Details for Patent: 8,703,781

Which drugs does patent 8,703,781 protect, and when does it expire?

Patent 8,703,781 protects TAFINLAR and MEKINIST and is included in four NDAs.

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

This patent has forty-five patent family members in thirty-two countries.

Summary for Patent: 8,703,781

Title:	Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors
Abstract:	A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-tr- ioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2- -fluorophen-}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
Inventor(s):	Dumble; Melissa (Collegeville, PA), Kumar; Rakesh (Collegeville, PA), Laquerre; Sylvie (Collegeville, PA), Lebowitz; Peter (Collegeville, PA)
Assignee:	GlaxoSmithKline LLC (Philadelphia, PA)
Application Number:	13/499,779
Patent Claim Types: see list of patent claims	Compound; Composition; Device; Use;

United States Patent 8,703,781: A Detailed Analysis of Scope and Claims

Introduction

The United States Patent 8,703,781, titled "Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors," is a significant patent in the field of oncology, particularly for the treatment of cancers such as melanoma. This patent, assigned to GlaxoSmithKline LLC, was issued on April 22, 2014. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background

The patent revolves around the combination therapy of MEK inhibitors and B-RAF inhibitors, which are crucial in targeting the MAPK/ERK signaling pathway. This pathway is often dysregulated in various cancers, leading to uncontrolled cell growth and tumor formation. The combination of these inhibitors has shown promise in treating cancers, especially those with specific genetic mutations such as BRAF V600E mutations[1][2][5].

Scope of the Patent

The scope of the patent is defined by its claims, which outline the specific inventions and their applications. Here are the key aspects:

Claims

• The patent claims cover a pharmaceutical combination comprising a MEK inhibitor and a B-RAF inhibitor.
• Specific compounds mentioned include dabrafenib (a B-RAF inhibitor) and trametinib (a MEK inhibitor)[1][2].
• The claims also include methods for treating cancers, such as melanoma, using these combinations.
• The patent specifies various formulations, including pharmaceutical compositions and dosing regimens.

Pharmaceutical Compositions

• The patent describes pharmaceutical compositions that include the MEK inhibitor and B-RAF inhibitor, either as separate entities or in a single formulation.
• These compositions can be administered in various forms, such as tablets, capsules, or solutions[1].

Methods of Treatment

• The patent claims methods for treating cancers, particularly melanoma, by administering the combination of MEK and B-RAF inhibitors.
• It also covers the treatment of other neoplasms and diseases associated with the MAPK/ERK signaling pathway[1].

Patent Claims and Their Significance

The claims in this patent are critical as they define the intellectual property rights of the inventors and the assignee, GlaxoSmithKline LLC.

Genus Claims

The patent includes genus claims, which are broad claims that cover a class of compounds rather than specific embodiments. These claims are significant in the pharmaceutical industry as they provide broader protection, making it more difficult for competitors to design around the patent[3].

Specific Compounds

The patent specifically mentions dabrafenib and trametinib, which are well-known inhibitors used in cancer treatment. These specific claims ensure that the combination of these particular compounds is protected under the patent[1].

Patent Landscape

The patent landscape surrounding US 8,703,781 is complex and involves multiple patents and assignees.

Related Patents

• Other patents, such as US 8,835,443 and US 8,952,018, also relate to similar combinations of MEK and B-RAF inhibitors. These patents are also assigned to GlaxoSmithKline LLC and Japan Tobacco Inc., respectively[2][5].
• These related patents often overlap in their claims but may differ in specific compounds, formulations, or methods of treatment.

Patent Expiration Dates

• The patent US 8,703,781 is set to expire, but the exact expiration date is not explicitly stated in the sources. However, related patents have expiration dates ranging from 2025 to 2030[2][5].

Impact on the Pharmaceutical Industry

This patent has significant implications for the pharmaceutical industry, particularly in the development and marketing of cancer treatments.

Radical Innovation

• The combination of MEK and B-RAF inhibitors represents a radical innovation in cancer treatment, offering improved efficacy and reduced side effects compared to single-agent therapies[4].

Market Protection

• The patent provides GlaxoSmithKline LLC with market protection, allowing them to exclusively market and sell the combination therapy for a specified period. This protection is crucial for recouping the significant investment in research and development[2].

Generic Availability

• The expiration of this patent and related patents will pave the way for generic versions of these drugs, potentially increasing accessibility and reducing costs for patients[2][5].

Challenges and Limitations

While the patent offers substantial protection, there are challenges and limitations to consider:

Patent Scope and Claims

• The breadth of the patent claims can be a double-edged sword. While broad claims offer more protection, they can also be challenged for being too broad and not commensurate with the invention described in the application[3].

Regulatory and Litigation Issues

• The patent landscape in the pharmaceutical industry is often fraught with regulatory and litigation challenges. The validity and scope of the claims can be contested in courts, affecting the patent's enforceability[3].

Key Takeaways

• Combination Therapy: The patent covers a combination of MEK and B-RAF inhibitors, which is a significant advancement in cancer treatment.
• Scope and Claims: The patent includes broad genus claims and specific claims for dabrafenib and trametinib.
• Patent Landscape: The patent is part of a complex landscape involving multiple related patents and assignees.
• Impact: The patent has substantial implications for market protection and the development of generic versions post-expiration.
• Challenges: The patent faces challenges related to the breadth of claims and potential regulatory and litigation issues.

FAQs

Q: What is the main subject of United States Patent 8,703,781? A: The main subject is the pharmaceutical combination of MEK inhibitors and B-RAF inhibitors for treating cancers, particularly melanoma.

Q: Which specific compounds are mentioned in the patent? A: The patent specifically mentions dabrafenib (a B-RAF inhibitor) and trametinib (a MEK inhibitor).

Q: Who is the assignee of this patent? A: The assignee is GlaxoSmithKline LLC.

Q: What is the significance of genus claims in this patent? A: Genus claims provide broader protection by covering a class of compounds, making it harder for competitors to design around the patent.

Q: When are the related patents set to expire? A: Related patents have expiration dates ranging from 2025 to 2030.

Sources

1. US8703781B2 - Pharmaceutical combination of MEK inhibitor and B-RAF inhibitors - Google Patents
2. Generic Tafinlar Availability - Drugs.com
3. Eviscerating Patent Scope - DigitalCommons@NYLS
4. Do current radical innovation measures actually capture radical drug innovation? - VU Research Portal
5. Generic Mekinist Availability - Drugs.com

Drugs Protected by US Patent 8,703,781

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	MEKINIST	trametinib dimethyl sulfoxide	SOLUTION;ORAL	217513-001	Mar 16, 2023		RX	Yes	Yes	8,703,781*PED				Y
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-001	May 29, 2013		RX	Yes	No	8,703,781*PED				Y
Novartis	MEKINIST	trametinib dimethyl sulfoxide	TABLET;ORAL	204114-002	May 29, 2013		DISCN	Yes	No	8,703,781*PED				Y
Novartis	TAFINLAR	dabrafenib mesylate	CAPSULE;ORAL	202806-001	May 29, 2013		RX	Yes	No	8,703,781*PED				Y
Novartis	TAFINLAR	dabrafenib mesylate	CAPSULE;ORAL	202806-002	May 29, 2013		RX	Yes	Yes	8,703,781*PED				Y
Novartis	TAFINLAR	dabrafenib mesylate	TABLET, FOR SUSPENSION;ORAL	217514-001	Mar 16, 2023		RX	Yes	Yes	8,703,781*PED				Y

Foreign Priority and PCT Information for Patent: 8,703,781

PCT Information
PCT Filed	October 15, 2010	PCT Application Number:	PCT/US2010/052808
PCT Publication Date:	April 21, 2011	PCT Publication Number:	WO2011/047238

International Family Members for US Patent 8,703,781

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2010306653
Brazil	112012008854
Canada	2775803
Chile	2012000964
China	102655753
Colombia	6531498