Pralsetinib

GAVRETO

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Pronunciation: pral-SE-ti-nib (gav-RE-toe)

Pralsetinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Pralsetinib ballicule

What it isAn oral selective RET receptor tyrosine kinase inhibitor active against oncogenic RET fusions and mutations.

Why this oneTreats RET fusion-positive non-small cell lung cancer and RET-altered thyroid cancers, giving high response rates in a molecularly defined niche.

What limits itA boxed warning for serious and opportunistic infections, plus interstitial lung disease/pneumonitis, hypertension, and hemorrhage, constrain its use.

Pralsetinib molecular structure (skeletal formula) — Molecular structure: Pralsetinib

Pralsetinib prescription history

Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Pralsetinib enters in 2020 (estimated).

Principal riskBoxed warning: increased risk of serious bacterial, fungal, viral, and opportunistic infections that can lead to hospitalization or death (added 12/2025).

Classes and tags

QT-prolonging medications

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades1 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Serious infections, including opportunistic infections — can lead to hospitalization or death; withhold, reduce dose, or permanently discontinue based on severity

FDA dosing	Population	Start	Target	Max
RET fusion-positive NSCLC (metastatic)	Adults	400 mg QD	400 mg QD until progression/unacceptable toxicity	400 mg QD
RET fusion-positive thyroid cancer	Adults and peds ≥12 yrs	400 mg QD	400 mg QD until progression/unacceptable toxicity	400 mg QD

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

Cost

Pralsetinib (GAVRETO)

Strength		#/mo	generic $/mo	CostPlus
100 mg	cap	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Pralsetinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2039 est.

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Self-check

Pralsetinib: Which kinase does it selectively inhibit?
RET.
Pralsetinib: What infection risk carries a boxed warning?
Serious and opportunistic infections.