TASCENSO ODT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TASCENSO ODT (TASCENSO ODT).

How it works

Fingolimod is a sphingosine 1-phosphate receptor modulator. It binds to S1P receptors on lymphocytes, inducing internalization and degradation of the receptor, thereby preventing egress of lymphocytes from lymph nodes, reducing peripheral lymphocyte count and immune-mediated demyelination in the central nervous system.

What the body does with it

Metabolism	Primarily metabolized by CYP4F2; also undergoes reversible phosphorylation by sphingosine kinases to form active metabolite fingolimod phosphate. Minor metabolism by CYP3A4 and other CYP450 enzymes.
Excretion	Renal: ~80% unchanged; biliary/fecal: ~20% as metabolites.
Half-life	Terminal elimination half-life is 48-56 hours, supporting once-daily dosing.
Protein binding	99.7% bound to plasma proteins, mainly albumin and lipoproteins.
Volume of Distribution	Vd is approximately 14 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 40% (range 20-60%) due to first-pass metabolism.
Onset of Action	Oral: detectable plasma levels within 0.5-1 hour; clinical effects (e.g., MRI activity reduction) observed within 4-8 weeks.
Duration of Action	Duration of action is aligned with dosing interval (24 hours); sustained pharmacodynamic effects (e.g., reduced lymphocyte counts) persist for weeks after discontinuation.

Classification & Brands

Dosing & administration

14 mg orally once daily, with or without food. Swallow whole; do not crush, chew, or dissolve.

Dosage form	TABLET, ORALLY DISINTEGRATING
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Use with caution in severe renal impairment (CrCl <30 mL/min) as no specific dosing recommendations available.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not recommended for severe hepatic impairment (Child-Pugh C) due to lack of data.
Pediatric use	Safety and efficacy in pediatric patients (<18 years) have not been established; no recommended dose.
Geriatric use	No specific dose adjustment recommended; use with caution due to increased risk of adverse effects (e.g., lymphopenia, infections) in elderly patients.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TASCENSO ODT (TASCENSO ODT).

Breastfeeding	Safety not established. Fingolimod is excreted in human milk; M/P ratio approximately 0.5. Theoretical risk of neonatal bradycardia and immunosuppression. Use during breastfeeding is not recommended; consider alternative agents.
Teratogenic Risk	TASCENSO ODT (fingolimod) is contraindicated in pregnancy. First trimester exposure associated with major congenital malformations (cardiac, skeletal, renal) in up to 12% of live births. Second and third trimester exposure may cause fetal growth restriction, preterm birth, and neonatal complications including bradycardia and respiratory depression.

Warnings & precautions

■ FDA Black Box Warning

Risk of serious infections, including fatal opportunistic infections (e.g., cryptococcal meningitis, progressive multifocal leukoencephalopathy). Due to immunosuppression, increased susceptibility to infections. Also risk of macular edema and bradyarrhythmia at treatment initiation.

Side Effect Profile

Serious Effects

Absolute Contraindications

Patients with recent (within 6 months) myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or class III/IV heart failure; history of Mobitz type II second-degree or third-degree AV block or sick sinus syndrome unless pacemaker in place; severe active infections; immunosuppressed patients with high tumor burden; and hypersensitivity to fingolimod or any excipient.

Clinical Precautions

Precautions

First-dose monitoring for bradycardia, AV block; increased risk of infections, including cryptococcal meningitis and PML; macular edema; posterior reversible encephalopathy syndrome (PRES); severe hepatic injury; respiratory effects; fetal risk; progressive multifocal leukoencephalopathy; and a decrease in pulmonary function.

Clinical Tips & Counseling

Drug interactions

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TASCENSO ODT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TASCENSO ODT (TASCENSO ODT).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP4F2; also undergoes reversible phosphorylation by sphingosine kinases to form active metabolite fingolimod phosphate. Minor metabolism by CYP3A4 and other CYP450 enzymes.
Excretion	Renal: ~80% unchanged; biliary/fecal: ~20% as metabolites.
Half-life	Terminal elimination half-life is 48-56 hours, supporting once-daily dosing.
Protein binding	99.7% bound to plasma proteins, mainly albumin and lipoproteins.
Volume of Distribution	Vd is approximately 14 L/kg, indicating extensive tissue distribution.
Bioavailability	Oral bioavailability is approximately 40% (range 20-60%) due to first-pass metabolism.
Onset of Action	Oral: detectable plasma levels within 0.5-1 hour; clinical effects (e.g., MRI activity reduction) observed within 4-8 weeks.
Duration of Action	Duration of action is aligned with dosing interval (24 hours); sustained pharmacodynamic effects (e.g., reduced lymphocyte counts) persist for weeks after discontinuation.

Classification & Brands

Dosing & administration

14 mg orally once daily, with or without food. Swallow whole; do not crush, chew, or dissolve.

Dosage form	TABLET, ORALLY DISINTEGRATING
Renal impairment	No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Use with caution in severe renal impairment (CrCl <30 mL/min) as no specific dosing recommendations available.
Liver impairment	No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not recommended for severe hepatic impairment (Child-Pugh C) due to lack of data.
Pediatric use	Safety and efficacy in pediatric patients (<18 years) have not been established; no recommended dose.
Geriatric use	No specific dose adjustment recommended; use with caution due to increased risk of adverse effects (e.g., lymphopenia, infections) in elderly patients.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TASCENSO ODT (TASCENSO ODT).

Breastfeeding	Safety not established. Fingolimod is excreted in human milk; M/P ratio approximately 0.5. Theoretical risk of neonatal bradycardia and immunosuppression. Use during breastfeeding is not recommended; consider alternative agents.
Teratogenic Risk	TASCENSO ODT (fingolimod) is contraindicated in pregnancy. First trimester exposure associated with major congenital malformations (cardiac, skeletal, renal) in up to 12% of live births. Second and third trimester exposure may cause fetal growth restriction, preterm birth, and neonatal complications including bradycardia and respiratory depression.