Afatinib,Markets and News,API,Afatinib Dimaleate,850140-73-7,ANQING CHICO PHARMACEUTICAL
Abstract
Afatinib dimaleate (CAS 850140?72?6), marketed as Gilotrif™, is an irreversible ErbB-family tyrosine kinase inhibitor developed by Boehringer Ingelheim for EGFR?mutated non?small cell lung cancer (NSCLC). This review outlines its chemical properties, original research and clinical development, regulatory approvals, market introduction and adoption, global sales trajectory, competitive landscape—including first?, second?, and third?generation EGFR inhibitors—and the status of generics. Sales data from 2020–2024 are speculatively projected based on published market analyses. Despite emerging competition (osimertinib, etc.), afatinib maintains a role in specific EGFR?mutation niches, with ongoing research in squamous NSCLC and HER2?driven tumors.
Keywords
Afatinib; BIBW?2992; NSCLC; EGFR inhibitor; Boehringer Ingelheim; Gilotrif; global sales; market competition;
Introduction
Non?small cell lung cancer (NSCLC) accounts for approximately 85 % of lung cancer cases worldwide. A subset of patients harbors activating mutations in the epidermal growth factor receptor (EGFR) gene, rendering tumors sensitive to EGFR tyrosine kinase inhibitors (TKIs). Afatinib, a second?generation TKI, was developed to overcome resistance seen with first?generation agents (erlotinib, gefitinib) by irreversibly inhibiting EGFR and HER2 kinases. Its clinical promise and subsequent adoption have shaped both treatment paradigms and the targeted therapy market.
1. Chemical Properties
Chemical Name:Afatinib
CAS No.:850140-72-6
Molecular Formula:C24H25ClFN5O3
Molecular Weight:485.946
Chemical Name:Afatinib Dimaleate
CAS No.:850140-73-7
Molecular Formula:2C4H4O4*C24H25ClFN5O3
Molecular Weight:718.092
2. Original Research and Approval Timeline
Discovery & Development: Boehringer Ingelheim (BIBW?2992) underwent preclinical development targeting EGFR/HER2 kinases.
Phase III Trials (LUX?Lung Series): Began in 2010 (LUX?Lung 5), demonstrating superior progression?free survival vs. chemotherapy and erlotinib in various EGFR?mutant NSCLC cohorts.
Orphan Drug Designation (NSCLC): 12 March 2012 (FDA)
FDA First?Line Approval: 12 July 2013 for metastatic EGFR exon 19/21 mutation?positive NSCLC
EMA Approval: 25 July 2013 for the same indication (Giotrif™)
China TFDA Approval: 17 May 2013 for EGFR?mutant NSCLC
Second?Line Squamous NSCLC: 15 April 2016 (FDA)
Patent/Exclusivity End: U.S. exclusivity ended 12 July 2020
3. Market Presence and Sales
Afatinib launched globally mid?2013 and has since gained inclusion on national formularies, including China’s NRDL. The global market size was estimated at USD 692.6 M in 2022. with an expected CAGR of 18.97 % through 2032. Based on this forecast and market dynamics, we project:
2020: ~ USD 490 M
2021: ~ USD 582 M
2022: USD 692.6 M
2023: ~ USD 823 M
2024: ~ USD 978 M
4. Market Competition
First?Generation EGFR TKIs: Erlotinib (Tarceva®), gefitinib (Iressa®) – face incremental competition in efficacy and safety profiles.
Third?Generation EGFR TKIs: Osimertinib (Tagrisso®) targeting T790M mutation has become standard in first?line and second?line, eroding afatinib’s market share
Other TKIs: Icotinib, dacomitinib, lazertinib.
Biologics/Combinations: Bevacizumab combinations, emerging immunotherapies, altering treatment algorithms.
5. Generics and Production
U.S. Market: No generic versions available as of April 2025; afatinib remains Boehringer Ingelheim’s proprietary product
China and Other Regions: Domestic manufacturers (e.g., Hengrui Medicine, Beacon Pharma) are preparing generics pending local approvals, driven by patent expirations and inclusion in national reimbursement schemes.
Contract Manufacturing: BI’s CDMO network continues supplying active ingredient for branded and future generic formulations.
6. Future Perspectives and Recent Developments
Additional Indications: Investigational in HER2?positive breast cancer; potential in other ErbB?driven malignancies.
Combination Strategies: Afatinib plus chemotherapy or other targeted agents under evaluation to enhance durability of response.
Health Economics: Budget?impact analyses suggest marginal per?patient cost increase upon NRDL listing, reflecting favorable cost?effectiveness in EGFR?del19 cohorts.
Regulatory Expansions: Indication broadened in January 2018 for non?resistant EGFR mutations beyond exon 19/21
References
Business Research Insights. Afatinib Market 2024 To 2032. Global Report. Global market size USD 692.6 M in 2022; CAGR 18.97 %
FDA. Drug Approval Package: Gilotrif (afatinib) Tablets. Approval Date: 7/12/2013
FDA OOPD Database. Orphan Drug Designation for afatinib. Marketing Approval: 04/15/2016; Exclusivity ends 04/15/2023.
Wikipedia. Afatinib Infobox: IUPAC name, formula, molar mass, mechanism of action.
Drugs.com. Generic Gilotrif Availability as of April 10. 2025: no generic available in U.S. .
Value in Health. Zhang et al., 2018. Budget Impact Analysis of Afatinib in China. First?line NRDL impact.
Wikipedia (zh). 阿法替尼 section on approvals: FDA, EMA, TFDA dates.
Note: Sales projections are speculative, based on a reported CAGR and may vary with real?world uptake, competition, and pricing dynamics.
Active Pharmaceutical Ingredient
Afatinib Dimaleate,850140-73-7(chemical grade, purity ≥99.0%) are currently supplied by our company. [Own compliance factory, fully support factory audit] For details, you can call the bottom line to get the latest price of the product!
Disclaimer:Products are only available to countries where there is no valid patent protection. Products still covered by patents rights are available exclusively for experimental or registration purpose pursuant to national applicable law, and shall be sold in strict accordance with the laws of the People's Republic of China and the laws of the Buyer's country. All products are not for human use. Buyer is obligated for evaluation of the patent situation in its domestic market and shall be held liable for uses which do not fall within the scope of the experimental or registration use exception and are not permitted by national applicable law.
References or other information:
FDA,Wikipedia,Chatgpt,DeepSeek,chemicalbook,lookchem.
If there is any infringement, please apologize and delete. If there are any errors, welcome to criticize and correct.
Under no circumstances shall the information or opinions expressed herein be construed as investment advice for any person.
International Department:
Copyright(C)2018 Anqing Chico Pharmaceutical Co., Ltd.
Supported byChinaChemNet
