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GDC-4198 (also known as RGT-419B) is a new generation small molecule inhibitor targeting cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6). Developed by Regor Therapeutics, and advanced in partnership with Genentech/Roche, it is being investigated primarily for the treatment of HER2-negative, hormone receptor positive (HR+), advanced/metastatic breast cancer, including in patients who have progressed on previous CDK4/6 inhibitor therapy. GDC-4198 demonstrates potent and selective inhibition of CDK4, with additional activity against CDK2 and CDK6, and has shown favorable safety and preliminary efficacy in early phase trials as both monotherapy and in combination with endocrine therapy (e.g. giredestrant). The drug is administered orally and is considered a new molecular entity within the antineoplastic small molecule class[1][3][4][5][7].
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