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BPI-1178 + letrozole is a combination therapy under investigation for the treatment of advanced or recurrent hormone receptor-positive (HR+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer. **BPI-1178** (also called eciruciclib) is a novel, orally administered, selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). By inhibiting CDK4/6, BPI-1178 blocks phosphorylation of the retinoblastoma protein (Rb), resulting in G1 cell cycle arrest and inhibition of tumor cell proliferation. **Letrozole** is an aromatase inhibitor that decreases estrogen production, thereby further suppressing estrogen receptor–positive tumor growth. The combination is being studied to evaluate the safety, pharmacokinetics, and preliminary anti-tumor activity in patients with HR+/HER2- breast cancer who relapsed after prior endocrine therapy[1][2][4][6].
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