Cabozantinib S-malate

Cabozantinib S-malate was approved by the U.S. Food and Drug Administration (FDA) on November 29, 2012, then approved by European Medicine Agency (EMA) on March 21, 2014. It was developed and marketed as Cometriq® by Exelixis in the US.

Cabozantinib S-malate is a multiple receptor tyrosine kinases inhibitor indicated for the treatment of patients with progressive, metastatic medullary thyroid cancer (MTC).

Cometriq® is available as capsule for oral use, containing 20 or 80 mg of free Cabozantinib, and the recommended dose is 140 mg once daily.

General Information

Update Date:2016-05-16

Drug Name:
Cabozantinib S-malate
Research Code:
XL-184; BMS-907351
Trade Name:
Cometriq®
MOA:
Multiple receptor tyrosine kinase inhibitor
Indication:
Medullary thyroid cancer (MTC); Advanced renal cell carcinoma (RCC)
Status:
Approved
Company:
Exelixis (Originator)
Sales:
$59.2 Million (Y2015);
$25.1 Million (Y2014);
$15 Million (Y2013);
ATC Code:
L01XE
Approved Countries or Area

Update Date:2016-05-16

Approval Date Approval Type Trade Name Indication Dosage Form Strength Company Review Classification
2016-04-25 New indication Cabometyx Advanced renal cell carcinoma (RCC) Tablet Eq. 20 mg/40 mg/60 mg Cabozantinib Exelixis
2012-11-29 Marketing approval Cometriq Medullary thyroid cancer (MTC) Capsule Eq. 20 mg/80 mg Cabozantinib Exelixis Priority; Orphan
Approval Date Approval Type Trade Name Indication Dosage Form Strength Company Review Classification
2014-03-21 Marketing approval Cometriq Medullary thyroid cancer (MTC) Capsule 20 mg/80 mg TMC Pharma Orphan; Conditional Approval
Chemical Structure

Update Date:2015-09-16

Molecular Weight 635.6
Formula C28H24FN3O5 • C4H6O5
CAS No. 849217-68-1 (Cabozantinib);
1140909-48-3 (Cabozantinib S-malate);
Chemical Name (S)-malate is described chemically as N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N'-(4-fluorophenyl)cyclopropane- 1,1-dicarboxamide, (2S)-hydroxybutanedioate
Cabozantinib (Free Acid/Base)Parameters:
MW HD HA FRB* PSA* cLogP*
501.51 2 8 8 98.8 3.077±1.151
*:Calculated by ACD/Labs software V11.02.
Related Patents

Update Date:2015-12-03

Synthesis & Impurities

Update Date:2016-05-11


1. WO2005030140A2 / US7579473B2



1. CN103664776A.

Impurity database is being updated!