The effects and efficacy of Alpelisib-Piqray

Alpelisib (Alpelisib)-Piqray is the first selective PI3Kα inhibitor. In preclinical models, it not only effectively inhibited the two most common PIK3CA mutations (H1047R and E545K) with an IC50 of approximately 4 nmol/L, but also demonstrated a dual mechanism of action, namely inhibiting PI3K and inducing p110α degradation in a dose-dependent manner in certain ER+/PIK3CA mutant breast cancer cell lines.

PIK3CA mutations and/or amplifications were shown in a human Phase I study of 134 patients with various cancer types who received apelix monotherapy. Objective tumor responses were only observed at once-daily doses of ≥270 mg, with an overall response rate (ORR) of 6.0%. The condition of 52.2%of the patients was stable, and the condition of 9.7%of the patients was maintained> for 24 weeks. In patients with ER+/HER2- advanced cancer who received ≥270 mg of apelvis once daily, the median progression-free survival (PFS) was 5.5 (95% CI 3.0–7.0) months.

The original drug of Apellis is not marketed in the country and therefore cannot be included in medical insurance. There are European and Indian versions of the original Apelvis drug sold overseas. The ingredients are basically the same. The price of the European version of 150mg*56 tablets per box may be more than 4 RMB 40,000 ( (The price may fluctuate due to the exchange rate), The price of the Indian version150mg*28 tablets per box may be more than 5,000 yuan (the price may fluctuate due to the exchange rate). There are currently no generic versions of Apelvis produced and marketed.