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Oncotelic and Sapu Nano Announces New PK Data Demonstrating IV Sapu003 Reduces GI Accumulation of Everolimus up to 67-Fold Compared With Oral Dosing
Globenewswire· 2025-12-03 14:00
Core Insights - Oncotelic Therapeutics, Inc. has announced significant advancements in its joint venture Sapu Nano, particularly regarding the intravenous formulation Sapu003 of everolimus, which shows a substantial reduction in gastrointestinal drug accumulation compared to the oral version [1][5]. Group 1: Pharmacokinetic and Tissue-Distribution Results - Sapu003 reduces gastrointestinal exposure to everolimus by 67-fold compared to oral dosing, with only 36-48 times plasma levels in GI tissues, significantly lower than the oral formulation [2][3]. - After oral administration, everolimus reaches extremely high plasma levels in the stomach (2,448×), small intestine (750×), and large intestine (323×), indicating that the gut is the primary exposure site for the oral formulation [2][3]. Group 2: Clinical Implications - The reduction in gastrointestinal accumulation is expected to improve clinical tolerability and reduce GI toxicity, which includes symptoms like stomatitis, mucositis, abdominal discomfort, and diarrhea [3][6]. - Sapu003 has demonstrated 97-98% tumor inhibition in glycolysis-addicted xenografts, outperforming paclitaxel, suggesting enhanced antitumor potency [5]. Group 3: Technology and Development - Sapu003 utilizes Sapu Nano's proprietary Deciparticle technology, designed to enhance the delivery of hydrophobic oncology agents while improving systemic exposure and reducing GI deposition [6][7]. - The Deciparticle platform encapsulates hydrophobic molecules as uniform nanoparticles for intravenous administration, supporting precision delivery and manufacturability at clinical scale [7]. Group 4: 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 aims to leverage its expertise to improve treatment outcomes for cancer patients, with a special emphasis on innovative drug delivery systems [11].