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Details

Stereochemistry ACHIRAL
Molecular Formula C19H30F3NO3
Molecular Weight 377.4416
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMISELIMOD

SMILES

CCCCCCCOC1=CC=C(CCC(N)(CO)CO)C=C1C(F)(F)F

InChI

InChIKey=JVCPIJKPAKAIIP-UHFFFAOYSA-N
InChI=1S/C19H30F3NO3/c1-2-3-4-5-6-11-26-17-8-7-15(12-16(17)19(20,21)22)9-10-18(23,13-24)14-25/h7-8,12,24-25H,2-6,9-11,13-14,23H2,1H3

HIDE SMILES / InChI

Description

Amiselimod (MT-1303) is a selective sphingosine 1-phosphate 1 (S1P1 ) receptor modulator which is currently being developed for the treatment of various autoimmune diseases. Unlike some other S1P receptor modulators, amiselimod seemed to show a favourable cardiac safety profile in preclinical, phase I and II studies. Amiselimod may be potentially useful for treatment of multiple sclerosis; inflammatory diseases; autoimmune diseases; psoriasis and inflammatory bowel diseases. Amiselimod is currently being developed by Mitsubishi Tanabe Pharma Corporation.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
0.211 ng/g
0.4 mg single, oral
AMISELIMOD plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
120 ng × h/g
0.4 mg single, oral
AMISELIMOD plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
451 h
0.4 mg single, oral
AMISELIMOD plasma
Homo sapiens

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer




Drug as victim

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
A total of 81 healthy subjects aged 18-55 years were equally randomized to receive amiselimod 0.4 mg, amiselimod 0.8 mg, placebo or fingolimod 0.5 mg once daily for 28 days.
Route of Administration: Oral
In Vitro Use Guide
HEK293 cells or HCMs were plated onto 48-well culture plates, cultured overnight and then incubated with 100 nmol/L of amiselimod for 3–12 h.