China-based Ascletis Pharma Inc. (HKG: 1672) has announced the approval of the Investigational New Drug (IND) application by China National Medical Products Administration (NMPA) for its in-house developed oral programmed-death ligand 1 (PD-L1) small molecule inhibitor ASC61. This approval will accelerate the global development of the drug, which is currently undergoing a Phase I dose escalation study in the US.
ASC61 Profile
ASC61 is an oral small molecule inhibitor prodrug. Its active metabolite, ASC61-A, is a potent and highly selective inhibitor that blocks PD-1/PD-L1 interaction through inducing PD-L1 dimerization and internalization. Preclinical studies have shown that ASC61 has good safety and pharmacokinetic profiles in animal models, demonstrating significant antitumor efficacy in multiple animal models, including humanized mouse models.
Benefits Over PD-1/PD-L1 Antibody Injections
Compared with PD-1/PD-L1 antibody injections, the oral PD-L1 inhibitor ASC61 offers several advantages:
- Higher patient compliance with easy and safe administration, eliminating the need for hospital visits for injections.
- Ease of combination with other oral anti-tumor drugs in all-oral therapies.
- Easier management of immune-related adverse effects (irAEs) through dose adjustment.
- Relatively lower cost.
- Higher permeability, allowing better distribution into targeted tissues.
Future Implications
The IND approval in China marks a significant milestone in the global development of ASC61. This approval positions Ascletis Pharma to further advance the clinical development of ASC61, leveraging its unique advantages to address unmet medical needs in the treatment of advanced solid tumors.-Fineline Info & Tech
