Enhanced Polyethylene Glycol-Linker-Drug Conjugate with Improved Stability, Solubility, and Bioavailability
Legal Citation
Summary of the Inventive Concept
The present disclosure relates to an improved polyethylene glycol-linker-drug conjugate, comprising a novel linker compound that enhances the stability, solubility, and bioavailability of the conjugate, and its preparation, pharmaceutical composition, and application.
Background and Problem Solved
The original patent disclosed a polyethylene glycol-linker-drug conjugate, which had limitations in terms of stability, solubility, and bioavailability. The present inventive concept addresses these limitations by introducing a novel linker compound that reduces the immunogenicity of the conjugate, improves its pharmacokinetics, and enhances its bioavailability.
Detailed Description of the Inventive Concept
The novel linker compound X is designed to enhance the stability and solubility of the conjugate, and is synthesized using a click chemistry approach. The linker compound L is modified to reduce the immunogenicity of the conjugate, and the drug moiety D is a protein or polypeptide drug. The pharmaceutical composition comprising the conjugate has improved pharmacokinetics and bioavailability, and the system for delivering the conjugate targets specific cells or tissues, resulting in improved efficacy and reduced side effects.
Novelty and Inventive Step
The novelty of the present inventive concept lies in the introduction of a novel linker compound X that reduces the immunogenicity of the conjugate, improves its pharmacokinetics, and enhances its bioavailability. The inventive step is the combination of the novel linker compound with the polyethylene glycol-linker-drug conjugate, resulting in a conjugate with improved stability, solubility, and bioavailability.
Alternative Embodiments and Variations
Alternative embodiments of the inventive concept include varying the structure of the linker compound X, modifying the drug moiety D, or using different polyethylene glycol residues. Variations of the pharmaceutical composition and system for delivering the conjugate could also be explored.
Potential Commercial Applications and Market
The enhanced polyethylene glycol-linker-drug conjugate has potential commercial applications in the pharmaceutical industry, particularly in the development of targeted therapies for various diseases. The market for such conjugates is expected to grow, driven by the need for more effective and safer treatments.
CPC Classifications
| Section | Class | Group |
|---|---|---|
| A | A61 | A61K47/60 |
| A | A61 | A61K31/704 |
| A | A61 | A61P35/00 |
Section 103 Obviousness Analysis (PHOSITA)
Field of Art
Pharmaceutical biotechnology, specifically drug delivery systems involving polyethylene glycol (PEG) conjugates, with expertise in chemical modification of therapeutic molecules and drug delivery strategies
Person of Ordinary Skill (PHOSITA) Profile
A skilled practitioner with advanced degrees in chemistry or pharmaceutical sciences, familiar with polymer chemistry, conjugation techniques, and drug delivery system design, capable of understanding complex molecular modifications and their potential impacts on drug performance
Obviousness Rationale
A person of ordinary skill would recognize that the PTD represents predictable variations on the source patent's core PEG-linker-drug conjugate technology. The disclosed modifications of linker compounds, click chemistry synthesis, and targeted delivery are logical extensions of existing pharmaceutical conjugation strategies. The technical improvements in stability, solubility, and bioavailability represent incremental advancements that would be expected through routine optimization by a skilled practitioner.
Obvious Combinations & Variations
Original Patent Information
| Patent Number | US 11,857,635 |
|---|---|
| Title | Linker compound, polyethylene glycol-linker conjugate and derivative thereof and polyethylene glycol-linker-drug conjugate |
| Assignee(s) | JenKem Technology Co., Ltd. (Tianjin) |