Pibutidine hydrochloride (IT-066), a novel histamine H2 receptor antagonist has powerful and long lasting antisecretory and antiulcer effects and is a useful antisecretory drug for treatment of peptic ulcer diseases.

Zanapezil (TAK-147) is a selective reversible acetylcholine (ACh) esterase inhibitor that was designed as a drug for Alzheimer's disease (AD) treatment. The development of the drug was discontinued due to a lack of a dose-dependent effect in the trials.

Suplatast is a novel immunomodulator that can adjust the imbalance in the Th1/Th2 immune response and shows clear clinical efficacy against bronchial asthma (BA). Suplatast tosilate helps to suppress the production of IgE, to block the production of cytokines and to suppress allergy-related eosinophils. Clinical studies on the efficacy of Suplatast were carried out in Japan. Suplatast showed adequate efficacy for the treatment of BA, allergic rhinitis and atopic dermatitis. Suplatast is now available for the management of BA as a controller of the Th2-dependent allergic inflammation. Suplatast tosilate is not approved in the United States, but is available in Japan as Tosilart® and IPD Capsules®. IPD-1151T (suplatast tosilate) was originated by Taiho and is being developed for the treatment of interstitial cystitis and chronic non-bacterial prostatitis as additional indications. IPD-1151T treatment for 1 year resulted in a significantly increased bladder capacity and decreased symptoms, such as urinary urgency, frequency and lower abdominal pain, in patients with nonulcerative interstitial cystitis.

Fasoracetam is a cognition enhancer that interacts with GABA(B) receptors, stimulates neuronal ACh receptors and modulates mGlu receptors. The drug is being tested in phase III/II of clinical trials for the treatment of Attention Deficit Disorder With Hyperactivity in people with genetic disorders impacting mGlu receptors and never been approved by FDA. Fasoracetam is also being marketed in the form of capsules for research purposes aimed at investigation of cognition and memory disorders.

Cefmatilen (codenamed S-1090) is an orally-active cephalosporin antibiotic, that shows high activity against a variety of Gram-positive and Gram-negative bacteria, including Streptococcus pyogenes and Neisseria gonorrhoeae.

Fadrozole (CGS 16949A) is a tetrahydroimidazole-pyridine derivative is a non-steroidal inhibitor of aromatase. In the third phase of clinical trials it was shown, that this drug has good therapeutic effect as a second-line treatment in postmenopausal women with metastatic breast cancer.

Olamufloxacin (HSR-903) is an oral fluoroquinolone antimicrobial agent which has been reported to have a potent activity against respiratory pathogens, such as Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Klebsiella pneumoniae, Staphylococcus aureus, Chlamydia spp. and Legionella spp., as well. Olamufloxacin inhibits DNA gyrase from the susceptible and resistant bacterial strains. It has been shown that olamufloxacin possesses a more potent antibacterial activity against potential respiratory pathogens compared with other quinolone derivatives. An oral formulation of olamufloxacin was undergoing phase III for Bacterial infections in Japan (Discontinued).

Exatecan (DX-8951f), a new hexacyclic camptothecin analogue, is a second-generation topoisomerase inhibitor that prevents rapidly dividing cells from replicating by interrupting DNA transcription, ultimately leading to cell death. Preclinical studies showed exatecan to have broad-spectrum antitumor efficacy. Exatecan is in phase III clinical trials for the treatment of pancreas cancer. However, there is no recent report of this research. The compound was co-developed by Daiichi Pharmaceutical (now Daiichi Sankyo) and Yakult Honsha.

Besipirdine is a potential novel first-in-class oral treatment for over active bladder currently in Phase II development, with a mechanism of action clearly different from that of antimuscarinics. It was under evaluation by Aventis up to phase III for Alzheimer’s disease, involving the administration of the compound to over 1500 patients. However, this research has been discontinued. Besipirdine antagonizes alpha-2 and alpha-1 adrenoceptors and inhibits both norepinephrine and serotonin uptake. The most common adverse events were asymptomatic postural hypotension and asymptomatic bradycardia.

Tezosentan (Veletri; Ro 61–0612) is a dual endothelin receptor antagonist that has been shown to improve cardiac output, decrease pulmonary capillary wedge pressure, and reduce pulmonary and systemic vascular resistance in initial clinical studies in acutely decompensated heart failure. Tezosentan is a water-soluble ET-1 receptor antagonist with high affinity to both ETA and ETB receptors but greater potency for the ETA receptor subtype. Clinical studies demonstrated mixed results for Tezosentan regarding its efficacy and tolerability in the management of decompensated heart failure. The side effects of Tezosentan include a headache, nausea, and hypotension.