PF-04634817

Investigational

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 Search

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

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30450458 | https://www.ncbi.nlm.nih.gov/pubmed/29847672 | https://adisinsight.springer.com/drugs/800032291

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

Title	Date	PubMed
A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema.	2018 May 1	29847672
Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy.	2018 Nov	30450458

Sample Use Guides

In Vivo Use Guide

200 mg once daily

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 11:35:41 GMT 2023` Edited by `admin` on `Sat Dec 16 11:35:41 GMT 2023`
Record UNII	51M3FB9B9E
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

PF-04634817

Common Name

English

1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-D-ERYTHRO-PENTITOL

Systematic Name

English

D-ERYTHRO-PENTITOL, 1,5-ANHYDRO-2,3-DIDEOXY-4-O-METHYL-3-(((1R,3S)-3-(1-METHYLETHYL)-3-(((1S,4S)-5-(6-(TRIFLUOROMETHYL)-4-PYRIMIDINYL)-2,5-DIAZABICYCLO(2.2.1)HEPT-2-YL)CARBONYL)CYCLOPENTYL)AMINO)-

Systematic Name

English

Code System Code Type Description

SMS_ID

300000041328