DICHLORISONE is a synthetic corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders.

Endrysone is a glucocorticoid with anti-inflammatory and antiallergic properties. It is used topically for skin conditions as an ophthalmic anti-inflammatory agent.

Tipredane is one of the compounds of a new series of sulfur-containing steroids synthesized at The Squibb Institute for Medical Research and is being developed for topical treatment of human dermatoses. Tipredane is structurally unique in that the classical l7-beta two-carbon side chain and the 17-alpha hydrogen of the steroid have been replaced by two alkylthio substituents. Tipredane has been shown to possess moderate to potent anti-inflammatory activity in various animal models, and to exhibit favorable separation of local anti-inflammatory activity from adverse systemic effects in both animals and humans. After oral administration, [3H]tipredane was rapidly absorbed, metabolized, and excreted into urine and feces. Metabolism of tipredane was rapid and complex, with significant species differences, although the disposition in rhesus and cynomolgus monkeys seemed to be similar to humans. Tipredane had been investigated as the therapeutic agent for the treatment of allergic rhinitis, asthma and skin disorders. However, this development was discontinued.

Edogesterone (PH-218) is steroid with progestational and antiandrogenic properties.

Lixivaptan is an orally-active, vasopressin 2 receptor antagonist. It is indicated for the treatment of symptomatic hypervolemic and euvolemic hyponatremia, associated with heart failure (HF) and syndrome of inappropriate antidiuretic hormone (SIADH). Adverse events likely to be result of the pharmacologic action of lixivaptan are: constipation, dry mouth, dizziness, insomnia. Grapefruit juice significantly increased the extent of lixivaptan absorption as compared to lixivaptan administered under fasted conditions but not under fed conditions. Lixivaptan Cmax and AUC∞ increased by 2.4-fold and 3.2-fold, respectively, when lixivaptan was administered with ketoconazole (the same in case of Simvastatin).

Gestaclone was developed as a progesterone receptor agonist; however, this compound has never been marketed. Information about the current use of this compound is not available.

Sepranolone (UC1010) is a GABA-A modulating steroid antagonist (GAMSA) and does not antagonize the effect of GABA itself or other GABAA agonists like benzodiazepines and barbiturates. The interaction of neuroactive steroids (i.e., allopregnanolone and Sepranolone) with GABA-A receptor is particularly important in mood disorders. For example, allopregnanolone administration decreased saccadic eye velocity in healthy female volunteers and induced sedation and these effects were diminished by simultaneous sepranolone administration. Thus, allopregnanolone effects are antagonized by its isomer sepranolone. UC1010 reduces symptom severity and impairment significantly more efficiently than placebo in women with a well-defined, pure premenstrual dysphoric disorder. No severe adverse events were reported during the UC1010 treatment and safety parameters (vital signs and blood chemistry) remained normal during the study. It was revealed also that increases in ring A-reduced progesterone metabolites, particularly Sepranolone, are associated with chronic fatigue syndrome.

Somatoprim (DG3173) is a heptapeptide somatostatin analog (SSA) that binds with high affinity to sstr2, sstr4 and sstr5 and shows a very low insulin suppression in contrast to other SSA. Initially developed by Ipsen, it is under active development by licensee Aspireo Pharmaceuticals, an Israeli company. In vitro as well as in vivo testing showed a dose-dependent GH lowering effect. Somatoprim has demonstrated a unique receptor binding and pharmacological profile which is differentiated from SSAs that are currently marketed or in clinical development. In particular, Somatoprim has shown an improved side effect profile with reduced adverse effects on the gastrointestinal tract and glucose metabolism. Furthermore, assessment of growth hormone secretion in cultured human somatotroph adenoma tissue treated with Somatoprim indicates that it has the potential to increase the response rate of acromegalic patients to SSA therapy. Somatoprim is currently in phase I/II of clinical development.

Selepressin (FE 202158) was designed as a selective and short-acting vasopressin type 1a receptor (V(1a)R) agonist. This drug was developed for the treatment of vasodilatory hypotension in shock. Selepressin successfully completed phase IIa clinical trial, where was found that in septic shock patients, selepressin 2.5 ng/kg/minute was able to rapidly replace norepinephrine, improve fluid balance and shorten the time of mechanical ventilation.