Glypinamide is a part of the second-generation sulfonamide derivatives. Members of this group of compounds are used to control blood sugar levels in diabetes mellitus type 2.

Glisamuride is a hypoglycemic agent and part of the second-generation sulfonamide derivatives. Sulphonylureas are used as medication to control blood sugar levels in patients with diabetes type 2. Compared to other hypoglycemic agents, glisamuride exerts greater binding affinity for peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity. This type of compound has also been studied for effects on tumor growth. In one study, several sulfonyl urea derivates, among which glisamuride, were shown to inhibit the adherence of intravenously injected carcinosarcoma cells to the vascular endothelium of the rat mesentery, and to significantly reduce the rate of instantly occurring terminal tumor cell embolism of the lung.

Glipalamide (Glipolamid) is a hypoglycemic agent and part of the second-generation sulfonamide derivatives. These sulphonylureas are used as medication to control blood sugar levels in patients with diabetes type 2. Like other sulphonylureas, glipalamide exerts extra-pancreatic activity. The antihyperglycemic action of this compound (and other sulphonylureas) may be explained by increased affinity of insulin receptors and the stimulating action of these compounds on peripheral glucose metabolism. Glipalamide was analyzed for its physical-chemical properties. After oral administration in animals, no differences were observed in insulin concentration between experimental and control groups, despite a significant fall in blood glucose level.

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.

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.

Picartamide had potent antisecretory and antiulcerogenic effects which were, at least, 10 times more pronounced than those of cimetidine. The mechanism of action of picartamide has not yet been determined but it seems that an anticholinergic or an H2 receptor antagonist effect should be excluded. The results show that picartamide is also active on the pure vagus-stimulated gastric acid secretion. The lack of effect upon gastric pepsin and plasma PP suggests that picartamide is not likely to act on the basolateral cholinergic receptor and that it affects further cellular steps involved in hydrogen ion secretion.

Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which is accompanied by an increase in the plasma level of 25-hydroxyvitamin D3. Treatment with peraclopone dramatically alters membrane sterol content in many membranes including the microvillus membrane of both the jejunum and ileum. In the jejunal microvillus membrane a major change in chemical composition occurred, presumably in response to the alteration in membrane sterol. The net result was a significant decline in both the static and dynamic component of membrane fluidity.

Metibride was developed as an antilipidemic agent. 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.