What it does
Pralsetinib is a medication used to treat certain types of cancer by targeting specific genetic changes in cancer cells.
Commonly used for: lung cancer (non-small cell lung cancer), thyroid cancer (RET fusion-positive thyroid cancer)
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
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Sourcing - Kenya onlyRegistration & product details
Source: Zambia Medicines Regulatory Authority · fetched 2026-03-12 00:02:57 · updated 2026-10-19 03:34:45
Drug Interactions
17Severe (4)
Ciclosporin - affects exposure
Pralsetinibmightaffecttheexposuretociclosporin.Avoid. oTheoretical
Pralsetinib - increases exposure
Grapefruit juice is predicted to increase the exposure to pralsetinib. Avoid.
Pralsetinib - increases exposure
Triamterene potentially increases the clearance of lithium. Pralsetinib FOOD AND LIFESTYLE Bitter (Seville) orange is predicted to increase the exposure to pralsetinib. Avoid.
Warfarin - affects exposure
Pralsetinibmightaffecttheexposuretowarfarin.Avoid. oTheoretical
Moderate (9)
Pralsetinib - increases exposure
Posaconazole is predicted to increase the exposure to pralsetinib. Avoid or adjust dose-consult product literature.
Pralsetinib - increases exposure
Cobicistatispredictedtoincreasetheexposuretopralsetinib. AvoidoradjustdosewithpotentCYP3A4inhibitors-consult productliterature.oStudy https://www.facebook.c (Books-Courses-Medic
Pralsetinib - increases exposure
Idelalisib is predicted to increase the exposure to pralsetinib. Avoid or adjust dose with potent CYP3A4 inhibitors-consult product literature.
Pralsetinib - increases exposure
Clarithromycin is predicted to increase the exposure to pralsetinib. Avoid or adjust dose with potent CYP3A4 inhibitors-consult product literature.
Pralsetinib - decreases exposure
Mitotane is predicted to decrease the exposure to pralsetinib. Avoid or adjust dose with potent CYP3A4 inducers-consult product literature.
Pralsetinib - decreases exposure
Rifamycins (rifabutin) are predicted to decrease the exposure to pralsetinib. Avoid or adjust dose-consult product literature.
Pralsetinib - decreases exposure
St John’s wort is predicted to decrease the exposure to pralsetinib. Avoid or adjust dose-consult product literature.
Pralsetinib - decreases exposure
Rifabutin is predicted to decrease the exposure to pralsetinib. Avoid or adjust dose-consult product literature.
Pralsetinib - decreases exposure
Rifampicin is predicted to decrease the exposure to pralsetinib. Avoid or adjust dose with potent CYP3A4 inducers-consult product literature.
Unknown (4)
Combined Hormonal Contraceptives - decreases efficacy
Pralsetinib might decrease the efficacy of combined hormonal contraceptives. Avoid or use additional contraceptive precautions.
Coumarins - affects exposure
Pralsetinibmightaffecttheexposuretocoumarins(warfarin). Avoid.oTheoretical
Paclitaxel - affects exposure
Pralsetinib might affect the exposure to taxanes (paclitaxel). Avoid. Theoretical Pramipexole → see dopamine receptor agonists Prasugrel → see TABLE 4 p. 1517 (antiplatelet effects)
Taxanes - affects exposure
Pralsetinib might affect the exposure to taxanes (paclitaxel). Avoid. Theoretical Pramipexole → see dopamine receptor agonists Prasugrel → see TABLE 4 p. 1517 (antiplatelet effects)
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Pralsetinib is a medication used to treat certain types of cancer by targeting specific genetic changes in cancer cells.
What it treats
- lung cancer (non-small cell lung cancer)
- thyroid cancer (RET fusion-positive thyroid cancer)
How it works
It works by blocking signals that help cancer cells grow and survive.
Who it's for
This medicine is for adults with specific types of cancer that have a certain genetic change.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Pralsetinib
BNF-referencedPralsetinib is a targeted therapy that acts as a selective inhibitor of rearranged during transfection (RET) fusion proteins. It is primarily utilized in the treatment of specific malignancies characterized by RET alterations, including non-small cell lung cancer (NSCLC) and other advanced solid tumors. Pralsetinib is designed to inhibit the activity of the RET tyrosine kinase, thereby interfering with tumor cell proliferation and survival.
Indications
- Non-small cell lung cancer (NSCLC) with RET fusions
- Other advanced solid tumors with RET alterations
Dosage
Children: There is no established pediatric dosing information for pralsetinib; refer to the BNF for Children for guidance.
Adults: The recommended dose for adults is 400 mg taken orally once daily. It should be administered with or without food.
Mechanism of action
Pralsetinib selectively inhibits the activity of RET fusion proteins, leading to reduced signaling through the RET pathway, which is implicated in tumorigenesis. This inhibition causes a decrease in cell proliferation and induces apoptosis in cancer cells that express RET fusions.
Pharmacodynamics
The pharmacodynamics of pralsetinib involve its ability to inhibit RET kinase activity, leading to decreased phosphorylated ret signaling pathways. This results in the inhibition of downstream survival and proliferation signals in tumor cells, ultimately contributing to tumor shrinkage and improved clinical outcomes in patients with RET-driven malignancies.
Pharmacokinetics
Pralsetinib exhibits a bioavailability of approximately 80% when administered orally. It is highly protein-bound (>99%) and primarily metabolized by CYP3A4 enzymes in the liver. The drug has a half-life of about 13 hours, allowing for once-daily dosing. Elimination occurs mainly through feces, and renal clearance is not a significant pathway due to high protein binding.
Contra-indications
- Uncontrolled hypertension
- Cardiomyopathy
- Cardiac arrhythmias
- Susceptibility to thrombosis
Adverse effects
- Anaemia
- Aplastic anaemia
- Arthralgia
- Asthenia
- Constipation
- Cough
- Diarrhoea
- Dizziness
- Dry mouth
- Dyspnoea
- Electrolyte imbalance
- Facial swelling
- Fever
- Gastrointestinal discomfort
- Headaches
- Hypertension
- Nausea
- Oedema
- Pain
- QT interval prolongation
- Vomiting
Interactions
- Pralsetinib + ciclosporin: Severe (affects exposure)
- Pralsetinib + warfarin: Severe (affects exposure)
- Grapefruit juice + pralsetinib: Severe (increases exposure)
- Triamterene + pralsetinib: Severe (increases exposure)
- Posaconazole + pralsetinib: Moderate (increases exposure)
- Cobicistat + pralsetinib: Moderate (increases exposure)
- Idelalisib + pralsetinib: Moderate (increases exposure)
- Clarithromycin + pralsetinib: Moderate (increases exposure)
- Mitotane + pralsetinib: Moderate (decreases exposure)
- Rifamycins + pralsetinib: Moderate (decreases exposure)
Precautions
- Monitor serum lipase every 2 weeks for the first 2 months and periodically thereafter
- Full blood count every 2 weeks
- Caution in hepatic impairment
- Caution in renal impairment if creatinine clearance < 50 mL/min
Pregnancy
Avoid - toxicity in animal studies.
Breast-feeding
Use with caution, effects not known.
Storage
Store at room temperature, protect from moisture.
Formulations
- Tablets
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Pralsetinib
PubChem CID 129073603Molecular formula: C27H32FN9O2
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.