Butafosfan is a phosphororganic supplement that is given, most commonly with cyanocobalamin, to cattle, swine, horses, and poultry for the prevention or treatment of phosphorus deficiencies. Butafosfan also plays a vital role in hepatic carbohydrate metabolism. In addition, butafosfan has been regarded as an antistress agent in combination with vitamin B12. Studies with butafosfan in different animals have shown that it improved general health status by stimulating feed intake, immune system, and digestive function. Butafosfan has been reported for the treatment of metabolic disorders caused by stress or nutrition problems in various species.

Vofopitant (previously known as GR205171), a tetrazole-derivative, was developed as a neurokinin1 receptor antagonist. Vofopitant was studied in clinical trials phase II for the treatment of primary insomnia and posttraumatic stress disorder. However, these studies were discontinued due to lack of effectiveness. In addition, vofopitant participated in phase I for patients with bipolar disorder. However, this study was terminated because of the slow recruitment; trial unlikely to reach completion.

Melquinast is an antiasthmatic, antiallergic substance not acting primarily as antihistamines.

Espatropate (UK 88060) is an antagonist of M3 muscarinic receptors. Espatropate is a bronchodilator with anticholinergic activity. It was undergoing preclinical development with Pfizer for the treatment of asthma.

Moxastine is a diarylmethane derivative with an antihistamine and anticholinergic activities.

Ruboxistaurin is an orally bioavailable, selective, potent inhibitor of protein kinase C β developed for treating diabetic retinopathy. In vitro and in vivo non-clinical models have demonstrated that Ruboxistaurin decreases PKC β activity and ameliorates many of the effects of PKC β on pathologic processes in the retina. Ruboxistaurin prevents the slowing of retinal blood flow that is observed by fluorescein video angiography in the eyes of diabetic rats. It is also reported to cause regression of retinal neovascularization produced by laser-induced major branch vein occlusions in a porcine model. Ruboxistaurin positively affected the diabetes-induced retinal blood flow abnormalities in a Phase Ib study in diabetic patients. Ruboxistaurin is in phase III clinical trials for the treatment of diabetic nephropathy and diabetic macular edema. Eli Lilly had submitted Ruboxistaurin for approval in the US and the EU; however, the company subsequently discontinued development as it was unable to demonstrate sufficient efficacy

Etibendazole (R34803 or methyl [5-(2-(4-fluorophenyl)-1,3-dioxolan-2-yl)-1H-benzimidazole-2-yl] carbamate), a benzimidazole derivative, is a microtubule inhibitor. Etibendazole exerts antihelmintic activity.

Varespladib (LY315920; A-001) is a potent and selective inhibitor of IIa, V, and X isoforms of human non-pancreatic secretory phospholipase A2 with nM IC50. The molecule acts as an anti-inflammatory agent by disrupting the first step of the arachidonic acid pathway of inflammation. Varespladib methyl is being developed by Anthera Pharmaceuticals Inc for the potential treatment of coronary artery disease, acute coronary syndrome and inflammation. Varespladib methyl is a prodrug that is rapidly metabolized to varespladib, and both compounds are able to potently inhibit the enzymes of the human secretory phospholipase groups. Phase II clinical trials of varespladib methyl in patients with coronary artery disease, rheumatoid arthritis, asthma and ulcerative colitis revealed that the drug was well tolerated. Varespladib methyl did not demonstrate a good efficacy profile in patients with rheumatoid arthritis, asthma and ulcerative colitis; whereas in patients with coronary artery disease, varespladib methyl consistently reduced LDL-cholesterol levels, (elevated LDL-cholesterol levels are a marker of increased cardiovascular risk). Varespladib methyl could represent a novel therapy for the treatment of cardiovascular disease, although the efficacy, safety profile and advantages of this drug compared with existing therapeutic options would need to be established in upcoming phase III trials.

Zosuquidar (LY-335979) is an experimental antineoplastic drug. It is is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Zosuqidar was initially characterized by Syntex Corporation, which was acquired by Roche in 1990. Roche licensed the drug to Eli Lilly in 1997. It was granted orphan drug status by the FDA in 2006 for AML. Zosuquidar Trihydrochloride had been in phase III clinical trials by Kanisa Pharmaceuticals for the treatment of acute myeloid leukaemia. However, this research has been discontinued.

Glicondamide is a derivative of sulphonamides (antibacterial sulfa drugs). It acts by increasing the release of insulin from pancreatic beta cells, resulting in lower blood glucose levels.