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PIK3CA Mutations

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Patients with PIK3CA mutations and/or PTEN aberrations treated with PI3K/Akt/mTOR inhibitors had a higher clinical response rate (18%) compared with wild-type (WT) PIK3CA patients (6%).
Damodaran et al. 2022 J Clin Oncol 40: 1552-1561

However, initial clinical efforts targeting PIK3CA mutations yielded mixed results because of the lack of isoform specificity of inhibitors and poor therapeutic index.
Damodaran et al. 2022 J Clin Oncol 40: 1552-1561

Copanlisib had mean IC50 values of 19 nM against cell lines with PIK3CA-activa…