What is carfilzomib?
People with multiple myeloma have abnormal plasma cells, which are a type of white blood cell found in your bone marrow that secrete antibodies (immunoglobulins). These antibodies are protective proteins that help fight infection. When plasma cells become cancerous they grow out of control and make an abnormal antibody.
Carfilzomib works by inhibiting the growth of myeloma cells and encouraging them to self-destruct. Myeloma cells use proteasomes to break down proteins within them. Carfilzomib blocks the action of proteasomes, causing the proteins to build up inside the cells and the cells to die.
Carfilzomib was approved by the US Food and Drug Administration (FDA) in 2012. It is a second generation proteasome inhibitor that was designed to overcome toxicity and resistance issues that some patients experienced with an older proteasome inhibitor called bortezomib (Velcade). Carfilzomib is available under the brand name Kyprolis. A generic version is also available.
What is carfilzomib used for?
Carfilzomib is a prescription medication used to treat adult patients with relapsed or refractory multiple myeloma who have received one to three previous treatments for multiple myeloma in combination with:
- Lenalidomide (Revlimid) and dexamethasone; or
- Dexamethasone; or
- Daratumumab (Darzalex) and dexamethasone; or
- Daratumumab and hyaluronidase-fihj (Darzalex Faspro) and dexamethasone
Carfilzomib is also approved for use as a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
Carfilzomib can cause serious side effects:
- Heart problems: carfilzomib can cause heart problems or worsen pre-existing heart conditions. Death due to cardiac arrest has occurred within one day of carfilzomib administration. Before starting carfilzomib, you should have a full medical work-up (including blood pressure and fluid management). You should be closely monitored during treatment.
- Kidney problems: There have been reports of sudden kidney failure in patients receiving carfilzomib. Your kidney function should be closely monitored during treatment.
- Tumor lysis syndrome (TLS): Cases of TLS have been reported in patients receiving carfilzomib, including fatalities. You should be closely monitored during treatment for any signs of TLS.
- Lung damage: Cases of lung damage have been reported in patients receiving carfilzomib, including fatal cases.
- Pulmonary hypertension (high blood pressure in the lungs): There have been reports of pulmonary hypertension in patients receiving carfilzomib.
- Lung complications: Shortness of breath was reported in patients receiving carfilzomib. Your lung function should be closely monitored during treatment.
- High blood pressure: Cases of high blood pressure, including fatal cases, have been reported in patients receiving carfilzomib. Your blood pressure should be closely monitored during treatment.
- Blood clots: There have been reports of blood clots in patients receiving carfilzomib. If you are at high risk for blood clots, your doctor can recommend ways to lower the risk. If you are using carfilzomib in combination with dexamethasone or with lenalidomide plus dexamethasone or with daratumumab and dexamethasone, your doctor should assess and may prescribe another medicine to help lower your risk for blood clots.
- If you are using birth control pills or other medical forms of birth control associated with a risk of blood clots, talk to your doctor and consider a different method of birth control during treatment with carfilzomib in combination with dexamethasone, with lenalidomide plus dexamethasone, or with daratumumab and dexamethasone.
- Infusion-related reactions: Signs and symptoms of infusion-related reactions included fever, chills, joint pain, muscle pain, facial flushing and/or swelling, swelling of the larynx (voice box), vomiting, weakness, shortness of breath, low blood pressure, fainting, chest tightness, and chest pain. These symptoms can occur immediately following infusion or up to 24 hours after administration of carfilzomib. If you experience any of these symptoms, contact your doctor immediately.
- Severe bleeding problems: Fatal or serious cases of bleeding problems have been reported in patients receiving carfilzomib. Your doctor should monitor your signs and symptoms of blood loss.
- Very low platelet count: Low platelet levels can cause unusual bruising and bleeding. You should have regular blood tests to check your platelet count during treatment.
- Liver problems: Cases of liver failure, including fatal cases, have been reported in patients receiving carfilzomib. Your liver function should be closely monitored during treatment.
- Blood problems: Cases of a blood disease called thrombotic microangiopathy, including thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), including fatal cases, have been reported in patients who received carfilzomib. Your doctor should monitor your signs and symptoms.
- Brain problems: A nerve disease called Posterior Reversible Encephalopathy Syndrome (PRES), formerly called Reversible Posterior Leukoencephalopathy Syndrome (RPLS), has been reported in patients receiving carfilzomib. It can cause seizure, headache, lack of energy, confusion, blindness, altered consciousness, and other visual and nerve disturbances, along with high blood pressure. Your doctor should monitor your signs and symptoms.
- Cases of a brain infection called Progressive Multifocal Leukoencephalopathy (PML), including fatal cases, have been reported in patients receiving carfilzomib. Your doctor should monitor your signs and symptoms.
Contact your doctor straight away if you experience any of the following while taking carfilzomib:
- Shortness of breath
- Prolonged, unusual or excessive bleeding
- Yellowing of the skin and/or eyes (jaundice)
- Headaches, confusion, seizures or loss of sight
Who should not receive carfilzomib?
Do not receive carfilzomib if you are allergic to carfilzomib or any of the ingredients in it. See below for a complete list of ingredients.
Patients taking melphalan and prednisone should not receive carfilzomib. Newly diagnosed transplant ineligible multiple myeloma patients have shown an increased risk of serious and fatal side effects when using carfilzomib in combination with melphalan and prednisone.
What should I tell my doctor before receiving carfilzomib?
Before you receive carfilzomib, tell your healthcare provider about all of your medical conditions.
How should I receive carfilzomib?
- Carfilzomib is given my a healthcare professional in a treatment center.
- Carfilzomib is administered by intravenous (IV) infusion - given via a needle in your arm.
- Your carfilzomib infusion will be delivered over 10 to 30 minutes depending on your particular treatment regimen. Check with your healthcare team about how long you'll need to spend at the treatment center before and after your infusion. You may receive other medications before your carfilzomib infusion.
- Carfilzomib is administered once or twice weekly. A typical treatment cycle if 3 weeks on treatment followed by 1 week off treatment.
- Remember to drink water before and after your treatment as instructed by your doctor
What happens if I miss a dose?
If you miss a scheduled treatment of carfilzomib contact your healthcare provider for advice.
What should I avoid while receiving carfilzomib?
- Do not drive or operate machinery if carfilzomib causes you to feel fatigued, dizzy, faint and/or makes your blood pressure drop.
- Avoid dehydration. Carfilzomib can cause nausea and vomiting, which can make dehydration worse.
The recommended dose of carfilzomib varies depending on your treatment regimen. See table below.
||20/70 mg/m2 once weekly||30|
||20/56 mg/m2 twice weekly||30|
||20/27 mg/m2 twice weekly||10|
See full prescribing information for further information about carfilzomib dosing.
What are the side effects of carfilzomib?
Carfilzomib can cause serious side effects including:
- See "Important information" above.
The most common side effects occurring in at least 20 percent of patients receiving carfilzomib in the combination therapy trials are:
- tiredness (fatigue)
- high blood pressure (hypertension)
- upper airway (respiratory tract) infection
- low platelets (thrombocytopenia)
- difficulty breathing (dyspnea)
- sleeplessness (insomnia)
The most common side effects occurring in at least 20 percent of patients receiving carfilzomib therapy alone in trials are:
- high blood pressure
- upper respiratory tract infection
- low platelets
- difficulty breathing
These are not all the possible side effects of carfilzomib. For more information, ask your doctor or pharmacist. Call your doctor for medical advice about side effects. Contact your doctor about any side effects that bother you or do not go away.
You may report side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.
Tell your healthcare provider about all the medicines you take, including prescriptions an over-the-counter medicine, vitamins, and herbal supplements. Talk to your doctor before starting any new medications during treatment with carfilzomib.
Pregnancy and breastfeeding
Tell your doctor if you are pregnant or plan to become pregnant. Carfilzomib can cause harm to a fetus (unborn baby) when given to a pregnant woman. Women should use effective contraception during treatment with carfilzomib and for 6 months following the final dose.
Men should use effective contraception during treatment with carfilzomib and for 3 months following the final dose.
Carfilzomib can cause harm to a fetus if used during pregnancy or if you or your partner become pregnant during treatment with carfilzomib.
Tell your doctor if you are breastfeeding or plan to breastfeed. Do not breastfeed while receiving carfilzomib. and for 2 weeks after the last dose. Talk to you doctor about the best way to feed your baby while receiving carfilzomib.
- Unopened vials of carfilzomib should be stored refrigerated 2°C to 8°C (36°F to 46°F).
- Retain in original package to protect from light.
What are the ingredients in carfilzomib?
Active ingredients: carfilzomib
Inactive ingredients (Kyprolis brand): betadex sulfobutyl ether sodium, anhydrous citric acid, sodium hydroxide, water
Carfilzomib is manufactured under the brand name Kyprolis by Onyx Pharmaceuticals, Inc. One Amgen Center Drive, Thousands Oaks, CA 91320-1799 U.S.A.
A generic version of carfilzomib is also made by Dr Reddy's.
Kyprolis (carfilzomib) is a type of chemotherapy drug. It works by inhibiting proteasomes - a complex of proteases (enzymes), which break down proteins in the body. Continue reading
- National Library of Medicine Kyprolis Product Label
- Jayaweera SPE, Wanigasinghe Kanakanamge SP, Rajalingam D, Silva GN. Carfilzomib: A Promising Proteasome Inhibitor for the Treatment of Relapsed and Refractory Multiple Myeloma. Front Oncol. 2021;11:740796. Published 2021 Nov 10. doi:10.3389/fonc.2021.740796
More about carfilzomib
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- Drug class: proteasome inhibitors
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