Daiichi Sankyo developed an inhibitor of acyl-coenzyme A:cholesterol acyltransferases (ACAT1 and ACAT2), pactimibe (also known as CS 505). Pactimibe has been used in trials phase II for reducing the progression of coronary artery disease and in patients with atherosclerosis. However, on October 26, 2005, the company made the decision to discontinue all ongoing clinical studies of pactimibe, because of the secondary endpoints that showed a lower effect of the drug on atherosclerosis than the standard of care alone and no beneficial effect on the frequency of cardiovascular events.

Nafagrel [DP 1904, SR 96325] is a thromboxane A2 synthetase inhibitor that was undergoing clinical trials with Daiichi Seiyaku, now Daiichi Pharmaceutical, for the diabetic angiopathies, lupus nephritis and Raynaud's disease in Japan. However the development of Nafagrel has been discontinued.

Ispinesib (SB-715992) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP). KSP, also known as HsEg5, is a kinesin that plays an essential role in the formation of a bipolar mitotic spindle and is required for cell cycle progression through mitosis. Ispinesib is the highly specific small-molecule inhibitor of KSP tested for the treatment of human disease. It causes mitotic arrest and growth inhibition in several human tumor cell lines and is currently being tested in multiple phase II clinical trials for treatment of the breast cancer and renal cell cancer.

Tuvatidine (HUK 978) is a potent H2-antagonist. HUK 978 was shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors. In both the guinea-pig gastric mucosa preparation and the rat perfused stomach model, HUK 978 was a powerful inhibitor of acid secretion. HUK 978 is a highly specific H2-antagonist and inhibits acid secretion for longer periods than other competitive compounds.

Tamitinol (also known as EMD 21657), a neurotropic drug that was developed as a cognition enhancer for the treatment of diffuse cerebral disease and organic brain syndrome. Tamitinol participated in clinical trials where the therapeutic effects of the drug were shown to be statistically significant compared to placebo in the global response. However, the treatment was interrupted because of side effects (increased aggressiveness, rash) in 2 cases.

Suloxifen is a aminoalkyl S,S-diphenylsulfoximine derivative patented by Warner-Lambert Pharmaceutical Co. as broncholytic and antispasmodic agent.

Pamapimod (R-1503, Ro4402257) is a potent and selective inhibitor of p38 mitogen-activated protein kinase alpha. The preclinical data support the conclusion that pamapimod has the ability to inhibit the signs and symptoms of rheumatoid arthritis and other autoimmune diseases. Pamapimod was being developed for use in the treatment of rheumatoid arthritis. There is no clear-cut evidence that pamapimod alone or in the presence of methotrexate is efficacious in subjects with rheumatoid arthritis but it does cause adverse effects. It is unlikely that pamapimod will be useful in the treatment of rheumatoid arthritis.

IPSALAZIDE is a sulfasalazine analog designed as a colon-specific delivery system for the treatment of inflammatory bowel disease by releasing 5-aminosalicylic acid in the gastrointestinal tract.

FLUBANILATE is a CNS stimulant.