Cefpimizole is an antibiotic of broad spectrum developed in Japan for the treatment of such conditions as uncomplicated gonorrhea and gynecologic infections. The drug was tested in clinical trials, however, its development was terminated.

FLUROGESTONE (9α-FLUORO-11β,17α-DIHYDROXYPROGESTERONE) is a steroidal progestin of the 17α-hydroxyprogesterone group that was never marketed. An acetate ester, flurogestone acetate, is used in veterinary medicine. It has progestational action higher than that of progesterone itself. It is intended for intravaginal use in sheep and goats to induce oestrus synchronisation. The proposed dosage is 1 sponge, impregnated with 30, 40 (for sheep) or 45 mg (for goats) flugestone acetate, which is to be removed after 12 to 14 days from ewes and after 17 to 21 days from goats. Flugestone acetate is not indicated for use in humans.

Methenolone (also known as primobolan) was described in 1960. Squibb Company began producing injectable drug in 1962. Methenolone originally was prescribed in case of muscle loss after operations, infections, long-term illnesses, aggressive therapy with corticoids or malnutrition, and in some cases it was used to treat osteoporosis and breast cancer. Methenolone was commonly used to promote weight gain in infants, weighing less than normal, without any side effects. Methenolone is an anabolic steroid, modification of dihydrotestosterone (DHT) with weak androgenic activity and a moderate anabolic effect. A notable trait of methenolone is that it can firmly bind to androgen receptors, stronger than testosterone. Adult doses for the treatment of aplastic anemia are usually in a range of 1–3 mg/kg per day. Adverse side effects include fluid and electrolyte retention, hypercalcaemia, increased bone growth and skeletal weight. In men, additional side priapism, azoospermia, hirsutism, male pattern baldness, acne andoedema. In women, side effects include virilization, amenorrhoea, menstrual irregularities, suppressed lactation, and increased libido. In children, side effects may include virilization symptoms. Metenolone may enhance effects of antidiabetics, ciclosporin, levothyroxine, warfarin. Resistance to the effects of neuromuscular blockers may occur, and metenolone also has the potential to interfere with glucose tolerance and thyroidfunction tests. Metenolone enanthate (methenolone enanthate) is an ester derivative of methenolone sold commonly under the brand names Primobolan (tablet form) orPrimobolan Depot (injectable). When it interacts with the aromatase enzyme it does not form any estrogens. It is used by people who are very susceptible to estrogenic side effects, having lowerestrogenic properties than nandrolone. This trait makes primobolan to be a good fat burner. Primobolan does not convert into estradiol. As an anabolic steroid, the use of metenolone is banned from use in sports governed by the World Anti-Doping Agency. Belarusian shot putter Nadzeya Ostapchuk was stripped of her gold medal after testing positive for metenolone at the London 2012 Olympic Games. She has been excluded from future IOC events. The NBA and NBPA also banned the use of methenolone under the Anti-Drug Program. In February 2013, Hedo Türkoğlu of the Orlando Magic was suspended for 20 games without pay by the league after testing positive for methenolone. In December 2013, Natalia Volgina was stripped of her 2013 Old Mutual Two Oceans Marathon title and received a two-year competition ban, subsequent to a final guilty verdict for using the steroid Metenolone.

Azacosterol (Ornitrol, 20,25-diazacholesterol dihydrochloride, SC 12937) is a cholesterol-lowering drug (hypocholesteremic) which was marketed previously but has since been discontinued. Azacosterol is a sterol derivative of cholesterol with two nitrogen atoms replacing two carbon atoms that acts as a hypocholesteremic agent by blocking delta-24-reductase. Azacosterol has the unintended side effect of causing myotonia. It is an avian contraceptive compound, which reduces fertility by inhibiting cholesterol synthesis. Azacosterol is also useful in the control of rodent populations.

Clevudine (also known as L-FMAU) is a nucleos(t)ide reverse transcriptase inhibitor, which inhibits the DNA synthesis activity of the hepatitis B virus polymerase. The drug was approved in Korea and Philippines and is being marketed under the names Levovir and Revovir. The drug is indicated in patients with chronic hepatitis B virus infection. Upon administration, clevudine is metabolized to the active metabolite, clevudine triphosphate, which is responsible for the inhibition of viral polymerase.

Cefsulodin is a third-generation of cephalosporin antibiotic with a narrow spectrum of activity. It has a specific activity against Pseudomonas aeruginosa. Cefsulodin’s targets are bacterial penicillin binding proteins. Drug is indicated for the treatment of infections of lower respiratory tract, skin and skin structures, urinary tract, bone and joint; treatment of gynecological infections; treatment of intra-abdominal infections; treatment of septicemia and CNS infections including meningitis caused by susceptible strains of specific microorganisms. Cefsulodin appears to be well tolerated and relatively free of any significant toxicity except for nausea and vomiting.

Astromicin is an aminoglycoside antibiotic produced by Micromonospora spp. It is effective against major gram-negative bacterias such as Proteus, Serratia, Citrobacter, Enterobacter spp., Klebsiella, Escherichia coli and Staphylococcus aureus. Astromicin sulfate has been given by intramuscular injection or intravenous infusion. Side effects are: rash, urticaria, itch, erythema, fever, nausea, vomiting, and diarrhea. Combination with strong diuretics can cause nephrotoxicity and ototoxicity.

Alphacetylmethadol (INN), aka α-acetylmethadol (AAM), is a synthetic opioid analgesic. Its levorotary enantiomer, levacetylmethadol, is an FDA-approved treatment for opioid addiction. Alphacetylmethadol is very similar in structure to methadone, a widely-prescribed treatment for opioid addiction. In the United States, it is a Schedule I controlled substance under the Controlled Substances Act with an ACSCN of 9603 and a 2013 annual manufacturing quota of 2 grams. Studies in rats indicate that alphacetylmethadol also evokes the heroin-like discriminative stimulus effects.

Ganglioside GM1 is a monosialo-glycosphingolipid belonging to the gangliotetrahexosyl series that abundant in neurons of all animal species and plays important roles in many cell physiological processes, including differentiation, memory control, cell signaling, neuronal protection, neuronal recovery, and apoptosis. Ganglioside GM1 in neurons helps to transfer information from the exterior to the interior of the cell, through specific recognition and binding of biologically active molecules (membrane receptors and ion channels), and has specific functions in nerve conduction and/or synaptic transmission. The mechanisms underlying the effects of Ganglioside GM1 remain unclear in many cases, but it appears that these effects are often due to specific interactions between Ganglioside GM1 and proteins involved in signaling processes, within Ganglioside GM1-enriched lipid rafts in the plasma membrane. Ganglioside GM1 is a major component of total ganglioside mixtures from mammalian brains, from which it can be extracted and purified in large amounts. Ganglioside GM1 was widely used in the past as a therapeutic drug for a wide variety of neurological disorders. Further studies have shown that Ganglioside GM1 has immunogenic properties and led to the production of antibodies that promoted peripheral neuropathies such as Guillain–Barré syndrome.

Diethylaminoethoxyhexestrol is a coronary dilating agent, approved for the treatment of angina in 1958 and marketed under tradename Coralgil. Diethylaminoethoxyhexestrol was withdrawn from the market because of drug-related phospholipidosis in liver, spleen and other tissues. Studies indicate that lipidosis is caused by the accumulation of the drug in lysosomes and inhibition of phospholipase A.