Drug intelligence / Profile preview

ziftomenib + imatinib

Development stage
Unknown
Lead developer
Kura Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Ziftomenib + imatinib is an investigational **oral small molecule combination therapy** composed of ziftomenib, a highly selective menin inhibitor, and imatinib, a standard-of-care tyrosine kinase inhibitor. This combination is under clinical investigation for the treatment of patients with **advanced gastrointestinal stromal tumors (GIST)** who have previously experienced disease progression during imatinib monotherapy. Ziftomenib acts by inhibiting the interaction between menin and histone methyltransferase proteins involved in epigenetic regulation of gene expression, while imatinib targets tyrosine kinases such as KIT and PDGFRA, which are commonly mutated in GIST. Early clinical studies are assessing safety, tolerability, and preliminary antitumor activity of this combination[1][2][5][6][7].

02

Targets

MEN1 (Menin)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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