PLATFORM (1)
Antivirals

(1)(a) Influenza Treatment using StatC™

This product is currently under active research and development as per our strategic plan 2007-2009.

Influenza is an infection caused by a family of viruses. These viruses are lipid membrane viruses and like the HIV and Herpes virus they must enter and exit the cells utilizing cholesterol rich cell membrane attachment sites. Statin's interfere with cholesterol synthesis and accordingly reduce the number of cholesterol rich attachment sites (rafts) available for viral entry and exit from cells. Canopus has developed a proprietary combination of prescription Statins together with another propriety GRAS molecule, trademarked StatC™, which has demonstrated in animal models superior preventative anti-viral effect to the prescription drug Tamiflu against virulent H5N1(Avian influenza). StatC™ has also shown anti-viral activity against a range of influenza viruses , the HIV1 virus and Hepatitis C.

(1)(b) AFP SEQUENCES HIV VACCINE CANDIDATE

This pipeline antiviral technology is scheduled for inclusion in the development plan 2009-11

Canopus BioPharma has developed a non-viral antigen as a potential therapeutic and prophylactic vaccine for protection from HIV infection. Canopus BioPharma researched the mechanism of the natural pregnancy associated peptide AFP which causes a specific type of immune suppression in the mother to prevent her rejection of the fetus. Canopus BioPharma discovered that this natural pregnancy associated peptide AFP (alpha-fetoprotein) shares an amino acid sequence homology with the specific amino acid sequences utilized by the HIV virus to cause immunosuppression. By utilizing these specific identified sequences as antigens a potential successful vaccine candidate to HIV will be developed and tested in a primate model.

(1)(c) SpirH™ specially formulated synthetic steroidal lactone as a HIV antiviral agent.

This pipeline technology will commence further development when a licensing partner is identified to fund the already approved clinical trials in South Africa.

SpirH™ is a prescription synthetic steroidal lactone with properties compatible with competitive mineral corticoid antagonism, which are used in the treatment of oedematous states, primary hyper aldosteronism and essential hypertension. The structure of SpirH™ is very similar to aldosterone in man. The active ingredient in SpirH™, steroidal lactone is well known in the medical field for its indication in the cardiovascular area, with very well documented pharmacokinetic profile and well known side effects.

During the course of Canopus BioPharma's research it was discovered that certain proteins on the coat of the HIV virus mimics in binding characteristics the steroid molecule aldosterone. The virus uses this steroid mimic peptide on its surface to bind a mineralocorticoid steroid type receptor and cause electrolyte changes in the infected cell .

Our researchers elucidated this mode of action of the HIV virus by incubating the virus in tissue culture with selected monoclonal antibodies; these monoclonal antibodies block the binding of aldosterone to its receptor, the monoclonals are directed against the steroid binding domain of the mineralocorticoid receptor (MR) and the AFP receptor. The results obtained demonstrated that viral replication was inhibited significantly and most effectively in Macrophages. Canopus BioPharma demonstrated that all Clades of HIV1 were similarly inhibited but that HIV2 was not inhibited, by this monoclonal antibody, thus demonstrating a different mode of cellular pathology for the HIV2 virus family. Following this, Canopus BioPharma screened a selection of prescription aldosterone agonists and antagonists and discovered that certain of these molecules significantly inhibited HIV replication.

SpirH™ and related formulations of aldosterone antagonists will offer the physician and HIV+ patients a new avenue to obstruct HIV viral replication both as a mono-therapy and in association with conventional antivirals to augment their effectiveness. Thus SpirH™ offers the patient and physician a new therapeutic approach to inhibiting the HIV virus and halting the decline of the immune system, utilizing a drug family with over 30 years of patient administration history.

The Medicines Control Council (MCC) of South Africa has granted us approval for to conduct a 30 patient HIV+ clinical trial using SpirH™. The objective of this study is to evaluate the efficacy and safety of SpirH™ in patients with HIV-1 infection as a mono-therapy.

International patent applications are pending on the use of the steroidal lactone family of compounds as antiviral agents.