I-Neratinib (698387-09-6) ipowder-Umvelisi weFektri yoMvelisi
I-AASraw ivelisa i-Cannabidiol (CBD) ipowder kunye ne-Hemp ebalulekileyo yeoyile ngobuninzi!

INeratinib

Akukho kalo Udidi:

I-Neratinib yinto enamandla, engenakuphinda ibuye i-tyrosine kinase inhibitor (TKI) ye-HER1, HER2, kunye ne-HER4, kwaye ngoku iphantsi kophuhliso. I-Neratinib ibophelela ngokungenakuphikiswa kwi-domain ye-intercellular signaling domain ye-HER1, HER2, HER3, kunye ne-epithelial growth factor receptor, kwaye inqanda i-phosphorylation kunye neendlela ezininzi zokubonisa ezantsi ze-HER. Iziphumo zinciphise ukwanda kunye nokufa kwesisele. Izifundo zeklinikhi zibonise ukuba inhibition ye-intracellular ye-HER signaling yi-neratinib yeyona ndlela isebenzayo yokucinezela ukukhula kwe-HER-mediated ukukhula kunye noloyiso kwiindlela zokubaleka zethumba ezinamava kunyango olujolise kwi-HER2 kunye neearhente zonyango.

Ingcaciso yeMveliso

Iimpawu ezisisiseko

Igama lemveliso Ineratinib powder
Inani leCAS 698387-09-6
I-Molecular Formula C30H29ClN6O3
Ubukhulu beFormula 557.04
Iintetho ezifanayo HKI-272;

PB272;

iNeratinib powder;

Nerlynx;

698387-09-6.

Kubonakala Ngaphandle komhlophe ukuya kumgubo otyheli okhanyayo
Ukugcina nokuPhatha Okomileyo, omnyama kunye no-0 ukuya ku-4 C okwexesha elifutshane (iintsuku ukuya kwiiveki) okanye -20 C ixesha elide (iinyanga ukuya kwiminyaka).

 

Inkcazo yeNeratinib powder

I-Neratinib powder, ekwabizwa ngokuba yi-HKI-272 okanye i-PB272, yinto ekhoyo ngomlomo, engenakuphinda ibuyiselwe ngaphakathi kwi-HER-2 receptor tyrosine kinase enokubakho kwimisebenzi ye-antineoplastic.

I-Neratinib powder ibopha kwi-HER-2 receptor ngokungenakuphikiswa, ngaloo ndlela kuncitshiswe i-autophosphorylation kwiiseli, ngokucacileyo ngokujolisa kwintsalela ye-cysteine ​​epokothweni yokubopha ye-ATP ye-receptor.

Unyango lweeseli ezinale arhente zikhokelela kuthintelo lweziganeko zokudluliselwa kwesiginali esezantsi kunye neendlela zolawulo lomjikelo weseli; ukubanjwa kwi-G1-S (Gap 1 / DNA synthesis) -isigaba sokutshintsha komjikelo wokwahlula iiseli; kwaye ekugqibeleni kunciphise ukwanda kweselula.

I-Neratinib powder ikwathintela ukukhula kwe-epidermal factor receptor (EGFR) kinase kunye nokwanda kweeseli ezixhomekeke kwi-EGFR.

 

Indlela yeNeratinib Powder yokuSebenza

I-Neratinib powder yinto enamandla, engenakuguqulwa i-tyrosine kinase inhibitor (TKI) ye-HER1, HER2, kunye ne-HER4, kwaye ngoku iphantsi kophuhliso. I-Neratinib powder ibophelela ngokungaguquguqukiyo kwi-domain ye-intercellular signaling domain ye-HER1, HER2, HER3, kunye ne-epithelial ukukhula factor receptor, kwaye inqanda i-phosphorylation kunye neendlela ezininzi zokubonisa ezantsi ze-HER. Iziphumo zinciphise ukwanda kunye nokufa kwesisele. Izifundo zeklinikhi zibonise ukuba inhibition ye-intracellular ye-HER signaling yi-neratinib powder yeyona ndlela isebenzayo yokucinezela ukukhula kwe-HER-mediated ukukhula kunye noloyiso kwiindlela zokubaleka kwethumba ezinamava kunyango olujolise kwi-HER2 kunye neearhente zonyango.

I-Neratinib powder ibonakalise ukuba iyasebenza kunyango lokuqala lwe-HER2-positive, umhlaza webele we-metastatic (MBC). Xa isetyenziswe ngokudibanisa ne-paclitaxel, i-neratinib powder ibonise i-ORR ye-73%. Xa idityaniswe ne-capecitabine, enye i-arhente ye-chemotherapeutic, i-ORR yayiyi-63%. Ukongeza kwi-HER2-positive MBC, i-neratinib powder yayisebenza kakuhle kwizigulana ezinomhlaza webele we-HER2-mutated. Kwisigaba sesi-2 sovavanyo lwe-SUMMIT, izigulana ezinomhlaza webele we-HER2 ziye zafumana i-33% ye-ORR kwiiveki ezisibhozo.

I-Neratinib powder yi-TKI yokuqala engqinayo yokunciphisa umngcipheko wokuphindaphinda kwesifo kwizigulana ezinomhlaza webele we-HER2-positive. Ngokusekwe ekusebenzeni kwe-neratinib powder kwinqanaba lokuqala lomhlaza webele we-HER2, i-MBC, kunye ne-HER2-mutant tumors, i-neratinib powder kulindeleke ukuba ibe ngumgangatho omtsha wokhathalelo kwizicwangciso zonyango lomhlaza wamabele ezininzi.

 

Isicelo se powder seNeratinib

I-Neratinib powder ibopha kwi-HER-2 receptor ngokungenakuphikiswa, ngaloo ndlela kuncitshiswe i-autophosphorylation kwiiseli, ngokucacileyo ngokujolisa kwintsalela ye-cysteine ​​epokothweni yokubopha ye-ATP ye-receptor.

Iimpawu zomhlaza webele ze-HER2 zenza kakhulu iprotein ye-HER2. Iprotein ye-HER2 ihleli kumphezulu weeseli zomhlaza kwaye ifumana imiqondiso exelela umhlaza ukuba ukhule kwaye usasazeke. I-Neratinib powder ilwa nomhlaza webele we-HER2 ngokuthintela amandla eeseli zomhlaza ekufumaneni imiqondiso yokukhula.

I-Neratinib powder yonyango ekujoliswe kulo, kodwa ngokungafaniyo neHerceptin (igama leekhemikhali: trastuzumab), iKadcyla (igama leekhemikhali: T-DM1 okanye i-ado-trastuzumab emtansine), kunye nePerjeta (igama leekhemikhali: pertuzumab), ayilolonyango ekujolise kulo mzimba. Unyango olujolise ekukhuselweni ngumzimba ziinguqulelo zezinto eziphilayo ezenzeka ngokwendalo ezisebenza njengezikhuseli zomzimba ezenziwe ngamajoni ethu omzimba. I-Neratinib powder yinkomfa yeekhemikhali, kungekhona i-antibody.

 

Iziphumo zeNeratinib Powder kunye nesilumkiso

I-Neratinib powder ingabangela isifo sohudo esisongela ubomi kwabanye abantu kunye nesifo sohudo esincinci ukuya kumodareyitha phantse kuwo wonke umntu; abantu abayithathayo basemngciphekweni weengxaki zorhudo njengokungabikho komzimba kunye nokungalingani kwe-electrolyte.

Ngokufanayo kukho umngcipheko wokonakala kwesibindi kwaye izigulana ezininzi zinenqanaba elithile lazo; Iimpawu zomonakalo wesibindi zibandakanya ukukhathala, isicaphucaphu, ukugabha, iintlungu ezikumgangatho ophakamileyo wesithathu okanye ukuthamba, umkhuhlane, irhashalala kunye namanqanaba aphezulu eeosinophil.

Ukongeza koku kungasentla, ngaphezulu kwe-10% yabantu abayithathayo banesicaphucaphu, iintlungu zesisu, ukugabha, izilonda emilebeni, ukukhathazeka esiswini, ukuncipha kokutya, irhashalala kunye nokudumba kwemisipha.

 

isingqiniso

[1] Xuhong JC, Qi XW, Zhang Y, Jiang J. Mechanism, ukhuseleko kunye nokusebenza kwe-tyrosine kinase inhibitors i-lapatinib, i-neratinib powder kunye ne-pyrotinib kwi-HER2-positive cancer cancer. NdinguJ Umhlaza Res. 2019 Oktobha 1; 9 (10): 2103-2119. eCollection 2019. Uphengululo. Ipapashwe kwi-PMID: 31720077; Ipapashwe kwi-PMCID eseMbindini: PMC6834479.

[2] I-LiverTox: Ulwazi lweKlinikhi kunye noPhando ngoKwenzakala kwesibindi [kwi-Intanethi]. I-Bethesda (MD): Iziko leSizwe leSwekile kunye neDigestive kunye neZifo zeZintso; 2012-. Ifumaneka kwi-http: //www.ncbi.nlm.nih.gov/books/NBK548937/ PubMed PMID: 31644242.

[3] I-Booth LA, i-Roberts JL, i-Dent P. Indima yokubonisa iseli kwi-crosstalk phakathi kwe-autophagy kunye ne-apoptosis kulawulo lokusinda kweseli le-tumor ukuphendula i-sorafenib kunye ne-neratinib. Umhlaza weSini seBiol. 2019 Oktobha 20. pii: S1044-579X (19) 30024-0. ikhonkco: 10.1016 / j.semcancer.2019.10.013. [Epub phambi kokuprinta] Uphengululo. I-PMID epapashiweyo: 31644944.

[4] Miles J, White Y. I-Neratinib yonyango lwe-HER2-Positive Cancer Breast. J Igqwetha eliQhelileyo le-Oncol. Ngo-2018 uNov-Dec; 9 (7): 750-754. Epub 2018 Novemba 1. Ukuphononongwa. Ipapashwe kwi-PMID: 31249722; Ipapashwe kwi-PMCID eseMbindini: PMC6570523.

[5] I-Collins DM, i-Conlon NT, i-Kannan S, i-Verma CS, i-Eli LD, i-Lalani AS, i-Crown J. Iimpawu eziphambili ze-Pan-HER Kinase Inhibitor Neratinib xa kuthelekiswa ne-Lapatinib: Iziphumo zoNyango lwe-HER2-Positive kunye ne-HER2- Umhlaza webele oguqulweyo. Umhlaza (iBasel). 2019 ngoMeyi 28; 11 (6). IPH: E737. ikhonkco: 10.3390 / cancerc11060737. Uphononongo. Ipapashwe kwi-PMID: 31141894; Ipapashwe kwi-PMCID eseMbindini: PMC6628314.

[6] Iidiski ze-ED. INeratinib: Ukuvunywa kokuqala kwehlabathi. Iziyobisi. Ngo-2017 Oktobha; 77 (15): 1695-1704. ikhonkco: 10.1007 / s40265-017-0811-4. Uphononongo. I-PMID epapashiweyo: 28884417.

[7] Kourie HR, El Rassy E, Clatot F, de Azambuja E, Lambertini M. Unyango oluvelayo lwe-HER2-intsholongwane yomhlaza webele wokuqala: gxila kwi-neratinib. Iithagethi ze-Onco Ther. Ngo-2017 ngoJulayi 10; 10: 3363-3372. ikhonkco: 10.2147 / OTT.S122397. eCollection 2017. Uphengululo. Ipapashwe kwi-PMID: 28744140; Ipapashwe kwi-PMCID eseMbindini: PMC5513878.

[8] "Inkcazo ye-neratinib - iZiko loMhlaza leSizwe i-Institute of Drug Dictionary". Ukufunyanwa kwe-1 kaDisemba ngo-2008.

[9] "Iitafile zepilisi zeNeratinib" (PDF). Ulawulo lwezoKutya kunye noLawulo lweziyobisi (FDA). NgoJulayi 2017. Ibuyisiwe nge-6 kaFebruwari 2018. Ukuhlaziywa kweelebheli jonga, iphepha lesalathiso le-FDA le-NDA 208051 Eli nqaku libandakanya isicatshulwa esivela kulo mthombo, okwindawo yoluntu. UGandhi L, et al. (2017). "MA04.02 I-Neratinib ± Temsirolimus kwi-HER2-mutant cancer cancer: isifundo samazwe aphesheya, esingahleliwe sesigaba II". Ijenali ye-Thoracic Oncology. I-12 (1): S358-9. ikhonkco: 10.1016 / j.jtho.2016.11.398.