Bernd Müller

Synergistic antiplatelet and antithrombotic effects of a prostacyclin analogue (iloprost) combined with a thromboxane antagonist (sulotroban) in guinea pigs and rats

The stable PGI2-analogue iloprost and the TXA2-receptor antagonist sulotroban were investigated for possible cooperative effects on platelet function and experimental thrombus formation in guinea pigs and rats. Iloprost and sulotroban inhibit intravascular platelet aggregation in guinea pigs and rats induced by the stable endoperoxide U 46.619 and collagen, with iloprost being the more potent and (for collagen) more efficacious drug. Combinations of both compounds show synergistic or additive effects on in vivo platelet function. Thrombus formation in rats induced by vascular damage is strongly reduced by combining doses of iloprost and sulotroban (BM 13.177) which given alone are ineffective. These results suggest a cooperative enhancement of antiplatelet and antithrombotic effects for combinations of iloprost and sulotroban. In view of disadvantages of currently used platelet inhibitors this cooperativity may offer a new approach in antiplatelet therapy.

Effects of Iloprost on Arrhythmias and Infarct Size in Rats After Coronary Artery Ligation

Iloprost is a stable, orally active prostacyclin (PGI2) analogue with a pharmacologic profile and activity nearly identical to PGI2 [1,2]. Both PGI2 and Iloprost have been shown in a variety of experimental models to protect acutely ischemic myocardium from functional deterioration, cell enzyme leakage, and ventricular arrhythmias [3–5].

Antithrombotic Profile of Iloprost in Experimental Models of Arterial and Venous Thrombosis

Clinical benefit from treatment with Iloprost in patients suffering from throm-boembolic disorders may arise from well known properties of the drug like inhibition of platelet aggregation, vasorelaxation, cytoprotection and stimulation of the plasma fibrinolytic activity [1–3]. Some, if not all, of these properties could qualify Iloprost as a drug with antithrombotic efficacy.

Schering: Synchronised Drug Development

In the early 90s, Schering divested of two non-pharmaceutical divisions and entered a third division, its plant protection business, into an independent jointventure firm with Hoechst AG/Germany.