MTTI obtains FDA allowance of Investigational New Drug (IND) for Hürthle Cell Thyroid Cancer

evathera on December 12, 2022

FOR IMMEDIATE RELEASE

West Chester, PA December 8, 2022, 6:01 am Eastern Standard Time (Business Wire)
— Molecular Targeting Technologies, Inc. (MTTI), a clinical stage radiopharmaceutical
therapy company focused on therapies for rare diseases, announced today the allowance of an Investigational New Drug (IND) application by the U.S. Food and Drug Administration (FDA). It is now waiting for Institutional Review Board (IRB) approval. Once approved by IRB, it will enable a Phase I/II clinical study of the Safety, Dosimetry and Efficacy of EBTATE in adult patients with metastatic, radioactive iodine nonresponsive Hürthle cell thyroid cancer.”

EBTATE is a new generation of peptide receptor radiotherapeutic drug that has demonstrated potential clinical superiority over standard of care. It selectively binds to somatostatin receptor 2 (SSTR2) on neuroendocrine and other tumors, which are then killed by the radionuclide. EvaThera platform products were designed to bind to serum albumin, due to the Evans blue moiety, extending in vivo residence time, enabling lower, less frequent dosing of the radiopharmaceutical and reducing risk of renal injury vs. the current standard of care.

Dr. Joanna Klubo-Gwiezdzinska, MD, Ph.D, MHSc, acting section chief of Thyroid Tumors and Functional Thyroid Disorders in the National Institute of Diabetes and Digestive and Kidney Diseases, part of the National Institutes of Health (NIH) and study author commented: “Hürthle cell thyroid cancer, which currently lacks effective treatment options, is characterized by a particularly high expression of SSTR2*. With this phase I/II clinical trial, we hope to implement individualized dosimetry-based dosing for each patient with Hürthle cell thyroid cancer that spread outside of the thyroid gland and analyze how much of an active agent is being accumulated in the tumor tissue to establish a threshold associated with the best efficacy and safety.”

Dr. Chris Pak, President & CEO of MTTI commented: “The clearance of our IND is an important milestone for MTTI. Having solidified our clinical trial preparedness and manufacturing readiness, we are well-positioned to advance EBTATE to target Hürthle cell thyroid cancer.”

About Molecular Targeting Technologies, Inc. (MTTI)

Molecular Targeting Technologies, Inc., is a privately held, rapidly growing, well financed, clinical-stage biotech company developing next-generation targeted radiotherapeutics and diagnostics for rare cancers. Evathera platform technology product has shown application for glioblastoma multiforme (GBM) cancer patients overexpressing integrin. MTTI is committed to building value by acquiring and translating innovative imaging, radiopharmaceutical and theranostics assets to improve human health, reduce healthcare costs and reward stakeholders. MTTI expects to be orchestrating multiple clinical trials in 2023. For more information: www.evathera.com

Contact : NIDDK, Email : niddkmedia@niddk.nih.gov
MTTI, Chris Pak, Email: cpak@mtarget.com

See* below:
Thakur S and Klubo-Gwiezdzinska J et al. 177Lu-DOTA-EB-TATE, A Radiolabeled Analog of
Somatostatin Receptor Type 2, for the Imaging and Treatment of Thyroid Cancer. Clin Cancer.

The content in this release is the sole responsibility of the authors and does not necessarily represent the official views or imply endorsement of the National Institutes of Health.

MTTI Receives Chinese Patent for EVATHERA Technology

evathera on December 12, 2022

FOR IMMEDIATE RELEASE

West Chester, Pennsylvania, December 6, 2022 — Molecular Targeting Technologies, Inc. (MTTI) announces the issuance of Chinese Patent CN109153641B covering MTTI’s lead radiotherapeutic product, EBTATE™ and others in its EvaThera™ platform. Approval of “Chemical conjugates of Evans blue derivatives and their use as radiotherapeutic and imaging agents” follows issued patents in the US, Europe, Singapore, and Japan this past year.

EBTATE is a new generation of peptide receptor radiotherapeutic drug that has demonstrated potential clinical superiority over standard of care. It selectively targets and binds to somatostatin receptor 2 on neuroendocrine and other tumors, which are then killed by the radionuclide. EvaThera platform products were designed to bind to serum albumin, due to the Evans blue moiety, extending in vivo residence time, enabling lower, less frequent dosing of the radiopharmaceutical and reducing risk of renal injury vs. the current standard of care.

Our recent 3-year follow-up report on a 30-patient, ex-US, EBTATE study showed stable
disease with progression-free survival of 43 months after three cycles of EBTATE. EBTATE
treatment is effective and less toxic for neuroendocrine tumor patients.

Chris Pak, MTTI’s President & CEO, commented, “This complements our IP portfolio, further
protecting our EvaThera platform.” He added, “We’re continuing to bolster our position in
radiotheranostics with planned clinical trials of our two platform products in multiple indications.”

About Molecular Targeting Technologies, Inc. (MTTI)

Molecular Targeting Technologies, Inc., is a privately held, rapidly growing, well financed, clinicalstage biotech company developing next-generation targeted radiotherapeutics and diagnostics for rare cancers. We are committed to building value by acquiring and translating innovative imaging, radiopharmaceutical and theranostics assets to improve human health, reduce healthcare costs and reward stakeholders. MTTI expects to be orchestrating multiple clinical trials in 2023. For more information: www.evathera.com

Contact: Chris Pak, Email: cpak@mtarget.com

See* below:
https://www.snmmi.org/NewsPublications/NewsDetail.aspx?ItemNumber=36701

MTTI doses first patient in EBTATE neuroendocrine tumor clinical trial

evathera on June 29, 2022

Molecular Targeting Technologies, Inc. (MTTI), announced that the first patient has been dosed in a clinical trial of EBTATE

West Chester, PA, June 29, 2022 — Molecular Targeting Technologies, Inc. (MTTI),
announced that the first patient has been dosed in a clinical trial of EBTATE (177Lu-DOTA-EB-
TATE) for the treatment of patients with advanced, well differentiated neuroendocrine tumors. This US based, Phase I clinical trial will evaluate the safety and dosimetry of EBTATE.

EBTATE is a patented peptide targeting radiotherapeutic drug. It selectively targets and binds
to somatostatin receptor 2 on neuroendocrine tumors, which are then killed by the radionuclide. EBTATE was designed to bind to serum albumin, extending in vivo residence time, enabling lower, less frequent dosing of the radiopharmaceutical vs. the current standard of care. Early, ex.-US, clinical results in 60 patients showed EBTATE is more effective and safer for neuroendocrine tumor patients*.

Chris Pak, President & CEO of MTTI comments “This is a substantive milestone for MTTI. It
marks the advent of safer, more effective, economical targeted radiotherapy drugs for
neuroendocrine tumors. Recent clinical data presented at the 2022 SNMMI meeting also
suggests that EBTATE treatment without the conventional amino acids infusion is safe and does no harm to kidney function, potentially, significantly improving patient comfort vs current treatments.”

About Molecular Targeting Technologies, Inc. (MTTI)

Molecular Targeting Technologies, Inc. is a privately held, rapidly growing, well financed, clinical stage biotech developing next-generation targeted radiotherapeutics and diagnostics for rare cancers. We are committed to building value by acquiring and translating innovative imaging, radiopharmaceutical and theranostic assets to improve human health, reduce healthcare costs and reward stakeholders. MTTI expects to be orchestrating multiple clinical trials in 2022. For more information: www.evathera.com

Contact: Chris Pak, Email: cpak@mtarget.com

See* below:
https://www.snmmi.org/NewsPublications/NewsDetail.aspx?ItemNumber=36701

SNMMI 2022 Accepted Oral Abstract: EBTATE safety with and without Amino Acid Infusion

evathera on June 29, 2022

Evaluation of Safety, Biodistribution and Dosimetry of a long-Acting Radiolabeled Somatostatin Analogue 177Lu-DOTA-EB-TATE with and without Amino Acid Infusion

Synopsis:

Evaluation of Safety, Biodistribution and Dosimetry of a long-Acting Radiolabeled Somatostatin Analogue 177Lu-DOTA-EB-TATE with and without Amino Acid Infusion.


Qingxing Liu, Peking Union Medical College Hospital (Primary Presenter); Yuanyuan Jiang, Peking Union Medical College Hospital Koon Pak, Molecular Targeting Tech. Inc
Guochang Wang, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Peking Union Medical Colleg Jingjing Zhang; Xiaoyuan Chen, NUS Zhaohui Zhu, Peking Union Medical College Hospital.

Purpose/Background:

Kidneys are considered one of the dose-limiting organs in peptide receptor radionuclide therapy (PRRT), especially when using 90Y-PRRT. Amino acid was infused to reduce renal absorbed dose by inhibiting the proximal tubular reabsorption of the radiopeptide. However, due to the lower penetration range of β- particles emitted by 177Lu, the renal dysfunction caused by 177Lu-PRRT is rare. An Evans blue-modified 177Lu-labeled octreotate (177Lu-DOTA-EB-TATE) have an extended circulation in the blood, making little protective effect of amino acids on the kidneys. The aim of this prospective study was to evaluate the safety, biodistribution and dosimetry of 177Lu-DOTA-EB-TATE with and without amino acid infusion. .Kidneys are considered one of the dose-limiting organs in peptide receptor radionuclide therapy (PRRT), especially when using 90Y-PRRT. Amino acid was infused to reduce renal absorbed dose by inhibiting the proximal tubular reabsorption of the radiopeptide. However, due to the lower penetration range of β- particles emitted by 177Lu, the renal dysfunction caused by 177Lu-PRRT is rare. An Evans blue-modified 177Lu-labeled octreotate (177Lu-DOTA-EB-TATE) have an extended circulation in the blood, making little protective effect of amino acids on the kidneys. The aim of this prospective study was to evaluate the safety, biodistribution and dosimetry of 177Lu-DOTA-EB-TATE with and without amino acid infusion.

Methods:

A total of 10 advanced metastatic neuroendocrine tumors were recruited and were randomly divided into 2 groups: group A (n=5, Male/Female=3/2, mean age 43±7 years old) received a single dose 3.9±0.2 GBq (105.6±4.6 mCi) of 177Lu-DOTA-EB-TATE without amino acid infusion; group B (n=5, Male/Female=3/2, mean age 56±8 years old) received a single dose 3.3±0.1 GBq (88.5±2.6 mCi) of 177Lu-DOTA-EB-TATE with amino acid infusion (25g lysine+25g arginine diluted in 2L of normal saline infused over 4 h, starting 30–60 min before PRRT). All patients underwent serial whole body planar at 1, 24, 96, 168h after administration and underwent single-photon emission computed tomography (SPECT) at 24h after administration. Abdominal CT was performed 2 days before administration for SPECT/CT image fusion. Hematological parameters, liver and renal function (creatinine and BUN) at baseline, 1 week and 4 weeks after administration were tested. 99mTc-DTPA dynamic renal imaging used for determination of the GFR was performed at baseline and 8 weeks after administration. Treatment-related adverse events were graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE), version 5.0. Dosimetric calculations were done using the HERMES software (HERMES Medical Solutions, Stockholm, Sweden).

Results:

Administration of 177Lu-DOTA-EB-TATE with/without amino acid was well tolerated, with no CTC-3/4 hematotoxicity, hepatotoxicity or nephrotoxicity being recorded. In group A, no significant difference was observed in creatinine (t=0.485, P=0.653), BUN (t=0.585, P=0.590) or GFR (t=0.741, P=0.512). In group B, no significant difference was observed in creatinine, BUN or GFR as well. The total body effective dose has no significant difference between group A and B (0.222±0.100 vs 0.105±0.014 mSv/MBq, P=0.279) as well as kidney effective dose (2.013±0.808 vs 0.622±0.117 mSv/MBq, P=0.127). The residence time of the kidneys was 6.6±2.5h in group A and 2.1±0.4h in group B (P=0.113).

Conclusion:

177Lu-DOTA-EB-TATE without amino acid infusion is safe, with no kidney dysfunction being occurred. It could not only greatly simplify the PRRT procedure, but also avoid amino acid-related side effects.

MTTI features EBTATE advances at the 2022 SNMMI meeting in Vancouver, BC

evathera on June 9, 2022

West Chester, PA, June 9, 2022 — Molecular Targeting Technologies, Inc. (MTTI), a clinical stage oncology company, will highlight advances on its EvaTheraTM radiotheranostics platform at the Society of Nuclear Medicine and Molecular Imaging (SNMMI) meeting in Vancouver, BC, on June 11-15, 2022 (Exhibit booth #1715).  The EvaThera platform includes  EBTATETM (177Lu-DOTA-EB-TATE) for Neuroendocrine Neoplasms (NENs), Hürthle cell thyroid and nasopharyngeal cancers and EBRGDTM (177Lu-DOTA-EB-RGD)  for glioblastoma multiforme and non-small cell lung cancer.

A video featuring the EBTATE story (see link below) will be released at the meeting. 

In addition, two abstracts highlighting MTTI’s EBTATE & our PET imaging agent,18F-glucarate, were selected for oral and poster presentations:

  • Evaluation of Safety, Biodistribution and Dosimetry of a long-Acting Radiolabeled Somatostatin Analogue 177Lu-DOTA-EB-TATE with and without Amino Acid Infusion by Qingxing Liu, Yuanyuan Jiang, Koon Pak, Guochang Wang, Jingjing Zhang, Xiaoyuan Chen and Zhaohui Zhu (oral presentation).
    EBTATE treatment without amino acid  infusion, normally used in current treatments to block drug impact on non-target organs, has acceptable, minor effects on the kidneys and does no harm to kidney function.  EBTATE may significantly improve patient comfort vs. current treatments.
  • Assessment of 18F-glucarate as a potential PET tracer for cancer imaging by Junling Li, Huaiyu Zheng, Levi Beverly, Brian Gray, Koon Pak and Chin K. Ng (poster presentation).
    18F-glucarate uptake in both in vitro and in vivo correlated well with the degree of cell death and shows early tumor response to chemotherapy, enabling faster assessment of treatment efficacy.

About MTTI

MTTI is a privately held, rapidly growing, well financed, clinical stage biotech developing targeted radiotherapeutics and diagnostics for rare cancers. We are committed to building value by acquiring and translating innovative imaging, radiopharmaceutical and theranostic assets to improve human health, reduce healthcare costs and reward stakeholders. MTTI expects to be orchestrating multiple clinical trials in 2022. For more information: www.mtarget.com; www.evathera.com 

Contact: Chris Pak, Email: cpak@mtarget.com