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Cabozantinib

Generic Name
Cabozantinib
Brand Names
Cabometyx, Cometriq
Drug Type
Small Molecule
Chemical Formula
C28H24FN3O5
CAS Number
849217-68-1
Unique Ingredient Identifier
1C39JW444G

Overview

Cabozantinib was first approved in 2012 and is a non-specific tyrosine kinase inhibitor. It was initially approved in the US under the brand name Cometriq, which is indicated for the treatment of metastatic medullary thyroid cancer. In 2016, a capsule formulation (Cabometyx) was approved for the treatment of advanced renal cell carcinoma, and this same formulation gained additional approval in both the US and Canada in 2019 for the treatment of hepatocellular carcinoma in previously treated patients.

Indication

⑴治疗进展的、不能切除的局部晚期或转移的髓性甲状腺癌。 ⑵用于舒尼替尼(索坦)治疗失败的晚期肾癌。

Associated Conditions

  • Advanced Renal Cell Carcinoma
  • Hepatocellular Carcinoma
  • Metastatic Differentiated Thyroid Cancer
  • Locally advanced Differentiated Thyroid Cancer (DTC)
  • Metastatic Clear Cell Renal Cell Carcinoma (ccRCC)
  • Progressive, metastatic Medullary thyroid cancer

Research Report

Published: Jul 15, 2025

Cabozantinib (DB08875): A Comprehensive Monograph on its Pharmacology, Clinical Development, and Therapeutic Role

Section 1: Executive Summary and Drug Profile

1.1. Overview of Cabozantinib as a Multi-Targeted Tyrosine Kinase Inhibitor

Cabozantinib is an orally bioavailable small molecule that represents a significant therapeutic advance in the field of oncology. It functions as a potent, non-specific inhibitor of multiple receptor tyrosine kinases (RTKs), which are key mediators of cellular signaling pathways that drive cancer progression.[1] The fundamental mechanism of action of cabozantinib involves the simultaneous suppression of critical processes including tumor growth (oncogenesis), the formation of new tumor-supplying blood vessels (angiogenesis), and the spread of cancer to distant sites (metastasis).[1] This broad-spectrum activity against the core drivers of malignancy underpins its demonstrated efficacy across a diverse and expanding range of solid tumors, establishing it as a versatile and powerful agent in the modern anticancer armamentarium.

1.2. Key Identifiers, Formulations, and Brand Names (Cometriq® vs. Cabometyx®)

The drug is identified by its DrugBank ID DB08875 and Chemical Abstracts Service (CAS) Number 849217-68-1. During its development, it was also known by the codes XL184 and BMS-907351.[1] A crucial aspect of cabozantinib's clinical and commercial profile is the existence of two distinct brand names, which correspond to different formulations, approved dosages, and initial therapeutic indications.[8] Understanding this distinction is fundamental to appreciating its development history and appropriate clinical use.

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/06/10
Phase 3
Not yet recruiting
2025/06/08
Phase 4
Not yet recruiting
Fujian Medical University
2025/04/18
Phase 4
Not yet recruiting
2025/03/28
Phase 2
Not yet recruiting
2025/02/19
Phase 1
Recruiting
2025/02/06
Phase 1
Recruiting
2024/12/04
Phase 1
Recruiting
2024/08/12
N/A
Recruiting
Gruppo Oncologico Italiano di Ricerca Clinica
2024/08/02
Phase 2
Not yet recruiting
2024/07/16
Phase 1
Not yet recruiting
Girish Dhall, MD

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Exelixis, Inc.
42388-013
ORAL
20 mg in 1 1
5/23/2016
Exelixis, Inc.
42388-023
ORAL
60 mg in 1 1
1/17/2023
Exelixis, Inc.
42388-025
ORAL
40 mg in 1 1
1/17/2023
Exelixis, Inc.
42388-024
ORAL
20 mg in 1 1
1/17/2023

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
Authorised
3/21/2014

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
CABOMETYX FILM COATED TABLET 20MG
SIN15606P
TABLET, FILM COATED
20mg
1/3/2019
CABOMETYX FILM COATED TABLET 60MG
SIN15608P
TABLET, FILM COATED
60mg
1/3/2019
CABOMETYX FILM COATED TABLET 40MG
SIN15607P
TABLET, FILM COATED
40mg
1/3/2019

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.

TGA Drug Approvals

Approved Product
ARTG ID
Sponsor
Registration Type
Status
Registration Date
No TGA approvals found for this drug.

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