Etazepine (5,6-dihydro-5-methyl-11H-11-ethoxy-dibenzo[b,e]azepin-6-one) demonstrates anticonvulsant activity in rodents. Etazepine seems to exert its anticonvulsant effects by activating the GABAergic system.

Fosquidone (also known as GR63178A), a pentacyclic pyrroloquinone that was developed as an anticancer agent. Fosquidone participated in phase II clinical trial for the treatment of patients with colorectal, renal and non-small cell lung cancer. However, the drug didn’t show significant antitumor activity. The further development of this drug was discontinued.

Gomisin A (BESIGOMSIN/GA) one of the major dibenzocyclooctadiene lignans isolated from Schisandra chinensis Baill, has proved to possess a variety of pharmacological effects. It has been found to promote hepatocyte growth factor, limit lipid peroxidation, and inhibit apoptosis in acute hepatic injury animal models. Besigomsine also acts as an anti-inflammatory by preventing the release of arachidonic acid in macrophages in vitro. Laboratory evidence suggests that Besigomsine may have anticarcinogenic effects. Chronic administration of Gomisin A had an antihypertensive effect in AngII-induced hypertensive mice. Gomisin A may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. Also it induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway.

Namitecan (ST1968) is a camptothecin analogue being developed by sigma-tau (a subsidiary of Alfasigma) in Switzerland for the treatment of cancer. Namitecan, a novel hydrophilic camptothecin analog of the 7-oxyiminomethyl series, was selected for clinical development on the basis of its promising preclinical efficacy. Namitecan is a topoisomerase I inhibitor. Namitecan exhibited an acceptable toxicity profile, with neutropenia being the dose-limiting toxic effect, and clinical benefit was appreciable in patients with different tumor types, particularly bladder and endometrium carcinomas.

Azanator (previously known as Sch 15280), a bronchodilator and an antihistamine drug that acts via a non-adrenergic mechanism to block both histaminergically and cholinergically mediated responses in the tracheobronchial tree. Besides, the drug inhibits cyclic CMP phosphodiesterase. Azanator can have a therapeutic application in cases of chronic cough and cystic fibrosis in man.

Sarafloxacin [A 55620] is a quinolone antibiotic that was under development with Abbott Laboratories in the USA. It was removed from clinical use by its manufacturer Abbott Laboratories from April 30, 2001. It was never approved for use in the US or Canada.

Cidoxepin is the cis-isomer of the widely prescribed tricyclic compound doxepin. Commercial preparations of the tricyclic anti-depressant doxepin contain 15% of the more active cis-doxepin and 85% of the trans-isomer. Elorac, Inc., a rapidly growing specialty pharmaceutical company focused on the treatment of dermatological disorders, is pleased to announce that it has acquired worldwide rights to the active agent Cidoxepin from Gideon Pharmaceuticals. Cidoxepin appears to be much more potent than doxepin while having less sedative and cholinergic side effects. Elorac plans to develop oral formulations of the drug to treat urticaria and topical formulations for treatment of atopic and contact dermatitis.

Pinadoline is a competitive PGE2 antagonist. It is an analgesic agent. Pinadoline demonstrated the antinociceptive activity in the rat using the writhing and the formalin tests. In the writhing test, pinadoline was significantly more potent than inhibitors of PG synthesis, but less potent than opiate analgesics. In the formalin test, pinadoline appeared less active than aspirin and ibuprofen and more active than acetaminophen. Pinadoline does not possess the antiinflammatory activity of aspirin and ibuprofen and may be more like acetaminophen, which had diminished antiinflammatory activity. At high concentrations, pinadoline is a non-competitive antagonist of serotonin in guinea-pig ileum.

Metitepine, a psychotropic agent was developed as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors. Metitepine has never been marketed.