Carfilzomib is a proteasome inhibitor used either alone or in conjunction with a chemotherapy regimen to treat patients with relapsed or refractory multiple myeloma. Carfilzomib is an injectable antineoplastic agent (IV only).
- Mechanism
- Curator reviewed
Carfilzomib is made up of four modified peptides and acts as a proteasome inhibitor. Carfilzomib irreversibly and selectively binds to N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. This 20S core has 3 catalytic active sites: the chymotrypsin, trypsin, and caspase-like sites. Inhibition of the chymotrypsin-like site by carfilzomib (β5 and β5i subunits) is the most effective target in decreasing cellular proliferation, ultimately resulting in cell cycle arrest and apoptosis of cancerous cells. At higher doses, carfilzomib will inhibit the trypsin-and capase-like sites.
- Primary indication
- Carfilzomib 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...Curator reviewed · 8 structured indications
- Formula / weight
- C40H57N5O7 · 719.9099 g/mol (avg)
- First approval
- Canada, 2016 · United States, 2012 · European Union, 2021
- Also known as
- karfilzomib
- Code names
- PR-171
- Brand names
Resolves to
BLMPQMFVWMYDKT-NZTKNTHTSA-NSMILESCC(C)C[C@H](NC(=O)[C@H](CCC1=CC=CC=C1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1What you can answer from here — as of December 11, 2025
Which drugs share a target with Carfilzomib, and which of those have an active Phase 3 trial?
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