Details of the Drug Combination

General Information of Drug Combination (ID: DCPQHMH)

Drug Combination Name
(-)-englerin A Lenvatinib
Indication
Disease Entry Status REF
Ewing sarcoma Investigative [1]
Component Drugs (-)-englerin A   DMPQBWY Lenvatinib   DMB1IU4
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL is unavailable 3D MOL
High-throughput Screening Result Testing Cell Line: TC-71
Zero Interaction Potency (ZIP) Score: 13.739
Bliss Independence Score: 14.202
Loewe Additivity Score: 4.154
LHighest Single Agent (HSA) Score: 5.27

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of (-)-englerin A
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [2]
(-)-englerin A Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Short transient receptor potential channel 5 (TRPC5) TT32NQ1 TRPC5_HUMAN Agonist [8]
Short transient receptor potential channel 4 (TRPC4) TTX0H5W TRPC4_HUMAN Agonist [8]
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Indication(s) of Lenvatinib
Disease Entry ICD 11 Status REF
Thyroid cancer 2D10 Approved [3]
Thyroid gland follicular carcinoma N.A. Approved [4]
Thyroid gland papillary carcinoma N.A. Approved [4]
Hepatocellular carcinoma 2C12.02 Phase 3 [5]
Renal cell carcinoma 2C90 Phase 3 [6]
Melanoma 2C30 Phase 2 [5]
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [6]
Ovarian cancer 2C73 Phase 1 [7]
Non-small-cell lung cancer 2C25.Y Application submitted [6]
Lenvatinib Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [7]
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Lenvatinib Interacts with 1 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [9]
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References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 Enantioselective synthesis of (-)-englerins A and B. Angew Chem Int Ed Engl. 2010 May 3;49(20):3517-9.
3 FDA Approved Drug Products from FDA Official Website. 2018. Application Number: (ANDA) 208627.
4 Lenvatinib FDA Label
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
8 (-)-Englerin is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91.
9 Influence of CYP3A4/5 and ABC transporter polymorphisms on lenvatinib plasma trough concentrations in Japanese patients with thyroid cancer. Sci Rep. 2019 Apr 1;9(1):5404.