ipatasertib + enzalutamide

**Ipatasertib + enzalutamide** is an investigational combination regimen comprising two small molecule drugs used in oncology, particularly in advanced prostate cancer. Ipatasertib is a potent pan-AKT inhibitor that binds AKT in an ATP-competitive manner, disrupting downstream signaling of the PI3K/AKT pathway, which is frequently dysregulated in cancer. Enzalutamide is an androgen receptor inhibitor, blocking androgen-induced tumor growth in prostate cancer. In preclinical models, the combination induces cell cycle arrest and apoptosis, even in enzalutamide-resistant cells, suggesting synergy. Clinical trials have demonstrated the combination is generally safe, though enzalutamide strongly induces CYP3A4 and can decrease ipatasertib plasma exposure by ~50%, potentially affecting efficacy.

Brand names

Xtandi (for enzalutamide)