Dupracetam is the piracetam derivative. It is amide type nootrope agent (cognition enhancer). Dupracetam was developed as central stimulant. Metabolite of dupracetam, 1-Methylhydantoin, was shown to be cytotoxic for renal proximal tubular cells.

Ritrosulfan (also known as R-74 and Lycurim) is a sulfonate-based alkylation agent that might exert antineoplastic activity, acting to stop the development of a tumor. By alkylating DNA and producing crosslinks, ritrosulfan is thought to cause tumor cell cycle arrest. However, no alkylating activity could be demonstrated in the plasma of cancer patients, using intracavitary application of ritrosulfan. Other studies in the 1980’s have confirmed some immunodepressive properties of ritrosulfan in cancer patients, but no information is available on current development of ritrosulfan.

Bicyclomycin has been used to treat diarrhea in humans and bacterial diarrhea in calves and pigs and is marketed by Fujisawa (Osaka, Japan) under the trade name Bicozamycin. This drug is the selective inhibitor of rho, a member of the RecA-type ATPase class of enzymes that use nucleotide contacts to couple oligonucleotide translocation to ATP hydrolysis.

FENETHAZINE was a first-generation phenothiazine-derived antihistamine drug. Promethazine was derived from FENETHAZINE.

Stannsoporfin is a mesoporphyrin derivative patented by Rockefeller University as competitive heme oxygenase (HO) inhibitor for the prevention of hyperbilirubinemia in infants at risk of developing jaundice. Parenteral administration of Stannsoporfin has been shown to suppress or moderate jaundice in a wide variety of experimental and naturally occurring forms of hyperbilirubinemia in animals and man. Stannsoporfin is rapidly cleared from the plasma in animals, in adult humans, and in newborn infants and may inhibit competitive heme oxygenase for prolonged periods. The Stannsoporfin decreases the production of carbon monoxide from heme and increases the biliary excretion of unmetabolized heme but has no effect on the metabolic disposition of preformed bilirubin.

Clazosentan is an endothelin receptor antagonist, developed by the Swiss pharmaceutical company Actelion, and licensed to its spin-off, Idorsia. The drug was designed to inhibit endothelin-mediated cerebral vasospasm and associated delayed ischaemic neurological deficit. The drug has been investigated in a phase III clinical trials in patients with aneurysmal subarachnoid hemorrhage. Clazosentan at 5 mg/h had no significant effect on mortality and vasospasm-related morbidity or functional outcome. Clinical investigation of a higher dose of the drug is underway.

Furaprevir (also known as TG-2349), an NS3/4A protease inhibitor, discovered and developed by TaiGen for the treatment of chronic hepatitis C. Furaprevir blocks the protease enzyme that is essential in hepatitis C virus replication. In April 2019, TaiGen started the Phase III trial of the combination therapy Furaprevir - Yimitasvir for the treatment of chronic hepatitis C patients.

Biclofibrate was investigated as an antilipidemic agent.

Necopidem, a zolpidem derivative, is an anxiolytic and sedative drug.