pralsetinib at a glance
Medicine class
Selective RET protein kinase inhibitor
Licensed role
Monotherapy for adults with RET fusion-positive advanced non-small cell lung cancer not previously treated with a RET inhibitor
How it is taken
Capsules are swallowed whole with water on an empty stomach
Additional monitoring
Suspected adverse reactions should be reported through the MHRA Yellow Card scheme
What is pralsetinib used for?
UK-licensed use represented by the selected product:
Treatment on its own for adults with RET fusion-positive advanced non-small cell lung cancer not previously treated with a RET inhibitor. A validated test must confirm the RET fusion.
How does pralsetinib work?
RET fusion genes can produce an abnormal signalling protein that drives cancer-cell growth. Pralsetinib selectively inhibits this RET kinase signal, which may slow tumour growth or cause the tumour to shrink.
How to take pralsetinib
Follow the cancer team's prescription and do not change or stop treatment without their advice.
Swallow capsules whole with a glass of water.
Take on an empty stomach: do not eat for at least 2 hours beforehand or 1 hour afterwards.
Avoid grapefruit, grapefruit juice and Seville oranges.
If vomiting occurs after taking pralsetinib, do not take an extra dose.
Keep capsules in their original packaging to protect them from moisture.
pralsetinib side effects
Common or expected effects
- Anaemia and reduced white blood cells or platelets
- Constipation, diarrhoea, nausea or abdominal discomfort
- Tiredness
- Muscle, joint or bone pain
- Raised blood pressure
- Cough or breathlessness
- Swelling
- Headache or altered taste
- Rash
- Changes in liver, kidney, mineral or muscle-enzyme blood tests
Get urgent medical advice
- New or worsening breathing symptoms suggesting pneumonitis or interstitial lung disease
- Pneumonia or another serious infection
- Severe or persistent hypertension
- Liver injury
- Significant bleeding
- Abnormal heart rhythm associated with QT prolongation
- Tuberculosis
pralsetinib in pregnancy
Pralsetinib may harm an unborn baby and should generally be avoided during pregnancy unless specialist assessment finds treatment clinically necessary. Pregnancy status should be checked before treatment. Highly effective non-hormonal contraception is required because pralsetinib may reduce hormonal contraceptive effectiveness; the oncology team should advise on contraception and fertility preservation.
pralsetinib while breastfeeding
It is unknown whether pralsetinib enters human milk, and risk to a breastfed child cannot be excluded. Breastfeeding should stop during treatment and for 1 week after the final dose; discuss alternative feeding with the specialist team.
pralsetinib interactions
The cancer team or pharmacist should review prescription, non-prescription and herbal products before treatment.
Strong CYP3A4 or combined CYP3A4/P-gp inhibitors, including itraconazole, voriconazole, posaconazole, ketoconazole, ritonavir and saquinavir
May increase pralsetinib exposure and the risk or severity of adverse effects; combination should generally be avoided.
Strong CYP3A4 inducers, including rifampicin, rifabutin, carbamazepine, phenytoin, phenobarbital and St John's wort
May lower pralsetinib exposure and reduce its effect; combination should generally be avoided.
Grapefruit and Seville oranges
May increase pralsetinib exposure and should be avoided.
Common questions about pralsetinib
Answers are fully visible for fast scanning and source review.
Why is RET testing needed before pralsetinib treatment?
Pralsetinib targets abnormal RET fusion proteins, so a validated test is needed to confirm that the cancer has the alteration the treatment is designed to inhibit.
Can pralsetinib be taken with food?
No. Swallow the capsules with water on an empty stomach, avoiding food for at least 2 hours beforehand and 1 hour afterwards.
What should I do if I vomit after taking pralsetinib?
Do not take an extra dose. Continue with the next prescribed dose.
Can I drink grapefruit juice while taking pralsetinib?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.