Treatment of bleeding with low half-life fibrinogen
US-9212215-B2 · Dec 15, 2015 · US
Factor VIII conjugates
US9364520B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9364520-B2 |
| Application number | US-54070309-A |
| Country | US |
| Kind code | B2 |
| Filing date | Aug 13, 2009 |
| Priority date | Nov 12, 2004 |
| Publication date | Jun 14, 2016 |
| Grant date | Jun 14, 2016 |
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- Title
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- Abstract
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Abstract
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This invention relates to Factor VIII muteins that are covalently bound, at a predefined site that is not an N-terminal amine, to one or more biocompatible polymers such as polyethylene glycol. The mutein conjugates retain FVIII procoagulant activity and have improved pharmacokinetic properties.
First claim
Opening claim text (preview).
We claim: 1. An isolated polypeptide conjugate comprising a functional factor VIII polypeptide and one or more biocompatible polymers, wherein the functional factor VIII polypeptide comprises the amino acid sequence of SEQ ID NO: 4 or an allelic variant thereof and has a B-domain, and further wherein the biocompatible polymer comprises polyalkylene oxide and is covalently attached to the functional factor VIII polypeptide at the B-domain. 2. The isolated polypeptide conjugate of claim 1 , wherein the biocompatible polymer comprises polyethylene glycol. 3. The isolated polypeptide conjugate of claim 2 , wherein the polyethylene glycol comprises methoxypolyethylene glycol. 4. The isolated polypeptide conjugate of claim 3 , wherein the methoxypolyethylene glycol has a size range of from 3 kD to 100 kD. 5. The isolated polypeptide conjugate of claim 3 , wherein the methoxypolyethylene glycol has a size range of from 5 kD to 64 kD. 6. The isolated polypeptide conjugate of claim 3 , wherein the methoxypolyethylene glycol has a size range of from 5 kD to 43 kD. 7. The isolated polypeptide conjugate of claim 2 , wherein the polyethylene glycol has a size of 5, 12, 22, 30, or 43 kD. 8. A pharmaceutical composition comprising a therapeutically effective amount of the isolated polypeptide conjugate of claim 1 and a pharmaceutically acceptable adjuvant. 9. A pharmaceutical composition comprising (1) a therapeutically effective amount of a monopegylated polypeptide conjugate, wherein the monopegylated polypeptide conjugate comprises a functional factor VIII polypeptide and one polyethylene glycol polymer, the functional factor VIII polypeptide comprises the amino acid sequence of SEQ ID NO: 4 or an allelic variant thereof and has a B-domain, and the polyethylene glycol is covalently attached to the functional factor VIII polypeptide at the B-domain; and (2) a pharmaceutically acceptable adjuvant.
Assignees
Inventors
Classifications
Local antiseptics · CPC title
the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol · CPC title
Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents · CPC title
Drugs for disorders of the blood or the extracellular fluid · CPC title
Fusion polypeptide · CPC title
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Frequently asked questions
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- What does patent US9364520B2 cover?
- This invention relates to Factor VIII muteins that are covalently bound, at a predefined site that is not an N-terminal amine, to one or more biocompatible polymers such as polyethylene glycol. The mutein conjugates retain FVIII procoagulant activity and have improved pharmacokinetic properties.
- Who is the assignee on this patent?
- Pan Clark Q, Murphy John E, Mei Baisong, and 7 more
- What technology area does this patent fall under?
- Primary CPC classification A61K38/37. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jun 14 2016 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).