Intravenous Everolimus Formulation Shows Reduced Gastrointestinal Exposure in New Pharmacokinetic Data

New pharmacokinetic data from Oncotelic Therapeutics, Inc. reveals that its intravenous Deciparticle formulation of everolimus, designated Sapu003, significantly reduces gastrointestinal drug accumulation when compared to oral administration of the same medication. The findings demonstrate that oral dosing results in extreme gut exposure, with drug levels in the stomach reaching up to 2,448 times those found in plasma. In contrast, intravenous Sapu003 limits gastrointestinal tissue concentrations to just 36–48 times plasma levels, representing reductions of up to 67-fold.

This substantial decrease in gastrointestinal exposure could lead to improved tolerability for patients receiving everolimus treatment. By minimizing drug accumulation in the gut while maintaining the drug's intrinsic metabolic profile, the intravenous formulation may provide more consistent systemic exposure to the medication. This development holds particular significance for cancer patients who frequently experience gastrointestinal side effects from oral targeted therapies, potentially enabling more effective dosing with fewer adverse effects.

The data release comes through BioMedWire, a specialized communications platform focusing on biotechnology and biomedical sciences developments. BioMedWire provides distribution services through the Dynamic Brand Portfolio at IBN, offering wire solutions, editorial syndication, and social media distribution to reach investors and the general public. More details about their services can be found at https://www.BioMedWire.com.

Oncotelic Therapeutics operates as a clinical-stage biopharmaceutical company focused on developing oncology and immunotherapy products, with particular attention to high-unmet-need cancers and rare pediatric indications. The company holds a 45% stake in the Sapu Nano joint venture responsible for developing the Sapu003 formulation. Additional information about the company's developments is available through their newsroom at https://ibn.fm/OTLC.

The implications of this pharmacokinetic data extend beyond immediate patient tolerability improvements. Reduced gastrointestinal exposure could potentially allow for higher or more frequent dosing regimens without increasing side effects, which might enhance therapeutic outcomes for patients with various cancers treated with everolimus. This intravenous formulation approach represents an important advancement in drug delivery technology that addresses a significant limitation of oral targeted cancer therapies.

As cancer treatment increasingly relies on targeted therapies that patients take orally over extended periods, managing gastrointestinal side effects becomes crucial for treatment adherence and quality of life. The substantial reduction in gut exposure demonstrated by Sapu003 suggests a potential paradigm shift in how everolimus and similar medications might be administered to maximize therapeutic benefit while minimizing debilitating side effects that often lead to dose reductions or treatment discontinuation.