IP Library Granted Patent US 12,458,705
Granted Patent B2
US 12,458,705 · App. 17/251,316 · Granted Nov 4, 2025

Antibody-oligonucleotide conjugates

Inventors: Paul A. Jaminet (Cambridge, MA); Shou-Ching S. Jaminet (Cambridge, MA); Edward Ha (Cambridge, MA)
Assignee: ANGIEX, INC.
A61K47/6807A61K45/06A61K47/6849A61K47/6855A61P35/00C07K16/28C07K19/00C12N15/113C12N15/1135C12N15/1137C12N15/1138C07K2317/55C12N2310/11C12N2310/14C12N2310/141C12N2310/3513C12N2320/32
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Quick Facts
Patent No.
US 12,458,705
App. No.
17/251,316
Granted
Nov 4, 2025
Kind
B2
Abstract

Conjugates are provided, comprising a targeting protein, e.g., an anti-TM4SFI antibody or antigen or binding fragments thereof. Methods of manufacture and use of said conjugates are also described.

Claims (21)

1 . A conjugate comprising an anti-TM4SF 1 antibody or an antigen binding fragment thereof conjugated to an oligonucleotide,

(1) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 94, 95, and 96, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 97, 98, and 99, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 92 and a light chain sequence of SEQ ID NO.: 93;

(2) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 1 and a light chain sequence of SEQ ID NO.: 2;

(3) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 6, 7, and 8, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 12, 13, and 14, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 3 and a light chain sequence of SEQ ID NO.: 9;

(4) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 18, 19, and 20, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 24, 25, and 26, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 15 and a light chain sequence of SEQ ID NO.: 21;

(5) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 30, 31, and 32, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 36, 37, and 38, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 27 and a light chain sequence of SEQ ID NO.: 33;

(6) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 54, 55, and 56, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 60, 61, and 62, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 51 and a light chain sequence of SEQ ID NO.: 57;

(7) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 66, 67, and 68, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 72, 73, and 74, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 63 and a light chain sequence of SEQ ID NO.: 69;

(8) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 78, 79, and 80, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 84, 85, and 86, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 75 and a light chain sequence of SEQ ID NO.: 81; or

(9) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 42, 43, and 44, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 48, 49, and 50, respectively, the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 39 and a light chain sequence of SEQ ID NO.: 45.

2 . The conjugate of claim 1 , wherein the oligonucleotide comprises a DNA molecule or an RNA molecule.

3 . The conjugate of claim 2 , wherein the oligonucleotide comprises the RNA molecule, and wherein the oligonucleotide comprises an antisense oligonucleotide, an siRNA, an antisense RNA, an miRNA, an antisense miRNA, an antagomir (anti-miRNA), an shiRNA, or an mRNA.

4 . The conjugate of claim 2 , wherein the oligonucleotide comprises the DNA molecule, and wherein the oligonucleotide comprises a modified DNA, a triple helical DNA, a supercoiled DNA, a Z-DNA, or any combinations thereof.

5 . The conjugate of claim 3 , wherein the oligonucleotide comprises the siRNA comprising a trinucleotide repeat.

6 . The conjugate of claim 5 , wherein the siRNA is a CAG/CUG trinucleotide repeat based siRNA.

7 . A composition comprising a conjugate according to claim 1 in combination with an antibody-drug conjugate.

8 . The composition of claim 7 , wherein the antibody-drug conjugate comprises a cytotoxic payload.

9 . The composition of claim 8 , wherein the cytotoxic payload comprises a V-ATPase inhibitor, a pro-apoptotic agent, a Bcl2 inhibitor, an MCL1 inhibitor, a HSP90 inhibitor, an 1AP inhibitor, an mTor inhibitor, a microtubule stabilizer, a microtubule destabilizer, an auri statin, a dolastatin, a maytansinoid, a MetAP (methionine aminopeptidase), an inhibitor of nuclear export of proteins CRM1, a DPPIV inhibitor, proteasome inhibitors, inhibitors of phosphoryl transfer reactions in mitochondria, a protein synthesis inhibitor, a kinase inhibitor, a CDK2 inhibitor, a CDK9 inhibitor, a kinesin inhibitor, an HD AC inhibitor, a DNA damaging agent, a DNA alkylating agent, a DNA intercalator a DNA minor groove binder, a DHFR inhibitor, a nucleic acid, or a CRISPR enzyme.

10 . The composition of claim 7 , wherein the antibody-drug conjugate comprises an anti-TM4SF 1 antibody or an antigen binding fragment thereof.

11 . The conjugate of claim 3 , wherein the oligonucleotide hybridizes with a polynucleotide encoding an inhibitor of p53.

12 . The conjugate of claim 3 , wherein the oligonucleotide hybridizes with a polynucleotide encoding an apoptosis inhibitor.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2021
From: JAMINET, PAUL A.; JAMINET, SHOU-CHING S.; HA, EDWARD
To: ANGIEX, INC.
Reel/Frame 055269/0499 →
Continuity (2)
Provisional Application 62684131 · Jun 12, 2018
Related Publication 20210260209A1 · Aug 26, 2021
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