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US Approved Rx

2

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Primary Target

Dihydroorotate dehydrogenase

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Dihydroorotate dehydrogenase (quinone), mitochondrial

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Approved

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1998

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Active rheumatoid arthritis

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Multiple sclerosis

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Palliative

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CNS Non-penetrant

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Sanofi-Aventis

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CHEBI

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Selective immunosuppressants

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TERIFLUNOMIDE

1C058IKG3B

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Status:

US Approved Rx (2019)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Dihydroorotate dehydrogenase

Dihydroorotate dehydrogenase (quinone), mitochondrial

Conditions:

Active rheumatoid arthritis

Multiple sclerosis

Teriflunomide (trade name Aubagio, marketed by Sanofi) is the active metabolite of leflunomide and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis by blocking the enzyme dihydroorotate dehydrogenase. Teriflunomide was investig...

ated in the Phase III clinical trial TEMSO as a medication for multiple sclerosis (MS). The drug was approved by the FDA on September 13, 2012 and in the European Union on August 26, 2013. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. Teriflunomide may decrease the risk of infections compared to chemotherapy-like drugs because of its more-limited effects on the immune system. It has been found that teriflunomide blocks the transcription factor NF-κB. It also inhibits tyrosine kinase enzymes, but only in high doses not clinically used.

LEFLUNOMIDE

G162GK9U4W

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Status:

US Approved Rx (2019)

First approved in 1998

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Dihydroorotate dehydrogenase

Dihydroorotate dehydrogenase (quinone), mitochondrial

Conditions:

Active rheumatoid arthritis

Multiple sclerosis

Teriflunomide (trade name Aubagio, marketed by Sanofi) is the active metabolite of leflunomide and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis by blocking the enzyme dihydroorotate dehydrogenase. Teriflunomide was investig...

ated in the Phase III clinical trial TEMSO as a medication for multiple sclerosis (MS). The drug was approved by the FDA on September 13, 2012 and in the European Union on August 26, 2013. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. Teriflunomide may decrease the risk of infections compared to chemotherapy-like drugs because of its more-limited effects on the immune system. It has been found that teriflunomide blocks the transcription factor NF-κB. It also inhibits tyrosine kinase enzymes, but only in high doses not clinically used.

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