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H3 Biomedicine Preclinical Studies Show Selective Estrogen Receptor Covalent Antagonist Inactivates Wild-type and Mutant Estrogen Receptor Alphas.

M2 PHARMA-December 8, 2017-H3 Biomedicine Preclinical Studies Show Selective Estrogen Receptor Covalent Antagonist Inactivates Wild-type and Mutant Estrogen Receptor Alphas

(C)2017 M2 COMMUNICATIONS

- Cambridge, Massachusetts-based oncology treatments specialist H3 Biomedicine Inc. scientists have presented data from preclinical studies involving H3B-6545, an oral, selective small molecule covalent antagonist of wild-type and mutant estrogen receptor (ER) in a poster session at the San Antonio Breast Cancer Symposium (SABCS) annual meeting, the company said.

The poster presented at SABCS demonstrated that H3B-6545 has a unique mode of estrogen receptor alpha (ER?) antagonism and exhibits superior preclinical anti-tumor activity to fulvestrant in the MCF-7 xenograft model with once daily oral dosing, achieving maximal antitumor activity at doses >10x below the maximum tolerated dose in mice.

In addition, H3B-6545 demonstrated superior preclinical anti-tumor activity to both tamoxifen and fulvestrant in patient derived xenograft models of breast cancer carrying estrogen receptor mutations.

Based on these results, in September, 2017, H3B-6545 entered into a Phase 1 multi-center, open-label study to evaluate the safety, pharmacokinetics, pharmacodynamics and clinical activity of the compound in women with ER-positive, Her2-negative metastatic breast cancer.

H3B-6545 is an orally bioavailable, potent and selective small molecule modulator of wild-type and mutant estrogen receptor. Scientists at H3 Biomedicine have discovered a new class of ER? antagonists called Selective Estrogen Receptor Covalent Antagonists (SERCAs) that inactivate the estrogen receptor by targeting a cysteine that is not present in other nuclear hormone receptors.

SERCAs have a unique biological and activity profile compared to Selective Estrogen Receptor Modulators (SERMs) and Selective Estrogen Receptor Degraders (SERDs).

Initial clinical development of H3B-6545 will target breast cancer patients with wild-type and mutant ER? and will assess the safety, pharmacokinetics, pharmacodynamics and preliminary efficacy of H3B-6545.

H3 Biomedicine, a member of Eisai's global Oncology Business Group established as a subsidiary of Eisai's US pharmaceutical operation Eisai Inc., specializes in the discovery and development of precision oncology treatments.

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Publication:M2 Pharma
Date:Dec 8, 2017
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