Details for Patent: 9,539,218

Which drugs does patent 9,539,218 protect, and when does it expire?

Patent 9,539,218 protects XARELTO and is included in one NDA.

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

This patent has twenty-nine patent family members in twenty-five countries.

Summary for Patent: 9,539,218

Title:	Prevention and treatment of thromboembolic disorders
Abstract:	The present invention relates to the field of blood coagulation, more specifically it relates to a method of treating a thromboembolic disorder by administering once daily a direct factor Xa inhibitor in oral dosage form to a patient in need thereof, wherein the factor Xa inhibitor has a plasma concentration half life indicative of a bid or tid administration interval, e.g. of 10 hours or less.
Inventor(s):	Frank Misselwitz, Dagmar Kubitza, Son-Mi Park, Klaus Wehling
Assignee:	Bayer Intellectual Property GmbH
Application Number:	US11/883,218
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,539,218
Patent Claim Types: see list of patent claims	Use; Dosage form;

United States Patent 9,539,218: Rivaroxaban Treatment-Method Claims, Scope, Expiration, and Patent Landscape

U.S. Patent No. 9,539,218 covers a dosing method for rivaroxaban, marketed as Xarelto, that administers the drug in a rapid-release tablet no more than once daily for at least five consecutive days to treat pulmonary embolism, deep vein thrombosis, or stroke. The patent does not claim rivaroxaban as a molecule, a tablet composition, or a manufacturing process. Its value depends on whether a competing product label, prescribing instructions, or actual use practices satisfy every limitation of claim 1.

The key commercial issue is the interaction between this patent and rivaroxaban’s FDA-approved dosing regimens. The approved acute DVT and pulmonary embolism regimen begins with twice-daily administration for 21 days, which does not satisfy the “no more than once daily” limitation during that period. Later once-daily treatment can present a stronger overlap risk. Stroke-related once-daily use, particularly for prevention of stroke in nonvalvular atrial fibrillation, presents a potentially closer fit, although claim construction and the specific indication remain important.

What drug does U.S. Patent 9,539,218 cover?

The compound identified in claim 1 is rivaroxaban:

Item	Description
Generic name	Rivaroxaban
Brand	Xarelto
Drug class	Direct factor Xa inhibitor
Molecular limitation	5-Chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
Patent type	Method of treatment
Dosage form required	Rapid-release tablet
Frequency required	No more than once daily
Minimum duration	At least five consecutive days
Covered disorders	Pulmonary embolism, deep vein thrombosis, or stroke

The structural definition is effectively compound-specific. A different direct factor Xa inhibitor, such as apixaban, edoxaban, or betrixaban, would not fall within claim 1 merely because it is used at the same frequency or for the same disease.

What are the claims of U.S. Patent 9,539,218?

Claim 1 is the only independent claim. It requires the concurrence of six substantive elements:

1. A method of treating a thromboembolic disorder.
2. Administration of rivaroxaban.
3. Administration no more than once daily.
4. Administration for at least five consecutive days.
5. Use of a rapid-release tablet.
6. Treatment of pulmonary embolism, deep vein thrombosis, or stroke.

Claims 2, 3, and 4 narrow claim 1 by selecting one disorder:

Claim	Covered indication
Claim 1	Pulmonary embolism, DVT, or stroke
Claim 2	Pulmonary embolism
Claim 3	Deep vein thrombosis
Claim 4	Stroke

The dependent claims do not add a dose, patient population, treatment duration beyond five days, or specific tablet composition.

How broad is the scope of claim 1?

Claim 1 is narrower than a conventional “rivaroxaban for treating DVT” claim because it contains both a dosing-frequency limitation and a dosage-form limitation.

Rivaroxaban limitation

The claim requires the specifically recited molecule. This excludes competing factor Xa inhibitors and likely excludes a materially different chemical entity, even if the alternative has similar pharmacology.

Once-daily limitation

“No more than once daily” includes once-daily administration and could, linguistically, include less frequent dosing. It excludes twice-daily administration during the claimed treatment period.

This limitation is central to infringement analysis. A regimen that begins with twice-daily dosing and later transitions to once-daily dosing may fall outside the claim during the initial phase but potentially fall within it during the later phase, provided all other limitations are met for at least five consecutive days.

Five-consecutive-day limitation

The claim requires continuous compliance with the frequency limitation for at least five consecutive days. Sporadic once-daily use, missed doses, or an isolated prescription does not necessarily establish performance of the claimed method.

For induced-infringement analysis, however, a label may be relevant if it instructs patients to use the product in a manner that necessarily or materially practices this limitation.

Rapid-release tablet limitation

The patent does not cover every rivaroxaban dosage form. It requires a rapid-release tablet. An extended-release tablet, transdermal system, injectable product, or other delivery system would not literally satisfy this limitation.

The phrase is likely interpreted in view of the patent specification and the ordinary pharmaceutical meaning of immediate or rapid release. Dissolution specifications, excipient composition, tablet hardness, and release testing could become relevant if the patent’s specification assigns a technical definition to the term.

Disorder limitation

The claim lists pulmonary embolism, DVT, and stroke. This closed “selected from the group consisting of” formulation generally limits the claim to those listed disorders.

A method directed only to prevention of a different thromboembolic event may not satisfy the claim. Stroke presents a particular issue because “treating stroke” is broader and potentially different from reducing the risk of stroke in atrial fibrillation.

What FDA-approved Xarelto regimens overlap with the patent?

The FDA-approved label contains several once-daily rivaroxaban regimens, but not all are directed to the disorders listed in the patent claims.

FDA use	Typical regimen	Potential relationship to claim 1
Acute DVT treatment	15 mg twice daily for 21 days, then 20 mg once daily	Initial phase falls outside once-daily limitation; later phase may overlap
Acute PE treatment	15 mg twice daily for 21 days, then 20 mg once daily	Same analysis as acute DVT
Reduction in recurrent DVT/PE after at least six months’ treatment	10 mg once daily	Frequency and duration may fit, but indication is recurrence reduction rather than necessarily active treatment
Stroke-risk reduction in nonvalvular atrial fibrillation	20 mg once daily, or 15 mg once daily in certain renal impairment	Potentially close to the stroke limitation, depending on claim construction and labeling
Hip or knee replacement prophylaxis	10 mg once daily	Does not correspond to the listed disease limitations
Coronary or peripheral artery disease risk reduction	Low-dose combination regimen	May not satisfy the thromboembolic-disorder and tablet-regimen limitations

The FDA label identifies rivaroxaban as a direct factor Xa inhibitor and establishes the dosing instructions relevant to an infringement analysis (U.S. Food and Drug Administration, 2024).

The strongest practical overlap is not necessarily the acute treatment label. For DVT and PE, the required initial twice-daily phase creates a non-infringing segment. The maintenance phase may still be relevant if the patent covers treatment after the transition to once-daily dosing. For stroke, the once-daily regimen creates a closer textual match, but the patent claim says “treating” stroke rather than expressly reciting stroke-risk reduction.

When does U.S. Patent 9,539,218 expire?

U.S. Patent 9,539,218 was granted on January 10, 2017. Its term is governed principally by the earliest effective nonprovisional filing date and any applicable patent-term adjustment or terminal disclaimer, rather than by the grant date alone.

Public patent records identify the patent as part of the Bayer rivaroxaban development estate and associate it with an international priority framework predating the U.S. grant. The expected nominal term is in the late 2020s, subject to the official USPTO patent-term calculation.

The controlling date for commercial planning is the USPTO term-adjustment and continuity record, not an expiration date inferred from the grant date. Patent-term extension under 35 U.S.C. § 156 is generally associated with regulatory review of a patented product, but the existence and duration of any extension must be confirmed from the official patent record.

What patents protect the broader Xarelto product?

Xarelto’s U.S. protection has historically involved several patent categories rather than one patent.

Protection category	Typical subject matter	Relevance to generic entry
Compound patents	Rivaroxaban chemical structure	Core molecule; earliest and generally strongest product protection
Salt, crystal, or solid-state patents	Polymorphs, crystalline forms, physical properties	May affect API or finished-product selection
Formulation patents	Rapid-release tablets, excipients, dissolution, particle size	Can constrain formulation design or create Paragraph IV exposure
Method-of-use patents	DVT, PE, stroke prevention, atrial fibrillation, recurrence reduction	Supports label-based or induced-infringement theories
Manufacturing patents	Synthetic routes, intermediates, purification, process controls	Usually avoidable through alternative manufacturing routes
Combination or risk-reduction patents	Rivaroxaban with antiplatelet therapy or in specific cardiovascular populations	Relevant to narrower indications and label strategy

U.S. Patent 9,539,218 is significant because it sits in the method-of-use layer. It does not independently block manufacture of rivaroxaban API or every rivaroxaban tablet.

What is the Orange Book status of U.S. Patent 9,539,218?

Orange Book status must be evaluated against the specific NDA patent listing and the current FDA Orange Book entry for Xarelto. A patent can be listed for an NDA and still present a narrower enforcement position than the product’s commercial label.

For a generic applicant, the principal possibilities are:

• Paragraph IV certification if the applicant asserts that the patent is invalid, unenforceable, or not infringed.
• A Paragraph III certification if the applicant accepts a later expiration date.
• A section viii statement carving out a patented method of use from the proposed labeling, where FDA rules permit the carve-out.
• A label that retains non-patented uses while omitting a patented indication or dosing instruction.

Because claim 1 is a method claim tied to a specific frequency and dosage form, a section viii strategy may be commercially relevant if the proposed generic label can omit the claimed use without removing essential FDA-approved information. The strategy becomes more difficult where the same once-daily instructions are needed for multiple indications.

What Paragraph IV risks apply to generic rivaroxaban?

A generic applicant would likely assess at least four non-infringement positions.

Regimen-based non-infringement

For acute DVT and PE, the applicant could argue that the mandated 15 mg twice-daily initiation period does not meet the “no more than once daily” limitation. The patent holder could respond that later once-daily treatment independently satisfies the claim for five consecutive days.

Indication carve-out

A generic label could attempt to omit a patented stroke or thromboembolic indication. The effectiveness of this strategy depends on whether the remaining label still directly encourages the claimed use.

Dosage-form distinction

A product with a release profile outside the patent’s rapid-release definition could avoid literal infringement. This position would require technical support from dissolution data and formulation records.

Claim-validity challenges

Potential validity issues would likely include:

• Anticipation or obviousness based on prior art describing once-daily rivaroxaban use.
• Written-description and enablement questions concerning the full range of disorders and regimens.
• Definiteness of “rapid-release tablet.”
• Obviousness based on clinical trial protocols, published dosing studies, and known rivaroxaban pharmacokinetics.

The patent’s defensibility would depend heavily on the prosecution history, cited prior art, and whether the claimed once-daily treatment was materially distinguished from earlier rivaroxaban treatment disclosures.

Which companies are challenging Xarelto exclusivity?

The relevant competitive field includes generic pharmaceutical manufacturers seeking approval for rivaroxaban tablets and branded anticoagulant competitors.

The major branded competitors are:

Company	Product	Mechanism
Bayer and Johnson & Johnson/Janssen	Xarelto, rivaroxaban	Direct factor Xa inhibition
Bristol Myers Squibb and Pfizer	Eliquis, apixaban	Direct factor Xa inhibition
Daiichi Sankyo	Savaysa/Lixiana, edoxaban	Direct factor Xa inhibition
Boehringer Ingelheim	Pradaxa, dabigatran	Direct thrombin inhibition
Warfarin manufacturers	Warfarin	Vitamin K antagonism

Generic competition is primarily a small-molecule ANDA issue. Biosimilar risk does not apply because rivaroxaban is a chemically synthesized small molecule, not a biologic.

Public litigation analysis should distinguish between:

• Patent litigation involving the core rivaroxaban compound.
• ANDA litigation involving generic tablets.
• Disputes involving method-of-use patents.
• Commercial settlements that establish a permitted generic launch date.
• Regulatory approval dates, which do not necessarily equal commercial launch dates.

A definitive list of current challengers and settlement terms requires review of the docket, FDA Orange Book, ANDA litigation notices, and publicly filed settlement agreements.

What licensing deals affect Xarelto?

Xarelto was developed and commercialized through the Bayer and Johnson & Johnson/Janssen collaboration. The commercial allocation has generally divided geographic and market responsibilities between the two companies. Bayer has held substantial rights outside the United States, while Janssen has participated in U.S. commercialization.

This collaboration matters to patent enforcement because the relevant plaintiff, NDA holder, patent owner, and commercial distributor may differ by jurisdiction and by patent. Patent ownership, licensing rights, and standing should be checked patent by patent rather than inferred solely from the Xarelto brand relationship.

How strong is the patent estate for U.S. Patent 9,539,218?

The patent has moderate, targeted strength rather than broad product-level strength.

Factor	Assessment
Chemical specificity	Strong against alternative descriptions of rivaroxaban, but irrelevant to other anticoagulants
Claim breadth	Narrow because of the once-daily and rapid-release limitations
FDA-label overlap	Meaningful for once-daily maintenance and certain stroke-related uses
Acute DVT/PE overlap	Weaker during the initial twice-daily phase; stronger during later once-daily therapy
Formulation dependence	Material; non-rapid-release products may avoid the claim
Invalidity exposure	Depends on prior art and prosecution history
Generic carve-out potential	Potentially meaningful for selected indications
Biosimilar relevance	None
Manufacturing leverage	Limited because the patent is not a process claim

The patent is more useful as a secondary barrier than as a standalone blocker to all generic rivaroxaban competition. A generic developer could potentially design around the method claim, carve out selected indications, or challenge validity while relying on other patents for the principal exclusivity analysis.

What patent litigation affects generic rivaroxaban launch timing?

The principal litigation risk is Hatch-Waxman litigation triggered by a Paragraph IV certification. A suit filed within the statutory period can trigger a 30-month stay of FDA approval, subject to statutory exceptions and court developments.

A launch assessment should track:

1. The patent numbers listed for Xarelto in the Orange Book.
2. The generic applicant’s certifications.
3. The date of any infringement complaint.
4. District court claim construction.
5. Federal Circuit appeals.
6. Any settlement and agreed launch date.
7. FDA approval status after the stay expires or is lifted.

A patent-specific finding of non-infringement does not eliminate risk from separate formulation, compound, or method patents. Conversely, expiration or invalidation of this method patent does not necessarily authorize immediate unrestricted generic commercialization if other listed patents remain enforceable.

What revenue exposure does this patent create?

Xarelto has been a major anticoagulant product for Bayer and Janssen, with multibillion-dollar global annual sales during its peak commercial period. The patent’s direct revenue exposure is narrower than total Xarelto revenue because the claim covers only:

• Rivaroxaban;
• Rapid-release tablets;
• No-more-than-once-daily administration;
• At least five consecutive days; and
• PE, DVT, or stroke treatment.

Revenue from hip and knee prophylaxis, coronary artery disease, peripheral artery disease, or other uses may fall outside the claim. The exposure is therefore indication- and regimen-specific. Generic entry affecting the molecule or broad product label would have a larger commercial effect than invalidation of this method claim alone.

Key Takeaways

• U.S. Patent 9,539,218 is a rivaroxaban method-of-treatment patent.
• Claim 1 requires a rapid-release tablet administered no more than once daily for at least five consecutive days.
• The covered disorders are pulmonary embolism, deep vein thrombosis, and stroke.
• The patent does not claim rivaroxaban itself, every rivaroxaban tablet, or the manufacturing process.
• The twice-daily 21-day initiation regimen for acute DVT and PE does not satisfy the once-daily limitation during that initial period.
• Later once-daily treatment may create overlap after the transition from twice-daily dosing.
• Once-daily stroke-related use presents a potentially closer claim match.
• Generic developers may consider Paragraph IV, section viii, formulation-based non-infringement, or claim-validity strategies.
• Rivaroxaban is a small molecule, so biosimilar competition is not relevant.
• The commercial effect of this patent must be assessed together with compound, formulation, solid-state, method-of-use, and manufacturing patents in the broader Xarelto estate.
• The official USPTO, FDA Orange Book, FDA label, and litigation dockets control current expiration, listing, and enforcement conclusions.

FAQs About U.S. Patent 9,539,218 and Rivaroxaban Exclusivity

Does U.S. Patent 9,539,218 cover Eliquis?

No. The claims require rivaroxaban by chemical structure. Eliquis contains apixaban and is outside the literal compound limitation.

Can a once-daily rivaroxaban generic avoid this patent?

Potentially. Avoidance may depend on the indication, treatment duration, tablet release profile, label wording, and whether the product is used in a manner that satisfies every limitation of claim 1.

Does the patent cover rivaroxaban 10 mg once daily?

The claim does not recite a dose. A 10 mg once-daily regimen could satisfy the frequency limitation if the indication, rapid-release tablet, and five-day duration limitations are also met.

Does the patent cover stroke prevention in atrial fibrillation?

The claim recites stroke as a covered thromboembolic disorder but does not expressly recite atrial fibrillation or stroke-risk reduction. The answer depends on claim construction, the patent specification, the FDA label, and the accused labeling or conduct.

Is U.S. Patent 9,539,218 the last patent blocking generic Xarelto?

Not necessarily. Generic entry depends on the complete Orange Book listing and any other enforceable patents covering rivaroxaban, its formulations, approved uses, or related products.

References

1. Bayer AG. (2024). Annual report 2023. Bayer AG.

2. Johnson & Johnson. (2024). Annual report 2023. Johnson & Johnson.

3. U.S. Food and Drug Administration. (2024). Xarelto (rivaroxaban) prescribing information. Janssen Pharmaceuticals, Inc.

4. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. U.S. Department of Health and Human Services.

5. U.S. Patent and Trademark Office. (2017). U.S. Patent No. 9,539,218, methods of treating thromboembolic disorders. U.S. Department of Commerce.

6. U.S. Patent and Trademark Office. (2024). Patent term adjustment and patent term information. U.S. Department of Commerce.

7. 35 U.S.C. §§ 271(e), 282, 156, 271(e)(4). United States Code.

Drugs Protected by US Patent 9,539,218

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Pharms	XARELTO	rivaroxaban	TABLET;ORAL	022406-001	Jul 1, 2011	AB	RX	Yes	No	9,539,218*PED				Y
Janssen Pharms	XARELTO	rivaroxaban	TABLET;ORAL	022406-002	Nov 4, 2011	AB	RX	Yes	No	9,539,218*PED				Y
Janssen Pharms	XARELTO	rivaroxaban	TABLET;ORAL	022406-003	Nov 4, 2011	AB	RX	Yes	Yes	9,539,218*PED				Y

Foreign Priority and PCT Information for Patent: 9,539,218

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	05001893	Jan 31, 2005

PCT Information
PCT Filed	January 19, 2006	PCT Application Number:	PCT/EP2006/000431
PCT Publication Date:	August 03, 2006	PCT Publication Number:	WO2006/079474

International Family Members for US Patent 9,539,218

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	052565
Argentina	110413
Australia	2006208613
Brazil	PI0606760
Canada	2596145
China	101111236