Tulaga Autu

Igoa oloa	Ceritinib (LDK378) pauta
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) efuefufaʻamatalaga

E faʻaaogaina le pauta o le Ceritinib mo le togafitia o tagata mamaʻi e maua i le mama o le kanesa o le limapoma (ALK +) e leʻo laʻititi le kanesa o le mama (NSCLC) ua faʻateleina pe ua le mafai ona onosaʻi 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 fesuiaʻi non-laiti-sela mama kanesa. Ole faʻateleina ole faʻamaonia ole malosiʻaga ole papala ole ALK, pei ole crizotinib ma le taimi lata mai nei ole ceritinib (LDK378) paʻu, faʻavae i luga ole vaega lelei ole faʻataʻitaʻiga I / II na avea ma faʻamanuiaga iloga ile suʻesuʻeina ole kanesa ole falemaʻi ma saofaga ile vaitau fou o oncogenic target togafitiga faʻamatalaina e matagofie tisaini tofotofoga togafitiga. ceritinib efuefu ia avea ma se malosiaga sui i le crizotinib mo le ALK-toe faʻafouina le leai-laʻititi sela sela kanesa o loʻo faʻaalia foi.

 

Ceritinib (LDK378) pauta Mechanism of Action

O le Ceritinib paula e faʻaaogaina e togafitia ai tagata mamaʻi ma le kanesa o le sela e le o tamaʻi sela (NSCLC) e lelei mo le anaplastic lymphoma kinase (ALK) ma o latou tuma o loʻo alualu i luma pe le mafai onosaʻi Crotinib (crizotinib).

Ceritinib efuefu o se filifilia ma malosi taofiofia o 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. Ae ui i lea, o le chromosomal translocation ma fusion e faʻatupuina ai le oncogenic form o le ALK lea na aafia i le alualu i luma o le NSCLC. O le Ceritinib efuefu o loʻo galue e taofia lenei mutated enzyme ma taofi le faʻateleina o sela, ma iʻu ai ona taofi le alualu i luma o le kanesa. Talu ai ona o le ceritinib paula ua manatu o se faʻataʻitaʻiina o le kanesa togafitiga, e manaʻomia ai se suʻesuʻega ua faʻamaonia e le FDA e faʻamautinoa ai poʻo fea tagata gasegase e tauva mo le ceritinib paula. O lenei suʻega na atiaʻe e Roche, ole VENTANA ALK (D5F3) CDx Assay ma e faʻaaogaina e faʻailoaina ai tagata gasegase ole ALK-positive NSCLC e faʻamanuiaina ile ceritinib paʻu togafitiga.

 

Ceritinib (LDK378) efuefu talosaga

O le Ceritinib efuefu o le anaplastic lymphoma kinase (ALK) -positive inhibitor e masani ona faʻaaogaina mo le togafitia o le metastatic NSCLC. Talu ai, na faʻailoaina lava mo tagata mamaʻi na atiaʻe teteʻe atu i le crizotinib, o le isi ALK-lelei taofi, ae talu mai lona faʻateleina faʻaaoga e avea o se muamua filifiliga mo metastatic NSCLC.

 

Ceritinib (LDK378) efuefu 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 faʻaiuga, o le ceritinib pauta o se mea taua ma malosi faʻalavelaveina o le enzyme CYP3A4, o vailaʻau la e tatau ona vaʻavaʻaia ma le totoʻa e ono fesoʻotaʻi ma le ceritinib paula.

 

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.

 

Tusitaiala

[1] "Zykadia (ceritinib paʻu) Capsules, mo le Gutu Faʻaaoga. Faʻamatalaga Atoa atoatoa ”(PDF). Novartis Fale Faʻafomai Toe aumai 14 Fepuari 2017.

[2] "Faʻavaomalo igoa le faʻaaogaina mo vailaʻau vailaʻau (INN). Fautuaina Faʻavaomalo Faʻavaea Igoa: Lisi 71 "(PDF). WHO. 2014. i. 79. Toe aumai ile 14 Fepuari 2017

[3] "Faʻamaonia e le FDA le Ceritinib paʻu mo le ALK-Positive Lung Cancer". Medscape Aperila 29, 2014.

[4] "Faʻamatalaina faʻamatalaga" (PDF). www.pharma.us.novartis.com. Toe aumai 2019-06-12.

[5] "Faʻalauteleina e le FDA Ceritinib paʻu Faʻamaonia mo kanesa o le mama". National Cancer Institute. 27 Iuni 2017

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