Drug intelligence / Profile preview

glesatinib + sitravatinib + mocetinostat

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

A combination regimen consisting of **glesatinib**, **sitravatinib**, and **mocetinostat**—each an investigational **small molecule inhibitor**—has been evaluated in parallel, in combination with immune checkpoint inhibitor nivolumab, for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC). - **Glesatinib** is a multi-targeted tyrosine kinase inhibitor of **MET** and **AXL** receptors, associated with dysregulated signaling in NSCLC. - **Sitravatinib** inhibits a spectrum of receptor tyrosine kinases (RTKs), including **MET, AXL, MERTK, VEGFR family, PDGFR family, KIT, FLT3, Trk family, RET, DDR2, and selected Eph family members**. - **Mocetinostat** is a histone deacetylase (**HDAC**) inhibitor with epigenetic modulating activity. All agents are orally administered small molecules and intended for use with nivolumab (a monoclonal antibody inhibiting PD-1). This combination was tested in Phase 2 trials in NSCLC patients pre-treated with checkpoint inhibitors or platinum-based chemotherapy. Cohorts received each agent separately, not the three-drug combination together[1][3][9]. No identified evidence supports clinical use of the three agents as a single, combined drug product, only as parallel individual combinations with immunotherapy in trial arms.

Brand names
none known; all are investigational drugs
Other names
none known; drug names are standard
02

Targets

TEK (Angiopoietin-1 receptor)HDAC1 (Histone Deacetylase 1)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)FLT3 (Fms related receptor tyrosine kinase 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)KIT (c-KIT proto-oncogene receptor tyrosine kinase)EPHA3/EPHB2/EPHB4 (Ephrin type-A receptor 3 / Ephrin type-B receptor 2 / Ephrin type-B receptor 4)SMO (Smoothened)RET (Rearranged during transfection receptor tyrosine kinase)AXL (AXL receptor tyrosine kinase)NTRK1 (Tropomyosin-related receptor kinase A)ABCG2 (Breast cancer resistance protein)PDGFRA (Platelet-derived growth factor receptor alpha)DDR2 (Discoidin domain receptor tyrosine kinase 2)MET (Mesenchymal-epithelial transition factor receptor)VEGFR2 (Vascular endothelial growth factor receptor 2)MST1R (Recepteur d'origine nantais)

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