Ipriflavone (chemical structure: 7-isopropoxyisoflavone), derived from the soy isoflavone, daidzein, holds great promise for osteoporosis prevention and treatment. Ipriflavone (IP) was discovered in the 1930s but has only recently begun to be embraced by the medical community in this country. Over 150 studies on safety and effectiveness, both animal and human, have been conducted in Italy, Hungary, and Japan. As of 1997, 2,769 patients had been treated a total of 3,132 patient years. Preliminary studies have pointed to its effectiveness in the treatment of other conditions involving bone pathology, including Paget’s disease, hyperparathyroidism, renal osteodystrophy, and tinnitus due to otosclerosis. Ipriflavone appears to have several mechanisms of action, all of which enhance bone density, making them seemingly superior to many of the other treatments available for osteoporosis prevention and treatment. IP also inhibits osteoclastic activity (motility and resorptive activity) by modulating intracellular free calcium. IP’s bone-forming mechanisms include stimulation of cell proliferation and maturation of osteoblasts by inhibiting calcium influx into osteoblasts and phosphoinositide hydrolysis. Despite similarities to estrogen, IP possesses no intrinsic estrogenic activity, but does potentiate estrogen. Importantly, IP does not change bone mineral composition or crystalline structure. A clinical trial reported in 2001 that it was not effective in prevention or treatment of osteoporosis.

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.

Anxiolytic drug, Gedocarnil [SH 530, ZK 113315], was undergoing phase I clinical trials with Schering AG in Germany as a potential nootropic agent. However it`s development for the treatment of cognition disorders was discontinued.

Pazufloxacin is a fused tricyclic quinolone derivative that has a broad spectrum of anti-bacterial activity. Pazufloxacin inhibits bot DNA gyrase and topoisomerase IV and has shown in vitro activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella, Enterobacter, Hafnia, Citrobacter, Proteus, Providencia, Serratia, Shigella, Salmonella, Aeromonas and Yersinia. The drug is used for the treatment of infectious diseases such as abdominal infections, genital infections, urinary tract infections, respiratory tract infections, etc.

Meticrane is a diuretic. Meticrane is used to treat essential hypertension.

4,5-diphenylimidazole is an antihistaminic and antiallergic drug. It was shown to be an inhibitor of phenytoin p-hydroxylation in rat hepatic microsomes, however 1-imidazoles had higher inhibitory potency observed at submicromolar concentrations.

Tobicillin (TBPC) is an ester derivative of penicillin G. It is a beta-Lactam antibiotic, peptidoglycan biosynthesis inhibitor. TBPC was shown to be the effective antibiotic for the treatment of enterococcicosis in yellowtail.

Bibenzonium is an antitussive agent. Bibenzonium bromide is a cough suppressant which is stated to have a central action.

Bevonium is a parasympatolytic antimuscarinic compound. It possesses spasmolytic properties. The use of the drug is discontinued.