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ARTS-021 is an orally bioavailable, highly potent and selective small molecule inhibitor of cyclin-dependent kinase 2 (CDK2), a key enzyme involved in cell cycle regulation. By inhibiting the CDK2/CyclinE1 complex, it disrupts abnormal cell proliferation driven by CCNE1 amplification or cyclin E overexpression. The drug is being developed primarily for the treatment of advanced solid tumors, including hormone receptor positive/HER2 negative breast cancer and CCNE1-amplified cancers. It may also be used in combination with CDK4/6 inhibitors to overcome resistance mechanisms in certain cancers. The developer is Avenzo Therapeutics, with Allorion Therapeutics as the originator.
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