Methods and compositions for delivering active agents with enhanced pharmacological properties

a technology of enhancing pharmacological properties and active agents, which is applied in the direction of enzymology, peptide/protein ingredients, transferases, etc., can solve the problems of low bioavailability of active compounds, insufficient or unsatisfactory in vivo efficacy, and insufficient in vivo efficacy, so as to enhance the in vivo efficacy of active agents

Inactive Publication Date: 2013-07-04
DUKE UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0009]The present invention provides a method of enhancing in vivo efficacy of an active agent, comprising: administering to a subject an active agent that is coupled to a bioelastic polymer or elastin-like peptide, wherein the in vivo efficacy of the active agent is enhanced as compared to the same active agent when administered to the subject not coupled to (or not associated with) a bioelastic polymer or ELP. In vivo efficacy may be enhanced in one, or more, of the following ways: solubility, bioavailability, effective therapeutic dose, formulation compatibility, resistance to proteolysis, half-life of the administered peptide active therapeutic agent, persistence in the body subsequent to administration, and rate of clearance from the body subsequent to administration.

Problems solved by technology

A significant problem with many candidate drugs, or even drugs in clinical use, is insufficient or unsatisfactory in vivo efficacy.
Insufficient in vivo efficacy can be manifested in a variety of ways, such as (i) low bioavailability of the active compound; (ii) undesirably short half-life of the active compound, (iii) and / or undesirably high systemic toxicity of the active compound.

Method used

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  • Methods and compositions for delivering active agents with enhanced pharmacological properties
  • Methods and compositions for delivering active agents with enhanced pharmacological properties
  • Methods and compositions for delivering active agents with enhanced pharmacological properties

Examples

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examples

[0063]The goal of this invention is to selectively deliver drugs or imaging agents to diseased sites in order to improve therapeutic efficacy and limit systemic toxicity.

[0064]The invention has four parts:

[0065]1. Drug or Imaging Agent carriers: The carrier is a novel macromolecular drug carrier, consisting of elastin-like polypeptides (ELPs). ELPs belong to a unique class of biopolymers that undergo an inverse temperature phase transition; they are soluble at temperatures below their transition temperature (Tt) but become insoluble and aggregate at temperatures above their Tt[1-3].

[0066](i) The ELP may be designed with a Tt that is below the local temperature at the diseased site so that it will aggregate at the diseased site.

[0067](ii) Alternatively the ELP may be designed to have a Tt that is above the diseased site so as to remain in soluble form.

[0068](iii) The ELP may contain sites for the covalent or enzymatic attachment of drugs or imaging agents or targeting moieties.

[0069]...

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Abstract

Provided herein are methods of enhancing in vivo efficacy of an active agent, comprising: administering to a subject an active agent that is coupled to a bioelastic polymer or elastin-like peptide, wherein the in vivo efficacy of the active agent is enhanced as compared to the same active agent when administered to the subject not coupled to (or not associated with) a bioelastic polymer or ELP.

Description

PRIORITY[0001]This application is a continuation-in-part of U.S. patent application Ser. No. 13 / 674,285, filed Nov. 12, 2012, which is a continuation of Ser. No. 12 / 158,190, filed Sep. 2, 2008 (now U.S. Pat. No. 8,334,257), which is a national phase application of PCT Application No. PCT / US2006 / 048572, filed Dec. 20, 2006, and published in English on Jun. 28, 2007, as International Publication No. WO 2007 / 073486, and which claims the benefit of U.S. Provisional Patent Application Ser. No. 60 / 751,896, filed Dec. 20, 2005, the disclosure of each of which is incorporated by reference herein in its entirety.GOVERNMENT FUNDING[0002]This invention was made with Government support under grant number EB00188 and GM-061232 from the National Institutes of Health. The US Government has certain rights to this invention.DESCRIPTION OF THE TEXT FILE SUBMITTED ELECTRONICALLY[0003]The contents of the text file submitted electronically herewith are incorporated herein by reference in their entirety:...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K47/48A61K38/08A61K38/095
CPCA61K47/48292A61K47/64A61K47/6435A61K31/704A61K38/08A61K38/10A61K38/16A61K38/17A61K38/1709A61K38/22A61K38/2264A61K38/2271A61K38/23A61K38/44A61K38/45C12Y113/12007C12Y203/01028C12Y203/02013A61K38/095A61K39/44A61K49/0056A61K49/14A61K2039/505C07K2319/31
Inventor CHILKOTI, ASHUTOSH
Owner DUKE UNIV
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