Cabozantinib

Cabozantinib 2D
Brand name: Cabometyx
Brand name: Cometriq®
IUPAC: 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
FDA approval: Yes
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Usage:

Cabozantinib is used in the treatment of metastatic medullary thyroid cancer (MTC) and is typically administered in tablet form.1  Cometriq™ is a targeted therapy. It is an oral receptor tyrosine kinase inhibitor. Used for the treatment of metastatic medullary thyroid cancer (MTC). Cometriq™ is a pill taken by mouth.

  • Take COMETRIQ™ on an empty stomach. Do not eat for at least 2 hours before and at least 1 hour after taking COMETRIQ™. 

  • You should not drink grapefruit juice or eat grapefruit during treatment with COMETRIQ™. It may change the amount of COMETRIQ™ in your blood. 

  • Take COMETRIQ™ exactly as prescribed. 

  • Swallow COMETRIQ™ capsules whole with at least 8 ounces of water. Do not crush, dissolve or open capsules. 

  • Do not change your dose or stop COMETRIQ™ unless your health care provider tells you to. 

  • If you miss a dose and your next dose is due in: 

  • Less than 12 hours, take your next dose at the normal time. Do not make up the next dose. 

  • 12 hours or more, take the missed dose as soon as you remember. Take your next dose at the normal time. 

  • Do not take more than 1 dose of COMETRIQ™ at one time. Call your health care provider right away if you take too much. 

  • The amount of COMETRIQ™ that you will receive depends on many factors, your general health or other health problems, and the type of cancer or condition being treated. Current recommendation is for one tablet twice daily, higher doses do not give a better response and may cause increased toxicity. Your doctor will determine your dose and schedule. 

  • 1Cabometyx. (n.d.). Retrieved June 29, 2017, from https://hcp.cabometyx.com/index.php
Mechanism:

Cabozantinib works by disrupting tumors by inhibiting the function of tyrosine kinases.  These kinases are important for tumor growth and migration, and when turned off can lead to apoptosis.1

The diagram below shows the 3D molecular structure of Cabozantinib.

 

  • 1COMETRIQ® (cabozantinib) is the first and only FDA-approved therapy for the treatment of progressive, metastatic MTC that has been shown to inhibit MET; VEGFR-1, -2, and -3; and RET. (n.d.). Retrieved June 29, 2017, from http://www.cometriq.com/hcp/moa/
Side effects:

The following side effects are common (occurring in greater than 30%) for patients taking Cometriq: increased liver enzymes, diarrhea, low calcium, mouth sores, weight loss, decreased appetite, fatigue, oral pain, neutropenia, low platelets, taste changes, hair color changes, high blood pressure and hand-foot syndrome. Hand-foot syndrome (Palmar-plantar erythrodysesthesia or PPE) consists of skin rash, swelling, redness, pain and/or peeling of the skin on the palms of hands and soles of feet. Usually mild, starting 5-6 weeks after start of treatment. May require reductions in the dose of the medication. 

The following side effects are common (occurring around 10-29%) for patients taking Cometriq: low phosphorous, abdominal pain, constipation high bilirubin levels, vomiting, weakness, voice changes, dry skin, rash, low magnesium, headache, low potassium, hair loss, dizziness, joint pain, swallowing trouble, muscle spasms, dyspepsia (indigestion), skin redness, and low sodium.