MITOTOX

Drug

D1423 | Leflunomide

Properties

Molecular Formula	C12H9F3N2O2
Molecular Weight	270.21
Structure
State	solid
Volume of distribution	* 0.13 L/kg
Route of elimination	The active metabolite is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion. In a 28 day study of drug elimination (n=3) using a single dose of radiolabeled compound, approximately 43% of the total radioactivity was eliminated in the urine and 48% was eliminated in the feces. It is not known whether leflunomide is excreted in human milk. Many drugs are excreted in human milk, and there is a potential for serious adverse reactions in nursing infants from leflunomide.
Protein binding	>99.3%
Half life	2 weeks
Absorption	Well absorbed, peak plasma concentrations appear 6-12 hours after dosing
Trade names	Arava
Description	immunosuppressive disease-modifying antirheumatic drug (DMARD); pyrimidine synthesis inhibitor by inhibiting dihydroorotate dehydrogenase

Therapeutic Classification Source: DrugBank

L

L04AA13 Leflunomide

[L04AA] Selective immunosuppressants

[L04A] IMMUNOSUPPRESSANTS

[L04] IMMUNOSUPPRESSANTS

[L] Antineoplastic and immunomodulating agents

Mitochondrial Toxicity Evaulation

Toxicity	Dose	Time	Species	Model	Method	Action	Positive criterion	Reference
FUSION	50 μM	48 hr		HeLa cells, C2C12 muscle cells, MEF cells	Mfn2 and Mfn1 mRNA levels; MFN2, MFN1, and porin protein levels; images of mitochondrial morphology ;	induce		295

Targets

Target	Dose	Time	Species	Model	Method	Action	Positive criterion	Reference
Quinol--cytochrome-c reductase	50 μM	48 hr		MEF cells	Mitochondrial Complex III Activity Assay kit(BioVision)	inhibit		295
Dihydroorotate dehydrogenase	50 μM	48 hr		HeLa cells, C2C12 muscle cells, MEF cells	Mfn2 and Mfn1 mRNA levels; MFN2, MFN1, and porin protein levels; images of mitochondrial morphology ;	inhibit		295

Indications Source: SIDER

External IDs

DrugBank	DB01097
CAS Number	75706-12-6
PubChem Compound	3899

References