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.

Quinotolast (also known as FK021) is an orally active mast cell stabilizer which has a cytoprotective effect on the gastric mucosa. Quinotolast was patented in 1985 by Japanese pharmaceutical company Fujisawa Pharmaceutical Co., Ltd. as an antiallergic and antiulcer agent. In preclinical models, Quinotolast potently inhibited such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. Quinotolast inhibited histamine release from rat peritoneal cells, but it had no antagonistic effect on histamine-, serotonin-, platelet activating factor- or bradykinin-induced cutaneous reactions in rats. Moreover, it was clearly demonstrated that quinotolast and DSCG had a cross tachyphylaxis to inhibit PCA in rats, suggesting that these drugs, at least in part, share the same mechanism of action. Quinotolast caused a significant increase in the mucociliary transport rate in quails. Quinotolast significantly depressed the cough reflex induced by citric acid in normal and bronchitic guinea pigs.

Aranotin, a metabolite of Arachniotus aureus, possesses the antiviral and antibiotic properties. It inhibits viral RNA synthesis against strains of rhino-, coxsackie, polio- and parainfluenza viruses.

Sparfosate (PALA) is a stable transition state analogue for an aspartate transcarbamylase- cartalyzed reaction with antineoplastic activity. PALA is a potent inhibitor of aspartate transcarbamylase (Ki about 10(-8) M for ACTases of various origins), which in whole cells blocks the de novo synthesis of pyrimidines. Thus PALA inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA. In vivo, low doses of PALA inhibit whole body pyrimidine synthesis. While this action is cytotoxic in vitro, extensive human testing demonstrates that PALA alone is devoid of selective antitumor activity. Interest in the therapeutic action of PALA derives from the demonstration that its action potentiates the cytotoxicity of several cytotoxic drugs, notably 5-fluorouracil (5-FU). Development of Sparfosate for cancer and Hepatitis B treatment is assumed to have been discontinued.

Satigrel (previously known as E5510) was developed as an antithrombotic agent. Satigrel antagonized platelet activation by inhibiting phospholipase C and/or A2, which results in suppression of both phosphatidylinositol breakdown and arachidonic acid release from phospholipids, as well as by inhibiting cyclooxygenase. Satigrel was studied in patients with intermittent claudication due to arteriosclerosis obliterans, where the drug improved the cutaneous circulation and symptoms of patients. In addition, the therapeutic effect of satigrel was studied on biopsy-proven chronic rejection after kidney transplantation. Also was shown that the drug had a clinical benefit over aspirin for the treatment of transient ischemic attacks. However, all these studied were apparently discontinued.

Sanfetrinem cilexetil (formerly known as GV 118819), a beta-lactam antibiotic, is the oral prodrug of sanfetrinem. Experiments on rodents have revealed that sanfetrinem cilexetil had strong antibacterial activity in vitro and good pharmacokinetic behavior in mice. This drug was suitable for the treatment of infections caused by a variety of bacteria and participated in a phase II clinical trial. However, this study was discontinued.

Clogestone Acetate (AY-11440) is a steroidal progestin that was synthesized in 1964 and was investigated as a progestin-only contraceptive but was never marketed.

Bucricaine is tetrahydroaminoacridine derivative that has been studied as acetylcholinesterase and monoamine oxidase inhibitor. In animal models, Bucricaine shows a wide spectrum of pharmacological properties, which include analgesic, local anesthetic, analeptic, and respiratory stimulant activities.

Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.

Fluorescein Lisicol (NRL972) is a fluorescent-labelled bile acid analog that is used as an investigational marker for liver function, specifically hepatic biliary transporter function. Fluorescein Lisicol has been used in trials investigating the pharmacokinetics of hepatic cirrhosis, viral hepatitis, non-alcoholic steatohepatitis and non-alcoholic fatty liver disease.