Pegloticase

What is Pegloticase?

• Pegloticase (KRYSTEXXA) is a PEGylated uric acid specific enzyme used to treat patients with chronic refractory and symptomatic gout.

Dual Energy CT images with gout tophi shown in green

PegUricase

What are the uses of this medicine?

• Pegloticase (KRYSTEXXA) is a prescription medicine used in adults to help reduce the signs and symptoms of gout that are not controlled by other treatments.
• People with gout have too much uric acid in their bodies.
• Uric acid crystals collect in joints, kidneys, and other organs.
• This may cause pain, redness and swelling (inflammation).
• KRYSTEXXA works to lower blood levels of uric acid.

How does this medicine work?

• Pegloticase (peg loe’ ti kase) is a recombinant DNA-produced form of the porcine enzyme uricase that metabolizes urate to allantoin, an inert and water soluble purine metabolite that, unlike uric acid, is rapidly cleared by the kidney.
• Infusions of pegloticase decrease serum uric acid concentrations and can alleviate the symptoms and complications of gout.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• have a rare blood problem called glucose 6-phosphate dehydrogenase (G6PD) deficiency or favism.

What drug interactions can this medicine cause?

• No studies of interactions of KRYSTEXXA with other drugs have been conducted.

Is this medicine FDA approved?

• It was approved in the United States in 2010, after two clinical trials found it lowered uric acid levels and reduced deposits of uric acid crystals in joints and soft tissue.

How should this medicine be used?

Recommended dosage:

• The recommended dose and regimen of KRYSTEXXA for adult patients is 8 mg (uricase protein) given as an intravenous infusion every two weeks.

Administration:

• You will receive KRYSTEXXA through a needle in your vein (i.v. infusion).
• Your treatment will take about 2 hours or sometimes longer. A doctor or nurse will give you the treatment.
• You will receive KRYSTEXXA every 2 weeks.
• If you have side effects, your doctor may stop or slow the infusion and may give you medicine to help the side effects.
• A doctor or nurse will watch you for side effects while you receive KRYSTEXXA and for some time afterwards.
• Your doctor may stop your KRYSTEXXA if your uric acid levels do not become normal and stay controlled or you have certain side effects.
• Your gout flares may increase in the first 3 months when you start receiving KRYSTEXXA.
• Do not stop receiving KRYSTEXXA even if you have a flare as the amount of flares will decrease after 3 months of treatment.
• Your doctor may give you other medicines to help reduce your gout flares for the first few months after starting KRYSTEXXA.

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

This medicine is available in fallowing doasage form:

• As KRYSTEXXA (pegloticase) Injection, for intravenous infusion

This medicine is available in fallowing brand namesː

• KRYSTEXXA

What side effects can this medication cause?

The most common side effects of this medicine include:

• gout flares
• allergic reactions
• bruising
• sore throat
• constipation
• chest pain
• vomiting

KRYSTEXXA may cause serious side effects:

• allergic reactions can be life threatening

What special precautions should I follow?

• Anaphylaxis occurred in patients treated with KRYSTEXXA. Anaphylaxis may occur with any infusion, including a first infusion, and generally manifests within 2 hours of the infusion. However, delayed-type hypersensitivity reactions have also been reported. KRYSTEXXA should be administered in healthcare settings and by healthcare providers prepared to manage anaphylaxis. Patients should be pre-medicated with antihistamines and corticosteroids. Patients should be closely monitored for an appropriate period of time for anaphylaxis after administration of KRYSTEXXA.
• Infusion reactions occurred in patients treated with KRYSTEXXA. KRYSTEXXA should be administered in a healthcare setting and by healthcare providers prepared to manage infusion reactions. Patients should be pre-medicated with antihistamines and corticosteroids. Monitor patients closely for signs and symptoms of infusion reactions. In the event of an infusion reaction, the infusion should be slowed, or stopped and restarted at a slower rate. If a severe infusion reaction occurs, discontinue infusion and institute treatment as needed. The risk of an infusion reaction is higher in patients who have lost therapeutic response.
• An increase in gout flares is frequently observed upon initiation of anti-hyperuricemic therapy, including treatment with KRYSTEXXA. If a gout flare occurs during treatment, KRYSTEXXA need not be discontinued. Gout flare prophylaxis (i.e., non-steroidal anti-inflammatory drugs [NSAID] or colchicine upon initiation of treatment) is recommended for at least the first 6 months of therapy unless medically contraindicated or not tolerated.
• KRYSTEXXA has not been formally studied in patients with congestive heart failure, but some patients in clinical trials experienced exacerbation. Exercise caution when using KRYSTEXXA in patients who have congestive heart failure and monitor patients closely following infusion.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• No reports of overdosage with KRYSTEXXA have been reported.

Management of overdosage:

• Patients suspected of receiving an overdose should be monitored, and general supportive measures should be initiated as no specific antidote has been identified.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• KRYSTEXXA should be used during pregnancy only if clearly needed.

Can this medicine be used in children?

• The safety and effectiveness of KRYSTEXXA in pediatric patients less than 18 years of age have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: pegloticase
• Inactive ingredients: disodium hydrogen phosphate dihydrate, sodium chloride, sodium dihydrogen phosphate dihydrate, and water for injection.

Who manufactures and distributes this medicine?

Manufactured by: Savient Pharmaceuticals, Inc. 400 Crossing Boulevard Bridgewater, NJ

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

• Before the preparation for use, KRYSTEXXA must be stored in the carton and maintained at all times under refrigeration between 2° to 8°C (36° to 46°F).
• Protect from light.
• Do not shake or freeze.

The following drugs are considered antigout medications:

• Allopurinol
• Benzbromarone
• Colchicine
• Febuxostat
• Lesinurad
• Pegloticase
• Probenecid
• Rasburicase

• Dailymed label info on Pegloticase
• FDA Pegloticase