Mayzent Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Mayzent Indications
Indications
Mayzent Dosage and Administration
Adult
Children
Other Modifications
Females and Males of Reproductive Potential
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Counsel women of childbearing potential on the potential for a serious risk to the fetus and the need for effective contraception during treatment with Mayzent. Since it takes approximately 10 days to eliminate the compound from the body after stopping treatment, the potential risk to the fetus may persist and women should use effective contraception during this period
CYP2C9 Genotype
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Test patients to determine CYP2C9 genotype before initiating treatment.
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Mayzent is contraindicated in patients homozygous for CYP2C9*3 (i.e., CYP2C9*3/*3 genotype). Mayzent dosage adjustment is recommended in patients with CYP2C9*1/*3 or *2/*3 genotype.
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The impact of variants other than *2 and *3 on the pharmacokinetics of siponimod has not been evaluated. It is anticipated that variants that result in loss of CYP2C9 function (e.g., *6) will have similar effects on siponimod pharmacokinetics as the *3 variant.
Mayzent Contraindications
Contraindications
Mayzent Boxed Warnings
Not Applicable
Mayzent Warnings/Precautions
Warnings/Precautions
Mayzent Pharmacokinetics
Absorption
The time (Tmax) to reach maximum plasma concentrations (Cmax) after oral administration of immediate release oral dosage forms of siponimod was about 4 hours (range, 3 to 8 hours). Siponimod absorption is extensive (greater than or equal to 70%, based on the amount of radioactivity excreted in urine and the amount of metabolites in feces extrapolated to infinity). The absolute oral bioavailability of siponimod is approximately 84%. Steady-state was reached after approximately 6 days of once-daily administration of siponimod.
Food intake resulted in delayed absorption (the median Tmax increased by approximately 2 to 3 hours). Food intake had no effect on the systemic exposure of siponimod (Cmax and AUC). Therefore, Mayzent may be taken without regard to meals.
Distribution
Siponimod distributes to body tissues with a moderate mean volume of distribution of 124 L. Siponimod fraction found in plasma is 68% in humans. Animal studies show that siponimod readily crosses the blood-brain barrier. Protein binding of siponimod is greater than 99.9% in healthy subjects and in hepatic and renal impaired patients.
Elimination
The apparent elimination half-life is approximately 30 hours. Siponimod is eliminated from the systemic circulation mainly due to metabolism, and subsequent biliary/fecal excretion. Unchanged siponimod was not detected in urine.
Mayzent Interactions
Interactions
Mayzent Adverse Reactions
Adverse Reactions
Mayzent Clinical Trials
Mayzent Note
Not Applicable
Mayzent Patient Counseling
Cost Savings Program
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