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US 12,721,897 B2Granted
Pharmaceutical compositions of polypeptide conjugates and methods of uses thereof
AssigneeBeijing Ql Biopharmaceutical Co., Ltd.
InventorsYuanyuan Zhang, Hongyu Shi, Xiaona Dong, Peng Zhai, Hongzhou Dong
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Abstract
The present disclosure provides polypeptide conjugates comprising GLP-1 receptor agonist and a peptide linker, and pharmaceutical compositions comprising the same. Methods of using such for treating diseases are also provided.
Claims9
A pharmaceutical composition comprising a polypeptide conjugate and an absorption enhancing excipient, wherein:
- the polypeptide conjugate comprises a polypeptide portion and one clearance-reducing moiety (CRM) conjugated to a lysine (K) residue on the polypeptide portion, wherein the polypeptide portion comprises the amino acid sequence of SEQ ID NO:
- 52, 55, 56, 60, 61, or 62:
- wherein the CRM has the structure of below formula:
- wherein “*” represents the point of attachment to a reactive group of the lysine residue on the polypeptide portion:
- wherein the absorption enhancing excipient comprises sodium N-(8-(2-hydroxybenzoyl) amino) caprylic acid (SNAC);
- and
- wherein the pharmaceutical composition is a unit dosage form comprising approximately 0.5-50 mg of the polypeptide conjugate, approximately 50-300 mg of SNAC, and approximately 1-10 mg magnesium stearate.
4 more elements
A pharmaceutical composition comprising a polypeptide conjugate and an absorption enhancing excipient, wherein:
- the polypeptide conjugate comprises a polypeptide portion and two clearance-reducing moieties (CRM) conjugated to lysine (K) residues on the polypeptide portion, wherein the polypeptide portion comprises the amino acid sequence of SEQ ID NO:
- 51, 53, 54, 57, 58, 59, 85, or 86;
- wherein the CRM has the structure of below formula:
- wherein “*” represents the point of attachment to a reactive group of the lysine residue on the polypeptide portion:
- wherein the absorption enhancing excipient comprises SNAC;
- and
- wherein the pharmaceutical composition is a unit dosage form comprising approximately 10-100 mg of the polypeptide conjugate, approximately 100-500 mg of SNAC, and approximately 1-20 mg magnesium stearate.
4 more elements
Dependencies are inferred from the claim text.