Entrectinib
Non-Small-Cell Lung Carcinoma
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Drug Status
Government Approvals
US(FDA), UK(BNF)
WHO Essential Medicine
NO
Known Teratogen
No
Pharmaceutical Class
NA
Controlled Drug Substance
No
Entrectinib
Summary
Entrectinib is used to treat certain types of non-small cell lung cancer and solid tumors that have specific gene fusions. It can be used when the cancer has spread to other parts of the body or cannot be surgically removed.
Entrectinib works by inhibiting specific proteins, known as kinases, that are involved in the growth and spread of cancer cells. By blocking these proteins, it helps to slow or stop the growth of cancer cells.
For adults, the recommended dose of Entrectinib is 600 mg taken orally once daily. For children aged 12 years and older, the dose is based on body surface area, with 300 mg/m being the standard.
Common side effects of Entrectinib include fatigue, constipation, diarrhea, nausea, and dizziness. Serious adverse effects can include congestive heart failure, central nervous system effects, and QT interval prolongation.
Entrectinib can cause fetal harm when administered to pregnant women. Women of reproductive potential should use effective contraception during treatment and for at least 5 weeks after the last dose. It can also interact with CYP3A inhibitors and inducers, affecting its metabolism.
Indications and Purpose
How does Entrectinib work?
Entrectinib works by inhibiting specific proteins known as kinases, which are involved in the growth and spread of cancer cells. By blocking these proteins, Entrectinib helps to slow or stop the proliferation of cancer cells, making it an effective treatment for tumors with certain genetic mutations.
Is Entrectinib effective?
Entrectinib has been shown to be effective in treating certain types of non-small cell lung cancer and solid tumors with specific gene fusions. Clinical trials have demonstrated significant response rates and duration of response in patients with these conditions, supporting its use as a targeted cancer therapy.
What is Entrectinib?
Entrectinib is used to treat certain types of non-small cell lung cancer and solid tumors with specific gene fusions. It works by inhibiting the action of proteins that signal cancer cells to multiply, thereby slowing or stopping the spread of cancer. This targeted approach helps manage cancer more effectively in patients with these genetic markers.
Directions for Use
For how long do I take Entrectinib?
Entrectinib is typically used until disease progression or unacceptable toxicity occurs. The duration of use can vary significantly depending on the individual's response to treatment and the specific condition being treated.
How do I take Entrectinib?
Entrectinib can be taken with or without food, but patients should avoid grapefruit and grapefruit juice as they can affect the medication's metabolism. It's important to take the medication at the same time each day and follow the prescribed dosage instructions from your healthcare provider.
How long does it take for Entrectinib to start working?
The time it takes for Entrectinib to start working can vary depending on the individual and the condition being treated. Patients may begin to see improvements in symptoms or tumor response within a few weeks, but it's important to continue taking the medication as prescribed and attend regular follow-up appointments to monitor progress.
How should I store Entrectinib?
Entrectinib should be stored at room temperature, between 68°F to 77°F (20°C to 25°C), in its original container to protect from moisture. If prepared as a suspension, it should not be stored for more than 2 hours at room temperature and should be discarded if not used within this time.
What is the usual dose of Entrectinib?
For adults, the recommended dose of Entrectinib is 600 mg taken orally once daily. For pediatric patients aged 12 years and older, the dose is based on body surface area (BSA), with 300 mg/m² being the standard. Always follow your healthcare provider's instructions for dosing.
Warnings and Precautions
Can Entrectinib be taken safely while breastfeeding?
Women are advised not to breastfeed while taking Entrectinib and for 7 days after the last dose due to the potential for serious adverse reactions in breastfed children. It is unknown if Entrectinib is excreted in human milk, so caution is advised.
Can Entrectinib be taken safely while pregnant?
Entrectinib can cause fetal harm when administered to pregnant women. Women of reproductive potential should use effective contraception during treatment and for at least 5 weeks after the last dose. If pregnancy occurs, patients should inform their healthcare provider immediately. There is no strong evidence from human studies, but animal studies suggest potential risks.
Can I take Entrectinib with other prescription drugs?
Entrectinib interacts with CYP3A inhibitors and inducers, which can affect its metabolism. Strong CYP3A inhibitors can increase Entrectinib levels, leading to more side effects, while inducers can decrease its effectiveness. Patients should avoid grapefruit products and consult their healthcare provider about all medications they are taking.
Is Entrectinib safe for the elderly?
Elderly patients may experience more frequent side effects such as dizziness, increased blood creatinine, hypotension, and ataxia. It's important for elderly patients to be closely monitored by their healthcare provider while taking Entrectinib to manage any adverse effects effectively.
Is it safe to exercise while taking Entrectinib?
Entrectinib may cause fatigue, dizziness, and muscle pain, which could limit the ability to exercise. If you experience these symptoms, it's important to discuss them with your healthcare provider to determine the best course of action.
Who should avoid taking Entrectinib?
Key warnings for Entrectinib include the risk of congestive heart failure, central nervous system effects, skeletal fractures, hepatotoxicity, hyperuricemia, QT interval prolongation, and vision disorders. Patients should be monitored for these conditions, and the medication should be used with caution in those with pre-existing heart, liver, or vision problems.
