Sapu Nano Reports Major Reduction In GI Drug Exposure With IV Sapu003, Highlighting Strong PK And Tissue-Distribution Benefits; Supports Enhanced Tolerability and Antitumor Activity

Oncotelic Therapeutics’ joint venture, Sapu Nano, has released new pharmacokinetic and tissue-distribution data showing that its IV Deciparticle™ formulation of everolimus, Sapu003, dramatically reduces gastrointestinal exposure compared with the oral drug Afinitor®. The findings highlight a major advantage of the IV approach, which maintains the drug’s normal metabolic behavior while offering more consistent systemic delivery and potentially better tolerability.

The study confirms that oral everolimus results in extreme GI accumulation, with concentrations reaching more than 2,000 times higher than plasma in the stomach and hundreds of times higher in various intestinal segments. Sapu003, delivered intravenously, significantly lowers this burden, reducing stomach exposure by 67-fold and substantially decreasing small and large intestinal accumulation. This directly addresses the long-recognized GI toxicity linked to oral everolimus use.

"The fundamental challenge with oral everolimus is that the majority of the drug ends up in the gut, leading directly to the GI toxicity that limits its use," said Dr. Cynthia Lee, VP of R&D. "These new data show that IV Sapu003 avoids that problem entirely. By reducing GI accumulation by up to 67-fold, Sapu003 has the potential to offer a far more tolerable and clinically versatile version of everolimus."

The reduced GI concentrations help explain why patients frequently experience issues such as stomatitis, mucositis, abdominal discomfort, and diarrhea with oral dosing. By avoiding the gastrointestinal tract and providing steady systemic exposure, Sapu003 may offer a more tolerable therapeutic option while improving drug delivery to tumor-relevant tissues.

These pharmacokinetic advantages build on previously reported efficacy data showing that Sapu003 achieved 97–98% tumor inhibition in glycolysis-dependent xenograft models and outperformed paclitaxel. Together, the results reinforce the potential of Sapu003 to enhance both tolerability and antitumor activity in future clinical development.