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Drug intelligence / Profile preview
PF-08165784 is an orally administered small molecule inhibitor targeting phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA). Developed by Pfizer, the drug is designed to treat advanced or metastatic solid tumors harboring PIK3CA mutations, including hormone receptor-positive (HR+), HER2-negative (HER2-) breast cancer and colorectal cancer. By selectively inhibiting PIK3CA, PF-08165784 blocks the hyperactive PI3K/Akt/mTOR signaling pathway that drives tumor cell proliferation and survival. It is currently being evaluated in Phase 1 clinical trials as a monotherapy and in combination with other anti-cancer agents such as fulvestrant, letrozole, cetuximab, and atirmociclib.
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