Asengeprast

Investigational

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=CC(\C=C\C(=O)NC2=CC=CC=C2C(O)=O)=CC=C1OCC#C

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+

HIDE SMILES / InChI

Molecular Formula	C20H17NO5
Molecular Weight	351.3527
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Approval Year

Patents

Patents

Substance Class	Chemical
Record UNII	C6V7ZU2NPR
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

Asengeprast

Official Name

English

2-[(2E)-3-{3-methoxy-4-[(prop-2-yn-1-yl)oxy]phenyl}prop-2-enamido]benzoic acid

Preferred Name

English

Benzoic acid, 2-[[(2E)-3-[3-methoxy-4-(2-propyn-1-yloxy)phenyl]-1-oxo-2-propen-1-yl]amino]-

Systematic Name

English

FT-011

Code

English

asengeprast [INN]

Common Name

English

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Code System

Code

Type

Description

INN

13056

PRIMARY

NCI_THESAURUS

C206878

PRIMARY

PUBCHEM

23648966

PRIMARY

FDA UNII

C6V7ZU2NPR

PRIMARY

SMS_ID

300000033002

PRIMARY

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Type

Details


					T7D25J14LT

HUMAN TRANSFORMING GROWTH FACTOR .BETA.-1

TARGET -> INHIBITOR

Interaction Type:

IN-VITRO

Amount:

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Type

Details


					C6V7ZU2NPR

Asengeprast

ACTIVE MOIETY

Comments:

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.

Amount:


					C6V7ZU2NPR

Asengeprast

ACTIVE MOIETY

Comments:

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

Amount:

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