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Roskoski R. Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update. Pharmacol Res. 2021;175:106037doi: 10.1016/j.phrs.2021.106037.
Roskoski, R. (2022). Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update. Pharmacological research, 175106037. https://doi.org/10.1016/j.phrs.2021.106037
Roskoski, Robert. "Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update." Pharmacological research vol. 175 (2022): 106037. doi: https://doi.org/10.1016/j.phrs.2021.106037
Roskoski R. Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update. Pharmacol Res. 2022 Jan;175:106037. doi: 10.1016/j.phrs.2021.106037. Epub 2021 Dec 15. PMID: 34921994; PMCID: PMC8691985.
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Pharmacol Res. 2022 Jan;175:106037. doi: 10.1016/j.phrs.2021.106037. Epub 2021 Dec 15.

Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update.

Pharmacological research

Robert Roskoski

Affiliations

  1. Blue Ridge Institute for Medical Research, 3754 Brevard Road, Suite 106, Box 19, Horse Shoe, NC 28742-8814, United States. Electronic address: [email protected].

PMID: 34921994 PMCID: PMC8691985 DOI: 10.1016/j.phrs.2021.106037

Abstract

Owing to the dysregulation of protein kinase activity in many diseases including cancer, this enzyme family has become one of the most important drug targets in the 21st century. There are 68 FDA-approved therapeutic agents that target about two dozen different protein kinases and six of these drugs were approved in 2021. Of the approved drugs, twelve target protein-serine/threonine protein kinases, four are directed against dual specificity protein kinases (MEK1/2), thirteen block nonreceptor protein-tyrosine kinases, and 39 target receptor protein-tyrosine kinases. The data indicate that 58 of these drugs are prescribed for the treatment of neoplasms (49 against solid tumors including breast, lung, and colon, five against nonsolid tumors such as leukemias, and four against both solid and nonsolid tumors: acalabrutinib, ibrutinib, imatinib, and midostaurin). Three drugs (baricitinib, tofacitinib, upadacitinib) are used for the treatment of inflammatory diseases including rheumatoid arthritis. Of the 68 approved drugs, eighteen are used in the treatment of multiple diseases. The following six drugs received FDA approval in 2021 for the treatment of these specified diseases: belumosudil (graft vs. host disease), infigratinib (cholangiocarcinomas), mobocertinib and tepotinib (specific forms of non-small cell lung cancer), tivozanib (renal cell carcinoma), and trilaciclib (to decrease chemotherapy-induced myelosuppression). All of the FDA-approved drugs are orally effective with the exception of netarsudil, temsirolimus, and the newly approved trilaciclib. This review summarizes the physicochemical properties of all 68 FDA-approved small molecule protein kinase inhibitors including lipophilic efficiency and ligand efficiency.

Copyright © 2021 Elsevier Ltd. All rights reserved.

Keywords: Belumosudil (PubChem CID: 11950170); Cabozantinib (PubChem CID: 2510847); Catalytic spine; Hydrophobic interaction; Imatinib (PubChem CID: 5291); Infigratinib (PubChem CID: 53235510); Mobocertinib (PubChem CID: 118607832); Protein kinase inhibitor classification; Protein kinase structure; Regulatory spine; Shell residues; Sorafenib (PubChem CID: 216239); Sunitinib (PubChem CID: 5329102); Tepotinib (PubChem CID: 25171648); Tivozanib (PubChem CID: 9911830); Trilaciclib (PubChem CID: 68029832)

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