@article{60da67234ed445c49cd4d915ab255d5b,
title = "Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties",
abstract = "Inhibition of glutaminase-1 (GLS-1) hampers the proliferation of tumor cells reliant on glutamine. Known glutaminase inhibitors have potential limitations, and in vivo exposures are potentially limited due to poor physicochemical properties. We initiated a GLS-1 inhibitor discovery program focused on optimizing physicochemical and pharmacokinetic properties, and have developed a new selective inhibitor, compound 27 (IPN60090), which is currently in phase 1 clinical trials. Compound 27 attains high oral exposures in preclinical species, with strong in vivo target engagement, and should robustly inhibit glutaminase in humans.",
author = "Soth, {Michael J.} and Kang Le and {Di Francesco}, {Maria Emilia} and Hamilton, {Matthew M.} and Gang Liu and Burke, {Jason P.} and Carroll, {Chris L.} and Kovacs, {Jeffrey J.} and Bardenhagen, {Jennifer P.} and Bristow, {Christopher A.} and Mario Cardozo and Barbara Czako and {De Stanchina}, Elisa and Ningping Feng and Garvey, {Jill R.} and Gay, {Jason P.} and Do, {Mary K.Geck} and Jennifer Greer and Michelle Han and Angela Harris and Zachary Herrera and Sha Huang and Virginia Giuliani and Yongying Jiang and Johnson, {Sarah B.} and Johnson, {Troy A.} and Zhijun Kang and Leonard, {Paul G.} and Zhen Liu and Timothy McAfoos and Meredith Miller and Pietro Morlacchi and Mullinax, {Robert A.} and Palmer, {Wylie S.} and Jihai Pang and Norma Rogers and Rudin, {Charles M.} and Shepard, {Hannah E.} and Spencer, {Nakia D.} and Jay Theroff and Qi Wu and Alan Xu and Yau, {Ju Anne} and Giulio Draetta and Carlo Toniatti and Heffernan, {Timothy P.} and Philip Jones",
note = "Publisher Copyright: {\textcopyright} 2020 American Chemical Society. All rights reserved.",
year = "2020",
month = nov,
day = "12",
doi = "10.1021/acs.jmedchem.0c01398",
language = "English (US)",
volume = "63",
pages = "12957--12977",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "21",
}