Glisentide (glypentide) is a hypoglycemic agent and part of the second-generation sulfonamide derivatives. Glisentide is used as an oral medication to control blood sugar levels in patients with diabetes mellitus type 2. Glisentide is patented by Uriach as Staticum®. This compound appears to decrease total lipid and cholesterol levels. Results of glisentide administration in humans showed that this oral hypoglycemic drug was well tolerated and had a similar, and in many instances superior, activity to other similar drugs such as glybenclamide and glipizide.

Glisolamide is a second-generation sulfonylurea with antihyperglycemic activity. Glisolamide is comparable to glyburide and gliquidone in controlling blood glucose levels. It is sold as Diabenor in several countries outside the US.

Halethazole has been studied as an active antifungal compound.

Heptaverine was used as a spasmolytic agent. Information about the current use of this compound is not available.

Balaglitazone is a second generation peroxisome proliferator-activated receptor (PPAR) gamma agonist with only partial agonistic properties. It passed phase III clinical trial for the treatment of type 2 diabetes. However, Dr. Reddy's Laboratories decided to terminate further clinical development of balaglitazone.

Apan (PPI-1019) is the lead compound of a series of β-amyloid-derived peptides designed by Praecis Pharmaceuticals in the US to interact with β-amyloid peptide, facilitating its clearance. Apan is derived from the D-enantiomeric Cholyl-LVFFA-NH2. Apan is developed by Praecis Pharmaceuticals to treat Alzheimer's Disease. Apan inhibits the aggregation of beta-amyloid and its associated nerve cell toxicity. In addition, Apan reaches the brain in quantities that are sufficient to block the aggregation of beta-amyloid molecules and alter the course of the disease. PPI-1019 completed phase I and II clinical trials and was found to be safe, well tolerated and amenable to cross bbb. After peptide administration, levels of Aβ1-40 in the CSF increased, which might be discussed as a sign for Aβ clearance out of the brain. PI-1019 had been in phase I/II clinical trials by Praecis Pharmaceuticals (acquired by GlaxoSmithKline in 2007) for the treatment of Alzheimer's disease(AD). However, this study had been discontinued.

Metioprim is a competitive inhibitor of bacterial dihydrofolate reductase with an in vitro activity against most important gram-negative and gram-positive bacteria causing urinary and respiratory tract infections. The use of this drug was studied in the treatment of pyelonephritis and against atypical mycobacterial infections - especially leprosy. Information about the current use of this compound is not available.

Eprotirome (KB2115) is a thyroid hormone mimetic developed at Karo Bio AB (Huddinge, Sweden). Eprotirome has a 22-fold higher affinity for thyroid hormone receptor (TR)β in comparison with TRα. It lowers plasma LDL cholesterol and stimulates bile acid synthesis. Eprotirome can lower LDL cholesterol concentrations in patients with familial hypercholesterolaemia when added to conventional statin treatment with or without ezetimibe, but that it has the potential to induce liver injury. These findings, along with findings of cartilage damage in dogs, raise serious doubts about selective thyroid hormone mimetics as a therapeutic approach to lower LDL cholesterol concentrations. Eprotirome development was discontinued.

Fenestrel (ORF-3858) is a nonsteroidal antizygotic compound. It antagonizes progesterone. Fenestrel is a post-coital contraceptive.

Idalopirdine (Lu AE58054) is a Serotonin 6 receptor (5-HT6) antagonist. Idalopirdine exrets good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. In rats idalopirdine potentiates the effects of acetylcholinesterase inhibitor donepezil on two pharmacodynamic biomarkers associated with cognition, i.e. neuronal oscillations and extracellular ACh levels in the hippocampus. Such potentiation could contribute to the procognitive effects of idalopirdine observed in donepezil-treated Alzheimer's disease patients. The compound is being developed by Lundbeck as an adjunctive therapy with acetylcholinesterase inhibitor donepezil, and is in phase III development for the treatment of Alzheimer's disease in multiple countries worldwide. A phase II trial for the treatment of cognitive impairment associated with schizophrenia was conducted; however no recent reports of development for idalopirdine have been identified.