General Information of DME (ID: DMEN063)
DME Name Aldo-keto reductases (AKR), .
Gene Name AKR
      Click to Show/Hide the Molecular/Functional Data (Sequence/Structure/Pathway/Function) of This DME
Full List of Drug(s) Metabolized by This DME
      Drugs Approved by FDA Click to Show/Hide the Full List of Drugs:          1 Drugs
Brexanolone
Drug Info Approved Depression ICD11: 6A71 [1]
Full List of Metabolic Reactions (MR) Catalyzed by This DME
MR ID Reactant Product MR Type Source Drug REF
MR005754 Brexanolone Unclear Reduction - Reduction Brexanolone [1]
MR000999 Exemestane 17beta-dihydroexemestane Reduction - Reduction Exemestane [2], [3], [4]
MR011407 ITI-007 ICI200131 Reduction - Reduction ITI-007 [5]
MR001556 Linagliptin CD10604 Linagliptin CD1790 Reduction - Reduction Linagliptin [6]
MR010266 Lumateperone tosylate ICI200131 Reduction - Reduction lumateperone tosylate [7]
MR014073 Lumateperone tosylate ICI200131 Reduction - Reduction lumateperone tosylate [7]
MR002364 Telaprevir . Reduction - Reduction Telaprevir [8]
MR014203 TH-4000 TH-4000E Reduction - Reduction TH-4000 [9]
⏷ Show the Full List of 8 MR(s)
References
1 FDA Label of Brexanolone
2 In vitro metabolism of exemestane by hepatic cytochrome P450s: impact of nonsynonymous polymorphisms on formation of the active metabolite 17beta-dihydroexemestane. Pharmacol Res Perspect. 2017 Apr 27;5(3):e00314.
3 Inhibition of the aromatase enzyme by exemestane cysteine conjugates. Mol Pharmacol. 2022 Aug 11;102(5):216-22. doi: 10.1124/molpharm.122.000545.
4 Influence of Glutathione-S-Transferase A1*B Allele on the Metabolism of the Aromatase Inhibitor, Exemestane, in Human Liver Cytosols and in Patients Treated With Exemestane. J Pharmacol Exp Ther. 2022 Sep;382(3):327-334. doi: 10.1124/jpet.122.001232.
5 An evaluation of lumateperone tosylate for the treatment of schizophrenia
6 The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans Drug Metab Dispos. 2010 Apr;38(4):667-78. doi: 10.1124/dmd.109.031476.
7 Dopamine D(2) receptor occupancy of lumateperone (ITI-007): a Positron Emission Tomography Study in patients with schizophrenia
8 NCIVEK- telaprevir tablet, film coated Vertex Pharmaceuticals Incorporated
9 Targeting the hypoxic fraction of tumours using hypoxia-activated prodrugs

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