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PIK3CA突变是编码PI3K亚基p110a的基因发生突变,被认为与激素受体阳性乳腺癌的抗雌激素治疗耐药相关。而产生抗雌激素耐药的患者仍对来曲唑治疗有效,这提示我们治疗ER阳性/PI3K发生突变的乳腺癌药物包括PI3K抑制剂和抗雌激素药物。BKM120是PI3K亚型1的口服可逆抑制剂,在单独使用或联合内分泌治疗中都表现出抗肿瘤生长活性。2012年美国ASCO大会公布了一项在绝经后ER阳性的转移性乳腺癌患者中联合应用来曲唑和pan-PI3K抑
The PIK3CA mutation, a gene encoding the PI3K subunit p110a, is mutated and is believed to be associated with resistance to antiestrogen therapy of hormone receptor-positive breast cancer. While anti-estrogen-resistant patients are still effective letrozole therapy, suggesting that we treat ER-positive / PI3K mutations in breast cancer drugs, including PI3K inhibitors and anti-estrogen drugs. BKM120 is an orally reversible inhibitor of PI3K subtype 1 and exhibits anti-tumor growth activity either alone or in combination with endocrine therapy. 2012 ASCO Conference announced a combination of letrozole and pan-PI3K in patients with post-menopausal ER-positive metastatic breast cancer