Drug intelligence / Profile preview

napabucasin + imatinib

Development stage
Phase 1
Lead developer
Sumitomo Pharma America
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of **napabucasin**, a small molecule cancer stemness inhibitor that targets and inhibits oncogenic pathways including phosphorylated STAT3, β-catenin, and PD-L1, and **imatinib**, a small molecule tyrosine kinase inhibitor that primarily targets the BCR-ABL tyrosine kinase, as well as KIT and PDGFR. Napabucasin is orally administered and bioactivated by NAD(P)H:quinone oxidoreductase 1, increasing intracellular reactive oxygen species to cytotoxic levels. Imatinib is primarily used for hematological malignancies, such as chronic myeloid leukemia and gastrointestinal stromal tumors, by inhibiting tyrosine kinase signaling crucial for tumor cell survival and proliferation. There is currently no evidence of this specific combination being used or studied together in clinical or preclinical settings as of the present, although napabucasin has commonly been studied in combination with various chemotherapies and targeted agents, and imatinib is a staple in targeted therapy regimens.

Other names
napabucasin plus imatinibnapabucasin and imatinibBBI608 plus imatinibBBI-608 plus imatinibBBI 608 plus imatinibSTI571 plus napabucasinSTI-571 plus napabucasinSTI 571 plus napabucasin
02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)NQO1STAT3 (Signal Transducer and Activator of Transcription 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFR (PDGFR family)CD274 (Programmed cell death protein 1 ligand 1)CTNNB1 (Beta-catenin)

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