CKIT antibody drug conjugates
US-10786578-B2 · Sep 29, 2020 · US
Antibody drug conjugates for ablating hematopoietic stem cells
US11357864B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11357864-B2 |
| Application number | US-201716470897-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 19, 2017 |
| Priority date | Dec 21, 2016 |
| Publication date | Jun 14, 2022 |
| Grant date | Jun 14, 2022 |
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- Title
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Abstract
Official abstract text for this publication.
The present invention provides antibody drug conjugates, wherein an antibody or antibody fragment that specifically binds to human cKIT is linked to a drug moiety, optionally through a linker. The present invention further provides pharmaceutical compositions comprising the antibody drug conjugates; and methods of making and using such pharmaceutical compositions for ablating hematopoietic stem cells in a patient in need thereof.
First claim
Opening claim text (preview).
What is claimed is: 1. A conjugate of Formula (I) or a pharmaceutically acceptable salt thereof; A-(L B -(D) n ) y Formula (I) wherein: A is an antibody fragment that specifically binds to human cKIT, wherein the antibody fragment is selected from any of the following: (1) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 (Heavy Chain Complementarity Determining Region 1) of SEQ ID NO: 1, (b) a HCDR2 (Heavy Chain Complementarity Determining Region 2) of SEQ ID NO: 2, and (c) a HCDR3 (Heavy Chain Complementarity Determining Region 3) of SEQ ID NO: 3; and (ii) a light chain variable region that comprises: (d) a LCDR1 (Light Chain Complementarity Determining Region 1) of SEQ ID NO: 16, (e) a LCDR2 (Light Chain Complementarity Determining Region 2) of SEQ ID NO: 17, and (f) a LCDR3 (Light Chain Complementarity Determining Region 3) of SEQ ID NO: 18; (2) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 4, (b) a HCDR2 of SEQ ID NO: 5, (c) a HCDR3 of SEQ ID NO: 3; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 19, (e) a LCDR2 of SEQ ID NO: 20, and (f) a LCDR3 of SEQ ID NO: 21; (3) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 6, (b) a HCDR2 of SEQ ID NO: 2, (c) a HCDR3 of SEQ ID NO: 3; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 16, (e) a LCDR2 of SEQ ID NO: 17, and (f) a LCDR3 of SEQ ID NO: 18; (4) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 7, (b) a HCDR2 of SEQ ID NO: 8, (c) a HCDR3 of SEQ ID NO: 9; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 22, (e) a LCDR2 of SEQ ID NO: 20, and (f) a LCDR3 of SEQ ID NO: 18; (5) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 27, (b) a HCDR2 of SEQ ID NO: 28, (c) a HCDR3 of SEQ ID NO: 29; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 42, (e) a LCDR2 of SEQ ID NO: 17, and (f) a LCDR3 of SEQ ID NO: 43; (6) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 30, (b) a HCDR2 of SEQ ID NO: 31, (c) a HCDR3 of SEQ ID NO: 29; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 44, (e) a LCDR2 of SEQ ID NO: 20, and (f) a LCDR3 of SEQ ID NO: 45; (7) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 32, (b) a HCDR2 of SEQ ID NO: 28, (c) a HCDR3 of SEQ ID NO: 29; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 42, (e) a LCDR2 of SEQ ID NO: 17, and (f) a LCDR3 of SEQ ID NO: 43; (8) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 33, (b) a HCDR2 of SEQ ID NO: 34, (c) a HCDR3 of SEQ ID NO: 35; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 46, (e) a LCDR2 of SEQ ID NO: 20, and (f) a LCDR3 of SEQ ID NO: 43; (9) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 60, (b) a HCDR2 of SEQ ID NO: 61, (c) a HCDR3 of SEQ ID NO: 62; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 75, (e) a LCDR2 of SEQ ID NO: 76, and (f) a LCDR3 of SEQ ID NO: 77; (10) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 63, (b) a HCDR2 of SEQ ID NO: 64, (c) a HCDR3 of SEQ ID NO: 62; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 78, (e) a LCDR2 of SEQ ID NO: 79, and (f) a LCDR3 of SEQ ID NO: 80; (11) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 65, (b) a HCDR2 of SEQ ID NO: 61, (c) a HCDR3 of SEQ ID NO: 62; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 75, (e) a LCDR2 of SEQ ID NO: 76, and (f) a LCDR3 of SEQ ID NO: 77; (12) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 66, (b) a HCDR2 of SEQ ID NO: 67, (c) a HCDR3 of SEQ ID NO: 68; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 81, (e) a LCDR2 of SEQ ID NO: 79, and (f) a LCDR3 of SEQ ID NO: 77; (13) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 86, (b) a HCDR2 of SEQ ID NO: 87, (c) a HCDR3 of SEQ ID NO: 88; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 101, (e) a LCDR2 of SEQ ID NO: 102, and (f) a LCDR3 of SEQ ID NO: 103; (14) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 89, (b) a HCDR2 of SEQ ID NO: 90, (c) a HCDR3 of SEQ ID NO: 88; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 104, (e) a LCDR2 of SEQ ID NO: 105, and (f) a LCDR3 of SEQ ID NO: 106; (15) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 91, (b) a HCDR2 of SEQ ID NO: 87, (c) a HCDR3 of SEQ ID NO: 88; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 101, (e) a LCDR2 of SEQ ID NO: 102, and (f) a LCDR3 of SEQ ID NO: 103; (16) a Fab or Fab′ comprising (i) a heavy chain variable region that comprises (a) a HCDR1 of SEQ ID NO: 92, (b) a HCDR2 of SEQ ID NO: 93, (c) a HCDR3 of SEQ ID NO: 94; and (ii) a light chain variable region that comprises: (d) a LCDR1 of SEQ ID NO: 107, (e) a LCDR2 of SEQ ID NO: 105, and (f) a LCDR3 of SEQ ID NO: 103; (17) a Fab or Fab′ comprising a heavy chain variable region (VH) that comprises SEQ ID NO: 10, and a light chain variable region (VL) that comprises SEQ ID NO: 23; (18) a Fab or Fab′ comprising a VH that comprises SEQ ID NO: 36, and a VL that comprises SEQ ID NO: 47; (19) a Fab or Fab′ comprising a VH that comprises SEQ ID NO: 69, and a VL that comprises SEQ ID NO: 82; (20) a Fab or Fab′ comprising a VH that comprises SEQ ID NO: 95, and a VL that comprises SEQ ID NO: 108; (21) a Fab′ comprising a heavy chain that that comprises SEQ ID NO: 14, and a light chain that comprises SEQ ID NO: 25; (22) a Fab′ comprising a heavy chain that that comprises SEQ ID NO: 40, and a light chain that comprises SEQ ID NO: 49; (23) a Fab′ comprising a heavy chain that that comprises SEQ ID NO: 73, and a light chain that comprises SEQ ID NO: 84; (24) a Fab′ comprising a heavy chain that that comprises SEQ ID NO: 99, and a light chain that comprises SEQ ID NO:110; (25) a Fab comprising a heavy chain that comprises SEQ ID NO: 118, and a light chain that comprises SEQ ID NO: 122; (26) a Fab comprising a heavy chain that comprises SEQ ID NO: 118, and a light chain that comprises SEQ ID NO: 123; (27) a Fab comprising a heavy chain that comprises SEQ ID NO: 124, and a light chain that comprises SEQ ID NO: 128; (28) a Fab comprising a heavy chain that comprises SEQ ID NO: 124, and a light chain that comprises SEQ ID NO: 129; (29) a Fab comprising a heavy chain that comprises SEQ ID NO: 130, and a light chain that comprises SEQ ID NO: 134; (30) a Fab comprising a heavy chain that comprises SEQ ID NO: 130, and a light chain that comprises SEQ ID NO: 135; (31) a Fab comprising a heavy chain that comprises SEQ ID NO: 136, and a light chain that comprises SEQ ID NO: 140; (32) a Fab comprising a heavy chain that comprises SEQ ID NO: 141, and a light chain that comprises SEQ ID NO: 145; (33) a Fab comprising a heavy chain that comprises an amino acid sequence selected from SEQ ID NO: 119, 120 or 121, and a light chain comprising the amino acid sequence of SEQ ID NO: 25; (34) a Fab comprising a heavy chain that comprises an amino acid sequence selected from SEQ ID NO: 125, 126, or 127, and a light chain comprising the amino acid sequence
Assignees
Inventors
Classifications
Linear peptides containing at least one abnormal peptide link · CPC title
specific for leukemia · CPC title
Antineoplastic agents · CPC title
Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title
Antianaemics · CPC title
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- What does patent US11357864B2 cover?
- The present invention provides antibody drug conjugates, wherein an antibody or antibody fragment that specifically binds to human cKIT is linked to a drug moiety, optionally through a linker. The present invention further provides pharmaceutical compositions comprising the antibody drug conjugates; and methods of making and using such pharmaceutical compositions for ablating hematopoietic stem…
- Who is the assignee on this patent?
- Novartis Ag
- What technology area does this patent fall under?
- Primary CPC classification A61K47/6803. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Jun 14 2022 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 5 related publications on this page (citations in our corpus or others sharing the same primary CPC).