Discovery and Characterization of JDQ443: a Structurally Novel Covalent Inhibitor of KRASG12C

Elizabeth McKenna, PhD, interviews Saskia Brachmann, PhD, Anna Farago, MD, PhD, and Andreas Weiss, PhD, about their paper describing a novel KRAS G12C inhibitor that was published concurrently with a Clinical Trials Minisymposium presentation at the 2022 AACR Annual Meeting. aacrjournals.org/cancerdiscovery/article/12/6/1500/699171
https://vimeo.com/720726054 iPRECIO SMP-310R Programmable pumps were used to better understand the relationship between PK, target occupancy, and efficacy.

[Webinar] "Discovery of JDQ443, a structurally novel, potent and selective covalent oral inhibitor of KRASG12C"; MedChemCASES #16: Dr. Simona Cotesta - " We describe the hit to lead and lead optimization by structure-based design of the novel chemical series leading to the discovery of NVP-JDQ443 (JDQ443), a novel, potent and selective, orally bioavailable KRASG12C covalent inhibitor. JDQ443 showed dose dependent antitumor efficacy in KRAS G12C-mutated cell-derived models and is currently in clinical development as monotherapy as well as in combination with TNO155, a SHP2 inhibitor (NCT04699188). " excerpt from https://www.gdch.de/netzwerk-strukturen/fachstrukturen/medizinische-chemie/veranstaltungen/medchemcases.html

dr Simona Cotesta (Novartis)
June 22, 2022
5:00 PM (Berlin time)
Registration link:https://us06web.zoom.us/webinar/register/WN_sgiCAfMKSISajiGRxoeb8w

iPRECIO SMP-310R Programmable pumps were used to better understand the relationship between PK, target occupancy, and efficacy.
" These findings demonstrate that antitumor activity can be achieved under both q.d. and b.i.d. dosing. To better understand the relationship between PK, target occupancy, and efficacy, a continuous infusion xenograft study was performed in the LU99 xenograft model and the PK/TO model applied to estimate the resulting levels of KRAS(G12C) target occupancy. " excerpt from publication, "Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRAS(G12C) Wiess et al. Cancer Discov OF1–OF18. https://lnkd.in/dikpP9Ej [Open Access]

Now all open access. No registration required: Compound Delivery, PK-PD, & Validation Studies in Oncology Research.
Slide deck, Expert Answers, Q&A Report, and On-demand Webinar< here >. Learn how Christian Schnell, Associate Director Oncology NIBR, Novartis Pharma AG, Basel, CH reached his conclusions.

Our iPRECIO Mouse pumps were mentioned by Jamie Oliver Chief Medical Officer of Starton Therapeutics at Precision Blood Cancer Symposium September 2021. Presentation available <here>