PIQRAY - The First and Only Treatment for Patients with A PIK3CA Mutation in HR+/HER2- Advanced Breast Cancer: A Review

Mutations in the PIK3CA gene in HR-positive or HER2-negative breast cancer patient is one of the most common causes of tumour growth and endocrine treatment resistance. Approximately 40% of the HR-positive or HER2-negative breast cancer patients have PIK3CA mutation worldwide. Alpelisib, a selective oral inhibitor of the class I PI3K catalytic subunit p110α, has shown synergistic antitumor activity with endocrine therapy against ER+/PIK3CA-mutated breast cancer cells.The phosphatidylinositol 3-kinase (PI3K) pathway is frequently activated in patients with estrogen receptor-positive (ER+), endocrine therapy-resistant breast cancers. PIK3CA mutations may lead to hyperactivation of PI3Kα, a key upstream component of the PI3K pathway Inhibiting PI3Kα interrupts AKT-dependent and AKT-independent signaling cascades in the PI3K pathway.PIQRAY and fulvestrant work synergistically to inhibit both the PI3K and ER pathways. in this review we discussed about the pharmacology, pharmacokinetics, pharmacodynamics and detailed clinical study of the piqray(alpelisib) the first and only treatment for the ER+/PIK3CA-mutated breast cancer.