Meglitinide (HB 699) is an antidiabetic compound. Meglitinide is a short-acting insulin secretagogue that targets one of the main defects that characterizes type 2 diabetes: the progressive loss of early phase prandial insulin secretion. It acts in a glucose-dependent manner to close adenosine triphosphate (ATP)-dependent potassium channels on the β-cell membrane, depolarize the β-cell, resulting in the opening of calcium channels, increased calcium influx and insulin secretion.

Englitazone is a thiazolidinedione antidiabetic agent. It has insulinomimetic and insulin-enhancing actions in vitro and glucose-, insulin-, triglyceride-, and cholesterol-lowering properties in an animal model of non-insulin-dependent diabetes mellitus. It acts as a peroxisome-proliferator-activated receptor-gamma ligand. Englitazone inhibits ATP-sensitive potassium and calcium-activated non-selective cation channels in a voltage-independent manner.

Moctamide is a synthetic linoleamide derivative patented by major Japanese chemical company Sumitomo Chemical Co., Ltd. as hypocholesterolemic agent useful as prophylactics against arteriosclerosis. Administration of Moctamide significantly lowered serum and liver cholesterol and significantly prevented formation of aortic atheromatous changes in animal models.

Molfarnate is difarnesyl compound patented by Kotobuki Seiyaku as an antiulcer and anti-inflammatory agent. In combination with a bisphosphonate, Molfarnate may also be useful for osteoporosis treatment.

Clinolamide (cyclohexylamine of linoleic acid) is a drug developed by a Japanese company Sumitomo Chemical Co. Ltd. Clinolamide has been found to lower serum and liver cholesterol levels and to reduce the severity of atherosclerosis in cholesterol-fed rabbits.

Teglicar, an antihyperglycemic agent, is a carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor that was studied for the treatment of type 2 diabetes. The drug participated in phase II clinical trial in Italy; however, the further development apparently was discontinued.

Rivoglitazone hydrochloride (CS-011) is a thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist. It has been developed as potential treatment in type 2 diabetes mellitus and was shown to decrease plasma glucose and triglyceride levels in a dose-dependent manner in animals. Phase II and III clinical studies have assessed the efficacy and safety of rivoglitazone hydrochloride in patients with type 2 diabetes mellitus.

Tizoprolic acid is an anti-lipolytic drug, a blood ketone lowering agent.

Lobeglitazone (trade name Duvie; Chong Kun Dang Pharmaceutical Corporation) was developed as effective and safe antidiabetic TZD drug. Lobeglitazone is a peroxisome proliferator-activated receptor-γ agonist. Lobeglitazone was conceptually designed by modification of the rosiglitazone structure with a substituted pyrimidine. Lobeglitazone has a p-methoxyphenoxy group at the 4-position of the pyrimidine moiety. Lobeglitazone showed more potent activity than the reference compounds (pioglitazone and rosiglitazone) with an EC50 value of 0.018 uM in a type 2 diabetes animal model, which is 16 times lower than pioglitazone (EC50 0.30 uM). Lobeglitazone exhibited similar efficacy profiles in glycemic control and lipid modulation to pioglitazone, but with a 30 times smaller dose in clinical studies. Lobeglitazone displays 12 times higher affinity to PPARγ than rosiglitazone and pioglitazone. Lobeglitazone acts as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By promoting the binding of insulin at fat cells, lobeglitazone has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles. Lobeglitazone was approved by the Ministry of Food and Drug Safety (Korea) in 2013. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.

Tolpentamide is a first-generation cyclopentyl-containing sulfonylurea with the hypoglycemic activity. It has never been marketed.