Vesselon Introduces the First On-site Co-Formulation Platform that Dramatically Improves How Cells Receive and Act on Drugs

The platform allows pharmaceutical companies to extend patents, better manage product lifecycles, and generate differentiated blockbusters.

GREENWICH, Conn., Aug. 28, 2023 /PRNewswire/ -- Vesselon, Inc. introduces the first on-site platform to enhance the cellular uptake and response to any intravenous therapy – without altering the active drug in any way. The process penetrates targeted tissues or tumors more effectively to improve drug efficacy several fold.

For drug companies, this system can offset the loss of exclusivity on mature drugs with new patentable co-formulations. Because it combines the drugs on-site, the platform can be adopted seamlessly without any changes in pharmaceutical manufacturing, packaging, or distribution processes.

Consisting of an FDA-approved lipid drug combined with any FDA-approved IV therapy, the formulation is targeted at the diseased tissue using Agency-authorized levels of ultrasound. Therefore, the regulatory risk is very low. As an indication, the FDA has provided guidance regarding a late-stage clinical trial to enhance the efficacy of Keytruda that could be the basis of an initial product registration.

"We encapsulate many different classes of drugs, from small molecules, monoclonal antibodies, nucleic acids to viruses," said Clay Larsen, President and CEO of Vesselon. "The best way to think about our approach is not just as a delivery platform, but one that changes the ability of tissues to receive and act on the drug much more effectively."

To make the target more responsive and the treatment more effective, the platform employs standard ultrasound that initiates up to nine biophysical activities, or Modes of Action, at the cellular and tissue level:

Open Tissue and Capillary Barriers

1. Capillary Permeability: Cavitation pressure opens nanoscale pores in capillary walls, improving access to targeted tissues (sonoporation).

2. Deep Tissue Penetration: Biophysical pressure releases the encapsulated drug at the target and facilitates its movement through dense tissue (inertial cavitation).

3. Improved Access to Cells: Reduces interstitial fluid pressure so more drug reaches the intended target cells.

Trigger Cellular Actions

4. Enhanced Cell Entry: Alters cell wall polarity, facilitating drug access to target cells through endocytosis.

5. Cell Membrane Fusion: The liposomes enhance fusion with cell membranes, aiding drug delivery.

6. Induction of Cell Death: The liposomes induce apoptosis in tumor cells, contributing to therapeutic effects.

7. Increased Cell Membrane Permeability: Rearranges the cell cytoskeleton to enhance cell membrane permeability, improving drug uptake.

8. Suppression of Drug Efflux: Down-regulates PGP efflux pumps, ensuring more drug remains within cells.

Initiate Immune and Abscopal Effects

9.  Immune Response Activation: Stimulated cell membranes recruit T-cells to the tumor, enhancing the immune response and strong abscopal activity.

These multiple Modes of Action make the tissue or tumor far more receptive to the active drug, improving its pharmacokinetic and pharmacodynamic profile, and potentially improving the Therapeutic Index. This cutting-edge technology, according to The Wall Street Journal, “could hold a key to a problem that has long challenged drug developers.”

Despite the compelling evidence garnered from five human studies, preclinical data from Vesselon, and the publication of more than 1,600 independent preclinical studies, no major drug company has participated in researching sonicated microspheres—other than in partnership with Vesselon. This is due to a lack of IP, as well as concerns about adoption and the FDA. The Vesselon platform overcomes these issues.

First, this advance creates new patentable entities that will extend the exclusivity of existing franchises. The technology is protected with manufacturing trade secrets and filed patents covering the never-observed-before on-site self-assembly and self-encapsulation of an active drug in up to 10 billion lipid microspheres and 50 trillion self-organizing liposomes.

Second, Vesselon offers a "no change in practice" adoption methodology, as there is no need to modify the active drug or change its packaging, manufacturing, or distribution. The active drug is delivered to the clinic as-is, with the co-formulation done on-site.

Finally, Vesselon provides a low-friction regulatory path because it co-formulates already approved drugs with an FDA-approved lipid. This combination therapy is activated by FDA-authorized ultrasound energy levels.

These factors pave the way to a rapid speed to market for any co-formulated products. Experienced drug industry executive Joe Truitt commented, "This platform really does not pose many risks. With minimal technology, clinical, manufacturing, and regulatory issues, the risk boils down to executing life cycle trials. But these are for approved products. The promise of potential better efficacy along with the new chemical entity designation and patent is attractive for any franchise."

This proprietary, practical, and low-friction regulatory path can give new life to older drugs and provide step-function performance improvements for future pipeline blockbusters.

Larsen concluded, "Beyond enhancing the patent life of mature drugs, we believe that the platform also has the ability to produce multiple billion-dollar new drug co-formulations before 2030."

About Vesselon, Inc.
Vesselon develops patentable drug co-formulations. The on-site platform combines any intravenous drug with the Vesselon FDA-approved lipid microsphere and uses commercial ultrasound equipment to safely trigger nanoscale cellular and tissue activities that make targeted cells much more responsive to treatment. These co-formulated drugs can offset the loss of exclusivity for mature therapies and deliver unprecedented levels of efficacy for pipeline drugs.

For additional information, please visit www.Vesselon.com.

Additional materials:

• Roland, Denise, "New Ultrasound Therapy Could Help Treat Alzheimer's, Cancer," The Wall Street Journal, July 31. 2023.
• XU J. et al. "Sonoporation-Enhanced Delivery of STING Agonist Induced Robust Immune Modulation and Tumor Regression," Advanced Therapeutics, 2021. 2100154. 
• Qin, Jiale, Wang, Tzu-Yin, Willmann, Jurgen K., "Sonoporation: Applications for Cancer Therapy, Therapeutic Ultrasound," Advances in Experimental Medicine and Biology, Vol. 880.
• Dimcevski, Georg et al, "A human clinical trial using ultrasound and microbubbles to enhance gemcitabine treatment of inoperable pancreatic cancer," Journal of Controlled Release 243, October 12, 2016.

SOURCE Vesselon, Inc.