Metabolizer profile CYP3A5

Cytochrome CYP3A5 is an enzyme of the hepatic cytochrome P450 family, whose main function is the metabolism of xenobiotics. This CYP is responsible for the oxidative metabolism of multiple drugs and is involved in the metabolism of cholesterol, steroids and other lipids.

CYP P450 is a superfamily of enzymes involved in enzymatic oxidation of steroids, fatty acids, xenobiotics and other biosynthetic pathways. These enzymes convert xenobiotics into water-soluble derivatives to facilitate their excretion. CYP3A5 is mainly found in the liver and prostate, but can also be found in the intestine, bile duct or nasal mucosa.

CYP3A5 is involved in the metabolism of multiple drugs including tacrolimus, cyclosporine, sirolimus, midazolam, vincristine and some statins. The physiological function of this cytochrome is still unknown.

The activity of this cytochrome can vary markedly between individuals, influenced by the presence of inducers or inhibitors, diseases and by the presence of certain genetic polymorphisms, the latter being the main reason for the variability. CYP3A5 is a polymorphic gene with different alleles whose frequency varies between populations, being very frequent the presence of loss-of-function alleles that decrease its metabolizing capacity. The strongest evidence of the clinical impact of genetic variations relates to tacrolimus metabolism and has been shown to play a key role in the immunosuppressive treatment of transplant recipients.It is important to bear in mind that, independently of the genetic profile of the individual, the genetic profile of the patient should be determined in order to ensure correct therapeutic monitoring and dose adjustment.

It is important to bear in mind that, independently of the effects on activity that the different genotypes may have, there are multiple compounds that can act as inhibitors or inducers and that significantly affect their function. This is important, above all, in polytherapy because it can condition the therapeutic effect and the presence of side effects of drugs metabolized by CYP3A5.