Cabozantinib
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| Names | |
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| IUPAC name
N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
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| Other names
XL184, BMS907351
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| Identifiers | |
3D model (JSmol)
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| ChemSpider | |
| ECHA InfoCard | 100.221.147 |
| KEGG | |
| UNII | |
CompTox Dashboard (EPA)
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| Properties | |
| C28H24FN3O5 | |
| Molar mass | 501.514 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Cabozantinib (XL184) is a small molecule inhibitor of the tyrosine kinases c-Met and VEGFR2, and has been shown to reduce tumor growth, metastasis, and angiogenesis.
It is being developed by Exelixis Inc.
Cabozantinib was granted orphan-drug status by the FDA in January 2011.[1]
It is currently in a number of clinical trials for prostate, ovarian, brain, melanoma, breast, non-small cell lung, hepatocellular, kidney, and medullary thyroid cancer.
Positive data from clinical trials indicate cabozantinib is particularly beneficial in metastatic advanced prostate cancer. 97% of patients either had stabilization or improvement in bone malignancies. The median time to disease progression was 29 weeks.[2][3]
One US trial reported in May 2011 : The best results were seen in patients with liver, prostate, and ovarian cancer: 22 of 29 patients with liver cancer, 71 of 100 patients with prostate cancer, and 32 of 51 with ovarian cancer experienced either partial tumor shrinkage or stable disease. Fifty-nine out of 68 patients who had bone metastases had their metastases shrink or disappear during the trial.[4]
See also
References
- ^ Exelixis’ XL184 Granted Orphan Drug Designation and Assigned the Generic Name Cabozantinib. Jan 2011
- ^ "Exelixis drug slows prostate cancer spread in trial". Reuters. 6 June 2011.
- ^ Cabozantinib (XL184) Phase 2 Data Demonstrate Encouraging Clinical Activity in Patients with Castration-Resistant Prostate Cancer. Feb 2011
- ^ "Cabozantinib Shrinks Tumors and Bone Metastases in Prostate and Other Cancers". 31 May 2011.
External links
- Exelixis: Looming Cancer Conference a Favorable Swing Trade Opportunity
- A phase II study of XL184 in patients (pts) with progressive glioblastoma multiforme (GBM) in first or second relapse. 2009
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