Small molecules, big impact: Advancing immune checkpoint inhibitors for cancer

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 also highlights the potential of combining small molecule ICIs with other therapeutic strategies, such as immune regulation and anti-angiogenesis, to amplify treatment efficacy. This comprehensive analysis of various small molecule inhibitors demonstrates their potential to revolutionize cancer treatment by addressing the limitations of antibody-based ICIs and offering more effective and accessible options for patients.

Dr. Chuan Xu, the senior researcher, stated, “The development of small molecule ICIs represents a significant leap in cancer therapy. These drugs not only address the limitations of current antibody-based therapies but also offer new avenues for combination treatments, enhancing overall efficacy and patient outcomes.”

The study’s findings suggest that small molecule ICIs could revolutionize cancer treatment, providing more accessible and cost-effective options. By improving tissue penetration and reducing production costs, these drugs have the potential to make advanced cancer therapies more widely available. The research paves the way for further exploration and clinical trials, aiming to establish small molecule ICIs as a cornerstone of modern cancer treatment.

More information:
Luoyi Chen et al, Development of small molecule drugs targeting immune checkpoints, Cancer Biology & Medicine (2024). DOI: 10.20892/j.issn.2095-3941.2024.0034

Provided by
University of Electronic Science and Technology of China