Pralsetinib (pralsetinib)

Pralsetinib is approved for: Adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test (regular approval granted 9 Aug 2023); Adult and pediatric patients 12 years of age and older with advanced or metastatic RET fusion-positive thyroid cancer who require systemic therapy and who are radioactive iodine-refractory (if radioactive iodine is appropriate) (accelerated approval); Note: the RET-mutant medullary thyroid cancer (MTC) indication was removed from the US label in July 2023. It is a pralsetinib (Oral selective RET receptor tyrosine kinase inhibitor), originally marketed as Gavreto (US/EU); 普吉华 in China by Discovered by Blueprint Medicines; co-commercialised with Genentech (Roche) in the US and by Roche ex-US; Blueprint regained global rights (excluding Greater China) in 2023.

Standard dosing for pralsetinib: 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after the dose), continued until disease progression or unacceptable toxicity. Available strength: 100 mg capsules. Dose adjustments: Adverse-reaction dose reductions: 300 mg once daily, then 200 mg, then 100 mg once daily; permanently discontinue if 100 mg once daily is not tolerated. With a combined P-gp and strong CYP3A inhibitor: 400 mg -> 200 mg once daily. With a strong CYP3A inhibitor, moderate CYP3A inhibitor, P-gp inhibitor, or combined P-gp + moderate CYP3A inhibitor: 400 mg -> 300 mg once daily. With a strong CYP3A inducer: increase starting dose from 400 mg -> 800 mg once daily (from Day 7 of coadministration); with a moderate CYP3A inducer: 400 mg -> 600 mg once daily. Confirmed grade 3-4 or recurrent ILD/pneumonitis: permanently discontinue. Grade 4 hypertension: discontinue.

No FDA- or EMA-approved generic (ANDA/abbreviated) pralsetinib was identified. The Lao-made 'generic' LuciPral is a nationally registered copy (Lao MOH registration no. 08 L 1007/23) and is not an FDA/EMA-approved product. No published bioequivalence study against Gavreto was found in this search. Originator patents/use exclusivities remain in force in Western markets; Lao copies are marketed only under Lao domestic registration. Manufacturers supplying pralsetinib generic versions include Lucius Pharmaceuticals. Brands registered in Bangladesh include not in the MedEx registry.

No FDA- or EMA-approved generic (ANDA/abbreviated) pralsetinib was identified. The Lao-made 'generic' LuciPral is a nationally registered copy (Lao MOH registration no. 08 L 1007/23) and is not an FDA/EMA-approved product. No published bioequivalence study against Gavreto was found in this search. Originator patents/use exclusivities remain in force in Western markets; Lao copies are marketed only under Lao domestic registration. Manufacturers supplying pralsetinib generic versions include Lucius Pharmaceuticals. Brands registered in Bangladesh include not in the MedEx registry.

The most frequently reported side effects of pralsetinib are musculoskeletal pain (>=25%), constipation, hypertension (35% overall, 18% grade 3), diarrhoea, fatigue, oedema, pyrexia. Serious but less common reactions include interstitial lung disease / pneumonitis (12%, 3.3% grade 3-4, 0.2% fatal), hepatotoxicity (increased ast 49%, alt 37%), tumour lysis syndrome. Routine monitoring: Blood pressure: after 1 week, at least monthly thereafter and as clinically indicated; do not start in uncontrolled hypertension; Liver function (AST, ALT) before starting, every 2 weeks for the first 3 months, then monthly and as clinically indicated; Pulmonary symptoms for ILD/pneumonitis (dyspnoea, cough, fever). Report any new or worsening symptom to your treating physician — most adverse effects are managed by dose reduction rather than stopping treatment.

Pralsetinib (Oral selective RET receptor tyrosine kinase inhibitor (small molecule), originally Gavreto (US/EU); 普吉华 in China by Discovered by Blueprint Medicines; co-commercialised with Genentech (Roche) in the US and by Roche ex-US; Blueprint regained global rights (excluding Greater China) in 2023) Pralsetinib blocks RET, a kinase protein that is switched on abnormally in some lung and thyroid cancers by RET gene fusions or mutations. When RET signalling is blocked, tumour cells stop receiving continuous growth signals and tumour growth is slowed or stopped. 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after the dose), continued until disease progression or unacceptable toxicity. Available strength: 100 mg capsules.

Elimination half-life: Mean plasma elimination half-life 15.7 hours (SD 9.8) after single doses and 20 hours (SD 11.7) after multiple doses; mean steady-state apparent oral clearance 10.9 L/h. Dosing intervals are designed around this, which is why most regimens are once or twice daily.

Pralsetinib (Oral selective RET receptor tyrosine kinase inhibitor (small molecule), originally Gavreto (US/EU); 普吉华 in China by Discovered by Blueprint Medicines; co-commercialised with Genentech (Roche) in the US and by Roche ex-US; Blueprint regained global rights (excluding Greater China) in 2023) Pralsetinib blocks RET, a kinase protein that is switched on abnormally in some lung and thyroid cancers by RET gene fusions or mutations. When RET signalling is blocked, tumour cells stop receiving continuous growth signals and tumour growth is slowed or stopped. 400 mg orally once daily on an empty stomach (no food intake for at least 2 hours before and at least 1 hour after the dose), continued until disease progression or unacceptable toxicity. Available strength: 100 mg capsules.

Storage: Store at 20-25 C (68-77 F); excursions permitted between 15 and 30 C (59-86 F); protect from moisture Keep the product in its original packaging and check the expiry date printed on the pack.

Bangladesh unit prices for pralsetinib are not published per unit; the registry lists pack prices only. Prices move with pack size, pharmacy and the exchange rate — confirm current stock and price with a licensed importer before ordering.