Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C20H24FN3O2S.C4H6O4 |
Molecular Weight | 507.575 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CCC(O)=O.CC(C)(NC(=O)O[C@@H]1CN2CCC1CC2)C3=CSC(=N3)C4=CC=C(F)C=C4
InChI
InChIKey=TWRYSLPYKQOKAO-PKLMIRHRSA-N
InChI=1S/C20H24FN3O2S.C4H6O4/c1-20(2,17-12-27-18(22-17)14-3-5-15(21)6-4-14)23-19(25)26-16-11-24-9-7-13(16)8-10-24;5-3(6)1-2-4(7)8/h3-6,12-13,16H,7-11H2,1-2H3,(H,23,25);1-2H2,(H,5,6)(H,7,8)/t16-;/m1./s1
Molecular Formula | C20H24FN3O2S |
Molecular Weight | 389.487 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C4H6O4 |
Molecular Weight | 118.088 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Ibiglustat (GZ/SAR402671 or Genz-682452) is a small molecule inhibitor of glucosylceramide synthase. Ibiglustat has been demonstrated to effectively lower glycosphingolipid synthesis. Genzyme, a Sanofi Company is developing Ibiglustat for the treatment of Parkinson's Disease, Gaucher Disease, and Fabry Disease.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2063 Sources: http://adisinsight.springer.com/drugs/800036945 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
68 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
142 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
529 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1100 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2420 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
20600 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
26.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/32851809 |
150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered: |
VENGLUSTAT plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/32851809/ |
yes | |||
yes | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02228460
A phase 2 study assessed the safety, pharmacokinetics (PK), pharmacodynamics (PD), and exploratory efficacy of Ibiglustat (GZ/SAR402671) in enzyme replacement therapy treatment-naïve adult male participants diagnosed with Fabry disease: GZ/SAR402671 15 mg once daily orally for 26 weeks.
Route of Administration:
Oral
Substance Class |
Chemical
Created
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Edited
Fri Dec 15 15:55:39 GMT 2023
by
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Fri Dec 15 15:55:39 GMT 2023
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Record UNII |
XW65IGE2BT
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Record Status |
Validated (UNII)
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Record Version |
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