Therapy Detail

Therapy Name Merestinib
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 48 MET Inhibitor 50 RON Inhibitor 10 ROS1 Inhibitor 14 Trk Receptor Inhibitor (Pan) 21 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 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 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...
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 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 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...
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...
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
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
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
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
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
Clinical Trial Phase Therapies Title Recruitment Status
NCT02711553 Phase II Ramucirumab Merestinib Gemcitabine + Cisplatin A Study of Ramucirumab (LY3009806) or Merestinib (LY2801653) in Advanced or Metastatic Biliary Tract Cancer Active, not recruiting
NCT03292536 Phase I Merestinib Merestinib on Bone Metastases in Subjects With Breast Cancer Recruiting
NCT01285037 Phase I Cisplatin Cetuximab Merestinib A Study of LY2801653 in Advanced Cancer Completed
NCT02920996 Phase II Merestinib Merestinib In Non-Small Cell Lung Cancer And Solid Tumors Recruiting