US-based Tensha Therapeutics has initiated the first clinical study of TEN-010, a bromodomain and extra-terminal domain (BET) bromodomain inhibitor, for cancer treatment.
This clinical study has been designed to evaluate the safety, tolerability and anti-tumour activity of the TEN-010 in patients with advanced solid tumours that are refractory or intolerant to standard/approved therapies and NUT midline carcinoma (NMC).
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.
Tensha chief medical officer Dr Steven Landau said: "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."
Bromodomain-containing proteins are a class of epigenetic regulators that can influence gene expression once they are bound to chromatin.
Bromodomains play important roles in influencing gene transcription by functioning as readers of epigenetic marks.
Tensha founder Dr James Bradner has recognised the broad potential of small molecule BET bromodomain inhibitors across a range of therapeutic areas. He has identified NMC as sensitive to BET bromodomain inhibition.
Subsequent studies from Dr Bradner and collaborating laboratories have established BET bromodomain inhibition as a therapeutic strategy to target Myc overexpression and showed the potential of this approach to other cancers that include multiple myeloma, acute myeloid leukemia, non-small cell lung cancer and neuroblastoma.
"Tensha is now poised to test TEN-010’s ability to deliver clinically on the promise that we saw in our preclinical experiments," Dr Bradner said.
Image: Micrograph of a NUT midline carcinoma. Photo: courtesy of Nephron.