Drug intelligence / Profile preview

esuberaprost

Development stage
Phase 3
Lead developer
United Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Esuberaprost is a single-isomer, orally available small molecule prostacyclin analog developed as an active enantiomer of beraprost. It acts primarily as an agonist of the prostacyclin (IP) receptor on vascular smooth muscle cells and platelets, leading to vasodilation and inhibition of platelet aggregation. Esuberaprost was investigated for the treatment of pulmonary arterial hypertension (PAH), with clinical trials reaching up to Phase 3. Compared to beraprost, esuberaprost demonstrates significantly higher potency in relaxing pulmonary arteries and inhibiting proliferation of pulmonary artery smooth muscle cells—effects that are mediated by both IP receptor activation and nitric oxide pathways. Despite promising pharmacological properties, development for PAH was discontinued after failing to meet efficacy endpoints in late-stage clinical trials[1][2][3][5][6][8].

Other names
esuberaprost sodiumesuberaprost potassium
02

Targets

PTGER3 (Prostaglandin E2 receptor EP3 subtype)PTGIR (Prostanoid IP Receptor)

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