Napsagatran [RO 466240], a reversible and highly selective thrombin inhibitor, was in development with Roche for use in myocardial infarction and thrombosis. Napsagatran efficiently inhibits and delays thrombin generation in human coagulating plasma. This reduced thrombin generation might be caused by inhibition of thrombin-mediated feedback reactions during blood coagulation. Ro 46-6240 inhibited clot-bound thrombin three times more potently than fluid-phase thrombin (IC50 19 vs 56 ng/ml) while hirudin was two times (IC50 8 vs 3 ng/ml) and heparin six times (IC50 1,205 vs 200 ng/ml) less active against clot-bound thrombin compared with fluid-phase thrombin.

Elinogrel, previously known as PRT060128 or PRT128, is a direct-acting, reversible P2Y12 inhibitor for both intravenous and oral administration. Elinogrel has been tested in 2 phase II studies for the treatment of acute coronary syndrome, myocardial infarction and prevention of secondary thrombotic events. Elinogrel therapy was associated with an increased incidence of dyspnea and incidence of elevated liver transaminases. The development of the drug was terminated in January 2012 by Novartis.

Elarofiban is a novel nonpeptide glycoprotein IIb/IIIa (GPIIb/IIIa) antagonist. It inhibits thrombin-induced platelet aggregation in human gel-filtered platelets and platelet aggregation in human platelet-rich plasma (PRP) in response to collagen, arachidonic acid, ADP, and SFLLRN-NH(2). Elarofiban had adequate oral pharmacokinetics in dogs and excellent oral pharmacodynamics. Elarofiban has been in phase II clinical trials for the treatment of myocardial infarction and thrombosis. However, this research has been discontinued.

Gantofiban (or EMD 122 347) is an oral double prodrug of the drug, EMD 132338 and is GPIIb/IIIa antagonist. The drug participated in phase II clinical trials in Japan in patients with thrombosis. However, in May 2004, Yamanouchi, the developing company, announced that the study was discontinued. Besides gantofiban was involved in phase II trials, like a treatment option in patients with the acute coronary syndrome. However, further information is not available.

Oxamarin was developed as a hemostatic agent. Information about the current use of this compound is not available.

Aprosulate or lactobionic acid is a highly sulfated analogue of heparin which was undergoing clinical trials in Europe as a potential antithrombotic drug. Aprosulate exerts a strong anticoagulant effect in plasma as a result of its interaction with heparin cofactor II.

FERMAGATE is a phosphate binder with phosphate plasma levels lowering activity. It is in Phase 3 development in the US and in Europe for the treatment of hyperphosphatemia in dialysis patients. It is made up of magnesium and ferric iron atoms held in an insoluble, rigid, crystalline-layered structure, with carbonate groups lying between the layers. Upon oral administration, the carbonate ions in FERMAGATE are exchanged for free phosphate ions released from food in the gastrointestinal tract; thereby, strongly binding phosphate. This inhibits phosphate uptake and preventing hyperphosphatemia.

Lotrafiban (SmithKline Beecham) is a member of the latest generation of orally-active platelet GPIIb/IIIa blockers undergoing Phase III clinical trials to test the relative effectiveness versus other oral platelet inhibitors for ischaemic conditions including unstable angina, restenosis after PCI and stroke. Lotrafiban is converted from an esterified prodrug by plasma and liver esterases to a peptidomimetic of the arginine-glycine-aspartic acid amino acid sequence. This sequence itself mimics the binding site of fibrinogen and von Willebrand Factor to the platelet GPIIb/IIIa receptor. Preliminary results of the clinical trial APLAUD (antiplatelet useful dose) show that lotrafiban is clinically safe and well-tolerated in patients with recent myocardial infarction, unstable angina, transient ischaemic attack (TIA), or stroke when added to aspirin therapy. The Blockade of the IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) trial of SmithKline Beecham's oral GpIIb/IIIa blocker, lotrafiban, has been stopped early because of concerns about both safety and efficacy. The drug was showing a higher mortality rate than placebo, and was also associated with an increased incidence of serious thrombocytopenia and major bleeding. As a result of these findings the company has discontinued development of lotrafiban.

LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.

Efegatran (GYKI 14766; LY 294468) is a tripeptide D-methyl-phenylalanyl-prolyl-arginal thrombin inhibitor. It was developed by IVAX for the potential treatment of thromboembolic disorders, mainly myocardial infarction. However, information about the further development is not available.