| ID Source | ID |
|---|---|
| PubMed CID | 383414 |
| CHEMBL ID | 262746 |
| SCHEMBL ID | 678434 |
| MeSH ID | M0023526 |
| PubMed CID | 448601 |
| CHEMBL ID | 1680 |
| CHEBI ID | 7726 |
| SCHEMBL ID | 10044649 |
| MeSH ID | M0023526 |
| Synonym |
|---|
| LS-15492 |
| gtpl2055 |
| sms 201,995 |
| 10-(4-aminobutyl)-19-[(2-amino-3-phenylpropanoyl)amino]-n-(1,3-dihydroxybutan-2-yl)-7-(1-hydroxyethyl)-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-16-(phenylmethyl)-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide |
| NCI60_025753 |
| C07306 |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l- threonyl-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)propyl)-l- cysteinamide cyclic (2->7)-disulfide |
| 83150-76-9 |
| octreotide (usan/inn) |
| D00442 |
| (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-n-[(2r,3r)-1,3-dihydroxybutan-2-yl]-7-[(1r)-1-hydroxyethyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxa |
| L000453 |
| (4r,7s,10s,13r,16s,19r)-10-(4-aminobutyl)-19-[[(2r)-2-amino-3-phenyl-propanoyl]amino]-16-benzyl-7-[(1r)-1-hydroxyethyl]-n-[(1r,2r)-2-hydroxy-1-(hydroxymethyl)propyl]-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosan |
| A840511 |
| CHEMBL262746 |
| FT-0630918 |
| 10-(4-aminobutyl)-16-benzyl-n-(1,3-dihydroxybutan-2-yl)-7-(1-hydroxyethyl)-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-(phenylalanylamino)-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxam |
| STL483734 |
| SCHEMBL678434 |
| AKOS026750549 |
| BCP28870 |
| octreotide acetate; longastatin; sms-201-995; octreotide-lar; sms 201-995 |
| Q27088142 |
| 1240797-41-4 |
| octreotide-phenylalanine-d8;sandostatin-d8; sandostatin lar-d8 |
| octreotide d8 |
| BCP31200 |
| NCGC00379009-01 |
| sms 201-995 |
| l-cysteinamide, d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l- threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic (2->7)-disulfide, (r-(r*,r*))- |
| sms-995 |
| octrotide |
| DB00104 |
| octreotida [spanish] |
| sms-201-995 |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)propyl)-l-cysteinamide cyclic (2-7)-disulfide |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-l-cysteinyl-l-threoninol cyclic (2-7)-disulfide |
| octreotide [usan:inn:ban] |
| drg-0115 |
| octreotidum [latin] |
| l-cysteinamide, d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic (2-7)-disulfide, (r-(r*,r*))- |
| HMS2090C09 |
| bdbm50272772 |
| 2-{[(13r,16s,19r)-10-(4-amino-butyl)-19-((s)-2-amino-3-phenyl-propionylamino)-16-benzyl-7-(1-hydroxy-ethyl)-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-amino}-3-hydroxy-butyric acid |
| 10-(4-amino-butyl)-19-(2-amino-3-phenyl-propionylamino)-16-benzyl-7-(1-hydroxy-ethyl)-13-(1h-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carboxylic acid (2-hydroxy-1- |
| CHEMBL1680 , |
| sms995 |
| octreotide-lar |
| rwm8ccw8gp , |
| octreotida |
| octreotidum |
| unii-rwm8ccw8gp |
| dtxcid6028608 |
| dtxsid0048682 , |
| AKOS015994656 |
| octreotide [who-dd] |
| octreotide [ep monograph] |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-((1r,2r)-2-hydroxy-1-(hydroxymethyl)propyl)-l-cysteinamide cyclic (2->7)-disulfide |
| l-cysteinamide, d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic (2->7)-disulfide, (r-(r*,r*))- |
| octreotide [mi] |
| octreotide [inn] |
| octreotide [usan] |
| d-phenylalanyl-l-hemicystyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-l-hemicystyl-l-threoninol cyclic (2->7)-disulfide |
| octreotide [vandf] |
| HS-2020 , |
| DEQANNDTNATYII-OULOTJBUSA-N |
| AB01275486-01 |
| CHEBI:7726 , |
| SCHEMBL10044649 |
| Q-201501 |
| AC-28733 |
| mfcd00871400 |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-l-cysteinyl-l-threoninol cyclic (2->7)-disulfide |
| octreotide, >=98% (hplc) |
| (4r,7s,10s,13r,16s,19r)-13-((1h-indol-3-yl)methyl)-19-((r)-2-amino-3-phenylpropanamido)-10-(4-aminobutyl)-16-benzyl-n-((2r,3r)-1,3-dihydroxybutan-2-yl)-7-((r)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide |
| Q419935 |
| 83150-76-9 (free base) |
| CCG-270610 |
| EX-A4865 |
| octreotode acetate |
| [r-(r*,r*)]-d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-[2-hydroxy-1-(hydroxy-methyl)propyl]-cysteinamide cyclic(2-->7)-disulfide |
| octreotide crs |
| octreotide (ep monograph) |
| d-phenylalanyl-l-cysteinyl-l-phenylalanyl-d-tryptophyl-l-lysyl-l-threonyl-n-((1r,2r)-2-hydroxy-1-(hyroxymethyl)propyl)-l-cysteinamide, cyclic (2->7)-disulfide |
| h01cb02 |
| octreotidum (latin) |
| d-phenylalanyl-l-cysteinyl-l-phenyl-alanyl-d-tryptophyl-l-lysyl-l-threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl)-l-cysteinamide cyclic (2->7)-disulfide |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Somatostatin receptor type 2 | Homo sapiens (human) | Ki | 0.0004 | 0.0000 | 0.4091 | 4.7200 | AID1571190 |
| Somatostatin receptor type 4 | Homo sapiens (human) | IC50 (µMol) | 1.0000 | 0.0001 | 0.0021 | 0.0042 | AID1533639 |
| Somatostatin receptor type 4 | Homo sapiens (human) | Ki | 0.0660 | 0.0006 | 0.2733 | 3.2000 | AID1571189 |
| Somatostatin receptor type 5 | Homo sapiens (human) | IC50 (µMol) | 0.0220 | 0.0002 | 0.0472 | 0.3930 | AID1533640 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Somatostatin receptor type 2 | Homo sapiens (human) | EC50 (µMol) | 0.0000 | 0.0000 | 0.0008 | 0.0023 | AID1781889 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein binding | Somatostatin receptor type 2 | Homo sapiens (human) |
| PDZ domain binding | Somatostatin receptor type 2 | Homo sapiens (human) |
| somatostatin receptor activity | Somatostatin receptor type 2 | Homo sapiens (human) |
| neuropeptide binding | Somatostatin receptor type 2 | Homo sapiens (human) |
| protein binding | Somatostatin receptor type 4 | Homo sapiens (human) |
| somatostatin receptor activity | Somatostatin receptor type 4 | Homo sapiens (human) |
| neuropeptide binding | Somatostatin receptor type 4 | Homo sapiens (human) |
| protein binding | Somatostatin receptor type 5 | Homo sapiens (human) |
| neuropeptide binding | Somatostatin receptor type 5 | Homo sapiens (human) |
| somatostatin receptor activity | Somatostatin receptor type 5 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytosol | Somatostatin receptor type 2 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 2 | Homo sapiens (human) |
| neuron projection | Somatostatin receptor type 2 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 2 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 4 | Homo sapiens (human) |
| neuron projection | Somatostatin receptor type 4 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 4 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 5 | Homo sapiens (human) |
| plasma membrane | Somatostatin receptor type 5 | Homo sapiens (human) |
| neuron projection | Somatostatin receptor type 5 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Nov, Volume: 360, Issue:5 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1994 | Endocrinology, Dec, Volume: 135, Issue:6 | Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). |
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1994 | Endocrinology, Dec, Volume: 135, Issue:6 | Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). |
| AID1346419 | Rat SST2 receptor (Somatostatin receptors) | 1998 | Reviews of physiology, biochemistry and pharmacology, , Volume: 133 | The elucidation of somatostatin receptor functions: a current view. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Nov, Volume: 360, Issue:5 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1998 | European journal of pharmacology, May-08, Volume: 348, Issue:2-3 | [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. |
| AID1346420 | Rat SST5 receptor (Somatostatin receptors) | 1998 | Reviews of physiology, biochemistry and pharmacology, , Volume: 133 | The elucidation of somatostatin receptor functions: a current view. |
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1996 | Metabolism: clinical and experimental, Aug, Volume: 45, Issue:8 Suppl 1 | Binding properties of somatostatin receptor subtypes. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1998 | Proceedings of the National Academy of Sciences of the United States of America, Sep-01, Volume: 95, Issue:18 | Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. |
| AID1346311 | Mouse SST2 receptor (Somatostatin receptors) | 1998 | Reviews of physiology, biochemistry and pharmacology, , Volume: 133 | The elucidation of somatostatin receptor functions: a current view. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1996 | Metabolism: clinical and experimental, Aug, Volume: 45, Issue:8 Suppl 1 | Binding properties of somatostatin receptor subtypes. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1999 | Naunyn-Schmiedeberg's archives of pharmacology, Nov, Volume: 360, Issue:5 | Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, May, Volume: 357, Issue:5 | [125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1998 | European journal of pharmacology, May-08, Volume: 348, Issue:2-3 | [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. |
| AID1346424 | Human SST2 receptor (Somatostatin receptors) | 1996 | Metabolism: clinical and experimental, Aug, Volume: 45, Issue:8 Suppl 1 | Binding properties of somatostatin receptor subtypes. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1998 | Reviews of physiology, biochemistry and pharmacology, , Volume: 133 | The elucidation of somatostatin receptor functions: a current view. |
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1993 | FEBS letters, Apr-26, Volume: 321, Issue:2-3 | A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1998 | Proceedings of the National Academy of Sciences of the United States of America, Sep-01, Volume: 95, Issue:18 | Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. |
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, May, Volume: 357, Issue:5 | [125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
| AID1346397 | Mouse SST5 receptor (Somatostatin receptors) | 2000 | Neuropharmacology, Jun-08, Volume: 39, Issue:8 | Cloning, expression and pharmacological characterisation of the mouse somatostatin sst(5) receptor. |
| AID1346332 | Human SST3 receptor (Somatostatin receptors) | 1998 | Proceedings of the National Academy of Sciences of the United States of America, Sep-01, Volume: 95, Issue:18 | Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1998 | Naunyn-Schmiedeberg's archives of pharmacology, May, Volume: 357, Issue:5 | [125I]Tyr10-cortistatin14 labels all five somatostatin receptors. |
| AID1346321 | Rat SST3 receptor (Somatostatin receptors) | 1998 | Reviews of physiology, biochemistry and pharmacology, , Volume: 133 | The elucidation of somatostatin receptor functions: a current view. |
| AID1346404 | Mouse SST3 receptor (Somatostatin receptors) | 1993 | Molecular pharmacology, Jun, Volume: 43, Issue:6 | Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. |
| AID1346413 | Human SST5 receptor (Somatostatin receptors) | 1994 | Endocrinology, Dec, Volume: 135, Issue:6 | Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5). |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1533639 | Inhibition of human SSTR4 by radioligand binding assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Ligand design for somatostatin receptor isoforms 4 and 5. |
| AID1571189 | Binding affinity to human SST4 receptor | |||
| AID1381540 | Agonist activity at SSTR5 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced CRE promoter activity at 10 to 1000 nM by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | New somatostatin-drug conjugates for effective targeting pancreatic cancer. |
| AID1882821 | Stability of the compound in simulated gastric fluid at pH 1.2 assessed as half life measured up to 24 hrs by RP-HPLC-UV analysis | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 | On the Utility of Chemical Strategies to Improve Peptide Gut Stability. |
| AID1381538 | Agonist activity at SSTR3 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced CRE promoter activity at 10 to 1000 nM by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | New somatostatin-drug conjugates for effective targeting pancreatic cancer. |
| AID1882822 | Stability of the compound in simulated intestinal fluid at pH 6.8 assessed as half life measured up to 24 hrs by RP-HPLC-UV analysis | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 | On the Utility of Chemical Strategies to Improve Peptide Gut Stability. |
| AID1781889 | Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay | 2021 | Bioorganic & medicinal chemistry, 11-01, Volume: 49 | Design, synthesis, and biological evaluation of novel somatostatin receptor subtype-2 agonists: Optimization for potency and risk mitigation of hERG and phospholipidosis. |
| AID1533640 | Inhibition of human SSTR5 by radioligand binding assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Ligand design for somatostatin receptor isoforms 4 and 5. |
| AID1381537 | Agonist activity at SSTR2 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced CRE promoter activity at 10 to 1000 nM by luciferase reporter gene assay | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | New somatostatin-drug conjugates for effective targeting pancreatic cancer. |
| AID1571190 | Binding affinity to human SST2 receptor | |||
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [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 | 9 (52.94) | 18.2507 |
| 2000's | 1 (5.88) | 29.6817 |
| 2010's | 4 (23.53) | 24.3611 |
| 2020's | 3 (17.65) | 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 (104.57) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (20.00%) | 6.00% |
| Reviews | 1 (14.29%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 8 (80.00%) | 84.16% |
| Other | 6 (85.71%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Double-blind Randomised Placebo-controlled Feasibility Study to Assess the Impact of Octreotide Infusion During Liver Transplantation on Post-operative Renal Failure. [NCT04941911] | Phase 2 | 30 participants (Actual) | Interventional | 2022-05-27 | Active, not recruiting | ||
| Everolimus Added to Long Acting Octreotide as a Volume Reducing Treatment of Polycystic Livers [NCT01157858] | Phase 2 | 44 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| Randomized Controlled Trial on Role of Octreotide in Preventing Pancreatic Fistula and Complications After Pancreaticoduodenectomy in Patients With Soft Pancreas [NCT01301222] | Phase 4 | 110 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| Continuing Somatostatin Analogues Upon Progression in Neuroendocrine Tumour pAtients - The SAUNA Trial [NCT05701241] | Phase 4 | 270 participants (Anticipated) | Interventional | 2023-06-28 | Recruiting | ||
| Al18F-NOTA-octreotide PET Imaging of the Somatostatin Receptor in Neuroendocrine Tumors: a First-in-human PET/CT Study [NCT03883776] | Phase 1 | 12 participants (Actual) | Interventional | 2019-04-11 | Completed | ||
| [NCT01587222] | Phase 2 | 0 participants (Actual) | Interventional | 2016-07-31 | Withdrawn(stopped due to the sponsor did not provide the treatment) | ||
| Terlipressin Versus Somatostatin/Octreotide on Effect of Renal Function in Cirrhotic Patients With Acute Gastrointestinal Hemorrhage (TORCH): A Retrospective Multicenter Observational Study [NCT03846180] | 1,682 participants (Actual) | Observational | 2019-03-01 | Completed | |||
| Phase II Study of the Combination of Bevacizumab Plus Somatostatin Analogue and Metronomic Capecitabine in Patients With Advanced Inoperable Well-Differentiated Neuroendocrine Tumors [NCT01203306] | Phase 2 | 42 participants (Anticipated) | Interventional | 2006-01-31 | Recruiting | ||
| Phase I Study of Anti-IGF-1R Monoclonal Antibody, IMC-A12, and mTOR Inhibitor, Everolimus, in Advanced Low to Intermediate Grade Neuroendocrine Carcinoma [NCT01204476] | Phase 1 | 27 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| A Phase 1 Study of the Safety and Pharmacokinetics of Single Doses of Octreotide Administered Orally Via the RaniPill™ Capsule in Healthy Subjects [NCT03798912] | Phase 1 | 62 participants (Actual) | Interventional | 2019-07-09 | Completed | ||
| A Phase II Study on Everolimus, an mTOR Inhibitor (Oral Formulation), With Octreotide LAR® in Adult Patients With Advanced, Non-functioning, Well-differentiated Gastrointestinal Neuroendocrine Tumours (GI NET) [NCT01567488] | Phase 2 | 43 participants (Actual) | Interventional | 2011-06-08 | Completed | ||
| A Randomized, Double-blind, Placebo-Controlled, Four- Part Study to Assess the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of ONO-5788 in Healthy Adult Volunteers [NCT03571594] | Phase 1 | 76 participants (Actual) | Interventional | 2018-06-07 | Terminated(stopped due to The study met a pre-defined protocol study stopping criteria) | ||
| Continuous 5-fluorouracil Infusion Plus Long Acting Octreotide in Advanced Well Differentiated Neuroendocrine Carcinomas. A Phase II Trial of the Piemonte Oncology Network. [NCT00953394] | Phase 2 | 29 participants (Actual) | Interventional | 2002-02-28 | Completed | ||
| Gastrointestinal Nutrient Transit and Enteroendocrine Function After Upper Gastrointestinal Surgery [NCT03734627] | 40 participants (Actual) | Observational | 2016-07-01 | Completed | |||
| The Longitudinal Approach to Acromegaly: A Pattern of Treatment and Comparative Effectiveness Research [NCT03158090] | 1,965 participants (Anticipated) | Observational | 2017-12-15 | Recruiting | |||
| Gallium-68 DOTATOC for Management of Neuroendocrine Tumors [NCT02375464] | 0 participants | Expanded Access | 2015-04-30 | No longer available | |||
| A PROSPECTIVE, RANDOMIZED, DOUBLE-BLIND, PLACEBO CONTROLLED CLINICAL TRIAL TO ASSESS THE EFFECTS OF LONG-ACTING SOMATOSTATIN (OCTREOTIDE LAR) THERAPY ON DISEASE PROGRESSION IN PATIENTS WITH AUTOSOMAL DOMINANT POLYCYSTIC KIDNEY DISEASE AND MODERATE TO SEVE [NCT01377246] | Phase 3 | 100 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
| The Effect of Octreotide on the Duration of Post-mastectomy Wound Drainage: a Randomized Controlled Trial [NCT05682209] | Phase 4 | 41 participants (Actual) | Interventional | 2020-12-18 | Completed | ||
| A Multicentre, Stratified, Open, Randomized, Comparator-controlled, Parallel-group Phase III Study Comparing Treatment With 177Lu-DOTA0-Tyr3-Octreotate to Octreotide LAR in Patients With Inoperable, Progressive, Somatostatin Receptor Positive Midgut Carci [NCT01578239] | Phase 3 | 231 participants (Actual) | Interventional | 2012-09-06 | Completed | ||
| Prophylactic Octreotide to Prevent Post Duodenal EMR and Ampullectomy Bleeding [NCT02032784] | Phase 4 | 33 participants (Actual) | Interventional | 2014-03-31 | Terminated(stopped due to Difficult to enroll subjects) | ||
| 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.) | |||
| A Randomized, Multicenter, Phase II Study to Investigate Efficacy and Safety of ITF2984 in Acromegalic Patients [NCT02111044] | Phase 2 | 48 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
| Selective Intra-arterial Injection of Peptide Receptor Radionuclide Therapy (PRRT) in Neuroendocrine Tumor Patients With Liver Metastases [NCT03724409] | Early Phase 1 | 3 participants (Actual) | Interventional | 2018-10-11 | Terminated(stopped due to Pandemic) | ||
| Adjuvant Use of Autologous Platelet-rich Fibrin Glue in the Treatment of Fistulas and Anastomotic Leakages of the Digestive Tract [NCT01561066] | Phase 1 | 122 participants (Anticipated) | Interventional | 2008-01-31 | Completed | ||
| A Randomized, Double-blind Placebo-controlled, Multicenter Phase III Study in Patients With Advanced Carcinoid Tumor Receiving Octreotide Depot and Everolimus 10 mg/Day or Octreotide Depot and Placebo [NCT00412061] | Phase 3 | 429 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
| A Phase II Clinical and Biologic Study of AMG 706 and Octreotide in Patients With Low-Grade Neuroendocrine Tumors [NCT00427349] | Phase 2 | 46 participants (Actual) | Interventional | 2008-11-07 | Completed | ||
| Investigation of the Developmental, Nutritional and Hormonal Regulation of Ghrelin in Children and Young Adults With Prader-Willi Syndrome (PWS): Octreotide Intervention Sub-study [NCT00399893] | 5 participants (Actual) | Interventional | 2006-12-31 | Terminated(stopped due to Inadequate recruitment) | |||
| Treatment With Octreotide in Patients With Lymphangioleiomyomatosis [NCT00005906] | Phase 2 | 4 participants (Actual) | Interventional | 2000-06-30 | Completed | ||
| 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 | |||
| PANasta Trial Cattell-Warren Versus Blumgart Techniques of Pancreatico-jejunostomy Following Pancreato-duodenectomy - a Double Blinded Multi Centred Trial [NCT02457156] | Phase 3 | 506 participants (Anticipated) | Interventional | 2015-04-30 | Active, not recruiting | ||
| Open Label Study to Evaluate the Pharmacokinetics, Efficacy and Safety of Two Doses of an Octreotide Implant in Patients With Carcinoid Syndrome [NCT00884715] | Phase 1/Phase 2 | 10 participants (Actual) | Interventional | 2009-07-31 | Terminated(stopped due to Program was terminated for business reasons) | ||
| Octreotide for Management of Bronchorrhea in Mechanically Ventilated Patients: A Randomized Controlled Trial [NCT02916433] | Phase 2 | 5 participants (Actual) | Interventional | 2016-09-30 | Completed | ||
| Yttrium-90 DOTA-TOC Intra-arterial (IA) Peptide Receptor Radionuclide Therapy (PRRT) for Neuroendocrine Tumor [NCT03197012] | Early Phase 1 | 10 participants (Actual) | Interventional | 2017-07-01 | Completed | ||
| A Prospective Randomized, Placebo (Saline)-Controlled, Balanced, 3-treatment Regimen Crossover Study Comparing the Effects of Prolonged (13 h) Hyperglucagonemia With Those of Acute (3 hr) Hyperglucagonemia on Energy Expenditure and Endogenous Glucose Prot [NCT02237053] | Phase 1 | 6 participants (Actual) | Interventional | 2014-09-30 | Completed | ||
| Beijing Children's Hospital, Capital Medical University, National Center for Children's Health [NCT05171751] | 50 participants (Actual) | Observational | 2021-11-01 | Completed | |||
| PHASE IIIB, OPEN-LABEL, MULTICENTER STUDY TO EVALUATE THE LONG-TERM SAFETY AND EFFICACY OF AN 84-MG OCTREOTIDE SUBCUTANEOUS HYDROGEL IMPLANT IN SUBJECTS WITH ACROMEGALY [NCT01295060] | Phase 3 | 12 participants (Actual) | Interventional | 2011-02-28 | Terminated(stopped due to Program was terminated for business reasons) | ||
| Hemodynamic Effects of Terlipressin and High Dose Octreotide on Patients With Liver Cirrhosis Related Esophageal Varices: A Randomized, Placebo-controlled Multicenter Trial [NCT02119884] | Phase 4 | 88 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
| Randomized, Open, Positive Control Phase III Clinical Trial of Lutetium (177Lu) Oxodotreotide Injection Combined With Standard-dose Long-acting Octreotide Versus High-dose Long-acting Octreotide in the Treatment of Somatostatin Receptor-positive Advanced [NCT05884255] | Phase 3 | 220 participants (Anticipated) | Interventional | 2023-07-06 | Recruiting | ||
| Activity and Safety of Everolimus in Combination With Octreotide LAR and Metformin in Patients With Advanced Pancreatic Well-differentiated Neuroendocrine Tumors (pWDNETs): a Phase II, Open, Monocentric, Prospective Study [NCT02294006] | Phase 2 | 26 participants (Actual) | Interventional | 2014-06-30 | Active, not recruiting | ||
| Efficacy of 68Ga-DOTATOC Positron Emission Tomography (PET) CT in Children and Young Adults With Brain Tumors [NCT02194452] | 0 participants (Actual) | Interventional | 2013-09-30 | Withdrawn | |||
| Comparative Effectiveness Research: Effects of Terlipressin When Usual Somatostatin or Octreotide Dose Fails to Treat the Patients With Acute Variceal Bleeding [NCT02311608] | 1,320 participants (Anticipated) | Observational | 2014-02-28 | Recruiting | |||
| Studio Esplorativo Monocentrico Non Controllato, in Aperto, Volto a Sviluppare e Valutare l'Applicazione di Una Tecnica Innovativa di Rimozione Radioguidata Dei Tumori Neuroendocrini Gastro-entero-pancreatici [NCT04296149] | Phase 2 | 5 participants (Actual) | Interventional | 2017-02-16 | Completed | ||
| A Phase 2 Open Label Study to Evaluate the Safety and Effectiveness of 212Pb-DOTAMTATE in Subjects With Somatostatin Receptor Expressing Neuroendocrine Tumors [NCT05153772] | Phase 2 | 68 participants (Anticipated) | Interventional | 2021-12-21 | Recruiting | ||
| A Phase III Multi-center, Randomized, Open-label Study to Evaluate the Efficacy and Safety of Lutathera in Patients With Grade 2 and Grade 3 Advanced GEP-NET [NCT03972488] | Phase 3 | 222 participants (Actual) | Interventional | 2020-01-22 | Active, not recruiting | ||
| Phase III Prospective Randomized Comparison of Depot Octreotide Plus Interferon Alpha Versus Depot Octreotide Plus Bevacizumab (NSC #704865) in Advanced, Poor Prognosis Carcinoid Patients [NCT00569127] | Phase 3 | 427 participants (Actual) | Interventional | 2007-12-01 | Active, not recruiting | ||
| A Study of 18F-AlF-NOTA-octreotide PET/CT for Imaging Neuroendocrine Neoplasms [NCT03511768] | Phase 1/Phase 2 | 65 participants (Anticipated) | Interventional | 2018-01-02 | Recruiting | ||
| A Study Comparing Treatment With Lutetium[177Lu] Oxodotreotide Injection to Octreotide LAR in Patients With Inoperable, Progressive, , Well Differentiated， Somatostatin Receptor Positive Gastroenteropancreatic Neuroendocrine Tumours [NCT05459844] | Phase 3 | 196 participants (Anticipated) | Interventional | 2022-08-31 | Recruiting | ||
| Hepatic Hemodynamic Responses to Long-acting Octreotide in Patients With Cirrhosis Hepatic Hemodynamic Responses to Long-acting Octreotide in Patients With Cirrhosis [NCT01188733] | Phase 1/Phase 2 | 39 participants (Actual) | Interventional | 1998-06-30 | Completed | ||
| A Phase 1, Non-Randomized, Open-Label, Dose Escalation, Single-Center Study to Determine the Safety, Bio-distribution, and Preliminary Effectiveness of AlphaMedix™ in Adult Subjects With SSRT(+) NETs. [NCT03466216] | Phase 1 | 33 participants (Anticipated) | Interventional | 2018-02-05 | Recruiting | ||
| An Observational Study Investigating Recurrence Rates of Type I Gastric Neuroendocrine Tumors Treated With Long-acting Somatostatin Analogs [NCT03812939] | 30 participants (Anticipated) | Observational | 2019-01-01 | Recruiting | |||
| "Efficacy of Octreotide in the Prevention of Postoperative Complications After Pancreaticodudenectomy in Patients With Soft Pancreas and Non-dilated Pancreatic Duct: A Prospective Randomized Trial" [NCT02474914] | 104 participants (Actual) | Interventional | 2014-05-31 | Completed | |||
| Impact of Pasireotide on Postoperative Pancreatic Fistulas Following Distal Resections [NCT04281680] | 258 participants (Actual) | Observational | 2014-07-01 | Completed | |||
| Terlipressin + Albumin Versus Midodrine + Octreotide in the Treatment of Hepatorenal Syndrome (HRS): An Open Multicentric Randomized Study [NCT00742339] | Phase 2/Phase 3 | 49 participants (Actual) | Interventional | 2005-05-31 | Terminated(stopped due to Decision of independent monitoring committee: Risk of non-response to treatment significantly higher in midodrine group than in terlipressin group.) | ||
| Comparison of 2 Days Versus 5 Days of Octreotide After Endoscopic Therapy in Preventing Early Esophageal Varices Rebleed: A Randomized Controlled Study [NCT05199038] | Phase 4 | 184 participants (Anticipated) | Interventional | 2022-06-30 | Not yet recruiting | ||
| Effect of Octreotide on Saliva [NCT05340192] | Phase 1 | 4 participants (Actual) | Interventional | 2019-09-24 | Completed | ||
| Does Surgical Debulking Of Pituitary Adenomas Improve Responsiveness To Octreotide LAR In The Treatment Of Acromegaly: An Investigator-Initiated Study [NCT01371643] | Phase 4 | 41 participants (Actual) | Interventional | 2004-04-30 | Completed | ||
| Role of Hyperinsulinemia in NAFLD: Dexamethasone-Pancreatic Clamp Pilot & Feasibility Study [NCT06126354] | Phase 1 | 16 participants (Anticipated) | Interventional | 2023-12-01 | Not yet recruiting | ||
| A Randomized Control Study to Determine the Efficacy and Safety of Combining Hemospray With Medical Standard of Care Treatment in the Management of Acute Variceal Bleeding in Cirrhotic Patients. [NCT03061604] | 105 participants (Actual) | Interventional | 2014-11-30 | Completed | |||
| Phase II Study of RAD001 Plus Octreotide Depot in Patients With Metastatic or Unresectable Low Grade Neuroendocrine Carcinoma (Carcinoid, Islet Cell) [NCT00113360] | Phase 2 | 67 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
| Peptide Receptor Radionuclide Therapy (PRRT) in Tumors With High Expression of Somatostatin Receptors [NCT04790708] | 250 participants (Anticipated) | Interventional | 2018-07-02 | Recruiting | |||
| Randomized Phase II Study of Octreotide LAR as Maintenance Treatment After First-line Chemotherapy for Patients With Unresectable or Metastatic Gastro-entero-pancreatic or Esophageal Neuroendocrine Carcinomas [NCT02409849] | Phase 2 | 92 participants (Anticipated) | Interventional | 2015-04-30 | Not yet recruiting | ||
| A Phase 1, Open-label, Single-center, 2-period, Single Sequence Drug-drug Interaction Study to Evaluate the Effects of Octreotide Acetate Injection (Sandostatin®) on the Pharmacokinetics of Single-dose Telotristat Etiprate in Healthy Male and Female Subje [NCT02195635] | Phase 1 | 24 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
| Real-world Effectiveness of Adjuvant Octreotide Therapy in High Recurrence Risk Patients With Pancreatic Neuroendocrine Tumors [NCT06080204] | 411 participants (Actual) | Interventional | 2008-03-31 | 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 | ||
| Vasoconstrictors as Alternatives to Albumin After Large Volume Paracentesis in Cirrhosis [NCT00108355] | Phase 4 | 29 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Replace Sandostatine® in Three Daily Subcutaneous Injections by a Single Intramuscular Injection of Sandostatine® LP Per Month in Patients With a Diffuse Form of Hyperinsulinism [NCT00987168] | Phase 2 | 10 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
| Ghrelin Suppression by Sandostatin LAR® Depot (Octreotide Acetate for Injectable Suspension) in Patients With Prader-Willi Syndrome [NCT01613495] | 2 participants (Actual) | Interventional | 2005-08-31 | Active, not recruiting | |||
| Multicenter, Randomised Open Trial Comparing the Efficacy of a Medical Treatment With Sandostatin LP 30 mg Performed Before Surgery to a Prime Line transsphenoïdal Surgery in Previously Untreated Acromegalic Patients With Either a Micro or a Macro Pituita [NCT01029275] | 89 participants (Actual) | Interventional | 2005-01-31 | Completed | |||
| Octreotide Improves Human Lymphatic Fluid Transport a Translational Trial [NCT05683444] | Early Phase 1 | 16 participants (Actual) | Interventional | 2020-07-01 | Completed | ||
| A Phase 2, Multicenter, Two Tier Study of IMC-A12 in Combination With Depot Octreotide in Patients With Metastatic, Well or Moderately Differentiated Carcinoid or Islet Cell Carcinoma [NCT00781911] | Phase 2 | 43 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| Phase II Study of Octreotide Treatment of Advanced, Recurrent Thymoma [NCT00003283] | Phase 2 | 38 participants (Anticipated) | Interventional | 1998-10-13 | Completed | ||
| Phase II Study of [90Y-DOTA]-TOC and [177Lu-DOTA]-TOC in Metastasized Neuroendocrine Tumors [NCT00978211] | Phase 2 | 1,499 participants (Actual) | Interventional | 1997-09-30 | Completed | ||
| Efficacy and Safety of High Dose Regimen of Octreotide LAR in Patients With Neuroendocrine Tumors in Progressive Disease: A Phase II, Open, Multicentric Prospective Study [NCT00990535] | Phase 2 | 28 participants (Actual) | Interventional | 2006-01-31 | 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 | ||
| Treatment of Orthostatic Intolerance [NCT00262470] | Phase 1/Phase 2 | 150 participants (Anticipated) | Interventional | 1997-04-30 | Active, not recruiting | ||
| An Open Label, Stratified, Single-arm Phase II Study of Everolimus in Patients With Advanced Pancreatic Neuroendocrine Tumor (NET) After Failure of Cytotoxic Chemotherapy [NCT00363051] | Phase 2 | 160 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
| Effect of Hyperglycemia on Microvascular Perfusion in Healthy Adults [NCT03520569] | Early Phase 1 | 15 participants (Actual) | Interventional | 2019-02-04 | Completed | ||
| Clinical Study of the Use of Yttrium-90 (90Y) and/or Lutecium-177 (177Lu) DOTATATE (DOTA-0-Tyr3-Octreotate) in the Treatment of Disseminated and / or Symptomatic Tumors With Somatostatin Receptor Overexpression [NCT04029428] | Phase 2 | 150 participants (Anticipated) | Interventional | 2004-11-02 | Recruiting | ||
| A Multicenter, Randomized, Blinded Efficacy and Safety Study of Pasireotide LAR vs Octreotide LAR in Patients With Metastatic Carcinoid Tumors Whose Disease-related Symptoms Are Inadequately Controlled by Somatostatin Analogues. [NCT00690430] | Phase 3 | 186 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| An Open-Label Study to Evaluate the Pharmacokinetic and Pharmacodynamic Response of a Hydrated and Non-Hydrated 84mg Octreotide Implant in Patients With Acromegaly [NCT00913055] | Phase 2 | 34 participants (Actual) | Interventional | 2007-02-28 | 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 | |||
| A Phase 3, Randomized, Active Controlled Study to Evaluate Maintenance of Response, Safety and Patient Reported Outcomes in Acromegaly Patients Treated With Octreotide Capsules vs. Parenteral Somatostatin Receptor Ligands [NCT02685709] | Phase 3 | 146 participants (Actual) | Interventional | 2016-02-29 | Completed | ||
| Angiotensin 2 as a Novel Treatment for Hepatorenal Syndrome [NCT04048707] | Phase 2 | 48 participants (Anticipated) | Interventional | 2021-07-01 | Not yet recruiting | ||
| Safety and Biological Activity of a New Prolonged Release Formulation of Octreotide Acetate, C2l-OCT-01 PR, Administered Intra Muscularly Every 4, 5 or 6 Weeks in Acromegalic Patients [NCT00642421] | Phase 3 | 40 participants (Anticipated) | Interventional | 2008-02-29 | Terminated(stopped due to Commercial reasons) | ||
| Randomized Trial of High-Dose Versus Conventional Dose Octreotide Acetate Versus Loperamide in the Treatment of Chemotherpay-Related Diarrhea in Patients With Colorectal Cancer [NCT00003057] | Phase 3 | 500 participants (Anticipated) | Interventional | 1997-03-26 | Completed | ||
| LARCID: Evaluation of Octreotide LAR in Prevention of Chemotherapy-induced Diarrhea [NCT00582426] | Phase 3 | 139 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| Comparison of Octreotide and Standard Therapy vs. Standard Therapy Alone for the Treatment of Hypoglycemia in Patients Taking Sulfonylureas or a Combination of Insulin and Sulfonylureas Presenting to the Emergency Department [NCT00804297] | Phase 3 | 40 participants | Interventional | 2005-06-30 | Completed | ||
| Food Intake and Gut Hormone Release in Patients in Cancer Remission Who Have Undergone Upper Gastrointestinal Surgery [NCT02385617] | 20 participants (Actual) | Interventional | 2014-01-31 | Completed | |||
| A Randomised, Open-label, Multicenter Study Comparing the Efficacy and Safety of Medical Treatment With Octreotide Acetate 30 mg Administered Every 21 Days for 6 Months With That of Octreotide Acetate 60 mg Administered Every 28 Days for 6 Months in Acrom [NCT00372697] | Phase 3 | 28 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
| Changes in Pancreatic Texture After Single-shot Administration of 500 µg Octreotide in the Gastroduodenal Artery During Pancreatoduodenectomy - a Double-Blinded Randomized Controlled Trial [NCT01400100] | 26 participants (Actual) | Interventional | 2011-08-31 | Completed | |||
| Investigation of the Effects of Obesity Surgery on Appetitive Behaviour - Impact of Gut Hormones [NCT02010385] | 30 participants (Actual) | Interventional | 2013-02-28 | Completed | |||
| An Uncontrolled, Pilot-study Assessing the Efficacy of Octreotide Long-acting Release to Decrease Transfusion Requirements and Endoscopy Frequency in Patients With Rendu-Osler-Weber and Gastrointestinal Bleeding [NCT02874326] | Phase 2 | 15 participants (Anticipated) | Interventional | 2016-10-31 | Active, not recruiting | ||
| Phase I Study Of Octreotide Acetate (Sandostatin) (SMS) As A Biomodulator Of Doxorubicin (DOX) [NCT00008073] | Phase 1 | 0 participants | Interventional | 1996-01-31 | Completed | ||
| Prospective, Randomized, Double-Blind, Placebo-Controlled Multicenter Phase III-Study to Evaluate the Efficacy of Octreotide in Patients With Inoperable Hepatocellular Carcinoma [NCT00386984] | Phase 3 | 108 participants | Interventional | 1999-10-31 | Completed | ||
| A Randomized, Open Label, Multicenter Study Evaluating the Effects of Octreotide Acetate on Circulating Levels of Chromogranin A in Advanced Prostate Cancer Patients [NCT00166725] | Phase 2 | 40 participants (Anticipated) | Interventional | 2004-02-29 | Completed | ||
| Effect of Somatostatin on Ghrelin Concentrations, Food Seeking Behaviour and Weight in Patients With Prader-Willi Syndrome [NCT00175305] | Phase 3 | 10 participants (Anticipated) | Interventional | 2004-08-31 | Terminated | ||
| A Randomized, Open Label, Controlled Study on the Efficacy and Safety of Octreotide i.m. in Patients With Proliferative Diabetic Retinopathy (PDR) After Start of Laser Coagulation [NCT00170742] | Phase 3 | 17 participants | Interventional | 2003-12-31 | Terminated(stopped due to trial stopped on Sept 24, 2007) | ||
| Impact of Prophylactic Octreotide to Pancreatic Exocrine Secretion and Pancreatic Fistula After Pancreatoduodenectomy [NCT02920567] | 282 participants (Anticipated) | Interventional | 2014-01-31 | Recruiting | |||
| Evaluation of the Effect of Octreotide Compared to Placebo in Patients With Inoperable Bowel Obstruction Due to Peritoneal Carcinomatosis [NCT00332696] | Phase 2 | 64 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, Ascending, Multidose Study To Determine Safety and Tolerability of Orally Administered LX1606 in Subjects With Symptomatic Carcinoid Syndrome Refractory to Stable-Dose Octreotide Long-A [NCT00853047] | Phase 2 | 23 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| Predictive Value of 3 Months Results on 12 Months Tumor Shrinkage After First-Line Octreotide-LAR Therapy in Patients With Acromegaly [NCT00616408] | 61 participants (Actual) | Observational | 1997-01-31 | Completed | |||
| Pharmacodynamics Of Product Octreotide Acetate Lar 30 Mg, Imported And Distributed By The Laboratory Chemical Pharm. Bergamo, Compared To Product Sandostatin LAR®30 MG Manufactured By Novartis Biosciences S/A [NCT01086982] | Phase 1 | 16 participants (Anticipated) | Interventional | 2010-03-31 | Suspended | ||
| Sandostatin LAR vs. Surgery in Acromegalics With Macroadenoma [NCT00001860] | Phase 2 | 5 participants | Interventional | 1999-08-31 | Completed | ||
| A Randomized, Double-Blind, Double Dummy, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy of LF-PB 10 mg, 20 mg, and 30 mg to Treat Lymphorrhea Post Axillary Dissection in Breast Cancer [NCT01754285] | Phase 2 | 114 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
| The Use of Midodrine, Octreotide and Albumin in Refractory Ascites [NCT00240045] | Phase 2/Phase 3 | 9 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| Evaluation of the Efficacy of Long-acting Release Octreotide in Patients With Advanced Hepatocellular Carcinoma [NCT00241020] | Phase 3 | 270 participants (Actual) | Interventional | 2002-06-30 | Completed | ||
| Combination of Everolimus and Octreotide LAR in Aggressive Recurrent Meningiomas. [NCT02333565] | Phase 2 | 20 participants (Actual) | Interventional | 2015-01-22 | Completed | ||
| Open Label Study Assessing the Efficacy and Safety of Octreotide Acetate in Patients With Acromegaly, With Micro or Macroadenomas [NCT00242541] | Phase 4 | 50 participants (Actual) | Interventional | 2003-03-31 | Terminated | ||
| Evaluation and Treatment of Autonomic Failure. [NCT00223691] | Phase 1 | 389 participants (Actual) | Interventional | 2002-03-31 | Completed | ||
| PHASE II TRIAL OF FLUDARABINE AND SANDOSTATIN FOR RELAPSED LOW-GRADE NON-HODGKIN'S LYMPHOMA [NCT00002779] | Phase 2 | 34 participants (Actual) | Interventional | 1998-02-28 | Completed | ||
| RCT for the Effect of Early Administration of Vasoactive Substances When Combined With Endoscopic Treatment in Acute Gastro-esophageal Variceal Bleeds: Comparisons Among Terlipressin, Somatostatin, and Octreotide [NCT00966355] | Phase 4 | 1,034 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
| A Double-Blind, Randomized, Placebo-Controlled, Single-Dose, 3-Period, 4 Treatment Incomplete Crossover Study to Assess the Effects of Single Oral Doses of L-001241689 on Glucagon-Induced Glycemic Excursion in Healthy Male Subjects Following Intravenous A [NCT02012166] | Phase 1 | 18 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
| Comparison of 24-hours Versus 72-hours of Octreotide Infusion Along With Endoscopic Therapy in Preventing Early Rebleed From Esophageal Varices: a Multi-center, Randomized Clinical Study [NCT03624517] | Phase 4 | 160 participants (Anticipated) | Interventional | 2018-09-19 | Recruiting | ||
| A Phase I Study of Safety and Immunogenicity of Survivin Long Peptide Vaccine (SurVaxM) in Patients With Metastatic Neuroendocrine Tumors (NETs) [NCT03879694] | Phase 1 | 14 participants (Anticipated) | Interventional | 2019-06-17 | Recruiting | ||
| A Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Crossover Study in Women With Irritable Bowel Syndrome to Evaluate Feasibility and Reproducibility of Barostat Assessments of Colorectal Sensation During Colorectal Distention and Its Pharmacol [NCT00584298] | Phase 1 | 50 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| 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 | ||
| Study to Investigate the Antiproliferative Effect of Octreotide in Patients With Metastasized Neuroendocrine Tumors of the Midgut [NCT00171873] | Phase 3 | 85 participants (Actual) | Interventional | 2001-09-30 | Completed | ||
| [NCT02217839] | Phase 1 | 42 participants (Actual) | Interventional | 2012-04-30 | Completed | ||
| The Effect of Acute Application of Pegvisomant Alone and in Combination With Octreotide on Endogenous GH Levels During a 6 Hour Test in Patients With Acromegaly on Constant Pegvisomant Treatment [NCT00595140] | Phase 4 | 10 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| Role of Octreotide Intravenous Infusion in Non-variceal GI Bleeding in ICU [NCT06062719] | Phase 2/Phase 3 | 56 participants (Anticipated) | Interventional | 2023-08-23 | Recruiting | ||
| The Effect of Satiety Gut Hormone Modulation on Appetitive Drive After Upper Gastrointestinal Surgery [NCT02381249] | 40 participants (Actual) | Interventional | 2015-03-31 | Completed | |||
| A Multicentre, Double Blind, Randomized Placebo Controlled Trial to Assess the Effect of LF-PB on Seroma Formation in Women With Breast Cancer Undergoing Axillary Lymph Node Dissection [NCT02668588] | Phase 2 | 48 participants (Actual) | Interventional | 2015-10-22 | Completed | ||
| A Multicenter, Randomized, Blinded Study to Assess Safety and Efficacy of Pasireotide LAR vs. Octreotide LAR in Patients With Active Acromegaly [NCT00600886] | Phase 3 | 358 participants (Actual) | Interventional | 2008-02-11 | 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 | ||
| Efficacy And Safety Of Terlipressin Vs Octreotide As Adjuvant Therapy In Bleeding Esophageal Varices [NCT00534677] | Phase 4 | 320 participants (Actual) | Interventional | 2004-05-31 | Completed | ||
| Efficacy of Medical Treatment With Octreotide in Patients With Primary Inoperable Thymoma to Reduce Tumor Size [NCT00332969] | Phase 2 | 25 participants (Actual) | Interventional | 2005-09-30 | Completed | ||
| A Pilot, Phase II Study With a Prospective, Randomized, Cross-Over, Placebo-Controlled, Double-Blind Design to Assess the Short-Term Effects of Tolvaptan Plus Placebo vs Tolvaptan Plus Octreotide LAR Combination Therapy in ADPKD Patients With Normal Kidne [NCT03541447] | Phase 2 | 20 participants (Actual) | Interventional | 2018-12-12 | Completed | ||
| Metabolic, Cardiovascular and Body Composition Effects of Sandostatin LAR® Therapy of Acromegaly, Effect of Reduction of Serum Insulin-like Growth Factor 1 (IGF-1) Levels Into a New Normative Range [NCT01424241] | Phase 4 | 20 participants (Anticipated) | Interventional | 2006-08-31 | Active, not recruiting | ||
| A Multicenter, Randomized, Crossover, Open Label Dose Finding Study to Compare the Safety, Efficacy and PK/PD Relationship of Multiple Doses of SOM230 and Sandostatin in Acromegalic Patients [NCT00088582] | Phase 2 | 62 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| Phase 1 Trial Using 131I MIBG and 90Y DOTATOC in a Dosimetrically Determined Optimal Combination for Therapy of Selected Patients With Midgut Neuroendocrine Tumors. [NCT03044977] | Early Phase 1 | 20 participants (Anticipated) | Interventional | 2017-05-07 | Active, not 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 Prospective, Randomized Trial of Sandostatin LAR Depot for the Prevention of Irinotecan-Induced Diarrhea in Patients With Metastatic Colorectal Cancer [NCT00006269] | Phase 3 | 89 participants (Actual) | Interventional | 1999-12-31 | Terminated | ||
| Functional MRI-based Assessment of Terlipressin vs. Octreotide on Renal Function in Cirrhotic Patients With Acute Variceal Bleeding (CHESS1903): A Multicenter, Single-blind, Randomised Controlled Trial [NCT04028323] | Phase 4 | 60 participants (Anticipated) | Interventional | 2019-07-16 | Recruiting | ||
| Open Label, Randomized Study Comparing the Biological Efficacy & Safety of a New Prolonged Release Formulation of Octreotide Acetate, C2L-OCT-01 PR, 30 mg Administered Every 42 Days for 84 Days With Sandostatin LAR 30 mg Administered Every 28 Days for 84 [NCT00616551] | Phase 3 | 65 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
| Incidence of Medical and Nutritional Complications After Bariatric Surgery, Especially Focusing on Assessment and Treatment of Severe Hypoglycemia [NCT01865760] | 33 participants (Actual) | Interventional | 2013-06-30 | Completed | |||
| A Within Group, Randomised, Phase I, Repeated Doses, Placebo and Octreotide Controlled Study in Healthy Volunteers to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics After Incremental Doses of ITF2984 [NCT01871844] | Phase 1 | 46 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Dosimetry Based PRRT Versus Standard Dose PRRT With Lu-177-DOTATOC in NEN Patients- a Randomized Study; a Step Towards Tailored PRRT [NCT04917484] | Phase 2 | 100 participants (Anticipated) | Interventional | 2020-02-01 | Recruiting | ||
| Validation of 99mTc- EDDA - HYNIC -TOC Kits for Diagnosis of Neuroendocrine Tumors [NCT02691078] | Phase 2 | 15 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
| A Phase I , Open Label, Single Center, Dose Escalation Study to Assess the Pharmacokinetics, Safety and Tolerability of a Single Dose of a New Extended Long-acting Formulation of Octreotide Pamoate Administered i.m. in Healthy Cholecystectomized Volunteer [NCT00432068] | Phase 1 | 48 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| Phase 2 Study of Long Acting Octreotide in Idiopathic Pulmonary Fibrosis [NCT00463983] | Phase 1/Phase 2 | 25 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
| Clinical Trial of Sir-Spheres® in Patients With Symptomatic or Progressive Hepatic Metastases From Neuroendocrine Tumors [NCT00466856] | Phase 2 | 10 participants (Actual) | Interventional | 2003-12-31 | Terminated(stopped due to due to slow accrual) | ||
| Preoperative Octreotide Treatment of Patients With Growth Hormone Producing Pituitary Adenomas [NCT00521300] | Phase 4 | 62 participants (Actual) | Interventional | 1999-09-30 | Completed | ||
| Efficacy and Safety of Octreotide in Laparoscopic Hepatectomy Surgery: Effect on Blood Loss, Need for Vasoactive Drugs, Transfusion Requirements. [NCT06085976] | Phase 2 | 62 participants (Anticipated) | Interventional | 2023-08-14 | Recruiting | ||
| Pros & Cons of Norepinephrine Infusion Versus Midodrine & Octreotide in Patients With Hepatorenal Syndrome Type 1 in Intensive Care Unit. [NCT03455322] | Phase 4 | 60 participants (Actual) | Interventional | 2018-08-15 | Completed | ||
| GI-072: Randomized Controlled Trial of the Use of Octreotide to Enhance Liver Recovery After Major Hepatectomy [NCT03179995] | Phase 2 | 24 participants (Actual) | Interventional | 2017-07-07 | Terminated(stopped due to Grantor closed study) | ||
| A Phase II Study of Octreotide Acetate for the Treatment of Advanced or Metastatic Hepatocellular Carcinoma [NCT00257426] | Phase 2 | 31 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
| An Open-label, Two-step, Multicenter European Study to Evaluate the Efficacy and Safety of Sandostatin LAR at High Dose or in Combination Either With GH-receptor Antagonist or Dopamine-agonist in Acromegalic Patients Not Adequately Controlled by Conventio [NCT01278342] | Phase 4 | 70 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
| The Effect of Preoperative Long Period Octreotide Combined With Postoperative Short Period Octreotide on the Complications After Pancreatectomy. A Prospective, Multicenter Clinical Trial [NCT03398941] | 150 participants (Anticipated) | Interventional | 2018-02-01 | Recruiting | |||
| A Phase II Clinical Trial of Cabazitaxel Plus Prednisone With Octreotide in the Treatment of Castration-Resistant Prostate Cancer (CRPC) Previously Treated With Docetaxel [NCT01469338] | Phase 2 | 9 participants (Actual) | Interventional | 2012-07-31 | Terminated(stopped due to lack of funding) | ||
| a Prospective Study on the Efficacy and Safety Using Sequential Therapy of Irinotecan Combined With Cisplatin (IP)and Octretide Lar in the First Line Treatment of Metastatic or Inoperable Gastrointestinal Poorly Differentiated Neuroendocrine Carcinoma: th [NCT01480986] | Phase 2 | 40 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Safety and Efficacy of Octreotide LAR Depot in Left Ventricular Assist Device (LVAD) Associate Gastrointestinal (GI) [NCT01707225] | Phase 1 | 10 participants (Actual) | Interventional | 2013-02-28 | Completed | ||
| [NCT00076362] | Phase 4 | 60 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
| An Open-label Extension Study to Evaluate the Long-term Safety and Tolerability of Octreotide Acetate in Microspheres in the Therapy of Patients With Moderately Severe or Severe Non-proliferative Diabetic Retinopathy (NPDR) or Low Risk Proliferative Diabe [NCT00248131] | Phase 3 | 260 participants | Interventional | 2005-11-30 | Terminated | ||
| A Study To Compare The Efficacy And Safety Of Pegvisomant To That Of Sandostatin Lar Depot In Patients With Acromegaly [NCT00068042] | Phase 4 | 100 participants | Interventional | 2003-04-30 | Completed | ||
| A Multicenter, Randomized, Open-label Clinical Trial Assessing the Efficacy of Octreotide in Decreasing Blood and Iron Requirements in Patients With Refractory Anemia Due to Angiodysplasias [NCT02384122] | Phase 3 | 62 participants (Actual) | Interventional | 2015-09-30 | Completed | ||
| [NCT00094146] | Phase 2 | 160 participants | Interventional | 2002-01-31 | Completed | ||
| Safety and Efficacy of Octreotide LAR in Treatment Naïve Acromegalic Patients [NCT00128232] | Phase 3 | 100 participants | Interventional | 2002-12-31 | Completed | ||
| A Randomized, Controlled Study on the Efficacy and Safety of Octreotide Acetate in Microspheres in the Therapy of Patients With Moderately Severe or Severe Non-proliferate Diabetic Retinopathy (NPDR) or Low Risk Proliferative Diabetic Retinopathy (PDR) [NCT00130845] | Phase 3 | 312 participants (Actual) | Interventional | 2000-02-29 | Completed | ||
| Beneficial Effect of Dose Escalation of Octreotide-LAR as First-Line Therapy in Patients With Resistant Acromegaly [NCT00461149] | Phase 4 | 50 participants | Interventional | 1995-01-31 | Completed | ||
| A Randomized, Controlled Study on the Efficacy and Safety of Octreotide Acetate in Microspheres in the Therapy of Patients With Moderately Severe or Severe Non-proliferate Diabetic Retinopathy (NPDR) or Low Risk Proliferative Diabetic Retinopathy (PDR) [NCT00131144] | Phase 3 | 583 participants (Actual) | Interventional | 1999-11-30 | 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 | |||
| Role of Hyperinsulinemia in Non-Alcoholic Fatty Liver Disease (NAFLD) Pathogenesis: Pancreatic Clamp Pilot & Feasibility Study [NCT05724134] | Phase 1 | 20 participants (Anticipated) | Interventional | 2023-08-29 | Recruiting | ||
| An Open-label Extension Study to Evaluate the Long-term Safety and Tolerability of Octreotide Acetate in Microspheres in the Therapy of Patients With Moderately Severe or Severe Non-proliferative Diabetic Retinopathy (NPDR) or Low Risk Proliferative Diabe [NCT00248157] | Phase 3 | 105 participants (Actual) | Interventional | 2005-11-30 | Terminated(stopped due to Inconsistent treatment benefit) | ||
| 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 Multicenter Placebo-Controlled Dose Titration Study to Evaluate the Efficacy and Safety of Sandostatin (SMS 201-995) in the Treatment of Patients With Acquired Immunodeficiency Related Diarrhea [NCT00002252] | 0 participants | Interventional | Completed | ||||
| [NCT00050635] | Phase 4 | 150 participants | Interventional | 2002-12-31 | Completed | ||
| A Randomized, Parallel Group, Three-Arm Study To Evaluate Treatment With A Combination Of Pegvisomant Plus Sandostatin Lar, Pegvisomant (Alone), And Sandostatin Lar (Alone) In Patients With Acromegaly [NCT00068029] | Phase 4 | 75 participants | Interventional | 2003-10-31 | Completed | ||
| A Randomized, Double Blind, Placebo-Controlled Phase III Study To Determine The Efficacy Of Sandostatin LAR® Depot (Octreotide Acetate) In Preventing Or Reducing The Severity Of Chemoradiation-Induced Diarrhea In Patients With Anal Or Rectal Cancer [NCT00075868] | Phase 3 | 233 participants (Actual) | Interventional | 2003-12-31 | Completed | ||
| Macro and Microcirculatory Effects of the Combination of Norepinephrine and Octreotide for the Treatment of Cirrhotic Patients With Hemorrhagic Shock [NCT03891849] | 0 participants (Actual) | Interventional | 2021-09-01 | Withdrawn(stopped due to No participant enrolled. Equipment unvailable.) | |||
| Hemodynamic Profile of Terlipressin and Octreotide in Patients With Cirrhosis and Portal Hypertension. A Randomised, Single Blinded Clinical Trial. [NCT04353193] | Phase 4 | 36 participants (Anticipated) | Interventional | 2020-06-30 | Not yet recruiting | ||
| A Phase I, Open Label, Maximum Tolerated Dose-Finding Study to Evaluate the Safety and Tolerability of 90Y-DOTA-tyr3-Octreotide Administered by Intravenous Infusion to Children With Refractory Somatostatin-Receptor Positive Tumors [NCT00049023] | Phase 1 | 27 participants (Actual) | Interventional | 2002-01-31 | Completed | ||
| Phase III Double-Blind Study Of Depot Octreotide Versus Placebo In The Prevention Of Acute Diarrhea In Patients Receiving Pelvic Radiation Therapy [NCT00033605] | Phase 3 | 130 participants (Actual) | Interventional | 2002-04-30 | 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 Study of Octreotide Depot vs Saline Control in Pediatric Hypothalamic Obesity Patients [NCT00171613] | Phase 4 | 32 participants | Interventional | 2005-02-28 | Completed | ||
| Octreotide Efficacy and Safety in First-line Acromegalic Patients [NCT00171886] | Phase 4 | 20 participants (Actual) | Interventional | 2002-07-31 | Completed | ||
| Safety and Efficacy of Long-acting Repeatable Octreotide Acetate for Injectable Suspension vs. Surgery in Treatment-naïve Patients With Acromegaly [NCT00225979] | Phase 3 | 100 participants (Actual) | Interventional | 2002-11-30 | Completed | ||
| Phase II Study of Vatalanib and Octreotide in Patients With Progressive Low-Grade Neuroendocrine Tumors [NCT00227773] | Phase 2 | 0 participants (Actual) | Interventional | Withdrawn | |||
| A Phase II, Open-label, Multicentre, Randomised Study of the Pharmacokinetics, Pharmacodynamics, Efficacy, and Safety of CAM2029 in Patients With Acromegaly and Neuroendocrine Tumours (NETs) Previously Treated With Sandostatin® LAR® [NCT02299089] | Phase 2 | 12 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
| Stress, Diurnal Cortisol, and Breast Cancer Survival [NCT00226967] | 115 participants (Anticipated) | Observational | 2002-09-08 | Completed | |||
| [NCT02217826] | Phase 1 | 8 participants (Actual) | Interventional | Completed | |||
| Randomized Evaluation of Octreotide Versus Compazine for Emergency Department Treatment of Migraine Headache [NCT00274170] | Phase 1/Phase 2 | 56 participants | Interventional | 2006-01-31 | Recruiting | ||
| Trial of Thalidomide, a- Interferon +/- Octreotide in Patients With Unresectable Hepatocellular Carcinoma [NCT00250796] | Phase 2 | 12 participants (Actual) | Interventional | 2000-09-30 | Completed | ||
| Phase II, Dosimetry-Guided, Peptide Receptor Radiotherapy (PRRT) With 90Y-DOTA- tyr3-Octreotide (90Y-DOTATOC) in Children and Adults With Neuroendocrine and Other Somatostatin Receptor Expressing Tumors [NCT03013387] | Phase 2 | 0 participants (Actual) | Interventional | 2017-01-31 | Withdrawn(stopped due to This project has undergone a significant amount of updates and has been resubmitted under IRB# 201708778) | ||
| 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 | ||
| Treatment of Acromegaly With Somatostatin Analogs: GH vs. IGF-I as Primary Biochemical Target [NCT01618513] | Phase 4 | 84 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
| [NCT02374632] | Phase 4 | 40 participants (Actual) | Interventional | 2014-10-31 | Active, not recruiting | ||
| A Phase II/III Randomized Double-blind Study of Sandostatin LAR in Combination With Axitinib Versus Sandostatin LAR With Placebo in Patients With Advanced G1-G2 Neuroendocrine Tumours (WHO 2010) of Non-pancreatic Origin [NCT01744249] | Phase 2/Phase 3 | 255 participants (Anticipated) | Interventional | 2011-11-30 | Active, not recruiting | ||
| The Effect of Obesity-induced Cytokine Elevation on the Molecular Regulation of Protein Turnover and Carbohydrate Metabolism in Human Skeletal Muscle [NCT02305069] | 26 participants (Actual) | Interventional | 2009-10-31 | Completed | |||
| Study to Determine Whether Ultrasound Guidance Improves Delivery and Efficacy of Intramuscular Injection of Long-Acting Octreotide in the Treatment of Acromegaly [NCT00552071] | Phase 4 | 15 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
| The Effect of Subcutaneous Infusions of 3 Doses of a Novel Somatostatin Analogue, DG3173, on Growth Hormone Levels in Untreated Acromegalics [NCT02217800] | Phase 2 | 8 participants (Actual) | Interventional | 2013-11-30 | Completed | ||
| Prospective Randomized, Double-blind, Placebo-controlled Parallel Group Study of the Efficacy of Octreotide in Prevention of Salivary Fistulae After Post Radiation Salvage Surgery [NCT02437825] | Phase 2 | 40 participants (Anticipated) | Interventional | 2015-10-31 | Recruiting | ||
| 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 | ||
| "A Multicenter Placebo-Controlled Double Blind Study to Evaluate the Efficacy and Safety of Sandostatin ( SMS 201-995 ) in Patients With Acquired Immunodeficiency Related Diarrhea Who Were Either Responders or Non-Responders in a Prior Placebo-Controlled [NCT00002253] | 0 participants | Interventional | 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 | ||
| An Expanded Access Imaging of Neuroendocrine Tumors Using 68Ga-DOTA-TOC [NCT03001349] | Early Phase 1 | 4 participants (Actual) | Interventional | 2017-05-16 | Terminated(stopped due to Per PI Request) | ||
| A Two-Part, Phase 1, Randomized, Crossover Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Intranasal Octreotide (DP1038) Versus Subcutaneous Sandostatin® Injection in Healthy Adult Volunteers [NCT03031535] | Phase 1 | 32 participants (Actual) | Interventional | 2017-01-31 | Completed | ||
| Phase III, Open-Label, Multicenter International Study to Evaluate the Efficacy and Safety of an Octreotide Implant vs. Sandostatin LAR Depot in Patients With Acromegaly [NCT00765323] | Phase 3 | 169 participants (Actual) | Interventional | 2008-09-30 | Terminated | ||
| Sandostatin (Octreotide LAR) May Lead to Clinical Improvement Through Receptor Occupation Optimisation A Prospective Interventional Trial of Patients With Neuro-endocrine Tumors With Carcinoid Syndrome Receiving Octreotide LAR [NCT04140409] | Phase 4 | 10 participants (Actual) | Interventional | 2016-02-02 | Terminated(stopped due to Slow recruitment) | ||
| Phase II Study of Above-Label Octreotide-LAR in Patients With Insufficiently Controlled Carcinoid Syndrome [NCT01886287] | Phase 2 | 2 participants (Actual) | Interventional | 2013-12-31 | Terminated(stopped due to Slow accrual) | ||
| IMMUNeOCT Study: Octreotide LAR in the Induction of Immunologic Response in Patient With Neuroendocrine Tumors: an Interventional Pharmacological Study [NCT04129255] | Phase 2 | 34 participants (Actual) | Interventional | 2017-06-28 | Completed | ||
| A Study of the Effect of Ascending Single Doses of DG3173 and 300 μg of Octreotide on Human Growth Hormone Levels in Untreated Acromegalics. [NCT02235987] | Phase 2 | 20 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| Evaluation of Gallium-68 DOTA-TOC Imaging of Somatostatin Receptor Positive Malignancies [NCT02177773] | Phase 1/Phase 2 | 300 participants (Actual) | Interventional | 2014-06-23 | Terminated(stopped due to FDA approved agent for this indication during enrollment) | ||
| Evaluation of Impact of Sandostatin® Injection Before Axillary Clearance on Lymphocele Formation In Patients With Breast Cancer [NCT03791736] | 4 participants (Actual) | Interventional | 2016-07-06 | Terminated(stopped due to The surgical technique is no longer used) | |||
| Phase II, Dosimetry Guided, Peptide Receptor Radiotherapy (PRRT) Using 90Y-DOTA tyr3-Octreotide (90Y-DOTATOC) in Children and Adults With Neuroendocrine and Other Somatostatin Receptor Positive Tumors [NCT03273712] | Phase 2 | 39 participants (Actual) | Interventional | 2017-09-29 | Completed | ||
| A Randomized, Placebo-controlled, Double-blind, Multi-center Trial to Assess Efficacy and Safety of Octreotide Subcutaneous Depot (CAM2029) in Patients With Symptomatic Polycystic Liver Disease [NCT05281328] | Phase 2/Phase 3 | 69 participants (Anticipated) | Interventional | 2022-06-28 | Recruiting | ||
| An Exploratory, Randomized, Placebo-Controlled Trial of Depot Octreotide (Sandostatin LARDepot) for Symptomatic Ascites in Cancer Patients [NCT00182754] | Phase 3 | 33 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
| Effect of Octreotide on the Colonic Motility in Pediatric Patients [NCT01917773] | Phase 4 | 13 participants (Actual) | Interventional | 2013-08-31 | Completed | ||
| Comparator Study of 68Ga-DOTATOC PET/CT With Octreoscan + High-resolution, Contrast-enhanced CT for Diagnosis and Staging in Neuroendocrine Tumors and Other Somatostatin Receptor Positive Tumors [NCT01869725] | Phase 2 | 68 participants (Actual) | Interventional | 2013-04-01 | Completed | ||
| A Randomized Trial of Antiestrogen Therapy Versus Combined Antiestrogen and Octreotide Therapy in the Adjuvant Treatment of Breast Cancer in Post-Menopausal Women [NCT00002864] | Phase 3 | 667 participants (Actual) | Interventional | 1996-09-24 | Completed | ||
| [NCT00004327] | Phase 2 | 8 participants | Interventional | 1995-01-31 | Completed | ||
| A Clinical Trial to Evaluate the Benefit of Adding Octreotide (SMS 201-995 PA LAR) to Tamoxifen Alone or to Tamoxifen and Chemotherapy in Patients With Axillary Node-Negative, Estrogen-Receptor-Positive, Primary Invasive Breast Cancer [NCT00002967] | Phase 3 | 0 participants | Interventional | 1997-05-31 | Completed | ||
| Octreotide Treatment to Improve Nutritional Recovery After Surgery for Patients With Esophageal or Gastric Cancer, a Prospective Randomized Open Label Phase II Study - OTIS [NCT04871204] | Phase 2 | 152 participants (Anticipated) | Interventional | 2021-06-16 | Recruiting | ||
| A Phase 3, Randomized, Double-blind, Placebo-controlled, Multicenter Study to Evaluate Efficacy and Safety of Octreotide Capsules in Patients Who Demonstrated Biochemical Control on Injectable Somatostatin Receptor Ligands (SRL) Treatment [NCT03252353] | Phase 3 | 56 participants (Actual) | Interventional | 2017-09-01 | Active, not recruiting | ||
| Fecal Calprotectin Levels in Mycophenolate Mofetil Induced Diarrhea and Treatment With Octreotide [NCT02977897] | 10 participants (Anticipated) | Observational | 2017-01-31 | Not yet recruiting | |||
| A Multicenter, Single Arm, Proof of Concept Study to Investigate the Efficacy of an 8 Month Combination Therapy of Octreotide and Cabergoline in Acromegalic Patients Only Partially Responsive to Somatostatin Analog Monotherapy [NCT00376064] | Phase 4 | 20 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
| Safety and Efficacy Study of 68Ga-Dotatoc Positron Emission Tomography for Diagnosis for Staging, Restaging and Assessment of Response to Treatment in Somatostatin Receptor-Positive Neuroendocrine Tumors [NCT02359500] | Phase 1 | 71 participants (Actual) | Interventional | 2014-12-31 | Terminated(stopped due to compound no longer available) | ||
| Pilot Study Of Long-Acting Octreotide (Octreotide LAR® Depot) In The Treatment Of Patients With Severe Polycystic Liver Disease [NCT00426153] | Phase 2/Phase 3 | 42 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| Monocentric Interventionnal Pilot Study Pilot Study Evaluating Somatostatin Receptor's PET Imaging to Detect Inflammatory Phases of Myocarditis [NCT03347760] | 33 participants (Anticipated) | Interventional | 2020-07-13 | Recruiting | |||
| Long-term (up to 3 Years) Clinical and Hormonal Outcomes in Acromegalic Patients With Treated Surgery With or Without Long Acting Somatostatin Analogues: Open-labeled, Prospective, Parallel Group Study [NCT02427295] | Phase 4 | 1 participants (Anticipated) | Interventional | 2014-03-31 | Recruiting | ||
| A Phase 3, Randomized, Double-blind, Placebo-controlled, Multi-center Trial to Assess Efficacy and Safety of Octreotide Subcutaneous Depot (CAM2029) in Patients With Acromegaly [NCT04076462] | Phase 3 | 72 participants (Actual) | Interventional | 2019-08-14 | Completed | ||
| Al18F-NOTA-octreotide PET Imaging of the Somatostatin Receptor in Neuroendocrine Tumors [NCT04552847] | Phase 2/Phase 3 | 85 participants (Actual) | Interventional | 2020-10-07 | Completed | ||
| Application of Al18F-octreotide PET/CT in Neuroendocrine Tumor [NCT05749289] | Phase 1 | 50 participants (Anticipated) | Interventional | 2022-12-20 | Recruiting | ||
| A Phase 3, Open-label, Single-arm, Multi-center Trial to Assess the Long-term Safety of Octreotide Subcutaneous Depot (CAM2029) in Patients With Acromegaly [NCT04125836] | Phase 3 | 135 participants (Actual) | Interventional | 2019-10-10 | Active, not recruiting | ||
| Phase II Study of the Combination of Bevacizumab, Pertuzumab, and Sandostatin for Patients With Advanced Neuroendocrine Cancers. [NCT01121939] | Phase 2 | 43 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
| Palliative Management of Inoperable Malignant Bowel Obstruction: A Prospective, Open Label, Phase-2 Study at an NCI Comprehensive Cancer Center [NCT04027348] | Phase 2 | 15 participants (Actual) | Interventional | 2019-06-26 | Terminated(stopped due to low accrual) | ||
| A Pilot Study Of Ga-68-DOTA-TOC Imaging In Participants With Small Bowel Carcinoid Tumors [NCT03057509] | Phase 1 | 0 participants (Actual) | Interventional | 2018-11-30 | Withdrawn(stopped due to Slow accrual) | ||
| A Phase II Study of the Somatostatin Analog Sandostatin LAR in Patients With Androgen Independent Prostate Cancer [NCT00510224] | Phase 2 | 13 participants (Actual) | Interventional | 2007-07-31 | Terminated(stopped due to Stopped at interim analyses phase due to lack of efficacy) | ||
| An Open-label, Multi-center Everolimus Roll-over Protocol for Patients Who Have Completed a Previous Novartis-sponsored Everolimus Study and Are Judged by the Investigator to Benefit From Continued Everolimus Treatment [NCT01789281] | Phase 4 | 34 participants (Actual) | Interventional | 2013-05-14 | Completed | ||
| Prevention of Postoperative Pancreatic Fistula by SOMATOSTATIN Compared to OCTREOTIDE: Prospective, Randomized, Controlled Study [NCT03000946] | Phase 3 | 655 participants (Actual) | Interventional | 2017-05-15 | Completed | ||
| Randomized Phase II Study of Everolimus Alone Versus Everolimus Plus Bevacizumab in Patients With Locally Advanced or Metastatic Pancreatic Neuroendocrine Tumors [NCT01229943] | Phase 2 | 150 participants (Actual) | Interventional | 2010-10-15 | Completed | ||
| Efficacy and Safety of Oral Octreolin™ in Patients With Acromegaly Who Are Currently Receiving Parenteral Somatostatin Analogs [NCT01412424] | Phase 3 | 155 participants (Actual) | Interventional | 2012-03-31 | Completed | ||
| Octreotide for Palliation of Inoperable Bowel Obstruction: A Phase II Study [NCT00004895] | Phase 2 | 0 participants | Interventional | 1999-10-31 | Completed | ||
| Nor-epinephrine Versus Midodrine/Octreotide in Patients With Hepatorenal Acute Kidney Injury [NCT04522297] | 91 participants (Actual) | Interventional | 2018-04-15 | Completed | |||
| A Single-dose Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Octreotide Injection in Healthy Adult Subjects [NCT05761431] | Phase 1 | 56 participants (Actual) | Interventional | 2023-03-02 | Completed | ||
| A Randomised, Multicentre, Open Label, Phase II Study of Prophylactic Octreotide to Prevent or Reduce the Frequency and Severity of Diarrhoea in Subjects Receiving Lapatinib With Capecitabine for the Treatment of Metastatic Breast Cancer [NCT02294786] | Phase 2 | 62 participants (Actual) | Interventional | 2014-12-17 | Terminated | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||
Octreotide treatment will be considered successful if the patient receiving treatment for six months shows a reduction in total tumor mass/ fluid collection or reaccumulation of at least 20%. (NCT00005906)
Timeframe: Six months
| Intervention | Participants (Number) |
|---|---|
| Octreotide | 0 |
"Octreotide treatment will be considered successful if the reported pain/symptom score is reduced by at least 2 levels at termination of treatment.~A simple visual numeric distress scale ranging from zero to 10 will be employed to rate the severity of individual symptoms. The best score is zero, which means absence of symptoms and the maximal is 10, meaning that the symptoms are very severe." (NCT00005906)
Timeframe: Six months
| Intervention | Participants (Number) |
|---|---|
| Octreotide | 1 |
"One or more abnormality of the following liver function tests:~Alkaline phosphatase above 116 i.u.~SGPT above 41 i.u.~SGOT from 34 i.u.~Total bilirubin above 1.0 mg/dl" (NCT00005906)
Timeframe: Six months
| Intervention | Participants (Number) |
|---|---|
| Octreotide | 1 |
Comparison between Albumin (Control group) and Vasoconstrictor (Treatment group) (NCT00108355)
Timeframe: Variable depending on the patient, average 10 days
| Intervention | days (Median) |
|---|---|
| Albumin (Control Group) | 10 |
| Vasoconstrictor (Treatment Group) | 8 |
Defined as an increase in Plasma Renin Activity (PRA) by >50% from baseline to a level > 4 ng/mL/h at post-paracentesis day (NCT00108355)
Timeframe: 6 days after paracentesis
| Intervention | participants (Number) |
|---|---|
| Albumin (Control Group) | 2 |
| Vasoconstrictor (Treatment Group) | 2 |
PFS is measured from date of trial entry until documented progression of disease or death from any cause. PFS is measured by computed tomography (CT) scans or magnetic resonance imaging (MRI) performed at baseline and after every three cycles. (NCT00113360)
Timeframe: PFS assessed every 12 weeks (at the end of every 3 cycles) or more frequently if clinically indicated
| Intervention | Weeks (Median) |
|---|---|
| RAD001 Plus Octreotide Depot | 60 |
Median time to tumor progression at the time of the planned interim analysis that includes all data observed until June 2008. (NCT00171873)
Timeframe: Up to 7 years
| Intervention | Months (Median) |
|---|---|
| Octreotide LAR (SMS995) | 14.3 |
| Placebo | 6.0 |
Kaplan Meier curves will be constructed for each group; patients lost to follow up will be censored. A log rank test will be used to compare groups. We will adjust for the volume of fluid withdrawn at paracentesis and for change in abdominal circumference between baseline and the next procedure because a patient may require an extra paracentesis if only a small volume is withdrawn at baseline. (NCT00182754)
Timeframe: Up to 2 years
| Intervention | days (Median) |
|---|---|
| Arm I | 28 |
| Arm II | 14 |
We will compare the number of paracenteses between groups. Parametric or nonparametric testing will be used as appropriate. (NCT00182754)
Timeframe: Up to 2 years
| Intervention | number of paracenteses per patient (Median) |
|---|---|
| Arm I | 0.5 |
| Arm II | 1 |
Quality of life will be recorded and analyzed in a descriptive, exploratory fashion. We acknowledge that this study will represent the first to attempt a prospective assessment of quality of life in patients with symptomatic ascites. The underlying hypothesis of this quality of life assessment is that patients who are receiving octreotide will enjoy a better quality of life compared to patients who receive placebo. Quality of life scores from the CLDQ will be summed for all patients on a monthly basis. Again we anticipate high patient drop out rates over time within these two cohorts. With due diligence, we will attempt to ascertain the reason for each patient drop out, and appropriate imputation techniques will be employed for each.Quantified as: 1='All of the time' 2='Most of the time' 3='A good bit of the time' 4='Some of the time' 5='A little bit of the time' 6='Hardly any of the time' 7='None of the time' 0='Missing'; (NCT00182754)
Timeframe: Up to 2 years
| Intervention | QOL score (Median) | ||
|---|---|---|---|
| abdominal bloating | shortness of breath | abdominal discomfort | |
| Arm I | 4 | 4 | 4.5 |
| Arm II | 3 | 3 | 2 |
The Edmonton Scale consisted of 9 items: pain, activity, nausea, depression, anxiety, fatigue, appetite, sensation of well-being and dyspnea (difficult or labored breathing). Participants rated these items on a scale of 0 to 10, with 10 being the worse. (NCT00332696)
Timeframe: Day 1, Day 7, Day 14, Month 1, Month 2 and Month 3
| Intervention | Scores on a scale (Mean) | |||||
|---|---|---|---|---|---|---|
| Day 1 (n=30,29) | Day 7 (n=24,26) | Day 14 (n=20,14) | Month 1 (n=11,13) | Month 2 (n=7,4) | Month 3 (n=2,2) | |
| Octreotide | 4.12 | 4.23 | 4.30 | 4.18 | 3.46 | 0.05 |
| Placebo | 4.12 | 3.37 | 3.85 | 4.49 | 3.23 | 1.60 |
The mean number of vomiting episodes per a 24 hour period is presented for Day 1, Day 7 and Day 14. (NCT00332696)
Timeframe: Day 1, Day 7 and Day 14
| Intervention | Vomiting episodes (Mean) | ||
|---|---|---|---|
| Day 1 | Day 7 (n=31,31) | Day 14 (n=28,27) | |
| Octreotide | 1.2 | 0.3 | 0.3 |
| Placebo | 0.6 | 0.4 | 0.5 |
"Treatment Success was defined as: less than 2 episodes of vomiting on average per day for the 4 days prior to Day 14 [from Day 10 to Day 13] and no use of an Nasogastric Tube (NGT) since at least Day 10 and no use of an anticholinergic agent until Day 14.~Treatment Failure is defined as: 2 or more episodes of vomiting per day on average for the 4 days prior to Day 14 or use of an NGT after Day 9 or use of an anticholinergic agent before Day 14 or withdrawal from the trial between Day 1 and Day 14 (included), whatever the cause." (NCT00332696)
Timeframe: Day 10 to Day 13
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| TREATMENT SUCCESS | Vomiting episodes <2 (per day) | Vomiting episodes ≥2 (per day) | No Nasogastric Tube since Day 10 | Nasogastric Tube used since Day 10 | No Anticholinergic agents | Anticholinergic agents taken | Premature discontinuation/missing data, failure | |
| Octreotide | 12 | 19 | 2 | 14 | 7 | 18 | 3 | 11 |
| Placebo | 9 | 13 | 2 | 13 | 2 | 11 | 4 | 17 |
Relief from obstruction is defined by combining restart of stools for at least the previous 3 days, less than 2 episodes of vomiting on average for the previous 4 days and the restarting of flatus (gas generated in the stomach or bowels) for at least the previous 12 hours. (NCT00332696)
Timeframe: Day 7 and Day 14
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Relief from Obstruction: Day 7 | No Relief from Obstruction: Day 7 | Relief from Obstruction: Day 14 | No Relief from Obstruction: Day 14 | |
| Octreotide | 9 | 20 | 11 | 10 |
| Placebo | 15 | 12 | 10 | 5 |
Recurrence of bowel obstruction was confirmed by abdominal X-ray. (NCT00332696)
Timeframe: Month 3
| Intervention | Participants (Number) | |
|---|---|---|
| Recurrence at Month 3 | No Recurrence at Month 3 | |
| Octreotide | 0 | 3 |
| Placebo | 0 | 2 |
Recurrence of bowel obstruction was confirmed by abdominal X-ray. (NCT00332696)
Timeframe: Month 2
| Intervention | Participants (Number) | |
|---|---|---|
| Recurrence at Month 2 | No Recurrence at Month 2 | |
| Octreotide | 2 | 6 |
| Placebo | 2 | 5 |
Recurrence of bowel obstruction was confirmed by abdominal X-ray. (NCT00332696)
Timeframe: 1 Month
| Intervention | Participants (Number) | |
|---|---|---|
| Recurrence at Month 1 | No Recurrence at Month 1 | |
| Octreotide | 1 | 13 |
| Placebo | 2 | 13 |
Participants rated their nausea intensity on a scale of 0 to 3, with 3 being the worse. The number of participants with a score of 0, a score of 1, a score of 2 and a score of 3 are presented for Day 7. (NCT00332696)
Timeframe: Day 7
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Score=0 | Score=1 | Score=2 | Score=3 | |
| Octreotide | 21 | 2 | 5 | 3 |
| Placebo | 15 | 9 | 6 | 1 |
Participants rated their nausea intensity on a scale of 0 to 3, with 3 being the worse. The number of participants with a score of 0, a score of 1, a score of 2 and a score of 3 are presented for Day 14. (NCT00332696)
Timeframe: Day 14
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Score=0 | Score=1 | Score=2 | Score=3 | |
| Octreotide | 22 | 2 | 2 | 2 |
| Placebo | 22 | 3 | 1 | 1 |
Participants rated their nausea intensity on a scale of 0 to 3, with 3 being the worse. The number of participants with a score of 0, a score of 1, a score of 2 and a score of 3 are presented for Day 1. (NCT00332696)
Timeframe: Day 1
| Intervention | Participants (Number) | |||
|---|---|---|---|---|
| Score=0 | Score=1 | Score=2 | Score=3 | |
| Octreotide | 16 | 1 | 7 | 8 |
| Placebo | 13 | 2 | 9 | 8 |
Day 7 treatment success was defined as improvement of symptoms in the previous 2 days (average number of vomiting episodes less than 2 from Day 5, no Nasogastric Tube (NGT) since Day 5 and no anticholinergic agent or withdrawal from trial). (NCT00332696)
Timeframe: Day 5 to Day 7
| Intervention | Participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| TREATMENT SUCCESS | Vomiting episodes <2 (per day) since Day 5 | Vomiting episodes ≥2 (per day) since Day 5 | No Nasogastric Tube since Day 5 | Nasogastric Tube used since Day 5 | No Anticholinergic agents | Anticholinergic agents taken | Premature discontinuation/missing data | |
| Octreotide | 22 | 28 | 1 | 22 | 7 | 26 | 3 | 3 |
| Placebo | 20 | 25 | 2 | 24 | 3 | 25 | 2 | 5 |
"Overall survival measures the time of survival , with any response or disease progression, until death. The OS is defined as the time from date of start of treatment to date of death due to any cause.~If a patient is not known to have died, survival was censored at the date of last contact. In each treatment stratum, the Kaplan-Meier estimate of the overall survival function was constructed." (NCT00363051)
Timeframe: from randomisation to dates of disease progression, death from any cause, reported between day of first patient randomised, 26 June 2006, until cut-off date 13 April 2012
| Intervention | months (Median) |
|---|---|
| Stratum 1: Everolimus 10 mg | 28.78 |
"Overall survival measures the time of survival , with any response or disease progression, until death. The OS is defined as the time from date of start of treatment to date of death due to any cause.~If a patient is not known to have died, survival was censored at the date of last contact. In each treatment stratum, the Kaplan-Meier estimate of the overall survival function was constructed." (NCT00363051)
Timeframe: from randomisation to dates of disease progression, death from any cause, reported between day of first patient randomised, 26 June 2006, until cut-off date 13 April 2012
| Intervention | months (Median) |
|---|---|
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 38.77 |
Objective response rate was defined by RECIST criteria: Partial response (PR) must have ≥ 30% decrease in the sum of longest diameter of all target lesions, from the baseline sum. Complete response (CR) must have disappearance of all target and non-target lesions. For CR or PR, tumor measurements must be confirmed by 2nd assessments within 4 weeks. Progression = 20% increase in the sum of longest diameter of all target lesions, from smallest sum of longest diameter of all target lesions recorded at or after baseline; or a new lesion; or progression of non-target lesions. (NCT00363051)
Timeframe: from date of randomization/start of treatment until first documented response confirmed 4 weeks later (at least 3 months)
| Intervention | percentage of participants (Number) |
|---|---|
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 4.4 |
Objective response rate was defined by RECIST criteria: Partial response (PR) must have ≥ 30% decrease in the sum of longest diameter of all target lesions, from the baseline sum. Complete response (CR) must have disappearance of all target and non-target lesions. For CR or PR, tumor measurements must be confirmed by 2nd assessments within 4 weeks. Progression = 20% increase in the sum of longest diameter of all target lesions, from smallest sum of longest diameter of all target lesions recorded at or after baseline; or a new lesion; or progression of non-target lesions. (NCT00363051)
Timeframe: from date of randomization/start of treatment until first documented response confirmed 4 weeks later( at least 3 months)
| Intervention | percentage of participants (Number) |
|---|---|
| Stratum 1: Everolimus 10 mg | 9.6 |
For all patients in both strata, a blood sample for everolimus trough level determination will be collected immediately prior to the everolimus administration on Cycle 1 Day 15, Cycle 2 Day 1, and every month thereafter. A treatment cycle was defined as 28 days of consecutive daily treatment with everolimus and treatment continued until tumor progression. It is critical that patients not take their daily everolimus dose before the sample is drawn. (NCT00363051)
Timeframe: Cycle 1 Day 15
| Intervention | ng/ml (Mean) |
|---|---|
| Stratum 1: Everolimus 10 mg | 15.7 |
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 17.3 |
"Duration of overall response applies only to patients whose best overall response was complete response (CR) or partial response (PR):~Complete Response (CR) = at least two determinations of CR at least 4 weeks apart before progression.~Partial response (PR) = at least two determinations of PR or better at least 4 weeks apart before progression.~Progression = 20% increase in the sum of the longest diameter of all target lesions, from the smallest sum of longest diameter of all target lesions recorded at or after baseline; or a new lesion; or progression of non-target lesions" (NCT00363051)
Timeframe: from date of first documented confirmed response to time to progression, at least 3 months
| Intervention | Months (Median) |
|---|---|
| Stratum 1: Everolimus 10 mg | 10.64 |
Adverse events are defined as any unfavorable and unintended diagnosis, symptom, sign (including an abnormal laboratory finding), syndrome or disease which either occurs during study, having been absent at baseline, or, if present at baseline, appears to worsen. Serious adverse events are any untoward medical occurrences that result in death, are life threatening, require (or prolong) hospitalization, cause persistent or significant disability/incapacity, result in congenital anomalies or birth defects, or are other conditions which in judgment of investigators represent significant hazards. (NCT00363051)
Timeframe: on or after the day of the first intake of study treatment to starting no later than 28 days after study treatment discontinuation, at least every month
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Adverse Events | Death | Serious Adverse Events | |
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 45 | 2 | 27 |
The effect of Octreotide Depot on the trough concentrations of everolimus was assessed at Cycle 1 Day 15. (NCT00363051)
Timeframe: Cycle 1 Day 1, Cycle 2 Day 1
| Intervention | ng/ml (Mean) | |
|---|---|---|
| Cycle 1 Day 1 (pre-treatment baseline) (n=37) | Cycle 2 Day 1 (n= 38) | |
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 3.2 | 3.7 |
"Progression free survival (PFS) is defined as the time from randomization to the date of first documented disease progression or death from any cause. The Kaplan-Meier estimate of the PFS survival function was constructed.~Median PFS was obtained and displayed along with 95% confidence intervals." (NCT00363051)
Timeframe: from randomisation to dates of disease progression, death from any cause or last tumor assessment, reported between day of first patient randomised, 26 June 2006, until cut-off date 13 September 2010
| Intervention | Months (Median) |
|---|---|
| Stratum 2: Everolimus 10 mg + Octreotide Depot | 16.69 |
"Progression free survival (PFS) is defined as the time from randomization to the date of first documented disease progression or death from any cause. The Kaplan-Meier estimate of the PFS survival function was constructed.~Median PFS was obtained and displayed along with 95% confidence intervals." (NCT00363051)
Timeframe: from randomisation to dates of disease progression, death from any cause or last tumor assessment, reported between day of first patient randomised, 26 June 2006, until cut-off date 13 September 2010
| Intervention | Months (Median) |
|---|---|
| Stratum 1: Everolimus 10 mg | 9.69 |
Adverse events are defined as any unfavorable and unintended diagnosis, symptom, sign (including an abnormal laboratory finding), syndrome or disease which either occurs during study, having been absent at baseline, or, if present at baseline, appears to worsen. Serious adverse events are any untoward medical occurrences that result in death, are life threatening, require (or prolong) hospitalization, cause persistent or significant disability/incapacity, result in congenital anomalies or birth defects, or are other conditions which in judgment of investigators represent significant hazards. (NCT00363051)
Timeframe: on or after the day of the first intake of study treatment to starting no later than 28 days after study treatment discontinuation, at least every month
| Intervention | Participants (Number) | ||
|---|---|---|---|
| Adverse Events | Death | Serious Adverse Events | |
| Stratum 1: Everolimus 10 mg | 115 | 10 | 63 |
Insulin-like growth factor 1 (IGF-1) level was measured in a blood sample with an automated immunometric assay in a central laboratory. (NCT00372697)
Timeframe: Screening to end of study (Week 24)
| Intervention | µg/L (Mean) |
|---|---|
| Octreotide 30 mg Every 21 Days | -40.4 |
| Octreotide 60 mg Every 28 Days | -135.0 |
A pre-treatment magnetic resonance image (MRI) assessment of the pituitary area was required within 12 weeks prior to Screening as a baseline evaluation. A second MRI was performed at the end of the study (Week 24). All MRIs were performed according to protocol-defined guidelines. The tumor volume (mm^3) was calculated from measurements obtained in 3 axes from the MRI images. (NCT00372697)
Timeframe: Screening to end of study (Week 24)
| Intervention | mm^3 (Mean) |
|---|---|
| Octreotide 30 mg Every 21 Days | 15.9 |
| Octreotide 60 mg Every 28 Days | -0.4 |
The investigator asked the participant to score the following symptoms of acromegaly: Headache, perspiration, paresthesia, fatigue, osteoarthralgia, and carpal tunnel syndrome on a 5-point scale (0=absent; 1=mild; 2=moderate; 3=severe, but not disabling; 4=severe and disabling). The percentage of asymptomatic participants, ie, with a score of 0 for all symptoms, was calculated. (NCT00372697)
Timeframe: Week 12 and end of study (Week 24)
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Week 12 | Week 24 | |
| Octreotide 30 mg Every 21 Days | 33.3 | 20.0 |
| Octreotide 60 mg Every 28 Days | 9.09 | 9.09 |
A pre-treatment magnetic resonance image (MRI) assessment of the pituitary area was required within 12 weeks prior to Screening as a baseline evaluation. A second MRI was performed at the end of the study (Week 24). All MRIs were performed according to protocol-defined guidelines. The tumor volume (mm^3) was calculated from measurements obtained in 3 axes from the MRI images. (NCT00372697)
Timeframe: Screening to end of study (Week 24)
| Intervention | Percentage of participants (Number) |
|---|---|
| Octreotide 30 mg Every 21 Days | 14.3 |
| Octreotide 60 mg Every 28 Days | 11.1 |
The AcroQoL contains 8 items on Physical aspects. Participants were asked to rate each item on a 1-5 Likert scale measuring either the frequency of occurrence (always, most of the time, sometimes, rarely, or never) or the degree of agreement (completely agree, moderately agree, neither agree nor disagree, moderately disagree, completely disagree). The score on the physical scale can range from 8-40. A higher score indicates better Quality of Life. (NCT00372697)
Timeframe: End of study (Week 24)
| Intervention | Percent of maximum score (Mean) |
|---|---|
| Octreotide 30 mg Every 21 Days | 67.9 |
| Octreotide 60 mg Every 28 Days | 58.0 |
The AcroQoL contains 14 items on Psychological aspects. Participants were asked to rate each item on a 1-5 Likert scale measuring either the frequency of occurrence (always, most of the time, sometimes, rarely, or never) or the degree of agreement (completely agree, moderately agree, neither agree nor disagree, moderately disagree, completely disagree). The score on the psychological scale ranges from 14-70. A higher score indicates better Quality of Life. (NCT00372697)
Timeframe: End of study (Week 24)
| Intervention | Percent of maximum score (Mean) |
|---|---|
| Octreotide 30 mg Every 21 Days | 65.1 |
| Octreotide 60 mg Every 28 Days | 72.1 |
Growth hormone (GH) level was the average value measured in 3 blood samples collected at 15 minute intervals at each visit. GH was measured with an automated immunometric assay in a central laboratory. (NCT00372697)
Timeframe: Screening to end of study (Week 24)
| Intervention | µg/L (Mean) |
|---|---|
| Octreotide 30 mg Every 21 Days | -1.7 |
| Octreotide 60 mg Every 28 Days | -2.1 |
Number of participants with improved Leptin regulation from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 1 |
| Placebo Comparator | 2 |
Number of participants with improved Insulin regulation from baseline to 6 months of Octreotide or Placebo therapy. Insulin regulation was measured by immunochemiluminescent assay. (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 2 |
| Placebo Comparator | 0 |
Number of participants with decreased BMI z-score from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 0 |
| Placebo Comparator | 2 |
Number of participants showing a decrease in Fasting total ghrelin from baseline to 6 months of treatment with Octreotide or placebo (NCT00399893)
Timeframe: 6 months
| Intervention | Participants (Number) |
|---|---|
| Octreotide | 1 |
| Placebo Comparator | 1 |
Number of participants who had a decrease in weight from baseline to 6 months of Octreotide or placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 0 |
| Placebo Comparator | 2 |
Number of participants with decreased body-composition as Measured by BOD POD® body composition tracking system from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 2 |
| Placebo Comparator | 3 |
Number of participants with improved Adiponectin regulation from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 2 |
| Placebo Comparator | 2 |
Number of participants with decreased body-composition as Measured by Dual Energy X-ray Absorptiometry (DEXA) scan from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 0 |
| Placebo Comparator | 0 |
Number of participants with improved Peptide YY (PYY) regulation from baseline to 6 months of Octreotide or Placebo therapy (NCT00399893)
Timeframe: 6 months
| Intervention | participants (Number) |
|---|---|
| Octreotide | 1 |
| Placebo Comparator | 1 |
Progression free survival (PFS) is defined as the time from randomization to the date of first documented disease progression or death from any cause. The primary analysis of PFS was based on the independent central adjudicated assessment using Kaplan-Meier method. (NCT00412061)
Timeframe: Time from randomisation to dates of disease progression, death from any cause or last tumor assessment, reported between day of first patient randomised, 10 January 2007, until cut-off date 02 April 2010
| Intervention | Months (Median) |
|---|---|
| Octreotide+ Everolimus | 16.43 |
| Octreotide+ Placebo | 11.33 |
AEs are defined as any unfavorable and unintended diagnosis, symptom, sign (including an abnormal laboratory finding), syndrome or disease which either occurs during study, having been absent at baseline, or, if present at baseline, appears to worsen. SAEs are any untoward medical occurrences that result in death, are life threatening, require (or prolong) hospitalization, cause persistent or significant disability/incapacity, result in congenital anomalies or birth defects, or are other conditions which in judgment of investigators represent significant hazards. (NCT00412061)
Timeframe: From first day of treatment up to 28 days after last day of treatment in double blind
| Intervention | Patients (Number) | |||
|---|---|---|---|---|
| Clinically notable AE | Grade 3-4 Adverse Events | On treatment death | Serious adverse events | |
| Octreotide+ Everolimus | 208 | 162 | 19 | 126 |
| Octreotide+ Placebo | 146 | 109 | 11 | 74 |
The best overall response rate is defined as the percentage of patients having achieved confirmed Complete Response + Partial Response. Complete Response (CR) = at least two determinations of CR at least 4 weeks apart before progression. • Partial response (PR) = at least two determinations of PR or better at least 4 weeks apart before progression. (NCT00412061)
Timeframe: Time from randomisation to dates of disease progression, death from any cause or last tumor assessment, reported between day of first patient randomised, 10 January 2007, until cut-off date 02 April 2010
| Intervention | Percentage of patients (Number) |
|---|---|
| Octreotide+ Everolimus | 2.3 |
| Octreotide+ Placebo | 1.9 |
Overall survival was defined as the time from the date of randomization to the date of death from any cause. If a patient was not known to have died, survival was censored at the date of last contact. Kaplan-Meier methodology was used to estimate the median overall survival for each treatment group. (NCT00412061)
Timeframe: Months 12, 24, 36, 48
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| 12 Months | 24 Months | 36 Months | 48 Months | |
| Octreotide+ Everolimus | 80.5 | 57.0 | 42.9 | 38.0 |
| Octreotide+ Placebo Followed by Open Label Arm | 81.8 | 63.6 | 48.5 | 41.6 |
5-HIAA levels in urine are frequently elevated in patients with advanced carcinoid tumors. Baseline levels of 5-HIAA in urine were defined as 'High' if they exceeded the median value, and 'Low' if they were lower than or equal to the median. (NCT00412061)
Timeframe: If elevated at baseline, evaluated every cycle visit (28 days/cycle) reported between day of first patient randomised, 10 January 2007, until cut-off date 02 April 2010
| Intervention | Months (Median) | |
|---|---|---|
| 5-HIAA <=median (n=93,96) | 5-HIAA > median (n=94,95) | |
| Octreotide+ Everolimus | 21.75 | 13.83 |
| Octreotide+ Placebo | 13.90 | 8.41 |
AEs are defined as any unfavorable and unintended diagnosis, symptom, sign (including an abnormal laboratory finding), syndrome or disease which either occurs during study, having been absent at baseline, or, if present at baseline, appears to worsen. SAEs are any untoward medical occurrences that result in death, are life threatening, require (or prolong) hospitalization, cause persistent or significant disability/incapacity, result in congenital anomalies or birth defects, or are other conditions which in judgment of investigators represent significant hazards. (NCT00412061)
Timeframe: From first day of treatment up to 28 days after last day of treatment in double blind
| Intervention | Patients (Number) | |||
|---|---|---|---|---|
| Clinically notable AE | Grade 3-4 Adverse Events | On treatment death | Serious adverse events | |
| Everolimus Open Label Arm | 154 | 115 | 22 | 93 |
"Serum CgA levels in urine are frequently elevated in patients with advanced carcinoid tumors. Baseline levels of serum CgA were characterized relative to the upper limited of normal (ULN). CgA levels exceeding 2 x ULN were considered to be 'Elevated'; otherwise considered as Non-elevated." (NCT00412061)
Timeframe: If elevated at baseline, evaluated every cycle visit (28 days/cycle) reported between day of first patient randomised, 10 January 2007, until cut-off date 02 April 2010
| Intervention | Months (Median) | |
|---|---|---|
| CgA<=2x ULN (n=60,78) | CgA>2x ULN (n=152,130) | |
| Octreotide+ Everolimus | 31.31 | 13.93 |
| Octreotide+ Placebo | 20.07 | 8.41 |
Scores on the Medical Outcomes Study 36-Item Short-Form General Health Survey (SF-36), version 2. Subjects completed the SF-36 which consists of 8 sub-scales which are additionally summarized into 2 summary components (physical and mental). The subscales and the summary scales both range from 0 to 100, with (0 = worst imaginable, 100 = best imaginable). (NCT00426153)
Timeframe: Baseline, 12 months
| Intervention | units on a scale (Mean) | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical functioning at baseline | Physical functioning at 12 months | Physical role at baseline | Physical role at 12 months | Bodily Pain at baseline | Bodily pain at 12 months | General health at baseline | General health at 12 months | Vitality at baseline | Vitality at 12 months | Social functioning at baseline | Social functioning at 12 months | Emotional role at baseline | Emotional role at 12 month | Mental health at baseline | Mental health at 12 months | Standardized physical component at baseline | Standardized physical component at 12 months | Standardized mental component at baseline | Standardized mental component at 12 month | |
| Octreotide | 74.8 | 77.0 | 59.8 | 74.1 | 67.8 | 75.7 | 55.9 | 53.5 | 49.6 | 54.4 | 79.0 | 82.9 | 82.1 | 91.4 | 76.0 | 76.9 | 42.6 | 44.7 | 50.8 | 52.2 |
| Placebo | 80.4 | 82.1 | 76.8 | 75.0 | 65.5 | 68.7 | 58.0 | 63.4 | 53.9 | 54.6 | 75.0 | 81.3 | 73.8 | 81.0 | 75.4 | 80.7 | 46.0 | 46.1 | 48.4 | 51.3 |
Percent change from baseline in renal volume, measured in milliliters by MRI or CT scans (NCT00426153)
Timeframe: Baseline, 12 months
| Intervention | percent change (Mean) |
|---|---|
| Octreotide | 0.25 |
| Placebo | 8.61 |
Percent change from baseline in renal function/GFR, measured by clearance of iothalamate with monitoring of bladder emptying using ultrasound (NCT00426153)
Timeframe: Baseline, 12 months
| Intervention | percent change (Mean) |
|---|---|
| Octreotide | -5.1 |
| Placebo | -7.2 |
Percent change from baseline in liver volume, measured in milliliters by Magnetic Resonance Imaging (MRI)or Computed Tomography (CT) scans (NCT00426153)
Timeframe: Baseline, 12 months
| Intervention | percent change (Mean) |
|---|---|
| Octreotide | -5.0 |
| Placebo | 0.9 |
Overall survival (OS) is defined as the time from registration until death (event), or censored at last date known alive. OS was estimated using the Kaplan-Meier method , with 95% confidence intervals calculated using Greenwood's formula (NCT00427349)
Timeframe: assessed every 3 months if patient is < 2 years from study entry, then every 6 months up to 5 years
| Intervention | months (Median) |
|---|---|
| AMG 706+Octreotide | 27.5 |
Four-month progression-free survival (PFS) rate is defined as number of patients who are still progression free at 4 months after study entry divided by number of eligible and treated patients enrolled to the study. Progression is evaluated using the Response Evaluation Criteria in Solid Tumors (RECIST) version 1.0, and defined as at least a 20% increase in the sum of the longest diameters of target lesions, taking as reference the smallest sum longest diameter recorded since the baseline measurements, or the appearance of one or more new lesion(s), or unequivocal progression of existing non-target lesions. (NCT00427349)
Timeframe: assessed every 4 weeks while on treatment and at three months post-treatment for participants treated for one cycle, up to month four
| Intervention | percentage of participants (Number) |
|---|---|
| AMG 706+Octreotide | 78.5 |
Tumor response was evaluated using the Response Evaluation Criteria in Solid Tumors (RECIST) version 1.0. Objective response rate is defined as number of patients with complete response (CR) or partial response (PR) divided by the total number of analyzable patients. CR is defined as complete disappearance of all tumor lesions, and partial response is defined as at least a 30% decrease in the sum of the longest diameters of target lesions, taking as reference the baseline sum longest diameter. (NCT00427349)
Timeframe: assessed every 8 weeks while on treatment, and frequency of tumor measurements during follow-up were determined by the treating physician, assessed up to 5 years
| Intervention | percentage of participants (Number) |
|---|---|
| AMG 706+Octreotide | 13.6 |
Serum was batched and IGF and IGFBP levels were assayed at one time at the end of the study using an enzyme-linked immunoabsorbent assay (ELISA) method by Diagnostic Systems Laboratories (Webster, TX). (NCT00510224)
Timeframe: Baseline, 12 weeks
| Intervention | percent change (Median) | |
|---|---|---|
| IGF-1 | IGFBP-1 | |
| Octreotide Acetate | -34.5 | 76.3 |
(NCT00510224)
Timeframe: 12 weeks
| Intervention | Adverse Events (Number) |
|---|---|
| Octreotide Acetate | 0 |
Number of participants with a PSA decline of at least 50% from Baseline during the first 3 cycles of therapy, confirmed by a second measurement at least 2 weeks later. (NCT00510224)
Timeframe: 12 weeks
| Intervention | Participants (Number) |
|---|---|
| Octreotide Acetate | 0 |
Venous sampling was performed at each visit immediately prior to each IM injection. Levels were measured at each visit and mean for the group was calculated after each treatment phase. (NCT00552071)
Timeframe: 3 months
| Intervention | percentage of upper limit of normal (Mean) |
|---|---|
| Ultrasound-guided Injections of Octreotide LAR | 132 |
| Regular Injections of Octreotide LAR | 124 |
Venous sampling was performed at each visit immediately prior to each IM injection. Levels were measured at each visit and mean for the group was calculated after each treatment phase. (NCT00552071)
Timeframe: 3 months
| Intervention | pg/mL (Mean) |
|---|---|
| Ultrasound-guided Injections of Octreotide LAR | 885 |
| Regular Injections of Octreotide LAR | 1167 |
From date of randomization (which is the date of registration) to date of first documentation of progression based on Central Radiological Review of the appropriate CT or MRI scans, or symptomatic deterioration (as defined in Section 10.2e)), or development of new lesions or disease not identified on CT or MRI, or death due to any cause. Patients who have a local assessment of progression based on imaging, but for whom central review does not concur, will be censored at the last Central Radiological Review date, unless subsequent scans or documentation of symptomatic deterioration provides evidence of progression. Patients last known not to have progressed are censored at the date of last contact. Patients with incomplete Central Radiological Review are censored at the date of last Central Radiological Review if patient has not progressed prior to that time. (NCT00569127)
Timeframe: Up to 3 years
| Intervention | months (Median) |
|---|---|
| Octreotide, Bevacizumab | 16.6 |
| Octreotide, Interferon Alpha-2b | 15.4 |
From date of randomization (which is the date of registration) to date of first documentation of progression [per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) as defined in Section 10.2d] or symptomatic deterioration (as defined in Section 10.2e), or death due to any cause. Patients last known not to have progressed are censored at date of last contact. Progression (Section 10.2d) includes one or more of the following: 20% increase in the sum of the longest diameters of target measurable lesions over smallest sum observed using the same techniques as baseline; unequivocal progression of non-measurable disease in the opinion of the treating physician; appearance of new lesion/site; or death due to disease without prior documentation of progression and without symptomatic deterioration. Symptomatic deterioration (Section 10.2e) is global deterioration of health status requiring discontinuation of treatment without objective evidence of progression. (NCT00569127)
Timeframe: Up to 3 years
| Intervention | months (Median) |
|---|---|
| Octreotide, Bevacizumab | 15.4 |
| Octreotide, Interferon Alpha-2b | 10.6 |
From date of registration to date of death due to any cause. Patients last known to be alive are censored at date of last contact. (NCT00569127)
Timeframe: Up to 7 years
| Intervention | months (Median) |
|---|---|
| Octreotide, Bevacizumab | 35.2 |
| Octreotide, Interferon Alpha-2b | 47.3 |
From date of randomization (which is the date of registration) to date of first observation of progressive disease (as defined in Section 10.2d), death due to any cause, symptomatic deterioration (as defined in Section 10.2e), or discontinuation of treatment. This has been calculated using Central-Review based progression events. Patients last known not to have failed treatment are censored at date last known not to have failed. Patients with incomplete Central Radiological Review are censored at the date of last Central Radiological Review if patient has not failed treatment prior to that time. (NCT00569127)
Timeframe: Up to 3 years
| Intervention | months (Median) |
|---|---|
| Octreotide, Bevacizumab | 9.9 |
| Octreotide, Interferon Alpha-2b | 5.6 |
Only adverse events that are possibly, probably or definitely related to study drug are reported. (NCT00569127)
Timeframe: Up to 3 years
| Intervention | Participants (Number) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ALT, SGPT (serum glutamic pyruvic transaminase) | AST, SGOT | Albumin, serum-low (hypoalbuminemia) | Alkaline phosphatase | Allergic reaction/hypersensitivity | Anorexia | Ataxia (incoordination) | Auditory/Ear-Other (Specify) | Bilirubin (hyperbilirubinemia) | CNS cerebrovascular ischemia | Cardiac troponin I (cTnI) | Cardiac-ischemia/infarction | Cardiopulmonary arrest, cause unknown (non-fatal) | Cholecystitis | Cognitive disturbance | Colitis | Constipation | Creatinine | Dehydration | Dental: periodontal disease | Diarrhea | Dizziness | Dyspnea (shortness of breath) | Edema: limb | Fatigue (asthenia, lethargy, malaise) | Fever in absence of neutropenia, ANC lt1.0x10e9/L | Fistula, GI - Colon/cecum/appendix | Fistula, GU - Vagina | Glucose, serum-high (hyperglycemia) | Hearing: pts w/o audiogram not enroll monitor prgm | Heartburn/dyspepsia | Hemoglobin | Hemorrhage, CNS | Hemorrhage, GI - Rectum | Hemorrhage, GI - Upper GI NOS | Hemorrhage, pulmonary/upper respiratory - Nose | Hemorrhage/Bleeding-Other (Specify) | Hot flashes/flushes | Hydrocephalus | Hypertension | Hypotension | Hypoxia | INR (of prothrombin time) | Ileus, GI (functional obstruction of bowel) | Inf (clin/microbio) w/Gr 3-4 neuts - Blood | Inf (clin/microbio) w/Gr 3-4 neuts - Lung | Inf (clin/microbio) w/Gr 3-4 neuts - Nose | Inf w/normal ANC or Gr 1-2 neutrophils - Ab NOS | Inf w/normal ANC or Gr 1-2 neutrophils - Lung | Inf w/normal ANC or Gr 1-2 neutrophils - UTI | Infection with unknown ANC - Scrotum | Infection with unknown ANC - Urinary tract NOS | Insomnia | Left ventricular systolic dysfunction | Leukocytes (total WBC) | Lipase | Lymphopenia | Mental status | Mood alteration - agitation | Mood alteration - anxiety | Mood alteration - depression | Mucositis/stomatitis (clinical exam) - Oral cavity | Mucositis/stomatitis (functional/symp) - Oral cav | Muscle weakness, not d/t neuropathy - body/general | Nausea | Neuropathy: motor | Neutrophils/granulocytes (ANC/AGC) | Obstruction, GI - Gallbladder | Obstruction, GI - Small bowel NOS | Pain - Abdomen NOS | Pain - Back | Pain - Bone | Pain - Chest wall | Pain - Chest/thorax NOS | Pain - Esophagus | Pain - Extremity-limb | Pain - Gallbladder | Pain - Head/headache | Pain - Liver | Pain - Muscle | Pain - Stomach | Pain-Other (Specify) | Phosphate, serum-low (hypophosphatemia) | Platelets | Pneumonitis/pulmonary infiltrates | Potassium, serum-low (hypokalemia) | Proteinuria | Pruritus/itching | Rash/desquamation | Renal failure | Renal/Genitourinary-Other (Specify) | Seizure | Sodium, serum-low (hyponatremia) | Somnolence/depressed level of consciousness | Syncope (fainting) | Thrombosis/embolism (vascular access-related) | Thrombosis/thrombus/embolism | Triglyceride, serum-high (hypertriglyceridemia) | Ulcer, GI - Duodenum | Ulcer, GI - Stomach | Uric acid, serum-high (hyperuricemia) | Vasculitis | Vessel injury-artery - Aorta | Vision-blurred vision | Vomiting | Weight loss | |
| Octreotide, Bevacizumab | 0 | 1 | 0 | 2 | 1 | 1 | 2 | 0 | 1 | 1 | 1 | 1 | 0 | 2 | 1 | 1 | 1 | 1 | 3 | 1 | 7 | 2 | 1 | 4 | 13 | 0 | 1 | 1 | 2 | 0 | 1 | 0 | 2 | 1 | 1 | 1 | 1 | 0 | 1 | 62 | 2 | 1 | 1 | 1 | 0 | 1 | 0 | 1 | 2 | 1 | 1 | 1 | 0 | 1 | 2 | 0 | 3 | 1 | 0 | 0 | 1 | 0 | 1 | 0 | 5 | 1 | 0 | 1 | 2 | 7 | 1 | 0 | 2 | 2 | 1 | 1 | 0 | 9 | 0 | 1 | 0 | 1 | 1 | 3 | 1 | 1 | 17 | 0 | 1 | 0 | 2 | 0 | 1 | 3 | 2 | 3 | 3 | 0 | 1 | 1 | 1 | 0 | 1 | 0 | 4 | 2 |
| Octreotide, Interferon Alpha-2b | 4 | 6 | 1 | 6 | 0 | 8 | 0 | 1 | 1 | 0 | 0 | 0 | 1 | 0 | 1 | 0 | 1 | 0 | 5 | 0 | 9 | 3 | 2 | 1 | 50 | 1 | 0 | 0 | 5 | 1 | 0 | 4 | 0 | 0 | 0 | 0 | 0 | 1 | 0 | 4 | 0 | 0 | 0 | 0 | 1 | 0 | 1 | 0 | 1 | 2 | 0 | 0 | 1 | 0 | 14 | 1 | 5 | 1 | 2 | 1 | 7 | 1 | 0 | 3 | 9 | 1 | 23 | 0 | 1 | 5 | 2 | 1 | 1 | 2 | 0 | 1 | 1 | 3 | 1 | 1 | 1 | 1 | 0 | 0 | 1 | 1 | 1 | 1 | 1 | 1 | 0 | 2 | 0 | 1 | 1 | 1 | 1 | 1 | 0 | 0 | 0 | 1 | 0 | 1 | 2 | 3 |
Per Response Evaluation Criteria in Solid Tumors Criteria (RECIST v1.0): Complete Response (CR) is disappearance of all measurable and non-measurable disease, and no new lesions; Partial Response (PR) is greater than or equal to 30% decrease under baseline of the sum of longest diameters of all target measurable lesions, no unequivocal progression of non-measurable disease, and no new lesions. Confirmed response is two or more objective statuses of CR a minimum of four weeks apart documented before progression or symptomatic deterioration. Partial response is two or more objective statuses of PR or better a minimum of four weeks apart documented before progression or symptomatic deterioration. Unconfirmed CR is one objective status of CR documented before progression or symptomatic deterioration but not qualifying as CR or PR. Unconfirmed PR is one objective status of PR documented before progression or symptomatic deterioration but not qualifying as CR, PR or unconfirmed CR. (NCT00569127)
Timeframe: Up to 3 years
| Intervention | participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Complete Response | Partial Response | Unconfirmed Complete Response | Unconfirmed Partial Response | Stable/No Resposne | Increasing Disease | Symptomatic Deterioration | Assessment Inadequate | |
| Octreotide, Bevacizumab | 2 | 20 | 0 | 7 | 135 | 20 | 0 | 16 |
| Octreotide, Interferon Alpha-2b | 0 | 8 | 1 | 6 | 137 | 30 | 3 | 17 |
Lesions that can be accurately measured in at least one dimension (longest diameter (LD) to be recorded) as > 20 mm with conventional techniques (CT, MRI) or as > 10 mm with spiral CT scan. All measurable lesions up to maximum of 5 lesions per organ and 10 lesions in total representative of all involved organs should be identified as target lesions and recorded and measured at baseline. Complete Response is defined as Disappearance of all target lesions. Partial Response is defined at least a 30% decrease in the sum of LD of target lesions taking as reference the baseline sum LD. (NCT00582426)
Timeframe: Day 56, Day 84, Day 112, Day 140, Day 168
| Intervention | Percentage of Participants (Number) | ||||
|---|---|---|---|---|---|
| Day 56 (N=11,2) | Day 84 (N=5,3) | Day 112 (N=1,1) | Day 140 (N=9,1) | Day 168 (N=2,1) | |
| Octreotide Long Acting Release | 45.5 | 60.0 | 100 | 44.4 | 100 |
| Standard Treatment | 0.0 | 100 | 0.0 | 100 | 100 |
Mean number of episodes of diarrhea is evaluated by patient diaries recorded by cycle. (cycle 1 to cycle 7.) (NCT00582426)
Timeframe: at each cycle (28 days per cycle)
| Intervention | Episodes/patient/cycle (Mean) | ||||||
|---|---|---|---|---|---|---|---|
| Cycle 1 (n=20, 18) | Cycle 2 (n=36,38) | Cycle 3 (n=33,39) | Cycle 4 (n=24, 27) | Cycle 5 (n=20,29) | Cycle 6 (n=22, 22) | Cycle 7 (n= 16, 20) | |
| Octreotide Long Acting Release | 2.6 | 8.2 | 6.9 | 8.6 | 8.1 | 6.1 | 4.8 |
| Standard Treatment | 2.2 | 5.9 | 6.7 | 7.1 | 7 | 5.8 | 6.6 |
(NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of Participants (Number) |
|---|---|
| Octreotide Long Acting Release | 4.5 |
| Standard Treatment | 7.0 |
(NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of patients (Number) |
|---|---|
| Octreotide Long Acting Release | 6 |
| Standard Treatment | 4.2 |
Grade (severity)of episodes of diarrhea is evaluated by patient diaries recorded on a daily basis by considering only worse grade of diarrhea for each patient. Diarrhea was graded according to Common Toxicity Criteria where Grade 1 = Increase of <4 stools/day over pretreatment, Grade 2 = Increase of 4-6 stools/day, or nocturnal stools, Grade 3 = Increase of ≥7 stools/day or incontinence;or need for parenteral support for dehydration and Grade 4= Physiologic consequences requiring intensive care; or hemodynamic collapse. (NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of Episodes (Number) | |||
|---|---|---|---|---|
| Grade 1 | Grade 2 | Grade 3 | Grade 4 | |
| Octreotide Long Acting Release | 65.4 | 23.3 | 11.3 | 0 |
| Standard Treatment | 66.9 | 27.2 | 5.9 | 0 |
Grade (severity) of episodes of diarrhea is evaluated by patient diaries recorded on a daily basis by considering only worse grade of diarrhea for each patient. Diarrhea was graded according to Common Toxicity Criteria where Grade 0 = None, 1 = Increase of <4 stools/day over pretreatment, Grade 2 = Increase of 4-6 stools/day, or nocturnal stools, Grade 3 = Increase of ≥7 stools/day or incontinence; or need for parenteral support for dehydration and Grade 4= Physiologic consequences requiring intensive care; or hemodynamic collapse. (NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| Grade 1 | Grade 2 | Grade 3 | Grade 4 | |
| Octreotide Long Acting Release | 41.2 | 25.5 | 33.3 | 0 |
| Standard Treatment | 26.8 | 51.8 | 21.4 | 0 |
(NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of Participants (Number) |
|---|---|
| Octreotide Long Acting Release | 1.5 |
| Standard Treatment | 1.4 |
For patient, chemotherapy dose reduction due to diarrhea as counted each time it occurred. Chemotherapy dose reduction because of other adverse events related to chemotherapy was not considered. (NCT00582426)
Timeframe: 6 months overall
| Intervention | Percentage of participants (Number) |
|---|---|
| Octreotide Long Acting Release | 26.9 |
| Standard Treatment | 11.3 |
Number of episodes of diarrhea is evaluated by patient diaries recorded on a daily basis. (NCT00582426)
Timeframe: 6 months overall
| Intervention | Episodes/patients/day (Mean) |
|---|---|
| Octreotide Long Acting Release | 21.6 |
| Standard Treatment | 20.4 |
The percentage of patients developing diarrhea (incidence of grade 1 to 4) during treatment, considering only the worst grade of diarrhea for each patient. Diarrhea was graded according to Common Toxicity Criteria where Grade 0=None, 1 = Increase of <4 stools/day over pretreatment, Grade 2 = Increase of 4-6 stools/day, or nocturnal stools, Grade 3 = Increase of ≥7 stools/day or incontinence; or need for parenteral support for dehydration and Grade 4= Physiologic consequences requiring intensive care; or hemodynamic collapse. (NCT00582426)
Timeframe: 6 month overall
| Intervention | Percentage of Participants (Number) |
|---|---|
| Octreotide Long Acting Release | 76.1 |
| Standard Treatment | 78.9 |
Quality of life (QoL) is evaluated using FACIT-D scale. FACIT-D is composed of 38 items, whose responses range from 0 to 4. The total FACIT-D score may range from 0 to 152. The 38 items compose five subscales, each evaluating a different component of the (QOL). For calculating the subscale score, some items are computed in a reverse fashion, so that higher FACIT-D scores indicate a better (QoL). Descriptive statistics (mean, standard deviation, median, minimum and maximum) are used to summarize FACIT-D scores (total and subscales) by study group at each time point. (NCT00582426)
Timeframe: Baseline to Day 168
| Intervention | Units on a scale (Mean) |
|---|---|
| Octreotide Long Acting Release | 0.5 |
| Standard Treatment | 3.4 |
"Percentage of participants with a reduction of mean GH levels to <2.5μg/L (based on a 5-point 2-hour profile) and normalization of sex- and age-adjusted IGF-1.~Post surgery = patients with prior surgery but no previous medical treatment for acromegaly De novo = patients with de novo disease who refused pituitary surgery or for whom pituitary surgery was contraindicated." (NCT00600886)
Timeframe: 12 months
| Intervention | Percentage of Participants (Number) | ||
|---|---|---|---|
| Overall | Post Surgery | De novo | |
| Octreotide LAR (Core) | 19.2 | 21.8 | 17.3 |
| Pasireotide LAR (Core) | 31.3 | 39.4 | 25.7 |
Percentage of participants with normalization of sex- and age-adjusted IGF-1. Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). Denominator for time points up to Month 12 is the FAS. Denominator for time points after Month 12 excludes patients who completed the core and did not enter the extension. Patients who discontinued were considered non-responders for the time points after discontinuation, patients who crossed over were considered non-responders for all time points after crossover. (NCT00600886)
Timeframe: Months 3, 6, 9, 12, 16, 19, 22, 25
| Intervention | Percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| M3 | M6 | M9 | M12 | M16 | M19 | M22 | M25 | |
| Octreotide LAR (Core & Extension) | 25.3 | 24.2 | 28.0 | 22.0 | 13.7 | 15.7 | 17.0 | 14.4 |
| Pasireotide LAR (Core & Extension) | 35.2 | 35.8 | 34.1 | 35.8 | 29.9 | 25.2 | 25.9 | 25.9 |
Percentage of participants with normalization of sex- and age-adjusted IGF-1. Post surgery = patients with prior surgery but no previous medical treatment for acromegaly De novo = patients with de novo disease who refused pituitary surgery or for whom pituitary surgery was contraindicated. (NCT00600886)
Timeframe: 12 Months
| Intervention | Percentage of participants (Number) | ||
|---|---|---|---|
| Overall | Post surgery | De novo | |
| Octreotide LAR (Core) | 23.6 | 26.9 | 21.2 |
| Pasireotide LAR (Core) | 38.6 | 50.7 | 30.5 |
Percentage of participants with normalization of sex- and age-adjusted IGF-1. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). Denominator for all time points is the Crossover Analysis Set (CAS). (NCT00600886)
Timeframe: Months 3, 6, 9, 12 after crossover
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| M3 after crossover | M6 after crossover | M9 after crossover | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 7.9 | 7.9 | 10.5 | 5.3 |
| Crossed Over to Pasireotide LAR (Extension) | 19.8 | 30.9 | 29.6 | 27.2 |
Ring size (based on jeweler's finger gauge). Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, Months 12, 25
| Intervention | ring zize (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Baseline left hand (LH) 4th digit | Baseline left hand 5th digit | Baseline right hand (RH) 4th digit | Baseline right hand 5th digit | M12 LH 4th digit | M12 LH 5th digit | M12 RH 4th digit | M12 RH 5th digit | M25 LH 4th digit | M25 LH 5th digit | M25 RH 4th digit | M25 RH 5th digit | |
| Octreotide LAR (Core & Extension) | 11.8 | 12.4 | 11.4 | 11.3 | 11.1 | 12.4 | 11.3 | 10.5 | 11.1 | 14.3 | 10.9 | 7.5 |
| Pasireotide LAR (Core & Extension) | 11.6 | 11.7 | 12.5 | 11.2 | 10.6 | 11.8 | 12.2 | 10.7 | 10.1 | 10.0 | 11.8 | 7.8 |
Ring size (based on jeweler's finger gauge). Extension baseline was defined as last measurement prior to the start of crossover treatment. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). BL = baseline, LH = left hand, RH = right hand, CO = crossover (NCT00600886)
Timeframe: Extension baseline, month 12 after crossover
| Intervention | ring size (Mean) | |||||
|---|---|---|---|---|---|---|
| Ext. BL LH 4th digit | Ext. BL LH 5th digit | Ext. BL RH 4th digit | M12 after CO LH 4th digit | M12 after CO LH 5th digit CO | M12 after CO RH 4th digit | |
| Crossed Over to Octreotide LAR (Extension) | 11.0 | 12.3 | 12.4 | 11.2 | 12.5 | 11.4 |
Ring size (based on jeweler's finger gauge). Extension baseline was defined as last measurement prior to the start of crossover treatment. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). BL = baseline, LH = left hand, RH = right hand, CO = crossover (NCT00600886)
Timeframe: Extension baseline, month 12 after crossover
| Intervention | ring size (Mean) | |||||||
|---|---|---|---|---|---|---|---|---|
| Ext. BL LH 4th digit | Ext. BL LH 5th digit | Ext. BL RH 4th digit | Ext. BL RH 5th digit | M12 after CO LH 4th digit | M12 after CO LH 5th digit CO | M12 after CO RH 4th digit | M12 after CO RH 5th digit | |
| Crossed Over to Pasireotide LAR (Extension) | 11.2 | 11.6 | 11.4 | 10.7 | 10.9 | 11.9 | 11.6 | 11.5 |
Severity scores of acromegaly symptoms (Headache, Fatigue, Perspiration, Paresthesias, Osteoarthralgia). Symptoms were scored from 0 (no symptom) to 4 (very severe). Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, Months 12, 25
| Intervention | scores on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Headache - Baseline | Fatigue - Baseline | Perspiration - Baseline | Paresthesia - Baseline | Osteoarthraliga - Baseline | Headache - M12 | Fatigue - M12 | Perspiration - M12 | Paresthesia - M12 | Osteoarthraliga - M12 | Headache - M25 | Fatigue - M25 | Perspiration - M25 | Paresthesia - M25 | Osteoarthraliga - M25 | |
| Octreotide LAR (Core & Extension) | 1.0 | 1.4 | 1.3 | 0.8 | 1.3 | 0.6 | 0.7 | 0.5 | 0.4 | 0.7 | 0.6 | 0.7 | 0.4 | 0.4 | 0.8 |
| Pasireotide LAR (Core & Extension) | 0.9 | 1.2 | 1.1 | 0.7 | 1.0 | 0.5 | 0.8 | 0.4 | 0.3 | 0.5 | 0.4 | 0.5 | 0.4 | 0.2 | 0.4 |
"Severity scores of acromegaly symptoms (Headache, Fatigue, Perspiration, Paresthesias, Osteoarthralgia).~Symptoms were scored from 0 (no symptom) to 4 (very severe). Extension baseline was defined as last measurement prior to the start of crossover treatment. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over)." (NCT00600886)
Timeframe: Extension baseline, month 12 after crossover
| Intervention | scores on a scale (Mean) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Headache: Ext. BL | Headache: M12 after crossover | Fatigue: Ext. BL | Fatigue: M12 after crossover | Perspiration: Ext. BL | Perspiration: M12 after crossover | Paresthesia: Ext. BL | Paresthesia: M12 after crossover | Osteoarthralgia: Ext. BL | Osteoarthralgia: M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 0.4 | 0.7 | 0.7 | 0.7 | 0.6 | 0.5 | 0.4 | 0.4 | 0.6 | 0.7 |
| Crossed Over to Pasireotide LAR (Extension) | 0.6 | 0.5 | 0.8 | 0.8 | 0.5 | 0.6 | 0.4 | 0.3 | 0.6 | 0.5 |
Mean GH levels (based on a 5-point profile over 2 hours). Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, Months 3, 6, 9, 12, 16, 19, 22, 25
| Intervention | μg/L (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline | Month 3 | Month 6 | Month 9 | Month 12 | Month 16 | Month 19 | Month 22 | Month 25 | |
| Octreotide LAR (Core & Extension) | 18.8 | 5.8 | 5.2 | 4.3 | 4.5 | 1.4 | 1.5 | 1.4 | 1.2 |
| Pasireotide LAR (Core & Extension) | 21.9 | 6.3 | 5.6 | 4.9 | 4.6 | 2.3 | 2.1 | 2.1 | 2.0 |
Mean GH levels (based on a 5-point profile over 2 hours). Extension baseline was defined as last measurement prior to the start of crossover treatment. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). (NCT00600886)
Timeframe: Extension baseline, months 3, 6, 9, 12 after crossover
| Intervention | μg/L (Mean) | ||||
|---|---|---|---|---|---|
| Ext. Baseline | M3 after crossover | M6 after crossover | M9 after crossover | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 7.1 | 9.8 | 9.8 | 8.7 | 10.4 |
| Crossed Over to Pasireotide LAR (Extension) | 5.9 | 5.9 | 4.8 | 2.6 | 2.5 |
Prolactin Levels. Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, Months 12, 25
| Intervention | μg/L (Mean) | ||
|---|---|---|---|
| Baseline | M12 | M25 | |
| Octreotide LAR (Core & Extension) | 15.8 | 11.7 | 6.7 |
| Pasireotide LAR (Core & Extension) | 20.6 | 8.9 | 5.4 |
Prolactin (PRL) levels. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). Extension baseline was defined as last measurement prior to the start of crossover treatment. (NCT00600886)
Timeframe: Extension baseline, month 12 after crossover
| Intervention | μg/L (Mean) | |
|---|---|---|
| Ext. Baseline | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 15.7 | 16.1 |
| Crossed Over to Pasireotide LAR (Extension) | 11.9 | 7.5 |
Octreotide LAR trough concentrations by incident dose (last dose administered prior to PK sample collection). PK observations with missing concentrations, missing dose, missing elapsed time or an elapsed time from previous injection outside of 28±2 days window were excluded. (NCT00600886)
Timeframe: Months 1 - 12
| Intervention | ng/mL (Mean) | |||||
|---|---|---|---|---|---|---|
| M2 | M3 | M4 | M6 | M7 | M12 | |
| Octreotide LAR 10mg | 0.61 | 0.62 | 0.19 | 1.33 | 0.70 | 0.30 |
"The duration of response is defined as the time from the date that patient first met and maintained the response criteria based on primary efficacy variable to the date that patient lost response status.~Median and corresponding 95% CI are derived based on Kaplan-Meier method. Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included)." (NCT00600886)
Timeframe: Up to 26 months
| Intervention | Weeks (Median) |
|---|---|
| Pasireotide LAR (Core & Extension) | 64.4 |
| Octreotide LAR (Core & Extension) | 64.6 |
Time to first response for patients achieving a reduction of mean GH level to < 2.5 μg/L and normalization of IGF-1. Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Up to 26 months
| Intervention | Weeks (Median) |
|---|---|
| Pasireotide LAR (Core & Extension) | 12.6 |
| Octreotide LAR (Core & Extension) | 12.4 |
Percentage change from baseline in tumor volume (assessed by pituitary MRI). Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, months 6, 12, 19, 25
| Intervention | mm^3 (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Baseline | M6 | M12 | M19 | M25 | % change at M6 | % change at M12 | % change at M19 | % change at M25 | |
| Octreotide LAR (Core & Extension) | 2259.2 | 1565.4 | 1390.4 | 1009.9 | 814.1 | -28.8 | -38.0 | -47.2 | -55.0 |
| Pasireotide LAR (Core & Extension) | 2420.7 | 1614.1 | 1482.4 | 956.6 | 840.4 | -29.9 | -39.7 | -48.9 | -51.8 |
Absolute and percentage change from baseline in tumor volume (assessed by pituitary MRI) Post surgery = patients with prior surgery but no previous medical treatment for acromegaly De novo = patients with de novo disease who refused pituitary surgery or for whom pituitary surgery was contraindicated. (NCT00600886)
Timeframe: Baseline, 12 Months
| Intervention | mm^3 (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Overall at baseline | Overall % change at month 12 | Post surgery at baseline | Post surgery % change at month 12 | De novo at baseline | De novo % change at month 12 | Overall absolute change at month 12 | Post surgery abs. change at month 12 | De novo absolute change at month 12 | |
| Octreotide LAR (Core) | 2259.2 | -38.0 | 2196.5 | -39.0 | 2308.1 | -37.2 | -801.2 | -713.8 | -867.1 |
| Pasireotide LAR (Core) | 2420.7 | -39.7 | 2185.2 | -39.5 | 2592.4 | -39.9 | -987.1 | -873.7 | -1051.9 |
"Percentage change from extension baseline in tumor volume (assessed by pituitary MRI).~Extension baseline was defined as last assessment prior to the administration of the new treatment after crossover. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over)." (NCT00600886)
Timeframe: Extension baseline, months 6, 12 after crossover
| Intervention | mm^3 (Mean) | ||||
|---|---|---|---|---|---|
| Ext. Baseline | Value at M6 after crossover | % change - M6 after crossover | Value at M12 after crossover | % change - M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 1809.6 | 1794.9 | -12.3 | 1610.4 | -17.9 |
| Crossed Over to Pasireotide LAR (Extension) | 1420.9 | 1027.5 | -18.1 | 949.0 | -24.7 |
Acromegalyy quality of life (AcroQoL) total scores. The AcroQoL questionnaire is unidimensional and contains 22 items divided in two scales: one that evaluates physical aspects (eight items) and another one that evaluates psychological aspects (14 items). 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. Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). (NCT00600886)
Timeframe: Baseline, Months 12, 25
| Intervention | Score on a scale (Mean) | ||
|---|---|---|---|
| Baseline | M12 | M25 | |
| Octreotide LAR (Core & Extension) | 55.6 | 61.6 | 62.9 |
| Pasireotide LAR (Core & Extension) | 58.4 | 65.7 | 69.3 |
AcroQoL total scores. The AcroQoL questionnaire is unidimensional and contains 22 items divided in two scales: one that evaluates physical aspects (eight items) and another one that evaluates psychological aspects (14 items). The scoring of the questionnaire was performed as specified by the instrument developers. Extension baseline was defined as last measurement prior to the start of crossover treatment. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). Total scores range from 0 to 100. Higher scores represent better quality of life. (NCT00600886)
Timeframe: Extension baseline, months 12 after crossover
| Intervention | scores on a scale (Mean) | |
|---|---|---|
| Ext. Baseline | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 59.8 | 61.2 |
| Crossed Over to Pasireotide LAR (Extension) | 58.9 | 60.3 |
Octreotide LAR trough concentrations by incident dose (last dose administered prior to PK sample collection). PK observations with missing concentrations, missing dose, missing elapsed time or an elapsed time from previous injection outside of 28±2 days window were excluded. (NCT00600886)
Timeframe: Months 1 - 12
| Intervention | ng/mL (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| M1 | M2 | M3 | M4 | M5 | M6 | M7 | M8 | M9 | M10 | M11 | M12 | |
| Octreotide LAR 20 mg | 0.86 | 1.21 | 1.29 | 1.45 | 1.65 | 1.58 | 1.46 | 1.55 | 1.74 | 1.66 | 1.74 | 1.58 |
Octreotide LAR trough concentrations by incident dose (last dose administered prior to PK sample collection). PK observations with missing concentrations, missing dose, missing elapsed time or an elapsed time from previous injection outside of 28±2 days window were excluded. (NCT00600886)
Timeframe: Months 1 - 12
| Intervention | ng/mL (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| M4 | M5 | M6 | M7 | M8 | M9 | M10 | M11 | M12 | |
| Octreotide LAR 30 mg | 1.55 | 2.14 | 2.12 | 2.14 | 2.16 | 2.20 | 2.50 | 2.39 | 2.55 |
"Pasireotide LAR trough concentrations by incident dose (last dose administered prior to PK sample collection). PK observations with missing concentrations, missing dose, missing elapsed time or an elapsed time from previous injection outside of 28±2 days window were excluded.~5 patients with evaluable PK data in the pasireotide arm received erroneously 20 mg pasireotide LAR at baseline." (NCT00600886)
Timeframe: Months 1 - 12
| Intervention | ng/mL (Mean) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| M1 | M2 | M3 | M4 | M5 | M6 | M7 | M8 | M9 | M10 | M11 | M12 | |
| Pasireotide LAR 20 mg | 4.65 | 2.88 | 3.39 | 3.93 | 5.22 | 2.87 | 2.29 | 3.65 | 4.80 | 5.66 | 5.10 | 4.54 |
| Pasireotide LAR 40 mg | 6.65 | 7.81 | 8.70 | 9.51 | 10.92 | 10.59 | 11.85 | 12.33 | 12.75 | 12.42 | 12.62 | 11.11 |
"Pasireotide LAR trough concentrations by incident dose (last dose administered prior to PK sample collection). PK observations with missing concentrations, missing dose, missing elapsed time or an elapsed time from previous injection outside of 28±2 days window were excluded.~5 patients with evaluable PK data in the pasireotide arm received erroneously 20 mg pasireotide LAR at baseline." (NCT00600886)
Timeframe: Months 1 - 12
| Intervention | ng/mL (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| M4 | M5 | M6 | M7 | M8 | M9 | M10 | M11 | M12 | |
| Pasireotide LAR 60mg | 13.48 | 13.42 | 13.08 | 14.76 | 15.88 | 16.03 | 16.01 | 16.31 | 16.16 |
"Percentage of participants with a reduction of mean GH levels to < 2.5μg/L (based on a 5-point 2-hour profile).~Analysis was based on data up to crossover (i.e., included data from both blinded core and extension phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included). Denominator for time points up to Month 12 is the Full Analysis Set. Denominator for time points after Month 12 excludes patients who completed the core and did not enter the extension. Patients who discontinued were considered non-responders for the time points after discontinuation, patients who crossed over were considered non-responders for all time points after crossover." (NCT00600886)
Timeframe: Months 3, 6, 9, 12, 16, 19, 22, 25
| Intervention | Percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| M3 | M6 | M9 | M12 | M16 | M19 | M22 | M25 | |
| Octreotide LAR (Core & Extension) | 43.4 | 47.8 | 46.2 | 47.3 | 22.2 | 21.6 | 22.2 | 24.2 |
| Pasireotide LAR (Core & Extension) | 49.4 | 45.5 | 42.6 | 43.2 | 33.3 | 36.7 | 35.4 | 35.4 |
"Percentage of participants with a reduction of mean GH levels to < 2.5μg/L (based on a 5-point 2-hour profile).~Post surgery = patients with prior surgery but no previous medical treatment for acromegaly De novo = patients with de novo disease who refused pituitary surgery or for whom pituitary surgery was contraindicated." (NCT00600886)
Timeframe: 12 Months
| Intervention | Percentage of participants (Number) | ||
|---|---|---|---|
| Overall | Post surgery | De novo | |
| Octreotide LAR (Core) | 51.6 | 51.3 | 51.9 |
| Pasireotide LAR (Core) | 48.3 | 52.1 | 45.7 |
Percentage of participants with a reduction of mean GH levels to < 2.5μg/L (based on a 5-point 2-hour profile). Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). Denominator for all time points is the Crossover Analysis Set (CAS). (NCT00600886)
Timeframe: Months 3, 6, 9, 12 after crossover
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| M3 after crossover | M6 after crossover | M9 after crossover | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 28.9 | 31.6 | 31.6 | 23.7 |
| Crossed Over to Pasireotide LAR (Extension) | 49.4 | 43.2 | 54.3 | 44.4 |
"Percentage of participants with a reduction of mean GH levels to < 2.5μg/L (based on a 5-point 2-hour profile) and normalization of sex- and age-adjusted IGF-1.~Denominator for time points up to Month 12 is the Full Analysis Set (FAS). Denominator for time points after Month 12 excludes patients who completed the core and did not enter the extension. Patients who discontinued were considered non-responders for the time points after discontinuation, patients who crossed over were considered non-responders for all time points after crossover. Analysis was based on data up to crossover (i.e., included data from both blinded core & ext. phase up to 26 Months for patients who continued the same treatment in the extension. For patients who switched to the other treatment, only data collected before crossover was included.)" (NCT00600886)
Timeframe: Months 3, 6, 9, 12, 16, 19, 22, 25
| Intervention | Percentage of participants (Number) | |||||||
|---|---|---|---|---|---|---|---|---|
| Month 3 | Month 6 | Month 9 | Month 12 | Month 16 | Month 19 | Month 22 | Month 25 | |
| Octreotide LAR (Core & Extension) | 21.4 | 19.8 | 23.1 | 17.6 | 12.4 | 13.7 | 16.3 | 13.7 |
| Pasireotide LAR (Core & Extension) | 30.1 | 30.1 | 27.8 | 29.0 | 25.2 | 23.1 | 25.2 | 24.5 |
Percentage of participants with a reduction of mean GH levels to < 2.5μg/L (based on a 5-point 2-hour profile) and normalization of sex- and age-adjusted IGF-1. Analysis was based on data after crossover (i.e., included data from blinded extension phase collected after the crossover time point for patients who crossed over). Denominator for all time points is the Crossover Analysis Set (CAS). (NCT00600886)
Timeframe: Months 3, 6, 9, 12 after crossover
| Intervention | Percentage of participants (Number) | |||
|---|---|---|---|---|
| M3 after crossover | M6 after crossover | M9 after crossover | M12 after crossover | |
| Crossed Over to Octreotide LAR (Extension) | 2.6 | 2.6 | 5.3 | 0.0 |
| Crossed Over to Pasireotide LAR (Extension) | 17.3 | 21.0 | 22.2 | 17.3 |
Baseline evaluations were to include Triphasic CT scan or MRI of the abdomen. Triphasic CT or MRIs were to be read by same radiologist at each assessment, measuring the same target and non-target lesions and accounting for all lesions that were present at Baseline. All known disease was accounted for when assessing objective tumor status. Current objective tumor status was to be captured on Tumor Assessment CRF. Objective response rate was defined by RECIST criteria: Partial response (PR) must have ≥ 30% decrease in the sum of longest diameter of all target lesions, from the baseline sum. Complete response (CR) must have disappearance of all target and non-target lesions. For CR or PR, tumor measurements must be confirmed by 2nd assessments within 4 weeks. Progression = 20% increase in the sum of longest diameter of all target lesions, from smallest sum of longest diameter of all target lesions recorded at or after baseline; or a new lesion; or progression of non-target lesions. (NCT00690430)
Timeframe: Month 6
| Intervention | Percentage of Participants (Number) |
|---|---|
| Pasireotide LAR | 2.0 |
| Octreotide LAR | 3.8 |
Disease control rate (DCR) is the proportion of patients with a best overall response of Complete Response (CR) or Partial Response (PR) or Stable Disease (SD). Complete Response (CR): Disappearance of all target lesions Partial Response (PR): At least a 30% decrease in the sum of the longest diameter of all target lesions, taking as reference the baseline sum of the longest diameters. Progressive Disease (PD): At least a 20% increase in the sum of the longest diameter of all measured target lesions, taking as reference the smallest sum of longest diameter of all target lesions recorded at or after baseline, or a new lesion; or progression of non-target lesions. Stable Disease (SD): Neither sufficient shrinkage to qualify for PR or CR nor an increase in lesions which would qualify for PD. Unknown (UNK) Progression has not been documented and one or more target lesions have not been assessed or have been assessed using a different method than baseline. (NCT00690430)
Timeframe: Month 6
| Intervention | Percentage of participants (Number) |
|---|---|
| Pasireotide LAR | 62.7 |
| Octreotide LAR | 46.2 |
Percent change from Baseline in mean daily bowel movements at Month 6 were compared between the two treatment groups using ANCOVA model with treatment as the main effect and symptom levels at Baseline (e.g. mean daily bowel movement at Baseline) and randomization stratum (D+F or D) as covariates. Percentage change = (Month 6 - baseline)/baseline. (NCT00690430)
Timeframe: 6 months
| Intervention | Percentage of Episodes (Mean) | ||
|---|---|---|---|
| Diarrhea and Flushing (N=24, 28) | Predominantly Diarrhea (D) (N=2, 4) | Overall (N=26, 32) | |
| Octreotide LAR | -38.4 | -22.9 | -36.5 |
| Pasireotide LAR | -23.5 | -44.2 | -25.1 |
Percent change from Baseline in total number of flushing episodes comprising Month 6 were compared between the two treatment groups using ANCOVA model with treatment as the main effect and symptom levels at Baseline (e.g. total number of flushing episodes at Baseline) and randomization stratum (D+F or F) as covariates. (NCT00690430)
Timeframe: 6 months
| Intervention | Percentage of Episodes (Mean) | ||
|---|---|---|---|
| Diarrhea and Flushing (N=24, 28) | Predominately Flushing (N=4, 1) | Overall (N=28, 29) | |
| Octreotide LAR | -52.8 | 47.2 | -49.4 |
| Pasireotide LAR | -41.0 | -48.4 | -42.1 |
Percentage of patients who received clinical benefit in symptom (diarrhea and/or flushing) improvement as: Diarrhea (D)+Flushing (F): Patients with a daily mean number (#) of at least four bowel movements and a total of five or more flushing episodes. Clinical Benefit Response Criteria (CBRC): <4 daily mean bowel movements AND at least 20% reduction from Baseline in the daily mean # of bowel movements AND any reduction in the total # of flushing episodes compared with Baseline. (D) Patients with a daily mean # of at least four bowel movements and a total # of <5 flushing episodes. (CBRC) <4 daily mean bowel movements AND at least a 20% reduction from Baseline in the daily mean # of bowel movements. (F) Patients with a total # of at least 14 flushing episodes and a daily mean # of <4 bowel movements (CBRC) At least a 30% reduction from Baseline in the total # of flushing episodes. (NCT00690430)
Timeframe: Month 6
| Intervention | Percentage of Participants (Number) | |||
|---|---|---|---|---|
| Diarrhea and Flushing (N=37, 39) | Diarrhea (N=2, 5) | Flushing (N=4, 1) | Overall (N=43, 45) | |
| Octreotide LAR | 28.2 | 20.0 | 0.0 | 26.7 |
| Pasireotide LAR | 13.5 | 100 | 50 | 20.9 |
Modified ORR is defined as CR+ PR + MR. According to RECIST v1.0, CR was defined as the disappearance of all target and non-target lesions; PR defined as a >30% decrease in the sum of the longest diameters (LD) of the target lesions, taking as reference the baseline sum of the LD and MR defined as 20% - 29% reduction. Disease progression defined as at least a 20% increase in the sum of the longest diameters of target lesions, taking as reference the smallest sum longest diameter recorded since the baseline measurements, and/or the appearance of one or more new lesion(s), and/or unequivocal progression of existing nontarget lesions. (NCT00781911)
Timeframe: From Start of Treatment Baseline to Disease Progression (Up to 18 Months)
| Intervention | percentage of participants (Number) |
|---|---|
| Carcinoid Tumor | 3.2 |
| Islet Cell Carcinoma | 0 |
Number of participants that had at least one TEAE is presented. A summary of other non-serious adverse events and all serious adverse events, regardless of causality, is located in the Reported Adverse Events Section. (NCT00781911)
Timeframe: 18 months
| Intervention | Participants (Count of Participants) |
|---|---|
| Carcinoid Tumor | 31 |
| Islet Cell Carcinoma | 12 |
Determine the biochemical response rate (≥ 50% reduction in tumor-specific markers; may include, not limited to 24 hour urine 5-hydroxyindoleacetic acid, chromogranin A, adrenocorticotropin hormone (ACTH), or gastrin) in the subset of participants with biochemically measurable disease. (NCT00781911)
Timeframe: From Start of Treatment Up to 18 Months
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Chromogranin A | Gastrin | |
| Carcinoid Tumor | 0.0 | 0.0 |
| Islet Cell Carcinoma | 22.2 | 0.0 |
Percentage of participants who are alive and progression-free at 6 month from start of the study treatment over all participants. PFS is defined as the time from the start of study treatment until the date of objectively determined progressive disease (PD) or death due to any cause. Disease progression was assessed via Response Evaluation Criteria in Solid Tumors (RECIST) version 1.0, and defined as at least a 20% increase in the sum of the longest diameters of target lesions, taking as reference the smallest sum longest diameter recorded since the baseline measurements, and/or the appearance of one or more new lesion(s), and/or unequivocal progression of existing nontarget lesions. Participants without documentation of progression or death will be censored at the date of last tumor assessment. The PFS was estimated by the binomial distribution and Kaplan-Meier method. (NCT00781911)
Timeframe: From Start of Study Treatment to Progressive Disease or Death Due to Any Cause (Up to 6 Months)
| Intervention | percentage of participants (Number) | |
|---|---|---|
| Binomial Distribution; Primary Analysis | Kaplan-Meier Method; Secondary Analysis | |
| Carcinoid Tumor | 45.2 | 54.1 |
| Islet Cell Carcinoma | 41.7 | 61.4 |
Time to the first subcutaneous injections of rescue, short-acting octreotide was determined from the participant's daily diary. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | days (Median) |
|---|---|
| Placebo Core Phase | 1.00 |
| Telotristat Etiprate 500 mg Core Phase | 1.00 |
An adverse event (AE) was defined as any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug-related. A TEAE was an AE reported after the first dose of randomized treatment on Day 1. (NCT00853047)
Timeframe: Up to 4 Weeks Core Phase
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Any TEAE | Related TEAEs | |
| Placebo Core Phase | 4 | 3 |
| Telotristat Etiprate 150 mg Core Phase | 3 | 3 |
| Telotristat Etiprate 250 mg Core Phase | 3 | 0 |
| Telotristat Etiprate 350 mg Core Phase | 2 | 2 |
| Telotristat Etiprate 500 mg Core Phase | 9 | 6 |
Participants recorded the number of BMs per day in a daily diary. The total number of BMs per day were averaged over the 4-week period. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | bowel movements/day (Mean) |
|---|---|
| Placebo Core Phase | 0.82 |
| Telotristat Etiprate 150 mg Core Phase | -1.37 |
| Telotristat Etiprate 250 mg Core Phase | -2.17 |
| Telotristat Etiprate 350 mg Core Phase | -0.20 |
| Telotristat Etiprate 500 mg Core Phase | -0.71 |
An AE was defined as any untoward medical occurrence associated with the use of a drug in humans, whether or not considered drug related. A TEAE was an AE reported after receiving treatment. (NCT00853047)
Timeframe: Up to 180 weeks in the open-label extension phase
| Intervention | Participants (Count of Participants) |
|---|---|
| Telotristat Etiprate Open-Label Extension Phase | 18 |
"Complete Response to treatment was defined as one of the following: 1. Less than 4 bowel movements per day; or 2. A decrease in daily bowel movements that is ≥ 50% from baseline; or 3. A positive response to the global assessment question (In the past 7 days, have you had adequate relief of your carcinoid syndrome bowel complaints such as diarrhea, urgent need to have a bowel movement, abdominal pain or discomfort?) for each of the last 2 weeks of the Treatment Period." (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo Core Phase | 0 |
| Telotristat Etiprate 150 mg Core Phase | 1 |
| Telotristat Etiprate 250 mg Core Phase | 2 |
| Telotristat Etiprate 350 mg Core Phase | 1 |
| Telotristat Etiprate 500 mg Core Phase | 2 |
"Participants were asked to answer the following question: In the past 7 days, have you had adequate relief of your carcinoid syndrome bowel complaints such as diarrhea, urgent need to have a bowel movement, abdominal pain, or discomfort?. The number of participants who answered Yes are reported." (NCT00853047)
Timeframe: Week 4
| Intervention | Participants (Count of Participants) |
|---|---|
| Placebo Core Phase | 0 |
| Telotristat Etiprate 150 mg Core Phase | 1 |
| Telotristat Etiprate 250 mg Core Phase | 2 |
| Telotristat Etiprate 350 mg Core Phase | 1 |
| Telotristat Etiprate 500 mg Core Phase | 3 |
u5-HIAA is a standard test used in clinical practice to assess the neuroendocrine tumor (NET) activity and is collected as a 24-hour urine specimen. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | mg/24 hours (Mean) |
|---|---|
| Placebo Core Phase | -20.73 |
| Telotristat Etiprate 150 mg Core Phase | -27.55 |
| Telotristat Etiprate 250 mg Core Phase | -0.67 |
| Telotristat Etiprate 350 mg Core Phase | 13.60 |
| Telotristat Etiprate 500 mg Core Phase | -35.49 |
Participants recorded the severity of abdominal pain or discomfort in a daily diary assessed using a 4-point scale (0-none, 1-mild, 2-moderate, 3-severe). A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo Core Phase | 0.04 |
| Telotristat Etiprate 150 mg Core Phase | 0.03 |
| Telotristat Etiprate 250 mg Core Phase | -0.53 |
| Telotristat Etiprate 350 mg Core Phase | 0.03 |
| Telotristat Etiprate 500 mg Core Phase | 0.16 |
Participants recorded the sensation of urgency to defecate (Yes or No) in a daily diary. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | percentage of days (Mean) |
|---|---|
| Placebo Core Phase | -2.72 |
| Telotristat Etiprate 150 mg Core Phase | -34.43 |
| Telotristat Etiprate 250 mg Core Phase | -32.13 |
| Telotristat Etiprate 350 mg Core Phase | 0.00 |
| Telotristat Etiprate 500 mg Core Phase | -8.49 |
Participants recorded the number of daily flushing episodes per day in a daily diary. The total number of flushing episodes per day were averaged over the 4-week period. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | cutaneous flushing episodes (Mean) |
|---|---|
| Placebo Core Phase | -0.43 |
| Telotristat Etiprate 150 mg Core Phase | -0.60 |
| Telotristat Etiprate 250 mg Core Phase | -0.30 |
| Telotristat Etiprate 350 mg Core Phase | -0.10 |
| Telotristat Etiprate 500 mg Core Phase | -0.03 |
Participants recorded details (location and frequency of injection) of subcutaneous injections of rescue, short-acting octreotide, if taken, in the daily diary. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | injections per day (Mean) |
|---|---|
| Placebo Core Phase | -0.38 |
| Telotristat Etiprate 150 mg Core Phase | -0.03 |
| Telotristat Etiprate 250 mg Core Phase | 0.03 |
| Telotristat Etiprate 350 mg Core Phase | 0.00 |
| Telotristat Etiprate 500 mg Core Phase | -0.29 |
Participants recorded stool form in a daily diary using a 6-point scale (0-none,1-hard, 2-firm, 3-soft, 4-loose, 5-watery). A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | units on a scale (Mean) |
|---|---|
| Placebo Core Phase | -0.07 |
| Telotristat Etiprate 150 mg Core Phase | -0.50 |
| Telotristat Etiprate 250 mg Core Phase | 0.00 |
| Telotristat Etiprate 350 mg Core Phase | 0.00 |
| Telotristat Etiprate 500 mg Core Phase | -0.17 |
Blood samples were collected for assessment of Chromogranin A level. A negative change from Baseline indicates improvement. (NCT00853047)
Timeframe: Baseline to Week 4
| Intervention | ng/mL (Mean) |
|---|---|
| Placebo Core Phase | -3251.2 |
| Telotristat Etiprate 150 mg Core Phase | -190.5 |
| Telotristat Etiprate 250 mg Core Phase | -12.3 |
| Telotristat Etiprate 350 mg Core Phase | 52.5 |
| Telotristat Etiprate 500 mg Core Phase | 26011.4 |
(NCT00966355)
Timeframe: 5 days after enrollment
| Intervention | participants (Number) |
|---|---|
| Octreotide | 218 |
| Somatostatin | 216 |
| Terlipressin | 225 |
at least one of the three criteria (NCT00966355)
Timeframe: 5 days after enrollment
| Intervention | participants (Number) |
|---|---|
| Octreotide | 113 |
| Somatostatin | 115 |
| Terlipressin | 114 |
The Length of Time, in Months, That Patients Were Alive From Their First Date of Protocol Treatment Until Death (NCT01121939)
Timeframe: 18 months
| Intervention | months (Median) |
|---|---|
| Typical Carcinoid | NA |
| Pancreatic Islet Cell | 26.4 |
The Length of Time, in Months, That Patients Were Alive From Their First Date of Protocol Treatment Until Worsening of Their Disease. Progression is defined using Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0), as a 20% increase in the sum of the longest diameter of target lesions, or a measurable increase in a non-target lesion, or the appearance of new lesions. (NCT01121939)
Timeframe: 18 months
| Intervention | months (Median) |
|---|---|
| Typical Carcinoid | 11.96 |
| Pancreatic Islet Cell | 5.49 |
To define the toxicity and safety of the combination of bevacizumab, pertuzumab and Sandostatin LAR® when used in patients with advanced low grade neuroendocrine cancer - defined by grade 3/4, treatment-related toxicity (NCT01121939)
Timeframe: 18 months
| Intervention | participants (Number) | |||||
|---|---|---|---|---|---|---|
| Hypertension | Pain | Left ventricular systolic dysfunction | Diarrhea | Anemia | Leukopenia | |
| All Patients | 11 | 5 | 5 | 3 | 1 | 1 |
The Percentage of Patients Who Experience an Objective Benefit From Treatment or Experience Stable Disease. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI or CT: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Stable Disease (SD), Neither Sufficient Shrinkage to Qualify For PR, Nor Sufficient Increase to Qualify for Progressive Disease; Disease Control Rate = CR + PR + SD. (NCT01121939)
Timeframe: 18 months
| Intervention | percentage of participants (Number) |
|---|---|
| Typical Carcinoid | 72 |
| Pancreatic Islet Cell | 91 |
| All Patients | 77 |
The Percentage of Patients Who Experience an Objective Benefit From Treatment. Per Response Evaluation Criteria In Solid Tumors Criteria (RECIST v1.0) for target lesions and assessed by MRI or CT: Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Overall Response (OR) = CR + PR. (NCT01121939)
Timeframe: 18 months
| Intervention | percentage of participants (Number) |
|---|---|
| Typical Carcinoid | 16 |
| Pancreatic Islet Cell | 18 |
| All Patients | 16 |
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 |
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 |
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 |
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 |
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 |
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 |
(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 |
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 |
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 |
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 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 |
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 < 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 |
"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 |
Overall survival (OS) is defined as the time from study entry to death from any cause. The median OS was estimated using the Kaplan-Meier method. (NCT01229943)
Timeframe: From registration to time of death, assessed up to 3 years
| Intervention | months (Median) |
|---|---|
| Arm I (Octreotide Acetate and Everolimus) | 35.0 |
| Arm II (Octreotide Acetate, Everolimus, and Bevacizumab) | 36.7 |
Progression Free Survival (PFS) was defined as the time from study entry until disease progression or death, whichever occurs first. The median PFS was estimated using the Kaplan-Meier method. Progression was assessed per RECIST criteria, and defined as at least a 20% increase in the sum of the longest diameters of target lesions (and an absolute increase of at least 0.5 cm) or the appearance of new lesions. (NCT01229943)
Timeframe: From study entry to the date of documented progression or death from any cause, up to 3 years
| Intervention | months (Median) |
|---|---|
| Arm I (Octreotide Acetate and Everolimus) | 14.0 |
| Arm II (Octreotide Acetate, Everolimus, and Bevacizumab) | 16.7 |
The proportion of patients who respond (completely or partially) to each combination regimen will be estimated. Response was defined using Response Evaluation Criteria In Solid Tumors (RECIST) criteria: Complete Response (CR): disappearance of all target lesions; Partial Response (PR) 30% decrease in sum of longest diameter of target lesions. (NCT01229943)
Timeframe: Up to 3 years
| Intervention | percentage of participants (Number) |
|---|---|
| Arm I (Octreotide Acetate and Everolimus) | 12 |
| Arm II (Octreotide Acetate, Everolimus, and Bevacizumab) | 31 |
"A patient was classified as CR if both biochemical parameters were controlled at the end of 3 months of treatment:~Mean 1 hour GH < 2.5µg/L (according to Central Laboratory); and~IGF-I within the Central Laboratory Normal Range (for age and gender)" (NCT01278342)
Timeframe: From Baseline to 3 months
| Intervention | percent (Number) |
|---|---|
| Sandostatin LAR High Dose Alone | 60 |
| Sandostatin LAR High Dose + Pegvisomat | 0 |
| Sandostatin LAR High Dose + Cabergoline | 0 |
"Patients who met one of the following criteria at the end of 8 months of treatment were defined as Partial Responders, regardless of the treatment.~Mean 1 hour GH > 2.5 µg/L and < 5 µg/L and either a decrease in IGF-I of at least 50% compared to baseline or IGF-I within normal range.~Mean 1 hour GH < 2.5 µg/L and a decrease in IGF-I of at least 50% compared to baseline and IGF-I outside normal range." (NCT01278342)
Timeframe: From Baseline to 8 months
| Intervention | percent (Number) |
|---|---|
| Sandostatin LAR High Dose Alone | 25 |
| Sandostatin LAR High Dose + Pegvisomat | 22.6 |
| Sandostatin LAR High Dose + Cabergoline | 21.9 |
"A patient was classified as a Complete Responder (CR) if both biochemical parameters were controlled at the end of 8 months of treatment:~Mean 1 hour GH < 2.5µg/L (according to Central Laboratory); and~IGF-I within the Central Laboratory Normal Range (for age and gender)." (NCT01278342)
Timeframe: From Baseline to 8 months
| Intervention | percent (Number) |
|---|---|
| Sandostatin LAR High Dose Alone | 25 |
| Sandostatin LAR High Dose + Pegvisomat | 0 |
| Sandostatin LAR High Dose + Cabergoline | 9.4 |
Nadir growth hormone <1 ng/mL during a standard 2 hour oral glucose tolerance test using 75 g glucose and normal IGF-I according to age and gender-matched standards. (NCT01371643)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Medical Treatment by Octreotide LAR | 6.7 |
| Surgical Debulking Followed by Octreotide LAR | 50 |
Nadir growth hormone <1 ng/mL during a standard 2 hour oral glucose tolerance test using 75 g glucose and normal IGF-I according to age and gender-matched standards. (NCT01371643)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Medical Treatment by Octreotide LAR | 6.7 |
| Surgical Debulking Followed by Octreotide LAR | 53.9 |
Nadir growth hormone <1 ng/mL during a standard 2 hour oral glucose tolerance test using 75 g glucose and normal IGF-I according to age and gender-matched standards. (NCT01371643)
Timeframe: 3 months
| Intervention | percentage of participants (Number) |
|---|---|
| Medical Treatment by Octreotide LAR | 6.7 |
| Surgical Debulking Followed by Octreotide LAR | 76.9 |
Maintenance of an insulin-like growth factor-1 (IGF-1) response during the extension treatment period was defined as the percentage of participants with an IGF-1 concentration < 1.3 times the upper limit of normal at the beginning of the extension treatment period and at the end of the extension treatment period. IGF-1 concentration was determined in serum samples taken at the same visits growth hormone concentration was assessed. (NCT01412424)
Timeframe: Beginning of the extension treatment period and the end of the extension treatment period (up to 13 months)
| Intervention | Percentage of participants (Number) |
|---|---|
| Octreotide Capsules | 87.8 |
A responder was defined as a participant with a serum insulin-like growth factor-1 (IGF-1) concentration < 1.3 times the upper limit of normal (adjusted for age and gender) and a growth hormone (GH) concentration < 2.5 ng/mL. The growth hormone concentration was the mean of 5 fasted GH serum concentrations collected at 30 minute intervals for 2 hours, 2 to 4 hours post-octreotide dose. IGF-1 concentration was determined in serum samples taken at the same visits GH concentration was assessed. (NCT01412424)
Timeframe: End of the core treatment period (up to 7 months)
| Intervention | Percentage of responders (Number) |
|---|---|
| Octreotide 40 mg | 86.9 |
| Octreotide 60 mg | 66.7 |
| Octreotide 80 mg | 40.4 |
| Octreotide 40, 60, or 80 mg - All Participants | 64.9 |
Percentage of participants with the following serum insulin-like growth factor-1 (IGF-1) and growth hormone (GH) concentrations at the beginning (BETP) and at the end (EETP) of the extension treatment period: IGF-1 < 1.3 times the upper level of normal (ULN) and GH < 5.0 ng/mL, IGF-1 < 1.3 times ULN and GH < 1.0 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 5.0 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 2.5 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 1.0 ng/mL, IGF-1 < 1.3 times ULN, IGF-1 ≤ 1.0 times ULN, GH < 5.0 ng/mL, GH < 2.5 ng/mL, GH < 1.0 ng/mL, IGF-1 ≥ 1.3 times ULN and GH < 2.5 ng/mL, IGF-1 < 1.3 times ULN and GH ≥ 2.5 ng/mL, and IGF-1 ≥ 1.3 times ULN and GH ≥ 2.5 ng/mL. The growth hormone concentration was the mean of 5 fasted GH serum concentrations collected at 30 minute intervals for 2 hours, 2 to 4 hours post-octreotide dose. IGF-1 concentration was determined in serum samples taken at the same visits GH concentration was assessed. (NCT01412424)
Timeframe: Beginning and the end of the extension treatment period (up to 6 months)
| Intervention | Percentage of participants (Number) | |||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| IGF-1 < 1.3 & GH < 5.0: BETP | IGF-1 < 1.3 & GH < 5.0: EETP | IGF-1 < 1.3 & GH < 1.0: BETP | IGF-1 < 1.3 & GH < 1.0: EETP | IGF-1 ≤ 1.0 & GH < 5.0: BETP | IGF-1 ≤ 1.0 & GH < 5.0: EETP | IGF-1 ≤ 1.0 & GH < 2.5: BETP | IGF-1 ≤ 1.0 & GH < 2.5: EETP | IGF-1 ≤ 1.0 & GH < 1.0: BETP | IGF-1 ≤ 1.0 & GH < 1.0: EETP | IGF-1 < 1.3: BETP | IGF-1 < 1.3: EETP | IGF-1 ≤ 1.0: BETP | IGF-1 ≤ 1.0: EETP | GH < 5.0: BETP | GH < 5.0: EETP | GH < 2.5: BETP | GH < 2.5: EETP | GH < 1.0: BETP | GH < 1.0: EETP | IGF-1 ≥ 1.3 & GH < 2.5: BETP | IGF-1 ≥ 1.3 & GH < 2.5: EETP | IGF-1 < 1.3 & GH ≥ 2.5: BETP | IGF-1 < 1.3 & GH ≥ 2.5: EETP | IGF-1 ≥ 1.3 & GH ≥ 2.5: BETP | IGF-1 ≥ 1.3 & GH ≥ 2.5: EETP | |
| Octreotide Capsules | 84.1 | 79.5 | 69.3 | 68.2 | 48.9 | 50.0 | 48.9 | 50.0 | 42.0 | 44.3 | 84.1 | 79.5 | 48.9 | 50.0 | 100.0 | 97.7 | 98.9 | 95.5 | 83.0 | 83.0 | 14.8 | 17.0 | 0.0 | 1.1 | 1.1 | 3.4 |
A responder was defined as a participant with a serum insulin-like growth factor-1 (IGF-1) concentration < 1.3 times the upper limit of normal (adjusted for age and gender) and a growth hormone (GH) concentration < 2.5 ng/mL. The growth hormone concentration was the mean of 5 fasted GH serum concentrations collected at 30 minute intervals for 2 hours, 2 to 4 hours post-octreotide dose. IGF-1 concentration was determined in serum samples taken at the same visits GH concentration was assessed. (NCT01412424)
Timeframe: End of the extension treatment period (up to 13 months)
| Intervention | Percentage of responders (Number) |
|---|---|
| Octreotide Capsules | 78.4 |
Maintenance of response during the fixed dose phase of the core treatment period was defined as the percentage of participants with an insulin-like growth factor-1 (IGF-1) concentration < 1.3 times the upper limit of normal at the beginning of the fixed dose phase of the core treatment period and at the end of the core treatment period. IGF-1 concentration was determined in serum samples taken at the same visits growth hormone concentration was assessed. (NCT01412424)
Timeframe: Beginning of the fixed dose phase of the core treatment period and the end of the core treatment period (up to 7 months)
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Beginning of the FDP of the CTP | End of the CTP | |
| Octreotide Capsules | 82.7 | 80.0 |
Reported is the percentage of participants who had ≥ 1, 2, or 3 of the 5 symptoms of acromegaly (headaches, perspiration, asthenia, swelling of extremities, or joint pain) of any severity (mild, moderate, or severe). This was a post hoc analysis. (NCT01412424)
Timeframe: Baseline and the end of the extension treatment period (up to 13 months)
| Intervention | Percentage of participants (Number) | |||||
|---|---|---|---|---|---|---|
| 1 Symptom - Baseline | 1 Symptom - End of the extension treatment period | 2 Symptoms - Baseline | 2 Symptoms - End of the extension treatment period | 3 Symptoms - Baseline | 3 Symptoms - End of the extension treatment period | |
| Octreotide Capsules | 78 | 65 | 61 | 43 | 43 | 25 |
The severity (absent, mild, moderate, severe) of the 5 acromegaly symptoms headache, perspiration, asthenia, swelling of extremities, and joint pain was assessed at Baseline and at the end of the extension treatment period. The percentage of participants with improved or maintained (no change) acromegaly symptoms from Baseline at the end of the extension treatment period is reported. (NCT01412424)
Timeframe: Baseline and the end of the extension treatment period (up to 13 months)
| Intervention | Percentage of participants (Number) | |
|---|---|---|
| Maintained | Improved | |
| Octreotide Capsules | 27 | 57 |
Percentage of participants with the following serum insulin-like growth factor-1 (IGF-1) and growth hormone (GH) concentrations at Baseline and at the end of the core treatment period (ECTP): IGF-1 < 1.3 times the upper limit of normal (ULN) and GH < 5.0 ng/mL, IGF-1 < 1.3 times ULN and GH < 1.0 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 5.0 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 2.5 ng/mL, IGF-1 ≤ 1.0 times ULN and GH < 1.0 ng/mL, IGF-1 < 1.3 times ULN, IGF-1 ≤ 1.0 times ULN, GH < 5.0 ng/mL, GH < 2.5 ng/mL, GH < 1.0 ng/mL, IGF-1 ≥ 1.3 times ULN and GH < 2.5 ng/mL, IGF-1 < 1.3 times ULN and GH ≥ 2.5 ng/mL, and IGF-1 ≥ 1.3 times ULN and GH ≥ 2.5 ng/mL. The growth hormone concentration was the mean of 5 fasted GH serum concentrations collected at 30 minute intervals for 2 hours, 2 to 4 hours post-octreotide dose. IGF-1 concentration was determined in serum samples taken at the same visits GH concentration was assessed. (NCT01412424)
Timeframe: Baseline and the end of the core treatment period (up to 7 months)
| Intervention | Percentage of participants (Number) | |||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| IGF-1 < 1.3 & GH < 5.0: Baseline | IGF-1 < 1.3 & GH < 5.0: ECTP | IGF-1 < 1.3 & GH < 1.0: Baseline | IGF-1 < 1.3 & GH < 1.0: ECTP | IGF-1 ≤ 1.0 & GH < 5.0: Baseline | IGF-1 ≤ 1.0 & GH < 5.0: ECTP | IGF-1 ≤ 1.0 & GH < 2.5: Baseline | IGF-1 ≤ 1.0 & GH < 2.5: ECTP | IGF-1 ≤ 1.0 & GH < 1.0: Baseline | IGF-1 ≤ 1.0 & GH < 1.0: ECTP | IGF-1 < 1.3: Baseline | IGF-1 < 1.3: ECTP | IGF-1 ≤ 1.0: Baseline | IGF-1 ≤ 1.0: ECTP | GH < 5.0: Baseline | GH < 5.0: ECTP | GH < 2.5: Baseline | GH < 2.5: ECTP | GH < 1.0: Baseline | GH < 1.0: ECTP | IGF-1 ≥ 1.3 & GH < 2.5: Baseline | IGF-1 ≥ 1.3 & GH < 2.5: ECTP | IGF-1 < 1.3 & GH ≥ 2.5: Baseline | IGF-1 < 1.3 & GH ≥ 2.5: ECTP | IGF-1 ≥ 1.3 & GH ≥ 2.5: Baseline | IGF-1 ≥ 1.3 & GH ≥ 2.5: ECTP | |
| Octreotide Capsules | 91.4 | 65.6 | 62.9 | 53.0 | 63.6 | 35.8 | 61.6 | 35.8 | 43.0 | 31.8 | 91.4 | 66.9 | 63.6 | 37.1 | 100.0 | 97.4 | 96.0 | 94.7 | 66.2 | 77.5 | 7.3 | 29.8 | 2.6 | 0.7 | 1.3 | 2.0 |
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 |
"The Quality of Life Questionnaire C30 (QLQ-C30) was developed by the European Organization for Research and Treatment of Cancer (EORTC) to assess quality of life in cancer patients. It includes five function domains (physical, emotional, social, role, cognitive), eight symptoms (fatigue, pain, nausea/vomiting, constipation, diarrhea, insomnia, dyspnea, and appetite loss), as well as global health/quality-of-life and financial impact. Subjects respond on a four-point scale from not at all to very much for most items. Raw scores are linearly transformed so each score ranged a 0-100, where higher scores indicate worse symptoms (e.g., more severe/worsened) and lower scores indicate less symptoms (e.g., less severe/improvement)." (NCT01578239)
Timeframe: Inclusion (Baseline) (BL), Week 72, Week 120
| Intervention | Scores on a scale (Mean) | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical functioning: chg from BL @ wk 72 (n=33,11) | Role functioning: chg from BL @ wk 72 (n=33,11) | Emotional functioning: chg from BL @ wk 72 (n=33,11) | Cognitive functioning: chg from BL @ wk 72 (n=33,11) | Social functioning: chg from BL @ wk 72 (n=33,11) | Global Health Status/QoL: chg from BL @ wk 72 (n=33,11) | Fatigue: chg from BL @ wk 72 (n=33,11) | Nausea & Vomiting: chg from BL @ wk 72 (n=33,11) | Pain: chg from BL @ wk 72 (n=33,11) | Dyspnoea: chg from BL @ wk 72 (n=33,11) | Insomnia: chg from BL @ wk 72 (n=33,11) | Appetite loss: chg from BL @ wk 72 (n=33,11) | Constipation: chg from BL @ wk 72 (n=33,11) | Diarrhoea: chg from BL @ wk 72 (n=33,11) | Financial difficulties: chg from BL @ wk 72 (n=33,11) | |
| Octreotide LAR | -4.242 | -3.030 | 6.061 | 1.515 | -7.576 | 1.515 | -2.020 | -4.545 | -3.030 | 3.030 | 6.061 | 9.091 | 0.000 | -3.030 | 6.061 |
"The Quality of Life Questionnaire C30 (QLQ-C30) was developed by the European Organization for Research and Treatment of Cancer (EORTC) to assess quality of life in cancer patients. It includes five function domains (physical, emotional, social, role, cognitive), eight symptoms (fatigue, pain, nausea/vomiting, constipation, diarrhea, insomnia, dyspnea, and appetite loss), as well as global health/quality-of-life and financial impact. Subjects respond on a four-point scale from not at all to very much for most items. Raw scores are linearly transformed so each score ranged a 0-100, where higher scores indicate worse symptoms (e.g., more severe/worsened) and lower scores indicate less symptoms (e.g., less severe/improvement)." (NCT01578239)
Timeframe: Inclusion (Baseline) (BL), Week 72, Week 120
| Intervention | Scores on a scale (Mean) | |||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Physical functioning: chg from BL @ wk 72 (n=33,11) | Physical functioning: chg from BL @ wk 120 (n=2,0) | Role functioning: chg from BL @ wk 72 (n=33,11) | Role functioning: chg from BL @ wk 120 (n=2,0) | Emotional functioning: chg from BL @ wk 72 (n=33,11) | Emotional functioning: chg from BL @ wk 120 (n=2,0) | Cognitive functioning: chg from BL @ wk 72 (n=33,11) | Cognitive functioning: chg from BL @ wk 120 (n=2,0) | Social functioning: chg from BL @ wk 72 (n=33,11) | Social functioning: chg from BL @ wk 120 (n=2,0) | Global Health Status/QoL: chg from BL @ wk 72 (n=33,11) | Global Health Status/QoL: chg from BL @ wk 120 (n=2,0) | Fatigue: chg from BL @ wk 72 (n=33,11) | Fatigue: chg from BL @ wk 120 (n=2,0) | Nausea & Vomiting: chg from BL @ wk 72 (n=33,11) | Nausea & Vomiting: chg from BL @ wk 120 (n=2,0) | Pain: chg from BL @ wk 72 (n=33,11) | Pain: chg from BL @ wk 120 (n=2,0) | Dyspnoea: chg from BL @ wk 72 (n=33,11) | Dyspnoea: chg from BL @ wk 120 (n=2,0) | Insomnia: chg from BL @ wk 72 (n=33,11) | Insomnia: chg from BL @ wk 120 (n=2,0) | Appetite loss: chg from BL @ wk 72 (n=33,11) | Appetite loss: chg from BL @ wk 120 (n=2,0) | Constipation: chg from BL @ wk 72 (n=33,11) | Constipation: chg from BL @ wk 120 (n=2,0) | Diarrhoea: chg from BL @ wk 72 (n=33,11) | Diarrhoea: chg from BL @ wk 120 (n=2,0) | Financial difficulties: chg from BL @ wk 72 (n=33,11) | Financial difficulties: chg from BL @ wk 120 (n=2,0) | |
| 177Lu-DOTA0-Tyr3-Octreotate | 3.232 | -3.333 | 5.051 | 8.333 | 7.744 | 12.500 | 5.556 | 16.667 | 8.586 | 8.333 | 5.556 | -16.667 | -7.239 | 11.111 | -4.545 | 0.000 | -8.586 | 0.000 | -3.030 | 0.000 | 0.000 | 33.333 | -8.081 | 0.000 | 0.000 | 0.000 | -12.121 | -16.667 | -7.071 | -16.667 |
The Quality of Life GI Neuroendocrine Tumor survey (QLQ GINET21) contains a total of 21 items: four single-item assessments relating to muscle and/or bone pain (MBP), body image (BI), information (INF) and sexual functioning (SX), together with 17 items organized into five proposed scales: endocrine symptoms (ED; three items), GI symptoms (GI; five items), treatment-related symptoms (TR; three items), social functioning (SF) and disease-related worries (DRW; three items). The response format of the questionnaire is a four-point Likert scale. Responses are linearly transformed to a 0-100 scale using EORTC guidelines, with higher scores reflecting more severe symptoms. (NCT01578239)
Timeframe: Inclusion (Baseline) (BL), Week 72, Week 120
| Intervention | Scores on a scale (Mean) | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Endocrine scale: chg from BL @ wk 72 (n=33,11) | Endocrine scale: chg from BL @ wk 120 (n=2,0) | G.I. scale: chg from BL @ wk 72 (n=33,11) | G.I. scale: chg from BL @ wk 120 (n=2,0) | Treatment scale: chg from BL @ wk 72 (n=21,5) | Treatment scale: chg from BL @ wk 120 (n=1,0) | Social function scale: chg from BL @ wk 72 (n=33,11) | Social function scale: chg from BL @ wk 120 (n=2,0) | Diseases rel. worries scale: chg from BL @ wk 72 (n=33,11) | Diseases rel. worries scale: chg from BL @ wk 120 (n=2,0) | Muscle/Bone pain symptom: chg from BL @ wk 72 (n=33,10) | Muscle/Bone pain symptom: chg from BL @ wk 120 (n=2,0) | Sexual function: chg from BL @ wk 72 (n=21,7) | Sexual function: chg from BL @ wk 120 (n=2,0) | Information/Communication: chg from BL @ wk 72 (n=33,11) | Information/Communication: chg from BL @ wk 120 (n=2,0) | Body image: chg from BL @ wk 72 (n=33,11) | Body image: chg from BL @ wk 120 (n=2,0) | |
| 177Lu-DOTA0-Tyr3-Octreotate | -8.754 | 0.000 | -2.727 | -13.333 | -8.995 | -16.667 | -7.576 | 11.111 | -6.061 | 33.333 | -5.051 | -16.667 | 6.349 | 50.000 | -4.040 | 0.000 | -4.040 | 16.667 |
The Quality of Life GI Neuroendocrine Tumor survey (QLQ GINET21) contains a total of 21 items: four single-item assessments relating to muscle and/or bone pain (MBP), body image (BI), information (INF) and sexual functioning (SX), together with 17 items organized into five proposed scales: endocrine symptoms (ED; three items), GI symptoms (GI; five items), treatment-related symptoms (TR; three items), social functioning (SF) and disease-related worries (DRW; three items). The response format of the questionnaire is a four-point Likert scale. Responses are linearly transformed to a 0-100 scale using EORTC guidelines, with higher scores reflecting more severe symptoms. (NCT01578239)
Timeframe: Inclusion (Baseline) (BL), Week 72, Week 120
| Intervention | Scores on a scale (Mean) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Endocrine scale: chg from BL @ wk 72 (n=33,11) | G.I. scale: chg from BL @ wk 72 (n=33,11) | Treatment scale: chg from BL @ wk 72 (n=21,5) | Social function scale: chg from BL @ wk 72 (n=33,11) | Diseases rel. worries scale: chg from BL @ wk 72 (n=33,11) | Muscle/Bone pain symptom: chg from BL @ wk 72 (n=33,10) | Sexual function: chg from BL @ wk 72 (n=21,7) | Information/Communication: chg from BL @ wk 72 (n=33,11) | Body image: chg from BL @ wk 72 (n=33,11) | |
| Octreotide LAR | -11.111 | 2.424 | 0.000 | -7.576 | 1.010 | -16.667 | 14.286 | -12.121 | -3.030 |
The distribution of adverse events was done via the analysis of frequencies for Adverse Event (AEs), Serious Adverse Event (SAEs) and Deaths, through the monitoring of relevant clinical and laboratory safety parameters. (NCT01578239)
Timeframe: From informed consent signature through study completion reached at final safety cutoff date on 18July2021, assessed up to approximately 101 Months
| Intervention | Participants (Count of Participants) | |||
|---|---|---|---|---|
| Adverse Events (AEs) | Serious Adverse Events (SAEs) | Deaths during treatment period | Deaths during follow-up period | |
| 177Lu-DOTA0-Tyr3-Octreotate | 105 | 40 | 4 | 66 |
| Octreotide LAR | 90 | 31 | 5 | 63 |
Survival estimates were collected every 12 Months up to 60 Months to compare OS between the two treatment groups. (NCT01578239)
Timeframe: 12 months, 24 months, 36 months, 48 months, 60 months
| Intervention | Percentage of Survival Estimates (Number) | ||||
|---|---|---|---|---|---|
| 12 months | 24 months | 36 months | 48 months | 60 months | |
| 177Lu-DOTA0-Tyr3-Octreotate | 91.0 | 76.0 | 61.4 | 49.5 | 37.1 |
| Octreotide LAR | 79.7 | 62.7 | 50.1 | 41.8 | 35.4 |
The Duration of Response (DoR) was defined as the time from initially meeting the criteria for response (CR or PR) until the time of progression by RECIST 1.1. (NCT01578239)
Timeframe: From date of randomization until date of progression or date of death from any cause, whichever comes first until Primary Analysis cutoff date reached on 24July2015, assessed up to approximately 34 months
| Intervention | Months (Median) |
|---|---|
| 177Lu-DOTA0-Tyr3-Octreotate | NA |
| Octreotide LAR | 1.9 |
Objective Response Rate (ORR) was calculated as the proportion of patients with tumour size reduction (sum of partial responses (PR) and complete responses (CR)) according to RECIST 1.1. (NCT01578239)
Timeframe: From date of randomization until date of progression or date of death from any cause, whichever comes first until Primary Analysis cutoff date reached on 24July2015, assessed up to approximately 34 months
| Intervention | Percentage of Participants (Number) |
|---|---|
| 177Lu-DOTA0-Tyr3-Octreotate | 14.7 |
| Octreotide LAR | 4.0 |
Overall Survival (OS) was defined as the time from the date of randomization to the date of death due to any cause or the date of last contact (censored observation) prior to the date of the data cut-off, and during the entire study period (i.e. the treatment period plus follow-up). (NCT01578239)
Timeframe: From date of randomization until date of death from any cause up to final safety cut-off date reached on 18Jan2021, assessed up to approximately 100 months
| Intervention | Months (Median) |
|---|---|
| 177Lu-DOTA0-Tyr3-Octreotate | 48.0 |
| Octreotide LAR | 36.3 |
Progression Free Survival (PFS) was defined as the time from randomization to documented centrally assessed disease progression, as evaluated by the Independent Review Committee (IRC), or death due to any cause. If a participant had no centrally assessed progression and had not died at the time of the primary endpoint analysis, the participant was regarded as censored in the context of a time to event analysis at the date of last evaluable tumor assessment. Disease progression was determined by objective tumor response status using Response Evaluation Criteria in Solid Tumors Criteria (RECIST v1.1). (NCT01578239)
Timeframe: From date of randomization until date of radiographic progression or date of death from any cause, whichever comes first until Primary Analysis cutoff date reached on 24July2015, assessed up to approximately 34 months
| Intervention | months (Median) |
|---|---|
| 177Lu-DOTA0-Tyr3-Octreotate | NA |
| Octreotide LAR | 8.5 |
Time to Tumour Progression (TTP) was defined as the time from randomization to progression centrally assessed. It included patients who dropped out due to toxicity, but omitted patients who died without measured progression (censored to last follow-up date or death date). (NCT01578239)
Timeframe: From date of randomization until date of progression or date of death from any cause, whichever comes first until Primary Analysis cutoff date reached on 24July2015, assessed up to approximately 34 months
| Intervention | Months (Median) |
|---|---|
| 177Lu-DOTA0-Tyr3-Octreotate | NA |
| Octreotide LAR | 8.7 |
(NCT01707225)
Timeframe: 24 weeks
| Intervention | participants (Number) |
|---|---|
| Octreotide LAR Depot | 10 |
"Cardiovascular:~Sinus bradycardia (19% to 25%) Hypertension (≤13%) conduction abnormalities (9% to 10%)~Central nervous system:~Fatigue (1% to 32%) headache (6% to 30%) malaise (16% to 20%) fever (16% to 20%) dizziness (5% to 20%) Pain (4% to 15%)~Dermatologic:~Pruritus (≤18%) Rash (15%; depot formulation) alopecia (≤13%)~Endocrine & metabolic:~Hyperglycemia (2% to 27%)~Gastrointestinal:~Abdominal pain (5% to 61%) loose stools (5% to 61%) nausea (5% to 61%) diarrhea (34% to 58%) flatulence (≤38%) cholelithiasis (13% to 38%; length of therapy dependent) constipation (9% to 21%) vomiting (4% to 21%)~Hematologic Anemia (5-15%)~Local:~Injection site pain (2% to 50%; dose and formulation related)~Neuromuscular & skeletal:~Back pain (1% to 27%) arthropathy (8% to 19%) myalgia (≤18%)~Renal Kidney Stones (5-15%)~Respiratory:~Upper respiratory infection (10% to 23%)~Miscellaneous:~flu symptoms (1% to 20%)" (NCT01707225)
Timeframe: 24 weeks
| Intervention | participants (Number) |
|---|---|
| Octreotide LAR Depot | 10 |
Percentage of patients with clinical benefit as judged by the investigator. Investigator attestation of continued clinical benefit was collected in clinical database after protocol amendment (release date 18 March 2016). Clinical benefit assessment before protocol amendment was done retrospectively. (NCT01789281)
Timeframe: After 3 months from enrollment, every 3 months, until end of treatment, assessed up to 7.2 years
| Intervention | Participants (Count of Participants) | |||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| At 3 months | At 6 months | At 9 months | At 12 months | At 15 months | At 18 months | At 21 months | At 24 months | At 27 months | At 30 months | At 33 months | At 36 months | At 39 months | At 42 months | At 45 months | At 48 months | At 51 months | At 54 months | At 57 months | At 60 months | At 63 months | At 66 months | At 69 months | At 72 months | At 75 months | At 78 months | At 81 months | At 84 months | |
| Everolimus | 9 | 8 | 8 | 8 | 8 | 8 | 8 | 6 | 5 | 3 | 2 | 1 | 1 | 1 | 1 | 1 | 1 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 |
| Everolimus+Sandostatin LAR | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 7 | 6 | 6 | 6 | 6 | 6 | 5 | 5 | 4 | 4 | 3 | 3 | 3 | 2 | 1 | 0 |
Any sign or symptom that occurs during the study treatment plus the 30 days post treatment. All SAEs were captured in safety database from enrollment. Safety data collection was changed in the protocol amendment released in March 2016: AEs and SAEs were captured in the clinical database from protocol amendment release (18 March 2016). Hence, SAEs from both safety database and clinical database are summarized separately. (NCT01789281)
Timeframe: SAEs collected in safety database from enrollment to end of treatment (EOT) plus 30 days, up to approximately 7.2 years. AEs/SAEs collected in clinical database from protocol amendment date 18 March 2016 to EOT plus 30 days, up to approximately 4.5 years
| Intervention | Participants (Count of Participants) | |||||
|---|---|---|---|---|---|---|
| SAEs (Safety database) | Treatment-related SAEs (Safety database) | AEs (Clinical Database) | Tretament-related AEs (Clinical Database) | SAEs (Clinical Database) | Treatment-related SAEs (Clinical Database) | |
| Everolimus | 6 | 1 | 7 | 4 | 2 | 0 |
| Everolimus+Sandostatin LAR | 9 | 4 | 7 | 4 | 4 | 2 |
Compare specificity of 68Ga-DOTATOC PET/CT with Octreoscan + high-resolution, contrast-enhanced CT for diagnosis and staging in neuroendocrine tumors and other somatostatin receptor positive tumors (NCT01869725)
Timeframe: 6 months
| Intervention | percentage of specificity (Number) | ||
|---|---|---|---|
| Specificity of 68Ga-DOTATOC | Specificity of Octreoscan | Specificity of Conventional Imaging (CI) | |
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 100 | 100 | 47.82 |
Compare sensitivity of 68Ga-DOTATOC PET/CT with Octreoscan + high-resolution, contrast-enhanced CT for diagnosis and staging in neuroendocrine tumors and other somatostatin receptor positive tumors (NCT01869725)
Timeframe: Up to 6 months
| Intervention | percentage of sensitivity (Number) | ||
|---|---|---|---|
| Sensitivity of Ga-68-DOTATOC | Sensitivity of OctreoScan | Sensitivity of Conventional Imaging (CI) | |
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 96.55 | 79.31 | 82.24 |
Tumor lesions detected on 68Ga-DOTATOC PET/CT compared with tumor lesions detected on Octreoscan SPECT imaging plus high-resolution, contrast-enhanced CT. (NCT01869725)
Timeframe: Up to 6 months between the timing of the Octreoscan SPECT/CT plus high-resolution, contrast-enhanced CT and the time of the 68Ga-DOTATOC PET/CT (either imaging type may occur first)
| Intervention | Participants (Count of Participants) | |||||||
|---|---|---|---|---|---|---|---|---|
| Sensitivity and Specificity for Ga-68-DOTATOC as Compared to Pathology72023597 | Sensitivity and Specificity for OctreoScan as Compared to Pathology72023597 | |||||||
| Total positive | False position | False negative | Total negative | |||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 28 | |||||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 1 | |||||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 23 | |||||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 0 | |||||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 6 | |||||||
| Diagnostic (Gallium Ga 68-edotreotide PET/CT) | 5 | |||||||
The frequencies of flushing, diarrhea, and carcinoid syndrome control rating (scale 1-5) will be measured and compared at week 0 and week 12 . These measurements will be compared using two-sided non-parametric paired Wilcoxon signed-rank. (NCT01886287)
Timeframe: At 12 weeks
| Intervention | participants (Number) |
|---|---|
| Octreotide Long-acting Release (LAR) | 1 |
"Colonic motility was measured using a solid-state catheter. The catheter had 36 sensors spaced 5-cm apart for the first 15 sensors and 1-cm apart for the remaining sensors. Pressures were transmitted to a transducer and recorded on a personal computer system (Medical Measurement Systems USA, Dover, NH).~Motility index (MI) was calculated using the Medical Measurement Systems computer program. The MI represents the area under the curve of the pressure tracing for a certain period (21). The MI was calculated for each channel. The MIs from all of the channels were then averaged to give each patient 1 average MI for the particular period under study. In this study, MI was calculated for the periods of 15, 30, and 45 minutes before and after infusion of octreotide. MI is reported as millimeters of mercury (mmHg) per 15, 30, or 45 minutes." (NCT01917773)
Timeframe: Average MI for all patients was calculated over 15-minutes, 30-minutes and 45- minutes before and after administration of octreotide.
| Intervention | mm Hg (Mean) | |
|---|---|---|
| pre-octreotide | post-octreotide | |
| 15 Minutes | 6.03 | 5.32 |
| 30 Minutes | 6.89 | 6.71 |
| 45 Minutes | 7.73 | 7.53 |
(NCT02217800)
Timeframe: 23 hours following each treatment
| Intervention | participants with trough hGH < 2.5 µg/mL (Number) |
|---|---|
| Saline (Control) | 0 |
| 920 µg DG3173 | 1 |
| 2760 µg DG3173 | 2 |
| 5520 µg DG3173 | 3 |
| Active Control (Octreotide) | 4 |
(NCT02235987)
Timeframe: Pre dose and 0.33, 0.67 hours and 1, 1.5, 2, 3, 4, 5, 6 and 8 hours post dose on each dosing day.
| Intervention | participants with trough hGH < 2.5 µg/mL (Number) |
|---|---|
| Baseline (Untreated Control) | 1 |
| 300 µg Octreotide | 8 |
| 100 µg DG3173 | 4 |
| 300 µg DG3173 | 6 |
| 900 µg DG3173 | 7 |
| 1800 µg DG3173 | 8 |
Proportion of subjects requiring diarrhoea related Lapatinib and Capecitabine treatment withdrawal as recorded in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Requiring treatment withdrawal in Lapatinib | Requiring treatment withdrawal in Capecitabine | |
| No Octreotide Treatment | 0 | 0 |
| Octreotide Treatment | 0 | 0 |
Proportion of subjects taking anti-diarrhoeal medication as recorded in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 7 |
| No Octreotide Treatment | 11 |
"Clinical benefit response as measured in accordance with the Response Evaluation Criteria In Solid Tumours (RECIST) version 1.1. Complete Response (CR), Disappearance of all target lesions; Partial Response (PR), >=30% decrease in the sum of the longest diameter of target lesions; Stable Disease (SD), Neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD.~Clinical Benefit Response rate (CBR) is defined as the percentage of subjects with a CR, PR or SD at week 24." (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 7 |
| No Octreotide Treatment | 9 |
Duration of diarrhoea of any grade of severity, recorded as AEs in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | days (Mean) |
|---|---|
| Octreotide Treatment | 8.7 |
| No Octreotide Treatment | 36.8 |
The proportion of subjects contacting a health care professional other than the hospital doctors/nurses to discuss diarrhoea are summarised (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 4 |
| No Octreotide Treatment | 3 |
Proportion of subjects experiencing diarrhoea of any grade of severity as defined by the NCI CTCAE, version 4.03 and recorded as AEs in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 18 |
| No Octreotide Treatment | 14 |
Proportion of subjects experiencing diarrhoea with a severity of Grade 3 and above, as defined by the NCI CTCAE, version 4.03 and recorded as AEs in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 2 |
| No Octreotide Treatment | 0 |
The proportion of subjects making dietary changes to help with the diarrhoea are summarised (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 9 |
| No Octreotide Treatment | 11 |
All subjects completed the baseline DMD during the 3 days prior to randomisation, before any study-related treatment is administered. Subjects randomised to receive Octreotide completed a second baseline DMD before starting the first cycle of treatment with Lapatinib and Capecitabine. The baseline DMD comprised of 3 questions to record stool form and consistency. The DMD to be completed throughout the rest of the study comprised of 3 questions in the baseline DMD and a further 5 questions and 6 sub-questions to evaluate the consequences and management of diarrhoea. (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 23 |
| No Octreotide Treatment | 29 |
The proportion of subjects reducing or completely stopping the number of anti-cancer tablets to help with diarrhoea are summarised (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 2 |
| No Octreotide Treatment | 3 |
The proportion of subjects taking medication at least once as a result of diarrhoea are summarised (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Treatment | 2 |
| No Octreotide Treatment | 2 |
Time to onset of the first episode of diarrhoea of any grade of severity, recorded as an AE in the eCRF. Subject are censored if there was no event. Median time and 95% confidence intervals were calculated using Kaplan-Meier estimates. (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Days (Median) |
|---|---|
| Octreotide Treatment | NA |
| No Octreotide Treatment | 170 |
Event is defined as Subjects reporting change in frequency and/or consistency of bowel movements from baseline at least once in DMD. Subject are censored if there is no change in bowel movement frequency/consistency as compared to baseline. Median time and 95% confidence intervals were calculated using Kaplan-Meier estimates. (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Days (Median) |
|---|---|
| Octreotide Treatment | 22.0 |
| No Octreotide Treatment | 8.0 |
Number of Lapatinib and Capecitabine tablets dispensed and returned as recorded in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | tablets (Mean) | |||
|---|---|---|---|---|
| Number of Lapatinib tablets dispensed | Number of Lapatinib tablets returned | Number of Capecitabine tablets dispensed | Number of Capecitabine tablets returned | |
| No Octreotide Treatment | 1115.6 | 403.3 | 1011.2 | 210 |
| Octreotide Treatment | 1197.5 | 477.1 | 1022.6 | 186.1 |
Proportion of subjects experiencing at least one episode of diarrhoea with a severity of Grade 2 and above, as defined by the National Cancer Institute common terminology criteria for adverse events (NCI CTCAE) version 4.03, recorded as AEs in the Electronic case report form (eCRF) (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Cyclce 1-3 (up to 9 weeks)with impuation | Cyclce 1-8 (up to 24 weeks)without imputation | |
| No Octreotide Treatment | 9 | 5 |
| Octreotide Treatment | 7 | 6 |
Proportion of subjects requiring diarrhoea related Lapatinib and Capecitabine dose delay as recorded in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Subjects requiring dose delay in Lapatinib | Subjects requiring dose delay in Capecitabine | |
| No Octreotide Treatment | 2 | 2 |
| Octreotide Treatment | 2 | 2 |
Proportion of subjects requiring diarrhoea related Lapatinib and Capecitabine dose reduction as recorded in the eCRF (NCT02294786)
Timeframe: Up to 24 weeks
| Intervention | Participants (Count of Participants) | |
|---|---|---|
| Subjects requiring dose reduction in Lapatinib | Subjects requiring dose reduction in Capecitabine | |
| No Octreotide Treatment | 0 | 2 |
| Octreotide Treatment | 1 | 1 |
"Pharmacokinetics (PK) of octreotide after injection of Sandostatin Long-acting Release (LAR) was determined for the dosing period Day -28 to Day 0; Ctrough (ng/mL).~Ctrough; Concentration levels assessed prior to next injection for the final (Sandostatin LAR) dosing interval (ng/mL)." (NCT02299089)
Timeframe: Pre-dose; study Day -28- to Day 0 (PK analysis:Sandostatin (LAR®) sampling time points: 0, 1hour, 24hours, 7days, 14days, 21days and 28days)
| Intervention | ng/mL (Mean) |
|---|---|
| Sandostatin LAR 10 mg (Acromegaly) | 0.225 |
| Sandostatin LAR 30mg (Acromegaly) | 1.20 |
| Sandostatin LAR 20 mg (NET) | 0.901 |
| Sandostatin LAR 30 mg (NET) | 1.27 |
"Pharmacokinetics (PK) of octreotide after injection of Sandostatin Long-acting Release (LAR) was determined for the dosing period Day -28 to Day 0; Cmax (ng/mL).~Cmax (ng/mL): Maximum observed plasma concentration over the final (Sandostatin LAR) dosing interval (ng/mL)" (NCT02299089)
Timeframe: Pre-dose; study Day -28- to Day 0 (PK analysis:Sandostatin (LAR®) sampling time points: 0, 1hour, 24hours, 7days, 14days, 21days and 28days)
| Intervention | ng/mL (Mean) |
|---|---|
| Sandostatin LAR 10 mg (Acromegaly) | 0.349 |
| Sandostatin LAR 30mg (Acromegaly) | 1.41 |
| Sandostatin LAR 20 mg (NET) | 1.68 |
| Sandostatin LAR 30 mg (NET) | 2.48 |
GH (growth hormone) levels measured on Day 84 in patients with acromegaly (NCT02299089)
Timeframe: Day 84
| Intervention | participants (Number) | |
|---|---|---|
| GH level < 2.5 μg/L | GH level >2.5 μg/L | |
| CAM2029 10 mg q2w (Acromegaly) | 2 | 1 |
| CAM2029 20 mg q4w (Acromegaly) | 2 | 0 |
"Data is presented as number of patients~Within the reference limits (see below)~Above ULN (Upper Limits of Normal)~In the Acromegaly group both males and females were included the age was between 42-70 years. The IGF normal range for the different genders and age are presented below.~REFERENCE VALUES~Males (NMOL/L) 8.34-27.44 (41-45 years) 7.7-26.36 (46-50 years) 7.3-26.34 (51-55 years) 6.64-25.44 (56-60 years) 6.17-25.02 (61-65 years) 5.96-25.48 (66-70 years)~Females (NMOL/L) 8.06-26.89 (41-45 years) 7.39-25.44 (46-50 years) 6.92-24.98 (51-55 years) 5.92-22.7 (56-60 years) 5.42-21.96 (61-65 years) 5.07-21.97 (66-70 years)" (NCT02299089)
Timeframe: Day 84
| Intervention | participants (Number) | |
|---|---|---|
| Within Normal Limits | Above ULN | |
| CAM2029 10 mg q2w (Acromegaly) | 2 | 1 |
| CAM2029 20 mg q4w (Acromegaly) | 1 | 1 |
"Pharmacokinetics (PK) of octreotide after administrations of CAM2029 was determined for the dosing period Day 0 to Day 84 ; AUC0-28d (day*ng/mL).~AUC0-28d: AUC from 0 to 28 days over the dosing intervals (day*ng/mL) for CAM2029 20 mg q4w and CAM2029 10 mg q2w (to estimate AUC0-28d for those patients receiving CAM2029 10 mg q2w, AUC0-14d was multiplied by a factor of 2 as an estimate of the AUC0-28d) dosing intervals" (NCT02299089)
Timeframe: (Day 0) to Day 84 (PK analysis:CAM2029 sampling time points: CAM2029 10mg q2w; 0, 2hours, 24hours, 48hours, 7days and 14days CAM2029 20mg q4w; 0, 2hours, 24hours, 48hours, 7days, 21days and 28days)
| Intervention | day*ng/mL (Mean) | |
|---|---|---|
| AUC0-28d (day*ng/mL) Day 0 | AUC0-28d (day*ng/mL) Day 56 | |
| CAM2029 10 mg q2w (Acromegaly) | 92.9 | 95.6 |
| CAM2029 10 mg q2w (NET) | 72.9 | 83.3 |
| CAM2029 20 mg q4w (Acromegaly) | 72.4 | 78.5 |
| CAM2029 20 mg q4w (NET) | 135 | 135 |
"Pharmacokinetics (PK) of octreotide after administrations of CAM2029 was determined for the dosing period Day 0 to Day 84; Ctrough (ng/mL).~Ctrough; Concentration levels assessed prior to next injection for CAM2029 20 mg q4w and CAM2029 10 mg q2w dosing intervals (ng/mL)" (NCT02299089)
Timeframe: (Day 0) to Day 84 (PK analysis:CAM2029 sampling time points: CAM2029 10mg q2w; 0, 2hours, 24hours, 48hours, 7days and 14days CAM2029 20mg q4w; 0, 2hours, 24hours, 48hours, 7days, 21days and 28days)
| Intervention | ng/ml (Mean) | |
|---|---|---|
| Ctrough (ng/mL) Day 0 | Ctrough (ng(mL) Day 56 | |
| CAM2029 10 mg q2w (Acromegaly) | 1.32 | 1.03 |
| CAM2029 10 mg q2w (NET) | 1.80 | 1.27 |
| CAM2029 20 mg q4w (Acromegaly) | 0.403 | 1.01 |
| CAM2029 20 mg q4w (NET) | 1.81 | 1.73 |
"Number of bowel movements and flushing during period 0 and 1, data is presented as patients experience symptoms~Bowel movement without flushing Bowel movement and flushing No Bowel movement or Flushing" (NCT02299089)
Timeframe: Baseline (Day 0), Day 84
| Intervention | participants (Number) | ||
|---|---|---|---|
| Bowel movements without flushing | Bowel movements with flushing | No Bowel movement or Flushing | |
| CAM2029 10 mg q2w (NET) | 1 | 0 | 0 |
| CAM2029 20 mg q4w (NET) | 0 | 2 | 2 |
"Pharmacokinetics (PK) of octreotide after injection of Sandostatin Long-acting Release (LAR) was determined for the dosing period Day -28 to Day 0; AUC0-28d (day*ng/mL).~AUC0-28d: AUC from 0 to 28 days over the final dosing interval (day*ng/mL) for Sandostatin LAR." (NCT02299089)
Timeframe: Pre-dose; study Day -28- to Day 0 (PK analysis:Sandostatin (LAR®) sampling time points: 0, 1hour, 24hours, 7days, 14days, 21days and 28days)
| Intervention | day*ng/mL (Mean) |
|---|---|
| Sandostatin LAR 10 mg (Acromegaly) | 6.23 |
| Sandostatin LAR 30mg (Acromegaly) | 24.1 |
| Sandostatin LAR 20 mg (NET) | 27.8 |
| Sandostatin LAR 30 mg (NET) | 39.9 |
Safety (number of adverse events and serious adverse events) after repeated doses of CAM2029 (assessment period from Day 0 to Day 84) and single dose Sandostatin LAR (assessment period Day -28 to Day 0) (NCT02299089)
Timeframe: Day -28 to Day 84
| Intervention | Participants (Count of Participants) |
|---|---|
| CAM2029 10 mg q2w (Acromegaly) | 2 |
| CAM2029 20 mg q4w (Acromegaly) | 4 |
| CAM2029 10 mg q2w (NET) | 0 |
| CAM2029 20 mg q4w (NET) | 2 |
| Sandostatin LAR (Acromegaly) | 4 |
| Sandostain LAR (NET) | 2 |
"Pharmacokinetics (PK) of octreotide after administrations of CAM2029 was determined for the dosing period Day 0 to Day 84 ; Cmax (ng/mL).~Cmax (ng/mL): Maximum observed plasma concentration over CAM2029 20 mg q4w and CAM2029 10 mg q2w dosing intervals (ng/mL)" (NCT02299089)
Timeframe: (Day 0) to Day 84 (PK analysis:CAM2029 sampling time points: CAM2029 10mg q2w; 0, 2hours, 24hours, 48hours, 7days and 14days CAM2029 20mg q4w; 0, 2hours, 24hours, 48hours, 7days, 21days and 28days)
| Intervention | ng/mL (Mean) | |
|---|---|---|
| Cmax (ng/mL) Day 0 | Cmax (ng/mL) Day 56 | |
| CAM2029 10 mg q2w (Acromegaly) | 10.4 | 10.6 |
| CAM2029 10 mg q2w (NET) | 6.33 | 5.61 |
| CAM2029 20 mg q4w (Acromegaly) | 13.4 | 11.3 |
| CAM2029 20 mg q4w (NET) | 16.3 | 15.7 |
"Proportion of patients with improved AIS score at the end of the Run-in phase compared to Baseline Acromegaly index of severity (AIS) at the end of Run-in phase compared to Baseline.~The Acromegaly Index of Severity (AIS) symptom score is calculated based on the presence and severity of 5 acromegaly signs/symptoms: headache, swelling of extremities, joint pain, sweating, and fatigue. Each symptom was graded from no symptoms (score 0), to mild symptoms (1), moderate (2), or severe symptoms (3)." (NCT02685709)
Timeframe: 26 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Run-in Phase | 45 |
Proportion of patients with a reduction in the overall number of active acromegaly symptoms at the end of the Run-in phase compared to Baseline (NCT02685709)
Timeframe: 26 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Run-in Phase | 97 |
Proportion of patients who maintain or reduce the overall number of active acromegaly symptoms at the end of the RCT phase (week 62/ EOT) , compared to week 26 (start of the RCT phase (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 41 |
| RCT Phase - Injectables | 26 |
Proportion of patients who maintain or improve their overall Acromegaly index of severity (AIS) score at the end of the RCT phase (improvement defined as a reduction of at least one point in the AIS score), compared to week 26 (start of the RCT phase) (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 40 |
| RCT Phase - Injectables | 25 |
Proportion of patients who are biochemically controlled throughout the RCT phase. A patient was considered biochemically controlled if IGF-1 Time Weighted Average (TWA) during the RCT phase is <1.3 ULN (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 50 |
| RCT Phase - Injectables | 37 |
"Proportion of patients reporting interference with daily activities in the Acromegaly Treatment Satisfaction Questionnaire (Acro-TSQ) during the RCT phase.~Acro-TSQ is a validated PRO tool assessing overall convenience and satisfaction with treatment and patient perception of symptomatic control and adverse drug. It includes 6 scales: Symptom Interference, (4 items); Treatment Convenience, (6 items); Injection Site Interference (2 items); GI Interference (3 items); Treatment Satisfaction, (3 items); and Emotional Reaction (3 items). Each scale score can range from 0 to 100, with 0 representing the lowest (highest burden/lower satisfaction) and 100 representing the best possible score (lowest burden/highest satisfaction) for each of the 6 scales. Positive Acro-TSQ change scores indicate improvement while negative change scores indicate worsening." (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 0 |
| RCT Phase - Injectables | 13 |
"Change in Acromegaly treatment satisfaction questionnaire (ACRO-TSQ) PRO questionnaire from baseline to end of Run-in phase in randomized patients.~Acro-TSQ is a validated PRO tool assessing overall convenience and satisfaction with treatment and patient perception of symptomatic control and adverse drug. It includes 6 scales: Symptom Interference, (4 items); Treatment Convenience, (6 items); Injection Site Interference (2 items); GI Interference (3 items); Treatment Satisfaction, (3 items); and Emotional Reaction (3 items). Each scale score can range from 0 to 100, with 0 representing the lowest (highest burden/lower satisfaction) and 100 representing the best possible score (lowest burden/highest satisfaction) for each of the 6 scales. Positive Acro-TSQ change scores indicate improvement while negative change scores indicate worsening." (NCT02685709)
Timeframe: 26 weeks
| Intervention | score on a scale (Mean) | ||||
|---|---|---|---|---|---|
| Emotional reaction - Change from baseline | GI interference - Change from baseline | Symptom interference- Change from baseline | Treatment convenience - Change from baseline | Treatment satisfaction - Change from baseline | |
| Run-in Phase | 9.65 | 4.24 | 2.45 | 6.37 | 6.73 |
"Work Productivity and Activity Impairment Questionnaire- Run-in phase. WPAI:SHP is a standardized and validated PRO questionnaire to measure health outcomes in clinical trial settings. It measures time missed from work, impairment of work and regular activities due to overall health and symptoms, relative to measures of general health perceptions, role (physical), role (emotional), pain, symptom severity, and global measures of work and interference with regular activity.~The WPAI yields 4 types of scores: (1) absenteeism (work time missed); (2) presenteeism (impairment at work/reduced on-the-job effectiveness); (3) work productivity loss (overall work impairment/absenteeism plus presenteeism); and (4) activity impairment. Each of the 4 WPAI outcomes are expressed as impairment percentages, with higher numbers indicating greater impairment and less productivity (i.e., worse outcomes)." (NCT02685709)
Timeframe: 62 weeks
| Intervention | Percentage change from Run-in baseline (Least Squares Mean) | |||
|---|---|---|---|---|
| Absenteeism (%) | Presenteeism (%) | Work Productivity Loss (%) | Activity Impairment (%) | |
| Run-in Phase | -0.81 | -6.65 | -6.92 | -4.94 |
Proportion of patients reporting injection site reactions (ISRs). Acromegaly treatment satisfaction questionnaire (ACRO-TSQ) is a validated PRO tool assessing overall convenience and satisfaction with treatment and patient perception of symptomatic control and adverse drug. It includes 6 scales: Symptom Interference, (4 items); Treatment Convenience, (6 items); Injection Site Interference (2 items); GI Interference (3 items); Treatment Satisfaction, (3 items); and Emotional Reaction (3 items). Each scale score can range from 0 to 100, with 0 representing the lowest (highest burden/lower satisfaction) and 100 representing the best possible score (lowest burden/highest satisfaction) for each of the 6 scales. Positive ACRO-TSQ change scores indicate improvement while negative change scores indicate worsening. (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 0 |
| RCT Phase - Injectables | 17 |
Proportion of patients on octreotide capsules who are biochemically controlled at the end of the RCT phase defined as IGF-1< 1.3 x ULN based on average of weeks 58 and 62 (NCT02685709)
Timeframe: Average of weeks 58 and 62
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 49 |
| RCT Phase - Injectables | 35 |
Proportion of patients of those completing the RCT phase (at a time octreotide capsules were not commercially available at the specific country), who entered the Study Extension phase, overall and by treatment group (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 34 |
| RCT Phase - Injectables | 18 |
Proportion of patients biochemically controlled at the end of the Run-in phase, defined as average IGF-1 levels during weeks 24 and 26 < 1.3xULN (NCT02685709)
Timeframe: 26 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| Run-in Phase | 94 |
"Change from baselines in EQ-5D-5L Index scores in randomized participants during the Run-in phase.~EQ-5D-5L (five severity levels EQ-5D) is a standardized instrument completed by the patient for use as a measure of health outcome applicable to a wide range of health conditions. It comprises 5 dimensions of health: mobility, ability to self care, ability to undertake usual activities, pain and discomfort, and anxiety and depression. Based on qualitative and quantitative studies conducted by the EuroQol Group, there are 5 levels under each domain: 'no problems' (assigned a value of 1), 'slight problems' (assigned a value of 2), 'moderate problems' (assigned a value of 3), 'severe problems' (assigned a value of 4), and 'unable to/extreme problems' (assigned a value of 5). An EQ-5D Index score is calculated based on the responses to these 5 dimensions of health. Weights for use in the index calculation are not universally available. Higher values represent better health states." (NCT02685709)
Timeframe: 26 weeks
| Intervention | units on a scale (Mean) |
|---|---|
| Run-in Phase | 0.0433 |
"Proportion of patients with clinical and biochemical control at the end of the RCT phase. Patients were considered biochemically and clinically controlled if they met both of the following criteria:~Their IGF-1 TWA during the RCT phase was <1.3 times ULN~Their AIS score at week 62/EOT was maintained or reduced compared to week 26 (start of RCT phase)" (NCT02685709)
Timeframe: Week 62/ End of treatment; EOT
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 36 |
| RCT Phase - Injectables | 27 |
"Work Productivity and Activity Impairment Questionnaire- RCT phase. WPAI:SHP is a standardized and validated PRO questionnaire to measure health outcomes in clinical trial settings. It measures time missed from work, impairment of work and regular activities due to overall health and symptoms, relative to measures of general health perceptions, role (physical), role (emotional), pain, symptom severity, and global measures of work and interference with regular activity.~The WPAI yields 4 types of scores: (1) absenteeism (work time missed); (2) presenteeism (impairment at work/reduced on-the-job effectiveness); (3) work productivity loss (overall work impairment/absenteeism plus presenteeism); and (4) activity impairment. Each of the 4 WPAI outcomes are expressed as impairment percentages, with higher numbers indicating greater impairment and less productivity (i.e., worse outcomes)." (NCT02685709)
Timeframe: 26 weeks
| Intervention | Percentage change from Baseline RCT (Least Squares Mean) | |||
|---|---|---|---|---|
| Absenteeism (%) | Presenteeism (%) | Work productivity loss (%) | Activity impairment (%) | |
| RCT Phase - Injectables | 0.79 | 5.98 | 6.93 | 4.34 |
| RCT Phase - Oral | -0.34 | 1.85 | 1.49 | 0.84 |
Proportion of patients on Octreotide Capsules Who Are Biochemically Controlled at the End of the RCT Phase- Landmark sensitivity analysis- Week 26 responders (NCT02685709)
Timeframe: 62 weeks
| Intervention | Participants (Count of Participants) |
|---|---|
| RCT Phase - Oral | 45 |
| RCT Phase - Injectables | 34 |
"Change in IGF-1 levels from the start of the randomized phase to the end of RCT phase.~Complete Responder (CR) is defined as IGF-1 ≤ 1 x ULN; Partial Responder (PR) is defined as 1 x ULN < IGF-1 < 1.3 x ULN, and Non-Responder (NR): IGF-1 ≥ 1.3 x ULN" (NCT02685709)
Timeframe: Change from Week 26 to week 62
| Intervention | "x Upper limit of normal (ULN)" (Mean) |
|---|---|
| RCT Phase - Oral | -0.01 |
| RCT Phase - Injectables | -0.04 |
Change in GH levels from the start of the randomized phase through the end of RCT phase. (NCT02685709)
Timeframe: Change from Week 26 to week 62
| Intervention | ng/mL (Mean) |
|---|---|
| RCT Phase - Oral | -0.02 |
| RCT Phase - Injectables | 0.27 |
Change in the rate of bronchial secretion at 24, 48, and 72 hours post-intervention initiation, as compared to the baseline rate (NCT02916433)
Timeframe: baseline, 24, 48, 72 hours
| Intervention | mL/24 hr (Number) | |||
|---|---|---|---|---|
| Baseline | 24 hr time point | 48 hr time point | 72 hr time point | |
| Octreotide #1 | 310 | 185 | 120 | NA |
| Octreotide #2 | 200 | 185 | 170 | 140 |
| Usual Care | 220 | 70 | 195 | 25 |
Percentage of patients who were extubated within 72 hours of intervention initiation (NCT02916433)
Timeframe: 72 hours
| Intervention | percentage of patients (Number) |
|---|---|
| Usual Care | 0 |
| Octreotide | 50 |
Number of Patients who Began Rescue Treatment Prior to and Including Week 36 (NCT03252353)
Timeframe: Week 36
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Capsules | 7 |
| Placebo | 19 |
Maintenance of response was defined by using the average IGF-1 level of the last 2 available assessments in the DPC period. If the average IGF-1 is ≤ 1×ULN, a patient was classified as a responder (i.e., maintained their biochemical response). If the average IGF-1 is > 1×ULN, a patient was classified as a non-responder. Patients who discontinue study medication during the DPC period for any reason was classified as non-responders for the primary analysis, regardless of their IGF-1 values. (NCT03252353)
Timeframe: Week 36
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Capsules | 16 |
| Matching Placebo | 5 |
Maintenance of GH response was defined as having mean Growth Hormone (5 measurements 30 minutes apart) < 2.5 ng/mL at the end of the double blind placebo controlled period, out of those who were responders on Somatostatin Receptor Ligands (SRLs) injections at Screening. (NCT03252353)
Timeframe: Week 36
| Intervention | Participants (Count of Participants) |
|---|---|
| Octreotide Capsules | 21 |
| Placebo | 7 |
The percentage of patients who experience a grade 4 or higher renal adverse event. Renal adverse events were graded using CTCAE v4.0 criteria. (NCT03273712)
Timeframe: Initiation of treatment through last follow-up visit (6-9 months after last treatment), up to approximately 10-13 months.
| Intervention | Participants (Count of Participants) |
|---|---|
| 90Y-DOTA-tyr3-Octreotide | 0 |
The percentage of patients who experience a grade 4 or higher irreversible adverse event. Adverse events were graded using CTCAE v4.0 criteria. (NCT03273712)
Timeframe: Initiation of treatment through last follow-up visit (6-9 months after last treatment), up to approximately 10-13 months.
| Intervention | Participants (Count of Participants) |
|---|---|
| 90Y-DOTA-tyr3-Octreotide | 0 |
The time required for a blood pressure wave to travel from the carotid to the femoral artery was measured in meter/sec. This is a measurement of central artery stiffness. Higher numbers indicate stiffer vessels (NCT03520569)
Timeframe: baseline and after 2 hour insulin clamp
| Intervention | m/sec (Mean) |
|---|---|
| Octreotide- Euglycemia | 5.21 |
| Octreotide - Euglycemia- Insulin Clamp | 5.06 |
| Octreotide- Hyperglycemia | 4.79 |
| Octreotide- Hyperglycemia - Insulin Clamp | 5.07 |
Flow mediated dilation measures the change in brachial diameter in response to 5 minutes of ischemia using B-mode ultrasound. It provides an index of nitric oxide generation by the endothelium . (NCT03520569)
Timeframe: baseline and after 2 hour insulin clamp
| Intervention | % change (Mean) |
|---|---|
| Octreotide- Euglycemia | 11.8 |
| Octreotide - Euglycemia- Insulin Clamp | 11.8 |
| Octreotide- Hyperglycemia | 8.9 |
| Octreotide- Hyperglycemia - Insulin Clamp | 8.95 |
The augmentation index (AIx) measured at the radial artery is a measure of systemic arterial stiffness, and is defined as the ratio of augmentation (Δ P) to central pulse pressure and expressed as percent. AIx = (ΔP/PP) x 100, where P = pressure and PP = Pulse Pressure. Higher percentages indicate increased arterial stiffness. (NCT03520569)
Timeframe: baseline and after 2 hour insulin clamp
| Intervention | percentage (Mean) |
|---|---|
| Octreotide- Euglycemia | -4.15 |
| Octreotide - Euglycemia- Insulin Clamp | -2.23 |
| Octreotide- Hyperglycemia | -4.80 |
| Octreotide- Hyperglycemia - Insulin Clamp | -8.45 |
"The primary efficacy endpoint is the proportion of eligible patients whose malignant bowel obstruction clears (de-obstruction) within 7 days of starting the protocol therapy. Patients meeting de-obstruction criteria within 7 days will be deemed treatment successes.~De-obstruction is defined as:~Effective introduction of oral intake (yes/no)~Distinguished from small volumes of oral fluid that may be allowed with unresolved MBO~Tolerating oral liquid diet (day 1 of de-obstruction) that is able to be progressively more solid (oral or enteral)~Cessation of vomiting or ability for NGT or venting G tube to remain clamped without vomiting~Rate of de-obstruction is defined as:~- From the date of study enrollment to the first observation of de-obstruction." (NCT04027348)
Timeframe: Within 7 days of starting protocol therapy
| Intervention | Participants (Count of Participants) |
|---|---|
| Treatment (Octreotide, Dexamethasone, Metoclopramide) | 10 |
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| lanreotide acetate [no description available] | 4.98 | 7 | 0 | ||
| bim 23268 [no description available] | 3.09 | 1 | 0 | ||
| 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 | 5.21 | 9 | 0 | ||
| l 054522 L 054522: somatostatin receptor subtype 2 agonist; structure in first source | 1.99 | 1 | 0 | ||
| cgp 23996 CGP 23996: nonreducible analog of somatostatin; used to test binding sites for somatostatin | 4.19 | 5 | 0 | ||
| prosomatostatin [no description available] | 5.21 | 9 | 0 | heterodetic cyclic peptide; peptide hormone | fungal metabolite; mouse metabolite; rat metabolite |
| betaine glycine betaine : The amino acid betaine derived from glycine. | 3.23 | 1 | 0 | amino-acid betaine; glycine derivative | fundamental metabolite |
| bupropion Bupropion: A propiophenone-derived antidepressant and antismoking agent that inhibits the uptake of DOPAMINE.. bupropion : An aromatic ketone that is propiophenone carrying a tert-butylamino group at position 2 and a chloro substituent at position 3 on the phenyl ring. | 3.23 | 1 | 0 | aromatic ketone; monochlorobenzenes; secondary amino compound | antidepressant; environmental contaminant; xenobiotic |
| aminocaproic acid Aminocaproic Acid: An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.. 6-aminohexanoic acid : An epsilon-amino acid comprising hexanoic acid carrying an amino substituent at position C-6. Used to control postoperative bleeding, and to treat overdose effects of the thrombolytic agents streptokinase and tissue plasminogen activator. | 3.23 | 1 | 0 | amino acid zwitterion; epsilon-amino acid; omega-amino fatty acid | antifibrinolytic drug; hematologic agent; metabolite |
| niacin Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group. | 3.23 | 1 | 0 | pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3 | antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent |
| pyrazinamide pyrazinecarboxamide : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of pyrazinoic acid (pyrazine-2-carboxylic acid) with ammonia. A prodrug for pyrazinoic acid, pyrazinecarboxamide is used as part of multidrug regimens for the treatment of tuberculosis. | 3.23 | 1 | 0 | monocarboxylic acid amide; N-acylammonia; pyrazines | antitubercular agent; prodrug |
| pyridoxine 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol: structure in first source. vitamin B6 : Any member of the group of pyridines that exhibit biological activity against vitamin B6 deficiency. Vitamin B6 deficiency is associated with microcytic anemia, electroencephalographic abnormalities, dermatitis with cheilosis (scaling on the lips and cracks at the corners of the mouth) and glossitis (swollen tongue), depression and confusion, and weakened immune function. Vitamin B6 consists of the vitamers pyridoxine, pyridoxal, and pyridoxamine and their respective 5'-phosphate esters (and includes their corresponding ionized and salt forms). | 3.23 | 1 | 0 | hydroxymethylpyridine; methylpyridines; monohydroxypyridine; vitamin B6 | cofactor; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| thiamine thiamine(1+) : A primary alcohol that is 1,3-thiazol-3-ium substituted by (4-amino-2-methylpyrimidin-5-yl)methyl, methyl and 2-hydroxyethyl groups at positions 3, 4 and 5, respectively. | 3.23 | 1 | 0 | primary alcohol; vitamin B1 | Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite |
| phenytoin [no description available] | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| acebutolol Acebutolol: A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action.. acebutolol : An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol. | 3.23 | 1 | 0 | aromatic amide; ethanolamines; ether; monocarboxylic acid amide; propanolamine; secondary amino compound | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympathomimetic agent |
| acetaminophen Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group. | 3.23 | 1 | 0 | acetamides; phenols | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; cyclooxygenase 3 inhibitor; environmental contaminant; ferroptosis inducer; geroprotector; hepatotoxic agent; human blood serum metabolite; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| acetazolamide Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337) | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfonamide; thiadiazoles | anticonvulsant; diuretic; EC 4.2.1.1 (carbonic anhydrase) inhibitor |
| acetohydroxamic acid acetohydroxamic acid: urease inhibitor. oxime : Compounds of structure R2C=NOH derived from condensation of aldehydes or ketones with hydroxylamine. Oximes from aldehydes may be called aldoximes; those from ketones may be called ketoximes.. N-hydroxyacetimidic acid : A carbohydroximic acid consisting of acetimidic acid having a hydroxy group attached to the imide nitrogen.. acetohydroxamic acid : A member of the class of acetohydroxamic acids that is acetamide in which one of the amino hydrogens has been replaced by a hydroxy group. | 3.23 | 1 | 0 | acetohydroxamic acids; carbohydroximic acid | algal metabolite; EC 3.5.1.5 (urease) inhibitor |
| alaproclate alaproclate: specific 5-hydroxytryptamine uptake inhibitors; RN given refers to (DL)-isomer | 3.23 | 1 | 0 | alpha-amino acid ester | |
| albendazole [no description available] | 3.23 | 1 | 0 | aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester | anthelminthic drug; microtubule-destabilising agent; tubulin modulator |
| albuterol Albuterol: A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.. albuterol : A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). | 3.23 | 1 | 0 | phenols; phenylethanolamines; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; environmental contaminant; xenobiotic |
| alendronate alendronic acid : A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); primary amino compound | bone density conservation agent; EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor |
| alfuzosin alfuzosin: structure given in first source | 3.23 | 1 | 0 | monocarboxylic acid amide; quinazolines; tetrahydrofuranol | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| alosetron alosetron : A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position. | 3.23 | 1 | 0 | imidazoles; pyridoindole | antiemetic; gastrointestinal drug; serotonergic antagonist |
| alprazolam Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238). alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug. | 3.23 | 1 | 0 | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| altretamine Altretamine: A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine. | 3.23 | 1 | 0 | triamino-1,3,5-triazine | |
| amantadine amant: an antiviral compound consisting of an adamantane derivative chemically linked to a water-solube polyanioic matrix; structure in first source | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | analgesic; antiparkinson drug; antiviral drug; dopaminergic agent; NMDA receptor antagonist; non-narcotic analgesic |
| ambenonium ambenonium : A symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens. | 3.23 | 1 | 0 | quaternary ammonium ion | EC 3.1.1.8 (cholinesterase) inhibitor |
| diatrizoic acid Diatrizoate: A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography.. amidotrizoic acid : A member of the class of benzoic acids that is benzoic acid having iodo substituents at the 2-, 4- and 6-positions and acetamido substituents at the 3- and 5-positions. It is used, mainly as its N-methylglucamine and sodium salts, as an X-ray contrast medium in gastrointestinal studies, angiography, and urography. | 3.23 | 1 | 0 | acetamides; benzoic acids; organoiodine compound | environmental contaminant; radioopaque medium; xenobiotic |
| amifostine anhydrous Amifostine: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.. amifostine : An organic thiophosphate that is the S-phospho derivative of 2-[(3-aminopropyl)amino]ethanethiol. A prodrug for the free thiol, WR-1065, which is used as a cytoprotectant in cancer chemotherapy and radiotherapy. | 3.23 | 1 | 0 | diamine; organic thiophosphate | antioxidant; prodrug; radiation protective agent |
| p-aminohippuric acid p-Aminohippuric Acid: The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.. p-aminohippurate : A hippurate that is the conjugate base of p-aminohippuric acid, arising from deprotonation of the carboxy group.. p-aminohippuric acid : An N-acylglycine that is the 4-amino derivative of hippuric acid; used as a diagnostic agent in the measurement of renal plasma flow. | 3.23 | 1 | 0 | N-acylglycine | Daphnia magna metabolite |
| theophylline [no description available] | 3.23 | 1 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| amiodarone Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone; organoiodine compound; tertiary amino compound | cardiovascular drug |
| amitriptyline Amitriptyline: Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines.. amitriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(dimethylamino)propylidene group at position 5. | 3.23 | 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. | 3.23 | 1 | 0 | dihydropyridine; ethyl ester; methyl ester; monochlorobenzenes; primary amino compound | antihypertensive agent; calcium channel blocker; vasodilator agent |
| amoxapine Amoxapine: The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both; it also blocks dopamine receptors. Amoxapine is used for the treatment of depression.. amoxapine : A dibenzooxazepine compound having a chloro substituent at the 2-position and a piperazin-1-yl group at the 11-position. | 3.23 | 1 | 0 | dibenzooxazepine | adrenergic uptake inhibitor; antidepressant; dopaminergic antagonist; geroprotector; serotonin uptake inhibitor |
| anastrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity. | 3.23 | 1 | 0 | benzoic acids; phenyl acetates; salicylates | anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent |
| atenolol Atenolol: A cardioselective beta-1 adrenergic blocker possessing properties and potency similar to PROPRANOLOL, but without a negative inotropic effect.. atenolol : An ethanolamine compound having a (4-carbamoylmethylphenoxy)methyl group at the 1-position and an N-isopropyl substituent. | 3.23 | 1 | 0 | ethanolamines; monocarboxylic acid amide; propanolamine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; sympatholytic agent; xenobiotic |
| azathioprine Azathioprine: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed). azathioprine : A thiopurine that is 6-mercaptopurine in which the mercapto hydrogen is replaced by a 1-methyl-4-nitroimidazol-5-yl group. It is a prodrug for mercaptopurine and is used as an immunosuppressant, prescribed for the treatment of inflammatory conditions and after organ transplantation and also for treatment of Crohn's didease and MS. | 3.23 | 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] | 3.23 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| bendazac bendazac : A monocarboxylic acid that is glycolic acid in which the hydrogen attached to the 2-hydroxy group is replaced by a 1-benzyl-1H-indazol-3-yl group. Although it has anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties and has been used for the treatment of various inflammatory skin disorders, its principal effect is to inhibit the denaturation of proteins. Its lysine salt is used in the management of cataracts. | 3.23 | 1 | 0 | indazoles; monocarboxylic acid | non-steroidal anti-inflammatory drug; radical scavenger |
| bendroflumethiazide Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810). bendroflumethiazide : A sulfonamide consisting of 7-sulfamoyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position 6 is substituted by a trifluoromethyl group and that at position 3 is substituted by a benzyl group. | 3.23 | 1 | 0 | benzothiadiazine; sulfonamide | antihypertensive agent; diuretic |
| benzbromarone Benzbromarone: Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.. benzbromarone : 1-Benzofuran substituted at C-2 and C-3 by an ethyl group and a 3,5-dibromo-4-hydroxybenzoyl group respectively. An inhibitor of CYP2C9, it is used as an anti-gout medication. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ketone | uricosuric drug |
| betaxolol [no description available] | 3.23 | 1 | 0 | propanolamine | antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bethanechol Bethanechol: A slowly hydrolyzing muscarinic agonist with no nicotinic effects. Bethanechol is generally used to increase smooth muscle tone, as in the GI tract following abdominal surgery or in urinary retention in the absence of obstruction. It may cause hypotension, HEART RATE changes, and BRONCHIAL SPASM.. bethanechol : The carbamic acid ester of 2-methylcholine. A slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. | 3.23 | 1 | 0 | carbamate ester; quaternary ammonium ion | muscarinic agonist |
| bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol | |
| biperiden Biperiden: A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine.. biperiden : A member of the class of piperidines that is N-propylpiperidine in which the methyl hydrogens have been replaced by hydroxy, phenyl, and 5-norbornen-2-yl groups. A muscarinic antagonist affecting both the central and peripheral nervous systems, it is used in the treatment of all forms of Parkinson's disease. | 3.23 | 1 | 0 | piperidines; tertiary alcohol; tertiary amino compound | antidote to sarin poisoning; antidyskinesia agent; antiparkinson drug; muscarinic antagonist; parasympatholytic |
| bisacodyl Bisacodyl: A diphenylmethane stimulant laxative used for the treatment of CONSTIPATION and for bowel evacuation. (From Martindale, The Extra Pharmacopoeia, 30th ed, p871) | 3.23 | 1 | 0 | diarylmethane | |
| bisoprolol Bisoprolol: A cardioselective beta-1 adrenergic blocker. It is effective in the management of HYPERTENSION and ANGINA PECTORIS. | 3.23 | 1 | 0 | secondary alcohol; secondary amine | anti-arrhythmia drug; antihypertensive agent; beta-adrenergic antagonist; sympatholytic agent |
| bumetanide [no description available] | 3.23 | 1 | 0 | amino acid; benzoic acids; sulfonamide | diuretic; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 3.23 | 1 | 0 | azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines | anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist |
| busulfan [no description available] | 3.23 | 1 | 0 | methanesulfonate ester | alkylating agent; antineoplastic agent; carcinogenic agent; insect sterilant; teratogenic agent |
| secbutabarbital secbutabarbital: Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital | 3.23 | 1 | 0 | barbiturates | |
| caffeine [no description available] | 3.23 | 1 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. | 3.23 | 1 | 0 | aromatic ether; nitrile; polyether; tertiary amino compound | |
| candesartan candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| carbamazepine Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. | 3.23 | 1 | 0 | dibenzoazepine; ureas | analgesic; anticonvulsant; antimanic drug; drug allergen; EC 3.5.1.98 (histone deacetylase) inhibitor; environmental contaminant; glutamate transporter activator; mitogen; non-narcotic analgesic; sodium channel blocker; xenobiotic |
| carbinoxamine carbinoxamine: Note: tradenames that start with Histex refer to more than one drug. carbinoxamine : An organochlorine compound that is 2-(4-chlorobenzyl)pyridine in which one of the benzylic hydrogens is substituted by 2-(dimethylamino)ethoxy group. It is an ethanolamine-type antihistamine, used as its maleate salt for treating hay fever, as well as mild cases of Parkinson's disease. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist |
| carisoprodol Carisoprodol: A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202). carisoprodol : A carbamate ester that is the mono-N-isopropyl derivative of meprobamate (which is a significant metabolite). Carisoprodol interrupts neuronal communication within the reticular formation and spinal cord, resulting in sedation and alteration in pain perception. It is used as a muscle relaxant in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. | 3.23 | 1 | 0 | carbamate ester | muscle relaxant |
| carvedilol [no description available] | 3.23 | 1 | 0 | carbazoles; secondary alcohol; secondary amino compound | alpha-adrenergic antagonist; antihypertensive agent; beta-adrenergic antagonist; cardiovascular drug; vasodilator agent |
| celecoxib [no description available] | 3.23 | 1 | 0 | organofluorine compound; pyrazoles; sulfonamide; toluenes | cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively. | 3.23 | 1 | 0 | ether; monocarboxylic acid; monochlorobenzenes; piperazines | anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic |
| chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. | 3.23 | 1 | 0 | aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| chlorcyclizine chlorcyclizine: was heading 1964-94 (Prov 1964-73); CHLOROCYCLIZINE & HISTACHLORAZINE were see CHLORCYCLIZINE 1977-94; use PIPERAZINES to search CHLORCYCLIZINE 1966-94; histamine H1-blocker used both orally and topically in allergies and also for the prevention of motion sickness | 3.23 | 1 | 0 | diarylmethane | |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. | 3.23 | 1 | 0 | benzodiazepine | |
| chlormezanone Chlormezanone: A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm.. chlormezanone : A 1,3-thiazine that is 1,3-thiazinan-4-one S,S-dioxide in which a hydrogen at position 2 is substituted by a 4-chlorophenyl group and the hydrogen attached to the nitrogen is substituted by methyl. A non-benzodiazepine muscle relaxant, it was used in the management of anxiety and in the treatment of muscle spasms until being discontinued worldwide by its manufacturer in 1996, due to rare but serious cutaneous reactions. | 3.23 | 1 | 0 | 1,3-thiazine; lactam; monochlorobenzenes; sulfone | antipsychotic agent; anxiolytic drug; muscle relaxant |
| chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug |
| chlorothiazide Chlorothiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p812). thiazide : Heterocyclic compound with sulfur and nitrogen in the ring.. chlorothiazide : 4H-1,2,4-benzothiadiazine 1,1-dioxide in which the hydrogen at position is substituted by chlorine and that at position 7 is substituted by a sulfonamide group. A diuretic, it is used for treatment of oedema and hypertension. | 3.23 | 1 | 0 | benzothiadiazine | antihypertensive agent; diuretic |
| chlorpheniramine Chlorpheniramine: A histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than PROMETHAZINE.. chlorphenamine : A tertiary amino compound that is propylamine which is substituted at position 3 by a pyridin-2-yl group and a p-chlorophenyl group and in which the hydrogens attached to the nitrogen are replaced by methyl groups. A histamine H1 antagonist, it is used to relieve the symptoms of hay fever, rhinitis, urticaria, and asthma. | 3.23 | 1 | 0 | monochlorobenzenes; pyridines; tertiary amino compound | anti-allergic agent; antidepressant; antipruritic drug; H1-receptor antagonist; histamine antagonist; serotonin uptake inhibitor |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 3.23 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| chlorpropamide Chlorpropamide: A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). chlorpropamide : An N-sulfonylurea that is urea in which a hydrogen attached to one of the nitrogens is substituted by 4-chlorobenzenesulfonyl group and a hydrogen attached to the other nitrogen is substituted by propyl group. Chlorpropamide is a hypoglycaemic agent used in the treatment of type 2 (non-insulin-dependent) diabetes mellitus not responding to dietary modification. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | hypoglycemic agent; insulin secretagogue |
| chlorthalidone Chlorthalidone: A benzenesulfonamide-phthalimidine that tautomerizes to a BENZOPHENONES form. It is considered a thiazide-like diuretic. | 3.23 | 1 | 0 | isoindoles; monochlorobenzenes; sulfonamide | |
| chlorzoxazone Chlorzoxazone: A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202). chlorzoxazone : A member of the class of 1,3-benzoxazoles that is 1,3-benzoxazol-2-ol in which the hydrogen atom at position 5 is substituted by chlorine. A centrally acting muscle relaxant with sedative properties, it is used for the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | 1,3-benzoxazoles; heteroaryl hydroxy compound; organochlorine compound | muscle relaxant; sedative |
| cilostazol [no description available] | 3.23 | 1 | 0 | lactam; tetrazoles | anticoagulant; bronchodilator agent; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; fibrin modulating drug; neuroprotective agent; platelet aggregation inhibitor; vasodilator agent |
| cimetidine Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | 3.23 | 1 | 0 | aliphatic sulfide; guanidines; imidazoles; nitrile | adjuvant; analgesic; anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively. | 3.23 | 1 | 0 | aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion | antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic |
| citalopram Citalopram: A furancarbonitrile that is one of the serotonin uptake inhibitors used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.. citalopram : A racemate comprising equimolar amounts of (R)-citalopram and its enantiomer, escitalopram. It is used as an antidepressant, although only escitalopram is active.. 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile : A nitrile that is 1,3-dihydro-2-benzofuran-5-carbonitrile in which one of the hydrogens at position 1 is replaced by a p-fluorophenyl group, while the other is replaced by a 3-(dimethylamino)propyl group. | 3.23 | 1 | 0 | 2-benzofurans; cyclic ether; nitrile; organofluorine compound; tertiary amino compound | |
| clofibrate angiokapsul: contains clofibrate & insoitolnicotinate | 3.23 | 1 | 0 | aromatic ether; ethyl ester; monochlorobenzenes | anticholesteremic drug; antilipemic drug; geroprotector; PPARalpha agonist |
| clomiphene [no description available] | 3.23 | 1 | 0 | tertiary amine | estrogen antagonist; estrogen receptor modulator |
| clomipramine Clomipramine: A tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.. clomipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(dimethylamino)propyl group. One of the more sedating tricyclic antidepressants, it is used as the hydrochloride salt for the treatment of depression as well as obsessive-compulsive disorder and phobias. | 3.23 | 1 | 0 | dibenzoazepine | anticoronaviral agent; antidepressant; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; serotonergic antagonist; serotonergic drug; serotonin uptake inhibitor |
| clonazepam Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses.. clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. | 3.23 | 1 | 0 | clonidine; imidazoline | |
| chlorazepate clorazepic acid : A 1,4-benzodiazepinone in which the oxo group is at position 2, and which is substituted at positions 3, 5, and 7 by carboxy, phenyl and chloro groups, respectively. | 3.23 | 1 | 0 | 1,4-benzodiazepinone | anticonvulsant; anxiolytic drug; GABA modulator; prodrug |
| clotrimazole [no description available] | 3.23 | 1 | 0 | conazole antifungal drug; imidazole antifungal drug; imidazoles; monochlorobenzenes | antiinfective agent; environmental contaminant; xenobiotic |
| cyclobenzaprine cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure. cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant; muscle relaxant; tranquilizing drug |
| cyclofenil Cyclofenil: A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE. | 3.23 | 1 | 0 | organic molecular entity | |
| cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| dapsone [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | acyclic desferrioxamine | bacterial metabolite; ferroptosis inhibitor; iron chelator; siderophore |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 3.23 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 3.23 | 1 | 0 | primary amine | |
| diazepam Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| diazoxide Diazoxide: A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.. diazoxide : A benzothiadiazine that is the S,S-dioxide of 2H-1,2,4-benzothiadiazine which is substituted at position 3 by a methyl group and at position 7 by chlorine. A peripheral vasodilator, it increases the concentration of glucose in the plasma and inhibits the secretion of insulin by the beta- cells of the pancreas. It is used orally in the management of intractable hypoglycaemia and intravenously in the management of hypertensive emergencies. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfone | antihypertensive agent; beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; diuretic; K-ATP channel agonist; sodium channel blocker; sympathomimetic agent; vasodilator agent |
| diclofenac Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; dichlorobenzene; monocarboxylic acid; secondary amino compound | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| dichlorphenamide Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma. | 3.23 | 1 | 0 | dichlorobenzene; sulfonamide | antiglaucoma drug; EC 4.2.1.1 (carbonic anhydrase) inhibitor; ophthalmology drug |
| dicyclomine Dicyclomine: A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms.. dicyclomine : The ester resulting from the formal condensation of 1-cyclohexylcyclohexanecarboxylic acid with 2-(diethylamino)ethanol. An anticholinergic, it is used as the hydrochloride to treat or prevent spasm in the muscles of the gastrointestinal tract, particularly that associated with irritable bowel syndrome. | 3.23 | 1 | 0 | carboxylic ester; tertiary amine | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| pentetic acid Pentetic Acid: An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. | 3.23 | 1 | 0 | pentacarboxylic acid | copper chelator |
| diflunisal Diflunisal: A salicylate derivative and anti-inflammatory analgesic with actions and side effects similar to those of ASPIRIN.. diflunisal : An organofluorine compound comprising salicylic acid having a 2,4-difluorophenyl group at the 5-position. | 3.23 | 1 | 0 | monohydroxybenzoic acid; organofluorine compound | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| dimercaprol Dimercaprol: An anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning.. dimercaprol : A dithiol that is propane-1,2-dithiol in which one of the methyl hydrogens is replaced by a hydroxy group. a chelating agent originally developed during World War II as an experimental antidote against the arsenic-based poison gas Lewisite, it has been used clinically since 1949 for the treatment of poisoning by arsenic, mercury and gold. It can also be used for treatment of poisoning by antimony, bismuth and possibly thallium, and (with sodium calcium edetate) in cases of acute leaad poisoning. Administration is by (painful) intramuscular injection of a suspension of dimercaprol in peanut oil, typically every 4 hours for 2-10 days depending on the toxicity. In the past, dimercaprol was also used for the treatment of Wilson's disease, a severely debilitating genetic disorder in which the body tends to retain copper, with resultant liver and brain injury. | 3.23 | 1 | 0 | dithiol; primary alcohol | chelator |
| diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration. | 3.23 | 1 | 0 | ether; tertiary amino compound | anti-allergic agent; antidyskinesia agent; antiemetic; antiparkinson drug; antipruritic drug; antitussive; H1-receptor antagonist; local anaesthetic; muscarinic antagonist; oneirogen; sedative |
| dipyridamole Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752). dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. | 3.23 | 1 | 0 | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| disopyramide Disopyramide: A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties.. disopyramide : A monocarboxylic acid amide that is butanamide substituted by a diisopropylamino group at position 4, a phenyl group at position 2 and a pyridin-2-yl group at position 2. It is used as a anti-arrhythmia drug. | 3.23 | 1 | 0 | monocarboxylic acid amide; pyridines; tertiary amino compound | anti-arrhythmia drug |
| disulfiram [no description available] | 3.23 | 1 | 0 | organic disulfide; organosulfur acaricide | angiogenesis inhibitor; antineoplastic agent; apoptosis inducer; EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor; EC 3.1.1.1 (carboxylesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 5.99.1.2 (DNA topoisomerase) inhibitor; ferroptosis inducer; fungicide; NF-kappaB inhibitor |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 3.23 | 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 |
| donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group. | 3.23 | 1 | 0 | aromatic ether; indanones; piperidines; racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent |
| doxapram Doxapram: A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225). doxapram : A member of the class of pyrrolidin-2-ones that is N-ethylpyrrolidin-2-one in which both of the hydrogens at the 3 position (adjacent to the carbonyl group) are substituted by phenyl groups, and one of the hydrogens at the 4 position is substituted by a 2-(morpholin-4-yl)ethyl group. A central and respiratory stimulant with a brief duration of action, it is used (generally as the hydrochloride or the hydrochloride hydrate) as a temporary treatment of acute respiratory failure, particularly when superimposed on chronic obstructive pulmonary disease, and of postoperative respiratory depression. It has also been used for treatment of postoperative shivering. | 3.23 | 1 | 0 | morpholines; pyrrolidin-2-ones | central nervous system stimulant |
| doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure. | 3.23 | 1 | 0 | aromatic amine; benzodioxine; monocarboxylic acid amide; N-acylpiperazine; N-arylpiperazine; quinazolines | alpha-adrenergic antagonist; antihyperplasia drug; antihypertensive agent; antineoplastic agent; vasodilator agent |
| doxepin Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.. doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. | 3.23 | 1 | 0 | dibenzooxepine; tertiary amino compound | antidepressant |
| doxylamine Doxylamine: Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM. | 3.23 | 1 | 0 | pyridines; tertiary amine | anti-allergic agent; antiemetic; antitussive; cholinergic antagonist; H1-receptor antagonist; histamine antagonist; sedative |
| droperidol Droperidol: A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593). droperidol : An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; organofluorine compound | anaesthesia adjuvant; antiemetic; dopaminergic antagonist; first generation antipsychotic |
| dyphylline Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.. dyphylline : An oxopurine that is theophylline bearing a 2,3-dihydroxypropyl group at the 7 position. It has broncho- and vasodilator properties, and is used in the treatment of asthma, cardiac dyspnea, and bronchitis. It is also an ingredient in preparations that have been promoted for coughs. | 3.23 | 1 | 0 | oxopurine; propane-1,2-diols | bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; muscle relaxant; vasodilator agent |
| edrophonium Edrophonium: A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles.. edrophonium : A quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals. | 3.23 | 1 | 0 | phenols; quaternary ammonium ion | antidote; diagnostic agent; EC 3.1.1.8 (cholinesterase) inhibitor |
| estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia. | 3.23 | 1 | 0 | triazoles; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA modulator |
| ethacrynic acid Ethacrynic Acid: A compound that inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. This compound has been classified as a loop or high ceiling diuretic.. etacrynic acid : An aromatic ether that is phenoxyacetic acid in which the phenyl ring is substituted by chlorines at positions 2 and 3, and by a 2-methylidenebutanoyl group at position 4. It is a loop diuretic used to treat high blood pressure resulting from diseases such as congestive heart failure, liver failure, and kidney failure. It is also a glutathione S-transferase (EC 2.5.1.18) inhibitor. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor; ion transport inhibitor; loop diuretic |
| ethosuximide Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.. ethosuximide : A dicarboximide that is pyrrolidine-2,5-dione in which the hydrogens at position 3 are substituted by one methyl and one ethyl group. An antiepileptic, it is used in the treatment of absence seizures and may be used for myoclonic seizures, but is ineffective against tonic-clonic seizures. | 3.23 | 1 | 0 | dicarboximide; pyrrolidinone | anticonvulsant; geroprotector; T-type calcium channel blocker |
| ethotoin ethotoin: was heading 1966-94 (see under HYDANTOINS 1966-90); use HYDANTOINS to search ETHOTOIN 1966-94. ethotoin : An imidazolidine-2,4-dione that is hydantoin substituted by ethyl and phenyl at positions 3 and 5, respectively. An antiepileptic, it is less toxic than phenytoin but also less effective. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| etidronate Etidronic Acid: A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.. etidronic acid : A 1,1-bis(phosphonic acid) that is (ethane-1,1-diyl)bis(phosphonic acid) having a hydroxy substituent at the 1-position. It inhibits the formation, growth, and dissolution of hydroxyapatite crystals by chemisorption to calcium phosphate surfaces. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid) | antineoplastic agent; bone density conservation agent; chelator |
| etodolac Etodolac: A non-steroidal anti-inflammatory agent and cyclooxygenase-2 (COX-2) inhibitor with potent analgesic and anti-arthritic properties. It has been shown to be effective in the treatment of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; ANKYLOSING SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).. etodolac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is substituted by a 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indol-1-yl moiety. A preferential inhibitor of cyclo-oxygenase 2 and non-steroidal anti-inflammatory, it is used for the treatment of rheumatoid arthritis and osteoarthritis, and for the alleviation of postoperative pain. Administered as the racemate, only the (S)-enantiomer is active. | 3.23 | 1 | 0 | monocarboxylic acid; organic heterotricyclic compound | antipyretic; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| brl 42810 [no description available] | 3.23 | 1 | 0 | 2-aminopurines; acetate ester | antiviral drug; prodrug |
| felbamate Felbamate: A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.. felbamate : The bis(carbamate ester) of 2-phenylpropane-1,3-diol. An anticonvulsant, it is used in the treatment of epilepsy. | 3.23 | 1 | 0 | carbamate ester | anticonvulsant; neuroprotective agent |
| felodipine Felodipine: A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.. felodipine : The mixed (methyl, ethyl) diester of 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid. A calcium-channel blocker, it lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. It is used in the management of hypertension and angina pectoris. | 3.23 | 1 | 0 | dichlorobenzene; dihydropyridine; ethyl ester; methyl ester | anti-arrhythmia drug; antihypertensive agent; calcium channel blocker; vasodilator agent |
| fenofibrate Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE | 3.23 | 1 | 0 | aromatic ether; chlorobenzophenone; isopropyl ester; monochlorobenzenes | antilipemic drug; environmental contaminant; geroprotector; xenobiotic |
| fenoldopam Fenoldopam: A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. | 3.23 | 1 | 0 | benzazepine | alpha-adrenergic agonist; antihypertensive agent; dopamine agonist; dopaminergic antagonist; vasodilator agent |
| fenoprofen Fenoprofen: A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent.. fenoprofen : A monocarboxylic acid that is propanoic acid in which one of the hydrogens at position 2 is substituted by a 3-phenoxyphenyl group. A non-steroidal anti-inflammatory drug, the dihydrate form of the calcium salt is used for the management of mild to moderate pain and for the relief of pain and inflammation associated with disorders such as arthritis. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| fexofenadine fexofenadine: a second generation antihistamine; metabolite of the antihistaminic drug terfenadine; structure in first source; RN refers to HCl. fexofenadine : A piperidine-based anti-histamine compound. | 3.23 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; H1-receptor antagonist |
| fipexide fipexide: regulates dopaminergic systems at macromolecular level | 3.23 | 1 | 0 | benzodioxoles | |
| flavoxate Flavoxate: A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.. flavoxate : A carboxylic ester resulting from the formal condensation of 3-methylflavone-8-carboxylic acid with 2-(1-piperidinyl)ethanol. | 3.23 | 1 | 0 | carboxylic ester; flavones; piperidines; tertiary amino compound | antispasmodic drug; muscarinic antagonist; parasympatholytic |
| flecainide Flecainide: A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.. flecainide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with the primary amino group of piperidin-2-ylmethylamine. An antiarrhythmic agent used (in the form of its acetate salt) to prevent and treat tachyarrhythmia (abnormal fast rhythm of the heart). | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid amide; organofluorine compound; piperidines | anti-arrhythmia drug |
| fluconazole Fluconazole: Triazole antifungal agent that is used to treat oropharyngeal CANDIDIASIS and cryptococcal MENINGITIS in AIDS.. fluconazole : A member of the class of triazoles that is propan-2-ol substituted at position 1 and 3 by 1H-1,2,4-triazol-1-yl groups and at position 2 by a 2,4-difluorophenyl group. It is an antifungal drug used for the treatment of mucosal candidiasis and for systemic infections including systemic candidiasis, coccidioidomycosis, and cryptococcosis. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; tertiary alcohol; triazole antifungal drug | environmental contaminant; P450 inhibitor; xenobiotic |
| flucytosine Flucytosine: A fluorinated cytosine analog that is used as an antifungal agent.. flucytosine : An organofluorine compound that is cytosine that is substituted at position 5 by a fluorine. A prodrug for the antifungal 5-fluorouracil, it is used for the treatment of systemic fungal infections. | 3.23 | 1 | 0 | aminopyrimidine; nucleoside analogue; organofluorine compound; pyrimidine antifungal drug; pyrimidone | prodrug |
| fluphenazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; organofluorine compound; phenothiazines | anticoronaviral agent; dopaminergic antagonist; phenothiazine antipsychotic drug |
| flumazenil Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses.. flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. | 3.23 | 1 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| fluorescite fluorescein (acid form) : A xanthene dye that is highly fluorescent and commonly used as a fluorescent tracer. | 3.23 | 1 | 0 | benzoic acids; cyclic ketone; hydroxy monocarboxylic acid; organic heterotricyclic compound; phenols; xanthene dye | fluorescent dye; radioopaque medium |
| fluorouracil Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth. | 3.23 | 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. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| flurazepam Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; monofluorobenzenes; organochlorine compound; tertiary amino compound | anticonvulsant; anxiolytic drug; GABAA receptor agonist; sedative |
| flurbiprofen Flurbiprofen: An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.. flurbiprofen : A monocarboxylic acid that is a 2-fluoro-[1,1'-biphenyl-4-yl] moiety linked to C-2 of propionic acid. A non-steroidal anti-inflammatory, analgesic and antipyretic, it is used as a pre-operative anti-miotic as well as orally for arthritis or dental pain. | 3.23 | 1 | 0 | fluorobiphenyl; monocarboxylic acid | antipyretic; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| flutamide Flutamide: An antiandrogen with about the same potency as cyproterone in rodent and canine species. | 3.23 | 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. | 3.23 | 1 | 0 | pyrazoles | antidote; EC 1.1.1.1 (alcohol dehydrogenase) inhibitor; protective agent |
| foscarnet Foscarnet: An antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.. phosphonoformic acid : Phosphoric acid in which one of the hydroxy groups is replaced by a carboxylic acid group. It is used as the trisodium salt as an antiviral agent in the treatment of cytomegalovirus retinitis (CMV retinitis, an inflamation of the retina that can lead to blindness) and as an alternative to ganciclovir for AIDS patients who require concurrent antiretroviral therapy but are unable to tolerate ganciclovir due to haematological toxicity. | 3.23 | 1 | 0 | carboxylic acid; one-carbon compound; phosphonic acids | antiviral drug; geroprotector; HIV-1 reverse transcriptase inhibitor; sodium-dependent Pi-transporter inhibitor |
| furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure. | 3.23 | 1 | 0 | chlorobenzoic acid; furans; sulfonamide | environmental contaminant; loop diuretic; xenobiotic |
| gabapentin Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic |
| gemfibrozil [no description available] | 3.23 | 1 | 0 | aromatic ether | antilipemic drug |
| glafenine Glafenine: An anthranilic acid derivative with analgesic properties used for the relief of all types of pain.. glafenine : A carboxylic ester that is 2,3-dihydroxypropyl anthranilate in which the amino group is substituted by a 7-chloroquinolin-4-yl group. A non-steroidal anti-inflammatory drug, glafenine and its hydrochloride salt were used for the relief of all types of pain, but high incidence of anaphylactic reactions resulted in their withdrawal from the market. | 3.23 | 1 | 0 | aminoquinoline; carboxylic ester; glycol; organochlorine compound; secondary amino compound | inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| glimepiride glimepiride: structure given in first source | 3.23 | 1 | 0 | sulfonamide | |
| glipizide Glipizide: An oral hypoglycemic agent which is rapidly absorbed and completely metabolized.. glipizide : An N-sulfonylurea that is glyburide in which the (5-chloro-2-methoxybenzoyl group is replaced by a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it is used in the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; N-sulfonylurea; pyrazines | EC 2.7.1.33 (pantothenate kinase) inhibitor; hypoglycemic agent; insulin secretagogue |
| glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-sulfonylurea | anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester [no description available] | 3.23 | 1 | 0 | benzenes | |
| granisetron [no description available] | 3.23 | 1 | 0 | aromatic amide; indazoles | |
| guaifenesin Guaifenesin: An expectorant that also has some muscle relaxing action. It is used in many cough preparations. | 3.23 | 1 | 0 | methoxybenzenes | |
| guanethidine Guanethidine: An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues.. guanethidine : A member of the class of guanidines in which one of the hydrogens of the amino group has been replaced by a 2-azocan-1-ylethyl group.. guanethidine sulfate : A organic sulfate salt composed of two molecules of guanethidine and one of sulfuric acid. | 3.23 | 1 | 0 | azocanes; guanidines | adrenergic antagonist; antihypertensive agent; sympatholytic agent |
| guanfacine Guanfacine: A centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS. | 3.23 | 1 | 0 | acetamides | |
| guanidine Guanidine: A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.. guanidine : An aminocarboxamidine, the parent compound of the guanidines. | 3.23 | 1 | 0 | carboxamidine; guanidines; one-carbon compound | |
| haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety. | 3.23 | 1 | 0 | aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol | antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist |
| hydralazine Hydralazine: A direct-acting vasodilator that is used as an antihypertensive agent.. hydralazine : The 1-hydrazino derivative of phthalazine; a direct-acting vasodilator that is used as an antihypertensive agent. | 3.23 | 1 | 0 | azaarene; hydrazines; ortho-fused heteroarene; phthalazines | antihypertensive agent; vasodilator agent |
| hydrochlorothiazide Hydrochlorothiazide: A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.. hydrochlorothiazide : A benzothiadiazine that is 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide substituted by a chloro group at position 6 and a sulfonamide at 7. It is diuretic used for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | benzothiadiazine; organochlorine compound; sulfonamide | antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| hydroflumethiazide Hydroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p822). hydroflumethiazide : A benzothiadiazine consisting of a 3,4-dihydro-HH-1,2,4-benzothiadiazine bicyclic system dioxygenated on sulfur and carrying trifluoromethyl and aminosulfonyl groups at positions 6 and 7 respectively. A diuretic with actions and uses similar to those of hydrochlorothiazide. | 3.23 | 1 | 0 | benzothiadiazine; thiazide | antihypertensive agent; diuretic |
| hydroxychloroquine Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions. | 3.23 | 1 | 0 | aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound | anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug |
| hydroxyurea [no description available] | 3.23 | 1 | 0 | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent |
| hydroxyzine Hydroxyzine: A histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.. hydroxyzine : A N-alkylpiperazine that is piperzine in which the nitrogens atoms are substituted by 2-(2-hydroxyethoxy)ethyl and (4-chlorophenyl)(phenyl)methyl groups respectively. | 3.23 | 1 | 0 | hydroxyether; monochlorobenzenes; N-alkylpiperazine | anticoronaviral agent; antipruritic drug; anxiolytic drug; dermatologic drug; H1-receptor antagonist |
| ibuprofen Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine | 3.23 | 1 | 0 | monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; radical scavenger; xenobiotic |
| phenelzine Phenelzine: One of the MONOAMINE OXIDASE INHIBITORS used to treat DEPRESSION; PHOBIC DISORDERS; and PANIC. | 3.23 | 1 | 0 | primary amine | |
| lidocaine Lidocaine: A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.. lidocaine : The monocarboxylic acid amide resulting from the formal condensation of N,N-diethylglycine with 2,6-dimethylaniline. | 3.23 | 1 | 0 | benzenes; monocarboxylic acid amide; tertiary amino compound | anti-arrhythmia drug; drug allergen; environmental contaminant; local anaesthetic; xenobiotic |
| ifosfamide [no description available] | 3.23 | 1 | 0 | ifosfamides | alkylating agent; antineoplastic agent; environmental contaminant; immunosuppressive agent; xenobiotic |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 3.23 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| amrinone Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell.. amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. | 3.23 | 1 | 0 | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| indapamide Indapamide: A benzamide-sulfonamide-indole derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. indapamide : A sulfonamide formed by condensation of the carboxylic group of 4-chloro-3-sulfamoylbenzoic acid with the amino group of 2-methyl-2,3-dihydro-1H-indol-1-amine. | 3.23 | 1 | 0 | indoles; organochlorine compound; sulfonamide | antihypertensive agent; diuretic |
| indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis. | 3.23 | 1 | 0 | aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole | analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic |
| ioversol [no description available] | 3.23 | 1 | 0 | amidobenzoic acid | |
| iproniazid [no description available] | 3.23 | 1 | 0 | carbohydrazide; pyridines | |
| avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. | 3.23 | 1 | 0 | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| isocarboxazid Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) | 3.23 | 1 | 0 | benzenes | |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 3.23 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| isoproterenol Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.. isoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders. | 3.23 | 1 | 0 | catechols; secondary alcohol; secondary amino compound | beta-adrenergic agonist; bronchodilator agent; cardiotonic drug; sympathomimetic agent |
| isoxsuprine Isoxsuprine: A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. | 3.23 | 1 | 0 | alkylbenzene | |
| isradipine Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. | 3.23 | 1 | 0 | benzoxadiazole; dihydropyridine; isopropyl ester; methyl ester | |
| itraconazole [no description available] | 3.23 | 1 | 0 | piperazines | |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 3.23 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively. | 3.23 | 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. | 3.23 | 1 | 0 | benzophenones; oxo monocarboxylic acid | antipyretic; drug allergen; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| ketorolac Ketorolac: A pyrrolizine carboxylic acid derivative structurally related to INDOMETHACIN. It is an NSAID and is used principally for its analgesic activity. (From Martindale The Extra Pharmacopoeia, 31st ed). ketorolac : A racemate comprising equimolar amounts of (R)-(+)- and (S)-(-)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid. While only the (S)-(-) enantiomer is a COX1 and COX2 inhibitor, the (R)-(+) enantiomer exhibits potent analgesic activity. A non-steroidal anti-inflammatory drug, ketorolac is mainly used (generally as the tromethamine salt) for its potent analgesic properties in the short-term management of post-operative pain, and in eye drops to relieve the ocular itching associated with seasonal allergic conjunctivitis. It was withdrawn from the market in many countries in 1993 following association with haemorrhage and renal failure.. 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid : A member of the class of pyrrolizines that is 2,3-dihydro-1H-pyrrolizine which is substituted at positions 1 and 5 by carboxy and benzoyl groups, respectively. | 3.23 | 1 | 0 | amino acid; aromatic ketone; monocarboxylic acid; pyrrolizines; racemate | analgesic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| labetalol Labetalol: A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.. labetalol : A diastereoisomeric mixture of approximately equal amounts of all four possible stereoisomers ((R,S)-labetolol, (S,R)-labetolol, (S,S)-labetalol and (R,R)-labetalol). It is an adrenergic antagonist used to treat high blood pressure.. 2-hydroxy-5-{1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl}benzamide : A member of the class of benzamides that is benzamide substituted by a hydroxy group at position 2 and by a 1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl group at position 5. | 3.23 | 1 | 0 | benzamides; benzenes; phenols; primary carboxamide; salicylamides; secondary alcohol; secondary amino compound | |
| lamotrigine [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; dichlorobenzene; primary arylamine | anticonvulsant; antidepressant; antimanic drug; calcium channel blocker; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; excitatory amino acid antagonist; geroprotector; non-narcotic analgesic; xenobiotic |
| lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| leflunomide Leflunomide: An isoxazole derivative that inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway. It is used an immunosuppressive agent in the treatment of RHEUMATOID ARTHRITIS and PSORIATIC ARTHRITIS.. leflunomide : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-methyl-1,2-oxazole-4-carboxylic acid with the anilino group of 4-(trifluoromethyl)aniline. The prodrug of teriflunomide. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; isoxazoles; monocarboxylic acid amide | antineoplastic agent; antiparasitic agent; EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; hepatotoxic agent; immunosuppressive agent; non-steroidal anti-inflammatory drug; prodrug; pyrimidine synthesis inhibitor; tyrosine kinase inhibitor |
| letrozole [no description available] | 3.23 | 1 | 0 | nitrile; triazoles | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor |
| lomefloxacin lomefloxacin: structure given in first source. lomefloxacin : A fluoroquinolone antibiotic, used (generally as the hydrochloride salt) to treat bacterial infections including bronchitis and urinary tract infections. It is also used to prevent urinary tract infections prior to surgery. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antimicrobial agent; antitubercular agent; photosensitizing agent |
| lomustine [no description available] | 3.23 | 1 | 0 | N-nitrosoureas; organochlorine compound | alkylating agent; antineoplastic agent |
| loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease. | 3.23 | 1 | 0 | monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol | anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist |
| loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders. | 3.23 | 1 | 0 | benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide | anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist |
| lorazepam Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | 3.23 | 1 | 0 | benzodiazepine | |
| losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position | 3.23 | 1 | 0 | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| loxapine Loxapine: An antipsychotic agent used in SCHIZOPHRENIA. | 3.23 | 1 | 0 | dibenzooxazepine | antipsychotic agent; dopaminergic antagonist |
| maprotiline Maprotiline: A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. | 3.23 | 1 | 0 | anthracenes | |
| mebendazole Mebendazole: A benzimidazole that acts by interfering with CARBOHYDRATE METABOLISM and inhibiting polymerization of MICROTUBULES.. mebendazole : A carbamate ester that is methyl 1H-benzimidazol-2-ylcarbamate substituted by a benzoyl group at position 5. | 3.23 | 1 | 0 | aromatic ketone; benzimidazoles; carbamate ester | antinematodal drug; microtubule-destabilising agent; tubulin modulator |
| mecamylamine Mecamylamine: A nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. | 3.23 | 1 | 0 | primary aliphatic amine | |
| mechlorethamine nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR. | 3.23 | 1 | 0 | nitrogen mustard; organochlorine compound | alkylating agent |
| meclizine Meclizine: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. | 3.23 | 1 | 0 | diarylmethane | |
| meclofenamic acid Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; organochlorine compound; secondary amino compound | analgesic; anticonvulsant; antineoplastic agent; antipyretic; antirheumatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mefenamic acid Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | aminobenzoic acid; secondary amino compound | analgesic; antipyretic; antirheumatic drug; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; non-steroidal anti-inflammatory drug; xenobiotic |
| memantine [no description available] | 3.23 | 1 | 0 | adamantanes; primary aliphatic amine | antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist |
| mepenzolate mepenzolic acid: anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure | 3.23 | 1 | 0 | diarylmethane | |
| meperidine Meperidine: A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration.. pethidine : A piperidinecarboxylate ester that is piperidine which is substituted by a methyl group at position 1 and by phenyl and ethoxycarbonyl groups at position 4. It is an analgesic which is used for the treatment of moderate to severe pain, including postoperative pain and labour pain. | 3.23 | 1 | 0 | ethyl ester; piperidinecarboxylate ester; tertiary amino compound | antispasmodic drug; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| mephenytoin Mephenytoin: An anticonvulsant effective in tonic-clonic epilepsy (EPILEPSY, TONIC-CLONIC). It may cause blood dyscrasias.. mephenytoin : An imidazolidine-2,4-dione (hydantoin) in which the imidazolidine nucleus carries a methyl group at N-3 and has ethyl and phenyl substituents at C-5. An anticonvulsant, it is no longer available in the USA or the UK but is still studied largely because of its interesting hydroxylation polymorphism. | 3.23 | 1 | 0 | imidazolidine-2,4-dione | anticonvulsant |
| mepivacaine Mepivacaine: A local anesthetic that is chemically related to BUPIVACAINE but pharmacologically related to LIDOCAINE. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168). mepivacaine : A piperidinecarboxamide in which N-methylpipecolic acid and 2,6-dimethylaniline have combined to form the amide bond. It is used as a local amide-type anaesthetic. | 3.23 | 1 | 0 | piperidinecarboxamide | drug allergen; local anaesthetic |
| meprobamate Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) | 3.23 | 1 | 0 | organic molecular entity | |
| mesalamine Mesalamine: An anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE. (From Martindale, The Extra Pharmacopoeia, 30th ed). mesalamine : A monohydroxybenzoic acid that is salicylic acid substituted by an amino group at the 5-position. | 3.23 | 1 | 0 | amino acid; aromatic amine; monocarboxylic acid; monohydroxybenzoic acid; phenols | non-steroidal anti-inflammatory drug |
| mesoridazine Mesoridazine: A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE.. mesoridazine : A phenothiazine substituted at position 2 (para to the S atom) by a methylsulfinyl group, and on the nitrogen by a 2-(1-methylpiperidin-2-yl)ethyl group. | 3.23 | 1 | 0 | phenothiazines; sulfoxide; tertiary amino compound | dopaminergic antagonist; first generation antipsychotic |
| metaproterenol Metaproterenol: A beta-2 adrenergic agonist used in the treatment of ASTHMA and BRONCHIAL SPASM.. orciprenaline : A racemate composed of equimolar amounts of (R)- and (S)-orciprenaline. Used (as its sulfate salt) to relax the airway muscles and improve breathing for patients suffering from asthma or bronchitis.. 5-[1-hydroxy-2-(isopropanylamino)ethyl]benzene-1,3-diol : A member of the class of resorcinols bearing an additional 1-hydroxy-2-(isopropanylamino)ethyl substituent at position 5 of resorcinol itself. | 3.23 | 1 | 0 | aralkylamino compound; phenylethanolamines; resorcinols; secondary alcohol; secondary amino compound | |
| metformin Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1. | 3.23 | 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. | 3.23 | 1 | 0 | benzenes; diarylmethane; ketone; tertiary amino compound | |
| methazolamide Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma. | 3.23 | 1 | 0 | sulfonamide; thiadiazoles | |
| methocarbamol Methocarbamol: A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206). methocarbamol : A racemate comprising equimolar amounts of (R)- and (S)-methocarbamol. A centrally acting skeletal muscle relaxant, it is used as an adjunct in the short-term symptomatic treatment of painful muscle spasm. The (R)-enantiomer is more active than the (S)-enantiomer.. 2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate : A carbamate ester that is glycerol in which one of the primary alcohol groups has been converted to its 2-methoxyphenyl ether while the other has been converted to the corresponding carbamate ester. | 3.23 | 1 | 0 | aromatic ether; carbamate ester; secondary alcohol | |
| methoxsalen Methoxsalen: A naturally occurring furocoumarin compound found in several species of plants, including Psoralea corylifolia. It is a photoactive substance that forms DNA ADDUCTS in the presence of ultraviolet A irradiation.. methoxsalen : A member of the class of psoralens that is 7H-furo[3,2-g]chromen-7-one in which the 9 position is substituted by a methoxy group. It is a constituent of the fruits of Ammi majus. Like other psoralens, trioxsalen causes photosensitization of the skin. It is administered topically or orally in conjunction with UV-A for phototherapy treatment of vitiligo and severe psoriasis. | 3.23 | 1 | 0 | aromatic ether; psoralens | antineoplastic agent; cross-linking reagent; dermatologic drug; photosensitizing agent; plant metabolite |
| methyclothiazide Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) | 3.23 | 1 | 0 | benzothiadiazine | |
| methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group. | 3.23 | 1 | 0 | beta-amino acid ester; methyl ester; piperidines | |
| metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine. | 3.23 | 1 | 0 | benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound | antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic |
| metolazone Metolazone: A quinazoline-sulfonamide derived DIURETIC that functions by inhibiting SODIUM CHLORIDE SYMPORTERS.. metolazone : A quinazoline that consists of 1,2,3,4-tetrahydroquinazolin-4-one bearing additional methyl, 2-tolyl, sulfamyl and chloro substituents at positions 2, 3, 6 and 7 respectively. A quinazoline diuretic, with properties similar to thiazide diuretics. | 3.23 | 1 | 0 | organochlorine compound; quinazolines; sulfonamide | antihypertensive agent; diuretic; ion transport inhibitor |
| metoprolol Metoprolol: A selective adrenergic beta-1 blocking agent that is commonly used to treat ANGINA PECTORIS; HYPERTENSION; and CARDIAC ARRHYTHMIAS.. metoprolol : A propanolamine that is 1-(propan-2-ylamino)propan-2-ol substituted by a 4-(2-methoxyethyl)phenoxy group at position 1. | 3.23 | 1 | 0 | aromatic ether; propanolamine; secondary alcohol; secondary amino compound | antihypertensive agent; beta-adrenergic antagonist; environmental contaminant; geroprotector; xenobiotic |
| metronidazole Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death. | 3.23 | 1 | 0 | C-nitro compound; imidazoles; primary alcohol | antiamoebic agent; antibacterial drug; antimicrobial agent; antiparasitic agent; antitrichomonal drug; environmental contaminant; prodrug; radiosensitizing agent; xenobiotic |
| metyrapone Metyrapone: An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.. metyrapone : An aromatic ketone that is 3,3-dimethylbutan-2-one in which the methyl groups at positions 1 and 4 are replaced by pyridin-3-yl groups. A steroid 11beta-monooxygenase (EC 1.14.15.4) inhibitor, it is used in the diagnosis of adrenal insufficiency. | 3.23 | 1 | 0 | aromatic ketone | antimetabolite; diagnostic agent; EC 1.14.15.4 (steroid 11beta-monooxygenase) inhibitor |
| mexiletine Mexiletine: Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.. mexiletine : An aromatic ether which is 2,6-dimethylphenyl ether of 2-aminopropan-1-ol. | 3.23 | 1 | 0 | aromatic ether; primary amino compound | anti-arrhythmia drug |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 3.23 | 1 | 0 | imidazobenzodiazepine; monofluorobenzenes; organochlorine compound | anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative |
| midodrine Midodrine: An ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.. midodrine : An aromatic ether that is 1,4-dimethoxybenzene which is substituted at position 2 by a 2-(glycylamino)-1-hydroxyethyl group. A direct-acting sympathomimetic with selective alpha-adrenergic agonist activity, it is used (generally as its hydrochloride salt) as a peripheral vasoconstrictor in the treatment of certain hypotensive states. The main active moiety is its major metabolite, deglymidodrine. | 3.23 | 1 | 0 | amino acid amide; aromatic ether; secondary alcohol | alpha-adrenergic agonist; prodrug; sympathomimetic agent; vasoconstrictor agent |
| milrinone [no description available] | 3.23 | 1 | 0 | bipyridines; nitrile; pyridone | cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| minoxidil Minoxidil: A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371). minoxidil : A pyrimidine N-oxide that is pyrimidine-2,4-diamine 3-oxide substituted by a piperidin-1-yl group at position 6. | 3.23 | 1 | 0 | dialkylarylamine; tertiary amino compound | |
| mirtazapine Mirtazapine: A piperazinoazepine tetracyclic compound that enhances the release of NOREPINEPHRINE and SEROTONIN through blockage of presynaptic ALPHA-2 ADRENERGIC RECEPTORS. It also blocks both 5-HT2 and 5-HT3 serotonin receptors and is a potent HISTAMINE H1 RECEPTOR antagonist. It is used for the treatment of depression, and may also be useful for the treatment of anxiety disorders. | 3.23 | 1 | 0 | benzazepine; tetracyclic antidepressant | alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist |
| mitotane Mitotane: A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression. | 3.23 | 1 | 0 | diarylmethane | |
| mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8. | 3.23 | 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. | 3.23 | 1 | 0 | monocarboxylic acid amide; sulfoxide | |
| moxisylyte Moxisylyte: An alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) | 3.23 | 1 | 0 | monoterpenoid | |
| nabumetone Nabumetone: A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS.. nabumetone : A methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthylacetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. | 3.23 | 1 | 0 | methoxynaphthalene; methyl ketone | cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| nadolol [no description available] | 3.23 | 1 | 0 | tetralins | |
| nalidixic acid [no description available] | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; DNA synthesis inhibitor |
| naratriptan naratriptan: structure given in first source | 3.23 | 1 | 0 | heteroarylpiperidine; sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| nefazodone nefazodone: may be useful as an opiate adjunct | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazoles | alpha-adrenergic antagonist; analgesic; antidepressant; serotonergic antagonist; serotonin uptake inhibitor |
| nevirapine Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS.. nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. | 3.23 | 1 | 0 | cyclopropanes; dipyridodiazepine | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nialamide Nialamide: An MAO inhibitor that is used as an antidepressive agent. | 3.23 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| nicardipine Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.. nicardipine : A racemate comprising equimolar amounts of (R)- and (S)-nicardipine. It is a calcium channel blocker which is used to treat hypertension.. 2-[benzyl(methyl)amino]ethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine substituted by a methyl, {2-[benzyl(methyl)amino]ethoxy}carbonyl, 3-nitrophenyl, methoxycarbonyl and methyl groups at positions 2, 3, 4, 5 and 6, respectively. | 3.23 | 1 | 0 | benzenes; C-nitro compound; diester; dihydropyridine; methyl ester; tertiary amino compound | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 3.23 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| nilutamide [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; imidazolidinone | androgen antagonist; antineoplastic agent |
| nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups. | 3.23 | 1 | 0 | aromatic ether; C-nitro compound; sulfonamide | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| nimodipine Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.. nimodipine : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a (2-methoxyethoxy)carbonyl group at position 3, a m-nitrophenyl group at position 4, and an isopropoxycarbonyl group at position 5. An L-type calcium channel blocker, it acts particularly on cerebral circulation, and is used both orally and intravenously for the prevention and treatment of subarachnoid hemorrhage from ruptured intracranial aneurysm. | 3.23 | 1 | 0 | 2-methoxyethyl ester; C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; isopropyl ester | antihypertensive agent; calcium channel blocker; cardiovascular drug; vasodilator agent |
| nisoldipine Nisoldipine: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.. nisoldipine : A racemate consisting of equimolar amounts of (R)- and (S)-nisoldipine. A calcium channel blocker, it is used in the treatment of hypertension and angina pectoris.. methyl 2-methylpropyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate : A dihydropyridine that is 1,4-dihydropyridine which is substituted by methyl groups at positions 2 and 6, a methoxycarbonyl group at position 3, an o-nitrophenyl group at position 4, and an isobutoxycarbonyl group at position 5. The racemate, a calcium channel blocker, is used in the treatment of hypertension and angina pectoris. | 3.23 | 1 | 0 | C-nitro compound; dicarboxylic acids and O-substituted derivatives; diester; dihydropyridine; methyl ester | |
| nitroglycerin Nitroglycerin: A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.. nitroglycerol : A nitrate ester that is glycerol in which nitro group(s) replace the hydrogen(s) attached to one or more of the hydroxy groups.. nitroglycerin : A nitroglycerol that is glycerol in which the hydrogen atoms of all three hydroxy groups are replaced by nitro groups. It acts as a prodrug, releasing nitric oxide to open blood vessels and so alleviate heart pain. | 3.23 | 1 | 0 | nitroglycerol | explosive; muscle relaxant; nitric oxide donor; prodrug; tocolytic agent; vasodilator agent; xenobiotic |
| nizatidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; C-nitro compound; carboxamidine; organic sulfide; tertiary amino compound | anti-ulcer drug; cholinergic drug; H2-receptor antagonist |
| nomifensine Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266). nomifensine : An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively. | 3.23 | 1 | 0 | isoquinolines | dopamine uptake inhibitor |
| norfloxacin Norfloxacin: A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE.. norfloxacin : A quinolinemonocarboxylic acid with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase. | 3.23 | 1 | 0 | fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug; DNA synthesis inhibitor; environmental contaminant; xenobiotic |
| nortriptyline Nortriptyline: A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.. nortriptyline : An organic tricyclic compound that is 10,11-dihydro-5H-dibenzo[a,d][7]annulene substituted by a 3-(methylamino)propylidene group at position 5. It is an active metabolite of amitriptyline. | 3.23 | 1 | 0 | organic tricyclic compound; secondary amine | adrenergic uptake inhibitor; analgesic; antidepressant; antineoplastic agent; apoptosis inducer; drug metabolite |
| ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. | 3.23 | 1 | 0 | 3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline | |
| omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; pyridines; sulfoxide | |
| ondansetron Ondansetron: A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. | 3.23 | 1 | 0 | carbazoles | |
| orphenadrine Orphenadrine: A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.. orphenadrine : A tertiary amino compound which is the phenyl-o-tolylmethyl ether of 2-(dimethylamino)ethanol. | 3.23 | 1 | 0 | ether; tertiary amino compound | antidyskinesia agent; antiparkinson drug; H1-receptor antagonist; muscarinic antagonist; muscle relaxant; NMDA receptor antagonist; parasympatholytic |
| oxaprozin Oxaprozin: An oxazole-propionic acid derivative, cyclooxygenase inhibitor, and non-steroidal anti-inflammatory drug that is used in the treatment of pain and inflammation associated with of OSTEOARTHRITIS; RHEUMATOID ARTHRITIS; and ARTHRITIS, JUVENILE.. oxaprozin : A monocarboxylic acid that is a propionic acid derivative having a 4,5-diphenyl-1,3-oxazol-2-yl substituent at position 3. It is non-steroidal anti-inflammatory drug commonly used to relieve the pain and inflammatory responses associated with osteoarthritis and rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-oxazoles; monocarboxylic acid | analgesic; non-steroidal anti-inflammatory drug |
| oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. | 3.23 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| oxybutynin oxybutynin: RN given refers to parent cpd. oxybutynin : A racemate comprising equimolar amounts of (R)-oxybutynin and esoxybutynin. An antispasmodic used for the treatment of overactive bladder. | 3.23 | 1 | 0 | acetylenic compound; carboxylic ester; racemate; tertiary alcohol; tertiary amino compound | antispasmodic drug; calcium channel blocker; local anaesthetic; muscarinic antagonist; muscle relaxant; parasympatholytic |
| aminosalicylic acid Aminosalicylic Acid: An antitubercular agent often administered in association with ISONIAZID. The sodium salt of the drug is better tolerated than the free acid.. 4-aminosalicylic acid : An aminobenzoic acid that is salicylic acid substituted by an amino group at position 4. | 3.23 | 1 | 0 | aminobenzoic acid; phenols | antitubercular agent |
| pamidronate [no description available] | 3.23 | 1 | 0 | phosphonoacetic acid | |
| pantoprazole Pantoprazole: 2-pyridinylmethylsulfinylbenzimidazole proton pump inhibitor that is used in the treatment of GASTROESOPHAGEAL REFLUX and PEPTIC ULCER.. pantoprazole : A member of the class of benzimidazoles that is 1H-benzimidazole substituted by a difluoromethoxy group at position 5 and a [(3,4-dimethoxypyridin-2-yl)methyl]sulfinyl group at position 2. | 3.23 | 1 | 0 | aromatic ether; benzimidazoles; organofluorine compound; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor; environmental contaminant; xenobiotic |
| papaverine Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels.. papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. | 3.23 | 1 | 0 | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pemoline Pemoline: A central nervous system stimulant used in fatigue and depressive states and to treat hyperkinetic disorders in children.. pemoline : A member of the class of 1,3-oxazoles that is 1,3-oxazol-4(5H)-one which is substituted by an amino group at position 2 and by a phenyl group at position 5. A central nervous system stimulant, it was used to treat hyperactivity disorders in children, but withdrawn from use following reports of serious hepatotoxicity. | 3.23 | 1 | 0 | 1,3-oxazoles | central nervous system stimulant |
| pentamidine Pentamidine: Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.. pentamidine : A diether consisting of pentane-1,5-diol in which both hydroxyl hydrogens have been replaced by 4-amidinophenyl groups. A trypanocidal drug that is used for treatment of cutaneous leishmaniasis and Chagas disease. | 3.23 | 1 | 0 | aromatic ether; carboxamidine; diether | anti-inflammatory agent; antifungal agent; calmodulin antagonist; chemokine receptor 5 antagonist; EC 2.3.1.48 (histone acetyltransferase) inhibitor; NMDA receptor antagonist; S100 calcium-binding protein B inhibitor; trypanocidal drug; xenobiotic |
| pentobarbital Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. | 3.23 | 1 | 0 | barbiturates | GABAA receptor agonist |
| pentoxifylline [no description available] | 3.23 | 1 | 0 | oxopurine | |
| perhexiline Perhexiline: 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. | 3.23 | 1 | 0 | piperidines | cardiovascular drug |
| perphenazine Perphenazine: An antipsychotic phenothiazine derivative with actions and uses similar to those of CHLORPROMAZINE.. perphenazine : A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10. | 3.23 | 1 | 0 | N-(2-hydroxyethyl)piperazine; N-alkylpiperazine; organochlorine compound; phenothiazines | antiemetic; dopaminergic antagonist; phenothiazine antipsychotic drug |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 3.23 | 1 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| phenoxybenzamine Phenoxybenzamine: An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. | 3.23 | 1 | 0 | aromatic amine | |
| phentermine Phentermine: A central nervous system stimulant and sympathomimetic with actions and uses similar to those of DEXTROAMPHETAMINE. It has been used most frequently in the treatment of obesity. | 3.23 | 1 | 0 | primary amine | adrenergic agent; appetite depressant; central nervous system drug; central nervous system stimulant; dopaminergic agent; sympathomimetic agent |
| 4-phenylbutyric acid 4-phenylbutyric acid: RN refers to the parent cpd. 4-phenylbutyric acid : A monocarboxylic acid the structure of which is that of butyric acid substituted with a phenyl group at C-4. It is a histone deacetylase inhibitor that displays anticancer activity. It inhibits cell proliferation, invasion and migration and induces apoptosis in glioma cells. It also inhibits protein isoprenylation, depletes plasma glutamine, increases production of foetal haemoglobin through transcriptional activation of the gamma-globin gene and affects hPPARgamma activation. | 3.23 | 1 | 0 | monocarboxylic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor; prodrug |
| pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol. | 3.23 | 1 | 0 | indoles; secondary amine | antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent |
| pioglitazone Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. | 3.23 | 1 | 0 | aromatic ether; pyridines; thiazolidinediones | antidepressant; cardioprotective agent; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; geroprotector; hypoglycemic agent; insulin-sensitizing drug; PPARgamma agonist; xenobiotic |
| polythiazide [no description available] | 3.23 | 1 | 0 | benzothiadiazine | |
| duodote duodote: consists of atropine and pralidoxime chloride; for treating those exposed to organophosphorus-containing nerve agents | 3.23 | 1 | 0 | pyridinium ion | antidote to organophosphate poisoning; antidote to sarin poisoning; cholinergic drug; cholinesterase reactivator |
| praziquantel azinox: Russian drug | 3.23 | 1 | 0 | isoquinolines | |
| prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively. | 3.23 | 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. | 3.23 | 1 | 0 | aminoquinoline; aromatic ether; N-substituted diamine | antimalarial |
| primidone Primidone: A barbiturate derivative that acts as a GABA modulator and anti-epileptic agent. It is partly metabolized to PHENOBARBITAL in the body and owes some of its actions to this metabolite.. primidone : A pyrimidone that is dihydropyrimidine-4,6(1H,5H)-dione substituted by an ethyl and a phenyl group at position 5. It is used as an anticonvulsant for treatment of various types of seizures. | 3.23 | 1 | 0 | pyrimidone | anticonvulsant; environmental contaminant; xenobiotic |
| probenecid Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups. | 3.23 | 1 | 0 | benzoic acids; sulfonamide | uricosuric drug |
| procainamide Procainamide: A class Ia antiarrhythmic drug that is structurally-related to PROCAINE.. procainamide : A benzamide that is 4-aminobenzamide substituted on the amide N by a 2-(diethylamino)ethyl group. It is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | benzamides | anti-arrhythmia drug; platelet aggregation inhibitor; sodium channel blocker |
| procarbazine Procarbazine: An antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone (the MOPP protocol) in the treatment of Hodgkin's disease.. procarbazine : A benzamide obtained by formal condensation of the carboxy group of 4-[(2-methylhydrazino)methyl]benzoic acid with the amino group of isopropylamine. An antineoplastic chemotherapy drug used for treatment of Hodgkin's lymphoma. Metabolism yields azo-procarbazine and hydrogen peroxide, which results in the breaking of DNA strands. | 3.23 | 1 | 0 | benzamides; hydrazines | antineoplastic agent |
| prochlorperazine Prochlorperazine: A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612). prochlorperazine : A member of the class of phenothiazines that is 10H-phenothiazine having a chloro substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position. | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organochlorine compound; phenothiazines | alpha-adrenergic antagonist; antiemetic; cholinergic antagonist; dopamine receptor D2 antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic |
| procyclidine Procyclidine: A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism.. procyclidine : A tertiary alcohol that consists of propan-1-ol substituted by a cyclohexyl and a phenyl group at position 1 and a pyrrolidin-1-yl group at position 3. | 3.23 | 1 | 0 | pyrrolidines; tertiary alcohol | antidyskinesia agent; antiparkinson drug; muscarinic antagonist |
| promethazine Promethazine: A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.. promethazine : A tertiary amine that is a substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropan-2-amine moiety. | 3.23 | 1 | 0 | phenothiazines; tertiary amine | anti-allergic agent; anticoronaviral agent; antiemetic; antipruritic drug; H1-receptor antagonist; local anaesthetic; sedative |
| propafenone Propafenone: An antiarrhythmia agent that is particularly effective in ventricular arrhythmias. It also has weak beta-blocking activity.. propafenone : An aromatic ketone that is 3-(propylamino)propane-1,2-diol in which the hydrogen of the primary hydroxy group is replaced by a 2-(3-phenylpropanoyl)phenyl group. It is a class 1C antiarrhythmic drug with local anesthetic effects, and is used as the hydrochloride salt in the management of supraventricular and ventricular arrhythmias. | 3.23 | 1 | 0 | aromatic ketone; secondary alcohol; secondary amino compound | anti-arrhythmia drug |
| propantheline Propantheline: A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. | 3.23 | 1 | 0 | xanthenes | |
| propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. | 3.23 | 1 | 0 | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| propranolol Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.. propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. | 3.23 | 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 |
| protriptyline Protriptyline: Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. | 3.23 | 1 | 0 | carbotricyclic compound | antidepressant |
| pyridostigmine [no description available] | 3.23 | 1 | 0 | pyridinium ion | |
| pyrimethamine Maloprim: contains above 2 cpds | 3.23 | 1 | 0 | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| sch 16134 quazepam: structure given in first source | 3.23 | 1 | 0 | benzodiazepine | |
| quetiapine [no description available] | 3.23 | 1 | 0 | dibenzothiazepine; N-alkylpiperazine; N-arylpiperazine | adrenergic antagonist; dopaminergic antagonist; histamine antagonist; second generation antipsychotic; serotonergic antagonist |
| rabeprazole Rabeprazole: A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. | 3.23 | 1 | 0 | benzimidazoles; pyridines; sulfoxide | anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor |
| raloxifene raloxifene : A member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. | 3.23 | 1 | 0 | 1-benzothiophenes; aromatic ketone; N-oxyethylpiperidine; phenols | bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| riluzole Riluzole: A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS. | 3.23 | 1 | 0 | benzothiazoles | |
| rimantadine Rimantadine: An RNA synthesis inhibitor that is used as an antiviral agent in the prophylaxis and treatment of influenza. | 3.23 | 1 | 0 | alkylamine | |
| risperidone Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA.. risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. | 3.23 | 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 |
| rizatriptan rizatriptan: structure given in first source; RN given refers to benzoate | 3.23 | 1 | 0 | tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| ropinirole [no description available] | 3.23 | 1 | 0 | indolones; tertiary amine | antidyskinesia agent; antiparkinson drug; central nervous system drug; dopamine agonist |
| salicylsalicylic acid salicylsalicylic acid: structure. salsalate : A dimeric benzoate ester obtained by intermolecular condensation between the carboxy of one molecule of salicylic acid with the phenol group of a second. It is a prodrug for salycylic acid that is used for treatment of rheumatoid arthritis and osteoarthritis and also shows activity against type II diabetes. | 3.23 | 1 | 0 | benzoate ester; benzoic acids; phenols; salicylates | antineoplastic agent; antirheumatic drug; EC 3.5.2.6 (beta-lactamase) inhibitor; hypoglycemic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug |
| secobarbital Secobarbital: A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.. secobarbital : A member of the class of barbiturates that is barbituric acid in which the hydrogens at position 5 are substituted by prop-2-en-1-yl and pentan-2-yl groups. | 3.23 | 1 | 0 | barbiturates | anaesthesia adjuvant; GABA modulator; sedative |
| sibutramine sibutramine: serotonin and norepinephrine transporter inhibitor; Meridia is tradename for sibutramine hydrochloride | 3.23 | 1 | 0 | organochlorine compound; tertiary amino compound | anti-obesity agent; serotonin uptake inhibitor |
| sulfadiazine Sulfadiazine: One of the short-acting SULFONAMIDES used in combination with PYRIMETHAMINE to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections.. sulfadiazine : A sulfonamide consisting of pyrimidine with a 4-aminobenzenesulfonamido group at the 2-position.. diazine : The parent structure of the diazines. | 3.23 | 1 | 0 | pyrimidines; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; antimicrobial agent; antiprotozoal drug; coccidiostat; drug allergen; EC 1.1.1.153 [sepiapterin reductase (L-erythro-7,8-dihydrobiopterin forming)] inhibitor; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| risedronic acid Risedronic Acid: A pyridine and diphosphonic acid derivative that acts as a CALCIUM CHANNEL BLOCKER and inhibits BONE RESORPTION. | 3.23 | 1 | 0 | pyridines | |
| sotalol Sotalol: An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.. sotalol : A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is substituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. | 3.23 | 1 | 0 | ethanolamines; secondary alcohol; secondary amino compound; sulfonamide | anti-arrhythmia drug; beta-adrenergic antagonist; environmental contaminant; xenobiotic |
| imatinib [no description available] | 3.23 | 1 | 0 | aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines | antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor |
| vorinostat Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL). | 3.23 | 1 | 0 | dicarboxylic acid diamide; hydroxamic acid | antineoplastic agent; apoptosis inducer; EC 3.5.1.98 (histone deacetylase) inhibitor |
| succinylcholine Succinylcholine: A quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for.. succinylcholine : A quaternary ammonium ion that is the bis-choline ester of succinic acid. | 3.23 | 1 | 0 | quaternary ammonium ion; succinate ester | drug allergen; muscle relaxant; neuromuscular agent |
| sulfamethizole Sulfamethizole: A sulfathiazole antibacterial agent.. sulfamethizole : A sulfonamide consisting of a 1,3,4-thiadiazole nucleus with a methyl substituent at C-5 and a 4-aminobenzenesulfonamido group at C-2. | 3.23 | 1 | 0 | sulfonamide antibiotic; sulfonamide; thiadiazoles | antiinfective agent; antimicrobial agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor |
| sulfasalazine Sulfasalazine: A drug that is used in the management of inflammatory bowel diseases. Its activity is generally considered to lie in its metabolic breakdown product, 5-aminosalicylic acid (see MESALAMINE) released in the colon. (From Martindale, The Extra Pharmacopoeia, 30th ed, p907). sulfasalazine : An azobenzene consisting of diphenyldiazene having a carboxy substituent at the 4-position, a hydroxy substituent at the 3-position and a 2-pyridylaminosulphonyl substituent at the 4'-position. | 3.23 | 1 | 0 | ||
| sulfathiazole Sulfathiazole: A sulfathiazole compound that is used as a short-acting anti-infective agent. It is no longer commonly used systemically due to its toxicity, but may still be applied topically in combination with other drugs for the treatment of vaginal and skin infections, and is still used in veterinary medicine.. sulfathiazole : A 1,3-thiazole compound having a 4-aminobenzenesulfonamido group at the 2-position. | 3.23 | 1 | 0 | 1,3-thiazoles; substituted aniline; sulfonamide antibiotic; sulfonamide | antiinfective agent; drug allergen; EC 2.5.1.15 (dihydropteroate synthase) inhibitor; environmental contaminant; xenobiotic |
| 2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| sumatriptan Sumatriptan: A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.. sumatriptan : A sulfonamide that consists of N,N-dimethyltryptamine bearing an additional (N-methylsulfamoyl)methyl substituent at position 5. Selective agonist for a vascular 5-HT1 receptor subtype (probably a member of the 5-HT1D family). Used (in the form of its succinate salt) for the acute treatment of migraine with or without aura in adults. | 3.23 | 1 | 0 | sulfonamide; tryptamines | serotonergic agonist; vasoconstrictor agent |
| temazepam Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | 3.23 | 1 | 0 | benzodiazepine | |
| temozolomide [no description available] | 3.23 | 1 | 0 | imidazotetrazine; monocarboxylic acid amide; triazene derivative | alkylating agent; antineoplastic agent; prodrug |
| terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia | 3.23 | 1 | 0 | furans; piperazines; primary amino compound; quinazolines | alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent |
| terbutaline Terbutaline: A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic.. terbutaline : A member of the class of phenylethanolamines that is catechol substituted at position 5 by a 2-(tert-butylamino)-1-hydroxyethyl group. | 3.23 | 1 | 0 | phenylethanolamines; resorcinols | anti-asthmatic drug; beta-adrenergic agonist; bronchodilator agent; EC 3.1.1.7 (acetylcholinesterase) inhibitor; hypoglycemic agent; sympathomimetic agent; tocolytic agent |
| thalidomide Thalidomide: A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppressive and anti-angiogenic activity. It inhibits release of TUMOR NECROSIS FACTOR-ALPHA from monocytes, and modulates other cytokine action.. thalidomide : A racemate comprising equimolar amounts of R- and S-thalidomide.. 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione : A dicarboximide that is isoindole-1,3(2H)-dione in which the hydrogen attached to the nitrogen is substituted by a 2,6-dioxopiperidin-3-yl group. | 3.23 | 1 | 0 | phthalimides; piperidones | |
| thiabendazole Tresaderm: dermatologic soln containing dexamethasone, thiabendazole & neomycin sulfate | 3.23 | 1 | 0 | 1,3-thiazoles; benzimidazole fungicide; benzimidazoles | antifungal agrochemical; antinematodal drug |
| thioridazine Thioridazine: A phenothiazine antipsychotic used in the management of PHYCOSES, including SCHIZOPHRENIA.. thioridazine : A phenothiazine derivative having a methylsulfanyl subsitituent at the 2-position and a (1-methylpiperidin-2-yl)ethyl] group at the N-10 position. | 3.23 | 1 | 0 | phenothiazines; piperidines | alpha-adrenergic antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| thiotepa Thiotepa: A very toxic alkylating antineoplastic agent also used as an insect sterilant. It causes skin, gastrointestinal, CNS, and bone marrow damage. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), thiotepa may reasonably be anticipated to be a carcinogen (Merck Index, 11th ed). | 3.23 | 1 | 0 | aziridines | |
| ticlopidine Ticlopidine: An effective inhibitor of platelet aggregation commonly used in the placement of STENTS in CORONARY ARTERIES.. ticlopidine : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group. | 3.23 | 1 | 0 | monochlorobenzenes; thienopyridine | anticoagulant; fibrin modulating drug; hematologic agent; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| tinidazole Tinidazole: A nitroimidazole alkylating agent that is used as an antitrichomonal agent against TRICHOMONAS VAGINALIS; ENTAMOEBA HISTOLYTICA; and GIARDIA LAMBLIA infections. It also acts as an antibacterial agent for the treatment of BACTERIAL VAGINOSIS and anaerobic bacterial infections.. tinidazole : 1H-imidazole substituted at C-1 by a (2-ethylsulfonyl)ethyl group, at C-2 by a methyl group and at C-5 by a nitro group. It is used as an antiprotozoal, antibacterial agent. | 3.23 | 1 | 0 | imidazoles | antiamoebic agent; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| tiopronin Tiopronin: Sulfhydryl acylated derivative of GLYCINE. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| tizanidine tizanidine: RN given refers to parent cpd; structure. tizanidine : 2,1,3-Benzothiadiazole substituted at C-4 by a Delta(1)-imidazolin-2-ylamino group and at C-4 by a chloro group. It is an agonist at alpha2-adrenergic receptor sites. | 3.23 | 1 | 0 | benzothiadiazole; imidazoles | alpha-adrenergic agonist; muscle relaxant |
| tolazamide Tolazamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.. tolazamide : An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | N-sulfonylurea | hypoglycemic agent; potassium channel blocker |
| tolbutamide Tolbutamide: A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290). tolbutamide : An N-sulfonylurea that consists of 1-butylurea having a tosyl group attached at the 3-position. | 3.23 | 1 | 0 | N-sulfonylurea | human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker |
| tolmetin Tolmetin: A non-steroidal anti-inflammatory agent (ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL) similar in mode of action to INDOMETHACIN.. tolmetin : A monocarboxylic acid that is (1-methylpyrrol-2-yl)acetic acid substituted at position 5 on the pyrrole ring by a 4-methylbenzoyl group. Used in the form of its sodium salt dihydrate as a nonselective nonsteroidal anti-inflammatory drug. | 3.23 | 1 | 0 | aromatic ketone; monocarboxylic acid; pyrroles | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| ultram 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)cyclohexanol : A tertiary alcohol that is cyclohexanol substituted at positions 1 and 2 by 3-methoxyphenyl and dimethylaminomethyl groups respectively. | 3.23 | 1 | 0 | aromatic ether; tertiary alcohol; tertiary amino compound | |
| tranexamic acid Tranexamic Acid: Antifibrinolytic hemostatic used in severe hemorrhage. | 3.23 | 1 | 0 | amino acid | |
| trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine | adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor |
| triamterene Triamterene: A pteridinetriamine compound that inhibits SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS.. triamterene : Pteridine substituted at positions 2, 4 and 7 with amino groups and at position 6 with a phenyl group. A sodium channel blocker, it is used as a diuretic in the treatment of hypertension and oedema. | 3.23 | 1 | 0 | pteridines | diuretic; sodium channel blocker |
| triazolam Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. | 3.23 | 1 | 0 | triazolobenzodiazepine | sedative |
| trifluoperazine [no description available] | 3.23 | 1 | 0 | N-alkylpiperazine; N-methylpiperazine; organofluorine compound; phenothiazines | antiemetic; calmodulin antagonist; dopaminergic antagonist; EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor; EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor; phenothiazine antipsychotic drug |
| trihexyphenidyl Trihexyphenidyl: One of the centrally acting MUSCARINIC ANTAGONISTS used for treatment of PARKINSONIAN DISORDERS and drug-induced extrapyramidal movement disorders and as an antispasmodic. | 3.23 | 1 | 0 | amine | |
| trimethadione Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent. | 3.23 | 1 | 0 | oxazolidinone | anticonvulsant; geroprotector |
| trimethobenzamide trimethobenzamide: major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd. trimethobenzamide : The amide obtained by formal condensation of 3,4,5-trihydroxybenzoic acid with 4-[2-(N,N-dimethylamino)ethoxy]benzylamine. It is used to prevent nausea and vomitting in humans. | 3.23 | 1 | 0 | benzamides; tertiary amino compound | antiemetic |
| trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge. | 3.23 | 1 | 0 | aminopyrimidine; methoxybenzenes | antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic |
| trimetrexate Trimetrexate: A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. | 3.23 | 1 | 0 | ||
| trimipramine Trimipramine: Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties.. trimipramine : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)-2-methylpropyl group at the nitrogen atom. It is used as an antidepressant. | 3.23 | 1 | 0 | dibenzoazepine; tertiary amino compound | antidepressant; environmental contaminant; xenobiotic |
| troglitazone Troglitazone: A chroman and thiazolidinedione derivative that acts as a PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS (PPAR) agonist. It was formerly used in the treatment of TYPE 2 DIABETES MELLITUS, but has been withdrawn due to hepatotoxicity. | 3.23 | 1 | 0 | chromanes; thiazolidinone | anticoagulant; anticonvulsant; antineoplastic agent; antioxidant; EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; hypoglycemic agent; platelet aggregation inhibitor; vasodilator agent |
| tyramine [no description available] | 3.23 | 1 | 0 | monoamine molecular messenger; primary amino compound; tyramines | EC 3.1.1.8 (cholinesterase) inhibitor; Escherichia coli metabolite; human metabolite; mouse metabolite; neurotransmitter |
| delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group. | 3.23 | 1 | 0 | cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound | adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic |
| vigabatrin [no description available] | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitor |
| ici 204,219 zafirlukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | carbamate ester; indoles; N-sulfonylcarboxamide | anti-asthmatic agent; leukotriene antagonist |
| zaleplon zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam. zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position. | 3.23 | 1 | 0 | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position. | 3.23 | 1 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zonisamide Zonisamide: A benzisoxazole and sulfonamide derivative that acts as a CALCIUM CHANNEL blocker. It is used primarily as an adjunctive antiepileptic agent for the treatment of PARTIAL SEIZURES, with or without secondary generalization.. zonisamide : A 1,2-benzoxazole compound having a sulfamoylmethyl substituent at the 3-position. | 3.23 | 1 | 0 | 1,2-benzoxazoles; sulfonamide | anticonvulsant; antioxidant; central nervous system drug; protective agent; T-type calcium channel blocker |
| cortisone acetate Cortisone Acetate: The acetate ester of cortisone that is used mainly for replacement therapy in adrenocortical insufficiency and in the treatment of many allergic and inflammatory disorders. | 3.23 | 1 | 0 | corticosteroid hormone | |
| mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae. | 3.23 | 1 | 0 | mitomycin | alkylating agent; antineoplastic agent |
| prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone. | 3.23 | 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 |
| reserpine Reserpine: An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use.. reserpine : An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. | 3.23 | 1 | 0 | alkaloid ester; methyl ester; yohimban alkaloid | adrenergic uptake inhibitor; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; first generation antipsychotic; plant metabolite; xenobiotic |
| phentolamine Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension. | 3.23 | 1 | 0 | imidazoles; phenols; substituted aniline; tertiary amino compound | alpha-adrenergic antagonist; vasodilator agent |
| sorbitol D-glucitol : The D-enantiomer of glucitol (also known as D-sorbitol). | 3.23 | 1 | 0 | glucitol | cathartic; Escherichia coli metabolite; food humectant; human metabolite; laxative; metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite; sweetening agent |
| thyroxine Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions. | 3.23 | 1 | 0 | 2-halophenol; iodophenol; L-phenylalanine derivative; non-proteinogenic L-alpha-amino acid; thyroxine zwitterion; thyroxine | antithyroid drug; human metabolite; mouse metabolite; thyroid hormone |
| dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration. | 3.23 | 1 | 0 | 1-phenylpropan-2-amine | adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent |
| spironolactone Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827). spironolactone : A steroid lactone that is 17alpha-pregn-4-ene-21,17-carbolactone substituted by an oxo group at position 3 and an alpha-acetylsulfanyl group at position 7. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; oxaspiro compound; steroid lactone; thioester | aldosterone antagonist; antihypertensive agent; diuretic; environmental contaminant; xenobiotic |
| penicillamine Penicillamine: 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.. penicillamine : An alpha-amino acid having the structure of valine substituted at the beta position with a sulfanyl group. | 3.23 | 1 | 0 | non-proteinogenic alpha-amino acid; penicillamine | antirheumatic drug; chelator; copper chelator; drug allergen |
| cysteine [no description available] | 3.23 | 1 | 0 | cysteine zwitterion; cysteine; L-alpha-amino acid; proteinogenic amino acid; serine family amino acid | EC 4.3.1.3 (histidine ammonia-lyase) inhibitor; flour treatment agent; human metabolite |
| prednisone Prednisone: A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.. prednisone : A synthetic glucocorticoid drug that is particularly effective as an immunosuppressant, and affects virtually all of the immune system. Prednisone is a prodrug that is converted by the liver into prednisolone (a beta-hydroxy group instead of the oxo group at position 11), which is the active drug and also a steroid. | 3.23 | 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. | 3.23 | 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. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid | anabolic agent; androgen |
| penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug; drug allergen; epitope |
| pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine. | 3.23 | 1 | 0 | pilocarpine | antiglaucoma drug |
| triiodothyronine Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. | 3.23 | 1 | 0 | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| chloramphenicol Amphenicol: Chloramphenicol and its derivatives. | 3.23 | 1 | 0 | C-nitro compound; carboxamide; diol; organochlorine compound | antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor |
| glutamine Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4. | 3.23 | 1 | 0 | amino acid zwitterion; glutamine family amino acid; glutamine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid | EC 1.14.13.39 (nitric oxide synthase) inhibitor; Escherichia coli metabolite; human metabolite; metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| vincristine [no description available] | 3.23 | 1 | 0 | acetate ester; formamides; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; drug; microtubule-destabilising agent; plant metabolite; tubulin modulator |
| physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. | 3.23 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. | 3.23 | 1 | 0 | aporphine alkaloid | alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug |
| methyltestosterone Methyltestosterone: A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).. methyltestosterone : A 17beta-hydroxy steroid that is testosterone bearing a methyl group at the 17alpha position. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; enone | anabolic agent; androgen; antineoplastic agent |
| tetrabenazine 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. | 3.23 | 1 | 0 | benzoquinolizine; cyclic ketone; tertiary amino compound | |
| kanamycin a Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.. kanamycin : Kanamycin is a naturally occurring antibiotic complex from Streptomyces kanamyceticus that consists of several components: kanamycin A, the major component (also usually designated as kanamycin), and kanamycins B, C, D and X the minor components. | 3.23 | 1 | 0 | kanamycins | bacterial metabolite |
| edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive. | 3.23 | 1 | 0 | ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid | anticoagulant; antidote; chelator; copper chelator; geroprotector |
| cysteamine Cysteamine: A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.. cysteamine : An amine that consists of an ethane skeleton substituted with a thiol group at C-1 and an amino group at C-2. | 3.23 | 1 | 0 | amine; thiol | geroprotector; human metabolite; mouse metabolite; radiation protective agent |
| acetylcholine chloride acetylcholine chloride : The chloride salt of acetylcholine, and a parasympatomimetic drug. | 3.23 | 1 | 0 | quaternary ammonium salt | |
| mepazine mepazine: major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd. pacatal : A phenothiazine derivative in which 10H-phenothiazine has an N-methylpiperidin-4-ylmethyl substituent at the N-10 position. | 3.23 | 1 | 0 | phenothiazines | |
| cloxacillin Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6. | 3.23 | 1 | 0 | penicillin allergen; penicillin; semisynthetic derivative | antibacterial agent; antibacterial drug |
| calcium acetate calcium acetate: a principal compound used as phosphate binders in patients with chronic renal failure; used like sevelamer. calcium acetate : The calcium salt of acetic acid. It is used, commonly as a hydrate, to treat hyperphosphataemia (excess phosphate in the blood) in patients with kidney disease: the calcium ion combines with dietary phosphate to form (insoluble) calcium phosphate, which is excreted in the faeces. | 3.23 | 1 | 0 | calcium salt | chelator |
| methionine Methionine: A sulfur-containing essential L-amino acid that is important in many body functions.. methionine : A sulfur-containing amino acid that is butyric acid bearing an amino substituent at position 2 and a methylthio substituent at position 4. | 3.23 | 1 | 0 | aspartate family amino acid; L-alpha-amino acid; methionine zwitterion; methionine; proteinogenic amino acid | antidote to paracetamol poisoning; human metabolite; micronutrient; mouse metabolite; nutraceutical |
| colchicine (S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions. | 3.23 | 1 | 0 | alkaloid; colchicine | anti-inflammatory agent; gout suppressant; mutagen |
| mebanazine mebanazine: RN given refers to parent cpd without isomeric designation; structure | 3.23 | 1 | 0 | benzenes | |
| oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta. | 3.23 | 1 | 0 | penicillin | antibacterial agent; antibacterial drug |
| cycloserine Cycloserine: Antibiotic substance produced by Streptomyces garyphalus.. D-cycloserine : A 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus and is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. An analogue of D-alanine, it interferes with bacterial cell wall synthesis in the cytoplasm by competitive inhibition of L-alanine racemase (which forms D-alanine from L-alanine) and D-alanine--D-alanine ligase (which incorporates D-alanine into the pentapeptide required for peptidoglycan formation and bacterial cell wall synthesis). | 3.23 | 1 | 0 | 4-amino-1,2-oxazolidin-3-one; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic; zwitterion | antiinfective agent; antimetabolite; antitubercular agent; metabolite; NMDA receptor agonist |
| benziodarone benziodarone: minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) | 3.23 | 1 | 0 | aromatic ketone | |
| ampicillin Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group. | 3.23 | 1 | 0 | beta-lactam antibiotic; penicillin allergen; penicillin | antibacterial drug |
| mannitol [no description available] | 3.23 | 1 | 0 | mannitol | allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent |
| cytarabine [no description available] | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; pyrimidine nucleoside | antimetabolite; antineoplastic agent; antiviral agent; immunosuppressive agent |
| arginine Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group. | 3.23 | 1 | 0 | arginine; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | biomarker; Escherichia coli metabolite; micronutrient; mouse metabolite; nutraceutical |
| perflutren Definity: a fluorocarbon-filled ultrasonic contrast agent; Definity is tradename. octafluoropropane : A fluorocarbon that is propane in which all of the hydrogens have been replaced by fluorines. | 3.23 | 1 | 0 | fluoroalkane; fluorocarbon | |
| fluoxymesterone Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid | anabolic agent; antineoplastic agent |
| methsuximide methsuximide: anticonvulsant effective in petit mal & psychomotor epilepsy; has a number of unpleasant & toxic side effects; minor descriptor (75-86); on-line & INDEX MEDICUS search SUCCINIMIDES (75-86); RN given refers to parent cpd without isomeric designation | 3.23 | 1 | 0 | organic molecular entity | |
| tromethamine Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424) | 3.23 | 1 | 0 | primary amino compound; triol | buffer |
| methylprednisolone Methylprednisolone: A PREDNISOLONE derivative with similar anti-inflammatory action.. 6alpha-methylprednisolone : The 6alpha-stereoisomer of 6-methylprednisolone. | 3.23 | 1 | 0 | 6-methylprednisolone; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | adrenergic agent; anti-inflammatory drug; antiemetic; environmental contaminant; neuroprotective agent; xenobiotic |
| brompheniramine Brompheniramine: Histamine H1 antagonist used in treatment of allergies, rhinitis, and urticaria.. brompheniramine : Pheniramine in which the hydrogen at position 4 of the phenyl substituent is substituted by bromine. A histamine H1 receptor antagonist, brompheniramine is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | organobromine compound; pyridines | anti-allergic agent; H1-receptor antagonist |
| penicillin v Penicillin V: A broad-spectrum penicillin antibiotic used orally in the treatment of mild to moderate infections by susceptible gram-positive organisms.. phenoxymethylpenicillin : A penicillin compound having a 6beta-(phenoxyacetyl)amino side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | |
| isosorbide dinitrate Isosorbide Dinitrate: A vasodilator used in the treatment of ANGINA PECTORIS. Its actions are similar to NITROGLYCERIN but with a slower onset of action. | 3.23 | 1 | 0 | glucitol derivative; nitrate ester | nitric oxide donor; vasodilator agent |
| pseudoephedrine Pseudoephedrine: A phenethylamine that is an isomer of EPHEDRINE which has less central nervous system effects and usage is mainly for respiratory tract decongestion.. pseudoephedrine : A member of the class of the class of phenylethanolamines that is (1S)-2-(methylamino)-1-phenylethan-1-ol in which the pro-S hydrogen at position 2 is replaced by a methyl group. | 3.23 | 1 | 0 | phenylethanolamines; secondary alcohol; secondary amino compound | anti-asthmatic drug; bronchodilator agent; central nervous system drug; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| diethylpropion Diethylpropion: A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290). diethylpropion : An aromatic ketone that is propiophenone in which one of the hydrogens alpha- to the carbonyl is substituted by a diethylamino group. A central stimulant and indirect-acting sympathomimetic, it is an appetite depressant and is used as the hydrochloride as an anoretic in the short term management of obesity. | 3.23 | 1 | 0 | aromatic ketone; tertiary amine | appetite depressant |
| benzonatate benzonatate: structure in Merck Index, 9th ed, #1107. benzonatate : The ester obtained by formal condensation of 4-butylaminobenzoic acid with nonaethylene glycol monomethyl ether. Structurally related to procaine and benzocaine, it has an anaesthetic effect on the stretch sensors in the lungs, and is used as a non-narcotic cough suppressant. | 3.23 | 1 | 0 | benzoate ester; secondary amino compound; substituted aniline | anaesthetic; antitussive |
| methylergonovine Methylergonovine: A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed) | 3.23 | 1 | 0 | ergoline alkaloid | |
| cinchophen cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | 3.23 | 1 | 0 | quinolines | |
| nafcillin Nafcillin: A semi-synthetic antibiotic related to penicillin.. nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| methohexital Methohexital: An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia.. methohexital : A barbiturate, the structure of which is that of barbituric acid substituted at N-1 by a methyl group and at C-5 by allyl and 1-methylpent-2-ynyl groups. | 3.23 | 1 | 0 | acetylenic compound; barbiturates | drug allergen; intravenous anaesthetic |
| ephedrine Ephedrine: A phenethylamine found in EPHEDRA SINICA. PSEUDOEPHEDRINE is an isomer. It is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. It has been used for asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists.. (-)-ephedrine : A phenethylamine alkaloid that is 2-phenylethanamine substituted by a methyl group at the amino nitrogen and a methyl and a hydroxy group at position 2 and 1 respectively. | 3.23 | 1 | 0 | phenethylamine alkaloid; phenylethanolamines | bacterial metabolite; environmental contaminant; nasal decongestant; plant metabolite; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 3.23 | 1 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| azacitidine Azacitidine: A pyrimidine analogue that inhibits DNA methyltransferase, impairing DNA methylation. It is also an antimetabolite of cytidine, incorporated primarily into RNA. Azacytidine has been used as an antineoplastic agent.. 5-azacytidine : An N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via an N-glycosidic linkage. An antineoplastic agent, it is used in the treatment of myeloid leukaemia. | 3.23 | 1 | 0 | N-glycosyl-1,3,5-triazine; nucleoside analogue | antineoplastic agent |
| galantamine Galantamine: A benzazepine derived from norbelladine. It is found in GALANTHUS and other AMARYLLIDACEAE. It is a cholinesterase inhibitor that has been used to reverse the muscular effects of GALLAMINE TRIETHIODIDE and TUBOCURARINE and has been studied as a treatment for ALZHEIMER DISEASE and other central nervous system disorders.. galanthamine : A benzazepine alkaloid isolated from certain species of daffodils. | 3.23 | 1 | 0 | benzazepine alkaloid fundamental parent; benzazepine alkaloid; organic heterotetracyclic compound; tertiary amino compound | antidote to curare poisoning; cholinergic drug; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; plant metabolite |
| nandrolone decanoate Nandrolone Decanoate: Decanoic acid ester of nandrolone that is used as an anabolic agent to prevent or treat WASTING SYNDROME associated with severe chronic illness or HIV infection (HIV WASTING SYNDROME). It may also be used in the treatment of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | steroid ester | |
| dextropropoxyphene Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.. propoxyphene : A racemate of the (1R,2R)- and (1S,2R)- diastereoisomers.. dextropropoxyphene : The (1S,2R)-(+)-diastereoisomer of propoxyphene. | 3.23 | 1 | 0 | 1-benzyl-3-(dimethylamino)-2-methyl-1-phenylpropyl propanoate | mu-opioid receptor agonist; opioid analgesic |
| chenodeoxycholic acid Chenodeoxycholic Acid: A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.. chenodeoxycholic acid : A dihydroxy-5beta-cholanic acid that is (5beta)-cholan-24-oic acid substituted by hydroxy groups at positions 3 and 7 respectively.. chenodeoxycholate : Conjugate base of chenodeoxycholic acid; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| 4-hydroxybutyric acid 4-hydroxybutyric acid: was an entry term to Sodium Oxybate (74-98). 4-hydroxybutyric acid : A 4-hydroxy monocarboxylic acid that is butyric acid in which one of the hydrogens at position 4 is replaced by a hydroxy group. | 3.23 | 1 | 0 | 4-hydroxy monocarboxylic acid; hydroxybutyric acid | general anaesthetic; GHB receptor agonist; neurotoxin; sedative |
| dihydroergotamine Dihydroergotamine: A 9,10alpha-dihydro derivative of ERGOTAMINE. It is used as a vasoconstrictor, specifically for the therapy of MIGRAINE DISORDERS.. dihydroergotamine : Ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine, it is used (as the methanesulfonic or tartaric acid salts) for the treatment of migraine and orthostatic hypotension. | 3.23 | 1 | 0 | ergot alkaloid; semisynthetic derivative | dopamine agonist; non-narcotic analgesic; serotonergic agonist; sympatholytic agent; vasoconstrictor agent |
| medroxyprogesterone [no description available] | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | contraceptive drug; progestin; synthetic oral contraceptive |
| dimenhydrinate gravinol: has antioxidant and ant-inflammatory activities; structure in first source | 3.23 | 1 | 0 | diarylmethane | |
| methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent. | 3.23 | 1 | 0 | amphetamines; secondary amine | central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic |
| levocarnitine (R)-carnitine : The (R)-enantiomer of carnitine. | 3.23 | 1 | 0 | carnitine | antilipemic drug; nootropic agent; nutraceutical; Saccharomyces cerevisiae metabolite; water-soluble vitamin (role) |
| sulfanilylurea sulfanilylurea: antimicrobial agent; structure | 3.23 | 1 | 0 | benzenes; sulfonamide | |
| lactulose [no description available] | 3.23 | 1 | 0 | glycosylfructose | gastrointestinal drug; laxative |
| pamabrom [no description available] | 3.23 | 1 | 0 | ||
| acetylcysteine N-acetyl-L-cysteine : An N-acetyl-L-amino acid that is the N-acetylated derivative of the natural amino acid L-cysteine. | 3.23 | 1 | 0 | acetylcysteine; L-cysteine derivative; N-acetyl-L-amino acid | antidote to paracetamol poisoning; antiinfective agent; antioxidant; antiviral drug; ferroptosis inhibitor; geroprotector; human metabolite; mucolytic; radical scavenger; vulnerary |
| erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively. | 3.23 | 1 | 0 | cyclic ketone; erythromycin | |
| levonorgestrel Levonorgestrel: A synthetic progestational hormone with actions similar to those of PROGESTERONE and about twice as potent as its racemic or (+-)-isomer (NORGESTREL). It is used for contraception, control of menstrual disorders, and treatment of endometriosis. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin; synthetic oral contraceptive |
| diphenoxylate Diphenoxylate: A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity.. diphenoxylate : A piperidinecarboxylate ester that is the ethyl ester of difenoxin. | 3.23 | 1 | 0 | ethyl ester; nitrile; piperidinecarboxylate ester; tertiary amine | antidiarrhoeal drug |
| ethambutol Ethambutol: An antitubercular agent that inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863). ethambutol : An ethylenediamine derivative that is ethane-1,2-diamine in which one hydrogen attached to each of the nitrogens is sutstituted by a 1-hydroxybutan-2-yl group (S,S-configuration). It is a bacteriostatic antimycobacterial drug, effective against Mycobacterium tuberculosis and some other mycobacteria. It is used (as the dihydrochloride salt) in combination with other antituberculous drugs in the treatment of pulmonary and extrapulmonary tuberculosis; resistant strains of M. tuberculosis are readily produced if ethambutol is used alone. | 3.23 | 1 | 0 | ethanolamines; ethylenediamine derivative | antitubercular agent; environmental contaminant; xenobiotic |
| vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. | 3.23 | 1 | 0 | glycopeptide | antibacterial drug; antimicrobial agent; bacterial metabolite |
| d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils. | 3.23 | 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 |
| ibufenac ibufenac: used in the treatment of rheumatism; also possesses antipyretic properties; minor descriptor (75-84); on-line & Index Medicus search PHENYLACETATES (75-84); RN given refers to parent cpd. ibufenac : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens is replaced by a 4-isobutylphenyl group. Although it was shown to be effective in treatment of rheumatoid arthritis, the clinical use of ibufenac was discontinued due to hepatotoxic side-effects. | 3.23 | 1 | 0 | monocarboxylic acid | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| metaxalone [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| spectinomycin Spectinomycin: An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of GONORRHEA.. spectinomycin dihydrochloride : A hydrochloride obtained by combining spectinomycin with two molar equivalents of hydrochloric acid. An antibiotic that is active against gram-negative bacteria and used (as its pentahydrate) to treat gonorrhea.. spectinomycin : A pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis. | 3.23 | 1 | 0 | cyclic acetal; cyclic hemiketal; cyclic ketone; pyranobenzodioxin; secondary alcohol; secondary amino compound | antibacterial drug; antimicrobial agent; bacterial metabolite |
| dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. | 3.23 | 1 | 0 | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| amiloride Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid. | 3.23 | 1 | 0 | aromatic amine; guanidines; organochlorine compound; pyrazines | diuretic; sodium channel blocker |
| pimozide Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403). pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. | 3.23 | 1 | 0 | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| dexbrompheniramine dexbrompheniramine : The (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. A histamine H1 receptor antagonist, it is used (commonly as its maleate salt) for the symptomatic relief of allergic conditions, including rhinitis and conjunctivitis. | 3.23 | 1 | 0 | brompheniramine | anti-allergic agent; H1-receptor antagonist |
| stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase | 3.23 | 1 | 0 | dihydrofuran; nucleoside analogue; organic molecular entity | antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group. | 3.23 | 1 | 0 | dichlorobenzene; penicillin | antibacterial drug |
| megestrol Megestrol: A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.. megestrol : A 3-oxo Delta(4)-steroid that is pregna-4,6-diene-3,20-dione substituted by a methyl group at position 6 and a hydroxy group at position 17. | 3.23 | 1 | 0 | 17alpha-hydroxy steroid; 20-oxo steroid; 3-oxo-Delta(4) steroid; tertiary alpha-hydroxy ketone | antineoplastic agent; appetite enhancer; contraceptive drug; progestin; synthetic oral contraceptive |
| streptomycin [no description available] | 3.23 | 1 | 0 | antibiotic antifungal drug; antibiotic fungicide; streptomycins | antibacterial drug; antifungal agrochemical; antimicrobial agent; antimicrobial drug; bacterial metabolite; protein synthesis inhibitor |
| cladribine [no description available] | 3.23 | 1 | 0 | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent |
| carbenicillin Carbenicillin: Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function.. carbenicillin : A penicillin antibiotic having a 6beta-2-carboxy-2-phenylacetamido side-chain. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| clomacran clomacran: RN given refers to parent cpd; structure | 3.23 | 1 | 0 | acridines | |
| methenamine hippurate methenamine hippurate: both parts of molecule contribute to its antibacterial action | 3.23 | 1 | 0 | N-acylglycine | |
| olsalazine olsalazine: cpd with 2 salicylate molecules linked together by an azo bond. olsalazine : An azobenzene that consists of two molecules of 4-aminosalicylic acid joined by an azo linkage. A prodrug for mesalazine, an anti-inflammatory drug, it is used (as the disodium salt) in the treatment of inflammatory bowel disease. | 3.23 | 1 | 0 | azobenzenes; dicarboxylic acid | non-steroidal anti-inflammatory drug; prodrug |
| camptothecin NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source | 2.17 | 1 | 0 | delta-lactone; pyranoindolizinoquinoline; quinoline alkaloid; tertiary alcohol | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor; genotoxin; plant metabolite |
| sodium thiosulfate sodium thiosulfate: do not confuse synonym sodium hyposulfite with sodium hyposulfite, synonym for di-Na salt of dithionous acid. sodium thiosulfate : An inorganic sodium salt composed of sodium and thiosulfate ions in a 2:1 ratio. | 3.23 | 1 | 0 | inorganic sodium salt | antidote to cyanide poisoning; antifungal drug; nephroprotective agent |
| selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. | 3.23 | 1 | 0 | selegiline; terminal acetylenic compound | geroprotector |
| clemastine Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions. | 3.23 | 1 | 0 | monochlorobenzenes; N-alkylpyrrolidine | anti-allergic agent; antipruritic drug; H1-receptor antagonist; muscarinic antagonist |
| cephalexin Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative | antibacterial drug |
| danazol Danazol: A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; terminal acetylenic compound | anti-estrogen; estrogen antagonist; geroprotector |
| fenclozic acid fenclozic acid: an analgesic & antipyretic with anti-inflammatory properties; minor descriptor (75-86); on-line & INDEX MEDICUS search THIAZOLES (75-86); RN given refers to parent cpd | 3.23 | 1 | 0 | ||
| laxagetten 4,4'-diacetoxydiphenylpyridylemethane [no description available] | 3.23 | 1 | 0 | ||
| daunorubicin Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola. | 3.23 | 1 | 0 | aminoglycoside antibiotic; anthracycline; p-quinones; tetracenequinones | antineoplastic agent; bacterial metabolite |
| fludarabine phosphate fludarabine phosphate: structure given in first source. fludarabine phosphate : A purine arabinonucleoside monophosphate having 2-fluoroadenine as the nucleobase. A prodrug, it is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. Once incorporated into DNA, 2-fluoro-ara-ATP functions as a DNA chain terminator. It is used for the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to, or whose disease has progressed during, treatment with at least one standard alkylating-agent containing regimenas. | 3.23 | 1 | 0 | nucleoside analogue; organofluorine compound; purine arabinonucleoside monophosphate | antimetabolite; antineoplastic agent; antiviral agent; DNA synthesis inhibitor; immunosuppressive agent; prodrug |
| alclofenac alclofenac: was heading 1975-94 (was see under PHENYLACETATES 1975-90); use PHENYLACETATES to search ALCLOFENAC 1975-94; an anti-inflammatory agent used in the treatment of rheumatoid arthritis; acts also as an analgesic and an antipyretic. alclofenac : An aromatic ether in which the ether oxygen links an allyl group to the 4-position of (3-chlorophenyl)acetic acid.A non-steroidal anti-inflammatory drug, it was withdrawn from the UK market in 1979 due to concerns with its association with vasculitis and rash. | 3.23 | 1 | 0 | aromatic ether; monocarboxylic acid; monochlorobenzenes | drug allergen; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| bromocriptine Bromocriptine: A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. | 3.23 | 1 | 0 | indole alkaloid | antidyskinesia agent; antiparkinson drug; dopamine agonist; hormone antagonist |
| oxyphenisatin [no description available] | 3.23 | 1 | 0 | indoles | |
| fludrocortisone Fludrocortisone: A synthetic mineralocorticoid with anti-inflammatory activity. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; fluorinated steroid; mineralocorticoid | adrenergic agent; anti-inflammatory drug |
| ursodeoxycholic acid Ursodeoxycholic Acid: An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.. ursodeoxycholic acid : A bile acid found in the bile of bears (Ursidae) as a conjugate with taurine. Used therapeutically, it prevents the synthesis and absorption of cholesterol and can lead to the dissolution of gallstones.. ursodeoxycholate : A bile acid anion that is the conjugate base of ursodeoxycholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3. | 3.23 | 1 | 0 | bile acid; C24-steroid; dihydroxy-5beta-cholanic acid | human metabolite; mouse metabolite |
| dexchlorpheniramine dexchlorpheniramine: RN given refers to parent cpd(S)-isomer | 3.23 | 1 | 0 | chlorphenamine | |
| clometacin clometacin: structure | 3.23 | 1 | 0 | N-acylindole | |
| cefazolin Cefazolin: A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.. cefazolin : A first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; tetrazoles; thiadiazoles | antibacterial drug |
| amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| timolol (S)-timolol (anhydrous) : The (S)-(-) (more active) enantiomer of timolol. A beta-adrenergic antagonist, both the hemihydrate and the maleate salt are used in the mangement of glaucoma, hypertension, angina pectoris and myocardial infarction, and for the prevention of migraine. | 3.23 | 1 | 0 | timolol | anti-arrhythmia drug; antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist |
| oxcarbazepine Oxcarbazepine: A carbamazepine derivative that acts as a voltage-gated sodium channel blocker. It is used for the treatment of PARTIAL SEIZURES with or without secondary generalization. It is also an inducer of CYTOCHROME P-450 CYP3A4.. oxcarbazepine : A dibenzoazepine derivative, having a carbamoyl group at the ring nitrogen, substituted with an oxo group at C-4 of the azepeine ring which is also hydrogenated at C-4 and C-5. It is a anticholinergic anticonvulsant and mood stabilizing drug, used primarily in the treatment of epilepsy. | 3.23 | 1 | 0 | cyclic ketone; dibenzoazepine | anticonvulsant; drug allergen |
| carbidopa carbidopa (anhydrous) : 3-(3,4-Dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used (commonly as its hydrate) in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa. | 3.23 | 1 | 0 | catechols; hydrazines; monocarboxylic acid | antiparkinson drug; dopaminergic agent; EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor |
| moricizine Moricizine: An antiarrhythmia agent used primarily for ventricular rhythm disturbances.. moricizine : A phenothiazine substituted on the nitrogen by a 3-(morpholin-4-yl)propanoyl group, and at position 2 by an (ethoxycarbonyl)amino group. | 3.23 | 1 | 0 | carbamate ester; morpholines; phenothiazines | anti-arrhythmia drug |
| amineptin amineptin: used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure. amineptine : A carbocyclic fatty acid that is 5-aminoheptanoic acid in which one of the hydrogens attached to the nitrogen is replaced by a 10,11-dihydro-5H-dibenzo[a,d][7]annulen-5-yl group. A tricyclic antidepressant, it was never approved in the US and was withdrawn from the French market in 1999 due to concerns over abuse, dependence and severe acne. | 3.23 | 1 | 0 | amino acid; carbocyclic fatty acid; carbotricyclic compound; secondary amino compound | antidepressant; dopamine uptake inhibitor |
| zidovudine Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase. | 3.23 | 1 | 0 | azide; pyrimidine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; HIV-1 reverse transcriptase inhibitor |
| pirprofen pirprofen: anti-inflammatory agent used in therapy of rheumatoid arthritis; prostaglandin synthetase inhibitor; more potent than indomethacin; structure | 3.23 | 1 | 0 | pyrroline | |
| paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL). | 3.23 | 1 | 0 | taxane diterpenoid; tetracyclic diterpenoid | antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent |
| etoposide [no description available] | 3.23 | 1 | 0 | beta-D-glucoside; furonaphthodioxole; organic heterotetracyclic compound | antineoplastic agent; DNA synthesis inhibitor |
| dobutamine Dobutamine: A catecholamine derivative with specificity for BETA-1 ADRENERGIC RECEPTORS. It is commonly used as a cardiotonic agent after CARDIAC SURGERY and during DOBUTAMINE STRESS ECHOCARDIOGRAPHY.. dobutamine : A catecholamine that is 4-(3-aminobutyl)phenol in which one of the hydrogens attached to the nitrogen is substituted by a 2-(3,4-dihydroxyphenyl)ethyl group. A beta1-adrenergic receptor agonist that has cardiac stimulant action without evoking vasoconstriction or tachycardia, it is used as the hydrochloride to increase the contractility of the heart in the management of acute heart failure. | 3.23 | 1 | 0 | catecholamine; secondary amine | beta-adrenergic agonist; cardiotonic drug; sympathomimetic agent |
| penbutolol Penbutolol: A nonselective beta-blocker used as an antihypertensive and an antianginal agent. | 3.23 | 1 | 0 | ethanolamines | |
| ribavirin Rebetron: Rebetron is tradename | 3.23 | 1 | 0 | 1-ribosyltriazole; aromatic amide; monocarboxylic acid amide; primary carboxamide | anticoronaviral agent; antiinfective agent; antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| amikacin Amikacin: A broad-spectrum antibiotic derived from KANAMYCIN. It is reno- and oto-toxic like the other aminoglycoside antibiotics.. amikacin : An amino cyclitol glycoside that is kanamycin A acylated at the N-1 position by a 4-amino-2-hydroxybutyryl group. | 3.23 | 1 | 0 | alpha-D-glucoside; amino cyclitol glycoside; aminoglycoside; carboxamide | antibacterial drug; antimicrobial agent; nephrotoxin |
| cephradine Cephradine: A semi-synthetic cephalosporin antibiotic.. cephradine : A first-generation cephalosporin antibiotic with a methyl substituent at position 3, and a (2R)-2-amino-2-cyclohexa-1,4-dien-1-ylacetamido substituent at position 7, of the cephem skeleton. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin | antibacterial drug |
| ticrynafen Ticrynafen: A novel diuretic with uricosuric action. It has been proposed as an antihypertensive agent.. tienilic acid : An aromatic ketone that is 2,3-dichlorophenoxyacetic acid in which the hydrogen at position 4 on the benzene ring is replaced by a thiophenecarbonyl group. A loop diuretic used to treat hypertension, it was withdrawn from the market in 1982 due to links with hepatitis. | 3.23 | 1 | 0 | aromatic ether; aromatic ketone; dichlorobenzene; monocarboxylic acid; thiophenes | antihypertensive agent; hepatotoxic agent; loop diuretic |
| methyldopa Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | alpha-adrenergic agonist; antihypertensive agent; hapten; peripheral nervous system drug; sympatholytic agent |
| diltiazem Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.. diltiazem : A 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate in which both stereocentres have S configuration. A calcium-channel blocker and vasodilator, it is used as the hydrochloride in the management of angina pectoris and hypertension. | 3.23 | 1 | 0 | 5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepin-3-yl acetate | antihypertensive agent; calcium channel blocker; vasodilator agent |
| vecuronium vecuronium : A 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidino- and 16beta-N-methylpiperidinium substituents. | 3.23 | 1 | 0 | acetate ester; androstane; quaternary ammonium ion | drug allergen; muscle relaxant; neuromuscular agent; nicotinic antagonist |
| benoxaprofen benoxaprofen: RN given refers to parent cpd; structure. benoxaprofen : A monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals. | 3.23 | 1 | 0 | 1,3-benzoxazoles; monocarboxylic acid; monochlorobenzenes | antipsoriatic; antipyretic; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; hepatotoxic agent; nephrotoxin; non-narcotic analgesic; non-steroidal anti-inflammatory drug; protein kinase C agonist |
| exifone [no description available] | 3.23 | 1 | 0 | benzophenones | |
| mefloquine (-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown. | 3.23 | 1 | 0 | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol | antimalarial |
| nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug | 3.23 | 1 | 0 | benzamides; carboxylic ester | |
| sufentanil Sufentanil: An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent.. sufentanil : An anilide resulting from the formal condensation of the aryl amino group of 4-(methoxymethyl)-N-phenyl-1-[2-(2-thienyl)ethyl]piperidin-4-amine with propanoic acid. | 3.23 | 1 | 0 | anilide; ether; piperidines; thiophenes | anaesthesia adjuvant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic |
| acarbose [no description available] | 3.23 | 1 | 0 | tetrasaccharide derivative | EC 3.2.1.1 (alpha-amylase) inhibitor; EC 3.2.1.20 (alpha-glucosidase) inhibitor; geroprotector; hypoglycemic agent |
| torsemide Torsemide: A pyridine and sulfonamide derivative that acts as a sodium-potassium chloride symporter inhibitor (loop diuretic). It is used for the treatment of EDEMA associated with CONGESTIVE HEART FAILURE; CHRONIC RENAL INSUFFICIENCY; and LIVER DISEASES. It is also used for the management of HYPERTENSION.. torasemide : An N-sulfonylurea obtained by formal condensation of [(3-methylphenyl)amino]pyridine-3-sulfonic acid with the free amino group of N-isopropylurea. It is a potent loop diuretic used for the treatment of hypertension and edema in patients with congestive heart failure. | 3.23 | 1 | 0 | aminopyridine; N-sulfonylurea; secondary amino compound | antihypertensive agent; loop diuretic |
| epirubicin Epirubicin: An anthracycline which is the 4'-epi-isomer of doxorubicin. The compound exerts its antitumor effects by interference with the synthesis and function of DNA. | 3.23 | 1 | 0 | aminoglycoside; anthracycline antibiotic; anthracycline; deoxy hexoside; monosaccharide derivative; p-quinones; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone | antimicrobial agent; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| idarubicin Idarubicin: An orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA. | 3.23 | 1 | 0 | anthracycline antibiotic; deoxy hexoside; monosaccharide derivative | |
| piperacillin Piperacillin: Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics.. piperacillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-[(4-ethyl-2,3-dioxopiperazin-1-yl)carboxamido]-2-phenylacetamido group. | 3.23 | 1 | 0 | penicillin allergen; penicillin | antibacterial drug |
| paroxetine Paroxetine: A serotonin uptake inhibitor that is effective in the treatment of depression.. paroxetine : A benzodioxole that consists of piperidine bearing 1,3-benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively; the (3S,4R)-diastereomer. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibition of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2 or H1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (Ki = 42 nM). Antidepressant and anxiolytic in vivo. | 3.23 | 1 | 0 | aromatic ether; benzodioxoles; organofluorine compound; piperidines | antidepressant; anxiolytic drug; hepatotoxic agent; P450 inhibitor; serotonin uptake inhibitor |
| captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug. | 3.23 | 1 | 0 | alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| cefoperazone Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| atracurium Atracurium: A non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.. atracurium : A diester compound consisting of pentane-1,5-diol with both hydroxyls bearing 3-[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-3,4-dihydroisoquinolinium-2(1H)-yl]propanoyl groups. | 3.23 | 1 | 0 | diester; quaternary ammonium ion | muscle relaxant; nicotinic antagonist |
| pergolide Pergolide: A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES.. pergolide : A diamine that is ergoline in which the beta-hydrogen at position 8 is replaced by a (methylthio)methyl group and the hydrogen attached to the piperidine nitrogen (position 6) is replaced by a propyl group. A dopamine D2 receptor agonist which also has D1 and D2 agonist properties, it is used as the mesylate salt in the management of Parkinson's disease, although it was withdrawn from the U.S. and Canadian markets in 2007 due to an increased risk of cardiac valve dysfunction. | 3.23 | 1 | 0 | diamine; methyl sulfide; organic heterotetracyclic compound | antiparkinson drug; dopamine agonist |
| cefadroxil anhydrous Cefadroxil: Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative.. cefadroxil : A cephalosporin bearing methyl and (2R)-2-amino-2-(4-hydroxyphenyl)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| fialuridine [no description available] | 3.23 | 1 | 0 | ||
| cefaclor anhydrous Cefaclor: Semisynthetic, broad-spectrum antibiotic derivative of CEPHALEXIN.. cefaclor : A cephalosporin bearing chloro and (R)-2-amino-2-phenylacetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| alfentanil Alfentanil: A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients.. alfentanil : A member of the class of piperidines that is piperidine having a 2-(4-ethyl-5-oxo-4,5-dihydro-1H-tetrazol-1-yl)ethyl group at the 1-position as well as N-phenylpropanamido- and methoxymethyl groups at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; piperidines | central nervous system depressant; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; peripheral nervous system drug |
| miglustat miglustat: a glucosylceramide synthase inhibitor. miglustat : A hydroxypiperidine that is deoxynojirimycin in which the amino hydrogen is replaced by a butyl group. | 3.23 | 1 | 0 | piperidines; tertiary amino compound | anti-HIV agent; EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor |
| haloperidol decanoate [no description available] | 3.23 | 1 | 0 | organic molecular entity | |
| cefotetan Cefotetan: A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms.. cefotetan : A semi-synthetic second-generation cephamycin antibiotic with [(1-methyl-1H-tetrazol-5-yl)sulfanyl]methyl, methoxy and {[4-(2-amino-1-carboxy-2-oxoethylidene)-1,3-dithietan-2-yl]carbonyl}amino groups at the 3, 7alpha, and 7beta positions, respectively, of the cephem skeleton. It is resistant to a wide range of beta-lactamases and is active against a broad spectrum of aerobic and anaerobic Gram-positive and Gram-negative microorganisms. | 3.23 | 1 | 0 | ||
| lovastatin Lovastatin: A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.. lovastatin : A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom). | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; polyketide; statin (naturally occurring) | anticholesteremic drug; antineoplastic agent; Aspergillus metabolite; prodrug |
| tolrestat tolrestat: RN & structure given in first source | 3.23 | 1 | 0 | naphthalenes | EC 1.1.1.21 (aldehyde reductase) inhibitor |
| simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug. | 3.23 | 1 | 0 | delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic) | EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug |
| balsalazide balsalazide: a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine; structure in first source. balsalazide : A monohydroxybenzoic acid consisting of 5-aminosalicylic acid (mesalazine) linked to 4-aminobenzoyl-beta-alanine via an azo bond. | 3.23 | 1 | 0 | ||
| pravastatin Pravastatin: An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).. pravastatin : A carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin. | 3.23 | 1 | 0 | 3-hydroxy carboxylic acid; carbobicyclic compound; carboxylic ester; hydroxy monocarboxylic acid; secondary alcohol; statin (semi-synthetic) | anticholesteremic drug; environmental contaminant; metabolite; xenobiotic |
| cabergoline Cabergoline: An ergoline derivative and dopamine D2-agonist that inhibits PROLACTIN secretion. It is used in the management of HYPERPROLACTINEMIA, and to suppress lactation following childbirth for medical reasons. Cabergoline is also used in the management of PARKINSON DISEASE.. cabergoline : An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substituted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia. | 3.23 | 1 | 0 | N-acylurea | antineoplastic agent; antiparkinson drug; dopamine agonist |
| atomoxetine atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | 3.23 | 1 | 0 | aromatic ether; secondary amino compound; toluenes | adrenergic uptake inhibitor; antidepressant; environmental contaminant; xenobiotic |
| quinapril Quinapril: A tetrahydroisoquinoline derivative and ANGIOTENSIN CONVERTING ENZYME inhibitor that is used in the treatment of HYPERTENSION and HEART FAILURE.. quinapril : A member of the class of isoquinolines that is (3S)-2-L-alanyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid in which the alpha-amino group of the alanyl residue has been substituted by a 1-ethoxycarbonyl-4-phenylbutan-2-yl group (the all-S isomer). A prodrug for quinaprilat (by hydrolysis of the ethyl ester to the corresponding carboxylic acid), it is used as an angiotensin-converting enzyme inhibitor (ACE inhibitor) used (generally as the hydrochloride salt) for the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dicarboxylic acid monoester; ethyl ester; isoquinolines; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| alpidem [no description available] | 3.23 | 1 | 0 | imidazoles | |
| mifepristone Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; acetylenic compound; tertiary amino compound | abortifacient; contraceptive drug; hormone antagonist; synthetic oral contraceptive |
| fosphenytoin fosphenytoin: structure given in first & second source | 3.23 | 1 | 0 | imidazolidine-2,4-dione | |
| ranolazine Ranolazine: An acetanilide and piperazine derivative that functions as a SODIUM CHANNEL BLOCKER and prevents the release of enzymes during MYOCARDIAL ISCHEMIA. It is used in the treatment of ANGINA PECTORIS.. N-(2,6-dimethylphenyl)-2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetamide : An aromatic amide obtained by formal condensation of the carboxy group of 2-{4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl}acetic acid with the amino group of 2,6-dimethylaniline.. ranolazine : A racemate comprising equal amounts of (R)- and (S)-ranolazine. Used for treatment of chronic angina. | 3.23 | 1 | 0 | aromatic amide; monocarboxylic acid amide; monomethoxybenzene; N-alkylpiperazine; secondary alcohol | |
| finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. | 3.23 | 1 | 0 | 3-oxo steroid; aza-steroid; delta-lactam | androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| esmolol methyl 3-{4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}propanoate : A methyl ester that is methyl 3-(4-hydroxyphenyl)propanoate in which the hydrogen attached to the phenolic hydroxy group is substituted by a 2-hydroxy-3-(isopropylamino)propyl group.. esmolol : A racemate comprising equimolar amounts of (R)- and (S)-esmolol. A cardioselective and short-acting beta1 receptor blocker with rapid onset but lacking intrinsic sympathomimetic and membrane-stabilising properties, it is used as the hydrochloride salt in the management of supraventricular arrhythmias, and for the control of hypertension and tachycardia during surgery. While the S enantiomer possesses all of the heart rate control, both enantiomers contribute to lowering blood pressure. | 3.23 | 1 | 0 | aromatic ether; ethanolamines; methyl ester; secondary alcohol; secondary amino compound | |
| adefovir adefovir: inhibitor of African swine fever virus. adefovir(1-) : A organophosphonate oxoanion obtained by removal of a proton from the phosphonate group of adefovir, a nucleoside reverse transcriptase inhibitor. It is the major microspecies at pH 7.3 (according to Marvin v 6.2.0.).. adefovir : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens has been replaced by a 2-(6-amino-9H-purin-9-yl)ethoxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(t-butoxycarbonyloxymethyl) ester (dipivoxil ester) prodrug is used to treat chronic hepatitis B viral infection. | 3.23 | 1 | 0 | 6-aminopurines; ether; phosphonic acids | antiviral drug; DNA synthesis inhibitor; drug metabolite; HIV-1 reverse transcriptase inhibitor; nephrotoxic agent |
| aromasil [no description available] | 3.23 | 1 | 0 | 17-oxo steroid; 3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent; EC 1.14.14.14 (aromatase) inhibitor; environmental contaminant; xenobiotic |
| zileuton [no description available] | 3.23 | 1 | 0 | 1-benzothiophenes; ureas | anti-asthmatic drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; ferroptosis inhibitor; leukotriene antagonist; non-steroidal anti-inflammatory drug |
| clopidogrel Clopidogrel: A ticlopidine analog and platelet purinergic P2Y receptor antagonist that inhibits adenosine diphosphate-mediated PLATELET AGGREGATION. It is used to prevent THROMBOEMBOLISM in patients with ARTERIAL OCCLUSIVE DISEASES; MYOCARDIAL INFARCTION; STROKE; or ATRIAL FIBRILLATION.. clopidogrel : A thienopyridine that is 4,5,6,7-tetrahydrothieno[3,2-c]pyridine in which the hydrogen attached to the nitrogen is replaced by an o-chlorobenzyl group, the methylene hydrogen of which is replaced by a methoxycarbonyl group (the S enantiomer). A P2Y12 receptor antagonist, it is used to inhibit blood clots and prevent heart attacks. | 3.23 | 1 | 0 | methyl ester; monochlorobenzenes; thienopyridine | anticoagulant; P2Y12 receptor antagonist; platelet aggregation inhibitor |
| cidofovir anhydrous Cidofovir: An acyclic nucleoside phosphonate that acts as a competitive inhibitor of viral DNA polymerases. It is used in the treatment of RETINITIS caused by CYTOMEGALOVIRUS INFECTIONS and may also be useful for treating HERPESVIRUS INFECTIONS.. cidofovir anhydrous : Cytosine substituted at the 1 position by a 3-hydroxy-2-(phosphonomethoxy)propyl group (S configuration). A nucleoside analogue, it is an injectable antiviral used for the treatment of cytomegalovirus (CMV) retinitis in AIDS patients. | 3.23 | 1 | 0 | phosphonic acids; pyrimidone | anti-HIV agent; antineoplastic agent; antiviral drug; photosensitizing agent |
| tiagabine Tiagabine: A nipecotic acid derivative that acts as a GABA uptake inhibitor and anticonvulsant agent. It is used in the treatment of EPILEPSY, for refractory PARTIAL SEIZURES.. tiagabine : A piperidinemonocarboxylic acid that is (R)-nipecotic acid in which the hydrogen attached to the nitrogen has been replaced by a 1,1-bis(3-methyl-2-thienyl)but-1-en-4-yl group. A GABA reuptake inhibitor, it is used (generally as the hydrochloride salt) for the treatment of epilepsy. | 3.23 | 1 | 0 | beta-amino acid; piperidinemonocarboxylic acid; tertiary amino compound; thiophenes | anticonvulsant; GABA reuptake inhibitor |
| topotecan Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.. topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks. | 3.23 | 1 | 0 | pyranoindolizinoquinoline | antineoplastic agent; EC 5.99.1.2 (DNA topoisomerase) inhibitor |
| bromfenac bromfenac: bromfenac sodium is the active cpd; structure in first source. bromfenac : Amfenac in which the the hydrogen at the 4 position of the benzoyl group is substituted by bromine. It is used for the management of ocular pain and treatment of postoperative inflammation in patients who have undergone cataract extraction. It was withdrawn from the US market in 1998, following concerns over off-label abuse and hepatic failure. | 3.23 | 1 | 0 | aromatic amino acid; benzophenones; organobromine compound; substituted aniline | non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer. | 3.23 | 1 | 0 | organofluorine compound; pyrimidine 2'-deoxyribonucleoside | antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic |
| ibutilide ibutilide: RN & structure in first source; RN refers to the fumarate salt | 3.23 | 1 | 0 | benzenes; organic amino compound | |
| aripiprazole Aripiprazole: A piperazine and quinolone derivative that is used primarily as an antipsychotic agent. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A. It is used for the treatment of SCHIZOPHRENIA and BIPOLAR DISORDER, and as an adjunct therapy for the treatment of depression.. aripiprazole : An N-arylpiperazine that is piperazine substituted by a 4-[(2-oxo-1,2,3,4-tetrahydroquinolin-7-yl)oxy]butyl group at position 1 and by a 2,3-dichlorophenyl group at position 4. It is an antipsychotic drug used for the treatment of Schizophrenia, and other mood disorders. | 3.23 | 1 | 0 | aromatic ether; delta-lactam; dichlorobenzene; N-alkylpiperazine; N-arylpiperazine; quinolone | drug metabolite; H1-receptor antagonist; second generation antipsychotic; serotonergic agonist |
| remifentanil Remifentanil: A piperidine-propionate derivative and opioid analgesic structurally related to FENTANYL. It functions as a short-acting MU OPIOID RECEPTOR agonist, and is used as an analgesic during induction or maintenance of general anesthesia, following surgery, during childbirth, and in mechanically ventilated patients under intensive care.. remifentanil : A piperidinecarboxylate ester that is methyl piperidine-4-carboxylate in which the hydrogen attached to the nitrogen is substituted by a 3-methoxy-3-oxopropyl group and the hydrogen at position 4 is substituted the nitrogen of N-propanoylaniline. | 3.23 | 1 | 0 | alpha-amino acid ester; anilide; monocarboxylic acid amide; piperidinecarboxylate ester | intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic; sedative |
| atorvastatin [no description available] | 3.23 | 1 | 0 | aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic) | environmental contaminant; xenobiotic |
| lamivudine [no description available] | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; oxacycle; primary alcohol | allergen; anti-HBV agent; antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor; HIV-1 reverse transcriptase inhibitor; prodrug |
| duloxetine [no description available] | 3.23 | 1 | 0 | duloxetine | |
| irinotecan [no description available] | 3.23 | 1 | 0 | carbamate ester; delta-lactone; N-acylpiperidine; pyranoindolizinoquinoline; ring assembly; tertiary alcohol; tertiary amino compound | antineoplastic agent; apoptosis inducer; EC 5.99.1.2 (DNA topoisomerase) inhibitor; prodrug |
| valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. | 3.23 | 1 | 0 | biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| ibandronic acid Ibandronic Acid: Aminobisphosphonate that is a potent inhibitor of BONE RESORPTION. It is used in the treatment of HYPERCALCEMIA associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of POSTMENOPAUSAL OSTEOPOROSIS. | 3.23 | 1 | 0 | ||
| ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms. | 3.23 | 1 | 0 | 1,2-benzisothiazole; indolones; organochlorine compound; piperazines | antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist |
| zolmitriptan zolmitriptan: an antimigraine compound; a serotonin (5HT)-1D receptor agonist. zolmitriptan : A member of the class of tryptamines that is N,N-dimethyltryptamine in which the hydrogen at position 5 of the indole ring has been replaced by a [(4S)-2-oxo-1,3-oxazolidin-4-yl]methyl group. A serotonin 5-HT1 B and D receptor agonist, it is used for the treatment of migraine. | 3.23 | 1 | 0 | oxazolidinone; tryptamines | anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| emtricitabine Emtricitabine: A deoxycytidine analog and REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B viruses. It is used to treat HIV INFECTIONS.. emtricitabine : An organofluorine compound that is 5-fluorocytosine substituted at the 1 position by a 2-(hydroxymethyl)-1,3-oxathiolan-5-yl group (2R,5S configuration). It is used in combination therapy for the treatment of HIV-1 infection. | 3.23 | 1 | 0 | monothioacetal; nucleoside analogue; organofluorine compound; pyrimidone | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| tasosartan tasosartan: angiotensin II antagonist; structure given in first source | 3.23 | 1 | 0 | biphenyls | |
| tiludronic acid tiludronic acid: a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source | 3.23 | 1 | 0 | organochlorine compound | |
| tirofiban Tirofiban: Tyrosine analog and PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX antagonist that inhibits PLATELET AGGREGATION and is used in the treatment of ACUTE CORONARY SYNDROME.. tirofiban : A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group. | 3.23 | 1 | 0 | L-tyrosine derivative; piperidines; sulfonamide | anticoagulant; fibrin modulating drug; platelet glycoprotein-IIb/IIIa receptor antagonist |
| capecitabine Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers. | 3.23 | 1 | 0 | carbamate ester; cytidines; organofluorine compound | antimetabolite; antineoplastic agent; prodrug |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 3.23 | 1 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| trovafloxacin trovafloxacin: a trifluoronaphthyridone derivative of 7-(3-azabicyclo(3.1.0)hexyl)naphthyridone; has antineoplastic activity. trovafloxacin : A 1,8-naphthyridine derivative that is 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid bearing additional 2,4-difluorophenyl, fluoro and 6-amino-3-azabicyclo[3.1.0]hex-3-yl substituents at positions 1, 6 and 7 respectively. A broad-spectrum antibiotic that was withdrawn from the market due to risk of liver failure. | 3.23 | 1 | 0 | ||
| cefprozil [no description available] | 3.23 | 1 | 0 | cephalosporin; semisynthetic derivative | antibacterial drug |
| efavirenz efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection. | 3.23 | 1 | 0 | acetylenic compound; benzoxazine; cyclopropanes; organochlorine compound; organofluorine compound | antiviral drug; HIV-1 reverse transcriptase inhibitor |
| nelfinavir Nelfinavir: A potent HIV protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.. nelfinavir : An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties. | 3.23 | 1 | 0 | aryl sulfide; benzamides; organic heterobicyclic compound; phenols; secondary alcohol; tertiary amino compound | antineoplastic agent; HIV protease inhibitor |
| fenofibric acid fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate. | 3.23 | 1 | 0 | aromatic ketone; chlorobenzophenone; monocarboxylic acid | drug metabolite; marine xenobiotic metabolite |
| plerixafor plerixafor: a bicyclam derivate, highly potent & selective inhibitor of HIV-1 & HIV-2. plerixafor : An azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. | 3.23 | 1 | 0 | azacycloalkane; azamacrocycle; benzenes; crown amine; secondary amino compound; tertiary amino compound | anti-HIV agent; antineoplastic agent; C-X-C chemokine receptor type 4 antagonist; immunological adjuvant |
| amprenavir [no description available] | 3.23 | 1 | 0 | carbamate ester; sulfonamide; tetrahydrofuryl ester | antiviral drug; HIV protease inhibitor |
| oseltamivir Oseltamivir: An acetamido cyclohexene that is a structural homolog of SIALIC ACID and inhibits NEURAMINIDASE.. oseltamivir : A cyclohexenecarboxylate ester that is the ethyl ester of oseltamivir acid. An antiviral prodrug (it is hydrolysed to the active free carboxylic acid in the liver), it is used to slow the spread of influenza. | 3.23 | 1 | 0 | acetamides; amino acid ester; cyclohexenecarboxylate ester; primary amino compound | antiviral drug; EC 3.2.1.18 (exo-alpha-sialidase) inhibitor; environmental contaminant; prodrug; xenobiotic |
| histamine phosphate histamine phosphate : A phosphate salt that is the diphosphate salt of histamine. | 3.23 | 1 | 0 | phosphate salt | histamine agonist |
| tilbroquinol [no description available] | 3.23 | 1 | 0 | organohalogen compound; quinolines | |
| bendamustine [no description available] | 3.23 | 1 | 0 | benzimidazoles | |
| droxicam droxicam: structure given in first source. droxicam : An organic heterotricyclic compound that is 2H,5H-[1,3]oxazino[5,6-c][1,2]benzothiazine-2,4(3H)-dione 6,6-dioxide substituted at positions 3 and 5 by pyridin-2-yl and methyl groups respectively. A prodrug of piroxicam, it is used for the relief of pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis. | 3.23 | 1 | 0 | organic heterotricyclic compound; pyridines | cyclooxygenase 1 inhibitor; hepatotoxic agent; non-narcotic analgesic; non-steroidal anti-inflammatory drug; platelet aggregation inhibitor; prodrug |
| ebrotidine ebrotidine: an H2-receptor antagonist and gastric mucosa protector | 3.23 | 1 | 0 | sulfonamide | |
| repaglinide [no description available] | 3.23 | 1 | 0 | piperidines | |
| telmisartan Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. | 3.23 | 1 | 0 | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| sertraline Sertraline: A selective serotonin uptake inhibitor that is used in the treatment of depression.. sertraline : A member of the class of tetralins that is tetralin which is substituted at positions 1 and 4 by a methylamino and a 3,4-dichlorophenyl group, respectively (the S,S diastereoisomer). A selective serotonin-reuptake inhibitor (SSRI), it is administered orally as the hydrochloride salt as an antidepressant for the treatment of depression, obsessive-compulsive disorder, panic disorder and post-traumatic stress disorder. | 3.23 | 1 | 0 | dichlorobenzene; secondary amino compound; tetralins | antidepressant; serotonin uptake inhibitor |
| zoledronic acid Zoledronic Acid: An imidobisphosphonate inhibitor of BONE RESORPTION that is used for the treatment of malignancy-related HYPERCALCEMIA; OSTEITIS DEFORMANS; and OSTEOPOROSIS.. zoledronic acid : An imidazole compound having a 2,2-bis(phosphono)-2-hydroxyethane-1-yl substituent at the 1-position. | 3.23 | 1 | 0 | 1,1-bis(phosphonic acid); imidazoles | bone density conservation agent |
| acamprosate Acamprosate: Structural analog of taurine that is used for the prevention of relapse in individuals with ALCOHOLISM.. acamprosate : An organosulfonic acid that is propane-1-sulfonic acid substituted by an acetylamino group at position 3. | 3.23 | 1 | 0 | acetamides; organosulfonic acid | environmental contaminant; neurotransmitter agent; xenobiotic |
| isaxonine isaxonine: promotes nerve growth | 3.23 | 1 | 0 | aminopyrimidine | |
| nebivolol 2,2'-iminobis[1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)ethanol] : A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group. | 3.23 | 1 | 0 | chromanes; diol; organofluorine compound; secondary alcohol; secondary amino compound | |
| uk 68798 [no description available] | 3.23 | 1 | 0 | aromatic ether; sulfonamide; tertiary amino compound | anti-arrhythmia drug; potassium channel blocker |
| hp 873 iloperidone: an atypical, negative symptom antipsychotic agent. iloperidone : A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation antipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; aromatic ether; aromatic ketone; methyl ketone; monoamine; organofluorine compound; piperidines; tertiary amino compound | dopaminergic antagonist; second generation antipsychotic; serotonergic antagonist |
| dexrazoxane Dexrazoxane: The (+)-enantiomorph of razoxane. | 3.23 | 1 | 0 | razoxane | antineoplastic agent; cardiovascular drug; chelator; immunosuppressive agent |
| fenoxypropazine [no description available] | 3.23 | 1 | 0 | aromatic ether | |
| voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4. | 3.23 | 1 | 0 | conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug | P450 inhibitor |
| aceclofenac [no description available] | 3.23 | 1 | 0 | amino acid; carboxylic ester; dichlorobenzene; monocarboxylic acid; secondary amino compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| nitrefazole [no description available] | 3.23 | 1 | 0 | imidazoles | |
| doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS. | 3.23 | 1 | 0 | carbapenems | |
| atovaquone Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position. | 3.23 | 1 | 0 | hydroxy-1,2-naphthoquinone | |
| rivastigmine [no description available] | 3.23 | 1 | 0 | carbamate ester; tertiary amino compound | cholinergic drug; EC 3.1.1.8 (cholinesterase) inhibitor; neuroprotective agent |
| frovatriptan [no description available] | 3.23 | 1 | 0 | carbazoles | |
| eletriptan eletriptan: 5-HT(1B/1D) receptor agonist; structure in first source. eletriptan : An N-alkylpyrrolidine, that is N-methylpyrrolidine in which the pro-R hydrogen at position 2 is replaced by a {5-[2-(phenylsulfonyl)ethyl]-1H-indol-3-yl}methyl group. | 3.23 | 1 | 0 | indoles; N-alkylpyrrolidine; sulfone | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| rosiglitazone [no description available] | 3.23 | 1 | 0 | aminopyridine; thiazolidinediones | EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor; ferroptosis inhibitor; insulin-sensitizing drug |
| bexarotene [no description available] | 3.23 | 1 | 0 | benzoic acids; naphthalenes; retinoid | antineoplastic agent |
| clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic |
| moexipril [no description available] | 3.23 | 1 | 0 | peptide | |
| mci 9038 [no description available] | 3.23 | 1 | 0 | peptide | |
| fulvestrant Fulvestrant: An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.. fulvestrant : A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-hydroxy steroid; organofluorine compound; sulfoxide | antineoplastic agent; estrogen antagonist; estrogen receptor antagonist |
| bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. | 3.23 | 1 | 0 | primary alcohol; pyrimidines; sulfonamide | antihypertensive agent; endothelin receptor antagonist |
| perindopril Perindopril: An angiotensin-converting enzyme inhibitor. It is used in patients with hypertension and heart failure.. perindopril : An alpha-amino acid ester that is the ethyl ester of N-{(2S)-1-[(2S,3aS,7aS)-2-carboxyoctahydro-1H-indol-1-yl]-1-oxopropan-2-yl}-L-norvaline | 3.23 | 1 | 0 | alpha-amino acid ester; dicarboxylic acid monoester; ethyl ester; organic heterobicyclic compound | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| tadalafil [no description available] | 3.23 | 1 | 0 | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| paliperidone 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one : A member of the class of pyridopyrimidines that is 9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2.. paliperidone : A racemate comprising equimolar amounts of (R)- and (S)-paliperidone. Paliperidone is the primary active metabolite of the older antipsychotic risperidone and is used for treatment of schizophrenia. | 3.23 | 1 | 0 | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine; secondary alcohol | |
| nitisinone [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; C-nitro compound; cyclohexanones; mesotrione | EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor |
| clofarabine [no description available] | 3.23 | 1 | 0 | adenosines; organofluorine compound | antimetabolite; antineoplastic agent |
| pramipexole Pramipexole: A benzothiazole derivative and dopamine agonist with antioxidant properties that is used in the treatment of PARKINSON DISEASE and RESTLESS LEGS SYNDROME.. pramipexole : A member of the class of benzothiazoles that is 4,5,6,7-tetrahydro-1,3-benzothiazole in which the hydrogens at the 2 and 6-pro-S-positions are substituted by amino and propylamino groups, respectively. | 3.23 | 1 | 0 | benzothiazoles; diamine | antidyskinesia agent; antiparkinson drug; dopamine agonist; radical scavenger |
| valdecoxib [no description available] | 3.23 | 1 | 0 | isoxazoles; sulfonamide | antipyretic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug |
| almotriptan almotriptan : An indole compound having a 2-(dimethylamino)ethyl group at the 3-position and a (pyrrolidin-1-ylsulfonyl)methyl group at the 5-position. | 3.23 | 1 | 0 | indoles; sulfonamide; tertiary amine | non-steroidal anti-inflammatory drug; serotonergic agonist; vasoconstrictor agent |
| gefitinib [no description available] | 3.23 | 1 | 0 | aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound | antineoplastic agent; epidermal growth factor receptor antagonist |
| desloratadine desloratadine: major metabolite of loratadine. desloratadine : Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis and chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness. | 3.23 | 1 | 0 | benzocycloheptapyridine | anti-allergic agent; cholinergic antagonist; drug metabolite; H1-receptor antagonist |
| desvenlafaxine O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine. | 3.23 | 1 | 0 | cyclohexanols; phenols; tertiary amino compound | antidepressant; drug metabolite; marine xenobiotic metabolite |
| azatoxin azatoxin: structure given in first source; a topoisomerase II inhibitor | 2.17 | 1 | 0 | ||
| methotrexate [no description available] | 3.23 | 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 |
| tamsulosin [no description available] | 3.23 | 1 | 0 | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist; antineoplastic agent |
| rufinamide rufinamide: for treatment of Lennox-Gastaut syndrome; structure in first source | 3.23 | 1 | 0 | aromatic amide; heteroarene | |
| olmesartan medoxomil Olmesartan Medoxomil: An ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to manage HYPERTENSION. | 3.23 | 1 | 0 | biphenyls | |
| dexpanthenol dexpanthenol: The alcohol of pantothenic acid | 3.23 | 1 | 0 | amino alcohol; monocarboxylic acid amide | cholinergic drug; provitamin |
| fosamprenavir fosamprenavir: a prodrug of the protease inhibitor amprenavir. fosamprenavir : A sulfonamide with a structure based on that of sulfanilamide substituted on the sulfonamide nitrogen by a (2R,3S)-4-phenyl-2-(phosphonooxy)-3-({[(3S)-tetrahydrofuran-3-yloxy]carbonyl}amino)butyl group. It is a pro-drug of the HIV protease inhibitor and antiretroviral drug amprenavir. | 3.23 | 1 | 0 | sulfonamide | prodrug |
| febuxostat Febuxostat: A thiazole derivative and inhibitor of XANTHINE OXIDASE that is used for the treatment of HYPERURICEMIA in patients with chronic GOUT.. febuxostat : A 1,3-thiazolemonocarboxylic acid that is 4-methyl-1,3-thiazole-5-carboxylic acid which is substituted by a 3-cyano-4-(2-methylpropoxy)phenyl group at position 2. It is an orally-active, potent, and selective xanthine oxidase inhibitor used for the treatment of chronic hyperuricaemia in patients with gout. | 3.23 | 1 | 0 | 1,3-thiazolemonocarboxylic acid; aromatic ether; nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor |
| escitalopram Escitalopram: S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.. escitalopram : A 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile that has S-configuration at the chiral centre. It is the active enantiomer of citalopram. | 3.23 | 1 | 0 | 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile | antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| 10-propargyl-10-deazaaminopterin 10-propargyl-10-deazaaminopterin: structure in first source. pralatrexate : A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma. | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pteridines; terminal acetylenic compound | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group. | 3.23 | 1 | 0 | secondary alpha-hydroxy ketone; tetracyclic diterpenoid | antimalarial; antineoplastic agent; photosensitizing agent |
| atazanavir atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). | 3.23 | 1 | 0 | carbohydrazide | antiviral drug; HIV protease inhibitor |
| levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase. | 3.23 | 1 | 0 | 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic | antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor |
| ezetimibe Ezetimibe: An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS.. ezetimibe : A beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer). | 3.23 | 1 | 0 | azetidines; beta-lactam; organofluorine compound | anticholesteremic drug; antilipemic drug; antimetabolite |
| ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract. | 3.23 | 1 | 0 | carbapenemcarboxylic acid; pyrrolidinecarboxamide | antibacterial drug |
| cox 189 lumiracoxib: a COX-2 inhibitor. lumiracoxib : An amino acid that is phenylacetic acid which is substituted at position 2 by the nitrogen of 2-chloro-6-fluoroaniline and at position 5 by a methyl group. A highly selective cyclooxygenase 2 inhibitor, it was briefly used for the treatment of osteoarthritis, but was withdrawn due to concersns of hepatotoxicity. | 3.23 | 1 | 0 | amino acid; monocarboxylic acid; organochlorine compound; organofluorine compound; secondary amino compound | cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| conivaptan conivaptan : The amide resulting from the formal condensation of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid with the benzazepine nitrogen of 2-methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine. It is an antagonist for two of the three types of arginine vasopressin (AVP) receptors, V1a and V2. It is used as its hydrochloride salt for the treatment of hyponatraemia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). | 3.23 | 1 | 0 | benzazepine | aquaretic; vasopressin receptor antagonist |
| moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. | 3.23 | 1 | 0 | aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone | antibacterial drug |
| pralnacasan pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source | 3.23 | 1 | 0 | ||
| clevidipine clevidipine: a calcium channel blocker and antihypertensive agent; structure in first source | 3.23 | 1 | 0 | dihydropyridine | |
| solifenacin [no description available] | 3.23 | 1 | 0 | isoquinolines | |
| dexmethylphenidate dexmethylphenidate : A methyl phenyl(piperidin-2-yl)acetate in which both stereocentres have R configuration. It is the active enantiomer in the racemic drug methylphenidate. | 3.23 | 1 | 0 | methyl phenyl(piperidin-2-yl)acetate | adrenergic agent |
| naproxen Naproxen: An anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout.. naproxen : A methoxynaphthalene that is 2-methoxynaphthalene substituted by a carboxy ethyl group at position 6. Naproxen is a non-steroidal anti-inflammatory drug commonly used for the reduction of pain, fever, inflammation and stiffness caused by conditions such as osteoarthritis, kidney stones, rheumatoid arthritis, psoriatic arthritis, gout, ankylosing spondylitis, menstrual cramps, tendinitis, bursitis, and for the treatment of primary dysmenorrhea. It works by inhibiting both the COX-1 and COX-2 enzymes. | 3.23 | 1 | 0 | methoxynaphthalene; monocarboxylic acid | antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; environmental contaminant; gout suppressant; non-narcotic analgesic; non-steroidal anti-inflammatory drug; xenobiotic |
| cinacalcet cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| lubiprostone [no description available] | 3.23 | 1 | 0 | ||
| telbivudine [no description available] | 3.23 | 1 | 0 | pyrimidine 2'-deoxyribonucleoside | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| paromomycin Paromomycin: An aminoglycoside antibacterial and antiprotozoal agent produced by species of STREPTOMYCES.. paromomycin : An amino cyclitol glycoside that is the 1-O-(2-amino-2-deoxy-alpha-D-glucopyranoside) and the 3-O-(2,6-diamino-2,6-dideoxy-beta-L-idopyranosyl)-beta-D-ribofuranoside of 4,6-diamino-2,3-dihydroxycyclohexane (the 1R,2R,3S,4R,6S diastereoisomer). It is obtained from various Streptomyces species. A broad-spectrum antibiotic, it is used (generally as the sulfate salt) for the treatment of acute and chronic intestinal protozoal infections, but is not effective for extraintestinal protozoal infections. It is also used as a therapeutic against visceral leishmaniasis. | 3.23 | 1 | 0 | amino cyclitol glycoside; aminoglycoside antibiotic | anthelminthic drug; antibacterial drug; antiparasitic agent; antiprotozoal drug |
| anidulafungin Anidulafungin: Echinocandin antifungal agent that is used in the treatment of CANDIDEMIA and CANDIDIASIS.. anidulafungin : A semisynthetic echinocandin anti-fungal drug. It is active against Aspergillus and Candida species and is used for the treatment of invasive candidiasis. | 3.23 | 1 | 0 | antibiotic antifungal drug; azamacrocycle; echinocandin; heterodetic cyclic peptide; semisynthetic derivative | |
| 17 alpha-hydroxyprogesterone caproate 17 alpha-Hydroxyprogesterone Caproate: Hydroxyprogesterone derivative that acts as a PROGESTIN and is used to reduce the risk of recurrent MISCARRIAGE and of PREMATURE BIRTH. It is also used in combination with ESTROGEN in the management of MENSTRUATION DISORDERS. | 3.23 | 1 | 0 | corticosteroid hormone | |
| varenicline Varenicline: A benzazepine derivative that functions as an ALPHA4-BETA2 NICOTINIC RECEPTOR partial agonist. It is used for SMOKING CESSATION.. varenicline : An organic heterotetracyclic compound that acts as a partial agonist for nicotinic cholinergic receptors and is used (in the form of its tartate salt) as an aid to giving up smoking. | 3.23 | 1 | 0 | ||
| fiduxosin fiduxosin: fiduxosin (ABT-980) is the (3aR,9bR)-isomer; structure in first source | 3.23 | 1 | 0 | ||
| atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3. | 3.23 | 1 | 0 | ||
| erlotinib [no description available] | 3.23 | 1 | 0 | aromatic ether; quinazolines; secondary amino compound; terminal acetylenic compound | antineoplastic agent; epidermal growth factor receptor antagonist; protein kinase inhibitor |
| etravirine [no description available] | 3.23 | 1 | 0 | aminopyrimidine; aromatic ether; dinitrile; organobromine compound | antiviral agent; HIV-1 reverse transcriptase inhibitor |
| dronedarone Dronedarone: A non-iodinated derivative of amiodarone that is used for the treatment of ARRHYTHMIA.. dronedarone : A member of the class of 1-benzofurans used for the treatment of cardiac arrhythmias. | 3.23 | 1 | 0 | 1-benzofurans; aromatic ether; aromatic ketone; sulfonamide; tertiary amino compound | anti-arrhythmia drug; environmental contaminant; xenobiotic |
| ramelteon ramelteon: melatonin MT1/MT2 receptor agonist | 3.23 | 1 | 0 | indanes | |
| lapatinib [no description available] | 3.23 | 1 | 0 | furans; organochlorine compound; organofluorine compound; quinazolines | antineoplastic agent; tyrosine kinase inhibitor |
| darunavir Darunavir: An HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.. darunavir : An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors. | 3.23 | 1 | 0 | carbamate ester; furofuran; sulfonamide | antiviral drug; HIV protease inhibitor |
| deferasirox Deferasirox: A triazole and benzoate derivative that acts as a selective iron chelator. It is used in the management of chronic IRON OVERLOAD due to blood transfusion or non-transfusion dependent THALASSEMIA.. deferasirox : A member of the class of triazoles, deferasirox is 1,2,4-triazole substituted by a 4-carboxyphenyl group at position 1 and by 2-hydroxyphenyl groups at positions 3 and 5. An orally active iron chelator, it is used to manage chronic iron overload in patients receiving long-term blood transfusions. | 3.23 | 1 | 0 | benzoic acids; monocarboxylic acid; phenols; triazoles | iron chelator |
| tbc-11251 sitaxsentan: endothelin A receptor antagonist; structure in first source | 3.23 | 1 | 0 | benzodioxoles | |
| tolvaptan [no description available] | 3.23 | 1 | 0 | benzazepine; benzenedicarboxamide | aquaretic; vasopressin receptor antagonist |
| sorafenib [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide | angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor |
| lenalidomide [no description available] | 3.23 | 1 | 0 | aromatic amine; dicarboximide; isoindoles; piperidones | angiogenesis inhibitor; antineoplastic agent; immunomodulator |
| regadenoson [no description available] | 3.23 | 1 | 0 | purine nucleoside | |
| lacosamide Lacosamide: An acetamide derivative that acts as a blocker of VOLTAGE-GATED SODIUM CHANNELS. It is used as an anticonvulsant, for adjunctive or monotherapy, in the treatment of PARTIAL SEIZURES. | 3.23 | 1 | 0 | N-acyl-amino acid | |
| vincaleukoblastine [no description available] | 3.23 | 1 | 0 | acetate ester; indole alkaloid fundamental parent; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; tertiary alcohol; tertiary amino compound; vinca alkaloid | antineoplastic agent; immunosuppressive agent; microtubule-destabilising agent; plant metabolite |
| benzarone benzarone: antihemorrhagic agent; structure | 3.23 | 1 | 0 | 1-benzofurans | |
| estramustine Estramustine: A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.. estramustine : A carbamate ester obtained by the formal condensation of the hydroxy group of 17beta-estradiol with the carboxy group of bis(2-chloroethyl)carbamic acid. | 3.23 | 1 | 0 | 17beta-hydroxy steroid; carbamate ester; organochlorine compound | alkylating agent; antineoplastic agent; radiation protective agent |
| bortezomib [no description available] | 3.23 | 1 | 0 | amino acid amide; L-phenylalanine derivative; pyrazines | antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor |
| ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver. | 3.23 | 1 | 0 | 1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas | antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic |
| oxytocin Oxytocin: A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.. oxytocin : A cyclic nonapeptide hormone with amino acid sequence CYIQNCPLG that also acts as a neurotransmitter in the brain; the principal uterine-contracting and milk-ejecting hormone of the posterior pituitary. Together with the neuropeptide vasopressin, it is believed to influence social cognition and behaviour. | 3.71 | 2 | 0 | heterodetic cyclic peptide; peptide hormone | oxytocic; vasodilator agent |
| pentostatin Pentostatin: A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.. pentostatin : A member of the class of coformycins that is coformycin in which the hydroxy group at position 2' is replaced with a hydrogen. It is a drug used for the treatment of hairy cell leukaemia. | 3.23 | 1 | 0 | coformycins | antimetabolite; antineoplastic agent; Aspergillus metabolite; bacterial metabolite; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy. | 3.23 | 1 | 0 | cinchona alkaloid | alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker |
| meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively. | 3.23 | 1 | 0 | alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide | antibacterial agent; antibacterial drug; drug allergen |
| griseofulvin Griseofulvin: An antifungal agent used in the treatment of TINEA infections.. griseofulvin : An oxaspiro compound produced by Penicillium griseofulvum. It is used by mouth as an antifungal drug for infections involving the scalp, hair, nails and skin that do not respond to topical treatment. | 3.23 | 1 | 0 | 1-benzofurans; antibiotic antifungal drug; benzofuran antifungal drug; organochlorine compound; oxaspiro compound | antibacterial agent; Penicillium metabolite |
| cefoxitin Cefoxitin: A semisynthetic cephamycin antibiotic resistant to beta-lactamase.. cefoxitin : A semisynthetic cephamycin antibiotic which, in addition to the methoxy group at the 7alpha position, has 2-thienylacetamido and carbamoyloxymethyl side-groups. It is resistant to beta-lactamase. | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; cephalosporin; cephamycin; semisynthetic derivative | antibacterial drug |
| saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease. | 3.23 | 1 | 0 | L-asparagine derivative; quinolines | antiviral drug; HIV protease inhibitor |
| pancuronium Pancuronium: A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.. pancuronium : A steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant. | 3.23 | 1 | 0 | acetate ester; steroid ester | cholinergic antagonist; muscle relaxant; nicotinic antagonist |
| abacavir abacavir: a carbocyclic nucleoside with potent selective anti-HIV activity. abacavir : A 2,6-diaminopurine that is (1S)-cyclopent-2-en-1-ylmethanol in which the pro-R hydrogen at the 4-position is substituted by a 2-amino-6-(cyclopropylamino)-9H-purin-9-yl group. A nucleoside analogue reverse transcriptase inhibitor (NRTI) with antiretroviral activity against HIV, it is used (particularly as the sulfate) with other antiretrovirals in combination therapy of HIV infection. | 3.23 | 1 | 0 | 2,6-diaminopurines | antiviral drug; drug allergen; HIV-1 reverse transcriptase inhibitor |
| miglitol [no description available] | 3.23 | 1 | 0 | piperidines | |
| metyrosine alpha-methyl-L-tyrosine : An L-tyrosine derivative that consists of L-tyrosine bearing an additional methyl substituent at position 2. An inhibitor of the enzyme tyrosine 3-monooxygenase, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with pheochromocytoma. | 3.23 | 1 | 0 | L-tyrosine derivative; non-proteinogenic L-alpha-amino acid | antihypertensive agent; EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor |
| linezolid [no description available] | 3.23 | 1 | 0 | acetamides; morpholines; organofluorine compound; oxazolidinone | antibacterial drug; protein synthesis inhibitor |
| clindamycin phosphate [no description available] | 3.23 | 1 | 0 | ||
| eplerenone Eplerenone: A spironolactone derivative and selective ALDOSTERONE RECEPTOR antagonist that is used in the management of HYPERTENSION and CONGESTIVE HEART FAILURE, post-MYOCARDIAL INFARCTION. | 3.23 | 1 | 0 | 3-oxo-Delta(4) steroid; epoxy steroid; gamma-lactone; methyl ester; organic heteropentacyclic compound; oxaspiro compound; steroid acid ester | aldosterone antagonist; antihypertensive agent |
| tolterodine [no description available] | 3.23 | 1 | 0 | tertiary amine | antispasmodic drug; muscarinic antagonist; muscle relaxant |
| darifenacin darifenacin : 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence. | 3.23 | 1 | 0 | 1-benzofurans; monocarboxylic acid amide; pyrrolidines | antispasmodic drug; muscarinic antagonist |
| tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry. | 3.23 | 1 | 0 | retinoic acid; vitamin A | anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule |
| retinol Vitamin A: Retinol and derivatives of retinol that play an essential role in metabolic functioning of the retina, the growth of and differentiation of epithelial tissue, the growth of bone, reproduction, and the immune response. Dietary vitamin A is derived from a variety of CAROTENOIDS found in plants. It is enriched in the liver, egg yolks, and the fat component of dairy products.. vitamin A : Any member of a group of fat-soluble retinoids produced via metabolism of provitamin A carotenoids that exhibit biological activity against vitamin A deficiency. Vitamin A is involved in immune function, vision, reproduction, and cellular communication.. all-trans-retinol : A retinol in which all four exocyclic double bonds have E- (trans-) geometry.. retinol : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraen-1-ol substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified). | 3.23 | 1 | 0 | retinol; vitamin A | human metabolite; mouse metabolite; plant metabolite |
| tacrolimus Tacrolimus: A macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.. tacrolimus (anhydrous) : A macrolide lactam containing a 23-membered lactone ring, originally isolated from the fermentation broth of a Japanese soil sample that contained the bacteria Streptomyces tsukubaensis. | 3.23 | 1 | 0 | macrolide lactam | bacterial metabolite; immunosuppressive agent |
| rosuvastatin rosuvastatin : A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; monofluorobenzenes; pyrimidines; statin (synthetic); sulfonamide | anti-inflammatory agent; antilipemic drug; cardioprotective agent; CETP inhibitor; environmental contaminant; xenobiotic |
| mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | 2-benzofurans; gamma-lactone; monocarboxylic acid; phenols | anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic |
| clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic. | 3.23 | 1 | 0 | ||
| fosfomycin Fosfomycin: An antibiotic produced by Streptomyces fradiae.. fosfomycin : A phosphonic acid having an (R,S)-1,2-epoxypropyl group attached to phosphorus. | 3.23 | 1 | 0 | epoxide; phosphonic acids | antimicrobial agent; EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor |
| zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections. | 3.23 | 1 | 0 | macrolide antibiotic | antibacterial drug; environmental contaminant; xenobiotic |
| eptifibatide [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; macrocycle; organic disulfide | anticoagulant; platelet aggregation inhibitor |
| decitabine [no description available] | 3.23 | 1 | 0 | 2'-deoxyribonucleoside | |
| teniposide [no description available] | 3.23 | 1 | 0 | aromatic ether; beta-D-glucoside; cyclic acetal; furonaphthodioxole; gamma-lactone; monosaccharide derivative; phenols; thiophenes | antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor |
| dactinomycin Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015) | 3.23 | 1 | 0 | actinomycin | mutagen |
| melphalan Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring. | 3.23 | 1 | 0 | L-phenylalanine derivative; nitrogen mustard; non-proteinogenic L-alpha-amino acid; organochlorine compound | alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent |
| tenofovir tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. | 3.23 | 1 | 0 | nucleoside analogue; phosphonic acids | antiviral drug; drug metabolite; HIV-1 reverse transcriptase inhibitor |
| posaconazole [no description available] | 3.23 | 1 | 0 | aromatic ether; conazole antifungal drug; N-arylpiperazine; organofluorine compound; oxolanes; triazole antifungal drug; triazoles | trypanocidal drug |
| micafungin Micafungin: A cyclic lipo-hexapeptide echinocandin antifungal agent that is used for the treatment and prevention of CANDIDIASIS.. micafungin : A cyclic hexapeptide echinocandin antibiotic which exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. It is used as the sodium salt for the treatment of invasive candidiasis, and of aspergillosis in patients who are intolerant of other therapy. | 3.23 | 1 | 0 | antibiotic antifungal drug; echinocandin | antiinfective agent |
| riboflavin vitamin B2 : Any member of a group of vitamers that belong to the chemical structural class called flavins that exhibit biological activity against vitamin B2 deficiency. Symptoms associated with vitamin B2 deficiency include glossitis, seborrhea, angular stomaitis, cheilosis and photophobia. The vitamers include riboflavin and its phosphate derivatives (and includes their salt, ionised and hydrate forms). | 3.23 | 1 | 0 | flavin; vitamin B2 | anti-inflammatory agent; antioxidant; cofactor; Escherichia coli metabolite; food colouring; fundamental metabolite; human urinary metabolite; mouse metabolite; photosensitizing agent; plant metabolite |
| sodium bicarbonate Sodium Bicarbonate: A white, crystalline powder that is commonly used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions. | 3.23 | 1 | 0 | one-carbon compound; organic sodium salt | antacid; food anticaking agent |
| arsenic trioxide Tetraarsenic Oxide: A form of As2O3 that exists as As4O6 in the solid state. It dissociates to As2O3 upon heating to the vapor phase above 800 degrees Celsius. | 3.23 | 1 | 0 | arsenic oxide | antineoplastic agent; insecticide |
| sr 90107 fondaparinux sodium : An organic sodium salt, being the decasodium salt of fondaparinux. | 3.23 | 1 | 0 | ||
| meglumine iodipamide [no description available] | 3.23 | 1 | 0 | organoammonium salt | radioopaque medium |
| thyrotropin-releasing hormone PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence. | 3.23 | 1 | 0 | peptide hormone; tripeptide | human metabolite |
| arginine vasopressin Arginine Vasopressin: The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.. argipressin : The predominant form of mammalian vasopressin (antidiuretic hormone). It is a nonapeptide containing an arginine at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. | 3.71 | 2 | 0 | vasopressin | cardiovascular drug; hematologic agent; mitogen |
| s 1033 [no description available] | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| propylthiouracil Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534). 6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group. | 3.23 | 1 | 0 | pyrimidinethione | antidote to paracetamol poisoning; antimetabolite; antioxidant; antithyroid drug; carcinogenic agent; EC 1.14.13.39 (nitric oxide synthase) inhibitor; hormone antagonist |
| etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. | 3.23 | 1 | 0 | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| mercaptopurine Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.. purine-6-thiol : A thiol that is the tautomer of mercaptopurine.. mercaptopurine : A member of the class of purines that is 6,7-dihydro-1H-purine carrying a thione group at position 6. An adenine analogue, it is used in the treatment of acute lymphocytic leukemia (ALL), chronic myeloid leukemia (CML), Crohn's disease, and ulcerative colitis. | 3.23 | 1 | 0 | aryl thiol; purines; thiocarbonyl compound | anticoronaviral agent; antimetabolite; antineoplastic agent |
| pyrantel Pyrantel: A depolarizing neuromuscular-blocking agent, that causes persistent nicotinic activation resulting in spastic paralysis of susceptible nematodes. It is a drug of second-choice after benzimidazoles for treatment of ascariasis, hookworm, and pinworm infections, being effective after a single dose. (From Smith and Reynard, Textbook of Pharmacology, 1992, p920). pyrantel : A carboxamidine that is 1,4,5,6-tetrahydropyrimidine that is substituted at position 1 by a methyl group and at position 2 by an (E)-2-(2-thienyl)vinyl group. It is used, particularly as the embonate [4,4'-methylenebis(3-hydroxy-2-naphthoate)] salt, as an anthelmintic that is effective against intestinal nematodes including threadworms, roundworms and hookworms, and is included in the WHO 'Model List of Essential Medicines'. | 3.23 | 1 | 0 | 1,4,5,6-tetrahydropyrimidines; carboxamidine; thiophenes | antinematodal drug |
| thiothixene [no description available] | 3.23 | 1 | 0 | N-methylpiperazine | anticoronaviral agent |
| eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. | 3.23 | 1 | 0 | zopiclone | central nervous system depressant; sedative |
| benztropine Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.. benzatropine : Tropane in which a hydrogen at position 3 is substituted by a diphenylmethoxy group (endo-isomer). An acetylcholine receptor antagonist, it is used (particularly as its methanesulphonate salt) in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments. | 3.23 | 1 | 0 | diarylmethane | |
| methimazole Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. | 3.23 | 1 | 0 | 1,3-dihydroimidazole-2-thiones | antithyroid drug |
| sulindac Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects.. sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions. | 3.23 | 1 | 0 | monocarboxylic acid; organofluorine compound; sulfoxide | analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent |
| terbinafine [no description available] | 3.23 | 1 | 0 | acetylenic compound; allylamine antifungal drug; enyne; naphthalenes; tertiary amine | EC 1.14.13.132 (squalene monooxygenase) inhibitor; P450 inhibitor; sterol biosynthesis inhibitor |
| thioguanine anhydrous Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia. | 3.23 | 1 | 0 | 2-aminopurines | anticoronaviral agent; antimetabolite; antineoplastic agent |
| succimer Succimer: A mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them.. succimer : A sulfur-containing carboxylic acid that is succinic acid bearing two mercapto substituents at positions 2 and 3. A lead chelator used as an antedote to lead poisoning. | 3.23 | 1 | 0 | dicarboxylic acid; dithiol; sulfur-containing carboxylic acid | chelator |
| digoxin Digoxin: A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666). digoxin : A cardenolide glycoside that is digitoxin beta-hydroxylated at C-12. A cardiac glycoside extracted from the foxglove plant, Digitalis lanata, it is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation, but the margin between toxic and therapeutic doses is small. | 3.23 | 1 | 0 | cardenolide glycoside; steroid saponin | anti-arrhythmia drug; cardiotonic drug; EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor; epitope |
| streptozocin [no description available] | 3.23 | 1 | 0 | ||
| tamoxifen [no description available] | 3.23 | 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. | 3.23 | 1 | 0 | pyridines; thiocarboxamide | antilipemic drug; antitubercular agent; fatty acid synthesis inhibitor; leprostatic drug; prodrug |
| cancidas [no description available] | 3.23 | 1 | 0 | ||
| lincomycin Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis. | 3.23 | 1 | 0 | carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound | antimicrobial agent; bacterial metabolite |
| ranitidine Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease. | 3.23 | 1 | 0 | C-nitro compound; furans; organic sulfide; tertiary amino compound | anti-ulcer drug; drug allergen; environmental contaminant; H2-receptor antagonist; xenobiotic |
| aplaviroc aplaviroc: a spiro-diketo-piperazine; a potent noncompetitive allosteric antagonist of the CCR5 receptor with concomitantly potent antiviral effects for HIV-1; structure in first source | 3.23 | 1 | 0 | ||
| hmr 3647 [no description available] | 3.23 | 1 | 0 | ||
| maraviroc [no description available] | 3.23 | 1 | 0 | tropane alkaloid | |
| toremifene Toremifene: A first generation selective estrogen receptor modulator (SERM). Like TAMOXIFEN, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. | 3.23 | 1 | 0 | aromatic ether; organochlorine compound; tertiary amine | antineoplastic agent; bone density conservation agent; estrogen antagonist; estrogen receptor modulator |
| nelarabine nelarabine: prodrug of ara-G. nelarabine : A purine nucleoside in which O-methylguanine is attached to arabinofuranose via a beta-N(9)-glycosidic bond. Inhibits DNA synthesis and causes cell death; a prodrug of 9-beta-D-arabinofuranosylguanine (ara-G). | 3.23 | 1 | 0 | beta-D-arabinoside; monosaccharide derivative; purine nucleoside | antineoplastic agent; DNA synthesis inhibitor; prodrug |
| dermatan sulfate Dermatan Sulfate: A naturally occurring glycosaminoglycan found mostly in the skin and in connective tissue. It differs from CHONDROITIN SULFATE A (see CHONDROITIN SULFATES) by containing IDURONIC ACID in place of glucuronic acid, its epimer, at carbon atom 5. (from Merck, 12th ed). alpha-L-IdopA-(1->3)-beta-D-GalpNAc4S : An oligosaccharide sulfate that is 2-acetamido-2-deoxy-4-O-sulfo-beta-D-galactopyranose in which the hydroxy group at position 3 has been converted to the corresponding alpha-L-idopyranuronoside.. dermatan sulfate : Any of a group of glycosaminoglycans with repeating units consisting of variously sulfated beta1->4-linked L-iduronyl-(alpha1->3)-N-acetyl-D-galactosamine units. | 3.23 | 1 | 0 | amino disaccharide; glycosylgalactose derivative; iduronic acids; oligosaccharide sulfate | |
| dolasetron [no description available] | 3.23 | 1 | 0 | indolyl carboxylic acid | |
| orlistat Orlistat: A lactone derivative of LEUCINE that acts as a pancreatic lipase inhibitor to limit the absorption of dietary fat; it is used in the management of obesity.. orlistat : A carboxylic ester resulting from the formal condensation of the carboxy group of N-formyl-L-leucine with the hydroxy group of (3S,4S)-3-hexyl-4-[(2S)-2-hydroxytridecyl]oxetan-2-one. A pancreatic lipase inhibitor, it is used as an anti-obesity drug. | 3.23 | 1 | 0 | beta-lactone; carboxylic ester; formamides; L-leucine derivative | anti-obesity agent; bacterial metabolite; EC 2.3.1.85 (fatty acid synthase) inhibitor; EC 3.1.1.3 (triacylglycerol lipase) inhibitor |
| quinine [no description available] | 3.23 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| fospropofol [no description available] | 3.23 | 1 | 0 | alkylbenzene | |
| rasagiline [no description available] | 3.23 | 1 | 0 | indanes; secondary amine; terminal acetylenic compound | EC 1.4.3.4 (monoamine oxidase) inhibitor; neuroprotective agent |
| dasatinib N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN). | 3.23 | 1 | 0 | 1,3-thiazoles; aminopyrimidine; monocarboxylic acid amide; N-(2-hydroxyethyl)piperazine; N-arylpiperazine; organochlorine compound; secondary amino compound; tertiary amino compound | anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor |
| sitagliptin sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity. | 3.23 | 1 | 0 | triazolopyrazine; trifluorobenzene | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; environmental contaminant; hypoglycemic agent; serine proteinase inhibitor; xenobiotic |
| tolcapone Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase. | 3.23 | 1 | 0 | 2-nitrophenols; benzophenones; catechols | antiparkinson drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| calcitriol dihydroxy-vitamin D3: as a major in vitro metabolite of 1alpha,25-dihydroxyvitamin D3, produced in primary cultures of neonatal human keratinocytes | 3.23 | 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 |
| vitamin d 2 Ergocalciferols: Derivatives of ERGOSTEROL formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. They differ from CHOLECALCIFEROL in having a double bond between C22 and C23 and a methyl group at C24.. vitamin D2 : A vitamin D supplement and has been isolated from alfalfa. | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-ergostane; vitamin D | bone density conservation agent; nutraceutical; plant metabolite; rodenticide |
| amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections. | 3.23 | 1 | 0 | antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic | antiamoebic agent; antiprotozoal drug; bacterial metabolite |
| pulmicort Budesonide: A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.. budesonide : A glucocorticoid steroid having a highly oxygenated pregna-1,4-diene structure. It is used mainly in the treatment of asthma and non-infectious rhinitis and for treatment and prevention of nasal polyposis. | 3.23 | 1 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; cyclic acetal; glucocorticoid; primary alpha-hydroxy ketone | anti-inflammatory drug; bronchodilator agent; drug allergen |
| oxymetholone Oxymetholone: A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed). oxymetholone : A 3-oxo-5alpha- steroid that is 4,5alpha-dihydrotestosterone which is substituted by a hydroxymethylidene group at position 2 and by a methyl group at the 17alpha position. A synthetic androgen, it was mainly used for the treatment of anaemias until being replaced by treatments with fewer side effects. | 3.23 | 1 | 0 | ||
| eprosartan eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. | 3.23 | 1 | 0 | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| montelukast montelukast: a leukotriene D4 receptor antagonist | 3.23 | 1 | 0 | aliphatic sulfide; monocarboxylic acid; quinolines | anti-arrhythmia drug; anti-asthmatic drug; leukotriene antagonist |
| mivacurium Mivacurium: An isoquinoline derivative that is used as a short-acting non-depolarizing agent. | 3.23 | 1 | 0 | isoquinolines | |
| hemabate carboprost tromethamine : The tromethamine salt of carboprost. It is used as an abortifacient agent that is effective in both the first and second trimesters of pregnancy. | 3.23 | 1 | 0 | ||
| mycophenolate mofetil mycophenolate mofetil : A carboxylic ester resulting from the formal condensation between the carboxylic acid group of mycophenolic acid and the hydroxy group of 2-(morpholin-4-yl)ethanol. In the liver, it is metabolised to mycophenolic acid, an immunosuppressant for which it is a prodrug. It is widely used to prevent tissue rejection following organ transplants as well as for the treatment of certain autoimmune diseases. | 3.23 | 1 | 0 | carboxylic ester; ether; gamma-lactone; phenols; tertiary amino compound | anticoronaviral agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; immunosuppressive agent; prodrug |
| entacapone entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group. | 3.23 | 1 | 0 | 2-nitrophenols; catechols; monocarboxylic acid amide; nitrile | antidyskinesia agent; antiparkinson drug; central nervous system drug; EC 2.1.1.6 (catechol O-methyltransferase) inhibitor |
| paricalcitol [no description available] | 3.23 | 1 | 0 | hydroxy seco-steroid; seco-cholestane | antiparathyroid drug |
| 7432 s Ceftibuten: A cephalosporin antibacterial agent that is used in the treatment of infections, including urinary-tract and respiratory-tract infections.. ceftibuten : A third-generation cephalosporin antibiotic with a [(2Z)-2-(2-amino-1,3-thiazol-4-yl)-4-carboxybut-2-enoyl]amino substituent at the 7 position of the cephem skeleton. An orally-administered agent, ceftibuten is used as the dihydrate to treat urinary-tract and respiratory-tract infections. | 3.23 | 1 | 0 | cephalosporin; dicarboxylic acid | antibacterial drug |
| isotretinoin Isotretinoin: A topical dermatologic agent that is used in the treatment of ACNE VULGARIS and several other skin diseases. The drug has teratogenic and other adverse effects.. isotretinoin : A retinoic acid that is all-trans-retinoic acid in which the double bond which is alpha,beta- to the carboxy group is isomerised to Z configuration. A synthetic retinoid, it is used for the treatment of severe cases of acne and other skin diseases. | 3.23 | 1 | 0 | retinoic acid | antineoplastic agent; keratolytic drug; teratogenic agent |
| epoprostenol [no description available] | 3.23 | 1 | 0 | prostaglandins I | mouse metabolite |
| indocyanine green [no description available] | 3.23 | 1 | 0 | 1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye | |
| triprolidine Triprolidine: Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness.. triprolidine : An N-alkylpyrrolidine that is acrivastine in which the pyridine ring is lacking the propenoic acid substituent. It is a sedating antihistamine that is used (generally as the monohydrochloride monohydrate) for the relief of the symptoms of uticaria, rhinitis, and various pruritic skin disorders. | 3.23 | 1 | 0 | N-alkylpyrrolidine; olefinic compound; pyridines | H1-receptor antagonist |
| pitavastatin pitavastatin : A dihydroxy monocarboxylic acid that is (6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]hept-6-enoic acid in which the two hydroxy groups are located at positions 3 and 5 (the 3R,5S-stereoisomer). Used as its calcium salt for treatment of hypercholesterolemia (elevated levels of cholesterol in the blood) on patients unable to sufficiently lower their cholesterol levels by diet and exercise. | 3.23 | 1 | 0 | cyclopropanes; dihydroxy monocarboxylic acid; monofluorobenzenes; quinolines; statin (synthetic) | antioxidant |
| ethamolin monoethanolamine oleate: used for treatment of pyogenic granuloma | 3.23 | 1 | 0 | long-chain fatty acid | |
| alatrofloxacin mesylate [no description available] | 3.23 | 1 | 0 | ||
| codeine [no description available] | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | antitussive; drug allergen; environmental contaminant; opioid analgesic; opioid receptor agonist; prodrug; xenobiotic |
| cyclosporine ramihyphin A: one of the metabolites produced by Fusarium sp. S-435; RN given refers to cpd with unknown MF | 3.23 | 1 | 0 | homodetic cyclic peptide | anti-asthmatic drug; anticoronaviral agent; antifungal agent; antirheumatic drug; carcinogenic agent; dermatologic drug; EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor; geroprotector; immunosuppressive agent; metabolite |
| acitretin Acitretin: An oral retinoid effective in the treatment of psoriasis. It is the major metabolite of ETRETINATE with the advantage of a much shorter half-life when compared with etretinate.. acitretin : A retinoid that consists of 3,7-dimethylnona-2,4,6,8-tetraenoic acid having a 4-methoxy-2,3,6-trimethylphenyl group attached at position 9. | 3.23 | 1 | 0 | acitretin; alpha,beta-unsaturated monocarboxylic acid; retinoid | keratolytic drug |
| estropipate estropipate: used therapeutically in menopausal patients | 3.23 | 1 | 0 | piperazinium salt; steroid sulfate | |
| hydromorphone Hydromorphone: An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine.. hydromorphone : A morphinane alkaloid that is a hydrogenated ketone derivative of morphine. A semi-synthetic drug, it is a centrally acting pain medication of the opioid class. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound | mu-opioid receptor agonist; opioid analgesic |
| levetiracetam Levetiracetam: A pyrrolidinone and acetamide derivative that is used primarily for the treatment of SEIZURES and some movement disorders, and as a nootropic agent.. levetiracetam : A pyrrolidinone and carboxamide that is N-methylpyrrolidin-2-one in which one of the methyl hydrogens is replaced by an aminocarbonyl group, while another is replaced by an ethyl group (the S enantiomer). An anticonvulsant, it is used for the treatment of epilepsy in both human and veterinary medicine. | 3.23 | 1 | 0 | pyrrolidin-2-ones | anticonvulsant; environmental contaminant; xenobiotic |
| ly 163892 loracarbef: 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring. loracarbef : A synthetic "carba" analogue of cefaclor, with carbon replacing sulfur at position 1. Used to treat a wide range of infections caused by both gram-positive and gram-negative bacteria. | 3.23 | 1 | 0 | carbacephem; zwitterion | antibacterial drug; antimicrobial agent |
| nabilone nabilone: cannabinol deriv; RN given refers to cpd without isomeric designation; structure | 3.23 | 1 | 0 | ||
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| oxycodone Oxycodone: A semisynthetic derivative of CODEINE.. oxycodone : A semisynthetic opioid of formula C18H21NO4 that is derived from thebaine. It is a moderately potent opioid analgesic, generally used for relief of moderate to severe pain. | 3.23 | 1 | 0 | organic heteropentacyclic compound; semisynthetic derivative | antitussive; mu-opioid receptor agonist; opioid analgesic |
| oxymorphone Oxymorphone: An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) | 3.23 | 1 | 0 | morphinane alkaloid | |
| vitamin k 1 Vitamin K 1: A family of phylloquinones that contains a ring of 2-methyl-1,4-naphthoquinone and an isoprenoid side chain. Members of this group of vitamin K 1 have only one double bond on the proximal isoprene unit. Rich sources of vitamin K 1 include green plants, algae, and photosynthetic bacteria. Vitamin K1 has antihemorrhagic and prothrombogenic activity.. phylloquinone : A member of the class of phylloquinones that consists of 1,4-naphthoquinone having methyl and phytyl groups at positions 2 and 3 respectively. The parent of the class of phylloquinones. | 3.23 | 1 | 0 | phylloquinones; vitamin K | cofactor; human metabolite; plant metabolite |
| sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent. | 3.23 | 1 | 0 | antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol | antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor |
| topiramate Topiramate: A sulfamate-substituted fructose analog that was originally identified as a hypoglycemic agent. It is used for the treatment of EPILEPSY and MIGRAINE DISORDERS, and may also promote weight loss.. topiramate : A hexose derivative that is 2,3:4,5-di-O-isopropylidene-beta-D-fructopyranose in which the hydroxy group has been converted to the corresponding sulfamate ester. It blocks voltage-dependent sodium channels and is used as an antiepileptic and for the prevention of migraine. | 3.23 | 1 | 0 | cyclic ketal; ketohexose derivative; sulfamate ester | anticonvulsant; sodium channel blocker |
| trospium chloride trospium chloride : An organic chloride salt of trospium. It is an antispasmodic drug used for the treatment of overactive bladder. | 3.23 | 1 | 0 | ||
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 3.23 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound | anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic |
| benzphetamine Benzphetamine: A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222). benzphetamine : Dextroamphetamine in which the the hydrogens attached to the amino group are substituted by a methyl and a benzyl group. A sympathomimetic agent with properties similar to dextroamphetamine, it is used as its hydrochloride salt in the treatment of obesity. | 3.23 | 1 | 0 | amphetamines; tertiary amine | adrenergic uptake inhibitor; appetite depressant; dopamine uptake inhibitor; sympathomimetic agent |
| deamino arginine vasopressin Deamino Arginine Vasopressin: A synthetic analog of the pituitary hormone, ARGININE VASOPRESSIN. Its action is mediated by the VASOPRESSIN receptor V2. It has prolonged antidiuretic activity, but little pressor effects. It also modulates levels of circulating FACTOR VIII and VON WILLEBRAND FACTOR. | 3.71 | 2 | 0 | heterodetic cyclic peptide | diagnostic agent; renal agent; vasopressin receptor agonist |
| dexmedetomidine [no description available] | 3.23 | 1 | 0 | medetomidine | alpha-adrenergic agonist; analgesic; non-narcotic analgesic; sedative |
| goserelin Goserelin: A synthetic long-acting agonist of GONADOTROPIN-RELEASING HORMONE. Goserelin is used in treatments of malignant NEOPLASMS of the prostate, uterine fibromas, and metastatic breast cancer. | 3.23 | 1 | 0 | organic molecular entity | |
| nalbuphine Nalbuphine: A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. | 3.23 | 1 | 0 | organic heteropentacyclic compound | mu-opioid receptor antagonist; opioid analgesic |
| nateglinide Nateglinide: A phenylalanine and cyclohexane derivative that acts as a hypoglycemic agent by stimulating the release of insulin from the pancreas. It is used in the treatment of TYPE 2 DIABETES.. nateglinide : An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-administered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus. | 3.23 | 1 | 0 | phenylalanine derivative | |
| vinorelbine [no description available] | 3.23 | 1 | 0 | acetate ester; methyl ester; organic heteropentacyclic compound; organic heterotetracyclic compound; ring assembly; vinca alkaloid | antineoplastic agent; photosensitizing agent |
| silodosin silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source | 3.23 | 1 | 0 | indolecarboxamide | |
| fluvoxamine Fluvoxamine: A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.. fluvoxamine : An oxime O-ether that is benzene substituted by a (1E)-N-(2-aminoethoxy)-5-methoxypentanimidoyl group at position 1 and a trifluoromethyl group at position 4. It is a selective serotonin reuptake inhibitor that is used for the treatment of obsessive-compulsive disorder. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; 5-methoxyvalerophenone O-(2-aminoethyl)oxime | antidepressant; anxiolytic drug; serotonin uptake inhibitor |
| su 11248 [no description available] | 3.23 | 1 | 0 | monocarboxylic acid amide; pyrroles | angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist |
| fosbretabulin [no description available] | 2.17 | 1 | 0 | stilbenoid | |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid : A dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers. | 3.23 | 1 | 0 | dihydroxy monocarboxylic acid; indoles; organofluorine compound | |
| levorphanol Levorphanol: A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. | 3.23 | 1 | 0 | morphinane alkaloid | |
| naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | 3.23 | 1 | 0 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| dextromethorphan Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.. dextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough. | 3.23 | 1 | 0 | 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene | antitussive; environmental contaminant; neurotoxin; NMDA receptor antagonist; oneirogen; prodrug; xenobiotic |
| butorphanol Butorphanol: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.. butorphanol : Levorphanol in which a hydrogen at position 14 of the morphinan skeleton is substituted by hydroxy and one of the hydrogens of the N-methyl group is substituted by cyclopropyl. A semi-synthetic opioid agonist-antagonist analgesic, it is used as its (S,S)-tartaric acid salt for relief or moderate to severe pain. | 3.23 | 1 | 0 | morphinane alkaloid | antitussive; kappa-opioid receptor agonist; mu-opioid receptor agonist; opioid analgesic |
| cefixime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug; drug allergen |
| lisinopril Lisinopril: One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure. | 3.23 | 1 | 0 | dipeptide | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| benazepril benazepril: structure given in first source. benazepril : A benzazepine that is benazeprilat in which the carboxy group of the 2-amino-4-phenylbutanoic acid moiety has been converted to the corresponding ethyl ester. It is used (generally as its hydrochloride salt) as a prodrug for the angiotensin-converting enzyme inhibitor benazeprilat in the treatment of hypertension and heart failure. | 3.23 | 1 | 0 | benzazepine; dicarboxylic acid monoester; ethyl ester; lactam | EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| ramipril Ramipril: A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.. ramipril : A dipeptide that is the prodrug for ramiprilat, the active metabolite obtained by hydrolysis of the ethyl ester group. An angiotensin-converting enzyme (ACE) inhibitor, used to treat high blood pressure and congestive heart failure.. quark : Quarks comprise one of two classes of the fundamental particles. Quarks possess fractional electric charges and are not observed in free state. The word "quark" first appears in James Joyce's Finnegans Wake and has been chosen by Murray Gell-Mann as a name for fundamental building blocks of particles. | 3.23 | 1 | 0 | azabicycloalkane; cyclopentapyrrole; dicarboxylic acid monoester; dipeptide; ethyl ester | bradykinin receptor B2 agonist; cardioprotective agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; matrix metalloproteinase inhibitor; prodrug |
| verteporfin (2R,2(1)S)-8-ethenyl-2(1),2(2)-bis(methoxycarbonyl)-17-(3-methoxy-3-oxopropyl)-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13-propanoic acid : The 2(1),2(2),17-trimethyl ester of (2R,2(1)S)-2(1),2(2)-dicarboxy-8-ethenyl-2,7,12,18-tetramethyl-2,2(1)-dihydrobenzo[b]porphyrin-13,17-dipropanoic acid. | 3.23 | 1 | 0 | ||
| indinavir sulfate Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. | 3.23 | 1 | 0 | dicarboxylic acid diamide; N-(2-hydroxyethyl)piperazine; piperazinecarboxamide | HIV protease inhibitor |
| zimeldine Zimeldine: One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) | 3.23 | 1 | 0 | styrenes | |
| enalapril Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration). | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; geroprotector; prodrug |
| trientine hydrochloride [no description available] | 3.23 | 1 | 0 | ||
| n-methylscopolamine bromide scopolamine methobromide : A quaternary ammonium salt resulting from the reaction of the amino group of scopolamine with methyl bromide. | 3.23 | 1 | 0 | ||
| bleomycin [no description available] | 3.23 | 1 | 0 | bleomycin | antineoplastic agent; metabolite |
| enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate. | 3.23 | 1 | 0 | dicarboxylic acid; dipeptide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor |
| ximelagatran ximelagatran: prodrug (via hydroxylation) of melagatran & a direct thrombin inhibitor; liver toxicity concerns so AZD0837 being developed to replace this. ximelagatran : A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | 3.23 | 1 | 0 | amidoxime; azetidines; carboxamide; ethyl ester; hydroxylamines; secondary amino compound; secondary carboxamide; tertiary carboxamide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor; prodrug; serine protease inhibitor |
| cefuroxime [no description available] | 3.23 | 1 | 0 | 3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether | drug allergen |
| ceftriaxone [no description available] | 3.23 | 1 | 0 | 1,2,4-triazines; 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 3.5.2.6 (beta-lactamase) inhibitor |
| cefepime Cefepime: A fourth-generation cephalosporin antibacterial agent that is used in the treatment of infections, including those of the abdomen, urinary tract, respiratory tract, and skin. It is effective against PSEUDOMONAS AERUGINOSA and may also be used in the empiric treatment of FEBRILE NEUTROPENIA.. cefepime : A cephalosporin bearing (1-methylpyrrolidinium-1-yl)methyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug |
| pafuramidine pafuramidine: a prodrug of furamidine | 3.23 | 1 | 0 | ||
| ceftazidime [no description available] | 3.23 | 1 | 0 | cephalosporin; oxime O-ether | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| trandolapril trandolapril : A heterobicylic compound that is (2S,3aR,7aS)-1-[(2S)-2-aminopropanoyl]octahydro-1H-indole-2-carboxylic acid in which the hydrogen of the amino group is substituted by a (2R)-1-ethoxy-1-oxo-4-phenylbutan-2-yl group. It is a angiotensin-converting enzyme inhibitor and a prodrug used for the treatment of hypertension. | 3.23 | 1 | 0 | dicarboxylic acid monoester; dipeptide; ethyl ester; organic heterobicyclic compound; secondary amino compound; tertiary carboxamide | antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug |
| pregabalin Pregabalin: A gamma-aminobutyric acid (GABA) derivative that functions as a CALCIUM CHANNEL BLOCKER and is used as an ANTICONVULSANT as well as an ANTI-ANXIETY AGENT. It is also used as an ANALGESIC in the treatment of NEUROPATHIC PAIN and FIBROMYALGIA.. pregabalin : A gamma-amino acid that is gamma-aminobutyric acid (GABA) carrying an isobutyl substitutent at the beta-position (the S-enantiomer). Binds with high affinity to the alpha2-delta site (an auxiliary subunit of voltage-gated calcium channels) in central nervous system tissues. | 3.23 | 1 | 0 | gamma-amino acid | anticonvulsant; calcium channel blocker |
| alvimopan anhydrous alvimopan: mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain | 3.23 | 1 | 0 | peptide | |
| aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position. | 3.23 | 1 | 0 | monocarboxylic acid amide; monomethoxybenzene | antihypertensive agent |
| famotidine [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; guanidines; sulfonamide | anti-ulcer drug; H2-receptor antagonist; P450 inhibitor |
| cefotaxime Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups. | 3.23 | 1 | 0 | 1,3-thiazoles; cephalosporin; oxime O-ether | antibacterial drug; drug allergen |
| aztreonam [no description available] | 3.23 | 1 | 0 | beta-lactam antibiotic allergen; monobactam | antibacterial drug; drug allergen; EC 2.4.1.129 (peptidoglycan glycosyltransferase) inhibitor |
| cefpodoxime [no description available] | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| palonosetron Palonosetron: Isoquinoline and quinuclidine derivative that acts as a 5-HT3 RECEPTOR antagonist. It is used in the prevention of nausea and vomiting induced by cytotoxic chemotherapy, and for the prevention of post-operative nausea and vomiting.. palonosetron : An organic heterotricyclic compound that is an antiemetic used (as its hydrochloride salt) in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. | 3.23 | 1 | 0 | azabicycloalkane; delta-lactam; organic heterotricyclic compound | antiemetic; serotonergic antagonist |
| rifaximin [no description available] | 3.23 | 1 | 0 | acetate ester; cyclic ketal; lactam; macrocycle; organic heterohexacyclic compound; rifamycins; semisynthetic derivative | antimicrobial agent; gastrointestinal drug; orphan drug |
| everolimus [no description available] | 3.23 | 1 | 0 | cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol | anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor |
| ixabepilone [no description available] | 3.23 | 1 | 0 | 1,3-thiazoles; beta-hydroxy ketone; epoxide; lactam; macrocycle | antineoplastic agent; microtubule-destabilising agent |
| ceftizoxime [no description available] | 3.23 | 1 | 0 | cephalosporin | antibacterial drug |
| 1-methyl-d-lysergic acid butanolamide [no description available] | 3.23 | 1 | 0 | ergot alkaloid; monocarboxylic acid amide | serotonergic antagonist; sympatholytic agent; vasoconstrictor agent |
| nitrofurantoin Nitrofurantoin: A urinary anti-infective agent effective against most gram-positive and gram-negative organisms. Although sulfonamides and antibiotics are usually the agents of choice for urinary tract infections, nitrofurantoin is widely used for prophylaxis and long-term suppression.. nitrofurantoin : An imidazolidine-2,4-dione that is hydantoin substituted at position 1 by a [(5-nitro-2-furyl)methylene]amino group. An antibiotic that damages bacterial DNA. | 3.23 | 1 | 0 | imidazolidine-2,4-dione; nitrofuran antibiotic; organonitrogen heterocyclic antibiotic; organooxygen heterocyclic antibiotic | antibacterial drug; antiinfective agent; hepatotoxic agent |
| dantrolene [no description available] | 3.23 | 1 | 0 | ||
| cefdinir [no description available] | 3.23 | 1 | 0 | cephalosporin; ketoxime | antibacterial drug |
| etonogestrel [no description available] | 3.23 | 1 | 0 | 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; terminal acetylenic compound | contraceptive drug; female contraceptive drug; progestin |
| temsirolimus [no description available] | 3.23 | 1 | 0 | macrolide lactam | |
| dutasteride Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA.. dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| lu 208075 ambrisentan: an ET(A) receptor antagonist and antihypertensive agent; studied for use in pulmonary arterial hypertension | 3.23 | 1 | 0 | diarylmethane | |
| bibx 1382bs BIBX 1382BS: an ErbB receptor kinase inhibitor; no further information available 4/2001 | 3.23 | 1 | 0 | substituted aniline | |
| fesoterodine fesoterodine: a muscarinic antagonist for treatment of overactive bladder | 3.23 | 1 | 0 | diarylmethane | |
| gemifloxacin Gemifloxacin: A naphthyridine and fluoroquinolone derivative antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used for the treatment of community-acquired pneumonia and acute bacterial infections associated with chronic bronchitis.. gemifloxacin : A 1,4-dihydro-1,8-naphthyridine with a carboxy group at the 3-position, an oxo sustituent at the 4-position, a fluoro substituent at the 5-position and a substituted pyrrolin-1-yl group at the 7-position. | 3.23 | 1 | 0 | 1,8-naphthyridine derivative; fluoroquinolone antibiotic; monocarboxylic acid; quinolone antibiotic | antibacterial drug; antimicrobial agent; topoisomerase IV inhibitor |
| dexlansoprazole Dexlansoprazole: The R-isomer of lansoprazole that is used to treat severe GASTROESOPHAGEAL REFLUX DISEASE. | 3.23 | 1 | 0 | benzimidazoles; sulfoxide | |
| fosinopril [no description available] | 3.23 | 1 | 0 | ||
| armodafinil armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness. | 3.23 | 1 | 0 | 2-[(diphenylmethyl)sulfinyl]acetamide | central nervous system stimulant; eugeroic |
| sincalide Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas. | 3.23 | 1 | 0 | oligopeptide | |
| tapentadol Tapentadol: An opioid analgesic, MU OPIOID RECEPTOR agonist, and noradrenaline reuptake inhibitor that is used in the treatment of moderate to severe pain, and of pain associated with DIABETIC NEUROPATHIES. | 3.23 | 1 | 0 | alkylbenzene | |
| pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. | 3.23 | 1 | 0 | organic molecular entity | |
| cefditoren cefditoren: structure given in first source; RN given refers to the (6R-(3(Z),6alpha,7beta(Z)))-isomer. cefditoren : A broad spectrum, third-generation cephalosporin antibiotic with (Z)-2-(4-methyl-1,3-thiazol-5-yl)ethenyl and (2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido groups at positions 3 and 7, respectively, of the cephem skeleton. Generally administered as its orally absorbed pivaloyloxymethyl ester prodrug, it is used for the treatment of mild to moderate infections caused by susceptible strains of microorganisms in acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia, pharyngitis/tonsillitis, and uncomplicated skin and skin-structure infections. | 3.23 | 1 | 0 | carboxylic acid; cephalosporin | antibacterial drug |
| pazopanib pazopanib: a protein kinase inhibitor. pazopanib : A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer. | 3.23 | 1 | 0 | aminopyrimidine; indazoles; sulfonamide | angiogenesis modulating agent; antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist |
| prasugrel hydrochloride Prasugrel Hydrochloride: A piperazine derivative and PLATELET AGGREGATION INHIBITOR that is used to prevent THROMBOSIS in patients with ACUTE CORONARY SYNDROME; UNSTABLE ANGINA and MYOCARDIAL INFARCTION, as well as in those undergoing PERCUTANEOUS CORONARY INTERVENTIONS.. prasugrel hydrochloride : A racemate comprising equal amounts of (R)- and (S)-prasugrel hydrochloride. Used to prevent blood clots in people with acute coronary syndrome who are undergoing a procedure after a recent heart attack or stroke, and in people with certain disorders of the heart or blood vessels. | 3.23 | 1 | 0 | ||
| baci-im [no description available] | 3.23 | 1 | 0 | homodetic cyclic peptide; polypeptide; zwitterion | antibacterial agent; antimicrobial agent |
| bms 477118 [no description available] | 3.23 | 1 | 0 | adamantanes; azabicycloalkane; monocarboxylic acid amide; nitrile; tertiary alcohol | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; hypoglycemic agent |
| nystatin a1 Nystatin: Macrolide antifungal antibiotic complex produced by Streptomyces noursei, S. aureus, and other Streptomyces species. The biologically active components of the complex are nystatin A1, A2, and A3.. nystatin : A heterogeneous mixture of polyene compounds produced by cultures of Streptomyces noursei. It mainly consists of three biologically active components designated nystatin A1, nystatin A2, and nystatin A3. It is used to treat oral and dermal fungal infections.. nystatin A1 : A polyene macrolide antibiotic; part of the nystatin complex produced by several Streptomyces species. It is an antifungal antibiotic used for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species. | 3.23 | 1 | 0 | nystatins | |
| milnacipran [no description available] | 3.23 | 1 | 0 | acetamides | |
| scopolamine hydrobromide [no description available] | 3.23 | 1 | 0 | ||
| bivalirudin bivalirudin: designed to bind to the alpha-thrombin catalytic site and anion-binding exosite for fibrin(ogen) recognition. bivalirudin : A synthetic peptide of 20 amino acids, comprising D-Phe, Pro, Arg, Pro, Gly, Gly, Gly, Gly, Asn, Gly, Asp, Phe, Glu, Glu, Ile, Pro, Glu, Glu, Tyr, and Leu in sequence. A congener of hirudin (a naturally occurring drug found in the saliva of the medicinal leech), it a specific and reversible inhibitor of thrombin, and is used as an anticoagulant. | 3.23 | 1 | 0 | polypeptide | anticoagulant; EC 3.4.21.5 (thrombin) inhibitor |
| somatostatin [no description available] | 2.93 | 3 | 0 | heterodetic cyclic peptide; peptide hormone | |
| enfuvirtide Enfuvirtide: A synthetic 36-amino acid peptide that corresponds to the heptad repeat sequence of HIV-1 gp41. It blocks HIV cell fusion and viral entry and is used with other anti-retrovirals for combination therapy of HIV INFECTIONS and AIDS.. enfuvirtide : A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutaminyl, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryptophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes. | 3.23 | 1 | 0 | ||
| ganirelix [no description available] | 3.23 | 1 | 0 | polypeptide | |
| teriparatide [no description available] | 3.23 | 1 | 0 | polypeptide | |
| salmon calcitonin [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; peptide hormone; polypeptide | bone density conservation agent; metabolite |
| ly-146032 [no description available] | 3.23 | 1 | 0 | heterodetic cyclic peptide; lipopeptide antibiotic; lipopeptide; macrocycle; macrolide | antibacterial drug; bacterial metabolite; calcium-dependent antibiotics |
| acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ilys-prolyl-alaninamide acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide: FE-200486 is the acetate salt | 3.23 | 1 | 0 | polypeptide | |
| exenatide [no description available] | 3.23 | 1 | 0 | ||
| carbetocin carbetocin : Oxytocin in which the hydrogen on the phenolic hydroxy group is substituted by methyl, the amino group on the cysteine residue is substituted by hydrogen, and the sulfur of the cysteine residue is replaced by a methylene group. A synthetic carba-analogue of oxytocin, it is used to control bleeding after giving birth. Like oxytocin, it causes contraction of the uterus. | 2.41 | 1 | 0 | heterodetic cyclic peptide | oxytocic |
| mesna Mesna: A sulfhydryl compound used to prevent urothelial toxicity by inactivating metabolites from ANTINEOPLASTIC AGENTS, such as IFOSFAMIDE or CYCLOPHOSPHAMIDE. | 3.23 | 1 | 0 | organosulfonic acid | |
| sodium lactate Sodium Lactate: The sodium salt of racemic or inactive lactic acid. It is a hygroscopic agent used intravenously as a systemic and urinary alkalizer.. sodium lactate : An organic sodium salt having lactate as the counterion. | 3.23 | 1 | 0 | lactate salt; organic sodium salt | food acidity regulator; food preservative |
| sodium iothalamate [no description available] | 3.23 | 1 | 0 | ||
| cetrorelix cetrorelix: LHRH antagonist. cetrorelix : A synthetic ten-membered oligopeptide comprising N-acetyl-3-(naphthalen-2-yl)-D-alanyl, 4-chloro-D-phenylalanyl, 3-(pyridin-3-yl)-D-alanyl, L-seryl, L-tyrosyl, N(5)-carbamoyl-D-ornithyl, L-leucyl, L-arginyl, L-prolyl, and D-alaninamide residues coupled in sequence. A gonadotrophin-releasing hormone (GnRH) antagonist, it is used for treatment of infertility and of hormone-sensitive cancers of the prostate and breast. | 3.23 | 1 | 0 | oligopeptide | antineoplastic agent; GnRH antagonist |
| ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms. | 3.23 | 1 | 0 | ascorbic acid; vitamin C | coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent |
| raltegravir [no description available] | 3.23 | 1 | 0 | 1,2,4-oxadiazole; dicarboxylic acid amide; hydroxypyrimidine; monofluorobenzenes; pyrimidone; secondary carboxamide | antiviral drug; HIV-1 integrase inhibitor |
| tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria. | 3.23 | 1 | 0 | ||
| oxytetracycline, anhydrous Oxytetracycline: A TETRACYCLINE analog isolated from the actinomycete STREPTOMYCES RIMOSUS and used in a wide variety of clinical conditions.. oxytetracycline : A tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae. | 3.23 | 1 | 0 | ||
| minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5. | 3.23 | 1 | 0 | ||
| piroxicam [no description available] | 3.23 | 1 | 0 | benzothiazine; monocarboxylic acid amide; pyridines | analgesic; antirheumatic drug; cyclooxygenase 1 inhibitor; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-steroidal anti-inflammatory drug |
| mobic Meloxicam: A benzothiazine and thiazole derivative that acts as a NSAID and cyclooxygenase-2 (COX-2) inhibitor. It is used in the treatment of RHEUMATOID ARTHRITIS; OSTEOARTHRITIS; and ANKYLOSING SPONDYLITIS.. meloxicam : A benzothiazine that is piroxicam in which the pyridin-2-yl group is replaced by a 5-methyl-1,3-thiazol-2-yl group. A non-steroidal anti-inflammatory drug and selective inhibitor of COX-2, it is used particularly for the management of rheumatoid arthritis. | 3.23 | 1 | 0 | 1,3-thiazoles; benzothiazine; monocarboxylic acid amide | analgesic; antirheumatic drug; cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug |
| warfarin Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group. | 3.23 | 1 | 0 | benzenes; hydroxycoumarin; methyl ketone | |
| demeclocycline Demeclocycline: A TETRACYCLINE analog having a 7-chloro and a 6-methyl. Because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.. demeclocycline : Tetracycline which lacks the methyl substituent at position 7 and in which the hydrogen para- to the phenolic hydroxy group is substituted by chlorine. Like tetracycline, it is an antibiotic, but being excreted more slowly, effective blood levels are maintained for longer. It is used (mainly as the hydrochloride) for the treatment of Lyme disease, acne and bronchitis, as well as for hyponatraemia (low blood sodium concentration) due to the syndrome of inappropriate antidiuretic hormone (SIADH) where fluid restriction alone has been ineffective. | 3.23 | 1 | 0 | ||
| tipranavir tipranavir: inhibits HIV-1 protease. tipranavir : A pyridine-2-sulfonamide substituted at C-5 by a trifluoromethyl group and at the sulfonamide nitrogen by a dihydropyrone-containing m-tolyl substituent. It is an HIV-1 protease inhibitor. | 3.23 | 1 | 0 | sulfonamide | antiviral drug; HIV protease inhibitor |
| tigecycline [no description available] | 3.23 | 1 | 0 | ||
| plecanatide plecanatide: A uroguanylin analog and guanylate cyclase (GC-C receptor) agonist that activates receptors on gut epithelial cells to maintain barrier function, mucus production, and suppress inflammation. It is used in the treatment of chronic idiopathic constipation and other gastrointestinal disorders. | 2.41 | 1 | 0 | ||
| fertinex [no description available] | 3.23 | 1 | 0 | ||
| entecavir entecavir (anhydrous) : Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus. Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it has no activity against HIV. It is used for the treatment of chronic hepatitis B. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine; primary alcohol; secondary alcohol | antiviral drug; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor |
| acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections. | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antimetabolite; antiviral drug |
| folic acid folcysteine: used to promote fertility in chickens. vitamin B9 : Any B-vitamin that exhibits biological activity against vitamin B9 deficiency. Vitamin B9 refers to the many forms of folic acid and its derivatives, including tetrahydrofolic acid (the active form), methyltetrahydrofolate (the primary form found in blood), methenyltetrahydrofolate, folinic acid amongst others. They are present in abundance in green leafy vegetables, citrus fruits, and animal products. Lack of vitamin B9 leads to anemia, a condition in which the body cannot produce sufficient number of red blood cells. Symptoms of vitamin B9 deficiency include fatigue, muscle weakness, and pale skin. | 3.23 | 1 | 0 | folic acids; N-acyl-amino acid | human metabolite; mouse metabolite; nutrient |
| rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) | 3.23 | 1 | 0 | cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion | angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor |
| clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound | adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic |
| dacarbazine (E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration. | 3.23 | 1 | 0 | dacarbazine | |
| didanosine Didanosine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite.. didanosine : A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen. An antiviral drug, it is used as a medication to treat HIV/AIDS. | 3.23 | 1 | 0 | purine 2',3'-dideoxyribonucleoside | antimetabolite; antiviral drug; EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor; geroprotector; HIV-1 reverse transcriptase inhibitor |
| ganciclovir [no description available] | 3.23 | 1 | 0 | 2-aminopurines; oxopurine | antiinfective agent; antiviral drug |
| valacyclovir Valacyclovir: A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. | 3.23 | 1 | 0 | L-valyl ester | antiviral drug |
| sildenafil sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | 3.23 | 1 | 0 | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4. | 3.23 | 1 | 0 | benzodiazepine; N-arylpiperazine; N-methylpiperazine | antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor |
| vardenafil vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | 3.23 | 1 | 0 | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| allopurinol Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring. | 3.23 | 1 | 0 | nucleobase analogue; organic heterobicyclic compound | antimetabolite; EC 1.17.3.2 (xanthine oxidase) inhibitor; gout suppressant; radical scavenger |
| citrovorum factor [no description available] | 3.23 | 1 | 0 | tetrahydrofolic acid | |
| leucovorin 5-formyltetrahydrofolic acid : A formyltetrahydrofolic acid in which the formyl group is located at position 5. | 3.23 | 1 | 0 | formyltetrahydrofolic acid | Escherichia coli metabolite; mouse metabolite |
| rifapentine rifapentine: cyclopentyl derivative of rifampicin | 3.23 | 1 | 0 | N-alkylpiperazine; N-iminopiperazine; rifamycins | antitubercular agent; leprostatic drug |
| bl 4162a anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source. anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions. | 3.23 | 1 | 0 | imidazoquinazoline | anticoagulant; antifibrinolytic drug; cardiovascular drug; platelet aggregation inhibitor |
| tegaserod tegaserod: a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source | 3.23 | 1 | 0 | carboxamidine; guanidines; hydrazines; indoles | gastrointestinal drug; serotonergic agonist |
| pemetrexed pemetrexed disodium : An organic sodium salt that is the disodium salt of N-{4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid. Inhibits thymidylate synthase (TS), 421 dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). | 3.23 | 1 | 0 | N-acyl-L-glutamic acid; pyrrolopyrimidine | antimetabolite; antineoplastic agent; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; EC 2.1.1.45 (thymidylate synthase) inhibitor; EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor |
| valganciclovir Valganciclovir: A ganciclovir prodrug and antiviral agent that is used to treat CYTOMEGALOVIRUS RETINITIS in patients with AIDS, and for the prevention of CYTOMEGALOVIRUS INFECTIONS in organ transplant recipients who have received an organ from a CMV-positive donor.. valganciclovir : The L-valinyl ester of ganciclovir, into which it is rapidly converted by intestinal and hepatic esterases. It is a synthetic analogue of 2'-deoxyguanosine. | 3.23 | 1 | 0 | L-valyl ester; purines | antiviral drug; prodrug |
| aprepitant Aprepitant: A morpholine neurokinin-1 (NK1) receptor antagonist that is used in the management of nausea and vomiting caused by DRUG THERAPY, and for the prevention of POSTOPERATIVE NAUSEA AND VOMITING.. aprepitant : A morpholine-based antiemetic, which is or the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; triazoles | antidepressant; antiemetic; neurokinin-1 receptor antagonist; peripheral nervous system drug; substance P receptor antagonist |
| fosaprepitant fosaprepitant: a pro-drug form of aprepitant. fosaprepitant : A morpholine derivative that is the (1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl ether of (3-{[(2R,3S)-3-(4-fluorophenyl)-2-hydroxymorpholin-4-yl]methyl}-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid. | 3.23 | 1 | 0 | (trifluoromethyl)benzenes; cyclic acetal; morpholines; phosphoramide; triazoles | antiemetic; neurokinin-1 receptor antagonist; prodrug |
| rifabutin [no description available] | 3.23 | 1 | 0 | ||
| levomefolate calcium levomefolate calcium: an ingredient in Contraceptives, Oral, Combined. levomefolate calcium : An organic calcium salt of (6S)-5-methyltetrahydrofolic acid. | 3.23 | 1 | 0 | organic calcium salt | antidepressant |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Acute Liver Injury, Drug-Induced [description not available] | 0 | 3.04 | 1 | 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 | 3.04 | 1 | 0 |
| Cancer of Pancreas [description not available] | 0 | 2.17 | 1 | 0 |
| Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA). | 1 | 4.17 | 1 | 0 |