axitinib (Inlyta)

Introduction

FDA-approved Jan 27, 2012

Indications

• treatment of advanced renal cell carcinoma after failure of one prior systemic therapy

Dosage

• 5 mg PO BID

Tabs: 1 mg, 5 mg

Adverse effects

• most common
  • diarrhea, hypertension, fatigue, decreased appetite, nausea, dysphonia, palmar-plantar erythrodysesthesia (hand-foot syndrome), weight decreased, vomiting, asthenia, constipation
• severe adverse reactions
  • hypertensive crisis, arterial thrombosis, venous thrombosis, hemorrhage, gastrointestinal perforation, fistula formation, reversible posterior leukoencephalopathy syndrome

• drug adverse effects of tyrosine kinase inhibitor(s)

Mechanism of action

• tyrosine kinase inhibitor
• inhibits VEGFR-1, VEGFR-2, VEGFR-3, PDGFR & cKIT (CD117)

More general terms

• small inhibitory antineoplastic agent (ib drug)
• antineoplastic tyrosine kinase inhibitor

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=6450551
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=49849411
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=23724859