Drug reference

Regorafenib

Tyrosine Kinase Inhibitor · Antineoplastic Agent

Tyrosine Kinase InhibitorAntineoplastic Agent

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

AbciximabSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter
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AnagrelideSevereDatabaseDDInter

Mechanism

Regorafenib is a small molecule inhibitor that targets and inhibits several protein kinases. This action interferes with various cellular processes crucial for tumor growth, angiogenesis, and metastasis.

Indications

Metastatic colorectal cancer (specialist use only)Unresectable or metastatic gastrointestinal stromal tumours (specialist use only)Hepatocellular carcinoma (specialist use only)Metastatic chemorefractory colorectal cancermetastatic colorectal cancer after previous chemotherapy, anti-VEGF therapy, or anti-EGFR therapyhepatocellular carcinoma who have been previously treated with sorafeniblocally advanced, unresectable, or metastatic GIST after imatinib or sunitinib

Dosing

Adult: BY MOUTH: 160 mg once daily for 21 consecutive days of repeated 28-day cycles (for dose adjustment due to side effects—consult product literature)
Max dose: 160 mg once daily

Pharmacokinetics

Half-life

about 28 h (elimination)

Bioavailability

—

Protein binding

99.5%

Metabolism

CYP3A (mostly)

Excretion

—

Contraindications

Myocardial ischaemia or infarction
Hypertensive crisis
Major surgical procedures (prior to procedure, due to impaired wound healing)
Predisposition to bleeding

Side effects

Common

AlopeciaAnaemiaAppetite decreasedAstheniaDiarrhoeaDry mouthDysphoniaElectrolyte imbalanceFeverGastro-oesophageal reflux diseaseHeadacheHyperbilirubinaemiaHypertensionHand-foot skin reaction

Serious