Effect of saxagliptin on the pharmacokinetics of the active components of Ortho‐Cyclen®, a combined oral contraceptive containing ethinyl estradiol and norgestimate,in healthy women

Saxagliptin (Onglyza?) is a dipeptidyl peptidase‐4 (DPP4) inhibitor for treating type 2 diabetes mellitus. This open‐label, randomized, two‐way crossover study in 20 healthy female subjects investigated the effect of saxagliptin on the pharmacokinetics (PK) of the active components of a combined oral contraceptive (COC). Subjects received either COC (Ortho‐Cyclen^®) once daily (QD) for 21 days, then 5 mg saxagliptin QD + COC QD for 21 days, or vice versa. Coadministration of saxagliptin and COC did not alter the steady‐state PK of the primary active oestrogen (ethinyl estradiol) or progestin (norelgestromin) COC components. The area under the concentration–time curve (AUC) and peak plasma concentration (C_max) of an active metabolite of norelgestromin (norgestrel) were increased by 13 and 17%, respectively, a magnitude that was not considered clinically meaningful. Coadministration of saxagliptin and COC in this study was generally well‐tolerated. Saxagliptin can be co‐prescribed with an oestrogen/progestin combination for women taking oral contraceptive.