Drug reference

Axitinib

Selective VEGFR tyrosine kinase inhibitor (antineoplastic) · Antineoplastic agent

Also known as Inlyta

START

5 mg PO twice daily; up-titrate to 7 or 10 mg BID if BP/AEs allow

TYPICAL MAX

20 mg/day

STOP IF

Severe BP / hypertensive crisis, thrombotic event, perforation, or hepatotoxicity

WATCH

BP weekly × 6 weeks then monthly, TSH, urine protein, LFTs

CDSCO approvedSchedule HATC L01EK01

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · absorption
PEAK: 3h · Tmax
t½: 4h · t½
DURATION: 12h · twice-daily

EXCRETION

Mainly faecal (~41%); ~23% renal

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Can cause fetal harm — avoid; effective contraception during and 1 week after.

FDA category + note

Top interactionssee all 12 →

AmprenavirSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter
AtazanavirSevereDatabaseDDInter
BoceprevirSevereDatabaseDDInter

Mechanism

Selective ATP-competitive inhibitor of VEGFR-1/2/3 tyrosine kinases, blocking VEGF-mediated tumour angiogenesis; less off-target activity (PDGFR, c-KIT) than first-gen TKIs.

Indications

Advanced renal cell carcinoma (after failure of one prior systemic therapy; or first-line combinations with pembrolizumab/avelumab)

Dosing

Adult: 5 mg PO twice daily; titrate after 2 weeks if BP controlled and no AEs to 7 or 10 mg twice daily (max 20 mg/day); reduce for toxicity.
Pediatric: Not established.
Renal adjustment: No adjustment for any eGFR (limited data ESRD).
Hepatic adjustment: Moderate impairment: halve starting dose (2 mg twice daily). Severe: not recommended.
Geriatric: No specific adjustment.
Max dose: 20 mg/day (10 mg twice daily)

Pharmacokinetics

Onset

Tumour response over weeks

Peak effect

~2.5–4.1 h (Tmax)

Duration

~12 h (twice-daily)

Half-life

~2.5–6 h

Bioavailability

~58% (food does not significantly affect)

Protein binding

>99%

Metabolism

Hepatic CYP3A4/5 (primary), CYP1A2/2C19 (minor)

Excretion

Mainly faecal (~41%); ~23% renal (metabolites)

Contraindications

Severe hypersensitivity
Caution: poorly-controlled hypertension, recent CV event, untreated thyroid disease

Side effects

Common

HypertensionDiarrhoeaFatigueHand-foot syndromeHypothyroidismProteinuria

Serious

Severe hypertension / hypertensive crisis
Arterial / venous thromboembolism
Haemorrhage (incl. ICH)
GI perforation / fistula
Posterior reversible encephalopathy
Severe hepatotoxicity

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective contraception during and 1 week after.

Lactation

Avoid breastfeeding during and 2 weeks after therapy.