Carfilzomib
DRACPC ID DRACPC0012
Active Ingredients Carfilzomib
Description An epoxomicin derivate with potential antineoplastic activity. Chemically, it is a modified tetrapeptidyl epoxide and an analog of epoxomicin. It is also a selective proteasome inhibitor. 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.
Synonyms Kyprolis; PR-171; (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
Type Small Molecule
Disease Relapsed multiple myeloma
Classification
Proteasome inhibitor Peptide and derivative
Structure Information
Molecular Formula C40H57N5O7
Molecular Weight 719.924
Active Sequence Not available
Sequence Length Not available
Modification Not available
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
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
InChI_Key BLMPQMFVWMYDKT-NZTKNTHTSA-N
SMILES O=C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C(N[C@@H](CC(C)C)C([C@@]1(C)CO1)=O)=O)CC2=CC=CC=C2)=O)=O)CCC3=CC=CC=C3)CN4CCOCC4
External Codes
PubChem CID 11556711
DrugBank Accession Number DB08889
NCI Thesaurus Code C52196
UNII 72X6E3J5AR GSRS
CAS 868540-17-4
Drug approval
Drug indication
Carfilzomib is indicated for the treatment of adult patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy in combination with lenalidomide and dexamethasone; or dexamethasone; or daratumumab and dexamethasone; or daratumumab and hyaluronidase-fihj and dexamethasone; or isatuximab and dexamethasone. It is also 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.
| Drug Name | Strength | Dosage Form/Route | Company | Marketing Status | Drug ID | Approval year |
|---|---|---|---|---|---|---|
| Kyprolis | 30 mg/vial; 60 mg/vial | Powder; Intravenous | Onyx Therap | Prescription | NDA: 202714 | 2012 |
| Kyprolis | 60 mg/vial | Powder; Intravenous | Amgen Canada Inc | Prescription | DIN: 02451034 | 2016 |
| Kyprolis | 10 mg/vial | Powder; Intravenous | Amgen Canada Inc | Prescription | DIN: 02459930 | 2017 |
| Kyprolis | 30 mg/vial | Powder; Intravenous | Amgen Canada Inc | Prescription | DIN: 02459949 | 2017 |
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT01775553 | Recapturing Disease Response: A Phase II Study of High Dose Carfilzomib in Patients With Relapsed or Refractory Multiple Myeloma Who Have Progressed on Standard Dose Carfilzomib | Relapse Multiple Myeloma; Refractory Multiple Myeloma | Phase 2 | Treatment |
| NCT02257476 | A Phase I Study of Extended Infusion Carfilzomib on a Weekly Schedule in Patients With Advanced Solid Malignancies | Neoplasms; Malignancies | Phase 1 | Treatment |
| NCT02145403 | Phase 1/2 Study of Carfilzomib for the Prevention of Relapse and Graft-versus-host Disease in Allogeneic Hematopoietic Cell Transplantation for High-risk Hematologic Malignancies | Hematologic Malignancies ; Relapse; Graft-Versus-HostDisease | Phase 1/2 | Treatment |
| NCT02142530 | Carfilzomib Plus Belinostat in Relapsed/Refractory Non-Hodgkin Lymphoma Subtypes: A Phase 1 Study | Non-Hodgkin Lymphoma; Diffuse Large B-cell Lymphoma; Mantle Cell Lymphoma; Follicular Lymphoma; Peripheral T-cell Lymphoma | Phase 1 | Treatment |
| NCT01926665 | Carfilzomib Consolidation Therapy After Autologous Stem Cell Transplantation (ASCT) for Patients With Mantle Cell (MCL), T-cell (TCL), and Diffuse B-Cell Lymphoma (DLBCL) | Lymphoma | Phase 1 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
