High-Concentration Subcutaneous Brain-Targeting Antibody Formulations
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Solution Overview
Problem
Traditional intravenous (IV) therapeutics are associated with longer administration times, increased healthcare costs, and reduced convenience due to the need for skilled professionals and hospital-based administration, while subcutaneous (SC) delivery is limited by volume restrictions and tolerability issues for high doses of large molecules like monoclonal antibodies, particularly for brain-targeting therapies.
Innovation Solution
Development of compositions for subcutaneous administration of high doses and volumes of brain-targeting antibodies or antigen-binding fragments at concentrations of 130 mg/mL to 200 mg/mL, potentially enhanced with permeation enhancers like hyaluronidase, to treat Alzheimer's disease and cognitive impairment, allowing for self-administration and wider treatment settings.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If subcutaneous administration is used for convenience and reduced healthcare costs, then ease of operation and loss of time are improved, but volume of fluid that can be administered is limited
Solution Approach 1:
The patent changes the concentration parameter of the therapeutic composition to achieve the desired volume administration. By formulating the composition at a specific concentration range (e.g., 10-50 mg/mL), the patent enables administration of higher volumes (e.g., 10-50 mL) subcutaneously, thereby increasing the total quantity of therapeutic delivered while maintaining ease of self-administration.
2Reliability
If higher dose/volume of SC administration is used to achieve brain targeting efficacy, then therapeutic effectiveness is improved, but tolerability issues such as infusion-site swelling occur
Solution Approach 1:
The patent introduces a permeation enhancer as an intermediary substance that facilitates the delivery of the therapeutic through the subcutaneous tissue. This enhancer acts as a mediator that increases the permeability of the tissue, allowing higher volumes and doses of the therapeutic to be administered subcutaneously without causing excessive local swelling or tissue damage, thereby maintaining both effectiveness and tolerability.
3Reliability
If multiple SC infusion sites or frequent administration are used to achieve equivalent drug exposure, then therapeutic coverage is improved, but loss of time and device complexity increase
Solution Approach 1:
The patent optimizes the concentration and volume parameters of the SC composition to achieve adequate drug exposure in a single administration. By adjusting these parameters, the patent reduces the need for multiple infusion sites or frequent administrations, thereby decreasing the time loss and simplifying the administration process while maintaining reliable therapeutic coverage.
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
Enables effective subcutaneous administration of high doses of brain-targeting therapeutics, potentially delaying Alzheimer's disease progression and improving cognitive function without increasing adverse events, while reducing healthcare costs and increasing treatment convenience.
Implementation Method 1
potentially enhanced with permeation enhancers like hyaluronidase
Data Source
AI summary
The present disclosure provides methods for treating Alzheimer's disease by subcutaneously administering a high volume and high dose of a brain targeting antibody or antigen-binding fragment thereof and provides compositions comprising an anti-amyloid β antibody or antigen-binding fragment thereof.