Pharmacokinetics, pharmacodynamics and clinical efficacy of dapagliflozin for the treatment of type 2 diabetes

Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):125-37. doi: 10.1517/17425255.2015.986457. Epub 2014 Nov 24.

Abstract

Introduction: Dapagliflozin (DAPA) (Farxiga or Forxiga) is a sodium glucose cotransporter 2 (SGLT2) inhibitor approved for type 2 diabetes mellitus(T2DM) treatment.

Areas covered: The review focuses on the pharmacokinetics (PK), pharmacodynamics(PD) and clinical studies published on DAPA. The authors searched PubMed database for English language studies describing DAPA characteristics and use in T2DM subjects published through June 2014.

Expert opinion: DAPA exhibits favorable PK and PD properties and is effective in reducing glycemic levels. In addition, DAPA shows beneficial/neutral effects on other risk factors contributing to T2DM metabolic control. Increased risk of genital and urinary infections and episodes of volume depletion represent the major concerns for its use. FDA requires additional data to assess imbalances in bladder cancer and drug cardiovascular safety. The mechanism of action and the very low risk of drug-drug interaction make it an ideal drug for rapidly reducing glucotoxicity and restoring clinical response to other antidiabetic drugs.

Keywords: SGLT2 inhibitors; dapagliflozin; kidney; type 2 diabetes.

Publication types

  • Review

MeSH terms

  • Animals
  • Benzhydryl Compounds / pharmacokinetics
  • Benzhydryl Compounds / therapeutic use*
  • Clinical Trials as Topic / methods
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Glucosides / pharmacokinetics
  • Glucosides / therapeutic use*
  • Humans
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / therapeutic use*
  • Sodium-Glucose Transport Proteins / antagonists & inhibitors*
  • Sodium-Glucose Transport Proteins / metabolism
  • Treatment Outcome

Substances

  • Benzhydryl Compounds
  • Glucosides
  • Hypoglycemic Agents
  • Sodium-Glucose Transport Proteins
  • dapagliflozin