Chemistry:IDRX-42
From HandWiki
IDRX-42 (formerly M4205) is a highly selective small molecule KIT inhibitor compound developed for the treatment of gastrointestinal stromal tumors.[1][2][3] The compound was originally discovered by the German company Merck[4] and later out-licensed to IDRX. In November 2024, promising anti-tumor data from ongoing Phase 1/1B studies were reported.[5] In January 2025, the compound played a key role in the $1 billion acquisition of IDRX by GSK.[6]
References
- ↑ "Antitumor Efficacy of the Novel KIT Inhibitor IDRX-42 (Formerly M4205) in Patient- and Cell Line-Derived Xenograft Models of Gastrointestinal Stromal Tumor (GIST)". Clinical Cancer Research 29 (15): 2859–2868. August 2023. doi:10.1158/1078-0432.CCR-22-3822. PMID 37223931.
- ↑ "Phase 1/1b first-in-human study of IDRX-42, a novel oral tyrosine kinase inhibitor (TKI), in patients with metastatic and/Or unresectable gastrointestinal stromal tumors (GISTs)". Journal of Clinical Oncology 41 (4_suppl). 2023. doi:10.1200/JCO.2023.41.4_suppl.TPS483.
- ↑ "StrateGIST 1: A first-in-human (FIH), phase 1 study of IDRX-42 in patients with metastatic gastrointestinal stromal tumors resistant to prior treatment with tyrosine kinase inhibitors (TKIs)". Journal of Clinical Oncology 42 (16_suppl). 2024. doi:10.1200/JCO.2024.42.16_suppl.11501.
- ↑ "Identification of M4205─A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors". Journal of Medicinal Chemistry 66 (4): 2386–2395. February 2023. doi:10.1021/acs.jmedchem.2c00851. PMID 36728508.
- ↑ "IDRx Announces Updated Phase 1 Data from Ongoing Phase 1/1b StrateGIST 1 Trial of IDRX-42 in Advanced Gastrointestinal Stromal Tumors (GIST) at CTOS 2024". IDRx. https://idrx.com/resources/idrx-announces-updated-phase-1-data-from-ongoing-phase-1-1b-strategist-1-trial-of-idrx-42-in-advanced-gastrointestinal-stromal-tumors-gist-at-ctos-2024/.
- ↑ "GSK enters agreement to acquire IDRx, Inc.". GSK. https://www.gsk.com/en-gb/media/press-releases/gsk-enters-agreement-to-acquire-idrx-inc/.
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