12 July, 2020, Shanghai—Abbisko Therapeutics Co., Ltd. (“Abbisko” hereafter) today announces that it has obtained the regulatory approval from the Therapeutic Goods Administration (TGA) of Australia to initiate a phase I clinical study for ABSK043, an oral small molecule PD-L1 inhibitor, in subjects with solid tumors. 

ABSK043 is a brand-new orally bioavailable, highly potent and selective small molecule PD-L1 inhibitor. PD-1 and its ligand PD-L1 perform important roles in tumor progression and survival by escaping tumor neutralizing immune surveillance in the tumor microenvironment. A number of anti-PD-1/PD-L1 antibodies have been approved for market use, but no small molecule inhibitors of PD-1/PD-L1 have been approved so far. ABSK043 specifically binds to PD-L1 and leads to its internalization from the cell surface. Pre-clinical data have demonstrated strong inhibition of PD-1/PD-L1 interaction by ABSK043, and rescue of PD-L1-mediated inhibition of T-cell activation. ABSK043 has also demonstrated strong anti-tumor efficacy in several pre-clinical models.

“We are very happy to obtain the regulatory approval of ABSK043 in Australia, which is a critical first step for our following clinical trials.”said Dr. Jing Ji, Chief Medical Officer of Abbisko Therapeutics, “While anti-PD-1/anti-PD-L1 antibodies have revolutionized cancer treatment, the antibody-based immunotherapies carry a number of disadvantages such as high cost, lack of oral bioavailability, and immunogenicity, which could likely be improved with small molecule inhibitors. We look forward to advancing the development of ABSK043 to provide an attractive alternative to current therapies and address the unmet medical needs worldwide.”