FOROPAFANT

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H40N4S
Molecular Weight	464.709
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(C)C1=CC(C(C)C)=C(C2=CSC(=N2)N(CCN(C)C)CC3=CN=CC=C3)C(=C1)C(C)C

InChI

InChIKey=VVBFISAUNSXQGZ-UHFFFAOYSA-N

InChI=1S/C28H40N4S/c1-19(2)23-14-24(20(3)4)27(25(15-23)21(5)6)26-18-33-28(30-26)32(13-12-31(7)8)17-22-10-9-11-29-16-22/h9-11,14-16,18-21H,12-13,17H2,1-8H3

HIDE SMILES / InChI

Molecular Formula	C28H40N4S
Molecular Weight	464.709
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

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

Description

Foropafant is a platelet-activating factor (PAF) antagonist which was developed by Sanofi. It was in clinical development for the treatment of asthma, thrombosis and ulcerative colitis. The development of the drug was discontinued due to lack of efficacy.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Platelet-activating factor receptor 3	Antagonist 2,849		57.0 pM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Ulcerative colitis 125	Primary	Not Provided 511	Unknown
Acute asthma 2	Primary	Not Provided 511	Unknown
Thrombosis 22	Primary	Not Provided 511	Unknown

PubMed

Show entries

Title	Date	PubMed
Effect of SR 27417 on the binding of [3H]PAF to rabbit and human platelets and human polymorphonuclear leukocytes.	1993 May	8395255
Role of tachykinins in castor oil diarrhoea in rats.	1997 Jun	9179376
Platelet-leukocyte cross talk in whole blood.	2000 Dec	11116075
Activation of PAF receptor by oxidised LDL in human monocytes stimulates chemokine releases but not urokinase-type plasminogen activator expression.	2004 Jun	15149885

Showing 1 to 4 of 4 entries

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Patents

Sample Use Guides

In Vivo Use Guide

In acute asthma study, foropafant was administered orally at 20 mg dosage

Route of Administration: Oral

In Vitro Use Guide

Foropafant displayed marked in vitro inhibition of PAF-induced oxidative burst in guinea pig macrophages (IC50 = 32 nM). Foropafant potently inhibited PAF-induced aggregation of rabbit and human platelets in vitro (IC50 = 0.10 and 0.50 nM, respectively).