PHARMACEUTICAL COMPOSITIONS CONTAINING sc(Fv)2
US-2016168259-A1 · Jun 16, 2016 · US
Structural isomers of sc(Fv)2
US9493569B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9493569-B2 |
| Application number | US-91011706-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 31, 2006 |
| Priority date | Mar 31, 2005 |
| Publication date | Nov 15, 2016 |
| Grant date | Nov 15, 2016 |
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Abstract
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Structural isomers in sc(Fv)2 compositions of anti-human Mpl antibody and humanized anti-human Mpl antibody were separated, and the obtained structural isomers were cleaved at their linkers to confirm that the structural isomers are of single chain diabody type and bivalent scFv type. In addition, the agonistic activities of these structural isomers were revealed to be significantly different. Furthermore, the present inventors discovered that the content ratio of the structural isomers in sc(Fv)2 compositions could be regulated by altering temperature, modifying lengths of the linkers of sc(Fv)2, or amino acids in their variable regions.
First claim
Opening claim text (preview).
The invention claimed is: 1. A pharmaceutical composition comprising a monospecific sc(Fv)2 that comprises four variable regions V1 to V4 in order from amino terminus to carboxy terminus, a first peptide linker connecting variable regions V1 and V2, a second peptide linker connecting variable regions V2 and V3, and a third peptide linker connecting variable regions V3 and V4, wherein the length of each of the first, second, and third linkers is 15 to 30 amino acids, and wherein at least 90% of the sc(Fv)2 in the pharmaceutical composition is in the form of a single-chain diabody-type isomer, in which V1 is associated with V4 and V2 is associated with V3. 2. The pharmaceutical composition of claim 1 , wherein the single-chain diabody-type isomer binds to a receptor. 3. The pharmaceutical composition of claim 1 , wherein the single-chain diabody-type isomer has an agonistic activity. 4. The pharmaceutical composition of claim 1 , wherein the first, second, and third linkers are each 15 amino acids in length. 5. A pharmaceutical composition comprising a monospecific sc(Fv)2 that comprises four variable regions V1 to V4 in order from amino terminus to carboxy terminus, a first peptide linker connecting variable regions V1 and V2, a second peptide linker connecting variable regions V2 and V3, and a third peptide linker connecting variable regions V3 and V4, wherein the length of each of the first, second, and third linkers is 15 to 30 amino acids, wherein at least 90% of the sc(Fv)2 in the pharmaceutical composition is in the form of a single-chain diabody-type isomer, in which V1 is associated with V4 and V2 is associated with V3, and wherein the single-chain diabody-type isomer of the sc(Fv)2 has greater activity than a bivalent scFv-type isomer of the sc(Fv)2. 6. The pharmaceutical composition of claim 5 , wherein the single-chain diabody-type isomer binds to a receptor. 7. The pharmaceutical composition of claim 5 , wherein the single-chain diabody-type isomer has an agonistic activity. 8. The pharmaceutical composition of claim 5 , wherein the first, second, and third linkers are each 15 amino acids in length. 9. The pharmaceutical composition of claim 1 , wherein at least 95% of the sc(Fv)2 in the pharmaceutical composition is in the form of the single-chain diabody-type isomer. 10. The pharmaceutical composition of claim 5 , wherein at least 95% of the sc(Fv)2 in the pharmaceutical composition is in the form of the single-chain diabody-type isomer. 11. The pharmaceutical composition of claim 1 , wherein the first, second, and third linkers are each 20 amino acids in length. 12. The pharmaceutical composition of claim 1 , wherein the first, second, and third linkers are each 30 amino acids in length. 13. The pharmaceutical composition of claim 5 , wherein the first, second, and third linkers are each 20 amino acids in length. 14. The pharmaceutical composition of claim 5 , wherein the first, second, and third linkers are each 30 amino acids in length.
Assignees
Inventors
Classifications
Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title
Diabody or triabody · CPC title
Agonist effect on antigen · CPC title
- C07K16/2866Primary
against receptors for cytokines, lymphokines, interferons · CPC title
Single chain antibody (scFv) · CPC title
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Frequently asked questions
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- What does patent US9493569B2 cover?
- Structural isomers in sc(Fv)2 compositions of anti-human Mpl antibody and humanized anti-human Mpl antibody were separated, and the obtained structural isomers were cleaved at their linkers to confirm that the structural isomers are of single chain diabody type and bivalent scFv type. In addition, the agonistic activities of these structural isomers were revealed to be significantly different. …
- Who is the assignee on this patent?
- Igawa Tomoyuki, Tsunoda Hiroyuki, Koga Akiko, and 2 more
- What technology area does this patent fall under?
- Primary CPC classification C07K16/2866. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Nov 15 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 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).