Roxifiban (also known as DMP754), a potent antiplatelet agent in inhibiting platelet aggregation, and has a high specificity and affinity for human platelet glycoprotein IIb/IIIa complex (GPIIb/IIIa) receptors. Roxifiban participated in clinical trials phase III for the treatment of peripheral arterial disorders. This drug was also well tolerated in patients with chronic stable angina pectoris and was studied in the treatment of heparin-induced thrombocytopenia, and thrombosis. However, the development of this drug appears to have been discontinued.

Razaxaban (also known as BMS-561389 or DPC 906) is an oral factor Xa inhibitor that was being developed for the treatment of thrombosis. It showed excellent results in the lab for efficacy and bioavailability and was therefore selected for further development. In a phase 1 clinical trial with healthy subjects, Razaxaban was well tolerated with minor bleeding. However, higher bleeding was reported in thrombosis patients in a phase 2 clinical trial, and the development of this drug was therefore discontinued in 2005.

Ifetroban was developed as a thromboxane A2/prostaglandin H2 receptor antagonist by Bristol-Myers Squibb for cardiovascular indications. In spite of the positive preclinical results where the drug has shown the cardioprotective and antithrombotic activities and was effective. The development of this drug for coronary thrombosis, peripheral vascular disorders, and thrombosis was discontinued. Bristol-Myers Squibb donated the entire program to Vanderbilt University, which further identified ifetroban’s potential in treating patients for several niche indications. Cumberland acquired the ifetroban program from Vanderbilt through its majority-owned subsidiary, Cumberland Emerging Technologies taking responsibility for development and commercialization of the product. Ifetroban oral capsule is being developed by Cumberland for the treatment of systemic sclerosis (SSc) also called scleroderma. With pulmonary disease emerging as the major cause of death in SSc patients, preclinical work indicates that ifetroban is capable of preventing cardiac fibrosis in a model of pulmonary arterial hypertension. In addition, this drug successfully completed phase II clinical trials for the treatment of hepatorenal syndrome (HRS) in hospitalized adult patients, where were determined the safety and pharmacokinetics of 3 days of intravenous ifetroban. In addition, the recruitment is anticipated for Phase 2 study of daily, oral anti-fibrotic therapy to prevent heart muscle disease and improve heart muscle function in ambulatory and non-ambulatory Duchenne patients. In December 2018, Vanderbilt-Ingram Cancer Center and Cumberland Pharmaceuticals initiated a phase II trial to assess the safety and feasibility of ifetroban in treating patients with malignant solid tumors that are at high risk of coming back after treatment and spreading throughout the body.

Tecarfarin (also known as ATI-5923), an anticoagulant, is a vitamin K reductase antagonist. Tecarfarin is participating in phase III clinical trials for the treatment of thromboembolism and thrombosis. On March 11, 2019, Espero BioPharma Inc. announced that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation (ODD) for tecarfarin for the prevention of systemic thromboembolism of cardiac origin. Tecarfarin is metabolized by esterases, escaping metabolism by the cytochrome P450 system and thereby avoiding cytochrome P450-mediated drug-drug or drug-food interactions as well as genetic variations found in the cytochrome P450 system.

Vorapaxar is a tricyclic himbacine-derived oral thrombin receptor antagonist that acts by reversible inhibition of the protease-activated receptor-1 (PAR-1). PAR-1 is expressed on platelets and its inhibition prevents platelets from aggregation. Vorapaxar is approved by FDA and is indicated for the reduction of recurring thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Vorapaxar at the same time may cause bleeding complications including intracranial haemorrhage (ICH), when compared to standard therapy alone. That is why Vorapaxar is contraindicated in patients with prior stroke, transient ischemic attack and ICH.

Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. In phase II of clinical trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.

Pamabrom is a diuretic drug, available in over-the-counter medications. The active diuretic ingredient in pamabrom is 8-bromotheophylline. It is used for the relief of temporary water weight gain; bloating; swelling; full feeling associated with the premenstrual and menstrual periods.

MERSALYL (Mersal) is an organomercury compound, mercurial diuretics that superseded by safer diuretics such as thiazides, and is hardly used anymore. Due to the idiosyncratic nature of mercury toxicity, the risk of severe disease and sudden death are unpredictable and frequently show no warning signs. Mercurial diuretics cause diuresis by reducing the reabsorption sodium in the ascending loop of Henle, thus causing more water being delivered to the distal convoluted tubule. Unfortunately, earlier physicians misconstrued hallmark symptoms of mercury poisoning such as excessive salivation as signs of mercury's efficacy, including up until the early 1960s when the use of mercurial diuretics was halted in medicine.

Hydrastinine is a synthetic alkaloid prepared by various processes from either hydrastine, berberine, or narcotine. It exerts a strong stimulating action on the uterus of all species studied, including human. Hydrastinine and the closely related alkaloid cotarnine have been employed as hemostatics, particularly in abnormal uterine conditions. In the non-pregnant animal, hydrastinine in doses of 10 mg. depressed both tonus and activity, even after the section of the hypogastric. In the pregnant cat, it caused the uterus to contract. A stimulant action was also noted in the non-pregnant animal if nicotine were administered prior to hydrastinine. The rabbit uterus in situ was strongly contracted. Laidlaw believed that hydrastinine acted on the uterus both directly on the smooth muscle and also through its sympathetic innervation. Repeated administration of large doses for a period of time resulted in greatly increased amplitude of contractions which persisted after removal of the drug. The drug was patented by Bayer as a haemostatic drug during the 1910s.