How effective is brigatinib in the brain?

The effect of brigatinib on entering the brain has been proven to be quite significant in clinical practice.

Brigatinib improves the penetration of the blood-brain barrier with its unique structural design. This property allows drugs to efficiently enter the brain and achieve the drug concentrations needed to treat brain diseases. By constantly adjusting the molecular structure, the brigatinib molecule has the characteristics of high solubility and high permeability, which creates favorable conditions for penetrating the blood-brain barrier and maintaining drug concentration in the brain.

Because brigatinib can effectively penetrate the blood-brain barrier, it has shown significant efficacy in treating tumors that metastasize to the brain. Especially in the treatment of patients with brain metastases from ALK positive non-small cell lung cancer (NSCLC), brigatinib has shown excellent results. According to clinical research data, brigatinib's intracranial response duration for people with baseline measurable brain metastases is as long as 27.9 months, and the intracranial lesion response rate is 78%. This data exceeds other similar drugs, such as crizotinib.

While showing strong brain penetration and efficacy, brigatinib also demonstrates good safety and tolerability. The adverse reactions are mainly grade 1~2, and grade 3 adverse reactions are mostly changes in laboratory or blood indicators, which are usually asymptomatic and do not affect the patient's disease management.

In addition to being excellent at treating brain tumors, brigatinib works by increasing levels of the important neurotransmitter dopamine in the brain. Dopamine is an important substance that controls attention, mood, and the reward system. Therefore, brigatinib not only helps improve patients' cognitive functions, such as attention and memory, but also improves emotional stability and reduces feelings of stress and anxiety.

References:

https://pmc.ncbi.nlm.nih.gov/articles/PMC10883856/