Precision ADC Platform for Safer Glucocorticoid Therapies

Background:

Glucocorticoids are cornerstone drugs for inflammation, autoimmune disorders, and cancer therapy, but their systemic use is constrained by severe side effects such as bone loss, metabolic disturbances, and immunosuppression. Current delivery methods lack precision, exposing healthy tissues to drug activity and compromising patient safety. These limitations reduce treatment duration, therapeutic efficacy, and regulatory acceptance. The described invention directly addresses these challenges by coupling glucocorticoids to antibodies through a stable linker that ensures selective uptake and release within diseased, antigen-expressing cells.

Technology Overview:

This technology introduces a new class of glucocorticoid antibody-drug conjugates (ADCs) that combine therapeutic glucocorticoids with antibodies via a highly polar peptide linker and a stable, self-immolative release system. The design provides plasma stability and precise intracellular delivery, overcoming challenges of glucocorticoid hydrophobicity and non-specific toxicity. Upon internalization, the ADCs selectively release the glucocorticoid receptor modulators within target antigen-expressing cells, ensuring localized action and minimal systemic exposure. This precision delivery platform represents a significant advance for safer and more effective glucocorticoid-based therapies.

Advantages:

• Targeted delivery reduces systemic side effects of glucocorticoids
• Stable linker design enables controlled release in tumor and immune cells
• Demonstrated stability in mouse and human plasma
• Effective against inflammatory disorders, autoimmune diseases, and blood cancers
• Enables higher, safer dosing through targeted mechanism
• Overcomes hydrophobic formulation challenges

Applications:

• Treatment of autoimmune diseases such as lupus, rheumatoid arthritis, and multiple sclerosis
• Therapies for inflammatory conditions including asthma, colitis, and dermatitis
• Targeted treatment of leukemias and lymphomas
• Adjunct therapy for solid tumors where glucocorticoid modulation improves outcomes
• Potential use in organ transplant immunomodulation

Intellectual Property Summary:

• US Provisional Application: 63/724,465 (Filed 11/25/2024)

Stage of Development:

Validated in vitro and in vivo animal studies demonstrating targeted delivery and plasma stability.

Licensing Status:

This technology is available for licensing.

Licensing Potential:

Ideal for biopharmaceutical partners developing safer anti-inflammatory and oncology therapeutics seeking targeted delivery platforms that enhance efficacy while minimizing systemic toxicity.

Additional Information:

Preclinical pharmacokinetic and stability data available upon request.