tivantinib
Small moleculeexperimental
Tivantinib is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase in vitro. Tivantinib is being tested clinically as a highly selective MET inhibitor. However, the mechanism of action of tivantinib is still unclear. — Wikipedia
Clinical trial activity
111 trials · 75 clinical orgs · 0 marketing orgs
Phase 1
30
Phase 2
66
Phase 3
33
Phase 4
12
Earliest trial started Jul 1, 2001 (NCT00192153)
Timeline
Indications
Approved for
Studied for
- Arthritis, Rheumatoid · Phase 4
- Asthma · Phase 3
- Breast Neoplasms · Phase 2
- Carcinoma, Hepatocellular · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Carcinoma, Renal Cell · Phase 2
- Carcinoma, Small Cell · Phase 2
- Colorectal Neoplasms · Phase 2
- Dengue · Phase 2
- Dengue Virus · Phase 2
- Esophageal Neoplasms · Phase 1/Phase 2
- Fever · Phase 3
- Fibrosis · Phase 1
- Healthy Volunteers · Phase 4
- Influenza A Virus, H5N1 Subtype · Phase 3
- Influenza, Human · Phase 4
- Influenza in Birds · Phase 3
- Influenza Vaccines · Phase 3
- Liver Diseases · Phase 1
- Liver Neoplasms · Phase 3
- Mesothelioma · Phase 2
- Mesothelioma, Malignant · Phase 1/Phase 2
- Multiple Myeloma · Phase 2
- Neoplasms · Phase 1/Phase 2
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Orthomyxoviridae · Phase 3
- Pancreatic Neoplasms · Phase 2
- Pandemics · Phase 2
- Pneumococcal Infections · Phase 4
- Prostatic Neoplasms · Phase 2
- Proto-Oncogene Proteins c-met · Phase 2
- Respiratory Syncytial Virus Infections · Phase 1
- Respiratory Tract Infections · Phase 3
- Sarcoma · Phase 2
- Sarcoma, Clear Cell · Phase 2
- Severe Dengue · Phase 2
- Small Cell Lung Carcinoma · Phase 1/Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
- Vaccines · Phase 4
Mechanism of action
- Hepatocyte growth factor receptorINHIBITOR
MET inhibitor
Mechanism of action is still unclear, it is thought that Tivantinib displays cytotoxic activity via mechanisms other than only cMET inhibition (PMID:23712183)
Chemistry & pharmacology
Loading structure…
SMILES
O=C1NC(=O)[C@@H]([C@H]1C2=CNC3=C2C=CC=C3)C4=CN5CCCC6=CC=CC4=C56- Mol. weight
- 369.4159 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTivantinib ↗
- NCATSE9UU0ESM69 ↗
- ChEMBLCHEMBL2103882 ↗
Also known as
- arq197
- arq197
- arq197
- arq 197
- arq 197
- arq 197
- arq-197
- arq-197
- arq-197
- tiv
- tiv
- tivantinib
- tivantinib
- tivantinib
- tivantinib
- tivantinib
- tivantinib (arq 197)
- (-)-trans-3-(5,6-dihydro-4h-pyrrolo(3,2,1-ij)quinolin-1-yl)-4-(1h-indol-3-yl)pyrrolidin-2,5-dione
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03144518 | N/A | Aug 1, 2017 | Northumbria University, University of Nottingham |
| NCT02936180 | Phase 4 | Oct 1, 2016 | McGill University, The Arthritis Society, Canada |
| NCT02806804 | Phase 3 | May 1, 2016 | Capital Medical University |
| NCT02665871 | Phase 1 | Mar 1, 2016 | Capital Medical University |
| NCT02608411 | Phase 2 | Oct 1, 2015 | Istituto Oncologico Veneto IRCCS |
| NCT02529904 | Phase 2 | Aug 1, 2015 | Emory University, University of Oxford, VisMederi srl |
| NCT02293317 | Phase 2 | Nov 1, 2014 | BiondVax Pharmaceuticals |
| NCT02307851 | Phase 2 | Nov 1, 2014 | Department of Health and Human Services, Novavax |
| NCT02255279 | Phase 3 | Oct 1, 2014 | Novartis |
| NCT02256488 | Phase 3 | Sep 1, 2014 | Novartis |
| NCT02213432 | N/A | Sep 1, 2014 | Green Cross Corporation, Seoul National University |
| NCT02228980 | Phase 4 | Sep 1, 2014 | Sanofi, Sanofi-Aventis |
| NCT02229357 | Phase 2 | Jun 1, 2014 | Mahidol University, The Government Pharmaceutical Organization, World Health Organization |
| NCT02153671 | Phase 2 | May 1, 2014 | Government of Russia, PATH, Russian Institute of Influenza |
| NCT02150733 | Phase 1 | Apr 1, 2014 | Daiichi Sankyo, Medpace, Inc. |
| NCT02091908 | Phase 3 | Apr 1, 2014 | CSL Behring, Novartis |
| NCT02107807 | Phase 3 | Apr 1, 2014 | CSL Behring, Novartis |
| NCT02029157 | Phase 3 | Jan 1, 2014 | Kyowa Hakko Kirin |
| NCT02062281 | Phase 4 | Nov 1, 2013 | Chengdu Institute of Biological Products Co.,Ltd., China National Biotec Group Co., Ltd, Government of China |
| NCT01992107 | Phase 3 | Nov 1, 2013 | Novartis |
Showing 20 of 111 trials
Page 1 / 6
Organizations
Research & Development (75)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Novartis | For profit | 25 | 22 | 3 | 2004 |
| ArQule | For profit | 18 | 15 | 3 | 2006 |
| National Cancer Institute (NCI) | Government | 11 | 11 | 2 | 2011 |
| Daiichi Sankyo | For profit | 9 | 8 | 3 | 2010 |
| Kyowa Hakko Kirin | For profit | 8 | 8 | 3 | 2008 |
| CSL Behring | For profit | 6 | 6 | 2 | 2008 |
| MedImmune | For profit | 4 | 4 | 2 | 2001 |
| BiondVax Pharmaceuticals | For profit | 3 | 3 | 1 | 2010 |
| Covance | For profit | 3 | 0 | 2 | 2008 |
| Medpace, Inc. | For profit | 3 | 0 | 1 | 2011 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 3 | 1 | 2 | 2011 |
| Novavax | For profit | 3 | 3 | 2 | 2012 |
| Ology Bioservices | For profit | 3 | 3 | 1 | 2003 |
| University of Oxford | Academic/Hospital | 3 | 3 | 2 | 2011 |
| Wyeth | For profit | 3 | 0 | 2 | 2001 |
| Astellas | For profit | 2 | 2 | 1 | 2012 |
| Capital Medical University | Academic/Hospital | 2 | 2 | 2 | 2016 |
| Department of Health and Human Services | Government | 2 | 0 | 1 | 2012 |
| Hebrew University | Academic/Hospital | 2 | 1 | 2 | 2008 |
| Humanitas University | Academic/Hospital | 2 | 2 | 1 | 2013 |
75 organizations
Page 1 / 4