UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)

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27d

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.

27 days ago

Preclinical • Journal

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)

4ms

Physiologically Based Pharmacokinetic Modeling and Simulations in Lieu of Clinical Pharmacology Studies to Support the New Drug Application of Asciminib. (PubMed, Pharmaceutics)

Additional studies evaluated the impact of strong CYP3A4 perpetrators and imatinib on a single 40 mg dose of asciminib. This PBPK model was applied in lieu of clinical pharmacology studies to support the new drug application of Scemblix® and to bridge data from 40 mg BID to the 80 mg QD and 200 mg BID dose regimens. The PBPK predictions informed the drug product label and are estimated to have replaced at least 10 clinical studies.

4 months ago

NDA • PK/PD data • Journal

CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • UGT2B17 (UDP Glucuronosyltransferase Family 2 Member B17) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)

imatinib • Scemblix (asciminib)

almost2years

Metabolism characterization and toxicity of N-hydap, a marine candidate drug for lung cancer therapy by LC-MS method. (PubMed, Nat Prod Bioprospect)

Furthermore, N-hydap was found to affect the catalytic activity of drug metabolic enzymes (DMEs), particularly increasing the activity of UGT1A3, suggesting potential for DDIs. Understanding the metabolic pathways and properties of N-hydap should improve our knowledge of its drug efficacy, toxicity, and potential for DDIs.

almost 2 years ago

Journal

UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)

2years

Pharmacogenetics and Pharmacokinetics of Posaconazole in Patients with Acute Myeloid Leukemia: Useful Tools for Antifungal Stewardship (ASH 2023)

According to EORTC criteria, two patients (10%) had a probable IFI on day 14, and antifungal therapy with liposomal amphotericin B was started [3]...Isavuconazonium or posaconazole for antifungal prophylaxis in patients with acute myeloid leukemia... Twenty patients were included: 9 were women (45%) with a median age of 67 years old (±10. 5) and a median Charlson Comorbidity Index of 5 (±1. 3).

2 years ago

Clinical • PK/PD data

ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • SLCO1B3 (Solute carrier organic anion transporter family member 1B3) • ABCC2 (ATP Binding Cassette Subfamily C Member 2) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)

UGT1A1*1*1

Noxafil (posaconazole)

over2years

Characterization of the glucuronidating pathway of pectolinarigenin, the major active constituent of the Chinese medicine Daji, in humans and its influence on biological activities. (PubMed, J Ethnopharmacol)

Our results demonstrate that 7-O-glucuronidation is the major metabolic pathway of PEC in human tissues, while UGT1A1, 1A3 and 1A9 are key contributing enzymes responsible for PEC-7-O-glucuronidation in human liver. It is also found that PEC 7-O-glucuronidation significantly weakens the Nrf2 and PPAR agonist effects. All these findings are very helpful for the pharmacologists to deep understand the metabolic rates of PEC in humans.

over 2 years ago

Journal

UGT1A1 (UDP glucuronosyltransferase family 1 member A1) • UGT1A9 (UDP Glucuronosyltransferase Family 1 Member A9) • PPARA (Peroxisome Proliferator Activated Receptor Alpha) • UGT1A3 (UDP Glucuronosyltransferase Family 1 Member A3)

UGT1A1*1*1

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.

over 2 years ago

Journal

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)

HER-2 positive • UGT1A1*1*1

Tukysa (tucatinib)