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Metabolism class new report! To ensure the effect of drugs and avoid adverse reactions depends on it

Issuing time:2020-10-24 10:51

Hello everyone, my name is CYP3A5 and I am very happy to join the big family of metabolism classes.



I am one of the important drug-metabolizing enzymes in the human cytochrome CYP450 family. I participate in the metabolism of tacrolimus, midazolam, dapsone, cortisone, nifedi and other drugs.


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Chromosome 7


The gene encoding me is located on human chromosome 7q22.1 and has 14 exons


There is a 6986A>G mutation (rs776746, CYP3A5*3) at position 22893 in the third intron of the gene encoding my gene. This SNP can cause abnormal splicing of CYP3A5 mRNA, causing the stop codon to cut the CYP3A5 protein prematurely, thereby causing it to be lost Enzyme activity, therefore, the expression and activity of CYP3A5 protein in liver and intestine of CYP3A5*3 homozygous individuals are significantly decreased.


The distribution frequency of different CYP3A5 genotypes in different ethnic groups and different regions is very different. In the study, Kyoung-Ah Kim et al. found that the genotype frequencies of CYP3A5*3/*3, CYP3A5*1/*3, and CYP3A5*1/*1 were 60%, 35%, and 5%, respectively.


Among the many antihypertensive drugs, I have a soft spot for calcium antagonist (CCB) drugs.


Researchers have conducted a thorough study on me and found that after taking 5mg amlodipine in individuals of different genotypes, the plasma amlodipine concentration in carriers of CYP3A5*3/*3 is significantly lower than that of CYP3A5*1/* 1 carrier



Of course, this is only a small example of my many metabolic drugs, and my business scope is very large!


Because I participate in the metabolism of many commonly used drugs in the body, it affects many pharmacokinetic characteristics, such as drug half-life, liver first pass effect, drug interaction, clearance rate and bioavailability.


It can be said that my existence is of great significance for ensuring the safe and effective use of drugs and avoiding adverse drug reactions.


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Having said so much, everyone must have a certain understanding of me in the future, if you see me somewhere in the future, please remember to say hello to me!


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