Drug intelligence / Profile preview

iloprost + sildenafil

Development stage
Preclinical
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Inhalation, Intravenous
01

Overview

Iloprost + sildenafil is a combination of two small-molecule vasodilators used together primarily for the management of pulmonary arterial hypertension (PAH) and in research or clinical contexts for conditions involving ischemia or acute pulmonary hypertension. Iloprost is a synthetic prostacyclin analog that acts as a potent vasodilator, platelet aggregation inhibitor, and cytoprotective agent by agonizing the prostacyclin receptor and other prostaglandin receptors. Sildenafil is a selective phosphodiesterase type 5 inhibitor that increases cyclic GMP levels leading to relaxation of vascular smooth muscle, especially in the pulmonary vasculature. When used together, these agents have demonstrated additive or synergistic effects on pulmonary vasodilation, reduction of pulmonary vascular resistance, and improvement in cardiac output. This combination is most often used when PAH is severe, refractory, or acutely decompensated, particularly in hospital or research settings, and has been investigated for synergy in ischemia-reperfusion injury models and pulmonary hypertension[1][2].

02

Targets

PDE5 (Phosphodiesterase 5A)PTGIR (Prostanoid IP Receptor)PTGER1 (Prostaglandin E Receptor 1)PTGDR2 (Prostaglandin D2 receptor 2)PTGER2 (Prostaglandin E2 receptor EP2)

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