Fabesetron is a dual 5HT3 and 5HT4 receptors antagonist that was developed in Japan for the treatment of chemotherapy-induced emesis and gastrointestinal disorders. The development of the drug was terminated in phase II.

Deptropine citrate is a well-known H1-histamine receptor antagonist and muscarinic receptor antagonist. It is prescribed frequently for treatment of asthma, although there has been a sharp decrease in prescriptions since 1994. Deptropine is gradually being replaced by inhaled beta 2 adrenergic agonists and glucocorticosteroids as the preferred clinical prescription. Recently deptropine has garnered interest as a potential treatment for breast cancer. In vitro studies have shown deptropine citrate has inhibitory effects on cell viability and mammosphere formation in Breast Cancer Stem Cells (BCSCs). However, it does not seem to inhibit the self-renewal capacity of the breast cancer cell line MDA-MB-231 when it is enriched with Cancer Stem Cells.

Oral dehydroemetine dihydrochloride (+/-) (Mebadin) was found useful both as a tissue and contact amoebicide. It is much less toxic and more active than emetine and can be given in larger doses and for longer periods with safety. Owing to the quick excretion, repeat courses can be given at short intervals, as necessary, without danger. No serious side effects were noted particularly with the oral form and it was far better tolerated by children, who received relatively higher dosage than most adults. The only contra-indication is for patients with manifest decompensation of vital organs, or fevers. Mebadin injection and Mebadin tablets are discontinued products.

Minodronic acid (RECALBON®, Bonoteo®), a third-generation bisphosphonate, was approved in Japan for the oral treatment of osteoporosis. This drug increases the bone mineral density and the strength by inhibiting osteoclastic bone resorption. Nitrogen-containing bisphosphonates, such as minodronic acid (RECALBON®, Bonoteo®) induce osteoclast apoptosis by inhibiting farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Inhibition of FPPS in osteoclasts prevents the biosynthesis of isoprenoid lipids that are required for the prenylation of small GTPase signaling proteins necessary for osteoclast function. Similarly, nitrogen-containing bisphosphonates have been shown to inhibit farnesyl pyrophosphate/geranyl pyrophosphate synthase activity.

Fadrozole (CGS 16949A) is a tetrahydroimidazole-pyridine derivative is a non-steroidal inhibitor of aromatase. In the third phase of clinical trials it was shown, that this drug has good therapeutic effect as a second-line treatment in postmenopausal women with metastatic breast cancer.

Dexfenfluramine, also marketed under the name Redux, is a serotoninergic anorectic drug. Dexfenfluramine, the dextrorotatory isomer of fenfluramine, is indicated for use in the management of obesity in patients with a body mass index of > or = 30 kg/m2, or > or = 27 kg/m2 in the presence of other risk factors. Unlike fenfluramine, dexfenfluramine is a pure serotonin agonist. Dexfenfluramine increases serotonergic activity by stimulating serotonin (5-hydroxytryptamine; 5-HT) release into brain synapses, inhibiting its reuptake into presynaptic neurons and by directly stimulating postsynaptic serotonin receptors. Dexfenfluramine reduces blood pressure, percent glycosylated hemoglobin, and concentrations of blood glucose and blood lipids, but these benefits may be indirect. Dexfenfluramine may also be of some value in controlling eating habits in diabetic patients, preventing weight gain after smoking cessation, and treating bulimia, seasonal affective disorder, neuroleptic-induced obesity, and premenstrual syndrome. Dexfenfluramine's most frequent adverse effects are insomnia, diarrhea, and headache; it has also been associated with primary pulmonary hypertension. The drug should not be combined with other serotonergic agonists because of the risk of serotonin syndrome. The recommended dosage is 15 mg twice daily. Dexfenfluramine is effective in the treatment of obesity in selected patients. Because its efficacy is lost after six months of continuous treatment, it should be viewed primarily as an adjunct to diet and exercise. Dexfenfluramine was approved by the FDA in 1996 and has been widely used for the treatment of obesity. However, Dexfenfluramine was removed from the U.S. market in 1997 following reports of valvular heart disease and pulmonary hypertension.

Metralindole (Inkazan) is a reversible inhibitor of monoamine oxidase A (RIMA) which was used in Russia as an antidepressant. Inkasan (3-methyl-8-methoxy-3H, 1,2,5,6- tetrahydropyrazine /1.2.3-ab/-beta-carboline hydrochloride) has pharmacological properties characteristic of antidepressants. The clinical antidepressant effect of inkasan is combined with stimulating action. The drug is primarily indicated for patients in whom adynamic (anergic) disturbances are predominant in the clinical picture of depression.

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.

Mosapramine (Cremin) is used to treat chronic schizophrenia in Japan. It is a potent dopamine antagonist with high affinity to the dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT2 receptors

Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Due to its hypnotic activity the drug is used to treat short-term sleep disordes.