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]
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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
TTD ID: D39UDP

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 Interaction Atlas (MIA)

MIA Detail

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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

Molecular Expression Atlas (MEA)

MEA Detail

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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.