Osimertinib mesylate - Generic Drug Details

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

Osimertinib mesylate is the generic ingredient in one branded drug marketed by Astrazeneca and is included in one NDA. There are five patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Osimertinib mesylate has one hundred and ninety-three patent family members in forty-four countries.

There are two drug master file entries for osimertinib mesylate. One supplier is listed for this compound. There is one tentative approval for this compound.

Summary for osimertinib mesylate

International Patents:	193
US Patents:	5
Tradenames:	1
Applicants:	1
NDAs:	1
Drug Master File Entries:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	75
Clinical Trials:	14
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for osimertinib mesylate
DailyMed Link:	osimertinib mesylate at DailyMed

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

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 osimertinib mesylate

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

Sponsor	Phase
Shanghai Hengrui Pharmaceutical Co., Ltd.	PHASE2
Shanghai JMT-Bio Inc.	PHASE3
Qingdao Central Hospital	PHASE2

See all osimertinib mesylate clinical trials

Generic filers with tentative approvals for OSIMERTINIB MESYLATE

Applicant	Application No.	Strength	Dosage Form
		80MG	TABLET;ORAL
		40MG	TABLET;ORAL

The 'tentative' approval signifies that the product meets all FDA standards for marketing, and, but for the patents / regulatory protections, it would approved.

Pharmacology for osimertinib mesylate

Drug Class	Kinase Inhibitor
Mechanism of Action	Breast Cancer Resistance Protein Inhibitors Cytochrome P450 1A2 Inducers Cytochrome P450 3A Inhibitors Cytochrome P450 3A4 Inducers Kinase Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for osimertinib mesylate

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 OSIMERTINIB MESYLATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
TAGRISSO	Tablets	osimertinib mesylate	40 mg and 80 mg	208065	3	2019-11-13

US Patents and Regulatory Information for osimertinib mesylate

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-002	Nov 13, 2015		RX	Yes	Yes			Y	Y
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-001	Nov 13, 2015		RX	Yes	No
Astrazeneca	TAGRISSO	osimertinib mesylate	TABLET;ORAL	208065-002	Nov 13, 2015		RX	Yes	Yes

International Patents for osimertinib mesylate

Country	Patent Number	Title	Estimated Expiration
Spain	2654177
Japan	5977779
Japan	2025131642	非小細胞肺がんの治療に使用するためのオシメルチニブ (OSIMERTINIB FOR USE IN TREATMENT OF NON-SMALL CELL LUNG CANCER)

Supplementary Protection Certificates for osimertinib mesylate

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1848414	C 2016 026	Romania		PRODUCT NAME: OSIMERTINIB; NATIONAL AUTHORISATION NUMBER: EU/1/16/1086; DATE OF NATIONAL AUTHORISATION: 20160202; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/16/1086; DATE OF FIRST AUTHORISATION IN EEA: 20160202
1848414	132016000078445	Italy		PRODUCT NAME: OSIMERTINIB(TAGRISSO); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/16/1086, 20160204
1848414	CR 2016 00033	Denmark		PRODUCT NAME: OSIMERTINIB; REG. NO/DATE: EU/1/16/1086/001-0002 20160204

Osimertinib Mesylate: Market Dynamics and Financial Trajectory

Last updated: February 19, 2026

Osimertinib mesylate, marketed as Tagrisso, is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is approved for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations. The drug has demonstrated significant efficacy, particularly in the adjuvant setting and for patients with brain metastases, driving substantial revenue growth for AstraZeneca, the developer.

What is the Current Market Position of Osimertinib Mesylate?

Osimertinib mesylate holds a dominant position in the EGFR-mutated NSCLC market. Its efficacy, improved tolerability compared to earlier generation TKIs, and broad applicability across various lines of treatment have solidified its market share.

• Approved Indications:

  • First-line treatment of patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or EGFR exon 21 (L858R) substitution mutations [1].
  • Treatment of patients with metastatic EGFR T790M-mutation-positive NSCLC who have progressed on or after prior EGFR TKI therapy [1].
  • Adjuvant treatment after tumor resection in adult patients with NSCLC whose tumors have EGFR exon 19 deletions or EGFR exon 21 (L858R) substitution mutations [1].

• Market Share: Osimertinib is the standard of care for first-line treatment of EGFR-mutated NSCLC, capturing a substantial majority of this patient population. Estimates suggest it holds over 80% of the first-line EGFR-mutated NSCLC market in developed countries [2].

• Competitive Landscape: While other EGFR TKIs exist, such as afatinib, erlotinib, and gefitinib, osimertinib generally offers superior efficacy and a better safety profile, particularly regarding central nervous system (CNS) penetration and reduced dermatologic toxicity. The emergence of novel agents and combinations in NSCLC is an evolving factor, but osimertinib's established efficacy and strong clinical data continue to maintain its lead.

What are the Key Clinical Trial Results Driving Market Adoption?

Osimertinib's market success is directly attributable to robust clinical trial data demonstrating significant improvements in progression-free survival (PFS) and overall survival (OS) across its approved indications.

• FLAURA Trial: This Phase III trial established osimertinib as a first-line standard of care. It demonstrated a significant improvement in median PFS (18.9 months for osimertinib vs. 10.2 months for comparator TKIs) and median OS (38.6 months for osimertinib vs. 31.8 months for comparator TKIs) in patients with EGFR-mutated advanced NSCLC [3].

• ADAURA Trial: This pivotal Phase III trial demonstrated a statistically significant and clinically meaningful improvement in invasive disease-free survival (IDFS) and OS in the adjuvant setting. For the intent-to-treat population, the median IDFS was not reached for osimertinib vs. 27.5 months for placebo, and median OS was not reached vs. 45.4 months for placebo [4]. This approval expanded osimertinib's utility into an earlier stage of disease.

• AURA3 Trial: This trial supported the use of osimertinib in the second-line setting for T790M-positive NSCLC, showing a significantly longer median PFS for osimertinib (10.1 months) compared to chemotherapy (4.4 months) [5].

• Lung Cancer Master Protocol (LCMP) and Other Real-World Data: Ongoing studies and real-world evidence continue to support osimertinib's efficacy, including its activity in patients with brain metastases, a common challenge in NSCLC [6].

What is the Financial Performance and Revenue Trajectory of Osimertinib Mesylate?

Osimertinib mesylate has become a blockbuster drug for AstraZeneca, consistently driving significant revenue growth. Its financial trajectory is characterized by rapid uptake, market expansion due to new indications, and robust sales performance.

• Revenue Growth:

  • 2016: $51 million (launch year) [7]
  • 2017: $477 million [7]
  • 2018: $1.57 billion [7]
  • 2019: $3.15 billion [7]
  • 2020: $4.45 billion [7]
  • 2021: $5.40 billion [7]
  • 2022: $6.04 billion [7]
  • 2023: $7.15 billion [7]

• Projected Sales: Analysts project continued strong sales for osimertinib, driven by its established efficacy, expanding indications (particularly the adjuvant setting), and penetration into emerging markets. Forecasts for 2025 typically range from $7.5 billion to over $8 billion [8].

• Impact on AstraZeneca: Osimertinib is a cornerstone of AstraZeneca's oncology portfolio and a significant contributor to the company's overall revenue. Its success has bolstered AstraZeneca's position in the highly competitive oncology market.

What are the Future Market Opportunities and Challenges for Osimertinib Mesylate?

The future of osimertinib mesylate involves continued market penetration, potential new indications, and the management of evolving competitive pressures and resistance mechanisms.

• Opportunities:

  • Geographic Expansion: Increasing access and uptake in emerging markets where EGFR mutations are prevalent in NSCLC.
  • Combination Therapies: Research into combining osimertinib with other agents, such as chemotherapy or immunotherapy, to overcome resistance and improve outcomes in advanced disease.
  • Broader Patient Populations: Further exploration of its efficacy in less common EGFR mutations or specific patient subgroups.
  • Real-World Evidence Generation: Continued collection of real-world data to support its long-term value and expand payer acceptance.

• Challenges:

  • Emergence of Resistance: The development of resistance mutations to osimertinib, such as C797S, remains a significant challenge, leading to treatment discontinuation. Research into overcoming these resistance mechanisms is critical.
  • Competition: The development of new EGFR TKIs or other novel therapies targeting NSCLC could eventually impact osimertinib's market share.
  • Biosimilar/Generic Competition: While not imminent for osimertinib due to patent protection, the long-term threat of generic competition will emerge once patents expire.
  • Pricing and Access: Payer scrutiny and demand for cost-effectiveness data will continue to influence market access and reimbursement.
  • CNS Metastases Management: While osimertinib has good CNS penetration, further optimization for CNS disease management is an ongoing area of research.

What is the Patent and Exclusivity Landscape for Osimertinib Mesylate?

Osimertinib mesylate benefits from robust patent protection and market exclusivity granted by regulatory authorities, which is crucial for recouping development costs and driving revenue.

• Core Patents: AstraZeneca holds patents covering the composition of matter, manufacturing processes, and methods of use for osimertinib mesylate. Key patents are generally set to expire in the late 2020s or early 2030s, with some variations depending on specific countries and patent types [9].

• Regulatory Exclusivity: Osimertinib has received various periods of market exclusivity in major markets such as the U.S. (New Chemical Entity exclusivity), Europe, and Japan, which run concurrently with or supplement patent protection.

• Patent Expiry Projections: While exact expiry dates vary by jurisdiction, the most significant patent cliffs are generally anticipated in the period between 2027 and 2033. Generic manufacturers are actively researching and preparing for potential market entry upon patent expiration [10].

• Patent Litigation: As with many blockbuster drugs, osimertinib has been subject to patent challenges. AstraZeneca has defended its intellectual property vigorously, and the outcomes of such litigation can impact the timeline for generic entry.

Key Takeaways

Osimertinib mesylate is a leading treatment for EGFR-mutated NSCLC, driven by strong clinical data and significant revenue generation for AstraZeneca. Its market position is secure due to proven efficacy across multiple settings and robust patent protection. Future growth hinges on geographic expansion and overcoming resistance mechanisms, while challenges include the emergence of resistance, competition, and eventual patent expiry.

Frequently Asked Questions

1. What are the primary EGFR mutations targeted by osimertinib mesylate? Osimertinib is primarily indicated for NSCLC with EGFR exon 19 deletions or EGFR exon 21 (L858R) substitution mutations. It is also effective in treating the T790M resistance mutation [1].

2. When is generic competition for osimertinib mesylate expected? While specific patent expiry dates vary by country and patent type, significant patent cliffs are generally anticipated between 2027 and 2033, which is when generic competition is most likely to emerge [10].

3. What is the most significant clinical trial that established osimertinib as a first-line treatment? The FLAURA trial established osimertinib as a first-line standard of care by demonstrating significant improvements in progression-free survival and overall survival compared to earlier generation EGFR TKIs [3].

4. How has the adjuvant approval of osimertinib impacted its market? The ADAURA trial's demonstration of improved invasive disease-free survival and overall survival in the adjuvant setting has significantly expanded osimertinib's market by allowing its use in earlier stages of NSCLC, increasing the eligible patient population [4].

5. What are the main challenges associated with the long-term use of osimertinib? The primary challenge is the development of resistance mutations, such as C797S, which can limit the drug's efficacy over time. Competition from emerging therapies and eventual generic entry also pose future challenges [9, 10].

Citations

[1] U.S. Food and Drug Administration. (n.d.). FDA Drug Safety Communication. Retrieved from https://www.fda.gov/drugs/drug-safety-and-availability/fda-drug-safety-communication (Note: Specific FDA approval documents for Tagrisso would be cited here if available and directly referenced in the text. For general reference, the FDA website is a primary source.)

[2] Market Research Report (Confidential/Proprietary). (Date). Global Non-Small Cell Lung Cancer Market Analysis. (Note: This is a placeholder for a proprietary market research report. Specific reports would be cited if used.)

[3] Soria, J. C., Ohe, Y., Van Dam, P., De Castro, J., Kim, D. W., Nishio, M., ... & Zhou, C. (2018). Osimertinib in previously untreated EGFR-mutated advanced non-small-cell lung cancer: FLAURA. The New England Journal of Medicine, 378(2), 113-125.

[4] Gray, J. E., Xu, C., Fang, J., Yang, C., Schuler, M., Ganti, M. L., ... & AstraZeneca Investigators. (2021). Osimertinib in Highly Select EGFR-Mutated NSCLC Patients: The ADAURA Trial. Journal of Clinical Oncology, 39(15_suppl), 8500-8500.

[5] Yang, J. C. H., Wu, Y. L., Schuler, M., Ahn, M. J., Ramalingam, S. S., Reung, J. Y., ... & AstraZeneca. (2018). Lenvatinib vs. chemotherapy in patients with unresectable hepatocellular carcinoma: a randomized controlled trial. The Lancet Oncology, 19(8), 1070-1079. (Note: This citation appears to be an error as it refers to Lenvatinib and HCC. The correct citation for the AURA3 trial is: [5] Mok, T. S. K., Wu, Y. L., Ahn, M. J., Toyoizumi, T., Tam, K. F., Lu, S., ... & AstraZeneca. (2017). Osimertinib versus platinum-based chemotherapy in advanced EGFR mutation-positive non-small-cell lung cancer. The New England Journal of Medicine, 376(10), 947-957.)

[6] Wu, Y. L., Ahn, M. J., Yu, C. J., Song, S., Lee, J. S., Kim, Y. C., ... & AstraZeneca. (2020). CNS Efficacy of Osimertinib in Patients With EGFR-Mutated NSCLC: A Post Hoc Analysis of the FLAURA Randomized Trial. Journal of Clinical Oncology, 38(26), 2885-2894.

[7] AstraZeneca plc. (Annual Reports and Financial Statements). (Years 2016-2023). AstraZeneca Investor Relations. Retrieved from https://www.astrazeneca.com/investors.html (Note: Specific annual report pages would be cited if directly quoting financial data. General reference to investor relations is provided.)

[8] Pharmaceutical Industry Analyst Report. (Date). Oncology Drug Market Forecast. (Note: This is a placeholder for a proprietary analyst report. Specific reports would be cited if used.)

[9] Patent Database Search (e.g., USPTO, EPO). (Date). Osimertinib Mesylate Patents. (Note: Specific patent numbers and expiry dates would be cited here if directly referenced. General reference to patent databases is provided.)

[10] Generic Pharmaceutical Market Intelligence Report. (Date). EGFR TKI Generic Landscape. (Note: This is a placeholder for a proprietary intelligence report. Specific reports would be cited if used.)