Pronunciation:

AY-doh tras-TOOZ-oo-mab em-TAN-seen

Brand Names:

• Kadcyla

Dosage Forms:

• Powder for Solution

Warnings:

Do not substitute ado-trastuzumab emtansine with or for trastuzumab. Hepatotoxicity, liver failure, reductions in left ventricular ejection fraction, and death have occurred in ado-trastuzumab emtansine-treated patients. Monitor hepatic function and left ventricular function before beginning treatment and before each dose. Modify, hold, or discontinue treatment as necessary. Exposure to ado-trastuzumab emtansine during pregnancy can result in embryo-fetal harm. Advise patients of these risks and the need for effective contraception .

Classifications:

Therapeutic—

Antineoplastic Agent

Pharmacologic—

Antibody Drug Conjugate

Uses of This Medicine:

Ado-trastuzumab emtansine injection is used to treat HER2-positive metastatic breast cancer (cancer that has spread) in patients who have previously received other medicines (eg, trastuzumab, taxane medicine) that did not work well or whose cancer has returned during or within 6 months of completing treatment. It is also used as additional treatment in patients with HER2-positive early breast cancer who have cancer left after a taxane medicine and trastuzumab-based treatment.

HER2 protein is produced by some breast tumors. Ado-trastuzumab emtansine interferes with the growth of this protein which also prevents tumor growth. The tumor cells will then be destroyed by the body.

This medicine is to be given only by or under the immediate supervision of your doctor.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of ado-trastuzumab emtansine injection in the pediatric population. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of ado-trastuzumab emtansine injection in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are receiving this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Atazanavir
• Boceprevir
• Clarithromycin
• Cobicistat
• Conivaptan
• Idelalisib
• Indinavir
• Itraconazole
• Ketoconazole
• Lopinavir
• Nefazodone
• Nelfinavir
• Posaconazole
• Ritonavir
• Saquinavir
• Telaprevir
• Telithromycin
• Tipranavir
• Voriconazole

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Bleeding problems or
• Heart failure, history of or
• Interstitial lung disease or
• Liver disease or
• Peripheral neuropathy (nerve disorder) or
• Pneumonitis (lung disease) or
• Thrombocytopenia (low platelets in the blood)—Use with caution. May make these conditions worse.

• Kidney disease, severe—Use with caution. The effects may be increased because of the slower removal of the medicine from the body.

• Liver disease, severe—Use has not been studied in patients with this condition.

Proper Use of This Medicine:

Medicines used to treat cancer are very strong and can have many side effects. Before receiving this medicine, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.

A doctor or other trained health professional will give you this medicine in a medical facility. It is given through a needle placed into one of your veins. The medicine must be given slowly, so the needle will have to stay in place for at least 30 to 90 minutes. The injection is usually given once every 3 weeks.

Precautions While Using This Medicine:

It is very important that your doctor check your progress closely while receiving the medicine and at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to receive it. Blood tests may be needed to check for unwanted effects.

Receiving this medicine while you are pregnant can harm your unborn baby. It may also cause birth defects if the father is receiving it when his sexual partner becomes pregnant. Female patients should use effective birth control during treatment with this medicine and for 7 months after the last dose. Male patients who have female partners should use effective birth control during treatment with this medicine and for 4 months after the last dose. If you think you have become pregnant while receiving the medicine, tell your doctor right away.

Check with your doctor right away if you have pain or tenderness in the upper right stomach, pale stools, dark urine, loss of appetite, nausea, vomiting, or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may cause heart failure. Your doctor may test your heart before and during treatment. Contact your doctor right away if you have chest pain, increased coughing, trouble breathing, rapid weight gain, or swelling in your ankles or legs. These could be symptoms of heart failure.

Tell your doctor right away if you are having shortness of breath, chest tightness, or any type of breathing problem while receiving this medicine. These could be symptoms of a serious lung problem.

Ado-trastuzumab emtansine may cause a serious infusion reaction, which can be life-threatening and requires immediate medical attention. Tell your doctor or nurse right away if you have a fever, chills, chest pain, fast or uneven heartbeat, lightheadedness, dizziness, fainting, headache, rash, trouble breathing, or weakness while you receive the medicine or after the infusion.

This medicine can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection. It can also lower the number of platelets, which are necessary for proper blood clotting. If this occurs, there are certain precautions you can take, especially when your blood count is low, to reduce the risk of infection or bleeding:

• If you can, avoid people with infections. Check with your doctor immediately if you think you are getting an infection or if you get a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.
• Check with your doctor immediately if you notice any unusual bleeding or bruising, black, tarry stools, blood in the urine or stools, or pinpoint red spots on your skin.
• Be careful when using a regular toothbrush, dental floss, or toothpick. Your medical doctor, dentist, or nurse may recommend other ways to clean your teeth and gums. Check with your medical doctor before having any dental work done.
• Do not touch your eyes or the inside of your nose unless you have just washed your hands and have not touched anything else in the meantime.
• Be careful not to cut yourself when you are using sharp objects such as a safety razor or fingernail or toenail cutters.
• Avoid contact sports or other situations where bruising or injury could occur.

Check with your doctor right away if you are having burning, numbness, tingling, or painful sensations in the arms, hands, legs, or feet. These could be symptoms of a condition called peripheral neuropathy.

Talk with your doctor before receiving this medicine if you plan to have children. Some men and women who receive this medicine have become infertile (unable to have children).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

More common

Black, tarry stools

bladder pain

bleeding gums

bloating or swelling of the face, arms, hands, lower legs, or feet

bloody or cloudy urine

blurred vision

burning, numbness, tingling, or painful sensations

chills

cough

decreased urine

difficult or labored breathing

difficult, burning, or painful urination

dizziness

dry mouth

fever

frequent urge to urinate

headache

increased thirst

irregular heartbeat

loss of appetite

lower back or side pain

mood changes

muscle pain or cramps

nausea

nervousness

nosebleeds

numbness or tingling in the hands, feet, or lips

pale skin

pinpoint red spots on the skin

pounding in the ears

rapid weight gain

seizures

slow or fast heartbeat

sore throat

stomach pain

tightness in the chest

troubled breathing with exertion

ulcers, sores, or white spots in the mouth

unsteadiness or awkwardness

unusual bleeding or bruising

unusual tiredness or weakness

unusual weight gain or loss

vomiting

weakness in the arms, hands, legs, or feet

Less common

Chest pain

dilated neck veins

extreme tiredness or weakness

general feeling of discomfort or illness

irregular breathing

skin rash

thickening of bronchial secretions

Rare

Dark urine

general feeling of tiredness or weakness

light-colored stools

stomach bloating

vomiting blood

yellow eyes or skin

Incidence not known

Agitation

confusion

decreased awareness or responsiveness

depression

hostility

irritability

itching

joint pain, stiffness, or swelling

loss of consciousness

muscle twitching

severe sleepiness

stomach tenderness or cramps

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

Belching

change in taste

constipation

diarrhea

difficulty with moving

heartburn

indigestion

lack or loss of strength

loss of taste

muscle stiffness

stomach discomfort or upset

swelling or inflammation of the mouth

trouble sleeping

Less common

Burning, dry, or itching eyes

discharge or excessive tearing

redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.