KRLS-017

KRLS-017 is an orally bioavailable, reversible small molecule inhibitor of cyclin-dependent kinase 7 (CDK7) being developed as a precision oncology therapy for advanced solid tumors and hematologic malignancies. It shows high biochemical selectivity for CDK7 in large kinase panels and potent antiproliferative activity across a broad range of tumor cell lines, with significant tumor growth inhibition and regression in multiple xenograft models at tolerated doses.[1][3][5][9][11][14][7] By inhibiting CDK7-dependent transcriptional programs and cell cycle regulation, KRLS-017 can suppress oncogenic drivers such as c-MYC and enhances the antitumor efficacy of androgen receptor–targeted therapy (enzalutamide) in androgen receptor–positive triple-negative breast cancer models.[2][3][5][7][14] The drug is being advanced by Kirilys Therapeutics, under license from Ube Industries, with a first-in-human phase 1 trial planned/initiated in patients with treatment-refractory advanced solid tumor malignancies.[3][5][9][11][13]