Carfilzomib

Carfilzomib
Clinical data
Trade names	Kyprolis
Other names	PX-171-007
AHFS/Drugs.com	Monograph
MedlinePlus	a612031
License data	US DailyMed: Carfilzomib;
Pregnancy; category	AU: C;
Routes of; administration	Intravenous
ATC code	L01XG02 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Protein binding	97%
Metabolism	Extensive; CYP plays a minor role
Identifiers
	IUPAC name (2S)-4-Methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide;
CAS Number	868540-17-4;
PubChem CID	11556711;
IUPHAR/BPS	7420;
DrugBank	DB08889;
ChemSpider	9731489;
UNII	72X6E3J5AR;
KEGG	D08880;
ChEBI	CHEBI:65347;
ChEMBL	ChEMBL451887;
CompTox Dashboard (EPA)	DTXSID4048690 ;
ECHA InfoCard	100.219.957
Chemical and physical data
Formula	C40H57N5O7
Molar mass	719.924 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)[C@@]1(OC1)C)CC(C)C)Cc2ccccc2)CC(C)C)CCc3ccccc3)CN4CCOCC4;
	InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1; Key:BLMPQMFVWMYDKT-NZTKNTHTSA-N;

Carfilzomib, sold under the brand name Kyprolis, is an anti-cancer medication acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin.^[4] It was developed by Onyx Pharmaceuticals.

The US Food and Drug Administration (FDA) approved it in July 2012.^[5]^[6]

^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
^ ^a ^b "Kyprolis- carfilzomib injection, powder, lyophilized, for solution". DailyMed. 26 August 2020. Retrieved 13 November 2020.
^ "NCI Drug Dictionary". National Cancer Institute. Retrieved 13 November 2020.
^ "FDA Approves Kyprolis for Some Patients with Multiple Myeloma". FDA. 2012-07-20. Archived from the original on 2013-01-28. Retrieved 2013-07-23.
^ "Drug Approval Package: Kyprolis (carfilzomib) for Injection NDA #202714". U.S. Food and Drug Administration (FDA). 20 August 2012. Archived from the original on April 13, 2016. Retrieved 10 April 2023.

[1] "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.

[2] "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.

[Kyprolis_FDA_label-3] "Kyprolis- carfilzomib injection, powder, lyophilized, for solution". DailyMed. 26 August 2020. Retrieved 13 November 2020.

[dd-4] "NCI Drug Dictionary". National Cancer Institute. Retrieved 13 November 2020.

[FDA_PR_20120720-5] "FDA Approves Kyprolis for Some Patients with Multiple Myeloma". FDA. 2012-07-20. Archived from the original on 2013-01-28. Retrieved 2013-07-23.

[6] "Drug Approval Package: Kyprolis (carfilzomib) for Injection NDA #202714". U.S. Food and Drug Administration (FDA). 20 August 2012. Archived from the original on April 13, 2016. Retrieved 10 April 2023.

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