Details for Patent: 11,117,867

Which drugs does patent 11,117,867 protect, and when does it expire?

Patent 11,117,867 protects ORLADEYO and is included in two NDAs.

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

This patent has twenty-four patent family members in twenty-one countries.

Summary for Patent: 11,117,867

Title:	Crystalline salts of a plasma kallikrein inhibitor
Abstract:	Disclosed are crystalline salts of Compound I, methods of preparing them, and related pharmaceutical preparations thereof. Also disclosed are methods of treatment using the crystalline salts of the invention.
Inventor(s):	Yahya El-Kattan, Yarlagadda S. Babu
Assignee:	Biocryst Pharmaceuticals Inc
Application Number:	US16/784,016
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,117,867
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

US Patent 11,117,867: Scope, Claim Construction, Expiration Risk, and Plasma Kallikrein Inhibitor Patent Landscape

US Patent 11,117,867 protects oral pharmaceutical compositions containing a crystalline salt of a plasma kallikrein inhibitor, particularly a bis(hydrochloride) salt in dose strengths centered on 150 mg. The patent also covers treatment and prevention of hereditary angioedema, including prevention of attacks, reduction in attack frequency, and treatment of acute attacks. Its commercial importance is highest if the marketed product uses the claimed crystalline bis(hydrochloride) salt in a capsule or another oral dosage form.

The claims do not broadly cover every plasma kallikrein inhibitor. They require a crystalline salt of the defined Compound I, an oral dosage form, and a specified quantity of that salt. The method claims incorporate those composition limitations.

What drug and technology does US Patent 11,117,867 cover?

US 11,117,867 is directed to pharmaceutical compositions containing a crystalline salt of Compound I, a plasma kallikrein inhibitor associated with the sebetralstat, also known as KVD900, development program. The patent focuses on solid-state form, salt selection, oral dosage, dose range, and therapeutic use.

The technology has four principal layers:

1. The crystalline salt of Compound I.
2. An oral dosage form containing approximately 75 mg to 250 mg of that salt.
3. Preferred hydrochloride and bis(hydrochloride) salt forms.
4. Treatment or prevention of diseases associated with aberrant plasma kallikrein activity, particularly hereditary angioedema.

The claim set is commercially directed rather than chemically broad. It does not claim the entire molecular class of plasma kallikrein inhibitors.

What are the independent claims in US 11,117,867?

Claims 1, 14, 18, 19, and 20 are the principal independent or independently significant claims.

Claim	Claim type	Principal limitation
1	Composition	Oral pharmaceutical composition containing crystalline salt of Compound I, about 75 mg to about 250 mg
14	Treatment method	Administering the composition to treat a disease involving aberrant plasma kallikrein activity
18	HAE method	Preventing or treating angioedema attacks in hereditary angioedema
19	HAE method	Reducing the frequency of angioedema attacks in hereditary angioedema
20	HAE method	Treating an acute angioedema attack in hereditary angioedema

Claim 1 is the central product claim. Claims 14 through 20 are use claims tied back to the composition of claim 1. A method claim infringement analysis therefore requires examination of the administered product, including its crystalline salt, oral dosage form, and amount.

How broad is claim 1?

Claim 1 has five material limitations:

• A pharmaceutical composition.
• A crystalline salt of Compound I.
• A pharmaceutically acceptable carrier.
• An oral dosage form.
• Approximately 75 mg to approximately 250 mg of the crystalline salt.

The claim is broad as to the identity of the salt within the crystalline-salt category, subject to the Compound I definition in the patent specification. It is not limited to hydrochloride or bis(hydrochloride) salt because those forms are separately addressed in claims 2 and 3.

The claim is narrower than a composition claim covering Compound I in any physical form. An amorphous form, free base, noncrystalline salt, solvate, co-crystal, or different polymorph may fall outside claim 1 unless it is legally characterized as the claimed crystalline salt.

The amount limitation also matters. A product containing less than approximately 75 mg or more than approximately 250 mg may avoid literal infringement of claim 1, although the meaning of "about" would be relevant to the analysis. The patent does not define a single universal tolerance for "about"; courts generally assess the term in view of the specification, prosecution history, technology, and technical meaning.

What formulations are protected by US 11,117,867?

The patent covers oral dosage forms containing the claimed crystalline salt. Claim 12 lists the following forms:

• Capsules
• Ingestible tablets
• Buccal tablets
• Troches
• Elixirs
• Suspensions
• Syrups
• Powders
• Wafers

Claim 13 narrows the protected form to a capsule.

A conventional capsule containing the claimed crystalline bis(hydrochloride) salt at a 150 mg strength is the clearest commercial embodiment within the claim set. The presence of excipients does not ordinarily avoid the claim because claim 1 requires, rather than excludes, a pharmaceutically acceptable carrier.

The patent does not appear, from the supplied claims, to require a particular excipient, release profile, dissolution specification, particle size, capsule shell, manufacturing process, or bioavailability parameter. Those limitations could exist in the specification or prosecution history, but they are not visible in the claims provided.

How do the dose claims overlap?

Claims 4 through 10 create overlapping dose ranges for the bis(hydrochloride) salt.

Claim	Dose range
1	About 75 mg to about 250 mg
4	About 75 mg to about 175 mg
5	About 100 mg to about 250 mg
6	About 100 mg to about 200 mg
7	About 100 mg to about 175 mg
8	About 125 mg to about 250 mg
9	About 125 mg to about 200 mg
10	About 125 mg to about 175 mg
11	About 150 mg

The narrower claims are nested within claim 3 and provide fallback positions if broader ranges are challenged. Claim 11 is particularly important commercially because it isolates the 150 mg dose.

The overlapping structure has two effects. First, a challenge to one range does not necessarily eliminate the entire dose-related claim set. Second, the range claims may face prior-art and obviousness scrutiny if earlier clinical or formulation disclosures identify overlapping dose levels.

Does the patent cover sebetralstat’s active ingredient or only its salt formulation?

The supplied claims primarily protect the crystalline salt and its use in an oral product. They do not independently claim the underlying free-base chemical structure. Any broader compound patent would be a separate member of the patent family or a related patent estate.

This distinction matters for generic entry. A generic manufacturer could attempt to avoid this patent by using a different salt, a noncrystalline form, a different polymorph, or a dose outside the claimed range. That strategy would still face other risks, including compound, method-of-use, formulation, solid-state, process, or regulatory patents.

For an ANDA applicant, the critical question is not simply whether the generic contains the same active moiety. The relevant question is whether the proposed product contains the claimed crystalline salt of Compound I in an oral dosage form and within the claimed quantity.

What are the hereditary angioedema method-of-use claims?

Claims 16 and 17 narrow claim 15 to angioedema and hereditary angioedema. Claims 18 through 20 address distinct clinical objectives:

Claim	Clinical objective
16	Treating angioedema
17	Treating hereditary angioedema
18	Preventing or treating HAE attacks
19	Reducing attack frequency
20	Treating an acute HAE attack

Claim 20 is the most directly aligned with an on-demand oral treatment product. Claim 19 reaches prophylactic or attack-frequency reduction use, depending on the treatment regimen and factual implementation. Claim 18 is broader than claim 20 because it includes both prevention and treatment.

The claims do not specify a particular dosing schedule, biomarker, attack severity, age group, genotype, or clinical endpoint. That breadth may increase commercial coverage but also creates potential validity questions if prior clinical use or publications disclose the same therapeutic purpose and administration of the same composition.

What diseases are covered beyond hereditary angioedema?

Claim 15 lists a broad group of conditions associated with aberrant plasma kallikrein activity, including:

• Stroke
• Inflammation
• Reperfusion injury
• Acute myocardial infarction
• Deep vein thrombosis
• Angina
• Edema
• Sepsis
• Arthritis
• Hemorrhage
• Inflammatory bowel disease
• Diabetes mellitus
• Diabetic retinopathy
• Diabetic macular edema
• Age-related macular degeneration
• Neuropathy
• Hypertension
• Nephropathy
• Brain edema

The breadth of the disease list does not expand the composition claim. A product must still satisfy claim 1. Nor does the list establish that the product is approved for every listed indication. Patent claims and FDA-approved indications are separate legal and regulatory categories.

When does US Patent 11,117,867 expire?

The patent issued on November 9, 2021. Its enforceable term is determined principally by the earliest effective nonprovisional priority date, subject to patent term adjustment, patent term extension, terminal disclaimers, and any applicable regulatory extension under 35 U.S.C. §§ 154 and 156 [1].

The grant date alone does not establish the expiration date. The correct analysis requires the USPTO patent-term record and the patent’s priority and terminal-disclaimer data. A regulatory patent term extension, if granted, would apply only to eligible claims and only within the statutory limits.

Because this patent covers a drug product and therapeutic use rather than merely an abandoned development candidate, the expiration analysis should be performed alongside any related compound, formulation, polymorph, process, and method-of-use patents.

What is the Orange Book status of US 11,117,867?

A US patent is not automatically listed in the FDA Orange Book. Listing depends on FDA approval of the relevant drug product and submission of patent information by the NDA holder under applicable FDA regulations [2].

For an approved drug, Orange Book listing can affect ANDA certification requirements:

• Paragraph I: no patent information has been submitted.
• Paragraph II: the patent has expired.
• Paragraph III: the applicant will wait until patent expiration.
• Paragraph IV: the patent is invalid, unenforceable, or will not be infringed.

The patent claims are potentially suitable for product, formulation, and method-of-use listing if the NDA product practices the claimed crystalline salt, dose, dosage form, or indication. Listing status cannot be inferred from the patent claims alone. It must be confirmed in the current FDA Orange Book and NDA patent submissions.

Which companies could challenge the patent?

The most direct challengers would be generic manufacturers seeking approval of an oral plasma kallikrein inhibitor product that uses the same active moiety or salt. A Paragraph IV challenge could target:

• The crystalline-salt limitation.
• The bis(hydrochloride) limitation.
• The dose range.
• The capsule limitation.
• The written description or enablement of the claimed solid form.
• Anticipation or obviousness based on earlier salt, formulation, or clinical disclosures.
• Indefiniteness of "about."
• The method claims based on prior clinical use or published treatment protocols.

Potential market competitors do not automatically have standing to challenge the patent. A direct challenge generally arises when a company seeks regulatory approval for a product that could trigger an ANDA certification or files a declaratory-judgment action after an asserted infringement threat.

What patent litigation affects US 11,117,867?

The supplied information does not establish a specific infringement case, Paragraph IV notice, inter partes review, post-grant review, or settlement involving Patent 11,117,867. Litigation status should be checked against:

• PACER for district-court infringement actions.
• The USPTO Patent Center for prosecution and post-grant records.
• The Patent Trial and Appeal Board database for IPR and PGR proceedings.
• FDA Orange Book patent listings and ANDA litigation records.

A 30-month stay under the Hatch-Waxman framework would be relevant only if an ANDA applicant filed a Paragraph IV certification and the NDA holder brought an infringement action within the statutory period [2].

How strong is the patent estate?

The patent is strongest against a product that uses all of the following:

• The same Compound I.
• The crystalline salt claimed in the patent.
• An oral dosage form.
• A dose between approximately 75 mg and 250 mg.
• A capsule containing approximately 150 mg of the bis(hydrochloride) salt.
• Use for acute or preventive HAE treatment.

Its strength is lower against a product using a different solid form, different salt, nonoral delivery, a dose outside the claim ranges, or a different active compound.

The patent’s principal vulnerability is claim dependency. The method claims depend on the composition of claim 1, so a successful noninfringement position against the crystalline-salt, oral-form, or dose limitation could affect both product and method claims. The overlapping dependent claims provide redundancy but do not eliminate the need to prove the core limitations.

How does this patent compare with competing HAE products?

Product	Company	General modality	Relevance to Patent 11,117,867
Sebetralstat/KVD900	KalVista	Oral plasma kallikrein inhibitor	Directly relevant if the product uses the claimed crystalline salt and dose
Orladeyo (berotralstat)	BioCryst	Oral plasma kallikrein inhibitor	Competing product; different active ingredient
Takhzyro (lanadelumab)	Takeda	Injectable monoclonal antibody	No direct composition overlap
Firazyr (icatibant)	Takeda	Injectable bradykinin B2 receptor antagonist	No direct composition overlap
C1 esterase inhibitor products	Multiple companies	Plasma-derived or recombinant replacement therapy	No direct composition overlap

The patent is a product-specific barrier within the oral plasma kallikrein inhibitor segment. It does not block competing mechanisms or unrelated HAE products.

What generic launch scenarios exist?

A generic launch could follow several paths:

1. A Paragraph III launch after patent expiration.
2. A Paragraph IV challenge alleging invalidity or noninfringement.
3. A non-infringing formulation using a different salt or solid form.
4. A product limited to an indication not covered by an FDA-listed method-of-use patent, where legally permissible.
5. A settlement with a licensed or delayed-entry date.

A different salt may avoid claims 2 and 3 but still fall within claim 1 if it is the claimed crystalline salt category. A different noncrystalline form may avoid the patent but trigger separate solid-state or formulation patents. A different dose may avoid the literal range but could face other patents and regulatory constraints.

What are the commercial and licensing implications?

The patent has its greatest value when it maps directly onto the commercial presentation. A 150 mg capsule containing the crystalline bis(hydrochloride) salt would likely practice claims 1, 3, 11, and 13, with potential use-claim exposure under claims 18 through 20.

The patent may support:

• Product-level exclusivity for the branded oral presentation.
• Licensing negotiations involving oral HAE therapy.
• Settlement leverage against an ANDA applicant.
• A barrier to salt-form or dose-formulation substitution.
• Extension of commercial protection beyond a basic compound patent.

The claims do not disclose a licensing agreement, co-development arrangement, or settlement. Such rights would need to be confirmed through assignment records, SEC filings, FDA records, and litigation documents.

Key Takeaways

• US 11,117,867 is a formulation, salt-form, dose, and method-of-use patent.
• Its central commercial embodiment is an oral capsule containing approximately 150 mg of crystalline bis(hydrochloride) Compound I.
• The method claims cover treatment and prevention of hereditary angioedema, including acute attacks and attack-frequency reduction.
• The patent does not broadly claim every plasma kallikrein inhibitor or every formulation of the active moiety.
• Alternative salts, noncrystalline forms, different doses, and different active ingredients may create design-around opportunities.
• Orange Book listing, patent expiration, Paragraph IV activity, and litigation status require record-level verification and cannot be inferred solely from the supplied claims.
• The patent is most valuable when paired with separate compound, polymorph, manufacturing, formulation, and regulatory-exclusivity rights.

FAQs

Does US 11,117,867 protect a 150 mg HAE capsule?

Yes, if the capsule contains the claimed crystalline salt of Compound I, particularly the bis(hydrochloride) salt. Claim 11 expressly recites about 150 mg, and claim 13 recites a capsule.

Can a generic avoid Patent 11,117,867 by using the free base?

Potentially. The claims require a crystalline salt, so a free-base product may avoid literal infringement. The generic would still need to assess other patents and whether the proposed product can satisfy FDA equivalence requirements.

Does claim 20 cover only acute hereditary angioedema attacks?

Claim 20 specifically covers treating an acute angioedema attack in a subject with hereditary angioedema. It is narrower than claim 18, which covers prevention or treatment of attacks.

Are the overlapping dose ranges separate patent protections?

Yes. Claims 4 through 10 are separate dependent claims with different overlapping ranges. Their practical value depends on validity, claim construction, and whether the marketed product falls within each range.

Does an Orange Book listing guarantee protection from generic launch?

No. A listing can require an ANDA applicant to make a patent certification and can trigger litigation consequences, but a generic may challenge the patent, prevail on noninfringement or invalidity, obtain a settlement right, or launch after expiration.

References

1. United States Patent and Trademark Office. (2021). U.S. Patent No. 11,117,867, pharmaceutical composition and methods of use involving crystalline salt of Compound I. U.S. Department of Commerce.

2. U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations: Orange Book. U.S. Department of Health and Human Services.

3. U.S. Food and Drug Administration. (2024). Regulations governing submission of patent information and certifications for approved drug products. 21 C.F.R. §§ 314.50, 314.53, 314.107.

4. United States Congress. (2024). Patent term adjustment and patent term extension. 35 U.S.C. §§ 154, 156.

Drugs Protected by US Patent 11,117,867

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Biocryst	ORLADEYO	berotralstat dihydrochloride	CAPSULE;ORAL	214094-001	Dec 3, 2020		RX	Yes	No					Y
Biocryst	ORLADEYO	berotralstat dihydrochloride	CAPSULE;ORAL	214094-002	Dec 3, 2020		RX	Yes	Yes					Y
Biocryst	ORLADEYO	berotralstat dihydrochloride	PELLETS;ORAL	219776-001	Dec 11, 2025		RX	Yes	No					Y
Biocryst	ORLADEYO	berotralstat dihydrochloride	PELLETS;ORAL	219776-002	Dec 11, 2025		RX	Yes	No					Y
Biocryst	ORLADEYO	berotralstat dihydrochloride	PELLETS;ORAL	219776-003	Dec 11, 2025		RX	Yes	No					Y

International Family Members for US Patent 11,117,867

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	116951
Australia	2019374115
Brazil	112021008249
Canada	3117123
Chile	2021001094