Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.

Telapristone acetate, a selective progesterone receptor modulator (SPRM), was developed for the long-term treatment of symptoms associated with endometriosis and uterine fibroids. It is known, that the progesterone is a steroid hormone that plays an important role in the breast. Deregulation of the progesterone-signaling pathway is implicated in the formation, development, and progression of breast cancer. Thus, the telapristone acetate is studied in phase II clinical trial in stage I-II primary breast cancer. Besides, telapristone acetate participated in phase III clinical trials in pre-menopausal anemic women with symptomatic uterine fibroids. However, FDA terminated these studies because of the safety.

Detirelix is a synthetic decapeptide containing five D-amino acids. It is a very potent Gonadotropin-releasing hormone (GnHR) antagonist. The acute effects of detirelix were consistent with peripheral vasodilation. Subchronic effects were associated with inhibition of pituitary gonadotropic and gonadal hormone secretion. As long-acting GnRH antagonist detirelix can rapidly suppress gonadotropin secretion, inhibit follicular development, and prevent ovulation. It can be used as luteolytic agent. A projected use is for the treatment of sex hormone-releasing diseases, as part of anticancer hormone therapy of sex-hormone-dependent tumors.

Resocortol is a synthetic corticosteroid. Information about current use of this compound is not available.

Timobesone is a topical corticosteroid and thiol ester derivative with anti-inflammatory activity.

Spiroxasone is a synthetic, steroidal antimineralocorticoid of the spirolactone group patented by Merck & Co., Inc. as a diuretic and antihypertensive agent. Spiroxasone acts as potent aldosterone antagonists in animals and humans.

Ticabesone is a thioetianic acid derivative patented by Syntex, Inc. as anti-inflammatory agent. The topical antiinflammatory activity of Ticabesone was assessed in humans by vasoconstriction assay.

Ticabesone Propionate is Ticabesone ester patented by Syntex, Inc. as an anti-inflammatory agent. Ticabesone Propionate shows potent antiinflammatory activity silver nitrate-induced inflammation in the rat cornea.

Ulimorelin (TZP101) is a small molecule, intravenously administered, ghrelin receptor agonist that is being developed by Lyric Pharmaceuticals. Ulimorelin stimulates intestinal motility, but also reduces blood pressure in rodents and humans and dilates blood vessels. It has been proposed as a treatment for intestinal motility disorders. Ulimorelin has progressed to phase III human clinical trials for the treatment of postoperative ileus.