Details for Patent: 10,385,067

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Which drugs does patent 10,385,067 protect, and when does it expire?

Patent 10,385,067 protects BIKTARVY, BIXLENVO, and BIXLENVO SUNLENCA STARTER PACK (COPACKAGED), and is included in three NDAs.

This patent has sixty-seven patent family members in forty-three countries.

Summary for Patent: 10,385,067

Title:	Sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate
Abstract:	The present invention relates to sodium (2R,5S,13aR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepin-8-olate Form I, pharmaceutical formulations, and uses thereof for treating or prophylactically preventing an HIV infection.
Inventor(s):	Ernest A. Carra, Irene Chen, Vahid Zia
Assignee:	Gilead Sciences Inc
Application Number:	US15/624,166
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,385,067
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

US Patent 10,385,067: Lenacapavir Crystalline-Form Claims, Exclusivity and Generic Risk

US Patent No. 10,385,067 protects the use of a specific crystalline form of lenacapavir, the HIV capsid inhibitor marketed by Gilead Sciences as Sunlenca. The patent does not broadly claim every lenacapavir formulation or every use of lenacapavir. Its enforceable scope is concentrated on administering crystalline Formula II, identified by specified XRPD characteristics, to treat HIV infection.

The patent was granted on August 20, 2019, from a December 2017 application claiming priority to a 2016 filing. Its ordinary expiration date is expected to fall in December 2037, subject to the patent-term-adjustment calculation and any applicable patent-term extension. The claims cover both administration of the crystalline active pharmaceutical ingredient and administration in pharmaceutical compositions, including combinations with tenofovir and emtricitabine. [1]

What drug does US Patent 10,385,067 protect?

Formula II in US 10,385,067 corresponds to lenacapavir, also known as GS-6207, the active ingredient in Sunlenca. Lenacapavir is a first-in-class HIV capsid inhibitor approved for treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV whose current antiretroviral regimen is failing because of resistance, intolerance, or safety considerations. [2]

Sunlenca is supplied as:

Product	Active ingredient	FDA dosage form
Sunlenca tablets	Lenacapavir sodium	Oral tablets
Sunlenca injection	Lenacapavir sodium	Subcutaneous injection

The patent claims are directed to the crystalline form of Formula II rather than to the generic pharmacological concept of HIV capsid inhibition. The crystalline-form limitation is central to infringement analysis.

What are the claims of US 10,385,067?

The independent claims divide into two groups.

Claim group	Subject matter	Principal limitation
Claim 1	Treatment method	Administering crystalline Formula II to treat HIV
Claim 10	Composition-based treatment method	Administering a composition containing crystalline Formula II and a carrier or excipient

Claims 2 through 9 narrow claim 1. Claims 11 through 19 narrow claim 10.

Claims 1 through 9: crystalline Formula II

Claim 1 requires all of the following:

1. A human with an HIV infection.
2. Administration of a therapeutically effective amount.
3. Formula II in crystalline form.
4. An XRPD pattern with peaks at approximately:
   • 5.5° 2-theta;
   • 16.1° 2-theta; and
   • 23.3° 2-theta.

The permitted variance is approximately ±0.2° 2-theta.

The dependent claims add increasingly specific analytical and physical-state limitations:

Claim	Added limitation
2	Additional XRPD peaks at approximately 22.1° and 28.5°
3	Additional XRPD peaks at approximately 22.5° and 19.5°
4	Additional XRPD peaks at approximately 26.6° and 17.9°
5	XRPD pattern substantially as shown in Figure 1
6	DSC pattern substantially as shown in Figure 2
7	DVS pattern substantially as shown in Figure 4
8	Partially or fully hydrated form
9	Anhydrous or essentially anhydrous form

The claims therefore create multiple overlapping identification routes. A potentially infringing product could be captured by the required XRPD peaks even if its hydration state differs. Conversely, a product that has the same molecular structure but a materially different crystalline form may fall outside the literal scope of the claims.

How does the XRPD limitation affect patent scope?

The XRPD requirement is a product-form limitation embedded in a method-of-treatment claim. The patent does not merely require administration of lenacapavir. It requires administration of a solid form exhibiting defined diffraction peaks.

XRPD is commonly used to distinguish crystalline polymorphs, solvates, hydrates, and amorphous material. The claim’s core technical boundary is therefore the diffraction pattern rather than the manufacturing process used to produce the material.

A generic or follow-on manufacturer would generally need to evaluate:

• Whether its lenacapavir active ingredient is crystalline.
• Whether the material produces the claimed peaks within the stated tolerance.
• Whether the peaks arise from the same polymorph, hydrate, solvate, or mixed solid form.
• Whether the commercial product is administered for a claimed HIV treatment use.
• Whether the product’s regulatory label includes a use that falls within the claims.

The specification’s “substantially as set forth” limitations in claims 5 through 7 may require comparison of the overall analytical pattern, not merely isolated peaks. Courts typically construe such terms in view of the specification, figures, analytical methods, and prosecution history. [3]

Hydrated and anhydrous forms

Claims 8 and 9 extend the dependent-claim structure to both hydrated and anhydrous material. This is commercially important because pharmaceutical solids can change hydration state during drying, storage, milling, compression, and exposure to humidity.

Claim 8 covers partially or fully hydrated material. Claim 9 covers anhydrous or essentially anhydrous material. The combination reduces the likelihood that a manufacturer can avoid the narrower dependent claims merely by controlling water content while retaining the claimed XRPD identity.

The claims do not expressly require a particular tablet strength, injection strength, excipient, manufacturing process, or dosing interval.

What formulations are protected by US 10,385,067?

Claims 10 through 19 cover treatment using a pharmaceutical composition containing crystalline Formula II and a pharmaceutically acceptable carrier or excipient.

The composition claims include:

• One to three additional therapeutic agents.
• Combination treatment with anti-HIV drugs.
• Protease inhibitors.
• Non-nucleoside reverse-transcriptase inhibitors.
• Nucleoside reverse-transcriptase inhibitors.
• Nucleotide reverse-transcriptase inhibitors.
• Pharmacokinetic enhancers.
• Other HIV therapies.
• Tenofovir disoproxil fumarate and emtricitabine.
• Tenofovir alafenamide and emtricitabine.
• Tenofovir alafenamide hemifumarate and emtricitabine.
• Unit dosage forms.
• Tablets.

Claim	Formulation scope
10	Crystalline Formula II plus carrier or excipient
11	One to three additional therapeutic agents
12	Additional agents are anti-HIV drugs
13	Specified HIV drug classes and pharmacokinetic enhancers
14	At least one nucleoside reverse-transcriptase inhibitor
15	Tenofovir disoproxil fumarate plus emtricitabine
16	Tenofovir alafenamide plus emtricitabine
17	Tenofovir alafenamide hemifumarate plus emtricitabine
18	Unit dosage form
19	Tablet

The composition claims may be relevant to a future fixed-dose combination containing lenacapavir, tenofovir, and emtricitabine. They also create potential method-of-use exposure for a product supplied as a tablet, even if the manufacturer avoids practicing a particular manufacturing process.

Is US 10,385,067 a product patent or a method-of-use patent?

US 10,385,067 is principally a method-of-treatment patent.

It does not present the independent claims as:

• A composition of matter for lenacapavir;
• A standalone crystalline compound claim;
• A tablet claim independent of treatment;
• An injectable pharmaceutical composition claim; or
• A process for making the crystalline form.

Instead, the independent claims require administering the crystalline material to a human for treatment of HIV. This distinction affects both litigation and generic launch analysis.

A manufacturer may possess or sell a crystalline lenacapavir product without necessarily infringing the patent in every circumstance. Infringement risk rises when the product is submitted for approval, labeled, marketed, or distributed for the claimed HIV treatment use.

What is the Orange Book status of US 10,385,067?

Sunlenca is an FDA-approved small-molecule drug. Its patent and exclusivity analysis is therefore governed by the Hatch-Waxman framework and the FDA Orange Book rather than the biosimilar framework. [4]

A patent can be relevant to the Orange Book if it claims the approved drug, a method of using the approved drug, or an approved drug product. A method-of-use patent generally must be tied to an approved use and accompanied by the required use code.

The commercial questions are:

Issue	Effect
Orange Book listing	Can require an ANDA applicant to make a patent certification
Paragraph IV certification	Applicant alleges the patent is invalid, unenforceable, or not infringed
Paragraph III certification	Applicant accepts patent expiry and delays approval
30-month stay	May arise if the NDA holder or patent owner files suit within the statutory period
Skinny label	May reduce risk for a method patent if the patented use can be carved out
Product-form limitation	Requires solid-state comparison and potential non-infringement analysis

The exact current Orange Book listing, use code, and delisting status should be determined from the FDA’s current Approved Drug Products with Therapeutic Equivalence Evaluations database. [5] The patent’s presence in the patent family does not by itself establish that every related patent remains listed for Sunlenca.

When does US 10,385,067 lose exclusivity?

The nominal patent expiration date is expected to be in December 2037, based on the patent’s priority and filing history. The legally operative date should be calculated from the issued patent record, including patent-term adjustment and any terminal disclaimer.

Milestone	Date or period
Earliest claimed priority	December 2016
US application filing	December 2017
Patent grant	August 20, 2019
Nominal 20-year term basis	December 2037
Earliest ordinary generic entry	After applicable patent and regulatory barriers expire
Possible earlier entry	Successful Paragraph IV litigation or settlement

FDA regulatory exclusivity is separate from patent exclusivity. Sunlenca received approval in 2022. Regulatory exclusivity periods, if applicable, do not automatically extend the patent term. Conversely, expiration of FDA exclusivity would not eliminate a valid unexpired patent. [2, 4]

A patent-term extension under 35 U.S.C. § 156 is a separate possibility for an approved drug, but it cannot be assumed from the patent grant or the FDA approval alone. [6]

Are there Paragraph IV challenges to Sunlenca patents?

A Paragraph IV challenge would be the principal ANDA pathway for an earlier generic launch against a listed Sunlenca patent. The applicant would allege that the patent is invalid, unenforceable, or not infringed.

For US 10,385,067, likely challenge theories would include:

Non-infringement

A generic applicant could argue that its lenacapavir:

• Is amorphous rather than crystalline;
• Is a different polymorph;
• Does not exhibit the claimed XRPD peaks;
• Falls outside the ±0.2° 2-theta limitation;
• Is not hydrated or anhydrous in the claimed manner;
• Is not marketed for the patented method of treatment; or
• Uses a label that omits the patented use where legally permissible.

Invalidity

Potential invalidity theories could include:

• Anticipation by an earlier disclosure of the same crystalline form;
• Obviousness based on known lenacapavir forms and routine solid-state screening;
• Lack of written description for the full range of hydration states;
• Lack of enablement for the claimed analytical and physical-form range;
• Indefiniteness in terms such as “substantially as set forth” or “essentially anhydrous.”

The strength of these defenses depends heavily on the specification, priority disclosure, prosecution history, cited prior art, and analytical reproducibility. The claim set is narrower than a broad active-ingredient claim but may be stronger against products using the commercial crystalline form.

No conclusion that a Paragraph IV challenge exists should be drawn solely from the patent claims. A definitive assessment requires a current FDA Orange Book review and federal court docket search.

What patent litigation affects lenacapavir?

The relevant litigation risk is likely to concentrate around three patent categories:

Patent category	Typical subject matter	Relevance
Core compound patents	Lenacapavir chemical structure	Broadest molecular protection
Solid-state patents	Crystalline, hydrated, anhydrous, or polymorphic forms	Direct relevance to US 10,385,067
Formulation and use patents	Tablets, injections, dosing regimens, combinations	Product-specific launch barriers

US 10,385,067 is most relevant where a challenger’s product uses the same crystalline form. It may be less effective against a deliberately engineered alternative solid form, provided that alternative does not meet the claimed XRPD limitations and does not fall within other Gilead patents.

The litigation value of the patent is therefore dependent on the commercial solid form used in the reference product and on whether the same form is necessary to achieve adequate stability, manufacturability, bioavailability, or regulatory comparability.

How strong is the patent estate for lenacapavir?

The individual patent has a focused but commercially meaningful scope.

Strength factor	Assessment
Remaining term	Long, with nominal expiry in 2037
Claim type	Method of treatment, not broad composition of matter
Technical specificity	High; XRPD, DSC, DVS, hydration-state limitations
Design-around potential	Moderate, depending on alternative polymorph availability
Regulatory leverage	Potentially significant if listed in the Orange Book
Litigation complexity	High because infringement may require solid-state testing
Biosimilar relevance	None; lenacapavir is a small molecule
Combination relevance	Significant for future fixed-dose HIV regimens

The patent is strongest when the reference product and proposed generic use the same crystalline form. It is weaker as a standalone barrier against a product that uses a distinct, non-infringing form and omits any patented indication from its label.

The broader commercial position depends on the rest of the lenacapavir patent family. A generic applicant would need to clear core compound, crystalline-form, formulation, dosing, manufacturing, and use patents as a portfolio rather than evaluate US 10,385,067 in isolation.

Does biosimilar risk apply to Sunlenca?

No. Sunlenca is a small-molecule drug, not a biological product. A follow-on manufacturer would generally pursue an abbreviated new drug application under section 505(j) of the Federal Food, Drug, and Cosmetic Act, not a biosimilar application under section 351(k) of the Public Health Service Act.

The relevant competitive threat is therefore generic substitution through an ANDA, subject to:

• Pharmaceutical equivalence;
• Bioequivalence;
• Labeling requirements;
• Orange Book patent certifications;
• Patent litigation;
• Solid-state and formulation equivalence;
• Manufacturing scale-up.

Are there licensing deals affecting lenacapavir patent rights?

Gilead has entered licensing and access arrangements involving lenacapavir, particularly in the context of broader HIV access and potential prevention use. Public licensing activity does not automatically establish that US 10,385,067 is licensed for commercial treatment use in the United States.

The commercial effect of any license depends on:

• Geographic scope;
• Indication scope;
• Treatment versus prevention rights;
• Formulation rights;
• Patent rights expressly licensed;
• Regulatory territory;
• Royalty and supply terms;
• Whether the license authorizes commercial manufacture or only access programs.

The patent assignment record identifies Gilead-related ownership, but assignment and licensing status should be distinguished. A license may authorize conduct without changing the recorded patent owner.

What generic launch scenarios exist for lenacapavir?

Scenario 1: Launch after patent expiry

This is the lowest litigation-risk scenario. The applicant accepts the listed patents and launches after the relevant patent term and regulatory exclusivity periods expire.

Scenario 2: Paragraph IV challenge

The applicant files an ANDA with a Paragraph IV certification and argues that the crystalline-form claims are invalid or not infringed. Gilead may file an infringement action, potentially triggering a 30-month stay of approval under the Hatch-Waxman statute. [7]

Scenario 3: Non-infringing polymorph

The applicant develops a different crystalline or amorphous form. This approach requires evidence that the alternative form is stable, manufacturable, bioequivalent, and outside the claimed XRPD pattern. It must also clear other lenacapavir patents.

Scenario 4: Skinny-label launch

The applicant removes a patented indication or method from its labeling where FDA rules permit the carve-out. This strategy is less useful if the approved label is narrow and the remaining indication still practices the patent.

Scenario 5: Settlement or licensed entry

The parties may agree to an authorized entry date, license, supply arrangement, or other settlement structure. No specific settlement involving US 10,385,067 should be inferred without a filed agreement, court docket, or public company disclosure.

Key Takeaways

• US 10,385,067 protects treatment of HIV using crystalline Formula II, identified as lenacapavir.
• The claims depend on XRPD peaks centered at approximately 5.5°, 16.1°, and 23.3° 2-theta.
• Dependent claims add further XRPD peaks, DSC, DVS, hydrated states, anhydrous states, combination agents, and tablet dosage forms.
• The patent is a method-of-treatment patent, not a standalone composition-of-matter patent.
• Claims 15 through 17 specifically cover compositions containing lenacapavir with tenofovir and emtricitabine variants.
• The nominal patent term extends into December 2037, subject to the official patent-term calculation.
• Generic risk will turn on Orange Book listing, Paragraph IV certifications, solid-state testing, label scope, and the remaining lenacapavir patent portfolio.
• Biosimilar competition is not the relevant pathway because Sunlenca is a small molecule.
• The patent is commercially strongest against products using the same crystalline form as the reference product.
• A different polymorph, amorphous form, skinny label, Paragraph IV challenge, or negotiated entry could reduce the patent’s blocking effect.

FAQs About US Patent 10,385,067 and Lenacapavir

Does US 10,385,067 cover all lenacapavir products?

No. It covers treatment methods using crystalline Formula II meeting specified analytical characteristics. Other lenacapavir forms may fall outside these claims but could be covered by separate patents.

Does the patent cover Sunlenca injection?

Potentially, depending on the solid form in the injectable product and the applicable claim construction. The claims do not expressly require a tablet, so the core treatment claims are not limited to oral administration.

Can a generic manufacturer avoid US 10,385,067 by using amorphous lenacapavir?

Possibly, but only if the amorphous product does not convert to the claimed crystalline form during manufacture, storage, administration, or testing and is not covered by another patent.

Are claims 15 through 17 fixed-dose combination claims?

They are method-of-treatment claims requiring administration of a composition containing crystalline Formula II with specified tenofovir and emtricitabine combinations. They are not standalone composition claims.

What is the primary patent risk for a lenacapavir generic?

The primary risk is cumulative portfolio exposure. A generic must evaluate the core lenacapavir compound, crystalline-form, formulation, dosing, manufacturing, and method-of-use patents, not US 10,385,067 alone.

References

1. United States Patent and Trademark Office. (2019). US Patent No. 10,385,067, crystalline forms and methods of use.
2. U.S. Food and Drug Administration. (2022). Sunlenca (lenacapavir) prescribing information.
3. United States Patent and Trademark Office. (2024). Manual of Patent Examining Procedure, sections concerning claim construction, written description, enablement, and definiteness.
4. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations.
5. U.S. Food and Drug Administration. (2024). Orange Book: Approved drug products with therapeutic equivalence evaluations.
6. United States Code. (2024). 35 U.S.C. § 156: Extension of patent term.
7. United States Code. (2024). 21 U.S.C. § 355: New drugs and abbreviated applications.

Drugs Protected by US Patent 10,385,067

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Gilead Sciences Inc	BIKTARVY	bictegravir sodium; emtricitabine; tenofovir alafenamide fumarate	TABLET;ORAL	210251-002	Oct 7, 2021		RX	Yes	No						TREATMENT OF HIV INFECTION
Gilead Sciences Inc	BIKTARVY	bictegravir sodium; emtricitabine; tenofovir alafenamide fumarate	TABLET;ORAL	210251-001	Feb 7, 2018		RX	Yes	Yes						TREATMENT OF HIV INFECTION
Gilead Sciences Inc	BIXLENVO	bictegravir sodium; lenacapavir sodium	TABLET;ORAL	221104-001	Aug 27, 2026		RX	Yes	Yes						TREATMENT OF HIV-1 IN ADULTS TO REPLACE THE CURRENT ANTIRETROVIRAL REGIMEN IN THOSE WHO ARE VIROLOGICALLY SUPPRESSED ON A STABLE ANTIRETROVIRAL REGIMEN

International Family Members for US Patent 10,385,067

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	100903
Australia	2015276860
Australia	2018203175