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carfilzomib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
proteasome inhibitors	4483	868540-17-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carfilzomib kyprolis PR-171 PR 171	epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells Molecular weight: 719.92 Formula: C40H57N5O7 CLOGP: 4.21 LIPINSKI: 3 HAC: 12 HDO: 4 TPSA: 158.47 ALOGS: -5.17 ROTB: 20 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carfilzomib
kyprolis
PR-171
PR 171

epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells

Molecular weight: 719.92
Formula: C40H57N5O7
CLOGP: 4.21
LIPINSKI: 3
HAC: 12
HDO: 4
TPSA: 158.47
ALOGS: -5.17
ROTB: 20

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
CL (Clearance)	39.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.10 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.13 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
July 20, 2012	FDA	ONYX PHARMS
July 4, 2016	PMDA	Ono Pharmaceutical

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intercepted product preparation error	390.01	18.45	78	17614	619	63470711
Thrombocytopenia	342.91	18.45	305	17387	150852	63320478
Plasma cell myeloma	308.15	18.45	165	17527	35740	63435590
Tumour lysis syndrome	189.42	18.45	77	17615	8913	63462417
Cytopenia	186.55	18.45	82	17610	11519	63459811
Death	178.47	18.45	349	17343	374032	63097298
Thrombotic microangiopathy	158.09	18.45	71	17621	10490	63460840
Neutropenia	155.02	18.45	216	17476	174789	63296541
Off label use	152.89	18.45	472	17220	673990	62797340
Platelet count decreased	151.63	18.45	174	17518	115948	63355382

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Thrombocytopenia	287.08	18.00	408	20637	155839	34780047
Plasma cell myeloma	269.02	18.00	214	20831	41823	34894063
Intercepted product preparation error	240.40	18.00	91	20954	3987	34931899
Off label use	206.55	18.00	635	20410	418889	34516997
Thrombotic microangiopathy	184.26	18.00	101	20944	10529	34925357
Plasma cell myeloma recurrent	167.53	18.00	72	20973	4393	34931493
Pneumonia	157.15	18.00	526	20519	362101	34573785
Plasmacytoma	140.06	18.00	60	20985	3631	34932255
Plasma cell myeloma refractory	138.39	18.00	38	21007	577	34935309
Neuropathy peripheral	133.02	18.00	204	20841	83059	34852827

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Intercepted product preparation error	515.19	16.54	144	33428	3416	79707400
Thrombocytopenia	502.16	16.54	587	32985	264672	79446144
Plasma cell myeloma	488.73	16.54	295	33277	52964	79657852
Cytopenia	308.26	16.54	157	33415	20226	79690590
Thrombotic microangiopathy	304.00	16.54	155	33417	20014	79690802
Pneumonia	276.78	16.54	751	32821	659495	79051321
Off label use	276.01	16.54	921	32651	906294	78804522
Death	269.66	16.54	676	32896	565838	79144978
Plasma cell myeloma recurrent	257.74	16.54	92	33480	4909	79705907
Unevaluable event	250.83	16.54	199	33373	55386	79655430

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XG02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Proteasome inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:52726	proteasome inhibitors
FDA EPC	N0000175604	Proteasome Inhibitor
FDA MoA	N0000175075	Proteasome Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538
Relapse multiple myeloma	indication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.37	acidic
pKa2	5.23	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	7491704	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8129346	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED AS A SINGLE AGENT FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE OR MORE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DARATUMUMAB PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	8207127	April 14, 2025	KYPROLIS IS INDICATED IN COMBINATION WITH DEXAMETHASONE OR WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	9511109	Oct. 21, 2029	KYPROLIS IS INDICATED IN COMBINATION WITH LENALIDOMIDE PLUS DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 7, 2018	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
30MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	June 3, 2016	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE
60MG/VIAL	KYPROLIS	ONYX PHARMS AMGEN	N202714	July 20, 2012	RX	POWDER	INTRAVENOUS	Aug. 20, 2023	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY MULTIPLE MYELOMA WHO HAVE RECEIVED ONE TO THREE LINES OF THERAPY IN COMBINATION WITH DARATUMUMAB AND DEXAMETHASONE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Proteasome subunit beta type-5	Enzyme	P28074	PSB5_HUMAN	INHIBITOR	IC50	8.22	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Cathepsin B	Enzyme	P07858	CATB_HUMAN		IC50	4.96	CHEMBL
Proteasome subunit beta type-8	Enzyme	P28062	PSB8_HUMAN		IC50	7.85	CHEMBL
Proteasome subunit beta type-1	Enzyme	P20618	PSB1_HUMAN		IC50	5.84	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.04	CHEMBL
Glutathione S-transferase omega-1	Unclassified	P78417	GSTO1_HUMAN		IC50	6.82	CHEMBL
Proteasome subunit beta type-9	Enzyme	P28065	PSB9_HUMAN		IC50	5.62	CHEMBL
Proteasome subunit beta type-10	Enzyme	P40306	PSB10_HUMAN		IC50	6.21	CHEMBL
Proteasome subunit beta type-2	Enzyme	P49721	PSB2_HUMAN		IC50	6.69	CHEMBL

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External reference:

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ID	Source
014536	NDDF
11556711	PUBCHEM_CID
1302966	RXNORM
192152	MMSL
28679	MMSL
3BV	PDB_CHEM_ID
4031662	VUID
4031662	VANDF
713463006	SNOMEDCT_US
714783001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-101	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	60 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-102	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	30 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections
KYPROLIS	HUMAN PRESCRIPTION DRUG LABEL	1	76075-103	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	10 mg	INTRAVENOUS	NDA	31 sections

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