Iloprost

DB01088ApprovedInvestigationalSmall moleculeProstacyclin Analogues

Iloprost is a synthetic prostacyclin analog used to treat pulmonary arterial hypertension (PAH) and frostbites. Iloprost is an analog of prostacyclin (PGI2; epoprostenol), an endogenous prostanoid mainly produced in the vascular endothelium.

Mechanism: In pulmonary arterial hypertension, endothelial vasoactive mediators such as nitric oxide and prostacyclin are released to induce vasoconstriction. Iloprost mimics the biological actions of prostacyclin, a short-lived prostanoid and potent vasodilator mainly produced in the vascular endothelium.
The exact mechanism of iloprost in cytoprotection has not been fully elucidated; however, it is proposed that iloprost decreases catecholamine outflow from sympathetic nerve terminals, preserves mitochondrial function, and reduces oxidative stress. Decreased neutrophil accumulation and membrane stabilization have also been suggested.
Curator reviewed · 3 references
Primary indication: Inhaled iloprost solution is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve a composite endpoint consisting of exercise tolerance, symptoms (NYHA Class), and lack of deterioration.Curator reviewed · 3 structured indications
Formula / weight: C₂₂H₃₂O₄ · 360.494 g/mol (avg)
First approval: United States, 2005 · European Union, 2016
Also known as: (5E)-[3aS,4R,5R,6aS)-5-Hydroxy-4-[(1E)-(3S,4RS)-3-hydroxy-4-methyloct-1-en-6-ynyl]-hexahydropentalen-2(1H)-ylidene]pentanoic acid · (E)-(3aS, 4R, 5R, 6aS)-hexahydro-5-hydroxy-4-[(E)-(3S,4RS) 3-hydroxy-4-methyl-1-octen-6-ynyl]-Δ2(1H),Δ-pentalenevaleric acid · PENTANOIC ACID, 5-((3AS,4R,5R,6AS)-HEXAHYDRO-5-HYDROXY-4-((1E,3S)-3-HYDROXY-4-METHYL-1-OCTEN-6-YNYL)-2(1H)-PENTALENYLIDENE)-, (5E)-
Code names: ZK-00036374 · ZK-36374
Brand names: Aurlumyn
Ventavis