Details of the Drug Combination

General Information of Drug Combination (ID: DCFV208)

Drug Combination Name
Idelalisib GS-9973
Indication
Disease Entry Status REF
Chronic Lymphocytic Leukemia Phase 1 [1]
Component Drugs Idelalisib   DM602WT GS-9973   DMKWCTR
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL is unavailable 3D MOL is unavailable

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Idelalisib
Disease Entry ICD 11 Status REF
Chronic lymphocytic leukaemia 2A82.0 Approved [2]
Small lymphocytic lymphoma 2A82.0 Approved [3]
Follicular lymphoma 2A80 Investigative [3]
Idelalisib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
PI3-kinase delta (PIK3CD) TTGBPJE PK3CD_HUMAN Inhibitor [6]
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Idelalisib Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [7]
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Idelalisib Interacts with 1 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [8]
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Idelalisib Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Tumor necrosis factor receptor superfamily member 6 (FAS) OTP9XG86 TNR6_HUMAN Affects Response To Substance [9]
Phosphoinositide-3-kinase-interacting protein 1 (PIK3IP1) OTWE5G4T P3IP1_HUMAN Increases Expression [10]
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Indication(s) of GS-9973
Disease Entry ICD 11 Status REF
Acute myeloid leukaemia 2A60 Phase 2 [4]
B-cell lymphoma 2A86 Phase 2 [5]
Haematological malignancy 2B33.Y Phase 2 [4]
GS-9973 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Tyrosine-protein kinase SYK (SYK) TTOU65C KSYK_HUMAN Modulator [11]
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References

1 ClinicalTrials.gov (NCT01796470) Entospletinib in Combination With Idelalisib in Adults With Relapsed or Refractory Hematologic Malignancies
2 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).
3 Idelalisib FDA Label
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 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: 7889).
6 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
7 DrugBank 5.0: a major update to the DrugBank database for 2018. Nucleic Acids Res. 2018 Jan 4;46(D1):D1074-D1082. (ID: DB09054)
8 FDA label of Idelalisib. The 2020 official website of the U.S. Food and Drug Administration.
9 PI3K/AKT inhibitors aggravate death receptor-mediated hepatocyte apoptosis and liver injury. Toxicol Appl Pharmacol. 2019 Oct 15;381:114729. doi: 10.1016/j.taap.2019.114729. Epub 2019 Aug 22.
10 Induction of prolonged early G1 arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3K inhibition through PIK3IP1. Cell Cycle. 2013 Jun 15;12(12):1892-900. doi: 10.4161/cc.24928. Epub 2013 May 15.
11 An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2015 Apr 9;125(15):2336-43.