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. 2022 Oct 12;54(10):1670–1694. doi: 10.1038/s12276-022-00864-3

Table 1.

Classes of selected kinase inhibitors26,28.

Class Mechanism of action Examples
Type I Binding in the ATP-binding pocket of the active conformation of the enzyme (DFG-in and αC-helix-in) cabozantinib, ceritinib, gefitinib, palbociclib, pazopanib, ponatinib, ruxolitinib, tofacitinib

Type I1/2

Type II

Binding in the ATP-binding pocket of the inactive conformation of the enzyme (type I1/2: DFG-Asp in; type II: DFG-Asp out) dasatinib, imatinib, lapatinib, lenvatinib, nilotinib, regorafenib, sorafenib, sunitinib, vemurafenib

Type III

Type IV

Allosteric inhibitors binding to a site in the kinase domain either next to the ATP-binding pocket or remote from the ATP-binding pocket trametinib, everolimus, sirolimus, temsirolimus
Type V Bivalent inhibitors that bind two different portions of the kinase lobe lenvatinib28
Type VI Covalent inhibitors afatinib, ibrutinib

In Ref. 26, lenvatinib is classified as a type I1/2 inhibitor.