entrectinib at a glance
Medicine class
Targeted protein kinase inhibitor.
Main uses
Selected NTRK fusion-positive solid tumours and ROS1-positive advanced non-small-cell lung cancer.
Genetic testing
NTRK or ROS1 status must be confirmed using a validated test before treatment.
Administration
Swallow capsules whole, with or without food; avoid grapefruit and Seville oranges.
What is entrectinib used for?
UK-licensed uses include:
Monotherapy for adults and young people aged 12 years or over with an NTRK fusion-positive solid tumour that is locally advanced, metastatic or unsuitable for surgery because resection is likely to cause severe morbidity. They must not have received an NTRK inhibitor and must have no satisfactory treatment options.
Monotherapy for adults with ROS1-positive advanced non-small-cell lung cancer who have not previously received a ROS1 inhibitor.
How does entrectinib work?
NTRK and ROS1 gene fusions can produce continuously active kinase proteins that drive cancer-cell growth. Entrectinib inhibits TRKA, TRKB, TRKC and ROS1 signalling; its active metabolite M5 has similar activity.
entrectinib preparations and strengths
Capsule
Route: Oral
Strengths: 100 mg, 200 mg
How to take entrectinib
Follow the specialist team's instructions. The capsules may be taken with or without food.
Swallow each capsule whole.
Do not crush, chew, open or dissolve capsules; their contents are very bitter.
Avoid grapefruit, grapefruit juice, grapefruit products and Seville oranges.
entrectinib side effects
Common or expected effects
- Tiredness
- Constipation or diarrhoea
- Dizziness, unsteadiness or altered coordination
- Changes in taste
- Swelling or weight gain
- Nausea or vomiting
- Tingling, burning or altered sensation
- Headache, muscle, joint or other pain
- Blurred vision
- Changes in memory, attention or thinking
- Anaemia, neutropenia or altered liver and kidney blood-test results
Get urgent medical advice
- Breathlessness, cough or limb swelling suggesting heart failure
- Fast or irregular heartbeat, severe light-headedness or fainting
- Significant confusion, memory change, mood change or hallucinations
- New bone or joint pain, deformity, abnormal walking or reduced mobility suggesting a fracture
- Kidney symptoms or acute joint inflammation associated with high uric acid
- Fever or other features of a serious infection
- Rapid deterioration or reduced urine output that could indicate tumour lysis syndrome
entrectinib in pregnancy
Entrectinib is not recommended during pregnancy because animal evidence and its mechanism indicate potential fetal harm. Pregnancy testing is advised before treatment where relevant. Highly effective contraception is required during treatment and for at least 5 weeks afterwards for patients who could become pregnant, and for at least 3 months afterwards for male patients with a partner who could become pregnant. Because hormonal contraception may be less reliable, an additional barrier method is advised.
entrectinib while breastfeeding
It is unknown whether entrectinib or its metabolites enter human milk, and risk to a breastfed child cannot be excluded. Breastfeeding should be stopped during treatment; discuss feeding options with the oncology and maternity teams.
entrectinib interactions
The oncology team should review prescription, over-the-counter and herbal products before treatment and whenever they change.
Strong or moderate CYP3A inhibitors, including itraconazole, voriconazole, posaconazole, ketoconazole and some antiviral medicines
These can substantially increase entrectinib exposure and adverse effects, so combined use should usually be avoided.
CYP3A or P-glycoprotein inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort
These can lower entrectinib exposure and reduce its anticancer effect, so combined use should be avoided.
Grapefruit products and Seville oranges
These may raise entrectinib concentrations and should be avoided.
Common questions about entrectinib
Answers are fully visible for fast scanning and source review.
Is entrectinib chemotherapy?
No. It is a targeted protein kinase inhibitor that blocks signalling from certain abnormal NTRK or ROS1 fusion proteins.
What cancers can entrectinib treat?
Its UK licence covers selected NTRK fusion-positive solid tumours in adults and young people aged 12 years or over, and ROS1-positive advanced non-small-cell lung cancer in adults.
Do I need a genetic test before taking entrectinib?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.