Roxolonium, a derivative of glycyrrhetic acid, was studied as an antiulcer agent. Information about the further development of this compound is not available.

Thiarabine (also known as OSI-7836) is a new-generation deoxycytidine nucleoside analog with potent anticancer activity. As with other nucleoside analogs, Thiarabine is a prodrug and requires intracellular phosphorylation by deoxycytidine kinase to the active form (Thiarabine-triphosphate), which then competes with deoxycytidine for incorporation into DNA resulting in cell death. In xenograft studies using lung, colon, pancreatic, breast, and melanoma models, Thiarabine shows superior antitumor activity in most of these tumors, particularly in lung and pancreatic models, compared with gemcitabine, cisplatin, and paclitaxel. Thiarabine seems to be less schedule dependent than gemcitabine, showing antitumor activity with a variety of schedules in preclinical studies. In clinical trials, Thiarabine administration was associated with excessive fatigue, and despite changes in its schedule and duration of administration.

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.

Relomycin is a macrolide antibiotic that was first reported in the literature in 1963. It is a fermentation product of Streptomyces hygroscopicus and has also been observed in cultures of Streptomyces fradiae (a species of Actinobacteria).

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.

Cloracetodol is a para-aminophenol NSAID analgesic with anti-inflammatory and antipyretic activity.

Brolaconazole is imidazole derivative with potent antimicrobial activity against pathogenic fungi, molds, yeasts, and Gram-positive bacteria. Brolaconazole showed an inhibition band of 20-40 mM against Candida albican and it demonstrates higher activity compare bifonazole. Brolaconazole is useful for the treatment of dermal and vaginal infections such as vaginal candidiasis, tinea corporis, tinea pedis, tinea cruris, and other dermal infections.

1-(2-DEOXY-2-FLUORO-β-D-ARABINOFURANOSYL)URACIL (FAU) is a thymidine analog. In several cancer cell lines, FAU was phosphorylated intracellularly to its monophosphate, 1-(2-deoxy-2-fluoro--Darabinofuranosyl) uracil monophosphate (FAUMP), by thymidine kinase and methylated in the 5-position by thymidylate synthase to form the product, 1-(2-deoxy-2-fluoro- -D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FAU strongly inhibits the growth of tumor cells with high thymidylate synthase activity. FAU had been in phase I clinical trial for the treatment of advanced solid tumors.

Pracinostat is a pan-histone deacetylase inhibitor being tested in phase II of clinical trials for the treatment of sarcoma, prostate cancer, acute myeloid leukemia, myelofibrosis, myelodysplastic syndrome. The drug was shown to be active in vitro on HCT116 and HL-60 cells.