IROXANADINE, a pyridine derivative, is under development for the treatment of atherosclerosis and the complications of atherosclerosis such as ischaemic heart disease, peripheral arterial disease, and restenosis. It induces phosphorylation of p38 stress-activated protein kinase, which plays an important role in endothelial cells (EC) homeostasis. EC function plays a central role in vascular diseases.

Lambda-cyhalothrin (λ-cyhalothrin), a mixture of isomers of cyhalothrin belongs to a class of insecticides known as synthetic pyrethroids. Synthetic pyrethroids are often preferred to the real thing as an active ingredient because they offer the added bonus of remaining effective for longer period. λ-cyhalothrin was the most commonly used pyrethroid insecticide for vegetable farming in Benin. Experiments have shown that λ-cyhalothrin residues in lettuce and cabbage from farms and markets in Parakou and Cotonou were relatively safe for consumption.

Alozafone is an anticonvulsant (CNS depressant).

Enerisant is a histamine H3 receptor antagonist. In H3 receptor binding assay using (R)​-​α-​methyl[3H]​histamine, enerisant showed IC50 of 4.9 nM. Enerisant may be useful for the treatment of Alzheimer's disease, schizophrenia, etc.

Enerisant is a histamine H3 receptor antagonist. In H3 receptor binding assay using (R)​-​α-​methyl[3H]​histamine, enerisant showed IC50 of 4.9 nM. Enerisant may be useful for the treatment of Alzheimer's disease, schizophrenia, etc.

4-Isothioureidobutyronitrile (Kevetrin) is a small molecule that has demonstrated the potential of becoming a breakthrough cancer treatment by inducing activation of p53. It is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity. Upon intravenous administration, 4-thioureidobutyronitrile activates p53 which in turn induces the expressions of p21 and PUMA (p53 up-regulated modulator of apoptosis), thereby inhibiting cancer cell growth and causing tumor cell apoptosis. 4-Thioureidobutyronitrile may be effective in drug-resistant cancers with mutated p53. p53 tumor suppressor, a transcription factor regulating the expression of many stress response genes and mediating various anti-proliferative processes, is often mutated in cancer cells. Cellceutix continues to build upon the successful Phase 1 trial evaluating Kevetrin in treating advanced solid tumors conducted at Dana-Farber Cancer Institute and Beth Israel Deaconess Medical Center. Kevetrin, in IV form, was shown to safely modulate, in a non-genotoxic manner, the key tumor suppressor protein p53 as measured through increased expression of p21, a key downstream biomarker of p53. Cellceutix is advancing Kevetrin under an Orphan Drug designation from the Food and Drug Administration (FDA) for the treatment of ovarian cancer, pancreatic cancer and childhood retinoblastoma.

Domoxin is a hydrazine derivative. It is monoamineoxidase inhibitor. Domoxin was developed as antithrombotic agent.

Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.