1 min read Drug R&D

Small molecules still hold giant potential in drug discovery

Small molecules still hold giant potential in drug discovery
3D small molecule

Nat Rev Drug Discov 2025 Mar 6.(in press) Tumour-agnostic kinase inhibitors

Author: Jacob J Adashek, Mina Nikanjam, Razelle Kurzrock

PMID: 40050521

DOI: 10.1038/s41573-025-01147-y

  • While the biopharma industry has poured resources into large-molecule therapies, small molecules—especially kinase inhibitors—remain a frontier brimming with untapped potential.

  • Of over 600 kinases identified to date, 90% lack approved drugs, leaving vast opportunities for innovation.

  • Though uncertainties persist about the “druggability” of many kinase targets, their central roles in cancer, inflammation, and other diseases underscore their value.

  • Advances in computational modeling and novel screening tools are now enabling researchers to explore once-intractable kinases.

  • The future of precision medicine hinges not just on size but on smart science—small molecules could redefine therapeutic landscapes where 9 out of 10 kinase targets still await their first breakthrough.

Yan J

Shanghai, China