PKI166

PKI166 is a **synthetic small molecule**, specifically a pyrrolo-pyrimidine compound, that functions as a **reversible inhibitor of the epidermal growth factor receptor (EGFR/HER1) and ErbB2 (HER2) tyrosine kinases**[3][6][7]. It was developed as a targeted antineoplastic agent for the treatment of various solid malignancies, including human prostate cancer and broader neoplasm indications[1][3][4][6]. This agent works by competitively inhibiting ATP binding to the tyrosine kinase domain of EGFR, leading to reduced receptor autophosphorylation, blockade of downstream signaling, induction of smooth muscle cell apoptosis, and inhibition of tumor cell proliferation and growth[2][3][6][7]. PKI166 was developed by Novartis and advanced to clinical trials but **development was discontinued** after Phase I/II studies, and it is not marketed for any condition[3][5][7].

Other names

PKI 166PKI166PKI-166CGP 75166CGP75166CGP-75166NVP-PKI166NVP-PKI-166NVP-PKI 166