TABLE 1.
FDA-approved kinase inhibitors used in this studya
| Agent (designation) | Drug name | Sponsor | Date of FDA approval | Kinase inhibitorb | Primary target(s) |
|---|---|---|---|---|---|
| Afatinib (Gilotrif) | Tovok | Boehringer Ingelheim | July 2013 | Y | EGFR, ErbB2/4 |
| Axitinib (AG013736) | Inlyta | Pfizer | January 2012 | Y | VEGFRs, c-Kit, PDGFRβ |
| Bosutinib (SKI-606) | Bosulif | Wyeth | September 2012 | Y | BCR-Abl, Src, Lyn, Hck |
| Cabozantinib (XL184) | Cometriq | Exelixis | November 2012 | Y | VEGFRs, c-Met, Ret, Kit, TrkB, Flt3, Tie2, Axl |
| Ceritinib (LDK378) | Zykadia | Novartis | April 2014 | Y | ALK, IGF-1R, InsR, ROS1 |
| Crizotinib (PF-02341066) | Xalkori | Pfizer | August 2011 | Y | ALK, c-Met (HGFR), ROS1, MST1R |
| Dabrafenib (6964) | Tafinlar | GlaxoSmithKline | May 2013 | S/T | B-Raf |
| Dasatinib (BM-354825) | Sprycel | Bristol-Myers Squibb | June 2006 | Y | BCR-Abl, Src, Lck, Lyn, Yes, Fyn, c-Kit, EphA2, PDGFRβ |
| Erlotinib (OSI-744) | Tarceva | (OSI)pharmaceuticals | November 2004 | Y | EGFRs |
| Gefitinib (ZD1839) | Iressa | AstraZeneca | May 2003 | Y | EGFRs, PDGFR |
| Ibrutinib (PCI-32765) | Imbruvica | Pharmacyclics | November 2013 | Y | BTK |
| Imatinib (STI571) | Gleevec | Novartis | May 2001 | Y | BCR-Abl, c-Kit, PDGFR |
| Lapatinib (GW2016) | Tykerb | GlaxoSmithKline | March 2007 | Y | EGFR, ErbB2 |
| Lenvatinib (E7080) | Lenvima | Eisai | February 2015 | Y | VEGFRs, PDGFRs, FGFRs, Kit, RET |
| Nilotinib (AMN107) | Tasigna | Novartis | October 2007 | Y | BCR-Abl, PDGFR, Kit, DDR1 |
| Nintedanib (BIBF1120) | Ofev | Boehringer Ingelheim | October 2014 | Y | VEGFRs, FGFRs, PDGFRs, Lck |
| Palbocicnib (PD-0332991) | Ibrance | Pfizer | February 2015 | S/T | CDK4, CDK6 |
| Pazopanib (GW-786034) | Votrient | GlaxoSmithKline | October 2009 | Y | VEGFRs, PDGFRs, FGDRs, c-Kit, Lck, Fms, Itk |
| Ponatinib (AP24534) | Iclusig | Ariad | December 2012 | Y | BCR-Abl, PDGFRs, VEGFRs, FGFRs, Src, EphR, Kit, RET, Tie2, Flt3 |
| Regorafenib (BAY 73-4506) | Stivarga | Bayer | September 2012 | Y/S/T | VEGFRs, PDGFRs, Kit, RET, Raf-1, Tie2, EphA2 |
| Ruxolitinib (INC424) | Jakafi | Incyte | November 2011 | Y | JAK1/2 |
| Sorafenib (BAY 43-9006) | Nexavar | Bayer | December 2005 | Y/S/T | VEGFRs, PDGFRs, B-Raf, Kit, Flt3, RET, CDK8 |
| Sunitinib (SU11248) | Sutent | Pfizer | January 2006 | Y | VEGFRs, PDGFRs, c-Kit, RET, Flt3 |
| Tofacitinib (CP-690550) | Xeljanz | Pfizer | November 2012 | Y | JAK3 |
| Trametinib (6495) | Mekinist | GlaxoSmithKline | May 2013 | S/T | MEK1/2 |
| Vandetanib (ZD6474) | Caprelsa | AstraZeneca | April 2011 | Y | VEGFRs, EGFRs, RET, Tie2, Brk, EphR |
| Vemurafenib (PLX4043) | Zelboraf | Roche | August 2011 | S/T | Raf |
a
FDA-approved small-molecule kinase inhibitors. More details may be found in reference 97.
b
Inhibiting phosphorylation of tyrosine (Y), serine (S) or threonine (T) residues.