1802168-46-2COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OCONIQOQHATWINJY-UHFFFAOYSA-NCabozantinib is a dicarboxylic acid diamide that is N-phenyl-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It is a member of quinolines, an aromatic ether, a dicarboxylic acid diamide and an organofluorine compound.
1802168-46-2CHEMBL2105717CHEBI:72317Pharmaceuticals -> Listed in ZINC15
Pharmaceuticals -> Antineoplastic and immunomodulating agents -> Antineoplastic agents
Breast Feeding; Lactation; Antineoplastic Agents; Enzyme Inhibitors; Protein Kinase Inhibitors; Signal Transduction Inhibitors; Tyrosine Kinase Inhibitors;
FDA approved drugs -> Active ingredient
EMA approved medicines: Human medicine
EMA approved medicines: Human medicine (Orphan designations)
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In large clinical trials of cabozantinib, elevations in serum aminotransferase levels were common, occurring in 16% to 97% of patients. Values greater than 5 times the upper limit of normal (ULN), however, occurred in only 2% to 8% of recipients. Serum alkaline phosphatase elevations were also common and were above 3 times ULN in 3% of patients. Despite the high rate of serum enzyme elevations, cases of clinically apparent liver injury including acute liver failure were not reported in the preregistration trials of cabozantinib. Since the approval of cabozantinib, there have been no published case reports of hepatotoxicity attributed to its use. Serum ALT, AST and alkaline phosphatase elevations are listed as adverse reactions in the product label for cabozantinib, and cholestatic hepatitis is mentioned as a rare occurrence, but monitoring of serum enzymes during treatment is not specifically recommended.
L01XE26
L - Antineoplastic and immunomodulating agents
QL - Antineoplastic and immunomodulating agents
1C39JW444G
CABOZANTINIB
Established Pharmacologic Class [EPC] - Kinase Inhibitor
Mechanisms of Action [MoA] - Protein Kinase Inhibitors
Cabozantinib is a Kinase Inhibitor. The mechanism of action of cabozantinib is as a Protein Kinase Inhibitor.
CABOZANTINIB
After oral administration, peak plasma concentration was achieved in 2-5 hours.
Cabozantinib is eliminated mostly by the feces (54%) and also by the urine (27%).
The volume of distribution is 349L.
At steady state, the clearance is 4.4 L/hr.
VerwendenCabozantinib-d6 is the labelled analogue of Cabozantinib (X745500), a medication used to treat medullary thyroid cancer. As well it can be used in biological study. Computational network biological approach based on pathway cross-talk inhibition identified new synergistic drug combinations using raloxifene and cabozantinib for treatment of human breast cancer in xenograft mouse model. Potent c-MET inhibitor.
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