Narciclasine Water-Soluble Prodrug

Description:

This invention introduces narciclasine-2-esters, prodrugs of the natural anticancer alkaloid narciclasine, engineered to significantly improve aqueous solubility and bioavailability. The lead compound, narciclasine-2-succinate, increases water solubility by over tenfold without compromising anticancer efficacy, facilitating effective delivery in vivo. The prodrug is designed for enzymatic activation within the body, releasing active narciclasine to target cancer cells.

Key Advantages:

• Significant enhancement of aqueous solubility (>10x increase).
• Retention of potent anticancer activity in vitro.
• Improved potential for effective in vivo delivery.
• Prodrug design enables controlled release of active drug via enzymatic hydrolysis.
• Addresses major limitations of native narciclasine related to protein binding and poor solubility.

Problems Solved:

• Poor water solubility limiting narciclasine’s clinical use.
• Strong protein binding reducing drug bioavailability.
• Challenges in delivering narciclasine effectively in vivo.
• Restricted therapeutic application against metastatic colon cancer.

Market Applications:

• Development of anticancer therapeutics, especially targeting colorectal cancer.
• Pharmaceutical formulations requiring improved solubility prodrugs.
• Product candidates for clinical trials in oncology.
• Collaborations and licensing opportunities with pharmaceutical companies.