Ceritinib

Anaplastic lymphoma kinase (ALK) fusion mutation is an important driver subtype of non-small cell lung cancer (NSCLC), accounting for approximately 3% to 5% of NSCLC cases. Patients of this type often face the dilemma of limited treatment options after developing resistance to first-generation ALK inhibitors. Ceritinib belongs to the second-generation ALK tyrosine kinase inhibitor. By highly selectively binding to the ALK target, it inhibits the activation of downstream signaling pathways and further blocks the proliferation of tumor cells. It not only has a significant therapeutic effect on ALK-positive treatment-naïve NSCLC patients, but also covers common drug-resistant mutations of first-generation inhibitors. At present, it has been approved for the first-line and subsequent-line treatment of ALK-positive locally advanced or metastatic NSCLC, providing a longer-acting treatment option for the population with ALK-mutant lung cancer.

The global market size of ALK inhibitors has exceeded USD 9 billion in 2023, with a compound annual growth rate maintained at around 12%. Among them, the second-generation ALK inhibitors have accounted for more than 60% of the market share due to their prominent clinical advantages. In terms of the domestic market, after entering China in 2018, ceritinib was included in the National Medical Insurance Catalog in 2020, which greatly improved the accessibility of medication. At present, 3 domestic enterprises have obtained approval for generic preparations of ceritinib, and the market share of the original research product has dropped from 89% in 2021 to 57% in 2023. With the continuous increase in the penetration rate of generic drugs, the market demand for upstream API is expected to maintain an annual growth rate of 15%.

The original research enterprise of ceritinib is Novartis, and the original research trade name is Zykadia. Its core compound patent will expire in China in September 2024, and the crystal form patent will expire in 2029. The dosage form approved by the original research is capsule, with a specification including 150 mg. It has been included in the China Listed Medicines Catalogue as the reference listed drug, and is also included in the FDA Reference Listed Drug Catalog. Up to now, the Center for Drug Evaluation (CDE) of the National Medical Products Administration of China has publicized 6 registration entries of ceritinib API, among which 3 are in Status A, which can be associated with domestic preparation applications. Domestically, ceritinib capsules from Novartis' original research and 3 generic drug enterprises have been approved for marketing. (Data as of June 2025, please refer to the official website of CDE for the latest information.)

CATO can provide a full set of impurity standards for ceritinib API. All reference standards meet the compliance requirements of multiple regulatory systems such as Chinese Pharmacopoeia and FDA. Most products support spot supply. Spot orders submitted before 16:00 can be delivered on the same day, fully meeting the supply chain needs of pharmaceutical enterprises in the whole process of R&D, quality research and declaration.