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CPO-166 is an orally bioavailable small molecule inhibitor of cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6) currently under development by CONJ Biotherapeutics. By simultaneously targeting CDK2 along with CDK4 and CDK6, CPO-166 is designed to overcome the resistance mechanisms that frequently emerge during treatment with selective CDK4/6 inhibitors in patients with metastatic breast cancer. The inhibition of these kinases prevents the phosphorylation of the retinoblastoma (Rb) protein, leading to cell-cycle arrest in the G1 phase and the suppression of tumor cell proliferation. The drug is currently being evaluated in Phase 2 clinical trials for the treatment of metastatic breast cancer.
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