ARTICLE - PHARMACOKINETICS OF FLUCONAZOLE, KETOCONAZOLE AND TOFACITINIB IN HEALTHY SUBJECTS

Co-administration of moderate to potent CYP3A4 inhibitors is likely to increase the systemic exposure of tofacitinib and thus may warrant dosage adjustments or restrictions

09/02/2015 - 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

Evaluation of the effect of fluconazole and ketoconazole on the pharmacokinetics of tofacitinib in healthy adult subjects

Gupta, P., Chow, V., Wang, R., Kaplan, I., Chan, G., Alvey, C., Ni, G., Ndongo, M.-N., LaBadie, R. R. and Krishnaswami, S

Clinical Pharm in Drug Dev, 3: 72–77. doi: 10.1002/cpdd.71

Find this article here

RECENT NEWS | ARCHIVE