Drug reference

pralsetinib

Selective RET tyrosine kinase inhibitor (antineoplastic) · antineoplastic, targeted therapy

START

400 mg PO once daily on empty stomach

TYPICAL MAX

400 mg/day

STOP IF

Pneumonitis (any grade), severe HTN, severe haemorrhage, or hepatotoxicity

WATCH

BP, LFTs, CBC, pulmonary symptoms; pause >5 days before/after surgery

CDSCO approvedATC L01EX23

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · absorption
PEAK: 3h · Tmax
t½: 18h · t½
DURATION: 1d · once-daily

EXCRETION

Mainly faecal (~73%); ~6% renal

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Can cause fetal harm — avoid; effective contraception during and 2 weeks after.

FDA category + note

Top interactionssee all 12 →

AmprenavirSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
BoceprevirSevereDatabaseDDInter

Mechanism

Selective ATP-competitive inhibitor of RET (rearranged-during-transfection) tyrosine kinase, including fusion and mutant forms (M918T, etc.) — designed for RET-altered tumours with low off-target activity (less HTN/diarrhoea than older TKIs).

Indications

RET fusion-positive non-small-cell lung cancer (metastatic)RET-mutant medullary thyroid cancer (advanced/metastatic)RET fusion-positive thyroid cancer (radioactive-iodine refractory)

Dosing

Adult: 400 mg PO once daily on empty stomach (no food for ≥2 h before and 1 h after); reduce for toxicity (e.g., 300, 200 mg).
Pediatric: Not established (adult-only).
Renal adjustment: No adjustment for mild–moderate; severe and ESRD not studied.
Hepatic adjustment: No adjustment for mild–moderate; severe (Child-Pugh C) not studied.
Geriatric: No specific adjustment.
Max dose: 400 mg/day

Pharmacokinetics

Onset

Tumour effect over weeks

Peak effect

~2–4 h (Tmax)

Duration

~24 h (once-daily)

Half-life

~14–22 h

Bioavailability

Reduced by food (40% high-fat meal) — fasting required

Protein binding

~97%

Metabolism

Hepatic CYP3A4 (major), UGT1A4

Excretion

Mainly faecal (~73%); ~6% renal

Contraindications

Severe hypersensitivity
Caution: pneumonitis history, severe hypertension, severe haemorrhage risk

Side effects

Common

ConstipationHypertensionFatigueMyalgiaDiarrhoeaAnaemia / neutropenia / leukopenia

Serious

Pneumonitis / ILD
Severe hypertension / hypertensive crisis
Hepatotoxicity
Tumour lysis syndrome
Severe haemorrhage
Impaired wound healing

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective contraception during and 2 weeks after.

Lactation

Avoid breastfeeding during and 1 week after therapy.