United States Patent 10,584,113: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 10,584,113, titled "Methylphenidate-prodrugs, processes of making and using the same," is a significant patent in the field of pharmaceuticals, particularly for the treatment of attention deficit hyperactivity disorder (ADHD). This patent, assigned to KemPharm, Inc., introduces innovative prodrug compositions and methods related to methylphenidate.
Background
Methylphenidate is a well-known stimulant medication used to treat ADHD and certain other conditions. The development of prodrugs, which are inactive compounds that undergo metabolic conversion in the body to release the active drug, has been a focus for improving the efficacy, safety, and patient compliance of methylphenidate treatments.
Scope of the Patent
Prodrug Compositions
The patent describes compositions comprising d-threo-methylphenidate conjugates and unconjugated methylphenidate. These prodrugs are designed to be metabolized in the body to release the active methylphenidate, providing a controlled and sustained release profile. The prodrugs can be conjugated to various moieties such as alcohols, amines, oxoacids, and thiols, or their derivatives, often with the inclusion of linkers[2][5].
Synthesis and Manufacturing
The patent outlines detailed processes for the synthesis of these methylphenidate prodrugs. This includes methods for conjugating methylphenidate to the aforementioned moieties and the use of specific linkers to enhance stability and bioavailability[2].
Therapeutic Applications
The primary therapeutic application of these prodrugs is the treatment of ADHD. However, the patent also suggests potential uses in other diseases or disorders where methylphenidate or its derivatives could be beneficial[2][5].
Claims of the Patent
Composition Claims
The patent includes claims related to the composition of matter of the methylphenidate prodrugs. These claims cover the specific chemical structures of the prodrugs, including the types of conjugates and linkers used[2].
Method of Use Claims
In addition to composition claims, the patent also includes method of use claims. These claims cover the administration and dosing regimens for the prodrugs, as well as their use in treating specific conditions like ADHD[2].
Dosage Forms
The patent claims various dosage forms of the prodrugs, including tablets, capsules, and other formulations designed to optimize the delivery and bioavailability of the active drug[1][2].
Patent Landscape
Related Patents
KemPharm, Inc. has a series of related patents that complement and expand upon the technology described in US 10,584,113. These include patents such as US 10,759,778 and US 10,954,213, which also pertain to methylphenidate prodrugs and their methods of synthesis and use[2].
Patent Expiration Dates
The patent is set to expire on July 27, 2032, providing KemPharm, Inc. with exclusive rights to the technology until that date. This exclusivity period is crucial for protecting the intellectual property and market position of AZSTARYS, a product that utilizes this prodrug technology[2].
Orange Book Listing
The patents covering the composition of matter and method of use for serdexmethylphenidate (SDX), the primary active pharmaceutical ingredient in AZSTARYS, have been listed in the FDA's Orange Book. This listing confirms the New Chemical Entity (NCE) status of SDX, granting five years of market exclusivity[5].
Impact on the Market
AZSTARYS and Its Significance
AZSTARYS, conditionally approved by the FDA in March 2021, is a once-daily product for treating ADHD. It combines SDX, a prodrug of d-methylphenidate, with immediate-release d-methylphenidate. This formulation leverages the prodrug technology described in the patent to offer improved pharmacokinetics and patient compliance[5].
Competitive Advantage
The exclusive rights granted by this patent and its related patents provide KemPharm, Inc. with a significant competitive advantage. The absence of therapeutically equivalent generic versions of AZSTARYS in the U.S. market ensures that KemPharm can maintain market dominance for the duration of the patent exclusivity period[2].
Future Directions and Opportunities
Expanding Therapeutic Indications
The prodrug technology described in the patent has potential applications beyond ADHD. KemPharm is exploring the use of similar prodrugs for other CNS disorders and conditions, such as stimulant use disorder (SUD) and idiopathic hypersomnia (IH)[5].
Patent Analytics and Management
Effective management of the patent portfolio, including tracking claims and scope concepts, is crucial for maintaining and expanding intellectual property protection. Tools like ClaimScape® software can help in analyzing and managing large numbers of patent claims efficiently[3].
Key Takeaways
- Innovative Prodrug Technology: The patent introduces novel prodrug compositions of methylphenidate, enhancing its therapeutic profile.
- Exclusive Rights: The patent and related patents provide KemPharm, Inc. with exclusive rights until 2032, protecting AZSTARYS from generic competition.
- Market Impact: AZSTARYS, leveraging this technology, offers improved treatment options for ADHD patients.
- Future Potential: The prodrug technology has potential applications in other CNS disorders.
FAQs
What is the primary active ingredient in AZSTARYS?
The primary active ingredient in AZSTARYS is serdexmethylphenidate (SDX), a prodrug of d-methylphenidate[5].
What is the significance of the Orange Book listing for SDX?
The Orange Book listing confirms the NCE status of SDX, granting five years of market exclusivity and protecting AZSTARYS from generic competition[5].
What are the potential future applications of the prodrug technology described in the patent?
The prodrug technology has potential applications in other CNS disorders, including stimulant use disorder (SUD) and idiopathic hypersomnia (IH)[5].
How does the prodrug technology improve the therapeutic profile of methylphenidate?
The prodrug technology provides a controlled and sustained release profile, enhancing the efficacy and patient compliance of methylphenidate treatments[2].
When is the patent set to expire?
The patent is set to expire on July 27, 2032[2].
Cited Sources:
- US10584113B2 - Methylphenidate-prodrugs, processes of making and using the same - Google Patents
- Generic Azstarys Availability - Drugs.com
- Patent Analytics | Intellectual Property Law - Schwegman
- Dexmethylphenidate: Uses, Interactions, Mechanism of Action - DrugBank
- KemPharm, Inc. Announces Orange Book Listing for Six Patents Covering Serdexmethylphenidate (SDX) and Confirmation of NCE Status - KemPharm
