This invention describes the discovery and development of BPR5K230, a potent, orally bioavailable AXL and MERTK selective kinase inhibitor targeting tumor and tumor immune microenvironment for the treatment of triple negative breast cancer patients who fail current therapies and whose tumors and immune cells overexpress AXL and MERTK. The current invention represents a novel target-driven, patient-stratified precision cancer medicine for tough-to-treat cancers.

BPR5K230 is a potent, oral bioavailable AXL and MERTK selective kinase inhibitor with anti-tumor efficacy and immunomodulatory activities discovered from our propritory compound library and optimized by structure-based drug design by protein crytalography. The anti-tumor effect of BPR5K230, alone or in combination with immune checkpoint inhibitor was superior to the clinical stage agent Ono-7475. BPR5K230 is most suitable for TNBC patients who are prone to recurrence, refractory and metastasis.

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