Elimusertib (BAY-1895344) hydrochloride (Synonyms: BAY-1895344 HCl)

Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.

In vitro, BAY 1895344 is shown to be a very potent and highly selective ATR inhibitor (IC50 = 7 nM), which potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC50 = 78 nM). In cellular mechanistic assays BAY 1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC50 = 36 nM)[1].

BAY 1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. It also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies[1]. BAY 1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models[2].

[1] Ulrich T. Luecking, et al. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 983. [2] Antje Margret Wengner, et al. AACR; Cancer Res 2017. 77(13 Suppl):Abstract nr 836.