Drug intelligence / Profile preview

olverembatinib

Development stage
Phase 3
Lead developer
Ascentage Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Olverembatinib is an orally administered **small-molecule tyrosine kinase inhibitor** developed by Ascentage Pharma. It was designed as a third-generation BCR-ABL1 inhibitor and has broader multikinase activity that includes **KIT, platelet-derived growth factor receptor alpha, fibroblast growth factor receptor, and SRC family kinases**, supporting development beyond leukemia into solid tumors such as gastrointestinal stromal tumor. In the GIST setting, olverembatinib has been studied in a Phase 1 trial in patients with unresectable or metastatic GIST and other solid tumors, including SDH-deficient GIST after prior tyrosine kinase inhibitor therapy. The drug is already approved in China for certain chronic myeloid leukemia indications, while in GIST it remains an investigational targeted anticancer therapy.

Brand names
Olveremb
Other names
olverembatinib
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)CD36 (CD36 antigen)FGFR (Fibroblast growth factor receptor)PDGFRA (Platelet-derived growth factor receptor alpha)VEGFR (VEGFR family)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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