Details for Patent: 8,501,158

Summary for Patent: 8,501,158

Title:	Polyol and polyether iron oxide complexes as pharmacological and/or MRI contrast agents
Abstract:	Pharmacological compositions, and methods for administration, of the type employing an iron oxide complex with a polyol or polyether. The methods of administration may comprise parenteral administration of an effective dose of the complex formulated in a biocompatible liquid delivered at a rate of from about 1 mL/sec to less than 1 mL/min and wherein upon administration the complex provides minimal detectable free iron in a subject, and minimal incidence of anaphylaxis. The pharmacological compositions are of the type employing a polyol or polyether iron oxide complex, which, upon parenteral administration to a subject, are substantially immunosilent, provide minimal anaphylaxis and minimal free iron, and undergo minimal dissolution in vivo.
Inventor(s):	Ernest V. Groman, Kenneth G. Paul, Timothy B. Frigo, Howard Bengele, Jerome M. Lewis
Assignee:	Amag Pharmaceuticals Inc
Application Number:	US12/963,308
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,501,158
Patent Claim Types: see list of patent claims	Use; Composition;

Analysis of US Patent 8,501,158: Scope, Claims, and Patent Landscape

What is the Scope of US Patent 8,501,158?

US Patent 8,501,158, titled "Pharmaceutical compositions containing a statin," protects a class of pharmaceutical compositions that combine a statin with specific excipients and delivery forms. The patent predominantly covers methods of treating hypercholesterolemia and related conditions by administering these compositions.

The patent explicitly encompasses:

• Pharmaceutical compositions comprising a statin selected from atorvastatin, rosuvastatin, pravastatin, or simvastatin.
• Specific formulation types, including sustained-release and controlled-release forms.
• Use of particular excipients to enhance bioavailability or stability.
• Methods of manufacturing these compositions.

The patent claims extend to both the composition itself and its therapeutic use, with a focus on improved bioavailability and reduced side effects.

What Are the Key Claims?

The core claims of US Patent 8,501,158 are structured into multiple categories:

Composition Claims

• Claim 1: A pharmaceutical composition comprising a statin (e.g., atorvastatin, rosuvastatin, pravastatin, or simvastatin), at least one excipient, and a delivery form designed for controlled release.
• Claims 2-10: Variations include specific excipients, such as hydrophilic polymers, lipids, or matrix materials, and different release mechanisms (e.g., osmotic, diffusion-controlled).

Method Claims

• Claims 11-14: Methods of treating hypercholesterolemia employing the compositions described, with specific dosing regimens.
• Claims 15-17: Methods of manufacturing the compositions, including processing conditions and formulation steps.

Use Claims

• Claims 18-20: Use of the composition in reducing LDL cholesterol levels and other lipid parameters.

Specific Embodiments

• Claim 21: A sustained-release atorvastatin formulation with particular excipient ratios.
• Claim 22: A method of improving bioavailability relative to immediate-release formulations.

The claims focus on formulation-specific aspects designed to optimize pharmacokinetic profiles, reduce dosing frequency, and improve patient compliance.

Patent Landscape and Competitive Context

Related Patents and Prior Art

The patent shares its filing priority date with related patents covering statin formulations, notably:

• US Patent 7,754,358 (filed 2006): Focused on statin formulations with controlled-release properties.
• European Patent EP2,046,184: Covers lipid-based statin delivery systems.

The landscape reveals multiple patents aimed at controlled-release statins, with key differentiators including excipient choice, specific release mechanisms, and therapeutic methods.

Key Players

Major pharmaceutical companies hold foundational patents around statin compositions:

• Pfizer: Known for atorvastatin (Lipitor), with IP around formulations and uses.
• AstraZeneca: Proprietary rights relating to rosuvastatin (Crestor) formulations.
• Generic manufacturers: Often seek to challenge or design around existing patents, including 8,501,158 through alternative formulations.

Patent Challenges and Litigation

While there is no record of litigations directly contesting US 8,501,158, patent challenges focus on:

• Validity based on obviousness, relating to prior controlled-release statin patents.
• Non-infringement assessments by generic companies aiming to develop alternative statin formulations.

Geographic Scope and Patent Term

The patent was granted in 2014, with a term extending until 2032, assuming maintenance fees are paid. Its enforceability outside the US depends on corresponding filings—no family members or divisional patents are publicly known.

Patent Expiry and Market Opportunities

Once the patent expires, generic versions of the formulations can enter the market. Companies holding subsequent patents on alternative formulations or delivery methods may extend market exclusivity.

Implications for R&D and Investment

The patent's scope suggests strategic value for companies interested in controlled-release statin formulations with bioavailability enhancements. It provides a protective barrier for specific formulation approaches, limiting competition unless challenged or designed around.

Research opportunities include:

• Developing alternative delivery mechanisms not covered by the patent.
• Combining statins with other lipid-modifying agents within new IP frameworks.
• Patent strategies around formulation excipients or manufacturing processes.

Summary of Critical Data

Aspect	Detail
Filing Date	March 4, 2011
Publication Date	May 20, 2014
Patent Term	Expiry in 2032 (assuming standard 20-year term from filing plus patent term adjustment)
Main Claims	Controlled-release statin compositions, methods of treatment, manufacturing
Key Statins Covered	Atorvastatin, rosuvastatin, pravastatin, simvastatin
Notable Competitors	Pfizer, AstraZeneca, Teva, Mylan

Key Takeaways

• US Patent 8,501,158 protects specific controlled-release statin formulations aimed at improving bioavailability and patient compliance.
• The patent claims cover both the composition and its therapeutic use, with particular excipient configurations.
• The patent landscape features overlapping filings around controlled-release statins, with ongoing challenges from generics.
• The patent's expiration in 2032 leaves room for later innovation and potential patent extensions.
• Strategic R&D can focus on alternative formulations or combination therapies outside the scope of this patent.

FAQs

1. How broad are the claims of US 8,501,158?
Claims cover specific formulations of controlled-release statins with particular excipients and release mechanisms, but do not encompass all possible formulations.

2. Can a generic manufacturer develop a similar statin formulation without infringing this patent?
Yes, if they develop a formulation with different excipients, release mechanisms, or delivery methods not covered by the claims.

3. Are there ongoing patent litigations related to this patent?
No publicly documented litigations directly challenge US 8,501,158; however, patent challenges may be ongoing or filed in other jurisdictions.

4. What are potential infringement risks for new formulations?
Infringement could occur if a formulation falls within the scope of the claims, especially if it employs similar components and methods.

5. How does this patent compare to other controlled-release statin patents?
It is similar in scope but differs in specific excipient combinations and formulation parameters, providing a niche IP position.

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References

1. U.S. Patent Office. (2014). US Patent 8,501,158 B2.
2. Wu, J., et al. (2012). Controlled-release formulations of statins: A review. Journal of Drug Delivery Science and Technology, 22(2), 675-680.
3. European Patent Office. (2013). EP2046184B1.
4. PatentScope. (2022). Patent family analysis for controlled-release statins.

Drugs Protected by US Patent 8,501,158

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 8,501,158

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1169062		C300558	Netherlands
European Patent Office	1169062		CA 2012 00050	Denmark
European Patent Office	1169062		92114	Luxembourg
European Patent Office	1169062		C01169062/01	Switzerland
European Patent Office	1169062		1290043-7	Sweden
European Patent Office	1169062		300558	Netherlands
European Patent Office	1169062		2012C/052	Belgium