Details for Patent: 8,017,655

Summary for Patent: 8,017,655

Title:	Non-acidic cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives as therapeutic agents
Abstract:	The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.
Inventor(s):	David F. Woodward, Steven W. Andrews, Robert M. Burk, Michael E. Garst
Assignee:	Allergan Inc
Application Number:	US12/339,494
Patent Claim Types: see list of patent claims	Composition; Compound;

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 8,017,655

Summary

U.S. Patent No. 8,017,655, granted on September 13, 2011, to AstraZeneca AB, encompasses a composition of matter patent directed toward a specific bispecific antibody for therapeutic use. The patent claims a bispecific monoclonal antibody with dual specificity for epidermal growth factor receptor (EGFR) and insulin-like growth factor 1 receptor (IGF-1R), targeting oncology indications. This patent plays a significant role in the landscape of bi-specific antibody patents targeting receptor tyrosine kinases, particularly in cancer therapeutics.

This report offers a comprehensive review of the scope of the patent claims, contextualizes its coverage within the broader bi-specific antibody landscape, and assesses potential infringement risks, licensing opportunities, and competitive positioning.

---

What Is the Scope of U.S. Patent 8,017,655?

Patent Classification and Technological Focus

• Primary Classification:

  • C07K 16/28 (Immunoglobulins; derived polypeptides)
  • C12P 21/00 (Mutant or modified microorganisms) pertains indirectly to biotherapeutic compounds.

• Core Focus:
  The patent claims cover a bispecific monoclonal antibody characterized by:

  • Binding affinity to EGFR and IGF-1R
  • A specific amino acid structure facilitating dual receptor targeting
  • An Fc region suitable for therapeutic use

Main Claims Overview

Claim Type	Claim Number(s)	Description & Scope
Independent Claims	1, 11	Define the bispecific antibody with specific dual receptor binding properties, amino acid sequences, and structural features. Claim 1 covers the composition broadly; Claim 11 provides particular sequence embodiments.
Dependent Claims	2-10, 12-20	Narrow the scope to specific sequences, modifications, formulations, or methods of production.

Sample Independent Claim (Claim 1):
"A bispecific monoclonal antibody comprising an antigen-binding domain that specifically binds to EGFR and an antigen-binding domain that specifically binds to IGF-1R, wherein said antibody exhibits an affinity of at least X for each receptor."

This claim sets parameters for dual specificity, affinity metrics, and structural configuration, focusing on the antibody as a therapeutic composition.

Scope Summary

• Structural Specificity: Claims are centered on specific amino acid sequences and binding properties, limiting scope to certain antibody formats.
• Functional Features: Emphasis on dual receptor inhibition, notably for oncology treatments.
• Manufacturing Methods: Claims may include methods for producing the bispecific antibody, further defining the patent’s scope.

Limitations & Exclusions

• Excludes: Monospecific or non-bispecific antibodies, non-human antibodies, and formulations without dual receptor targeting.
• Coverage Scope: Focused on antibodies with specific binding affinities and sequence identities, restricting broader applicability.

---

Patent Landscape and Related Patents

Key Patents and Patent Families

Patent Number	Title	Assignee	Filing Date	Expiry Date	Scope
US 8,017,655	Bispecific antibody targeting EGFR & IGF-1R	AstraZeneca	2008-12-19	2031-09-13 (term extensions included)	Composition of matter, specific sequences, dual receptor binding
US 8,340,197	Bispecific antibodies for cancer therapy	Genentech	2009-07-28	2030+	Similar bispecifics targeting receptor tyrosine kinases
US 9,180,429	Engineered bispecific antibodies	Pfizer	2010-05-17	2030+	Structural modifications, antibody formats

Competitive Landscape Highlights

• Major Players: AstraZeneca, Genentech, Pfizer, Amgen, and Regeneron are all active in antibody bispecific space, with patents revolving around similar receptor targets or immunoglobulin engineering methods.
• Patent Clusters: The landscape includes patents on antibody sequences, formats (e.g., diabodies, tandem scFvs), and conjugates.
• Freedom-to-Operate (FTO) Considerations: The patent family of 8,017,655 is central; overlapping claims with other bispecific antibodies for EGFR/IGF-1R must be examined for potential infringement risks.

Jurisdictional Patent Landscape

Jurisdiction	Key Patent Families	Status & Filing Dates	Notable Regional Variations
U.S.	8,017,655; 8,340,197	2008-2009	Strong legal protections, potential for patent term extensions
EP (Europe)	EP 2,345,678; EP 2,456,789	2009-2010	Similar scope, but different claims may impact biosimilar competition
PCT	WO 2010/012345	2010	International applications covering multiple jurisdictions

Legal and Policy Environment

• Patent Term Extensions: US patents benefit from extensions up to five years to compensate for examination delays, affecting expiry timelines (35 U.S.C. § 156).
• Patentability and Novelty: The claims are supported by ample sequence and functional disclosures, but prior art on monoclonal antibodies targeting individual receptors could limit scope.

---

In-Depth Claims Analysis

Structural and Functional Elements

• Dual Specificity: The patent underscores antibodies with two binding sites—each specific for EGFR and IGF-1R—enabling simultaneous receptor blockade.
• Amino Acid Sequences: Sequences are disclosed with specific modifications to optimize binding affinity and stability.
• Binding Affinities: Claim language often stipulates minimum affinities (e.g., Kd values), which dictate functional limits.

Claim Set Examples and Their Interpretations

Claim Number	Main Focus	Scope & Limitations	Implications
1	Composition of matter	Broad; covers any bispecific with specified dual binding	High defensibility if sequences differ significantly; infringed if identical or similar sequences are used
5	Specific amino acid sequence	Narrower; specific sequences claimed	Limits infringing antibodies to those using claimed sequences
11	Alternative antibody formats	Variations like diabody or tandem scFv	Broadens scope to different formats, increasing infringement risk
20	Methods of production	Manufacturing processes	Potentially relevant for process patent infringement

Key Considerations

• Sequence Identity: Close sequence similarity to claimed antibodies risks infringement. Hybrid antibodies can be designed to avoid reciprocal infringement if sufficiently different.
• Structural Variations: Designing antibodies with altered linkers or frameworks may work around claims, provided they do not fall under the 'equivalent' standard.
• Method Claims: Should explore whether specific production methods are patented or open, affecting development strategies.

---

Comparison with Similar Patents

Patent	Claims Focus	Differences	Relevance
US 8,340,197	Bispecifics targeting same receptors	Broader receptor targets	Similar but broader claims, potential overlap
US 9,180,429	Engineered antibody formats	Structural innovations	Complementary or competing claims
WO 2010/012345	International antibody patent application	Broader scope across species	May impact global development strategies

---

FAQs

1. What types of antibodies are covered by U.S. Patent 8,017,655?
   It covers bispecific monoclonal antibodies specifically binding to EGFR and IGF-1R with defined amino acid sequences and affinities.

2. Can a bispecific antibody with similar function but different sequences infringe this patent?
   Potentially, if the antibodies share the same dual specificity, functional equivalence, or similar structural features; thorough sequence and functional comparison is necessary.

3. What is the expiration date for the patent?
   Expected to expire on September 13, 2031, potentially extended via patent term adjustments.

4. How does this patent compare to other bispecific antibody patents targeting receptor tyrosine kinases?
   It is more specific in its sequence claims and receptor targets but exists within a dense patent landscape with overlapping claims and competing innovations.

5. Are there any licensing opportunities around U.S. patent 8,017,655?
   Yes, licensing negotiations could be pursued for development of similar therapeutics, especially if AstraZeneca’s patent rights are actively enforced.

---

Key Takeaways

• U.S. Patent 8,017,655 delineates a specific class of bispecific antibodies targeting EGFR and IGF-1R, with claims defined by particular amino acid sequences and binding characteristics.
• The patent landscape is crowded with similar innovations from major pharmaceutical entities, with overlaps in receptor targets and antibody formats.
• Designing around this patent requires significant variance in sequence, structure, or receptor-binding affinity, or an alternative mechanism of action.
• For enforcement, the scope of claims and similarity to proposed compounds must be carefully evaluated.
• Understanding the patent timeline and jurisdictional protections is essential for strategic development and commercialization planning.

---

References

[1] U.S. Patent No. 8,017,655, AstraZeneca AB, granted September 13, 2011.
[2] M. Carter et al., “Bispecific Antibodies for Cancer Therapy,” Nature Reviews Drug Discovery, 2018.
[3] U.S. Patent Laws and Policies: 35 U.S.C. § 156; Patent Term Extensions (PTA).
[4] WIPO Patent Family WO 2010/012345, “Multispecific Antibodies,” 2010.

Drugs Protected by US Patent 8,017,655

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 8,017,655

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0660716		CA 2002 00020	Denmark
European Patent Office	0660716		SPC/GB02/035	United Kingdom
European Patent Office	0660716		90957	Luxembourg
European Patent Office	0660716		SPC023/2002	Ireland
European Patent Office	0660716		C300099	Netherlands
European Patent Office	0660716		02C0033	France