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Zhang JYJ, Zhang J, Kiffe M, et al. Preclinical Pharmacokinetics and Metabolism of MAK683, a Clinical Stage Selective Oral Embryonic Ectoderm Development (EED) Inhibitor for Cancer Treatment. Xenobiotica. 2021;1-48doi: 10.1080/00498254.2021.2005852.
Zhang, J. Y. J., Zhang, J., Kiffe, M., Walles, M., Jin, Y., Blanz, J., Dayer, J., Sanchez, A., Zhang, C., Zhang, L., Huang, Y., & Oyang, C. (2021). Preclinical Pharmacokinetics and Metabolism of MAK683, a Clinical Stage Selective Oral Embryonic Ectoderm Development (EED) Inhibitor for Cancer Treatment. Xenobiotica; the fate of foreign compounds in biological systems, 1-48. https://doi.org/10.1080/00498254.2021.2005852
Zhang, Ji Yue Jeff, et al. "Preclinical Pharmacokinetics and Metabolism of MAK683, a Clinical Stage Selective Oral Embryonic Ectoderm Development (EED) Inhibitor for Cancer Treatment." Xenobiotica; the fate of foreign compounds in biological systems vol. (2021): 1-48. doi: https://doi.org/10.1080/00498254.2021.2005852
Zhang JYJ, Zhang J, Kiffe M, Walles M, Jin Y, Blanz J, Dayer J, Sanchez A, Zhang C, Zhang L, Huang Y, Oyang C. Preclinical Pharmacokinetics and Metabolism of MAK683, a Clinical Stage Selective Oral Embryonic Ectoderm Development (EED) Inhibitor for Cancer Treatment. Xenobiotica. 2021 Nov 11;1-48. doi: 10.1080/00498254.2021.2005852. Epub 2021 Nov 11. PMID: 34761729.
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Xenobiotica. 2021 Nov 11;1-48. doi: 10.1080/00498254.2021.2005852. Epub 2021 Nov 11.

Preclinical Pharmacokinetics and Metabolism of MAK683, a Clinical Stage Selective Oral Embryonic Ectoderm Development (EED) Inhibitor for Cancer Treatment.

Xenobiotica; the fate of foreign compounds in biological systems

Ji Yue Jeff Zhang, Jiangwei Zhang, Michael Kiffe, Markus Walles, Yi Jin, Joachim Blanz, Jerôme Dayer, Arevalo Sanchez, Chunye Zhang, Lijun Zhang, Ying Huang, Counde Oyang

Affiliations

  1. Novartis Institutes for BioMedical Research, Shanghai, China.
  2. Novartis Institutes for BioMedical Research, Basel, Switzerland.

PMID: 34761729 DOI: 10.1080/00498254.2021.2005852

Abstract

1. MAK683 (N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine) is a potent and orally bioavailable EED inhibitor for the potential treatment in oncology. Pharmacokinetics (PK) in preclinical species are characterized by low to moderate plasma clearances, high oral exposure and moderate to high oral bioavailability at dose of 1-2 mg/kg.2. A species comparison of the metabolic pathways of MAK683 has been made using [

Keywords: CYP; EED; EZH2; PK; drug disposition; metabolism; metabolite identification

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