Oxeglitazar (also known as EMD 336340 or LM 4156), an orally administered poorly water-soluble dual peroxisome proliferator-activated receptor α/γ agonist. This drug was used in the treatment of type II diabetes mellitus and metabolic syndrome. In addition, oxeglitazar participated in phase I trials for the gout treatment; however, this study was halted. Information about the further development of this drug is not available.

Avasimibe (CI 1011) is a potent ACAT (Acyl-CoA:cholesterol acyltransferase) inhibitor. Avasimibe inhibits both ACAT1 and ACAT2 isoforms. Avasimibe was in development by Parke-Davis (now Pfizer) in the US for the treatment of atherosclerosis and hyperlipidaemia. Avasimibe was in phase III studies and more than 1300 patients had been treated for up to one year, however, in October 2003, Pfizer announced that development had been discontinued.

Saroglitazar, a dual peroxisome proliferator-activated receptor PPAR-α/γ agonist, was an emerging therapeutic option on glycemic and lipid parameters. The Zydus Group has launched LipaglynTM ((Saroglitazar) in India for diabetic dyslipidemia and hypertriglyceridemia with type 2 diabetes mellitus not controlled by statin therapy. In addition, saroglitazar participated in phase II clinical trials that completed enrolment in patients with primary biliary cholangitis and in patients with non-alcoholic steatohepatitis.

TAK-875 (Fasiglifam) is the potent, selective and orally bioavailable GPR40 agonist. The drug was in Phase III clinical trials for the treatment of type 2 diabetes mellitus. Termination phase III development of TAK-875 for the potential treatment of type-2 diabetes mellitus was announced in 2013 due to concerns about liver safety.

Diethylhomospermine is the polyamine analogue. It suppressed the activity of the major biosynthetic enzymes, ornithine decarboxylase and S-adenosylmethionine decarboxylase in human bladder cancer cell lines. Diethylhomospermine given as the subcutaneous injection is overall well tolerated at lower doses, but significant toxicities were observed at the 37.5mg/m2/day dose level. Maximal tolerated dose was established at 25 mg/m2/day but further investigation with this study drug is not recommended secondary to the potential for neurotoxicities and hepatic damage as a result of cumulative doses. Diethylhomospermine had been in phase II clinical trials for the treatment of AIDS-related chronic diarrhea. However, this research has been discontinued.

LAPAQUISTAT is a squalene synthase inhibitor. It was shown to lower cholesterol levels in several animal models. It was investigated for the treatment of diabetes and hypercholesterolemia, however, its development was discontinued.

Tocofibrate is a peroxisomotropic ester compound consisting of both clofibric acid and alpha-tocopherol. Tocofibrate is a hypocholesterolemic drug. Lowering activity of tocofibrate in cholesterol level in blood was no less than that of clofibrate in rats fed high-fat cholesterol diet. In view of the fact that only a fraction of tocofibrate is not hydrolyzed in the liver 24-hr following oral administration, it was reasonable to assume that tocofibrate exerts its effect in an unaltered state rather than as a result of hydrolysis to clofibric acid and alpha-tocopherol. The distribution of tocofibrate clearly differs from that of both clofibrate and alpha-tocofibrate is primarily associated with its effect upon liver peroxisomes. Tocofibrate acts upon peroxisomes to lower plasma lipid levels.

Camiglibose is a glucopyranoside and inhibitor of alpha-glucosidase with antihyperglycemic activity patented by Merrell Dow Pharmaceuticals. In rats, a single oral dose of Camiglibose administered simultaneously with 2 g/kg body wt sucrose resulted in a dose dependent reduction in the area under the 0- to 3-h glycemic response curve, A reduction in the glycemic response to sucrose was accompanied by reduced insulin secretion. Camiglibose was more effective against a sucrose load in streptozocin-administered rats than in control rats and was as effective after 16 daily doses as after a single dose. Doses that reduced the glycemic response to carbohydrate did not inhibit liver lysosomal a-glucosidase activity or cause lysosomal glycogen accumulation. In cynomolgus monkeys, an oral dose of 1 mg/kg Camiglibose reduced the glycemic and insulin responses to sucrose

Spiriprostil (IBI-P-01028 or R,S-cis-6-(6'-carboxyhexyl)-7-trans-n-hexyl-1,3-diazaspiro-[4-4]-nona n-2,4- dione) is a cytoprotective agent. It is an anti-ulcer agent.