Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000017)
Formula
SVG example
Amide Hydrolysis; Oxidation
Reactant ACP-5862 Product Acalabrutinib M2 metabolite
Reactant Info Product Info
Metabolic Type Oxidation - Amide Hydrolysis; Oxidation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Produce The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000023 Acalabrutinib ACP-5862 Oxidation - Oxidation Acalabrutinib [1], [2], [3]
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000019 ACP-5862 Acalabrutinib M16 metabolite Reduction - Reduction Acalabrutinib [1]
MR000018 ACP-5862 Acalabrutinib M3 metabolite Oxidation - N-Dealkylation; Oxidation Acalabrutinib [1]
Other MR(s) Related to The Product of This MR
Other MR(s) That Produce The Product of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000024 Acalabrutinib Acalabrutinib M2 metabolite Oxidation - Amide Hydrolysis; Oxidation Acalabrutinib [1]
References
1 Bioavailability, Biotransformation, and Excretion of the Covalent Bruton Tyrosine Kinase Inhibitor Acalabrutinib in Rats, Dogs, and Humans Drug Metab Dispos. 2019 Feb;47(2):145-154. doi: 10.1124/dmd.118.084459.
2 Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors?. J Pharmacol Exp Ther. 2023 Jan;384(1):173-186. doi: 10.1124/jpet.122.001116.
3 Bioequivalence and Relative Bioavailability Studies to Assess a New Acalabrutinib Formulation That Enables Coadministration With Proton-Pump Inhibitors. Clin Pharmacol Drug Dev. 2022 Nov;11(11):1294-1307. doi: 10.1002/cpdd.1153.

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