Gilenia Property

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,

pka

12.20±0.20(Predicted)

form 

Solid

color 

Off-White

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H402Harmful to aquatic life

H412Harmful to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

Gilenia Chemical Properties,Usage,Production

Chemical Properties

white solid

Uses

Prophylaxis of organ rejection in patients receiving allogenic renal transplants (sphingosine-1-phosphate receptor).

Uses

Fingolimod is a novel immune modulator that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs.

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.