Details of the Drug

General Information of Drug (ID: DM3CJ5N)

Drug Name
PF-07258669
Synonyms
PF-07258669; CHEMBL5183637; 2755890-53-8; SCHEMBL24853368; GTPL12158; GLXC-27032; (2R)-2-(5-fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(pyrimidin-2-yl)-3,4-dihydro-1H-spiro[1,8-naphthyridine-2,3'-pyrrolidin]-1'-yl]propan-1-one; EX-A6871; BDBM50598696; HY-148349; CS-0619625; (2R)-2-(5-Fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-pyrimidin-2-ylspiro[3,4-dihydro-1H-1,8-naphthyridine-2,3'-pyrrolidine]-1'-yl]propan-1-one
Indication
Disease Entry ICD 11 Status REF
Malnutrition 5B50-5B71 Phase 1 [1]
Drug Type
Small molecule
Structure
3D MOL 2D MOL
Chemical Identifiers
Formula
C25H27FN6O2
Canonical SMILES
CC1=C(C=C2CCC3(CCN(C3)C(=O)C(C)C4=CC(=NC=C4F)OC)NC2=N1)C5=NC=CC=N5
InChI
InChI=1S/C25H27FN6O2/c1-15(18-12-21(34-3)29-13-20(18)26)24(33)32-10-7-25(14-32)6-5-17-11-19(16(2)30-22(17)31-25)23-27-8-4-9-28-23/h4,8-9,11-13,15H,5-7,10,14H2,1-3H3,(H,30,31)/t15-,25+/m1/s1
InChIKey
PARGFYLSRQUWHR-BZQUYTCOSA-N
Cross-matching ID
PubChem CID
164889476
ChEBI ID
CHEMBL5183637
TTD ID
D39UDP
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Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Melanocortin receptor 4 (MC4R) TTD0CIQ MC4R_HUMAN Antagonist [2]
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Molecular Expression Atlas of This Drug

The Studied Disease Malnutrition
ICD Disease Classification 5B50-5B71
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Melanocortin receptor 4 (MC4R) DTT MC4R 5.64E-01 -0.04 -0.18
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References

1 ClinicalTrials.gov (NCT04628793) A PHASE 1, RANDOMIZED, DOUBLE-BLIND, SPONSOR-OPEN, PLACEBO-CONTROLLED, FIRST-IN-HUMAN STUDY TO EVALUATE THE SAFETY, TOLERABILITY, AND PHARMACOKINETICS OF SINGLE ASCENDING ORAL DOSES OF PF-07258669 ADMINISTERED TO HEALTHY ADULT PARTICIPANTS. U.S.National Institutes of Health.
2 Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss. J Med Chem. 2023 Mar 9;66(5):3195-3211.