Oncotelic and Sapu Nano Announces New PK Data Demonstrating IV Sapu003 Reduces GI Accumulation of Everolimus up to 67-Fold Compared With Oral Dosing

Core Insights - Oncotelic Therapeutics, Inc. announced that its joint venture, Sapu Nano, has demonstrated that its intravenous formulation Sapu003 of everolimus significantly reduces gastrointestinal drug accumulation compared to oral dosing, potentially improving tolerability and systemic exposure [1][5]. Pharmacokinetic and Tissue-Distribution Results - Sapu003 reduces gastrointestinal exposure to everolimus by 67-fold compared to oral dosing, with only 36–48× plasma levels in GI tissues versus 2,448× in the stomach, 750× in the small intestine, and 323× in the large intestine for oral everolimus [2][3]. - The findings provide a mechanistic explanation for the gastrointestinal toxicity associated with oral everolimus, which includes stomatitis, mucositis, abdominal discomfort, and diarrhea [3]. Clinical Implications - By bypassing the gastrointestinal tract, Sapu003 aims to enhance clinical tolerability and maintain antitumor potency, achieving 97–98% tumor inhibition in specific cancer models while outperforming paclitaxel [5]. - Dr. Cynthia Lee, VP of R&D, emphasized that the reduction of GI accumulation by up to 67-fold could make Sapu003 a more tolerable and versatile option for patients [6]. Technology Overview - Sapu003 utilizes the Deciparticle™ platform, a proprietary nanotechnology designed to encapsulate hydrophobic molecules for intravenous administration, improving systemic exposure and reducing gastrointestinal deposition [7][9]. - The platform supports precision delivery while maintaining manufacturability at a clinical scale, which is crucial for rapid progression from formulation to clinical trial supply [10]. Company Background - Oncotelic Therapeutics, Inc. focuses on oncology drug development, particularly for rare pediatric cancers, and has a history of evolving through various name changes and strategic acquisitions [11]. - The company is also developing AL-101 for Parkinson's Disease and erectile dysfunction, addressing significant unmet medical needs in these areas [12].