Mafoprazine is a phenylpiperazine derivative exerting postsynaptic dopamine D2 receptor blocking activity and alpha-adrenergic activity (alpha 1 receptor blocking activity and alpha 2 receptor stimulating activity). In animal models, mafoprazine demonstrated antipsychotic, aggression-inhibiting and cataleptogenic actions.

Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. The effects of mafosfamide on various types of cancer cells were determined during preclinical investigations and clinical trials. Its development has been discontinued.

Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.

Mofarotene is an analog of retinoic acid patented by a Swiss multinational healthcare company Hoffmann-La Roche as neoplasm inhibitors and agent for treating dermatoses. Like other retinoic acid agents, mofarotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. Mofarotene has demonstrated considerable antitumor activity in a number of cancer cell lines. Mofarotene in combination with cisplatin and etoposide was studied in phase I clinical trials but further development was discontinued.

Aconiazide, the isonicotinylhydrazone of 2-formylphenoxyacetic acid, has been used in the treatment and prophylaxis of tuberculosis. Aconiazide is a pro-drug of isoniazid which was designed to be less toxic than the parent drug. Aconiazide is hydrolyzed in the body to isoniazid and 2-formylphenoxyacetic acid. 2-Formylphenoxyacetic acid has been shown to bind hydrazine and acetylhydrazine. This binding could explain the lower toxicity of aconiazide and also could provide a reason for postulating its lack of carcinogenicity.

Tulopafant [RP 59227] is a platelet-activating factor (PAF) antagonist which was being developed by Rhône-Poulenc Rorer as an antiasthmatic agent. Double-blind, placebo-controlled clinicacl trial showed that RP 59227 attenuated the release of NCA and ECA after antigen challenge, and reduced the effect of exogenously added PAF in inducing eosinophil chemotaxis but did not protect against the antigen-induced early or late phase response in asthmatics. RP 59227 has also been shown to effectively reduce myocardial infarct size and the incidence of ischemia and reperfusion-induced arrhythmias in barbital-anesthetized dogs. Development of Tulopafant for asthma treatment has been discontinued.

Embeconazole (CS 758 or R 120758) is a triazole antifungal agent. Embeconazole exerts potent antifungal activity both in vitro and in vivo. It was being developed for the treatment of mycoses.

Netoglitazone (also called MCC-555) is a hypoglycemic agent belonging to the thiazolidinedione group that exerts both peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist activity. It was developed by Mitsubishi-Tokyo (formerly Mitsubishi Chemical) as a potential treatment for type 2 diabetes due to the enhancement of insulin sensitivity. This drug was in clinical trial phase II but then was discontinued. In addition, was also investigated the behaviour of MCC-555 on colorectal cancer (CRC) cells and was revealed, that the drug had an effect on the early events of colon carcinogenesis and could be a potential preventive compound for CRC.