Drug intelligence / Profile preview

glesatinib + docetaxel

Development stage
Discontinued
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Glesatinib (MGCD265) in combination with docetaxel is an investigational therapeutic regimen developed by Mirati Therapeutics for the treatment of advanced solid tumors, including non-small cell lung cancer (NSCLC). Glesatinib is an orally bioavailable, small molecule multi-kinase inhibitor that targets the MET and AXL receptor tyrosine kinases, which are often implicated in tumor growth, invasion, and resistance to therapy. It also exhibits activity against the VEGFR and PDGFR families. Docetaxel is a taxane-based cytotoxic chemotherapy agent that promotes the assembly of tubulin into stable microtubules and inhibits their disassembly, leading to cell cycle arrest and apoptosis. The combination was studied in Phase I/II clinical trials to evaluate whether the dual inhibition of key signaling pathways and microtubule stabilization could provide enhanced clinical benefit in patients with advanced malignancies.

Other names
glesatinib + docetaxelMGCD265 + docetaxel
02

Targets

AXL (AXL receptor tyrosine kinase)BCL-2 (BCL-2 family)DDR2 (Discoidin domain receptor tyrosine kinase 2)EPH (EPH receptor family)FLT3 (Fms related receptor tyrosine kinase 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)MET (Mesenchymal-epithelial transition factor receptor)PDGFR (PDGFR family)RET (Rearranged during transfection receptor tyrosine kinase)Trk (Trk receptor family)VEGFR (VEGFR family)TUBB (Tubulin (alpha and beta subunits))

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