Details for Patent: 8,536,122

Which drugs does patent 8,536,122 protect, and when does it expire?

Patent 8,536,122 protects OZEMPIC, WEGOVY, and RYBELSUS, and is included in four NDAs.

This patent has forty-two patent family members in twenty-two countries.

Summary for Patent: 8,536,122

Title:	Acylated GLP-1 compounds
Abstract:	Protracted GLP-1 compounds and therapeutic uses thereof.
Inventor(s):	Jesper Lau, Florencio Zaragoza Doerwald, Paw Bloch, Thomas Kruse Hansen
Assignee:	Novo Nordisk AS
Application Number:	US13/412,283
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,536,122
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 8,536,122: Semaglutide Claim Scope, Patent Landscape, and Generic Entry Risk

U.S. Patent No. 8,536,122 covers a broad genus of acylated GLP-1 analogs and expressly includes semaglutide-related structures, particularly Aib8, Aib22, Arg34-GLP-1 analogs carrying a long-chain acidic substituent. The patent was assigned to Novo Nordisk and is a foundational U.S. patent for semaglutide products, including Ozempic, Rybelsus, and Wegovy.

The patent’s principal commercial relevance is claim 9, which identifies Aib8, Arg34-GLP-1(7-37) and Aib8,22, Arg34-GLP-1(7-37). The latter is the peptide backbone of semaglutide. Claims 10 through 12 address the spacer and acidic lipid-containing substituent used to extend half-life. Claims 13 through 16 cover pharmaceutical compositions and treatment of hyperglycemia and type 2 diabetes.

What drug does U.S. Patent 8,536,122 protect?

U.S. Patent 8,536,122 protects GLP-1 analogs that combine selected peptide substitutions with a covalently attached spacer and acidic group. Semaglutide is the most commercially important compound falling within the disclosed and claimed subject matter.

Product	Active ingredient	Relationship to U.S. 8,536,122
Ozempic	Semaglutide injection	Covered by composition and method claims
Rybelsus	Oral semaglutide	Covered by compound, composition, and treatment claims, subject to product-specific patent listings
Wegovy	Higher-dose semaglutide injection	Covered by compound and treatment claims
Victoza	Liraglutide	Structurally related GLP-1 analog, but not the principal commercial embodiment of this patent
Trulicity	Dulaglutide	Different GLP-1 receptor agonist and not the claimed semaglutide structure
Mounjaro/Zepbound	Tirzepatide	GIP/GLP-1 agonist with a different peptide architecture

Semaglutide differs from native GLP-1 through, among other modifications, Aib at position 8, Aib at position 22, Arg at position 34, and acylation of Lys26 with a linker and C18 fatty diacid substituent. Those modifications improve metabolic stability, albumin binding, and dosing duration.

What are the broadest claims in U.S. Patent 8,536,122?

Claim 1 is the broad independent compound claim. It covers a formula II GLP-1 analog having:

• A variable amino acid at position 7, including histidine and multiple histidine or pyridylalanine alternatives.
• A variable residue at position 8, including Gly, Val, Leu, Ile, Lys, Aib, and cyclic amino acids.
• Defined substitutions at positions 16, 18, 19, 20, 22, 23, 25, 27, 33, 34, and 35.
• Optional residues or deletions at positions 36 through 38.
• A spacer U with variable linker lengths and compositions.
• An acidic group B attached through the spacer.

The claim is a combination claim. A competing molecule must satisfy both the peptide limitations and the acyl-linker limitations to fall literally within claim 1.

How does claim 1 differ from the narrower claims?

Claims 2 through 8 narrow the amino-acid sequence. They reduce the number of permitted substitutions and focus the claim set on GLP-1 analogs more closely related to GLP-1(7-37).

Claims 4 and 5 specifically require Gly8 or Aib8, with claim 5 limited to Aib8. Claim 6 allows no more than six exchanges, additions, or deletions compared with GLP-1(7-37), while claim 7 permits no more than three.

Claim 8 requires only one lysine residue. This limitation is relevant because the acyl group must be attached at a defined lysine site without competing lysine residues that could create positional isomers.

Claim 9 identifies specific analogs:

1. Aib8, Arg34-GLP-1(7-37); and
2. Aib8,22, Arg34-GLP-1(7-37).

The second species corresponds to the central semaglutide peptide sequence. The claim still must be read together with the compound structure and any applicable spacer and acidic-group limitations.

Does U.S. Patent 8,536,122 cover semaglutide?

Yes. Semaglutide falls within the technical disclosure and claim architecture of the patent. Its relevant structural elements include:

Semaglutide element	Claimed feature
Aib at position 8	Claim 5 and claim 9
Aib at position 22	Claim 9
Arg at position 34	Claim 9
GLP-1(7-37) backbone	Claims 1 through 9
Lys26 acylation	Formula II and spacer provisions
Hydrophilic linker	Claims 1, 10, and 11
Long-chain acidic fatty substituent	Formula II and claims 10 through 12
Diabetes treatment	Claims 15 and 16

The supplied claim text contains transcription defects. It repeats “Xaa33” with different amino-acid lists, omits the displayed chemical structures for U and B, and contains malformed language in several dependent claims. Those defects prevent a complete reconstruction of every literal Markush alternative from the text alone. The issued patent drawings, sequence listings, and official claim record control the precise scope.

What formulations are protected by U.S. Patent 8,536,122?

Claims 13 and 14 cover pharmaceutical compositions comprising a claimed GLP-1 analog and a pharmaceutically acceptable excipient. These are composition claims rather than detailed formulation claims.

The patent does not, based on the supplied claims, require a particular:

• Injection concentration
• Buffer system
• Preservative
• Device
• Tablet coating
• Absorption enhancer
• Dosage regimen
• Route of administration

A product can infringe a composition claim if it contains a claimed compound, even if the excipients or delivery device differ. Formulation-specific protection may arise from separate Novo Nordisk patents directed to oral delivery, tablet compositions, injection formulations, or dosing regimens.

Does the patent protect oral semaglutide?

The compound claims are route-neutral. Claims 13 and 14 are also not limited to injection. Claims 15 and 16 address treatment of hyperglycemia and type 2 diabetes without specifying a particular route.

That structure creates a potential basis for coverage of oral semaglutide, but the relevant Orange Book listing and infringement analysis depend on the specific Rybelsus formulation and the separate patents listed for that product.

What method-of-use claims does U.S. Patent 8,536,122 contain?

Claims 15 and 16 cover administering a claimed GLP-1 analog to treat:

• Hyperglycemia
• Type 2 diabetes

The claims do not require a particular dose, titration schedule, frequency, administration device, or patient subgroup. They are therefore broader than a narrowly drafted regimen claim, although their enforceability depends on the precise product, indication, prescribing information, and induced-infringement facts.

The patent does not, based on the supplied claims, expressly cover obesity, cardiovascular-risk reduction, chronic kidney disease, or obstructive sleep apnea. Those indications may be covered by later patents or regulatory exclusivities associated with Wegovy or other semaglutide products.

When does U.S. Patent 8,536,122 lose exclusivity?

The commonly reported U.S. expiration date for U.S. Patent 8,536,122 is March 20, 2026, subject to the patent’s recorded term adjustment and any applicable regulatory extension. The controlling date should be confirmed against the current USPTO Patent Center record and FDA Orange Book listing.[1][2]

Event	Date or status
U.S. patent grant	September 17, 2013
Patent number	8,536,122
Patent holder	Novo Nordisk A/S
Core subject matter	Acylated GLP-1 analogs
Principal commercial molecule	Semaglutide
Reported U.S. patent expiration	March 20, 2026
Regulatory exclusivity	Product-specific and separate from patent term
Post-expiration risk	ANDA or 505(b)(2) entry, subject to other unexpired patents

Expiration of this patent alone would not necessarily permit unrestricted semaglutide entry. Later patents may cover semaglutide compositions, manufacturing methods, oral formulations, dosing regimens, or specific indications.

What other patents protect semaglutide after U.S. 8,536,122?

The semaglutide estate includes multiple patent families. The most important categories are:

Patent category	Protected subject matter	Commercial effect
Core compound patents	Semaglutide peptide and acylated GLP-1 analogs	Protect the active pharmaceutical ingredient
Formulation patents	Injectable or oral semaglutide compositions	Can delay product-specific entry
Oral-delivery patents	Semaglutide with absorption enhancers such as SNAC	Relevant primarily to Rybelsus
Manufacturing patents	Peptide synthesis, acylation, purification, and processing	Raise development and scale-up risk
Method-of-use patents	Diabetes, obesity, weight management, and related indications	Create use-code and carve-out issues
Dosing patents	Titration, maintenance dosing, and specific treatment regimens	Support infringement allegations against labeled use
Device patents	Prefilled pens and delivery systems	May affect device substitution and combination products

A widely cited later Novo Nordisk family includes U.S. Patent No. 9,266,951, which has been associated with semaglutide protection extending into 2031. Other later patents may have different expiration dates and may apply differently to Ozempic, Rybelsus, and Wegovy.[3]

What is the Orange Book status of semaglutide?

FDA Orange Book listings are product-specific. A patent listed for Ozempic is not automatically listed for Rybelsus or Wegovy, and each product may have different patents and use codes.

The Orange Book analysis should separate:

1. Ozempic injection patents.
2. Rybelsus oral-tablet patents.
3. Wegovy injection and obesity-treatment patents.
4. Device or combination-product listings.
5. Patents with method-of-use codes.
6. Patent term and regulatory exclusivity dates.

U.S. 8,536,122 has been treated as a foundational semaglutide patent in public patent databases and product patent analyses. The practical effect of its expiration depends on whether later Orange Book-listed patents remain enforceable against the proposed generic or 505(b)(2) product.[2]

Which companies are challenging semaglutide patents?

Generic and specialty pharmaceutical companies have pursued or publicly reported Paragraph IV challenges to semaglutide patents. Publicly reported challengers have included companies such as Mylan/Viatris, Sun Pharmaceutical Industries, Aurobindo-related entities, Dr. Reddy’s Laboratories, Hetero, Zydus, and other ANDA applicants.

The litigation pattern is typical for a high-value peptide product:

• ANDA applicants provide Paragraph IV notices.
• Novo Nordisk files patent-infringement actions under the Hatch-Waxman Act.
• The statutory 30-month stay may delay FDA approval of the challenged ANDA.
• The litigation may resolve before trial through dismissal, judgment, license, or settlement.
• A successful Paragraph IV judgment can create an earlier launch opportunity.
• A non-infringement or invalidity judgment may affect only the patents and products before the court.

The existence of a Paragraph IV filing does not establish that the challenger will launch. It establishes that the applicant has certified that one or more listed patents are invalid, unenforceable, or not infringed.

What generic entry risks exist after the patent expires?

Semaglutide presents higher entry barriers than a conventional small-molecule generic.

Regulatory barriers

Semaglutide is a synthetic peptide administered by injection or formulated for oral delivery. FDA approval may involve:

• Complex analytical characterization
• Demonstration of peptide identity and purity
• Impurity and aggregate control
• Device compatibility for injectable products
• Comparative pharmacokinetic or clinical data
• Product-specific requirements for oral absorption
• Interchangeability issues for biological or peptide products

An ANDA applicant must also address Orange Book-listed patents. A 505(b)(2) applicant may face separate patent and clinical-development obligations.

Manufacturing barriers

Semaglutide production requires control over:

• Solid-phase peptide synthesis
• Unnatural amino acids such as Aib
• Site-selective acylation
• Linker attachment at Lys26
• Long-chain fatty diacid chemistry
• Purification and impurity removal
• Batch consistency
• Aggregation and stability

A process that avoids Novo Nordisk manufacturing patents may require different reaction sequences, protecting groups, purification systems, or acylation methods. Process freedom to operate is therefore separate from compound-patent freedom to operate.

Commercial barriers

The incumbent has substantial advantages in:

• Prescriber familiarity
• Supply-chain scale
• Injection-device infrastructure
• Insurance coverage
• Clinical-outcomes data
• Brand recognition
• Manufacturing capacity

A first generic or 505(b)(2) entrant may still obtain significant value through limited competition, authorized-generic arrangements, hospital channels, or niche distribution.

How strong is the patent estate for semaglutide?

The estate is strong in commercial breadth but time-limited at the core-compound level.

Factor	Assessment
Core molecule coverage	Strong; claim 9 directly identifies the semaglutide backbone
Genus coverage	Broad; claim 1 covers numerous sequence and linker alternatives
Formulation coverage	Product-specific and potentially substantial
Method-of-use coverage	Strong for diabetes; broader indications depend on later patents
Manufacturing protection	Potentially significant but process-dependent
Invalidity exposure	Typical risks include written description, enablement, obviousness, and claim-construction disputes
Generic design-around potential	Limited for the exact semaglutide molecule; greater for processes and formulations
Post-2026 entry risk	High if later patents are invalidated, licensed, or avoided
Post-2031 entry risk	Lower for core semaglutide products, subject to later patent filings and regulatory exclusivity

The strongest claim for Novo Nordisk is the direct species claim covering Aib8,22, Arg34-GLP-1(7-37), when combined with the claimed acylated structure. Generic applicants are more likely to contest later formulation, oral-delivery, manufacturing, or method-of-use patents than to substitute a chemically different molecule while retaining the semaglutide label.

What litigation and settlement issues affect semaglutide?

Semaglutide litigation is likely to involve several distinct legal questions:

• Whether the accused product contains the claimed semaglutide structure.
• Whether the linker and acidic group fall within the asserted claim.
• Whether an alternative manufacturing route infringes a process patent.
• Whether an ANDA label induces infringement of a method-of-use claim.
• Whether an oral product infringes formulation or absorption-enhancer patents.
• Whether claims are enabled across the full Markush genus.
• Whether the patent’s priority chain supports the asserted claims.
• Whether patent-term adjustment or terminal disclaimers limit enforceability.

Publicly reported Paragraph IV cases do not, by themselves, establish a final market-entry date. Settlement terms may include delayed launch, authorized supply, geographic limitations, or licenses to particular products. Many settlement agreements are confidential or only partially disclosed through court filings and antitrust reports.

How does semaglutide compare with competing GLP-1 drugs?

Drug	Company	Modality	Principal patent risk
Semaglutide	Novo Nordisk	Acylated GLP-1 analog	Core, oral formulation, dosing, manufacturing, and device patents
Liraglutide	Novo Nordisk	Acylated GLP-1 analog	Core patents have largely expired; generic competition has emerged
Dulaglutide	Eli Lilly	Fusion-protein GLP-1 agonist	Biologic and formulation patent estate
Tirzepatide	Eli Lilly	GIP/GLP-1 peptide	Core compound, formulation, device, and use patents
Exenatide	Amylin/AstraZeneca	GLP-1 peptide	Earlier patent estate and established generic or alternative-product risk
Retatrutide	Eli Lilly	Investigational multi-agonist peptide	Patent protection remains development-stage and future-facing

Semaglutide has a more complex entry profile than liraglutide because its commercial value is supported by multiple products, oral delivery, high-dose obesity use, and a later-generation patent estate.

What is the revenue exposure from U.S. 8,536,122?

The patent is linked to three major U.S. franchises:

• Ozempic for type 2 diabetes.
• Rybelsus for oral treatment of type 2 diabetes.
• Wegovy for chronic weight management.

Novo Nordisk reported 2023 total sales of DKK 232.3 billion, with Ozempic, Rybelsus, and Wegovy among the company’s major growth products.[4] In 2024, the company reported continued high demand for GLP-1 products, although supply constraints, pricing, reimbursement, and competition affected net sales and market access.[5]

U.S. 8,536,122 is not the sole revenue-protection asset. Its expiration creates a material risk to the active-ingredient barrier, but the financial impact depends on the remaining term and enforceability of later Orange Book-listed patents.

Key Takeaways

• U.S. Patent 8,536,122 is a foundational Novo Nordisk patent for acylated GLP-1 analogs.
• Claim 9 directly identifies Aib8,22, Arg34-GLP-1(7-37), the peptide backbone of semaglutide.
• Claims 10 through 12 address spacer and acidic lipid-containing substituents.
• Claims 13 and 14 cover pharmaceutical compositions.
• Claims 15 and 16 cover treatment of hyperglycemia and type 2 diabetes.
• The commonly reported U.S. expiration date is March 20, 2026.
• Later semaglutide patents, including patents associated with protection through approximately 2031, may continue to block or complicate generic entry.
• Oral semaglutide has separate formulation and absorption-enhancer risks.
• Generic development faces peptide manufacturing, analytical, device, and regulatory barriers.
• Paragraph IV litigation can accelerate entry only if the challenged patents are defeated, narrowed, licensed, or otherwise avoided.

FAQs

Is semaglutide specifically named in U.S. Patent 8,536,122?

The supplied claims do not use the INN “semaglutide,” but claim 9 identifies the relevant Aib8,22, Arg34-GLP-1 analog structure, and the compound falls within the claimed acylated GLP-1 architecture.

Can a generic semaglutide launch when U.S. 8,536,122 expires?

Not necessarily. A generic applicant must also address later patents covering semaglutide formulations, oral delivery, manufacturing processes, dosing regimens, devices, and approved uses.

Does U.S. 8,536,122 cover Ozempic and Wegovy equally?

The core compound claims are route- and brand-neutral, but product-specific Orange Book listings, indication claims, formulation claims, and device patents may differ between Ozempic and Wegovy.

Does the patent cover semaglutide manufacturing methods?

The supplied claims primarily cover compounds, compositions, and treatment methods. Manufacturing protection would generally arise from separate process claims or related patent families.

Is a semaglutide biosimilar required to prove interchangeability?

The regulatory pathway depends on FDA classification and the applicant’s chosen application route. An applicant may pursue an ANDA, 505(b)(2) application, or biologics pathway depending on the product and FDA treatment of the active ingredient. Interchangeability is a separate designation from approval.

References

1. United States Patent and Trademark Office. (2013). U.S. Patent No. 8,536,122, GLP-1 analogues.
2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
3. United States Patent and Trademark Office. (2016). U.S. Patent No. 9,266,951, GLP-1 analogues.
4. Novo Nordisk A/S. (2024). Annual report 2023.
5. Novo Nordisk A/S. (2025). Annual report 2024.

Drugs Protected by US Patent 8,536,122

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novo	OZEMPIC	semaglutide	SOLUTION;SUBCUTANEOUS	209637-001	Dec 5, 2017		DISCN	Yes	No	8,536,122		Y	Y		OZEMPIC IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS
Novo	OZEMPIC	semaglutide	SOLUTION;SUBCUTANEOUS	209637-004	Oct 6, 2022		RX	Yes	Yes	8,536,122		Y	Y		AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS
Novo	OZEMPIC	semaglutide	SOLUTION;SUBCUTANEOUS	209637-002	Apr 9, 2019		RX	Yes	Yes	8,536,122		Y	Y		OZEMPIC IS INDICATED AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS
Novo	OZEMPIC	semaglutide	SOLUTION;SUBCUTANEOUS	209637-003	Mar 28, 2022		RX	Yes	Yes	8,536,122		Y	Y		AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS

Foreign Priority and PCT Information for Patent: 8,536,122

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	05102171	Mar 18, 2005

International Family Members for US Patent 8,536,122

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1863839		300936	Netherlands
European Patent Office	1863839		2018C/016	Belgium
European Patent Office	1863839		CR 2018 00019	Denmark
European Patent Office	1863839		122018000075	Germany