Carfilzomib (3 brand names, 3 dosage forms, 3 routes)
Available dosage forms: POWDER, INJECTABLE, VIAL.
Routes of administration: INTRAVENOUS, INJECTION, SINGLE-USE.
Brand Names
- CARFILZOMIB
- KITPROZY
- KYPROLIS
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: Cardiac Toxicities [see Warnings and Precautions (5.1)] Acute Renal Failure [see Warnings and Precautions (5.2)] Tumor Lysis Syndrome [see Warnings and Precautions (5.3)] Pulmonary Toxicity [see Warnings and Precautions (5.4)] Pulmonary Hypertension [see Warnings and Precautions (5.5)] Dyspnea [see Warnings and Precautions (5.6)] Hypertension [see Warnings and Precautions (5.7)] Venous Thrombosis [see Warnings and Precautions (5.8)] Infusion-Related Reactions [see Warnings and Precautions (5.9)] Hemorrhage [see Warnings and Precautions (5.10)] Thrombocytopenia [see Warnings and Precautions (5.11)] Hepatic Toxicity and Hepatic Failure [see Warnings and Precautions (5.12)] Thrombotic Microangiopathy [see Warnings and Precautions (5.13)] Posterior Reversible Encephalopathy Syndrome [see Warnings and Precautions (5.14)] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions (5.15)]
Mechanism of Action
Carfilzomib is a tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. Carfilzomib had antiproliferative and proapoptotic activities in vitro in solid and hematologic tumor cells. In animals, carfilzomib inhibited proteasome activity in blood and tissue and delayed tumor growth in models of multiple myeloma, hematologic, and solid tumors.
Overdosage
Acute onset of chills, hypotension, renal insufficiency, thrombocytopenia, and lymphopenia has been reported following a dose of 200 mg of Kyprolis administered in error. There is no known specific antidote for Kyprolis overdosage. In the event of overdose, monitor patients for adverse reactions and provide supportive care as appropriate.