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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

General Review Article

Small Molecules as PD-1/PD-L1 Pathway Modulators for Cancer Immunotherapy

Author(s): Peifu Jiao, Qiaohong Geng*, Peng Jin, Gaoxing Su, Houyun Teng, Jinlong Dong and Bing Yan*

Volume 24, Issue 41, 2018

Page: [4911 - 4920] Pages: 10

DOI: 10.2174/1381612824666181112114958

open access plus


Blockade of PD-1/PD-L1 interactions using PD-1/PD-L1 pathway modulators has shown unprecedented clinical efficacy in various cancer models. Current PD-1/PD-L1 modulators approved by FDA are exclusively dominated by therapeutic antibodies. Nevertheless, therapeutic antibodies also exhibit several disadvantages such as low tumor penetration, difficulty in crossing physiological barriers, lacking oral bioavailability, high manufacturing costs, inaccessible to intracellular targets, immunogenicity, immune-related adverse events (irAEs). Modulation of PD-1/PD-L1 pathway using small molecules may be an alternative approach to mobilize immune system to fight against cancers. In this review, we focus on summarizing the recently disclosed chemical structures and preliminary structure-activity relationships (SARs) of small molecules as PD-1/PD-L1 modulators for cancer immunotherapy.

Keywords: Immune checkpoint modulators, sulfonamides, thiadiazoles, oxadiazoles, biphenyl derivatives, molecular docking.

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