±±¾©Ê¯ÓÍ»¯¹¤Ñ§Ôº2026ÄêÑо¿ÉúÕÐÉú½ÓÊÕµ÷¼Á¹«¸æ
²é¿´: 4391  |  »Ø¸´: 15
µ±Ç°Ö»ÏÔʾÂú×ãÖ¸¶¨Ìõ¼þµÄ»ØÌû£¬µã»÷ÕâÀï²é¿´±¾»°ÌâµÄËùÓлØÌû

³ÕÃÎäìÏæ

ľ³æ (ÖøÃûдÊÖ)


[½»Á÷] Õý´óÌìÇç3000ÍòÃÀÔªÂòÈëÒ»¸öÁÙ´²Ç°¿¹HCVÒ©ÎïÔÚÖйúµØÇøµÄÐí¿É£¬Ìì¼Û? ÒÑÓÐ12È˲ÎÓë

2013Äê6Ô£¬½­ËÕÕý´óÌìÇç3000ÍòÃÀÔª»ñµÃBL-8030ÔÚÖйúºÍÏã¸ÛµÄÐí¿É¡£
http://www.biolinerx.com/default.asp?pageid=16&itemid=198

NS3/4Aµ°°×øÒÖÖÆ¼Á£ºBL-8030£¨ÁÙ´²Ç°£©
Ñз¢µ¥Î»£ºBioLineRx Ltd.
»¯ºÏÎï½á¹¹£ºÎ´¹«¿ª
»¯ºÏÎïרÀû£ºÎ´¹«¿ª£¨2010ÄêÉêÇ룩
ÊÊÓ¦Ö¢£º±ûÐ͸ÎÑ×
×ÛºÏ×ÊÁÏ£ºBL-8030: A Novel, Potent, Selective, Orally Available Inhibitor of Hepatitis C Virus NS3/4A Protease. EASL 48th Annual Meeting, April 24th - 28th 2013
http://www.natap.org/2013/EASL/EASL_89.htm

ÌåÍâ»îÐÔ£º
£¨1£©Huh-7 cell based HCV replicon assay (qRT-PCR)£º
BL-8030¶Ô»ùÒòÐÍ1a¡¢1bµÄ»îÐÔ·Ö±ðΪ5.2nm¡¢1.64nm£¬ÑôÐÔ¶ÔÕÕtelaprevirµÄ»îÐÔ·Ö±ðΪ10nm¡¢240nM£»
BL-8030¶Ô»ùÒòÐÍ2aµÄ»îÐÔΪ168.25nm£¬ÑôÐÔ¶ÔÕÕboceprevirµÄ»îÐÔΪ217.35nm¡£
£¨2£©wild type and PI mutant enzymes£º
¶ÔÓÚ»ùÒòÐÍ1a£¬BL-8030¡¢telaprevir¡¢TMC-435µÄ»îÐÔ·Ö±ðΪ1.32nm¡¢111nm¡¢1.52nm£¬BL-8030¶ÔÓÚ1a¡¢1b¡¢2a¡¢3a¡¢4dµÄ»îÐÔ·Ö±ðΪ1.32nm¡¢1.00nm¡¢4.36nm¡¢158nm¡¢10.59nm£¬ÆäËû»îÐÔÊý¾Ý¼ûEASL2013Äê»á×ÊÁÏ£»
¶ÔÓÚ¶àÖÖ±äÒìÐ͵°°×ø£¬BL-8030µÄ»îÐÔÓëTMC-435Ï൱£¬Ô¶¸ßÓÚtelaprevir£¬¾ßÌå»îÐÔÊý¾Ý¼ûEASL2013Äê»á×ÊÁÏ£»
£¨3£©human proteases£º
BL-8030¶ÔÈ˵°°×øµÄ»îÐԺܵͣ¬ÓëvaniprevirÏ൱£¬Ñ¡ÔñÐÔÔ¶ÓÅÓÚtelaprevir£¬¾ßÌå»îÐÔÊý¾Ý¼ûEASL2013Äê»á×ÊÁÏ¡£
£¨4£©Human cytochrome P450 enzyme£º
BL-8030¶ÔÖ÷ÒªCYPÎÞÒÖÖÆ»îÐÔ¡£

PK£º
´óÊó10mg/kg¡¢100mg/kgµ¥´Î¸øÒ©¿Ú·þÉúÎïÀûÓöȷֱðΪ17.4%¡¢33.7%¡£
Liver/plasmaÒ©Îï·Ö²¼±ÈÔÚ28.4ÖÁ45.4¡£
¸øÒ©24Сʱºó£¬ÑªÒ©Å¨¶È¸ßÓÚEC50£¬Ö§³ÖÿÌì¿Ú·þÒ»´Î¡£

µãÆÀ£ºBL-8030Êǵڶþ´úHCVµ°°×øÒÖÖÆ¼Á£¬Æä»îÐÔºÍÑ¡ÔñÐÔÊDz»±ØËµµÄ£¬Ô¶ÓÅÓÚÒÑÉÏÊеÄtelaprevir¡£BL-8030µÄÁÁµãÊÇ£¨1£©Äܹ»¶Ô¿¹¸÷ÖÖÄÍÒ©Í»±ä£¨2£©¿ÉÒÔ¿Ú·þÇÒÿÌìÖ»Ðè¿Ú·þÒ»´Î£¨3£©Liver/plasma±ÈÖµ¸ß£¬°²È«ÐÔÓ¦¸Ã²»´í¡£

[ Last edited by ³ÕÃÎäìÏæ on 2013-6-12 at 21:48 ]
»Ø¸´´ËÂ¥
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû

fw8505

½ð³æ (ÕýʽдÊÖ)

¡ï ¡ï
Сľ³æ: ½ð±Ò+0.5, ¸ø¸öºì°ü£¬Ð»Ð»»ØÌû
ºÓ±ßµÄ«έ: ½ð±Ò+1, ¸ÐлÄãµÄ»ØÌû½»Á÷~ 2013-07-02 15:08:40
ÒýÓûØÌû:
5Â¥: Originally posted by iamzane at 2013-06-13 08:52:13
HCV¹úÄÚ¸ºµ£ÈçºÎ£¿...

ÖªÃûµ÷Ñй«Ë¾Decision Resources×îб¨¸æÏÔʾ£¬ÖйúµÄ±ûÐ͸ÎÑ×£¨HCV£©Êг¡ÓÐÍû½«´Ó2010ÄêµÄ1.37ÒÚÔªÔö³¤ÖÁ2015ÄêµÄ2.47Ôª¡£ÖйúÅÓ´óµÄHCV»¼ÕßȺÌå¡¢Õþ¸®Ö÷µ¼È«ÃñÒ½±£µÄÍÆ½ø¡¢¸ß°ºµÄHCVÖÎÁÆ·ÑÓÃÄÉÈëÒ½±£±¨ÏúÊǸÃÊг¡³ÖÐøÔö³¤µÄÔ´¶¯Á¦¡£

Decision Resources¹«Ë¾µÄ·ÖÎöʦJing WuÖ¸³ö£¬ÖйúµÄHCV»¼ÕßÈËÊýλ¾ÓÊÀ½çµÚÒ»£¬ÊÇÆäËûÆß¸öÖ÷ÒªÒ½Ò©Êг¡HCV¸ÐȾÕßÈËÊý×ܺ͵ÄÎå±¶¶à¡£ÔÚÖйú£¬Ä¿Ç°HCV»¼ÕߵĩÕïÂʷdz£¸ß£¬Decision ResourcesÔ¤¼Æ£¬Ò»µ©Õï¶ÏÂÊС·ùÔö¼Ó£¬½«µ¼ÖÂÕûÌåµÄÒ©ÎïÖÎÁÆ»¼ÕßÊýÄ¿´óÔö¡£

±¨¸æÍ¬ÑùÏÔʾ£¬¾¡¹Ü¾ÛÒÒ¶þ´¼-¸ÉÈÅËØ-¦ÁÖÆ¼Á¡ª¡ªÂÞÊϹ«Ë¾µÄPegasysºÍĬ¿Ë¹«Ë¾µÄPegIntron£¬±»¡¶Öйú±ûÐ͸ÎÑ×·ÀÖÎÖ¸ÄÏ¡·ÍƼöΪһÏßÓÃÒ©£¬µ«°º¹óµÄÖÎÁƳɱ¾ÏÞÖÆÁËËüÃǵÄÁÙ´²Ó¦Ó᣾ÛÒÒ¶þ´¼-¸ÉÈÅËØ-¦ÁÖÆ¼ÁÒѾ­ÈëÑ¡2009°æ¹ú¼ÒÒ½±£Ä¿Â¼£¬²¢ÇÒ¸÷¸öµØÇø±¨Ïú±ÈÀýÓÐËù²»Í¬£¬·¶Î§´Ó50%~90%¡£

·ÖÎöʦJing WuÖ¸³ö£¬¾ÛÒÒ¶þ´¼-¸ÉÈÅËØ-¦ÁÖÆ¼ÁÖÎÁÆ·ÑÓõIJ¿·Ö±¨Ïú£¬½«Ê¹Äܸºµ£Æð·ÑÓõϼÕßÈËȺÀ©´ó£¬ÓÈÆäÊdzÇÊÐÈËȺ¡£µ«ÊÇ£¬±¨ÏúÖ®ÍâµÄ×Ô·Ñ·ÑÓã¬ÈÔÈ»ÊÇ»¼Õß³ÁÖØµÄ¾­¼Ã¸ºµ££¬´ËÍ⣬ĿǰÈÔÓг¬¹ýÈý·ÖÖ®Ò»µÄ³ÇÊÐÈË¿ÚûÓб»Õþ¸®Ö÷µ¼µÄÈ«ÃñÒ½±£¼Æ»®Ëù¸²¸Ç¡£
10Â¥2013-06-14 08:32:11
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
²é¿´È«²¿ 16 ¸ö»Ø´ð

youngtcm

½û³æ (³õÈëÎÄ̳)

¡ï
Сľ³æ: ½ð±Ò+0.5, ¸ø¸öºì°ü£¬Ð»Ð»»ØÌû
±¾ÌûÄÚÈݱ»ÆÁ±Î

2Â¥2013-06-13 08:17:38
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû

youngtcm

½û³æ (³õÈëÎÄ̳)

¡ï
ºÓ±ßµÄ«έ: ½ð±Ò+1, ¸ÐлÄãµÄ»ØÌû½»Á÷~ 2013-07-02 15:07:55
ºÓ±ßµÄ«έ: »ØÌûÖö¥ 2013-07-02 15:08:06
±¾ÌûÄÚÈݱ»ÆÁ±Î

3Â¥2013-06-13 08:18:10
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû

fw8505

½ð³æ (ÕýʽдÊÖ)

¡ï
Сľ³æ: ½ð±Ò+0.5, ¸ø¸öºì°ü£¬Ð»Ð»»ØÌû
ΪÂïÊÇ¿¹±û¸ÎµÄ£¬ÒÒ¸Î×ö±¥ºÍÁË£¿
4Â¥2013-06-13 08:22:22
ÒÑÔÄ   »Ø¸´´ËÂ¥   ¹Ø×¢TA ¸øTA·¢ÏûÏ¢ ËÍTAºì»¨ TAµÄ»ØÌû
×î¾ßÈËÆøÈÈÌûÍÆ¼ö [²é¿´È«²¿] ×÷Õß »Ø/¿´ ×îºó·¢±í
[¿¼ÑÐ] 346Çóµ÷¼Á Ò»Ö¾Ô¸070303Óлú»¯Ñ§ +4 Âܲ·ìÀÇà²Ë 2026-03-28 4/200 2026-03-30 13:42 by Iveryant
[¿¼ÑÐ] 292Çóµ÷¼Á +9 ÊÇåû×ÓÒ²ÊÇÑÐ×Ó 2026-03-30 9/450 2026-03-30 13:34 by chemdavid
[¿¼ÑÐ] ²ÄÁϹ¤³Ìר˶Çóµ÷¼Á +6 hyl3153942 2026-03-29 6/300 2026-03-30 12:04 by 1018329917
[˶²©¼ÒÔ°] Çóµ÷¼Á Óлú»¯Ñ§¿¼ÑÐ356·Ö +10 Nadiums 2026-03-25 11/550 2026-03-30 11:56 by yjolah
[¿¼ÑÐ] 297Çóµ÷¼Á +13 ÌïºéÓÐ 2026-03-26 13/650 2026-03-30 11:33 by Ìæ´úÆ·000
[ÂÛÎÄͶ¸å] arxiv±³ÊéÈËÓʼþÇóÖú 20+3 redcom 2026-03-25 7/350 2026-03-30 10:56 by bobvan
[¿¼ÑÐ] Ò»Ö¾Ô¸»ª¶«Ê¦·¶´óѧÓлú»¯Ñ§×¨Òµ£¬³õÊÔ351·Ö£¬¸´ÊÔ±»Ë¢Çóµ÷¼Á! +5 ÕæÃûÓбù 2026-03-29 6/300 2026-03-29 20:53 by ÌÆãå¶ù
[¿¼ÑÐ] 343Çóµ÷¼Á +6 °®î¿°í 2026-03-29 6/300 2026-03-29 12:00 by Î޼ʵIJÝÔ­
[¿¼ÑÐ] 2026Ä껪ÄÏʦ·¶´óѧ»¶Ó­»¯Ñ§£¬»¯¹¤£¬ÉúÎÉúÒ½¹¤µÈרҵÓÅÐãѧ×Ó¼ÓÈ룡 +3 llss0711 2026-03-28 6/300 2026-03-29 10:26 by llss0711
[¿¼ÑÐ] 081200-11408-276ѧ˶Çóµ÷¼Á +6 ´Þwj 2026-03-26 6/300 2026-03-29 01:11 by hanserlol
[¿¼²©] 26É격 +3 ¼ÓÓͳ尡£¡ 2026-03-26 3/150 2026-03-27 15:38 by cls512
[¿¼ÑÐ] 085600£¬²ÄÁÏÓ뻯¹¤321·Ö£¬Çóµ÷¼Á +9 ´ó²öС×Ó 2026-03-27 9/450 2026-03-27 14:30 by mmm just
[¿¼ÑÐ] 305Çóµ÷¼Á +5 ÍÛ¬¿¨¿â 2026-03-26 5/250 2026-03-27 14:01 by laoshidan
[¿¼ÑÐ] 316Çóµ÷¼Á +5 Pigcasso 2026-03-24 5/250 2026-03-27 12:10 by zhshch
[˶²©¼ÒÔ°] ±±¾©ÁÖÒµ´óѧ˶µ¼ÕÐÉú¹ã¸æ +6 kongweilin 2026-03-26 8/400 2026-03-27 10:18 by FF_16
[¿¼ÑÐ] 07»¯Ñ§303Çóµ÷¼Á +5 î£08 2026-03-25 5/250 2026-03-25 22:46 by 418490947
[¿¼ÑÐ] 285Çóµ÷¼Á +3 AZMK 2026-03-24 3/150 2026-03-25 12:23 by userper
[¿¼ÑÐ] 292Çóµ÷¼Á +4 ¶ì¶ì¶ì¶î¶î¶î¶î¶ 2026-03-24 4/200 2026-03-24 16:41 by peike
[¿¼ÑÐ] 085404µç×ÓÐÅÏ¢284·ÖÇóµ÷¼Á +4 13659058978 2026-03-24 4/200 2026-03-24 12:15 by syl20081243
[¿¼ÑÐ] 284Çóµ÷¼Á +3 yanzhixue111 2026-03-23 6/300 2026-03-23 22:58 by pswait
ÐÅÏ¢Ìáʾ
ÇëÌî´¦ÀíÒâ¼û