Anecortave is a novel angiogenesis inhibitor used in the treatment of the exudative (wet) form of age-related macular degeneration. It will be marketed by Alcon as anecortave acetate (AA) for depot suspension under the trade name Retaane. In 2007 they received their letter of approval for Retaane’s indication to treat wet age-related macular degeneration (AMD), but final approval would require the completion of an additional clinical study. As a result, the Anecortave Acetate Risk-Reduction Trial (AART) was continued to be supported by Alcon. This study looked at the efficacy of Retaane to reduce the progression of the dry from of AMD to the wet-form. In 2008, Alcon Inc. announced they were terminating the development of anecortave acetate for the prevention of developing sight-threatening choroidal neovascularization secondary to age-related macular degeneration. In 2009, Alcon Inc. announced they would terminate the development of the drug for the reducing intraocular pressure associated with glaucoma. Currently, anecortave acetate is not on the market or being made for therapeutic use by Alcon Inc.[7] This could be due to the lack of efficacy of clinical trials with anecortave acetate or because of newer more efficacious products that are currently on the market. Anecortave acetate functions as an antiangiogenic agent, inhibiting blood vessel growth by decreasing extracellular protease expression and inhibiting endothelial cell migration. Its angiostatic activity does not seem to be mediated through any of the commonly known pharmacological receptors. RETAANE blocks signals from multiple growth factors because it acts downstream and independent of the initiating angiogenic stimuli and inhibits angiogenesis subsequent to the angiogenic stimulation. Recently was discovered, that phosphodiesterase 6-delta (PDE6D) was a molecular binding partner of AA and this provided insight into the role of this drug candidate in treating glaucoma.

Quingestanol is a metabolite of the quingestanol acetate, oral contraceptive, which was studied for therapy of menopausal diabetic women. Quingestanol is also a prodrug of norethisterone, which is used in birth control.

Halopredone (THS-201; (17,21-bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione; halopredone acetate; Topicon) is a highly topical corticosteroid. When it is used for intraarticular injections, the effects last longer than any other steroids which have been used, and it has less general effects. Halopredone acetate is used for arthritis and osteoarthritis (OA) patients. For RA patients, mean dose for a wrist is 12.5 mg and that for a knee is 25 mg. About 90% cases showed effectiveness and in about 45% cases the duration of effect is longer than 4 weeks. More than half cases of OA showed also improvements. It also possesses positive anti-inflammatory properties in dermatologic patients.

Roxatidine is an histamine H2-receptor antagonist. Roxatidine is a potent and selective inhibitor of basal and stimulated gastric acid secretion through competitive blockade of H2-receptors. Total pepsin secretion is reduced in a dose-dependent manner. There is an independent mucosal protection action. Roxatidine is indicated for the treatment of peptic ulcer, gastro-oesophageal reflux disease, gastritis, upper gastrointestinal haemorrhage and Zollinger-Ellison syndrome also it can be used as a premedication before anaesthesia. Roxatidine possessed a robust estrogenic activity.

Zuclopenthixol is indicated the management of the manifestations of schizophrenia and other mental illnesses with disturbances in thinking, emotional reactions and behaviour. It is also used to treat the manic phase of manic depressive illness. Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1-adrenergic and 5-HT2 receptors. Zuclopenthixol (CLOPIXOL®) is avavilable in the form of tablets and solution for intramuscular injections.

Roxatidine is an histamine H2-receptor antagonist. Roxatidine is a potent and selective inhibitor of basal and stimulated gastric acid secretion through competitive blockade of H2-receptors. Total pepsin secretion is reduced in a dose-dependent manner. There is an independent mucosal protection action. Roxatidine is indicated for the treatment of peptic ulcer, gastro-oesophageal reflux disease, gastritis, upper gastrointestinal haemorrhage and Zollinger-Ellison syndrome also it can be used as a premedication before anaesthesia. Roxatidine possessed a robust estrogenic activity.

Tilarginine is L-N-monomethyl arginine (L -NMMA), a non-selective inhibitor of nitric oxide synthase (NOS), which has been studied in the treatment of septic shock and cardiogenic shock complicating myocardial infarction. Despite strong evidence that excessive nitric oxide (NO) production plays a pivotal role in the pathogenesis of septic shock and may contribute to the pathogenesis of cardiogenic shock complicating myocardial infarction, outcome studies in these two disorders have proved disappointing. Tilarginine therapy was associated with an excess mortality, particularly at doses > 5 mg/(kg h), in septic shock, whereas the effects of a lower dose (1 mg/(kg h)) in cardiogenic shock complicating myocardial infarction were neutral. The excess mortality in patients with septic shock was almost certainly the result of unfavorable hemodynamic changes induced by Tilarginine (decreased cardiac output, increased pulmonary vascular resistance and reduced tissue oxygen delivery) whereas the lack of benefit in patients with cardiogenic shock complicating myocardial infarction may have been because the dose of Tilarginine was too low.

Methenolone (also known as primobolan) was described in 1960. Squibb Company began producing injectable drug in 1962. Methenolone originally was prescribed in case of muscle loss after operations, infections, long-term illnesses, aggressive therapy with corticoids or malnutrition, and in some cases it was used to treat osteoporosis and breast cancer. Methenolone was commonly used to promote weight gain in infants, weighing less than normal, without any side effects. Methenolone is an anabolic steroid, modification of dihydrotestosterone (DHT) with weak androgenic activity and a moderate anabolic effect. A notable trait of methenolone is that it can firmly bind to androgen receptors, stronger than testosterone. Adult doses for the treatment of aplastic anemia are usually in a range of 1–3 mg/kg per day. Adverse side effects include fluid and electrolyte retention, hypercalcaemia, increased bone growth and skeletal weight. In men, additional side priapism, azoospermia, hirsutism, male pattern baldness, acne andoedema. In women, side effects include virilization, amenorrhoea, menstrual irregularities, suppressed lactation, and increased libido. In children, side effects may include virilization symptoms. Metenolone may enhance effects of antidiabetics, ciclosporin, levothyroxine, warfarin. Resistance to the effects of neuromuscular blockers may occur, and metenolone also has the potential to interfere with glucose tolerance and thyroidfunction tests. Metenolone enanthate (methenolone enanthate) is an ester derivative of methenolone sold commonly under the brand names Primobolan (tablet form) orPrimobolan Depot (injectable). When it interacts with the aromatase enzyme it does not form any estrogens. It is used by people who are very susceptible to estrogenic side effects, having lowerestrogenic properties than nandrolone. This trait makes primobolan to be a good fat burner. Primobolan does not convert into estradiol. As an anabolic steroid, the use of metenolone is banned from use in sports governed by the World Anti-Doping Agency. Belarusian shot putter Nadzeya Ostapchuk was stripped of her gold medal after testing positive for metenolone at the London 2012 Olympic Games. She has been excluded from future IOC events. The NBA and NBPA also banned the use of methenolone under the Anti-Drug Program. In February 2013, Hedo Türkoğlu of the Orlando Magic was suspended for 20 games without pay by the league after testing positive for methenolone. In December 2013, Natalia Volgina was stripped of her 2013 Old Mutual Two Oceans Marathon title and received a two-year competition ban, subsequent to a final guilty verdict for using the steroid Metenolone.

Alfadolone or alphadolone is an oral neurosteroid, which can be useful as an analgesic.

Avorelin is a superagonist of natural luteinizing-hormone-releasing-hormone. Avorelin has been formulated in high molecular weight polylactic glycolic acid to afford protracted and continuous release of the peptide from subcutaneous implants. Avorelin has been in phase II clinical trials by Mediolanum for the treatment of prostate cancer, breast cancer and endometriosis. However, this research has been discontinued. Adverse events mainly related to androgen suppression (hot flushes, decreased libido and impotence) or the nature of the disease (skeletal pain).