Aceburic acid (INN), also known as 4-acetoxybutanoic acid or 4-hydroxybutyric acid acetate, is drug described as an analgesic which was never marketed. It is the acetyl ester of gamma-hydroxybutyrate, and based on its structural relation to GHB, is likely to behave as a prodrug to it.
Oxetorone (INN), as oxetorone fumarate (USAN), is a serotonin antagonist, antihistamine, and alpha blocker used as an antimigraine drug. Association with hyperprolactinemia has been described and antidopaminergic actions are also suspected.
Alfadolone (INN), or alphadolone is a neuroactive steroid and general anesthetic. Along with alfaxolone, as alfadolone acetate, it is one of the components of the anesthetic drug mixture althesin.
Sercloremine (CGP-4718A), usually as the hydrochloride salt, is a drug which was developed in the 1980s and was formerly under investigation as an antidepressant, but was never marketed. It acts as a selective, reversible inhibitor of monoamine oxidase A (RIMA) and serotonin reuptake inhibitor.
Diacetylnalorphine (BAN), also known as O3,O6-diacetyl-N-allyl-normorphine, is an opioid drug described as an analgesic and antidote which was never marketed. It is the 3,6-diacetyl ester of nalorphine, and therefore the heroin analogue of nalorphine. Diacetylnalorphine may behave as a prodrug to nalorphine, similarly to the cases of heroin (diacetylmorphine) to morphine and diacetyldihydromorphine to dihydromorphine.
Octotiamine (INN, JAN; Gerostop, Neuvita, Neuvitan), also known as thioctothiamine, is an analogue of vitamin B1 which is used in Japan and Finland.
Ciclafrine (INN) is a sympathomimetic phenethylamine and antihypertensive that was never marketed.
Berefrine, also known as burefrine, is a sympathomimetic and mydriatic agent that was never marketed. It is an oxazolidine prodrug of phenylephrine, and hence, an α1-adrenergic receptor agonist.
Pivenfrine (INN), also known as pivalylphenylephrine, is a sympathomimetic and mydriatic agent.
Morforex, also referable to as N-morpholinoethylamphetamine, is an anorectic which was never marketed.
Picilorex is an anorectic which is no longer marketed. It is a monoamine reuptake inhibitor, a stimulant as well as a derivate of Pyrrolidine.
Acridorex is an amphetamine which was investigated as an anorectic but does not appear to have ever been marketed.
Oxifentorex (INN) is an amphetamine described as an anorectic which does not appear to have ever been marketed.
Fenisorex is an amphetamine-like anorectic drug which does not appear to have ever been marketed.
Flucetorex (INN) is an amphetamine. It was investigated as an anorectic, but does not appear to have ever been marketed. It is related to fenfluramine.
Metaglycodol (INN) is a drug described as a tranquilizer which was never marketed.
Perafensine (INN) is a drug which was investigated as an antidepressant but was never marketed. It has been reported to antagonize the effects of reserpine and to inhibit the reuptake of norepinephrine ; whether it also affects the reuptake of serotonin or dopamine is unclear.
Hydromadinone (INN), also known as 6α-chloro-17α-hydroxyprogesterone, is a steroidal progestin of the 17α-hydroxyprogesterone group which was patented in 1967 but was never marketed. The C17α acetate ester of hydromadinone, hydromadinone acetate, also exists, but similarly was never marketed.
Methestrol or methoestrol, also known as promethestrol or promethoestrol (BAN) or as dimethylhexestrol, is a synthetic nonsteroidal estrogen of the stilbestrol group related to diethylstilbestrol which is no longer marketed.
Cioteronel is a nonsteroidal antiandrogen (NSAA) that was never marketed. It was under development between 1989 and 2001 for the topical treatment of androgenetic alopecia and acne and for the oral treatment of benign prostatic hyperplasia; it reached phase III clinical trials for acne and phase II studies for androgenetic alopecia, but was ultimately discontinued due to poor efficacy.
