US 12,753,242 B2Granted

Antibody conjugates and uses thereof

AssigneeGlycoNex Inc.

InventorsTong-Hsuan Chang, Mei-Chun Yang, Liahng-Yirn Liu, Jerry Ting, Shu-Yen Chang, Yen-Ying Chen, Yu-Yu Lin, Shu-Lun Tang

Life of this patent

Estimating the term…

patentgrep

Loading patent…

Abstract

Disclosed herein are humanized antibodies, antigen-binding fragments thereof, and antibody conjugates, that are capable of specifically binding to certain biantennary Lewis antigens, which antigens are expressed in a variety of cancers. The presently disclosed antibodies are useful to target antigen-expressing cells for treatment or detection of disease, including various cancers. Also provided are polynucleotides, vectors, and host cells for producing the disclosed antibodies and antigen-binding fragments thereof. Pharmaceutical compositions, methods of treatment and detection, and uses of the antibodies, antigen-binding fragments, antibody conjugates, and compositions are also provided.

Claims26

Dependent claims

An antibody conjugate comprising an isolated antibody or antigen-binding fragment thereof, and a payload molecule covalently linked by a cleavable linker to the isolated antibody or antigen-binding fragment thereof,

wherein the cleavable linker is a protease-sensitive linker comprising a valine-citrulline dipeptide, and the payload molecule is a therapeutic agent, a detectable indicator, or a combination thereof,
wherein the isolated antibody or antigen-binding fragment thereof comprises:
(a) an immunoglobulin heavy chain variable region (VH) comprising
a complementarity determining region 1 (VH CDR1) comprising the amino acid sequence set forth in SEQ ID NO:
2 or a variant thereof, wherein the variant consists of a Y to A substitution at position 33 of SEQ ID NO:
35,
a complementarity determining region 2 (VH CDR2) comprising the amino acid sequence set forth in SEQ ID NO:
3 or a variant thereof, wherein the variant consists of a T to S substitution at position 55 of SEQ ID NO:
35,
a complementarity determining region 3 (VH CDR3) comprising the amino acid sequence set forth in SEQ ID NO:
4 or a variant thereof, wherein the variant consists of a Y to A substitution at position 104 of SEQ ID NO:
35, a A to H substitution at position 106 of SEQ ID NO:
35, or both;
and
(b) an immunoglobulin light chain variable region (VL) comprising
a complementarity determining region 1 (VL CDR1) comprising the amino acid sequence set forth in SEQ ID NO:
6 or a variant thereof, wherein the variant consists of a Y to A substitution at position 30 of SEQ ID NO:
5,
a complementarity determining region 2 (VL CDR2) comprising the amino acid sequence set forth in SEQ ID NO:
7 or a variant thereof, wherein the variant consists of a G to A substitution at position 50 of SEQ ID NO:
5, and
a complementarity determining region 3 (VL CDR3) comprising the amino acid sequence set forth in SEQ ID NO:
8 or a variant thereof, wherein the variant consists of a T to S substitution at position 93 of SEQ ID NO:
5.

21 more elements

An antibody conjugate comprising an isolated antibody or antigen-binding fragment thereof linked to a payload molecule by a cleavable linker, wherein:

(i) the isolated antibody or antigen-binding fragment thereof comprises:
(a) in an immunoglobulin heavy chain variable region, a complementarity determining region 1 (VH CDR1) comprising the amino acid sequence set forth in SEQ ID NO:
2 or a variant thereof, wherein the variant consists of a Y to A substitution at position 33 of SEQ ID NO:
35, a VH CDR2 comprising the amino acid sequence set forth in SEQ ID NO:
3 or a variant thereof, wherein the variant consists of a T to S substitution at position 55 of SEQ ID NO:
35, a VH CDR3 comprising the amino acid sequence set forth in SEQ ID NO:
4 or a variant thereof, wherein the variant consists of a Y to A substitution at position 104 of SEQ ID NO:
35, a A to H substitution at position 106 of SEQ ID NO:
35, or both;
(b) in an immunoglobulin light chain variable region (VL), a complementarity determining region 1 (VL CDR1) comprising the amino acid sequence set forth in SEQ ID NO:
6 or a variant thereof, wherein the variant consists of a Y to A substitution at position 30 of SEQ ID NO:
5, a VL CDR2 comprising the amino acid sequence set forth in SEQ ID NO:
7 or a variant thereof, wherein the variant consists of a G to A substitution at position 50 of SEQ ID NO:
5, and a VL CDR3 comprising the amino acid sequence set forth in SEQ ID NO:
8 or a variant thereof, wherein the variant consists of a T to S substitution at position 93 of SEQ ID NO:
5, and
(c) means for coupling to the linker:
(ii) the cleavable linker is a protease-sensitive linker comprising a valine-citrulline dipeptide;
and
(iii) the payload molecule is a therapeutic agent.

17 more elements

Dependencies are inferred from the claim text.

Facts

Application: 18/175,905Filed 28 Feb 2023 · division
Priority: 31 May 2018
Published: US 2024/0067746 A129 Feb 2024
Granted: 6 Oct 2026
Term ends: Not estimatedThe source records don’t support an estimate.

Classification11 codes

C07K 16/2896
Against receptors, cell surface antigens or cell surface determinants: against molecules with a "CD"-designation, not provided for elsewhere
A61K 47/65
The modifying agent being a protein, peptide or polyamino acid: peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/6801
The modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment: drug-antibody or immunoglobulin conjugates…
A61K 49/0058
Characterised by the carrier molecule carrying the fluorescent agent: antibodies

Family

Application62/678,890Us provisional application · filed 31 May 2018
Application16/427,146Parent of this division · filed 30 May 2019
Application17/815,117Parent of this division · filed 26 Jul 2022
US 11,440,967 B2Parent of this division · filed 13 Sep 2022
US 11,643,471 B2Parent of this division · filed 9 May 2023
US 2024/0067746 A1Pre-grant publication · published 29 Feb 2024
US 2019/0367632 A1Published application
US 2022/0403042 A1Published application
US 12,753,242 B2This patent

From the US filing history. Foreign family members aren’t listed.