tepotinib
Trade name: Tepmetko
Small moleculeapprovedOrphan Drug FDA
Approved
Feb 3, 2021
c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor of hepatocyte growth factor/scatter factor (HGF/SF). These inhibitors may have therapeutic application in the treatment of various types of cancers. — Wikipedia
Clinical trial activity
25 trials · 13 clinical orgs · 1 marketing orgs
Phase 1
19
Phase 2
12
Phase 3
0
Phase 4
0
Earliest trial started Nov 1, 2009 (NCT01014936)
Timeline
2000s
- Jan 1, 2009
Merck Serono — Earliest Phase 1 Sponsor(trial)
2010s
- Jan 1, 2016
Merck Serono — Earliest Phase 2 Sponsor(trial)
2020s
- Oct 26, 2020
Orphan Drug Designation
- Feb 3, 2021
Merck Serono — Earliest FDA Approval
- Feb 3, 2021
Merck Serono — Marketing Organization
- Feb 3, 2021
Merck Serono — NDA Secondary Org
- Feb 3, 2021
Merck Serono — NDA Organization
Indications
Approved for
Studied for
- Brain Neoplasms · Phase 1
- Carcinoma, Hepatocellular · Phase 1/Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Colorectal Neoplasms · Phase 2
- Esophageal Neoplasms · Phase 1/Phase 2
- Healthy Volunteers · Phase 1
- Liver Diseases · Phase 1
- Lung Neoplasms · Phase 2
- Mutation · Phase 2
- Neoplasms · Phase 2
- Proto-Oncogene Proteins c-met · Phase 2
- Stomach Neoplasms · Phase 1/Phase 2
Mechanism of action
- Hepatocyte growth factor receptorINHIBITOR
MET inhibitor
Approval history
- approvedPriority reviewAcceleratedFeb 3, 2021
Chemistry & pharmacology
Loading structure…
SMILES
CN1CCC(COc2cnc(-c3cccc(Cn4nc(-c5cccc(C#N)c5)ccc4=O)c3)nc2)CC1- Mol. weight
- 492.58 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaC-Met inhibitor ↗
- ChEMBLCHEMBL4594292 ↗
- ChEMBLCHEMBL3402762 ↗
Also known as
- emd-1214063
- emd-1214063
- msc-2156119
- msc-2156119
- msc2156119j
- msc2156119j
- msc-2156119j
- msc-2156119j
- tepotinib
- tepotinib
- tepotinib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06083857 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2024 | University of Texas at Houston |
| NCT06106802 | Phase 2 | Feb 2, 2024 | Sungkyunkwan University |
| NCT06031688 | Phase 2 | Jan 6, 2024 | National Cancer Institute (NCI), SWOG Cancer Research Network |
| NCT05782361 | Phase 1 | May 3, 2023 | Merck, Merck Serono, Royal Marsden Hospital NHS Trust, University of London |
| NCT05120960 | Phase 1 | Apr 30, 2022 | University of Texas at Houston |
| NCT05439993 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2022 | Hallym University |
| NCT05203822 | Phase 1 | Jan 21, 2022 | Merck KGaA |
| NCT05213481 | Phase 1 | Dec 15, 2021 | Merck KGaA |
| NCT04739358 | Phase 1/Phase 2 (Phase 2) | Jul 2, 2021 | Criterium, Inc., Merck Serono, University of Colorado, Denver |
| NCT04515394 | Phase 2 | Jan 21, 2021 | Merck KGaA, Merck Serono |
| NCT04647838 | Phase 2 | Jan 16, 2020 | Chonbuk National University, Merck KGaA |
| NCT04204902 | Phase 1 | Oct 17, 2019 | Merck KGaA |
| NCT03940703 | Phase 2 | Jul 18, 2019 | Merck KGaA, Merck Serono |
| NCT03629223 | Phase 1 | Aug 28, 2018 | Merck KGaA |
| NCT03628339 | Phase 1 | Aug 20, 2018 | Merck KGaA |
| NCT03546608 | Phase 1 | Jun 13, 2018 | Merck KGaA, Merck Serono |
| NCT03492437 | Phase 1 | May 17, 2018 | Merck KGaA |
| NCT03531762 | Phase 1 | May 14, 2018 | Merck KGaA |
| NCT02864992 | Phase 2 | Sep 13, 2016 | Merck KGaA, Merck Serono |
| NCT03021642 | Phase 1 | Jan 1, 2016 | Merck KGaA |
Showing 20 of 25 trials
Page 1 / 2
Organizations
Research & Development (13)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Merck KGaA | For profit | 18 | 12 | 2 | 2009 |
| Merck Serono | For profit | 8 | 5 | 2 | 2009 |
| University of Texas at Houston | Academic/Hospital | 2 | 2 | 2 | 2022 |
| Chonbuk National University | Academic/Hospital | 1 | 1 | 1 | 2020 |
| Criterium, Inc. | For profit | 1 | 1 | 1 | 2021 |
| Hallym University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Merck | For profit | 1 | 0 | 1 | 2023 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2024 |
| Royal Marsden Hospital NHS Trust | Academic/Hospital | 1 | 0 | 1 | 2023 |
| Sungkyunkwan University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| SWOG Cancer Research Network | Academic/Hospital | 1 | 1 | 1 | 2024 |
| University of Colorado, Denver | Academic/Hospital | 1 | 0 | 1 | 2021 |
| University of London | Academic/Hospital | 1 | 1 | 1 | 2023 |
13 organizations
Page 1 / 1
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Merck Serono | For profit | MKTG | Feb 3, 2021 |
| Merck Serono | For profit | NDA2 | Feb 3, 2021 |
| Merck Serono | For profit | NDA | Feb 3, 2021 |