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Neratinib

 

  1. Zvakawanda Sei Tinoziva Nezve Kenza Yezamu?
  2. Clinical Mhedzisiro Ne FDA Apprvoal
  3. Chii chinonzi Neratinib?
  4. Ndiani Angangoda Neratinib?
  5. Nzira yekuziva sei kuti Neratinib Yakakukodzera Iwe?
  6. Neratinib Inoshanda Sei?
  7. Isu Tinotora Sei Neratinib?
  8. Zvatingaone Nezvakashata Mhedzisiro yeNeratinib?
  9. mhedziso

 

Zvakawanda Sei Tinoziva Nezve Kansa yepabonde

Gomarara repazamu ndiyo kenza yakajairika muvakadzi, inomiririra 15% yenyaya dzese dzekenza muUnited States. Muna 2017, 252,710 40,600 zviitiko zvitsva zvekenza yemazamu zvakafungidzirwa kuongororwa, uye vakadzi vanopfuura makumi mana nemazana matanhatu kufa nechirwere ichi. Gomarara repazamu rinogona zvakare, kashoma, kubata varume, iine angangoita mazana maviri nemakumi maviri nematanhatu emakesi matsva anoonekwa gore rega.

Inenge 15% kusvika 20% yemakenza emukaka wemazamu ane HER2-yakanaka. Gomarara repazamu rine huwandu hwakakwira hweHER2 hune njodzi yakawedzera yemastastasis, isina kukwana kurapwa mhinduro, uye kudzoka.

Iyo budiriro uye inotevera US Chikafu neDrug Administration (FDA) tendero yetrastuzumab (Herceptin), anopesana HER2 anopikisa, akachinja paradigm yekurapa yevarwere vane HER2-yakanaka chirwere. Kana trastuzumab yakawedzerwa kune chemotherapy, huwandu hwese hwekupona kwevakadzi vane yekutanga-nhanho HER2-yakanaka kenza yemazamu yakagadziridzwa kusvika pa37%. Zvisinei, vanenge 26% yevarwere vane chirwere chinowanzoitika mushure mekurapwa ne trastuzumab.

Dzimwe nzira dzokurapa dzinotarisa kenza yemazamu yeHER2-inosanganisira pertuzumab (Perjeta), monoclonal antibody; ado-trastuzumab emtansine (Kadcyla), monoclonal antibody yakanamatira kune chemotherapy mushonga; uye lapatinib (Tykerb), kinase inhibitor.

 

Clinical Results Na FDA Kugamuchirwa

Iyo FDA kubvumidzwa kweNeratinib kwaive kwakavakirwa paChikamu chechitatu cheExteNET kuyedza, multicenter, yakasarudzika, yakapofomara-yakapofumara, yekuedzwa-kwenzvimbo-inodzorwa kutongwa kwe neratinib inotevera adjuvant trastuzumab kurapwa. Kuedzwa kwakanyora vakadzi mazana maviri nemazana mana nemakumi mana nemazana ekutanga-nhanho HER2,840-yakanaka kenza yemazamu uye mukati memakore maviri ekupedzisa adjuvant trastuzumab. Zvidzidzo izvi zvaive zvakasarudzika kuti zvigamuchire neratinib (n = 2) kana placebo (n = 1420) kwegore rimwe. Mhedzisiro yeExteNET kuyedzwa yakaratidza kuti mushure memakore maviri ekutevera, kurwisa-kusarwara kwezvirwere (iDFS) yaive 1420% muzvidzidzo zvakarapwa neratinib zvichienzaniswa ne94.2% kune avo vanogamuchira placebo.

Neratinib yakaongororwawo muChikamu chechitatu cheNALA kuyedzwa, kuyedzwa kwakarongedzwa kweeratinib plus capecitabine mune varwere vane HER2-yakanaka metastatic kenza yemazamu avo vakagamuchira maviri kana kupfuura apfuura anti-HER2-based regimens. Muedzo wakanyorera varwere ve621 avo vakasarudzika (1: 1) kuti vagamuchire neratinib 240 mg muromo kamwe kamwe pazuva pamazuva 1-21 mukubatana ne capecitabine 750 mg / m2 yakapihwa nemuromo kaviri pazuva pamazuva 1-14 kune yega yega 21-zuva kutenderera ( n = 307) kana lapatinib 1250 mg muromo kamwe chete zuva nezuva pamazuva 1-21 pamwe chete ne capecitabine 1000 mg / m2 inopiwa muromo kaviri zuva nezuva pamazuva 1-14 kune rimwe nerimwe rezuva re21 (n = 314). Varwere vaibatwa kusvika pakukura kwechirwere kana kusagamuchirwa chepfu. Kurapa neeratinib pamwe ne capecitabine kwakakonzera kuwanda kwakakosha mukufambira mberi-kwemahara kupona (PFS) zvichienzaniswa nekurapwa ne lapatinib pamwe capecitabine. Chiyero chePFS pamwedzi gumi nembiri chaive 12% yevarwere vakagamuchira neratinib plus capecitabine vs 29% yevarwere vakagamuchira lapatinib pamwe capecitabine; mwero wePFS pamwedzi makumi maviri nemana yaive 15% vs 24%, zvichiteerana. Median OS yaive nemwedzi makumi maviri neshanu yevarwere vakagamuchira neratinib pamwe chete necapecitabine zvichienzaniswa nemwedzi 12 yevarwere vakagamuchira lapatinib mukubatana pamwe necapecitabine.

 

Neratinib

 

chii Is Neratinib?

Neratinib (CAS: 698387-09-6) yakanangidzirwa (yeubereka) kurapa mushonga unodzivirira kukura uye kupararira kwekenza yemazamu. Neratinib ndiro zita risingazivikanwe remushonga. Zita rayo rezita ndiNerlynx.

 

ani Might Unoda Neratinib?

Neratinib inogona kupihwa kune vanhu vane kenza yepazamu yekutanga izvo zviri zviviri:

❶ Hormone receptor yakanaka (kenza yemazamu inokurudzirwa kukura nemahomoni estrogen kana progesterone)

❷ HER2 yakanaka (kenza yemazamu ine yakakwira kupfuura yakajairwa chikamu cheiyo HER2 protein)

 

Nzira yekuziva sei kuti Neratinib Yakakukodzera Iwe?

Pane bvunzo dzinoverengeka dzinoshandiswa kutsvaga kana kenza yemazamu iri HER2-yakanaka. Miviri yemiedzo yakajairika ndeiyi:

 

 IHC (ImmunoHistoChemistry)

Iyo IHC bvunzo inoshandisa kemikari dhayi kusvibisa iyo HER2 mapuroteni. IHC inopa mamakisi e0 kusvika ku3+ ayo anoyera huwandu hweHER2 mapuroteni ari pamusoro pemasero mune yemukaka yemazamu tishu sampuro. Kana iyo zvibodzwa iri 0 kusvika 1+, inoonekwa se HER2-isina. Kana zvibodzwa zviri 2+, zvinotorwa semuganhu. Chikamu che3+ chinoonekwa seHER2-yakanaka.

Kana iyo IHC bvunzo mhedzisiro iri pamuganhu, zvingangoita kuti chiedzo cheFISH chizoitwa pane muenzaniso wecancer tishu kuti uone kana cancer iri HER2-yakanaka.

 

 FISH (Fluorescence In Situ Hybridization)

Iyo FISH bvunzo inoshandisa akakosha mavara anonamatira kune HER2 mapuroteni. Mavara akakosha ane makemikari akawedzerwa kwavari saka vanoshandura ruvara uye kupenya murima pavanonamira kune HER2 mapuroteni. Uyu muedzo ndiwo wakanyanya kurongeka, asi unodhura uye zvinotora nguva yakareba kudzosa mhedzisiro. Ichi ndicho chikonzero iyo IHC bvunzo inowanzo kuve yekutanga bvunzo inoitwa kuti uone kana kenza iri HER2-yakanaka. Uine bvunzo yeFISH, unowana mamakisi ezvingave zvakanaka kana zvisina kunaka (zvimwe zvipatara zvinodaidza mhedzisiro yekutadza "zero").

 

Neratinib Inoshanda Sei?

HER2-yakanaka kenza yemazamu inoita yakawandisa yeiyo HER2 protein. Iyo HER2 protein inogara pamusoro pecancer maseru uye inogamuchira zviratidzo zvinotaurira kenza kuti ikure uye ipararire. Inenge imwe chete pagumi yekenza yemazamu ndeye HER2-yakanaka. HER2-yakanaka kenza yemazamu inowanzo kuve ine hukasha uye yakaoma kurapa kupfuura HER2-isina kunaka kenza yemazamu. Neratinib isingachinjiki pani-HER inhibitor. Neratinib inorwira HER2-inovhenekera kenza yemazamu nekuvharira gomarara maseru ekenza kugashira zviratidzo zvekukura.

Neratinib iri yakanangwa kurapwa, asi kusiyana naHerceptin (zita remakemikari: trastuzumab), Kadcyla (zita remakemikari: T-DM1 kana ado-trastuzumab emtansine), uye Perjeta (zita remakemikari: pertuzumab), haisi mishonga inotarisirwa kuzvidzivirira. Zvirwere zvekuzvidzivirira mumuviri maumbirwo eanowanzoitika masoja anoshanda semasoja ekudzivirira chirwere. Neratinib chinhu chemakemikari, kwete antibody.

 

Isu Tinotora Sei Neratinib?

Iyo yakakurudzirwa dhizaini yeNeratinib ndeye 240 mg (6 mapiritsi), inotorwa nemuromo kamwe zuva nezuva nechikafu, uye inoshandiswa ichienderera kwegore rimwe. Neratinib inowanikwa se1-mg piritsi.

Kune antidiarrheal prophylaxis, loperamide inofanirwa kushandiswa zvine mutsindo pamwe neyekutanga muyero weeratinib uye kuenderera mukati mekutanga maviri macircuit (kureva, mazuva makumi mashanu) yekurapa, uyezve pazvinenge zvichidikanwa. Varwere vanofanirwa kurairwa kuchengetedza 2 kusvika 56 ura kufamba zuva nezuva, uye vanofanirwa kurairwa mashandisiro ekurapa antirerrheal kurapwa marodhi.

Kukanganiswa kweiyo dhosi uye / kana kurudziro yekudzora dhizaini, zvichibva mukutsungirira kwemurwere, zvakatsanangurwa mune yekutsanangura ruzivo. Kune varwere vane hutachiona hwakakomba hwekuremara, iyo yekutanga neratinib dose inofanirwa kudzikiswa kusvika 80 mg.

 

Inotarisirwa: madata ese aingova sereferenzi, kubva NERLYNX (neratinib) mahwendefa (PDF)

 

Zvatingaone Nezvakashata Mhedzisiro yeNeratinib? 

Dhairrhea yakanyanya mushure mekutanga neratinib yakajairika mhedzisiro. Mukuyedzwa kweExteNET, vangangoita makumi mana muzana evakadzi vaibatwa neratatinib vaive nemanyoka akanyanya semhedzisiro.

Mvumo yeDAA inokurudzira kuti loperamide (mazita ezita anosanganisira Imodium, Kaopectate 1-D, uye Pepto Dhijitrosi Kudzora) kupihwa neratinib kwemazuva ekutanga makumi mashanu nematanhatu ekurapa uyezve sezvazvinodiwa kubatsira kubata manyoka.

 

Mimwe mhedzisiro inowanzoitika ye neratinib vari:

▪ kurutsa

▪ kusvotwa

▪ kurwadziwa nemudumbu

▪ kuneta

▪ mapundu

▪ maronda emuromo

 

Muzviitiko zvisingawanzoitiki, neratinib zvinogona kukonzera matambudziko akakomba echiropa. Udza chiremba wako ipapo kana iwe uine chero anotevera zviratidzo zvechiropa matambudziko:

▪ kuita yero kweganda kana kuchena kwemaziso

▪ weti ine rima kana shava

▪ kunzwa kuneta

▪ kushaya nzara

▪ marwadzo kumusoro kwekurudyi kwedumbu

Kubuda ropa kana kupwanya zviri nyore pane zvakajairwa

AASraw ndiye nyanzvi yekugadzira Neratinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo Cont Cont us

 

mhedziso

Iyo FDA tendero yeNeratinib, yemuromo kinase inhibitor, yakaratidza kuwanikwa kweiyo yekutanga yakawedzerwa adjuvant kurapwa sarudzo yevarwere vakakodzera vane yekutanga-nhanho, HER2-yakanaka zamu. kenza. Varwere vane HER2-yakanaka kenza yebonde ndiani akagamuchira neratinib kwegore rimwe yakawana yakanyanya kuvandudzwa 1-gore risingaiti chirwere-chisina kupona ichienzaniswa nevarwere vakagamuchira placebo, mushure memakemikari uye trastuzumab-based adjuvant therapy.

 

Reference

[1] Chan A, Delaloge S, Holmes FA, et al; yeExteNET Yekudzidza Boka. Neratinib mushure trastuzumab-based adjuvant therapy mune varwere vane HER2positive kenza yemazamu (ExteNET): multicentre, randomized, double-blind, placebocontroll, phase 3 kutongwa. Lancet Oncol. 2016; 17: 367-377.

[2] US Kudya neDrug Administration. FDA inobvumidza kurapwa kutsva kudzikisa njodzi yekenza yemazamu inodzoka. Dhinda rekuburitsa. Chikunguru 17, 2017.

[3] Nerlynx (neratinib) mahwendefa [achiisa ruzivo]. Los Angeles, CA: Puma Biotechnology; Chikunguru 2017.

[4] National Cancer Institute. Vakanangwa vamiririri vanoshanda vachipesana neHER2-yakanaka kenza yemazamu: mibvunzo nemhinduro Yakagadziridzwa June 1, 2014. www.cancer.gov/types/breast/research/altto-qa. Yakasvika Nyamavhuvhu 22, 2017.

[5] Singh J, Petter RC, Baillie TA, Whitty A (Kubvumbi 2011). "Kumukazve kwemishonga inodakadza". Kuongorora Kwezvisikwa. Kuwana Zvinodhaka. 10 (4): 307-17. doi: 10.1038 / nrd3410. PMID 21455239. S2CID 5819338.

[6] Minami Y, Shimamura T, Shah K, LaFramboise T, Glatt KA, Liniker E, et al. (Chikunguru 2007). "Iyo mikuru yemapapu-yakatorwa mutant yeEERBB2 iri oncogenic uye inosanganisirwa nekunzwa kune isingachinjiki EGFR / ERBB2 inhibitor HKI-272". Oncogene. 26 (34): 5023-7. doi: 10.1038 / sj.onc.1210292. PMID 17311002.

[7] National Cancer Institute. Kurapwa kenza yemazamu yemurume (PDQ) - hutano nyanzvi vhezheni. Yakagadziridzwa Chivabvu 25, 2017. www.cancer.gov/types/breast/hp/male-breast-treatment-pdq. Yakasvika Nyamavhuvhu 22, 2017.

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