Mizoribine (MZB) is an imidazole nucleoside and an immunosuppressive agent. Eupenicillium brefeldianum, an ascomycetes harvested from the soil of Hachijo Island, Tokyo, Japan, in 1971, produces mizoribine (MZB). MZB is a nucleoside of the imidazole class, and was found to have weak antimicrobial activity against Candida albicans, but it proved ineffective against experimental candidiasis. MZB has been approved in Japan for the treatment of lupus nephritis (1990), rheumatoid arthritis (1992), and primary nephritic syndrome (1995), and in these diseases, it has often been used in combination with corticosteroids and/or anti-inflammatory drugs. Mizoribine also has been used in renal transplantation, and in steroid-resistant nephrotic syndrome. After phosphorylation, misoribine-5’-monophosphate (MZB-P) inhibits guanosine monophosphate (GMP) synthesis by antagonistic blocking of inosine monophasphate dehydrogenase (IMPDH) and GMP-synthetase in the pathway from inosine [ 5’-] monophasphate (IMP) to GMP in the purine synthesis system. MZB-P appears to almost completely inhibits guanine nucleotide synthesis Suppressive effect of MZB on cell growth is attributable to MZB-P and not to MZB itself. Thus, MZB has less toxicity than azathioprine, another immunosuppressant used for some of the same diseases.

Eprozinol inhibits bronchoconstriction by an action on histamine H1 receptors and has been used in the treatment of asthma and bronchitis. No significant changes in cAMP and cGMP levels are observed in guinea pig trachea, with eprozinol or isoprenaline, at doses capable of inducing relaxation. Eprozinol is only a very weak phosphodiesterase inhibitor, at large concentrations. The anti-bronchoconstrictor activities of eprozinol and isoprenaline with regard to histamine are directly additive and show absolutely no interference with one another. Propranolol is without effect on in vivo anti-bronchoconstrictor activity of eprozinol on tracheal musculature. It is concluded, that the mechanisms brought into play by eprozinol to exert anti-bronchoconstrictor and bronchorelaxant activity, are completely independent of the adrenergic system. In a retrospective study of 199 cases of accidental or intentional acute poisoning with eprozinol, eprazinone and zipeprol, collected at the Poison Control Center were seven cases of seizures, all after ingestion of eight times the therapeutic dose. They resolved rapidly and without recurrence with symptomatic treatment.

Anaxirone is a triepoxide compound with cytotoxic activity. By analogy with bifunctional epoxides, anaxirone probably acts as an alkylating agent. Despite a wide spectrum of activity against experimental tumors in rats and mice, clinical investigation of anaxirone has shown that the drug was inactive for the treatment of advanced colorectal cancer, advanced soft tissue sarcoma, small cell lung cancer, ovarian cancer, and advanced malignant melanoma.

Anitrazafen is a topically effective anti-inflammatory agent. Аpplied topically to guinea-pigs, anitrazafen is a potent anti-inflammatory agent capable both of delaying the onset of and reversing, developing erythema induced by U.V. light. Anitrazafen, following oral administration to rats, showed only slight to moderate activity in the carrageenan-induced paw oedema and adjuvant-induced arthritis tests

Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine is an H1 receptor inverse agonist. Bilastine also exerts anti-inflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-α from human mast cells and granulocytes. Common side effects are headache and drowsiness.

Barmastine [bermastine, R 57959, ramastine], is an oral antihistamine agent which was being developed by Johnson & Johnson for use in asthma. Development was discontinued later.

Repirinast is an antiallergic drug developed and introduced into the market in Japan in 1987. It is a histamine release inhibitor. It has demonstrated effectiveness for treating bronchial asthma in humans.

Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis. Tranilast is used for the treatment of bronchial asthma, keloid and hypertrophic scar, and allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Oxatomide is a H1-histamine receptor antagonist developed for the treatment of broad spectrum of allergic and other hypersensitivity reactions. The drug is currently marketed in Japan, Taiwan, Italy, Portugal, Indonesia, Argentina, South Africa.

Inosine pranobex is an antiviral drug that is a combination of inosine and dimepranol acedoben (a salt of acetamidobenzoic acid and dimethylaminoisopropanol) in a ratio of 1 to 3. Inosine pranobex is used to treat mucocutaneous infections due to herpes simplex virus (type 1 and/or type II), genital warts as adjunctive therapy to podophyllin or carbon dioxide laser, and subacute sclerosing panencephalitis. The in vivo antiviral and activity of inosine pranobex is believed to result from an enhancement of host immune responses due to the drug. The drug does not by itself stimulate resting lymphocytes, but augments immunological processes by lymphocytes once they have been triggered by mitogens or viral antigens.