3 September, 2021, Shanghai – Abbisko Therapeutics Co., Ltd. (“Abbisko” hereafter) today announced dosing of the first patient in a phase I clinical study in Australia for ABSK043, an oral small molecule PD-L1 inhibitor. The purpose of the trial is to assess the safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity of ABSK043 in patients 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. Small molecule inhibitor may address the disadvantages of anti-PD-1/anti-PD-L1 antibodies, such as lack of oral bioavailability, limited blood-brain barrier permeability, and immunogenicity. 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 has also demonstrated strong anti-tumor efficacy in several pre-clinical models.” said Dr. Jing Ji, Chief Medical Officer of Abbisko Therapeutics, “The development of this oral small molecule PD-L1 inhibitor takes lead at home and abroad. As Abbisko’s first IND approval in Australia, the program will greatly accelerate the company's global multi-center clinical development. The oral small molecule PD-L1 inhibitor will play as the cornerstone of immune-oncology therapies for the company and further demonstrates our layout in the combination therapies development. We look forward to help cancer patients around the world to live better and longer lives.”