Making Drug Proteins Last Longer and Target Diseases Better

This patent describes ways to make protein and peptide drugs stay in the body longer and target specific diseases like autoimmune conditions or cancer more precisely by linking them together or combining them with other molecules.

What it covers

This patent describes two main methods to improve drug treatments. First, it details how to extend the active life of peptide drugs in the body (their "half-life"). This is done by connecting at least three individual peptide units, called monomers, in a linear chain using a special "self-immolative linker" (Claim 1). This creates a larger molecule, an "oligomer," with a total molecular weight greater than 60,000 (Claim 1). The linker is designed to break apart inside the body, releasing the active peptides when needed. For example, this method could be applied to peptides like Exenatide (Claim 3) or CNP peptide (Claim 4). Second, the patent describes creating specialized combinations, or "conjugates," to treat autoimmune diseases, specifically systemic lupus erythematosus (Claim 6). These conjugates combine an "auto antigen" (a substance that causes the immune system to attack the body's own tissues, such as B cell antigen or DNA, as in Claims 7-8) with a "second antigen" that the body already has natural antibodies against (like alpha-gal or L-rhamnose, as in Claim 9). The goal is to redirect the body's immune response to treat the disease more effectively.

What it doesn't cover

• —Does not cover extending peptide half-life by connecting fewer than three peptide units.
• —Does not cover peptide oligomers with a total molecular weight of 60,000 or less.
• —Does not cover linkers that are not "self-immolative" or are not cleavable inside a living organism.
• —Does not cover conjugates for autoimmune diseases other than systemic lupus erythematosus, unless additional claims specify.
• —Does not cover conjugates where the second antigen is not something the body already has natural antibodies against.

The clever bit

The core innovation involves using a cleavable linker to temporarily increase the size of a peptide drug, which helps it stay in the body longer by preventing rapid breakdown, while still allowing the active drug to be released when and where it's needed. For autoimmune diseases, the cleverness lies in hijacking existing antibodies to deliver or redirect an immune response against specific disease targets.

Why it matters

Many protein and peptide drugs break down quickly in the body, requiring frequent injections, which can be inconvenient for patients. This patent's methods could lead to drugs that last longer, meaning patients might need fewer doses. For autoimmune diseases, the targeted approach could reduce unwanted side effects by focusing the immune response more precisely on the disease-causing elements.

Real-world examples

• 1.Long-acting versions of Exenatide for type 2 diabetes
• 2.Other long-acting peptide drugs for chronic conditions
• 3.Experimental targeted therapies for systemic lupus erythematosus