teriflunomide

Teriflunomide is an oral immunomodulatory agent used for the treatment of patients with relapsing forms of multiple sclerosis (MS). It inhibits dihydroorotate dehydrogenase, an enzyme used to make pyrimidine which is used to build DNA. The exact mechanism of action of teriflunomide in the treatment of MS is unknown. However, it is thought to reduce the over activation of the immune system by decreasing the number of white blood cells (T and B lymphocytes) in the central nervous system. Teriflunomide decreases the number of MS relapses. The FDA approved teriflunomide in September 2013.

Aubagio

GENERIC AVAILABLE: No

Yes

The most common side effects associated with teriflunomide treatment are

• alopecia (hair thinning or loss),
• diarrhea,
• influenza,
• paresthesia (tingling, burning, prickling or pricking sensations of the skin),
• and increase in liver enzymes.

Serious liver injury, kidney problems, decrease in white blood cell counts, risk for serious infections such as

• tuberculosis, increase in blood potassium levels (hyperkalemia),
• increase in blood pressure, breathing problems,
• and serious skin problems were also reported in clinical studies.

The recommended dose is one 7 mg or 14 mg tablet once daily with or without food. Note that a monthly blood test for liver enzyme measurements for 6 months is recommended to detect potential liver problems (see side effects section).

Teriflunomide may increase blood levels of

• repaglinide (Prandin),
• paclitaxel, pioglitazone (Actos),
• or rosiglitazone (Avandia).

Teriflunomide may also decrease the effectiveness of warfarin (Coumadin) and increases the risk for blood clots.

Teriflunomide may increase the effects of oral contraceptives (birth control pills) containing ethinylestradiol or levonorgestrel.

Teriflunomide may decrease the blood levels of drugs such as

• duloxetine (Cymbalta),
• alosetron (Lotronex),
• theophylline (Respbid, Slo-Bid, Theo-24, Theolair),
• and tizanidine that are metabolized by the CYP1A2 liver enzymes.

Blood levels of teriflunomide may be increased by

• cyclosporine,
• eltrombopag,
• and gefitinib (Iressa).

It is not known whether teriflunomide is secreted into breast milk.

What preparations of teriflunomide are available?

Film-coated tablets: 7 mg and 14 mg

How should I keep teriflunomide stored?

STORAGE: Tablets should to be stored at 20 C to 25 C (68 F to 77 F), but also may be stored at 15 C to 30 C (59 F to 86 F)