US Patent 8,247,400: Ceftaroline Fosamil Composition Claims, Patent Scope, Expiration and Generic Risk

US Patent No. 8,247,400 covers pharmaceutical compositions containing ceftaroline or a pharmaceutically acceptable salt, particularly compositions combining ceftaroline fosamil with low amounts of ceftaroline. It also covers specified antibacterial-treatment methods, 400 mg and 600 mg ceftaroline fosamil regimens, and a crystalline hydrochloride form of ceftaroline.

The patent is narrower than the foundational composition-of-matter patents for ceftaroline and ceftaroline fosamil. Its principal commercial relevance is formulation and residual-active-ingredient coverage rather than ownership of the ceftaroline molecule itself.

What does US Patent 8,247,400 cover?

The patent has four principal claim groups:

Claim group	Subject matter	Commercial significance
Claims 1-3	Ceftaroline and broad analog or salt coverage	Broad chemical genus, narrowed by claim 3 to ceftaroline
Claims 4-9	Compositions containing ceftaroline with ceftaroline fosamil or ceftaroline fosamil acetate	Formulation and composition protection
Claims 10-11, 13-23	Treatment of bacterial infections using specified compositions and dosing regimens	Method-of-use protection
Claim 12	Crystalline ceftaroline hydrochloride defined by XRPD peaks	Solid-state and polymorph protection

The patent’s most commercially relevant compound is the compound identified in claim 3:

(6R,7R)-7-[[(2Z)-2-(ethoxyimino)-2-[5-(acetamido)-1,2,4-thiadiazol-3-yl]acetyl]amino]-3-[[4-(1-methylpyridinium-4-yl)-1,3-thiazol-2-yl]sulfanyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate.

That compound is ceftaroline. Ceftaroline fosamil is the water-soluble prodrug used in the intravenous product Teflaro. The patent therefore does not simply claim an unrelated cephalosporin analog. It reaches compositions in which the active ceftaroline is present with its prodrug.

How broad is claim 1 of US 8,247,400?

Claim 1 uses a Markush structure in which R1 may be hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, acyl-derived groups, amino-acid-derived groups, and other substituents. The claim also allows extensive substitution of those groups.

At the claim-language level, claim 1 is broad. Its practical scope is constrained by several factors:

The claimed compound must satisfy the complete formula (I), not merely contain a cephalosporin nucleus.
The permitted R1 substituents must fit the structural definitions in the specification.
A compound must remain within the stereochemical and functional limitations of the formula.
A pharmaceutically acceptable salt is covered only where the underlying compound is itself within the claim.

Claim 2 narrows R1 to hydrogen, alkyl or aryl. Claim 3 narrows the claim to ceftaroline itself. In a validity or infringement analysis, claim 3 is easier to map to a commercial product than claim 1, but it has a materially narrower chemical scope.

The broad genus claim may face greater prior-art exposure than the specific ceftaroline claim. The commercial importance of the patent therefore rests more heavily on claims 4-23 than on the full breadth of claim 1.

What formulations are protected by US Patent 8,247,400?

Claims 4-9 cover compositions containing ceftaroline and ceftaroline fosamil or ceftaroline fosamil acetate.

Composition claim structure

Claim	Required composition or limitation
Claim 4	Ceftaroline, ceftaroline fosamil, ceftaroline fosamil acetate, or a salt or prodrug, together with ceftaroline
Claim 5	Ceftaroline fosamil or ceftaroline fosamil acetate together with ceftaroline
Claim 6	Up to about 10 mg ceftaroline
Claim 7	Up to about 5 mg ceftaroline
Claim 8	Up to about 2.5 mg ceftaroline
Claim 9	Up to about 1 mg ceftaroline

Claims 6-9 are nested limitations. A composition containing 1 mg or less of ceftaroline would generally fall within the numerical ceiling of claims 6, 7, 8 and 9, assuming the other claim elements are satisfied. A composition containing more than 1 mg but no more than 2.5 mg may fall within claims 6-8 but not claim 9.

The phrase “up to about” introduces a claim-construction issue. Courts typically assess the term in view of the specification, examples, analytical tolerances and prosecution history. The scope is not necessarily limited to exact integer amounts.

Why the low-ceftaroline limits matter

The claims may reach a ceftaroline fosamil product that contains ceftaroline as:

An intentionally added component;
A process-related impurity;
A degradation product;
A conversion product formed during manufacture or storage; or
A separately formulated ceftaroline component.

Whether an accused product contains ceftaroline within a claimed amount would require product-specific analytical testing. The claim does not, on its face, require a particular excipient, vial configuration, reconstitution volume, concentration or manufacturing process.

The patent is therefore potentially relevant to products that contain ceftaroline below a specified threshold, even where the principal active pharmaceutical ingredient is ceftaroline fosamil.

Does US Patent 8,247,400 cover Teflaro?

Teflaro is an intravenous ceftaroline fosamil product approved by the FDA for community-acquired bacterial pneumonia and acute bacterial skin and skin structure infections. The labeled adult dose is generally 600 mg administered by intravenous infusion over approximately one hour every 12 hours, with a 400 mg every-12-hour regimen used in certain renal-impairment settings. [2]

Claims 14-18 and 19 directly track these commercial treatment parameters:

600 mg ceftaroline fosamil;
Community-acquired bacterial pneumonia;
Bacterial skin and skin structure infections; and
Administration every 12 hours by intravenous infusion.

Claims 20-23 add the 400 mg regimen and the same every-12-hour intravenous administration schedule.

The claims do not automatically establish infringement by every Teflaro dose. The relevant question is whether the administered composition also contains ceftaroline in the amount required by claims 7-9, and whether the complete composition and method limitations are met.

The patent is strongest against a product or method that intentionally includes a measured amount of ceftaroline with ceftaroline fosamil. It is less direct against a product containing only ceftaroline fosamil unless the claimed ceftaroline component is present and legally attributable to the product.

What method-of-use patents does US Patent 8,247,400 contain?

Claims 10, 11 and 13-23 are method claims. They require administering a composition covered by an earlier composition claim to treat a bacterial infection.

The principal method limitations are:

Method feature	Claims
Treatment of a bacterial infection	10, 11
Community-acquired bacterial pneumonia or bacterial skin and skin structure infection	13, 16, 19, 20, 22
600 mg ceftaroline fosamil	14, 17, 19
400 mg ceftaroline fosamil	20, 22
Intravenous administration every 12 hours	15, 18, 21, 23

These claims are narrower than a general claim to treating bacterial infections with ceftaroline. They require use of a composition that includes the claimed ceftaroline component. A generic product label that omits the patented indications may reduce inducement risk, but it would not resolve composition claims. Conversely, a product that practices the claimed composition could face risk even if the manufacturer does not promote every patented method.

What crystalline form is protected by claim 12?

Claim 12 covers a crystalline form of ceftaroline hydrochloride characterized by an X-ray powder diffraction pattern using CuKα radiation and peaks at approximately:

9.6° 2θ;
20.6° 2θ;
21.9° 2θ;
23.0° 2θ; and
24.3° 2θ,

with a stated tolerance of approximately ±0.2° 2θ.

This is a solid-state claim. It does not require the formulation or dosing limitations in claims 4-11 and 13-23. A product containing a different salt, amorphous material or polymorph may avoid literal infringement of claim 12, subject to equivalence and claim-construction issues.

Analytical comparison would normally require XRPD testing of the isolated drug substance or relevant formulation material. A manufacturer could face a separate risk if its process produces the claimed crystalline hydrochloride form even where the finished dosage form is reconstituted before administration.

When does US Patent 8,247,400 lose exclusivity?

The patent issued on Aug. 21, 2012. Its term is governed by the 20-year patent term measured from the applicable nonprovisional filing date, subject to patent-term adjustment, terminal disclaimers and other statutory provisions. [1]

Public patent records associate the patent with the ceftaroline development program and identify the patent as an issued US composition and treatment patent. The ordinary term analysis places expiration in the late 2020s rather than during the original 2010-2015 launch period. The precise enforceable expiration date must be taken from the USPTO Patent Center term calculation, including any patent-term adjustment.

The expiration of this patent would not necessarily eliminate all US exclusivity for ceftaroline fosamil. Separate patents may cover:

The ceftaroline molecule;
Ceftaroline fosamil;
Manufacturing intermediates;
Salt forms;
Polymorphs;
Pharmaceutical formulations;
Stability improvements; and
FDA-approved uses.

Patent expiry and FDA regulatory exclusivity are separate issues. The FDA approved Teflaro in 2010 under NDA 200327. [2] Any five-year new chemical entity exclusivity associated with the original approval would have expired years before the later patent terms.

What is the Orange Book status of US Patent 8,247,400?

The Orange Book is the FDA’s principal public source for patents submitted for listing against approved small-molecule drug products. It distinguishes patent types such as drug substance, drug product and method-of-use patents. [3]

Because ceftaroline fosamil is a small-molecule injectable product, biosimilar listing rules do not apply. The relevant competitive pathway is an ANDA or, in some circumstances, a 505(b)(2) application.

The commercial significance of US 8,247,400 depends on whether it is listed against the relevant Teflaro NDA and which claims are identified in the listing. A listed formulation or method patent can trigger a Paragraph IV certification by an ANDA applicant. A Paragraph IV certification is an assertion that the listed patent is invalid, unenforceable or not infringed.

A Paragraph IV notice can support patent litigation under Hatch-Waxman. If the NDA holder files suit within the statutory period after receiving notice, FDA approval may be subject to a 30-month stay, subject to statutory exceptions and court developments. [4]

The patent number alone does not establish:

That every claim is Orange Book-listed;
That the patent covers every Teflaro presentation;
That an ANDA applicant has made a Paragraph IV certification; or
That the patent has been asserted in litigation.

Those questions must be resolved from the current Orange Book listing, FDA certifications and court dockets.

Which companies are relevant to the patent landscape?

Entity	Role in the ceftaroline landscape
Cerexa	Original developer and commercialization vehicle for ceftaroline
Forest Laboratories	Historical commercial owner associated with Teflaro
Actavis	Acquired Forest Laboratories and its pharmaceutical assets
Allergan	Later holder of the Forest/Actavis business
AbbVie	Acquired Allergan in 2020
Generic ANDA applicants	Potential challengers after or during remaining listed patent terms

Teflaro’s ownership history does not change the claim scope of US 8,247,400, but it affects the identity of the NDA holder, patent owner and potential Hatch-Waxman plaintiff.

Ceftaroline has no biosimilar pathway because it is a conventional small-molecule antibacterial. Competitive entry would come from generic injectable ceftaroline fosamil products, not from biosimilars.

How strong is the patent estate for ceftaroline fosamil?

US 8,247,400 has a mixed-strength profile.

Stronger elements

The most commercially defensible elements are:

The specific ceftaroline composition claims in claims 4-9;
The 600 mg and 400 mg dosing claims tied to the claimed composition;
The crystalline-form claim if the commercial drug substance uses the claimed XRPD form; and
The linkage between a ceftaroline fosamil product and low levels of ceftaroline.

These claims can create analytical and formulation barriers for an ANDA applicant.

Weaker or more vulnerable elements

The following elements present greater validity or enforcement risk:

The broad Markush genus in claim 1;
The broad compound category in claim 2;
Method claims dependent on proving the composition contains ceftaroline within a numerical limit;
“About” language surrounding the low-dose thresholds; and
Claims requiring a specific crystalline form where the generic manufacturer uses a different solid form.

The estate is narrower than a basic active-ingredient patent but can be more difficult to design around if the commercial product necessarily contains the claimed ceftaroline form or concentration.

What generic launch scenarios exist?

Scenario 1: Launch after patent expiry

A generic applicant waits until the relevant listed patents expire or become unenforceable. This is the lowest litigation-risk pathway but may leave the applicant exposed to other ceftaroline fosamil patents.

Scenario 2: Paragraph IV challenge

The applicant certifies that US 8,247,400 is invalid, unenforceable or not infringed. Likely grounds could include:

The generic product does not contain ceftaroline;
The amount of ceftaroline is outside the claimed range;
The product uses a different salt or crystalline form;
The claims are anticipated or obvious;
The claimed composition lacks adequate written description or enablement; or
The method claims are not practiced by the proposed label.

Scenario 3: Carve-out of patented uses

The applicant may omit or narrow labeling for the patented indications or dosing regimens. This strategy is more relevant to claims 10-11 and 13-23 than to composition claims 4-9.

Scenario 4: Formulation design-around

A manufacturer could seek to avoid the patent by using:

Ceftaroline fosamil without added ceftaroline;
A different salt;
A nonclaimed polymorph or amorphous form;
A manufacturing process that does not produce the claimed crystalline hydrochloride; or
A formulation that does not meet the numerical ceftaroline limits.

The effectiveness of a design-around depends on analytical testing and the application of the doctrine of equivalents.

What litigation or settlement agreements affect US 8,247,400?

The patent record and the claim set alone do not establish a specific final judgment, settlement agreement, license or covenant not to sue for US 8,247,400. Hatch-Waxman activity would need to be assessed from the relevant federal court docket, FDA Paragraph IV records and Orange Book history.

A settlement could alter the practical launch date without changing the patent’s statutory expiration. Common settlement structures include:

A licensed entry date before patent expiry;
Authorized-generic supply;
Restrictions tied to dosage form or indication;
No-challenge provisions; and
Allocation of manufacturing or distribution rights.

No settlement term should be inferred from the existence of the patent or from the Teflaro product history.

How does US 8,247,400 compare with foundational ceftaroline patents?

Patent category	Typical scope	Relationship to US 8,247,400
Ceftaroline composition-of-matter patent	Ceftaroline molecule and salts	Broader product-level protection
Ceftaroline fosamil prodrug patent	Fosamil prodrug and related salts	Protects the commercial prodrug itself
Process patent	Manufacturing route or intermediates	Can block production even after compound claims expire
Formulation patent	Injectable composition, stability or reconstitution	Overlaps with claims 4-9 in a narrower way
Solid-state patent	Specific polymorph or crystalline form	Claim 12 is in this category
Method patent	Indication, dose and administration	Claims 10-11 and 13-23

US 8,247,400 is best characterized as a secondary composition, solid-state and method patent. It does not provide the same breadth as a foundational ceftaroline composition-of-matter patent, but it can extend practical market protection where the claimed composition is used in the marketed product.

Key Takeaways

US 8,247,400 principally covers ceftaroline-containing compositions, especially ceftaroline fosamil combined with low amounts of ceftaroline.
Claim 3 specifically identifies ceftaroline.
Claims 4-9 are the core formulation claims, with ceftaroline limits ranging from up to about 10 mg down to up to about 1 mg.
Claims 10-23 cover treatment of bacterial infections using those compositions, including 400 mg and 600 mg intravenous every-12-hour regimens.
Claim 12 protects a crystalline ceftaroline hydrochloride form defined by five XRPD peaks.
The patent is relevant to Teflaro but does not automatically cover every ceftaroline fosamil product.
Generic risk depends heavily on whether the product contains ceftaroline within the claimed range and whether it uses the claimed crystalline form.
Ceftaroline is a small molecule, so generic competition, not biosimilar competition, is the relevant pathway.
The patent’s enforceable expiration date must be determined from the USPTO term calculation, including patent-term adjustment and any terminal disclaimer.
Orange Book listing status, Paragraph IV certifications, litigation and settlements must be evaluated separately from the patent’s claim language.

FAQs

Is ceftaroline fosamil the same compound as ceftaroline?

No. Ceftaroline fosamil is a prodrug designed for intravenous administration. It is converted in vivo to ceftaroline, the active antibacterial agent.

Does claim 12 cover every form of ceftaroline hydrochloride?

No. Claim 12 is directed to a crystalline form characterized by specified XRPD peaks. A different polymorph, amorphous form or salt may fall outside the literal claim.

Can a generic applicant avoid US 8,247,400 by omitting ceftaroline from its formulation?

Potentially, if the finished product does not contain ceftaroline within the claimed amount and does not use the claimed crystalline form. The conclusion depends on the actual composition and manufacturing process.

Does an ANDA applicant need a Paragraph IV certification for every claim?

The certification must address each relevant listed patent and the applicable patent claims. An applicant may rely on noninfringement, invalidity, unenforceability or a regulatory carve-out, depending on the patent listing and proposed product.

Does expiration of US 8,247,400 permit immediate generic launch?

Not necessarily. Other listed patents, regulatory exclusivity, court orders, settlement agreements or separate manufacturing and formulation patents may delay or restrict launch.

References

United States Patent and Trademark Office. (2012). US Patent No. 8,247,400, compositions and methods for treating bacterial infections.
U.S. Food and Drug Administration. (2010). Teflaro (ceftaroline fosamil) prescribing information.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
U.S. Food and Drug Administration. (2024). Abbreviated new drug application approvals and patent certifications under the Hatch-Waxman Amendments.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Abbvie	TEFLARO	ceftaroline fosamil	POWDER;INTRAVENOUS	200327-001	Oct 29, 2010	AP	RX	Yes	Yes	8,247,400	⤷ Start Trial	Y			METHOD OF TREATING BACTERIAL INFECTIONS	⤷ Start Trial
Abbvie	TEFLARO	ceftaroline fosamil	POWDER;INTRAVENOUS	200327-002	Oct 29, 2010	AP	RX	Yes	Yes	8,247,400	⤷ Start Trial	Y			METHOD OF TREATING BACTERIAL INFECTIONS	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Canada	2753387	⤷ Start Trial
World Intellectual Property Organization (WIPO)	2010096798	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,247,400

Which drugs does patent 8,247,400 protect, and when does it expire?

Summary for Patent: 8,247,400