First PI3Kα Inhibitor for Breast Cancer Surpasses $116 Million in Sales Within Seven Months of Launch; Novartis Submits Clinical Application in China

Text | Baihuawen

On February 19, Novartis’ clinical trial application for BYL719 in China was accepted by the Center for Drug Evaluation (CDE). This new drug, marketed under the brand name Piqray, had just received FDA approval on May 24, 2019, and achieved sales of $116 million within nearly seven months of its launch.

BYL719 (alpelisib) is a PI3Kα inhibitor. Its first approved indication is in combination with fulvestrant for postmenopausal women with HR+, HER2-, PI3Kα-mutated advanced breast cancer who have experienced disease progression following endocrine therapy. It is the first PI3Kα inhibitor approved for the treatment of breast cancer.

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

Source: Medicine Cube NextPharma

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