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 show that oral dosing leads to 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.

The company suggests this substantial reduction 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 is particularly relevant for cancer patients who often experience gastrointestinal side effects from oral targeted therapies, potentially allowing for more effective dosing with fewer adverse effects.

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.

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The implications of this pharmacokinetic data are significant for cancer treatment optimization. Everolimus, an mTOR inhibitor used in various cancers including renal cell carcinoma and breast cancer, often causes gastrointestinal toxicities that can limit dosing and treatment efficacy. The demonstrated reduction in gut exposure with intravenous administration suggests a potential pathway to maintain therapeutic benefits while minimizing debilitating side effects that frequently lead to dose reductions or treatment discontinuation.

This development represents an important step in addressing treatment-related toxicities that impact patient quality of life and treatment adherence. The ability to deliver targeted therapies with reduced gastrointestinal burden could expand treatment options for patients who cannot tolerate standard oral formulations, particularly those with pre-existing gastrointestinal conditions or heightened sensitivity to drug side effects. The data supports further investigation into intravenous formulations as a strategy to optimize the therapeutic index of established cancer medications.