Dosing & Uses
Dosage Forms and Strengths
tablet
- 7mg
- 14mg
Multiple Sclerosis
Indicated for treatment of relapsing forms of multiple sclerosis
7 mg or 14 mg PO qDay
Dosing Considerations
Gender: Drug clearance decreased by 23% in females compared with males
Monitoring to assess safety
- Obtain transaminase and bilirubin levels within 6 months before initiation of therapy; monitor ALT levels at least monthly for six months after starting therapy
- Obtain a complete blood cell count (CBC) within 6 months before the initiation of treatment; further monitoring should be based on signs and symptoms of infection
- Prior to initiating therapy, screen patients for latent tuberculosis infection with a tuberculin skin test or blood test for mycobacterium tuberculosis infection
- Exclude pregnancy prior to initiation of treatment in females of reproductive potential
- Check blood pressure before start of treatment and periodically thereafter
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (8)
- axicabtagene ciloleucel
teriflunomide, axicabtagene ciloleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- brexucabtagene autoleucel
teriflunomide, brexucabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- ciltacabtagene autoleucel
teriflunomide, ciltacabtagene autoleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- etrasimod
teriflunomide will increase the level or effect of etrasimod by Other (see comment). Avoid or Use Alternate Drug. Increased exposure of etrasimod expected in patients who are CYP2C9 poor metabolizers if coadministered with moderate to strong CYP2C8 inhibitors.
- idecabtagene vicleucel
teriflunomide, idecabtagene vicleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- lisocabtagene maraleucel
teriflunomide, lisocabtagene maraleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tisagenlecleucel
teriflunomide, tisagenlecleucel. Either increases effects of the other by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.
- tucatinib
teriflunomide will increase the level or effect of tucatinib by Other (see comment). Avoid or Use Alternate Drug. Coadministration of tucatinib (a CYP2C8 substrate) with a strong or moderate CYP2C8 inhibitors increases tucatinib plasma concentrations and risk of toxicities.
Monitor Closely (63)
- alosetron
teriflunomide decreases levels of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- amiodarone
teriflunomide increases levels of amiodarone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- amitriptyline
teriflunomide decreases levels of amitriptyline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- betaxolol
teriflunomide decreases levels of betaxolol by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- caffeine
teriflunomide decreases levels of caffeine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- carbamazepine
teriflunomide increases levels of carbamazepine by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- clomipramine
teriflunomide decreases levels of clomipramine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- clozapine
teriflunomide decreases levels of clozapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- cyclobenzaprine
teriflunomide decreases levels of cyclobenzaprine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- dacarbazine
teriflunomide decreases levels of dacarbazine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- daprodustat
teriflunomide will increase the level or effect of daprodustat by Other (see comment). Modify Therapy/Monitor Closely. Moderate CYP2C8 inhibitors increase daprodustat exposure. If coadministered with moderate CYP2C8 inhibitors, reduce daprodustat starting dose by half (except if starting dose is already 1 mg). Monitor hemoglobin and adjust daprodustat dose when initiating or stopping therapy with moderate CYP2C8 inhibitors during treatment
- dapsone
teriflunomide increases levels of dapsone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- diclofenac
teriflunomide increases levels of diclofenac by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- doxepin
teriflunomide decreases levels of doxepin by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- duloxetine
teriflunomide decreases levels of duloxetine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- enzalutamide
teriflunomide increases levels of enzalutamide by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- estradiol
teriflunomide decreases levels of estradiol by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- estrogens conjugated synthetic
teriflunomide decreases levels of estrogens conjugated synthetic by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- estrogens esterified
teriflunomide decreases levels of estrogens esterified by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- estropipate
teriflunomide decreases levels of estropipate by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ethinylestradiol
teriflunomide increases levels of ethinylestradiol by unknown mechanism. Use Caution/Monitor.
- flutamide
teriflunomide decreases levels of flutamide by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- fluvastatin
teriflunomide increases levels of fluvastatin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- fluvoxamine
teriflunomide will decrease the level or effect of fluvoxamine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ifosfamide
ifosfamide, teriflunomide. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor.
- isotretinoin
teriflunomide increases levels of isotretinoin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- lapatinib
teriflunomide increases levels of lapatinib by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- letermovir
teriflunomide increases levels of letermovir by decreasing metabolism. Use Caution/Monitor. Coadminstration of letermovir, an OATP1B1/3 substrate, with OATP1B1/3 inhibitors may increase letermovir plasma concentrations.
- levonorgestrel intrauterine
teriflunomide increases levels of levonorgestrel intrauterine by unknown mechanism. Use Caution/Monitor.
- levonorgestrel oral
teriflunomide increases levels of levonorgestrel oral by unknown mechanism. Use Caution/Monitor.
- lomustine
lomustine and teriflunomide both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Concomitant therapy is expected to increase the risk of immunosuppression. Use caution when switching patients from long-acting therapies with immune effects.
- metaxalone
teriflunomide increases levels of metaxalone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
teriflunomide decreases levels of metaxalone by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. - methadone
teriflunomide increases levels of methadone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- mexiletine
teriflunomide decreases levels of mexiletine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- mirtazapine
teriflunomide decreases levels of mirtazapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ofatumumab SC
ofatumumab SC, teriflunomide. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- olanzapine
teriflunomide decreases levels of olanzapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- paclitaxel
teriflunomide increases levels of paclitaxel by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- paclitaxel protein bound
teriflunomide increases levels of paclitaxel protein bound by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- pazopanib
teriflunomide increases levels of pazopanib by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- pimozide
teriflunomide decreases levels of pimozide by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- pioglitazone
teriflunomide increases levels of pioglitazone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- pitavastatin
teriflunomide increases levels of pitavastatin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- propranolol
teriflunomide decreases levels of propranolol by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ramelteon
teriflunomide decreases levels of ramelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- rasagiline
teriflunomide decreases levels of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- repaglinide
teriflunomide increases levels of repaglinide by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- riluzole
teriflunomide decreases levels of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ropinirole
teriflunomide decreases levels of ropinirole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ropivacaine
teriflunomide decreases levels of ropivacaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- rosiglitazone
teriflunomide increases levels of rosiglitazone by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- selegiline
teriflunomide increases levels of selegiline by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- selegiline transdermal
teriflunomide increases levels of selegiline transdermal by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- selexipag
teriflunomide will increase the level or effect of selexipag by decreasing metabolism. Modify Therapy/Monitor Closely. Reduce selexipag dose to once daily if coadministered with moderate CYP2C8 inhibitors.
- sitagliptin
teriflunomide increases levels of sitagliptin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- theophylline
teriflunomide decreases levels of theophylline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- thiothixene
teriflunomide decreases levels of thiothixene by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- tizanidine
teriflunomide decreases levels of tizanidine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- trastuzumab
trastuzumab, teriflunomide. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy.
- trastuzumab deruxtecan
trastuzumab deruxtecan, teriflunomide. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy.
- treprostinil
teriflunomide increases levels of treprostinil by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- tretinoin
teriflunomide increases levels of tretinoin by Other (see comment). Use Caution/Monitor. Comment: Teriflunomide inhibits CYP2C8; caution when coadministered with CYP2C8 substrates.
- trifluoperazine
teriflunomide decreases levels of trifluoperazine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
Minor (0)
Adverse Effects
>10%
Headache (19-22%)
Diarrhea (15-18%)
Increased ALT (12-14%)
Alopecia (10-13%)
Influenza (9-12%)
Nausea (9-14%)
Paresthesia (9-10%)
Phosphatemia (5-18%)
1-10%
URTI (9%)
Bronchitis (5-8%)
Upper abdominal pain (5-6%)
Sinusitis (4-6%)
Musculoskeletal pain (4-5%)
Hypertension (4%)
Toothache (4%)
Increased GGT (3-5%)
Anxiety (3-4%)
Myalgia (3-4%)
Pruritus (3-4%)
Blurred vision (3%)
Cystitis (2-4%)
Viral gastroenteritis (2-4%)
Oral herpes (2-4%)
Neutropenia (2-4%)
Increased AST (2-3%)
Seasonal allergy (2-3%)
Burning sensation (2-3%)
Palpitations (2-3%)
Decreased weight (2-3%)
Decreased neutrophil count (2-3%)
Sciatica (1-3%)
Conjunctivitis (1-3%)
Increased WBC (1-3%)
Acne (1-3%)
Carpal tunnel syndrome (1-3%)
Leukopenia (1-2%)
Abdominal distention (1-2%)
<1%
Cardiovascular death (0.25%)
Postmarketing Reports
Hypersensitivity reactions
Severe skin reactions (including toxic epidermal necrolysis and Stevens-Johnson syndrome, drug reaction with eosinophilia and systemic symptoms)
Thrombocytopenia
Interstitial lung disease
Pancreatitis
Colitis
Psoriasis or worsening of psoriasis (including pustular psoriasis and nail psoriasis); nail disorders
Warnings
Black Box Warnings
Hepatotoxicity
- Clinically significant and potentially life-threatening liver injury, including acute liver failure requiring transplant, reported
- Concomitant use of teriflunomide with other potentially hepatotoxic drugs may increase the risk of severe liver injury
- Obtain transaminase and bilirubin levels within 6 months before initiating therapy; monitor ALT levels at least monthly for 6 months after starting therapy
- If drug-induced liver injury is suspected, discontinue treatment and start an accelerated elimination procedure with cholestyramine or charcoal
- Contraindicated in patients with severe hepatic impairment; patients with pre-existing liver disease may be at increased risk of developing elevated serum transaminases during treatment
Embryofetal toxicity
- Use is contraindicated in pregnant women and in females of reproductive potential who are not using effective contraception because of the potential for fetal harm
- Teratogenicity and embryo lethality occurred in animals at plasma teriflunomide exposures lower than that in humans
- Exclude pregnancy before initiating treatment in females of reproductive potential
- Females of reproductive potential should use effective contraception during treatment and during an accelerated drug elimination procedure after treatment
- Stop teriflunomide and use an accelerated drug elimination procedure if patient becomes pregnant
Contraindications
History of hypersensitivity reaction to teriflunomide, leflunomide, or excipients
Severe hepatic impairment
Pregnancy
Current leflunomide treatment
Cautions
Risk of malignancy, particularly lymphoproliferative disorders, is increased with use of some immunosuppressive medications; there is potential for immunosuppression with this drug; no apparent increase in the incidence of malignancies and lymphoproliferative disorders reported in clinical trials, but larger and longer-term studies would be needed to determine whether there is an increased risk of malignancy or lymphoproliferative disorders with therapy
No clinical data available on efficacy and safety of live vaccinations in patients receiving therapy; vaccination with live vaccines is not recommended; the long half-life of the drug should be considered when contemplating administration of a live vaccine after stopping therapy
May take an average of 8 months to clear drug from plasma; consider accelerated elimination with cholestyramine or activated charcoal
Decreases in white blood cell count and platelet count have been observed; a recent CBC should be available before starting teriflunomide; monitor for signs and symptoms of infection; consider suspending treatment with teriflunomide in case of serious infection; do not start teriflunomide in patients with active infections
Not recommended for patients with serious immunodeficiency; do not initiate treatment in patients with active acute or chronic infections
Peripheral neuropathy, including polyneuropathy and mononeuropathy, have been reported; evaluate patient and consider discontinuing therapy; if a patient taking drug develops symptoms consistent with peripheral neuropathy, such as bilateral numbness or tingling of hands or feet, consider discontinuing therapy and performing accelerated elimination procedure
May cause an increase in renal uric acid clearance and decreases in serum uric acid
Use caution in hyperkalemia
Anaphylaxis and severe allergic reactions reported; signs and symptoms have included dyspnea, urticaria, and angioedema including lips, eyes, throat, and tongue; inform patients of signs and symptoms of anaphylaxis and angioedema
May increase blood pressure; measure blood pressure at treatment initiation and monitor blood pressure during treatment; elevated blood pressure should be appropriately managed during treatment
Interstitial lung disease may be fatal and may occur acutely at any time during therapy with a variable clinical presentation; new onset or worsening pulmonary symptoms, such as cough and dyspnea, with or without associated fever, may be a reason for discontinuation of therapy and for further investigation as appropriate; if discontinuation of the drug is necessary, consider initiation of accelerated elimination procedure
Pancreatitis reported; if pancreatitis is suspected, discontinue teriflunomide and start an accelerated elimination procedure
Cases of tuberculosis reported; prior to initiating therapy, screen patients for latent tuberculosis infection with a tuberculin skin test or with a blood test for mycobacterium tuberculosis infection
Hepatotoxicity
- Clinically significant and potentially life-threatening liver injury, including acute liver failure requiring transplant, reported in patients receiving therapy in the postmarketing setting; patients with pre-existing liver disease and patients taking other hepatotoxic drugs may be at increased risk for developing liver injury when taking this drug; clinically significant liver injury can occur at any time during therapy
- Patients with pre-existing acute or chronic liver disease, or those with serum alanine aminotransferase (ALT) greater than two times upper limit of normal (ULN) before initiating treatment, should not normally be treated with this drug
- Obtain serum transaminase and bilirubin levels within 6 months before initiation of therapy; monitor ALT levels at least monthly for six months after starting treatment; consider additional monitoring when therapy administered with other potentially hepatotoxic drugs
- Consider discontinuing therapy if serum transaminase increase (>3x ULN) is confirmed; monitor serum transaminase and bilirubin, particularly in patients who develop symptoms suggestive of hepatic dysfunction, such as unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, or jaundice and/or dark urine
- If liver injury suspected to be therapy-induced, discontinue drug and start an accelerated elimination procedure and monitor liver tests weekly until normalized; if drug-induced liver injury is unlikely because some other probable cause found, resumption of therapy may be considered
Accelerated elimination of teriflunomide
- This drug is eliminated slowly from plasma; without accelerated elimination procedure, it takes on average 8 months to reach plasma concentrations < 0.02 mg/L, although because of individual variations in drug clearance it may take as long as 2 years
- An accelerated elimination procedure could be used at any time after discontinuation of treatment; elimination can be accelerated by either of the following procedures:
- Administration of cholestyramine 8 g q8hr for 11 days; if cholestyramine 8 g TID not well tolerated, cholestyramine 4 g TID can be used
- Administration of 50 g oral activated charcoal powder every 12 hours for 11 days
- If either elimination procedure is poorly tolerated, treatment days do not need to be consecutive unless there is need to lower teriflunomide plasma concentration rapidly
- At end of 11 days, both regimens successfully have accelerated teriflunomide elimination, leading to more than 98% decrease in teriflunomide plasma concentrations; use of accelerated elimination procedure may potentially result in return of disease activity if patient had been responding to treatment
Skin reactions
- Cases of serious skin reactions, including cases of Stevens-Johnson syndrome (SJS) and a fatal case of toxic epidermal necrolysis (TEN), reported
- Drug reaction with eosinophilia and systemic symptoms (DRESS), also known as multiorgan hypersensitivity, has occurred with therapy; DRESS typically, although not exclusively, presents with fever, rash, lymphadenopathy and/or facial swelling, in association with other organ system involvement, such as hepatitis, nephritis, hematologic abnormalities, myocarditis, or myositis, sometimes resembling an acute viral infection
- Eosinophilia is often present; this disorder is variable in itsexpression, and other organ systems not noted here may be involved; it is important to note that early manifestations of hypersensitivity (eg, fever, lymphadenopathy) may be present even though rash is not evident; if such signs or symptoms are present, the patient should be evaluatedimmediately
- Inform patients of signs and symptoms that may signal a serious skin reaction; instruct patients to discontinue therapy and seek immediate medical care should these signs and symptoms occur
- Unless reaction is clearly not drug-related, discontinue therapy and begin an accelerated elimination procedure immediately; in such cases, patients should not be re-exposed to drug
- Early manifestations of hypersensitivity (eg, fever, lymphadenopathy) may be present even though rash is not evident; if such signs or symptoms are present, the patient should be evaluated immediately
- Discontinue therapy unless an alternative etiology for the signs or symptoms is established, and begin an accelerated elimination procedure immediately; in such cases, patients should not be re-exposed to drug
Bone Marrow Effects / Immunosuppression Potential
- Cases of thrombocytopenia, including rare cases with platelet counts < 50,000/mm3, reported in postmarketing setting; obtain a complete blood cell count (CBC) within 6 months before initiation of treatment; further monitoring should be based on signs and symptoms suggestive of bone marrow suppression
- A mean decrease compared to baseline in white blood cell (WBC) count of approximately 15% (mainly neutrophils and lymphocytes) and in platelet count of approximately 10% observed
- Most reports confounded by concomitant immunosuppressant therapy and/or comorbid illness which, in addition to rheumatoid disease, may predispose patients to infection
Risk of infection
- Patients with active acute or chronic infections should not start treatment until infection(s) is resolved; if patient develops a serious infection consider suspending treatment and using an accelerated elimination procedure; reassess benefits and risks prior to resumption of therapy; instruct patients to report symptoms of infections to a physician
- Therapy not recommended for patients with severe immunodeficiency, bone marrow disease, or severe, uncontrolled infections; medications that have immunosuppression potential may cause patients to be more susceptible to infections, including opportunistic infections
- One fatal case of klebsiella pneumonia sepsis reported in a patient taking this medication (14 mg) for 1.7 years; fatal infections reported in postmarketing setting in patients receiving this drug, especially Pneumocystis jirovecii pneumonia and aspergillosis
- Most reports were confounded by concomitant immunosuppressant therapy and/or comorbid illness which, in addition to rheumatoid disease, may predispose patients to infection; in clinical studies, cytomegalovirus hepatitis reactivation has been observed
- In clinical tirals in adult patients, cases of tuberculosis observed; prior to initiating treatment, screen patients for latent tuberculosis infection with a tuberculin skin test or with blood test for mycobacterium tuberculosis infection
- This drug has not been studied in patients with a positive tuberculosis screen, and safety in individuals with latent tuberculosis infection is unknown; for patients testing positive in tuberculosis screening, treat by standard medical practice prior to administering therapy
Drug interaction overview
- Teriflunomide is CYP2C8 inhibitor, weak CYP1A2 inducer, organic anion transporter 3 (OAT3) inhibitor; BCRP and organic anion transporting polypeptide B1 and B3 (OATP1B1/1B3) inhibitor
- Coadministration with CYP2C8 substrates (eg, paclitaxel, pioglitazone, repaglinide, rosiglitazone) may increase exposure to the CYP2C8 substrates
- Coadministration with warfarin requires close monitoring of INR because teriflunomide may decrease peak INR by ~25%
- Teriflunomide may increase the systemic exposures of ethinylestradiol and levonorgestrel; consider the type or dose of contraceptives used in combination with teriflunomide
- Coadministration with OAT3 substrates may increase exposure of the OAT3 substrates
- Concomitant use with CYP1A2 substrates and teriflunomide may reduce expose of the CYP1A2 substrates
-
Immunosuppressive or immunomodulating therapies
- Coadministration with antineoplastic or immunosuppressive therapies used for treatment of multiple sclerosis has not been evaluated
- When switching from teriflunomide to another agent with a known potential for hematologic suppression, monitor for hematologic toxicity, because there will be overlap of systemic exposure to both compounds
- Use of an accelerated elimination procedure may decrease this risk, but may also potentially result in return of disease activity if the patient had been responding to treatment
Pregnancy & Lactation
Pregnancy
Contraindicated for use in pregnant women and females of reproductive potential not using effective contraception because of potential for fetal harm based on animal data
Exclude pregnancy before initiating treatment in females of reproductive potential; advise females to notify their healthcare provider immediately if pregnancy occurs or is suspected during treatment
Discontinue treatment in female who wish to become pregnantand undergo accelerated elimination procedure to decrease plasma concentration of teriflunomide to less than 0.02 mg/L (0.02 mcg/mL); use effective contraception until is verified that plasma concentrations of teriflunomide are less than 0.02 mg/L (0.02 mcg/mL), which are expected to have minimal embryofetal risk
If patient becomes pregnant during therapy, stop treatment, inform patient of potential risk to fetus, and perform accelerated drug elimination procedure to achieve plasma concentrations of less than 0.02 mg/L (0.02 mcg/mL); refer patient to obstetrician/gynecologist, preferably experienced in reproductive toxicity, for further evaluation and counseling
Pregnancy exposure registry
- Registry monitors pregnancy outcomes in women exposed to therapy during pregnancy; healthcare providers and patients are encouraged to report pregnancies by calling 1-800-745-4447, option 2
Males
- Drug is detected in human semen; animal studies to specifically evaluate risk of male mediated fetal toxicity have not been conducted; to minimize any possible risk, men not wishing to father a child and their female partners should use effective contraception
- Discontinue therapy in men wishing to father a child and either undergo an accelerated elimination procedure or wait until verification that the plasma teriflunomide concentration is less than 0.02 mg/L (0.02 mcg/ml)
- To minimize any possible risk, men not wishing to father a child and their female partners should use effective contraception
Lactation
Not known whether drug is excreted in human milk; detected in rat milk following a single oral dose; because of potential for adverse reactions in a breastfed infant from therapy, women should not breastfeed during treatment
Consider developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Immunomodulatory agent that inhibits dihydroorotate dehydrogenase, a mitochondrial enzyme involved in de novo pyrimidine synthesis
Exact mechanism of action on multiple sclerosis is unknown; may involve reducing the number of lymphocytes in the CNS
Absorption
Peak plasma time: 1-4 hr
Distribution
Protein Bound: >99%
Vd: 11 L (single IV-dose)
Metabolism
Primary biotransformation to minor (inactive) metabolites by hydrolysis
Secondary pathways: Oxidation, N-acetylation, sulfate conjugation
CYP2C8 inhibitor; CYP1A2 inducer
Elimination
Total body clearance: 30.5 mL/hr
Excretion (after 21 days): Feces (60.1%); urine (22.6%)
Administration
Oral Administration
Take with or without food
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| teriflunomide oral - | 14 mg tablet |  | |
| teriflunomide oral - | 14 mg tablet |  | |
| teriflunomide oral - | 7 mg tablet |  | |
| teriflunomide oral - | 14 mg tablet |  | |
| teriflunomide oral - | 14 mg tablet |  | |
| teriflunomide oral - | 7 mg tablet |  | |
| teriflunomide oral - | 7 mg tablet |  | |
| teriflunomide oral - | 7 mg tablet |  | |
| teriflunomide oral - | 14 mg tablet |  | |
| teriflunomide oral - | 7 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
teriflunomide oral
TERIFLUNOMIDE - ORAL
(TER-i-FLOO-noe-mide)
COMMON BRAND NAME(S): Aubagio
WARNING: Teriflunomide must not be used during pregnancy because it may cause serious harm (such as birth defects, death) in an unborn baby. Women of childbearing age must have a negative pregnancy test before starting this medication. Men and women must use reliable forms of birth control (such as condoms, birth control pills) while taking teriflunomide and for as long as directed by your doctor to prevent pregnancy. After stopping treatment with teriflunomide, your doctor may prescribe a different drug to help speed up the removal of teriflunomide from your body. If you become pregnant or think you may be pregnant or cause a pregnancy, tell your doctor right away. (See also How to Use and Precautions sections.)This drug may rarely cause serious (possibly fatal) liver disease. Careful monitoring by your doctor may help decrease your risk. Your doctor will perform liver function tests before you start treatment and once a month for at least the first 6 months of treatment. Tell your doctor right away if you notice nausea/vomiting that doesn't stop, dark urine, loss of appetite, stomach/abdominal pain, or yellowing eyes/skin.
USES: This medication is used by adults to treat multiple sclerosis-MS. It is not a cure for MS but is thought to work by decreasing certain immune system cells (lymphocytes) which can attack the nerves in your brain and spinal cord. This helps decrease the number of flare-ups (relapses) and may help slow down physical problems caused by MS.
HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking teriflunomide and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily. The dosage is based on your medical condition and response to treatment.Take this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.After treatment is stopped, your doctor may prescribe a different drug (cholestyramine or activated charcoal powder) to help speed up the removal of teriflunomide from your body. This may be used if you have severe side effects, or if you are a woman of childbearing age, or a man planning to father a child. Otherwise, teriflunomide can stay in your body for as long as 2 years after stopping treatment. Consult your doctor or pharmacist for more details.Tell your doctor if your symptoms do not improve or if they worsen.
SIDE EFFECTS: See also Warning section.Diarrhea, nausea, or tingling/burning/numbness/prickling feelings in your skin may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.Temporary hair loss may occur. Normal hair growth should return after treatment has ended.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: easy bruising/bleeding, new/worsening shortness of breath, new/worsening numbness/tingling of hands/feet, pain in your side (flank pain), symptoms of high potassium blood levels (such as muscle weakness, slow/irregular heartbeat), unusual tiredness.This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high.This medication may lower your ability to fight infections. This may make you more likely to get a serious (rarely fatal) infection or make any infection you have worse. Get medical help right away if you have any signs of infection (such as sore throat that doesn't go away, fever, chills, cough, swollen lymph nodes).Teriflunomide can cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking teriflunomide, tell your doctor or pharmacist if you are allergic to it; or to leflunomide; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: bone marrow/blood disorder, immune system disorder (such as due to cancer, HIV infection), current/recent infection (such as tuberculosis), high blood pressure, liver problems, lung disease.Teriflunomide can make you more likely to get infections or may make current infections worse. Stay away from anyone who has an infection that may easily spread (such as chickenpox, COVID-19, measles, flu). Talk to your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using teriflunomide before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Teriflunomide may pass into the semen of men treated with this medication and the effects on sperm are unknown. Men not wishing to father a child with their female partners should use reliable birth control (such as condoms). After stopping this medication, men wishing to father a child should take a different drug as prescribed by the doctor to speed up removal of teriflunomide from the body. (See also How to Use section.)This medication must not be used during pregnancy. It may harm an unborn baby. Before starting this medication, women of childbearing age must have a negative pregnancy test. Discuss the use of reliable forms of birth control (such as birth control pills, intrauterine device-IUD) with your doctor. If you become pregnant or think you may be pregnant, tell your doctor right away. See also Warning section.This drug may pass into breast milk and could have undesirable effects on a nursing infant. Breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Because leflunomide (used to treat rheumatoid arthritis) is very similar to this medication, do not take it while you are taking teriflunomide.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as tuberculosis skin test, kidney/liver function, complete blood counts, blood pressure, potassium blood levels) should be done before you start taking this medication and while you are taking it. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised March 2023. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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