Enhanced Polyethylene Glycol-Linker-Drug Conjugate with Improved Stability, Solubility, and Bioavailability

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.

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.

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.

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 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.

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.