Tolrestat is an orally active aldose reductase inhibitor. It was used for the pharmacological control of certain diabetic complications. It was discontinued by Wyeth in 1997 because of the risk of severe liver toxicity and death.

Epomediol (trade name Clesidren) is a synthetic terpenoid with choleretic effects that have been used in the symptomatic treatment of itching due to intrahepatic cholestasis of pregnancy. Epomediol is able to restore a normal hepatocyte bile acid uptake when given in vivo simultaneously with ethinyloestradiol but does not influence bile acid transport in cultured hepatocyte

Dimethylaminopropionylphenothiazine was first synthesized in 1951 by Swedish pharmaceutical company Astra AG. It demonstrated anesthetic and antispasmodic activities in vivo.

Aluminium acetoacetate is an aluminum containing antacid for acid related disorders

Magnesium levulinate, the magnesium salt of levulinic acid, is a mineral supplement. It has been shown that in some cases of congenital non-spherocytic haemolytic anaemia (CNSHA) with pyruvate kinase deficiency, the primary defect may be related to diminished magnesium-stimulated ATPase activity, followed by elevation of the erythrocyte ATP level. In CNSHA patients the administration of Magnesium levulinate was followed by an increase in PK activity almost to the control value. This may indicate that magnesium ions stimulate deficient ATPase activity and lead to diminution of ATP as a negative effector for other regulatory enzymes.

Nicotinyl methylamide (N-methylnicotinamide) is an experimental drug with no approved indication or marketed formulation. Nicotinyl methylamide is a metabolite of niacin (or nicotinamide) and is commonly found in human urine. However low levels of urinary excretion of N-methylnicotinamide indicates niacin deficiency. In patients with liver cirrhosis nicotinamide methylation is increased leading to a rise in urinary N-methylnicotinamide. The hyperfunction of this methylating pathway might play a protective role against the toxic effect of intracellular accumulation of nicotinamide deriving from the catabolic state of cirrhosis. N-methylnicotinamide is known to inhibit choline transport and reduce choline clearance out of the brain. N-methylnicotinamide has been found to be a microbial metabolite. N-methylnicotinamide inhibits arterial thrombosis in hypertensive rats. N-methylnicotinamide via production/release of prostacyclin inhibits arterial thrombosis development. The antithrombotic effect of N-methylnicotinamide is accompanied by platelet inhibition and enhanced fibrinolysis, due to the decrease production of plasminogen activator inhibitor -1.

Evogliptin (Suganon) is an orally bioavailable, selective dipeptidyl peptidase-4 (DPP-4; CD26 antigen) inhibitor being developed by Dong-A ST for the treatment of type 2 diabetes mellitus. Evogliptin was approved in South Korea on 2 October 2015 for blood glucose lowering in patients with type 2 diabetes mellitus inadequately controlled by diet and exercise alone or by metformin plus diet and exercise. In July 2015, Dong-A ST signed a licensing out agreement for evogliptin with Geropharm for Russia, Ukraine and Kazakhstan markets. In April 2015, Dong-A ST signed a licensing agreement with Eurofarma Laboratorios of Brazil for 17 Latin America countries including Mexico. Evogliptin is a potent DPP-4 inhibitor with a 50 % inhibitory concentration (IC50) against soluble human DPP-4 of 0.98 nmol/L and an IC50 of 1.26 nmol/L against membrane-bound human DPP-4. It displayed 6000-fold higher potency for human DPP-4 than for human DPP-8 and DPP-9, and 20,000-fold greater potency for DPP-4 than for DPP-1, DPP-2 and other closely-related enzymes. Evogliptin is effective in improving glycosylated hemoglobin (HbA1c) and fasting plasma glucose without inducing hypoglycemia events, which potentially can improve adherence and prevent complications. It is also found that evogliptin has benefits on insulin secretory and β-cell functions. Based on the current clinical data, evogliptin has a neutral effect on body weight. These attributes contribute to the clinical practice in monotherapy or in combination with other antidiabetic agents. Evogliptin was generally well tolerated in clinical trials.

Pinaverium, known under the brand name DICETEL, is a spasmolytic agent used for functional gastrointestinal disorders. It is a quaternary ammonium compound that acts as an atypical calcium antagonist to restore normal bowel function. It is shown to relieve GI spasm and pain, transit disturbances and other symptoms related to motility disorders and may be considered as effective first-lline therapy for patients with irritable bowel syndrome (IBS). Pinaverium is also used to help relieve symptoms caused by certain disorders of the gallbladder associated with secretion of bile. Pinaverium bromide is the common ingredient in formulations, mostly as oral tablets. Although it is not a currently approved drug by the FDA, pinaverium is available in over 60 countries including Canada. DICETEL® (pinaverium bromide) is a calcium antagonist which inhibits the calcium influx by blocking the voltage-dependent calcium channel at the smooth muscle cell level. It possesses a high degree of selectivity for the intestinal smooth muscle.

METHYLMETHIONINE (S-Methionine methyl sulfonium, SMMS) chloride is a derivative of methionine metabolism in some plants. Methylmethionine has therapeutic effects on gastrointestinal ulceration potentially via its ability to promote dermal fibroblast migration and growth. The natural derivative Methylmethionine is biosynthesized from L-methionine which is first converted to S-adenosylmethionine. The subsequent conversion, involving replacement of the adenosyl group by a methyl group is catalyzed by the enzyme methionine S-methyltransferase. Methylmethionine is particularly abundant in plants, being more abundant than methionine. S-Methylmethionine is sometimes referred to as vitamin U, but it is not considered a true vitamin. The term was coined in 1950 by Garnett Cheney for uncharacterized anti-ulcerogenic factors in raw cabbage juice that may help speed healing of peptic ulcers.