ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC 50 of 5.0 nM for Bruton tyrosine kinase ( BTK ) . ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8 . Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor , with an IC 50 of 3 nM and EC 50 of 8 nM.
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