Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM930LE)

• Drug Name: GSK4172239 Drug Info

Indication

Disease Entry	ICD 11	Status	REF
Sickle-cell disorder	3A51	Phase 1	[1]

• Cross-matching ID: TTD Drug ID: DM930LE

Molecule-Related Drug Atlas

Drug(s) Targeting DNA [cytosine-5]-methyltransferase 1 (DNMT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CC-486	DMTNQB0	Acute myeloid leukaemia	2A60	Phase 3	[3]
S-110	DMXY34J	Acute myeloid leukaemia	2A60	Phase 3	[4]
SGI110	DM1NQDW	Acute myeloid leukaemia	2A60	Phase 3	[5]
Guadecitabine	DM9Y3EG	Myelodysplastic syndrome	2A37	Phase 3	[6]
Palifosfamide	DMMIYZ7	Soft tissue sarcoma	2B57	Phase 2	[7]
RX-3117	DME8ARP	Bladder cancer	2C94	Phase 2	[8]
Antroquinonol	DMRGQVZ	Non-small-cell lung cancer	2C25.Y	Phase 2	[9]
PMID27376512-Compound-MTC-424	DMGNRZU	N. A.	N. A.	Patented	[10]
PMID27376512-Compound-MTC-427	DMWXEZD	N. A.	N. A.	Patented	[10]
PMID27376512-Compound-MTC-422	DM1MVQD	N. A.	N. A.	Patented	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
DNA [cytosine-5]-methyltransferase 1 (DNMT1)	TT6S2FE	DNMT1_HUMAN	Inhibitor	[2]

References

• [1] ClinicalTrials.gov (NCT05660265) A Randomized, Placebo-controlled, Double-Blind (Sponsor Unblind), Parallel Group, Single Dose, Dose Escalation Phase I Study in Sickle Cell Disease Participants, to Evaluate the Safety, Tolerability, and Pharmacokinetics of GSK4172239D. U.S.National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of GlaxoSmithKline
• [3] Efficacy and safety of extended dosing schedules of CC-486 (oral azacitidine) in patients with lower-risk myelodysplastic syndromes. Leukemia. 2016 Apr;30(4):889-96.
• [4] S110, a 5-Aza-2'-deoxycytidine-containing dinucleotide, is an effective DNA methylation inhibitor in vivo and can reduce tumor growth. Mol Cancer Ther. 2010 May;9(5):1443-50.
• [5] Immunomodulatory action of the DNA methyltransferase inhibitor SGI-110 in epithelial ovarian cancer cells and xenografts. Epigenetics. 2015;10(3):237-46.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Anticancer activity of stabilized palifosfamide in vivo: schedule effects, oral bioavailability, and enhanced activity with docetaxel and doxorubicin. Anticancer Drugs. 2012 Feb;23(2):173-84.
• [8] Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360). Invest New Drugs. 2013 Dec;31(6):1444-57.
• [9] Antroquinonol D, isolated from Antrodia camphorata, with DNA demethylation and anticancer potential. J Agric Food Chem. 2014 Jun 18;62(24):5625-35.
• [10] DNA methyltransferase inhibitors: an updated patent review (2012-2015).Expert Opin Ther Pat. 2016 Sep;26(9):1017-30.