Details for Patent: 9,616,028

Which drugs does patent 9,616,028 protect, and when does it expire?

Patent 9,616,028 protects QTERNMET XR and XIGDUO XR and is included in two NDAs.

Protection for XIGDUO XR has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has thirty-six patent family members in nineteen countries.

Summary for Patent: 9,616,028

Title:	Bilayer tablet formulations
Abstract:	The present invention relates to bilayer tablet formulations comprising metformin extended release (XR) or reduced mass metformin XR formulation as the first layer, an SGLT2 inhibitor formulation as the second layer, and optionally a film coating. The present invention provides methods of preparing the bilayer tablet formulations and methods of treating diseases or disorders associated with SGLT2 activity employing the bilayer tablet formulations.
Inventor(s):	Abebe; Admassu (Princeton, NJ), Martin; Kyle (Princeton, NJ), Patel; Jatin M. (Princeton, NJ), Desai; Divyakant (Princeton, NJ), Timmins; Peter (Moreton, GB)
Assignee:	AstraZeneca AB (Sodertalje, SE) AstraZeneca UK Limited (London, GB)
Application Number:	14/706,077
Patent Claim Types: see list of patent claims	Formulation; Compound; Dosage form;

United States Patent 9,616,028: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 9,616,028, hereafter referred to as the '028 patent, is a significant patent related to the pharmaceutical composition and formulation of dapagliflozin and metformin hydrochloride extended-release tablets. This patent is crucial for understanding the intellectual property landscape surrounding these diabetes treatments.

Patent Overview

The '028 patent, titled "Bilayer tablet formulations," was issued on April 11, 2017. It is owned by AstraZeneca AB and is listed in the FDA's Orange Book for the drug product Xigduo XR, which combines dapagliflozin and metformin hydrochloride[2][5].

Patent Claims

The '028 patent primarily focuses on the formulation and composition of bilayer tablets containing dapagliflozin and metformin hydrochloride. The claims include:

• Bilayer Tablet Formulations: The patent describes specific formulations where the active ingredients are distributed in two distinct layers within the tablet. This design ensures controlled release of the drugs, enhancing their efficacy and patient compliance[2][5].

• Pharmaceutical Compositions: The claims cover various pharmaceutical compositions that include dapagliflozin and metformin hydrochloride, along with other excipients and ingredients necessary for the bilayer tablet formulation[5].

Patent Scope

The scope of the '028 patent is defined by its claims, which are narrowly focused on the specific formulation and composition of the bilayer tablets. Here are some key aspects:

• Specific Formulation: The patent protects the unique bilayer design, ensuring that only the patent holder can manufacture and market this specific formulation until the patent expires[2].

• Exclusivity: The '028 patent includes a pediatric exclusivity extension, which adds six months to the patent term, extending its expiration date to May 12, 2031[1][4].

Patent Expiration

The '028 patent is set to expire on May 12, 2031, inclusive of the pediatric exclusivity extension. This expiration date is critical for generic manufacturers, as it marks the earliest date they can seek approval to market generic versions of the drug without infringing on AstraZeneca's patent rights[1][4].

Patent Landscape

The '028 patent is part of a broader patent landscape surrounding dapagliflozin and metformin hydrochloride extended-release tablets. Here are some key patents in this landscape:

• US7919598: This patent, expiring in December 2029, covers the crystal structures of SGLT2 inhibitors and processes for preparing them. It is another critical patent in the portfolio protecting the active ingredient dapagliflozin[1][2].

• US685934: Expiring on May 26, 2030, this patent covers compounds and methods for treating diabetes and related diseases, further protecting the intellectual property around dapagliflozin/metformin hydrochloride formulations[2][5].

• Expired Patents: Patents such as US6414126 and US6515117, which expired in October 2020, previously protected other aspects of the drug, including earlier formulations and methods of preparation[1][2].

Litigation and Enforcement

The '028 patent has been involved in litigation to protect AstraZeneca's intellectual property rights. For instance, AstraZeneca has filed patent infringement suits against generic manufacturers like Apotex Inc. and Apotex Corp., alleging that their ANDA filings infringe on the '028 patent among others[5].

Impact on Generic Manufacturers

The '028 patent, along with other related patents, creates a significant barrier for generic manufacturers seeking to enter the market. Generic companies must either wait for the patent to expire or challenge the patent through litigation or other means to gain approval for their products.

Conclusion

The United States Patent 9,616,028 is a pivotal patent in the intellectual property landscape surrounding dapagliflozin and metformin hydrochloride extended-release tablets. Its focus on bilayer tablet formulations and pharmaceutical compositions ensures AstraZeneca's exclusive rights to manufacture and market this specific drug formulation until its expiration in May 2031.

Key Takeaways

• Patent Title: "Bilayer tablet formulations"
• Issuance Date: April 11, 2017
• Expiration Date: May 12, 2031 (including pediatric exclusivity)
• Claims: Focus on bilayer tablet formulations and pharmaceutical compositions of dapagliflozin and metformin hydrochloride
• Patent Landscape: Part of a broader portfolio including US7919598 and US685934
• Litigation: Involved in patent infringement suits to protect intellectual property rights

FAQs

Q1: What is the main focus of the '028 patent? The '028 patent primarily focuses on the formulation and composition of bilayer tablets containing dapagliflozin and metformin hydrochloride.

Q2: When does the '028 patent expire? The '028 patent is set to expire on May 12, 2031, including the pediatric exclusivity extension.

Q3: What other patents are part of the same intellectual property landscape? Other significant patents include US7919598 and US685934, which protect various aspects of dapagliflozin and metformin hydrochloride formulations.

Q4: Why is the '028 patent important for generic manufacturers? The '028 patent creates a barrier for generic manufacturers, requiring them to wait for its expiration or challenge it through litigation to gain market approval.

Q5: Has the '028 patent been involved in any litigation? Yes, the '028 patent has been involved in patent infringement suits filed by AstraZeneca against generic manufacturers like Apotex Inc. and Apotex Corp.

Sources

1. Pharsight: Xigduo Xr patent expiration.
2. FDA: Dapagliflozin and Metformin Hydrochloride Extended-Release Tablets.
3. SSRN: Patent Claims and Patent Scope.
4. DrugBank: Saxagliptin: Uses, Interactions, Mechanism of Action.
5. IN THE UNITED STATES DISTRICT COURT FOR THE DISTRICT OF DELAWARE: AstraZeneca AB v. Apotex Inc. and Apotex Corp.

Drugs Protected by US Patent 9,616,028

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-001	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-002	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	XIGDUO XR	dapagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205649-005	Jul 28, 2017		RX	Yes	No					Y
Astrazeneca Ab	XIGDUO XR	dapagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205649-002	Oct 29, 2014		RX	Yes	No					Y

International Family Members for US Patent 9,616,028

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2498758		301040	Netherlands
European Patent Office	2498758		LUC00152	Luxembourg
European Patent Office	2498758		PA2020003	Lithuania
European Patent Office	2498758		CA 2020 00017	Denmark
European Patent Office	2498758		2020C/509	Belgium
European Patent Office	2498758		132020000000034	Italy