1. Small Molecule Kinase Inhibitor Drugs (1995–2021): Medical Indication, Pharmacology, and Synthesis
- Author
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Ayala-Aguilera, Cecilia C., Valero, Teresa, Lorente-Macías, Álvaro, Baillache, Daniel J., Croke, Stephen, and Unciti-Broceta, Asier
- Subjects
0303 health sciences ,United States Food and Drug Administration ,Chemistry ,Kinase ,Drug discovery ,Antineoplastic Agents ,Pharmacology ,Small molecule ,United States ,3. Good health ,Small Molecule Libraries ,03 medical and health sciences ,0302 clinical medicine ,Neoplasms ,030220 oncology & carcinogenesis ,Drug Discovery ,Humans ,Molecular Medicine ,Kinase activity ,Drug Approval ,Protein Kinase Inhibitors ,030304 developmental biology - Abstract
The central role of dysregulated kinase activity in the etiology of progressive disorders, including cancer, has fostered incremental efforts on drug discovery programs over the last 40 years. As a result, kinase inhibitors are today one of the most important classes of drugs. The FDA approved 72 small molecule kinase inhibitor drugs until Aug 2021, and additional inhibitors were approvedby other regulatory agencies during that time. To complement the published literature on clinical kinase inhibitors, we have prepared a review that recaps this large dataset into an accessible format for the medicinal chemistry community. Along with the therapeutic and pharmacological properties of each kinase inhibitor approved across the world until 2020, we provide the synthesisroutes originally used during the discovery phase, many of which were only available in patent applications. In the last section, we also provide an update on kinase inhibitor drugs approved in2021.
- Published
- 2021
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