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.