Activating mutations in FLT3 are found in 30% of Acute Myeloid Leukemia (AML) and associated with poor prognosis. Approved FLT3 inhibitors show clinical benefit but patients relapse with novel secondary mutations; KinaRX’s lead compound KRX-107 shows superior efficacy against FLT3 and novel gatekeeper mutations and is currently being evaluated in preclinical safety studies.

RET aberrations are major drivers in medullary thyroid cancer, multiple endocrine neoplasia, non small cell lung cancer, and colorectal cancer. RET Kinase inhibitors show significant promise for treatment of RET mutant cancers but eventually patients relapse due to secondary mutations. KinaRX has developed highly potent, second generation RET inhibitors with activity against RET drug resistant mutations.

Oncogenic rearrangements in NTRK1, NTRK2, and NTRK3 lead to constitutively-active TRKA, TRKB, and TRKC receptors and are frequently observed in colon, lung, thyroid, head and neck cancers and glioblastoma. KinaRX is screening compounds that inhibit TRKA/B/C.