Brigatinib

Brigatinib is a reversible dual inhibitor of ALK and epidermal growth factor receptor (EGFR), with activity against various kinases including ALK, ROS1, insulin-like growth factor 1 receptor, etc.

Brigatinib is mainly used to treat ALK positive metastatic non-small cell lung cancer patients who have developed or are intolerant to crizotinib. However, ALK mutations, overexpression, and the presence of several oncogenic fusion proteins in solid and hematological tumors all indicate its importance and potential as a cancer treatment target.

1.Main components

Brigatinib

2.Adapt to the population

Locally advanced or metastatic non-small cell lung cancer (NSCLC) patients with anaplastic lymphoma kinase (ALK) positivity.

3.Medication for special populations

3.1Pregnant women

Pregnant women taking brigatinib can cause harm to the fetus. If brigatinib is taken during pregnancy, or if the patient becomes pregnant while taking Brigatinib, the potential risks of brigatinib to the fetus should be communicated to the patient.

3.2Lactating women

Due to the possibility of adverse reactions in breastfeeding infants, it is recommended that lactating women do not breastfeed during treatment with brigatinib and within one week after the last dose.

3.3Geriatric Use

No overall difference in safety or efficacy was observed between patients aged ≥ 65 and younger patients, and it is recommended to use it under the guidance of a doctor.

3.4Pediatric Use

There is currently no data on the efficacy and safety of using Brigatinib in pediatric patients.

4.Drug overdose

At present, there is no specific antidote for drug overdose of Brigatinib. Patients who experience drug overdose should be closely monitored and receive supportive treatment.

5.Drug storage

Store at a temperature not exceeding 30 ℃ in the original packaging.

6.Pharmacokinetics

The geometric mean (CV%) steady-state maximum concentrations (Cmax) of Brigatinib at doses of 90mg and 180mg once daily were 552 (65%) ng/mL and 1452 (60%) ng/mL, respectively, with corresponding area under the concentration time curve (AUC0 Tau) of 8165 (57%) ng · h/mL and 20276 (56%) ng · h/mL.

from FDA，2022.02