Synonyms: PR610 | tarloxotinib cation | TH-4000
Compound class:
Synthetic organic
Comment: Tarloxotinib (TH-4000) is a hypoxia-activated prodrug (HAP) [1] being developed by Threshold Pharmaceuticals. Delivered as the bromide salt (PubChem CID 51038315) as described in its INN record. The compound undergoes activation selectively within the hypoxic tumour compartment to produce an irreversible pan-ErbB tyrosine-kinase inhibitor, represented by TH-4000E [1]. The 4-nitroimidazole trigger on the tertiary amine side chain facilitates activation. This is one of the first molecularly targeted HAPs to be developed.
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Bioactivity Comments |
To date (Nov 2016) data for this drug has been published in abstract form only (Abstract 5358: The hypoxia-activated EGFR-TKI TH-4000 overcomes erlotinib-resistance in preclinical NSCLC models at plasma levels achieved in a Phase 1 clinical trial and Abstract e13548: TH-4000, a hypoxia-activated EGFR/Her2 inhibitor to treat EGFR-TKI resistant T790M-negative NSCLC. We await publication in a peer reviewed article. |
Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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