Modified therapeutic agents and compositions thereof
AssigneeThe Scripps Research Institute
InventorsWeijun SHEN, Pengyu YANG, Peter G. SCHULTZ
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Abstract
Methods and compositions are provided for extending the half-life of a therapeutic agent. A modified therapeutic agent (mTA) comprises a therapeutic agent, a staple, and a half-life extending molecule. The mTAs disclosed herein may be used to treat a disease or a condition in a subject in need thereof.
Claims21
1-41. (canceled)
A modified therapeutic agent (mTA) of Formula (I):
- wherein:
- TA is a therapeutic agent, wherein the therapeutic agent is a single peptide comprising an amino acid sequence that is at least 95% homologous to any one of SEQ ID NO:
- 7 and 12-30;
- Q is
- A1 is
- P1 is PEG-A2;
- wherein:
- PEG is
- m and n are each 1, 2, 3, or 4;
- and
- A2 is
- L is a lipid derivative selected from a group consisting of sterols, bile acids, vitamin E, fatty di-acids, fatty acids, fatty amides, fatty amines, and fatty alcohols;
- a is 1;
- and
- b is 1;
- wherein the TA is covalently attached to Q via two amine-containing sidechain amino acids on the single peptide;
- and wherein the two amine-containing sidechain amino acids are at least two amino acids apart, and less than 20 amino acids apart.
A modified therapeutic agent (mTA) comprising (i) a therapeutic agent, (ii) a half-life extending molecule, and (iii) a staple, wherein:
- (i) the therapeutic agent is a single peptide chain having an amino acid sequence that is at least 95% homologousto any one of SEQ ID NOs:
- 7 and 12-30 that is covalently attached to the staple via two amine-containing sidechain amino acids on the single peptide chain;
- and
- wherein the two amine-containing sidechain amino acids are at least two amino acids apart, and less than 20 amino acids apart;
- (ii) the half-life extending molecule is covalently attached to the first staple;
- and
- (iii) the staple has the following structure:
A modified therapeutic agent (mTA) comprising (i) a therapeutic agent, (ii) a half-life extending molecule, and (iii) a staple, wherein:
- (i) the therapeutic agent is a single peptide GLP-1R/GCGR/GIPR tri-agonist that is covalently attached to the staple via two amine-containing sidechain amino acids on the single peptide;
- wherein the two amine-containing sidechain amino acids are at least two amino acids apart, and less than 20 amino acids apart;
- (ii) the half-life extending molecule is covalently attached to the first staple;
- and
- (iii) the staple has the following structure:
Dependencies are inferred from the claim text.