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Last Updated: October 16, 2019

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Claims for Patent: 9,920,311

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Summary for Patent: 9,920,311
Title:PEGylated L-asparaginase
Abstract: Disclosed is a conjugate of a protein having substantial L-asparagine aminohydrolase activity and polyethylene glycol. In particular, the polyethylene glycol has a molecular weight less than or equal to about 5000 Da and the protein is an L-asparaginase from Erwinia. The conjugate of the invention has shown superior properties such as maintenance of a high level of in vitro activity and an unexpected increase in half-life in vivo. Also disclosed are methods of producing the conjugate and use of the conjugate in therapy. In particular, a method is disclosed for use of the conjugate in the treatment of cancer, particularly Acute Lymphoblastic Leukemia (ALL). More specifically, a method is disclosed for use of the conjugate as a second line therapy for patients who have developed hypersensitivity or have had a disease relapse after treatment with other L-asparaginase preparations.
Inventor(s): Abribat; Thierry (Sainte Foy les Lyon, FR)
Assignee: Jazz Pharmaceuticals II SAS (Lyons, FR)
Application Number:14/819,305
Patent Claims:1. A conjugate comprising an L-asparaginase from Erwinia chrysanthemi having at least 90% sequence identity to the amino acid of SEQ ID NO:1 and conjugated to at least one polyethylene glycol (PEG) molecule, wherein the at least one PEG has a molecular weight less than 5000, 4000, 3000, or 2500 Da and the conjugate has at least fifty times more in vivo L-asparaginase activity compared to an Erwinia chrysanthemi L-asparaginase not conjugated to PEG.

2. The conjugate of claim 1, wherein said L-asparaginase has at least 95% to 99% sequence identity to the amino acid of SEQ ID NO: 1.

3. The conjugate of claim 1, wherein said L-asparaginase comprises the amino acid of SEQ ID NO: 1.

4. The conjugate of claim 1, wherein the PEG is covalently linked to one or more amino groups of said L-asparaginase.

5. The conjugate of claim 4, wherein the PEG molecules are covalently linked to at least from about 40% to about 100% of the accessible amino groups of said L-asparaginase.

6. The conjugate of claim 1 having the formula: Asp-[NH--CO--(CH.sub.2)x-CO--NH-PEG]n wherein Asp is the L-asparaginase, NH is one or more of the NH groups of the lysine residues and/or the N-terminus in the Asp, PEG is a polyethylene glycol moiety, n is a number that represents at least 40% to 100% of the accessible amino groups in the Asp, and x is an integer ranging from 1 to 8.

7. The conjugate of claim 1, wherein said PEG is monomethoxy-polyethylene glycol.

8. The conjugate of claim 1, wherein said conjugate has at least sixty, seventy, eighty, ninety or one-hundred times more in vivo L-asparaginase activity compared to an Erwinia chrysanthemi L-asparaginase not conjugated to PEG.

9. The conjugate of claim 1, wherein the conjugate has increased residual enzymatic activity in vivo when compared to Erwinia chrysanthemi L-asparaginase conjugated to at least one PEG molecule with a molecular weight of 10,000 Da.

10. The conjugate of claim 1, wherein the L-asparaginase does not cross-react with antibodies which react with Escherichia coli L-asparaginase.

11. The conjugate of claim 1 comprising an L-asparaginase from Erwinia chrysanthemi consisting of the amino acid of SEQ ID NO: 1 and the conjugate has reduced immunogenicity when administered to a human subject hypersensitive to Escherichia coli L-asparaginase.

12. The conjugate of claim 1, wherein the conjugate has an in vitro L-asparaginase activity of at least 60%, 70%, 80%, or 87% of an L-asparaginase not conjugated to PEG.

13. The conjugate of claim 1, wherein said PEG has a molecular weight of less than 5000 Da.

14. The conjugate of claim 1, wherein the PEG molecules are covalently linked to at least 60%, 70%, 80%, 90% or 100% of the accessible amino groups of said L-asparaginase.

Summary for Patent:   See Pricing

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
PCT/EP2010/054156Mar 30, 2010

Details for Patent 9,920,311

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Merck ELSPAR asparaginase VIAL 101063 001 1978-01-10   See Pricing Jazz Pharmaceuticals II SAS (Lyons, FR) 2030-03-30 RX search
Jazz Pharms Inc ERWINAZE asparaginase erwinia chrysanthemi INJECTABLE; INJECTION 125359 001 2011-11-18   See Pricing Jazz Pharmaceuticals II SAS (Lyons, FR) 2030-03-30 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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