On September 22, 2026 Molecular Targeting Technologies, Inc. (MTTI), a clinical-stage radiopharmaceutical company, reported 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).
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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."
(Press release, Molecular Targeting Technologies, SEP 22, 2026, https://www.mtarget.com/mm5/pdfs/NCI%20Grant.pdf [SID1234670989])