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
Zactima
Zactima

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.

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

*** Taking medicines without doctor's advice can cause long-term problems.
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