Erlotinib (183321-74-6) phofo - Mofani oa thepa ea moetsi
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Erlotinib

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Erlotinib Powder, e rekisoang tlasa lebitso la lebitso la Tarceva har'a ba bang, ke moriana o sebelisetsoang ho alafa mofetše o seng o monyane oa lisele tsa matšoafo (NSCLC) le mofetše oa pancreatic. Haholo-holo e sebelisetsoa NSCLC e nang le liphetoho liphatseng tsa lefutso tsa li-epidermal factor factor (EGFR) - ekaba phetoho ea 19 exel 19 (del21) kapa exon 858 (LXNUMXR) - e nametseng likarolong tse ling tsa 'mele.

Tlhaloso ea Sehlahisoa

Litšobotsi tsa Motheo

Name Product Erlotinib phofo
Nomoro ea CAS 183321-74-6
Molecular Formula C22H23N3O4
Boima ba 'mele 393.443
Li-synonyms EA-358774;

OSI774;

Erlotinib phofo mahala;

183321-74-6.

Ponahalo Ho soeufetse ho fihlela ho e-na le phofo e tšoeu ea kristale
Ho Boloka le ho Sebetsana E omme, e lefifi ebile e le 0 - 4 C ka nako e khuts'oane (matsatsi ho isa ho libeke) kapa -20 C nako e telele (likhoeli ho isa ho lilemo).

 

Tlhaloso ea phofo ea Erlotinib

Phofo ea Erlotinib, e rekisoang tlasa lebitso la lebitso la Tarceva har'a ba bang, ke moriana o sebelisetsoang ho alafa mofetše o seng o monyane oa lisele tsa matšoafo (NSCLC) le mofetše oa pancreatic. Haholo-holo e sebelisetsoa NSCLC e nang le liphetoho liphatseng tsa lefutso tsa li-epidermal factor factor (EGFR) - ekaba phetoho ea 19 exel 19 (del21) kapa exon 858 (LXNUMXR) - e nametseng likarolong tse ling tsa 'mele. E nkoa ka molomo.

Erlotinib phofo ke sehlahisoa sa quinazoline se nang le thepa ea antineoplastic. Ho qothisana lehlokoa le adenosine triphosphate, phofo ea erlotinib e tlamahane le sehlahisoa sa li-intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, ka hona e thibela phosphorylation ea EGFR le ho thibela liketsahalo tsa phetisetso ea matšoao le litlamorao tsa tumorigenic tse amanang le ts'ebetso ea EGFR.

Phofo ea Erlotinib e ile ea amoheloa bakeng sa ts'ebeliso ea bongaka United States ka 2004. E lethathamong la Meriana ea Bohlokoa ea Mokhatlo oa Lefatše oa Bophelo, e thathamisang meriana e bolokehileng le e sebetsang ka ho fetisisa e hlokahalang tsamaisong ea bophelo bo botle.

 

Mokhoa oa Ketso oa Phofo ea Erlotinib

Erlotinib phofo ke epidermal growth factor receptor inhibitor (EGFR inhibitor). Lithethefatsi li latela Iressa (gefitinib), eo e neng e le sethethefatsi sa pele sa mofuta ona.

Phofo ea Erlotinib e shebile haholo-holo epidermal growth factor receptor (EGFR) tyrosine kinase, e hlahisoang haholo le ho fetoha ka linako tse ling ka mefuta e fapaneng ea mofets'e. E tlama ka mokhoa o ka khutlisoang ho saete e tlamang ea adenosine triphosphate (ATP) ea seamoheli. Bakeng sa ho fetisoa ha lets'oao, limolek'hule tse peli tsa EGFR li hloka ho kopana ho etsa homodimer.

Tsena li sebelisa molek'hule ea ATP ho fetisetsa phosphorylate e mong ho e mong masaleng a tyrosine, a hlahisang masala a phosphotyrosine, ho thaotha liprotheine tse tlamang phosphotyrosine ho EGFR ho kopanya li-protein tse fetisang lipontšo tsa lipontšo mokokotlong kapa ho kenya tšebetsong tse ling lisele tsa biochemical. Ha phofo ea erlotinib e tlama ho EGFR, ha ho khonehe ho theha masala a phosphotyrosine ho EGFR mme likhakanyo tsa matšoao ha li qaloe.

Phofo ea Erlotinib hape ke tyrosine kinase receptor inhibitor e sebelisitsoeng kalafong ea mofets'e o tsoetseng pele kapa metastatic pancreatic kapa e seng e nyane ea mofetše oa lisele tsa matšoafo. Phekolo ea phofo ea Erlotinib e amahanngoa le ho phahama ha nakoana maemong a serum aminotransferase nakong ea kalafo le maemong a sa tloaelehang a ho lemala hampe hoa sebete.

 

Kopo ea Erlotinib Powder 

Erlotinib phofo ke moloko oa pele oa receptor tyrosine kinase inhibitor (hammoho le Gefitinib) e sebetsang haholo ho epidermal growth factor receptor (EGFR), setho sa lelapa la ErbB receptor. Lithethefatsi li sebelisana le mofuta oa hlaha le phetoho ea EGFR. Lelapa la ErbB le ka theha li-homodimers kapa li-heterodimers, tse atisang ho ameha litlamorao tse tlase le pathogenesis ea mefuta e mengata ea li-carcinomas tse ithutiloeng bathong. Receptor tyrosine kinase inhibitors (TKI) e thibela phosphorylation ea substrate ea bona tseleng e supang sele. EGFR hangata e bapala karolo mesebetsing e mengata ea lisele, ho kenyelletsa phapang, keketseho le angiogenesis, tseo kaofela e leng matšoao a mofets'e.

Phetoho ea EGFR ho NSCLC hangata ke phetoho e sebetsang. Litšobotsi tse ling tsa mamello tse etsang hore boteng ba phetoho ea EGFR li se ke tsa kenyelletsa nalane ea ho tsuba e netefalitseng adenocarcinoma ka tlhahlobo ea histologic, morabe oa Asia le bong ba basali. Liphetoho tsa bobeli ho EGFR li etsahala hangata, tseo sengoloa sena se li hlalositseng ka tlase.

 

Litla-morao tsa Erlotinib Powder & Temoso

Litla-morao tse latelang li atile ho bakuli ba nkang Powder ea Erlotinib:

▪ Lehare

▪ Letšollo

▪ Ho hloka takatso ea lijo

▪ Mokhathala

▪ Phefumoloho e khutšoanyane

▪ Khohlela

▪ Ho nyekeloa le pelo le ho hlatsa

 

Litla-morao tsena ha li atisehe haholo ho bakuli ba fumanang phofo ea Erlotinib:

▪ Tšoaetso

▪ Liso tsa molomo

▪ Ho hlohlona

▪ Letlalo le omeletseng

▪ Ho teneha mahlo

▪ Ho opeloa ke mpa

 

Ha se litla-morao tsohle tse thathamisitsoeng kaholimo. Tse ling tse sa tloaelehang (tse etsahalang ka tlase ho 10% ea bakuli) ha li thathamisitsoe mona. Leha ho le joalo, o lokela ho tsebisa mofani oa tlhokomelo ea bophelo ba hau kamehla haeba u ba le matšoao a sa tloaelehang.

 

Reference

[1] Gao JW, Zhan P, Qiu XY, Jin JJ, Lv TF, Song Y. Erlotinib-based doublet targeted therapy versus erlotinib powder feela ho kankere ea matšoafo e seng e nyane ea matšoafo e ileng ea phekoloa pele liteko tse laoloang. Oncotarget. 24 Mots'eanong 2017; 31 (8): 42-73258. doi: 73270 / oncotarget.10.18632. eCollection 18319 Sep 2017. Tlhahlobo. E fetotsoe PMID: 22; E fetotsoe PMCID e bohareng: PMC29069867.

[2] Lee CK, Davies L, Wu YL, Mitsudomi T, Inoue A, Rosell R, Zhou C, Nakagawa K, Thongprasert S, Fukuoka M, Lord S, Marschner I, Tu YK, Gralla RJ, Gebski V, Mok T , Yang JC. Gefitinib kapa Erlotinib powder vs Chemotherapy bakeng sa Kankere ea Lung ea Phetoho ea 'mele ea EGFR: Boitsebiso ba Mokuli ka bomong Meta-Analysis ea Ho Pholoha ka Kakaretso. J Natl Kankere Inst. Ka 2017 Jun 1; 109 (6). doi: 10.1093 / jnci / djw279. Hlahloba. E hatisitsoe PMID: 28376144.

[3] Yang Z, Hackshaw A, Feng Q, Fu X, Zhang Y, Mao C, Tang J. Papiso ea gefitinib, phofo ea erlotinib le afatinib ka mofets'e o seng o monyane oa kankere ea matšoafo: Tlhatlhobo ea meta. Kankere ea Int J. Kajeno Jun 2017; 15 (140): 12-2805. doi: 2819 / ijc.10.1002. Epub 30691 Mar 2017. Hlahloba. E fetotsoe PMID: 27.

[4] "Erlotinib powder (Tarceva) Sebelisa Nakong ea Bokhachane". Lithethefatsi.com. 1 Pulungoana 2019. E khutlisitsoe ka la 23 Tšitoe 2019.

[5] "Erlotinib phofo Monograph bakeng sa Litsebi". Lithethefatsi.com. E khutlisitsoe ka la 12 Pulungoana 2019.

[6] “Letlapa la Tarceva-erlotinib powder hydrochloride”. DailyMed. La 12 Tšitoe 2018. E khutlisitsoe ka la 23 Tšitoe 2019.

[7] "Sephutheloana sa Kamohelo ea Lithethefatsi: Tarceva (Erlotinib phofo) NDA # 021743". Tsamaiso ea Tsamaiso ea Lijo le Lithethefatsi ea US (FDA). La 28 Hlakubele 2005. E khutlisitsoe ka la 23 Tšitoe 2019.

[8] Raymond E, Faivre S, Armand JP (2000). "Epidermal growth factor receptor tyrosine kinase e le sepheo sa kalafo ea anticancer". Lithethefatsi. 60 Tlatsetso ea 1: 15-23, puisano 41-2. doi: 10.2165 / 00003495-200060001-00002. PMID 11129168. S2CID 10555942.