Anti-Cancer Drugs Targeting Protein Kinases Approved by FDA in 2020

Cancers are a large group of diseases that mostly emerge because of the uncontrollable action of many different genes in human cells [...].

decision was made relying on results from the FIGHT-202 (NCT02924376) multicenter, openlabel, single-arm trial that enrolled 107 participants with locally advanced or metastatic cholangiocarcinoma with an FGFR2 fusion or rearrangement who had received prior treatment and failed it [14].
Capmatinib (INC280) (brand name Tabrecta) (Figure 1b) was approved by the FDA on May 5, 2020, for the treatment of metastatic non-small cell lung cancer (NSCLC) harboring exon 14 mutations in the MET receptor tyrosine kinase (also known as hepatocyte growth factor receptor). Capmatinib is used as an inhibitor of the human MET receptor kinase. The decision was made relying on results from the GEOMETRY mono-1 trial (NCT02414139), a multicenter, non-randomized, open-label, multicohort study enrolling 334 participants with metastatic NSCLC with confirmed MET exon 14 skipping [15].
Selpercatinib (LOXO-292) (brand name Retevmo) (Figure 1b) was approved by the FDA on May 8, 2020, for the treatment of non-small cell lung cancer, metastatic medullary thyroid cancer or advanced or metastatic thyroid cancer caused by an abnormal RET gene. It is used as an inhibitor of the human RET receptor kinase. The decision was made relying on results from the LIBRETTO-001 clinical trial (NCT03157128) of 702 patients 15-92 years old with certain cancers caused by abnormal RET gene expression [16]. Ripretinib (DCC-2618) (brand name Qinlock) (Figure 1b) was approved by the FDA on May 15, 2020, for the treatment of advanced GIST patients previously treated with imatinib, sunitinib, and regorafenib. It is used as an inhibitor of the human PDGFRA and KIT receptor kinases, usually mutated in GIST. The decision was made relying on results from INVICTUS (NCT03353753), an international, multicenter, randomized, double-blind, placebo-controlled clinical trial that enrolled 129 participants with GIST. [17].
Pralsetinib (BLU-667) (brand name Gavreto) (Figure 1b) was approved by the FDA on September 4, 2020, for the treatment of thyroid cancer, non-small cell lung cancer, and some other tumors. It is used as an inhibitor of the human RET receptor kinase. The decision was made relying on results from the ARROW clinical trial (NCT03037385), which included 220 patients 26-87 years old with NSCLC caused by abnormal RET genes [18].
Margetuximab (brand name Margenza) was approved by the FDA on December 16, 2020, for the treatment of HER2-positive breast cancer. It is a chimeric IgG monoclonal antibody medication against HER2 receptor tyrosine kinase. The decision was made based on evidence from a clinical trial (NCT02492711) of 536 patients 27 to 86 years old with HER2positive metastatic breast cancer who had been previously treated for their metastatic disease [19].
Current progress in the field of small-molecule inhibitors of kinases has led to the development of a number of compounds, with various choices for each target molecule, as well as antitumor potencies and specificity for different types/stages of cancers. On the other hand, there are already a lot of antibodies targeting kinases available. Nevertheless, there is still ample room for additional development. Hopefully, there will be a lot of new anti-kinase drugs that can be used either as monotherapy or combined with other anti-cancer medications in the future.