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Details

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

SHOW SMILES / InChI
Structure of PF-04634817

SMILES

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=MCRWZBYTLVCCJJ-DKALBXGISA-N
InChI=1S/C25H36F3N5O3/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/h9,14-20,31H,4-8,10-13H2,1-3H3/t16-,17+,18+,19+,20-,24+/m1/s1

HIDE SMILES / InChI

Molecular Formula C25H36F3N5O3
Molecular Weight 511.5802
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 6 / 6
E/Z Centers 0
Optical Activity UNSPECIFIED

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

Sample Use Guides

In Vivo Use Guide
200 mg once daily
Route of Administration: Oral
Substance Class Chemical
Record UNII
51M3FB9B9E
Record Status Validated (UNII)
Record Version