The board of directors of Sino Biopharmaceutical Limited announced that the Group's self-developed "TQB3019 (BTK PROTAC)" has been approved for clinical trial by the National Medical Products Administration (NMPA) of China. The drug is intended for use in the treatment of hematologic tumours. TQB3019 is an orally available proteolysis targeting chimera (PROTAC) targeting BTK developed on the Group's OAPD® technology platform.
As a heterobifunctional molecule, TQB3019 activates the ubiquitin-proteasome pathway by binding to BTK proteins and E3 ubiquitin ligases to degrade targeted proteins. This mechanism of action can inhibit BTK and downstream signal transduction, thereby inhibiting tumour growth. Compared with traditional BTK inhibitors, PROTACs show greater potential in overcoming the challenge of BTK inhibitor resistance.
Preclinical studies have demonstrated that TQB3019 has significant efficacy, a clear mechanism as well as good safety, and has the potential to solve the problem of cancer drug resistance. In vitro studies have shown that TQB3019 has a significant inhibitory effect on the proliferation of a variety of in vitro cultured BTK wild-type and different mutant types of tumour cells. In animal models, TQB3019 can significantly inhibit the growth of subcutaneous transplantation tumours in mice with BTK wild-type and different drug-resistant mutant cells, with strong inhibitory activity.
At present, no PROTAC with the same target has been approved for marketing in the world. The Group is actively engaged in the development of BTK inhibitors and PROTACs. In addition to TQB3019, Phase II clinical studies have been initiated for TQB3702 (a second-generation BTK inhibitor), while TQB3201 (AR PROTAC) and TQB3142 (BCL-XL-PROTAC) are in the pre-Investigational New Drug (pre-IND) stage.
The Group will expedite the clinical development of these products and focus on unmet clinical needs around the world, with a view to providing patients with better treatment options. The OAPD® (Orally Available Protein Degrader) drug discovery platform is independently developed by the Group with global independent intellectual property rights. Based on the highly innovative and proprietary E3 ubiquitin ligase ligands, the platform accelerates the discovery of protein degraders by leveraging generative AI-based molecular design.
Through precise design and optimization, the degraders developed on the OAPD ® platform not only exhibit excellent degradation activity and remarkable oral bioavailability, but also significantly reduce safety concerns associated with immunomodulatory activity. Currently, TQB3019 developed on the platform has been approved for clinical trial by the NMPA, with several other projects in the pre-IND stage.
