Broxyquinoline is an anti-infective agent. It exerts activity against fungi and protozoa. Broxyquinoline (Intestopan) has been used in the treatment of diarrhoeas of different aetiology. Broxyquinoline is able to promote neovascularization.

Epalrestat is an aldose reductase inhibitor that is approved in Japan for the improvement of subjective neuropathy symptoms, abnormality of vibration sense, and abnormal changes in heart beat associated with diabetic peripheral neuropathy.

Enocitabine is an anti-cancer nucleoside that was developed for the treatment of acute myeloid leukemia. Although the exact mechanism of its action is unknow, Enocitabine effectively inhibits tumor cell growht in vitro and the inhibition is supposed to be related to its metabolism to Ara-C, an inhibitor of DNA polymerase. The drug was approved in Japan and Korea and was marketed under the name Sunrabin, however, its current marketing status is unknown and is assumed to be discontinued.

Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.

Buterizine was developed by Janssen Pharmaceutical as a peripheral vasodilator

Milacainide (Ro 22-9194) is structurally related to lidocaine and has a pyridine ring in the side chain. Ro 22-9194 is a new Class I antiarrhythmic agent with a TXA, synthase inhibitory activity. In anesthetized, open-chest dogs Ro 22-9194 transiently decreased arterial blood pressure and affected AV conduction more selectively, with a prolongation of the HV interval, than sinoatrial nodal pacemaker activity. In isolated, blood-perfused atria of dogs, Ro 22-9 194 decreased myocardial contractility more than sinoatrial nodal pacemaker activity. Studies in guinea pig papillary muscles and single ventricular myocytes showed that Ro 22-9194 inhibits sodium channels in a use- and voltage-dependent manner, and belongs to the group comprising intermediate kinetic drugs and activated channel blockers. Epinephrine-, digitalis-, two-stage coronary ligation-, and 3-hr coronary ligation-reperfusion-induced ventricular arrhythmias, or aconitine-induced atrial arrhythmias, in dogs were potently suppressed by Ro 22-9194 administered orally or intravenously. In myocardial ischemia and reperfusion-induced arrhythmias of dogs, Ro 22-9194 had an antifibrillatory effect and prevented an increase in venous levels of TXB, released from the ischemic myocardium.

Isoconazole is structurally related to miconazole and econazole and was synthesized by Janssen Pharmaceutica. The compound has been marketed in several countries, but not in the United States. It has broad-spectrum activity in vitro against dermatophytes, pathogenic yeasts, pathogenic filamentous fungi, gram-positive bacteria, and trichomonads . The mode of action appears to include rapid reduction in ATP concentrations caused by damage to the fungal cell membrane. Isoconazole interacted with the cell wall and caused convolutions and wrinkles. Isoconazole also inhibited the enzyme-catalyzed release of spheroplasts from young yeast cells. A recent study has demonstrated that application of the free base of isoconazole in combination with a volatile/nonvolatile vehicle, e.g., ethanol/propylene glycol, can increase drug bioavailability in the skin. This observation may lead to newer formulations of isoconazole and broaden its use for topical (e.g., spray) treatment of yeast and dermatophytic infections. Dermatophytic Isoconazole has been developed and marketed primarily as a once-a-day, topical anti-Candida agent for the treatment of vaginal candidiasis. Studies evaluating isoconazole have demonstrated that 80 to 90% of patients with vaginal candidiasis who were treated once a day with the drug remained clinically and mycologically cured. Following insertion of two 300-mg tablets, concentrations of isoconazole in the vagina remained above minimum inhibitory and minimum fungicidal levels for at least 72 h. Isoconazole has been developed and marketed primarily as a once-a-day, topical anti-Candida agent for the treatment of vaginal candidiasis. In clinical studies, very little of the drug entered the blood after a single vaginal application of a 600-mg dose; the same dose did not adversely affect intestinal flora by inducing a proliferation of yeast like species following prolonged administration. Studies evaluating demonstrated that 80 90% of patients.

Thiazinamium is an anti-cholinergic phenothiazine deriva¬tive, which also has antihistaminic properties. Intramuscular injection of Thiazinamium induces considerable bronchodilatation, but inconsistent results have been obtained after oral administration. The bioavailability of oral Thiazinamium is only 2-3% of that occurring after intramuscular injection. Intrarectal Thiazinamium is slightly better absorbed (3-9%). The elimination half-life of the parenteral drug is short, being about 20 minutes in most patients. Thiazinamium has been available for the treatment of asthma since the early 1960s but currently withdrawn in most countries. Compared with inhaled ipratropium bromide, intramuscular Thiazinamium and intramuscular atropine were associated with 'extremely frequent side-effects’. Notable tachycardia occurred shortly after intramuscular injection of Thiazinamium in two trials. Dry mouth was reported as ‘frequent’ with oral Thiazinamium, and micturition problems of moderate severity affected 13% of patients.

Febarbamate is a derivative of barbituric acid and carbamate, used for the treatment of generalized anxiety and alcohol withdrawal syndrome. The drug was marketed in Europe in the 1980s as a single agent or in combination with difebarbamate and phenobarbital, but it was later withdrawn from the market because of the potential risk of liver damage.

LB80380 is a prodrug of besifovir, a novel antiviral agent for the treatment of chronic hepatitis B.