[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/) › Carfilzomib

# 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.

Updated Nov 1, 2026

## Quick facts

**Group**
[Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/)

**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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Clinical What the labels mean

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

✂**26S proteasome, chymotrypsin-like site (β5 subunit of the 20S core)**Carfilzomib

ⓘ No public structure shows carfilzomib on the human proteasome. The figure shows bortezomib, which blocks the same active sites, in the human 20S core.

**Target in 3D:** 26S proteasome, chymotrypsin-like site (β5 subunit of the 20S core). PDB structure 5LF3 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/5LF3) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/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

### Serious (rare, important)

- Heart toxicity: heart failure, ischaemia and arrhythmias
- Acute kidney injury and dehydration
- Lung toxicity and severe shortness of breath
- High blood pressure, liver toxicity and venous blood clots
- Infusion reactions up to a day after the dose; bleeding from low platelets

## 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.

## Memory aid

CARfilzomib: think CARdiac first — heart, blood pressure, kidneys and lungs are checked before every dose.

## 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.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/carfilzomib/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## What the labels mean

**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…

## Connections

## Related drugs 3

- [Bortezomib](https://durgical.com/en/pharmacology/bortezomib/)
- [Ixazomib](https://durgical.com/en/pharmacology/ixazomib/)
- [Lenalidomide](https://durgical.com/en/pharmacology/lenalidomide/)

## Related conditions 1

- [Multiple myeloma](https://durgical.com/en/conditions/multiple-myeloma/)

[← Back to the class: Other antineoplastics (differentiating agents, asparaginases, proteasome inhibitors)](https://durgical.com/en/pharmacology/classes/other-antineoplastics/)

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](https://medlineplus.gov/druginfo/meds/a612031.html) (MedlinePlus (U.S. National Library of Medicine), 2022); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L01XG02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [Human 20S proteasome complex with Bortezomib at 2.1 Angstrom](https://www.rcsb.org/structure/5LF3) (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.

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Source: https://durgical.com/en/pharmacology/carfilzomib/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/carfilzomib/