tarloxotinib

Tarloxotinib is a hypoxia-activated prodrug of a pan-ErbB (HER) kinase inhibitor, designed to exploit the low oxygen environment of tumors for selective activation. Once inside hypoxic tumor cells, it is converted into an irreversible inhibitor targeting multiple members of the ErbB family, including epidermal growth factor receptor (EGFR), HER2 (ERBB2), and potentially other HER kinases. This mechanism aims to inhibit cellular proliferation and differentiation in tumor cells overexpressing these kinases while sparing normal tissues, potentially reducing systemic toxicity. Tarloxotinib has been investigated primarily for non-small cell lung cancer (NSCLC) with EGFR exon 20 insertions or HER2 activating mutations, as well as other solid tumors harboring NRG1 fusions or alterations in ERBB genes[3][4][5][6]. It was developed by Rain Oncology and originated at the University of Auckland[3].

Brand names

Hypoxin

Other names

tarloxotinib cationtarloxotinib ionH8768UL06VH-8768UL06VH 8768UL06V