| Description | Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton"s tyrosine kinase (BTK). Orelabrutinib has potential antineoplastic activity. | |
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| In vitro | Orelabrutinib potently inhibits BTK enzymatic activity with an IC50 value of 1.6 nM. In KINOMEscan assay conducted in parallel at 1 μM against a panel of 456 kinases, orelabrutinib only targets BTK with > 90% inhibition while ibrutinib inhibits additional many other kinases including EGFR, TEC and BMX, demonstrating orelabrutinib's superior kinase selectivity.[2] | |
| In vivo | Orelabrutinib has a favorable PK profile with an ideal T1/2 (~1.5-4 h) and good oral bioavailability (~20-80%) as well as prolonged BTK target occupancy in preclinical PK/PD studies. The superior selectivity translates into improved safety profile and large safety window in the GLP toxicology studies in rats and dogs.[2] |
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