CBR1 rs9024 genotype status impacts the bioactivation of loxoprofen in human liver.
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Quinones-Lombrana A, Li N, Del Solar V, Atilla-Gokcumen GE, Blanco JG
CBR1 rs9024 genotype status impacts the bioactivation of loxoprofen in human liver.
Biopharm Drug Dispos. 2018 Jun;39(6):315-318. doi: 10.1002/bdd.2135.
- PubMed ID
- 29851133 [ View in PubMed]
- Abstract
Loxoprofen is an anti-inflammatory drug that requires bioactivation into the trans-OH metabolite to exert pharmacological activity. Evidence suggests that carbonyl reductase 1 (CBR1) is important during the bioactivation of loxoprofen. This study examined the impact of the functional single nucleotide polymorphism CBR1 rs9024 on the bioactivation of loxoprofen in a collection of human liver samples. The synthesis ratios of trans-OH loxoprofen/cis-OH loxoprofen were 33% higher in liver cytosols from donors homozygous for the CBR1 rs9024 G allele in comparison with the ratios in samples from donors with heterozygous GA genotypes. Complementary studies examined the impact of CBR1 rs9024 on the bioactivation of loxoprofen in lymphoblastoid cell lines. CBR1 rs9024 genotype status impacts the synthesis of the bioactive trans-OH metabolite of loxoprofen in human liver.
DrugBank Data that Cites this Article
- Drugs
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Loxoprofen Carbonyl reductase [NADPH] 1 Protein Humans NoSubstrateDetails