MAYZENT Film-coated tablet (2020)

Βιβλιογραφική αναφορά

Συγγραφείς

Novartis Pharmaceuticals Corporation

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1. Indications and Usage

MAYZENT is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in ...

2. Dosage and Administration

2.1 Assessments Prior to First Dose of MAYZENT Before initiation of treatment with MAYZENT, assess the following: CYP2C9 Genotype Determination: Test patients for CYP2C9 variants to determine CYP2C9 ...

3. Dosage Forms and Strengths

0.25 mg tablet: Pale red, unscored, round biconvex film-coated tablet with beveled edges, debossed with on one side and T on other side. 2 mg tablet: Pale yellow, unscored, round biconvex film-coated ...

4. Contraindications

MAYZENT is contraindicated in patients who have: A CYP2C9*3/*3 genotype [see Use in Specific Populations (8.6) and Clinical Pharmacology (12.5)] In the last 6 months experienced myocardial infarction, ...

5. Warnings and Precautions

5.1 Infections Risk of Infections MAYZENT causes a dose-dependent reduction in peripheral lymphocyte count to 20% to 30% of baseline values because of reversible sequestration of lymphocytes in lymphoid ...

6. Adverse Reactions

The following serious adverse reactions are described elsewhere in labeling: Infections [see Warnings and Precautions (5.1)] Macular Edema [see Warnings and Precautions (5.2)] Bradyarrhythmia ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reactions rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

7. Drug Interactions

7.1 Anti-Neoplastic, Immune-Modulating, or Immunosuppressive Therapies MAYZENT has not been studied in combination with anti-neoplastic, immune-modulating, or immunosuppressive therapies. Caution should ...

8. Use in Specific Populations

8.6 CYP2C9 Genotype Before initiation of treatment with MAYZENT, test patients to determine CYP2C9 genotype. MAYZENT is contraindicated in patients homozygous for CYP2C9*3 (i.e., CYP2C9*3/*3 genotype), ...

8.1. Pregnancy

Risk Summary There are no adequate data on the developmental risk associated with the use of MAYZENT in pregnant women. Based on animal data and its mechanism of action, MAYZENT can cause fetal harm when ...

8.2. Lactation

Risk Summary There are no data on the presence of siponimod in human milk, the effects of MAYZENT on the breastfed infant, or the effects of the drug on milk production. A study in lactating rats has shown ...

8.3. Females and Males of Reproductive Potential

Contraception Females Before initiation of MAYZENT treatment, women of childbearing potential should be counselled on the potential for a serious risk to the fetus and the need for effective contraception ...

8.4. Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

8.5. Geriatric Use

Clinical studies of MAYZENT did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not ...

10. Overdosage

In patients with overdosage of MAYZENT, it is important to observe for signs and symptoms of bradycardia, which may include overnight monitoring. Regular measurements of pulse rate and blood pressure are ...

11. Description

MAYZENT tablets contains siponimod, an S1P receptor modulator, as 2:1 co-crystal of siponimod and fumaric acid and has the following chemical name: 1-[[4-[(1E)1[[[4-Cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-3-azetidinecarboxylic ...

12.1. Mechanism of Action

Siponimod is an S1P receptor modulator. Siponimod binds with high affinity to S1P receptors 1 and 5. Siponimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes ...

12.2. Pharmacodynamics

Immune System MAYZENT induces a dose-dependent reduction of the peripheral blood lymphocyte count within 6 hours of the first dose, caused by the reversible sequestration of lymphocytes in lymphoid tissues. ...

12.3. Pharmacokinetics

Siponimod concentration increases in an apparent dose-proportional manner after multiple once-daily doses of siponimod 0.3 mg to 20 mg. Steady-state plasma concentrations are reached after approximately ...

12.5. Pharmacogenomics

The CYP2C9 genotype has a significant impact on siponimod metabolism. After a single dose of 0.25 mg siponimod, AUCinf and AUClast was approximately 2- and 4-fold higher in subjects ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis Oral carcinogenicity studies of siponimod were conducted in mice and rats. In mice administered siponimod (0, 2, 8, or 25 mg/kg/day) for up to 104 weeks, there was an increase in malignant ...

14. Clinical Studies

The efficacy of MAYZENT was demonstrated in Study 1, a randomized, double-blind, parallel-group, placebo-controlled, time-to-event study in patients with secondary progressive multiple sclerosis (SPMS) ...

16.1 How Supplied

MAYZENT film-coated tablets are supplied as follows: 0.25 mg tablet: Pale red, unscored, round biconvex film-coated tablet with beveled edges, debossed with p=. on one side and T on other side. Starter ...

16.2 Storage and Handling

Unopened Containers Store MAYZENT 0.25 mg and 2 mg film-coated tablets in a refrigerator between 2°C to 8°C (36°F to 46°F). After pharmacy dispensing to patient, MAYZENT 0.25 mg and 2 mg film-coated tablets ...

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Medication Guide). Tell patients not to discontinue MAYZENT without first discussing this with the prescribing physician. Advise patients to ...