Aubagio for treating relapsing forms of multiple sclerosis in adults

Aubagio is an oral medication approved for the treatment of relapsing forms of multiple sclerosis (MS) in adults. It works by inhibiting pyrimidine synthesis, helping to reduce MS disease activity. Aubagio is available as 7 mg and 14 mg tablets taken once daily, with or without food.

Aubagio is indicated for the treatment of relapsing forms of multiple sclerosis (MS) in adults. This includes clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.

teriflunomide

Aubagio’s active ingredient, teriflunomide, works by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase, which is involved in pyrimidine synthesis. This inhibition reduces the proliferation of activated T- and B-lymphocytes that are thought to contribute to the damaging inflammatory process in multiple sclerosis.

The recommended dose of Aubagio is either 7 mg or 14 mg taken orally once daily. It can be taken with or without food.

Monitoring:

• Obtain liver function tests including transaminase and bilirubin levels within 6 months prior to starting therapy.
• Monitor alanine aminotransferase (ALT) levels at least monthly for the first six months of treatment.
• Obtain a complete blood cell count (CBC) within 6 months before initiating Aubagio and monitor for signs of infection during treatment.
• Screen for latent tuberculosis infection before starting treatment.
• Check blood pressure before treatment initiation and periodically thereafter.
• Pregnancy must be excluded before starting in females of reproductive potential.

• Severe hepatic impairment
• Pregnancy or females of reproductive potential not using effective contraception
• History of hypersensitivity to teriflunomide, leflunomide, or any ingredient in Aubagio
• Concurrent leflunomide treatment

Hepatotoxicity

Serious liver injury, including acute liver failure requiring transplant, has been reported. Patients with pre-existing liver disease or those taking other hepatotoxic drugs are at increased risk. Aubagio is contraindicated in patients with severe hepatic impairment. Liver enzymes should be monitored closely, and treatment discontinued if ALT elevations greater than three times the upper limit of normal are confirmed.

Embryofetal Toxicity

Aubagio may cause fetal harm. It is contraindicated in pregnant women and females of reproductive potential not using effective contraception. Pregnancy must be excluded prior to starting treatment. Effective contraception is required during treatment and during the accelerated elimination procedure after stopping Aubagio. If pregnancy occurs, Aubagio should be stopped immediately and an accelerated elimination procedure started.

Hypersensitivity Reactions

Anaphylaxis, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, and drug reaction with eosinophilia and systemic symptoms (DRESS) have been reported and can be fatal. Discontinue Aubagio and initiate accelerated elimination if such reactions develop.

Bone Marrow Effects and Infection Risk

Aubagio can decrease white blood cells and platelets. Patients with active infections should not start treatment. Serious infections and tuberculosis, including fatal cases, have been reported; screening for latent tuberculosis is required before treatment. Live vaccines are not recommended during or shortly after treatment.

Peripheral Neuropathy

Peripheral neuropathy has occurred more frequently with Aubagio than placebo. If symptoms develop, evaluate and consider stopping the medication.

Other Warnings

• Aubagio may increase blood pressure; monitor regularly.
• Cases of interstitial lung disease have been reported in the postmarketing setting.
• Cutaneous or mucocutaneous ulcers and impaired wound healing have been reported; consider discontinuing if they occur.
• Adjustments and monitoring are particularly important in older adults and those on concurrent neurotoxic or immunosuppressive therapies.

Common Side Effects

• Elevations in liver enzymes (ALT and AST)
• Hypertension
• Decreased white blood cell and platelet counts
• Peripheral neuropathy symptoms such as numbness or tingling

Serious Side Effects

• Severe liver injury including liver failure
• Severe allergic reactions including anaphylaxis and angioedema
• Severe skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis
• Drug reaction with eosinophilia and systemic symptoms (DRESS)
• Serious infections including fatal pneumonia and tuberculosis
• Interstitial lung disease
• Pancytopenia and agranulocytosis (rare, reported postmarketing)

Aubagio is contraindicated with leflunomide due to similar active metabolites. Concomitant use of other hepatotoxic drugs may increase the risk of liver injury. Caution is advised when combining Aubagio with other immunosuppressive or antineoplastic therapies, as the long-term safety of such combinations is unknown.

Pregnancy

Aubagio may cause fetal harm and is contraindicated during pregnancy. Exclude pregnancy before treatment and instruct females of reproductive potential to use effective contraception during treatment and accelerated elimination afterward. If pregnancy occurs, discontinue Aubagio and initiate accelerated elimination of the drug.

Breastfeeding

No specific information is provided in the label regarding breastfeeding. Due to potential risks, breastfeeding during treatment should be approached with caution.

There is no specific confirmed overdose treatment. In case of overdose, supportive care and monitoring for hepatotoxicity and other adverse effects are recommended. If needed, an accelerated elimination procedure with cholestyramine or activated charcoal may be employed to reduce teriflunomide plasma levels.