REGORAFENIB - Generic Drug Details

What are the generic sources for regorafenib and what is the scope of patent protection?

Regorafenib is the generic ingredient in two branded drugs marketed by Actavis Labs Fl and Bayer Hlthcare, and is included in two NDAs. There are four patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Regorafenib has one hundred and sixty-eight patent family members in forty-nine countries.

There are two drug master file entries for regorafenib. One supplier is listed for this compound.

Summary for REGORAFENIB

International Patents:	168
US Patents:	4
Tradenames:	2
Applicants:	2
NDAs:	2
Drug Master File Entries:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	98
Clinical Trials:	312
Patent Applications:	6,980
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for REGORAFENIB
What excipients (inactive ingredients) are in REGORAFENIB?	REGORAFENIB excipients list
DailyMed Link:	REGORAFENIB at DailyMed

Recent Clinical Trials for REGORAFENIB

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

Sponsor	Phase
M.D. Anderson Cancer Center	PHASE1
Zhejiang Hisun Pharmaceutical Co. Ltd.	PHASE2
M.D. Anderson Cancer Center	PHASE2

See all REGORAFENIB clinical trials

Pharmacology for REGORAFENIB

Drug Class	Kinase Inhibitor
Mechanism of Action	Breast Cancer Resistance Protein Inhibitors Cytochrome P450 2C9 Inhibitors Kinase Inhibitors UGT1A1 Inhibitors UGT1A9 Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for REGORAFENIB

L01EX	Other protein kinase inhibitors
L01E	PROTEIN KINASE INHIBITORS
L01	ANTINEOPLASTIC AGENTS
L	Antineoplastic and immunomodulating agents

Paragraph IV (Patent) Challenges for REGORAFENIB

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
STIVARGA	Tablets	regorafenib	40 mg	203085	2	2016-09-27

US Patents and Regulatory Information for REGORAFENIB

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Bayer Hlthcare	STIVARGA	regorafenib	TABLET;ORAL	203085-001	Sep 27, 2012		RX	Yes	Yes
Bayer Hlthcare	STIVARGA	regorafenib	TABLET;ORAL	203085-001	Sep 27, 2012		RX	Yes	Yes			Y	Y
Actavis Labs Fl	REGORAFENIB	regorafenib	TABLET;ORAL	209728-001	Jan 13, 2025		DISCN	No	No
Bayer Hlthcare	STIVARGA	regorafenib	TABLET;ORAL	203085-001	Sep 27, 2012		RX	Yes	Yes			Y
Bayer Hlthcare	STIVARGA	regorafenib	TABLET;ORAL	203085-001	Sep 27, 2012		RX	Yes	Yes				Y

Expired US Patents for REGORAFENIB

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Bayer Hlthcare	STIVARGA	regorafenib	TABLET;ORAL	203085-001	Sep 27, 2012

EU/EMA Drug Approvals for REGORAFENIB

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Bayer Pharma AG	Stivarga	regorafenib	EMEA/H/C/002573Stivarga is indicated as monotherapy for the treatment of adult patients with:metastatic colorectal cancer (CRC) who have been previously treated with, or are not considered candidates for, available therapies - these include fluoropyrimidine-based chemotherapy, an anti-VEGF therapy and an anti-EGFR therapy;unresectable or metastatic gastrointestinal stromal tumors (GIST) who progressed on or are intolerant to prior treatment with imatinib and sunitinib;hepatocellular carcinoma (HCC) who have been previously treated with sorafenib.	Authorised	no	no	no	2013-08-26

International Patents for REGORAFENIB

Country	Patent Number	Title	Estimated Expiration
Peru	20130181	PROCEDIMIENTO PARA LA PREPARACION DE 4-{4-[({[4-CLORO-3-(TRIFLUOROMETIL)FENIL]AMINO}CARBONIL)AMINO]-3-FLUOROFENOXI}-N-METILPIRIDINA-2-CARBOXAMIDA, SUS SALES Y SU MONOHIDRATO
Argentina	062927	4- [4-( [ [ 4- CLORO-3-( TRIFLUOROMETIL) FENIL) CARBAMOIL] AMINO] -3- FLUOROFENOXI) -N- METILPIRIDIN-2- CARBOXAMIDA MONOHIDRATADA
Mexico	2012011734
Poland	2558448
European Patent Office	2558448
World Intellectual Property Organization (WIPO)	2005009961
Colombia	6630136

Supplementary Protection Certificates for REGORAFENIB

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1663978	122013000086	Germany		PRODUCT NAME: REGORAFENIB ODER EIN SALZ DAVON; REGISTRATION NO/DATE: EU/1/13/858 20130826
1663978	475	Finland
1663978	92300	Luxembourg		PRODUCT NAME: REGORAFENIB ET SES SELS PHARMACEUTIQUEMENT ACCEPTABLES(STIVARGA)
1663978	C20130034 00099	Estonia		PRODUCT NAME: REGORAFENIIB;REG NO/DATE: K(2013)5622 (LOPLIK) 26.08.2013
2097381	C02097381/01	Switzerland		PRODUCT NAME: REGORAFENIB; REGISTRATION NO/DATE: SWISSMEDIC-ZULASSUNG 62808 15.03.2018
1663978	2013/050	Ireland		PRODUCT NAME: REGORAFENIB AND ITS SALTS; REGISTRATION NO/DATE: EU/1/13/858 20130826
1663978	C01663978/01	Switzerland		FORMER OWNER: BAYER HEALTHCARE LLC, US

REGORAFENIB Market Analysis and Financial Projection

Last updated: February 13, 2026

What Is the Current Market Landscape for Regorafenib?

Regorafenib (brand names: Stivarga, Bayer) is an oral multikinase inhibitor approved for metastatic colorectal cancer (mCRC), gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC). The drug's market position depends on indications, competitors, and regional regulatory approvals.

In 2022, the global regorafenib market was valued approximately USD 720 million. It is projected to grow at a compound annual growth rate (CAGR) of 6.2% from 2023 to 2030. Growth is driven by increasing incidence of mCRC and HCC, expanded labeling, and post-marketing approvals in emerging regions.

Major markets include North America, Europe, and Asia-Pacific. North America accounts for nearly 45% of sales, owing to high adoption in oncology protocols and robust healthcare infrastructure. Europe follows, with approximately 25% of the market, while Asia-Pacific contributes an estimated 20%, with growth influenced by expanding healthcare access and regulatory approvals in China, Japan, and India.

How Do Regorafenib's Indications Shape Its Market Dynamics?

Metastatic Colorectal Cancer (mCRC):
Approved since 2012, regorafenib targets patients who progressed after standard chemotherapy. Its inclusion in treatment guidelines (e.g., NCCN, ESMO) sustains demand.

Gastrointestinal Stromal Tumors (GIST):
Since 2013, indicated for unresectable or metastatic GIST after prior lines. It competes with imatinib, sunitinib, and newer agents. Its efficacy broadens its use but limits market size relative to colorectal indications.

Hepatocellular Carcinoma (HCC):
Since 2017, approved for unresectable HCC. The rise of targeted therapies like sorafenib and lenvatinib exerts competitive pressure.

The expansion into multiple indications diversifies revenue streams but introduces complexities with distinct pricing and reimbursement pathways.

What Are the Key Competitive Forces?

Major competitors include:

• Lenvatinib (Eisai): Approved for HCC, rival to regorafenib in liver cancer.
• Cabozantinib (Bristol-Myers Squibb): Approved for HCC, GIST, and other tumors.
• Sunitinib (Pfizer): Used for GIST, competes in similar GIST indications.
• Avapritinib and ripretinib: Emerging agents for GIST, with novel mechanisms.

Patent protections for regorafenib are expected to expire by 2027 in major markets, opening opportunities for generics and biosimilars, which will impact pricing and market share.

What Is the Financial Trajectory?

Revenue Trends:
Regorafenib's revenue peaked in 2019 at approximately USD 750 million. Since then, growth has slowed due to market saturation and increased competitive pressure. In 2022, sales declined marginally to USD 720 million, with projections indicating stabilization around USD 700–750 million in the near term.

Pricing:
Average wholesale prices vary by region. In the U.S., the monthly cost is approximately USD 13,000–15,000. European prices range between EUR 8,000–12,000, reflecting reimbursement negotiations.

Market Penetration Factors:
Use is limited by side effect profiles—hypertension, hand-foot skin reactions, diarrhea—which influence patient adherence. High treatment costs restrict access in lower-income regions.

R&D and Expansion:
Bayer continues to explore combinatorial therapies incorporating regorafenib, aiming for label extensions. Positron emission tomography (PET) imaging has been investigated as a biomarker to optimize patient selection, potentially improving outcomes and economic viability.

Regulatory Outlook:
Filing for approval or expansion in China and other emerging markets is ongoing. As patent cliffs approach, Bayer's pipeline efforts and strategies for biosimilars will influence future revenues.

How Do External Factors Affect Regorafenib's Market and Financials?

• Regulatory Changes: Stringent pricing policies in Europe and the U.S. could limit price growth. Positive reimbursement decisions enhance market access.
• Market Entry of Generics: Anticipated post-2027, could reduce prices by up to 80%, impacting Bayer's revenues.
• Healthcare Trends: Increased adoption of immunotherapies and combination regimens may diminish monotherapy use, shrinking market share if regorafenib doesn't integrate into combination protocols.
• Regional Healthcare Investment: Growing healthcare budgets in Asian markets expand access, supporting revenue growth there.

What Are the Key Strategic Considerations?

• Bayer’s efforts in clinical trials for combination therapies could extend label indications.
• Negotiating pricing and reimbursement in emerging markets is critical for growth.
• Investment in biosimilar development and patent litigation strategies will shape future profitability.
• Collaborations or licensing deals with biotech firms could position regorafenib within new treatment paradigms.

Key Takeaways

• Regorafenib's global market was valued at USD 720 million in 2022, with prospects for modest growth.
• Its revenue is influenced by competition, patent expirations, and regional reimbursement policies.
• Multiple indications diversify revenue but complicate clinical and commercial strategies.
• Pricing varies significantly by region, with upcoming generics threatening market share.
• Emerging combination therapies and biomarker-driven patient selection could impact future sales trajectories.

FAQs

Q1: When will generic versions of regorafenib likely enter the market?
A: Patent expiry in major markets is expected around 2027, after which generics are likely.

Q2: What are the main side effects impacting regorafenib's market adoption?
A: Hypertension, hand-foot skin reactions, diarrhea, fatigue, and liver enzyme elevations.

Q3: How does regorafenib compare with new targeted therapies?
A: It offers benefits in late-line settings; however, newer agents, especially immunotherapies, may supplant it in some indications.

Q4: What is the outlook for regorafenib's use in hepatocellular carcinoma?
A: Its approval in HCC supports growth, but competition from other targeted therapies and immunotherapies remains strong.

Q5: How might regional healthcare policies affect regorafenib’s future sales?
A: Stronger reimbursement practices boost access in developed regions; restrictive policies may limit growth.

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Sources:

1. MarketWatch. "Regorafenib Market Size & Share, Industry Analysis," 2023.
2. EvaluatePharma. "Global Oncology Market Data," 2022.
3. FDA & EMA Label Approvals (2012–2023).
4. Bayer Annual Reports, 2020–2022.
5. IQVIA. "Pharmaceutical Sales Data," 2022.