Axitinib (Inlyta)

General information

Class/mechanism: Tyrosine kinase inhibitor of vascular endothelial growth factor receptors VEGFR-1, VEGFR-2, and VEGFR-3, which interferes with tumor angiogenesis, growth, and cancer progression, at picomolar concentrations. Inhibits PDGFRA, PDGFRB and c-kit at nanomolar concentrations.
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is established (work in progress)

• Renal cell carcinoma

Diseases for which it is used

• Hepatocellular carcinoma
• Thyroid cancer
  • Differentiated thyroid cancer
  • Medullary thyroid cancer

Patient drug information

• Inlyta Side Effect Tips & Videos (Pfizer)
• Axitinib (Inlyta) package insert
• Axitinib (Inlyta) patient drug information (Chemocare)
• Axitinib (Inlyta) patient drug information (UpToDate)

History of changes in FDA indication

• 2012-01-27: Initial approval for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. (Based on AXIS)
• 2019-05-14: Approved in combination with avelumab for first-line treatment of patients with advanced renal cell carcinoma (RCC). (Approval extended to first-line setting, in combination; based on JAVELIN Renal 101)
• 2020-06-04: Approved in combination with pembrolizumab, for the first-line treatment of patients with advanced RCC. (Based on KEYNOTE-426)

History of changes in EMA indication

• 2012-09-03: Initial marketing authorization as Inlyta. Inlyta is indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of prior treatment with sunitinib or a cytokine. (Based on AXIS)

History of changes in Health Canada indication

• 2012-07-12: Initial notice of compliance
• Uncertain date: Indicated for the treatment of patients with metastatic renal cell carcinoma (RCC) of clear cell histology after failure of prior systemic therapy with either a cytokine or the VEGFR-TKI, sunitinib.
• Uncertain date: in combination with pembrolizumab, is indicated for the treatment of adult patients with advanced or metastatic renal cell carcinoma (RCC) with no prior systemic therapy for metastatic RCC.

History of changes in PMDA indication

• 2012-06-29: Initial approval for the treatment of unresectable or metastatic renal cell carcinoma.

Also known as

• Code names: AG-013736
• Brand name: Axishil, Axpero, Inlybest, Inlyta, Luciax