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

General Information of Drug (ID: DM602WT)

Drug Name

Idelalisib Drug Info

Synonyms

Idelalisib; 870281-82-6; CAL-101; Zydelig; GS-1101; CAL101; CAL 101; (S)-2-(1-((9H-Purin-6-yl)amino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one; UNII-YG57I8T5M0; CAL-101 (Idelalisib, GS-1101); YG57I8T5M0; CHEMBL2216870; CHEBI:82701; 5-Fluoro-3-phenyl-2-((S)-1-(9H-purin-6-ylamino)-propyl)-3H-quinazolin-4-one; AK145603; Idelalisib; CAL-101; (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one; 1146702-54-6; 5-FLUORO-3-PHENYL-2-[(1S)-1-(9H-PURIN-6-YLAMINO)PROPYL]-4(3H)-QUINAZOLINONE

Indication

Disease Entry	ICD 11	Status	REF
Chronic lymphocytic leukaemia	2A82.0	Approved	[1]
Small lymphocytic lymphoma	2A82.0	Approved	[2]
Follicular lymphoma	2A80	Investigative	[2]

Cross-matching ID

PubChem CID: 11625818
ChEBI ID: CHEBI:82701
CAS Number: CAS 870281-82-6
TTD Drug ID: DM602WT
VARIDT Drug ID: DR00219
INTEDE Drug ID: DR0854
ACDINA Drug ID: D00322

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
PI3-kinase delta (PIK3CD)	TTGBPJE	PK3CD_HUMAN	Inhibitor	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[5]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
PI3-kinase delta (PIK3CD)	DTT	PIK3CD	5.711	5.814	6.011	6.508
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Chronic lymphocytic leukaemia

ICD Disease Classification

2A82.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
PI3-kinase delta (PIK3CD)	DTT	PIK3CD	4.31E-16	-0.37	-0.91
Breast cancer resistance protein (ABCG2)	DTP	BCRP	1.20E-13	-1.20E+00	-1.06E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	7.29E-03	-3.47E-02	-1.80E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6741).
2	Idelalisib FDA Label
3	2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
4	DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB09054)
5	FDA label of Idelalisib. The 2020 official website of the U.S. Food and Drug Administration.