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.

IVARIMOD is a hepatoprotectant.

Nelezaprine is a skeletal muscle relaxant.

Doxpicomine is the hydrochloride salt of l-3[(dimethylamino)-(m-dioxan-5-yl)methyl]pyridine, a derivative of substituted 1,3 dioxanes. Its analgesic effect appears to be mediated centrally through opiate-like receptors. Preclinical animal studies revealed analgesic activity and duration of action of the same order as that of meperidine and codeine when administered subcutaneously and of codeine but of shorter duration when administered orally. The analgesic effects were reversed by naloxone. The drug did not reduce or antagonize the analgesic effect of morphine. Drowsiness is an expected response to effective analgesics. It was the foremost side effect observed but was of short duration and minimal intensity and did not interfere with the postoperative regimen of coughing, deep breathing, and early ambulation. Nausea and vomiting were not reported after doxpicomine.

Pipramadol is an analgesic agent. Pipramadol exhibits not only antinociceptive but also central and peripheral antiserotonin properties.

Tamethicillin is a basic ester pro-drug of methicillin (MET) which is converted in the body by non-specific esterases to MET. Tamethicillin was used as an antibacterial agent in the veterinary as a useful alternative for the treatment of mastitis in livestock, especially in mastitis due to beta-lactamase-producing Staphylococcus.

Oxibetaine was developed as a lipotropic agent. Information about the current use of this compound is not available.

Oxetacillin was developed as an antibacterial drug that has never been marketed.

Brefonalol also known as BDF 8186, a beta-adrenergic blocking agent with vasodilating properties. This drug was being developed for the treatment of hypertension, arrhythmias and angina pectoris. However, these studies were discontinued.

E7107 is a semisynthetic derivative of the natural product pladienolide B which was originally isolated from Streptomyces platensis. E7107 is the first compound a new class of anti-cancer agents targeting the spliceosome. Specifically E7107 interacts with the Splicing factor 3B subunit 1 (SF3b1) to block the normal splicing of oncogenes. Development of E7107 was suspended after Phase I clinical trials due to an unacceptable profile of adverse events.