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348 Warning: mysql_real_escape_string(): Access denied for user 'et1ssh96'@'localhost' (using password: NO) in /service/web/biospcmbl/comlib/dblib.php on line 30 Warning: mysql_real_escape_string(): A link to the server could not be established in /service/web/biospcmbl/comlib/dblib.php on line 30 Warning: mysql_query(): Access denied for user 'et1ssh96'@'localhost' (using password: NO) in /service/web/biospcmbl/comlib/dblib.php on line 530 Warning: mysql_query(): A link to the server could not be established in /service/web/biospcmbl/comlib/dblib.php on line 530 Warning: mysql_fetch_array() expects parameter 1 to be resource, boolean given in /service/web/biospcmbl/comlib/dblib.php on line 531 크리스탈지노믹스 FLT3/BTK 저해제, "기존 약물 대비 효과↑" - 바이오스펙테이터

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크리스탈지노믹스 FLT3/BTK 저해제, "기존 약물 대비 효과↑"

입력 2018-04-19 06:28 수정 2018-09-02 13:10

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기술이전 앱토즈 바이오사이언스 2018 AACR서 발표.."in vitro 기존 약물대비 효능↑, BTK-C481S 내성 극복 가능성 확인"

크리스탈지노믹스의 pan-FLT3/pan-BTK 저해제인 ‘CG’806’의 비임상 결과가 공개됐다. 동종 계열약물과 직접 비교해 in vitro에서 CG‘806의 세포사멸 효과가 10배 더 우수하고 약물내성을 극복한다는 내용이다.

크리스탈로부터 CG‘806을 기술이전한 앱토즈 바이오사이언스(Aptose Biosciences)는 미국 시카고에서 열린 2018년 미국암학회(AACR)에서 CG‘806의 in vitro 효능과 작용기전 연구를 발표하면서 급성 골수성백혈병(AML) 치료제로서 가능성을 제시했다.

CG‘806는 세계최초로 FLT3(FMS-like tyrosine kinase 3)와 BTK(Bruton's tyrosine kinase)를 동시에 저해하는 ’first-in-class' 저분자화합물이다. 급성 골수성백혈구 환자에서 발견되는 FLT3/BTK 변이형과 정상형을 모두 억제하는 차별성을 갖는 기전으로 지난 2016년 총 3억300만달러 규모로 앱토즈 바이오사이언스에 기술수출됐다.

AACR에서 공개한 포스터를 살펴보면, CG'806은 FLT3-ITD 돌연변이가 발현된 AML 세포에서 FLT3, STAT5, ERK의 인산화를 감소시키면서 FLT3 신호전달을 억제했다. 암세포가 증식을 위해 진행하는 세포분열과정 중 G0/G1기를 차단해 세포사멸을 일으켰다. 이러한 효과는 FLT3-ITD 저해제 '퀴자티닙(quizartinib)‘ 보다 10배 더 우수한 것으로 나타났다. FLT3-ITD 돌연변이는 AML 환자의 25~30%에서 발현되며, 대부분의 AML 환자는 FLT WT이 발견된다.

▲Ba/Fe 세포에서 CG'806과 FLT3 억제제의 IC50 값 (출처: 2018 AACR 포스터 #794)

CG'806은 다른 약물과 비교했을 때 적은 농도로도 우월한 항암효과를 나타냈다. FLT3 WT이 발현된 Ba/F3 세포주에서 CG'806의 IC50 값은 11nM로 기존 약물인 퀴자티닙(1956nM), 길터리티닙(gilteritinib)(500nM), 크레놀라닙(crenolanib)(2617nM) 보다 적은 농도로 탁월한 효과를 냈다....

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