Drug intelligence / Profile preview

inositol nicotinate

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Inositol nicotinate is a compound formed from niacin (vitamin B3) and inositol. It is used primarily as a vasodilator and lipid-lowering agent. The drug acts as a source of niacin when hydrolyzed in the body and is associated with reduced flushing compared to other forms of niacin due to its slower breakdown. Its main mechanisms include widening blood vessels (vasodilation), lowering blood levels of fats such as cholesterol and triglycerides by acting on hydroxycarboxylic acid receptor 2 (HCAR2/GPR109A) and hydroxycarboxylic acid receptor 3 (HCAR3/GPR109B), decreasing lipolysis via cAMP reduction in adipocytes. In clinical practice—especially Europe—it has been prescribed for peripheral vascular diseases such as intermittent claudication and Raynaud’s phenomenon. Other uses include high cholesterol management and improving symptoms related to poor circulation[1][2][3][5].

Brand names
HexopalNiacin NFHexolipErgovasInohexEcasXantirinGrinotelCalmigen ForteHrb PlusBipoxim
Other names
no-flush niacinmeso-inositol hexanicotinate
02

Targets

HCAR2 (Hydroxycarboxylic acid receptor 2)HCAR3 (Hydroxycarboxylic acid receptor 3)

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