ipatasertibi

Ipatasertibi, often written as ipatasertib, is a small-molecule inhibitor of the serine/threonine kinase AKT (AKT1/AKT2/AKT3). By inhibiting AKT, ipatasertibi disrupts the PI3K/AKT/mTOR signaling pathway, reducing cancer cell growth and survival in tumors dependent on this axis. It is studied as a targeted therapy in oncology and has been evaluated in various cancer types, including breast and prostate cancer, both as a single agent and in combination regimens.

Development and research have focused on ipatasertibi’s ability to enhance the effectiveness of hormonal therapies or chemotherapy. It has entered multiple phase II and phase III clinical trials to assess outcomes such as progression-free survival and overall survival, as well as biomarker-driven subgroups. Results have been mixed across trials, with some showing signal in molecularly defined subsets (for example, tumors with alterations that heighten PI3K/AKT pathway dependence) and others failing to demonstrate a clear survival benefit. The efficacy of ipatasertibi appears to be influenced by tumor type, biomarker status, and treatment combination.

Regulatory status: as of 2024, ipatasertibi/ipatasertib has not received broad regulatory approval and remains under investigation in clinical research settings. Ongoing work continues to define which patients, if any, may derive meaningful benefit, and to identify reliable predictive biomarkers.

Safety and tolerability: common adverse events reported in trials include diarrhea, nausea, fatigue, hyperglycemia, rash, and decreased appetite, with some patients experiencing anemia or vomiting. Pharmacokinetic data support oral administration with metabolic clearance requiring careful monitoring in practice.

See also: AKT inhibitors, PI3K/AKT/mTOR pathway, targeted cancer therapy.