letrozole + pilaralisib

Letrozole + pilaralisib is a combination therapy that pairs letrozole, an aromatase inhibitor, with pilaralisib (also known as XL147), a pan-class I phosphoinositide 3-kinase (PI3K) inhibitor. This combination was developed to address endocrine therapy resistance in hormone receptor-positive (HR+), HER2-negative breast cancer. The rationale behind this combination stems from the understanding that activation of the PI3K pathway can contribute to resistance to endocrine therapy in breast cancer. Letrozole works by inhibiting the aromatase enzyme, thereby reducing estrogen production, while pilaralisib targets the PI3K pathway, which is often activated in endocrine-resistant breast cancer. In clinical trials, this combination has shown an acceptable safety profile but limited efficacy in patients with HR+, HER2-negative, non-steroidal aromatase inhibitor-refractory, recurrent or metastatic breast cancer[1][3].

Other names

SAR245408SAR-245408SAR 245408