Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update
Because of the dysregulation of protein kinase activity in lots of illnesses including cancer, this enzyme family members have become probably the most important drug targets these days. You will find 72 Food and drug administration-approved therapeutic agents that concentrate on about 24 different protein kinases and three of those drugs were approved in 2022. From the approved drugs, twelve target protein-serine/threonine protein kinases, four are directed against dual specificity protein kinases (MEK1/2), 16 block nonreceptor protein-tyrosine kinases, and 40 target receptor protein-tyrosine kinases. The information indicate that 62 of those medicine is prescribed to treat neoplasms (57 against solid tumors including breast, lung, and colon, ten against nonsolid tumors for example leukemia, and 4 against both solid and nonsolid tumors: acalabrutinib, ibrutinib, imatinib, and midostaurin). Four drugs (abrocitinib, baricitinib, tofacitinib, upadacitinib) are utilized to treat inflammatory illnesses (atopic eczema, psoriatic joint disease, rheumatoid arthritis symptoms, Crohn disease, and ulcerative colitis). From the 72 approved drugs, 18 are utilized in treating multiple illnesses. The next three drugs received Food and drug administration approval in 2022 to treat these specified illnesses: abrocitinib (atopic eczema), futibatinib (cholangiocarcinomas), pacritinib (myelofibrosis). All the Food and drug administration-approved medicine is orally effective except for netarsudil, temsirolimus, and trilaciclib. This review summarizes the physicochemical qualities of 72 Food and drug administration-approved small molecule protein kinase inhibitors TAS-120 including lipophilic efficiency and ligand efficiency.