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Potent and highly selective inhibition of selpercatinib towards UDP-glucuronosyltransferase 1A4 (UGT1A4) isoform.

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Toxicology and applied pharmacology 2025 Vol.500() p. 117393
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유사 논문
P · Population 대상 환자/모집단
환자: RET fusion-positive thyroid cancer and non-small-cell lung cancer
I · Intervention 중재 / 시술
추출되지 않음
C · Comparison 대조 / 비교
추출되지 않음
O · Outcome 결과 / 결론
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.

Liu Y, Lv X, Yin H, Jiang L

PubMed ↗ DOI ↗ BibTeX ↓ RIS ↓
📝 환자 설명용 한 줄

Selpercatinib is a potent and highly selective Rearranged during Transfection (RET) kinase inhibitor for patients with RET fusion-positive thyroid cancer and non-small-cell lung cancer.

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↓ .bib ↓ .ris
APA Liu Y, Lv X, et al. (2025). Potent and highly selective inhibition of selpercatinib towards UDP-glucuronosyltransferase 1A4 (UGT1A4) isoform.. Toxicology and applied pharmacology, 500, 117393. https://doi.org/10.1016/j.taap.2025.117393
MLA Liu Y, et al.. "Potent and highly selective inhibition of selpercatinib towards UDP-glucuronosyltransferase 1A4 (UGT1A4) isoform.." Toxicology and applied pharmacology, vol. 500, 2025, pp. 117393.
PMID 40354983
DOI 10.1016/j.taap.2025.117393

Abstract

Selpercatinib is a potent and highly selective Rearranged during Transfection (RET) kinase inhibitor for patients with RET fusion-positive thyroid cancer and non-small-cell lung cancer. The present study aims to investigate the inhibitory effects of selpercatinib towards human UDP-glucuronosyltransferases (UGTs), and assess its risk for drug-drug interactions (DDIs) via UGT inhibition. The inhibition of selpercatinib towards 12 recombinant human UGT isoforms were measured. Our data demonstrated that selpercatinib exhibited highly selective inhibition towards UGT1A4. Enzyme kinetic study indicated that selpercatinib competitively inhibited the activity of UGT1A4, with a K value of 1.57 ± 0.14 μM. 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.

MeSH Terms

Glucuronosyltransferase; Humans; Pyrazoles; Isoenzymes; Drug Interactions; Protein Kinase Inhibitors; Kinetics; Recombinant Proteins; Pyridines

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