Therapy Detail

Therapy Name Merestinib
Synonym
Therapy Description

Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Merestinib LY2801653 AXL Inhibitor 24 DDR1 Inhibitor 8 DDR2 inhibitor 7 FLT3 Inhibitor 50 MET Inhibitor 51 RON Inhibitor 10 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 23 TYRO3 Inhibitor 8 Merestinib (LY2801653) inhibits several receptor tyrosine kinases including MET, MST1R (RON), AXL, MERTK, TYRO3, ROS1 fusions, PDGFRA, FLT3, TEK, DDR1/2, MKNK1/2, and NTRK1/2/3 with greatest activity against NTRK1, and may result in decreased tumor growth (PMID: 23275061, PMID: 24305878, PMID: 29568395).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
MET D1228V Advanced Solid Tumor sensitive Merestinib Preclinical - Cell culture Actionable In a preclinical study, transformed human cells expressing MET D1228V were sensitive to Merestinib (LY2801653) in culture, resulting in suppression of Met phosphorylation (PMID: 27694386). 27694386
MET wild-type cholangiocarcinoma sensitive Merestinib Preclinical - Pdx & cell culture Actionable In a preclinical study, LY2801653 inhibited phosphorylation of Met, resulting in inhibition of cholangiocarcinoma proliferation in cell culture and growth of tumors in Pdx models (PMID: 26757360). 26757360
MET act mut malignant glioma sensitive Merestinib Preclinical - Cell line xenograft Actionable In a preclinical study, Merestinib (LY2801653) demonstrated anti-tumor activity in cell line xenograft models of glioma with autocrine activation of Met signaling (PMID: 23275061). 23275061
MET over exp lung adenocarcinoma sensitive Merestinib Preclinical - Cell line xenograft Actionable In a preclinical study, Merestinib (LY2801653) demonstrated anti-tumor activity in cell line xenograft models of lung adenocarcinoma with Met over expression (PMID: 23275061). 23275061
MET positive Advanced Solid Tumor predicted - sensitive Merestinib Preclinical - Pdx Actionable In a preclinical study, Merestinib (LY2801653) treatment resulted in growth inhibition correlating with Met expression level in a panel of patient-derived xenograft models of solid tumors (Cancer Res 2010;70(8 Suppl):Abstract nr 3611). detail...
MET over exp stomach cancer sensitive Merestinib Preclinical - Cell line xenograft Actionable In a preclinical study, LY2801653 blocked tumor growth in a gastric cancer cell line xenograft model over expressing Met (PMID: 23275061). 23275061
MET amp non-small cell lung carcinoma predicted - sensitive Merestinib Preclinical - Pdx Actionable In a preclinical study, Merestinib (LY2801653) treatment resulted in growth inhibition in patient-derived xenograft (PDX) models of MET-amplified non-small cell lung carcinoma that were resistant to Egfr inhibitors (Cancer Res 2010;70(8 Suppl):Abstract nr 3611). detail...
Unknown unknown colorectal cancer not applicable Merestinib Phase I Actionable In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including patients with colorectal cancer (Cancer Res October 1, 2014 74:CT237). detail...
Unknown unknown Advanced Solid Tumor not applicable Merestinib Phase I Actionable In a Phase I trial, LY2801653 demonstrated safety and preliminary efficacy in patients with advanced solid tumors (Cancer Res October 1, 2014 74:CT237). detail...
Unknown unknown non-small cell lung carcinoma not applicable Merestinib Preclinical Actionable In a preclinical study, LY2801653 inhibited tumor growth in mouse xenograft models of non-small cell lung cancer (PMID: 24305878). 24305878
ETV6-NTRK3 head and neck squamous cell carcinoma sensitive Merestinib Preclinical - Pdx Actionable In a preclinical study, a head and neck squamous cell carcinoma patient-derived xenograft (PDX) model harboring ETV6-NTRK3 was sensitive to treatment with Merestinib (LY2801653) compared to vehicle, demonstrating decreased tumor growth (PMID: 29568395). 29568395
MET D1228N Advanced Solid Tumor sensitive Merestinib Preclinical - Cell culture Actionable In a preclinical study, Merestinib (LY2801653) inhibited growth of transformed cells over expressing MET D1228N in culture (PMID: 23275061). 23275061
MET Y1230C Advanced Solid Tumor sensitive Merestinib Preclinical - Cell culture Actionable In a preclinical study, Merestinib (LY2801653) inhibited growth of transformed cells over expressing MET Y1230C in culture (PMID: 23275061). 23275061
Clinical Trial Phase Therapies Title Recruitment Status
NCT02920996 Phase II Merestinib Merestinib In Non-Small Cell Lung Cancer And Solid Tumors Recruiting
NCT03292536 Phase I Merestinib Merestinib on Bone Metastases in Subjects With Breast Cancer Recruiting
NCT02711553 Phase II Ramucirumab Merestinib Cisplatin + Gemcitabine A Study of Ramucirumab (LY3009806) or Merestinib (LY2801653) in Advanced or Metastatic Biliary Tract Cancer Active, not recruiting
NCT01285037 Phase I Cisplatin Cetuximab Merestinib A Study of LY2801653 in Advanced Cancer Completed