CBR1 rs9024 genotype status impacts the bioactivation of loxoprofen in human liver.

Article Details

Citation

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
DrugEnzymeKindOrganismPharmacological ActionActions
LoxoprofenCarbonyl reductase [NADPH] 1ProteinHumans
No
Substrate
Details