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Ceitinib (LDK378)

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Ceritinib Powder inoshandiswa kurapa varwere vane metastatic isiri-diki kenza yemapapu kenza (NSCLC) vane hutano hweaplastic lymphoma kinase (ALK) uye vane mamota ari kufambira mberi kana asingakwanise kutsungirira Crotinib (crizotinib).

Product Description

Basic Hunhu

Product Name Ceritinib (LDK378) upfu
CAS Number 1032900-25-6
Molecular Formula C28H36CIN5O3S
Formula Weight 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.

Kuonekwa Muchena kusvika pachena-poda yakachena
Kuchengeta uye Kubata Zvichengetedze pamhepo tembiricha uye kure nekupisa kwakanyanya uye hunyoro.

 

Ceritinib (LDK378) Podatsananguro

Ceritinib powder inoshandiswa pakurapa varwere vane anaplastic lymphoma tumor-positive (ALK +) metastatic isiri-diki kenza yemapapu kenza (NSCLC) iyo yakawedzera kana isingashivirane necrizotinib mushure mekurapwa ne crizotinib.

Iyo chromosomal rearrangements inosanganisira iyo anaplastic lymphoma kinase (ALK) semutyairi wecocogenic yakanyatso shandura kurapwa kweasina-madiki-maseru kenza yemapapu. Mumakore gumi apfuura, zvinodhaka zvakanangwa zvakabuda seyakarongeka nzira yakasarudzika yeALK-yakagadziriswazve isiri-diki-sero kenza yemapapu. Iko kukurumidza kubvumidzwa kweakasimba ALK inhibitors, senge crizotinib uye ichangoburwa ceritinib (LDK378) poda, zvichibva pachikamu chakanyatsogadzirwa chikamu cheI / II miedzo kwave kubudirira kwakakosha mukutsvagisa kenza yekiriniki uye kunopa nguva nyowani yeoncogenic yakanangwa kurapwa kunozivikanwa yakashongedzwa yekiriniki kuyedza dhizaini. ceritinib powder kuti ive imwe nzira ine simba kune crizotinib yekenza yeAlk-yakagadzirwazve isiri-diki-kenza yemapapu yemapapu inowanikwawo.

 

Ceritinib (LDK378) upfu Mechanism of Action

Ceritinib powder inoshandiswa kurapa varwere vane metastatic isiri-diki kenza yemapapu kenza (NSCLC) vane hutano hweaplastic lymphoma kinase (ALK) uye vane mamota ari kufambira mberi kana asingakwanise kutsungirira Crotinib (crizotinib).

Ceritinib powder inosarudza uye ine simba inhibitor yeaplastic lymphoma kinase (ALK). Mune zvakajairwa physiology, ALK inoshanda senhanho yakakosha mukuvandudza uye mashandiro enervous system tishu. Nekudaro, chromosomal translocation uye fusion zvinomutsa imwe oncogenic fomu ye ALK iyo yakave yakabatanidzwa mukufambira mberi kweNSCLC. Ceritinib powder nokudaro inoshanda kudzivirira iyi enzyme yakachinja uye kumisa kuwanda kwesero, pakupedzisira ichimisa kufambira mberi kwekenza. Nekuti ceritinib powder inoonekwa seyakanangana nekenza yekurapa, bvunzo yeDAA-inogamuchirwa inodiwa kuti uone kuti ndevapi varwere vari kukwikwidza ceritinib powder. Iyi bvunzo, yakagadziriswa naRoche, ndiyo VENTANA ALK (D5F3) CDx Assay uye inoshandiswa kuzivisa ALK-positive NSCLC varwere vaizobatsirwa neceritinib powder kurapwa.

 

Ceritinib (LDK378) Poda kunyoresa

Ceritinib powder is an anaplastic lymphoma kinase (ALK) -positive inhibitor inonyanya kushandiswa pakurapa metastatic NSCLC. kushanda senzira yekutanga yeMastastatic NSCLC.

 

Ceritinib (LDK378) Poda Side Migumisiro & Yambiro

Migumisiro yakakomba yakakomba inosanganisira gastrointestinal toxicity, hepatotoxicity, interstitial mapapu chirwere, yakareba QT syndrome, hyperglycemia, bradycardia, uye pancreatitis.

Mhedzisiro inowanzo kutaurwa ndeye manyoka, kusvotwa, makemikari eropa akakwidziridzwa, kurutsa, kurwadziwa mudumbu, kuneta, kuderera kwechido, uye kupatira. Nekuda kwenjodzi yemakemikari eropa akakwidziridzwa, bvunzo dzechiropa dzinofanirwa kuitwa vhiki mbiri dzese kwemavhiki mapfumbamwe ekurapa.

Chekupedzisira, ceritinib poda iri mbiri substrate uye ine simba inhibitor yeiyo enzyme CYP3A4, saka mishonga inofanirwa kutariswa zvine hungwaru iyo inogona kusangana ne ceritinib powder.

 

Danaidzawo chiremba wako kamwechete kana iwe uine:

▪ manyoka akanyanya;

▪ kutemwa nemusoro, kuvhiringidzika, kuchinja mamiriro epfungwa, kurasikirwa nemaziso, kufenda (kugwinha);

▪ kuita weti shoma kana kusaita;

▪ kubuda ropa zvisina kujairika (kubuda ropa mumhino, kubuda ropa kwakanyanya kumwedzi), kana kumwe kubuda ropa kusingamiri;

Zviratidzo zvekubuda ropa mudumbu - zvituru zvine ropa kana zvekumira, kukosora ropa kana kurutsa zvinoita senzvimbo yekofi;

▪ matambudziko emwoyo - kurwadziwa kwepfupa, kurwadziwa mushaya kana pabendekete, kuzvimba, kuwedzera uremu nekukurumidza, kunzwa kufema kwekufema;

▪ zviratidzo zvekuvhara kweropa-kamwe kamwe kushaya simba kana kushaya simba, matambudziko ekuona kana kutaura;

▪ matambudziko echiropa- weti yakasviba, zvituru zvine ruvara rwevhu, jaundice (yero yeganda kana maziso);

▪ yakaderera calcium level-mhasuru spasms kana contractions, chiveve kana kushushikana kunzwa (kutenderedza muromo wako, kana muzvigunwe nezvigunwe);

▪ kuwedzerwa kweBP - kutemwa nemusoro kwakakomba, kusaona zvakanaka, kurova muhuro kana nzeve, kushushikana, kubuda ropa mumhino.

Zvirwere zvako zvegomarara zvinogona kunonoka kana kumiswa zvachose kana uine mamwe mhedzisiro.

 

Reference

[1] “Zykadia (ceritinib powder) Makapisi, ekushandisa Oral. Yakazara Kurondedzera Ruzivo ”(PDF). Novartis Pharmaceuticals Corporation. Yakadzorerwa 14 Kukadzi 2017.

[2] "Mazita Enyika dzese Asiri ekuzvitengesera eMishonga yeMishonga (INN). Yakakurudzirwa Mazita Asiri Ekuzvimiririra Emarudzi: Rondedzero 71 ”(PDF). Sangano Rinoona nezve Utano Pasi pose. 2014. p. 79. Yakadzorerwa 14 Kukadzi 2017

[3] "FDA Inobvumira Ceritinib powder yeAlk-Positive Lung Cancer". Medscape. Kubvumbi 29, 2014.

[4] "Kunyora data" (PDF). www.pharma.us.novartis.com. Yakadzorerwa 2019-06-12.

[5] "FDA Inowedzera Ceritinib powder Kubvumidzwa kweLung Cancer". National Cancer Institute. 27 Chikumi 2017.