Acefurtiamine is a vitamin B1 analog. It is as an analgesic.

Difenoximide is a water insoluble derivative of diphenoxylate, a chemical congener of meperidine. Difenoximide has been shown to have a greater ability than methadone to suppress opiate withdrawal in addicted mice and it has produced less physical dependence than morphine and methadone in laboratory animals. Since diphenoxylic acid is the major metabolite of both difenoximide and diphenoxylate, it is assumed that difenoximide will have essentially the same dependence liability and long-term toxicologic effects as those of diphenoxylate. Difenoximide has been given to human volunteers and it showed antidiarrheal action without side effects. Difenoximide appeared to be a potentially useful agent for ambulatory narcotic detoxification. The only significant side-effect was constipation.

Dimesna is a prodrug of mesna (dimer of mesna). Dimesna is reduced to mesna in the kidneys. Dimesna does not prevent cellular damage by metabolites of ifosfamide and cyclophosphamide in the renal tubular cell line LLC-PK1. Dimesna is a mucolytic agent used to alleviate toxic side effects of antitumor drugs. The organic acid transporter OAT4 on the luminal side of the proximal renal tubule facilitates the reabsorption of dimesna, and therefore its reduction to mesna, whereas the multidrug and toxin extrusion protein MATE1, the multidrug resistance protein MRP2, and P glycoprotein facilitate the efflux of mesna and/or dimesna back into the lumen; dimesna may also be excreted unchanged by MRP4. It has therefore been suggested that polymorphism of these renal transport proteins or transporter-mediated drug-drug interactions may reduce the efficacy of mesna and dimesna.

FLETAZEPAM, a benzodiazepine derivative, is a centrally-acting muscle relaxant more effective than diazepam in preventing convulsions and muscle rigidity.

Sudoxicam is a nonsteroidal anti-inflammatory drug patented by American multinational pharmaceutical corporation Pfizer for the treatment of thrombosis. Sudoxicam strongly inhibited aggregation of rabbit, dog, and human platelets caused by collagen, but not by ADP. Sudoxicam inhibited the secondary phase of the biphasic response of guinea pig platelets to ADP and suppressed the release of ADP from human platelets caused by collagen. Sudoxicam shows superior anti-inflammatory activity compare to indomethacin in rat paw edema model. In clinical trials, sudoxicam was associated with several cases of severe hepatotoxicity that led to its discontinuation.

Oxfenicine is a CPT-1b-specific inhibitor. It must be transaminated to its active form, 4-hydroxyphenyl-glyoxylate, which is competitive with carnitine, preventing the formation of acylcarnitine. Because CPT-1b shows the highest sensitivity to 4-hydroxyphenyl-glyoxylate, inhibition of fatty acid oxidation by oxfenicine takes place selectively in those tissues that express this CPT isoform. It may be effective for treating noninsulin-dependent diabetes mellitus which is characterized by elevated fatty acid levels and obesity. In 1980 it was also tested in preclinical models of angina pectoris and ischemia.

Furacrinic acid (also known as GP 48 674) was studied as a diuretic agent and participated in clinical trials. However, information about the further development of this drug is not available.

Isamoltan (CGP 361A) is a β-adrenoceptor and serotonin 1B receptor antagonist. Isamoltane has reported activity as an anxiolytic in man. Isamoltan had been in phase III clinical trials for the treatment of anxiety. However, this research has been discontinued.

Milacemide, a prodrug for glycine, is an inhibitor of the B form of monoamine oxidase. This drug could enhance dopaminergic activity in the brain and could be used as therapy for Parkinson's disease. Milacemide participated in clinical trials as a treatment for senile dementia of the Alzheimer type (SDAT). However, results have shown the drug was not an effective treatment in enhancing cognition in SDAT patients. In addition, milacemide has been tested for antiepileptic efficacy; however, this study was discontinued.