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Tropomyosin receptor kinase / ROS1 inhibitor (specialist)

Entrectinib

Brand names: Rozlytrek

Entrectinib is an oral tyrosine kinase inhibitor used to treat NTRK fusion-positive solid tumours and ROS1-positive non-small-cell lung cancer.

Dosing — being independently re-sourced

ClinCalc Pro is rebuilding its dose data from primary open sources — the manufacturer SmPC (eMC), the WHO Model Formulary and other official references — under clinician review. This drug's structured dose is not yet published here. Confirm all doses against the product SmPC and your local formulary before prescribing.

Clinical monograph

How it works

It inhibits the tyrosine kinases encoded by NTRK1/2/3 and ROS1, blocking the oncogenic signalling produced by these gene fusions, and it crosses the blood-brain barrier giving activity against central nervous system disease.

Prescribing in practice

  • It is used only where an NTRK gene fusion or ROS1 rearrangement has been confirmed by validated testing.
  • Recognised adverse effects include congestive heart failure, QT prolongation, cognitive and neurological effects, and fractures, which require monitoring.
  • Exposure is affected by CYP3A4 inhibitors and inducers, so concomitant medicines should be checked against the SPC.

Monitoring

Monitor cardiac function, ECG for QT interval, and neurological status, and assess for confirmed NTRK or ROS1 alterations before starting.

Counselling the patient

  • Do not drive if you feel dizzy or your concentration is affected.
  • Tell your team about all other medicines and avoid grapefruit, which can affect drug levels.

Evidence & guidelines

Entrectinib is supported by trial evidence in NTRK fusion-positive tumours and ROS1-positive lung cancer and is appraised by NICE within licensed indications.

Reference: NICE TA644; ESMO; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.

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