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    GENE:

    UGT1A4 (UDP Glucuronosyltransferase Family 1 Member A4)

    i
    Other names: UGT1A4, UDP Glucuronosyltransferase Family 1 Member A4, HUG-BR2, UGT1D, UDP Glycosyltransferase 1 Family, Polypeptide A4, Bilirubin-Specific UDPGT Isozyme 2, UDP-Glucuronosyltransferase 1A4, UDP-Glucuronosyltransferase 1-4, UDP-Glucuronosyltransferase 1-D, UDPGT 1-4, UGT1-04, UGT-1D, UGT1.4, GNT1, UGT1, UDP Glucuronosyltransferase 1 Family, Polypeptide A4, UDP-Glucuronosyltransferase 1 Family Polypeptide A4s, Bilirubin UDP-Glucuronosyltransferase Isozyme 2, Bilirubin-Specific UDPGT Isozyme 1, UDP-Glucuronosyltransferase 1-1, UDP-Glucuronosyltransferase 1-A, UDP-Glucuronosyltransferase 1A1, UDPGT 1-1, UGT1-01, UGT1A4S, HUG-BR1, UGT-1A, UGT1.1, UGT1A1, UGT1*4, UDPGT, UGT1A
    Associations

    News

    Trials
    3ms
    Association of SULT2A1 Locus With Abiraterone Clearance in the Alliance A031201: Randomized Phase III Study of Enzalutamide Compared With Enzalutamide Plus Abiraterone for Metastatic Castration-Resistant Prostate Cancer. (PubMed, Clin Transl Sci)
    Genetic variation in SULT2A1 may be useful to inform personalized dosing of abiraterone. ClinicalTrials.gov Identifier: NCT01949337.
    Clinical • P3 data • Journal
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    CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • CYP3A5 (Cytochrome P450 Family 3 Subfamily A Member 5) • SLCO2B1 (Solute Carrier Organic Anion Transporter Family Member 2B1) • UGT1A4 (UDP Glucuronosyltransferase Family 1 Member A4)
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    Xtandi (enzalutamide) • abiraterone acetate
    10ms
    Potent and highly selective inhibition of selpercatinib towards UDP-glucuronosyltransferase 1A4 (UGT1A4) isoform. (PubMed, Toxicol Appl Pharmacol)
    The quantitative prediction of DDIs risk indicated that the co-administration of selpercatinib with UGT1A4 substrate might trigger clinically significant DDIs. Additional caution should be taken to avoid unexpected DDIs when selpercatinib and other UGT1A4 substrates are combined.
    Journal
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    RET (Ret Proto-Oncogene) • UGT1A4 (UDP Glucuronosyltransferase Family 1 Member A4)
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    RET fusion • RET positive
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    Retevmo (selpercatinib)
    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)