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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5311128 |
| CHEMBL ID | 1201247 |
| CHEBI ID | 5523 |
| SCHEMBL ID | 8643 |
| SCHEMBL ID | 19712239 |
| SCHEMBL ID | 20459194 |
| MeSH ID | M0026217 |
| Synonym |
|---|
| AB01275466-01 |
| decapeptide i |
| ici-118630 |
| zd-9393 |
| goserelin [usan:inn:ban] |
| d-ser(t-bu)(sup 6)aza-gly(sup 10)-gnrh |
| goserelina [spanish] |
| 1-(5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-o-tert-butyl-d-seryl-l-leucyl-l-arginyl-l-prolyl)semicarbazide |
| goserelinum [latin] |
| ici 118630 |
| gosereline [french] |
| goserelin (usan/inn) |
| 65807-02-5 |
| D04405 |
| goserelin |
| DB00014 |
| HMS2089D16 |
| ici 118,630 |
| CHEMBL1201247 |
| AKOS015994653 |
| unii-0f65r8p09n |
| goserelina |
| 0f65r8p09n , |
| goserelinum |
| gosereline |
| hsdb 7606 |
| gtpl3879 |
| HY-13673 |
| SCHEMBL8643 |
| HS-2015 , |
| DTXSID7048297 , |
| goserelin [who-dd] |
| goserelin [inn] |
| goserelin [usan] |
| goserelin [mart.] |
| goserelin [ep monograph] |
| goserelin [hsdb] |
| goserelin [mi] |
| AKOS030213245 |
| CHEBI:5523 |
| (d-ser(tbu)6,azagly10)-lhrh (free base) |
| mfcd00867894 |
| SCHEMBL19712239 |
| SCHEMBL20459194 |
| 1233494-97-7 |
| Q1992653 |
| goserelin-acetate |
| NCGC00390804-01 |
| (s)-n-((6s,9s,12r,15s,18s,21s,24s)-21-((1h-indol-3-yl)methyl)-1-amino-12-(tert-butoxymethyl)-6-((s)-2-(2-carbamoylhydrazine-1-carbonyl)pyrrolidine-1-carbonyl)-15-(4-hydroxybenzyl)-18-(hydroxymethyl)-25-(1h-imidazol-4-yl)-1-imino-9-isobutyl-8,11,14,17,20,2 |
| l02ae03 |
| goserelin (ep monograph) |
| dtxcid2028272 |
| goserelinum (latin) |
| goserelin (mart.) |
| 6-(o-(1,1-dimethylethyl)-d-serine)-10-deglycinamide luteinizing hormone-releasing factor (pig) 2-(aminocarbonyl)hydrazide |
| (2s)-1-[(2s)-2-[(2s)-2-[(2r)-3-(tert-butoxy)-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]propanamido]-4-methyl |
| EN300-7480905 |
Goserelin acetate (Gos) is a luteinizing hormone-releasing hormone agonist. It is commonly used in patients with prostate cancer, endometriosis, and precocious puberty. GOSErelin is a biodegradable, sustained-release 3.6 mg depot.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Goserelin acetate is a gonadotropin-releasing hormone analog that is commonly used in patients with prostate cancer, endometriosis, and precocious puberty. " | ( Erythema nodosum caused by goserelin acetate sustained-release: Case report and literature review. Du, S; Ling, L; Liu, W; Meng, F; Peng, J; Su, R; Yan, W, 2023) | 2.65 |
| "Goserelin acetate (Gos) is a luteinizing hormone-releasing hormone agonist, used in treatment of prostate cancer in which desired concentration of Gos in blood is maintained for longer duration. " | ( Nanoparticulate delivery of LHRH analogue for the treatment of prostate cancer. Dixit, VK; Jain, N; Tomar, P, ) | 1.57 |
| "Goserelin acetate is a LH-RH agonist developed by AstraZeneca (formerly ICI, UK), and has been used clinically for the treatment of prostate cancer as a 4-week controlled-release formulation (Zoladex 3.6 mg depot). " | ( [A new LH-RH agonist for treatment of prostate cancer, 3-month controlled-release formulation of goserelin acetate (Zoladex LA 10.8 mg depot)--outline of pre-clinical and clinical studies]. Tsukagoshi, S, 2002) | 1.97 |
| "Goserelin is a biodegradable, sustained-release 3.6 mg depot that is administered by subcutaneous injection every 28 days." | ( Goserelin ('Zoladex')--offering patients more choice in early breast cancer. Mitchell, H, 2004) | 2.49 |
| "Goserelin is an effective short-term treatment for mastalgia. " | ( European randomized, multicenter study of goserelin (Zoladex) in the management of mastalgia. Gateley, C; Goyal, A; Kubista, E; Leinster, S; Maddox, PR; Mansel, RE; Preece, P; von Fournier, D, 2004) | 2.03 |
| "Goserelin acetate is a member of this class, and 10 of 11 major Phase III trials demonstrating better outcomes with ADT and RT used goserelin acetate." | ( Goserelin acetate in combination with radiotherapy for prostate cancer. Izaguirre, A; Roach, M, 2007) | 2.5 |
| "Goserelin is a gonadotrophin-releasing hormone (GnRH) analogue which during long term administration reduces circulating levels of gonadotrophins (luteinising hormone and follicle stimulating hormone) and sex hormones. " | ( Goserelin. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in prostate cancer. Brogden, RN; Faulds, D, 1995) | 3.18 |
| "Goserelin is a gonadotrophin-releasing hormone (GnRH) analogue that induces the suppression of gonadal steroidogenesis, and it could therefore be a medical alternative to irreversible surgical castration. " | ( Ovarian function suppression with the gonadotrophin-releasing hormone (GnRH) analogue goserelin in premenopausal advanced breast cancer. Bajetta, E; Bono, A; Buzzoni, R; Celio, L; Ferrari, L; Galluzzo, D; Longhi, A; Zampino, MG; Zilembo, N, 1994) | 1.95 |
| "Goserelin acetate is a synthetic GnRH agonist suitable for safe and effective therapy of pelvic endometriosis. " | ( [Treatment of pelvic endometriosis with goserelin, an LHRH agonist]. Crha, I; Mlyncek, M; Müller, P; Ventruba, P, 1996) | 2 |
| "Goserelin is a gonadotrophin-releasing hormone (GnRH) analogue which, during continuous administration, down-regulates the pituitary-ovarian gonadal axis and reduces levels of the gonadotrophins, luteinising hormone and follicle-stimulating hormone. " | ( Goserelin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in benign gynaecological disorders. Brogden, RN; Perry, CM, 1996) | 3.18 |
| "Goserelin is a synthetic decapeptide analogue of luteinising hormone-releasing hormone (LHRH). " | ( Clinical pharmacokinetics of goserelin. Cockshott, ID, 2000) | 2.04 |
| "Goserelin is an important drug with recognized therapeutical application for palliative treatment of prostatic and breast carcinomas." | ( Liquid chromatography-electrospray mass spectrometry of multicomponent peptide mixtures. Characterization of a mixture from the synthesis of the hormone goserelin. Barbosa, J; Benavente, F; Castillo, A; Sanz-Nebot, V, 2000) | 1.23 |
| "Goserelin is a synthetic analogue of gonadotrophin-releasing hormone (GnRH) [luteinising hormone-releasing hormone (LHRH); or gonadorelin] which stimulates gonadotrophin and sex hormone release in the short term, and then causes suppression with continued administration. " | ( Goserelin. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use in sex hormone-related conditions. Chrisp, P; Goa, KL, 1991) | 3.17 |
Goserelin has better injection site safety, single-step delivery, and an efficient administration schedule compared with degarelix. It also has maximum benefit in prostate-specific antigen suppression.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Goserelin also has maximum benefit in prostate-specific antigen suppression." | ( Gonadotropin-releasing hormone agonists in prostate cancer: A comparative review of efficacy and safety. Addla, S; Jain, M; Patil, K; Raja, T; Sarkar, KK; Sridhar, PS; Sud, R; Talreja, V, 2022) | 1.44 |
| "Goserelin has better injection site safety, single-step delivery, and an efficient administration schedule compared with degarelix, which has significantly higher injection site reactions and less efficient administration mechanism." | ( A review of clinical evidence to assess differences in efficacy and safety of luteinizing hormone-releasing hormone (LHRH) agonist (goserelin) and LHRH antagonist (degarelix). Bahl, A; Bakshi, G; Murthy, V; Patil, K; Rajappa, S; Rawal, S, 2022) | 1.65 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Goserelin achieves lower PSA, improved time to progression, and better survival outcomes when administered adjunctively to radiotherapy compared with radiotherapy alone, with significant results even over long-term follow-up." | ( A review of clinical evidence to assess differences in efficacy and safety of luteinizing hormone-releasing hormone (LHRH) agonist (goserelin) and LHRH antagonist (degarelix). Bahl, A; Bakshi, G; Murthy, V; Patil, K; Rajappa, S; Rawal, S, 2022) | 1.65 |
Goserelin treatment decreased circulating levels of oestradiol and progesterone. Treatment with goserelin and tamoxifen led to a 90% fall in the mean follicle-stimulating hormone.
The number of CV adverse events (AEs) for degarelix, buserelin, gose Relin, leuprorelin and triptorelin until September 2021 were recorded. Adverse drug reaction:rates of a adverse reactions were 21% (15/70) in Leuprolide acetate group and 20% (13/66) in Goserelin acetate Group.
This research was to investigate the role of goserelin in combination with endocrine therapy for the treatment of advanced breast cancer in premenopausal women positive for hormone receptors. The RP2D of alpelisib and buparlisib in combination were 350 mg and 100 mg, respectively.
8-mg goserelin-acetate depot provided a dosing schedule that was convenient for the patient and the physician. It has the potential to reduce health care costs while maintaining the quality of life in patients being treated for advanced prostate cancer.
| Class | Description |
|---|---|
| organic molecular entity | Any molecular entity that contains carbon. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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] | |||
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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] | |||
| 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] | |||
| 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] | |||
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| 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] | |||
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| 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 | |||
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 184 (11.70) | 18.7374 |
| 1990's | 529 (33.63) | 18.2507 |
| 2000's | 485 (30.83) | 29.6817 |
| 2010's | 331 (21.04) | 24.3611 |
| 2020's | 44 (2.80) | 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 (72.24) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 557 (33.61%) | 5.53% |
| Reviews | 164 (9.90%) | 6.00% |
| Case Studies | 201 (12.13%) | 4.05% |
| Observational | 3 (0.18%) | 0.25% |
| Other | 732 (44.18%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Phase III Randomized, Double-blind, Placebo-controlled Study of LEE011 or Placebo in Combination With Tamoxifen and Goserelin or a Non-steroidal Aromatase Inhibitor (NSAI) and Goserelin for the Treatment of Premenopausal Women With Hormone Receptor Posi [NCT02278120] | Phase 3 | 672 participants (Actual) | Interventional | 2014-11-20 | Completed | ||
| A Phase I Dose Escalation Trial of RO4929097 Administered in Combination With Exemestane in Pre- and Postmenopausal Patients With ER + Metastatic Breast Cancer [NCT01149356] | Phase 1 | 15 participants (Actual) | Interventional | 2010-10-31 | Terminated(stopped due to Manufacturer discontinued drug development.) | ||
| A Phase Ib Dose Finding Study Assessing Safety and Activity of [177Lu]Lu-NeoB in Combination With Ribociclib and Fulvestrant in Participants With Estrogen Receptor Positive, Human Epidermal Growth Factor Receptor-2 Negative and Gastrin Releasing Peptide R [NCT05870579] | Phase 1 | 45 participants (Anticipated) | Interventional | 2023-11-13 | Recruiting | ||
| A Randomized Phase III Trial Evaluating Pathologic Complete Response Rates in Patients With Hormone Receptor-Positive, HER2-Positive, Large Operable and Locally Advanced Breast Cancer Treated With Neoadjuvant Therapy of Docetaxel, Carboplatin, Trastuzumab [NCT02003209] | Phase 3 | 315 participants (Actual) | Interventional | 2014-01-15 | Active, not recruiting | ||
| Two Arm, Multicentric, Randomized, Open Label, Parallel, Multiple Dose Study Subcutaneous Injection of Goserelin 3.6 mg (Eurofarma) vs ZOLADEX 3.6 mg (AstraZeneca) Administered Subcutaneously in Premenopausal Patients With Breast Cancer. [NCT03936933] | Phase 3 | 68 participants (Anticipated) | Interventional | 2020-10-30 | Recruiting | ||
| A Two Arm, Multi Centric, Randomised, Open Label, Parallel Study to Compare Pharmacodynamics of Subcutaneous Goserelin 10.8mg Injection (Sponsor) With ZOLADEX® 10.8mg Injection (AstraZeneca) in Patients With Advanced Prostate Cancer [NCT03936218] | Phase 3 | 94 participants (Anticipated) | Interventional | 2020-09-30 | Recruiting | ||
| Phase III Trial of LHRH Analog Administration During Chemotherapy to Reduce Ovarian Failure Following Chemotherapy in Early Stage, Hormone-Receptor Negative Breast Cancer [NCT00068601] | Phase 3 | 257 participants (Actual) | Interventional | 2003-10-31 | 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) | ||
| Randomized Phase II Study OF Goserelin (G) Plus Fulvestrant (F) vs. G Plus Anastrozole (A)vs. G Alone for HR+, Tamoxifen Pretreated, Premenopausal Woman [NCT01266213] | Phase 2 | 147 participants (Anticipated) | Interventional | 2010-12-31 | Active, not recruiting | ||
| A Randomized ,Open Label Study Comparing the Efficacy of Zoladex® Combined With Arimidex® for 3-2 Years After Selective Estrogen Receptor Modulators (SERMs) as an Adjuvant Therapy for 2-3 Years Versus Continuing Tamoxifen up to 5 Years for Premenopausal E [NCT01352091] | Phase 3 | 670 participants (Anticipated) | Interventional | 2008-05-31 | Recruiting | ||
| Multicentre, International Neoadjuvant Randomized Double-blind Trial Comparing Fulvestrant® to a Combination of Fulvestrant® and Palbociclib (CDK 4/6 Inhibitor) in Patients With Operable Luminal Breast Cancer Responding to Fulvestrant® [NCT03447132] | Phase 3 | 354 participants (Actual) | Interventional | 2017-12-20 | Completed | ||
| Hypo-Combi Trial: Combined Hypofractionated External Beam Radiation Therapy (EBRT) Plus Interstitial High-Dose-Rate Brachytherapy (HDR-BT) Boost for Intermediate/High Risk Prostate Cancer [NCT05003752] | Phase 1/Phase 2 | 40 participants (Actual) | Interventional | 2021-08-01 | Active, not recruiting | ||
| The TEEL Study: A Phase I Trial of Tamoxifen With Ribociclib (LEE011) in Adult Patients With Advanced ER+ (HER2 Negative) Breast Cancer [NCT02586675] | Phase 1 | 7 participants (Actual) | Interventional | 2016-02-23 | Completed | ||
| The Study of Goserelin Plus Fulvestrant Comparing With Goserelin Plus Anastrozole for Advanced Breast Cancer [NCT02072512] | Phase 2 | 180 participants (Anticipated) | Interventional | 2014-01-31 | Recruiting | ||
| Study of Adjuvant Toremifene With or Without Goserrelin in Premenopausal Women With Stage I-IIIA, Hormonal Receptor Positive Breast Cancer Accompanied With or Without Chemotherapy Induced Amenorrhoea [NCT02132390] | Phase 3 | 300 participants (Anticipated) | Interventional | 2014-05-31 | Not yet recruiting | ||
| A National Phase IIIb, Multi-center, Open Label Study for Women and Men With Hormone-receptor Positive, HER-2 Negative Locally Advanced or Metastatic Breast Cancer Treated With Ribociclib (LEE011) in Combination With Letrozole [NCT03096847] | Phase 3 | 502 participants (Actual) | Interventional | 2016-10-24 | Completed | ||
| Neoadjuvant Androgen Deprivation and Enzalutamide: Using Multiparametric MRI to Evaluate Intraprostatic Tumor Responses and Androgen Resistance Patterns in Newly Diagnosed Prostate Cancer [NCT02430480] | Phase 2 | 39 participants (Actual) | Interventional | 2015-06-03 | Active, not recruiting | ||
| Asian, International, Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 3 Trial of Tamoxifen With or Without Palbociclib ± Goserelin in Women With Hormone Receptor-Positive, HER2-Negative Advanced or Metastatic Breast Cancer [NCT03423199] | Phase 3 | 180 participants (Anticipated) | Interventional | 2018-02-09 | Active, not recruiting | ||
| A Phase II Study of Neoadjuvant Androgen Deprivation Therapy Combined With Enzalutamide and Abiraterone Using Multiparametric MRI and 18F-DCFPyL-PET/CT in Newly Diagnosed Prostate Cancer [NCT03860987] | Phase 2 | 11 participants (Actual) | Interventional | 2019-04-30 | Active, not recruiting | ||
| Phase II Study of Goserelin for Ovarian Protection in Premenopausal Patients Receiving Cyclophosphamide Containing Chemotherapy: Menstruation Outcome [NCT03475758] | Phase 2 | 100 participants (Anticipated) | Interventional | 2018-03-31 | Not yet 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 Multicenter, Randomized Phase ll Study of Letrozole Versus Letrozole Plus Everolimus for Hormone Receptor-PositivePremenopausal Women With Recurrent or Metastatic Breast Cancer on Goserelin Treatment After Progression on Tamoxifen [NCT02313051] | Phase 2 | 200 participants (Anticipated) | Interventional | 2014-12-31 | Not yet recruiting | ||
| Treatment With Long Acting GnRH Antagonist Degarelix in Women With Endometriosis Recurrence [NCT01712763] | Phase 3 | 360 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| 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 | ||
| An Open Label, Randomised, Parallel Group, Multicentre, Non-inferiority Study to Compare ZOLADEX 10.8 mg With ZOLADEX 3.6 mg in Chinese Pre-menopausal Patients With Estrogen Receptor-Positive and HER2 Negative Early Breast Cancer [NCT03658213] | Phase 3 | 0 participants (Actual) | Interventional | 2020-03-31 | Withdrawn(stopped due to CTP of LARES has been out of the expire date, we are trying RWS pathway for the indication expend) | ||
| A PHASE III TRIAL COMPARING WHOLE PELVIC IRRADIATION FOLLOWED BY A CONEDOWN BOOST TO BOOST IRRADIATION ONLY AND COMPARING NEOADJUVANT TO ADJUVANT TOTAL ANDROGEN SUPPRESSION (TAS) [NCT00769548] | Phase 3 | 1,322 participants (Actual) | Interventional | 1995-04-30 | Completed | ||
| A Randomized Phase 2 Non-inferiority Trial of (Z)-Endoxifen and Exemestane + Goserelin as Neoadjuvant Treatment in Premenopausal Women With ER+/HER2- Breast Cancer [NCT05607004] | Phase 2 | 180 participants (Anticipated) | Interventional | 2023-02-14 | Recruiting | ||
| A Phase II Study of PROSTVAC-V (Vaccinia)/TRICOM and PROSTVAC-F (Fowlpox)/TRICOM With GM-CSF in Patients With PSA Progression After Local Therapy for Prostate Cancer [NCT00108732] | Phase 2 | 50 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| Evaluation of the Antitumor Activity, Safety, and Pharmacokinetic Profile of FCN-437c in Combination With Fulvestrant or Letrozole + Goserelin in Female Patients With ER+, HER2- Advanced Breast Cancer [NCT05004142] | Phase 2 | 70 participants (Anticipated) | Interventional | 2020-06-30 | Recruiting | ||
| Intramuscular Mechanisms of Androgen Deprivation-related Sarcopenia [NCT03867357] | 60 participants (Actual) | Observational | 2018-12-07 | Active, not recruiting | |||
| Role of Fulvestrant in The Treatment of Metastatic Breast Cancer in Premenopausal Women [NCT03591549] | Phase 4 | 30 participants (Anticipated) | Interventional | 2018-08-01 | Not yet recruiting | ||
| 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 | ||
| Androgen Suppression With Stereotactic Body or External Beam Radiation Therapy (ASSERT): A Phase II Randomized Trial for Intermediate and High Risk Prostate Cancer [NCT02594072] | 80 participants (Anticipated) | Interventional | 2016-04-30 | Active, not recruiting | |||
| 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 | ||
| Novel Magnetic Resonance Imaging Strategies as a Non-invasive Biomarker of Vascular and Extracellular Matrix Morphology in Women With Uterine Fibroids. [NCT00746031] | Phase 4 | 30 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| Phase 3 Study of Experience With a Gonadotropin-releasing Hormone Agonist Prior to Myomectomy - Comparison of 2 Versus 3 Monthly Doses. [NCT01581944] | Phase 3 | 68 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| Adjuvant Androgen Deprivation Versus Mitoxantrone Plus Prednisone Plus Androgen Deprivation in Selected High-Risk Prostate Cancer Patients Following Radical Prostatectomy [NCT00004124] | Phase 3 | 983 participants (Actual) | Interventional | 1999-10-15 | 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 | ||
| 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 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 | ||
| Intermittent Androgen Deprivation in Patients With Stage D2 Prostate Cancer, Phase III [NCT00002651] | Phase 3 | 3,040 participants (Actual) | Interventional | 1995-05-31 | 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 | ||
| Aromatase Inhibitors or Gonadotropin-releasing Hormone Agonists for the Management of Uterine Adenomyosis: A Randomized Controlled Trial [NCT01218581] | Phase 2/Phase 3 | 32 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Precision Platform Study of HR+/ HER2-advanced Breast Cancer Based on SNF Typing (A Prospective, Open-label, Multi-center, Phase II Platform Study) [NCT05594095] | Phase 2 | 140 participants (Anticipated) | Interventional | 2022-12-30 | Recruiting | ||
| Prospective Randomized Controlled Study on the Risk and Clinical Benefit of Chemotherapy and Intensive Endocrine Therapy for Luminal B1 Early-stage Breast Cancer [NCT03373708] | Phase 2/Phase 3 | 200 participants (Anticipated) | Interventional | 2017-12-20 | Not yet recruiting | ||
| Randomized, Multicentre, Phase III Study in Patients With Intermediate-risk T1 T2 Prostate Adenocarcinomas, to Verify the Role of Six Months of Total Androgen Blockade for Two Dosage Levels of Prostate Radiation Therapy (70 Gy and 76 Gy) Versus Prostate R [NCT00223145] | Phase 3 | 600 participants (Actual) | Interventional | 2000-12-31 | Active, not recruiting | ||
| A Phase III Trial of External Beam of Radiotherapy +/- Total Androgen Suppression for High Risk Clinically Organ-Confined Prostate Cancer [NCT00116220] | Phase 3 | 206 participants (Actual) | Interventional | 1995-09-30 | Completed | ||
| Presurgical Treatment With Ribociclib and Letrozole in Patients With Locally Advanced Breast Cancer: the NEOLETRIB Study. [NCT05163106] | Phase 2 | 100 participants (Anticipated) | Interventional | 2022-12-01 | Recruiting | ||
| 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 | ||
| A Phase II Trial of Endocrine Therapy in Combination With OSI-906 (an IGF-1R Inhibitor) and Erlotinib (Tarceva®, an EGFR Inhibitor) in Patients With Hormone-sensitive Metastatic Breast Cancer [NCT01205685] | Phase 2 | 11 participants (Actual) | Interventional | 2010-05-31 | Terminated(stopped due to PI closed study early, all patients experienced severe toxicities and progressed) | ||
| Neuropsychobiological Correlates of Sex-steroid Hormone Manipulation in Healthy Women: a Risk Model for Depression [NCT02661789] | 63 participants (Actual) | Interventional | 2011-01-31 | Completed | |||
| 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 Randomized, Open-label, Parallel, Active-controlled Phase 1 Study to Compare Pharmacokinetics Pharmacodynamics and Safety of Goserelin Acetate Sustained-Release Microspheres for Injection (LY01022) With Zoladex® 10.8mg Following Single Administration in [NCT05856630] | Phase 1 | 24 participants (Anticipated) | Interventional | 2023-05-31 | Not yet recruiting | ||
| Bone Mineral Density Alterations and Correlations With Bone and Muscle Metabolism Parameters During Menstrual Cessation Due to GnRH Therapy and After Menstrual Restoration [NCT04203212] | 41 participants (Actual) | Observational | 2019-10-01 | Completed | |||
| Effect of Goserelin (Zoladex®) in Spinal and Bulbar Muscular Atrophy in Thai Patients [NCT00851461] | Phase 4 | 10 participants (Actual) | Interventional | 2008-04-30 | 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) | ||
| Phase 2 Study Assessing the Safety and Efficacy of a Monthly Dosing Regimen of Ozarelix Versus Goserelin Depot (Zoladex®) in Men With Prostate Cancer [NCT01252693] | Phase 2 | 203 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
| Phase II Study of Neoadjuvant IMC-A12 Combined With Androgen Deprivation Prior to Prostatectomy [NCT00769795] | Phase 2 | 29 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| Goserline Acetate Versus Dienogest in Treatment of Pain Associated With Endometriosis [NCT05013242] | Phase 4 | 40 participants (Anticipated) | Interventional | 2020-12-25 | Recruiting | ||
| A Phase IV, Randomised, Open-label, Multi-centre Study to Assess the Impact on Disease Control, Safety, Patient and Clinician Experience of Changing Patients With Advanced Prostate Cancer From a 3-monthly LHRH Agonist to 6-monthly Injections of Decapeptyl [NCT01673984] | Phase 4 | 27 participants (Actual) | Interventional | 2012-08-31 | Terminated(stopped due to The study was discontinued prematurely by the sponsor due to non-medical reasons) | ||
| 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 | ||
| 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 | ||
| A Phase II Trial of Arimidex Plus Zoladex in the Treatment of Hormone Receptor Positive, Metastatic Carcinoma of the Breast in Premenopausal Women [NCT00186121] | Phase 2 | 35 participants (Actual) | Interventional | 2000-10-31 | Completed | ||
| 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 | ||
| Autonomic and Renal Contributions to Hypertension With Androgen Deprivation Therapy [NCT05700903] | Phase 4 | 228 participants (Anticipated) | Interventional | 2023-09-20 | Recruiting | ||
| Pilot Study to Evaluate the Effects of a New Depot Formulation of Goserelin Acetate 10.8 mg, on Testosterone Levels in Ambulatory Patients With Carcinoma of the Prostate [NCT04060043] | Early Phase 1 | 11 participants (Actual) | Interventional | 2017-02-21 | Completed | ||
| "A Randomized Multicenter Phase II Trial to Evaluate the Effectiveness of Selective Neoadjuvant Treatment According to Immunohistochemical Subtype for HER2 Negative Breast Cancer Patients" [NCT00432172] | Phase 2 | 189 participants (Actual) | Interventional | 2007-04-24 | Completed | ||
| A Phase II Randomized Study of the Combination of Ribociclib Plus Goserelin Acetate With Hormonal Therapy Versus Physician Choice Chemotherapy in Premenopausal or Perimenopausal Patients With Hormone Receptor-positive/ HER2-negative Inoperable Locally Adv [NCT03839823] | Phase 2 | 223 participants (Actual) | Interventional | 2019-02-25 | Completed | ||
| Randomisierte Phase II Studie Zum Einsatz Von Goserelin Und Oralen Kontrazeptiva Zur Reduktion Ovarieller Toxizitäten während Zytostatischer Primärtherapie Bei Fertilen Patientinnen Mit Hodgkin Lymphom in Fortgeschrittenen Stadien [NCT01014507] | Phase 2 | 60 participants (Actual) | Interventional | 2004-01-31 | Completed | ||
| 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 | ||
| A Randomized Phase II Trial on the Addition of Dutasteride to Combined Androgen Blockade Therapy Versus Combined Androgen Blockade Therapy Alone in Patients With Recurrent and/or Metastatic Salivary Duct Carcinoma - DUCT Study [NCT05513365] | Phase 2 | 98 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
| 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 | ||
| Evaluation of the Luteolytic Effect of a Gonadotropin Releasing Hormone (GnRH) Agonist After the Administration of Human Chorionic Gonadotropin (hCG) in the Initial Follicular Phase a Its Influence on the Prognosis of in Vitro Fertilization Treatment [NCT00948805] | Phase 3 | 25 participants (Anticipated) | Interventional | 2009-01-31 | Recruiting | ||
| Phase II Randomized Clinical Trial Comparing 3-D Conformal Radiation Therapy (RT) vs. Intensity Modulated Radiation Therapy in Post- Prostatectomy Prostate Cancer Patients [NCT02678520] | Phase 2 | 0 participants (Actual) | Interventional | 2015-12-31 | Withdrawn(stopped due to PI no longer at institution. Study terminated prior to enrolling subjects.) | ||
| PErsonalized TREatment of High-risk MAmmary Cancer - the PETREMAC Trial [NCT02624973] | Phase 2 | 200 participants (Actual) | Interventional | 2016-04-15 | Active, not recruiting | ||
| GnRHa Combined With hCG and hMG for Treatment of Patients With Non-obstructive Azoospermia: A Single-center Prospective Study in China [NCT02544191] | Phase 2 | 30 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
| The Effect of Androgen Deprivation Therapy on Regulation of Muscle Protein Metabolism and Blood Glucose [NCT03440879] | 23 participants (Actual) | Interventional | 2018-09-21 | Terminated(stopped due to Low recruitment rate) | |||
| Phase II Study of Darolutamide (ODM-201) in Patients With Androgen Receptor-positive Salivary Gland Carcinoma (Discovary Study) [NCT05694819] | Phase 2 | 56 participants (Anticipated) | Interventional | 2020-04-17 | 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 | ||
| Multi-centre, Randomised, Double-blind, Parallel-group Study to Compare Efficacy and Safety Between Anastrozole (ZD1033) and Tamoxifen in Pre- and Post-operative Administration Under Goserelin Acetate Treatment for Premenopausal Breast Cancer Patients [NCT00605267] | Phase 3 | 197 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
| An Open-label, Randomised, Parallel Group, Multicentre Study to Compare ZOLADEX 10.8 mg Given Every 12 Weeks With ZOLADEX 3.6 mg Given Every 4 Weeks in Pre-menopausal Women With Oestrogen Receptor Positive Advanced Breast Cancer [NCT00322348] | Phase 2 | 98 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
| Comparison of Neoadjuvant Aromatase Inhibitors With Ovarian Suppression Versus Chemotherapy in Premenopausal Patients With Hormone Receptor-positive Breast Cancer (COMPETE): a Randomized Phase 3 Trial [NCT02532400] | Phase 3 | 21 participants (Actual) | Interventional | 2016-03-31 | Terminated(stopped due to Hard to enroll expected number of eligible patients.) | ||
| A Randomised Phase III Study for Evaluating the Role of the Addition of Ovarian Function Suppression to Tamoxifen in Young Women With Hormone-Sensitive Breast Cancer Who Remain in Premenopause or Regain Menstruation After Chemotherapy [NCT00912548] | Phase 3 | 1,234 participants (Anticipated) | Interventional | 2009-05-31 | Enrolling by invitation | ||
| A Randomised, Parallel-arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Reduction in International Prostate Symptom Score (IPSS), in Patients With Lower Urinary Tract Symptoms (LUTS) [NCT00831233] | Phase 3 | 42 participants (Actual) | Interventional | 2009-04-30 | Terminated(stopped due to Poor recruitment due to rare targeted population) | ||
| A Randomised, Parallel-arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Volume Reduction of the Prostate in Patients With Prostate Cancer Being Candidates for Medical Castration [NCT00884273] | Phase 3 | 182 participants (Actual) | Interventional | 2009-08-31 | 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 | ||
| A Randomized Comparison of Immediate Versus Deferred Androgen Deprivation Therapy Using Goserelin for Recurrent Prostate Cancer After Radical Radiotherapy. [NCT00439751] | Phase 3 | 79 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| Effect of Increasing Testosterone on Insulin Sensitivity in Men With the Metabolic Syndrome [NCT00438321] | Phase 1 | 66 participants (Actual) | Interventional | 2006-09-30 | Terminated(stopped due to PI relocated) | ||
| PREDIX Luminal B - Neoadjuvant Response-guided Treatment of ER Positive Tumors With High Proliferation or Low Proliferation With Metastatic Nodes. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02603679] | Phase 2 | 181 participants (Actual) | Interventional | 2015-02-28 | 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 | |||
| Phase III Randomized Comparison of Pelvic Radiotherapy Alone vs Pelvic Radiotherapy Plus the LHRH Analogue Goserelin and Cyproterone Acetate in Carcinoma of the Prostate at High Risk for Metastasis [NCT00849082] | Phase 3 | 0 participants | Interventional | 1987-05-31 | Completed | ||
| Phase I Study Evaluating Extended Field Intensity Modulated Radiation Therapy and Docetaxel in Patients With Prostate Cancer Associated With Pelvic Node Metastasis [NCT00482807] | Phase 1 | 9 participants (Actual) | Interventional | 2004-08-31 | Completed | ||
| Protection of Ovarian Function With Goserelin Acetate in Premenopausal Early Breast Cancer Patients Undergoing Adjuvant Chemotherapy: An Open Label, Randomised, Multi-Centre, Phase IIIb Study [NCT00888082] | Phase 3 | 102 participants (Anticipated) | Interventional | Withdrawn | |||
| An Assessment of the Biological and Clinical Effects of Palbociclib (PD 0332991) With Ovarian Suppression and Letrozole in the Neoadjuvant Treatment of Patients With Premenopausal Estrogen-Receptor Positive/HER2-Negative Primary Breast Cancer [NCT03628066] | Phase 2 | 24 participants (Actual) | Interventional | 2018-10-22 | Completed | ||
| The Effects of Adjuvant Zoladex Plus Tamoxifen on Breast Density in Pre- or Peri-menopausal Women With Early-stage Breast Cancer [NCT00827307] | 100 participants (Anticipated) | Interventional | 2008-06-30 | Completed | |||
| Phase III Study of the Comparison of Abarelix Versus Goserelin Plus Bicalutamide in Patients With Advanced or Metastatic Prostate Cancer. A One Year Randomised, Open Label, Multi-Centre Phase III Trial. [NCT00841113] | Phase 3 | 177 participants (Actual) | Interventional | 1999-01-31 | Completed | ||
| 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 | ||
| Phase III, Open-Label Randomized, Parallel, Active-Control Study to Evaluate Efficacy and Safety of Histrelin Subdermal Implant in Patients With Metastatic Prostate Cancer [NCT01394263] | Phase 3 | 59 participants (Actual) | Interventional | 2000-05-31 | Completed | ||
| A PHASE III TRIAL OF THE USE OF LONG TERM TOTAL ANDROGEN SUPPRESSION FOLLOWING NEOADJUVANT HORMONAL CYTOREDUCTION AND RADIOTHERAPY IN LOCALLY ADVANCED CARCINOMA OF THE PROSTATE [NCT00767286] | Phase 3 | 0 participants | Interventional | Completed | |||
| 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 | ||
| 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 | ||
| 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 Randomised, Parallel Arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Prostate Size Reduction in Prostate Cancer Patients of Intermediate-to-high Risk, Who Require Neoadjuvant Hormo [NCT00833248] | Phase 3 | 246 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| A Phase II Clinical Trial Assessing the Safety of an Alternative Dosing Schedule of Palbociclib in Metastatic Hormone Receptor Positive Breast Cancer [NCT03007979] | Phase 2 | 55 participants (Actual) | Interventional | 2017-06-15 | 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 | ||
| A Post-trial Access Roll-over Study to Allow Access to Ribociclib (LEE011) for Patients Who Are on Ribociclib Treatment in Novartis-sponsored Study [NCT05161195] | Phase 4 | 137 participants (Anticipated) | Interventional | 2022-07-07 | Recruiting | ||
| Phase III Randomized Study of Adjuvant Radiotherapy With Versus Without Concurrent Goserelin in Patients Who Have Undergone Surgery for Recurrent or Refractory Prostate Cancer [NCT00423475] | Phase 3 | 743 participants (Actual) | Interventional | 2006-10-31 | 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 | ||
| PREDIX Luminal A - Neoadjuvant Response-guided Treatment of Slowly Proliferating Hormone Receptor Positive Tumors. Part of a Platform of Translational Phase II Trials Based on Molecular Subtypes [NCT02592083] | Phase 2 | 10 participants (Actual) | Interventional | 2015-10-31 | Active, not recruiting | ||
| Long Term Changes in Bone Mineral Density and Fracture Risk in Patients Receiving Androgen Deprivation Therapy for Advanced Prostate Cancer, With Stratification of Treatment Based on Presenting Values [NCT00536653] | 618 participants (Actual) | Interventional | 1999-10-31 | Completed | |||
| Phase II Randomized, Double-blind, Placebo-controlled Study of LEE011(Ribociclib) or Placebo in Combination With Endocrine Therapy for the Treatment of Pre- and Postmenopausal Chinese Women With HR Positive, HER2-negative, Advanced Breast Cancer, Includin [NCT03671330] | Phase 2 | 327 participants (Actual) | Interventional | 2018-08-29 | Active, not recruiting | ||
| A Phase II Neoadjuvant Study of Palbociclib in Combination With Letrozole and Trastuzumab as Neoadjuvant Treatment of Stage II-III ER+ HER2+ Breast Cancer (PALTAN) [NCT02907918] | Phase 2 | 26 participants (Actual) | Interventional | 2017-06-30 | Terminated(stopped due to Futility) | ||
| [NCT00286351] | Phase 4 | 20 participants | Interventional | 2005-01-31 | 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 | ||
| ASP3550 Phase III Study - An Open-Label, Active-Controlled, Parallel-Arm Study, Comparing ASP3550 With Goserelin Acetate in Patients With Prostate Cancer - [NCT01964170] | Phase 3 | 234 participants (Actual) | Interventional | 2013-08-13 | Completed | ||
| A Phase II Trial of Neoadjuvant PD 0332991, a Cyclin-Dependent Kinase (Cdk) 4/6 Inhibitor, in Combination With Anastrozole in Women With Clinical Stage 2 or 3 Estrogen Receptor Positive and HER2 Negative Breast Cancer [NCT01723774] | Phase 2 | 84 participants (Actual) | Interventional | 2013-04-10 | 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 | ||
| 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 | ||
| A Multicenter, Randomized, Open-Label Phase Ⅲ Trial to Compare Efficacy and Safety of Goserelin Acetate Sustained-Release Microspheres for Injection (LY01005) and ZOLADEX® in Patients With Prostate Cancer [NCT04563936] | Phase 3 | 290 participants (Actual) | Interventional | 2020-01-06 | Completed | ||
| 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 | ||
| 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 | ||
| A Randomized Study Comparing Goserelin or Expectant Management Following Laparoscopic Surgery for Advanced Endometriosis [NCT00654524] | Phase 4 | 60 participants (Anticipated) | Interventional | 2008-03-31 | Recruiting | ||
| 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 | ||
| A Multicenter, Randomized Clinical Investigation of Trelstar Versus Continued Therapy in Patients Receiving Lupron or Zoladex for Advanced Prostate Cancer [NCT02749825] | Phase 4 | 41 participants (Actual) | Interventional | 2002-09-30 | Terminated(stopped due to Withdrawal of funding support) | ||
| Phase II Randomized Study of Abiraterone Acetate Plus ADT Versus APALUTAMIDE Versus Abiraterone and APALUTAMIDE in Patients With Advanced Prostate Cancer With Non-castrate Testosterone Levels [NCT02867020] | Phase 2 | 128 participants (Actual) | Interventional | 2017-10-11 | Completed | ||
| An Open Label, Randomised, Parallel Group, Multicentre Study to Compare ZOLADEX™ 10.8 mg Given Every 12 Weeks With ZOLADEX 3.6 mg Given Every 4 Weeks in Pre-menopausal Women With Oestrogen Receptor Positive Advanced Breast Cancer. [NCT01073865] | Phase 3 | 222 participants (Actual) | Interventional | 2010-02-26 | Completed | ||
| An Open-Label, Multi-Centre, Randomised, Parallel-Arm One-Year Trial, Comparing the Efficacy and Safety of Degarelix Three-Month Dosing Regimen With Goserelin Acetate in Patients With Prostate Cancer Requiring Androgen Deprivation Therapy [NCT00946920] | Phase 3 | 859 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Efficacy of Laparoscopic Surgery Combined With GnRH-a in the Treatment of Endometriosis Associated Infertility: A Multicenter, Prospective, Randomized-control-trial [NCT02779387] | 1,184 participants (Anticipated) | Interventional | 2016-05-31 | Not yet recruiting | |||
| Neoadjuvant Estradiol or Androgen Deprivation in Clinically Localized Prostate Cancer [NCT00167648] | Phase 2 | 17 participants (Actual) | Interventional | 2005-03-31 | Completed | ||
| A Phase II Trial of Endocrine Therapy in Combination With OSI-906 (an IGF-1R Inhibitor) With or Without Erlotinib (Tarceva, an EGFR Inhibitor) in Patients With Hormone-sensitive Metastatic Breast Cancer. [NCT01013506] | Phase 2 | 0 participants (Actual) | Interventional | 2009-08-31 | Withdrawn(stopped due to Study was abandoned before opening to accrual. Replaced by another study.) | ||
| An Open, Multicenter, Randomized Controlled Clinical Study of Chidamide Combined With Exemestane (+/- Goserelin) Versus Neoadjuvant Chemotherapy in Patients of Stage II-III HR-positive/HER2-negative Breast Cancer [NCT05253066] | Phase 2/Phase 3 | 130 participants (Anticipated) | Interventional | 2022-02-25 | Not yet recruiting | ||
| A Phase II, Multicenter, Randomized, Open-label Study to Evaluate the Safety and Efficacy of 400 mg of Ribociclib in Combination With Non-steroidal Aromatase Inhibitors for the Treatment of Pre- and Postmenopausal Women With Hormone Receptor-positive, HER [NCT03822468] | Phase 2 | 376 participants (Actual) | Interventional | 2019-06-11 | Active, not recruiting | ||
| 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 | ||
| A Phase II Study of Goserelin Plus Anastrozole for the Treatment of Male Patients With Hormone-Receptor Positive Metastatic or Recurrent Breast Cancer [NCT00217659] | Phase 2 | 0 participants (Actual) | Interventional | 2005-09-30 | Withdrawn(stopped due to poor accrual) | ||
| A Randomized, Open-label and Parallel Phase I Study to Compare Pharmacokinetics, Pharmacodynamics and Safety of Goserelin Acetate Sustained-Release Microspheres for Injection (LY01005) and ZOLADEX® Following Multiple Administration in Patients With Prosta [NCT05140512] | Phase 1 | 23 participants (Actual) | Interventional | 2021-02-04 | Completed | ||
| A Multicenter, Randomized, Open-Label Phase Ⅲ Trial to Compare Efficacy and Safety of Goserelin Acetate Sustained-Release Microspheres for Injection (LY01005) and ZOLADEX® in Patients With Breast Cancer [NCT05110170] | Phase 3 | 188 participants (Actual) | Interventional | 2020-10-15 | Completed | ||
| A Randomized Trial Of Raloxifene Plus Zoladex For Prevention Of Breast Cancer [NCT00031850] | 150 participants (Anticipated) | Interventional | 2000-03-31 | Completed | |||
| Phase III Randomized Study Of Adjuvant Hormonal Therapy With And Without Docetaxel And Estramustine In Patients With Advanced Prostate Cancer Or With A High Risk Of Relapse [NCT00055731] | Phase 3 | 413 participants (Actual) | Interventional | 2002-11-14 | Completed | ||
| 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 | ||
| A Phase Ib Trial of MK-2206 (an AKT Inhibitor) in Combination With Endocrine Therapy in Patients With Hormone Receptor-Positive Breast Cancer [NCT01240928] | Phase 1 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to Funding not available, study did not open to accrual and will not open in future) | |||
| 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 | ||
| Density Lowering Effect of Ovarian Function Suppression in Premenopausal Breast Cancer Patients Who Had no Density Change With One Year of Tamoxifen Treatment [NCT03664895] | Phase 3 | 224 participants (Anticipated) | Interventional | 2018-09-03 | Recruiting | ||
| A Randomized Phase III Trial of Endocrine Therapy Plus Entinostat/Placebo in Patients With Hormone Receptor-Positive Advanced Breast Cancer [NCT02115282] | Phase 3 | 608 participants (Actual) | Interventional | 2014-03-29 | Active, not recruiting | ||
| A Phase II Study of Ovarian Function Suppression And ExemesTane With or Without PalbocIclib in PreMenopausal Women With ER Positive / HER-2 Negative MetAstatic Breast Cancer [NCT02917005] | Phase 2 | 160 participants (Anticipated) | Interventional | 2019-05-07 | 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 II Non-randomized, Parallel Group Study of Goserelin or Leuprorelin Plus Letrozole in Premenopausal Patients Versus Letrozole Alone in Postmenopausal Patients With Metastatic Breast Cancer [NCT00532272] | Phase 2 | 78 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| Comparison of the Therapeutic Effects of Vaginal Repair and Vaginal Repair Combined With GnRHa in the Treatment of Cesarean Scar Diverticula: a Randomized Clinical Trial [NCT02932761] | 220 participants (Anticipated) | Interventional | 2016-11-30 | Not yet recruiting | |||
| Medical Ethics Committee of Nanjing Drum Tower Hospital Affiliated to Medical School of Nanjing University [NCT04356430] | Phase 2 | 75 participants (Anticipated) | Interventional | 2019-04-01 | Active, not recruiting | ||
| A Multi-centre, Single-arm, Prospective Study to Assess Efficacy and Safety of Neoadjuvant Hormone Therapy Using Zoladex (Goserelin) and Casodex (Bicalutamide) in Patients With Advanced Prostate Cancer Undergoing Radical Prostatectomy. [NCT03971110] | Phase 4 | 9 participants (Actual) | Interventional | 2021-01-28 | Terminated(stopped due to Due to the limited potential patients pool, the enrollment goal could not be achieved. After review and communication, the decision to teminate study was made.) | ||
| 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 | ||
| A Pilot Study of Hormonal Therapy Combined With Central Memory T Cells (Tcm) for Patients With Advanced Prostate Cancer [NCT03587285] | Phase 1/Phase 2 | 11 participants (Actual) | Interventional | 2018-09-23 | Active, not recruiting | ||
| Phase III Randomized Study of Adjuvant Therapy With Tamoxifen vs Endocrine Ablation vs Tamoxifen Plus Endocrine Ablation vs No Adjuvant Therapy in Patients Under Age 50 With Operable Breast Cancer [NCT00002460] | Phase 3 | 0 participants | Interventional | 1987-09-30 | Active, not recruiting | ||
| PROTOCOL FOR THE SCOTTISH PREMENOPAUSAL CHEMO-ENDOCRINE TRIAL [NCT00002580] | Phase 3 | 1,000 participants (Anticipated) | Interventional | 1993-06-30 | 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 | ||
| Longitudinal, Randomized, Open and Prospective Clinical Trial to Evaluate the Efficacy of Continuous vs Intermittent Maximum Androgen Blockade (CMAB vs IMAB) With Goserelin-Bicalutamide Combination in the Treatment of Hormonal naïve With Metastatic Prosta [NCT00255268] | Phase 4 | 15 participants (Anticipated) | Interventional | 2004-08-31 | Withdrawn | ||
| Randomized Phase III Trial Comparing an Association of Hormonal Treatment and Docetaxel Versus the Hormonal Treatment Alone in Metastatic Prostate Cancers [NCT00104715] | Phase 3 | 385 participants (Actual) | Interventional | 2004-10-18 | Completed | ||
| A Randomized-Controlled Trial of Transcutaneous Oestrogen Patches Versus LHRH Agonists in Prostate Cancer [NCT00303784] | Phase 3 | 2,200 participants (Anticipated) | Interventional | 2006-03-31 | Recruiting | ||
| 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 | ||
| Abnormal Uterine Bleeding in Women With Uterine Leiomyomas: Open Randomized Clinical Trial Of Non Inferiority Between Oral Dienogest, Oral Desogestrel and Subcutaneous Goserelin [NCT01738724] | Phase 4 | 14 participants (Actual) | Interventional | 2012-01-31 | Terminated(stopped due to PI went for a post-doc course and when he came back he moved for another job) | ||
| A Prospective, Single-Arm Study to Evaluate the Efficacy and Safety of Zoladex 3.6mg Combined With CEF Chemotherapy as Neo-Adjuvant Therapy in Hormone Responsive, Premenopausal, Operable Breast Cancer [NCT00488722] | 0 participants | Interventional | 2007-04-30 | 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 | ||
| An Open-label, Multi-Centre, Extension Trial, Evaluating the Long-Term Progression-Free Survival of Degarelix or Goserelin Three-Month Dosing Regimens in Patients With Prostate Cancer Requiring Androgen Deprivation Therapy [NCT01242748] | Phase 3 | 288 participants (Actual) | Interventional | 2010-10-31 | Terminated(stopped due to Inadequate recruitment resulting in a too low patient number for collection of long term efficacy data.) | ||
| 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 | ||
| Docetaxel, Estramustine and Short Term Androgen Withdrawal for Patients With a Rising PSA After Definitive Local Treatment [NCT00165399] | Phase 2 | 62 participants (Actual) | Interventional | 2004-03-31 | 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 | ||
| Pilot Phase II Trial of Bevacizumab in Combination With Hormonal and Radiotherapy in Patients With High-Risk Prostate Cancer [NCT00348998] | Phase 2 | 18 participants (Anticipated) | Interventional | 2006-04-30 | Active, not recruiting | ||
| Phase II Trial of MK-2206 (an AKT Inhibitor) in Combination With Endocrine Therapy in Patients With Hormone Receptor Positive Breast Cancer [NCT01240941] | Phase 2 | 0 participants (Actual) | Interventional | 2011-02-28 | Withdrawn(stopped due to Funding was not available) | ||
| Administration During Chemotherapy to Reduce Ovarian Failure Following Chemotherapy in Early Stage, Hormone-Receptor Negative Breast Cancer [NCT01530607] | Phase 3 | 416 participants (Actual) | Interventional | 2009-11-30 | 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 Phase II Trial Of Oral Bicalutamide With Subcutaneous Goserelin In Patients With Epithelial Ovarian, Fallopian Tube, Or Peritoneal Carcinoma In Second Or Greater Remission [NCT00012090] | Phase 2 | 0 participants | Interventional | 2000-09-30 | Completed | ||
| Randomized Phase III Step-Up Study On Initial Antiandrogen Monotherapy In Comparison With Watchful Waiting In Asymptomatic T1-3 Any G (Any Gleason) NO or Nx M0 Prostate Cancer Patients Without Local Treatment With Curative Intent [NCT00014586] | Phase 3 | 110 participants (Actual) | Interventional | 2001-01-31 | Terminated(stopped due to low accrual) | ||
| Randomized And Multicentric Phase III Study Evaluating The Benefit By Using A Chemotherapy With FEC 100 And Docetaxel In Non Metastatic Breast Cancer Which Has Relapsed After A Conservative Surgery [NCT00053911] | Phase 3 | 0 participants | Interventional | 2002-11-30 | Terminated | ||
| Phase III Randomized Trial Study Comparing the Outcome of High-Dose IMRT (86.4 GY) Alone With IMRT to 75.6 GY Plus Neoadjuvant/Adjuvant Androgen Deprivation in Patients With High Grade Intermediate Risk and Unfavorable Risk Prostate Cancer [NCT00067015] | Phase 3 | 3 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
| A Phase II Study of the Combination of Exemestane and Goserelin in Premenopausal Women With Metastatic Hormone Receptor Positive Breast Cancer [NCT00010010] | Phase 2 | 0 participants | Interventional | 2000-06-30 | Completed | ||
| Three Dimensional Conformal Radiotherapy / Intensity Modulated Radiotherapy Alone Vs Three Dimensional Conformal Therapy / Intensity Modulated Radiotherapy Plus Adjuvant Hormonal Therapy In Localized T1b-c, T2a, N0, M0 Prostatic Carcinoma. A Phase III Ran [NCT00021450] | Phase 3 | 819 participants (Actual) | Interventional | 2001-04-30 | Completed | ||
| A Randomized Phase III Trial Comparing FEC-Chemotherapy vs. EC-Doc-Chemotherapy in Patients With Primary Breast Cancer [NCT00047099] | Phase 3 | 446 participants (Anticipated) | Interventional | 2001-08-31 | Completed | ||
| Evaluation of Response Rate to Pre-Operative Docetaxel + Herceptin Study Part A and Docetaxel Study Part B in Locally Advanced Breast Cancer Patients, Stratified by HER2-Status Trial - PHASE II [(Herceptin Docetaxel Neoadjuvant) HEDON] [NCT00398489] | Phase 2 | 94 participants (Anticipated) | Interventional | 2006-10-31 | Active, not recruiting | ||
| Prospective Randomized Multicenter Study to Prevent Chemotherapy Induced Ovarian Failure With the GnRH-Agonist Goserelin in Young Hormone Insensitive Breast Cancer Patients Receiving Anthracycline Containing (Neo-)Adjuvant Chemotherapy [NCT00196846] | Phase 2 | 62 participants (Anticipated) | Interventional | 2005-03-31 | Completed | ||
| Phase III Randomized Study of a Goserelin Acetate for Preservation of Ovarian Function in Patients With Primary Breast Cancer (PBC) [NCT00429403] | Phase 3 | 1 participants (Actual) | Interventional | 2006-08-31 | Terminated(stopped due to Study stopped due to low accrual.) | ||
| A Randomized Phase II Study of Tecemotide in Combination With Standard Androgen Deprivation Therapy and Radiation Therapy for Untreated, Intermediate and High Risk Prostate Cancer Patients [NCT01496131] | Phase 2 | 28 participants (Actual) | Interventional | 2011-10-24 | Completed | ||
| Neoadjuvant Hormone and Radiation Therapy Followed by Radical Prostatectomy in Patients With High-Risk Locally Advanced Prostate Cancer and Biomarker Research [NCT04894188] | 38 participants (Anticipated) | Interventional | 2022-01-27 | Recruiting | |||
| 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 | ||
| A Randomized and Open-label Study to Assess Pharmacokinetics, Pharmacodynamics and Safety of LY01005 Versus Goserelin Comparator (ZOLADEX®) Following a Single Administration in Patients With Prostate Cancer [NCT03450109] | Phase 1 | 19 participants (Actual) | Interventional | 2017-12-22 | Completed | ||
| An Open, Phase II Trial Assessing the Objective Response Rate After Combination of Arimidex® 1mg Per os/Day and Zoladex® 3.6 mg Sub Cut/Monthly as 1st Treatment for Premenopausal Receptor Positive Advanced or Metastatic Breast Cancer [NCT00235937] | Phase 2 | 45 participants (Anticipated) | Interventional | 2001-12-31 | Completed | ||
| Intermittent Vs Continuous Androgen Deprivation in Patients With Advanced Prostate Cancer [NCT00293670] | Phase 4 | 573 participants | Interventional | 1997-05-31 | Active, not 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 | ||
| A Randomised Pilot Study to Evaluate the Effect(s) of Casodex 150 mg and Zoladex 3.6 mg on Pathological and Genomic Tumour Markers in Subjects Undergoing Radical Prostatectomy for Localised Prostate Carcinoma [NCT00293696] | Phase 4 | 30 participants (Actual) | Interventional | 2004-10-31 | Completed | ||
| An Open-label, Randomized, Parallel Group, Multicentre Study to Compare Oestradiol Suppression Between ZOLADEX 10.8 mg Depot Given 3 Monthly and ZOLADEX 3.6 mg Depot Given Monthly in Pre-menopausal Patients With ER Positive Early Breast Cancer [NCT00303524] | Phase 2 | 170 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
| 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 | ||
| A Randomized, Multicenter, Double-blind Phase 3 Study of Amcenestrant (SAR439859) Plus Palbociclib Versus Letrozole Plus Palbociclib for the Treatment of Patients With ER (+), HER2 (-) Breast Cancer Who Have Not Received Prior Systemic Anti-cancer Treatme [NCT04478266] | Phase 3 | 1,068 participants (Actual) | Interventional | 2020-10-14 | Terminated(stopped due to The study was terminated based on the review by an independent data monitoring committee of the prespecified interim analysis of the Phase 3 AMEERA-5 efficacy data. No new safety signals were observed.) | ||
| A Prospective, Randomised, Multi-centre Phase II Study Evaluating the Adjuvant, Neoadjuvant or Palliative Treatmant With Tamoxifen +/- GnRH Analogue Versus Aromatase Inhibitor + GnRH Analogue in Male Breast Cancer Patients [NCT01638247] | Phase 3 | 56 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| Neoadjuvant Endocrine Therapy in Breast Cancer. Real Clinical Practice in Russia [NCT05800197] | 300 participants (Anticipated) | Observational | 2014-04-15 | Recruiting | |||
| A Phase III,Randomized,Open Label Study Comparing Simultaneous Versus Sequential Use of Adjuvant Chemotherapy and GnRHa up to 2-3 Years for ≤ 45 Year Old Pre-menopausal Hormone Receptor-positive Breast Cancer [NCT01712893] | Phase 3 | 216 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| An Open-label, Multi-centre, Randomised, Parallel-group Trial, Comparing Efficacy and Safety of Degarelix One-month Dosing Regimen With Goserelin in Chinese Patients With Prostate Cancer Requiring Androgen Ablation Therapy [NCT01744366] | Phase 3 | 285 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| A Phase I Pilot Study of Samarium-153 Combined With Neoadjuvant Hormonal Therapy and Radiation Therapy in Men With Locally Advanced Prostate Cancer [NCT00328614] | Phase 1 | 32 participants (Actual) | Interventional | 2003-03-31 | 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 | ||
| IVF Outcome in Patients With Peritoneal Endometriosis. The Impact of a Hormonal Treatment of the Endometriosis Prior to the IVF on the Pregnancy Rates. [NCT01682642] | Phase 4 | 120 participants (Actual) | Interventional | 2012-03-31 | 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 | ||
| Fudan University Shanghai Cancer Center Breast Cancer Precision Platform Series Study- Neoadjuvant Therapy (FASCINATE-N) [NCT05582499] | Phase 1/Phase 2 | 716 participants (Anticipated) | Interventional | 2022-11-01 | Recruiting | ||
| Effect of Goserelin on the Protection of Ovarian Reserve During (Neo)Adjuvant Chemotherapy for Young Breast Cancer Patients: A Prospective Cohort Trial [NCT02430103] | 240 participants (Anticipated) | Observational | 2015-12-25 | 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 | ||
| 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 | ||
| The Regulation of Skeletal Muscle Protein Synthesis by Systemic Hormones and Its Influence on Ageing and Anabolic Resistance [NCT03054168] | Phase 3 | 34 participants (Actual) | Interventional | 2016-12-15 | Active, not recruiting | ||
| COMPARISON OF A NEW FORMULATION OF GOSERELIN (Pepti 3.6 mg) to Zoladex® 3.6 mg IN PATIENTS WITH DYSFUNCTIONAL UTERINE BLEEDING REQUIRING ENDOMETRIAL ABLATION. [NCT04428684] | Phase 1 | 80 participants (Actual) | Interventional | 2018-10-29 | Completed | ||
| Prospective Phase II Randomized Trial of Evaluating the Effect of Adding LHRH Analogue to the Neoadjuvant Chemotherapy Treatment of Triple Negative Breast Cancer on Pathologic Complete Response (pCR) Rates [NCT03444025] | Phase 2 | 180 participants (Anticipated) | Interventional | 2018-03-31 | Not yet recruiting | ||
| 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 | ||
| 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 | ||
| Dose-Response of Gonadal Steroids and Bone Turnover in Older Men [NCT00114114] | 177 participants (Actual) | Interventional | 2004-09-30 | 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 | ||
| A Randomized, Phase II Study for Premenopausal Metastatic or Locally Advanced Breast Cancer Patients: Capivasertib, Goserelin, Fulvestrant With/Without Durvalumab, Versus Goserelin, Fulvestrant, and Durvalumab, Versus Goserelin/ Fulvestrant. [NCT05720260] | Phase 2 | 56 participants (Anticipated) | Interventional | 2023-01-17 | Recruiting | ||
| Pilot Phase II Trial of Bevacizumab in Combination With Hormonal and Radiotherapy in Patients With High-Risk Prostate Cancer [NCT00349557] | Phase 2 | 18 participants (Anticipated) | Interventional | 2006-04-30 | Completed | ||
| Ovarian Protection Trial In Premenopausal Breast Cancer Patients [OPTION] [NCT00427245] | Phase 3 | 400 participants (Anticipated) | Interventional | 2004-08-31 | Completed | ||
| Effect of Increasing Testosterone on Insulin Sensitivity in Men With the Metabolic Syndrome [NCT00433173] | 72 participants (Anticipated) | Interventional | 2006-05-31 | Suspended(stopped due to Primary investigator is taking a leave of absence) | |||
| Phase II Trial of Androgen Deprivation Therapy (ADT) and Pembrolizumab for Advanced Stage Androgen Receptor-positive Salivary Gland Carcinoma: Big Ten Cancer Research Consortium BTCRC-HN17-111 [NCT03942653] | Phase 2 | 20 participants (Anticipated) | Interventional | 2019-05-30 | Recruiting | ||
| 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 | ||
| Effect of Increasing Testosterone Levels on Insulin Sensitivity in Men With the Metabolic Syndrome [NCT00382057] | Phase 2 | 72 participants (Anticipated) | Interventional | 2006-05-31 | Withdrawn | ||
| 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 | ||
| 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 | ||
| 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 | ||
| A Randomized Phase III Study Comparing Cyclophosphamide + Methotrexate + Fluorouracil vs. Goserelin + Tamoxifen in Premenopausal, Hormone Receptor-positive, Lymph Node-positive or -Negative Patients [NCT00309478] | Phase 3 | 1,099 participants (Actual) | Interventional | 1990-12-31 | Completed | ||
| Tamoxifen Versus Anastrozole, Alone or in Combination With Zoledronic Acid, in Premenopausal, Hormone Receptor-positive Breast Cancer Patients (Stage I, II) [NCT00295646] | Phase 3 | 1,803 participants (Actual) | Interventional | 1999-06-30 | 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 Multicenter, Randomized, Double-blind, Placebo-controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of FCN-437c Versus Placebo in Combination With Letrozole or Anastrozole ± Goserelin in Women With HR-positive and HER2-negative Advanc [NCT05439499] | Phase 3 | 434 participants (Anticipated) | Interventional | 2022-03-02 | Recruiting | ||
| A Multicenter, Randomized, Double-blind, Placebo-controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of FCN-437c Versus Placebo Combined With Fulvestrant ± Goserelin in Women With HR+ and HER2- Advanced Breast Cancer [NCT05438810] | Phase 3 | 312 participants (Anticipated) | Interventional | 2022-01-18 | Recruiting | ||
| A Single-center, Phase II Neoadjuvant Study of Abiraterone Acetate in the Treatment of Intraductal Carcinoma of the Prostate [NCT04736108] | Phase 2 | 50 participants (Anticipated) | Interventional | 2021-05-31 | Not yet recruiting | ||
| 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 | ||
| 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) | ||
| Maximal Suppression of the Androgen Axis in Clinically Localized Prostate Cancer [NCT00298155] | Phase 2 | 35 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
| A Multicenter，Prospective Clinical Trial for Reducing Remaining Submucous Fibroids Volume and Preventing Recurrence by Treating With GnRH Analogues or Mifepristone After Transcervical Resection of Type I-II Myoma [NCT05898321] | 294 participants (Anticipated) | Interventional | 2023-06-01 | Not yet recruiting | |||
| Randomized Trial of Neoadjuvant Endocrine Therapy Versus Chemotherapy in Premenopausal Patients With Estrogen Receptor-Positive HER2 Negative Breast Cancer [NCT02535221] | Phase 3 | 234 participants (Anticipated) | Interventional | 2015-07-29 | Recruiting | ||
| 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 | ||
| Effects of GnRHa on Ovarian Function Against Chemotherapy-induced-gonadotoxicity in Women With Breast Cancer in China [NCT02518191] | Phase 3 | 345 participants (Actual) | Interventional | 2015-09-01 | Completed | ||
| Phase II Study of Neoadjuvant Androgen Deprivation Therapy Plus Abiraterone With or Without Apalutamide for Patients With High-Risk Localized Prostate Cancer Prior to Radical Prostatectomy [NCT02789878] | Phase 2 | 64 participants (Actual) | Interventional | 2019-01-24 | Completed | ||
| Neoadjuvant Study of Targeting ROS1 in Combination With Endocrine Therapy in Invasive Lobular Carcinoma of the Breast [NCT04551495] | Phase 2 | 65 participants (Anticipated) | Interventional | 2021-01-14 | 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 Trial of Neoadjuvant MK-2206 in Combination With Either Anastrozole if Postmenopausal or Anastrozole and Goserelin if Premenopausal in Women With Clinical Stage 2 or 3 PIK3CA Mutant Estrogen Receptor Positive and HER2 Negative Invasive Breast C [NCT01776008] | Phase 2 | 16 participants (Actual) | Interventional | 2013-01-31 | Terminated(stopped due to Study did not pass Stage 1 interim analysis.) | ||
| 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 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 | ||
| 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) | ||
| An Open, Randomized, Two-way Cross-over Phase I Study to Compare the Bioavailability, Safety and Tolerability of Single s.c. Doses of 300 IU XM17 With 300 IU Gonal-f® in 36 Healthy, Down-regulated Young Women [NCT02592031] | Phase 1 | 49 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Phase Ib Dose Escalation Study of the Combination of LEE011 With Letrozole and Dose Expansion of LEE011 With Hormonal Therapy for the Treatment of Pre-(With Goserelin) and Postmenopausal Women With Hormone Receptor Positive, HER2-negative, Advanced Brea [NCT02333370] | Phase 1 | 88 participants (Actual) | Interventional | 2015-02-04 | 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 | ||
| Endocrine Treatment Alone as Primary Treatment for Elderly Patients With Estrogen Receptor Positive Operable Breast Cancer and Low Recurrence Score [NCT02476786] | Phase 2 | 50 participants (Anticipated) | Interventional | 2017-01-17 | Recruiting | ||
| Docetaxel Followed by Radical Prostatectomy in Patients With High Risk Localized Prostate Cancer [NCT01250717] | Phase 2 | 28 participants (Actual) | Interventional | 2001-01-31 | Completed | ||
| A Multisite International Collaborative Phase 2 Study of Neoadjuvant Goserelin and a Non-steroidal Aromatase Inhibitor for Premenopausal Women With Estrogen Receptor Positive HER2 Negative Clinical Stage 2 and 3 Breast Cancer [NCT01368263] | Phase 2 | 8 participants (Actual) | Interventional | 2011-09-30 | Terminated(stopped due to Due to funding source and lack of accrual) | ||
| 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 | ||
| 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 | |||
| Neoadjuvant Treatment of Breast Cancer - a Prospective Observational Study, PANnon ONCology (PANONC) Group Non-commercial Clinical Trial [NCT05131893] | 300 participants (Anticipated) | Observational [Patient Registry] | 2022-03-31 | Not yet recruiting | |||
| Phase I Dose-Escalation Study of Combination of Gedatolisib (a Dual Inhibitor of PI3-K and mTOR) With Palbociclib and Faslodex in the Neoadjuvant Setting in Previously Untreated Patients With ER+/HER2- Breast Cancer [NCT02626507] | Phase 1 | 18 participants (Anticipated) | Interventional | 2016-01-31 | Active, not recruiting | ||
| 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 | ||
| Gonadotropin-Releasing Hormone Agonist for the Preservation of Ovarian Function During Chemotherapy in Premenopausal Breast Cancer [NCT02483767] | Phase 3 | 98 participants (Actual) | Interventional | 2015-06-30 | 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 | ||
| Prevention of Chemotherapy-Induced Ovarian Failure With Goserelin in Premenopausal Lymphoma Patients [NCT04536467] | Phase 2 | 80 participants (Anticipated) | Interventional | 2019-03-01 | Enrolling by invitation | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
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 |
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 |
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 |
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 |
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 |
This outcome was scored on a scale of 0 to 100, with higher scores indicating better functioning. Change from Baseline in SF-36 Score at 3 Months (NCT00002651)
Timeframe: 3 months
| Intervention | units on a scale (Mean) |
|---|---|
| Continuous Hormonal Therapy | -1.74 |
| Intermittent Hormonal Therapy | 0.09 |
Non-inferiority test to determine if intermittent combined androgen deprivation (CAD) overall survival is not substantially worse than continuous CAD overall survival. Specifically, the trial is designed for a one-sided test of the hypothesis that the hazard ratio of intermittent CAD to continuous CAD is 1.2. The assumptions used to compute the trial size are an overall type I error rate of 0.05 and a type II error of 0.10 (power = 0.9). (NCT00002651)
Timeframe: Up to 15 years
| Intervention | years (Median) |
|---|---|
| Consolidation Arm I | 5.8 |
| Consolidation Arm II | 5.1 |
"This outcome was assessed by having patients report whether their interest in sexual activities was very high, high, or moderate (a score of 1) or low or very low (a score of 0). This outcome measure is reporting a change from baseline in the percentage of participants with High Libido at 3 months. High Libido is defined as very high, high or moderate interest in sexual activities." (NCT00002651)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Continuous Hormonal Therapy | -2 |
| Intermittent Hormonal Therapy | 16 |
This outcome was assessed by having patients report whether they had erectile dysfunction (a score of 1) or no erectile dysfunction (a score of 0). This analysis looks at change from Baseline to 3 Months. (NCT00002651)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Continuous Hormonal Therapy | 2 |
| Intermittent Hormonal Therapy | -7 |
This outcome was scored on a scale of 0 to 100, with higher scores indicating better functioning. Change from Baseline in SF-36 Score at 3 Months (NCT00002651)
Timeframe: 3 months
| Intervention | units on a scale (Mean) |
|---|---|
| Continuous Hormonal Therapy | -0.95 |
| Intermittent Hormonal Therapy | 1.92 |
This outcome was scored on a scale of 0 to 100, with higher scores indicating better functioning. This analysis looks at mean change from Baseline score to 3 Months. (NCT00002651)
Timeframe: 3 months
| Intervention | units on a scale (Mean) |
|---|---|
| Continuous Hormonal Therapy | -1.42 |
| Intermittent Hormonal Therapy | -0.11 |
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 |
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 |
Number of patients with adverse events that are related to study drug (NCT00004124)
Timeframe: Up to 22 months from registration
| Intervention | Participants (Number) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Abdominal pain/cramping | Abscess | Alkaline phosphatase increase | Allergic reaction | Allergic rhinitis | Alopecia | Anal incontinence | Anemia | Anorexia | Anxiety/agitation | Apnea | Arrhythmia, NOS | Arthralgia | Arthritis | Ataxia (incoordination) | Bilirubin increase | Blurred vision | Bone pain | Bruising | CPK increase | Cardiac ischemia/infarction | Cardiovascular-other | Cataract | Cerebrovascular ischemia | Chest pain,not cardio or pleur | Conduction abnormality/block | Confusion | Conjunctivitis | Constipation/bowel obstruction | Cough | Creatinine increase | Cushingoid appearance | Dehydration | Depression | Diarrhea without colostomy | Dizziness/light headedness | Dry eye | Dry skin | Dysmenorrhea | Dyspepsia/heartburn | Dyspnea | Dysuria | Ear-other | Edema | Endocrine-other | Epistaxis | Erectile impotence | Eryth/rash/eruption/desq, NOS | Esophagitis/dysphagia | Eye-other | Fatigue/malaise/lethargy | Febrile neutropenia | Feminization of male | Fever without neutropenia | Fever, NOS | Flatulence | Flu-like symptoms-other | Flushing | GGT increase | GI Mucositis, NOS | GI-other | GU-other | Gastritis | Gastritis/ulcer, NOS | Glaucoma | Gynecomastia | Headache | Hematologic-other | Hematuria | Hemolysis | Hemoptysis | Hemorrhage-other | Hiccoughs | Hot flashes | Hypercalcemia | Hypercholesterolemia | Hyperglycemia | Hyperkalemia | Hypermagnesemia | Hypernatremia | Hypertension | Hypertriglyceridemia | Hypoalbuminemia | Hypocalcemia | Hypoglycemia | Hypokalemia | Hypomagnesemia | Hyponatremia | Hypotension | Hypothyroidism | Hypoxia | Incontinence | Infection w/o 3-4 neutropenia | Infection with 3-4 neutropenia | Infection, unk ANC | Inner ear-hearing loss | Insomnia | Invol. movement/restlessness | Joint,muscle,bone-other | LVEF decrease/CHF | Leukopenia | Libido loss | Local injection site reaction | Lung-other | Lymphopenia | Male infertility | Melena/ GI bleeding | Memory loss | Metabolic-other | Middle ear-hearing loss/otitis | Mood/consciousness change, NOS | Mouth dryness | Muscle weakness (not neuro) | Myalgia | Myalgia/arthralgia, NOS | Myocarditis | Nail changes | Nausea | Neuro-other | Neuropathic pain | Neutropenia/granulocytopenia | PRBC transfusion | Pain-other | Palpitations | Pelvic pain | Pericar. effusion/pericarditis | Personality/behavioral change | Phlebitis | Pigmentation changes/yellowing | Pleural effusions | Pneumonitis/infiltrates | Proctitis | Proteinuria | Pruritus | RT-GI mucositis, NOS | RT-focal dermatitis, NOS | RT-late bladder morbidity | RT-late intestinal morbidity | RT-pain | Rash/desquamation | Rectal bleeding/hematochezia | Rectal/perirectal pain | Respiratory infect w/o neutrop | Respiratory infection, unk ANC | Rigors/chills | SGOT (AST) increase | SGPT (ALT) increase | Salivary change, NOS | Second primary | Seizures | Sensory neuropathy | Sexual/reproductive-other | Sinus bradycardia | Skin-other | Speech impairment | Stomatitis/pharyngitis | Supraventricular arrhythmia | Surgery-wound infection | Sweating | Syncope | Taste disturbance | Tearing | Thrombocytopenia | Thrombosis/embolism | Tremor | Troponin T (cTnT) increase | Urinary frequency/urgency | Urinary retention | Urinary tr infect w/ neutrop | Urinary tr infect w/o neutrop | Urinary tr infection, unk ANC | Urine color change | Urticaria | Ventricular arrhythmia | Vertigo | Vision,NOS | Voice change/stridor/larynx | Vomiting | Weakness (motor neuropathy) | Weight gain | Weight loss | |
| Arm I: Bicalutamide + Goserelin | 19 | 0 | 11 | 1 | 2 | 91 | 2 | 52 | 7 | 52 | 1 | 0 | 43 | 17 | 1 | 5 | 3 | 19 | 1 | 0 | 1 | 0 | 5 | 1 | 11 | 1 | 6 | 0 | 57 | 10 | 7 | 0 | 0 | 80 | 55 | 33 | 1 | 11 | 0 | 7 | 21 | 14 | 0 | 40 | 3 | 0 | 181 | 0 | 2 | 1 | 258 | 0 | 1 | 0 | 1 | 2 | 2 | 5 | 1 | 0 | 12 | 9 | 2 | 0 | 2 | 140 | 37 | 1 | 9 | 0 | 0 | 1 | 0 | 439 | 4 | 5 | 44 | 0 | 0 | 0 | 38 | 2 | 1 | 1 | 0 | 8 | 1 | 3 | 3 | 2 | 0 | 88 | 5 | 0 | 1 | 3 | 79 | 2 | 11 | 0 | 14 | 163 | 11 | 0 | 4 | 2 | 0 | 15 | 0 | 0 | 2 | 10 | 55 | 26 | 1 | 0 | 4 | 26 | 5 | 0 | 11 | 0 | 112 | 1 | 9 | 0 | 12 | 0 | 0 | 0 | 0 | 4 | 3 | 13 | 0 | 3 | 1 | 2 | 1 | 46 | 12 | 7 | 1 | 1 | 7 | 42 | 22 | 0 | 0 | 1 | 37 | 2 | 0 | 11 | 0 | 5 | 0 | 0 | 138 | 0 | 1 | 0 | 3 | 2 | 0 | 0 | 86 | 13 | 0 | 1 | 3 | 3 | 3 | 1 | 1 | 0 | 0 | 10 | 3 | 179 | 12 |
| Arm II: Mitoxantrone + Prednisone + Bivalutamid + Goserelin | 41 | 1 | 11 | 5 | 16 | 131 | 2 | 141 | 41 | 62 | 1 | 1 | 64 | 17 | 1 | 20 | 6 | 34 | 14 | 2 | 1 | 5 | 6 | 0 | 19 | 0 | 14 | 4 | 117 | 34 | 17 | 8 | 6 | 85 | 75 | 71 | 5 | 28 | 1 | 44 | 49 | 11 | 2 | 56 | 2 | 2 | 146 | 2 | 13 | 6 | 357 | 2 | 0 | 9 | 6 | 3 | 6 | 4 | 0 | 10 | 20 | 9 | 0 | 1 | 0 | 100 | 82 | 1 | 13 | 1 | 1 | 4 | 4 | 422 | 5 | 2 | 78 | 4 | 1 | 4 | 38 | 0 | 6 | 7 | 1 | 11 | 1 | 2 | 11 | 0 | 4 | 71 | 10 | 2 | 4 | 2 | 92 | 2 | 27 | 8 | 317 | 133 | 17 | 2 | 49 | 3 | 2 | 12 | 1 | 1 | 3 | 13 | 77 | 45 | 12 | 1 | 57 | 205 | 4 | 1 | 239 | 3 | 127 | 6 | 11 | 1 | 11 | 5 | 3 | 1 | 1 | 4 | 1 | 23 | 1 | 1 | 0 | 1 | 0 | 63 | 10 | 5 | 7 | 8 | 24 | 42 | 26 | 1 | 6 | 1 | 57 | 1 | 4 | 11 | 1 | 49 | 2 | 1 | 129 | 3 | 46 | 6 | 35 | 5 | 2 | 1 | 101 | 7 | 1 | 2 | 2 | 44 | 4 | 0 | 1 | 1 | 6 | 51 | 6 | 151 | 29 |
Measured from date of randomization to date of first observation of recurrence or death due to any cause. Patients without recurrence are censored at date of last contact. (NCT00004124)
Timeframe: at 10 Years
| Intervention | percentage of probability of survival (Number) |
|---|---|
| Arm I: Bicalutamide + Goserelin | 72 |
| Arm II: Mitoxantrone + Prednisone + Bivalutamid + Goserelin | 72 |
Measured from date of randomization to date of death from any cause. Patient known to be alive are censored at date of last contact. (NCT00004124)
Timeframe: at 10 Years
| Intervention | percentage of probability of survival (Number) |
|---|---|
| Arm I: Bicalutamide + Goserelin | 87 |
| Arm II: Mitoxantrone + Prednisone + Bivalutamid + Goserelin | 86 |
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 |
Ovarian dysfunction is defined as amenorrhea for the preceding three months and the presence of FSH, estradiol and/or inhibin B levels in the postmenopausal range. (NCT00068601)
Timeframe: 1 year
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Chemotherapy | 28 |
| Chemotherapy Plus Goserelin | 18 |
Ovarian failure at two years is defined as amenorrhea (absence of menstrual bleeding) for the preceding six months AND the presence of follicle-stimulating hormone (FSH) in the post-menopausal range. (NCT00068601)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Chemotherapy | 15 |
| Chemotherapy Plus Goserelin | 5 |
Ovarian dysfunction is defined as amenorrhea for the preceding three months and the presence of FSH, estradiol and/or inhibin B levels in the postmenopausal range. (NCT00068601)
Timeframe: 2 years
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Chemotherapy | 22 |
| Chemotherapy Plus Goserelin | 9 |
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 |
"PSA response is defined as complete biochemical response or partial response.~Complete Response:~A PSA < 0.2 ng/mL confirmed by a repeat PSA one month later is considered a complete biochemical response for patients with prior radical prostatectomy. A PSA < 1 ng/mL on three separate occasions taken at least one month apart is considered a complete biochemical response in patients with radiation therapy only.~Partial Response:~A reduction in PSA by > 50% from baseline, confirmed by repeat PSA 1 month later." (NCT00108732)
Timeframe: Assessed monthly during the first 24 weeks and then every 3 months for a maximum total of 24 months
| Intervention | Proportion of patients (Number) |
|---|---|
| Vaccinia/Fowlpox/GM-CSF | 0 |
PSA level was assessed on Day 4 and Day 15 of cycle 1, and a comparison between the two measurements was done. (NCT00108732)
Timeframe: Assessed at day 4 and day 15 of cycle 1
| Intervention | ng/mL (Median) |
|---|---|
| Vaccinia/Fowlpox/GM-CSF | 0.45 |
"For patients who achieved a > 50% decline in PSA, an increase in PSA value by 50% over the nadir, confirmed by a second PSA two weeks later is considered progressive disease. The PSA rise must be at least 5 ng/mL or back to pretreatment baseline, whichever is greater.~Changes in PSA below 5 ng/mL will not be considered assessable for progression.~For patients whose PSA has not decreased by 50%, an increase in PSA value > 50% of baseline (on trial) or nadir PSA, whichever is lower, confirmed by a repeat PSA two weeks later is considered progressive disease. The PSA must have risen by at least 5 ng/mL." (NCT00108732)
Timeframe: Assessed at 6 months
| Intervention | Proportion of patients (Number) |
|---|---|
| Vaccinia/Fowlpox/GM-CSF | 0.625 |
PSA slopes were assessed by multiple PSA values obtained prior to registration and during treatment. Only patients who completed at least 3 months of treatment were included in this analysis. The PSA slopes were calculated by a piecewise linear model using the three or four PSA values obtained prior to registration and PSA measurements obtained every 4 weeks for the first six months of treatment. Natural log transformed PSA levels were used in this analysis, and the difference between PSA slopes before and after treatment was calculated. (NCT00108732)
Timeframe: Assessed monthly during the first 24 weeks and then every 3 months for a maximum total of 24 months
| Intervention | log PSA/month (Median) |
|---|---|
| Vaccinia/Fowlpox/GM-CSF | -0.04 |
Based on International Index of Erectile Function (IIEF) scale, question #15, which asked subjects to rate their confidence that they could achieve and maintain an erection. Scores range from 1 to 5, with higher scores being better. (NCT00114114)
Timeframe: Baseline and 16 weeks
| Intervention | units on a scale (Mean) |
|---|---|
| Group 1: 0 g/Day | -1.4 |
| Group 2: 1.25 g/Day | -0.5 |
| Group 3: 2.5 g/Day | -0.2 |
| Group 4: 5 g/Day | -0.1 |
| Group 5: 10* g/Day | 0.2 |
| Group 6: PBO/PBO | -0.3 |
(NCT00114114)
Timeframe: Baseline and 16 weeks
| Intervention | percentage change (Mean) |
|---|---|
| Group 1: 0 g/Day | 103 |
| Group 2: 1.25 g/Day | 41 |
| Group 3: 2.5 g/Day | 29 |
| Group 4: 5 g/Day | 15 |
| Group 5: 10* g/Day | 4 |
| Group 6: Placebo/Placebo (PBO/PBO) | 11 |
(NCT00114114)
Timeframe: Baseline and 16 weeks
| Intervention | Percentage change (Mean) |
|---|---|
| Group 1: 0 g/Day | 9.8 |
| Group 2: 1.25 g/Day | 5.7 |
| Group 3: 2.5 g/Day | 1.9 |
| Group 4: 5 g/Day | 0.4 |
| Group 5: 10* g/Day | -1.6 |
| Group 6: PBO/PBO | 2.3 |
Assessed by quantitative computed tomography (QCT) (NCT00114114)
Timeframe: Baseline and 16 weeks
| Intervention | percentage change (Mean) |
|---|---|
| Group 1: 0 g/Day | -1.5 |
| Group 2: 1.25 g/Day | -1.6 |
| Group 3: 2.5 g/Day | -0.4 |
| Group 4: 5 g/Day | -0.5 |
| Group 5: 10* g/Day | 0.5 |
| Group 6: PBO/PBO | -0.9 |
Change in libido from baseline (scale ranges from -2 to +2), with -2 being much less, -1 somewhat less, 0 same, +1 somewhat more, +2 much more (NCT00114114)
Timeframe: 16 weeks
| Intervention | units on a scale (Mean) |
|---|---|
| Group 1: 0 g/Day | -1.6 |
| Group 2: 1.25 g/Day | -0.6 |
| Group 3: 2.5 g/Day | -0.6 |
| Group 4: 5 g/Day | -0.2 |
| Group 5: 10* g/Day | 0 |
| Group 6: PBO/PBO | -0.3 |
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 |
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 |
"The overall clinical benefit rate of goserelin followed by anastrozole was evaluated, as determined as the sum of the Complete Response (CR) rate + Partial Response (PR) rate + Stable Disease (SD) rate.~CR = Complete disappearance of all clinically- or pathologically-detectable malignant disease for at least 4 weeks.~PR = ≥ 50% decrease in tumor size for at least 4 weeks, without any new lesion or any ≥ 25% increase in size of any lesion.~SD = No significant change in measurable or evaluable disease for at least 4 weeks.~All measurements by ruler or calipers." (NCT00186121)
Timeframe: 6 months
| Intervention | percentage of participants (Number) |
|---|---|
| Anastrozole + Goserelin | 71.9 |
The toxicity of the treatment regimen of goserelin followed by anastrozole is estimated by the rate of Serious Adverse Events (SAEs) that occurred during the course of the study. (NCT00186121)
Timeframe: 6 months
| Intervention | Serious Adverse Events (SAEs) (Number) |
|---|---|
| Anastrozole + Goserelin | 0 |
"ORR was determined as the sum of the Complete Response (CR) rate + Partial Response (PR) rates.~CR = Complete disappearance of all clinically- or pathologically-detectable malignant disease for at least 4 weeks.~PR = ≥ 50% decrease in tumor size for at least 4 weeks, without any new lesion or any ≥ 25% increase in size of any lesion.~All measurements by ruler or calipers." (NCT00186121)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Anastrozole + Goserelin | 37.5 |
Overall survival (OS) was assessed as the median observed in the participants receiving goserelin followed by anastrozole. (NCT00186121)
Timeframe: up to 63 months
| Intervention | months (Median) |
|---|---|
| Anastrozole + Goserelin | NA |
"Time-to-progression (TTP) was assessed as the median observed in the participant group.~Progression of disease was considered, per protocol, to be ≤ 25% increase in the area of any malignant lesion greater than 2 square cm, or ≤ 25% increase in the sum of the products of the longest perpendicular diameters of individual lesions in a given organ, when compared to baseline values or after therapeutic response." (NCT00186121)
Timeframe: up to 63 months
| Intervention | months (Median) |
|---|---|
| Anastrozole + Goserelin | 8.3 |
Plasma estradiol determinations were performed at baseline, 1 month, 3 months, and 6 months using the Coat-A-Count Estradiol competitive binding assay system, which has a calibrated range for estradiol of 20 to 3,600 pg/mL with an analytical sensitivity of 10 pg/mL. (NCT00186121)
Timeframe: 6 months
| Intervention | pg/mL estradiol (Mean) | |||
|---|---|---|---|---|
| Mean at Baseline | Mean at 1 month treatment | Mean at 3 months treatment | Mean at 6 months treatment | |
| Anastrozole + Goserelin | 74.7 | 20.8 | 18.7 | 14.8 |
"The numbers of participants with metastatic breast cancer experiencing Complete Response (CR); Partial Response (PR); or Stable Disease (SD) after treatment with goserelin followed by anastrozole are reported.~CR = Complete disappearance of all clinically- or pathologically-detectable malignant disease for at least 4 weeks.~PR = ≥ 50% decrease in tumor size for at least 4 weeks, without any new lesion or any ≥ 25% increase in size of any lesion.~SD = No significant change in measurable or evaluable disease for at least 4 weeks.~All measurements by ruler or calipers." (NCT00186121)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| Complete Response (CR) | Partial Response (PR) | Stable Disease (SD) | |
| Anastrozole + Goserelin | 1 | 11 | 11 |
Serum DHT (NCT00298155)
Timeframe: After 12 weeks of neoadjuvant androgen deprivation
| Intervention | ng/dL (Mean) |
|---|---|
| Group 1 | 4.2 |
| Group 2 | 3.6 |
| Group 3 | 5.7 |
Tissue dihydrotesterone (DHT) (NCT00298155)
Timeframe: After 12 weeks of neoadjuvant androgen deprivation
| Intervention | ng/g (Mean) |
|---|---|
| Group 1 | 0.03 |
| Group 2 | 0.06 |
| Group 3 | 0.03 |
A comparison of mean E2 serum concentrations at timepoint(s) post Day 1 performed using analysis of covariance (ANCOVA), with treatment group, baseline E2 serum concentrations and country as covariates. Data analysed on the log scale; log scale mean and pooled log scale standard deviation from Analysis of Covariance (ANCOVA) presented. (NCT00322348)
Timeframe: Blood samples for measurement of E2 concentrations collected from all patients at scheduled visits of screening, Day 1 and Weeks 12 and 24 (+/- 7 days). Week 24 data is presented
| Intervention | pmol/L (Log Mean) |
|---|---|
| ZOLADEX 10.8 mg | 1.42 |
| ZOLADEX 3.6 mg | 1.49 |
Number of participants who were objective responders at Week 24 over the number of participants evaluable for response x 100. An objective responder = a participants whose best unconfirmed response is either CR (Complete Response Disappearance of all target lesions) or PR (Partial Response At least a 30% decrease in target lesions) (NCT00322348)
Timeframe: Response Evaluation Criteria in Solid Tumours (RECIST) tumour assessments carried out every 12 weeks from randomisation until Week 24 in those patients with measurable disease at baseline.
| Intervention | Percentage of participants (Number) |
|---|---|
| ZOLADEX 10.8 mg | 28.9 |
| ZOLADEX 3.6 mg | 25.6 |
Area under the plasma concentration curve (0-12 weeks) derived from analysis of pharmacokinetic (PK) outcomes samples provided only by participants in the PK subgroup set (all of whom received ZOLADEX 10.8 mg) (NCT00322348)
Timeframe: Blood samples taken at Days 1, 2 and 3, Weeks 4, 12 and 24. Derived from the individual goserelin plasma concentration-time profiles following the first dose of study drug for patients in the pharmacokinetic (PK) subgroup
| Intervention | ng/mL (Geometric Mean) |
|---|---|
| ZOLADEX 10.8 mg | 33.021 |
Maximum plasma concentration, Cmax (ng/mL), derived from analysis of pharmacokinetic (PK) outcomes samples provided only by participants in the PK subgroup set (all of whom received ZOLADEX 10.8 mg) (NCT00322348)
Timeframe: Blood samples taken at Days 1, 2 and 3, Weeks 4, 12 and 24. Derived from the individual goserelin plasma concentration-time profiles following the first dose of study drug for patients in the pharmacokinetic (PK) subgroup
| Intervention | ng/mL (Geometric Mean) |
|---|---|
| ZOLADEX 10.8 mg | 4.565 |
Time to maximum plasma concentration, Tmax (hours), derived from analysis of pharmacokinetic (PK) outcomes samples provided only by participants in the PK subgroup set (all of whom received ZOLADEX 10.8 mg) (NCT00322348)
Timeframe: Blood samples taken at Days 1, 2 and 3, Weeks 4, 12 and 24. Derived from the individual goserelin plasma concentration-time profiles following the first dose of study drug for patients in the pharmacokinetic (PK) subgroup
| Intervention | hours (Geometric Mean) |
|---|---|
| ZOLADEX 10.8 mg | 1.9 |
The number of participants for whom neither objective disease progression or death (due to any cause) has been observed at Week 24 over the number of randomised participants x 100. (NCT00322348)
Timeframe: Objective tumour assessments carried out every 12 weeks (+/- 7 days) until Week 24, and then every 24 weeks (+/- 14 days) until Week 96 or objective progression is confirmed according to Response Evaluation Criteria in Solid Tumours (RECIST).
| Intervention | Percentage of participants (Number) |
|---|---|
| ZOLADEX 10.8 mg | 69.4 |
| ZOLADEX 3.6 mg | 73.5 |
"To determine the maximum tolerated dose (MTD) of Samarium as adjuvant to combined hormonal therapy (HT) and external beam radiation therapy (RT).~Dose levels:~Dose I: 0.25 mCi/kg IV Dose II: 0.5 mCi/kg IV Dose III: 0.75 mCi/kg IV Dose IV: 1.0 mCi/kg IV Dose V: 1.5 mCi/kg IV Dose VI: 2.0 mCi/kg IV~Dose-limiting toxicity will be defined as Grade 3 hematologic toxicity per NCI Common Toxicity Criteria. The maximally tolerated dose (MTD) will then be the last dose studied or the previous dose, based on clinical judgment of the degree of toxicity seen at the last dose." (NCT00328614)
Timeframe: 5 months (1 month HT, administration of drug, 4 months HT and RT)
| Intervention | mCi/kg (Number) |
|---|---|
| Samarium-153 | 2.0 |
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 |
"Outcome characterized in terms of two variables, each measured repeatedly over time: Follicle-stimulating hormone (FSH) level and whether vaginal bleeding occurs, each to be measured from the end of chemotherapy. For treatment comparison, response defined as a composite event: both [FSH < 15] and vaginal bleeding observed within 12 months after the end of chemotherapy, with both FSH and vaginal bleeding baseline observed before start of chemotherapy." (NCT00429403)
Timeframe: Baseline prior to chemotherapy then every 3 months after chemotherapy for 1 year
| Intervention | participants (Number) |
|---|---|
| Goserelin | 1 |
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 |
Clinical Response Rate was measured according to the Response Evaluation Criteria in Solid Tumors (RECIST) Criteria for target lesions before surgery: 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. (NCT00432172)
Timeframe: Up to week 24
| Intervention | Participants (Count of Participants) |
|---|---|
| Group 1 (Luminal A) Standard Treatment | 31 |
| Group 1 (Luminal A) Selective Treatment | 23 |
| Group 2 (Basal) Standard Treatment | 32 |
| Group 2 (Basal) Selective Treatment | 36 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 319 |
(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) | 24 |
(NCT00589472)
Timeframe: Up to 1 year
| Intervention | ng/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 256 |
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 | mcg/dL (Median) |
|---|---|
| Treatment (Antihormone Therapy and Enzyme Inhibitor Therapy) | 90 |
Trough Plasma concentrations (Cmin) of Anastrozole - only Anastrozole arm was evaluated for Trough Plasma concentrations. (NCT00605267)
Timeframe: Assessed at week 12
| Intervention | ng/mL (Geometric Mean) |
|---|---|
| Anastrozole 1 mg | 29.7 |
"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period (based on the data from calliper measurement).~CR (or PR) criteria are met at 2 or more time in points every 4 weeks. Per RECIST Criteria (V1.0) and assessed by Calliper: 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." (NCT00605267)
Timeframe: 24 weeks
| Intervention | Percentage of Participants (Number) |
|---|---|
| Anastrozole 1 mg | 70.4 |
| Tamoxifen 20 mg | 50.5 |
"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period(based on the data from magnetic resonance imaging (MRI) or computed tomography (CT) measurement).~CR (or PR) criteria are met at either 12 weeks or 24 weeks. Per RECIST Criteria (V1.0) and assessed by MRI or CT: 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." (NCT00605267)
Timeframe: 24 weeks
| Intervention | Percentage of Participants (Number) |
|---|---|
| Anastrozole 1 mg | 64.3 |
| Tamoxifen 20 mg | 37.4 |
"The BORR were defined as the percentage of patients with confirmed CR or PR in the ITT population during 24 weeks pre-operative treatment period (based on the data from ultra sound (US) measurement).~CR (or PR) criteria are met at 2 or more time in points every 4 weeks. Per RECIST Criteria (V1.0) and assessed by US: 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." (NCT00605267)
Timeframe: 24 weeks
| Intervention | Participants (Number) |
|---|---|
| Anastrozole 1 mg | 58.2 |
| Tamoxifen 20 mg | 42.4 |
Change from baseline in Bone Mineral Density value (percentage), in all subjects who used DXA(Dual-energy X-ray absorptiometry) method throughout the study, at 24 weeks measured at cervical thighbone. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | PercentageBMD=Patient'sBMD/standard BMD) (Mean) |
|---|---|
| Anastrozole 1 mg | -2.5 |
| Tamoxifen 20 mg | -0.5 |
Change from baseline in Bone Mineral Density value (percentage), in all subjects who used DXA(Dual-energy X-ray absorptiometry) method throughout the study, at 24 weeks measured at lumbar spine. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | PercentageBMD=Patient's BMD/standard BMD (Mean) |
|---|---|
| Anastrozole 1 mg | -5.8 |
| Tamoxifen 20 mg | -2.9 |
Change from baseline in serum Bone-Alkaline Phosphatase (BAP) at 24 weeks measured by CLEIA method (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | ug/L (Mean) |
|---|---|
| Anastrozole 1 mg | 3.96 |
| Tamoxifen 20 mg | -0.75 |
Change from baseline in serum Bone-Alkaline Phosphatase (BAP) at 24 weeks measured by EIA method (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | U/L (Mean) |
|---|---|
| Anastrozole 1 mg | 7.1941 |
| Tamoxifen 20 mg | 0.7333 |
Change from baseline in serum crosslinked N-Telopeptide of type I collagen (NTX) at 24 weeks (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | nmolBCE(Bone Collagen Equivalent) /L (Mean) |
|---|---|
| Anastrozole 1 mg | 9.17 |
| Tamoxifen 20 mg | 2.59 |
"Change from baseline in Endocrine Symptom Subscale (ES)) in the ITT population at 24 weeks. ES score = the sum of the responses to all the questions on ES, low scores reflect poor quality of life and high scores reflects better quality of life.~Score range: 0-72" (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | ES score (Mean) |
|---|---|
| Anastrozole 1 mg | -8.85 |
| Tamoxifen 20 mg | -6.27 |
"Change from baseline in Functional Assessment of Cancer Therapy-Breast (FACT-B)in the ITT population at 24 weeks. Trial Outcome Index (TOI) = the sum of the Physical Well-Being (PWB), Functional Well-Being (FWB), and Breast Cancer Scale (BCS) subscales of FACT-B.~FACT-B includes 36 questions; 7 in PWB (Physical Well-Being); 7 inSWB (Social / Family Well-Being); 6 in EWB (Emotional Well-Being); 7 in FWB (Functional Well-Being); 9 in BCS (Breast Cancer Subscale).~Total score of subscores or TOI is calculated from each score of question. Higher score means better and lower score means worthier.~Score range; 0-28 in PWB; 0-28 in SWB; 0-24 in EWB; 0-28 in FWB; 0-36 in BCS; 0-92 in TOI." (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Trial Outcome Index (TOI) (Prorated) (Mean) |
|---|---|
| Anastrozole 1 mg | -4.42 |
| Tamoxifen 20 mg | -2.65 |
Number of patients in the ITT population defined as histopathological responders over the total number of patients x 100. An histopathological responder = a patient classified as Grade 1b, 2 or 3 for the histopathological response (Grade 0 = no response, 1a = mild response, 1b = moderate response, 2 = marked response or 3 = complete response) (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Percentage of Participants (Number) |
|---|---|
| Anastrozole 1 mg | 41.8 |
| Tamoxifen 20 mg | 27.3 |
Ratio of serum Oestradiol (E2) concentration (pg/mL) in the ITT population from baseline at 24 weeks. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Ratio (Mean) |
|---|---|
| Anastrozole 1 mg | 0.041 |
| Tamoxifen 20 mg | 0.082 |
Ratio of serum Oestrone (E1) concentration (pg/mL) in the ITT population from baseline at 24 weeks. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Ratio (Mean) |
|---|---|
| Anastrozole 1 mg | 0.028 |
| Tamoxifen 20 mg | 0.341 |
ER status in the ITT population is categorized as Positive or Negative (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Baseline Positive & 24 weeks Negative | Baseline Positive & 24 weeks Positive | Baseline Negative & 24 weeks Negative | Baseline Negative & 24 weeks Positive | |
| Anastrozole 1 mg | 2 | 92 | 0 | 0 |
| Tamoxifen 20 mg | 1 | 89 | 0 | 0 |
PgR status in the ITT population is categorized as Positive or Negative. (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Baseline Positive & 24 weeks Negative | Baseline Positive & 24 weeks Positive | Baseline Negative & 24 weeks Negative | Baseline Negative & 24 weeks Positive | |
| Anastrozole 1 mg | 60 | 29 | 4 | 1 |
| Tamoxifen 20 mg | 19 | 59 | 9 | 3 |
HER2 status in the ITT population is categorized as Positive or Negative (NCT00605267)
Timeframe: Assessed at baseline and after 24 weeks of treatment
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Baseline Positive & 24 weeks Negative | Baseline Positive & 24 weeks Positive | Baseline Negative & 24 weeks Negative | Baseline Negative & 24 weeks Positive | |
| Anastrozole 1 mg | 0 | 0 | 92 | 2 |
| Tamoxifen 20 mg | 0 | 0 | 88 | 2 |
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 |
TRUS is a method of measuring the size of the prostate. (NCT00831233)
Timeframe: After 12 weeks treatment compared to Baseline
| Intervention | mL (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -22.4 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -13.4 |
The IPSS is a tool commonly used to assess the severity of lower urinary tract symptoms (LUTS), and to monitor the progress of the disease once treatment has been initiated. The participant completes a questionnaire containing 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia. Each question is assigned a score of 0-5. The total score is then classified according to the following scale: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT00831233)
Timeframe: After treatment of 12 weeks compared to Baseline
| Intervention | score on scale (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -11.2 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -7.69 |
Uroflowmetry was used to quantify the maximum urine flow (Qmax; mL/sec) (NCT00831233)
Timeframe: After treatment of 4, 8 and 12 weeks compared to Baseline
| Intervention | mL/sec (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | 3.63 | 4.74 | 3.62 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 3.55 | 3.52 | 2.07 |
The IPSS questionnaire included an additional single question to assess the participant's QoL in relation to his urinary symptoms. The question was: 'If you were to spend the rest of your life with your urinary condition the way it is now, how would you feel about that?' The possible answers to this question ranged from 'delighted' (a score of '0') to 'terrible' (a score of '6'). The figures in the tables present the change (ie decrease) in IPSS QoL score, i.e. the bigger the decrease the better QoL. (NCT00831233)
Timeframe: After treatment of 4, 8 and 12 weeks compared to Baseline
| Intervention | score on scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -0.96 | -1.54 | -1.77 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -0.54 | -0.73 | -0.55 |
Uroflowmetry was used to quantify the residual volume (Vresidual; mL) (NCT00831233)
Timeframe: After treatment of 4, 8 and 12 weeks compared to Baseline
| Intervention | mL (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -36.2 | -43.8 | -50.7 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -19.8 | -19.6 | -13.4 |
The IPSS is a tool commonly used to assess the severity of lower urinary tract symptoms (LUTS), and to monitor the progress of the disease once treatment has been initiated. The participant completes a questionnaire containing 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia. Each question is assigned a score of 0-5. The total score is then classified according to the following scale: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT00831233)
Timeframe: After treatment of 4 and 8 weeks compared to Baseline
| Intervention | score on scale (Mean) | |
|---|---|---|
| Week 4 | Week 8 | |
| Degarelix 240 mg/80 mg | -7.31 | -9.46 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -4.62 | -8.08 |
The figures present the number of participants who had abnormal (defined as above upper limit of normal range (ULN)) levels of safety laboratory variables. Only the laboratory variables that had at least on participant with one abnormal value are presented, many more variables were included in the trial. (NCT00831233)
Timeframe: Baseline to 12 weeks of treatment
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| B-Haematocrit (Ratio) <=0.37 | B-Platelet count (10^9/L) <=75 | S-Calcium (mmol/L) <=1.8 | S-Potassium (mmol/L) >=5.8 | S-Urea nitrogen (mmol/L) >=10.7 | |
| Degarelix 240 mg/80 mg | 5 | 1 | 1 | 0 | 1 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 1 | 0 | 0 | 1 | 2 |
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 and at least one post-baseline markedly abnormal value. (NCT00831233)
Timeframe: Baseline to 12 weeks 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 240 mg/80 mg | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 1 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
(NCT00831233)
Timeframe: After treatment of 4, 8 and 12 weeks compared to Baseline
| Intervention | participants (Number) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | 26 | 25 | 27 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 12 | 12 | 12 |
(NCT00831233)
Timeframe: After treatment of 4, 8 and 12 weeks compared to Baseline
| Intervention | percentage (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -85.72 | -89.2 | -93.87 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -93.44 | -97.26 | -97.78 |
(NCT00833248)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | nanogram per deciliter (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -1.55 | -1.6 | -1.55 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -1.65 | -1.65 | -1.6 |
TRUS is a method of measuring the size of the prostate. (NCT00833248)
Timeframe: After treatment of 12 weeks compared to Baseline
| Intervention | milliliter (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -36.0 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -35.3 |
TRUS is a method of measuring the size of the prostate. (NCT00833248)
Timeframe: After treatment of 12 weeks compared to Baseline
| Intervention | milliliter (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -36.2 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -35.4 |
The IPSS questionnaire included an additional single question to assess the participant's QoL in relation to his urinary symptoms. The question was: 'If you were to spend the rest of your life with your urinary condition the way it is now, how would you feel about that?' The possible answers to this question ranged from 'delighted' (a score of '0') to 'terrible' (a score of '6'). (NCT00833248)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -0.07 | -0.24 | -0.33 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 0.16 | 0.05 | 0.16 |
(NCT00833248)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | nanograms per milliliter (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -6.3 | -7.95 | -8.35 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -5.9 | -8.8 | -9.05 |
(NCT00833248)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | nanograms per milliliter (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -3.8 | -3.77 | -3.81 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -4.22 | -4.26 | -4.3 |
The IPSS is a tool commonly used to assess the severity of lower urinary tract symptoms (LUTS), and to monitor the progress of the disease once treatment has been initiated. The participant completes a questionnaire containing 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia. Each question is assigned a score of 0-5. The total score is then classified according to the following scale: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT00833248)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -0.21 | -1.53 | -1.71 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 0.36 | 0.02 | 0.11 |
The figures present the number of participants who had abnormal (defined as above upper limit of normal range (ULN)) levels of safety laboratory variables. Only the laboratory variables that had at least one percentage of participants in either group with abnormal value are presented, more variables were included in the study. (NCT00833248)
Timeframe: Baseline to 12 weeks of treatment
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| B-Haematocrit (Ratio) <=0.37 | B-Haemoglobin (g/L) <=115 | S-Alanine aminotransferase (IU/L) >3 x ULN | S-Potassium (mmol/L) >=5.8 | S-Urea nitrogen (mmol/L) >=10.7 | |
| Degarelix 240 mg/80 mg | 31 | 4 | 1 | 4 | 10 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 8 | 1 | 1 | 1 | 3 |
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 and at least one post-baseline markedly abnormal value. (NCT00833248)
Timeframe: Baseline to 12 weeks 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 240 mg/80 mg | 0 | 3 | 0 | 1 | 1 | 0 | 3 | 5 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 0 | 0 | 0 | 1 | 1 | 0 | 2 | 0 |
TRUS is a method of measuring the size of the prostate. (NCT00884273)
Timeframe: After treatment of 4 and 8 weeks compared to Baseline
| Intervention | milliliter (Mean) | |
|---|---|---|
| Week 4 | Week 8 | |
| Degarelix 240 mg/80 mg | -19.2 | -33.1 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -21.2 | -33.2 |
The IPSS questionnaire included an additional single question to assess the participant's QoL in relation to his urinary symptoms. The question was: 'If you were to spend the rest of your life with your urinary condition the way it is now, how would you feel about that?' The possible answers to this question ranged from 'delighted' (a score of '0') to 'terrible' (a score of '6'). (NCT00884273)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -0.46 | -0.83 | -0.99 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -0.56 | -0.79 | -1.01 |
The IPSS is a tool commonly used to assess the severity of lower urinary tract symptoms (LUTS), and to monitor the progress of the disease once treatment has been initiated. The participant completes a questionnaire containing 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia. Each question is assigned a score of 0-5. The total score is then classified according to the following scale: 0 to 7 = mildly symptomatic; 8 to 19 = moderately symptomatic; and 20 to 35 = severely symptomatic. (NCT00884273)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -2.09 | -3.55 | -4.39 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -1.36 | -3.13 | -2.74 |
(NCT00884273)
Timeframe: At 4, 8, and 12 weeks compared to baseline.
| Intervention | nanograms per milliliter (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -20.25 | -22.5 | -25.15 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -12.10 | -14.6 | -13.1 |
The figures present the number of participants who had abnormal (defined as above upper limit of normal range (ULN)) levels of safety laboratory variables. Only the laboratory variables that had at least one percentage of participants in either group with abnormal value are presented, more variables were included in the study. (NCT00884273)
Timeframe: Baseline to 12 weeks of treatment
| Intervention | participants (Number) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| B-Haematocrit (Ratio) <=0.37 | B-Haemoglobin (g/L) <=115 | B-Red blood cell count (10^12/L) <=3.5 | B-White blood cell count (10^9/L) <=2.8 | S-Alanine aminotransferase (IU/L) >3xULN | S-Alkaline phosphatase (IU/L) >3xULN+25% increase | S-Aspartate aminotransferase (IU/L) >3xULN | S-Cholesterol (mmol/L) >=8.0 | S-Glutamyltransferase (IU/L) >3xULN | S-Potassium (mmol/L) >=5.8 | S-Urea nitrogen (mmol/L) >=10.7 | |
| Degarelix 240 mg/80 mg | 13 | 2 | 1 | 3 | 1 | 0 | 0 | 2 | 1 | 3 | 10 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 16 | 1 | 0 | 1 | 2 | 1 | 2 | 0 | 0 | 3 | 3 |
(NCT00884273)
Timeframe: At 4, 8, and 12 weeks compared to baseline.
| Intervention | nanograms per milliliter (Median) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -3.91 | -3.97 | -4.09 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -4.17 | -4.24 | -4.23 |
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 and at least one post-baseline markedly abnormal value. (NCT00884273)
Timeframe: Baseline to 12 weeks 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 240 mg/80 mg | 0 | 0 | 0 | 2 | 1 | 0 | 0 | 2 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | 0 | 1 | 0 | 4 | 0 | 0 | 5 | 3 |
TRUS is a method of measuring the size of the prostate. (NCT00884273)
Timeframe: After treatment of 12 weeks compared to Baseline
| Intervention | milliliter (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -37.2 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -39.0 |
TRUS is a method of measuring the size of the prostate. (NCT00884273)
Timeframe: After treatment of 12 weeks compared to Baseline
| Intervention | milliliter (Mean) |
|---|---|
| Degarelix 240 mg/80 mg | -37.3 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -39.0 |
The Benign Prostatic Hyperplasia Impact Index (BPHII) is a self-administered questionnaire to measure how much urinary problems affect various domains of health. The higher value the worse are the urinary problems. The minimum possible total value is 0 and the maximum possible total value is 16. (NCT00884273)
Timeframe: After treatment of 4, 8, and 12 weeks compared to Baseline
| Intervention | scores on a scale (Mean) | ||
|---|---|---|---|
| Week 4 | Week 8 | Week 12 | |
| Degarelix 240 mg/80 mg | -0.78 | -0.88 | -1.28 |
| Goserelin (3.6 mg) + Bicalutamide (50 mg) | -0.70 | -1.09 | -1.16 |
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 |
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 |
"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 |
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 |
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 |
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 |
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 |
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 |
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 (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 |
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 |
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 |
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 |
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 |
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 |
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 |
This co-primary outcome measure was used to demonstrate that degarelix is effective with respect to achieving and maintaining testosterone suppression to castrate levels, evaluated as the proportion of patients with testosterone suppression ≤0.5 ng/mL from Day 28 to Day 364. (NCT00946920)
Timeframe: From Day 28 to Day 364
| Intervention | percentage of participants (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 90.0 |
This co-primary outcome measure was used to establish non-inferiority of degarelix as compared to goserelin with regard to achieving and maintaining testosterone suppression at castrate levels (≤0.5 ng/mL) from Day 3 to Day 364, using a non-inferiority margin of 5 percentage points. (NCT00946920)
Timeframe: Day 3 to Day 364
| Intervention | percentage of participants (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 85.0 |
| Goserelin Acetate | 5.3 |
Median testosterone levels are presented as absolute values at Baseline (in Baseline measures) and after 1, 2, 3, 6 and 13 months (below). One treatment month equals 28 days. (NCT00946920)
Timeframe: Baseline and after 1, 2, 3, 6 and 13 months
| Intervention | ng/mL (Median) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 2 | Month 3 | Month 6 | Month 13 | |
| Degarelix 240 mg/480 mg | 0.10 | 0.09 | 0.09 | 0.09 | 0.11 |
| Goserelin Acetate | 0.16 | 0.10 | 0.09 | 0.09 | 0.09 |
The SF-36 is a multi-purpose, short-form health survey with only 36 questions and with a minimum score of 0 and a maximum score of 100. The higher score the better health. It yields an 8-scale profile of functional health and well-being scores as well as psychometrically-based physical and mental health summary measures and a preference-based health utility index. The SF-36 has proven useful in surveys of general and specific populations, comparing the relative burden of diseases, and in differentiating the health benefits produced by a wide range of different treatments. (NCT00946920)
Timeframe: At baseline, 10 months and 13 months
| Intervention | units on a scale (Mean) | |
|---|---|---|
| Month 10 | Month 13 | |
| Degarelix 240 mg/480 mg | 0.52 | 0.18 |
| Goserelin Acetate | 0.27 | -0.87 |
"IPSS is used to assess severity of lower urinary tract symptoms and to monitor the progress of symptoms once treatment has been initiated. It contains 7 questions regarding incomplete emptying, frequency, intermittency, urgency, weak stream, straining, and nocturia. Each question is assigned a score of 0-5 (i.e. the minimum total score is 0 and the maximum is 35). A score of 0 corresponds to a response of not at all for the first six symptoms and none for nocturia, and a score of 5 corresponds to a response of almost always for the first six symptoms and 5 times or more for nocturia." (NCT00946920)
Timeframe: At baseline, 1 month, 4 months, 7 months and 13 months
| Intervention | units on a scale (Mean) | |||
|---|---|---|---|---|
| Month 1 | Month 4 | Month 7 | Month 13 | |
| Degarelix 240 mg/480 mg | -1.06 | -2.31 | -2.47 | -2.04 |
| Goserelin Acetate | -0.21 | -1.74 | -2.45 | -1.52 |
Serum PSA levels are presented as mean percent change from Baseline (in Baseline measures) after 1, 2, 3, 6 and 13 months. One treatment month equals 28 days. (NCT00946920)
Timeframe: Baseline and after 1, 2, 3, 6 and 13 months
| Intervention | percent change (Mean) | ||||
|---|---|---|---|---|---|
| Month 1 | Month 2 | Month 3 | Month 6 | Month 13 | |
| Degarelix 240 mg/480 mg | -77 | -89 | -90 | -90 | -82 |
| Goserelin Acetate | -57 | -86 | -86 | -91 | -77 |
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 |
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 |
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 |
E2 serum concentrations (pg/mL) at 24 weeks (NCT01073865)
Timeframe: 24 weeks after the first dosing
| Intervention | pg/mL (Mean) |
|---|---|
| Zoladex 10.8 mg | 20.302 |
| Zoladex 3.6 mg | 24.798 |
A patient is judged as progression-free survive at Week 24 if their PFS time is at least 24 weeks with no progression event prior to Week 24 (ie, overall visit response is complete response (CR), partial response (PR) or stable disease (SD) at a tumour assessment at least 24 weeks after randomization). Overall visit response is assessed according to the RECIST version 1.1. %PFS is the proportion of patients with PFS. (NCT01073865)
Timeframe: 24 weeks after the first dosing
| Intervention | Participants (Count of Participants) |
|---|---|
| Zoladex 10.8 mg | 67 |
| Zoladex 3.6 mg | 68 |
Responders are defined as those patients with a best objective tumour response of CR or PR during the first 24 weeks of therapy. Tumour response is assessed according to the RECIST version 1.1. ORR is defined as the proportion of patients who are responders. (NCT01073865)
Timeframe: 24 weeks after the first dosing
| Intervention | Participants (Count of Participants) |
|---|---|
| Zoladex 10.8 mg | 21 |
| Zoladex 3.6 mg | 25 |
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 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 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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
Per RECIST criteria v. 1.1: measurable lesions: complete response (CR) disappearance of target lesions, partial response (PR) > 30% decrease in the sum of the longest diameter (LD) of target lesions, progressive disease (PD) > 20% increase in the sum of the LD of target lesions or appearance of new lesions, stable disease (SD) neither sufficient decrease nor increase of the sum of smallest sum of the LD of target lesions (NCT01205685)
Timeframe: Every 12 weeks to tumor progression
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Complete Response | Partial Response | Stable Disease | Progressive disease | |
| OSI-906 + Erlotinib + Letrozole + Goserelin | 0 | 0 | 0 | 10 |
Time to progression measured in months from study entry to date of disease progression (NCT01205685)
Timeframe: From study entry to 6 months
| Intervention | months (Median) |
|---|---|
| OSI-906 + Erlotinib + Letrozole + Goserelin | 2 |
According to National Cancer Institute Common Toxicity Criteria for Adverse Events with 1 = mild, 2 = moderate, 3 = severe, 4 = life threatening/disabling, and 5 = death. (NCT01205685)
Timeframe: Every 4 weeks up to 24 weeks
| Intervention | participants (Number) | ||||
|---|---|---|---|---|---|
| Patients with worst grade toxicity of 1 | Patients with worst grade toxicity of 2 | Patients with worst grade toxicity of 3 | Patients with worst grade toxicity of 4 | Patients with worst grade toxicity of 5 | |
| OSI-906 + Erlotinib + Letrozole + Goserelin | 2 | 6 | 3 | 0 | 0 |
Median PSA levels are presented as absolute values in nanograms per milliliter (ng/mL) at baseline and after 1, 6, 12, 19, and 22 months. One month equals 28 days. After 22 months, only a limited number of samples were analysed. (NCT01242748)
Timeframe: Baseline and after 1, 6, 12, 19, and 22 months
| Intervention | ng/mL (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Month 1 | Month 6 | Month 12 | Month 19 | Month 22 | |
| Degarelix 240 mg/480 mg | 19 | 3.79 | 0.82 | 0.6 | 0.54 | 0.535 |
| Goserelin Acetate | 19.1 | 6.5 | 0.73 | 0.43 | 0.28 | 0.26 |
Testosterone escape is defined as serum levels >0.5 ng/mL. The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of no testosterone escape. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of no testosterone escape (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 83.7 |
| Goserelin Acetate | 96.7 |
Median testosterone levels are presented as absolute values in nanograms per milliliter (ng/mL) at baseline and after 1, 6, 12, 19, and 22 months. One month equals 28 days. After 22 months, only a limited number of samples were analysed. (NCT01242748)
Timeframe: Baseline and after 1, 6, 12, 19, and 22 months
| Intervention | ng/mL (Median) | |||||
|---|---|---|---|---|---|---|
| Baseline | Month 1 | Month 6 | Month 12 | Month 19 | Month 22 | |
| Degarelix 240 mg/480 mg | 4.52 | 0.10 | 0.09 | 0.10 | 0.11 | 0.11 |
| Goserelin Acetate | 4.62 | 0.16 | 0.09 | 0.09 | 0.05 | 0.05 |
The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of death. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of deaths (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 4.6 |
| Goserelin Acetate | 5.3 |
PFS failure is defined as either PSA failure, introduction of additional therapy related to prostate cancer (radiation, anti-androgens or second-line treatment), or death, whichever is first. The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of no PFS failure. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of no PFS failure (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 71.5 |
| Goserelin Acetate | 69.0 |
PSA PFS failure is defined as either PSA failure (defined as increase in serum PSA of 50%, and at least 5 ng/mL, compared to nadir, measured on two consecutive occasions at least 2 weeks apart) or death, whichever is first. The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of no PSA-PFS. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of no PSA-PFS (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 75.5 |
| Goserelin Acetate | 75.4 |
PSA failure is defined as increase in serum PSA of 50%, and at least 5 ng/mL, compared to nadir, measured on two consecutive occasions at least 2 weeks apart. The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of no PSA failure. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of no PSA failure (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 77.5 |
| Goserelin Acetate | 79.6 |
Additional therapy related to prostate cancer included radiation, anti-androgens and second-line treatment. The number below present the unadjusted rates (estimated using the Kaplan-Meier method) of no additional therapy related to prostate cancer. (NCT01242748)
Timeframe: From baseline to 3 years
| Intervention | percentage of no additional therapy (Number) |
|---|---|
| Degarelix 240 mg/480 mg | 84.5 |
| Goserelin Acetate | 83.4 |
One of two pathologists (SR, EG), assigned the Gleason scores for each patient from pre-treatment prostate biopsies and assessed pathological staging on post- prostatectomy specimens. Staging including a description of all tumor foci within the gland, presence or absence of perineural invasion and/or lymphovascular invasion, presence of extraprostatic extension of tumor (including seminal vesicle invasion), and margin status. The pathologists reviewed the presence or absence of cancer in each prostate gland removed on the study patients. RECIST has to my knowledge not been used for pathological examination in neoadjuvant studies. 0 out of 28 participants acheived complete response. RECIST is not appropriate as cancer within the gland at the time of treatment is not measurable by RECIST. The primary outcome is a pathological complete response. (NCT01250717)
Timeframe: status post prostectomy
| Intervention | participants (Number) |
|---|---|
| Docetaxel Followed by Radical Prostatectomy | 0 |
(NCT01368263)
Timeframe: 16 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Group 1 (Ki67 <10%, E2 <= 15 pg/ml) | 0 |
To obtain the PEPI score, risk points for relapse-free survival (RFS) and breast cancer-specific survival (BCSS) are assigned depending on the hazard ratio (HR) from the multivariable analysis. The total PEPI score assigned to each patient is the sum of the risk points derived from the pT stage, pN stage, Ki67 level, and estrogen receptor status of the surgical specimen. A HR in the range of 1 to 2 receives one risk point; a HR in the 2 to 2.5 range, two risk points; a HR greater than 2.5, three risk points. The total risk point score for each patient is the sum of all the risk points accumulated from the four factors in the model, ranges from 0 (best possible outcome) to 12 (worst possible outcome). (NCT01368263)
Timeframe: At time of definitive surgery
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| PEPI Score 1 | PEPI Score 4 | PEPI Score 7 | PEPI Score 8 | |
| Group 1 (Ki67 <10%, E2 <= 15 pg/ml) | 1 | 1 | 1 | 1 |
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 |
"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 |
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 |
Doubling in number of T-cells was assessed by immunologic responses (in the tumor microenvironment) in subjects consenting to undergo study biopsies. Baseline was defined as the measurement taken within 8 weeks of prior to the first dose of study medication (Day 1). (NCT01496131)
Timeframe: Baseline, Week 6-12 (Pre-RT), Week 40 (Post-RT)
| Intervention | Participants (Count of Participants) |
|---|---|
| Pre-RT | |
| Standard Therapy | 1 |
"Progression/recurrence status was reported based on Prostate-specific Antigen (PSA) Levels. Recurrence of PSA after completion of therapy represents disease progression and was determined using the American Society for Therapeutic Radiology and Oncology (ASTRO) Phoenix criteria. These criteria define biochemical recurrence after radiation therapy as a PSA level equal to the lowest (nadir) PSA level achieved after therapy plus 2 nanogram per milliliter." (NCT01496131)
Timeframe: From randomization up to 24 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Therapy | 2 |
| Standard Therapy Plus Tecemotide (L-BLP25) | 0 |
MUC1-specific systemic immune response was measured by intracellular cytokine antigen specific staining following a period of in vitro stimulation (IVS) with overlapping 15-mer peptide pools encoding the tumor-associated antigen (TAA) MUC-1. Baseline was defined as the measurement taken prior to the first dose of study medication (Day 1). (NCT01496131)
Timeframe: Baseline and Day 60 (Pre-Radiation)
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Therapy | 2 |
| Standard Therapy Plus Tecemotide (L-BLP25) | 3 |
Doubling in number of T-cells was assessed by immunologic responses (in the tumor microenvironment) in subjects consenting to undergo study biopsies. Baseline was defined as the measurement taken within 8 weeks of prior to the first dose of study medication (Day 1). (NCT01496131)
Timeframe: Baseline, Week 6-12 (Pre-RT), Week 40 (Post-RT)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Pre-RT | Post-RT | |
| Standard Therapy Plus Tecemotide (L-BLP25) | 1 | 1 |
MUC1-specific systemic immune response was measured by intracellular cytokine antigen specific staining following a period of in vitro stimulation (IVS) with overlapping 15-mer peptide pools encoding the tumor-associated antigen (TAA) MUC-1. Baseline was defined as the measurement taken prior to the first dose of study medication (Day 1). (NCT01496131)
Timeframe: Baseline and Day 190 (Post-radiation)
| Intervention | Participants (Count of Participants) |
|---|---|
| Standard Therapy | 1 |
| Standard Therapy Plus Tecemotide (L-BLP25) | 1 |
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 |
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 |
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 |
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 |
(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 |
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 |
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 |
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 |
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 |
Patients with serum total testosterone (STT) level lower than 0.5 ng/mL after 6 months of treatment. (NCT01673984)
Timeframe: 6 months
| Intervention | percentage of participants (Number) |
|---|---|
| Decapeptyl® SR 22.5mg | 92.9 |
| Current 3-monthly LHRH Agonist | 100 |
TSQM comprised of four dimensions: effectiveness, side effects, convenience and overall global satisfaction. Each score ranged from 0 to 100. For effectiveness, convenience and overall global satisfaction scores, 0 indicated an extreme dissatisfaction and 100 indicated an extreme satisfaction. For side effects score, 0 indicated an extreme dissatisfaction and 100 indicated no dissatisfaction at all. (NCT01673984)
Timeframe: 6 and 12 month
| Intervention | units on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Baseline to 6 months - Effectiveness (n= 13, 7) | Baseline to 12 months - Effectiveness (n= 3, 2) | Baseline to 6 months - Side Effects (n= 13, 7) | Baseline to 12 months - Side Effects (n= 3, 2) | Baseline to 6 months - Convenience (n= 13, 7) | Baseline to 12 months - Convenience (n= 3, 2) | Baseline to 6months -Global Satisfaction(n= 12, 6) | Baseline to 12months -Global Satisfaction(n= 2, 2) | |
| Current 3-monthly LHRH Agonist | 13.1 | -12.5 | 4.8 | 12.5 | 2.0 | 2.8 | -4.2 | 4.2 |
| Decapeptyl® SR 22.5mg | 3.2 | -33.3 | -2.6 | -25.0 | 4.7 | -1.9 | -0.7 | -12.5 |
Stable PSA level was noted as value either lower or less than 25% higher than the baseline value, or PSA value ≤0.5 ng/mL higher than the baseline value, if value ≥25% higher than the baseline value. (NCT01673984)
Timeframe: 6 and 12 months
| Intervention | percentage of participants (Number) | |
|---|---|---|
| 6 months (n = 13, 7) | 12 months (n = 2, 1) | |
| Current 3-monthly LHRH Agonist | 100 | 100 |
| Decapeptyl® SR 22.5mg | 84.6 | 50 |
The EQ-5D-5L questionnaire consisted of a description of raw data which comprised of five dimensions (mobility, self-care, usual activities, pain/discomfort and anxiety/depression). Each dimension had five levels: no problems, slight problems, moderate problems, severe problems, and extreme problems. The visual analogical scale of the EQ-5D-5L questionnaire was numbered from 0 to 100 (0 meaning the worst health the patient can imagine and 100 the best health the patient can imagine). (NCT01673984)
Timeframe: Baseline and Month 12
| Intervention | units on a scale (Mean) |
|---|---|
| Decapeptyl® SR 22.5mg | 71.7 |
| Current 3-monthly LHRH Agonist | 70.0 |
Patients with serum total testosterone (STT) level lower than 0.5 ng/mL, 12 months after randomisation.. (NCT01673984)
Timeframe: 12 months
| Intervention | percentage of participants (Number) |
|---|---|
| Decapeptyl® SR 22.5mg | 22.2 |
| Current 3-monthly LHRH Agonist | 25.0 |
(NCT01673984)
Timeframe: Month 12
| Intervention | percentage of participants (Number) |
|---|---|
| Decapeptyl® SR 22.5mg | 80 |
| Current 3-monthly LHRH Agonist | 0 |
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 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 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 |
number of blastocytes that can be cryopreserved (NCT01682642)
Timeframe: 1 week after oocyte retrieval
| Intervention | number of cryopreserved embryos (Mean) |
|---|---|
| Zoladex | 0.9 |
| Vaporization Only | 1.6 |
The development of the embryo at the time of transfer on day 3. Good quality is defined by more than 7 cells and less then 20% fragmentation on day 3. (NCT01682642)
Timeframe: 3 days after oocyte retrieval
| Intervention | percentage of good quality embryos (Number) |
|---|---|
| Zoladex | 59.3 |
| Vaporization Only | 67.3 |
total dose of FSH needed at the end of stimulation (NCT01682642)
Timeframe: 3 weeks
| Intervention | IUs (Mean) |
|---|---|
| Zoladex | 2561 |
| Vaporization Only | 2303 |
The number of ongoing pregnancies obtained which still is the most important issue for the patients. (NCT01682642)
Timeframe: 12 weeks
| Intervention | percentage of ongoing pregnancies (Number) |
|---|---|
| Zoladex | 39.3 |
| Vaporization Only | 39.7 |
number of 2PN (NCT01682642)
Timeframe: 1 day after oocyte retrieval
| Intervention | number of pro nuclear cells (Mean) |
|---|---|
| Zoladex | 5.4 |
| Vaporization Only | 5.6 |
number of MII cells retrieved (NCT01682642)
Timeframe: 3 weeks
| Intervention | MII cells (Mean) |
|---|---|
| Zoladex | 8.2 |
| Vaporization Only | 8.2 |
number of days needed before follicles in the ovary are mature for oocyte retrieval (NCT01682642)
Timeframe: 3 weeks
| Intervention | days (Mean) |
|---|---|
| Zoladex | 12.3 |
| Vaporization Only | 11.3 |
Complete cell cycle arrest is defined as Ki67 ≤ 2.7% following 2 weeks of neoadjuvant PD 0332991 (NCT01723774)
Timeframe: At cycle 1 day 15 (2 weeks)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 2: PIK3CA Mutant Type Cohort | 16 |
"Preoperative endocrine prognostic index (PEPI) score is derived from four factors assigned a numerical score following neoadjuvant endocrine therapy, including Ki67 expression in the surgical specimen, pathologic tumor size (indicated as T below), lymph node status (indicated as N below), and estrogen receptor (ER) level (indicated as ER Allred below).~PEPI-0 score indicates T1 or T2, N0, Ki67 < 2.7%, ER Allred > 2.~It predicts a low risk of recurrence." (NCT01723774)
Timeframe: At the time of surgery (estimated to be 5 months)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1: PIK3CA Wild Type Cohort | 3 |
| Arm 2: PIK3CA Mutant Type Cohort | 2 |
| Arm 3: Endocrine Resistant Cohort | 1 |
"The clinical response rate is the number of patients whose disease meets the WHO criteria of complete or partial response prior to surgery divided by the total number of eligible patients who began combination neoadjuvant treatment.~Complete Response (CR) is defined as the disappearance of all known disease based on a comparison between the pre-treatment measurements and the measurements taken at the completion of neo-adjuvant therapy (that is, at the end of cycle 4 neo-adjuvant combination therapy). In addition there is no appearance of new lesions.~Partial Response (PR) is defined as a 50% or greater decrease in the product of the bidimensional measurements of the lesion (total tumor size) between the pre-treatment measurements and the measurements taken at the completion of neo-adjuvant therapy (that is, at the end of cycle 4 neo-adjuvant combination therapy). In addition there can be no appearance of new lesions or progression of any lesion." (NCT01723774)
Timeframe: 16 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1: PIK3CA Wild Type Cohort | 21 |
| Arm 2: PIK3CA Mutant Type Cohort | 10 |
| Arm 3: Endocrine Resistant Cohort | 16 |
Complete cell cycle arrest is defined as Ki67 ≤ 2.7% following 2 weeks of neoadjuvant PD 0332991 (NCT01723774)
Timeframe: At cycle 1 day 15 (2 weeks)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 3: Endocrine Resistant Cohort | 19 |
Complete cell cycle arrest is defined as Ki67 ≤ 2.7% following 2 weeks of neoadjuvant PD 0332991 (NCT01723774)
Timeframe: At cycle 1 day 15 (2 weeks)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1: PIK3CA Wild Type Cohort | 23 |
-A pathologic complete response is defined as no histology evidence of invasive tumor cells in the surgical breast specimen and sentinel or axillary lymph nodes. (NCT01723774)
Timeframe: At the time of surgery (estimated to be 5 months)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1: PIK3CA Wild Type Cohort | 0 |
| Arm 2: PIK3CA Mutant Type Cohort | 0 |
| Arm 3: Endocrine Resistant Cohort | 0 |
To assess Ki67 level on serially collected tumor specimens (NCT01723774)
Timeframe: Cycle 1 day 15 and at time of surgery (approximately 2-4 weeks post completion of cycle 4 - each cycle is 28 days)
| Intervention | percentage of Ki67 in tumor sample (Mean) | |
|---|---|---|
| Cycle 1 Day 15 | At time of surgery | |
| Arm 1: PIK3CA Wild Type Cohort | 11.70 | 23.00 |
| Arm 2: PIK3CA Mutant Type Cohort | 0.51 | 8.75 |
| Arm 3: Endocrine Resistant Cohort | 0.97 | 2.84 |
"The radiological response rate is the number of patients whose disease meets with WHO criteria for complete or partial response at the evaluation prior to surgery divided by the total number of eligible patients who began combination neo-adjuvant therapy.~Complete Response (CR) is defined as the disappearance of all known disease based on a comparison between the pre-treatment measurements and the measurements taken at the completion of neo-adjuvant therapy (that is, at the end of cycle 4 neo-adjuvant combination therapy). In addition there is no appearance of new lesions.~Partial Response (PR) is defined as a 50% or greater decrease in the product of the bidimensional measurements of the lesion (total tumor size) between the pre-treatment measurements and the measurements taken at the completion of neo-adjuvant therapy (that is, at the end of cycle 4 neo-adjuvant combination therapy). In addition there can be no appearance of new lesions or progression of any lesion." (NCT01723774)
Timeframe: At the end of cycle 4 prior to surgery (estimated to be 16 weeks)
| Intervention | Participants (Count of Participants) |
|---|---|
| Arm 1: PIK3CA Wild Type Cohort | 7 |
| Arm 2: PIK3CA Mutant Type Cohort | 3 |
| Arm 3: Endocrine Resistant Cohort | 6 |
The maximum grade for each type of adverse event will be recorded for each patient using the NCI-CTCAE v4.0 coding scheme, and frequency tables will be reviewed to determine patterns. Additionally, the relationship (possibly related, probably related, and definitely related) of the adverse event(s) to the study treatment will be taken into consideration. (NCT01723774)
Timeframe: From start of adjuvant therapy through 30 days after completion of adjuvant therapy (estimated to be 2 years)
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Grade 1/2 anemia | Grade 1/2 blurred vision | Grade 1/2 watering eyes | Grade 1/2 diarrhea | Grade 1/2 gastritis | Grade 1/2 mucositis oral | Grade 1/2 nausea | Grade 1/2 vomiting | Grade 1/2 fatigue | Grade 1/2 upper respiratory infection | Grade 1/2 bruising | Grade 1/2 aspartate aminotransferase increased | Grade 1/2 lymphocyte count decreased | Grade 3/4 lymphocyte count decreased | Grade 1/2 neutrophil count decreased | Grade 3/4 neutrophil count decreased | Grade 1/2 platelet count decreased | Grade 1/2 white blood cell count decreased | Grade 3/4 white blood cell count decreased | Grade 1/2 hyperglycemia | Grade 1/2 arthralgia | Grade 1/2 alopecia | |
| Adjuvant Continuation | 1 | 1 | 1 | 1 | 1 | 1 | 2 | 1 | 1 | 1 | 1 | 1 | 3 | 2 | 2 | 3 | 1 | 1 | 2 | 1 | 1 | 2 |
The maximum grade for each type of adverse event will be recorded for each patient using the NCI-CTCAE v4.0 coding scheme, and frequency tables will be reviewed to determine patterns. Additionally, the relationship (possibly related, probably related, and definitely related) of the adverse event(s) to the study treatment will be taken into consideration. (NCT01723774)
Timeframe: From start of treatment through 30 days after completion of an estimated 4 months of neoadjuvant therapy
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Grade 1/2 anemia | Grade 1/2 dry eye | Grade 1/2 constipation | Grade 1/2 diarrhea | Grade 1/2 dry mouth | Grade 1/2 dyspepsia | Grade 1/2 flatulence | Grade 1/2 gastroesophageal reflux disease | Grade 1/2 gastrointestinal pain | Grade 1/2 mucositis oral | Grade 1/2 nausea | Grade 1/2 oral pain | Grade 1/2 rectal pain | Grade 1/2 stomatitis | Grade 1/2 vomiting | Grade 1/2 chills | Grade 1/2 edema limbs | Grade 1/2 fatigue | Grade 1/2 fever | Grade 1/2 localized edema | Grade 1/2 pain | Grade 1/2 shingles | Grade 1/2 sinusitis | Grade 1/2 urinary tract infection | Grade 1/2 seroma | Grade 1/2 alanine aminotransferase increased | Grade 3/4 alanine aminotransferase increased | Grade 1/2 aspartate aminotransferase increased | Grade 3/4 aspartate aminotransferase increased | Grade 1/2 lymphocyte count decreased | Grade 1/2 neutrophil count decreased | Grade 3/4 neutrophil count decreased | Grade 1/2 platelet count decreased | Grade 1/2 weight loss | Grade 1/2 white blood cell decreased | Grade 3/4 white blood cell decreased | Grade 1/2 anorexia | Grade 1/2 hypocalcemia | Grade 1/2 hypokalemia | Grade 1/2 hyponatremia | Grade 1/2 arthralgia | Grade 1/2 back pain | Grade 1/2 bone pain | Grade 1/2 myalgia | Grade 1/2 osteoporosis | Grade 1/2 dizziness | Grade 1/2 dysgeusia | Grade 1/2 headache | Grade 1/2 memory impairment | Grade 1/2 peripheral motor neuropathy | Grade 1/2 peripheral sensory neuropathy | Grade 1/2 confusion | Grade 1/2 depression | Grade 1/2 insomnia | Grade 1/2 pelvic pain | Grade 1/2 allergic rhinitis | Grade 1/2 cough | Grade 1/2 dyspnea | Grade 1/2 epistaxis | Grade 1/2 nasal congestion | Grade 1/2 postnasal drip | Grade 1/2 sore throat | Grade 1/2 alopecia | Grade 1/2 dry skin | Grade 1/2 hyperhidrosis | Grade 1/2 papulopustular rash | Grade 1/2 pruritus | Grade 1/2 rash maculo-papular | Grade 3/4 rash maculo-papular | Grade 1/2 fever blister | Grade 1/2 itching | Grade 1/2 hot flashes | |
| Arm 1: PIK3CA Wild Type Cohort | 4 | 0 | 4 | 4 | 0 | 1 | 1 | 0 | 0 | 9 | 8 | 0 | 1 | 1 | 0 | 2 | 1 | 15 | 3 | 0 | 0 | 1 | 1 | 0 | 0 | 1 | 1 | 1 | 1 | 3 | 14 | 7 | 6 | 1 | 23 | 0 | 2 | 3 | 1 | 1 | 5 | 2 | 1 | 2 | 0 | 3 | 1 | 5 | 1 | 0 | 1 | 0 | 2 | 2 | 1 | 1 | 2 | 0 | 1 | 1 | 1 | 0 | 1 | 2 | 2 | 1 | 1 | 1 | 1 | 1 | 0 | 10 |
| Arm 2: PIK3CA Mutant Type Cohort | 5 | 0 | 3 | 1 | 0 | 1 | 1 | 1 | 0 | 3 | 3 | 0 | 0 | 0 | 0 | 1 | 0 | 8 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 4 | 6 | 5 | 0 | 6 | 1 | 3 | 0 | 0 | 0 | 4 | 1 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 4 | 1 | 2 | 0 | 1 | 0 | 0 | 0 | 0 | 7 |
| Arm 3: Endocrine Resistant Cohort | 7 | 1 | 1 | 0 | 1 | 0 | 1 | 0 | 1 | 3 | 10 | 1 | 0 | 0 | 2 | 0 | 0 | 6 | 1 | 0 | 1 | 0 | 0 | 1 | 1 | 0 | 0 | 0 | 0 | 1 | 12 | 13 | 3 | 0 | 11 | 2 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 0 | 0 | 2 | 0 | 1 | 0 | 0 | 0 | 1 | 0 | 0 | 1 | 2 | 1 | 0 | 0 | 1 | 2 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 3 |
Compare rate of complete cell cycle arrest (defined as Ki67 ≤ 2.7%) arrest between C1D1 and C1D15 (NCT01723774)
Timeframe: Cycle 1 day 1 and cycle 1 day 15 (2 weeks)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Cycle 1 Day 1 complete cell cycle arrest | Cycle 1 Day 15 complete cell cycle arrest | |
| Arm 1: PIK3CA Wild Type Cohort | 8 | 23 |
| Arm 2: PIK3CA Mutant Type Cohort | 4 | 16 |
| Arm 3: Endocrine Resistant Cohort | 0 | 19 |
To assess Ki67 level on serially collected tumor specimens (NCT01723774)
Timeframe: Pre-treatment and cycle 1 day 15
| Intervention | percentage of Ki67 in tumor sample (Mean) | |
|---|---|---|
| Pre-treatment | Cycle 1 Day 15 | |
| Arm 1: PIK3CA Wild Type Cohort | 29.75 | 8.18 |
| Arm 2: PIK3CA Mutant Type Cohort | 19.76 | 0.51 |
| Arm 3: Endocrine Resistant Cohort | 33.52 | 15.27 |
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 |
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 |
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 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 |
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 |
(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 |
Any woman whose Ki67 value ≤10% on cycle 1 day 17 of combination treatment who does not receive alternative treatment prior to surgery and has no histologic evidence of invasive tumor cells in the surgical breast specimen and the axillary lymph nodes is considered to have a pathological complete response (pCR). A ninety percent confidence interval for the true pathologic complete response rate will be calculated using the Duffy-Santer approach. (NCT01776008)
Timeframe: At time of surgery (up to 3 weeks after 4, 28-day cycles)
| Intervention | participants (Number) |
|---|---|
| Treatment (MK2206, Anastrozole, Goserelin Acetate) | 0 |
The maximum grade for each type of adverse event will be recorded for each patient, and frequency tables will be reviewed to determine patterns. For this endpoint, we are reporting the number of patients that reported a grade 3 or higher graded adverse event during neoadjuvent treatment. A complete list of all reported adverse events is in the Adverse Events section of the report. (NCT01776008)
Timeframe: Baseline to end of Cycle 4 (28 day cycles)
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Grade 3+ Adverse Event | Grade 4+ Adverse Event | |
| Treatment (MK2206, Anastrozole, Goserelin Acetate) | 6 | 2 |
Percentage of Tumor-infiltrating lymphocytes present in the stroma in tissue specimen. (NCT02003209)
Timeframe: 2.8 years
| Intervention | percentage of TILs (Median) | |
|---|---|---|
| No pCR | pCR | |
| Arm I (Combination Chemotherapy, Surgery, Radiation) | 10 | 10 |
| Arm II (Chemo, Estrogen Deprivation, Surgery, Radiation) | 10 | 10 |
Proportion of patients with pCR evaluated histologically, and defined as the absence of any invasive component in the resected breast specimen and all resected lymph nodes following completion of neoadjuvant therapy calculated separately for premenopausal and postmenopausal women. (NCT02003209)
Timeframe: Up to 2.8 years (when all patients completed primary breast surgery)
| Intervention | percentage of participants with pCR (Number) | |
|---|---|---|
| Premenopausal Women | Postmenopausal Women | |
| Arm I (Combination Chemotherapy, Surgery, Radiation) | 44.2 | 38.2 |
| Arm II (Chemo, Estrogen Deprivation, Surgery, Radiation) | 46.2 | 45.5 |
Percentage of patients with grade 1 or higher toxicity from the Cardiac Disorders System Organ Class. (NCT02003209)
Timeframe: Up to 6 weeks post surgery
| Intervention | percentage of pts with cardiac toxicity (Number) |
|---|---|
| Arm I (Combination Chemotherapy, Surgery, Radiation) | 4.46 |
| Arm II (Chemo, Estrogen Deprivation, Surgery, Radiation) | 4.46 |
Proportion of patients with pCR evaluated histologically, and defined as the absence of any invasive component in the resected breast specimen and all resected lymph nodes following completion of neoadjuvant therapy. (NCT02003209)
Timeframe: Up to 2.8 years (when all patients completed primary breast surgery)
| Intervention | percentage of participants (Number) |
|---|---|
| Arm I (Combination Chemotherapy, Surgery, Radiation) | 41.2 |
| Arm II (Chemo, Estrogen Deprivation, Surgery, Radiation) | 45.8 |
Proportion of patients with pCR in the breast, defined as the absence of any invasive component in the resected breast specimen. (NCT02003209)
Timeframe: Up to 2.8 years (when all patients completed primary breast surgery)
| Intervention | percentage of participants (Number) |
|---|---|
| Arm I (Combination Chemotherapy, Surgery, Radiation) | 44.4 |
| Arm II (Chemo, Estrogen Deprivation, Surgery, Radiation) | 47.1 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
(NCT02059213)
Timeframe: Up to 54 months
| Intervention | Participants (Count of Participants) |
|---|---|
| ADT Alone | 13 |
| ADT + Ibrance® | 22 |
Nausea and anorexia were measured by The Functional Assessment of Anorexia/Cachexia Treatment (FAACT)-additional concerns, which had 12 items, all items were rated on a 5-point Likert scale from 0 to 4. FAACT-additional concerns subscale score was calculated based on scoring manual. Subscale score ranges from 0 to 48, and higher scores indicate less nausea and anorexia. The primary comparison of patient-reported nausea and anorexia between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3
| Intervention | units on a scale (Mean) |
|---|---|
| Arm A (Exemestane, Entinostat) | 35.8 |
| Arm B (Exemestane, Placebo) | 37.0 |
Progression-free survival (PFS) was defined to be time from randomization to the earliest documented disease progression as defined by the RECIST criteria, new primary breast cancer, or death without progression. Disease assessment was to continue until disease progression, even after non-protocol anti-cancer therapy was started. Cases with incomplete follow up or without adequate disease evaluations were censored at the date last documented to be free of progression, regardless of whether non-protocol anti-cancer therapy was started or not. Disease progression was based on central review, and defined as at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study. In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. In addition, the appearance of one or more new lesions was also considered progression. Kaplan-Meier method was used to estimate PFS rate. (NCT02115282)
Timeframe: Assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression
| Intervention | months (Median) |
|---|---|
| Arm A (Exemestane, Entinostat) | 3.3 |
| Arm B (Exemestane, Placebo) | 3.1 |
Time-to-treatment deterioration (TTD) was defined as time from randomization to disease progression or death or worsening of symptoms, whichever occurred first. Disease progression was assessed per RECIST v1.1. Symptoms deterioration was measured by 6 items (GP1, GP2, GP4, GF7, B1, P2, scored 0-24) from the 8-item FACT-Breast Symptom Index (FBSI). Symptom deterioration was defined as two consecutive available decreases of at least 3 points from baseline using the 6-item FBSI in this trial, and the second visit time was used as the time of symptom deterioration in this case, unless it was the final score, for which one decrease was sufficient. Kaplan-Meier method was used to estimate the median TTD and TTD rate at a certain time point. Symptoms were assessed every cycle for the first six months after randomization, every two cycles between 6 months and 1 year. It then were assessed based on the same schedule for tumor assessments until disease progression as specified below. (NCT02115282)
Timeframe: Disease assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression
| Intervention | months (Median) |
|---|---|
| Arm A (Exemestane, Entinostat) | 2.9 |
| Arm B (Exemestane, Placebo) | 2.9 |
Objective response rate was defined as number of patients with complete response (CR) or partial response (PR) divided by all randomized patients. Responses were evaluated using the revised Response Evaluation Criteria in Solid Tumors (RECIST) guideline. CR was defined as disappearance of all target and non-target lesions. PR was defined as at least a 30% decrease in the sum of the diameters of target lesions (taking as reference the baseline sum diameters), and/or persistence of one or more non-target lesion(s). (NCT02115282)
Timeframe: Assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression
| Intervention | percentage of participants (Number) |
|---|---|
| Arm A (Exemestane, Entinostat) | 4.6 |
| Arm B (Exemestane, Placebo) | 4.3 |
Overall survival (OS) was defined to be time from randomization to death from any cause. Cases who were still alive were censored at the date last known alive. (NCT02115282)
Timeframe: Assessed every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until death
| Intervention | months (Median) |
|---|---|
| Arm A (Exemestane, Entinostat) | 23.4 |
| Arm B (Exemestane, Placebo) | 21.7 |
Diarrhea was measured by Functional Assessment of Chronic Illness Therapy for Patients With Diarrhea (FACIT-Diarrhea) subscale form, which had 11 items, all items were rated on a 5-point Likert scale from 0 to 4. FACIT-Diarrhea subscale score was calculated based on the scoring manual, subscale score ranges from 0 to 44, and higher score indicates less diarrhea. The primary comparison of patient-reported diarrhea between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3
| Intervention | units on a scale (Mean) |
|---|---|
| Arm A (Exemestane, Entinostat) | 38.8 |
| Arm B (Exemestane, Placebo) | 41.5 |
Fatigue was measured by PROMIS Fatigue short form, it had 7 items and all items were rated on a 5-point Likert scale from 1 to 5. The PROMIS Fatigue total score and T score were calculated based on the scoring manual. The total score ranges from 7 to 35, the T score ranges from 29.4 to 83.2, higher scores indicate more fatigue. The PROMIS Fatigue T score was used for arm comparison. The primary comparison of patient-reported fatigue between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3
| Intervention | T-score (Mean) |
|---|---|
| Arm A (Exemestane, Entinostat) | 55.5 |
| Arm B (Exemestane, Placebo) | 54.1 |
Health-related quality of life (HRQL) was measured using Functional Assessment of Cancer Therapy - General (FACT-G). The primary endpoint for HRQL was the FACT-G Trial Outcome Index (TOI) which was an aggregate score of 5 items from the FACT-G-Physical subscale (GP2, GP3, GP4, GP6, and GP7) and 6 items from the FACT-G-Functional subscale (GF1, GF2, GF3, GF4, GF6, and GF7). All items were rated on a 5-point Likert scale from 0 to 4. FACT-G TOI subscale score was calculated based on the scoring manual, subscale score ranges from 0 to 44, and higher scores indicate better quality of life. The primary comparison of HRQL between treatment arms was based on the end of cycle 3 assessment. (NCT02115282)
Timeframe: Assessed at baseline and end of cycle 3
| Intervention | units on a scale (Mean) |
|---|---|
| Arm A (Exemestane, Entinostat) | 20.5 |
| Arm B (Exemestane, Placebo) | 20.9 |
Peripheral blood samples (PBMCs) were collected prior to therapy and on Days 8 and 15 of cycle 1, for assessment of lysine acetylation, using an assay developed by the Trepel Laboratory, NCI/NIH. CD45 blood mononuclear cells were measured. Patients with lysine acetylation change of 1.5 folds or higher were compared to patients with lysine acetylation change of less than 1.5 folds. (NCT02115282)
Timeframe: Disease assessed at baseline, then every 12 weeks until treatment discontinuation, then every 3 months within 2 years from study entry, every 6 months between 2-5 years and annually between 6-10 years from study entry, until first disease progression
| Intervention | months (Median) |
|---|---|
| Arm A (Exemestane, Entinostat)- Lysine Acetylation Change>=1.5 Fold | 2.8 |
| Arm A (Exemestane, Entinostat)- Lysine Acetylation Change<1.5 Fold | 2.7 |
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 |
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 |
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 |
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 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 |
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 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 |
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 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 |
ORR is the percentage of participants with the best overall response of complete response (CR) or partial response (PR) according to RECIST 1.1. 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. (NCT02278120)
Timeframe: Up to approximately 25 months
| Intervention | Percentage of participants (Number) |
|---|---|
| LEE011 + NSAI/Tamoxifen + Goserelin | 40.9 |
| LEE011 Placebo + NSAI/Tamoxifen+ Goserelin | 29.7 |
Percentage of participants with complete response (CR) or partial response (PR) or stable disease (SD) lasting 24 weeks or longer as defined in RECIST 1.1.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: PD = At least a 20% increase in the sum of diameter of all measured target lesions, taking as reference the smallest sum of diameter of all target lesions recorded at or after baseline. In addition to the relative increase of 20% the sum must also demonstrate an absolute increase of at least 5 mm. (NCT02278120)
Timeframe: Up to approximately 25 months
| Intervention | Percentage of participants (Number) |
|---|---|
| LEE011 + NSAI/Tamoxifen + Goserelin | 79.1 |
| LEE011 Placebo + NSAI/Tamoxifen+ Goserelin | 69.7 |
Time from the first documented response (CR or PR) to the first documented progression or death due to underlying cancer (NCT02278120)
Timeframe: Up to approximately 25 months
| Intervention | Months (Median) |
|---|---|
| LEE011 + NSAI/Tamoxifen + Goserelin | 21.3 |
| LEE011 Placebo + NSAI/Tamoxifen+ Goserelin | 17.5 |
Time to response is the time from the date of randomization to the first documented response (CR or PR, which must be confirmed subsequently) according to RECIST 1.1. All patients will be included in time to response calculations. Patients who do not achieve a confirmed response will be censored at the maximum follow-up time (i.e. first patient first visit to last patient last visit used for the analysis) for patients who had a PFS event (i.e. either progressed or died due to any cause) or at the date of last adequate tumor assessment otherwise. (NCT02278120)
Timeframe: Up to approximately 25 months
| Intervention | months (Median) |
|---|---|
| LEE011 + NSAI/Tamoxifen + Goserelin | NA |
| LEE011 Placebo + NSAI/Tamoxifen+ Goserelin | NA |
PFS, defined as the time from the date of randomization to the date of the first documented progression or death due to any cause and assessed according to Response Evaluation Criteria In Solid Tumors (RECIST) v1.1]. PFS was assessed via a local radiology assessment according to RECIST 1.1 (NCT02278120)
Timeframe: Up to approximatley 25 months
| Intervention | Months (Median) |
|---|---|
| LEE011 + NSAI/Tamoxifen + Goserelin | 23.8 |
| LEE011 Placebo + NSAI/Tamoxifen+ Goserelin | 13.0 |
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 |
"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 |
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 |
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 |
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 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 |
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 |
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 |
ERG protein overexpression was evaluated using immunohistochemistry in post treatment specimens. A positive ETS-related ERG overexpression is a bad outcome. (NCT02430480)
Timeframe: Approximately one month-3 months post-treatment
| Intervention | Participants (Count of Participants) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 14 |
"The effect of intense androgen suppression and inhibition was measured on tumors using anti-AR immunostains of biopsy and surgical specimens. Detection of tumor nuclear AR was quantified on a per-nucleus basis using computer-aided image analysis with Definiens Developer XD 64, grouping nuclei into high, medium, low, and absent bins, a histology score was assigned to each sample.~Nucleus classification is low vs. med. at 0.7; med. vs. high at 0.95. Definiens reported the total # of positively stained nuclei or cells, along with the distribution of low-, med.-, and high-intensity stained nuclei/cells for ea. tumor focus. A %positive index score was calculated using a weighted avg. divided by the total # of objects, where index = [ (1 × nuclei/cells stained low) + (2 × nuclei/cells stained med.) + (3 × nuclei/cells stained high) ](3 × total nuclei)." (NCT02430480)
Timeframe: 6 months
| Intervention | scores on a scale (Median) | |
|---|---|---|
| biopsy specimen | residual tumor | |
| 1/Arm 1- Enzalutamide and Goserelin | 0.7568 | 0.1661 |
Prostate lesion volumes on baseline and post-treatment multiparametric magnetic resonance imaging (mpMRI) were calculated from T2W-MRI sequences using software embedded in the PACS after manual contouring by the same radiologist. Lesion volume scores were categorized as low (2 or fewer positive sequences), moderate (3 positive sequences) and high (4 positive sequences). Lesion volume values are in cubic centimeters (cc's). (NCT02430480)
Timeframe: Baseline and 6 months
| Intervention | cubic centimeters (Median) | |
|---|---|---|
| Baseline | 6 months | |
| 1/Arm 1- Enzalutamide and Goserelin | 39.5 | 20.0 |
The prostate lesion is contoured manually by an expert radiologist. Research software (mim-vista) calculates the volume. Greater tumor volumes may indicate higher prostate tumor growth. (NCT02430480)
Timeframe: Baseline and 6 months
| Intervention | cc (Median) | |
|---|---|---|
| Baseline | 6 months | |
| 1/Arm 1- Enzalutamide and Goserelin | 3.44 | 0.62 |
The Youden index was used as a measure for evaluating biomarker effectiveness and was calculated to determine the cutoffs that gave the optimal combination of sensitivity and specificity for patient response to treatment. The index is: J=sensitivity + specificity -1. Its value ranges from 0 through 1 (inclusive). A value of 1 indicates that there are no false positives or false negatives, i.e. the test is perfect. The index gives equal weight to false positive and false negative values, so all tests with the same value of the index give the same proportion of total misclassified results. Sensitivity and specificity are the probability of truly identifying relative tumor burden on multiparametric magnetic resonance imaging (mpMRI) respectively at a statistically established cut point. (NCT02430480)
Timeframe: 6 months
| Intervention | Percentage of sensitivity (Number) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 81 |
The Youden index was used as a measure for evaluating biomarker effectiveness and was calculated to determine the cutoffs that gave the optimal combination of sensitivity and specificity for patient response to treatment. The index is: J=sensitivity + specificity -1. Its value ranges from 0 through 1 (inclusive). A value of 1 indicates that there are no false positives or false negatives, i.e. the test is perfect. The index gives equal weight to false positive and false negative values, so all tests with the same value of the index give the same proportion of total misclassified results. Sensitivity and specificity are the probability of truly identifying relative tumor burden on multiparametric magnetic resonance imaging (mpMRI) respectively at a statistically established cut point. (NCT02430480)
Timeframe: 6 months
| Intervention | Percentage of specificity (Number) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 87 |
Complete response was evaluated after neoadjuvant treatment with androgen deprivation therapy (ADT) and enzalutamide and assessed by pathologic exam. Pathologic complete response: the absence of residual invasive cancer confirmed by immunohistochemistry (IHC). (NCT02430480)
Timeframe: After neoadjuvant treatment with androgen deprivation therapy (ADT) and enzalutamide, approximately 6 months
| Intervention | Participants (Count of Participants) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 2 |
PTEN level reduction was evaluated using immunohistochemistry in post treatment specimens. For anti-PTEN immunohistochemistry, a case was considered PTEN-reduced (abnormal) if at least 5% of tumor cells demonstrated reduced PTEN intensity relative to PTEN in benign cells (lower than 5%, then abnormal). (NCT02430480)
Timeframe: post treatment, approximately 1-3 months
| Intervention | Participants (Count of Participants) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 21 |
Here is the number of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria for 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. (NCT02430480)
Timeframe: Date treatment consent signed to date off study, approximately 51 months and 2 days.
| Intervention | Participants (Count of Participants) |
|---|---|
| 1/Arm 1- Enzalutamide and Goserelin | 38 |
Adverse events were assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0). A non-serious adverse event (i.e., Grade 1) is any untoward medical occurrence. A serious adverse event (i.e., Grade 2-3) is an adverse event or suspected adverse reaction that results in an adverse drug experience, and/or disruption of the ability to conduct normal life functions attributable to the research. (NCT02430480)
Timeframe: Date treatment consent signed to date off study, approximately 51 months and 2 days.
| Intervention | Adverse events (Number) | ||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Fatigue | Edema, limbs | Erectile dysfunction | Gynecomastia | Hot flashes | Hypertension | Confusion | Libido decreased | Insomnia | Mood changes | Personality change | Restlessness | Headache | Dizziness | Memory impairment | Concentration impairment | Dysuria | Urinary incontinence | Dysgeusia | Dyspepsia | Nausea | Cough | Sore throat | Arthralgia | Back pain | Muscle weakness | Myalgia | Rash | Weight gain | |
| Grade 1 | 20 | 2 | 9 | 3 | 34 | 1 | 2 | 15 | 12 | 2 | 3 | 2 | 5 | 5 | 3 | 3 | 1 | 2 | 1 | 2 | 4 | 3 | 2 | 2 | 3 | 2 | 2 | 1 | 2 |
| Grade 2 | 2 | 0 | 3 | 0 | 1 | 7 | 0 | 0 | 4 | 0 | 0 | 1 | 0 | 0 | 0 | 0 | 1 | 4 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 1 | 2 | 0 |
| Grade 3 | 0 | 0 | 1 | 0 | 0 | 7 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
Prostate lesion volumes on baseline and post-treatment mpMRI were calculated from T2W-MRI sequences using software embedded in the PACS after manual contouring by the same radiologist. (NCT02430480)
Timeframe: Baseline and 6 months
| Intervention | Lesions (Number) | |
|---|---|---|
| Baseline | 6 months | |
| 1/Arm 1- Enzalutamide and Goserelin | 58 | 40 |
Overall Survival & Tumor Free Survival (NCT02518191)
Timeframe: 5 years
| Intervention | months (Mean) |
|---|---|
| GnRHa Group | 48.17 |
| None GnRHa Group | 49.33 |
The serum levels of anti-Müllerian hormone (AMH) were measured using human AMH ELISA kit (11351, Biofine)). POI (premature ovarian insufficiency) was defined as AMH<0.5ng/mL in this study. (NCT02518191)
Timeframe: 1 years
| Intervention | Participants (Count of Participants) |
|---|---|
| GnRHa (Gonadotrophin-releasing Hormone Analogues) Group | 10 |
| None GnRHa (Gonadotrophin-releasing Hormone Analogues) Group | 38 |
Occurrence of Overall Survival at 6 months. OS: On study date to expired date or last visit date if not deceased. (NCT02586675)
Timeframe: 6 months
| Intervention | percentage of participants (Number) |
|---|---|
| Tamoxifen and Ribociclib With Goserelin | 83.3 |
Occurrence of Progression Survival at 6 months. PFS: On study date to date of progression or the same as overall survival time if not progressed. Progressive Disease (PD): At least a 20% increase in the sum of the longest diameter (LD) of target lesions, taking as reference the smallest sum LD recorded since the treatment started or the appearance of one or more new lesions. (NCT02586675)
Timeframe: 6 months
| Intervention | percentage of participants (Number) |
|---|---|
| Tamoxifen and Ribociclib With Goserelin | 57.1 |
400-600 mg of Ribociclib, when taken with Tamoxifen 20 mg. The Phase I portion of the study is a dose escalation to confirm the dose limiting toxicity (DLT) and the RP2D for ribociclib with Tamoxifen. DLT is defined as an adverse event or abnormal laboratory value assessed as having a reasonable possibility related to the study medication, unrelated to disease, disease progression, inter-current illness, or concomitant medications that occurs within the first 28 days of treatment (cycle 1) with LEE011 and Tamoxifen. National Cancer Institute Common Terminology Criteria for Adverse events (NCI CTCAE) version 4.03 will be used for all grading. In this study, a DLT will occur if CTCAE grade 4 neutropenia lasts more than 4 consecutive days, if CTCAE grade 3 thrombocytopenia is associated with clinically significant bleeding or if there is grade 4 thrombocytopenia. (NCT02586675)
Timeframe: Up to 12 months
| Intervention | dose in mg (Number) |
|---|---|
| Tamoxifen and Ribociclib With Goserelin | 400 |
-The descriptions and grading scales found in the revised NCI Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 will be utilized for all toxicity reporting. (NCT02907918)
Timeframe: 30 days after completion of neoadjuvant therapy (approximately 21 weeks)
| Intervention | Participants (Count of Participants) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Neutrophil count decreased | Lymphocyte count decreased | Hypertension | White blood cell decreased | Colitis | Hypokalemia | Pulmonary edema | Ventricular tachycardia | Alanine aminotransferase increased | Aspartate aminotransferase increased | Colonic obstruction | |
| Palbociclib + Letrozole + Trastuzumab +/- Goserelin | 13 | 1 | 8 | 2 | 1 | 1 | 1 | 1 | 1 | 1 | 1 |
"Answers ranging from None to Very Severe (none=0 to very severe=4); Not at All to Very Much (not at all=0 to very much=4), Never to Almost Constantly (0=never to almost constantly=4)~PRO-CTCAE responses are scored from 0 to 4, and there are no standardized scoring rules yet established for how to combine attributes into a single score or how best to analyze PRO-CTCAE data longitudinally.~PRO-CTCAE scores for each attribute (frequency, severity and/or interference) will be presented descriptively" (NCT02907918)
Timeframe: Baseline, cycle 2 day 1 (approximately 29 days), and end of cycle 4 (approximately 16 weeks)
| Intervention | score on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| In the last 7 days, what was the severity of your decreased appetite at its worst? | In the last 7 days, how much did decreased appetite interfere with your usual or daily activities? | In the last 7 days, how often did you have nausea? | In the last 7 days, what was the severity of your nausea at its worst? | In the last 7 days, what was the severity of your shortness of breath (SOB) at its worst? | In the last 7 days, how much did your SOB interfere with your usual or daily activities? | In the last 7 days, what was the severity of your cough at its worst? | In the last 7 days, how much did your cough interfere with your usual and daily activities? | In the last 7 days, how often did you have arm or leg swelling? | In the last 7 days, what was the severity of your arm or leg swelling at its worst? | In the last 7 days, how much did arm or leg swelling interfere with your usual or daily activities? | In the last 7 days, how often did you feel a pounding or racing heartbeat (palpitations)? | In the last 7 days, what was the severity of your pounding or racing heartbeat at its worst? | In the last 7 days, did you have any rash? | In the last 7 days, what was the severity of your dry skin at its worst? | In the last 7 days, did you have any hair loss? | In the last 7 days, what was the severity of your problems with concentration at their worst? | In the past 7 days, how much did problems with concentration interfere with usual/daily activities? | |
| Baseline: Palbociclib + Letrozole + Trastuzumab +/- Goserelin | 1.3461538 | 1.0769231 | 1.2307692 | 1.1923077 | 1.1923077 | 0.9615385 | 1.1923077 | 1.0000000 | 1.0000000 | 0.8846154 | 0.9230769 | 1.1538462 | 1.0384615 | 1.8461538 | 1.3076923 | 1.0769231 | 1.1923077 | 1.1538462 |
| Cycle 2 Day 1: Palbociclib + Letrozole + Trastuzumab +/- Goserelin | 1.3461538 | 0.9615385 | 1.5000000 | 1.4230769 | 1.1153846 | 1.0384615 | 1.2307692 | 1.0384615 | 1.0384615 | 1.0384615 | 0.8846154 | 1.1923077 | 1.1923077 | 1.6153846 | 1.6923077 | 1.1153846 | 1.5000000 | 1.3076923 |
| End of Cycle 4: Palbociclib + Letrozole + Trastuzumab +/- Goserelin | 1.3043478 | 1.0434783 | 1.2608696 | 1.2173913 | 1.4347826 | 1.173913 | 1.5217391 | 1.3043478 | 1.2608696 | 1.1304348 | 1.0434783 | 1.173913 | 1.1304348 | 1.826087 | 1.5652174 | 1.6086957 | 1.4782609 | 1.3478261 |
A pathologic complete response (pCR) is defined as no histology evidence of invasive tumor cells in the surgical breast specimen and sentinel or axillary lymph nodes. (NCT02907918)
Timeframe: Completion of 4 cycles of treatment (approximately 16 weeks)
| Intervention | Participants (Count of Participants) |
|---|---|
| Palbociclib + Letrozole + Trastuzumab +/- Goserelin | 2 |
"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 |
"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 |
"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 |
"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 |
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 |
"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 |
"The descriptions and grading scales found in the revised NCI Common Terminology Criteria for Adverse Events (CTCAE) version 4.0 will be utilized for all toxicity reporting.~Grade 3 neutropenia: <1000-500/mm^3; <1.0-0.5 x 10e9/L~Grade 4 neutropenia: <500/mm^3; <0.5 x 10e9/L" (NCT03007979)
Timeframe: Through the first 29 days of treatment
| Intervention | Participants (Count of Participants) |
|---|---|
| Palbociclib + Letrozole or + Fulvestrant | 10 |
PFS based on radiologic assessment by investigator using RECIST 1.1 criteria (NCT03096847)
Timeframe: Up to approximately month 25
| Intervention | Months (Median) |
|---|---|
| Ribociclib + Letrozole Cohort A | 21.8 |
| Ribociclib + Letrozole Cohort B1 | 16.5 |
| Ribociclib + Letrozole Cohort B2 | 8.8 |
Time to 10% deterioration in the European Organisation for Research and Treatment of Cancer (EORTC) global health status (NCT03096847)
Timeframe: up to approximately 10 months
| Intervention | months (Median) |
|---|---|
| Ribociclib + Letrozole Cohort A | 3.3 |
| Ribociclib + Letrozole Cohort B1 | 3.7 |
| Ribociclib + Letrozole Cohort B2 | 2.8 |
| Total | 3.0 |
On treatment deaths were collected from FPFT up to 30 days after study drug discontinuation, for a maximum duration of 1150 days (approx 3.15 years). (Treatment duration ranged from 2 days to 1120 days). Deaths post treatment survival follow up were collected after the on- treatment period, up to approx. 3.15 years. Patients who didn't die during the on-treatment period and had not stopped study participation at the time of data cut-off (end of study) were censored. (NCT03096847)
Timeframe: on-treatment deaths: up to approx 3.15 years; all deaths: approx 3.15 years
| Intervention | Participants (Number) | |
|---|---|---|
| on-treatment deaths | Total deaths | |
| Ribociclib + Letrozole Cohort A | 6 | 67 |
| Ribociclib + Letrozole Cohort B1 | 0 | 9 |
| Ribociclib + Letrozole Cohort B2 | 6 | 60 |
| Total | 12 | 136 |
"The QLQ-C30 is the core questionnaire of the EORTC QLQ, which has been developed for the assessment of the health-related QOL of cancer patients participating in international clinical trials. Using a linear transformation to standardize the raw scores, all scores finally range from 0 to 100, where a higher score represents a higher response level, e.g., a higher (better) level of functioning (applies to the first 6 items, items 1 to 6), but a higher (worse) level of symptoms (applies to the last 9 items, items 7 to 15). There is no aggregated total score, i.e., all scale scores were analyzed separately." (NCT03096847)
Timeframe: Change from Baseline to Week 24
| Intervention | Scores on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Global health status - Change from baseline to Week 24 (C7D1) | Physical Functioning - Change from baseline to Week 24 (C7D1) | Role Functioning - Change from baseline to Week 24 (C7D1) | Emotional Functioning - Change from baseline to Week 24 (C7D1) | Cognitive Functioning - Change from baseline to Week 24 (C7D1) | Social Functioning - Change from baseline to Week 24 (C7D1) | Fatigue - Change from baseline to Week 24 (C7D1) | Nausea / Vomiting - Change from baseline to Week 24 (C7D1) | Pain - Change from baseline to Week 24 (C7D1) | Dyspnoea - Change from baseline to Week 24 (C7D1) | Insomnia - Change from baseline to Week 24 (C7D1) | Appetite loss - Change from baseline to Week 24 (C7D1) | Constipation - Change from baseline to Week 24 (C7D1) | Diarrhea - Change from baseline to Week 24 (C7D1) | Financial Problems - Change from baseline to Week 24 (C7D1) | |
| Ribociclib + Letrozole Cohort A | 8.8 | -3.1 | -6.6 | -9.6 | 2.7 | -6.9 | 6.3 | 0.1 | 13.2 | 3.8 | 4.2 | 11.2 | -2.7 | 2.6 | 0.2 |
| Ribociclib + Letrozole Cohort B | 6.1 | -2.4 | -3.9 | -4.6 | 1.3 | -7.0 | 5.1 | -3.9 | 10.1 | -3.7 | 5.2 | 2.2 | -2.6 | 1.9 | -1.9 |
| Ribociclib + Letrozole Cohort B1 | 11.7 | -3.6 | -17 | -9.4 | 2.2 | -16 | 11.1 | 1.1 | 15.6 | 4.4 | 6.7 | 6.7 | 2.2 | 0.0 | -4.4 |
| Ribociclib + Letrozole Cohort B2 | 5.0 | -2.2 | -1.3 | -3.6 | 1.1 | -5.3 | 3.9 | -4.9 | 9.0 | -5.3 | 4.9 | 1.4 | -3.6 | 2.3 | -1.4 |
Clinical Benefit Rate (CBR) after 24 weeks of treatment as defined by RECIST 1.1 as percentage of patients with Complete Response (CR), Partial response (PR) or Stable disease (SD) lasting 24 weeks or longer as well as patients with Non-complete response, nonprogressive disease (NCRNPD). (NCT03096847)
Timeframe: At 24 weeks after last patient enrolled in trial
| Intervention | Percentage of Participants (Number) | |
|---|---|---|
| CBR by week 24 (= BOR of CR or PR or SD or NCRNPD(Confirmed Best Overall Response (BOR)) | CBR by week 24 (= BOR of CR or PR or SD or NCRNPD (non-confirmed BOR) | |
| Ribociclib + Letrozole Cohort A | 63.2 | 71.7 |
| Ribociclib + Letrozole Cohort B1 | 57.7 | 69.2 |
| Ribociclib + Letrozole Cohort B2 | 56.5 | 64.3 |
| Total | 60.8 | 69.2 |
Adverse Events (AEs) were separated into TEAEs (defined as AEs occurring/worsening from first study drug treatment until 30 days after the last study drug treatment) and AEs in the pre-/post-treatment period. (NCT03096847)
Timeframe: Up to Week 72
| Intervention | Number of Participants (Number) | |||||
|---|---|---|---|---|---|---|
| Total AEs (i.e., Includes any type of AE.) | Serious AEs | Non-serious AEs | AEs with suspected relationship to ribociclib | AEs leading to discontinuation of ribociclib | AEs with fatal outcome | |
| Ribociclib + Letrozole Cohort A | 318 | 97 | 317 | 302 | 76 | 6 |
| Ribociclib + Letrozole Cohort B1 | 25 | 5 | 25 | 25 | 7 | 0 |
| Ribociclib + Letrozole Cohort B2 | 157 | 45 | 157 | 144 | 38 | 6 |
Overall response rate (ORR) is the best overall response (BOR) of complete response (CR) or partial response (PR) as defined by RECIST 1.1. (NCT03096847)
Timeframe: At week 24
| Intervention | Percentage of Participants (Number) | |
|---|---|---|
| ORR by week 24 - (BOR of CR or PR) (confirmed) | ORR by week 24 - (BOR of CR or PR) (unconfirmed) | |
| Ribociclib + Letrozole Cohort A | 22.8 | 24.8 |
| Ribociclib + Letrozole Cohort B1 | 23.1 | 30.8 |
| Ribociclib + Letrozole Cohort B2 | 11.7 | 16.2 |
Overall survival (OS) defined as the time from date of start of treatment to date of death due to any cause. (NCT03096847)
Timeframe: Up to approximatley 38 months
| Intervention | Participants (Number) | |
|---|---|---|
| No. of censored (no death), n | No. of events (deaths due to any cause), n | |
| Ribociclib + Letrozole Cohort A | 240 | 67 |
| Ribociclib + Letrozole Cohort B1 | 17 | 9 |
| Ribociclib + Letrozole Cohort B2 | 94 | 60 |
"To evaluate health related quality of life (QoL) via EORTC BR-23. The scoring approach for the QLQ-BR23 is identical in principle to that for the function and symptom scales / single items of the QLQ-C30, i.e., all scores finally range from 0 to 100, where a higher score represents a higher response level, e.g., a higher (better) level of functioning, (applies to the first 4 items, items 1 to 4) but a higher (worse) level of symptoms (applies to the last 4 items, items 5 to 8)." (NCT03096847)
Timeframe: Baseline and Week 24 (Cycle 7)
| Intervention | Scores on a scale (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| EORTC QLQ-BR23 BODY IMAGE during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 SEXUAL FUNCTIONING during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 SEXUAL ENJOYMENT during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 FUTURE PERSPECTIVE during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 SYSTEMATIC THERAPY during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 BREAST SYMPTOMS during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 ARM SYMPTOMS during the study - change from baseline at cycle 7 | EORTC QLQ-BR23 HAIR LOSS during the study - change from baseline at cycle 7 | |
| Ribociclib + Letrozole Cohort A | -1.5 | -1.1 | -1.9 | -20 | -9.4 | 3.3 | 4.1 | -22 |
| Ribociclib + Letrozole Cohort B | 0.2 | 0.7 | 5.0 | -14 | -7.1 | 2.2 | -2.0 | -15 |
| Ribociclib + Letrozole Cohort B1 | -0.6 | 0.0 | -17 | -24 | -13 | 8.3 | -1.5 | -17 |
| Ribociclib + Letrozole Cohort B2 | 0.4 | 0.8 | 7.4 | -12 | -6.0 | 0.9 | -2.1 | -14 |
PFS based on radiologic assessment by investigator using RECIST 1.1 criteria (NCT03096847)
Timeframe: At week 24 , week 48 and week 72
| Intervention | Percentage of Participants (Number) | ||
|---|---|---|---|
| Kaplan-Meier estimates (%, 95% CI) - Week 24 | Kaplan-Meier estimates (%, 95% CI) - Week 48 | Kaplan-Meier estimates (%, 95% CI) - week 72 | |
| Ribociclib + Letrozole Cohort A | 73.1 | 61.9 | 54.5 |
| Ribociclib + Letrozole Cohort B1 | 67.0 | 58.7 | 49.6 |
| Ribociclib + Letrozole Cohort B2 | 63.8 | 47.5 | 39.3 |
Overall survival (OS) defined as the time from date of start of treatment to date of death due to any cause. For the Kaplan-Meier estimates (%, 95% CI), the probability of survival at week 24, 48 and 72 is reported below. (NCT03096847)
Timeframe: At Week 24, Week 48 and Week 72
| Intervention | Percentage of Participants (Number) | ||
|---|---|---|---|
| Kaplan-Meier estimates (%, 95% CI) - Week 24 | Kaplan-Meier estimates (%, 95% CI) - Week 48 | Kaplan-Meier estimates (%, 95% CI) - Week 72 | |
| Ribociclib + Letrozole Cohort A | 98.6 | 93.3 | 89.7 |
| Ribociclib + Letrozole Cohort B1 | 100.0 | 87.5 | 87.5 |
| Ribociclib + Letrozole Cohort B2 | 93.9 | 86.1 | 81.0 |
Overall survival (OS) defined as the time from date of start of treatment to date of death due to any cause. (NCT03096847)
Timeframe: Up to approximatley 38 months
| Intervention | Months (Median) |
|---|---|
| Ribociclib + Letrozole Cohort A | NA |
| Ribociclib + Letrozole Cohort B1 | NA |
| Ribociclib + Letrozole Cohort B2 | NA |
PFS2 was defined as the time interval (in months) from the date of randomization to the date of first documentation of PD on the next systemic anti-cancer therapy according to investigator, or death due to any cause in the absence of documented PD on the next systemic anti-cancer therapy, whichever occurs first. PD was defined as at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. Analysis was performed by Kaplan-Meier method. (NCT04478266)
Timeframe: From randomization to date first documented disease progression on the next systemic anti-cancer therapy, or death due to any cause, or data cut-off date, whichever comes first (maximum duration: 81 weeks)
| Intervention | months (Median) |
|---|---|
| Letrozole + Palbociclib | NA |
| Amcenestrant + Palbociclib | NA |
PFS was defined as the time interval (in months) from the date of randomization to the date of first documented tumor progression as per Response Evaluation Criteria in Solid Tumors (RECIST 1.1) assessed by local radiologist or investigator, or death (due to any cause), whichever comes first. Progressive Disease (PD) as per RECIST 1.1: at least a 20 percent (%) increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. Analysis was performed by Kaplan-Meier method. (NCT04478266)
Timeframe: From randomization to the date of first documented tumor progression or death due to any cause or data cut-off date whichever comes first (maximum duration: 81 weeks)
| Intervention | months (Median) |
|---|---|
| Letrozole + Palbociclib | 16.6 |
| Amcenestrant + Palbociclib | 14.1 |
Objective response was defined as percentage of participants having a partial response (PR) or complete response (CR) according to the RECIST version 1.1 assessed by investigator. As per RECIST 1.1, CR was defined as disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to less than (<) 10 millimeters (mm). PR was defined as at least a 30%decrease in the sum of diameters of target lesions, taking as reference the Baseline sum diameters. (NCT04478266)
Timeframe: From randomization to the date of first documented tumor progression, death due to any cause or data cut-off date whichever comes first (maximum duration: 81 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Letrozole + Palbociclib | 42.3 |
| Amcenestrant + Palbociclib | 32.2 |
Clinical Benefit was defined as the percentage of participants having a confirmed CR, PR, or stable disease (SD) for at least 24 weeks determined by investigator as per RECIST 1.1, from date of randomization until disease progression, or death, or data cut-off date, or initiation of post treatment anti-cancer therapy, whichever occurs first. As per RECIST 1.1; CR was defined as disappearance of all target, non-target lesions & normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to <10 mm. PR: at least a 30% decrease in sum of diameters of target lesions, taking as reference Baseline sum diameters. SD: neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference smallest sum diameters. PD: at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. (NCT04478266)
Timeframe: From randomization until disease progression, or death, or data cut-off date, whichever comes first (maximum duration: 81 weeks)
| Intervention | percentage of participants (Number) |
|---|---|
| Letrozole + Palbociclib | 82.4 |
| Amcenestrant + Palbociclib | 76.0 |
OS was defined as the interval (in months) from the date of randomization to the date of documented death (due to any cause). In the absence of observation of death, survival time was censored to last date the participant was known to be alive or at the cut-off date, whichever comes first. Analysis was performed by Kaplan-Meier method. (NCT04478266)
Timeframe: From randomization to the death due to any cause or data cut-off date, whichever comes first (maximum duration: 81 weeks)
| Intervention | months (Median) |
|---|---|
| Letrozole + Palbociclib | NA |
| Amcenestrant + Palbociclib | NA |
DOR was defined as time (in months) from first documented evidence of CR or PR until disease progression determined by investigator as per RECIST 1.1, or start of any anti-cancer therapy, or death from any cause, whichever occurs first. For participants with ongoing response at the time of the analysis, DOR was censored at the date of the last valid disease assessment not showing documented progression performed before the initiation of a new anticancer treatment (if any). As per RECIST 1.1, CR was defined as disappearance of all target and non-target lesions and normalization of tumor marker level. Any pathological lymph nodes (whether target or non-target) must have reduction in short axis to <10 mm. PR: at least a 30% decrease in the sum of diameters of target lesions, taking as reference the Baseline sum diameters. PD: at least 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. Analysis was performed by Kaplan-Meier method. (NCT04478266)
Timeframe: From the date of first response of CR or PR until disease progression or death, or start of any anti-cancer therapy or data cut-off date, whichever comes first (maximum duration: 81 weeks)
| Intervention | months (Median) |
|---|---|
| Letrozole + Palbociclib | 14.0 |
| Amcenestrant + Palbociclib | NA |
EQ-5D-5L is a standardized measure of health status, provides a simple, generic measure of health for clinical and economic appraisal, and consists of 2 sections: the EQ-5D-5L health state utility index (descriptive system) and the EQ-5D-5L VAS. The Visual Analogue Scale is designed to rate the participant's current health state on a scale from 0 to 100, where 0 represents the worst imaginable health state and 100 represents the best imaginable health state. LS mean and SE are derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from Baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 21]) for VAS was reported in this outcome measure. (NCT04478266)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 21 [i.e., 81 weeks])
| Intervention | score on a scale (Least Squares Mean) |
|---|---|
| Letrozole + Palbociclib | 3.2 |
| Amcenestrant + Palbociclib | 3.8 |
Percentage of participants who were disease progression-free at Month 12 after randomization were reported in this outcome measure. PFS was defined as the time interval (in months) from the date of randomization to the date of first documented tumor progression as per RECIST 1.1 assessed by local radiologist or investigator, or death (due to any cause), whichever comes first. PD as per RECIST 1.1: at least a 20% increase in sum of diameters of target lesions, unequivocal progression of existing non-target lesions. The PFS rate at Month 12 was estimated using the Kaplan-Meier method and provided an estimation of the percentage of participants who were disease progression-free at Month 12 after randomization. (NCT04478266)
Timeframe: Month 12
| Intervention | percentage of participants (Number) |
|---|---|
| Letrozole + Palbociclib | 68.2 |
| Amcenestrant + Palbociclib | 65.5 |
QLQ-BR23: disease-specific Health-related QOL assesses breast cancer impact & side effects of treatment. EORTCQLQ- BR23 contains 23 items: multi-item scales & single-item measures. 4 functional scales (body image, sexual functioning, sexual enjoyment, future perspective) & 4 scales related to symptoms of disease or treatment (arm symptoms, breast symptoms, systemic therapy side effects, & upset by hair loss). All items scored 1 (not at all) to 4 (very much). Scores of all scales transformed from raw scores to linear scales ranging 0-100. Higher score for functional scales=better outcome; higher score for symptoms scales=higher symptom burden. LS mean & SE were derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value & stratifications factors as fixed effect. Average of LS mean change from Baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 21]) for each domain was reported. (NCT04478266)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 21 [i.e., 81 weeks])
| Intervention | score on a scale (Least Squares Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Body image | Sexual functioning | Sexual enjoyment | Future perspective | Systemic therapy side effects | Breast symptoms | Arm symptoms | Upset by hair loss | |
| Amcenestrant + Palbociclib | 1.1 | -1.5 | -8.7 | 10.8 | 3.7 | -7.0 | -1.8 | -0.2 |
| Letrozole + Palbociclib | 1.3 | -1.4 | -10.4 | 11.6 | 4.9 | -7.6 | -1.9 | -2.7 |
Palbociclib plasma concentrations at specified time points were reported. (NCT04478266)
Timeframe: Cycle 1 Day 1: 3 hr post-dose, Cycle 1 Day 15: pre-dose, Cycle 2 Day 1: pre-dose, 3 hr post-dose, Cycle 2 Day 15: pre-dose, Cycle 3 Day 1: pre-dose, Cycle 4 Day 1: pre-dose, Cycle 7 Day 1: pre-dose, Cycle 10 Day 1: pre-dose
| Intervention | nanograms per milliliter (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cycle 1 Day 1: 3 hr post-dose | Cycle 1 Day 15: pre-dose | Cycle 2 Day 1: pre-dose | Cycle 2 Day 1: 3 hr post-dose | Cycle 2 Day 15: pre-dose | Cycle 3 Day 1: pre-dose | Cycle 4 Day 1: pre-dose | Cycle 7 Day 1: pre-dose | Cycle 10 Day 1: pre-dose | |
| Amcenestrant + Palbociclib | 37.780 | 45.903 | 2.159 | 27.144 | 42.882 | 1.615 | 1.390 | 1.461 | 1.489 |
| Letrozole + Palbociclib | 36.265 | 82.541 | 3.409 | 30.234 | 72.176 | 4.301 | 4.767 | 2.716 | 3.793 |
Amcenestrant plasma concentrations at specified time points were reported. Data for this outcome measure was not planned to be collected and analyzed for Letrozole+Palbociclib arm as pre-specified in protocol. (NCT04478266)
Timeframe: Cycle 1 Day 1: 3 hours (hr) post-dose, Cycle 1 Day 15: pre-dose, Cycle 2 Day 1: pre-dose, 3 hr post-dose, Cycle 2 Day 15: pre-dose, Cycle 3 Day 1: pre-dose, Cycle 4 Day 1: pre-dose, Cycle 7 Day 1: pre-dose, Cycle 10 Day 1: pre-dose
| Intervention | nanograms per milliliter (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Cycle 1 Day 1: 3 hr post-dose | Cycle 1 Day 15: pre-dose | Cycle 2 Day 1: pre-dose | Cycle 2 Day 1: 3 hr post-dose | Cycle 2 Day 15: pre-dose | Cycle 3 Day 1: pre-dose | Cycle 4 Day 1: pre-dose | Cycle 7 Day 1: pre-dose | Cycle 10 Day 1: pre-dose | |
| Amcenestrant + Palbociclib | 2890.0 | 399.5 | 387.5 | 2729.3 | 361.3 | 303.4 | 349.3 | 337.5 | 310.9 |
Liver Function parameters assessed were aspartate aminotransferase increased, alanine aminotransferase increased, alkaline phosphatase increased, total bilirubin increased, gamma-glutamyl transferase increased. Parameters were assessed as per the NCI-CTCAE v 5.0, where Grade 1 = Mild; Grade 2 = Moderate; Grade 3 = Severe; Grade 4 = Potentially Life Threatening. Grade refers to the severity of the AEs. Treatment period was defined as the time from the first dose of study treatments up to 30 days after last dose of study treatment. Participants with Grade 3 and 4 liver function abnormalities were reported in this outcome measure. (NCT04478266)
Timeframe: From first dose of study treatment up to 30 days after last dose of study treatment (maximum duration: 112 weeks)
| Intervention | Participants (Count of Participants) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Aspartate aminotransferase increased: Grade 3 | Aspartate aminotransferase increased: Grade 4 | Alanine aminotransferase increased: Grade 3 | Alanine aminotransferase increased: Grade 4 | Alkaline phosphatase increased: Grade 3 | Alkaline phosphatase increased: Grade 4 | Total bilirubin increased: Grade 3 | Total bilirubin increased: Grade 4 | Gamma-GT increased: Grade 3 | Gamma-GT increased: Grade 4 | |
| Amcenestrant + Palbociclib | 23 | 1 | 32 | 3 | 1 | 0 | 5 | 0 | 20 | 1 |
| Letrozole + Palbociclib | 9 | 0 | 12 | 1 | 3 | 0 | 3 | 0 | 9 | 0 |
Hematological parameters assessed were anemia, lymphocyte count decreased, neutrophil count decreased, white blood cell decreased, platelet count decreased. Parameters were assessed as per the National Cancer Institute Common Terminology Criteria for Adverse Experience version 5.0 (NCI-CTCAE v 5.0), where Grade 1 = Mild; Grade 2 = Moderate; Grade 3 = Severe; Grade 4 = Potentially Life Threatening. Grade refers to the severity of the AEs. Treatment period was defined as the time from the first dose of study treatments up to 30 days after last dose of study treatment. (NCT04478266)
Timeframe: From first dose of study treatment up to 30 days after last dose of study treatment (maximum duration: 112 weeks)
| Intervention | Participants (Count of Participants) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Anemia: Grade 1 | Anemia: Grade 2 | Anemia: Grade 3 | Anemia: Grade 4 | Lymphocyte count decreased: Grade 1 | Lymphocyte count decreased: Grade 2 | Lymphocyte count decreased: Grade 3 | Lymphocyte count decreased: Grade 4 | Neutrophil count decreased: Grade 1 | Neutrophil count decreased: Grade 2 | Neutrophil count decreased: Grade 3 | Neutrophil count decreased: Grade 4 | White blood cell decreased: Grade 1 | White blood cell decreased: Grade 2 | White blood cell decreased: Grade 3 | White blood cell decreased: Grade 4 | Platelet count decreased: Grade 1 | Platelet count decreased: Grade 2 | Platelet count decreased: Grade 3 | Platelet count decreased: Grade 4 | |
| Amcenestrant + Palbociclib | 302 | 78 | 17 | 0 | 101 | 124 | 48 | 22 | 45 | 217 | 199 | 21 | 146 | 267 | 95 | 3 | 220 | 12 | 8 | 10 |
| Letrozole + Palbociclib | 309 | 108 | 22 | 0 | 98 | 138 | 46 | 23 | 22 | 150 | 277 | 70 | 81 | 279 | 163 | 7 | 285 | 30 | 18 | 8 |
Time to chemotherapy was defined as the time interval (in months) from the date of randomization to the start date of the first chemotherapy after disease progression. (NCT04478266)
Timeframe: From randomization to the start date of the first chemotherapy (maximum duration: 81 weeks)
| Intervention | months (Median) |
|---|---|
| Letrozole + Palbociclib | NA |
| Amcenestrant + Palbociclib | NA |
EORTC-QLQ-C30: cancer-specific instrument with 30 questions for evaluation of new chemotherapy & assessment of participant reported outcome. These include 5 functional scales, 9 symptom scales, & Global Health Status/quality of life scale (GHS/QoL). All 14 items/domains were scored on scale of 1 (not at all) to 4 (very much) & GHS/QoL, scored on scale of 1 (very poor) to 7 (excellent). All scales are transformed from raw scores to linear scales ranging 0 to 100. Higher score for functional & GHS/QoL=higher level of functioning, & higher score for symptoms scales=higher symptom burden. Least Square (LS) mean and Standard Error (SE) were derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from Baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 21]) for each domain was reported in this outcome measure. (NCT04478266)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 21 [i.e., 81 weeks])
| Intervention | score on a scale (Least Squares Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| GHS/QoL | Physical functioning | Role functioning | Emotional functioning | Cognitive functioning | Social functioning | Fatigue | Nausea and vomiting | Pain | Dyspnea | Insomnia | Appetite loss | Constipation | Diarrhea | Financial difficulties | |
| Amcenestrant + Palbociclib | 3.1 | 2.6 | 2.0 | 4.1 | -1.2 | 4.4 | -2.0 | -0.6 | -6.8 | -0.7 | -3.9 | -2.7 | 0.0 | 0.4 | -4.0 |
| Letrozole + Palbociclib | 2.8 | 2.3 | 1.8 | 4.2 | -0.8 | 2.2 | -1.6 | -1.3 | -5.8 | -1.1 | -2.9 | -3.0 | 0.1 | -0.4 | -5.1 |
EORTC QLQ-BR45: comprised of all 23 items from the QLQ-BR23 plus an additional 22 items assessing endocrine therapy symptoms (10 items), endocrine sexual symptoms (4 items), breast satisfaction (2 items), and skin mucosis symptoms (6 items). All items scored 1 (not at all) to 4 (very much). Scores of all scales transformed from raw scores to linear scales ranging 0 to 100. Higher score for functional scales = better outcome; higher score for symptoms scales = higher symptom burden. LS mean and SE are derived from Mixed Model Repeated Measures (MMRM) model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from Baseline values of overall treatment (i.e., each cycle [Cycle 1 up to Cycle 21]) for each domain (endocrine therapy symptoms, endocrine sexual symptoms, breast satisfaction and skin mucosis symptoms) was reported. (NCT04478266)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 21 [i.e., 81 weeks])
| Intervention | score on a scale (Least Squares Mean) | |||
|---|---|---|---|---|
| Breast Satisfaction | Endocrine Sexual Symptoms | Endocrine Therapy Symptoms | Skin Mucosis Symptoms | |
| Amcenestrant + Palbociclib | 1.0 | 2.3 | 1.2 | 2.5 |
| Letrozole + Palbociclib | -1.7 | 4.8 | 1.5 | 3.5 |
EQ-5D-5L: consists of 2 sections: EQ-5D-5L health state utility index (descriptive system) & VAS. The EQ-5D descriptive system consists of 5 dimensions: mobility, self-care, usual activities, pain/discomfort & anxiety/depression. Each dimension has 5 levels: no problems, slight problems, moderate problems, severe problems, & extreme problems. Response options are measured with 5-point Likert scale (for 5L version). The EQ-5D-5L responses are converted into single index utility score between 0 to 1, where higher score indicates better health state & lower score indicate worse health state. LS mean and SE were derived from MMRM model with change from Baseline values as response variable, treatment, time, treatment-by-time interaction, Baseline value and stratifications factors as fixed effect. Average of LS mean change from Baseline values overall treatment (i.e., each cycle [Cycle 1 up to Cycle 21]) for health utility index value score was reported in this outcome measure. (NCT04478266)
Timeframe: Baseline, overall treatment duration (Cycle 1 up to Cycle 21 [i.e., 81 weeks])
| Intervention | score on a scale (Least Squares Mean) |
|---|---|
| Letrozole + Palbociclib | 0.0 |
| Amcenestrant + Palbociclib | 0.0 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4. | 3.55 | 2 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid | human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule |
| acetic acid Acetic Acid: Product of the oxidation of ethanol and of the destructive distillation of wood. It is used locally, occasionally internally, as a counterirritant and also as a reagent. (Stedman, 26th ed). acetic acid : A simple monocarboxylic acid containing two carbons. | 2.51 | 2 | 0 | monocarboxylic acid | antimicrobial food preservative; Daphnia magna metabolite; food acidity regulator; protic solvent |
| betaine glycine betaine : The amino acid betaine derived from glycine. | 4.2 | 2 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| salicylic acid Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL). | 2.17 | 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 |
| bupropion Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. | 3.23 | 1 | 0 | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| aminocaproic acid Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator. | 3.23 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| lactic acid Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group. | 2.61 | 2 | 0 | 2-hydroxy monocarboxylic acid | algal metabolite; Daphnia magna metabolite |
| glycine [no description available] | 2 | 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 |
| 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 | |
| niacinamide nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group. | 2.06 | 1 | 0 | pyridine alkaloid; pyridinecarboxamide; vitamin B3 | anti-inflammatory agent; antioxidant; cofactor; EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor; EC 3.5.1.98 (histone deacetylase) inhibitor; Escherichia coli metabolite; geroprotector; human urinary metabolite; metabolite; mouse metabolite; neuroprotective agent; Saccharomyces cerevisiae metabolite; Sir2 inhibitor |
| niacin Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group. | 3.23 | 1 | 0 | pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3 | antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent |
| 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. | 1.97 | 1 | 0 | glycol; propane-1,2-diols | allergen; human xenobiotic metabolite; mouse metabolite; protic solvent |
| propionic acid propionic acid : A short-chain saturated fatty acid comprising ethane attached to the carbon of a carboxy group. | 1.97 | 1 | 0 | saturated fatty acid; short-chain fatty acid | antifungal drug |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 3.23 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| pyridoxine 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms). | 3.23 | 1 | 0 | hydroxymethylpyridine; methylpyridines; monohydroxypyridine; vitamin B6 | cofactor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thiamine thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively. | 3.23 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thymine [no description available] | 3.13 | 1 | 0 | pyrimidine nucleobase; pyrimidone | Escherichia coli metabolite; human metabolite; mouse metabolite |
| phenytoin [no description available] | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| acebutolol Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. | 3.23 | 1 | 0 | aromatic amide; ethanolamines; ether; monocarboxylic acid amide; propanolamine; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympathomimetic agent |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 3.23 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohydroxamic acid acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group. | 3.23 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| alaproclate alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer | 3.23 | 1 | 0 | alpha-amino acid ester | |
| albendazole [no description available] | 3.23 | 1 | 0 | aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester | anthelminthic drug; microtubule-destabilising agent; tubulin modulator |
| albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). | 3.23 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alendronate alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| alfuzosin alfuzosin: structure given in first source | 3.23 | 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. | 3.23 | 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. | 3.23 | 1 | 0 | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| altretamine Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine. | 3.23 | 1 | 0 | triamino-1,3,5-triazine | |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ambenonium ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens. | 3.23 | 1 | 0 | quaternary ammonium ion | EC 3.1.1.8 (cholinesterase) inhibitor |
| diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 3.23 | 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. | 3.23 | 1 | 0 | diamine; organic thiophosphate | antioxidant; prodrug; radiation protective agent |
| aminoglutethimide Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position. | 11.71 | 8 | 3 | dicarboximide; piperidones; substituted aniline | adrenergic agent; anticonvulsant; antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| p-aminohippuric acid p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow. | 3.23 | 1 | 0 | N-acylglycine | Daphnia magna metabolite |
| theophylline [no description available] | 3.23 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| amiodarone Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. | 3.23 | 1 | 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. | 4.13 | 2 | 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. | 3.23 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amoxapine Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position. | 3.23 | 1 | 0 | dibenzooxazepine | adrenergic uptake inhibitor; antidepressant; dopaminergic antagonist; geroprotector; serotonin uptake inhibitor |
| anastrozole [no description available] | 15.24 | 49 | 23 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| 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. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | ethanolamines; monocarboxylic acid amide; propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic |
| azathioprine Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS. | 3.59 | 2 | 0 | aryl sulfide; C-nitro compound; imidazoles; thiopurine | antimetabolite; antineoplastic agent; carcinogenic agent; DNA synthesis inhibitor; hepatotoxic agent; immunosuppressive agent; prodrug |
| baclofen [no description available] | 3.23 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| bendazac bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts. | 3.23 | 1 | 0 | indazoles; monocarboxylic acid | non-steroidal anti-inflammatory drug; radical scavenger |
| bendroflumethiazide Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group. | 3.23 | 1 | 0 | benzothiadiazine; sulfonamide | antihypertensive agent; diuretic |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| betaxolol [no description available] | 3.23 | 1 | 0 | propanolamine | antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bethanechol Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | 3.23 | 1 | 0 | carbamate ester; quaternary ammonium ion | muscarinic agonist |
| bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. | 17.48 | 123 | 54 | (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. | 3.23 | 1 | 0 | piperidines; tertiary alcohol; tertiary amino compound | antidote to sarin poisoning; antidyskinesia agent; antiparkinson drug; muscarinic antagonist; parasympatholytic |
| bisacodyl Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | 3.23 | 1 | 0 | diarylmethane | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 3.23 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bumetanide [no description available] | 3.23 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 3.23 | 1 | 0 | azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines | anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist |
| busulfan [no description available] | 3.23 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| secbutabarbital secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital | 3.23 | 1 | 0 | barbiturates | |
| caffeine [no description available] | 3.23 | 1 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. | 3.23 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 3.23 | 1 | 0 | dibenzoazepine; ureas | analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic |
| carbinoxamine carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist |
| carisoprodol Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. | 3.23 | 1 | 0 | carbamate ester | muscle relaxant |
| carvedilol [no description available] | 3.23 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 3.23 | 1 | 0 | organofluorine compound; pyrazoles; sulfonamide; toluenes | cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively. | 3.23 | 1 | 0 | ether; monocarboxylic acid; monochlorobenzenes; piperazines | anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 3.23 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlorcyclizine chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness | 3.23 | 1 | 0 | diarylmethane | |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 3.23 | 1 | 0 | benzodiazepine | |
| chlormezanone Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions. | 3.23 | 1 | 0 | 1,3-thiazine; lactam; monochlorobenzenes; sulfone | antipsychotic agent; anxiolytic drug; muscle relaxant |
| chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chlorothiazide Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension. | 3.23 | 1 | 0 | benzothiadiazine | antihypertensive agent; diuretic |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 3.23 | 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. | 3.23 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| chlorpropamide Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 3.23 | 1 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cilostazol [no description available] | 3.23 | 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. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion | antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 3.23 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 3.23 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 3.23 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor modulator |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 3.23 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| clonazepam Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. | 3.23 | 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. | 9.34 | 3 | 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. | 3.23 | 1 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 3.23 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cyclobenzaprine cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant; muscle relaxant; tranquilizing drug |
| cyclofenil Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE. | 3.23 | 1 | 0 | organic molecular entity | |
| cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| dapsone [no description available] | 3.59 | 2 | 0 | substituted aniline; sulfone | anti-inflammatory drug; antiinfective agent; antimalarial; leprostatic drug |
| deferoxamine Deferoxamine: Natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form.. desferrioxamine B : An acyclic desferrioxamine that is butanedioic acid in which one of the carboxy groups undergoes formal condensation with the primary amino group of N-(5-aminopentyl)-N-hydroxyacetamide and the second carboxy group undergoes formal condensation with the hydroxyamino group of N(1)-(5-aminopentyl)-N(1)-hydroxy-N(4)-[5-(hydroxyamino)pentyl]butanediamide. It is a siderophore native to Streptomyces pilosus biosynthesised by the DesABCD enzyme cluster as a high affinity Fe(III) chelator. | 3.23 | 1 | 0 | acyclic desferrioxamine | bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 3.23 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 3.23 | 1 | 0 | primary amine | |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| diazoxide Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfone | antihypertensive agent; beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; diuretic; K-ATP channel agonist; sodium channel blocker; sympathomimetic agent; vasodilator agent |
| diclofenac Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; dichlorobenzene; monocarboxylic acid; secondary amino compound | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| dichlorphenamide Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma. | 3.23 | 1 | 0 | dichlorobenzene; sulfonamide | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor; ophthalmology drug |
| dicyclomine Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome. | 3.23 | 1 | 0 | carboxylic ester; tertiary amine | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| pentetic acid Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. | 3.23 | 1 | 0 | pentacarboxylic acid | copper chelator |
| diflunisal Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position. | 3.23 | 1 | 0 | monohydroxybenzoic acid; organofluorine compound | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| dimercaprol Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury. | 3.23 | 1 | 0 | dithiol; primary alcohol | chelator |
| diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. | 3.23 | 1 | 0 | ether; tertiary amino compound | anti-allergic agent; antidyskinesia agent; antiemetic; antiparkinson drug; antipruritic drug; antitussive; H1-receptor antagonist; local anaesthetic; muscarinic antagonist; oneirogen; sedative |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 3.23 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug. | 3.23 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 3.23 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 3.56 | 2 | 0 | branched-chain fatty acid; branched-chain saturated fatty acid | anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent |
| donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. | 3.23 | 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. | 3.23 | 1 | 0 | morpholines; pyrrolidin-2-ones | central nervous system stimulant |
| doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| doxylamine Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM. | 3.23 | 1 | 0 | pyridines; tertiary amine | anti-allergic agent; antiemetic; antitussive; cholinergic antagonist; H1-receptor antagonist; histamine antagonist; sedative |
| droperidol Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; organofluorine compound | anaesthesia adjuvant; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| dyphylline Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs. | 3.23 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| edrophonium Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals. | 3.23 | 1 | 0 | phenols; quaternary ammonium ion | antidote; diagnostic agent; EC 3.1.1.8 (cholinesterase) inhibitor |
| estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. | 3.23 | 1 | 0 | triazoles; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA modulator |
| ethacrynic acid Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethosuximide Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures. | 3.23 | 1 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| ethotoin ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces. | 3.54 | 2 | 0 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| etodolac Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active. | 3.23 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 3.23 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| felbamate Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy. | 3.23 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 3.23 | 1 | 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 | 3.23 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fenoldopam Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. | 3.23 | 1 | 0 | benzazepine | alpha-adrenergic agonist; antihypertensive agent; dopamine agonist; dopaminergic antagonist; vasodilator agent |
| fenoprofen Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fipexide fipexide: regulates dopaminergic systems at macromolecular level | 3.23 | 1 | 0 | benzodioxoles | |
| flavoxate Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol. | 3.23 | 1 | 0 | carboxylic ester; flavones; piperidines; tertiary amino compound | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| flecainide Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines | anti-arrhythmia drug |
| fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug | environmental contaminant; P450 inhibitor; xenobiotic |
| flucytosine Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections. | 3.23 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 3.23 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 3.23 | 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. | 14.37 | 51 | 23 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flurazepam Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monofluorobenzenes; organochlorine compound; tertiary amino compound | anticonvulsant; anxiolytic drug; GABAA receptor agonist; sedative |
| flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. | 4.06 | 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. | 20.17 | 214 | 123 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
| fomepizole Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4. | 3.23 | 1 | 0 | pyrazoles | antidote; EC 1.1.1.1 (alcohol dehydrogenase) inhibitor; protective agent |
| foscarnet Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 3.23 | 1 | 0 | carboxylic acid; one-carbon compound; phosphonic acids | antiviral drug; geroprotector; HIV-1 reverse transcriptase inhibitor; sodium-dependent Pi-transporter inhibitor |
| furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure. | 3.23 | 1 | 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. | 4.37 | 3 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 3.23 | 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. | 3.23 | 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 | 3.23 | 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. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester [no description available] | 3.23 | 1 | 0 | benzenes | |
| granisetron [no description available] | 3.23 | 1 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 3.23 | 1 | 0 | methoxybenzenes | |
| guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid. | 3.23 | 1 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 3.23 | 1 | 0 | acetamides | |
| guanidine Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines. | 3.23 | 1 | 0 | carboxamidine; guanidines; one-carbon compound | |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 3.23 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| hydralazine Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent. | 3.23 | 1 | 0 | azaarene; hydrazines; ortho-fused heteroarene; phthalazines | antihypertensive agent; vasodilator agent |
| hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure. | 3.53 | 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. | 3.23 | 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. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 3.23 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| hydroxyzine Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively. | 3.23 | 1 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; radical scavenger; xenobiotic |
| phenelzine Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. | 3.23 | 1 | 0 | primary amine | |
| lidocaine Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. | 3.23 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 3.23 | 1 | 0 | ifosfamides | alkylating agent; antineoplastic agent; environmental contaminant; immunosuppressive agent; xenobiotic |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 3.23 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| amrinone Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. | 3.23 | 1 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine. | 3.23 | 1 | 0 | indoles; organochlorine compound; sulfonamide | antihypertensive agent; diuretic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 3.23 | 1 | 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 |
| ioversol [no description available] | 3.23 | 1 | 0 | amidobenzoic acid | |
| iproniazid [no description available] | 3.23 | 1 | 0 | carbohydrazide; pyridines | |
| avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. | 3.23 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| 1-methyl-3-isobutylxanthine 1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES. 3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively. | 1.96 | 1 | 0 | 3-isobutyl-1-methylxanthine | |
| isocarboxazid Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) | 3.23 | 1 | 0 | benzenes | |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 3.23 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders. | 3.51 | 2 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| isoxsuprine Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | 3.23 | 1 | 0 | alkylbenzene | |
| isradipine Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. | 3.23 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 3.23 | 1 | 0 | piperazines | |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 3.23 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| 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. | 7.21 | 6 | 2 | dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine | |
| ketoprofen Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2. | 3.23 | 1 | 0 | benzophenones; oxo monocarboxylic acid | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| ketorolac Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively. | 3.23 | 1 | 0 | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| labetalol Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5. | 3.23 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; isoxazoles; monocarboxylic acid amide | antineoplastic agent; antiparasitic agent; EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; hepatotoxic agent; immunosuppressive agent; non-steroidal anti-inflammatory drug; prodrug; pyrimidine synthesis inhibitor; tyrosine kinase inhibitor |
| letrozole [no description available] | 8.99 | 15 | 3 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lomefloxacin lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antimicrobial agent; antitubercular agent; photosensitizing agent |
| lomustine [no description available] | 3.23 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease. | 3.23 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 3.23 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| lorazepam Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | 3.23 | 1 | 0 | benzodiazepine | |
| losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | 3.23 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| loxapine Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. | 3.23 | 1 | 0 | dibenzooxazepine | antipsychotic agent; dopaminergic antagonist |
| maprotiline Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. | 3.23 | 1 | 0 | anthracenes | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 3.23 | 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. | 3.23 | 1 | 0 | primary aliphatic amine | |
| mechlorethamine nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR. | 3.23 | 1 | 0 | nitrogen mustard; organochlorine compound | alkylating agent |
| meclizine Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. | 3.23 | 1 | 0 | diarylmethane | |
| meclofenamic acid Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; organochlorine compound; secondary amino compound | analgesic; anticonvulsant; antineoplastic agent; antipyretic; antirheumatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 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 |
| memantine [no description available] | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist |
| mepenzolate mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure | 3.23 | 1 | 0 | diarylmethane | |
| meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | 3.23 | 1 | 0 | ethyl ester; piperidinecarboxylate ester; tertiary amino compound | antispasmodic drug; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| mephenytoin Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| mepivacaine Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic. | 3.23 | 1 | 0 | piperidinecarboxamide | drug allergen; local anaesthetic |
| meprobamate Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) | 3.23 | 1 | 0 | organic molecular entity | |
| mesalamine Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| mesoridazine Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group. | 3.23 | 1 | 0 | phenothiazines; sulfoxide; tertiary amino compound | dopaminergic antagonist; first generation antipsychotic |
| metaproterenol Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself. | 3.23 | 1 | 0 | aralkylamino compound; phenylethanolamines; resorcinols; secondary alcohol; secondary amino compound | |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 5.81 | 3 | 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. | 3.23 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 3.23 | 1 | 0 | sulfonamide; thiadiazoles | |
| methocarbamol Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester. | 3.23 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| methoxsalen Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis. | 3.23 | 1 | 0 | aromatic ether; psoralens | antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite |
| methyclothiazide Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) | 3.23 | 1 | 0 | benzothiadiazine | |
| methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group. | 3.23 | 1 | 0 | beta-amino acid ester; methyl ester; piperidines | |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 3.23 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metolazone Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics. | 3.23 | 1 | 0 | organochlorine compound; quinazolines; sulfonamide | antihypertensive agent; diuretic; ion transport inhibitor |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 3.23 | 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. | 3.23 | 1 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| metyrapone Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency. | 3.23 | 1 | 0 | aromatic ketone | antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor |
| mexiletine Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. | 3.23 | 1 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 3.23 | 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. | 3.23 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 3.23 | 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. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| mitotane Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression. | 3.23 | 1 | 0 | diarylmethane | |
| mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8. | 9.84 | 9 | 6 | dihydroxyanthraquinone | analgesic; antineoplastic agent |
| modafinil Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group. | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfoxide | |
| moxisylyte Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) | 3.23 | 1 | 0 | monoterpenoid | |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 3.23 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nadolol [no description available] | 3.23 | 1 | 0 | tetralins | |
| naftopidil [no description available] | 2.03 | 1 | 0 | piperazines | |
| nalidixic acid [no description available] | 3.23 | 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. | 1.98 | 1 | 0 | ||
| naratriptan naratriptan: structure given in first source | 3.23 | 1 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles | alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 3.23 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 3.23 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| nicardipine Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. | 3.23 | 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. | 3.23 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 7.27 | 10 | 2 | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 3.23 | 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. | 3.23 | 1 | 0 | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| nisoldipine Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris. | 3.23 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain. | 3.23 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | isoquinolines | dopamine uptake inhibitor |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 3.23 | 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. | 3.23 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. | 8.51 | 2 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | carbazoles | |
| orphenadrine Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol. | 3.23 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxaprozin Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-oxazoles; monocarboxylic acid | analgesic; non-steroidal anti-inflammatory drug |
| oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxybutynin oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder. | 3.23 | 1 | 0 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| aminosalicylic acid Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4. | 3.23 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pamidronate [no description available] | 5.21 | 3 | 1 | phosphonoacetic acid | |
| pantoprazole Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; organofluorine compound; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; environmental contaminant; xenobiotic |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 3.23 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pemoline Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity. | 3.23 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentamidine Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | 3.23 | 1 | 0 | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
| pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 3.23 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 3.23 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 3.23 | 1 | 0 | piperidines | cardiovascular drug |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 3.23 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 3.23 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 3.23 | 1 | 0 | aromatic amine | |
| phentermine Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity. | 3.23 | 1 | 0 | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| 4-phenylbutyric acid 4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation. | 3.23 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol. | 3.23 | 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. | 3.23 | 1 | 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 |
| polythiazide [no description available] | 3.23 | 1 | 0 | benzothiadiazine | |
| potassium chloride Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion. | 1.97 | 1 | 0 | inorganic chloride; inorganic potassium salt; potassium salt | fertilizer |
| duodote duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents | 3.23 | 1 | 0 | pyridinium ion | antidote to organophosphate poisoning; antidote to sarin poisoning; cholinergic drug; cholinesterase reactivator |
| praziquantel azinox: Russian drug | 3.23 | 1 | 0 | isoquinolines | |
| prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. | 4.04 | 2 | 0 | aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| primaquine Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia. | 3.23 | 1 | 0 | aminoquinoline; aromatic ether; N-substituted diamine | antimalarial |
| primidone Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures. | 3.23 | 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. | 3.23 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| procarbazine Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands. | 4.2 | 5 | 0 | benzamides; hydrazines | antineoplastic agent |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines | alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic |
| procyclidine Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3. | 3.23 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 3.23 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propafenone Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. | 3.23 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propantheline Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. | 3.23 | 1 | 0 | xanthenes | |
| propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. | 3.23 | 1 | 0 | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 3.56 | 2 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| protriptyline Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant |
| pyridostigmine [no description available] | 3.23 | 1 | 0 | pyridinium ion | |
| pyrimethamine Maloprim: contains above 2 cpds | 3.23 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| sch 16134 quazepam: structure given in first source | 3.23 | 1 | 0 | benzodiazepine | |
| quetiapine [no description available] | 3.23 | 1 | 0 | dibenzothiazepine; N-alkylpiperazine; N-arylpiperazine | adrenergic antagonist; dopaminergic antagonist; histamine antagonist; second generation antipsychotic; serotonergic antagonist |
| rabeprazole Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| raloxifene raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. | 3.23 | 1 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 3.23 | 1 | 0 | benzothiazoles | |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 3.23 | 1 | 0 | alkylamine | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 3.56 | 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 | 3.23 | 1 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| ropinirole [no description available] | 3.23 | 1 | 0 | indolones; tertiary amine | antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist |
| salicylsalicylic acid salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes. | 3.23 | 1 | 0 | benzoate ester; benzoic acids; phenols; salicylates | antineoplastic agent; antirheumatic drug; EC 3.5.2.6 (beta-lactamase) inhibitor; hypoglycemic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| secobarbital Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups. | 3.23 | 1 | 0 | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 3.23 | 1 | 0 | organochlorine compound; tertiary amino compound | anti-obesity agent; serotonin uptake inhibitor |
| sulfadiazine Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines. | 3.23 | 1 | 0 | pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; antiprotozoal drug; coccidiostat; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| risedronic acid Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION. | 3.23 | 1 | 0 | pyridines | |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 3.23 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 3.23 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 3.23 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| succinylcholine Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid. | 3.23 | 1 | 0 | quaternary ammonium ion; succinate ester | drug allergen; muscle relaxant; neuromuscular agent |
| sulfamethizole Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2. | 3.23 | 1 | 0 | sulfonamide antibiotic; sulfonamide; thiadiazoles | antiinfective agent; antimicrobial agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| 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. | 3.23 | 1 | 0 | ||
| sulfathiazole Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. | 3.23 | 1 | 0 | 1,3-thiazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| 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. | 3.77 | 2 | 1 | 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. | 3.23 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| 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. | 4.9 | 2 | 1 | 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 |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 3.23 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 3.23 | 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 | 4.04 | 2 | 0 | furans; piperazines; primary amino compound; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 3.23 | 1 | 0 | phenylethanolamines; resorcinols | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hypoglycemic agent; sympathomimetic agent; tocolytic agent |
| 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. | 7.79 | 4 | 3 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 3.23 | 1 | 0 | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| thioridazine Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position. | 3.23 | 1 | 0 | phenothiazines; piperidines | alpha-adrenergic antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| thiotepa Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed). | 3.23 | 1 | 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. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| tizanidine tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | 3.23 | 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. | 3.23 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; potassium channel blocker |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 3.23 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolmetin Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug. | 3.23 | 1 | 0 | aromatic ketone; monocarboxylic acid; pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| ultram 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively. | 3.23 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 3.66 | 2 | 0 | amino acid | |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 3.56 | 2 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 3.23 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| triazolam Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. | 3.23 | 1 | 0 | triazolobenzodiazepine | sedative |
| trifluoperazine [no description available] | 3.5 | 2 | 0 | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug |
| trihexyphenidyl Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic. | 3.23 | 1 | 0 | amine | |
| trimethadione Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent. | 3.23 | 1 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| trimethobenzamide trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans. | 3.23 | 1 | 0 | benzamides; tertiary amino compound | antiemetic |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 3.23 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| trimetrexate Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. | 3.23 | 1 | 0 | ||
| trimipramine Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant. | 3.23 | 1 | 0 | dibenzoazepine; tertiary amino compound | antidepressant; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 3.23 | 1 | 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 |
| tyramine [no description available] | 3.23 | 1 | 0 | monoamine molecular messenger; primary amino compound; tyramines | EC 3.1.1.8 (cholinesterase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter |
| delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 3.23 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 3.23 | 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. | 3.23 | 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. | 3.23 | 1 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position. | 3.23 | 1 | 0 | 1,2-benzoxazoles; sulfonamide | anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker |
| cortisone acetate Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders. | 3.23 | 1 | 0 | corticosteroid hormone | |
| mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae. | 5.41 | 4 | 1 | mitomycin | alkylating agent; antineoplastic agent |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 3.59 | 2 | 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. | 3.38 | 1 | 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. | 3.23 | 1 | 0 | alkaloid ester; methyl ester; yohimban alkaloid | adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic |
| phentolamine Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. | 3.23 | 1 | 0 | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| sorbitol D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol). | 3.23 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| thymidine [no description available] | 2.38 | 2 | 0 | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite; human metabolite; metabolite; mouse metabolite |
| 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. | 3.78 | 2 | 1 | 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. | 8.58 | 2 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. | 3.23 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| 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. | 6.78 | 5 | 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. | 4.91 | 2 | 1 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 3.23 | 1 | 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). | 3.35 | 1 | 0 | steroid | |
| cysteine [no description available] | 3.23 | 1 | 0 | cysteine zwitterion; cysteine; L-alpha-amino acid; proteinogenic amino acid; serine family amino acid | EC 4.3.1.3 (histidine ammonia-lyase) inhibitor; flour treatment agent; human metabolite |
| prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid. | 10.39 | 10 | 8 | 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. | 6.41 | 7 | 2 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| methylprednisolone acetate Methylprednisolone Acetate: Methylprednisolone derivative that is used as an anti-inflammatory agent for the treatment of ALLERGY and ALLERGIC RHINITIS; ASTHMA; and BURSITIS; and for the treatment of ADRENAL INSUFFICIENCY.. methylprednisolone acetate : An acetate ester resulting from the formal condensation of the 21-hydroxy function of 6alpha-methylprednisolone compound with acetic acid. | 1.98 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid; acetate ester; glucocorticoid; steroid ester; tertiary alpha-hydroxy ketone | anti-inflammatory drug |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| androsterone [no description available] | 4.4 | 1 | 1 | 17-oxo steroid; 3alpha-hydroxy steroid; androstanoid; C19-steroid | androgen; anticonvulsant; human blood serum metabolite; human metabolite; human urinary metabolite; mouse metabolite; pheromone |
| 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. | 1.97 | 1 | 0 | 17-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; androstanoid | androgen; human metabolite; mouse metabolite |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine. | 3.23 | 1 | 0 | pilocarpine | antiglaucoma drug |
| triiodothyronine Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. | 3.23 | 1 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 3.23 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4. | 3.23 | 1 | 0 | amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid | EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| vincristine [no description available] | 3.23 | 1 | 0 | acetate ester; formamides; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; drug; microtubule-destabilising agent; plant metabolite; tubulin modulator |
| physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. | 3.23 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration. | 9.64 | 3 | 2 | 17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound | xenoestrogen |
| 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. | 3.76 | 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. | 3.23 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| methyltestosterone Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position. | 4.05 | 2 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; enone | anabolic agent; androgen; antineoplastic agent |
| tetrabenazine 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. | 3.23 | 1 | 0 | benzoquinolizine; cyclic ketone; tertiary amino compound | |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 3.23 | 1 | 0 | kanamycins | bacterial metabolite |
| galactose galactopyranose : The pyranose form of galactose. | 2.15 | 1 | 0 | D-galactose; galactopyranose | Escherichia coli metabolite; mouse metabolite |
| edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive. | 3.23 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| tyrosine Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring. | 2 | 1 | 0 | amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; proteinogenic amino acid; tyrosine | EC 1.3.1.43 (arogenate dehydrogenase) inhibitor; fundamental metabolite; micronutrient; nutraceutical |
| cysteamine Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2. | 3.23 | 1 | 0 | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| acetylcholine chloride acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug. | 3.23 | 1 | 0 | quaternary ammonium salt | |
| mepazine mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position. | 3.23 | 1 | 0 | phenothiazines | |
| cloxacillin Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6. | 3.23 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| calcium acetate calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces. | 3.23 | 1 | 0 | calcium salt | chelator |
| androstenedione Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.. androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads. | 14.27 | 18 | 10 | 17-oxo steroid; 3-oxo-Delta(4) steroid; androstanoid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
| methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4. | 3.52 | 2 | 0 | aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid | antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 3.23 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| mebanazine mebanazine: RN given refers to parent cpd without isomeric designation; structure | 3.23 | 1 | 0 | benzenes | |
| oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta. | 3.23 | 1 | 0 | penicillin | antibacterial agent; antibacterial drug |
| 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. | 1.96 | 1 | 0 | antibiotic fungicide; cyclic ketone; dicarboximide; piperidine antibiotic; piperidones; secondary alcohol | anticoronaviral agent; bacterial metabolite; ferroptosis inhibitor; neuroprotective agent; protein synthesis inhibitor |
| 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. | 6.72 | 8 | 8 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound; tertiary alcohol | progestin; synthetic oral contraceptive |
| cycloserine Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis). | 3.23 | 1 | 0 | 4-amino-1,2-oxazolidin-3-one; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic; zwitterion | antiinfective agent; antimetabolite; antitubercular agent; metabolite; NMDA receptor agonist |
| benziodarone benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) | 3.23 | 1 | 0 | aromatic ketone | |
| 17-alpha-hydroxyprogesterone 17alpha-hydroxyprogesterone : A 17alpha-hydroxy steroid that is the 17alpha-hydroxy derivative of progesterone. | 2.38 | 2 | 0 | 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. | 3.23 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 3.23 | 1 | 0 | mannitol | allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent |
| cytarabine [no description available] | 6.14 | 3 | 1 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| medroxyprogesterone acetate [no description available] | 11.63 | 25 | 14 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester | adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive |
| arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group. | 8.85 | 3 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| ethyl chloride Ethyl Chloride: A gas that condenses under slight pressure. Because of its low boiling point ethyl chloride sprayed on skin produces an intense cold by evaporation. Cold blocks nerve conduction. Ethyl chloride has been used in surgery but is primarily used to relieve local pain in sports medicine.. chloroethane : The simplest and least toxic member of the class of chloroethanes, that is ethane in which a single hydrogen is substituted by a chlorine. A colourless gas at room temperature and pressure (boiling point 12degreeC), it is used as a mild topical anaesthetic to numb the skin prior to ear piercing, skin biopsies, etc., and is also used in the treatment of sports injuries. It was formerly used in the production of tetraethyllead. | 1.98 | 1 | 0 | chloroethanes | antipruritic drug; inhalation anaesthetic; local anaesthetic |
| 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. | 3.4 | 1 | 1 | monocarboxylic acid; organochlorine compound | carcinogenic agent; metabolite; mouse metabolite |
| perflutren Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines. | 3.23 | 1 | 0 | fluoroalkane; fluorocarbon | |
| fluoxymesterone Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
| methsuximide methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation | 3.23 | 1 | 0 | organic molecular entity | |
| tromethamine Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424) | 3.23 | 1 | 0 | primary amino compound; triol | buffer |
| isoprene isoprene: used in manufacture of ''synthetic'' rubber, butyl rubber; copolymer in production of elastomers; structure. isoprene : A hemiterpene with the formula CH2=C(CH3)CH=CH2; the monomer of natural rubber and a common structure motif to the isoprenoids, a large class of other naturally occurring compounds. | 2.04 | 1 | 0 | alkadiene; hemiterpene; volatile organic compound | plant metabolite |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 3.53 | 2 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| brompheniramine Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | organobromine compound; pyridines | anti-allergic agent; H1-receptor antagonist |
| penicillin v Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | |
| isosorbide dinitrate Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. | 3.23 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| pseudoephedrine Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group. | 3.23 | 1 | 0 | phenylethanolamines; secondary alcohol; secondary amino compound | anti-asthmatic drug; bronchodilator agent; central nervous system drug; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| diethylpropion Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity. | 3.23 | 1 | 0 | aromatic ketone; tertiary amine | appetite depressant |
| benzoyl peroxide Benzoyl Peroxide: A peroxide derivative that has been used topically for BURNS and as a dermatologic agent in the treatment of ACNE and POISON IVY DERMATITIS. It is used also as a bleach in the food industry. | 1.99 | 1 | 0 | carbonyl compound | |
| benzonatate benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant. | 3.23 | 1 | 0 | benzoate ester; secondary amino compound; substituted aniline | anaesthetic; antitussive |
| pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen. | 3.85 | 2 | 1 | pyrrole; secondary amine | |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 3.23 | 1 | 0 | ergoline alkaloid | |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 3.23 | 1 | 0 | quinolines | |
| pregnenolone [no description available] | 1.97 | 1 | 0 | 20-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; C21-steroid | human metabolite; mouse metabolite |
| 20-alpha-dihydroprogesterone 20-alpha-Dihydroprogesterone: A biologically active 20-alpha-reduced metabolite of PROGESTERONE. It is converted from progesterone to 20-alpha-hydroxypregn-4-en-3-one by the 20-ALPHA-HYDROXYSTEROID DEHYDROGENASE in the CORPUS LUTEUM and the PLACENTA. | 1.97 | 1 | 0 | 20-hydroxypregn-4-en-3-one | human metabolite; mouse metabolite |
| nafcillin Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| methohexital Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups. | 3.23 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| dydrogesterone [no description available] | 3.83 | 2 | 1 | 20-oxo steroid; 3-oxo-Delta(4) steroid | progestin |
| thiazoles [no description available] | 3.64 | 2 | 0 | 1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| ephedrine Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively. | 3.23 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| hydrazine diamine : Any polyamine that contains two amino groups. | 2 | 1 | 0 | azane; hydrazines | EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitor |
| chlormadinone acetate Chlormadinone Acetate: An orally active synthetic progestational hormone used often in combinations as an oral contraceptive (CONTRACEPTIVES, ORAL). | 6.84 | 8 | 1 | corticosteroid hormone | |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 3.23 | 1 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. | 3.23 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. | 3.23 | 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. | 3.23 | 1 | 0 | steroid ester | |
| cyproterone acetate [no description available] | 13.21 | 49 | 25 | 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. | 5.63 | 4 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid | human metabolite |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 3.23 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| 4-hydroxybutyric acid 4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group. | 3.23 | 1 | 0 | 4-hydroxy monocarboxylic acid; hydroxybutyric acid | general anaesthetic; GHB receptor agonist; neurotoxin; sedative |
| 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. | 4.11 | 4 | 0 | ||
| dihydroergotamine Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension. | 3.23 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| medroxyprogesterone [no description available] | 12.49 | 9 | 2 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | contraceptive drug; progestin; synthetic oral contraceptive |
| androstenediol Androstenediol: An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES).. androst-5-ene-3beta,17beta-diol : A 3beta-hydroxy-Delta(5)-steroid that is 3beta-hydroxyandrost-5-ene carrying an additional hydroxy group at position 17beta. | 1.99 | 1 | 0 | 17beta-hydroxy steroid; 3beta-hydroxy-Delta(5)-steroid | androgen; human metabolite; mouse metabolite; radiation protective agent |
| 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. | 6.47 | 6 | 3 | 17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid | androgen; Daphnia magna metabolite; human metabolite; mouse metabolite |
| dimenhydrinate gravinol: has antioxidant and ant-inflammatory activities; structure in first source | 3.23 | 1 | 0 | diarylmethane | |
| methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. | 3.23 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| levocarnitine (R)-carnitine : The (R)-enantiomer of carnitine. | 3.23 | 1 | 0 | carnitine | antilipemic drug; nootropic agent; nutraceutical; Saccharomyces cerevisiae metabolite; water-soluble vitamin (role) |
| malondialdehyde Malondialdehyde: The dialdehyde of malonic acid.. malonaldehyde : A dialdehyde that is propane substituted by two oxo groups at the terminal carbon atoms respectively. A biomarker of oxidative damage to lipids caused by smoking, it exists in vivo mainly in the enol form. | 2.44 | 2 | 0 | dialdehyde | biomarker |
| sulfanilylurea sulfanilylurea: antimicrobial agent; structure | 3.23 | 1 | 0 | benzenes; sulfonamide | |
| formestane [no description available] | 13.47 | 11 | 7 | 17-oxo steroid; 3-oxo-Delta(4) steroid; enol; hydroxy steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lactulose [no description available] | 3.23 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| megestrol acetate [no description available] | 4.88 | 8 | 1 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| pamabrom [no description available] | 3.23 | 1 | 0 | ||
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 3.23 | 1 | 0 | acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid | antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary |
| erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively. | 5.21 | 3 | 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. | 3.11 | 5 | 0 | 17-oxo steroid; steroid sulfate | EC 2.7.1.33 (pantothenate kinase) inhibitor; human metabolite; mouse metabolite |
| 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. | 7.12 | 5 | 3 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| boldenone boldenone: RN given refers to (17beta)-isomer. boldenone : An 3-oxo-Delta(1),Delta(4)-steroid substituted by an oxo group at position 3 and a beta-hydroxy group at position 17. It is an anabolic androgenic steroid that has been developed for veterinary use. | 3.77 | 2 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; anabolic androgenic steroid | |
| diphenoxylate Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin. | 3.23 | 1 | 0 | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
| deoxycytidine [no description available] | 2.43 | 2 | 0 | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| ethambutol Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. | 3.23 | 1 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 3.23 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils. | 3.85 | 3 | 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 |
| ibufenac ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects. | 3.23 | 1 | 0 | monocarboxylic acid | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| metaxalone [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| spectinomycin Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis. | 3.23 | 1 | 0 | cyclic acetal; cyclic hemiketal; cyclic ketone; pyranobenzodioxin; secondary alcohol; secondary amino compound | antibacterial drug; antimicrobial agent; bacterial metabolite |
| dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. | 3.23 | 1 | 0 | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| amiloride Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid. | 3.23 | 1 | 0 | aromatic amine; guanidines; organochlorine compound; pyrazines | diuretic; sodium channel blocker |
| pimozide Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. | 3.23 | 1 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| methylprednisolone hemisuccinate Methylprednisolone Hemisuccinate: A water-soluble ester of METHYLPREDNISOLONE used for cardiac, allergic, and hypoxic emergencies. | 1.99 | 1 | 0 | corticosteroid hormone; hemisuccinate | |
| dexbrompheniramine dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | brompheniramine | anti-allergic agent; H1-receptor antagonist |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 3.23 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group. | 3.23 | 1 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| megestrol Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17. | 5.73 | 6 | 1 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| streptomycin [no description available] | 3.23 | 1 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| cladribine [no description available] | 3.23 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| carbenicillin Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| clomacran clomacran: RN given refers to parent cpd; structure | 3.23 | 1 | 0 | acridines | |
| methenamine hippurate methenamine hippurate: both parts of molecule contribute to its antibacterial action | 3.23 | 1 | 0 | N-acylglycine | |
| olsalazine olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease. | 3.23 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| 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. | 3.62 | 3 | 0 | metal allergen; nickel group element atom; platinum group metal atom | |
| gold Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts. | 2.11 | 1 | 0 | copper group element atom; elemental gold | |
| helium Helium: A noble gas with the atomic symbol He, atomic number 2, and atomic weight 4.003. It is a colorless, odorless, tasteless gas that is not combustible and does not support combustion. It was first detected in the sun and is now obtained from natural gas. Medically it is used as a diluent for other gases, being especially useful with oxygen in the treatment of certain cases of respiratory obstruction, and as a vehicle for general anesthetics. | 4.27 | 1 | 0 | monoatomic helium; noble gas atom; s-block element atom | food packaging gas |
| 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. | 3.42 | 1 | 1 | iron molecular entity; metal sulfate | reducing agent |
| sodium thiosulfate sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio. | 3.23 | 1 | 0 | inorganic sodium salt | antidote to cyanide poisoning; antifungal drug; nephroprotective agent |
| deuterium Deuterium: The stable isotope of hydrogen. It has one neutron and one proton in the nucleus. | 2 | 1 | 0 | dihydrogen | |
| hexadimethrine bromide Hexadimethrine Bromide: A synthetic polymer which agglutinates red blood cells. It is used as a heparin antagonist. | 2.03 | 1 | 0 | ||
| selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. | 3.23 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| clemastine Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions. | 3.59 | 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. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| 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. | 4.3 | 3 | 0 | 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. | 2.01 | 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 |
| 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. | 11.22 | 36 | 12 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| fenclozic acid fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd | 3.23 | 1 | 0 | ||
| laxagetten 4,4'-diacetoxydiphenylpyridylemethane [no description available] | 3.23 | 1 | 0 | ||
| daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola. | 3.23 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| lofexidine lofexidine: reduces narcotic withdrawal symptoms; RN given refers to parent cpd without isomeric designation; structure in Negwer, 5th ed, #6247 | 3.19 | 1 | 0 | aromatic ether; carboxamidine; dichlorobenzene; imidazoles | alpha-adrenergic agonist; antihypertensive agent |
| 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. | 2.05 | 1 | 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. | 3.23 | 1 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| alclofenac alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash. | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid; monochlorobenzenes | drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 5.58 | 5 | 1 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| oxyphenisatin [no description available] | 3.23 | 1 | 0 | indoles | |
| fludrocortisone Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; fluorinated steroid; mineralocorticoid | adrenergic agent; anti-inflammatory drug |
| ursodeoxycholic acid Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 3.23 | 1 | 0 | chlorphenamine | |
| clometacin clometacin: structure | 3.23 | 1 | 0 | N-acylindole | |
| cefazolin Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| adenosine diphosphate ribose Adenosine Diphosphate Ribose: An ester formed between the aldehydic carbon of RIBOSE and the terminal phosphate of ADENOSINE DIPHOSPHATE. It is produced by the hydrolysis of nicotinamide-adenine dinucleotide (NAD) by a variety of enzymes, some of which transfer an ADP-ribosyl group to target proteins. | 2 | 1 | 0 | ADP-sugar | Escherichia coli metabolite; mouse metabolite |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| timolol (S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine. | 3.23 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. | 3.23 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| carbidopa carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa. | 3.23 | 1 | 0 | catechols; hydrazines; monocarboxylic acid | antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor |
| moricizine Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group. | 3.23 | 1 | 0 | carbamate ester; morpholines; phenothiazines | anti-arrhythmia drug |
| amineptin amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne. | 3.23 | 1 | 0 | amino acid; carbocyclic fatty acid; carbotricyclic compound; secondary amino compound | antidepressant; dopamine uptake inhibitor |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 3.23 | 1 | 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 | 3.23 | 1 | 0 | pyrroline | |
| 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). | 5.93 | 4 | 1 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 3.23 | 1 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| dobutamine Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure. | 3.23 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| penbutolol Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent. | 3.23 | 1 | 0 | ethanolamines | |
| ribavirin Rebetron: Rebetron is tradename | 3.23 | 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 |
| amikacin Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group. | 3.23 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| cephradine Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin | antibacterial drug |
| ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes | antihypertensive agent; hepatotoxic agent; loop diuretic |
| methyldopa Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 3.23 | 1 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
| vecuronium vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents. | 3.23 | 1 | 0 | acetate ester; androstane; quaternary ammonium ion | drug allergen; muscle relaxant; neuromuscular agent; nicotinic antagonist |
| benoxaprofen benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals. | 3.23 | 1 | 0 | 1,3-benzoxazoles; monocarboxylic acid; monochlorobenzenes | antipsoriatic; antipyretic; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; hepatotoxic agent; nephrotoxin; non-narcotic analgesic; non-steroidal anti-inflammatory drug; protein kinase C agonist |
| exifone [no description available] | 3.23 | 1 | 0 | benzophenones | |
| mefloquine (-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown. | 3.23 | 1 | 0 | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | antimalarial |
| desogestrel Desogestrel: A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED). | 3.35 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | contraceptive drug; progestin; synthetic oral contraceptive |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 3.23 | 1 | 0 | benzamides; carboxylic ester | |
| sufentanil Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid. | 3.23 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| acarbose [no description available] | 3.23 | 1 | 0 | tetrasaccharide derivative | EC 3.2.1.1 (alpha-amylase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; geroprotector; hypoglycemic agent |
| torsemide Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure. | 3.23 | 1 | 0 | aminopyridine; N-sulfonylurea; secondary amino compound | antihypertensive agent; loop diuretic |
| epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. | 7.86 | 7 | 2 | 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 |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 3.23 | 1 | 0 | anthracycline antibiotic; deoxy hexoside; monosaccharide derivative | |
| nitrosobis(2-oxopropyl)amine nitrosobis(2-oxopropyl)amine: structure. nitrosobis(2-oxopropyl)amine : A nitrosamine that is iminodiacetone that is substituted by a nitroso group at the N-atom. It induces pancreatic ductal adenocarcinomas in Syrian golden hamsters (other rodents are not susceptible). | 1.97 | 1 | 0 | ketone; nitrosamine | carcinogenic agent |
| piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo. | 3.23 | 1 | 0 | aromatic ether; benzodioxoles; organofluorine compound; piperidines | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug. | 3.23 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| cefoperazone Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| atracurium Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. | 3.23 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| pergolide Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. | 3.23 | 1 | 0 | diamine; methyl sulfide; organic heterotetracyclic compound | antiparkinson drug; dopamine agonist |
| 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. | 1.96 | 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. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| agreal veralipride: used in treatment of menopausal disorders; RN given refers to parent cpd | 3.36 | 1 | 1 | sulfonamide | |
| buserelin Buserelin: A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications. | 16.75 | 345 | 91 | oligopeptide | |
| fialuridine [no description available] | 3.23 | 1 | 0 | ||
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 3.23 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| haloperidol decanoate [no description available] | 3.23 | 1 | 0 | organic molecular entity | |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 3.23 | 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). | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| tolrestat tolrestat: RN & structure given in first source | 3.23 | 1 | 0 | naphthalenes | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 3.23 | 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 |
| balsalazide balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. | 3.23 | 1 | 0 | ||
| pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 3.23 | 1 | 0 | 3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic) | anticholesteremic drug; environmental contaminant; metabolite; xenobiotic |
| cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia. | 3.23 | 1 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 3.23 | 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. | 3.23 | 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] | 3.23 | 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. | 3.86 | 2 | 1 | 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. | 3.51 | 2 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| fosphenytoin fosphenytoin: structure given in first & second source | 3.23 | 1 | 0 | imidazolidine-2,4-dione | |
| ranolazine Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; monomethoxybenzene; N-alkylpiperazine; secondary alcohol | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 12.3 | 7 | 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 |
| fadrozole Fadrozole: A selective aromatase inhibitor effective in the treatment of estrogen-dependent disease including breast cancer. | 3.5 | 2 | 0 | imidazopyridine | |
| esmolol methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure. | 3.23 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | 3.23 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| aromasil [no description available] | 7.39 | 7 | 1 | 17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic |
| zileuton [no description available] | 3.23 | 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 |
| clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks. | 3.23 | 1 | 0 | methyl ester; monochlorobenzenes; thienopyridine | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 3.23 | 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. | 3.23 | 1 | 0 | beta-amino acid; piperidinemonocarboxylic acid; tertiary amino compound; thiophenes | anticonvulsant; GABA reuptake inhibitor |
| topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks. | 3.23 | 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. | 3.23 | 1 | 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. | 3.23 | 1 | 0 | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
| ibutilide ibutilide: RN & structure in first source; RN refers to the fumarate salt | 3.23 | 1 | 0 | benzenes; organic amino compound | |
| aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders. | 3.23 | 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. | 3.23 | 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] | 3.23 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 3.23 | 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 |
| duloxetine [no description available] | 3.23 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 3.23 | 1 | 0 | carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound | antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. | 3.23 | 1 | 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. | 4.98 | 2 | 1 | ||
| ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms. | 3.23 | 1 | 0 | 1,2-benzisothiazole; indolones; organochlorine compound; piperazines | antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist |
| zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine. | 3.23 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| tasosartan tasosartan: angiotensin II antagonist; structure given in first source | 3.23 | 1 | 0 | biphenyls | |
| tiludronic acid tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source | 3.23 | 1 | 0 | organochlorine compound | |
| tirofiban Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group. | 3.23 | 1 | 0 | L-tyrosine derivative; piperidines; sulfonamide | anticoagulant; fibrin modulating drug; platelet glycoprotein-IIb/IIIa receptor antagonist |
| capecitabine Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers. | 3.84 | 3 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 3.23 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| trovafloxacin trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure. | 3.23 | 1 | 0 | ||
| cefprozil [no description available] | 3.23 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 3.23 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| fenofibric acid fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate. | 3.23 | 1 | 0 | aromatic ketone; chlorobenzophenone; monocarboxylic acid | drug metabolite; marine xenobiotic metabolite |
| plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. | 3.23 | 1 | 0 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| amprenavir [no description available] | 3.23 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| oseltamivir Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. | 3.23 | 1 | 0 | acetamides; amino acid ester; cyclohexenecarboxylate ester; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; environmental contaminant; prodrug; xenobiotic |
| histamine phosphate histamine phosphate : A phosphate salt that is the diphosphate salt of histamine. | 3.23 | 1 | 0 | phosphate salt | histamine agonist |
| tilbroquinol [no description available] | 3.23 | 1 | 0 | organohalogen compound; quinolines | |
| bendamustine [no description available] | 3.23 | 1 | 0 | benzimidazoles | |
| droxicam droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis. | 3.23 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| ebrotidine ebrotidine: an H2-receptor antagonist and gastric mucosa protector | 3.23 | 1 | 0 | sulfonamide | |
| repaglinide [no description available] | 3.23 | 1 | 0 | piperidines | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| trenbolone acetate Trenbolone Acetate: An anabolic steroid used mainly as an anabolic agent in veterinary practice. | 3.78 | 2 | 1 | steroid ester | |
| 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. | 15.08 | 51 | 24 | 1,2,3-triazole | |
| fluorodeoxyglucose f18 Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162) | 2 | 1 | 0 | 2-deoxy-2-((18)F)fluoro-D-glucose; 2-deoxy-2-fluoro-aldehydo-D-glucose | |
| 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. | 4.05 | 2 | 0 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 12.32 | 24 | 13 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| dienogest [no description available] | 5.63 | 4 | 1 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; aliphatic nitrile; steroid hormone | progesterone receptor agonist; progestin; synthetic oral contraceptive |
| 5-fluoropyrimidine [no description available] | 2.02 | 1 | 0 | ||
| acamprosate Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3. | 3.23 | 1 | 0 | acetamides; organosulfonic acid | environmental contaminant; neurotransmitter agent; xenobiotic |
| isaxonine isaxonine: promotes nerve growth | 3.23 | 1 | 0 | aminopyrimidine | |
| nebivolol 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group. | 3.23 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 3.23 | 1 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| hp 873 iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound | dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 3.23 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| fenoxypropazine [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| aceclofenac [no description available] | 3.23 | 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 |
| nitrefazole [no description available] | 3.23 | 1 | 0 | imidazoles | |
| doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | 3.23 | 1 | 0 | carbapenems | |
| atovaquone Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position. | 3.23 | 1 | 0 | hydroxy-1,2-naphthoquinone | |
| rivastigmine [no description available] | 3.23 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 3.23 | 1 | 0 | carbazoles | |
| eletriptan eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group. | 3.23 | 1 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 3.23 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| bexarotene [no description available] | 3.23 | 1 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic 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. | 3.23 | 1 | 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) | 3.11 | 1 | 0 | ||
| moexipril [no description available] | 3.23 | 1 | 0 | peptide | |
| 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. | 7.01 | 1 | 0 | amino acid zwitterion; homocysteine; serine family amino acid | fundamental metabolite; mouse metabolite |
| mci 9038 [no description available] | 3.23 | 1 | 0 | peptide | |
| 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. | 9.66 | 10 | 4 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| ici 164384 ICI 164384: structure given in first source. ICI-164384 : A 3-hydroxy steroid that is 17beta-estradiol substituted by a 11-[butyl(methyl)amino]-11-oxoundecyl group at position 7R. It is a steroidal antioestrogen that inhibits the cell proliferation of breast-carcinoma cell lines. | 1.97 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; tertiary carboxamide | anti-estrogen; antineoplastic agent; estrogen receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 3.23 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| pyridinoline pyridinoline: 3-hydroxypyridinium derivative collagen crosslink; structure | 4.86 | 4 | 2 | organonitrogen compound; organooxygen compound | |
| deoxypyridinoline deoxypyridinoline: structure given in first source | 5.04 | 5 | 2 | ||
| 22-hydroxycholesterol [no description available] | 1.96 | 1 | 0 | cholanoid | |
| perindopril Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline | 3.23 | 1 | 0 | alpha-amino acid ester; dicarboxylic acid monoester; ethyl ester; organic heterobicyclic compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| deoxyglucose Deoxyglucose: 2-Deoxy-D-arabino-hexose. An antimetabolite of glucose with antiviral activity.. deoxyglucose : A deoxyhexose comprising glucose having at least one hydroxy group replaced by hydrogen. | 2 | 1 | 0 | ||
| tadalafil [no description available] | 3.23 | 1 | 0 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| paliperidone 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
| estrone-3-glucuronide [no description available] | 3.76 | 2 | 1 | 17-oxo steroid; beta-D-glucosiduronic acid; steroid glucosiduronic acid | human metabolite; mouse metabolite |
| nitisinone [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| clofarabine [no description available] | 3.23 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| pramipexole Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively. | 3.23 | 1 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 3.23 | 1 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| almotriptan almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. | 3.23 | 1 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| gefitinib [no description available] | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| desloratadine desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | 3.23 | 1 | 0 | benzocycloheptapyridine | anti-allergic agent; cholinergic antagonist; drug metabolite; H1-receptor antagonist |
| desvenlafaxine O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine. | 3.23 | 1 | 0 | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
| methotrexate [no description available] | 13.88 | 44 | 22 | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent |
| tamsulosin [no description available] | 5.74 | 3 | 1 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| rufinamide rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source | 3.23 | 1 | 0 | aromatic amide; heteroarene | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 3.23 | 1 | 0 | biphenyls | |
| dexpanthenol dexpanthenol: The alcohol of pantothenic acid | 3.23 | 1 | 0 | amino alcohol; monocarboxylic acid amide | cholinergic drug; provitamin |
| fosamprenavir fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir. | 3.23 | 1 | 0 | sulfonamide | prodrug |
| abiraterone [no description available] | 6.44 | 4 | 1 | 3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor |
| febuxostat Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout. | 3.23 | 1 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| escitalopram Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram. | 3.23 | 1 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| 10-propargyl-10-deazaaminopterin 10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma. | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pteridines; terminal acetylenic compound | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | 10.85 | 16 | 9 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). | 3.23 | 1 | 0 | carbohydrazide | antiviral drug; HIV protease inhibitor |
| levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | 3.23 | 1 | 0 | 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). | 3.23 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract. | 3.23 | 1 | 0 | carbapenemcarboxylic acid; pyrrolidinecarboxamide | antibacterial drug |
| cox 189 lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity. | 3.23 | 1 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| conivaptan conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). | 3.23 | 1 | 0 | benzazepine | aquaretic; vasopressin receptor antagonist |
| moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. | 3.23 | 1 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| pralnacasan pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source | 3.23 | 1 | 0 | ||
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 3.23 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 3.23 | 1 | 0 | isoquinolines | |
| dexmethylphenidate dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate. | 3.23 | 1 | 0 | methyl phenyl(piperidin-2-yl)acetate | adrenergic agent |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 3.23 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| cinacalcet cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| lubiprostone [no description available] | 3.23 | 1 | 0 | ||
| atazanavir sulfate Atazanavir Sulfate: An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS. | 3.51 | 1 | 0 | organic sulfate salt | |
| telbivudine [no description available] | 3.23 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| carbazic acid [no description available] | 2 | 1 | 0 | monocarboxylic acid; one-carbon compound | |
| 16-hydroxyprogesterone 16-hydroxyprogesterone: RN given refers to unlabeled cpd without isomeric designation | 1.97 | 1 | 0 | corticosteroid hormone | |
| folligen [no description available] | 2.38 | 2 | 0 | ||
| paromomycin Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis. | 3.23 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | anthelminthic drug; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| anidulafungin Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis. | 3.23 | 1 | 0 | antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative | |
| 17 alpha-hydroxyprogesterone caproate 17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS. | 3.23 | 1 | 0 | corticosteroid hormone | |
| varenicline Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. | 3.23 | 1 | 0 | ||
| fiduxosin fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source | 3.23 | 1 | 0 | ||
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 3.23 | 1 | 0 | ||
| erlotinib [no description available] | 3.23 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| etravirine [no description available] | 3.23 | 1 | 0 | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor |
| dronedarone Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 3.23 | 1 | 0 | indanes | |
| lapatinib [no description available] | 3.23 | 1 | 0 | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor |
| darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. | 3.23 | 1 | 0 | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
| deferasirox Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. | 3.23 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 3.23 | 1 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 3.23 | 1 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| sorafenib [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor |
| lenalidomide [no description available] | 3.23 | 1 | 0 | aromatic amine; dicarboximide; isoindoles; piperidones | angiogenesis inhibitor; antineoplastic agent; immunomodulator |
| regadenoson [no description available] | 3.23 | 1 | 0 | purine nucleoside | |
| lacosamide Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| cortisone [no description available] | 1.98 | 1 | 0 | 11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| vincaleukoblastine [no description available] | 3.23 | 1 | 0 | acetate ester; indole alkaloid fundamental parent; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; immunosuppressive agent; microtubule-destabilising agent; plant metabolite |
| benzarone benzarone: antihemorrhagic agent; structure | 3.23 | 1 | 0 | 1-benzofurans | |
| estramustine Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid. | 14.99 | 14 | 6 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| bortezomib [no description available] | 3.23 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 3.23 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour. | 3.54 | 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. | 3.23 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 3.23 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively. | 3.23 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| griseofulvin Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment. | 3.23 | 1 | 0 | 1-benzofurans; antibiotic antifungal drug; benzofuran antifungal drug; organochlorine compound; oxaspiro compound | antibacterial agent; Penicillium metabolite |
| cefoxitin Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; cephamycin; semisynthetic derivative | antibacterial drug |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 3.23 | 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. | 3.23 | 1 | 0 | acetate ester; steroid ester | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| abacavir abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | 3.23 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| miglitol [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | antihypertensive agent; EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor |
| linezolid [no description available] | 3.23 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| clindamycin phosphate [no description available] | 3.23 | 1 | 0 | ||
| eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
| tolterodine [no description available] | 3.23 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| 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. | 11.17 | 7 | 5 | 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. | 3.23 | 1 | 0 | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 3.23 | 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 |
| retinol Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified). | 3.23 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 3.23 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. | 3.23 | 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. | 3.23 | 1 | 0 | ||
| fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus. | 3.23 | 1 | 0 | epoxide; phosphonic acids | antimicrobial agent; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor |
| zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| epothilone b [no description available] | 2.01 | 1 | 0 | epothilone; epoxide | antineoplastic agent; apoptosis inducer; microtubule-stabilising 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. | 16.74 | 35 | 15 | 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 |
| octreotide [no description available] | 3.23 | 1 | 0 | ||
| epothilone a Epothilones: A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES). | 2.01 | 1 | 0 | epothilone; epoxide | antineoplastic agent; metabolite; microtubule-stabilising agent; tubulin modulator |
| eptifibatide [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| imidazolidines [no description available] | 6.65 | 9 | 2 | azacycloalkane; imidazolidines; saturated organic heteromonocyclic parent | |
| decitabine [no description available] | 3.23 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 3.23 | 1 | 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 |
| dactinomycin Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015) | 3.23 | 1 | 0 | actinomycin | mutagen |
| 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. | 1.97 | 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. | 3.23 | 1 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| enkephalin, leucine Enkephalin, Leucine: One of the endogenous pentapeptides with morphine-like activity. It differs from MET-ENKEPHALIN in the LEUCINE at position 5. Its first four amino acid sequence is identical to the tetrapeptide sequence at the N-terminal of BETA-ENDORPHIN.. Leu-enkephalin : A pentapeptide comprising L-tyrosine, glycine, glycine, L-phenylalanine and L-leucine residues joined in sequence by peptide linkages. It is an endogenous opioid peptide produced in vertebrate species, including rodents, primates and humans that results from decomposition of proenkephalin or dynorphin and exhibits antinociceptive properties. | 2.04 | 1 | 0 | pentapeptide; peptide zwitterion | analgesic; delta-opioid receptor agonist; human metabolite; mu-opioid receptor agonist; neurotransmitter; rat metabolite |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 3.23 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 3.23 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy. | 3.23 | 1 | 0 | antibiotic antifungal drug; echinocandin | antiinfective agent |
| riboflavin vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms). | 3.23 | 1 | 0 | flavin; vitamin B2 | anti-inflammatory agent; antioxidant; cofactor; Escherichia coli metabolite; food colouring; fundamental metabolite; human urinary metabolite; mouse metabolite; photosensitizing agent; plant metabolite |
| sodium bicarbonate Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions. | 3.23 | 1 | 0 | one-carbon compound; organic sodium salt | antacid; food anticaking agent |
| arsenic trioxide Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius. | 3.23 | 1 | 0 | arsenic oxide | antineoplastic agent; insecticide |
| sr 90107 fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux. | 3.23 | 1 | 0 | ||
| meglumine iodipamide [no description available] | 3.23 | 1 | 0 | organoammonium salt | radioopaque medium |
| nemorosone [no description available] | 3.13 | 1 | 0 | ||
| thyrotropin-releasing hormone PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence. | 3.23 | 1 | 0 | peptide hormone; tripeptide | human metabolite |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 3.23 | 1 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| s 1033 [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| leuprolide Leuprolide: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE that regulates the synthesis and release of pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE.. leuprolide : An oligopeptide comprising pyroglutamyl, histidyl, tryptophyl, seryl, tyrosyl, D-leucyl, leucyl, arginyl, and N-ethylprolinamide residues joined in sequence. It is a synthetic nonapeptide analogue of gonadotropin-releasing hormone, and is used as a subcutaneous hydrogel implant (particularly as the acetate salt) for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty. | 19.98 | 232 | 73 | oligopeptide | anti-estrogen; antineoplastic agent; gonadotropin releasing hormone agonist |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 3.23 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. | 3.23 | 1 | 0 | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 3.23 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| pyrantel Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'. | 3.23 | 1 | 0 | 1,4,5,6-tetrahydropyrimidines; carboxamidine; thiophenes | antinematodal drug |
| thiothixene [no description available] | 3.23 | 1 | 0 | N-methylpiperazine | anticoronaviral agent |
| eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. | 3.23 | 1 | 0 | zopiclone | central nervous system depressant; sedative |
| benztropine Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments. | 3.23 | 1 | 0 | diarylmethane | |
| thiohydantoins Thiohydantoins: Sulfur analogs of hydantoins with one or both carbonyl groups replaced by thiocarbonyl groups. | 4.51 | 1 | 1 | ||
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 3.23 | 1 | 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. | 3.23 | 1 | 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. | 4.06 | 3 | 1 | ||
| terbinafine [no description available] | 3.23 | 1 | 0 | acetylenic compound; allylamine antifungal drug; enyne; naphthalenes; tertiary amine | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor; sterol biosynthesis inhibitor |
| thioguanine anhydrous Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia. | 3.23 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| succimer Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning. | 3.23 | 1 | 0 | dicarboxylic acid; dithiol; sulfur-containing carboxylic acid | chelator |
| digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. | 3.23 | 1 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| streptozocin [no description available] | 3.23 | 1 | 0 | ||
| tamoxifen [no description available] | 19.78 | 188 | 56 | 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 |
| ethionamide Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide. | 3.23 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 3.23 | 1 | 0 | ||
| lincomycin Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis. | 3.23 | 1 | 0 | carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound | antimicrobial agent; bacterial metabolite |
| ranitidine Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease. | 3.23 | 1 | 0 | C-nitro compound; furans; organic sulfide; tertiary amino compound | anti-ulcer drug; drug allergen; environmental contaminant; H2-receptor antagonist; xenobiotic |
| aplaviroc aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source | 3.23 | 1 | 0 | ||
| hmr 3647 [no description available] | 3.23 | 1 | 0 | ||
| maraviroc [no description available] | 3.23 | 1 | 0 | tropane alkaloid | |
| toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. | 4.06 | 2 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| nelarabine nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| fosfestrol fosfestrol: Rx of prostatic carcinoma; RN given refers to parent cpd with unspecified isomeric designation; structure | 4.51 | 4 | 0 | aryl phosphate | |
| dermatan sulfate Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units. | 3.23 | 1 | 0 | amino disaccharide; glycosylgalactose derivative; iduronic acids; oligosaccharide sulfate | |
| dolasetron [no description available] | 3.23 | 1 | 0 | indolyl carboxylic acid | |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 3.23 | 1 | 0 | beta-lactone; carboxylic ester; formamides; L-leucine derivative | anti-obesity agent; bacterial metabolite; EC 2.3.1.85 (fatty acid synthase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor |
| quinine [no description available] | 3.23 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| win 33377 WIN 33377: structure in first source | 3.11 | 1 | 0 | ||
| fospropofol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| rasagiline [no description available] | 3.23 | 1 | 0 | indanes; secondary amine; terminal acetylenic compound | EC 1.4.3.4 (monoamine oxidase) inhibitor; neuroprotective agent |
| dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). | 3.23 | 1 | 0 | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| 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. | 1.96 | 1 | 0 | ||
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 3.23 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 3.23 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 5.95 | 5 | 0 | D3 vitamins; hydroxycalciol; triol | antineoplastic agent; antipsoriatic; bone density conservation agent; calcium channel agonist; calcium channel modulator; hormone; human metabolite; immunomodulator; metabolite; mouse metabolite; nutraceutical |
| beta carotene beta Carotene: A carotenoid that is a precursor of VITAMIN A. Beta carotene is administered to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria (PORPHYRIA, ERYTHROPOIETIC).. provitamin A : A provitamin that can be converted into vitamin A by enzymes from animal tissues. | 1.96 | 1 | 0 | carotenoid beta-end derivative; cyclic carotene | antioxidant; biological pigment; cofactor; ferroptosis inhibitor; human metabolite; mouse metabolite; plant metabolite; provitamin A |
| vitamin d 2 Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa. | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| gamma-linolenic acid gamma-Linolenic Acid: An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed). gamma-linolenic acid : A C18, omega-6 acid fatty acid comprising a linolenic acid having cis- double bonds at positions 6, 9 and 12. | 2.38 | 2 | 0 | linolenic acid; omega-6 fatty acid | human metabolite; mouse metabolite; plant metabolite |
| amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections. | 3.23 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| oxymetholone Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects. | 3.23 | 1 | 0 | ||
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 3.23 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | aliphatic sulfide; monocarboxylic acid; quinolines | anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist |
| mivacurium Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent. | 3.23 | 1 | 0 | isoquinolines | |
| hemabate carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy. | 3.23 | 1 | 0 | ||
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 3.23 | 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] | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| 7432 s Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections. | 3.23 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 3.23 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| misoprostol Misoprostol: A synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties.. misoprostol : A diastereoisomeric mixture composed of approximately equal amounts of a double racemate of four of the sixteen possible diastereoisomers of methyl (13E)-11,16-dihydroxy-16-methyl-9-oxoprost-13-en-1-oate that is racemic prostaglandin E1 which is lacking the hydroxy group at position 15, but which has an additional hydroxy group at position 16. It is a synthetic prostaglandin E1 analogue, used in the treatment of gastric and duodenal ulcers. A weak abortifacient, it is also used for cervical ripening prior to surgical termination of pregnancy. The (11R,16S)-diastereoisomer is the pharmacologically active form. | 8.37 | 1 | 1 | ||
| epoprostenol [no description available] | 3.23 | 1 | 0 | prostaglandins I | mouse metabolite |
| indocyanine green [no description available] | 3.23 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| triprolidine Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders. | 3.23 | 1 | 0 | N-alkylpyrrolidine; olefinic compound; pyridines | H1-receptor antagonist |
| pitavastatin pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise. | 3.23 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| ethamolin monoethanolamine oleate: used for treatment of pyogenic granuloma | 3.23 | 1 | 0 | long-chain fatty acid | |
| alatrofloxacin mesylate [no description available] | 3.23 | 1 | 0 | ||
| codeine [no description available] | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | antitussive; drug allergen; environmental contaminant; opioid analgesic; opioid receptor agonist; prodrug; xenobiotic |
| cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | 3.23 | 1 | 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 |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 3.23 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| 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. | 7.72 | 15 | 4 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; chlorinated steroid; tertiary alpha-hydroxy ketone | androgen antagonist |
| estropipate estropipate: used therapeutically in menopausal patients | 3.23 | 1 | 0 | piperazinium salt; steroid sulfate | |
| hydromorphone Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | mu-opioid receptor agonist; opioid analgesic |
| levetiracetam Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine. | 3.23 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| ly 163892 loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria. | 3.23 | 1 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nabilone nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure | 3.23 | 1 | 0 | ||
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| oxycodone Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain. | 3.23 | 1 | 0 | organic heteropentacyclic compound; semisynthetic derivative | antitussive; mu-opioid receptor agonist; opioid analgesic |
| oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) | 3.23 | 1 | 0 | morphinane alkaloid | |
| vitamin k 1 Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones. | 3.23 | 1 | 0 | phylloquinones; vitamin K | cofactor; human metabolite; plant metabolite |
| sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. | 3.23 | 1 | 0 | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 3.23 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| trospium chloride trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder. | 3.23 | 1 | 0 | ||
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound | anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic |
| benzphetamine Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity. | 3.23 | 1 | 0 | amphetamines; tertiary amine | adrenergic uptake inhibitor; appetite depressant; dopamine uptake inhibitor; sympathomimetic agent |
| cloprostenol Cloprostenol: A synthetic prostaglandin F2alpha analog. The compound has luteolytic effects and is used for the synchronization of estrus in cattle. | 1.96 | 1 | 0 | prostanoid | |
| deamino arginine vasopressin Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR. | 3.23 | 1 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 3.23 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| nalbuphine Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. | 3.23 | 1 | 0 | organic heteropentacyclic compound | mu-opioid receptor antagonist; opioid analgesic |
| nateglinide Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 3.23 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| onapristone onapristone: induces vaginal bleeding and luteal regression in monkeys; structure given in first source; progesterone antagonist | 1.99 | 1 | 0 | ||
| silodosin silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source | 3.23 | 1 | 0 | indolecarboxamide | |
| fluvoxamine Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 5.26 | 3 | 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] | 4.86 | 2 | 1 | aminopyridine; aromatic ketone; cyclopentanes; piperidines; pyridopyrimidine; secondary amino compound; tertiary amino compound | antineoplastic agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| levorphanol Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. | 3.23 | 1 | 0 | morphinane alkaloid | |
| naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | 3.23 | 1 | 0 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough. | 3.23 | 1 | 0 | 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene | antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic |
| butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | 3.23 | 1 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| lisinopril Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| benazepril benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. | 3.23 | 1 | 0 | benzazepine; dicarboxylic acid monoester; ethyl ester; lactam | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 3.23 | 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 |
| verteporfin (2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid. | 3.23 | 1 | 0 | ||
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 3.23 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| zimeldine Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) | 3.23 | 1 | 0 | styrenes | |
| enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration). | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| trientine hydrochloride [no description available] | 3.23 | 1 | 0 | ||
| n-methylscopolamine bromide scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. | 3.23 | 1 | 0 | ||
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic agent; metabolite |
| enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. | 3.23 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ximelagatran ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | 3.23 | 1 | 0 | amidoxime; azetidines; carboxamide; ethyl ester; hydroxylamines; secondary amino compound; secondary carboxamide; tertiary carboxamide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor; prodrug; serine protease inhibitor |
| cefuroxime [no description available] | 3.23 | 1 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 3.5.2.6 (beta-lactamase) inhibitor |
| cefepime Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| pafuramidine pafuramidine: a prodrug of furamidine | 3.23 | 1 | 0 | ||
| ceftazidime [no description available] | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| trandolapril trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; organic heterobicyclic compound; secondary amino compound; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| ay 25,205 surfagon: potent LHRH agonist; RN given refers to (D-Ala-L-Pro)-isomer | 1.96 | 1 | 0 | ||
| pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 3.23 | 1 | 0 | peptide | |
| aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; monomethoxybenzene | antihypertensive agent |
| famotidine [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| lhrh, n-et-alanh2(6)- [no description available] | 1.97 | 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. | 2.1 | 1 | 0 | alkaline earth metal atom | |
| cefpodoxime [no description available] | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| palonosetron Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | 3.23 | 1 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| pregnanediol [no description available] | 3.76 | 2 | 1 | ||
| rifaximin [no description available] | 3.23 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 3.64 | 2 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| ceftizoxime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 3.23 | 1 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 3.23 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| dantrolene [no description available] | 3.23 | 1 | 0 | ||
| cefdinir [no description available] | 3.23 | 1 | 0 | cephalosporin; ketoxime | antibacterial drug |
| etonogestrel [no description available] | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| vorozole vorozole: structure given in first source; vorozole/R 83842 is ((+)/dextro-isomer), RN 129731-10-8; R 83839 ((-)/levo-isomer) | 8.38 | 1 | 1 | benzotriazoles | |
| temsirolimus [no description available] | 3.23 | 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. | 5.92 | 2 | 1 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 3.23 | 1 | 0 | diarylmethane | |
| bibx 1382bs BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001 | 3.23 | 1 | 0 | substituted aniline | |
| fesoterodine fesoterodine: a muscarinic antagonist for treatment of overactive bladder | 3.23 | 1 | 0 | diarylmethane | |
| taxane taxane: produced by Taxomyces andreanae | 2.47 | 2 | 0 | diterpene; terpenoid fundamental parent | |
| gemifloxacin Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position. | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; fluoroquinolone antibiotic; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; topoisomerase IV inhibitor |
| dexlansoprazole Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | 3.23 | 1 | 0 | benzimidazoles; sulfoxide | |
| fosinopril [no description available] | 3.23 | 1 | 0 | ||
| armodafinil armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness. | 3.23 | 1 | 0 | 2-[(diphenylmethyl)sulfinyl]acetamide | central nervous system stimulant; eugeroic |
| amoxicillin-potassium clavulanate combination Amoxicillin-Potassium Clavulanate Combination: A fixed-ratio combination of amoxicillin trihydrate and potassium clavulanate. | 2 | 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. | 4.51 | 1 | 1 | pyridines; sterol ester | antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor; prodrug |
| sincalide Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas. | 3.23 | 1 | 0 | oligopeptide | |
| tapentadol Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES. | 3.23 | 1 | 0 | alkylbenzene | |
| pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. | 3.23 | 1 | 0 | organic molecular entity | |
| 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. | 2.1 | 1 | 0 | tetracyclic diterpenoid | antineoplastic agent; microtubule-stabilising agent |
| cefditoren cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections. | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| medrogestone Medrogestone: 6,17-Dimethylpregna-4,6-diene-3,20-dione. A synthetic progestational hormone with actions similar to those of progesterone. It is used in the treatment of menstrual irregularities and has also been employed in the treatment of prostatic hypertrophy and endometrial carcinoma. | 8.38 | 1 | 1 | corticosteroid hormone | |
| cgp 20712a CGP 20712A: structure given in first source; CGP 26505, a beta1-selective beta-adrenoceptor antagonist, is the (S)-isomer of CGP 20712A | 1.97 | 1 | 0 | ||
| altrenogest altrenogest: a synthetic PROGESTERONE agonist; used in estrus synchronization | 3.78 | 2 | 1 | 3-hydroxy steroid | |
| pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. | 3.23 | 1 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| prasugrel hydrochloride Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels. | 3.23 | 1 | 0 | ||
| baci-im [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| bms 477118 [no description available] | 3.23 | 1 | 0 | adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| nystatin a1 Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species. | 3.23 | 1 | 0 | nystatins | |
| milnacipran [no description available] | 3.23 | 1 | 0 | acetamides | |
| calcimycin Calcimycin: An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems. | 2.37 | 2 | 0 | benzoxazole | |
| scopolamine hydrobromide [no description available] | 3.23 | 1 | 0 | ||
| pituitrin Pituitrin: A substance or extract from the neurohypophysis (PITUITARY GLAND, POSTERIOR). | 1.97 | 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 | 2.05 | 1 | 0 | ||
| 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. | 7.55 | 23 | 7 | ||
| mdv 3100 [no description available] | 5.08 | 4 | 0 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent |
| 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. | 3.06 | 1 | 0 | ||
| bivalirudin bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | 3.23 | 1 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| enfuvirtide Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes. | 3.23 | 1 | 0 | ||
| lhrh, his(5)-trp(7)-tyr(8)- LHRH, His(5)-Trp(7)-Tyr(8)-: isolated from chicken hypothalamus; also ostrich; RN given refers to all-(L)-isomer | 2.05 | 1 | 0 | ||
| ganirelix [no description available] | 3.23 | 1 | 0 | polypeptide | |
| adrenocorticotropin zinc [no description available] | 3.06 | 1 | 0 | ||
| 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. | 10.76 | 3 | 2 | polypeptide | antineoplastic agent; hormone antagonist |
| gastrins Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters. | 1.97 | 1 | 0 | ||
| 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. | 8.36 | 1 | 1 | peptide hormone | |
| neuropeptide y Neuropeptide Y: A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones. | 2 | 1 | 0 | ||
| teriparatide [no description available] | 3.23 | 1 | 0 | polypeptide | |
| salmon calcitonin [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone; polypeptide | bone density conservation agent; metabolite |
| ly-146032 [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt | 11.44 | 15 | 7 | polypeptide | |
| 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. | 3.78 | 2 | 1 | ||
| exenatide [no description available] | 3.23 | 1 | 0 | ||
| 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 | ||
| buparlisib NVP-BKM120: a pan class I PI3 kinase inhibitor with antineoplastic activity; structure in first source | 8.64 | 2 | 0 | aminopyridine; aminopyrimidine; morpholines; organofluorine compound | antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| 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. | 7.64 | 11 | 6 | ||
| chitosan [no description available] | 2.15 | 1 | 0 | ||
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 3.23 | 1 | 0 | organosulfonic acid | |
| 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. | 1.96 | 1 | 0 | 3',5'-cyclic purine nucleotide | |
| sodium lactate Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion. | 3.23 | 1 | 0 | lactate salt; organic sodium salt | food acidity regulator; food preservative |
| sodium iothalamate [no description available] | 3.23 | 1 | 0 | ||
| apalutamide [no description available] | 4.51 | 1 | 1 | ||
| quetiapine fumarate Quetiapine Fumarate: A dibenzothiazepine and ANTIPSYCHOTIC AGENT that targets the SEROTONIN 5-HT2 RECEPTOR; HISTAMINE H1 RECEPTOR, adrenergic alpha1 and alpha2 receptors, as well as the DOPAMINE D1 RECEPTOR and DOPAMINE D2 RECEPTOR. It is used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER and DEPRESSIVE DISORDER. | 2.02 | 1 | 0 | fumarate salt | |
| trelstar Triptorelin Pamoate: A potent synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE with D-tryptophan substitution at residue 6. | 12.89 | 44 | 10 | ||
| 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. | 11.47 | 7 | 2 | oligopeptide | antineoplastic agent; GnRH antagonist |
| lhrh, n-acetyl-(4-chlorophenylalanyl)(1)-(4-chlorophenylalanyl)(2)-tryptophyl(3)-arginyl(6)-alanine(10)- LHRH, N-acetyl-(4-chlorophenylalanyl)(1)-(4-chlorophenylalanyl)(2)-tryptophyl(3)-arginyl(6)-alanine(10)-: gonadorelin antagonist | 2.38 | 2 | 0 | ||
| 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. | 9.33 | 19 | 7 | 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 | 3.39 | 1 | 1 | 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. | 2.21 | 1 | 0 | oligopeptide | antineoplastic agent; gonadotropin releasing hormone agonist |
| ovurelin ovurelin: GnRH agonist | 2.38 | 2 | 0 | ||
| ribociclib ribociclib: inhibits both CDK4 and CDK6 | 2.66 | 2 | 0 | ||
| natriuretic peptide, brain Natriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS. | 5.36 | 2 | 2 | polypeptide | |
| ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms. | 3.59 | 2 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| raltegravir [no description available] | 3.23 | 1 | 0 | 1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide | antiviral drug; HIV-1 integrase inhibitor |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 3.23 | 1 | 0 | ||
| oxytetracycline, anhydrous Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae. | 3.23 | 1 | 0 | ||
| minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. | 3.23 | 1 | 0 | ||
| piroxicam [no description available] | 3.23 | 1 | 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 |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group. | 3.23 | 1 | 0 | benzenes; hydroxycoumarin; methyl ketone | |
| demeclocycline Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective. | 3.23 | 1 | 0 | ||
| tipranavir tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor. | 3.23 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| tigecycline [no description available] | 3.23 | 1 | 0 | ||
| byl719 [no description available] | 3.64 | 2 | 0 | proline derivative | |
| 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. | 3.24 | 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. | 3.42 | 1 | 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. | 2.05 | 1 | 0 | ||
| cyclin d1 Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms. | 4.34 | 1 | 1 | ||
| fertinex [no description available] | 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. | 2.04 | 1 | 0 | ||
| norgestrel Norgestrel: A synthetic progestational agent with actions similar to those of PROGESTERONE. This racemic or (+-)-form has about half the potency of the levo form (LEVONORGESTREL). Norgestrel is used as a contraceptive, ovulation inhibitor, and for the control of menstrual disorders and endometriosis. | 3.37 | 1 | 1 | ||
| 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. | 2.39 | 2 | 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). | 2.06 | 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. | 1.98 | 1 | 0 | ||
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| guanosine triphosphate Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety. | 3.41 | 1 | 1 | guanosine 5'-phosphate; purine ribonucleoside 5'-triphosphate | Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor |
| folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin. | 3.23 | 1 | 0 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 3.23 | 1 | 0 | cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion | angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor |
| clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound | adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic |
| dacarbazine (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | 3.23 | 1 | 0 | dacarbazine | |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 3.23 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 3.23 | 1 | 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. | 3.23 | 1 | 0 | L-valyl ester | antiviral drug |
| sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | 3.23 | 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. | 3.56 | 2 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| vardenafil vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | 3.23 | 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. | 3.59 | 2 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 3.23 | 1 | 0 | tetrahydrofolic acid | |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 3.23 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 3.23 | 1 | 0 | N-alkylpiperazine; N-iminopiperazine; rifamycins | antitubercular agent; leprostatic drug |
| bl 4162a anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions. | 3.23 | 1 | 0 | imidazoquinazoline | anticoagulant; antifibrinolytic drug; cardiovascular drug; platelet aggregation inhibitor |
| tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source | 3.23 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pyrrolopyrimidine | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor |
| valganciclovir Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine. | 3.23 | 1 | 0 | L-valyl ester; purines | antiviral drug; prodrug |
| aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| fosaprepitant fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; phosphoramide; triazoles | antiemetic; neurokinin-1 receptor antagonist; prodrug |
| rifabutin [no description available] | 3.23 | 1 | 0 | ||
| levomefolate calcium levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid. | 3.23 | 1 | 0 | organic calcium salt | antidepressant |
| 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. | 2.94 | 4 | 0 | ||
| pyrimidinones Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O. | 3.13 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 5.58 | 6 | 1 |
| Adverse Drug Event [description not available] | 0 | 4.9 | 4 | 2 |
| 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 | 5.58 | 6 | 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 | 4.9 | 4 | 2 |
| Breast Cancer [description not available] | 0 | 21.75 | 327 | 111 |
| Breast Neoplasms Tumors or cancer of the human BREAST. | 1 | 28.12 | 981 | 333 |
| Cancer of Prostate [description not available] | 0 | 26.34 | 974 | 558 |
| Prostatic Neoplasms Tumors or cancer of the PROSTATE. | 1 | 32.72 | 2,922 | 1,674 |
| Menstruation, Painful [description not available] | 0 | 6.72 | 11 | 2 |
| Dysmenorrhea Painful menstruation. | 0 | 6.72 | 11 | 2 |
| 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. | 1 | 11.84 | 6 | 1 |
| Cancer of Granulosa Cells [description not available] | 0 | 2.93 | 4 | 0 |
| Cancer of Ovary [description not available] | 0 | 9.13 | 24 | 5 |
| Meigs Syndrome The triad of benign FIBROMA or other ovarian tumors with ASCITES, and HYDROTHORAX due to large PLEURAL EFFUSIONS. | 0 | 2.31 | 1 | 0 |
| Ascites Accumulation or retention of free fluid within the peritoneal cavity. | 0 | 2.44 | 2 | 0 |
| 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 | 11.13 | 24 | 5 |
| 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 | 2.31 | 1 | 0 |
| Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. | 0 | 14.91 | 75 | 23 |
| Benign Neoplasms, Brain [description not available] | 0 | 2.8 | 3 | 0 |
| Astrocytoma, Grade IV [description not available] | 0 | 2.52 | 2 | 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 | 2.8 | 3 | 0 |
| Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures. | 0 | 2.52 | 2 | 0 |
| Diffuse Parenchymal Lung Disease [description not available] | 0 | 2.6 | 1 | 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 | 2.6 | 1 | 0 |
| HIV Coinfection [description not available] | 0 | 3.33 | 1 | 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). | 0 | 3.33 | 1 | 0 |
| Fibrosis, Radiation [description not available] | 0 | 3.51 | 5 | 0 |
| Radiation Pneumonitis Inflammation of the lung due to harmful effects of ionizing or non-ionizing radiation. | 0 | 3.51 | 5 | 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 | 16.46 | 129 | 52 |
| 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 | 18.46 | 129 | 52 |
| Fibroid [description not available] | 0 | 13.46 | 101 | 30 |
| Cancer of Lung [description not available] | 0 | 8.09 | 22 | 2 |
| Cancer of the Uterus [description not available] | 0 | 13.45 | 104 | 34 |
| 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 | 15.46 | 101 | 30 |
| Lung Neoplasms Tumors or cancer of the LUNG. | 0 | 8.09 | 22 | 2 |
| Uterine Neoplasms Tumors or cancer of the UTERUS. | 0 | 13.45 | 104 | 34 |
| Erythema Nodosum An erythematous eruption commonly associated with drug reactions or infection and characterized by inflammatory nodules that are usually tender, multiple, and bilateral. These nodules are located predominantly on the shins with less common occurrence on the thighs and forearms. They undergo characteristic color changes ending in temporary bruise-like areas. This condition usually subsides in 3-6 weeks without scarring or atrophy. | 0 | 8.52 | 1 | 0 |
| Visceral Pain Pain originating from internal organs (VISCERA) associated with autonomic phenomena (PALLOR; SWEATING; NAUSEA; and VOMITING). It often becomes a REFERRED PAIN. | 0 | 2.6 | 1 | 0 |
| Acute Post-operative Pain [description not available] | 0 | 6.17 | 4 | 3 |
| Pain, Postoperative Pain during the period after surgery. | 0 | 6.17 | 4 | 3 |
| Benign Neoplasms [description not available] | 0 | 4.86 | 5 | 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 | 6.86 | 5 | 0 |
| Recrudescence [description not available] | 0 | 9.55 | 19 | 11 |
| Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed) | 0 | 4.93 | 8 | 1 |
| Disease Exacerbation [description not available] | 0 | 13.13 | 53 | 21 |
| Local Neoplasm Recurrence [description not available] | 0 | 17.47 | 81 | 44 |
| Postpartum Amenorrhea [description not available] | 0 | 10.69 | 23 | 7 |
| Amenorrhea Absence of menstruation. | 0 | 15.69 | 23 | 7 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 5.24 | 4 | 1 |
| Impotence [description not available] | 0 | 8.68 | 9 | 7 |
| Erectile Dysfunction The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction. | 0 | 8.68 | 9 | 7 |
| Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders. | 0 | 9.58 | 10 | 6 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 0 | 5.21 | 4 | 1 |
| Atherogenesis [description not available] | 0 | 2.25 | 1 | 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 | 2.25 | 1 | 0 |
| Adenocarcinoma, Basal Cell [description not available] | 0 | 20.61 | 252 | 174 |
| Androgen-Independent Prostatic Cancer [description not available] | 0 | 5.98 | 4 | 2 |
| Adenocarcinoma A malignant epithelial tumor with a glandular organization. | 0 | 20.61 | 252 | 174 |
| 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 | 7.98 | 4 | 2 |
| Sterility, Female [description not available] | 0 | 11.57 | 31 | 5 |
| Pelvic Pain Pain in the pelvic region of genital and non-genital origin. | 0 | 10.76 | 12 | 5 |
| Infertility, Female Diminished or absent ability of a female to achieve conception. | 0 | 11.57 | 31 | 5 |
| 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 | 2.25 | 1 | 0 |
| Lower Urinary Tract Symptom [description not available] | 0 | 8.69 | 7 | 4 |
| FMR1-Related Primary Ovarian Insufficiency [description not available] | 0 | 11.35 | 23 | 10 |
| 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. | 1 | 13.35 | 23 | 10 |
| Lymph Node Metastasis [description not available] | 0 | 16.78 | 78 | 57 |
| Cancer of Skin [description not available] | 0 | 2.17 | 1 | 0 |
| Skin Neoplasms Tumors or cancer of the SKIN. | 0 | 2.17 | 1 | 0 |
| Skin Ulcer An ULCER of the skin and underlying tissues. | 0 | 2.17 | 1 | 0 |
| Bladder Cancer [description not available] | 0 | 2.15 | 1 | 0 |
| Angiomyxoma [description not available] | 0 | 4.56 | 5 | 0 |
| Cancer of the Vulva [description not available] | 0 | 2.75 | 3 | 0 |
| Invasiveness, Neoplasm [description not available] | 0 | 16.25 | 61 | 52 |
| Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER. | 0 | 2.15 | 1 | 0 |
| Vulvar Neoplasms Tumors or cancer of the VULVA. | 0 | 2.75 | 3 | 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 |
| Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM. | 0 | 13.46 | 36 | 33 |
| 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 |
| 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 | 2.17 | 1 | 0 |
| Epithelial Ovarian Cancer [description not available] | 0 | 7.17 | 1 | 0 |
| Epithelial Neoplasms [description not available] | 0 | 4.66 | 3 | 2 |
| 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 | 2.17 | 1 | 0 |
| Alopecia Cicatrisata [description not available] | 0 | 2.71 | 3 | 0 |
| Cirrhosis [description not available] | 0 | 4.35 | 4 | 1 |
| Alopecia Absence of hair from areas where it is normally present. | 0 | 2.71 | 3 | 0 |
| Atrophy Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes. | 0 | 2.72 | 3 | 0 |
| Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury. | 0 | 4.35 | 4 | 1 |
| Carcinoma, Intraepithelial [description not available] | 0 | 2.42 | 2 | 0 |
| 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 | 2.42 | 2 | 0 |
| Colonic Inertia Symptom characterized by the passage of stool once a week or less. | 0 | 4.48 | 1 | 1 |
| Nasopharyngitis Inflammation of the NASOPHARYNX, usually including its mucosa, related lymphoid structure, and glands. | 0 | 4.48 | 1 | 1 |
| 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 | 4.48 | 1 | 1 |
| Bleeding [description not available] | 0 | 3.38 | 2 | 0 |
| Cancer of Pelvis [description not available] | 0 | 5.39 | 5 | 1 |
| Ambulation Difficulty [description not available] | 0 | 3.09 | 1 | 0 |
| Abdominal Neoplasms New abnormal growth of tissue in the ABDOMEN. | 0 | 5.42 | 5 | 1 |
| Hemorrhage Bleeding or escape of blood from a vessel. | 0 | 3.38 | 2 | 0 |
| Neurofibroma A moderately firm, benign, encapsulated tumor resulting from proliferation of SCHWANN CELLS and FIBROBLASTS that includes portions of nerve fibers. The tumors usually develop along peripheral or cranial nerves and are a central feature of NEUROFIBROMATOSIS 1, where they may occur intracranially or involve spinal roots. Pathologic features include fusiform enlargement of the involved nerve. Microscopic examination reveals a disorganized and loose cellular pattern with elongated nuclei intermixed with fibrous strands. (From Adams et al., Principles of Neurology, 6th ed, p1016) | 0 | 3.09 | 1 | 0 |
| Metastase [description not available] | 0 | 13.62 | 40 | 25 |
| Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site. | 0 | 13.62 | 40 | 25 |
| Azoospermia A condition of having no sperm present in the ejaculate (SEMEN). | 0 | 3.09 | 1 | 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 | 5.02 | 3 | 1 |
| 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 | 6.38 | 5 | 1 |
| Abortion, Tubal [description not available] | 0 | 2.55 | 2 | 0 |
| 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 | 2.21 | 1 | 0 |
| Hemorrhage, Uterine [description not available] | 0 | 9.03 | 19 | 9 |
| Abortion, Spontaneous Expulsion of the product of FERTILIZATION before completing the term of GESTATION and without deliberate interference. | 0 | 2.55 | 2 | 0 |
| Uterine Hemorrhage Bleeding from blood vessels in the UTERUS, sometimes manifested as vaginal bleeding. | 0 | 9.03 | 19 | 9 |
| Genetic Predisposition [description not available] | 0 | 3.56 | 1 | 1 |
| Depression, Endogenous [description not available] | 0 | 3.67 | 3 | 0 |
| Depressive Disorder An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent. | 0 | 3.67 | 3 | 0 |
| Desmoid [description not available] | 0 | 3.64 | 3 | 0 |
| Adenomatous Polyposis Coli, Familial [description not available] | 0 | 3.62 | 3 | 0 |
| Adenomatous Polyposis Coli A polyposis syndrome due to an autosomal dominant mutation of the APC genes (GENES, APC) on CHROMOSOME 5. The syndrome is characterized by the development of hundreds of ADENOMATOUS POLYPS in the COLON and RECTUM of affected individuals by early adulthood. | 0 | 3.62 | 3 | 0 |
| Fibromatosis, Aggressive A childhood counterpart of abdominal or extra-abdominal desmoid tumors, characterized by firm subcutaneous nodules that grow rapidly in any part of the body but do not metastasize. The adult form of abdominal fibromatosis is FIBROMATOSIS, ABDOMINAL. (Stedman, 25th ed) | 0 | 3.64 | 3 | 0 |
| Bone Cancer [description not available] | 0 | 11 | 50 | 19 |
| Hormone-Dependent Neoplasms [description not available] | 0 | 16.53 | 76 | 30 |
| Bone Neoplasms Tumors or cancer located in bone tissue or specific BONES. | 0 | 11 | 50 | 19 |
| Lassitude [description not available] | 0 | 3.14 | 5 | 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 | 3.14 | 5 | 0 |
| Insulin Sensitivity [description not available] | 0 | 8.8 | 8 | 6 |
| 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 | 8.8 | 8 | 6 |
| Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY). | 0 | 7.67 | 5 | 4 |
| Heavy Menstrual Bleeding [description not available] | 0 | 10.66 | 33 | 16 |
| Menorrhagia Excessive uterine bleeding during MENSTRUATION. | 0 | 10.66 | 33 | 16 |
| Colicky Pain [description not available] | 0 | 2.73 | 3 | 0 |
| Abdominal Pain Sensation of discomfort, distress, or agony in the abdominal region. | 0 | 2.73 | 3 | 0 |
| 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 | 3.82 | 2 | 1 |
| Absence Seizure [description not available] | 0 | 2.08 | 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 | 2.08 | 1 | 0 |
| Carcinoma, Ductal, Breast An invasive (infiltrating) CARCINOMA of the mammary ductal system (MAMMARY GLANDS) in the human BREAST. | 0 | 6.06 | 10 | 1 |
| Carcinoma, Colloid [description not available] | 0 | 2.13 | 1 | 0 |
| Delayed Effects, Prenatal Exposure [description not available] | 0 | 2.43 | 2 | 0 |
| Adenocarcinoma, Mucinous An adenocarcinoma producing mucin in significant amounts. (From Dorland, 27th ed) | 0 | 2.13 | 1 | 0 |
| Breast Cancer, Male [description not available] | 0 | 2.99 | 4 | 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 | 2.99 | 4 | 0 |
| Ache [description not available] | 0 | 8.53 | 33 | 13 |
| Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. | 0 | 8.53 | 33 | 13 |
| Age-Related Osteoporosis [description not available] | 0 | 11.93 | 29 | 13 |
| 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 | 11.93 | 29 | 13 |
| 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. | 0 | 19.25 | 48 | 17 |
| Cancer of the Vagina [description not available] | 0 | 3 | 1 | 0 |
| Vaginal Neoplasms Tumors or cancer of the VAGINA. | 0 | 3 | 1 | 0 |
| 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 | 2.08 | 1 | 0 |
| Innate Inflammatory Response [description not available] | 0 | 2.08 | 1 | 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 | 2.08 | 1 | 0 |
| Injuries, Radiation [description not available] | 0 | 6.63 | 7 | 1 |
| Cystitis Inflammation of the URINARY BLADDER, either from bacterial or non-bacterial causes. Cystitis is usually associated with painful urination (dysuria), increased frequency, urgency, and suprapubic pain. | 0 | 2.08 | 1 | 0 |
| Proctitis INFLAMMATION of the MUCOUS MEMBRANE of the RECTUM, the distal end of the large intestine (INTESTINE, LARGE). | 0 | 2.08 | 1 | 0 |
| Bleeding Between Periods [description not available] | 0 | 5.81 | 6 | 4 |
| 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 | 5.81 | 6 | 4 |
| Ovarian Diseases Pathological processes of the OVARY. | 0 | 6.26 | 10 | 4 |
| Low Bone Density [description not available] | 0 | 8.02 | 6 | 5 |
| Bone Diseases, Metabolic Diseases that affect the METABOLIC PROCESSES of BONE TISSUE. | 0 | 8.02 | 6 | 5 |
| Pain, Chronic [description not available] | 0 | 3.01 | 1 | 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 | 3.01 | 1 | 0 |
| Blood Loss, Surgical Loss of blood during a surgical procedure. | 0 | 6.49 | 7 | 7 |
| Cardiac Toxicity [description not available] | 0 | 2.1 | 1 | 0 |
| Cardiac Diseases [description not available] | 0 | 2.48 | 2 | 0 |
| Heart Diseases Pathological conditions involving the HEART including its structural and functional abnormalities. | 0 | 2.48 | 2 | 0 |
| Cardiotoxicity Damage to the HEART or its function secondary to exposure to toxic substances such as drugs used in CHEMOTHERAPY; IMMUNOTHERAPY; or RADIATION. | 0 | 2.1 | 1 | 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 | 3.82 | 2 | 1 |
| Cancer of Liver [description not available] | 0 | 5.67 | 5 | 4 |
| Liver Neoplasms Tumors or cancer of the LIVER. | 0 | 5.67 | 5 | 4 |
| Paraphilias [description not available] | 0 | 3.6 | 3 | 0 |
| Complications, Neoplastic Pregnancy [description not available] | 0 | 6.04 | 6 | 1 |
| 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 | 5.81 | 8 | 3 |
| Condition, Preneoplastic [description not available] | 0 | 3.8 | 2 | 1 |
| Cancer of Endometrium [description not available] | 0 | 6.94 | 10 | 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 | 10.81 | 8 | 3 |
| Precancerous Conditions Pathological conditions that tend eventually to become malignant. | 0 | 3.8 | 2 | 1 |
| 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 | 6.94 | 10 | 3 |
| 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 |
| Complications, Pregnancy [description not available] | 0 | 3.81 | 2 | 1 |
| Hemorrhagic Shock [description not available] | 0 | 7.1 | 1 | 0 |
| Hematoma A collection of blood outside the BLOOD VESSELS. Hematoma can be localized in an organ, space, or tissue. | 0 | 7.43 | 2 | 0 |
| Chronic Illness [description not available] | 0 | 6.88 | 7 | 4 |
| Autoimmune Disease [description not available] | 0 | 2.49 | 2 | 0 |
| Hives [description not available] | 0 | 2.11 | 1 | 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 | 2.49 | 2 | 0 |
| 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 | 6.88 | 7 | 4 |
| Urticaria A vascular reaction of the skin characterized by erythema and wheal formation due to localized increase of vascular permeability. The causative mechanism may be allergy, infection, or stress. | 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 | 2.11 | 1 | 0 |
| Adenoma, Prostatic [description not available] | 0 | 6.46 | 9 | 2 |
| 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 | 6.46 | 9 | 2 |
| Muscle Pain [description not available] | 0 | 2.13 | 1 | 0 |
| Hot Flashes A sudden, temporary sensation of heat predominantly experienced by some women during MENOPAUSE. (Random House Unabridged Dictionary, 2d ed) | 0 | 12.43 | 10 | 5 |
| Myalgia Painful sensation in the muscles. | 0 | 2.13 | 1 | 0 |
| Carcinoma, Lobular A type of BREAST CANCER where the abnormal malignant cells form in the lobules, or milk-producing glands, of the breast. | 1 | 4.97 | 4 | 0 |
| Thoracic Diseases Disorders affecting the organs of the thorax. | 0 | 2.13 | 1 | 0 |
| Hemopneumothorax Collection of air and blood in the pleural cavity. | 0 | 2.13 | 1 | 0 |
| Nycturia [description not available] | 0 | 3.09 | 1 | 0 |
| Nocturia Frequent URINATION at night that interrupts sleep. It is often associated with outflow obstruction, DIABETES MELLITUS, or bladder inflammation (CYSTITIS). | 0 | 3.09 | 1 | 0 |
| Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. | 0 | 3.7 | 10 | 0 |
| Lymphangiomyomatosis [description not available] | 0 | 3.8 | 2 | 0 |
| Pneumothorax, Primary Spontaneous [description not available] | 0 | 3.85 | 4 | 0 |
| 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 | 2.96 | 1 | 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 | 8.85 | 4 | 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 |
| 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 | 3.8 | 2 | 0 |
| Malignant Melanoma [description not available] | 0 | 2.43 | 2 | 0 |
| 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) | 0 | 2.43 | 2 | 0 |
| Central Hypothyroidism [description not available] | 0 | 2.04 | 1 | 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 | 2.04 | 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 | 7.04 | 1 | 0 |
| Diabetes Mellitus, Adult-Onset [description not available] | 0 | 5 | 3 | 1 |
| 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 | 5 | 3 | 1 |
| Cells, Neoplasm Circulating [description not available] | 0 | 3.8 | 2 | 1 |
| Neoplasms, Bone Marrow [description not available] | 0 | 2.04 | 1 | 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 | 2.04 | 1 | 0 |
| Anemia A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN. | 0 | 4.99 | 3 | 1 |
| Uveitis, Anterior Inflammation of the anterior uvea comprising the iris, angle structures, and the ciliary body. Manifestations of this disorder include ciliary injection, exudation into the anterior chamber, iris changes, and adhesions between the iris and lens (posterior synechiae). Intraocular pressure may be increased or reduced. | 0 | 2.04 | 1 | 0 |
| Amentia [description not available] | 0 | 2.05 | 1 | 0 |
| Dementia An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness. | 0 | 2.05 | 1 | 0 |
| Familial Precocious Puberty [description not available] | 0 | 7.3 | 15 | 1 |
| 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 | 7.3 | 15 | 1 |
| Weight Gain Increase in BODY WEIGHT over existing weight. | 0 | 2.44 | 2 | 0 |
| Blood Loss, Postoperative [description not available] | 0 | 4.41 | 2 | 2 |
| Idiopathic Parkinson Disease [description not available] | 0 | 2.96 | 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 | 2.96 | 1 | 0 |
| Endometrial Diseases [description not available] | 0 | 6.36 | 11 | 4 |
| Uterine Diseases Pathological processes involving any part of the UTERUS. | 0 | 6.36 | 11 | 4 |
| Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply. | 0 | 3.44 | 1 | 1 |
| Testicular Diseases Pathological processes of the TESTIS. | 0 | 2.05 | 1 | 0 |
| Alcohol Drinking Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking. | 0 | 2.44 | 2 | 0 |
| Carcinoma, Anaplastic [description not available] | 0 | 9.23 | 32 | 11 |
| 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 | 14.23 | 32 | 11 |
| Hematoma, Subdural, Cranial [description not available] | 0 | 2.05 | 1 | 0 |
| Leukocytopenia [description not available] | 0 | 2.05 | 1 | 0 |
| Leukopenia A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000). | 0 | 2.05 | 1 | 0 |
| Hematoma, Subdural, Intracranial Accumulation of blood in the SUBDURAL SPACE over the CEREBRAL HEMISPHERE. | 0 | 2.05 | 1 | 0 |
| Angiogenesis, Pathologic [description not available] | 0 | 4.09 | 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 | 2.01 | 1 | 0 |
| Dermatoses [description not available] | 0 | 3.35 | 2 | 0 |
| Cicatrix The fibrous tissue that replaces normal tissue during the process of WOUND HEALING. | 0 | 2.01 | 1 | 0 |
| Skin Diseases Diseases involving the DERMIS or EPIDERMIS. | 0 | 3.35 | 2 | 0 |
| Hypomenorrhea [description not available] | 0 | 4.17 | 6 | 0 |
| Granulomas [description not available] | 0 | 8.87 | 4 | 0 |
| Granuloma A relatively small nodular inflammatory lesion containing grouped mononuclear phagocytes, caused by infectious and noninfectious agents. | 0 | 8.87 | 4 | 0 |
| Frigidity [description not available] | 0 | 2.96 | 1 | 0 |
| 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 | 2.96 | 1 | 0 |
| Convulsions, Grand Mal [description not available] | 0 | 2.05 | 1 | 0 |
| Epilepsy, Tonic-Clonic A generalized seizure disorder characterized by recurrent major motor seizures. The initial brief tonic phase is marked by trunk flexion followed by diffuse extension of the trunk and extremities. The clonic phase features rhythmic flexor contractions of the trunk and limbs, pupillary dilation, elevations of blood pressure and pulse, urinary incontinence, and tongue biting. This is followed by a profound state of depressed consciousness (post-ictal state) which gradually improves over minutes to hours. The disorder may be cryptogenic, familial, or symptomatic (caused by an identified disease process). (From Adams et al., Principles of Neurology, 6th ed, p329) | 0 | 2.05 | 1 | 0 |
| Hypocalcemia Reduction of the blood calcium below normal. Manifestations include hyperactive deep tendon reflexes, Chvostek's sign, muscle and abdominal cramps, and carpopedal spasm. (Dorland, 27th ed) | 0 | 2.43 | 2 | 0 |
| Shingles [description not available] | 0 | 2.05 | 1 | 0 |
| Herpes Zoster An acute infectious, usually self-limited, disease believed to represent activation of latent varicella-zoster virus (HERPESVIRUS 3, HUMAN) in those who have been rendered partially immune after a previous attack of CHICKENPOX. It involves the SENSORY GANGLIA and their areas of innervation and is characterized by severe neuralgic pain along the distribution of the affected nerve and crops of clustered vesicles over the area. (From Dorland, 27th ed) | 0 | 2.05 | 1 | 0 |
| Apoplexy, Pituitary [description not available] | 0 | 2.93 | 4 | 0 |
| Multiple Primary Neoplasms [description not available] | 0 | 3.63 | 3 | 0 |
| Complication, Postoperative [description not available] | 0 | 5.96 | 5 | 2 |
| 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 | 5.96 | 5 | 2 |
| Congenital Thrombotic Thrombocytopenic Purpura [description not available] | 0 | 2.05 | 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 | 2.05 | 1 | 0 |
| Bone Fractures [description not available] | 0 | 13.69 | 30 | 25 |
| Fractures, Bone Breaks in bones. | 0 | 13.69 | 30 | 25 |
| Adenoma, Basal Cell [description not available] | 0 | 2.71 | 3 | 0 |
| Cancer of Pituitary [description not available] | 0 | 2.91 | 4 | 0 |
| Adenoma A benign epithelial tumor with a glandular organization. | 0 | 7.71 | 3 | 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 | 2.91 | 4 | 0 |
| Arthritis, Degenerative [description not available] | 0 | 3.45 | 1 | 1 |
| 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 | 3.45 | 1 | 1 |
| Anaphylactic Reaction [description not available] | 0 | 2.45 | 2 | 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 | 2.45 | 2 | 0 |
| Cardiometabolic Syndrome A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY. | 0 | 2.06 | 1 | 0 |
| 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. | 1 | 4.06 | 1 | 0 |
| Gestational Pemphigoid [description not available] | 0 | 2.06 | 1 | 0 |
| Carcinoma, Medullary A carcinoma composed mainly of epithelial elements with little or no stroma. Medullary carcinomas of the breast constitute 5%-7% of all mammary carcinomas; medullary carcinomas of the thyroid comprise 3%-10% of all thyroid malignancies. (From Dorland, 27th ed; DeVita Jr et al., Cancer: Principles & Practice of Oncology, 3d ed, p1141; Segen, Dictionary of Modern Medicine, 1992) | 0 | 2.06 | 1 | 0 |
| Corpus Luteum Cyst [description not available] | 0 | 5.04 | 5 | 2 |
| Ovarian Cysts General term for CYSTS and cystic diseases of the OVARY. | 0 | 5.04 | 5 | 2 |
| 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 | 11.06 | 8 | 4 |
| 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. | 0 | 9.09 | 3 | 1 |
| Dermatitis Medicamentosa [description not available] | 0 | 2.42 | 2 | 0 |
| Dermatitis, Radiation-Induced [description not available] | 0 | 2.43 | 2 | 0 |
| Radiodermatitis A cutaneous inflammatory reaction occurring as a result of exposure to ionizing radiation. | 0 | 2.43 | 2 | 0 |
| Soft Tissue Neoplasms Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc. | 0 | 2.07 | 1 | 0 |
| Reproductive Sterility [description not available] | 0 | 2.45 | 2 | 0 |
| Infertility A reduced or absent capacity to reproduce. | 1 | 4.45 | 2 | 0 |
| Carcinoma, Epidermoid [description not available] | 0 | 2.07 | 1 | 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 | 2.07 | 1 | 0 |
| Muscular Weakness [description not available] | 0 | 2.44 | 2 | 0 |
| Atrophy, Muscular, Spinobulbar [description not available] | 0 | 2.07 | 1 | 0 |
| 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 | 2.44 | 2 | 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 | 2.07 | 1 | 0 |
| Cancer, Radiation-Induced [description not available] | 0 | 2.07 | 1 | 0 |
| Cancer, Second Primary [description not available] | 0 | 3.85 | 4 | 0 |
| Female Genital Neoplasms [description not available] | 0 | 5.21 | 4 | 1 |
| Genital Neoplasms, Female Tumor or cancer of the female reproductive tract (GENITALIA, FEMALE). | 0 | 5.21 | 4 | 1 |
| Hypergonadotropic Hypogonadism [description not available] | 0 | 8.03 | 13 | 1 |
| 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). | 0 | 8.03 | 13 | 1 |
| Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment. | 0 | 5.93 | 3 | 3 |
| Femoral Fractures Fractures of the femur. | 0 | 2.41 | 2 | 0 |
| Fracture, Pathologic [description not available] | 0 | 2.7 | 3 | 0 |
| Hangman Fracture [description not available] | 0 | 2.42 | 2 | 0 |
| Spinal Fractures Broken bones in the vertebral column. | 0 | 2.42 | 2 | 0 |
| Bone Loss, Osteoclastic [description not available] | 0 | 8.96 | 11 | 8 |
| Compensatory Hyperinsulinemia A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin. | 0 | 4.31 | 1 | 1 |
| 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 | 4.31 | 1 | 1 |
| Drug Withdrawal Symptoms [description not available] | 0 | 4.48 | 5 | 0 |
| 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 | 4.48 | 5 | 0 |
| Abdominal Migraine [description not available] | 0 | 3.78 | 2 | 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 | 3.78 | 2 | 1 |
| Cholera Infantum [description not available] | 0 | 3.61 | 3 | 0 |
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 5.92 | 3 | 3 |
| Polycystic Ovarian Syndrome [description not available] | 0 | 7.64 | 11 | 6 |
| 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 | 7.64 | 11 | 6 |
| Androgenization [description not available] | 0 | 2.01 | 1 | 0 |
| Germinoblastoma [description not available] | 0 | 2.43 | 2 | 0 |
| Angiitis [description not available] | 0 | 2.01 | 1 | 0 |
| Lymphoma A general term for various neoplastic diseases of the lymphoid tissue. | 0 | 2.43 | 2 | 0 |
| Vasculitis Inflammation of any one of the blood vessels, including the ARTERIES; VEINS; and rest of the vasculature system in the body. | 0 | 2.01 | 1 | 0 |
| Encephalopathy, Hepatic [description not available] | 0 | 2.02 | 1 | 0 |
| Tumour Lysis Syndrome [description not available] | 0 | 2.02 | 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 | 2.02 | 1 | 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 | 2.02 | 1 | 0 |
| Cyst [description not available] | 0 | 2.02 | 1 | 0 |
| Genital Diseases, Male Pathological processes involving the male reproductive tract (GENITALIA, MALE). | 0 | 2.02 | 1 | 0 |
| Sex Disorders [description not available] | 0 | 6.14 | 4 | 3 |
| Sexual Dysfunction, Physiological Physiological disturbances in normal sexual performance in either the male or the female. | 0 | 6.14 | 4 | 3 |
| Blood Poisoning [description not available] | 0 | 2.02 | 1 | 0 |
| Acute Lymphoid Leukemia [description not available] | 0 | 2.4 | 2 | 0 |
| Neutropenia A decrease in the number of NEUTROPHILS found in the blood. | 0 | 2.02 | 1 | 0 |
| Sepsis Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK. | 0 | 2.02 | 1 | 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 | 2.4 | 2 | 0 |
| Dyskinesia, Medication-Induced [description not available] | 0 | 2.02 | 1 | 0 |
| Dyskinesia, Drug-Induced Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199) | 0 | 2.02 | 1 | 0 |
| Breast Diseases Pathological processes of the BREAST. | 0 | 4.29 | 4 | 1 |
| 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 | 4.09 | 3 | 1 |
| Vaginal Diseases Pathological processes of the VAGINA. | 0 | 2.02 | 1 | 0 |
| Leiomyomatosis The state of having multiple leiomyomas throughout the body. (Stedman, 25th ed) | 0 | 5.8 | 8 | 3 |
| Colorectal Cancer [description not available] | 0 | 2.02 | 1 | 0 |
| Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI. | 0 | 2.02 | 1 | 0 |
| Cushing's Syndrome [description not available] | 0 | 3.32 | 2 | 0 |
| 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 | 3.32 | 2 | 0 |
| Orbital Neoplasms Neoplasms of the bony orbit and contents except the eyeball. | 0 | 2.41 | 2 | 0 |
| Age-Related Memory Disorders [description not available] | 0 | 3.41 | 1 | 1 |
| Aprosodia [description not available] | 0 | 3.41 | 1 | 1 |
| 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 | 3.41 | 1 | 1 |
| Granuloma, Hodgkin [description not available] | 0 | 3.41 | 1 | 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. | 1 | 5.41 | 1 | 1 |
| Acute Confusional Senile Dementia [description not available] | 0 | 2.02 | 1 | 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 | 2.02 | 1 | 0 |
| Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57) | 0 | 2.02 | 1 | 0 |
| Male Genitourinary Diseases [description not available] | 0 | 2.02 | 1 | 0 |
| Cystadenocarcinoma, Serous A malignant cystic or semicystic neoplasm. It often occurs in the ovary and usually bilaterally. The external surface is usually covered with papillary excrescences. Microscopically, the papillary patterns are predominantly epithelial overgrowths with differentiated and undifferentiated papillary serous cystadenocarcinoma cells. Psammoma bodies may be present. The tumor generally adheres to surrounding structures and produces ascites. (From Hughes, Obstetric-Gynecologic Terminology, 1972, p185) | 0 | 3.41 | 1 | 1 |
| Bone Loss, Perimenopausal [description not available] | 0 | 5.96 | 5 | 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 | 5.96 | 5 | 2 |
| Affective Disorders, Psychotic Disorders in which the essential feature is a severe disturbance in mood (depression, anxiety, elation, and excitement) accompanied by psychotic symptoms such as delusions, hallucinations, gross impairment in reality testing, etc. | 0 | 2.03 | 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 |
| Autoimmune Thrombocytopenia [description not available] | 0 | 2.03 | 1 | 0 |
| Hemoperitoneum Accumulations of blood in the PERITONEAL CAVITY due to internal HEMORRHAGE. | 0 | 2.03 | 1 | 0 |
| Purpura, Thrombocytopenic, Idiopathic Thrombocytopenia occurring in the absence of toxic exposure or a disease associated with decreased platelets. It is mediated by immune mechanisms, in most cases IMMUNOGLOBULIN G autoantibodies which attach to platelets and subsequently undergo destruction by macrophages. The disease is seen in acute (affecting children) and chronic (adult) forms. | 0 | 2.03 | 1 | 0 |
| Abscess Accumulation of purulent material in tissues, organs, or circumscribed spaces, usually associated with signs of infection. | 0 | 2.4 | 2 | 0 |
| Adnexitis Inflammation of the uterine appendages (ADNEXA UTERI) including infection of the FALLOPIAN TUBES (SALPINGITIS), the ovaries (OOPHORITIS), or the supporting ligaments (PARAMETRITIS). | 0 | 3.79 | 2 | 1 |
| Pelvic Inflammatory Disease A spectrum of inflammation involving the female upper genital tract and the supporting tissues. It is usually caused by an ascending infection of organisms from the endocervix. Infection may be confined to the uterus (ENDOMETRITIS), the FALLOPIAN TUBES; (SALPINGITIS); the ovaries (OOPHORITIS), the supporting ligaments (PARAMETRITIS), or may involve several of the above uterine appendages. Such inflammation can lead to functional impairment and infertility. | 0 | 3.79 | 2 | 1 |
| Fistula Abnormal communication most commonly seen between two internal organs, or between an internal organ and the surface of the body. | 0 | 2.03 | 1 | 0 |
| Urinary Bladder Fistula An abnormal passage in the URINARY BLADDER or between the bladder and any surrounding organ. | 0 | 2.03 | 1 | 0 |
| Collagenous Fibroma [description not available] | 0 | 2.03 | 1 | 0 |
| Allergy, Drug [description not available] | 0 | 2.41 | 2 | 0 |
| Drug Hypersensitivity Immunologically mediated adverse reactions to medicinal substances used legally or illegally. | 0 | 2.41 | 2 | 0 |
| Cataract, Membranous [description not available] | 0 | 2.03 | 1 | 0 |
| Cataract Partial or complete opacity on or in the lens or capsule of one or both eyes, impairing vision or causing blindness. The many kinds of cataract are classified by their morphology (size, shape, location) or etiology (cause and time of occurrence). (Dorland, 27th ed) | 0 | 2.03 | 1 | 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 |
| Endometrial Stromal Sarcoma [description not available] | 0 | 3.63 | 3 | 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 | 3.63 | 3 | 0 |
| Placenta Increta Invasion of CHORIONIC VILLI occurs deep into the MYOMETRIUM. | 0 | 2.03 | 1 | 0 |
| Placenta Accreta Abnormal placentation in which all or parts of the PLACENTA are attached directly to the MYOMETRIUM due to a complete or partial absence of DECIDUA. It is associated with POSTPARTUM HEMORRHAGE because of the failure of placental separation. | 0 | 2.03 | 1 | 0 |
| Signet Ring Cell Carcinoma [description not available] | 0 | 2.03 | 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 | 2.03 | 1 | 0 |
| Left Ventricular Dysfunction [description not available] | 0 | 2.03 | 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 | 2.03 | 1 | 0 |
| Peritoneal Carcinomatosis [description not available] | 0 | 3.33 | 2 | 0 |
| Peritoneal Neoplasms Tumors or cancer of the PERITONEUM. | 0 | 3.33 | 2 | 0 |
| Anemias, Iron-Deficiency [description not available] | 0 | 4.36 | 2 | 2 |
| 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 | 4.36 | 2 | 2 |
| 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 | 2.03 | 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 | 2.03 | 1 | 0 |
| Hematologic Malignancies [description not available] | 0 | 3.43 | 1 | 1 |
| Graft-Versus-Host Disease [description not available] | 0 | 3.43 | 1 | 1 |
| 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 | 3.43 | 1 | 1 |
| 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 | 3.43 | 1 | 1 |
| Acute Myelogenous Leukemia [description not available] | 0 | 4.34 | 1 | 1 |
| Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES. | 0 | 4.34 | 1 | 1 |
| Chorea Disorders [description not available] | 0 | 2.04 | 1 | 0 |
| Chorea Involuntary, forcible, rapid, jerky movements that may be subtle or become confluent, markedly altering normal patterns of movement. Hypotonia and pendular reflexes are often associated. Conditions which feature recurrent or persistent episodes of chorea as a primary manifestation of disease are referred to as CHOREATIC DISORDERS. Chorea is also a frequent manifestation of BASAL GANGLIA DISEASES. | 0 | 2.04 | 1 | 0 |
| Androblastoma [description not available] | 0 | 1.96 | 1 | 0 |
| Experimental Neoplasms [description not available] | 0 | 2.66 | 3 | 0 |
| Experimental Mammary Neoplasms [description not available] | 0 | 4.96 | 9 | 0 |
| Cancer of Parotid [description not available] | 0 | 1.98 | 1 | 0 |
| Parotid Neoplasms Tumors or cancer of the PAROTID GLAND. | 0 | 1.98 | 1 | 0 |
| Acute Disease Disease having a short and relatively severe course. | 0 | 4.98 | 3 | 1 |
| Urinary Retention Inability to empty the URINARY BLADDER with voiding (URINATION). | 0 | 4.47 | 5 | 1 |
| Benign Chronic Pemphigus [description not available] | 0 | 1.98 | 1 | 0 |
| Chronic Kidney Failure [description not available] | 0 | 1.98 | 1 | 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 | 2.39 | 2 | 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 | 1.98 | 1 | 0 |
| Puerperal Disorders Disorders or diseases associated with PUERPERIUM, the six-to-eight-week period immediately after PARTURITION in humans. | 0 | 3.3 | 2 | 0 |
| Ovarian Hyperstimulation Syndrome, Familial Gestational Spontaneous [description not available] | 0 | 3.37 | 1 | 1 |
| 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 | 3.37 | 1 | 1 |
| 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 | 12.17 | 10 | 4 |
| 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 | 12.17 | 10 | 4 |
| Abortion, Recurrent [description not available] | 0 | 1.98 | 1 | 0 |
| Abortion, Habitual Three or more consecutive spontaneous abortions. | 0 | 1.98 | 1 | 0 |
| Adenosis of Breast [description not available] | 0 | 1.98 | 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 | 1.98 | 1 | 0 |
| Alveolitis, Fibrosing [description not available] | 0 | 1.98 | 1 | 0 |
| Cold Fingers, Hereditary [description not available] | 0 | 1.98 | 1 | 0 |
| Sclerosis, Systemic [description not available] | 0 | 1.98 | 1 | 0 |
| Pulmonary Fibrosis A process in which normal lung tissues are progressively replaced by FIBROBLASTS and COLLAGEN causing an irreversible loss of the ability to transfer oxygen into the bloodstream via PULMONARY ALVEOLI. Patients show progressive DYSPNEA finally resulting in death. | 0 | 1.98 | 1 | 0 |
| Raynaud Disease An idiopathic vascular disorder characterized by bilateral Raynaud phenomenon, the abrupt onset of digital paleness or CYANOSIS in response to cold exposure or stress. | 0 | 1.98 | 1 | 0 |
| Scleroderma, Systemic A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA. | 0 | 1.98 | 1 | 0 |
| Spinal Neoplasms New abnormal growth of tissue in the SPINE. | 0 | 1.98 | 1 | 0 |
| 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 | 4.98 | 3 | 1 |
| Female Genital Diseases [description not available] | 0 | 5.21 | 4 | 1 |
| Genital Diseases, Female Pathological processes involving the female reproductive tract (GENITALIA, FEMALE). | 0 | 5.21 | 4 | 1 |
| Mastitis INFLAMMATION of the BREAST, or MAMMARY GLAND. | 0 | 1.98 | 1 | 0 |
| Palmoplantaris Pustulosis [description not available] | 0 | 1.98 | 1 | 0 |
| Psoriasis Arthropathica [description not available] | 0 | 1.98 | 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 | 1.98 | 1 | 0 |
| Arthritis, Psoriatic A type of inflammatory arthritis associated with PSORIASIS, often involving the axial joints and the peripheral terminal interphalangeal joints. It is characterized by the presence of HLA-B27-associated SPONDYLARTHROPATHY, and the absence of rheumatoid factor. | 0 | 1.98 | 1 | 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 |
| Lymphangioleiomyoma [description not available] | 0 | 2.38 | 2 | 0 |
| Retroperitoneal Neoplasms New abnormal growth of tissue in the RETROPERITONEAL SPACE. | 0 | 1.98 | 1 | 0 |
| Fibromatosis [description not available] | 0 | 3.58 | 3 | 0 |
| Gardner Syndrome A variant of ADENOMATOUS POLYPOSIS COLI caused by mutation in the APC gene (GENES, APC) on CHROMOSOME 5. It is characterized by not only the presence of multiple colonic polyposis but also extracolonic ADENOMATOUS POLYPS in the UPPER GASTROINTESTINAL TRACT; the EYE; the SKIN; the SKULL; and the FACIAL BONES; as well as malignancy in organs other than the GI tract. | 0 | 1.98 | 1 | 0 |
| Fibroma A benign tumor of fibrous or fully developed connective tissue. | 0 | 3.58 | 3 | 0 |
| Anemia, Hypochromic Anemia characterized by a decrease in the ratio of the weight of hemoglobin to the volume of the erythrocyte, i.e., the mean corpuscular hemoglobin concentration is less than normal. The individual cells contain less hemoglobin than they could have under optimal conditions. Hypochromic anemia may be caused by iron deficiency from a low iron intake, diminished iron absorption, or excessive iron loss. It can also be caused by infections or other diseases, therapeutic drugs, lead poisoning, and other conditions. (Stedman, 25th ed; from Miale, Laboratory Medicine: Hematology, 6th ed, p393) | 0 | 4.06 | 3 | 1 |
| Cancer of Pancreas [description not available] | 0 | 5.94 | 5 | 2 |
| 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 | 5.94 | 5 | 2 |
| 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 | 1.98 | 1 | 0 |
| Dyspareunia Recurrent genital pain occurring during, before, or after SEXUAL INTERCOURSE in either the male or the female. | 0 | 3.37 | 1 | 1 |
| Bladder Neck Obstruction [description not available] | 0 | 3.78 | 2 | 1 |
| Metaplasia A condition in which there is a change of one adult cell type to another similar adult cell type. | 0 | 1.99 | 1 | 0 |
| Acne [description not available] | 0 | 3.78 | 2 | 1 |
| Acne Vulgaris A chronic disorder of the pilosebaceous apparatus associated with an increase in sebum secretion. It is characterized by open comedones (blackheads), closed comedones (whiteheads), and pustular nodules. The cause is unknown, but heredity and age are predisposing factors. | 0 | 3.78 | 2 | 1 |
| Bilateral Headache [description not available] | 0 | 3.37 | 1 | 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 | 3.37 | 1 | 1 |
| Emergencies Situations or conditions requiring immediate intervention to avoid serious adverse results. | 0 | 1.99 | 1 | 0 |
| Hyperlipemia [description not available] | 0 | 1.99 | 1 | 0 |
| Blood Pressure, High [description not available] | 0 | 1.99 | 1 | 0 |
| Hyperlipidemias Conditions with excess LIPIDS in the blood. | 0 | 1.99 | 1 | 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 | 1.99 | 1 | 0 |
| Cancer of Penis [description not available] | 0 | 1.99 | 1 | 0 |
| Penile Neoplasms Cancers or tumors of the PENIS or of its component tissues. | 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 |
| Neoplasms, Pleural [description not available] | 0 | 2.39 | 2 | 0 |
| Muscle Disorders [description not available] | 0 | 1.99 | 1 | 0 |
| Muscular Diseases Acquired, familial, and congenital disorders of SKELETAL MUSCLE and SMOOTH MUSCLE. | 0 | 1.99 | 1 | 0 |
| Hepatocellular Carcinoma [description not available] | 0 | 3.38 | 1 | 1 |
| 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 | 3.38 | 1 | 1 |
| Angina at Rest [description not available] | 0 | 1.99 | 1 | 0 |
| Angina, Unstable Precordial pain at rest, which may precede a MYOCARDIAL INFARCTION. | 0 | 1.99 | 1 | 0 |
| Chondromalacia Softening and degeneration of the CARTILAGE. | 0 | 1.99 | 1 | 0 |
| Polychondritis, Chronic Atrophic [description not available] | 0 | 1.99 | 1 | 0 |
| Petechiae Pinhead size (3 mm) skin discolorization due to hemorrhage. | 0 | 1.99 | 1 | 0 |
| Cartilage Diseases Pathological processes involving the chondral tissue (CARTILAGE). | 0 | 1.99 | 1 | 0 |
| Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes. | 0 | 1.99 | 1 | 0 |
| Polychondritis, Relapsing An acquired disease of unknown etiology, chronic course, and tendency to recur. It is characterized by inflammation and degeneration of cartilage and can result in deformities such as floppy ear and saddle nose. Loss of cartilage in the respiratory tract can lead to respiratory obstruction. | 0 | 1.99 | 1 | 0 |
| 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 | 1.99 | 1 | 0 |
| Leiomyoblastoma [description not available] | 0 | 1.99 | 1 | 0 |
| Canine Diseases [description not available] | 0 | 3.38 | 1 | 1 |
| Animal Mammary Carcinoma [description not available] | 0 | 3.79 | 2 | 1 |
| Acute Hepatic Failure [description not available] | 0 | 2 | 1 | 0 |
| Liver Failure, Acute A form of rapid-onset LIVER FAILURE, also known as fulminant hepatic failure, caused by severe liver injury or massive loss of HEPATOCYTES. It is characterized by sudden development of liver dysfunction and JAUNDICE. Acute liver failure may progress to exhibit cerebral dysfunction even HEPATIC COMA depending on the etiology that includes hepatic ISCHEMIA, drug toxicity, malignant infiltration, and viral hepatitis such as post-transfusion HEPATITIS B and HEPATITIS C. | 0 | 2 | 1 | 0 |
| Hamartoma A focal malformation resembling a neoplasm, composed of an overgrowth of mature cells and tissues that normally occur in the affected area. | 0 | 2 | 1 | 0 |
| Froehlich's Syndrome [description not available] | 0 | 2 | 1 | 0 |
| Neoplasms, Vascular [description not available] | 0 | 2 | 1 | 0 |
| Cardiac Cancer [description not available] | 0 | 2 | 1 | 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 | 2.41 | 2 | 0 |
| Asthma, Bronchial [description not available] | 0 | 2 | 1 | 0 |
| Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL). | 0 | 2 | 1 | 0 |
| Congenital Adrenal Hyperplasia [description not available] | 0 | 2 | 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 | 2 | 1 | 0 |
| Anemia, Hypoplastic [description not available] | 0 | 2.91 | 1 | 0 |
| Anemia, Aplastic A form of anemia in which the bone marrow fails to produce adequate numbers of peripheral blood elements. | 0 | 2.91 | 1 | 0 |
| Hypesthesia Absent or reduced sensitivity to cutaneous stimulation. | 0 | 2 | 1 | 0 |
| Symptom Cluster [description not available] | 0 | 2 | 1 | 0 |
| Syndrome A characteristic symptom complex. | 0 | 2 | 1 | 0 |
| Liver Dysfunction [description not available] | 0 | 2 | 1 | 0 |
| Liver Diseases Pathological processes of the LIVER. | 0 | 2 | 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 | 1 | 0 |
| Weight Reduction [description not available] | 0 | 2 | 1 | 0 |
| Antidiuretic Hormone, Inappropriate Secretion [description not available] | 0 | 2 | 1 | 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 | 2 | 1 | 0 |
| Weight Loss Decrease in existing BODY WEIGHT. | 0 | 2 | 1 | 0 |
| Intraepithelial Prostatic Neoplasia [description not available] | 0 | 2 | 1 | 0 |
| 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 | 2 | 1 | 0 |
| Cancer of Cervix [description not available] | 0 | 2 | 1 | 0 |
| Uterine Cervical Neoplasms Tumors or cancer of the UTERINE CERVIX. | 0 | 2 | 1 | 0 |
| Diseases of Endocrine System [description not available] | 0 | 2 | 1 | 0 |
| Endocrine System Diseases Pathological processes of the ENDOCRINE GLANDS, and diseases resulting from abnormal level of available HORMONES. | 0 | 2 | 1 | 0 |
| Cafe-au-Lait Spots with Pulmonic Stenosis [description not available] | 0 | 2 | 1 | 0 |
| Adult Optic Nerve Glioma [description not available] | 0 | 2 | 1 | 0 |
| Gigantism The condition of accelerated and excessive GROWTH in children or adolescents who are exposed to excess HUMAN GROWTH HORMONE before the closure of EPIPHYSES. It is usually caused by somatotroph hyperplasia or a GROWTH HORMONE-SECRETING PITUITARY ADENOMA. These patients are of abnormally tall stature, more than 3 standard deviations above normal mean height for age. | 0 | 2 | 1 | 0 |
| Neurofibromatosis 1 An autosomal dominant inherited disorder (with a high frequency of spontaneous mutations) that features developmental changes in the nervous system, muscles, bones, and skin, most notably in tissue derived from the embryonic NEURAL CREST. Multiple hyperpigmented skin lesions and subcutaneous tumors are the hallmark of this disease. Peripheral and central nervous system neoplasms occur frequently, especially OPTIC NERVE GLIOMA and NEUROFIBROSARCOMA. NF1 is caused by mutations which inactivate the NF1 gene (GENES, NEUROFIBROMATOSIS 1) on chromosome 17q. The incidence of learning disabilities is also elevated in this condition. (From Adams et al., Principles of Neurology, 6th ed, pp1014-18) There is overlap of clinical features with NOONAN SYNDROME in a syndrome called neurofibromatosis-Noonan syndrome. Both the PTPN11 and NF1 gene products are involved in the SIGNAL TRANSDUCTION pathway of Ras (RAS PROTEINS). | 0 | 2 | 1 | 0 |
| Optic Nerve Glioma Glial cell derived tumors arising from the optic nerve, usually presenting in childhood. | 0 | 2 | 1 | 0 |
| Ureteral Diseases Pathological processes involving the URETERS. | 0 | 2 | 1 | 0 |
| Disease, Pulmonary [description not available] | 0 | 2 | 1 | 0 |
| Lung Diseases Pathological processes involving any part of the LUNG. | 0 | 2 | 1 | 0 |
| Behavior Disorders [description not available] | 0 | 2.38 | 2 | 0 |
| 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 | 2.38 | 2 | 0 |
| Aura [description not available] | 0 | 1.98 | 1 | 0 |
| Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313) | 0 | 6.98 | 1 | 0 |
| Cancer of Colon [description not available] | 0 | 1.98 | 1 | 0 |
| Colonic Neoplasms Tumors or cancer of the COLON. | 0 | 1.98 | 1 | 0 |
| Feminization Development of female secondary SEX CHARACTERISTICS in the MALE. It is due to the effects of estrogenic metabolites of precursors from endogenous or exogenous sources, such as ADRENAL GLANDS or therapeutic drugs. | 0 | 1.98 | 1 | 0 |
| Flushing A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress. | 0 | 3.36 | 1 | 1 |
| Pemphigoid [description not available] | 0 | 6.98 | 1 | 0 |
| Pemphigoid, Bullous A chronic and relatively benign subepidermal blistering disease usually of the elderly and without histopathologic acantholysis. | 0 | 1.98 | 1 | 0 |
| Angor Pectoris [description not available] | 0 | 1.98 | 1 | 0 |
| Hyperidrosis [description not available] | 0 | 1.98 | 1 | 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 | 1.98 | 1 | 0 |
| Hyperhidrosis Excessive sweating. In the localized type, the most frequent sites are the palms, soles, axillae, inguinal folds, and the perineal area. Its chief cause is thought to be emotional. Generalized hyperhidrosis may be induced by a hot, humid environment, by fever, or by vigorous exercise. | 0 | 1.98 | 1 | 0 |
| Hyperplasia An increase in the number of cells in a tissue or organ without tumor formation. It differs from HYPERTROPHY, which is an increase in bulk without an increase in the number of cells. | 0 | 6.97 | 1 | 0 |
| Absence Status [description not available] | 0 | 1.97 | 1 | 0 |
| Status Epilepticus A prolonged seizure or seizures repeated frequently enough to prevent recovery between episodes occurring over a period of 20-30 minutes. The most common subtype is generalized tonic-clonic status epilepticus, a potentially fatal condition associated with neuronal injury and respiratory and metabolic dysfunction. Nonconvulsive forms include petit mal status and complex partial status, which may manifest as behavioral disturbances. Simple partial status epilepticus consists of persistent motor, sensory, or autonomic seizures that do not impair cognition (see also EPILEPSIA PARTIALIS CONTINUA). Subclinical status epilepticus generally refers to seizures occurring in an unresponsive or comatose individual in the absence of overt signs of seizure activity. (From N Engl J Med 1998 Apr 2;338(14):970-6; Neurologia 1997 Dec;12 Suppl 6:25-30) | 0 | 1.97 | 1 | 0 |
| Lymphangitis A lymphatic disease characterized by INFLAMMATION of LYMPHATIC VESSELS. | 0 | 1.97 | 1 | 0 |
| Cancer of Intestines [description not available] | 0 | 2.89 | 1 | 0 |
| Intestinal Neoplasms Tumors or cancer of the INTESTINES. | 0 | 2.89 | 1 | 0 |
| Bacteroides Infections Infections with bacteria of the genus BACTEROIDES. | 0 | 1.97 | 1 | 0 |
| Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill. | 0 | 3.36 | 1 | 1 |
| Atypical Ductal Hyperplasia [description not available] | 0 | 1.97 | 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 | 1.97 | 1 | 0 |
| Cruveilhier-Baumgarten Syndrome Liver cirrhosis with intrahepatic portal obstruction, HYPERTENSION, and patent UMBILICAL VEINS. | 0 | 1.97 | 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 | 1.97 | 1 | 0 |
| Pederasty [description not available] | 0 | 2.37 | 2 | 0 |
| Urinary Tract Diseases [description not available] | 0 | 1.96 | 1 | 0 |
| Osteolysis Dissolution of bone that particularly involves the removal or loss of calcium. | 0 | 1.97 | 1 | 0 |