CHEYENNE, Wyo., Oct. 30, 2017 /PRNewswire/ — Xynomic Pharma, a clinical stage US oncology drug development company, today announced that it has acquired exclusive global rights to develop, manufacture and commercialize BI 882370, a 2nd-generation RAF inhibitor, from Boehringer Ingelheim, a top-20 global pharmaceutical company.  Under the terms of the agreement Xynomic will pay upfront, milestone and royalty payments up to approximately $502 million.

BI 882370 is a potent and selective RAF inhibitor uniquely binding to the DFG-out conformation, whereas marketed BRAF inhibitors occupy the DFG-in conformation.  BI 882370 inhibited proliferation of BRAF^mut melanoma cell lines with 100x higher potency (EC₅₀ 1 – 10 nM) than vemurafenib (VEM), a marketed BRAF inhibitor.

In the colorectal cancer (CRC) animal models, BI 882370 was superior to VEM in both the Colo-205^V600V/E model and HT-29^V600V/E model.  BI 882370 in combination with cetuximab induced tumor regressions in the less sensitive HT-29 model.

In melanoma’s G-361^V600V/E model, BI 882370 was superior to VEM, marketed BRAF inhibitor dabrafenib (DAB), marketed MEK inhibitor trametinib (TRA) and DAB-TRA combination. In a second melanoma model A375^V600E in which tumors developed resistance to VEM, the TRA-BI 882370 combination demonstrated superior efficacy over TRA-DAB combination.

There were no relevant findings in exploratory toxicology studies at exposures delivering efficacy superior to VEM, DAB and TRA.

“BI 882370, with an impressive efficacy and safety profile demonstrated in animal models, is well positioned to become a best-in-class 2nd-generation Pan-RAF inhibitor for the treatment of B-RAF mutant cancers including CRC and melanoma.  We are honored to partner with BI, a global leader in oncology, and will move this asset into clinical testing expeditiously,” said Y. Mark Xu, Chairman, CEO and President of Xynomic.

RAF inhibitors have attracted resurged and strong interest in oncology.  Compared to 1st-generation, BI 882370 may provide an improved therapeutic window, enabling more pronounced and longer-lasting pathway suppression and thus resulting in improved efficacy.

Xynomic’s pipeline also includes Abexinostat, a potentially best-in-class HDAC inhibitor entering global pivotal Ph 3 trials against Non-Hodgkin’s lymphoma and renal cell carcinoma.

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