cofetuzumab pelidotin
An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody against human inactive tyrosine-protein kinase 7 (PTK7) linked, via a cleavable valine-citrulline linker, to an analog of the auristatin microtubule inhibitor dolastatin 10, auristatin-0101, with potential antineoplastic activity. Upon administration, cofetuzumab pelidotin targets and binds to PTK7 expressed on tumor cells. Upon binding, internalization and cleavage, auristatin-0101 binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and apoptosis of PTK7-expressing tumor cells. PTK7, a tumor-associated antigen (TAA), is overexpressed on a variety of cancer cells.
| Synonym: | ADC PF-06647020 ADC PF-7020 |
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| Code name: | h6M24-vc0101 PF 06647020 PF 7020 PF-06647020 PF-7020 PF06647020 |
| Chemical structure: | immunoglobulin G1, anti-(human protein tyrosine kinase 7) (humanized Mus musculus clone hu24 gamma-chain), disulfide with humanized Mus musculus clone hu24 kappa-chain, dimer, thioether with N-(((4-((N-(6-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1-oxohexyl)-L-valyl-N5-(aminocarbonyl)-L-ornithyl)amino)phenyl)methoxy)carbonyl)-2-methylalanyl-N-((1S,2R)-2-methoxy-4-((2S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((1S)-2-phenyl-1-(2-thiazolyl)ethyl)amino)propyl)-1-pyrrolidinyl)-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-L-valinamide |