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. Author manuscript; available in PMC: 2014 May 1.
Published in final edited form as: Curr Probl Cancer. 2013 May-Jun;37(3):110–144. doi: 10.1016/j.currproblcancer.2013.06.001

Table 7.

Major adverse reactions associated with KIs are listed. Incidence is from across all FDA indications of each KI using the highest percent reported and landmark studies that lead to KI approval by FDA. Percent may be different from smaller phase 2 studies.

Kinase Inhibitor Black Box Warning Fatal Hepatic Failure Grade 3/4 AST/ALT Grade 3/4 Total Bilirubin Any Grade QT Prolongation Grade 3 QT Prolongation Tors ades
Axitinib None <1%
Bosutinib None 7% 1% <10% 0.2%
Cabozantinib Perforation, fistula, or hemorrhage 6% None
Crizotinib None 7% 3.5% 1.3%
Dasatinib None <1% 1% 1%
Erlotinib None 1% NSCLC, 13%) Pancreatic <1% NSCLC 10% Pancreatic
Gefitinib None
Imatinib None 3% 1.1%
Lapatinib Hepatotoxicity Few deaths 5% 4%
Nilotinib QT prologation, torsades 4% 4% 4.1% <1%
Pazopanib Hepatotoxicity 0.2% 12% 3% 2% <1%
Regorafenib Hepatotoxicity 0.3%-0.8% 6% 13%
Ruxolitinib None 1.3%
Sorafenib None Rare
Sunitinib Hepatotoxicity 0.3% 5% 1% <0.1 %
Vandetanib QT prologation, torsades 2% 0% 14% 8% Few cases
Vemurafenib None 2.8% 1.9%
Vismodegib Embryo-fetal death or severe birth defects
Ponatinib Arterial thrombosis Hepatotoxicity 3 fatal cases 8% 1% Mostly ≤20ms changes

Abbreviations: AST, aspartate aminotransferase; ALT, alanine aminotransferase; NSCLC, non-small cell lung carcinoma.