Repositioning Candidate Details

Candidate ID: R0396
Source ID: DB01088
Source Type: approved; investigational
Compound Type: small molecule
Compound Name: Iloprost
Synonyms: Iloprost
Molecular Formula: C22H32O4
SMILES: [H][C@]12C[C@@H](O)[C@H](\C=C\[C@@H](O)C(C)CC#CC)[C@@]1([H])C\C(C2)=C\CCCC(O)=O
Structure:
DrugBank Description: Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It is used to treat pulmonary arterial hypertension (PAH).
CAS Number: 78919-13-8
Molecular Weight: 360.494
DrugBank Indication: Used for the treatment of pulmonary arterial hypertension.
DrugBank Pharmacology: Iloprost is a synthetic analogue of prostacyclin PGI2 that dilates systemic and pulmonary arterial vascular beds. It was shown to affect platelet aggregation, but whether this effect contributes to its vasodilatory action has not been elucidated. There are two diastereoisomers of iloprost and the 4S isomer is reported to exhibit a higher potency in dilating blood vessels compared to the 4R isomer.
DrugBank MoA: Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, such as carbaprostacyclin. Iloprost binds with equal affinity to human prostacyclin (Prostanoid IP) and prostaglandin EP1 receptors. Iloprost constricts the ilium and fundus circular smooth muscle as strongly as prostaglandin E2 (PGE2) itself. Iloprost inhibits the ADP, thrombin, and collagen-induced aggregation of human platelets. In whole animals, iloprost acts as a vasodilator, hypotensive, antidiuretic, and prolongs bleeding time. All of these properties help to antagonize the pathological changes that take place in the small pulmonary arteries of patients with pulmonary hypertension.
Targets: Prostacyclin receptor agonist; Prostaglandin E2 receptor EP1 subtype agonist; cAMP-specific 3',5'-cyclic phosphodiesterase 4A inducer; cAMP-specific 3',5'-cyclic phosphodiesterase 4B inducer; cAMP-specific 3',5'-cyclic phosphodiesterase 4C inducer; cAMP-specific 3',5'-cyclic phosphodiesterase 4D inducer; Tissue-type plasminogen activator other/unknown; Prostaglandin D2 receptor 2 agonist
Inclusion Criteria: Therapeutic strategy associated