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

Triple negative breast cancer (TNBC) is the most aggressive subtype of breast cancer, but an effective targeted therapy has not been wellestablished 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.

Automated summary

TNBC, the most aggressive subtype of breast cancer, lacks effective targeted therapy. Novel small-molecule drugs targeting specific molecular characteristics of TNBC may be a promising intervention, but face challenges. Emerging strategies such as dual-target drugs, drug repurposing, and combination strategies offer new insights for improving TNBC therapeutics.