Carfilzomib (Kyprolis)

General information

Class/mechanism: Second-generation proteasome inhibitor that interferes with degradation of ubiquitinated proteins by binding irreversibly to the 20S proteasome, which is the proteolytic core particle inside the 26S proteasome. This disrupts normal homeostatic mechanisms, leading to impaired tumor proliferation, apoptosis/cell death.

Route: IV
Extravasation: no information
NDC: NDC 76075-101-01; NDC 76075-0101-01

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, Medscape, UpToDate (courtesy of Lexicomp), or the prescribing information.

Diseases for which it is used

• Multiple myeloma
• Waldenström macroglobulinemia

Patient drug information

• Brief patient counseling information is available on pages 21-22 of the Carfilzomib (Kyprolis) package insert.
• Carfilzomib (Kyprolis) patient drug information (Chemocare)
• Carfilzomib (Kyprolis) patient drug information (UpToDate)

History of changes in FDA indication

• 7/20/2012: Received accelerated approval for the treatment of patients with multiple myeloma who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression on or within 60 days of completion of the last therapy

Also known as

Precise Name: carfilzomib (RXCUI 1302966)

CFZ or PR-171.