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over1year
New P1 trial • Metastases
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RET (Ret Proto-Oncogene)
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RET fusion • RET mutation
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APS03118
2years
The preclinical selectivity and activity of APS03118, a highly selective and potent next-generation RET inhibitor (AACR 2022)
Selective RET inhibitors selpercatinib and pralsetinib were recently approved by the FDA and EMA for patients with RET-dependent NSCLC and thyroid cancers. APS03118 is a novel highly selective next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFMs-mediated resistance. A first-in-human phase 1 trial for patients with RET-driven solid tumors with activating RET alterations is planned for 2022.
Preclinical
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RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B) • KDR (Kinase insert domain receptor) • CCDC6 (Coiled-Coil Domain Containing 6)
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RET fusion • RET mutation • RET M918T • RET C634W • RET V804L • RET V804M • RET C634* • RET V804*
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Retevmo (selpercatinib) • Gavreto (pralsetinib) • APS03118