Faamatalaga oloa
Tulaga Autu
Igoa oloa | Ceritinib (LDK378) |
Numera CAS | 1032900-25-6 |
Faiga Faʻavae Molecular | C28H36CIN5O3S |
Fua Faatatau o le Umi | 558.135 |
Synonyms | LDK-378;
NVP-LDK378; NVP-LDK378-NX; 5-Chloro-N2-[5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl]-N4-[2-(propan-2-ylsulfonyl)phenyl]pyrimidine-2,4-diamine. |
Faʻaaliga | Paʻepaʻe i paʻu paʻepaʻe paʻepaʻe |
Teuina ma Taulimaina | Teu ia i le vevela potu ma alu ese mai le sili atu vevela ma susu. |
Ceritinib (LDK378)faʻamatalaga
O loʻo faʻaaogaina Ceritinib mo le togafitia o tagata mamaʻi ua iai le anaplastic lymphoma tum-posit (ALK +) i le kanesa o le sela niniʻi laʻititi (NSCLC) ua faʻateleina pe ua le mafai onosai ile crizotinib pe a uma togafitiga ma le crizotinib.
O le toe faʻataʻitaʻiga o le chromosomal aofia ai le anaplastic lymphoma kinase (ALK) o se avetaʻavale oncogenic ua uma ona suia atoa le togafitia o le kanesa o le mama e le o se sela laʻititi. I le sefulu tausaga ua tuanaʻi, o fualaʻau faʻatosina na aliaʻe mai o se auala lelei mo le tagata lava ia mo le ALK-toe faʻafouina le leai-laiti-sela mama kanesa. O le faʻateleina o le faʻamaonia o le malosi ALK taofi, e pei o le crizotinib ma lata mai nei ceritinib (LDK378), faʻavae i luga o le lelei fuafuaina vaega I / II faʻataʻitaʻiga, o se mataʻina manuia i togafitiga faʻafomaʻi kanesa ma fesoasoani ai i se vaitau fou o oncogenic faʻataʻitaʻia togafitiga faʻamatalaina e matagofie mamanu faʻataʻitaʻi falemaʻi. ceritinib ia avea ma se fesuiaiga malosi i crizotinib mo ALK-toe fesuiaʻi le-laiti-sela sela kanesa o loʻo faʻaalia foi.
Ceritinib (LDK378)Mechanism of Action
O le Ceritinib e faʻaaoga e togafitia ai tagata mamaʻi e leai se laʻititi o kanesa kanesa o le sela (NSCLC) e lelei mo le anaplastic lymphoma kinase (ALK) ma o latou patu o loʻo alualu i luma pe le mafai onosaia Crotinib (crizotinib).
Ceritinib o se filifilia ma malosi taofiofia o le anaplastic lymphoma kinase (ALK). I le masani ai o le tino, ALK galue o se ki laʻasaga i le atinaʻeina ma le faʻagaioiga o neula e faʻaaoga ai tino. Ae ui i lea, o le chromosomal translocation ma fusion e faʻatupuina ai se ituaiga oncogenic o le ALK lea na aafia i le alualu i luma o le NSCLC. Ceritinib o lea e galue e taofia ai lenei mutated enzyme ma taofi le faʻateleina o sela, mulimuli ane taofia le alualu i luma kanesa. Talu ai o le ceritinib ua manatu o se faʻataʻitaʻiga o le kanesa togafitiga, o le suʻega ua faʻamaonia e le FDA e manaʻomia e filifili ai poʻo fea tagata gasegase e tauva mo ceritinib. O lenei suʻega, na atiaʻe e Roche, ole VENTANA ALK (D5F3) CDx Assay ma e faʻaaogaina e faʻailoa ai ALK-positive NSCLC tagata mamaʻi e ono faʻamanuiaina ile togafitiga ole ceritinib.
Ceritinib (LDK378)talosaga
Ceritinib o se anaplastic lymphoma kinase (ALK) -positive inhibitor muamua faʻaaoga mo le togafitia o metastatic NSCLC. Talu ai, na na faʻailoa mai mo tagata mamaʻi na atiaʻe teteʻe atu i crizotinib, o le isi ALK-lelei taofia, ae talu mai lona faʻaaogaina faʻalauteleina i avea o se muamua filifiliga mo metastatic NSCLC.
Ceritinib (LDK378)Aafiaga Itu & Lapataiga
Ogaoga aafiaga leaga aofia ai gastrointestinal oona, hepatotoxicity, interstitial mama faamaʻi, umi QT syndrome, hyperglycemia, bradycardia, ma pancreatitis.
O aʻafiaga e masani ona lipotia mai o manava tata, niniva, maualuga le maualuga o le ate o le ate, puaʻi, tiga o le manava, lelava, faaitiitia le fiaai, ma le papala. Ona o le lamatiaga o le maualuga o le ate o le ate, e tatau ona faia suʻesuʻe gaioiga i le taʻilua vaiaso mo le 9 vaiaso muamua o togafitiga.
I le iuga, ceritinib o se substrate ma malosi inhibitor o le enzyme CYP3A4, o vailaʻau tatau ona vaʻavaʻaia ma le faʻaeteete e ono fegasoloaʻi ma ceritinib.
Valaʻau foʻi i lau fomaʻi i le taimi e tasi pe a fai oe i ai:
▪ ogaoga le manava tata;
▪ tiga le ulu, le mautonu, suia ile tulaga ole mafaufau, leiloa se vaʻai, faoa faamalosi (maʻi o le mafaufau);
▪ laititi pe leai foi se mimi;
▪ Toto e le masani ai (isu o le isu, palapala toto totoga mamafa), poʻo seisi lava palapala toto e le taofia;
▪ faʻailoga o le manava ua tafetotoi ile toto - poʻo nofo tuai, faʻasusu le toto poʻo le puaʻi e pei o kofe kofe;
▪ faʻafitauli i le fatu - tiga o le fatafata, tiga i lou auvae poʻo tauʻau, fulafula, vave oso mamafa, lagona le lava le manava;
▪ faʻailoga ole toto - faʻafuaseʻi poʻo le vaivai, faʻafitauli ile vaʻai poʻo le tautala;
▪ faʻafitauli o le ate - miaga pogisa, fata paʻu palapala, jaundice (samasama o le paʻu po o mata);
▪ maualalo le kalasiumalosi – maso maso poʻo le faʻapipiʻiina, niniva poʻo se lagona paʻu (i lou gutu, poʻo ou tamailima ma tamaivae);
▪ faʻateleina le toto - ogaoga le tiga o le ulu, faʻanenefu le vaʻai, o loulou i lou ua poʻo taliga, atuatuvale, maʻi isu.
O au togafitiga kanesa e ono faʻatuai pe le toe faʻaauauina pe a iai ni ou aʻafiaga.