carfilzomib
Carfilzomib (Kyprolis) is a proteasome inhibitor that blocks the cell's waste-disposal system. Cancer cells, especially multiple myeloma cells, produce large amounts of waste proteins; when the proteasome is blocked, these waste proteins build up and the cancer cells die. It is used alone or in combination to treat multiple myeloma.
This page is based on EMA and FDA prescribing information for carfilzomib injection, cross-checked with DailyMed and the National Cancer Institute dictionary; the mechanism is explained in plain language, and analogies are used only where they stay accurate.
How it works
Explains what the medicine does in the body, not dosing, side effects, or safety.
An analogy
Every cell has a recycling center called the proteasome that breaks down old or damaged proteins. Cancer cells, especially myeloma cells, produce so many proteins that they depend heavily on this recycling system. Carfilzomib jams the recycling center, so waste proteins pile up inside the cancer cell and it dies from the buildup.
In simple terms
Carfilzomib blocks the action of the proteasome, a structure inside cells that breaks down old or damaged proteins. Multiple myeloma cells produce large amounts of abnormal proteins and rely heavily on the proteasome to clear them away. When carfilzomib blocks the proteasome, these waste proteins build up inside the cancer cells, causing them to stop growing and die. Carfilzomib is used to treat multiple myeloma, a cancer of plasma cells in the bone marrow. It can be used alone or in combination with other medicines such as lenalidomide, dexamethasone, daratumumab, or isatuximab.
In depth
Carfilzomib is a tetrapeptide epoxyketone that irreversibly inhibits the chymotrypsin-like activity of the 20S catalytic core subunit of the 26S proteasome. The proteasome is a large protein complex responsible for degrading polyubiquitinated proteins and regulating key cellular processes including cell cycle progression and apoptosis. Inhibition of proteasomal activity leads to accumulation of polyubiquitinated proteins, disruption of protein homeostasis, activation of stress pathways, and induction of apoptosis. Carfilzomib forms an irreversible adduct with the proteasome active site, resulting in sustained proteasome inhibition. Multiple myeloma cells are particularly sensitive to proteasome inhibition due to their high rate of immunoglobulin production. Carfilzomib is indicated for relapsed or refractory multiple myeloma as monotherapy or in combination regimens.
See it in motion
A schematic animation of the mechanism — simplified for clarity, not drawn to scale.
Multiple myeloma cells produce large amounts of abnormal proteins and rely heavily on the proteasome to clear them away.
- Every cell has a recycling center called the proteasome that breaks down old or damaged proteins.
- Cancer cells, especially myeloma cells, produce so many proteins that they depend heavily on this recycling system.
- Carfilzomib jams the recycling center, so waste proteins pile up inside the cancer cell and it dies from the buildup.
- Carfilzomib is used to treat multiple myeloma, a cancer of plasma cells in the bone marrow.
Target: 20S proteasome
A large protein complex that degrades unneeded or damaged proteins; inhibition leads to accumulation of polyubiquitinated proteins, triggering cell cycle arrest and apoptosis in cancer cells.
Approved uses
Approved uses differ by country and change over time. Always follow your local prescribing information.
Approved uses in European Union
EMA- Kyprolis in combination with daratumumab and dexamethasone, with lenalidomide and dexamethasone, or with dexamethasone alone is indicated for the treatment of adult patients with multiple myeloma who have received at least one prior therapy
Approved uses in United States
FDA- Kyprolis is indicated for the treatment of adult patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy in combination with lenalidomide and dexamethasone; or dexamethasone; or daratumumab and dexamethasone; or daratumumab and hyaluronidase-fihj and dexamethasone; or isatuximab and dexamethasone
- Kyprolis is indicated 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
Approved uses in United States
DailyMed- Kyprolis is indicated for the treatment of adult patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy in combination with lenalidomide and dexamethasone; or dexamethasone; or daratumumab and dexamethasone; or daratumumab and hyaluronidase-fihj and dexamethasone; or isatuximab and dexamethasone
- Kyprolis is indicated 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
Official sources
The statements on this page trace back to these records.
- Kyprolis (carfilzomib) — Summary of product characteristics and package leaflet, English version
European Medicines Agency
- U.S. Food and Drug Administration: carfilzomib prescribing information
U.S. Food and Drug Administration
- DailyMed: carfilzomib labeling
DailyMed, U.S. National Library of Medicine
- National Cancer Institute: carfilzomib
National Cancer Institute
This page explains how the medicine works — it isn’t the patient leaflet. For anything that applies to you, read the leaflet that came with your medicine or ask your pharmacist.
MedUnfold provides educational content and is not medical advice. Always follow your local prescribing information and healthcare professional.