{"id":13429,"date":"2024-02-22T17:14:00","date_gmt":"2024-02-22T17:14:00","guid":{"rendered":"https:\/\/www.sygnaturediscovery.com\/?post_type=journal-paper&#038;p=13429"},"modified":"2026-01-30T09:10:10","modified_gmt":"2026-01-30T09:10:10","slug":"discovery-of-the-potent-and-selective-atr-inhibitor-camonsertib-rp-3500","status":"publish","type":"journal-paper","link":"https:\/\/www.sygnaturediscovery.com\/fr\/journal-paper\/discovery-of-the-potent-and-selective-atr-inhibitor-camonsertib-rp-3500\/","title":{"rendered":"Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500)"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">W Cameron Black,\u00a0<strong>Abbas Abdoli<\/strong>,\u00a0Xiuli An,\u00a0Anick Auger,\u00a0Patrick Beaulieu,\u00a0Michel Bernatchez,\u00a0Cathy Caron,\u00a0Amandine Chefson,\u00a0<strong>Sheldon Crane<\/strong>,\u00a0Mohamed Diallo,\u00a0St\u00e9phane Dorich,\u00a0Lee D Fader,\u00a0Gino B Ferraro,\u00a0Sara Fournier,\u00a0Qi Gao,\u00a0Yelena Ginzburg,\u00a0Martine Hamel,\u00a0Yongshuai Han,<strong>\u00a0Paul Jones<\/strong>,\u00a0<strong>St\u00e9phanie Lanoix<\/strong>,\u00a0<strong>Cyrus M Lacbay<\/strong>,\u00a0Marie-Eve Leclaire,\u00a0Maayan Levy,\u00a0Yael Mamane,\u00a0<strong>Amina Mulani<\/strong>,\u00a0Robert Papp,\u00a0Charles Pellerin,\u00a0Audrey Picard,\u00a0Alexander Skeldon,\u00a0Kathryn Skorey,\u00a0Rino Stocco,\u00a0Miguel St-Onge,\u00a0Jean-Fran\u00e7ois Truchon,\u00a0<strong>Vouy Linh Truong<\/strong>,\u00a0Michal Zimmermann<sup>\u00a0<\/sup><\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><strong>Abstract<\/strong><\/p>\n\n\n\n<p class=\"wp-block-paragraph\">ATR is a key kinase in the DNA-damage response (DDR) that is synthetic lethal with several other DDR proteins, making it an attractive target for the treatment of genetically selected solid tumors. Herein we describe the discovery of a novel ATR inhibitor guided by a pharmacophore model to position a key hydrogen bond. Optimization was driven by potency and selectivity over the related kinase mTOR, resulting in the identification of camonsertib (RP-3500) with high potency and excellent ADME properties. Preclinical evaluation focused on the impact of camonsertib on myelosuppression, and an exploration of intermittent dosing schedules to allow recovery of the erythroid compartment and mitigate anemia. Camonsertib is currently undergoing clinical evaluation both as a single agent and in combination with talazoparib, olaparib, niraparib, lunresertib, or gemcitabine (NCT04497116,&nbsp;NCT04972110,&nbsp;NCT04855656). A preliminary recommended phase 2 dose for monotherapy was identified as 160 mg QD given 3 days\/week.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\">Ref: <a href=\"https:\/\/pubmed.ncbi.nlm.nih.gov\/38299539\/\">J Med Chem 2024<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"","protected":false},"featured_media":0,"template":"","category":[682,713],"resource_tag":[],"class_list":["post-13429","journal-paper","type-journal-paper","status-publish","hentry","category-chemistry","category-medicinal-chemistry"],"acf":[],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.6 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Camonsertib (RP-3500): Selective ATR Inhibitor | Paper<\/title>\n<meta name=\"description\" content=\"Discovery of camonsertib, optimized for ATR potency and selectivity over mTOR, with intermittent dosing explored to mitigate myelosuppression. 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