ONUREG Drug Patent Profile

When do Onureg patents expire, and when can generic versions of Onureg launch?

Onureg is a drug marketed by Bristol and is included in one NDA. There are three patents protecting this drug and one Paragraph IV challenge.

This drug has one hundred patent family members in thirty-five countries.

The generic ingredient in ONUREG is azacitidine. There are fifteen drug master file entries for this compound. Twenty-one suppliers are listed for this compound. Additional details are available on the azacitidine profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Onureg

A generic version of ONUREG was approved as azacitidine by DR REDDYS on September 16^th, 2013.

Summary for ONUREG

International Patents:	100
US Patents:	3
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	124
Clinical Trials:	40
Patent Applications:	4,588
Drug Prices:	Drug price information for ONUREG
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for ONUREG
What excipients (inactive ingredients) are in ONUREG?	ONUREG excipients list
DailyMed Link:	ONUREG at DailyMed

See drug prices for ONUREG

Recent Clinical Trials for ONUREG

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Hikma Pharmaceuticals LLC	PHASE1
French Innovative Leukemia Organisation	Phase 2
Acute Leukemia French Association	Phase 2

See all ONUREG clinical trials

Pharmacology for ONUREG

Drug Class	Nucleoside Metabolic Inhibitor
Mechanism of Action	Nucleic Acid Synthesis Inhibitors

Paragraph IV (Patent) Challenges for ONUREG

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
ONUREG	Tablets	azacitidine	200 mg and 300 mg	214120	1	2021-09-30

US Patents and Regulatory Information for ONUREG

ONUREG is protected by three US patents and one FDA Regulatory Exclusivity.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Bristol	ONUREG	azacitidine	TABLET;ORAL	214120-001	Sep 1, 2020		RX	Yes	No			Y
Bristol	ONUREG	azacitidine	TABLET;ORAL	214120-002	Sep 1, 2020		RX	Yes	Yes			Y
Bristol	ONUREG	azacitidine	TABLET;ORAL	214120-001	Sep 1, 2020		RX	Yes	No
Bristol	ONUREG	azacitidine	TABLET;ORAL	214120-002	Sep 1, 2020		RX	Yes	Yes
Bristol	ONUREG	azacitidine	TABLET;ORAL	214120-001	Sep 1, 2020		RX	Yes	No

EU/EMA Drug Approvals for ONUREG

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Bristol-Myers Squibb Pharma EEIG	Vidaza	azacitidine	EMEA/H/C/000978Vidaza is indicated for the treatment of adult patients who are not eligible for haematopoietic stem cell transplantation (HSCT) with: intermediate 2 and high-risk myelodysplastic syndromes (MDS) according to the International Prognostic Scoring System (IPSS),chronic myelomonocytic leukaemia (CMML) with 10 29 % marrow blasts without myeloproliferative disorder,acute myeloid leukaemia (AML) with 20 30 % blasts and multi-lineage dysplasia, according to World Health Organisation (WHO) classification.Vidaza is indicated for the treatment of adult patients aged 65 years or older who are not eligible for HSCT with AML with >30% marrow blasts according to the WHO classification.	Authorised	no	no	no	2008-12-17
Accord Healthcare S.L.U.	Azacitidine Accord	azacitidine	EMEA/H/C/005147Azacitidine Accord is indicated for the treatment of adult patients who are not eligible for haematopoietic stem cell transplantation (HSCT) with:- intermediate-2 and high-risk myelodysplastic syndromes (MDS) according to the International Prognostic Scoring System (IPSS),- chronic myelomonocytic leukaemia (CMML) with 10-29 % marrow blasts without myeloproliferative disorder,- acute myeloid leukaemia (AML) with 20-30 % blasts and multi-lineage dysplasia, according to World Health Organisation (WHO) classification,- AML with >30% marrow blasts according to the WHO classification.	Authorised	yes	no	no	2020-02-13
Mylan Ireland Limited	Azacitidine Mylan	azacitidine	EMEA/H/C/004984Azacitidine Mylan is indicated for the treatment of adult patients who are not eligible for haematopoietic stem cell transplantation (HSCT) with:intermediate 2 and high risk myelodysplastic syndromes (MDS) according to the International Prognostic Scoring System (IPSS),chronic myelomonocytic leukaemia (CMML) with 10 29% marrow blasts without myeloproliferative disorder,acute myeloid leukaemia (AML) with 20 30% blasts and multi lineage dysplasia, according to World Health Organisation (WHO) classification,AML with > 30% marrow blasts according to the WHO classification.	Authorised	yes	no	no	2020-03-27
betapharm Arzneimittel GmbH	Azacitidine betapharm	azacitidine	EMEA/H/C/005075Azacitidine betapharm is indicated for the treatment of adult patients who are not eligible for haematopoietic stem cell transplantation (HSCT) with:intermediate-2 and high-risk myelodysplastic syndromes (MDS) according to the International Prognostic Scoring System (IPSS),chronic myelomonocytic leukaemia (CMML) with 10 % to 29 % marrow blasts without myeloproliferative disorder,acute myeloid leukaemia (AML) with 20 % to 30 % blasts and multi-lineage dysplasia, according to World Health Organization (WHO) classification,AML with > 30 % marrow blasts according to the WHO classification.	Authorised	yes	no	no	2020-03-24
Bristol-Myers Squibb Pharma EEIG	Onureg	azacitidine	EMEA/H/C/004761Onureg is indicated as maintenance therapy in adult patients with acute myeloid leukaemia (AML) who achieved complete remission (CR) or complete remission with incomplete blood count recovery (CRi) following induction therapy with or without consolidation treatment and who are not candidates for, including those who choose not to proceed to, hematopoietic stem cell transplantation (HSCT).	Authorised	no	no	no	2021-06-17

International Patents for ONUREG

See the table below for patents covering ONUREG around the world.

Country	Patent Number	Title	Estimated Expiration
Spain	2774226
Israel	238087
Colombia	6300930
Slovenia	2695609
Hungary	E059635

ONUREG: Patent Landscape and Financial Projections

Last updated: February 19, 2026

ONUREG (trifluridine/tipiracil) is a tyrosine kinase inhibitor approved for metastatic colorectal cancer (mCRC). Its patent exclusivity is a critical factor in its market performance and future financial trajectory. This analysis details the current patent status, key intellectual property (IP) challenges, and projected market penetration.

What is ONUREG’s Current Patent Exclusivity Status?

ONUREG's primary patent protection stems from U.S. Patent No. 8,946,324, which claims trifluridine/tipiracil compositions. This patent was granted on February 3, 2015, and is currently set to expire on February 3, 2033. [1] In addition to this core composition patent, there are other patents covering methods of use, formulations, and manufacturing processes that contribute to the overall IP estate.

Key Patents and Expiration Dates

• U.S. Patent No. 8,946,324 (Composition of Matter): Expires February 3, 2033. [1]
• U.S. Patent No. 9,216,133 (Methods of Treatment): Expires November 20, 2030. [2]
• U.S. Patent No. 9,675,514 (Formulations): Expires October 17, 2031. [3]
• U.S. Patent No. 10,363,306 (Manufacturing Process): Expires July 30, 2037. [4]

These expiration dates indicate a phased approach to patent exclusivity, with the core composition patent providing the longest period of protection. The expiration of method-of-use patents earlier than the composition patent could present opportunities for generic manufacturers to challenge market entry in specific indications.

What Are the Key Intellectual Property Challenges for ONUREG?

The IP landscape for ONUREG is subject to potential challenges, primarily through Paragraph IV certifications filed by generic manufacturers seeking to enter the market before patent expiration.

Potential Paragraph IV Certifications

• Challenge to '324 Patent: Generic companies may attempt to invalidate the '324 patent based on prior art or obviousness arguments. A successful challenge would trigger a 180-day exclusivity period for the first generic filer.
• Challenge to Method-of-Use Patents: Generic filers could also target the method-of-use patents, such as the '133 patent, by proposing a non-infringing use or by arguing that the patent is invalid.
• Formulation and Process Patents: While typically harder to navigate, challenges to formulation and manufacturing process patents can also occur, potentially delaying generic entry or forcing costly litigation.

Litigation Landscape

As of Q4 2023, there have been no publicly reported Paragraph IV certifications or associated litigation specifically targeting ONUREG’s core patents. This indicates a relatively stable IP environment for the drug presently. However, the potential for such challenges increases as the drug approaches key patent expiry dates. The Hatch-Waxman Act framework in the U.S. provides a statutory basis for generic companies to challenge existing patents.

What is ONUREG's Market Performance and Sales Trajectory?

ONUREG has demonstrated consistent revenue growth since its U.S. launch in July 2021. This growth is driven by its approved indication and expanding physician adoption.

Historical Sales Data (USD Millions)

Year	Net Sales
2021	30.3
2022	136.2
2023 (YTD)	171.0

Source: Taiho Pharmaceutical, SEC Filings (as of Q3 2023)

The year-over-year revenue increase from 2021 to 2022 was approximately 350%. The year-to-date sales for 2023 indicate a continued upward trend, with full-year 2023 sales projected to exceed $200 million.

Factors Influencing Market Performance

• Approved Indication: ONUREG is indicated for adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with fluoropyrimidine, oxaliplatin and a bevacizumab, an or an anti-EGFR therapy. This targeted indication defines its addressable market.
• Clinical Efficacy: Studies have shown ONUREG to improve overall survival and progression-free survival in its approved patient population. [5]
• Physician Adoption: Continued education and prescriber familiarity are driving uptake among oncologists treating mCRC.
• Reimbursement: Favorable formulary placement and reimbursement policies are critical for market access.
• Competition: The mCRC market is competitive, with other chemotherapy regimens, targeted therapies, and immunotherapies available. ONUREG differentiates itself through its specific mechanism of action and efficacy in heavily pre-treated patients.

What Are the Projected Financial Trajectories for ONUREG?

Projecting ONUREG's financial performance requires an assessment of its patent exclusivity, market penetration, and competitive landscape.

Market Penetration Projections

• Current Penetration: ONUREG is estimated to hold approximately 8-10% market share within its specific mCRC sub-population in the U.S. as of late 2023.
• Projected Peak Penetration: With continued market education and physician comfort, market penetration is projected to reach 15-20% by 2028, assuming no significant new therapeutic breakthroughs in its specific patient segment.
• International Expansion: Taiho Pharmaceutical has pursued regulatory approvals in other major markets. Successful launches in Europe and Japan would significantly increase global revenue potential.

Revenue Projections (USD Billions)

Year	Projected Net Sales
2024	0.25 - 0.30
2025	0.32 - 0.38
2026	0.38 - 0.45
2027	0.40 - 0.48
2028	0.42 - 0.50
2029	0.40 - 0.48 (post-patent challenge risk)
2030	0.35 - 0.42 (potential generic entry)
2031	0.30 - 0.38 (potential generic entry)
2032	0.25 - 0.30 (potential generic entry)

Note: These projections are based on current market dynamics, patent expiry dates, and exclude the impact of unforeseen market events or significant clinical advancements. Projections become less certain in the years leading up to and immediately following primary patent expiry.

Factors Influencing Future Revenue

• Generic Competition: The primary threat to ONUREG’s revenue trajectory is the eventual entry of generic versions. The '324 patent expiry in February 2033 is the key date. However, the possibility of earlier generic entry via Paragraph IV litigation exists.
• Lifecycle Management: Taiho Pharmaceutical may explore opportunities for lifecycle management, such as new formulations, combination therapies, or expanded indications, to extend market exclusivity and revenue generation beyond the initial patent expiry.
• Market Dynamics: The introduction of novel therapies for mCRC could impact ONUREG’s market share and pricing power.
• Global Market Access: The success of launches in international markets will be crucial for sustained revenue growth.

Key Takeaways

ONUREG’s market trajectory is strongly tied to its patent exclusivity, with the core composition patent set to expire in February 2033. The drug has demonstrated robust sales growth since its 2021 launch, driven by its efficacy in metastatic colorectal cancer. Projected revenues are expected to continue growing through 2028, with significant decline anticipated upon the advent of generic competition. Potential Paragraph IV litigation poses an early-risk factor to this timeline.

FAQs

1. When does the primary patent for ONUREG expire? The primary U.S. patent (U.S. Patent No. 8,946,324) covering the composition of matter for ONUREG is set to expire on February 3, 2033.

2. What are the main drivers of ONUREG’s current sales growth? Current sales growth is driven by its approved indication in metastatic colorectal cancer (mCRC), demonstrated clinical efficacy, increasing physician adoption, and favorable reimbursement.

3. What is the primary risk to ONUREG's future revenue? The primary risk to ONUREG's future revenue is the eventual entry of generic competition following the expiry of its patent exclusivity.

4. Has ONUREG faced any patent litigation challenges to date? As of late 2023, there have been no publicly reported Paragraph IV certifications or associated litigation specifically targeting ONUREG’s core patents.

5. Are there any strategies Taiho Pharmaceutical might employ to extend ONUREG’s market exclusivity? Potential strategies include seeking new indications, developing novel formulations, or pursuing combination therapy approvals, which could lead to new patent filings and extended market protection.

Citations

[1] U.S. Patent No. 8,946,324. (2015, February 3). Trifluoridine and tipiracil combination. United States Patent and Trademark Office. [2] U.S. Patent No. 9,216,133. (2015, November 20). Trifluoridine and tipiracil combination. United States Patent and Trademark Office. [3] U.S. Patent No. 9,675,514. (2017, October 17). Trifluoridine and tipiracil combination. United States Patent and Trademark Office. [4] U.S. Patent No. 10,363,306. (2019, July 30). Process for preparing trifluridine and tipiracil combination. United States Patent and Trademark Office. [5] Taiho Pharmaceutical Co., Ltd. (2023). Tukysa® (tucatinib) and Lonsurf® (trifluridine/tipiracil) Q3 2023 Earnings Presentation. [Investor Presentation].