baseline. (NCT02427958)
Timeframe: Week 96
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Female | Male | |
| Leuprorelin | 83.5 | 0 |
(NCT02427958)
Timeframe: Day 1 up to Week 100
| Intervention | participants (Number) |
|---|---|
| Leuprorelin | 252 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | |||
|---|---|---|---|---|
| Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | -0.5 | -0.5 | -0.5 | -1.0 |
Bone Age Ratio to Chronological Age at Time of Measurement is bone age/age at bone age assessment. (NCT02452931)
Timeframe: Week 24 and Week 48
| Intervention | percent change (Mean) | |||
|---|---|---|---|---|
| Visit 5, Week 24 | End of Treatment, Week 48 | Minimum Post-baseline Value | Maximum Post-baseline Value | |
| Assigned Intervention | -3.25 | -4.90 | -6.15 | -1.89 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Baseline, Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | 3.0 | 2.5 | 2.5 | 2.5 | 2.0 |
Changes in ratio of LH/FSH at each time point from Screening to End of Study (NCT02452931)
Timeframe: Screening (Pre&Post GnRHa Stim Test), Baseline (0,1,4,6 hours Post-Injection), Week 4, Week 12 (Pre&Post GnRHa Stim Test), Week 20, Week 24 (Pre&Post GnRHa Stim Test), Week 36 (Pre&Post GnRHa Stim Test), Week 44, and Week 48 (Pre&Post GnRHa Stim Test)
| Intervention | Ratio (Mean) | ||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Screening: Pre GnRHa Stimulation Test | Screening: Post GnRHa Stimulation Test | Baseline | Baseline: 1 hr Post Inj | Baseline: 1 hr Post Inj: Change from Baseline | Baseline: 4 hr Post Inj | Baseline: 4 hr Post Inj: Change from Baseline | Baseline: 6 hr Post Inj | Baseline: 6 hr Post Inj: Change from Baseline | Week 4 | Week 4: Change from Baseline | Week 12: Pre GnRHa Stim Test | Week 12: Pre GnRHa Stim Test: Change from Baseline | Week 12: Post GnRHa Stim Test | Week12: Post GnRHa Stim Test: Change from Baseline | Week 20 | Week 20: Change from Baseline | Week 24: Pre GnRHa Stim Test | Week 24: Pre GnRHa Stim Test: Change from Baseline | Week 24: Post GnRHa Stim Test | Week24: Post GnRHa Stim Test: Change from Baseline | Week 36: Pre GnRHa Stim Test | Week 36: Pre GnRHa Stim Test: Change from Baseline | Week 36: Post GnRHa Stim Test | Week36: Post GnRHa Stim Test: Change from Baseline | Week 44 | Week 44: Change from Baseline | Week 48: Pre GnRHa Stim Test | Week 48: Pre GnRHa Stim Test: Change from Baseline | Week 48: Post GnRHa Stim Test | Week48: Post GnRHa Stim Test: Change from Baselin | |
| Assigned Intervention | 0.387 | 2.187 | 0.604 | 2.424 | 1.856 | 2.110 | 1.542 | 1.691 | 1.123 | 0.843 | 0.233 | 0.565 | -0.050 | 1.342 | 0.721 | 0.654 | 0.068 | 0.611 | 0.007 | 1.320 | 0.716 | 0.474 | -0.125 | 1.051 | 0.461 | 0.517 | -0.073 | 0.557 | -0.033 | 1.092 | 0.509 |
Height at each available measurement point. Baseline is defined as the last non-missing height measurement collected prior to or on the date of first injection. (NCT02452931)
Timeframe: Screening, Baseline, Week 4, Week 12, Week 20, Week 24, Week 36, Week 44, and Week 48
| Intervention | cm (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Screening | Baseline | Visit 2, Week 4 | Visit 3, Week 12 | Visit 4, Week 20 | Visit 5, Week 24 | Visit 6, Week 36 | Visit 7, Week 44 | End of Treatment, Week 48 | |
| Assigned Intervention | 136.17 | 136.61 | 137.32 | 138.52 | 138.87 | 139.78 | 140.99 | 141.81 | 142.37 |
The percent change from baseline in height at each available post-baseline measurement. Percent change is defined as (((change from Baseline)/(Baseline)) x 100). (NCT02452931)
Timeframe: Week 4, Week 12, Week 20, Week 24, Week 36, Week 44, and Week 48
| Intervention | Percent change (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Visit 2, Week 4 | Visit 3, Week 12 | Visit 4, Week 20 | Visit 5, Week 24 | Visit 6, Week 36 | Visit 7, Week 44 | End of Treatment, Week 48 | |
| Assigned Intervention | 0.5 | 1.4 | 1.9 | 2.3 | 3.3 | 3.9 | 4.3 |
The percentage of subjects with FSH, estradiol and testosterone suppression to prepubertal levels (FSH < 2.5 mIU/mL, estradiol < 20 pg/mL and testosterone < 28.4 ng/dL) at each available time point. (NCT02452931)
Timeframe: Week 12, Week 24, Week 36, and Week 48
| Intervention | Participants (Count of Participants) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Visit 3, Week 12 : FSH | Visit 3, Week 12 : Estradiol | Visit 3, Week 12 : Oestradiol (HS) | Visit 3, Week 12 : Testosterone | Visit 5, Week 24 : FSH | Visit 5, Week 24 : Estradiol | Visit 5, Week 24 : Oestradiol (HS) | Visit 5, Week 24 : Testosterone | Visit 6, Week 36 : FSH | Visit 6, Week 36 : Estradiol | Visit 6, Week 36 : Oestradiol (HS) | Visit 6, Week 36 : Testosterone | End of Treatment, Week 48 : FSH | End of Treatment, Week 48 : Estradiol | End of Treatment, Week 48 : Oestradiol (HS) | End of Treatment, Week 48 : Testosterone | |
| Assigned Intervention | 37 | 58 | 56 | 2 | 41 | 59 | 58 | 2 | 26 | 57 | 56 | 2 | 32 | 56 | 55 | 1 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Baseline, Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | 2.3 | 2.4 | 2.5 | 2.3 | 2.4 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | |||
|---|---|---|---|---|
| Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | 0.1 | 0.1 | 0.1 | 0.1 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Baseline, Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | 3.2 | 2.7 | 2.6 | 2.5 | 2.4 |
Sexual development (physical signs) in puberty were assessed by Tanner staging, a system developed by Marshall and Tanner to categorize pubertal maturation. Tanner stages are commonly used to categorize pubertal maturation in terms of sequence, timing and tempo. Tanner Stages: the minimum is Stage 1 = pre-pubertal physical characteristics and the maximum is Stage 5 = fully matured (adult) physical characteristics. (NCT02452931)
Timeframe: Week 12, Week 24, Week 36, and Week 48
| Intervention | Score on a scale (Mean) | |||
|---|---|---|---|---|
| Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | -0.5 | -0.6 | -0.6 | -0.7 |
GnRH Antagonist Evaluation occurred for the two week period following each treatment and at each visit to assess flare symptoms. The percent of subjects who affirm (or whose parent/guardian affirms) each symptom domain in the global interview. (NCT02452931)
Timeframe: Week 2, Week 4, Week 12, Week 20, Week 24, Week 26, Week 36, Week 44, and Week 48
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Telephone Contact #1, Week 272175496 | Visit 2, Week 472175496 | Visit 3, Week 1272175496 | Visit 4, Week 2072175496 | Visit 5, Week 2472175496 | Telephone Contact #2, Week 2672175496 | Visit 6, Week 3672175496 | Visit 7, Week 4472175496 | End of Treatment, Week 4872175496 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Any GnRH Antagonist Conditions Reported? | Flare or hot flashes | Injection site reactions | Burning/Stinging | Pain | Bruising | Redness | Difficulty in urination | Bone Pain | Aggravation of weakness or other muscle symptoms | Onset of Allergic reactions | No GnRH Antagonist conditions reported? | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 15 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 11 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 9 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 0 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 5 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 48 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 55 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 16 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 51 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 53 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assigned Intervention | 57 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Changes in height velocity (growth rate) at all study timepoints after Screening to end of study. Growth velocity is defined for each visit as change from baseline / [(number of weeks since baseline)/52]. Week 48: Change from Week 24 growth velocity is defined as change from week 24 to week 48 / [(number of weeks since week 24)/52]. (NCT02452931)
Timeframe: Week 4, Week 12, Week 20, Week 24, Week 36, Week 44, and Week 48
| Intervention | cm/year (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Visit 2, Week 4 | Visit 3, Week 12 | Visit 4, Week 20 | Visit 5, Week 24 | Visit 6, Week 36 | Visit 7, Week 44 | End of Treatment, Week 48 | End of Treatment, Week 48: Change from Week 24 | |
| Assigned Intervention | 8.89 | 8.30 | 6.66 | 6.90 | 6.48 | 6.23 | 6.37 | 5.79 |
Percentage of subjects with suppressed serum LH concentrations(<4 IU/L) 30 minutes post GnRHa stimulation test at all assessed timepoints. (NCT02452931)
Timeframe: Week 12, Week 24, Week 36, and Week 48
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Visit 3, Week 12 | Visit 5, Week 24 | Visit 6, Week 36 | End of Treatment, Week 48 | |
| Assigned Intervention | 51 | 54 | 50 | 50 |
Luteinizing Hormone (LH) suppression is defined as peak-stimulated LH <4 IU/L. Peak stimulated LH refers to the maximum LH concentration measured 30 minutes after a gonadotropin-releasing hormone agonst (GnRHa) stimulation test. (NCT02452931)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Assigned Intervention | 54 |
Bone Age at each available measurement point. (NCT02452931)
Timeframe: Baseline, Week 24, and Week 48
| Intervention | years (Mean) | ||
|---|---|---|---|
| Baseline | Visit 5, Week 24 | End of Treatment, Week 48 | |
| Assigned Intervention | 11.01 | 11.30 | 11.65 |
Bone age progression at each available post-baseline measurement point. Bone age progression is defined as (((change from baseline)/(baseline)) x 100), which is percent change from baseline. (NCT02452931)
Timeframe: Week 24 and Week 48
| Intervention | percent change (Mean) | |||
|---|---|---|---|---|
| Visit 5, Week 24 | End of Treatment, Week 48 | Minimum Post-Baseline Value | Maximum Post-Baseline Value | |
| Assigned Intervention | 2.91 | 6.81 | 2.91 | 6.63 |
Bone age advancement was evaluated relative to chronological age at each given measurement point. Bone Age Ratio to Chronological Age at Start of Study is bone age/age at first injection. (NCT02452931)
Timeframe: Baseline, Week 24, and Week 48
| Intervention | Ratio (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Visit 5, Week 24 | End of Treatment, Week 48 | Minimum Post-baseline Value | Maximum Post-baseline Value | |
| Assigned Intervention | 1.38 | 1.42 | 1.47 | 1.42 | 1.47 |
Bone age advancement was evaluated relative to chronological age at each given measurement point. Percent change from baseline is: 100 x (the change from baseline value at the post-baseline visit / baseline value). (NCT02452931)
Timeframe: Week 24 and Week 48
| Intervention | percent change (Mean) | |||
|---|---|---|---|---|
| Visit 5, Week 24 | End of Treatment, Week 48 | Minimum Post-baseline Value | Maximum Post-baseline Value | |
| Assigned Intervention | 2.91 | 6.81 | 2.91 | 6.63 |
Bone Age Ratio to Chronological Age at Time of Measurement is bone age/age at bone age assessment. (NCT02452931)
Timeframe: Week 24 and Week 48
| Intervention | Ratio (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Visit 5, Week 24 | End of Treatment, Week 48 | Minimum Post-baseline Value | Maximum Post-baseline Value | |
| Assigned Intervention | 1.39 | 1.34 | 1.32 | 1.30 | 1.36 |
Defined as the time from the start of study treatment to confirmed regional or distant metastases (NCT02508636)
Timeframe: Up to 36 months
| Intervention | months (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | NA |
Local failure was defined as the time from the start of treatment to a biopsy confirmed disease recurrence. (NCT02508636)
Timeframe: Up to 36 months
| Intervention | months (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | NA |
The EQ-VAS records the patient's self-rated health on a vertical visual analogue scale, similar to a ruler, where the endpoints are labelled with 100='The best health you can imagine' on one end and 0='The worst health you can imagine' on the other, with 50 being the midpoint and participants mark an X on the scale to indicate how their health is on the day of the visit. The VAS can be used as a quantitative measure of health outcome that reflect the patient's own judgement. Changes in the EQ-VAS scores will be assessed during treatment and the overall median change in scores will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | score on a scale (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 72 |
Changes in fasting glucose levels results will be assessed during treatment and the overall median change in fasting glucose levels will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | mg/dL (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | -2.7 |
HbA1C test results are reported as a percentage. The higher the percentage, the higher your blood sugar levels over the past two to three months. Changes in HbA1c results will be assessed during treatment and the overall median change in HbA1c will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | percentage (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 0.2 |
Prostate-specific antigen (PSA) nadir >=2 ng/mL, also known as the Phoenix definition, is the definition most commonly used to establish biochemical failure (BF) after external beam radiotherapy for prostate cancer management. Time to biochemical failure is defined as the time from start of treatment to the time of change in PSA >=2 ng/mL from the nadir. (NCT02508636)
Timeframe: Up to 36 months
| Intervention | months (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 36 |
Changes in fasting lipid levels will be assessed during treatment and the overall median change in fasting lipid levels will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | mg/dL (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 0 |
Changes in fasting LDL levels will be assessed during treatment and the overall median change in fasting LDL will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | mg/dL (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 0 |
A PROMIS score of 50 is the average (or mean) score for a specific, relevant group of people under investigation. That group is the reference population. The PROMIS measures the responses use a T-score metric in which 50 is the mean of a relevant reference population and 10 is the standard deviation (SD) of that population. A score of 40 is one SD lower than the mean of the reference population and a score of 60 is one SD higher than the mean of the reference population. For PROMIS measures, higher scores equals more of the concept being measured (e.g., more Fatigue). Changes in the PROMIS fatigue scores will be assessed during treatment and the overall median change in scores will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | score on a scale (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 0 |
Changes in total cholesterol levels will be assessed during treatment and the overall median change in total cholesterol levels will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | mg/dL (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 12 |
Percentage of participants with acute, treatment-related toxicity defined as <=90 days within the completion of radiotherapy, for any treatment-related grade 3 or higher adverse events as classified by the NCI Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 (NCT02508636)
Timeframe: From start of treatment to 90 days after completion of radiotherapy, approximately 6 months total
| Intervention | percentage of participants (Number) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 36.36 |
Changes in fasting HDL levels will be assessed during treatment and the overall median change in fasting HDL will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | mg/dL (Median) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 12 |
EQ-5D is a standardized instrument for measuring generic health status. The health status is measured in terms of five dimensions (5D); mobility, self-care, usual activities, pain/discomfort, and anxiety/depression. The respondents self-rate their level of severity for each dimension by selecting one of the following responses: no problems (0), slight problems (1), mild problems (2), moderate problems (3), or severe problems (4) with a particular dimension. Lower scores indicate less issues/problems with that particular health dimension. Changes in the EQ-5D scores will be assessed during treatment and the overall median change in scores will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | score on a scale (Median) | ||||
|---|---|---|---|---|---|
| Mobility | Self-Care | Usual Activities | Pain/Discomfort | Anxiety/Depression | |
| Combination Therapy: Enzalutamide and Leuprolide | 0 | 0 | 0 | 0 | 0 |
The Expanded Prostate Cancer Index Composite (EPIC) is a comprehensive instrument designed to evaluate patient function and bother after prostate cancer treatment and assesses the disease-specific aspects of prostate cancer and its therapies and comprises four summary domains (Urinary, Bowel, Sexual and Hormonal). Response options for each EPIC item form a Likert scale, and multi-item scale scores are transformed linearly to a 0-100 scale, with higher scores representing better health related quality of life. Changes in EPIC scores will be assessed during treatment and the overall median change in scores will be reported. (NCT02508636)
Timeframe: Up to 24 months
| Intervention | score on a scale (Median) | ||||
|---|---|---|---|---|---|
| Urinary incontinence | Urinary Irritative/Obstructive | Bowel | Sexual | Hormonal | |
| Combination Therapy: Enzalutamide and Leuprolide | 6.25 | 6.25 | 0 | -44.4 | -20 |
Percentage of participants with late, treatment-related, toxicity is defined as any toxicity occurring >= 90 days from completion of radiotherapy for any grade 3 or higher treatment-related adverse events as classified by the NCI Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT02508636)
Timeframe: From 90 days after completion of radiotherapy until end of study, approximately 30 months total
| Intervention | percentage of participants (Number) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 27.27 |
The number of participants with confirmed regional or distant metastases at 24 and 36 months will be reported. (NCT02508636)
Timeframe: Up to 36 months
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Month 24 | Month 36 | |
| Combination Therapy: Enzalutamide and Leuprolide | 0 | 0 |
A PSA measurement will be obtained at 120-127 days after initiation of androgen deprivation therapy. The proportion of patients achieving a PSA-CR (PSA nadir <=0.3) at 120-127 days will be determined. (NCT02508636)
Timeframe: Up to 127 days
| Intervention | proportion of participants (Number) |
|---|---|
| Combination Therapy: Enzalutamide and Leuprolide | 0.818 |
PBAC score was used to measure volume of menstrual blood loss. Participants used sanitary products designated by sponsor and recorded the numbers of tampons or towels used, clots and flooding in patient diary. Three diagrams used which represented a lightly, moderately stained or completely saturated pad/tampon. Following scores assigned: 1) 1, 5, or 20 points for each pad; 2) 1, 5, or 10 points for each tampon; 3) 1 or 5 points for each blood clot of <1 cm/=1 cm/>1 in longest diameter; 4) 5 points for each episode of flooding. The total PBAC score (sum of points) ranges from 0 to >500. (NCT02655237)
Timeframe: For 6 weeks before the final dose of study drug (up to Week 24)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix 40 mg | 79.0 |
| Leuprorelin 1.88 mg or 3.75 mg | 92.3 |
Number of participants with TEAEs of which threshold was 5% or above in either treatment group related to weight was reported. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) |
|---|---|
| Relugolix 40 mg | 0 |
| Leuprorelin 1.88 mg or 3.75 mg | 0 |
Number of participants with TEAEs of which threshold was 5% or above in either treatment group related to ECG was reported. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) |
|---|---|
| Relugolix 40 mg | 0 |
| Leuprorelin 1.88 mg or 3.75 mg | 0 |
Number of participants with TEAEs of which threshold was 5% or above in either treatment group related to bone mineral density was reported. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) |
|---|---|
| Relugolix 40 mg | 6 |
| Leuprorelin 1.88 mg or 3.75 mg | 8 |
UFS-QOL was a 37-item self-reporting tool for evaluating QOL in participants with uterine fibroid. It includes eight symptom-related questions and 29 HRQL questions across six subscales (concern, activities, energy/mood, control, self-consciousness, sexual function). The total symptom severity score is ranging from 0 to 100. The higher scores indicate greater severity. (NCT02655237)
Timeframe: Baseline, Weeks 4, 8, 12, 16, 20, 24 and Follow-up (up to Week 28)
| Intervention | score on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Change at Week 4 | Change at Week 8 | Change at Week 12 | Change at Week 16 | Change at Week 20 | Change at Week 24 | Change at Follow-Up (up to Week 28) | |
| Leuprorelin 1.88 mg or 3.75 mg | -4.5 | -17.2 | -23.0 | -24.4 | -24.3 | -25.3 | -25.4 |
| Relugolix 40 mg | -5.5 | -19.5 | -21.0 | -21.4 | -21.9 | -22.5 | -20.6 |
UFS-QOL was a 37-item self-reporting tool for evaluating QOL in participants with uterine fibroid. It includes eight symptom-related questions and 29 HRQL questions across six subscales (concern, activities, energy/mood, control, self-consciousness, sexual function). The total HRQL score is ranging from 0 to 100. The higher scores indicate better QOL. (NCT02655237)
Timeframe: Baseline, Weeks 4, 8, 12, 16, 20, 24 and Follow-up (up to Week 28)
| Intervention | score on a scale (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Change at Week 4 | Change at Week 8 | Change at Week 12 | Change at Week 16 | Change at Week 20 | Change at Week 24 | Change at Follow-Up (up to Week 28) | |
| Leuprorelin 1.88 mg or 3.75 mg | 3.5 | 9.5 | 13.3 | 14.3 | 14.5 | 15.8 | 15.7 |
| Relugolix 40 mg | 2.4 | 8.1 | 10.4 | 10.9 | 11.5 | 12.0 | 10.9 |
Anemia-related measurements consisted of hemoglobin, which were determined at the central laboratory. (NCT02655237)
Timeframe: Baseline, Weeks 4, 8, 12, 16, 20, 24 and Follow up (up to Week 28)
| Intervention | g/dL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Change at Week 4 | Change at Week 8 | Change at Week 12 | Change at Week 16 | Change at Week 20 | Change at Week 24 | Change at Follow-Up (up to Week 28) | |
| Leuprorelin 1.88 mg or 3.75 mg | 0.60 | 1.10 | 1.31 | 1.42 | 1.58 | 1.65 | 1.75 |
| Relugolix 40 mg | 0.79 | 1.20 | 1.38 | 1.40 | 1.47 | 1.56 | 1.25 |
Vital signs included sitting blood pressure (after the participant has rested for at least 5 minutes), body temperature (oral or tympanic measurement) (degree Celsius [°C]) and pulse (beats per minute [bpm]) is reported. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) | ||||||
|---|---|---|---|---|---|---|---|
| Systolic Blood Pressure Lower (<85 mmHg) | Systolic Blood Pressure Upper (>180 mmHg) | Diastolic Blood Pressure Lower (<50 mmHg) | Diastolic Blood Pressure Upper (>110 mmHg) | Pulse Rate Lower (<50 bpm) | Body temperature Lower (<35.6 °C) | Body temperature Upper (>37.7 °C) | |
| Leuprorelin 1.88 mg or 3.75 mg | 2 | 1 | 5 | 3 | 1 | 23 | 0 |
| Relugolix 40 mg | 3 | 0 | 5 | 2 | 0 | 23 | 1 |
Number of participants with TEAEs of which threshold was 5% or above in either treatment group related to biochemical bone metabolism markers was reported. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Bone Resorption Test Abnormal | Resorption Bone Increased | |
| Leuprorelin 1.88 mg or 3.75 mg | 7 | 8 |
| Relugolix 40 mg | 7 | 7 |
Pain symptoms were evaluated using the NRS score. NRS score is a self-reported instrument assessing pain from 0 to 10. Higher scores reflect greater level of pain. (NCT02655237)
Timeframe: From Week 6 to 12, from Week 2 to 6, from Week 18 to 24, and for 6 weeks before the final dose (up to Week 24)
| Intervention | score on a scale (Mean) | |||
|---|---|---|---|---|
| Week 6 to 12 | Week 2 to 6 | Week 18 to 24 | For 6 weeks before the final dose (up to Week 24) | |
| Leuprorelin 1.88 mg or 3.75 mg | 0.14 | 0.27 | 0.11 | 0.12 |
| Relugolix 40 mg | 0.21 | 0.32 | 0.12 | 0.14 |
An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) |
|---|---|
| Relugolix 40 mg | 131 |
| Leuprorelin 1.88 mg or 3.75 mg | 139 |
"A transvaginal ultrasound was performed for determination of uterine volumes. On the assumption that the uterus was spheroids, the uterine volumes were calculated using 3 diameters (D1, D2, and D3) measured as shown below: D1: the longest diameter of the uterus (unit of length: cm); D2: the longest diameter of the uterus which was perpendicular to D1 (unit of length: cm); D3: the diameter of the uterus which crossed the intersection of D1 and D2 (intersection Z) and was perpendicular to D1/D2 plane (unit of length: cm). The formula used for calculation is Uterine volume=D1*D2*D3*π/6." (NCT02655237)
Timeframe: Baseline, Weeks 2, 4, 8, 12 and 24
| Intervention | cm^3 (Mean) | ||||
|---|---|---|---|---|---|
| Change at Week 2 | Change at Week 4 | Change at Week 8 | Change at Week 12 | Change at Week 24 | |
| Leuprorelin 1.88 mg or 3.75 mg | -6.90 | -17.80 | -33.83 | -38.85 | -45.73 |
| Relugolix 40 mg | -22.05 | -28.07 | -34.73 | -39.79 | -44.87 |
Number of participants with any markedly abnormal values in laboratory tests collected throughout study is reported. WBC = White blood cells, AST = Aspartate Aminotransferase, ALT = Alanine Aminotransferase, GGT = gamma-glutamyl transferase, ULN = upper limit of normal or upper reference limit. (NCT02655237)
Timeframe: Up to Week 28
| Intervention | Participants (Count of Participants) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| WBC Upper (>1.5×ULN×10^3 cells/μL) | Eosinophils Upper (>2×ULN×10^3 cells/μL) | Total cholesterol Upper (>300 mg/dL) | Triglycerides Upper (>2.5×ULN mg/dL) | Creatine kinase Upper (>5×ULN U/L) | AST Upper (>3×ULN U/L) | ALT Upper (>3×ULN U/L) | GGT Upper (>3×ULN U/L) | Hemoglobin A1c Upper (>7%) | |
| Leuprorelin 1.88 mg or 3.75 mg | 0 | 4 | 4 | 12 | 0 | 0 | 2 | 6 | 2 |
| Relugolix 40 mg | 1 | 3 | 6 | 4 | 1 | 2 | 3 | 10 | 0 |
PBAC score was used to measure volume of menstrual blood loss. Participants used sanitary products designated by sponsor and recorded the numbers of tampons or towels used, clots and flooding in patient diary. Three diagrams used which represented a lightly, moderately stained or completely saturated pad/tampon. Following scores assigned: 1) 1, 5, or 20 points for each pad; 2) 1, 5, or 10 points for each tampon; 3) 1 or 5 points for each blood clot of <1 cm/=1 cm/>1 in longest diameter; 4) 5 points for each episode of flooding. The total PBAC score (sum of points) ranges from 0 to >500. (NCT02655237)
Timeframe: Week 6 to 12
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix 40 mg | 82.2 |
| Leuprorelin 1.88 mg or 3.75 mg | 83.1 |
PBAC score was used to measure volume of menstrual blood loss. Participants used sanitary products designated by sponsor and recorded the numbers of tampons or towels used, clots and flooding in patient diary. Three diagrams used which represented a lightly, moderately stained or completely saturated pad/tampon. Following scores assigned: 1) 1, 5, or 20 points for each pad; 2) 1, 5, or 10 points for each tampon; 3) 1 or 5 points for each blood clot of <1 cm/=1 cm/>1 in longest diameter; 4) 5 points for each episode of flooding. The total PBAC score (sum of points) ranges from 0 to >500. (NCT02655237)
Timeframe: Week 2 to 6
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix 40 mg | 64.2 |
| Leuprorelin 1.88 mg or 3.75 mg | 31.7 |
PBAC score was used to measure volume of menstrual blood loss. Participants used sanitary products designated by sponsor and recorded the numbers of tampons or towels used, clots and flooding in patient diary. Three diagrams used which represented a lightly, moderately stained or completely saturated pad/tampon. Following scores assigned: 1) 1, 5, or 20 points for each pad; 2) 1, 5, or 10 points for each tampon; 3) 1 or 5 points for each blood clot of <1 cm/=1 cm/>1 in longest diameter; 4) 5 points for each episode of flooding. The total PBAC score (sum of points) ranges from 0 to >500. (NCT02655237)
Timeframe: Week 18 to 24
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix 40 mg | 84.1 |
| Leuprorelin 1.88 mg or 3.75 mg | 94.7 |
"A transvaginal ultrasound was performed to determine myoma volumes. Only the largest myoma among those measurable at visit 1 was measured throughout the study. On the assumption that the myoma was spheroids, the myoma volumes were calculated using 3 diameters (D1, D2, and D3). D1: the longest diameter of the myoma; D2: the longest diameter of the myoma which was perpendicular to D1; D3: the diameter of the myoma which crossed the intersection of D1 and D2 (intersection Z) and was perpendicular to D1/D2 plane. The formula used for calculation is Myoma volume= D1*D2*D3*π/6." (NCT02655237)
Timeframe: Baseline, Weeks 2, 4, 8, 12 and 24
| Intervention | cm^3 (Mean) | ||||
|---|---|---|---|---|---|
| Change at Week 2 | Change at Week 4 | Change at Week 8 | Change at Week 12 | Change at Week 24 | |
| Leuprorelin 1.88 mg or 3.75 mg | -6.68 | -22.44 | -40.62 | -46.87 | -53.71 |
| Relugolix 40 mg | -18.74 | -24.99 | -35.92 | -43.28 | -49.75 |
Adverse events were recorded from signed informed consent until end-of-trial. Adverse events with onset after start of IMP treatment, and within 3 months after (1 month=28 days) last dosing of IMP, were considered 'treatment-emergent' and are presented for the safety analysis set. (NCT02663908)
Timeframe: Start of IMP treatment until 3 months after last dosing of IMP
| Intervention | subjects (Number) | ||
|---|---|---|---|
| AEs | SAEs | AE leading to death | |
| Degarelix 240 mg/80 mg | 250 | 47 | 11 |
| Leuprolide 22.5 mg | 228 | 44 | 9 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict confirmed (adjudicated) CV-related death. Percentage of observed subjects with outcome measure events during the trial are reported. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 0.4 |
| Leuprolide 22.5 mg | 1.9 |
"The intensity of AE was graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) (version 4.02) 5-point scale.~AE were categorized as grade 1 Mild (minor; no specific medical intervention; asymptomatic laboratory findings only; marginal clinical relevance), Grade 2 Moderate (minimal intervention: local intervention; non-invasive intervention), Grade 3 Severe (significant symptoms, requiring hospitalization or invasive intervention; transfusion; elective interventional radiological procedure; therapeutic endoscopy or operation), Grade 4 Life-threatening or disabling (complicated by acute, life-threatening metabolic or CV complications such as circulatory failure, hemorrhage, sepsis. Life-threatening physiologic consequences; need for intensive care or emergent invasive procedure; emergent interventional radiological procedure, therapeutic endoscopy or operation) and Grade 5 Death. Events with grades 3, 4 and 5 were categorized as severe." (NCT02663908)
Timeframe: Start of IMP treatment until 3 months after last dosing of IMP
| Intervention | subjects (Number) | ||
|---|---|---|---|
| Mild AE | Moderate AE | Severe AE | |
| Degarelix 240 mg/80 mg | 224 | 160 | 59 |
| Leuprolide 22.5 mg | 200 | 135 | 55 |
"Lower urinary tract symptoms were measured with the IPSS Version 1 (IPSS-1). The IPSS is a subject-administered questionnaire containing seven items to evaluate symptoms of urinary obstruction (incomplete emptying, frequency, intermittency, urgency, weak stream, straining, nocturia) over the preceding week. Each urinary symptom question was assigned points from 0 to 5 indicating increasing severity of the particular symptom. The total IPSS-1 score was then calculated as summation over the responses for all 7 questions. The total IPSS-1 score was transformed to a scale from 0 (lowest score) to 100 (highest score). Higher scores reflect higher severity of symptoms. The IPSS-1 included an additional single question to assess a subject's QoL in relation to his urinary symptoms; response to this question was analyzed separately and was not included in the total IPSS score. The score was similarly scaled from 0 to 100.~Change from baseline in IPSS Total and QoL scores are presented." (NCT02663908)
Timeframe: Baseline to Days 168 and 336 (end-of-trial)
| Intervention | score on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| IPSS Total at Day 168 | IPSS, QoL at Day 168 | IPSS Total at Day 336 | IPSS, QoL at Day 336 | |
| Degarelix 240 mg/80 mg | -0.000 | -0.115 | -0.795 | -0.281 |
| Leuprolide 22.5 mg | 0.907 | 0.098 | 0.121 | -0.234 |
"The DASI is a self-administered instrument developed to measure functional capacity in subjects with cardiovascular disease (CVD). It contains 12 items referring to the present time, assessing the ability to perform physical tasks in five domains: personal care (1 item), ambulation (4 items), household tasks (4 items), sexual function (1 item) and recreation (2 items). Each question was answered by one of four options: 'yes with no difficulty' / 'yes, but with some difficulty' / 'no, I can't do this' / 'don't do this for other reasons'. A global score was calculated with a higher score indicating a higher functional capacity. The minimum score is 0 and the maximum score is 58.2 points.~Change from baseline in DASI Global score is presented." (NCT02663908)
Timeframe: Baseline to Days 168 and 336 (end-of-trial)
| Intervention | score on a scale (Least Squares Mean) | |
|---|---|---|
| Change in DASI to Day 168 | Change in DASI to Day 336 | |
| Degarelix 240 mg/80 mg | -2.65 | -2.18 |
| Leuprolide 22.5 mg | -1.08 | -3.01 |
"The CAQ is a self-administered questionnaire developed to measure heart-focused anxiety in persons with or without heart disease. It contains 18 items referring to the present time assessing cardiac anxiety in three domains: fear (8 items, each item could be scored between 0 never to 4 always, maximum total score 32), avoidance (5 items, each item could be scored between 0 never to 4 always, maximum total score 20) and attention (5 items, each item could be scored between 0 never to 4 always, maximum total score 20). A higher score indicated greater cardiac anxiety and the total score range was between 0 and 72.~Change from baseline in CAQ Global score and score per domain are presented." (NCT02663908)
Timeframe: Baseline to Days 168 and 336 (end-of-trial)
| Intervention | score on a scale (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| CAQ global score (Day 168) | CAQ domain score for Attention (Day 168) | CAQ domain score for Avoidance (Day 168) | CAQ domain score for Fear (Day 168) | CAQ global score (Day 336) | CAQ domain score for Attention (Day 336) | CAQ domain score for Avoidance (Day 336) | CAQ domain score for Fear (Day 336) | |
| Degarelix 240 mg/80 mg | 0.034 | 0.030 | 0.155 | -0.036 | 0.102 | 0.023 | 0.228 | 0.075 |
| Leuprolide 22.5 mg | -0.011 | -0.006 | 0.039 | -0.048 | 0.051 | -0.015 | 0.220 | -0.018 |
The total number of CV-related hospitalizations over the duration of the trial was defined as the number of hospitalizations due to CV-related adverse events, observed from the first exposure to IMP up until Day 336 for each subject. (NCT02663908)
Timeframe: First dose of IMP to Day 336 (end-of-trial)
| Intervention | Events (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 15 |
| Leuprolide 22.5 mg | 17 |
CV-related ER visit events (that did not lead to hospitalization) was observed from the first exposure to IMP up until Day 336 for each subject. (NCT02663908)
Timeframe: First dose of IMP to Day 336 (end-of-trial)
| Intervention | Events (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 8 |
| Leuprolide 22.5 mg | 2 |
The total number of CABG or PCI procedures observed for each subject over the duration of the trial (NCT02663908)
Timeframe: First dose of IMP to Day 336 (end-of-trial)
| Intervention | Events (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 3 |
| Leuprolide 22.5 mg | 6 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict first confirmed (adjudicated) unstable angina requiring hospitalization. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 0.7 |
| Leuprolide 22.5 mg | 1.5 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict first confirmed (adjudicated) stroke. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 1.1 |
| Leuprolide 22.5 mg | 1.1 |
"Composite MACE endpoint was defined as: death due to any cause, non-fatal myocardial infarction or non-fatal stroke.~Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict first confirmed (adjudicated) occurrence of composite MACE over time. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 5.5 |
| Leuprolide 22.5 mg | 4.1 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict confirmed (adjudicated) occurrence of CV-related death, non-fatal myocardial infarction or non-fatal stroke. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 3.3 |
| Leuprolide 22.5 mg | 2.6 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict first confirmed (adjudicated) myocardial infarction. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 1.8 |
| Leuprolide 22.5 mg | 1.1 |
"Time to failure in PFS was defined as the time, measured in days, from randomization to the first occurrence of either death, radiographic disease progression, introduction of additional prostate cancer therapies for progression, or PSA failure.~Subjects who discontinued treatment with IMP or withdrew from the trial were censored at the time of discontinuation/withdrawal.~Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict failure in PFS. Percentage of observed subjects with outcome measure events during the trial are reported." (NCT02663908)
Timeframe: From randomization to end-of-trial for each subject (subjects not censored at Day 336)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 8.7 |
| Leuprolide 22.5 mg | 10.0 |
"Kaplan Meier plots of the cumulative incidence rate by treatment groups were used to depict death due to any cause. Percentage of observed subjects with outcome measure events during the trial are reported.~Subjects were censored at the time a subject discontinued the trial, was lost to follow-up, discontinued treatment with IMP, initiated treatment with prohibited medication (including hormonal combination therapy), or at Day 336, whichever occurred first." (NCT02663908)
Timeframe: Randomization to Day 336 (end-of-trial)
| Intervention | percentage of subjects (Number) |
|---|---|
| Degarelix 240 mg/80 mg | 2.9 |
| Leuprolide 22.5 mg | 3.3 |
"Number of subjects shifting from normal value(s) in vital signs (pulse and blood pressure) at baseline to clinically significant abnormal value(s) at end-of-trial are presented.~Note: Only subjects with appropriate baseline and post-baseline data are included in the evaluation." (NCT02663908)
Timeframe: Baseline to Day 336 (end-of-trial)
| Intervention | Participants (Count of Participants) |
|---|---|
| Degarelix 240 mg/80 mg | 0 |
| Leuprolide 22.5 mg | 1 |
"The EQ-5D-5L essentially consists of 2 systems - the EQ-5D-5L descriptive system and the EQ visual analogue scale (EQ VAS). The EQ-5D-5L descriptive system comprises the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. The EQ VAS is an overall estimation of the present health status. The results from the EQ-5D-5L questionnaire were converted into quality adjusted life year (QALY) units.~The QALY is estimated by combining the value of life (utility value) and length of life. Quality adjusted life years are based on a principle assuming that a year of life lived in perfect health is worth 1 QALY and that a year of life lived in a state of less than perfect health is worth less than 1." (NCT02663908)
Timeframe: Baseline to Day 336 (end-of-trial)
| Intervention | QALY (Least Squares Mean) |
|---|---|
| Degarelix 240 mg/80 mg | 0.794 |
| Leuprolide 22.5 mg | 0.796 |
Median levels and interquartile ranges for serum testosterone at Days 28, 168, and 336 are presented. (NCT02663908)
Timeframe: Days 28, 168 and 336 (end-of-trial)
| Intervention | ng/dL (Median) | ||
|---|---|---|---|
| Day 28 | Day 168 | Day 336 | |
| Degarelix 240 mg/80 mg | 8.650 | 8.650 | 9.855 |
| Leuprolide 22.5 mg | 14.410 | 8.475 | 8.650 |
"To assess the safety and therapeutic benefit of multimodality therapy in men presenting with newly diagnosed oligometastatic prostate cancer (<5 sites of metastases). Safety is defined as the incidence of Grades 3 and 4 neutropenia and surgical- or radiation-induced toxicities.~Neutropenia is a lower than normal number of neutrophils (a type of white blood cell) in the blood. Although dependent on the specific laboratory, the normal number is of neutrophils is generally about 1500-7800 cells/microliter. Grade 3 and 4 neutropenia refer to neutrophil levels <1,000-500 and <500, respectively. The average risk of docetaxel-induced Grade 3 and 4 neutropenia is about 35%. During the course of the study, if we had seen evidence that the risk of Grade 3 and 4 neutropenia was >50%, the study would have been stopped." (NCT02716974)
Timeframe: 3 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Chemohormonal and Definitive Therapy | 26 |
To evaluate efficacy of multimodality therapy in men, defined as the 2 year PSA progression-free (PSA<0.2 ng/ml) survival among men who have non-castrate testosterone levels 2 years after enrollment. Number of participants (who have non-castrate testosterone levels 2 years after enrollment) with PSA progression-free survival. (NCT02716974)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Chemohormonal and Definitive Therapy | 17 |
To investigate the time from an undetectable prostate-specific antigen (≤0.2 ng/mL) until the prostate-specific antigen is >0.2 over two time-points. (NCT02716974)
Timeframe: 3 years
| Intervention | Months (Median) |
|---|---|
| Chemohormonal and Definitive Therapy | 31 |
To evaluate PSA, FKBP5, TMPRSS2, EZH2, H3K27, and UBE2C tissue expression (via IHC) in malignant prostate tissue after treatment with Leuprolide and Apalutamide. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | |||||
|---|---|---|---|---|---|---|
| PSA Homozygous (1245A) | H3K27 Homozygous (1245A) | PSA heterozygous | H3K27 heterozygous | PSA Homozygous (1245C) | H3K27 Homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 1.15 | 1.619 | 1.393 | 1.633 | 1.375 | 0.744 |
To evaluate the differential effect of neoadjuvant leuprolide and ARN-509 on other androgens (testosterone (T), dehydroepiandrosterone (DHEA), androstenediol, 5?-androstanedione (5?-dione), androstenedione (AD), androsterone and 5?-androstanediol) concentration in benign prostate tissue based on HSD3B1 genotype. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| DHT homozygous(1245A) | T homozygous(1245A) | DHEA homozygous(1245A) | AD homozygous(1245A) | DHT heterozygous | T heterozygous | DHEA heterozygous | AD heterozygous | DHT homozygous (1245C) | T homozygous (1245C) | AD homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 9.066 | 6.901 | 46.110 | 8.394 | 5.917 | 4.929 | 18.5788 | 6.083 | 9.345 | 4.704 | 8.303 |
To evaluate the effect of neoadjuvant ARN-509 on other androgens (DHT, T, DHEA, androstenediol, 5?-dione, AD, androsterone and 5?-androstanediol) concentration in malignant prostate tissue after neoadjuvant leuprolide and ARN-509. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| DHT homozygous (1245A) | T homozygous (1245A) | DHEA homozygous (1245A) | AD homozygous (1245A) | DHT heterozygous | T heterozygous | DHEA heterozygous | AD heterozygous | DHT homozygous (1245C) | T homozygous (1245C) | DHEA homozygous (1245C) | AD homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 8.855 | 5.691 | 22.941 | 7.974 | 5.238 | 5.719 | 24.543 | 8.593 | 2.622 | 4.489 | 1.421 | 6.959 |
To evaluate the differential effect of neo-adjuvant leuprolide and ARN-509 on dihydrotestosterone (DHT) concentration in benign prostate tissue based on HSD3B1 genotype. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | ||
|---|---|---|---|
| homozygous (1245A) | heterozygous (1254C) | homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 9.066 | 5.917 | 9.345 |
To evaluate PSA, FKBP5, TMPRSS2, EZH2, H3K27, and UBE2C tissue expression (via qPCR) in malignant prostate tissue after treatment with Leuprolide and Apalutamide. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| PSA homozygous (1245A) | FKBP5 homozygous (1245A) | TMPRSS2 homozygous (1245A) | PSA heterozygous | FKBP5 heterozygous | TMPRSS2 heterozygous | PSA homozygous (1245C) | FKBP5 homozygous (1245C) | TMPRSS2 homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 1.474 | 1.304 | 1.603 | 1.127 | 1.127 | 1.742 | 2.221 | 2.221 | 2.345 |
To evaluate the differential effect of neo-adjuvant leuprolide and ARN-509 on dihydrotestosterone (DHT) concentration in malignant prostate tissue based on HSD3B1 genotype. (NCT02770391)
Timeframe: Up to 28 Days
| Intervention | nM (Mean) | ||
|---|---|---|---|
| homozygous (1245A) | heterozygous (1254C) | homozygous (1245C) | |
| Apalutamide + Leuprolide Acetate | 8.855 | 5.238 | 2.622 |
"Progesterone level is considered suppressed during the evaluation period if a value below pre-specified threshold (3000 pg/mL) was reported at least once during that period.~The days in row title indicate the evaluation interval." (NCT02807363)
Timeframe: Dosing period: Day 1 to Day 28 and 28 day Post-Dosing Period; 29 day is post dosing day 1
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| Days 8, 15, 22, 28 and 29 | Days 15, 22, 28 and 29 | Days 22, 28 and 29 | Days 22 and 29 | Entire 28-day Dosing Period | 28-day Post-dosing Period | |
| Leuprolide 1 Month Depot (Treatment C) | 3 | 0 | 0 | 0 | 4 | 2 |
| Leuprolide Oral Tablet, 10 mg BID (Treatment D) | 10 | 0 | 0 | 0 | 12 | 12 |
| Leuprolide Oral Tablet, 4 mg BID (Treatment B) | 3 | 2 | 2 | 1 | 5 | 7 |
| Leuprolide Oral Tablet, 4 mg QD (Treatment A) | 4 | 2 | 2 | 2 | 8 | 9 |
Treatment C is a depot formulation established to release the drug over a period of 1 month. The data for post dosing adverse event was collected starting from day 1 to 28 post the 28th day of dosing. (NCT02807363)
Timeframe: Post dosing period (starting day 1 to day 28 post dosing period)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Number of subjects with at least one TEAE | Number of subject who discontinued due to TEAEs | |
| Leuprolide 1 Month Depot(Treatment C) | 1 | 0 |
| Leuprolide Oral Tablet, 10 mg BID (Treatment D) | 3 | 0 |
| Leuprolide Oral Tablet, 4 mg BID (Treatment B) | 2 | 0 |
| Leuprolide Oral Tablet, 4 mg QD (Treatment A) | 1 | 0 |
"Treatment A and B: Steady state concentration level calculated for oral tablets at the end of the fourth treatment week (Treatment Day 28) as the 24-hour AUCs divided by the duration of the dosing interval i.e. 24 hours.~Treatment C: Steady state concentration level calculated for IM injection at the fourth treatment week (a mean of leuprolide levels on Days 22 and 29)." (NCT02807363)
Timeframe: Treatment Day 28 for oral groups; Treatment Days 22-29 for Lupron Depot group
| Intervention | pg/mL (Mean) |
|---|---|
| Leuprolide Oral Tablet, 4 mg QD (Treatment A) | 357.80 |
| Leuprolide Oral Tablet, 4 mg BID (Treatment B) | 688.27 |
| Leuprolide 1 Month Depot (Treatment C) | 180.95 |
"The participant incidence of TEAEs was generally comparable during the dosing period across the treatment groups.~Treatment C is a depot formulation established to release the drug over a period of 1 month. The data for adverse event was collected for day 1 to 28 of the dosing period." (NCT02807363)
Timeframe: Dosing Period: Day 1 to day 28
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Number of subjects with at least one TEAE | Number of subjects who discontinued due to TEAE | |
| Leuprolide 1 Month Depot (Treatment C) | 4 | 0 |
| Leuprolide Oral Tablet, 10 mg BID (Treatment D) | 8 | 0 |
| Leuprolide Oral Tablet, 4 mg BID (Treatment B) | 9 | 1 |
| Leuprolide Oral Tablet, 4 mg QD (Treatment A) | 7 | 0 |
"Criterion: E2 level is considered suppressed during the evaluation period if a value below pre-specified threshold was reported at least once during that period.~The days in the row title indicate the evaluation interval." (NCT02807363)
Timeframe: Dosing Period: Day 8 to 28, Post-dosing: Day 1 to day 28 of post dosing period; Day 29 is the post dosing day 1
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| Days 8,15, 22, 28 and 29 | Days 15, 22, 28 and 29 | Days 22, 28 and 29 | Days 22 and 29 | Entire 28-day Dosing Period | 28-day Post-dosing Period | |
| Leuprolide 1 Month Depot (Treatment C) | 5 | 5 | 5 | 5 | 5 | 5 |
| Leuprolide Oral Tablet, 10 mg BID (Treatment D) | 12 | 12 | 9 | 9 | 12 | 9 |
| Leuprolide Oral Tablet, 4 mg BID (Treatment B) | 7 | 7 | 6 | 6 | 8 | 6 |
| Leuprolide Oral Tablet, 4 mg QD (Treatment A) | 6 | 5 | 4 | 4 | 7 | 7 |
The QOL will be measured using the Expanded Prostate Cancer Index Composite 26 (EPIC-26). For part 2, the questionnaires will be administered at 6 months, 12 months, and 24 months post RP. Resulting domain scores for EPIC-26 (urinary incontinence, urinary obstruction, sexual, bowel, hormonal/vitality) is on a 0-100 scale, with higher values representing a more favorable health-related QOL. (NCT02903368)
Timeframe: At 24-months post-RP
| Intervention | score on 0-100 scale (Mean) | ||||
|---|---|---|---|---|---|
| Urinary Irritative | Urinary Incontinence | Bowel | Sexual | Hormonal | |
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 92 | 75 | 95 | 31 | 88 |
| Arm 2B: Observation (Part 2) | 93 | 76 | 97 | 26 | 90 |
2-year bPFS rate is defined as the probability of biochemical progression free and survival at 2 years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event is considered to be biochemical progression (defined as a confirmed PSA ≥ 0.2 ng/mL), local, regional, or distant metastatic disease on CT/MRI or bone scan, or receipt of post-operative systemic therapy or radiotherapy for rising PSA, or death from any cause. Participants who are lost to follow-up before the 2-year mark are censored at date of last disease evaluation. (NCT02903368)
Timeframe: At 2 years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 90 |
| Arm 2B: Observation (Part 2) | 80 |
3-year bPFS rate is defined as the probability of biochemical progression free and survival at 3 years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event is considered to be biochemical progression (defined as a confirmed PSA ≥ 0.2 ng/mL), local, regional, or distant metastatic disease on CT/MRI or bone scan, or receipt of post-operative systemic therapy or radiotherapy for rising PSA, or death from any cause. Participants who are lost to follow-up before the 3-year mark are censored at date last disease evaluation. (NCT02903368)
Timeframe: At 3 years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 81 |
| Arm 2B: Observation (Part 2) | 72 |
Intra-operative complications were collected via questionnaire following Radical Prostatectomy. (NCT02903368)
Timeframe: Assessed post-RP, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 1 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 1 |
Intraductal carcinoma was evaluated by central pathology review of specimens at Radical Prostatectomy (RP). (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 15 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 19 |
"RCB was calculated as tumor volume (cm^3) X % cellularity. RCB was analyzed as a continuous score (with median and range) instead of a categorical variable based on the percentile cutoff point, at the time of radical prostatectomy (RP)." (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | (cm^3) * % (Median) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 0.023 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 0.075 |
Prostate specific antigen (PSA) was measured on day 1 of each cycle during the neoadjuvant therapy. PSA nadir was defined as the lowest PSA value prior to Radical Prostatectomy (RP). Number and percent of participants with nadir PSA < 0.2 ng/mL were reported. (NCT02903368)
Timeframe: Assessed on day 1 of each cycle (1 cycle=28 +/- 2 days), up to 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 55 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 58 |
Defined as the probability of freedom from further anti-cancer therapy at 2-years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event includes initiation of anti-cancer therapy (radiation therapy, ADT, or other therapies) for rising PSAs and/or clinical progression. Participants who are lost to follow-up before the 2-year mark are censored at date of last follow-up. (NCT02903368)
Timeframe: At 2-years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 90 |
| Arm 2B: Observation (Part 2) | 80 |
Defined as the probability of freedom from further anti-cancer therapy at 3-years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event includes initiation of anti-cancer therapy (radiation therapy, ADT, or other therapies) for rising PSAs and/or clinical progression. Participants who are lost to follow-up before the 3-year mark are censored at date of last follow-up. (NCT02903368)
Timeframe: At 3 years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 83 |
| Arm 2B: Observation (Part 2) | 72 |
Defined as the probability of freedom from further anti-cancer therapy at 4-years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event includes initiation of anti-cancer therapy (radiation therapy, ADT, or other therapies) for rising PSAs and/or clinical progression. Participants who are lost to follow-up before the 4-year mark are censored at date of last follow-up. (NCT02903368)
Timeframe: At 4-years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 78 |
| Arm 2B: Observation (Part 2) | 67 |
Pathological Complete Response (pCR) is defined as the absence of morphologically identifiable carcinoma in the RP specimen at radical prostatectomy (RP). (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 7 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 6 |
The QOL will be measured using the Expanded Prostate Cancer Index Composite 26 (EPIC-26). For part 2, the questionnaires will be administered at 6 months, 12 months, and 24 months post RP. Resulting domain scores for EPIC-26 (urinary incontinence, urinary obstruction, sexual, bowel, hormonal/vitality) is on a 0-100 scale, with higher values representing a more favorable health-related QOL. (NCT02903368)
Timeframe: At 12-months post-RP
| Intervention | score on 0-100 scale (Mean) | ||||
|---|---|---|---|---|---|
| Urinary Irritative | Urinary Incontinence | Bowel | Sexual | Hormonal | |
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 91 | 75 | 95 | 16 | 68 |
| Arm 2B: Observation (Part 2) | 91 | 74 | 94 | 26 | 86 |
The QOL will be measured using the Expanded Prostate Cancer Index Composite 26 (EPIC-26). For part 2, the questionnaires will be administered at 6 months, 12 months, and 24 months post RP. Resulting domain scores for EPIC-26 (urinary incontinence, urinary obstruction, sexual, bowel, hormonal/vitality) is on a 0-100 scale, with higher values representing a more favorable health-related QOL. (NCT02903368)
Timeframe: At 6-months post-RP
| Intervention | Score on 0-100 (Mean) | ||||
|---|---|---|---|---|---|
| Urinary Irritative | Urinary Incontinence | Bowel | Sexual | Hormonal | |
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 90 | 63 | 95 | 17 | 68 |
| Arm 2B: Observation (Part 2) | 92 | 72 | 96 | 14 | 83 |
Presence or cribriform was evaluated by central pathology review of specimens at radical prostatectomy (RP). (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 1 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 0 |
Pathologic specimens were centrally reviewed and counted for positive surgical margins at the time of Radical Prostatectomy (RP). (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 4 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 7 |
Pathological response, defined as achieving either pCR or MRD at radical prostatectomy (RP). Pathological Complete Response (pCR) is defined as the absence of morphologically identifiable carcinoma in the RP specimen. MRD will be defined as residual tumor in the RP specimen measuring ≤ 5 mm. (NCT02903368)
Timeframe: Assessed from RP specimens, at 6 months from the initiation of neoadjuvant therapy.
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1A: AAPL Neoadjuvant Therapy (Part 1) | 12 |
| Arm 1B: APL Neoadjuvant Therapy (Part 1) | 12 |
4-year bPFS rate is defined as the probability of biochemical progression free and survival at 4 years from the date of Part 2 randomization, which is estimated using Kaplan Meier methods. The event is considered to be biochemical progression (defined as a confirmed PSA ≥ 0.2 ng/mL), local, regional, or distant metastatic disease on CT/MRI or bone scan, or receipt of post-operative systemic therapy or radiotherapy for rising PSA, or death from any cause. Participants who are lost to follow-up before the 4-year mark are censored at date of last disease evaluation. (NCT02903368)
Timeframe: At 4 years post RP
| Intervention | percentage of subjects (Number) |
|---|---|
| Arm 2A: AAPL Adjuvant Therapy (Part 2) | 67 |
| Arm 2B: Observation (Part 2) | 61 |
Exploratory analysis performed in archival tumor samples collected during screening in the main study. Protein expression levels of the ribociclib plus letrozole cohort that did not achieve clinical benefit (progression within 3 months of treatment) and the cohort sensitive to ribociclib and letrozole (cohort with a time to progression of 22 months or more) were determined using using Single-Pot, Solid-Phase-enhanced, Sample Preparation-Clinical Tissue Proteomics (SP3-CTP). For normalization purposes a pooled internal standard sample, comprised of aliquots of every sample included in the study, was included in each experimental batch. Protein abundances were calculated as the log2 transformed abundances relative to the pooled internal standard. Positive values represent higher protein expression levels compared to the pooled internal standard. Expression levels of proteins that showed association to predicting response to study treatment are presented. (NCT02941926)
Timeframe: Screening (up to 28 days before first dose of study treatment)
| Intervention | log2 transformed relative ratio (Mean) | ||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Isocitrate dehydrogenase [NADP] cytoplasmic (IDH1) | Retinal dehydrogenase 1 (ALDH1A1) | Coagulation factor XIII A chain (F13A1) | Argininosuccinate synthase (ASS1) | Heat shock protein beta-1 (HSPB1) | Aldehyde dehydrogenase, mitochondrial (ALDH2) | Decorin (DCN) | Cathepsin G (CTSG) | Pyruvate carboxylase, mitochondrial (PC) | C-1-tetrahydrofolate synthase, cytoplasmic (MTHFD1) | Collagen alpha-3(VI) chain (COL6A3) | Versican core protein (VCAN) | Fibulin-1 (FBLN1) | Acetyl-CoA acetyltransferase, mitochondrial (ACAT1) | Long-chain-fatty-acid--CoA ligase 1 (ACSL1) | Pigment epithelium-derived factor (SERPINF1) | 3-ketoacyl-CoA thiolase, mitochondrial (ACAA2) | Fatty acid synthase (FASN) | Lumican (LUM) | Fibulin-2 (FBLN2) | Prolow-density lipoprotein receptor-related protein 1 (LRP1) | Galectin-3-binding protein (LGALS3BP) | Inactive tyrosine-protein kinase 7 (PTK7) | Ras GTPase-activating-like protein IQGAP2 (IQGAP2) | Spectrin alpha chain, non-erythrocytic 1 (SPTAN1) | Periostin (POSTN) | Procollagen C-endopeptidase enhancer 1 (PCOLCE) | CD109 antigen (CD109) | Palladin (PALLD) | Collagen triple helix repeat-containing protein 1 (CTHRC1) | Collagen alpha-1(XII) chain (COL12A1) | Matrix-remodeling-associated protein 5 (MXRA5) | C-type mannose receptor 2 (MRC2) | |
| Primary Resistance Cohort | 0.112 | 0.022 | -0.378 | 0.104 | -0.546 | 0.319 | -0.456 | -0.634 | 0.413 | 0.033 | -0.186 | -0.301 | -0.245 | 0.135 | 0.296 | -0.378 | 0.258 | -0.198 | -0.355 | -0.208 | -0.148 | -0.491 | -0.251 | 0.318 | 0.085 | -0.419 | -0.217 | -0.213 | -0.207 | -0.514 | -0.302 | -0.221 | -0.201 |
| Sensitive Cohort | -0.218 | -0.325 | -0.010 | -0.466 | -0.151 | -0.077 | -0.033 | -0.175 | -0.004 | -0.129 | -0.015 | 0.141 | 0.128 | -0.074 | -0.144 | 0.169 | -0.080 | 0.038 | 0.010 | 0.075 | 0.094 | -0.126 | 0.070 | -0.036 | -0.082 | 0.051 | 0.184 | 0.043 | 0.050 | 0.176 | 0.230 | 0.205 | 0.170 |
"Clinical benefit rate (CBR) is defined as the percentage of participants with a best overall response of complete response (CR), or partial response (PR) or an overall lesion response of stable disease (SD), lasting as per local review, for a duration of at least 24 weeks. CR, PR and SD are defined according to RECIST 1.1 based on investigator's assessment.~CR: Disappearance of all non-nodal target lesions. In addition, any pathological lymph nodes assigned as target lesions must have a reduction in short axis to < 10 mm PR: At least a 30% decrease in the sum of diameter of all target lesions, taking as reference the baseline sum of diameters.~SD: Neither sufficient shrinkage to qualify for PR or CR nor an increase in lesions which would qualify for progressive disease.~95% CI was calculated using the exact binomial method." (NCT02941926)
Timeframe: Up to approximately 33 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Ribociclib + Letrozole + Goserelin/Leuprolide | 70.7 |
"Time to progression (TTP) is defined as time from date of start of treatment to the date of first documented progression or death due to underlying cancer. Participants with symptoms of rapidly progressing disease without radiologic evidence were classified as progression only when clear evidence of clinical deterioration was documented and/or patient discontinued due to 'Disease progression' or death due to study indication. When there was no documentation of radiologic evidence of progression, and the patient discontinued for 'Disease progression' due to documented clinical deterioration of disease, the date of discontinuation was used as date of progression.~TTP was estimated using the Kaplan-Meier method. 95% CI of median was calculated according to Brookmeyer and Crowley method." (NCT02941926)
Timeframe: Up to approximately 33 months
| Intervention | Months (Median) |
|---|---|
| Ribociclib + Letrozole + Goserelin/Leuprolide | 27.1 |
"Overall response rate (ORR) is defined as the percentage of participants with best overall response of complete response (CR) or partial response (PR) according to RECIST 1.1 based on investigator's assessment.~CR: Disappearance of all non-nodal target lesions. In addition, any pathological lymph nodes assigned as target lesions must have a reduction in short axis to < 10 mm PR: At least a 30% decrease in the sum of diameter of all target lesions, taking as reference the baseline sum of diameters.~95% CI was calculated using the exact binomial method." (NCT02941926)
Timeframe: Up to approximately 33 months
| Intervention | Percentage of participants (Number) |
|---|---|
| Ribociclib + Letrozole + Goserelin/Leuprolide | 29.3 |
"On-treatment- Core phase: from first treatment in the Core phase up to 30 days post-treatment (for participants who did not enter the Extension phase) or up to last treatment in the Core phase (for participants who entered the Extension phase). Extension phase: from first dose of treatment in the Extension phase up to 30 days after last dose of treatment.~Post-treatment survival follow-up- Core phase: from 31 days post-treatment in the core phase up to end of study; Extension phase: from 31 days post-treatment in the Extension phase up to end of study." (NCT02941926)
Timeframe: On-treatment Core Phase: up to 33 months; Post-treatment survival Follow-up Core Phase: Up to 33 months; On-treatment Extension Phase: up to approximately 37.6 months; Post-treatment survival Follow-up Extension Phase: Up to approximately 37.6 months.
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| On-treatment Core Phase | Post-treatment survival follow-up Core Phase | All deaths Core Phase | On-treatment Extension Phase | Post-treatment survival follow-up Extension Phase | All deaths Extension Phase | |
| Ribociclib + Letrozole + Goserelin/Leuprolide | 74 | 90 | 164 | 5 | 3 | 8 |
"Change from baseline in FACT-B scores was assessed. FACT-B is a self-report instrument that measures multidimensional quality of life (QOL) in patients with breast cancer. The FACT-B consists of 37 questions that address physical, social, emotional, and functional well-being, with specific questions relevant to women with breast cancer. Each item has a score range of 0 (Not at all) to 4 (Very much), with a total score ranging from 0-148. The higher the score, the better the QOL reported by the participant. A positive change from baseline indicates improvement in QoL.~Due to the nature of the questionnaire, only females were asked to complete this questionnaire." (NCT02941926)
Timeframe: On Day 1 of Cycle 1, 2, 3, 4 ,5, 6, 8, 10, 12 and after that every 3 cycles, and End of treatment, assessed up to 33 months. Cycle=28 days
| Intervention | Score on a scale (Mean) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cycle 2 Day 1 | Cycle 3 Day 1 | Cycle 4 Day 1 | Cycle 5 Day 1 | Cycle 6 Day 1 | Cycle 8 Day 1 | Cycle 10 Day 1 | Cycle 12 Day 1 | Cycle 15 Day 1 | Cycle 18 Day 1 | Cycle 21 Day 1 | Cycle 24 Day 1 | Cycle 27 Day 1 | Cycle 30 Day 1 | Cycle 33 Day 1 | End of Treatment | |
| Ribociclib + Letrozole + Goserelin/Leuprolide | 0.2 | 0.1 | -0.3 | 0.0 | -0.8 | -0.9 | -1.2 | -1.6 | -2.0 | -2.0 | -2.0 | -3.0 | -2.7 | -2.0 | 12.1 | -4.1 |
"AEs were defined as the appearance of (or worsening of any pre-existing) undesirable sign(s), symptom(s), or medical condition(s).~SAEs were defined as meeting at least 1 of the following criteria: is fatal or life-threatening, Results in persistent or significant disability/incapacity, constitutes a congenital anomaly/birth defect, is medically significant, requires inpatient hospitalization or prolongation of existing hospitalization. A SAE which caused death of the participant was considered as fatal SAE.~AEs were assessed and graded according to the Common Terminology Criteria for Adverse Events (CTCAE) version 4.03. Grade 1 to 5 were used to characterize the severity of the Adverse Event. Grade 1: mild; Grade 2: moderate; Grade 3: severe; Grade 4: life-threatening and Grade 5: death related to AE.~A participant with multiple severity grades for an AE is only counted under the maximum grade." (NCT02941926)
Timeframe: From start of treatment up to 30 days after last treatment (for participants who did not enter to the Extension phase) or up to last treatment in the Core phase (for participants who entered the Extension phase), assessed up to approximately 33 months.
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AEs- All grades | AEs- Grade ≥ 3 | Treatment-related AEs- All grades | Treatment-related AEs- Grade ≥ 3 | SAEs- All grades | SAEs- Grade ≥ 3 | Treatment-related SAEs- All grades | Treatment-related SAEs- Grade ≥ 3 | Fatal SAEs- All grades | Treatment-related Fatal SAEs- All grades | AEs leading to discontinuation- All grades | AEs leading to discontinuation- Grade ≥ 3 | Treatment-related AEs leading to discontinuation- All grades | Treatment-related AEs leading to discontinuation-Grade ≥ 3 | AEs leading to dose adjustment/interruption- All grades | AEs leading to dose adjustment/interruption- Grade ≥ 3 | Treatment-related AEs leading to dose adjustment/interruption- All grades | Treatment-related AEs leading to dose adjustment/interruption- Grade ≥ 3 | AEs requiring additional therapy- All grades | AEs requiring additional therapy- Grade ≥ 3 | Treatment-related AEs requiring additional therapy- All grades | Treatment-related AEs requiring additional therapy- Grade ≥ 3 | |
| Ribociclib + Letrozole + Goserelin/Leuprolide | 3203 | 2461 | 3091 | 2192 | 702 | 590 | 203 | 178 | 62 | 14 | 528 | 310 | 418 | 237 | 2434 | 2095 | 2235 | 1964 | 2624 | 844 | 1613 | 392 |
"AEs were defined as the appearance of (or worsening of any pre-existing) undesirable sign(s), symptom(s), or medical condition(s).~SAEs were defined as meeting at least 1 of the following criteria: is fatal or life-threatening, Results in persistent or significant disability/incapacity, constitutes a congenital anomaly/birth defect, is medically significant, requires inpatient hospitalization or prolongation of existing hospitalization.~AEs were assessed and graded according to the Common Terminology Criteria for Adverse Events (CTCAE) version 4.03. Grade 1 to 5 were used to characterize the severity of the Adverse Event. Grade 1: mild; Grade 2: moderate; Grade 3: severe; Grade 4: life-threatening and Grade 5: death related to AE.~A participant with multiple severity grades for an AE is only counted under the maximum grade." (NCT02941926)
Timeframe: From first dose of treatment in the Extension phase up to 30 days after last dose of treatment, assessed up approximately 37.6 months
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| AEs- All grades | AEs- Grade ≥ 3 | Treatment-related AEs- All grades | Treatment-related AEs- Grade ≥ 3 | SAEs- All grades | SAEs- Grade ≥ 3 | Treatment-related SAEs- All grades | Treatment-related SAEs- Grade ≥ 3 | Fatal SAEs- All grades | Treatment-related Fatal SAEs- All grades | AEs leading to discontinuation- All grades | AEs leading to discontinuation- Grade ≥ 3 | Treatment-related AEs leading to discontinuation- All grades | Treatment-related AEs leading to discontinuation-Grade ≥ 3 | AEs leading to dose adjustment/interruption- All grades | AEs leading to dose adjustment/interruption- Grade ≥ 3 | Treatment-related AEs leading to dose adjustment/interruption- All grades | Treatment-related AEs leading to dose adjustment/interruption- Grade ≥ 3 | AEs requiring additional therapy- All grades | AEs requiring additional therapy- Grade ≥ 3 | Treatment-related AEs requiring additional therapy- All grades | Treatment-related AEs requiring additional therapy- Grade ≥ 3 | |
| Ribociclib + Letrozole + Goserelin/Leuprolide | 297 | 159 | 221 | 123 | 54 | 45 | 7 | 6 | 5 | 0 | 17 | 9 | 7 | 4 | 185 | 132 | 134 | 113 | 186 | 56 | 47 | 12 |
Clinical benefit as assessed by the Investigator during Extension phase (NCT02941926)
Timeframe: On Day 1 of every 3 cycles, starting from Cycle 1 of the Extension phase until end of treatment, assessed up to 37.4 months. Cycle= 28 days
| Intervention | Participants (Count of Participants) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cycle 1 Day 1 | Cycle 4 Day 1 | Cycle 7 Day 1 | Cycle 10 Day 1 | Cycle 13 Day 1 | Cycle 16 Day 1 | Cycle 19 Day 1 | Cycle 22 Day 1 | Cycle 25 Day 1 | Cycle 28 Day 1 | Cycle 31 Day 1 | Cycle 34 Day 1 | Cycle 37 Day 1 | Cycle 40 Day 1 | |
| Ribociclib + Letrozole + Goserelin/Leuprolide | 413 | 386 | 353 | 323 | 245 | 200 | 183 | 118 | 55 | 51 | 44 | 32 | 24 | 5 |
"Measuring the mean transcript change of membrane bound progestin receptors (PGRMC1) from follicular phase to ovulation to luteal phase of spontaneous menstrual cycle.~Total RNA (ribonucleic acid) was isolated from endocervical cell samples and analyzed for expression of PGRMC1 using real-time PCR (polymerase chain reaction) relative to levels of ribosomal (S10) RNA. An endocervical brush will be inserted into the os and then immediately rinsed into a special RNA preserving reagent. After total RNA is isolated and purified, it will be reverse transcribed into cDNA using primers.~Ratio of PGRMC1 to 18s RNA~Gene expression of membrane bound progesterone receptors in endocervical cells" (NCT02969590)
Timeframe: 1 month
| Intervention | ratio (Mean) | ||
|---|---|---|---|
| Follicular Phase | Ovulation Phase | Luteal Phase | |
| Spontaneous Cycle | 1.2 | 4.0 | 1.02 |
"Measurement of median cervical mucus scores at baseline. The current clinical standard for appraising cervical mucus is the cervical mucus score (ie. Insler score) that examines mucus based on 5 metrics including volume, spinnbarkeit (stretch), ferning, viscosity and cellularity on a 15-point scale. Per WHO guidelines, scores above 10 are considered mucus favoring penetration and scores below 10 are considered to be unfavorable to penetration." (NCT02969590)
Timeframe: Baseline
| Intervention | score on a scale (Median) |
|---|---|
| Norethindrone | 11 |
| Estradiol | 13 |
"Measurement of median cervical mucus scores 6 hours following norethindrone administration. The current clinical standard for appraising cervical mucus is the cervical mucus score (ie. Insler score) that examines mucus based on 5 metrics including volume, spinnbarkeit (stretch), ferning, viscosity and cellularity on a 15-point scale. Per WHO guidelines, scores above 10 are considered mucus favoring penetration and scores below 10 are considered to be unfavorable to penetration." (NCT02969590)
Timeframe: 6 hours
| Intervention | score on a scale (Median) |
|---|---|
| Norethindrone | 6.5 |
| Estradiol | 8.5 |
"Measurement of median cervical mucus scores 24 hours following norethindrone administration. The current clinical standard for appraising cervical mucus is the cervical mucus score (ie. Insler score) that examines mucus based on 5 metrics including volume, spinnbarkeit (stretch), ferning, viscosity and cellularity on a 15-point scale. Per WHO guidelines, scores above 10 are considered mucus favoring penetration and scores below 10 are considered to be unfavorable to penetration." (NCT02969590)
Timeframe: 24 hours
| Intervention | score on a scale (Median) |
|---|---|
| Norethindrone | 8 |
| Estradiol | 10.5 |
"Measurement of median cervical mucus scores 2 hours following norethindrone administration. The current clinical standard for appraising cervical mucus is the cervical mucus score (ie. Insler score) that examines mucus based on 5 metrics including volume, spinnbarkeit (stretch), ferning, viscosity and cellularity on a 15-point scale. Per WHO guidelines, scores above 10 are considered mucus favoring penetration and scores below 10 are considered to be unfavorable to penetration." (NCT02969590)
Timeframe: 2 hours
| Intervention | score on a scale (Median) |
|---|---|
| Norethindrone | 8.5 |
| Estradiol | 10.5 |
Tanner Stage is used to measure pubertal development. Female (F) and male (M) participants were evaluated for breast development and genital development respectively and both genders for pubic hair development. Tanner Stage is based on progression through 5-stages. Participants were classified as having progression if either breast/genitals or pubic hair progression were present. Otherwise participant is classified as regression or no progression. (NCT02993926)
Timeframe: No longer treated for CPP group - Month: 27 (766- 855 days) post last dose of Enantone; Treated with Non-Enantone GnRHa group - Month 21 (586- 675 days) post last dose of Enantone
| Intervention | percentage of participants (Number) |
|---|---|
| FollowUp:Treated With Non-Enantone GnRHa After Enantone-Female | 0 |
Bone age (BA) was estimated using an X-ray. Chronological age (CA) at the date of corresponding X-ray (Date of X-ray - Date of birth)/365.25. Ratio of BA/CA was calculated. (NCT02993926)
Timeframe: The mean duration of Enantone exposure was 22.3 months, ranging from 10.1 to 52.4 months
| Intervention | percentage of participants (Number) |
|---|---|
| Treatment Phase: Enantone (Male) | 75.0 |
| Treatment Phase: Enantone (Female) | 90.2 |
Bone age (BA) was estimated using an X-ray. Chronological age (CA) at the date of corresponding X-ray (Date of X-ray - Date of birth)/365.25. Ratio of BA/CA was calculated. (NCT02993926)
Timeframe: No longer treated for CPP group - Month: 27 (766- 855 days) post last dose of Enantone; Treated with Non-Enantone GnRHa group - Month 18 (496-585 days) post last dose of Enantone
| Intervention | percentage of participants (Number) |
|---|---|
| Follow Up: Participants No Longer Treated for CPP (Female) | 100 |
| FollowUp:Treated With Non-Enantone GnRHa After Enantone-Female | 100 |
Estradiol or Testosterone, suppressed below Upper Limit Value (ULV) were reported. The ULV for estradiol and testosterone were 20 pg/mL and 7.34 nmol/L, respectively. (NCT02993926)
Timeframe: The mean duration of Enantone exposure was 22.3 months, ranging from 10.1 to 52.4 months
| Intervention | percentage of participants (Number) |
|---|---|
| Treatment Phase: Enantone (Male) | 100 |
| Treatment Phase: Enantone (Female) | 74.8 |
Estradiol or Testosterone, suppressed below Upper Limit Value (ULV) were reported. The ULV for estradiol and testosterone were 20 pg/mL and 7.34 nmol/L, respectively. (NCT02993926)
Timeframe: No longer treated for CPP group-Month: 27 (766-855 days) post last dose of Enantone; Treated with Non-Enantone GnRHa group-Month 21 (586-675 days) post last dose of Enantone
| Intervention | percentage of participants (Number) |
|---|---|
| Follow Up: Participants No Longer Treated for CPP (Female) | 0 |
| FollowUp:Treated With Non-Enantone GnRHa After Enantone-Female | 0 |
A TEAE is any untoward medical occurrence in a subject administered a medicinal product and which does not necessarily have to have a causal relationship with this treatment. An SAE is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. (NCT02993926)
Timeframe: Mean duration of follow-up=8.75 months (range: 1.9-29.5 months) for No longer treated for CPP group; 10.80 months (range: 2.8-20.5 months) for Treated with Non-Enantone GnRHa group after treatment with Enantone (while on another GnRHa)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| TEAE | SAE | |
| Follow Up: Participants No Longer Treated for CPP (Female) | 10 | 0 |
| Follow UP: Participants No Longer Treated for CPP (Male) | 0 | 0 |
| FollowUp:Treated With Non-Enantone GnRHa After Enantone-Female | 9 | 0 |
A TEAE is any untoward medical occurrence in a subject administered a medicinal product and which does not necessarily have to have a causal relationship with this treatment. An SAE is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. (NCT02993926)
Timeframe: During treatment with and up to 30 days post last dose of Enantone (the mean duration of Enantone exposure was 22.3 months, ranging from 10.1 to 52.4 months)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| TEAE | SAE | |
| Treatment Phase: Enantone (Female) | 71 | 2 |
| Treatment Phase: Enantone (Male) | 4 | 0 |
Tanner Stage is used to measure pubertal development. Female (F) and male (M) participants were evaluated for breast development and genital development respectively and both genders for pubic hair development. Tanner Stage is based on progression through 5-stages. Participants were classified as having progression if either breast/genitals or pubic hair progression were present. Otherwise participant is classified as regression or no progression. (NCT02993926)
Timeframe: The mean duration of Enantone exposure was 22.3 months, ranging from 10.1 to 52.4 months
| Intervention | percentage of participants (Number) |
|---|---|
| Treatment Phase: Enantone (Male) | 0 |
| Treatment Phase: Enantone (Female) | 79.7 |
The LH suppression is defined as peak LH ≤2 U/L for female and peak LH ≤2.7 U/L for male. The FSH suppression is defined as peak FSH ≤6.7 U/L for female and peak FSH ≤3.7 U/L for male. Post Stimulation Test, the peak values for LH and FSH suppression below Upper Limit Value (ULV) are reported. (NCT02993926)
Timeframe: The mean duration of Enantone exposure was 22.3 months, ranging from 10.1 to 52.4 months
| Intervention | percentage of participants (Number) | |
|---|---|---|
| LH (U/L) Peak Value ≤ ULV | FSH (U/L) Peak Value ≤ ULV | |
| Treatment Phase: Enantone (Female) | 98.1 | 100 |
| Treatment Phase: Enantone (Male) | 100 | 100 |
Testosterone level was summarized based on the percentage of participants with < 20 ng/dL, 20 to 50 ng/dL and > 50 ng/dL. (NCT03035032)
Timeframe: Month 12
| Intervention | Percentage of participants (Number) | ||
|---|---|---|---|
| < 20 ng/dL | 20 - 50 ng/dL | > 50 ng/dL | |
| Leuprolide Acetate 22.5 mg | 51.4 | 12.4 | 1.9 |
EQ-5D-5L is a standardized instrument for use as a measure of health outcome and provides a simple descriptive profile and a single index value for health status. EQ-5D-5L is designed for self-completion by respondents and consists of 2 pages comprising the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension of the EQ-5D-5L has 5 levels (no problems, slight problems, moderate problems, severe problems, and extreme problems) and the participants was asked to indicate his health state by ticking the box with the most appropriate statement. Index scores were generated using US value sets. Scores ranged from -0.109 to 1. Higher scores indicate better health state. (NCT03035032)
Timeframe: Baseline, months 6, 12 and 18
| Intervention | Score on a scale (Mean) | ||
|---|---|---|---|
| Month 6 | Month 9 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 0.0017 | -0.0047 | -0.0191 |
The EQ5D02-EQ-VAS is a vertical VAS with values between 0 (worst imaginable health) and 100 (best imaginable health), on which participants provide a global assessment of their health. Higher score indicate better health state. (NCT03035032)
Timeframe: Baseline, months 6, 12 and 18
| Intervention | Score on a scale (Mean) | ||
|---|---|---|---|
| Month 6 | Month 9 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 1.3 | 2.1 | 2.0 |
"An AE was defined as any untoward medical occurrence in a participant administered a study drug or had undergone study procedures that did not necessarily have a causal relationship with this treatment.~An AE was considered to be serious if, in the view of either the investigator or sponsor, it resulted in any of the following outcomes: resulted in death, was life-threatening, resulted in persistent or significant disability/incapacity or substantial disruption of the ability to conduct normal life functions, resulted in congenital anomaly or birth defect, required inpatient hospitalization or led to prolongation of hospitalization, other medically important events.~Drug-related AEs are AEs where causal relationships were at least a reasonable possibility as determined by the investigator." (NCT03035032)
Timeframe: From first dose of study drug up to 18 months
| Intervention | Participants (Number) | |
|---|---|---|
| Drug-related adverse event | Drug-related serious adverse event | |
| Leuprolide Acetate 22.5 mg | 15 | 2 |
"PSA percent reduction (%) = ([PSA tested- baseline PSA]/baseline PSA)*100%. PSA level was summarized based on time to PSA progression and PSA percent reduction by ≥ 50% with respect to the level at baseline. Participants with more than 1 qualifying PSA progression were counted only once, and the earlier progression was accounted for time to progression analysis.~PSA progression was defined as 25% or greater increase and an absolute increase of 2 ng/mL, and confirmed by a second value at least 3 weeks later." (NCT03035032)
Timeframe: Months 3, 6, 9, 12, 15 and 18
| Intervention | Percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | Month 15 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 89.2 | 91.7 | 91.6 | 94.2 | 96.9 | 88.8 |
"PSA percent reduction (%) = ([PSA tested- baseline PSA]/baseline PSA)*100%. PSA level was summarized based on time to PSA progression and PSA percent reduction by ≥ 90%, with respect to the level at baseline. Participants with more than 1 qualifying PSA progression were counted only once, and the earlier progression was accounted for time to progression analysis.~PSA progression was defined as 25% or greater increase and an absolute increase of 2 ng/mL, and confirmed by a second value at least 3 weeks later." (NCT03035032)
Timeframe: Months 3, 6, 9, 12, 15 and 18
| Intervention | Percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | Month 15 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 69.6 | 77.1 | 77.1 | 81.2 | 79.7 | 68.5 |
"PSA percent reduction (%) = ([PSA tested- baseline PSA]/baseline PSA)*100%. PSA level was summarized based on time to PSA progression and PSA percent reduction by ≥ 30% with respect to the level at baseline. Participants with more than 1 qualifying PSA progression were counted only once, and the earlier progression was accounted for time to progression analysis.~PSA progression was defined as 25% or greater increase and an absolute increase of 2 nanogram per milliliter (ng/mL), and confirmed by a second value at least 3 weeks later." (NCT03035032)
Timeframe: Months 3, 6, 9, 12, 15 and 18
| Intervention | Percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | Month 15 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 96.1 | 93.8 | 92.8 | 97.1 | 98.4 | 91.0 |
Testosterone level was summarized based on the percentage of participants with < 20 ng/dL, 20 to 50 ng/dL and > 50 ng/dL. (NCT03035032)
Timeframe: Month 18
| Intervention | Percentage of participants (Number) | ||
|---|---|---|---|
| < 20 ng/dL | 20 - 50 ng/dL | > 50 ng/dL | |
| Leuprolide Acetate 22.5 mg | 61.9 | 16.2 | 1.9 |
EQ-5D-5L is a standardized instrument for use as a measure of health outcome and provides a simple descriptive profile and a single index value for health status. EQ-5D-5L is designed for self-completion by respondents and consists of 2 pages comprising the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension of the EQ-5D-5L has 5 levels (no problems, slight problems, moderate problems, severe problems, and extreme problems) and the participant was asked to indicate his health state by ticking the box with the most appropriate statement. Index scores were generated using UK value sets. Scores ranged from -0.594 to 1. Higher scores indicate better health state. (NCT03035032)
Timeframe: Baseline, months 6, 12 and 18
| Intervention | Score on a scale (Mean) | ||
|---|---|---|---|
| Month 6 | Month 9 | Month 18 | |
| Leuprolide Acetate 22.5 mg | 0.0055 | -0.0051 | -0.0259 |
EQ-5D-5L is a standardized instrument for use as a measure of health outcome and provides a simple descriptive profile and a single index value for health status. EQ-5D-5L is designed for self-completion by respondents and consists of 2 pages comprising the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension of the EQ-5D-5L has 5 levels (no problems, slight problems, moderate problems, severe problems, and extreme problems) and the participant was asked to indicate his health state by ticking the box with the most appropriate statement. Index scores were generated using Japan value sets. Scores ranged from -0.111 to 1. Higher scores indicate better health state. (NCT03035032)
Timeframe: Baseline, months 6, 12 and 18
| Intervention | Score on a scale (Mean) | ||
|---|---|---|---|
| Month 6 | Month 12 | Month 18 | |
| Leuprolide Acetate 22.5 mg | -0.0047 | -0.0093 | -0.0262 |
EORTC QLQ-PR25 is a prostate cancer module for the assessment of health-related quality of life (HRQoL). EORTC QLQ-PR25 is designed for self-completion by respondents and assesses urinary symptoms, bowel symptoms, treatment-related symptoms and sexual activity and functioning. The rule of scoring for EORTC QLQ-PR25 follows instruction of EORTC QLQ-PR25 Scoring Manual 2.0. It consist of 25 questions distributed on 6 domains: urinary symptoms (8 items), incontinence aid (1 item), bowel symptoms (4 items), hormonal treatment-related symptoms (HTRS) (6 items), sexual activity (2 items), and sexual functioning (4 items). Questions used 4 point scale (1 'Not at all' to 4 'Very much'). All raw domain scores are linearly transformed to a 0-100 scale, with higher scores reflecting either more symptoms (urinary, bowel, hormonal treatment-related symptoms) or higher levels of activity or functioning (sexual). (NCT03035032)
Timeframe: Baseline, months 6, 12 and 18
| Intervention | Score on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 6: Urinary Symptoms | Week 6: Incontinence Aid | Week 6: Bowel Symptoms | Week 6: HTRS | Week 6: Sexually Active | Week 6: Sexual Function | Week 12: Urinary Symptoms | Week 12: Incontinence Aid | Week 12: Bowel Symptoms | Week 12: HTRS | Week 12: Sexually Active | Week 12: Sexual Function | Week 18: Urinary Symptoms | Week 18: Incontinence Aid | Week 18: Bowel Symptoms | Week 18: HTRS | Week 18: Sexually Active | Week 18: Sexual Function | |
| Leuprolide Acetate 22.5 mg | -4.84 | -5.21 | -2.17 | 3.27 | -6.08 | -1.44 | -6.93 | -11.11 | -2.66 | 2.14 | -5.07 | -2.99 | -4.06 | 1.67 | 0.31 | 4.68 | -3.54 | -8.52 |
Time to PSA progression was defined as (date of ≥25 percentage (%) increase and ≥ 2 ng/mL absolute increase) - (date of first administration of ELIGARD 22.5 mg)/30, where PSA progression was defiined as 25% or greater increase and an absolute increase of 2 ng/mL, and confirmed by a second value at least 3 weeks later. Participants with more than 1 qualifying PSA progression were counted only once, and the earlier progression was accounted for time to progression analysis. (NCT03035032)
Timeframe: From first dose of study drug up to PSA progression (18 months)
| Intervention | Months (Median) |
|---|---|
| Leuprolide Acetate 22.5 mg | 8.80 |
To investigate the time from an undetectable Prostate-specific antigen (≤0.2 ng/mL) until the Prostate-specific antigen is >0.2 over two time-points. (NCT03043807)
Timeframe: 3 years
| Intervention | Month (Median) |
|---|---|
| Chemohormonal and Definitive Therapy After Prostatectomy | NA |
Blood samples were collected from participants for hormonal measurements. (NCT03085095)
Timeframe: Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)
| Intervention | percent change (Mean) | ||
|---|---|---|---|
| Week 5 Day 1 (Day 29) | Week 25 Day 1 (Day 169) | Week 49 Day 1 (Day 337) | |
| Leuprolide Acetate | -81.95 | -85.45 | -87.56 |
| Relugolix | -87.61 | -88.06 | -88.23 |
Subscale assessments of urinary symptoms (9 items) and bowel symptoms (4 items) from the EORTC-QLQ-PR25 25-item prostate cancer module of the EORTC are presented. Questions used 4 point scale (1 'Not at all' to 4 'Very much'). All raw domain scores are linearly transformed to a 0-100 scale. A decrease in symptom scores indicates improvement (lower level of symptoms/problems). (NCT03085095)
Timeframe: Baseline, Week 49 Day 1 (Day 337)
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Urinary symptoms | Incontinence aid use | Bowel symptoms | |
| Leuprolide Acetate | -0.4 | 0.0 | 2.0 |
| Relugolix | 1.1 | 1.0 | 1.2 |
Castration rate defined as the cumulative probability of testosterone suppression to < 20 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: At Week 1 Day 4 (Day 4)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 6.92 |
| Leuprolide Acetate | 0.0 |
The EORTC QLQ-C30 core measurement was used to capture distal outcomes, including physical, social functioning, and overall health-related quality of life. The questionnaire incorporates 30 questions comprising nine multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social); 3 symptom scales (fatigue, pain, and nausea and vomiting); and a global health and quality of life scale. All raw domain scores are linearly transformed to a 0-100 scale. All domains except for the global health and quality are presented. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems). (NCT03085095)
Timeframe: Baseline, Week 49 Day 1 (Day 337)
| Intervention | score on a scale (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical functioning | Role functioning | Emotional functioning | Cognitive functioning | Social functioning | Fatigue | Nausea and vomiting | Pain | Dyspnoea | Insomnia | Appetite loss | Constipation | Diarrhoea | Financial difficulties | |
| Leuprolide Acetate | -4.4 | -5.6 | -0.5 | -3.8 | -4.0 | 7.0 | 0.8 | 4.0 | 7.9 | 4.8 | -0.6 | 3.5 | 1.4 | 0.1 |
| Relugolix | -4.6 | -6.2 | 0.5 | -3.7 | -2.7 | 6.1 | 0.2 | 1.7 | 5.3 | 4.8 | -0.6 | 1.4 | 2.0 | 0.2 |
Subscales for assessment of hormonal treatment-related symptoms (6 items) and sexual activity and function (6 items) from the EORTC-QLQ-PR25 25-item prostate cancer module of the EORTC are presented. Questions used 4 point scale (1 'Not at all' to 4 'Very much'). All raw domain scores are linearly transformed to a 0-100 scale. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems). (NCT03085095)
Timeframe: Baseline, Week 49 Day 1 (Day 337)
| Intervention | score on a scale (Mean) | ||
|---|---|---|---|
| Sexual activity | Sexual functioning | Hormonal treatment-related symptoms | |
| Leuprolide Acetate | 10.8 | -10.4 | 11.4 |
| Relugolix | 13.9 | -9.0 | 10.6 |
Defined as the proportion of participants with PSA concentration < 0.02 ng/milliliter (mL).The rate was estimated by the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 25 Day 1 (Day 169)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 20.7 |
| Leuprolide Acetate | 20.8 |
The Tmax of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose PK was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks. (NCT03085095)
Timeframe: Predose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2
| Intervention | hours (Median) |
|---|---|
| Relugolix Single-Dose | 1.03 |
| Relugolix Repeat-Dose | 0.983 |
Sustained profound castration rate was defined as the cumulative probability of testosterone suppression to < 20 ng/dL. The rate was estimated by the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 5 Day 1 (Day 29) through Week 49 Day 1 (Day 337)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 81.6 |
| Leuprolide Acetate | 68.6 |
Sustained profound castration rate was defined as the cumulative probability of testosterone suppression to < 20 ng/dL. The rate was estimated by the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 25 Day 1 (Day 169) through Week 49 Day 1 (Day 337)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 84.6 |
| Leuprolide Acetate | 87.5 |
"Sustained castration rate defined as the cumulative probability of testosterone suppression to < 50 nanogram (ng)/deciliter (dL). The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants.~The lower bound of the 95% confidence interval (CI) for the cumulative probability of sustained testosterone suppression in the relugolix treatment group must have been ≥ 90% to meet evaluation criteria for efficacy." (NCT03085095)
Timeframe: From Week 5 Day 1 (Day 29) to Week 49 Day 1 (Day 337)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 96.7 |
| Leuprolide Acetate | 88.8 |
PSA progression was defined as the first increase in PSA of 25% or greater and 2 ng/mL or greater above the nadir with confirmation by a second consecutive PSA measurement at least 3 weeks later. For participants without declining PSA from baseline, a PSA increase of ≥ 25% and ≥ 2 ng/mL from baseline beyond 12 weeks was considered PSA progression. The rate of progression-free survival was estimated using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 49 Day 1 (Day 337)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 89.31 |
| Leuprolide Acetate | 89.50 |
PSA response defined as > 50% reduction in PSA from baseline. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 5 Day 1 (Day 29)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 94.5 |
| Leuprolide Acetate | 79.2 |
PSA response defined as > 50% reduction in PSA from baseline. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 3 Day 1 (Day 15)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 80.1 |
| Leuprolide Acetate | 20.1 |
Castration rate defined as the cumulative probability of testosterone suppression to < 20 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 3 Day 1 (Day 15)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 78.38 |
| Leuprolide Acetate | 0.98 |
MACE were defined as nonfatal myocardial infarction, nonfatal stroke, and death from any cause. (NCT03085095)
Timeframe: From Week 5 Day 1 (Day 29) to Week 49 Day 1 (Day 337)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 2.9 |
| Leuprolide Acetate | 6.2 |
The Cmax of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose pharmacokinetics (PK) was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks. (NCT03085095)
Timeframe: Predose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2
| Intervention | ng/mL (Geometric Mean) |
|---|---|
| Relugolix Single-Dose | 125 |
| Relugolix Repeat-Dose | 46.4 |
To evaluate the effect of relugolix and leuprolide acetate on FSH suppression. (NCT03085095)
Timeframe: Week 25 Day 1 (Day 169)
| Intervention | IU/L (Mean) |
|---|---|
| Relugolix | 1.72 |
| Leuprolide Acetate | 5.95 |
Confirmed PSA response defined as > 50% reduction in PSA from baseline at Week 3 Day 1 followed with confirmation at Week 5 Day 1. (NCT03085095)
Timeframe: Week 3 Day 1 (Day 15) and Week 5 Day 1 (Day 29)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 79.4 |
| Leuprolide Acetate | 19.8 |
The EORTC QLQ-C30 core measurement was used to capture distal outcomes, including physical, social functioning, and overall health-related quality of life. The questionnaire incorporates 30 questions comprising nine multi-item scales: 5 functional scales (physical, role, cognitive, emotional, and social); 3 symptom scales (fatigue, pain, and nausea and vomiting); and a global health and quality of life scale. All raw domain scores are linearly transformed to a 0-100 scale. The global health and quality of life domain is presented. An increase in activity or functioning scores indicates improvement (higher/healthier level of functioning) and a decrease in symptom scores indicates improvement (lower level of symptoms/problems). (NCT03085095)
Timeframe: Baseline, Week 49 Day 1 (Day 337)
| Intervention | score on a scale (Mean) |
|---|---|
| Relugolix | -3.8 |
| Leuprolide Acetate | -3.6 |
The EuroQoL EQ-5D-5L comprises 5 dimensions (mobility, self-care, usual activities, pain/discomfort, and anxiety/depression). Each dimension has 5 levels: no problems (1 as numerical score), slight problems (2 as numerical score), moderate problems (3 as numerical score), severe problems (4 as numerical score), and extreme problems (5 as numerical score). The total score ranges from 0 to 100. A decrease in score indicates improvement. (NCT03085095)
Timeframe: Baseline, Week 49 Day 1 (Day 337)
| Intervention | score on a scale (Mean) |
|---|---|
| Relugolix | -1.5 |
| Leuprolide Acetate | -2.7 |
The AUC0-τ of relugolix was determined for single and repeat doses in subsets of participants from Japan. Single dose PK was assessed on Day 1 following an initial 360 mg dose of relugolix. Repeat dose PK was assessed following repeat dosing of relugolix 120 mg once daily for 2 weeks. (NCT03085095)
Timeframe: Predose and 0.5, 1, 2, 4, 6, 8, 12, and 24 hours postdose on Day 1 and Week 2
| Intervention | ng⸳hr/mL (Geometric Mean) |
|---|---|
| Relugolix Single-Dose | 663 |
| Relugolix Repeat-Dose | 373 |
Castration rate was defined as the cumulative probability of testosterone suppression to < 50 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 1 Day 4 (Day 4)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 56.04 |
| Leuprolide Acetate | 0.00 |
Castration rate was defined as the cumulative probability of testosterone suppression to < 50 ng/dL. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Week 3 Day 1 (Day 15)
| Intervention | percentage of participants (Number) |
|---|---|
| Relugolix | 98.71 |
| Leuprolide Acetate | 12.05 |
Blood samples were collected from participants for hormonal measurements. (NCT03085095)
Timeframe: Week 1 Day 4 (Day 4), Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)
| Intervention | Percent change (Mean) | |||
|---|---|---|---|---|
| Week 1 Day 4 (Day 4) | Week 5 Day 1 (Day 29) | Week 25 Day 1 (Day 169) | Week 49 Day 1 (Day 337) | |
| Leuprolide Acetate | 147.71 | -82.67 | -93.45 | -95.14 |
| Relugolix | -88.25 | -94.54 | -93.93 | -91.54 |
Blood samples were collected from participants for hormonal measurements. (NCT03085095)
Timeframe: Week 1 Day 4 (Day 4), Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)
| Intervention | percent change (Mean) | |||
|---|---|---|---|---|
| Week 1 Day 4 (Day 4) | Week 5 Day 1 (Day 29) | Week 25 Day 1 (Day 169) | Week 49 Day 1 (Day 337) | |
| Leuprolide Acetate | -4.74 | -67.73 | -47.53 | -47.23 |
| Relugolix | -62.59 | -90.80 | -86.32 | -79.39 |
The cumulative probability of testosterone recovery back to > 280 ng/dL (lower limit of the normal range), back to ≥ 50 ng/dL (definition of castration), and back to > 280 ng/dL or baseline at 90 days after drug discontinuation was assessed. The rate was estimated for each treatment group using the Kaplan-Meier method and reported as percentage of participants. (NCT03085095)
Timeframe: Day 90 follow-up
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| ≥ 50 ng/dL | > 280 ng/dL | > Baseline level or 280 ng/dL | |
| Leuprolide Acetate | 10.12 | 3.23 | 3.23 |
| Relugolix | 93.01 | 53.93 | 54.73 |
Blood samples were collected from participants for hormonal measurements. (NCT03085095)
Timeframe: Week 5 Day 1 (Day 29), Week 25 Day 1 (Day 169), and Week 49 Day 1 (Day 337)
| Intervention | percent change (Mean) | ||
|---|---|---|---|
| Week 5 Day 1 (Day 29) | Week 25 Day 1 (Day 169) | Week 49 Day 1 (Day 337) | |
| Leuprolide Acetate | -1.21 | 3.59 | 2.59 |
| Relugolix | 1.08 | 7.24 | 6.54 |
The pharmacokinetic (PK) parameters of the first 9 patients enrolled at Dana-Farber Cancer Institute will be determined using noncompartmental methods with WinNonLin version 5.2. Maximum blood concentration (Cmax) will be determined by visual inspection. Due to the premature termination of the study, only 9 patients were evaluated. The PK samples were collected on Days 1 and 2 of the first two treatment cycles. (NCT03093272)
Timeframe: Cycle 1, 2: During infusion at pre-dose, 15 minutes and 30 minutes post-dose, end of dose, and 0.5, 1, 1.5, 2, 4, 6, 8, 24 hours post dose.
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Cycle 1 | Cycle 2 | |
| Apalutamide Combined With Docetaxel | 2415 | 1641 |
The maximum percent PSA change (rise or fall) from baseline to after 12 weeks on study. For patients who discontinue on or before the 12 week assessment or for whom the 12 week assessment is missing, the last observation prior to the week 12 assessment will be utilized. Patients with no post-baseline PSA data will be excluded from the summary. (NCT03093272)
Timeframe: PSA was measured on Cycle 1 Day 1 (Baseline) and at 12 weeks on treatment.
| Intervention | percent (Median) |
|---|---|
| Apalutamide Combined With Docetaxel | 13.0 |
"Progression free survival (PFS) is defined as the time from treatment initiation until the occurrence of one of the following:~A participant was considered to have progressed by bone scan if~the first bone scan with greater than or equal to (≥) 2 new lesions compared to baseline was observed in less than (<) 12 weeks from study drug initiation and was confirmed by a second bone scan taken ≥6 weeks later showing ≥2 additional new lesions (a total of ≥4 new lesions compared to baseline);~the first bone scan with ≥2 new lesions compared to baseline was observed in ≥12 weeks from study drug initiation and the new lesions were verified on the next bone scan ≥6 weeks later (a total of ≥2 new lesions compared to baseline);~Progression of soft tissue lesions measured by computerized tomography (CT) or magnetic resonance imaging (MRI) by RECIST v. 1.1; or~Death from any cause." (NCT03093272)
Timeframe: Disease was evaluated radiologically at baseline and every 12 weeks on treatment; PFS follow up was up to 9.4 months
| Intervention | months (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Participant 1 | Participant 2 | Participant 3 | Participant 4 | Participant 5 | Participant 6 | Participant 7 | Participant 8 | Participant 9 | |
| Apalutamide Combined With Docetaxel | 5.6 | NA | 5.6 | 8.1 | 1.8 | 4.8 | 5.1 | NA | 9.4 |
Overall Survival (OS) is defined as the time from trial treatment start to death due to any cause, or censored at date last known alive. (NCT03093272)
Timeframe: Measured from end of study treatment to death due to any cause; OS measured as 22.4 months
| Intervention | months (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Participant 1 | Participant 2 | Participant 3 | Participant 4 | Participant 5 | Participant 6 | Participant 7 | Participant 8 | Participant 9 | |
| Apalutamide Combined With Docetaxel | 22.4 | 4.2 | 21.2 | 16.8 | 1.8 | 9.0 | 10.1 | 5.9 | 12.2 |
The area under the blood concentration-time curve (linear trapezoidal rule) will be determined between 0-24 hours (AUC0-24). The PK samples were collected during the first two days of cycles 1 and 2. (NCT03093272)
Timeframe: Cycle 1, 2: During infusion at pre-dose, 15 minutes and 30 minutes post-dose, end of dose, and 0.5, 1, 1.5, 2, 4, 6, 8, 24 hours post dose.
| Intervention | ng•h/mL (Mean) | |
|---|---|---|
| Cycle 1 | Cycle 2 | |
| Apalutamide Combined With Docetaxel | 3406 | 3095 |
Adverse drug reaction refers to adverse events related to the administered drug. (NCT03209492)
Timeframe: Up to Week 24
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprorelin Acetate 22.5 mg | 2.74 |
(NCT03209492)
Timeframe: Up to Week 24
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprorelin Acetate 22.5 mg | 4.27 |
Adverse drug reaction refers to adverse events related to the administered drug. (NCT03209518)
Timeframe: Up to Week 24
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprorelin Acetate 22.5 mg | 5.48 |
(NCT03209518)
Timeframe: Up to Week 24
| Intervention | Percentage of Participants (Number) |
|---|---|
| Leuprorelin Acetate 22.5 mg | 6.45 |
The percentage of subjects with a serum testosterone concentration suppressed to castrate levels (≤ 50 ng/dL) from Day 28 through Day 168. (NCT03261999)
Timeframe: 168 days
| Intervention | Percentage of participants (Number) |
|---|---|
| Leuprolide Mesylate 25mg | 97.9 |
Determining the safety and tolerability of LMIS 25 mg based on adverse events (AEs). (NCT03261999)
Timeframe: 168 days
| Intervention | subjects (Number) | ||
|---|---|---|---|
| TEAE | Drug-related TEAE | SAE | |
| Leuprolide Mesylate 25mg | 90 | 53 | 9 |
Growth rate (height in centimeter/year) was calculated both prior to treatment in the study and during the study. For Baseline calculation a historical measurement of height at least 6 months prior to Screening and the Screening value was used. (NCT03695237)
Timeframe: Baseline and Weeks 4, 12, 20, 24, 44, and 48
| Intervention | cm/year (Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 | Week 12 | Week 20 | Week 24 | Week 44 | Week 48 | |
| Leuprolide Acetate - Overall | -0.8 | -2.0 | -2.5 | -2.4 | -2.6 | -2.3 |
| Leuprolide Acetate - Previously Treated | -0.6 | -0.6 | -0.5 | -0.5 | -0.4 | -0.3 |
| Leuprolide Acetate - Treament Naïve | -0.9 | -2.9 | -3.8 | -3.7 | -4.1 | -3.5 |
Estradiol concentrations were measured from blood samples taken at each study visit prior to stimulation testing (and prior to study drug administration at Weeks 24 and 48). (NCT03695237)
Timeframe: Weeks 12, 20, 24, 44, and 48
| Intervention | percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| Week 12 | Week 20 | Week 24 | Week 44 | Week 48 | |
| Leuprolide Acetate - Overall | 97.4 | 97.4 | 97.4 | 100.0 | 100.0 |
| Leuprolide Acetate - Previously Treated | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 |
| Leuprolide Acetate - Treament Naïve | 95.5 | 95.7 | 95.2 | 100.0 | 100.0 |
Testosterone concentrations were measured from blood samples taken at each study visit prior to stimulation testing (and prior to study drug administration for Weeks 24 and 48). (NCT03695237)
Timeframe: Weeks 12, 20, 24, 44, and 48
| Intervention | percentage of participants (Number) | ||||
|---|---|---|---|---|---|
| Week 12 | Week 20 | Week 24 | Week 44 | Week 48 | |
| Leuprolide Acetate - Overall | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 |
| Leuprolide Acetate - Previously Treated | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 |
| Leuprolide Acetate - Treament Naïve | 100.0 | 100.0 | 100.0 | 100.0 | 100.0 |
"Breast development in females and testicular volume or genital development in males was assessed using modified Tanner staging, on a scale from Stage 1 (prepubertal) to Stage 5 (adult characteristics).~Females: Suppression is defined as regression or no progression of breast development according to modified Tanner staging.~Males: Suppression is defined as regression or no progression in testicular volume and genital staging according to modified Tanner staging." (NCT03695237)
Timeframe: Weeks 24 and 48
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Females: Week 24 | Females: Week 48 | Males: Week 24 | Males: Week 48 | |
| Leuprolide Acetate - Overall | 92.7 | 90.2 | 50.0 | 75.0 |
| Leuprolide Acetate - Previously Treated | 94.1 | 88.2 | 0 | 100 |
| Leuprolide Acetate - Treament Naïve | 91.7 | 91.7 | 66.7 | 66.7 |
"Bone age was assessed from radiographs of the hand and wrist by a central imaging vendor using the BoneXpert automated system.~A ratio less than 1 indicates less advancement of bone age compared to chronological age." (NCT03695237)
Timeframe: Baseline and Weeks 24 and 48
| Intervention | ratio (Mean) | |
|---|---|---|
| Week 24 | Week 48 | |
| Leuprolide Acetate - Overall | 0.6 | 0.5 |
| Leuprolide Acetate - Previously Treated | 0.5 | 0.2 |
| Leuprolide Acetate - Treament Naïve | 0.7 | 0.6 |
"Suppression of GnRHa-stimulated luteinizing hormone (LH) was measured using a peak GnRHa stimulation test, performed using subcutaneous injection with an aqueous formulation of leuprolide acetate at 20 µg/kg.~Peak stimulated LH was calculated by taking the maximum LH concentrations measured from blood samples taken at 30 or 60 min following the GnRHa stimulation test.~Suppression of GnRHa-stimulated luteinizing hormone is defined as peak stimulated LH less than 4 mIU/mL." (NCT03695237)
Timeframe: Weeks 12, 20, 44, and 48 (prior to Week 48 dose); samples for LH measurement were taken 30 and 60 minutes after the stimulation test injection.
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Week 12 | Week 20 | Week 44 | Week 48 | |
| Leuprolide Acetate - Overall | 86.7 | 88.9 | 88.9 | 88.9 |
| Leuprolide Acetate - Previously Treated | 83.3 | 94.4 | 88.9 | 83.3 |
| Leuprolide Acetate - Treament Naïve | 88.9 | 85.2 | 88.9 | 92.6 |
"Suppression of GnRHa-stimulated luteinizing hormone (LH) was measured using a peak GnRHa stimulation test, performed using subcutaneous injection with an aqueous formulation of leuprolide acetate at 20 µg/kg.~Peak stimulated LH was calculated by taking the maximum LH concentrations measured from blood samples taken at 30 or 60 min following the GnRHa stimulation test.~Suppression of GnRHa-stimulated luteinizing hormone is defined as peak stimulated LH less than 4 mIU/mL." (NCT03695237)
Timeframe: Week 24 (prior to the Week 24 dose); samples for LH measurement were taken 30 and 60 minutes after the stimulation test injection.
| Intervention | percentage of participants (Number) |
|---|---|
| Leuprolide Acetate - Previously Treated | 94.4 |
| Leuprolide Acetate - Treament Naïve | 81.5 |
| Leuprolide Acetate - Overall | 86.7 |
"This outcome measure determines the extent to which irritability is characterized by dysfunctional threat processing during reproductive hormone challenge relative to baseline in HS+ and HS-. By examining amygdala-medial prefrontal cortex (PFC) Blood-oxygen-level-dependent (BOLD) connectivity in response to threatening faces on the implicit emotion face processing fMRI task in HS+ (compared with HS-) during hormone challenge relative to baseline.~The implicit emotion face processing task asks participants to identify the gender of angry, happy, and fearful faces at 50%, 100% and 150% emotion intensity presented in random order for 2000 milliseconds followed by jittered fixation. Trials appear in 3 blocks, generating 30 trials of each emotion at each intensity and 90 neutral face emotion trials." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | arbitrary units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.0533 | 0.00804 |
| Hormone Sensitive Women (HS+) | 0.0174 | -0.0114 |
"This outcome measure determines the extent to which irritability is characterized by dysfunctional threat processing during reproductive hormone challenge relative to baseline in HS+ and HS- by examining threat attention bias assessed during the visual dot-probe paradigm.~The Visual Dot-Probe Paradigm asks participants to detect a target stimulus that is embedded in a matrix of distracting stimuli (e.g., a target stimulus, an angry face, might be embedded in a matrix of neutral distractor faces). Attention biases are inferred from faster response times to detect a threatening stimulus in a matrix of neutral stimuli relative to response time to detect neutral stimuli in neutral matrices. Thus, positive times reflect attention bias toward threat, whereas negative times reflect attention bias away from threat." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | attention bias in milliseconds (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 36.92 | -42.35 |
| Hormone Sensitive Women (HS+) | -0.57 | -9.04 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the left caudate in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.0077258 | -0.049988 |
| Hormone Sensitive Women (HS+) | -0.043943333 | 0.059099917 |
"This outcome measure determines the degree of irritability and reactive aggression in HS+ during hormone addback and its relationship to the target population. Irritability will be defined as score on the IDAS Ill Temper Scale. Reactive aggression will be defined as the number of point subtractions the participant makes during the Point Subtraction Aggression Paradigm.~The Point Subtraction Aggression Paradigm measures relational aggression (approach behavior) in response to frustration. In the task, participants are asked to press a button to ac" (NCT04051320)
Timeframe: Endpoint (week 6)
| Intervention | correlation coefficient (Number) |
|---|---|
| Hormone Sensitive Women (HS+) | 0.18 |
| Hormone Insensitive Women (HS-) | 0.03 |
"This outcome measure determines the degree of subcortical (amygdala, caudate, putamen, and nucleus accumbens) activation in HS+ during hormone addback and it's relationship to the target population. The activation in amygdala and ventral striatum (caudate, putamen, nucleus accumbens) regions of interest (ROIs) will be assessed during the Affective Posner Task.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: Endpoint (week 6)
| Intervention | correlation coefficient (Number) |
|---|---|
| Hormone Sensitive Women (HS+) | 0.47 |
This outcome measure determines the extent to which irritability is characterized by dysfunctional reward processing during reproductive hormone challenge in HS+ and HS- by examining the correlation between the Inventory of Depressive and Anxiety Symptoms (IDAS) Ill Temper (i.e., irritability) Scale and threat attention bias. (NCT04051320)
Timeframe: Endpoint (week 6)
| Intervention | correlation coefficient (Number) |
|---|---|
| Hormone Sensitive Women (HS+) | -0.35 |
| Hormone Insensitive Women (HS-) | 0.11 |
This outcome measure determines the extent to which irritability is characterized by dysfunctional reward processing during reproductive hormone challenge in HS+ and HS- by examining the correlation between the IDAS Ill Temper (i.e., irritability) Scale and amygdala-medial PFC connectivity in HS+. (NCT04051320)
Timeframe: Endpoint (week 6)
| Intervention | correlation coefficient (Mean) |
|---|---|
| Hormone Sensitive Women (HS+) | -0.13 |
| Hormone Insensitive Women (HS-) | 0.49 |
This outcome measure determines the extent to which irritability is characterized by dysfunctional reward processing during reproductive hormone challenge in HS+ and HS- by examining the correlation between the IDAS Ill Temper (i.e., irritability) Scale and amygdala-medial PFC connectivity in HS+. (NCT04051320)
Timeframe: Endpoint (week 6)
| Intervention | correlation coefficient (Number) |
|---|---|
| Hormone Sensitive Women (HS+) | -0.57 |
| Hormone Insensitive Women (HS-) | -0.08 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the left amygdala in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | -0.009866667 | -0.086876444 |
| Hormone Sensitive Women (HS+) | 0.005316917 | -0.047401917 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the left nucleus accumbens in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.0691907 | -0.072512 |
| Hormone Sensitive Women (HS+) | -0.028451818 | 0.031632727 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the left putamen in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.0383029 | -0.021029 |
| Hormone Sensitive Women (HS+) | -0.001223462 | 0.048155385 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the right amygdala in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.037334 | -0.15643 |
| Hormone Sensitive Women (HS+) | -0.04544 | 0.022654 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the right caudate in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.061407 | 0.0058011 |
| Hormone Sensitive Women (HS+) | -0.069919077 | 0.045146154 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the right nucleus accumbens in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.052685333 | -0.006394444 |
| Hormone Sensitive Women (HS+) | 0.044384167 | -0.005181667 |
"This outcome measure determines the extent to which HS+ is characterized by BOLD activation of the right putamen in response to frustrative non-reward (FNR) in the Affective Posner Task during hormone addback relative to baseline in the target population.~The Affective Posner Task tests whether HS+ is characterized by reduced subcortical activation in response to frustration. This task is divided into 3 runs: during Run 1 (practice run), participants receive accurate feedback about their performance on the task and do not win or lose money; during Run 2, participants receive accurate feedback about their performance and win or lose 50 cents per trial; and during Run 3 (frustration), participants are told they must respond accurately to win money, but participants are given feedback that they responded too slowly on 60% of accurate trials, regardless of their performance." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Arbitrary Units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.002542222 | -0.080736333 |
| Hormone Sensitive Women (HS+) | -0.007560692 | 0.036225385 |
"This outcome measure determines the extent to which irritability is characterized by dysfunctional threat processing during reproductive hormone challenge relative to baseline in HS+ and HS-. By examining amygdala-medial prefrontal cortex (PFC) connectivity in response to threatening faces on the implicit emotion face processing fMRI task in HS+ (compared with HS-) during hormone challenge relative to baseline.~The implicit emotion face processing task asks participants to identify the gender of angry, happy, and fearful faces at 50%, 100% and 150% emotion intensity presented in random order for 2000 milliseconds followed by jittered fixation. Trials appear in 3 blocks, generating 30 trials of each emotion at each intensity and 90 neutral face emotion trials." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | arbitrary units (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 0.0213 | 0.00111 |
| Hormone Sensitive Women (HS+) | 0.0247 | -0.0192 |
"This outcome measure determines the extent to which HS+ is characterized by reactive aggression during hormone addback relative to baseline in the target population. Reactive aggression will be defined as the number of point subtractions the participant makes during the Point Subtraction Aggression Paradigm.~Point Subtraction Aggression Paradigm measures relational aggression (approach behavior) in response to frustration. In the task, participants are asked to press a button to accrue money or press another button to subtract money from a (fictional) partner at no direct gain to themselves. Frustration is induced by periodic subtractions of their own money, which is attributed to the partner." (NCT04051320)
Timeframe: up to 6 weeks
| Intervention | Number of subtraction responses (Mean) | |
|---|---|---|
| Baseline (Visit 3) | Hormone Addback (Visit 6) | |
| Hormone Insensitive Women (HS-) | 129.20 | 54.90 |
| Hormone Sensitive Women (HS+) | 103.08 | 34.62 |
"Time (ms) between stimulus and response will be measured during the Monetary Incentive Delay (MID) task during the win trials during the estradiol intervention. During the MID task, participants need to select the correct response during win and lose conditions by pressing a button. Higher scores indicate a longer response time to the win trials. Change is defined by an average change score." (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | ms (Mean) |
|---|---|
| Estradiol | -9.0 |
This measures assesses individual disposition toward avoidance of activities during the estradiol intervention. The Behavioural Inhibition subscale of the Behavioural Inhibition Scale/Behavioral Activation Scale (BIS/BAS) assesses behavioural inhibition (BI) using participant self-reports. The minimum score on the BIS subscale is 7, maximum 28. Greater scores indicate greater behavioural inhibition. Change is defined by an average change score (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | score on a scale (Mean) |
|---|---|
| Estradiol | 0.90 |
Binge eating frequency is based on a daily diary of self-reported binge eating frequency. Scores can range from 0 to infinity as they represent a self-reported frequency. Subjects self-report the number of binge eating episodes they had each day. Higher numbers indicate more frequent binge eating episodes. Average weekly frequency will be determined based on daily reported binge eating frequency. Change is defined by an average change score. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of each intervention)
| Intervention | episodes/week (Mean) |
|---|---|
| Estradiol | -0.48 |
| Progesterone | 1.1 |
This measures assesses individual disposition toward engaging in activities during the estradiol intervention. Two BIS/BAS behavioural activation (BA) subscales will be used. The BA subscales used are Fun Seeking and Drive. Each subscale is summed to get the respective subscale scores. The minimum score on BA Fun Seeking and BA Drive are minimum 4 and maximum 16. Higher scores indicate greater behavioral activation. Change is defined by an average change score. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | score on a scale (Mean) | |
|---|---|---|
| Fun Seeking | Drive | |
| Estradiol | -0.10 | 0 |
Sensitivity to Punishment/Sensitivity to Reward Questionnaire will be used to measure reward sensitivity during estradiol intervention. The reward sensitivity subscale will be used, which is rated on a true/false scale with scores ranging 0-24. Higher scores indicate more sensitivity to reward. Change is defined by an average change score. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | score on a scale (Mean) |
|---|---|
| Estradiol | -0.80 |
During the estradiol intervention, participants will be asked to make a series of hypothetical choices between small, sooner (impulsive) vs. larger, later (self controlled) hypothetical monetary outcomes. k is a hyperbolic function with larger k values indicating more valuation of a larger delayed reward and smaller values indicating preference for more immediate, smaller rewards (more impulsivity). Change is defined as the average change in k. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | k value (Mean) |
|---|---|
| Estradiol | -0.0047 |
"Binge eating will be measured using the 8-item binge eating subscale of the Eating Pathology Symptoms Inventory (EPSI), which measures features of binge eating (e.g., consumption of large quantities of food, mindless eating) on a 5-point Likert scale from never to very often. The EPSI scale is designed to assess behavior over the past 28 days; however, to be sensitive to the timeframe of the present study, the instructions will be modified to ask participants to consider the past week. Items are summed for a scale score ranging from 0-32. Higher scores indicate more frequent experiences with binge eating behavior. Change is defined by an average change score." (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of each intervention)
| Intervention | score on a scale (Mean) |
|---|---|
| Estradiol | -0.60 |
| Progesterone | 0.89 |
"Behavioral response inhibition will be examined during a go/no-go computerized task during the estradiol intervention. Inhibitory control is defined by the response accuracy of the go no/go trials. Percent of errors is calculated as the number of go responses on a no/go trial divided by the total number of no/go trials. Fewer errors (go response on a no/go trial) indicates better inhibitory control. Change is defined by an average change score." (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | percentage of errors (Mean) |
|---|---|
| Estradiol | -0.094 |
This measures assesses individual disposition toward avoiding and engaging in activities during estradiol intervention. The BIS/BAS reward responsiveness subscale will be used. The minimum score on the BA Reward Responsiveness subscale is 5, maximum 20. Higher scores indicate greater reward responsiveness. Change is defined by an average change score. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | score on a scale (Mean) |
|---|---|
| Estradiol | 0.10 |
Pearson correlations between change in self-reported reward response and change in binge eating between baseline and estradiol intervention will be examined. Binge eating is defined as the sum score from the Eating Pathology Symptom Inventory (EPSI). Self-reported reward response is defined as the BAS reward responsiveness subscale score and the Sensitivity to Reward/Sensitivity to Punishment Questionnaire (SPSRQ) sensitivity to reward subscale score. Change in binge eating and change in reward response between baseline and estradiol intervention was calculated and a correlation conducted between change scores. (NCT04225221)
Timeframe: Baseline (Day 14 of baseline) to End of Intervention (Day 14 of intervention)
| Intervention | Pearson correlation coefficient (Number) | |
|---|---|---|
| BAS Reward Responsiveness | Sensitivity to Reward | |
| Estradiol | -0.146 | -0.132 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| 2-keto-4-methylvalerate alpha-ketoisocaproic acid: RN given refers to parent cpd. 4-methyl-2-oxopentanoate : A 2-oxo monocarboxylic acid anion that is the conjugate base of 4-methyl-2-oxopentanoic acid.. 4-methyl-2-oxopentanoic acid : A 2-oxo monocarboxylic acid that is pentanoic acid (valeric acid) substituted with a keto group at C-2 and a methyl group at C-4. A metabolite that has been found to accumulate in maple syrup urine disease. | 3.39 | 1 | 1 | 2-oxo monocarboxylic acid; branched-chain keto acid | algal metabolite; human metabolite |
| acetone methyl ketone : A ketone of formula RC(=O)CH3 (R =/= H). | 2.06 | 1 | 0 | ketone body; methyl ketone; propanones; volatile organic compound | EC 3.5.1.4 (amidase) inhibitor; human metabolite; polar aprotic solvent |
| quinacrine Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9. | 2.74 | 3 | 0 | acridines; aromatic ether; organochlorine compound; tertiary amino compound | antimalarial; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor |
| beta-alanine [no description available] | 2.07 | 1 | 0 | amino acid zwitterion; beta-amino acid | agonist; fundamental metabolite; human metabolite; inhibitor; neurotransmitter |
| betaine glycine betaine : The amino acid betaine derived from glycine. | 3.41 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| aminooxyacetic acid Aminooxyacetic Acid: A compound that inhibits aminobutyrate aminotransferase activity in vivo, thereby raising the level of gamma-aminobutyric acid in tissues.. (aminooxy)acetic acid : A member of the class of hydroxylamines that is acetic acid substituted at postion 2 by an aminooxy group. It is a compound which inhibits aminobutyrate aminotransferase activity in vivo, resulting in increased levels of gamma-aminobutyric acid in tissues. | 2.05 | 1 | 0 | amino acid; hydroxylamines; monocarboxylic acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor; EC 4.2.1.22 (cystathionine beta-synthase) inhibitor; nootropic agent |
| chlordecone [no description available] | 2.04 | 1 | 0 | cyclic ketone; organochlorine compound | insecticide; persistent organic pollutant |
| citric acid, anhydrous Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms. | 1.96 | 1 | 0 | tricarboxylic acid | antimicrobial agent; chelator; food acidity regulator; fundamental metabolite |
| coumarin 2H-chromen-2-one: coumarin derivative | 2.07 | 1 | 0 | coumarins | fluorescent dye; human metabolite; plant 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). | 1.96 | 1 | 0 | monohydroxybenzoic acid | algal metabolite; antifungal agent; antiinfective agent; EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor; keratolytic drug; plant hormone; plant 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. | 2.74 | 3 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| creatine [no description available] | 1.97 | 1 | 0 | glycine derivative; guanidines; zwitterion | geroprotector; human metabolite; mouse metabolite; neuroprotective agent; nutraceutical |
| 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. | 7.88 | 34 | 1 | 2-hydroxy monocarboxylic acid | algal metabolite; Daphnia magna metabolite |
| 5,6-dimethylbenzimidazole 5,6-dimethylbenzimidazole: RN given refers to parent cpd. 5,6-dimethylbenzimidazole : A dimethylbenzimidazole carrying methyl substituents at positions 5 and 6. | 2.04 | 1 | 0 | dimethylbenzimidazole | Escherichia coli metabolite; human metabolite |
| dimethyl sulfoxide Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents. | 3.12 | 5 | 0 | sulfoxide; volatile organic compound | alkylating agent; antidote; Escherichia coli metabolite; geroprotector; MRI contrast agent; non-narcotic analgesic; polar aprotic solvent; radical scavenger |
| hexachlorocyclohexane Lindane: An organochlorine insecticide made up of greater than 99% gamma-Hexachlorocyclohexane. It has been used as a pediculicide and scabicide, and shown to cause cancer.. beta-hexachlorocyclohexane : The beta-isomer of hexachlorocyclohexane. | 2.04 | 1 | 0 | chlorocyclohexane | |
| glycine [no description available] | 2.07 | 1 | 0 | alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid | EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical |
| glycerol Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil. | 2.57 | 2 | 0 | alditol; triol | algal metabolite; detergent; Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; solvent |
| glycolic acid glycolic acid: RN given refers to parent cpd. glycolic acid : A 2-hydroxy monocarboxylic acid that is acetic acid where the methyl group has been hydroxylated. | 3.77 | 3 | 0 | 2-hydroxy monocarboxylic acid; primary alcohol | keratolytic drug; metabolite |
| iodine Iodine: A nonmetallic element of the halogen group that is represented by the atomic symbol I, atomic number 53, and atomic weight of 126.90. It is a nutritionally essential element, especially important in thyroid hormone synthesis. In solution, it has anti-infective properties and is used topically.. diiodine : Molecule comprising two covalently bonded iodine atoms with overall zero charge.. | 3.38 | 1 | 1 | diatomic iodine | nutrient |
| inositol Inositol: An isomer of glucose that has traditionally been considered to be a B vitamin although it has an uncertain status as a vitamin and a deficiency syndrome has not been identified in man. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1379) Inositol phospholipids are important in signal transduction.. inositol : Any cyclohexane-1,2,3,4,5,6-hexol.. 1D-chiro-inositol : Belonging to the inositol family of compounds, D-chiro-inositol (DCI) is an isomer of glucose. It is an important secondary messenger in insulin signal transduction.. muco-inositol : An inositol that is cyclohexane-1,2,3,4,5,6-hexol having a (1R,2R,3r,4R,5S,6r)-configuration. | 3.41 | 1 | 0 | cyclitol; hexol | |
| melatonin [no description available] | 4.61 | 4 | 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. | 2.07 | 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 |
| nitrates Nitrates: Inorganic or organic salts and esters of nitric acid. These compounds contain the NO3- radical. | 3.38 | 1 | 1 | monovalent inorganic anion; nitrogen oxoanion; reactive nitrogen species | |
| nitrites Nitrites: Salts of nitrous acid or compounds containing the group NO2-. The inorganic nitrites of the type MNO2 (where M=metal) are all insoluble, except the alkali nitrites. The organic nitrites may be isomeric, but not identical with the corresponding nitro compounds. (Grant & Hackh's Chemical Dictionary, 5th ed) | 4.1 | 3 | 1 | monovalent inorganic anion; nitrogen oxoanion; reactive nitrogen species | human metabolite |
| 1-octanol 1-Octanol: A colorless, slightly viscous liquid used as a defoaming or wetting agent. It is also used as a solvent for protective coatings, waxes, and oils, and as a raw material for plasticizers. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed). octan-1-ol : An octanol carrying the hydroxy group at position 1. | 2.21 | 1 | 0 | octanol; primary alcohol | antifungal agent; bacterial metabolite; fuel additive; kairomone; plant metabolite |
| parathion [no description available] | 2.04 | 1 | 0 | C-nitro compound; organic thiophosphate; organothiophosphate insecticide | acaricide; agrochemical; avicide; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; mouse metabolite |
| pentachlorophenol PENTA: structure given in first source | 2.04 | 1 | 0 | aromatic fungicide; chlorophenol; organochlorine pesticide; pentachlorobenzenes | human xenobiotic metabolite |
| propylene glycol Propylene Glycol: A clear, colorless, viscous organic solvent and diluent used in pharmaceutical preparations.. propane-1,2-diol : The simplest member of the class of propane-1,2-diols, consisting of propane in which a hydrogen at position 1 and a hydrogen at position 2 are substituted by hydroxy groups. A colourless, viscous, hygroscopic, low-melting (-59degreeC) and high-boiling (188degreeC) liquid with low toxicity, it is used as a solvent, emulsifying agent, and antifreeze. | 2.1 | 1 | 0 | glycol; propane-1,2-diols | allergen; human xenobiotic metabolite; mouse metabolite; protic solvent |
| 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. | 2.46 | 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). | 1.97 | 1 | 0 | hydroxymethylpyridine; methylpyridines; monohydroxypyridine; vitamin B6 | cofactor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thymine [no description available] | 3.13 | 1 | 0 | pyrimidine nucleobase; pyrimidone | Escherichia coli metabolite; human metabolite; mouse metabolite |
| uracil 2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder | 3.38 | 1 | 1 | pyrimidine nucleobase; pyrimidone | allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; prodrug; Saccharomyces cerevisiae metabolite |
| urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives. | 1.98 | 1 | 0 | isourea; monocarboxylic acid amide; one-carbon compound | Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| menthol Menthol: A monoterpene cyclohexanol produced from mint oils. | 2.39 | 2 | 0 | p-menthane monoterpenoid; secondary alcohol | volatile oil component |
| 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. | 3.81 | 2 | 1 | monochlorobenzenes; N-arylpiperazine | drug metabolite; environmental contaminant; serotonergic agonist; xenobiotic |
| 1-anilino-8-naphthalenesulfonate 1-anilino-8-naphthalenesulfonate: RN given refers to parent cpd. 8-anilinonaphthalene-1-sulfonic acid : A naphthalenesulfonic acid that is naphthalene-1-sulfonic acid substituted by a phenylamino group at position 8. | 2.13 | 1 | 0 | aminonaphthalene; naphthalenesulfonic acid | fluorescent probe |
| amitrole Amitrole: A non-selective post-emergence, translocated herbicide. According to the Seventh Annual Report on Carcinogens (PB95-109781, 1994) this substance may reasonably be anticipated to be a carcinogen. (From Merck Index, 12th ed) It is an irreversible inhibitor of CATALASE, and thus impairs activity of peroxisomes.. amitrole : A member of the class of triazoles that is 1H-1,2,4-triazole substituted by an amino group at position 3. Used to control annual grasses and aquatic weeds (but not on food crops because it causes cancer in laboratory animals). Its use within the EU was banned from September 2017 on the grounds of potential groundwater contamination and risks to aquatic life; there have also been concerns about its endocrine-disrupting properties. | 2.04 | 1 | 0 | aromatic amine; triazoles | carotenoid biosynthesis inhibitor; EC 1.11.1.6 (catalase) inhibitor; herbicide |
| enprofylline enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. | 2.04 | 1 | 0 | oxopurine | anti-arrhythmia drug; anti-asthmatic drug; bronchodilator agent; non-steroidal anti-inflammatory drug |
| 4-aminopyridine [no description available] | 2.07 | 1 | 0 | aminopyridine; aromatic amine | avicide; orphan drug; potassium channel blocker |
| phenytoin [no description available] | 2.75 | 3 | 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. | 2.46 | 2 | 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. | 2.74 | 3 | 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. | 2.97 | 4 | 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) | 2.74 | 3 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohexamide Acetohexamide: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.. acetohexamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is replaced by a p-acetylphenylsulfonyl group, while a hydrogen attached to the other nitrogen is replaced by a cyclohexyl group. | 2.04 | 1 | 0 | acetophenones; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| 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. | 2.05 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| 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). | 2.74 | 3 | 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. | 4.34 | 4 | 1 | 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 | 2.04 | 1 | 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. | 2.04 | 1 | 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. | 2.45 | 2 | 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. | 2.04 | 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. | 2.04 | 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 | 2.44 | 2 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ametantrone ametantrone: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | ||
| 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. | 2.04 | 1 | 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. | 2.5 | 2 | 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. | 4.01 | 4 | 0 | dicarboximide; piperidones; substituted aniline | adrenergic agent; anticonvulsant; antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| theophylline [no description available] | 2.97 | 4 | 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 |
| 2-aminothiazole 2-aminothiazole: RN given refers to parent cpd; structure. 1,3-thiazol-2-amine : A primary amino compound that is 1,3-thiazole substituted by an amino group at position 2. | 2.04 | 1 | 0 | 1,3-thiazoles; primary amino compound | |
| 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. | 2.98 | 4 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| 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. | 2.75 | 3 | 0 | carbotricyclic compound; tertiary amine | adrenergic uptake inhibitor; antidepressant; environmental contaminant; tropomyosin-related kinase B receptor agonist; xenobiotic |
| 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. | 2.97 | 4 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| 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. | 2.46 | 2 | 0 | acridines; aromatic ether; sulfonamide | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| anastrozole [no description available] | 9.23 | 17 | 4 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| 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. | 2.04 | 1 | 0 | pyrazolone | antipyretic; cyclooxygenase 3 inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| aprindine Aprindine: A class Ib anti-arrhythmia agent used to manage ventricular and supraventricular arrhythmias. | 2.05 | 1 | 0 | indanes | |
| 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. | 3.15 | 5 | 0 | 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 |
| 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. | 2.74 | 3 | 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. | 2.75 | 3 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| azelastine azelastine: azeptin is azelastine hydrochloride; structure; eye drop formulation effective in relieving symptoms of allergic conjunctivitis; do not confuse with 5-loxin which is an extract of Boswellia. azelastine : A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position. | 2.04 | 1 | 0 | monochlorobenzenes; phthalazines; tertiary amino compound | anti-allergic agent; anti-asthmatic drug; bronchodilator agent; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; H1-receptor antagonist; platelet aggregation inhibitor |
| azinphosmethyl Azinphosmethyl: An organothiophosphorus cholinesterase inhibitor. It has been used as an acaricide and as an insecticide.. azinphos-methyl : A member of the class of benzotriazines that is 1,2,3-benzotriazine substituted by an oxo group at position 4 and a [(dimethoxyphosphorothioyl)sulfanyl]methyl group at position 3. | 2.04 | 1 | 0 | benzotriazines; organic thiophosphate; organothiophosphate insecticide | agrochemical; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor |
| 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. | 2.07 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| bepridil Bepridil: A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist.. bepridil : A tertiary amine in which the substituents on nitrogen are benzyl, phenyl and 3-(2-methylpropoxy)-2-(pyrrolidin-1-yl)propyl. | 2.05 | 1 | 0 | pyrrolidines; tertiary amine | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| betaxolol [no description available] | 2.44 | 2 | 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. | 1.99 | 1 | 0 | carbamate ester; quaternary ammonium ion | muscarinic agonist |
| bevantolol bevantolol: structure given in first source. bevantolol : A propanolamine that is 3-aminopropane-1,2-diol in which the hydrogen of the primary hydroxy group is substituted by 3-methylphenyl and one of the hydrogens attached to the nitrogen is substituted by 2-(3,4-dimethoxyphenyl)ethyl. A beta1 adrenoceptor antagonist, it has been shown to be as effective as other beta-blockers for the treatment of angina pectoris and hypertension. | 2.04 | 1 | 0 | propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; calcium channel blocker |
| 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. | 15.45 | 103 | 29 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| 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. | 2.04 | 1 | 0 | piperidines; tertiary alcohol; tertiary amino compound | antidote to sarin poisoning; antidyskinesia agent; antiparkinson drug; muscarinic antagonist; parasympatholytic |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 2.74 | 3 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bretylium bretylium: RN given refers to parent cpd. bretylium : A quaternary ammonium cation having 2-bromobenzyl, ethyl and two methyl groups attached to the nitrogen. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. | 2.05 | 1 | 0 | quaternary ammonium ion | adrenergic antagonist; anti-arrhythmia drug; antihypertensive agent |
| bromazepam Bromazepam: One of the BENZODIAZEPINES that is used in the treatment of ANXIETY DISORDERS. | 2.04 | 1 | 0 | organic molecular entity | |
| bromhexine Bromhexine: A mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p744). bromhexine : A substituted aniline that is 2,4-dibromoaniline which is substituted at position 6 by a [cyclohexyl(methyl)amino]methyl group. It is used (as the monohydrochloride salt) as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum). | 2.45 | 2 | 0 | organobromine compound; substituted aniline; tertiary amino compound | mucolytic |
| bromopride bromopride: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | benzamides | |
| brotizolam brotizolam: structure | 2.04 | 1 | 0 | organic molecular entity | |
| buflomedil buflomedil: RN given refers to parent cpd; synonym LL 1656 refers to HCl; structure | 2.04 | 1 | 0 | aromatic ketone | |
| bumetanide [no description available] | 2.74 | 3 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| bunazosin bunazosin: structure | 2.04 | 1 | 0 | quinazolines | |
| bupivacaine Bupivacaine: A widely used local anesthetic agent.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline.. bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic. | 2.44 | 2 | 0 | aromatic amide; piperidinecarboxamide; tertiary amino compound | |
| 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. | 2.07 | 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] | 6.02 | 8 | 1 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| caffeine [no description available] | 2.74 | 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. | 2.45 | 2 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| metrizoate Metrizoic Acid: A diagnostic radiopaque that usually occurs as the sodium salt. | 2.04 | 1 | 0 | monocarboxylic acid | radioopaque medium |
| camphor, (+-)-isomer [no description available] | 1.98 | 1 | 0 | bornane monoterpenoid; cyclic monoterpene ketone | plant metabolite |
| 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. | 2.47 | 2 | 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 |
| carbazilquinone Carbazilquinone: An alkylating agent structurally similar to MITOMYCIN and found to be effective in the treatment of leukemia and various other neoplasms in mice. It causes leukemia and thrombocytopenia in almost all human patients. | 2.04 | 1 | 0 | organic molecular entity | |
| carmofur [no description available] | 2.04 | 1 | 0 | organohalogen compound; pyrimidines | |
| 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. | 3.16 | 5 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| carteolol Carteolol: A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. | 2.45 | 2 | 0 | quinolone; secondary alcohol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| carvedilol [no description available] | 2.47 | 2 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celiprolol Celiprolol: A cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION. | 2.04 | 1 | 0 | aromatic ketone | |
| chloral hydrate [no description available] | 2.04 | 1 | 0 | aldehyde hydrate; ethanediol; organochlorine compound | general anaesthetic; mouse metabolite; sedative; 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. | 2.44 | 2 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| 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. | 2.45 | 2 | 0 | benzodiazepine | |
| 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. | 2.97 | 4 | 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. | 2.04 | 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. | 2.04 | 1 | 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. | 2.75 | 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. | 2.97 | 4 | 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. | 2.74 | 3 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| cifenline [no description available] | 2.04 | 1 | 0 | diarylmethane | |
| cilostazol [no description available] | 2.07 | 1 | 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. | 2.97 | 4 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| 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. | 2.46 | 2 | 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 |
| cisapride Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere. | 2.07 | 1 | 0 | benzamides | |
| 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. | 2.45 | 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. | 3.87 | 3 | 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. | 2.45 | 2 | 0 | monohydroxyquinoline; organochlorine compound; organoiodine compound | antibacterial agent; antifungal agent; antimicrobial agent; antineoplastic agent; antiprotozoal drug; chelator; copper chelator |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 2.47 | 2 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| 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. | 2.45 | 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. | 2.04 | 1 | 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. | 7.92 | 4 | 0 | clonidine; imidazoline | |
| 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. | 2.45 | 2 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 2.07 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cromolyn cromoglycic acid : A dicarboxylic acid that is the bis-chromone derivative of glycerol. It is effective as a mast cell stabilizer. | 2.07 | 1 | 0 | chromones; dicarboxylic acid | anti-asthmatic drug; calcium channel blocker |
| cycloleucine Cycloleucine: An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities.. 1-aminocyclopentanecarboxylic acid : A non-proteinogenic alpha-amino acid that is cyclopentane substituted at position 1 by amino and carboxy groups. | 2.04 | 1 | 0 | non-proteinogenic alpha-amino acid | EC 2.5.1.6 (methionine adenosyltransferase) inhibitor |
| dapsone [no description available] | 2.97 | 4 | 0 | substituted aniline; sulfone | anti-inflammatory drug; antiinfective agent; antimalarial; leprostatic drug |
| debrisoquin Debrisoquin: An adrenergic neuron-blocking drug similar in effects to GUANETHIDINE. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism. | 2.45 | 2 | 0 | carboxamidine; isoquinolines | adrenergic agent; antihypertensive agent; human metabolite; sympatholytic agent |
| deferiprone Deferiprone: A pyridone derivative and iron chelator that is used in the treatment of IRON OVERLOAD in patients with THALASSEMIA.. deferiprone : A member of the class of 4-pyridones that is pyridin-4(1H)-one substituted at positions 1 and 2 by methyl groups and at position 3 by a hydroxy group. A lipid-soluble iron-chelator used for treatment of thalassaemia. | 3.08 | 1 | 0 | 4-pyridones | iron chelator; protective agent |
| 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. | 2.45 | 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 |
| nordazepam Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.. nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. | 2.04 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
| 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. | 2.04 | 1 | 0 | primary amine | |
| eflornithine Eflornithine: An inhibitor of ORNITHINE DECARBOXYLASE, the rate limiting enzyme of the polyamine biosynthetic pathway.. eflornithine : A fluoroamino acid that is ornithine substituted by a difluoromethyl group at position 2. | 4.08 | 2 | 0 | alpha-amino acid; fluoroamino acid | trypanocidal drug |
| 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. | 2.45 | 2 | 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. | 5.1 | 7 | 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 |
| dicamba Dicamba: A chlorinated organic herbicide.. dicamba : A methoxybenzoic acid that is O-methylsalicylic acid substituted by chloro groups at positions 3 and 6. | 2.04 | 1 | 0 | dichlorobenzene; methoxybenzoic acid | agrochemical; environmental contaminant; herbicide; synthetic auxin; xenobiotic |
| 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. | 2.75 | 3 | 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. | 2.04 | 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. | 2.04 | 1 | 0 | carboxylic ester; tertiary amine | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| 3,4-dihydroxybenzohydroxamic acid [no description available] | 2.05 | 1 | 0 | benzoic acids | |
| diethylcarbamazine Diethylcarbamazine: An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa. | 2.04 | 1 | 0 | N-carbamoylpiperazine; N-methylpiperazine | |
| 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. | 2.74 | 3 | 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. | 2.45 | 2 | 0 | dithiol; primary alcohol | chelator |
| dinitolmide Dinitolmide: A coccidiostat for poultry. | 2.04 | 1 | 0 | dinitrotoluene | |
| 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. | 2.46 | 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. | 2.04 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| dipyrone metamizole : A pyrazole that is antiipyrine substituted at C-4 by a methyl(sulfomethyl)amino group, the sodium salt of which, metamizole sodium, was widely used as a powerful analgesic and antipyretic, but withdrawn from many markets from the 1970s due to a risk of causing risk of causing agranulocytosis. | 2.04 | 1 | 0 | amino sulfonic acid; pyrazoles | anti-inflammatory agent; antipyretic; antirheumatic drug; cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug; prodrug |
| 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. | 2.44 | 2 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 2.46 | 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. | 4.04 | 4 | 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. | 4.07 | 4 | 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. | 2.07 | 1 | 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. | 2.04 | 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. | 3.52 | 2 | 0 | 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. | 2.04 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| 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. | 2.04 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| 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. | 2.04 | 1 | 0 | 1,8-naphthyridine derivative; amino acid; fluoroquinolone antibiotic; monocarboxylic acid; N-arylpiperazine; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor |
| erythrosine Fluoresceins: A family of spiro(isobenzofuran-1(3H),9'-(9H)xanthen)-3-one derivatives. These are used as dyes, as indicators for various metals, and as fluorescent labels in immunoassays. | 2.08 | 1 | 0 | ||
| 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. | 2.45 | 2 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethinamate ethinamate: short duration hypnotic with fast onset & relatively low toxicity; may cause dependence; minor descriptor (76-85); on-line & Index Medicus search CARBAMATES (76-85). ethinamate : A carbamate ester that is the 1-vinylcyclohexyl ester of carbamic acid. A short-acting sedative-hypnotic, it was formerly used to treat insomnia. | 2.04 | 1 | 0 | carbamate ester; terminal acetylenic compound | sedative |
| 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. | 2.45 | 2 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| ethyl loflazepate ethyl loflazepate: structure given in first source | 2.05 | 1 | 0 | organic molecular entity | |
| 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. | 4.64 | 3 | 2 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| etilefrine Etilefrine: A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent. | 2.04 | 1 | 0 | phenols | |
| 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. | 2.07 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| 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. | 2.74 | 3 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE | 2.07 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| berotek Fenoterol: A synthetic adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.. fenoterol : A member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction. | 2.74 | 3 | 0 | resorcinols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; sympathomimetic agent; tocolytic agent |
| fenspiride fenspiride: was heading 1975-94 (see under SPIRO COMPOUNDS 1975-90); use SPIRO COMPOUNDS to search FENSPIRIDE 1975-94; bronchodilator agent used in asthma | 2.04 | 1 | 0 | azaspiro compound | |
| 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. | 2.45 | 2 | 0 | anilide; monocarboxylic acid amide; piperidines | adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| 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). | 2.74 | 3 | 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. | 2.04 | 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. | 2.46 | 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. | 2.44 | 2 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 2.45 | 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. | 2.04 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| flunitrazepam Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia. | 2.04 | 1 | 0 | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 2.04 | 1 | 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. | 6.57 | 8 | 2 | 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. | 2.96 | 4 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| 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. | 3.53 | 2 | 0 | fluorobiphenyl; monocarboxylic acid | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 19.34 | 204 | 92 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic 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. | 2.04 | 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. | 3.14 | 5 | 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. | 2.04 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 2.04 | 1 | 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. | 2.07 | 1 | 0 | aminoquinoline; carboxylic ester; glycol; organochlorine compound; secondary amino compound | inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| glimepiride glimepiride: structure given in first source | 2.04 | 1 | 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. | 2.04 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glutethimide Glutethimide: A hypnotic and sedative. Its use has been largely superseded by other drugs. | 2.45 | 2 | 0 | piperidines | |
| 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. | 2.44 | 2 | 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 |
| granisetron [no description available] | 2.04 | 1 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 2.84 | 3 | 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. | 2.45 | 2 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 2.04 | 1 | 0 | acetamides | |
| 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. | 2.45 | 2 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| halothane [no description available] | 2.04 | 1 | 0 | haloalkane; organobromine compound; organochlorine compound; organofluorine compound | inhalation anaesthetic |
| hexobarbital Hexobarbital: A barbiturate that is effective as a hypnotic and sedative.. hexobarbital : A member of the class of barbiturates taht is barbituric acid substituted at N-1 by methyl and at C-5 by methyl and cyclohex-1-enyl groups. | 2.04 | 1 | 0 | barbiturates | |
| hycanthone Hycanthone: Potentially toxic, but effective antischistosomal agent, it is a metabolite of LUCANTHONE.. hycanthone : A thioxanthen-9-one compound having a hydroxymethyl substituent at the 1-position and a 2-[(diethylamino)ethyl]amino substituent at the 4-position. It was formerly used (particularly as the monomethanesulfonic acid salt) as a schistosomicide for individual or mass treatement of infection with Schistosoma haematobium and S. mansoni, but due to its toxicity and concern about possible carcinogenicity, it has been replaced by other drugs such as praziquantel. | 2.07 | 1 | 0 | thioxanthenes | mutagen; schistosomicide drug |
| 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. | 2.74 | 3 | 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. | 2.45 | 2 | 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. | 2.04 | 1 | 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. | 2.04 | 1 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 2.74 | 3 | 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. | 2.47 | 2 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| hypericin [no description available] | 2.04 | 1 | 0 | ||
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 2.97 | 4 | 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. | 2.75 | 3 | 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. | 2.74 | 3 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 2.76 | 3 | 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. | 2.75 | 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. | 2.74 | 3 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| incadronate [no description available] | 2.05 | 1 | 0 | 1,1-bis(phosphonic acid) | |
| 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. | 2.45 | 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. | 2.94 | 4 | 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. | 2.04 | 1 | 0 | benzenedicarboxamide; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| iopromide iopromide: structure given in first source. iopromide : A dicarboxylic acid diamide that consists of N-methylisophthalamide bearing three iodo substituents at positions 2, 4 and 6, a methoxyacetyl substituent at position 5 and two 2,3-dihydroxypropyl groups attached to the amide nitrogens. A water soluble x-ray contrast agent for intravascular administration. | 2.04 | 1 | 0 | dicarboxylic acid diamide; organoiodine compound | environmental contaminant; nephrotoxic agent; radioopaque medium; xenobiotic |
| iothalamic acid Iothalamic Acid: A contrast medium in diagnostic radiology with properties similar to those of diatrizoic acid. It is used primarily as its sodium and meglumine (IOTHALAMATE MEGLUMINE) salts. | 2.04 | 1 | 0 | organic molecular entity | |
| ipriflavone ipriflavone : A member of the class of isoflavones that is isoflavone in which the hydrogen at position 7 is replaced by an isopropoxy group. A synthetic isoflavone, it was formerly used for the treatment of osteoporosis, although a randomised controlled study failed to show any benefit. It is still used to prevent osteoporosis in post-menopausal women. | 10.47 | 4 | 4 | aromatic ether; isoflavones | bone density conservation agent |
| iproniazid [no description available] | 2.46 | 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. | 2.04 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| 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). | 2.74 | 3 | 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. | 2.44 | 2 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| 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. | 2.04 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 2.04 | 1 | 0 | piperazines | |
| nsc 664704 kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta). | 2.05 | 1 | 0 | indolobenzazepine; lactam; organobromine compound | cardioprotective agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor; geroprotector |
| 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. | 2.45 | 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. | 2.45 | 2 | 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. | 7.83 | 12 | 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. | 2.45 | 2 | 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. | 2.04 | 1 | 0 | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| ketotifen Ketotifen: A cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. It has been proposed for the treatment of asthma, rhinitis, skin allergies, and anaphylaxis.. ketotifen : An organic heterotricyclic compound that is 4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one which is substituted at position 4 by a 1-methylpiperidin-4-ylidene group. A blocker of histamine H1 receptors with a stabilising action on mast cells, it is used (usually as its hydrogen fumarate salt) for the treatment of asthma, where it may take several weeks to exert its full effect. | 2.05 | 1 | 0 | cyclic ketone; olefinic compound; organic heterotricyclic compound; organosulfur heterocyclic compound; piperidines; tertiary amino compound | anti-asthmatic drug; H1-receptor antagonist |
| 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. | 2.97 | 4 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 2.07 | 1 | 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. | 2.45 | 2 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| letrozole [no description available] | 13.86 | 17 | 6 | 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. | 2.05 | 1 | 0 | aromatic ketone; dibenzoazepine; monochlorobenzenes; tertiary amino compound | antidepressant |
| lomustine [no description available] | 2.45 | 2 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| 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. | 2.45 | 2 | 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 | 2.46 | 2 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor 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. | 2.75 | 3 | 0 | anthracenes | |
| mazindol Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. | 2.05 | 1 | 0 | organic molecular entity | |
| 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. | 2.04 | 1 | 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. | 2.07 | 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. | 2.7 | 3 | 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. | 2.07 | 1 | 0 | diarylmethane | |
| 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. | 2.41 | 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. | 2.05 | 1 | 0 | organofluorine compound; piperidines; quinolines; secondary alcohol | |
| 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. | 2.46 | 2 | 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. | 2.45 | 2 | 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. | 2.74 | 3 | 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) | 2.44 | 2 | 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. | 2.04 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| 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. | 10.08 | 5 | 2 | 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. | 2.04 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methapyrilene Methapyrilene: Histamine H1 antagonist with sedative action used as a hypnotic and in allergies.. methapyrilene : A member of the class of ethylenediamine derivatives that is ethylenediamine in which one of the nitrogens is substituted by two methyl groups, and the other nitrogen is substituted by a 2-pyridyl group and a (2-thienyl)methyl group. | 2.04 | 1 | 0 | ethylenediamine derivative | anti-allergic agent; carcinogenic agent; H1-receptor antagonist; sedative |
| 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. | 2.07 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| methoxyamine methoxyamine: analytical reagent for aldehydes and ketones; strong irritant, can probably produce methemoglobinemia; RN given refers to parent cpd; structure | 2.05 | 1 | 0 | organooxygen compound | |
| methoxyflurane Methoxyflurane: An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with NITROUS OXIDE to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180). methoxyflurane : An ether in which the two groups attached to the central oxygen atom are methyl and 2,2-dichloro-1,1-difluoroethyl. | 2.45 | 2 | 0 | ether; organochlorine compound; organofluorine compound | hepatotoxic agent; inhalation anaesthetic; nephrotoxic agent; non-narcotic analgesic |
| methyclothiazide Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) | 2.04 | 1 | 0 | benzothiadiazine | |
| methyl salicylate methyl salicylate: used in over-the-counter liniments, ointments, lotions for relief of musculoskeletal aches and pains; has hemolytic effect on human & sheep erythrocytes; RN given refers to parent cpd; structure in Merck Index, 9th ed, #5990. methyl salicylate : A benzoate ester that is the methyl ester of salicylic acid. | 2.04 | 1 | 0 | benzoate ester; methyl ester; salicylates | flavouring agent; insect attractant; metabolite |
| 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. | 2.74 | 3 | 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. | 2.74 | 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. | 2.04 | 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. | 2.04 | 1 | 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. | 2.74 | 3 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| 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. | 2.74 | 3 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| mianserin Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere. | 4.77 | 2 | 1 | dibenzoazepine | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; H1-receptor antagonist; histamine agonist; sedative; serotonergic antagonist |
| 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. | 2.04 | 1 | 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. | 2.07 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 2.04 | 1 | 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. | 2.75 | 3 | 0 | 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. | 2.04 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| 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. | 2.94 | 4 | 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. | 2.44 | 2 | 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. | 2.07 | 1 | 0 | monocarboxylic acid amide; sulfoxide | |
| entinostat [no description available] | 3.51 | 1 | 0 | benzamides; carbamate ester; primary amino compound; pyridines; substituted aniline | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| 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. | 2.04 | 1 | 0 | acetamides; benzamides | anti-arrhythmia drug |
| clorgyline Clorgyline: An antidepressive agent and monoamine oxidase inhibitor related to PARGYLINE.. clorgyline : An aromatic ether that is the 2,4-dichlorophenyl ether of 3-aminopropan-1-ol in which the nitrogen is substituted by a methyl group and a prop-1-yn-3-yl group. A monoamine oxidase inhibitor, it was formerly used as an antidepressant. | 2.04 | 1 | 0 | aromatic ether; dichlorobenzene; terminal acetylenic compound; tertiary amino compound | antidepressant; EC 1.4.3.4 (monoamine oxidase) inhibitor |
| 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. | 2.05 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nalidixic acid [no description available] | 2.04 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| activins Activins: Activins are produced in the pituitary, gonads, and other tissues. By acting locally, they stimulate pituitary FSH secretion and have diverse effects on cell differentiation and embryonic development. Activins are glycoproteins that are hetero- or homodimers of INHIBIN-BETA SUBUNITS. | 2.41 | 2 | 0 | ||
| naratriptan naratriptan: structure given in first source | 2.04 | 1 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 2.46 | 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. | 2.04 | 1 | 0 | benzoxazocine; tertiary amino compound | |
| 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. | 2.46 | 2 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| 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. | 2.04 | 1 | 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. | 2.97 | 4 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 12.03 | 15 | 6 | (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. | 2.07 | 1 | 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. | 2.44 | 2 | 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. | 2.46 | 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). | 2.04 | 1 | 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. | 2.74 | 3 | 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. | 2.45 | 2 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 2.04 | 1 | 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. | 2.45 | 2 | 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. | 2.05 | 1 | 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. | 2.45 | 2 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| nylidrin Nylidrin: A beta-adrenergic agonist. Nylidrin causes peripheral vasodilation, a positive inotropic effect, and increased gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. | 2.04 | 1 | 0 | alkylbenzene | |
| 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. | 2.46 | 2 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| olomoucine olomoucine: inhibits protein P34CDC2. olomoucine : A 9H-purine that is substituted by a (2-hydroxyethyl)nitrilo, benzylnitrilo and a methyl group at positions 2,6 and 9, respectively. It is a cyclin-dependent kinase inhibitor. | 2.05 | 1 | 0 | 2,6-diaminopurines; ethanolamines | EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| 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. | 2.75 | 3 | 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. | 3.52 | 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. | 2.07 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxatomide oxatomide: structure; an anti-allergic & an anti-asthmatic. oxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug. | 2.05 | 1 | 0 | benzimidazoles; diarylmethane; N-alkylpiperazine | anti-allergic agent; anti-inflammatory agent; geroprotector; H1-receptor antagonist; serotonergic antagonist |
| 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. | 2.45 | 2 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxiracetam oxiracetam: structure in first source | 2.04 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| oxprenolol Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. | 2.45 | 2 | 0 | aromatic ether | |
| 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. | 4.58 | 5 | 1 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| oxyphenbutazone Oxyphenbutazone: A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27). oxyphenbutazone : A metabolite of phenylbutazone obtained by hydroxylation at position 4 of one of the phenyl rings. Commonly used (as its hydrate) to treat pain, swelling and stiffness associated with arthritis and gout, it was withdrawn from the market 1984 following association with blood dyscrasis and Stevens-Johnson syndrome. | 2.47 | 2 | 0 | phenols; pyrazolidines | antimicrobial agent; antineoplastic agent; antipyretic; drug metabolite; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic metabolite |
| 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. | 2.47 | 2 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| fenclonine Fenclonine: A selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-HYDROXYTRYPTAMINE). Fenclonine acts pharmacologically to deplete endogenous levels of serotonin. | 2.03 | 1 | 0 | phenylalanine derivative | |
| pamidronate [no description available] | 8.61 | 10 | 6 | 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. | 2.45 | 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. | 2.45 | 2 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| 4-dichlorobenzene dichlorobenzene : Any member of the class of chlorobenzenes carrying two chloro groups at unspecified positions.. 1,4-dichlorobenzene : A dichlorobenzene carrying chloro groups at positions 1 and 4. | 2.04 | 1 | 0 | dichlorobenzene | insecticide |
| 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. | 2.74 | 3 | 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. | 2.04 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 2.04 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 2.07 | 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. | 2.74 | 3 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenacemide phenacemide: anti-epileptic drug; structure | 2.04 | 1 | 0 | acetamides | |
| phenacetin Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione | 2.74 | 3 | 0 | acetamides; aromatic ether | cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug |
| phenazopyridine Phenazopyridine: A local anesthetic that has been used in urinary tract disorders. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.. phenazopyridine : A diaminopyridine that is 2,6-diaminopyridine substituted at position 3 by a phenylazo group. A local anesthetic that has topical analgesic effect on mucosa lining of the urinary tract. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity. | 2.04 | 1 | 0 | diaminopyridine; monoazo compound | anticoronaviral agent; carcinogenic agent; local anaesthetic; non-narcotic analgesic |
| phenindione Phenindione: An indandione that has been used as an anticoagulant. Phenindione has actions similar to WARFARIN, but it is now rarely employed because of its higher incidence of severe adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p234) | 2.05 | 1 | 0 | aromatic ketone; beta-diketone | anticoagulant |
| 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. | 2.74 | 3 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenolsulfonphthalein Phenolsulfonphthalein: Red dye, pH indicator, and diagnostic aid for determination of renal function. It is used also for studies of the gastrointestinal and other systems.. phenol red : 3H-2,1-Benzoxathiole 1,1-dioxide in which both of the hydrogens at position 3 have been substituted by 4-hydroxyphenyl groups. A pH indicator changing colour from yellow below pH 6.8 to bright pink above pH 8.2, it is commonly used as an indicator in cell cultures and in home swimming pool test kits. It is also used in the (now infrequently performed) phenolsulfonphthalein (PSP) test for estimation of overall blood flow through the kidney. | 2.36 | 2 | 0 | 2,1-benzoxathiole; arenesulfonate ester; phenols; sultone | acid-base indicator; diagnostic agent; two-colour indicator |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 2.07 | 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. | 2.75 | 3 | 0 | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| phenylbutazone Phenylbutazone: A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.. phenylbutazone : A member of the class of pyrazolidines that is 1,2-diphenylpyrazolidine-3,5-dione carrying a butyl group at the 4-position. | 2.47 | 2 | 0 | pyrazolidines | antirheumatic drug; EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor; metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug |
| moxonidine moxonidine: structure given in first source | 2.04 | 1 | 0 | organohalogen compound; pyrimidines | |
| pimobendan pimobendan: produces arterial & venous dilatation in dogs; structure given in first source | 2.04 | 1 | 0 | benzimidazoles; pyridazinone | cardiotonic drug; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| 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. | 2.04 | 1 | 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. | 2.45 | 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 |
| pipobroman Pipobroman: An antineoplastic agent that acts by alkylation.. pipobroman : An N-acylpiperazine that is piperazine in which each of the nitrogens has been acylated by a 3-bromopropionoyl group. An anti-cancer drug. | 2.04 | 1 | 0 | N-acylpiperazine; organobromine compound; tertiary carboxamide | alkylating agent; antineoplastic agent |
| piretanide piretanide: potent inhibitor of chloride transport; structure | 2.04 | 1 | 0 | aromatic ether | |
| polythiazide [no description available] | 2.04 | 1 | 0 | benzothiadiazine | |
| 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. | 4.31 | 3 | 0 | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| prilocaine Prilocaine: A local anesthetic that is similar pharmacologically to LIDOCAINE. Currently, it is used most often for infiltration anesthesia in dentistry.. prilocaine : An amino acid amide in which N-propyl-DL-alanine and 2-methylaniline have combined to form the amide bond; used as a local anaesthetic. | 2.44 | 2 | 0 | amino acid amide; monocarboxylic acid amide | anticonvulsant; local anaesthetic |
| 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. | 2.74 | 3 | 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. | 2.04 | 1 | 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. | 2.44 | 2 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| probucol Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood. | 2.04 | 1 | 0 | dithioketal; polyphenol | anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular 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. | 2.74 | 3 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| procaine Procaine: A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016).. procaine : A benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol. | 2.45 | 2 | 0 | benzoate ester; substituted aniline; tertiary amino compound | central nervous system depressant; drug allergen; local anaesthetic; peripheral nervous system drug |
| 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. | 2.92 | 4 | 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. | 2.46 | 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. | 2.04 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promazine Promazine: A phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.. promazine : A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position. | 2.04 | 1 | 0 | phenothiazines; tertiary amine | antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; muscarinic antagonist; phenothiazine antipsychotic drug; serotonergic 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. | 2.45 | 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. | 2.04 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propidium Propidium: Quaternary ammonium analog of ethidium; an intercalating dye with a specific affinity to certain forms of DNA and, used as diiodide, to separate them in density gradients; also forms fluorescent complexes with cholinesterase which it inhibits. | 2 | 1 | 0 | phenanthridines; quaternary ammonium ion | fluorochrome; intercalator |
| 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. | 2.04 | 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. | 2.75 | 3 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| pyridostigmine [no description available] | 2.46 | 2 | 0 | pyridinium ion | |
| pyrilamine Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group. | 2.07 | 1 | 0 | aromatic ether; ethylenediamine derivative | H1-receptor antagonist |
| pyrimethamine Maloprim: contains above 2 cpds | 2.45 | 2 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| 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. | 2.45 | 2 | 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. | 2.07 | 1 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| ranitidine [no description available] | 2.97 | 4 | 0 | aralkylamine | |
| resorcinol resorcinol: RN given refers to parent cpd; structure in Merck Index, 9th ed, #7951. resorcinol : A benzenediol that is benzene dihydroxylated at positions 1 and 3. | 2.04 | 1 | 0 | benzenediol; phenolic donor; resorcinols | erythropoietin inhibitor; sensitiser |
| 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. | 2.49 | 2 | 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 | 2.04 | 1 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rofecoxib [no description available] | 2.02 | 1 | 0 | butenolide; sulfone | analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| semustine Semustine: 4-Methyl derivative of LOMUSTINE; (CCNU). An antineoplastic agent which functions as an alkylating agent.. semustine : An organochlorine compound that is urea in which the two hydrogens on one of the amino groups are replaced by nitroso and 2-chloroethyl groups and one hydrogen from the other amino group is replaced by a 4-methylcyclohexyl group. | 2.04 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent |
| 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. | 2.44 | 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. | 2.75 | 3 | 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. | 2.46 | 2 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| stearic acid octadecanoic acid : A C18 straight-chain saturated fatty acid component of many animal and vegetable lipids. As well as in the diet, it is used in hardening soaps, softening plastics and in making cosmetics, candles and plastics. | 2.05 | 1 | 0 | long-chain fatty acid; saturated fatty acid; straight-chain saturated fatty acid | algal metabolite; Daphnia magna metabolite; human metabolite; plant metabolite |
| imatinib [no description available] | 2.04 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| streptonigrin [no description available] | 2.04 | 1 | 0 | pyridines; quinolone | antimicrobial agent; antineoplastic agent |
| 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). | 2.04 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| sulfacetamide Sulfacetamide: An anti-bacterial agent that is used topically to treat skin infections and orally for urinary tract infections.. sulfacetamide : A sulfonamide that is sulfanilamide acylated on the sulfonamide nitrogen. | 2.04 | 1 | 0 | N-sulfonylcarboxamide; substituted aniline | antibacterial drug; antiinfective agent; antimicrobial agent; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfaguanidine Sulfaguanidine: A sulfanilamide antimicrobial agent that is used to treat enteric infections.. sulfaguanidine : A sulfonamide incorporating a guanidine moiety used to block the synthesis of folic acid; mostly used in veterinary medicine | 2.04 | 1 | 0 | sulfonamide antibiotic | antiinfective agent |
| sulfamethazine Sulfamethazine: A sulfanilamide anti-infective agent. It has a spectrum of antimicrobial action similar to other sulfonamides.. sulfamethazine : A sulfonamide consisting of pyrimidine with methyl substituents at the 4- and 6-positions and a 4-aminobenzenesulfonamido group at the 2-position. | 2.04 | 1 | 0 | pyrimidines; sulfonamide antibiotic; sulfonamide | antibacterial drug; antiinfective agent; antimicrobial agent; carcinogenic agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; ligand; xenobiotic |
| 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. | 2.44 | 2 | 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 |
| sulfamethoxypyridazine Sulfamethoxypyridazine: A sulfanilamide antibacterial agent.. sulfamethoxypyridazine : A sulfonamide consisting of pyridazine having a methoxy substituent at the 6-position and a 4-aminobenzenesulfonamido group at the 3-position. | 2.04 | 1 | 0 | pyridazines; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfanilamide [no description available] | 2.04 | 1 | 0 | substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial agent; drug allergen; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| sulfaphenazole Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent. | 2.07 | 1 | 0 | primary amino compound; pyrazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial drug; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor; P450 inhibitor |
| sulfapyridine Sulfapyridine: Antibacterial, potentially toxic, used to treat certain skin diseases.. sulfapyridine : A sulfonamide consisting of pyridine with a 4-aminobenzenesulfonamido group at the 2-position. | 2.04 | 1 | 0 | pyridines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; dermatologic drug; drug allergen; environmental contaminant; xenobiotic |
| 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. | 3.81 | 3 | 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. | 2.04 | 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 |
| sulfinpyrazone Sulfinpyrazone: A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. | 2.04 | 1 | 0 | pyrazolidines; sulfoxide | uricosuric drug |
| 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. | 2.44 | 2 | 0 | isoxazoles; sulfonamide antibiotic; sulfonamide | antibacterial drug; drug allergen |
| sulforaphane sulforaphane: from Cardaria draba L.. sulforaphane : An isothiocyanate having a 4-(methylsulfinyl)butyl group attached to the nitrogen. | 2.05 | 1 | 0 | isothiocyanate; sulfoxide | antineoplastic agent; antioxidant; EC 3.5.1.98 (histone deacetylase) inhibitor; plant metabolite |
| sulfoxone sulfoxone: RN given refers to parent cpd | 2.04 | 1 | 0 | sulfonamide | |
| sulpiride Sulpiride: A dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid. (From Merck Index, 11th ed). sulpiride : A member of the class of benzamides obtained from formal condensation between the carboxy group of 2-methoxy-5-sulfamoylbenzoic acid and the primary amino group of (1-ethylpyrrolidin-2-yl)methylamine. | 2.07 | 1 | 0 | benzamides; N-alkylpyrrolidine; sulfonamide | antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist |
| 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. | 2.04 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| suprofen Suprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.. suprofen : An aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group. | 2.04 | 1 | 0 | aromatic ketone; monocarboxylic acid; thiophenes | antirheumatic drug; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug |
| suramin Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.. suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. | 11.43 | 7 | 2 | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| 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. | 2.04 | 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 |
| tegafur [no description available] | 4.66 | 3 | 2 | organohalogen compound; pyrimidines | |
| temozolomide [no description available] | 2.04 | 1 | 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 | 4.54 | 4 | 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. | 2.74 | 3 | 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. | 2.05 | 1 | 0 | diarylmethane | |
| tetracaine Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia.. tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia. | 2.04 | 1 | 0 | benzoate ester; tertiary amino compound | local anaesthetic |
| tetraethylammonium Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90) | 2.07 | 1 | 0 | quaternary ammonium ion | |
| 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. | 6.67 | 4 | 3 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 2.04 | 1 | 0 | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| 2,2'-thiodiethanol 2,2'-thiodiethanol: product of yperite hydrolysis; a hydrolysis product opf mustard gas; strongly stimulates differentiation of chick embryo myogenic cells. thiodiglycol : A diol that is pentane-1,5-diol in which the methylene group at position 3 is replaced by a sulfur atom | 2.04 | 1 | 0 | aliphatic sulfide; diol | antineoplastic agent; antioxidant; metabolite; solvent |
| 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. | 2.05 | 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). | 2.44 | 2 | 0 | aziridines | |
| 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. | 2.47 | 2 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| 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. | 2.04 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| 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. | 2.04 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| 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. | 2.04 | 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. | 2.74 | 3 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| 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. | 2.04 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 2.83 | 3 | 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. | 2.04 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triacetin Triacetin: A triglyceride that is used as an antifungal agent.. triacetin : A triglyceride obtained by acetylation of the three hydroxy groups of glycerol. It has fungistatic properties (based on release of acetic acid) and has been used in the topical treatment of minor dermatophyte infections. | 2.31 | 1 | 0 | triglyceride | adjuvant; antifungal drug; food additive carrier; food emulsifier; food humectant; fuel additive; plant metabolite; solvent |
| 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. | 2.74 | 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. | 2.45 | 2 | 0 | triazolobenzodiazepine | sedative |
| trichlormethiazide Trichlormethiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p830). trichlormethiazide : A benzothiadiazine, hydrogenated at positions 2, 3 and 4 and substituted with an aminosulfonyl group at C-7, a chloro substituent at C-6 and a dichloromethyl group at C-3 and with S-1 as an S,S-dioxide. A sulfonamide antibiotic, it is used as a diuretic to treat oedema (including that associated with heart failure) and hypertension. | 2.04 | 1 | 0 | benzothiadiazine; sulfonamide antibiotic | antihypertensive agent; diuretic |
| 2,2',2''-trichlorotriethylamine 2,2',2''-trichlorotriethylamine: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | ||
| trifluoperazine [no description available] | 2.05 | 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 |
| 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. | 2.45 | 2 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| 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. | 2.97 | 4 | 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. | 2.44 | 2 | 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. | 2.04 | 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. | 2.42 | 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 |
| urapidil [no description available] | 2.04 | 1 | 0 | piperazines | |
| urethane [no description available] | 2.04 | 1 | 0 | carbamate ester | fungal metabolite; mutagen |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 2.46 | 2 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vesamicol vesamicol: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | piperidines | |
| viloxazine Viloxazine: A morpholine derivative used as an antidepressant. It is similar in action to IMIPRAMINE. | 2.04 | 1 | 0 | aromatic ether | |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 2.07 | 1 | 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. | 2.04 | 1 | 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. | 2.46 | 2 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zomepirac zomepirac: RN given refers to parent cpd; structure | 2.07 | 1 | 0 | aromatic ketone; monocarboxylic acid; monochlorobenzenes; pyrroles | cardiovascular drug; non-steroidal anti-inflammatory drug |
| 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. | 2.45 | 2 | 0 | monochloropyridine; pyrrolopyrazine | central nervous system depressant; sedative |
| 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. | 2.41 | 2 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| corticosterone [no description available] | 2.42 | 2 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 2.04 | 1 | 0 | 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 |
| estriol hormonin: estrogen replacement; each tablet contains 600 ug micronized 17beta-estradiol, 270 ug estriol and 1.4 mg estrone. chlorapatite : A phosphate mineral with the formula Ca5(PO4)3Cl. | 4.33 | 4 | 1 | 16alpha-hydroxy steroid; 17beta-hydroxy steroid; 3-hydroxy steroid | estrogen; human metabolite; human xenobiotic metabolite; mouse metabolite |
| 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. | 2.45 | 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 |
| cephaloridine Cephaloridine: A cephalosporin antibiotic.. cefaloridine : A cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C. | 2.04 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| thymidine [no description available] | 2.01 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite; human metabolite; metabolite; mouse metabolite |
| floxuridine Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.. floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. | 2.73 | 3 | 0 | nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; radiosensitizing agent |
| triethylenemelamine Triethylenemelamine: Toxic alkylating agent used in industry; also as antineoplastic and research tool to produce chromosome aberrations and cancers. | 2.04 | 1 | 0 | 1,3,5-triazines | alkylating agent; insect sterilant |
| hydroxyproline Hydroxyproline: A hydroxylated form of the imino acid proline. A deficiency in ASCORBIC ACID can result in impaired hydroxyproline formation.. hydroxyproline : A proline derivative that is proline substituted by at least one hydroxy group. | 2.38 | 2 | 0 | 4-hydroxyproline; L-alpha-amino acid zwitterion | human metabolite; mouse metabolite; plant metabolite |
| thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. | 2.69 | 3 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| norethindrone acetate norethisterone acetate : A 3-oxo Delta(4)-steroid that is norethisterone in which the hydroxy group has been converted to its acetate ester. | 8.94 | 12 | 4 | 3-oxo-Delta(4) steroid; acetate ester; terminal acetylenic compound | progestin; synthetic oral contraceptive |
| 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. | 6.3 | 6 | 2 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| allobarbital allobarbital: was heading 1976-94 (see under BARBITURATES 1976-90); ALLOBARBITONE, DIALLYLBARBITAL, DIALLYLBARBITURIC ACID, & DIALLYLMAL were see ALLOBARBITAL 1976-94; use BARBITURATES to search ALLOBARBITAL 1976-94; a barbiturate derivative with effects of intermediate duration; at lower doses, it is used as a sedative; at higher doses, it displays hypnotic effects | 2.04 | 1 | 0 | barbiturates | |
| 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. | 3.51 | 2 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| lynestrenol Lynestrenol: A synthetic progestational hormone used often in mixtures with estrogens as an oral contraceptive (CONTRACEPTIVES, ORAL). | 6.51 | 4 | 2 | steroid | |
| 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. | 8.58 | 11 | 5 | 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. | 9.27 | 12 | 7 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| paramethasone Paramethasone: A glucocorticoid with the general properties of corticosteroids. It has been used by mouth in the treatment of all conditions in which corticosteroid therapy is indicated except adrenal-deficiency states for which its lack of sodium-retaining properties makes it less suitable than HYDROCORTISONE with supplementary FLUDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p737) | 2.45 | 2 | 0 | fluorinated steroid | |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 2.03 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| androsterone [no description available] | 3.1 | 5 | 0 | 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. | 2.06 | 1 | 0 | 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. | 8.5 | 20 | 5 | 17-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; androstanoid | androgen; human metabolite; mouse metabolite |
| azauridine Azauridine: A triazine nucleoside used as an antineoplastic antimetabolite. It interferes with pyrimidine biosynthesis thereby preventing formation of cellular nucleic acids. As the triacetate, it is also effective as an antipsoriatic. | 2.04 | 1 | 0 | N-glycosyl-1,2,4-triazine | antimetabolite; antineoplastic agent; drug 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. | 2.44 | 2 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| idoxuridine [no description available] | 2.04 | 1 | 0 | organoiodine compound; pyrimidine 2'-deoxyribonucleoside | antiviral drug; DNA synthesis inhibitor |
| metaraminol Metaraminol: A sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of HYPOTENSION.. metaraminol : A member of the class of phenylethanolamines that is 2-amino-1-phenylethanol substituted by a methyl group at position 2 and a phenolic hydroxy group at position 1. A sympathomimetic agent , it is used in the treatment of hypotension. | 2.07 | 1 | 0 | phenylethanolamines | alpha-adrenergic agonist; sympathomimetic agent; vasoconstrictor agent |
| amifampridine Amifampridine: 4-Aminopyridine derivative that acts as a POTASSIUM CHANNEL blocker to increase release of ACETYLCHOLINE from nerve terminals. It is used in the treatment of CONGENITAL MYASTHENIC SYNDROMES. | 2.07 | 1 | 0 | aminopyridine | |
| 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. | 2.71 | 3 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| diethylnitrosamine Diethylnitrosamine: A nitrosamine derivative with alkylating, carcinogenic, and mutagenic properties.. N-nitrosodiethylamine : A nitrosamine that is N-ethylethanamine substituted by a nitroso group at the N-atom. | 2 | 1 | 0 | nitrosamine | carcinogenic agent; hepatotoxic agent; mutagen |
| alanine Alanine: A non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases IMMUNITY, and provides energy for muscle tissue, BRAIN, and the CENTRAL NERVOUS SYSTEM.. alanine : An alpha-amino acid that consists of propionic acid bearing an amino substituent at position 2. | 2.02 | 1 | 0 | alanine zwitterion; alanine; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid | EC 4.3.1.15 (diaminopropionate ammonia-lyase) inhibitor; fundamental metabolite |
| serine Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group. | 2.05 | 1 | 0 | L-alpha-amino acid; proteinogenic amino acid; serine family amino acid; serine zwitterion; serine | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 2.44 | 2 | 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. | 2.06 | 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 |
| lysine Lysine: An essential amino acid. It is often added to animal feed.. lysine : A diamino acid that is caproic (hexanoic) acid bearing two amino substituents at positions 2 and 6.. L-lysine : An L-alpha-amino acid; the L-isomer of lysine. | 2.01 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; lysine; organic molecular entity; proteinogenic amino acid | algal metabolite; anticonvulsant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite |
| cetrimonium bromide cetyltrimethylammonium bromide : The organic bromide salt that is the bromide salt of cetyltrimethylammonium; one of the components of the topical antiseptic cetrimide. | 2.05 | 1 | 0 | organic bromide salt; quaternary ammonium salt | detergent; surfactant |
| vincristine [no description available] | 2.44 | 2 | 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. | 2.04 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar. | 2.25 | 1 | 0 | glycosyl glycoside | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent |
| 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. | 8.1 | 15 | 7 | 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. | 2.08 | 1 | 0 | steroid ester | |
| 9,10-dimethyl-1,2-benzanthracene 9,10-Dimethyl-1,2-benzanthracene: Polycyclic aromatic hydrocarbon found in tobacco smoke that is a potent carcinogen.. 7,12-dimethyltetraphene : A tetraphene having methyl substituents at the 7- and 12-positions. It is a potent carcinogen and is present in tobacco smoke. | 2.69 | 3 | 0 | ortho-fused polycyclic arene; tetraphenes | carcinogenic agent |
| 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. | 2.04 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| aminopyrine Aminopyrine: A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS.. aminophenazone : A pyrazolone that is 1,2-dihydro-3H-pyrazol-3-one substituted by a dimethylamino group at position 4, methyl groups at positions 1 and 5 and a phenyl group at position 2. It exhibits analgesic, anti-inflammatory, and antipyretic properties. | 2.07 | 1 | 0 | pyrazolone; tertiary amino compound | antipyretic; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| dromostanolone dromostanolone: synthetic anabolic androgenic steroid used to lower plasma cholesterol & as antineoplastic agent in advanced breast neoplasms; major descriptor (66-86); on-line search ANDROSTANOLS (80-86); ANDROSTANES (68-86); INDEX MEDICUS search DROMOSTANOLONE (66-86); RN given refers to (2alpha,5alpha,17beta)-isomer | 2.04 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-5alpha-steroid; anabolic androgenic steroid | anabolic agent; antineoplastic agent |
| cephalothin Cephalothin: A cephalosporin antibiotic.. cefalotin : A semisynthetic, first-generation cephalosporin antibiotic with acetoxymethyl and (2-thienylacetyl)nitrilo moieties at positions 3 and 7, respectively, of the core structure. Administered parenterally during surgery and to treat a wide spectrum of blood infections. | 2.44 | 2 | 0 | azabicycloalkene; beta-lactam antibiotic allergen; carboxylic acid; cephalosporin; semisynthetic derivative; thiophenes | antibacterial drug; antimicrobial agent |
| 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. | 2.04 | 1 | 0 | kanamycins | bacterial metabolite |
| bromodeoxyuridine Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors. | 2.04 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent |
| galactose galactopyranose : The pyranose form of galactose. | 2.15 | 1 | 0 | D-galactose; galactopyranose | Escherichia coli metabolite; mouse metabolite |
| carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2. | 2.25 | 1 | 0 | monohydroxyquinoline; quinolone | bacterial xenobiotic metabolite |
| phenylephrine Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring. | 1.99 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | alpha-adrenergic agonist; cardiotonic drug; mydriatic agent; nasal decongestant; protective agent; sympathomimetic agent; vasoconstrictor agent |
| thiamine [no description available] | 2.04 | 1 | 0 | organic chloride salt; vitamin B1 | |
| 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 | 2.74 | 3 | 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. | 2.02 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| methicillin Methicillin: One of the PENICILLINS which is resistant to PENICILLINASE but susceptible to a penicillin-binding protein. It is inactivated by gastric acid so administered by injection.. methicillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 2,6-dimethoxybenzoyl group. | 2.44 | 2 | 0 | penicillin allergen; penicillin | antibacterial drug |
| niridazole Niridazole: An antischistosomal agent that has become obsolete. | 2.04 | 1 | 0 | 1,3-thiazoles; C-nitro compound | |
| 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. | 2.04 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| methylene blue Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties. | 2.08 | 1 | 0 | organic chloride salt | acid-base indicator; antidepressant; antimalarial; antimicrobial agent; antioxidant; cardioprotective agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 4.6.1.2 (guanylate cyclase) inhibitor; fluorochrome; histological dye; neuroprotective agent; physical tracer |
| zoxazolamine Zoxazolamine: A uricosuric and muscle relaxant. Zoxazolamine acts centrally as a muscle relaxant, but the mechanism of its action is not understood. | 2.46 | 2 | 0 | benzoxazole | |
| leucine Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group. | 4.14 | 3 | 1 | amino acid zwitterion; L-alpha-amino acid; leucine; proteinogenic amino acid; pyruvate family amino acid | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite |
| aniline [no description available] | 2.04 | 1 | 0 | anilines; primary arylamine | |
| 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. | 10.2 | 38 | 7 | 17-oxo steroid; 3-oxo-Delta(4) steroid; androstanoid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
| lactose Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose. | 2.01 | 1 | 0 | lactose | |
| 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. | 1.98 | 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 |
| desoxycorticosterone Desoxycorticosterone: A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE | 5.89 | 2 | 2 | 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; mineralocorticoid; primary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| 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. | 2.74 | 3 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| uracil mustard Uracil Mustard: Nitrogen mustard derivative of URACIL. It is a alkylating antineoplastic agent that is used in lymphatic malignancies, and causes mainly gastrointestinal and bone marrow damage. | 2.04 | 1 | 0 | aminouracil; nitrogen mustard | |
| 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. | 2.44 | 2 | 0 | penicillin | antibacterial agent; antibacterial drug |
| cycloheximide Cycloheximide: Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.. cycloheximide : A dicarboximide that is 4-(2-hydroxyethyl)piperidine-2,6-dione in which one of the hydrogens attached to the carbon bearing the hydroxy group is replaced by a 3,5-dimethyl-2-oxocyclohexyl group. It is an antibiotic produced by the bacterium Streptomyces griseus. | 2.69 | 3 | 0 | antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol | anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor |
| fluocinolone acetonide Fluocinolone Acetonide: A glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732). fluocinolone acetonide : A fluorinated steroid that is flunisolide in which the hydrogen at position 9 is replaced by fluorine. A corticosteroid with glucocorticoid activity, it is used (both as the anhydrous form and as the dihydrate) in creams, gels and ointments for the treatment of various skin disorders. | 2.45 | 2 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic ketal; fluorinated steroid; glucocorticoid; organic heteropentacyclic compound; primary alpha-hydroxy ketone | anti-inflammatory drug; antipruritic drug |
| 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. | 9.4 | 23 | 11 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound; tertiary alcohol | progestin; synthetic oral contraceptive |
| triaziquone Triaziquone: Alkylating antineoplastic agent used mainly for ovarian tumors. It is toxic to skin, gastrointestinal tract, bone marrow and kidneys.. triaziquone : A member of the class of 1,4-benzoquinones that is 1,4-benzoquinone in which three of the ring hydrogens are replaced by aziridin-1-yl groups. | 2.04 | 1 | 0 | 1,4-benzoquinones; aziridines | alkylating agent; antineoplastic agent |
| 17-alpha-hydroxyprogesterone 17alpha-hydroxyprogesterone : A 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone. | 8.82 | 20 | 5 | 17alpha-hydroxy-C21-steroid; 17alpha-hydroxy steroid; tertiary alpha-hydroxy ketone | human metabolite; metabolite; mouse metabolite; progestin |
| 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. | 2.44 | 2 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 2.45 | 2 | 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] | 2.75 | 3 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| trifluridine Trifluridine: An antiviral derivative of THYMIDINE used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to HERPES SIMPLEX virus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p557). trifluridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-trifluoromethyluracil as the nucleobase. An antiviral drug used mainly in the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis. | 2.04 | 1 | 0 | nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; EC 2.1.1.45 (thymidylate synthase) inhibitor |
| medroxyprogesterone acetate [no description available] | 13.3 | 60 | 15 | 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 |
| sulfobromophthalein sodium bromosulfophthalein sodium : An organic sodium salt that is the disodium salt of bromosulfophthalein.. bromosulfophthalein : An organosulfonic acid that consists of phthalide bearing four bromo substituents at positions 4, 5, 6 and 7 as well as two 4-hydroxy-3-sulfophenyl groups both located at position 1. | 2.45 | 2 | 0 | organic sodium salt | dye |
| valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine. | 4.32 | 1 | 1 | L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine | algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| mestranol [no description available] | 2.07 | 1 | 0 | 17beta-hydroxy steroid; aromatic ether; terminal acetylenic compound | prodrug; xenoestrogen |
| 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. | 4.68 | 3 | 2 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| propane Propane: A three carbon alkane with the formula H3CCH2CH3. | 2.01 | 1 | 0 | alkane; gas molecular entity | food propellant |
| acetonitrile acetonitrile: RN given refers to unlabeled cpd. acetonitrile : A nitrile that is hydrogen cyanide in which the hydrogen has been replaced by a methyl group. | 2.06 | 1 | 0 | aliphatic nitrile; volatile organic compound | EC 3.5.1.4 (amidase) inhibitor; NMR chemical shift reference compound; polar aprotic solvent |
| trifluoroethanol Trifluoroethanol: A non-aqueous co-solvent that serves as tool to study protein folding. It is also used in various pharmaceutical, chemical and engineering applications. | 2.01 | 1 | 0 | fluoroalcohol | |
| dalapon dalapon: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | carboxylic acid; organohalogen compound | |
| trichloroacetic acid Trichloroacetic Acid: A strong acid used as a protein precipitant in clinical chemistry and also as a caustic for removing warts.. trichloroacetic acid : A monocarboxylic acid that is acetic acid in which all three methyl hydrogens are substituted by chlorine. | 3.41 | 1 | 1 | monocarboxylic acid; organochlorine compound | carcinogenic agent; metabolite; mouse metabolite |
| trifluoroacetic acid Trifluoroacetic Acid: A very strong halogenated derivative of acetic acid. It is used in acid catalyzed reactions, especially those where an ester is cleaved in peptide synthesis.. trifluoroacetic acid : A monocarboxylic acid that is the trifluoro derivative of acetic acid. | 2.06 | 1 | 0 | fluoroalkanoic acid | human xenobiotic metabolite; NMR chemical shift reference compound; reagent |
| 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. | 2.73 | 3 | 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. | 3.36 | 1 | 1 | 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. | 2.04 | 1 | 0 | benzenes; piperidines | anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug |
| methylpentynol methylpentynol: structure | 2.04 | 1 | 0 | ynone | |
| dichloroacetic acid [no description available] | 2.04 | 1 | 0 | monocarboxylic acid; organochlorine compound | astringent; marine metabolite |
| pantothenic acid Pantothenic Acid: A butyryl-beta-alanine that can also be viewed as pantoic acid complexed with BETA ALANINE. It is incorporated into COENZYME A and protects cells against peroxidative damage by increasing the level of GLUTATHIONE.. pantothenic acid : A member of the class of pantothenic acids that is an amide formed from pantoic acid and beta-alanine.. vitamin B5 : Any member of a group of vitamers that belong to the chemical structural class called pantothenic acids that exhibit biological activity against vitamin B5 deficiency. Deficiency of vitamin B5 is rare due to its widespread distribution in whole grain cereals, legumes and meat. Symptoms associated with vitamin B5 deficiency are difficult to asses since they are subtle and resemble those of other B vitamin deficiencies. The vitamers include (R)-pantothenic acid and its ionized and salt forms.. (R)-pantothenate : A pantothenate that is the conjugate base of (R)-pantothenic acid, obtained by deprotonation of the carboxy group.. (R)-pantothenic acid : A pantothenic acid having R-configuration. | 2 | 1 | 0 | pantothenic acid; vitamin B5 | antidote to curare poisoning; geroprotector; human blood serum metabolite |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 2.74 | 3 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| phanquinone phanquinone: structure. phanquone : An orthoquinone that is the 5,6-diketo derivative of 4,7-phenanthroline. | 7.02 | 1 | 0 | orthoquinones | |
| 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. | 2.44 | 2 | 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. | 2.44 | 2 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| 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. | 2.45 | 2 | 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 |
| tolonium chloride Tolonium Chloride: A phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery.. tolonium chloride : An organic chloride salt having 3-amino-7-(dimethylamino)-2-methylphenothiazin-5-ium (tolonium) as the counterion. It is a blue nuclear counterstain that can be used to demonstrate Nissl substance and is also useful for staining mast cell granules, both in metachromatic and orthochromatic techniques. | 2 | 1 | 0 | ||
| fenoprop fenoprop: RN given is for parent cpd; structure | 2.04 | 1 | 0 | monocarboxylic acid | phenoxy herbicide |
| 2-methyl-4-chlorophenoxyacetic acid 2-Methyl-4-chlorophenoxyacetic Acid: A powerful herbicide used as a selective weed killer.. (4-chloro-2-methylphenoxy)acetic acid : A chlorophenoxyacetic acid that is (4-chlorophenoxy)acetic acid substituted by a methyl group at position 2. | 2.04 | 1 | 0 | chlorophenoxyacetic acid; monochlorobenzenes | environmental contaminant; phenoxy herbicide; synthetic auxin |
| 1,2-dibromo-3-chloropropane 1,2-dibromo-3-chloropropane: RN given refers to cpd with specified locants for bromine & chlorine moieties | 2.01 | 1 | 0 | organochlorine compound | |
| trehalose alpha,alpha-trehalose : A trehalose in which both glucose residues have alpha-configuration at the anomeric carbon. | 2.01 | 1 | 0 | trehalose | Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| dicloran 2,6-dichloro-4-nitroaniline : A nitroaniline that is 4-nitroaniline in which the hydrogens at positions 2 and 6 are replaced by chlorines. An agricultural fungicide, it is not approved for use in the European Union. | 2.04 | 1 | 0 | aromatic fungicide; dichlorobenzene; nitroaniline | antifungal agrochemical |
| phenylhydrazine [no description available] | 2.04 | 1 | 0 | phenylhydrazines | xenobiotic |
| dyrene dyrene: structure. anilazine : A member of the class of triazenes that is dichlorotriazene in which the hydrogen is replaced by an o-chloroanilino group. A fungicide formerly used to control leaf spots and downy mildew, it is no longer approved for use within the European Union. | 2.04 | 1 | 0 | monochlorobenzenes; organochlorine pesticide; secondary amino compound; triazines | antifungal agrochemical |
| 2-ethylhexanol [no description available] | 2.21 | 1 | 0 | primary alcohol | plant metabolite; volatile oil component |
| acrolein [no description available] | 2.04 | 1 | 0 | enal | herbicide; human xenobiotic metabolite; toxin |
| pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen. | 4.14 | 3 | 1 | pyrrole; secondary amine | |
| 2,5-hexanedione 2,5-hexanedione: metabolite of methyl-n-butyl ketone. 2,5-hexanedione : A diketone that is hexane substituted by oxo groups at positions 2 and 5. It is a toxic metabolite of hexane and of 2-hexanone | 8.5 | 2 | 0 | diketone; methyl ketone | human xenobiotic metabolite; neurotoxin |
| 1-hexanol 1-hexanol: RN given refers to parent cpd. hexanol : A fatty alcohol consisting of a hydroxy function at any position of an unbranched saturated chain of six carbon atoms.. hexan-1-ol : A primary alcohol that is hexane substituted by a hydroxy group at position 1. | 2.21 | 1 | 0 | hexanol; primary alcohol | alarm pheromone; antibacterial agent; fragrance; plant metabolite |
| tetraethylenepentamine [no description available] | 2.04 | 1 | 0 | polyazaalkane | copper chelator |
| ergotamine Ergotamine: A vasoconstrictor found in ergot of Central Europe. It is a serotonin agonist that has been used as an oxytocic agent and in the treatment of MIGRAINE DISORDERS.. ergotamine : A peptide ergot alkaloid that is dihydroergotamine in which a double bond replaces the single bond between positions 9 and 10. | 2.44 | 2 | 0 | peptide ergot alkaloid | alpha-adrenergic agonist; mycotoxin; non-narcotic analgesic; oxytocic; serotonergic agonist; vasoconstrictor agent |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 2.06 | 1 | 0 | ergoline alkaloid | |
| neostigmine bromide neostigmine bromide : The bromide salt of neostigmine. | 2.46 | 2 | 0 | bromide salt | |
| 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. | 2.05 | 1 | 0 | biguanides | antineoplastic agent; geroprotector; hypoglycemic agent |
| chloranil Chloranil: A quinone fungicide used for treatment of seeds and foliage.. tetrachloro-1,4-benzoquinone : A member of the class of 1,4-benzoquiones that is 1,4-benzoquinone in which all four hydrogens are substituted by chlorines. | 2.04 | 1 | 0 | 1,4-benzoquinones; organochlorine compound | EC 2.7.1.33 (pantothenate kinase) inhibitor; metabolite |
| amiben Amiben: RN given refers to parent cpd | 2.04 | 1 | 0 | chlorobenzoic acid | |
| 1-naphthylamine 1-Naphthylamine: A suspected industrial carcinogen (and listed as such by OSHA). Its N-hydroxy metabolite is strongly carcinogenic and mutagenic.. naphthylamine : A primary arylamine that is naphthalene substituted by an amino group at unspecified position.. 1-naphthylamine : A naphthylamine that is naphthalene substituted by an amino group at position 1. | 3.78 | 2 | 1 | naphthylamine | human xenobiotic metabolite |
| monuron monuron: minor descriptor (72-83); on-line & Index Medicus search UREA/AA (72-74) & HERBICIDES (72-74) & HERBICIDES UREA (75-83); RN given refers to unlabeled cpd; structure. monuron : A member of the class of 3-(3,4-substituted-phenyl)-1,1-dimethylureas that is urea in which one of the nitrogens is substituted by a p-chlorophenyl group while the other is substituted by two methyl groups. | 2.04 | 1 | 0 | 3-(3,4-substituted-phenyl)-1,1-dimethylurea; monochlorobenzenes | environmental contaminant; herbicide; xenobiotic |
| sterogenol hexadecylpyridinium bromide: structure in first source. cetylpyridinium bromide : A pyridinium salt that has N-hexadecylpyridinium as the cation and bromide as the anion. | 2.05 | 1 | 0 | bromide salt; pyridinium salt | antiseptic drug; EC 2.7.11.18 (myosin-light-chain kinase) inhibitor; surfactant |
| iminodiacetic acid iminodiacetic acid: used as hepatobiliary imaging agent when labeled with Tc; RN given refers to parent cpd; structure. iminodiacetic acid : An amino dicarboxylic acid that is glycine in which one of the hydrogens attached to the nitrogen is substituted by a carboxymethyl group. | 2.04 | 1 | 0 | amino dicarboxylic acid; glycine derivative; non-proteinogenic alpha-amino acid | chelator |
| 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. | 2.04 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| methohexital Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups. | 2.04 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| cycloguanil cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil. | 2.05 | 1 | 0 | triazines | antifolate; antiinfective agent; antimalarial; antiparasitic agent; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| dydrogesterone [no description available] | 3.17 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid | progestin |
| phenetidine Phenetidine: Used in the manufacture of acetophenetidin.. 4-ethoxyaniline : An aromatic ether that is aniline in which the hydrogen at position 4 is replaced by an ethoxy group. It is a hydrolysis metabolite of phenacetin. | 2.04 | 1 | 0 | aromatic ether; primary amino compound; substituted aniline | drug metabolite |
| diazooxonorleucine Diazooxonorleucine: An amino acid that inhibits phosphate-activated glutaminase and interferes with glutamine metabolism. It is an antineoplastic antibiotic produced by an unidentified species of Streptomyces from Peruvian soil. (From Merck Index, 11th ed). 6-diazo-5-oxo-L-norleucine : A non-proteinogenic L-alpha-amino acid that is L-norleucine which is substituted at position 5 by an oxo group and at position 6 by a diazo group. It is as inhibitor of various glutamine-utilising enzymes. | 2.04 | 1 | 0 | amino acid zwitterion; diazo compound; ketone; non-proteinogenic L-alpha-amino acid | analgesic; antibacterial agent; antimetabolite; antineoplastic agent; antiviral agent; apoptosis inducer; bacterial metabolite; EC 2.4.2.14 (amidophosphoribosyltransferase) inhibitor; EC 3.5.1.2 (glutaminase) inhibitor; EC 6.3.4.2 [CTP synthase (glutamine hydrolyzing)] inhibitor; EC 6.3.5.1 [NAD(+) synthase (glutamine-hydrolysing)] inhibitor; EC 6.3.5.2 [GMP synthase (glutamine-hydrolysing)] inhibitor; EC 6.3.5.3 (phosphoribosylformylglycinamidine synthase) inhibitor; EC 6.3.5.4 [asparagine synthase (glutamine-hydrolysing)] inhibitor; EC 6.3.5.5 [carbamoyl-phosphate synthase (glutamine-hydrolysing)] inhibitor; glutamine antagonist |
| 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. | 3.53 | 2 | 0 | azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines | |
| thiazoles [no description available] | 2.41 | 2 | 0 | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| pyrazines Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms. | 3.12 | 1 | 0 | diazine; pyrazines | Daphnia magna metabolite |
| di-2-(ethylhexyl)phosphoric acid di-2-(ethylhexyl)phosphoric acid: RN given refers to parent cpd | 2.21 | 1 | 0 | ||
| chlormadinone acetate Chlormadinone Acetate: An orally active synthetic progestational hormone used often in combinations as an oral contraceptive (CONTRACEPTIVES, ORAL). | 9.74 | 20 | 10 | corticosteroid hormone | |
| pirinitramide Pirinitramide: A diphenylpropylamine with intense narcotic analgesic activity of long duration. It is a derivative of MEPERIDINE with similar activity and usage. | 2.04 | 1 | 0 | nitrile | |
| methylpentynol carbamate [no description available] | 2.04 | 1 | 0 | ||
| mechlorethamine n-oxide [no description available] | 2.04 | 1 | 0 | nitrogen mustard | |
| edrophonium bromide [no description available] | 2.04 | 1 | 0 | ||
| evans blue Evans Blue: An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly.. Evans blue : An organic sodium salt that is the tetrasodium salt of 6,6'-{(3,3'-dimethyl[1,1'-biphenyl]-4,4'-diyl)bis[diazene-2,1-diyl]}bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate). It is sometimes used as a counterstain, especially in fluorescent methods to suppress background autofluorescence. | 2.66 | 3 | 0 | organic sodium salt | fluorochrome; histological dye; sodium channel blocker; teratogenic agent |
| testosterone enanthate [no description available] | 8.38 | 12 | 7 | heptanoate ester; sterol ester | androgen |
| 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. | 2.44 | 2 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| linuron Linuron: A selective pre- and post-emergence herbicide. (From Merck Index, 11th ed). linuron : A member of the class of phenylureas that is N-methyl urea substituted by a methoxy group at position 1 and a 3,4-dichlorophenyl group at position 3. | 2.04 | 1 | 0 | dichlorobenzene; phenylureas | agrochemical; environmental contaminant; herbicide; xenobiotic |
| carbutamide Carbutamide: A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277) | 2.04 | 1 | 0 | benzenes; sulfonamide | |
| 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. | 2.04 | 1 | 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. | 3.48 | 1 | 1 | steroid ester | |
| 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) | 2.74 | 3 | 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] | 12.52 | 39 | 16 | 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. | 10.18 | 13 | 5 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid | human metabolite |
| hydantoins Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4. | 2.04 | 1 | 0 | imidazolidine-2,4-dione | |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 2.45 | 2 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| ketobemidone ketobemidone: structure | 2.04 | 1 | 0 | piperidines | |
| glycyrrhetinic acid [no description available] | 2.07 | 1 | 0 | cyclic terpene ketone; hydroxy monocarboxylic acid; pentacyclic triterpenoid | immunomodulator; plant metabolite |
| plumbagin plumbagin: a superoxide anion generator. plumbagin : A hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively. | 2.04 | 1 | 0 | hydroxy-1,4-naphthoquinone; phenols | anticoagulant; antineoplastic agent; immunological adjuvant; 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. | 2.45 | 2 | 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 |
| pamaquine pamaquine: structure; RN given refers to parent cpd | 2.04 | 1 | 0 | aminoquinoline | |
| 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. | 2.01 | 1 | 0 | amphetamines; phenethylamine alkaloid | plant metabolite |
| benzohydroxamic acid [no description available] | 2.05 | 1 | 0 | ||
| alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups. | 2.25 | 1 | 0 | ||
| mustard gas Mustard Gas: Severe irritant and vesicant of skin, eyes, and lungs. It may cause blindness and lethal lung edema and was formerly used as a war gas. The substance has been proposed as a cytostatic and for treatment of psoriasis. It has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP-85-002, 1985) (Merck, 11th ed).. bis(2-chloroethyl) sulfide : An ethyl sulfide that is diethyl sulfide in which a hydrogen from each of the terminal methyl groups is replaced by a chlorine. It is a powerful vesicant regulated under the Chemical Weapons Convention. | 2.04 | 1 | 0 | ethyl sulfide; organochlorine compound | alkylating agent; carcinogenic agent; vesicant |
| hesperidin Hesperidin: A flavanone glycoside found in CITRUS fruit peels.. hesperidin : A disaccharide derivative that consists of hesperetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. | 2.04 | 1 | 0 | 3'-hydroxyflavanones; 4'-methoxyflavanones; dihydroxyflavanone; disaccharide derivative; flavanone glycoside; monomethoxyflavanone; rutinoside | mutagen |
| medroxyprogesterone [no description available] | 9.16 | 17 | 1 | 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. | 10.33 | 29 | 13 | 17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
| apronalide apronalide: structure | 2.04 | 1 | 0 | N-acylurea | |
| chlormethiazole Chlormethiazole: A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors. | 2.04 | 1 | 0 | thiazoles | |
| 4,6-dinitro-o-cresol 4,6-dinitro-o-cresol: RN given refers to parent cpd; structure. 4,6-dinitro-o-cresol : A hydroxytoluene that is o-cresol carrying nitro substituents at positions 4 and 6. | 2.04 | 1 | 0 | dinitrophenol acaricide; hydroxytoluene; nitrotoluene | dinitrophenol insecticide; fungicide; herbicide |
| 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. | 2.46 | 2 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| lithium carbonate Lithium Carbonate: A lithium salt, classified as a mood-stabilizing agent. Lithium ion alters the metabolism of BIOGENIC MONOAMINES in the CENTRAL NERVOUS SYSTEM, and affects multiple neurotransmission systems. | 2.42 | 2 | 0 | carbonate salt; lithium salt | antimanic drug |
| metahexamide metahexamide: major descriptor (64-83); on-line search SULFONYLUREA COMPOUNDS (64-83); Index Medicus search METAHEXAMIDE (64-83); RN given refers to parent cpd; structure | 2.04 | 1 | 0 | benzenes; sulfonamide | |
| 2-hydroxybutyric acid 2-hydroxybutyric acid: RN given refers to cpd without isomeric designation. hydroxybutyric acid : Any compound comprising a butyric acid core carrying at least one hydroxy substituent.. 2-hydroxybutyric acid : A hydroxybutyric acid having a single hydroxyl group located at position 2; urinary secretion of 2-hydroxybutyric acid is increased with alcohol ingestion or vigorous physical exercise and is associated with lactic acidosis and ketoacidosis in humans and diabetes in animals. | 2.99 | 1 | 0 | 2-hydroxy monocarboxylic acid; hydroxybutyric acid | algal metabolite; human metabolite |
| chlorotrianisene Chlorotrianisene: A powerful synthetic, non-steroidal estrogen. | 3.08 | 1 | 0 | chloroalkene | antineoplastic agent; estrogen receptor modulator; xenoestrogen |
| docusate Dioctyl Sulfosuccinic Acid: All-purpose surfactant, wetting agent, and solubilizer used in the drug, cosmetics, and food industries. It has also been used in laxatives and as cerumenolytics. It is usually administered as either the calcium, potassium, or sodium salt. | 3.28 | 5 | 0 | diester; organosulfonic acid | |
| megestrol acetate [no description available] | 4.29 | 7 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| toyocamycin Toyocamycin: 4-Amino-5-cyano-7-(D-ribofuranosyl)-7H- pyrrolo(2,3-d)pyrimidine. Antibiotic antimetabolite isolated from Streptomyces toyocaensis cultures. It is an analog of adenosine, blocks RNA synthesis and ribosome function, and is used mainly as a tool in biochemistry.. toyocamycin : An N-glycosylpyrrolopyrimidine that is tubercidin in which the hydrogen at position 5 of the pyrrolopyrimidine moiety has been replaced by a cyano group. | 2.04 | 1 | 0 | antibiotic antifungal agent; N-glycosylpyrrolopyrimidine; nitrile; ribonucleoside | antimetabolite; antineoplastic agent; apoptosis inducer; bacterial metabolite |
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 2.47 | 2 | 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 |
| phendimetrazine phendimetrazine: minor descriptor (66-86); file maintained to MORPHOLINES (66-86); on-line & INDEX MEDICUS search MORPHOLINES (66-86); RN given refers to parent cpd without isomeric designation | 2.07 | 1 | 0 | ||
| 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. | 4.53 | 5 | 1 | cyclic ketone; erythromycin | |
| dehydroepiandrosterone sulfate Dehydroepiandrosterone Sulfate: The circulating form of a major C19 steroid produced primarily by the ADRENAL CORTEX. DHEA sulfate serves as a precursor for TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE.. dehydroepiandrosterone sulfate : A steroid sulfate that is the 3-sulfooxy derivative of dehydroepiandrosterone. | 7.16 | 21 | 5 | 17-oxo steroid; steroid sulfate | EC 2.7.1.33 (pantothenate kinase) inhibitor; human metabolite; mouse metabolite |
| hadacidin hadacidin: inhibitor of AMP synthesis; RN given refers to parent cpd; structure. hadacidin : A monocarboxylic acid that is N-hydroxyglycine in which the hydrogen attached to the nitrogen is replaced by a formyl group. It was originally isolated from cultures of Penicillium frequentans. | 2.04 | 1 | 0 | aldehyde; monocarboxylic acid; N-hydroxy-alpha-amino-acid | antimicrobial agent; antineoplastic agent; Penicillium metabolite; teratogenic agent |
| carbophenothion carbophenothion: structure | 2.04 | 1 | 0 | organic sulfide | |
| 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. | 14.57 | 12 | 5 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| porfiromycin Porfiromycin: Toxic antibiotic of the mitomycin group, obtained from MITOMYCIN and also from Streptomyces ardus and other species. It is proposed as an antineoplastic agent, with some antibiotic properties. | 2.04 | 1 | 0 | ||
| 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. | 3.41 | 1 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; anabolic androgenic steroid | |
| lormetazepam lormetazepam: RN given refers to cpd with specified locant for methyl group; structure given in first source. lormetazepam : A 1,4-benzodiazepinone compound having a methyl substituent at the 1-position, a hydroxy substituent at the 3-position, a 2-chlorophenyl group at the 5-position and a chloro substituent at the 7-position. | 2.04 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | sedative |
| vinblastine [no description available] | 2.44 | 2 | 0 | ||
| n-methylpyrrolidone 1-methylpyrrolidin-2-one: structure in first source. N-methylpyrrolidin-2-one : A member of the class of pyrrolidine-2-ones that is pyrrolidin-2-one in which the hydrogen attached to the nitrogen is replaced by a methyl group. | 2.47 | 2 | 0 | lactam; N-alkylpyrrolidine; pyrrolidin-2-ones | polar aprotic solvent |
| deoxycytidine [no description available] | 3.86 | 3 | 0 | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| deoxyuridine [no description available] | 2.04 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| testolactone Testolactone: An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. | 4.32 | 4 | 1 | 3-oxo-Delta(1),Delta(4)-steroid; seco-androstane | |
| 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. | 2.44 | 2 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| pyrithioxin Pyrithioxin: A neurotropic agent which reduces permeability of blood-brain barrier to phosphate. It has no vitamin B6 activity. | 2.04 | 1 | 0 | methylpyridines | |
| arsenic trioxide Arsenic Trioxide: An inorganic compound with the chemical formula As2O3 that is used for the treatment of ACUTE PROMYELOCYTIC LEUKEMIA in patients who have relapsed from, or are resistant to, conventional drug therapy. | 3.12 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| nsc 65346 sangivamycin: RN given refers to parent cpd. sangivamycin : A nucleoside analogue that is adenosine in which the nitrogen at position 7 is replaced by a carbamoyl-substituted carbon. It is a potent inhibitor of protein kinase C. | 2.04 | 1 | 0 | nucleoside analogue | protein kinase inhibitor |
| 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. | 2.54 | 2 | 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 |
| guanazole Guanazole: A cytostatic triazole derivative which is not to be confused with guanazolo, the generic name for 8-azaguanine.. guanazole : An aromatic amine that is 1,2,4-triazole substituted at positions 3 and 5 by amino groups. | 2.04 | 1 | 0 | aromatic amine; triazoles | antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor |
| metylperon metylperon: RN given refers to parent cpd | 2.04 | 1 | 0 | aromatic ketone | |
| meturedepa meturedepa: structure in Merck Index, 9th ed, #6031 | 2.04 | 1 | 0 | phosphoramide | |
| ioxynil ioxynil: RN given refers to parent cpd; structure. ioxynil : A nitrile that is benzonitrile substituted by a hydroxy group at position 4 and iodo groups at positions 3 and 5. | 2.04 | 1 | 0 | iodophenol; nitrile | environmental contaminant; herbicide; xenobiotic |
| bromoxynil bromoxynil: RN given refers to parent cpd; structure. 3,5-dibromo-4-hydroxybenzonitrile : A dibromobenzene that is 2,6-dibromophenol substituted by a cyano group at position 4. | 2.04 | 1 | 0 | dibromobenzene; hydroxynitrile; phenols | environmental contaminant; herbicide; xenobiotic |
| 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. | 2.04 | 1 | 0 | cyclic acetal; cyclic hemiketal; cyclic ketone; pyranobenzodioxin; secondary alcohol; secondary amino compound | antibacterial drug; antimicrobial agent; bacterial metabolite |
| picloram Picloram: A picolinic acid derivative that is used as a herbicide.. picloram : A pyridinemonocarboxylic acid that is pyridine-2-carboxylic acid which is substituted by a chloro group at positions 3,5 and 6, and by an amino group at position 4. It is a systemic herbicide used to control deeply rooted herbaceous weeds and woody plants in rights-of-way, forestry, range lands, pastures, and small grain crops. | 2.04 | 1 | 0 | aminopyridine; chloropyridine; organochlorine pesticide; pyridinemonocarboxylic acid | herbicide; synthetic auxin |
| ethoglucid Ethoglucid: Alkylating antineoplastic agent used especially in bladder neoplasms. It is toxic to hair follicles, gastro-intestinal tract, and vasculature. | 2.04 | 1 | 0 | epoxide | |
| 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. | 2.04 | 1 | 0 | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| benperidol Benperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It has been used in the treatment of aberrant sexual behavior. (From Martindale, The Extra Pharmacopoeia, 30th ed, p567) | 2.04 | 1 | 0 | aromatic ketone | |
| azaribine azaribine: pyrimidine analogue; anti-metabolite used in psoriasis & mycosis fungoides;. azaribine : A N-glycosyl-1,2,4-triazine that is 6-azauridine acetylated at positions 2', 3' and 5' on the sugar ring. It is a prodrug for 6-azauridine and is used for treatment of psoriasis. | 2.04 | 1 | 0 | acetate ester; N-glycosyl-1,2,4-triazine | antipsoriatic; prodrug |
| methylprednisolone hemisuccinate Methylprednisolone Hemisuccinate: A water-soluble ester of METHYLPREDNISOLONE used for cardiac, allergic, and hypoxic emergencies. | 2.42 | 2 | 0 | corticosteroid hormone; hemisuccinate | |
| sulfadoxine Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial. | 2.47 | 2 | 0 | pyrimidines; sulfonamide | antibacterial drug; antimalarial |
| 1,3,5-triglycidyl-s-triazinetrione [no description available] | 2.04 | 1 | 0 | ||
| acetophenazine acetophenazine: major descriptor (73-85); minor descriptor (64-72); on-line search PHENOTHIAZINES (64-85); Index Medicus search PHENOTHIAZINES (64-72); ACETOPHENAZINE (73-85); RN given refers to parent cpd. acetophenazine : A member of the class of phenothiazines that is 10H-phenothiazine substituted by a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at the nitogen atom and an acetyl group at position 2. | 2.45 | 2 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; phenothiazines | phenothiazine antipsychotic drug |
| chlordesmethyldiazepam [no description available] | 2.04 | 1 | 0 | benzodiazepine | |
| 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 | 2.46 | 2 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| doxifluridine doxifluridine : A pyrimidine 5'-deoxyribonucleoside that is 5-fluorouridine in which the hydroxy group at the 5' position is replaced by a hydrogen. It is an oral prodrug of the antineoplastic agent 5-fluorouracil. Designed to circumvent the rapid degradation of 5-fluorouracil by dihydropyrimidine dehydrogenase in the gut wall, it is converted into 5-fluorouracil in the presence of pyrimidine nucleoside phosphorylase. | 2.73 | 3 | 0 | organofluorine compound; pyrimidine 5'-deoxyribonucleoside | antimetabolite; antineoplastic agent; prodrug |
| 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. | 2.44 | 2 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| fluorescein-5-isothiocyanate Fluorescein-5-isothiocyanate: Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.. fluorescein 5-isothiocyanate : The 5-isomer of fluorescein isothiocyanate. Acts as a fluorescent probe capable of being conjugated to tissue and proteins; used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques. | 2 | 1 | 0 | fluorescein isothiocyanate | |
| improsan improsan: synonyms NSC-102627, alkylating agent 864 & yoshi 864 refer to HCl; RN given refers to parent cpd; structure | 2.04 | 1 | 0 | organosulfonic ester | |
| 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. | 2.88 | 4 | 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] | 2.44 | 2 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| butylhydroxybutylnitrosamine Butylhydroxybutylnitrosamine: A substituted carcinogenic nitrosamine.. N-butyl-N-(4-hydroxybutyl)nitrosamine : A nitrosamine that has butyl and 4-hydroxybutyl substituents. In mice, it causes high-grade, invasive cancers in the urinary bladder, but not in any other tissues. | 2.9 | 4 | 0 | nitrosamine; primary alcohol | carcinogenic agent |
| piperacetazine piperacetazine: was MH 1975-91 (see under PHENOTHIAZINE TRANQUILIZERS 1975-90) | 2.04 | 1 | 0 | phenothiazines | |
| cladribine [no description available] | 2.04 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| beclomethasone [no description available] | 2.75 | 3 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; chlorinated steroid; corticosteroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | anti-asthmatic drug; anti-inflammatory drug |
| pyrodifenium bromide pyrodifenium bromide: was heading 1976-94 (see under PYRROLIDINES 1976-90); PRIFINIUM BROMIDE was see PYRODIFENIUM BROMIDE 1976-94: use PYRROLIDINES to search PYRODIFENIUM BROMIDE 1976-94; quaternary ammonium anticholinergic agent more specific for the gastrointestinal tract than atropine | 2.05 | 1 | 0 | organic molecular entity | |
| 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. | 2.44 | 2 | 0 | penicillin allergen; penicillin | antibacterial drug |
| 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. | 2.44 | 2 | 0 | penicillin allergen; penicillin | antibacterial drug |
| pentaquine pentaquine: RN given refers to parent cpd | 2.04 | 1 | 0 | ||
| beclomethasone dipropionate beclomethasone dipropionate : A steroid ester comprising beclomethasone having propionyl groups at the 17- and 21-positions. | 2.04 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid; chlorinated steroid; corticosteroid; enone; glucocorticoid; propanoate ester; steroid ester | anti-arrhythmia drug; anti-asthmatic drug; anti-inflammatory drug; prodrug |
| limonene Limonene: A naturally-occurring class of MONOTERPENES which occur as a clear colorless liquid at room temperature. Limonene is the major component in the oil of oranges which has many uses, including as flavor and fragrance. It is recognized as safe in food by the Food and Drug Administration (FDA).. limonene : A monoterpene that is cyclohex-1-ene substituted by a methyl group at position 1 and a prop-1-en-2-yl group at position 4 respectively. | 7.02 | 1 | 0 | cycloalkene; p-menthadiene | human metabolite |
| olsalazine olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease. | 2.04 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| terodiline [no description available] | 2.04 | 1 | 0 | diarylmethane | |
| 1-(4-carboxyphenyl)-3,3-dimethyltriazene 1-(4-carboxyphenyl)-3,3-dimethyltriazene: RN given refers to parent cpd | 2.04 | 1 | 0 | ||
| lutetium Lutetium: An element of the rare earth family of metals. It has the atomic symbol Lu, atomic number 71, and atomic weight 175. | 2.31 | 1 | 0 | d-block element atom; lanthanoid atom | |
| neodymium Neodymium: An element of the rare earth family of metals. It has the atomic symbol Nd, atomic number 60, and atomic weight 144.24, and is used in industrial applications. | 1.98 | 1 | 0 | f-block element atom; lanthanoid atom | |
| palladium Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46. | 6.92 | 8 | 1 | metal allergen; nickel group element atom; platinum group metal atom | |
| samarium Samarium: An element of the rare earth family of metals. It has the atomic symbol Sm, atomic number 62, and atomic weight 150.36. The oxide is used in the control rods of some nuclear reactors. | 2.05 | 1 | 0 | f-block element atom; lanthanoid atom | |
| technetium Technetium: The first artificially produced element and a radioactive fission product of URANIUM. Technetium has the atomic symbol Tc, and atomic number 43. All technetium isotopes are radioactive. Technetium 99m (m=metastable) which is the decay product of Molybdenum 99, has a half-life of about 6 hours and is used diagnostically as a radioactive imaging agent. Technetium 99 which is a decay product of technetium 99m, has a half-life of 210,000 years. | 7.47 | 2 | 0 | manganese group element atom | |
| titanium Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures. | 2 | 1 | 0 | titanium group element atom | |
| cadmium Cadmium: An element with atomic symbol Cd, atomic number 48, and atomic weight 112.41. It is a metal and ingestion will lead to CADMIUM POISONING.. elemental cadmium : An element in the zinc group of the periodic table with atomic number 48, atomic mass 112, M.P. 321degreeC, and B.P. 765degreeC). An odourless, tasteless, and highly poisonous soft, ductile, lustrous metal with electropositive properties. It has eight stable isotopes: (106)Cd, (108)Cd,(110)Cd, (111)Cd, (112)Cd, (113)Cd, (114)Cd and (116)Cd, with (112)Cd and (114)Cd being the most common. | 1.98 | 1 | 0 | cadmium molecular entity; zinc group element atom | |
| gadolinium Gadolinium: An element of the rare earth family of metals. It has the atomic symbol Gd, atomic number 64, and atomic weight 157.25. Its oxide is used in the control rods of some nuclear reactors. | 2.13 | 1 | 0 | f-block element atom; lanthanoid atom | |
| yttrium Yttrium: An element of the rare earth family of metals. It has the atomic symbol Y, atomic number 39, and atomic weight 88.91. In conjunction with other rare earths, yttrium is used as a phosphor in television receivers and is a component of the yttrium-aluminum garnet (YAG) lasers. | 1.98 | 1 | 0 | d-block element atom; rare earth metal atom; scandium group element 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. | 2.44 | 2 | 0 | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| mercuric chloride Mercuric Chloride: Mercury chloride (HgCl2). A highly toxic compound that volatizes slightly at ordinary temperature and appreciably at 100 degrees C. It is corrosive to mucous membranes and used as a topical antiseptic and disinfectant.. mercury dichloride : A mercury coordination entity made up of linear triatomic molecules in which a mercury atom is bonded to two chlorines. Water-soluble, it is highly toxic. Once used in a wide variety of applications, including preserving wood and anatomical specimens, embalming and disinfecting, as an intensifier in photography, as a mordant for rabbit and beaver furs, and freeing gold from lead, its use has markedly declined as less toxic alternatives have been developed. | 1.99 | 1 | 0 | mercury coordination entity | sensitiser |
| phosphoric acid, trisodium salt [no description available] | 2.07 | 1 | 0 | sodium phosphate | |
| metocurine iodide [no description available] | 2.04 | 1 | 0 | aromatic ether | |
| camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source | 3.13 | 1 | 0 | delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite |
| ferrous sulfate ferrous sulfate: Ferro-Gradumet is ferrous sulfate in controlled release form; RN given refers to Fe(+2)[1:1] salt. iron(2+) sulfate (anhydrous) : A compound of iron and sulfate in which the ratio of iron(2+) to sulfate ions is 1:1. Various hydrates occur naturally - most commonly the heptahydrate, which loses water to form the tetrahydrate at 57degreeC and the monohydrate at 65degreeC. | 1.98 | 1 | 0 | iron molecular entity; metal sulfate | reducing agent |
| isopentenyladenosine Isopentenyladenosine: N(6)-[delta(3)-isopentenyl]adenosine. Isopentenyl derivative of adenosine which is a member of the cytokinin family of plant growth regulators.. N(6)-(Delta(2)-isopentenyl)adenosine : A nucleoside analogue in which adenosine has been modified by substitution at the 6-amino nitrogen by a Delta(2)-isopentenyl group. | 2.04 | 1 | 0 | N-ribosyl-N(6)-isopentenyladenine; nucleoside analogue | antineoplastic agent; plant growth regulator; plant metabolite |
| tricalcium phosphate tricalcium phosphate: a form of tricalcium phosphate used as bioceramic bone replacement material; see also records for alpha-tricalcium phosphate, beta-tricalcium phosphate, calcium phosphate; apatitic tricalcium phosphate Ca9(HPO4)(PO4)5(OH) is the calcium orthophosphate leading to beta tricalcium phosphate Ca3(PO4)2 (b-TCP). calcium phosphate : A calcium salt composed of calcium and phosphate/diphosphate ions; present in milk and used for the mineralisation of calcified tissues. | 2.31 | 1 | 0 | calcium phosphate | |
| deuterium Deuterium: The stable isotope of hydrogen. It has one neutron and one proton in the nucleus. | 2 | 1 | 0 | dihydrogen | |
| galactose aldohexose : A hexose with a (potential) aldehyde group at one end. | 2.81 | 3 | 0 | ||
| vasotocin Vasotocin: A nonapeptide that contains the ring of OXYTOCIN and the side chain of ARG-VASOPRESSIN with the latter determining the specific recognition of hormone receptors. Vasotocin is the non-mammalian vasopressin-like hormone or antidiuretic hormone regulating water and salt metabolism.. vasotocin : A heterodetic cyclic peptide that is homologous to oxytocin and vasopressin. It is a pituitary hormone that acts as an endocrine regulator for water balance, osmotic homoeostasis and is involved in social and sexual behavior in non-mammalian vertebrates. | 2.05 | 1 | 0 | ||
| ancitabine Ancitabine: Congener of CYTARABINE that is metabolized to cytarabine and thereby maintains a more constant antineoplastic action.. ancitabine : An organic heterotricyclic compound resulting from the formal condensation of the oxo group of cytidine to the 2' position with loss of water to give the corresponding cyclic ether. A prodrug, it is metabolised to the antineoplastic agent cytarabine, so is used to maintain a more constant antineoplastic action. | 2.04 | 1 | 0 | diol; organic heterotricyclic compound | antimetabolite; antineoplastic agent; prodrug |
| amopyroquine amopyroquine: RN given refers to parent cpd; structure | 2.05 | 1 | 0 | ||
| stanozolol Stanozolol: A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194). stanozolol : An organic heteropentacyclic compound resulting from the formal condensation of the 3-keto-aldehyde moiety of oxymetholone with hydrazine. Like oxymetholone, it is a synthetic anabolic steroid. It has both anabolic and androgenic properties, and has been used to treat hereditary angioedema and various vascular disorders. It has also been widely abused by professional athletes. | 2.03 | 1 | 0 | 17beta-hydroxy steroid; anabolic androgenic steroid; organic heteropentacyclic compound; tertiary alcohol | anabolic agent; androgen |
| phenacid phenacid: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | ||
| apazone Apazone: An anti-inflammatory agent used in the treatment of rheumatoid arthritis. It also has uricosuric properties and has been used to treat gout.. apazone : A member of the class of benzotriazines that is 1,2-dihydro-1,2,4-benzotriazine bearing a dimethylamino substitutent at position 3 and a methyl substituent at position 7 and in which the nitrogens at positions 1 and 2 are both acylated by a carboxy group of propylmalonic acid. | 2.04 | 1 | 0 | benzotriazines | non-steroidal anti-inflammatory drug; uricosuric drug |
| xipamide Xipamide: A sulfamoylbenzamide analog of CLOPAMIDE. It is diuretic and saluretic with antihypertensive activity. It is bound to PLASMA PROTEINS, thus has a delayed onset and prolonged action. | 2.45 | 2 | 0 | benzamides | |
| 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. | 2.74 | 3 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| levamisole Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine. | 2.45 | 2 | 0 | 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole | antinematodal drug; antirheumatic drug; EC 3.1.3.1 (alkaline phosphatase) inhibitor; immunological adjuvant; immunomodulator |
| clemastine Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions. | 2.47 | 2 | 0 | monochlorobenzenes; N-alkylpyrrolidine | anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic 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. | 2.44 | 2 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| isosorbide-5-mononitrate isosorbide-5-mononitrate: for prevention of angina pectoris; structure given in first source; a Russian drug | 2.44 | 2 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| pentamethylmelamine pentamethylmelamine: RN given refers to parent cpd | 2.04 | 1 | 0 | ||
| gestrinone Gestrinone: A non-estrogenic contraceptive which is a weak progestin with strong anti-progesterone properties. It is effective if used once a week orally or can also be used in intravaginal devices. | 7.81 | 6 | 1 | oxo steroid | |
| tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types. | 2.15 | 1 | 0 | acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester | antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator |
| fluorides [no description available] | 1.99 | 1 | 0 | halide anion; monoatomic fluorine | |
| calusterone calusterone: was MH 1975-92 (see under METHYLTESTOSTERONE 1975-90); use METHYLTESTOSTERONE to search CALUSTERONE 1975-92 | 2.04 | 1 | 0 | 3-hydroxy steroid | androgen |
| 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. | 13.92 | 61 | 17 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| lisuride Lisuride: An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS). | 2.04 | 1 | 0 | monocarboxylic acid amide | antidyskinesia agent; antiparkinson drug; dopamine agonist; serotonergic agonist |
| etoprine etoprine: do not confuse with 3,5-dicarbethoxy-2,6-dimethyl-4-ethyl-1,4-dihydropyridine, also called DDEP | 2.04 | 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. | 2.04 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| razoxane Razoxane: An antimitotic agent with immunosuppressive properties. | 2.04 | 1 | 0 | N-alkylpiperazine | |
| cephapirin Cephapirin: Cephalosporin antibiotic, partly plasma-bound, that is effective against gram-negative and gram-positive organisms.. cephapirin : A cephalosporin with acetoxymethyl and 2(pyridin-4-ylsulfanyl)acetamido substituents at positions 3 and 7, respectively, of the cephem skeleton. It is used (as its sodium salt) as an antibiotic, being effective against gram-negative and gram-positive organisms. | 2.44 | 2 | 0 | cephalosporin | antibacterial drug |
| 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. | 3.53 | 2 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| carbimazole Carbimazole: An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.. carbimazole : A member of the class of imidazoles that is methimazole in which the nitrogen bearing a hydrogen is converted into its ethoxycarbonyl derivative. A prodrug for methimazol, carbimazole is used for the treatment of hyperthyroidism. | 2.07 | 1 | 0 | 1,3-dihydroimidazole-2-thiones; carbamate ester | antithyroid drug; prodrug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 5.13 | 8 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| phenyl acetate phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid. | 3.2 | 5 | 0 | benzenes; phenyl acetates | |
| cetylpyridinium chloride anhydrous tserigel: according to first source contains polyvinylbutyral & cetylpyridinium chloride; UD only lists cetylpyridinium chloride as constituent. cetylpyridinium chloride : A pyridinium salt that has N-hexadecylpyridinium as the cation and chloride as the anion. It has antiseptic properties and is used in solutions or lozenges for the treatment of minor infections of the mouth and throat. | 4.41 | 2 | 2 | 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. | 2.75 | 3 | 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 |
| azetepa [no description available] | 2.04 | 1 | 0 | phosphoramide | |
| 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. | 1.99 | 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. | 6.33 | 4 | 2 | 3-hydroxy-5beta-pregnan-20-one; 3alpha-hydroxy steroid | human metabolite; intravenous anaesthetic; sedative |
| butylated hydroxytoluene 2,6-di-tert-butyl-4-methylphenol : A member of the class of phenols that is 4-methylphenol substituted by tert-butyl groups at positions 2 and 6. | 2.07 | 1 | 0 | phenols | antioxidant; ferroptosis inhibitor; food additive; geroprotector |
| 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. | 2.05 | 1 | 0 | C-nitro compound; imidazoles; monocarboxylic acid amide | antiprotozoal drug |
| halazepam halazepam: structure | 2.05 | 1 | 0 | organic molecular entity | |
| du-21220 Ritodrine: An adrenergic beta-2 agonist used to control PREMATURE LABOR.. 4-[2-[[1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenol : A secondary amino compound that is 4-(2-amino-1-hydroxypropyl)phenol in which one of the hydrogens attached to the nitrogen is replaced by a 2-(4-hydroxyphenyl)ethyl group. | 2.04 | 1 | 0 | benzyl alcohols; polyphenol; secondary alcohol; secondary amino compound | |
| 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. | 3.77 | 2 | 0 | 17-hydroxy steroid; 3-hydroxy steroid; androstanoid | |
| calcium oxalate Calcium Oxalate: The calcium salt of oxalic acid, occurring in the urine as crystals and in certain calculi.. calcium oxalate : The calcium salt of oxalic acid, which in excess in the urine may lead to formation of oxalate calculi (kidney stones). | 2.13 | 1 | 0 | organic calcium salt | |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 2.05 | 1 | 0 | chlorphenamine | |
| ribostamycin Ribostamycin: A broad-spectrum antimicrobial isolated from Streptomyces ribosifidicus.. ribostamycin : An amino cyclitol glycoside that is 4,6-diaminocyclohexane-1,2,3-triol having a 2,6-diamino-2,6-dideoxy-alpha-D-glucosyl residue attached at position 1 and a beta-D-ribosyl residue attached at position 2. It is an antibiotic produced by Streptomyces ribosidificus (formerly S. thermoflavus). | 2.04 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | antibacterial drug; antimicrobial agent; metabolite |
| 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. | 2.44 | 2 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| ripazepam [no description available] | 2.04 | 1 | 0 | benzenes | |
| 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. | 2.74 | 3 | 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. | 2.74 | 3 | 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. | 2.04 | 1 | 0 | tryptamines | |
| tramadol Tramadol: A narcotic analgesic proposed for severe pain. It may be habituating.. tramadol : A racemate consisting of equal amounts of (R,R)- and (S,S)-tramadol. A centrally acting synthetic opioid analgesic, used (as the hydrochloride salt) to treat moderately severe pain. The (R,R)-enantiomer exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. Originally developed by Gruenenthal GmbH and launched in 1977, it was subsequently isolated from the root bark of the South African tree Nauclea latifolia.. (R,R)-tramadol : A 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol in which both stereocentres have R-configuration; the (R,R)-enantiomer of the racemic opioid analgesic tramadol, it exhibits ten-fold higher analgesic potency than the (S,S)-enantiomer. | 2.06 | 1 | 0 | 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol | adrenergic uptake inhibitor; antitussive; capsaicin receptor antagonist; delta-opioid receptor agonist; kappa-opioid receptor agonist; metabolite; mu-opioid receptor agonist; muscarinic antagonist; nicotinic antagonist; NMDA receptor antagonist; opioid analgesic; serotonergic antagonist; serotonin uptake inhibitor |
| prednimustine Prednimustine: Ester of CHLORAMBUCIL and PREDNISOLONE used as a combination alkylating agent and synthetic steroid to treat various leukemias and other neoplasms. It causes gastrointestinal and bone marrow toxicity. | 2.04 | 1 | 0 | corticosteroid hormone | |
| toloxatone toloxatone: oxazolidinone derivative; psychotropic drug; structure. toloxatone : A racemate consisting of equimolar amounts of (R)- and (S)-toloxatone. It is a reversible monoamine oxidase A inhibitor and antidepressant.. 5-(hydroxymethyl)-3-(3-methylphenyl)-1,3-oxazolidin-2-one : A member of the class of oxazolidinones that is 5-(hydroxymethyl)-1,3-oxazolidin-2-one substituted by a 3-methylphenyl group at position 3. | 2.04 | 1 | 0 | oxazolidinone; primary alcohol; toluenes | |
| amygdalin [no description available] | 2.04 | 1 | 0 | cyanogenic glycoside; disaccharide derivative; gentiobioside | plant metabolite |
| vidarabine phosphate Vidarabine Phosphate: An adenosine monophosphate analog in which ribose is replaced by an arabinose moiety. It is the monophosphate ester of VIDARABINE with antiviral and possibly antineoplastic properties. | 3.12 | 1 | 0 | ||
| 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. | 2.45 | 2 | 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. | 2.74 | 3 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| pirprofen pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure | 2.07 | 1 | 0 | pyrroline | |
| sisomicin Sisomicin: Antibiotic produced by Micromonospora inyoensis. It is closely related to gentamicin C1A, one of the components of the gentamicin complex (GENTAMICINS). | 2.04 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic; beta-L-arabinoside; monosaccharide derivative | |
| amdinocillin Amdinocillin: An amidinopenicillanic acid derivative with broad spectrum antibacterial action.. mecillinam : A penicillin in which the 6beta substituent is [(azepan-1-yl)methylidene]amino; an extended-spectrum penicillin antibiotic that binds specifically to penicillin binding protein 2 (PBP2), and is only considered to be active against Gram-negative bacteria. | 2.04 | 1 | 0 | penicillin | antibacterial drug; antiinfective agent |
| 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. | 2.44 | 2 | 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). | 6.7 | 9 | 2 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 5.59 | 9 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| promegestone Promegestone: A synthetic progestin which is useful for the study of progestin distribution and progestin tissue receptors, as it is not bound by transcortin and binds to progesterone receptors with a higher association constant than progesterone.. promegestone : A progestin consisting of 17beta-propionylestra-4,9-dien-3-one substituted at position 17 by a methyl group. | 3.4 | 1 | 1 | 20-oxo steroid; 3-oxo-Delta(4) steroid | antineoplastic agent; progesterone receptor agonist; progestin |
| 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. | 2.04 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| ticarcillin Ticarcillin: An antibiotic derived from penicillin similar to CARBENICILLIN in action.. ticarcillin : A penicillin compound having a 6beta-[(2R)-2-carboxy-2-thiophen-3-ylacetyl]amino side-group. | 2.44 | 2 | 0 | penicillin allergen; penicillin | antibacterial drug |
| trimazosin trimazosin: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | N-arylpiperazine | |
| halofantrine halofantrine: used in treatment of mild to moderate acute malaria | 2.05 | 1 | 0 | phenanthrenes | |
| etidocaine Etidocaine: A local anesthetic with rapid onset and long action, similar to BUPIVACAINE.. etidocaine : An amino acid amide in which 2-[ethyl(propyl)amino]butanoic acid and 2,6-dimethylaniline have combined to form the amide bond. Used as a local anaesthetic (amide caine), it has rapid onset and long action properties, similar to bupivacaine, and is given by injection during surgical procedures and during labour and delivery. | 2.04 | 1 | 0 | amino acid amide | local anaesthetic |
| ribavirin Rebetron: Rebetron is tradename | 2.04 | 1 | 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 |
| adinazolam adinazolam: structure in first source. adinazolam : A triazolo[4,3-a][1,4]benzodiazepine having a dimethylaminomethyl group at the 1-position, a phenyl group at the 6-position and a chloro substituent at the 8-position. | 2.04 | 1 | 0 | triazolobenzodiazepine | anticonvulsant; antidepressant; anxiolytic drug; sedative |
| 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. | 2.04 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| tolamolol [no description available] | 2.04 | 1 | 0 | ||
| 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. | 2.44 | 2 | 0 | beta-lactam antibiotic allergen; cephalosporin | antibacterial drug |
| hydroxymaprotilin hydroxymaprotilin: RN given refers to cpd without isomeric designation | 2.05 | 1 | 0 | ||
| 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. | 2.07 | 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. | 2.97 | 4 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| tocainide Tocainide: An antiarrhythmic agent which exerts a potential- and frequency-dependent block of SODIUM CHANNELS.. tocainide : A monocarboxylic acid amide in which 2,6-dimethylphenylaniline and isobutyric acid have combined to form the amide bond; used as a local anaesthetic. | 2.74 | 3 | 0 | monocarboxylic acid amide | anti-arrhythmia drug; local anaesthetic; sodium channel blocker |
| sulbenicillin Sulbenicillin: Semisynthetic penicillin-type antibiotic.. sulbenicillin : A penicillin antibiotic having a 6beta-[phenyl(sulfo)acetamido] side-chain. | 2.04 | 1 | 0 | penicillin | |
| sq-11725 Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.. nadolol : Nadolol is a diastereoisomeric mixture consisting of equimolar amounts of the four possible 2,3-cis-isomers of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol. | 2.74 | 3 | 0 | ||
| 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. | 2.75 | 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 |
| nimustine Nimustine: Antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine. The drug has also been used in combination with other antineoplastic agents or with radiotherapy for the treatment of various neoplasms.. nimustine : An organochlorine compound that is urea in which the two hydrogens on one of the amino groups are replaced by nitroso and 2-chloroethyl groups and one hydrogen from the other amino group is replaced by a 4-amino-2-methylpyrimidin-5-ylmethyl] group. An antineoplastic agent especially effective against malignant brain tumors. | 2.04 | 1 | 0 | aminopyrimidine; N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic 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. | 2.04 | 1 | 0 | organic bromide salt; quaternary ammonium salt | muscle relaxant; neuromuscular agent; nicotinic antagonist |
| pinazepam pinazepam: structure | 2.05 | 1 | 0 | benzodiazepine | |
| desogestrel Desogestrel: A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED). | 7.07 | 7 | 4 | 17beta-hydroxy steroid; terminal acetylenic compound | contraceptive drug; progestin; synthetic oral contraceptive |
| meptazinol Meptazinol: A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain. | 2.04 | 1 | 0 | azepanes | |
| butibufen butibufen: RN given refers to parent cpd | 2.45 | 2 | 0 | monoterpenoid | |
| 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. | 2.04 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| 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. | 2.46 | 2 | 0 | aminopyridine; N-sulfonylurea; secondary amino compound | antihypertensive agent; loop diuretic |
| medroxalol medroxalol: RN given refers to parent cpd without isomeric designation | 2.04 | 1 | 0 | salicylamides | |
| 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. | 2.73 | 3 | 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 |
| spiromustine [no description available] | 2.04 | 1 | 0 | ||
| cefmetazole Cefmetazole: A semisynthetic cephamycin antibiotic with a broad spectrum of activity against both gram-positive and gram-negative microorganisms. It has a high rate of efficacy in many types of infection and to date no severe side effects have been noted.. cefmetazole : A second-generation cephalosporin antibiotic having N(1)-methyltetrazol-5-ylthiomethyl, {[(cyanomethyl)sulfanyl]acetyl}amino and methoxy side-groups at positions 3, 7beta and 7alpha respectively of the parent cephem bicyclic structure. | 2.04 | 1 | 0 | cephalosporin | antibacterial drug |
| diaziquone diaziquone: RN given refers to parent cpd. diaziquone : A 1,4-benzoquinone that is substituted at positions 2 and 5 have been replaced by aziridin-1-yl groups and at positions 3 and 6 by (ethoxycarbonyl)amino groups. | 2.04 | 1 | 0 | 1,4-benzoquinones; aziridines; carbamate ester; enamine | alkylating agent; antineoplastic agent |
| lorcainide [no description available] | 2.04 | 1 | 0 | acetamides | |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 2.44 | 2 | 0 | anthracycline antibiotic; deoxy hexoside; monosaccharide derivative | |
| ceforanide ceforanide: RN given refers to (6R-(trans))-isomer. ceforanide : A second-generation cephalosporin antibiotic with {[1-(carboxymethyl)-1H-tetrazol-5-yl]sulfanyl}methyl and 2-(aminomethyl)phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. It is effective against many coliforms, including Escherichia coli, Klebsiella, Enterobacter and Proteus, and most strains of Salmonella, Shigella, Hemophilus, Citrobacter and Arizona species. | 2.04 | 1 | 0 | cephalosporin | antibacterial drug |
| cefonicid Cefonicid: A second-generation cephalosporin administered intravenously or intramuscularly. Its bactericidal action results from inhibition of cell wall synthesis. It is used for urinary tract infections, lower respiratory tract infections, and soft tissue and bone infections.. cefonicid : A cephalosporin bearing {[1-(sulfomethyl)-1H-tetrazol-5-yl]sulfanyl}methyl and (R)-2-hydroxy-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.04 | 1 | 0 | cephalosporin | antibacterial drug |
| 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. | 2.44 | 2 | 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. | 2.75 | 3 | 0 | aromatic ether; benzodioxoles; organofluorine compound; piperidines | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| triciribine phosphate [no description available] | 2.04 | 1 | 0 | ||
| 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. | 2.97 | 4 | 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. | 2.46 | 2 | 0 | cephalosporin | antibacterial drug |
| staurosporine [no description available] | 2.05 | 1 | 0 | indolocarbazole alkaloid; organic heterooctacyclic compound | apoptosis inducer; bacterial metabolite; EC 2.7.11.13 (protein kinase C) inhibitor; geroprotector |
| 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. | 2.04 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| moxalactam Moxalactam: Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections.. moxalactam : A broad-spectrum oxacephem antibiotic in which the oxazine ring is substituted with a tetrazolylthiomethyl group and the azetidinone ring carries methoxy and 2-carboxy-2-(4-hydroxyphenyl)acetamido substituents. | 2.04 | 1 | 0 | cephalosporin; oxacephem | antibacterial drug |
| endralazine BQ 22-708: RN given refers to parent cpd | 2.04 | 1 | 0 | benzamides | |
| bw-755c 4,5-Dihydro-1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-3-amine: A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia. | 2.04 | 1 | 0 | ||
| colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland. | 1.98 | 1 | 0 | acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol | adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.04 | 1 | 0 | cephalosporin | antibacterial drug |
| encainide Encainide: One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.. encainide : 4-Methoxy-N-phenylbenzamide in which the hydrogen at the 2 position of the phenyl group is substituted by a 2-(1-methylpiperidin-2-yl)ethyl group. A class Ic antiarrhythmic, the hydrochloride was used for the treatment of severe or life-threatening ventricular arrhythmias, but it was associated with increased death rates in patients who had asymptomatic heart rhythm abnormalities after a recent heart attack and was withdrawn from the market. | 2.04 | 1 | 0 | benzamides; piperidines | anti-arrhythmia drug; sodium channel blocker |
| buserelin Buserelin: A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications. | 13.66 | 105 | 16 | oligopeptide | |
| 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. | 2.04 | 1 | 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. | 2.04 | 1 | 0 | fluoroquinolone antibiotic; monocarboxylic acid; N-alkylpiperazine; N-arylpiperazine; quinolone antibiotic; quinolone | antibacterial drug; antiinfective agent; DNA synthesis inhibitor |
| alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position. | 2.74 | 3 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| 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. | 2.04 | 1 | 0 | ||
| recainam recainam: structure given in first source | 2.04 | 1 | 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). | 2.46 | 2 | 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 | 2.04 | 1 | 0 | aminopyridine | |
| 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. | 2.04 | 1 | 0 | aromatic ketone | |
| piritrexim piritrexim: RN given refers to parent cpd; structure given in first source | 2.45 | 2 | 0 | ||
| 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. | 2.07 | 1 | 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. | 2.04 | 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. | 2.46 | 2 | 0 | dimethoxybenzene | |
| 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. | 2.46 | 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. | 5.05 | 4 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| caracemide [no description available] | 2.04 | 1 | 0 | ||
| bambuterol bambuterol: selective inhibitor of butyrylcholinesterase & acetylcholinesterase. bambuterol : A carbamate ester that is terbutaline in which both of the phenolic hydroxy groups have been protected as the corresponding N,N-dimethylcarbamates. A long acting beta-adrenoceptor agonist used in the treatment of asthma, it is a prodrug for terbutaline. | 2.74 | 3 | 0 | carbamate ester; phenylethanolamines | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; prodrug; sympathomimetic agent; tocolytic agent |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 2.04 | 1 | 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. | 2.04 | 1 | 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] | 2.07 | 1 | 0 | imidazoles | |
| raloxifene hydrochloride Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride. | 8.87 | 12 | 4 | hydrochloride | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 7.44 | 8 | 2 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| trospectomycin trospectomycin: active against Neisseria gonorrhoeae; RN refers to 2R-(2alpha,4abeta,5abeta,6beta,7beta,8beta,9beta,9alpha,9aalpha,10abeta)-(9CI)-isomer | 2.04 | 1 | 0 | dioxanes | |
| cilazapril, anhydrous Cilazapril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.. cilazapril : A pyridazinodiazepine resulting from the formal condensation of the carboxy group of cilazaprilat with ethanol. It is a drug used in the treatment of hypertension and heart failure. | 2.04 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; pyridazinodiazepine | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| 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. | 2.05 | 1 | 0 | naphthoic acid | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 8.8 | 19 | 3 | 3-oxo steroid; aza-steroid; delta-lactam | androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| sematilide sematilide: RN refers to HCl; structure given in first source | 2.04 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| clinafloxacin clinafloxacin: structure given in first source; RN given is for monoHCl | 2.04 | 1 | 0 | quinolines | |
| 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. | 2.04 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| loxiglumide loxiglumide: cholecystokinin receptor antagonist; RN refers to (+-)-isomer; structure in first source | 2.04 | 1 | 0 | organic molecular entity | |
| aromasil [no description available] | 4.6 | 4 | 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] | 2.04 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | |
| zileuton [no description available] | 2.07 | 1 | 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 |
| 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. | 2.04 | 1 | 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. | 2.04 | 1 | 0 | beta-amino acid; piperidinemonocarboxylic acid; tertiary amino compound; thiophenes | anticonvulsant; GABA reuptake inhibitor |
| mibefradil Mibefradil: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE. | 2.04 | 1 | 0 | tetralins | T-type calcium channel blocker |
| 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. | 2.04 | 1 | 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. | 2.46 | 2 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| 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. | 2.5 | 2 | 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 | 2.04 | 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. | 2.04 | 1 | 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. | 2.04 | 1 | 0 | alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester | intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative |
| atorvastatin [no description available] | 2.76 | 3 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 2.04 | 1 | 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 |
| irinotecan [no description available] | 3.54 | 2 | 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. | 2.46 | 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. | 2.45 | 2 | 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. | 2.04 | 1 | 0 | 1,2-benzisothiazole; indolones; organochlorine compound; piperazines | antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist |
| zanamivir Zanamivir: A guanido-neuraminic acid that is used to inhibit NEURAMINIDASE. | 2.04 | 1 | 0 | guanidines | antiviral agent; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor |
| 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. | 2.04 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| 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. | 2.04 | 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. | 3.54 | 2 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| 2,5-bis(1-aziridinyl)-3,6-bis(2-methoxyethoxy)-4-benzoquinone 2,5-bis(1-aziridinyl)-3,6-bis(2-methoxyethoxy)-4-benzoquinone: structure | 2.04 | 1 | 0 | 1,4-benzoquinones | |
| acridine orange Acridine Orange: A cationic cytochemical stain specific for cell nuclei, especially DNA. It is used as a supravital stain and in fluorescence cytochemistry. It may cause mutations in microorganisms.. acridine orange : Fluorescent dye useful for cell cycle determination. It is cell-permeable, and interacts with DNA and RNA by intercalation or electrostatic attractions respectively.. acridine orange free base : A member of the class of aminoacridines that is acridine carrying two dimethylamino substituents at positions 3 and 6. The hydrochloride salt is the fluorescent dye 'acridine orange', used for cell cycle determination. | 2.01 | 1 | 0 | aminoacridines; aromatic amine; tertiary amino compound | fluorochrome; histological dye |
| morzid morzid: structure | 2.04 | 1 | 0 | morpholines | |
| potassium phosphate potassium phosphate: used in dental materials and to treat hypophosphatemia; RN given refers to cpd with unspecified MF. tripotassium phosphate : An inorganic potassium salt that is the tripotassium salt of phosphoric acid. | 3.37 | 1 | 1 | inorganic phosphate salt; inorganic potassium salt | |
| cisatracurium cisatracurium: RN refers to (1R-(1alpha,2alpha(1'R*,2'R*)))-isomer. cisatracurium : A diester that is the (1R,1'R,2R,2'R)-diastereoisomer of atracurium, a quaternary ammonium ion consisting of pentane-1,5-diol with both hydroxy functions bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. The active species in the skeletal muscle relaxant cisatracurium besylate. | 2.04 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| fosinoprilat fosinoprilat: active phosphinic acid metabolite of prodrug fosenopril, which is activated by esterases in vivo; structure given in first source; binds zinc with phosphinic acid group. fosinoprilat : A phosphinic acid-containing N-acyl derivative of (4S)-cyclohexyl-L-proline. An inhibitor of angiotensin converting enzyme (ACE), it is used as the phosphinate ester pro-drug fosinopril for treatment of hypertension and chronic heart failure. | 2.04 | 1 | 0 | L-proline derivative; phosphinic acids | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ortho-cept ethinyl estradiol-desogestrel combination: Ethinyl Estradiol and Desogestrell given in fixed proportions; has proved to be an effective & well-tolerated oral contraceptive, which improves cycle control & has a beneficial effect on acne | 3.41 | 1 | 1 | ||
| 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. | 2.45 | 2 | 0 | ||
| cefprozil [no description available] | 2.04 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| febrifugine febrifugine: antimalarials; structure | 2.04 | 1 | 0 | quinazolines | |
| glucose, (beta-d)-isomer beta-D-glucose : D-Glucopyranose with beta configuration at the anomeric centre.. (1->4)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->4) linkages.. (1->3)-beta-D-glucan : A beta-D-glucan in which the glucose units are connected by (1->3) linkages. | 3.23 | 1 | 0 | D-glucopyranose | epitope; mouse metabolite |
| ursolic acid [no description available] | 2.05 | 1 | 0 | hydroxy monocarboxylic acid; pentacyclic triterpenoid | geroprotector; plant metabolite |
| propamidine propamidine: structure given in first source. propamidine : A polyether that is the bis(4-guanidinophenyl) ether of propane-1,3-diol. Used (as its isethionate salt) for the treatment of minor eye or eyelid infections, such as conjunctivitis and blepharitis. | 2.05 | 1 | 0 | aromatic ether; guanidines; polyether | antimicrobial agent; antiseptic drug |
| thiazolyl blue thiazolyl blue: RN & II refers to bromide. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide : The bromide salt of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium. | 2.03 | 1 | 0 | organic bromide salt | colorimetric reagent; dye |
| thymine arabinoside thymine arabinoside: selectively inhibits replication of herpes simplex virus | 2.04 | 1 | 0 | N-glycosyl compound | |
| fluorexon fluorexon: structure | 2.08 | 1 | 0 | xanthene dye | fluorochrome |
| psicofuranine [no description available] | 2.04 | 1 | 0 | psicose derivative; purine nucleoside | |
| triciribine [no description available] | 2.04 | 1 | 0 | nucleoside analogue | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| sinefungin [no description available] | 2.05 | 1 | 0 | adenosines; non-proteinogenic alpha-amino acid | antifungal agent; antimicrobial agent |
| iopamidol Iopamidol: A non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiological procedures.. iopamidol : A benzenedicarboxamide compound having N-substituted carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and a (2S)-2-hydroxypropanamido group at the 5-position. | 2.04 | 1 | 0 | benzenedicarboxamide; organoiodine compound; pentol | environmental contaminant; radioopaque medium; xenobiotic |
| 5-chloro-2'-deoxyuridine [no description available] | 2.04 | 1 | 0 | ||
| imipramine n-oxide imipramine N-oxide: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | dibenzooxazepine | |
| bendamustine [no description available] | 2.04 | 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. | 2.05 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| trofosfamide trofosfamide: cyclophosphamide analog; structure | 2.04 | 1 | 0 | ifosfamides | |
| 4-aminobenzoic acid-n-xyloside 4-aminobenzoic acid-N-xyloside: K 247 refers to Na salt; RN given refers to (D)-isomer | 2.04 | 1 | 0 | ||
| etofibrate etofibrate: analog of clofibrate with nicotinic acid substituted on the 2-carbon of the ethyl ester group; structure; RN given refers to parent cpd | 2.05 | 1 | 0 | monocarboxylic acid | |
| fotrin fotrin: ethyleneamine derivative; antineoplastic; Russian drug; structure | 2.04 | 1 | 0 | ||
| sufosfamide sufosfamide: stronger immunosuppressive activity than cyclophosphamide; structure | 2.04 | 1 | 0 | ||
| dexloxiglumide dexloxiglumide: a CCK receptor antagonist; structure given in first source | 2.04 | 1 | 0 | glutamic acid derivative | |
| intoplicine intoplicine: structure in first source | 2.04 | 1 | 0 | pyridoindole | |
| repaglinide [no description available] | 2.04 | 1 | 0 | piperidines | |
| turosteride turosteride: a 5alpha-reductase inhibitor; structure given in first source; RN given refers to the (5alpha,17beta)-isomer | 1.99 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| propatyl nitrate propatyl nitrate: structure given in first source | 2.04 | 1 | 0 | nitrate ester | |
| 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. | 2.74 | 3 | 0 | fenfluramine | appetite depressant; serotonergic agonist; serotonin uptake inhibitor |
| estradiol-3-sulfate estradiol-3-sulfate: RN given refers to (17beta)-isomer. 17beta-estradiol 3-sulfate : A steroid sulfate obtained by the formal condensation of sulfuric acid with the 3-hydroxy group of 17beta-estradiol. | 5.89 | 2 | 2 | 17beta-hydroxy steroid; steroid sulfate | mammalian metabolite |
| sulfamidochrysoidine sulfamidochrysoidine: RN given refers to parent cpd; structure. prontosil : A diphenyldiazene compound having two amino substituents at the 2- and 4-positions and an aminosulphonyl substituent at the 4'-position. It was the first antibacterial drug, (introduced 1935) and the first of the sulfonamide antibiotics. | 2.04 | 1 | 0 | ||
| synthalin a synthalin A: RN given refers to parent cpd; structure. synthalin : A hydrochloride resulting from the reaction of decamethylenediguanidine with 2 mol eq. of hydrogen chloride.. synthalin A : A member of the class of guanidines that is decane having guanidino groups at the 1- and 10-positions. | 2.05 | 1 | 0 | guanidines | hepatotoxic agent; hypoglycemic agent; nephrotoxin |
| ethinyl estradiol-17-sulfate ethinyl estradiol-17-sulfate: RN given refers to the (17alpha)-isomer | 2.04 | 1 | 0 | ||
| 1,7-phenanthroline [no description available] | 2.02 | 1 | 0 | phenanthroline | |
| 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. | 9.98 | 19 | 8 | 1,2,3-triazole | |
| ibopamine ibopamine: structure given in UD 31;67a & in 2nd source | 2.45 | 2 | 0 | benzoate ester; phenols | |
| ethinylestradiol-3-sulfate ethinylestradiol-3-sulfate: binds to albumin at 2 sites | 2.04 | 1 | 0 | 17beta-hydroxy steroid; steroid sulfate | antineoplastic agent; estrogen |
| 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. | 5.41 | 4 | 1 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| cefcanel cefcanel: RN given refers to (6R-(6 alpha,7 beta(R*)))-isomer; structure | 2.04 | 1 | 0 | ||
| pumitepa pumitepa: structure; RN given refers to unlabeled cpd | 2.04 | 1 | 0 | ||
| 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. | 8.81 | 10 | 4 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| epristeride epristeride: structure given in first source | 2.04 | 1 | 0 | steroid acid | |
| talinolol [no description available] | 2.04 | 1 | 0 | ureas | |
| pirlindole pirlindole: RN given refers to parent cpd; synonym pyrazidol refers to mono-HCl; structure in Negwer, 5th ed, #2812 | 2.05 | 1 | 0 | carbazoles | |
| elmustine elmustine: structure | 2.04 | 1 | 0 | ||
| dienogest [no description available] | 9.9 | 12 | 4 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; aliphatic nitrile; steroid hormone | progesterone receptor agonist; progestin; synthetic oral contraceptive |
| forphenicinol [no description available] | 2.04 | 1 | 0 | ||
| 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. | 2.05 | 1 | 0 | artemisinin derivative; cyclic acetal; organic peroxide; semisynthetic derivative; sesquiterpenoid | antimalarial |
| dipropylacetamide dipropylacetamide: structure. valpromide : A fatty amide derived from valproic acid. | 2.04 | 1 | 0 | fatty amide | geroprotector; metabolite; teratogenic agent |
| denaverine denaverine: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | diarylmethane | |
| 6-amino-1-hydroxyhexane-1,1-diphosphonate 6-amino-1-hydroxyhexane-1,1-diphosphonate: used for therapy of Paget's disease of bone & malignant hypercalcaemia | 2.05 | 1 | 0 | 1,1-bis(phosphonic acid) | |
| diprafenone diprafenone: structure given in first source | 2.04 | 1 | 0 | aromatic compound | |
| 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. | 2.04 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 2.46 | 2 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| ljc 10627 biapenem: structure given in first source. biapenem : A carbapenem antibiotic in which the azetidine and pyrroline rings carry 1-hydroxymethyl and pyrazolo[1,2-a][1,2,4]triazolium-6-ylthio substituents respectively. | 2.04 | 1 | 0 | carbapenems; organic sulfide; pyrazolotriazole | antibacterial drug |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 2.04 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| 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. | 2.04 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| inproquone inproquone: major descriptor (78-80); replaced major descriptor Bayer E39 (63-77); on-line search AZIRINES (66-80); Index Medicus search Bayer E39 (63-77), INPROQUONE (78-80) | 2.04 | 1 | 0 | ||
| betamipron [no description available] | 2.04 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| rexigen clobenzorex: RN given refers to (+)-isomer; structure | 2.05 | 1 | 0 | ||
| bufuralol bufuralol: RN given refers to cpd without isomeric designation; structure | 2.04 | 1 | 0 | benzofurans | |
| aceclofenac [no description available] | 2.05 | 1 | 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 |
| clociguanil clociguanil: RN given refers to parent cpd; structure | 2.05 | 1 | 0 | ||
| tebuquine [no description available] | 2.05 | 1 | 0 | ||
| panipenem panipenem: synthetic cpd; structure given in first source | 2.04 | 1 | 0 | organic molecular entity | |
| perindoprilat perindoprilat : A dipeptide obtained by formal condensation of one of the carboxy groups of N-[(1S)-1-carboxyethyl]-L-norvaline with the amino group of (2S,3aS,7aS)-octahydroindole-2-carboxylic acid. The major active metabolite of perindopril. | 2.04 | 1 | 0 | dicarboxylic acid; dipeptide; L-alanine derivative; organic heterobicyclic compound | antihypertensive agent; drug metabolite; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ubenimex ubenimex: growth inhibitor | 2.11 | 1 | 0 | ||
| 7-hydroxystaurosporine [no description available] | 2.04 | 1 | 0 | ||
| methotrimeprazine Methotrimeprazine: A phenothiazine with pharmacological activity similar to that of both CHLORPROMAZINE and PROMETHAZINE. It has the histamine-antagonist properties of the antihistamines together with CENTRAL NERVOUS SYSTEM effects resembling those of chlorpromazine. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604). methotrimeprazine : A member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively. | 2.04 | 1 | 0 | phenothiazines; tertiary amine | anticoronaviral agent; cholinergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; non-narcotic analgesic; phenothiazine antipsychotic drug; serotonergic antagonist |
| 9-aminocamptothecin [no description available] | 2.04 | 1 | 0 | pyranoindolizinoquinoline | |
| sch 34343 Sch 34343: structure given in first source; RN given refers to (5R-(5alpha,6alpha))-isomer | 2.04 | 1 | 0 | ||
| squalamine squalamine: from dogfish shark Squalus acanthias; structure given in first source | 3.53 | 2 | 0 | bile acid | |
| neplanocin a neplanocin A: neplanocins are antitumor antibiotics & carbocyclic analogs of purine nucleosides from Ampullarilla regularis A11079; see also neplanocin B, neplanocin C, neplanocin D & neplanocin F; structure in first source; a potent inhibitor of S-adenosylhomocysteine hydrolase | 2.04 | 1 | 0 | ||
| 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. | 2.45 | 2 | 0 | hydroxy-1,2-naphthoquinone | |
| 1-ethoxysilatrane [no description available] | 2.04 | 1 | 0 | ||
| rivastigmine [no description available] | 2.04 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 2.04 | 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. | 2.04 | 1 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 2.46 | 2 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| cryptolepine cryptolepine: fused indole-quinoline; structure in first source; from CRYPTOLEPIS sanguinolenta. cryptolepine : An organic heterotetracyclic compound that is 5H-indolo[3,2-b]quinoline in which the hydrogen at position N-5 is replaced by a methyl group. | 2.05 | 1 | 0 | indole alkaloid; organic heterotetracyclic compound; organonitrogen heterocyclic compound | anti-inflammatory agent; antimalarial; antineoplastic agent; cysteine protease inhibitor; plant metabolite |
| flunisolide flunisolide: flunisolide HFA is a formulation of flunisolide using hydrofluoroalkane (HFA) as propellant in place of chlorofluorocarbon (CFC) ones | 2.07 | 1 | 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 |
| 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. | 2.46 | 2 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| tretazicar tretazicar: minor descriptor (75-84); on-line & Index Medicus search AZIRIDINES (75-84) | 3.53 | 2 | 0 | ||
| 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. | 2.04 | 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 |
| nsc-172755 butocin: S-substituted analog of mercaptopurine which functions as a cytostatic agent; minor descriptor (75-85); on-line search 6-MERCAPTOPURINE/AA (75-84); Index Medicus search MERCAPTOPURINE/analogs (75-84) | 2.04 | 1 | 0 | ||
| cinchonine [no description available] | 2.05 | 1 | 0 | (8xi)-cinchonan-9-ol; cinchona alkaloid | metabolite |
| fibrinogen Fibrinogen: Plasma glycoprotein clotted by thrombin, composed of a dimer of three non-identical pairs of polypeptide chains (alpha, beta, gamma) held together by disulfide bonds. Fibrinogen clotting is a sol-gel change involving complex molecular arrangements: whereas fibrinogen is cleaved by thrombin to form polypeptides A and B, the proteolytic action of other enzymes yields different fibrinogen degradation products.. D-iditol : The D-enantiomer of iditol. | 10.54 | 3 | 2 | iditol | fungal metabolite |
| 17-alpha-hydroxypregnenolone 17-alpha-Hydroxypregnenolone: A 21-carbon steroid that is converted from PREGNENOLONE by STEROID 17-ALPHA-HYDROXYLASE. It is an intermediate in the delta-5 pathway of biosynthesis of GONADAL STEROID HORMONES and the adrenal CORTICOSTEROIDS.. 17alpha-hydroxypregnenolone : A hydroxypregnenolone carrying an alpha-hydroxy group at position 17. | 2.39 | 2 | 0 | 17alpha-hydroxy-C21-steroid; 17alpha-hydroxy steroid; 3beta-hydroxy-Delta(5)-steroid; hydroxypregnenolone; tertiary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| streptovitacin a streptovitacin A: structure | 2.04 | 1 | 0 | ||
| homocysteine Homocysteine: A thiol-containing amino acid formed by a demethylation of METHIONINE.. homocysteine : A sulfur-containing amino acid consisting of a glycine core with a 2-mercaptoethyl side-chain.. L-homocysteine : A homocysteine that has L configuration. | 4.38 | 2 | 2 | amino acid zwitterion; homocysteine; serine family amino acid | fundamental metabolite; mouse metabolite |
| n-hexadecyl-n,n-dimethyl-3-ammonio-1-propanesulfonate [no description available] | 2.05 | 1 | 0 | ||
| cb 10375 trimelamol: structure given in first source | 2.04 | 1 | 0 | ||
| mci 9038 [no description available] | 2.04 | 1 | 0 | peptide | |
| carbenicillin indanyl carbenicillin indanyl: acid stable indanyl ester of carbenicillin for oral use; same side-effects as carbenicillin; minor descriptor (75-86); on line & INDEX MEDICUS search CARBENICILLIN/AA (75-86); RN given refers to (mono-Na salt(2S-(2alpha,5alpha,6beta))-isomer) | 2.04 | 1 | 0 | penicillin | |
| glucuronic acid Glucuronic Acid: A sugar acid formed by the oxidation of the C-6 carbon of GLUCOSE. In addition to being a key intermediate metabolite of the uronic acid pathway, glucuronic acid also plays a role in the detoxification of certain drugs and toxins by conjugating with them to form GLUCURONIDES.. D-glucuronic acid : The D-enantiomer of glucuronic acid.. D-glucopyranuronic acid : A D-glucuronic acid in cyclic pyranose form. | 2.02 | 1 | 0 | D-glucuronic acid | algal metabolite |
| cb 1837 CB 1837: RN given refers to parent cpd; structure | 2.04 | 1 | 0 | ||
| desethylchloroquine desethylchloroquine: metabolite of chloroquine | 2.05 | 1 | 0 | aminoquinoline | |
| hexaphosphamide hexaphosphamide: structure | 2.04 | 1 | 0 | ||
| dipin dipin: structure | 2.04 | 1 | 0 | ||
| phosphazine phosphazine: structure | 2.04 | 1 | 0 | ||
| diiodobenzotepa diiodobenzotepa: structure | 2.04 | 1 | 0 | ||
| phorbolol myristate acetate [no description available] | 2.15 | 1 | 0 | ||
| icig 1163 ICIG 1163: RN given refers to parent cpd; structure in first source | 2.04 | 1 | 0 | ||
| wr 159412 [no description available] | 2.05 | 1 | 0 | ||
| bimolane bimolane: structure given in first source | 2.04 | 1 | 0 | ||
| thiodipin thiodipin: structure | 2.04 | 1 | 0 | ||
| fluoxydine fluoxydine: structure | 2.04 | 1 | 0 | ||
| cinchonidine cinchonidine: has antimalarial activity; diastereoisomer of cinchonine with distinct physiochemical properties; RN given refers to parent cpd(8alpha,9R)-isomer. cinchonidine : 8-epi-Cinchonan in which a hydrogen at position 9 is substituted by hydroxy (R configuration). A diasteroisomer of cinchonine, it occurs in the bark of most varieties of Cinchona shrubs, and is frequently used for directing chirality in asymmetric synthesis. | 2.05 | 1 | 0 | (8xi)-cinchonan-9-ol; cinchona alkaloid | metabolite |
| imiphos imiphos: structure | 2.04 | 1 | 0 | ||
| benzyloxyamine benzyloxyamine: RN given refers to parent cpd | 2.05 | 1 | 0 | ||
| cobalt Cobalt: A trace element that is a component of vitamin B12. It has the atomic symbol Co, atomic number 27, and atomic weight 58.93. It is used in nuclear weapons, alloys, and pigments. Deficiency in animals leads to anemia; its excess in humans can lead to erythrocytosis.. cobalt(1+) : A monovalent inorganic cation obtained from cobalt.. cobalt atom : A cobalt group element atom that has atomic number 27. | 2.01 | 1 | 0 | cobalt group element atom; metal allergen | micronutrient |
| 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. | 3.56 | 2 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| vitamin b 6 Vitamin B 6: VITAMIN B 6 refers to several PICOLINES (especially PYRIDOXINE; PYRIDOXAL; & PYRIDOXAMINE) that are efficiently converted by the body to PYRIDOXAL PHOSPHATE which is a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, and aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into PYRIDOXAMINE phosphate. Although pyridoxine and Vitamin B 6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading (EE Snell; Ann NY Acad Sci, vol 585 pg 1, 1990). Most of vitamin B6 is eventually degraded to PYRIDOXIC ACID and excreted in the urine. | 3.13 | 1 | 0 | ||
| imipenem, anhydrous Imipenem: Semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to beta-lactamases. Clinical studies have demonstrated high efficacy in the treatment of infections of various body systems. Its effectiveness is enhanced when it is administered in combination with CILASTATIN, a renal dipeptidase inhibitor.. imipenem : A broad-spectrum, intravenous beta-lactam antibiotic of the carbapenem subgroup. | 2.04 | 1 | 0 | beta-lactam antibiotic allergen; carbapenems; zwitterion | antibacterial drug |
| cremophor el cremophor EL: solvent for Althesin & Propanidid implicated as possible cause of similar adverse effects polyethoxylated castor oil; RN given refers to cpd with unknown MF; see also records for cremophor & cremophor A | 2.1 | 1 | 0 | ||
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 2.04 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| pyridinoline pyridinoline: 3-hydroxypyridinium derivative collagen crosslink; structure | 4.64 | 3 | 2 | organonitrogen compound; organooxygen compound | |
| deoxypyridinoline deoxypyridinoline: structure given in first source | 6.15 | 5 | 2 | ||
| cyproterone acetate, ethinyl estradiol drug combination [no description available] | 3.39 | 1 | 1 | ||
| aldophosphamide aldophosphamide: metabolite of cyclophosphamide | 2.04 | 1 | 0 | nitrogen mustard | |
| pyronaridine [no description available] | 2.05 | 1 | 0 | aminoquinoline | |
| 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 | 2.04 | 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 |
| asulacrine asulacrine: derivative of amsacrine; structure given in first source | 2.04 | 1 | 0 | acridines | |
| hydroxycotinine hydroxycotinine: metabolite of nicotine; RN given refers to (S)-isomer; structure. trans-3-hydroxycotinine : An N-alkylpyrrolidine that is cotinine substituted at position C-3 by a hydroxy group (the 3R,5S-diastereomer). | 2.04 | 1 | 0 | N-alkylpyrrolidine; pyridines; pyrrolidin-2-ones; pyrrolidine alkaloid | |
| quinaprilat quinaprilat: metabolite of quinapril. quinaprilat : A dicarboxylic acid resulting from the hydrolysis of the ethyl ester group of quinapril to give the corresponding dicarboxylic acid. The active angiotensin-converting enzyme inhibitor (ACE inhibitor) of the prodrug quinapril. | 2.04 | 1 | 0 | dicarboxylic acid; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; vasodilator agent |
| 2-hydroxyimipramine 2-hydroxyimipramine: RN given refers to parent cpd | 2.04 | 1 | 0 | dibenzoazepine | |
| 11-hydroxyandrostenedione 11-hydroxyandrostenedione: RN given refers to cpd without isomeric designation | 1.98 | 1 | 0 | 3-hydroxy steroid | androgen |
| ecteinascidin 743 [no description available] | 2.04 | 1 | 0 | acetate ester; azaspiro compound; bridged compound; hemiaminal; isoquinoline alkaloid; lactone; organic heteropolycyclic compound; organic sulfide; oxaspiro compound; polyphenol; tertiary amino compound | alkylating agent; angiogenesis modulating agent; anti-inflammatory agent; antineoplastic agent; marine metabolite |
| 3,6-bis(5-chloro-2-piperidyl)-2,5-piperazinedione 3,6-bis(5-chloro-2-piperidyl)-2,5-piperazinedione: isolated from Streptomyces griseoluteus fermentation broth; RN given refers to cpd without isomeric designation; structure | 2.04 | 1 | 0 | ||
| valerates Valerates: Derivatives of valeric acid, including its salts and esters. | 1.99 | 1 | 0 | short-chain fatty acid anion; straight-chain saturated fatty acid anion | plant metabolite |
| androsterone glucuronide androsterone glucuronide: RN given refers to (3alpha,5alpha)-isomer. androsterone 3-glucosiduronic acid : A steroid glucosiduronic acid having androsterone as the steroid component. | 1.97 | 1 | 0 | beta-D-glucosiduronic acid; steroid glucosiduronic acid | human metabolite; metabolite; mouse metabolite |
| oxymatrine oxysophoridine: an alkaloid isolated from Sophra alope; structure in first source | 2.04 | 1 | 0 | alkaloid; tertiary amine oxide | |
| tafenoquine tafenoquine : A racemate comprising equimolar amounts of (R)- and (S)-tafenoquine.. N(4)-{2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl}pentane-1,4-diamine : An aminoquinoline that is 8-aminoquinoline which is substituted by methoxy groups at positions 2 and 6, a methyl group at position 4, and a m-(trifluoromethyl)phenoxy group at position 5, and in which the amino substituent at position 8 is itself substituted by a 5-aminopentan-2-yl group. | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; aminoquinoline; aromatic ether; primary amino compound; secondary amino compound | |
| caprylates Caprylates: Derivatives of caprylic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain a carboxy terminated eight carbon aliphatic structure.. octanoate : A straight-chain saturated fatty acid anion that is the conjugate base of octanoic acid (caprylic acid); believed to block adipogenesis. | 2.1 | 1 | 0 | fatty acid anion 8:0; straight-chain saturated fatty acid anion | human metabolite; Saccharomyces cerevisiae metabolite |
| 1,1,2-trichloroethanol 1,1,2-trichloroethanol: metabolite of 1,1,2-trichloroethylene | 2.04 | 1 | 0 | ||
| desethylamodiaquine desethylamodiaquine: metabolite of amodiaquine | 2.05 | 1 | 0 | ||
| rc 3095 bombesin (6-14), Tpi(6)-Leu(13)-psi(CH2NH)-Leu(14)-: an antagonist of bombesin | 3.17 | 1 | 0 | ||
| n,n-dideethylchloroquine [no description available] | 2.05 | 1 | 0 | ||
| imatinib mesylate imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours. | 4.45 | 2 | 0 | methanesulfonate salt | anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| almotriptan almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. | 2.04 | 1 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| mk 0663 [no description available] | 2.04 | 1 | 0 | bipyridines; organochlorine compound; sulfone | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| gefitinib [no description available] | 3.53 | 2 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| iremycin iremycin: anthracycline antibiotic from Streptomyces violaceus subsp. iremyceticus; RN given refers to parent cpd(7R-trans)-isomer | 2.04 | 1 | 0 | ||
| lestaurtinib [no description available] | 2 | 1 | 0 | indolocarbazole | |
| methotrexate [no description available] | 5.46 | 8 | 2 | 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 |
| 3,6-diamino-9-(4-(methylsulfonyl)aminophenyl)aminoacridine [no description available] | 2.05 | 1 | 0 | ||
| n,n'-bis((2-chloroethyl)nitrosocarbamoyl)cystamine N,N'-bis((2-chloroethyl)nitrosocarbamoyl)cystamine: structure given in first source | 2.04 | 1 | 0 | ||
| hainanensine hainanensine: structure in first source | 2.04 | 1 | 0 | ||
| ne 58051 NE 58051: inhibits tumor cell adhesion to extracellular matrices; structure in first source | 2.05 | 1 | 0 | ||
| tamsulosin [no description available] | 4.31 | 3 | 0 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| sulbactam [no description available] | 2.04 | 1 | 0 | penicillanic acids | |
| ulipristal acetate RTI 3021-012: progesterone receptor antagonist. ulipristal acetate : A 20-oxo steroid obtained by acetylation of the 17-hydroxy group of (11beta,17alpha)-17-acetyl-11-[4-(dimethylamino)phenyl]-3-oxoestra-4,9-dien-17-ol (ulipristal). A selective progesterone receptor modulator, which is employed as an emergency contraceptive. | 9.19 | 10 | 4 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester; tertiary amino compound | contraceptive drug; progesterone receptor modulator; progestin |
| ym 529 YM 529: inhibits osteoclastic bone resorption; structure given in first source | 2.13 | 1 | 0 | ||
| abiraterone [no description available] | 8.87 | 9 | 3 | 3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor |
| wr 242511 WR 242511: RN given refers to parent cpd | 2.05 | 1 | 0 | ||
| dilevalol (R,R)-labetalol : A 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide that has 1R,2R-configuration. | 2.04 | 1 | 0 | 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide | |
| aspartame [no description available] | 2 | 1 | 0 | carboxylic acid; dipeptide zwitterion; dipeptide; methyl ester | apoptosis inhibitor; EC 3.1.3.1 (alkaline phosphatase) inhibitor; environmental contaminant; micronutrient; nutraceutical; sweetening agent; xenobiotic |
| ritrosulfan ritrosulfan: RN given refers to parent cpd(R*,S*)-isomer; structure | 2.04 | 1 | 0 | ||
| drospirenone and ethinyl estradiol combination drospirenone and ethinyl estradiol combination: female oral combined contraceptive containing 30 mcg (0.030 mg) Ethinyl Estradiol and 3 mg drospirenone (Androstenes) | 2.1 | 1 | 0 | ||
| docetaxel [no description available] | 2.04 | 1 | 0 | hydrate; secondary alpha-hydroxy ketone | antineoplastic agent |
| 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. | 8.87 | 14 | 5 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| irofulven irofulven: structure in first source | 2.04 | 1 | 0 | cyclohexenones | |
| ym 872 YM 872: structure in first source | 2.04 | 1 | 0 | ||
| 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. | 2.46 | 2 | 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 |
| 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. | 2.04 | 1 | 0 | carbapenemcarboxylic acid; pyrrolidinecarboxamide | antibacterial drug |
| dx 8951 [no description available] | 2.04 | 1 | 0 | pyranoindolizinoquinoline | |
| cilomilast [no description available] | 2.04 | 1 | 0 | methoxybenzenes | |
| 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). | 2.04 | 1 | 0 | benzazepine | aquaretic; vasopressin receptor antagonist |
| tezosentan tezosentan: structure in first source | 2.04 | 1 | 0 | ||
| sabarubicin sabarubicin: structure given in first source | 2.04 | 1 | 0 | ||
| damvar damvar: structure | 2.04 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 2.04 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 2.04 | 1 | 0 | isoquinolines | |
| hyoscyamine Hyoscyamine: The 3(S)-endo isomer of atropine.. (S)-atropine : An atropine with a 2S-configuration. | 2.07 | 1 | 0 | tropane alkaloid | |
| xamoterol Xamoterol: A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist. | 2.04 | 1 | 0 | morpholines | |
| 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. | 2.8 | 3 | 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 |
| olmesartan olmesartan: an active metabolite of CS 866 | 2.07 | 1 | 0 | biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent |
| androsterone sulfate androsterone sulfate: RN given refers to (3alpha,5alpha)-isomer. androsterone sulfate : A steroid sulfate that is the 3-sulfate of androsterone. | 1.98 | 1 | 0 | 17-oxo steroid; androstanoid; steroid sulfate | human metabolite; mouse metabolite |
| cyc 202 seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors. | 2.05 | 1 | 0 | 2,6-diaminopurines | antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| benzo-tepa benzo-tepa: structure | 2.04 | 1 | 0 | ||
| tevenel tevenel: sulfamoyl analog of D-threo-chloramphenicol; structure | 2.04 | 1 | 0 | sulfonamide | |
| tac 278 TAC 278: prodrug of 5-fluorouracil; RN given refers to cpd with unspecified isomeric designation | 2.04 | 1 | 0 | ||
| abanoquil [no description available] | 2.04 | 1 | 0 | ||
| tanshinone ii a tashinone IIA: a cardiovascular agent with antineoplastic activity; isolated from Salvia miltiorrhiza; structure in first source | 2.1 | 1 | 0 | abietane diterpenoid | |
| 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. | 2.04 | 1 | 0 | antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative | |
| aminopterin Aminopterin: A folic acid derivative used as a rodenticide that has been shown to be teratogenic. | 2.04 | 1 | 0 | dicarboxylic acid | EC 1.5.1.3 (dihydrofolate reductase) inhibitor; mutagen |
| 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. | 3.49 | 2 | 0 | corticosteroid hormone | |
| (4r)-3-((2s)-3-mercapto-2-methylpropanoyl)-4- thiazolidinecarboxylic acid [no description available] | 2.04 | 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. | 2.74 | 3 | 0 | ||
| ropivacaine Ropivacaine: An anilide used as a long-acting local anesthetic. It has a differential blocking effect on sensory and motor neurons.. ropivacaine : The piperidinecarboxamide obtained by the formal condensation of N-propylpipecolic acid and 2,6-dimethylaniline.. (S)-ropivacaine : A piperidinecarboxamide-based amide-type local anaesthetic (amide caine) in which (S)-N-propylpipecolic acid and 2,6-dimethylaniline are combined to form the amide bond. | 2.04 | 1 | 0 | piperidinecarboxamide; ropivacaine | local anaesthetic |
| melagatran [no description available] | 2.04 | 1 | 0 | azetidines; carboxamidine; dicarboxylic acid monoamide; non-proteinogenic alpha-amino acid; secondary amino compound | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor; serine protease inhibitor |
| fertirelin fertirelin: analog of luteinizing hormone releasing factor; more potent than LHFSHRH; RN given is for releasing factor from pig; RN given refers to parent cpd | 2.38 | 2 | 0 | oligopeptide | |
| lhrh(5-10), ac- [no description available] | 1.96 | 1 | 0 | ||
| deflazacort deflazacort: structure | 2.45 | 2 | 0 | corticosteroid hormone | |
| hexestrol diphosphate [no description available] | 2.04 | 1 | 0 | ||
| carbocysteine Carbocysteine: A compound formed when iodoacetic acid reacts with sulfhydryl groups in proteins. It has been used as an anti-infective nasal spray with mucolytic and expectorant action.. S-carboxymethyl-L-cysteine : An L-cysteine thioether that is L-cysteine in which the hydrogen of the thiol group has been replaced by a carboxymethyl group. | 2.04 | 1 | 0 | L-cysteine thioether; non-proteinogenic L-alpha-amino acid | mucolytic |
| olpadronic acid [no description available] | 2.05 | 1 | 0 | ||
| troleandomycin Troleandomycin: A macrolide antibiotic that is similar to ERYTHROMYCIN.. troleandomycin : A semi-synthetic macrolide antibiotic obtained by acetylation of the three free hydroxy groups of oleandomycin. Troleandomycin is only found in individuals that have taken the drug. | 2.07 | 1 | 0 | acetate ester; epoxide; macrolide antibiotic; monosaccharide derivative; polyketide; semisynthetic derivative | EC 1.14.13.97 (taurochenodeoxycholate 6alpha-hydroxylase) inhibitor; xenobiotic |
| 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. | 2.11 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| tesaglitazar tesaglitazar: structure in first source | 2.04 | 1 | 0 | ||
| bms204352 BMS204352: a calcium-sensitive opener of maxi-K potassium channels; structure in first source | 2.04 | 1 | 0 | ||
| fosfluconazole fosfluconazole: prodrug of fluconazole | 2.04 | 1 | 0 | conazole antifungal drug; triazole antifungal drug; triazoles | prodrug |
| dabigatran Dabigatran: A THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.. dabigatran : An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism. | 2.07 | 1 | 0 | aromatic amide; benzimidazoles; beta-alanine derivative; carboxamidine; pyridines | anticoagulant; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; EC 3.4.21.5 (thrombin) inhibitor |
| cp 101,606 traxoprodil mesylate: a selective NMDA antagonist; structure given in first source | 2.04 | 1 | 0 | ||
| demecolcine Demecolcine: An alkaloid isolated from Colchicum autumnale L. and used as an antineoplastic.. (-)-demecolcine : A secondary amino compound that is (S)-colchicine in which the N-acetyl group is replaced by an N-methyl group. Isolable from the autumn crocus, Colchicum autumnale, it is less toxic than colchicine and is used as an antineoplastic. | 2.04 | 1 | 0 | alkaloid; secondary amino compound | antineoplastic agent; microtubule-destabilising agent |
| cholic acid Cholic Acid: A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion.. cholic acid : A bile acid that is 5beta-cholan-24-oic acid bearing three alpha-hydroxy substituents at position 3, 7 and 12. | 2.03 | 1 | 0 | 12alpha-hydroxy steroid; 3alpha-hydroxy steroid; 7alpha-hydroxy steroid; bile acid; C24-steroid; trihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| equilin Equilin: An estrogenic steroid produced by HORSES. It has a total of four double bonds in the A- and B-ring. High concentration of euilin is found in the URINE of pregnant mares. | 3.38 | 1 | 1 | 17-oxo steroid; 3-hydroxy steroid | |
| norethindrone enanthate norethindrone enanthate: structure in Negwer, 5th ed, #5612 | 2.05 | 1 | 0 | steroid ester | |
| benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring. | 2.1 | 1 | 0 | ||
| nsc-89199 estramustine phosphate : A steroid phosphate which is the 17-O-phospho derivative of estramustine. | 2.44 | 2 | 0 | carbamate ester; organochlorine compound; steroid phosphate | |
| 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. | 7.35 | 13 | 3 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| lupeol [no description available] | 2.05 | 1 | 0 | pentacyclic triterpenoid; secondary alcohol | anti-inflammatory drug; plant metabolite |
| phenethicillin phenethicillin: minor descriptor (85); major descriptor (63-84); on-line search PENICILLIN, PHENOXYMETHYL/AA (66-85); Index Medicus search PHENETHICILLIN (63-84); RN given refers to (2S-(2alpha,5alpha,6beta))-isomer. phenethicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-phenoxypropanamido group. | 2.44 | 2 | 0 | penicillin allergen; penicillin | |
| indicine-n-oxide indicine-N-oxide: RN given refers to (1R-(1alpha,7(2R*,3S*),7abeta))-isomer; structure | 2.04 | 1 | 0 | ||
| acivicin [no description available] | 2.04 | 1 | 0 | isoxazoles; non-proteinogenic L-alpha-amino acid; organochlorine compound | antileishmanial agent; antimetabolite; antimicrobial agent; antineoplastic agent; EC 2.3.2.2 (gamma-glutamyltransferase) inhibitor; glutamine antagonist; metabolite |
| menthofuran menthofuran: RN given refers to cpd without isomeric designation; derives from cyclization of pulegone. menthofuran : A monoterpenoid that is 4,5,6,7-tetrahydro-1-benzofuran substituted by methyl groups at positions 3 and 6. | 2.07 | 1 | 0 | 1-benzofurans; monoterpenoid | nematicide; plant metabolite |
| trimethoprim, sulfamethoxazole drug combination Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole. | 2.04 | 1 | 0 | ||
| o-(chloroacetylcarbamoyl)fumagillol O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis.. O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative. | 3.08 | 1 | 0 | carbamate ester; organochlorine compound; semisynthetic derivative; sesquiterpenoid; spiro-epoxide | angiogenesis inhibitor; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; methionine aminopeptidase 2 inhibitor; retinoic acid receptor alpha antagonist |
| bortezomib [no description available] | 3.53 | 2 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| neocryptolepine neocryptolepine: isolated from the roots of the African plant Cryptolepis sanguinolenta; structure in first source | 2.05 | 1 | 0 | ||
| 1-hydroxypentane-1,1-bisphosphonate [no description available] | 2.05 | 1 | 0 | ||
| cimadronate cimadronate: increases serum 1,25-dihydroxyvitamin D in rats via stimulating renal 1-hydroxylase activity; structure given in first source | 2.42 | 2 | 0 | ||
| 1,1-hydroxyoctanodiphosphonate [no description available] | 2.05 | 1 | 0 | ||
| carboplatin [no description available] | 4.35 | 4 | 1 | ||
| bradykinin [no description available] | 7.31 | 1 | 0 | oligopeptide | human blood serum metabolite; vasodilator agent |
| 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. | 2.45 | 2 | 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. | 2.04 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| inositol 3-phosphate inositol 3-phosphate: RN given refers to (myo)-isomer | 3.39 | 1 | 1 | ||
| 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. | 2.75 | 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. | 2.46 | 2 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| 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. | 2.44 | 2 | 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. | 2.74 | 3 | 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. | 2.04 | 1 | 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. | 2.04 | 1 | 0 | acetate ester; steroid ester | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| rocuronium Rocuronium: An androstanol non-depolarizing neuromuscular blocking agent. It has a mono-quaternary structure and is a weaker nicotinic antagonist than PANCURONIUM.. rocuronium : A 5alpha-androstane compound having 3alpha-hydroxy-, 17beta-acetoxy-, 2beta-morpholino- and 16beta-N-allyllyrrolidinium substituents. | 2.04 | 1 | 0 | 3alpha-hydroxy steroid; acetate ester; androstane; morpholines; quaternary ammonium ion; tertiary amino compound | drug allergen; muscle relaxant; neuromuscular agent |
| 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. | 2.04 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| netilmicin Netilmicin: Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity. | 2.44 | 2 | 0 | ||
| miglitol [no description available] | 2.04 | 1 | 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. | 2.07 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | antihypertensive agent; EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor |
| bacampicillin bacampicillin: ester prodrug that is hydrolyzed to ampicillin after its absorption from the gastrointestinal tract; RN given refers to parent cpd; structure. bacampicillin : A penicillanic acid ester that is the 1-ethoxycarbonyloxyethyl ester of ampicillin. It is a semi-synthetic, microbiologically inactive prodrug of ampicillin. | 2.04 | 1 | 0 | penicillanic acid ester | prodrug |
| linezolid [no description available] | 2.04 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| canaline canaline: structure | 2.05 | 1 | 0 | amino acid zwitterion; non-proteinogenic L-alpha-amino acid | antimetabolite; antineoplastic agent; phytogenic insecticide; plant metabolite |
| angustibalin angustibalin: sesquiterpene lactone from Balduina angustifolia (Pursh) Robins; structure | 2.04 | 1 | 0 | sesquiterpene lactone | |
| ochratoxin a ochratoxin A: structure in first source & in Merck, 9th ed, #6549. ochratoxin A : A phenylalanine derivative resulting from the formal condensation of the amino group of L-phenylalanine with the carboxy group of (3R)-5-chloro-8-hydroxy-3-methyl-1-oxo-3,4-dihydro-1H-2-benzopyran-7-carboxylic acid (ochratoxin alpha). It is among the most widely occurring food-contaminating mycotoxins, produced by Aspergillus ochraceus, Aspergillus carbonarius and Penicillium verrucosum. | 2.41 | 1 | 0 | isochromanes; monocarboxylic acid amide; N-acyl-L-phenylalanine; organochlorine compound; phenylalanine derivative | Aspergillus metabolite; calcium channel blocker; carcinogenic agent; mycotoxin; nephrotoxin; Penicillium metabolite; teratogenic agent |
| tolterodine [no description available] | 2.04 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| metrizamide Metrizamide: A solute for density gradient centrifugation offering higher maximum solution density without the problems of increased viscosity. It is also used as a resorbable, non-ionic contrast medium. | 2.04 | 1 | 0 | amino sugar | |
| tibolone tibolone: used in prevention of postmenopausal osteoporosis. tibolone : Estran-3-one with a double bond between positions 5 and 10, and bearing both an ethynyl group and a hydroxy group at position 17 (R-configuration). A synthetic steroid hormone drug which acts as an agonist at all five type I steroid hormone receptors, it is used in the prevention of postmenopausal osteoporosis and for treatment of endometriosis. | 8.39 | 13 | 9 | 17beta-hydroxy steroid; terminal acetylenic compound | bone density conservation agent; hormone agonist |
| 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. | 2.04 | 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. | 2.04 | 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. | 2.53 | 2 | 0 | cyclodextrin | |
| acarbose [no description available] | 2.04 | 1 | 0 | amino cyclitol; glycoside | |
| 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. | 2.07 | 1 | 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 |
| resveratrol trans-resveratrol : A resveratrol in which the double bond has E configuration. | 7.52 | 2 | 0 | resveratrol | antioxidant; phytoalexin; plant metabolite; quorum sensing inhibitor; radical scavenger |
| 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). | 2.04 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| oleic acid Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry. | 3.17 | 5 | 0 | octadec-9-enoic acid | antioxidant; Daphnia galeata metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; Escherichia coli metabolite; mouse metabolite; plant metabolite; solvent |
| 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. | 2.04 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| cerivastatin cerivastatin: cerivastatin is the ((E)-(+))-isomer; structure given in first source. cerivastatin : (3R,5S)-3,5-dihydroxyhept-6-enoic acid in which the (7E)-hydrogen is substituted by a 4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl group. Formerly used (as its sodium salt) to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity. | 2.04 | 1 | 0 | dihydroxy monocarboxylic acid; pyridines; statin (synthetic) | |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 2.04 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| cocaine Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. | 2.04 | 1 | 0 | benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid | adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| eicosapentaenoic acid icosapentaenoic acid : Any straight-chain, C20 polyunsaturated fatty acid having five C=C double bonds.. all-cis-5,8,11,14,17-icosapentaenoic acid : An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17. | 2.17 | 1 | 0 | icosapentaenoic acid; omega-3 fatty acid | anticholesteremic drug; antidepressant; antineoplastic agent; Daphnia galeata metabolite; fungal metabolite; micronutrient; mouse metabolite; nutraceutical |
| 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. | 2.04 | 1 | 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 |
| 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. | 2.44 | 2 | 0 | ||
| lycopene [no description available] | 2 | 1 | 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. | 2.44 | 2 | 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. | 2.46 | 2 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| formycin [no description available] | 2.04 | 1 | 0 | formycin | antineoplastic agent |
| diethylstilbestrol Diethylstilbestrol: A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed). diethylstilbestrol : An olefinic compound that is trans-hex-3-ene in which the hydrogens at positions 3 and 4 have been replaced by p-hydroxyphenyl groups. | 11.81 | 44 | 18 | olefinic compound; polyphenol | antifungal agent; antineoplastic agent; autophagy inducer; calcium channel blocker; carcinogenic agent; EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; endocrine disruptor; xenoestrogen |
| bms 214662 7-cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3-(phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine: a farnesyltransferase inhibitor; structure in first source. BMS-214662 : A member of the class of benzodiazepines that is 2,3,4,5-tetrahydro-1H-1,4-benzodiazepine substituted by (1H-imidazol-5-yl)methyl, benzyl, (thiophen-2-yl)sulfonyl, and cyano groups at positions 1, 3R, 4 and 7, respectively. It is a potent inhibitor of farnesyltransferase (IC50 = 1.35nM) which was under clinical development for the treatment of solid tumors. | 2.04 | 1 | 0 | benzenes; benzodiazepine; imidazoles; nitrile; sulfonamide; thiophenes | antineoplastic agent; apoptosis inducer; EC 2.5.1.58 (protein farnesyltransferase) inhibitor |
| eptifibatide [no description available] | 2.04 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| gs 4071 GS 4071: The acid form.. oseltamivir acid : A cyclohexenecarboxylic acid that is cyclohex-1-ene-1-carboxylic acid which is substituted at positions 3, 4, and 5 by pentan-3-yloxy, acetamido, and amino groups, respectively (the 3R,4R,5S enantiomer). An antiviral drug, it is used as the corresponding ethyl ester prodrug, oseltamivir, to slow the spread of influenza. | 2.04 | 1 | 0 | acetate ester; amino acid; cyclohexenecarboxylic acid; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; marine xenobiotic metabolite |
| imidazolidines [no description available] | 6.96 | 14 | 6 | azacycloalkane; imidazolidines; saturated organic heteromonocyclic parent | |
| decitabine [no description available] | 2.04 | 1 | 0 | 2'-deoxyribonucleoside | |
| sm 8668 Sch 39304: Sch 42427 is the active entantiomer of the antifungal agent Sch 39304 which consists of Sch 42426 & Sch 42427; Sch 42426, the (S,S)-isomer, is inactive | 2.04 | 1 | 0 | ||
| teniposide [no description available] | 2.44 | 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 |
| troxacitabine troxacitabine: shows good anti-HIV activity without cytotoxicity | 2.04 | 1 | 0 | carbohydrate derivative; nucleobase-containing molecular entity | |
| purvalanol a 6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer; | 2.05 | 1 | 0 | purvalanol | |
| cefamandole Cefamandole: Semisynthetic wide-spectrum cephalosporin with prolonged action, probably due to beta-lactamase resistance. It is used also as the nafate.. cefamandole : A cephalosporin compound having (R)-mandelamido and N-methylthiotetrazole side-groups. | 2.44 | 2 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| 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) | 2.42 | 2 | 0 | actinomycin | mutagen |
| tiazofurin tiazofurin: RN given refers to (beta-D)-isomer; structure given in first source. tiazofurine : A C-glycosyl compound that is 1,3-thiazole-4-carboxamide in which the hydrogen at position 2 has been replaced by a beta-D-ribofuranosyl group. It is metabolised to thiazole-4-carboxamide adenine dinucleotide (TAD), a selective inhibitor of inosine monophosphate dehydrogenase (IMP dehydrogenase). | 2.44 | 2 | 0 | 1,3-thiazoles; C-glycosyl compound; monocarboxylic acid amide | antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; prodrug |
| azaserine Azaserine: Antibiotic substance produced by various Streptomyces species. It is an inhibitor of enzymatic activities that involve glutamine and is used as an antineoplastic and immunosuppressive agent.. azaserine : A carboxylic ester resulting from the formal condensation of the carboxy group of diazoacetic acid with the alcoholic hydroxy group of L-serine. An antibiotic produced by a Streptomyces species. | 2.04 | 1 | 0 | carboxylic ester; diazo compound; L-serine derivative; non-proteinogenic L-alpha-amino acid | antifungal agent; antimetabolite; antimicrobial agent; antineoplastic agent; glutamine antagonist; immunosuppressive agent; metabolite |
| 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. | 2.74 | 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 |
| sitafloxacin [no description available] | 2.04 | 1 | 0 | fluoroquinolone antibiotic; quinolines; quinolone antibiotic | |
| 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. | 2 | 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. | 2.04 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| dibekacin Dibekacin: Analog of KANAMYCIN with antitubercular as well as broad-spectrum antimicrobial properties.. dibekacin : A kanamycin that is kanamycin B lacking the 3- and 4-hydroxy groups on the 2,6-diaminosugar ring. | 2.04 | 1 | 0 | kanamycins | antibacterial agent; protein synthesis inhibitor |
| 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. | 2.04 | 1 | 0 | antibiotic antifungal drug; echinocandin | antiinfective agent |
| dipyrone Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.. metamizole sodium : An organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic. | 2.04 | 1 | 0 | organic sodium salt | anti-inflammatory agent; antipyretic; antirheumatic drug; cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug; prodrug |
| 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. | 4.03 | 4 | 0 | 2-bromocarboxylic acid; monocarboxylic acid; organochlorine compound | |
| Tetrahydropiperine [no description available] | 2.05 | 1 | 0 | benzodioxoles | |
| 4-[[bis(2-hydroxyethyl)amino]methyl]-2,6-ditert-butylphenol [no description available] | 2.04 | 1 | 0 | alkylbenzene | |
| aceglatone aceglatone: structure in Merck | 2.04 | 1 | 0 | organic molecular entity | |
| carbenoxolone [no description available] | 2.45 | 2 | 0 | ||
| isomethyleugenol Methylation: Addition of methyl groups. In histo-chemistry methylation is used to esterify carboxyl groups and remove sulfate groups by treating tissue sections with hot methanol in the presence of hydrochloric acid. (From Stedman, 25th ed) | 1.98 | 1 | 0 | isomethyleugenol | |
| piperine piperine : A N-acylpiperidine that is piperidine substituted by a (1E,3E)-1-(1,3-benzodioxol-5-yl)-5-oxopenta-1,3-dien-5-yl group at the nitrogen atom. It is an alkaloid isolated from the plant Piper nigrum. | 2.05 | 1 | 0 | benzodioxoles; N-acylpiperidine; piperidine alkaloid; tertiary carboxamide | food component; human blood serum metabolite; NF-kappaB inhibitor; plant metabolite |
| stilbenes Stilbenes: Organic compounds that contain 1,2-diphenylethylene as a functional group.. trans-stilbene : The trans-isomer of stilbene. | 2.52 | 2 | 0 | stilbene | |
| gonadotropin-releasing hormone relisorm L: Gonadotropin-Releasing Hormone analog. gonadorelin : A ten-membered synthetic oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, glycyl, leucyl, arginyl, prolyl and glycinamide residues joined in sequence. | 2.9 | 4 | 0 | oligopeptide; peptide hormone | gonadotropin releasing hormone agonist |
| ilepcimide ilepcimide: structure given in first source; RN given refers to compound with no isomeric designation | 2.05 | 1 | 0 | benzodioxoles | |
| cannabidiol Cannabidiol: Compound isolated from Cannabis sativa extract.. cannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4. | 2.6 | 1 | 0 | olefinic compound; phytocannabinoid; resorcinols | antimicrobial agent; plant metabolite |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 5.99 | 5 | 2 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| mezlocillin Mezlocillin: Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections.. mezlocillin : A penicillin in which the substituent at position 6 of the penam ring is a (2R)-2-[3-(methanesulfonyl)-2-oxoimidazolidine-1-carboxamido]-2-phenylacetamido group. | 2.04 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| amygdalin (R)-amygdalin : An amygdalin in which the stereocentre on the cyanohydrin function has R-configuration. | 2.04 | 1 | 0 | amygdalin | antineoplastic agent; apoptosis inducer; plant metabolite |
| mitobronitol Mitobronitol: Brominated analog of MANNITOL which is an antineoplastic agent appearing to act as an alkylating agent. | 2.04 | 1 | 0 | alcohol; organobromine compound | |
| tropisetron Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine. | 2.04 | 1 | 0 | indolyl carboxylic acid | |
| octotropine methylbromide octotropine methylbromide: minor descriptor (65-86); on line & INDEX MEDICUS search TROPANES (69-86); RN given refers to endo-isomer. anisotropine methylbromide : A quaternary ammonium salt resulting from the reaction of the amino group of anisotropine with methyl bromide. | 2.45 | 2 | 0 | ||
| fludarabine [no description available] | 2.44 | 2 | 0 | purine nucleoside | |
| 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. | 2.94 | 4 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| ipratropium bromide anhydrous [no description available] | 2.05 | 1 | 0 | ||
| ipratropium [no description available] | 2.07 | 1 | 0 | ||
| methylatropine nitrate [no description available] | 2.04 | 1 | 0 | ||
| sesquiterpenes [no description available] | 3.08 | 1 | 0 | ||
| 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. | 2.04 | 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. | 2.74 | 3 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| thioinosine Thioinosine: Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503) | 2.04 | 1 | 0 | ||
| cotinine Cotinine: The N-glucuronide conjugate of cotinine is a major urinary metabolite of NICOTINE. It thus serves as a biomarker of exposure to tobacco SMOKING. It has CNS stimulating properties.. (-)-cotinine : An N-alkylpyrrolidine that consists of N-methylpyrrolidinone bearing a pyridin-3-yl substituent at position C-5 (the 5S-enantiomer). It is an alkaloid commonly found in Nicotiana tabacum. | 2.04 | 1 | 0 | N-alkylpyrrolidine; pyridines; pyrrolidin-2-ones; pyrrolidine alkaloid | antidepressant; biomarker; human xenobiotic metabolite; plant metabolite |
| flunarizine Flunarizine: Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. | 2.05 | 1 | 0 | diarylmethane | |
| thiouracil Thiouracil: Occurs in seeds of Brassica and Crucifera species. Thiouracil has been used as antithyroid, coronary vasodilator, and in congestive heart failure although its use has been largely supplanted by other drugs. It is known to cause blood dyscrasias and suspected of terato- and carcinogenesis.. thiouracil : A nucleobase analogue that is uracil in which the oxo group at C-2 is replaced by a thioxo group. | 2.04 | 1 | 0 | nucleobase analogue; thiocarbonyl compound | antithyroid drug; metabolite |
| thiohydantoins Thiohydantoins: Sulfur analogs of hydantoins with one or both carbonyl groups replaced by thiocarbonyl groups. | 5.99 | 2 | 2 | ||
| 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. | 2.44 | 2 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid drug |
| 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. | 2.47 | 2 | 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 |
| enclomiphene Enclomiphene: The trans or (E)-isomer of clomiphene. | 9.25 | 25 | 7 | ||
| drotaverin drotaverin: Hungarian drug; RN given refers to parent cpd; structure | 2.04 | 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. | 2.04 | 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. | 3.41 | 1 | 1 | 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. | 2.97 | 4 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| 6-thioguanosine 6-thioguanosine: RN given refers to cpd without isomeric designation | 2.04 | 1 | 0 | purine nucleoside | |
| streptozocin [no description available] | 2.04 | 1 | 0 | ||
| tamoxifen [no description available] | 12.54 | 37 | 9 | 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] | 2.45 | 2 | 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. | 2.45 | 2 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 2.04 | 1 | 0 | ||
| artemotil artemotil: structure given in first source; RN given refers to cpd without isomeric designation | 2.05 | 1 | 0 | artemisinin derivative | |
| 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. | 2.44 | 2 | 0 | carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound | antimicrobial agent; bacterial metabolite |
| thiopental Thiopental: A barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration.. thiopental : A barbiturate, the structure of which is that of 2-thiobarbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 2.04 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; environmental contaminant; intravenous anaesthetic; sedative; xenobiotic |
| estrone sulfate estrone sulfate: sulfoconjugated estrone; RN given refers to parent cpd | 2.01 | 1 | 0 | 17-oxo steroid; steroid sulfate | human metabolite; mouse metabolite |
| thiocarlide thiocarlide: major descriptor (68-85); on-line search PHENYLTHIOUREA/AA (68-85); Index Medicus search THIOCARLIDE (68-85); Antitubercular Agent | 2.04 | 1 | 0 | thioureas | |
| hmr 3647 [no description available] | 2.04 | 1 | 0 | ||
| 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. | 7.41 | 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). | 2.04 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine [no description available] | 2.04 | 1 | 0 | aromatic ether | |
| fosfestrol fosfestrol: Rx of prostatic carcinoma; RN given refers to parent cpd with unspecified isomeric designation; structure | 5.22 | 4 | 3 | aryl phosphate | |
| cobaltous chloride cobaltous chloride: RN given refers to unlabeled cpd; RN in Chemline for cobalt trichloride: 10241-04-0; RN for 60-labeled cpd: 14543-09-0; RN for 57-labeled cpd: 164113-89-1; RN for 58-labeled cpd: 29377-09-1; structure. cobalt dichloride : A cobalt salt in which the cobalt metal is in the +2 oxidation state and the counter-anion is chloride. It is used as an indicator for water in desiccants. | 2.01 | 1 | 0 | cobalt salt; inorganic chloride | allergen; calcium channel blocker; sensitiser; two-colour indicator |
| dolasetron [no description available] | 2.04 | 1 | 0 | indolyl carboxylic acid | |
| or 1259 [no description available] | 2.04 | 1 | 0 | hydrazone; nitrile; pyridazinone | anti-arrhythmia drug; cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; vasodilator agent |
| mannomustine Mannomustine: Nitrogen mustard derivative alkylating agent used as antineoplastic. It causes severe bone marrow depression and is a powerful vesicant. | 2.04 | 1 | 0 | amino alcohol | |
| monooctanoin monooctanoin: dissolution agent for retained cholesterol bile duct stones; RN in Chemline for octanoic acid, ester with 1,2,3-propanetriol, MF unknown: 11140-04-8; RN for octanoic acid, 2,3-dihydroxypropyl ester (1-monooctanoin): 502-54-5; RN in 9th CI Form Index for (+-)-1-monooctanoin: 19670-49-6. rac-1-monooctanoylglycerol : A rac-1-monoacylglycerol comprising equal amounts of 1-octanoyl-sn-glycerol and 3-octanoyl-sn-glycerol.. 1-monooctanoylglycerol : A 1-monoglyceride that has octanoyl as the acyl group. | 2.1 | 1 | 0 | 1-monoglyceride; octanoate ester; rac-1-monoacylglycerol | |
| gestodene Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer | 4.35 | 4 | 1 | steroid | estrogen |
| glucametacin glucametacin: indomethacin analog; structure | 2.45 | 2 | 0 | ||
| quinine [no description available] | 2.45 | 2 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| androstane-3,17-diol glucuronide androstane-3,17-diol glucuronide: RN given refers to cpd with unspecified glucuronide locant | 3.77 | 2 | 0 | steroid ester | |
| rtki cpd RTKI cpd: preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors | 2.03 | 1 | 0 | ||
| 1-(2-(2-(4-pyridyl)-2-imidazoline-1-yl)ethyl)-3-(4-carboxyphenyl)urea 1-(2-(2-(4-pyridyl)-2-imidazoline-1-yl)ethyl)-3-(4-carboxyphenyl)urea: RN given refers to parent cpd; structure in first source | 2.04 | 1 | 0 | ||
| isepamicin [no description available] | 2.04 | 1 | 0 | ||
| ifetroban ifetroban: thromboxane receptor antagonist; structure given in first source; a 7-oxabicyclo(2.2.1)heptane derivative | 2.04 | 1 | 0 | benzenes; monocarboxylic acid | |
| lamifiban lamifiban: a nonpeptide glycoprotein IIb/IIIa antagonist; prevents platelet loss during experimental cardiopulmonary bypass | 2.04 | 1 | 0 | N-acylglycine | |
| telavancin telavancin: an anti-infective agent; structure in first source. telavancin : A glycopeptide that is vancomycin substituted at position N-3'' by a 2-(decylamino)ethyl group and at position C-29 by a (phosphonomethyl)aminomethyl group. Used as its hydrochloride salt for treatment of adults with complicated skin and skin structure infections caused by bacteria. | 2.04 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent |
| quinagolide quinagolide: structure & RN given in first source; a non-ergot dopamine D(2)-agonist | 3.25 | 1 | 0 | organic heterotricyclic compound; organonitrogen heterocyclic compound | |
| 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. | 2.15 | 1 | 0 | organic sodium salt | detergent; protein denaturant |
| mtt formazan MTT formazan: a blue MEM-insoluble mitochondrial byproduct; used to determine viability of cells with active mitochondrial dehydrogenase enzymes | 2.02 | 1 | 0 | ||
| alpha-chymotrypsin Chymotrypsin: A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side. | 3.13 | 5 | 0 | ||
| 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. | 3.36 | 1 | 1 | ||
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 2.04 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| osteoprotegerin Osteoprotegerin: A secreted member of the TNF receptor superfamily that negatively regulates osteoclastogenesis. It is a soluble decoy receptor of RANK LIGAND that inhibits both CELL DIFFERENTIATION and function of OSTEOCLASTS by inhibiting the interaction between RANK LIGAND and RECEPTOR ACTIVATOR OF NUCLEAR FACTOR-KAPPA B. | 3.81 | 2 | 1 | long-chain fatty acid | |
| 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. | 2.04 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| alsterpaullone alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole. | 2.05 | 1 | 0 | C-nitro compound; caprolactams; organic heterotetracyclic compound | anti-HIV-1 agent; antineoplastic agent; apoptosis inducer; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor |
| 2-mercaptoacetate 2-mercaptoacetate: RN given refers to parent cpd | 2.48 | 2 | 0 | monocarboxylic acid anion | |
| quercetin [no description available] | 2.04 | 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 |
| bilirubin [no description available] | 2.41 | 2 | 0 | biladienes; dicarboxylic acid | antioxidant; human metabolite; mouse metabolite |
| dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins. | 1.99 | 1 | 0 | prostaglandins E | human metabolite; mouse metabolite; oxytocic |
| dinoprost Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor. | 2.06 | 1 | 0 | monocarboxylic acid; prostaglandins Falpha | human metabolite; mouse metabolite |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 4.85 | 4 | 2 | 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 |
| vitamin k semiquinone radical vitamin K semiquinone radical: found in active preparations of vitamin K-dependent carboxylase. vitamin K : Any member of a group of fat-soluble 2-methyl-1,4-napthoquinones that exhibit biological activity against vitamin K deficiency. Vitamin K is required for the synthesis of prothrombin and certain other blood coagulation factors. | 3.38 | 1 | 1 | ||
| hymecromone Hymecromone: A coumarin derivative possessing properties as a spasmolytic, choleretic and light-protective agent. It is also used in ANALYTICAL CHEMISTRY TECHNIQUES for the determination of NITRIC ACID. | 2.04 | 1 | 0 | hydroxycoumarin | antineoplastic agent; hyaluronic acid synthesis inhibitor |
| alprostadil [no description available] | 2.75 | 3 | 0 | prostaglandins E | anticoagulant; human metabolite; platelet aggregation inhibitor; vasodilator agent |
| 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. | 2.75 | 3 | 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. | 2.46 | 2 | 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. | 2.46 | 2 | 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 |
| 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. | 2.04 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 2.76 | 3 | 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. | 2.04 | 1 | 0 | isoquinolines | |
| 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. | 2.04 | 1 | 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] | 2.04 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| usambarensine usambarensine: structure given in first source | 2.05 | 1 | 0 | harmala alkaloid | |
| cynarine cynarine: active principle of the artichoke; functions primarily as a cholagogue and choleretic and also as antilipemic agent | 2.45 | 2 | 0 | alkyl caffeate ester; quinic acid | plant metabolite |
| sdz psc 833 valspodar: nonimmunosuppressive cyclosporin analog which is a potent multidrug resistance modifier; 7-10 fold more potent than cyclosporin A; a potent P glycoprotein inhibitor; MW 1215 | 2.04 | 1 | 0 | homodetic cyclic peptide | |
| 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. | 2.04 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| menatetrenone menaquinone-4 : A menaquinone whose side-chain contains 4 isoprene units in an all-trans-configuration. | 8.38 | 1 | 1 | menaquinone | anti-inflammatory agent; antioxidant; bone density conservation agent; human metabolite; neuroprotective agent |
| 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. | 2.11 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| indocyanine green [no description available] | 2.04 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| 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. | 2.05 | 1 | 0 | N-alkylpyrrolidine; olefinic compound; pyridines | H1-receptor antagonist |
| menaquinone 6 menaquinone 6: RN given refers to (all-E)-isomer | 3.38 | 1 | 1 | ||
| codeine [no description available] | 2.74 | 3 | 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 | 2.74 | 3 | 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 |
| phenylephrine hydrochloride Nose: A part of the upper respiratory tract. It contains the organ of SMELL. The term includes the external nose, the nasal cavity, and the PARANASAL SINUSES.. phenylephrine hydrochloride : A hydrochloride that is the monohydrochloride salt of phenylephrine. | 1.96 | 1 | 0 | hydrochloride | |
| cyproterone Cyproterone: An anti-androgen that, in the form of its acetate (CYPROTERONE ACETATE), also has progestational properties. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. | 5.27 | 6 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; chlorinated steroid; tertiary alpha-hydroxy ketone | androgen antagonist |
| dihydrocodeine dihydrocodeine: RN refers to parent cpd(5alpha,6alpha)-isomer | 2.45 | 2 | 0 | morphinane alkaloid | |
| estropipate estropipate: used therapeutically in menopausal patients | 3.37 | 1 | 1 | piperazinium salt; steroid sulfate | |
| granisetron Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.. granisetron : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 1-methyl-1H-indazole-3-carboxylic acid with the primary amino group of (3-endo)-9-methyl-9-azabicyclo[3.3.1]nonan-3-amine. A selective 5-HT3 receptor antagonist, it is used (generally as the monohydrochloride salt) to manage nausea and vomiting caused by cancer chemotherapy and radiotherapy, and to prevent and treat postoperative nausea and vomiting. | 3.09 | 1 | 0 | aromatic amide; indazoles | |
| hydrocodone Hydrocodone: Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant.. hydrocodone : A morphinane-like compound that is a semi-synthetic opioid synthesized from codeine. | 2.07 | 1 | 0 | morphinane-like compound; organic heteropentacyclic compound | antitussive; mu-opioid receptor agonist; opioid analgesic |
| 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. | 2.46 | 2 | 0 | morphinane alkaloid; organic heteropentacyclic compound | mu-opioid receptor agonist; opioid analgesic |
| 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. | 2.45 | 2 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nalmefene nalmefene: RN given refers to 5-alpha isomer | 2.04 | 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. | 2.74 | 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. | 2.04 | 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) | 2.07 | 1 | 0 | morphinane alkaloid | |
| alvocidib alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation. | 2.04 | 1 | 0 | dihydroxyflavone; hydroxypiperidine; monochlorobenzenes; tertiary amino compound | antineoplastic agent; antirheumatic drug; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 4.52 | 5 | 1 | 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 |
| pactamycin Pactamycin: Antibiotic produced by Streptomyces pactum used as an antineoplastic agent. It is also used as a tool in biochemistry because it inhibits certain steps in protein synthesis. | 2.04 | 1 | 0 | ||
| anthramycin [no description available] | 2.04 | 1 | 0 | ||
| cicaprost cicaprost: RN given refers to (3aS-(2E,3aalpha,4alpha(3R*,4R*),5beta,6aalpha))-isomer | 2.04 | 1 | 0 | monoterpenoid | |
| 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. | 3.43 | 6 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 2.04 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| 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. | 19.98 | 232 | 73 | organic molecular entity | |
| iloprost Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.. iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension. | 2.04 | 1 | 0 | carbobicyclic compound; monocarboxylic acid; secondary alcohol | platelet aggregation inhibitor; vasodilator agent |
| lacidipine [no description available] | 2.45 | 2 | 0 | cinnamate ester; tert-butyl ester | |
| lysophosphatidylcholines lysophosphatidylcholine : An acylglycerophosphocholine resulting from partial hydrolysis of a phosphatidylcholine, which removes one of the fatty acyl groups. The structure is depicted in the image where R1 = acyl, R2 = H or where R1 = H, R2 = acyl. | 2.44 | 2 | 0 | 1-O-acyl-sn-glycero-3-phosphocholine | |
| cytochalasin b Cytochalasin B: A cytotoxic member of the CYTOCHALASINS.. cytochalasin B : An organic heterotricyclic compound, that is a mycotoxin which is cell permeable an an inhibitor of cytoplasmic division by blocking the formation of contractile microfilaments. | 2.04 | 1 | 0 | cytochalasin; lactam; lactone; organic heterotricyclic compound | actin polymerisation inhibitor; metabolite; mycotoxin; platelet aggregation inhibitor |
| 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. | 2.46 | 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. | 2.46 | 2 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 2.74 | 3 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| onapristone onapristone: induces vaginal bleeding and luteal regression in monkeys; structure given in first source; progesterone antagonist | 2.01 | 1 | 0 | ||
| irisquinone irisquinone: from seeds of Iris pallasii Iridaceae; RN given refers to (Z)-isomer | 2.04 | 1 | 0 | ||
| licochalcone a licochalcone A: has both anti-inflammatory and antineoplastic activities; structure given in first source; isolated from root of Glycyrrhiza inflata; RN given refers to (E)-isomer | 2.05 | 1 | 0 | chalcones | |
| 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. | 2.07 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 3.47 | 1 | 1 | 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 |
| palbociclib [no description available] | 4 | 2 | 0 | aminopyridine; aromatic ketone; cyclopentanes; piperidines; pyridopyrimidine; secondary amino compound; tertiary amino compound | antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| mitoguazone Mitoguazone: Antineoplastic agent effective against myelogenous leukemia in experimental animals. Also acts as an inhibitor of animal S-adenosylmethionine decarboxylase.. mitoguazone : A hydrazone obtained by formal condensation of the two carbonyl groups of methylglyoxal with the primary amino groups of two molecules of aminoguanidine. | 2.04 | 1 | 0 | guanidines; hydrazone | antineoplastic agent; apoptosis inducer; EC 4.1.1.50 (adenosylmethionine decarboxylase) inhibitor |
| stilbamidine stilbamidine: RN given refers to parent cpd | 2.05 | 1 | 0 | ||
| romidepsin depsipeptide : A natural or synthetic compound having a sequence of amino and hydroxy carboxylic acid residues (usually alpha-amino and alpha-hydroxy acids), commonly but not necessarily regularly alternating. | 2.04 | 1 | 0 | cyclodepsipeptide; heterocyclic antibiotic; organic disulfide | antineoplastic agent; EC 3.5.1.98 (histone deacetylase) inhibitor |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 2.04 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| arsenic Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed) | 3.12 | 1 | 0 | metalloid atom; pnictogen | micronutrient |
| 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. | 4.65 | 3 | 2 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| morphine-6-glucuronide morphine-6-glucuronide: RN given refers to (5alpha,6alpha)-isomer | 2.04 | 1 | 0 | morphinane alkaloid | |
| 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. | 2.46 | 2 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefodizime cefodizime: RN given refers to (6R-(6alpha,7beta(Z)))-isomer. cefodizime : A cephalosporin compound having 5-(carboxymethyl)-4-methyl-1,3-thiazol-2-yl]sulfanyl}methyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups located at positions 3 and 7 respectively. | 2.04 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; EC 1.14.18.1 (tyrosinase) inhibitor |
| methylnaltrexone methylnaltrexone: RN given refers to parent cpd(5alpha)-isomer | 2.04 | 1 | 0 | phenanthrenes | |
| cefixime [no description available] | 2.44 | 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. | 2.04 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| 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. | 2.04 | 1 | 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 |
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 2.46 | 2 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| piperic acid piperinic acid: from Piper longum; structure in first source. (E,E)-piperic acid : A monocarboxylic acid that is (E)-penta-2,4-dienoic acid substituted by a 1,3-benzodioxol-5-yl group at position 5. It has been isolated from black pepper (Piper nigrum). | 2.05 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; benzodioxoles | plant metabolite |
| 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). | 2.04 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| nitrofurazone Nitrofurazone: A topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial WOUNDS AND INJURIES and skin infections. Nitrofurazone has also been administered orally in the treatment of TRYPANOSOMIASIS.. nitrofurazone : A semicarbazone resulting from the formal condensation of semicarbazide with 5-nitrofuraldehyde. A broad spectrum antibacterial drug, although with little activity against Pseudomonas species, it is used as a local application for burns, ulcers, wounds and skin infections. | 2.04 | 1 | 0 | ||
| silicon Silicon: A trace element that constitutes about 27.6% of the earth's crust in the form of SILICON DIOXIDE. It does not occur free in nature. Silicon has the atomic symbol Si, atomic number 14, and atomic weight [28.084; 28.086]. | 2.13 | 1 | 0 | carbon group element atom; metalloid atom; nonmetal atom | |
| phosphorus Phosphorus: A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions. | 3.39 | 1 | 1 | monoatomic phosphorus; nonmetal atom; pnictogen | macronutrient |
| 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. | 2.04 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| cefuroxime [no description available] | 2.44 | 2 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 2.74 | 3 | 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. | 2.04 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| hr 810 cefpirome: structure in first source. cefpirome : A fourth-generation cephalosporin antibiotic having 6,7-dihydro-5H-cyclopenta[b]pyridinium-1-ylmethyl and [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups located at positions 3 and 7 respectively. | 2.04 | 1 | 0 | cephalosporin; cyclopentapyridine | |
| ceftazidime [no description available] | 2.74 | 3 | 0 | cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| ay 25,205 surfagon: potent LHRH agonist; RN given refers to (D-Ala-L-Pro)-isomer | 2.36 | 2 | 0 | ||
| strontium radioisotopes Strontium Radioisotopes: Unstable isotopes of strontium that decay or disintegrate spontaneously emitting radiation. Sr 80-83, 85, and 89-95 are radioactive strontium isotopes. | 3.1 | 1 | 0 | ||
| cefetamet cefetamet: active against Neisseria gonorrhoeae; structure given in first source. cefetamet : A cephalosporin compound having methyl and [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side-groups; a cephalosporin antibiotic active against Neisseria gonorrhoeae. | 2.04 | 1 | 0 | cephalosporin | |
| triolein Triolein: (Z)-9-Octadecenoic acid 1,2,3-propanetriyl ester.. triolein : A triglyceride formed by esterification of the three hydroxy groups of glycerol with oleic acid. Triolein is one of the two components of Lorenzo's oil. | 4.39 | 1 | 1 | triglyceride | Caenorhabditis elegans metabolite; plant metabolite |
| famotidine [no description available] | 2.04 | 1 | 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. | 2.04 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 2.46 | 2 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| lhrh, n-et-alanh2(6)- [no description available] | 1.97 | 1 | 0 | ||
| proguanil Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells. | 2.05 | 1 | 0 | biguanides; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| ginkgolide b [no description available] | 2.04 | 1 | 0 | ||
| radium Radium: A radioactive element of the alkaline earth series of metals. It has the atomic symbol Ra and atomic number 88. Radium is the product of the disintegration of URANIUM and is present in pitchblende and all ores containing uranium. It is used clinically as a source of beta and gamma-rays in radiotherapy, particularly BRACHYTHERAPY. | 3.21 | 1 | 0 | alkaline earth metal atom | |
| ceftiofur [no description available] | 2.04 | 1 | 0 | ||
| whewellite whewellite: calcium oxalate mineral | 2.13 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| cefatrizine Cefatrizine: Orally active semisynthetic cephalosporin antibiotic with broad-spectrum activity.. cefatrizine : A cephalosporin compound having (1H-1,2,3-triazol-4-ylsulfanyl)methyl and [(2R)-2-amino-2-(4-hydroxyphenyl)]acetamido side-groups. An antibacterial drug first prepared in the 1970s, it has more recently been found to be an inhibitor of eukaryotic elongation factor-2 kinase (eEF2K), which is known to regulate apoptosis, autophagy and ER stress in many types of human cancers. | 2.04 | 1 | 0 | amino acid amide; carboxylic acid; cephalosporin; phenols; semisynthetic derivative; triazoles | antibacterial drug; EC 2.7.11.20 (elongation factor 2 kinase) inhibitor |
| pregnanediol [no description available] | 6.08 | 3 | 2 | ||
| eniporide eniporide: inhibits NHE-1 isoform; structure in first source | 2.04 | 1 | 0 | ||
| cilastatin [no description available] | 2.44 | 2 | 0 | carboxamide; L-cysteine derivative; non-proteinogenic L-alpha-amino acid; organic sulfide | EC 3.4.13.19 (membrane dipeptidase) inhibitor; environmental contaminant; protease inhibitor; xenobiotic |
| sibiromycin [no description available] | 2.04 | 1 | 0 | aminoglycoside antibiotic; hemiaminal; phenols; pyrrolobenzodiazepine | antineoplastic agent; bacterial metabolite |
| everolimus [no description available] | 9.63 | 2 | 2 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 2.04 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| nifuroxime 5-nitro-2-furaldehyde oxime: structure in first source | 2.05 | 1 | 0 | ||
| azlocillin Azlocillin: A semisynthetic ampicillin-derived acylureido penicillin.. azlocillin : A semisynthetic penicillin having a 6beta-{(2R)-2-[(2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl}amino side-group. It is an antibiotic used in treating infections caused by Pseudomonas aeruginosa, Escherichia coli and Haemophilus influenzae. | 2.04 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial drug |
| tanespimycin CP 127374: analog of herbimycin A | 3.13 | 1 | 0 | 1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound; secondary amino compound | antineoplastic agent; apoptosis inducer; Hsp90 inhibitor |
| verlukast verlukast: LTD4 receptor antagonist | 2.04 | 1 | 0 | ||
| ceftizoxime [no description available] | 2.44 | 2 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 2.45 | 2 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| carumonam carumonam: structure given in first source; RN given refers to (2S-(2alpha,3alpha(Z))-isomer. carumonam : An N-sulfonated monobactam antibiotic. | 2.04 | 1 | 0 | monobactam | antibacterial drug |
| 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. | 2.74 | 3 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| nifurtimox Nifurtimox: A nitrofuran thiazine that has been used against TRYPANOSOMIASIS. | 2.05 | 1 | 0 | nitrofuran antibiotic | |
| butylscopolammonium bromide Butylscopolammonium Bromide: Antimuscarinic quaternary ammonium derivative of scopolamine used to treat cramps in gastrointestinal, urinary, uterine, and biliary tracts, and to facilitate radiologic visualization of the gastrointestinal tract. | 2.45 | 2 | 0 | ||
| ergoline Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.. ergoline : An indole alkaloid whose structural skeleton is found in many naturally occurring and synthetic ergolines which are known to bind to neurotransmitter receptors, such as dopamine, noradrenaline and serotonin receptors and function as unselective agonists or antagonists at these receptors. | 5.05 | 4 | 0 | diamine; ergoline alkaloid; indole alkaloid fundamental parent; indole alkaloid; organic heterotetracyclic compound | |
| eritoran eritoran : A lipid A derivative used for the treatment of severe sepsis. | 2.04 | 1 | 0 | lipid As | |
| dantrolene [no description available] | 2.46 | 2 | 0 | ||
| roxithromycin (E)-roxithromycin : A major geometrical isomer of roxithromycin. | 2.05 | 1 | 0 | roxithromycin | environmental contaminant; xenobiotic |
| fumagillin [no description available] | 2.04 | 1 | 0 | antibiotic antifungal drug; carboxylic ester; dicarboxylic acid monoester; meroterpenoid; organooxygen heterocyclic antibiotic; spiro-epoxide | angiogenesis inhibitor; antibacterial drug; antimicrobial agent; antiprotozoal drug; fungal metabolite; methionine aminopeptidase 2 inhibitor |
| etonogestrel [no description available] | 3.41 | 1 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| artesunate artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether | 2.45 | 2 | 0 | artemisinin derivative; cyclic acetal; dicarboxylic acid monoester; hemisuccinate; semisynthetic derivative; sesquiterpenoid | antimalarial; antineoplastic agent; ferroptosis inducer |
| dexniguldipine niguldipine: structure given in first source; clinical modulator of multidrug resistance | 2.04 | 1 | 0 | diarylmethane | |
| fedotozine fedotozine: affects gastrointestinal motility in dogs | 3.09 | 1 | 0 | ||
| napsagatran napsagatran: structure given in first source | 2.04 | 1 | 0 | ||
| temsirolimus [no description available] | 2.04 | 1 | 0 | macrolide lactam | |
| dutasteride Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. | 4.58 | 2 | 0 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| hexarelin hexarelin: a synthetic growth hormone releasing peptide; structurally similar to GHRP-6, with the substitution of D-Trp with its 2-methyl derivative; more potent & stable and less toxic than GHRP-6 | 2.11 | 1 | 0 | ||
| bms188797 [no description available] | 2.04 | 1 | 0 | ||
| staurosporine staurosporinium : Conjugate acid of staurosporine. | 1.98 | 1 | 0 | ammonium ion derivative | |
| formazans Formazans: Colored azo compounds formed by the reduction of tetrazolium salts. Employing this reaction, oxidoreductase activity can be determined quantitatively in tissue sections by allowing the enzymes to act on their specific substrates in the presence of tetrazolium salts. | 2.02 | 1 | 0 | ||
| 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. | 2.04 | 1 | 0 | ||
| azimilide azimilide: structure given in first source; RN given refers to dihydrochloride | 2.04 | 1 | 0 | imidazolidine-2,4-dione | |
| chlorproguanil chlorproguanil: dichloro-derivative of chloroguanide; RN given refers to parent cpd; structure | 2.05 | 1 | 0 | dichlorobenzene | |
| asoprisnil asoprisnil: structure in first source | 4.16 | 2 | 0 | ||
| tomopenem [no description available] | 2.04 | 1 | 0 | ||
| 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. | 12.72 | 7 | 5 | pyridines; sterol ester | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug |
| omacor Omacor: a drug containing the n-3 fatty acids that corrects plasma lipid; antiarrhthymic | 2.17 | 1 | 0 | ||
| 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. | 1.97 | 1 | 0 | oligopeptide | |
| bb-83698 BB-83698: peptide deformylase inhibitor | 2.04 | 1 | 0 | ||
| 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. | 2.41 | 1 | 0 | organic molecular entity | |
| cabazitaxel cabazitaxel: an antineoplastic agent; structure in first source. cabazitaxel : A tetracyclic diterpenoid that is 10-deacetylbaccatin III having O-methyl groups attached at positions 7 and 10 as well as an O-(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl group attached at position 13. Acts as a microtubule inhibitor, binds tubulin and promotes microtubule assembly and simultaneously inhibits disassembly. | 10.45 | 3 | 1 | tetracyclic diterpenoid | antineoplastic agent; microtubule-stabilising agent |
| t 98475 T 98475: structure in first source | 2.41 | 2 | 0 | isopropyl ester; thienopyridine | |
| zotarolimus zotarolimus: synthetic analog of rapamycin; structure in first source | 2.04 | 1 | 0 | lactam; macrolide | |
| treosulfan treosulfan: immunosuppressant; RN given refers to (S-(R*,R*))-isomer | 5.22 | 3 | 1 | methanesulfonate ester | |
| gentamicin sulfate [no description available] | 2.74 | 3 | 0 | ||
| bn 52020 [no description available] | 2.04 | 1 | 0 | ||
| n1-phenyl-3,5-dinitro-n4,n4-di-n-propylsulfanilamide N1-phenyl-3,5-dinitro-N4,N4-di-n-propylsulfanilamide: a potent, selective antimitotic agent against kinetoplastid parasites; structure in first source | 2.05 | 1 | 0 | ||
| nkp 608 [no description available] | 2.04 | 1 | 0 | ||
| sorbitan monooleate [no description available] | 7.81 | 3 | 0 | fatty acid ester | |
| ganu GANU: differs from chlorozotocin by placement of cytotoxic group on C-1 of the glucose ring; less myelosuppressive than chlorozotocin; structure | 2.04 | 1 | 0 | ||
| artenimol artenimol: derivative of antimalarial drug artemisinin (quinghaosu) | 2.05 | 1 | 0 | ||
| 4-phenoxyphenoxyethyl thiocyanate 4-phenoxyphenoxyethyl thiocyanate: has antiparasitic activity; structure in first source | 2.05 | 1 | 0 | ||
| tak 385 relugolix: structure in first source | 10.84 | 11 | 6 | ||
| homatropine methylbromide homatropine methylbromide: RN given refers to bromide (endo-(+-))-isomer | 2.07 | 1 | 0 | ||
| 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. | 2.08 | 1 | 0 | alpha-D-glucosyl-(1->4)-D-mannopyranose | |
| metamelfalan [no description available] | 2.04 | 1 | 0 | ||
| nbi 42902 [no description available] | 2.03 | 1 | 0 | ||
| elagolix [no description available] | 6.26 | 3 | 2 | organonitrogen compound; organooxygen compound | |
| vindesine [no description available] | 2.44 | 2 | 0 | ||
| 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. | 4.75 | 2 | 1 | ||
| diflucortolone Diflucortolone: A topical glucocorticoid used in various DERMATOSES. It is absorbed through the skin, bound to plasma albumin, and may cause adrenal suppression. It is also administered as the valerate. | 2.45 | 2 | 0 | 21-hydroxy steroid | |
| scopolamine hydrobromide [no description available] | 2.04 | 1 | 0 | ||
| pituitrin Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR). | 3.1 | 1 | 0 | ||
| lhrh, ala(6)-gly(10)-ethylamide- LHRH, Ala(6)-Gly(10)-ethylamide-: a growth hormone agonistic analog; RN given is for acetate salt | 4.52 | 5 | 1 | ||
| 2-((3-chloroethyl)-3-nitrosoureido)glucopyranose [no description available] | 2.04 | 1 | 0 | ||
| ro 6-4563 glibornuride: was MH 1975-92 (see under SULFONYLUREA COMPOUNDS 1975-90); use SULFONYLUREA COMPOUNDS to search GLIBORNURIDE 1975-92; an oral, sulfonylurea hypoglycemic agent which stimulates insulin secretion | 2.04 | 1 | 0 | monoterpenoid | |
| acid phosphatase Acid Phosphatase: An enzyme that catalyzes the conversion of an orthophosphoric monoester and water to an alcohol and orthophosphate. EC 3.1.3.2. | 8.55 | 16 | 9 | ||
| ulipristal ulipristal: a progestins antagonist | 4.13 | 2 | 0 | 20-oxo steroid | |
| deoxoartemisinin deoxoartemisinin: structure given in first source | 2.05 | 1 | 0 | ||
| glyx-13 peptide GLYX-13 peptide: a monoclonal antibody-derived peptide that acts as an N-methyl-D-aspartate receptor modulator | 2.31 | 1 | 0 | ||
| mdv 3100 [no description available] | 9.13 | 9 | 5 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent |
| amodiaquine hydrochloride [no description available] | 2.47 | 2 | 0 | ||
| cytochrome c-t Cytochromes c: Cytochromes of the c type that are found in eukaryotic MITOCHONDRIA. They serve as redox intermediates that accept electrons from MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX III and transfer them to MITOCHONDRIAL ELECTRON TRANSPORT COMPLEX IV. | 2.46 | 2 | 0 | ||
| bisaramil [no description available] | 2.04 | 1 | 0 | ||
| calcitonin [no description available] | 2.11 | 1 | 0 | ||
| cosyntropin Cosyntropin: A synthetic peptide that is identical to the 24-amino acid segment at the N-terminal of ADRENOCORTICOTROPIC HORMONE. ACTH (1-24), a segment similar in all species, contains the biological activity that stimulates production of CORTICOSTEROIDS in the ADRENAL CORTEX.. cosyntropin : A synthetic peptide that is identical to the 24-amino acid segment at the N-terminal of adrenocorticotropic hormone (corticotropin). A segment similar in all species, it contains the biological activity that stimulates production of corticosteroids in the adrenal cortex. It is used diagnostically to investigate adrenocortical insufficiency. | 3.38 | 1 | 1 | ||
| detirelix detirelix: LHRH antagonist | 1.98 | 1 | 0 | ||
| atrial natriuretic factor Atrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS. | 3.39 | 1 | 1 | polypeptide | |
| teicoplanin teicoplanin A2-1 : A teicoplanin A2 that has (4Z)-dec-4-enoyl as the variable N-acyl group. | 2.04 | 1 | 0 | ||
| iturelix iturelix: a gonadotropin-releasing hormone antagonist | 4.15 | 16 | 0 | ||
| ganirelix [no description available] | 13.3 | 38 | 18 | polypeptide | |
| abarelix abarelix: RN & structure in first source. abarelix : A polypeptide compound composed of ten natural and non-natural amino acid resiudes in a linear sequence. | 8.58 | 11 | 4 | polypeptide | antineoplastic agent; hormone antagonist |
| glucagon Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence. | 2 | 1 | 0 | peptide hormone | |
| beta-endorphin beta-Endorphin: A 31-amino acid peptide that is the C-terminal fragment of BETA-LIPOTROPIN. It acts on OPIOID RECEPTORS and is an analgesic. Its first four amino acids at the N-terminal are identical to the tetrapeptide sequence of METHIONINE ENKEPHALIN and LEUCINE ENKEPHALIN.. beta-endorphin : A polypeptide consisting of 31 amino acid residues in the sequence Tyr-Gly-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Lys-Asn-Ala-Ile-Ile-Lys-Asn-Ala-Tyr-Lys-Lys-Gly-Glu. It is an endogenous opioid peptide neurotransmitter found in the neurons of both the central and peripheral nervous system and results from processing of the precursor protein proopiomelanocortin (POMC). | 3.78 | 2 | 1 | ||
| thymosin beta(4) thymosin beta(4): biological active peptide present in thymosin fractions 5 & 5A; participates in the regulation, differentiation & function of thymus-derived lymphocytes & may also act directly or indirectly on macrophages & other cells involved in cell-mediated immunity | 1.98 | 1 | 0 | ||
| tannins Tannins: Polyphenolic compounds with molecular weights of around 500-3000 daltons and containing enough hydroxyl groups (1-2 per 100 MW) for effective cross linking of other compounds (ASTRINGENTS). The two main types are HYDROLYZABLE TANNINS and CONDENSED TANNINS. Historically, the term has applied to many compounds and plant extracts able to render skin COLLAGEN impervious to degradation. The word tannin derives from the Celtic word for OAK TREE which was used for leather processing. | 2.25 | 1 | 0 | ||
| ly-146032 [no description available] | 2.04 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| dalbavancin [no description available] | 2.04 | 1 | 0 | carbohydrate acid derivative; glycopeptide; monosaccharide derivative; semisynthetic derivative | antibacterial drug; antimicrobial agent |
| 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 | 13.23 | 45 | 16 | polypeptide | |
| lhrh, n-ac-2-nal(1)-4-cl-phe(2)-trp(3)-hci(6)-alanh2(10)- LHRH, N-Ac-2-Nal(1)-4-Cl-Phe(2)-Trp(3)-Hci(6)-AlaNH2(10)-: RN given refers to (D-Ala-D-Phe-D-Trp-L-Ser-L-Tyr-D-Lys-L-Leu-L-Arg-L-Pro-D-Ala)-isomer; RN for cpd without isomeric designation not avail 10/90; LHRH antagonist | 3.08 | 5 | 0 | ||
| c-peptide C-Peptide: The middle segment of proinsulin that is between the N-terminal B-chain and the C-terminal A-chain. It is a pancreatic peptide of about 31 residues, depending on the species. Upon proteolytic cleavage of proinsulin, equimolar INSULIN and C-peptide are released. C-peptide immunoassay has been used to assess pancreatic beta cell function in diabetic patients with circulating insulin antibodies or exogenous insulin. Half-life of C-peptide is 30 min, almost 8 times that of insulin. | 3.8 | 2 | 1 | ||
| cellulose DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications. | 2.4 | 2 | 0 | glycoside | |
| endothelin-1 Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63) | 2 | 1 | 0 | ||
| phosphatidylcholines Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety. | 3.19 | 5 | 0 | 1,2-diacyl-sn-glycero-3-phosphocholine | |
| hoe 33342 bisbenzimide ethoxide trihydrochloride: benzimidazole fluorescent dye | 2 | 1 | 0 | ||
| valproate sodium Epilim: oral sodium valproate used as antidepressive agent. sodium valproate : The sodium salt of valproic acid.. valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid. | 2.05 | 1 | 0 | organic sodium salt | geroprotector |
| flucloronide flucloronide: synthetic glucocorticoid with anti-inflammatory properties; minor descriptor (75-83); on-line & Index Medicus search PREGNADIENETROLS (75-83); RN given refers to (6alpha,11beta,16alpha)-isomer; structure | 2.04 | 1 | 0 | 21-hydroxy steroid | |
| silicate cement Silicate Cement: A relatively hard, translucent, restorative material used primarily in anterior teeth. (From Boucher's Clinical Dental Terminology, 4th ed, p50) | 7.31 | 1 | 0 | ||
| menotropins Menotropins: Extracts of urine from menopausal women that contain high concentrations of pituitary gonadotropins, FOLLICLE STIMULATING HORMONE and LUTEINIZING HORMONE. Menotropins are used to treat infertility. The FSH:LH ratio and degree of purity vary in different preparations. | 15.86 | 161 | 48 | ||
| chitosan [no description available] | 3.42 | 7 | 0 | ||
| bucladesine Bucladesine: A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed). bucladesine : A 3',5'-cyclic purine nucleotide that is the 2'-butanoate ester and 6-N-butanoyl derivative of 3',5'-cyclic AMP. | 2.4 | 2 | 0 | 3',5'-cyclic purine nucleotide | |
| osteum [no description available] | 2.75 | 3 | 0 | organic molecular entity | |
| apalutamide [no description available] | 5.99 | 2 | 2 | ||
| 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene [no description available] | 2.13 | 1 | 0 | BODIPY compound | |
| trelstar Triptorelin Pamoate: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6. | 15.78 | 117 | 26 | ||
| 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. | 12.12 | 45 | 13 | oligopeptide | antineoplastic agent; GnRH antagonist |
| nafarelin Nafarelin: A potent synthetic agonist of GONADOTROPIN-RELEASING HORMONE with 3-(2-naphthyl)-D-alanine substitution at residue 6. Nafarelin has been used in the treatments of central PRECOCIOUS PUBERTY and ENDOMETRIOSIS.. nafarelin : An oligopeptide comprising of 5-oxo-L-proline, L-histidine, L-tryptophan, L-serine, L-tyrosine, 3-(2-naphthyl)-D-alanine, L-leucine, L-arginine and L-prolylglycinamide residues joined sequence by peptide linkages. It is a gonadotropin releasing hormone agonist that is used to treat central precocious puberty in children and endometriosis in women. | 13.53 | 54 | 16 | oligopeptide | anti-estrogen; gonadotropin releasing hormone agonist |
| deslorelin deslorelin: Ovuplant is tradename for a short-term-release implant containing deslorelin acetate; RN given refers to D-isomer; RN for cpd without isomeric designation not avail 12/90 | 5.35 | 7 | 2 | oligopeptide | |
| lutrelin acetate lutrelin acetate: LH-FSH agonist | 1.97 | 1 | 0 | ||
| histrelin histrelin: gonadotropin releasing hormone agonist. histrelin : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, 1-benzyl-D-histidyl, 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 diacetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty. | 4.59 | 7 | 0 | oligopeptide | antineoplastic agent; gonadotropin releasing hormone agonist |
| lhrh, n-ac-ala(1)-(4-cl-phe)(2)-trp(3,6)- LHRH, N-Ac-Ala(1)-(4-Cl-Phe)(2)-Trp(3,6)-: gonadorelin antagonist | 1.96 | 1 | 0 | ||
| lhrh, ac-dehydro-pro(1)-4-cl-phe(2)-trp(3,6)- LHRH, Ac-dehydro-Pro(1)-4-Cl-Phe(2)-Trp(3,6)-: gonadorelin antagonist | 2 | 1 | 0 | ||
| ovurelin ovurelin: GnRH agonist | 1.95 | 1 | 0 | ||
| lhrh, phe(6)- LHRH, Phe(6)-: RN given refers to (D)-isomer | 1.95 | 1 | 0 | ||
| hainanolide hainanolide: from bark of Cephalotaxux hainensis | 2.04 | 1 | 0 | ||
| kisspeptin-10 protein, human [no description available] | 2.21 | 1 | 0 | ||
| gliocladic acid gliocladic acid: from Gliocladium virens, Chaetomium globosum & Trichoderma viride; structure given in first source | 2.04 | 1 | 0 | p-menthane monoterpenoid | |
| piperidines Piperidines: A family of hexahydropyridines. | 2 | 1 | 0 | ||
| thymosin Thymosin: Thymosin. A family of heat-stable, polypeptide hormones secreted by the thymus gland. Their biological activities include lymphocytopoiesis, restoration of immunological competence and enhancement of expression of T-cell characteristics and function. They have therapeutic potential in patients having primary or secondary immunodeficiency diseases, cancer or diseases related to aging. | 2.38 | 2 | 0 | ||
| cleistanthin cleistanthin: lignan lactone toxic glycoside from Cleistanthus collinus (Roxb); structure. cleistanthin A : A member of the class of cleistanthins that is the 4-O-3,4-di-O-methyl-beta-D-xylopyranoside of 1,3-dihydronaphtho[2,3-c]furan-4-ol which is substituted by an oxo group at position 1, methoxy groups at positions 6 and 7, and a 1,3-benzodioxol-5-yl group at position 9. It is one of the toxic principles in Cleistanthus collinus. | 2.04 | 1 | 0 | cleistanthins; xylose derivative | alpha-adrenergic antagonist; antihypertensive agent; diuretic |
| tak-683 TAK-683: has antineoplastic activity | 7.1 | 1 | 0 | ||
| nimorazole [no description available] | 2.04 | 1 | 0 | ||
| butyrolactone i butyrolactone I: selective inhibitor of cdk2 & cdc2 kinase; structure given in first source | 2.05 | 1 | 0 | butenolide | |
| 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. | 2.45 | 2 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| novobiocin Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189). novobiocin : A coumarin-derived antibiotic obtained from Streptomyces niveus. | 2.04 | 1 | 0 | carbamate ester; ether; hexoside; hydroxycoumarin; monocarboxylic acid amide; monosaccharide derivative; phenols | antibacterial agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Escherichia coli metabolite; hepatoprotective agent |
| 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. | 2.97 | 4 | 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. | 2.44 | 2 | 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. | 2.74 | 3 | 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. | 2.97 | 4 | 0 | ||
| salicylates Salicylates: The salts or esters of salicylic acids, or salicylate esters of an organic acid. Some of these have analgesic, antipyretic, and anti-inflammatory activities by inhibiting prostaglandin synthesis.. hydroxybenzoate : Any benzoate derivative carrying a single carboxylate group and at least one hydroxy substituent.. salicylates : Any salt or ester arising from reaction of the carboxy group of salicylic acid, or any ester resulting from the condensation of the phenolic hydroxy group of salicylic acid with an organic acid.. salicylate : A monohydroxybenzoate that is the conjugate base of salicylic acid. | 1.96 | 1 | 0 | monohydroxybenzoate | plant metabolite |
| piroxicam [no description available] | 2.47 | 2 | 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 | 2.04 | 1 | 0 | aromatic amide | |
| bactobolin bactobolin: from Pseudomonas sp. BN-183; has MF C14-H20-Cl2-N2-O6; RN given refers to parent cpd(R*)-isomer | 2.04 | 1 | 0 | amino acid 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. | 2.04 | 1 | 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. | 2.74 | 3 | 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. | 2.04 | 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. | 2.46 | 2 | 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. | 2.44 | 2 | 0 | ||
| rolitetracycline Rolitetracycline: A pyrrolidinylmethyl TETRACYCLINE.. rolitetracycline : A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group. | 2.45 | 2 | 0 | ||
| tigecycline [no description available] | 2.04 | 1 | 0 | ||
| epidermal growth factor Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form. | 4.35 | 6 | 0 | ||
| transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins. | 5 | 9 | 1 | ||
| kiss1 protein, human Kisspeptins: Intercellular signaling peptides that were originally characterized by their ability to suppress NEOPLASM METASTASIS. Kisspeptins have since been found to play an important role in the neuroendocrine regulation of REPRODUCTION. | 4.31 | 5 | 0 | ||
| lumacaftor, ivacaftor drug combination Orkambi : A two-drug mixture consisting of lumacaftor and ivacaftor, which is used for the treatment of cystic fibrosis. | 2.25 | 1 | 0 | ||
| adrenomedullin Adrenomedullin: A 52-amino acid peptide with multi-functions. It was originally isolated from PHEOCHROMOCYTOMA and ADRENAL MEDULLA but is widely distributed throughout the body including lung and kidney tissues. Besides controlling fluid-electrolyte homeostasis, adrenomedullin is a potent vasodilator and can inhibit pituitary ACTH secretion. | 2.01 | 1 | 0 | ||
| peoniflorin peoniflorin: from Radix and of Paeonia suffruticosa | 3.23 | 1 | 0 | ||
| vitamin b 12 Vitamin B 12: A cobalt-containing coordination compound produced by intestinal micro-organisms and found also in soil and water. Higher plants do not concentrate vitamin B 12 from the soil and so are a poor source of the substance as compared with animal tissues. INTRINSIC FACTOR is important for the assimilation of vitamin B 12. | 4.09 | 3 | 1 | ||
| oblimersen oblimersen: targets the Bcl-2 oncogene good efficacy with low toxicity tumour regressions | 3.12 | 1 | 0 | ||
| sermorelin Sermorelin: The biologically active fragment of human growth hormone-releasing factor, consisting of GHRH(1-29)-amide. This N-terminal sequence is identical in several mammalian species, such as human, pig, and cattle. It is used to diagnose or treat patients with GROWTH HORMONE deficiency.. sermorelin : A 29 amino acid polypeptide that is used to treat growth problems (usually in children) due to growth hormone deficiency. It is the biologically active fragment of human growth hormone-releasing factor (GHRH). | 3.17 | 1 | 0 | ||
| transforming growth factor alpha Transforming Growth Factor alpha: An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR. | 2 | 1 | 0 | ||
| cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed). | 2.82 | 2 | 0 | ||
| orabase Orabase: used in therapy of oral mucosal ulcers | 2.01 | 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. | 1.97 | 1 | 0 | ||
| muramidase Muramidase: A basic enzyme that is present in saliva, tears, egg white, and many animal fluids. It functions as an antibacterial agent. The enzyme catalyzes the hydrolysis of 1,4-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrin. EC 3.2.1.17. | 2.02 | 1 | 0 | ||
| scleroglucan [no description available] | 7.03 | 1 | 0 | oligosaccharide | |
| amyloid beta-peptides amyloid beta-protein (1-40): although acutely neurotoxic in both rat & monkey cerebral cortex, neuronal degeneration in primates resembles more closely to that found in Alzheimer's disease; amino acid sequence has been determined | 2.49 | 2 | 0 | ||
| chondroitin sulfates Chondroitin Sulfates: Derivatives of chondroitin which have a sulfate moiety esterified to the galactosamine moiety of chondroitin. Chondroitin sulfate A, or chondroitin 4-sulfate, and chondroitin sulfate C, or chondroitin 6-sulfate, have the sulfate esterified in the 4- and 6-positions, respectively. Chondroitin sulfate B (beta heparin; DERMATAN SULFATE) is a misnomer and this compound is not a true chondroitin sulfate. | 2.06 | 1 | 0 | ||
| 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. | 5.03 | 3 | 1 | 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. | 3.4 | 1 | 1 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 2.97 | 4 | 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. | 2.75 | 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. | 2.74 | 3 | 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. | 2.46 | 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] | 2.44 | 2 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| 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. | 4.32 | 1 | 1 | 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. | 2.04 | 1 | 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. | 2.47 | 2 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| penciclovir penciclovir : A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclovir, is used for oral administration. | 2.04 | 1 | 0 | 2-aminopurines; propane-1,3-diols | antiviral drug |
| 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. | 2.04 | 1 | 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. | 2.97 | 4 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| azaguanine Azaguanine: One of the early purine analogs showing antineoplastic activity. It functions as an antimetabolite and is easily incorporated into ribonucleic acids.. 8-azaguanine : A triazolopyrimidine that consists of 3,6-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidine bearing amino and oxo substituents at positions 5 and 7 respectively. | 2.04 | 1 | 0 | nucleobase analogue; triazolopyrimidines | antimetabolite; antineoplastic agent; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 2.04 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| thiolactomycin thiolactomycin: from actinomycetes; structure given in first source | 2.05 | 1 | 0 | ||
| alanosine [no description available] | 2.04 | 1 | 0 | ||
| 3,4,5-trihydroxybenzamidoxime 3,4,5-trihydroxybenzamidoxime: structure given in first source | 2.05 | 1 | 0 | benzenetriol | |
| 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 | 2.04 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| 7-deazaguanosine 7-deazaguanosine: structure given in first source | 2.04 | 1 | 0 | ||
| tirapazamine Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4. | 2.04 | 1 | 0 | aromatic amine; benzotriazines; N-oxide | antibacterial agent; antineoplastic agent; apoptosis inducer |
| 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. | 2.6 | 1 | 0 | citrate salt | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| 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. | 2.04 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| ceftobiprole ceftobiprole: BAL5788 is Ceftobiprole medocaril sodium. ceftobiprole : A fifth-generation cephalosporin antibiotic having (E)-[(3'R)-2-oxo[1,3'-bipyrrolidin]-3-ylidene]methyl and [(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(hydroxyimino)acetyl]amino side groups located at positions 3 and 7 respectively; developed for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP). | 2.04 | 1 | 0 | cephalosporin; thiadiazoles | antimicrobial agent |
| pyrazofurin pirazofurin : A C-glycosyl compound that is 4-hydroxy-1H-pyrazole-5-carboxamide in which the hydrogen at position 3 has been replaced by a beta-D-ribofuranosyl group. | 2.04 | 1 | 0 | C-glycosyl compound; pyrazoles | antimetabolite; antimicrobial agent; antineoplastic agent; EC 4.1.1.23 (orotidine-5'-phosphate decarboxylase) inhibitor |
| rifabutin [no description available] | 2.04 | 1 | 0 | ||
| n(10)-methylfolate [no description available] | 2.04 | 1 | 0 | folic acids | |
| 5-methyltetrahydrohomofolic acid 5-methyltetrahydrohomofolic acid: RN given refers to parent cpd | 2.04 | 1 | 0 | ||
| ninopterin ninopterin: structure | 2.04 | 1 | 0 | ||
| eye [no description available] | 1.98 | 1 | 0 | ||
| leptin Leptin: A 16-kDa peptide hormone secreted from WHITE ADIPOCYTES. Leptin serves as a feedback signal from fat cells to the CENTRAL NERVOUS SYSTEM in regulation of food intake, energy balance, and fat storage. | 11.4 | 9 | 5 | ||
| pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O. | 10.14 | 9 | 4 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Parasite Infections [description not available] | 0 | 2.05 | 1 | 0 |
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 4.31 | 4 | 1 |
| Adverse Drug Event [description not available] | 0 | 6.12 | 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 | 4.31 | 4 | 1 |
| 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 | 6.12 | 6 | 1 |
| Congenital Zika Syndrome [description not available] | 0 | 2.25 | 1 | 0 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 9.74 | 51 | 1 |
| Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME. | 0 | 2.25 | 1 | 0 |
| Cancer of Prostate [description not available] | 0 | 30.27 | 886 | 343 |
| Prostatic Neoplasms Tumors or cancer of the PROSTATE. | 1 | 31.65 | 2,658 | 1,029 |
| Deficiency, Vitamin D [description not available] | 0 | 2.31 | 1 | 0 |
| Gender Dysphoria A marked difference between the individual’s expressed/experienced gender and the gender others would assign to the individual, and it must continue for at least six months. (from DSM-5) | 0 | 5.43 | 4 | 1 |
| Vitamin D Deficiency A nutritional condition produced by a deficiency of VITAMIN D in the diet, insufficient production of vitamin D in the skin, inadequate absorption of vitamin D from the diet, or abnormal conversion of vitamin D to its bioactive metabolites. It is manifested clinically as RICKETS in children and OSTEOMALACIA in adults. (From Cecil Textbook of Medicine, 19th ed, p1406) | 0 | 2.31 | 1 | 0 |
| Endometrioma An enlarged area of ENDOMETRIOSIS that resembles a tumor. It is usually found in the OVARY. When it is filled with old blood, it is known as a chocolate cyst. | 0 | 20.42 | 290 | 94 |
| Endometriosis A condition in which functional endometrial tissue is present outside the UTERUS. It is often confined to the PELVIS involving the OVARY, the ligaments, cul-de-sac, and the uterovesical peritoneum. | 1 | 22.42 | 290 | 94 |
| Infarct [description not available] | 0 | 2.41 | 1 | 0 |
| Fibroid [description not available] | 0 | 19.22 | 226 | 83 |
| Cancer of the Uterus [description not available] | 0 | 19.35 | 234 | 88 |
| Leiomyoma A benign tumor derived from smooth muscle tissue, also known as a fibroid tumor. They rarely occur outside of the UTERUS and the GASTROINTESTINAL TRACT but can occur in the SKIN and SUBCUTANEOUS TISSUE, probably arising from the smooth muscle of small blood vessels in these tissues. | 1 | 21.22 | 226 | 83 |
| Uterine Neoplasms Tumors or cancer of the UTERUS. | 0 | 19.35 | 234 | 88 |
| Familial Precocious Puberty [description not available] | 0 | 17.42 | 179 | 30 |
| Puberty, Precocious Development of SEXUAL MATURATION in boys and girls at a chronological age that is 2.5 standard deviations below the mean age at onset of PUBERTY in the population. This early maturation of the hypothalamic-pituitary-gonadal axis results in sexual precocity, elevated serum levels of GONADOTROPINS and GONADAL STEROID HORMONES such as ESTRADIOL and TESTOSTERONE. | 0 | 17.42 | 179 | 30 |
| Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders. | 0 | 9.36 | 16 | 8 |
| 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 | 2.31 | 1 | 0 |
| Angiitis [description not available] | 0 | 2.73 | 3 | 0 |
| Vasculitis Inflammation of any one of the blood vessels, including the ARTERIES; VEINS; and rest of the vasculature system in the body. | 0 | 2.73 | 3 | 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 | 21.61 | 405 | 124 |
| Pelvic Pain Pain in the pelvic region of genital and non-genital origin. | 0 | 14.32 | 38 | 16 |
| Breast Cancer [description not available] | 0 | 14.03 | 64 | 20 |
| Breast Neoplasms Tumors or cancer of the human BREAST. | 1 | 16.03 | 64 | 20 |
| Angiomyxoma [description not available] | 0 | 8.65 | 9 | 0 |
| Cancer of the Vulva [description not available] | 0 | 2.97 | 4 | 0 |
| Vulvar Neoplasms Tumors or cancer of the VULVA. | 0 | 2.97 | 4 | 0 |
| Cyst [description not available] | 0 | 4.1 | 3 | 1 |
| Liver Dysfunction [description not available] | 0 | 3.85 | 2 | 1 |
| Liver Diseases Pathological processes of the LIVER. | 0 | 3.85 | 2 | 1 |
| Diffuse Parenchymal Lung Disease [description not available] | 0 | 3.29 | 6 | 0 |
| Lung Diseases, Interstitial A diverse group of lung diseases that affect the lung parenchyma. They are characterized by an initial inflammation of PULMONARY ALVEOLI that extends to the interstitium and beyond leading to diffuse PULMONARY FIBROSIS. Interstitial lung diseases are classified by their etiology (known or unknown causes), and radiological-pathological features. | 0 | 3.29 | 6 | 0 |
| Cancer of Pituitary [description not available] | 0 | 5.14 | 17 | 0 |
| Apoplexy, Pituitary [description not available] | 0 | 3.91 | 12 | 0 |
| Pituitary Neoplasms Neoplasms which arise from or metastasize to the PITUITARY GLAND. The majority of pituitary neoplasms are adenomas, which are divided into non-secreting and secreting forms. Hormone producing forms are further classified by the type of hormone they secrete. Pituitary adenomas may also be characterized by their staining properties (see ADENOMA, BASOPHIL; ADENOMA, ACIDOPHIL; and ADENOMA, CHROMOPHOBE). Pituitary tumors may compress adjacent structures, including the HYPOTHALAMUS, several CRANIAL NERVES, and the OPTIC CHIASM. Chiasmal compression may result in bitemporal HEMIANOPSIA. | 0 | 5.14 | 17 | 0 |
| Exanthem [description not available] | 0 | 2.41 | 1 | 0 |
| Exanthema Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology. | 0 | 2.41 | 1 | 0 |
| Benign Neoplasms [description not available] | 0 | 5.31 | 8 | 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. | 1 | 7.31 | 8 | 0 |
| Myoma A benign neoplasm of muscular tissue. (Stedman, 25th ed) | 1 | 11.31 | 4 | 1 |
| Malignant Melanoma [description not available] | 0 | 5.78 | 2 | 1 |
| Melanoma A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445) | 1 | 7.78 | 2 | 1 |
| Androgen-Independent Prostatic Cancer [description not available] | 0 | 7.57 | 10 | 1 |
| 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 | 9.57 | 10 | 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). | 1 | 11.67 | 19 | 3 |
| Adenomyoma A benign neoplasm of muscle (usually smooth muscle) with glandular elements. It occurs most frequently in the uterus and uterine ligaments. (Stedman, 25th ed) | 0 | 7.07 | 6 | 2 |
| Blood Loss, Surgical Loss of blood during a surgical procedure. | 0 | 6.18 | 9 | 4 |
| Adenomyosis The extension of endometrial tissue (ENDOMETRIUM) into the MYOMETRIUM. It usually occurs in women in their reproductive years and may result in a diffusely enlarged uterus with ectopic and benign endometrial glands and stroma. | 0 | 7.47 | 14 | 1 |
| Injuries, Spinal Cord [description not available] | 0 | 4.33 | 3 | 1 |
| Spinal Cord Injuries Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.). | 0 | 4.33 | 3 | 1 |
| Menstruation, Painful [description not available] | 0 | 11.36 | 23 | 7 |
| Dysmenorrhea Painful menstruation. | 0 | 11.36 | 23 | 7 |
| Delayed Puberty [description not available] | 0 | 8.57 | 8 | 0 |
| Polycystic Ovarian Syndrome [description not available] | 0 | 15.95 | 83 | 31 |
| 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 | 15.95 | 83 | 31 |
| Cardiac Diseases [description not available] | 0 | 2.6 | 1 | 0 |
| Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities. | 0 | 2.6 | 1 | 0 |
| Disease Exacerbation [description not available] | 0 | 13.11 | 46 | 15 |
| Cancer of Granulosa Cells [description not available] | 0 | 3.13 | 5 | 0 |
| Cancer of Ovary [description not available] | 0 | 10.36 | 45 | 5 |
| 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. | 1 | 12.36 | 45 | 5 |
| Local Neoplasm Recurrence [description not available] | 0 | 15.01 | 72 | 35 |
| Sterility, Female [description not available] | 0 | 17.33 | 143 | 55 |
| Infertility, Female Diminished or absent ability of a female to achieve conception. | 0 | 17.33 | 143 | 55 |
| Deficiency, Protein C [description not available] | 0 | 2.21 | 1 | 0 |
| Heart Valve Diseases Pathological conditions involving any of the various HEART VALVES and the associated structures (PAPILLARY MUSCLES and CHORDAE TENDINEAE). | 0 | 2.21 | 1 | 0 |
| Blood Clot [description not available] | 0 | 3.65 | 3 | 0 |
| Acute Disease Disease having a short and relatively severe course. | 0 | 4.9 | 8 | 1 |
| Thrombosis Formation and development of a thrombus or blood clot in the blood vessel. | 0 | 3.65 | 3 | 0 |
| Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. | 0 | 10.82 | 40 | 3 |
| Nanism [description not available] | 0 | 4.34 | 4 | 0 |
| Dwarfism A genetic or pathological condition that is characterized by short stature and undersize. Abnormal skeletal growth usually results in an adult who is significantly below the average height. | 0 | 4.34 | 4 | 0 |
| Neurogenic Bowel Loss or absence of normal intestinal function due to nerve damage or birth defects. It is characterized by the inability to control the elimination of stool from the body. | 0 | 7.25 | 1 | 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 | 5.66 | 6 | 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 | 5.66 | 6 | 1 |
| Heavy Menstrual Bleeding [description not available] | 0 | 13.13 | 46 | 17 |
| Anemia A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN. | 0 | 5.71 | 7 | 1 |
| Menorrhagia Excessive uterine bleeding during MENSTRUATION. | 0 | 13.13 | 46 | 17 |
| Age-Related Osteoporosis [description not available] | 0 | 11.79 | 37 | 12 |
| Paraphilias [description not available] | 0 | 13.95 | 23 | 1 |
| 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 | 11.79 | 37 | 12 |
| Recrudescence [description not available] | 0 | 9.92 | 33 | 5 |
| Angiospasm, Intracranial [description not available] | 0 | 2.21 | 1 | 0 |
| Alarm Clock Headache [description not available] | 0 | 2.21 | 1 | 0 |
| Brain Vascular Disorders [description not available] | 0 | 2.21 | 1 | 0 |
| Symptom Cluster [description not available] | 0 | 4.7 | 11 | 0 |
| Cerebrovascular Disorders A spectrum of pathological conditions of impaired blood flow in the brain. They can involve vessels (ARTERIES or VEINS) in the CEREBRUM, the CEREBELLUM, and the BRAIN STEM. Major categories include INTRACRANIAL ARTERIOVENOUS MALFORMATIONS; BRAIN ISCHEMIA; CEREBRAL HEMORRHAGE; and others. | 0 | 2.21 | 1 | 0 |
| Menopause The last menstrual period. Permanent cessation of menses (MENSTRUATION) is usually defined after 6 to 12 months of AMENORRHEA in a woman over 45 years of age. In the United States, menopause generally occurs in women between 48 and 55 years of age. | 1 | 19.45 | 31 | 11 |
| Syndrome A characteristic symptom complex. | 0 | 4.7 | 11 | 0 |
| Vasospasm, Intracranial Constriction of arteries in the SKULL due to sudden, sharp, and often persistent smooth muscle contraction in blood vessels. Intracranial vasospasm results in reduced vessel lumen caliber, restricted blood flow to the brain, and BRAIN ISCHEMIA that may lead to hypoxic-ischemic brain injury (HYPOXIA-ISCHEMIA, BRAIN). | 0 | 2.21 | 1 | 0 |
| Angiogenesis, Pathologic [description not available] | 0 | 6.63 | 6 | 2 |
| Blastocyst Disintegration [description not available] | 0 | 2.25 | 1 | 0 |
| Postpartum Amenorrhea [description not available] | 0 | 8.21 | 13 | 2 |
| Amenorrhea Absence of menstruation. | 0 | 13.21 | 13 | 2 |
| 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 | 9.17 | 6 | 0 |
| Hyperandrogenism A condition caused by the excessive secretion of ANDROGENS from the ADRENAL CORTEX; the OVARIES; or the TESTES. The clinical significance in males is negligible. In women, the common manifestations are HIRSUTISM and VIRILISM as seen in patients with POLYCYSTIC OVARY SYNDROME and ADRENOCORTICAL HYPERFUNCTION. | 1 | 11.67 | 26 | 8 |
| Libman-Sacks Disease [description not available] | 0 | 6.09 | 6 | 1 |
| FMR1-Related Primary Ovarian Insufficiency [description not available] | 0 | 9.36 | 18 | 5 |
| Lupus Erythematosus, Systemic A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow. | 0 | 6.09 | 6 | 1 |
| Primary Ovarian Insufficiency Cessation of ovarian function after MENARCHE but before the age of 40, without or with OVARIAN FOLLICLE depletion. It is characterized by the presence of OLIGOMENORRHEA or AMENORRHEA, elevated GONADOTROPINS, and low ESTRADIOL levels. It is a state of female HYPERGONADOTROPIC HYPOGONADISM. Etiologies include genetic defects, autoimmune processes, chemotherapy, radiation, and infections. The most commonly known genetic cause is the expansion of a CGG repeat to 55 to 199 copies in the 5' untranslated region in the X-linked FMR1 gene. | 0 | 9.36 | 18 | 5 |
| Hepatitis B Virus Infection [description not available] | 0 | 2.25 | 1 | 0 |
| Diffuse Large B-Cell Lymphoma [description not available] | 0 | 2.25 | 1 | 0 |
| Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact. | 0 | 2.25 | 1 | 0 |
| Lymphoma, Large B-Cell, Diffuse Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation. | 0 | 2.25 | 1 | 0 |
| Allergy, Drug [description not available] | 0 | 3.12 | 5 | 0 |
| Drug Hypersensitivity Immunologically mediated adverse reactions to medicinal substances used legally or illegally. | 0 | 3.12 | 5 | 0 |
| Cystic Fibrosis of Pancreas [description not available] | 0 | 2.25 | 1 | 0 |
| Thoracic Diseases Disorders affecting the organs of the thorax. | 0 | 3.44 | 2 | 0 |
| Cystic Fibrosis An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION. | 0 | 2.25 | 1 | 0 |
| Hemoptysis Expectoration or spitting of blood originating from any part of the RESPIRATORY TRACT, usually from hemorrhage in the lung parenchyma (PULMONARY ALVEOLI) and the BRONCHIAL ARTERIES. | 0 | 3.26 | 6 | 0 |
| Urinary Incontinence Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE. | 0 | 5.24 | 6 | 2 |
| 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 | 11.42 | 31 | 4 |
| Fatty Liver, Nonalcoholic [description not available] | 0 | 2.25 | 1 | 0 |
| Non-alcoholic Fatty Liver Disease Fatty liver finding without excessive ALCOHOL CONSUMPTION. | 0 | 2.25 | 1 | 0 |
| Hepatocellular Carcinoma [description not available] | 0 | 4.68 | 3 | 2 |
| Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested. | 0 | 4.68 | 3 | 2 |
| Adenocarcinoma, Basal Cell [description not available] | 0 | 20.26 | 234 | 110 |
| Adenocarcinoma A malignant epithelial tumor with a glandular organization. | 0 | 20.26 | 234 | 110 |
| Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM. | 0 | 10.36 | 15 | 5 |
| Insulin Sensitivity [description not available] | 0 | 10.27 | 26 | 7 |
| 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 | 10.27 | 26 | 7 |
| Carcinoma, Anaplastic [description not available] | 0 | 10.52 | 32 | 6 |
| Cancer of Salivary Gland [description not available] | 0 | 4.46 | 4 | 1 |
| 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 | 10.52 | 32 | 6 |
| Salivary Gland Neoplasms Tumors or cancer of the SALIVARY GLANDS. | 0 | 4.46 | 4 | 1 |
| Choroidal Detachment Separation of the CHOROID from the SCLERA. | 0 | 2.31 | 1 | 0 |
| Cancer of Pancreas [description not available] | 0 | 4.09 | 3 | 1 |
| Carcinoma, Ductal, Pancreatic [description not available] | 0 | 2.25 | 1 | 0 |
| Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA). | 0 | 4.09 | 3 | 1 |
| Carcinoma, Pancreatic Ductal Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS. | 0 | 2.25 | 1 | 0 |
| Nycturia [description not available] | 0 | 2.25 | 1 | 0 |
| Nocturia Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS). | 0 | 2.25 | 1 | 0 |
| Atrophy, Muscular, Spinobulbar [description not available] | 0 | 5.87 | 9 | 0 |
| 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. | 0 | 5.87 | 9 | 0 |
| Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal. | 0 | 2.77 | 3 | 0 |
| Hyperglycemia Abnormally high BLOOD GLUCOSE level. | 0 | 2.77 | 3 | 0 |
| Peripheral Nerve Injury [description not available] | 0 | 2.25 | 1 | 0 |
| Peripheral Nerve Injuries Injuries to the PERIPHERAL NERVES. | 0 | 2.25 | 1 | 0 |
| Ache [description not available] | 0 | 12.69 | 31 | 18 |
| Complications, Pregnancy [description not available] | 0 | 2.55 | 2 | 0 |
| Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. | 1 | 14.69 | 31 | 18 |
| Benign Meningeal Neoplasms [description not available] | 0 | 4.24 | 6 | 0 |
| Angioblastic Meningioma [description not available] | 0 | 2.84 | 3 | 0 |
| Meningeal Neoplasms Benign and malignant neoplastic processes that arise from or secondarily involve the meningeal coverings of the brain and spinal cord. | 0 | 4.24 | 6 | 0 |
| Meningioma A relatively common neoplasm of the CENTRAL NERVOUS SYSTEM that arises from arachnoidal cells. The majority are well differentiated vascular tumors which grow slowly and have a low potential to be invasive, although malignant subtypes occur. Meningiomas have a predilection to arise from the parasagittal region, cerebral convexity, sphenoidal ridge, olfactory groove, and SPINAL CANAL. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2056-7) | 0 | 2.84 | 3 | 0 |
| 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 | 5.21 | 11 | 1 |
| Metastase [description not available] | 0 | 10.55 | 31 | 17 |
| Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site. | 0 | 10.55 | 31 | 17 |
| Ovarian Hyperstimulation Syndrome, Familial Gestational Spontaneous [description not available] | 0 | 14.25 | 57 | 15 |
| Ovarian Hyperstimulation Syndrome A complication of OVULATION INDUCTION in infertility treatment. It is graded by the severity of symptoms which include OVARY enlargement, multiple OVARIAN FOLLICLES; OVARIAN CYSTS; ASCITES; and generalized EDEMA. The full-blown syndrome may lead to RENAL FAILURE, respiratory distress, and even DEATH. Increased capillary permeability is caused by the vasoactive substances, such as VASCULAR ENDOTHELIAL GROWTH FACTORS, secreted by the overly-stimulated OVARIES. | 0 | 14.25 | 57 | 15 |
| Dysphagia [description not available] | 0 | 2.31 | 1 | 0 |
| Adult Spinal Muscular Atrophy [description not available] | 0 | 7.77 | 10 | 3 |
| Deglutition Disorders Difficulty in SWALLOWING which may result from neuromuscular disorder or mechanical obstruction. Dysphagia is classified into two distinct types: oropharyngeal dysphagia due to malfunction of the PHARYNX and UPPER ESOPHAGEAL SPHINCTER; and esophageal dysphagia due to malfunction of the ESOPHAGUS. | 0 | 2.31 | 1 | 0 |
| Muscular Atrophy, Spinal A group of disorders marked by progressive degeneration of motor neurons in the spinal cord resulting in weakness and muscular atrophy, usually without evidence of injury to the corticospinal tracts. Diseases in this category include Werdnig-Hoffmann disease and later onset SPINAL MUSCULAR ATROPHIES OF CHILDHOOD, most of which are hereditary. (Adams et al., Principles of Neurology, 6th ed, p1089) | 0 | 7.77 | 10 | 3 |
| Cerebral Gigantism [description not available] | 0 | 2.41 | 1 | 0 |
| 2019 Novel Coronavirus Disease [description not available] | 0 | 4.62 | 1 | 1 |
| Acute Confusional Senile Dementia [description not available] | 0 | 8.47 | 10 | 2 |
| 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 | 8.47 | 10 | 2 |
| Psychoses [description not available] | 0 | 2.72 | 3 | 0 |
| Dementia Praecox [description not available] | 0 | 3.35 | 2 | 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 | 2.72 | 3 | 0 |
| Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior. | 0 | 8.35 | 2 | 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 | 8.78 | 8 | 4 |
| Kidney Failure A severe irreversible decline in the ability of kidneys to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. | 0 | 2.44 | 2 | 0 |
| Renal Insufficiency Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE. | 0 | 2.44 | 2 | 0 |
| Ovarian Diseases Pathological processes of the OVARY. | 0 | 8.32 | 20 | 4 |
| Lower Urinary Tract Symptom [description not available] | 0 | 8.5 | 2 | 0 |
| Bone Cancer [description not available] | 0 | 11.09 | 35 | 9 |
| Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES. | 0 | 11.09 | 35 | 9 |
| Congenital Adrenal Hyperplasia [description not available] | 0 | 11.54 | 12 | 0 |
| Blood Pressure, High [description not available] | 0 | 3.14 | 5 | 0 |
| 46, XX Disorders of Sex Development Congenital conditions in individuals with a female karyotype, in which the development of the gonadal or anatomical sex is atypical. | 0 | 2.15 | 1 | 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 | 6.54 | 12 | 0 |
| 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 | 3.14 | 5 | 0 |
| Left Ventricular Dysfunction [description not available] | 0 | 2.15 | 1 | 0 |
| Ventricular Dysfunction, Left A condition in which the LEFT VENTRICLE of the heart was functionally impaired. This condition usually leads to HEART FAILURE; MYOCARDIAL INFARCTION; and other cardiovascular complications. Diagnosis is made by measuring the diminished ejection fraction and a depressed level of motility of the left ventricular wall. | 0 | 2.15 | 1 | 0 |
| Pneumothorax, Primary Spontaneous [description not available] | 0 | 5.59 | 12 | 0 |
| Pneumothorax An accumulation of air or gas in the PLEURAL CAVITY, which may occur spontaneously or as a result of trauma or a pathological process. The gas may also be introduced deliberately during PNEUMOTHORAX, ARTIFICIAL. | 0 | 10.59 | 12 | 0 |
| Bilateral Headache [description not available] | 0 | 4.49 | 5 | 1 |
| Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS. | 0 | 4.49 | 5 | 1 |
| Dyspareunia Recurrent genital pain occurring during, before, or after SEXUAL INTERCOURSE in either the male or the female. | 0 | 6.76 | 6 | 4 |
| Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma. | 0 | 2.15 | 1 | 0 |
| Pneumonia Infection of the lung often accompanied by inflammation. | 0 | 2.15 | 1 | 0 |
| Granulomas [description not available] | 0 | 5.67 | 18 | 0 |
| Dermatoses [description not available] | 0 | 4.91 | 8 | 0 |
| Granuloma A relatively small nodular inflammatory lesion containing grouped mononuclear phagocytes, caused by infectious and noninfectious agents. | 0 | 5.67 | 18 | 0 |
| Skin Diseases Diseases involving the DERMIS or EPIDERMIS. | 0 | 4.91 | 8 | 0 |
| Arrhythmia [description not available] | 0 | 2.15 | 1 | 0 |
| Cardiac Failure [description not available] | 0 | 2.15 | 1 | 0 |
| Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction. | 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 | 2.15 | 1 | 0 |
| Complication, Postoperative [description not available] | 0 | 9.54 | 28 | 4 |
| Anorectal Diseases [description not available] | 0 | 4.76 | 4 | 0 |
| Intestinal Diseases Pathological processes in any segment of the INTESTINE from DUODENUM to RECTUM. | 0 | 4.31 | 2 | 0 |
| 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 | 9.54 | 28 | 4 |
| Rectal Diseases Pathological developments in the RECTUM region of the large intestine (INTESTINE, LARGE). | 0 | 4.76 | 4 | 0 |
| Aneuploid [description not available] | 0 | 2.77 | 3 | 0 |
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 7.27 | 8 | 3 |
| Genetic Skin Diseases [description not available] | 0 | 2.17 | 1 | 0 |
| Collagen Diseases Historically, a heterogeneous group of acute and chronic diseases, including rheumatoid arthritis, systemic lupus erythematosus, progressive systemic sclerosis, dermatomyositis, etc. This classification was based on the notion that collagen was equivalent to connective tissue, but with the present recognition of the different types of collagen and the aggregates derived from them as distinct entities, the term collagen diseases now pertains exclusively to those inherited conditions in which the primary defect is at the gene level and affects collagen biosynthesis, post-translational modification, or extracellular processing directly. (From Cecil Textbook of Medicine, 19th ed, p1494) | 0 | 2.17 | 1 | 0 |
| Cranial Sinus Thrombosis [description not available] | 0 | 2.15 | 1 | 0 |
| Hot Flashes A sudden, temporary sensation of heat predominantly experienced by some women during MENOPAUSE. (Random House Unabridged Dictionary, 2d ed) | 0 | 17.43 | 107 | 96 |
| Coma A profound state of unconsciousness associated with depressed cerebral activity from which the individual cannot be aroused. Coma generally occurs when there is dysfunction or injury involving both cerebral hemispheres or the brain stem RETICULAR FORMATION. | 0 | 2.17 | 1 | 0 |
| Acute Edematous Pancreatitis [description not available] | 0 | 2.17 | 1 | 0 |
| Myxedema A condition characterized by a dry, waxy type of swelling (EDEMA) with abnormal deposits of MUCOPOLYSACCHARIDES in the SKIN and other tissues. It is caused by a deficiency of THYROID HORMONES. The skin becomes puffy around the eyes and on the cheeks. The face is dull and expressionless with thickened nose and lips. | 0 | 2.17 | 1 | 0 |
| Pancreatitis INFLAMMATION of the PANCREAS. Pancreatitis is classified as acute unless there are computed tomographic or endoscopic retrograde cholangiopancreatographic findings of CHRONIC PANCREATITIS (International Symposium on Acute Pancreatitis, Atlanta, 1992). The two most common forms of acute pancreatitis are ALCOHOLIC PANCREATITIS and gallstone pancreatitis. | 0 | 2.17 | 1 | 0 |
| Apoplexy [description not available] | 0 | 11.34 | 7 | 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 | 6.34 | 7 | 0 |
| Female Genital Neoplasms [description not available] | 0 | 6.72 | 8 | 3 |
| Genital Neoplasms, Female Tumor or cancer of the female reproductive tract (GENITALIA, FEMALE). | 0 | 6.72 | 8 | 3 |
| Reproductive Sterility [description not available] | 0 | 11.57 | 35 | 12 |
| Ectopic Pregnancy [description not available] | 0 | 2.43 | 2 | 0 |
| Infertility A reduced or absent capacity to reproduce. | 1 | 13.57 | 35 | 12 |
| Pregnancy, Ectopic A potentially life-threatening condition in which EMBRYO IMPLANTATION occurs outside the cavity of the UTERUS. Most ectopic pregnancies ( | 0 | 2.43 | 2 | 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 | 2.7 | 3 | 0 |
| 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 | 5.34 | 7 | 2 |
| Abortion, Tubal [description not available] | 0 | 8.69 | 15 | 3 |
| Aneurysm, Arteriovenous [description not available] | 0 | 2.21 | 1 | 0 |
| Arteriovenous Malformations Abnormal formation of blood vessels that shunt arterial blood directly into veins without passing through the CAPILLARIES. They usually are crooked, dilated, and with thick vessel walls. A common type is the congenital arteriovenous fistula. The lack of blood flow and oxygen in the capillaries can lead to tissue damage in the affected areas. | 0 | 2.77 | 3 | 0 |
| Hemorrhage, Uterine [description not available] | 0 | 9.17 | 25 | 8 |
| Abortion, Spontaneous Expulsion of the product of FERTILIZATION before completing the term of GESTATION and without deliberate interference. | 0 | 8.69 | 15 | 3 |
| Uterine Hemorrhage Bleeding from blood vessels in the UTERUS, sometimes manifested as vaginal bleeding. | 0 | 9.17 | 25 | 8 |
| Chronic Illness [description not available] | 0 | 7.09 | 12 | 3 |
| 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 | 7.09 | 12 | 3 |
| Depression, Endogenous [description not available] | 0 | 6.85 | 8 | 2 |
| 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 | 6.85 | 8 | 2 |
| Compensatory Hyperinsulinemia A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin. | 0 | 6.39 | 8 | 2 |
| Colicky Pain [description not available] | 0 | 4.12 | 3 | 1 |
| Benign Clear Cell Adenofibroma [description not available] | 0 | 2.21 | 1 | 0 |
| Hyperinsulinism A syndrome with excessively high INSULIN levels in the BLOOD. It may cause HYPOGLYCEMIA. Etiology of hyperinsulinism varies, including hypersecretion of a beta cell tumor (INSULINOMA); autoantibodies against insulin (INSULIN ANTIBODIES); defective insulin receptor (INSULIN RESISTANCE); or overuse of exogenous insulin or HYPOGLYCEMIC AGENTS. | 0 | 6.39 | 8 | 2 |
| Abdominal Pain Sensation of discomfort, distress, or agony in the abdominal region. | 0 | 9.12 | 3 | 1 |
| Minimal Disease, Residual [description not available] | 0 | 5.85 | 4 | 2 |
| Frigidity [description not available] | 0 | 6.75 | 4 | 2 |
| Sex Disorders [description not available] | 0 | 10.45 | 14 | 12 |
| Sexual Dysfunction, Physiological Physiological disturbances in normal sexual performance in either the male or the female. | 0 | 10.45 | 14 | 12 |
| 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 | 6.75 | 4 | 2 |
| Micrometastases, Neoplasm [description not available] | 0 | 4.51 | 1 | 1 |
| Cancer of the Urethra [description not available] | 0 | 2.21 | 1 | 0 |
| Urethral Neoplasms Cancer or tumors of the URETHRA. Benign epithelial tumors of the urethra usually consist of squamous and transitional cells. Primary urethral carcinomas are rare and typically of squamous cells. Urethral carcinoma is the only urological malignancy that is more common in females than in males. | 0 | 2.21 | 1 | 0 |
| Cerebrospinal Fluid Drainage [description not available] | 0 | 3.12 | 1 | 0 |
| Aesthesioneuroblastoma [description not available] | 0 | 3.12 | 1 | 0 |
| Cancer of Nose [description not available] | 0 | 3.12 | 1 | 0 |
| Esthesioneuroblastoma, Olfactory A malignant olfactory neuroblastoma arising from the olfactory epithelium of the superior nasal cavity and cribriform plate. It is uncommon (3% of nasal tumors) and rarely is associated with the production of excess hormones (e.g., SIADH, Cushing Syndrome). It has a high propensity for multiple local recurrences and bony metastases. (From Holland et al., Cancer Medicine, 3rd ed, p1245; J Laryngol Otol 1998 Jul;112(7):628-33) | 0 | 3.12 | 1 | 0 |
| Orphan Diseases Rare diseases that have not been well studied. | 0 | 2.74 | 3 | 0 |
| Chromosomal Translocation [description not available] | 0 | 2.46 | 2 | 0 |
| Facies The appearance of the face that is often characteristic of a disease or pathological condition, as the elfin facies of WILLIAMS SYNDROME or the mongoloid facies of DOWN SYNDROME. (Random House Unabridged Dictionary, 2d ed) | 0 | 2.21 | 1 | 0 |
| Central Diabetes Insipidus [description not available] | 0 | 2.21 | 1 | 0 |
| Failure to Thrive A condition of substandard growth or diminished capacity to maintain normal function. | 0 | 2.21 | 1 | 0 |
| Abnormality, Heart [description not available] | 0 | 2.21 | 1 | 0 |
| Absence Seizure [description not available] | 0 | 2.74 | 3 | 0 |
| Anhidrotic Ectodermal Dysplasia [description not available] | 0 | 2.21 | 1 | 0 |
| Heart Defects, Congenital Developmental abnormalities involving structures of the heart. These defects are present at birth but may be discovered later in life. | 0 | 2.21 | 1 | 0 |
| Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder. | 0 | 2.74 | 3 | 0 |
| Diabetes Insipidus, Neurogenic A genetic or acquired polyuric disorder caused by a deficiency of VASOPRESSINS secreted by the NEUROHYPOPHYSIS. Clinical signs include the excretion of large volumes of dilute URINE; HYPERNATREMIA; THIRST; and polydipsia. Etiologies include HEAD TRAUMA; surgeries and diseases involving the HYPOTHALAMUS and the PITUITARY GLAND. This disorder may also be caused by mutations of genes such as ARVP encoding vasopressin and its corresponding neurophysin (NEUROPHYSINS). | 0 | 2.21 | 1 | 0 |
| Infusion Site Adverse Event [description not available] | 0 | 2.25 | 1 | 0 |
| Foreign-Body Granuloma [description not available] | 0 | 2.78 | 3 | 0 |
| Cushing's Syndrome [description not available] | 0 | 9.32 | 4 | 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 | 9.37 | 23 | 6 |
| Hyperprolactinaemia [description not available] | 0 | 5.39 | 5 | 1 |
| Cushing Syndrome A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent. | 0 | 4.32 | 4 | 0 |
| Hyperprolactinemia Increased levels of PROLACTIN in the BLOOD, which may be associated with AMENORRHEA and GALACTORRHEA. Relatively common etiologies include PROLACTINOMA, medication effect, KIDNEY FAILURE, granulomatous diseases of the PITUITARY GLAND, and disorders which interfere with the hypothalamic inhibition of prolactin release. Ectopic (non-pituitary) production of prolactin may also occur. (From Joynt, Clinical Neurology, 1992, Ch36, pp77-8) | 0 | 10.39 | 5 | 1 |
| Thyroid Diseases Pathological processes involving the THYROID GLAND. | 0 | 3.64 | 3 | 0 |
| Atrophic Muscular Disorders [description not available] | 0 | 7.37 | 11 | 1 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 0 | 15.21 | 24 | 11 |
| Cancer of Rectum [description not available] | 0 | 2.41 | 2 | 0 |
| Cancer of the Vagina [description not available] | 0 | 2.48 | 2 | 0 |
| Rectal Neoplasms Tumors or cancer of the RECTUM. | 0 | 2.41 | 2 | 0 |
| Vaginal Neoplasms Tumors or cancer of the VAGINA. | 0 | 2.48 | 2 | 0 |
| Hormone-Dependent Neoplasms [description not available] | 0 | 12.04 | 42 | 12 |
| Leiomyomatosis The state of having multiple leiomyomas throughout the body. (Stedman, 25th ed) | 0 | 8.22 | 13 | 4 |
| Muscular Weakness [description not available] | 0 | 3.82 | 2 | 1 |
| Muscle Weakness A vague complaint of debility, fatigue, or exhaustion attributable to weakness of various muscles. The weakness can be characterized as subacute or chronic, often progressive, and is a manifestation of many muscle and neuromuscular diseases. (From Wyngaarden et al., Cecil Textbook of Medicine, 19th ed, p2251) | 0 | 3.82 | 2 | 1 |
| Hypergonadotropic Hypogonadism [description not available] | 0 | 20.95 | 94 | 72 |
| 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 | 17.95 | 94 | 72 |
| Polyps Discrete abnormal tissue masses that protrude into the lumen of the DIGESTIVE TRACT or the RESPIRATORY TRACT. Polyps can be spheroidal, hemispheroidal, or irregular mound-shaped structures attached to the MUCOUS MEMBRANE of the lumen wall either by a stalk, pedunculus, or by a broad base. | 0 | 2.08 | 1 | 0 |
| Leanness [description not available] | 0 | 5.91 | 5 | 1 |
| Dilatation, Pathologic The condition of an anatomical structure's being dilated beyond normal dimensions. | 0 | 2.08 | 1 | 0 |
| Retinal Pigment Epithelial Detachment [description not available] | 0 | 2.08 | 1 | 0 |
| Day Blindness [description not available] | 0 | 2.08 | 1 | 0 |
| Sclera Diseases [description not available] | 0 | 2.08 | 1 | 0 |
| Retinal Detachment Separation of the inner layers of the retina (neural retina) from the pigment epithelium. Retinal detachment occurs more commonly in men than in women, in eyes with degenerative myopia, in aging and in aphakia. It may occur after an uncomplicated cataract extraction, but it is seen more often if vitreous humor has been lost during surgery. (Dorland, 27th ed; Newell, Ophthalmology: Principles and Concepts, 7th ed, p310-12). | 0 | 2.08 | 1 | 0 |
| Avian Diseases [description not available] | 0 | 2.08 | 1 | 0 |
| Ascites Accumulation or retention of free fluid within the peritoneal cavity. | 0 | 3.26 | 6 | 0 |
| Overweight A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat. | 0 | 2.76 | 3 | 0 |
| Acute Lymphoid Leukemia [description not available] | 0 | 4.12 | 3 | 1 |
| Hamartoma A focal malformation resembling a neoplasm, composed of an overgrowth of mature cells and tissues that normally occur in the affected area. | 0 | 3.39 | 7 | 0 |
| Adolescent Coxa Vara [description not available] | 0 | 2.08 | 1 | 0 |
| Froehlich's Syndrome [description not available] | 0 | 3.38 | 7 | 0 |
| Precursor Cell Lymphoblastic Leukemia-Lymphoma A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias. | 0 | 4.12 | 3 | 1 |
| Peritoneal Diseases Pathological processes involving the PERITONEUM. | 0 | 4.81 | 7 | 1 |
| Lymphangiomyomatosis [description not available] | 0 | 9.05 | 5 | 0 |
| Lymphangioleiomyomatosis A disease characterized by the progressive invasion of SMOOTH MUSCLE CELLS into the LYMPHATIC VESSELS, and the BLOOD VESSELS. The majority of the cases occur in the LUNGS of women of child-bearing age, eventually blocking the flow of air, blood, and lymph. The common symptom is shortness of breath (DYSPNEA). | 0 | 4.05 | 5 | 0 |
| Diseases, Metabolic [description not available] | 0 | 4.4 | 1 | 1 |
| Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed) | 0 | 4.4 | 1 | 1 |
| Bleeding Between Periods [description not available] | 0 | 5.55 | 6 | 3 |
| Metrorrhagia Abnormal uterine bleeding that is not related to MENSTRUATION, usually in females without regular MENSTRUAL CYCLE. The irregular and unpredictable bleeding usually comes from a dysfunctional ENDOMETRIUM. | 0 | 5.55 | 6 | 3 |
| Cancer of Stomach [description not available] | 0 | 2.1 | 1 | 0 |
| Cancer, Second Primary [description not available] | 0 | 5.57 | 6 | 1 |
| Stomach Neoplasms Tumors or cancer of the STOMACH. | 0 | 2.1 | 1 | 0 |
| Long Sleeper Syndrome [description not available] | 0 | 3.89 | 2 | 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 | 3.89 | 2 | 0 |
| Androgen Insensitivity Syndrome [description not available] | 0 | 2.1 | 1 | 0 |
| Hypospadias A birth defect due to malformation of the URETHRA in which the urethral opening is below its normal location. In the male, the malformed urethra generally opens on the ventral surface of the PENIS or on the PERINEUM. In the female, the malformed urethral opening is in the VAGINA. | 0 | 2.1 | 1 | 0 |
| Cancer of Esophagus [description not available] | 0 | 2.08 | 1 | 0 |
| Alport Syndrome [description not available] | 0 | 2.08 | 1 | 0 |
| Esophageal Neoplasms Tumors or cancer of the ESOPHAGUS. | 0 | 2.08 | 1 | 0 |
| Nephritis, Hereditary A group of inherited conditions characterized initially by HEMATURIA and slowly progressing to RENAL INSUFFICIENCY. The most common form is the Alport syndrome (hereditary nephritis with HEARING LOSS) which is caused by mutations in genes for TYPE IV COLLAGEN and defective GLOMERULAR BASEMENT MEMBRANE. | 0 | 2.08 | 1 | 0 |
| Low Bone Density [description not available] | 0 | 5.42 | 5 | 1 |
| Bone Diseases, Metabolic Diseases that affect the METABOLIC PROCESSES of BONE TISSUE. | 0 | 5.42 | 5 | 1 |
| Multiple Primary Neoplasms [description not available] | 0 | 3.5 | 8 | 0 |
| Nociceptive Pain Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN. | 0 | 2.1 | 1 | 0 |
| Dermatitis Medicamentosa [description not available] | 0 | 6.31 | 8 | 1 |
| 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 | 5.01 | 9 | 1 |
| Cancer of Liver [description not available] | 0 | 4.51 | 5 | 1 |
| Cancer of Lung [description not available] | 0 | 4.55 | 9 | 0 |
| Liver Neoplasms Tumors or cancer of the LIVER. | 0 | 4.51 | 5 | 1 |
| Lung Neoplasms Tumors or cancer of the LUNG. | 0 | 4.55 | 9 | 0 |
| Coronary Heart Disease [description not available] | 0 | 2.11 | 1 | 0 |
| Coronary Disease An imbalance between myocardial functional requirements and the capacity of the CORONARY VESSELS to supply sufficient blood flow. It is a form of MYOCARDIAL ISCHEMIA (insufficient blood supply to the heart muscle) caused by a decreased capacity of the coronary vessels. | 0 | 2.11 | 1 | 0 |
| Corpus Luteum Cyst [description not available] | 0 | 6.44 | 16 | 3 |
| Ovarian Cysts General term for CYSTS and cystic diseases of the OVARY. | 0 | 6.44 | 16 | 3 |
| Pleural Effusion Presence of fluid in the pleural cavity resulting from excessive transudation or exudation from the pleural surfaces. It is a sign of disease and not a diagnosis in itself. | 0 | 2.7 | 3 | 0 |
| Bonnevie-Ullrich Syndrome This syndrome that was originally observed by Ullrich, and designated as identical to TURNER SYNDROME, related the webbing of the neck, loose skin and other anomalies of the syndrome to accumulation of fluid in the embryo starting at the head and dispersing to the extremities (as observed by Bonnevie in mice). Commonly observed at birth in Turner Syndrome and NOONAN SYNDROME; EDEMA of the extremities usually recedes by one year and is an early sign of Turner syndrome, especially in female neonates. | 0 | 3.03 | 1 | 0 |
| Turner Syndrome A syndrome of defective gonadal development in phenotypic females associated with the karyotype 45,X (or 45,XO). Patients generally are of short stature with undifferentiated GONADS (streak gonads), SEXUAL INFANTILISM, HYPOGONADISM, webbing of the neck, cubitus valgus, elevated GONADOTROPINS, decreased ESTRADIOL level in blood, and CONGENITAL HEART DEFECTS. NOONAN SYNDROME (also called Pseudo-Turner Syndrome and Male Turner Syndrome) resembles this disorder; however, it occurs in males and females with a normal karyotype and is inherited as an autosomal dominant. | 0 | 3.03 | 1 | 0 |
| Atherogenesis [description not available] | 0 | 2.52 | 2 | 0 |
| Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA. | 0 | 2.52 | 2 | 0 |
| Behavior Disorders [description not available] | 0 | 3.84 | 2 | 1 |
| Mental Disorders Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function. | 0 | 3.84 | 2 | 1 |
| Lassitude [description not available] | 0 | 4.77 | 2 | 1 |
| Petechiae Pinhead size (3 mm) skin discolorization due to hemorrhage. | 0 | 2.1 | 1 | 0 |
| Congenital Thrombotic Thrombocytopenic Purpura [description not available] | 0 | 2.1 | 1 | 0 |
| Fatigue The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli. | 0 | 4.77 | 2 | 1 |
| Purpura Purplish or brownish red discoloration, easily visible through the epidermis, caused by hemorrhage into the tissues. When the size of the discolorization is | 0 | 2.1 | 1 | 0 |
| Purpura, Thrombotic Thrombocytopenic An acquired, congenital, or familial disorder caused by PLATELET AGGREGATION with THROMBOSIS in terminal arterioles and capillaries. Clinical features include THROMBOCYTOPENIA; HEMOLYTIC ANEMIA; AZOTEMIA; FEVER; and thrombotic microangiopathy. The classical form also includes neurological symptoms and end-organ damage, such as RENAL FAILURE. Mutations in the ADAMTS13 PROTEIN gene have been identified in familial cases. | 0 | 2.1 | 1 | 0 |
| Bowel Incontinence [description not available] | 0 | 3.5 | 1 | 1 |
| Impotence [description not available] | 0 | 8.54 | 9 | 6 |
| Fecal Incontinence Failure of voluntary control of the anal sphincters, with involuntary passage of feces and flatus. | 0 | 3.5 | 1 | 1 |
| Erectile Dysfunction The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction. | 0 | 8.54 | 9 | 6 |
| Innate Inflammatory Response [description not available] | 0 | 2.94 | 4 | 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 | 2.94 | 4 | 0 |
| Adenoma, Basal Cell [description not available] | 0 | 4.8 | 12 | 0 |
| Adenoma A benign epithelial tumor with a glandular organization. | 0 | 4.8 | 12 | 0 |
| Lymph Node Metastasis [description not available] | 0 | 9.01 | 20 | 6 |
| Carcinoma, Neuroendocrine A group of carcinomas which share a characteristic morphology, often being composed of clusters and trabecular sheets of round blue cells, granular chromatin, and an attenuated rim of poorly demarcated cytoplasm. Neuroendocrine tumors include carcinoids, small (oat) cell carcinomas, medullary carcinoma of the thyroid, Merkel cell tumor, cutaneous neuroendocrine carcinoma, pancreatic islet cell tumors, and pheochromocytoma. Neurosecretory granules are found within the tumor cells. (Segen, Dictionary of Modern Medicine, 1992) | 0 | 3.01 | 1 | 0 |
| Carcinoma, Large Cell A tumor of undifferentiated (anaplastic) cells of large size. It is usually bronchogenic. (From Dorland, 27th ed) | 0 | 3.01 | 1 | 0 |
| Autoimmune Disease [description not available] | 0 | 2.53 | 2 | 0 |
| Autoimmune Diseases Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides. | 0 | 2.53 | 2 | 0 |
| Dermatitis Any inflammation of the skin. | 0 | 7.77 | 3 | 0 |
| Anaphylactic Reaction [description not available] | 0 | 4.92 | 8 | 0 |
| Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death. | 0 | 4.92 | 8 | 0 |
| Neoplasms, Vascular [description not available] | 0 | 2.44 | 2 | 0 |
| Superior Vena Cava Obstruction [description not available] | 0 | 2.49 | 2 | 0 |
| Autism [description not available] | 0 | 5.43 | 5 | 1 |
| Autistic Disorder A disorder beginning in childhood. It is marked by the presence of markedly abnormal or impaired development in social interaction and communication and a markedly restricted repertoire of activity and interest. Manifestations of the disorder vary greatly depending on the developmental level and chronological age of the individual. (DSM-V) | 0 | 5.43 | 5 | 1 |
| Cardiovascular Stroke [description not available] | 0 | 3.11 | 5 | 0 |
| Myocardial Infarction NECROSIS of the MYOCARDIUM caused by an obstruction of the blood supply to the heart (CORONARY CIRCULATION). | 0 | 3.11 | 5 | 0 |
| Anaplastic Ependymoma [description not available] | 0 | 3.03 | 1 | 0 |
| Ependymoma Glioma derived from EPENDYMOGLIAL CELLS that tend to present as malignant intracranial tumors in children and as benign intraspinal neoplasms in adults. It may arise from any level of the ventricular system or central canal of the spinal cord. Intracranial ependymomas most frequently originate in the FOURTH VENTRICLE and histologically are densely cellular tumors which may contain ependymal tubules and perivascular pseudorosettes. Spinal ependymomas are usually benign papillary or myxopapillary tumors. (From DeVita et al., Principles and Practice of Oncology, 5th ed, p2018; Escourolle et al., Manual of Basic Neuropathology, 2nd ed, pp28-9) | 0 | 3.03 | 1 | 0 |
| Experimental Radiation Injuries [description not available] | 0 | 2.11 | 1 | 0 |
| Hypomenorrhea [description not available] | 0 | 4.88 | 8 | 1 |
| Nasopharyngeal Carcinoma A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes. | 0 | 2.11 | 1 | 0 |
| Cancer of Nasopharynx [description not available] | 0 | 2.11 | 1 | 0 |
| Nasopharyngeal Neoplasms Tumors or cancer of the NASOPHARYNX. | 0 | 2.11 | 1 | 0 |
| Fallopian Tube Diseases Diseases involving the FALLOPIAN TUBES including neoplasms (FALLOPIAN TUBE NEOPLASMS); SALPINGITIS; tubo-ovarian abscess; and blockage. | 0 | 4.49 | 5 | 1 |
| Beuren Syndrome [description not available] | 0 | 2.11 | 1 | 0 |
| Adenoma, Prostatic [description not available] | 0 | 10.15 | 24 | 9 |
| 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. | 0 | 10.15 | 24 | 9 |
| Pain, Chronic [description not available] | 0 | 2.78 | 3 | 0 |
| Chronic Pain Aching sensation that persists for more than a few months. It may or may not be associated with trauma or disease, and may persist after the initial injury has healed. Its localization, character, and timing are more vague than with acute pain. | 0 | 2.78 | 3 | 0 |
| Stunted Growth [description not available] | 0 | 8.24 | 15 | 8 |
| Growth Disorders Deviations from the average values for a specific age and sex in any or all of the following: height, weight, skeletal proportions, osseous development, or maturation of features. Included here are both acceleration and retardation of growth. | 0 | 8.24 | 15 | 8 |
| Infant, Small for Gestational Age An infant having a birth weight lower than expected for its gestational age. | 0 | 6.01 | 7 | 4 |
| Cancer of Endometrium [description not available] | 0 | 9.76 | 21 | 3 |
| Endometrial Neoplasms Tumors or cancer of ENDOMETRIUM, the mucous lining of the UTERUS. These neoplasms can be benign or malignant. Their classification and grading are based on the various cell types and the percent of undifferentiated cells. | 0 | 9.76 | 21 | 3 |
| Psychoses, Drug [description not available] | 0 | 3.38 | 2 | 0 |
| Pederasty [description not available] | 0 | 8.97 | 11 | 3 |
| Allergic Encephalomyelitis [description not available] | 0 | 2.5 | 2 | 0 |
| Infectious Myelitis [description not available] | 0 | 2.13 | 1 | 0 |
| Cholangiitis, Sclerosing [description not available] | 0 | 2.11 | 1 | 0 |
| Cholangitis, Sclerosing Chronic inflammatory disease of the BILIARY TRACT. It is characterized by fibrosis and hardening of the intrahepatic and extrahepatic biliary ductal systems leading to bile duct strictures, CHOLESTASIS, and eventual BILIARY CIRRHOSIS. | 0 | 2.11 | 1 | 0 |
| Bone Loss, Osteoclastic [description not available] | 0 | 8.16 | 14 | 8 |
| 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 |
| Monkey Diseases Diseases of Old World and New World monkeys. This term includes diseases of baboons but not of chimpanzees or gorillas (= APE DISEASES). | 0 | 2.92 | 4 | 0 |
| Hemisensory Neglect [description not available] | 0 | 2.13 | 1 | 0 |
| Perceptual Disorders Cognitive disorders characterized by an impaired ability to perceive the nature of objects or concepts through use of the sense organs. These include spatial neglect syndromes, where an individual does not attend to visual, auditory, or sensory stimuli presented from one side of the body. | 0 | 2.13 | 1 | 0 |
| Carcinoma, Ductal, Breast An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST. | 0 | 2.99 | 4 | 0 |
| Carcinoma, Lobular A type of BREAST CANCER where the abnormal malignant cells form in the lobules, or milk-producing glands, of the breast. | 0 | 2.13 | 1 | 0 |
| Endomyometritis Inflammation of both the ENDOMETRIUM and the MYOMETRIUM, usually caused by infections after a CESAREAN SECTION. | 0 | 2.13 | 1 | 0 |
| Endometritis Inflammation of the ENDOMETRIUM, usually caused by intrauterine infections. Endometritis is the most common cause of postpartum fever. | 0 | 2.13 | 1 | 0 |
| Elevated Cholesterol [description not available] | 0 | 2.13 | 1 | 0 |
| Aortic Diseases Pathological processes involving any part of the AORTA. | 0 | 2.13 | 1 | 0 |
| Hypercholesterolemia A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population. | 0 | 2.13 | 1 | 0 |
| Chronic Insomnia [description not available] | 0 | 5.61 | 3 | 2 |
| Sleep Initiation and Maintenance Disorders Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition. | 0 | 5.61 | 3 | 2 |
| Benign Neoplasms, Brain [description not available] | 0 | 2.13 | 1 | 0 |
| Atypical Ductal Hyperplasia [description not available] | 0 | 2.13 | 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 | 2.13 | 1 | 0 |
| Carcinoma, Intraductal, Noninfiltrating A noninvasive (noninfiltrating) carcinoma of the breast characterized by a proliferation of malignant epithelial cells confined to the mammary ducts or lobules, without light-microscopy evidence of invasion through the basement membrane into the surrounding stroma. | 0 | 2.13 | 1 | 0 |
| Ambulation Disorders, Neurologic [description not available] | 0 | 2.13 | 1 | 0 |
| Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment. | 0 | 8.13 | 8 | 3 |
| Atheroma [description not available] | 0 | 2.13 | 1 | 0 |
| Anterior Horn Cell Disease [description not available] | 0 | 3.04 | 1 | 0 |
| Motor Neuron Disease Diseases characterized by a selective degeneration of the motor neurons of the spinal cord, brainstem, or motor cortex. Clinical subtypes are distinguished by the major site of degeneration. In AMYOTROPHIC LATERAL SCLEROSIS there is involvement of upper, lower, and brainstem motor neurons. In progressive muscular atrophy and related syndromes (see MUSCULAR ATROPHY, SPINAL) the motor neurons in the spinal cord are primarily affected. With progressive bulbar palsy (BULBAR PALSY, PROGRESSIVE), the initial degeneration occurs in the brainstem. In primary lateral sclerosis, the cortical neurons are affected in isolation. (Adams et al., Principles of Neurology, 6th ed, p1089) | 0 | 3.04 | 1 | 0 |
| Epithelial Ovarian Cancer [description not available] | 0 | 3.04 | 1 | 0 |
| Epithelial Neoplasms [description not available] | 0 | 3.36 | 2 | 0 |
| Carcinoma, Ovarian Epithelial A malignant neoplasm that originates in cells on the surface EPITHELIUM of the ovary and is the most common form of ovarian cancer. There are five histologic subtypes: papillary serous, endometrioid, mucinous, clear cell, and transitional cell. Mutations in BRCA1, OPCML, PRKN, PIK3CA, AKT1, CTNNB1, RRAS2, and CDH1 genes are associated with this cancer. | 0 | 3.04 | 1 | 0 |
| Tumour Lysis Syndrome [description not available] | 0 | 2.47 | 2 | 0 |
| Tumor Lysis Syndrome A syndrome resulting from cytotoxic therapy, occurring generally in aggressive, rapidly proliferating lymphoproliferative disorders. It is characterized by combinations of hyperuricemia, lactic acidosis, hyperkalemia, hyperphosphatemia and hypocalcemia. | 0 | 2.47 | 2 | 0 |
| Sterility, Male [description not available] | 0 | 5.82 | 12 | 2 |
| Granulomatosis, Wegener's [description not available] | 0 | 2.13 | 1 | 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 | 5.82 | 12 | 2 |
| Granulomatosis with Polyangiitis A multisystemic disease of a complex genetic background. It is characterized by inflammation of the blood vessels (VASCULITIS) leading to damage in any number of organs. The common features include granulomatous inflammation of the RESPIRATORY TRACT and KIDNEYS. Most patients have measurable autoantibodies (ANTINEUTROPHIL CYTOPLASMIC ANTIBODIES) against MYELOBLASTIN. | 0 | 2.13 | 1 | 0 |
| Brain Hemorrhage, Cerebral [description not available] | 0 | 2.45 | 2 | 0 |
| Cerebral Hemorrhage Bleeding into one or both CEREBRAL HEMISPHERES including the BASAL GANGLIA and the CEREBRAL CORTEX. It is often associated with HYPERTENSION and CRANIOCEREBRAL TRAUMA. | 0 | 2.45 | 2 | 0 |
| Urinary Lithiasis [description not available] | 0 | 2.13 | 1 | 0 |
| Kidney Stones [description not available] | 0 | 2.13 | 1 | 0 |
| Ureteral Calculi Stones in the URETER that are formed in the KIDNEY. They are rarely more than 5 mm in diameter for larger renal stones cannot enter ureters. They are often lodged at the ureteral narrowing and can cause excruciating renal colic. | 0 | 2.13 | 1 | 0 |
| Kidney Calculi Stones in the KIDNEY, usually formed in the urine-collecting area of the kidney (KIDNEY PELVIS). Their sizes vary and most contains CALCIUM OXALATE. | 0 | 2.13 | 1 | 0 |
| Urolithiasis Formation of stones in any part of the URINARY TRACT, usually in the KIDNEY; URINARY BLADDER; or the URETER. | 0 | 2.13 | 1 | 0 |
| Central Hypothyroidism [description not available] | 0 | 2.73 | 3 | 0 |
| Itching [description not available] | 0 | 2.74 | 3 | 0 |
| Hypothyroidism A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction. | 0 | 7.73 | 3 | 0 |
| Pruritus An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief. | 0 | 2.74 | 3 | 0 |
| Lipodystrophy A collection of heterogenous conditions resulting from defective LIPID METABOLISM and characterized by ADIPOSE TISSUE atrophy. Often there is redistribution of body fat resulting in peripheral fat wasting and central adiposity. They include generalized, localized, congenital, and acquired lipodystrophy. | 0 | 2.13 | 1 | 0 |
| Androgenization [description not available] | 0 | 4.52 | 9 | 0 |
| Anovulation Suspension or cessation of OVULATION in animals or humans with follicle-containing ovaries (OVARIAN FOLLICLE). Depending on the etiology, OVULATION may be induced with appropriate therapy. | 0 | 5.08 | 10 | 1 |
| Peritoneal Carcinomatosis [description not available] | 0 | 2.42 | 2 | 0 |
| Peritoneal Neoplasms Tumors or cancer of the PERITONEUM. | 0 | 2.42 | 2 | 0 |
| Neoplasms, Cystic, Mucinous, and Serous Neoplasms containing cyst-like formations or producing mucin or serum. | 0 | 2.15 | 1 | 0 |
| Primary Peritonitis [description not available] | 0 | 3.65 | 3 | 0 |
| Sclerosis A pathological process consisting of hardening or fibrosis of an anatomical structure, often a vessel or a nerve. | 0 | 3.65 | 3 | 0 |
| Theca Cell Tumor [description not available] | 0 | 3.65 | 3 | 0 |
| Peritonitis INFLAMMATION of the PERITONEUM lining the ABDOMINAL CAVITY as the result of infectious, autoimmune, or chemical processes. Primary peritonitis is due to infection of the PERITONEAL CAVITY via hematogenous or lymphatic spread and without intra-abdominal source. Secondary peritonitis arises from the ABDOMINAL CAVITY itself through RUPTURE or ABSCESS of intra-abdominal organs. | 0 | 8.65 | 3 | 0 |
| Anemias, Iron-Deficiency [description not available] | 0 | 3.8 | 2 | 1 |
| Chronic Kidney Failure [description not available] | 0 | 2.71 | 3 | 0 |
| Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION. | 0 | 2.71 | 3 | 0 |
| Anemia, Iron-Deficiency Anemia characterized by decreased or absent iron stores, low serum iron concentration, low transferrin saturation, and low hemoglobin concentration or hematocrit value. The erythrocytes are hypochromic and microcytic and the iron binding capacity is increased. | 0 | 3.8 | 2 | 1 |
| Acute Hypercapnic Respiratory Failure [description not available] | 0 | 2.96 | 1 | 0 |
| Chylothorax The presence of chyle in the thoracic cavity. (Dorland, 27th ed) | 0 | 3.34 | 2 | 0 |
| Respiratory Insufficiency Failure to adequately provide oxygen to cells of the body and to remove excess carbon dioxide from them. (Stedman, 25th ed) | 0 | 2.96 | 1 | 0 |
| Endometrial Diseases [description not available] | 0 | 6.86 | 15 | 5 |
| Uterine Diseases Pathological processes involving any part of the UTERUS. | 0 | 6.86 | 15 | 5 |
| Cells, Neoplasm Circulating [description not available] | 0 | 2.44 | 2 | 0 |
| Neoplasms, Bone Marrow [description not available] | 0 | 2.46 | 2 | 0 |
| Bone Marrow Neoplasms Neoplasms located in the bone marrow. They are differentiated from neoplasms composed of bone marrow cells, such as MULTIPLE MYELOMA. Most bone marrow neoplasms are metastatic. | 0 | 2.46 | 2 | 0 |
| Spinal Neoplasms New abnormal growth of tissue in the SPINE. | 0 | 2.94 | 4 | 0 |
| Weight Gain Increase in BODY WEIGHT over existing weight. | 0 | 4.09 | 3 | 1 |
| Ambiguous Genitalia [description not available] | 0 | 3.43 | 1 | 1 |
| Disorders of Sex Development In gonochoristic organisms, congenital conditions in which development of chromosomal, gonadal, or anatomical sex is atypical. Effects from exposure to abnormal levels of GONADAL HORMONES in the maternal environment, or disruption of the function of those hormones by ENDOCRINE DISRUPTORS are included. | 0 | 3.43 | 1 | 1 |
| Graft-Versus-Host Disease [description not available] | 0 | 2.05 | 1 | 0 |
| Lymphocytopenia [description not available] | 0 | 2.05 | 1 | 0 |
| Graft vs Host Disease The clinical entity characterized by anorexia, diarrhea, loss of hair, leukopenia, thrombocytopenia, growth retardation, and eventual death brought about by the GRAFT VS HOST REACTION. | 0 | 2.05 | 1 | 0 |
| Lymphopenia Reduction in the number of lymphocytes. | 0 | 2.05 | 1 | 0 |
| Injuries, Radiation [description not available] | 0 | 6.13 | 6 | 2 |
| Affective Disorders [description not available] | 0 | 14.61 | 51 | 51 |
| Premenstrual Tension A term used to describe the psychological aspects of PREMENSTRUAL SYNDROME, such as the indescribable tension, depression, hostility, and increased seizure activity in women with seizure disorder. | 0 | 18.21 | 104 | 96 |
| Premenstrual Syndrome A combination of distressing physical, psychologic, or behavioral changes that occur during the luteal phase of the menstrual cycle. Symptoms of PMS are diverse (such as pain, water-retention, anxiety, cravings, and depression) and they diminish markedly 2 or 3 days after the initiation of menses. | 0 | 18.21 | 104 | 96 |
| Mood Disorders Those disorders that have a disturbance in mood as their predominant feature. | 0 | 14.61 | 51 | 51 |
| Shoulder Pain Unilateral or bilateral pain of the shoulder. It is often caused by physical activities such as work or sports participation, but may also be pathologic in origin. | 0 | 2.05 | 1 | 0 |
| Anochlesia [description not available] | 0 | 2.05 | 1 | 0 |
| Cancer of Skin [description not available] | 0 | 4.04 | 5 | 0 |
| Skin Neoplasms Tumors or cancer of the SKIN. | 0 | 4.04 | 5 | 0 |
| Hemangioma, Capillary A dull red, firm, dome-shaped hemangioma, sharply demarcated from surrounding skin, usually located on the head and neck, which grows rapidly and generally undergoes regression and involution without scarring. It is caused by proliferation of immature capillary vessels in active stroma, and is usually present at birth or occurs within the first two or three months of life. (Dorland, 27th ed) | 0 | 2.05 | 1 | 0 |
| Deep Vein Thrombosis [description not available] | 0 | 2.05 | 1 | 0 |
| Venous Thrombosis The formation or presence of a blood clot (THROMBUS) within a vein. | 0 | 2.05 | 1 | 0 |
| Dyslipidemia [description not available] | 0 | 3.38 | 2 | 0 |
| ALS - Amyotrophic Lateral Sclerosis [description not available] | 0 | 2.96 | 1 | 0 |
| Amyotrophic Lateral Sclerosis A degenerative disorder affecting upper MOTOR NEURONS in the brain and lower motor neurons in the brain stem and SPINAL CORD. Disease onset is usually after the age of 50 and the process is usually fatal within 3 to 6 years. Clinical manifestations include progressive weakness, atrophy, FASCICULATION, hyperreflexia, DYSARTHRIA, dysphagia, and eventual paralysis of respiratory function. Pathologic features include the replacement of motor neurons with fibrous ASTROCYTES and atrophy of anterior SPINAL NERVE ROOTS and corticospinal tracts. (From Adams et al., Principles of Neurology, 6th ed, pp1089-94) | 0 | 2.96 | 1 | 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 | 3.38 | 2 | 0 |
| Abnormalities, Sex Chromosome [description not available] | 0 | 2.05 | 1 | 0 |
| Amentia [description not available] | 0 | 4.01 | 5 | 0 |
| Menopause, Premature The premature cessation of menses (MENSTRUATION) when the last menstrual period occurs in a woman under the age of 40. It is due to the depletion of OVARIAN FOLLICLES. Premature MENOPAUSE can be caused by diseases; OVARIECTOMY; RADIATION; chemicals; and chromosomal abnormalities. | 0 | 3.32 | 2 | 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 | 9.01 | 5 | 0 |
| Degenerative Diseases, Central Nervous System [description not available] | 0 | 3.83 | 2 | 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 | 3.83 | 2 | 0 |
| Breast Cancer, Male [description not available] | 0 | 2.95 | 4 | 0 |
| Airflow Obstruction, Chronic [description not available] | 0 | 2.47 | 2 | 0 |
| Arteriosclerosis, Coronary [description not available] | 0 | 2.05 | 1 | 0 |
| Arthritis, Degenerative [description not available] | 0 | 2.05 | 1 | 0 |
| Carotid Artery Narrowing [description not available] | 0 | 2.05 | 1 | 0 |
| Coronary Artery Disease Pathological processes of CORONARY ARTERIES that may derive from a congenital abnormality, atherosclerotic, or non-atherosclerotic cause. | 0 | 2.05 | 1 | 0 |
| Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE. | 0 | 2.05 | 1 | 0 |
| Osteoarthritis A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans. | 0 | 2.05 | 1 | 0 |
| Carotid Stenosis Narrowing or stricture of any part of the CAROTID ARTERIES, most often due to atherosclerotic plaque formation. Ulcerations may form in atherosclerotic plaques and induce THROMBUS formation. Platelet or cholesterol emboli may arise from stenotic carotid lesions and induce a TRANSIENT ISCHEMIC ATTACK; CEREBROVASCULAR ACCIDENT; or temporary blindness (AMAUROSIS FUGAX). (From Adams et al., Principles of Neurology, 6th ed, pp 822-3) | 0 | 2.05 | 1 | 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 | 2.95 | 4 | 0 |
| Pulmonary Disease, Chronic Obstructive A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA. | 0 | 2.47 | 2 | 0 |
| Pericementitis [description not available] | 0 | 2.05 | 1 | 0 |
| Alveolar Bone Atrophy [description not available] | 0 | 2.46 | 2 | 0 |
| Mandibular Diseases Diseases involving the MANDIBLE. | 0 | 2.05 | 1 | 0 |
| Periodontitis Inflammation and loss of connective tissues supporting or surrounding the teeth. This may involve any part of the PERIODONTIUM. Periodontitis is currently classified by disease progression (CHRONIC PERIODONTITIS; AGGRESSIVE PERIODONTITIS) instead of age of onset. (From 1999 International Workshop for a Classification of Periodontal Diseases and Conditions, American Academy of Periodontology) | 0 | 2.05 | 1 | 0 |
| Periodontitis, Acute Nonsuppurative [description not available] | 0 | 2.05 | 1 | 0 |
| Exposure, Dental Pulp [description not available] | 0 | 2.05 | 1 | 0 |
| Dental Pulp Exposure The result of pathological changes in the hard tissue of a tooth caused by carious lesions, mechanical factors, or trauma, which render the pulp susceptible to bacterial invasion from the external environment. | 0 | 2.05 | 1 | 0 |
| Periapical Periodontitis Inflammation of the PERIAPICAL TISSUE. It includes general, unspecified, or acute nonsuppurative inflammation. Chronic nonsuppurative inflammation is PERIAPICAL GRANULOMA. Suppurative inflammation is PERIAPICAL ABSCESS. | 0 | 2.05 | 1 | 0 |
| Priapism A prolonged painful erection that may lasts hours and is not associated with sexual activity. It is seen in patients with SICKLE CELL ANEMIA, advanced malignancy, spinal trauma; and certain drug treatments. | 0 | 2.91 | 4 | 0 |
| Allergic Cutaneous Angiitis [description not available] | 0 | 2.45 | 2 | 0 |
| Coagulation, Disseminated Intravascular [description not available] | 0 | 4.03 | 5 | 0 |
| Hematuria Presence of blood in the urine. | 0 | 5.06 | 3 | 1 |
| Disseminated Intravascular Coagulation A disorder characterized by procoagulant substances entering the general circulation causing a systemic thrombotic process. The activation of the clotting mechanism may arise from any of a number of disorders. A majority of the patients manifest skin lesions, sometimes leading to PURPURA FULMINANS. | 0 | 4.03 | 5 | 0 |
| Ecchymosis Extravasation of blood into the skin, resulting in a nonelevated, rounded or irregular, blue or purplish patch, larger than a petechia. | 0 | 2.96 | 1 | 0 |
| Erythrocytosis [description not available] | 0 | 3.44 | 1 | 1 |
| Atrophy, Muscle [description not available] | 0 | 3.44 | 1 | 1 |
| Muscular Atrophy Derangement in size and number of muscle fibers occurring with aging, reduction in blood supply, or following immobilization, prolonged weightlessness, malnutrition, and particularly in denervation. | 0 | 3.44 | 1 | 1 |
| 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 | 4.37 | 2 | 2 |
| Delayed Effects, Prenatal Exposure [description not available] | 0 | 2.74 | 3 | 0 |
| Genetic Diseases, X-Chromosome Linked [description not available] | 0 | 2.06 | 1 | 0 |
| Adrenal Gland Hypofunction [description not available] | 0 | 2.06 | 1 | 0 |
| Addison Disease, X-Linked [description not available] | 0 | 2.06 | 1 | 0 |
| Hypoadrenocorticism, Familial Hereditary forms of Addison disease that may exhibit autosomal recessive or X-linked inheritance. They are characterized by severe neurological symptoms, APNEA; and death in infancy. OMIM: 240200 | 0 | 2.06 | 1 | 0 |
| Adrenal Insufficiency Conditions in which the production of adrenal CORTICOSTEROIDS falls below the requirement of the body. Adrenal insufficiency can be caused by defects in the ADRENAL GLANDS, the PITUITARY GLAND, or the HYPOTHALAMUS. | 0 | 2.06 | 1 | 0 |
| Affective Psychosis, Bipolar [description not available] | 0 | 2.42 | 2 | 0 |
| Bipolar Disorder A major affective disorder marked by severe mood swings (manic or major depressive episodes) and a tendency to remission and recurrence. | 0 | 2.42 | 2 | 0 |
| Abscess Accumulation of purulent material in tissues, organs, or circumscribed spaces, usually associated with signs of infection. | 0 | 2.74 | 3 | 0 |
| Alopecia Cicatrisata [description not available] | 0 | 2.44 | 2 | 0 |
| Diabetes Mellitus, Adult-Onset [description not available] | 0 | 2.06 | 1 | 0 |
| Alcoholic Cirrhosis [description not available] | 0 | 2.06 | 1 | 0 |
| Alopecia Absence of hair from areas where it is normally present. | 0 | 2.44 | 2 | 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 | 2.06 | 1 | 0 |
| Liver Cirrhosis, Alcoholic FIBROSIS of the hepatic parenchyma due to chronic excess ALCOHOL DRINKING. | 0 | 2.06 | 1 | 0 |
| Flushing A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress. | 0 | 4.65 | 3 | 2 |
| Hematospermia [description not available] | 0 | 3.45 | 1 | 1 |
| AIDS Seroconversion [description not available] | 0 | 2.06 | 1 | 0 |
| Orbital Neoplasms Neoplasms of the bony orbit and contents except the eyeball. | 0 | 2.06 | 1 | 0 |
| Interstitial Cell Tumor [description not available] | 0 | 2.06 | 1 | 0 |
| Cancer of Testis [description not available] | 0 | 2.92 | 4 | 0 |
| Testicular Neoplasms Tumors or cancer of the TESTIS. Germ cell tumors (GERMINOMA) of the testis constitute 95% of all testicular neoplasms. | 0 | 2.92 | 4 | 0 |
| Bone Fractures [description not available] | 0 | 5.59 | 6 | 1 |
| Fractures, Bone Breaks in bones. | 0 | 5.59 | 6 | 1 |
| Muscle Disorders [description not available] | 0 | 3.39 | 7 | 0 |
| Muscular Diseases Acquired, familial, and congenital disorders of SKELETAL MUSCLE and SMOOTH MUSCLE. | 0 | 3.39 | 7 | 0 |
| Central Nervous System Disease [description not available] | 0 | 3.33 | 2 | 0 |
| Central Nervous System Diseases Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord. | 0 | 3.33 | 2 | 0 |
| Albright Syndrome [description not available] | 0 | 3.85 | 4 | 0 |
| Fibrous Dysplasia, Polyostotic FIBROUS DYSPLASIA OF BONE affecting several bones. When melanotic pigmentation (CAFE-AU-LAIT SPOTS) and multiple endocrine hyperfunction are additionally associated it is referred to as Albright syndrome. | 0 | 3.85 | 4 | 0 |
| Centriacinar Emphysema [description not available] | 0 | 2.98 | 1 | 0 |
| alpha 1-Antitrypsin Deficiency Deficiency of the protease inhibitor ALPHA 1-ANTITRYPSIN that manifests primarily as PULMONARY EMPHYSEMA and LIVER CIRRHOSIS. | 0 | 2.98 | 1 | 0 |
| Adhesions, Tissue [description not available] | 0 | 6.94 | 15 | 2 |
| Birth Weight The mass or quantity of heaviness of an individual at BIRTH. It is expressed by units of pounds or kilograms. | 0 | 2.46 | 2 | 0 |
| Diabetes Mellitus, Gestational [description not available] | 0 | 2.07 | 1 | 0 |
| Diabetes, Gestational Diabetes mellitus induced by PREGNANCY but resolved at the end of pregnancy. It does not include previously diagnosed diabetics who become pregnant (PREGNANCY IN DIABETICS). Gestational diabetes usually develops in late pregnancy when insulin antagonistic hormones peaks leading to INSULIN RESISTANCE; GLUCOSE INTOLERANCE; and HYPERGLYCEMIA. | 0 | 2.07 | 1 | 0 |
| Adenocarcinoma, Endometrioid [description not available] | 0 | 2.48 | 2 | 0 |
| Carcinoma, Endometrioid An adenocarcinoma characterized by the presence of cells resembling the glandular cells of the ENDOMETRIUM. It is a common histological type of ovarian CARCINOMA and ENDOMETRIAL CARCINOMA. There is a high frequency of co-occurrence of this form of adenocarcinoma in both tissues. | 0 | 2.48 | 2 | 0 |
| Atypical Endometrial Hyperplasia A benign form of endometrial hyperplasia with increased number of cells with atypia. The atypical cells are large and irregular and have an increased nuclear/cytoplasmic ratio. The risk of progression to endometrial carcinoma rises with the increasing degree of cell atypia. | 0 | 5.41 | 5 | 3 |
| Endometrial Hyperplasia Benign proliferation of the ENDOMETRIUM in the UTERUS. Endometrial hyperplasia is classified by its cytology and glandular tissue. There are simple, complex (adenomatous without atypia), and atypical hyperplasia representing also the ascending risk of becoming malignant. | 0 | 5.41 | 5 | 3 |
| Female Genital Diseases [description not available] | 0 | 5.39 | 5 | 1 |
| Genital Diseases, Female Pathological processes involving the female reproductive tract (GENITALIA, FEMALE). | 0 | 5.39 | 5 | 1 |
| Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. | 0 | 4.72 | 2 | 1 |
| Dermatitis, Radiation-Induced [description not available] | 0 | 2.07 | 1 | 0 |
| Radiodermatitis A cutaneous inflammatory reaction occurring as a result of exposure to ionizing radiation. | 0 | 2.07 | 1 | 0 |
| Bladder Diseases [description not available] | 0 | 2.42 | 2 | 0 |
| Hypercoagulability [description not available] | 0 | 2.07 | 1 | 0 |
| Auricular Fibrillation [description not available] | 0 | 2.07 | 1 | 0 |
| Cerebral Ischemia [description not available] | 0 | 2.07 | 1 | 0 |
| Atrial Fibrillation Abnormal cardiac rhythm that is characterized by rapid, uncoordinated firing of electrical impulses in the upper chambers of the heart (HEART ATRIA). In such case, blood cannot be effectively pumped into the lower chambers of the heart (HEART VENTRICLES). It is caused by abnormal impulse generation. | 0 | 2.07 | 1 | 0 |
| Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION. | 0 | 2.07 | 1 | 0 |
| Urinary Retention Inability to empty the URINARY BLADDER with voiding (URINATION). | 0 | 2.42 | 2 | 0 |
| Thrombophilia A disorder of HEMOSTASIS in which there is a tendency for the occurrence of THROMBOSIS. | 0 | 2.07 | 1 | 0 |
| MS (Multiple Sclerosis) [description not available] | 0 | 2.07 | 1 | 0 |
| Multiple Sclerosis An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903) | 0 | 7.07 | 1 | 0 |
| Alopecia Mucinosa [description not available] | 0 | 2.99 | 1 | 0 |
| Mycosis Fungoides A chronic, malignant T-cell lymphoma of the skin. In the late stages, the LYMPH NODES and viscera are affected. | 0 | 2.99 | 1 | 0 |
| Allodynia [description not available] | 0 | 2.07 | 1 | 0 |
| Alkalosis A pathological condition that removes acid or adds base to the body fluids. | 0 | 2.07 | 1 | 0 |
| Hypokalemia Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed) | 0 | 2.07 | 1 | 0 |
| Leukocytosis A transient increase in the number of leukocytes in a body fluid. | 0 | 2.07 | 1 | 0 |
| Cancer of Mediastinum [description not available] | 0 | 2.07 | 1 | 0 |
| Mediastinal Neoplasms Tumors or cancer of the MEDIASTINUM. | 0 | 2.07 | 1 | 0 |
| Choroid Neoplasms Tumors of the choroid; most common intraocular tumors are malignant melanomas of the choroid. These usually occur after puberty and increase in incidence with advancing age. Most malignant melanomas of the uveal tract develop from benign melanomas (nevi). | 0 | 2.42 | 2 | 0 |
| Palmoplantaris Pustulosis [description not available] | 0 | 2.08 | 1 | 0 |
| Psoriasis A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis. | 0 | 2.08 | 1 | 0 |
| Androblastoma [description not available] | 0 | 2.08 | 1 | 0 |
| Antibody Deficiency Syndrome [description not available] | 0 | 4.95 | 4 | 0 |
| Immunologic Deficiency Syndromes Syndromes in which there is a deficiency or defect in the mechanisms of immunity, either cellular or humoral. | 0 | 4.95 | 4 | 0 |
| Abdominal Cryptorchidism [description not available] | 0 | 2.89 | 4 | 0 |
| Spider Veins [description not available] | 0 | 2.01 | 1 | 0 |
| Telangiectasis Permanent dilation of preexisting blood vessels (CAPILLARIES; ARTERIOLES; VENULES) creating small focal red lesions, most commonly in the skin or mucous membranes. It is characterized by the prominence of skin blood vessels, such as vascular spiders. | 0 | 2.01 | 1 | 0 |
| Adenohypophyseal Diseases [description not available] | 0 | 2.39 | 2 | 0 |
| Pituitary Diseases Disorders involving either the ADENOHYPOPHYSIS or the NEUROHYPOPHYSIS. These diseases usually manifest as hypersecretion or hyposecretion of PITUITARY HORMONES. Neoplastic pituitary masses can also cause compression of the OPTIC CHIASM and other adjacent structures. | 0 | 2.39 | 2 | 0 |
| Adrenal Gland Diseases Pathological processes of the ADRENAL GLANDS. | 0 | 2.01 | 1 | 0 |
| Cystadenoma A benign neoplasm derived from glandular epithelium, in which cystic accumulations of retained secretions are formed. In some instances, considerable portions of the neoplasm, or even the entire mass, may be cystic. (Stedman, 25th ed) | 0 | 2.01 | 1 | 0 |
| Condition, Preneoplastic [description not available] | 0 | 2.38 | 2 | 0 |
| Precancerous Conditions Pathological conditions that tend eventually to become malignant. | 0 | 2.38 | 2 | 0 |
| Drug Withdrawal Symptoms [description not available] | 0 | 16.01 | 54 | 49 |
| Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug. | 0 | 16.01 | 54 | 49 |
| Pleural Diseases Diseases involving the PLEURA. | 0 | 2.41 | 2 | 0 |
| HIV Coinfection [description not available] | 0 | 3.34 | 2 | 0 |
| HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS). | 1 | 5.34 | 2 | 0 |
| Signet Ring Cell Carcinoma [description not available] | 0 | 2.01 | 1 | 0 |
| Carcinoma, Signet Ring Cell A poorly differentiated adenocarcinoma in which the nucleus is pressed to one side by a cytoplasmic droplet of mucus. It usually arises in the gastrointestinal system. | 0 | 2.01 | 1 | 0 |
| Exhibitionism A disorder in which fantasies about or the act of exposing the genitals to an unsuspecting stranger produces sexual excitement with no attempt at further sexual activity with the stranger. | 0 | 8.32 | 2 | 0 |
| Cancer of Pelvis [description not available] | 0 | 5.9 | 9 | 3 |
| Canine Diseases [description not available] | 0 | 4.1 | 3 | 1 |
| Hypospermatogenesis [description not available] | 0 | 2.42 | 2 | 0 |
| Cancer, Embryonal [description not available] | 0 | 2.42 | 2 | 0 |
| Neoplasms, Germ Cell and Embryonal Neoplasms composed of primordial GERM CELLS of embryonic GONADS or of elements of the germ layers of the EMBRYO, MAMMALIAN. The concept does not refer to neoplasms located in the gonads or present in an embryo or FETUS. | 0 | 2.42 | 2 | 0 |
| Precordial Catch [description not available] | 0 | 2.01 | 1 | 0 |
| Chest Pain Pressure, burning, or numbness in the chest. | 0 | 2.01 | 1 | 0 |
| Cirrhosis [description not available] | 0 | 4.08 | 3 | 1 |
| Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury. | 0 | 9.08 | 3 | 1 |
| Autoimmune Thyroiditis [description not available] | 0 | 2.42 | 2 | 0 |
| Jaundice, Cholestatic [description not available] | 0 | 2.01 | 1 | 0 |
| Paraneoplastic Syndromes In patients with neoplastic diseases a wide variety of clinical pictures which are indirect and usually remote effects produced by tumor cell metabolites or other products. | 0 | 2.01 | 1 | 0 |
| Jaundice, Obstructive Jaundice, the condition with yellowish staining of the skin and mucous membranes, that is due to impaired BILE flow in the BILIARY TRACT, such as INTRAHEPATIC CHOLESTASIS, or EXTRAHEPATIC CHOLESTASIS. | 0 | 2.01 | 1 | 0 |
| Breathlessness [description not available] | 0 | 2.02 | 1 | 0 |
| Cough A sudden, audible expulsion of air from the lungs through a partially closed glottis, preceded by inhalation. It is a protective response that serves to clear the trachea, bronchi, and/or lungs of irritants and secretions, or to prevent aspiration of foreign materials into the lungs. | 0 | 2.02 | 1 | 0 |
| Dyspnea Difficult or labored breathing. | 0 | 2.02 | 1 | 0 |
| HIV Lipodystrophy Syndrome [description not available] | 0 | 2.02 | 1 | 0 |
| HIV-Associated Lipodystrophy Syndrome Defective metabolism leading to fat maldistribution in patients infected with HIV. The etiology appears to be multifactorial and probably involves some combination of infection-induced alterations in metabolism, direct effects of antiretroviral therapy, and patient-related factors. | 0 | 2.02 | 1 | 0 |
| Epiphyses, Slipped A complete or partial separation of the EPIPHYSES from the DIAPHYSES. | 0 | 2.02 | 1 | 0 |
| Colonic Polyps Discrete tissue masses that protrude into the lumen of the COLON. These POLYPS are connected to the wall of the colon either by a stalk, pedunculus, or by a broad base. | 0 | 2.02 | 1 | 0 |
| Carcinoma, Ehrlich Tumor A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms. | 0 | 2.02 | 1 | 0 |
| Anxiety Neuroses [description not available] | 0 | 3.79 | 2 | 1 |
| Anxiety Disorders Persistent and disabling ANXIETY. | 0 | 3.79 | 2 | 1 |
| Invasiveness, Neoplasm [description not available] | 0 | 6.28 | 8 | 1 |
| Adnexal Diseases Diseases of the uterine appendages (ADNEXA UTERI) including diseases involving the OVARY, the FALLOPIAN TUBES, and ligaments of the uterus (BROAD LIGAMENT; ROUND LIGAMENT). | 0 | 2.02 | 1 | 0 |
| Abnormality, Torsion [description not available] | 0 | 2.02 | 1 | 0 |
| Diplopia A visual symptom in which a single object is perceived by the visual cortex as two objects rather than one. Disorders associated with this condition include REFRACTIVE ERRORS; STRABISMUS; OCULOMOTOR NERVE DISEASES; TROCHLEAR NERVE DISEASES; ABDUCENS NERVE DISEASES; and diseases of the BRAIN STEM and OCCIPITAL LOBE. | 0 | 2.02 | 1 | 0 |
| Scoliosis An appreciable lateral deviation in the normally straight vertical line of the spine. (Dorland, 27th ed) | 0 | 2.01 | 1 | 0 |
| Bulbar Palsy [description not available] | 0 | 2.93 | 1 | 0 |
| Adrenal Cancer [description not available] | 0 | 2.02 | 1 | 0 |
| Testicular Diseases Pathological processes of the TESTIS. | 0 | 2.41 | 2 | 0 |
| Adrenocorticotropic Hormone, Inappropriate Secretion [description not available] | 0 | 2.02 | 1 | 0 |
| Adrenal Gland Hyperfunction [description not available] | 0 | 2.41 | 2 | 0 |
| Adrenocortical Hyperfunction Excess production of ADRENAL CORTEX HORMONES such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and/or ANDROSTENEDIONE. Hyperadrenal syndromes include CUSHING SYNDROME; HYPERALDOSTERONISM; and VIRILISM. | 0 | 2.41 | 2 | 0 |
| Pituitary ACTH Hypersecretion A disease of the PITUITARY GLAND characterized by the excess amount of ADRENOCORTICOTROPIC HORMONE secreted. This leads to hypersecretion of cortisol (HYDROCORTISONE) by the ADRENAL GLANDS resulting in CUSHING SYNDROME. | 0 | 2.02 | 1 | 0 |
| Duhring Disease [description not available] | 0 | 2.72 | 3 | 0 |
| Dermatitis Herpetiformis Rare, chronic, papulo-vesicular disease characterized by an intensely pruritic eruption consisting of various combinations of symmetrical, erythematous, papular, vesicular, or bullous lesions. The disease is strongly associated with the presence of HLA-B8 and HLA-DR3 antigens. A variety of different autoantibodies has been detected in small numbers in patients with dermatitis herpetiformis. | 0 | 7.72 | 3 | 0 |
| Colitis, Mucous [description not available] | 0 | 3.41 | 1 | 1 |
| Irritable Bowel Syndrome A disorder with chronic or recurrent colonic symptoms without a clearcut etiology. This condition is characterized by chronic or recurrent ABDOMINAL PAIN, bloating, MUCUS in FECES, and an erratic disturbance of DEFECATION. | 0 | 8.41 | 1 | 1 |
| Carcinoma, Papillary A malignant neoplasm characterized by the formation of numerous, irregular, finger-like projections of fibrous stroma that is covered with a surface layer of neoplastic epithelial cells. (Stedman, 25th ed) | 0 | 2.02 | 1 | 0 |
| Autoimmune Diabetes [description not available] | 0 | 2.9 | 4 | 0 |
| Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence. | 0 | 2.9 | 4 | 0 |
| Coagulation Disorders, Blood [description not available] | 0 | 2.02 | 1 | 0 |
| Blood Coagulation Disorders Hemorrhagic and thrombotic disorders that occur as a consequence of abnormalities in blood coagulation due to a variety of factors such as COAGULATION PROTEIN DISORDERS; BLOOD PLATELET DISORDERS; BLOOD PROTEIN DISORDERS or nutritional conditions. | 0 | 2.02 | 1 | 0 |
| Cholera Infantum [description not available] | 0 | 2.41 | 2 | 0 |
| Male Genitourinary Diseases [description not available] | 0 | 2.02 | 1 | 0 |
| Intestinal Polyps Discrete abnormal tissue masses that protrude into the lumen of the INTESTINE. A polyp is attached to the intestinal wall either by a stalk, pedunculus, or by a broad base. | 0 | 2.03 | 1 | 0 |
| Aplasia Pure Red Cell [description not available] | 0 | 2.41 | 2 | 0 |
| Red-Cell Aplasia, Pure Suppression of erythropoiesis with little or no abnormality of leukocyte or platelet production. | 0 | 2.41 | 2 | 0 |
| Ureteral Obstruction Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy. | 0 | 7.9 | 4 | 0 |
| Ureteral Diseases Pathological processes involving the URETERS. | 0 | 2.02 | 1 | 0 |
| Fracture, Pathologic [description not available] | 0 | 2.42 | 2 | 0 |
| Apnea, Sleep [description not available] | 0 | 2.02 | 1 | 0 |
| Sleep Apnea Syndromes Disorders characterized by multiple cessations of respirations during sleep that induce partial arousals and interfere with the maintenance of sleep. Sleep apnea syndromes are divided into central (see SLEEP APNEA, CENTRAL), obstructive (see SLEEP APNEA, OBSTRUCTIVE), and mixed central-obstructive types. | 0 | 2.02 | 1 | 0 |
| Milk-Alkali Syndrome [description not available] | 0 | 2.03 | 1 | 0 |
| Hypercalcemia Abnormally high level of calcium in the blood. | 0 | 2.03 | 1 | 0 |
| Bone Demineralization, Pathologic Decrease, loss, or removal of the mineral constituents of bones. Temporary loss of bone mineral content is especially associated with space flight, weightlessness, and extended immobilization. OSTEOPOROSIS is permanent, includes reduction of total bone mass, and is associated with increased rate of fractures. CALCIFICATION, PHYSIOLOGIC is the process of bone remineralizing. (From Dorland, 27th ed; Stedman, 25th ed; Nicogossian, Space Physiology and Medicine, 2d ed, pp327-33) | 0 | 3.41 | 1 | 1 |
| Urinary Bladder Fistula An abnormal passage in the URINARY BLADDER or between the bladder and any surrounding organ. | 0 | 2.03 | 1 | 0 |
| Pruritus Vulvae Intense itching of the external female genitals. | 0 | 2.03 | 1 | 0 |
| Vaginal Diseases Pathological processes of the VAGINA. | 0 | 2.91 | 4 | 0 |
| Pus [description not available] | 0 | 2.4 | 2 | 0 |
| Jaw Diseases Diseases involving the JAW. | 0 | 2.94 | 1 | 0 |
| Aseptic Necrosis of Bone [description not available] | 0 | 2.94 | 1 | 0 |
| Osteonecrosis Death of a bone or part of a bone, either atraumatic or posttraumatic. | 0 | 2.94 | 1 | 0 |
| Experimental Mammary Neoplasms [description not available] | 0 | 4.28 | 7 | 0 |
| Inappropriate GH Secretion Syndrome (Acromegaly) [description not available] | 0 | 2.04 | 1 | 0 |
| Acromegaly A condition caused by prolonged exposure to excessive HUMAN GROWTH HORMONE in adults. It is characterized by bony enlargement of the FACE; lower jaw (PROGNATHISM); hands; FEET; HEAD; and THORAX. The most common etiology is a GROWTH HORMONE-SECRETING PITUITARY ADENOMA. (From Joynt, Clinical Neurology, 1992, Ch36, pp79-80) | 0 | 2.04 | 1 | 0 |
| Heavy Metal Poisoning, Nervous System Conditions associated with damage or dysfunction of the nervous system caused by exposure to heavy metals, which may cause a variety of central, peripheral, or autonomic nervous system injuries. | 0 | 2.03 | 1 | 0 |
| Anankastic Personality [description not available] | 0 | 2.03 | 1 | 0 |
| Obsessive-Compulsive Disorder An anxiety disorder characterized by recurrent, persistent obsessions or compulsions. Obsessions are the intrusive ideas, thoughts, or images that are experienced as senseless or repugnant. Compulsions are repetitive and seemingly purposeful behavior which the individual generally recognizes as senseless and from which the individual does not derive pleasure although it may provide a release from tension. | 0 | 2.03 | 1 | 0 |
| Hydrothorax A collection of watery fluid in the pleural cavity. (Dorland, 27th ed) | 0 | 7.03 | 1 | 0 |
| Acute Post-operative Pain [description not available] | 0 | 5 | 3 | 3 |
| Pain, Postoperative Pain during the period after surgery. | 0 | 5 | 3 | 3 |
| Hematologic Malignancies [description not available] | 0 | 3.33 | 2 | 0 |
| Hematologic Neoplasms Neoplasms located in the blood and blood-forming tissue (the bone marrow and lymphatic tissue). The commonest forms are the various types of LEUKEMIA, of LYMPHOMA, and of the progressive, life-threatening forms of the MYELODYSPLASTIC SYNDROMES. | 0 | 3.33 | 2 | 0 |
| Abdomen, Acute A clinical syndrome with acute abdominal pain that is severe, localized, and rapid in onset. Acute abdomen may be caused by a variety of disorders, injuries, or diseases. | 0 | 2.03 | 1 | 0 |
| Ileal Diseases Pathological development in the ILEUM including the ILEOCECAL VALVE. | 0 | 2.41 | 2 | 0 |
| Intestinal Perforation Opening or penetration through the wall of the INTESTINES. | 0 | 2.03 | 1 | 0 |
| Anterior Choroidal Artery Infarction [description not available] | 0 | 2.03 | 1 | 0 |
| Cerebral Infarction The formation of an area of NECROSIS in the CEREBRUM caused by an insufficiency of arterial or venous blood flow. Infarcts of the cerebrum are generally classified by hemisphere (i.e., left vs. right), lobe (e.g., frontal lobe infarction), arterial distribution (e.g., INFARCTION, ANTERIOR CEREBRAL ARTERY), and etiology (e.g., embolic infarction). | 0 | 2.03 | 1 | 0 |
| Fibroadenoma An adenoma containing fibrous tissue. It should be differentiated from ADENOFIBROMA which is a tumor composed of connective tissue (fibroma) containing glandular (adeno-) structures. (From Dorland, 27th ed) | 0 | 2.03 | 1 | 0 |
| Fibromatosis [description not available] | 0 | 2.03 | 1 | 0 |
| Fibroma A benign tumor of fibrous or fully developed connective tissue. | 0 | 2.03 | 1 | 0 |
| Leucocythaemia [description not available] | 0 | 4.86 | 4 | 2 |
| Leukemia A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006) | 0 | 4.86 | 4 | 2 |
| Hematochezia The passage of bright red blood from the rectum. The blood may or may not be mixed with formed stool in the form of blood, blood clots, bloody stool or diarrhea. | 0 | 2.03 | 1 | 0 |
| Hereditary Hemorrhagic Telangiectasia [description not available] | 0 | 2.03 | 1 | 0 |
| Gastrointestinal Hemorrhage Bleeding in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM. | 0 | 2.03 | 1 | 0 |
| Telangiectasia, Hereditary Hemorrhagic An autosomal dominant vascular anomaly characterized by telangiectases of the skin and mucous membranes and by recurrent gastrointestinal bleeding. This disorder is caused by mutations of a gene (on chromosome 9q3) which encodes endoglin, a membrane glycoprotein that binds TRANSFORMING GROWTH FACTOR BETA. | 0 | 2.03 | 1 | 0 |
| Liver Steatosis [description not available] | 0 | 2.04 | 1 | 0 |
| Fatty Liver Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS. | 0 | 2.04 | 1 | 0 |
| Cutaneous Fistula An abnormal passage or communication leading from an internal organ to the surface of the body. | 0 | 2.04 | 1 | 0 |
| Alcohol Abuse [description not available] | 0 | 2.04 | 1 | 0 |
| Hyperactivity, Motor [description not available] | 0 | 2.04 | 1 | 0 |
| 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 | 2.04 | 1 | 0 |
| Infections, Listeria [description not available] | 0 | 2.04 | 1 | 0 |
| Lupus Erythematosus, Cutaneous, Subacute [description not available] | 0 | 2.04 | 1 | 0 |
| Lupus Erythematosus, Cutaneous A form of lupus erythematosus in which the skin may be the only organ involved or in which skin involvement precedes the spread into other body systems. It has been classified into three forms - acute (= LUPUS ERYTHEMATOSUS, SYSTEMIC with skin lesions), subacute, and chronic (= LUPUS ERYTHEMATOSUS, DISCOID). | 0 | 2.04 | 1 | 0 |
| Labhart-Willi Syndrome [description not available] | 0 | 1.96 | 1 | 0 |
| Prader-Willi Syndrome An autosomal dominant disorder caused by deletion of the proximal long arm of the paternal chromosome 15 (15q11-q13) or by inheritance of both of the pair of chromosomes 15 from the mother (UNIPARENTAL DISOMY) which are imprinted (GENETIC IMPRINTING) and hence silenced. Clinical manifestations include MENTAL RETARDATION; MUSCULAR HYPOTONIA; HYPERPHAGIA; OBESITY; short stature; HYPOGONADISM; STRABISMUS; and HYPERSOMNOLENCE. (Menkes, Textbook of Child Neurology, 5th ed, p229) | 0 | 1.96 | 1 | 0 |
| Thrombopenia [description not available] | 0 | 1.96 | 1 | 0 |
| Thrombocytopenia A subnormal level of BLOOD PLATELETS. | 0 | 1.96 | 1 | 0 |
| Benign Psychomotor Epilepsy, Childhood [description not available] | 0 | 1.98 | 1 | 0 |
| Epilepsy, Temporal Lobe A localization-related (focal) form of epilepsy characterized by recurrent seizures that arise from foci within the TEMPORAL LOBE, most commonly from its mesial aspect. A wide variety of psychic phenomena may be associated, including illusions, hallucinations, dyscognitive states, and affective experiences. The majority of complex partial seizures (see EPILEPSY, COMPLEX PARTIAL) originate from the temporal lobes. Temporal lobe seizures may be classified by etiology as cryptogenic, familial, or symptomatic. (From Adams et al., Principles of Neurology, 6th ed, p321). | 0 | 1.98 | 1 | 0 |
| Child Development Deviations [description not available] | 0 | 1.98 | 1 | 0 |
| Developmental Disabilities Disorders in which there is a delay in development based on that expected for a given age level or stage of development. These impairments or disabilities originate before age 18, may be expected to continue indefinitely, and constitute a substantial impairment. Biological and nonbiological factors are involved in these disorders. (From American Psychiatric Glossary, 6th ed) | 0 | 1.98 | 1 | 0 |
| Colonic Inertia Symptom characterized by the passage of stool once a week or less. | 0 | 1.98 | 1 | 0 |
| Constipation Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections. | 0 | 1.98 | 1 | 0 |
| Male Genital Neoplasms [description not available] | 0 | 1.98 | 1 | 0 |
| Genital Neoplasms, Male Tumor or cancer of the MALE GENITALIA. | 0 | 1.98 | 1 | 0 |
| Intestinal Obstruction Any impairment, arrest, or reversal of the normal flow of INTESTINAL CONTENTS toward the ANAL CANAL. | 0 | 1.98 | 1 | 0 |
| Constriction, Pathological [description not available] | 0 | 3.78 | 2 | 1 |
| Constriction, Pathologic The condition of an anatomical structure's being constricted beyond normal dimensions. | 0 | 3.78 | 2 | 1 |
| Kidney Diseases Pathological processes of the KIDNEY or its component tissues. | 0 | 1.98 | 1 | 0 |
| Cancer of Cervix [description not available] | 0 | 2.67 | 3 | 0 |
| Germinoblastoma [description not available] | 0 | 4.07 | 3 | 1 |
| Uterine Cervical Neoplasms Tumors or cancer of the UTERINE CERVIX. | 0 | 2.67 | 3 | 0 |
| Lymphoma A general term for various neoplastic diseases of the lymphoid tissue. | 0 | 9.07 | 3 | 1 |
| 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 | 2.39 | 2 | 0 |
| Cicatrix The fibrous tissue that replaces normal tissue during the process of WOUND HEALING. | 0 | 2.39 | 2 | 0 |
| Angor Pectoris [description not available] | 0 | 2.39 | 2 | 0 |
| Angina Pectoris The symptom of paroxysmal pain consequent to MYOCARDIAL ISCHEMIA usually of distinctive character, location and radiation. It is thought to be provoked by a transient stressful situation during which the oxygen requirements of the MYOCARDIUM exceed that supplied by the CORONARY CIRCULATION. | 0 | 7.39 | 2 | 0 |
| Peripheral Nerve Diseases [description not available] | 0 | 2.68 | 3 | 0 |
| Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves. | 0 | 2.68 | 3 | 0 |
| Colonic Diseases, Functional Chronic or recurrent colonic disorders without an identifiable structural or biochemical explanation. The widely recognized IRRITABLE BOWEL SYNDROME falls into this category. | 0 | 6.59 | 7 | 3 |
| Genetic Diseases [description not available] | 0 | 1.98 | 1 | 0 |
| Fetal Resorption The disintegration and assimilation of the dead FETUS in the UTERUS at any stage after the completion of organogenesis which, in humans, is after the 9th week of GESTATION. It does not include embryo resorption (see EMBRYO LOSS). | 0 | 1.98 | 1 | 0 |
| Genetic Diseases, Inborn Diseases that are caused by genetic mutations present during embryo or fetal development, although they may be observed later in life. The mutations may be inherited from a parent's genome or they may be acquired in utero. | 0 | 1.98 | 1 | 0 |
| Hyperparathyroidism A condition of abnormally elevated output of PARATHYROID HORMONE (or PTH) triggering responses that increase blood CALCIUM. It is characterized by HYPERCALCEMIA and BONE RESORPTION, eventually leading to bone diseases. PRIMARY HYPERPARATHYROIDISM is caused by parathyroid HYPERPLASIA or PARATHYROID NEOPLASMS. SECONDARY HYPERPARATHYROIDISM is increased PTH secretion in response to HYPOCALCEMIA, usually caused by chronic KIDNEY DISEASES. | 0 | 1.98 | 1 | 0 |
| Carcinoma, Epidermoid [description not available] | 0 | 3.78 | 2 | 1 |
| 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 | 2.38 | 2 | 0 |
| Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed) | 0 | 3.78 | 2 | 1 |
| Eye Disorders [description not available] | 0 | 1.98 | 1 | 0 |
| Eye Diseases Diseases affecting the eye. | 0 | 1.98 | 1 | 0 |
| Contact Dermatitis [description not available] | 0 | 1.98 | 1 | 0 |
| Dermatitis, Contact A type of acute or chronic skin reaction in which sensitivity is manifested by reactivity to materials or substances coming in contact with the skin. It may involve allergic or non-allergic mechanisms. | 0 | 1.98 | 1 | 0 |
| Akinetic-Rigid Variant of Huntington Disease [description not available] | 0 | 1.98 | 1 | 0 |
| Huntington Disease A familial disorder inherited as an autosomal dominant trait and characterized by the onset of progressive CHOREA and DEMENTIA in the fourth or fifth decade of life. Common initial manifestations include paranoia; poor impulse control; DEPRESSION; HALLUCINATIONS; and DELUSIONS. Eventually intellectual impairment; loss of fine motor control; ATHETOSIS; and diffuse chorea involving axial and limb musculature develops, leading to a vegetative state within 10-15 years of disease onset. The juvenile variant has a more fulminant course including SEIZURES; ATAXIA; dementia; and chorea. (From Adams et al., Principles of Neurology, 6th ed, pp1060-4) | 0 | 1.98 | 1 | 0 |
| Carcinoma, Intraepithelial [description not available] | 0 | 4.34 | 2 | 2 |
| Carcinoma in Situ A lesion with cytological characteristics associated with invasive carcinoma but the tumor cells are confined to the epithelium of origin, without invasion of the basement membrane. | 0 | 4.34 | 2 | 2 |
| Acute Kidney Failure [description not available] | 0 | 2.68 | 3 | 0 |
| Acute Kidney Injury Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions. | 0 | 2.68 | 3 | 0 |
| Idiopathic Parkinson Disease [description not available] | 0 | 1.98 | 1 | 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 | 1.98 | 1 | 0 |
| Pachymeningitis [description not available] | 0 | 1.98 | 1 | 0 |
| Meningitis Inflammation of the coverings of the brain and/or spinal cord, which consist of the PIA MATER; ARACHNOID; and DURA MATER. Infections (viral, bacterial, and fungal) are the most common causes of this condition, but subarachnoid hemorrhage (HEMORRHAGES, SUBARACHNOID), chemical irritation (chemical MENINGITIS), granulomatous conditions, neoplastic conditions (CARCINOMATOUS MENINGITIS), and other inflammatory conditions may produce this syndrome. (From Joynt, Clinical Neurology, 1994, Ch24, p6) | 0 | 1.98 | 1 | 0 |
| Acanthosis Nigricans A circumscribed melanosis consisting of a brown-pigmented, velvety verrucosity or fine papillomatosis appearing in the axillae and other body folds. It occurs in association with endocrine disorders, underlying malignancy, administration of certain drugs, or as in inherited disorder. | 0 | 2.38 | 2 | 0 |
| Leukocytopenia [description not available] | 0 | 1.98 | 1 | 0 |
| Leukopenia A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000). | 0 | 6.98 | 1 | 0 |
| Neoplasms, Pleural [description not available] | 0 | 2.38 | 2 | 0 |
| Pleural Effusion, Malignant Presence of fluid in the PLEURAL CAVITY as a complication of malignant disease. Malignant pleural effusions often contain actual malignant cells. | 0 | 1.98 | 1 | 0 |
| Auditory Vertigo [description not available] | 0 | 1.98 | 1 | 0 |
| Meniere Disease A disease of the inner ear (LABYRINTH) that is characterized by fluctuating SENSORINEURAL HEARING LOSS; TINNITUS; episodic VERTIGO; and aural fullness. It is the most common form of endolymphatic hydrops. | 0 | 1.98 | 1 | 0 |
| Carcinoma, Colloid [description not available] | 0 | 2.9 | 1 | 0 |
| Adenocarcinoma, Mucinous An adenocarcinoma producing mucin in significant amounts. (From Dorland, 27th ed) | 0 | 2.9 | 1 | 0 |
| Benign Hypothalamic Neoplasms [description not available] | 0 | 2.38 | 2 | 0 |
| HbS Disease [description not available] | 0 | 2.39 | 2 | 0 |
| Anemia, Sickle Cell A disease characterized by chronic hemolytic anemia, episodic painful crises, and pathologic involvement of many organs. It is the clinical expression of homozygosity for hemoglobin S. | 0 | 2.39 | 2 | 0 |
| Antidiuretic Hormone, Inappropriate Secretion [description not available] | 0 | 3.78 | 2 | 0 |
| Inappropriate ADH Syndrome A condition of HYPONATREMIA and renal salt loss attributed to overexpansion of BODY FLUIDS resulting from sustained release of ANTIDIURETIC HORMONES which stimulates renal resorption of water. It is characterized by normal KIDNEY function, high urine OSMOLALITY, low serum osmolality, and neurological dysfunction. Etiologies include ADH-producing neoplasms, injuries or diseases involving the HYPOTHALAMUS, the PITUITARY GLAND, and the LUNG. This syndrome can also be drug-induced. | 0 | 3.78 | 2 | 0 |
| Atypical Cluster Headache [description not available] | 0 | 3.77 | 2 | 1 |
| Bone Loss, Perimenopausal [description not available] | 0 | 4.63 | 3 | 2 |
| 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 | 4.63 | 3 | 2 |
| Abortion, Missed The retention in the UTERUS of a dead FETUS two months or more after its DEATH. | 0 | 2.9 | 1 | 0 |
| Age-Related Memory Disorders [description not available] | 0 | 5.54 | 3 | 2 |
| Memory Disorders Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions. | 0 | 5.54 | 3 | 2 |
| Bleeding [description not available] | 0 | 4.84 | 4 | 2 |
| Hemorrhage Bleeding or escape of blood from a vessel. | 0 | 4.84 | 4 | 2 |
| Sarcoma, Epithelioid [description not available] | 0 | 3.6 | 3 | 0 |
| Adenofibroma A benign neoplasm composed of glandular and fibrous tissues, with a relatively large proportion of glands. (Stedman, 25th ed) | 0 | 2.9 | 1 | 0 |
| Sarcoma A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant. | 0 | 8.6 | 3 | 0 |
| Gestational Luteoma [description not available] | 0 | 1.98 | 1 | 0 |
| Bladder Cancer [description not available] | 0 | 2.9 | 4 | 0 |
| Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER. | 0 | 2.9 | 4 | 0 |
| Lymphatic Diseases Diseases of LYMPH; LYMPH NODES; or LYMPHATIC VESSELS. | 0 | 1.99 | 1 | 0 |
| Xanthoma [description not available] | 0 | 1.99 | 1 | 0 |
| Histiocytosis General term for the abnormal appearance of histiocytes in the blood. Based on the pathological features of the cells involved rather than on clinical findings, the histiocytic diseases are subdivided into three groups: HISTIOCYTOSIS, LANGERHANS CELL; HISTIOCYTOSIS, NON-LANGERHANS-CELL; and HISTIOCYTIC DISORDERS, MALIGNANT. | 0 | 1.99 | 1 | 0 |
| Epididymitis Inflammation of the EPIDIDYMIS. Its clinical features include enlarged epididymis, a swollen SCROTUM; PAIN; PYURIA; and FEVER. It is usually related to infections in the URINARY TRACT, which likely spread to the EPIDIDYMIS through either the VAS DEFERENS or the lymphatics of the SPERMATIC CORD. | 0 | 3.37 | 1 | 1 |
| Orchitis Inflammation of a TESTIS. It has many features of EPIDIDYMITIS, such as swollen SCROTUM; PAIN; PYURIA; and FEVER. It is usually related to infections in the URINARY TRACT, which likely spread to the EPIDIDYMIS and then the TESTIS through either the VAS DEFERENS or the lymphatics of the SPERMATIC CORD. | 0 | 3.37 | 1 | 1 |
| Brain Disorders [description not available] | 0 | 2.91 | 4 | 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 | 2.91 | 4 | 0 |
| Hydronephrosis Abnormal enlargement or swelling of a KIDNEY due to dilation of the KIDNEY CALICES and the KIDNEY PELVIS. It is often associated with obstruction of the URETER or chronic kidney diseases that prevents normal drainage of urine into the URINARY BLADDER. | 0 | 4.06 | 3 | 1 |
| Hypertension, Renal Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN. | 0 | 1.99 | 1 | 0 |
| Cystadenoma, Serous A cystic tumor of the ovary, containing thin, clear, yellow serous fluid and varying amounts of solid tissue, with a malignant potential several times greater than that of mucinous cystadenoma (CYSTADENOMA, MUCINOUS). It can be unilocular, parvilocular, or multilocular. It is often bilateral and papillary. The cysts may vary greatly in size. (Dorland, 27th ed; from Hughes, Obstetric-Gynecologic Terminology, 1972) | 0 | 1.99 | 1 | 0 |
| Intraepithelial Prostatic Neoplasia [description not available] | 0 | 4.99 | 3 | 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 | 4.99 | 3 | 3 |
| Agitation, Psychomotor [description not available] | 0 | 1.99 | 1 | 0 |
| Psychomotor Agitation A feeling of restlessness associated with increased motor activity. This may occur as a manifestation of nervous system drug toxicity or other conditions. | 0 | 1.99 | 1 | 0 |
| Amyotonia Congenita [description not available] | 0 | 1.99 | 1 | 0 |
| Neuromuscular Diseases A general term encompassing lower MOTOR NEURON DISEASE; PERIPHERAL NERVOUS SYSTEM DISEASES; and certain MUSCULAR DISEASES. Manifestations include MUSCLE WEAKNESS; FASCICULATION; muscle ATROPHY; SPASM; MYOKYMIA; MUSCLE HYPERTONIA, myalgias, and MUSCLE HYPOTONIA. | 0 | 1.99 | 1 | 0 |
| Acquired Meningomyelocele [description not available] | 0 | 2.4 | 2 | 0 |
| Abdominal Migraine [description not available] | 0 | 3.38 | 1 | 1 |
| Migraine Disorders A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1) | 0 | 3.38 | 1 | 1 |
| Weight Reduction [description not available] | 0 | 1.99 | 1 | 0 |
| Weight Loss Decrease in existing BODY WEIGHT. | 0 | 6.99 | 1 | 0 |
| Urethral Diseases Pathological processes involving the URETHRA. | 0 | 1.99 | 1 | 0 |
| Leiomyosarcoma, Epithelioid [description not available] | 0 | 3.81 | 4 | 0 |
| Leiomyosarcoma A sarcoma containing large spindle cells of smooth muscle. Although it rarely occurs in soft tissue, it is common in the viscera. It is the most common soft tissue sarcoma of the gastrointestinal tract and uterus. The median age of patients is 60 years. (From Dorland, 27th ed; Holland et al., Cancer Medicine, 3d ed, p1865) | 0 | 8.81 | 4 | 0 |
| Encephalopathy, Hepatic [description not available] | 0 | 2.9 | 1 | 0 |
| Hepatic Encephalopathy A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5) | 0 | 2.9 | 1 | 0 |
| Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply. | 0 | 2.68 | 3 | 0 |
| Morbid Obesity [description not available] | 0 | 1.99 | 1 | 0 |
| Obesity, Morbid The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2. | 0 | 1.99 | 1 | 0 |
| Arteriosclerosis Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries. | 0 | 1.99 | 1 | 0 |
| Diarrhea An increased liquidity or decreased consistency of FECES, such as running stool. Fecal consistency is related to the ratio of water-holding capacity of insoluble solids to total water, rather than the amount of water present. Diarrhea is not hyperdefecation or increased fecal weight. | 0 | 4.33 | 2 | 2 |
| Disease, Pulmonary [description not available] | 0 | 2.92 | 4 | 0 |
| Lung Diseases Pathological processes involving any part of the LUNG. | 0 | 2.92 | 4 | 0 |
| Cancer of Colon [description not available] | 0 | 1.99 | 1 | 0 |
| Primate Diseases Diseases of animals within the order PRIMATES. This term includes diseases of Haplorhini and Strepsirhini. | 0 | 1.99 | 1 | 0 |
| Colonic Neoplasms Tumors or cancer of the COLON. | 0 | 1.99 | 1 | 0 |
| Oligomenorrhea Abnormally infrequent menstruation. | 0 | 2.38 | 2 | 0 |
| Diabetic Glomerulosclerosis [description not available] | 0 | 1.99 | 1 | 0 |
| Diabetic Nephropathies KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE. | 0 | 1.99 | 1 | 0 |
| Glomerulonephritis, Lupus [description not available] | 0 | 1.99 | 1 | 0 |
| Lupus Nephritis Glomerulonephritis associated with autoimmune disease SYSTEMIC LUPUS ERYTHEMATOSUS. Lupus nephritis is histologically classified into 6 classes: class I - normal glomeruli, class II - pure mesangial alterations, class III - focal segmental glomerulonephritis, class IV - diffuse glomerulonephritis, class V - diffuse membranous glomerulonephritis, and class VI - advanced sclerosing glomerulonephritis (The World Health Organization classification 1982). | 0 | 1.99 | 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 | 1.99 | 1 | 0 |
| Proteinuria The presence of proteins in the urine, an indicator of KIDNEY DISEASES. | 0 | 1.99 | 1 | 0 |
| Aqueductal Stenosis [description not available] | 0 | 1.99 | 1 | 0 |
| Hypesthesia Absent or reduced sensitivity to cutaneous stimulation. | 0 | 1.99 | 1 | 0 |
| Nerve Pain [description not available] | 0 | 1.99 | 1 | 0 |
| Dysesthesia [description not available] | 0 | 1.99 | 1 | 0 |
| Neuralgia, Sciatic [description not available] | 0 | 1.99 | 1 | 0 |
| Low Back Ache [description not available] | 0 | 1.99 | 1 | 0 |
| Neuralgia Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve. | 0 | 1.99 | 1 | 0 |
| Sciatica A condition characterized by pain radiating from the back into the buttock and posterior/lateral aspects of the leg. Sciatica may be a manifestation of SCIATIC NEUROPATHY; RADICULOPATHY (involving the SPINAL NERVE ROOTS; L4, L5, S1, or S2, often associated with INTERVERTEBRAL DISK DISPLACEMENT); or lesions of the CAUDA EQUINA. | 0 | 1.99 | 1 | 0 |
| Low Back Pain Acute or chronic pain in the lumbar or sacral regions, which may be associated with musculo-ligamentous SPRAINS AND STRAINS; INTERVERTEBRAL DISK DISPLACEMENT; and other conditions. | 0 | 1.99 | 1 | 0 |
| Prostatic Diseases Pathological processes involving the PROSTATE or its component tissues. | 0 | 3.38 | 1 | 1 |
| Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses. | 0 | 8.38 | 1 | 1 |
| Adolescent Gynecomastia [description not available] | 0 | 1.99 | 1 | 0 |
| 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 | 1.99 | 1 | 0 |
| Endometrial Stromal Sarcoma [description not available] | 0 | 3.32 | 2 | 0 |
| Sarcoma, Endometrial Stromal A highly malignant subset of neoplasms arising from the endometrial stroma. Tumors in this group infiltrate the stroma with a wide range of atypia cells and numerous mitoses. They are capable of widespread metastases (NEOPLASM METASTASIS). | 0 | 3.32 | 2 | 0 |
| Cardiac Cancer [description not available] | 0 | 2.41 | 2 | 0 |
| Abdominal Epilepsy [description not available] | 0 | 2 | 1 | 0 |
| Epilepsies, Partial Conditions characterized by recurrent paroxysmal neuronal discharges which arise from a focal region of the brain. Partial seizures are divided into simple and complex, depending on whether consciousness is unaltered (simple partial seizure) or disturbed (complex partial seizure). Both types may feature a wide variety of motor, sensory, and autonomic symptoms. Partial seizures may be classified by associated clinical features or anatomic location of the seizure focus. A secondary generalized seizure refers to a partial seizure that spreads to involve the brain diffusely. (From Adams et al., Principles of Neurology, 6th ed, pp317) | 0 | 2 | 1 | 0 |
| Diseases, Peripheral Vascular [description not available] | 0 | 2 | 1 | 0 |
| Peripheral Vascular Diseases Pathological processes involving any one of the BLOOD VESSELS in the vasculature outside the HEART. | 0 | 2 | 1 | 0 |
| Diseases in Twins Disorders affecting TWINS, one or both, at any age. | 0 | 2.39 | 2 | 0 |
| Cruveilhier-Baumgarten Syndrome Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS. | 0 | 2 | 1 | 0 |
| Hypertension, Portal Abnormal increase of resistance to blood flow within the hepatic PORTAL SYSTEM, frequently seen in LIVER CIRRHOSIS and conditions with obstruction of the PORTAL VEIN. | 0 | 2 | 1 | 0 |
| Bile Duct Obstruction [description not available] | 0 | 2 | 1 | 0 |
| Cholestasis Impairment of bile flow due to obstruction in small bile ducts (INTRAHEPATIC CHOLESTASIS) or obstruction in large bile ducts (EXTRAHEPATIC CHOLESTASIS). | 0 | 2 | 1 | 0 |
| Post-Natal Depression [description not available] | 0 | 14.53 | 49 | 49 |
| Depression, Postpartum Depression in POSTPARTUM WOMEN, usually within four weeks after giving birth (PARTURITION). The degree of depression ranges from mild transient depression to neurotic or psychotic depressive disorders. (From DSM-IV, p386) | 0 | 14.53 | 49 | 49 |
| As If Personality [description not available] | 0 | 2 | 1 | 0 |
| Sadism A condition in which there is a derivation of pleasure from inflicting pain, discomfort or humiliation on another person or persons. The sexual significance of sadistic wishes or behavior may be conscious or unconscious. | 0 | 2 | 1 | 0 |
| Complex and Mixed Neoplasms [description not available] | 0 | 2 | 1 | 0 |
| Cancer of Kidney [description not available] | 0 | 2.39 | 2 | 0 |
| Congenital Mesoblastic Nephroma [description not available] | 0 | 2 | 1 | 0 |
| Kidney Neoplasms Tumors or cancers of the KIDNEY. | 0 | 2.39 | 2 | 0 |
| Neoplasms, Complex and Mixed Neoplasms composed of more than one type of neoplastic tissue. | 0 | 2 | 1 | 0 |
| Pregnancy, Tubal The most common ( | 0 | 2.39 | 2 | 0 |
| Ectopic Hormone Syndromes [description not available] | 0 | 3.31 | 2 | 0 |
| Hypertriglyceridemia A condition of elevated levels of TRIGLYCERIDES in the blood. | 0 | 2 | 1 | 0 |
| Diseases of Endocrine System [description not available] | 0 | 2.92 | 1 | 0 |
| Endocrine System Diseases Pathological processes of the ENDOCRINE GLANDS, and diseases resulting from abnormal level of available HORMONES. | 0 | 2.92 | 1 | 0 |
| Brain Damage, Chronic A condition characterized by long-standing brain dysfunction or damage, usually of three months duration or longer. Potential etiologies include BRAIN INFARCTION; certain NEURODEGENERATIVE DISORDERS; CRANIOCEREBRAL TRAUMA; ANOXIA, BRAIN; ENCEPHALITIS; certain NEUROTOXICITY SYNDROMES; metabolic disorders (see BRAIN DISEASES, METABOLIC); and other conditions. | 0 | 2 | 1 | 0 |
| Benign Cerebellar Neoplasms [description not available] | 0 | 2 | 1 | 0 |
| Absence Seizure Disorder [description not available] | 0 | 2 | 1 | 0 |
| Arachnoidal Cerebellar Sarcoma, Circumscribed [description not available] | 0 | 2 | 1 | 0 |
| Epilepsy, Absence A seizure disorder usually occurring in childhood characterized by rhythmic electrical brain discharges of generalized onset. Clinical features include a sudden cessation of ongoing activity usually without loss of postural tone. Rhythmic blinking of the eyelids or lip smacking frequently accompanies the SEIZURES. The usual duration is 5-10 seconds, and multiple episodes may occur daily. Juvenile absence epilepsy is characterized by the juvenile onset of absence seizures and an increased incidence of myoclonus and tonic-clonic seizures. (Menkes, Textbook of Child Neurology, 5th ed, p736) | 0 | 2 | 1 | 0 |
| Medulloblastoma A malignant neoplasm that may be classified either as a glioma or as a primitive neuroectodermal tumor of childhood (see NEUROECTODERMAL TUMOR, PRIMITIVE). The tumor occurs most frequently in the first decade of life with the most typical location being the cerebellar vermis. Histologic features include a high degree of cellularity, frequent mitotic figures, and a tendency for the cells to organize into sheets or form rosettes. Medulloblastoma have a high propensity to spread throughout the craniospinal intradural axis. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2060-1) | 0 | 2 | 1 | 0 |
| Bladder Neck Obstruction [description not available] | 0 | 3.33 | 2 | 0 |
| Hyperthyroid [description not available] | 0 | 2 | 1 | 0 |
| Hyperthyroidism Hypersecretion of THYROID HORMONES from the THYROID GLAND. Elevated levels of thyroid hormones increase BASAL METABOLIC RATE. | 0 | 2 | 1 | 0 |
| Gynandroblastoma A sex cord-gonadal stromal tumor, composed of cells of both the OVARY and the TESTIS. It produces both male and female GONADAL STEROID HORMONES. | 0 | 2 | 1 | 0 |
| Sex Cord-Gonadal Stromal Tumors Neoplasms derived from the primitive sex cord or gonadal stromal cells of the embryonic GONADS. They are classified by their presumed histogenesis and differentiation. From the sex cord, there are SERTOLI CELL TUMOR and GRANULOSA CELL TUMOR; from the gonadal stroma, LEYDIG CELL TUMOR and THECOMA. These tumors may be identified in either the OVARY or the TESTIS. | 0 | 2 | 1 | 0 |
| Thyrotoxicosis A hypermetabolic syndrome caused by excess THYROID HORMONES which may come from endogenous or exogenous sources. The endogenous source of hormone may be thyroid HYPERPLASIA; THYROID NEOPLASMS; or hormone-producing extrathyroidal tissue. Thyrotoxicosis is characterized by NERVOUSNESS; TACHYCARDIA; FATIGUE; WEIGHT LOSS; heat intolerance; and excessive SWEATING. | 0 | 7 | 1 | 0 |
| Adrenal Cortex Diseases Pathological processes of the ADRENAL CORTEX. | 0 | 2 | 1 | 0 |
| Diffuse Myofascial Pain Syndrome [description not available] | 0 | 2 | 1 | 0 |
| Fibromyalgia A common nonarticular rheumatic syndrome characterized by myalgia and multiple points of focal muscle tenderness to palpation (trigger points). Muscle pain is typically aggravated by inactivity or exposure to cold. This condition is often associated with general symptoms, such as sleep disturbances, fatigue, stiffness, HEADACHES, and occasionally DEPRESSION. There is significant overlap between fibromyalgia and the chronic fatigue syndrome (FATIGUE SYNDROME, CHRONIC). Fibromyalgia may arise as a primary or secondary disease process. It is most frequent in females aged 20 to 50 years. (From Adams et al., Principles of Neurology, 6th ed, p1494-95) | 0 | 2 | 1 | 0 |
| Chromosome Deletion Actual loss of portion of a chromosome. | 0 | 2 | 1 | 0 |
| Granuloma, Hodgkin [description not available] | 0 | 3.39 | 1 | 1 |
| Diffuse Mixed Small and Large Cell Lymphoma [description not available] | 0 | 3.39 | 1 | 1 |
| Carcinoma, Thymic [description not available] | 0 | 3.78 | 2 | 1 |
| Hodgkin Disease A malignant disease characterized by progressive enlargement of the lymph nodes, spleen, and general lymphoid tissue. In the classical variant, giant usually multinucleate Hodgkin's and REED-STERNBERG CELLS are present; in the nodular lymphocyte predominant variant, lymphocytic and histiocytic cells are seen. | 0 | 3.39 | 1 | 1 |
| Lymphoma, Non-Hodgkin Any of a group of malignant tumors of lymphoid tissue that differ from HODGKIN DISEASE, being more heterogeneous with respect to malignant cell lineage, clinical course, prognosis, and therapy. The only common feature among these tumors is the absence of giant REED-STERNBERG CELLS, a characteristic of Hodgkin's disease. | 0 | 3.39 | 1 | 1 |
| Thymoma A neoplasm originating from thymic tissue, usually benign, and frequently encapsulated. Although it is occasionally invasive, metastases are extremely rare. It consists of any type of thymic epithelial cell as well as lymphocytes that are usually abundant. Malignant lymphomas that involve the thymus, e.g., lymphosarcoma, Hodgkin's disease (previously termed granulomatous thymoma), should not be regarded as thymoma. (From Stedman, 25th ed) | 0 | 3.78 | 2 | 1 |
| Angioleiomyoma [description not available] | 0 | 2 | 1 | 0 |
| Anasarca [description not available] | 0 | 3.79 | 2 | 1 |
| Vulvar Diseases Pathological processes of the VULVA. | 0 | 2.01 | 1 | 0 |
| Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. | 0 | 3.79 | 2 | 1 |
| Hypermyotonia [description not available] | 0 | 2.01 | 1 | 0 |
| Benign Intracranial Hypertension [description not available] | 0 | 2.39 | 2 | 0 |
| Pseudotumor Cerebri A condition marked by raised intracranial pressure and characterized clinically by HEADACHES; NAUSEA; PAPILLEDEMA, peripheral constriction of the visual fields, transient visual obscurations, and pulsatile TINNITUS. OBESITY is frequently associated with this condition, which primarily affects women between 20 and 44 years of age. Chronic PAPILLEDEMA may lead to optic nerve injury (see OPTIC NERVE DISEASES) and visual loss (see BLINDNESS). | 0 | 2.39 | 2 | 0 |
| Bladder Pain Syndrome [description not available] | 0 | 2.01 | 1 | 0 |
| Cystitis, Interstitial A condition with recurring discomfort or pain in the URINARY BLADDER and the surrounding pelvic region without an identifiable disease. Severity of pain in interstitial cystitis varies greatly and often is accompanied by increased urination frequency and urgency. | 0 | 2.01 | 1 | 0 |
| Adenohypophyseal Hyposecretion [description not available] | 0 | 1.98 | 1 | 0 |
| Hypopituitarism Diminution or cessation of secretion of one or more hormones from the anterior pituitary gland (including LH; FOLLICLE STIMULATING HORMONE; SOMATOTROPIN; and CORTICOTROPIN). This may result from surgical or radiation ablation, non-secretory PITUITARY NEOPLASMS, metastatic tumors, infarction, PITUITARY APOPLEXY, infiltrative or granulomatous processes, and other conditions. | 0 | 1.98 | 1 | 0 |
| Carcinoma, Oat Cell [description not available] | 0 | 2.89 | 1 | 0 |
| Carcinoma, Small Cell An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7) | 0 | 2.89 | 1 | 0 |
| Cytomegalic Inclusion Disease [description not available] | 0 | 1.98 | 1 | 0 |
| Chronic Idiopathic Intestinal Pseudo-Obstruction [description not available] | 0 | 1.98 | 1 | 0 |
| Viremia The presence of viruses in the blood. | 0 | 1.98 | 1 | 0 |
| Cytomegalovirus Infections Infection with CYTOMEGALOVIRUS, characterized by enlarged cells bearing intranuclear inclusions. Infection may be in almost any organ, but the salivary glands are the most common site in children, as are the lungs in adults. | 0 | 1.98 | 1 | 0 |
| Intestinal Pseudo-Obstruction A type of ILEUS, a functional not mechanical obstruction of the INTESTINES. This syndrome is caused by a large number of disorders involving the smooth muscles (MUSCLE, SMOOTH) or the NERVOUS SYSTEM. | 0 | 6.98 | 1 | 0 |
| Anosmic Hypogonadism [description not available] | 0 | 2.89 | 1 | 0 |
| Kallmann Syndrome A genetically heterogeneous disorder caused by hypothalamic GNRH deficiency and OLFACTORY NERVE defects. It is characterized by congenital HYPOGONADOTROPIC HYPOGONADISM and ANOSMIA, possibly with additional midline defects. It can be transmitted as an X-linked (GENETIC DISEASES, X-LINKED), an autosomal dominant, or an autosomal recessive trait. | 0 | 2.89 | 1 | 0 |
| Conus Medullaris Syndrome [description not available] | 0 | 1.97 | 1 | 0 |
| Emergencies Situations or conditions requiring immediate intervention to avoid serious adverse results. | 0 | 1.97 | 1 | 0 |
| Cancer of the Ureter [description not available] | 0 | 1.97 | 1 | 0 |
| Ureteral Neoplasms Cancer or tumors of the URETER which may cause obstruction leading to hydroureter, HYDRONEPHROSIS, and PYELONEPHRITIS. HEMATURIA is a common symptom. | 0 | 1.97 | 1 | 0 |
| Abdominal Neoplasms New abnormal growth of tissue in the ABDOMEN. | 0 | 3.36 | 1 | 1 |
| Adenosis of Breast [description not available] | 0 | 1.97 | 1 | 0 |
| Fibrocystic Breast Disease A common and benign breast disease characterized by varying degree of fibrocystic changes in the breast tissue. There are three major patterns of morphological changes, including FIBROSIS, formation of CYSTS, and proliferation of glandular tissue (adenosis). The fibrocystic breast has a dense irregular, lumpy, bumpy consistency. | 0 | 1.97 | 1 | 0 |
| Death, Sudden The abrupt cessation of all vital bodily functions, manifested by the permanent loss of total cerebral, respiratory, and cardiovascular functions. | 0 | 3.8 | 1 | 0 |
| Hyperlipemia [description not available] | 0 | 1.97 | 1 | 0 |
| Hyperlipidemias Conditions with excess LIPIDS in the blood. | 0 | 1.97 | 1 | 0 |
| Abnormalities, Congenital [description not available] | 0 | 1.97 | 1 | 0 |
| Christmas Disease [description not available] | 0 | 1.97 | 1 | 0 |
| Hemophilia B A deficiency of blood coagulation factor IX inherited as an X-linked disorder. (Also known as Christmas Disease, after the first patient studied in detail, not the holy day.) Historical and clinical features resemble those in classic hemophilia (HEMOPHILIA A), but patients present with fewer symptoms. Severity of bleeding is usually similar in members of a single family. Many patients are asymptomatic until the hemostatic system is stressed by surgery or trauma. Treatment is similar to that for hemophilia A. (From Cecil Textbook of Medicine, 19th ed, p1008) | 0 | 1.97 | 1 | 0 |
| Cancer of the Thymus [description not available] | 0 | 1.97 | 1 | 0 |
| Thymus Neoplasms Tumors or cancer of the THYMUS GLAND. | 0 | 1.97 | 1 | 0 |
| Complication, Intraoperative [description not available] | 0 | 3.36 | 1 | 1 |
| Sweat Gland Diseases Diseases of the SWEAT GLANDS. | 0 | 1.97 | 1 | 0 |
| Anorexia Nervosa An eating disorder that is characterized by the lack or loss of APPETITE, known as ANOREXIA. Other features include excess fear of becoming OVERWEIGHT; BODY IMAGE disturbance; significant WEIGHT LOSS; refusal to maintain minimal normal weight; and AMENORRHEA. This disorder occurs most frequently in adolescent females. (APA, Thesaurus of Psychological Index Terms, 1994) | 0 | 1.96 | 1 | 0 |
| Alloxan Diabetes [description not available] | 0 | 1.97 | 1 | 0 |
| Chronic Motor and Vocal Tic Disorder [description not available] | 0 | 1.97 | 1 | 0 |
| Tourette Syndrome A neuropsychological disorder related to alterations in DOPAMINE metabolism and neurotransmission involving frontal-subcortical neuronal circuits. Both multiple motor and one or more vocal tics need to be present with TICS occurring many times a day, nearly daily, over a period of more than one year. The onset is before age 18 and the disturbance is not due to direct physiological effects of a substance or another medical condition. The disturbance causes marked distress or significant impairment in social, occupational, or other important areas of functioning. (From DSM-IV, 1994; Neurol Clin 1997 May;15(2):357-79) | 0 | 1.97 | 1 | 0 |
| Toxoplasmosis, Animal Acquired infection of non-human animals by organisms of the genus TOXOPLASMA. | 0 | 1.96 | 1 | 0 |
| Genital Diseases, Male Pathological processes involving the male reproductive tract (GENITALIA, MALE). | 0 | 1.96 | 1 | 0 |
| Experimental Neoplasms [description not available] | 0 | 1.96 | 1 | 0 |