20161009子宫内膜癌分子分型与靶向治疗10-08.ppt

5.PI3K抑制剂1)已上市药物：无研发阶段药物：Buparlisib（NVP-BKM120），Pilaralisib（XL147）2)作用靶点：选择性PI3K抑制剂，作用于PI3Kα/δ/γ等3)临床进展：2个II期临床试验完成，BKM120因药物毒性过大而终止，Pilaralisib有效率仅为6%6.PI3K/mTOR双重抑制剂1)已上市药物：无研发阶段药物：Apitolisib（GDC0980）2)作用靶点：I型PI3K抑制剂，作用于PI3Kα/β/δ/γ；同时为mTOR抑制剂3)临床进展：2个II期临床试验完成.PI3K/mTOR抑制剂——apitolisib?Amulticenter,single-arm,open-label,?phase?2?study?ofapitolisib(GDC-0980)forthetreatmentofrecurrentorpersistent?endometrial?carcinomaCancer.?2016Sep7All56patientsdiscontinuedthestudydrug.Reasonsfordiscontinuationwerediseaseprogression(24patients;43%),adverseevents(13patients;23%),andwithdrawalbysubject(12patients;21%).?ThemedianPFSwas3.5monthsandthemedianoverallsurvivalwas15.7months.MakkerV,?RecioFO,?MaL,?MatulonisUA,?LauchleJO,?ParmarH,?GilbertHN,?WareJA,?ZhuR,?LuS6,?HuwLY,?WangY,?KoeppenH,SpoerkeJM,?LacknerMR,?AghajanianCA.Amulticenter,single-arm,open-label,?phase?2?study?ofapitolisib(GDC-0980)forthetreatmentofrecurrentorpersistent?endometrial?carcinoma(MAGGIE?study).Cancer.?2016Sep7PI3K/mTOR双重抑制剂

——PFandgedatolisib?Arandomized?phase?II?non-comparative?study?ofPFandgedatolisib(PFinpatientswithrecurrent?endometrialcancer.GynecolOncol.?2016JulClinical?benefitresponserateMedianPFSgedatolisib/stathmin*-low53%(10/19)112daysgedatolisib/stathmin-high?26%(5/19)89daysThemedianPFSwas3.5monthsandthemedianoverallsurvivalwas15.7months.DelCampoJM,?BirrerM,?DavisC,?FujiwaraK,?GollerkeriA,?GoreM,?HoukB,?LauS,?PovedaA,?González-MartínA,?MullerC,?MuroK,?PierceK,?SuzukiM,?VermetteJ,?OzaA.Arandomized?phase?II?non-comparative?study?ofPFandgedatolisib(PFinpatientswithrecurrent?endometrialcancer.GynecolOncol.2016Jul;1