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Ceritinib (LDK378)

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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).

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.

 

Tusitaiala

[1] “Zykadia (ceritinib) Capsules, mo le Tautala i le Gutu. Faʻamatalaga Atoa atoatoa ”(PDF). Novartis Faletalavai Faʻalapotopotoga. 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 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 Faʻamaonia mo kanesa kanesa". National Cancer Institute. 27 Iuni 2017