merestinib
Small moleculeexperimental
Merestinib (LY2801653) is an experimental cancer drug in development by Eli Lilly. It is a small molecule inhibitor of MET and several other receptor tyrosine kinases such as MST1R, FLT3, AXL, MERTK, TEK, ROS1, NTRK1/2/3, and DDR1/2. — Wikipedia
Clinical trial activity
11 trials · 3 clinical orgs · 0 marketing orgs
Phase 1
9
Phase 2
2
Phase 3
0
Phase 4
0
Earliest trial started Sep 9, 2009 (NCT01285037)
Timeline
Indications
Studied for
- Biliary Tract Neoplasms · Phase 2
- Breast Neoplasms · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Cholangiocarcinoma · Phase 1
- Colorectal Neoplasms · Phase 1
- Healthy Volunteers · Phase 1
- Leukemia, Myeloid, Acute · Phase 1
- Lymphoma, Mantle-Cell · Phase 1
- Lymphoma, Non-Hodgkin · Phase 1
- Melanoma · Phase 1
- Neoplasm Metastasis · Phase 1
- Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 1
- Urinary Bladder Neoplasms · Phase 1
Mechanism of action
- Hepatocyte growth factor receptorINHIBITOR
MET inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cc1ccc(C(=O)Nc2ccc(Oc3cc4cnn(C)c4cc3-c3cn[nH]c3)c(F)c2)c(=O)n1-c1ccc(F)cc1- Mol. weight
- 552.54 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaMerestinib ↗
- ChEMBLCHEMBL3545307 ↗
Also known as
- ly2801653
- ly2801653
- ly2801653
- ly-2801653
- ly-2801653
- merestinib
- merestinib
- merestinib
- merestinib
- n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03292536 | Phase 1 | Jan 11, 2018 | Eli Lilly, University of Utah |
| NCT03125239 | Phase 1 | May 1, 2017 | Eli Lilly, Harvard University |
| NCT03027284 | Phase 1 | Feb 3, 2017 | Eli Lilly |
| NCT02920996 | Phase 2 | Nov 1, 2016 | Eli Lilly, Harvard University |
| NCT02745769 | Phase 1 | Oct 1, 2016 | Eli Lilly |
| NCT02791334 | Phase 1 | Jun 29, 2016 | Eli Lilly |
| NCT02779738 | Phase 1 | May 1, 2016 | Eli Lilly |
| NCT02711553 | Phase 2 | May 1, 2016 | Eli Lilly |
| NCT02370485 | Phase 1 | Feb 1, 2015 | Eli Lilly |
| NCT01981408 | Phase 1 | Nov 1, 2013 | Eli Lilly |
| NCT01285037 | Phase 1 | Sep 9, 2009 | Eli Lilly |
Showing 11 of 11 trials
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Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eli Lilly | For profit | 11 | 8 | 2 | 2009 |
| Harvard University | Academic/Hospital | 2 | 2 | 2 | 2016 |
| University of Utah | Academic/Hospital | 1 | 1 | 1 | 2018 |
3 organizations
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