Table 1.
Approved tyrosine kinase inhibitors in human medicine, 2011–2015 a.
| Drug | Target | Year Approved | Indication |
|---|---|---|---|
| Vandetanib (Caprelsa®) | Flt1, Flt4, KDR, EGFR, Ret | 2011 | MTC |
| Crizotinib (Xalkori®) | ALK, MET, EML4-ALK fusion protein | 2011 | NSCLC |
| Ruxolitinib (Jakafi®/Jakavi®) | JAK1, JAK2 | 2011 | Myelofibrosis |
| Vemurafenib (Zelboraf®) | BRAF | 2011 | Melanoma |
| Bosutinib (Bosulif®) | BCR/ABL1 | 2012 | CML |
| Axitinib (Inlyta®) | Flt1, Flt4, KDR, Kit, PDGF-Rα/β | 2012 | RCC |
| Cabozantinib (Cometriq®) | KDR, Mek | 2012 | MTC |
| Regorafinib (Stivarga®) | KDR, TEK | 2012 | CC, GIST |
| Ponatinib (Iclusig®) | BCR/ABL1 | 2012 | CML, ALL |
| Dabrafenib (Tafinlar®) | BRAF | 2013 | Melanoma |
| Trametinib (Mekinist®) | MEK1, MEK2 | 2013 | Melanoma |
| Afatinib (Gilotrif®) | ERBB2, EGFR | 2013 | NSCLC |
| Ibrutinib (Imbruvica®) | BTK | 2013 | MCL, CLL |
| Tofacitinib (Xeljanz®) | JAK3 | 2013 | Rheumatoid arthritis |
| Idelalisib (Zydelig®) | PI3-K | 2014 | CLL |
| Follicular B-cell NHL | |||
| Ceritinib (Zykadia®) | ALK | 2014 | ALK+ NSCLC |
| Lenvatinib (Lenvima®) | VEGFR2 and VEGFR3 | 2015 | Radioactive iodine-refractory DTC |
| Palbociclib (Ibrance®) | CDK4 and CDK6 | 2015 | Breast carcinoma |
a Abbreviations: ALL, acute lymphoblastic leukemia; CC, colorectal cancer; CML, chronic myelogenous leukemia; DTC, differentiated thyroid cancer; GIST, gastrointestinal stromal tumor; MCL, mantle cell lymphoma; MTC, medullary thyroid carcinoma; NHL, Non-Hodgkin’s lymphoma; NSCLC, non-small-cell lung carcinoma; RCC, renal cell carcinoma.