Clinical pharmacokinetics and pharmacodynamics of linagliptin.

Clinical Pharmacokinetics
Ulrike Graefe-ModyChristian Friedrich

Abstract

Linagliptin is an orally active small-molecule inhibitor of dipeptidyl peptidase (DPP)-4, which was first licensed in the US, Europe, Japan and other territories in 2011 to improve glycaemic control in adults with type 2 diabetes mellitus. Linagliptin is the first and thus far the only DPP-4 inhibitor, and oral antihyperglycaemic drug in general, to be approved as a single-strength once-daily dose (5 mg). Compared with other available DPP-4 inhibitors, linagliptin has a unique pharmacokinetic/pharmacodynamic profile that is characterized by target-mediated nonlinear pharmacokinetics, concentration-dependent protein binding, minimal renal clearance and no requirements for dose adjustment for any intrinsic or extrinsic factor. After single or multiple oral doses of 1-10 mg, linagliptin displays less than dose-proportional increases in maximum plasma concentration (C(max)) and area under the plasma concentration-time curve (AUC). Linagliptin is rapidly absorbed after oral administration, with C(max) occurring after approximately 90 minutes, and reaches steady-state concentrations within 4 days. With the therapeutic dose, steady-state C(max) (11-12 nmol/L) and AUC (∼150 nmol · h/L) are approximately 1.3-fold greater than after a si...Continue Reading

References

Nov 1, 1973·The Journal of Clinical Endocrinology and Metabolism·J DupreJ C Brown
Aug 2, 2003·Critical Reviews in Clinical Laboratory Sciences·Anne-Marie LambeirIngrid De Meester
May 15, 2007·Gastroenterology·Laurie L Baggio, Daniel J Drucker
Apr 22, 2008·Diabetes, Obesity & Metabolism·B F BurkeyJ E Foley
Jun 12, 2009·Nutrition, Metabolism, and Cardiovascular Diseases : NMCD·M MonamiE Mannucci
Jun 30, 2009·Biopharmaceutics & Drug Disposition·Holger FuchsAndreas Greischel
Nov 10, 2009·Diabetes Research and Clinical Practice·J E ShawP Z Zimmet
Jan 21, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Stefan BlechKlaus Wagner
May 26, 2010·International Journal of Clinical Pharmacology and Therapeutics·U Graefe-ModyK A Dugi
Sep 30, 2010·International Journal of Clinical Pharmacology and Therapeutics·E U Graefe-ModyK A Dugi
Feb 11, 2011·British Journal of Clinical Pharmacology·Arne RingKlaus A Dugi
Feb 23, 2011·European Journal of Drug Metabolism and Pharmacokinetics·C FriedrichH-J Woerle
Apr 2, 2011·Endocrine Practice : Official Journal of the American College of Endocrinology and the American Association of Clinical Endocrinologists·Nancy D Perrier
May 6, 2011·Diabetes Care·Simona Cernea, Itamar Raz
May 6, 2011·International Journal of Clinical Pharmacology and Therapeutics·E U Graefe-ModyH-J Woerle

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Citations

Nov 29, 2012·Current Diabetes Reports·Ashley TherasseMark E Molitch
Sep 21, 2013·Medical Molecular Morphology·Thomas KleinHiroyuki Yoneyama
Jun 12, 2013·Postgraduate Medicine·George Grunberger
Feb 5, 2013·Expert Opinion on Drug Metabolism & Toxicology·André J Scheen
Feb 21, 2013·Expert Opinion on Drug Safety·André J Scheen
Dec 10, 2014·Expert Opinion on Drug Safety·Sri Harsha Tella, Marc S Rendell
Dec 18, 2012·Expert Opinion on Drug Safety·Stephanie Aleskow SteinStephen N Davis
Apr 22, 2014·Expert Opinion on Drug Metabolism & Toxicology·Theodosios D FilippatosMoses S Elisaf
Nov 2, 2014·Clinical and Experimental Pharmacology & Physiology·Zhi-Xu HeShu-Feng Zhou
Jul 16, 2015·Clinical and Experimental Pharmacology & Physiology·Xiao-Wu ChenShu-Feng Zhou
Feb 18, 2014·European Journal of Medicinal Chemistry·Bhumika D Patel, Manjunath D Ghate
Sep 30, 2016·Postgraduate Medicine·Stuart A RossMaximilian von Eynatten
Nov 14, 2016·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·M RuscicaN Mitro
Jan 24, 2019·Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences·Maryam RameshradHossein Hosseinzadeh
Dec 10, 2013·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Tomohiro HondaTakashi Izumi
Jun 5, 2020·Angewandte Chemie·Xiaojun ZengWei Liu
Feb 5, 2019·Journal of Clinical Pharmacy and Therapeutics·Jones Chun Man ChanBrian Tomlinson
Apr 5, 2019·Journal of Analytical Methods in Chemistry·Raquel Balestri Heleno FerreiraClésio Soldateli Paim
Jan 1, 2013·Expert Review of Endocrinology & Metabolism·Thomas Forst, Andreas Pfützner
Sep 16, 2020·Nature Reviews. Endocrinology·Carolyn F Deacon
Sep 13, 2019·Expert Opinion on Drug Metabolism & Toxicology·Maria Del Mar GutierrezPere Domingo

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