Pharmaceutical composition of humanized monoclonal anti-PD-L1 antibody

Patent metadata

Field	Value
Publication number	US-12150990-B2
Application number	US-201816756409-A
Country	US
Kind code	B2
Filing date	Nov 2, 2018
Priority date	Nov 2, 2017
Publication date	Nov 26, 2024
Grant date	Nov 26, 2024

Abstract

The invention is in the field of antibody formulations, and particularly relates to a pharmaceutical composition of a humanized monoclonal anti-PD-L1 antibody, wherein the pharmaceutical composition comprises 1-150 mg/ml of the humanized monoclonal anti-PD-L1 antibody, a buffer at 3-50 mM, 2-150 mg/ml of an isotonic adjuster/stabilizer and 0.01-0.8 mg/ml of a surfactant, and has a pH of about 4.5-6.8. The formulations prevent antibody aggregates therein from increasing, while enabling better maintenance of the biological binding activity of the antibody for a long time.

First claim

The invention claimed is:

1. A pharmaceutical composition of humanized monoclonal anti-PD-L1 antibody, comprising:
(a) the humanized monoclonal anti-PD-L1 antibody at a mass concentration of 10 mg/mL,
(b) sucrose at a mass concentration of 80 mg/mL,
(c) polysorbate-80 at a mass concentration of 0.2 mg/ml,
(d) histidine at a molar concentration of 10 mM, and
(e) hydrochloric acid in an appropriate amount, for adjusting the pH of the composition to 5.5, wherein the humanized monoclonal anti-PD-L1 antibody comprises heavy chains CDR1, CDR2, and CDR3 having the amino acid sequences shown in SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3, respectively, and light chains CDR1, CDR2, and CDR3 having the amino acid sequences shown in SEQ ID NO: 7, SEQ ID NO: 8, and SEQ ID NO: 9, respectively.

2. A pharmaceutical composition of humanized monoclonal anti-PD-L1 antibody, comprising:
(a) the humanized monoclonal anti-PD-L1 antibody at a mass concentration of 30 mg/mL,
(b) sucrose at a mass concentration of 80 mg/mL,
(c) polysorbate-80 at a mass concentration of 0.2 mg/ml,
(d) histidine at a molar concentration of 10 mM, and
(e) hydrochloric acid in an appropriate amount, for adjusting the pH of the composition to 5.5, wherein the humanized monoclonal anti-PD-L1 antibody comprises heavy chains CDR1, CDR2, and CDR3 having the amino acid sequences shown in SEQ ID NO: 1, SEQ ID NO: 2, and SEQ ID NO: 3, respectively, and light chains CDR1, CDR2, and CDR3 having the amino acid sequences shown in SEQ ID NO: 7, SEQ ID NO: 8, and SEQ ID NO: 9, respectively.

3. The pharmaceutical composition of claim 2 , wherein the humanized monoclonal anti-PD-L1 antibody comprises the amino acid sequence as follows:
a heavy chain variable region as shown in SEQ ID NO: 13; a light chain variable region as shown in SEQ ID NO: 15.

4. The pharmaceutical composition of claim 2 , wherein the humanized monoclonal anti-PD-L1 antibody comprises the heavy chain amino acid sequence as shown in SEQ ID NO: 17, and the light chain amino acid sequence as shown in SEQ ID NO: 18.

5. The pharmaceutical composition of claim 1 , wherein the humanized monoclonal anti-PD-L1 antibody comprises the amino acid sequence as follows: a heavy chain variable region as shown in SEQ ID NO: 13; a light chain variable region as shown in SEQ ID NO: 15.

6. The pharmaceutical composition of claim 1 , wherein the humanized monoclonal anti-PD-L1 antibody comprises the heavy chain amino acid sequence as shown in SEQ ID NO: 17, and the light chain amino acid sequence as shown in SEQ ID NO: 18.

Assignees

• Nanjing Shunxin Pharmaceutical Co Ltd
• Chia Tai Tianqing Pharmaceutical Group Co Ltd

Inventors

• Li Jianwen
• Cheng Yanju
• Li Yingchun
• Zhao Wei
• Zhang Xiquan

Classifications

• C07K2317/24

  containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered · CPC title

• C07K16/2827 Primary

  against B7 molecules, e.g. CD80, CD86 · CPC title

• A61K2039/545

  characterised by the dose, timing or administration schedule · CPC title

• A61K2039/505

  comprising antibodies · CPC title

• A61K47/26

  Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin · CPC title