Immunoconjugates with an Intracellularly-Cleavable Linkage
US-2016287722-A1 · Oct 6, 2016 · US
Anti-HER2 antibody-drug conjugate
US10155821B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10155821-B2 |
| Application number | US-201615221851-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 28, 2016 |
| Priority date | Jan 31, 2014 |
| Publication date | Dec 18, 2018 |
| Grant date | Dec 18, 2018 |
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Abstract
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As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L 1 -L 2 -L P -NH—(CH 2 )n 1 -L a -(CH 2 )n 2 -C(═O)— wherein the anti-HER2 antibody is connected to the terminal L 1 , and the antitumor compound is connected to the carbonyl group of the —(CH 2 )n 2 -C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position.
First claim
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The invention claimed is: 1. An antibody-drug conjugate, wherein a linker and an antitumor compound represented by the following formula and anti-HER2 antibody are connected: -(Succinimid-3-yl-N)—CH 2 CH 2 CH 2 CH 2 CH 2 —C(═O)-GGFG (SEQ ID NO: 3) —NH—CH 2 —O—CH 2 —C(═O)—(NH-DX) wherein -(Succinimid-3-yl-N)— has a structure represented by the following formula: which is connected to the antibody at position 3 thereof and is connected to a methylene group in the linker structure containing this structure on the nitrogen atom at position 1, and (NH-DX) represents a group represented by the following formula: wherein the nitrogen atom of the amino group at position 1 is the connecting position. 2. The antibody-drug conjugate according to claim 1 , wherein an average number of units of the selected one drug-linker structure conjugated per antibody is in a range of from 2 to 8. 3. The antibody-drug conjugate according to claim 1 , wherein an average number of units of the selected one drug-linker structure conjugated per antibody is in a range of from 3 to 8. 4. A drug containing the antibody-drug conjugate according to claim 1 or a salt thereof. 5. A pharmaceutical composition containing the antibody-drug conjugate according to claim 1 or a salt thereof as an active component, and a pharmaceutically acceptable formulation component. 6. The antibody-drug conjugate according to claim 1 , wherein the anti-HER2 antibody comprises a heavy chain and a light chain selected from the group: a heavy chain consisting of an amino acid sequence consisting of amino acid residues 1 to 449 of SEQ ID NO: 1 and a light chain consisting of an amino acid sequence consisting of amino acid residues 1 to 214 of SEQ ID NO: 2, and a heavy chain consisting of the amino acid sequence of SEQ ID NO: 1 and a light chain consisting of the amino acid sequence of SEQ ID NO: 2. 7. The antibody-drug conjugate according to claim 6 , wherein the anti-HER2 antibody comprises a heavy chain consisting of the amino acid sequence consisting of amino acid residues 1 to 449 of SEQ ID NO: 1 and a light chain consisting of the amino acid sequence consisting of amino acid residues 1 to 214 of SEQ ID NO: 2. 8. The antibody-drug conjugate according to claim 6 , wherein the anti-HER2 antibody comprises a heavy chain consisting of the amino acid sequence of SEQ ID NO: 1 and a light chain consisting of the amino acid sequence of SEQ ID NO: 2.
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- C07K16/32Primary
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- What does patent US10155821B2 cover?
- As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L 1 -L 2 -L P -NH—(CH 2 )n 1 -L a -(CH 2 )n 2 -C(═O)—…
- Who is the assignee on this patent?
- Daiichi Sankyo Co Ltd
- What technology area does this patent fall under?
- Primary CPC classification C07K16/32. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Dec 18 2018 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).