Formestane (trade name Lentaron) is a type I, steroidal, selective aromatase inhibitor used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. Formestane has poor oral bioavailability and thus must be administered fortnightly (bi-weekly) by intramuscular injection. Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Estrogen-sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone-sensitive breast cancers. Common side effects associated with the use of an aromatase inhibitor include hot flashes, joint pain, weakness, fatigue, mood changes, depression, high blood pressure, swelling of the arms/legs, and headache. Aromatase inhibitors may also decrease bone mineral density, which may lead to osteoporosis and an increase in fractures in susceptible patients. Formestane was the first selective aromatase inhibitor to be developed as a prescription drug, first appearing in Europe during the mid-1990s under the Lentaron Depot brand name. With the emergence of newer and more effective aromatase inhibitors, however, formestane soon lost market presence at a rapid rate. Most of the initial Lentaron preparations have since been discontinued. Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance with the regulations of the World Anti-Doping Agency. The drug remains available today, but only in a small number of nations. This includes Austria, Brazil, Czech Republic, Hong Kong, and Turkey.

Etebenecid is a uricosuric agent, lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys, also inhibits penicillin tubular secretion. It is useful in the interval treatment of gout. As with other uricosuric drugs, etebenecid may provoke acute gouty attacks in the early stages of treatment, and colchicine should be given during the first 6 weeks of treatment. It caused dyspepsia and diarrhea less frequently than probenecid and sulphinpyrazone. Several patients reported drowsiness while taking etebenecid in the treatment of gout, but no other side-effects were noted. Etebenecid should be given with care to patients with a history of uric acid calculi or of renal colic.

Taltirelin (TA-0910), a synthetic thyrotropin-releasing hormone (TRH) analog, has been developed by Tanabe Seiyaku for the treatment of neurodegenerative diseases. Taltirelin mimics the physiological actions of TRH, but with a much longer half-life and duration of effects, and little development of tolerance following prolonged dosing. Taltirelin has nootropic, neuroprotective and analgesic effects. Taltirelin is primarily being researched for the treatment of spinocerebellar ataxia; limited research has also been carried out with regard to other neurodegenerative disorders, e.g., spinal muscular atrophy.

Dilazep is a coronary and cerebral vasodilator as an adenosine reuptake inhibitor. Dilazep is an inhibitor of platelet aggregation and of membrane transport of nucleosides. Dilazep is also known to have a vasodilating effect on renal vessels and is often used in patients with ischaemic heart disease, cerebral ischemia or renal dysfunction to improve tissue circulation.

Sertindole (brand names: "Serdolect" and "Serlect") is an antipsychotic medication. Sertindole was developed by the Danish pharmaceutical company Lundbeck and marketed under license by Abbott Labs. Like other atypical antipsychotics, it has activity at dopamine and serotonin receptors in the brain. It is used in the treatment of schizophrenia. Sertindole is not approved for use in the United States and was discontinued in Australia in January 2014. In Europe, sertindole was approved and marketed in 19 countries from 1996, but its marketing authorization was suspended by the European Medicines Agency in 1998 and the drug was withdrawn from the market. In 2002, based on new data, the EMA's CHMP suggested that Sertindole could be reintroduced for restricted use in clinical trials, with strong safeguards including extensive contraindications and warnings for patients at risk of cardiac dysrhythmias, a recommended reduction in maximum dose from 24 mg to 20 mg in all but exceptional cases, and extensive ECG monitoring requirement before and during treatment.

Lonidamine is a derivative of the indazole-3-carboxylic acid, with limited antineoplastic activity as a single agent but with exceptional potential in modulating the activities of conventional chemotherapeutic agents such as N-mustard alkylating agents and anthracyclines as well as hyperthermia, radiation therapy and photodynamic therapy. The most critical property of Lonidamine is its selective activity against a broad range of tumors with little to no effect on normal tissues provided that doses are below a threshold level of ~400 mg/m^2 (oral or i.v. doses). Selective effects of Lonidamine on tumors compared to other potential targets probably result from the dependence of most tumors on glycolytic metabolism, but the exact mechanism of specificity is still not fully known. Current evidence indicates that Lonidamine inhibits lactate export by the proton-linked monocarboxylate transporter(s) (MCT) and pyruvate uptake into mitochondria via the mitochondrial pyruvate carrier (MPC), whereas inhibition of respiration involves both diminished mitochondrial uptake of pyruvate via the MPC as well as inhibition of the mitochondrial electron-transport chain at Complex II and perhaps also Complex I, in both instances at the ubiquinone reduction step. There is also evidence that the drug may indirectly inhibit hexokinase as well as possibly other glycolytic and pentose shunt enzymes as a result of cytosolic acidification. Key problems that remain to be addressed are the production of Lonidamine under GMP conditions since Angelini Pharmaceuticals in Rome, Italy, the sole commercial source of this drug, stopped producing it in 2006. In addition, utilization of Lonidamine in the US requires IND approval by the FDA, which has previously been granted for a number of clinical trials. Finally, even though LND is a potent enhancer of the activity of a number of potent anti-cancer agents, potentially less toxic (and patentable) “targeted-tumor agents” are replacing traditional chemotherapy. Another problem remaining to be addressed is the limited solubility of Lonidamine at neutral pH. Oral delivery has led to variable results; more soluble derivatives that can be administered by the intravenous administration are needed to accurately control the dosing schedules.

Nifuroxazide is a nitrofuran antibiotic used for the treatment of acute infectious diarrhoea.Nifuroxazide is a potent inhibitor of Signal transducers and activators of transcription (STAT) signaling. It exerts antineoplastic potential both in vitro and in vivo.

Gabexate is a synthetic protease inhibitor, was shown to be effective in treating patients with sepsis-associated disseminated intravascular coagulation in which tumor necrosis factor-alpha (TNF-alpha) plays a critical role. Gabexate mesylate is a drug marketed only in Italy and Japan and it is considered an essential drug in the treatment of acute pancreatitis. Gabexate is marketed under the brand name REMINARON among others in Japan. It relieves inflammatory symptoms in the pancreas by inhibiting various enzymes. It also improves organ disorders and bleeding tendency caused by blood clots in blood vessels by inhibiting blood coagulation. It is usually used to treat acute pancreatitis with deviation of proteolytic enzymes (such as trypsin, kallikrein and plasmin), acute exacerbation of chronic recurrent pancreatitis, acute pancreatitis after surgery and disseminated intravascular coagulation.

Menbutone is a choleretic compound which is used in veterinary medicine at a dose rate up to 10 mg/kg bw by parenteral (intravenous or intramuscular) route in bovine, ovine, caprine, porcine, and equine species. Menbutone stimulates the digestive tract by increasing excretion of bile, gastric acid, and pancreatic juices by two to five times baseline. It is marketed for veterinary use in Europe under several brand names.

Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.