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Tengonermin, also known as NGR-hTNF, is a vascular-targeting drug. It is a recombinant protein and peptide-targeted agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. This drug works by modifying the tumor microenvironment and increasing intratumoral chemotherapy penetration and T-cell infiltration. NGR-hTNF specifically targets angiogenic tumor blood vessels using the NGR motif. Literature demonstrates that NGR-peptides bind to a CD13 isoform, of which expression is restricted to tumor vasculature cells. A study also demonstrated that binding of the NGR-motif to CD13 determined both the homing of NGR-hTNF to tumor vessels and the increase in its antiangiogenic activity.
Tengonermin, also known as NGR-hTNF, is a vascular-targeting drug. It is a recombinant protein and peptide-targeted agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide. This drug works by modifying the tumor microenvironment and increasing intratumoral chemotherapy penetration and T-cell infiltration. NGR-hTNF specifically targets angiogenic tumor blood vessels using the NGR motif. Literature demonstrates that NGR-peptides bind to a CD13 isoform, of which expression is restricted to tumor vasculature cells. A study also demonstrated that binding of the NGR-motif to CD13 determined both the homing of NGR-hTNF to tumor vessels and the increase in its antiangiogenic activity.
Tengonermin has highly selective homing to tumor blood vessels due to the NGR peptide portion binding specifically to a CD13 isoform (expressed selectively by endothelial cells of human tumor vessels during neoangiogenesis) which allows it to spare tumor-unrelated human tissues. This drug also increases apoptosis of angiogenic endothelial cells in vivo. The aforementioned effects significantly contribute to controlling the growth of tumors. Once the drug targets the tumor vasculature, multiple downstream effects occur, mediated by the interaction of both components of the molecule.
One entry per invention. Patent families filed in the US, EP, WO and CN offices.
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