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.

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).

Aldosterone is a hormone secreted by the adrenal cortex that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium. Recent findings have shown that the physiological functions of the hormone aldosterone go far beyond its well-known role in blood-pressure regulation and salt/water homeostasis. Aldosterone is for example involved in the regulation of inflammation, and also binds directly to mineralocorticoid receptors in specific brain regions. At the late distal tubule and collecting duct, aldosterone has two main actions: 1) aldosterone acts on mineralocorticoid receptors (MR) on principal cells in the distal tubule of the kidney nephron, increasing the permeability of their apical (luminal) membrane to potassium and sodium and activates their basolateral Na+/K+ pumps, stimulating ATP hydrolysis leading to phosphorylation of the pump and a conformational change in the pump exposes the Na+ ions to the outside. The phosphorylated form of the pump has a low affinity for Na+ ions, hence reabsorbing sodium (Na+) ions and water into the blood, and secreting potassium (K+) ions into the urine; 2) aldosterone stimulates H+ secretion by intercalated cells in the collecting duct, regulating plasma bicarbonate (HCO3−) levels and its acid/base balance; and 3) aldosterone may act on the central nervous system via the posterior pituitary gland to release vasopressin (ADH) which serves to conserve water by direct actions on renal tubular resorption.

Fluperolone (P-1742 or Methral) is a topical fluorinated prednisolone derivative exerting an anti-inflammatory activity. It demonstrated effectivity in the treatment of various dermatoses.