Cortisone acetate is a synthetic glucocorticoid corticosteroid and corticosteroid ester which is marketed in many countries throughout the world, including in the United States, the United Kingdom, and various other European countries. It is the C21 acetate ester of cortisone, and acts as a prodrug of cortisone in the body.
Oxabolone cipionate, or oxabolone cypionate, also known as 4-hydroxy-19-nortestosterone 17β-cypionate or estr-4-en-4,17β-diol-3-one 17β-cypionate, is synthetic and injected anabolic–androgenic steroid (AAS) and derivative of nandrolone (19-nortestosterone) which has been marketed in Europe. It is the C17β cypionate ester and a prodrug of oxabolone (4-hydroxy-19-nortestosterone).
Prednimustine, sold under the brand names Mostarina and Sterecyst, is a medication which is used in chemotherapy in the treatment of leukemias and lymphomas. It is the ester formed from two other drugs, prednisolone and chlorambucil. Rarely, it has been associated with myoclonus.
Oxymesterone, also known as methandrostenediolone, as well as 4-hydroxy-17α-methyltestosterone or 17α-methylandrost-4-en-4,17β-diol-3-one, is an orally active anabolic-androgenic steroid (AAS). It was known by 1960.
Stenbolone is an anabolic–androgenic steroid (AAS) of the dihydrotestosterone (DHT) group which was never marketed. A C17β ester prodrug of stenbolone, stenbolone acetate, is used as an AAS for depot intramuscular injection under the brand names Anatrofin and Stenobolone.
Oxabolone is a synthetic anabolic-androgenic steroid (AAS) of the nandrolone (19-nortestosterone) group which was never marketed. It can be formulated as the cipionate ester prodrug oxabolone cipionate, which, in contrast, has been marketed for medical use.
Metogest, also known as 16,16-dimethyl-19-nortestosterone, is a steroidal antiandrogen that was patented in 1975 and investigated as a treatment for acne but was never marketed.
Penmesterol, or penmestrol, also known as 17α-methyltestosterone 3-cyclopentyl enol ether, is a synthetic, orally active anabolic-androgenic steroid (AAS) that was developed in the early 1960s. It is the 3-cyclopentyl enol ether of methyltestosterone.
Orestrate, also known as estradiol 3-propionate 17β-(1-cyclohexenyl) ether, is an estrogen medication and estrogen ester which was never marketed. It is the C3 propionate ester and C17β-(1-cyclohexenyl) ether of estradiol.
Flumexadol (INN) is a drug described and researched as a non-opioid analgesic which was never marketed. It has been found to act as an agonist of the serotonin 5-HT1A and 5-HT2C receptors and, to a much lesser extent, of the 5-HT2A receptor. According to Nilsson (2006) in a paper on 5-HT2C receptor agonists as potential anorectics, "The (+)-enantiomer of this compound showed [...] affinity for the 5-HT2C receptor (Ki) 25 nM) [...] and was 40-fold selective over the 5-HT2A receptor in receptor binding studies. Curiously, the racemic version [...], also known as 1841 CERM, was originally reported to possess analgesic properties while no association with 5-HT2C receptor activity was mentioned." It is implied that flumexadol might be employable as an anorectic in addition to analgesic. Though flumexadol itself has never been approved for medical use, oxaflozane is a prodrug of the compound that was formerly used clinically in France as an antidepressant and anxiolytic agent.
Spirorenone (INN) is a steroidal antimineralocorticoid of the spirolactone group that was never marketed. Spirorenone possesses 5–8 times the antimineralocorticoid activity of spironolactone in animal studies. The initial discovery of spirorenone was deemed a great success, as no compound with greater antimineralocorticoid activity had been developed since spironolactone in 1957. Moreover, spirorenone itself has virtually no affinity for the androgen receptor while its progestogenic activity shows species differences, being somewhat greater than that of spironolactone in rabbits but absent in mice and rats. As such, it was characterized as a highly potent antimineralocorticoid with far fewer hormonal side effects relative to spironolactone.
Clostebol acetate (BAN), also known as 4-chlorotestosterone 17β-acetate (4-CLTA) or as 4-chloroandrost-4-en-17β-ol-3-one 17β-acetate, is a synthetic, injected anabolic-androgenic steroid (AAS) and a derivative of testosterone that is marketed in Germany and Italy. It is an androgen ester – specifically, the C17β acetate ester of clostebol (4-chlorotestosterone) – and acts as a prodrug of clostebol in the body. Clostebol acetate is administered via intramuscular injection.
Clostebol propionate, also known as 4-chlorotestosterone 17β-propionate or as 4-chloroandrost-4-en-17β-ol-3-one 17β-propionate, is a synthetic, injected anabolic-androgenic steroid (AAS) and a derivative of testosterone. It is an androgen ester – specifically, the C17β propionate ester of clostebol (4-chlorotestosterone) – and acts as a prodrug of clostebol in the body. Clostebol acetate is administered via intramuscular injection.
Androstenediol dipropionate, or 5-androstenediol 3β,17β-dipropionate, also known as androst-5-ene-3β,17β-diol 3β,17β-dipropionate, is a synthetic anabolic–androgenic steroid and an androgen ester – specifically, the dipropionate diester of 5-androstenediol (androst-5-ene-3β,17β-diol) – which has been marketed in Europe, including in Spain, Italy, and Austria.
Zindoxifene is a nonsteroidal selective estrogen receptor modulator (SERM) that was under development in the 1980s and early 1990s for the treatment of breast cancer but was not marketed. It showed estrogenic-like activity in preclinical studies and failed to demonstrate effectiveness as a treatment for breast cancer in clinical trials. Zindoxifene was the lead compound of the distinct 2-phenylindole class of SERMs, and the marketed SERM bazedoxifene was derived from the major active metabolite of zindoxifene, D-15414. Zindoxifene was first described in 1984.
Panomifene is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group related to tamoxifen that was under development as an antineoplastic agent by Egis Pharmaceuticals and IVAX Drug Research Institute in the 1990s for the treatment of breast cancer, but it was never marketed. It reached phase II clinical trials before development was terminated. The drug was described in 1981.
Spiroxasone is a synthetic, steroidal antimineralocorticoid of the spirolactone group which was developed as a diuretic and antihypertensive agent but was never marketed. It was synthesized and assayed in 1963. The drug is 7α-acetylthiospirolactone with the ketone group removed from the C17α spirolactone ring. Similarly to other spirolactones like spironolactone, spiroxasone also possesses antiandrogen activity.
Dacuronium bromide is an aminosteroid neuromuscular blocking agent which was never marketed. It acts as a competitive antagonist of the nicotinic acetylcholine receptor (nAChR).
Pinoxepin is an antipsychotic of the tricyclic group with a dibenzoxepin ring system which was developed in the 1960s but was never marketed. It was found in clinical trials to have effectiveness in the treatment of schizophrenia similar to that of chlorpromazine and thioridazine. The drug has marked sedative effects but causes relatively mild extrapyramidal symptoms.
