.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 8,105,586

« Back to Dashboard

Details for Patent: 8,105,586

Title:Soluble glycosaminoglycanases and methods of preparing and using soluble glycosaminoglycanases
Abstract: The invention relates to the discovery of novel soluble neutral active Hyaluronidase Glycoproteins (sHASEGPs), methods of manufacture, and their use to facilitate administration of other molecules or to alleviate glycosaminoglycan associated pathologies. Minimally active polypeptide domains of the soluble, neutral active sHASEGP domains are described that include asparagine-linked sugar moieties required for a functional neutral active hyaluronidase domain. Included are modified amino-terminal leader peptides that enhance secretion of sHASEGP. The invention further comprises sialated and pegylated form of a recombinant sHASEGP to enhance stability and serum pharmacokinetics over naturally occurring slaughterhouse enzymes. Further described are suitable formulations of a substantially purified recombinant sHASEGP glycoprotein derived from a eukaryotic cell that generate the proper glycosylation required for its optimal activity.
Inventor(s): Bookbinder; Louis H. (San Diego, CA), Kundu; Anirban (San Diego, CA), Frost; Gregory I. (Del Mar, CA)
Assignee: Halozyme, Inc. (San Diego, CA)
Filing Date:Jun 15, 2010
Application Number:12/802,864
Claims:1. A pharmaceutical composition, comprising: a) a hyaluronidase glycoprotein that is active at neutral pH and contains at least one sugar moiety that is covalently attached to an asparagine (N) residue of the hyaluronidase polypeptide, wherein: (i) the hyaluronidase glycoprotein consists of the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1; or (ii) the hyaluronidase glycoprotein contains amino acid substitutions in the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1, whereby the amino acid-substituted hyaluronidase glycoprotein consists of a sequence of amino acids that has at least 95% amino acid sequence identity with the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1; and b) a steroidal anti-inflammatory drug selected from among alclomethasones, algestones, beclomethasones, betamethasones, budesonides, clobetasols, clobetasones, clocortolones, cloprednols, corticosterones, cortisones, cortivazols, deflazacorts, desonides, desoximetasones, dexamethasones, difluorosones, diflucortolones, difluprednates, enoxolones, fluazacorts, flucloronides, flumethasones, flunisolides, fluocinolones, fluocinonides, fluocortins, fluocortolones, fluorometholones, fluperolones, fluprednidenes, fluprednisolones, flurandrenolides, fluticasones, formocortals, halcinonides, halobetasols, halometasones, halopredones, hydrocortamates, hydrocortisones, loteprednol etabonate, mazipredones, medrysones, meprednisones, methylprednisolones, mometasone furoate, paramethasones, prednicarbates, prednisolones, prednisones, prednivals, prednylidenes, rimexolones, tixocortolsand triamcinolones.

2. The pharmaceutical composition of claim 1, wherein the steroidal anti-inflammatory drug is a dexamethasone.

3. The pharmaceutical composition of claim 1, wherein the steroidal anti-inflammatory drug is selected from among hydrocortisone acetate, dexamethasone 21-phosphate, prednisolone 25-diethylamino-acetate, prednisolone sodium phosphate, triamcinolone acetonide, triamcinolone benetonide, and triamcinolone hexacetonide.

4. A pharmaceutical composition of claim 1, wherein the hyaluronidase glycoprotein is modified with a polymer.

5. A pharmaceutical composition of claim 4, wherein the polymer is a dextran or a pegylation moiety.

6. The pharmaceutical composition of claim 1, wherein the hyaluronidase glycoprotein is pegylated.

7. A pharmaceutical composition of claim 1, wherein the hyaluronidase glycoprotein consists of the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482 or 36-483 of SEQ ID NO:1.

8. A pharmaceutical composition of claim 1 that comprises a polypeptide that consists of the sequence of amino acids set forth as amino acids 36-482 of SEQ ID NO:1.

9. A pharmaceutical composition of claim 8, wherein the hyaluronidase glycoprotein is modified with a polymer.

10. A pharmaceutical composition of claim 9, wherein the polymer is a pegylation moiety or dextran.

11. The composition of claim 8, wherein the hyaluronidase glycoprotein is pegylated.

12. A pharmaceutical composition of claim 1, wherein the composition is formulated for subcutaneous administration.

13. The pharmaceutical composition of claim 1, wherein the hyaluronidase glycoprotein is produced by expression of a nucleic acid molecule that encodes amino acids 36-482 of SEQ ID NO:1 in a mammalian cell.

14. The pharmaceutical composition of claim 13, where the mammalian cell is a CHO cell.

15. The pharmaceutical composition of claim 1, wherein the hyaluronidase glycoprotein is secreted when expressed in CHO cells.

16. A combination, comprising: a) a first composition that comprises a hyaluronidase glycoprotein that is active at neutral pH and contains at least one sugar moiety that is covalently attached to an asparagine (N) residue of the hyaluronidase polypeptide, wherein: (i) the hyaluronidase glycoprotein consists of the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1; or (ii) the hyaluronidase glycoprotein contains amino acid substitutions in the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1, whereby the amino acid-substituted hyaluronidase glycoprotein consists of a sequence of amino acids that has at least 95% amino acid sequence identity with the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482, or 36-483 of SEQ ID NO:1; and b) a second composition that comprises a steroidal anti-inflammatory drug selected from among beclomethasones, betamethasones, budesonides, clobetasols, clobetasones, clocortolones, cloprednols, corticosterones, cortisones, cortivazols, deflazacorts, desonides, desoximetasones, dexamethasones, difluorosones, diflucortolones, difluprednates, enoxolones, fluazacorts, flucloronides, flumethasones, flunisolides, fluocinolones, fluocinonides, fluocortins, fluocortolones, fluorometholones, fluperolones, fluprednidenes, fluprednisolones, flurandrenolides, fluticasones, formocortals, halcinonides, halobetasols, halometasones, halopredones, hydrocortamates, hydrocortisones, loteprednol etabonate, mazipredones, medrysones, meprednisones, methylprednisolones, mometasone furoate, paramethasones, prednicarbates, prednisolones, prednisones, prednivals, prednylidenes, rimexolones, tixocortols and triamcinolones.

17. A combination of claim 16, wherein the hyaluronidase glycoprotein consists of the sequence of amino acids set forth as amino acids 36-477, 36-478, 36-479, 36-480, 36-481, 36-482 or 36-483 of SEQ ID NO:1.

18. A combination of claim 16, wherein the first composition comprises a polypeptide that consists of the sequence of amino acids set forth as amino acids 36-482 of SEQ ID NO:1.

19. A combination of claim 16, wherein the hyaluronidase glycoprotein is modified with a polymer.

20. A combination of claim 19, wherein the polymer is PEG or dextran.

21. A combination of claim 16, wherein the hyaluronidase glycoprotein is pegylated.

22. The combination of claim 16 that is packaged as a kit.

23. The combination of claim 21, wherein the hyaluronidase glycoprotein is produced by expression of a nucleic acid molecule that encodes amino acids 36-482 of SEQ ID NO:1 in a mammalian cell.

24. The combination of claim 16, wherein the hyaluronidase glycoprotein is produced by expression of a nucleic acid molecule that encodes amino acids 36-482 of SEQ ID NO:1 in a mammalian cell.

25. The combination of claim 24, where the mammalian cell is a CHO cell.

26. The combination of claim 16, wherein the steroidal anti-inflammatory drug is selected from among hydrocortisone acetate, dexamethasone 21-phosphate, prednisolone 25-diethylamino-acetate, prednisolone sodium phosphate, triamcinolone acetonide, triamcinolone benetonide and triamcinolone hexacetonide.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc