Detailed Analysis of the Scope and Claims of United States Patent 10,799,506
Introduction
United States Patent 10,799,506, titled "Ribociclib tablet," is a significant patent in the pharmaceutical industry, particularly in the field of oncology. This patent, issued on October 13, 2020, pertains to the formulation, composition, and manufacturing process of ribociclib tablets, a medication used to treat certain types of breast cancer.
Inventors and Assignee
The patent was invented by Gururajan Bindhumadhavan, Arnaud Grandeury, and Rui Costa, and is assigned to Novartis AG, a global healthcare company based in Basel, Switzerland[2][3].
Scope of the Patent
Active Ingredient and Composition
The patent describes a coated pharmaceutical oral tablet that contains at least 40% of ribociclib succinate by weight. Ribociclib is a selective cyclin-dependent kinase inhibitor, specifically targeting CDK4 and CDK6, which are crucial for cell cycle progression and are often overactive in cancer cells[4].
Tablet Formulation
The tablet core of the ribociclib formulation includes ribociclib succinate along with various excipients such as crospovidone, silicon dioxide, and other inactive ingredients. The coating of the tablet is designed to ensure immediate release of the active ingredient[1].
Claims of the Patent
Immediate Release Profile
One of the key claims of the patent is the immediate release profile of the ribociclib tablets. These tablets are designed to release at least 75% of the active ingredient within 45 minutes under standard dissolution test conditions. This is achieved using a rotating basket at 100 rpm with 900 ml of HCl at pH 1 or pH 2 as the dissolution medium at 37°C[1].
Physical Form and Stability
The patent emphasizes the physical form and stability of the tablets. The formulation has very good process performance and high stability, ensuring consistent and reliable drug delivery[1].
Patent Landscape
Related Patents and Exclusivity
The patent landscape surrounding ribociclib includes several related patents that cover various aspects of the compound and its uses. For example, patents such as 8,324,225 and 9,416,136 describe pyrrolopyrimidine compounds and their uses in treating proliferative diseases, including cancer. These patents highlight the broader scope of ribociclib and its derivatives in therapeutic applications[2].
Patent Expiration Dates
The patent 10,799,506 is part of a larger patent portfolio that includes several expiration dates. Key patents related to ribociclib are set to expire between 2028 and 2031, which will impact the exclusivity period for Novartis AG. For instance, the patent 9,416,136 expires on August 20, 2029, while another patent (9,193,732) expires on November 9, 2031[2].
Competitive Landscape
The patent landscape indicates a competitive environment with multiple players involved in the development and manufacturing of similar compounds. The expiration of these patents will open up opportunities for generic versions of ribociclib, potentially altering the market dynamics[2].
Manufacturing Process
The patent details the manufacturing process of the ribociclib tablets, including the preparation of the tablet core and the application of the coating. This process ensures the uniform distribution of the active ingredient and the stability of the final product[1].
Clinical and Therapeutic Implications
Ribociclib is used in combination with other therapies to treat advanced or metastatic breast cancer. The immediate release formulation described in the patent enhances the bioavailability and efficacy of the drug, making it a critical component in cancer treatment regimens[4].
Regulatory Aspects
The patent is compliant with regulatory standards, including those set by the USP (United States Pharmacopeia). The dissolution tests mentioned in the patent are standard procedures to ensure the quality and performance of the tablets[1].
Conclusion
United States Patent 10,799,506 is a significant contribution to the field of oncology, providing a stable and effective formulation of ribociclib. The patent's claims and scope highlight the innovative approach to drug delivery and the importance of immediate release formulations in cancer treatment.
Key Takeaways
- Active Ingredient: Ribociclib succinate, a selective cyclin-dependent kinase inhibitor.
- Formulation: Coated pharmaceutical oral tablet with immediate release profile.
- Stability and Performance: High stability and good process performance.
- Dissolution Profile: Releases at least 75% of the active ingredient within 45 minutes.
- Patent Expiration: Part of a larger patent portfolio with expiration dates between 2028 and 2031.
- Therapeutic Use: Used in treating advanced or metastatic breast cancer.
FAQs
Q: What is the primary use of ribociclib?
A: Ribociclib is primarily used to treat certain types of breast cancer by inhibiting cyclin-dependent kinases CDK4 and CDK6.
Q: What is the significance of the immediate release profile in the patent?
A: The immediate release profile ensures that at least 75% of the active ingredient is released within 45 minutes, enhancing the bioavailability and efficacy of the drug.
Q: Who is the assignee of the patent?
A: The patent is assigned to Novartis AG, a global healthcare company based in Basel, Switzerland.
Q: What are the key excipients mentioned in the patent?
A: The patent mentions crospovidone and silicon dioxide among other inactive ingredients.
Q: When does the patent expire?
A: The patent is part of a larger portfolio, but key related patents expire between 2028 and 2031.
Cited Sources
- US10799506B2 - Ribociclib tablet - Google Patents
- Generic Kisqali Availability - Drugs.com
- Ribociclib tablet - Justia Patents
- Ribociclib: Uses, Interactions, Mechanism of Action | DrugBank Online
