China’s first PI3K inhibitor: Is it Apelvis?

About the identity of the first PI3K inhibitor in ChinaIt does not belong to Alpelisib (Alpelisib), but Duvelisab Capsules (formerly known as Duencib). Apelix, a kinase inhibitor, has gained recognition globally, particularly in the United States, for its efficacy in the treatment of advanced or metastatic breast cancer, particularly in patients with specific gene mutations in PIK3CA. However, despite its international recognition, Apelvis is not yet available in the Chinese market.

On May 24, 2019, the U.S. Food and Drug Administration (FDA) officially approved the treatment regimen of apelvis combined with fulvestrant for patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced breast cancer carrying PIK3CA mutations. These patients often have disease progression during or after endocrine therapy. At the same time, the FDA also approved the therascreen PIK3CA RGQ PCR kit as an auxiliary diagnostic tool for use with Apelvis. Clinical studies have shown that in patients with tumors with PIK3CA mutations, the treatment regimen of fulvestrant combined with apelvis prolonged the progression-free survival (PFS) compared with fulvestrant plus placebo.

However, back to the topic of China’s first PI3K inhibitor, it actually belongs to Duvelicet capsules. Duveliced u200bu200bis an inhibitor that can act on both PI3K-δ and PI3K-γ targets. It received marketing approval from the National Medical Products Administration in March 2022 and is specifically used to treat adult patients with follicular lymphoma who have experienced at least two systemic treatments but are still relapsed or refractory. The launch of duvelicet capsules not only fills the gap in the domestic PI3K inhibitor market, but also brings new treatment options to Chinese lymphoma patients.