molecules of the month

ceralasertib (AZD6738)

ATR serine/threonine kinase inhibitor

oral agent in Ph. II for cancer

from mTOR-program derived hit + opt.

Clinical Cancer Research

AstraZeneca, Cambridge, UK

Chemical structure of Ceralasertib (AZD6738)
2 mins read

The AstraZeneca ATR serine/threonine kinase inhibitor, ceralasertib (AZD6738), is a potent (1 nM biochemical IC50), orally bioavailable, ATP-competitive inhibitor, and is one of the most clinically advanced sulfoximines with ~32 registered clinical studies. An indole to azaindole change was key to mitigating CYP TDI during discovery, which was important due to the number of drug combinations the molecule ended up being involved in. The molecule is broadly selective against other kinases (0/442 kinases with >50% inh. at 1 uM) likely thanks to the morpholine hinge-binding element which is a privileged motif for PI3K-like kinases. Though the structure and discovery campaign were disclosed years ago, this publication shares valuable data from its Ph. I study including human PK and its recommended Ph. II dose (40 mg QD) with…

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