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GSK256073A + niacin
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
GSK256073A is a potent and selective agonist of the hydroxy-carboxylic acid receptor 2 (HCA2), also known as G-protein coupled receptor 109A (GPR109A), developed by GSK. It was designed to mimic the antilipolytic effects of niacin while minimizing the common side effect of flushing. In preclinical and clinical studies, GSK256073 demonstrated similar efficacy to niacin in lowering non-esterified fatty acids (NEFA) and triglycerides but with minimal flushing response[6][8]. Niacin (nicotinic acid) is a B-complex vitamin used at therapeutic doses as a cholesterol-lowering medication; it decreases LDL cholesterol and triglycerides while increasing HDL cholesterol[2][5]. The combination has been studied for its potential to block or reduce niacin-induced flushing by using the HM74A/HCA2 agonist properties of GSK256073A[1].
- Brand names
- NiaspanB-3-50B3-50B 3-50B3-500-GrB-3-500-GrB 3-500-GrEndur-acinHDL BenefitNiacin SR
- Other names
- nicotinic acid
02
Targets
HCAR2 (Hydroxycarboxylic acid receptor 2)
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