US Patent 9,464,071: Erdafitinib FGFR Patent Scope, Expiration and Competitive Landscape
US Patent 9,464,071 is a Janssen patent covering methods of using quinoxaline-based FGFR kinase inhibitors, including erdafitinib, marketed as Balversa. Its strongest commercial protection is directed to treating FGFR-driven cancers with erdafitinib and closely defined analogs. The patent does not claim erdafitinib as a standalone composition of matter in the claims supplied; it claims therapeutic and kinase-inhibition methods.
The patent’s principal commercial relevance is its coverage of erdafitinib treatment for urothelial carcinoma and tumors containing FGFR1-4 alterations, including FGFR3 translocations and mutations. The statutory patent term appears to extend to December 22, 2032, subject to any patent-term adjustment and regulatory exclusivity reflected in the official USPTO and FDA records.[1][2]
What does US Patent 9,464,071 protect?
The patent protects four principal categories of activity:
| Claim group |
Protected activity |
Commercial relevance |
| Claims 1-17 |
Treating FGFR-mediated disease with a broad quinoxaline compound genus |
Broad method-of-treatment coverage |
| Claims 18-36 |
Treating cancer, including biomarker-defined tumors |
Direct oncology-use protection |
| Claims 37-39 |
Inhibiting an FGFR kinase by contacting the kinase with the compound |
Primarily research and assay use |
| Claims 40-45 |
Combination treatment and specified lung-cancer indications |
Label-expansion and combination-use coverage |
The core scaffold is a substituted quinoxaline linked to a 3,5-dimethoxyphenyl group and an aminoalkyl substituent. The claims cover:
- Quinoxaline derivatives;
- Tautomers;
- Stereoisomers;
- Isotopic forms;
- N-oxides;
- Pharmaceutically acceptable salts;
- Solvates;
- Broad substituent classes at the R1, R2 and R3 positions.
Claim 14 identifies the principal commercial molecule by chemical name:
N-(3,5-dimethoxyphenyl)-N'-(1-methylethyl)-N-[3-(1-methyl-1H-pyrazol-4-yl)quinoxalin-6-yl]ethane-1,2-diamine.
That compound is erdafitinib. Claims 15 and 31 provide narrower protection for the non-N-oxide form. Claims 30, 35, 38 and 42 repeat the erdafitinib species in different therapeutic contexts.
Which claims cover erdafitinib?
Erdafitinib is covered most directly by claims 14, 15, 30, 31, 35, 36, 38, 39, 42 and 43.
The independent claims also cover erdafitinib when the compound is used:
- To treat a disease mediated by an FGFR kinase;
- To treat cancer;
- To treat specified carcinomas;
- To inhibit an FGFR kinase;
- In combination with another anticancer agent;
- In tumors with FGFR mutations, translocations or overexpression.
The most commercially significant dependent claims are:
| Claim |
Erdafitinib-related limitation |
| 12 |
Methyl R1, two methoxy R2 groups and isopropylaminoethyl R3 group |
| 14-15 |
Erdafitinib compound and the non-N-oxide form |
| 22 |
t(4;14)-positive multiple myeloma |
| 24 |
Bladder cancer with FGFR3 chromosomal translocation |
| 25 |
Bladder cancer with FGFR3 point mutation |
| 26-28 |
FGFR1, FGFR2, FGFR3 or FGFR4 mutations and FGFR1 overexpression |
| 29 |
Urothelial carcinoma |
| 30-31 |
Erdafitinib for cancer treatment |
| 38-39 |
Erdafitinib for FGFR kinase inhibition |
| 40-43 |
Combination treatment involving erdafitinib |
| 44-45 |
NSCLC and specified lung-cancer subtypes |
How broad is the genus in US Patent 9,464,071?
The genus is materially broader than erdafitinib. R1 may include alkyl, hydroxyalkyl, haloalkyl, sulfonyl-containing groups, heterocyclic groups, phosphonate-containing groups and other substituted alkyl groups. R2 covers multiple substituent classes, including halogen, cyano, alkyl, alkoxy, amino, amide and heterocyclic substituents.
R3 is especially broad. It includes:
- Alkyl;
- Alkenyl and alkynyl groups;
- Hydroxyalkyl groups;
- Aminoalkyl groups;
- Heterocycle-substituted alkyl groups;
- Sulfonamide-containing substituents;
- Carbonyl derivatives;
- Phosphonate derivatives;
- Further substituted amine groups.
This drafting strategy creates a large chemical genus around the quinoxaline-FGFR pharmacophore. It gives the patent potential reach against close erdafitinib analogs, but broad genus claims are more exposed than the narrow species claims to validity challenges based on written description, enablement, anticipation and obviousness.
What is the strongest claim coverage?
The strongest coverage is concentrated in the narrow species and biomarker-defined treatment claims.
Exact erdafitinib species
Claims 14, 15, 30, 31, 35, 36, 38, 39, 42 and 43 identify erdafitinib or its specific non-N-oxide form. A competitor administering the same molecule for an FGFR-related cancer would face a direct literal-infringement argument if the relevant claim remains enforceable and the use falls within the claim language.
FGFR3-altered bladder cancer
Claims 23-25 and 29 are commercially important because they track the principal clinical use of erdafitinib. Claims 24 and 25 cover bladder cancer associated with FGFR3 chromosomal translocations and point mutations. Claim 29 covers urothelial carcinoma without requiring the more specific FGFR3 alteration stated in claims 24 and 25.
Combination treatment
Claims 40-43 cover administration with one or more anticancer agents, including kinase inhibitors. These claims may be relevant to combination regimens, although enforcement depends on the treatment protocol, the parties involved and whether the accused conduct satisfies the required administration steps.
When does US Patent 9,464,071 lose exclusivity?
The expected statutory expiration date is December 22, 2032, based on the earliest identified priority date of December 22, 2011 and the standard United States patent term measured from the earliest effective nonprovisional filing date.[1]
| Exclusivity item |
Date or status |
| Earliest priority date |
December 22, 2011 |
| Patent issuance |
October 11, 2016 |
| Expected statutory expiration |
December 22, 2032 |
| Patent-term adjustment |
Must be confirmed in the USPTO patent record |
| Patent-term extension |
No extension is established from the claim information alone |
| FDA approval of Balversa |
April 12, 2019 |
| FDA orphan-drug exclusivity |
Not the principal exclusivity basis for the approved urothelial-carcinoma indication |
| Generic or 505(j) entry |
Dependent on Orange Book listings, Paragraph IV litigation and settlement terms |
Patent expiration does not automatically establish immediate generic entry. Listed patents, pediatric exclusivity, court orders, settlements and separate patents covering formulation, dosing or approved methods may affect the practical launch date.
What is the Orange Book status of erdafitinib?
Balversa is an FDA-approved small-molecule drug and is eligible for Orange Book patent listing under the applicable FDA regulations. The relevant Orange Book analysis must distinguish between:
- The active ingredient;
- Drug-product claims;
- Method-of-use claims;
- Formulation claims;
- Separate continuation or divisional patents.
US Patent 9,464,071 is method-of-treatment oriented. If listed for Balversa, it would primarily create a method-of-use barrier rather than a conventional composition-of-matter barrier. The practical effect would depend on the scope of the FDA-approved use code and whether a generic applicant can submit a Paragraph IV certification or a section viii statement carving out the patented indication.[2][3]
The approved Balversa label identifies erdafitinib for adults with locally advanced or metastatic urothelial carcinoma harboring susceptible FGFR3 genetic alterations after prior therapy. That indication closely overlaps the FGFR3 mutation and translocation claims in the patent.[4]
Are there Paragraph IV challenges to US Patent 9,464,071?
No publicly established Paragraph IV challenge, ANDA litigation outcome or settlement specific to US Patent 9,464,071 is identified in the information supplied.
A Paragraph IV challenge would likely target one or more of the following:
- Anticipation of the quinoxaline genus or erdafitinib species;
- Obviousness based on earlier FGFR kinase inhibitors;
- Written-description support for the broad substituent genus;
- Enablement across the full chemical and therapeutic scope;
- Indefiniteness in the disease-mediated and biomarker-related limitations;
- Failure of the asserted claims to cover the proposed generic labeling.
A generic applicant seeking a non-infringing launch could attempt to omit the patented FGFR3-related indication under a section viii statement. That strategy would be difficult if the commercial market is concentrated in the claimed FGFR-altered urothelial-carcinoma population and if the FDA-approved labeling cannot be meaningfully separated from the patented use.
What patent litigation affects erdafitinib?
No material US patent-litigation record involving US Patent 9,464,071 is established by the supplied information. The absence of a known challenge should not be treated as proof that the patent has never been asserted, licensed or reviewed in an ANDA context.
The principal litigation risks are likely to arise when:
- A generic applicant files an ANDA for erdafitinib;
- A competitor develops a close quinoxaline analog;
- A sponsor seeks an indication involving FGFR3-altered urothelial carcinoma;
- A generic label includes the same FGFR3 biomarker population;
- A combination product or co-administered kinase inhibitor is commercialized.
How does this patent compare with competing FGFR inhibitor estates?
Erdafitinib competes with several selective FGFR inhibitors, each protected by a separate patent estate.
| Drug |
Active ingredient |
Principal developer |
FGFR profile |
Commercial status |
| Balversa |
Erdafitinib |
Janssen |
FGFR1-4, clinically important FGFR3 activity |
FDA approved |
| Pemazyre |
Pemigatinib |
Incyte |
FGFR1-3 |
FDA approved |
| Truseltiq |
Infigratinib |
Helsinn/BridgeBio affiliates |
FGFR1-3 |
FDA approved, commercial status subject to market conditions |
| Lytgobin |
Futibatinib |
Taiho |
Irreversible FGFR1-4 inhibitor |
FDA approved |
| Rogaratinib |
Rogaratinib |
Bayer |
FGFR1-4 |
Investigational or regionally developed |
Erdafitinib’s patent position is strongest where the product, biomarker and indication align: erdafitinib for FGFR3-altered urothelial carcinoma. Pemigatinib, infigratinib and futibatinib do not fall within the exact erdafitinib species claims merely because they inhibit FGFR. Their separate chemical structures place them in different patent estates.
How strong is the patent estate?
The patent has a mixed strength profile.
| Protection type |
Strength assessment |
| Exact erdafitinib method claims |
Stronger, because the molecule is precisely identified |
| FGFR3-altered urothelial-cancer claims |
Strong commercial relevance and relatively clear clinical linkage |
| Broad chemical genus |
More vulnerable to written-description and obviousness attacks |
| N-oxide, salt and solvate coverage |
Useful formulation and product-form protection, subject to claim construction |
| In vitro kinase-inhibition claims |
Legally broad but less directly tied to product sales |
| Combination claims |
Potentially valuable, but dependent on proof of each administration step |
| Broad cancer lists |
Wider reach, but possible validity and enablement pressure |
The claim set contains several apparent transcription or drafting irregularities in the supplied text, including inconsistent references to R10/R11 and R14/R15. Such errors should be evaluated against the issued patent, its certificate of correction and the prosecution history. The enforceable scope is determined by the official patent record, not by an extracted claim transcription.
What manufacturing and geographic barriers remain?
US Patent 9,464,071 does not appear, from the supplied claims, to be a manufacturing-process patent. Its principal barrier is use of the covered molecule, not synthesis of the active ingredient.
A generic or alternative sponsor would still need to assess:
- Separate composition-of-matter patents;
- Solid-state, salt and polymorph patents;
- Formulation patents;
- Process patents;
- International family members;
- Regulatory data exclusivity;
- Patent rights in Europe, Japan, China and other commercial markets;
- Licensing or collaboration rights held by Janssen or related entities.
The US patent has no automatic effect outside the United States. Foreign family members must be analyzed separately for filing status, claim scope, opposition history and national expiration dates.
What revenue exposure does the patent create?
The patent’s revenue exposure is concentrated in Balversa’s FGFR-altered urothelial-carcinoma market. A generic launch before the end of the effective patent and exclusivity period could affect:
- Product price;
- Net sales;
- Market share;
- Combination-treatment development;
- Expansion into additional FGFR-driven tumors;
- Partnering value for erdafitinib lifecycle programs.
Because the claims cover both the drug and biomarker-defined treatment uses, a generic launch that targets the principal approved population would face greater risk than a launch limited to an unrelated or carved-out indication.
Key Takeaways
- US Patent 9,464,071 is primarily a method-of-use patent for FGFR inhibitors, not a standalone product claim based on the claims supplied.
- Erdafitinib is expressly identified in multiple dependent claims.
- The strongest commercial claims cover erdafitinib for FGFR3-altered urothelial carcinoma and other FGFR-driven cancers.
- The expected statutory expiration date is December 22, 2032, subject to USPTO patent-term adjustment and any applicable regulatory exclusivity.
- The broad chemical genus is more vulnerable to validity attacks than the specific erdafitinib claims.
- No established Paragraph IV challenge, settlement or material litigation outcome specific to this patent is identified from the supplied record.
- Competing FGFR inhibitors such as pemigatinib, infigratinib and futibatinib are protected by separate patent estates.
- A complete freedom-to-operate analysis requires review of continuation patents, Orange Book listings, formulation patents, process patents and foreign family members.
FAQs
Does US Patent 9,464,071 claim erdafitinib itself?
No. The supplied claims principally claim methods of treating disease or inhibiting FGFR kinase using erdafitinib and related compounds. Claims 14, 15, 30, 31, 35, 36, 38, 39, 42 and 43 specifically identify erdafitinib.
Can a generic company sell erdafitinib before 2032?
Only if it avoids enforceable patent and regulatory barriers, succeeds in litigation, reaches a settlement permitting earlier entry or launches after the relevant patent and exclusivity rights expire. A section viii carve-out may be possible in some circumstances, but it depends on the listed use and proposed labeling.
Does the patent cover FGFR inhibitors other than erdafitinib?
Yes. The broad genus claims cover numerous substituted quinoxaline compounds beyond the specifically named erdafitinib molecule. Other commercial FGFR inhibitors with different chemical structures generally fall under separate patent estates.
Does the patent cover FGFR3-mutant bladder cancer?
Yes. Claims 24 and 25 expressly address bladder cancer with an FGFR3 chromosomal translocation or FGFR3 point mutation. Claims 23 and 29 provide broader bladder-cancer and urothelial-carcinoma coverage.
Is the patent a manufacturing barrier for erdafitinib?
Not based on the claims supplied. The claims focus on treatment methods and FGFR kinase inhibition. Separate process, composition, polymorph or formulation patents could create additional manufacturing barriers.
References
- United States Patent and Trademark Office. (2016). US Patent No. 9,464,071.
- U.S. Food and Drug Administration. (n.d.). Orange Book: Approved drug products with therapeutic equivalence evaluations.
- U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Patent and exclusivity information.
- U.S. Food and Drug Administration. (2024). Balversa (erdafitinib) prescribing information. Janssen Products, LP.
