Table 2.

Small-molecule KIs approved for oncology indications

DrugInitial indicationInitial date of approvalDose-related PMR or PMC
ImatinibCML05/10/2001No
GefitinibNSCLC05/05/2003No
ErlotinibNSCLC11/18/2004Yes
SorafenibRCC12/20/2005Yes
SunitinibRCC/gastrointestinal stromal tumor01/26/2006No
DasatinibCML06/28/2006No
TemsirolimusRCC03/30/2007No
LapatinibBreast cancer (HER2+)05/13/2007No
NilotinibCML10/29/2007No
EverolimusRCC03/30/2009No
PazopanibRCC10/19/2009No
VandetanibMedullary thyroid cancer04/06/2011Yes
VemurafenibMelanoma (with BRAF V600 mutation)08/17/2011No
CrizotinibNSCLC (with ALK fusion)08/26/2011No
RuxolitinibMyelofibrosis11/16/2011No
AxitinibRCC01/27/2012No
BosutinibCML09/04/2012No
RegorafenibColorectal cancer09/27/2012No
CabozantinibMedullary thyroid cancer11/29/2012Yes
PonatinibCML12/14/2012Yes
DabrafenibMelanoma (with BRAF V600 mutation)05/29/2013No
TrametinibMelanoma (with BRAF V600 mutation)05/29/2013No
AfatinibNSCLC [with EGFR exon 19 deletions or exon 21 substitution (L858R) mutations]07/12/2013No
IbrutinibMantle cell lymphoma02/12/2014No
CeritinibNSCLC (with ALK fusion)04/29/2014Yes
IdelalisibChronic lymphocytic leukemia07/23/2014Yes
PalbociclibBreast cancer (ER/PR+)02/03/2015No
LenvatinibDifferentiated thyroid cancer02/13/2015Yes
CobimetinibMelanoma (with BRAF V600 mutation)11/10/2015No
OsimertinibNSCLC (with EGFR T790M mutation)11/13/2015No
AlectinibNSCLC (with ALK fusion)12/11/2015No
  • Abbreviations: ALK, anaplastic lymphoma kinase; CML, chronic myelogenous leukemia; ER, estrogen receptor; NSCLC, non–small cell lung cancer; PR, progesterone receptor; RCC, renal cell carcinoma.