Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.

Droxacin is quinolone antibiotic. It is topoisomerase inhibitor.

Octimibate is a non-prostanoid inhibitor of platelet aggregation that acts via the prostacyclin receptor.

Tiomolibdic acid salt, Bis-choline tetrathiomolybdate (ATN-224, WTX-101), is under investigation as a therapy against different cancers and Wilson’s disease (WD). ATN-224 is a second-generation analog of ammonium tetrathiomolybdate. ATN-224 is a novel copper chelator. ATN-224 inhibits CuZn superoxide dismutase 1 (SOD1) leading to antiangiogenic and antitumor effects. Strategically tailoring combination regimens that include ATN-224 and target ROS may be a viable approach to advance the treatment of melanoma. ATN-224 is in phase III clinical trial for the treatment of Hepatolenticular degeneration. WTX-101 is in phase II clinical trials for the treatment of Wilson's disease. Once daily WTX-101 treatment over 24 weeks improved neurologic disease, hepatic status and copper control in newly diagnosed WD patients. WTX-101 appears well tolerated. Drug-induced, paradoxical, neurological deterioration was not observed. This compound has received orphan drug designation in both the United States and the European Union. WTX-101 was originally discovered by University of Michigan and now is being developed by Wilson Therapeutics by acquisition.

Lifibrol is a hypocholesterolemic compound. The effect of lifibrol on serum cholesterol levels has been examined in several animal models and clinical trials. The efficacy of lifibrol in lowering total cholesterol, LDL cholesterol, and apo B is comparable to the 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, the most potent lipid-lowering drugs known so far. In addition, lifibrol reduces serum triglycerides, lipoprotein (a), and fibrinogen. lifibrol acts synergistically upon key regulatory processes of cholesterol homeostasis: it reduces cholesterol absorption from the intestine, moderately decreases hepatic cholesterol biosynthesis and stimulates the expression of low density lipoprotein receptors, presumably by a sterol-independent mechanism. Lifibrol had been in phase II clinical trials for the treatment of hypercholesterolaemia. However, this study was discontinued. It has the potential to accumulate in the liver and induce hepatic peroxisome proliferation.

Methoprene is a pesticide that acts as a juvenile hormone agonist. Although developed initially against insects, it has since been shown to have toxic effects on larval and adult crustaceans. Methoprene was one of the several pesticides applied to the Western Long Island Sound (WLIS) watershed area during the summer of 1999. Methoprene is a racemic mixture of two enantiomers (R and S in a ratio of 1:1). The activity of the compound as a juvenile hormone is restricted to the S enantiomer. Recent data have been describing the male sexual enhancement after methoprene treatment in Anastrepha fraterculus (Diptera: Tephritidae). It has been shown, that a sustained response doesn`t not fade away after sexual maturation, thus the potential benefits of using methoprene to increase the efficiency of the sterile insect technique, which is an environmentally safe method to control this fruit pest, have been proposed.

Propenzolate is a pyridine derivative patented by National Research Development Corp. as an anticholinergic agent. Propenzolate is effective antidotes to the cholinesterase-inhibiting action of various organophosphorus compounds. In clinical trials, Propenzolate has an activity that decreases to some extent the secretion of hydrochloric acid and the volume of gastric juice. Adverse effects, including nausea, vomiting, weakness, and drowsiness, as well as xerostomia and cycloplegia, are observed in a high percentage of patients receiving 0.5 to 1.0 mg. every 12 hours.

Furegrelate (previously known as U-63557A), a selective orally active thromboxane synthase inhibitor, with potential for the treatment of various diseases including hypertension, thrombosis, and renal disorders, arrhythmias, but these studies were discontinued.

Indoximod is an orally available Indoleamine 2,3-dioxigenase inhibitor. It shows higher potency in reversing IDO-mediated T cell suppression. Indoximod improves the efficacy of multiple chemotherapeutics agents and some immunological checkpoints mediators in Phase I/II clinical studies for metastatic breast cancer, metastatic melanoma, non-small cell lung cancer, primary malignant brain tumors, metastatic pancreatic cancer, as well as metastatic prostate cancer.