Products
Vandetanib is commercially available in the form of film-coated tablets (Caprelsa). It was approved in the EU in 2011. It was registered in many countries in May 2012.
Structure and properties
Vandetanib (C22H24BrFN4O2, Mr = 475.4 g/mol) is a quinazolinamine and piperidine derivative that is practically insoluble in water.
Effects
Vandetanib (ATC L01XE12) is a tyrosine kinase inhibitor with antitumor, antiproliferative, and antiangiogenic properties. The kinases inhibited include VEGFR, EGFR, and RET.
Indications
For the treatment of patients with nonresectable, rapidly progressive, and symptomatic metastatic medullary thyroid carcinoma.
Dosage
According to the SmPC. Vandetanib is taken once daily, independent of meals, and always at the same time of day. It has a long half-life of 19 days. During treatment, the skin must be protected from the sun because vandetanib has photosensitizing properties.
Contraindications
- Hypersensitivity
- Congenital long QT syndrome
- Severe renal failure
- Lactation
Full precautions can be found in the drug label.
Interactions
Vandetanib is a substrate of CYP3A4 and a mild inducer of CYP450, as well as an inhibitor of OATP1B1, OATP1B3, P-gp, OCT1, and OCT2. CYP3A4 inducers such as rifampicin may reduce the bioavailability of vandetanib to a relevant extent. Vandetanib prolongs the QT interval and should not be administered with other drugs that also prolong the QT interval.
Adverse effects
The most common possible adverse effects include rash, skin reactions, photosensitivity, digestive disturbances such as diarrhea and vomiting, fatigue, weakness, weakness, weight loss, hypertension, headache, insomnia, prolongation of the QT interval, decreased appetite, and hypocalcemia.
