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Neratinib

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Neratinib waa awood, dib u celin karin tyrosine kinase inhibitor (TKI) ee HER1, HER2, iyo HER4, haatana wuxuu kusocdaa horumar. Neratinib wuxuu si aan macquul aheyn ugu xiraa qaybta isdhexgalka ee isku xidhka HER1, HER2, HER3, iyo soo-saaraha kobaca epithelial, wuxuuna horjoogsadaa fosforyaalka iyo dhowr jidadka calaamadaha hoose ee HER. Natiijadu waa hoos u dhac ku yimid iyo kordhinta dhimashada unugyada. Daraasadaha caafimaadka ayaa muujiyay in ka hortagga unugyada 'HER signaling' ee neratinib ay tahay hab wax ku ool ah oo lagu xakameynayo koritaanka burooyinka HER-dhexdhexaadinta iyo ka-guuleysiga farsamooyinka ka-baxsiga burooyinka ee khibradda u leh daaweynta HER2 ee hadda la beegsanayo iyo wakiillada daaweynta kiimikada.

Product Description

Astaamaha Aasaasiga ah

Product Name Budada Neratinib
CAS Number 698387-09-6
Formula kelli C30H29ClN6O3
Miisaanka Nooca 557.04
Isku mid ahaanshaha HKI-272;

PB272;

Budada Neratinib;

Nerlynx;

698387-09-6.

Imaanshaha Midab cad-cad ilaa budo huruud khafiif ah
Kaydinta iyo Isticmaalka Qalalan, madow iyo 0 - 4 C muddo gaaban (maalmo illaa toddobaadyo) ama -20 C muddo dheer (bilo illaa sannado).

 

Sharaxa budada Neratinib

Budada Neratinib, oo sidoo kale loo yaqaan HKI-272 ama PB272, waa hadal la heli karo, oo aan la celin karin oo ah HER-2 receptor tyrosine kinase oo leh firfircoonaan antineoplastic ah.

Budada Neratinib waxay ku xidhan tahay soo-dhoweynta HER-2 si aan macquul ahayn, taas oo yareyneysa autophosphorylation-ka unugyada, sida muuqata iyada oo la beegsanayo haraaga cysteine ​​ee ku jira jeebka ATP-qabashada.

Daaweynta unugyada ee wakiilkan waxay keeneysaa xakameynta dhacdooyinka wareejinta calaamadaha gunta hoose iyo dariiqooyinka nidaaminta wareegga unugyada; qabashada G1-S (Gap 1 / DNA synthesis) - wareejinta asalka wareegga unugyada; iyo ugu dambeyntii hoos u dhaca faafitaanka unugyada.

Budada Neratinib sidoo kale waxay horjoogsataa cuncunka epidermal factor reseptor (EGFR) kinase iyo faafitaanka unugyada ku tiirsan EGFR.

 

Nidaamka Budada 'Neratinib Powder' ee Ficilka

Budada Neratinib waa mid awood leh, oo aan la celin karin tyrosine kinase inhibitor (TKI) ee HER1, HER2, iyo HER4, haatana wuxuu ku jiraa horumar. Budada Neratinib waxay si aan macquul ahayn ugu xiraysaa qaybta isdhexgalka ee HER1, HER2, HER3, iyo soo-saaraha kobaca epithelial, wuxuuna xakameynayaa fosforyaalka iyo dhowr waddooyinka calaamadaha HER. Natiijadu waa hoos u dhac ku yimid iyo kordhinta dhimashada unugyada. Daraasadaha caafimaadka ayaa muujiyay in ka hortagga unugyada 'HER signaling' ee budada neratinib ay tahay qaab wax ku ool ah oo lagu xakameynayo koritaanka burooyinka HER-dhexdhexaadinta iyo ka-hortagga hababka ka-baxsiga burooyinka ee khibradda u leh daaweynta HER2 ee hadda la beegsanayo iyo wakiilada kiimikada.

Budada Neratinib ayaa sidoo kale muujisay inay waxtar leedahay daaweynta ugu horeysa ee HER2-positive, kansarka naasaha ee metastatic (MBC). Markii loo isticmaalo isku-darka paclitaxel, budada neratinib waxay muujisay ORR 73%. Markii lagu daro capecitabine, wakiil kale oo kiimiko ah, ORR wuxuu ahaa 63%. Marka lagu daro HER2-positive MBC, budada neratinib ayaa sidoo kale waxtar u leh bukaanada qaba kansarka naasaha ee HER2. Wajiga 2 SUMMIT tijaabada, bukaanada qaba kansarka naasaha ee HER2-mutated waxay la kulmeen 33% ORR usbuucyada 8.

Budada Neratinib waa TKI-da ugu horeysa ee la cadeeyo si loo yareeyo halista cudurka ku soo noqnoqda bukaanka qaba cudurka HER2-kansarka naasaha. Iyada oo ku saleysan waxtarka budada neratinib ee marxaladda hore HER2-kansarka naasaha, MBC, iyo burooyinka HER2-mutant, budada neratinib ayaa la rajeynayaa inay noqdaan heerka cusub ee daryeelka guud ahaan goobaha daaweynta kansarka naasaha.

 

Neratinib budada Codsiga

Budada Neratinib waxay ku xidhan tahay soo-dhoweynta HER-2 si aan macquul ahayn, taas oo yareyneysa autophosphorylation-ka unugyada, sida muuqata iyada oo la beegsanayo haraaga cysteine ​​ee ku jira jeebka ATP-qabashada.

Kansarka naasaha ee HER2-positive wuxuu aad uga sameeyaa borotiinka HER2. Borotiinka HER2 wuxuu ku fadhiyaa dusha unugyada kansarka wuxuuna helayaa calaamado u sheegaya kansarka inuu koro oo uu fido. Budada Neratinib waxay la dagaalantaa HER2-kansarka naasaha iyada oo laga hortagayo awooda unugyada kansarka si ay u helaan calaamadaha koritaanka.

Budada Neratinib waa daaweyn la bartilmaameedsaday, laakiin ka duwan Herceptin (magaca kiimikada: trastuzumab), Kadcyla (magaca kiimikada: T-DM1 ama ado-trastuzumab emtansine), iyo Perjeta (magaca kiimikada: pertuzumab), maahan daaweyn lala beegsado. Daaweynta la-bartilmaameedsaday ee difaaca jirka ayaa ah noocyada difaaca jirka ee sida dabiiciga ah u dhaca oo u shaqeeya sida difaaca jirka ee ay sameeyaan nidaamyada difaaca jirka. Budada Neratinib waa shey kiimiko ah, ee ma ahan antibody.

 

Neratinib Powder Side Raadka & Digniinta

Budada Neratinib waxay dadka qaarkood ku sababi kartaa shuban-halis gelin kara nolosha iyo shuban-biyood dhexdhexaad ama dhexdhexaad ah ku dhowaad qof walba; dadka qaata sidoo kale waxay halis ugu jiraan dhibaatooyinka shubanka sida fuuqbaxa iyo isu dheelitir la'aanta elektroolka.

Sidoo kale waxaa jira halista waxyeelo daran oo beerka ah bukaan badanna waxay leeyihiin heer; astaamaha waxyeelada beerka waxaa ka mid ah daal, lallabbo, matag, midigta kore ee midig xanuun ama danqasho, qandho, firiiric, iyo heerar sare oo eosinophils ah.

Waxaas kor ku xusan ka sokow, in ka badan 10% dadka qaata waxay leeyihiin lallabbo, calool xanuun, matag, nabarro bushimahooda, calool xanuun, cunno xumo, finan, iyo murqo xanuun.

 

Tixraaca

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[2] LiverTox: Macluumaadka Caafimaadka iyo Cilmi-baarista ee Dhaawaca Beerka ee Daroogada Ku Nool [Internet]. Bethesda (MD): Machadka Qaranka ee Sonkorowga iyo Cudurada Dheefshiidka iyo Kelyaha; 2012-. Waxaa laga heli karaa http://www.ncbi.nlm.nih.gov/books/NBK548937/ PubMed PMID: 31644242.

[3] Booth LA, Roberts JL, Dent P. Doorka calaamadaha unugyada ee isgoyska u dhexeeya autophagy iyo apoptosis ee qawaaniinta badbaadada unugyada burooyinka iyadoo laga jawaabayo sorafenib iyo neratinib. Semin Kansarka Biol. 2019 Oct 20. pii: S1044-579X (19) 30024-0. doi: 10.1016 / j.semcancer.2019.10.013. [Epub ka hor daabacaadda] Dib u eegid. Caawinta PMID: 31644944.

[4] Miles J, White Y. Neratinib loogu talagalay daaweynta marxaladda hore HER2-Kansarka Naasaha ee Wanaagsan. J Adv Pract Oncol. 2018 Noofambar-Dec; 9 (7): 750-754. Epub 2018 Nofeembar 1. Dib u eegid. PubMed PMID: 31249722; PubMed Bartamaha PMCID: PMC6570523.

[5] Collins DM, Conlon NT, Kannan S, Verma CS, Eli LD, Lalani AS, Crown J. Astaamaha takhasuska leh ee ka-hortagga Pan-HER Kinase Inhibitor Neratinib Marka La Barbardhigo Lapatinib: Saameynta Daaweynta HER2-Positive iyo HER2- Kansarka Naasaha oo isbedelay. Kansarrada (Basel). 2019 Meey 28; 11 (6). pii: E737. doi: 10.3390 / kansarrada11060737. Dib u eegis. PubMed PMID: 31141894; PubMed Bartamaha PMCID: PMC6628314.

[6] Deeks ED. Neratinib: Ansixinta Ugu Horeysa Caalamka. Daroogada. Oktoobar 2017; 77 (15): 1695-1704. doi: 10.1007 / s40265-017-0811-4. Dib u eegis. Caawinaad PMID: 28884417.

[7] Kourie HR, El Rassy E, Clatot F, de Azambuja E, Lambertini M. Daawooyinka soo ifbaxaya ee HER2-kansarka naasaha marxaladda hore: diiradda saarista neratinib. Bartilmaameedka Onco Ther. 2017 Jul 10; 10: 3363-3372. doi: 10.2147 / OTT.S122397. eCollection 2017. Dib u eegis. PubMed PMID: 28744140; PubMed Bartamaha PMCID: PMC5513878.

[8] “Qeexitaanka neratinib - Qaamuuska Maandooriyaha Qaranka ee Machadka Kansarka”. Waxaa dib loo helay 1 Diseembar 2008.

[9] "Calaamadda kiniiniga Neratinib" (PDF). Maamulka Cuntada iyo Dawooyinka ee Mareykanka (FDA). Luulyo 2017. Waxaa la soo celiyey 6 Febraayo 2018. Wixii ku saabsan cusbooneysiinta calaamadda arag, bogga tusmada FDA ee NDA 208051 Maqaalkani wuxuu ku darayaa qoraal ka yimid ilahaan, oo ku yaal qaybta dadweynaha. Gandhi L, et al. (2017). "MA04.02 Neratinib ± Temsirolimus ee HER2-kansarka sanbabada mutant: daraasad caalami ah, oo la kala soocay wejiga II". Joornaalka 'Thoracic Oncology'. 12 (1): S358-9. doi: 10.1016 / j.jtho.2016.11.398.