| ID Source | ID |
|---|---|
| PubMed CID | 6918011 |
| CHEMBL ID | 1201185 |
| MeSH ID | M0167728 |
| Synonym |
|---|
| lanreotide acetate |
| ipstyl |
| dc 13-116 |
| lanreotide [inn:ban] |
| lanreotidum [inn-latin] |
| lanreotida [inn-spanish] |
| l-threoninamide, 3-(2-naphthalenyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-, cyclic (2-7)-disulfide |
| autogel |
| bim 23014 |
| nal-cyclo(cys-tyr-trp-lys-val-cys)-thr-nh2 |
| somatulin |
| l-threoninamide, 3-(1-naphthalenyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-, cyclic (2-7)-disulfide |
| CHEMBL1201185 |
| (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-n-[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2r)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-p |
| naphthalenyl-cyclo(cysteinyl-tyrosyl-tryptophyl-lysyl-valyl-cysteinyl)threoninamide |
| naphthyl-cyclo(cys-tyr-trp-lys-val-cys)thr-nh2 |
| nal-cyclo(cys-tyr-trp-lys-val-cys)thr-nh2 |
| 118992-92-0 |
| 2-naphthylalanyl-cyclo(cysteinyl-tyrosyl-tryptophyl-lysyl-valyl-cysteinyl)-threoninamide |
| bdbm82470 |
| 3-(2-naphtyl)-d-ala-l-cys(1)-l-tyr-d-trp-l-lys-l-val-l-cys(1)-l-thr-nh2 |
| somatulin-autogel |
| unii-0g3de8943y |
| lanreotide autogel |
| lanreotida |
| 0g3de8943y , |
| lanreotidum |
| AKOS030573447 |
| l-threoninamide, 3-(2-naphthalenyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-, cyclic (2->7)-disulfide |
| l-threoninamide, 3-(2-naphthalenyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-, cyclic (2->7)-disulphide |
| 3-(2-naphthyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-l-threoninamide, cyclic (2->7)-disulfide |
| 3-(2-naphthyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-l-threoninamide, cyclic (2->7)-disulphide |
| DTXSID60897514 , |
| (4r,7s,10s,13r,16s,19r)-13-((1h-indol-3-yl)methyl)-19-((r)-2-amino-3-(naphthalen-2-yl)propanamido)-n-((2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl)-10-(4-aminobutyl)-16-(4-hydroxybenzyl)-7-isopropyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacyclo |
| Q1707877 |
| l-threoninamide, 3-(2-naphthalenyl)-d-alanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-valyl-l-cysteinyl-, cyclic (2-->7)-disulfide |
| 108736-35-2 (free base) |
| C71317 |
| CS-0103335 |
| HY-P1959 |
| dtxcid601326869 |
| lanreotidum (inn-latin) |
| dc 13116 |
| dermopeptin |
| h01cb03 |
| lanreotide (mart.) |
| lanreotida (inn-spanish) |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Somatostatin receptor type 1 | Homo sapiens (human) | Ki | 0.5012 | 0.0003 | 0.4123 | 2.3920 | AID203390 |
| Somatostatin receptor type 2 | Homo sapiens (human) | Ki | 0.0005 | 0.0000 | 0.4091 | 4.7200 | AID203409 |
| Somatostatin receptor type 4 | Homo sapiens (human) | Ki | 1.0000 | 0.0006 | 0.2733 | 3.2000 | AID203570 |
| Somatostatin receptor type 3 | Homo sapiens (human) | Ki | 0.0631 | 0.0001 | 0.0320 | 0.1290 | AID203551 |
| Somatostatin receptor type 5 | Homo sapiens (human) | Ki | 0.0040 | 0.0001 | 0.4479 | 4.0700 | AID203709 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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] | |||
| 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). |
| 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). |
| 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). |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' 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). |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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). |
| 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). |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID203409 | Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
| 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). |
| AID203551 | Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
| 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). |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| 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] | |||
| AID203709 | Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
| 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 | |||
| AID203570 | Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
| 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] | |||
| AID203390 | Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells | 2003 | Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12 | A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' 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). |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| 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] | |||
| 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] | |||
| 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). |
| AID195175 | In vitro GH release inhibiting potency on anterior pitutaries from adult male rats, relative to somatostatin | 1995 | Journal of medicinal chemistry, May-26, Volume: 38, Issue:11 | Three-dimensional quantitative structure-activity relationships of somatostatin analogues. 1. Comparative molecular field analysis of growth hormone release-inhibiting potencies. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' 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). |
| 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). |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' 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 | 0 (0.00) | 18.7374 |
| 1990's | 1 (25.00) | 18.2507 |
| 2000's | 1 (25.00) | 29.6817 |
| 2010's | 2 (50.00) | 24.3611 |
| 2020's | 0 (0.00) | 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 (75.54) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 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 | ||
|---|---|---|---|---|---|---|---|
| Long-Acting Lanreotide as a Volume Reducing Treatment of Polycystic Livers [NCT00565097] | Phase 2/Phase 3 | 38 participants (Anticipated) | Interventional | 2007-10-31 | Completed | ||
| Continuing Somatostatin Analogues Upon Progression in Neuroendocrine Tumour pAtients - The SAUNA Trial [NCT05701241] | Phase 4 | 270 participants (Anticipated) | Interventional | 2023-06-28 | Recruiting | ||
| The Longitudinal Approach to Acromegaly: A Pattern of Treatment and Comparative Effectiveness Research [NCT03158090] | 1,965 participants (Anticipated) | Observational | 2017-12-15 | Recruiting | |||
| Traitement Des Carcinomes à Cellules de Merkel inopérables et/ou métastatiques Par Analogue de la Somatostatine - Etude Nationale Multicentrique Mono-bras de Phase II. [NCT02351128] | Phase 2 | 35 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| A Prospective, Randomized Trial of Preoperative Lanreotide Treatment in Acromegalic Patients With Macroadenomas [NCT00993356] | Phase 2 | 96 participants (Anticipated) | Interventional | 2004-01-31 | Recruiting | ||
| Comparison of Combination Low-Dose SRL + Daily Pegvisomant Therapy, Low-Dose SRL + Weekly Pegvisomant Therapy, and High-Dose SRL + Weekly Pegvisomant Therapy [NCT01538966] | 76 participants (Actual) | Interventional | 2012-03-29 | Terminated(stopped due to Review of the 12-month data showed patients who deviated from protocol with full IRB monitoring and reporting could not be optimally analyzed. Reopening the study for new enrollment is not feasible and the study was terminated with IRB approval.) | |||
| An Open-label, Phase II Clinical Study to Evaluate the Efficacy and Safety of Lanreotide Autogel 90mg Every 4 Weeks in the Treatment of Symptomatic Polycystic Liver Disease, Including a Dose Escalation at Month 6 to Lanreotide Autogel 120mg for Non Respon [NCT01315795] | Phase 2/Phase 3 | 59 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| The Effect of Lanreotide on Volume of Polycystic Liver and Kidney in Autosomal Dominant Polycystic Kidney Disease [NCT01354405] | 43 participants (Actual) | Observational | 2011-05-31 | Completed | |||
| Open Label Extension Study of Lanreotide Autogel 120 mg in Patients With Non-functioning Entero-pancreatic Endocrine Tumour [NCT00842348] | Phase 3 | 89 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| Influence of Somatuline Autogel 120mg on Post-operative Drainage After Total Mesorectum Excision for Rectumcarcinoma [NCT01372007] | Phase 3 | 24 participants (Actual) | Interventional | 2011-07-31 | Completed | ||
| A Phase 3, Prospective, Randomized, Double-blind, Multi-center Study of the Efficacy and Safety of Lanreotide Autogel®/Depot 120 mg Plus BSC vs. Placebo Plus BSC for Tumour Control in Subjects With Well Differentiated, Metastatic and/or Unresectable, Typi [NCT02683941] | Phase 3 | 77 participants (Actual) | Interventional | 2017-03-06 | Terminated(stopped due to National Comprehensive Cancer Network & European Neuroendocrine Tumor Society guidelines (2015/2016) led to prescription of somatostatin analogues (SSAs) in this setting, thereby limiting recruitment.) | ||
| A Multicenter, Open, Prospective, Observational Study to Investigate the Effect of Lanreotide Autogel 120 mg on Control of GH and IGF-I Excess and Tumor Shrinkage in Newly Diagnosed Patients With Acromegaly [NCT00627796] | Phase 4 | 27 participants (Actual) | Interventional | 2003-01-31 | Completed | ||
| Evaluation of Lanreotide Efficacity in High Output Stoma: a Multicentric Randomized Study [NCT02354768] | Phase 3 | 19 participants (Actual) | Interventional | 2015-10-22 | Terminated | ||
| A Phase II Trial of Lanreotide for the Prevention of Postoperative Pancreatic Fistula [NCT03174353] | Phase 2 | 114 participants (Actual) | Interventional | 2018-02-20 | Completed | ||
| Open-Label Extension of the LOCKCYST Trial, LOCKCYST: Long Acting Lnareotide as as Volume Reducing Treatment of Polycystic Livers [NCT00771888] | Phase 2/Phase 3 | 54 participants (Anticipated) | Interventional | 2008-04-30 | Active, not recruiting | ||
| Phase II, Multicentre, Open Label Study to Evaluate the Efficacy of the Combination of Lanreotide Autogel 120mg and Temozolomide in Patients With Progressive Gastro-entero-pancreatic Neuroendocrine Tumours (GEP-NET) G1/G2 - A Pilot-Study [NCT02231762] | Phase 2 | 57 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
| Phase III, Randomised, Double-blind, Stratified Comparative, Placebo Controlled, Parallel Group, Multi-centre Study to Assess the Effect of Deep Subcutaneous Injections of Lanreotide Autogel 120mg Administered Every 28 Days on Tumour Progression Free Surv [NCT00353496] | Phase 3 | 264 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Resolving Bile Reflux by Lanreotide in Patients With Roux-en-Y Gastrojejunostomy [NCT02054637] | Phase 2 | 10 participants (Anticipated) | Interventional | 2014-04-30 | Not yet recruiting | ||
| Exploratory Phase II Study of LAnreotide in Metastatic Pheochromocytoma/PARAganglioma (LAMPARA) [NCT03946527] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-06-17 | Recruiting | ||
| Randomised, Phase III Multicenter, Open Study of Lanreotide in Non Metastatic Castration-resistant Prostate Cancer Patients Presenting Elevated Chromogranin A Levels [NCT01313273] | Phase 3 | 3 participants (Actual) | Interventional | 2011-06-30 | Terminated(stopped due to Poor enrolment) | ||
| A Phase III Multicentre Randomised Double-blind Comparative Study of Efficacy and Safety of Lanreotide 30 mg Versus Placebo for Treatment of Patients With Digestive Fistulae [NCT00729313] | Phase 3 | 111 participants (Actual) | Interventional | 2000-04-30 | Completed | ||
| A Phase IV, International, Open-label, Randomised, Cross-over Study to Assess Patient Preference and Health Economy in Patients With Neuroendocrine Tumours, Treated With Lanreotide Autogel Given as Self Administration. [NCT00681187] | Phase 4 | 26 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Evaluation of the Efficacity of Lanreotide LP 90 mg to Minimized the Lymphorrhea Post Axillary Lymphadenectomy in Breast Cancer [NCT00630695] | Phase 3 | 148 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
| Lanreotide In Polycystic Kidney Disease Study [NCT02127437] | Phase 3 | 159 participants (Actual) | Interventional | 2014-09-19 | Completed | ||
| Prospective Study to Assess the Efficacy and Safety of Lanreotide 120 mg as a Palliative Treatment of Clinical Symptoms Associated With Malignant Intestinal Obstruction in Inoperable Patients [NCT01076803] | Phase 2 | 40 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
| Phase 1b/3 Global, Randomized, Controlled, Open-label Trial Comparing Treatment With RYZ101 to Standard of Care Therapy in Subjects With Inoperable, Advanced, SSTR+, Well-differentiated GEP-NETs That Have Progressed Following Prior 177Lu-SSA Therapy [NCT05477576] | Phase 3 | 288 participants (Anticipated) | Interventional | 2022-03-24 | Recruiting | ||
| A Phase II-III, Multicentre, Prospective, Exploratory, Open Label Study to Assess the Efficacy and Safety of Lanreotide Autogel 120mg in the Symptomatic Treatment of Patients With Refractory Diarrhea [NCT00891371] | Phase 2/Phase 3 | 42 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| A Phase 1b Study in Patients With Acromegaly or Functioning Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs) to Characterize the Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Debio 4126, a 12-week Prolonged-release Octreotide Formu [NCT05364944] | Phase 1 | 30 participants (Anticipated) | Interventional | 2022-05-18 | Active, not recruiting | ||
| A Phase II Study of Lanreotide in Patients With Metastatic Gastrointestinal Neuroendocrine Tumors Undergoing Liver-directed Radioembolization With Yttrium-90 Microspheres (SIR-Spheres®) [NCT02859064] | Phase 2 | 6 participants (Actual) | Interventional | 2017-07-28 | Terminated(stopped due to Closed due to slow accrual) | ||
| Impact of Somatostatin Analogs vs. Surgery on Glucose Metabolism in Acromegaly: Results of a 5 Years Observational, Open, Prospective Study [NCT00703079] | 100 participants (Actual) | Observational | 1997-01-31 | Completed | |||
| Co-treatment With Pegvisomant and a Somatostatin Analogue (SA) in SA-responsive Acromegalic Patients: Impact on Insulin Sensitivity, Glucose Tolerance, and Pharmacoeconomics [NCT00652379] | 18 participants (Actual) | Interventional | 2008-06-30 | Completed | |||
| Randomized Phase III Clinical Trial of Lanreotide Combined With Telotristat Ethyl or Placebo for the First-line Treatment in Patients With Advanced Well Differentiated Small Intestinal Neuroendocrine Tumours (siNET) With Highly-functioning Carcinoid Syndr [NCT04065165] | Phase 3 | 0 participants (Actual) | Interventional | 2020-04-30 | Withdrawn(stopped due to Company decision) | ||
| A Multi Center Open Label Study to Assess the Ability of Subjects With Acromegaly or Their Partners to Administer Somatuline Autogel [NCT00447499] | Phase 3 | 59 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| Phase IIIb, Multicentre, Open-label, Single-arm, Study to Assess the Efficacy and Safety of Lanreotide Autogel 120 mg Administered Every 28 Days as Primary Medical Treatment in Acromegalic Patients With Macroadenoma [NCT00690898] | Phase 3 | 108 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| A Phase I/II Study Using Cabozantinib and Lanreotide as Treatment for Advanced Gastroenteropancreatic Neuroendocrine Tumors That Failed Molecular Targeted Therapies or Chemotherapy (SCALET) [NCT05048901] | Phase 1/Phase 2 | 49 participants (Anticipated) | Interventional | 2021-09-17 | Recruiting | ||
| A Double Blind, Randomized Placebo Controlled Clinical Trial Investigating the Efficacy and Safety of Somatuline Depot (Lanreotide) Injection in the Treatment of Carcinoid Syndrome [NCT00774930] | Phase 3 | 115 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| Phase II, Multicentre, Randomized, Double-blind Study in Acromegalic Patients Evaluating the Efficacy and Safety of a Single Deep Subcutaneous Administration of Lanreotide Autogel (60, 90 or 120mg) Versus Placebo Followed by a Single Blind Fixed Dose Phas [NCT00234572] | Phase 2/Phase 3 | 108 participants (Actual) | Interventional | 2000-05-31 | Completed | ||
| Treatment With Lanreotide Autogel (Somatostatin Analogue) in Patients With Congenital Hyperinsulinism of Infancy Already Treated With Somatostatin Analog by Pump [NCT01070758] | Phase 4 | 10 participants (Anticipated) | Interventional | 2010-02-28 | Recruiting | ||
| Phase III, Multicentre, Open Study to Assess the Efficacy and Safety Profiles of the Co-administration of Lanreotide Autogel 120 mg (Administered Via Deep Subcutaneous Injections Every 28 Days) and Pegvisomant 40 to 120 mg Per Week (Administered Via Subcu [NCT00383708] | Phase 3 | 125 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| A Phase IV, Open-label, Single Group Study to Evaluate the Dosing, Efficacy and Safety of Lanreotide Autogel® in Patients With Acromegaly Previously Treated With Octreotide LAR [NCT00216398] | Phase 4 | 8 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
| Non-interventional, Observational, Long Term Study to Evaluate Common Therapeutic Algorithms and Possible Predictive Parameters for Somatuline Autogel (ATG) Treatment in Patients With Acromegaly. [NCT02020499] | 5 participants (Actual) | Observational | 2014-08-31 | Terminated(stopped due to Poor enrolment) | |||
| A Phase III, Multicenter, Randomized, Parallel-group Study to Assess the Efficacy and Safety of Double-blind Pasireotide LAR 40 mg and Pasireotide LAR 60 mg Versus Open-label Octreotide LAR or Lanreotide ATG in Patients With Inadequately Controlled Acrome [NCT01137682] | Phase 3 | 198 participants (Actual) | Interventional | 2010-07-19 | Completed | ||
| An Open-Label Extension Trial of IONIS GHR-LRx, an Antisense Inhibitor of the Growth Hormone Receptor Administered Monthly Subcutaneously to Patients With Acromegaly Being Treated With Long-Acting Somatostatin Receptor Ligands (SRL) [NCT03967249] | Phase 2 | 39 participants (Actual) | Interventional | 2019-07-25 | Completed | ||
| Safety of Lanreotide 120 mg ATG in Combination With Metformin in Patients With Progressive Advanced Well-differentiated Gastro-intestinal (GI) or Lung Carcinoids: A Pilot, One-arm, Open-label, Prospective Study: the MetNET-2 Trial [NCT02823691] | Early Phase 1 | 20 participants (Actual) | Interventional | 2016-04-30 | Active, not recruiting | ||
| Treatment of the Dumping Syndrome With Lanreotide Autogel® [NCT00543179] | Phase 4 | 0 participants | Interventional | 2007-10-31 | Recruiting | ||
| A Phase III, Prospective, Multicenter, Randomized, Open, Parallel Group Comparison of Lanreotide Autogel® (90 and 120 mg) Administered by Deep Subcutaneous Injection Every Four Weeks, With Sandostatin LAR Depot (20 and 30 mg) Administered by Intramuscular [NCT00092287] | Phase 3 | 4 participants (Actual) | Interventional | 2004-07-31 | Terminated | ||
| A Pilot Study to Evaluate Safety and Effectiveness of Lanreotide in the Treatment of Patients With Small Bowel Motility Disorders (SBMD): a Prospective, Non-randomized, Single-center Study of 20 Participants [NCT03012594] | Phase 2 | 12 participants (Actual) | Interventional | 2017-05-11 | Completed | ||
| A Phase IV, Multicentre, Open Label, Controlled Study to Assess the Ability of Patients With Acromegaly, or Their Partners, to Administer Somatuline Autogel. [NCT00149188] | Phase 4 | 30 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
| A EUROPEAN, MULTICENTRE, PHASE II/III RANDOMISED DOUBLE-BLIND, PLACEBO CONTROLLED STUDY EVALUATING LANREOTIDE AS MAINTENANCE THERAPY IN PATIENTS WITH NON-RESECTABLE DUODENO-PANCREATIC NEUROENDOCRINE TUMOURS AFTER FIRST-LINE TREATMENT [NCT02288377] | Phase 2/Phase 3 | 53 participants (Actual) | Interventional | 2015-01-31 | Terminated(stopped due to Because of slow recruitment) | ||
| Prospective Observational Study to Assess the Effectiveness and Safety of Lanreotide Autogel® in Patients With Locally Advanced or Metastatic Gastroenteropancreatic Neuroendocrine Tumors (GEP-NETs) in Asia Region [NCT04696042] | 95 participants (Anticipated) | Observational [Patient Registry] | 2021-01-01 | Recruiting | |||
| Phase III, Multicentre, Open Clinical Study on the Efficacy and Tolerability of a New Slow-release Formulation of Lanreotide (Autogel 120 mg) in Patients With Active Acromegaly [NCT00499993] | Phase 3 | 63 participants (Actual) | Interventional | 2001-01-31 | Completed | ||
| Circulating Tumor Cells and Tumor DNA in HCC and NET - Patient-specific Biomarkers for Clinical Decision Support and Tailored Relapse Diagnostics [NCT02973204] | 167 participants (Actual) | Observational [Patient Registry] | 2016-11-30 | Completed | |||
| Phase III, Multicentre, Randomised, Double-blind, Comparative Study to Assess the Efficacy and Safety of Lanreotide 30 mg Versus Placebo as a Palliative Treatment of Clinical Symptoms Associated With Intestinal Obstruction Due to Peritoneal Carcinomatosis [NCT00216372] | Phase 3 | 80 participants (Actual) | Interventional | 2003-09-30 | Completed | ||
| A Phase III, Multicentre, Open Label, Comparative, Dose-interval Titration Study Evaluating the Efficacy and Safety of Six Repeated Deep Subcutaneous Administrations of Lanreotide Autogel 120mg, in Acromegalic Patients Previously Treated With Octreotide L [NCT00444873] | Phase 3 | 38 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
| Treatment of Advanced Hepatocellular Carcinoma With Depot Somatostatin Analogues: a Pilot Prospective Study Based on Somatostatin Receptors Tumors Expression [NCT00495846] | Phase 2/Phase 3 | 25 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| A Pilot Study to Evaluate the Correlation Between Plasma Lanreotide Levels and GH/IGF-1 Dynamics and Clinical Improvement in Patients With Acromegaly Treated With Lanreotide Autogel (Somatuline ATG) [NCT00517491] | Phase 2 | 0 participants (Actual) | Interventional | 2008-05-31 | Withdrawn(stopped due to Administrative reasons) | ||
| Phase III, Multicentre, Open Study to Assess the Efficacy and Safety of Lanreotide Autogel (60, 90 or 120 mg) in Acromegalic Patients Previously Treated or Not by Somatostatin Analogues. [NCT00210457] | Phase 3 | 63 participants (Actual) | Interventional | 2000-09-30 | Completed | ||
| Comparable Effects of Lanreotide Autogel and Octreotide LAR on GH, IGF-I Levels and Patient Satisfaction - A Twelve Month Randomized Cross-Over Study in Patients With Acromegaly [NCT00145405] | Phase 4 | 12 participants | Interventional | 2002-09-30 | Completed | ||
| A Phase II Trial Aiming to Assess the Safety and Activity of the Combination of Cabozantinib Plus Lanreotide in Gastroenteropancreatic (GEP) and Thoracic Neuroendocrine Tumor (NET): The LOLA Trial [NCT04427787] | Phase 2 | 69 participants (Anticipated) | Interventional | 2020-06-20 | Recruiting | ||
| PILOT STUDY OF LANREOTIDE IN METASTATIC OR RECURRENT GRADE I-II HINDGUT NET [NCT03083210] | Phase 4 | 28 participants (Anticipated) | Interventional | 2017-07-05 | Recruiting | ||
| A Phase II, Single Centre, Randomized, Double-blind, Parallel and Placebo Controlled, Pilot Study to Evaluate the Efficacy and Safety of Somatuline Autogel 60mg in Patients With Active Thyroid-associated Ophthalmopathy of Moderate Intensity. [NCT00288522] | Phase 2 | 5 participants (Actual) | Interventional | 2006-01-31 | Terminated | ||
| Phase II, Open, Single Group, Multicentre Study to Evaluate the Efficacy and Safety of Lanreotide Autogel Administered Every 4 Weeks by Deep Subcutaneous Injection in the Tumour's Growth Stabilization of Patients With Progressive Neuroendocrine Tumours Wh [NCT00326469] | Phase 2 | 30 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
| A Randomized, Multi-center, Open-label, Active-controlled Phase 3 Trial to Assess the Efficacy and Safety of Octreotide Subcutaneous Depot (CAM2029) Versus Octreotide LAR or Lanreotide ATG in Patients With GEP-NET [NCT05050942] | Phase 3 | 300 participants (Anticipated) | Interventional | 2021-10-22 | Recruiting | ||
| A RANDOMIZED PHASE II DOUBLE-BLIND TRIAL OF SUNITINIB VERSUS PLACEBO IN COMBINATION WITH LANREOTIDE IN PATIENTS WITH PROGRESSIVE ADVANCED/METASTATIC MIDGUT CARCINOID TUMORS [NCT01731925] | Phase 2 | 44 participants (Actual) | Interventional | 2013-01-07 | Active, not recruiting | ||
| A Prospective, International, Multi-centric, Open-label Study to Assess the Efficacy of an Extended Injection Interval Schedule of Lanreotide Autogel 120 mg in Acromegalic Subjects Who Are Biochemically Controlled on the Long Term Treatment With Octreotid [NCT00701363] | Phase 4 | 124 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
| Non-interventional, Observational Study to Evaluate Common Therapeutic Algorithms and Possible Predictive Parameters for Somatuline Autogel® (ATG) Treatment in Subjects With Either Acromegaly or Neuroendocrine Tumours (NET) [NCT01840449] | 156 participants (Actual) | Observational | 2012-06-30 | Completed | |||
| A Phase II, Multicentre, Randomized Controlled Study Evaluating The Quality Of Life In Patients With Inoperable Malignant Bowel Obstruction Treated With Lanreotide Autogel 120 mg in Combination With Standard Care vs. Standard Care Alone (QOL IN IMBO STUDY [NCT02365584] | Phase 2 | 43 participants (Actual) | Interventional | 2015-01-31 | Terminated(stopped due to The study was terminated early due to insufficient recruitment.) | ||
| An International, Multicentric, Prospective, Open Label Study to Assess the Efficacy and Safety of Lanreotide Autogel 120 MG Associated to Standard of Care in the Treatment of Clinical Symptoms Associated With Inoperable Malignant Intestinal Obstruction [NCT02275338] | Phase 2 | 52 participants (Actual) | Interventional | 2014-11-19 | Completed | ||
| A Phase II Study of Ramucirumab With Somatostatin Analog Therapy in Patients With Advanced, Progressive Carcinoid Tumors [NCT02795858] | Phase 2 | 44 participants (Actual) | Interventional | 2016-06-14 | Active, not recruiting | ||
| A Phase 3, Single-arm, Open-label, Multicentre Study to Assess the Efficacy and Safety of Deep Subcutaneous Injections of Lanreotide Autogel® 120 mg Administered Every 28 Days in Chinese Participants With Unresectable, Locally Advanced or Metastatic Grade [NCT04852679] | Phase 3 | 43 participants (Actual) | Interventional | 2021-05-24 | Completed | ||
| The DIPAK 1 Study: A Randomised, Controlled Clinical Trial Assessing the Efficacy of Lanreotide to Halt Disease Progression in ADPKD [NCT01616927] | Phase 3 | 300 participants (Anticipated) | Interventional | 2012-06-30 | Active, not recruiting | ||
| Phase IIa, Open Label, Dose Ascending Study to Determine the Maximum Tolerated Dose, Safety and Tolerability, Pharmacokinetics and Pharmacodynamics of a Single Dose of Lanreotide PRF in Subjects With Acromegaly Previously Treated and Controlled With Eithe [NCT02396953] | Phase 1/Phase 2 | 28 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
| Phase Ib/II Study of Pembrolizumab With Lanreotide Depot for Gastroenteropancreatic Neuroendocrine Tumors [NCT03043664] | Phase 1/Phase 2 | 22 participants (Actual) | Interventional | 2017-07-01 | Completed | ||
| A Pilot Study To Evaluate Patient Experience With the Somatostatin Analogs Octreotide Long Acting Release and Lanreotide During the Treatment of Advanced, Nonfunctional, Well Differentiated Neuroendocrine Tumors [NCT03289741] | Phase 4 | 53 participants (Actual) | Interventional | 2017-09-19 | Completed | ||
| Efficacy and Safety of Lanreotide Autogel® 120 mg Administered Every 14 Days in Well Differentiated, Metastatic or Locally Advanced, Unresectable Pancreatic or Midgut Neuroendocrine Tumours Having Progressed Radiologically While Previously Treated With La [NCT02651987] | Phase 2 | 99 participants (Actual) | Interventional | 2015-12-15 | Completed | ||
| A Phase III, Prospective, Randomised, Open Label Study to Compare the Efficacy and Safety of Lanreotide Autogel® 60, 90 or 120 mg With Lanreotide 40 mg PR in Subjects With Active Acromegaly [NCT02493517] | Phase 3 | 128 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
| A Pilot Study of Pre- and Post-operative Somatuline Depot Therapy in Acromegalic Patients Treated by Endonasal Endoscopic Surgery: Impact on Early Remission Rates and Perioperative Morbidity [NCT01861717] | Phase 4 | 4 participants (Actual) | Interventional | 2013-05-31 | Terminated(stopped due to Didn't enroll enough subjects) | ||
| SOMATULINE Autogel 90 mg IN DUMPING SYNDROME [NCT01923649] | Phase 2 | 24 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Multicenter Evaluation of the Effect of Upfront Radiosurgery on Residual Growth Hormone-secreting Pituitary Adenoma From an Endocrinological Point of View (MERGE Study): a Randomized, Phase 3 Trial [NCT03439709] | Phase 3 | 90 participants (Anticipated) | Interventional | 2018-03-01 | Not yet recruiting | ||
| A Phase IV, Multicentre, Open Label, Single Group Exploratory Study to Assess the Clinical Value of Enumeration of Circulating Tumour Cells (CTCs) to Predict Clinical Symptomatic Response and Progression Free Survival in Patients Receiving Deep Subcutaneo [NCT02075606] | Phase 4 | 50 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| Efficacy and Safety of Lanreotide ATG 120 mg in Combination With Temozolomide in Subjects With Progressive Well Differentiated Thoracic Neuroendocrine Tumors. A Phase II, Multicentre, Single Arm, Open-label Trial. [NCT02698410] | Phase 2 | 40 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
Transformed scores from European Organisation for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire responses (QLQ)-C30. Questionnaire response scores range from 0 to 100. Higher scores indicate best possible Quality of Life. (NCT00353496)
Timeframe: Week 12 to Week 96 (last visit)
| Intervention | score on a scale (Least Squares Mean) |
|---|---|
| Lanreotide (Autogel Formulation) | -5.2 |
| Placebo | -4.9 |
(NCT00353496)
Timeframe: Week 12 to Week 96 (last visit)
| Intervention | percentage of participants (Number) |
|---|---|
| Lanreotide (Autogel Formulation) | 42.2 |
| Placebo | 4.7 |
Overall survival defined as the time from randomisation to death due to any cause. Subjects were followed for overall survival beyond study completion/withdrawal via annual telephone contact until the last subject completed the study. (NCT00353496)
Timeframe: Randomisation to death or last visit, up to 321 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Lanreotide (Autogel Formulation) | 84 |
| Placebo | 77 |
Pharmacokinetic Profile of Lanreotide assessed by mean serum concentration at specified timepoints (NCT00353496)
Timeframe: Week 4, 12, 24, 36, 48, 72, 96
| Intervention | ng/mL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| At Week 4 predose (n=81) | At Week 12 predose (n=87) | At Week 24 predose (n=74) | At Week 36 predose (n=67) | At Week 48 predose (n=62) | At Week 72 predose (n=52) | At Week 96 predose (n=48) | |
| Lanreotide (Autogel Formulation) | 2.5 | 5.0 | 6.1 | 6.2 | 6.6 | 6.8 | 6.6 |
Percentage of patients still ongoing (or completing at Week 96) without centrally assessed disease progression or death at Weeks 48 and 96. (NCT00353496)
Timeframe: Week 48 & 96
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Week 48 | Week 96 | |
| Lanreotide (Autogel Formulation) | 66 | 53 |
| Placebo | 49 | 25 |
Time from randomization to first documentation of disease progression, or death. Disease progression centrally assessed using Response Evaluation Criteria in Solid Tumours (RECIST) v1.0 (NCT00353496)
Timeframe: From randomisation up to the last tumour assessment (scheduled at 96 weeks). Radiological scans were performed every 12 weeks during the first year and every 24 weeks during the second year
| Intervention | Weeks (Median) |
|---|---|
| Lanreotide (Autogel Formulation) | NA |
| Placebo | 72 |
Serum samples were assessed for GH levels at the same timepoints as the IGF-1 sample at V1 and V2 and during the OGTT (non diabetic subjects only) at V3 and V11 (or at the early withdrawal visit in case of premature discontinuation). Five samples were taken over 2 hours in order to assess GH nadir and confirm the subject's eligibility before entering the co-administration period. For diabetic subjects, the OGTT was replaced by a measurement of GH level on a blood sample taken at the same time as IGF-1 at V3 and V11 (or at the early withdrawal visit). The percentage of subjects with serum GH levels ≤ 2.5 ng/mL at Baseline, V11 and LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) | ||
|---|---|---|---|
| At V3 | At V11 | At LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 38.6 | 25.0 | 22.8 |
Serum IGF-1 is a well known and validated marker of acromegaly. IGF-1 assessments were performed at Visit (V) 1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit) and were based on a single serum sample taken in fasting conditions, prior to investigational medicinal product (IMP) administration. Percentage of subjects with a normalised (age and sex adjusted) IGF-1 level at the end of the co-administration period are presented. The last observation carried forward (LOCF) was used to replace missing IGF-1 values. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) |
|---|---|
| Lanreotide Autogel + Pegvisomant Co-administration | 57.9 |
Serum samples were assessed for acid labile subunit levels at V1, V2, V3 and V11 (or at the early withdrawal visit in case of premature discontinuation). The change in mean acid labile subunit levels from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | milli IU per millilitre (mIU/mL) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -561 | -541 |
Twelve-lead ECG recordings were performed at V2, V3 and V11. Sinus rhythm, heart rate, PR interval, RR interval, QRS interval and QT interval were measured and QTcF was calculated. The change in mean ECG parameter for PR interval, QRS interval, QT interval, RR interval and QTcF from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | milliseconds (ms) (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| PR Interval: Change at V11 | PR Interval: Change at LVA | QRS Interval: Change at V11 | QRS Interval: Change at LVA | QT Interval: Change at V11 | QT Interval: Change at LVA | RR Interval: Change at V11 | RR Interval: Change at LVA | QTcF: Change at V11 | QTcF: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 1.1 | 1.3 | 0.1 | 0.3 | 4.0 | 2.4 | 34.7 | 27.6 | -1.8 | -2.2 |
Weight was recorded at V2, V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). The change in mean weight from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | kilograms (kg) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.3 | -0.3 |
Blood pressure (supine after resting for 3 minutes) was recorded at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). The change in mean BP (systolic and diastolic) from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | millimetres mercury (mmHg) (Mean) | |||
|---|---|---|---|---|
| Supine Systolic BP: Change at V11 | Supine Systolic BP: Change at LVA | Supine Diastolic BP: Change at V11 | Supine Diastolic BP: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.4 | 0.2 | -0.1 | -0.3 |
Heart rate (supine after resting for 3 minutes) was recorded at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). The change in mean heart rate from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | beats per minute (bpm) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -3.1 | -2.5 |
Pituitary tumour size was assessed by Magnetic Resonance Imaging at V2, V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). The two longest diameters of the pituitary tumour were to be measured. The change in mean pituitary tumour size from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | mm^3 (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 2.4 | 6.3 |
Glycosylated haemoglobin (HbA1C) was measured at V2, V3 and V11 (or in case of premature discontinuation, at the early withdrawal visit). The change in mean HbA1C in diabetic and non diabetic subjects from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage (Mean) | |||
|---|---|---|---|---|
| Diabetic Subjects: Change at V11 | Diabetic Subjects: Change at LVA | Non Diabetic Subjects: Change at V11 | Non Diabetic Subjects: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.05 | -0.05 | 0.05 | 0.05 |
Serum samples were assessed for prolactin levels at V1, V2, V3 and V11 (or at the early withdrawal visit in case of premature discontinuation). The change in mean prolactin levels from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | micrograms per litre (mcg/L) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.1 | -0.4 |
Glucose tolerance was only evaluated in non diabetic subjects. Glucose tolerance was assessed based on measurement of fasting blood glucose and insulin levels taken at V2 and OGTT performed at V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). A dose of 75 g oral glucose was given to subjects and blood samples then taken at 30, 60, 90 and 120 minutes after oral glucose to measure glucose, insulin and GH levels, and to evaluate the GH nadir level. The OGTT was performed after the assessment of IGF-1 and all safety laboratory tests, but before IMPs administration at V3. Glucose, insulin and GH levels were assessed before OGTT in fasting conditions and at the same time as IGF-1 assessment. The change in mean fasting insulin concentration from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | picomoles per litre (pmol/L) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -12.7 | -11.7 |
Glucose tolerance was only evaluated in non diabetic subjects. Glucose tolerance was assessed based on measurement of fasting blood glucose and insulin levels taken at V2 and OGTT performed at V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). A dose of 75 g oral glucose was given to subjects and blood samples then taken at 30, 60, 90 and 120 minutes after oral glucose to measure glucose, insulin and GH levels, and to evaluate the GH nadir level. The OGTT was performed after the assessment of IGF-1 and all safety laboratory tests, but before IMPs administration at V3. Glucose, insulin and GH levels were assessed before OGTT in fasting conditions and at the same time as IGF-1 assessment. The change in mean fasting insulin / glucose ratio from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | ratio (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -2.61 | -2.33 |
Blood samples for clinical laboratory tests were taken at V1, V2, V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). During the co-administration period, hepatic toxicity was assessed at each visit (V5 to V10) by measuring ALT, AST, alkaline phosphatase, GGT, prothrombin time and total bilirubin. Prothrombin time was expressed as a percentage of the time taken for a control blood sample to clot (designated as 100%) and the mean change from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of time (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -3.7 | -3.6 |
Serum samples were assessed for GH binding protein levels at V1, V2, V3 and V11 (or at the early withdrawal visit in case of premature discontinuation). The change in mean serum GH binding protein from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | pmol/L (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 841 | 811 |
Serum samples were assessed for GH levels at the same timepoints as the IGF-1 sample at V1 and V2 and during the OGTT (non diabetic subjects only) at V3 and V11 (or at the early withdrawal visit in case of premature discontinuation). Five samples were taken over 2 hours in order to assess GH nadir and confirm the subject's eligibility before entering the co-administration period. For diabetic subjects, the OGTT was replaced by a measurement of GH level on a blood sample taken at the same time as IGF-1 at V3 and V11 (or at the early withdrawal visit). The change in mean serum GH levels from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | nanograms per millilitre (ng/mL) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 6.6 | 6.6 |
The change in serum IGF-1 levels, expressed as z-scores calculated using the age and sex specific mean and standard deviation [SD] values from Baseline to V11 and to LVA are presented. A z-score between +/- 2 indicates a normal IGF-1 concentration. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | z-score (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -4.50 | -4.25 |
Blood samples for clinical laboratory tests were taken at V1, V2, V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). During the co-administration period, hepatic toxicity was assessed at each visit (V5 to V10) by measuring ALT, AST, alkaline phosphatase, GGT, prothrombin time and total bilirubin. The change in mean total bilirubin from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | micromoles per litre (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -1.3 | -1.2 |
The correlation between the changes in ACROQoL (expressed as standardised scores and undertaken for global score, physical and psychological dimension scores and appearance and personal relationships sub-dimension scores) over the run-in period (V3 minus V2) and co-administration period (V11 and LVA minus V3) with the corresponding changes in z-score for the IGF-1 level is presented. A decrease in IGF-1 z-score represents an improvement and an increase in ACROQoL score represents an improvement. Spearman's rank correlation (r) values are presented for change from V2 to V3 (Baseline) and from Baseline to V11/LVA for each of the specified ACROQoL categories. Corr = Correlation; Dim = Dimension; Relnship = Relationship. (NCT00383708)
Timeframe: At V2 (Day 1; Run-in), V3 (Week 12; Baseline) and V11 (Week 44)
| Intervention | correlation value (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Corr: Change V2 to V3 for Global Score | Corr: Change V3 to V11/LVA for Global Score | Corr: Change V2 to V3 for Physical Dim | Corr: Change V3 to V11/LVA for Physical Dim | Corr: Change V2 to V3 for Psychological Dim | Corr: Change V3 to V11/LVA for Psychological Dim | Corr: Change V2 to V3 for Appearance | Corr: Change V3 to V11/LVA for Appearance | Corr: Change V2 to V3 for Personal Relnship | Corr: Change V3 to V11/LVA; Personal Relnship | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.16 | 0.09 | -0.17 | 0.14 | -0.1 | 0.08 | -0.12 | 0.04 | -0.01 | 0.02 |
Presence of putative antibodies to lanreotide and antibodies to pegvisomant were assessed prior to IMP administration at V2, V4 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). The number of subjects with putative antibodies to lanreotide and to pegvisomant during the co-administration period (Baseline up to V11) is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | Number of subjects (Number) | |
|---|---|---|
| Antibodies for Lanreotide | Antibodies for Pegvisomant | |
| Lanreotide Autogel + Pegvisomant Co-administration | 4 | 6 |
A gallbladder ultrasound was performed at V2, V3, and V11 (or in case of premature study discontinuation, at the early withdrawal visit). Presence of lithiasis and sludge was recorded. Number of subjects who developed or resolved lithiasis and developed or resolved sludge, comparing Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Developed Sludge: V11 vs V3 | Resolved Sludge: V11 vs V3 | Developed Lithiasis: V11 vs V3 | Resolved Lithiasis: V11 vs V3 | Developed Sludge: LVA vs V3 | Resolved Sludge: LVA vs V3 | Developed Lithiasis: LVA vs V3 | Resolved Lithiasis: LVA vs V3 | |
| Lanreotide Autogel + Pegvisomant Co-administration | 3 | 5 | 1 | 1 | 3 | 5 | 2 | 1 |
Serum IGF-1 is a well known and validated marker of acromegaly. IGF-1 assessments were performed at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit) and were based on a single serum sample taken in fasting conditions, prior to IMP administration. Percentage of subjects with a normalised (age and sex adjusted) IGF-1 level at least once during the co-administration period, summarised by 'while taking the final dose during co-administration' and 'at any time during co-administration' are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) | |
|---|---|---|
| While Taking Final Dose During Co-administration | At Any Time During Co-administration | |
| Lanreotide Autogel + Pegvisomant Co-administration | 66.7 | 78.9 |
Serum IGF-1 is a well known and validated marker of acromegaly. IGF-1 assessments were performed at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit) and were based on a single serum sample taken in fasting conditions, prior to IMP administration. Percentage of subjects with a normalised (age and sex adjusted) IGF-1 level at the end of the co-administration period, summarised by diabetic status are presented. The denominator used to calculate percentages was the number of subjects in each subgroup (diabetic and non diabetic). The LOCF approach was used to replace missing IGF-1 values. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) | |
|---|---|---|
| Diabetic Subjects | Non Diabetic Subjects | |
| Lanreotide Autogel + Pegvisomant Co-administration | 47.4 | 63.2 |
Serum IGF-1 is a well known and validated marker of acromegaly. IGF-1 assessments were performed at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit) and were based on a single serum sample taken in fasting conditions, prior to IMP administration. Percentage of subjects with a normalised (age and sex adjusted) IGF-1 level at the end of the co-administration period, summarised by previous treatment and by final pegvisomant dose are presented. The denominator used to calculate percentages was the number of subjects in each subgroup, comprising previous treatment with pegvisomant, lanreotide Autogel and octreotide long acting repeatable (LAR) and final pegvisomant dose as either 40 mg, 60 mg or 80 mg once a week or 40 mg or 60 mg twice per week. The LOCF approach was used to replace missing IGF-1 values. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Previous Treatment: Pegvisomant | Previous Treatment: Lanreotide Autogel | Previous Treatment: Octreotide LAR | Final Dose Pegvisomant: 40 mg/week | Final Dose Pegvisomant: 60 mg/week | Final Dose Pegvisomant: 80 mg/week | Final Dose Pegvisomant: 40 mg 2x/week | Final Dose Pegvisomant: 60 mg 2x/week | |
| Lanreotide Autogel + Pegvisomant Co-administration | 46.2 | 54.2 | 70.0 | 76.9 | 61.5 | 75.0 | 60.0 | 0 |
Serum IGF-1 is a well known and validated marker of acromegaly. IGF-1 assessments were performed at V1, V2, V3, V5, V7, V9 and V11 (or in case of premature study discontinuation, at the early withdrawal visit) and were based on a single serum sample taken in fasting conditions, prior to IMP administration. The percentage of subjects with a normalised (age and sex adjusted) IGF-1 level is presented. The denominator used to calculate the percentages was the number of ITT population subjects with an assessment at the visit. In addition to the data for each individual visit, the last value available (LVA) data is also presented. None of the ITT population subjects had serum IGF-1 normalised at V3, consistent with the criterion to continue in the study and be treated in the co-administration period. (NCT00383708)
Timeframe: V1 (Screening) up to V11 (Week 44)
| Intervention | percentage of subjects (Number) | ||||||
|---|---|---|---|---|---|---|---|
| V1 (Screening) | V2 (Day 1) | V5 (Week 20) | V7 (Week 28) | V9 (Week 36) | V11 (Week 44) | LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 17.5 | 24.5 | 56.4 | 48.1 | 57.7 | 61.5 | 57.9 |
Glucose tolerance was only evaluated in non diabetic subjects. Glucose tolerance was assessed based on measurement of fasting blood glucose and insulin levels taken at V2 and OGTT performed at V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). A dose of 75 g oral glucose was given to subjects and blood samples then taken at 30, 60, 90 and 120 minutes after oral glucose to measure glucose, insulin and GH levels, and to evaluate the GH nadir level. The OGTT was performed after the assessment of IGF-1 and all safety laboratory tests, but before IMPs administration at V3. Glucose, insulin and GH levels were assessed before OGTT in fasting conditions and at the same time as IGF-1 assessment. The change in mean fasting glucose concentration from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | mmol/L (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.05 | -0.09 |
Glucose tolerance was only evaluated in non diabetic subjects. Glucose tolerance was assessed based on measurement of fasting blood glucose and insulin levels taken at V2 and OGTT performed at V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). A dose of 75 g oral glucose was given to subjects and blood samples then taken at 30, 60, 90 and 120 minutes after oral glucose to measure glucose, insulin and GH levels, and to evaluate the GH nadir level. The OGTT was performed after the assessment of IGF-1 and all safety laboratory tests, but before IMPs administration at V3. Glucose, insulin and GH levels were assessed before OGTT in fasting conditions and at the same time as IGF-1 assessment. The change in mean blood glucose Cmax (as determined from OGTT) from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | millimoles per litre (mmol/L) (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 0.53 | 0.61 |
Blood samples for clinical laboratory tests were taken at V1, V2, V3 and V11 (or in case of premature study discontinuation, at the early withdrawal visit). During the co-administration period, hepatic toxicity was assessed at each visit (V5 to V10) by measuring alanine amino transferase (ALT), aspartate amino transferase (AST), alkaline phosphatase, gamma glutamyl transferase (GGT), prothrombin time and total bilirubin. The change in mean ALT, AST, GGT and alkaline phosphatase from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | IU/L (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| AST: Change at V11 | AST: Change at LVA | ALT: Change at V11 | ALT: Change at LVA | GGT: Change at V11 | GGT: Change at LVA | Alkaline Phosphatase: Change at V11 | Alkaline Phosphatase: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 3.3 | 4.5 | 4.1 | 7.8 | -1.0 | 1.5 | -1.7 | -0.8 |
Twelve-lead ECG recordings were performed at V2, V3 and V11. Sinus rhythm, heart rate, PR interval, RR interval, QRS interval and QT interval were measured and heart rate corrected QT interval using the Fridericia method (QTcF) was calculated. The change in ECG mean heart rate from Baseline to V11 and to LVA is presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | bpm (Mean) | |
|---|---|---|
| Change at V11 | Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -2.8 | -2.2 |
Acromegaly symptoms, including arthralgia, excessive perspiration, fatigue, headache and soft tissue swelling were assessed with scores ranging from 0 (no symptoms) to 8 (severe, incapacitating symptoms). Symptoms were assessed by the subject in paper format before any other procedure planned during the visit. The change in acromegaly symptoms from Baseline to V11 and to LVA are presented. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | units on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Arthralgia: Change at V11 | Arthralgia: Change at LVA | Excessive Perspiration: Change at V11 | Excessive Perspiration: Change at LVA | Fatigue: Change at V11 | Fatigue: Change at LVA | Headache: Change at V11 | Headache: Change at LVA | Soft Tissue Swelling: Change at V11 | Soft Tissue Swelling: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | -0.7 | -0.6 | -0.4 | -0.4 | -0.2 | -0.2 | -0.4 | -0.3 | -0.6 | -0.6 |
The ACROQoL is a health-related quality of life (QoL) questionnaire for patients with acromegaly consisting of 22 items measured on a 5-point Likert-type scale that assesses frequency of occurrence (always to never) or degree of agreement (completely agree to completely disagree) with the statements. The ACROQoL consists of questions that evaluate physical (8 items) and psychological aspects related to appearance and personal relations (7 items each). Answers are transformed to a percentage value, where 100 is the maximal (best) and 0 the minimum (worse) score depicting self-perceived quality QoL. An increase in ACROQoL score is associated with an improved QoL. The change in ACROQoL global score, physical and psychological dimension scores and appearance and personal relationships sub-dimension scores from Baseline to V11 and to LVA are presented. Relnship = Relationship; Dim = Dimension. (NCT00383708)
Timeframe: V3 (Week 12; Baseline) up to V11 (Week 44)
| Intervention | units on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Global Score: Change at V11 | Global Score: Change at LVA | Physical Dimensions Score: Change at V11 | Physical Dimensions Score: Change at LVA | Psychological Dimensions Score: Change at V11 | Psychological Dimensions Score: Change at LVA | Appearance Sub-Dimension Score: Change at V11 | Appearance Sub-Dimension Score: Change at LVA | Personal Relnship Sub-Dim Score: Change at V11 | Personal Relnship Sub-Dim Score: Change at LVA | |
| Lanreotide Autogel + Pegvisomant Co-administration | 2.4 | 2.2 | 4.2 | 3.5 | 1.3 | 1.4 | 3.8 | 3.7 | -0.1 | -0.9 |
Acromegaly symptoms are sweating, snoring, joint pain, headache and fatigue. Each symptom was scored as -2 = 'always', -1 = 'most of the time', 0 = 'sometimes', 1 = 'rarely and 2 = 'never'. The total score was used to evaluate symptom control in each patient at Week 0 and Week 24/Termination. The total worst score is -10 and best score is 10. (NCT00447499)
Timeframe: 24 Weeks
| Intervention | On a Scale from -10 to 10 (Mean) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate) Injection | 0.9 |
Blood samples taken before and 60 and 120 min after glucose load from fasting patient. (NCT00447499)
Timeframe: 24 Weeks
| Intervention | ng/mL (Mean) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate) Injection | -0.3 |
Blood samples taken before and 60 and 120 min after glucose load from fasting patient. (NCT00447499)
Timeframe: 24 Weeks
| Intervention | Percent of Participants (Number) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate) | 89 |
Experienced Convenience of Somatuline® Autogel® Injections was assessed by the subject as: Very convenient; somewhat convenient; neither convenient nor inconvenient; Neither convenient nor inconvenient; Somewhat inconvenient; very inconvenient. (NCT00447499)
Timeframe: 24 weeks
| Intervention | Percent of Participants (Number) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate)/Switch Patient | 91 |
The primary efficacy endpoint was the percentage of patients (Switch and other) or their partners who were competent to self-administer lanreotide at the end of the study (Week 24/Early Termination), as assessed by the Assessment of Competence Questionnaire (0 = 'No' and 1 = 'Yes'). (NCT00447499)
Timeframe: 24 weeks
| Intervention | Percentage of Participants (Number) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate) Injection | 98 |
Healthcare professional convenience questionnaires are: Confident the Subject Properly Administering the Injection; Subject Complained About Pain When Administering the Injection; Subject Appreciated the Option of Self-Injection at Home. Each Healthcare professional convenience questionnaire was scored -2, -1, 0, 1 and 2; from most negative to most positive response. A total score across all questions was calculated and was used to evaluate the convenience. The worst total score is -6 and best total score is 6. (NCT00447499)
Timeframe: 24 weeks
| Intervention | On a Scale from -6 to 6 (Mean) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate) Injection | 4.6 |
Blood sample was collected while subject is in a fasting state or non-fasting state for measuring the level of IGF-1. (NCT00447499)
Timeframe: 24 weeks
| Intervention | Percent of Participants (Number) |
|---|---|
| Somatuline Autogel (Lanreotide Acetate)/Switch Patient | 94 |
"Biochemical control was assessed by analysing 5-HIAA levels at each site visit, which was judged as necessary by the investigator at each site.~'Before self or partner administration' was assessed at baseline for group 1 and at week 12 for group 2.~'After self or partner administration' was assessed at week 16 to 20 for group 1 and at week 12 for group 2.~'Before HCP administration' was assessed at week 16 to 20 for group 1 and at baseline for group 2.~'After HCP administration' was assessed at week 30 to 34 for group 1 and week 12 for group 2." (NCT00681187)
Timeframe: Group 1 - Baseline, week 16 to 20 and 30 to 34. Group 2 - Baseline, week 12 and 30 to 34.
| Intervention | nmol/l (Mean) |
|---|---|
| Before Self or Partner Administration | 220.17 |
| After Self or Partner Administration | 219.17 |
| Before HCP Administration | 217.08 |
| After HCP Administration | 219.58 |
"Biochemical control was assessed by analysing chromogranin A levels at each site visit, which was mandatory for all subjects.~'Before self or partner administration' was assessed at baseline for group 1 and at week 12 for group 2.~'After self or partner administration' was assessed at week 16 to 20 for group 1 and at week 12 for group 2.~'Before HCP administration' was assessed at week 16 to 20 for group 1 and at baseline for group 2.~'After HCP administration' was assessed at week 30 to 34 for group 1 and week 12 for group 2." (NCT00681187)
Timeframe: Group 1 - Baseline, week 16 to 20 and 30 to 34. Group 2 - Baseline, week 12 and 30 to 34.
| Intervention | nmol/l (Mean) |
|---|---|
| Before Self or Partner Administration | 37.48 |
| After Self or Partner Administration | 47.85 |
| Before HCP Administration | 42.05 |
| After HCP Administration | 37.42 |
Health care and patient costs associated with the treatment of carcinoid symptoms in subjects treated with lanreotide Autogel were assessed through recording loss of production for subject through total number of days sick leave of the employed patients (n=6). (NCT00681187)
Timeframe: Group 1 - between week 8 to 20 (self or partner administration), between week 20 to 32 (HCP administration). Group 2 - between week 20 to 32 (self or partner administration), between week 0 to week 12 (HCP administration)
| Intervention | days (Number) |
|---|---|
| Self or Partner Administration | 23 |
| HCP Administration | 0 |
"Assessed by the number of HCP with a positive response 'yes' to two questions:~Based on your experience during this trial, did you feel confident in the safety of your patients?~Based on your experience during this trial, would you recommend suitable patients to try self or partner administration?" (NCT00681187)
Timeframe: Between week 30 to 34
| Intervention | participants (Number) |
|---|---|
| Overall Study Group | 9 |
The subject was asked: 'Does the treatment administration used today negatively interfere with your psychological wellbeing?' (NCT00681187)
Timeframe: Between baseline to week 32, after each injection (8-9 injections)
| Intervention | participants (Number) |
|---|---|
| Training Period | 4 |
| Self or Partner Administration | 2 |
| HCP Administration | 1 |
A global question was asked: 'If you could choose, which administration method would you like to use on a regular basis?' A) Healthcare professional provided injection B) Self/ partner administered injection (NCT00681187)
Timeframe: Between week 30 to 34
| Intervention | participants (Number) |
|---|---|
| Group 1 Self or Partner First Then HCP Administration | 10 |
| Group 2 HCP Then Self or Partner Administration | 12 |
Health care and patient costs associated with the treatment of carcinoid symptoms in subjects treated with lanreotide Autogel were assessed by recording the total number of visits made by participants (n=12) to HCP due to carcinoid symptoms. (NCT00681187)
Timeframe: Group 1 - between week 8 to 20 (self or partner administration), between week 20 to 32 (HCP administration). Group 2 - between week 20 to 32 (self or partner administration), between week 0 to week 12 (HCP administration)
| Intervention | visits (Number) |
|---|---|
| Self or Partner Administration | 17 |
| HCP Administration | 25 |
Participants were asked how they perceived the symptoms in respect to episodes of diarrhoea since the last injection. Participants included in the study were previously treated with lanreotide autogel and therefore the assessment at baseline was made in comparison to previous injection outside of the study protocol. (NCT00681187)
Timeframe: Group 1 - baseline, week 16 to 20 (self or partner administration) and week 30 to 34 (HCP administration). Group 2 - baseline, week 12 to 16 (HCP administration) and week 30 to 34 (self or partner administration).
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Worsened | Similar | Improved | Missing | |
| Baseline | 1 | 22 | 2 | 0 |
| HCP Administration | 0 | 24 | 1 | 0 |
| Self or Partner Administration | 4 | 17 | 3 | 1 |
Participants were asked how they perceived the symptoms in respect to episodes of flushing since the last injection. Participants included in the study were previously treated with lanreotide Autogel and therefore the assessment at baseline was made in comparison to their previous injection outside of the study protocol. (NCT00681187)
Timeframe: Group 1 - baseline, week 16 to 20 (self or partner administration) and week 30 to 34 (HCP administration). Group 2 - baseline, week 12 (HCP administration) and week 30 (self or partner administration).
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Worsened | Similar | Improved | Missing | |
| Baseline | 0 | 24 | 1 | 0 |
| HCP Administration | 1 | 20 | 4 | 0 |
| Self or Partner Administration | 1 | 21 | 2 | 1 |
The subject was asked: 'Does the treatment administration used today interfere with your daily activities?' (NCT00681187)
Timeframe: Between baseline to week 32, after each injection (8-9 injections)
| Intervention | Participants (Number) |
|---|---|
| Training Period | 6 |
| Self or Partner Administration | 2 |
| HCP Administration | 6 |
(NCT00690898)
Timeframe: Baseline (week 1) to week 12 and week 24
| Intervention | participants (Number) | |||
|---|---|---|---|---|
| Greater than or equal to 20% at week 12 (n=85) | Less than 20% at week 12 (n=85) | Greater than or equal to 20% at week 24 (n=80) | Less than 20% at week 24 (n=80) | |
| Lanreotide Autogel 120 mg | 46 | 39 | 45 | 35 |
(NCT00690898)
Timeframe: Week 12, 24, and 48
| Intervention | percentage change (Mean) | ||
|---|---|---|---|
| Week 12 (n=85) | Week 24 (n=78) | Week 48 (n=62) | |
| Lanreotide Autogel 120 mg | -43.8 | -47.4 | -56.7 |
(NCT00690898)
Timeframe: Week 12, 24, and 48
| Intervention | percentage change (Mean) | ||
|---|---|---|---|
| Week 12 (n=85) | Week 24 (n=78) | Week 48 (n=63) | |
| Lanreotide Autogel 120 mg | -62.1 | -64.6 | -70.9 |
The status of clinical signs of acromegaly assessed by an acromegaly symptoms questionnaire (paper form) completed by the patient at each study visit. The scoring for each clinical sign of acromegaly on the questionnaire is from 0 (no symptom) to 8 (severe, incapacitating symptom). The variation (or no variation) in scores indicate whether the clinical sign of acromegaly had improved, worsened or was unchanged. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline to week 12 - Worsened (n=88) | Baseline to week 12 - Unchanged (n=88) | Baseline to week 12 - Improved (n=88) | Baseline to week 24 - Worsened (n=81) | Baseline to week 24 - Unchanged (n=81) | Baseline to week 24 - Improved (n=81) | Baseline to week 48 - Worsened (n=62) | Baseline to week 48 - Unchanged (n=62) | Baseline to week 48 - Improved (n=62) | |
| Lanreotide Autogel 120 mg | 9.1 | 26.1 | 64.8 | 11.1 | 24.7 | 64.2 | 17.7 | 22.6 | 59.7 |
The status of clinical signs of acromegaly assessed by an acromegaly symptoms questionnaire (paper form) completed by the patient at each study visit. The scoring for each clinical sign of acromegaly on the questionnaire is from 0 (no symptom) to 8 (severe, incapacitating symptom). The variation (or no variation) in scores indicate whether the clinical sign of acromegaly had improved, worsened or was unchanged. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline to week 12 - Worsened (n=88) | Baseline to week 12 - Unchanged (n=88) | Baseline to week 12 - Improved (n=88) | Baseline to week 24 - Worsened (n=81) | Baseline to week 24 - Unchanged (n=81) | Baseline to week 24 - Improved (n=81) | Baseline to week 48 - Worsened (n=62) | Baseline to week 48 - Unchanged (n=62) | Baseline to week 48 - Improved (n=62) | |
| Lanreotide Autogel 120 mg | 13.6 | 25.0 | 61.4 | 16.0 | 17.3 | 66.7 | 14.5 | 29.0 | 56.5 |
The status of clinical signs of acromegaly assessed by an acromegaly symptoms questionnaire (paper form) completed by the patient at each study visit. The scoring for each clinical sign of acromegaly on the questionnaire is from 0 (no symptom) to 8 (severe, incapacitating symptom). The variation (or no variation) in scores indicate whether the clinical sign of acromegaly had improved, worsened or was unchanged. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline to week 12 - Worsened (n=88) | Baseline to week 12 - Unchanged (n=88) | Baseline to week 12 - Improved (n=88) | Baseline to week 24 - Worsened (n=81) | Baseline to week 24 - Unchanged (n=81) | Baseline to week 24 - Improved (n=81) | Baseline to week 48 - Worsened (n=62) | Baseline to week 48 - Unchanged (n=62) | Baseline to week 48 - Improved (n=62) | |
| Lanreotide Autogel 120 mg | 13.6 | 46.6 | 39.8 | 11.1 | 42.0 | 46.9 | 14.5 | 46.8 | 38.7 |
The status of clinical signs of acromegaly assessed by an acromegaly symptoms questionnaire (paper form) completed by the patient at each study visit. The scoring for each clinical sign of acromegaly on the questionnaire is from 0 (no symptom) to 8 (severe, incapacitating symptom). The variation (or no variation) in scores indicate whether the clinical sign of acromegaly had improved, worsened or was unchanged. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline to week 12 - Worsened (n=88) | Baseline to week 12 - Unchanged (n=88) | Baseline to week 12 - Improved (n=88) | Baseline to week 24 - Worsened (n=81) | Baseline to week 24 - Unchanged (n=81) | Baseline to week 24 - Improved (n=81) | Baseline to week 48 - Worsened (n=62) | Baseline to week 48 - Unchanged (n=62) | Baseline to week 48 - Improved (n=62) | |
| Lanreotide Autogel 120 mg | 10.2 | 26.1 | 63.6 | 11.1 | 22.2 | 66.7 | 14.5 | 19.4 | 66.1 |
A blinded, centrally assessed evaluation of all MRIs was performed. A 20% reduction from the volume at Visit 1 was considered to be clinically relevant. (NCT00690898)
Timeframe: Week 1 and Week 48
| Intervention | percentage of subjects (Number) | |
|---|---|---|
| Greater than or equal to 20% | Less than 20% | |
| Lanreotide Autogel 120 mg | 62.9 | 37.1 |
The status of clinical signs of acromegaly assessed by an acromegaly symptoms questionnaire (paper form) completed by the patient at each study visit. The scoring for each clinical sign of acromegaly on the questionnaire is from 0 (no symptom) to 8 (severe, incapacitating symptom). The variation (or no variation) in scores indicate whether the clinical sign of acromegaly had improved, worsened or was unchanged. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline to week 12 - Worsened (n=88) | Baseline to week 12 - Unchanged (n=88) | Baseline to week 12 - Improved (n=88) | Baseline to week 24 - Worsened (n=81) | Baseline to week 24 - Unchanged (n=81) | Baseline to week 24 - Improved (n=81) | Baseline to week 48 - Worsened (n=62) | Baseline to week 48 - Unchanged (n=62) | Baseline to week 48 - Improved (n=62) | |
| Lanreotide Autogel 120 mg | 11.4 | 25.0 | 63.6 | 14.8 | 21.0 | 64.2 | 9.7 | 24.2 | 66.1 |
(NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | mcg/L (Mean) | |||
|---|---|---|---|---|
| Prolactin levels at baseline (n=21) | Change From Baseline to Week 12 (n=20) | Change From Baseline to Week 24 (n=20) | Change From Baseline to Week 48 (n=12) | |
| Lanreotide Autogel 120 mg | 48.0 | -18.0 | -18.6 | -17.3 |
Acromegaly Quality of Life Assessment (AcroQoL) questionnaire response scores range from 0 to 100. Higher scores indicate best possible Quality of Life. (NCT00690898)
Timeframe: Week 12, 24 and 48
| Intervention | units on a scale (Mean) | ||
|---|---|---|---|
| Baseline to week 12 (n=82) | Baseline to week 24 (n=75) | Baseline to week 48 (n=59) | |
| Lanreotide Autogel 120 mg | 7.8 | 8.0 | 9.5 |
(NCT00701363)
Timeframe: Baseline (visit 1)
| Intervention | Percentage of ULN (Mean) | ||
|---|---|---|---|
| Uncontrolled IGF-1 levels at Week 24 (n=14) | Normalized IGF-1 levels at Week 24 (A+B+C) (n=108) | Difference in Mean Baseline | |
| Overall Study | 95.92 | 67.49 | 28.43 |
(NCT00701363)
Timeframe: At Baseline, week 24 and week 48
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| ITT - Baseline (n=15, 13, 70, 26, and 124) | ITT - Week 24 (n=3, 13, 70, 26, and 112) | ITT - Week 48 (n=0, 13, 68, 26, and 107) | MITT - Baseline (n=0, 13, 70, 26, and 109) | MITT - Week 24 (n=0, 13, 70, 26, and 109) | MITT - Week 48 (n=0, 13, 68, 26, and 107) | |
| Overall Study | 0.97 | 0.99 | 0.92 | 0.96 | 0.88 | 0.92 |
| Phase 1 Only: Lanreotide Autogel 120 mg | 1.04 | 4.89 | NA | NA | NA | NA |
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | 0.92 | 0.90 | 0.69 | 0.92 | 0.90 | 0.69 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | 0.92 | 0.95 | 0.99 | 0.92 | 0.95 | 0.99 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | 1.08 | 0.67 | 0.83 | 1.08 | 0.67 | 0.83 |
The criterion for a subject is satisfied if he extended his injection interval to eight weeks during Phase 2 of the study, whilst maintaining normalised IGF-1 levels at Week 48. (NCT00701363)
Timeframe: At week 48
| Intervention | Percentage of subjects (Number) | |
|---|---|---|
| Intention-to-Treat (n=124) | Modified Intention-to-Treat (n=109) | |
| Overall Study | 20.2 | 22.9 |
A subject was responder if he maintained his injection interval schedule of 6 weeks or increased his injection interval to eight weeks whilst keeping his normalised IGF-1 level (age and sex adjusted) at the end of the study (Week 48) (NCT00701363)
Timeframe: At week 48 (End of Study)
| Intervention | Percentage of subjects (Number) | |
|---|---|---|
| Intention-to-Treat (n=124) | Modified Intention-to-Treat (n=109) | |
| Overall Study | 75.8 | 86.2 |
The criterion for a subject is satisfied if he maintained an injection interval of six weeks or increasing his injection interval to eight weeks during Phase 2 of the study. (NCT00701363)
Timeframe: During phase 2 of the study (up to week 48)
| Intervention | Percentage of subjects (Number) | |
|---|---|---|
| Intention-to-Treat (n=124) | Modified Intention-to-Treat (n=109) | |
| Overall Study | 78.2 | 88.1 |
Short Form-36 questionnaire (SF-36) score comprises eight components: Physical function, role-physical, bodily pain, general health, vitality, social functioning, role-emotional and mental health on a scale of 100, where a score of 100 corresponds to the best possible QoL and 0 to the worst. (NCT00701363)
Timeframe: At weeks 24 and 48
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| At week 24 (n=3, 13, 70, 26, and 112) | At week 48 (n=0, 13, 68, 26, and 107) | |
| Overall Study | 1.03 | 0.06 |
| Phase 1 Only: Lanreotide Autogel 120 mg | -0.66 | NA |
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | 4.91 | 4.96 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | 1.79 | -0.61 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | -2.75 | -0.62 |
AcroQoL score groups 22 components: Eight physical, Seven psychological appearance and Seven psychological personal relations, adjusted to a scale of 100, where a score of 100 corresponds to the best possible QoL and 0 to the worst. (NCT00701363)
Timeframe: At weeks 24 and 48
| Intervention | Units on a scale (Mean) | |
|---|---|---|
| At week 24 (n=1, 9, 55, 21, and 86) | At week 48 (n=0, 9, 53, 21, and 83) | |
| Overall Study | -0.35 | -1.08 |
| Phase 1 Only: Lanreotide Autogel 120 mg | 21.59 | NA |
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | -2.15 | 1.31 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | -0.27 | -1.32 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | -0.84 | -1.52 |
"At week 24, the preference assessed between Octreotide Long Acting Repeatable intramuscular injection (Oct-LAR IM) every 4 weeks and Lanreotide Autogel 120 mg subcutaneous injection (SC) every 6 weeks.~At week 48, the preference is assessed between Oct-LAR IM every 4 weeks and Lanreotide Autogel 120 mg SC either injected every 4, 6 or 8 weeks (as injected during Phase II of the study)." (NCT00701363)
Timeframe: At weeks 24 and 48
| Intervention | Percentage of subjects (Number) | |||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| W24:Oct-LAR IM inj evy 4 wks Phs 1 only (n=15) | W24:Lan Autogel inj evy 6 wks Phs 1 only (n=15) | W24:Oct-LAR IM inj evy 4 wks Phs 1/Grp A(n=13) | W24:Lan Autogel inj evy 6 wks Phs 1/Grp A(n=13) | W24:Oct-LAR IM inj evy 4 wks Phs 1/Grp B(n=70) | W24:Lan Autogel inj evy 6 wks Phs 1/Grp B(n=70) | W24:Non precised Phs 1/Grp B (n=70) | W24:Oct-LAR IM inj evy 4 wks Phs 1/Grp C(n=26) | W24:Lan Autogel inj every 6 wks Phs 1/Grp C(n=26) | W 24:Oct-LAR IM inj evy 4 wks-Overall study(n=124) | W24:Lan Autogel inj evy 6 wks-Overall study(n=124) | W 24: Non precised - Overall study (n=124) | W48:Oct-LAR IM inj evy 4 wks Phs 1/Grp A(n=13) | W48:Lan Autogel inj evy 6 wks Phs 1/Grp A(n=13) | W48:Non precised Phs 1/Grp A (n=13) | W48:Oct-LAR IM inj evy 4 wks Phs 1/Grp B(n=70) | W48:Lan Autogel inj evy 4 wks Phs 1/Grp B(n=70) | W48:Lan Autogel inj evy 6 wks Phs 1/Grp B(n=70) | W48:Non precised Phs 1/Grp B (n=70) | W48:Oct-LAR IM inj evy 4 wks Phs 1/Grp C(n=26) | W48:Lan Autogel inj evy 8 wks Phs 1/Grp C(n=26) | W48:Oct-LAR IM inj evy 4 wks-Overall study(n=124) | W48:Lan Autogel inj evy 4 wks-Overall study(n=124) | W48:Lan Autogel inj evy 6 wks-Overall study(n=124) | W48:Lan Autogel inj evy 8 wks-Overall study(n=124) | W48:Non precised-Overall study (n=124) | |
| Overall Study | 20 | 80 | 7.7 | 92.3 | 10.3 | 85.3 | 4.4 | 3.8 | 96.2 | 8.9 | 88.4 | 2.7 | 15.4 | 76.9 | 7.7 | 14.7 | 1.5 | 77.9 | 5.9 | 7.7 | 92.3 | 13.1 | 10.3 | 49.5 | 22.4 | 4.7 |
Acromegaly symptoms were assessed by the patients using the Patient Assessed Acromegaly Symptom Questionnaire (PASQ) scale ranging from 0 (No symptoms) to 8 (Severe, incapacitating symptoms). (NCT00701363)
Timeframe: At baseline, week 24 and week 48
| Intervention | Units on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline - Headache | Baseline - Excessive perspiration | Baseline - Fatigue | Baseline - Soft tissue swelling | Baseline - Arthralgia | Week 24 - Headache | Week 24 - Excessive perspiration | Week 24 - Fatigue | Week 24 - Soft tissue swelling | Week 24 - Arthralgia | Week 48 - Headache | Week 48 - Excessive perspiration | Week 48 - Fatigue | Week 48 - Soft tissue swelling | Week 48 - Arthralgia | |
| Phase 1 Only: Lanreotide Autogel 120 mg | 2.73 | 2.80 | 3.40 | 1.13 | 2.73 | 2.67 | 2.00 | 2.33 | 1.33 | 2.00 | NA | NA | NA | NA | NA |
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | 2.15 | 1.92 | 4.23 | 2.77 | 3.46 | 1.38 | 2.08 | 3.85 | 2.46 | 3.62 | 1.77 | 2.31 | 3.77 | 2.85 | 3.46 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | 1.80 | 2.41 | 3.27 | 1.81 | 3.13 | 1.93 | 2.25 | 3.36 | 1.71 | 3.09 | 2.32 | 2.50 | 3.16 | 2.10 | 3.60 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | 2.04 | 2.08 | 3.31 | 1.42 | 4.42 | 2.04 | 2.64 | 4.08 | 1.76 | 3.68 | 2.62 | 2.50 | 3.92 | 1.62 | 4.04 |
IGF-1 change from Baseline to Week 48 = Mean IGF-1 level at Week 48 - Mean IGF-1 level at Baseline (NCT00701363)
Timeframe: Baseline (visit 1) and week 48
| Intervention | Percentage of ULN (Mean) |
|---|---|
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | -1.70 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | 5.74 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | -4.33 |
(NCT00701363)
Timeframe: Baseline (visit 1)
| Intervention | Percentage of ULN (Mean) |
|---|---|
| Phase 2 (Group A): Lanreotide Autogel 120 mg Every 4 Weeks | 98.69 |
| Phase 2 (Group B): Lanreotide Autogel 120 mg Every 6 Weeks | 67.75 |
| Phase 2 (Group C): Lanreotide Autogel 120 mg Every 8 Weeks | 51.30 |
"AcroQoL change from Baseline to Week 24 (48) = AcroQoL at Week 24 (48) - AcroQoL at Baseline.~IGF-1 change from Baseline to Week 24 (48) = IGF-1 at Week 24 (48) - IGF-1 at Baseline.~Correlation presented is a Spearman correlation (non parametric)." (NCT00701363)
Timeframe: At weeks 24 and 48
| Intervention | Correlation coefficient (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 24: Phase I / Group A (n=8) | Week 24: Phase I / Group B (n=55) | Week 24: Phase I / Group C (n=21) | Week 24: Overall study (n=85) | Week 48: Phase I / Group A (n=8) | Week 48: Phase I / Group B (n=53) | Week 48: Phase I / Group C (n=21) | Week 48: Overall study (n=82) | |
| Overall Study | 0.43 | -0.02 | -0.41 | -0.01 | 0.69 | -0.06 | -0.09 | -0.01 |
(NCT00701363)
Timeframe: At weeks 24 and 48
| Intervention | Percentage of subjects (Number) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ITT: Week 24 - Phase I only (n=15) | ITT: Week 24 - Phase I / Group A (n=13) | ITT: Week 24 - Phase I / Group B (n=70) | ITT: Week 24 - Phase I / Group C (n=26) | ITT: Week 24 - Overall study (n=124) | ITT: Week 48 - Phase I / Group A (n=13) | ITT: Week 48 - Phase I / Group B (n=70) | ITT: Week 48 - Phase I / Group C (n=26) | ITT: Week 48 - Overall study (n=124) | MITT: Week 24 - Phase I / Group A (n=13) | MITT: Week 24 - Phase I / Group B (n=70) | MITT: Week 24 - Phase I / Group C (n=26) | MITT: Week 24 - Overall study (n=109) | MITT: Week 48 - Phase I / Group A (n=13) | MITT: Week 48 - Phase I / Group B (n=70) | MITT: Week 48 - Phase I / Group C (n=26) | MITT: Week 48 - Overall study (n=109) | |
| Overall Study | 66.7 | 100.0 | 91.4 | 100.0 | 93.8 | 100.0 | 92.6 | 96.2 | 94.4 | 100.0 | 91.4 | 100.0 | 94.5 | 100.0 | 92.6 | 96.2 | 94.4 |
The criterion for a subject is satisfied if he has a normalised IGF-1 level (age and sex adjusted) at week 24. (NCT00701363)
Timeframe: At week 24
| Intervention | Percentage of subjects (Number) | |
|---|---|---|
| Intention-to-Treat (n=124) | Modified Intention-to-Treat (n=109) | |
| Overall Study | 88.7 | 100 |
The criterion for a subject is satisfied if he had a IGF-1 level (age and sex adjusted) without any worsening of the AcroQoL change score between Inclusion and Week 48. (NCT00701363)
Timeframe: At week 48 (End of Study)
| Intervention | Percentage of subjects (Number) | |||
|---|---|---|---|---|
| Phase I / Group A (n=9) | Phase I / Group B (n=55) | Phase I / Group C (n=21) | Overall study (n=85) | |
| Overall Study | 44.4 | 47.2 | 38.1 | 44.6 |
Usage of other concomitant rescue medications for diarrhoea and/or flushing events, measured as the percentage of days that the medications were used as rescue medication based on subject IVRS/IWRS diary records. Subjects were required to record the use and dose of s.c. octreotide, if any, as well as the use of other concomitant rescue medications (e.g. loperamide 2 mg tabs, and/or tincture of opium). (NCT00774930)
Timeframe: 16-week DB phase
| Intervention | Percentage of days (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 8.86 |
| Placebo | 6.25 |
Use of s.c. octreotide required to control symptoms associated with carcinoid syndrome, measured as the percentage of days that s.c. octreotide was used as rescue medication, based on subject Interactive Voice Response System (IVRS) or Interactive Web Response System (IWRS) diary records. (NCT00774930)
Timeframe: 16-week DB phase
| Intervention | Percentage of days (Least Squares Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 33.72 |
| Placebo | 48.49 |
Subjects who rolled over early were those who received less than four DB injections before receiving the first IOL injection. (NCT00774930)
Timeframe: 16-week DB phase
| Intervention | Percentage of subjects (Number) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 18.6 |
| Placebo | 21.4 |
"Baseline is defined as the last non-missing observation obtained prior to the initiation of study treatment.~Q29 and Q30 range from 1 (Very poor) to 7 (Excellent) with 1 being worst case and 7 the most favourable answer. Scores were derived according to the rules contained within the EORTC scoring manual. All of the scores range in score from 0 to 100. A high score for global health status/QoL represents high QoL. The principle for scoring the scale is: Estimate the average of the items (I1, I2, ..., In) that contribute to the scale; this is the raw score. Raw score = RS = (I1 + I2 +…+ In)/n.~For global health status/QoL: Score = {(RS - 1)/range} x 100, where range is the difference between the maximum possible value of RS and the minimum possible value of RS." (NCT00774930)
Timeframe: Baseline and Week 12 of DB phase
| Intervention | Units on a scale (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 4.17 |
| Placebo | -1.72 |
"Baseline is defined as the last non-missing observation obtained prior to the initiation of study treatment.~The QLQ-G.I.NET21 questionnaire contains 21 single items (Q31 to Q51) which are supplemental items to the EORTC QLQ-C30 questionnaire. Q31 to Q51 range from 1 to 4 with 1 being the most favourable answer and 4 the worst case (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much). Based on these items the scores were generated. All of the scores range in score from 0 to 100. A high score for a symptom scale represents a high level of symptomatology. The principle for scoring the scale is: Estimate the average of the items (I1, I2, ..., In) that contribute to the scale; this is the raw score. RS = (I1 + I2 +…+ In)/n.~For symptom scales: Score = {(RS - 1)/range} x 100, where range is the difference between the maximum possible value of RS and the minimum possible value of RS." (NCT00774930)
Timeframe: Baseline and Week 12 of DB phase
| Intervention | Units on a scale (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | -6.83 |
| Placebo | -2.69 |
Baseline is defined as the last non-missing observation obtained prior to the initiation of study treatment. (NCT00774930)
Timeframe: Baseline and Week 12 of DB phase
| Intervention | μg/L (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 1125.8 |
| Placebo | 801.5 |
Baseline is defined as the last non-missing observation obtained prior to the initiation of study treatment. (NCT00774930)
Timeframe: Baseline and Week 12 of DB phase
| Intervention | μmol/day (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | -201.4 |
| Placebo | 36.3 |
(NCT00774930)
Timeframe: 16-week DB phase
| Intervention | Number of events per day (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 1.56 |
| Placebo | 1.35 |
(NCT00774930)
Timeframe: 16-week DB phase
| Intervention | Number of events per day (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | 0.92 |
| Placebo | 1.75 |
"Baseline is defined as the last non-missing observation obtained prior to the initiation of study treatment.~The QLQ-G.I.NET21 questionnaire contains 21 single items (Q31 to Q51) which are supplemental items to the EORTC QLQ-C30 questionnaire. Q31 to Q51 range from 1 to 4 with 1 being the most favourable answer and 4 the worst case (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much). Based on these items the scores were generated. All of the scores range in score from 0 to 100. A high score for a symptom scale represents a high level of symptomatology. The principle for scoring the scale is: Estimate the average of the items (I1, I2, ..., In) that contribute to the scale; this is the raw score. RS = (I1 + I2 +…+ In)/n.~For symptom scales: Score = {(RS - 1)/range} x 100, where range is the difference between the maximum possible value of RS and the minimum possible value of RS." (NCT00774930)
Timeframe: Baseline and Week 12 of DB phase
| Intervention | Units on a scale (Mean) |
|---|---|
| Lanreotide Autogel (Somatuline Depot) 120 mg | -4.06 |
| Placebo | 0.10 |
"The time from randomisation in Study 726 to the first occurrence of either disease progression (measured using Response Evaluation Criteria In Solid Tumours [RECIST] criteria) or death in Study 726 or in Study 729, or equivalently, the Progression Free Survival (PFS) time.~Tumour assessments for the placebo group after switching to open label lanreotide Autogel were excluded for the purpose of this analysis. Estimation of the median was based on the Kaplan-Meier method." (NCT00842348)
Timeframe: Throughout the study (every 24 weeks and at completion/withdrawal visit)
| Intervention | weeks (Median) |
|---|---|
| Lanreotide Autogel - Randomised Treatment in Study 726 | 154.14 |
| Placebo - Randomised Treatment in Study 726 | 72.00 |
"Adverse events (AEs) that were ongoing from Study 726 at the time of entry into Study 729 were transcribed into the case report form (CRF) for Study 729 with a start date corresponding to the original report of this AE in Study 726. All new AEs that started after the last visit in Study 726 (i.e. irrespective of whether the AE had onset before or after giving informed consent for Study 729) were recorded Study 729.~An AE was considered as a treatment emergent adverse event (TEAE) for Study 729 if:~It was not present prior to receiving the first dose of study treatment in Study 729; or,~It was present prior to receiving the first dose of study treatment in Study 729 but the intensity increased after the first dose of study treatment in Study 729.~Adverse event data are presented in the AE section." (NCT00842348)
Timeframe: Throughout the study until the completion/early discontinuation visit.
| Intervention | participants with any TEAEs (Number) |
|---|---|
| Lanreotide Autogel | 40 |
| Placebo | 46 |
| Total | 86 |
(NCT00891371)
Timeframe: Day 56
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Reduction of at least 50% or normalization - Yes | Reduction of at least 50% or normalization - No | |
| Lanreotide Autogel 120 mg | 54.3 | 45.7 |
(NCT00891371)
Timeframe: Day 28
| Intervention | Percentage of patients (Number) | |
|---|---|---|
| Reduction of at least 50% or normalization - Yes | Reduction of at least 50% or normalization - No | |
| Lanreotide Autogel 120 mg | 44.4 | 55.6 |
(NCT00891371)
Timeframe: Baseline (Day 1), Day 28 and Day 56
| Intervention | Percent change (Mean) | |
|---|---|---|
| Change from Baseline to Day 28 | Change from Baseline to Day 56 | |
| Lanreotide Autogel 120 mg | -25.9 | -30.7 |
"SF36 QOL includes 1 multi-item scale measuring each of 8 health concepts. These scores are summed to produce raw scale scores for each health concept which are transformed to a 0-100 scale. The lower the score the more disability. The higher the score the less disability. There is in addition a single-item measure of Health Transition~IBS-QOL is a self-report QOL measure specific to IBS that can be used to assess impact of IBS and its treatment. This consists of 34 items,each with a 5 point response scale.Individual responses to 34 items are summed and averaged for a total score and transformed to a 0-100 scale with higher scores indicating better IBS specific QOL" (NCT00891371)
Timeframe: Baseline (Day 1), Day 21, Day 28, Day 49 and Day 56
| Intervention | units on a scale (Mean) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SF36 QOL: Physical Functioning (D21), n=33 | SF36 QOL: Physical Functioning (D28), n=34 | SF36 QOL: Physical Functioning (D49), n=26 | SF36 QOL: Physical Functioning (D56), n=35 | SF36 QOL: Role Physical (D21), n=33 | SF36 QOL: Role Physical (D28), n=34 | SF36 QOL: Role Physical (D49), n=26 | SF36 QOL: Role Physical (D56), n=35 | SF36 QOL: Role Emotional (D21), n=33 | SF36 QOL: Role Emotional (D28), n=34 | SF36 QOL: Role Emotional (D49), n=25 | SF36 QOL: Role Emotional (D56), n=35 | SF36 QOL: Vitality (D21), n=32 | SF36 QOL: Vitality (D28), n=33 | SF36 QOL: Vitality (D49), n=24 | SF36 QOL: Vitality (D56), n=34 | SF36 QOL: Mental Health (D21), n=32 | SF36 QOL: Mental Health (D28), n=33 | SF36 QOL: Mental Health (D49), n=24 | SF36 QOL: Mental Health (D56), n=34 | SF36 QOL: Social Functioning (D21), n=31 | SF36 QOL: Social Functioning (D28), n=33 | SF36 QOL: Social Functioning (D49), n=24 | SF36 QOL: Social Functioning (D56), n=33 | SF36 QOL: Bodily Pain (D21), n=33 | SF36 QOL: Bodily Pain (D28), n=34 | SF36 QOL: Bodily Pain (D49), n=26 | SF36 QOL: Bodily Pain (D56), n=35 | SF36 QOL: General Health (D21), n=33 | SF36 QOL: General Health (D28), n=33 | SF36 QOL: General Health (D49), n=26 | SF36 QOL: General Health (D56), n=34 | IBS QOL: Total Score (D21), n=27 | IBS QOL: Total Score (D28), n=26 | IBS QOL: Total Score (D49), n=22 | IBS QOL: Total Score (D56), n=29 | |
| Lanreotide Autogel 120 mg | -1.3 | 2.4 | 2.9 | 1.1 | 4.5 | 12.9 | 6.3 | 11.8 | -0.3 | 3.4 | 7.0 | 5.0 | 3.1 | 5.9 | 2.1 | 7.2 | 5.8 | 8.3 | 8.3 | 10.1 | 9.3 | 16.7 | 19.3 | 14.0 | -4.6 | 8.3 | 8.8 | 5.3 | -2.8 | 2.8 | 4.1 | 3.7 | 9.9 | 13.9 | 16.8 | 16.3 |
Each patient scored his/her stool on the Bristol Stool Form Scale: Type 1 - Separate hard lumps, like nuts (hard to pass); Type 2 - Sausage-shaped but lumpy; Type 3 - Like a sausage but with cracks on its surface; Type 4 - Like a sausage or snake, smooth and soft; Type 5 - Soft blobs with clear-cut edges (passed easily); Type 6 - Fluffy pieces with ragged edges, a mushy stool; Type 7 - Water no solid pieces, Entirely liquid (NCT00891371)
Timeframe: Baseline (day 1), day 28 and day 56
| Intervention | units on a scale (Median) | |
|---|---|---|
| Change from Baseline to Day 28 | Change from Baseline to Day 56 | |
| Lanreotide Autogel 120 mg | 0.0 | -0.5 |
Normalization of stool frequency in subjects with refractory diarrhoea at Day 28 and Day 56 (mean of last 7 days) compared to Baseline. (NCT00891371)
Timeframe: Baseline (Day 1), Day 28 and Day 56
| Intervention | Percentage of days per Week (Mean) | |
|---|---|---|
| Change from Baseline to Day 28 | Change from Baseline to Day 56 | |
| Lanreotide Autogel 120 mg | 27.5 | 33.0 |
Change from CORE baseline at each scheduled assessment was performed for patients randomized to pasireotide arms. Change from extension baseline at each scheduled assessment was performed for patients randomized to active control arm. Standardized IGF-1 = IGF-1 value / ULN, where ULN is the upper limit of the normal range (NCT01137682)
Timeframe: CORE and extension baseline up to approximately 268 weeks
| Intervention | mcg/L (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 extension | Week 28 extension | Week 40 extension | Week 52 extension | Week 64 extension | Week 76 extension | Week 88 extension | Week 100 extension | Week 112 extension | Week 124 extension | Week 136 extension | Week 148 extension | Week 160 extension | Week 172 extension | Week 184 extension | Week 196 extension | Week 208 extension | Week 220 extension | Week 232 extension | Week 244 extension | Week 256 extension | Week 268 extension | |
| Cross Over to Pasireotide Extension | -0.9 | -0.9 | -1.1 | -1.1 | -1.3 | -1.3 | -1.3 | -1.3 | -1.4 | -1.3 | -1.4 | -1.3 | -1.4 | -1.3 | -1.4 | -1.3 | -1.2 | -1.4 | -1.7 | -1.5 | -1.8 | -1.7 |
| Pasireotide LAR 40 mg Extension | -0.8 | -0.9 | -1.1 | -1.1 | -1.3 | -1.3 | -1.3 | -1.4 | -1.5 | -1.4 | -1.4 | -1.4 | -1.4 | -1.5 | -1.3 | -1.4 | -1.4 | -1.4 | -1.4 | -1.3 | -1.3 | -1.4 |
| Pasireotide LAR 60 mg Extension | -1.4 | -1.3 | -1.4 | -1.3 | -1.4 | -1.5 | -1.6 | -1.5 | -1.5 | -1.5 | -1.7 | -1.5 | -1.6 | -1.6 | -1.5 | -1.5 | -1.6 | -1.6 | -1.5 | -1.9 | -1.4 | -1.7 |
The percentage of patients achieving mean growth hormone (GH) levels < 1.0 μg/L and normalization of sex and age-adjusted IGF-1 was calculated with two sided 95% confidence interval. All GH assessments were based on a 5-point mean growth hormone (GH) assessed from a 2-hour profile. Scheduled time points for blood sampling were pre-dose at 0, 30, 60, 90 and 120 minutes. Total insulin-like growth factor (IGF-1) levels were assessed with one pre-dose sample at the same visits as GH. Concomitant medication known to affect GH or IGF-1 levels were allowed in patients who were not biochemically controlled after at least one year treatment with pasireotide LAR monotherapy: dopamine agonists and growth hormone receptor antagonists (Extension full analysis set (NCT01137682)
Timeframe: Extension baseline up to approximately week 268
| Intervention | Participants (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 | Week 28 | Week 40 | Week 52 | Week 64 | Week 76 | Week 88 | Week 100 | Week 112 | Week 124 | Week 136 | Week 148 | Week 160 | Week 172 | Week 184 | Week 196 | Week 208 | Week 220 | Week 232 | Week 244 | Week 256 | Week 268 | |
| Cross Over to Pasireotide Extension | 6.5 | 8.1 | 4.8 | 4.8 | 9.7 | 6.5 | 4.8 | 8.1 | 9.7 | 8.1 | 11.3 | 8.1 | 9.7 | 8.1 | 3.2 | 8.1 | 6.5 | 6.5 | 4.8 | 6.5 | 3.2 | 1.6 |
| Pasireotide LAR 40 mg Extension | 10.5 | 8.8 | 10.5 | 8.8 | 8.8 | 10.5 | 7.0 | 12.3 | 14.0 | 7.0 | 3.5 | 10.5 | 8.8 | 14.0 | 7.0 | 8.8 | 8.8 | 10.5 | 10.5 | 8.8 | 8.8 | 1.8 |
| Pasireotide LAR 60 mg Extension | 16.7 | 14.8 | 9.3 | 13.0 | 13.0 | 13.0 | 20.4 | 14.8 | 20.4 | 14.8 | 18.5 | 14.8 | 14.8 | 13.0 | 13.0 | 13.0 | 9.3 | 7.4 | 3.7 | 3.7 | 3.7 | 3.7 |
The percentage of patients achieving mean growth hormone (GH) levels < 2.5 μg/L and normalization of sex and age-adjusted IGF-1 was calculated with two sided 95% confidence interval. All GH assessments were based on a 5-point mean growth hormone (GH) assessed from a 2-hour profile. Scheduled time points for blood sampling were pre-dose at 0, 30, 60, 90 and 120 minutes. Total insulin-like growth factor (IGF-1) levels were assessed with one pre-dose sample at the same visits as GH. Concomitant medication known to affect GH or IGF-1 levels were allowed in patients who were not biochemically controlled after at least one year treatment with pasireotide LAR monotherapy: dopamine agonists and growth hormone receptor antagonists (extension full analysis set) (NCT01137682)
Timeframe: Extension baseline up to approximately week 268
| Intervention | percentage of participants (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 | Week 28 | Week 40 | Week 52 | Week 64 | Week 76 | Week 88 | Week 100 | Week 112 | Week 124 | Week 136 | Week 148 | Week 160 | Week 172 | Week 184 | Week 196 | Week 208 | Week 220 | Week 232 | Week 244 | Week 256 | Week 268 | |
| Cross Over to Pasireotide Extension | 19.4 | 19.4 | 17.7 | 21.0 | 25.8 | 27.4 | 25.8 | 32.3 | 25.8 | 25.8 | 29.0 | 29.0 | 30.6 | 21.0 | 17.7 | 24.2 | 19.4 | 14.5 | 14.5 | 11.3 | 3.2 | 1.6 |
| Pasireotide LAR 40 mg Extension | 19.3 | 17.5 | 21.1 | 21.1 | 22.8 | 21.1 | 24.6 | 24.6 | 24.6 | 21.1 | 15.8 | 21.1 | 19.3 | 22.8 | 17.5 | 15.8 | 17.5 | 21.1 | 14.0 | 14.0 | 10.5 | 5.3 |
| Pasireotide LAR 60 mg Extension | 25.9 | 25.9 | 27.8 | 29.6 | 20.4 | 29.6 | 31.5 | 24.1 | 25.9 | 24.1 | 24.1 | 20.4 | 20.4 | 20.4 | 20.4 | 20.4 | 18.5 | 11.1 | 14.8 | 7.4 | 7.4 | 5.6 |
The percentage of patients achieving mean growth hormone (GH) levels < 1.0 μg/L was calculated with two sided 95% confidence interval. All GH assessments were based on a 5-point mean growth hormone (GH) assessed from a 2-hour profile. Scheduled time points for blood sampling were pre-dose at 0, 30, 60, 90 and 120 minutes. Concomitant medication known to affect GH levels were allowed in patients who were not biochemically controlled after at least one year treatment with pasireotide LAR monotherapy: dopamine agonists and growth hormone receptor antagonists (Extension full analysis set) (NCT01137682)
Timeframe: Extension baseline up to approximately week 268
| Intervention | percentage of participants (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 | Week 28 | Week 40 | Week 52 | Week 64 | Week 76 | Week 88 | Week 100 | Week 112 | Week 124 | Week 136 | Week 148 | Week 160 | Week 172 | Week 184 | Week 196 | Week 208 | Week 220 | Week 232 | Week 244 | Week 256 | Week 268 | |
| Cross Over to Pasireotide Extension | 8.1 | 9.7 | 4.8 | 9.7 | 11.3 | 11.3 | 11.3 | 17.7 | 16.1 | 14.5 | 14.5 | 14.5 | 14.5 | 14.5 | 6.5 | 12.9 | 9.7 | 9.7 | 8.1 | 8.1 | 4.8 | 1.6 |
| Pasireotide LAR 40 mg Extension | 14.0 | 14.0 | 14.0 | 12.3 | 15.8 | 12.3 | 15.8 | 17.5 | 17.5 | 12.3 | 8.8 | 14.0 | 17.5 | 17.5 | 17.5 | 15.8 | 17.5 | 15.8 | 15.8 | 12.3 | 12.3 | 3.5 |
| Pasireotide LAR 60 mg Extension | 27.8 | 22.2 | 13.0 | 22.2 | 18.5 | 22.2 | 22.2 | 20.4 | 25.9 | 16.7 | 25.9 | 16.7 | 18.5 | 14.8 | 18.5 | 13.0 | 13.0 | 11.1 | 3.7 | 5.6 | 3.7 | 3.7 |
"PK samples were collected for those patients treated with pasireotide LAR in the core study and who continued on pasireotide LAR in the extension phase. PK samples were collected before the injection of pasireotide LAR only at weeks 112 and 196. PK samples were also collected at weeks 48 and 132 only for all patients treated with octreotide LAR 30 mg or lanreotide ATG 120 mg in the core study who started treatment with pasireotide LAR in the extension study.~Blood samples (2.5 mL each sample) were collected to yield 1-mL plasma for analysis of pasireotide LAR oncentration." (NCT01137682)
Timeframe: Extension baseline up to approximately 196 weeks
| Intervention | mL (Mean) | |
|---|---|---|
| Week 112 | Week 196 | |
| Pasireotide LAR 60 mg | 14.06 | 14.96 |
"PK samples were collected for those patients treated with pasireotide LAR in the core study and who continued on pasireotide LAR in the extension phase. PK samples were collected before the injection of pasireotide LAR only at weeks 112 and 196. PK samples were also collected at weeks 48 and 132 only for all patients treated with octreotide LAR 30 mg or lanreotide ATG 120 mg in the core study who started treatment with pasireotide LAR in the extension study.~Blood samples (2.5 mL each sample) were collected to yield 1-mL plasma for analysis of pasireotide LAR oncentration." (NCT01137682)
Timeframe: Extension baseline up to approximately 196 weeks
| Intervention | mL (Mean) | |||
|---|---|---|---|---|
| Week 48 | Week 112 | Week 132 | Week 196 | |
| Pasireotide LAR 40 mg | 5.70 | 8.66 | 9.28 | 10.32 |
The percentage of patients achieving normalization of sex and age-adjusted IGF-1 was calculated with two sided 95% confidence interval. Total insulin-like growth factor (IGF-1) levels were assessed with one pre-dose sample at the same visits as GH. Concomitant medication known to affect IGF-1 levels were allowed in patients who were not biochemically controlled after at least one year treatment with pasireotide LAR monotherapy: dopamine agonists and growth hormone receptor antagonists (Extension full analysis set) (NCT01137682)
Timeframe: Extension baseline up to approximately week 268
| Intervention | percentage of participants (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 | Week 28 | Week 40 | Week 52 | Week 64 | Week 76 | Week 88 | Week 100 | Week 112 | Week 124 | Week 136 | Week 148 | Week 160 | Week 172 | Week 184 | Week 196 | Week 208 | Week 220 | Week 232 | Week 244 | Week 256 | Week 268 | |
| Cross Over to Pasireotide Extension | 25.8 | 22.6 | 24.2 | 25.8 | 29.0 | 29.0 | 25.8 | 32.3 | 30.6 | 29.0 | 37.1 | 33.9 | 33.9 | 22.6 | 22.6 | 27.4 | 21.0 | 19.4 | 17.7 | 14.5 | 6.5 | 1.6 |
| Pasireotide LAR 40 mg Extension | 33.3 | 29.8 | 36.8 | 28.1 | 33.3 | 26.3 | 28.1 | 31.6 | 31.6 | 24.6 | 21.1 | 26.3 | 24.6 | 26.3 | 19.3 | 24.6 | 22.8 | 22.8 | 14.0 | 14.0 | 12.3 | 5.3 |
| Pasireotide LAR 60 mg Extension | 29.0 | 33.3 | 37.0 | 33.3 | 27.8 | 35.2 | 35.2 | 29.6 | 27.8 | 31.5 | 25.9 | 22.2 | 25.9 | 22.2 | 22.2 | 22.2 | 22.2 | 11.1 | 14.8 | 9.3 | 7.4 | 5.6 |
Change from CORE baseline at each scheduled assessment was performed for patients randomized to pasireotide arms. Change from extension baseline at each scheduled assessment was performed for patients randomized to active control arm. (NCT01137682)
Timeframe: CORE and extension baseline up to approximately 268 weeks
| Intervention | mcg/L (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 - extension | Week 28 - extension | Week 40 - extension | Week 52 - extension | Week 64 - extension | Week 76 - extension | Week 88 - extension | Week 100 - extension | Week 112 - extension | Week 124 - extension | Week 136 - extension | Week 148 - extension | Week 160 - extension | Week 172 - extension | Week 184 - extension | Week 196 - extension | Week 208 - extension (n=22,20,23) | Week 220 - extension | Week 232 - extension | Week 244 - extension | Week 256 - extension | Week 268 - extension | |
| Cross Over to Pasireotide Extension | -8.4 | -3.0 | -11.2 | -2.5 | -15.7 | -3.5 | -3.6 | -3.8 | -3.9 | -4.0 | -4.0 | -3.8 | -3.2 | -3.0 | -3.3 | -3.4 | -3.5 | -3.8 | -4.2 | -4.2 | -5.0 | -3.7 |
| Pasireotide LAR 40 mg Extension | -7.9 | -9.0 | -9.7 | -10.7 | -11.3 | -5.5 | -5.7 | -5.6 | -5.8 | -5.5 | -6.0 | -6.3 | -5.5 | -6.3 | -6.3 | -7.1 | -7.0 | -7.1 | -5.7 | -6.0 | -6.4 | -3.6 |
| Pasireotide LAR 60 mg Extension | -6.9 | -4.5 | -5.8 | -7.1 | -7.9 | -7.2 | -6.2 | -5.3 | -4.4 | -6.0 | -5.3 | 6.1 | -4.9 | -5.9 | -5.8 | -6.5 | -6.2 | -7.1 | -6.8 | -2.4 | -4.9 | -2.5 |
(NCT01137682)
Timeframe: CORE baseline up to approximately 24 weeks
| Intervention | mcg/L (Mean) | |
|---|---|---|
| Week 12 - CORE | Week 24 - CORE | |
| Pasireotide LAR 40 mg | -0.8 | -0.6 |
| Pasireotide LAR 60 mg | -6.4 | -7.2 |
The percentage of patients achieving mean growth hormone (GH) levels < 2.5 μg/L was calculated with two sided 95% confidence interval. All GH assessments were based on a 5-point mean growth hormone (GH) assessed from a 2-hour profile. Scheduled time points for blood sampling were pre-dose at 0, 30, 60, 90 and 120 minutes. Concomitant medication known to affect GH levels were allowed in patients who were not biochemically controlled after at least one year treatment with pasireotide LAR monotherapy: dopamine agonists and growth hormone receptor antagonists (Extension full analysis set) (NCT01137682)
Timeframe: Extension baseline up to approximately week 268
| Intervention | percentage of participants (Number) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 | Week 28 | Week 40 | Week 52 | Week 64 | Week 76 | Week 88 | Week 100 | Week 112 | Week 124 | Week 136 | Week 148 | Week 160 | Week 172 | Week 184 | Week 196 | Week 208 | Week 220 | Week 232 | Week 244 | Week 256 | Week 268 | |
| Control Arm (Octreotide or Lanreotide) Extension | 33.9 | 43.5 | 40.3 | 41.9 | 41.9 | 45.2 | 45.2 | 46.8 | 40.3 | 41.9 | 43.5 | 43.5 | 40.3 | 38.7 | 33.9 | 35.5 | 25.8 | 22.6 | 21.0 | 12.9 | 6.5 | 3.2 |
| Pasireotide LAR 40 mg Extension | 38.6 | 40.4 | 38.6 | 38.6 | 40.4 | 33.3 | 40.4 | 40.4 | 36.8 | 40.4 | 36.8 | 40.4 | 38.6 | 40.4 | 33.3 | 29.8 | 31.6 | 29.8 | 24.6 | 19.3 | 15.8 | 7.0 |
| Pasireotide LAR 60 mg Extension | 55.6 | 44.4 | 42.6 | 46.3 | 37.0 | 44.4 | 42.6 | 40.7 | 44.4 | 31.5 | 35.2 | 33.3 | 33.3 | 37.0 | 31.5 | 29.6 | 24.1 | 18.5 | 18.5 | 11.1 | 9.3 | 5.6 |
Standardized IGF-1 = IGF-1 value / ULN, where ULN is the upper limit of the normal range (NCT01137682)
Timeframe: CORE baseline up to approximately 24 weeks
| Intervention | mcg/L (Mean) | |
|---|---|---|
| CORE Week 12 | CORE Week 24 | |
| Pasireotide LAR 40 mg | 0.7 | -0.7 |
| Pasireotide LAR 60 mg | -1.1 | -1.1 |
Acromegaly Quality of Life questionnaire (AcroQoL) is a validated disease specific questionnaire. It contains 22 items divided into two scales: physical aspects (8 items) and psychological aspects (14 items) which is divided in two sub-scales: physical appearance and personal relationships of the patient (seven items each). The total score and sub-scores were calculated using the following formula: ((X -Y) / 4Y) x 100, X=sum of the scores for individual items (between 1 and 5 for each item), Y=number of individual items included in above sum (i.e. 22 for the total score, 8 for the physical sub-score, 14 for the psychological sub-score, 7 for the sub-score 'appearance' and 'personal relations'). The scoring of the questionnaire was performed as specified by the instrument developers. Total scores range from 0 to 100. Higher scores represent better quality of life. If more than 25% of items are not completed, results were considered invalid. (NCT01137682)
Timeframe: CORE baseline up to approximately 24 weeks
| Intervention | scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Week 4 CORE | Week 8 CORE | Week 12 CORE | Week 16 CORE | Week 20 CORE | Week24 CORE | |
| Pasireotide LAR 40 mg | 3.5 | 2.4 | 3.0 | 3.3 | 3.5 | 3.0 |
| Pasireotide LAR 60 mg | 2.3 | 2.5 | 1.9 | 6.6 | 4.0 | 5.4 |
Time to first response is defined as the time from the date of first dose to the date of first occurrence of a reduction of mean GH < 2.5 µg/L and the normalization of IGF-1. The weeks correspond to time taken to achieve first mean GH < 2.5 µg/L and the normalization of IGF-1. (NCT01137682)
Timeframe: CORE baseline up to approximately 268 weeks
| Intervention | weeks (Median) |
|---|---|
| Pasireotide LAR 40 mg Extension | 112.3 |
| Pasireotide LAR 60 mg Extension | 65.3 |
| Cross Over to Pasireotide Extension | 95.1 |
The primary objective of this study was to compare the percentage of patients achieving biochemical control (defined as mean GH levels <2.5 µg/L and normalization of sex- and age- adjusted IGF-1) at 24 weeks with pasireotide LAR 40 mg and pasireotide LAR 60 mg separately versus continued treatment with octreotide LAR 30 mg or lanreotide autogel (ATG) 120 mg. The primary efficacy variable is the proportion of patients with a reduction of mean GH levels to < 2.5 µg/L and normalization of sex- and age-adjusted IGF-1 at 24 weeks. (NCT01137682)
Timeframe: At 24 weeks
| Intervention | percentage of participants (Number) |
|---|---|
| Pasireotide LAR 40 mg | 15.4 |
| Pasireotide LAR 60 mg | 20.0 |
| Control Arm (Octreotide or Lanreotide) | 0 |
n is the number of patients achieving response criteria. The weeks correspond to duration of first response (in weeks) for patients achieving biomedical control. Median and 95% CI are derived from Kaplan-Meier curves. Kaplan-Meier estimates [95% CI] at each time point are estimates of probability of response. (NCT01137682)
Timeframe: CORE baseline up to approximately 268 weeks
| Intervention | weeks (Median) |
|---|---|
| Pasireotide LAR 40 mg Extension | 29.1 |
| Pasireotide LAR 60 mg Extension | 26.9 |
| Cross Over to Pasireotide Extension | 24.9 |
Acromegaly Quality of Life questionnaire (AcroQoL) is a validated disease specific questionnaire. It contains 22 items divided into two scales: physical aspects (8 items) and psychological aspects (14 items) which is divided in two sub-scales: physical appearance and personal relationships of the patient (seven items each). The total score and sub-scores were calculated using the following formula: ((X -Y) / 4Y) x 100, X=sum of the scores for individual items (between 1 and 5 for each item), Y=number of individual items included in above sum (i.e. 22 for the total score, 8 for the physical sub-score, 14 for the psychological sub-score, 7 for the sub-score 'appearance' and 'personal relations'). The scoring of the questionnaire was performed as specified by the instrument developers. Total scores range from 0 to 100. Higher scores represent better quality of life. If more than 25% of items are not completed, results were considered invalid. (NCT01137682)
Timeframe: CORE Baseline and extension baseline up to approximately 268 weeks
| Intervention | scores on a scale (Mean) | |||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 16 extension | Week 28 extension | Week 40 extension | Week 52 extension | Week 64 extension | Week 76 extension | Week 88 extension | Week 100 extension | Week 112 extension | Week 124 extension | Week 136 extension | Week 148 extension | Week 160 extension | Week 172 extension | Week 184 extension | Week 196 extension | Week 208 extension | Week 220 extension | Week 232 extension | Week 244 extension | Week 256 extension | Week 268 extension | |
| Cross Over to Pasireotide Extension | 0.8 | 3.3 | 3.2 | 4.2 | 5.4 | 7.7 | 6.4 | 5.9 | 4.1 | 2.0 | 6.5 | 5.5 | 1.5 | 2.1 | 1.6 | 3.8 | 4.5 | 7.3 | 7.0 | 3.0 | 0.3 | -10.6 |
| Pasireotide LAR 40 mg Extension | 4.2 | 5.6 | 3.2 | 6.1 | 5.8 | 7.7 | 4.6 | 4.3 | 4.6 | 5.8 | 7.5 | 7.6 | 7.0 | 4.8 | 5.8 | 6.1 | 1.2 | 4.8 | 2.1 | 4.5 | 6.1 | 0.6 |
| Pasireotide LAR 60 mg Extension | 2.9 | 4.8 | 2.5 | 5.7 | 4.2 | 2.5 | 5.6 | 3.9 | 6.5 | 2.0 | 5.4 | 6.8 | 5.1 | 5.7 | 5.8 | 6.0 | 6.2 | 5.8 | -0.2 | 6.3 | -3.0 | -4.9 |
We evaluated cost-effectiveness of combination low-dose SRL and weekly or daily pegvisomant compared to combination high-dose SRL and weekly pegvisomant by assessing cost of therapy per month in each treatment arm among patients who achieved normal IGF-1 levels. (NCT01538966)
Timeframe: 24 weeks
| Intervention | US dollars/month (Mean) |
|---|---|
| High Dose SRL + Weekly Pegvisomant | 14,261.33 |
| Low Dose SRL + Daily Pegvisomant | 22,542.86 |
| Low Dose SRL + Weekly Pegvisomant | 9,836.52 |
"Subjects underwent CT or MRI scans at baseline and Week 53. Progression was assessed by investigators using RECIST v1.1. The best overall response to study treatment is the highest time point response achieved by the subject and was assessed as a complete response, partial response, stable disease, progressive disease or non evaluable. For analysis of PFS, event dates were assigned to the first time that progressive disease was noted or the date of death. In case of progressive disease followed by death, the first event was considered in the analysis. Censoring dates were defined in subjects with no progressive disease or death before end of study.~At one year (end of study), the mean percentage of subjects who were alive and progression free, as calculated using the Kaplan-Meier method, is reported by CTC presence and overall." (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | percentage of subjects (Mean) |
|---|---|
| CTC Presence at Baseline | 69.00 |
| No CTC Presence at Baseline | 67.75 |
| Lanreotide Autogel | 66.43 |
"This endpoint was assessed using 2 efficacy variables:~CTCs, enumerated at baseline and Weeks 5, 17, 25, 53~Clinical symptomatic response, assessed by the use of symptom reporting~Subjects recorded 24-hour symptom frequency and severity for 7 days prior to first treatment (baseline), throughout the study, and up to 28 days following final drug administration. Symptoms were recorded by answering predetermined questions on the interactive voice response system (IVRS).~Subjects were considered to have a clinical symptomatic response between baseline and last study visit if any 1 of the following criteria were fulfilled: the average number of episodes of diarrhoea decreased by at least 50%, the average number of episodes of flushing decreased by at least 50%, the mode severity of flushing decreased by at least 1 level. Clinical symptomatic response was assessed as a qualitative variable (Yes/No) and reported according to CTC presence at baseline and overall." (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | Percentage of Subjects (Number) | |
|---|---|---|
| Clinical Symptomatic Response = Yes(2) | Clinical Symptomatic Response = No(3) | |
| CTC Presence at Baseline | 77.8 | 22.2 |
| Lanreotide Autogel | 87.5 | 12.5 |
| No CTC Presence at Baseline | 95.5 | 4.5 |
"The effect of lanreotide Autogel on the symptoms of diarrhoea and flushing in subjects was assessed through subject reporting of symptoms every 24-hours for the 7 days prior to treatment (baseline), for the first 16 weeks and on days 11 to 17 after each subsequent injection interval. After the final study drug injection at Week 49, subjects provided 24-hour symptom frequency on days 11 to 28 (up to Week 53). Symptom frequency was recorded by answering predetermined questions on the IVRS.~Mean change from baseline in frequency (number of episodes) of diarrhoea and flushing are described at Visit 2 (average number of episodes in Week 1) and at Visit 14 (average number of episodes over days 11 to 17 after Week 49 injection and over days 11 to 28 after Week 49 injection) by CTC presence at baseline and overall. A negative change indicates an improvement in symptoms from baseline." (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | number of episodes (Mean) | |
|---|---|---|
| Diarrhoea: Visit 2 (daily) | Flushing: Visit 2 (daily) | |
| Missing CTC Status at Baseline | 0.38 | 0.00 |
"The effect of lanreotide Autogel on the symptoms of diarrhoea and flushing in subjects was assessed through subject reporting of symptoms every 24-hours for the 7 days prior to treatment (baseline), for the first 16 weeks and on days 11 to 17 after each subsequent injection interval. After the final study drug injection at Week 49, subjects provided 24-hour symptom frequency on days 11 to 28 (up to Week 53). Symptom frequency was recorded by answering predetermined questions on the IVRS.~Mean change from baseline in frequency (number of episodes) of diarrhoea and flushing are described at Visit 2 (average number of episodes in Week 1) and at Visit 14 (average number of episodes over days 11 to 17 after Week 49 injection and over days 11 to 28 after Week 49 injection) by CTC presence at baseline and overall. A negative change indicates an improvement in symptoms from baseline." (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | number of episodes (Mean) | |||||
|---|---|---|---|---|---|---|
| Diarrhoea: Visit 2 (daily) | Diarrhoea: Visit 14 (days 11-17) | Diarrhoea: Visit 14 (days 11-28) | Flushing: Visit 2 (daily) | Flushing: Visit 14 (days 11-17) | Flushing: Visit 14 (days 11-28) | |
| CTC Presence at Baseline | -0.66 | -1.91 | -2.15 | -1.76 | -3.37 | -3.49 |
| Lanreotide Autogel | -0.42 | -1.18 | -1.30 | -1.43 | -2.88 | -2.79 |
| No CTC Presence at Baseline | -0.27 | -0.64 | -0.63 | -1.25 | -2.51 | -2.23 |
The effect of lanreotide Autogel on the mode severity of flushing was assessed through subject reporting of symptoms every 24-hours for the 7 days prior to treatment (baseline), for the first 16 weeks and on days 11 to 17 after each subsequent injection interval until Week 49. After the final study drug injection at Week 49, subjects provided 24-hour symptom severity on days 11 to 28 (up to Week 53). Symptom severity was recorded by answering predetermined questions on the IVRS using a three-point system (mild, moderate or severe). The mode (most frequent) intensity of flushing are reported at baseline and at Visit 14 (average number of episodes over days 11 to 17 after Week 49 injection and over days 11 to 28 after Week 49 injection). Percentages of subjects in each severity category are based on the number of subjects in the analysis set with available responses. Data is presented according to CTC presence at baseline and overall. (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | percentage of subjects (Number) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| No flushing: Baseline | Mild: Baseline | Moderate: Baseline | Severe: Baseline | No flushing: Visit 14 (days 11-17) | Mild: Visit 14 (days 11-17) | Moderate: Visit 14 (days 11-17) | Severe: Visit 14 (days 11-17) | No flushing: Visit 14 (days 11-28) | Mild: Visit 14 (days 11-28) | Moderate: Visit 14 (days 11-28) | Severe: Visit 14 (days 11-28) | |
| CTC Presence at Baseline | 22.7 | 27.3 | 45.5 | 4.5 | 37.5 | 43.8 | 18.8 | 0.0 | 13.3 | 60.0 | 26.7 | 0.0 |
| Lanreotide Autogel | 14.0 | 38.0 | 46.0 | 2.0 | 32.4 | 45.9 | 21.6 | 0.0 | 23.5 | 55.9 | 17.6 | 2.9 |
| No CTC Presence at Baseline | 0.0 | 50.0 | 50.0 | 0.0 | 28.6 | 47.6 | 23.8 | 0.0 | 31.6 | 52.6 | 10.5 | 5.3 |
The effect of lanreotide Autogel on the mode severity of flushing was assessed through subject reporting of symptoms every 24-hours for the 7 days prior to treatment (baseline), for the first 16 weeks and on days 11 to 17 after each subsequent injection interval until Week 49. After the final study drug injection at Week 49, subjects provided 24-hour symptom severity on days 11 to 28 (up to Week 53). Symptom severity was recorded by answering predetermined questions on the IVRS using a three-point system (mild, moderate or severe). The mode (most frequent) intensity of flushing are reported at baseline and at Visit 14 (average number of episodes over days 11 to 17 after Week 49 injection and over days 11 to 28 after Week 49 injection). Percentages of subjects in each severity category are based on the number of subjects in the analysis set with available responses. Data is presented according to CTC presence at baseline and overall. (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | percentage of subjects (Number) | |||
|---|---|---|---|---|
| No flushing: Baseline | Mild: Baseline | Moderate: Baseline | Severe: Baseline | |
| Missing CTC Status at Baseline | 100 | 0.0 | 0.0 | 0.0 |
"Subjects underwent Computed Tomography (CT) or Magnetic Resonance Imaging (MRI) scans at baseline, Visit 8 (Week 25) and Visit 15 (Week 53). Progression was assessed by investigators using RECIST v1.1, and classified as a complete response, partial response, stable disease, progressive disease or non evaluable.~The time point responses at Week 25 and Week 53 were analysed by CTC presence at baseline and overall. The percentage of subjects within each response category are presented. Percentages are based on the number of subjects in the concerned population with available responses." (NCT02075606)
Timeframe: Week 25 and Week 53.
| Intervention | percentage of subjects (Number) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Week 25: Complete Response | Week 25: Partial Response | Week 25: Stable Disease | Week 25: Progressive Disease | Week 25: Non evaluable | Week 53: Complete Response | Week 53: Partial Response | Week 53: Stable Disease | Week 53: Progressive Disease | Week 53: Non evaluable | |
| CTC Presence at Baseline | 0.0 | 18.2 | 72.7 | 9.1 | 0.0 | 0.0 | 6.7 | 66.7 | 26.7 | 0.0 |
| Lanreotide Autogel | 0.0 | 13.0 | 73.9 | 13.0 | 0.0 | 0.0 | 5.4 | 64.9 | 29.7 | 0.0 |
| No CTC Presence at Baseline | 0.0 | 8.3 | 75.0 | 16.7 | 0.0 | 0.0 | 4.5 | 63.6 | 31.8 | 0.0 |
The effect of lanreotide Autogel treatment on QoL was assessed using the EORTC QLQ-G.I.NET21 at baseline, Weeks 13 (Visit 5), 25 (Visit 8) and 53 (Visit 15/end of study). The QLQ-G.I.NET21 questionnaire contained 21 questions that used a 4-point scale (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much) to evaluate 3 defined multi-item symptom scales (endocrine, gastrointestinal and treatment related side effects), 2 single item symptoms (bone/muscle pain and concern about weight loss), 2 psychosocial scales (social function and disease-related worries) and 2 other single items (sexuality and communication). Each individual subscore was transformed to range from 0 to 100. Higher scores indicate worse symptoms or more problems. The mean change from baseline at each time point is reported for each of the category subscores. (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | Units on a scale (Mean) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Endocrine symptoms: Visit 5 | Endocrine symptoms: Visit 8 | Endocrine symptoms: End of study | Gastrointestinal symptoms: Visit 5 | Gastrointestinal symptoms: Visit 8 | Gastrointestinal symptoms: End of study | Treatment symptoms: Visit 5 | Treatment symptoms: Visit 8 | Treatment symptoms: End of study | Social function: Visit 5 | Social function: Visit 8 | Social function: End of study | Disease related worries: Visit 5 | Disease related worries: Visit 8 | Disease related worries: End of study | Muscle/Bone pain: Visit 5 | Muscle/Bone pain: Visit 8 | Muscle/Bone pain: End of study | Sexual function: Visit 5 | Sexual function: Visit 8 | Sexual function: End of study | Information/communication function: Visit 5 | Information/communication function: Visit 8 | Information/communication function: End of study | Body image: Visit 5 | Body image: Visit 8 | Body image: End of study | |
| Lanreotide Autogel | -15.4 | -17.0 | -16.0 | 2.1 | 1.2 | 1.0 | 1.2 | 7.6 | 12.0 | -11.3 | -6.5 | -4.5 | -14.1 | -15.9 | -12.2 | -7.9 | -6.5 | -11.8 | -5.6 | -8.9 | -13.3 | -8.5 | -3.7 | -5.6 | 0.9 | 1.9 | -1.0 |
"The effect of lanreotide Autogel treatment on QoL was assessed using the EORTC QLQ-C30 at baseline, Weeks 13 (Visit 5), 25 (Visit 8) and 53 (Visit 15/end of study). The 30 item scale is divided into 9 multi item scales (including 5 functional scales, 1 global health status/QoL scale and 3 general symptom scales) and 6 single items. Possible answers to the first 28 items (all items except the 2 concerning global quality of life) go from 1 (Not at all) to 4 (Very much). The answers for the 2 last questions (Q29- 30) go from 1 (Very poor) to 7 (Excellent). All of the scales and single-item measures range in score from 0 to 100. For multi-item scales, the raw score will be calculated by the addition of item responses divided by the number of items. Higher scores for global health and functional domains indicate a better QoL, while higher symptom scores indicate worse symptoms.~The mean change from baseline at each time point is reported for each of the category subscores." (NCT02075606)
Timeframe: From baseline up to Week 53.
| Intervention | Units on a scale (Mean) | ||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical functioning: Visit 5 | Physical functioning: Visit 8 | Physical functioning: End of study | Role functioning: Visit 5 | Role functioning: Visit 8 | Role functioning: End of study | Emotional functioning: Visit 5 | Emotional functioning: Visit 8 | Emotional functioning: End of study | Cognitive functioning: Visit 5 | Cognitive functioning: Visit 8 | Cognitive functioning: End of study | Social functioning: Visit 5 | Social functioning: Visit 8 | Social functioning: End of study | Global QoL: Visit 5 | Global QoL: Visit 8 | Global QoL: End of study | Fatigue: Visit 5 | Fatigue: Visit 8 | Fatigue: End of study | Nausea and vomiting: Visit 5 | Nausea and vomiting: Visit 8 | Nausea and vomiting: End of study | Pain: Visit 5 | Pain: Visit 8 | Pain: End of study | Dyspnoea: Visit 5 | Dyspnoea: Visit 8 | Dyspnoea: End of study | Insomnia: Visit 5 | Insomnia: Visit 8 | Insomnia: End of study | Appetite loss: Visit 5 | Appetite loss: Visit 8 | Appetite loss: End of study | Constipation: Visit 5 | Constipation: Visit 8 | Constipation: End of study | Diarrhoea: Visit 5 | Diarrhoea: Visit 8 | Diarrhoea: End of study | Financial difficulties: Visit 5 | Financial difficulties: Visit 8 | Financial difficulties: End of study | |
| Lanreotide Autogel | 1.2 | 2.0 | 1.9 | 1.3 | 3.2 | -1.4 | 6.1 | 4.3 | 1.1 | -0.9 | 1.5 | -2.4 | 10.0 | 4.5 | 3.9 | 12.5 | 7.4 | 4.3 | -4.4 | -6.3 | -4.2 | -4.2 | -1.4 | -0.9 | -7.9 | -2.3 | 1.8 | -3.5 | 1.0 | -4.8 | -6.3 | -5.7 | -2.9 | -0.9 | -6.5 | -0.0 | 1.9 | -1.0 | 1.9 | -18.5 | -12.7 | -10.8 | -6.7 | -4.0 | -1.0 |
"Symptomatic response was evaluated as absolute change from baseline in the number of episodes of the lead symptoms (i.e. diarrhoea and flushing) using the mean of the last 3 days before the visit, at each visit, as compared to baseline.~Symptomatic responses were categorised as: Reduction, Increase or Stability of occurrences of diarrhoea / Reduction, Increase or Stability of occurrences of flushing.~The number of subjects in each response category at week 48 (end of study) is presented. Analysis was only carried out on subjects in the ITT population with functioning NET." (NCT02231762)
Timeframe: 12 months
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| Diarrhoea - Reduction | Diarrhoea - Increase | Diarrhoea - Stability | Diarrhoea - Missing | Flushing - Reduction | Flushing - Increase | Flushing - Stability | Flushing - Missing | |
| Maintenance Phase - Functioning NET, Lanreotide | 4 | 1 | 3 | 3 | 2 | 3 | 3 | 3 |
"Symptomatic response was evaluated as absolute change from baseline in the number of episodes of the lead symptoms (i.e. diarrhoea and flushing) using the mean of the last 3 days before the visit, at each visit, as compared to baseline.~Symptomatic responses were categorised as: Reduction, Increase or Stability of occurrences of diarrhoea / Reduction, Increase or Stability of occurrences of flushing.~The number of subjects in each response category at week 24 (end of the combination phase) is presented. Analysis was only carried out on subjects in the ITT population with functioning NET." (NCT02231762)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| Diarrhoea - Reduction | Diarrhoea - Increase | Diarrhoea - Stability | Diarrhoea - Missing | Flushing - Reduction | Flushing - Increase | Flushing - Stability | Flushing - Missing | |
| Combination Phase - Functioning NET | 4 | 2 | 5 | 6 | 4 | 4 | 3 | 6 |
"Urine samples for 5-HIAA urinary tumour marker analysis were taken at at baseline, weeks 12, 24and early withdrawal.~Biochemical response based on 5-HIAA levels was categorised as: Response (5-HIAA reduction compared to baseline) or Progression (5-HIAA increase compared to baseline).~The number of subjects in each response category at each time point in the combination phase is presented. Analysis was only carried out on subjects in the ITT population with functioning NET." (NCT02231762)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 12 - Progression | Week 12 - Response | Week 12 - Not evaluable | Week 12 - Missing | Week 24 - Progression | Week 24 - Response | Week 24 - Not evaluable | Week 24 - Missing | Early Withdrawal - Progression | Early Withdrawal - Response | Early Withdrawal - Not Evaluable | Early Withdrawal - Missing | |
| Combination Phase - Functioning NET | 4 | 6 | 1 | 6 | 6 | 3 | 1 | 3 | 0 | 1 | 0 | 7 |
"All tumour assessments were performed using the RECIST criteria (1.1). CT-scan or MRI could be used for as method of tumour measurement and the same method of tumour measurement was used throughout the study for each subject. CT scans/MRI were performed at screening or baseline visit then at baseline, weeks 12, 24, 36, 48 (end of study) and at study withdrawal or at anytime during the study in the case of any clinical or biological signs of tumour progression.~The DCR was defined as the proportion of subjects with a response of CR, PR or SD after 6 months combination treatment followed by either 6 months of lanreotide ATG 120 mg maintenance treatment or no treatment. The DCR was described in the ITT population along with its 95% CI and was compared to 45% with an exact binomial proportion test. The LOCF method was used to replace missing assessments at the end of the maintenance phase." (NCT02231762)
Timeframe: 12 months
| Intervention | percentage of subjects (Number) |
|---|---|
| Maintenance Phase - Functioning NET, Lanreotide | 54.5 |
| Maintenance Phase - Non-functioning NET, Lanreotide | 71.4 |
| Maintenance Phase - Non-functioning NET, No Treatment | 41.7 |
"All tumour assessments were performed using the Response Evaluation Criteria In Solid Tumours (RECIST) criteria (1.1). Computer Tomography (CT-scan) or Magnetic Resonance Imaging (MRI) could be used for as method of tumour measurement and the same method of tumour measurement was used throughout the study for each subject. CT scans/MRI were performed at screening or baseline visit then at weeks 12, 24 and at early withdrawal or at anytime during the study in the case of any clinical or biological signs of tumour progression.~The DCR was defined as the proportion of subjects with a response of CR, PR or SD after 6 months of combination treatment and was described in the ITT population along with its 95% Confidence Interval (CI) and was compared to 45% with an exact binomial proportion test. The Last Observation Carried Forward (LOCF) method was used to replace missing assessments at the end of the combination phase." (NCT02231762)
Timeframe: 6 months
| Intervention | percentage of subjects (Number) |
|---|---|
| Combination Phase | 73.5 |
"The DoR is an estimation of the time from first documented objective response (CR or PR) to the first date of progressive disease (PD) or death due to disease progression for subjects who experienced an objective response within the first 12 months of treatment (combination and maintenance phases).~The Kaplan-Meier method was used to estimate the median DoR and its 95% CI for subjects in the ITT population who had an objective response." (NCT02231762)
Timeframe: 12 months
| Intervention | months (Median) |
|---|---|
| Intention-to-treat (ITT) Population | NA |
"PFS was defined as the time from the date of treatment start to the date of the first documented disease progression or death due to any cause within the first 12 months of treatment. If a subject had not progressed or died after 12 months of treatment or when any further anti-neoplastic therapy was received, PFS was censored at the time of the last tumour assessment before the analysis cut-off date or the anti-neoplastic therapy date.~A Kaplan-Meier estimate of the PFS was calculated to determine the number of subjects at risk. Median PFS time (50% of subjects who would not progress or die) of the ITT population is presented along with 95 % CI." (NCT02231762)
Timeframe: 12 months
| Intervention | months (Median) |
|---|---|
| Intention-to-treat (ITT) Population | 11.1 |
"TtR was defined as the time from the date of treatment start to the date of the first documented objective response (CR or PR) within the first 12 months of treatment (combination and maintenance phases). A Kaplan Meier estimate of the TtR survival function was constructed.~The Kaplan-Meier method was used to estimate the median TtR and its 95% CI for subjects in the ITT population (50% of subjects were expected to have a CR or PR at this time)." (NCT02231762)
Timeframe: 12 months
| Intervention | months (Median) |
|---|---|
| Intention-to-treat (ITT) Population | NA |
"In all subjects whose tumour tissue was available, MGMT expression/methylation and SSTR expression was analysed. After 6 months, the DCR (SD+PR+CR) by MGMT methylation and expression and by SSTR 2a and SSTR 5 expression was evaluated.~DCR in response to MGMT methylation and expression results are presented. SSTR 2a and SSTR 5 expression is categorised as: No Receptors, Cytoplasmatic Expression (CE), Focal Expression (FE), Complete Circumferent Membrane Expression (CCME).~The DCR was defined as the proportion of subjects with a response of CR, PR or SD after 6 months of combination treatment within each methylation/expression category. The DCR was described in the ITT population along with its 95% CI and was compared to 45% with an exact binomial proportion test." (NCT02231762)
Timeframe: 6 months
| Intervention | percentage of subjects (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| MGMT Methylation | MGMT No methylation | MGMT Expression | MGMT No expression | SSTR 2a FE | SSTR 2a CCME | SSTR 5 - No Receptors | SSTR 5 CE | SSTR 5 FE | |
| Combination Phase | 100.0 | 84.6 | 90.9 | 70.0 | 86.7 | 72.7 | 75.0 | 100.0 | 81.8 |
Subjects were instructed to complete QLQ-C30 questionnaire at baseline, weeks 12, 24, 36, 48 (end of study) or at early withdrawal. The first 28 questions used a 4-point scale (1=not at all, 2=a little, 3=quite a bit, 4=very much) for evaluating 5 functional scales (physical, role, emotional, cognitive, social), 3 symptom scales (fatigue, nausea/vomiting, pain) & 6 other single items. The last 2 questions represented subject's assessment of overall health & quality of life, coded on a 7-point scale (1=very poor to 7=excellent). The mean change from baseline at week 48 (end of study) is presented for global health status (scoring of questions 29 & 30) and 5 functional scales, 3 symptom scales and other single items (scoring of questions 1 to 28). Each individual subscore was transformed to range from 0 to 100. A higher score represents a higher level response. Thus, a better QoL/a better level of functioning/a worse level of symptoms. (NCT02231762)
Timeframe: 12 months
| Intervention | units on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Global health status | Physical functioning | Role functioning | Emotional functioning | Cognitive functioning | Social functioning | Fatigue | Nausea and vomiting | Pain | Dyspnoea | Insomnia | Appetite loss | Constipation | Diarrhoea | Financial difficulties | |
| Maintenance Phase - Functioning NET, Lanreotide | -11.7 | 8.0 | 3.3 | 15.0 | 3.3 | 13.3 | -22.2 | -10.0 | -13.3 | -8.3 | -13.3 | 0.0 | 20.0 | -40.0 | 6.7 |
| Maintenance Phase - Non-functioning NET, Lanreotide | -3.1 | -12.5 | -2.1 | -6.2 | -2.1 | -22.9 | -9.7 | 4.2 | 4.2 | 4.2 | -8.3 | 0.0 | -4.2 | 8.3 | 4.2 |
| Maintenance Phase - Non-functioning NET, No Treatment | -7.1 | -11.4 | -7.1 | -6.0 | 2.4 | -4.8 | 4.8 | 2.4 | 9.5 | 9.5 | 16.7 | 14.3 | -4.8 | 0.0 | 9.5 |
Subjects were instructed to complete the QLQ-C30 questionnaire at baseline, weeks 12, 24 or at early withdrawal. The first 28 questions used a 4-point scale (1=not at all, 2=a little, 3=quite a bit, 4=very much) for evaluating 5 functional scales (physical, role, emotional, cognitive, social), 3 symptom scales (fatigue, nausea/vomiting, pain) & 6 other single items. The last 2 questions represented subject's assessment of overall health & quality of life, coded on a 7-point scale (1=very poor to 7=excellent). The mean change from baseline at week 24 (end of the combination phase) is presented for global health status (scoring of questions 29 & 30) and 5 functional scales, 3 symptom scales and other single items (scoring of questions 1 to 28). Each individual subscore was transformed to range from 0 to 100. A higher score represents a higher level response. Thus, a better QoL/a better level of functioning/a worse level of symptoms. (NCT02231762)
Timeframe: 6 months
| Intervention | units on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Global health status | Physical functioning | Role functioning | Emotional functioning | Cognitive functioning | Social functioning | Fatigue | Nausea and vomiting | Pain | Dyspnoea | Insomnia | Appetite loss | Constipation | Diarrhoea | Financial difficulties | |
| Combination Phase | -4.9 | -9.6 | -8.3 | -4.7 | -5.9 | -11.8 | 6.9 | 6.9 | -1.0 | 12.7 | 0.0 | 2.0 | 6.9 | -3.9 | 2.9 |
"Lanreotide ATG levels were measured in a subset of subjects to evaluate if temozolomide co-treatment had an impact on lanreotide serum concentration over a 12 month period.~Blood samples were collected for the determination of lanreotide ATG in serum at baseline, weeks 4, 12, 24 and 48 (end of study).~The concentrations of lanreotide ATG in serum were determined by a validated radioimmunoassay analysis method with a lower limit of quantitation of 0.08 nanograms [ng]/mL).~Serum concentrations of lanreotide ATG at each of the time points in the combination and maintenance phase are presented. Only subjects with data available for analysis are presented." (NCT02231762)
Timeframe: Baseline (week 1) and weeks 4, 12, 24 and 48
| Intervention | ng/mL (Mean) | ||||
|---|---|---|---|---|---|
| Baseline | Week 4 | Week 12 | Week 24 | Week 48 | |
| PK Subset | 0.44 | 2.45 | 5.06 | 5.83 | 3.68 |
Subjects were instructed to complete the QLQ-GI.NET21 questionnaire at baseline, weeks 12, 24, 36, 48 (end of study) or at early withdrawal. It contained 21 questions that used a 4-point scale (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much) to evaluate 3 defined multi-item symptom scales (endocrine, gastrointestinal and treatment related side effects), 2 single item symptoms (bone/muscle pain and concern about weight loss), 2 psychosocial scales (social function and disease-related worries) and 2 other single items (sexuality and communication). Answers were converted into grading scale, with values between 0 and 100. Each individual subscore was transformed to range from 0 to 100. The mean change from baseline at week 48 (end of study) is presented with a higher score representing a higher level response. Thus, a better level of functioning/a worse level of symptoms. (NCT02231762)
Timeframe: 12 months
| Intervention | units on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Endocrine symptoms | G.I. symptoms | Treatment related symptoms | Social function | Disease related worries | Muscle/bone pain symptoms | Body image | Weight gain | Information/communication function | Sexual function | |
| Maintenance Phase - Functioning NET, Lanreotide | -13.3 | -4.0 | 0.0 | -6.7 | -6.7 | -6.7 | 0.0 | -20.0 | 0.0 | 0.0 |
| Maintenance Phase - Non-functioning NET, Lanreotide | -5.6 | 0.0 | -11.1 | 9.7 | 1.4 | 4.2 | 4.2 | 9.5 | 0.0 | 0.0 |
Subjects were instructed to complete the QLQ-GI.NET21 questionnaire at baseline, weeks 12, 24, 36, 48 (end of study) or at early withdrawal. It contained 21 questions that used a 4-point scale (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much) to evaluate 3 defined multi-item symptom scales (endocrine, gastrointestinal and treatment related side effects), 2 single item symptoms (bone/muscle pain and concern about weight loss), 2 psychosocial scales (social function and disease-related worries) and 2 other single items (sexuality and communication). Answers were converted into grading scale, with values between 0 and 100. Each individual subscore was transformed to range from 0 to 100. The mean change from baseline at week 48 (end of study) is presented with a higher score representing a higher level response. Thus, a better level of functioning/a worse level of symptoms. (NCT02231762)
Timeframe: 12 months
| Intervention | units on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Endocrine symptoms | G.I. symptoms | Social function | Disease related worries | Muscle/bone pain symptoms | Body image | Weight gain | Information/communication function | Sexual function | |
| Maintenance Phase - Non-functioning NET, No Treatment | 1.6 | 6.7 | -6.3 | -3.2 | 4.8 | 4.8 | -9.5 | -4.8 | 0.0 |
Subjects were instructed to complete the QLQ-GI.NET21 questionnaire at baseline, weeks 12, 24 or at early withdrawal. It contained 21 questions that used a 4-point scale (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much) to evaluate 3 defined multi-item symptom scales (endocrine, gastrointestinal and treatment related side effects), 2 single item symptoms (bone/muscle pain and concern about weight loss), 2 psychosocial scales (social function and disease-related worries) and 2 other single items (sexuality and communication). Each individual subscore was transformed to range from 0 to 100. The mean change from baseline at week 24 (end of combination phase) is presented with a higher score representing a higher level response. Thus, a better level of functioning/a worse level of symptoms. (NCT02231762)
Timeframe: 6 months
| Intervention | Units on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Endocrine symptoms | Gastrointestinal (G.I.) symptoms | Treatment related symptoms | Social function | Disease related worries | Muscle/bone pain symptoms | Body image | Weight gain | Information/communication function | Sexual function | |
| Combination Phase | -1.0 | 5.7 | 3.6 | 2.3 | 1.6 | 1.0 | 0.0 | -11.8 | -9.4 | -4.8 |
"Urine samples for 5-HIAA urinary tumour marker analysis were taken at baseline, weeks 12, 24, 36, 48 (end of study) and early withdrawal.~Biochemical response based on 5-HIAA levels was categorised as: Response (5-HIAA reduction compared to baseline) or Progression (5-HIAA increase compared to baseline).~The number of subjects in each response category at each time point in the maintenance phase is presented. Analysis was only carried out on subjects in the ITT population with functioning NET." (NCT02231762)
Timeframe: 12 months
| Intervention | Participants (Count of Participants) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 24 - Progression | Week 24 - Response | Week 24 - Not evaluable | Week 24 - Missing | Week 36 - Progression | Week 36 - Response | Week 36 - Not evaluable | Week 36 - Missing | Week 48 - Progression | Week 48 - Response | Week 48 - Not evaluable | Week 48 - Missing | Early Withdrawal - Progression | Early Withdrawal - Response | Early Withdrawal - Not evaluable | Early Withdrawal - Missing | |
| Maintenance Phase - Functioning NET, Lanreotide | 6 | 3 | 1 | 1 | 3 | 3 | 0 | 3 | 4 | 2 | 0 | 2 | 0 | 0 | 0 | 3 |
"Blood samples for CgA blood tumour marker analysis were taken at baseline, weeks 12, 24, 36, 48 (end of study) and at early withdrawal. The biochemical response after 12 months combination and maintenance treatment was estimated for subjects with abnormal CgA levels at baseline. Abnormal CgA levels were defined as above the upper limit of normal range (≥100 mcg/L).~Biochemical response based on CgA levels was categorised as: PR (decrease of CgA ≥50 % compared to the baseline CgA), SD (decrease < 50% or an increase ≤ 25% compared to the baseline CgA) or PD (defined as an increase ≥ 25%, compared to the baseline CgA).~The number of subjects in each response category at each time point in the maintenance phase is presented. Analysis was only carried out on subjects in the ITT population who had abnormal CgA at baseline." (NCT02231762)
Timeframe: 12 months
| Intervention | Participants (Count of Participants) | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 24 - PD | Week 24 - SD | Week 24 - PR | Week 24 - Missing | Week 36 - PD | Week 36 - SD | Week 36 - PR | Week 36 - Missing | Week 48 - PD | Week 48 - SD | Week 48 - PR | Week 48 - Missing | Early Withdrawal - PD | Early Withdrawal - SD | Early Withdrawal - PR | Early Withdrawal - Missing | |
| Maintenance Phase - Functioning NET, Lanreotide | 2 | 3 | 0 | 0 | 1 | 2 | 0 | 0 | 1 | 0 | 1 | 0 | 1 | 0 | 0 | 2 |
| Maintenance Phase - Non-functioning NET, Lanreotide | 1 | 4 | 3 | 1 | 1 | 4 | 1 | 1 | 1 | 2 | 2 | 0 | 2 | 0 | 1 | 0 |
| Maintenance Phase - Non-functioning NET, No Treatment | 2 | 2 | 3 | 2 | 3 | 2 | 4 | 0 | 2 | 3 | 1 | 0 | 1 | 0 | 1 | 0 |
"Blood samples for CgA blood tumour marker analysis were taken at baseline, weeks 12, 24 and at early withdrawal. The biochemical response after 6 months combination treatment was estimated for subjects with abnormal CgA levels at baseline. Abnormal CgA levels were defined as above the upper limit of normal range (≥100 micrograms/litre [mcg/L]).~Biochemical response based on CgA levels was categorised as: PR (decrease of CgA ≥ 50%, compared to the baseline CgA), SD (decrease < 50 % or an increase ≤25%, compared to the baseline CgA) or PD (defined as an increase ≥25 %, compared to the baseline CgA).~The number of subjects in each response category at each time point in the combination phase is presented. Analysis was only carried out on subjects in the ITT population who had abnormal CgA at baseline." (NCT02231762)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 12- PD | Week 12 - SD | Week 12- PR | Week 12 - Missing | Week 24 - PD | Week 24 - SD | Week 24 - PR | Week 24 - Missing | Early Withdrawal - PD | Early Withdrawal - SD | Early Withdrawal - PR | Early Withdrawal - Missing | |
| Combination Phase | 8 | 15 | 10 | 1 | 5 | 9 | 7 | 0 | 1 | 2 | 1 | 14 |
The time for clinical response in Phase 1 (up to Day 28) was defined as the time from inclusion (Day 0) to the date of clinical response. A response was defined as occurrence of ≤ 2 vomiting episodes/day for at least 3 consecutive days at any timepoint between Day 0 and Day 28 (for patients without NGT use at baseline) or the removal of NGT for at least 3 consecutive days at any timepoint between Day 0 and Day 28 without vomiting recurrence (for patients with NGT use at baseline). The Kaplan-Meier estimate of median time to clinical response are presented. (NCT02275338)
Timeframe: From Day 0 to Day 28
| Intervention | days (Median) |
|---|---|
| Lanreotide Autogel® 120 mg - All Subjects | 9.00 |
The primary endpoint assessed the percentage of responding subjects before or at Day 7. A responder was defined as a subject experiencing ≤2 vomiting episodes/day during at least 3 consecutive days at any timepoint between Day 0 and Day 7 (for subjects without NGT at baseline), or as a subject in whom the NGT had been removed during at least 3 consecutive days at any timepoint between Day 0 and Day 7 without vomiting recurrence (for subjects with NGT at baseline), as recorded on diary cards which were completed every day. (NCT02275338)
Timeframe: From Day 0 to Day 7
| Intervention | percentage of responders (Number) | ||
|---|---|---|---|
| Without NGT at Baseline | With NGT at Baseline | All Subjects | |
| Lanreotide Autogel® 120 mg | 88.2 | 25.7 | 46.2 |
Quality of Life was assessed by both subject and investigator based on the ESAS. The ESAS scale evaluates 9 symptoms common in cancer subjects: pain, tiredness, nausea, depression, anxiety, drowsiness, appetite, wellbeing and shortness of breath. The severity at the time of assessment of each symptom is rated from 0 to 10 on a numerical scale, 0 = symptom is absent and 10 = worst possible severity. Each symptom rating was interpreted independently and a total symptom distress score was calculated for both subject and investigator assessed scores as the sum of the 9 items. Median change from baseline (Day 0) in total symptom distress score, at each of the Phase 2 timepoints is presented and a positive change indicates a worsening condition. (NCT02275338)
Timeframe: Days 0, 35, 42 and 56
| Intervention | units on a scale (Median) | |||||
|---|---|---|---|---|---|---|
| Day 35 - assessed by subject | Day 35 - assessed by investigator | Day 42 - assessed by subject | Day 42 - assessed by investigator | Day 56 - assessed by subject | Day 56 - assessed by investigator | |
| Lanreotide Autogel® 120 mg - All Subjects | -4.0 | -12.0 | -10.5 | -13.5 | -8.0 | -9.0 |
"The mean number of daily episodes of nausea were calculated as the sum of episodes of nausea reported the last 3 days before the corresponding visit, divided by 3.~The median change from baseline (Day 0) at each of the Phase 1 timepoints is presented and positive change indicates a worsening condition." (NCT02275338)
Timeframe: Days 0, 7, 14 and 28
| Intervention | Daily episodes of nausea (Median) | ||
|---|---|---|---|
| At Day 7 | At Day 14 | At Day 28 | |
| Lanreotide Autogel® 120 mg - All Subjects | -0.17 | -1.50 | -1.50 |
The KPS scale was used to quantify subject's general well-being and activities of daily life. Subjects were classified based on their functional impairment and KPS scores range from 0 (death) to 100 (no evidence of disease). KPS scores are classified as 0-40 = unable to care for self; requires equivalent of institutional or hospital care; disease may be progressing rapidly; 50-70 = unable to work; able to live at home and care for most personal needs; varying amount of assistance needed; 80-100 = able to carry on normal activity and to work; no special care needed. Median change from baseline (Day 0) at each of the Phase 1 timepoints is presented and a negative change indicates a worsening condition. (NCT02275338)
Timeframe: Days 0, 7, 14 and 28
| Intervention | units on a scale (Median) | ||
|---|---|---|---|
| At Day 7 | At Day 14 | At Day 28 | |
| Lanreotide Autogel® 120 mg - All Subjects | 0.0 | 0.0 | 10.0 |
Abdominal pain was assessed using the VAS numeric pain distress scale. The VAS is a 100-millimetre (10-centimetre) scoring scale on which subjects marked on their perceived level of pain. Score range on VAS is from 0 to 100 where 0 = no pain and 100 = unbearable pain. Median change from baseline (Day 0) at each of the Phase 1 timepoints is presented and a positive change indicates a worsening condition. (NCT02275338)
Timeframe: Days 0, 7, 14 and 28
| Intervention | units on a scale (Median) | ||
|---|---|---|---|
| At Day 7 | At Day 14 | At Day 28 | |
| Lanreotide Autogel® 120 mg - All Subjects | -3.0 | -1.0 | 0.0 |
Quality of Life was assessed by both subject and investigator based on the ESAS. The ESAS scale evaluates 9 symptoms common in cancer subjects: pain, tiredness, nausea, depression, anxiety, drowsiness, appetite, wellbeing and shortness of breath. The severity at the time of assessment of each symptom is rated from 0 to 10 on a numerical scale; 0 = symptom is absent and 10 = worst possible severity. Each symptom rating was interpreted independently and a total symptom distress score was calculated for both subject and investigator assessed scores as the sum of the 9 items. Median change from baseline (Day 0) in total symptom distress score, at each of the Phase 1 timepoints is presented and a positive change indicates a worsening condition. (NCT02275338)
Timeframe: Days 0, 7, 14 and 28
| Intervention | units on a scale (Median) | |||||
|---|---|---|---|---|---|---|
| Day 7 - assessed by subject | Day 7 - assessed by investigator | Day 14 - assessed by subject | Day 14 - assessed by investigator | Day 28 - assessed by subject | Day 28 - assessed by investigator | |
| Lanreotide Autogel® 120 mg - All Subjects | -3.0 | -4.5 | -2.0 | -7.5 | -5.5 | -5.0 |
This endpoint assessed the overall percentage of subjects continuing from Phase 1 and confirmed as a responder at the end of Phase 1, showing a continued response at Days 35, 42 and 56. A responder was defined as a subject experiencing ≤2 vomiting episodes/day during at least 3 consecutive days at any timepoint between Day 0 and Days 35, 42, 56 (for subjects without NGT at baseline), or as a subject in whom the NGT had been removed during at least 3 consecutive days at any timepoint between Day 0 and Days 35, 42, 56 without vomiting recurrence (for subjects with NGT at baseline), as recorded on diary cards which were completed every day. (NCT02275338)
Timeframe: From Day 0 to Day 56
| Intervention | percentage of responders (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| By Day 35: Without NGT at Baseline | By Day 35: With NGT at Baseline | By Day 35: All Subjects | By Day 42: Without NGT at Baseline | By Day 42: With NGT at Baseline | By Day 42: All Subjects | By Day 56: Without NGT at Baseline | By Day 56: With NGT at Baseline | By Day 56: All Subjects (n=21) | |
| Lanreotide Autogel® 120 mg - All Subjects | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
This endpoint assessed the overall percentage of responding subjects at the Phase 1 timepoints of Days 14 and 28. A responder was defined as a subject experiencing ≤ 2 vomiting episodes/day during at least 3 consecutive days at any timepoint between Day 0 and Days 14 or 28 (for subjects without NGT at baseline) or as a subject in whom the NGT has been removed, during at least 3 consecutive days without vomiting recurrence, at any timepoint between Day 0 and Days 14 and 28 (for subjects with NGT at baseline), as recorded on diary cards which were completed every day. (NCT02275338)
Timeframe: From Day 0 to Day 28
| Intervention | percentage of responders (Number) | |||||
|---|---|---|---|---|---|---|
| By Day 14: Without NGT at Baseline | By Day 14: With NGT at Baseline | By Day 14: All Subjects | By Day 28: Without NGT at Baseline | By Day 28: With NGT at Baseline | By Day 28: All Subjects | |
| Lanreotide Autogel® 120 mg - All Subjects | 88.2 | 45.7 | 59.6 | 88.2 | 54.3 | 65.4 |
"The progression-free survival is the time from inclusion to the first radiological progression or death (all causes). For patients alive without progression date of last news will be considered.~Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1), as a 20% increase in the sum of the longest diameter of target lesions compared the little sum of diameters observed durin the study (NADIR), or a measurable increase in a nontarget lesion, or the appearance of new lesions" (NCT02288377)
Timeframe: up to 2 years
| Intervention | Months (Median) |
|---|---|
| Placebo | 7.6 |
| Lanreotide | 19.4 |
Overall survival considered all deaths, and time was calculated from randomisation to death. (NCT02288377)
Timeframe: 2 years after the end of the treatment
| Intervention | Percentage of patients alive (Number) |
|---|---|
| Placebo | 86.1 |
| Lanreotide | 95.0 |
The primary endpoint for this phase II study was the proportion of pts alive and progression-free at 6 months after randomisation, evaluated according to the results of the imaging assessment done by the investigator in line with RECIST 1.1 criteria. (NCT02288377)
Timeframe: 6 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo | 13 |
| Lanreotide | 19 |
Vomiting episodes were recorded on the Patient Diary daily until the end of study (Day 28), by the patient or filled in by the nurse/caregiver in case of patient's physical inability. Mean change from baseline in number of daily vomiting episodes is presented for the ITT population. (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Episodes (daily) (Mean) | ||
|---|---|---|---|
| Change at Day 7 | Change at Day 14 | Change at Day 28 | |
| Standard Care | 5.7 | 10.6 | 16.5 |
| Standard Care + Lanreotide Autogel | 6.0 | 10.4 | 14.1 |
"The KPS allows patients to be classified as to their functional impairment and was used to assess general activity. KPS scores range from 0 (dead) to 100 (normal/no disease) and are classified as 0-40 = unable to care for self; 50-70 = unable to work; 80-100 = able to work. The lower the KPS score, the worse the survival for most serious illnesses. Scores were recorded on the patient's medical file at each study visit (Days 1, 7, 14 and 28).~Mean change from baseline of KPS score at Days 7, 14 and 28 is presented for the ITT population (all randomised patients); a negative change indicates a worsening condition." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| Change at Day 7 | Change at Day 14 | Change at Day 28 | |
| Standard Care | -2.8 | -5.6 | -5.0 |
| Standard Care + Lanreotide Autogel | -3.7 | -5.4 | -7.1 |
"Quality of Life was assessed using ESAS, evaluating 9 common symptoms in cancer patients: pain, activity, nausea, depression, anxiety, drowsiness, appetite, well-being and shortness of breath. Symptom severity is rated 0-10 on a numerical scale (0=symptom absent; 10=worst severity). Low scores indicate good quality of life; high scores indicate strong discomfort. Questionnaire assessments by the patient or by nurse/caregiver in case of patient's physical inability.~Mean change from baseline of each individual ESAS item score at Days 7, 14 and 28 is presented; a positive change indicates a worsening condition." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Scores on a scale (Mean) | ||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Change at Day 7: Pain | Change at Day 14: Pain | Change at Day 28: Pain | Change at Day 7: Activity | Change at Day 14: Activity | Change at Day 28: Activity | Change at Day 7: Nausea | Change at Day 14: Nausea | Change at Day 28: Nausea | Change at Day 7: Depression | Change at Day 14 Depression | Change at Day 28: Depression | Change at Day 7: Anxiety | Change at Day 14: Anxiety | Change at Day 28: Anxiety | Change at Day 7: Drowsiness | Change at Day 14: Drowsiness | Change at Day 28: Drowsiness | Change at Day 7: Appetite | Change at Day 14: Appetite | Change at Day 28: Appetite | Change at Day 7: Well-being | Change at Day 14: Well-being | Change at Day 28: Well-being | Change at Day 7: Shortness of breath | Change at Day 14: Shortness of breath | Change at Day 28: Shortness of breath | |
| Standard Care | -1.8 | -1.3 | -3.0 | -0.3 | -0.3 | -1.4 | 0.5 | 0.1 | -0.6 | -1.8 | -1.9 | -2.6 | 0.0 | 0.4 | -1.1 | -0.7 | -0.1 | -1.9 | -0.2 | 0.9 | 0.4 | -0.8 | 0.4 | 0.4 | -0.1 | 0.6 | -0.4 |
| Standard Care + Lanreotide Autogel | 0.1 | -1.9 | -1.3 | 0.7 | -0.7 | -0.3 | 0.9 | 0.5 | 0.0 | -1.1 | -2.4 | -3.7 | -0.2 | -2.7 | -1.5 | 0.4 | -0.6 | -1.5 | 0.5 | 0.4 | -2.0 | -0.4 | -0.5 | -2.3 | 0.7 | 0.7 | -0.2 |
NGT presence and related secretion volume were recorded on the Patient Diary daily until the end of study (Day 28), by the patient or filled in by the nurse/caregiver in case of patient's physical inability. Mean daily secretion volumes, in patients with NGT, is presented. (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | millilitres (Mean) | |||
|---|---|---|---|---|
| Baseline | Day 7 | Day 14 | Day 28 | |
| Standard Care | 200.0 | 4875.0 | 12675.0 | 27501.0 |
| Standard Care + Lanreotide Autogel | 700.0 | 1025.0 | 7090.8 | 18301.4 |
"Quality of Life was assessed using ESAS, evaluating 9 common symptoms in cancer patients: pain, activity, nausea, depression, anxiety, drowsiness, appetite, well-being and shortness of breath. Symptom severity is rated 0-10 on a numerical scale (0=symptom absent; 10=worst severity). ESAS total score is sum of the 9 items (min score=0, max score=90). Low scores indicate good quality of life; high scores indicate strong discomfort. Questionnaire assessments by the patient or by nurse/caregiver in case of patient's physical inability.~Secondary endpoints were analysed using the ITT population but to permit following the FAS which was used for primary endpoint analysis, ESAS total score results are reported for both the ITT and the FAS. Mean change from baseline of ESAS total score at Days 7, 14 and 28 is presented here for the FAS; a positive change indicates a worsening condition." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| Change at Day 7 | Change at Day 14 | Change at Day 28 | |
| Standard Care | -5.1 | -1.3 | -6.8 |
| Standard Care + Lanreotide Autogel | 1.9 | -7.3 | -10.3 |
Vomiting episodes and NGT presence were recorded on the Patient Diary daily until the end of study (Day 28), by the patient or filled in by the nurse/caregiver in case of patient's physical inability. Number of patients experiencing ≤ 2 vomiting episodes/day during at least 3 consecutive days, in patients without NGT, is presented. (NCT02365584)
Timeframe: From Baseline (Day 1, before randomisation) to Days 7, 14 and 28.
| Intervention | Participants (Count of Participants) | ||
|---|---|---|---|
| From Day 1 to Day 7 | From Day 1 to Day 14 | From Day 1 to Day 28 | |
| Standard Care | 5 | 4 | 4 |
| Standard Care + Lanreotide Autogel | 4 | 4 | 4 |
Passage of stools assessments (Yes/No) were recorded on the Patient Diary daily until the end of study (Day 28), by the patient or filled in by the nurse/caregiver in case of patient's physical inability. (NCT02365584)
Timeframe: From Baseline (Day 1, before randomisation) to Day 28.
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Day 172161255 | Day 172161256 | Day 272161255 | Day 272161256 | Day 372161255 | Day 372161256 | Day 472161255 | Day 472161256 | Day 572161256 | Day 572161255 | Day 672161255 | Day 672161256 | Day 772161255 | Day 772161256 | Day 872161255 | Day 872161256 | Day 972161255 | Day 972161256 | Day 1072161255 | Day 1072161256 | Day 1172161255 | Day 1172161256 | Day 1272161255 | Day 1272161256 | Day 1372161255 | Day 1372161256 | Day 1472161256 | Day 1472161255 | Day 1572161256 | Day 1572161255 | Day 1672161256 | Day 1672161255 | Day 1772161256 | Day 1772161255 | Day 1872161255 | Day 1872161256 | Day 1972161255 | Day 1972161256 | Day 2072161255 | Day 2072161256 | Day 2172161256 | Day 2172161255 | Day 2272161255 | Day 2272161256 | Day 2372161255 | Day 2372161256 | Day 2472161256 | Day 2472161255 | Day 2572161256 | Day 2572161255 | Day 2672161256 | Day 2672161255 | Day 2772161255 | Day 2772161256 | Day 2872161255 | Day 2872161256 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Yes | No | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 19 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 20 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 18 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 15 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 16 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 16 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 17 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 5 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 14 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 13 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 15 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 5 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 10 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 11 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 11 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 12 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 13 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 10 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 9 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 8 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 8 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 7 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 9 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 3 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 7 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care | 1 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Standard Care + Lanreotide Autogel | 4 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
"Quality of Life was assessed using ESAS, evaluating 9 common symptoms in cancer patients: pain, activity, nausea, depression, anxiety, drowsiness, appetite, well-being and shortness of breath. Symptom severity is rated 0-10 on a numerical scale (0=symptom absent; 10=worst severity). ESAS total score is sum of the 9 items (min score=0, max score=90). Low scores indicate good quality of life; high scores indicate strong discomfort. Questionnaire assessments by the patient or by nurse/caregiver in case of patient's physical inability. AUC is area under the line which joins the points defined by plotting ESAS total score on vertical axis and time values on horizontal axis, computed using trapezoidal rule.~Primary endpoint was analysed using the FAS. LS mean AUC of ESAS total scores during first 7 days is presented." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation), Days 2, 3, 4, 5, 6 and 7.
| Intervention | Scores on a scale x time (day) (Least Squares Mean) |
|---|---|
| Standard Care | 179 |
| Standard Care + Lanreotide Autogel | 190 |
"Abdominal pain was assessed using the VAS numeric pain distress scale which is a 100-millimetre (10-centimetre) scoring scale on which patients mark their perceived level of pain. Scores range from 0 to 100 where 0=no pain and 100=unbearable pain. Higher scores indicate a worse outcome. Scores were recorded on the Patient Diary daily until the end of study (Day 28), by the patient or filled in by the nurse/caregiver in case of patient's physical inability.~Mean change from baseline of VAS for abdominal pain at Days 7, 14 and 28 is presented for the ITT population; a positive change indicates a worsening condition." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| Change at Day 7 | Change at Day 14 | Change at Day 28 | |
| Standard Care | -22.0 | -15.6 | -32.0 |
| Standard Care + Lanreotide Autogel | -9.6 | -27.7 | -17.0 |
"Quality of Life was assessed using ESAS, evaluating 9 common symptoms in cancer patients: pain, activity, nausea, depression, anxiety, drowsiness, appetite, well-being and shortness of breath. Symptom severity is rated 0-10 on a numerical scale (0=symptom absent; 10=worst severity). ESAS total score is sum of the 9 items (min score=0, max score=90). Low scores indicate good quality of life; high scores indicate strong discomfort. Questionnaire assessments by the patient or by nurse/caregiver in case of patient's physical inability.~Secondary endpoints were analysed using the ITT population but to permit following the FAS which was used for primary endpoint analysis, ESAS total score results are reported for both the ITT and the FAS. Mean change from baseline of ESAS total score at Days 7, 14 and 28 is presented here for the ITT population; a positive change indicates a worsening condition." (NCT02365584)
Timeframe: Baseline (Day 1, before randomisation) and Days 7, 14 and 28.
| Intervention | Scores on a scale (Mean) | ||
|---|---|---|---|
| Change at Day 7 | Change at Day 14 | Change at Day 28 | |
| Standard Care | -5.1 | -1.3 | -6.8 |
| Standard Care + Lanreotide Autogel | 1.5 | -7.3 | -10.3 |
Blood samples for determination of the excipients (N1-glycofurol and N2-glycofurol) serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8, 12 and 24 hours post-dose and on Days 3 and 5. Mean serum N1-glycofurol and N2-glycofurol Cmax values were determined using non-compartmental analysis. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Day 5.
| Intervention | ng/mL (Mean) | |
|---|---|---|
| N1-glycofurol | N2-glycofurol | |
| Glycofurol PK Set: 180 mg Lanreotide PRF | 75.4 | 79.7 |
| Glycofurol PK Set: 270 mg Lanreotide PRF | 61.7 | 62.1 |
"Blood samples for determination of the excipients (N1-glycofurol and N2-glycofurol) serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8, 12 and 24 hours post-dose and on Days 3 and 5.~Median serum N1-glycofurol and N2-glycofurol Tmax values were determined using non-compartmental analysis." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Day 5.
| Intervention | hours (Median) | |
|---|---|---|
| N1-glycofurol | N2-glycofurol | |
| Glycofurol PK Set: 180 mg Lanreotide PRF | 2.00 | 2.00 |
| Glycofurol PK Set: 270 mg Lanreotide PRF | 2.00 | 2.00 |
AEs reported by the investigators using the National Cancer Institute-Common Toxicity Criteria (NCI CTCAE) classification (Version 4.03) and incidence of all reported treatment emergent AEs (TEAEs) and serious AEs (SAEs) are presented by dose cohort. AEs were assigned to a NCI CTCAE Grade from 1 through 5 as follows: Grade 1: Mild; Grade 2: Moderate; Grade 3: Severe or medically significant but not immediately life threatening or requiring hospitalisation; Grade 4: Life-threatening consequences; Grade 5: Death related to AE. TEAEs were defined as any AE that occurs during the active phase of the study (between the start of the 3 month treatment period and 3 months after the end of study treatment). The worst intensity of TEAES at each grade are reported for all and for related TEAES. In the event of multiple occurrences of the same AEs being reported by the same subject, the maximum intensity and the most serious causality were reported. (NCT02396953)
Timeframe: From Day -42 up to Week 25.
| Intervention | participants (Number) | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| TEAEs | Related TEAEs | TEAEs leading to study drug withdrawal | SAEs | Serious TEAEs | Serious related TEAEs | AEs leading to death | Worst TEAE: Grade 1 | Worst TEAE: Grade 2 | Worst TEAE: Grade 3 | Worst TEAE: Grade 4 | Worst TEAE: Grade 5 | Worst related TEAE: Grade 1 | Worst related TEAE: Grade 2 | Worst related TEAE: Grade 3 | Worst related TEAE: Grade 4 | Worst related TEAE: Grade 5 | |
| 180 mg Lanreotide PRF | 6 | 2 | 0 | 1 | 1 | 0 | 0 | 1 | 3 | 2 | 0 | 0 | 0 | 2 | 0 | 0 | 0 |
| 270 mg Lanreotide PRF | 7 | 3 | 0 | 0 | 0 | 0 | 0 | 3 | 4 | 0 | 0 | 0 | 1 | 2 | 0 | 0 | 0 |
| 360 mg Lanreotide PRF | 7 | 4 | 0 | 1 | 1 | 0 | 0 | 5 | 1 | 1 | 0 | 0 | 3 | 1 | 0 | 0 | 0 |
Blood samples were collected for the determination of TSH in serum at Baseline (pre-dose) and at Weeks 2, 5, 13 and 25 (or EW). Summary data for serum concentrations of TSH were calculated and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | mIU/L (Mean) | |||
|---|---|---|---|---|
| Week 2 | Week 5 | Week 13 | Week 25 (EOS/EW) | |
| 180 mg Lanreotide PRF | -0.222 | -0.156 | -0.404 | -0.480 |
| 270 mg Lanreotide PRF | 0.119 | 0.062 | -0.060 | 0.073 |
| 360 mg Lanreotide PRF | 0.047 | 0.051 | 0.601 | 0.235 |
"Blood samples for determination of the excipients (N1-glycofurol and N2-glycofurol) serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8, 12 and 24 hours post-dose and on Days 3 and 5.~Mean serum N1-glycofurol and N2-glycofurol AUC0-∞ and AUC0-t values were determined using non-compartmental analysis. Only AUC0-∞ values fulfilling the accuracy determination rules were analysed." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Day 5.
| Intervention | ng*h/mL (Mean) | |||
|---|---|---|---|---|
| AUC0-∞: N1-glycofurol | AUC0-∞: N2-glycofurol | AUC0-t: N1-glycofurol | AUC0-t: N2-glycofurol | |
| Glycofurol PK Set: 180 mg Lanreotide PRF | 779 | 1008 | 783 | 1007 |
| Glycofurol PK Set: 270 mg Lanreotide PRF | 1049 | 1359 | 1082 | 1360 |
The MTD was defined based on the DLTs observed in each cohort. A DLT was defined as an adverse event (AE) (excluding anorexia and fatigue) or an abnormal laboratory value occurring within the first week (up to Week 2) following lanreotide PRF administration and during the entire study duration, assessed as unrelated to acromegaly, intercurrent illness or concomitant medications and which met any of the pre-established toxicity criteria. If no DLTs were reported then no MTD could be defined. (NCT02396953)
Timeframe: From Day 1 up to Week 25.
| Intervention | participants (Number) |
|---|---|
| 180 mg Lanreotide PRF | 0 |
| 270 mg Lanreotide PRF | 0 |
| 360 mg Lanreotide PRF | 0 |
"Blood samples for determination of lanreotide serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8,12 and 24 hours post-dose, on Days 3 and 5 and at Weeks 2, 3, 5, 9 and 13 after lanreotide PRF administration. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW).~Mean serum lanreotide t1/2 values were determined using non-compartmental analysis. Only values fulfilling the determination rules for t1/2 were analysed." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | days (Mean) |
|---|---|
| Lanreotide PK Set: 180 mg Lanreotide PRF | 54.2 |
| Lanreotide PK Set: 270 mg Lanreotide PRF | 61.7 |
| Lanreotide PK Set: 360 mg Lanreotide PRF | 63.1 |
"Blood samples for determination of lanreotide serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8,12 and 24 hours post-dose, on Days 3 and 5 and at Weeks 2, 3, 5, 9 and 13 after lanreotide PRF administration. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW).~Mean serum lanreotide AUC0-∞ values were determined using non-compartmental analysis. Only values fulfilling the accuracy determination rules for AUC0-∞ were analysed." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | ng*day/mL (Mean) |
|---|---|
| Lanreotide PK Set: 180 mg Lanreotide PRF | NA |
| Lanreotide PK Set: 270 mg Lanreotide PRF | NA |
| Lanreotide PK Set: 360 mg Lanreotide PRF | NA |
"Blood samples for determination of lanreotide serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8,12 and 24 hours post-dose, on Days 3 and 5 and at Weeks 2, 3, 5, 9 and 13 after lanreotide PRF administration. Sample were also collected during follow-up at Weeks 17, 21 and 25 (or EW).~Mean serum lanreotide AUC0-85 values were determined using non-compartmental analysis." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Day 85
| Intervention | ng*day/mL (Mean) |
|---|---|
| Lanreotide PK Set: 180 mg Lanreotide PRF | 161 |
| Lanreotide PK Set: 270 mg Lanreotide PRF | 179 |
| Lanreotide PK Set: 360 mg Lanreotide PRF | 265 |
"Blood samples for determination of lanreotide serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8,12 and 24 hours post-dose, on Days 3 and 5 and at Weeks 2, 3, 5, 9 and 13 after lanreotide PRF administration. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW).~Mean serum lanreotide Cmax values were determined using non-compartmental analysis." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | nanograms/millilitre (ng/mL) (Mean) |
|---|---|
| Lanreotide PK Set: 180 mg Lanreotide PRF | 19.0 |
| Lanreotide PK Set: 270 mg Lanreotide PRF | 14.0 |
| Lanreotide PK Set: 360 mg Lanreotide PRF | 20.5 |
"Blood samples for determination of lanreotide serum concentrations were collected at Baseline (pre-dose), at 1, 2, 4, 6, 8,12 and 24 hours post-dose, on Days 3 and 5 and at Weeks 2, 3, 5, 9 and 13 after lanreotide PRF administration. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW).~Median serum lanreotide Tmax values were determined using non-compartmental analysis." (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | days (Median) |
|---|---|
| Lanreotide PK Set: 180 mg Lanreotide PRF | 0.250 |
| Lanreotide PK Set: 270 mg Lanreotide PRF | 0.253 |
| Lanreotide PK Set: 360 mg Lanreotide PRF | 0.250 |
Blood samples were collected for the determination of FT3 and FT4 in serum at Baseline (pre-dose) and at Weeks 2, 5, 13 and 25 (or EW). Summary data for serum concentrations of FT3 and FT4 were calculated and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | picomole/litre (L) (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| FT3: Week 2 | FT3: Week 5 | FT3: Week 13 | FT3: Week 25 (EOS/EW) | FT4: Week 2 | FT4: Week 5 | FT4: Week 13 | FT4: Week 25 (EOS/EW) | |
| 180 mg Lanreotide PRF | -0.278 | -0.132 | 0.100 | 0.268 | 0.50 | 1.18 | 1.69 | 0.81 |
| 270 mg Lanreotide PRF | -0.164 | -0.170 | 0.191 | 0.295 | -0.02 | 0.33 | 1.80 | 1.06 |
| 360 mg Lanreotide PRF | -0.374 | 0.170 | 0.438 | 0.396 | -0.68 | -0.67 | -0.46 | 0.38 |
GH cycle assessments were performed by taking 5 samples in the morning (with a sample taken every 30 minutes for 2 hours) at Baseline (pre-dose), Week 5 and Week 13. Summary data for the mean of the 5 samplings of the GH cycle were generated and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 13.
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Week 5 | Week 13 | |
| 180 mg Lanreotide PRF | 0.268 | 0.667 |
| 270 mg Lanreotide PRF | 0.367 | 0.684 |
| 360 mg Lanreotide PRF | -0.228 | 0.003 |
Blood samples were collected for the determination of IGF-1 in serum at Baseline (pre-dose), 6 hours post-dose and at Weeks 5, 9 and 13. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW). Serum concentrations of IGF-1 were calculated using the Immulite 2000 Platform for all subjects in the safety population. The production of the reagent kits was stopped by the vendor during the study. The old reagent kits were used for Cohorts 1 and 2 until their expiry date and then the kits were switched to a new reagent and used for remaining subjects in Cohorts 2 and 3. Summary data for serum concentrations of IGF-1 were obtained using both methods (old and new reagent) and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | ng/mL (Mean) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Old Reagent: 6 hours post-dose | Old Reagent: Week 5 | Old Reagent: Week 9 | Old Reagent: Week 13 | Old Reagent: Week 17 | Old Reagent: Week 21 | Old Reagent: Week 25 (EOS/EW) | New Reagent: 6 hours post-dose | New Reagent: Week 5 | New Reagent: Week 9 | New Reagent: Week 13 | New Reagent: Week 17 | New Reagent: Week 21 | New Reagent: Week 25 (EOS/EW) | |
| 270 mg Lanreotide PRF | -7.1 | 27.9 | 71.4 | 111.1 | 96.2 | 135.5 | 136.4 | 6.0 | 3.0 | 13.0 | 30.0 | 20.5 | 65.0 | 45.5 |
Blood samples were collected for the determination of IGF-1 in serum at Baseline (pre-dose), 6 hours post-dose and at Weeks 5, 9 and 13. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW). Serum concentrations of IGF-1 were calculated using the Immulite 2000 Platform for all subjects in the safety population. The production of the reagent kits was stopped by the vendor during the study. The old reagent kits were used for Cohorts 1 and 2 until their expiry date and then the kits were switched to a new reagent and used for remaining subjects in Cohorts 2 and 3. Summary data for serum concentrations of IGF-1 were obtained using both methods (old and new reagent) and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | ng/mL (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Old Reagent: 6 hours post-dose | Old Reagent: Week 5 | Old Reagent: Week 9 | Old Reagent: Week 13 | Old Reagent: Week 17 | Old Reagent: Week 21 | Old Reagent: Week 25 (EOS/EW) | |
| 180 mg Lanreotide PRF | -1.8 | 2.4 | 72.3 | 53.4 | 48.3 | 72.4 | 86.3 |
Blood samples were collected for the determination of IGF-1 in serum at Baseline (pre-dose), 6 hours post-dose and at Weeks 5, 9 and 13. Samples were also collected during follow-up at Weeks 17, 21 and 25 (or EW). Serum concentrations of IGF-1 were calculated using the Immulite 2000 Platform for all subjects in the safety population. The production of the reagent kits was stopped by the vendor during the study. The old reagent kits were used for Cohorts 1 and 2 until their expiry date and then the kits were switched to a new reagent and used for remaining subjects in Cohorts 2 and 3. Summary data for serum concentrations of IGF-1 were obtained using both methods (old and new reagent) and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | ng/mL (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Old Reagent: 6 hours post-dose | Old Reagent: Week 5 | New Reagent: 6 hours post-dose | New Reagent: Week 5 | New Reagent: Week 9 | New Reagent: Week 13 | New Reagent: Week 17 | New Reagent: Week 21 | New Reagent: Week 25 (EOS/EW) | |
| 360 mg Lanreotide PRF | -46.5 | -32.0 | -11.6 | 1.3 | 25.2 | 47.1 | 40.9 | 56.9 | 64.1 |
Blood samples were collected for the determination of prolactin in serum at Baseline (pre-dose) and at Weeks 2, 5, 13 and 25 (or EW). Summary data for serum concentration of prolactin were calculated and the mean change from Baseline at each time point is presented. (NCT02396953)
Timeframe: From Baseline (pre-dose) up to Week 25.
| Intervention | mU/L (Mean) | |||
|---|---|---|---|---|
| Week 2 | Week 5 | Week 13 | Week 25 (EOS/EW) | |
| 180 mg Lanreotide PRF | -33.2 | -10.4 | -1.9 | 19.3 |
| 270 mg Lanreotide PRF | 37.6 | 16.3 | 33.9 | 58.3 |
| 360 mg Lanreotide PRF | 1.0 | 0.3 | -6.4 | -3.1 |
"The standardised mean change from Baseline in age-adjusted log-transformed IGF-1 standard deviation score (SDS) at EOST/EW is presented for subjects treated with both lanreotide Autogel and lanreotide PR. Back-transformed results are presented in addition to the results without back-transformation.~For each subject the IGF-1 SDS value was calculated based on the z-score derivation: IGF-1 SDS = (IGF-1 - mean)/ standard deviation (SD), with mean and SD derived from the upper limit of normal (ULN) and lower limit of normal (LLN) margins for each age category. ULN = Mean + 2 SD; LLN = Mean - 2 SD.~The SDS indicates the number of standard deviations away from the mean. A SDS of 0 is equal to the mean with negative numbers indicating values lower than the mean and positive values higher. A negative change in the SDS indicates a decrease in the mean age-adjusted IGF-1 values." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | SDS (Least Squares Mean) | |
|---|---|---|
| Without back-transformation | With back transformation | |
| Lanreotide Autogel | -0.84 | 0.43 |
| Lanreotide PR | -0.52 | 0.59 |
"The median percentage change in the solid component of the tumour volume from baseline to the EOST/EW Visit is presented.~The tumour volume was measured by MRI at Screening and at the EOST/EW Visit, and then assessed by two independent blinded readers." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage change in tumour volume (Median) |
|---|---|
| Lanreotide Autogel | -17.870 |
| Lanreotide PR | -20.120 |
The mean change from baseline in GH values at the EOST/EW Visit is presented for subjects treated with lanreotide Autogel and lanreotide PR. (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | mcg/L (Mean) |
|---|---|
| Lanreotide Autogel | -9.548 |
| Lanreotide PR | -13.182 |
"The percentage of subjects with GH ≤2.5 mcg/L at the EOST/EW Visit is presented for subjects treated with lanreotide Autogel and lanreotide PR.~At baseline, all subjects had GH levels >2.5 mcg/L as per protocol entry criteria." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) |
|---|---|
| Lanreotide Autogel | 29.7 |
| Lanreotide PR | 31.3 |
"The percentage of subjects with at least a 20% reduction in the solid component of the tumour volume at the EOST/EW Visit compared to baseline is presented for the subgroup of subjects who had solid tumours at baseline.~The tumour volume was measured by Magnetic Resonance Imaging (MRI) at Screening and at the EOST/EW Visit, and then assessed by two independent blinded readers." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) |
|---|---|
| Lanreotide Autogel | 45.5 |
| Lanreotide PR | 50.9 |
"The percentage of subjects with normal age-adjusted IGF-1 levels and who have GH levels >1 mcg/L but ≤2.5 mcg/L at the EOST/EW Visit is presented for subjects treated with lanreotide Autogel and lanreotide PR. The calculation of percentages was based on the overall ITT population.~At baseline, all subjects had abnormal IGF-1 levels and GH levels >2.5 mcg/L as per protocol entry criteria." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) |
|---|---|
| Lanreotide Autogel | 7.8 |
| Lanreotide PR | 3.1 |
"The percentage of subjects with normal age-adjusted IGF-1 levels at the EOST/EW Visit is presented for subjects treated with Lanreotide Autogel and Lanreotide PR.~At baseline, all subjects had abnormal IGF-1 levels as per protocol entry criteria." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) |
|---|---|
| Lanreotide Autogel | 15.6 |
| Lanreotide PR | 9.4 |
"The percentage of subjects with GH ≤1 mcg/L at the EOST/EW Visit is presented for subjects treated with lanreotide Autogel and lanreotide PR.~At baseline, all subjects had GH levels >2.5 mcg/L as per protocol entry criteria." (NCT02493517)
Timeframe: Baseline to EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) |
|---|---|
| Lanreotide Autogel | 10.9 |
| Lanreotide PR | 9.4 |
The percentage of subjects with at least one symptom of acromegaly at Week 13 and at the EOST/EW Visit compared with baseline is presented for subjects treated with lanreotide Autogel and lanreotide PR. The symptoms of acromegaly monitored included: headache, excessive perspiration, fatigue, soft tissue swelling and arthralgia. (NCT02493517)
Timeframe: Baseline, Week 13 Visit and EOST/EW Visit (up to Week 33 for the lanreotide Autogel group and up to Week 32 for the lanreotide PR group).
| Intervention | Percentage of Subjects (Number) | |
|---|---|---|
| Week 13 Visit | EOST/EW Visit | |
| Lanreotide Autogel | 70.3 | 75.0 |
| Lanreotide PR | 59.4 | 59.4 |
PanNET specific tumour peptide biomarkers were evaluated in pancreas subjects at baseline. Only the tumour biomarkers that were above normal range at baseline were evaluated every 12 weeks thereafter and at the end of study visit. The mean change from baseline values in picomole/liter (pmol/L) are presented for the end of study visit. (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks)
| Intervention | pmol/L (Mean) | |
|---|---|---|
| Pancreatic Polypeptide | Gastrin | |
| PanNET Cohort | 82.7 | -9.8 |
Subjects were asked to complete the EORTC QLQ-GI.NET21 module which comprised 21 questions that used a 4-point scale (1 = Not at all, 2 = A little, 3 = Quite a bit, 4 = Very much) to evaluate 3 defined multi-item symptom scales (endocrine, gastrointestinal and treatment related side effects), 2 single item symptoms (bone/muscle pain and concern about weight loss), 2 psychosocial scales (social function and disease-related worries) and 2 other single items (sexuality and communication). Answers were converted into grading scale, with values between 0 and 100. Each individual sub-score was transformed to range from 0 to 100. The mean change from baseline at the end of study/early withdrawal visit is presented with a higher score representing more or worse problems. (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET (and overall) cohort)
| Intervention | score on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Endocrine Symptoms | Gastrointestinal Symptoms | Treatment Related Symptoms | Social Function | Disease Related Worries | Muscle/Bone Pain | Sexual Function | Information/Communication Function | Body Image | |
| Midgut NET Cohort | -5.09 | -2.78 | -3.47 | -9.49 | -0.93 | 0.00 | -2.78 | -2.90 | -7.58 |
| Overall | -2.96 | -3.11 | 1.08 | -5.43 | 0.99 | -0.76 | 0.00 | 2.27 | -3.97 |
| PanNET Cohort | -0.53 | -3.49 | 5.93 | -0.79 | 3.17 | -1.67 | 2.38 | 7.94 | 0.00 |
The ORR was defined as the percentage of subjects who achieve either complete response (CR) or partial response (PR) according to RECIST v1.0 criteria. ORR was evaluated every 12 weeks and results are presented for each cohort. (NCT02651987)
Timeframe: Weeks 12, 24, 36, 48, 60 (for both cohorts) and Weeks 72, 84, and 96 (for midgut cohort)
| Intervention | percentage of subjects (Number) | ||||
|---|---|---|---|---|---|
| Week 12 | Week 24 | Week 36 | Week 48 | Week 60 | |
| PanNET Cohort | 0.0 | 0.0 | 0.0 | 0.0 | 0.0 |
The ORR was defined as the percentage of subjects who achieve either complete response (CR) or partial response (PR) according to RECIST v1.0 criteria. ORR was evaluated every 12 weeks and results are presented for each cohort. (NCT02651987)
Timeframe: Weeks 12, 24, 36, 48, 60 (for both cohorts) and Weeks 72, 84, and 96 (for midgut cohort)
| Intervention | percentage of subjects (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 12 | Week 24 | Week 36 | Week 48 | Week 60 | Week 72 | Week 84 | Week 96 | |
| Midgut NET Cohort | 0.0 | 0.0 | 0.0 | 0.0 | 2.0 | 3.9 | 2.0 | 2.0 |
The percentage of subjects alive and progression-free was assessed throughout the study up to Week 60 for the panNET cohort and Week 96 for the midgut cohort. Disease progression was assessed by tumour response evaluation according to RECIST v1.0, every 12 weeks measured by independent central review using the same imaging technique (CT scan or MRI) for each subject throughout the study. The percentage of subjects alive and progression free was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: Weeks 12, 24, 36, 48, 60 (for both cohorts) and Weeks 72, 84 and 96 (for midgut NET cohort)
| Intervention | percentage of subjects (Number) | ||||
|---|---|---|---|---|---|
| Week 12 | Week 24 | Week 36 | Week 48 | Week 60 | |
| PanNET Cohort | 93.3 | 64.4 | 37.8 | 28.5 | 20.7 |
The percentage of subjects alive and progression-free was assessed throughout the study up to Week 60 for the panNET cohort and Week 96 for the midgut cohort. Disease progression was assessed by tumour response evaluation according to RECIST v1.0, every 12 weeks measured by independent central review using the same imaging technique (CT scan or MRI) for each subject throughout the study. The percentage of subjects alive and progression free was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: Weeks 12, 24, 36, 48, 60 (for both cohorts) and Weeks 72, 84 and 96 (for midgut NET cohort)
| Intervention | percentage of subjects (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Week 12 | Week 24 | Week 36 | Week 48 | Week 60 | Week 72 | Week 84 | Week 96 | |
| Midgut NET Cohort | 91.8 | 65.3 | 59.2 | 38.3 | 36.1 | 29.8 | 27.5 | 25.2 |
"A univariate cox proportional hazards model was used to assess whether the following factors were associated with PFS:~Hepatic tumour load: >25% versus reference ≤25%~Tumour Grade: Grade 2 versus reference Grade 1,~Previous surgery of the primary tumour: No versus reference Yes,~Proliferation index Ki67: ≥10% versus reference <10%~Duration of treatment with lanreotide Autogel® 120 mg every 28 days by category: ≥median value versus reference
Timeframe: Screening/Baseline (Day 1)
| Intervention | Hazard Ratio (Number) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Hepatic tumour load: >25% Vs ≤25% | Tumour Grade: 2 Vs 1 | Previous surgery: No Vs Yes | Ki67: ≥10% Vs <10% | Duration of treatment with lanreotide Autogel® 120 mg every 28 days: ≥median Vs | Age: ≥65 years Vs <65 years | Time from diagnosis: ≥3 years Vs <3 years | Time between CT scans: ≥12 months Vs <12 months | Symptoms: No Vs Yes | | |
| Midgut NET Cohort | 1.54 | 0.90 | 2.14 | 2.26 | 0.76 | 1.15 | 0.94 | 0.72 | 1.32 |
| PanNET Cohort | 0.96 | 0.68 | 1.04 | 3.60 | 0.68 | 1.55 | 0.49 | 0.47 | 2.55 |
"Subjects were instructed to complete the EQ-5D-5L descriptive system at baseline and every 12 weeks throughout the study.~The EQ-5D-5L descriptive system comprised the following 5 dimensions: mobility, self-care, usual activities, pain/discomfort and anxiety/depression. Each dimension had 5 levels: no problems, slight problems, moderate problems, severe problems, extreme problems. The EQ-5D-5L health states, defined by the EQ-5D-5L descriptive system, was converted into a single index value with scores ranging from 0 (no problems) to 1 (extreme problems). The mean change from baseline at the end of study/early withdrawal visit is presented with a positive change from baseline in the index values indicating a worsening of symptoms." (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET (and overall) cohort)
| Intervention | Index value (Mean) |
|---|---|
| PanNET Cohort | -0.04 |
| Midgut NET Cohort | 0.00 |
| Overall | -0.02 |
Subjects were instructed to complete the EQ-5D-5L VAS at baseline and every 12 weeks throughout the study. The EQ-5D-5L VAS recorded the subject's self-rated health on a vertical VAS which is numbered from 0 (worst health state) to 100 (best health state). The mean change from baseline at the end of study/early withdrawal visit is presented with a positive change in the VAS indicating an improvement in symptoms. (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET (and overall) cohort)
| Intervention | score on a scale (Mean) |
|---|---|
| PanNET Cohort | -1.90 |
| Midgut NET Cohort | -1.76 |
| Overall | -1.83 |
PanNET specific tumour peptide biomarkers were evaluated in pancreas subjects at baseline. Only the tumour biomarkers that were above normal range at baseline were evaluated every 12 weeks thereafter and at the end of study visit. The mean change from baseline values in nanograms (ng)/L are presented for the end of study visit. (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks)
| Intervention | ng/L (Mean) |
|---|---|
| PanNET Cohort | 5.5 |
"Subjects were instructed to complete the 30 questions in the EORTC-QLQ-C30 v3.0 questionnaire at baseline and every 12 weeks throughout the study.~The global health status sub-score was assessed using the last 2 questions which represented subject's assessment of overall health & QoL. Each question was coded on a 7-point scale (1=very poor to 7=excellent). The sub-score was transformed to range from 0-100, with a high score for global health status representing a high QoL. The mean change from baseline in the transformed global health status are presented for the end of study/early withdrawal visit, with a positive change indicating an improvement in QoL." (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET (and overall) cohort)
| Intervention | score on a scale (Mean) |
|---|---|
| PanNET Cohort | -0.38 |
| Midgut NET Cohort | -1.33 |
| Overall | -0.89 |
Median duration of SD was the time from first injection of lanreotide Autogel® 120 mg every 14 days until the first occurrence of PD by central assessment. Disease progression was assessed by tumour response evaluation according to RECIST v1.0, every 12 weeks, measured using the same imaging technique (CT scan or MRI) for each subject throughout the study. Median duration of stable disease was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: From Day 1 up to Week 60 for the panNET cohort and Week 103 for the midgut NET cohort
| Intervention | months (Median) |
|---|---|
| PanNET Cohort | 8.3 |
| Midgut NET Cohort | 13.8 |
PFS was defined as the time from first injection of lanreotide Autogel® 120 mg every 14 days to progression or death. Disease progression was assessed by tumour response evaluation according to RECIST v1.0, every 12 weeks, measured by independent central review using the same imaging technique (computed tomography [CT] scan or magnetic resonance imaging [MRI]) for each subject throughout the study. The median PFS time was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: From Day 1 up to Week 60 for the panNET cohort and Week 103 for the midgut NET cohort
| Intervention | months (Median) |
|---|---|
| PanNET Cohort | 5.6 |
| Midgut NET Cohort | 8.3 |
Time to Progression was defined as time from first injection of lanreotide Autogel® 120 mg every 14 days to progression. Disease progression was assessed by tumour response evaluation according to RECIST v1.0, every 12 weeks, measured by independent central review using the same imaging technique (CT scan or MRI) for each subject throughout the study. Median time to progression was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: From Day 1 up to Week 60 for the panNET cohort and Week 103 for the midgut NET cohort
| Intervention | months (Median) |
|---|---|
| PanNET Cohort | 5.6 |
| Midgut NET Cohort | 8.7 |
Overall survival was defined as the time in months from the first injection of lanreotide Autogel® 120 mg every 14 days to death due to any cause. Median overall survival was estimated using the Kaplan Meier method for each cohort. (NCT02651987)
Timeframe: From Day 1 up to Week 60 for the panNET cohort and Week 103 for the midgut NET cohort
| Intervention | months (Median) |
|---|---|
| PanNET Cohort | NA |
| Midgut NET Cohort | NA |
Best overall response was defined as the best response recorded from the initiation of treatment until disease progression, according to RECIST v1.0 evaluation. The percentage of subjects in each response category and those who were non-evaluable (i.e. with no tumour assessment after the start of study treatment) throughout the study are presented for each cohort. (NCT02651987)
Timeframe: From Day 1 up to Week 60 for the panNET cohort and Week 103 for the midgut NET cohort
| Intervention | percentage of subjects (Number) | ||||
|---|---|---|---|---|---|
| CR | PR | SD | PD | Not evaluable | |
| Midgut NET Cohort | 0.0 | 3.9 | 68.6 | 23.5 | 2.0 |
| PanNET Cohort | 0.0 | 0.0 | 66.7 | 31.3 | 0.0 |
The DCR was defined as the percentage of subjects who achieved CR plus PR plus Stable Disease (SD), evaluated according to RECIST v1.0 criteria. The DCR at Weeks 24 and 48 is presented for each cohort. (NCT02651987)
Timeframe: Weeks 24 and 48
| Intervention | percentage of subjects (Number) | |
|---|---|---|
| Week 24 | Week 48 | |
| Midgut NET Cohort | 58.8 | 33.3 |
| PanNET Cohort | 43.8 | 22.9 |
Nonspecific tumour peptide biomarkers (chromogranin A [CgA], neuron specific enolase [NSE] and plasma/urinary 5-hydroxyindoleacetic acid [5-HIAA]) were evaluated in both pancreas and midgut subjects at baseline and Week 12 and every 12 weeks thereafter. At all scheduled visits, except baseline, plasma/urinary 5-HIAA was only performed in subjects with symptoms of carcinoid syndrome (diarrhoea and/or flushing) or if urinary 5-HIAA was elevated (above upper limit of normal [ULN]) at baseline. Mean change from baseline values were normalised by the ULN (xULN) and are presented for each cohort. (NCT02651987)
Timeframe: Baseline (Day 1) and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET cohort)
| Intervention | xULN (Mean) | ||
|---|---|---|---|
| CgA | NSE | Plasma 5-HIAA | |
| Midgut NET Cohort | 0.370 | -0.49 | 3.90 |
| PanNET Cohort | 0.205 | 0.03 | -0.42 |
Symptom control was measured by the total number of stools (diarrhoea) and flushing episodes during the 7 days prior to the visit, reported orally by the subject to the investigator. The mean change from baseline in number of stools and flushing episodes reported at each visit is presented for each cohort. (NCT02651987)
Timeframe: Baseline (Day 1), Weeks 8,12, 48 and end of study (approximately 64 weeks for panNET cohort and 108 weeks for midgut NET cohort)
| Intervention | episodes (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Stools - Week 8 | Stools - Week 12 | Stools - Week 48 | Stools - End of Study | Flushing - Week 8 | Flushing - Week 12 | Flushing - Week 48 | Flushing - End of Study | |
| Midgut NET Cohort | -1.0 | 0.7 | 3.4 | -1.2 | -3.3 | 1.5 | -1.5 | -0.5 |
| PanNET Cohort | 1.0 | -1.2 | -1.0 | 0.5 | 0.7 | -1.0 | -1.0 | 0.0 |
Blood samples were collected to determine plasma CgA. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). The x of upper limit of normal (ULN) was calculated as raw value/ULN. (NCT02683941)
Timeframe: Baseline, Weeks 8, 12, 24, and 48, and post-treatment in the double-blind phase (a maximum of 15 months); Baseline, Weeks 12, 24, and 48, and post-treatment in the the open-label treatment phase (a maximum of 33 months)
| Intervention | x of ULN (Mean) | ||||
|---|---|---|---|---|---|
| Week 8 | Week 12 | Week 24 | Week 48 | Post-treatment | |
| Double-Blind Phase: Lanreotide | -213.63 | -214.49 | -3.42 | -4.07 | 12.22 |
| Double-Blind Phase: Placebo | 0.09 | 5.73 | 60.41 | 1.24 | 160.11 |
Blood samples were collected to determine plasma CgA. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). The x of upper limit of normal (ULN) was calculated as raw value/ULN. (NCT02683941)
Timeframe: Baseline, Weeks 8, 12, 24, and 48, and post-treatment in the double-blind phase (a maximum of 15 months); Baseline, Weeks 12, 24, and 48, and post-treatment in the the open-label treatment phase (a maximum of 33 months)
| Intervention | x of ULN (Mean) | |||
|---|---|---|---|---|
| Week 12 | Week 24 | Week 48 | Post-treatment | |
| Open-Label Treatment Phase: All Subjects | -28.27 | -1.42 | -1.66 | -31.59 |
TTF was defined as the time from randomisation to disease progression using RECIST v1.1, death, consent withdrawn, an adverse event, protocol deviations, lost to follow-up, the appearance of carcinoid syndrome or other hormone related syndrome necessitating the initiation of SSAs (rescue octreotide and/or long-acting release SSA), or initiation of anticancer treatment in the double-blind phase. The distribution of TTF times were estimated using the Kaplan-Meier product limit method. (NCT02683941)
Timeframe: Up to a maximum of 15 months
| Intervention | months (Median) |
|---|---|
| Double-Blind Phase: Lanreotide | 13.3 |
| Double-Blind Phase: Placebo | 9.8 |
Measured in subjects with an elevated CgA at baseline (≥2 x ULN). Blood samples were collected to determine plasma CgA. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). (NCT02683941)
Timeframe: Baseline and Week 8 in the double-blind phase; Baseline and Week 8 in the open-label treatment phase
| Intervention | percentage of subjects (Number) |
|---|---|
| Double-Blind Phase: Lanreotide | 63.3 |
| Double-Blind Phase: Placebo | 7.7 |
| Open-Label Treatment Phase: All Subjects | 73.7 |
QoL deterioration was defined by a decrease from baseline in EORTC QLQ-C30 Global Health Status/QoL Score of at least 10 points. The EORTC QLQ-C30 (V3.0) consisted of 30 questions. The final 2 questions were related to global health status/QoL, with responses requested on a 7-point scale from 1 ('Very poor') to 7 ('Excellent'). The global health status/QoL scale ranges in score from 0 to 100. A high score for the global health status/QoL scale represents a high QoL, thus, an increase in score represents an increase in QoL. 95% Clopper-Pearson confidence intervals were estimated using the exact method for binomial distributions. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). (NCT02683941)
Timeframe: Baseline and post-treatment in the double-blind phase (a maximum of 15 months); Baseline and post-treatment in the open-label treatment phase (a maximum of 33 months)
| Intervention | percentage of subjects (Number) |
|---|---|
| Double-Blind Phase: Lanreotide | 32.0 |
| Double-Blind Phase: Placebo | 66.7 |
| Open-Label Treatment Phase: All Subjects | 23.5 |
PFS for subjects randomised in the lanreotide group, assessed by central review using Response Evaluation Criteria In Solid Tumours Version 1.1 (RECIST v1.1) criteria every 12 weeks, defined as the time from randomisation to disease progression or death from any causes during either the double-blind phase, or the open-label treatment phase. The distribution of PFS times were estimated using the Kaplan-Meier product limit method. (NCT02683941)
Timeframe: Up to a maximum of 33 months
| Intervention | months (Median) |
|---|---|
| Overall Study: Lanreotide | 16.6 |
Measured in subjects with an elevated 5-HIAA at baseline (≥2 x ULN). The assessment of urinary 5-HIAA required subjects to collect their urine for the 24 hour period prior to the study visit. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). The x of ULN was calculated as raw value/ULN. (NCT02683941)
Timeframe: Baseline, Weeks 8, 12, 24, and 48, and post-treatment in the double-blind phase (a maximum of 15 months); Baseline, Weeks 12, 24, and 48, and post-treatment in the the open-label treatment phase (a maximum of 33 months)
| Intervention | x of ULN (Mean) | |||
|---|---|---|---|---|
| Week 12 | Week 24 | Week 48 | Post-treatment | |
| Open-Label Treatment Phase: All Subjects | -0.47 | -4.84 | -2.47 | 0.60 |
PFS was assessed by central review using RECIST v1.1 criteria every 12 weeks, defined as the time from randomisation to disease progression or death from any causes during the double-blind phase. The distribution of PFS times were estimated using the Kaplan-Meier product limit method. (NCT02683941)
Timeframe: Up to a maximum of 15 months
| Intervention | months (Median) |
|---|---|
| Double-Blind Phase: Lanreotide | 16.6 |
| Double-Blind Phase: Placebo | 13.6 |
ORR was assessed by central review and local review using RECIST v1.1 criteria every 12 weeks, defined as the percentage of subjects who achieved a best overall response of complete response or partial response in the double-blind phase. (NCT02683941)
Timeframe: Up to a maximum of 15 months
| Intervention | Percentage of subjects (Number) | |
|---|---|---|
| Central review | Local review | |
| Double-Blind Phase: Lanreotide | 14.00 | 6.00 |
| Double-Blind Phase: Placebo | 0.00 | 4.00 |
PFS was assessed by local review using RECIST v1.1 criteria every 12 weeks, defined as the time from randomisation to disease progression or death from any causes during the double-blind phase. The distribution of PFS times were estimated using the Kaplan-Meier product limit method. (NCT02683941)
Timeframe: Up to a maximum of 15 months
| Intervention | months (Median) |
|---|---|
| Double-Blind Phase: Lanreotide | 14.1 |
| Double-Blind Phase: Placebo | 13.6 |
Measured in subjects with an elevated 5-HIAA at baseline (≥2 x ULN). The assessment of urinary 5-HIAA required subjects to collect their urine for the 24 hour period prior to the study visit. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). The x of ULN was calculated as raw value/ULN. (NCT02683941)
Timeframe: Baseline, Weeks 8, 12, 24, and 48, and post-treatment in the double-blind phase (a maximum of 15 months); Baseline, Weeks 12, 24, and 48, and post-treatment in the the open-label treatment phase (a maximum of 33 months)
| Intervention | x of ULN (Mean) | ||||
|---|---|---|---|---|---|
| Week 8 | Week 12 | Week 24 | Week 48 | Post-treatment | |
| Double-Blind Phase: Lanreotide | -2.90 | 0.21 | 0.15 | -3.00 | -1.27 |
| Double-Blind Phase: Placebo | 2.78 | 5.38 | -1.40 | 1.13 | -5.13 |
The EORTC QLQ-C30 (V3.0) consisted of 30 questions. The final 2 questions were related to global health status/QoL, with responses requested on a 7-point scale from 1 ('Very poor') to 7 ('Excellent'). The global health status/QoL scale ranges in score from 0 to 100. A high score for the global health status/QoL scale represents a high QoL, thus, an increase in score represents an increase in QoL. 95% Clopper-Pearson confidence intervals were estimated using the exact method for binomial distributions. Baseline was defined as the last non-missing measurement collected prior to the first dose of study treatment (lanreotide). (NCT02683941)
Timeframe: Baseline and post-treatment in the double-blind phase (a maximum of 15 months); Baseline and post-treatment in the open-label treatment phase (a maximum of 33 months)
| Intervention | score on a scale (Mean) |
|---|---|
| Double-Blind Phase: Lanreotide | -2.7 |
| Double-Blind Phase: Placebo | -19.4 |
| Open-Label Treatment Phase: All Subjects | 0.0 |
Differences between central radiology review and local investigator review were assessed according to the DCR status and the number of agreements and disagreements between the evaluators (central versus local) along with the p-values from the kappa test. A kappa statistic was used to evaluate the concordance between the central and the local review. (NCT02698410)
Timeframe: Month 9
| Intervention | kappa coefficient (Number) |
|---|---|
| Lanreotide ATG Plus Temozolomide | 0.71 |
The DCR was defined as SD, PR or CR according to RECIST criteria v1.1. A second set of the original computed tomography (CT) scan images were used for a centralized RECIST v1.1 assessment by an independent radiologist. (NCT02698410)
Timeframe: Up to Month 9
| Intervention | percentage of participants (Number) |
|---|---|
| Lanreotide ATG Plus Temozolomide | 28.2 |
The BOR was defined as the highest OR achieved by the participant from the time of first treatment until disease progression/recurrence or the end of study according to RECIST criteria v1.1 and was classified as: CR > PR > Non-CR/Non-progressive disease (NCR/NPD) > SD > PD > ND > not evaluable (NE). The BOR was assessed locally by the investigator and centrally by an independent radiologist. Percentages are based on the number of participants in the ITT/Safety population with non-missing observations. (NCT02698410)
Timeframe: From Day 1 up to end of study, 52 weeks
| Intervention | percentage of participants (Number) | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Local assessment: CR | Local assessment: PR | Local assessment: SD | Local assessment: NCR/NPD | Local assessment: PD | Local assessment: NE | Local assessment: Not applicable | Central assessment: CR | Central assessment: PR | Central assessment: SD | Central assessment: NCR/NPD | Central assessment: PD | Central assessment: NE | Central assessment: Not applicable | |
| Lanreotide ATG Plus Temozolomide | 0 | 7.7 | 71.8 | 0 | 20.5 | 0 | 0 | 0 | 13.2 | 65.8 | 2.6 | 15.8 | 0 | 2.6 |
The DCR was defined as SD, PR or CR according to RECIST criteria v1.1. The DCR was assessed locally by the investigator and centrally by an independent radiologist. (NCT02698410)
Timeframe: Month 12
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Local assessment | Central assessment | |
| Lanreotide ATG Plus Temozolomide | 17.5 | 15.4 |
The influence of type of carcinoid [typical, atypical and undetermined carcinoid neuroendocrine tumors (NET)] on the local and central DCR at 9 months was analysed. Typical carcinoids were defined with absent foci of necrosis and mitotic count < 2 mitoses/2 millimeters^2 (mm^2); atypical carcinoids were defined with presence of foci of necrosis and/or 2 mitoses/2 mm^2 <= mitotic count <= 10 mitoses/2 mm^2; and carcinoid NET were defined as confirmed carcinoid without foci of necrosis and/or mitotic count reported. The DCR was assessed locally by the investigator and centrally by an independent radiologist. (NCT02698410)
Timeframe: Up to Month 9
| Intervention | percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| Local assessment: Typical carcinoid | Local assessment: Atypical carcinoid | Local assessment: Carcinoid NET | Central assessment: Typical carcinoid | Central assessment: Atypical carcinoid | Central assessment: Carcinoid NET | |
| Lanreotide ATG Plus Temozolomide | 12.5 | 47.6 | 27.3 | 0 | 35.0 | 36.4 |
Responders were participants who showed disease control according to Response Evaluation Criteria in Solid Tumors (RECIST) criteria v 1.1 assessed locally by the investigator. The DCR was defined as complete response (CR), partial response (PR) or stable disease (SD) according to RECIST criteria v1.1. A sensitivity analysis-1 of local DCR was performed excluding participants withdrawn before 9 months with reason other than progressive disease (PD) or missing assessment and considering participants with PD prior or at 9 months as failures. In addition, a sensitivity analysis-2 was performed in order to consider assessments done between 7.5 and 10.5 months as 9 months assessments when 9-month assessment was missing using same methodology, i.e. considering PD prior or at 9 months and participants withdrawn with other or missing reasons as failures. (NCT02698410)
Timeframe: Up to Month 9; for sensitivity analysis-2, up to 10.5 months
| Intervention | percentage of participants (Number) | ||
|---|---|---|---|
| DCR at Month 9 | Sensitivity analysis-1 | Sensitivity analysis-2 | |
| Lanreotide ATG Plus Temozolomide | 35.0 | 45.2 | 45.0 |
The following biomarkers were investigated: Immunohistochemistry assay SSTR2 including HER-2 score (0, 1+, 2+, 3+ and +ve versus -ve); H-score (from 0 to 300 as quantitative variable and +ve versus -ve); IRS score (from 0 to 12 and reference for odds ratio was 0-1). Ki67 index (from 0% to 100% and reference for odds ratio was 4%-25%). MGMT expression including percentage of +ve nuclei stained and methylated sites and H-score (from 0 to 300 as quantitative variable). For all these categories, higher score indicates a higher expression of biomarkers. Carcinoid type (typical or NET) was also investigated. Prognostic value of biomarkers expression at screening on DCR were assessed locally and centrally using univariate logistic regression models. (NCT02698410)
Timeframe: Screening period, Months 9 and 12
| Intervention | odds ratio (Number) | |||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Month 9: Local: SSTR2: HER-2 score; +ve (2+, 3+) | Month 9: Local: SSTR2: H-score; +ve (>= 50) | Month 9: Local: SSTR2: IRS score; 2-3 | Month 9: Local: SSTR2: IRS score; 4-8 | Month 9: Local: SSTR2: IRS score; 9-12 | Month 9: Local: Ki67: <4 | Month 9: Local: Ki67: >=25 | Month 9:Local: MGMT: +ve nuclei stained; +ve(>=5%) | Month 9: Local: MGMT: Methylated sites; +ve (>10%) | Month 9: Local: MGMT: H-score | Month 9: Local: Carcinoid type: Typical | Month 9: Local: Carcinoid type: Carcinoid NET | Month 9: Central: SSTR2: HER-2 score; +ve (2+, 3+) | Month 9: Central: SSTR2: H-score; +ve (>= 50) | Month 9: Central: SSTR2: IRS score; 2-3 | Month 9: Central: SSTR2: IRS score; 4-8 | Month 9: Central: SSTR2: IRS score; 9-12 | Month 9: Central: Ki67: <4 | Month 9: Central: Ki67: >=25 | Month 9:Central:MGMT:+ve nuclei stained; +ve(>=5%) | Month 9:Central: MGMT: Methylated sites; +ve(>10%) | Month 9: Central: MGMT: H-score | Month 9: Central: Carcinoid type: Typical | Month 9: Central: Carcinoid type: Carcinoid NET | Month 12: Local: SSTR2: HER-2 score; +ve (2+, 3+) | Month 12: Local: SSTR2: H-score; +ve (>= 50) | Month 12: Local: SSTR2: IRS score; 2-3 | Month 12: Local: SSTR2: IRS score; 4-8 | Month 12: Local: SSTR2: IRS score; 9-12 | Month 12: Local: Ki67: <4 | Month 12: Local: Ki67: >=25 | Month 12:Local:MGMT: +ve nuclei stained; +ve(>=5%) | Month 12: Local: MGMT: Methylated sites; +ve(>10%) | Month 12: Local: MGMT: H-score | Month 12: Local: Carcinoid type: Typical | Month 12: Local: Carcinoid type: Carcinoid NET | Month 12: Central: SSTR2: HER-2 score; +ve(2+, 3+) | Month 12: Central: SSTR2: H-score; +ve (>= 50) | Month 12: Central: SSTR2: IRS score; 2-3 | Month 12: Central: SSTR2: IRS score; 4-8 | Month 12: Central: SSTR2: IRS score; 9-12 | Month 12: Central: Ki67: <4 | Month 12: Central: Ki67: >=25 | Month 12:Central:MGMT:+ve nuclei stained;+ve(>=5%) | Month 12:Central: MGMT: Methylated sites;+ve(>10%) | Month 12: Central: MGMT: H-score | Month 12: Central: Carcinoid type: Typical | Month 12: Central: Carcinoid type: Carcinoid NET | |
| Lanreotide ATG Plus Temozolomide | 0.90 | 0.78 | NA | 0.67 | 12.00 | NA | 1.67 | NA | 3.25 | 0.99 | 0.16 | 0.41 | 1.40 | 2.25 | 3.00 | 0.67 | 12.00 | NA | NA | 0.50 | 5.00 | 1.00 | NA | 1.06 | 3.00 | 4.40 | NA | 0.70 | 10.50 | NA | NA | 0.20 | 2.13 | 0.99 | 0.46 | 0.32 | 2.08 | 3.00 | NA | NA | 10.50 | NA | NA | 0.14 | 3.00 | 0.99 | 0.57 | 0.40 |
The following biomarkers were investigated: Immunohistochemistry assay human somatostatin receptors 2 (SSTR2) including human epidermal growth factor receptor 2 (HER-2) score [0, 1+, 2+, 3+ and positive (+ve) versus negative (-ve)]; hormone receptor score (H-score) (from 0 to 300 as quantitative variable and +ve versus -ve); immunoreactive score (IRS) score (from 0 to 12 and reference for hazard ratio was 0-1). Ki67 index (from 0% to 100% and reference for hazard ratio was 4%-25%). O^6-methylguanine-DNA methyltransferase (MGMT) expression including percentage of +ve nuclei stained and methylated sites and H-score (from 0 to 300 as quantitative variable). For all these categories, higher score indicates a higher expression of biomarkers. Carcinoid type (typical or NET) was also investigated. Prognostic value of biomarkers expression at screening on PFS were assessed locally and centrally using univariate cox proportional hazard models. (NCT02698410)
Timeframe: From Screening period (-4 weeks) up to Week 52
| Intervention | hazard ratio (Number) | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Local: SSTR2: HER-2 score; +ve (2+, 3+) | Local: SSTR2: H-score; +ve (>= 50) | Local: SSTR2: IRS score; 2-3 | Local: SSTR2: IRS score; 4-8 | Local: SSTR2: IRS score; 9-12 | Local: Ki67: <4 | Local: Ki67: >=25 | Local: MGMT: +ve nuclei stained; +ve (>=5%) | Local: MGMT: Methylated sites; +ve (>10%) | Local: MGMT: H-score | Local: Carcinoid type: Typical | Local: Carcinoid type: Carcinoid NET | Central: SSTR2: HER-2 score; +ve (2+, 3+) | Central: SSTR2: H-score; +ve (>= 50) | Central: SSTR2: IRS score; 2-3 | Central: SSTR2: IRS score; 4-8 | Central: SSTR2: IRS score; 9-12 | Central: Ki67: <4 | Central: Ki67: >=25 | Central: MGMT: +ve nuclei stained; +ve (>=5%) | Central: MGMT: Methylated sites; +ve (>10%) | Central: MGMT: H-score | Central: Carcinoid type: Typical | Central: Carcinoid type: Carcinoid NET | |
| Lanreotide ATG Plus Temozolomide | 0.71 | 0.66 | 0.31 | 0.90 | 0.12 | 1.08 | 1.68 | 2.06 | 0.41 | 1.00 | 1.05 | 1.59 | 0.50 | 0.36 | 0.78 | 0.88 | 0.10 | 0.00 | 2.75 | 2.11 | 0.73 | 1.00 | 0.99 | 0.61 |
The DOR was defined as the time from onset of the first objective tumor response (PR or CR) to objective tumor progression (PD) according to RECIST criteria v 1.1. The DOR was assessed locally by the investigator and centrally by an independent radiologist. (NCT02698410)
Timeframe: From Day 1 up to end of study, 52 weeks
| Intervention | weeks (Median) | |
|---|---|---|
| Local assessment | Central assessment | |
| Lanreotide ATG Plus Temozolomide | NA | NA |
The PFS was defined as the time from the first treatment administration to disease progression according to RECIST criteria v 1.1 or death from any cause. The PFS was assessed locally by the investigator and centrally by an independent radiologist. The distribution of PFS times was estimated using the Kaplan-Meier method. The PFS of participants who were lost to follow-up and those who had not progressed at end of study were censored at the date of the last disease assessment. (NCT02698410)
Timeframe: From Day 1 up to end of study, 52 weeks
| Intervention | weeks (Median) | |
|---|---|---|
| Local assessment | Central assessment | |
| Lanreotide ATG Plus Temozolomide | 37.1 | 37.1 |
The TTP was defined as the time from first treatment administration to the first objective tumor progression (PD) according to RECIST criteria v 1.1. The TTP was assessed locally by the investigator and centrally by an independent radiologist. The distribution of TTP times was estimated using the Kaplan-Meier method. The TTP of participants who were lost to follow-up, and those who had not progressed at end of study were censored at the date of the last disease assessment. (NCT02698410)
Timeframe: From Day 1 up to end of study, 52 weeks
| Intervention | weeks (Median) | |
|---|---|---|
| Local assessment | Central assessment | |
| Lanreotide ATG Plus Temozolomide | 37.1 | 37.1 |
The TTR was defined as the time from first treatment administration to the first objective tumor response (PR or CR according to RECIST criteria v 1.1). The TTR was assessed locally by the investigator and centrally by an independent radiologist. The distribution of TTR was estimated using the Kaplan-Meier method. The TTR of participants who were lost to follow-up or died prior to any objective tumor response were censored at the date of the last disease assessment. (NCT02698410)
Timeframe: From Day 1 up to end of study, 52 weeks
| Intervention | weeks (Median) | |
|---|---|---|
| Local assessment | Central assessment | |
| Lanreotide ATG Plus Temozolomide | NA | NA |
The NSE and CgA levels were classified according to ULN as follows: < 1 ULN, 1-2 ULN and > 2 ULN. Baseline was defined as value at Day 1. Percentages are based on the number of participants in the ITT/Safety population who attended the visit with non-missing observations. (NCT02698410)
Timeframe: Baseline and Weeks 4, 12, 24, 36 and 52
| Intervention | percentage of participants (Number) | |||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| CgA: Baseline: <1 ULN | CgA: Baseline: 1-2 ULN | CgA: Baseline: >2 ULN | CgA: Week 4: <1 ULN | CgA: Week 4: 1-2 ULN | CgA: Week 4: >2 ULN | CgA: Week 12: <1 ULN | CgA: Week 12: 1-2 ULN | CgA: Week 12: >2 ULN | CgA: Week 24: <1 ULN | CgA: Week 24: 1-2 ULN | CgA: Week 24: >2 ULN | CgA: Week 36: <1 ULN | CgA: Week 36: 1-2 ULN | CgA: Week 36: >2 ULN | CgA: Week 52: <1 ULN | CgA: Week 52: 1-2 ULN | CgA: Week 52: >2 ULN | NSE: Baseline: <1 ULN | NSE: Baseline: 1-2 ULN | NSE: Baseline: >2 ULN | NSE: Week 4: <1 ULN | NSE: Week 4: 1-2 ULN | NSE: Week 4: >2 ULN | NSE: Week 12: <1 ULN | NSE: Week 12: 1-2 ULN | NSE: Week 12: >2 ULN | NSE: Week 24: <1 ULN | NSE: Week 24: 1-2 ULN | NSE: Week 24: >2 ULN | NSE: Week 36: <1 ULN | NSE: Week 36: 1-2 ULN | NSE: Week 36: >2 ULN | NSE: Week 52: <1 ULN | NSE: Week 52: 1-2 ULN | NSE: Week 52: >2 ULN | |
| Lanreotide ATG Plus Temozolomide | 40.0 | 15.0 | 45.0 | 34.3 | 22.9 | 42.9 | 46.4 | 17.9 | 35.7 | 30.0 | 25.0 | 45.0 | 31.3 | 12.5 | 56.3 | 27.3 | 9.1 | 63.6 | 65.0 | 25.0 | 10.0 | 62.9 | 25.7 | 11.4 | 78.6 | 17.9 | 3.6 | 80.0 | 10.0 | 10.0 | 87.5 | 6.3 | 6.3 | 63.6 | 18.2 | 18.2 |
The ORR was defined as the percentage of participants with CR or PR according to RECIST criteria v1.1. The ORR was assessed locally by the investigator and centrally by an independent radiologist. The ORR was based on the participants with PD prior to 9 and 12 months with respectively PD at 9 and 12 months, and participants withdrawn before the assessment for reason other than PD or missing as failures. (NCT02698410)
Timeframe: Months 9 and 12
| Intervention | percentage of participants (Number) | |||
|---|---|---|---|---|
| Local assessment: Month 9 | Local assessment: Month 12 | Central assessment: Month 9 | Central assessment: Month 12 | |
| Lanreotide ATG Plus Temozolomide | 2.5 | 2.5 | 5.1 | 2.6 |
Participants with baseline CgA plasma levels greater than the upper limit of normal (ULN) were assessed for a biochemical response. A biochemical responder was defined as a participant who had a decrease of CgA >= 50% compared to baseline, while biochemical SD was defined as a decrease < 50% or an increase <= 25% compared to baseline. Biochemical non-responders had an increase >25% compared to baseline. Baseline was defined as value at Day 1. (NCT02698410)
Timeframe: Baseline (Day 1) and Week 4, 12, 24, 36 and 52
| Intervention | percentage of participants (Number) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Week 4: Responders | Week 4: SD | Week 4: Non-responders | Week 12: Responders | Week 12: SD | Week 12: Non-responders | Week 24: Responders | Week 24: SD | Week 24: Non-responders | Week 36: Responders | Week 36: SD | Week 36: Non-responders | Week 52: Responders | Week 52: SD | Week 52: Non-responders | |
| Lanreotide ATG Plus Temozolomide | 27.3 | 59.1 | 13.6 | 37.5 | 37.5 | 25.0 | 23.1 | 30.8 | 46.2 | 36.4 | 27.3 | 36.4 | 12.5 | 50.0 | 37.5 |
Treatment-emergent Adverse Events were assessed according to National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) v4.03. (NCT02859064)
Timeframe: From the day of the first dose to 30 days after the last dose of study medication, up to 52 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Lanreotide/Y-90 Microspheres | 6 |
Percentage of patients with CR, PR or stable disease (SD) according to RECIST v1.1. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1),: Complete Response (CR): Disappearance of all target and non-target lesions; Partial Response (PR): >=30% decrease in the sum of the diameters of target lesions; Stable Disease: Meeting neither criteria for PR or Progression (PD= greater than 20% increase in the sum of diameters of target lesions, or an unequivocal increase in a non-target lesion, or the appearance of new lesions). Disease Control Rate (DCR) = CR + PR + SD. (NCT02859064)
Timeframe: At 12 weeks post-treatment with SIR-Spheres then every 8 weeks, up to 52 months.
| Intervention | percentage of participants (Number) |
|---|---|
| Lanreotide/Y-90 Microspheres | 100 |
Percentage of patients with confirmed complete or partial response (CR or PR) according to Response Evaluation Criteria in Solid Tumors (RECIST) v1.1. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.1),: Complete Response (CR): Disappearance of all target and non-target lesions; Partial Response (PR): >=30% decrease in the sum of the diameters of target lesions; Overall Response (OR) = CR + PR. (NCT02859064)
Timeframe: At 12 weeks post-treatment with SIR-Spheres then every 8 weeks, up to 52 months
| Intervention | percentage of participants (Number) |
|---|---|
| Lanreotide/Y-90 Microspheres | 16.7 |
The time from Day 1 of study drug administration until death from any cause. (NCT02859064)
Timeframe: At 12 weeks post-treatment with SIR-Spheres then every 8 weeks, up to 52 months
| Intervention | months (Median) |
|---|---|
| Lanreotide/Y-90 Microspheres | 11.5 |
The time from Day 1 of study drug administration to disease progression as defined by RECIST v1.1, or death on study. Per RECIST V1.1 criteria, progression is defined as a greater than 20% increase in the sum of diameters of target lesions, or an unequivocal increase in a non-target lesion, or the appearance of new lesions. (NCT02859064)
Timeframe: At 12 weeks post-treatment with SIR-Spheres then every 8 weeks, up to 52 months
| Intervention | months (Median) |
|---|---|
| Lanreotide/Y-90 Microspheres | 11 |
If the small bowel transit time, as measured by wireless capsule endoscopy, is decreased to < 6hrs, then patient would be considered a responder and that lanreotide is efficacious. (NCT03012594)
Timeframe: 3 months
| Intervention | minutes (Mean) | ||||
|---|---|---|---|---|---|
| Gastric emptying time | Small bowel transit time | Colonic transit time | Small bowel and Colonic transit time | Whole gut transit time | |
| Lanreotide | 371.52 | 392 | 4767 | 5159 | 5530 |
"Improvement in symptoms assessed by improvement in Patient Assessment of Gastrointestinal Disorders Symptom Severity Index(PAGI-SYM) scores. If the PAGI-Sym scores were decreased by at least 0.7 points at 3 months when compared to baseline/pre treatment, then it will be considered that Lanreotide has significantly improved the symptom severity. Higher values represent worse symptoms.~The participant rated each of the measured gastrointestinal symptom severity as described 0=No symptom, 1=Very Mild Symptom, 2= Mild Symptoms, 3= Moderate symptom, 4=Severe symptom, 5= Very Severe symptom.~PAGI-SYM is a brief (20-items with 6 sub scales) symptom severity questionnaire that captures information on common upper gastrointestinal symptoms which include including Heartburn/regurgitation, Nausea/vomiting, Fullness/early satiety, bloating, Upper abdominal pain, and Lower abdominal pain. The presented data is an average of each sub scale." (NCT03012594)
Timeframe: 3 months
| Intervention | score on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Heartburn/regurgitation | Nausea/vomiting | Fullness/early satiety | Bloating | Upper abdominal pain | Lower abdominal pain | |
| Lanreotide | 1.48 | 1.00 | 2.36 | 2.43 | 2.14 | 2.00 |
Adverse events were graded using the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE) version 4.0. (NCT03043664)
Timeframe: First 12 weeks of treatment
| Intervention | Participants (Count of Participants) |
|---|---|
| Somatuline Depot and Keytruda | 0 |
ORR is calculated as the number of people with a complete response (CR) or partial response (PR), divided by the total number of people treated. Complete response is defined as disappearance of all target lesions. Partial response is defined as at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum diameters. A lower limit of the true ORR will be estimated by the 90% exact lower confidence bound (LCB) for the binomial proportion. A 90% LCB of < 0.1 will be considered not to be of clinical value. If the 90% LCB is ≥ 0.1, the regimen will be considered efficacious. (NCT03043664)
Timeframe: Approximately every 12 weeks until study completion (up to 2 years)
| Intervention | proportion of participants (Number) |
|---|---|
| Somatuline Depot and Keytruda | 0.045 |
Treatment response as assessed by irRC instead of RECIST v1.1. ORR is calculated as the number of people with a complete response (CR) or partial response (PR), divided by the total number of people treated. Complete response is defined as complete disappearance of all lesions (whether measurable or not, and no new lesions), confirmed by a repeat, consecutive assessment no less than 4 weeks from the date first documented. Partial response is defined as a decrease in tumor burden ≥ 50% relative to baseline, confirmed by a consecutive assessment at least 4 weeks after first documentation. A lower limit of the true ORR will be estimated by the 90% exact lower confidence bound (LCB) for the binomial proportion. (NCT03043664)
Timeframe: Approximately every 12 weeks until study completion (up to 2 years)
| Intervention | proportion of participants (Number) |
|---|---|
| Somatuline Depot and Keytruda | 0.045 |
Months from treatment start date until the date of first documented radiographic progression or date of death from any cause (whichever is first); assessed up to 48 weeks after the last subject has finished study drug regimen. Progression is defined as at least a 20% increase in the sum of diameters of target lesions, taking as reference the smallest sum on study (this includes the baseline sum if that is the smallest on study). In addition to the relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. The appearance of one or more new lesions is also considered progression. (NCT03043664)
Timeframe: Up to 3 years
| Intervention | months (Median) |
|---|---|
| Somatuline Depot and Keytruda | 5.04 |
Months from treatment start date until the date of death from any cause; assessed up to 48 weeks after the last subject has finished the study drug regimen (NCT03043664)
Timeframe: Up to 59 months
| Intervention | months (Median) |
|---|---|
| Somatuline Depot and Keytruda | 28.6 |
Overall morbidity was defined based on the National Surgical Quality Improvement Program (NSQIP) templates. This measure counts the number of participants who had a complication during the 60-day study period. (NCT03174353)
Timeframe: Measured throughout 60 days
| Intervention | Participants (Count of Participants) |
|---|---|
| Lanreotide Arm | 26 |
Reduction in the incidence of intraabdominal abscess or development of clinically significant (grade B or C) pancreatic fistula within 60 postoperative days. The grading of the primary outcome measure is based on a method published by the International Study Group of Pancreatic Surgery (ISGPS) in 2005 and then revised in 2016. As this study was developed prior to the revision, the 2005 version was used. This system for grading pancreatic fistula is based on progressively increasing severity of the complication from grade A to C. Grade Grade A fistula are characterized by elevated amylase detected within fluid coming from drain(s) placed at the time of surgery. Grade B fistula require change in patient management such as need for drain placement or institution of antimicrobial therapy, while grade C fistula are associated with severe clinical signs or symptoms such as sepsis. Please refer to page 12 of the study protocol for further details. (NCT03174353)
Timeframe: Measured throughout 60 days
| Intervention | Participants (Count of Participants) |
|---|---|
| Lanreotide Arm | 8 |
Grade A pancreatic fistula will be defined based on principles noted in evaluation of Primary endpoint. Grade A fistula are characterized by elevated amylase detected within fluid coming from drain(s) placed at the time of surgery, but do not cause deviation from standard post-operative recovery. (NCT03174353)
Timeframe: Measured throughout 60 days
| Intervention | Participants (Count of Participants) |
|---|---|
| Lanreotide Arm | 12 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| 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. | 2.05 | 1 | 0 | monocarboxylic acid | antimicrobial food preservative; Daphnia magna metabolite; food acidity regulator; protic solvent |
| acetamide acetimidic acid : A carboximidic acid that is acetic acid in which the carbonyl oxygen is replaced by an imino group. | 2.05 | 1 | 0 | acetamides; carboximidic acid; monocarboxylic acid amide; N-acylammonia | |
| adenine [no description available] | 2.05 | 1 | 0 | 6-aminopurines; purine nucleobase | Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| allantoin [no description available] | 2.05 | 1 | 0 | imidazolidine-2,4-dione; ureas | Escherichia coli metabolite; human metabolite; Saccharomyces cerevisiae metabolite; vulnerary |
| quinacrine Quinacrine: An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.. quinacrine : A member of the class of acridines that is acridine substituted by a chloro group at position 6, a methoxy group at position 2 and a [5-(diethylamino)pentan-2-yl]nitrilo group at position 9. | 2.05 | 1 | 0 | acridines; aromatic ether; organochlorine compound; tertiary amino compound | antimalarial; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor |
| betaine glycine betaine : The amino acid betaine derived from glycine. | 2.05 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| carnitine [no description available] | 2.05 | 1 | 0 | amino-acid betaine | human metabolite; mouse metabolite |
| citric acid, anhydrous Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms. | 2.05 | 1 | 0 | tricarboxylic acid | antimicrobial agent; chelator; food acidity regulator; 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). | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| creatine [no description available] | 2.05 | 1 | 0 | glycine derivative; guanidines; zwitterion | geroprotector; human metabolite; mouse metabolite; neuroprotective agent; nutraceutical |
| lactic acid Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group. | 2.05 | 1 | 0 | 2-hydroxy monocarboxylic acid | algal metabolite; Daphnia magna metabolite |
| dimethyl sulfoxide Dimethyl Sulfoxide: A highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during CRYOPRESERVATION. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation.. dimethyl sulfoxide : A 2-carbon sulfoxide in which the sulfur atom has two methyl substituents. | 2.05 | 1 | 0 | sulfoxide; volatile organic compound | alkylating agent; antidote; Escherichia coli metabolite; geroprotector; MRI contrast agent; non-narcotic analgesic; polar aprotic solvent; radical scavenger |
| formaldehyde paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy | 2.05 | 1 | 0 | aldehyde; one-carbon compound | allergen; carcinogenic agent; disinfectant; EC 3.5.1.4 (amidase) inhibitor; environmental contaminant; Escherichia coli metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| glycine [no description available] | 2.05 | 1 | 0 | alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid | EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical |
| glycerol Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil. | 2.05 | 1 | 0 | alditol; triol | algal metabolite; detergent; Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; solvent |
| hydroquinone [no description available] | 2.05 | 1 | 0 | benzenediol; hydroquinones | antioxidant; carcinogenic agent; cofactor; Escherichia coli metabolite; human xenobiotic metabolite; mouse metabolite; skin lightening agent |
| 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. | 2.05 | 1 | 0 | cyclitol; hexol | |
| niacinamide nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group. | 2.05 | 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. | 2.05 | 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 |
| orotic acid Orotic Acid: An intermediate product in PYRIMIDINE synthesis which plays a role in chemical conversions between DIHYDROFOLATE and TETRAHYDROFOLATE.. orotic acid : A pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. | 2.05 | 1 | 0 | pyrimidinemonocarboxylic acid | Escherichia coli metabolite; metabolite; mouse metabolite |
| 4-aminobenzoic acid 4-Aminobenzoic Acid: An aminobenzoic acid isomer that combines with pteridine and GLUTAMIC ACID to form FOLIC ACID. The fact that 4-aminobenzoic acid absorbs light throughout the UVB range has also resulted in its use as an ingredient in SUNSCREENS.. 4-ammoniobenzoate : A zwitterion obtained by transfer of a proton from the carboxy to the amino group of 4-aminobenzoic acid.. 4-aminobenzoic acid : An aminobenzoic acid in which the amino group is para to the carboxy group. | 2.05 | 1 | 0 | aminobenzoic acid; aromatic amino-acid zwitterion | allergen; Escherichia coli metabolite; plant metabolite |
| phenol [no description available] | 2.05 | 1 | 0 | phenols | antiseptic drug; disinfectant; human xenobiotic metabolite; mouse metabolite |
| phenylacetic acid phenylacetic acid : A monocarboxylic acid that is toluene in which one of the hydrogens of the methyl group has been replaced by a carboxy group. | 2.05 | 1 | 0 | benzenes; monocarboxylic acid; phenylacetic acids | allergen; Aspergillus metabolite; auxin; EC 6.4.1.1 (pyruvate carboxylase) inhibitor; Escherichia coli metabolite; human metabolite; plant growth retardant; plant metabolite; Saccharomyces cerevisiae metabolite; toxin |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 2.05 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| pyridoxal phosphate Pyridoxal Phosphate: This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).. pyridoxal 5'-phosphate : The monophosphate ester obtained by condensation of phosphoric acid with the primary hydroxy group of pyridoxal. | 2.05 | 1 | 0 | methylpyridines; monohydroxypyridine; pyridinecarbaldehyde; vitamin B6 phosphate | coenzyme; cofactor; EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| 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). | 2.05 | 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. | 2.05 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| uracil 2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder | 2.05 | 1 | 0 | pyrimidine nucleobase; pyrimidone | allergen; Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; prodrug; Saccharomyces cerevisiae metabolite |
| urea pseudourea: clinical use; structure. isourea : A carboximidic acid that is the imidic acid tautomer of urea, H2NC(=NH)OH, and its hydrocarbyl derivatives. | 2.05 | 1 | 0 | isourea; monocarboxylic acid amide; one-carbon compound | Daphnia magna metabolite; Escherichia coli metabolite; fertilizer; flour treatment agent; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| catechin [no description available] | 2.05 | 1 | 0 | hydroxyflavan | |
| menthol Menthol: A monoterpene cyclohexanol produced from mint oils. | 2.05 | 1 | 0 | p-menthane monoterpenoid; secondary alcohol | volatile oil component |
| phenytoin [no description available] | 2.05 | 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. | 2.05 | 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. | 2.05 | 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) | 2.05 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohexamide Acetohexamide: A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide.. acetohexamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is replaced by a p-acetylphenylsulfonyl group, while a hydrogen attached to the other nitrogen is replaced by a cyclohexyl group. | 2.05 | 1 | 0 | acetophenones; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| acetohydroxamic acid acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group. | 2.05 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| albendazole [no description available] | 2.05 | 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). | 2.05 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alfuzosin alfuzosin: structure given in first source | 2.05 | 1 | 0 | monocarboxylic acid amide; quinazolines; tetrahydrofuranol | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 2.05 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ambroxol Ambroxol: A metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract. It is usually administered as the hydrochloride. | 2.05 | 1 | 0 | aromatic amine | |
| aminoglutethimide Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.. aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position. | 2.05 | 1 | 0 | dicarboximide; piperidones; substituted aniline | adrenergic agent; anticonvulsant; antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| pimagedine pimagedine: diamine oxidase & nitric oxide synthase inhibitor; an advanced glycosylation end product inhibitor; used in the treatment of diabetic complications; structure. aminoguanidine : A one-carbon compound whose unique structure renders it capable of acting as a derivative of hydrazine, guanidine or formamide. | 2.05 | 1 | 0 | guanidines; one-carbon compound | EC 1.14.13.39 (nitric oxide synthase) inhibitor; EC 1.4.3.4 (monoamine oxidase) inhibitor |
| theophylline [no description available] | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | carbotricyclic compound; tertiary amine | adrenergic uptake inhibitor; antidepressant; environmental contaminant; tropomyosin-related kinase B receptor agonist; xenobiotic |
| amlodipine Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.. amlodipine : A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina. | 2.05 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amobarbital Amobarbital: A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565). amobarbital : A member of the class of barbiturates that is pyrimidine-2,4,6(1H,3H,5H)-trione substituted by a 3-methylbutyl and an ethyl group at position 5. Amobarbital has been shown to exhibit sedative and hypnotic properties. | 2.05 | 1 | 0 | barbiturates | |
| amsacrine Amsacrine: An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.. amsacrine : A sulfonamide that is N-phenylmethanesulfonamide substituted by a methoxy group at position 3 and an acridin-9-ylamino group at position 4. It exhibits antineoplastic activity. | 2.05 | 1 | 0 | acridines; aromatic ether; sulfonamide | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| anastrozole [no description available] | 2.05 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| anethole trithione Anethole Trithione: Choleretic used to allay dry mouth and constipation due to tranquilizers. | 2.05 | 1 | 0 | methoxybenzenes | |
| anthralin Anthralin: An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.. anthralin : An anthracene compound derived by the substitution of -OH groups for hydrogen at C-1 and C-8, and with an oxo group at C-9. | 2.05 | 1 | 0 | anthracenes | antipsoriatic |
| 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 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] | 2.05 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| barbital 5,5-diethylbarbituric acid : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by two ethyl groups. Formerly used as a hypnotic (sleeping aid). | 2.05 | 1 | 0 | barbiturates | drug allergen |
| 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. | 2.05 | 1 | 0 | indazoles; monocarboxylic acid | non-steroidal anti-inflammatory drug; radical scavenger |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 2.05 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| 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. | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| bay h 4502 bifonazole : A racemate comprising equimolar amounts of R- and S-bifonazole. It is a broad spectrum antifungal drug used for the treatment of fungal skin and nail infections.. 1-[biphenyl-4-yl(phenyl)methyl]imidazole : A member of the class of imidazoles carrying an alpha-(biphenyl-4-yl)benzyl substituent at position 1. | 2.05 | 1 | 0 | biphenyls; imidazoles | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 2.05 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bromisovalum Bromisovalum: A sedative and mild hypnotic with potentially toxic effects.. bromisoval : A racemate comprising equimolar amounts of (R)- and (S)-bromisoval. It was previously used for its hypnotic and sedative properties but the use of bromides is now deprecated due to the possibility of the toxic accumulation of bromine in the body.. 2-bromo-N-carbamoyl-3-methylbutanamide : An N-acylurea that is urea in which one of the hydrogens is replaced by a 2-bromo-3-methybutanoyl group. | 2.05 | 1 | 0 | N-acylurea; organobromine compound | |
| brotizolam brotizolam: structure | 2.05 | 1 | 0 | organic molecular entity | |
| bumetanide [no description available] | 2.05 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| bupivacaine Bupivacaine: A widely used local anesthetic agent.. 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide : A piperidinecarboxamide obtained by formal condensation of the carboxy group of N-butylpipecolic acid with the amino group of 2,6-dimethylaniline.. bupivacaine : A racemate composed of equimolar amounts of dextrobupivacaine and levobupivacaine. Used (in the form of its hydrochloride hydrate) as a local anaesthetic. | 2.05 | 1 | 0 | aromatic amide; piperidinecarboxamide; tertiary amino compound | |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 2.05 | 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] | 2.05 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| butalbital butalbital: management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol; RN given refers to parent cpd. butalbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by an allyl group and an isobutyl group. Frequently combined with other medicines, such as aspirin, paracetamol and codeine, it is used for treatment of pain and headache. | 2.05 | 1 | 0 | barbiturates | analgesic; sedative |
| caffeine [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| candesartan cilexetil candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects | 2.05 | 1 | 0 | biphenyls | |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 2.05 | 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 |
| 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. | 2.05 | 1 | 0 | carbamate ester | muscle relaxant |
| carmustine Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group. | 2.05 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| carprofen carprofen: RN given refers to cpd without isomeric designation. carprofen : Propanoic acid in which one of the methylene hydrogens is substituted by a 6-chloro-9H-carbazol-2-yl group. A non-steroidal anti-inflammatory drug, it is no longer used in human medicine but is still used for treatment of arthritis in elderly dogs. | 2.05 | 1 | 0 | carbazoles; organochlorine compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug; photosensitizing agent |
| carvedilol [no description available] | 2.05 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | ether; monocarboxylic acid; monochlorobenzenes; piperazines | anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic |
| chloral hydrate [no description available] | 2.05 | 1 | 0 | aldehyde hydrate; ethanediol; organochlorine compound | general anaesthetic; mouse metabolite; sedative; xenobiotic |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 2.05 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chloroxylenol chloroxylenol: topical antiseptic; RN given refers to parent cpd; structure. 4-chloro-3,5-dimethylphenol : A member of the class of phenols that is 3,5-xylenol which is substituted at position 4 by chlorine. It is bactericidal against most Gram-positive bacteria but less effective against Staphylococci and Gram-negative bacteria, and often inactive against Pseudomonas species. It is ineffective against bacterial spores. | 2.05 | 1 | 0 | monochlorobenzenes; phenols | antiseptic drug; disinfectant; molluscicide |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 2.05 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antidepressant; antipruritic drug; H1-receptor antagonist; histamine antagonist; serotonin uptake inhibitor |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 2.05 | 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. | 2.05 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| 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. | 2.05 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 2.05 | 1 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cinoxacin Cinoxacin: Synthetic antimicrobial related to OXOLINIC ACID and NALIDIXIC ACID and used in URINARY TRACT INFECTIONS.. cinoxacin : A member of the class of cinnolines that is 6,7-methylenedioxycinnolin-4(1H)-one bearing an ethyl group at position 1 and a carboxylic acid group at position 3. An analogue of oxolinic acid, it has similar antibacterial actions. It was formerly used for the treatment of urinary tract infections. | 2.05 | 1 | 0 | cinnolines; oxacycle; oxo carboxylic acid | antibacterial drug; antiinfective agent |
| ciprofibrate [no description available] | 2.05 | 1 | 0 | cyclopropanes; monocarboxylic acid; organochlorine compound | antilipemic drug |
| ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | 2.05 | 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 |
| cisapride Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere. | 2.05 | 1 | 0 | benzamides | |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 2.05 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clioquinol Clioquinol: A potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide.. 5-chloro-7-iodoquinolin-8-ol : A monohydroxyquinoline that is quinolin-8-ol in which the hydrogens at positions 5 and 7 are replaced by chlorine and iodine, respectively. It has antibacterial and atifungal properties, and is used in creams for the treatment of skin infections. It has also been investigated as a chelator of copper and zinc ions for the possible treatment of Alzheimer's disease. | 2.05 | 1 | 0 | monohydroxyquinoline; organochlorine compound; organoiodine compound | antibacterial agent; antifungal agent; antimicrobial agent; antineoplastic agent; antiprotozoal drug; chelator; copper chelator |
| clobazam Clobazam: A benzodiazepine derivative that is a long-acting GABA-A RECEPTOR agonist. It is used as an antiepileptic in the treatment of SEIZURES, including seizures associated with LENNOX-GASTAUT SYNDROME. It is also used as an anxiolytic, for the short-term treatment of acute ANXIETY.. clobazam : 7-Chloro-1H-1,5-benzodiazepine-2,4(3H,5H)-dione in which the hydrogen attached to the nitrogen at position 1 is substituted by a methyl group, whilst that attached to the other nitrogen is substituted by a phenyl group. It is used for the short-term management of acute anxiety and as an adjunct in the treatment of epilepsy in association with other antiepileptics. | 2.05 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator |
| clofazimine Clofazimine: A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619). clofazimine : 3-Isopropylimino-3,5-dihydro-phenazine in which the hydrogen at position 5 is substituted substituted by a 4-chlorophenyl group, and that at position 2 is substituted by a (4-chlorophenyl)amino group. A dark red crystalline solid, clofazimine is an antimycobacterial and is one of the main drugs used for the treatment of multi-bacillary leprosy. However, it can cause red/brown discolouration of the skin, so other treatments are often preferred in light-skinned patients. | 2.05 | 1 | 0 | monochlorobenzenes; phenazines | dye; leprostatic drug; non-steroidal anti-inflammatory drug |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 2.05 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 2.05 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor 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. | 2.05 | 1 | 0 | clonidine; imidazoline | |
| clotiazepam clotiazepam: was heading 1975-94 (see under AZEPINES 1978-90; was Y 6047 see under AZEPINES 1975-77); Y 6047 was see CLOTIAZEPAM 1978-94; use AZEPINES to search CLOTIAZEPAM 1975-94; thienodiazepine derivative with actions similar to those of benzodiazepines | 2.05 | 1 | 0 | organic molecular entity | |
| clotrimazole [no description available] | 2.05 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cyclandelate Cyclandelate: A direct-acting SMOOTH MUSCLE relaxant used to dilate BLOOD VESSELS.. cyclandelate : The ester obtained by formal condensation of mandelic acid and 3,3,5-tricyclohexanol. It is a direct-acting smooth muscle relaxant used to dilate blood vessels. | 2.05 | 1 | 0 | carboxylic ester; secondary alcohol | vasodilator agent |
| 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. | 2.05 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| danthron danthron: structure. chrysazin : A dihydroxyanthraquinone that is anthracene-9,10-dione substituted by hydroxy groups at positions 1 and 8. | 2.05 | 1 | 0 | dihydroxyanthraquinone | apoptosis inducer; plant metabolite |
| dapsone [no description available] | 2.05 | 1 | 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. | 2.05 | 1 | 0 | acyclic desferrioxamine | bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 2.05 | 1 | 0 | primary amine | |
| eflornithine Eflornithine: An inhibitor of ORNITHINE DECARBOXYLASE, the rate limiting enzyme of the polyamine biosynthetic pathway.. eflornithine : A fluoroamino acid that is ornithine substituted by a difluoromethyl group at position 2. | 2.05 | 1 | 0 | alpha-amino acid; fluoroamino acid | trypanocidal drug |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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 |
| ddt 1,1-bis(p-chlorophenyl)-2,2,2-trichloroethane: structure in first source | 2.05 | 1 | 0 | benzenoid aromatic compound; chlorophenylethane; monochlorobenzenes; organochlorine insecticide | bridged diphenyl acaricide; carcinogenic agent; endocrine disruptor; persistent organic pollutant |
| diflunisal Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position. | 2.05 | 1 | 0 | monohydroxybenzoic acid; organofluorine compound | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 2.05 | 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. | 2.05 | 1 | 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 |
| doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. | 2.05 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| 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. | 2.05 | 1 | 0 | aromatic ketone; benzimidazoles; organofluorine compound | anaesthesia adjuvant; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| econazole Econazole: An imidazole derivative that is commonly used as a topical antifungal agent.. econazole : A racemate composed of equimolar amounts of (R)- and (S)-econazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections.. 1-{2-(4-chlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl}imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 4-chlorobenzyl group. | 2.05 | 1 | 0 | dichlorobenzene; ether; imidazoles; monochlorobenzenes | |
| enflurane Enflurane: An extremely stable inhalation anesthetic that allows rapid adjustments of anesthesia depth with little change in pulse or respiratory rate.. enflurane : An ether in which the oxygen atom is connected to 2-chloro-1,1,2-trifluoroethyl and difluoromethyl groups. | 2.05 | 1 | 0 | ether; organochlorine compound; organofluorine compound | anaesthetic |
| enoxacin Enoxacin: A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID.. enoxacin : A 1,8-naphthyridine derivative that is 1,4-dihydro-1,8-naphthyridine with an ethyl group at the 1 position, a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a piperazin-1-yl group at the 7 position. An antibacterial, it is used in the treatment of urinary-tract infections and gonorrhoea. | 2.05 | 1 | 0 | 1,8-naphthyridine derivative; amino acid; fluoroquinolone antibiotic; monocarboxylic acid; N-arylpiperazine; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor |
| estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. | 2.05 | 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. | 2.05 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethoxzolamide Ethoxzolamide: A carbonic anhydrase inhibitor used as diuretic and in glaucoma. It may cause hypokalemia.. ethoxzolamide : A sulfonamide that is 1,3-benzothiazole-2-sulfonamide which is substituted by an ethoxy group at position 6. A carbonic anhydrase inhibitor, it has been used in the treatment of glaucoma, and as a diuretic. | 2.05 | 1 | 0 | aromatic ether; benzothiazoles; sulfonamide | antiglaucoma drug; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| 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. | 2.05 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 2.05 | 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 | 2.05 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid. | 2.05 | 1 | 0 | anilide; monocarboxylic acid amide; piperidines | adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| flecainide Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| flufenamic acid Flufenamic Acid: An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16). flufenamic acid : An aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent. An analgesic and anti-inflammatory, it is used in rheumatic disorders. | 2.05 | 1 | 0 | aromatic amino acid; organofluorine compound | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 2.05 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| flunitrazepam Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug.. flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia. | 2.05 | 1 | 0 | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
| 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. | 2.05 | 1 | 0 | nucleobase analogue; organofluorine compound | antimetabolite; antineoplastic agent; environmental contaminant; immunosuppressive agent; radiosensitizing agent; xenobiotic |
| fluoxetine Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.. fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. | 2.05 | 1 | 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. | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide | androgen antagonist; antineoplastic agent |
| fomepizole Fomepizole: A pyrazole and competitive inhibitor of ALCOHOL DEHYDROGENASE that is used for the treatment of poisoning by ETHYLENE GLYCOL or METHANOL.. fomepizole : A member of the class of pyrazoles that is 1H-pyrazole substituted by a methyl group at position 4. | 2.05 | 1 | 0 | pyrazoles | antidote; EC 1.1.1.1 (alcohol dehydrogenase) inhibitor; protective agent |
| 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. | 2.05 | 1 | 0 | chlorobenzoic acid; furans; sulfonamide | environmental contaminant; loop diuretic; xenobiotic |
| gemfibrozil [no description available] | 2.05 | 1 | 0 | aromatic ether | antilipemic drug |
| glafenine Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market. | 2.05 | 1 | 0 | aminoquinoline; carboxylic ester; glycol; organochlorine compound; secondary amino compound | inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gliclazide Gliclazide: An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion. | 2.05 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; insulin secretagogue; radical scavenger |
| glutethimide Glutethimide: A hypnotic and sedative. Its use has been largely superseded by other drugs. | 2.05 | 1 | 0 | piperidines | |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 2.05 | 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 |
| gossypol Gossypol: A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer. | 2.05 | 1 | 0 | ||
| guaiazulene guaiazulene: structure | 2.05 | 1 | 0 | sesquiterpene | |
| fasudil fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia. | 2.05 | 1 | 0 | isoquinolines; N-sulfonyldiazepane | antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 2.05 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| halothane [no description available] | 2.05 | 1 | 0 | haloalkane; organobromine compound; organochlorine compound; organofluorine compound | inhalation anaesthetic |
| hexachlorophene Hexachlorophene: A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797). hexachlorophene : An organochlorine compound that is diphenylmethane in which each of the phenyl groups is substituted by chlorines at positions 2, 3, and 5, and by a hydroxy group at position 6. An antiseptic that is effective against Gram-positive organisms, it is used in soaps and creams for the treatment of various skin disorders. It is also used in agriculture as an acaricide and fungicide, but is not approved for such use within the European Union. | 2.05 | 1 | 0 | bridged diphenyl fungicide; polyphenol; trichlorobenzene | acaricide; antibacterial agent; antifungal agrochemical; antiseptic drug |
| miltefosine miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine. | 2.05 | 1 | 0 | phosphocholines; phospholipid | anti-inflammatory agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antiprotozoal drug; apoptosis inducer; immunomodulator; protein kinase inhibitor |
| hexestrol [no description available] | 2.05 | 1 | 0 | stilbenoid | |
| hexetidine Hexetidine: A bactericidal and fungicidal antiseptic. It is used as a 0.1% mouthwash for local infections and oral hygiene. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797) | 2.05 | 1 | 0 | organic heteromonocyclic compound; organonitrogen heterocyclic compound | |
| hexobarbital Hexobarbital: A barbiturate that is effective as a hypnotic and sedative.. hexobarbital : A member of the class of barbiturates taht is barbituric acid substituted at N-1 by methyl and at C-5 by methyl and cyclohex-1-enyl groups. | 2.05 | 1 | 0 | barbiturates | |
| hydralazine Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent. | 2.05 | 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. | 2.05 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroxyurea [no description available] | 2.05 | 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. | 2.05 | 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 | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| alverine alverine : A tertiary amine having one ethyl and two 3-phenylprop-1-yl groups attached to the nitrogen. An antispasmodic that acts directly on intestinal and uterine smooth muscle, it is used (particularly as the citrate salt) in the treatment of irritable bowel syndrome. | 2.05 | 1 | 0 | tertiary amine | antispasmodic drug |
| idebenone [no description available] | 2.05 | 1 | 0 | 1,4-benzoquinones; primary alcohol | antioxidant; ferroptosis inhibitor |
| ifosfamide [no description available] | 2.05 | 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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 |
| iohexol Iohexol: An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality.. iohexol : A benzenedicarboxamide compound having N-(2,3-dihydroxypropyl)carbamoyl groups at the 1- and 3-positions, iodo substituents at the 2-, 4- and 6-positions and an N-(2,3-dihydroxypropyl)acetamido group at the 5-position. | 2.05 | 1 | 0 | benzenedicarboxamide; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| iodipamide Iodipamide: A water-soluble radiographic contrast media for cholecystography and intravenous cholangiography.. adipiodone : An organoiodine compound that is 3-amino-2,4,6-triiodobenzoic acid in which one of the amino hydrogens is substituted by a 6-(3-carboxy-2,4,6-triiodoanilino)-6-oxohexanoyl group. It is a water-soluble radiographic contrast media for cholecystography and intravenous cholangiography. | 2.05 | 1 | 0 | benzoic acids; organoiodine compound; secondary carboxamide | radioopaque medium |
| iproniazid [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| isoflurane Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects. | 2.05 | 1 | 0 | organofluorine compound | inhalation anaesthetic |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 2.05 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| 2-propanol 2-Propanol: An isomer of 1-PROPANOL. It is a colorless liquid having disinfectant properties. It is used in the manufacture of acetone and its derivatives and as a solvent. Topically, it is used as an antiseptic.. propan-2-ol : A secondary alcohol that is propane in which one of the hydrogens attached to the central carbon is substituted by a hydroxy group. | 2.05 | 1 | 0 | secondary alcohol; secondary fatty alcohol | protic solvent |
| isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders. | 2.05 | 1 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| isoxsuprine Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | 2.05 | 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. | 2.05 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| ketanserin Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.. ketanserin : A member of the class of quinazolines that is quinazoline-2,4(1H,3H)-dione which is substituted at position 3 by a 2-[4-(p-fluorobenzoyl)piperidin-1-yl]ethyl group. | 2.05 | 1 | 0 | aromatic ketone; organofluorine compound; piperidines; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; cardiovascular drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; serotonergic antagonist |
| ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. | 2.05 | 1 | 0 | dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine | |
| ketoprofen Ketoprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis.. ketoprofen : An oxo monocarboxylic acid that consists of propionic acid substituted by a 3-benzoylphenyl group at position 2. | 2.05 | 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 |
| khellin Khellin: A vasodilator that also has bronchodilatory action. It has been employed in the treatment of angina pectoris, in the treatment of asthma, and in conjunction with ultraviolet light A, has been tried in the treatment of vitiligo. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1024). khellin : A furanochrome in which the basic tricyclic skeleton is substituted at positions 4 and 9 with methoxy groups and at position 7 with a methyl group. A major constituent of the plant Ammi visnaga it is a herbal folk medicine used for various illnesses, its main effect being as a vasodilator. | 2.05 | 1 | 0 | furanochromone; organic heterotricyclic compound; oxacycle | anti-asthmatic agent; bronchodilator agent; cardiovascular drug; vasodilator agent |
| labetalol Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5. | 2.05 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 2.05 | 1 | 0 | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic |
| lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. | 2.05 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| beta-lapachone beta-lapachone: antineoplastic inhibitor of reverse transcriptase, DNA topoisomerase, and DNA polymerase. beta-lapachone : A benzochromenone that is 3,4-dihydro-2H-benzo[h]chromene-5,6-dione substituted by geminal methyl groups at position 2. Isolated from Tabebuia avellanedae, it exhibits antineoplastic and anti-inflammatory activities. | 2.05 | 1 | 0 | benzochromenone; orthoquinones | anti-inflammatory agent; antineoplastic agent; plant metabolite |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 2.05 | 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 |
| lofepramine Lofepramine: A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE. | 2.05 | 1 | 0 | aromatic ketone; dibenzoazepine; monochlorobenzenes; tertiary amino compound | antidepressant |
| lomustine [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | 2.05 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| malathion Malathion: A wide spectrum aliphatic organophosphate insecticide widely used for both domestic and commercial agricultural purposes.. malathion : A racemate comprising equimolar amounts of (R) and (S)-malathion. It is a broad spectrum organophosphate proinsecticide used to control a wide range of pests including Coleoptera, Diptera, fruit flies, mosquitos and spider mites.. diethyl 2-[(dimethoxyphosphorothioyl)thio]succinate : A diester that is diethyl succinate in which position 2 is substituted by a (dimethoxyphosphorothioyl)thio group. | 2.05 | 1 | 0 | diester; ethyl ester; organic thiophosphate | |
| diisopropyl 1,3-dithiol-2-ylidenemalonate diisopropyl 1,3-dithiol-2-ylidenemalonate: structure in first source | 2.05 | 1 | 0 | isopropyl ester | |
| mazindol Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. | 2.05 | 1 | 0 | organic molecular entity | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 2.05 | 1 | 0 | aromatic ketone; benzimidazoles; carbamate ester | antinematodal drug; microtubule-destabilising agent; tubulin modulator |
| meclizine Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. | 2.05 | 1 | 0 | diarylmethane | |
| meclofenoxate Meclofenoxate: An ester of DIMETHYLAMINOETHANOL and para-chlorophenoxyacetic acid. | 2.05 | 1 | 0 | monocarboxylic acid | |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 2.05 | 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 |
| vitamin k 3 Vitamin K 3: A synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo. | 2.05 | 1 | 0 | 1,4-naphthoquinones; vitamin K | angiogenesis inhibitor; antineoplastic agent; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; human urinary metabolite; nutraceutical |
| meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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) | 2.05 | 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. | 2.05 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 2.05 | 1 | 0 | guanidines | environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic |
| methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4. | 2.05 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| 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. | 2.05 | 1 | 0 | aromatic ether; psoralens | antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite |
| methoxyflurane Methoxyflurane: An inhalation anesthetic. Currently, methoxyflurane is rarely used for surgical, obstetric, or dental anesthesia. If so employed, it should be administered with NITROUS OXIDE to achieve a relatively light level of anesthesia, and a neuromuscular blocking agent given concurrently to obtain the desired degree of muscular relaxation. (From AMA Drug Evaluations Annual, 1994, p180). methoxyflurane : An ether in which the two groups attached to the central oxygen atom are methyl and 2,2-dichloro-1,1-difluoroethyl. | 2.05 | 1 | 0 | ether; organochlorine compound; organofluorine compound | hepatotoxic agent; inhalation anaesthetic; nephrotoxic agent; non-narcotic analgesic |
| methyl salicylate methyl salicylate: used in over-the-counter liniments, ointments, lotions for relief of musculoskeletal aches and pains; has hemolytic effect on human & sheep erythrocytes; RN given refers to parent cpd; structure in Merck Index, 9th ed, #5990. methyl salicylate : A benzoate ester that is the methyl ester of salicylic acid. | 2.05 | 1 | 0 | benzoate ester; methyl ester; salicylates | flavouring agent; insect attractant; metabolite |
| methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group. | 2.05 | 1 | 0 | beta-amino acid ester; methyl ester; piperidines | |
| methyprylon methyprylon: was heading 1973-94 (see under HYPNOTICS AND SEDATIVES 1963-72); use PIPERIDONES to search METHYPRYLON 1973-94 | 2.05 | 1 | 0 | organic molecular entity | |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 2.05 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 2.05 | 1 | 0 | aromatic ether; propanolamine; secondary alcohol; secondary amino compound | antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic |
| metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death. | 2.05 | 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. | 2.05 | 1 | 0 | aromatic ketone | antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor |
| mianserin Mianserin: A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.. mianserin : A dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere. | 2.05 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; H1-receptor antagonist; histamine agonist; sedative; serotonergic antagonist |
| miconazole Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion.. 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group.. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes. | 2.05 | 1 | 0 | dichlorobenzene; ether; imidazoles | |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 2.05 | 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 |
| minoxidil Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | 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. | 2.05 | 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) | 2.05 | 1 | 0 | monoterpenoid | |
| deet N,N-diethyl-m-toluamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of m-toluic acid with the nitrogen of diethylamine. First developed by the U.S. Army in 1946 for use by military personnel in insect-infested areas, it is the most widely used insect repellent worldwide. | 2.05 | 1 | 0 | benzamides; monocarboxylic acid amide | environmental contaminant; insect repellent; xenobiotic |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 2.05 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nalidixic acid [no description available] | 2.05 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| nefazodone nefazodone: may be useful as an opiate adjunct | 2.05 | 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. | 2.05 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 2.05 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| niceritrol Niceritrol: An ester of nicotinic acid that lowers cholesterol and triglycerides in total plasma and in the VLD- and LD-lipoprotein fractions. | 2.05 | 1 | 0 | organic molecular entity | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 2.05 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| niflumic acid Niflumic Acid: An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis. | 2.05 | 1 | 0 | aromatic carboxylic acid; pyridines | |
| nilutamide [no description available] | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 2.05 | 1 | 0 | aromatic ether; C-nitro compound; sulfonamide | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| nimodipine Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. | 2.05 | 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. | 2.05 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitrazepam Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic.. nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome). | 2.05 | 1 | 0 | 1,4-benzodiazepinone; C-nitro compound | anticonvulsant; antispasmodic drug; drug metabolite; GABA modulator; sedative |
| nitrendipine Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.. nitrendipine : A dihydropyridine that is 1,4-dihydropyridine substituted by methyl groups at positions 2 and 6, a 3-nitrophenyl group at position 4, a ethoxycarbonyl group at position 3 and a methoxycarbonyl group at position 5. It is a calcium-channel blocker used in the treatment of hypertension. | 2.05 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; ethyl ester; methyl ester | antihypertensive agent; calcium channel blocker; geroprotector; vasodilator agent |
| nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain. | 2.05 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 2.05 | 1 | 0 | 1,3-thiazoles; C-nitro compound; carboxamidine; organic sulfide; tertiary amino compound | anti-ulcer drug; cholinergic drug; H2-receptor antagonist |
| masoprocol nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata) | 2.05 | 1 | 0 | catechols; lignan; tetrol | antioxidant; ferroptosis inhibitor; geroprotector; plant metabolite |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 2.05 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug; DNA synthesis inhibitor; environmental contaminant; xenobiotic |
| nortriptyline Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline. | 2.05 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxamniquine Oxamniquine: An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martindale, The Extra Pharmacopoeia, 31st ed, p121). oxamniquine : A racemate comprising equimolar amounts of (R)- and (S)-oxamniquine. An anthelmintic, it is administered orally for the treatment of schistomiasis caused by Schistosoma mansoni (but not by other Schistosoma species); intramuscular administration is no longer used as it causes severe pain at the injection site.. {2-[(isopropylamino)methyl]-7-nitro-1,2,3,4-tetrahydroquinolin-6-yl}methanol : A member of the class of quinolines that is 1,2,3,4-tetrahydroquinoline which is substituted at positions 2, 6, and 7 by (isopropylamino)methyl, hydroxymethyl, and nitro groups, respectively. | 2.05 | 1 | 0 | aromatic primary alcohol; C-nitro compound; quinolines; secondary amino compound | |
| 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. | 2.05 | 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. | 2.05 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxethazaine [no description available] | 2.05 | 1 | 0 | amino acid amide | |
| oxprenolol Oxprenolol: A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. | 2.05 | 1 | 0 | aromatic ether | |
| oxybenzone oxybenzone : A hydroxybenzophenone that is benzophenone which is substituted at the 2- and 4-positions of one of the benzene rings by hydroxy and methoxy groups respectively. | 2.05 | 1 | 0 | hydroxybenzophenone; monomethoxybenzene | dermatologic drug; environmental contaminant; protective agent; ultraviolet filter; xenobiotic |
| oxyphenbutazone Oxyphenbutazone: A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27). oxyphenbutazone : A metabolite of phenylbutazone obtained by hydroxylation at position 4 of one of the phenyl rings. Commonly used (as its hydrate) to treat pain, swelling and stiffness associated with arthritis and gout, it was withdrawn from the market 1984 following association with blood dyscrasis and Stevens-Johnson syndrome. | 2.05 | 1 | 0 | phenols; pyrazolidines | antimicrobial agent; antineoplastic agent; antipyretic; drug metabolite; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic metabolite |
| aminosalicylic acid Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4. | 2.05 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pantoprazole Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2. | 2.05 | 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 |
| 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. | 2.05 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 2.05 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 2.05 | 1 | 0 | oxopurine | |
| perazine Perazine: A phenothiazine antipsychotic with actions and uses similar to those of CHLORPROMAZINE. Extrapyramidal symptoms may be more common than other side effects.. perazine : A phenothiazine derivative in which 10H-phenothiazinecarries a 3-(4-methylpiperazin-1-yl)propyl substituent at the N-10 position. | 2.05 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; phenothiazines | dopaminergic antagonist; phenothiazine antipsychotic drug |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 2.05 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenacetin Saridon: contains phenacetin, caffeine, propyphenazone & pyrithyldione | 2.05 | 1 | 0 | acetamides; aromatic ether | cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 2.05 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenolphthalein Phenolphthalein: An acid-base indicator which is colorless in acid solution, but turns pink to red as the solution becomes alkaline. It is used medicinally as a cathartic. | 2.05 | 1 | 0 | phenols | |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 2.05 | 1 | 0 | aromatic amine | |
| phenylbutazone Phenylbutazone: A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS.. phenylbutazone : A member of the class of pyrazolidines that is 1,2-diphenylpyrazolidine-3,5-dione carrying a butyl group at the 4-position. | 2.05 | 1 | 0 | pyrazolidines | antirheumatic drug; EC 1.1.1.184 [carbonyl reductase (NADPH)] inhibitor; metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug |
| moxonidine moxonidine: structure given in first source | 2.05 | 1 | 0 | organohalogen compound; pyrimidines | |
| pinacidil Pinacidil: A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed) | 2.05 | 1 | 0 | pyridines | |
| pipemidic acid Pipemidic Acid: Antimicrobial against Gram negative and some Gram positive bacteria. It is protein bound and concentrated in bile and urine and used for gastrointestinal, biliary, and urinary infections.. pipemidic acid : A pyridopyrimidine that is 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid substituted at position 2 by a piperazin-1-yl group and at position 8 by an ethyl group. A synthetic broad-spectrum antibacterial, it is used for treatment of gastrointestinal, biliary, and urinary infections. | 2.05 | 1 | 0 | amino acid; monocarboxylic acid; N-arylpiperazine; pyridopyrimidine; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor |
| piperazine [no description available] | 2.05 | 1 | 0 | azacycloalkane; piperazines; saturated organic heteromonocyclic parent | anthelminthic drug |
| praziquantel azinox: Russian drug | 2.05 | 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. | 2.05 | 1 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | pyrimidone | anticonvulsant; environmental contaminant; xenobiotic |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 2.05 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| probucol Probucol: A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993).. probucol : A dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood. | 2.05 | 1 | 0 | dithioketal; polyphenol | anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 2.05 | 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. | 2.05 | 1 | 0 | benzamides; hydrazines | antineoplastic agent |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 2.05 | 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 |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 2.05 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. | 2.05 | 1 | 0 | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 2.05 | 1 | 0 | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| pyridinolcarbamate Pyridinolcarbamate: A drug that has been given by mouth in the treatment of atherosclerosis and other vascular disorders, hyperlipidemias, and thrombo-embolic disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1408) | 2.05 | 1 | 0 | pyridines | |
| pyrimethamine Maloprim: contains above 2 cpds | 2.05 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| ranitidine [no description available] | 2.05 | 1 | 0 | aralkylamine | |
| opc 12759 rebamipide: structure in first source; RN refers to (+-)-isomer; inhibits gastric xanthine oxidase | 2.05 | 1 | 0 | secondary carboxamide | |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 2.05 | 1 | 0 | benzothiazoles | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 2.05 | 1 | 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 |
| rofecoxib [no description available] | 2.05 | 1 | 0 | butenolide; sulfone | analgesic; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| salicylamide salamide: a major impurity of hydrochlorothiazide; structure in first source | 2.05 | 1 | 0 | phenols; salicylamides | antirheumatic drug; non-narcotic analgesic |
| sevoflurane Sevoflurane: A non-explosive inhalation anesthetic used in the induction and maintenance of general anesthesia. It does not cause respiratory irritation and may also prevent PLATELET AGGREGATION.. sevoflurane : An ether compound having fluoromethyl and 1,1,1,3,3,3-hexafluoroisopropyl as the two alkyl groups. | 2.05 | 1 | 0 | ether; organofluorine compound | central nervous system depressant; inhalation anaesthetic; platelet aggregation inhibitor |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 2.05 | 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. | 2.05 | 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 |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 2.05 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| 4-phenylbutyric acid, sodium salt sodium phenylbutyrate : The organic sodium salt of 4-phenylbutyric acid. A prodrug for phenylacetate, it is used to treat urea cycle disorders. | 2.05 | 1 | 0 | organic sodium salt | EC 3.5.1.98 (histone deacetylase) inhibitor; geroprotector; neuroprotective agent; orphan drug; prodrug |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 2.05 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| sulfadimethoxine Sulfadimethoxine: A sulfanilamide that is used as an anti-infective agent.. sulfadimethoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 2- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. | 2.05 | 1 | 0 | aromatic ether; pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; drug allergen; environmental contaminant; xenobiotic |
| sulfamerazine [no description available] | 2.05 | 1 | 0 | pyrimidines; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen |
| sulfameter Sulfameter: Long acting sulfonamide used in leprosy, urinary, and respiratory tract infections.. sulfamethoxydiazine : A sulfonamide consisting of pyrimidine having a methoxy substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 2-position. | 2.05 | 1 | 0 | pyrimidines; sulfonamide antibiotic; sulfonamide | antiinfective agent; leprostatic drug; renal agent |
| sulfamethazine Sulfamethazine: A sulfanilamide anti-infective agent. It has a spectrum of antimicrobial action similar to other sulfonamides.. sulfamethazine : A sulfonamide consisting of pyrimidine with methyl substituents at the 4- and 6-positions and a 4-aminobenzenesulfonamido group at the 2-position. | 2.05 | 1 | 0 | pyrimidines; sulfonamide antibiotic; sulfonamide | antibacterial drug; antiinfective agent; antimicrobial agent; carcinogenic agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; ligand; xenobiotic |
| 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. | 2.05 | 1 | 0 | sulfonamide antibiotic; sulfonamide; thiadiazoles | antiinfective agent; antimicrobial agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfamethoxazole Sulfamethoxazole: A bacteriostatic antibacterial agent that interferes with folic acid synthesis in susceptible bacteria. Its broad spectrum of activity has been limited by the development of resistance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p208). sulfamethoxazole : An isoxazole (1,2-oxazole) compound having a methyl substituent at the 5-position and a 4-aminobenzenesulfonamido group at the 3-position. | 2.05 | 1 | 0 | isoxazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial agent; antiinfective agent; antimicrobial agent; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; epitope; P450 inhibitor; xenobiotic |
| sulfanilamide [no description available] | 2.05 | 1 | 0 | substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial agent; drug allergen; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| sulfaphenazole Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent. | 2.05 | 1 | 0 | primary amino compound; pyrazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antibacterial drug; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor; P450 inhibitor |
| sulfapyridine Sulfapyridine: Antibacterial, potentially toxic, used to treat certain skin diseases.. sulfapyridine : A sulfonamide consisting of pyridine with a 4-aminobenzenesulfonamido group at the 2-position. | 2.05 | 1 | 0 | pyridines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; dermatologic drug; drug allergen; environmental contaminant; xenobiotic |
| sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. | 2.05 | 1 | 0 | ||
| sulfinpyrazone Sulfinpyrazone: A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. | 2.05 | 1 | 0 | pyrazolidines; sulfoxide | uricosuric drug |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | benzamides; N-alkylpyrrolidine; sulfonamide | antidepressant; antiemetic; antipsychotic agent; dopaminergic antagonist |
| suprofen Suprofen: An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.. suprofen : An aromatic ketone that is thiophene substituted at C-2 by a 4-(1-carboxyethyl)benzoyl group. | 2.05 | 1 | 0 | aromatic ketone; monocarboxylic acid; thiophenes | antirheumatic drug; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; peripheral nervous system drug |
| suramin Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.. suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. | 2.05 | 1 | 0 | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
| gatifloxacin Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes. | 2.05 | 1 | 0 | N-arylpiperazine; organofluorine compound; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antiinfective agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| tegafur [no description available] | 2.05 | 1 | 0 | organohalogen compound; pyrimidines | |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 2.05 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 2.05 | 1 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 2.05 | 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 |
| terfenadine Terfenadine: A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. | 2.05 | 1 | 0 | diarylmethane | |
| tetracaine Tetracaine: A potent local anesthetic of the ester type used for surface and spinal anesthesia.. tetracaine : A benzoate ester in which 4-N-butylbenzoic acid and 2-(dimethylamino)ethanol have combined to form the ester bond; a local ester anaesthetic (ester caine) used for surface and spinal anaesthesia. | 2.05 | 1 | 0 | benzoate ester; tertiary amino compound | local anaesthetic |
| thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group. | 2.05 | 1 | 0 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 2.05 | 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. | 2.05 | 1 | 0 | phenothiazines; piperidines | alpha-adrenergic antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| tiaprofenic acid tiaprofenic acid: RN given refers to parent cpd; structure. tiaprofenic acid : An aromatic ketone that is thiophene substituted at C-2 by benzoyl and at C-4 by a 1-carboxyethyl group. | 2.05 | 1 | 0 | aromatic ketone; monocarboxylic acid; thiophenes | drug allergen; non-steroidal anti-inflammatory drug |
| ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group. | 2.05 | 1 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 2.05 | 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. | 2.05 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| tolazamide Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus. | 2.05 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; potassium channel blocker |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 2.05 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolperisone Tolperisone: A centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1211) | 2.05 | 1 | 0 | aromatic ketone | |
| ultram 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively. | 2.05 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 2.05 | 1 | 0 | amino acid | |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 2.05 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triclosan [no description available] | 2.05 | 1 | 0 | aromatic ether; dichlorobenzene; monochlorobenzenes; phenols | antibacterial agent; antimalarial; drug allergen; EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; fungicide; persistent organic pollutant; xenobiotic |
| triflupromazine Triflupromazine: A phenothiazine used as an antipsychotic agent and as an antiemetic.. triflupromazine : A member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(dimethylamino)propyl group at the N-10 position. | 2.05 | 1 | 0 | organofluorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| trimethadione Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent. | 2.05 | 1 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 2.05 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 2.05 | 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 |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 2.05 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vesnarinone [no description available] | 2.05 | 1 | 0 | organic molecular entity | |
| vigabatrin [no description available] | 2.05 | 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 | 2.05 | 1 | 0 | carbamate ester; indoles; N-sulfonylcarboxamide | anti-asthmatic agent; leukotriene antagonist |
| zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position. | 2.05 | 1 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| guanidine hydrochloride [no description available] | 2.05 | 1 | 0 | one-carbon compound; organic chloride salt | protein denaturant |
| hydrocortisone acetate hydrocortisone acetate: RN given refers to cpd without isomeric designation | 2.05 | 1 | 0 | cortisol ester; tertiary alpha-hydroxy ketone | |
| 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. | 2.05 | 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. | 2.05 | 1 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 2.05 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic |
| estriol hormonin: estrogen replacement; each tablet contains 600 ug micronized 17beta-estradiol, 270 ug estriol and 1.4 mg estrone. chlorapatite : A phosphate mineral with the formula Ca5(PO4)3Cl. | 2.05 | 1 | 0 | 16alpha-hydroxy steroid; 17beta-hydroxy steroid; 3-hydroxy steroid | estrogen; human metabolite; human xenobiotic metabolite; mouse metabolite |
| reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. | 2.05 | 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 |
| cephaloridine Cephaloridine: A cephalosporin antibiotic.. cefaloridine : A cephalosporin compound having pyridinium-1-ylmethyl and 2-thienylacetamido side-groups. A first-generation semisynthetic derivative of cephalosporin C. | 2.05 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| 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. | 2.05 | 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). | 2.05 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| floxuridine Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.. floxuridine : A pyrimidine 2'-deoxyribonucleoside compound having 5-fluorouracil as the nucleobase; used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. | 2.05 | 1 | 0 | nucleoside analogue; organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; radiosensitizing agent |
| piperonyl butoxide [no description available] | 2.05 | 1 | 0 | benzodioxoles | pesticide synergist |
| bromouracil Bromouracil: 5-Bromo-2,4(1H,3H)-pyrimidinedione. Brominated derivative of uracil that acts as an antimetabolite, substituting for thymine in DNA. It is used mainly as an experimental mutagen, but its deoxyriboside (BROMODEOXYURIDINE) is used to treat neoplasms.. 5-bromouracil : A pyrimidine having keto groups at the 2- and 4-positions and a bromo group at the 5-position. Used mainly as an experimental mutagen. | 2.05 | 1 | 0 | nucleobase analogue; pyrimidines | mutagen |
| 3,3',5-triiodothyroacetic acid tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome. | 2.05 | 1 | 0 | ||
| histamine dihydrochloride Ceplene: Tradename for histamine dihydrochloride. | 2.05 | 1 | 0 | ||
| thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. | 2.05 | 1 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. | 2.05 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS. | 2.05 | 1 | 0 | ammonium salt; carbamate ester | cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic |
| 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. | 2.05 | 1 | 0 | 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. | 2.05 | 1 | 0 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| cyclobarbital cyclobarbital: was heading 1977-94 (see under BARBITURATES 1977-90); CYCLOBARBITONE, HEXEMAL, & TETRAHYDROPHENOBARBITAL were see CYCLOBARBITAL 1977-94; use BARBITURATES to search CYCLOBARBITAL 1977-94; short to intermediate duration barbiturate used as hypnotic and sedative | 2.05 | 1 | 0 | barbiturates | |
| allobarbital allobarbital: was heading 1976-94 (see under BARBITURATES 1976-90); ALLOBARBITONE, DIALLYLBARBITAL, DIALLYLBARBITURIC ACID, & DIALLYLMAL were see ALLOBARBITAL 1976-94; use BARBITURATES to search ALLOBARBITAL 1976-94; a barbiturate derivative with effects of intermediate duration; at lower doses, it is used as a sedative; at higher doses, it displays hypnotic effects | 2.05 | 1 | 0 | barbiturates | |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 2.05 | 1 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| trichlorfon Trichlorfon: An organochlorophosphate cholinesterase inhibitor that is used as an insecticide for the control of flies and roaches. It is also used in anthelmintic compositions for animals. (From Merck, 11th ed). trichlorfon : A phosphonic ester that is dimethyl phosphonate in which the hydrogen atom attched to the phosphorous is substituted by a 2,2,2-trichloro-1-hydroxyethyl group. | 2.05 | 1 | 0 | organic phosphonate; organochlorine compound; phosphonic ester | agrochemical; anthelminthic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; insecticide |
| 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. | 2.05 | 1 | 0 | 11-oxo steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antineoplastic agent; immunosuppressive agent; prodrug |
| estrone Hydroxyestrones: Estrone derivatives substituted with one or more hydroxyl groups in any position. They are important metabolites of estrone and other estrogens. | 2.05 | 1 | 0 | 17-oxo steroid; 3-hydroxy steroid; phenolic steroid; phenols | antineoplastic agent; bone density conservation agent; estrogen; human metabolite; mouse metabolite |
| oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| dehydroepiandrosterone Dehydroepiandrosterone: A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.. dehydroepiandrosterone : An androstanoid that is androst-5-ene substituted by a beta-hydroxy group at position 3 and an oxo group at position 17. It is a naturally occurring steroid hormone produced by the adrenal glands. | 2.05 | 1 | 0 | 17-oxo steroid; 3beta-hydroxy-Delta(5)-steroid; androstanoid | androgen; human metabolite; mouse metabolite |
| nad [no description available] | 2.05 | 1 | 0 | NAD | geroprotector |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 2.05 | 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. | 2.05 | 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 |
| cetrimonium bromide cetyltrimethylammonium bromide : The organic bromide salt that is the bromide salt of cetyltrimethylammonium; one of the components of the topical antiseptic cetrimide. | 2.05 | 1 | 0 | organic bromide salt; quaternary ammonium salt | detergent; surfactant |
| vincristine [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar. | 2.05 | 1 | 0 | glycosyl glycoside | algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent |
| ethinyl estradiol Ethinyl Estradiol: A semisynthetic alkylated ESTRADIOL with a 17-alpha-ethinyl substitution. It has high estrogenic potency when administered orally, and is often used as the estrogenic component in ORAL CONTRACEPTIVES.. 17alpha-ethynylestradiol : A 3-hydroxy steroid that is estradiol substituted by a ethynyl group at position 17. It is a xenoestrogen synthesized from estradiol and has been shown to exhibit high estrogenic potency on oral administration. | 2.05 | 1 | 0 | 17-hydroxy steroid; 3-hydroxy steroid; terminal acetylenic compound | xenoestrogen |
| testosterone propionate Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors. | 2.05 | 1 | 0 | steroid ester | |
| apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. | 2.05 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| aminopyrine Aminopyrine: A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS.. aminophenazone : A pyrazolone that is 1,2-dihydro-3H-pyrazol-3-one substituted by a dimethylamino group at position 4, methyl groups at positions 1 and 5 and a phenyl group at position 2. It exhibits analgesic, anti-inflammatory, and antipyretic properties. | 2.05 | 1 | 0 | pyrazolone; tertiary amino compound | antipyretic; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| 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. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; enone | anabolic agent; androgen; antineoplastic agent |
| tetrabenazine 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. | 2.05 | 1 | 0 | benzoquinolizine; cyclic ketone; tertiary amino compound | |
| cephalothin Cephalothin: A cephalosporin antibiotic.. cefalotin : A semisynthetic, first-generation cephalosporin antibiotic with acetoxymethyl and (2-thienylacetyl)nitrilo moieties at positions 3 and 7, respectively, of the core structure. Administered parenterally during surgery and to treat a wide spectrum of blood infections. | 2.05 | 1 | 0 | azabicycloalkene; beta-lactam antibiotic allergen; carboxylic acid; cephalosporin; semisynthetic derivative; thiophenes | antibacterial drug; antimicrobial agent |
| uridine [no description available] | 2.05 | 1 | 0 | uridines | drug metabolite; fundamental metabolite; human metabolite |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 2.05 | 1 | 0 | kanamycins | bacterial metabolite |
| phenylephrine Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring. | 2.05 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | alpha-adrenergic agonist; cardiotonic drug; mydriatic agent; nasal decongestant; protective agent; sympathomimetic agent; vasoconstrictor agent |
| levodopa Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease | 2.05 | 1 | 0 | amino acid zwitterion; dopa; L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | allelochemical; antidyskinesia agent; antiparkinson drug; dopaminergic agent; hapten; human metabolite; mouse metabolite; neurotoxin; plant growth retardant; plant metabolite; prodrug |
| niridazole Niridazole: An antischistosomal agent that has become obsolete. | 2.05 | 1 | 0 | 1,3-thiazoles; C-nitro compound | |
| carbaryl Carbaryl: A carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries.. carbaryl : A carbamate ester obtained by the formal condensation of 1-naphthol with methylcarbamic acid. | 2.05 | 1 | 0 | carbamate ester; naphthalenes | acaricide; agrochemical; carbamate insecticide; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant growth retardant |
| lactose Lactose: A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry.. lactose : A glycosylglucose disaccharide, found most notably in milk, that consists of D-galactose and D-glucose fragments bonded through a beta-1->4 glycosidic linkage. The glucose fragment can be in either the alpha- or beta-pyranose form, whereas the galactose fragment can only have the beta-pyranose form.. beta-lactose : The beta-anomer of lactose. | 2.05 | 1 | 0 | lactose | |
| methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4. | 2.05 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid | antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical |
| Mebutamate [no description available] | 2.05 | 1 | 0 | organic molecular entity | |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 2.05 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| norethindrone Norethindrone: A synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for CONTRACEPTION.. norethisterone : A 17beta-hydroxy steroid that is testosterone in which the hydrogen at position 17 is replaced by an ethynyl group and in which the methyl group attached to position 10 is replaced by hydrogen. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound; tertiary alcohol | progestin; synthetic oral contraceptive |
| norethynodrel Norethynodrel: A synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and ENDOMETRIOSIS. As a contraceptive (CONTRACEPTIVE AGENTS), it has usually been administered in combination with MESTRANOL. | 2.05 | 1 | 0 | oxo steroid | |
| benziodarone benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) | 2.05 | 1 | 0 | aromatic ketone | |
| ampicillin Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group. | 2.05 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 2.05 | 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] | 2.05 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| medroxyprogesterone acetate [no description available] | 2.05 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester | adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive |
| mestranol [no description available] | 2.05 | 1 | 0 | 17beta-hydroxy steroid; aromatic ether; terminal acetylenic compound | prodrug; xenoestrogen |
| methaqualone Methaqualone: A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604). methaqualone : A member of the class of quinazolines that is quinazolin-4-one substituted at positions 2 and 3 by methyl and o-tolyl groups respectively. A depressant that increases the activity of the GABA receptors in the brain and nervous system, it is used as a sedative and hypnotic medication. It became popular as a recreational drug and club drug in the late 1960s and 1970s. | 2.05 | 1 | 0 | quinazolines | GABA agonist; sedative |
| trypan blue VisionBlue: A trypan blue ophthalmic solution. | 2.05 | 1 | 0 | ||
| cordycepin [no description available] | 2.05 | 1 | 0 | 3'-deoxyribonucleoside; adenosines | antimetabolite; nucleoside antibiotic |
| tryptophan Tryptophan: An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals.. tryptophan : An alpha-amino acid that is alanine bearing an indol-3-yl substituent at position 3. | 2.05 | 1 | 0 | erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; tryptophan zwitterion; tryptophan | antidepressant; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite |
| arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group. | 2.05 | 1 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| 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. | 2.05 | 1 | 0 | monocarboxylic acid; organochlorine compound | carcinogenic agent; metabolite; mouse metabolite |
| triamcinolone acetonide Triamcinolone Acetonide: An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions.. triamcinolone acetonide : A synthetic glucocorticoid that is the 16,17-acetonide of triamcinolone. Used to treat various skin infections. | 2.05 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; cyclic ketal; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone | anti-allergic agent; anti-inflammatory drug |
| allylpropymal allylpropymal: RN given refers to parent cpd. aprobarbital : A member of the class of barbiturates that is pyrimidine-2,4,6(1H,3H,5H)-trione substituted by an isopropyl and a prop-1-en-3-yl group at position 5. | 2.05 | 1 | 0 | barbiturates | |
| butobarbital butobarbital: Butobarbital should be distinguished from Butabarbital (a synonym for Secbutabarbital) | 2.05 | 1 | 0 | barbiturates | |
| trichloroethylene Trichloroethylene: A highly volatile inhalation anesthetic used mainly in short surgical procedures where light anesthesia with good analgesia is required. It is also used as an industrial solvent. Prolonged exposure to high concentrations of the vapor can lead to cardiotoxicity and neurological impairment.. triol : A chemical compound containing three hydroxy groups. | 2.05 | 1 | 0 | chloroethenes | inhalation anaesthetic; mouse metabolite |
| dehydrocholic acid Dehydrocholic Acid: A semisynthetic bile acid made from cholic acid. It is used as a cholagogue, hydrocholeretic, diuretic, and as a diagnostic aid.. 3,7,12-trioxo-5beta-cholanic acid : An oxo-5beta-cholanic acid in which three oxo substituents are located at positions 3, 7 and 12 on the cholanic acid skeleton. | 2.05 | 1 | 0 | 12-oxo steroid; 3-oxo-5beta-steroid; 7-oxo steroid; oxo-5beta-cholanic acid | gastrointestinal drug |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 2.05 | 1 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| isosorbide dinitrate Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. | 2.05 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| synephrine [no description available] | 2.05 | 1 | 0 | ethanolamines; phenethylamine alkaloid; phenols | alpha-adrenergic agonist; plant metabolite |
| 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. | 2.05 | 1 | 0 | carbonyl compound | |
| furan furan : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing four carbons and one oxygen, with formula C4H4O. It is a toxic, flammable, low-boiling (31degreeC) colourless liquid. | 2.05 | 1 | 0 | furans; mancude organic heteromonocyclic parent; monocyclic heteroarene | carcinogenic agent; hepatotoxic agent; Maillard reaction product |
| ergotamine Ergotamine: A vasoconstrictor found in ergot of Central Europe. It is a serotonin agonist that has been used as an oxytocic agent and in the treatment of MIGRAINE DISORDERS.. ergotamine : A peptide ergot alkaloid that is dihydroergotamine in which a double bond replaces the single bond between positions 9 and 10. | 2.05 | 1 | 0 | peptide ergot alkaloid | alpha-adrenergic agonist; mycotoxin; non-narcotic analgesic; oxytocic; serotonergic agonist; vasoconstrictor agent |
| neostigmine bromide neostigmine bromide : The bromide salt of neostigmine. | 2.05 | 1 | 0 | bromide salt | |
| phenformin Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis. | 2.05 | 1 | 0 | biguanides | antineoplastic agent; geroprotector; hypoglycemic agent |
| mephobarbital Mephobarbital: A barbiturate that is metabolized to PHENOBARBITAL. It has been used for similar purposes, especially in EPILEPSY, but there is no evidence mephobarbital offers any advantage over PHENOBARBITAL.. mephobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by ethyl and phenyl groups. | 2.05 | 1 | 0 | barbiturates | anticonvulsant |
| hexachlorobenzene Hexachlorobenzene: An agricultural fungicide and seed treatment agent.. hexachlorobenzene : A member of the class of chlorobenzenes that is benzene in which all of the hydrogens are replaced by chlorines. An agricultural fungicide introduced in the mid-1940s and formerly used as a seed treatment, its use has been banned since 1984 under the Stockholm Convention on Persistent Organic Pollutants. | 2.05 | 1 | 0 | aromatic fungicide; chlorobenzenes | antifungal agrochemical; carcinogenic agent; persistent organic pollutant |
| trinitrotoluene Trinitrotoluene: A 2,4,6-trinitrotoluene, which is an explosive chemical that can cause skin irritation and other toxic consequences.. 2,4,6-trinitrotoluene : A trinitrotoluene having the nitro groups at positions 2, 4 and 6. | 2.05 | 1 | 0 | trinitrotoluene | explosive |
| framycetin Framycetin: A component of NEOMYCIN that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed). framycetin : A tetracyclic antibacterial agent derived from neomycin, being a glycoside ester of neamine and neobiosamine B. | 2.05 | 1 | 0 | aminoglycoside | allergen; antibacterial drug; Escherichia coli metabolite |
| pyrazolanthrone pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase. | 2.05 | 1 | 0 | anthrapyrazole; aromatic ketone; cyclic ketone | antineoplastic agent; c-Jun N-terminal kinase inhibitor; geroprotector |
| meglumine Meglumine: 1-Deoxy-1-(methylamino)-D-glucitol. A derivative of sorbitol in which the hydroxyl group in position 1 is replaced by a methylamino group. Often used in conjunction with iodinated organic compounds as contrast medium.. N-methylglucamine : A hexosamine that is D-glucitol in which the hydroxy group at position 1 is substituted by the nitrogen of a methylamino group. A crystalline base, it is used in preparing salts of certain acids for use as diagnostic radiopaque media, while its antimonate is used as an antiprotozoal in the treatment of leishmaniasis. | 2.05 | 1 | 0 | hexosamine; secondary amino compound | |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 2.05 | 1 | 0 | quinolines | |
| yohimbine Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina. | 2.05 | 1 | 0 | methyl 17-hydroxy-20xi-yohimban-16-carboxylate | alpha-adrenergic antagonist; dopamine receptor D2 antagonist; serotonergic antagonist |
| mequinol mequinol: depigmenting agent; RN given refers to parent cpd | 2.05 | 1 | 0 | methoxybenzenes; phenols | metabolite |
| quinestrol Quinestrol: The 3-cyclopentyl ether of ETHINYL ESTRADIOL. After gastrointestinal absorption, it is stored in ADIPOSE TISSUE, slowly released, and metabolized principally to the parent compound. It has been used in ESTROGEN REPLACEMENT THERAPY. (From AMA Drug Evaluations Annual, 1992, p1011) | 2.05 | 1 | 0 | 17-hydroxy steroid; terminal acetylenic compound | xenoestrogen |
| dydrogesterone [no description available] | 2.05 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid | progestin |
| 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. | 2.05 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| chlormadinone acetate Chlormadinone Acetate: An orally active synthetic progestational hormone used often in combinations as an oral contraceptive (CONTRACEPTIVES, ORAL). | 2.05 | 1 | 0 | corticosteroid hormone | |
| 2,3-dimercaptosuccinic acid [no description available] | 2.05 | 1 | 0 | ||
| evans blue Evans Blue: An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly.. Evans blue : An organic sodium salt that is the tetrasodium salt of 6,6'-{(3,3'-dimethyl[1,1'-biphenyl]-4,4'-diyl)bis[diazene-2,1-diyl]}bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate). It is sometimes used as a counterstain, especially in fluorescent methods to suppress background autofluorescence. | 2.05 | 1 | 0 | organic sodium salt | fluorochrome; histological dye; sodium channel blocker; teratogenic agent |
| testosterone enanthate [no description available] | 2.05 | 1 | 0 | heptanoate ester; sterol ester | androgen |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 2.05 | 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. | 2.05 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| phenyramidol phenyramidol: considered as a drug that possibly causes hepatotoxicity | 2.05 | 1 | 0 | aminopyridine | |
| carbutamide Carbutamide: A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277) | 2.05 | 1 | 0 | benzenes; sulfonamide | |
| 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. | 2.05 | 1 | 0 | steroid ester | |
| bucladesine [no description available] | 2.05 | 1 | 0 | 3',5'-cyclic purine nucleotide; butanamides; butyrate ester | agonist; cardiotonic drug; vasodilator agent |
| betamethasone Betamethasone: A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724) | 2.05 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | anti-asthmatic agent; anti-inflammatory drug; immunosuppressive agent |
| perflubron perflubron: potential anti-obesity compound; reduces food adsorption; 8-carbon perfluorocarbon radiopaque compound; an oral contrast agent for use with MRI to enhance delineation of the bowel distinguishing it from adjacent organs. perflubron : A haloalkane that is perfluorooctane in which a fluorine attached to one of the terminal carbons has been replaced by a bromine. | 2.05 | 1 | 0 | haloalkane; organobromine compound; perfluorinated compound | blood substitute; radioopaque medium |
| cyproterone acetate [no description available] | 2.05 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; chlorinated steroid; steroid ester | androgen antagonist; geroprotector; progestin |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 2.05 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| glycyrrhetinic acid [no description available] | 2.05 | 1 | 0 | cyclic terpene ketone; hydroxy monocarboxylic acid; pentacyclic triterpenoid | immunomodulator; plant metabolite |
| 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. | 2.05 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| dihydralazine Dihydralazine: 1,4-Dihydrazinophthalazine. An antihypertensive agent with actions and uses similar to those of HYDRALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p354) | 2.05 | 1 | 0 | phthalazines | |
| phenylpropanolamine Phenylpropanolamine: A sympathomimetic that acts mainly by causing release of NOREPINEPHRINE but also has direct agonist activity at some adrenergic receptors. It is most commonly used as a nasal vasoconstrictor and an appetite depressant.. phenylpropanolamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group. A decongestant and appetite suppressant, it is commonly used in prescription and over-the-counter cough and cold preparations.. (-)-norephedrine : An amphetamine that is propylbenzene substituted by a hydroxy group at position 1 and by an amino group at position 2 (the 1R,2S-stereoisomer). It is a plant alkaloid. | 2.05 | 1 | 0 | amphetamines; phenethylamine alkaloid | plant metabolite |
| 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. | 2.05 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| podophyllotoxin Podophyllum: A genus of poisonous American herbs, family BERBERIDACEAE. The roots yield PODOPHYLLOTOXIN and other pharmacologically important agents. The plant was formerly used as a cholagogue and cathartic. It is different from the European mandrake, MANDRAGORA. | 2.05 | 1 | 0 | furonaphthodioxole; lignan; organic heterotetracyclic compound | antimitotic; antineoplastic agent; keratolytic drug; microtubule-destabilising agent; plant metabolite; tubulin modulator |
| hesperidin Hesperidin: A flavanone glycoside found in CITRUS fruit peels.. hesperidin : A disaccharide derivative that consists of hesperetin substituted by a 6-O-(alpha-L-rhamnopyranosyl)-beta-D-glucopyranosyl moiety at position 7 via a glycosidic linkage. | 2.05 | 1 | 0 | 3'-hydroxyflavanones; 4'-methoxyflavanones; dihydroxyflavanone; disaccharide derivative; flavanone glycoside; monomethoxyflavanone; rutinoside | mutagen |
| chlormethiazole Chlormethiazole: A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors. | 2.05 | 1 | 0 | thiazoles | |
| methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. | 2.05 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| gentian violet Gentian Violet: A dye that is a mixture of violet rosanilinis with antibacterial, antifungal, and anthelmintic properties.. crystal violet : An organic chloride salt that is the monochloride salt of crystal violet cation. It has been used in creams for the topical treatment of bacterial and fungal infections, being effective against some Gram-positive bacteria (notably Staphylococcus species) and some pathogenic fungi (including Candida species) but use declined following reports of animal carcinogenicity. It has also been used for dying wood, silk, and paper, as well as a histological stain. | 2.05 | 1 | 0 | organic chloride salt | anthelminthic drug; antibacterial agent; antifungal agent; antiseptic drug; histological dye |
| hematoporphyrin Hematoporphyrins: Iron-free derivatives of heme with 4 methyl groups, 2 hydroxyethyl groups and 2 propionic acid groups attached to the pyrrole rings. Some of these PHOTOSENSITIZING AGENTS are used in the PHOTOTHERAPY of malignant NEOPLASMS.. hematoporphyrin : A dicarboxylic acid that is protoporphyrin in which the vinyl groups at positions 7 and 12 are replaced by 1-hydroxyethyl groups. | 2.05 | 1 | 0 | ||
| lactulose [no description available] | 2.05 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| megestrol acetate [no description available] | 2.05 | 1 | 0 | 20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; steroid ester | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 2.05 | 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 stearate [no description available] | 2.05 | 1 | 0 | aminoglycoside | |
| 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. | 2.05 | 1 | 0 | cyclic ketone; erythromycin | |
| vinblastine [no description available] | 2.05 | 1 | 0 | ||
| estradiol valerate [no description available] | 2.05 | 1 | 0 | steroid ester | |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 2.05 | 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. | 2.05 | 1 | 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 |
| dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| sulfadoxine Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial. | 2.05 | 1 | 0 | pyrimidines; sulfonamide | antibacterial drug; antimalarial |
| acadesine [no description available] | 2.05 | 1 | 0 | 1-ribosylimidazolecarboxamide; aminoimidazole; nucleoside analogue | antineoplastic agent; platelet aggregation inhibitor |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 2.05 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| doxifluridine doxifluridine : A pyrimidine 5'-deoxyribonucleoside that is 5-fluorouridine in which the hydroxy group at the 5' position is replaced by a hydrogen. It is an oral prodrug of the antineoplastic agent 5-fluorouracil. Designed to circumvent the rapid degradation of 5-fluorouracil by dihydropyrimidine dehydrogenase in the gut wall, it is converted into 5-fluorouracil in the presence of pyrimidine nucleoside phosphorylase. | 2.05 | 1 | 0 | organofluorine compound; pyrimidine 5'-deoxyribonucleoside | antimetabolite; antineoplastic agent; prodrug |
| iproclozide iproclozide: structure | 2.05 | 1 | 0 | aromatic ether | |
| streptomycin [no description available] | 2.05 | 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] | 2.05 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| carbenicillin disodium [no description available] | 2.05 | 1 | 0 | organic sodium salt | |
| dehydroemetine dehydroemetine: was MH 1991-94 (see under EMETINE 1976-90); use EMETINE to search DEHYDROEMETINE 1976-94; amebicide, derivative of emetine. dehydroemetine : A pyridoisoquinoline which was developed in response to the cardiovascular toxicity associated with emetine and results from the dehydrogenation of the heterotricylic ring of emetine. It is an antiprotozoal agent and displays antimalarial, antiamoebic, and antileishmanial properties. | 2.05 | 1 | 0 | aromatic ether; isoquinolines; pyridoisoquinoline | antileishmanial agent; antimalarial; antiprotozoal drug |
| benorilate benorilate: was heading 1980-94 (see under SALICYLATES 1980-90); was BENORYLATE see under SALICYLATES 1975-79; BENORYLATE was see BENORILATE 1980-94; use SALICYLATES to search BENORILATE 1980-90 & BENORYLATE 1975-79; an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases; it has less severe side effects than aspirin | 2.05 | 1 | 0 | carbonyl compound | |
| trimetazidine Trimetazidine: A vasodilator used in angina of effort or ischemic heart disease. | 2.05 | 1 | 0 | aromatic amine | |
| floxacillin Floxacillin: Antibiotic analog of CLOXACILLIN.. flucloxacillin : A penicillin compound having a 6beta-[3-(2-chloro-6-fluorophenyl)-5-methyl-1,2-oxazole-4-carboxamido] side-chain. | 2.05 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| vidarabine adenine arabinoside : A purine nucleoside in which adenine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. | 2.05 | 1 | 0 | beta-D-arabinoside; purine nucleoside | antineoplastic agent; bacterial metabolite; nucleoside antibiotic |
| tiadenol tiadenol: structure | 2.05 | 1 | 0 | aliphatic sulfide | |
| zalcitabine Zalcitabine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.. zalcitabine : A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase. | 2.05 | 1 | 0 | pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source | 2.05 | 1 | 0 | delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite |
| stanozolol Stanozolol: A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194). stanozolol : An organic heteropentacyclic compound resulting from the formal condensation of the 3-keto-aldehyde moiety of oxymetholone with hydrazine. Like oxymetholone, it is a synthetic anabolic steroid. It has both anabolic and androgenic properties, and has been used to treat hereditary angioedema and various vascular disorders. It has also been widely abused by professional athletes. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; anabolic androgenic steroid; organic heteropentacyclic compound; tertiary alcohol | anabolic agent; androgen |
| clodronic acid Clodronic Acid: A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification.. clodronic acid : An organochlorine compound that is methylene chloride in which both hydrogens are replaced by phosphonic acid groups. It inhibits bone resorption and soft tissue calcification, and is used (often as the disodium salt tetrahydrate) as an adjunct in the treatment of severe hypercalcaemia associated with malignancy, and in the management of osteolytic lesions and bone pain associated with skeletal metastases. | 2.05 | 1 | 0 | 1,1-bis(phosphonic acid); one-carbon compound; organochlorine compound | antineoplastic agent; bone density conservation agent |
| xipamide Xipamide: A sulfamoylbenzamide analog of CLOPAMIDE. It is diuretic and saluretic with antihypertensive activity. It is bound to PLASMA PROTEINS, thus has a delayed onset and prolonged action. | 2.05 | 1 | 0 | benzamides | |
| selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. | 2.05 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| levamisole Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine. | 2.05 | 1 | 0 | 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole | antinematodal drug; antirheumatic drug; EC 3.1.3.1 (alkaline phosphatase) inhibitor; immunological adjuvant; immunomodulator |
| thiamphenicol [no description available] | 2.05 | 1 | 0 | monocarboxylic acid amide; sulfone | antimicrobial agent; immunosuppressive agent |
| pizotyline Pizotyline: Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches.. pizotifen : A benzocycloheptathiophene that is 9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophene 4-ylidene)-1-methylpiperidine which is joined from the 4 position to the 4 position of an N-methylpiperidine moiety by a double bond. It is a sedating antihistamine, with strong serotonin antagonist and weak antimuscarinic activity. It is generally used as the malate salt for the treatment of migraine and the prevention of headache attacks during cluster periods. | 2.05 | 1 | 0 | benzocycloheptathiophene | histamine antagonist; muscarinic antagonist; serotonergic antagonist |
| isosorbide-5-mononitrate isosorbide-5-mononitrate: for prevention of angina pectoris; structure given in first source; a Russian drug | 2.05 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| 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. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola. | 2.05 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| carbimazole Carbimazole: An imidazole antithyroid agent. Carbimazole is metabolized to METHIMAZOLE, which is responsible for the antithyroid activity.. carbimazole : A member of the class of imidazoles that is methimazole in which the nitrogen bearing a hydrogen is converted into its ethoxycarbonyl derivative. A prodrug for methimazol, carbimazole is used for the treatment of hyperthyroidism. | 2.05 | 1 | 0 | 1,3-dihydroimidazole-2-thiones; carbamate ester | antithyroid drug; prodrug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 2.05 | 1 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| triamcinolone Triamcinolone: A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739). triamcinolone : A C21-steroid hormone that is 1,4-pregnadiene-3,20-dione carrying four hydroxy substituents at positions 11beta, 16alpha, 17alpha and 21 as well as a fluoro substituent at position 9. Used in the form of its 16,17-acetonide to treat various skin infections. | 2.05 | 1 | 0 | 11beta-hydroxy steroid; 16alpha-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; fluorinated steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | anti-allergic agent; anti-inflammatory drug |
| oxyphenisatin [no description available] | 2.05 | 1 | 0 | indoles | |
| tetrachloroethylene Tetrachloroethylene: A chlorinated hydrocarbon used as an industrial solvent and cooling liquid in electrical transformers. It is a potential carcinogen. | 2.05 | 1 | 0 | chlorocarbon; chloroethenes | nephrotoxic agent |
| 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. | 2.05 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| butachlor butachlor : An aromatic amide that is 2-choro-N-(2,6-diethylphenyl)acetamide in which the amide nitrogen has been replaced by a butoxymethyl group. | 2.05 | 1 | 0 | aromatic amide; organochlorine compound; tertiary carboxamide | environmental contaminant; herbicide; xenobiotic |
| rose bengal b disodium salt [no description available] | 2.05 | 1 | 0 | ||
| glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2. | 2.05 | 1 | 0 | glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical |
| cefazolin Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. | 2.05 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 2.05 | 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. | 2.05 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| nicergoline Nicergoline: An ergot derivative that has been used as a cerebral vasodilator and in peripheral vascular disease. It may ameliorate cognitive deficits in CEREBROVASCULAR DISORDERS. | 2.05 | 1 | 0 | organic heterotetracyclic compound; organonitrogen heterocyclic compound | |
| 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. | 2.05 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| amineptin amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne. | 2.05 | 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. | 2.05 | 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 | 2.05 | 1 | 0 | pyrroline | |
| tobramycin Tobramycin: An aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius. It is effective against gram-negative bacteria, especially the PSEUDOMONAS species. It is a 10% component of the antibiotic complex, NEBRAMYCIN, produced by the same species.. tobramycin : A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring. | 2.05 | 1 | 0 | amino cyclitol glycoside | antibacterial agent; antimicrobial agent; toxin |
| paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | 2.05 | 1 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| ribavirin Rebetron: Rebetron is tradename | 2.05 | 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. | 2.05 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis. | 2.05 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes | antihypertensive agent; hepatotoxic agent; loop diuretic |
| methyldopa Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | 2.05 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| bezafibrate [no description available] | 2.05 | 1 | 0 | aromatic ether; monocarboxylic acid amide; monocarboxylic acid; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| sq-11725 Nadolol: A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor.. nadolol : Nadolol is a diastereoisomeric mixture consisting of equimolar amounts of the four possible 2,3-cis-isomers of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-1,2,3,4-tetrahydronaphthalene-2,3-diol. | 2.05 | 1 | 0 | ||
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 2.05 | 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 |
| 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. | 2.05 | 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 |
| permethrin hemoglobin Atlanta-Coventry: Leu replaced by Pro at beta75 and Leu deleted at beta141 | 2.05 | 1 | 0 | cyclopropanecarboxylate ester; cyclopropanes | agrochemical; ectoparasiticide; pyrethroid ester acaricide; pyrethroid ester insecticide; scabicide |
| pirfenidone pirfenidone : A pyridone that is 2-pyridone substituted at positions 1 and 5 by phenyl and methyl groups respectively. An anti-inflammatory drug used for the treatment of idiopathic pulmonary fibrosis. | 2.05 | 1 | 0 | pyridone | antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| desogestrel Desogestrel: A synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents (ORAL CONTRACEPTIVES, COMBINED). | 2.05 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | contraceptive drug; progestin; synthetic oral contraceptive |
| muzolimine Muzolimine: A pyrazole diuretic with long duration and high capacity of action. It was proposed for kidney failure and hypertension but was withdrawn worldwide because of severe neurological effects. | 2.05 | 1 | 0 | dichlorobenzene | |
| epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. | 2.05 | 1 | 0 | aminoglycoside; anthracycline antibiotic; anthracycline; deoxy hexoside; monosaccharide derivative; p-quinones; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | antimicrobial agent; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| desflurane Desflurane: A fluorinated ether that is used as a volatile anesthetic for maintenance of general anesthesia. | 2.05 | 1 | 0 | organofluorine compound | inhalation anaesthetic |
| piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | cephalosporin | antibacterial drug |
| foscarnet sodium trisodium phosphonoformate : The trisodium salt of phosphonoformic acid. It is used as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 2.05 | 1 | 0 | one-carbon compound; organic sodium salt | antiviral drug |
| moxalactam Moxalactam: Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections.. moxalactam : A broad-spectrum oxacephem antibiotic in which the oxazine ring is substituted with a tetrazolylthiomethyl group and the azetidinone ring carries methoxy and 2-carboxy-2-(4-hydroxyphenyl)acetamido substituents. | 2.05 | 1 | 0 | cephalosporin; oxacephem | antibacterial drug |
| nicorandil Nicorandil: A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.. nicorandil : A pyrimidinecarboxamide that is nicotinamide in which one of the hydrogens attached to the carboxamide nitrogen is replaced by a 2-(nitrooxy)ethyl group. It has both nitrate-like and ATP-sensitive potassium channel activator properties, and is used for the prevention and treatment of angina pectoris. | 2.05 | 1 | 0 | nitrate ester; pyridinecarboxamide | potassium channel opener; vasodilator agent |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.05 | 1 | 0 | cephalosporin | antibacterial drug |
| encainide Encainide: One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM.. encainide : 4-Methoxy-N-phenylbenzamide in which the hydrogen at the 2 position of the phenyl group is substituted by a 2-(1-methylpiperidin-2-yl)ethyl group. A class Ic antiarrhythmic, the hydrochloride was used for the treatment of severe or life-threatening ventricular arrhythmias, but it was associated with increased death rates in patients who had asymptomatic heart rhythm abnormalities after a recent heart attack and was withdrawn from the market. | 2.05 | 1 | 0 | benzamides; piperidines | anti-arrhythmia drug; sodium channel blocker |
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 2.05 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 2.05 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 2.05 | 1 | 0 | ||
| lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom). | 2.05 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| enoximone Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE. | 2.05 | 1 | 0 | aromatic ketone | |
| piritrexim piritrexim: RN given refers to parent cpd; structure given in first source | 2.05 | 1 | 0 | ||
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 2.05 | 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 |
| pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 2.05 | 1 | 0 | 3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic) | anticholesteremic drug; environmental contaminant; metabolite; xenobiotic |
| atomoxetine hydrochloride Atomoxetine Hydrochloride: A propylamine derivative and selective ADRENERGIC UPTAKE INHIBITOR that is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER.. atomoxetine hydrochloride : The hydrochloride salt of atomoxetine. | 2.05 | 1 | 0 | hydrochloride | adrenergic uptake inhibitor; antidepressant |
| quinapril Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. | 2.05 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| gepirone gepirone: RN given refers to parent cpd; structure given in first source | 2.05 | 1 | 0 | N-arylpiperazine | |
| 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. | 2.05 | 1 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| sparfloxacin [no description available] | 2.05 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | |
| zileuton [no description available] | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| bromfenac bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure. | 2.05 | 1 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| atorvastatin [no description available] | 2.05 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 2.05 | 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] | 2.05 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| adefovir dipivoxil bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine: structure given in first source. adefovir pivoxil : An organic phosphonate that is the dipivoxil ester of adefovir. A prodrug for adefovir, an HIV-1 reverse transcriptase inhibitor, adefovir pivoxil is used to treat chronic hepatitis B viral infection. | 2.05 | 1 | 0 | 6-aminopurines; carbonate ester; ether; organic phosphonate | antiviral drug; DNA synthesis inhibitor; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent; prodrug |
| 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. | 2.05 | 1 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 2.05 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| halofuginone [no description available] | 2.05 | 1 | 0 | quinazolines | |
| ortho-cept ethinyl estradiol-desogestrel combination: Ethinyl Estradiol and Desogestrell given in fixed proportions; has proved to be an effective & well-tolerated oral contraceptive, which improves cycle control & has a beneficial effect on acne | 2.05 | 1 | 0 | ||
| cefprozil [no description available] | 2.05 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol [no description available] | 2.05 | 1 | 0 | stilbenoid | |
| 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. | 2.05 | 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. | 2.05 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| doxapram hydrochloride [no description available] | 2.05 | 1 | 0 | hydrochloride | central nervous system stimulant |
| 1,5-anhydroglucitol 1,5-anhydroglucitol: structure. 1,5-anhydro-D-glucitol : An anhydro sugar of D-glucitol. | 2.05 | 1 | 0 | anhydro sugar | human metabolite |
| betulinic acid [no description available] | 2.05 | 1 | 0 | hydroxy monocarboxylic acid; pentacyclic triterpenoid | anti-HIV agent; anti-inflammatory agent; antimalarial; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; plant metabolite |
| amprenavir [no description available] | 2.05 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| glutathione disulfide Glutathione Disulfide: A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized. | 2.05 | 1 | 0 | glutathione derivative; organic disulfide | Escherichia coli metabolite; mouse metabolite |
| bendamustine [no description available] | 2.05 | 1 | 0 | benzimidazoles | |
| erdosteine [no description available] | 2.05 | 1 | 0 | N-acyl-amino acid | |
| mizolastine [no description available] | 2.05 | 1 | 0 | benzimidazoles | |
| intoplicine intoplicine: structure in first source | 2.05 | 1 | 0 | pyridoindole | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 2.05 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| dexfenfluramine Dexfenfluramine: The S-isomer of FENFLURAMINE. It is a serotonin agonist and is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity.. (S)-fenfluramine : The S-enantiomer of fenfluramine. It stimulates the release of serotonin and selectively inhibits its reuptake, but unlike fenfluramine it does not possess catecholamine agonist activity. It was formerly given by mouth as the hydrochloride in the treatment of obesity, but, like fenfluramine, was withdrawn wolrdwide following reports of valvular heart defects. | 2.05 | 1 | 0 | fenfluramine | appetite depressant; serotonergic agonist; serotonin uptake inhibitor |
| 2-methoxyestradiol 2-methoxy-17beta-estradiol : A 17beta-hydroxy steroid, being 17beta-estradiol methoxylated at C-2. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid | angiogenesis modulating agent; antimitotic; antineoplastic agent; human metabolite; metabolite; mouse metabolite |
| medetomidine Medetomidine: An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE. | 2.05 | 1 | 0 | imidazoles | |
| 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. | 2.05 | 1 | 0 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| picosulfate sodium picosulfate sodium: contains two active ingredients, sodium picosulfate and magnesium citrate, which are both laxatives; structure | 2.05 | 1 | 0 | aryl sulfate; pyridines | |
| dienogest [no description available] | 2.05 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; aliphatic nitrile; steroid hormone | progesterone receptor agonist; progestin; synthetic oral contraceptive |
| morphazinamide morphazinamide: RN given refers to parent cpd; RN in Chemline for mono-HCL: 1473-73-0; structure in Merck Index | 2.05 | 1 | 0 | morpholines; pyrazines; secondary carboxamide | |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 2.05 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 2.05 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| cyclobutyrol cyclobutyrol: RN given refers to parent cpd; structure. cyclobutyrol : A hydroxy monocarboxylic acid in which the hydroxy group is geminal to a 1-carboxypropyl group on a cyclohexane ring. | 2.05 | 1 | 0 | hydroxy monocarboxylic acid | bile therapy drug |
| terlipressin terlivaz: first FDA approved injection to improve kidney function in adults with hepatorenal syndrome (HRS) with rapid reduction in kidney function. | 2.05 | 1 | 0 | polypeptide | |
| isoflavone [no description available] | 2.05 | 1 | 0 | isoflavones | |
| clevudine [no description available] | 2.05 | 1 | 0 | ||
| tetrandrine tetrandrine: a bisbenzylisoquinoline that exhibits antifibrogenic activity | 2.05 | 1 | 0 | bisbenzylisoquinoline alkaloid; isoquinolines | |
| rosiglitazone [no description available] | 2.05 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis. | 2.05 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum. | 2.05 | 1 | 0 | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic |
| lopinavir [no description available] | 2.05 | 1 | 0 | amphetamines; dicarboxylic acid diamide | anticoronaviral agent; antiviral drug; HIV protease inhibitor |
| sr141716 [no description available] | 2.05 | 1 | 0 | amidopiperidine; carbohydrazide; dichlorobenzene; monochlorobenzenes; pyrazoles | anti-obesity agent; appetite depressant; CB1 receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 2.05 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| selenomethionine [no description available] | 2.05 | 1 | 0 | amino acid zwitterion; selenomethionine | plant metabolite |
| perindopril Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline | 2.05 | 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 |
| fingolimod fingolimod : An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate. | 2.05 | 1 | 0 | aminodiol; primary amino compound | antineoplastic agent; CB1 receptor antagonist; immunosuppressive agent; prodrug; sphingosine-1-phosphate receptor agonist |
| ecteinascidin 743 [no description available] | 2.05 | 1 | 0 | acetate ester; azaspiro compound; bridged compound; hemiaminal; isoquinoline alkaloid; lactone; organic heteropolycyclic compound; organic sulfide; oxaspiro compound; polyphenol; tertiary amino compound | alkylating agent; angiogenesis modulating agent; anti-inflammatory agent; antineoplastic agent; marine metabolite |
| nitisinone [no description available] | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| marimastat marimastat: a matrix metalloproteinase inhibitor active in patients with advanced carcinoma of the pancreas, prostate, or ovary. marimastat : A secondary carboxamide resulting from the foraml condensation of the carboxy group of (2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the alpha-amino group of N,3-dimethyl-L-valinamide. | 2.05 | 1 | 0 | hydroxamic acid; secondary carboxamide | antineoplastic agent; matrix metalloproteinase inhibitor |
| clofarabine [no description available] | 2.05 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| mitiglinide mitiglinide: a rapid and short-acting hypoglycemic agent; acts on sulfonylurea receptor closing KATP channels; considered one of the glinides-an imprecise grouping; structure given in first source | 2.05 | 1 | 0 | benzenes; monocarboxylic acid | |
| imatinib mesylate imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours. | 2.05 | 1 | 0 | methanesulfonate salt | anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| gefitinib [no description available] | 2.05 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine: structure given in first source; a selective A(3) adenosine receptor agonist. 3-iodobenzyl-5'-N-methylcarboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and one of the hydrogens of the exocyclic amino function is substituted by a 3-iodobenzyl group. | 2.05 | 1 | 0 | adenosines; monocarboxylic acid amide; organoiodine compound | adenosine A3 receptor agonist |
| methotrexate [no description available] | 2.05 | 1 | 0 | dicarboxylic acid; monocarboxylic acid amide; pteridines | abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent |
| antiprimod azaspirane: structure given in first source | 2.05 | 1 | 0 | ||
| sulbactam [no description available] | 2.05 | 1 | 0 | penicillanic acids | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 2.05 | 1 | 0 | biphenyls | |
| ilomastat CS 610: matrix metalloproteinase inhibitor; structure in first source. ilomastat : An N-acyl-amino acid obtained by formal condensation of the carboxy group of (2R)-2-[2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoic acid with the amino group of N-methyl-L-tryptophanamide. A cell permeable broad-spectrum matrix metalloproteinase (MMP) inhibitor | 2.05 | 1 | 0 | hydroxamic acid; L-tryptophan derivative; N-acyl-amino acid | anti-inflammatory agent; antibacterial agent; antineoplastic agent; EC 3.4.24.24 (gelatinase A) inhibitor; neuroprotective agent |
| docetaxel [no description available] | 2.05 | 1 | 0 | hydrate; secondary alpha-hydroxy ketone | antineoplastic 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). | 2.05 | 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. | 2.05 | 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). | 2.05 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| cariporide cariporide: a selective sodium-hydrogen exchange subtype 1 inhibitor; structure in first source | 2.05 | 1 | 0 | ||
| tezosentan tezosentan: structure in first source | 2.05 | 1 | 0 | ||
| moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. | 2.05 | 1 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| jtt 501 JTT 501: an insulin sensitizer; structure in first source | 2.05 | 1 | 0 | ||
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 2.05 | 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 |
| cyc 202 seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors. | 2.05 | 1 | 0 | 2,6-diaminopurines | antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| 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. | 2.05 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | anthelminthic drug; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| avasimibe [no description available] | 2.05 | 1 | 0 | monoterpenoid | |
| biotin vitamin B7 : Any member of a group of vitamers that belong to the chemical structural class called biotins that exhibit biological activity against vitamin B7 deficiency. Vitamin B7 deficiency is very rare in individuals who take a normal balanced diet. Foods rich in biotin are egg yolk, liver, cereals, vegetables (spinach, mushrooms) and rice. Symptoms associated with vitamin B7 deficiency include thinning hair, scaly skin rashes around eyes, nose and mouth, and brittle nails. The vitamers include biotin and its ionized and salt forms. | 2.05 | 1 | 0 | biotins; vitamin B7 | coenzyme; cofactor; Escherichia coli metabolite; fundamental metabolite; human metabolite; mouse metabolite; nutraceutical; prosthetic group; Saccharomyces cerevisiae metabolite |
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 2.05 | 1 | 0 | ||
| troleandomycin Troleandomycin: A macrolide antibiotic that is similar to ERYTHROMYCIN.. troleandomycin : A semi-synthetic macrolide antibiotic obtained by acetylation of the three free hydroxy groups of oleandomycin. Troleandomycin is only found in individuals that have taken the drug. | 2.05 | 1 | 0 | acetate ester; epoxide; macrolide antibiotic; monosaccharide derivative; polyketide; semisynthetic derivative | EC 1.14.13.97 (taurochenodeoxycholate 6alpha-hydroxylase) inhibitor; xenobiotic |
| 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. | 2.05 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 2.05 | 1 | 0 | benzodioxoles | |
| sitosterol, (3beta)-isomer Sobatum: tradename; active fraction of Solanum trilobatum; reduces side-effects of radiation-induced toxicity. sitosterol : A member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3. | 2.05 | 1 | 0 | 3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; C29-steroid; phytosterols; stigmastane sterol | anticholesteremic drug; antioxidant; mouse metabolite; plant metabolite; sterol methyltransferase inhibitor |
| benzarone benzarone: antihemorrhagic agent; structure | 2.05 | 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. | 2.05 | 1 | 0 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| noscapine Noscapine: A naturally occurring opium alkaloid that is a centrally acting antitussive agent.. (-)-noscapine : A benzylisoquinoline alkaloid that is 1,2,3,4-tetrahydroisoquinoline which is substituted by a 4,5-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-1-yl group at position 1, a methylenedioxy group at positions 6-7 and a methoxy group at position 8. Obtained from plants of the Papaveraceae family, it lacks significant painkilling properties and is primarily used for its antitussive (cough-suppressing) effects. | 2.05 | 1 | 0 | aromatic ether; benzylisoquinoline alkaloid; cyclic acetal; isobenzofuranone; organic heterobicyclic compound; organic heterotricyclic compound; tertiary amino compound | antineoplastic agent; antitussive; apoptosis inducer; plant metabolite |
| homoharringtonine Homoharringtonine: Semisynthetic derivative of harringtonine that acts as a protein synthesis inhibitor and induces APOPTOSIS in tumor cells. It is used in the treatment of MYELOID LEUKEMIA, CHRONIC.. omacetaxine mepesuccinate : A cephalotaxine-derived alkaloid ester obtained from Cephalotaxus harringtonia; used for the treatment of chronic or accelerated phase chronic myeloid leukaemia. | 2.05 | 1 | 0 | alkaloid ester; enol ether; organic heteropentacyclic compound; tertiary alcohol | anticoronaviral agent; antineoplastic agent; apoptosis inducer; protein synthesis inhibitor |
| o-(chloroacetylcarbamoyl)fumagillol O-(Chloroacetylcarbamoyl)fumagillol: Semisynthetic analog of fumagillin (a cyclohexane-sesquiterpene antibiotic isolated from ASPERGILLUS FUMIGATUS) that inhibits angiogenesis.. O-(chloroacetylcarbamoyl)fumagillol : A carbamate ester that is fumagillol in which the hydroxy group has been converted to the corresponding N-(chloroacetyl)carbamate derivative. | 2.05 | 1 | 0 | carbamate ester; organochlorine compound; semisynthetic derivative; sesquiterpenoid; spiro-epoxide | angiogenesis inhibitor; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; methionine aminopeptidase 2 inhibitor; retinoic acid receptor alpha antagonist |
| bortezomib [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| nexavar [no description available] | 2.05 | 1 | 0 | organosulfonate salt | |
| glucosamine D-glucosamine : An amino sugar whose structure comprises D-glucose having an amino substituent at position 2.. 2-amino-2-deoxy-D-glucopyranose : A D-glucosamine whose structure comprises D-glucopyranose having an amino substituent at position 2. | 2.05 | 1 | 0 | D-glucosamine | Escherichia coli metabolite; geroprotector; mouse metabolite |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | 1-benzofurans; antibiotic antifungal drug; benzofuran antifungal drug; organochlorine compound; oxaspiro compound | antibacterial agent; Penicillium metabolite |
| digitoxin Digitoxin: A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665). digitoxin : A cardenolide glycoside in which the 3beta-hydroxy group of digitoxigenin carries a 2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-D-ribo-hexopyranosyl trisaccharide chain. | 2.05 | 1 | 0 | cardenolide glycoside | EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 2.05 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| netilmicin Netilmicin: Semisynthetic 1-N-ethyl derivative of SISOMYCIN, an aminoglycoside antibiotic with action similar to gentamicin, but less ear and kidney toxicity. | 2.05 | 1 | 0 | ||
| trimethaphan camsylate trimethaphan camsylate : The (S)-camphorsulfonate salt of trimethaphan. | 2.05 | 1 | 0 | ||
| erythromycin estolate Erythromycin Estolate: A macrolide antibiotic, produced by Streptomyces erythreus. It is the lauryl sulfate salt of the propionic ester of erythromycin. This erythromycin salt acts primarily as a bacteriostatic agent. 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. | 2.05 | 1 | 0 | aminoglycoside sulfate salt; erythromycin derivative | enzyme inhibitor |
| cyclopamine [no description available] | 2.05 | 1 | 0 | piperidines | glioma-associated oncogene inhibitor |
| devazepide Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.. devazepide : An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders. | 2.05 | 1 | 0 | 1,4-benzodiazepinone; indolecarboxamide | antineoplastic agent; apoptosis inducer; cholecystokinin antagonist; gastrointestinal drug |
| tolterodine [no description available] | 2.05 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| doxorubicin hydrochloride [no description available] | 2.05 | 1 | 0 | anthracycline | |
| erythromycin ethylsuccinate Erythromycin Ethylsuccinate: A macrolide antibiotic, produced by Streptomyces erythreus. This compound is an ester of erythromycin base and succinic acid. It acts primarily as a bacteriostatic agent. 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 ethylsuccinate : A erythromycin derivative that is erythromycin A in which the hydroxy group at position 3R is substituted by a (4-ethoxy-4-oxobutanoyl)oxy group. It is used for the treatment of a wide variety of bacterial infections. | 2.05 | 1 | 0 | cyclic ketone; erythromycin derivative; ethyl ester; succinate ester | |
| ao 128 AO 128: alpha-glucosidase inhibitor; structure given in first source | 2.05 | 1 | 0 | organic molecular entity | |
| acarbose [no description available] | 2.05 | 1 | 0 | amino cyclitol; glycoside | |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 2.05 | 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). | 2.05 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| alpha-D-fructofuranose 1,6-bisphosphate alpha-D-fructofuranose 1,6-bisphosphate : A D-fructofuranose 1,6-bisphosphate with an alpha-configuration at the anomeric position. | 2.05 | 1 | 0 | D-fructofuranose 1,6-bisphosphate | |
| docosahexaenoate efalex: a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement. docosahexaenoic acid : Any C22 polyunsaturated fatty acid containing six double bonds.. docosahexaenoate : A polyunsaturated fatty acid anion that is the conjugate base of docosahexaenoic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.. all-cis-docosa-4,7,10,13,16,19-hexaenoic acid : A docosahexaenoic acid having six cis-double bonds at positions 4, 7, 10, 13, 16 and 19. | 2.05 | 1 | 0 | docosahexaenoic acid; omega-3 fatty acid | algal metabolite; antineoplastic agent; Daphnia tenebrosa metabolite; human metabolite; mouse metabolite; nutraceutical |
| oleic acid Oleic Acid: An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed). oleic acid : An octadec-9-enoic acid in which the double bond at C-9 has Z (cis) stereochemistry. | 2.05 | 1 | 0 | octadec-9-enoic acid | antioxidant; Daphnia galeata metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; Escherichia coli metabolite; mouse metabolite; plant metabolite; solvent |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 2.05 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| cerivastatin cerivastatin: cerivastatin is the ((E)-(+))-isomer; structure given in first source. cerivastatin : (3R,5S)-3,5-dihydroxyhept-6-enoic acid in which the (7E)-hydrogen is substituted by a 4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl group. Formerly used (as its sodium salt) to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity. | 2.05 | 1 | 0 | dihydroxy monocarboxylic acid; pyridines; statin (synthetic) | |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 2.05 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| cocaine Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. | 2.05 | 1 | 0 | benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid | adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| eicosapentaenoic acid icosapentaenoic acid : Any straight-chain, C20 polyunsaturated fatty acid having five C=C double bonds.. all-cis-5,8,11,14,17-icosapentaenoic acid : An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17. | 2.05 | 1 | 0 | icosapentaenoic acid; omega-3 fatty acid | anticholesteremic drug; antidepressant; antineoplastic agent; Daphnia galeata metabolite; fungal metabolite; micronutrient; mouse metabolite; nutraceutical |
| mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. | 2.05 | 1 | 0 | 2-benzofurans; gamma-lactone; monocarboxylic acid; phenols | anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic |
| clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| drf 2725 ragaglitazar: a phenoxazine analogue of phenyl propanoic acid; Ragaglitazar is a coligand of PPARalpha and PPARgamma | 2.05 | 1 | 0 | ||
| 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. | 2.05 | 1 | 0 | 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 |
| alitretinoin Alitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA. | 2.05 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; metabolite; retinoid X receptor agonist |
| decitabine [no description available] | 2.05 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 2.05 | 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) | 2.05 | 1 | 0 | actinomycin | mutagen |
| tiazofurin tiazofurin: RN given refers to (beta-D)-isomer; structure given in first source. tiazofurine : A C-glycosyl compound that is 1,3-thiazole-4-carboxamide in which the hydrogen at position 2 has been replaced by a beta-D-ribofuranosyl group. It is metabolised to thiazole-4-carboxamide adenine dinucleotide (TAD), a selective inhibitor of inosine monophosphate dehydrogenase (IMP dehydrogenase). | 2.05 | 1 | 0 | 1,3-thiazoles; C-glycosyl compound; monocarboxylic acid amide | antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; prodrug |
| melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring. | 2.05 | 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 |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 2.05 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| rubitecan rubitecan: RN refers to (+-)-isomer; anti-HIV agent; DNA Topoisomerases, Type I inhibitor. rubitecan : A pyranoindolizinoquinoline that is camptothecin in which the hydrogen at position 9 has been replaced by a nitro group. It is a prodrug for 9-aminocamptothecin. | 2.05 | 1 | 0 | C-nitro compound; delta-lactone; pyranoindolizinoquinoline; semisynthetic derivative; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy. | 2.05 | 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). | 2.05 | 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. | 2.05 | 1 | 0 | one-carbon compound; organic sodium salt | antacid; food anticaking agent |
| sodium acetate, anhydrous Sodium Acetate: The trihydrate sodium salt of acetic acid, which is used as a source of sodium ions in solutions for dialysis and as a systemic and urinary alkalizer, diuretic, and expectorant. | 2.05 | 1 | 0 | organic sodium salt | NMR chemical shift reference compound |
| sodium benzoate Sodium Benzoate: The sodium salt of BENZOIC ACID. It is used as an antifungal preservative in pharmaceutical preparations and foods. It may also be used as a test for liver function.. sodium benzoate : An organic sodium salt resulting from the replacement of the proton from the carboxy group of benzoic acid by a sodium ion. | 2.05 | 1 | 0 | organic sodium salt | algal metabolite; antimicrobial food preservative; drug allergen; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor; human xenobiotic metabolite; plant metabolite |
| dipyrone Dipyrone: A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.. metamizole sodium : An organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic. | 2.05 | 1 | 0 | organic sodium salt | anti-inflammatory agent; antipyretic; antirheumatic drug; cyclooxygenase 3 inhibitor; non-narcotic analgesic; peripheral nervous system drug; prodrug |
| ditiocarb sodium [no description available] | 2.05 | 1 | 0 | organic molecular entity | |
| carbenoxolone [no description available] | 2.05 | 1 | 0 | ||
| discodermolide [no description available] | 2.05 | 1 | 0 | diterpenoid | |
| cannabidiol Cannabidiol: Compound isolated from Cannabis sativa extract.. cannabidiol : An cannabinoid that is cyclohexene which is substituted by a methyl group at position 1, a 2,6-dihydroxy-4-pentylphenyl group at position 3, and a prop-1-en-2-yl group at position 4. | 2.05 | 1 | 0 | olefinic compound; phytocannabinoid; resorcinols | antimicrobial agent; plant metabolite |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 2.05 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| prothionamide Prothionamide: Antitubercular agent similar in action and side effects to ETHIONAMIDE. It is used mostly in combination with other agents. | 2.05 | 1 | 0 | pyridines | |
| etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. | 2.05 | 1 | 0 | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 2.05 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 2.05 | 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. | 2.05 | 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 |
| capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers. | 2.05 | 1 | 0 | capsaicinoid | non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker |
| terbinafine [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| tacrine hydrochloride [no description available] | 2.05 | 1 | 0 | ||
| sodium propionate sodium propionate: was term of propionic acid (1986-2006). sodium propionate : An organic sodium salt comprising equal numbers of sodium and propionate ions. | 2.05 | 1 | 0 | organic sodium salt | antifungal drug; food preservative |
| digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. | 2.05 | 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] | 2.05 | 1 | 0 | ||
| tamoxifen [no description available] | 2.05 | 1 | 0 | stilbenoid; tertiary amino compound | angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator |
| ethionamide Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide. | 2.05 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| fusidic acid Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum. | 2.05 | 1 | 0 | 11alpha-hydroxy steroid; 3alpha-hydroxy steroid; alpha,beta-unsaturated monocarboxylic acid; steroid acid; steroid antibiotic; sterol ester | EC 2.7.1.33 (pantothenate kinase) inhibitor; Escherichia coli metabolite; protein synthesis inhibitor |
| estrone sulfate estrone sulfate: sulfoconjugated estrone; RN given refers to parent cpd | 2.05 | 1 | 0 | 17-oxo steroid; steroid sulfate | human metabolite; mouse metabolite |
| hmr 3647 [no description available] | 2.05 | 1 | 0 | ||
| toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. | 2.05 | 1 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| telaprevir [no description available] | 2.05 | 1 | 0 | cyclopentapyrrole; cyclopropanes; oligopeptide; pyrazines | antiviral drug; hepatitis C protease inhibitor; peptidomimetic |
| droloxifene [no description available] | 2.05 | 1 | 0 | stilbenoid | |
| or 1259 [no description available] | 2.05 | 1 | 0 | hydrazone; nitrile; pyridazinone | anti-arrhythmia drug; cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; vasodilator agent |
| gestodene Gestodene: synthetic steroid with progestational activity; RN given refers to (17alpha)-isomer | 2.05 | 1 | 0 | steroid | estrogen |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 2.05 | 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 |
| idoxifene idoxifene: structure given in first source | 2.05 | 1 | 0 | stilbenoid | |
| zd 6474 CH 331: structure in first source | 2.05 | 1 | 0 | aromatic ether; organobromine compound; organofluorine compound; piperidines; quinazolines; secondary amine | antineoplastic agent; tyrosine kinase inhibitor |
| silybin [no description available] | 2.05 | 1 | 0 | ||
| chloramine-t chloramine-T: RN given refers to unlabeled parent cpd. chloramine T : An organic sodium salt derivative of toluene-4-sulfonamide with a chloro substituent in place of an amino hydrogen. | 2.05 | 1 | 0 | organic sodium salt | allergen; antifouling biocide; disinfectant |
| flosequinan [no description available] | 2.05 | 1 | 0 | quinolines | |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 2.05 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins. | 2.05 | 1 | 0 | prostaglandins E | human metabolite; mouse metabolite; oxytocic |
| dinoprost Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor. | 2.05 | 1 | 0 | monocarboxylic acid; prostaglandins Falpha | human metabolite; mouse metabolite |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 2.05 | 1 | 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. | 2.05 | 1 | 0 | carotenoid beta-end derivative; cyclic carotene | antioxidant; biological pigment; cofactor; ferroptosis inhibitor; human metabolite; mouse metabolite; plant metabolite; provitamin A |
| alprostadil [no description available] | 2.05 | 1 | 0 | prostaglandins E | anticoagulant; human metabolite; platelet aggregation inhibitor; vasodilator agent |
| cholecalciferol Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24.. calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone. | 2.05 | 1 | 0 | D3 vitamins; hydroxy seco-steroid; seco-cholestane; secondary alcohol; steroid hormone | geroprotector; human 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. | 2.05 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| clavulanic acid Clavulanic Acid: A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase.. clavulanate : The conjugate base of clavulanic acid.. clavulanic acid : Antibiotic isolated from Streptomyces clavuligerus. It acts as a suicide inhibitor of bacterial beta-lactamase enzymes. | 2.05 | 1 | 0 | oxapenam | antibacterial drug; anxiolytic drug; bacterial metabolite; EC 3.5.2.6 (beta-lactamase) inhibitor |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 2.05 | 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. | 2.05 | 1 | 0 | ||
| montelukast montelukast: a leukotriene D4 receptor antagonist | 2.05 | 1 | 0 | aliphatic sulfide; monocarboxylic acid; quinolines | anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist |
| 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. | 2.05 | 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. | 2.05 | 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 |
| astaxanthine astaxanthine: a keto form of carotene; pigment in flesh of Scottish salmon (Salmo salar) crustacoa-lobster (Homarus gammarus, flamingo feathers; structure; a carotenoid without vitamin A activity, has shown anti-oxidant and anti-inflammatory activities. astaxanthin : A carotenone that consists of beta,beta-carotene-4,4'-dione bearing two hydroxy substituents at positions 3 and 3' (the 3S,3'S diastereomer). A carotenoid pigment found mainly in animals (crustaceans, echinoderms) but also occurring in plants. It can occur free (as a red pigment), as an ester, or as a blue, brown or green chromoprotein. | 2.05 | 1 | 0 | carotenol; carotenone | animal metabolite; anticoagulant; antioxidant; food colouring; plant metabolite |
| diosmin [no description available] | 2.05 | 1 | 0 | dihydroxyflavanone; disaccharide derivative; glycosyloxyflavone; monomethoxyflavone; rutinoside | anti-inflammatory agent; antioxidant |
| cynarine cynarine: active principle of the artichoke; functions primarily as a cholagogue and choleretic and also as antilipemic agent | 2.05 | 1 | 0 | alkyl caffeate ester; quinic acid | plant metabolite |
| sdz psc 833 valspodar: nonimmunosuppressive cyclosporin analog which is a potent multidrug resistance modifier; 7-10 fold more potent than cyclosporin A; a potent P glycoprotein inhibitor; MW 1215 | 2.05 | 1 | 0 | homodetic cyclic peptide | |
| coenzyme q10 coenzyme Q10: Ubiquinone ring with a chain of 10 isoprene units; redox equilibrium with ubiqunol serving in mitochondrial inner membrane to transfer electrons; presence during reconstitution of acetylcholine receptor into phospholipid vesicles yields vesicles active in catalyzing carbamylcholine-sensitive Na+ flux; coenzyme Q10 depletion has been noted with use of statins. coenzyme Q10 : A ubiquinone having a side chain of 10 isoprenoid units. In the naturally occurring isomer, all isoprenyl double bonds are in the E- configuration. | 2.05 | 1 | 0 | ubiquinones | antioxidant; ferroptosis inhibitor; human metabolite |
| tranilast tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis. tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group. | 2.05 | 1 | 0 | amidobenzoic acid; cinnamamides; dimethoxybenzene; secondary carboxamide | anti-allergic agent; anti-asthmatic drug; antineoplastic agent; aryl hydrocarbon receptor agonist; calcium channel blocker; hepatoprotective agent; nephroprotective agent |
| etretinate retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof. | 2.05 | 1 | 0 | enoate ester; ethyl ester; retinoid | keratolytic drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 2.05 | 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. | 2.05 | 1 | 0 | ||
| ozagrel ozagrel: RN refers to (E)-isomer | 2.05 | 1 | 0 | cinnamic acids | |
| 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. | 2.05 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| alatrofloxacin mesylate [no description available] | 2.05 | 1 | 0 | ||
| codeine [no description available] | 2.05 | 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 | 2.05 | 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 |
| natamycin [no description available] | 2.05 | 1 | 0 | antibiotic antifungal drug; dicarboxylic acid monoester; epoxide; macrolide antibiotic; monosaccharide derivative; polyene antibiotic | antifungal agrochemical; antimicrobial food preservative; apoptosis inducer; bacterial metabolite; ophthalmology drug |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 2.05 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| dothiepin [no description available] | 2.05 | 1 | 0 | dothiepin | |
| 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. | 2.05 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| nalorphine Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete. | 2.05 | 1 | 0 | morphinane alkaloid | |
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 2.05 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) | 2.05 | 1 | 0 | morphinane alkaloid | |
| 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. | 2.05 | 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. | 2.05 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| alvocidib alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation. | 2.05 | 1 | 0 | dihydroxyflavone; hydroxypiperidine; monochlorobenzenes; tertiary amino compound | antineoplastic agent; antirheumatic drug; apoptosis inducer; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor |
| seocalcitol seocalcitol: structure given in first source | 2.05 | 1 | 0 | ||
| fenretinide Fenretinide: A synthetic retinoid that is used orally as a chemopreventive against prostate cancer and in women at risk of developing contralateral breast cancer. It is also effective as an antineoplastic agent.. 4-hydroxyphenyl retinamide : A retinoid obtained by formal condensation of the carboxy group of all-trans retinoic acid and the anilino group of 4-hydroxyaniline. Synthetic retinoid agonist. Antiproliferative, antioxidant and anticancer agent with a long half-life in vivo. Apoptotic effects appear to be mediated by a mechanism distinct from that of 'classical' retinoids. | 2.05 | 1 | 0 | monocarboxylic acid amide; retinoid | antineoplastic agent; antioxidant |
| geldanamycin [no description available] | 2.05 | 1 | 0 | 1,4-benzoquinones; ansamycin; carbamate ester; organic heterobicyclic compound | antimicrobial agent; antineoplastic agent; antiviral agent; cysteine protease inhibitor; Hsp90 inhibitor |
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 2.05 | 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 |
| demycarosylturimycin h [no description available] | 2.05 | 1 | 0 | ||
| iloprost Iloprost: An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of EPOPROSTENOL, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation.. iloprost : A carbobicyclic compound that is prostaglandin I2 in which the endocyclic oxygen is replaced by a methylene group and in which the (1E,3S)-3-hydroxyoct-1-en-1-yl side chain is replaced by a (3R)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl group. A synthetic analogue of prostacyclin, it is used as the trometamol salt (generally by intravenous infusion) for the treatment of peripheral vascular disease and pulmonary hypertension. | 2.05 | 1 | 0 | carbobicyclic compound; monocarboxylic acid; secondary alcohol | platelet aggregation inhibitor; vasodilator agent |
| seglitide seglitide: more potent than somatostatin for inhibition of insulin, glucagon & growth hormone release; used experimentally in treatment of Alzheimer's disease; somatostatin receptor antagonist | 2.4 | 2 | 0 | ||
| vinorelbine [no description available] | 2.05 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| furazolidone [no description available] | 2.05 | 1 | 0 | ||
| fluvoxamine Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder. | 2.05 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| semaxinib semaxanib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is replaced by a 3,5-dimethylpyrrol-2-yl group. | 2.05 | 1 | 0 | olefinic compound; oxindoles; pyrroles | angiogenesis modulating agent; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist |
| orantinib orantinib: an antiangiogenic agent. orantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1. | 2.05 | 1 | 0 | ||
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 2.05 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| molsidomine [no description available] | 2.05 | 1 | 0 | ethyl ester; morpholines; oxadiazole; zwitterion | antioxidant; apoptosis inhibitor; cardioprotective agent; nitric oxide donor; vasodilator agent |
| 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. | 2.05 | 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. | 2.05 | 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 |
| cefixime [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 2.05 | 1 | 0 | azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester | bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug |
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 2.05 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration). | 2.05 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| nitrofurazone Nitrofurazone: A topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial WOUNDS AND INJURIES and skin infections. Nitrofurazone has also been administered orally in the treatment of TRYPANOSOMIASIS.. nitrofurazone : A semicarbazone resulting from the formal condensation of semicarbazide with 5-nitrofuraldehyde. A broad spectrum antibacterial drug, although with little activity against Pseudomonas species, it is used as a local application for burns, ulcers, wounds and skin infections. | 2.05 | 1 | 0 | ||
| bleomycin [no description available] | 2.05 | 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. | 2.05 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| imidapril imidapril: structure given in first source. imidapril : A member of the class of imidazolidines that is (4S)-1-methyl-2-oxoimidazolidine-4-carboxylic acid in which the hydrogen of the imidazolidine nitrogen has been substituted by (1S)-1-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}ethyl group. It is the prodrug for imidaprilat, an ACE inhibitor used for the treatment of chronic heart failure. | 2.05 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; imidazolidines; N-acylurea; secondary amino compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| sulindac sulfone sulindac sulfone: inhibits K-ras-dependent cyclooxygenase-2; sulfated analog of indomethacin;; CP248 is an antineoplastic agent that fosters microtubule depolymerization; structure in first source. sulindac sulfone : A sulfone metabolite of sulindac that inhibits cell growth by inducing apoptosis independently of cyclooxygenase inhibition. It inhibits the development and induces regression of premalignant adenomatous polyps. Lipoxygenase and Cox-2 inhibitor. | 2.05 | 1 | 0 | monocarboxylic acid; organofluorine compound; sulfone | apoptosis inducer; cyclooxygenase 2 inhibitor; EC 1.13.11.34 (arachidonate 5-lipoxygenase) 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. | 2.05 | 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 |
| ceftriaxone [no description available] | 2.05 | 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 |
| 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. | 2.05 | 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 |
| guanabenz acetate [no description available] | 2.05 | 1 | 0 | dichlorobenzene | geroprotector |
| famotidine [no description available] | 2.05 | 1 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cefotaxime Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups. | 2.05 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 2.05 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| proguanil Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells. | 2.05 | 1 | 0 | biguanides; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| rifamycin sv rifamycin SV: RN given refers to parent cpd; structure in Merck Index, 9th ed, #8009. rifamycin SV : A member of the class of rifamycins that exhibits antibiotic and antitubercular properties. | 2.05 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterotetracyclic compound; polyphenol; rifamycins | antimicrobial agent; antitubercular agent; bacterial metabolite |
| epoprostenol sodium [no description available] | 2.05 | 1 | 0 | prostanoid | |
| ixabepilone [no description available] | 2.05 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| azlocillin Azlocillin: A semisynthetic ampicillin-derived acylureido penicillin.. azlocillin : A semisynthetic penicillin having a 6beta-{(2R)-2-[(2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl}amino side-group. It is an antibiotic used in treating infections caused by Pseudomonas aeruginosa, Escherichia coli and Haemophilus influenzae. | 2.05 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial drug |
| dantrolene sodium dantrolene sodium (anhydrous) : The anhydrous sodium salt of dantrolene. | 2.05 | 1 | 0 | ||
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 2.05 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| nifurtimox Nifurtimox: A nitrofuran thiazine that has been used against TRYPANOSOMIASIS. | 2.05 | 1 | 0 | nitrofuran antibiotic | |
| roxithromycin (E)-roxithromycin : A major geometrical isomer of roxithromycin. | 2.05 | 1 | 0 | roxithromycin | environmental contaminant; xenobiotic |
| beraprost beraprost: stable prostacyclin analog; structure given in first source. beraprost : An organic heterotricyclic compound that is (3aS,8bS)-2,3,3a,8b-tetrahydro-1H-benzo[b]cyclopenta[d]furan in which the hydrogens at positions 1R, 2R and 5 are replaced by (3S)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl, hydroxy and 3-carboxypropyl groups, respectively. It is a prostaglandin receptor agonist which is approved to treat pulmonary arterial hypertension in Asia. | 2.05 | 1 | 0 | enyne; monocarboxylic acid; organic heterotricyclic compound; secondary alcohol; secondary allylic alcohol | anti-inflammatory agent; antihypertensive agent; platelet aggregation inhibitor; prostaglandin receptor agonist; vasodilator agent |
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 2.05 | 1 | 0 | diarylmethane | |
| acetylcarnitine O-acetyl-L-carnitine : An O-acyl-L-carnitine where the acyl group specified is acetyl. It facilitates movement of acetyl-CoA into the matrices of mammalian mitochondria during the oxidation of fatty acids. | 2.05 | 1 | 0 | O-acetylcarnitine; saturated fatty acyl-L-carnitine | human metabolite; Saccharomyces cerevisiae metabolite |
| nifurtoinol nifurtoinol : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group and at position 3 by a hydroxymethyl group. | 2.05 | 1 | 0 | hydrazone; imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| fosinopril [no description available] | 2.05 | 1 | 0 | ||
| eflucimibe eflucimibe: a powerful and systemic acylcoenzyme A: cholesterol acyltransferase inhibitor | 2.05 | 1 | 0 | ||
| etomoxir [no description available] | 2.05 | 1 | 0 | aromatic ether | |
| pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. | 2.05 | 1 | 0 | organic molecular entity | |
| gentamicin sulfate [no description available] | 2.05 | 1 | 0 | ||
| l 363301 [no description available] | 2.4 | 2 | 0 | ||
| pasireotide pasireotide : A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing's disease. | 2.01 | 1 | 0 | homodetic cyclic peptide; peptide hormone | antineoplastic agent |
| bim 23052 [no description available] | 1.98 | 1 | 0 | ||
| azd 6244 AZD 6244: a MEK inhibitor | 2.05 | 1 | 0 | benzimidazoles; bromobenzenes; hydroxamic acid ester; monochlorobenzenes; organofluorine compound; secondary amino compound | anticoronaviral agent; antineoplastic agent; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor |
| vinflunine vinflunine: inhibits tubulin assembly; structure in first source. vinflunine : An organic heteropentacyclic compound and an organic heterotetracyclic compound that is vinorelbine in which the tetrahydropyridine moiety of the heterotetracyclic part of the molecule has been redced to the corresponding piperidine, and in which the ethyl group attached to this ring has been replaced by a 1,1-difluoroethyl group. | 2.05 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; semisynthetic derivative; vinca alkaloid | antineoplastic agent |
| baci-im [no description available] | 2.05 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| pf 03491390 [no description available] | 2.05 | 1 | 0 | ||
| amodiaquine hydrochloride [no description available] | 2.05 | 1 | 0 | ||
| somatostatin [no description available] | 2.01 | 1 | 0 | heterodetic cyclic peptide; peptide hormone | |
| tannins gallotannin : A class of hydrolysable tannins obtained by condensation of the carboxy group of gallic acid (and its polymeric derivatives) with the hydroxy groups of a monosaccharide (most commonly glucose). | 2.05 | 1 | 0 | tannin | |
| bim 23056 [no description available] | 1.98 | 1 | 0 | ||
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 2.05 | 1 | 0 | organosulfonic acid | |
| cerivastatin sodium cerivastatin sodium : The sodium salt of cerivastatin. Formerly used to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity. | 2.05 | 1 | 0 | organic sodium salt; statin (synthetic) | |
| monensin [no description available] | 2.05 | 1 | 0 | ||
| oxacillin sodium [no description available] | 2.05 | 1 | 0 | organic sodium salt | |
| sodium diatrizoate histopaque: used for separating mononuclear & other cells. sodium amidotrizoate : The sodium salt of a benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, often as a mixture with the meglumine salt, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 2.05 | 1 | 0 | organic sodium salt; organoiodine compound | radioopaque medium |
| ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms. | 2.05 | 1 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| novobiocin Novobiocin: An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189). novobiocin : A coumarin-derived antibiotic obtained from Streptomyces niveus. | 2.05 | 1 | 0 | carbamate ester; ether; hexoside; hydroxycoumarin; monocarboxylic acid amide; monosaccharide derivative; phenols | antibacterial agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; Escherichia coli metabolite; hepatoprotective agent |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 2.05 | 1 | 0 | ||
| chlortetracycline Chlortetracycline: A TETRACYCLINE with a 7-chloro substitution.. chlortetracycline : A member of the class of tetracyclines with formula C22H23ClN2O8 isolated from Streptomyces aureofaciens. | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | ||
| dicumarol Dicumarol: An oral anticoagulant that interferes with the metabolism of vitamin K. It is also used in biochemical experiments as an inhibitor of reductases. | 2.05 | 1 | 0 | hydroxycoumarin | anticoagulant; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor; Hsp90 inhibitor; vitamin K antagonist |
| piroxicam [no description available] | 2.05 | 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 |
| acenocoumarol Acenocoumarol: A coumarin that is used as an anticoagulant. Its actions and uses are similar to those of WARFARIN. (From Martindale, The Extra Pharmacopoeia, 30th ed, p233). acenocoumarol : A hydroxycoumarin that is warfarin in which the hydrogen at position 4 of the phenyl substituent is replaced by a nitro group. | 2.05 | 1 | 0 | C-nitro compound; hydroxycoumarin; methyl ketone | anticoagulant; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 2.05 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| mobiflex tenoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain and inflammation in osteoarthritis and rheumatoid arthritis. It is also indicated for short term treatment of acute musculoskeletal disorders including strains, sprains and other soft-tissue injuries. | 2.05 | 1 | 0 | heteroaryl hydroxy compound; monocarboxylic acid amide; pyridines; thienothiazine | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group. | 2.05 | 1 | 0 | benzenes; hydroxycoumarin; methyl ketone | |
| phenprocoumon Phenprocoumon: Coumarin derivative that acts as a long acting oral anticoagulant.. phenprocoumon : A hydroxycoumarin that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenylpropyl group. | 2.05 | 1 | 0 | hydroxycoumarin | anticoagulant; EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor |
| rolitetracycline Rolitetracycline: A pyrrolidinylmethyl TETRACYCLINE.. rolitetracycline : A derivative of tetracycline in which the amide function is substituted with a pyrrolidinomethyl group. | 2.05 | 1 | 0 | ||
| lornoxicam lornoxicam : A thienothiazine-derived monocarboxylic acid amide obtained by formal condensation of the carboxy group of 6-chloro-4-hydroxy-2-methylthieno[2,3-e][1,2]thiazine-3-carboxylic acid 1,1-dioxide with the amino group of 2-aminopyridine. Used for the treatment of pain, primarily resulting from inflammatory diseases of the joints, osteoarthritis, surgery, sciatica and other inflammations. | 2.05 | 1 | 0 | heteroaryl hydroxy compound; monocarboxylic acid amide; organochlorine compound; pyridines; thienothiazine | antipyretic; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| ajmaline [no description available] | 2.05 | 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. | 2.05 | 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. | 2.05 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| inosine [no description available] | 2.05 | 1 | 0 | inosines; purines D-ribonucleoside | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin. | 2.05 | 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) | 2.05 | 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. | 2.05 | 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. | 2.05 | 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. | 2.05 | 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] | 2.05 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | 2.05 | 1 | 0 | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. | 2.05 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| penciclovir penciclovir : A member of the class of 2-aminopurines that is guanine in which the hydrogen at position 9 is substituted by a 4-hydroxy-3-(hydroxymethyl)but-1-yl group. An antiviral drug, it is administered topically for treatment of herpes labialis. A prodrug, famciclovir, is used for oral administration. | 2.05 | 1 | 0 | 2-aminopurines; propane-1,3-diols | antiviral drug |
| oxypurinol Oxypurinol: A xanthine oxidase inhibitor.. alloxanthine : A pyrazolopyrimidine that is 4,5,6,7-tetrahydro-H-pyrazolo[3,4-d]pyrimidine substituted by oxo groups at positions 4 and 6. | 2.05 | 1 | 0 | pyrazolopyrimidine | drug metabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor |
| raltitrexed [no description available] | 2.05 | 1 | 0 | N-acyl-amino acid | |
| allopurinol Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. | 2.05 | 1 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 2.05 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| alanosine [no description available] | 2.05 | 1 | 0 | ||
| tirapazamine Tirapazamine: A triazine derivative that introduces breaks into DNA strands in hypoxic cells, sensitizing tumor cells to the cytotoxic activity of other drugs and radiation.. tirapazamine : A member of the class of benzotriazines that is 1,2,4-benzotriazine carrying an amino substituent at position 3 and two oxido substituents at positions 1 and 4. | 2.05 | 1 | 0 | aromatic amine; benzotriazines; N-oxide | antibacterial agent; antineoplastic agent; apoptosis inducer |
| rifabutin [no description available] | 2.05 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 2.46 | 2 | 0 |
| 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 | 2.46 | 2 | 0 |
| Adverse Drug Event [description not available] | 0 | 2.06 | 1 | 0 |
| Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals. | 0 | 2.06 | 1 | 0 |