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Crizotinib (Xalkori®)

Status: Available in 2019 for NF2 in the United States and Canada


Crizotinib - Chemical Structure
Trade Name: Xalkori™
Chemical Compound: Crizotinib
Synonyms: CRZ, PF-2341066, PF-02341066,
PF2341066, PF-2341066, PF 2341066
Pharmaceutical Company: Pfizer
Legal Status: ℞ - Prescription
Administered By: Pill - Oral
Tumor Target: Schwannoma
Protein Target: FAK1 (PTK2) Inhibitor
NF2 Trials: Recruiting Trial: NCT02465060
IUPAC/Chemical Name: (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-
5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
Formula: C21H22Cl2FN5O

Helpful Facts

  • In trials for: Breast Cancer, solid tumor cancer
  • Solubility: Soluble in DMSO, not in water. Dimethyl Sulfoxide (DMSO) is an organosulfur compound with the formula (CH3)2SO.
  • Mammalian target of rapamycin (mTOR) serine/threonine kinase (dual mTOR Complex 1 and 2 inhibitor, mTORC1 and mTORC2)
  • Inhibitor: inhibits the membrane receptor MET and activation of the MET signaling pathway

Side Effects

  • fatigue
  • nausea
  • mucositis
  • rash
  • constipation
  • vomiting
  • dyspnea
  • cough

Sources

  1. Zhao, Yingchao, et al. "Targeting the cMET pathway augments radiation response without adverse effect on hearing in NF2 schwannoma models." Proceedings of the National Academy of Sciences (2018): 201719966.
    Source: http://www.pnas.org/content/early/2018/02/07/1719966115 | DOI: 10.1073/pnas.1719966115

  2. Troutman, Scott, et al. "Crizotinib inhibits NF2-associated schwannoma through inhibition of focal adhesion kinase 1." Oncotarget 7.34 (2016): 54515.
    Source: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5342359/ | DOI: 10.18632/oncotarget.10248

  3. National Center for Biotechnology Information. PubChem Compound Database; "CID=11626560", (accessed Jan. 12, 2018) Source: https://pubchem.ncbi.nlm.nih.gov/compound/11626560

  4. MedKoo Biosciences. "Crizotinib - MedKoo CAT#: 202222" (accessed Jan. 12, 2018) Source: http://www.medkoo.com/products/4537
  5. U.S. Food and Drug Administration. "FDA expands use of Xalkori to treat rare form of advanced non-small cell lung cancer." (March 11, 2016)
    Source: https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm490329.htm