title: 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.
abstract: 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 (Cmax) 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.
authors: Discovery Medicine and Clinical Pharmacology, Bristol-Myers Squibb Company (BMS), Princeton, NJ, USA.
authors: V V
authors: VV
authors: Upreti
authors: C B
authors: CB
authors: Hsiang
authors: L
authors: L
authors: Li
authors: X
authors: X
authors: Xu
authors: F P
authors: FP
authors: LaCreta
authors: D W
authors: DW
authors: Boulton
mesh_terms: D000218:Adamantane / Q000031:analogs & derivatives* / Q000494:pharmacology; D000328:Adult; D003277:Contraceptives, Oral, Combined / Q000493:pharmacokinetics*; D003280:Contraceptives, Oral, Synthetic / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D004151:Dipeptides / Q000494:pharmacology*; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000494:pharmacology*; D004338:Drug Combinations; D004347:Drug Interactions; D004997:Ethinyl Estradiol / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D009644:Norgestrel / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D016896:Treatment Outcome
chemical_list: D003277:Contraceptives, Oral, Combined; D003280:Contraceptives, Oral, Synthetic; D004151:Dipeptides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D004338:Drug Combinations; C109079:norgestimate, ethinyl estradiol drug combination; D009644:Norgestrel; D004997:Ethinyl Estradiol; C502994:saxagliptin; D000218:Adamantane