Last reviewed 2026-04-20 · How we verify

Xalkori (crizotinib)

Xalkori works by blocking the hepatocyte growth factor receptor, a protein that helps cancer cells grow and spread.

Xalkori (crizotinib) is a small molecule kinase inhibitor developed by PF PRISM CV and currently owned by the same. It targets the hepatocyte growth factor receptor, a protein involved in the growth and spread of cancer cells. Xalkori is FDA-approved for the treatment of non-small cell lung cancer and has a half-life of approximately 38.9 hours. The drug is patented and has no generic manufacturers. Key safety considerations include its potential to cause liver damage and other side effects.

At a glance

Mechanism of action

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur dOrigine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the genes expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met.In vitro, crizotinib induced apoptosis and inhibited proliferation and ALK-mediated signaling in ALCL-derived cell lines (containing NPM-ALK) at clinical

Approved indications

• Non-small cell lung cancer

Common side effects

• Vision disorder
• Nausea
• Diarrhea
• Vomiting
• Edema
• Constipation
• Elevated transaminases
• Fatigue
• Decreased appetite
• Upper respiratory infection
• Dizziness
• Neuropathy

Drug interactions

• P-glycoprotein Substrates
• alfentanil
• amiodarone
• artemether
• bepridil
• boceprevir
• carbamazepine
• ciclosporin
• cisapride
• clarithromycin
• colchicine
• conivaptan

Key clinical trials

• A Clinical Trial Testing The Efficacy Of Crizotinib Versus Standard Chemotherapy Pemetrexed Plus Cisplatin Or Carboplatin In Patients With ALK Positive Non Squamous Cancer Of The Lung (PHASE3)
• Crizotinib in Treating Younger Patients With Relapsed or Refractory Solid Tumors or Anaplastic Large Cell Lymphoma (PHASE1,PHASE2)
• An Investigational Drug, PF-02341066 Is Being Studied Versus Standard Of Care In Patients With Advanced Non-Small Cell Lung Cancer With A Specific Gene Profile Involving The Anaplastic Lymphoma Kinase (ALK) Gene (PHASE3)
• Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
• Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) (PHASE2)
• Genetic Testing in Screening Patients With Stage IB-IIIA Non-small Cell Lung Cancer That Has Been or Will Be Removed by Surgery (The ALCHEMIST Screening Trial) (NA)
• Testing Crizotinib as Potentially Targeted Treatment in Cancers With MET Exon 14 Deletion Genetic Changes (MATCH - Subprotocol C2) (PHASE2)
• Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer (PHASE2)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Xalkori CI brief — competitive landscape report
• Xalkori updates RSS · CI watch RSS
• Pfizer portfolio CI