Cabozantinib


Other name

-

International/Other brands

Cabometyx

Groups

Approved

Structure

Prescription products

NameDosageStrengthRouteLabeller
CabometyxTablet40 mg/1OralExelixis
CabometyxTablet20 mg/1OralExelixis
CabometyxTablet60 mg/1OralExelixis
CometriqCapsule20 mg/1OralExelixis
CometriqCapsule20 mgOralTmc Pharma Services Ltd.
CometriqKit--Exelixis

Target

MET, KDR, RET

Description

Cabozantinib was approved in 2012 and is a non-specific tyrosine kinase inhibitor. It is marketed as Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer. It's label includes a black box warning of gastrointestinal perforations, fistulas, and hemorrhage. The FDA approved cabozantinib as Cabometyx for patients with advanced renal cell carcinoma in April 2016.

Indications

Advanced Renal Cell Carcinoma; Progressive, metastatic Medullary thyroid cancer

Other indications

-

Mechaism of action

-

Absorption

After oral administration, peak plasma concentration was achieved in 2-5 hours.

Metabolism

Cabozantinib is metabolized mostly by CYP3A4 and, to a minor extent, by CYP2C9. Both enzyme produce an N-oxide metabolite.

Toxicity

Cabozantinib has a black box warning of serious gastrointestinal fistulas and perforations, and potentially fatal hemoptysis and gastrointestinal hemorrhage.