Vandetanib

What is Vandetanib?

• Vandetanib (Caprelsa) is a kinase inhibitor used to treat medullary thyroid cancer that is locally advanced or has spread to other parts of the body.
• It is used in patients whose cancer cannot be removed by surgery.
• It is also being studied in the treatment of other types of cancer.

Vandetanib

Vandetanib structure

Vandetanib metabolism

What are the uses of this medicine?

• Vandetanib (Caprelsa) is a prescription medicine used to treat medullary thyroid cancer that cannot be removed by surgery or that has spread to other parts of the body.
• It takes a long time to get rid of Caprelsa from your body and you may be at risk for side effects related to Caprelsa after you have stopped your treatment.

How does this medicine work?

• Vandetanib (van det’ a nib) is an orally available, multi-kinase inhibitor with activity against vascular endothelial growth factor (VEGF) and epidermal growth factor (EGF) receptor families as well as RET (rearranged-during- transfection), BRK, TIE2 and Src kinases.
• Vandetanib has potent anti-angiogenesis activity and specific potency against mutant RET tyrosine kinases that are found in most hereditary and a large proportion of spontaneous medullary thyroid cancers.
• Clinical trials of vandetanib in advanced or metastatic medullary thyroid cancer have documented significant prolongation of progression free survival.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have had QT prolongation

What drug interactions can this medicine cause?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take:

• St. John's wort. You should not take St. John's wort while taking Caprelsa
• certain medicines that can affect how your liver breaks down medicine
• a medicine for your heart

Be sure to mention any of the following:

• carbamazepine (Tegretol, Carbatrol, Equetro), dexamethasone, phenobarbital, phenytoin (Dilantin, Phenytek), rifabutin (Mycobutin), rifampin (Rifadin, in Rifamate), rifapentin (Priftin), and thyroid hormones such as levothyroxine (Synthroid)
• chloroquine (Aralen); clarithromycin (Biaxin, in Prevpac)

haloperidol (Haldol)

• medications for an irregular heartbeat such as amiodarone (Cordarone, Pacerone), disopyramide (Norpace), dofetilide (Tikosyn), procainamide, and sotalol (Betapace)
• certain medications for nausea such as dolasetron (Anzemet) and granisetron (Sancuso)
• methadone (Dolophine, Methadose)
• moxifloxacin (Avelox)
• pimozide (Orap)

Is this medicine FDA approved?

• Vandetanib received approval for use in the United States in 2011 and current indications are for symptomatic or progressive, unresectable or metastatic medullary thyroid cancer.

How should this medicine be used?

Recommended dosage:

• The recommended dose of Caprelsa is 300 mg taken orally once daily until disease progression or unacceptable toxicity occurs.
• Dosage reduction may be necessary in the event of severe toxicities or QTc interval prolongation.
• The starting dose is 200 mg in patients with moderate renal impairment.

Administration:

• Caprelsa may be taken with or without food.
• Swallow Caprelsa tablets whole with water.
• Do not crush Caprelsa tablets.
• If Caprelsa tablets are accidentally crushed, contact with skin should be avoided.
• If contact occurs, wash affected areas well with water.

If you cannot swallow Caprelsa tablets whole:

• place your dose of Caprelsa in a glass that contains 2 ounces of noncarbonated water (no other liquids should be used).
• stir the Caprelsa tablet(s) and water mixture for about 10 minutes or until the tablet(s) are in very small pieces (the tablets will not completely dissolve).
• swallow Caprelsa and water mixture right away.
• if any Caprelsa and water mixture remains in the glass, mix with an additional 4 ounces of noncarbonated water and swallow the mixture to make sure that you take your full dose of Caprelsa.

If you miss a dose and your next dose is in:

• less than 12 hours, take your next dose at the normal time.
• Do not make up for the missed dose.
• 12 hours or more, take the missed dose as soon as you remember.
• Take the next dose at the normal time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 100 mg and 300 mg tablets

This medicine is available in fallowing brand namesː

• Caprelsa

What side effects can this medication cause?

The most common side effects of this medicine include:

• rash
• acne
• high blood pressure
• nausea
• headache
• upper respiratory tract infections
• decreased appetite
• stomach-area (abdominal) pain

Caprelsa may cause serious side effects, including:

• QT prolongation
• Severe skin reactions
• interstitial lung disease
• Stroke
• Bleeding
• Heart failure
• Diarrhea
• Thyroid hormones
• hypertension
• Reversible Posterior Leukoencephalopathy Syndrome
• Kidney problems
• Wound healing problems

What special precautions should I follow?

• Caprelsa can prolong the QT interval in a concentration-dependent manner. Monitor electrocardiograms and levels of serum potassium, calcium, magnesium and TSH. Reduce Caprelsa dose as appropriate.
• Severe and sometimes fatal skin reactions, including toxic epidermal necrolysis (TEN) and Stevens-Johnson syndrome, have occurred in patients treated with Caprelsa. Permanently discontinue Caprelsa for severe skin reactions and refer the patient for urgent medical evaluation. Photosensitivity reactions can occur during Caprelsa treatment and up to 4 months after treatment discontinuation.
• Interstitial Lung Disease (ILD) or pneumonitis, including fatalities, has occurred in patients treated with Caprelsa. Interrupt Caprelsa for acute or worsening pulmonary symptoms. Discontinue Caprelsa if ILD is confirmed.
• Ischemic cerebrovascular events, including fatalities, occurred in patients treated with Caprelsa. Discontinue Caprelsa in patients who experience a severe ischemic cerebrovascular event.
• Serious hemorrhagic events, including fatalities, occurred in patients treated with Caprelsa. Discontinue Caprelsa in patients with severe hemorrhage.
• Heart failure, including fatalities, occurred in patients treated with Caprelsa. Consider discontinuation of Caprelsa in patients with heart failure. Heart failure may not be reversible upon stopping Caprelsa.
• Diarrhea of Grade 3 or greater severity occurred in 11% of patients receiving Caprelsa. Interrupt Caprelsa for severe diarrhea. Upon improvement, resume Caprelsa at a reduced dose.
• Obtain Thyroid-stimulating hormone (TSH) at baseline, at 2 to 4 weeks and 8 to 12 weeks after starting treatment with Caprelsa, and every 3 months thereafter. If signs or symptoms of hypothyroidism occur, examine thyroid hormone levels and adjust thyroid replacement therapy accordingly.
• Hypertension, including hypertensive crisis, has occurred in patients treated with Caprelsa. If hypertension cannot be controlled, do not resume Caprelsa.
• Reversible posterior leukoencephalopathy syndrome (RPLS), a syndrome of subcortical vasogenic edema diagnosed by an MRI of the brain, has occurred in patients treated with Caprelsa. Discontinue Caprelsa treatment in patients with RPLS.
• Renal failure occurred in patients treated with Caprelsa. Vandetanib is not recommended for use in patients with severe renal impairment.
• Caprelsa is not recommended for use in patients with moderate and severe hepatic impairment, as safety and efficacy have not been established.
• Impaired wound healing has occurred in patients treated with Caprelsa. Do not administer Caprelsa for at least 2 weeks following major surgery and until adequate wound healing.
• Based on its mechanism of action, Caprelsa can cause fetal harm when administered to a pregnant woman. Advise women of the potential hazard to a fetus. Advise women of reproductive potential to use effective contraception during treatment with Caprelsa and for at least 4 months following the last dose.
• Advise women not to breastfeed during treatment with Caprelsa and for 4 months after the last dose.
• Vandetanib therapy is commonly associated with transient elevations in serum aminotransferase during therapy, but has not been linked to cases of clinically apparent acute liver injury with jaundice. 

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• QTc prolongation

Management of overdosage:

• In the event of an overdose, monitor patients closely for QTc prolongation.
• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

Based on its mechanism of action, Caprelsa can cause fetal harm when administered to a pregnant woman. Advise pregnant women of the potential risk to a fetus.

Can this medicine be used in children?

• Safety and efficacy of Caprelsa in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient: vandetanib Inactive ingredients:

• Tablet core: calcium hydrogen phosphate dihydrate, microcrystalline cellulose, crospovidone, povidone, and magnesium stearate
• Tablet film-coat: hypromellose 2910, macrogol 300, and titanium dioxide

Who manufactures and distributes this medicine?

Manufactured for:

• Genzyme Corporation, Cambridge, MA
• Caprelsa is a registered trademark of Genzyme Corporation.

What should I know about storage and disposal of this medication?

• Store Caprelsa tablets at room temperature between 68°F and 77°F (20°C and 25°C).
• Safely throw away medicine that is out of date or that you no longer need.

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• Dailymed label info on Vandetanib
• FDA Vandetanib

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