Drug Information

Drug (ID: DG02020) and It's Reported Resistant Information

Name	PF-04620110
Synonyms	PF-04620110; 1109276-89-2; CHEMBL1835919; 2-(trans-4-(4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)acetic acid; PF-4620110; trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexaneacetic acid; 2-(trans-4-(4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f]-[1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)acetic acid; UNII-CQ4M18RLJW; CQ4M18RLJW; SCHEMBL1424362; SCHEMBL1425038; GTPL7829; SCHEMBL1424359; SCHEMBL13954265; DTXSID90677361; GEVVQZHMFVFGLN-HDJSIYSDSA-N Click to Show/Hide
Indication	In total 1 Indication(s) Type-2 diabetes [ICD-11: 5A11] Terminated
Structure
Target	Diacylglycerol acyltransferase 1 (DGAT1)	DGAT1_HUMAN
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Formula	119
IsoSMILES	GEVVQZHMFVFGLN-UHFFFAOYSA-N
InChI	C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)N3CCOC4=NC=NC(=C4C3=O)N
InChIKey	2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid
PubChem CID	46926360
TTD Drug ID	D0M0NT

Type(s) of Resistant Mechanism of This Drug

MRAP: Metabolic Reprogramming via Altered Pathways

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

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Breast invasive carcinoma [ICD-11: 2C61]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Metabolic Reprogramming via Altered Pathways (MRAP)		Click to Show/Hide
Key Molecule: Neurofibromin 1 (NF1)			[1]
Metabolic Type	Lipid metabolism
Sensitive Disease	ER+ breast adenocarcinoma [ICD-11: 2C61.1]		Disease Info
Molecule Alteration	Mutation	.	Molecule Info
Experimental Note	Revealed Based on the Cell Line Data
In Vivo Model	Rat, with ER + MCF7 cell lines		Rats
Experiment for Molecule Alteration	LC-MS
Experiment for Drug Resistance	Incucyte proliferation assay
Mechanism Description	Lastly,NF1deficiency alters the synergy between metabolic inhibitors and traditional targeted inhibitors. This includes increased synergy with inhibitors targeting glycolysis, glutamine metabolism, mitochondrial fatty acid transport, and TG synthesis.

References

Ref 1	NF1 deficiency drives metabolic reprogramming in ER+ breast cancer. Mol Metab. 2024 Feb;80:101876.