Serine/threonine protein kinase (AKT, also known as PKB)
Oral, allosteric sub-type specific selective inhibitor of AKT (AKT 1/2).
Akt/PKB is a critical signalling molecule that promotes cell growth and survival pathways in many tumour types. It is often dysregulated in many cancers and although importantly modulated through PI3K pathway it is also possible to get PI3K independent activation of Akt suggesting inhibition of Akt directly rather than PI3K could be a more effective therapeutic option. An allosteric inhibitor to Akt as compared to an ATP site inhibitor has the advantage that the pathway is not hyperactived.
ALM301 is an allosteric AKT1/2 inhibitor with IC50 of <5 nM and no significant off-targeting activity against a panel of >50 kinases. Consistent with its mechanism of action, ALM301 reduces cellular levels of phosphorylated Thr-308, Ser-473 and downstream effectors both in vitro and in vivo. Pre-clinical studies have also confirmed that ALM301 significantly reduces cell growth in a variety of cell lines and exhibits strong tumour growth regression in multiple human xenograft tumour models.
Alternative Akt specific inhibitors of other isoforms are also available
ALM301 has an excellent safety profile, has successfully completed pre-clinical development and is fully Phase I ready for a global best-in-class partnering opportunity. It is being positioned for clinical development in Oesophageal-gastric cancer along with a parallel biomarker strategy.
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