Kinases have become an extremely important molecular target for a range of therapeutic targets. The kinase inhibitors are a large group of unique and potent antineoplastic agents which specifically target protein kinases that are altered in cancer cells and that account for some of their abnormal growth. Here are the small molecule kinase inhibitors approved by the FDA in 2021.
1. Tepmetko (tepotinib)
On February 3, 2021, the Food and Drug Administration granted accelerated approval to tepotinib (Tepmetko, EMD Serono Inc.) for adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations. Tepotinib is an orally bioavailable inhibitor of MET tyrosine kinase with potential antineoplastic activity. Tepotinib selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways, which may induce apoptosis in tumor cells overexpressing this kinase.
2. Ukoniq(umbralisib)
On February 5, 2021, the Food and Drug Administration granted accelerated approval to umbralisib (Ukoniq, TG Therapeutics), a kinase inhibitor including PI3K-delta and casein kinase CK1-epsilon, for the following indications:
(1) Adult patients with relapsed or refractory marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen.
(2) Adult patients with relapsed or refractory follicular lymphoma (FL) who have received at least three prior lines of systemic therapy.
3. Cosela (trilaciclib)
On February 12, 2021, the Food and Drug Administration granted accelerated approval to Cosela (trilaciclib) as the first therapy in its class to reduce the frequency of chemotherapy-induced bone marrow suppression in adults receiving certain types of chemotherapy for extensive-stage (when the cancer has spread beyond the lungs) small cell lung cancer. Trilaciclib is a small molecule, competitive inhibitor of cyclin dependent kinases 4 and 6 (CDK4/6), with potential antineoplastic and chemoprotective activities.
4. Truseltiq (infigratinib)
On May 28, 2021, the Food and Drug Administration granted accelerated approval to infigratinib (Truseltiq, QED Therapeutics, Inc.), a kinase inhibitor for adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.
5. Lumakras(sotorasib)
On May 28, 2021, the Food and Drug Administration granted accelerated approval to sotorasib (Lumakras, Amgen, Inc.), a RAS GTPase family inhibitor, for adult patients with KRAS G12C mutated-locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy.
6. Rezurock (belumosudil)
On July 16, 2021, the Food and Drug Administration approved belumosudil (Rezurock, Kadmon Pharmaceuticals, LLC), a kinase inhibitor, for adult and pediatric patients 12 years and older with chronic graft-versus-host disease (chronic GVHD) after failure of at least two prior lines of systemic therapy. Belumosudil is a Rho-associated coiled-coil-containing protein kinase (ROCK) inhibitor.
7. Exkivity (mobocertinib)
On September 15, 2021, the Food and Drug Administration granted accelerated approval to mobocertinib (Exkivity, Takeda Pharmaceuticals, Inc.) for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy.
8. Scemblix (asciminib)
On October 29, 2021, the Food and Drug Administration granted accelerated approval to asciminib (Scemblix, Novartis AG) for patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors (TKIs), and approved asciminib for adult patients with Ph+ CML in CP with the T315I mutation.