What is Carfilzomib
- Carfilzomib (Kyprolis) a proteasome inhibitor used alone or with other drugs to treat multiple myeloma that has gotten worse or came back after treatment with other anticancer therapy.
- It is also being studied in the treatment of other types of cancer.
- Kyprolis blocks the action of enzymes called proteasomes, which may help keep cancer cells from growing and may kill them.
- It is a type of proteasome inhibitor.
What are the uses of this medicine?
- Kyprolis is used as a single agent for the treatment of adult patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
How does this medicine work?
- Carfilzomib (kar filz’ oh mib) is an orally available, small molecule inhibitor of the 26S proteasome, the intracellular complex that degrades proteins involved in cell signaling and cell cycle regulation.
- Blocking proteasome activity prevents activation of factors involved in cell growth and resistance to chemotherapy induced apoptosis, leading to cancer cell death.
- Carfilzomib was the second proteasome inhibitor developed as an antineoplastic agent, differing from the initial (bortezomib) in being an irreversible inhibitor and not being metabolized by the CYP 3A4 system.
- Clinical trials of carfilzomib in patients with multiple myeloma showed at least partial responses in patients who were resistant to other antineoplastic agents including bortezomib.
Who Should Not Use this medicine ?
- This medicine have no usage limitations.
What drug interactions can this medicine cause?
- No formal drug interaction studies have been conducted with Kyprolis.
Is this medicine FDA approved?
- Carfilzomib received accelerated approval for use in the United States in 2012 for therapy of previously treated, refractory or relapsing multiple myeloma.
How should this medicine be used?
- Hydrate prior to and following Kyprolis as needed.
- Monitor serum potassium levels regularly during treatment with Kyprolis
- Premedicate with the recommended dose of dexamethasone for monotherapy or dexamethasone administered as part of the combination therapy.
- Provide thromboprophylaxis for patients being treated with Kyprolis in combination with other therapies.
- Consider antiviral prophylaxis to decrease the risk of herpes zoster reactivation.
- The typical starting dose is 20 mg per meter-squared per day intravenously for two days each week for 3 weeks, and then in cycles after a rest period. It is typically administered with dexamethasone with or without lenalidomide.
- Visually inspect for particulate matter and discoloration prior to administration. The reconstituted product should be a clear, colorless solution and should not be administered if any discoloration or particulate matter is observed.
- Discard any unused portion left in the vial. DO NOT pool unused portions from the vials. DO NOT administer more than one dose from a vial.
- Administer Kyprolis directly by intravenous infusion or in a 50 mL to 100 mL intravenous bag containing 5% Dextrose Injection, USP. Do not administer as an intravenous push or bolus.
- When administering in an intravenous bag, use a 21-gauge or larger gauge needle (0.8 mm or smaller external diameter needle) to withdraw the calculated dose from the vial and dilute into 50 mL or 100 mL intravenous bag containing only 5% Dextrose Injection, USP (based on the calculated total dose and infusion time).
- Flush the intravenous administration line with normal saline or 5% Dextrose Injection, USP immediately before and after Kyprolis administration.
- Do not mix Kyprolis with or administer as an infusion with other medicinal products.
What are the dosage forms and brand names of this medicine?
This medicine is available in fallowing doasage form:
- As injection: 10 mg, 30 mg or 60 mg lyophilized powder in single-dose vial for reconstitution.
This medicine is available in fallowing brand namesː
What side effects can this medication cause?
The most common adverse reactions of Kyprolis in monotherapy trials:
- anemia, fatigue, thrombocytopenia, nausea, pyrexia, dyspnea, diarrhea, headache, cough, edema peripheral.
The most common adverse reactions when Kyprolis used in the combination therapy:
- anemia, diarrhea, fatigue, hypertension, pyrexia, upper respiratory tract infection, thrombocytopenia, cough, dyspnea, and insomnia.
What special precautions should I follow?
- New onset or worsening of pre-existing cardiac failure (e.g., congestive heart failure, pulmonary edema, decreased ejection fraction), cardiomyopathy, myocardial ischemia, and myocardial infarction including fatalities have occurred following administration of Kyprolis. Monitor for signs and symptoms of cardiac failure or ischemia. Withhold Kyprolis and evaluate promptly.
- Cases of acute renal failure have occurred in patients receiving Kyprolis. Monitor serum creatinine regularly.
- Cases of TLS, including fatal outcomes, have been reported in patients who received Kyprolis. Administer pre-treatment hydration. Monitor for TLS, including uric acid levels and treat promptly.
- Acute Respiratory Distress Syndrome (ARDS) and acute respiratory failure have occurred in approximately 2% of patients who received Kyprolis. Withhold Kyprolis and evaluate promptly.
- Pulmonary arterial hypertension was reported in approximately 2% of patients who received Kyprolis. Withhold Kyprolis and evaluate.
- Dyspnea was reported in 25% of patients treated with Kyprolis. For severe or life-threatening dyspnea, withhold Kyprolis and evaluate.
- Hypertension, including hypertensive crisis and hypertensive emergency, has been observed with Kyprolis. Monitor blood pressure regularly. If hypertension cannot be controlled, interrupt treatment with Kyprolis.
- Venous thromboembolic events (including deep venous thrombosis and pulmonary embolism) have been observed with Kyprolis. Thromboprophylaxis is recommended.
- Infusion-related reactions, including life-threatening reactions, have occurred in patients receiving Kyprolis. Premedicate with dexamethasone.
- Fatal or serious cases of hemorrhage have been reported in patients treated with Kyprolis.
- Kyprolis causes thrombocytopenia. Monitor platelet counts; interrupt or reduce Kyprolis dosing as clinically indicated.
- Cases of hepatic failure, including fatal cases, have been reported (2%) during treatment with Kyprolis. Monitor liver enzymes regularly. Withhold Kyprolis if suspected.
- Cases of thrombotic microangiopathy, including thrombotic thrombocytopenic purpura/ hemolytic uremic syndrome (TTP/HUS), have been reported in patients who received Kyprolis. Monitor for signs and symptoms. Discontinue Kyprolis if suspected.
- Cases of posterior reversible encephalopathy syndrome (PRES) have been reported in patients receiving Kyprolis. Consider neuro-radiological imaging (MRI) for onset of visual or neurological symptoms; discontinue Kyprolis if suspected.
- Progressive multifocal leukoencephalopathy (PML), which can be fatal, has been reported with Kyprolis. Consider PML if new or worsening neurologic manifestations. Discontinue Kyprolis in patients who develop PML.
- Based on the mechanism of action and findings in animals, Kyprolis can cause fetal harm when administered to a pregnant woman.
- Increased Fatal and Serious Toxicities in Combination with Melphalan and Prednisone in Newly Diagnosed Transplant-Ineligible Patients
What to do in case of emergency/overdose?
Symptoms of overdosage may include:
Management of overdosage:
- There is no known specific antidote for Kyprolis overdosage.
- In the event of overdose, monitor patients for adverse reactions and provide supportive care as appropriate.
Can this medicine be used in pregnancy?
- Kyprolis can cause fetal harm based on findings from animal studies and its mechanism of action.
- There are no available data on Kyprolis use in pregnant women to evaluate for drug-associated risks.
Can this medicine be used in children?
- The safety and effectiveness of Kyprolis in pediatric patients have not been established.
What are the active and inactive ingredients in this medicine?
- BETADEX SULFOBUTYL ETHER SODIUM
- ANHYDROUS CITRIC ACID
- SODIUM HYDROXIDE
Who manufactures and distributes this medicine?
- Manufactured for:
Onyx Pharmaceuticals, Inc. One Amgen Center Drive Thousand Oaks, CA U.S.A.
What should I know about storage and disposal of this medication?
- Unopened vials should be stored refrigerated 2°C to 8°C (36°F to 46°F). Retain in original package to protect from light.
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Reviews for Carfilzomib
Learn more about Carfilzomib
- Dailymed label info on Carfilzomib
- Scientific articles
- Drug portal Carfilzomib
- toxicity info on Carfilzomib
- FDA Carfilzomib