selpercatinib at a glance
Medicine class
Selective RET receptor tyrosine kinase inhibitor
Main uses
Selected advanced RET-altered non-small-cell lung and thyroid cancers
Testing required
A validated tumour test must confirm a qualifying RET fusion or mutation before treatment
Administration
Swallow tablets or capsules whole; do not crush, chew or split them
What is selpercatinib used for?
Licensed uses represented by the selected products are:
Adults with advanced RET fusion-positive non-small-cell lung cancer who have not previously received a RET inhibitor.
Adults and adolescents aged 12 years and over with advanced RET fusion-positive thyroid cancer that is refractory to radioactive iodine, when radioactive iodine is appropriate.
Adults and adolescents aged 12 years and over with advanced RET-mutant medullary thyroid cancer.
How does selpercatinib work?
RET is a receptor tyrosine kinase involved in cell growth. Certain gene fusions or mutations keep RET signalling switched on. Selpercatinib selectively inhibits this abnormal signalling, helping to slow cancer-cell growth.
selpercatinib preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg, 80 mg
How to take selpercatinib
Take selpercatinib exactly as directed by the specialist cancer team. It can usually be taken with or without food, but must be taken with a meal when used with a proton-pump inhibitor. Swallow tablets or capsules whole with water; do not crush, chew or split them. If a larger tablet is difficult to swallow, ask whether the prescribed amount can be supplied using smaller tablets.
Tell the cancer team about acid-reducing treatments because food requirements or medicine timing may need changing.
Do not stop treatment or alter the prescribed amount without advice from the cancer team.
selpercatinib side effects
Common or expected effects
- Diarrhoea, constipation, nausea or vomiting
- Tiredness, headache or dizziness
- Dry mouth, reduced appetite or abdominal pain
- Swelling caused by fluid retention
- Rash or mouth inflammation
- High blood pressure
- Changes in liver, kidney, thyroid, blood-cell or electrolyte test results
Get urgent medical advice
- Severe skin reaction, including blistering, peeling or mucosal sores
- New or worsening breathlessness, cough and fever suggesting pneumonitis
- Liver injury, including jaundice, dark urine or right-sided upper abdominal pain
- Severe or persistent bleeding
- Allergic reaction with fever, rash and muscle or joint pain
- Abnormal heart rhythm associated with QT prolongation
- Tumour lysis syndrome, which can cause kidney problems or abnormal heart rhythms
selpercatinib in pregnancy
Selpercatinib is not recommended during pregnancy because animal studies indicate potential fetal harm and human data are unavailable. Pregnancy plans or a suspected pregnancy require prompt discussion with the oncology team. Effective contraception is required during treatment and for at least one week after the final dose; this applies to patients who could become pregnant and to men with partners who could become pregnant.
selpercatinib while breastfeeding
Breastfeeding should stop during selpercatinib treatment and for at least one week after the final dose. It is unknown whether selpercatinib enters human milk, and harm to a breastfed child cannot be excluded.
selpercatinib interactions
The oncology team should review prescription medicines, over-the-counter products and herbal remedies before and during treatment.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John’s wort
Can substantially lower selpercatinib exposure and reduce its effectiveness, so concurrent use should be avoided.
Strong CYP3A or P-glycoprotein inhibitors, including itraconazole, voriconazole, posaconazole and ritonavir
Can increase selpercatinib exposure and toxicity, requiring specialist review and possible treatment adjustment.
Proton-pump inhibitors, such as omeprazole
Reduce absorption when selpercatinib is taken fasting; selpercatinib must be taken with a meal if both are required.
Common questions about selpercatinib
Answers are fully visible for fast scanning and source review.
Why is RET testing needed before selpercatinib?
Selpercatinib targets cancers driven by particular RET fusions or mutations. Testing confirms whether the tumour has an alteration covered by the licensed indications.
Can selpercatinib be taken with food?
Yes, it can usually be taken with or without food. It must be taken with a meal if a proton-pump inhibitor is also being used.
Can selpercatinib tablets be crushed or split?
No. Tablets should be swallowed whole; do not crush, chew or split them.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.