Invented by Robert Lyon, Svetlana O. Doronina, Timothy Bovee, Seagen Inc

The market for self-stabilizing linker conjugates is rapidly growing as researchers and pharmaceutical companies recognize their potential in drug delivery systems. These conjugates offer a unique solution to the challenges faced in traditional drug delivery methods, such as poor stability and limited targeting capabilities. Self-stabilizing linker conjugates are designed to improve the stability and efficacy of drug molecules by attaching them to a carrier molecule through a linker. The linker acts as a bridge between the drug and the carrier, ensuring that the drug remains stable and active until it reaches its target site. One of the key advantages of self-stabilizing linker conjugates is their ability to enhance drug stability. Many drugs are susceptible to degradation or inactivation when exposed to various environmental factors, such as pH changes or enzymatic degradation. By attaching the drug to a carrier molecule through a self-stabilizing linker, the drug is protected from these factors, allowing for improved stability and a longer shelf life. Additionally, self-stabilizing linker conjugates offer enhanced targeting capabilities. The carrier molecule can be designed to specifically recognize and bind to target cells or tissues, allowing for precise drug delivery. This targeted approach not only increases the efficacy of the drug but also reduces the potential for off-target side effects. The market for self-stabilizing linker conjugates is driven by the increasing demand for more effective and targeted drug delivery systems. Traditional drug delivery methods often suffer from limitations, such as poor bioavailability, low stability, and non-specific targeting. Self-stabilizing linker conjugates address these challenges, offering a promising solution for the development of novel therapeutics. Pharmaceutical companies are investing heavily in research and development of self-stabilizing linker conjugates, with a focus on improving drug stability, enhancing targeting capabilities, and optimizing the release of the drug at the target site. These efforts are aimed at developing more efficient and safer drug delivery systems that can improve patient outcomes. The market for self-stabilizing linker conjugates is also supported by advancements in nanotechnology and biotechnology. These fields provide the tools and techniques necessary for the design and synthesis of carrier molecules and linkers with specific properties. The ability to precisely control the size, shape, and surface properties of these conjugates allows for further customization and optimization of their drug delivery capabilities. In conclusion, the market for self-stabilizing linker conjugates is experiencing significant growth as researchers and pharmaceutical companies recognize their potential in improving drug delivery systems. These conjugates offer enhanced stability, targeting capabilities, and release profiles, making them an attractive option for the development of novel therapeutics. With continued advancements in nanotechnology and biotechnology, the market for self-stabilizing linker conjugates is expected to expand further, revolutionizing the field of drug delivery and improving patient outcomes.

The Seagen Inc invention works as follows

The present invention consists of Ligand-Drug conjugates, Drug-Linkers and Linkers as well as Ligand-Linker Combinations that contain a self-stabilizing assembly linker component.

Background for Self-stabilizing linker conjugates

Abbreviations & Definitions

General

The Self-Stabilizing Links Assembly

Selected embodiments of the Invention

Functional Agent-Linker Conjugates

Further embodiments of the Invention

Hydrolysis Enhancers (HE) and Electronic-Withdrawing groups

Drug Loading

Treatment of Cancer

Compositions & Methods of Administration

EXAMPLES

Example 1?” Synthesis of Representative Self Stabilizing Components

Maleyl-Lysine(boc)OH

Maleoyl-Lysine(boc)-OH

Maleyl-DPR(boc)OH

Maleoyl-DPR(boc)-OH

Maleyl-Dimethyllysine

Maleoyl-dimethyllysine

Example 2?Synthesis of mDPR-Val-Cit-PAB-MMAE

Scheme:

Preparation of Fmoc-Val-Cit-PAB-MMAE

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