Bayer's Copanlisib Becomes First PI3K Inhibitor Filed for Market Approval in China

On March 10, the CDE website showed that Bayer’s application for market approval of Copanlisib lyophilized powder for injection in China has been officially accepted by the CDE. It is the first PI3K inhibitor to be submitted for marketing approval in China.

Copanlisib is an intravenously administered phosphatidylinositol 3-kinase (PI3K) inhibitor that exhibits inhibitory activity against both the PI3K-α and PI3K-δ isoforms expressed in malignant B cells, inducing tumor cell death through apoptosis and inhibition of malignant B-cell proliferation.

In October 2020, Bayer announced the results of the Phase III CHRONOS-3 study evaluating copanlisib in combination with rituximab for the treatment of patients with relapsed indolent non-Hodgkin lymphoma (iNHL).

The CHRONOS-3 study is an international, multicenter, randomized, double-blind, placebo-controlled Phase III clinical trial designed to evaluate the efficacy of copanlisib in combination with rituximab versus placebo in combination with rituximab in prolonging progression-free survival (PFS). The study enrolled patients with relapsed indolent non-Hodgkin lymphoma (iNHL) who had received at least one prior line of therapy (including rituximab), including those with follicular lymphoma (FL), small lymphocytic lymphoma (SLL), lymphoplasmacytic lymphoma/Waldenström macroglobulinemia (LPL/WM), and marginal zone lymphoma (MZL). The study results demonstrated that the primary endpoint of prolonging progression-free survival (PFS) was met.

According to the PharmaGo database by Medicine Cube, the CHRONOS-3 study (China registration number: CTR20160337) began recruiting participants in China in February 2017, and Bayer announced the results of this study in October 2020.

Copanlisib was first approved by the FDA in September 2017 for the treatment of patients with relapsed follicular lymphoma (FL) who had received at least two prior lines of therapy. This accelerated approval was based on the results of the open-label, single-arm Phase II CHRONOS-1 study, which demonstrated an overall response rate (ORR) of 59%, including a complete response (CR) rate of 14%. Updated results after a 2-year follow-up showed an ORR of 59% in the FL population, with a CR rate of 20%.

In addition, Copanlisib is currently being evaluated in the CHRONOS-4 (China Clinical Trial Registration No.: CTR20160362) Phase III study, which combines standard immunochemotherapy for the treatment of relapsed indolent non-Hodgkin lymphoma (iNHL). The first patient was enrolled in July 2017. Patient recruitment is currently ongoing in China.

In China, the most advanced development for this target is Bayer’s Copanlisib. Novartis’s Alpelisib and Buparlisib, as well as Roche’s Taselisib and GDC-0077, are all in Phase III clinical trials. Domestic companies, including Chia Tai Tianqing, Innovent, Hutchison China MediTech, and CSPC Pharmaceutical Group, have also entered this field, with their candidates currently in Phase I/II clinical trials.

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