eflornithine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
990 70052-12-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • eflornithine hydrochloride monohydrate
  • eflornithine hydrochloride anhydrous
  • vaniqa
  • eflornithine hydrochloride
  • eflornithine
  • elfornithine
  • ornidyl
  • alpha-(Difluoromethyl)-DL-ornithine
  • eflornithine hydrochloride hydrate
  • eflornithine HCl
An inhibitor of ORNITHINE DECARBOXYLASE, the rate limiting enzyme of the polyamine biosynthetic pathway.
  • Molecular weight: 182.17
  • Formula: C6H12F2N2O2
  • CLOGP: -1.84
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 3
  • TPSA: 89.34
  • ALOGS: -0.56
  • ROTB: 5

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 55 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
Nov. 28, 1990 FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC D11AX16 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC P01CX03 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTIPROTOZOALS
AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS
Other agents against leishmaniasis and trypanosomiasis
FDA EPC N0000175485 Antiprotozoal
FDA EPC N0000175845 Decarboxylase Inhibitor
FDA MoA N0000175844 Decarboxylase Inhibitors
CHEBI has role CHEBI:36335 trypanocidal drug
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D000981 Antiprotozoal Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065108 Ornithine Decarboxylase Inhibitors
MeSH PA D014344 Trypanocidal Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
African trypanosomiasis indication 27031003 DOID:10112
Female Facial Hirsutism indication
Eruption of skin contraindication 271807003 DOID:0050486
Skin irritation contraindication 367466007

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.31 acidic
pKa2 10.94 Basic
pKa3 5.21 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
Ornithine decarboxylase Enzyme INHIBITOR Kd 4.89 IUPHAR CHEMBL
Ornithine decarboxylase Enzyme INHIBITOR DRUG LABEL SCIENTIFIC LITERATURE
Ornithine decarboxylase Unclassified Ki 4.41 CHEMBL

External reference:

IDSource
D000518 MESH_DESCRIPTOR_UI
C0939525 UMLSCUI
D00829 KEGG_DRUG
4NH22NDW9H UNII
96020-91-6 SECONDARY_CAS_RN
108715006 SNOMEDCT_US
569 RXNORM
372533004 SNOMEDCT_US
4023581 VANDF
005117 NDDF
3009 PUBCHEM_CID
CHEBI:41948 CHEBI
CHEMBL830 ChEMBL_ID
CHEMBL536971 ChEMBL_ID
DB06243 DRUGBANK_ID
5551 INN_ID
5176 IUPHAR_LIGAND_ID
CHEMBL1201037 ChEMBL_ID

Pharmaceutical products:

None