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UGT1A1 enzyme

The enzyme UGT1A1 is part of the group of uridine diphosphate-glucuronosyltransferases (UGTs) and is involved in the conversion of fat-soluble substances, such as bilirubin, hormones and drugs, into water-soluble substances that can be excreted from the body. The toxic waste product bilirubin is converted in the liver only by the enzyme UGT1A1.
Drugs that can be metabolised by the enzyme UGT1A1 include:

  • Cytostatics, such as irinotecan and etoposide
  • Other drugs, such as atazanavir (antiretroviral) and raloxifene (oestrogen receptor modulator)

Atazanavir and the enzyme UGT1A1

Atazanavir inhibits the enzyme UGT1A1. UGT1A1 is the only enzyme in the body that can make bilirubin water-soluble so that it can be excreted in bile by the liver. Bilirubin is a waste product that is released when red blood cells are broken down and is toxic to the body. It causes jaundice (hyperbilirubinaemia) and, depending on your genetic predisposition to reduced UGT1A1 enzyme activity, you may be at an increased risk of developing this condition. People who have two UGT1A1 decreased-function alleles are most at risk of developing jaundice. The UGT1A1 enzyme is not involved in breaking down atazanavir.

Information about your genetic predisposition may therefore provide grounds for extra vigilance in relation to a treatment with atazanavir.

Read more about Atazanavir »

Atazanavir and the enzyme UGT1A1

Atazanavir inhibits the enzyme UGT1A1. UGT1A1 is the only enzyme in the body that can make bilirubin water-soluble so that it can be excreted in bile by the liver. Bilirubin is a waste product that is released when red blood cells are broken down and is toxic to the body. It causes jaundice (hyperbilirubinaemia) and, depending on your genetic predisposition to reduced UGT1A1 enzyme activity, you may be at an increased risk of developing this condition. People who have two UGT1A1 decreased-function alleles are most at risk of developing jaundice. The UGT1A1 enzyme is not involved in breaking down atazanavir.

Information about your genetic predisposition may therefore provide grounds for extra vigilance in relation to a treatment with atazanavir.

Read more about Atazanavir »

Irinotecan and the enzyme UGT1A1

Irinotecan is processed to a large extent by the enzyme UGT1A1. The activity of this enzyme can vary considerably depending on your genetic predisposition, which means the efficacy of irinotecan can also differ from person to person.

Information about your genetic predisposition may therefore provide grounds for extra vigilance in relation to a treatment with irinotecan.

Read more about Irinotecan »

Irinotecan and the enzyme UGT1A1

Irinotecan is processed to a large extent by the enzyme UGT1A1. The activity of this enzyme can vary considerably depending on your genetic predisposition, which means the efficacy of irinotecan can also differ from person to person.

Information about your genetic predisposition may therefore provide grounds for extra vigilance in relation to a treatment with irinotecan.

Read more about Irinotecan »

Genetic predisposition
The activity of the enzyme UGT1A1 varies from one individual to another. As a result, the efficacy of a drug can differ from person to person, as can the potential side effects. This variation can be partly explained by genetic variations in the UGT1A1 gene. When a genotype is determined these variations in the UGT1A1 gene are indicated by two so-called alleles. Each allele has a name consisting of an asterisk and a number. An example of a possible UGT1A1 genotype is UGT1A1*1*28.
At iGene we determine the following variants (alleles) of the UGT1A1 gene: UGT1A1*6, UGT1A1*27, UGT1A1*28 (via UGT1A1*80) and other (classified as UGT1A1*1).

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