EN
IT

The theragnostic radiopharmaceutical is structurally related to the neurotransmitter norepinephrine which, because of this similarity, is the substrate of the axonal norepinephrine transporter (NET). Depending on the specific radiometal incorporated, this radiopharmaceutical can be potentially useful both as a tracer for the surgical removal guided by beta minus radiation and for diagnostic imaging and radiometabolic therapy of the neuroendocrine tumors that over-express the NET (pheochromocytomas, paragangliomas, neuroblastomas, etc.).

Patent status

SUBMITTED

Priority Number

102019000000202

Priority Date

08/01/2019

License

INTERNATIONAL

Problem

Radiotracers are medicines that include one or more radioisotopes capable of emitting radiation. For this reason they are used in the surgical removal of tumors driven by the radiation emitted that serve to discriminate the cancerous tissue from the surrounding healthy organs, improving the process of tumor removal.
The problem and the major limit of the current radio-guided surgery is represented by the high penetration power of gamma rays (γ), the only ones until now used for such application.

Since these can pass through large amounts of tissue, any possible radio-pickingtracer γ emitter by healthy tissues adjacent to the tumor lesion may result in a not negligible background radiation which very often may preclude or render ineffective the application of the technique. For the same reason, medical personnel may be exposed to a large dose of radiation, unless a very low dose of radiotracer is administered, often compromising the effectiveness of the approach.

Radio-guided surgery with γ radiation cannot therefore be applied to most cancers.

Current Technology Limitations

Although γ-guided radio surgery is widely validated, current clinical applications of this technique are limited to colon cancer, sentinel lymph node identification in malignant melanoma and breast cancer, the identification of parathyroid adenoma and some bone tumors. In fact, all pediatric and abdominal cancers of adults are currently excluded due to the limited distance between the organs or the high uptake by the excretory organs located in the abdominal cavity.

Among the tumors for which until now radio-guided surgery by tracers γ has been substantially ineffective include neuroendocrine tumors over-expressing the transporter of norepinephrine (NET) such as pheochromocytomas, neuroblastomas, paragangliomas, etc.

Killer Application

Indicate the starting application from which to develop a potential business related to the patent (if available or the team has already developed / is developing an idea related to the development of a project related to a concrete application in view of patent enhancement)

The initial application of the radio pharmaceuticals described in the patent is radio-guided surgery of abdominal relapses or metastases of pheochromocytomas.

Our Technology and solutions

The inventive activity gave rise to a teragnostic Radiofarmaco (RF) structurally attributable to the norepinephrine neurotransmitter which, by virtue of this similarity, appears to be substrate of the axonal transporter of norepinephrine (NET). Depending on the specific embedded metal radionuclide, RF can be useful as tracer for surgical removal guided by beta minus radiation and for diagnostic imaging (PET and SPECT) and radiometabolic therapy of hyper-secreting neuroendocrine tumors catecholamines that overexpress NET (pheochromocytomas, paragangliomas, neuroblastomas, etc.).

The RF consists of 4 main portions: a pharmacophoric group that Mima the neurotransmitter norepinephrine and that contributes to make RF a preferential substrate of the NET, a connecting portion to which is linked a bifunctional chelating group, and finally a radioactive trivalent metal cation. RF can be picked up preferentially by cancer cells that overexpress the NET, has low intrinsic toxicity and high metabolic stability.

Advantages

If marked with the pure emitter β- 90Y3+, exploiting the low penetration power of the emission β- compared to photons γ, allows to extend the field of application of radio-guided surgery (RGS) to tumors NET positive exceeding the limits of the current "gold standard", the emitter γ Meta-iodobenzuanidine (MIBG);
Simplified, fast and low cost preparation procedure;
It can be formulated in very effective preparations despite low specific activity;
Multiple theragnostic applications for tumors that overexpress the NET.

Roadmap

The radio pharmaceuticals described in patent no. 102019000000202 of 08.01.2019 if marked with an emitter beta minus which yttrium 90 has the potential to determine a paradigm shift in radioguided surgery of neuroendocrine tumors hyper-secreting catecholamines (positive NET).

The first step to be taken (manageable by a small-medium company in the biotechnology-pharmaceutical sector) is to complete the preclinical studies and prepare the documentation to be submitted to the regulatory bodies for the attribution of the status of Investigational New Drug.

A more important business entity will then have to intervene to cover the costs of the clinical development phase.

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Basic Principles
Basic principles tested
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Formulation
Technology concept formulated
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Proof of concept
Experimental proof of concept
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Laboratory Prototype
Technology validated in lab
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Prototype tested on pilot-scale/large-scale
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Commercial prototype
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Real world validation
System prototype demonstration in operational/real-world environment
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First complete and commercial product
System complete and qualified
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Full commercial application
Actual system proven in commercial environment (competitive manufacturing in the case of key enabling technologies; or in space)

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The team

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