IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alpha reductase and a non-competitive inhibitor of type II 5-alpha reductase. It was under development for the treatment of prostatic cancer.

Mesabolone is a synthetic anabolic androgen.

Diflucortolone pivalate is a glucocorticoid drug. It might be used as anti-inflammatory and anti-allergic agent.

The information related to the biological or pharmacological application of fluprednisolone valerate is absent.

Bifluranol (brand name Prostarex), a fluorinated bibenzyl anti-androgen was developed as a nonsteroidal estrogen and was studied for the treatment of benign prostatic hyperplasia. Besides, was shown that bifluranol inhibited 17 alpha-hydroxylase/C17-C20 lyase.

Thymocartin (also known as T4 and RGH-0206) is a protected synthetic tetrapeptide patented by Hungarian multinational pharmaceutical and biotechnology company Gedeon Richter Plc. (Richter, Gedeon, Vegyeszeti Gyar Rt) as an immunomodulating agent. In preclinical models, Thymocartin shows to exert similar immunomodulatory activities to thymopoietin affecting both humoral and cellular responses. In skin graft mouse model Thymocartin increases the number of splenic T cells and restored the rejection capacity of thymectomized C57Bl mice. In chronic 28-days i.v. toxicity studies in dogs no adverse reaction has been found. The low toxicity of Thymocartin is probably attributable to their short half-life as the half-life of the Thymocartin is less than 3 min in humans.

Furostilbestrol (diethylstilbestrol di(2-furoate)) is a synthetic estrogen that was first described in 1952. It is an ester of diethylstilbestrol (DES), a synthetic estrogen that was prescribed to pregnant women until 1971 to prevent miscarriages and that has been associated with cancer, birth defects and several other developmental abnormalities. Furostilbestrol was never marketed.

Etiprednol dicloacetate (BNP-166; ethyl-17alpha-dichloroacetoxy-11beta-hydroxyandrosta-1,4-diene-3-one-17beta-carboxylate) is a new soft steroid. The compound proved to be a dissociated glucocorticoid, showing a reduction in transactivating activity while preserving transrepressive abilities. The compound effectively decreased cytokine production in lipopolysaccharide-stimulated lymphocytes and attenuated lectin-induced proliferation of blood mononuclear cells in tissue culture. The significant local effect of the compound will very likely be accompanied by a drastically reduced systemic activity indicating an encouraging selectivity of the pharmacological action of etiprednol dicloacetate. Etiprednol dicloacetate had been in a clinical trial for the treatment of allergic rhinitis, asthma and Crohn's disease. However, development has been discontinued.

Retosiban is a small molecule oxytocin receptor antagonist that is under evaluation for treatment of premature labor. Retosiban was found to be safe in healthy non-pregnant volunteers in phase I studies. Intravenous retosiban also had good safety and tolerability in phase II studies and was suggested to prolong pregnancies in women with preterm labor. Phase III studies have been conducted to demonstrate the efficacy of retosiban to prolong pregnancy and improve neonatal outcomes, and compare effects with a similar drug atosiban, but these studies were terminated in 2018 (not due to adverse events).