Tresperimus is a new stable immunosuppressive analog of 15-deoxyspergualin (DSG) obtained by organic chemical synthesis. It was initially developed as an antitumor agent. Tresperimus has been designed to be chemically stable in aqueous solution. Tresperimus controlled alloreactivity in a fully major histocompatibility complex (MHC) mismatched rat cardiac transplant model and also induced donor-specific long-lasting unresponsiveness. Posttransplant tresperimus therapy effectively protected mice from lethal graft-versus-host disease (GVHD) in a dose-related manner. It has been shown to suppress graft rejection as efficiently as cyclosporine A. Indeed, a short course of tresperimus has similar or better effects compared to the effects of cyclosporine in bone marrow, cardiac, and skin transplant models. Prevention of rejection is related to the induction of donor-specific tolerance without affecting immunity to third-party antigens. In addition, CD4+ T-cells from tresperimus-treated animals can transfer donorspecific tolerance to naive animals, an effect not seen with cyclosporine or other traditional immunosuppressive drugs. The mechanism by which tolerance is induced is not clear. Tresperimus binds to Hsc70, a heat shock protein– chaperoned peptide that, among other effects, inhibits nuclear localization of nuclear factor (NF)-kB, which is required for CD40 and CD28 ligation signaling in antigen-presenting cells, an important early step in T-cell costimulation. Locally administered tresperimus appears to be a potential immunosuppressive agent in the management of intraocular inflammation. Tresperimus had been in phase III clinical trial for the treatment of graft-versus-host disease. However, this development was discontinued.

Cinalukast (Ro 24-5913 ) is a selective leukotriene D4 receptor antagonist originated by Roche. Cinalukast inhibits the actions of Leukotriene D4 at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Leukotriene receptor occupation has been correlated with the pathophysiology of asthma, including airway edema and altered cellular activity associated with the inflammatory process, which contributes to the signs and symptoms of asthma. Cinalukast had been investigated for the treatment of asthma, but that study was discontinued.

Cinflumide is a cinnamamide derivative manufactured by Burroughs Wellcome Co. It is claimed to be a CNS voluntary muscle relaxant.

Metazide (RO 2-4969), a isonicotinic acid hydrazide derivative, is a tuberculostatic agent. Metazid causes damage to the membrane of Mycobacterium tuberculosis, inhibits metabolic and oxidative processes, inhibits the synthesis of nucleic acids, inhibiting the proliferation of bacteria inside and outside the cell. It has been used in the treatment of all forms and localizations of active tuberculosis in adults and children

Mesulfamide is a synthetic antibacterial agent.

Tetronasin is a furanone derivative patented by Imperial Chemical Industries Ltd. as antibiotic and feed additive for ruminants. Tetronasin acts as divalent antiporter that binds preferentially with Ca2+ or Mg2+ and inhibits anaerobic fungi and Gram-negative bacteria in vitro.

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.