Sapu Nano 公布新的药代动力学数据显示，与口服给药相比，静脉注射 Sapu003 可将依维莫司的胃肠道积累量减少 67 倍

Core Insights - Sapu Nano announced significant findings regarding the pharmacokinetics and tissue distribution of its intravenous formulation Sapu003, which utilizes the proprietary Deciparticle™ technology to reduce gastrointestinal accumulation of the drug everolimus, addressing a major limitation of the oral formulation [1][4]. Group 1: Pharmacokinetics and Efficacy - Sapu003, administered intravenously, reduces gastrointestinal exposure to everolimus by 67 times compared to oral administration, with concentrations in the stomach being 2,448 times, in the small intestine 750 times, and in the large intestine 323 times that of plasma levels for the oral form [2]. - The intravenous formulation shows a concentration in the gastrointestinal tract of only 36 to 48 times that of plasma levels, significantly lowering exposure in the stomach by 67 times, in the small intestine by 15.7 times, and in the large intestine by 7.4 times [2]. - In preclinical models, Sapu003 demonstrated a tumor suppression rate of 97% to 98%, outperforming paclitaxel, indicating its potential for enhanced antitumor efficacy [3]. Group 2: Management Commentary - Dr. Cynthia Lee, VP of R&D, highlighted that the primary challenge with oral everolimus is its accumulation in the gastrointestinal tract, leading to toxicity that limits clinical use. The new data suggests that Sapu003 can avoid this issue, potentially offering better tolerability and broader clinical applications [4]. Group 3: Product and Technology Overview - Sapu003 is a novel intravenous formulation of everolimus developed using Sapu Nano's proprietary Deciparticle technology, aimed at addressing issues such as low bioavailability, gastrointestinal toxicity, and variability in patient drug exposure [4][6]. - The Deciparticle platform is designed to encapsulate hydrophobic molecules into uniform nanoparticles smaller than 20 nanometers for intravenous delivery, improving systemic exposure and reducing gastrointestinal drug accumulation [5].