Details of the Drug Combination

General Information of Drug Combination (ID: DC6L3OW)

Drug Combination Name
Karenitecin Valproic Acid
Indication
Disease Entry Status REF
Malignant Melanoma Phase 1 [1]
Component Drugs Karenitecin   DMCRGY4 Valproic Acid   DMS49KH
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Karenitecin
Disease Entry ICD 11 Status REF
Lung cancer 2C25.0 Phase 3 [2]
Ovarian cancer 2C73 Phase 3 [2]
Karenitecin Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
DNA topoisomerase I (TOP1) TTGTQHC TOP1_HUMAN Inhibitor [5]
DNA topoisomerase (TOP) TT2GPK3 NOUNIPROTAC Inhibitor [6]
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Karenitecin Interacts with 2 DTP Molecule(s)
DTP Name DTP ID UniProt ID Mode of Action REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [7]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [8]
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Karenitecin Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [9]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Metabolism [9]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Metabolism [9]
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Indication(s) of Valproic Acid
Disease Entry ICD 11 Status REF
Absence epilepsy N.A. Approved [3]
Epilepsy 8A60-8A68 Approved [3]
Glioblastoma 2A00 Approved [3]
Coronavirus Disease 2019 (COVID-19) 1D6Y Investigative [4]
Neuroblastoma 2D11.2 Investigative [3]

References

1 ClinicalTrials.gov (NCT00358319) Phase I/II Trial of Valproic Acid and Karenitecin for Melanoma
2 ClinicalTrials.gov (NCT00477282) Karenitecin Versus Topotecan in Patients With Advanced Epithelial Ovarian Cancer. U.S. National Institutes of Health.
3 Valproic Acid FDA Label
4 Immunopharmacological management of COVID-19: Potential therapeutic role of valproic acid. Med Hypotheses. 2020 May 27;143:109891.
5 Characterization of protein kinase chk1 essential for the cell cycle checkpoint after exposure of human head and neck carcinoma A253 cells to a novel topoisomerase I inhibitor BNP1350. Mol Pharmacol.2000 Mar;57(3):453-9.
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 Pharmacogenomic importance of ABCG2. Pharmacogenomics. 2008 Aug;9(8):1005-9.
8 Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev. 2011 Mar;63(1):157-81.
9 Evaluation of in vitro drug interactions with karenitecin, a novel, highly lipophilic camptothecin derivative in phase II clinical development. J Clin Pharmacol. 2003 Sep;43(9):1008-14.