ЧÀÍÈÈÏß
Ò¼ºÅÓéÀÖ¹¹½¨ÏµÁÐBa/F3-RET¹¤³Ìϸ°ûÖêÖúÁ¦RETÒÖÖÆ¼ÁÑз¢
Ðû²¼Ê±¼ä£º
2020-05-21
Ò¼ºÅÓéÀÖ Ba/F3-RET ϸ°ûÖê
Õë¶ÔRETÒÖÖÆ¼ÁÒ©Î↑·¢ÐèÇ󣬣¬£¬£¬£¬£¬£¬£¬Ò¼ºÅÓéÀÖ¹¹½¨ÏµÁÐBa/F3-RET¹¤³Ìϸ°ûÖ꣬£¬£¬£¬£¬£¬£¬£¬°üÀ¨×îз¢Ã÷µÄRET-G810R/S/CµÈÄÍÒ©Í»±ä£¬£¬£¬£¬£¬£¬£¬£¬ÓÃÓÚÕë¶ÔRET°ÐµãµÄ»¯ºÏÎïɸѡÆÀ¼Û¼°¶¯ÎïҩЧÆÀ¼Û£¬£¬£¬£¬£¬£¬£¬£¬½Ó´ý´¹Ñ¯¡£¡£¡£¡£¡£¡£¡£
ϸ°ûÖêÁбíÈçÏ£º

01 RETÏà¹ØÐźÅͨ·
RET(rearranged during transfection)ÊÇÒ»¸öÔ°©»ùÒò£¬£¬£¬£¬£¬£¬£¬£¬Î»ÓÚ10ºÅȾɫÌ峤±Û£¬£¬£¬£¬£¬£¬£¬£¬±àÂëÒ»ÖÖÊÜÌåÀÒ°±Ëἤø(RTK)¡£¡£¡£¡£¡£¡£¡£Í¨³££¬£¬£¬£¬£¬£¬£¬£¬½ºÖÊϸ°ûÔ´ÐÔÉñı»®ÑøÒò×Ó(Glial cell-line derived neurotrophic factor, GDNF)Ê×ÏÈÓëGFR¦Á1Á¬ÏµÐγÉGDNF-GFR¦Á1¸´ºÏÎ£¬£¬£¬£¬£¬£¬£¬¸Ã¸´ºÏÎïÔÙÓëRETÁ¬ÏµÐγÉÈý¾ÛÌ帴ºÏÎ£¬£¬£¬£¬£¬£¬£¬µ¼ÖÂRETµÄ¶þ¾Û»¯£¬£¬£¬£¬£¬£¬£¬£¬½øÒ»²½ÒýÆðÀÒ°±Ëá²Ð»ù×ÔÁ×Ëữ£¬£¬£¬£¬£¬£¬£¬£¬´Ó¶ø¼¤»îÏÂÓÎÐźÅͨ·¡£¡£¡£¡£¡£¡£¡£RETÏÂÓÎÏà¹ØÐźÅͨ·Ö÷Òª°üÀ¨RAS-MAPKºÍPI3K¨CAKTµÈ¡£¡£¡£¡£¡£¡£¡£

02 RET°ÐµãÓëÏà¹Ø°©Ö¢
RET»ùÒòÒì³£»£»£»£»£»£»î»¯Ö÷Òª°üÀ¨»ùÒòÈںϡ¢µãÍ»±ä¡¢¹ý±í´ïÈýÖÖ»úÖÆ£¬£¬£¬£¬£¬£¬£¬£¬¿Éµ¼Ö¶àÖÖ°©Ö¢¡£¡£¡£¡£¡£¡£¡£RET»ùÒòµãÍ»±äÔÚ¼××´ÏÙËèÑù°©(MTC)Öеı¬·¢ÂÊԼΪ60%-90%£¬£¬£¬£¬£¬£¬£¬£¬ÆäÖÐ×î³£¼ûµÄÍ»±äλµãÊÇM918T¡£¡£¡£¡£¡£¡£¡£RET»ùÒòÈÚºÏÔÚ¼××´ÏÙÈéÍ·×´°©(PTC)Öб¬·¢ÂÊΪ10%-20%;ÔÚ·ÇСϸ°û·ÎÏÙ°©»¼ÕßÖеı¬·¢ÂÊԼΪ1-2%£¬£¬£¬£¬£¬£¬£¬£¬ÆäÖÐÒÔKIF5B-RET×îΪ¶à¼û¡£¡£¡£¡£¡£¡£¡£

03 RET ÒÖÖÆ¼ÁÑз¢Ã÷×´
ÏÖÔÚ¹ØÓÚRET»ùÒò¸Ä±äÀàÖ×ÁöµÄÖÎÁƼƻ®Ö÷ÒªÊÇʹÓöà°Ðµã¼¤Ã¸ÒÖÖÆ¼ÁÀàÒ©Î£¬£¬£¬£¬£¬£¬£¬ºÃ±È¿¨²©ÌæÄá¡¢·²µÂËûÄᣬ£¬£¬£¬£¬£¬£¬£¬ÕâЩҩÎï²»µ«ÒÖÖÆRETÂѰף¬£¬£¬£¬£¬£¬£¬£¬Í¬Ê±»áÒÖÖÆVEGFR¡¢EGFRµÈÆäËûÂѰס£¡£¡£¡£¡£¡£¡£2020Äê5ÔÂ8ÈÕ£¬£¬£¬£¬£¬£¬£¬£¬FDA¼ÓËÙÅú×¼ÁËÈ«ÇòÊ׸ö¸ßÑ¡ÔñÐÔRET¼¤Ã¸ÒÖÖÆ¼ÁLOXO-292 (selpercatinib £¬£¬£¬£¬£¬£¬£¬£¬ÀñÀ´)£¬£¬£¬£¬£¬£¬£¬£¬ºÍÆäËû°ÐÏòÒ©Ò»Ñù£¬£¬£¬£¬£¬£¬£¬£¬LOXO-292Ò²»áÄÍÒ©¡£¡£¡£¡£¡£¡£¡£ÁÙ´²Ç°Ñо¿ÏÔʾ£¬£¬£¬£¬£¬£¬£¬£¬RETÈÚºÏNSCLC»¼ÕßʹÓÃLOXO-292ÖÎÁƺ󣬣¬£¬£¬£¬£¬£¬£¬¿É±¬·¢G810R/S/CÈܼÁÇ°ÑØÍ»±ä£¬£¬£¬£¬£¬£¬£¬£¬µ¼ÖÂLOXO-292ÄÍÒ©¡£¡£¡£¡£¡£¡£¡£
ÓÉTurning Point Therapeutics¹«Ë¾¿ª·¢µÄС·Ö×ÓÖÆ¼ÁTPX-0046µÄÁÙ´²Ç°Ñо¿Ð§¹ûÏÔʾÆä¶ÔRET-G810R/SÍ»±ä½ÏΪÃô¸Ð£¬£¬£¬£¬£¬£¬£¬£¬ÒÑ¿ªÕ¹Ò»ÆÚÁÙ´²ÊµÑ飬£¬£¬£¬£¬£¬£¬£¬ÁíÒ»¿î¿ª·¢ËÙÂʽϿìµÄRETÒÖÖÆ¼ÁBLU-667 (pralsetinib £¬£¬£¬£¬£¬£¬£¬£¬Blueprint¹«Ë¾)ÒÑÏòFDAÌá½»ÁËÉÏÊÐÉêÇë¡£¡£¡£¡£¡£¡£¡£
04 ²¿·Öϸ°ûÑéÖ¤Êý¾Ý
1)Ba/F3-KIF5B-RETÑéÖ¤Êý¾Ý

2)Ba/F3-KIF5B-RET-V804MÑéÖ¤Êý¾Ý

3)Ba/F3-KIF5B-RET-V804LÑéÖ¤Êý¾Ý

4)Ba/F3-KIF5B-RET-G810RÑéÖ¤Êý¾Ý

5)Ba/F3-KIF5B-RET-G810SÑéÖ¤Êý¾Ý

6)Ba/F3-KIF5B-RET-G810CÑéÖ¤Êý¾Ý

ͼƬȪԴ¼Î¿½å¼ÎÄÏ×£º
¡¾1¡¿Advances in Targeting RET-Dependent Cancers. Cancer Discov. ,2020,10:498¨C505.
¡¾2¡¿RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies. J.Thorac. Oncol.;2020, 15:541-549.
Ò¼ºÅÓéÀÖ¹«ÖÚºÅ
Á¢ÒìÒ©ÎïÆÀ¼Û
ÖпÆÒ½ÂöС³ÌÐò
µç»°£º4006 0551 06£¨¹Ù·½ÈÈÏߣ©
0551—67129201£¨¹«Ë¾×ܲ¿£©
꿅᣼www.precedo.cn
µØµã£ººÏ·ÊÊиßÐÂÇøÏ°ÓÑ·¹ú¼Ò¿µ½¡´óÊý¾Ý¹¤ÒµÔ°A6¶°
Copyright © 2021 Ò¼ºÅÓéÀÖ °æÈ¨ËùÓÐ | SEO±êÇ©
ÍøÕ¾½¨É裺ÖÐÆó¶¯Á¦ ºÏ·Ê