Afatinib

In the clinical treatment of EGFR mutation-positive non-small cell lung cancer (NSCLC), the advent of second-generation irreversible EGFR-TKIs has filled the treatment gap for some patients after the development of resistance to first-generation drugs, and afatinib is a representative drug in this category. It covalently binds to multiple ErbB family receptors such as EGFR, HER2 and HER4, irreversibly blocking the phosphorylation process of tyrosine kinases, and has a stronger and more durable inhibitory effect on signaling pathways compared with first-generation reversible inhibitors. It is clinically mainly used for the first-line treatment of locally advanced or metastatic NSCLC with EGFR exon 19 deletion or exon 21 (L858R) substitution mutation, and can also be used for locally advanced or metastatic squamous histological NSCLC with disease progression during or after platinum-containing chemotherapy. It is one of the first-line treatment options for patients with EGFR sensitive mutations recommended by guidelines.

The global market size of afatinib has maintained steady growth in recent years. In 2023, the overall market size was approximately USD 1.8 billion, with a growth rate of 7.2% in emerging markets. The main driving factors are the increase in the detection rate of EGFR mutations in NSCLC and the continuous improvement of the clinical penetration rate of targeted drugs. In terms of the domestic market, after afatinib was included in the National Medical Insurance Catalog in 2018, the accessibility for patients has been greatly improved. In 2023, the terminal sales in public medical institutions exceeded RMB 900 million. At present, generic drugs from 3 domestic enterprises have been approved for marketing, the market share of the original research drug is gradually diverted by generic products, and the overall market price tends to be reasonable.

The original research enterprise of afatinib is Boehringer Ingelheim, and the original research trade name is "Gilotrif". The core compound patent of afatinib will expire in China in 2029, and other related patents on crystal forms, preparation methods, etc. will expire successively around 2030. The dosage form of the original research drug approved in China is tablet, with specifications of 20mg, 30mg and 40mg, which has been included in the China Listed Medicines Catalog as a reference preparation. In terms of domestic API registration, there are currently 7 afatinib API registration numbers, of which 5 are in status A, which can be jointly reviewed and approved with associated preparations. In China, afatinib tablets from 4 enterprises have been approved for marketing. (Data as of May 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of impurity reference standards for afatinib API, and most of the products are in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards comply with the regulatory requirements of the Chinese Pharmacopoeia, FDA and other regulations, and can fully support the quality research needs in all stages of API R&D, production and registration.