Merestinib

Last updated
Merestinib
Merestinib.svg
Clinical data
Routes of
administration 		PO
ATC code
  • none
Identifiers
  • 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
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
ECHA InfoCard 100.233.673 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C30H22F2N6O3
Molar mass 552.542 g·mol−1
3D model (JSmol)
  • Cc1ccc(c(=O)n1c2ccc(cc2)F)C(=O)Nc3ccc(c(c3)F)Oc4cc5cnn(c5cc4c6c[nH]nc6)C
  • 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

  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.
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