Owing to the dysregulation of protein kinase activity in many diseases including cancer, the
protein kinase enzyme family has become one of the most important drug targets in the 21st
century. There are 62 FDA-approved therapeutic agents that target about two dozen different
protein kinases and eight of these were approved in 2020. All of the FDA-approved drugs
are orally effective with the exception of netarsudil (a ROCK1/2 non-receptor protein-
serine/threonine kinase antagonist given as an eye drop for the treatment of glaucoma) and …

Because genetic alterations including mutations, overexpression, translocations, and
dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this
enzyme family is currently the subject of many drug discovery programs in the
pharmaceutical industry. The US FDA approved four small molecule protein kinase
antagonists in 2019; these include entrectinib, erdafitinib, pexidartinib, and fedratinib.
Entrectinib binds to TRKA/B/C and ROS1 and is prescribed for the treatment of solid tumors …

Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most
important drug targets in the past 20 years. The US FDA has approved 48 small molecule
protein kinase inhibitors, nearly all of which are orally effective with the exceptions of
netarsudil (which is given as an eye drop) and temsirolimus (which is given intravenously).
Of the 48 approved drugs, the majority (25) target receptor protein-tyrosine kinases, ten …

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 …

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 21 st century. There
are 72 FDA-approved therapeutic agents that target about two dozen different protein
kinases and three of these drugs were approved in 2022. Of the approved drugs, twelve
target protein-serine/threonine protein kinases, four are directed against dual specificity
protein kinases (MEK1/2), sixteen block nonreceptor protein-tyrosine kinases, and 40 target …