Ergoline is a chemical compound whose structural skeleton is contained in a variety of alkaloids, referred to as ergoline derivatives or ergoline alkaloids. Ergoline alkaloids, one being ergine, were initially characterized in ergot. Some of these are implicated in the condition ergotism, which can take a convulsive form or a gangrenous form. Even so, many ergoline alkaloids have been found to be clinically useful. Annual world production of ergot alkaloids has been estimated at 5,000–8,000 kg of all ergopeptines and 10,000–15,000 kg of lysergic acid, used primarily in the manufacture of semi-synthetic derivatives.
Fluorometholone, also known as 6α-methyl-9α-fluoro-11β,17α-dihydroxypregna-1,4-diene-3,20-dione, is a synthetic glucocorticoid which is used in the treatment of inflammatory eye diseases. The C17α acetate ester, fluorometholone acetate, is also a glucocorticoid and is used for similar indications. Specifically, it is indicated for use in the treatment of steroid-responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the eye.
Mitotane, sold under the brand name Lysodren, is a steroidogenesis inhibitor and cytostatic antineoplastic medication which is used in the treatment of adrenocortical carcinoma and Cushing's syndrome. It is a derivative of the early insecticide DDT and an isomer of p,p'-DDD (4,4'-dichlorodiphenyldichloroethane) and is also known as 2,4'-(dichlorodiphenyl)-2,2-dichloroethane (o,p'-DDD).
Thiotepa (INN,, sold under the brand name Tepadina, is an alkylating agent medication used to treat cancer.
Cefalotin (INN) or cephalothin (USAN) is a first-generation cephalosporin antibiotic. It was the first cephalosporin marketed (1964) and continues to be widely used. It is an intravenously administered agent with a similar antimicrobial spectrum to cefazolin and the oral agent cefalexin. Cefalotin sodium is marketed as Keflin (Lilly) and under other trade names.
Ethylestrenol, also known as ethyloestrenol or ethylnandrol and sold under the brand names Maxibolin and Orabolin among others, is an androgen and anabolic steroid (AAS) medication which has been used in the past for a variety of indications such as to promote weight gain and to treat anemia and osteoporosis but has been discontinued for use in humans. It is still available for veterinary use in Australia and New Zealand however. It is taken by mouth.
Phenacemide, also known as phenylacetylurea, is an anticonvulsant of the ureide (acetylurea) class. It is a congener and ring-opened analogue of phenytoin, and is structurally related to the barbiturates and to other hydantoins. Phenacemide was introduced in 1949 for the treatment of epilepsy, but was eventually withdrawn due to toxicity.
Naftidrofuryl (INN), also known as nafronyl or as the oxalate salt naftidrofuryl oxalate or nafronyl oxalate, is a vasodilator used in the management of peripheral and cerebral vascular disorders. It is also claimed to enhance cellular oxidative capacity. The drug act as a selective antagonist of 5-HT2 receptors (with action as an inverse agonist of the 5-HT2A receptor specifically characterized). Naftidrofuryl is also licensed for the treatment of intermittent claudication due to peripheral arterial disease.
Medrysone, also known as hydroxymethylprogesterone, methylhydroxyprogesterone, or hydroxymesterone, as well as 6α-methyl-11β-hydroxyprogesterone or 6α-methyl-11β-hydroxypregn-4-ene-3,20-dione, is a synthetic glucocorticoid that is or has been used in the treatment of inflammatory eye diseases. It has been discontinued in the United States. Although it is very similar in structure to progesterone, neither progestogenic nor androgenic activity has been demonstrated for or attributed to medrysone.
Norfenefrine is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain.
Testolactone is a non-selective, irreversible, steroidal aromatase inhibitor which is used as an antineoplastic drug to treat advanced-stage breast cancer. The drug was discontinued in 2008 and is no longer available for medical use. However, it has been reported to still be marketed in the United States by Bristol-Myers Squibb under the brand name Teslac.
Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly by Sanofi-Aventis as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence. Though initially studied as a potential treatment for a variety of different medical conditions, Sanofi-Aventis eventually narrowed down the therapeutic indications of the compound to just appetite suppression. Drinabant reached phase IIb clinical trials for this purpose in the treatment of obesity but was shortly thereafter discontinued, likely due to the observation of severe psychiatric side effects including anxiety, depression, and thoughts of suicide in patients treated with the now-withdrawn rimonabant, another CB1 antagonist that was also under development by Sanofi-Aventis.
Topterone, also known as 17α-propyltestosterone or as 17α-propylandrost-4-en-17β-ol-3-one, is a steroidal antiandrogen that was first reported in 1978 and was developed for topical administration but, due to poor effectiveness, was never marketed.
Funapide (INN) is a novel analgesic under development by Xenon Pharmaceuticals for the treatment of a variety of chronic pain conditions, including osteoarthritis, neuropathic pain, postherpetic neuralgia, and erythromelalgia, as well as dental pain. It acts as a small-molecule Nav1.7 and Nav1.8 voltage-gated sodium channel blocker. Funapide is being evaluated in humans in both oral and topical formulations, and as of July 2014, has reached phase IIb clinical trials.
Dipraglurant (INN) is a negative allosteric modulator of the mGlu5 receptor which is under development by Addex Therapeutics for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID). As of 2014, it is in phase II clinical trials for this indication. Addex Therapeutics is also investigating an extended-release formulation of dipraglurant for the treatment of non-parkinsonian dystonia.
Nepadutant (INN) (code name MEN-11420) is a glycosylated bicyclic cyclohexapeptide drug which acts as a highly selective NK2 receptor antagonist. It was developed by the Menarini Group and investigated for the treatment of functional gastrointestinal disorders and asthma but was never marketed.
Zonampanel is a quinoxalinedione derivative drug and competitive antagonist of the AMPA receptor which was being investigated by Yamanouchi/Astellas Pharma as a neuroprotective drug for the treatment of ischemic stroke but never completed clinical trials. In clinical trials, zonampanel produced severe side effects including hallucinations, agitation, and catatonia in patients, resulting in early termination of the trials.
Quinestradol, also known as quinestradiol or quinestriol, as well as estriol 3-cyclopentyl ether (E3CPE), is a synthetic estrogen and estrogen ether which is no longer marketed. It is the 3-cyclopentyl ether of estriol. The medication has been studied in the treatment of stress incontinence in elderly women, with effectiveness observed.
Atrimustine (INN), also known as bestrabucil or busramustine, is a cytostatic antineoplastic agent which was under development in Japan by Kureha Chemicals for the treatment of breast cancer and non-Hodgkin's lymphoma as well as for the prevention of graft-versus-host disease in bone marrow transplant recipients. It is the benzoate ester of an ester conjugate of estradiol and chlorambucil, which results in targeted/site-directed cytostatic activity toward estrogen receptor-positive tissues such as breast and bone. It reached preregistration for the treatment of cancer but was ultimately discontinued. Estrogenicic side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia. The drug was first patented in 1980.
Toripristone (INN) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed. It is reported as a potent and highly selective antagonist of the glucocorticoid receptor (GR), though it also acts as an antagonist of the progesterone receptor (PR). The pharmacological profile of toripristone is said to be very similar to that of mifepristone, except that toripristone does not bind to orosomucoid. The drug has been used to study the hypothalamic-pituitary-adrenal axis and has been used as a radiotracer for the GR. Its INN was given in 1990.
