Supplementary Tables 1 - 8 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Autor: Shin-San Michael Su, Scott A. Biller, Virginie Penard-Lacronique, Marion Dorsch, Lenny Dang, Hua Yang, Wei Liu, Lee Silverman, Shengfang Jin, Wentao Wei, Fan Jiang, Cheng Fang, YingXia Xu, Monika Pilichowska, Benoît S. Marteyn, Stéphane de Botton, Olivier A. Bernard, Sophie Broutin, Angelo Paci, Véronique Saada, Olivia Bawa, Paule Opolon, Cyril Quivoron, Francesco G. Salituro, Jeffrey O. Saunders, Giovanni Cianchetta, Zenon Konteatis, Lei Jin, Sung Choe, Raj Nagaraja, Yue Chen, Erica Tobin, Byron DeLaBarre, Stefan Gross, Anil Padyana, Kimberly Straley, Erin Artin, Muriel D. David, Fang Wang, Jeremy Travins, Katharine Yen

Supplementary Table 1. Drug metabolism and pharmacokinetic attributes of AG-221. Supplementary Table 2. Selectivity of AG-221 confirmed by testing against a panel of kinases. Supplementary Table 3. Clinical characteristics of patients with IDH2R140Q-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bd472a11c8ff29b3f26438ea494ea5d
https://doi.org/10.1158/2159-8290.22531936

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion

Autor: Joshua Murtie, Anil K. Padyana, Lei Jin, Marc L. Hyer, Zhixiao Liu, Scott A. Biller, Jeremy Travins, Amelia Barnett, Katya Marjon, Brandon Nicolay, Wentao Wei, Raj Nagaraja, Cheng Fang, Yi Gao, Yabo Sun, Ye Zhixiong, Fan Jiang, Peter Kalev, Stefan Gross, Zenon D. Konteatis, Byron DeLaBarre, Zhihua Sui, Kevin Marks, Lenny Dang, Jie Yu, Everton Mandley, Yue Chen

Publikováno v: Journal of Medicinal Chemistry. 64:4430-4449

The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (MTAP) gene, which is adjacent to the CDKN2A tumor suppressor and co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::97283e129d6853ac6b9ff735db2724ec
https://doi.org/10.1021/acs.jmedchem.0c01895

Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous

Autor: Zenon, Konteatis, Jeremy, Travins, Stefan, Gross, Katya, Marjon, Amelia, Barnett, Everton, Mandley, Brandon, Nicolay, Raj, Nagaraja, Yue, Chen, Yabo, Sun, Zhixiao, Liu, Jie, Yu, Zhixiong, Ye, Fan, Jiang, Wentao, Wei, Cheng, Fang, Yi, Gao, Peter, Kalev, Marc L, Hyer, Byron, DeLaBarre, Lei, Jin, Anil K, Padyana, Lenny, Dang, Joshua, Murtie, Scott A, Biller, Zhihua, Sui, Kevin M, Marks

Publikováno v: Journal of medicinal chemistry. 64(8)

The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::6ec9204e0504cb32589dbe975f9a1cd3
https://pubmed.ncbi.nlm.nih.gov/33829783

Effect of Mild and Moderate Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of a Single Dose of Oral Ivosidenib in Otherwise Healthy Participants

Autor: Marvin Cohen, Feng Yin, Frank G. Basile, Bin Fan, Caroline Almon, Michelle Mobilia, David Dai, Hua Yang, Raj Nagaraja, Huansheng Xu

Publikováno v: Clinical pharmacology in drug developmentReferences. 10(1)

Ivosidenib, a small-molecule inhibitor of mutant isocitrate dehydrogenase 1, is primarily cleared by hepatic metabolism. This open-label study investigated the impact of hepatic impairment on ivosidenib pharmacokinetics (ClinicalTrials.gov: NCT032825

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https://pubmed.ncbi.nlm.nih.gov/32648303

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Autor: Olivia Bawa, Monika Pilichowska, Paule Opolon, Jeffrey O. Saunders, Fang Wang, Cyril Quivoron, Anil K. Padyana, Zenon D. Konteatis, Kimberly Straley, Erica Tobin, Sophie Broutin, Marion Dorsch, Hua Yang, Byron DeLaBarre, Jeremy Travins, Sung Choe, Yue Chen, Lei Jin, Wentao Wei, Virginie Penard-Lacronique, Raj Nagaraja, Wei Liu, Lenny Dang, Shengfang Jin, Cheng Fang, Lee Silverman, Fan Jiang, Katharine E. Yen, Giovanni Cianchetta, Olivier Bernard, Erin Artin, Muriel D. David, Shin-San Michael Su, Stefan Gross, Francesco G. Salituro, Véronique Saada, Stéphane de Botton, Scott A. Biller, Angelo Paci, Benoit S. Marteyn, Yingxia Xu

Publikováno v: Cancer Discovery
Cancer Discovery, American Association for Cancer Research, 2017, 7 (5), pp.478-493. ⟨10.1158/2159-8290.CD-16-1034⟩

Somatic gain-of-function mutations in isocitrate dehydrogenases (IDH) 1 and 2 are found in multiple hematologic and solid tumors, leading to accumulation of the oncometabolite (R)-2-hydroxyglutarate (2HG). 2HG competitively inhibits α-ketoglutarate�

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e5319b71d47ef568ebb071e758566cc
https://doi.org/10.1158/2159-8290.cd-16-1034