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    GENE:

    UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)

    i
    Other names: UGT1A8, UDP Glucuronosyltransferase Family 1 Member A8, UGT1H, UDP Glycosyltransferase 1 Family, Polypeptide A8, UDP-Glucuronosyltransferase 1A8, UDP-Glucuronosyltransferase 1-8, UDP-Glucuronosyltransferase 1-H, UDPGT 1-8, UGT1-08, UGT-1H, UGT1.8, GNT1, UGT1, UDP Glucuronosyltransferase 1 Family, Polypeptide A8, UDP-Glucuronosyltransferase 1 Family Polypeptide A8s, Bilirubin-Specific UDPGT Isozyme 1, UDP-Glucuronosyltransferase 1-1, UDP-Glucuronosyltransferase 1-A, UDP-Glucuronosyltransferase 1A1, UDPGT 1-1, UGT1-01, UGT1A8S, HUG-BR1, UGT-1A, UGT1.1, UGT1A1, UGT1*8, UDPGT, UGT1A
    Associations

    News

    Trials
    3ms
    Characterization of In Vitro metabolic profiles of crepidatin in human liver microsomes and hepatocytes using HPLC-MS/MS and HPLC-Q-Orbitrap-HRMS. (PubMed, J Pharm Biomed Anal)
    Crepidatin was primarily metabolized by CYP3A4, 2C8, 2C19, UGT1A1, UGT1A8, and UGT1A9. This study describes the first integrated HPLC-MS/MS and HPLC-Q-Orbitrap-HRMS method for its in vitro metabolic profiling, and the results facilitate prediction of in vivo pharmacokinetics.
    Preclinical • Journal
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • UGT1A9 (UDP Glucuronosyltransferase Family 1 Member A9) • UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)
    almost2years
    Inhibition of Human UDP-Glucuronosyltransferase Enzyme by Entrectinib: Implications for Drug-Drug Interactions. (PubMed, Chem Biol Interact)
    Furthermore, the results from quantitative prediction research suggested that the combination of entrectinib at 600 mg/day with substrates primarily metabolized by hepatic UGT2B15 or intestinal UGT1A7 and UGT1A8 might cause clinical DDIs. Thus, special attention should be paid to avoid adverse reactions induced by DDIs when co-administration of entrectinib and drugs metabolized by UGTs.
    Journal
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    UGT1A7 (UDP Glucuronosyltransferase Family 1 Member A7) • UGT2B15 (UDP Glucuronosyltransferase Family 2 Member B15) • UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)
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    Rozlytrek (entrectinib)
    almost2years
    Activation of Cryptic Donor Splice Sites Within the UGT1A First-Exon Region Generates Variant Transcripts That Encode UGT1A Proteins With Truncated Aglycone-binding Domains. (PubMed, Drug Metab Dispos)
    The present study reports a series of novel UGT1A variants resulting from use of cryptic donor splice sites in both normal and cancerous tissues, several of which are predicted to encode variant UGT1A proteins with truncated aglycone-binding domains. Of these, 1A8_n2 shows exceptionally high abundance in colorectal tissues, highlighting its potential role in the first-pass metabolism in gut through the glucuronidation pathway.
    Journal
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    UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)
    over2years
    Identification of a Discrete Diglucuronide of GDC-0810 in Human Plasma after Oral Administration. (PubMed, Drug Metab Dispos)
    M2 could be the first discrete diglucuronide that was formed from both acyl- and N-glucuronidation on a molecule identified in human plasma. Significance Statement A discrete diglucuronidation metabolite of GDC-0810, a breast cancer drug candidate, was characterized as a unique circulating metabolite in humans that was not observed in rats or little formed human in vitro system.
    Journal
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    UGT1A4 (UDP Glucuronosyltransferase Family 1 Member A4) • UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)
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    brilanestrant (GDC-0810)
    over2years
    Drug-drug interaction potentials of tucatinib inhibition of human UDP-glucuronosyltransferases. (PubMed, Chem Biol Interact)
    The quantitative prediction of DDIs risk indicated that the co-administration of tucatinib with drugs mainly metabolized by hepatic or intestinal UGTs (UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B15 and UGT2B17) might result in potential DDIs risk through inhibition of glucuronidation. More attention should be paid to the influence of tucatinib on UGTs in liver and intestine to avoid unnecessary clinical DDIs risk.
    Journal
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    HER-2 (Human epidermal growth factor receptor 2) • UGT1A9 (UDP Glucuronosyltransferase Family 1 Member A9) • UGT1A6 (UDP Glucuronosyltransferase Family 1 Member A6) • UGT1A7 (UDP Glucuronosyltransferase Family 1 Member A7) • UGT2B15 (UDP Glucuronosyltransferase Family 2 Member B15) • UGT2B17 (UDP Glucuronosyltransferase Family 2 Member B17) • UGT1A10 (UDP Glucuronosyltransferase Family 1 Member A10) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3) • UGT1A8 (UDP Glucuronosyltransferase Family 1 Member A8)
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    HER-2 positive • UGT1A1*1*1
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    Tukysa (tucatinib)