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Crizotinib (Xalkori™)

  • Trial Availability: USA
  • Tumor Target: Schwannoma
  • Company: Pfizer
  • Treatment by: IV. Soluble in DMSO, not in water. Dimethyl Sulfoxide (DMSO) is an organosulfur compound with the formula (CH3)2SO.
  • Inhibotor of: FAK1 (PTK2)
  • IUPAC/Chemical Name: (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
  • Solubility: Soluble in DMSO, not in water. Dimethyl Sulfoxide (DMSO) is an organosulfur compound with the formula (CH3)2SO.
  • Other Names: PF-2341066, PF-02341066, PF2341066, PF-2341066, PF 2341066
  • Chemical Formula: C21H22Cl2FN5O
  • Recruiting Trial: NCT02465060

PI3K/Akt/mTOR signaling pathway
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
Also In Use For: Breast Cancer, solid tumor cancer
Dose: Single doses up to 100 mg two times a day, but study duration 1 month
http://www.medkoo.com/products/4537
https://ncats.nih.gov/files/AZD2014.pdf
Troutman, Scott, et al. "Crizotinib inhibits NF2-associated schwannoma through inhibition of focal adhesion kinase 1." Oncotarget 7.34 (2016): 54515. doi: 10.18632/oncotarget.10248 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5342359/