Belimumab

What is Belimumab?

• Belimumab (Benlysta) is a B-lymphocyte stimulator (BLyS)-specific inhibitor used in the therapy of systemic lupus erythematous.

Belimumab 5Y9K

Belimumab 5Y9K binding BAFF homotrimer

What are the uses of this medicine?

• Belimumab (Benlysta) is used to treat people with active systemic lupus erythematosus (SLE or lupus) or active lupus nephritis (lupus-related kidney inflammation), who are receiving other lupus medicines.
• Benlysta contains belimumab which is in a group of medicines called monoclonal antibodies.
• Lupus is a disease of the immune system (the body system that fights infection). When given together with other medicines for lupus, Benlysta decreases lupus disease activity more than other lupus medicines alone.

Limitations of use:

• It is not known if Benlysta is safe and effective in people with severe active central nervous system lupus.
• It is not known if Benlysta is safe and effective for use in children under 5 years of age when given in a vein (intravenously).
• It is not known if Benlysta is safe and effective for use in children under 18 years of age when given under the skin (subcutaneously).

How does this medicine work?

• Belimumab (be lim’ ue mab) is a human monoclonal IgG1 antibody to the B-lymphocyte stimulator (BLyS, B cell activating factor), a growth factor required for B cell activation, survival, maturation into plasma cells and immunoglobulin production.
• Belimumab binds to soluble BLyS and blocks its binding to B cell receptors, which results in a depletion of activated B cells.
• This monoclonal antibody has been shown to be effective in reducing disease activity in patients with systemic lupus erythematosus, a disease marked by elevated levels of soluble BLyS, B cell dysregulation and production of pathogenic autoantibodies and immune complexes.

Who Should Not Use this medicine ?

This medicine cannot be used:

• are allergic to belimumab or any of the ingredients in Benlysta.

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.

Be sure to mention any of the following:

• intravenous cyclophosphamide
• monoclonal antibodies or other biologic medications.

Is this medicine FDA approved?

• Belimumab was approved for use in the United States in 2011 and current indications are for treatment of adult patients with active, autoantibody positive systemic lupus erythematosus (SLE) who are receiving standard therapy.

How should this medicine be used?

Recommended dosage: Intravenous Dosage for Adult and Pediatric Patients with SLE or Lupus Nephritis:

• 10 mg/kg at 2‑week intervals for the first 3 doses and at 4‑week intervals thereafter.
• Reconstitute, dilute, and administer as an intravenous infusion over a period of 1 hour.
• Consider prophylactic premedication for infusion reactions and hypersensitivity reactions.

Subcutaneous Dosage for Adults with SLE:

• 200 mg once weekly.

Subcutaneous Dosage for Adults with Lupus Nephritis:

• 400 mg (two 200-mg injections) once weekly for 4 doses, then 200 mg once weekly thereafter.

Administration: When given in a vein (intravenously):

• You will be given Benlysta by a healthcare provider through a needle placed in a vein (IV infusion). It takes about 1 hour to give you the full dose of Benlysta.
• Your healthcare provider will tell you how often you should receive Benlysta.
• Your healthcare provider may give you medicines before you receive Benlysta to help reduce your chance of having a reaction.

When given under the skin (subcutaneously):

• Benlysta may be prescribed as a single-dose autoinjector or as a single-dose prefilled syringe.
• Before you use Benlysta, your healthcare provider will show you or your caregiver how to give the injections and review the signs and symptoms of possible allergic reactions.
• Benlysta is injected under your skin (subcutaneously) of your stomach (abdomen) or thigh.
• Use Benlysta 1 time a week on the same day each week.
• If you have lupus nephritis, one dose may be 2 injections.
• If you miss your dose of Benlysta on your planned day, inject a dose as soon as you remember.
• Then, inject your next dose at your regularly scheduled time or continue weekly dosing based on the new day injected.

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

This medicine is available in fallowing doasage form:

• As Intravenous Infusion:
• For Injection: 120 mg or 400 mg of belimumab lyophilized powder in single-dose vial for reconstitution and dilution prior to intravenous infusion.
• Subcutaneous Injection:
• Injection: 200 mg/mL of belimumab in single-dose prefilled autoinjector or single-dose prefilled syringe.

This medicine is available in fallowing brand namesː

• Benlysta

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• diarrhea
• fever
• stuffy or runny nose and sore throat (nasopharyngitis)
• persistent cough (bronchitis)
• trouble sleeping (insomnia)
• leg or arm pain
• depression
• headache (migraine)
• pain, redness, itching, or swelling at the site of injection (when given subcutaneously)

Benlysta can cause serious side effects, including:

• Progressive multifocal leukoencephalopathy (PML)
• Cancer
• Infections
• Allergic reactions
• Mental health problems and suicide

What special precautions should I follow?

• Serious and sometimes fatal infections have occurred in patients receiving immunosuppressive agents, including Benlysta. Use with caution in patients with severe or chronic infections. Consider interrupting therapy with Benlysta if patients develop a new infection during treatment with Benlysta.
• Acute hypersensitivity reactions, including anaphylaxis and death, and infusion-related reactions have been reported in association with Benlysta. Consider administering premedication as prophylaxis prior to intravenous dosing. Inform patients receiving Benlysta of the signs and symptoms of hypersensitivity reactions and instruct them to seek immediate medical care should a reaction occur.
• Cases of JC virus-associated PML resulting in neurological deficits, including fatal cases, have been reported in patients with SLE receiving immunosuppressants, including Benlysta. Evaluate patients with new-onset or deteriorating neurological signs and symptoms for PML. If confirmed, consider discontinuation of immunosuppressant therapy, including Benlysta.
• There is an increased risk of malignancies with the use of immunosuppressants. In patients who develop malignancies, consider the risk and benefit of continued treatment with Benlysta.
• Depression and suicidality were reported in trials with Benlysta. Assess for depression and risk of suicide before treatment with Benlysta and monitor during treatment. Instruct patients to contact their healthcare provider if new or worsening depression, suicidal thoughts, or other mood changes occur.
• Because of its mechanism of action, Benlysta may interfere with the response to immunizations. Live vaccines should not be given concurrently with Benlysta.
• Benlysta has not been studied in combination with other biologic therapies, including B-cell-targeted therapies. Therefore, use of Benlysta is not recommended in combination with biologic therapies.
• It is not known if Benlysta passes into your breast milk. You and your healthcare provider should talk about whether or not you should receive Benlysta and breastfeed.
• Belimumab has been linked to an uncommon incidence of transient serum enzyme elevations during therapy, but has yet to be linked to instances of clinically apparent liver injury.

What to do in case of emergency/overdose?

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?

• It is not known if Benlysta will harm your unborn baby. You should talk to your healthcare provider about whether to prevent pregnancy while on Benlysta. If you choose to prevent pregnancy, you should use an effective method of birth control while receiving Benlysta and for at least 4 months after the final dose of Benlysta.
• Tell your healthcare provider right away if you become pregnant during your treatment with Benlysta or if you think you may be pregnant.
• If you become pregnant while receiving Benlysta, talk to your healthcare provider about enrolling in the Benlysta Pregnancy Registry. You can enroll in this registry by calling 1-877-681-6296.

Can this medicine be used in children?

• It is not known if Benlysta is safe and effective for use in children under 5 years of age when given in a vein (intravenously).
• It is not known if Benlysta is safe and effective for use in children under 18 years of age when given under the skin (subcutaneously).

What are the active and inactive ingredients in this medicine?

• Active ingredient: belimumab.
• Inactive ingredients (intravenous): citric acid, polysorbate 80, sodium citrate, sucrose.
• Inactive Ingredients (subcutaneous): L-arginine hydrochloride, L-histidine, L-histidine monohydrochloride, polysorbate 80, sodium chloride.

Who manufactures and distributes this medicine?

Manufactured by:

• GlaxoSmithKline LLC
• Philadelphia, PA , U.S. License No. 1727, and

Distributed by:

• GlaxoSmithKline
• Durham, NC

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

• Store autoinjectors and prefilled syringes in the refrigerator at 36°F to 46°F (2°C to 8°C).
• Do not freeze.
• Keep Benlysta autoinjectors and prefilled syringes in the original package until time of use to protect from light.
• Do not shake.
• Keep away from heat and sunlight.
• Do not use and do not place back in the refrigerator if left out at room temperature for more than 12 hours.
• Safely throw away medicine that is out of date or no longer needed.

• Dailymed label info on Belimumab
• FDA Belimumab