Zactima
Zactima Uses, Dosage, Side Effects, Food Interaction and all others data.
Zactima is an oral once-daily kinase inhibitor of tumour angiogenesis and tumour cell proliferation with the potential for use in a broad range of tumour types.
On April 6 2011, vandetanib was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients.
Mean IC50 of approximately 2.1 μg/mL.
Trade Name | Zactima |
Availability | Prescription only |
Generic | Vandetanib |
Vandetanib Other Names | Vandetanib |
Related Drugs | Armour Thyroid, doxorubicin, NP Thyroid, Adriamycin, Lenvima, cabozantinib |
Type | |
Formula | C22H24BrFN4O2 |
Weight | Average: 475.354 Monoisotopic: 474.106666884 |
Protein binding | Protein binding of about 90%. |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zactima is an antineoplastic kinase inhibitor used to treat symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease.
Zactima is currently approved as an alternative to local therapies for both unresectable and disseminated disease. Because Zactima can prolong the Q-T interval, it is contraindicated for use in patients with serious cardiac complications such as congenital long QT syndrome and uncompensated heart failure.
Zactima is also used to associated treatment for these conditions: Metastatic Medullary Thyroid Cancer, Locally advanced Medullary thyroid cancer
How Zactima works
ZD-6474 is a potent and selective inhibitor of VEGFR (vascular endothelial growth factor receptor), EGFR (epidermal growth factor receptor) and RET (REarranged during Transfection) tyrosine kinases.
VEGFR- and EGFR-dependent signalling are both clinically validated pathways in cancer, including non-small-cell lung cancer (NSCLC). RET activity is important in some types of thyroid cancer, and early data with vandetanib in medullary thyroid cancer has led to orphan-drug designation by the regulatory authorities in the USA and EU.
Food Interaction
- Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum levels of vandetanib.
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum levels of vandetanib.
- Take with or without food.
Zactima Hypertension interaction
[Moderate] Hypertension, including hypertensive crisis, has occurred in patients treated with vandetanib.
Monitor all patients for hypertension and a dose reduction or interruption may be necessary.
If hypertension cannot be controlled, do not resume vandetanib.
Care should be taken when using this agent in hypertensive patients.
Close monitoring is recommended.
Zactima Drug Interaction
Major: lithiumModerate: glycerinMinor: sulfamethoxazole / trimethoprimUnknown: charcoal, ubiquinone, copper gluconate, glucose, diltiazem, ethanol, ledipasvir / sofosbuvir, arginine, levocarnitine, cysteine, valproic acid, thiamine, cyanocobalamin, pyridoxine, cholecalciferol, phytonadione, menaquinone
Zactima Disease Interaction
Major: QT prolongationModerate: lung toxicity, heart failure, hemorrhage, hepatic impairment, hypertension, hypothyroidism, ischemic attack, renal impairment, RPL syndrome
Volume of Distribution
Vd of about 7450 L.
Elimination Route
Slow- peak plasma concentrations reached at a median 6 hours. On multiple dosing, Zactima accumulates about 8 fold with steady state reached after around 3 months.
Half Life
Median half life of 19 days.
Elimination Route
About 69% was recovered following 21 days after a single dose of vandentanib. 44% was found in feces and 25% in urine.
Innovators Monograph
You find simplified version here Zactima