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Neratinib

Rating: Māhele:

ʻO Neratinib kahi mea mana, mea hiki ʻole ke tyrosine kinase inhibitor (TKI) o HER1, HER2, a me HER4, a ke hoʻomohala ʻia nei i kēia manawa. Hoʻopili paʻa ʻole ʻo Neratinib i ka inoa hōʻailona intercellular o HER1, HER2, HER3, a me ka receptor ulu ulu epithelial, a kāpae i ka phosphorylation a me nā HER mau hōʻailona hōʻailona i lalo. Hoʻemi ʻia ka hopena a hoʻonui ʻia ka make o ka cell. Ua hōʻike ʻia nā noiʻi hoʻokolohua ʻo ka pāpā ʻana intracellular o ka hōʻailona HER e neratinib kahi ala ʻoi aku ka maikaʻi o ka kaohi ʻana i ka ulu ulu ulu ʻana o HER a me ka hoʻopio ʻana i nā ʻano hana pakele lele i ʻike ʻia me nā HER2 i hoʻolālā ʻia me nā lāʻau chemotherapeutic.

Product Description

Nā ʻano kikoʻī

Product Name Paukū Neratinib
Kāleka CAS 698387-09-6
Ka Lā Molecular C30H29ClN6O3
Kaumaha Kaumaha 557.04
'O Synonyms HKI-272;

PB272;

Paukū Neratinib;

Nerlynx;

698387-09-6.

Keʻano Keʻokeʻo keʻokeʻo i ka pauka melemele māmā
Ka mālama a me ka lima lima Maloʻo, ʻeleʻele a ma 0 - 4 C no ka wā pōkole (mau lā a i mau pule) a i ʻole -20 C no ka wā lōʻihi (mau mahina i mau makahiki).

 

Neratinib pauka wehewehe

ʻO ka pauma Neratinib, i ʻike ʻia ʻo HKI-272 a i ʻole PB272, kahi mea loaʻa waha, a me ka mea i hiki ʻole ke hoʻoliʻiliʻi o ka HER-2 receptor tyrosine kinase me ka hiki i ka antineoplastic hana.

Hoʻopili ka Neratinib pauma i ka mea loaʻa iā HER-2 i hiki ʻole ke hoʻoliʻiliʻi, a laila e hoʻemi ana i ka autophosphorylation i loko o nā keena, i ʻike ʻia e ke kuhi ʻana i ke koena cysteine ​​i ka ʻeke paʻa paʻa ATP o ka mea loaʻa.

ʻO ka mālama ʻana i nā hunaola me kēia agena ka hopena o ka pāpā ʻana i nā hanana transduction hōʻailona lalo a me nā ala ʻōnaehana pōʻaiapuni paʻa; hopu ʻia ma ka G1-S (Gap 1 / synthese DNA) -ʻāpana o ka hoʻololi o ka mahele o ka ʻāpana. a hōʻemi loa i ka hoʻonui ʻana o ke kelepona.

Hoʻopili pū ka Neratinib pauma i ka ʻepekema ulu uluola epidermal (EGFR) kinase a me ka hoʻonui ʻana o nā hunaola hilinaʻi EGFR.

 

ʻO Neratinib Powder Mekanika o ka Hana

ʻO Neratinib ka paukū kahi mea mana, hiki ʻole ke tyrosine kinase mea hōʻoki (TKI) o HER1, HER2, a me HER4, a ke hoʻomohala ʻia nei i kēia manawa. Hoʻopili paʻa ʻole ʻo Neratinib pauka i ke kikowaena hōʻailona intercellular o HER1, HER2, HER3, a me ka receptor ulu ulu epithelial, a kāpae i nā phosphorylation a me nā ala HER i lalo e hōʻailona ana. Hoʻemi ʻia ka hopena a hoʻonui ʻia ka make o ka cell. Ua hōʻike ʻia nā noiʻi haukapila ke kāohi intracellular o ka hōʻailona HER e ka neratinib pauka he mea ʻoi aku ka maikaʻi o ka kaohi ʻana i ka ulu ulu ulu o HER a me ka hoʻopio ʻana i nā hana pakele lele i ʻike ʻia me nā HER2 i hoʻolālā ʻia a me nā mea chemotherapeutic.

ʻO Neratinib ka paukū kahi mea maikaʻi i ka hoʻomaʻamaʻa laina mua o HER2-positive, metastatic breast cancer (MBC). Ke hoʻohana ʻia me ka paclitaxel, ua hōʻike ka neratinib pauka i kahi ORR o 73%. Ke hoʻohui ʻia me capecitabine, kahi mea chemotherapeutic hou, ʻo ka ORR he 63%. Ma waho aʻe o ka HER2-maikaʻi MBC, ua hoʻohana pono ʻia ka paukū neratinib i nā mea maʻi me ka maʻi maʻi umauma HER2-mutated I ka pae 2 SUMMIT hoʻokolokolo, nā mea maʻi me ka HER2-mutated umauma maʻi 'aʻai i loaʻa i ka 33% ORR ma 8 mau pule.

ʻO ka pauma Neratinib ka TKI mua i hōʻoia e hoʻemi i ka makaʻu no ka hoʻi hou ʻana o ka maʻi i nā mea maʻi me ka maʻi kanulau umauma HER2-maikaʻi ma mua. Ma muli o ka maikaʻi o ka neratinib pauka i ka wā mua o ka maʻi ʻaʻai umauma HER2-maikaʻi, MBC, a me nā tumors HER2-mutant, ke kakali ʻia ka paukū neratinib e lilo i kūlana hou o ka mālama ma nā wahi o ka mālama ʻana i ka maʻi ʻaʻai umauma.

 

Neratinib pauma palapala noi

Hoʻopili ka Neratinib pauma i ka mea loaʻa iā HER-2 i hiki ʻole ke hoʻoliʻiliʻi, a laila e hoʻemi ana i ka autophosphorylation i loko o nā keena, i ʻike ʻia e ke kuhi ʻana i ke koena cysteine ​​i ka ʻeke paʻa paʻa ATP o ka mea loaʻa.

ʻO nā kanesa umauma HER2-maikaʻi e hana i ka nui o ka protein HER2. Noho ka protein HER2 ma luna o nā hunaola maʻi ʻaʻai a loaʻa nā hōʻailona e haʻi i ka maʻi ʻaʻai e ulu a hoʻolaha. Neratinib pauma hakakā me HER2-maikaʻi umauma maʻi 'aʻai ma ka ālai' ana i nā maʻi 'aʻai keena e loaʻa nā hōʻailona hōʻailona.

ʻO Neratinib ka paukū kahi lāʻau hoʻomākaukau ʻia, akā ʻaʻole like me Herceptin (inoa kemika: trastuzumab), Kadcyla (inoa kemika: T-DM1 a i ʻole ado-trastuzumab emtansine), a me Perjeta (inoa kemika: pertuzumab), ʻaʻole ia he lāʻau pale pale pale pale maʻi. ʻO nā ʻōnaehana pale pale Immune nā mana o nā ʻōpala kūlohelohe maoli e hana e like me nā antibodies i hana ʻia e kā mākou ʻōnaehana pale. ʻO ka pauma Neratinib kahi hui kemika, ʻaʻole kahi antibody.

 

Nā hopena ʻaoʻao Neratinib Powder & ʻōlelo aʻoaʻo

Hiki i ka pauma Neratinib ke hana i ka maʻi diarrhea hoʻoweliweli i kekahi poʻe a me ka liʻiliʻi a me ka liʻiliʻi o ka diarrhea ma kahi o nā mea āpau. ʻO ka poʻe e lawe iā ia aia nō ia i ka makaʻu no nā pilikia o ka diarrhea e like me ka make wai a me ke kaulike ʻole electrolyte.

Pēlā nō ka makaʻu o ka hōʻeha nui o ke ake a he nui nā mea maʻi i loaʻa i kekahi pae o ia; ʻo nā hōʻailona o ka hōʻino o ke ake e komo pū me ka luhi, nausea, ka luaʻi, ʻehā o luna quadrant ʻeha a palupalu paha, ke kuni, ka pehu, a me nā kiʻekiʻe o nā eosinophil.

Ma waho aʻe o ka mea i luna, ʻoi aku ma mua o 10% o ka poʻe e lawe ana i ka maʻi heusea, ʻeha o ka ʻōpū, ka luaʻi, ʻeha ma ko lākou lehelehe, huhū ka ʻōpū, hoʻoliʻiliʻi ka makemake, rashes, a me nā spasms muscle.

 

Reference

[1] Xuhong JC, Qi XW, Zhang Y, Jiang J. Mekanism, palekana a me ka pono o ʻekolu mau tyrosine kinase inhibitors lapatinib, neratinib pauma a me pyrotinib i ka maʻi maʻi umauma HER2-maikaʻi. ʻO Am J Cancer Res. 2019 ʻOkakopa 1; 9 (10): 2103-2119. eCollection 2019. Nānā. PubMed PMID: 31720077; PubMed Central PMCID: PMC6834479.

[2] LiverTox: ʻIlikino olakino a me ka ʻikepili noiʻi e pili ana i ka hōʻeha ʻia o ka ate e pili ana i ka lāʻau. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Loaʻa mai http://www.ncbi.nlm.nih.gov/books/NBK548937/ PubMed PMID: 31644242.

[3] Booth LA, Roberts JL, Dent P. Ke kuleana o ka cell signaling i ka crosstalk ma waena o ka autophagy a me ka apoptosis i ka hoʻoponopono ʻana i ke ola ʻana o ka huelo tumora i ka pane ʻana i ka sorafenib a me ka neratinib. ʻO Semin Cancer Biol. 2019 ʻOkakopa 20. pii: S1044-579X (19) 30024-0. hana: 10.1016 / j.semcancer.2019.10.013. [Epub ma mua o ka paʻi] Nānā. ʻO PubMed PMID: 31644944.

[4] Miles J, Keʻokeʻo Y. Neratinib no ka mālama ʻana i ka Early-Stage HER2-Positive Breast Cancer. ʻO J Adv Hoʻolālā Oncol. 2018 Nov-Dec; 9 (7): 750-754. Epub 2018 Nov 1. Loiloi. PubMed PMID: 31249722; PubMed Central PMCID: PMC6570523.

[5] Collins DM, Conlon NT, Kannan S, Verma CS, Eli LD, Lalani AS, Crown J. Preclinical Characteristics o ka Irreversible Pan-HER Kinase Inhibitor Neratinib Hoʻohālikelike ʻia me Lapatinib: Nā hopena no ka mālama ʻana iā HER2-Positive a me HER2- Ka maʻi ʻaʻai ʻo Mutated. Nā Cancers (Basel). 2019 Mei 28; 11 (6). pii: E737. doi: 10.3390 / maʻi ʻaʻai11060737. Loiloi. PubMed PMID: 31141894; PubMed Central PMCID: PMC6628314.

[6] ʻO Deeks ED. Neratinib: ʻĀpono Honua Mua. Nā lāʻau. 2017 ʻOkakopa; 77 (15): 1695-1704. hana: 10.1007 / s40265-017-0811-4. Loiloi. ʻO PubMed PMID: 28884417.

[7] Kourie HR, El Rassy E, Clatot F, de Azambuja E, Lambertini M. Nā lāʻau e kū nei no ka HER2-maikaʻi maikaʻi i ka maʻi ʻaʻai umauma mua: kau i ka neratinib. ʻO Target Onco Ther. 2017 Jul 10; 10: 3363-3372. hana: 10.2147 / OTT.S122397. eCollection 2017. Nānā. PubMed PMID: 28744140; PubMed Central PMCID: PMC5513878.

[8] "Ka wehewehe ʻana o neratinib - National Cancer Institute Drug Dictionary". Ua kiʻi ʻia 1 Kekemapa 2008.

[9] "Neratinib papa inoa lepili" (PDF). ʻO ka US Food and Drug Administration (FDA). Iulai 2017. Ua kiʻi ʻia 6 Pepeluali 2018. No nā mea hou lepili e nānā, ʻaoʻao papa kuhikuhi FDA no NDA 208051 Hoʻohui kēia ʻatikala i nā huaʻōlelo mai kēia kumuwaiwai, aia i ka papa aupuni. Gandhi L, et al. (2017). "MA04.02 Neratinib ± Temsirolimus i nā maʻi maʻi HER2-mutant lung: kahi kūloko, kahi pae II i hoʻopaʻa ʻia". Ka Nūpepa o Thoracic Oncology. 12 (1): S358-9. hana: 10.1016 / j.jtho.2016.11.398.


 

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