Serabelisib is an investigational small molecule inhibitor targeting the PI3K/AKT/mTOR signaling pathway, specifically inhibiting the p110α isoform of phosphoinositide 3-kinase (PI3Kα). This pathway is frequently dysregulated in various cancers, making Serabelisib a candidate for oncology therapeutics. It has been studied in clinical trials for solid tumors, including breast cancer, endometrial cancer, and lymphoma, particularly in patients with PIK3CA mutations. The compound aims to suppress tumor growth and proliferation by blocking downstream signaling involved in cell survival, metabolism, and angiogenesis. Research has also explored its use in combination with other targeted therapies or hormonal agents to enhance antitumor effects and overcome resistance mechanisms. Despite promising preclinical activity, development has faced challenges related to toxicity and efficacy, leading to ongoing evaluation in biomarker-selected populations.