A groundbreaking discovery by UT Health San Antonio scientists could revolutionize drug delivery, enabling intravenous medications to be taken orally, potentially transforming treatments for diseases like cancer and Alzheimer’s.
Key Points at a Glance
- New chemical strategy allows large, polar drugs to be absorbed orally.
- Utilizes CD36 receptors to facilitate drug entry into cells.
- Potential to cross the blood-brain barrier, aiding in treating brain diseases.
- Could redefine drug design and personalized medicine approaches.
- Findings published in the journal Cell on April 17, 2025.
In a significant advancement for pharmaceutical science, researchers at The University of Texas Health Science Center at San Antonio have developed a method that may allow intravenous (IV) drugs to be administered orally. This innovation could simplify treatment regimens for patients with complex diseases such as brain cancer and Alzheimer’s.
Traditionally, certain medications, especially those with large and water-soluble molecules, require IV administration due to their inability to be absorbed effectively through the digestive system. The new approach, termed “chemical endocytic medicinal chemistry,” addresses this challenge by leveraging the body’s own cellular mechanisms.
The strategy focuses on the CD36 receptor, a protein found on the surface of many cells. By chemically modifying drugs to enhance their interaction with CD36, the researchers facilitated the drugs’ entry into cells via endocytosis—a process where cells engulf external substances. This method not only improves oral absorption but also shows promise in enabling drugs to cross the blood-brain barrier, a significant hurdle in treating neurological conditions.
Dr. Robert A. Hromas, dean of the Joe R. and Teresa Lozano Long School of Medicine at UT Health San Antonio, emphasized the potential impact: “This innovative chemical approach can potentially make any intravenous drug able to be taken orally. It also can promote any drug crossing the blood-brain barrier. This will remarkably broaden the number of agents we have to treat brain cancer or dementia.”
The research, led by Dr. Hong-yu Li, professor of medicinal chemistry and chemical biology, in collaboration with Duke University and the University of Arkansas for Medical Sciences, was published in the journal Cell on April 17, 2025. The study, titled “C36-mediated endocytosis of proteolysis-targeting chimeras,” details how optimizing drug interactions with CD36 can overcome previous limitations in drug delivery.
This breakthrough challenges the long-standing “Rule of 5” in drug development, which posits that molecules larger than 500 Daltons are unlikely to be orally bioavailable. By enabling larger molecules to be absorbed through the digestive tract, this discovery opens new avenues for drug design and personalized medicine, potentially improving treatment accessibility and patient compliance.
As the medical community continues to explore the implications of this research, the prospect of converting IV therapies into oral medications offers hope for more convenient and effective treatments for patients worldwide.
Source: University of Texas Health Science Center at San Antonio
