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cabozantinib (Cometriq, Cabometyx, XL184)

FDA desgination as Orphan drug in Jan 2011. Indications: - treatment of medullary thyroid carcinoma (FDA-approved 2012) [4] - metastatic castration-resistant prostate cancer [5] (investigational) - advanced renal cell carcinoma - patients previously treated with VEGF inhibitor - patients with bone metastases [6] - advanced hepatocellular carcinoma [7] Dosage: - oral dosing - take on empty stomach: - do not eat for at least 2 hours before & 1 hour after taking Cometriq Monitor: - complete blood count - liver function tests - serum calcium Adverse effects: - diarrhea - stomatitis - hand-foot syndrome - weight loss - loss of appetite - nausea - fatigue - oral pain - graying or loss of hair color - dysgeusia - hypertension - abdominal pain - constipation - abnormal liver function tests - hypocalcemia - hypophosphatemia - leukopenia - thrombocytopenia Mechanism of action: - tyrosine kinase inhibitor - inhibits c-Met, VEGFR2, FLT3, TIE2, KIT & RET - reduces tumor growth, metastasis, & angiogenesis

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

small inhibitory antineoplastic agent (ib drug) antineoplastic tyrosine kinase inhibitor

Database Correlations

PUBCHEM correlations

References

  1. FDA News Release: Nov. 29, 2012 FDA approves Cometriq to treat rare type of thyroid cancer http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm330143.htm
  2. Hussain M et al Cabozantinib (XL184) in metastatic castration-resistant prostate cancer (mCRPC): Results from a phase II randomized discontinuation trial. J Clin Oncol 29: 2011 (suppl; abstr 4516) http://www.asco.org/ASCOv2/Meetings/Abstracts?&vmview=abst_detail_view&confID=102&abstractID=82339
  3. Wikipedia: Cabozantinib http://en.wikipedia.org/wiki/Cabozantinib
  4. SelleckBio.com http://www.selleckbio.com/xl184-cabozantinib-S1119.html?gclid=CJmK79zkrLUCFQfhQgodhGwAhA
  5. Smith DC et al. Cabozantinib in patients with advanced prostate cancer: Results of a Phase II randomized discontinuation trial. J Clin Oncol 2013 Feb 1; 31:412 PMID: 23169517
  6. Minerd J MedPage Today. January 14, 2018 Cabozantinib Bests Everolimus in RCC with Bone Metastases. Subgroup analysis of METEOR trial showed improved survival. https://www.medpagetoday.com/hematologyoncology/renalcellcarcinoma/70501 - Escudier B, Powles T, Motzer RJ et al Cabozantinib, a new standard of care for patients with advanced renal cell carcinoma and bone metastases? Subgroup analysis of the METEOR trial J Clin Oncol. 2018 Jan 8:JCO2017747352 PMID: 29309249
  7. Abou-Alfa GK, Meyer T, Cheng AL et al Cabozantinib in Patients with Advanced and Progressing Hepatocellular Carcinoma. N Engl J Med 2018; 379:54-63. July 5, 2018 PMID: 29972759 https://www.nejm.org/doi/full/10.1056/NEJMoa1717002
  8. Medscape: cabozantinib (Rx) https://reference.medscape.com/drug/cometriq-cabometyx-cabozantinib-999791