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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제50권 제1호
- 발행연도
- 2020.1
- 수록면
- 71 - 79 (9page)
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초록· 키워드
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Nabumetone is a prodrug, used as an anti-inflammation agent and having the active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA). The role of the polymorphic enzyme responsible for the 6-O-demethylation of 6-MNA to 6-hydroxy- 2-naphtylacetic acid (6-HNA) was studied using recombinant cytochrome CYP2C9 microsomes (CYP2C9.1, CYP2C9.2 and CYP2C9.3) and human liver microsomes of known genotypes of CYP2C9. Utilizing recombinant CYP2C9.1, Vmax and Vmax/Km values of 6.3 ± 3.3 pmol/min/pmol P450 and 12.4 ± 4.7 nL/min/pmol P450, respectively, were obtained for the 6-MNA metabolism, and were almost similar to those in CYP2C9.2. In contrast, the Vmax/Km value in recombinant CYP2C9.3 was about one-third that of CYP2C9.1. In kinetic studies using liver microsomes of humans genotyped for the CYP2C9 genes, a sample genotyped as *3/*3 revealed about 4- to sixfold lower intrinsic clearance for 6-HNA formation than did samples genotyped as *1/*1. No appreciable differences were observed in kinetic parameters for 6-HNA formation in *1/*2 and *1/*3, while *2/*2 microsomes was comparable to wild type microsomes. In addition, S-warfarin 7-hydroxylation by recombinant CYP2C9.1 and CYP2C9.3 was inhibited by 6-MNA in a mixed manner. The apparent Ki value of 6-MNA on S-warfarin 7-hydroxylation by CYP2C9.3 was higher than that by CYP2C9.1. These results may provide valuable information for optimizing the anticoagulant activity of warfarin when nabumetone is co-administrated to patients.
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참고문헌 (31)
참고문헌 신청
Crespi CL / 1997 / The R144C change in the CYP2C9*2allele alters interaction of the cytochrome P450 with NADPH : cytochrome P450 oxidoreductase / Pharmacogenetics 7:203~210
Davies NM / 1997 / Clinical Pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition? / Clin Pharmacokinet 33:403~416
Dennis VC / 2000 / Potentiation of oral anticoagulation and hemarthrosis associated with nabumetone / Pharmacotherapy 20:234~239
Hanatani T / 2003 / No major difference in inhibitory susceptibility between CYP2C9.1 and CYP2C9.3 / Eur J Clin Pharmacol 59:233~235
Iida I / 2004 / Catalytic roles of CYP2C9 and its variants(CYP2C9*2 and CYP2C9*3)in lornoxicam 5′-hydroxylation / Drug Metab Dispos 32:7~9
Davies NM / 1997 / Clinical Pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition? / Clin Pharmacokinet 33:403~416
Dennis VC / 2000 / Potentiation of oral anticoagulation and hemarthrosis associated with nabumetone / Pharmacotherapy 20:234~239
Hanatani T / 2003 / No major difference in inhibitory susceptibility between CYP2C9.1 and CYP2C9.3 / Eur J Clin Pharmacol 59:233~235
Iida I / 2004 / Catalytic roles of CYP2C9 and its variants(CYP2C9*2 and CYP2C9*3)in lornoxicam 5′-hydroxylation / Drug Metab Dispos 32:7~9
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