Instructions for taking and using brigatinib

Indications:

1.It is mainly used to treat patients with anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC). For such patients, brigatinib can effectively prevent the growth and spread of tumor cells by specifically inhibiting the activity of ALK protein.

2.Suitable for patients with ALK positive non-small cell lung cancer who are resistant to crizotinib treatment. For patients who have been treated with crizotinib but encounter resistance issues,

3.For patients who are resistant to osimertinib, especially when the tumor contains both EGFR and ALK targets, brigatinib is also an effective treatment option.

Mechanism of action:

Brigatinib is a small molecule targeted drug that mainly targets the fusion genes of ALK (anaplastic lymphoma kinase) and ROS1 (proto-oncogene receptor tyrosine kinase). Its mechanism of action is by binding to these fusion genes, inhibiting their kinase activity, thereby blocking downstream signaling pathways. This blocking effect can significantly interfere with the proliferation and survival of tumor cells, leading to cell cycle arrest or death. In addition, brigatinib can also inhibit tumor angiogenesis and prevent tumors from obtaining necessary nutrients and oxygen, thereby further enhancing its anti-tumor effect and promoting tumor cell apoptosis.

Medication method:

The recommended starting dose of brigatinib is 90mg daily, with a dose increase to 180mg daily during the first seven days of initial treatment if the patient tolerates this dose well.

Side effects:

Using brigatinib may be associated with some side effects. About 30% of patients may experience gastrointestinal discomfort, including nausea, vomiting, diarrhea or loss of appetite. These are generally mild and can be relieved by dietary modification, meal sharing and oral antiemetic drugs. In addition, about 10% of patients may develop interstitial lung disease, manifested by coughing and dyspnea. This is a more serious side effect. Once it occurs, the medication should be stopped immediately and medical evaluation should be sought.

In addition, about15% of patients may have abnormal liver function, specifically manifested as elevated liver enzymes, so liver function indicators need to be monitored regularly during treatment. In addition, some patients may develop blood system problems such as anemia or neutropenia, which need to be monitored through regular blood tests. Other possible side effects include skin rash, high blood sugar, fatigue, headache, dizziness, and cardiovascular problems such as high blood pressure and cardiac arrhythmia. Most of these side effects are mild to moderate, but still require close attention and prompt treatment.

Warnings and precautions:

There are some potential risks that require special attention when using brigatinib. First, patients may be at risk for severe interstitial lung disease (ILD), a life-threatening condition. In clinical trials, ILD occurred in 3.7% and 9.1% of patients in the 90 mg and 180 mg groups, respectively. Therefore, patients need to be closely monitored for new or worsening respiratory symptoms. Secondly, brigatinib treatment may cause hypertension, especially when the dose is increased. In clinical trials, the incidence of hypertension in the 90 mg group was 11% an>, and the 90→180mg group was as high as 21%. The incidence of grade 3 hypertension is 5.9%, so patients need to undergo routine blood pressure monitoring.

In addition, brigatinib may also cause bradycardia, and patients' heart rate should be monitored during treatment. In the trial, heart rates below 50 beats per minute occurred at 90mg and 180mgThe groups were 5.7% and 7.6% respectively. Also, brigatinib may cause visual impairment, including blurred vision and double vision. In clinical trials, the incidence rates of such adverse reactions in different dose groups were 7.3% and 10% respectively.

Drug interactions:

Due to the potential for drug interactions, concurrent use with strong CYP3A ** should be avoided or dosage adjustments should be made as necessary to ensure the safety and effectiveness of the treatment.

Medication for special populations:

For pregnant and lactating women, and those with liver and kidney dysfunction, the use of brigatinib needs to be carefully considered and is best done under the guidance of a professional physician to reduce potential risks.

References:

https://www.drugs.com/mtm/brigatinib.html#dosage