Therapy Detail

Therapy Name Glesatinib
Therapy Description

Glesatinib (MGCD265) inhibits several tyrosine kinases including MET, MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Glesatinib MGCD265 AXL Inhibitor 24 MET Inhibitor 50 RON Inhibitor 10 VEGFR Inhibitor (Pan) 29 Glesatinib (MGCD265) inhibits several tyrosine kinases including MET, MST1R (RON), and AXL, as well as VEGFR1-3, and TIE2, which may result in decreased tumor growth (PMID: 25806189, PMID: 26555154).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
MET amp lung cancer sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, Glesatinib (MGCD265) inhibited Met phosphorylation and growth of MET-amplified lung cancer cells in culture (PMID: 28765324). 28765324
MET wild-type bladder carcinoma decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in only partial growth inhibition in cell line xenograft models of MET wild-type urinary bladder carcinoma (PMID: 28765324). 28765324
MET del exon14 Advanced Solid Tumor sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing deletion of MET exon 14 were sensitive to Glesatinib (MGCD265) treatment in culture, demonstrating inhibition of spheroid growth (PMID: 28765324). 28765324
Unknown unknown Advanced Solid Tumor not applicable Glesatinib Phase I Actionable In a Phase I trial, Glesatinib (MGCD265) displayed safety and preliminary efficacy in patients with advanced solid tumors (J Clin Oncol 27, 2009 (suppl; abstr e14525)). detail...
MET amp stomach cancer sensitive Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in tumor regression in MET-amplified gastric cancer cell line xenograft models (PMID: 28765324). 28765324
MET del exon14 MET D1228N Advanced Solid Tumor sensitive Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells expressing MET deletion exon 14 and MET D1228N were sensitive to Glesatinib (MGCD265) treatment, demonstrating cell growth inhibition in culture and 21% tumor regression in xenograft models (PMID: 28765324). 28765324
MET del exon14 MET Y1230C Advanced Solid Tumor sensitive Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, transformed cells expressing MET deletion exon 14 and MET Y1230C were sensitive to Glesatinib (MGCD265) treatment, demonstrating cell growth inhibition in culture and 52% tumor regression in xenograft models (PMID: 28765324). 28765324
MET amp MET del exon14 lung cancer sensitive Glesatinib Preclinical - Pdx Actionable In a preclinical study, a lung cancer patient-derived xenograft (PDX) model harboring MET amplification and MET exon 14 deletion demonstrated tumor regression when treated with Glesatinib (MGCD265) (PMID: 28765324). 28765324
MET del exon14 lung cancer sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, Glesatinib (MGCD265) inhibited Met phosphorylation and growth in lung cancer cells harboring MET exon 14 deletion and loss of the wild-type MET allele in culture (PMID: 28765324). 28765324
MET wild-type breast cancer decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment only resulted in partial growth inhibition in cell line xenograft models of MET wild-type breast cancer (PMID: 28765324). 28765324
MET act mut Advanced Solid Tumor sensitive Glesatinib Preclinical Actionable In a preclinical study, cells harboring MET activating mutations demonstrated sensitivity to treatment with Glesatinib (MGCD265) in cell-based assays (AACR; Cancer Res 2010;70(8 Suppl):Abstract nr 3609). detail...
MET D1228V Advanced Solid Tumor sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, transformed human cells expressing MET D1228V were sensitive to Glesatinib (MGCD265) in culture, resulting in suppression of Met phosphorylation (PMID: 27694386). 27694386
MET del exon14 lung adenocarcinoma sensitive Glesatinib Clinical Study Actionable In a clinical study, a patient with lung adenocarcinoma harboring a deletion of MET exon 14 demonstrated a 66% reduction in target lesion size and maintained a partial response for 7 months when treated with Glesatinib (MGCD265) (PMID: 28765324). 28765324
MET Y1230C Advanced Solid Tumor sensitive Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, a transformed cell line expressing MET Y1230C was sensitive to Glesatinib (MGCD265), demonstrating inhibition of cell growth in culture and 88% tumor regression in xenograft models (PMID: 28765324). 28765324
MET amp MET del exon14 MET D1228N MET G1163R MET L1195V lung adenocarcinoma resistant Glesatinib Clinical Study Actionable In a clinical case study, a lung adenocarcinoma patient previously harboring MET amp, MET deletion exon 14, MET D1228N, MET Y1230H, MET Y1230S, and MET G1163R demonstrated a decrease in lesion size when treated with Glesatinib (MGCD265), however, progression ensued and plasma testing indicated the patient lost Y1230H and Y1230S, but acquired MET L1195V (PMID: 28765324). 28765324
MET amp MET del exon14 non-small cell lung carcinoma sensitive Glesatinib Preclinical - Pdx Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in tumor regression in patient-derived xenograft (PDX) models of non-small cell lung cancer harboring deletion of MET exon 14 and varying degrees of MET amplification (PMID: 28765324). 28765324
MET wild-type Advanced Solid Tumor decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in only partial growth inhibition in MET wild-type cell line xenograft models of various tumor types (PMID: 28765324). 28765324
MET F1200L MET Y1230H stomach cancer sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, a gastric adenocarcinoma cell line (PMID: 15494073) co-harboring MET Y1230H and MET F1200L was sensitive to treatment with Glesatinib (MGCD265), demonstrating cell growth inhibition in culture (PMID: 28765324). 28765324 15494073
MET wild-type colorectal cancer decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in only partial growth inhibition in cell line xenograft models of MET wild-type colorectal cancer (PMID: 28765324). 28765324
MET Y1230C stomach cancer sensitive Glesatinib Preclinical - Cell culture Actionable In a preclinical study, a gastric adenocarcinoma cell line (PMID: 15494073) harboring MET Y1230C was sensitive to treatment with Glesatinib (MGCD265), demonstrating cell growth inhibition in culture (PMID: 28765324). 28765324 15494073
MET wild-type prostate cancer decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in only partial growth inhibition in cell line xenograft models of MET wild-type prostate caner (PMID: 28765324). 28765324
MET del exon14 stomach cancer sensitive Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) inhibited Met phosphorylation and growth in gastric cancer cells harboring MET exon 14 deletion and amplification of the mutant allele in culture, and resulted in tumor regression in cell line xenograft models (PMID: 28765324). 28765324
MET wild-type pancreatic cancer decreased response Glesatinib Preclinical - Cell line xenograft Actionable In a preclinical study, Glesatinib (MGCD265) treatment resulted in only partial growth inhibition in cell line xenograft models of MET wild-type pancreatic cancer (PMID: 28765324). 28765324
Clinical Trial Phase Therapies Title Recruitment Status
NCT00697632 Phase I Glesatinib Safety Study of Oral MGCD265 Administered Without Interruption to Subjects With Advanced Malignancies Completed
NCT02544633 Phase II Glesatinib Phase 2 Study of MGCD265 in Patients With Non-Small Cell Lung Cancer With Activating Genetic Alterations in MET Completed