caprelsa

caprelsa Uses, Dosage, Side Effects, Food Interaction and all others data.

caprelsa 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.

caprelsa
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	caprelsa
Availability	Prescription only
Generic	Vandetanib
Vandetanib Other Names	Vandetanib
Related Drugs	Armour Thyroid, doxorubicin, NP Thyroid, Adriamycin, Lenvima, cabozantinib
Weight	100mg, 300mg,
Type	Film-coated Tablet, Tablet, Oral Tablet
Formula	C₂₂H₂₄BrFN₄O₂
Weight	Average: 475.354 Monoisotopic: 474.106666884
Protein binding	Protein binding of about 90%.
Groups	Approved
Therapeutic Class
Manufacturer	Genzyme Europe B,v,, Sanofi Genzyme
Available Country	Saudi Arabia, Australia, Canada, United Kingdom, United States,
Last Updated:	September 19, 2023 at 7:00 am

Uses

caprelsa is an antineoplastic kinase inhibitor used to treat symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease.

caprelsa is currently approved as an alternative to local therapies for both unresectable and disseminated disease. Because caprelsa 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.

caprelsa is also used to associated treatment for these conditions: Metastatic Medullary Thyroid Cancer, Locally advanced Medullary thyroid cancer

How caprelsa 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.

caprelsa 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.

caprelsa 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

caprelsa 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, caprelsa accumulates about 8 fold with steady state reached after around 3 months.