Brand and Chemical Names
- Brand name: Calquence® 1, 2
- Chemical name: 4-{8-Amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide (2Z)-2-butenedioic acid hydrate 1
- Salt form: Acalabrutinib maleate 1
- Development code: ACP-196 3
Active Metabolite
- Major active metabolite: ACP-5862 (also known as M27), which is a pyrrolidine ring-opened ketone/amide derivative that contributes to the clinical efficacy of acalabrutinib 4
- ACP-5862 is formed through CYP3A4-mediated metabolism and demonstrates potent and selective covalent BTK inhibition, with only twofold lower potency than the parent compound 4