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Pictilisib + erlotinib is a combination of two small molecule inhibitors developed for cancer therapy. **Pictilisib** (GDC-0941) is an oral, selective class I pan-phosphatidylinositol 3-kinase (PI3K) inhibitor, blocking the PI3K/AKT signaling pathway involved in cell proliferation and survival. **Erlotinib** is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that blocks EGFR/ERBB1, critical for tumor growth in various cancers. The rationale behind combining these two drugs is to achieve dual inhibition of two key oncogenic signaling pathways, especially in solid tumors harboring dysregulation of PI3K and/or EGFR. In clinical studies, the combination was evaluated for safety, tolerability, and early efficacy signals in patients with advanced solid tumors, but showed notable toxicity and limited anti-tumor activity.
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