Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would withdraw pending applications for marketing approval after reports of hepatotoxicity (liver damage) during trials, and discontinue its distribution in countries where the drug had been approved (Germany, Portugal, Sweden, Finland, Norway, Iceland, Austria, Denmark, France, Switzerland, Argentina and Brazil). Ximelagatran is a prodrug that is rapidly converted after oral administration to the active compound melagatran. Melagatran is able to inhibit thrombin activity directly and quickly. The melagatran molecule binds to the arginine side pocket of thrombin, inactivating the thrombin. Following oral administration of ximelagatran, oral bioavailability (measured as melagatran) is 18% to 25%. Peak melagatran levels after a ximelagatran dose of 48 mg twice daily are achieved within approximately 2 hours. Ximelagatran is rapidly and extensively converted to melagatran in the liver and other tissues. This conversion is achieved by ester hydrolysis and reduction via two intermediate metabolites, hydroxymelagatran, and ethylmelagatran. The predominant compound in plasma is the active drug, melagatran. The elimination half-life of melagatran after an oral dose of ximelagatran is 2.5 to 4.3 hours.

Incadronate (Disodium Cycloheptylaminomethylene diphosphate) is used to treat malignancy-associated hypercalcemia (MAH) in Japan. Experiments on rodents have revealed that this drug could be an effective agent for the treatment of various arthritic conditions, including human rheumatoid arthritis. In addition was shown, that incadronate induced growth inhibition and apoptotic death of pancreatic cancer cells. Incadronate also inhibited migration presumably by preventing the activation of Rho by lysophosphatidic acid. Thus, this drug can be of value in regimens for the treatment of pancreatic cancer.

Dimetacrine is a tricyclic antidepressant. It has been used in the treatment of depressive states. Dimetacrine usage associates with risk of cardiovascular side effects.

Mozavaptan hydrochloride was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on July 26, 2006. It was developed and marketed as Physuline® by Otsuka in Japan. Mozavaptan hydrochloride is a vasopressin receptor antagonist. It is indicated for the treatment of hyponatremia due to excessive fluid retention when restriction of fluid intake is ineffective. Physuline® is available as film-coated tablet for oral use, containing 30 mg of Mozavaptan hydrochloride. The recommended dose is one tablet (30 mg) once daily after a meal.

Sucrosofate (sucrose octasulfate) is a class of organic compounds known as disaccharide sulfates carrying one or more sulfate group on a sugar unit. It is used to encapsulate some anticancer drugs in liposomes allowing for highly active formulations against solid tumors and immunotargeting to cancer-overexpressing cell surface receptors. ONIVYDE (liposomal irinotecan) for intravenous use encapsulates an aqueous space containing irinotecan in a gelated or precipitated state as the sucrose octasulfate salt was initially approved by FDA in 1996 for treatment of pancreatic cancer. Sucrose octasulfate (SOS), a chemical analogue of heparin, has been demonstrated to activate fibroblast growth factors signalling pathways and SOS-mediated dimerization of FGF1 was observed. SOS can suppress thrombin generation in plasma that suggests a potential for oversulfated disaccharides in controlling heparin cofactor II -regulated thrombin generation.

Sucrosofate (sucrose octasulfate) is a class of organic compounds known as disaccharide sulfates carrying one or more sulfate group on a sugar unit. It is used to encapsulate some anticancer drugs in liposomes allowing for highly active formulations against solid tumors and immunotargeting to cancer-overexpressing cell surface receptors. ONIVYDE (liposomal irinotecan) for intravenous use encapsulates an aqueous space containing irinotecan in a gelated or precipitated state as the sucrose octasulfate salt was initially approved by FDA in 1996 for treatment of pancreatic cancer. Sucrose octasulfate (SOS), a chemical analogue of heparin, has been demonstrated to activate fibroblast growth factors signalling pathways and SOS-mediated dimerization of FGF1 was observed. SOS can suppress thrombin generation in plasma that suggests a potential for oversulfated disaccharides in controlling heparin cofactor II -regulated thrombin generation.

DODICIN (Tego-51), one of the amphoteric surfactants based on the dodecyl-di( aminoethyl)-glycine, has been considered as an effctive disinfectant having a broad specturn of antimicrobial activity. Tego-51 disinfectant was effective for the disinfection of commonly isolated bacteria and yeast from hospital. It may be recommended that Tego-51 should be used at concentration greater than 0.1% for the effective disinfection of skin, instruments and hospital floors.

Cadrofloxacin hydrochloride was studied for the treatment of bacterial infections. The compound was originally developed by UBE and Daiichi Sankyo. However, this study was discontinued. The compound currently was developed by Hengrui. Cadrofloxacin showed potent bactericidal activity against S. aureus, Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa.

Laninamivir ocatanoate is a prodrug of Laninamivir (R-125489), a new neuraminidase (NA) inhibitor, was discovered, and in this study, its NA inhibitory activities against various influenza viruses including oseltamivir-resistant viruses are reported. Laninamivir octanoate has been approved for use in Japanese clinics for the treatment and prevention of influenza in both adults and children. The inhaled laninamivir octanoate is converted into its active form, laninamivir, in the lungs where a high concentration persists for a long period of time.

Azapropazone is a non-steroidal anti-inflammatory drug. It is indicated for use in the treatment of rheumatoid arthritis, osteo-arthritis and gout. Gastro-intestinal disturbances, allergic skin rashes and photosensitivity, headache, vertigo, oedema and kidney impairment may occur. Gastro-intestinal bleeding and angioedema have been reported. Pre-treatment with this drug failed to modify plasma concentrations of phenobarbitone. Brain levels of imipramine or desmethyl imipramine were unaffected 60 minutes after oral administration of imipramine.