Details for Patent: 8,598,185

Which drugs does patent 8,598,185 protect, and when does it expire?

Patent 8,598,185 protects ATRIPLA and is included in one NDA.

This patent has sixty-one patent family members in twenty-seven countries.

Summary for Patent: 8,598,185

Title:	Unitary pharmaceutical dosage form
Abstract:	In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.
Inventor(s):	Dahl; Terrence C. (Sunnyvale, CA), Hussain; Munir A. (Belle Mead, NJ), Lipper; Robert A. (Pennington, NJ), Jerzewski; Robert L. (Belle Mead, NJ), Menning; Mark M. (San Francisco, CA), Oliyai; Reza (San Carlos, CA), Yang; Taiyin (Saratoga, CA)
Assignee:	Bristol-Myers Squibb & Gilead Sciences, Inc. (Foster City, CA)
Application Number:	11/453,122
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,598,185
Patent Claim Types: see list of patent claims	Dosage form; Formulation;

Understanding the Scope and Claims of United States Patent 8,598,185

Introduction

United States Patent 8,598,185, titled "Unitary pharmaceutical dosage form," is a significant patent in the pharmaceutical industry, particularly in the development of antiviral medications. This patent, assigned to Bristol-Myers Squibb and Gilead Sciences, Inc., describes a novel pharmaceutical product containing a combination of efavirenz, emtricitabine, and tenofovir disoproxil fumarate.

Patent Overview

Publication Details

• Publication Number: US8598185B2
• Filing Date: June 13, 2006
• Priority Date: February 7, 2006 (U.S. Patent Appl. Ser. No. 60/771,353)[4].

Inventors and Assignees

The patent was assigned to Bristol-Myers Squibb and Gilead Sciences, Inc., reflecting a collaborative effort in developing this pharmaceutical product.

Scope of the Patent

Description of the Invention

The patent describes a unitary pharmaceutical dosage form that combines three active ingredients: efavirenz, emtricitabine, and tenofovir disoproxil fumarate. This combination is designed to treat HIV infection and is a significant advancement in antiviral therapy.

Manufacturing Process

The manufacturing process involves several steps, including:

• Wet granulating the efavirenz component with a surfactant and other excipients.
• Separately manufacturing the Truvada component (emtricitabine and tenofovir disoproxil fumarate) using dry granulation.
• Mixing the granulates together.
• Compressing the mixture into tablets.
• Film-coating the tablets to ensure bioequivalence and patient compliance[4].

Claims of the Patent

Independent Claims

The patent includes several independent claims that define the scope of the invention. Key claims include:

• The composition of the unitary dosage form containing efavirenz, emtricitabine, and tenofovir disoproxil fumarate.
• The specific manufacturing process to achieve the desired bioequivalence.
• The physical form of the tablets, including size and coating, to ensure ease of swallowing and therapeutic efficacy[4].

Dependent Claims

Dependent claims further specify the details of the composition, such as the ratios of the active ingredients, the types of excipients used, and the coating materials. These claims help to narrow down the scope and ensure that any variations must still meet the core requirements outlined in the independent claims.

Patent Landscape

Classification

The patent is classified under various categories in the International Patent Classification (IPC) system, including:

• A61K9/20—Pills, tablets, discs, rods.
• A61K9/2072—Tablets characterized by shape, structure, or size.
• A61P31/12—Antivirals[4].

Prior Art and Novelty

The patent addresses a significant challenge in pharmaceutical manufacturing by providing a novel solution to combine three antiviral drugs into a single, bioequivalent tablet. This innovation overcomes the shortcomings of previous approaches that failed to achieve the desired bioequivalence between the commercial products (Viread, Emtriva, and Sustiva) and the proposed triple combination product[4].

Impact on the Pharmaceutical Industry

Therapeutic Significance

The combination of efavirenz, emtricitabine, and tenofovir disoproxil fumarate in a single tablet simplifies treatment regimens for HIV patients, improving adherence and reducing the complexity of managing multiple medications.

Regulatory Compliance

The patent emphasizes the importance of meeting stringent FDA requirements for bioequivalence, ensuring that the final product is both effective and safe for patients.

Litigation and Enforcement

Patent Infringement

The patent has been involved in litigation, such as the case between Bristol-Myers Squibb and Lupin, where infringement of U.S. Patent No. 8,598,185 was alleged[2].

Metrics for Patent Scope

Claim Length and Count

Research on patent scope metrics suggests that the length and count of independent claims can be indicative of the patent's breadth and complexity. For US8598185B2, the claims are carefully crafted to ensure a balanced scope that protects the innovation while allowing for future developments in the field[3].

Conclusion

United States Patent 8,598,185 represents a significant advancement in pharmaceutical technology, particularly in the treatment of HIV. The patent's scope and claims are meticulously defined to protect the novel combination and manufacturing process of the unitary dosage form.

Key Takeaways

• Novel Combination: The patent combines efavirenz, emtricitabine, and tenofovir disoproxil fumarate into a single tablet.
• Manufacturing Process: The process involves wet and dry granulation, mixing, compression, and film-coating.
• Bioequivalence: The final product must meet stringent FDA requirements for bioequivalence to commercial products.
• Regulatory Impact: The patent ensures compliance with FDA regulations and simplifies treatment regimens for HIV patients.
• Litigation: The patent has been involved in infringement cases, highlighting its importance in the pharmaceutical industry.

FAQs

1. What is the main innovation of U.S. Patent 8,598,185?

   • The main innovation is the development of a unitary pharmaceutical dosage form combining efavirenz, emtricitabine, and tenofovir disoproxil fumarate for treating HIV.

2. How is the combination tablet manufactured?

   • The manufacturing process involves wet granulating the efavirenz component, dry granulating the Truvada component, mixing the granulates, compressing into tablets, and film-coating.

3. Why is bioequivalence important for this patent?

   • Bioequivalence is crucial to ensure that the combination tablet meets FDA requirements and is therapeutically equivalent to the individual commercial products (Viread, Emtriva, and Sustiva).

4. What are the therapeutic benefits of this combination tablet?

   • The combination simplifies treatment regimens for HIV patients, improving adherence and reducing the complexity of managing multiple medications.

5. Has this patent been involved in any litigation?

   • Yes, the patent has been involved in infringement cases, such as the case between Bristol-Myers Squibb and Lupin.

Sources

1. Google Patents - US8598185B2 - Unitary pharmaceutical dosage form.
2. Typepad - Case 2:14-cv-00795-JRG Document 1 Filed 07/24/14 Page 1 of 10.
3. SSRN - Patent Claims and Patent Scope.
4. Google Patents - US8598185B2 - Unitary pharmaceutical dosage form.
5. Googleapis - (12) United States Patent (10) Patent No. 8,598,185.

Drugs Protected by US Patent 8,598,185

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Gilead Sciences	ATRIPLA	efavirenz; emtricitabine; tenofovir disoproxil fumarate	TABLET;ORAL	021937-001	Jul 12, 2006		DISCN	Yes	No	8,598,185		Y

International Family Members for US Patent 8,598,185

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	054060
Argentina	054511
Austria	E419839