Carfilzomib
Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)
Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)High alert
An error with this medicine can cause serious harm: double checks and protocols are used.Pregnancy: avoid
Avoid in pregnancy. Can harm the fetus; a pregnancy test is done before starting, contraception is used by women and by men with partners who could become pregnant, and…
Second-generation intravenous proteasome inhibitor (an epoxyketone) for relapsed multiple myeloma. Watch the heart, kidneys, lungs and blood pressure.
Quick facts
- Group
- Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)
- Target
- 26S proteasome, chymotrypsin-like site (β5 subunit of the 20S core)
- Key effects
- Anaemia and thrombocytopenia · Diarrhoea · Headache
- Monitor
- Blood pressure · Kidney function and electrolytes
- ATC
- L01XG02
No doses: the clinician sets them by the current guideline.
Mechanism of action
No public structure shows carfilzomib on the human proteasome. The figure shows bortezomib, which blocks the same active sites, in the human 20S core.
The proteasome breaks down proteins tagged with ubiquitin, including regulators of the cell cycle and of apoptosis. Carfilzomib, a tetrapeptide epoxyketone, selectively blocks the proteasome's protein-cutting sites. Unwanted and misfolded proteins pile up; myeloma cells, which make huge amounts of antibody protein, are especially sensitive to this stress and die by apoptosis.
- Carfilzomib blocks the proteasome's protein-cutting sites
- Ubiquitin-tagged and misfolded proteins pile up
- Protein-loaded myeloma cells undergo apoptosis
Indications
- Relapsed or refractory multiple myeloma after at least one earlier therapy, alone or with dexamethasone, or with lenalidomide and dexamethasone. Multiple myeloma →
Adverse effects
Common
- Anaemia and thrombocytopenia
- Diarrhoea, nausea, constipation
- Shortness of breath and leg swelling
- Headache, muscle spasms, back and limb pain, trouble sleeping
- Fever and flu-like symptoms after the infusion
Contraindications
- No absolute contraindications in the label apart from hypersensitivity; see the warnings
Key interactions
- Lenalidomide and dexamethasone (combination regimen)
- Intended combination; the regimen is watched for venous clots, low blood counts and infection.
- Other drugs that harm the heart or kidneys
- Add to carfilzomib's cardiac and renal toxicity.
What is monitored
- Blood pressure, heart and breathing symptoms at every visit
- Kidney function and electrolytes
- Blood count (platelets)
- Liver tests; signs of leg clots
Administration and safety
- Powder mixed with liquid and infused intravenously by a doctor or nurse in a clinic.
- Medicines to prevent infusion reactions are given before each dose.
- Plenty of fluids are encouraged before and during the treatment period.
- Hazardous drug: prepared and disposed of under cytotoxic-drug procedures.
Pregnancy and breastfeeding
Avoid in pregnancy. Can harm the fetus; a pregnancy test is done before starting, contraception is used by women and by men with partners who could become pregnant, and breastfeeding is stopped.
Nursing care
- Ask about heart failure, heart attack, arrhythmia, high blood pressure, kidney disease and dialysis before starting.
- Check blood pressure and ask about breathlessness, chest pain and swelling before each dose.
- Teach to drink enough fluids, especially with vomiting or diarrhoea, and to report less urine.
- Warn that it can cause dizziness or fainting; ask about herpes infections and seizures.
Pharmacokinetics
- Absorption
- Intravenous infusion only, over a short period.
Test yourself
Think of the answer, then tap the question to see it.
Why are myeloma cells especially sensitive to proteasome inhibitors?
They make large amounts of antibody protein, so blocking protein disposal overloads them with unfolded protein and triggers apoptosis.
Which organ toxicities are watched most closely with carfilzomib?
Heart (failure, ischaemia, arrhythmia), kidneys, lungs, liver and blood pressure.
Why are patients on carfilzomib asked to drink enough fluids?
Carfilzomib can cause dehydration and acute kidney injury, especially with vomiting or diarrhoea.
Connections
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Carfilzomib Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2022); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Human 20S proteasome complex with Bortezomib at 2.1 Angstrom (RCSB Protein Data Bank, 2016).
Spotted a mistake?We are always improving for the community. Tell us what is wrong and our team will review it.Report a mistake
Representative model, for educational purposes only.