TY - JOUR

T1 - Bile acid sequestrants

T2 - Glucose-lowering mechanisms and efficacy in type 2 diabetes

AU - Hansen, Morten

AU - Sonne, David P.

AU - Knop, Filip K.

N1 - Funding Information: Conflict of Interest M. Hansen has received an unrestricted educational stipend from the Novo Nordisk Foundation. D. P. Sonne has received an unrestricted educational stipend from the Novo Nordisk Foundation. F. K. Knop has received research funding from Sanofi-Aventis Deutschland GmbH and lecture fees from AstraZeneca, Boehringer Ingelheim Pharmaceuticals, Bristol-Myers Squibb, Eli Lilly and Company, Gilead Sciences, Merck Sharp & Dohme, Novo Nordisk, Ono Pharmaceuticals, Sanofi, and Zealand Pharma. He is part of the Advisory Boards of Eli Lilly Denmark, Bristol-Myers Squibb/AstraZeneca, and Zealand Pharma. He has consulted for AstraZeneca, Gilead Sciences, Novo Nordisk, Ono Pharmaceuticals, and Zealand Pharma. He also has 2 pending patents.

PY - 2014/5

Y1 - 2014/5

N2 - Bile acids are synthesized in the liver from cholesterol and have traditionally been recognized for their role in absorption of lipids and in cholesterol homeostasis. In recent years, however, bile acids have emerged as metabolic signaling molecules that are involved in the regulation of lipid and glucose metabolism, and possibly energy homeostasis, through activation of the bile acid receptors farnesoid X receptor (FXR) and TGR5. Bile acid sequestrants (BASs) constitute a class of drugs that bind bile acids in the intestine to form a nonabsorbable complex resulting in interruption of the enterohepatic circulation. This increases bile acid synthesis and consequently reduces serum low-density lipoprotein cholesterol. Also, BASs improve glycemic control in patients with type 2 diabetes. Despite a growing understanding of the impact of BASs on glucose metabolism, the mechanisms behind their glucose-lowering effect in patients with type 2 diabetes remain unclear. This article offers a review of the mechanisms behind the glucose-lowering effect of BASs, and the efficacy of BASs in the treatment of type 2 diabetes.

AB - Bile acids are synthesized in the liver from cholesterol and have traditionally been recognized for their role in absorption of lipids and in cholesterol homeostasis. In recent years, however, bile acids have emerged as metabolic signaling molecules that are involved in the regulation of lipid and glucose metabolism, and possibly energy homeostasis, through activation of the bile acid receptors farnesoid X receptor (FXR) and TGR5. Bile acid sequestrants (BASs) constitute a class of drugs that bind bile acids in the intestine to form a nonabsorbable complex resulting in interruption of the enterohepatic circulation. This increases bile acid synthesis and consequently reduces serum low-density lipoprotein cholesterol. Also, BASs improve glycemic control in patients with type 2 diabetes. Despite a growing understanding of the impact of BASs on glucose metabolism, the mechanisms behind their glucose-lowering effect in patients with type 2 diabetes remain unclear. This article offers a review of the mechanisms behind the glucose-lowering effect of BASs, and the efficacy of BASs in the treatment of type 2 diabetes.

KW - Bile acid sequestrants

KW - Glucose-lowering mechanisms

KW - Glycemic control

KW - Mechanism of action

KW - Resins

KW - Type 2 diabetes

U2 - 10.1007/s11892-014-0482-4

DO - 10.1007/s11892-014-0482-4

M3 - Review

C2 - 24623198

AN - SCOPUS:84895775124

VL - 14

JO - Current Diabetes Reports

JF - Current Diabetes Reports

SN - 1534-4827

IS - 5

M1 - 482

ER -