^
    10ms
    Phase I, open-label, first-in-human (FIH) study of JZP815 in advanced or metastatic solid tumors harboring mitogen-activated protein kinase (MAPK) alterations (ESMO 2023)
    2022; 82:2677. https://doi.org/10.1158/1538-7445.AM2022-2677
    Clinical • P1 data • Metastases
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    BRAF (B-raf proto-oncogene) • NRAS (Neuroblastoma RAS viral oncogene homolog)
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    BRAF V600E • NRAS mutation • BRAF V600 • RAS mutation • NRAS Q61
    |
    JZP815
    2years
    JZP815, a potent and selective pan-RAF inhibitor, demonstrates efficacy in RAF and RAS mutant tumor pre-clinical models (AACR 2022)
    JZP815 demonstrated enhanced activity when combined with inhibitors of other MAPK pathway components in both class 2 and class 3 mutant BRAF patient-derived tumor cells ex vivo, and KRAS mutant NSCLC and CRC xenografts in vivo. In summary, JZP815 is a potent and selective pan-RAF inhibitor that is orally bioavailable in multiple preclinical species with a well-behaved safety profile and pharmacokinetic properties predicted to provide drug exposure required for target engagement in humans, and therefore suitable for advancing into first-in-human trials.
    Preclinical
    |
    KRAS (KRAS proto-oncogene GTPase) • ARAF (A-Raf Proto-Oncogene)
    |
    KRAS mutation • BRAF mutation
    |
    JZP815