Fingolimod comes from the fungus Isaria sinclairii, originally associated with traditional Chinese medicine
Classified as
a sphingosine-1-phosphate receptor modulating agent.
Both
Neither
Clinical use/uses for fingolimod:
Treating relapsing multiple sclerosis
May be used in treating chronic inflammatory demyelinating polyneuropathy.
Both
Neither
Fingolimod administration produces immunomodulation by lymphocyte sequestration.
True
False
Fingolimod exhibits structural similarity to sphingosine:
True
False
Fingolimod pharmacokinetics:
Slow and food-independent fingolimod absorption following oral administration.
Good oral bioavailability (about 93%)
Both
Neither
Fingolimod pharmacokinetics: metabolic pathways
Phosphorylation to fingolimod phosphate by sphingosine kinases
Hydroxylation/oxidation mediated by the cytochrome P450 drug metabolizing enzyme isoform CYP4F2 (inactivating step).
Also, metabolism results in non-polar ceramide species.
Both
Neither
Fingolimod exhibits relatively slow clearance from blood with a terminal half-life on the order of
a week following repetitive drug administration.
True
False
In addition to lymphopenia as the mechanism by which fingolimod modifies multiple sclerosis, this agent may also influence which one(s) of the following?
Gliosis
Neurodegeneration
Both
Neither
Fingolimod cardiotoxicities:
Bradycardia as well as prolongation of QT interval
Cardiotoxicities necessitate cardiac monitoring following first dose (6 hour monitoring)
If you wish to return to the Table of Contents
in ENGLISH, press the RETURN button above.
Otherwise, if the text is NOT displayed in
English and you are ready to leave this page,
Press here
to return to the Table of Contents
Source Material:
Rothlin C Gutkind J Chapter 39
Immunosuppressants, Immunomodulation and Tolerance In
Goodman & Gilman's The Pharmacological Basis of Therapeutics
(Brunton LL Knollman BC eds) McGraw Hill LLC (2023).
Lake D & Briggs A Ch 55 Immunopharmacology
in Katzung's Basic & Clinical Pharmacology (Vanderah TW, ed)
16e McGraw Hill 2023.
Chrouos G Ch 39 Adrenocorticosteroids &
Adrenocortical Antagonists in Katzung's Basic & Clinical
Pharmacology (Vanderah TW, ed) 16e McGraw Hill 2023
Brezinski E Klickstein L Armstrong A Ch 46
Pharmacology of Immunosuppression in Principles of
Pharmacology: The Pathophysiologic Basis of Drug Therapy.
(Golan DE Armstrong EJ Armstrong AW, eds) 4e 2017 ls) 4e
2017
Ritter JM Flower R Henderson G Loke YK
MacEwan D Robinson E Fullerton J Ch 54 Anti-inflammatory and
Immunosuppressant Drugs Rang & Dale's Pharmacology 10e
Elsevier 2024.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 72 Immunosuppressants Elsevier 2022.
Burchum J Rosenthal L Lehne's Pharmacology
for Nursing Care Ch 75 Glucocorticoids in Nonendrocrine
Disorders Elsevier 2022.
Bass A Rogatsky Ch 32 Immunomodulatory Drugs
in Goldman-Cecil Medicine (Goldman L Schafer, eds) Elsevier
26e 2020
Leiva M Takemoto Ch 238 Immunosuppressants in
Lippincott Illustrated Reviews: Pharmacology 8e ((Walen et
al, eds) Wolters Kluwer 2023.
Hall J Hall M Ch 78 Adrenocortical
Hormones Guyton and Hall Textbook of Medical Physiology 14e
Elsevier 2021.
