Unlocking the Potential of Alpelisib in Breast Cancer: A Comprehensive Review

Alpelisib is a cancer therapy drug that has shown significant promise in the treatment of certain types of cancer. Its pharmacokinetics and pharmacodynamics indicate that it is absorbed better orally and has a prolong half-life, allowing for once-every day dosing. Currently, its mechanism of action is established to be the suppression of phosphatidylinositol-4, 5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA), which is the pivotal enzyme of PI3K pathway, which is abnomal in most cancers. The chemistry of alpelisib involves its selective inhibition of PI3K, targeting specifically HR-positive, HER2-negative breast cancer with PIK3CA mutations. The common side effects associated with alpelisib include fever, peripheral edema, fatigue, headache, skin rash, alopecia, pruritis, hyperglycemia, increased gamma-glutamyl transferase, decreased serum calcium, weight loss, diarrhea, nausea, increased serum lipase, decreased appetite, stomatitis, vomiting, dysgeusia, lymphocytopenia, prolonged PTT, and increased serum creatinine. The use of alpelisib in cancer therapy is being extensively studied through various clinical trials, aiming to determine the optimal patient populations for treatment and explore alternative tumor indications and drug combine regimens.