Norbolethone is a 19-nor anabolic steroid first synthesized in 1966. During the 1960s it was administered to humans in efficacy studies concerned with short stature and underweight conditions. It has never been reported by doping control laboratories prior to 2001. Norbolethone matches the description for what is described as a "designer steroid. " In fact, Norbolethone was given in clinical trials over 30 years ago and never given the green light. No supply was ever manufactured, and no test was ever developed to detect this substance, yet ironically, it was suspected of being used in the 2000 Olympics based on blood and urine assays done by the IOC. Norbolethone was used in the treatment of idiopathic underweight, prevention of indomethacin-induced intestinal ulcers.

Furaprofen (also known as R-803), a nonsteroidal drug possesses anti-inflammatory properties. This drug was studied for the treatment of rheumatoid arthritis. However, information about the further development of this drug is not available.

Dimepheptanol is one of the phenylpiperidine series, an opioid receptor agonist, which is active as an opioid analgesic. It is also elaborated in a number of close analogues, derivatives or diastereoisomers with similar properties. Dimepheptanol is a synthetic narcotic analgesic that has no accepted medical use in the United States.

Secoverine is a selective muscarinic receptor antagonist that was studied as a neurotropic spasmolytic agent. It was shown that the drug had no nicotinolytic or antihistaminic activity, a moderate antisterotonic activity, an inhibiting effect on the noradrenaline uptake mechanism of the vas deferens and marked local anesthetic activity.

Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of the non-steroidal anti-inflammatory drug (NSAID) naproxen that is hydrolysed to pharmacologically active naproxen once absorbed. Naproxen etemesil was in development with Logical Therapeutics for the treatment of osteoarthritis. However, no recent development has been reported. It is also in phase I clinical trials for the treatment of inflammation and arthritis.The compound was originally developed by Medinox, licensed to Logical Therapeutics in 2006 for partial rights.

Rioprostil is a methylprostaglandin E1 analog. Rioprostil inhibits gastric acid secretion and enhances the gastric mucus-bicarbonate barrier. In peptic ulcer cases, it facilitates the healing process and the elimination of pain. Rioprostil can also be used to prevent recurrence of duodenal ulcers. However, its development has been discontinued in 2000.

Meisoindigo ((E)-1,1'-dimethyl-[3,3'-biindolinylidene]-2,2'-dione) is a derivative of Indigo Naturalis, that has been used in China for chronic myeloid leukemia. In vitro cell line studies have shown that this agent might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML). Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In phase III clinical trial of Meisoindigo involving 402 patients, it was shown that Meisoindigo was equally efficient for both newly diagnosed and previously treated CML patients after oral administration. The hematological complete response (CR) and partial response (PR) rates, respectively, were 45.0 and 39.3% for newly diagnosed patients and 35.9 and 41.4% for previously treated patients. Meisoindigo was generally well tolerated. The most frequent side‑effects were bone, joint and/or muscle pain of varying degrees when the dosage was more than the suitable one.