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

General Information of Drug (ID: DMO2PY8)

Drug Name

ETP-46321 Drug Info

Synonyms

1252594-99-2; CHEMBL2087474; 5-(2-((4-(methylsulfonyl)piperazin-1-yl)methyl)-8-morpholinoimidazo[1,2-a]pyrazin-6-yl)pyrimidin-2-amine; 5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-ylimidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine; SCHEMBL10100315; BCP19935; ETP46321; EX-A1284; BDBM50420714; ZINC68247289; CS-3350; ETP 46321;ETP46321; HY-12340; 5-[2-[(4-methylsulfonylpiperazin-1-yl)methyl]-8-morpholin-4-yl-imidazo[1,2-a]pyrazin-6-yl]pyrimidin-2-amine

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Investigative	[1]

Cross-matching ID

PubChem CID: 46927938
TTD Drug ID: DMO2PY8

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting PI3-kinase delta (PIK3CD)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[2]
Idelalisib	DM602WT	Chronic lymphocytic leukaemia	2A82.0	Approved	[3]
Umbralisib	DMYRBO1	Follicular lymphoma	2A80	Approved	[4]
IPI-145	DMWA24P	Follicular lymphoma	2A80	Approved	[5]
Leniolisib	DMWAD93	Stomach cancer	2B72	Approved	[6]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[7]
INCB50465	DMZJP2T	Diffuse large B-cell lymphoma	2A81	Phase 2	[8]
ME-401	DMK0UOY	Follicular lymphoma	2A80	Phase 2	[8]
RP6530	DMYILGK	Chronic lymphocytic leukaemia	2A82.0	Phase 2	[8]
Parsaclisib	DMYBIFS	Follicular lymphoma	2A80	Phase 2	[9]
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Drug(s) Targeting PI3-kinase alpha (PIK3CA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[2]
Alpelisib	DMEXMYK	Breast cancer	2C60-2C65	Approved	[10]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[7]
GDC-0032	DMT4QHD	Breast cancer	2C60-2C65	Phase 3	[11]
LY3023414	DMD9KYF	Prostate cancer	2C82.0	Phase 2	[12]
PA-799	DMLSYJQ	Colorectal cancer	2B91.Z	Phase 1/2	[13]
MLN1117	DMCVBQD	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[14]
PWT-33597	DMJY15D	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
BLY719	DMYHNV3	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
HHCYH33	DMRQ4L6	Breast cancer	2C60-2C65	Phase 1	[17]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase alpha (PIK3CA)	TTEUNMR	PK3CA_HUMAN	Inhibitor	[1]
PI3-kinase delta (PIK3CD)	TTGBPJE	PK3CD_HUMAN	Inhibitor	[1]

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References

1	ETP-46321, a dual p110alpha/ class IA phosphoinositide 3-kinase inhibitor modulates T lymphocyte activation and collagen-induced arthritis. Biochem Pharmacol. 2016 Apr 15;106:56-69.
2	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
3	2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
5	PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
6	Effective "activated PI3K syndrome"-targeted therapy with the PI3K inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316.
7	Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
8	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9	Parsaclisib, a potent and highly selective PI3K inhibitor, in patients with relapsed or refractory B-cell malignancies. Blood. 2019 Apr 18;133(16):1742-1752.
10	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
11	Company report (BioOncology)
12	Company report (Lilly)
13	The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
14	National Cancer Institute Drug Dictionary (drug id 714372).
15	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
16	In vitro anticancer activity of PI3K alpha selective inhibitor BYL719 in head and neck cancer. Anticancer Res. 2015 Jan;35(1):175-82.
17	Adaptive resistance to PI3Kalpha-selective inhibitor CYH33 is mediated by genomic and transcriptomic alterations in ESCC cells. Cell Death Dis. 2021 Jan 14;12(1):85.