omacetaxine mepesuccinate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4677 26833-87-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • omacetaxine mepesuccinate
  • synribo
  • homoharringtonine
  • CGX-635
  • NSC 141633
  • NSC-141633
Semisynthetic derivative of harringtonine that acts as a protein synthesis inhibitor and induces APOPTOSIS in tumor cells. It is used in the treatment of MYELOID LEUKEMIA, CHRONIC.
  • Molecular weight: 545.63
  • Formula: C29H39NO9
  • CLOGP: 2.33
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 2
  • TPSA: 123.99
  • ALOGS: -3.70
  • ROTB: 11

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.96 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 9.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Oct. 26, 2012 FDA IVAX INTL

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bone marrow failure 63.96 44.74 20 470 29649 46655923
Platelet count decreased 52.70 44.74 24 466 100000 46585572
Injection site erythema 49.33 44.74 21 469 74406 46611166

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Injection site erythema 58.28 40.90 17 436 13817 29938208
Platelet count decreased 45.86 40.90 25 428 106104 29845921
Blood count abnormal 43.27 40.90 13 440 11639 29940386

Pharmacologic Action:

SourceCodeDescription
ATC L01XX40 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000972 Antineoplastic Agents, Phytogenic
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011500 Protein Synthesis Inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:48001 protein synthesis inhibitors
CHEBI has role CHEBI:68495 type i programmed cell-death inducer
CHEBI has role CHEBI:149553 anti-coronaviral agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic myeloid leukemia indication 92818009 DOID:8552

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.86 acidic
pKa2 8.15 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
SARS-CoV-2 Virus INHIBITOR EC50 5.59 SCIENTIFIC LITERATURE

External reference:

IDSource
D08956 KEGG_DRUG
4031782 VUID
N0000186058 NUI
24316-19-6 SECONDARY_CAS_RN
4031782 VANDF
4031814 VANDF
C2709279 UMLSCUI
C3528000 UMLSCUI
CHEBI:71019 CHEBI
HMT PDB_CHEM_ID
CHEMBL46286 ChEMBL_ID
DB04865 DRUGBANK_ID
D000077863 MESH_DESCRIPTOR_UI
285033 PUBCHEM_CID
7454 IUPHAR_LIGAND_ID
8885 INN_ID
6FG8041S5B UNII
84MI6OYN4Z UNII
65305 PUBCHEM_CID
1356689 RXNORM
194347 MMSL
27023 MMSL
d07573 MMSL
009753 NDDF
421021001 SNOMEDCT_US
421815001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SYNRIBO HUMAN PRESCRIPTION DRUG LABEL 1 63459-177 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3.50 mg SUBCUTANEOUS NDA 27 sections