Gliflumide is a compound with a long-lasting hypoglycemic effect. This blood glucose lowering sulfonamide has shown a large decrease of blood glucose levels in healthy volunteers who where administered the drug orally or intravenously. A very similar reaction but delayed and prolonged response was observed for this drug compared to other insulin secretion-stimulating compounds (such as glibenclamide). High affinity of gliflumide to plasma proteins has been suggested to contribute to this delayed activity.

Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist. Binds to the ligand-binding domain (LBD) of human FXR. Turofexorate Isopropyl resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. Turofexorate Isopropyl promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. Turofexorate Isopropyl had been in phase I clinical trials for the treatment of hyperlipidemia. This compound was originally discovered by Exelixis Pharmaceuticals, then licensed to Wyeth (now a wholly-owned subsidiary of Pfizer). However, the studies were discontinued.

Tiafibrate is a dithiahexadecanediol derivative patented by Juste S. A. Quimico-Farmaceutica as a hypocholesteremic agent. In rats, Tiafibrate at 125 mg/kg day orally for 14 days gave a 38.8% decrease in blood lipids and a 33.7% decrease in blood cholesterol.

Soraprazan (remofuscin), a potassium-competitive acid blocker (P-CAB; formerly called an acid pump antagonist [APA]), is being developed by Katairo GmbH for the treatment of Stargardt's disease and dry age-related macular degeneration (AMD). Clinical development is underway for Stargardt's disease and dry age-related macular degeneration in the Netherlands and Germany. On 13 November 2013, orphan designation was granted by the European Commission to Katairo GmbH, Germany, for soraprazan for the treatment of Stargardt’s disease. Soraprazan is a a highly potent reversible, and fast-acting inhibitor of gastric H,K-ATPase. Soraprazan shows immediate inhibition of acid secretion in various in vitro models and in vivo and was found to be more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.

Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.

Eldacimibe is a Meldrum's acid derivative that inhibits sterol O-acyltransferase and oxidative modification of LDL.

Deloxolone was devoid of aldosterone-like properties. Deloxolone could be of therapeutic value in peptic ulcer diseases without inducing fluid retention, hypertension and hypokaliemia. Carbenoxolone and deloxolone were orally administered to healthy volunteers in a cross-over double-blind trial. Both the concentration in gastric juice and the output of PGE2, determined by an RIA method in basal conditions and after pentagastrin bolus, increased in drug-treated compared to vehicle-treated subjects thus supporting the hypothesis that cytoprotection might be due to gastric PGE, levels. Moreover, deloxolone induced less marked effects than carbenoxolone on body weight, hematocrit, plasma potassium and proteins, confirming that deloxolone is less similar to aldosterone than the reference drug.

Glysobuzole (stabinol) is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glysobuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.