Opportunities for Small Molecules in Cancer Immunotherapy

Trends Immunol. 2020 Jun;41(6):493-511. doi: 10.1016/j.it.2020.04.004. Epub 2020 May 4.


Cancer immunotherapy has proven remarkably successful through instigation of systemic antitumor T cell responses. Despite this achievement, further advancements are needed to expand the scope of susceptible cancer types and overcome variation in treatment outcomes between patients. Small-molecule drugs targeting defined pathways and/or cells capable of immune modulation are expected to substantially improve efficacy of cancer immunotherapy. Small-molecule drugs possess unique properties compatible with systemic administration and amenable to both extracellular and intracellular targets. These compounds can modify molecular pathways to overcome immune tolerance and suppression towards effective antitumor responses. Here, we provide an overview of how such effects might be achieved by combining immunotherapy with conventional and/or new small-molecule chemotherapeutics.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use
  • Humans
  • Immune Tolerance
  • Immunotherapy*
  • Neoplasms* / therapy
  • Small Molecule Libraries* / therapeutic use
  • T-Lymphocytes / immunology


  • Antineoplastic Agents
  • Small Molecule Libraries