Granted Patent B2

US 12,564,642 · App. 17/522,443 · Granted Mar 3, 2026

Inventors: Jean-René Authelin (Paris, FR); Fethi Bensaid (Paris, FR); Audrey Bonestebe (Paris, FR); Sylvain Huille (Paris, FR); Marie Leman (Paris, FR); Lucie Manache-Alberici (Paris, FR)

Assignee: SANOFI

A61K47/6849A61K47/68033A61K47/6853A61P35/00C07K16/2818C07K16/2827C07K16/3023A61K2039/505A61K2039/545

Abstract

Claims (29)

1 . A liquid pharmaceutical formulation comprising:

an antibody-drug conjugate (ADC) comprising an anti-human carcinoembryonic antigen-related cell adhesion molecule 5 (hCEACAM5) antibody conjugated to a maytansinoid derivative 4 (DM4) by a N-succinimidyl-4-(2-pyridyldithio) butanoic acid (SPDB) linker conjugate; wherein the antibody comprises a variable heavy (VH) domain of amino acid sequence of SEQ ID NO:6 and a variable light (VL) domain of amino acid sequence of SEQ ID NO: 7, at a concentration of about 5 mg/mL;

the formulation consisting of the following excipients:

i) sodium acetate at a concentration of about 10 mM;

ii) sorbitol at a concentration of about 5% w/v,

iii) polysorbate 80 at a concentration of about 0.04% w/v; and

iv) disodium EDTA at a concentration of between about 1 μM and about 50 μM, wherein the formulation has a pH of about 5.5.

2 . The pharmaceutical formulation of claim 1 , wherein the disodium EDTA is at a concentration of about 1 μM, about 10 μM or about 50 μM.

3 . The pharmaceutical formulation of claim 1 , wherein the antibody-drug conjugate has a drug-to-conjugate ratio ranging from about 1 to about 10, from about 2 to about 5, or from about 3 to about 4.

4 . A method of treating a cancer, comprising administering to a subject in need thereof an effective amount of a pharmaceutical formulation comprising:

an antibody-drug conjugate (ADC) comprising an anti-human carcinoembryonic antigen-related cell adhesion molecule 5 (hCEACAM5) antibody bound to a maytansinoid derivative 4 (DM4) by a N-succinimidyl-4-(2-pyridyldithio) butanoic acid (SPDB) linker; wherein the antibody comprises a variable heavy (VH) domain of amino acid sequence of SEQ ID NO: 6 and a variable light (VL) domain of amino acid sequence of SEQ ID NO:7;

the formulation consisting of the following excipients:

i) sodium acetate at a concentration of about 10 mM;

ii) sorbitol at a concentration of about 5% w/v;

iii) polysorbate 80 at a concentration of about 0.04% w/v; and

iv) disodium EDTA at a concentration of between about 1 μM and about 50 μM;

wherein the formulation has a pH of about 5.5.

5 . The method according to claim 4 , wherein the cancer is a high carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5) expressing cancer.

6 . The method according to claim 4 , wherein the cancer is selected from the group consisting of colorectal, gastric, lung, breast, prostate, ovarian, cervical, pancreatic and bladder cancer.

7 . The method according to claim 4 , wherein the cancer expresses carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5).

8 . The method according to claim 4 , wherein the cancer is selected from the group consisting of pancreatic and prostate cancer.

9 . A liquid pharmaceutical formulation consisting of:

i) 5 mg/mL anti-human carcinoembryonic antigen-related cell adhesion molecule 5 (hCEACAM5) antibody-drug conjugate (ADC);

ii) sodium acetate at a concentration of 10 mM;

iii) sorbitol at a concentration of 5% w/v;

iv) polysorbate 80 at a concentration of 0.04% w/v; and

v) disodium EDTA at a concentration of 10 μM;

wherein the liquid dosage form has a pH of 5.5, and

wherein the ADC consists of huMAb2-3-SPDB-DM4.

Assignments (2)

Priority Claims (1)

Continuity (1)

References Cited (400)