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    GENE:

    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)

    i
    Other names: UGT1A1, UDP glucuronosyltransferase family 1 member A1, GNT1, UGT1, UDPGT, UGT1A, HUG-BR1, BILIQTL1, UDPGT 1-1
    10d
    TRIPP-FFX: FOLFIRINOX Versus OncoSil™ in Addition to FOLFIRINOX in Patients With Locally Advanced Pancreatic Adenocarcinoma (clinicaltrials.gov)
    P2, N=88, Active, not recruiting, OncoSil Medical Limited | Recruiting --> Active, not recruiting | Trial completion date: Sep 2025 --> Jul 2027 | Trial primary completion date: Jun 2025 --> Jan 2026
    Enrollment closed • Trial completion date • Trial primary completion date
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    5-fluorouracil • oxaliplatin • irinotecan • leucovorin calcium
    16d
    Icaritin enhances the antitumor efficacy of irinotecan by dual-targeting carboxylesterase 2 and p53 in vitro and in vivo. (PubMed, Biochem Pharmacol)
    Molecular docking simulations demonstrated that the interation energy between CES2 and icaritin was significantly higher than that with cisplatin (a reported CES2 activator), which might suggest that CES2 has a higher affinity for icaritin than cisplatin. These findings have important clinical significance for reducing chemotherapy drug resistance in cancer patients. Abbreviations: CES2, Carboxylesterase 2; CRC, Colorectal cancer; CPT-11, Irinotecan; CYP3A, Cytochrome P450 3A; NR, Nuclear receptor; P53, Tumor protein p53; PPAR-α, Peroxisome proliferator-activated receptor α; PXR, Pregnane X receptor; SN-38, 7-Ethyl-10-hydroxycamptothecin; UGT1A1, UDP-glucuronosyltransferase 1A1.
    Preclinical • Journal
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    cisplatin • irinotecan • icaritin (SNG-162)
    17d
    RP-6306 in Patients With Advanced Cancer (clinicaltrials.gov)
    P2, N=28, Completed, Canadian Cancer Trials Group | Active, not recruiting --> Completed
    Trial completion
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    HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • CCNE1 (Cyclin E1) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • PPP2R1A (Protein Phosphatase 2 Scaffold Subunit Aalpha)
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    TP53 mutation • KRAS mutation • HER-2 amplification • RAS mutation
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    Herceptin (trastuzumab) • gemcitabine • 5-fluorouracil • irinotecan • leucovorin calcium • lunresertib (RP-6306) • camonsertib (RP-3500)
    18d
    Vincristine and Temozolomide in Combination With PEN-866 for Adolescents and Young Adults With Relapsed or Refractory Solid Tumors (clinicaltrials.gov)
    P1/2, N=64, Suspended, National Cancer Institute (NCI) | Trial completion date: Dec 2026 --> Dec 2027 | Recruiting --> Suspended | Trial primary completion date: Feb 2026 --> Dec 2026
    Trial completion date • Trial suspension • Trial primary completion date
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    temozolomide • vincristine • locnartecan (PEN-866)
    27d
    Risk of neutropenia associated with Sacituzumab govitecan: a systematic review combined with the FAERS database and meta-analysis. (PubMed, Front Pharmacol)
    This AE exhibits significant cancer species specificity. Early intervention and management of neutropenia are therefore of considerable clinical importance.
    Retrospective data • Review • Journal
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    Trodelvy (sacituzumab govitecan-hziy)
    27d
    Impact of UGT1A1*28 Allele on the Safety and Effectiveness of Sacituzumab Govitecan in Metastatic Triple-Negative Breast Cancer: Real-World Evidence. (PubMed, J Clin Med)
    Improving treatment tolerability through dose reductions may enhance SG effectiveness. These findings support the implementation of UGT1A1 genotyping in routine clinical practice.
    Journal • HEOR • Real-world evidence
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    Trodelvy (sacituzumab govitecan-hziy)
    28d
    Comparative Proteomics Of Hepatocytes And Hepatic Cell Lines Using Swath-MS Reveals Significant Variations In Proteins Involved In Energy, Lipid, And Xenobiotic Metabolism. (PubMed, Curr Drug Metab)
    This study highlights the potential of untargeted global proteomics in detecting differences in protein expression among various hepatic cell lines and provides a comprehensive database to inform the choice of the cell line in future studies.
    Preclinical • Journal
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • CYP2C9 (Cytochrome P450 Family 2 Subfamily C Member 9) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • UGT1A6 (UDP Glucuronosyltransferase Family 1 Member A6) • UGT2B15 (UDP Glucuronosyltransferase Family 2 Member B15) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)
    28d
    SATROPIN: Study of Sacituzumab Govitecan With Atropine to Improve Tolerability in Advanced TNBC and HR+/HER2- Breast Cancer (clinicaltrials.gov)
    P2, N=30, Not yet recruiting, MedSIR
    New P2 trial
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    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    Trodelvy (sacituzumab govitecan-hziy) • Neupogen (filgrastim)
    1m
    Phase 1b Study of EZH1/2 Inhibitor Valemetostat in Combination With Trastuzumab Deruxtecan in Subjects With HER2 Low/Ultra-low/Null Metastatic Breast Cancer (clinicaltrials.gov)
    P1, N=17, Active, not recruiting, M.D. Anderson Cancer Center | Recruiting --> Active, not recruiting | N=37 --> 17
    Enrollment closed • Enrollment change
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    HER-2 (Human epidermal growth factor receptor 2) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    PATHWAY antiHer2/neu (4B5) Rabbit Monoclonal Primary Antibody
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    Enhertu (fam-trastuzumab deruxtecan-nxki) • Ezharmia (valemetostat)
    1m
    Axatilimab Plus Standard of Care Therapy for the Prevention of Graft Versus Host Disease Following Allogeneic Hematopoietic Stem Cell Transplantation in Patients With Hematologic Cancer, ABRAXAS Trial (clinicaltrials.gov)
    P2, N=72, Not yet recruiting, Mayo Clinic
    New P2 trial
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    cyclophosphamide • Niktimvo (axatilimab-csfr)
    1m
    NALIRIFOX versus gemcitabine plus nab-paclitaxel in Chinese patients with advanced pancreatic adenocarcinoma: a randomized, open-label phase II trial. (PubMed, Nat Commun)
    In this phase 2 study (NCT05047991), patients with unresectable metastatic pancreatic adenocarcinoma were randomized to receive NALIRIFOX (liposomal irinotecan, 5-FU, leucovorin, and oxaliplatin) or gemcitabine plus nab-paclitaxel...≥ Grade 3 treatment-emergent adverse events (TEAEs) occurred in 73.1% of patients receiving NALIRIFOX and 84.6% of patients receiving gemcitabine plus nab-paclitaxel, respectively. Despite the premature termination (predetermined sample size of n = 153 not reached) of the study, NALIRIFOX demonstrated improvement in PFS compared with gemcitabine plus nab-paclitaxel, with a manageable safety profile in Chinese patients with advanced pancreatic adenocarcinoma.
    P2 data • Journal
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    gemcitabine • 5-fluorouracil • albumin-bound paclitaxel • oxaliplatin • leucovorin calcium • irinotecan liposomal
    1m
    A Clinical Trial Testing the Safety of BNT327 (an Investigational Drug) and How Well it Works When Combined With Chemotherapy for People Who Have Not Been Treated Yet for Pancreatic Cancer (clinicaltrials.gov)
    P2, N=105, Recruiting, BioNTech SE | Not yet recruiting --> Recruiting
    Enrollment open
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    UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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    gemcitabine • albumin-bound paclitaxel • irinotecan • pumitamig (BNT327)