Carfilzomib
Highest phase reached
Approved
Drug type
Protein
First approval year
2009
- First approval year
- 2009
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Protein
- Drug name
- Carfilzomib
- Molecular weight
- 719.92
- Structure (SMILES)
- CC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1
- kyprolis
- Kyprolis
- (2S)-N-[(1S)-1-Benzyl-2-[[(1S)-3-methyl-1-[[(2R)-2-methyloxiran-2-yl]carbonyl]butyl]amino]-2-oxoethyl]-4-methyl-2-[[(2S)-2-[(morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide
- 2s n 1s 1 benzyl 2 1s 3 methyl 1 2r 2 methyloxiran 2 yl carbonyl butyl amino 2 oxoethyl 4 methyl 2 2s 2 morpholin 4 ylacetyl amino 4 phenylbutanoyl amino pentanamide
- carfilzomib
- Carfilzomib
- carfilzomib (infusion)
- carfilzomib [INN]
- CARFILZOMIB [JAN]
- CARFILZOMIB [MI]
- CARFILZOMIB [ORANGE BOOK]
- CARFILZOMIB [USAN]
- CARFILZOMIB [VANDF]
- Carfilzomib [WHO-DD]
- Carfilzomib Injection
- carfilzomib inn
- carfilzomib jan
- carfilzomib mi
- carfilzomib orange book
- carfilzomib usan
- carfilzomib vandf
- carfilzomib who dd
- Drug: Carfilzomib
- kitprozy
- KITPROZY
- Kyprolis
- l phenylalaninamide alpha s alpha 4 morpholinylacetyl amino benzenebutanoyl l leucyl n 1s 3 methyl 1 2r 2 methyloxiranyl carbonyl butyl
And 5 more, listed on the interactive page.
- CAS registry numbers
- 868540-17-4
- ChEMBL ID
- CHEMBL451887
- InChIKey
- BLMPQMFVWMYDKT-NZTKNTHTSA-N
- PubChem compound IDs
- 11556711
- RxNorm IDs (RxCUI)
- 1302966
- FDA ingredient codes (UNII)
- 72X6E3J5AR
- L01XG02
- L01XX45
Sources for recorded values
- Applicant
- ONYX PHARMS AMGEN
- Approval date
- 20 Jul 2012
- Application number
- NDA202714
- Status
- Authorised
- Status date
- 19 Nov 2015
- Authorisation date
- 19 Nov 2015
- Approved indications
- Kyprolis in combination with daratumumab and dexamethasone, with lenalidomide and dexamethasone, or with dexamethasone alone is indicated for the treatment of adult patients with multiple myeloma who have received at least one prior therapy.
- Product number
- EMEA/H/C/003790
- Authorisation holder
- Amgen Europe B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- Yes
- Exceptional circumstances
- No
Therapeutic areas
- Multiple Myeloma
European medicines record
- Patents
- 8
- Designations
- 3
- Earliest recorded loss of exclusivity
- 27 Aug 2033
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- Yes
- Availability
- Prescription only
- Pharmacology name
- carfilzomib
- Type
- Synthetic organic
- Drug name stem
- -zomib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Parenteral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- proteasome 20S subunit beta 5
- Gene symbol
- PSMB5
- Protein identifier
- P28074
- Median affinity
- 8.24
- Affinity units
- pIC50
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- A5LHX3
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- O00231
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- O00232
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- O00487
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- O14818
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- O43242
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P17980
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P20618
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P25786
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P25787
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P25788
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P25789
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28062
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28065
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28066
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28070
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28072
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P28074
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P35998
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P40306
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P43686
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P48556
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P49720
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
- Protein identifier
- P49721
And 14 more, listed on the interactive page.
Open Targets mechanisms
- Mechanism
- 26S proteasome inhibitor
- Action type
- Inhibitor
- Target
- 26S proteasome
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- PSMB5
- Protein identifier
- P28074
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Leukemia, Lymphocytic, Chronic, B-Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000095
- Subject identifier
- D015451
- Condition
- Lymphoma, Follicular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000096
- Subject identifier
- D008224
- Condition
- Hodgkin Disease
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000183
- Subject identifier
- D006689
- Condition
- Lymphoma, T-Cell, Peripheral
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000211
- Subject identifier
- D016411
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Leukemia, Myeloid, Acute
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000222
- Subject identifier
- D015470
- Condition
- Lymphoma, Large B-Cell, Diffuse
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000403
- Subject identifier
- D016403
- Condition
- Leukemia
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000565
- Subject identifier
- D007938
- Condition
- Lymphoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Small Cell Lung Carcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000702
- Subject identifier
- D055752
- Condition
- Multiple Myeloma
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Lymphoma, T-Cell, Cutaneous
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002913
- Subject identifier
- D016410
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Smoldering Multiple Myeloma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003073
- Subject identifier
- D000075122
- Condition
- Lymphoma, Non-Hodgkin
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005952
- Subject identifier
- D008228
- Condition
- Leukemia, Plasma Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0006475
- Subject identifier
- D007952
- Condition
- Plasmacytoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0006738
- Subject identifier
- D010954
- Condition
- Waldenstrom Macroglobulinemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0009441
- Subject identifier
- D008258
- Condition
- Sezary Syndrome
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000785
- Subject identifier
- D012751
- Condition
- Mycosis Fungoides
- Highest recorded phase
- 1
- Condition identifier
- EFO:1001051
- Subject identifier
- D009182
- Condition
- Lymphoma, Mantle-Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001469
- Subject identifier
- D020522
- Condition
- Amyloidosis
- Highest recorded phase
- 1
- Condition identifier
- EFO:1001875
- Subject identifier
- D000686
- Condition
- Leukemia, Prolymphocytic
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0001023
- Subject identifier
- D015463
- Condition
- Carcinoma, Neuroendocrine
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0002120
- Subject identifier
- D018278
And 6 more, listed on the interactive page.
- Condition identifier
- EFO_0000095
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000211
- Condition identifier
- EFO_0000565
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000702
- Condition identifier
- EFO_0001378
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0009441
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009909
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000430
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0000607
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001023
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002120
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002367
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004948
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004949
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004952
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004964
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004977
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005005
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005059
- Highest recorded phase
- 1
And 29 more, listed on the interactive page.
- Event
- acute kidney injury
- Reports
- 291
- Reporting signal score
- 119.536
- Event
- cardiac failure
- Reports
- 208
- Reporting signal score
- 177.458
- Event
- cytopenia
- Reports
- 103
- Reporting signal score
- 172.984
- Event
- disease progression
- Reports
- 230
- Reporting signal score
- 131.471
- Event
- intercepted product preparation error
- Reports
- 186
- Reporting signal score
- 486.565
- Event
- plasma cell myeloma
- Reports
- 538
- Reporting signal score
- 1,221.57
- Event
- plasma cell myeloma recurrent
- Reports
- 67
- Reporting signal score
- 155.212
- Event
- pneumonia
- Reports
- 410
- Reporting signal score
- 130.487
- Event
- thrombocytopenia
- Reports
- 401
- Reporting signal score
- 269.414
- Event
- thrombotic microangiopathy
- Reports
- 111
- Reporting signal score
- 204.435
- Event
- unevaluable event
- Reports
- 162
- Reporting signal score
- 118.208
- NCT00511238
- NCT00530816
- NCT00603447
- NCT00721734
- NCT00884312
- NCT01029054
- NCT01057225
- NCT01080391
- NCT01246063
- NCT01279694
- NCT01297764
- NCT01301807
- NCT01302392
- NCT01346787
- NCT01351623
- NCT01365559
- NCT01372540
- NCT01402284
- NCT01464034
- NCT01496118
- NCT01537861
- NCT01549431
- NCT01554852
- NCT01559935
- NCT01568866
And 168 more, listed on the interactive page.
- Dose
- 20/70 mg/m2
- Route
- Intravenous
- How often
- Once weekly
- Administer as a 30-minute infusion
- Administer on Days 1, 8, and 15 of each 28-day cycle
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 4
- Polar surface area
- 158.47
- Calculated partition coefficient (ALogP)
- 2.58
- Calculated partition coefficient (XLogP)
- 4.7
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 20
- Heavy atoms
- 52
- Molecular formula
- C40H57N5O7
- Monoisotopic mass
- 719.42579917
- Natural product
- Yes
- 76075-101
- 76075-102
- 76075-103
- Recorded assays
- 1,511
- Active assays
- 770
- Confirmatory
- Screening
- Summary
These details could not be displayed.
Related records
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- A Clinical Study on the Safety, Tolerance, and Preliminary Efficacy of γδ-T Cell Injection in the Treatment of Advanced Bladder Cancer
- A Clinical Trial of Four Medicines (Elranatamab Plus Carfilzomib and Dexamethasone or Maplirpacept) in People With Relapsed Refractory Multiple Myeloma
- A Clinical Trial to Learn About the Study Medicine Called Maplirpacept (PF-07901801), Alone and When Used in Combination With Other Medicines to Treat Participants With Advanced Hematological Malignancies, Including Lymphoma, Leukemia and Multiple Myeloma
- A Dose Escalation Study of Carfilzomib Taken With Thalidomide and Dexamethasone in Relapsed AL Amyloidosis
- A First in Human Study to Evaluate the Safety of Infusion of MNV-BM-PLC (Autologous CD34+ Cells Enriched With Placenta Derived Allogeneic Mitochondria) in Patients With Primary Mitochondrial Diseases Associated With Mitochondrial DNA Mutation or Deletion
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Approved for (3)
- Cancer
- Neoplasm
- Plasma cell myeloma
In development for (28)
- Acute lymphoblastic leukemia Phase 1
- Acute myeloid leukemia Phase 1
- Amyloidosis Phase 1
- B-cell chronic lymphocytic leukemia Phase 1
- Chronic graft versus host disease Phase 2
- Diffuse large B-cell lymphoma Phase 1
- Follicular lymphoma Phase 2
- Hodgkins lymphoma Phase 1
- Kidney cancer Phase 2
- Leukemia Phase 1
- Lymphoma Phase 2
- Mantle cell lymphoma Phase 2
- Mycosis fungoides Phase 1
- Neoplasm of mature B-cells Phase 2
- Neuroendocrine carcinoma Phase 2
- Non-Hodgkin lymphoma Phase 1
- Non-small cell lung carcinoma Phase 1
- Peripheral T-cell lymphoma, not otherwise specified Phase 1
- Plasma cell leukemia Phase 1
- Plasmacytoma Phase 1
Targets (38)
- ADRM1 26S proteasome inhibitor
- PSMA1 26S proteasome inhibitor
- PSMA2 26S proteasome inhibitor
- PSMA3 26S proteasome inhibitor
- PSMA4 26S proteasome inhibitor
- PSMA5 26S proteasome inhibitor
- PSMA6 26S proteasome inhibitor
- PSMA7 26S proteasome inhibitor
- PSMA8 26S proteasome inhibitor
- PSMB1 26S proteasome inhibitor
- PSMB10 26S proteasome inhibitor
- PSMB11 26S proteasome inhibitor
- PSMB2 26S proteasome inhibitor
- PSMB3 26S proteasome inhibitor
- PSMB4 26S proteasome inhibitor
- PSMB5 26S proteasome inhibitor
- PSMB6 26S proteasome inhibitor
- PSMB7 26S proteasome inhibitor
- PSMB8 26S proteasome inhibitor
- PSMB9 26S proteasome inhibitor