The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in February-March, 2017.
Intranasal Insulin Administration for the Minimization of Anesthesia-Induced Memory Loss; C. X. Gong; The Research Foundation for Mental Hygiene, Inc., U.S. Patent # 9,603,905, March 28, 2017.
Tauopathies are a family of age-associated neurodegenerative diseases, which are characterized histopathologically by the abnormal hyperphosphorylation and aggregation of tau in the brain, and clinically by cognitive impairment and/or motor dysfunction. Tau proteins are proteins that perform the function of stabilizing microtubules in nerve cells. Insulin dysfunction has been shown to induce tau hyperphosphorylation. This patent describes an intranasal administration of insulin that prevents abnormal hyperphosphorylation of tau and cognitive impairment. The patent claims a method of minimizing anesthesia induced memory loss in subject, comprising the step of administering intranasal insulin to the subject prior to administering any anesthesia for plurality of times.
Particles Coated with Zwitterionic Polymers Comprising Sulfobetaine or Carboxybetaine; S. Jiang, S. Chen, Y. Chang, and Z. Zhang; University of Washington; U.S. Patent # 9,598,544; March 21, 2017.
One of the largest obstacles to nanoparticle based applications is non-specific protein adsorption, which can result in cellular uptake, nanoparticle aggregation, immune system response and other disastrous problems for in vivo applications. There is lack of a versatile effective nonfouling (avoiding contamination/adsorption) material. It is a crucial issue for nanoparticle-based applications, particularly in complex media. The invention provides zwitterionic particles (sulfobetaine/carboxybetaine) in which the particle surface has zwitterionic polymers grafted from/to the surface. The surface of the particle has a layer of sulfobetaine/carboxybetaine polymers coupled to the surface having a fibrinogen adsorption of less than about 30 ng/cm2. It is also claimed that nanogels can be prepared using these zwitterionic polymers.
Anti-Pancreatic Cancer Antibodies; D. M. Goldenberg, H. J. Hansen, C. H. Chang, and D. V. Gold; Immunomedics, Inc.; U.S. Patent # 9,599,619; March 21, 2017.
The invention describes the compositions and methods of use of anti-pancreatic cancer antibodies or fragments such as murine, chimeric, humanized or human PAM4 antibodies. The subject antibodies show a number of novel and useful therapeutic characteristics, such as binding with high specificity to pancreatic and other cancers, but not to normal or benign pancreatic tissues and binding to a high percentage of early stage pancreatic cancers. The preferred antibodies are PAM4, which bind to a PAM4 antigen that shows unique cell and tissue distributions compared with other known antibodies. The antibodies and fragments are used for the detection, diagnosis and/ or treatment of cancer, such as pancreatic cancer.
Monoclonal Antibody Therapy for Pancreas Cancer; M. Arlen and K. Tasang; Precision Biologics, Inc., U.S. Patent # 9,592,290; March 14, 2017.
At present, the only potentially curative treatment for pancreatic cancer is surgical removal of the tumor. The invention claims a method of killing cells that express a pancreatic carcinoma associated antigen, by delivering an effective amount of 31.1 monoclonal antibody to the cells, so that they are killed in vitro. Antibody 31.1 represents a protein-directed monoclonal antibody derived by immunizing BALB(c) mice with a preparation of membrane obtained from pooled (human) allogeneic colon carcinoma specimens. The present invention relates to the use of binding equivalents of monoclonal antibody 31.1, including chimerized and/or humanized versions.
Combination Bacteriolytic Therapy for the Treatment of Tumors; L. Dang, C. Bettegowda, K.W. Kinzler, and B.Vogelstein; The Johns Hopkins University; U.S. Patent # 9,572,843; February 21, 2017.
It is still hard to treat solid tumors. The present invention has been attempting to determine whether spores of C. novyi-NT, a strain of anaerobic bacteria, can be used. Angiogenesis is the formation of new blood vessels. This process involves the migration, growth, and differentiation of endothelial cells, which line the inside wall of blood vessels. Solid tumors require angiogenesis to grow to a clinically important size and have often large regions that are poorly vascularized. It becomes difficult to deliver anticancer medicines to these poorly vascularized regions. The tumors are treated by administering to the mammal spores of a toxin-defective, anaerobic bacterium selected from the group consisting of Clostridium novyi and Clostridium sordellii; and administering to the mammal one or more taxane microtubule stabilizing anti-tumor agents; whereby the tumor regresses or its growth is slowed or arrested. The spores are administered intravenously or intratumorally. In another embodiment, the spores, anti-tumor agent and nitrix oxide synthetase inhibitor are administered serially.
Therapeutic Vitamin D Conjugates; T. Soliman, L.M. Hales, D.B. Hall, C. So, H.P. Sard, and V. Hegde; Extend Biosciences, Inc., U.S. Patent # 9,585,934; March 7, 2017
Vitamin D is a group of fat-soluble secosteroids which exists in two main forms - D2 or ergocalciferol, and D3 or cholecalciferol. Vitamin D is made in the skin by sunlight or ingested. It has to be activated via several hydroxylation steps. The non-hormonal form of Vitamin D is converted to the hormonal form as needed. The invention provides a carrierdrug conjugate comprising a targeting group that is a nonhormonal vitamin D and it is not hydroxylated at the carbon 1 position, conjugated at the carbon 3 position to a protein having apelin activity. Apelin is a peptide which in humans is encoded by the APLN gene. Apelin is the endogenous ligand for the G-protein-coupled APJ receptor that is expressed at the surface of some cell types. Here the targeting group is conjugated to said protein via a scaffold that is poly(ethylene glycol). It is administered by a subcutaneous injection.
Emulsion-Derived Particles; J. Jordaan, C. Simpson, D. Brady, N.S. Gardiner, and I.B. Gerber; CSIR; U.S. Patent # 9,574,054; February 21, 2017.
The invention relates to a process for producing emulsionderived particles. Particles containing immobilized enzymes are typically used for biocatalysis and for diagnostics. A key drawback for the current technology is an inadequate surface area for sufficient enzyme immobilization. By “emulsion-derived” it is meant that the particles have been produced or formed using an emulsion technique. Each particle comprising a lattice of the polyethyleneimine strands cross-linked by means of the cross-linking agent, interstitial openings. There are aldehyde functional groups on the lattice with which proteins and/or modified proteins can react, thereby to be bonded to the lattice and hence immobilized. Such particles can be made from o/w, w/o, w/o/w, o/w/o emulsion types. Protein loading is followed by determining the protein concentration in bound and in a dissolved form.