Merestinib

Merestinib
Clinical data
Routes of; administration	PO
ATC code	none;
Identifiers
	IUPAC name 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;
CAS Number	1206799-15-6;
ChemSpider	29361338;
UNII	5OGS5K699E;
KEGG	D11763;
CompTox Dashboard (EPA)	DTXSID20659635 ;
ECHA InfoCard	100.233.673
Chemical and physical data
Formula	C30H22F2N6O3
Molar mass	552.542 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1ccc(c(=O)n1c2ccc(cc2)F)C(=O)Nc3ccc(c(c3)F)Oc4cc5cnn(c5cc4c6c[nH]nc6)C;
	InChI InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39); Key:QHADVLVFMKEIIP-UHFFFAOYSA-N;

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.^[1]

Meristinib is part of a phase II clinical trial for advanced billiary tract cancer. The study is expected to be complete in April 2018.^[2] Phase II clinical trials for non-small cell lung cancer and solid tumors began in November 2016.^[3]

References

^ Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, et al. (March 2018). "Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors". Oncotarget. 9 (17): 13796–13806. doi:10.18632/oncotarget.24488. PMC 5862616. PMID 29568395.
^ Clinical trial number NCT02711553 for "A Study of Ramucirumab (LY3009806) or Merestinib (LY2801653) in Advanced or Metastatic Biliary Tract Cancer" at ClinicalTrials.gov
^ "Merestinib - Eli Lilly". AdisInsight. Springer Nature Switzerland AG.

[Konicek_2018-1] Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, et al. (March 2018). "Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors". Oncotarget. 9 (17): 13796–13806. doi:10.18632/oncotarget.24488. PMC 5862616. PMID 29568395.

[2] Clinical trial number NCT02711553 for "A Study of Ramucirumab (LY3009806) or Merestinib (LY2801653) in Advanced or Metastatic Biliary Tract Cancer" at ClinicalTrials.gov

[3] "Merestinib - Eli Lilly". AdisInsight. Springer Nature Switzerland AG.

[1]

[2]

[3]

Clinical data

Routes of administration	PO
ATC code	none
Identifiers
IUPAC name 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
CAS Number	1206799-15-6
ChemSpider	29361338
UNII	5OGS5K699E
KEGG	D11763
CompTox Dashboard (EPA)	DTXSID20659635
ECHA InfoCard	100.233.673
Chemical and physical data
Formula	C₃₀H₂₂F₂N₆O₃
Molar mass	552.542 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES Cc1ccc(c(=O)n1c2ccc(cc2)F)C(=O)Nc3ccc(c(c3)F)Oc4cc5cnn(c5cc4c6c[nH]nc6)C
InChI InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39) Key:QHADVLVFMKEIIP-UHFFFAOYSA-N