Oxpheneridine is a mu opioid receptor agonist that possesses the spasmolytic activity and acts as a narcotic analgesic. However, this compound was not listed as an illegal drug, because of its poor solubility and low doses didn’t produce any addiction. Information about the current use of this drug is not available.

Clazuril is benzene-acetonitrile derivative, developed by Janssen Pharmaceutica as an anticoccidial agent for the treatment of pigeons. The anticoccidial effect is due to a cidal effect on the endogenous stages of the Eimeria species.

Octafonium (or octaphonium) was used as an antiseptic. Information about the current use of this drug is not available.

Lufironil (HOE 077) is an inhibitor of prolyl 4-hydroxylase. In preclinical studies, it prevented liver fibrosis by inhibiting not only the hydroxylation of proline but also the activation of Ito cells, which are considered the main collagen-producing cells, resulting in reduced expression of procollagen mRNA. Lufironil was being developed for the treatment of chronic liver diseases including alcoholic hepatitis and liver cirrhosis.

Declopramide is an apoptosis inducer. Also, it inhibits NFkappaB activation by inhibition of IkappaBbeta breakdown. In preclinical research, Declopramide demonstrated strong antitumor properties. It had been in phase II clinical trials for the treatment of colorectal cancer. However, this research has been discontinued.

Loviride (R 89439) is a non-nucleoside inhibitor of reverse transcriptase. It inhibits virion and recombinant reverse transcriptase of HIV-1. It was being studied in the combination therapy of HIV infection with other anti-HIV agents.

Zibotentan (ZD4054) is a potent and specific orally available endothelin A (ETA) receptor antagonist, with no measurable affinity for endothelin B receptor. Activation of the ETA receptor by ET-1 has emerged as an important factor promoting tumor cell proliferation, survival, angiogenesis, migration, invasion, and metastasis in several tumor types. Zibotentan inhibits endothelin-mediated mechanisms that promote tumour cell proliferation. Zibotentan was being developed by AstraZeneca as treatment for heart failure, hormone resistant prostate cancer and other cancers including non-small cell lung, ovarian and breast cancer. However, following disappointing results from a phase III trial in patients with advanced prostate cancer, AstraZeneca decided to discontinue the development of zibotentan as a potential treatment for cancer. AstraZeneca undertook preclinical studies in the UK with zibotentan to investigate its potential as a treatment for heart failure. However, development for this indication has been discontinued.

Rafabegron (also known as TAK-677 ) is an indole derivative patented by Dainippon Pharmaceutical Co., Ltd., as antidiabetics and antiobesity agent. Rafabegron asts as beta3-adrenergic agonist. In preclinical studies Rafabegron reduced the total weight of white adipose tissues by reducing the size of the adipocytes, an effect associated with the normalization of tumor necrosis factor-alpha and leptin expression levels in micce. The levels of uncoupling protein (UCP)-1 mRNA in brown adipose tissue were increased threefold. Rafabegron caused a marked increase (20- to 80-fold) in the expression of UCP-1 in white adipose tissues. In clinical trials. Rafabegron has no effect on 24-h respiratory quotient or fat oxidation but does slightly increase 24-h energy expenditure at the highest dose. The acute studies showed large interindividual variability in plasma concentrations of Rafabegron indicating some possible problems with bioavailability and therefore efficacy. Based on these data further development was discontinued.

Pfizer's CP-547632 is a selective inhibitor of VEGFR-2 tyrosine kinase that was discovered during Pfizer's collaboration with OSI Pharmaceuticals. CP-547632, was identified as a potent inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases (IC(50) = 11 and 9 nM, respectively). It is selective relative to epidermal growth factor receptor, platelet-derived growth factor beta, and other related TKs. It also inhibits VEGF-stimulated autophosphorylation of VEGFR-2 in a whole cell assay with an IC(50) value of 6 nM. After oral administration of CP-547632 to mice bearing NIH3T3/H-ras tumors, VEGFR-2 phosphorylation in tumors was inhibited in a dose-dependent fashion (EC(50) = 590 ng/ml). CP-547,632 is a well-tolerated, orally-bioavailable inhibitor presently under clinical investigation for the treatment of human malignancies. CP-547632 is in phase I for the treatment of diabetic retinopathy and age-related macular degeneration.

Demethoxycurcumin is a derivative or curcumin and represents one of the major active components of curcumin products isolated from Curcumae sp. In preclinical models, Demethoxycurcumin inhibits LPS-induced nitric oxide (NO) production, and expression of iNOS and COX2 in RAW264.7 cells by blocking NF-kB activation. Demethoxycurcumin also inhibits NF-kB dependent iNOS, TNFα and IL-1β expression in LPS-treated rat microglial cells. Demethoxycurcumin suppresses the expression of MMPs and ICAM-1 in MDA-MB-231 human breast cancer cells by inhibition of NF-kB. Demethoxycurcumin is currently in Phase I clinical trials.