Is entrectinib effective against brain metastases?

Enrectinib is effective against brain metastases, especially for metastatic ROS1-positive non-small cell lung cancer brain metastases and NTRK gene fusion-positive solid tumor brain metastases. It should be noted that because the condition of brain metastasis is relatively complex and each patient's situation is different, whether entrectinib is effective for a certain case of brain metastasis needs to be determined based on the patient's specific situation and the doctor's evaluation.

About entrectinib

, trade name Rozlytrek, is an anti-cancer drug used to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. Entrectinib is a selective tyrosine kinase inhibitor (TKI) of tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK).

Indications

In the United States, entrectinib is suitable for the treatment of ROS1-positive cancer patients (with specific genetic characteristics (biomarkers)), and is suitable for patients with the following solid tumors:

1. Caused by certain abnormal neurotrophic tyrosine receptor kinase (NTRK) genes.

2. Surgery for cancer that has spread or removed may cause serious complications.

3. There is no acceptable treatment, or the cancer grows or spreads during other treatments.

Enrectinib is not approved for use in children under twelve years of age.

In the EU, entrectinib is indicated as monotherapy for the treatment of adults and adolescents 12 years and older with solid tumors that express neurotrophic tyrosine receptor kinase (NTRK) gene fusions.

1. Suffering from locally advanced, metastatic or disease that may result in serious morbidity if surgical resection.

2. Patients who have not received NTRK inhibitors before.

3. Patients without satisfactory treatment options.

4. It is also suitable for the treatment of adult patients with ROS1-positive advanced non-small cell lung cancer (NSCLC) who have not previously received ROS1 inhibitor treatment.

The effect of entrectinib on brain metastases

In heterosexual clinical studies, the intracranial objective response rate (ORR) of entrectinib in patients with brain metastases was 54.5%, and more than 1/4 of the patients achieved complete response (CR). In addition, for patients without CNS (central nervous system) metastasis at baseline, there was 100% no CNS progression during entrectinib treatment, showing potential CNS protective effects.

The intracranial efficacy of entrectinib has been confirmed in multiple clinical studies, especially in patients with ROS1 fusion-positive non-small cell lung cancer (NSCLC). Entrectinib is not only effective in patients who have developed CNS metastasis, but can also provide potential CNS protection for patients without CNS metastasis and reduce the risk of CNS progression.

The above data show that entrectinib is not only effective against primary tumors, but also has a good therapeutic effect on brain metastases, making entrectinib an important choice for the treatment of patients with NTRK fusion-positive solid tumors and ROS1-positive NSCLC, especially in the fight against brain metastases. However, the specific therapeutic effect may vary due to individual differences.

Dosage regimen of entrectinib

Entrectinib is available in the form of capsules, suspensions, or oral pills. Usually taken once daily with food or on an empty stomach.

For patients who are unable to swallow the capsule or require administration via a gastric or nasogastric tube, the capsule may be swallowed whole or administered as a prepared oral suspension. If the capsules are to be taken as an oral suspension, open the correct number of capsules and pour the contents into room temperature drinking water or milk according to the prescription directions, allowing the suspension to sit for 15 minutes before taking and then adding the prescribed amount of water.

If the suspension cannot be taken immediately, it can be kept at room temperature for up to 2 hours. Throw it away if it exceeds 2 hours. Granules can be placed on one or more spoonfuls of soft food (such as applesauce, pudding, yogurt) and taken within 20 minutes of placing on the food, followed by water. Be sure to use the entire package of granules and do not use them to form a suspension or to administer via a gastric or nasogastric tube.

Take entrectinib at about the same time each day, carefully following the directions on your prescription label or as directed by your doctor. Do not take more, less, or more often than prescribed by your doctor.

What to do if you forget to take a dose

If you miss a dose by less than 12 hours, take the missed dose as soon as you remember and then take the next dose at the scheduled time. But if you miss a dose by more than 12 hours, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for the missed dose.

Summary

Entrectinib is not only effective against primary tumors, but also has a good therapeutic effect on brain metastases, making entrectinib an important choice for the treatment of patients with NTRK fusion-positive solid tumors and ROS1-positive NSCLC, especially in the fight against brain metastases. Patients should be treated with entrectinib under the guidance of a doctor and monitored regularly according to the doctor's recommendations.

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