General
Preferred name
TERIFLUNOMIDE
Synonyms
A 77-1726 ()
2-cyano-3-hydroxy-n-[4-(Trifluoromethyl)phenyl]but-2-enamide ()
(E/Z)-Teriflunomide ()
(E/Z)-A77 1726 ()
A77 1726 ()
A77 1726, HMR-1726 ()
A-771726 ()
Aubagio ()
HMR1726 ()
Teriflunomida ()
HMR-1726 ()
Teriflunomide mylan ()
Teriflunomide accord ()
Leflunomide related compound b rs ()
Leflunomide related compound b ()
P&D ID
PD010419
CAS
108605-62-5
163451-81-8
Tags
available
drug
Approved by
FDA
EMA
First approval
2012
Drug indication
Hyperlipidaemia
Multiple sclerosis
Rheumatoid arthritis
Kidney disease
Hepatitis B virus infection
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Inhibits dihydroorotate dehydrogenase
ABSORPTION After oral administration of teriflunomide, maximum plasma concentrations are reached, on average, in 1-4 hours.; ;
ROE Teriflunomide is eliminated unchanged and mainly through bile. Specifically 37.5% is eliminated in the feces and 22.6% in urine.;
PHARMACODYNAMICS Teriflunomide is an immunomodulatory agent that decreases the amount of activated CNS lymphocytes, which results in anti-inflammatory and antiproliferative effects.;
MOA The exact mechanism by which teriflunomide acts in MS is not known. What is known is that teriflunomide prevents pyrimidine synthesis by inhibiting the mitochondrial enzyme; dihydroorotate dehydrogenase, and this may be involved in its immunomodulatory effect in MS.
DESCRIPTION Teriflunomide inhibits dihydroorotate dehydrogenase (DHODH). It is the active metabolite of . (GtoPdb)
DESCRIPTION (E/Z)-Teriflunomide ((E/Z)-A77 1726) is the active metabolite of ; Leflunomide (HY-B0083). Leflunomide is an immunomodulatory agent that may exert effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). Leflunomide can be used for the research of rheumatoid arthritis (RA)[1].
DESCRIPTION Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
PRICE 37
DESCRIPTION Adenylyl cyclase inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Dihydroorotate dehydrogenase inhibitor (Tocriscreen Plus)
DESCRIPTION Teriflunomide (A 77-1726) is the principal active metabolite of leflunomide, an approved therapy for rheumatoid arthritis and multiple sclerosis. (TargetMol Bioactive Compound Library)
Cell lines
4
Organisms
1
Compound Sets
26
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
43
Properties
(calculated by RDKit )
Molecular Weight
270.06
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
1
Aromatic Ring Count
1
cLogP
3.0
TPSA
73.12
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzymes
Primary Target
Dihydroorotate Dehydrogenase
MOA
Inhibitor
Dihydroorotate Dehydrogenase (DHODH) Inhibitors
Member status
member
Target
Drug Metabolite
Dehydrogenase,Immunology & Inflammation related
Pathway
Metabolic Enzyme/Protease
Source data