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10 years into the resurgence of covalent drugs.

Elena De Vita
Published in: Future medicinal chemistry (2020)
In the first decade of targeted covalent inhibition, scientists have successfully reversed the previous trend that had impeded the use of covalent inhibition in drug development. Successes in the clinic, mainly in the field of kinase inhibitors, are existing proof that safe covalent inhibitors can be designed and employed to develop effective treatments. The case of KRASG12C covalent inhibitors entering clinical trials in 2019 has been among the hottest topics discussed in drug discovery, raising expectations for the future of the field. In this perspective, an overview of the milestones hit with targeted covalent inhibitors, as well as the promise and the needs of current research, are presented. While recent results have confirmed the potential that was foreseen, many questions remain unexplored in this branch of precision medicine.
Keyphrases
  • clinical trial
  • drug discovery
  • primary care
  • cancer therapy
  • machine learning
  • drug delivery
  • climate change
  • human health
  • open label
  • phase ii
  • phase iii