Tezacitabine is a cytidine derivative patented by Merrell Dow Pharmaceuticals, Inc. as an antineoplastic and antiviral agent. Tezacitabine acts as irreversible ribonucleotide reductase inhibitor and DNA chain terminator. Tezacitabine shows as potent activity in a broad spectrum of tumor cell lines and in vivo tumor models, including human colon, prostate, and breast tumor xenografts, In clinical trials combination of Tezacitabine and 5-Fluorouracil exerts favor influences in patients with advanced solid tumors particularly in patients with esophageal and other gastrointestinal carcinomas.

Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.

Nikkomycin Z is an antifungal drug that inhibits chitin synthase. It has been reported that it inhibits chitin synthases (Chs) 1 and 3, but not 2, of Saccharomyces cerevisiae. Later it was found that nikkomycin Z inhibited all three Chs isozymes of Candida albicans (CaChs). The IC(50) value for CaChs1 is 15 uM, for CaChs2 0.8 uM, and for CaChs3 13 uM. Nikkomycin Z is under development as an orphan product for treatment of coccidioidomycosis. Nikkomycin Z has been used in trials studying the treatment and basic science of Coccidioidomycosis. In February 2006, nikkomycin z was designated as an orphan drug for the treatment of Coccidioidomycosis.

Dovitinib is an orally active small molecule that exhibits potent inhibitory activity against multiple receptor tyrosine kinases (RTK) involved in tumor growth and angiogenesis. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. There are several ongoing Phase I/III clinical trials for dovitinib.

Mofegiline (MDL 72,974A or (E)-2-(4-fluorophenethyl)-3-fluoroallylamine, hydrochloride), is a selective and irreversible inhibitor of monoamine oxidase type B (MAO-B) both in vitro and in vivo. In addition, mofegiline inhibits semicarbazide-sensitive amine oxidase activity from human serum and saphenous vein. In phase II studies, MDL 72,974A is proving to be a useful adjunct to conventional therapy of Parkinson's disease. It seems mofegiline development was discontinued.

Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.

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.

Mirfentanil was developed as CNS analgesic with a short duration of action. It induced antinociception predominately through mu opioid receptors. It was shown that at doses larger than those, which exert opioid effects, mirfentanil had nonopioid analgesic effects. The drug was successfully encapsulated in liposomes having a variety of compositions. The lipid composition of the formulation was varied to optimize the stabilization of liposomes and the encapsulation of solutes. Mirfentanil participated in phase II clinical trials for the treatment of pain. However, this study was discontinued.

FLESINOXAN, a phenylpiperazine derivative, is a selective agonist for 5-HT1A receptors. It is an antidepressant agent which clinical development was stopped.

Galdansetron is a selective serotonin antagonist compound that is effective against vomiting and nausea. This type of drug is used to treat motion sickness or side effects of chemotherapy or anesthetics.