Molecular Targeting Technologies, Inc. (MTTI), a clinical-stage radiopharmaceutical company, today announced that it has been awarded a $3.17 million, five-year National Cancer Institute (NCI) grant to advance the development of ¹⁷⁷Lu-EBRGD, an investigational radiopharmaceutical targeting integrin αvβ3, for non-small cell lung cancer (NSCLC).

The award, under NIH grant R01CA299133, will support an integrated translational program encompassing preclinical research, drug product manufacturing, regulatory preparation, and planned clinical studies. These activities are intended to establish the scientific, manufacturing, and regulatory foundation for evaluating ¹⁷⁷Lu-EBRGD in patients with NSCLC, subject to applicable regulatory requirements and clinical readiness.

Advancing a Targeted Radiopharmaceutical Approach for NSCLC

¹⁷⁷Lu-EBRGD is designed to target integrin αvβ3, a cell-surface receptor associated with tumor biology and angiogenesis. MTTI is investigating this molecular target as part of its strategy to develop targeted radiopharmaceutical therapies for oncology.

The program builds on MTTI’s EvaThera™ pharmacokinetic engineering platform, which incorporates Evans Blue (EB)-based reversible albumin binding into targeted molecules to modify their circulation and tissue distribution.

NCI-funded research will characterize ¹⁷⁷Lu-EBRGD’s tumor-targeting properties, pharmacokinetics, dosimetry, therapeutic activity, and safety-related characteristics to inform its continued development.

Integrated Development Program

The five-year award will support coordinated activities to advance ¹⁷⁷Lu-EBRGD toward potential clinical evaluation, including:

  • Preclinical evaluation: Investigating tumor targeting, biodistribution, pharmacokinetics, dosimetry, antitumor activity, and normal-tissue toxicity.

  • Drug product manufacturing: Supporting drug product development and manufacturing under applicable current Good Manufacturing Practice (cGMP) requirements for future clinical development.

  • Regulatory preparation: Developing scientific, manufacturing, and supporting documentation toward a potential Investigational New Drug (IND) application, subject to applicable regulatory requirements.

  • Clinical development: Planning and preparation for clinical studies in patients with metastatic NSCLC following first-line systemic therapy, subject to regulatory authorization and appropriate clinical and operational readiness.

Preclinical Research Supports Further Investigation

Published preclinical studies of Evans Blue-modified RGD radiopharmaceutical, including investigations using NSCLC patient-derived xenograft (PDX) models, have reported enhanced tumor accumulation and retention compared with non-albumin-binding comparators, along with tumor-growth inhibition in experimental models.

These findings provide a scientific rationale for further investigation. Preclinical findings do not establish safety, efficacy, or clinical benefit in patients. The therapeutic potential of ¹⁷⁷Lu-EBRGD remains to be evaluated in appropriately designed clinical studies.

Expanding MTTI’s EvaThera™ Platform and Oncology Pipeline

MTTI is advancing EvaThera™ across multiple molecular targets and oncology programs.

Its lead clinical program, ¹⁷⁷Lu-EBTATE, targets somatostatin receptor 2 (SSTR2) for peptide receptor radionuclide therapy (PRRT) in gastroenteropancreatic neuroendocrine tumors (GEP-NETs). The company is also developing ¹⁷⁷Lu-EBRGD for potential application in NSCLC.

Additional planned projects include EB-FAPI and EB-GRPR, extending the company’s research into fibroblast activation protein (FAP)- and gastrin-releasing peptide receptor (GRPR)-targeted radiopharmaceutical approaches. MTTI’s broader research strategy also includes investigating both lutetium-177 (¹⁷⁷Lu) and actinium-225 (²²⁵Ac) within the EvaThera™ platform, subject to program-specific research and development plans.

Leadership Perspectives

“Receiving this five-year, $3.17 million NCI award is a significant milestone for MTTI and our EvaThera™ platform,” said Dr. Chris Pak, Chairman and Chief Executive Officer of MTTI and Principal Investigator of the award. “This support will advance ¹⁷⁷Lu-EBRGD toward clinical evaluation and extend our platform into integrin αvβ3-targeted radiopharmaceutical development. Building on our lead EBTATE program, this initiative broadens our oncology research and strengthens our efforts to explore new treatment approaches for patients with NSCLC. We are deeply grateful to the NCI for its support.”

“NSCLC remains a significant unmet medical need, as many patients are diagnosed only after the disease has spread beyond the lung. For patients with distant-stage NSCLC in the United States, the five-year relative survival rate is approximately 12%, underscoring the urgent need for new, effective, and well-tolerated treatment options,” said Dr. Norman LaFrance, Chief Strategy Officer of MTTI. “With support from this NCI-funded program, we aim to advance the scientific and development data needed to evaluate the therapeutic potential of ¹⁷⁷Lu-EBRGD and inform its progression toward clinical evaluation for patients with NSCLC.”

About Molecular Targeting Technologies, Inc.

Molecular Targeting Technologies, Inc. (MTTI) is a clinical-stage radiopharmaceutical company developing targeted radiopharmaceuticals for oncology. Its EvaThera™ platform uses Evans Blue-based reversible albumin binding to engineer the pharmacokinetic properties of targeted molecules.

MTTI’s pipeline includes ¹⁷⁷Lu-EBTATE, a clinical-stage program targeting SSTR2 for GEP-NETs; ¹⁷⁷Lu-EBRGD, an investigational integrin αvβ3-targeted program for NSCLC; and planned development projects involving EB-FAPI and EB-GRPR.

For more information, please visit www.mtarget.com.

Forward-Looking Statements

This press release contains forward-looking statements, including statements regarding the scope and execution of the NCI-funded program; the development, manufacturing, and regulatory preparation of ¹⁷⁷Lu-EBRGD; planned clinical studies; planned EB-FAPI and EB-GRPR projects; and the potential of MTTI’s EvaThera™ platform and investigational radiopharmaceuticals. These statements are based on current expectations and assumptions and are subject to risks and uncertainties that could cause actual results or developments to differ materially.

¹⁷⁷Lu-EBRGD, EB-FAPI, and EB-GRPR are investigational or planned development projects, as applicable, and have not been established as safe or effective for any clinical use. Planned clinical studies and development activities are subject to regulatory authorization, successful completion of required development activities, funding conditions, and other applicable requirements. MTTI undertakes no obligation to update forward-looking statements except as required by law.

NIH Funding Acknowledgment

This work is supported by the National Cancer Institute of the National Institutes of Health under Award Number R01CA299133. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health.

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