varespladib methyl : A methyl ester resulting from the formal condensation of the carboxy group of varespladib with methanol. It is a potential therapy for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 9886917 |
| CHEMBL ID | 2105659 |
| CHEBI ID | 192805 |
| SCHEMBL ID | 25678 |
| MeSH ID | M0541152 |
| Synonym |
|---|
| D08221 |
| varespladib methyl (usan) |
| 172733-08-3 |
| CHEBI:192805 |
| s 3013 |
| a-002 , |
| varespladib methyl |
| ly 333013 |
| methyl-varespladib |
| ly333013 |
| methyl varespladib |
| varespladib-methyl |
| s-3013 |
| methyl ({3-[amino(oxo)acetyl]-1-benzyl-2-ethyl-1h-indol-4-yl}oxy)acetate |
| varespladib methyl ester |
| ly-333013 |
| methyl ((3-(aminooxoacetyl)-1-benzyl-2-ethyl-1h-indol-4-yl)oxy)acetate |
| unii-0nb98nbx3d |
| varespladib methyl [usan] |
| acetic acid, ((3-(aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1h-indol-4-yl)oxy)-, methyl ester |
| methyl ((3-(aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1h-indol-4-yl)oxy)acetate |
| 0nb98nbx3d , |
| CHEMBL2105659 |
| varespladib methyl ester [mi] |
| SCHEMBL25678 |
| CS-6574 |
| HY-17448 |
| NCGC00387871-03 |
| DB05737 |
| methyl 2-((3-(2-amino-2-oxoacetyl)-1-benzyl-2-ethyl-1h-indol-4-yl)oxy)acetate |
| DTXSID40938196 |
| AS-16898 |
| Q7915615 |
| SB16537 |
| AKOS037643560 |
| methyl 2-(1-benzyl-2-ethyl-3-oxamoylindol-4-yl)oxyacetate |
| XGA73308 |
Varespladib methyl is an oral secretory phospholipase A2 inhibitor. It is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Varespladib methyl is an oral secretory phospholipase A2 inhibitor that is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. " | ( Varespladib methyl, an oral phospholipase A2 inhibitor for the potential treatment of coronary artery disease. Karakas, M; Koenig, W, 2009) | 3.24 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Varespladib methyl treatment resulted in statistically significant dose-dependent reductions that were different from placebo in sPLA(2) concentration, low-density lipoprotein (LDL) cholesterol, and non-high-density lipoprotein (HDL) cholesterol." | ( Randomized trial of an inhibitor of secretory phospholipase A2 on atherogenic lipoprotein subclasses in statin-treated patients with coronary heart disease. Elliott, M; Hislop, C; Rosenson, RS; Stasiv, Y, 2011) | 1.09 |
| Role | Description |
|---|---|
| prodrug | A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. |
| anti-inflammatory drug | A substance that reduces or suppresses inflammation. |
| antidote | Any protective agent counteracting or neutralizing the action of poisons. |
| EC 3.1.1.4 (phospholipase A2) inhibitor | An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of phospholipase A2 (EC 3.1.1.4). |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| methyl ester | Any carboxylic ester resulting from the formal condensation of a carboxy group with methanol. |
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| benzenes | Any benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives. |
| indoles | Any compound containing an indole skeleton. |
| primary carboxamide | A carboxamide resulting from the formal condensation of a carboxylic acid with ammonia; formula RC(=O)NH2. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 13.4504 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 13.4504 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 1 (4.55) | 29.6817 |
| 2010's | 16 (72.73) | 24.3611 |
| 2020's | 5 (22.73) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (23.65) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (18.18%) | 5.53% |
| Reviews | 4 (18.18%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (63.64%) | 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 | ||
|---|---|---|---|---|---|---|---|
| VISTA-16 Trial: Evaluation of the Safety and Efficacy of Short-Term A-002 Treatment in Subjects With Acute Coronary Syndromes [NCT01130246] | Phase 3 | 5,189 participants (Actual) | Interventional | 2010-05-31 | Terminated(stopped due to Lack of efficacy) | ||
| A Phase 1, Open-label, Pharmacokinetic, Safety, and Tolerability Study of a Single Oral Dose of Varespladib Methyl in Subjects With Normal Renal Function, and Subjects With Mild, Moderate, or Severe Renal Impairment [NCT01359579] | Phase 1 | 28 participants (Actual) | Interventional | 2011-06-30 | Terminated(stopped due to Lack of efficacy) | ||
| An Open-Label, Single-Dose, Study to Assess the Metabolism and Elimination of Varespladib After Oral Administration of [14C]-Labeled Varespladib Methyl in Healthy Male Subjects [NCT01359605] | Phase 1 | 6 participants (Actual) | Interventional | 2011-06-30 | Completed | ||
| FRANCIS-ACS Trial: A Study of the Safety and Efficacy of A 002 in Subjects With Acute Coronary Syndromes [NCT00743925] | Phase 2 | 625 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| A Randomized, Double-blind, Placebo-Controlled Study With Varespladib Infusion (A-001) in Subjects With Sickle Cell Disease and Vaso-Occlusive Crisis for the Prevention of Acute Chest Syndrome At-Risk Subjects. [NCT01522196] | Phase 2 | 2 participants (Actual) | Interventional | 2012-02-29 | Terminated(stopped due to change in company plans) | ||
| A Randomized, Placebo/Active Controlled, Single/Multiple Dosing, Dose Escalation Clinical Phase 1a/b Trial to Evaluate the Safety, Tolerability and Pharmacokinetic Properties of IN-A002 Ointment in Healthy Adult Male Volunteers and Mild to Moderate Atopic [NCT05729074] | Phase 1 | 80 participants (Anticipated) | Interventional | 2023-02-13 | Not yet recruiting | ||
| A Phase 2, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, and Efficacy of Varespladib in Patients Hospitalized With Severe COVID 19 Caused by SARS-CoV-2 [NCT04969991] | Phase 2 | 18 participants (Actual) | Interventional | 2021-06-30 | Terminated(stopped due to Part 2 of the study was paused on 03-May-2022 due to slow enrollment following low infection rates and hospitalizations of patients with severe COVID-19, and did not recommence prior to study closure (early termination) on 22-Nov-2022.) | ||
| sPLA2 Inhibition to Decrease Enzyme Release After PCI (SPIDER-PCI) Trial [NCT00533039] | Phase 2 | 164 participants (Anticipated) | Interventional | 2007-10-31 | Completed | ||
| Randomized, Double-Blinded, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Efficacy of a Multi-Dose Regimen of Oral Varespladib-Methyl in Subjects Bitten by Venomous Snakes [NCT04996264] | Phase 2 | 96 participants (Actual) | Interventional | 2021-08-15 | Completed | ||
| A Randomized, Open-label, Single-dose, 2-way Crossover Clinical Trial to Investigate the Effect of Food on the Pharmacokinetics of IN-A002 Capsule in Healthy Male Subjects [NCT05019755] | Phase 1 | 12 participants (Anticipated) | Interventional | 2021-08-13 | Recruiting | ||
| Randomized, Double-Blinded, Placebo-Controlled Study to Evaluate the Safety, Tolerability, and Efficacy of Intravenous Varespladib Followed by Oral Varespladib in Addition to Standard of Care in Subjects Bitten by Venomous Snakes [NCT05717062] | Phase 2 | 140 participants (Anticipated) | Interventional | 2023-05-30 | Recruiting | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||