Furmonertinib belongs to which generation of targeted drugs and an introduction to its technical advantages

Furmonertinib (Furmonertinib) is a drug that targets EGFR mutation-positive non-small cell lung cancer (NSCLC) oral targeted drugs, which belong to the third generation of EGFRtyrosine kinase inhibitors (EGFR-TKI). Compared with first-generation (such as gefitinib, erlotinib) and second-generation (such as afatinib, dacomitinib) EGFR-TKI, third-generation drugs can more effectively target EGFR-TKIs with T790Mtumor cells with drug-resistant mutations also have less inhibitory effect on wild-type EGFR, thus prolonging the survival of patients while reducing the risk of side effects.

The technical advantage of fumetinib is mainly reflected in its high selectivity for drug-resistant mutations. T790M mutation is the main cause of early EGFR-TKI resistance. Traditional first- and second-generation drugs are not sensitive enough to this mutation. , and fumetinib can specifically inhibit the T790M mutated EGFR, thereby significantly delaying the occurrence of drug resistance and improving the therapeutic effect. This makes it an important option for patients with EGFR mutated NSCLC in first- or second-line treatment, especially for patients who have developed resistance after prior EGFR-TKI treatment.

Another significant advantage is the good blood-brain barrier permeability of fumetinib. The incidence of brain metastasis is higher in lung cancer patients, and fumetinib can effectively cross the blood-brain barrier and also has a certain inhibitory effect on central nervous system lesions. This is very critical clinically, because brain metastasis is often one of the main factors for poor prognosis of patients, and fumetinib has shown potential advantages in controlling brain metastasis and improving quality of life.

In addition, fumetinib also performed well in terms of tolerability and safety. Compared with the previous two generations of EGFR-TKI, it has weaker inhibition of wild-type EGFR, so the incidence of side effects such as rash and diarrhea is reduced, and patients can take long-term oral treatment to improve medication compliance. Combined with its high selectivity, drug-resistant mutation coverage and brain metastasis control capabilities, fumetinib has shown comprehensive technical advantages in patients with EGFR mutated NSCLC and has become one of the important representatives of the current third-generation targeted therapy.

Reference materials:https://www.drugs.com/