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Carfilzomib
CAS NO.: 868540-17-4
Chemical Formula: C40H57N5O7
Molecular Weight: 719.9000
DMF&GMP status: Please contact us for details.
Description:
Carfilzomib is an epoxomicin derivate with potential antineoplastic activity. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S catalytic core subunit of the proteasome, a protease complex responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth.

Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma. Carfilzomib is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal.

Carfilzomib is a synthetic tetrapeptide consisting of morpholin-4-acetyl, L-2-amino-4-phenylbutanoyl, L-leucyl and L-phenylalanyl residues joined in sequence with the C-terminus connected to the amino group of (2S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-1-one via an amide linkage. Used for the treatment of patients with multiple myeloma It has a role as an antineoplastic agent and a proteasome inhibitor. It is a tetrapeptide, a member of morpholines and an epoxide.

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Approvals
Active Ingredient Dosage Form; Route Strength Proprietary Name Applicant
CARFILZOMIBPOWDER;INTRAVENOUS60MG/VIALCARFILZOMIBDR REDDYS LABORATORIES LTD
CARFILZOMIBPOWDER;INTRAVENOUS10MG/VIALKYPROLISONYX THERAPEUTICS INC A WHOLLY OWNED SUB OF AMGEN INC
CARFILZOMIBPOWDER;INTRAVENOUS30MG/VIALKYPROLISONYX THERAPEUTICS INC A WHOLLY OWNED SUB OF AMGEN INC
CARFILZOMIBPOWDER;INTRAVENOUS60MG/VIALKYPROLISONYX THERAPEUTICS INC A WHOLLY OWNED SUB OF AMGEN INC
CARFILZOMIBPOWDER;INTRAVENOUS30MG/VIALCARFILZOMIBAPOTEX INC
CARFILZOMIBPOWDER;INTRAVENOUS60MG/VIALCARFILZOMIBAPOTEX INC
Patent Data
Patent No. Patent Expiration Drug Substance Claim Drug Product Claim Patent Use Code
N.A.N.A.N.A.N.A.N.A.
Exclusive Data
Exclusivity Code Exclusivity Expiration
D-172 09/28/2021
I-842 08/20/2023