CAMBRIDGE, MA, USA I November 20, 2013 I Tensha Therapeutics announced today it has begun the first clinical trial of its small molecule, bromodomain and extra-terminal domain (BET) bromodomain inhibitor, TEN-010 for the treatment of cancer. The trial is designed to assess the safety, tolerability and anti-tumor activity of TEN-010 in patients with advanced solid tumors that are refractory or intolerant to standard/approved therapies and NUT midline carcinoma (NMC), a highly aggressive cancer with very limited treatment options.

“BET bromodomains are a new and highly promising class of epigenetic targets that are directly implicated in the activation of oncogenes such as Myc, one of the most common overexpressed genes in many cancers,” said Douglas E. Onsi, Chief Executive Officer of Tensha and Managing Director of Tensha’s venture capital investor, HealthCare Ventures. “We are very enthusiastic about the broad potential clinical applicability of targeting these chromatin ‘readers’.”

“TEN-010 is a highly selective, potent BET bromodomain inhibitor and we have moved rapidly to advance its development,” said Steven Landau, MD, Chief Medical Officer of Tensha and Director of Clinical and Scientific Analysis for HealthCare Ventures. “We are very pleased to be bringing this new molecule into the clinic in this patient group, for which there is a critical need for new treatment options.”

Bromodomains, which are modules contained within epigenetic proteins, play critical roles in influencing gene transcription by functioning as ‘readers’ of epigenetic marks. Once bound to chromatin, these bromodomain-containing proteins can influence gene expression. Tensha’s Founder, James Bradner, MD, an Assistant Professor at Harvard Medical School and Investigator at the Dana-Farber Cancer Institute, was the first to recognize the broad potential of small molecule BET bromodomain inhibitors across a range of therapeutic areas. Dr. Bradner’s seminal work identified NMC as sensitive to BET bromodomain inhibition. NMC is a rare, invariably fatal cancer caused in the majority of cases by a gene translocation event that results in the expression of the NUT protein fused to the BET bromodomains of BRD3 or BRD4.

Subsequent studies from Dr. Bradner’s and collaborating laboratories have established BET bromodomain inhibition as a therapeutic strategy to target Myc overexpression and demonstrated the potential of this approach to other cancers, including multiple myeloma, acute myeloid leukemia, non-small cell lung cancer and neuroblastoma.

“From the time of our initial publication of the BET bromodomain inhibitor JQ1 in Nature in 2010, we looked forward to the day when we would see novel BET bromodomain inhibitors translated from lab bench to bedside to treat patients with cancer. Tensha is now poised to test TEN-010’s ability to deliver clinically on the promise that we saw in our preclinical experiments,” said James Bradner, MD, Founder of Tensha and Assistant Professor, Harvard Medical School and Investigator, Department of Medical Oncology, Dana-Farber Cancer Institute.

About Tensha Therapeutics

Tensha Therapeutics is developing small molecule bromodomain inhibitors, a new class of epigenetic modulators of gene expression, to treat cancer and other serious disorders. The company’s programs are based on the discovery of potent small molecule BET bromodomain inhibitors from the laboratory of Dr. James Bradner at Harvard Medical School and the Dana-Farber Cancer Institute. Tensha’s lead compound, TEN-010, is currently in early clinical development for the treatment of patients with solid tumors, including NUT midline carcinoma. Tensha is a Focused Portfolio Company funded by HealthCare Ventures. For more information on Tensha, visit www.tenshatherapeutics.com.

SOURCE: Tensha Therapeutics