MI130004 Shows Positive in vivo Activity against HER2-Expressing Tumors

Positive results of MI130004, a novel antibody-drug conjugate combining trastuzumab via Cys residues through a non-hydrolysable linker, with PM050489, a molecule of marine origin, were published Molecular Cancer Therapeutics, published by the American Association for Cancer Research (AACR).[1]

The investigational ADC is being developed by PharmaMar.

The cytotoxic payload, PM050489, originally isolated from the marine sponge lithoplocamia lithistoides, binds β-tubulin with very high affinity and disrupts the microtubule network, impairing its function during divison, which leads to mitotic aberrations and cell death.

MabPlex
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In HER2-expressing tumors, MI130004 generates a longer lasting response and inhibits significantly tumor growth providing a higher median progression free survival time in comparison with trastuzumab.


Researchers at PharmaMar have analyzed the antitumor activity of MI130004 in different tumor cell lines, including breast, ovarian and gastric cancers, that express different levels of HER2 in both in vitro and in vivo tests.

Formula: The choro-derivative, PM-050489, is the payload Pharmamar’s investigational ADC MI130004, using a non-hydrolyzable linker to traztuzumab.

The results show that in HER2-expressing tumors, MI130004 generates a longer lasting response and inhibits significantly tumor growth providing a higher median progression free survival time in comparison with trastuzumab.

MI130004 is the result of the research carried out by researchers at PharmaMar to identify and synthesize molecules of a marine origin for their use as active agents in antibody-drug conjugates, as is the case with PM050489.

PharmaMar is positioning itself as a supplier of cytotoxic products that are necessary for companies specialized in the antibody-drug conjugate technology.