Drug intelligence / Profile preview

limaprost

Development stage
Phase 4
Lead developer
Ono Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral
01

Overview

Limaprost (OP-1206) is a synthetic analog of **prostaglandin E1** with structural modifications designed for greater potency and prolonged half-life. It functions primarily as a **potent vasodilator**, increasing blood flow and inhibiting platelet aggregation. Limaprost is **orally active** and is primarily indicated to improve ischemic symptoms such as ulcer, pain, and intermittent claudication; it is also used in chronic lung disease and has shown the ability to lower pulmonary arterial pressure and vascular resistance and enhance cardiac performance. Its mechanism involves prostaglandin E receptor agonism, resulting in vasodilation, antiplatelet activity, and modulation of nerve growth factor expression in vitro. Developed and commercialized mainly in Japan, limaprost alfadex is a formulation utilizing an alpha-cyclodextrin clathrate for improved stability and delivery[1][3][4][5].

Brand names
LimaprostLimaprost alfadex
Other names
17S,20-Dimethyl-trans-delta2-PGE117α,20-dimethyl-δ2-PGE1LimaprostumLimaprostum alpha-cyclodextrin clathrateLimaprost alfadexLIMAPROSTLIMAPROST [JAN]LIMAPROST [MI]LIMAPROST [MART.]LIMAPROST [WHO-DD]Limaprostum (Latin)
02

Targets

PTGER3 (Prostaglandin E2 receptor EP3 subtype)PTGER2 (Prostaglandin E2 receptor EP2)PTGER1 (Prostaglandin E Receptor 1)

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