AFATINIB DIMALEATE - Generic Drug Details

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

Afatinib dimaleate is the generic ingredient in one branded drug marketed by Boehringer Ingelheim and is included in one NDA. There are five patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Afatinib dimaleate has one hundred and eighty-seven patent family members in forty-six countries.

There are six drug master file entries for afatinib dimaleate. One supplier is listed for this compound.

Summary for AFATINIB DIMALEATE

International Patents:	187
US Patents:	5
Tradenames:	1
Applicants:	1
NDAs:	1
Drug Master File Entries:	6
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	48
Clinical Trials:	10
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for AFATINIB DIMALEATE
DailyMed Link:	AFATINIB DIMALEATE at DailyMed

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

Constraining patent/regulatory exclusivity:

8,545,884*PED

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.

Recent Clinical Trials for AFATINIB DIMALEATE

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

Sponsor	Phase
Petrov, Andrey	PHASE1
Shanghai Chest Hospital	Phase 4
University of Washington	Phase 1

See all AFATINIB DIMALEATE clinical trials

Pharmacology for AFATINIB DIMALEATE

Drug Class	Kinase Inhibitor
Mechanism of Action	Protein Kinase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for AFATINIB DIMALEATE

L01EB	Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
L01E	PROTEIN KINASE INHIBITORS
L01	ANTINEOPLASTIC AGENTS
L	Antineoplastic and immunomodulating agents

Paragraph IV (Patent) Challenges for AFATINIB DIMALEATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
GILOTRIF	Tablets	afatinib dimaleate	20 mg, 30 mg and 40 mg	201292	7	2017-07-12

US Patents and Regulatory Information for AFATINIB DIMALEATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-002	Jul 12, 2013		RX	Yes	No
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-003	Jul 12, 2013		RX	Yes	Yes	RE43431*PED				Y
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-002	Jul 12, 2013		RX	Yes	No	8,545,884*PED				Y
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-001	Jul 12, 2013		RX	Yes	No	RE43431*PED				Y
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-001	Jul 12, 2013		RX	Yes	No	10,004,743*PED				Y
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-002	Jul 12, 2013		RX	Yes	No

Expired US Patents for AFATINIB DIMALEATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-002	Jul 12, 2013	6,251,912
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-001	Jul 12, 2013	6,251,912
Boehringer Ingelheim	GILOTRIF	afatinib dimaleate	TABLET;ORAL	201292-003	Jul 12, 2013	6,251,912

International Patents for AFATINIB DIMALEATE

Country	Patent Number	Title	Estimated Expiration
Ecuador	SP066509	PROCEDIMIENTO PARA LA PREPARACIÓN DE COMPUESTOS DE AMINOCROTONILO
Denmark	2299971
Denmark	1678165
Spain	2588031
Japan	3827641
Ukraine	91401	ДИМАЛЕАТ 4-[(3-ХЛОР-4-ФТОРФЕНІЛ)АМІНО]-6-{[4-(N,N-ДИМЕТИЛАМІНО)-1-ОКСО-2-БУТЕН-1-ІЛ]АМІНО}-7-((S)-ТЕТРАГІДРОФУРАН-3-ІЛОКСИ)ХІНАЗОЛІНУ, СПОСІБ ЙОГО ОДЕРЖАННЯ ТА ЗАСТОСУВАННЯ[ДИМАЛЕАТ 4-[(3-ХЛОР-4-ФТОРФЕНИЛ)АМИНО]-6-{[4-(N,N-ДИМЕТИЛАМИНО)-1-ОКСО-2-БУТЕН-1-ИЛ]АМИНО}-7-((S)-ТЕТРАГИДРОФУРАН-3-ИЛОКСИ)ХИНАЗОЛИНА, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ (4-[(3-CHLORO-4-FLUOROPHENYL)AMINO]-6-{[4-(N,N-DIMETHYLAMINO)-1-OXO-2-BUTENE-1-YL]AMINO}-7-((S)-TETRAHYDROFURANE-3-YLOXY)-QUINAZOLINE MALEATE, PRODUCTION METHOD AND USES THEREOF)

Supplementary Protection Certificates for AFATINIB DIMALEATE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1345910	CR 2014 00006	Denmark		PRODUCT NAME: AFATINIB, INKLUSIVE TAUTOMERERNE, STEREOISOMERERNE OG SALTENE DERAF, EVENTUELT I FORM AF ET FYSIOLOGISK ACCEPTABELT SALT DERAF, FORTRINSVIS ET MALEATSALT DERAF OG MERE FORETRUKKET ET DIMALEATSALT DERAF; REG. NO/DATE: EU/1/13/879 20130925
1345910	CA 2014 00006	Denmark		PRODUCT NAME: AFATINIB, INKLUSIVE TAUTOMERERNE, STEREOISOMERERNE OG SALTENE DERAF, EVENTUELT I FORM AF ET FYSIOLOGISK ACCEPTABELT SALT DERAF, FORTRINSVIS ET MALEATSALT DERAF OG MERE FORETRUKKET ET DIMALEATSALT DERAF; REG. NO/DATE: EU/1/13/879 20130925
1345910	PA2014005	Lithuania		PRODUCT NAME: AFATINIBUM; REGISTRATION NO/DATE: EU/1/13/879/001-EU/1/13/879/012 20130925
1345910	SPC/GB14/015	United Kingdom		PRODUCT NAME: AFATINIB, OPTIONALLY IN THE FORM OF A PHYSIOLOGICALLY ACCEPTABLE SALT, IN PARTICULAR A SALT WITH MALEIC ACID; REGISTERED: UK EU/1/13/879/001 20130927; UK EU/1/13/879/002 20130927; UK EU/1/13/879/003 20130927; UK EU/1/13/879/004 20130927; UK EU/1/13/879/005 20130927; UK EU/1/13/879/006 20130927; UK EU/1/13/879/007 20130927; UK EU/1/13/879/008 20130927; UK EU/1/13/879/009 20130927; UK EU/1/13/879/010 20130927; UK EU/1/13/879/011 20130927; UK EU/1/13/879/012 20130927
1345910	C 2014 005	Romania		PRODUCT NAME: AFATINIB,TAUTOMERII, STEREOIZOMERII SI SARURILE ACESTUIA, SARURI FIZIOLOGIC ACCEPTABILE CU ACIZI SAU BAZE ANORGANICE SAUORGANICE, PREFERABIL O SARE MALEAT A ACESTUIA, SI MAI PREFERABIL SARE DIMALEATAACESTUIA; NATIONAL AUTHORISATION NUMBER: EU/1/13/879; DATE OF NATIONAL AUTHORISATION: 20130925; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/13/879; DATE OF FIRST AUTHORISATION IN EEA: 20130925
1345910	C01345910/01	Switzerland		PRODUCT NAME: AFATINIB; REGISTRATION NO/DATE: SWISSMEDIC 63042 17.01.2014

Market Dynamics and Financial Trajectory for AFATINIB DIMALEATE

Last updated: July 28, 2025

Introduction

Afatinib Dimaleate, marketed under the brand name Gilotrif among others, is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) approved for the treatment of non-small cell lung cancer (NSCLC) harboring specific EGFR mutations. As a second-generation irreversible inhibitor, afatinib has carved a niche within targeted cancer therapies, demonstrating significant clinical efficacy. Its market trajectory is shaped by a confluence of scientific advances, regulatory landscapes, competitive dynamics, and evolving cancer treatment protocols.

This comprehensive analysis explores the current market environment, ongoing research efforts, regulatory influences, competitive positioning, and financial outlook for afatinib dimaleate, providing stakeholders with strategic insights into its future potential.

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Market Landscape and Epidemiological Context

The global burden of non-small cell lung cancer (NSCLC) predominantly influences afatinib’s market potential. According to the World Health Organization, lung cancer accounts for approximately 1.8 million deaths annually [1]. NSCLC constitutes roughly 85% of lung cancer cases, often diagnosed at advanced stages where targeted therapies like afatinib become essential.

The prevalence of EGFR mutations in NSCLC varies geographically, with higher incidences in East Asian populations (~30-50%) compared to Western populations (~10-15%) [2]. This epidemiological pattern underpins regional demand variability, with Asian markets representing a significant share of afatinib’s usage.

Market Dynamics Influencing Afatinib

1. Clinical Adoption and Efficacy

   Afatinib’s approval in 2013 by the FDA and subsequent approvals in multiple territories cemented its position as a first-line treatment for EGFR-mutated NSCLC [3]. Clinical trials, notably the LUX-Lung series, demonstrated superior progression-free survival (PFS) compared to chemotherapy, reinforcing its clinical acceptance [4]. However, the emergence of third-generation TKIs like osimertinib has introduced competition by addressing resistance mechanisms, thereby impacting afatinib’s market share.

2. Competitive Landscape

   The therapeutic landscape for EGFR-mutated NSCLC is intensely competitive. Osimertinib (Tagrisso) notably gained prominence after demonstrating superior central nervous system penetration and efficacy against T790M resistance mutations, leading to initial approval as a second-line agent and later as a first-line therapy [5].

   Other second-generation inhibitors, such as dacomitinib, also compete in the first-line setting. The choice among these agents hinges on their efficacy profiles, safety, resistance patterns, and patient-specific factors.

3. Regulatory and Patent Considerations

   Patent expirations impact market exclusivity. Pfizer’s patent protection for afatinib was expected to expire in major markets around 2023–2025, opening pathways for generic or biosimilar competition with potential price erosion [6].

   Additionally, regulatory re-evaluations, label updates, and indications for resistance mutations influence market access. For example, approvals expanding afatinib’s use beyond first-line settings or in combination regimens could stimulate market growth.

4. Pricing and Reimbursement Policies

   Price sensitivity varies across regions. In high-income countries, reimbursement favors innovative therapies, but cost-effectiveness remains scrutinized, especially as generics enter the market. In emerging markets, affordability may limit afatinib’s penetration unless supported by government programs or pricing strategies.

5. R&D and Pipeline Developments

   Ongoing research aims to optimize afatinib’s use, including combination treatments with immunotherapies or anti-angiogenic agents. Positive clinical trial results could extend its indications and market lifespan.

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Financial Trajectory and Revenue Projections

Pfizer’s 2022 financial reports indicated that afatinib generated approximately $0.7 billion globally, accounting for a significant fraction of its oncology revenues [7]. With upcoming patent expirations, revenue forecasts predict a decline, barring strategic maneuvers or pipeline developments.

Revenue Drivers

• Market Penetration and Adoption Rates: Continued clinical acceptance in regions with high EGFR mutation prevalence sustains revenues. However, the rise of competitors may temper growth.
• Pricing Strategies: Premium pricing dominates early in the product life cycle, but price reductions are inevitable as generics or biosimilars enter.
• Regional Expansion: Expansion into emerging markets could offset declines in mature markets, contingent on effective reimbursement policies.

Forecast Scenarios

• Conservative Scenario: Earnings decline at 10–15% annually post-patent expiry, consistent with typical patent cliffs.
• Optimistic Scenario: Strategic alliances, label expansions, or combination therapies prolong revenues and stabilize market share.
• Pessimistic Scenario: Rapid competitive erosion, unsuccessful pipeline translation, or unfavorable regulatory changes could precipitate sharper declines.

Investment and Market Valuation

Investors assessing afatinib’s prospects should consider the timeline for patent expiration, pipeline milestones, and the competitive landscape. Pfizer’s oncology portfolio diversification serves as a buffer against individual drug obsolescence, but standalone revenue from afatinib will likely diminish over the next few years.

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Regulatory and Future Outlook

Regulatory agencies have shown a proclivity for approving next-generation inhibitors over second-generation agents like afatinib due to their efficacy in overcoming resistance mutations. Nonetheless, afatinib’s solid evidence base and established efficacy in first-line settings maintain clinician interest.

Upcoming regulatory considerations include potential label updates to include combination treatments or expanded indications, which could influence its financial trajectory positively.

Research and Development Trajectory

Emerging strategies focus on overcoming resistance and integrating afatinib within combination regimens. Early-phase trials exploring complementarity with immunotherapeutics could renew interest if positive results emerge [8].

Market Entry of Biosimilars and Generics

Patent expiration facilitates biosimilar entry, likely diminishing afatinib’s market share and pricing power. Industry analysts project generic versions could reduce costs by 50–70%, markedly affecting profitability [9].

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Key Market Challenges and Opportunities

• Challenges: Patent expiry, competition from third-generation TKIs (e.g., osimertinib), evolving resistance profiles, and regional reimbursement hurdles.
• Opportunities: Expansion into new indications, combination therapies, and strategic licensing could sustain its market relevance.

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Conclusion

Afatinib dimaleate remains a pivotal therapy within the NSCLC treatment paradigm, buoyed by strong clinical data and regional demand in high-incidence areas. However, its financial trajectory is under significant pressure from patent expiries, emerging competitors, and evolving treatment paradigms. Strategic positioning, including pipeline innovation and regional market expansion, will determine its longevity and profitability.

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Key Takeaways

• Market Position: Afatinib holds a substantial market share in EGFR-mutated NSCLC, especially in Asian markets with high mutation prevalence, but faces growing competition from third-generation TKIs.
• Revenue Outlook: Anticipate revenue decline post-patent expiry, mitigated by potential label expansions, combination therapies, and regional growth.
• Competitive Landscape: Osimertinib dominates as the preferred first-line agent; afatinib's role may shift to combination or later-line therapies.
• Regulatory Trends: Future approvals for resistance mutation management and combination regimens could bolster afatinib’s market viability.
• Strategic Focus: Biodiversity in research, regional expansion, and diversification through combination treatments are critical to extending financial relevance.

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FAQs

1. What factors primarily influence afatinib’s declining revenue potential?
   Patent expiration, increased competition from third-generation TKIs like osimertinib, and the availability of generics post-patent expiry significantly impact revenue prospects.

2. How does regional variation affect afatinib’s market dynamics?
   Higher EGFR mutation prevalence and reimbursement policies in Asia boost demand, whereas Western markets are more sensitive to competition and price considerations.

3. Are there ongoing research efforts to extend afatinib’s clinical utility?
   Yes. Current studies explore combination therapies with immunotherapies and anti-angiogenic agents, aiming to overcome resistance and expand indications.

4. What strategic moves could sustain afatinib’s market relevance?
   Label expansion, line extension, combination therapies, and partnerships for regional distribution are vital strategies.

5. What is the outlook for biosimilar versions of afatinib?
   Biosimilar entrants are likely following patent expiration, creating cost competition and substantially reducing pricing and market share.

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References

[1] WHO. Global Cancer Statistics 2020.
[2] Shigematsu, H., & Seto, T. (2019). Personalized Therapy in Lung Cancer. J Thorac Oncol.
[3] U.S. FDA. Afatinib (Gilotrif) approval. 2013.
[4] Sequist, L. V., et al. (2013). Randomized Phase III Trial. Lancet Oncology.
[5] Soria, J. C., et al. (2018). Osimertinib in Untreated EGFR-Mutated Advanced NSCLC. NEJM.
[6] Pfizer Patent filing and expiry data, 2023–2025.
[7] Pfizer Annual Report 2022.
[8] ClinicalTrials.gov. Trials combining afatinib with immunotherapies.
[9] MarketWatch. Outlook on biosimilar entry post-patent expiry, 2023.