Sanfetrinem cilexetil (formerly known as GV 118819), a beta-lactam antibiotic, is the oral prodrug of sanfetrinem. Experiments on rodents have revealed that sanfetrinem cilexetil had strong antibacterial activity in vitro and good pharmacokinetic behavior in mice. This drug was suitable for the treatment of infections caused by a variety of bacteria and participated in a phase II clinical trial. However, this study was discontinued.

Amifloxacin [WIN 49375] is a fluoroquinolone antibacterial with a broad range of activity against aerobic Gram-negative and some aerobic Gram-positive organisms. Amifloxacin is a DNA gyrase inhibitor. The 50% inhibiory concentration for supercoiling activity of E.coli KL16 DNA gyrase of amifloxacin (MIC, 0.10 ug/ml) was 2.47 ug/ml. Amifloxacin was in trials for the treatment of gram-negative infections, septic shock and urinary tract infections. However, development of amifloxacin has been discontinued.

Amotosalen (S-59, psoralen derivative), a chemical capable of binding to nucleic acids is added to platelets. UVA illumination (320 – 400 nm wavelengths) of amotosalen-treated platelet components induces covalent cross-linking of any nucleic acids to which amotosalen is bound; thereby, preventing further replication. Amotosalen is used in the INTERCEPT process to cross-link DNA and RNA. Amotosalen has protective activity against pathogens such as bacteria, viruses, protozoa, and leukocytes. Prior to administration amotosalen is added to plasma and platelets, then in vivo this agent penetrates pathogens and targets DNA and RNA. Upon activation by ultraviolet A light, amotosalen forms interstrand DNA and RNA crosslinks and prevents replication. Thus, the pathogen-inactivation system using amotosalen/ultraviolet A offers the potential to mitigate the risk of ZIKV transmission by plasma and platelet transfusion. Inactivation of leukocytes can prevent graft versus host disease upon transfusion.

Dazopride is an antagonist of the 5-HT3 receptor and agonist of the 5-HT4 receptor, structurally related to metoclopramide. Dazopride was developed by A. H. Robins Company as an antiemetic and gastroprokinetic drug. Dazoptide demonstrated an antiemetic effect in the clinic after i.v. infusion to patients, receiving anticancer therapy.

Sulamserod is a methanesulfonamide derivative patented by British multinational pharmaceutical company GlaxoSmithKline as 5-HT4 receptor antagonist, with antiarrhythmic activities for the treatment of the certain cardiovascular condition. 5-HT4 receptor blockade could have antiarrhythmic effects by decreasing intracellular Ca2+ concentration and delayed rectifier potassium current and prolonging atrial refractory period. In preclinical models, Sulamserod prolongs mean atrial effective refractory period and wavelength, reduces the dispersion of effective refractory period, and minimally slows conduction velocity in pigs.

Atrasentan (ABT-627, A-127722) is a selective endothelin A receptor antagonist. Atrasentan is being developed by AbbVie as an oral treatment for diabetic nephropathies.Abbott Laboratories was conducting clinical development of atrasentan for the treatment of certain cancers, including phase II trials for prostate cancer. However, no recent development has been reported for cancer indications and development is presumed to be discontinued.

Duoperone is a neuroleptic agent. Duoperone blocked d-amphetamine lethality in mice under aggregated conditions when the pretreatment interval was between one hour and seven days. Conditioned avoidance responding in mice and cats was suppressed by duoperone in doses that did not impair escape behavior. Duoperone produced catalepsy in rats. The onset of this effect was delayed and the duration was prolonged when compared with that of chlorpromazine. It was a potent antiemetic agent in dogs, with a delayed onset and prolonged duration of action.

Mexrenoate potassium is an aldosterone antagonist, which was developed as an antihypertensive agent. However, this drug has never been marketed.

Ciclosidomine is morpholine derivative and nitric oxide donors developed for vascular diseases treatment.

Piperamide is substituted piperazine with a tertiary amine group. It was used as an anthelmintic agent. Initially, it was investigated because of its effectiveness against Trypanosoma. Piperamide distorts choroid plexus epithelial ultrastructure by engendering hydropic vacuoles.