Caprelsa

What Is Caprelsa?

Caprelsa (vandetanib) is a cancer medication indicated for the treatment of the latter stages of a rare form of thyroid cancer called medullary thyroid cancer.

What Are Side Effects of Caprelsa?

Common side effects of Caprelsa include:

• nausea
• diarrhea
• abdominal pain
• vomiting
• indigestion
• dry mouth
• loss of appetite
• rash
• high blood pressure
• general feeling of being unwell (malaise)
• acne
• dry skin
• skin sensitivity to sunlight
• itching
• nail abnormalities
• hair loss
• headache
• changes in taste
• fatigue
• upper respiratory tract infection
• blurred vision
• depression, and
• muscle spasms

Dosage for Caprelsa

Caprelsa (vandetanib) is available in two strengths, 100 and 300 mg tablets. Because of the potential for sudden death and cardiac problems, Caprelsa is available only through a restricted distribution program called CAPRELSA REMS Program. Only prescribers and pharmacies certified with the program are able to prescribe and dispense Caprelsa. The recommended daily dose is 300 mg of Caprelsa taken orally, with or without food.

What Drugs, Substances, or Supplements Interact with Caprelsa?

Caprelsa should not be taken with medications prescribed for a heart rhythm defect called long QT syndrome. While taking Caprelsa, patients should avoid taking St. John's wort or drugs that may prolong the QT interval. Caprelsa tablets should not be crushed. Direct contact of crushed tablets with the skin or mucous membranes should be avoided. Serious side effects include respiratory problems, heart failure, cardiac arrhythmias, hypothyroidism, and a serious infection of the blood called sepsis. Heart rhythm disorders and sudden deaths have been reported.

Caprelsa During Pregnancy and Breastfeeding

Caprelsa can cause fetal harm when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should be advised to avoid becoming pregnant during treatment with Caprelsa. Breastfeeding mothers are advised to discontinue nursing while receiving Caprelsa therapy. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Caprelsa, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Safety and efficacy of Caprelsa in pediatric patients have not been established.

Additional Information

Our Caprelsa Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication. Caprelsa tablets should not be crushed.

 

Caprelsa Consumer Information

Get emergency medical help if you have signs of an allergic reaction (hives, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).

You may need to stop taking vandetanib permanently if you have a severe skin reaction.

Call your doctor at once if you have:

• fast or pounding heartbeats, fluttering in your chest, sudden dizziness (like you might pass out);
• wheezing, dry cough, feeling short of breath;
• any wound that will not heal;
• severe or ongoing diarrhea;
• unusual bruising or bleeding;
• cough with bloody mucus, vomit that looks like coffee grounds;
• swelling, rapid weight gain;
• headache, confusion, change in mental status, seizure;
• thyroid symptoms--extreme tiredness, dry skin, joint pain or stiffness, muscle pain or weakness, hoarse voice, feeling more sensitive to cold temperatures, weight gain; or
• high blood pressure--severe headache, pounding in your neck or ears, anxiety, irregular heartbeats.

Stop using vandetanib and call your doctor at once if you have signs of a stroke:

• sudden numbness or weakness (especially on one side of the body);
• confusion, trouble speaking or understanding what is said to you;
• sudden severe headache; or
• problems with vision or balance.

Common side effects may include:

• high blood pressure;
• diarrhea, stomach pain, nausea, loss of appetite;
• headache, tiredness;
• acne, skin rash; or
• cold symptoms such as stuffy nose, sneezing, sore throat.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Caprelsa (Vandetanib)

 

Caprelsa Professional Information

SIDE EFFECTS

The following serious adverse reactions are discussed elsewhere in the label:

• QT Prolongation and Torsades de Pointes [see BOXED WARNING, WARNINGS AND PRECAUTIONS]
• Severe Skin Reactions [see WARNINGS AND PRECAUTIONS]
• Interstitial Lung Disease [see WARNINGS AND PRECAUTIONS]
• Ischemic Cerebrovascular Events [see WARNINGS AND PRECAUTIONS]
• Hemorrhage [see WARNINGS AND PRECAUTIONS]
• Heart Failure [see WARNINGS AND PRECAUTIONS]
• Diarrhea [see WARNINGS AND PRECAUTIONS]
• Hypothyroidism [see WARNINGS AND PRECAUTIONS]
• Hypertension [see WARNINGS AND PRECAUTIONS]
• Reversible Posterior Leukoencephalopathy Syndrome [see WARNINGS AND PRECAUTIONS]

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Patients with unresectable locally advanced or metastatic medullary thyroid cancer were treated with CAPRELSA 300 mg (n=231) or Placebo (n=99). The population exposed to CAPRELSA was 58% male, 94% white, and had a median age of 50 years. The data described below reflect a median exposure to CAPRELSA for 607 days.

The most commonly reported adverse drug reactions which occurred in >20% of CAPRELSA-treated patients and with a between-arm difference of ≥5% included, in order of decreasing frequency: diarrhea/colitis, rash, acneiform dermatitis, hypertension, nausea, headache, upper respiratory tract infection, decreased appetite, and abdominal pain.

Among CAPRELSA-treated patients, dose interruption occurred in 109 (47%) and dose reduction occurred in 83 (36%). Adverse reactions led to study treatment discontinuation in 28 of 231 patients (12%) receiving CAPRELSA and in 3 of 99 patients (3.0%) receiving placebo. Adverse reactions leading to permanent discontinuation in 2 or more (≥0.9%) patients treated with CAPRELSA were: asthenia (1.7%), rash (1.7%), diarrhea (0.9%), fatigue (0.9%), pyrexia (0.9%), elevated creatinine (0.9%), QT prolongation (0.9%), and hypertension (0.9%).

Table 1: Per-Patient Incidence of Selected Adverse Reactions Occurring at a Higher Incidence in CAPRELSA-Treated Patients During Randomized Treatment (Between-Arm Difference of ≥5% [All Grades]¹)

System Organ Class Preferred Term	CAPRELSA 300 mg N=231		Placebo N=99
	All Grades (%)	Grade 3-4 (%)	All Grades (%)	Grade 3-4 (%)
Gastrointestinal Disorders
Diarrhea/Colitis	57	11	27	2
Nausea	33	1	16	0
Abdominal Pain2	21	3	11	0
Vomiting	15	1	7	0
Dyspepsia	11	0	4	0
Dry Mouth	9	0	3	0
Skin and Cutaneous Disorders
Rash3	53	5	12	0
Dermatitis Acneiform/Acne	35	1	7	0
Dry Skin	15	0	5	0
Photosensitivity Reaction	13	2	0	0
Pruritus	11	1	4	0
Nail abnormalities4	9	0	0	0
Alopecia	8	N/A	0	N/A
Vascular Disorders
Hypertension/Hypertensive Crisis/Accelerated Hypertension	33	9	5	1
Nervous System Disorders
Headache	26	1	9	0
Dysgeusia	8	0	3	0
General Disorders
Fatigue5	24	6	23	1
Infections
Upper Respiratory Tract Infections6	23	0	16	0
Metabolic and Nutritional Disorders
Decreased Appetite	21	4	12	0
Hypocalcemia	11	2	3	0
Investigations
ECG QT Prolonged7	14	8	1	1
Eye Disorders
Corneal Abnormalities8	13	0	1	0
Blurred Vision	9	0	1	0
Renal Disorders
Proteinuria	10	0	2	0
Psychiatric Disorders
Depression	10	2	3	0
Endocrine Disorders
Hypothyroidism	6	0	0	0
Musculoskeletal Disorders
Muscle Spasms	6	0	1	0
1CTCAE version 3 was used to grade adverse events. 2Includes abdominal pain, abdominal pain upper, lower abdominal pain and abdominal discomfort. 3Includes rash, rash (erythematous, generalized, macular, maculopapular, papular, pruritic, and exfoliative), dermatitis, dermatitis bullous, generalized erythema, and eczema. 4Includes nail disorder, nail bed inflammation, nail bed tenderness, paronychia, nail bed infection, and nail infection. 5Included in Table 1 due to the increased incidence of severe fatigue in the CAPRELSA group compared to the placebo group. 6Includes laryngitis, nasopharyngitis, pharyngitis, sinusitis, upper respiratory tract infection, acute sinusitis, rhinitis, and tracheitis. 769% had QT prolongation >450 ms and 7% had QT prolongation >500 ms by ECG using Fridericia correction. 8Includes corneal edema, corneal opacity, corneal dystrophy, corneal pigmentation, keratopathy, arcus lipoides, corneal deposits, acquired corneal dystrophy.

Clinically important uncommon adverse drug reactions in patients who received CAPRELSA versus patients who received placebo included pancreatitis (0.4% vs. 0%) and heart failure (0.9% vs. 0%).

Blurred vision was more common in patients who received CAPRELSA versus patients who received placebo for medullary thyroid cancer (9% vs. 1%, respectively). Scheduled slit lamp examinations revealed corneal opacities (vortex keratopathies) in treated patients, which can lead to halos and decreased visual acuity. Perform ophthalmologic examination, including slit lamp examination, in patients who report visual changes.

Class Effects

CAPRELSA is an inhibitor of vascular endothelial growth factor receptor (VEGFR) signaling. Inhibition of VEGFR signaling can result in intestinal perforation. Intestinal perforation occurred in 0.4% of CAPRELSA treated patients versus 0% of placebo treated patients.

The incidence of Grade 1-2 bleeding events was 14% in patients receiving CAPRELSA compared with 7% on placebo in the randomized portion of the medullary thyroid cancer (MTC) study.

Table 2: Per-Patient Incidence of Selected Laboratory Abnormalities in Patients with MTC Occurring at a Higher Incidence in CAPRELSA-Treated Patients (Between-Arm Difference of ≥5% [All Grades]¹)

Laboratory Abnormalities	CAPRELSA 300 mg N=231		Placebo N=99
	All Grades (%)	Grade 3-4 (%)	All Grades (%)	Grade 3-4 (%)
Chemistries
Hypocalcemia	57	6	25	3
ALT Increased	51	2	19	0
Hypoglycemia	24	0	7	1
Creatinine Increased	16	0	1	0
Hypomagnesemia	7	<1	2	0
Hematologic
Neutropenia	10	<1	5	2
Thrombocytopenia	9	0	3	0
1 CTCAE version 3 was used to grade laboratory abnormalities.

No patient with a Grade 3-4 ALT elevation had a concomitant increase in bilirubin in the MTC study.

Read the entire FDA prescribing information for Caprelsa (Vandetanib)