US 2026/0284216 A1 · IMMUNOCONJUGATES CONTAINING TNF-ALPHA AND RELATED METHODS AND COMPOSITIONS THEREOF

Abstract

Provided herein are immunoconjugate molecules containing a TNF-α polypeptide and a masking moiety capable of inhibiting and activating the TNF-α activity under suitable conditions. Also provided herein are methods for producing the immunoconjugate molecules. Finally, provided herein are the therapeutic uses of the immunoconjugate molecules due to their modulating effects on the immune system for treating diseases such as cancer and other chronic infectious diseases.

Claims90

Dependent claims

A two-in-one antibody or antigen-binding fragment thereof that binds to TNF-α and FAP, wherein the antibody or antigen-binding fragment thereof comprises:

(a) a light chain variable region (VL) comprising VL complementarity determining region 1 (CDR1), VL CDR2, and VL CDR3 of antibody FN15 as set forth in Table 15;
and/or a heavy chain variable region (VH) comprising VH complementarity determining region 1 (CDR1), VH CDR2, and VH CDR3 of antibody FN15 as set forth in Table 16;
or
(b) a VL comprising a VL CDR1, a VL CDR2, and a VL CDR3 having an amino acid sequence of a VL CDR1, a VL CDR2, and a VL CDR3, respectively, of a VL having an amino acid sequence of SEQ ID NO:27;
and/or a VH comprising a VH CDR1, a VH CDR2, and a VH CDR3 having an amino acid sequence of a VH CDR1, a VH CDR2, and a VH CDR3, respectively, of a VH having an amino acid sequence of SEQ ID NO:28.

2 more elements

An immunoconjugate molecule comprising a first polypeptide chain and a second polypeptide chain, wherein the first polypeptide chain comprises a TNF-α moiety fused to a heavy chain variable region (VH) of a first antibody, wherein the second polypeptide chain comprises a light chain variable region (VL) of the first antibody fused to a second antibody capable of binding to FAP;

and wherein the VH and VL forms a two-in-one binding domain capable of binding to TNF-α and FAP.

A two-in-one antibody or antigen-binding fragment thereof that binds to TNF-α and Trop-2, wherein the antibody or antigen-binding fragment thereof comprises:

(a) a light chain variable region (VL) comprising VL complementarity determining region 1 (CDR1), VL CDR2, and VL CDR3 of antibody TN01 as set forth in Table 19;
and/or a heavy chain variable region (VH) comprising VH complementarity determining region 1 (CDR1), VH CDR2, and VH CDR3 of antibody TN01 as set forth in Table 20;
or
(b) a VL comprising a VL CDR1, a VL CDR2, and a VL CDR3 having an amino acid sequence of a VL CDR1, a VL CDR2, and a VL CDR3, respectively, of a VL having an amino acid sequence of SEQ ID NO:29;
and/or a VH comprising a VH CDR1, a VH CDR2, and a VH CDR3 having an amino acid sequence of a VH CDR1, a VH CDR2, and a VH CDR3, respectively, of a VH having an amino acid sequence of SEQ ID NO:30.

2 more elements

and wherein the VH and VL forms a two-in-one binding domain capable of binding to TNF-α and Trop-2.

Dependencies are inferred from the claim text.

Facts

Application

19/469,641Filed 27 Mar 2024

Priority

WO PCT/CN2023/08411227 Mar 2023

Published

24 Sep 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification26 codes

A61K 47/6813
The drug being a protein or peptide, e.g. transferrin or bleomycin: the drug being a peptidic cytokine, e.g. an interleukin or interferon
A61K 39/3955
Against materials from animals: against proteinaceous materials, e.g. enzymes, hormones, lymphokines
A61K 39/39558
Against materials from animals: against tumor tissues, cells, antigens
A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…

Abstract

Claims90

Dependent claims

A two-in-one antibody or antigen-binding fragment thereof that binds to TNF-α and FAP, wherein the antibody or antigen-binding fragment thereof comprises:

(a) a light chain variable region (VL) comprising VL complementarity determining region 1 (CDR1), VL CDR2, and VL CDR3 of antibody FN15 as set forth in Table 15;
and/or a heavy chain variable region (VH) comprising VH complementarity determining region 1 (CDR1), VH CDR2, and VH CDR3 of antibody FN15 as set forth in Table 16;
or
(b) a VL comprising a VL CDR1, a VL CDR2, and a VL CDR3 having an amino acid sequence of a VL CDR1, a VL CDR2, and a VL CDR3, respectively, of a VL having an amino acid sequence of SEQ ID NO:27;
and/or a VH comprising a VH CDR1, a VH CDR2, and a VH CDR3 having an amino acid sequence of a VH CDR1, a VH CDR2, and a VH CDR3, respectively, of a VH having an amino acid sequence of SEQ ID NO:28.

2 more elements

and wherein the VH and VL forms a two-in-one binding domain capable of binding to TNF-α and FAP.

A two-in-one antibody or antigen-binding fragment thereof that binds to TNF-α and Trop-2, wherein the antibody or antigen-binding fragment thereof comprises:

(a) a light chain variable region (VL) comprising VL complementarity determining region 1 (CDR1), VL CDR2, and VL CDR3 of antibody TN01 as set forth in Table 19;
and/or a heavy chain variable region (VH) comprising VH complementarity determining region 1 (CDR1), VH CDR2, and VH CDR3 of antibody TN01 as set forth in Table 20;
or
(b) a VL comprising a VL CDR1, a VL CDR2, and a VL CDR3 having an amino acid sequence of a VL CDR1, a VL CDR2, and a VL CDR3, respectively, of a VL having an amino acid sequence of SEQ ID NO:29;
and/or a VH comprising a VH CDR1, a VH CDR2, and a VH CDR3 having an amino acid sequence of a VH CDR1, a VH CDR2, and a VH CDR3, respectively, of a VH having an amino acid sequence of SEQ ID NO:30.

2 more elements

and wherein the VH and VL forms a two-in-one binding domain capable of binding to TNF-α and Trop-2.

Dependencies are inferred from the claim text.

Immunoconjugates containing tnf-alpha and related methods and compositions thereof

Life of this patent

Abstract

Claims90

Immunoconjugates containing tnf-alpha and related methods and compositions thereof

Life of this patent

Abstract

Claims90