Asciminib

There has long been an unmet clinical need for the treatment of advanced solid tumors with KRAS G12C mutation. As a second-generation KRAS G12C inhibitor, adagrasib covalently binds to the cysteine residue of the KRAS G12C mutant protein, locks the inactive conformation of the protein, and blocks the conduction of downstream signaling pathways. Compared with the first-generation drugs of the same class, it has higher target selectivity and lower off-target risk. Currently, its approved indication is mainly for adult patients with KRAS G12C mutation-positive locally advanced or metastatic non-small cell lung cancer who have received at least one prior systemic therapy. In the meantime, clinical studies in the fields of solid tumors such as colorectal cancer and pancreatic cancer are also in progress.

The size of the global KRAS inhibitor market had exceeded USD 1.8 billion in 2023, with a compound annual growth rate of over 75%. Among them, adagrasib, with its better safety and efficacy data, achieved a global sales revenue of USD 290 million in 2023, accounting for 16% of the KRAS inhibitor market share. At present, only the original research enterprise holds the commercialization rights and interests of adagrasib worldwide, the compound patent has not yet expired, and the layout of generic drugs is still in the early stage. More than 10 domestic pharmaceutical companies have initiated the research and development of generic drugs and bioequivalence trials.

The original research enterprise of adagrasib is Mirati Therapeutics in the United States, with the trade name Adagrasib. The core compound patent of adagrasib will expire in 2036 in the United States, and in 2037 in China. The dosage form approved by the original research is tablet, with two specifications of 100mg and 200mg, which has been included in the Reference Listed Drug Catalog of the US FDA, and has not yet been included in the *Catalog of Chemical Drugs* of China. There is no domestic Drug Master File (DMF) registration number for adagrasib API approved for marketing. The original research preparation was granted conditional marketing approval by the National Medical Products Administration in September 2023, and no domestic generic drug preparation has been approved yet. (Data as of June 2025, please refer to the official website of CDE for the latest information)

CATO can provide a full set of adagrasib impurity reference standards, covering all types of research reference substances including process impurities and degradation impurities. Most of the products are available from stock. For stock orders placed before 16:00, delivery can be made on the same day. All products meet the requirements of multiple regulatory systems such as the Chinese Pharmacopoeia and FDA, and can fully meet various use needs in the stages of API research and development, quality research and declaration.