PLATFORM (3)
Oncology

(3)(a) Canopus BioPharma's patented flavonoid CB980.

These pipeline technologies are scheduled for inclusion in the development plan 2009-2011, however ongoing negotiations with Pharma partners may expedite this development program.

CB980 is a substituted flavone that has demonstrated antiviral activity against certain strains of picornaviruses, notably the common cold virus (Rhinoviruses). CB980 and its precursors have shown antiviral activity in culture against HIV in T cells and macrophages. Additionally CB980 has demonstrated anti-toxoplasmosis activity, in both tissue culture and animal studies comparable in activity to prescription drugs currently available for the treatment of toxoplasmosis.

In the course of our research with CB980 Canopus BioPharma has discovered and confirmed a unique attribute of this compound. When combined with anti-cancer or antiviral nucleotide therapeutic drugs CB980 has the unique ability of stimulating the expression and activity of Na+/nucleoside co-transporter [CNT] molecules, which preferentially transport pyrimidine nucleosides and also accept adenosine and guanosine. This nucleoside transporter enhancing property accounts for CB980's ability, when used in combination with specific therapeutic nucleosides (antibacterial, anti-parasitic, anti-cancer and antiviral drugs), of lowering the associated toxicity of the combination drug and enhancing efficacy. For example when CB980 was given in combination with the anti-metabolite cancer drug gemcitabine (GemzarTM) (4-amino-1-[3,3-difluoro-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-1H-pyrimidin- 2-one) it caused a shifting of the IC70 values corresponding to 10 to 19 fold increase of anti-tumor activity. Similar enhancement of IC50 values was demonstrated for the anti-viral prescription drug, Zidovudine when combined with CB980.

CB980 has the unique potential to add substantial therapeutic value to current generic prescription nucleoside compounds since it synergistically lowers toxicity and, combined with its own ability to inhibit viruses and certain pathogens (toxoplasmosis), CB980 enhances the effectiveness of the nucleoside with which it is combined. Canopus BioPharma will exploit this novel formulation advantage which CB980 will give to generic drugs.

Canopus BioPharma has a patent granted in the USA, for the use of CB980 and related compounds, in the treatment of infections, particularly for viral or parasite infections. Other patents are pending relating to the use of other CB980 analogues in combination therapy for reduction of toxicity of chemotherapeutic agents. Additional patents are pending relating to the unique ability of CB980 to improve the therapeutic effects and substantially reduce the toxicity of dihydrofolate reductase inhibitor compounds ,such as methotrexate , pirexicham etc. for the therapy of cancer and rheumatoid arthritis's, and psoriasis.

(3)(b) Steroid Metabolic Enzyme Inhibitors for Cancer Treatment-

This pipeline technology is scheduled for inclusion in the development plan 2009-2011.

Canopus BioPharma has acquired the anti-cancer rights for the use of Compounds coded CB300 and CB310. These compounds have previously demonstrated in-vitro and in-vivo inhibition of tumor growth. These compounds are steroids in structure, but not in their biological action, i.e. they have no androgenic or estrogenic action. These compounds competitively inhibit key enzymes involved cancer cell growth.

(3)(c) Immune Modulation Compounds for Cancer Treatment-

This pipeline technology is scheduled for inclusion in the development plan 2008-2011

Canopus BioPharma has acquired the right to novel plant extracts coded CB3555, CB7524 and CB3411. Following studies by in a Germany Oncology laboratory of the cytotoxic effects of these compounds on human tumor cells line, HT29 and PC3( prostrate cancer cell line) the researcher concluded that CB3555 and CB3536 activity in PC3 are remarkable and might lead to in-vivo efficacy if carefully evaluated in a preclinical model systems.

(3)(d) Cancer Vaccine Candidate.

This technology is currently under active research and development as per our strategic development plan 2007-2009 to initiate a Phase1 study of the vaccine in healthy individuals.

Canopus BioPharma's licensee utilized an anti-serum to a non-cancer antigen (Venom peptide) against a panel of six cancer cell lines (Lymphoma, pancreatic, bladder, small cell lung tumor, colorectal tumor and breast tumor) in a study, the data generated at Nottingham University Hospital showed that the antiserum to the venom peptides inhibited each of the cancer cell lines to a significant degree. Canopus BioPharma has acquired the right to the further development of this cancer vaccine candidate. Our researchers believe that this technology offers the potential to identify and synthesize novel peptide sequences for use as broad spectrum cancer vaccine antigens. Vaccine studies have been completed in primates and humans with venoms as a prophylactic measure for snake bite. The pharmacokinetics and toxicity data from these third party independent studies are available and are facilitating expedited human studies of cancer patients with our venom peptide based cancer vaccine.