carfilzomib indications/contra

Stem definitionDrug idCAS RN
proteasome inhibitors 4483 868540-17-4

Description:

MoleculeDescription

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: 719.91
  • Formula: C40H57N5O7
  • CLOGP: 6.40
  • LIPINSKI: 3
  • HAC: 8
  • HDO: 4
  • TPSA: 158.47
  • ALOGS: -5.17
  • RINGS: 4
  • ROTB: 20

Drug dosage:

DoseUnitRoute
40 mg P

Approvals:

DateAgencyCompanyOrphan
July 20, 2012 FDA ONYX PHARMS

Pharmacologic Action:

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SourceCodeDescription
ATC L01XX45 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA MoA N0000175075 Proteasome Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:52726 proteasome inhibitor

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Proteasome subunit beta type-5 Enzyme INHIBITOR IC50 8.22 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Cathepsin B Enzyme IC50 4.96 CHEMBL
Proteasome subunit beta type-8 Enzyme IC50 7.85 CHEMBL

External reference:

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IDSource
4031662 VANDF
N0000185509 NDFRT
014536 NDDF
1302966 RXNORM
28679 MMSL
d07882 MMSL
713463006 SNOMEDCT_US
714783001 SNOMEDCT_US
DB08889 DRUGBANK_ID
C519125 MESH_SUPPLEMENTAL_RECORD_UI
C524865 MESH_SUPPLEMENTAL_RECORD_UI
D08880 KEGG_DRUG
8859 INN_ID
72X6E3J5AR UNII
3BV PDB_CHEM_ID
CHEBI:65347 CHEBI
11556711 PUBCHEM_CID
7420 IUPHAR_LIGAND_ID
CHEMBL451887 ChEMBL_ID
N0000185509 NUI
C2001856 UMLSCUI
4031662 VUID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
KYPROLIS HUMAN PRESCRIPTION DRUG LABEL 1 76075-101 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 60 mg INTRAVENOUS NDA 16 sections
KYPROLIS HUMAN PRESCRIPTION DRUG LABEL 1 76075-102 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 mg INTRAVENOUS NDA 16 sections