On May 28, 2025, Novartis announced that its new generation of anti vascular endothelial growth factor (anti-VEGF) monoclonal antibody, Brolucizumab (trade name: Beiyoushi^®), was approved by the National Medical Products Administration of China, and its indication was diabetes macular edema (DME). The application for marketing license of Busizumab for the treatment of neovascular (wet) age-related macular degeneration (wAMD) and proliferative diabetes retinopathy (PDR) indications has been submitted to the National Medical Products Administration in October 2024 and December 2024 respectively.

Brolucizumab is a humanized single chain variable fragment monoclonal antibody targeting vascular endothelial growth factor A (VEGF-A), with a molecular weight of 26kDa. Compared with the first generation of drugs, its molecular weight is smaller and the molar concentration is higher (6.0mg/0.05mL), allowing it to penetrate the retina more deeply and have stronger binding, quickly reaching the deep layers of retinal lesions. By directly inhibiting the VEGF-A pathway, it effectively blocks pathological vascular leakage, thereby rapidly improving the visual prognosis of DME patients.

The advantage of Brolucizumab is that the injection frequency is once every 3 months, and the dosing interval is longer than that of Ranibizumab (once a month) and Aflibercept (once every 2 months). In the Phase III HAWK and HARRIER studies targeting wAMD, the improvement effect of Brolucizumab on the best corrected visual acuity (BCVA) score was non inferior to that of aflibercept; In the Phase III KESTREL and KITE studies targeting DME, the efficacy of Brolucizumab in improving patients’ vision was not inferior to that of aflibercept. The KESTREL and KITE clinical studies targeting newly diagnosed DME patients have both achieved the primary efficacy endpoint, with visual benefits lasting up to 100 weeks; In two studies, patients in the 6mg group of Brolucizumab had fewer IRF (intraretinal fluid) and/or SRF (subretinal fluid), and patients receiving Brolucizumab treatment had 7 injections in the first year. The efficacy and safety results of the phase 3 KINGLET study of DME in the Chinese population are basically consistent with the global results.

Brolucizumab was first approved for marketing in the United States in October 2019, under the trade name Beovu^®, for the treatment of wAMD; In March 2022, Brolucizumab expanded the indication to DME. In February 2020, Brolucizumab was approved by the European Union for the treatment of wet age-related macular degeneration. Brolucizumab has also approved for the treatment of wAMD and DME in other countries and regions, such as Japan.

At present, the patent information registration platform for drugs in China and the US FDA drug database have not linked any patents to Brolucizumab; Based on the author’s patent analysis, it has been preliminarily determined that there are at least the patents listed in the table below for Brolucizumab in China. Therefore, it can be concluded that Brolucizumab has a comprehensive patent layout in China and is not easily broken through.

References:

1. https://mp.weixin.qq.com/s/C0owZIx957JLySL-W5i9JA?from=industrynews&color_scheme=light

2. https://zhuanlan.zhihu.com/p/1911352483281868047