Novartis' PI3Kα Inhibitor Alpelisib (BYL719) Granted Clinical Approval in China for PIK3CA-Mutated HR+/HER2- Advanced Breast Cancer

By Baihuawen

On April 27, Novartis received clinical trial approval in China for BYL719, in combination with fulvestrant, for the treatment of postmenopausal women and male patients with hormone receptor-positive, HER2-negative, PIK3CA-mutated advanced breast cancer who have experienced disease progression during or after endocrine therapy.

BYL719 (alpelisib), marketed under the brand name Piqray, received FDA approval on May 24, 2019, becoming the first PI3Kα inhibitor approved by the FDA for the treatment of breast cancer. Within just over seven months of its market launch, Piqray generated $116 million in sales.

PIK3CA gene mutations account for approximately 40% of patients with HR+, HER2- advanced or metastatic breast cancer. Results from the randomized, double-blind, phase III SOLAR-1 trial demonstrated that treatment with alpelisib plus fulvestrant significantly improved median progression-free survival compared with placebo plus fulvestrant (11 vs. 5.7 months).

Source: PharmaCube NextPharma

Currently, two PI3Kα inhibitors have been approved worldwide. In addition to Novartis’ alpelisib, Bayer’s copanlisib is the first PI3Kα inhibitor launched globally, having received approval on September 14, 2017, for the treatment of follicular lymphoma. In China, several candidates targeting this pathway are under development: CYH33 (Phase I clinical trial) by Haihe Biopharma/Shanghai Institute of Materia Medica, JS105 (preclinical) by Runjia Pharmaceutical/Junshi Biosciences, and DW09849 (preclinical) by Shanghai Institute of Materia Medica.