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

Stem definition	Drug id	CAS RN
	990	70052-12-9

Description:

Molecule

Description

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: OFM

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

Drug dosage:

None

ADMET properties:

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

Approvals:

Date	Agency	Company	Orphan
Nov. 28, 1990	FDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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
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
FDA MoA	N0000175844	Decarboxylase Inhibitors
FDA EPC	N0000175845	Decarboxylase Inhibitor
CHEBI has role	CHEBI:36335	trypanocidal drugs

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

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Ornithine decarboxylase	Enzyme	P11926	DCOR_HUMAN	INHIBITOR	Kd	4.89		IUPHAR	CHEMBL
Ornithine decarboxylase	Enzyme		Q9TZZ6_TRYBG	INHIBITOR				DRUG LABEL	SCIENTIFIC LITERATURE
Ornithine decarboxylase	Enzyme		DCOR_RAT		Ki	4.41		CHEMBL

External reference:

ID	Source
D00829	KEGG_DRUG
68278-23-9	SECONDARY_CAS_RN
96020-91-6	SECONDARY_CAS_RN
4020660	VANDF
4023581	VANDF
C0002260	UMLSCUI
CHEBI:41948	CHEBI
CHEMBL830	ChEMBL_ID
DB06243	DRUGBANK_ID
CHEMBL1201037	ChEMBL_ID
D000518	MESH_DESCRIPTOR_UI
3009	PUBCHEM_CID
5551	INN_ID
5176	IUPHAR_LIGAND_ID
ZQN1G5V6SR	UNII
284913	RXNORM
15655	MMSL
37870	MMSL
005117	NDDF
005118	NDDF
108715006	SNOMEDCT_US
108716007	SNOMEDCT_US
1269007006	SNOMEDCT_US
372533004	SNOMEDCT_US
783271002	SNOMEDCT_US
DMO	PDB_CHEM_ID
CHEMBL536971	ChEMBL_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
VANIQA	HUMAN PRESCRIPTION DRUG LABEL	1	0023-4857	CREAM	139 mg	TOPICAL	NDA	24 sections
VANIQA	HUMAN PRESCRIPTION DRUG LABEL	1	0023-4857	CREAM	139 mg	TOPICAL	NDA	24 sections
VANIQA	HUMAN PRESCRIPTION DRUG LABEL	1	54868-5124	CREAM	139 mg	TOPICAL	NDA	19 sections
Florexa	HUMAN PRESCRIPTION DRUG LABEL	1	82160-125	CREAM	41.70 mg	TOPICAL	unapproved drug other	16 sections
Florexa	HUMAN PRESCRIPTION DRUG LABEL	1	82160-125	CREAM	4170 mg	TOPICAL	unapproved drug other	16 sections