FFAR1

Synonyms

FFAR1, Free Fatty Acid Receptor 1, G-Protein Coupled Receptor 40, GPR40, G Protein-Coupled Receptor 40, GPCR40, FFA1R,

Description

Free fatty acid receptor 1 (FFA1), also known as GPR40, is a class A G-protein coupled receptor that in humans is encoded by the FFAR1 gene.G-protein coupled receptor for medium and long chain saturated and unsaturated fatty acids that plays an important role in glucose homeostasis. Fatty acid binding increases glucose-stimulated insulin secretion, and may also enhance the secretion of glucagon-like peptide 1 (GLP-1). May also play a role in bone homeostasis; receptor signaling activates pathways that inhibit osteoclast differentiation. Ligand binding leads to a conformation change that triggers signaling via G-proteins that activate phospholipase C, leading to an increase of the intracellular calcium concentration. Seems to act through a G(q) and G(i)-mediated pathway. Mediates the anti-inflammatory effects of omega-3 polyunsaturated fatty acids (PUFAs) via inhibition of NLRP3 inflammasome activation.

KO Status

F0

Drug Information

Launched drugs: 5
Drugs in clinical trials: 0
Latest Research Phase:Phase 3 Clinical

Drug Name

Code

Phase

Company

Indications

Clinical Trials

Setogepram

PBI-4050

Phase 3 Clinical

Prometic Life Sciences

Cystic Fibrosis, Diabetes Mellitus, Type 2, Idiopathic Pulmonary Fibrosis, Metabolic Syndrome, Alstrom Syndrome, Diabetes Mellitus

HOB-047

HD-6277, HOB-047, GPR-6277, HDNO-1605

Phase 1 Clinical

Hyundai Pharmaceutical

Diabetes Mellitus, Type 2

CPL-207-280

CPL-207280, CPL-207-280

Phase 1 Clinical

Celon Pharma

Diabetes Mellitus, Type 2

PBI-4547

PBI-4547

Phase 1 Clinical

Prometic Life Sciences

Non-alcoholic Fatty Liver Disease, Liver Cirrhosis, Obesity, Diabetes Mellitus

Fuglifam

Phase 1 Clinical

Jiangsu Hengrui Medicine Co Ltd

Diabetes Mellitus, Type 2

AMG-837 (free acid)

AMG-837 (free acid)

Pending

Amgen Inc

Diabetes Mellitus, Type 2

P-11187

P-11187

Pending

Piramal Phytocare

Diabetes Mellitus, Type 2, Overweight

LY-2922470

LY-2922470

Pending

Eli Lilly And Company

Diabetes Mellitus, Type 2

MK-8666

MK-8666

Pending

Merck Sharp & Dohme Corp

Diabetes Mellitus, Type 2

LY-2922083

LY-2922083

Pending

Eli Lilly And Company

Diabetes Mellitus, Type 2

Fasiglifam

TAK-875

Discontinued

Takeda Pharmaceutical Co Ltd

Diabetes Mellitus, Type 2, Cardiovascular Diseases, Renal Insufficiency, Chronic, Diabetes Mellitus

JTT-851

JTT-851

Discontinued

Japan Tobacco

Diabetes Mellitus, Type 2

ASP-4178

ASP-4178, AS-2034178

Discontinued

Astellas Pharma Inc

Diabetes Mellitus, Type 2

LY-2881835

LY-2881835

Discontinued

Eli Lilly And Company

Diabetes Mellitus, Type 2