Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000022)
Formula Reactant Acalabrutinib Product ACP-5530
Reactant Info Product Info
Metabolic Type Conjugation - Glutathione Conjugation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000024 Acalabrutinib Acalabrutinib M2 metabolite Oxidation - Amide Hydrolysis; Oxidation Acalabrutinib [1]
MR000026 Acalabrutinib Acalabrutinib M25 metabolite Oxidation - Dehydration; Oxidation Acalabrutinib [1]
MR000027 Acalabrutinib Acalabrutinib M37 metabolite Oxidation - N-Dealkylation Acalabrutinib [1]
MR000025 Acalabrutinib ACP-5134 Other reaction - Hydration Acalabrutinib [1]
MR000028 Acalabrutinib ACP-5825 Oxidation - Hydroxylation Acalabrutinib [1]
MR000023 Acalabrutinib ACP-5862 Oxidation - Oxidation Acalabrutinib [1], [2], [3]
Other MR(s) Related to The Product of This MR
Other MR(s) That Metabolize The Produtc of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000015 ACP-5530 ACP-5531 Conjugation - Conjugation 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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