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Selective RET kinase inhibitor Pregnancy: Retsevmo is not recommended during pregnancy or in women of childbearing potential not using contraception, and should only be used during pregnancy if the potential benefit justifies the potential risk to the foetus. There are no available data in pregnant women; animal studies have shown reproductive toxicity. Women of childbearing potential must use highly effective contraception during treatment and for at least one week after the last dose; men with female partners of childbearing potential should use effective contraception for the same period. Breast-feeding should be discontinued during treatment and for at least one week after the last dose.

Selpercatinib (Specialist drug)

Brand names: Retsevmo

Selpercatinib is an oral selective RET kinase inhibitor used as a specialist treatment for RET-fusion-positive non-small-cell lung cancer and RET-altered thyroid cancers.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Dose is based on body weight: less than 50 kg — 120 mg twice daily; 50 kg or greater — 160 mg twice daily
Route: Oral — tablets swallowed whole (do not crush, chew or split), with or without food
Frequency: Twice daily at approximately the same time every day; continue until disease progression or unacceptable toxicity
Therapy should be initiated and supervised by physicians experienced in the use of anti-cancer therapies. The presence of a RET gene fusion (NSCLC and non-medullary thyroid cancer) or mutation (MTC) must be confirmed by a validated test prior to initiation. If a patient vomits or misses a dose, take the next dose at its scheduled time — do not take an additional dose. Reduce the current dose by 50% if co-administering with a strong CYP3A inhibitor; when the inhibitor is discontinued, increase back (after 3-5 half-lives of the inhibitor) to the pre-inhibitor dose. Retsevmo must be accompanied by a meal if used concomitantly with a proton pump inhibitor, and should be administered 2 hours before or 10 hours after H2 receptor antagonists. Dose reduction levels for adults and adolescents >= 50 kg: starting 160 mg twice daily, first reduction 120 mg twice daily, second 80 mg twice daily, third 40 mg twice daily. For adults and adolescents < 50 kg: starting 120 mg twice daily, first reduction 80 mg twice daily, second 40 mg twice daily, no third reduction. Grade 3/4 ALT or AST rise: suspend until resolved to baseline then resume reduced by 2 levels, escalating stepwise if tolerated; permanently discontinue if it recurs despite dose modification. Hypersensitivity (all grades): suspend until resolved and start corticosteroids at 1 mg/kg, resume at 40 mg twice daily while continuing steroids, then increase by 1 dose level each week; discontinue for recurrent hypersensitivity. Grade 3 QT prolongation: suspend for QTcF >500 ms until QTcF returns to <470 ms or baseline, resume at the next lower dose level; permanently discontinue for Grade 4, for uncontrolled QT prolongation after two dose reductions, or for signs/symptoms of serious arrhythmia. Grade 3 hypertension: control blood pressure before starting, suspend for medically significant hypertension until controlled, resume at the next lower dose; discontinue permanently (Grade 4) if it cannot be controlled. Grade 3 haemorrhage: suspend until recovery to baseline, resume reduced; discontinue for Grade 4 or recurrent Grade 3. Grade 2 ILD/pneumonitis: withhold until resolution then resume reduced; discontinue for Grade 3/4 or recurrent ILD. Other Grade 3/4 reactions: suspend until recovery to baseline then resume reduced. Hepatic impairment: no dose adjustment for mild (Child-Pugh A) or moderate (Child-Pugh B); severe (Child-Pugh C) should be dosed with 80 mg twice daily. PAEDIATRIC (non per-kg, so not given as a structured paediatric dose): Retsevmo should not be used in children aged less than 12 years. It is intended to be used from the age of 12 years for RET-mutant MTC and RET fusion-positive thyroid cancer, dosed according to the same body-weight bands as adults (<50 kg: 120 mg twice daily; >=50 kg: 160 mg twice daily). There are very limited data in children or adolescents aged less than 18 years and no data in children or adolescents with RET fusion-positive NSCLC. Open growth plates in adolescent patients should be monitored, and dose interruption or discontinuation considered based on the severity of any growth plate abnormalities and an individual risk-benefit assessment.

Dose adjustments

Renal

Dose adjustment is not necessary in patients with mild, moderate or severe renal impairment. There are no data in patients with end stage renal disease or in patients on dialysis.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance or to any of the excipients

Side effects

  • Hypertension (very common, including Grade >= 3)
  • Diarrhoea, nausea, vomiting and abdominal pain
  • Increased ALT/AST and electrocardiogram QT prolonged
  • Hypothyroidism
  • Haemorrhage
  • Also very common: urinary tract infections, pneumonia, decreased appetite, headache, dizziness, dry mouth, constipation, stomatitis, rash. Most common serious ADRs: pneumonia (5.3%), haemorrhage (2.4%), abdominal pain (2.1%). Interstitial lung disease/pneumonitis and chylothorax are common

Interactions

  • Strong CYP3A inhibitors — reduce the current selpercatinib dose by 50% during co-administration; increase back to the previous dose after 3-5 half-lives once the inhibitor is stopped (from eMC §4.2)
  • Proton pump inhibitors — Retsevmo must be accompanied by a meal if used concomitantly (from eMC §4.2)
  • H2 receptor antagonists — administer Retsevmo 2 hours before or 10 hours after (from eMC §4.2)
  • Medicinal products known to prolong the QT interval — monitor the QT interval with ECGs more frequently (from eMC §4.4)
  • Note: eMC section 4.5 (interactions) was not present in the fetched bundle — the above are drawn from the posology and warnings sections only; clinician to source the full §4.5 list

Clinical monograph

How it works

It selectively inhibits RET receptor tyrosine kinase signalling driven by RET gene fusions and activating point mutations, suppressing tumour growth.

Prescribing in practice

  • It can prolong the QT interval and cause hepatotoxicity and hypertension, so baseline and periodic ECG, liver function and blood pressure monitoring are required.
  • Patients must have a confirmed RET alteration by a validated test before treatment, which is restricted to specialist oncology services.
  • It is a CYP3A4 substrate with relevant interactions, so co-prescribed strong inhibitors and inducers should be reviewed per current prescribing references.

Monitoring

Monitor ECG (QTc), liver function tests and blood pressure before and during treatment.

Counselling the patient

  • Report fainting, palpitations, yellowing of the skin or severe headache.
  • Tell the team about all other medicines and avoid grapefruit.
  • Attend for regular blood pressure, blood test and ECG checks.

Evidence & guidelines

Use is supported by NICE guidance and the LIBRETTO-001 trial in RET-altered cancers.

Reference: NICE TA760/TA819; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.