Patent Granted on Long-Acting Drug for Multiple Sclerosis

Mountain View Pharmaceuticals, Inc. (“MVP”), a privately-held California corporation with expertise in the application of advanced polymer-coupling technology to make protein-based drugs safer and longer acting, announced today that it has been awarded European Patent No. 1 667 708 B1, titled “Polyethylene Glycol Conjugates of Interferon-beta-1b with Enhanced in vitro Biological Potency.” The conjugates covered by this patent could enable less frequent and better tolerated dosing of one of the most widely used treatments worldwide for relapsing-remitting multiple sclerosis, interferon-beta-1b.

The invention described in the European Patent relates to methods for the preparation of conjugates of poly(ethylene glycol), and derivatives thereof, with interferon-beta-1b. Compared to the corresponding unconjugated bioactive components, the conjugates of the invention have increased stability (i.e., longer shelf life and longer half-lives in vivo). In addition, compared to conjugates of the same bioactive component prepared with polymer chains that are attached randomly to solvent-accessible sites along the polypeptide chains, the conjugates of the invention have increased receptor-binding activity and increased potency.

The MVP invention also provides the conjugates used in methods of preventing, diagnosing, or treating physical disorders. Physical disorders treated or prevented include cancers (e.g., a breast cancer, a uterine cancer, an ovarian cancer, a prostate cancer, a testicular cancer, a lung cancer, a leukemia, a lymphoma, a colon cancer, a gastrointestinal cancer, a pancreatic cancer, a bladder cancer, a kidney cancer, a bone cancer, a neurological cancer, a head and neck cancer, a skin cancer, a sarcoma, a carcinoma, an adenoma and a myeloma); infectious diseases (e.g., bacterial diseases, fungal diseases, parasitic diseases and viral diseases (such as a viral hepatitis, a disease caused by a cardiotropic virus, HIV/AIDS )); and genetic disorders (e.g., anemia, neutropenia, thrombocytopenia, hemophilia, dwarfism and se- vere combined immunodeficiency disease (“SCID”); autoimmune disorders (e.g., psoriasis, systemic lupus erythematosus and rheumatoid arthritis) and neurodegenerative disorders (e.g., various forms and stages of multiple sclerosis (“MS”) such as relapsing-remitting MS, primary progressive MS and secondary progressive MS; Creutzfeldt-Jakob Disease; Alzheimer’s Disease; and the like).

The granting of this latest European Patent comes just months three months after the United States Patent and Trademark Office issued U.S. Patent No. 8,129,330 titled “Polymer Conjugates with Decreased Antigenicity, Methods of Preparation and Uses Thereof.”  

“The U.S. patent that was issued to MVP on March 6th has been granted more than five-and-one-half years of patent term adjustment, in recognition of the long delay between the filing of the application in 2002 and issuance of the patent. As a result, this patent is not scheduled to expire before mid-2028,” stated Dr. Eldora Ellison, MVP’s lead patent attorney at Sterne Kessler Goldstein & Fox, in Washington, D.C.  MVP’s recently issued U.S. patent, which includes 94 claims covering PharmaPEG conjugates of numerous classes of proteins, glycoproteins and peptides.  The company believes the U.S. Patent will be a key component of future business development and licensing activities.

Patents disclosing and claiming PharmaPEG conjugates have been granted to MVP previously in 18 other countries, while patents disclosing and claiming PEG conjugates of interferon-beta-1b have been granted to MVP previously in 13 countries outside of Europe. The new European patent, with 46 claims including claims to methoxyPEG (“mPEG”) and hydroxyPEG conjugates of non-glycosylated interferon-beta, will be a key component of the company’s partnering and licensing activities.

“In contrast with other patents and publications relating to PEG conjugates of interferon-beta, MVP’s new European patent claims polymer conjugates of interferon-beta-1b that have increased in vitro potency, measured with human cancer cells in culture, and methods of synthesis of these novel conjugates,” stated Dr. Mark G. P. Saifer, MVP’s Vice President and Scientific Director. “If our preclinical results are predictive of the performance of the PEG conjugates in humans, conversion of interferon-beta-1b to a long-acting form with higher potency could enhance the utility of this drug in the treatment of multiple sclerosis, viral infections and other conditions.”

MVP also announced the publication of an invited scientific report, titled “Next-Generation PEGylation Enables Reduced Immunoreactivity of PEG-Protein Conjugates,” in the June 2012 issue of Drug Development & Delivery.  This new publication provides additional evidence for the immunologic advantages of protein conjugates synthesized with the company’s improved PEGylation reagents (PharmaPEG® conjugates). PharmaPEG®forms significantly less antigenic and less immunogenic conjugates than mPEG, which is used in all currently marketed PEGylated drugs. For a wide variety of proteins, the reductions in immune responses to PharmaPEG conjugates, compared with mPEG conjugates of the same proteins, have ranged from 2-fold to >1,000-fold, as reported in Drug Development & Delivery, as well as in a recent publication in Bioconjugate Chemistry. The decreased immunoreactivity results from replacement of the methoxy group of mPEG by a hydroxy group at the end of the polymer that is not attached to the protein.

“MVP’s technology related to long-acting forms of drugs based on therapeutic enzymes or cytokines is the product of more than a decade of research and represents a major advance directed toward the multi-billion-dollar market for PEGylated proteins,” said Dr. Merry R. Sherman, Chief Executive Officer and President of MVP. “Our recent publications illustrating the advantages of PharmaPEG-protein conjugates, compared with conventional mPEG-protein conjugates, are expected to reach a wide audience of pharmaceutical professionals, including those attending the Biotechnology International Organization Conference (“BIO 2012”) in Boston.”

Dr. Sherman will make a presentation on MVP’s “Next-Generation PEGylation Technology” at BIO 2012 in the BioProcess Theater in Booth 0387 of the Exhibition Hall, at 2 pm on Tuesday, June 19th.

To date, MVP has been granted 170 patents in 50 countries and regions. Of these patents, 105 are co-assigned to Duke University and are licensed to Savient Pharmaceuticals, Inc. for the right to make, use, offer for sale and sell pegloticase.


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