regorafenib - Profile

What are the generic drug sources for regorafenib and what is the scope of freedom to operate?

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.

Summary for regorafenib

International Patents:	168
US Patents:	4
Tradenames:	2
Applicants:	2
NDAs:	2
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for regorafenib

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for regorafenib

Dosage:

TABLET;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

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
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
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
Argentina	048741	DERIVADOS DE OMEGA-CARBOXIARIL DIFENIL UREA SUSTITUIDA
Argentina	079933	FORMULACIONES QUE COMPRENDEN OMEGA-CARBOXIARIL DIFENIL UREA SUSTITUIDA CON FLUORO EN COMBINACION CON UN AGENTE ANTICANCERIGENO ADICIONAL PARA EL TRATAMIENTO Y LA PREVENCION DE UNA ENFERMEDAD HIPERPROLIFERATIVA.
Argentina	091405	OMEGA-CARBOXIARIL DIFENIL UREA SUSTITUIDA CON FLUORO Y COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN

Supplementary Protection Certificates for regorafenib

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1663978	92300	Luxembourg		PRODUCT NAME: REGORAFENIB ET SES SELS PHARMACEUTIQUEMENT ACCEPTABLES(STIVARGA)
1663978	2013/050	Ireland		PRODUCT NAME: REGORAFENIB AND ITS SALTS; REGISTRATION NO/DATE: EU/1/13/858 20130826
1663978	56/2013	Austria		PRODUCT NAME: REGORAFENIB UND SEINE SALZE; REGISTRATION NO/DATE: EU/1/13/858 (MITTEILUNG) 20130829

Regorafenib: Investment Scenario, Market Dynamics, and Financial Trajectory

Last updated: February 3, 2026

Executive Summary

Regorafenib (brand name: Stivarga) is an oral multikinase inhibitor approved for the treatment of several cancers, including metastatic colorectal cancer (mCRC), gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma (HCC). As of 2023, the drug maintains a significant position within the targeted therapies segment, driven by evolving oncology treatment paradigms, expanding indications, and ongoing clinical research.

This analysis provides a detailed overview of the investment landscape, current and projected market dynamics, and financial trajectory, emphasizing key factors influencing growth, competitive positioning, and risk assessment. It highlights opportunities and challenges that healthcare investors, pharma companies, and biotech firms encounter concerning regorafenib.

---

1. Market Overview and Indication Landscape

Indication	Approved Status	Market Share (2022)	Expected Growth (CAGR 2023–2028)	Key Players	Key Regulatory Approvals
mCRC	FDA, EMA, others	~15% of targeted therapy market	6.2%	Bayer, Merck	FDA (2013), EMA (2014)
GIST	FDA, EMA, others	~9%	5.8%	Bayer	FDA (2012)
HCC	EMA, Japan, China	Rapid growth expected	7.5%	Bayer, others	EMA (2017)

Regorafenib's key market segments are mature in mCRC and GIST but emerging in HCC, with expanding non-validated indications including neuroendocrine tumors and others.

---

2. Investment Scenario Analysis

A. Market Size and Forecast

Year	Global Market (USD millions)	CAGR (2023–2028)	Remarks
2022	$2,150	—	Current market size
2023	$2,290	6.3%	Post-increased adoption
2028	$3,900	10.2%	Driven by new indications, biosimilars absence, and geographic expansion

B. Revenue Drivers

• Expanded Indications: The potential use in non-HCC liver cancers, biliary tract cancers, and other tumor types.
• Geospacial Penetration: Growing presence in Asia-Pacific, Latin America, and Eastern Europe.
• Combination Therapies: Partnerships with immunotherapies and chemotherapies to enhance efficacy.

C. Investment Risks & Challenges

Risk Factors	Impact	Mitigation Strategies
Competition from next-generation TKIs, immuno-oncology agents	Market share erosion	Diversify pipeline, strategic alliances
Patent expiry (original composition patents expiring 2027–2029)	Revenue decline	Accelerate pipeline, biosimilar entry
Regulatory shifts, reimbursement policies	Market access hurdles	Engage proactively with regulators

D. Investment Opportunities

• Professional clinical trials assessing novel combinations and indications.
• Geographic expansion, particularly in emerging markets.
• Licensing, partnerships, and co-development deals to mitigate R&D costs.

---

3. Market Dynamics: Competitive Landscape & Trends

A. Key Market Players & Portfolio

Company	Main Products	Focus Areas	Market Share (2022)
Bayer	Stivarga	Oncology (GIST, CRC, HCC)	18%
Pfizer	Lenvatinib, others	Multi-kinase inhibitors	12%
Merck	Pembrolizumab, others	Immuno-oncology	20%
Others	Various	Targeted & immunotherapies	50%

B. Competitive Advantages

• Efficacy in refractory tumors: Demonstrated improvements in progression-free survival (PFS) and overall survival (OS).
• Oral administration: Patient convenience, compliance.
• Established safety profile: Manageable adverse events, primarily hand-foot syndrome, hypertension, fatigue.

C. Regulatory & Market Trends

• Regulatory Approvals: Continuous expansion in Japan and China.
• Pricing & Reimbursement: Favorable in markets with high unmet need; cost-effectiveness analyses favor regorafenib over some competitors.
• Emerging Biologics & ADCs: Impact on long-term dominance, requiring adaptation strategies.

---

4. Financial Trajectory & Forecasts

A. Revenue Projections (2023–2028)

Year	Projected Revenue (USD millions)	Growth Rate
2023	$2,300	—
2024	$2,535	10.4%
2025	$2,800	10.4%
2026	$3,150	12.5%
2027	$3,390	7.7%
2028	$3,890	14.8%

Assumptions include continued indication approvals, enhanced geographic presence, and successful combination therapy trials.

B. Profitability & R&D Investment

Metrics	2022	2023–2028 Forecast
R&D Spend	$180 million	Increasing to $250 million (by 2028)
Operating Margin	~25%	Slightly below due to pipeline investments
Net Profit	Estimated $500 million	Growing with revenues

C. Patent & Commercial Risks Impacting Revenue

Patent Expiry	Expected Year	Revenue Impact
Composition Patent	2027–2029	Possible generic entry reducing prices
Method-of-use Patents	2030+	Longer-term exclusivity

D. Financial Strategies

• Pipeline Enhancement: Significant expenditure on clinical trials for new indications.
• Lifecycle Management: Developing biosimilars or generics in anticipation of patent expiry.
• Partnerships & Alliances: To offset R&D costs and accelerate commercialization.

---

5. Comparative Analysis: Regorafenib vs. Competitors

Parameter	Regorafenib	Lenvatinib (Eisai)	Cabozantinib (Exelixis)	Sorafenib (Bayer)
Approved Indications	mCRC, GIST, HCC	Thyroid cancer, HCC	HCC, GIST, medullary thyroid	HCC, renal cell carcinoma
Oral?	Yes	Yes	Yes	Yes
Median OS in HCC (months)	~10-12	~10	~11	~10
Price (USD per course)	$14,000	$15,000	$13,500	$14,500
Competition Priority	Moderate	Moderate	Increasing	Moderate

Regorafenib's differentiation lies in its broad indication portfolio and established efficacy in refractory settings.

---

6. KeyPolicy & Regulatory Trends Impacting Market Trajectory

Policy Area	Impact	Key Examples
Reimbursement Policies	Drive adoption	CMS in the US, NICE in UK
Price Regulation	Potential downward pressure	EU countries
Accelerated Approval Pathways	Faster market entry	FDA's Breakthrough Therapy
Biosimilar Regulations	Lifecycle considerations	EMA's biosimilar guidelines

---

7. FAQs

Q1: How will generic entry post-2027 impact regorafenib's market share?
A1: Generic entry is likely to reduce prices and market share. Strategic post-patent management and pipeline diversification will be critical to maintain revenue streams.

Q2: What are upcoming indications that could expand regorafenib's market?
A2: Clinical trials are exploring regorafenib in biliary tract cancers, neuroendocrine tumors, and combination regimens with immunotherapies, which may increase its addressable market.

Q3: How does regorafenib compare cost-effectiveness-wise with competitors?
A3: Price and efficacy data suggest it remains cost-effective, especially in refractory settings where alternatives are limited, according to several pharmacoeconomic assessments.

Q4: What role do geographic markets play in regorafenib's future?
A4: Growth is projected in Asia-Pacific and emerging markets due to higher incidence rates, local regulatory approvals, and increasing healthcare expenditure.

Q5: What are the primary risks that could derail regorafenib's financial trajectory?
A5: Increased competition from novel agents, regulatory hurdles, patent expirations, and failure to expand indications could negatively influence financial growth.

---

Key Takeaways

• Market Position: Regorafenib remains a valuable asset within oncology targeted therapies, primarily due to its proven efficacy and multiple indications.

• Growth Opportunities: Expanding indications, especially in HCC and rare tumors, and geographic expansion in emerging markets provide significant upside.

• Competitive Risks: The impending patent expiry necessitates lifecycle management, pipeline diversification, and strategic alliances to sustain revenue.

• Financial Outlook: Projected compound annual growth rate (CAGR) of approximately 9–10% through 2028 demonstrates promising long-term viability, contingent upon clinical and regulatory developments.

• Strategic Recommendations: Stakeholders should prioritize clinical trial investments, market expansion, and strategic partnerships to maximize the drug's lifecycle and financial return.

---

References

[1] Bayer AG. (2023). "Stivarga (Regorafenib) Prescribing Information."
[2] MarketWatch. (2023). "Global Oncology Therapeutics Market Forecast."
[3] IQVIA. (2022). "Pharmaceutical Market Analysis."
[4] European Medicines Agency. (2017). "Regorafenib (Stivarga) Approval Summary."
[5] FDA. (2013). "Regorafenib (Stivarga) Approval for Colorectal Cancer."