Coleneuramide (MCC-257) is a cholestane amide conjugate originated in Mitsubishi Pharma Corporation. It has been shown to enhance the effect of nerve growth factor (NGF) on cell survival and on tyrosine phosphorylation in PC12 cells. Coleneuramide is believed to act directly on TrkA receptor. In preclinical models, MCC-257 rescued clinical sign and pathological changes in rats after exposure to environmental neurotoxin methylmercury and protected against dysfunction of the peripheral nervers in hyperglycemic animals. The compound was investigated in phase 2 clinical study for the treatment of diabetic polyneuropathy, but no results were reported.

Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Anisodamine is a non-specific cholinergic antagonist. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Anisodamine has been employed therapeutically since 1965 in the People’s Republic of China primarily to improve blood flow in circulatory disorders such as septic shock, disseminated intravascular coagulation (DIC) and as an antidote to organophosphate poisoning.

Mideplanin (MDL 62873), a teicoplanin amide derivative, was studied as an antibacterial agent against Gram-positive bacteria. However, further, development appears to have been discontinued.

Vinleurosine is a vinca alkaloid found in species of Catharanthus. This compound was studied as an anticancer agent and participated in clinical trials. However, the drug was more toxic and unpredictable in effect in comparison with vinblastine. Its further development was discontinued.

Carbenzide is hydrazine derivative with the high antidepressant activity and low toxicity patented by pharmaceutical company Warner-Lambert Pharmaceutical Co. Carbenzide acts via monoamine oxidase (MAO) inhibition and increase the level of brain serotonin.

Onapristone is a type I progesterone receptor (PR) antagonist that prevents PR- mediated DNA transcription and was studied as an antitumor agent. This drug possessed activity in breast cancer and is participating in phase II clinical trials to test any good and bad effect for the treatment of endometrial cancer, ovarian cancer, peritoneal cancer, and prostate cancer.

Bidisomide (previously known as SC 40230) was developed as a sodium channel antagonist with class I antiarrhythmic properties. Bidisomide participated in clinical trials for patients with arrhythmia. However, the development was discontinued due to a lack of demonstrable efficacy.

Efepristin (RPR 106972) is an oral streptogramin consisting of two synergistic components RPR 112808 (pristinamycin IB) and RPR 106950 (pristinamycin IIB). It demonstrated activity against Gram-positive microorganisms in vitro and in vivo, including those with multi-drug resistance. The streptogramins inhibit bacterial growth by disrupting the translation of mRNA into protein.

Oxaprotiline (also known as hydroxymaprotiline) is a norepinephrine reuptake inhibitor and blocked the histamine H1 receptor. Oxaprotiline was studied in the treatment of hospitalized depressive patients. However, this drug has never been marketed.