Abstract: The invention relates to a composition comprising buprenorphine and a ? opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein; AAnAI = [ C max ? ( BUP ) / EC 50 ] [ C max ? ( ANTAGONIST ) / IC 50 ] .
Abstract: The present invention provides fusion polypeptides comprising polypeptide ligands that are modified by circular permutation and fused to at least one polypeptide fusion partner wherein such fusion polypeptides have new, improved or enhanced biological functions or activities. Such improvements include, but are not limited to, increased binding affinity, increased activity, increased agonist activity (super agonist), antagonist activity, increased accessibility, increased flexibility of the active site, increased stability, broader and/or changed substrate specificity, and combinations thereof.
Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
Type:
Application
Filed:
April 15, 2016
Publication date:
August 11, 2016
Applicant:
Alkermes Pharma Ireland Limited
Inventors:
Niels P. Ryde, Peter Snyder, Wei Liu, David M. Slifer
Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
Type:
Application
Filed:
April 15, 2016
Publication date:
August 11, 2016
Applicant:
Alkermes Pharma Ireland Limited
Inventors:
Niels P. Ryde, Peter Snyder, Wei Liu, David M. Slifer
Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
Type:
Grant
Filed:
November 19, 2015
Date of Patent:
June 14, 2016
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
Abstract: The present invention provides fusion polypeptides comprising polypeptide ligands that are modified by circular permutation and fused to at least one polypeptide fusion partner wherein such fusion polypeptides have new, improved or enhanced biological functions or activities. Such improvements include, but are not limited to, increased binding affinity, increased activity, increased agonist activity (super agonist), antagonist activity, increased accessibility, increased flexibility of the active site, increased stability, broader and/or changed substrate specificity, and combinations thereof.
Abstract: This invention is directed to reduction of flake-like aggregation in nanoparticulate compositions. Also encompassed by the invention are compositions comprising a nanoparticulate active agent, at least one surface stabilizer and a flake-like aggregation reducing agent, such as a buffer and a sugar. The nanoparticulate active agent compositions comprise particles of the active agent having an effective average particle size of less than about 2000 nm.
Type:
Grant
Filed:
December 18, 2013
Date of Patent:
May 24, 2016
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Niels P. Ryde, Peter Snyder, Wei Liu, David M. Slifer
Abstract: The invention provides fusion proteins having improved bioactivity comprising a first polypeptide fusion partner and a second polypeptide fusion partner wherein the first fusion partner is linked to the second fusion partner by a mucin-domain polypeptide linker and wherein the bioactivity of the fusion protein of the invention is improved as compared to fusion of the first polypeptide fusion partner and the second polypeptide fusion partner in the absence of the mucin-domain polypeptide linker. Mucin-domain polypeptide linkers comprise a mucin domain that is rich in potential glycosylation sites, and has a high content of serine and/or threonine and proline, which can represent greater than 40% of the amino acids within the mucin domain and further comprise at least about 60% of its mass due to the glycans.
Abstract: This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.
Inventors:
Steven G. Wright, Troy Christensen, Thean Yeoh, Michael E. Rickey, Joyce M. Hotz, Rajesh Kumar, Mark Fineman, Christine Smith, John Ong, David M. Lokensgard, Henry R. Costantino
Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
Type:
Grant
Filed:
February 3, 2015
Date of Patent:
December 29, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.
Abstract: The present invention provides fusion proteins comprising a mucin-domain polypeptide covalently linked to an active protein that has improved properties (e.g. pharmacokinetic and/or physicochemical properties) compared to the same active protein not linked to mucin-domain polypeptide, as well as methods for making and using the fusion proteins of the invention.
Type:
Grant
Filed:
June 6, 2013
Date of Patent:
October 13, 2015
Assignee:
Alkermes, Inc.
Inventors:
Juan Alvarez, Jean Chamoun, Heather C. Losey
Abstract: A drug delivery device having a housing containing a gas generator controlled by an electronic controller. The gas generator generates gas into a reciprocable chamber, whereby reciprocation of the chamber causes a lever to reciprocate a pawl, and this action causes a ratchet to undergo incremental advancement. The device may also be provided with manual control for delivering a bolus dose of drug when necessary.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
September 15, 2015
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Joseph Gross, Izrail Tsals, Gilad Lavi, Gil Yigal, Ehoud Carmel
Abstract: The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.