Table 3.

Clinical pharmacokinetic drug-drug interactions.

Drug	Metabolized by	Change in AUC by P450 inhibitors	Change in AUC by P450 inducers	Active metabolite	Tissue Accumulation
Imatinib	CYP3A4/5 (Minor –1A2, 2D6, 2C9, 2C19)	+ 40% with Ket (9)	− 50% with Rif (10)	Yes (15%)	Liver, GB
nilotinib	CYP3A4/5	+ 300% with Ket (19)	− 80% with Rif (19)	No
dasatinib	CYP3A4/5, 1A1 (120) (minor – FMO3, UGT)	+ 480% with Ket (30)	− 80% with Rif (121)	Yes (5%)
gefitinib	CYP3A4/5 (minor – 1A1, 2D6) (59)	+ 60–80% with itraconazole (122)	−80% with Rif (122)		Liver, Lung GB
erlotinib	CYP3A4/5, CYP1A1 (60)	+ 70% with Ket (80)	− 60–80% with Rif (80) − 50–70% in smokers (82)		Liver
lapatinib	CYP3A4/5	+ 360% with Ket (92)	− 70% with CBZ
sorafenib	UGT1A9 (100) (minor CYP3A4/5)	None with Ket (100)		Yes (9–16%)
sunitinib	CYP3A4/5	+ 50% with Ket (123)	− 50% with Rif (123)	Yes (30%)

(Ket) – ketoconazole, (Rif) – rifampicin, (CBZ) – carbamazepine, (GB) – gall bladder