Yesterday abstracts were released for the American Association of Cancer Research meeting, which is being convened in Philadelphia, April 18-22. The development of ARIA's potentially best-in-class ALK inhibitor will be presented in an oral session #2872 where we assume data on selectivity as outlined in abstract #781 will be discussed. As outlined in #782, ARIA has tested Brigatinib against Crizotinib (Xalkori), Ceritinib (Zykadia) and Alectinib in an in-vivo model of Ba/F3 cells expressing wild type or one of 17 different resistance mutations, using drug levels that are clinical effective (Ceff) based on reported steady state data. For index compound Xalkori, the Ceff for WT ALK was only - 2 fold higher than the 1C50 and 8110 previously described mutants conferring clinical resistance were found to have IC50s higher than Ceff. Only for Brigatinib was the IC50 for all 17 mutants below the Ceff, and only Brigatinib demonstrated significant efficacy against the most challenging G1202R mutant. ARIA also note that in a brain metastasis model, Brigatinib markedly enhanced survival vs. Xalkori.
• In our view these are the most compelling data presented to date that Brigatinib is a best-in-class ALK inhibitor.
• Data of this caliber should be sufficient to engage a partner in meaningful discussion for Brigatinib co-development.
One of the company's shareholders who did not want to be named told the Boston Business Journal that "numerous large shareholders" in the company — which includes BlackRock, Fidelity and Adage Capital — agree that Berger's departure from the company would increase its value.