Pemetinib/pemetinib is the first generation of targeted therapy drugs

Pemigatinib is a selective fibroblast growth factor receptor (FGFR) inhibitor. Strictly speaking, it does not belong to the “generation” targeted drug classification system in the traditional sense. Different from targeted drugs targeting common mutation pathways such as EGFR, ALK or HER2, FGFR inhibitors are mainly used to treat tumors carrying FGFR fusions, rearrangements or mutations, representing the exploration of new molecular pathways in the field of targeted therapy.

The innovation of Pemetinib is that it breaks through the limitations of traditional targets and specifically targets FGFR gene mutations that drive the development of cancer in certain malignant tumors. In the development sequence of targeted drugs, the first-generation drugs are usually non-selective inhibitors, which may bring more side effects; the second or third generation emphasizes selectivity and drug-resistant mutation coverage. Pemetinib is one of the first FGFR inhibitors approved by the FDA for the treatment of FGFR2 fusion-positive patients with cholangiocarcinoma, and represents a highly selective targeting strategy for rare mutation pathways. Therefore, in the field of targeted therapy, it can be regarded as the "first representative" of the FGFR targeting pathway, ushering in a new era of FGFR therapy.

From the perspective of technology platform, pemetinib combines the emerging achievements of genetic testing and molecular pharmacology, emphasizing "gene first, precise matching" in the treatment strategy, and is a highly dependent targeted drug for companion diagnosis. This also means that its applicable population is relatively precise, and the efficacy is highly related to the patient’s genetic status. In addition, pemetinib also has a tolerable safety profile, allowing patients to maintain a good quality of life during treatment.

Overall, although it cannot be accurately positioned in the traditional generation system, pemetinib is undoubtedly a key representative in the process of expanding targeted therapy to more rare mutation pathways, and is an important achievement in the diversified development trend of modern molecular targeted therapy.

Reference materials:https://go.drugbank.com/drugs/DB15102