Clometherone is an investigational derivative of progesterone, possessing antiestrogen and antiandrogen activities. It was developed by Eli Lilly in the 1960s and was found to significantly suppress the estrone induced uterine hypertrophy in mice at an oral or subcutaneous dose of 10ug. In a clinical trial, administration of clometherone to adult males lead to a slight increase in sebum production.

Otenabant (CP-945,598) is Pfizer developed as a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, which exhibits 10,000-fold greater selectivity against human CB2 receptor, for treatment of obesity. In clinical trial III Pfizer decided to discontinue the development program based on changing regulatory perspectives on the risk/benefit profile of the CB1 class and likely new regulatory requirements for approval.

Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.

Iometopane I-123 is a tropane derivative labeled with iodine-123 that was being developed by MGI GP (MGI Pharma) as an injectable Single-photon emission computed tomography (SPECT) imaging agent. The ability of iometopane to bind to the dopamine transporter on presynaptic dopaminergic nerve terminal in the striatum has been used to differentiate the uptake of the agent by the neurons in the striatum in patients with a Parkinsonian disorder from patients without a Parkinsonian disorder with high sensitivity and specificity. The diminished uptake of iometopane in the striatum on the SPECT images of patients with a Parkinsonian disorder can be applied to assess both disease trait and disease state (severity) reflected by the severity of the brain dopamine neuron loss. Unfortunately Phase III clinical trials and further development of iometopane was discontinued due to the inability to contract a suitable manufacturer for the clinical and commercial supply of iometopane on acceptable conditions in the US. Currently, Iometopane is mainly used in scientific research into the dopamine reuptake transporter.

Tianafac (also known as L8109) is a thienylacetic acid derivative patented by Labaz group as antipyretics and anti-inflammatory agent useful for the treatment of arthritis. In preclinical models, Tianafac inhibits prostaglandin formation by seminal vesicle microsomes and exerts antipyretic, analgetic, and moderate gastric ulcerogenic activity and had a wide safety margin between toxic and pharmacologically active doses.

Pheneridine is a synthetic opioid. It was developed as a narcotic agent.

Carbubarb is hydroxyalkylmalonylurea derivatives patented by pharmaceutical company Consortium Mondial des Grandes Marques as sedatives and hypnotic agent.

Talmetacin is a cyclo-oxygenase inhibitor that was studied as an analgesic and antipyretic agent. This drug was studied in Argentina in patients with rheumatic disorders. However, further development of talmetacin is not available.

Idremcinal (previously known as EM574), a motilin receptor agonist, has been studied for the treatment of gastritis. The drug was involved in phase II in Japan for the treatment of chronic gastritis and Gastro-esophageal reflux in the USA. However, the development of the drug was discontinued.