• Sapu003 Phase 1 trial begins: Australian HREC approval validates Oncotelic’s proprietary 20nm nanoparticle technology for enhanced breast cancer drug delivery
• 20nm Deciparticle(TM) achieves full bioavailability: Intravenous delivery of Everolimus (Afinitor(R)) maximizes tumor targeting and efficacy compared to 10% absorption with oral formulations
• Rapid IND platform accelerates pipeline: Strategic partnership with Medicilon supports up to 20 IND projects, shortening development timelines and enabling multiple Deciparticle(TM) drug candidates to reach clinical testing quickly

Oncotelic Therapeutics Inc. (OTCQB: OTLC) is advancing precision nanomedicine with its proprietary Deciparticle(TM) platform, beginning human trials for Sapu003, a 20nm nanoparticle formulation of Everolimus (Afinitor(R)). This scientific briefing explores why particle size is critical to drug efficacy, how Oncotelic’s technology enhances tumor targeting, and how its rapid IND platform accelerates clinical development across multiple assets.

Particle Size: The Key to Targeted Drug Delivery

Delivering anticancer drugs effectively remains a central challenge in oncology. Conventional chemotherapy exposes healthy tissues to cytotoxic agents, producing severe side effects, while oral targeted therapies often fail to reach tumors at therapeutic concentrations. Nanomedicine offers a solution, but particle size determines whether a drug reaches its intended site.

Nanoparticles in the range of 10–100 nanometers exploit the enhanced permeability and retention (“EPR”) effect, a phenomenon where leaky tumor vasculature allows small particles to penetrate and accumulate in tumor tissue while largely sparing healthy organs. However, not all nanoparticles in this size range perform equally. Particles smaller than 10nm are rapidly filtered by the kidneys, limiting exposure, whereas particles above 100nm trigger immune clearance before reaching tumors.

Recent research highlights ~20nm as an optimal size for balancing systemic circulation, tissue penetration, and tumor accumulation. These particles are small enough to traverse vascular pores but large enough to avoid premature renal clearance, allowing sustained drug exposure within tumors for enhanced therapeutic effect.

Translating Nanoparticle Precision into Clinical Potential

Oncotelic’s first Deciparticle(TM) candidate, Sapu003, reformulates Everolimus (Afinitor(R)), an mTOR inhibitor approved for breast cancer and other tumors, into 20nm nanoparticles for intravenous delivery. Oral Everolimus (Afinitor(R)) faces a critical limitation: only ~10% bioavailability, as most of the drug is lost in the digestive system and causes gastric toxicity. By contrast, Sapu003 delivers 100% of the drug directly into circulation, maximizing tumor exposure.

To that point, Sapu003 nanoparticle enables the drug to exit blood vessels through their large pores and reach tumor tissue efficiently. Larger particles would require breakdown before extravasation, reducing both efficacy and safety.

Preclinical studies support this principle. Nanomedicines ≤50nm demonstrate superior tissue penetration, enhanced tumor inhibition, and reduced systemic toxicity compared to larger formulations. By hitting the 20nm target, Sapu003 achieves a combination of precision targeting, high bioavailability, and safety, representing a meaningful advance over prior nanomedicine approaches such as Abraxane(R) (130nm) and Cynviloq(TM) (80nm).

Manufacturing at Scale: Achieving 20nm Consistency

Engineering nanoparticles at precise dimensions is technically challenging. Sapu Nano, Oncotelic’s joint venture, operates the world’s first GMP-certified facility designed specifically for Deciparticle(TM) production. The facility allows consistent 20nm particle generation at clinical scale, supporting both current trials and future pipeline expansion.

This capability distinguishes Oncotelic from earlier nanomedicine efforts, where size variability limited reproducibility and clinical translation. By controlling particle engineering at scale, Oncotelic ensures that each dose behaves predictably in vivo, a critical factor for regulatory approval and clinical efficacy.

Rapid IND Platform: Accelerating Multiple Drug Candidates

Oncotelic is leveraging its Deciparticle(TM) technology as a platform capable of reformulating multiple drugs with known safety profiles. Its strategic February 2025 partnership with Shanghai Medicilon Inc. supports up to 20 IND projects, providing a rapid IND pathway that accelerates clinical readiness.

Medicilon brings extensive regulatory experience with the FDA, EMEA, and NMPA, including a clean inspection history with no FDA 483 citations. This reduces risk and shortens timelines for Oncotelic’s clinical programs. Under this partnership, drug candidates can move from proof-of-concept to preclinical to first-in-human studies more efficiently than typical development cycles.

The 505(b)(2) regulatory pathway is particularly well-suited to Deciparticle(TM) reformulations. Because the underlying drugs are already FDA-approved, Oncotelic can leverage existing safety and efficacy data, potentially reducing clinical development time from 10–15 years to 5–10 years, while lowering cost and risk. This strategy enables rapid testing of multiple assets, expanding Oncotelic’s pipeline and positioning the company as a platform innovator in nanomedicine.

Clinical Trial Design and Market Implications

Sapu003’s Phase 1 trial (ACTRN12625001083482) is now enrolling at Australian oncology centers through partnerships with SOCRU and Ingenū, focusing on adults with advanced HR+/HER2- breast cancer or other mTOR-sensitive tumors who have exhausted standard therapies.

Breast cancer represents a global market exceeding $30 billion, forecasted to reach over $40 billion by 2030. Oral Everolimus (Afinitor(R)) has historically captured a portion of this market, generating over $1.5 billion in 2020. An injectable formulation with superior bioavailability could reclaim share while expanding access to patients unable to tolerate oral therapy, as full drug absorption through intravenous delivery has the potential to achieve meaningful tumor shrinkage where oral formulations have been limited.

From Particle Engineering to Patient Outcomes

The global nanomedicine market was valued at ~$215 billion in 2023 and is projected to exceed $500 billion by 2032, largely driven by oncology applications and the recognition that particle size optimization can transform outcomes. Oncotelic’s Deciparticle(TM) platform aligns with this trend, offering a scalable, reproducible, and clinically validated approach to nanoparticle drug delivery.

With Sapu003 entering human trials, GMP-scale manufacturing of 20nm particles, and rapid IND support for up to 20 drug candidates, Oncotelic has built a comprehensive ecosystem for translating nanomedicine innovation into measurable clinical impact. For investors and stakeholders interested in next-generation cancer therapeutics, OTLC exemplifies how precision particle engineering and streamlined regulatory pathways can combine to shorten development cycles and enhance patient outcomes.

For more information, visit the company’s website at www.Oncotelic.com.

NOTE TO INVESTORS: The latest news and updates relating to OTLC are available in the company’s newsroom at ibn.fm/OTLC

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