Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H17NO5 |
| Molecular Weight | 351.3527 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(OCC#C)C=CC(\C=C\C(=O)NC2=C(C=CC=C2)C(O)=O)=C1
InChI
InChIKey=UIWZIDIJCUEOMT-PKNBQFBNSA-N
InChI=1S/C20H17NO5/c1-3-12-26-17-10-8-14(13-18(17)25-2)9-11-19(22)21-16-7-5-4-6-15(16)20(23)24/h1,4-11,13H,12H2,2H3,(H,21,22)(H,23,24)/b11-9+
| Molecular Formula | C20H17NO5 |
| Molecular Weight | 351.3527 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:28:32 UTC 2023
by
admin
on
Sat Dec 16 11:28:32 UTC 2023
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| Record UNII |
C6V7ZU2NPR
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| Record Status |
Validated (UNII)
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| Record Version |
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23648966
Created by
admin on Sat Dec 16 11:28:32 UTC 2023 , Edited by admin on Sat Dec 16 11:28:32 UTC 2023
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C6V7ZU2NPR
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300000033002
Created by
admin on Sat Dec 16 11:28:32 UTC 2023 , Edited by admin on Sat Dec 16 11:28:32 UTC 2023
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1001288-58-9
Created by
admin on Sat Dec 16 11:28:32 UTC 2023 , Edited by admin on Sat Dec 16 11:28:32 UTC 2023
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TARGET -> INHIBITOR |
IN-VITRO
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ACTIVE MOIETY |
FT011 is Fibrotechs lead anti-fibrotic compound currently in clinical development for diabetic nephropathy. Kidney failure in diabetes occurs as a result of kidney fibrosis (scarring). This fibrosis is in turn due to the long term damage from excessive sugar levels in the blood.
In preclinical testing FT011 was effective at preventing kidney fibrosis in animal models of diabetic kidney disease.
The Phase Ia study was a double blind, randomised, placebo-controlled, dose-escalating study of the safety, tolerability, food effect and pharmacokinetics of single and repeat doses of FT011 administered orally to healthy volunteers. There were three stages in the study. In the first stage, 40 healthy volunteers received single doses of FT011 (10, 30, 100, 300 and 1000 mg). In the second stage, 8 heathy volunteers were given a 100mg dose under fed rather than fasting conditions to examine food effects. In the third and final stage healthy volunteers were administered daily doses of FT011 (250 or 500mg) for 14 days. All stages of the study demonstrated the safety and tolerability of FT011 with a once daily pharmacokinetic profile and no food effects or any observed adverse events.
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ACTIVE MOIETY |
Originator: Fibrotech Therapeutics, University of Melbourne; Developer: Shire; Class: Anthranilic acid, Antifibrotic, Caffeic acid, Small molecule; Mechanism of Action: Collagen inhibitor, Platelet-derived growth factor inhibitor, TGF-beta superfamily protein inhibitor;
Highest Development Phases: Phase I for Diabetic nephropathies, Focal segmental glomerulosclerosis, Preclinical for Heart failure, Kidney disorders; Most Recent Events: 02 May 2014 Fibrotech Therapeutics has been acquired by Shire, 11 Mar 2014 Fibrotech initiates a phase Ib trial for Diabetic nephropathy in Australia, 10 Mar 2014 Adverse events data from a phase Ia trial in Diabetic nephropathy (in volunteers) released by Fibrotech Therapeutics
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