Ocrelizumab

Mechanism of Action

Humanized monoclonal antibody designed to selectively target CD20, a cell surface antigen present on pre-B and mature B lymphocytes

Following cell surface binding to B lymphocytes, ocrelizumab results in antibody-dependent cellular cytolysis and complement-mediated lysis

Absorption

Peak plasma concentration: 212 mcg/mL (600 mg); 141 mcg/mL (300 mg)

AUC: 3510 mcg·mL/day

Distribution

Vd

• Central volume distribution: 2.78 L
• Peripheral volume compartment: 2.68 L/day
• Intercompartment: 0.29 L/day

Elimination

Terminal half-life: 26 days

Constant clearance: 0.17 L/day

Initial time-dependent clearance: 0.05 L/day (declines with a half-life of 33 wk)

Ocrelizumab is a monoclonal antibody that affects the actions of the body's immune system. Monoclonal antibodies are made to target and destroy only certain cells in the body. This may help to protect healthy cells from damage.

Ocrelizumab is used to treat multiple sclerosis (relapsing or progressive forms).

Ocrelizumab may also be used for purposes not listed in this medication guide.

Ocrelizumab may cause unpleasant side effects while the medicine is injected, or up to 24 hours later. Tell your caregivers right away if you have any unusual discomfort during the injection.

Call your doctor if you have unpleasant side effects such as dizziness, nausea, skin rash, chest tightness, or trouble breathing within 24 hours after your injection.

You should not be treated with ocrelizumab if you are allergic to it, or if you have:

• active infection with hepatitis B.

Tell your doctor if you have received any vaccine within the past 6 weeks.

To make sure ocrelizumab is safe for you, tell your doctor if you have:

• any type of active infection;
• a history of using medicine that can weaken your immune system;
• if you are a carrier of hepatitis B; or
• if you are scheduled to receive any vaccines.

Using ocrelizumab may increase your risk of developing certain types of cancer, such as breast cancer. Ask your doctor about your specific risk.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 6 months after your last dose.

It is not known whether ocrelizumab passes into breast milk or if it could affect the nursing baby. Tell your doctor if you are breast-feeding.

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Some side effects may occur during the injection or up to 24 hours later. Tell your caregiver right away if you feel dizzy, sleepy, nauseated, light-headed, feverish, sweaty, itchy, or have a red skin rash, headache, fast heartbeats, chest tightness, trouble breathing, or swelling and irritation in your throat.

Call your doctor at once if you have:

• fever, chills, cough with yellow or green mucus;
• stabbing chest pain, wheezing, feeling short of breath;
• skin warmth, redness, or swelling;
• skin sores, blisters, pus, or oozing;
• cold sores or fever blisters on or around your lips;
• nerve pain (tingling, burning pain, "pins and needles" feeling);
• any change in your mental state;
• weakness on one side of your body; or
• problems with vision, speech, or walking.

Your ocrelizumab treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

• reactions to an injection; or
• respiratory infections (affecting the nose, sinuses, throat, or lungs).

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.

Before you start treatment with ocrelizumab, your doctor may perform tests to make sure you do not have hepatitis B or other infections.

Ocrelizumab is injected into a vein through an IV. A healthcare provider will give you this injection.

You may be given other medications to prevent certain side effects of ocrelizumab.

Your first dose of ocrelizumab will be split into 2 separate infusions. You will receive these infusions 2 weeks apart. The following doses will be given once every 6 months.

Ocrelizumab must be given slowly and each infusion can take up to 3 hours and 30 minutes to complete.

You will be watched closely for at least 1 hour after receiving ocrelizumab, to make sure you do not have an allergic reaction to the medication.

If you have ever had hepatitis B, ocrelizumab can cause this condition to come back or get worse. You will need frequent blood tests to check your liver function during treatment and for several months after you stop using this medicine.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Call your doctor for instructions if you miss a dose of ocrelizumab.

You should not be treated with ocrelizumab if you are allergic to it, or if you have:

• active infection with hepatitis B.

Tell your doctor if you have received any vaccine within the past 6 weeks.

To make sure ocrelizumab is safe for you, tell your doctor if you have:

• any type of active infection;

• a history of using medicine that can weaken your immune system;

• if you are a carrier of hepatitis B; or

• if you are scheduled to receive any vaccines.

Using ocrelizumab may increase your risk of developing certain types of cancer, such as breast cancer. Ask your doctor about your specific risk.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 6 months after your last dose.

It is not known whether ocrelizumab passes into breast milk or if it could affect the nursing baby. Tell your doctor if you are breast-feeding.

Ocrelizumab, a CD20-directed cytolytic antibody, is an immunomodulatory agent.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.
• This medicine comes with an extra patient fact sheet called a Medication Guide. Read it with care. Read it again each time this medicine is refilled. If you have any questions about ocrelizumab, please talk with the doctor, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about ocrelizumab. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using ocrelizumab.

Review Date: October 4, 2017

• Anti-CD20 Monoclonal Antibody
• Monoclonal Antibody

There are no dosage adjustments provided in the manufacturer's labeling; however, no significant change in pharmacokinetics was observed in patients with renal impairment.

Commonly reported side effects of ocrelizumab include: lower respiratory tract infection, upper respiratory tract infection, cough, and infusion related reaction. See below for a comprehensive list of adverse effects.

This drug is not recommended for use in children.

Consult WARNINGS section for additional precautions.