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

San Diego, Calif., Dec. 04, 2025 (GLOBE NEWSWIRE) -- Sapu Nano today announced new pharmacokinetic (PK) and tissue-distribution results demonstrating that Sapu003, the company’s intravenous (IV) Deciparticle^™ formulation of everolimus, substantially reduces gastrointestinal (GI) drug accumulation, addressing one of the most significant and well-recognized limitations of oral everolimus (Afinitor^®). The data indicate that Sapu003 may offer improved tolerability while preserving the drug’s intrinsic metabolic profile and enabling more consistent systemic exposure.

IV Sapu003 Reduces GI Exposure to Everolimus by 67-Fold Compared With Oral Dosing

New tissue-distribution data show that Sapu003, delivered intravenously, eliminates the extreme gastrointestinal accumulation characteristic of oral everolimus. After oral dosing, everolimus reaches 2,448× plasma levels in the stomach, 750× plasma in the small intestine, and 323× plasma in the large intestine, confirming that the gut is the dominant exposure site for the oral formulation.

In contrast, IV Sapu003 demonstrates only 36–48× plasma levels across the same GI tissues, representing a 67-fold reduction in stomach exposure, a 15.7-fold reduction in small-intestinal exposure, and a 7.4-fold reduction in large-intestinal exposure.

These findings provide a clear mechanistic explanation for the well-documented GI toxicity of oral everolimus—including stomatitis, mucositis, abdominal discomfort, and diarrhea.

Presentation information: PS4-06-05. Sapu003: Everolimus for Injection — Pharmacokinetic Rationale for Phase I Evaluation in HR⁺/HER2⁻ Metastatic Breast Cancer.

Potential for Improved Clinical Tolerability and Antitumor Potency

By bypassing the gastrointestinal tract and delivering the drug directly into circulation, Sapu003:

• Avoids the high local GI concentrations associated with oral toxicity
• Produces more consistent systemic exposure
• Enhances drug penetration into tumor-relevant tissues
  

These PK advantages complement previously reported efficacy findings in which Sapu003 achieved 97–98% tumor inhibition in glycolysis-addicted xenograft while outperforming paclitaxel.

Management Commentary
“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.”

About Sapu003
Sapu003 is a novel intravenous nanoparticle formulation of everolimus engineered using Sapu Nano’s proprietary Deciparticle^™ technology. It is designed to overcome the poor bioavailability, intestinal toxicity, and variable patient exposure seen with oral everolimus while enabling reliable, predictable weekly IV dosing.

About the Deciparticle^™ Platform
The Deciparticle^™ platform is a proprietary nanotechnology engineered to encapsulate hydrophobic molecules as uniform, sub-20 nm nanoparticles for intravenous administration. The platform improves systemic exposure, reduces GI deposition, and supports precision delivery while maintaining manufacturability at clinical scale.

About Sapu Nano
Sapu Nano is a clinical-stage biotechnology company developing Deciparticle^™ nanomedicine therapeutics designed to optimize the delivery of hydrophobic oncology agents and peptide-based therapeutics. The company operates an integrated ISO-5 cGMP manufacturing facility supporting rapid progression from formulation to clinical trial supply.

For more information, visit www.sapunano.com.

Investor & Media Contact
Sapu Nano (US) LLC
Investor Relations
ir@sapubio.com