U.S. Patent 8,114,885: Pazopanib Scope, Claims, Expiration, Orange Book Status and Generic Risk

U.S. Patent 8,114,885 covers pazopanib hydrochloride, pharmaceutical compositions containing the active ingredient, oral dosage forms, and methods of treating colon and breast cancer. The patent is part of the pazopanib, or Votrient, patent estate historically associated with GlaxoSmithKline. Its principal commercial relevance was protection against generic formulations and selected cancer-treatment uses. Based on the earliest priority date and the standard 20-year patent term, the patent term ended in 2023, subject to any applicable patent-term adjustment or extension. The claims supplied contain a material chemical inconsistency in claim 6 that could affect construction and enforcement.

What drug does U.S. Patent 8,114,885 protect?

The compound in the claims is pazopanib, administered commercially as pazopanib hydrochloride.

The relevant chemical name is:

5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide hydrochloride.

Pazopanib is an oral multi-kinase inhibitor that blocks signaling through vascular endothelial growth factor receptors, platelet-derived growth factor receptors and related kinases. FDA approved Votrient tablets in 2009 for advanced renal cell carcinoma and later for advanced soft-tissue sarcoma after prior chemotherapy. The cancer indications recited in Patent 8,114,885 are narrower and different from the principal FDA-labeled renal-cell-carcinoma indication.[1]

Patent identification

Item	Data
Patent	U.S. Patent 8,114,885
Patent type	Small-molecule pharmaceutical patent
Active ingredient	Pazopanib hydrochloride
Commercial product	Votrient
Patent holder associated with estate	Glaxo Group Limited / GlaxoSmithKline
Issue date	February 14, 2012
Claim categories	Compound, composition, oral dosage form, cancer treatment
Cancers expressly claimed	Colon cancer and breast cancer
FDA product	Votrient tablets
FDA approval date	October 19, 2009
Expected ordinary term endpoint	2023, based on the applicable priority and filing chain

What are the independent claims in Patent 8,114,885?

The supplied claims contain three substantive independent claim groups.

Claim 1: Pazopanib hydrochloride compound

Claim 1 covers the compound defined by the structural formula. Based on claim 2, the intended compound is pazopanib hydrochloride.

A structure claim generally has the broadest direct infringement potential because it reaches the active pharmaceutical ingredient itself, regardless of whether the defendant sells tablets, capsules, bulk API or another dosage form. The claim’s enforceability depends on the exact structure shown in the patent, the written description, prosecution amendments and any terminal disclaimer.

If claim 1 covers pazopanib hydrochloride without a limitation to a particular crystal form, hydrate, particle size or manufacturing process, it would not ordinarily distinguish among conventional solid-state presentations of the same salt.

Claim 2: Composition containing pazopanib hydrochloride

Claim 2 covers a pharmaceutical composition comprising:

an effective amount of an active ingredient;
one or more pharmaceutically acceptable carriers, diluents or excipients; and
pazopanib hydrochloride as the active ingredient.

This is a formulation claim, but it is broad. It does not require a specific tablet weight, concentration, dissolution profile, excipient identity or manufacturing process. A conventional oral tablet containing pazopanib hydrochloride and standard pharmaceutical excipients could fall within the literal scope if the claim remains enforceable and the product satisfies the “effective amount” limitation.

Claim 8: Treatment of colon or breast cancer

Claim 8 covers administering an effective amount of the compound of claim 1 to a human with colon cancer or breast cancer.

Claims 12 through 16 extend the treatment coverage to administration of the pharmaceutical composition in claim 2 and separately specify breast cancer and colon cancer. Claim 19 adds combination treatment to the breast-cancer method.

These method claims require proof of the disease condition, administration of the claimed compound or composition, and the required therapeutic purpose. They do not necessarily cover every use of pazopanib, particularly uses outside the listed diseases.

How do claims 3 through 7 and 17 through 18 narrow the formulation scope?

Claims 3 through 7 and 17 through 18 depend from the composition claims and add dosage-form or excipient limitations.

Claim	Added limitation	Commercial effect
3	Oral administration	Targets tablets, capsules and other oral products
4	At least one diluent	Covers common tablet diluents
5	At least one excipient	Broad excipient limitation
6	Diluent, disintegrant and pazopanib-related compound	More specific tablet composition
7	Lubricant added to claim 6	Targets conventional compressed tablets
17	Oral administration plus diluent	Narrower oral formulation
18	Oral administration, diluent and excipient	Narrower oral formulation

The formulation claims are significant because a generic applicant may avoid a broad product claim only if it can establish that its product does not contain the claimed compound, does not contain the required excipient category, or does not meet another claim limitation. In practice, the product-by-process and formulation details in the ANDA, including inactive ingredients and manufacturing information, would determine the infringement analysis.

What is the defect in claim 6?

Claim 6, as supplied, recites:

“5-({4-[(2H-indazol-6yl)methyl)amino]pyrimidin-2yl}amino)-2-methylbenzenesulfonamide monohydrochloride.”

This wording differs from the pazopanib structure in several respects:

It omits the “2,3-dimethyl” substitution appearing in the pazopanib name.
It contains mismatched parentheses.
It uses “6yl” and “2yl” rather than the more conventional “6-yl” and “2-yl.”
It appears to identify a different or incompletely identified indazole derivative.

This issue cannot be resolved from the claim text alone. Courts construe claims using the patent specification, prosecution history and applicable correction doctrines. The written description may establish that claim 6 contains a typographical error. A court could consider whether the error is correctable and whether the intended correction is evident. If multiple chemically plausible corrections exist, the claim may face indefiniteness or written-description challenges.

The inconsistency is less damaging to claims that independently recite the fully identified pazopanib hydrochloride compound, but it creates a specific vulnerability for claim 6 and its dependent claim 7.

What cancer-treatment methods does Patent 8,114,885 cover?

The treatment claims cover:

colon cancer;
breast cancer;
administration of pazopanib hydrochloride;
administration of a pazopanib-containing pharmaceutical composition;
combination with another pharmaceutical active agent;
combination with surgery; and
combination with radiotherapy.

Claim 19 is directed to breast cancer treatment combined with an additional anti-cancer therapy. Claims 9 through 11 similarly cover combination treatment.

The claims do not identify a specific companion drug, chemotherapy regimen, radiation dose or surgical procedure. The “at least one additional anti-cancer therapy” language is expansive, but its practical strength depends on the validity of the underlying treatment claim and proof that the accused conduct satisfies the combination-treatment limitation.

Method-of-use strength

The method claims are weaker than a broad active-ingredient claim when:

the accused product label omits the patented indication;
the use occurs outside colon or breast cancer;
the generic product is distributed under a label that excludes the claimed uses; or
the patent term has expired.

Before expiration, induced-infringement risk could remain relevant where a label, promotional material or other conduct encouraged the claimed use. After expiration, the claims no longer create an enforceable exclusionary right.

When did U.S. Patent 8,114,885 lose exclusivity?

The ordinary patent term ended in 2023 based on the relevant filing and priority chain. The exact enforceability endpoint should be determined from the issued patent, any patent-term adjustment, any terminal disclaimer and the FDA’s regulatory exclusivity records.[2]

The patent’s economic protection is therefore historical rather than prospective. Generic applicants no longer need to establish a noninfringement position against an expired patent for commercial launch purposes, although expired claims remain relevant to historical litigation, damages periods and the interpretation of related patent families.

FDA regulatory exclusivity is separate from patent exclusivity. Votrient’s approval did not give pazopanib an orphan-drug exclusivity period for the renal-cell-carcinoma indication. The FDA’s Orange Book lists patents associated with approved products, but listing does not itself establish validity or infringement.[3]

What is the Orange Book status of pazopanib?

Pazopanib hydrochloride is associated with NDA 022465 for Votrient tablets. The Orange Book historically identified patents covering the active ingredient and related protection for Votrient. Patent 8,114,885 should be assessed together with the other patents listed for the NDA, including the foundational pazopanib patent family.

The Orange Book is relevant because an ANDA applicant must address listed patents through:

Paragraph I certification, where no patent information is listed;
Paragraph II certification, where the patent has expired;
Paragraph III certification, where the applicant will wait until patent expiration; or
Paragraph IV certification, alleging invalidity, unenforceability or noninfringement.

For an expired patent such as Patent 8,114,885, a Paragraph II certification is generally the relevant pathway. A Paragraph IV challenge would have been commercially relevant before expiration.

Which companies challenged the pazopanib patent estate?

The supplied material does not establish the identity of a particular ANDA filer, Paragraph IV challenger or litigation defendant. Patent litigation cannot be inferred solely from the patent claims.

The relevant historical defendants would have been generic applicants filing ANDAs for pazopanib tablets and sending Paragraph IV notices to the NDA holder. Any litigation analysis must distinguish:

the specific patent challenged;
the ANDA product strength;
the proposed label;
the date of notice;
the statutory 30-month stay;
the court’s disposition; and
any settlement or license.

No settlement terms should be attributed to a company without a court docket, SEC filing, FDA litigation record or other primary source.

What is the broader pazopanib patent landscape?

Foundational compound protection

The foundational pazopanib patent family covers substituted indazole compounds and related kinase inhibitors. U.S. Patent 7,943,621 is commonly identified with the core pazopanib compound estate. Its expiration date and any applicable term adjustment must be reviewed against the issued patent and Orange Book record.[4]

Composition and dosage-form protection

Patent 8,114,885 adds protection for:

pazopanib hydrochloride compositions;
oral dosage forms;
diluents and excipients;
disintegrants and lubricants; and
selected tablet formulations.

These claims are most relevant to generic tablet products that use the same salt and conventional inactive ingredients.

Solid-state and manufacturing protection

Separate patent families may address:

crystalline pazopanib hydrochloride;
hydrates or solvates;
polymorphic forms;
particle-size characteristics;
improved dissolution;
salt preparation; and
manufacturing processes.

A generic company can face additional barriers if its proposed product uses a claimed solid form or process, even where the basic compound patent has expired. Process patents generally create a different infringement analysis from product claims, particularly where the product is imported or the manufacturing process occurs outside the United States.

Geographic coverage

U.S. Patent 8,114,885 has U.S.-only enforceability. Foreign counterparts must be analyzed independently because prosecution amendments, claim scope, opposition proceedings and expiration dates vary by jurisdiction. Key commercial jurisdictions for pazopanib include the European Union, United Kingdom, Japan, Canada, China, Australia and India.

A U.S. patent expiration does not establish freedom to operate in those markets. Conversely, a foreign patent loss does not remove U.S. restrictions.

How strong is the patent estate for pazopanib?

The estate was strongest before 2023 because it combined:

compound protection;
salt and composition coverage;
oral tablet claims;
selected method-of-use claims; and
FDA-listed patent status supporting Paragraph IV litigation.

Its present strength is limited by expiration. The remaining commercial risks are more likely to involve:

later-expiring formulation or solid-state patents;
regulatory exclusivity;
trade secrets relating to manufacturing;
supply agreements;
controlled-release or combination products; and
jurisdiction-specific patents outside the United States.

Patent 8,114,885 itself is not a durable current barrier to generic U.S. entry if its term has expired and no enforceable related patent remains in force.

What generic launch scenarios applied to pazopanib?

Before expiration, the main scenarios were:

Scenario	Result
Paragraph III certification	Launch deferred until patent expiration
Paragraph IV certification with no suit	Potential launch after statutory period
Paragraph IV certification followed by suit	Possible 30-month stay and patent litigation
Successful noninfringement position	Earlier launch subject to other patents
Successful invalidity challenge	Patent barrier removed
Settlement or license	Launch date controlled by agreement
Skinny-label strategy	Possible use-label carveout, subject to induced-infringement risk

After expiration, the commercial question shifts from Patent 8,114,885 to remaining Orange Book patents, FDA approval status, manufacturing capacity and payer substitution.

What is the revenue exposure from Patent 8,114,885?

Patent 8,114,885 protected a product with substantial oncology revenue exposure because Votrient was marketed globally for renal-cell carcinoma and soft-tissue sarcoma. The patent’s listed colon- and breast-cancer uses were not the principal labeled commercial indications, which reduces the direct value of those method claims relative to the compound and formulation claims.

The largest economic risk was generic substitution of oral pazopanib tablets after loss of compound and formulation protection. Revenue impact depended on:

the number of approved ANDAs;
generic launch timing;
launch at risk;
price discounting;
payer substitution;
remaining patents; and
supply and manufacturing capacity.

Key Takeaways

Patent 8,114,885 covers pazopanib hydrochloride, oral compositions and treatment methods for colon and breast cancer.
Claim 1 is the principal compound claim; claims 2 through 7 and 17 through 18 address formulations.
Claims 8 through 16 and 19 cover selected cancer-treatment and combination-treatment methods.
Claim 6 contains a significant chemical and drafting inconsistency that could create construction and validity issues.
The patent’s ordinary U.S. term ended in 2023, subject to the official term calculation.
Historical Paragraph IV litigation risk was material before expiration; current U.S. generic risk depends primarily on later-expiring related patents and FDA approval status.
The patent should be analyzed with the foundational pazopanib patent, Orange Book listings and any solid-state, formulation or manufacturing patents.
The listed cancer indications do not correspond exactly to Votrient’s principal FDA-approved indications.

FAQs

Is Patent 8,114,885 a compound patent or a formulation patent?

It contains both compound and formulation protection. Claim 1 is directed to the compound structure, while claims 2 through 7 and 17 through 18 cover pazopanib hydrochloride compositions and oral dosage forms.

Does Patent 8,114,885 cover renal-cell-carcinoma treatment?

The supplied claims expressly recite colon cancer and breast cancer, not renal cell carcinoma. The FDA-approved renal-cell-carcinoma indication must be analyzed against separate patents and the Votrient label.

Can a generic avoid Patent 8,114,885 by using pazopanib free base?

Potentially, but the answer depends on claim construction and the precise claim 1 structure. A generic using a different chemical form could avoid a hydrochloride-specific composition claim but may still encounter compound, salt, formulation or process claims in related patents.

Does an expired Orange Book patent block an ANDA?

No. An expired patent generally supports a Paragraph II certification and does not independently prevent FDA approval or commercial launch. Other listed patents may still create a barrier.

Does the typo in claim 6 invalidate the entire patent?

No. A defect confined to claim 6 does not automatically invalidate unrelated claims. The effect depends on whether the court can correct the language and whether the remaining claims independently satisfy patentability and definiteness requirements.

References

U.S. Food and Drug Administration. (2009). Votrient (pazopanib) prescribing information.
United States Patent and Trademark Office. (n.d.). Patent term adjustment and patent term information for U.S. Patent No. 8,114,885.
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
United States Patent and Trademark Office. (2011). U.S. Patent No. 7,943,621, substituted indazole compounds.
United States Patent and Trademark Office. (2012). U.S. Patent No. 8,114,885, pazopanib hydrochloride compositions and therapeutic methods.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1343782	⤷ Start Trial	C300456	Netherlands	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	CA 2010 00024	Denmark	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	91710	Luxembourg	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	SPC025/2010	Ireland	⤷ Start Trial
European Patent Office	1343782	⤷ Start Trial	10C0037	France	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,114,885

Summary for Patent: 8,114,885