GDC-0941 + fulvestrant

**GDC-0941 + fulvestrant** is a combination therapy investigated for advanced and metastatic breast cancer, specifically in patients who are estrogen receptor (ER) positive and HER2 negative and whose disease has progressed after aromatase inhibitor treatment[1][5][6]. GDC-0941 (pictilisib) is an orally bioavailable, selective inhibitor of class I phosphoinositide 3-kinase (PI3K), targeting the PI3K/AKT/mTOR signaling pathway that is often activated in cancers[2][3]. Fulvestrant is a selective estrogen receptor degrader (SERD) that blocks and degrades the estrogen receptor, reducing estrogen-driven cancer cell proliferation. The rationale for the combination is to simultaneously block estrogen signaling and PI3K pathway activation, which can be synergistic in ER+ breast cancer with acquired resistance to endocrine therapy, particularly in tumors with *PIK3CA* mutations[3].

Other names

pictilisib + fulvestrant