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 concentrations 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 compared to oral administration.

The company indicates 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 implications extend to treatment adherence and quality of life considerations for patients undergoing long-term therapy with mTOR inhibitors like everolimus.

Oncotelic Therapeutics operates as a clinical-stage biopharmaceutical company developing oncology and immunotherapy products, with focus on high-unmet-need cancers and rare pediatric indications. The company's CEO, Dr. Vuong Trieu, has contributed significantly to its intellectual property portfolio with more than 150 patent applications and 39 issued U.S. patents. Additional information about the company's developments is available through their newsroom at https://ibn.fm/OTLC.

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. The pharmacokinetic findings represent an important step in addressing treatment-limiting toxicities associated with oral targeted cancer therapies, potentially expanding therapeutic options for patients who cannot tolerate current formulations.