Avutometinib

Avutometinib(RO5126766,CH5126766,VS 6766, CKI-27, R-7304, RG-7304)是一种双重RAF/MEK抑制剂，对BRAF V600E，BRAF，CRAF，和 MEK1的IC50分别为8.2 nM，19 nM，56 nM，和160 nM。

1、CAS号：946128-88-7

2、分子量：471.46

3、用法用量：Avutometinib 单药时，每周吃两天（例如，周一/周四、周二/周五），每天吃4毫克；吃三周停一周。Avutometinib联药治疗时，每周吃两天（例如，周一/周四、周二/周五），每天吃3.2毫克；吃三周停一周。（“Avutometinib Monotherapy Dosing: Avutometinib 4.0 mg PO 2x/wk 21/28 days.”“Avutometinib + Defactinib Dosing: Avutometinib 3.2 mg PO 2x/wk 21/28 days + Defactinib 200 mg PO BID: 21/28 days.”“Avutometinib will be dosed at 3.2 mg orally taken twice weekly (eg, Monday/Thursday, Tuesday/Friday) for 3 weeks (21 days) followed by 1 week (7 days) off treatment, in a 4 week cycle.”见《Initial eicacy and safety results from ENGOT-ov60/GOG-3052/RAMP 201: A phase 2 study of avutometinib (VS-6766) ± defactinib in recurrent low-grade serous ovarian cancer (LGSOC)》、《GOG-3097/ENGOT-ov81/GTG-UK/RAMP 301: a phase 3, randomized trial evaluating avutometinib plus defactinib compared with investigator’s choice of treatment in patients with recurrent low grade serous ovarian cancer》）

4、常见副作用：恶心呕吐、腹泻、cpk升高、皮炎皮疹、视力模糊、外周水肿、疲劳贫血