Stable, Concentrated Radionuclide Complex Solutions: A Detailed Analysis of US Patent 10,596,278
Introduction
The United States Patent 10,596,278, issued on March 24, 2020, is a significant innovation in the field of radiopharmaceuticals. This patent, assigned to Advanced Accelerator Applications (Italy) S.R.L., pertains to the development of stable, concentrated radionuclide complex solutions. Here, we delve into the scope, claims, and patent landscape surrounding this invention.
Scope of the Invention
High Concentration and Stability
The patent focuses on radionuclide complex solutions that are characterized by their high concentration and chemical stability. These solutions are designed for use as drug products in diagnostic and therapeutic applications, particularly in the field of nuclear medicine[1][2][4].
Targeted Drug Delivery
A key aspect of this invention is the concept of targeted drug delivery. The radionuclides are designed to bind to specific cell receptors that are overexpressed in target cells, such as tumor cells, while leaving non-target cells unaffected. This targeted approach enhances the efficacy and safety of the treatment[1].
Claims of the Patent
Composition of the Solution
The patent claims a pharmaceutical aqueous solution that includes:
- A radionuclide complex with high chemical and radiochemical stability.
- At least one stabilizer to prevent radiolytic degradation.
- The stabilizer(s) present in a total concentration of at least 0.2 mg/mL, with preferred concentrations ranging from 0.5 mg/mL to 2.7 mg/mL[1][2].
Manufacturing Process
The claims also detail the manufacturing process, which involves introducing stabilizers at different stages to ensure high stability. The use of two stabilizers is highlighted as particularly advantageous[1][2].
Stability and Shelf Life
The solution must maintain at least 95% chemical and radiochemical stability over 72 hours at 25°C and even under short-term elevated temperature conditions. This stability ensures a shelf life of at least 3 days, facilitating centralized pharmaceutical production and distribution[1].
Patent Landscape
Assignee and Inventors
The patent is assigned to Advanced Accelerator Applications (Italy) S.R.L., with inventors including Francesco de Palo, Lorenza Fugazza, Donato Barbato, Maurizio Mariani, Daniela Chicco, Giovanni Tesoriere, and Clementina Brambati[2].
Patent Expiration Dates
The patent is set to expire on July 25, 2038, providing the assignee with exclusive rights for nearly two decades from the date of issuance[2].
Related Patents
Several related patents, such as US Patent 10,596,276 and US Patent 11,904,027, also pertain to stable, concentrated radionuclide complex solutions. These patents share similar claims and focus on improving the stability and manufacturing process of these solutions[2][4].
Industrial Scale Production
Centralized Production
The invention enables centralized pharmaceutical production at industrial scale, adhering to the highest quality standards (e.g., cGMP). This allows for the production of large batch sizes, such as 74 GBq or 148 GBq, which can be divided into numerous dose units for treating multiple patients simultaneously[1].
Clinical Applications
Treatment of Neuroendocrine Tumors (NET)
The patent specifically mentions the use of these radionuclide complex solutions for the treatment of neuroendocrine tumors (NET) in human patients. The solution is administered intravenously, allowing for high doses to be delivered within a short time frame, typically 20-30 minutes[1].
Advantages
Absence of Ethanol
The solution does not require the presence of ethanol, which enhances its physiological tolerability and makes it more suitable for patient use[1].
High Dose Administration
The high concentration of the solution allows for the administration of high doses in small volumes, which is a significant advantage in clinical settings[1].
Analytical Tools for Patent Landscape
Patent Analytics
To understand the full scope of the patent landscape, tools like patent analytics can be employed. These tools help in tracking patents by claims and scope concepts, identifying gaps or opportunities, and analyzing large numbers of patent claims concurrently[3].
Conclusion
US Patent 10,596,278 represents a significant advancement in the development of stable, concentrated radionuclide complex solutions for diagnostic and therapeutic purposes. The invention's focus on high stability, targeted drug delivery, and industrial-scale production makes it a valuable asset in the field of radiopharmaceuticals.
Key Takeaways
- High Concentration and Stability: The patent ensures high chemical and radiochemical stability of radionuclide complex solutions.
- Targeted Drug Delivery: The solutions are designed to target specific cell receptors, enhancing treatment efficacy and safety.
- Manufacturing Process: The use of stabilizers at different stages ensures high stability.
- Industrial Scale Production: Centralized production adheres to high quality standards and facilitates large batch sizes.
- Clinical Applications: The solution is particularly useful for treating neuroendocrine tumors (NET).
FAQs
What is the primary focus of US Patent 10,596,278?
The primary focus is on the development of stable, concentrated radionuclide complex solutions for diagnostic and therapeutic purposes.
Who is the assignee of this patent?
The patent is assigned to Advanced Accelerator Applications (Italy) S.R.L.
What is the significance of the stabilizers in this invention?
The stabilizers prevent radiolytic degradation, ensuring high chemical and radiochemical stability of the radionuclide complex solutions.
How does the solution facilitate targeted drug delivery?
The solution is designed to bind to specific cell receptors overexpressed in target cells, such as tumor cells, while leaving non-target cells unaffected.
What is the expected shelf life of the solution?
The solution has a shelf life of at least 3 days, ensuring it can be manufactured centrally and distributed widely.
Why is the absence of ethanol in the solution advantageous?
The absence of ethanol enhances the physiological tolerability of the solution, making it more suitable for patient use.
Sources
- US10596278B2 - Stable, concentrated radionuclide complex solutions - Google Patents
- Generic Lutathera Availability - Drugs.com
- Patent Analytics - SLWIP
- US11904027B2 - Stable, concentrated radionuclide complex solutions - Google Patents
