Phase 1/2, Open-Label Study of the Safety, Dosimetry and Efficacy of a 3-Dose Regimen of Escalating Doses of 177Lu-DOTA-EB-TATE in Adult Patients With Metastatic, Radioactive Iodine Non-Responsive Oncocytic (Hurthle-Cell) Thyroid Cancer

Background:
Oncocytic (Hurthle cell) thyroid cancer (HTC) is a rare disease with few treatment options. Researchers are developing a radioactive drug that targets a protein that appears in high numbers on HTC cancer cells.
Objective:
To test a radioactive drug (177LuDOTA-EB-TATE) in people with HTC.
Eligibility:
People aged 18 years and older with HTC. The HTC must have failed to respond to conventional radioactive treatment; it must also have spread to other parts of the body.
Design:
Participants will be screened. They will have a physical exam with blood tests. They will have imaging scans and a test of their heart function.
177LuDOTA-EB-TATE is infused into a vein. Participants will receive 4 infusions spaced 8 to 12 weeks apart. They will stay in the hospital for 4 to 10 days after each infusion. During and after each infusion, participants will remain in a lead-lined room until their radiation levels go down; this usually takes about 24 hours.
Participants will have 4 to 6 follow-up visits in the weeks after each infusion. Procedures will vary at each visit, but may include more imaging scans; blood and urine tests; and tests of heart function. Participants will have 2 single-photon emission computerized tomography (SPECT) scans. SPECT scans show where the study drug is sticking to tumors or maybe other parts of their body. They will lie on a table while a machine rotates around them. Participants will fill in questionnaires about how their thyroid condition affects their life.
Participants will have follow-ups visits for 5 years after their last study treatment.

Start Date16 Sep 2026

Sponsor / Collaborator

National Institute of Diabetes & Digestive & Kidney Diseases

NCT05475210

/ Unknown statusPhase 1

Phase I, Open-Label Study of the Safety and Dosimetry of a 3-Dose Regimen of Escalating Doses of 177Lu-DOTA-EB-TATE in Adult Patients With Advanced, Well- Differentiated Neuroendocrine Tumors

This is a Phase I clinical trial to assess the safety and dosimetry profiles of 177Lu-DOTA-EB-TATE in patients with advanced, metastatic or inoperable, somatostatin receptor-positive, well-differentiated GEP-NETs.

Start Date18 Jun 2022

Sponsor / Collaborator

Molecular Targeting Technologies, Inc.

[+1]

NCT03478358

/ Unknown statusPhase 1IIT

Treatment of a Long-lasting Radiolabeled Somatostatin Analogue 177Lu-DOTA-EB-TATE in Patients With Advanced Metastatic Neuroendocrine Tumors

This is a prospective study to investigate the long-lasting radiolabeled somatostatin analogue based peptide receptor radionuclide therapy and evaluate response to 177Lu-DOTA-EB-TATE in patients with advanced metastatic neuroendocrine tumors. Different groups with doses of 0.37GBq-0.74GBq (10-20 mCi) and 1.85GBq (50 mCi)of 177Lu-DOTA-EB-TATE, 3.7GBq (100 mCi)of 177Lu-DOTA-TATE will be injected intravenously. Besides, we evaluated the safety and dosimetry of 3.7GBq (100 mCi) of 177Lu-DOTA-EB-TATE with and without amino acid infusion. All patients will undergo 68Ga-DOTATATE PET/CT scans before and after the treatment.

Start Date30 Apr 2017

Sponsor / Collaborator

Peking Union Medical College Hospital

100 Clinical Results associated with 177Lu-DOTA-EB-TATE

100 Translational Medicine associated with 177Lu-DOTA-EB-TATE

100 Patents (Medical) associated with 177Lu-DOTA-EB-TATE

Literatures (Medical) associated with 177Lu-DOTA-EB-TATE

01 Jun 2023·Clinical nuclear medicine

Evaluation of Safety, Biodistribution, and Dosimetry of a Long-Acting Radiolabeled Somatostatin Analog 177Lu-DOTA-EB-TATE With and Without Amino Acid Infusion

Article

Author: Guochang Wang ; Zhaohui Zhu ; Qingxing Liu ; Jingjing Zhang ; Xiaoyuan Chen ; Yuanyuan Jiang

Purpose:

Kidney is considered to be one of the dose-limiting organs in peptide receptor radionuclide therapy (PRRT). Amino acid cocktail infusion has been applied to reduce renal absorbed dose by inhibiting the proximal tubular reabsorption of the radiopeptide. An Evans blue-modified 177Lu-labeled octreotate (177Lu-DOTA-EB-TATE) has an extended circulation in the blood, which may make the amino acid infusion unnecessary. The aim of this study was to evaluate the safety, biodistribution, and dosimetry of 177Lu-DOTA-EB-TATE with and without amino acid infusion.

Patients and Methods:

Ten patients with metastatic neuroendocrine tumors were randomly divided into 2 groups. The effect of amino acid infusion on renal uptake was assessed in a crossover randomized setting. Group A received 177Lu-DOTA-EB-TATE at a dose of 3.7 GBq without amino acid infusion for the first cycle and with amino acid infusion for the second cycle; group B received 177Lu-DOTA-EB-TATE at a dose of 3.7 GBq with amino acid infusion for the first cycle and without amino acid infusion for the second cycle. All patients underwent serial whole-body planar imaging at 1, 24, 96, and 168 hours and SPECT scan at 24 hours after radioligand administration. Abdominal CT was performed 2 days before PRRT for SPECT/CT fusion. The dosimetry was calculated using the HERMES software. Dosimetry evaluation was compared on a between-group and intrapatient basis.

Results:

Administrations of 177Lu-DOTA-EB-TATE with or without amino acids were well tolerated. No grade 4 hematotoxicity was observed in any of the patients. Grade 3 thrombocytopenia was reported in 1 patient. No nephrotoxicity of any grade was recorded. No significant difference was observed in creatinine (75.1 ± 21.7 vs 67.5 ± 18.1 μmol/L, P = 0.128), blood urea nitrogen (4.5 ± 0.8 vs 5.1 ± 1.4 mmol/L, P = 0.612), or GFR (109.3 ± 25.2 vs 100.9 ± 24.9 mL/min, P = 0.398) before and after PRRT. For each cycle, there was no significant difference in whole-body effective dose, kidney effective dose, as well as residence time of the kidneys between group A and B (P > 0.05). By intrapatient comparison, without and with amino acid infusion also did not show significant difference in whole-body effective dose (0.14 ± 0.05 vs 0.12 ± 0.04 mSv/MBq, P = 0.612), kidney effective dose (1.09 ± 0.42 vs 0.73 ± 0.31 mSv/MBq, P = 0.093), and residence time of the kidneys (2.95 ± 1.58 vs 3.13 ± 1.11 hours, P = 0.674).

Conclusions:

177Lu-DOTA-EB-TATE PRRT with and without amino acid infusion demonstrated a favorable safety profile in neuroendocrine tumor patients. Administration of 177Lu-DOTA-EB-TATE without amino acid infusion has acceptable slightly increased kidney absorbed dose and residence time of the kidneys, and does not affect kidney function. Further investigation in a larger cohort and long-term follow-up are warranted.

01 Jan 2022·Theranostics

Safety and efficacy of peptide receptor radionuclide therapy with ¹⁷⁷Lu-DOTA-EB-TATE in patients with metastatic neuroendocrine tumors

Article

Author: Zhu, Zhaohui ; Wang, Guochang ; Zhang, Jingjing ; Liu, Qingxing ; Jiang, Yuanyuan ; Sui, Huimin ; Chen, Xiaoyuan ; Wang, Jiarou ; Wang, Rongxi

Rationale: This study aimed to assess the safety, efficacy, and survival of ¹⁷⁷Lu-DOTA-EB-TATE in patients with metastatic neuroendocrine tumors (NETs). Methods: Thirty patients with metastatic NETs were prospectively enrolled and treated with ¹⁷⁷Lu-DOTA-EB-TATE (3 intended cycles at 8 to 12-week intervals, 3.7 GBq/cycle). Treatment-related adverse events were graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE), version 5.0. The treatment response was graded according to RECIST 1.1 and PERCIST 1.0 criteria. Kaplan-Meier analysis was performed to calculate progression-free survival (PFS) and overall survival (OS). Results: Patients tolerated therapy well without acute adverse effects. During peptide receptor radionuclide therapy (PRRT), no grade 4 toxicity was observed in any of the patients; grade 3 hematotoxicity was recorded in 4 patients, including grade 3 thrombocytopenia in 4 patients (13.3%) and grade-3 anemia in 1 patient (3.3%); grade 3 hepatotoxicity was recorded in 1 (3.3%) patient, and no grade 2/3/4 nephrotoxicity was observed. On long-term follow-up, none of the patients developed grade 4 hematotoxicity or nephrotoxicity of any grade, reversible grade 3 hematotoxicity (thrombocytopenia) occurred in 1 patient. There was no incidence of leukemia or myelodysplastic syndrome for the duration of follow-up. Of 27 patients with RECIST-measurable disease, partial response and stable disease were seen in 9 and 14 patients, respectively, resulting in a response rate of 33.3% and disease control rate of 85.2%. Of 29 patients evaluable for response on ⁶⁸Ga-DOTATATE PET/CT, 14 had partial response and 11 had stable disease, with a response rate of 48.3% and disease control rate of 86.2%. The follow-up period ranged from 5 to 57 months after the first ¹⁷⁷Lu-DOTA-EB-TATE PRRT with a median follow-up of 46 months. The median PFS was 36 months, and the median OS was not reached. Ki-67 index of greater than 10% was associated with poorer PFS (P = 0.012). Conclusions: Our results suggest that PRRT with approximately 3.7 GBq ¹⁷⁷Lu-DOTA-EB-TATE has acceptable toxicity profile and is effective in treating metastatic NET with high disease control rate. In addition, ¹⁷⁷Lu-DOTA-EB-TATE achieved a favorable survival outcome with encouraging PFS.

01 Mar 2021·Journal of nuclear medicine : official publication, Society of Nuclear MedicineQ1 · MEDICINE

Peptide Receptor Radionuclide Therapy of Late-Stage Neuroendocrine Tumor Patients with Multiple Cycles of¹⁷⁷Lu-DOTA-EB-TATE

Q1 · MEDICINE

Article

Author: Chen, Xiaoyuan ; Wang, Rongxi ; Guo, Hua ; Zhu, Zhaohui ; Wang, Hao ; Liu, Qingxing ; Jacobson, Orit ; Sui, Huimin ; Zhang, Jingjing ; Zang, Jie ; Cheng, Yuejuan ; Ren, Jiakun

This study aimed to evaluate the safety and efficacy of multiple cycles of ¹⁷⁷Lu-DOTA-Evans blue (EB)-TATE peptide receptor radionuclide therapy (PRRT) at escalating doses in neuroendocrine tumors (NETs). Methods: Thirty-two NET patients were randomly divided into 3 groups and treated with escalating doses. Group A received 1.17 ± 0.09 GBq/cycle; group B, 1.89 ± 0.53 GBq/cycle; and group C, 3.97 ± 0.84 GBq/cycle. The treatment was planned for up to 3 cycles. Treatment-related adverse events were graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE), version 5.0. Treatment response was evaluated according to the European Organisation for Research and Treatment of Cancer criteria and modified PERCIST. Results: Administration of PRRT was well tolerated, without life-threatening adverse events (CTCAE grade 4). CTCAE grade 3 hematotoxicity was recorded in 1 patient (16.6%) in group B (thrombocytopenia) and 3 patients (21.4%) in group C (thrombocytopenia in 3, anemia in 1). CTCAE grade 3 hepatotoxicity (elevated aspartate aminotransferase) was recorded in 1 patient in group A (8.3%) and 1 patient in group C (7.1%). No nephrotoxicity was observed. According to the criteria of the European Organisation for Research and Treatment of Cancer, the overall disease response rates were similar in groups A, B, and C (50.0%, 50.0%, and 42.9%, respectively), and the overall disease control rates were higher in groups B (83.3%) and C (71.5%) than in group A (66.7%). According to modified PERCIST, a lower disease response rate but a similar disease control rate were found. When a comparable baseline SUV_max ranging from 15 to 40 was selected, the percentage change in SUV_max increased slightly in group A (2.1% ± 40.8%) but decreased significantly in groups B and C (-38.7% ± 10.0% and -14.7% ± 20.0%, respectively) after the first PRRT (P = 0.001) and decreased in all 3 groups after the third PRRT (groups A, B, and C: -6.9% ± 42.3%, -49.2% ± 30.9%, -11.9% ± 37.9%, respectively; P = 0.044). Conclusion: Dose escalations of up to 3.97 GBq/cycle seem to be well tolerated for ¹⁷⁷Lu-DOTA-EB-TATE. ¹⁷⁷Lu-DOTA-EB-TATE doses of 1.89 and 3.97 GBq/cycle were effective in tumor control and more effective than 1.17 GBq/cycle.

News (Medical) associated with 177Lu-DOTA-EB-TATE

01 Sep 2026

·www.biospace.com

Molecular Targeting Technologies Receives Pharma Tech Outlook’s 2026 “Radiopharmaceutical Therapy Solution of the Year” Award for EvaThera™

Industry Recognition Highlights EvaThera™ as a Next-Generation Pharmacokinetic Engineering Platform for Precision Radiopharmaceutical Therapy WEST CHESTER, Pa.--(BUSINESS WIRE)--Molecular Targeting Technologies, Inc. (MTTI), a clinical-stage biotechnology company developing next-generation targeted radiopharmaceuticals, today announced that Pharma Tech Outlook has named MTTI its Radiopharmaceutical Therapy Solution of the Year 2026 , recognizing EvaThera™ , MTTI’s proprietary pharmacokinetic engineering platform based on Evans Blue (EB)-mediated reversible albumin binding. The recognition highlights EvaThera™’s differentiated approach to radiopharmaceutical development: engineering pharmacokinetics to enhance the performance of targeted radiopharmaceuticals . By combining reversible albumin binding with established and investigational targeting ligands, EvaThera™ is designed to extend circulation, increase tumor exposure, and prolong tumor retention. MTTI believes this approach represents an important complementary dimension of innovation in radiopharmaceutical therapy. Molecular targeting determines where a therapeutic agent goes; pharmacokinetic engineering can help determine how long and how effectively it remains there. According to Pharma Tech Outlook , the recognition reflects growing industry interest in optimizing how therapeutic radiation is delivered as an important dimension of innovation alongside the discovery and validation of molecular targets. Why EvaThera™ Matters EvaThera™ is a target-agnostic, modular pharmacokinetic engineering platform designed to enhance the pharmacokinetic properties of targeted radiopharmaceuticals through reversible albumin binding. Rather than relying exclusively on the discovery of new molecular targets, EvaThera™ is designed to complement established and investigational targeting ligands by optimizing their circulation and tumor-exposure characteristics. The platform is being developed across multiple molecular targets and therapeutic radionuclides, providing pharmaceutical and biotechnology developers with a potential strategy for pharmacokinetic enhancement of existing and next-generation radiopharmaceutical programs. MTTI believes that the next generation of radiopharmaceutical therapy will be shaped not only by identifying the right biological targets, but also by engineering how therapeutic radiation is delivered . EvaThera™ is designed to complement—not replace—molecular targeting by enhancing pharmacokinetics and potentially improving the therapeutic index of targeted radiopharmaceuticals. Clinical Evidence Supporting the EvaThera™ Platform The EvaThera™ platform is supported by clinical experience with 177 Lu-EBTATE , an albumin-binding somatostatin receptor 2 (SSTR2)-targeted radiopharmaceutical being developed for gastroenteropancreatic neuroendocrine tumors (GEP-NETs). Clinical evidence supporting the EvaThera™ concept: Clinical experience with 177 Lu-EBTATE in 81 patients demonstrated sustained tumor retention for up to 15 days , supporting the ability of Evans Blue-mediated albumin binding to extend tumor exposure following administration. Enhanced tumor exposure: Comparative clinical analyses demonstrated up to approximately eight-fold higher tumor uptake and/or retention with 177 Lu-EBTATE relative to 177 Lu-DOTA-TATE. In preclinical studies, 177 Lu-EBTATE demonstrated up to 35-fold greater tumor uptake and retention compared with 177 Lu-DOTA-TATE in certain models. Lower administered radioactivity in the evaluated regimen: The evaluated two-cycle 177 Lu-EBTATE regimen represented approximately 12.5% of the cumulative administered radioactivity of a conventional four-cycle Lutathera® regimen . This comparison refers to administered activity and should not be interpreted as a direct measure of whole-body or organ radiation exposure. Encouraging renal safety profile: Clinical experience to date has shown an encouraging renal safety profile, with no clinically significant nephrotoxicity observed through one year of follow-up in the evaluated population . Together, these findings provide clinical evidence supporting the underlying EvaThera™ pharmacokinetic engineering concept: prolonging systemic circulation and tumor retention may increase tumor radiation exposure and potentially improve the therapeutic index of targeted radiopharmaceuticals. A Modular Platform Across Targets and Radionuclides EvaThera™ is being developed as a modular technology designed to integrate with multiple targeting ligands and therapeutic radionuclides. The EvaThera™ platform is being advanced across multiple oncology targets, including: SSTR2 , through the clinical development of 177 Lu-EBTATE for GEP-NETs; Integrin αvβ3 , including programs targeting solid tumors such as non-small cell lung cancer; FAP , with programs advancing toward fibroblast activation protein-targeted radiopharmaceutical applications; and GRPR , with programs advancing toward gastrin-releasing peptide receptor-targeted applications across additional solid tumors. EvaThera™ is also being developed for integration with different therapeutic radionuclides, including 177 Lu , a beta-emitting radionuclide, and 225 Ac , an alpha-emitting radionuclide. This radionuclide-flexible design may allow the platform to address different therapeutic strategies and disease settings. Strategic Opportunity for Pharmaceutical and Radiopharmaceutical Developers The modular nature of EvaThera™ creates potential opportunities beyond MTTI’s proprietary pipeline. Pharmaceutical and biotechnology companies may be able to explore EvaThera™ as a pharmacokinetic enhancement strategy for existing or investigational radiopharmaceutical programs , potentially without requiring the identification and validation of an entirely new molecular target. Potential applications include: Enhancing tumor exposure and retention of established targeting ligands; Exploring pharmacokinetic optimization of investigational radiopharmaceuticals; Supporting development of next-generation beta- or alpha-emitting radiotherapeutics; and Creating opportunities for strategic licensing, co-development, and portfolio enhancement . MTTI is actively engaging pharmaceutical, biotechnology, and radiopharmaceutical companies interested in evaluating EvaThera™ as a pharmacokinetic engineering technology for existing and next-generation radiopharmaceutical programs. Executive Perspectives “We are honored to receive this recognition from Pharma Tech Outlook ,” said Chris Pak, Ph.D., Chairman and Chief Executive Officer of MTTI. “We believe the next generation of radiopharmaceutical therapy will come not only from discovering new molecular targets, but from fundamentally improving how therapeutic radiation is delivered. EvaThera™ represents our effort to establish pharmacokinetic engineering as a new dimension of precision radiopharmaceutical therapy. By enhancing tumor exposure and retention, we believe pharmacokinetic engineering has the potential to complement molecular targeting and help advance the therapeutic index of targeted radiopharmaceuticals.” “EvaThera™ offers pharmaceutical and radiopharmaceutical developers a new opportunity to optimize the pharmacokinetic performance of existing or investigational targeting strategies,” said Norman LaFrance, M.D., Chief Strategy Officer of MTTI. “The ability to enhance pharmacokinetics without requiring discovery of an entirely new molecular target could provide an attractive complementary strategy for developing next-generation radiopharmaceutical therapies. We believe this creates meaningful opportunities for strategic collaborations, licensing, and co-development with companies seeking to enhance their radiopharmaceutical pipelines.” A Broader Vision for Precision Radiopharmaceutical Therapy As precision oncology advances, MTTI believes the future of radiopharmaceutical therapy will be defined not only by what tumors are targeted, but also by how efficiently, safely, and precisely therapeutic radiation is delivered . Through EvaThera™, MTTI is developing a scalable pharmacokinetic engineering platform designed to enhance tumor exposure and retention of established and investigational targeting ligands across multiple molecular targets and therapeutic radionuclides. The recognition by Pharma Tech Outlook underscores growing industry interest in pharmacokinetic engineering as a complementary strategy to molecular targeting for improving the therapeutic potential of precision radiopharmaceutical therapies. By enabling pharmacokinetic optimization of established targeting strategies, EvaThera™ may provide pharmaceutical developers with an opportunity to enhance existing radiopharmaceutical programs while potentially reducing reliance on novel target discovery alone . MTTI is actively seeking strategic relationships with pharmaceutical, biotechnology, and radiopharmaceutical companies interested in evaluating EvaThera™ for potential licensing, co-development, or integration with existing and next-generation radiopharmaceutical programs. About Molecular Targeting Technologies, Inc. Molecular Targeting Technologies, Inc. (MTTI) is a clinical-stage biotechnology company advancing precision radiopharmaceuticals through its proprietary EvaThera™ pharmacokinetic engineering platform , based on Evans Blue-mediated reversible albumin binding. The first clinical application supporting the EvaThera™ platform is 177 Lu-EBTATE , which is being advanced toward pivotal Phase III clinical development for gastroenteropancreatic neuroendocrine tumors (GEP-NETs). MTTI is also expanding the platform across additional oncology targets, including integrin αvβ3, FAP, and GRPR , with therapeutic programs utilizing both lutetium-177 and actinium-225 . MTTI is actively engaging pharmaceutical and biotechnology companies interested in evaluating EvaThera™ for potential licensing, co-development, and integration with existing or next-generation radiopharmaceutical programs . For additional information, visit or . Forward-Looking Statements This press release contains forward-looking statements regarding the potential capabilities and future applications of the EvaThera™ technology, the development and commercialization of the Company’s product candidates, anticipated clinical and regulatory milestones, potential strategic collaborations and licensing opportunities, intellectual property, and future business prospects. These statements are based on current expectations and assumptions and are subject to risks and uncertainties that could cause actual results to differ materially. Readers are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date of this release. MTTI undertakes no obligation to update these forward-looking statements except as required by applicable law. The complete Pharma Tech Outlook feature article is available at: Contacts Media Contact Molecular Targeting Technologies, Inc. Chris Pak, Ph.D. Chairman and Chief Executive Officer Email: cpak@mtarget.com

07 Jul 2026

·www.biospace.com

Molecular Targeting Technologies Presents First Clinical Validation of the Evans Blue Platform, Demonstrating Up to 15-Day Tumor Retention Using Approximately 12.5% of the Radioactivity Required for Conventional PRRT

Largest Reported Clinical Dataset for an Albumin-Binding Radiotherapeutic Supports the Evans Blue Platform as a Foundational Technology for Next-Generation Targeted Radiopharmaceuticals WEST CHESTER, Pa.--(BUSINESS WIRE)--Molecular Targeting Technologies, Inc. (MTTI), a clinical-stage biotechnology company developing next-generation radiopharmaceutical platform technologies, today announced that clinical data from 81 patients—the largest reported clinical dataset for an albumin-binding radiotherapeutic—will be presented at the 5th Targeted Radiopharmaceuticals Summit. The dataset provides what the Company believes is the first clinical validation of its proprietary Evans Blue (EB) platform, a reversible albumin-binding technology designed to enhance the pharmacokinetics and therapeutic performance of targeted radiopharmaceuticals. The presentation supports an emerging paradigm in radiopharmaceutical oncology: optimizing pharmacokinetics may become as important as discovering new molecular targets. The Evans Blue platform is designed to enhance the therapeutic performance of existing and next-generation targeted radiopharmaceuticals across multiple validated molecular targets. Clinical imaging and dosimetry demonstrated tumor retention for up to 15 days, approximately eight-fold greater tumor uptake , and efficient therapeutic radiation delivery while requiring only approximately 12.5% of the cumulative administered radioactivity used in conventional peptide receptor radionuclide therapy (PRRT). These findings suggest that improving pharmacokinetics through reversible albumin binding may substantially improve therapeutic efficiency while reducing the administered radioactivity required to achieve comparable tumor radiation delivery. Key clinical and preclinical findings include: Largest reported clinical dataset evaluating an albumin-binding PRRT in 81 patients with GEP-NETs. Tumor retention sustained for up to 15 days after a single administration. Approximately eight-fold greater tumor uptake and retention than conventional 177 Lu-DOTA-TATE, based on clinical dosimetry evaluations. Comparable tumor radiation dose delivery achieved using approximately 12.5% of the cumulative administered radioactivity required for conventional PRRT. Across multiple Evans Blue–enabled radiopharmaceuticals, preclinical studies demonstrated up to 35-fold greater tumor retention, than conventional 177 Lu-DOTA-TATE supporting the broad applicability of the Evans Blue platform across validated molecular targets, including SSTR2 and integrin αvβ3. In preclinical studies, 225 Ac-EBTATE demonstrated antitumor activity comparable to that observed with RayzeBio's RYZ101 while using approximately 40% of the administered radioactivity under the study conditions evaluated. 177 Lu-EBTATE demonstrated superior, dose-dependent, and durable antitumor efficacy compared with 177 Lu-DOTA-TATE in human lung adenocarcinoma and pancreatic xenograft models. 177 Lu-EBRGD combined with anti-PD-1 immunotherapy produced complete long-term survival and substantially outperformed monotherapy and sequential treatment in preclinical colorectal cancer models. Modular platform compatible with diverse radionuclides, targeting ligands, peptide classes, and both beta- and alpha-emitting therapeutic payloads, supporting broad applicability across multiple radiopharmaceutical programs. Because the Evans Blue platform functions independently of the targeting ligand, it has the potential to enhance a broad range of approved and investigational targeted radiopharmaceuticals across multiple molecular targets. Its modular design enables integration with diverse targeting ligands, radionuclides, and therapeutic payloads, providing a versatile platform for extending the lifecycle of established radiopharmaceuticals while enabling development of next-generation targeted radiotherapeutics. "Radiopharmaceutical oncology is entering a new era in which optimizing pharmacokinetics may become as important as discovering new molecular targets. Our clinical dataset from 81 patients provides what we believe is the first clinical validation of reversible albumin binding. We believe the Evans Blue platform has the potential to provide a broadly applicable pharmacokinetic enhancement platform for existing approved radiopharmaceuticals as well as next-generation therapeutic candidates across multiple validated molecular targets,” said Norman LaFrance, M.D., Chief Strategy Officer. "We believe the Evans Blue platform has the potential to redefine the development of targeted radiopharmaceuticals. Rather than replacing established radiopharmaceuticals, our strategy is to enhance the therapeutic performance of established and next-generation radiopharmaceuticals through reversible albumin binding. The Evans Blue platform is designed to increase tumor exposure, improve therapeutic efficiency, and enhance the clinical and commercial potential of both proprietary and partner radiopharmaceutical programs. Our vision is to establish Evans Blue as the foundational enabling technology powering the next generation of targeted radiopharmaceuticals through internal innovation, strategic collaborations, and licensing partnerships," said Chris Pak, Ph.D., Chairman and Chief Executive Officer. MTTI is actively seeking strategic collaborations with pharmaceutical and biotechnology companies interested in applying the Evans Blue platform to enhance approved and investigational radiopharmaceuticals through research collaborations, co-development, licensing, or other strategic partnerships. The Company welcomes discussions with partners seeking to improve the therapeutic performance of existing and next-generation targeted radiopharmaceuticals through the Evans Blue platform. About Molecular Targeting Technologies, Inc. Molecular Targeting Technologies (MTTI) is a clinical-stage biotechnology company developing the proprietary Evans Blue (EB) platform, a reversible albumin-binding technology designed to enhance pharmacokinetics, improve tumor targeting, and optimize the therapeutic performance of targeted radiopharmaceuticals. The Company's pipeline includes EB-TATE, EB-RGD, EB-FAPI, and EB-GRPR, reflecting the broad applicability of the Evans Blue platform across multiple molecular targets. For more information, visit . Forward-Looking Statements This press release contains forward-looking statements regarding the development, potential applications, and future evaluation of MTTI's Evans Blue platform and related product candidates. These statements involve risks and uncertainties that may cause actual results to differ materially from those expressed or implied. Preclinical and clinical observations may not be predictive of future clinical outcomes or regulatory decisions. MTTI undertakes no obligation to update these statements except as required by applicable law. Contacts Media Contact: Chris Pak, Ph.D., Chairman and Chief Executive Officer; Email: cpak@mtarget.com

10 Jun 2026

·www.businesswire.com

MTTI Highlights Clinical Experience in 81 GEP-NETs Patients and Differentiated Profile of Next-Generation PRRT Candidate EBTATE Following Presentation at SNMMI 2026

WEST CHESTER, Pa.--(BUSINESS WIRE)--Molecular Targeting Technologies, Inc. (MTTI), a clinical-stage radiopharmaceutical company developing next-generation albumin-binding targeted radiotherapeutics, today announced updated clinical findings from patients with gastroenteropancreatic neuroendocrine tumors (GEP-NETs) treated with its lead investigational product candidate, ¹⁷⁷Lu-DOTA-EB-TATE (EBTATE), following presentation at the 2026 Society of Nuclear Medicine and Molecular Imaging (SNMMI) Annual Meeting. The 81-patient experience represents one of the largest clinical datasets reported to date for an albumin-binding peptide receptor radionuclide therapy (PRRT) and provides growing evidence that EBTATE may offer a differentiated and potentially best-in-class profile compared with conventional PRRT approaches. Key Clinical Highlights from 81 Treated GEP-NET Patients Approximately 8-fold higher tumor uptake compared with conventional PRRT Potential two-cycle treatment regimen versus the conventional four-cycle PRRT Clinical activity achieved using only approximately 12.5% of the cumulative radioactivity administered in current standard-of-care PRRT The findings further validate MTTI's proprietary Evans Blue (EB) technology platform, which utilizes reversible albumin binding to extend circulation time, enhance tumor uptake, and increase tumor retention. Preclinical studies have demonstrated up to 26-fold higher tumor retention compared with conventional radiopharmaceutical approaches, supporting broad applicability across multiple radionuclides, targeting vectors, and tumor types. "The clinical experience in 81 patients validates both EBTATE and the broader Evans Blue platform," said Chris Pak, Chairman and Chief Executive Officer of MTTI. "By improving tumor delivery and retention while requiring only approximately 12.5% of the cumulative radioactivity administered in current standard-of-care PRRT, the platform has the potential to enhance the therapeutic index of radiopharmaceuticals across multiple cancers and with both beta- and alpha-emitting radionuclides. The combination of enhanced tumor uptake, prolonged tumor retention, favorable clinical responses, and robust safety observations supports the continued development of EBTATE and highlights the broader potential of the Evans Blue platform to improve targeted radiotherapeutics across a wide range of solid tumors." "EBTATE achieved markedly higher tumor uptake and longer tumor retention than conventional ¹⁷⁷Lu-DOTATATE while maintaining a favorable safety profile," said Lisa Bodei, MD, PhD, a nuclear medicine physician at Memorial Sloan Kettering Cancer Center and recipient of the 2026 Castle Connolly America's Top Doctor Award. "The ability to deliver higher radiation doses to tumors with significantly lower administered radioactivity highlights the potential of this albumin-binding approach to improve the therapeutic index of PRRT. This data from NET patients supports continued clinical development and further evaluation of a streamlined treatment regimen." About Molecular Targeting Technologies, Inc. Molecular Targeting Technologies, Inc. (MTTI) is a clinical-stage radiopharmaceutical company developing next-generation albumin-binding targeted radiotherapeutics for cancer. Powered by its proprietary Evans Blue (EB) technology platform, MTTI is advancing a pipeline of beta- and alpha-emitting radiopharmaceuticals designed to improve tumor targeting, increase therapeutic index, and enhance treatment efficiency. In addition to EBTATE, MTTI is developing 225Ac-EBTATE for small cell lung cancer, where preclinical studies have demonstrated comparable efficacy to 225Ac-DOTATATE at approximately 40% of the administered dose. For more information, visit www.mtarget.com. Forward-Looking Statements This press release contains forward-looking statements regarding the potential safety, efficacy, clinical benefits, development plans, and commercial opportunities of EBTATE and MTTI's Evans Blue technology platform. Actual results may differ materially from those indicated by such forward-looking statements. EBTATE is an investigational product candidate that has not been approved by the U.S. Food and Drug Administration or any other regulatory authority.

Radiation TherapyAACRClinical ResultClinical Study

100 Deals associated with 177Lu-DOTA-EB-TATE

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Thyroid Cancer, Hurthle Cell	Phase 2	United States	National Institute of Diabetes & Digestive & Kidney Diseases	16 Sep 2026
Apudoma	Phase 1	United States	Molecular Targeting Technologies, Inc.	18 Jun 2022

Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


SNMMI2026	Phase 1	Neuroendocrine Tumors somatostatin receptor (SSTR) overexpression	6	177Lu-DOTA-EB-TATE 1.85 GBq	jyjtbzwvhm(xzzohgygsg) = Hematologic toxicity was dose-limiting, with one patient in this study experiencing persistent Grade 3 febrile neutropenia at the 3.70 GBq dose level. Another patient from an external cohort also experienced a dose-limiting toxicity (DLT) at the same dose level, jxjfwzoqnx (nobiaxydwf )	Positive	27 May 2026
NCT03478358 (Pubmed \| Clin Nucl Med)	Phase 1	-	10	177Lu-DOTA-EB-TATE without amino acid infusion	sgypufbyrk(swhkmvxeko) = cknecekngi rmqfdlycgm (jvaptuhbxl ) View more	-	18 Apr 2023
				177Lu-DOTA-EB-TATE with amino acid infusion	sgypufbyrk(swhkmvxeko) = jgdnfjqkhr rmqfdlycgm (jvaptuhbxl ) View more
SNMMI2020	Not Applicable	Advanced Neuroendocrine Neoplasm	-	Group A (1.17 ± 0.09 GBq/dose)	gdbtjtugdt(myfvnyltdv) = 0.63% (1/160) occurrence in all of the performed blood tests zkgecwcrjo (bceqzxtpbj ) View more	-	15 May 2020
				Group B (1.89 ± 1.53 GBq/dose)
NCT03478358 (Treatment Using 177Lu-DOTA-EB-TATE, Pubmed \| Eur J Nucl Med Mol Imaging)	Phase 1	Neuroendocrine Tumors	-	Group A	qqkjzixlgp(tfllyarjqh) = foztjrwcvd zxdhctkrjh (tcxohphrmw )	-	01 Apr 2020
				Group C	qqkjzixlgp(tfllyarjqh) = eygxmqzjan zxdhctkrjh (tcxohphrmw )

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