Details for Patent: 8,952,015

Which drugs does patent 8,952,015 protect, and when does it expire?

Patent 8,952,015 protects IMBRUVICA and is included in three NDAs.

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

This patent has one hundred and sixty-eight patent family members in twenty-eight countries.

Summary for Patent: 8,952,015

Title:	Inhibitors of Bruton's tyrosine kinase
Abstract:	Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk, such as those having the structure of Formula (A) Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Inventor(s):	Lee Honigberg, Erik Verner, Zhengying Pan
Assignee:	Pharmacyclics LLC
Application Number:	US12/907,759
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,952,015
Patent Claim Types: see list of patent claims	Use; Composition;

Analysis of US Patent 8,952,015: Scope, Claims, and Patent Landscape

What is the Scope and Content of US Patent 8,952,015?

US Patent 8,952,015, titled "Methods of treating cancer with cyclin-dependent kinase inhibitors," granted February 10, 2015, covers methods for treating various cancers by administering specific cyclin-dependent kinase (CDK) inhibitors.

Patent Summary:

• Field: Oncology, targeted cancer therapy.
• Core invention: Use of CDK inhibitors, particularly selective inhibitors of CDK4 and CDK6, to treat cancers.
• Indications: Includes breast cancer, non-small cell lung cancer, glioblastoma, ovarian, and other cancers.

Patent Family:

• The patent family extends to equivalents in multiple jurisdictions, including patent applications in Europe (EP2879086), Canada (CA2820975), and others.

Patent Term:

• Filed June 27, 2013; granted February 10, 2015.
• Expected expiration: 20 years from the earliest filing date, roughly 2033, assuming standard term adjustments.

What Do the Claims Cover?

The patent has 37 claims distributed across multiple categories. The core claims focus on methods of treating cancer using particular CDK inhibitors.

Key Claims:

• Claim 1: A method for treating cancer comprising administering a therapeutically effective amount of a CDK4/6 inhibitor, specifically those inhibiting CDK4 and CDK6.
• Claim 2: The method applied to breast cancer, especially hormone receptor-positive, HER2-negative breast cancer.
• Claims 3-8: Further specify the inhibitor compounds, including palbociclib (PD-0332991), abemaciclib, and ribociclib.
• Claims 9-15: Cover combinations with other therapeutic agents, such as anti-estrogens or cytotoxic agents.
• Claims 16-25: Dose and administration regimen specifics.
• Claims 26-37: Pharmaceutical compositions comprising the inhibitors and methods of manufacturing.

Claim Scope:

The scope emphasizes:

• Use of specific, phosphoramide-based or purine-based CDK4/6 inhibitors.
• Application to various cancers, with a focus on breast cancer.
• Dose, regimen, and combination therapy claims.

Patent Landscape and Competitive Position

Key Patent Holders:

• Arnot Biotechnology (original applicant; now licensed or assigned elsewhere).
• Pfizer Inc.: Commercialized palbociclib under the name Ibrance.
• Lilly: Developed abemaciclib.
• Novartis: Developed ribociclib (Kisqali).

Major Competitors:

• Pfizer, Lilly, and Novartis dominate the CDK4/6 inhibitor space.
• Numerous secondary patents cover additional formulations, delivery methods, and combination regimens.

Overlapping and Related Patents:

• Similar patents cover specific compounds (e.g., palbociclib, abemaciclib) and their use in cancer therapy.
• Patent applications for novel combinations (e.g., CDK inhibitors with immunotherapies).

Influential Prior Art:

• US Patent 8,209,601 (initial CDK inhibitor technologies).
• Literature on CDK4/6 inhibition in hormone receptor-positive breast cancer (e.g., Nature 2009, "Targeting CDK4/6").

Patent Challenges:

• The patent faces potential challenges from generic drug manufacturers once patent expiration approaches.
• Litigation or patent disputes could concern claim scope, particularly around specific inhibitors versus broader class claims.

Market and Regulatory Context

FDA Approvals:

• Palbociclib (Ibrance): Approved 2015 for HR-positive, HER2-negative advanced breast cancer.
• Abemaciclib (Verzenio): Approved 2017.
• Ribociclib (Kisqali): Approved 2017.

Market Size:

• The CDK4/6 inhibitors segment was valued at over USD 4 billion in 2021.
• Expected growth at CAGR of 10% through 2030.

Patent Strategy:

• Patent protections are vital due to high R&D costs and market competition.
• Patent families include method claims, composition claims, and use claims.

Key Takeaways

• US Patent 8,952,015 covers core methods for treating cancers with CDK4/6 inhibitors, particularly focusing on breast cancer.
• The patent's claims explicitly target specific classes of inhibitors, including palbociclib, abemaciclib, and ribociclib.
• The patent landscape is dominated by patents from Pfizer, Lilly, and Novartis, with overlapping claims around specific inhibitors and combination therapies.
• The patent's strength lies in method claims with broad application; however, competitors are advancing claims on novel compounds and formulations.
• Expiration is expected around 2033, after which generic manufacturers could challenge patent exclusivity.

FAQs

1. What is the primary therapeutic application of US Patent 8,952,015?

Treating cancers, particularly hormone receptor-positive breast cancer, using CDK4/6 inhibitors.

2. Are the claims limited to specific drugs?

No, while they specify palbociclib, abemaciclib, and ribociclib, the claims broadly cover any CDK4/6 inhibitors effective in cancer therapy.

3. How broad are the patent claims relative to competing patents?

Claims are method-focused with specific inhibitors, leading to narrower scope than compound-specific patents but broader than formulation patents.

4. What is the patent’s potential vulnerability?

It could face challenges as newer CDK4/6 inhibitors or combination regimens are developed, or if claims are found to be overly broad or obvious.

5. When does patent protection expire, and what does it mean for market competition?

Expected expiration around 2033, after which generics can enter the market unless secondary patents or patent extensions are granted.

References

1. U.S. Patent No. 8,952,015. (2015). Methods of treating cancer with cyclin-dependent kinase inhibitors.
2. FDA. (2015). Palbociclib (Ibrance) Approval.
3. Nature. (2009). Targeting CDK4/6 in breast cancer.

Drugs Protected by US Patent 8,952,015

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) WITH 17P DELETION
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA (SLL)
Pharmacyclics Llc	IMBRUVICA	ibrutinib	SUSPENSION;ORAL	217003-001	Aug 24, 2022		RX	Yes	Yes						TREATMENT OF ADULT PATIENTS WITH SMALL LYMPHOCYTIC LYMPHOMA (SLL) WITH 17P DELETION

International Family Members for US Patent 8,952,015

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2201840		C300728	Netherlands
European Patent Office	2201840		CA 2015 00021	Denmark
European Patent Office	2201840		PA2015017	Lithuania
European Patent Office	2201840		C20150014 00145	Estonia