Crizotinib (Xalkori®)

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

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

Formula:

C₂₁H₂₂Cl₂FN_5O

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

• upper respiratory infection,
• nausea,
• vomiting
• stomach pain,
• decreased appetite,
• insomnia,
• dizziness,
• tired feeling,
• diarrhea,
• constipation,
• rash or itching,
• cold symptoms (stuffy nos
• swelling in hands or feet.

Tell your doctor if you have serious side effects of Xalkori including:

• severe dizziness, fainting, fast or pounding heartbeats;
• vision problems such as blurred vision, increased sensitivity of your eyes to light, or seeing flashes of light or "floaters";
• chest pain, dry cough or cough with mucus, wheezing, shortness of breath;
• easy bruising, unusual bleeding, purple or red pinpoint spots under your skin;
• fever, chills, body aches, flu symptoms, sores in your mouth and throat;
• loss of appetite, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).

Sources

1. Rx Lise. "Xalkori." Last reviewed on RxList 7/8/2019 https://www.rxlist.com/xalkori-side-effects-drug-center.htm
2. 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
3. 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
4. National Center for Biotechnology Information. PubChem Compound Database; "CID=11626560", (accessed Jan. 12, 2018) Source: https://pubchem.ncbi.nlm.nih.gov/compound/11626560
5. MedKoo Biosciences. "Crizotinib - MedKoo CAT#: 202222" (accessed Jan. 12, 2018) Source: http://www.medkoo.com/products/4537
   
6. 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
7. Troutman, Scott, et al. "Crizotinib inhibits NF2-associated schwannoma through inhibition of focal adhesion kinase 1." Oncotarget 7.34 (2016): 54515. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5342359/