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Entrectinib is available as a 100 mg and 200 mg oral capsule and 50 mg per packet of pellets.

Entrectinib is a tyrosine kinase inhibitor that is used to treat:
Metastatic non-small cell lung cancer (NSCLC) with ROS1 gene changes Advanced and metastatic cancers with NTRK gene changes, when prior treatment hasn’t worked and no other treatment is available

Certain types of cancer have changes in the NTRK and ROS1 genes. These changes result in abnormal proteins called NTRK fusions and ROS1 fusions that can send signals for tumors to grow. Entrectinib works by attaching to these abnormal proteins and blocking the tumors from growing and spreading.

Entrectinib is typically dosed as follows: NSCLC with ROS1 mutations Adults: The typical dose is 600 mg by mouth once a day.

Cancers with NTRK gene changes

• Adults: The typical dose is 600 mg by mouth once a day
• Children (ages 12 years and older): Your child’s provider will calculate the dose based on your child’s body surface area (BSA), which takes into account their height and weight. The typical dose ranges between 400 mg to 600 mg by mouth once a day

Entrectinib is a safe and effective treatment when used for FDA licensed indications. However, like all medications, they may give you unwanted side effects. You should always discuss potential side effects with your physician to ensure the medication is suitable and right for you.

Common side effects of Entrectinib:

• Lower blood cell counts
• Feeling very tired
• Constipation
• Changes in taste
• Swelling
• Dizziness
• Diarrhea
• Nausea
• Feeling numbness, pain, or tingling
• Trouble catching your breath

Serious side effects are rare with Entrectinib. Contact your healthcare provider immediately if you experience any of the following.

• Hallucinations and confusion
• Depression and thoughts of self-harm
• Serious eye problems: changes in vision, blurry vision
• Heart problems: feeling lightheaded, trouble catching your breath, racing heartbeat, swelling in the legs
• Broken bones: muscle or bone pain, changes in mobility
• Serious liver injury: pain in the right side of the stomach, yellowing of the eyes or skin, dark or brown urine

The following medications may interact with Entrectinib:

• Moderate and Strong CYP3A Inhibitors: For adult and pediatric patients 2 years and older, reduce the dose of
• Entrectinib if coadministration of moderate or strong CYP3A inhibitors cannot be avoided. For pediatric patients less than 2 years, avoid coadministration with Entrectinib
• Moderate and Strong CYP3A Inducers: Avoid coadministration with Entrectinib
• Drugs That Prolong QTc Interval: Avoid concomitant use with Entrectinib

Various FDA-approved generic manufacturers

Entrectinib can cause harm to your unborn baby. Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with Entrectinib. Females who can become pregnant: Your healthcare provider will do a pregnancy test before you start treatment with Entrectinib. Use effective birth control (contraception) during treatment with Entrectinib and for at least 5 weeks after the last dose. Males with female partners that can become pregnant: Use effective birth control (contraception) during treatment with Entrectinib and for 3 months after the last dose.

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