Tazatred Drug Interactions

Drugs That May Increase Dasatinib Plasma Concentrations: CYP3A4 Inhibitors: Dasatinib is a CYP3A4 substrate. In a study of 18 patients with solid tumors, 20-mg DASATINIB once daily coadministered with 200 mg of ketoconazole twice daily increased the dasatinib Cmax and AUC by four- and five-fold, respectively. Concomitant use of DASATINIB and drugs that inhibit CYP3A4 may increase exposure to dasatinib and should be avoided. In patients receiving treatment with DASATINIB, close monitoring for toxicity and a DASATINIB dose reduction should be considered if systemic administration of a potent CYP3A4 inhibitor cannot be avoided [see Dosage & Administration].
Drugs That May Decrease Dasatinib Plasma Concentrations: CYP3A4 Inducers: When a single morning dose of DASATINIB was administered following 8 days of continuous evening administration of 600 mg of rifampin, a potent CYP3A4 inducer, the mean Cmax and AUC of dasatinib were decreased by 81% and 82%, respectively. Alternative agents with less enzyme induction potential should be considered. If DASATINIB must be administered with a CYP3A4 inducer, a dose increase in DASATINIB should be considered [see Dosage & Administration].
Antacids: Nonclinical data demonstrate that the solubility of dasatinib is pH dependent. In a study of 24 healthy subjects, administration of 30 mL of aluminum hydroxide/magnesium hydroxide 2 hours prior to a single 50-mg dose of DASATINIB was associated with no relevant change in dasatinib AUC; however, the dasatinib Cmax increased 26%. When 30 mL of aluminum hydroxide/magnesium hydroxide was administered to the same subjects concomitantly with a 50-mg dose of DASATINIB, a 55% reduction in dasatinib AUC and a 58% reduction in Cmax were observed. Simultaneous administration of DASATINIB with antacids should be avoided. If antacid therapy is needed, the antacid dose should be administered at least 2 hours prior to or 2 hours after the dose of DASATINIB.
H2 Antagonists/Proton Pump Inhibitors: Long-term suppression of gastric acid secretion by H2 antagonists or proton pump inhibitors (eg, famotidine and omeprazole) is likely to reduce dasatinib exposure. In a study of 24 healthy subjects, administration of a single 50-mg dose of DASATINIB 10 hours following famotidine reduced the AUC and Cmax of dasatinib by 61% and 63%, respectively. The concomitant use of H2 blockers or proton pump inhibitors with DASATINIB is not recommended. The use of antacids should be considered in place of H2 blockers or proton pump inhibitors in patients receiving DASATINIB therapy.
Drugs That May Have Their Plasma Concentration Altered By Dasatinib: CYP3A4 Substrates: Single-dose data from a study of 54 healthy subjects indicate that the mean Cmax and AUC of simvastatin, a CYP3A4 substrate, were increased by 37% and 20%, respectively, when simvastatin was administered in combination with a single 100-mg dose of DASATINIB. Therefore, CYP3A4 substrates known to have a narrow therapeutic index, such as alfentanil, astemizole, terfenadine, cisapride, cyclosporine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus, or ergot alkaloids (ergotamine, dihydroergotamine) should be administered with caution in patients receiving DASATINIB.