omacetaxine mepesuccinate 🐶 Veterinary Use | 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: 1.76
  • 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 66.15 44.45 20 490 27604 50577010
Platelet count decreased 53.46 44.45 24 486 100702 50503912
Injection site erythema 49.99 44.45 21 489 74915 50529699

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 57.62 45.20 17 444 13939 29560127
Platelet count decreased 45.47 45.20 25 436 104647 29469419

FDA Adverse Event Reporting System (Geriatric)

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 76.29 38.04 27 796 47925 64449984
Platelet count decreased 74.25 38.04 38 785 167673 64330236
Injection site erythema 55.94 38.04 24 799 70776 64427133
Nausea 44.72 38.04 52 771 785748 63712161

FDA Adverse Event Reporting System (Pediatric)

None

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 antineoplastic agents
CHEBI has role CHEBI:48001 protein synthesis inhibitors
CHEBI has role CHEBI:68495 Type I cell-death inducers
CHEBI has role CHEBI:149553 anticoronaviral drug

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

DiseaseRelationSNOMED_IDDOID
Chronic myeloid leukemia indication 92818009 DOID:8552




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3.5MG/VIAL SYNRIBO TEVA PHARMS INTL N203585 Oct. 26, 2012 RX POWDER SUBCUTANEOUS 6987103 Oct. 26, 2026 TREATMENT OF PATIENTS WITH TYROSINE KINASE INHIBITOR (TKI) RESISTANT OR INTOLERANT CHRONIC MYELOID/MYELOGENOUS LEUKEMIA (CML)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D08956 KEGG_DRUG
4031782 VUID
N0000186058 NUI
4031782 VANDF
4031814 VANDF
CHEBI:71019 CHEBI
HMT PDB_CHEM_ID
CHEMBL46286 ChEMBL_ID
7454 IUPHAR_LIGAND_ID
8885 INN_ID
24316-19-6 SECONDARY_CAS_RN
DB04865 DRUGBANK_ID
6FG8041S5B UNII
285033 PUBCHEM_CID
65305 PUBCHEM_CID
1356689 RXNORM
194347 MMSL
27023 MMSL
d07573 MMSL
009753 NDDF
421021001 SNOMEDCT_US
421815001 SNOMEDCT_US
D000077863 MESH_DESCRIPTOR_UI
C0062941 UMLSCUI
C3528000 UMLSCUI
84MI6OYN4Z UNII

Pharmaceutical products:

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