Pralsetinib

FDA label

Read the full label on DailyMed ↗

Renal Undefined

Hepatic No adjustment needed

Instructions

• Confirm RET gene fusion before treatment
• Take on an empty stomach: no food ≥2 h before and ≥1 h after dose
• Missed dose: take same day, resume schedule next day; if vomiting after a dose, do not re-dose — take next scheduled dose
• Toxicity dose reductions: 300 → 200 → 100 mg QD; discontinue if 100 mg QD not tolerated
• Avoid CYP3A and/or P-gp inhibitors; if unavoidable reduce dose per label (e.g., 400→200 mg QD with combined P-gp + strong CYP3A inhibitor; 400→300 mg QD with strong/moderate CYP3A or P-gp inhibitor), resume prior dose 3-5 half-lives after inhibitor stops
• Avoid strong/moderate CYP3A inducers; if unavoidable increase dose from Day 7 of coadministration (e.g., 400→800 mg QD strong; 400→600 mg QD moderate), resume prior dose ≥14 days after inducer stops
• Hold ≥5 days before elective surgery; do not give for ≥2 weeks after major surgery and until adequate wound healing

Available strengths

• cap 100 mg

Cautions

• Serious/opportunistic infections (boxed) — infections in 72% (7% fatal) in AcceleRET-Lung; monitor and treat; withhold/reduce/discontinue by severity
• ILD/pneumonitis (12%, can be fatal) — withhold and investigate new/worsening respiratory symptoms; permanently discontinue if recurrent or Grade 3-4
• Hypertension (35%; Grade 3 in 18%) — do not initiate with uncontrolled BP; optimize BP first; monitor at 1 week then at least monthly
• Hepatotoxicity — monitor AST/ALT at baseline, q2 weeks x3 months, then monthly
• Hemorrhagic events (Grade ≥3 in 4.1%) — permanently discontinue for severe/life-threatening hemorrhage
• Tumor lysis syndrome (reported in MTC) — monitor at-risk patients; consider hydration/prophylaxis
• Impaired wound healing (VEGF-pathway effect)
• Embryo-fetal toxicity — effective NON-hormonal contraception (may render hormonal contraceptives ineffective)
• Adolescents: monitor open growth plates; consider interruption/discontinuation for abnormalities

Adverse reactions

• Musculoskeletal pain
• Constipation
• Hypertension
• Diarrhea
• Fatigue
• Edema
• Pyrexia
• Cough
• Grade 3-4 labs: lymphopenia, neutropenia, anemia, thrombocytopenia, leukopenia; low phosphate/sodium/calcium/potassium; high AST/ALT/ALP/bilirubin/potassium

Pregnancy Can cause fetal harm (animal malformations/embryolethality below human exposure); verify pregnancy status before starting; non-hormonal contraception during and 2 weeks after (females); males with partners of reproductive potential: contraception during and 1 week after; may impair fertility

Lactation Do not breastfeed during treatment and for 1 week after last dose