GENERAL NEWS – TOFACITINIB (IMMUNOSUPPRESSANT) AND PITAVASTATIN (LIPID LOWERING AGENT) ADDED TO FUNGAL PHARMACOLOGY

Significant interactions with fluconazole, itraconazole, voriconazole and posaconazole

09/02/2015 - Two new interacting agents have been added to Fungal Pharmacology: Tofacitinib (immunosuppressant: clinically significant interactions with fluconazole, itraconazole, voriconazole and posaconazole) and Pitavastatin (lipid lowering agent; no clinically significant interactions with itraconazole and posaconazole)

Coadministration of fluconazole (400 mg on day 1, 200 mg QD on days 2-7) and tofacitinib (30 mg, single dose on day 5) increased tofacitinib AUC and Cmax by 79% and 27%, respectively, in 12 healthy subjects. In addition, coadministration of ketoconazole (400 mg QD on days 1-3, a strong CYP3A4 inhibitor) and tofacitinib (10 mg, single dose on day 3) increased tofacitinib AUC and Cmax by 103% and 16%, respectively, in 12 healthy subjects. Tofacitinib half-life increased by 1h both with fluconazole and ketoconazole.

Coadministration of itraconazole (200 mg on days 5 - 9) and pitavastatin (4 mg, single dose on days 1 and 8) decreased pitavastatin AUC(0-tau) and Cmax by 23% and 22%, respectively, in 18 healthy subjects. In addition, the safety and tolerability of pitavastatin was not affected by coadministration with itraconazole. The authors concluded pitavastatin was not a substrate of CYP3A4.

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