Reversible Binding Moiety Prodrug Complexes for Controlled Drug Release

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Solution Overview

Problem

Current drug administration methods, such as divided doses and IV infusions, often lead to adverse effects like cytokine release syndrome, which can be severe and life-threatening, and are burdensome for patients and the healthcare system, necessitating improved approaches to mitigate these issues.

Innovation Solution

Development of slow-release compositions, or prodrug complexes, where a binding moiety reversibly binds to a drug molecule, inhibiting its biological activity and allowing gradual release over time, reducing peak concentrations and minimizing adverse effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If divided doses or IV infusions are used to mitigate adverse effects, then safety is improved, but patient compliance deteriorates and treatment complexity increases

Engineering Contradiction:
ImprovesafetyVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent segments the drug delivery process by using a binding moiety that temporarily complexes with the drug molecule, releasing it in controlled portions over time rather than all at once. This segmentation of drug release mimics the effect of divided doses while using a single administration event, thereby improving patient compliance without sacrificing safety.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The binding moiety is pre-complexed with the drug molecule before administration, creating a prodrug complex that inherently controls release kinetics. This preliminary action of complex formation ensures that the drug is delivered in a controlled manner from the start, eliminating the need for multiple dosing events or infusion protocols while maintaining safety.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If divided doses are administered to reduce adverse effects, then safety is improved, but treatment duration and healthcare system strain increase

Engineering Contradiction:
ImprovesafetyVSAvoidtreatment duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The binding moiety provides continuous drug release over an extended period through a single administration event. The controlled dissociation of the drug from the binding moiety maintains therapeutic levels continuously, eliminating the gaps and repetitions associated with divided dosing schedules, thereby reducing overall treatment duration and healthcare system strain.

Inventive Principle:
Principle #20Continuity of useful action

3Quantity of substance

If high concentration of drug is administered to achieve efficacy, then therapeutic effect is improved, but adverse effects worsen

Engineering Contradiction:
Improvedrug concentrationVSAvoidadverse effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent employs dynamic control of drug concentration through the binding moiety, which maintains the drug in a complexed, inactive state during circulation and only allows gradual release at the target site or over time. This dynamic regulation ensures high local efficacy while preventing systemic peak concentrations that cause adverse effects.

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The binding moiety acts as an intermediary between the drug molecule and the biological system. It temporarily sequesters the drug, preventing premature or excessive interaction with biological targets, and facilitates controlled delivery. This intermediary role allows high drug quantities to be administered safely by buffering the release kinetics.

Inventive Principle:
Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The slow release of active drug molecules through prodrug complexes minimizes adverse effects and reduces the risk of severe reactions, improving patient compliance and treatment outcomes while reducing the strain on healthcare systems.

Implementation Method 1

a binding moiety reversibly binds to a drug molecule to form a prodrug complex that slowly releases the drug molecule

Methodology Applied
Scientific EffectReversible binding: Adsorption

Data Source

PatentUS20240108746A1Novel slow-release prodrugs
Publication Date: 2024.04.04 MOLECULAR PARTNERS AG
  • US20240108746A1 patent drawing
  • US20240108746A1 patent drawing
  • US20240108746A1 patent drawing

AI summary

The present invention relates to compositions comprising a binding moiety and a drug molecule, wherein said binding moiety reversibly binds to said drug molecule to form a prodrug complex that slowly releases the drug molecule upon administration in vivo. The present invention further relates to methods of forming such compositions and to methods of treatment using such compositions. Also described are binding moieties, nucleic acids encoding said binding moieties and methods of making these using host cells.