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Details

Stereochemistry ACHIRAL
Molecular Formula C25H36F3N5O3.C4H6O4
Molecular Weight 629.6683
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-04634817 SUCCINATE

SMILES

OC(=O)CCC(O)=O.CO[C@@H]1COCC[C@@H]1N[C@@H]2CC[C@](C2)(C(C)C)C(=O)N3C[C@@H]4C[C@H]3CN4C5=NC=NC(=C5)C(F)(F)F

InChI

InChIKey=WRPPUEHVLSHXJG-HTQYHTRRSA-N
InChI=1S/C25H36F3N5O3.C4H6O4/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22;5-3(6)1-2-4(7)8/h9,14-20,31H,4-8,10-13H2,1-3H3;1-2H2,(H,5,6)(H,7,8)/t16-,17+,18+,19+,20-,24+;/m1./s1

HIDE SMILES / InChI

Molecular Formula C25H36F3N5O3
Molecular Weight 511.5802
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula C4H6O4
Molecular Weight 118.088
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

PF-04634817 is a small molecule chemokine CCR2 and CCR5 receptor dual antagonist. Treatment with PF-04634817 was associated with a modest improvement in best-corrected visual acuity, which was inferior to intravitreal ranibizumab. Analysis of the primary endpoint, Urine Albumin-to-Creatinine Ratio, indicated a modest effect of PF-04634817 in reducing albuminuria in subjects with type 2 diabetes who received angiotensin receptor blocker therapy after 12 weeks of treatment. Despite the tolerable safety profile shown by PF-04634817, clinical development was discontinued in light of the modest efficacy observed.

Originator

Approval Year

PubMed

PubMed

TitleDatePubMed
A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema.
2018 May 1
Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy.
2018 Nov

Sample Use Guides

In Vivo Use Guide
200 mg once daily
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Tue Oct 22 13:15:34 UTC 2019
Edited
by admin
on Tue Oct 22 13:15:34 UTC 2019
Record UNII
FMG601PUW3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PF-04634817 SUCCINATE
Common Name English
Code System Code Type Description
PUBCHEM
121596583
Created by admin on Tue Oct 22 13:15:35 UTC 2019 , Edited by admin on Tue Oct 22 13:15:35 UTC 2019
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE