Fidarestat (SNK-860) is an aldose reductase inhibitor codeveloped by Sanwa Kagaku, NK Curex, and Sankyo for the treatment of distal symmetric polyneuropathy (DSP). In a Phase III trial, 279 patients with DSP were randomized to receive fidarestat (1 mg daily) or placebo for 52 weeks. Evaluation of efficacy was based on changes in clinical symptoms (numbness, pain, rigidity, alterations in temperature perception, paresthesia, hypesthesia, and weakness) as well as changes in electrophysiological measurements such as F-wave NCV. Five of six electrophysiological measures assessing function in motor nerves showed statistically significant improvement from baseline within the treatment group; a comparison of the placebo and treatment groups on these measures, however, showed the statistical difference on only two of the six measures. Two electrophysiological measures of sensory function failed to show a statistically significant difference from baseline in the fidarestat group. Statistically significant improvements over placebo were noted on several measures of subjective symptoms (e.g., numbness of upper extremities, decreased tactile sensitivity in lower extremities, paresthesia in the sole), with a greater divergence between the two groups associated with the duration of treatment. The incidence of adverse events was 5.8% in the fidarestat group and 5% in the placebo group and no serious adverse events were noted.

Moxaverine, a derivative of papaverine, is a phosphodiesterase inhibitor. Moxaverine has been studied in phase III of a clinical trial for the treatment of ocular blood flow in patients with age- related macular degeneration and primary open angle glaucoma. In addition, it has been studied in phase II of the clinical trial for the treatment of ischemia. This compound is prohibited by FEI (International Federation of equine).

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.

Cynarine (Cynarin) is the most noteworthy active ingredient of the artichoke, and is considered a medicinal foodstuff due to its beneficial effect on the organism, derived from its condition as a stimulant of bile secretion (choleretic effect). Cynarine is present in artichoke leaves and has a beneficial effect on the control of gallstones, helps control cholesterol levels and improves gallbladder function. Chlorogenic acid and cynarin have been shown to have activity against oxidative stress in human leukocytes, whereas cynarin has also been shown to have hypocholesterolemic, hepatoprotective, and, more recently, antihuman immunodeficiency virus-1 (anti-HIV-1; 44) activities. Cynarin had marked antioxidant, anticholinergic, reducing ability, radical-scavenging, and metal-binding activities.

Oteracil is an adjunct to antineoplastic therapy, used in combination with Gimeracil and Tegafur. Gimeracil/oteracil/tegafur combination is approved for the gastric cancer treatment. Oteracil is an orotate phosphoribosyltransferase (OPRT) inhibitor that decreases the activity of 5-fluorocil (tegafur is a prodrug of 5-fluorocil) in normal gastrointestinal mucosa.

Phoxim (Diethyl-O-(alpha-cyanobenzylideneamino)-thiophosphate) is an organophosphorus insecticide used in veterinary medicine for the control of mites, lice and other ectoparasites in cattle, pigs, sheep, and goats. Phoxim is also used for plant protection, in tea production. The insecticidal activity of phoxim is mediated through inhibition of cholinesterase. Phoxim is an insecticide with selective properties: it is toxic to insects but virtually non-toxic to mammals. Although differences in sensitivity to cholinesterase inhibition contribute to this selectivity, metabolism plays a more important role. In both insects and mammals, phoxim is oxidatively desulfurated to the oxo-analog, PO-phoxim, which is a more potent inhibitor of cholinesterases than phoxim itself. In mammals, however, PO-phoxim is an extremely short-lived intermediate and, together with phoxim, is rapidly hydrolyzed to non-toxic products.

Cridanimod (Virexxa) is a small-molecule immunomodulator and interferon inducer, which, in preliminary studies, has been shown to increase progesterone receptor expression in endometrial tissue. Restoration of progesterone receptor expression may re-sensitize endometrial tumor tissue to progestin therapy in previously unresponsive tumors. Cridanimod was originally developed by Polysan and Pharmsynthez and licensed to Xenetic Biosciences. Virexxa is currently being studied in an ongoing Phase 2 multi-national study in conjunction with progestin therapy for the treatment of endometrial cancer in women with the recurrent or persistent disease who have failed progestin monotherapy.

Choline alfoscerate (alpha-Glycerylphosphorylcholine or Alpha-GPC) is a nootropic choline-containing phospholipid. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. In Europe alpha-GPC is a prescription medication for the treatment of Alzheimer's disease. It is available in two forms; one is taken by mouth, and the other is given as a shot. In the United States alpha-GPC is only available as a dietary supplement, mostly in products promoted to improve memory. Other uses for alpha-GPC include treatment of various kinds of dementia, stroke, and "mini-stroke" (transient ischemic attack, TIA). Alpha-GPC is also used for improving memory, thinking skills, and learning.

Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 / dopamine D2 blocking activity. It is not available in the US but marketed in other countries for prophylaxis of a migraine, occlusive peripheral vascular disease, the vertigo of central and peripheral origin, motion sickness and as an adjuvant in the therapy of epilepsy. The drug is also investigated for the treatment of schizophrenia.

Lidamidine, also known as WHR-1142A and Lidaral, is an alpha2-adrenergic receptor agonist that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. Lidamidine hydrochloride is used to treat diarrhoea and other gastrointestinal disorders. Lidamidine’s intestinal antisecretory effects are mediated through the activation of peripheral alpha-2 adrenoceptors. Lidamidine crosses the blood brain barrier poorly and is therefore devoid of the centrally mediated alpha-2 effects that have limited the use of other alpha-2 adrenoceptor agonists in the intestinal tract.