12:00 AM
Jun 09, 2014
 |  BioCentury  |  Emerging Company Profile

Glactone: ProSTATe stopper

Glactone's covalent STAT3 inhibitor arrests castration-resistant prostate cancer

Glactone Pharma AB is developing small molecule inhibitors of a mitogenic transcription factor that is overactive in castration-resistant prostate cancer and other solid tumors. The company has mechanistic evidence that its derivatives of the fungal metabolite galiellalactone directly and irreversibly block the activity of STAT3, and could be more bioavailable and better tolerated than more advanced compounds going after the target.

STAT3 (signal transducer and activator of transcription 3) is on the receiving end of the JAK/STAT signaling pathway, which is constitutively active in many cancers as well as autoimmune and inflammatory indications. STAT3 is usually dormant in the cytosol, but when activated by phosphorylation, it enters the nucleus to turn on transcription of mitogenic and pro-inflammatory genes.

Efforts to hit the pathway have focused on inhibiting Janus kinases (JAKs), which phosphorylate STAT proteins in response to cytokines. For example, Novartis AG and Incyte Corp. market Jakafi ruxolitinib, a dual inhibitor of JAK-1 and JAK-2 to treat hematological malignancies. Jakafi is in Phase...

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