Novartis Introduces Alpelisib (Piqray®), the First Global Therapy for PIK3CA-Mutated Breast Cancer, to Boao Lecheng Pilot Zone

(August 16, 2021, Hainan, China) Novartis’s advanced breast cancer treatment Piqray® (alpelisib) was recently prescribed at Hainan Boao Super Hospital, enabling patients in China to benefit from innovative drugs simultaneously with the global community. As the world’s first and currently the only oral medication approved overseas for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated advanced breast cancer, Novartis’s alpelisib has been authorized for clinical use to address urgent clinical needs in specific medical institutions within the Hainan Boao Lecheng International Medical Tourism Pilot Zone. This fills a gap in China in this field, bringing hope to patients with urgent treatment needs.

# PIK3CA-Mutated Breast Cancer Presents Therapeutic Challenges

According to the latest 2020 global cancer data released by the International Agency for Research on Cancer (IARC) of the World Health Organization, there were 2.26 million new cases of breast cancer worldwide, surpassing the 2.2 million new cases of lung cancer and making breast cancer the most common cancer globally1. In China, breast cancer is the malignancy with the highest incidence among women, with 70% of patients diagnosed with HR+/HER2- breast cancer. PIK3CA is one of the most frequently mutated genes in the HR+/HER2- breast cancer subtype1.

Data from Chinese studies indicate that 49.3% of patients with HR+/HER2- breast cancer harbor PIK3CA mutations2. Meanwhile, numerous preclinical and clinical studies suggest that PIK3CA mutations are associated with the activation of the oncogenic PI3K/AKT/mTOR pathway, leading to its aberrant activation, which in turn stimulates tumor proliferation, metastasis, and invasion. Furthermore, these mutations are correlated with poor treatment response, unfavorable prognosis, or resistance to endocrine therapy3, thereby rendering treatment more challenging.

For more than a decade, efforts in China and internationally have been dedicated to developing drugs targeting the PI3K signaling pathway, but these have largely focused on hematological malignancies, lymphomas, and other conditions. It was not until May 2019 that the U.S. FDA approved the combination of Novartis’ alpelisib and fulvestrant for the treatment of postmenopausal women and men with HR+/HER2−, PIK3CA-mutated advanced breast cancer whose disease has progressed during or after endocrine therapy 4, opening the door for the application of PI3K inhibitors in solid tumors. Subsequently, alpelisib rapidly gained approval for the same indication in over 40 countries and regions, including Canada and the European Union.

The introduction of Novartis's innovative drug Alpelisib is pivotal to transforming the treatment landscape for patients with HR+/HER2- advanced breast cancer harboring PIK3CA mutations, and also provides clinicians and patients with a clear treatment option.

Alpelisib Brings Hope to Breast Cancer Patients with PIK3CA Mutations

Alpelisib is the first drug for HR+/HER2-, PIK3CA-mutated advanced breast cancer. As an oral small-molecule PI3Kα-specific class I phosphatidylinositol 3-kinase (PI3K) inhibitor, it demonstrates the ability to inhibit the PI3K pathway and exhibits antiproliferative effects in breast cancer cell lines harboring PIK3CA gene mutations.

Responsible Editor: Liuli

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