Velzatinib

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** An orally bioavailable small molecule inhibitor of multiple mutated forms of mast/stem cell factor receptor KIT (c-Kit; SCFR), with potential antineoplastic activity. Upon oral administration, velzatinib targets, binds to and inhibits specific c-Kit mutants. This may inhibit tumor cell proliferation in cancer cell types that overexpress these c-Kit mutations. c-Kit, a transmembrane protein and receptor tyrosine kinase (RTK) overexpressed in various solid tumors and hematological malignancies, plays a key role in the regulation of cell differentiation and proliferation. Mutant forms of c-Kit are often associated with tumor chemoresistance.

**Synonyms:** - IDRX 42 - IDRX-42 - IDRX42 - KIT Inhibitor IDRX-42 - KIT-mutant Inhibitor IDRX-42 - M 4205 - M-4205 - M4205 - Multi-mutant-selective KIT Inhibitor IDRX-42 - VELZATINIB - c-KIT Inhibitor IDRX-42