Sitagliptin, a dipeptidyl peptidase-4 inhibitor, does not affect the pharmacokinetics of ethinyl estradiol or norethindrone in healthy female subjects

Journal of Clinical Pharmacology

Volumn 51, Issue 9, 2011, Pages 1319-1325

  Migoya, Elizabeth ^a   Larson, Patrick ^a   Bergman, Arthur ^a   Miller, Jutta ^a   Johnson Levonas, Amy O ^a   Lasseter, Kenneth C ^b   Wagner, John A ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b Clinical Pharmacology of Miami Inc   (United States)

Author keywords

dipeptidyl peptidase 4 inhibitor; DPP 4; estradiol; norethindrone; pharmacokinetics; Sitagliptin

Indexed keywords

ALBUMIN; CHORIONIC GONADOTROPIN BETA SUBUNIT; ETHINYLESTRADIOL; MESTRANOL PLUS NORETHISTERONE; NORETHISTERONE; PLACEBO; SEX HORMONE BINDING PROTEIN; SITAGLIPTIN;

ADULT; ALBUMIN BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; BODY WEIGHT; COMPARATIVE STUDY; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG EFFECT; DRUG SAFETY; DRUG TOLERABILITY; ELECTROCARDIOGRAM; FEMALE; HEADACHE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; MAXIMUM PLASMA CONCENTRATION; MENSTRUAL CYCLE; MULTIPLE CYCLE TREATMENT; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; SPOTTING; TANDEM MASS SPECTROMETRY; UNSPECIFIED SIDE EFFECT;

ADULT; CONTRACEPTIVES, ORAL, COMBINED; CROSS-OVER STUDIES; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DRUG INTERACTIONS; ETHINYL ESTRADIOL; FEMALE; HUMANS; NORETHINDRONE; PYRAZINES; TRIAZOLES; YOUNG ADULT;

EID: 80051723086     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270010381497     Document Type: Article

References (17)

1. Kim D, Wang L, Beconi M, et al. (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6- dihydro[1,2,4]triazolo[4,3-a]pyrazin -7(8H)-yl]-1-(2,4,5-triflu or ophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes. J Med Chem. 2005 ; 48: 141-151 (Pubitemid 40105255)
2. Bergman AJ, Stevens C, Zhou Y, et al. Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther. 2006 ; 28: 55-72 (Pubitemid 43254990)
3. Herman GA, Bergman A, Liu F, et al. Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006 ; 46: 876-886 (Pubitemid 44050824)
4. Whitehouse Station, NJ: Merck & Co, Inc ; 2007 :
5. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006 ; 368: 1696-1705 (Pubitemid 46048557)
6. Herman GA, Stevens C, Van Dyck K, et al. Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase-IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 2005 ; 78: 675-688 (Pubitemid 41773643)
7. Herman GA, Bergman A, Stevens C, et al. Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes. J Clin Endocrinol Metab. 2006 ; 91: 4612-4619 (Pubitemid 44833446)
8. Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP. Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008 ; 24: 489-496 (Pubitemid 351294398)
9. Herman GA, Bergman A, Wagner JA. Sitagliptin, a DPP-4 inhibitor: an overview of the pharmacokinetic (PK) profile and the propensity for drug-drug interactions (DDI). Diabetologia. 2006 ; 49: 481-482
10. Herman GA, Bergman A, Yi B, Kipnes M. Tolerability and pharmacokinetics of metformin and the dipeptidyl peptidase-4 inhibitor sitagliptin when co-administered in patients with type 2 diabetes. Curr Med Res Opin. 2006 ; 22: 1939-1947 (Pubitemid 44663399)
11. Mistry GC, Bergman AJ, Luo WL, et al. Multiple-dose administration of sitagliptin, a dipeptidyl peptidase-4 inhibitor, does not alter the single-dose pharmacokinetics of rosiglitazone in healthy subjects. J Clin Pharmacol. 2007 ; 47: 159-164 (Pubitemid 46146481)
12. Raritan, NJ: Ortho-McNeil Pharmaceutical, Inc ; 2007 :
13. Hendrix CW, Jackson KA, Whitmore E, et al. The effect of isotretinoin on the pharmacokinetics and pharmacodynamics of ethinyl estradiol and norethindrone. Clin Pharmacol Ther. 2004 ; 75: 464-475 (Pubitemid 38534567)
14. Vincent SH, Reed JR, Bergman AJ, et al. Metabolism and excretion of the dipeptidyl peptidase-4 inhibitor [14C] sitagliptin in humans. Drug Metab Dispos. 2007 ; 35: 533-538 (Pubitemid 46513255)
15. Dunn JF, Nisula BC, Rodbard D. Transport of steroid hormones: binding of 21 endogenous steroids to both testosterone-binding globulin and corticosteroid-binding globulin in human plasma. J Clin Endocrinol Metab. 1981 ; 53: 58-68 (Pubitemid 13245381)
16. Boyd R, Zegarac E, Eldon M, Koup J. Induction of sex hormone binding globulin (SHBG) by a single dose of norethindrone acetate/ethinyl estradiol (NA/EE). Clin Pharmacol Ther. 1997 ; 61: 171 (Pubitemid 127791388)
17. Mandel FP, Geola FL, Lu JK, et al. Biologic effects of various doses of ethinyl estradiol in postmenopausal women. Obstet Gynecol. 1982 ; 59: 673-679 (Pubitemid 12107423)