COPANLISIB HCl

Description: copanlisib (formerly BAY 80-6946; brand name: Aliqopa) is a potent pan-class I PI3K (phosphoinositide 3-kinase) with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kalpha/beta/gamma/delta, respectively. In 2017, copanlisib was approved by FDA to treat adults with relapsed follicular lymphoma. BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity, which inhibits proliferation with IC50 of 147 nM in HuCCT-1 (KRASG12D ) and 137 nM in EGI-1 (KRASG12D ) cell lines. BAY 80-6946 is generally well tolerated through the maximum tolerated dose (MTD) of 0.8 mg/kg. pharmacokinetics (PK) results support dosing weekly. Grade 2 or 3 hyperglycemia in the first 24 hrs after receiving a MTD dose. Pharmacokinetics, clinical SD as well as FDG-PET data are consistent with effective exposure and PI3K pathway inhibition.

References: Mol Cancer Ther. 2013 Nov; 12(11):2319-30; Breast Cancer Res Treat. 2015 Jan; 149(2):373-83.

Related CAS #: 1402152-13-9 (HCl); 1032568-63-0 (free base); 1402152-46-8 (HCl hydrate)