Lapatinib

For the treatment of HER2-positive advanced breast cancer, targeted combination regimens have become the core clinical pathway. As a small-molecule tyrosine kinase inhibitor, lapatinib can simultaneously inhibit the intracellular kinase domains of epidermal growth factor receptor (EGFR) and HER2, block the conduction of downstream MAPK and PI3K/AKT signaling pathways, and can more comprehensively inhibit tumor proliferation compared with single-target drugs. It is often clinically used in combination with capecitabine to treat patients with HER2-positive metastatic breast cancer who have previously received anthracycline, taxane and trastuzumab therapy, and can also be combined with letrozole for postmenopausal women with metastatic breast cancer who are hormone receptor-positive and HER2-positive, providing an important oral treatment option for patients after trastuzumab resistance.

The global lapatinib market size exceeded USD 420 million in 2021. Driven by the increase in breast cancer screening rates and the growth of targeted therapy penetration in emerging markets, the compound annual growth rate is expected to remain at around 3.8% in 2025. In terms of the Chinese market, as HER2-positive breast cancer targeted drugs are included in the medical insurance, the in-hospital sales of lapatinib in China reached RMB 1.27 billion in 2023. At present, the original research product still accounts for nearly 60% of the market share, and 3 domestic enterprises have been approved to market generic drugs. After the implementation of the centralized procurement policy, the price drop has exceeded 70%, and the accessibility has been significantly improved.

The original research enterprise of lapatinib is GlaxoSmithKline, and the original research trade name is Tykerb. The expiration date of its core compound patent in the United States is 2021, and the expiration date of the compound patent in China is 2019. The main dosage form approved for the original research is tablet, with the specification of 250mg. It has been included in the *Catalogue of Reference Preparations of Chemical Drugs* of China, and is also a reference preparation recognized by the FDA. Up to now, China NMPA has approved 10 registration numbers of lapatinib API, 7 of which are in status A (can be used in marketed preparations), and a number of preparation varieties including original research and generic drugs have been approved for marketing in China. (Data as of September 2024, please refer to the official CDE website for the latest information)

CATO provides a full set of lapatinib impurity reference standards, covering synthetic starting materials, intermediates, process impurities and degradation impurities. Most 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 compliance requirements of multiple regulations such as the Chinese Pharmacopoeia and FDA, and can meet the needs of the whole process of API R&D, quality research and declaration.