Roche Submits NDA in China for Inavolisib, the First Domestic PI3Kα Inhibitor for PIK3CA-Mutated HR+/HER2- Advanced Breast Cancer

On June 3, the CDE website showed,Roche's PI3Kα Inhibitor Inavolisib (GDC-0077, Inavolisib) Submitted for Marketing Authorization in China, in combination with palbociclib and fulvestrant, for the treatment of adult patients with locally advanced or metastatic breast cancer that is PIK3CA-mutated, hormone receptor-positive (HR+), and human epidermal growth factor receptor 2-negative (HER2-), who have relapsed within 12 months after previous adjuvant endocrine therapy or completion of adjuvant endocrine therapy. Recently,Roche has also submitted an application to the FDA for the drug's market approval.。

Source: Center for Drug Evaluation, National Medical Products Administration

Inalisib is an orally administered, highly selective PI3Kα inhibitor., with higher selectivity and potency for PI3Kα than other subtypes (PI3Kβ/δ/γ), and is capable of specifically triggering the degradation of mutant PI3Kα protein. With this unique dual mechanism of action, inavolisib may offer well-tolerated, durable disease control for patients with HR+/HER2- PI3Kα-mutant advanced breast cancer and could potentially improve their prognosis.

Currently, only Alpelisib (Novartis), a selective PI3Kα inhibitor, has been approved for marketing globally. Besides,Three selective PI3Kα inhibitors are in Phase III, namely Inalisib, Taselisib (Roche), and Serabelisib (Kaken/Petra Pharma),Inavolisib is one of the fastest progressing products.