Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions

J Med Chem. 2021 Mar 11;64(5):2382-2418. doi: 10.1021/acs.jmedchem.0c01180. Epub 2021 Mar 2.

Abstract

Triple negative breast cancer (TNBC) is the most aggressive subtype of breast cancer, but an effective targeted therapy has not been well-established so far. Considering the lack of effective targets, where do we go next in the current TNBC drug development? A promising intervention for TNBC might lie in de novo small-molecule drugs that precisely target different molecular characteristics of TNBC. However, an ideal single-target drug discovery still faces a huge challenge. Alternatively, other new emerging strategies, such as dual-target drug, drug repurposing, and combination strategies, may provide new insight into the improvement of TNBC therapeutics. In this review, we focus on summarizing the current situation of a series of candidate small-molecule drugs in TNBC therapy, including single-target drugs, dual-target drugs, as well as drug repurposing and combination strategies that will together shed new light on the future directions targeting TNBC vulnerabilities with small-molecule drugs for future therapeutic purposes.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antibodies / immunology
  • Antibodies / therapeutic use
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials as Topic
  • Drug Combinations
  • Drug Discovery
  • Drug Repositioning
  • Humans
  • Immunologic Factors / chemistry
  • Immunologic Factors / therapeutic use
  • Molecular Targeted Therapy
  • Triple Negative Breast Neoplasms / drug therapy*
  • Triple Negative Breast Neoplasms / immunology
  • Triple Negative Breast Neoplasms / therapy

Substances

  • Antibodies
  • Antineoplastic Agents
  • Drug Combinations
  • Immunologic Factors