Midazogrel (CBS-645) is a specific inhibitor of thromboxane synthetase. It inhibits the platelet enzyme in human and is potentially useful as an antithrombotic agent. Midazogrel could be of interest in the treatment of the various diseases in which the pathological role of thromboxane A2 is suspected. However, information about the further development of this drug is not available.

Setipafant [BN 50727], triazolothienodiazepine, is a synthetic platelet activating factor antagonist that was under development with Beaufour-Ipsen for the treatment of diarrhoea, inflammatory bowel diseases, peptic ulcer and ulcerative colitis. The research has been discontinued.

FLUFOSAL is an antithrombotic agent.

Moxicoumone is orally available coumarin derivative patented by Francesco, Vismara, Societa per Azioni for capillary fragility treatment

Boehringer Ingelheim developed samixogrel as thromboxane A2 receptor antagonists. This drug participated in clinical trials for the treatment patients with diabetic complications, thrombosis, and unstable angina pectoris. However, all these studies were discontinued.

FLUINDAROL, an indanedione derivative, is an anticoagulant.

Darexaban (YM150) is a direct inhibitor of coagulation factor Xa (FXa), discovered by Astellas Pharmaceuticals. FXa is a crucial serine protease in the coagulation cascade, responsible for the cleavage of prothrombin to its active form thrombin, which then converts soluble fibrinogen to insoluble fibrin, activates platelets and causes a formation of a blood clot. Darexaban inhibits factor Xa with a Ki value of 31 nM and shows anticoagulant activity in human plasma. In venous and A-V shunt thrombosis models in rats, darexaban strongly suppressed thrombus formation without affecting bleeding time. Darexaban was investigated in a number of clinical trials for prevention of venous thromboembolism in patients undergoing surgery, prevention of ischaemic events in acute coronary syndrome, prophylaxis of stroke in atrial fibrillation. In 2011 Astellas announced the discontinuation of darexaban because of high competition on anti-FXa drugs market.

Mespirenone (ZK 94679, 15β,16β-methylene-spironolactone) is a steroid aldosterone antagonist. In addition, it is a quite specific inhibitor of adrenocortical mineralocorticoid synthesis. In rodents mespirenone effectively prevents aldosterone-induced hypertension. It exerts natriuretic efficacy. Although it reached phase II clinical trials, it was discontinued in 1989.

Teclothiazide is a thiazide diuretic that has never been marketed. Information about the current use of this drug is not available.

Otamixaban is a synthetically derived parenteral fXa inhibitor currently in late stage clinical development at Sanofi-Aventis for the management of acute coronary syndrome. Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and extrinsic pathways of the blood coagulation cascade. FXa catalyzes the conversion of prothrombin to thrombin via the prothrombinase complex. Its singular role in thrombin generation, coupled with its potentiating effects on clot formation render it an attractive target for therapeutic intervention. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. Following the results of the Treatment of non-ST elevation Acute coronary syndrome with otamixaban, Sanofi has decided to discontinue the investigational programme with otamixaban, due to efficacy lower than expected. Otamixaban did not show superior benefit/risk to the combination of unfractionated heparin.