Immunotherapy has revolutionized cancer treatment, with immune checkpoint inhibitors (ICIs) playing a pivotal role. However, current ICIs, primarily monoclonal antibodies, face significant challenges like poor tissue penetration, high production costs, and off-target effects. These limitations hinder their efficacy and accessibility.
Due to these issues, there is an urgent need to explore alternative approaches. Small molecule drugs targeting immune checkpoints offer a promising solution, potentially overcoming these barriers and providing more effective cancer therapies. A recent review by researchers from the University of Electronic Science and Technology of China, affiliated with Sichuan Provincial People's Hospital, published in Cancer Biology & Medicine , explores the development of small molecule drugs targeting immune checkpoints.
The study presents an innovative approach to cancer therapy by focusing on the efficacy and mechanisms of small molecule ICIs. The study underscores the advantages of small molecule ICIs over traditional antibody-based therapies. These small molecule drugs exhibit superior tissue permeability, better oral bioavailability, and favorable pharmacokinetic properties.
Key examples include BMS-202, which induces PD-L1 dimerization to block PD-1/PD-L1 interactions, and CA-170, the first oral ICI to enter clinical trials. Additionally, YPD-29B has shown promising results in promoting PD-L1 degradation and enhancing antitumor immunity. The research a.