L04AE01 - Fingolimod |
Propably not porphyrinogenic |
PNP |
Important Information
Patients on immunosuppressive therapy have an increased risk of infections. Since infections have a potential to trigger acute porphyric attacks vigilance is motivated regarding signs or symptoms of infection and/or possible symptoms of a porphyric attack. Diarrhoea is a very common side effect that may potentially be porphyrinogenic through reduction in carbohydrate intake.
Side effects
Infections are common in patients using immunosuppressants and since infections might trigger an acute porphyric attack, vigilance regarding signs and symptoms of an infection and/ or a porphyric attack is recommended. Diarrhoea is a very common side effect that can be potentially porphyrinogenic through reduction in carbohydrate intake.
Rationale
Fingolimod is mainly metabolized by CYP4F2, and has little or no capacity to inhibit or induce expression of CYP enzymes.
Chemical description
Fingolimod is a sphingosine 1-phosphate receptor modulator
Therapeutic characteristics
Fingolimod is used in the treatment of relapsing forms of multiple sclerosis. It is administered orally.
Metabolism and pharmacokinetics
Fingolimod is biotransformed by reversible stereoselective phosphorylation to the pharmacologically active (S)-enantiomer of fingolimod-phosphate, by oxidative biotransformation mainly via the cytochrome P450 4F2 isoenzyme and subsequent fatty acid-like degradation to inactive metabolites, and by formation of pharmacologically inactive non-polar ceramide analogs of fingolimod.
Fingolimod is primarily metabolized via human CYP4F2 with a minor contribution of CYP2D6, 2E1, 3A4, and 4F12. (FDA)
Co-administration of fingolimod with ciclosporin did not elicit any change in the ciclosporin or fingolimod exposure. Also, co-administration of fingolimod with oral contraceptives (ethinylestradiol and levonorgestrel) did not elicit any change in oral contraceptive exposure. Fingolimod has little or no capacity to inhibit or induce expression of CYP enzymes (SPC, David 2012).
References
- Scientific articles
- David OJ, Kovarik JM et al. Clinical pharmacokinetics of fingolimod. Clin Pharmacokinet 2012 Jan 1;51 (1): 15-28. PMID 22149256. #4753
- Drug reference publications
- DrugBank. fingolimod. #3120
- Micromedex® 2.0 (electronic version). Fingolimod. (Drugdex System). (19.11.2014). #3121
- Government bodies
- U.S Food and Drug Administration (FDA). Label information. Fingolimod. #3123
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). Gilenya. #3122
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