Identification | Back Directory | [Name]
Gilenia | [CAS]
162359-55-9 | [Synonyms]
Gilenia Fingolise fingolimo fenogliMod Fingolimod FingoliMod-D4 FingoliMod Base Gilenia USP/EP/BP Gilenya(Fingolise) Fingolimod(FTY720) Gilenia, Fingolimod 2-amino-2-(4-octylphenethyl)propane-1,3-diol 2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol 2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol 1,3-Propanediol,2-aMino-2-[2-(4-octylphenyl)ethyl]- | [EINECS(EC#)]
1308068-626-2 | [Molecular Formula]
C19H33NO2 | [MDL Number]
MFCD14705150 | [MOL File]
162359-55-9.mol | [Molecular Weight]
307.47 |
Chemical Properties | Back Directory | [Melting point ]
103-105° | [Boiling point ]
479.5±45.0 °C(Predicted) | [density ]
1.016 | [storage temp. ]
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | [solubility ]
Chloroform (Very Slightly, Heated), DMSO (Slightly, Heated), Methanol (Slightly, | [form ]
Solid | [pka]
12.20±0.20(Predicted) | [color ]
Off-White |
Hazard Information | Back Directory | [Chemical Properties]
white solid | [Uses]
Prophylaxis of organ rejection
in patients receiving allogenic renal transplants (sphingosine-1-phosphate receptor). | [Definition]
ChEBI: An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimo
is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate. | [Clinical Use]
Sphingosine 1-phosphate receptor modulator:Treatment of highly active relapsing-remitting
multiple sclerosis | [Drug interactions]
Potentially hazardous interactions with other drugs
Anti-arrhythmics: possible increased risk of
bradycardia with amiodarone, disopyramide and
dronedarone.
Antifungals: concentration increased by
ketoconazole.
Beta-blockers: possibly increased risk of bradycardia.
Calcium channel blockers: possible increased risk of
bradycardia with diltiazem and verapamil. | [Metabolism]
Transformed by reversible stereoselective phosphorylation
to the pharmacologically active (S)-enantiomer of
fingolimod phosphate. It is eliminated 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 analogues
of fingolimod. The main enzyme involved in the
metabolism of fingolimod is partially identified and may
be either CYP4F2 or CYP3A4.
81% excreted as inactive metabolites in the urine and
<2.5% in the faeces as metabolites and unchanged drug. |
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