<\/span><\/h2>\nQu\u00e1 m\u1eabn v\u1edbi ho\u1ea1t ch\u1ea5t ho\u1eb7c v\u1edbi b\u1ea5t k\u1ef3 t\u00e1 d\u01b0\u1ee3c n\u00e0o v\u00e0 cho con b\u00fa.<\/span><\/p>\n<\/span>D\u01b0\u1ee3c l\u1ef1c h\u1ecdc<\/b><\/span><\/span><\/h2>\n\n- Niraparib l\u00e0 m\u1ed9t ch\u1ea5t \u1ee9c ch\u1ebf c\u00e1c enzym poly (ADP-ribose) polymerase (PARP), PARP-1 v\u00e0 PARP-2, c\u00f3 vai tr\u00f2 trong vi\u1ec7c s\u1eeda ch\u1eefa DNA. C\u00e1c nghi\u00ean c\u1ee9u trong \u1ed1ng nghi\u1ec7m \u0111\u00e3 ch\u1ec9 ra r\u1eb1ng \u0111\u1ed9c t\u00ednh t\u1ebf b\u00e0o do niraparib g\u00e2y ra c\u00f3 th\u1ec3 li\u00ean quan \u0111\u1ebfn vi\u1ec7c \u1ee9c ch\u1ebf ho\u1ea1t \u0111\u1ed9ng c\u1ee7a enzym PARP v\u00e0 t\u0103ng h\u00ecnh th\u00e0nh ph\u1ee9c h\u1ee3p PARP-DNA d\u1eabn \u0111\u1ebfn t\u1ed5n th\u01b0\u01a1ng DNA, apoptosis v\u00e0 ch\u1ebft t\u1ebf b\u00e0o.\u00a0<\/span><\/li>\n
- T\u0103ng \u0111\u1ed9c t\u00ednh t\u1ebf b\u00e0o do Niraparib g\u00e2y ra \u0111\u00e3 \u0111\u01b0\u1ee3c quan s\u00e1t th\u1ea5y \u1edf c\u00e1c d\u00f2ng t\u1ebf b\u00e0o kh\u1ed1i u c\u00f3 ho\u1eb7c kh\u00f4ng thi\u1ebfu h\u1ee5t BRCA1 \/ 2. Niraparib l\u00e0m gi\u1ea3m s\u1ef1 ph\u00e1t tri\u1ec3n kh\u1ed1i u trong c\u00e1c m\u00f4 h\u00ecnh xenograft chu\u1ed9t c\u1ee7a c\u00e1c d\u00f2ng t\u1ebf b\u00e0o ung th\u01b0 \u1edf ng\u01b0\u1eddi b\u1ecb thi\u1ebfu h\u1ee5t BRCA1 \/ 2 v\u00e0 trong c\u00e1c m\u00f4 h\u00ecnh kh\u1ed1i u xenograft c\u00f3 ngu\u1ed3n g\u1ed1c t\u1eeb b\u1ec7nh nh\u00e2n v\u1edbi s\u1ef1 thi\u1ebfu h\u1ee5t t\u00e1i t\u1ed5 h\u1ee3p t\u01b0\u01a1ng \u0111\u1ed3ng c\u00f3 BRCA1 \/ 2 \u0111\u1ed9t bi\u1ebfn ho\u1eb7c ki\u1ec3u hoang d\u00e3.<\/span><\/li>\n<\/ul>\n
<\/span>D\u01b0\u1ee3c \u0111\u1ed9ng h\u1ecdc<\/b><\/span><\/span><\/h2>\n<\/span>S\u1ef1 h\u1ea5p th\u1ee5<\/b><\/span><\/span><\/h3>\nSinh kh\u1ea3 d\u1ee5ng tuy\u1ec7t \u0111\u1ed1i c\u1ee7a niraparib l\u00e0 kho\u1ea3ng 73%. Sau khi u\u1ed1ng Niraparib, n\u1ed3ng \u0111\u1ed9 \u0111\u1ec9nh trong huy\u1ebft t\u01b0\u01a1ng, Cmax, \u0111\u1ea1t \u0111\u01b0\u1ee3c trong v\u00f2ng 3 gi\u1edd. D\u00f9ng \u0111\u1ed3ng th\u1eddi m\u1ed9t b\u1eefa \u0103n nhi\u1ec1u ch\u1ea5t b\u00e9o (800-1,000 calo v\u1edbi kho\u1ea3ng 50% t\u1ed5ng l\u01b0\u1ee3ng calo c\u1ee7a b\u1eefa \u0103n l\u00e0 t\u1eeb ch\u1ea5t b\u00e9o) kh\u00f4ng \u1ea3nh h\u01b0\u1edfng \u0111\u00e1ng k\u1ec3 \u0111\u1ebfn d\u01b0\u1ee3c \u0111\u1ed9ng h\u1ecdc c\u1ee7a Niraparib.<\/span><\/p>\n<\/span>Ph\u00e2n b\u1ed5<\/b><\/span><\/span><\/h3>\nNiranib li\u00ean k\u1ebft 83,0% v\u1edbi protein huy\u1ebft t\u01b0\u01a1ng c\u1ee7a con ng\u01b0\u1eddi. Th\u1ec3 t\u00edch ph\u00e2n b\u1ed1 bi\u1ec3u ki\u1ebfn \u200b\u200btrung b\u00ecnh (\u00b1 SD) (Vd \/ F) l\u00e0 1220 (\u00b1 1114) L. Trong m\u1ed9t ph\u00e2n t\u00edch d\u01b0\u1ee3c \u0111\u1ed9ng h\u1ecdc d\u00e2n s\u1ed1, Vd \/ F c\u1ee7a Niraparib l\u00e0 1074 L \u1edf b\u1ec7nh nh\u00e2n ung th\u01b0.<\/span><\/p>\n<\/span>Lo\u1ea1i b\u1ecf<\/b><\/span><\/span><\/h3>\nSau khi d\u00f9ng nhi\u1ec1u li\u1ec1u h\u00e0ng ng\u00e0y 300 mg Niraparib, th\u1eddi gian b\u00e1n th\u1ea3i trung b\u00ecnh (t1 \/ 2) l\u00e0 36 gi\u1edd. Trong m\u1ed9t ph\u00e2n t\u00edch d\u01b0\u1ee3c \u0111\u1ed9ng h\u1ecdc qu\u1ea7n th\u1ec3, t\u1ed5ng \u0111\u1ed9 thanh th\u1ea3i r\u00f5 r\u00e0ng (CL \/ F) c\u1ee7a niraparib l\u00e0 16,2 L \/ h \u1edf b\u1ec7nh nh\u00e2n ung th\u01b0.<\/span><\/p>\n<\/span>S\u1ef1 trao \u0111\u1ed5i ch\u1ea5t<\/b><\/span><\/span><\/h3>\nNiraparib \u0111\u01b0\u1ee3c chuy\u1ec3n h\u00f3a ch\u1ee7 y\u1ebfu b\u1edfi c\u00e1c carboxylesterase (CE) \u0111\u1ec3 t\u1ea1o th\u00e0nh m\u1ed9t ch\u1ea5t chuy\u1ec3n h\u00f3a ch\u00ednh kh\u00f4ng ho\u1ea1t \u0111\u1ed9ng, sau \u0111\u00f3 tr\u1ea3i qua qu\u00e1 tr\u00ecnh glucuronid h\u00f3a.<\/span><\/p>\n<\/span>B\u00e0i ti\u1ebft<\/b><\/span><\/span><\/h3>\nSau khi s\u1eed d\u1ee5ng m\u1ed9t li\u1ec1u duy nh\u1ea5t 300 mg Niraparib \u0111\u00e1nh d\u1ea5u v\u00f4 tuy\u1ebfn b\u1eb1ng \u0111\u01b0\u1eddng u\u1ed1ng, ph\u1ea7n tr\u0103m ph\u1ee5c h\u1ed3i trung b\u00ecnh c\u1ee7a li\u1ec1u \u0111\u00e3 d\u00f9ng trong 21 ng\u00e0y l\u00e0 47,5% (kho\u1ea3ng 33,4% \u0111\u1ebfn 60,2%) trong n\u01b0\u1edbc ti\u1ec3u v\u00e0 38,8% (kho\u1ea3ng 28,3% \u0111\u1ebfn 47,0%) trong ph\u00e2n. Trong c\u00e1c m\u1eabu g\u1ed9p \u0111\u01b0\u1ee3c thu th\u1eadp trong 6 ng\u00e0y, Niraparib kh\u00f4ng thay \u0111\u1ed5i l\u1ea7n l\u01b0\u1ee3t chi\u1ebfm 11% v\u00e0 19% li\u1ec1u s\u1eed d\u1ee5ng \u0111\u01b0\u1ee3c thu h\u1ed3i trong n\u01b0\u1edbc ti\u1ec3u v\u00e0 ph\u00e2n.<\/span><\/p>\n<\/span>Li\u1ec1u l\u01b0\u1ee3ng & C\u00e1ch d\u00f9ng<\/b><\/span><\/span><\/h2>\n\n- Li\u1ec1u khuy\u1ebfn c\u00e1o c\u1ee7a Niranib d\u01b0\u1edbi d\u1ea1ng \u0111\u01a1n tr\u1ecb li\u1ec7u l\u00e0 300 mg (ba vi\u00ean nang 100 mg) u\u1ed1ng m\u1ed9t l\u1ea7n m\u1ed7i ng\u00e0y.\u00a0<\/span><\/li>\n
- H\u01b0\u1edbng d\u1eabn b\u1ec7nh nh\u00e2n d\u00f9ng li\u1ec1u Niraparib c\u1ee7a h\u1ecd v\u00e0o c\u00f9ng th\u1eddi \u0111i\u1ec3m m\u1ed7i ng\u00e0y. M\u1ed7i vi\u00ean nang n\u00ean nu\u1ed1t to\u00e0n b\u1ed9. Niraparib c\u00f3 th\u1ec3 \u0111\u01b0\u1ee3c d\u00f9ng c\u00f9ng ho\u1eb7c kh\u00f4ng c\u00f9ng th\u1ee9c \u0103n.<\/span><\/li>\n<\/ul>\n