Vandetanib

Vandetanib

Clinical data
Trade names	Caprelsa
Synonyms	ZD6474
AHFS/Drugs.com	caprelsa
MedlinePlus	a611037
License data	EU EMA: by INN US FDA: Vandetanib
Pregnancy category	AU: D US: D (Evidence of risk)
Routes of administration	Oral
ATC code	L01XE12 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) CA: ℞-only UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Protein binding	90–96%
Metabolism	CYP3A4, FMO1, FMO3
Biological half-life	19 days (mean)
Excretion	44% faeces, 25% urine
Identifiers
IUPAC name N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
CAS Number	443913-73-3 N
PubChem CID	3081361
IUPHAR/BPS	5717
DrugBank	DB08764 Y
ChemSpider	2338979 Y
UNII	YO460OQ37K
ChEBI	CHEBI:49960 Y
ChEMBL	CHEMBL24828 Y
PDB ligand	ZD6 (PDBe, RCSB PDB)
ECHA InfoCard	100.195.611
Chemical and physical data
Formula	C22H24BrFN4O2
Molar mass	475.354 g/mol
3D model (JSmol)	Interactive image
SMILES CN1CCC(CC1)COc2cc3c(cc2OC)c(ncn3)Nc4ccc(cc4F)Br
InChI InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27) Y Key:UHTHHESEBZOYNR-UHFFFAOYSA-N Y
NY (what is this?)

Vandetanib (INN, trade name Caprelsa) is an anti-cancer drug that is used for the treatment of certain tumours of the thyroid gland. It acts as a kinase inhibitor of a number of cell receptors, mainly the vascular endothelial growth factor receptor (VEGFR), the epidermal growth factor receptor (EGFR), and the RET-tyrosine kinase. The drug was developed by AstraZeneca and later on Sanofi.

Vandetanib is used to treat medullary thyroid cancer in adults who are ineligible for surgery.

People whose cancer develops a V804M mutation in RET stop responding to vandetanib.

In people with moderate and severe hepatic impairment, no dosage for vandetanib has been recommended, as its safety and efficacy has not been established yet. Vandetanib is contraindicated in people with congenital long QT syndrome.

Very common (present in greater than 10% of people) adverse effects include colds, bronchitis, upper respiratory tract infections, urinary tract infections, decreased appetite, low calcium absorption, insomnia, depressed mood, Headache, tingling sensations, weird, painful sensations, dizziness, blurred vision, damage to the cornea, long QT syndrome, high blood pressure, stomach pain, diarrhea, nausea, vomiting, indigestion, sensitivity to sunlight, rash, acne, dry and itchy skin, nail disorders, protein in urine, kidney stones, weakness, fatigue, pain, and edema.