Imidapril (Tanatril), through its active metabolite imidaprilat, acts as an ACE inhibitor to suppress the conversion of angiotensin I to angiotensin II and thereby reduce total peripheral resistance and systemic blood pressure (BP). In clinical trials, oral imidapril was an effective antihypertensive agent in the treatment of mild to moderate essential hypertension. Some evidence suggests that imidapril also improves exercise capacity in patients with chronic heart failure (CHF) and reduces urinary albumin excretion rate in patients with type 1 diabetes mellitus. Imidapril was well tolerated, with a lower incidence of dry cough than enalapril or benazepril, and is a first choice ACE inhibitor for the treatment of mild to moderate essential hypertension.

Camphoric acid is a product of oxidation of camphor, naturally occurring in rosemary. In the early twentieth century, camphoric acid was used in the night-sweats of phthisis and was also employed in solution as a local antiseptic to the nose, throat, and bladder. Camphoric acid was found to induce the expression of glutamate receptors NMDAR1, GluR3/4, and mGluR8.

Tebipenem pivoxil is an oral carbapenem prodrug that was originated by Wyeth (now Pfizer). It was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Apr 22, 2009. It was developed and marketed as Orapenem® by Meiji Seika in Japan. Tebipenem pivoxil is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics. Carbapenems are a class of beta-lactam antibiotics, which act by inhibiting the synthesis of the peptidoglycan layer of bacterial cell walls. It is used to treat otorhinolaryngological infection, otitis media and bacterial pneumonia. Orapenem® is available as granules for oral use, containing 100 mg Tebipenem pivoxil/g granules. According to the weight of children, 4 mg/kg, and twice a day after dinner.

Indobufen inhibits platelet aggregation by reversibly inhibiting the platelet cyclooxygenase enzyme thereby suppressing thromboxane synthesis. Indobufen under brand name ibustrin is used in Italy for the following conditions: cerebrovascular insufficiency, atherosclerosis of peripheral and cerebral vessels, thrombophlebitis, deep vein thrombosis, and diabetes mellitus. In addition, this drug has been investigated in the phase II clinical trial for the prevention of thromboembolic events in patients with nonrheumatic atrial fibrillation. After oral administration, it is quickly and completely absorbed.

Cinnarizine is a piperazine derivative with antihistaminic, antiserotonergic, antidopaminergic, and calcium channel-blocking activities. It inhibits calcium translocation across the vestibular sensory cells in the ampullae and maintains endolymph flow by preventing constriction of the stria vascularis. It is currently used for the treatment of nausea, vomiting, and vertigo caused by Meniere’s disease and other vestibular disorders. Cinnarizine is also used for prevention and treatment of motion sickness. Chronic use of cinnarizine may induce extrapyramidal symptoms.

Sitafloxacin hydrate (DU-6859a, Gracevit), a new-generation, broad-spectrum oral fluoroquinolone that is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections. This is a new quinolone oral antibacterial to inhibit DNA replication of bacteria at the time of infection, and shows antibacterial action. Sitafloxacin is active against methicillin-resistant staphylococci, Streptococcus pneumoniae and other streptococci with reduced susceptibility to levofloxacin and other quinolones and enterococci. Sitafloxacin has also demonstrated activity against clinical isolates of Klebsiella pneumoniae (including about 67% of strains producing extended-spectrum, beta-lactamases and resistant to ciprofloxacin), Enterobacter cloacae, Pseudomonas aeruginosa with some activity against quinolone-resistant strains and Acinetobacter baumannii. The in vitro activity against anaerobes is comparable to imipenem or metronidazole. Sitafloxacin showed dual inhibitory activity against both enzymes: Streptococcus pneumoniae DNA gyrase and topoisomerase IV.

Pelubiprofen, 2-[4-(Oxocyclohexylidene methyl)phenyl]propionic acid, is one of the 2-arylpropionic acid class of non-steroidal anti-inflammatory drugs (NSAIDs). It has wide variety of indications proposed: osteoarthritis, rheumatoid arthritis, musculoskeletal pain, post-operative trauma, backache, neck-shoulder syndrome and dental pain. Pelubiprofen is a prodrug of 2-arylpropionic acid with relatively selective effects on cyclooxygenase-2 activity. Antiinflammatory properties of pelubiprofen are due to its ability to both decrease prostaglandin synthesis by inhibiting the activities of cyclooxygenases (COXs) and IkB kinase-b (IKK-b). Pelubiprofen was found to have an anti-edema effect in the carrageenan-induced paw edema model in rats, one of the well-established acute inflammatory models in vivo. Pelubiprofen was well tolerated in single doses up to 120mg and at a dosage of 180 mg/day. No drug accumulation was evident, suggesting that it may be useful for long term treatment.

Isocarbacyclin methylester (clinprost) (isocarbacyclin methylester; methyl 5-{(1S,5S,6R,7R)-7-hydroxy-6-[(E)- (S)-3-hydroxy-1-octenyl] bicyclo[3.3.0]oct-2-en-3-yl} pentanoate) and its active metabolite, isocarbacyclin (TEI-7165), are chemically stable PGI2 analogues. TTC- 909 is a drug preparation of clinprost incorporated into lipid microspheres (LM). The hypothetical sequence of events for TTC-909 to exert pharmacological effects is as follows: the LM would deliver clinprost to most tissues including the blood and the brain, clinprost would be released gradually from the LM, and then the clinprost would be hydrolyzed to TEI-7165 by esterase action to exert pharmacological activity. Both clinprost and TEI-7165 inhibit platelet aggregation and platelet adhesion in vitro and suppress prostaglandin F2 (PGF2 )-induced contraction of isolated canine arteries. TTC-909 also has vasodilative and anti-platelet activity in vivo, similar to PGI2. TTC-909 was shown to inhibit cerebral infarction, maybe by improving cerebral blood flow and by protecting against neuronal damage.

Isoniazid glucuronate is a less toxic derivative the antibacterial drug isoniazid. Isoniazid is recommended for all forms of tuberculosis in which organisms are susceptible. Isoniazid itself is a prodrug and must be activated by bacterial catalase. Isoniazid inhibits InhA, the enoyl reductase from Mycobacterium tuberculosis, by forming a covalent adduct with the NAD cofactor.

Erdosteine is an antioxidant compound developed by Edmond Pharma and approved in Europe for the treatment of chronic bronchitis and COPD. Erdosteine has two thiol groups and is believed to act as a free radicals scavenger (through the formation of the active metabolite I, N-thiodiglycolylhomocysteine). Also the drug effect may be due to the inhibition of the activity of elastase enzyme and its interaction with mucosa. The drug got Orphan Drug designation by FDA for the treatment of bronchiectasis.