Telapristone is an orally available 21-substituted-19-nor-progestin and selective progesterone receptor modulator (SPRM), with potential anti-progesterone and antineoplastic activities. Its acetate form, the telapristone Acetate is a clinically used and a studied drug.

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.

Toripristone has a high inhibiting activity against the cortisol receptors. Toripristone enhanced the antibacterial activities of the sparfloxacin in combination with ethambutol in the treatment of M. avium complex infections. Also, toripristone is a glucocorticoid type II receptor and progesterone receptor antagonist. Toripristone treatment was estimated to selectively occupy approximately 50% of glucocorticoid receptors in rat brain.

Sanofi-Synthélabo has developed satavaptan (previously known as SR121463) as a non-peptidic vasopressin V2 receptor antagonist for the potential treatment for cardiovascular indications such as congestive heart failure (CHF) and hypertension. The drug reached phase II for these indications before the studies were discontinued. Satavaptan was also studied for the potential treatment of glaucoma. In addition, this drug was involved in phase III clinical trials in patients with ascites due to cirrhosis of the liver and in in patients with dilutional hyponatremia. However, the further development of the satavaptan was discontinued in 2009.

Nelivaptan is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V1B subtype. It showed promise in preclinical animal models and advanced to phase II clinical trials for the treatment of anxiety and depression; however, in 2008, Sanofi-Aventis announced that further development of this drug had been halted.

Aglepristone (RU 46534) is a competitive progesterone antagonist; it binds to progesterone receptors (PRs) without inducing the molecular cascade associated with progesterone. Its affinity to PRs is higher than progesterone (3.12, 3.8, and 9.26 times greater in the bitch, doe rabbit,and queen, respectively). Aglepristone can therefore beused in various progesterone-dependent physiological orpathologic conditions, with the aim of blocking the action of progesterone. Aglepristone has proven to be an effective and safe means of inducing pregnancy termination or parturition in a large number of domestic species. In domestic species, aglepristone is routinely used for the treatment of pyometra and feline mammary fibroadenomatous hyperplasia, both of which are progesterone dependent. Aglepristone is marketed under the brand name Alizin used as the treatment option for unwanted mating and pregnancy in dogs

Benorterone (or SKF 7690), a steroidal antiandrogen that was studied in the treatment of acne, seborrhea, and hirsutism in women but was never marketed.

Barusiban, a long-acting oxytocin antagonist, has been studied to stop preterm labor in pregnant women at late gestational age. The experiments failed to demonstrate the effectiveness and were discontinued. However, barusiban participates in phase II clinical trials for female infertility.

Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist (both PR isoforms PR-A and PR-B); binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Lonaprisan showed limited efficacy as second-line endocrine therapy in postmenopausal women with PR-positive metastatic breast cancer. Lonaprisan had been in phase II clinical trials by Bayer for the treatment of breast cancer and dysmenorrhea. However, this research has been discontinued.

Delanterone is an antiandrogen steroid, developed by the Dutch company Gist-Brocades N.V. for the treatment of various dermatological disorders, including hirsutism, acne, seborrhea, alopecia androgenetica, and baldness. The compound is claimed to show topical anti-androgenic activity with very weak systemic anti-androgenic activity, a lack of progesterone, anti-gonadotrophin and corticosteroid-like activity and very low toxicity.