What are the main contents of Vebreltinib instructions?

Vebreltinib (vebreltinib) is a new type of targeted drug that has attracted much attention in recent years. It was developed by BridgeBio Pharma in cooperation with its subsidiaries. The trade name has not yet been unified globally. The drug is a highly selective MET tyrosine kinase inhibitor (MET-TKI) that mainly targets malignant tumors with MET gene abnormalities, especially in non-small cell lung cancer (NSCLC) and specific types of brain gliomas. Since the end of 2024, bricitinib has been granted orphan drug status by the US FDA and has entered the clinical application stage in many countries around the world. In 2025, its instructions have been updated in multiple international drug databases, marking its continuous improvement in precision tumor treatment.

From the drug information, the indications of boricitinib mainly include two categories: first, patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with stromal-epithelial transformation factor (MET) exon 14 skipping. This mutation subtype accounts for about 3% of the lung cancer population and is often associated with advanced age and a low smoking history. It is a type of driver gene mutation. Bripretinib inhibits the abnormal activation of the MET pathway and blocks the growth and metastasis signals of tumor cells, thereby achieving targeted inhibition. Secondly, another indication mentioned in its instructions is patients with IDH-mutant astrocytoma (WHO grade 4) with PTPRZ1-MET fusion gene or glioblastoma that progresses from low-grade astrocytoma. Brixitinib offers a new precision treatment option for patients with this type of brain tumor, which has rare genetic signatures and a poor prognosis.

In terms of usage and dosage, the instructions recommend that the starting dose for patients with non-small cell lung cancer is200mg orally taken twice a day (once in the morning and once in the evening), while the recommended starting dose for patients with glioma is slightly higher, 300mg, taken orally twice a day. The medicine needs to be taken on an empty stomach, that is, fasting is required at least 2 hours before taking the medicine and half an hour after taking the medicine, but you can drink water. Studies have found that taking it on an empty stomach can improve drug bioavailability and reduce the interference of gastric acid on absorption. Treatment should be continued until the patient develops intolerable adverse reactions or disease progression, reflecting the characteristics of long-term maintenance treatment.

From a pharmacological perspective, boricitinib binds to the MET kinase domain, inhibits MET phosphorylation, blocks the downstream PI3K/AKT and RAS/MAPK signaling pathways, thereby inhibiting tumor cell proliferation, migration and invasion. Compared with the first-generation MET inhibitors (such as crizotinib), bripretinib has higher molecular selectivity, stronger inhibitory effect on common MET mutations, and excellent central nervous system (CNS) penetration. This is also an important basis for its use in the treatment of MET fusion glioma.

In terms of drug safety, the instructions indicate that the most common adverse reactions of boricitinib include mild to moderate gastrointestinal reactions (such as nausea, diarrhea), mild elevation of aminotransferases, fatigue, and peripheral edema. Most side effects can be alleviated by dose adjustment or symptomatic treatment. The instructions suggest that in the event of grade 3 or above liver function abnormalities, severe rash, or persistent gastrointestinal reactions, administration should be suspended and resumed after evaluation by a physician.

Reference materials:https://www.asymbio.com.cn/