Cabozantinib (XL184)

Cabozantinib, formerly known as XL184, is a potent dual inhibitor of the MET and VEGF pathways designed to block MET driven tumor escape. In multiple preclinical studies cabozantinib has been shown to kill tumor cells, reduce metastases, and inhibit angiogenesis (the formation of new blood vessels necessary to support tumor growth).1

See more information on MET and VEGFR inhibition.

See cabozantinib's mechanism of action below:

Single-agent activity has been observed in several clinical trials, in diseases including medullary thyroid cancer, castration-resistant prostate cancer, lung cancer, and ovarian cancer. To date, we have observed objective responses in 12 of 13 tumor types studied and observed activity against metastatic bone lesions in five tumor types, including prostate, renal, breast, thyroid, and melanoma.2,3

See additional information on bone metastases.

The depth and breadth of clinical activity observed to date with cabozantinib reflect its broad potential as a new addition to the oncology landscape. Exelixis is evaluating cabozantinib in multiple clinical trials.

 
Phase 3 Medullary Thyroid Cancer
Phase 2 Non-Randomized Extension Cohorts Metastatic Castration-Resistant Prostate Cancer
Ovarian Cancer
Phase 2 Randomized Discontinuation Trial (RDT) Breast Cancer
Gastric/GE Junctional Cancer
Hepatocellular Carcinoma
Melanoma
Castration-Resistant Prostate Cancer
Non-small Cell Lung Cancer
Ovarian Cancer
Pancreatic Cancer
Small Cell Lung Cancer
Phase 1B Differentiated Thyroid Cancer
Renal Cell Carcinoma

 

References:

  1. Yakes, F.M., et. al. Draft Manuscript.  Data on file.  Exelixis, Inc.
  2. Smith, M.C., et. al. 2011.  Presented at the American Society of Clinical Oncology Genitourinary Cancers Symposium, Abstract #127.
  3. Vergote, I., et. al.. 2010.  Presented at the 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, Abstract #407.