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Gefitinib

  1. Kakaretso ea Gefitinib
  2. Mokhoa oa ketso oa Gefitinib
  3. Ts'ebeliso ea Gefitinib Lefatšeng
  4. Litla-morao tsa Gefitinib
  5. Polokelo ea Gefitinib
  6. More Rearch: "Mmolai oa Kankere ea Lung" Gefitinib

 

Gefitinib Overview

Lebitso la lik'hemik'hale la gefitinib ke 4-Quinazolinamine N- (3-chloro-4-fluorophenyl) -7-methoxy-6- [3- (4-morpholinyl) propoxy]. Gefitinib e na le molek'hule ea C22H24ClFN4O3 , boima ba 'mele bo lekanyelitsoeng ba li-dalton tse 446.9 mme ke phofo e' mala o mosoeu. Gefitinib ke setsi sa mahala. Molek'hule e na le pKas ea 5.4 le 7.2. Gefitinib e ka hlalosoa e qhibiliha hanyane ho pH 1, empa ha e qhibilihe kaholimo ho pH 7, 'me ho qhibiliha ho fokotseha haholo lipakeng tsa pH 4 le pH 6.Ho li-solvents tse se nang metsi, gefitinib e qhibiliha ka bolokolohi ka asiti ea glacial le dimethyl sulfoxide, e qhibilihang ka pyridine, e qhibilihang hanyane ka hanyane ho tetrahydrofuran, mme e qhibiliha hanyane ka hanyane ho methanol, ethanol (99.5%), ethyl acetate, propan-2-ol le acetonitrile.

Matlapa a Gefitinib a fumaneha e le matlapa a sootho a koahetsoeng ka filimi, a nang le 250 mg ea sebetse phofo, bakeng sa tsamaiso ea molomo. Lisebelisoa tse sa sebetseng tsa letlapa la matlapa a lipilisi tsa IRESSA ke lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate le magnesium stearate. Sekoahelo sa letlapa se entsoe ka hypromellose, polyethylene glycol 300, titanium dioxide, red ferric oxide le yellow ferric oxide.

 

Information Technical:

lebitso Gefitinib
Lebitso le tloaelehileng N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Nomoro ea CAS 184475-35-2
Li-synonyms EA-1839-ZD
Molecular Formula EA-KO22-C24
Boima ba 'mele 446.9
Ho hloeka ≥98%
paakanyong Kristalline e tiileng
Solubility DMF: 20 mg / ml
DMSO: 20 mg / ml
DMSO: PBS (pH7.2) (1: 1): 0.5 mg / ml
Ethanol: 0.3 mg / ml
SMILES COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
In Code Code InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
Ke senotlolo sa InChi XGALLCVXEZPNRQ-UHFFFAOYSA-N
Storage -20 ° C

 

Gefitinib e sebelisetsoa ho alafa mofetše o seng o monyane oa lisele tsa matšoafo o hasaneng likarolong tse ling tsa 'mele ho batho ba nang le mefuta e itseng ea lihlahala. Gefitinib o sehlopheng sa meriana e bitsoang kinase inhibitors. E sebetsa ka ho thibela ts'ebetso ea ntho e itseng e hlahang ka tlhaho e ka hlokang ho thusa tsoaroa ke kankere lisele lia ikatisa.

AASraw ke moetsi oa litsebi oa Gefitinib.

Ka kopo tlanya mona bakeng sa tlhaiso-leseling e qotsitsoeng: Lethathamo la rona

 

Gefitinib Mokhoa oa ketso

Gefitinib ke sesitisi sa epidermal growth factor receptor (EGFR) tyrosine kinase e tlamang ho adenosine triphosphate (ATP) -binding sa enzyme. EGFR hangata e bonts'oa hore e na le khatello e fetelletseng ea lisele tsa motho ea carcinoma, joalo ka matšoafo le sefuba lisele tsa kankere. Ho hatella maikutlo ho lebisa ho ntlafatseng ts'ebetso ea li-cascades tsa anti-apoptotic Ras signal transduction, tse qetellang li bakile pholoho e eketsehileng ea lisele tsa mofetše le ho ata ha lisele tse sa laoleheng. Gefitinib ke eona khetho ea pele ea khetho ea EGFR tyrosine kinase eo hape e bitsoang Her1 kapa ErbB-1. Ka ho thibela EGFR tyrosine kinase, li-cascade tse tšoaeang tse tlase le tsona lia thibeloa, ho fella ka ho ata ha lisele tse mpe.

 

Gefitinib Sebelisa Lefatšeng

Gefitinib hajoale e rekisoa linaheng tse fetang 64. Gefitinib e ile ea amoheloa mme ea bapatsoa ho tloha ka Phupu 2002 Japane, ea e etsa naha ea pele ho kenya setlhare.

The FDA e amohetse gefitinib ka Mots'eanong 2003 bakeng sa mofets'e o seng o monyane oa lisele tsa kankere ea matšoafo (NSCLC) E ile ea amoheloa e le monotherapy bakeng sa kalafo ea bakuli ba NSCLC e tsoetseng pele kapa ea metastatic kamora ho hloleha ha chemotherapies ea platinamo le docetaxel, e le kalafo ea mohala oa boraro.

Ka Phuptjane 2005 FDA e ile ea tlosa tumello ea ho sebelisoa ho bakuli ba bacha ka lebaka la ho haelloa ke bopaki ba hore e atolositse bophelo.

Europe gefitinib e bonts'oa ho tloha ka 2009 ho NSCLC e tsoetseng pele mekhoeng eohle ea kalafo bakeng sa bakuli ba bolokang liphetoho tsa EGFR. Label ena e fuoe kamora hore gefitinib e bontšoe e le kalafo ea mohala oa pele ho ntlafatsa haholo pholoho e senang tsoelo-pele khahlano le puso e habeli ea platinamo ho bakuli ba bolokang liphetoho tse joalo. IPASS e bile ea pele ho liteko tse 'ne tsa mokhahlelo oa boraro ho netefatsa bophahamo ba gefitinib bathong bana ba mokuli.

Linaheng tse ling tse ngata moo gefitinib e rekisoang hona joale e lumelloa bakeng sa bakuli ba nang le NSCLC e tsoetseng pele ba neng ba fumane bonyane puso e le 'ngoe ea chemotherapy e fetileng. Leha ho le joalo, likopo tsa ho holisa lebitso la eona e le kalafo ea mohala oa pele ho bakuli ba bolokang liphetoho tsa EGFR hajoale li ntse li sebetsoa ho ipapisitsoe le bopaki ba morao-rao ba mahlale. Phetoho ea EGFR bakeng sa NSCLC e sa tsebeng letho ea lehae kapa ea metastatic. Sena se tšehelitsoe phatlalatsa bakeng sa nako ea pele ea likhoeli tse 2012 le nchafatso haeba ho se tsoelo-pele Ka la 4 Phupu, 13, FDA e amohetse gefitinib e le kalafo ea mohala oa pele bakeng sa NSCLC.

Gefitinib

Litla-morao tsa Gefitinib

Lintho tsa bohlokoa tseo u lokelang ho li hopola ka litla-morao tsa gefitinib:

Batho ba bangata ha ba na litla-morao tsohle tse thathamisitsoeng.

Litla-morao hangata li ka tsejoa esale pele ho latela hore na li qala joang le hore na li nka nako e kae.

Litla-morao li lula li khutlisoa hape li tla fela kamora hore kalafo e phethe.

♦ Ho na le likhetho tse ngata ho thusa ho fokotsa kapa ho thibela litla-morao.

Ha ho na kamano lipakeng tsa boteng kapa ho tiea ha litla-morao le katleho ea meriana.

 

Litla-morao tse latelang li tloaelehile (li etsahala ho feta 30%) bakeng sa bakuli ba nkang gefitinib:

♦ Letšollo

Karabelo ea letlalo (lekhopho, makhopho)

AASraw ke moetsi oa litsebi oa Gefitinib.

Ka kopo tlanya mona bakeng sa tlhaiso-leseling e qotsitsoeng: Lethathamo la rona

 

Litla-morao tsena ke litla-morao tse sa tloaelehang (tse etsahalang ka 10-29%) ea bakuli ba fumanang gefitinib:

♦ Ho nyekeloa ke pelo

Ho hlatsa

♦ Ho hlohlona

Takatso e fosahetseng ea lijo

Ho teneha mahlo

 

Maemo a sa tloaelehang (hoo e ka bang 1%) a litlamorao tse mpe tsa lefu la sefuba (pneumonia, kapa ho ruruha ha matšoafo ntle le tšoaetso) Ha litla-morao tsena li etsahala, hangata e ne e tsamaea le ho hema ka thata ka ho khohlela kapa feberu e tlase e hlokang ho kena sepetlele. 1/3 ea linyeoe li ne li lebisitse lefung. Haeba phefumoloho e hlaha ka tšohanyetso, khohlela le / kapa feberu e etsahala ha u ntse u nka gefitinib, tsebisa setsebi sa tlhokomelo ea bophelo bo botle.

Ho phahama ha liteko tsa ts'ebetso ea sebete (transaminase, bilirubin, le alkaline phosphatase) ho bonoe ho bakuli ba alafshoang ka gefitinib. Litekanyetso tsena li ne li sa tsamaee le matšoao afe kapa afe a chefo ea sebete. Leha ho le joalo, setsebi sa hau sa tlhokomelo ea bophelo se ka hlahloba liteko tsa mali ho lekola sebete sa hau nako le nako, ha o ntse o nka gefitinib.

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.

 

Gefitinib Storage

Boloka gefitinib ka setshelong seo e keneng ho sona, e koetsoe ka thata, ebile e sa fihlelehe ho bana. E boloke ka mocheso oa kamore le hole le mocheso o feteletseng le mongobo (eseng ka ntloaneng).

Ha ho hlokahale gefitinib e lokela ho lahloa ka litsela tse ikhethang ho netefatsa hore liphoofolo tse ruuoang lapeng, bana le batho ba bang ba ke ke ba li ja. Leha ho le joalo, ha ua lokela ho tšela gefitinib ena ka tlung ea ntloana. Sebakeng seo, tsela e molemohali ea ho lahla gefitinib ea hau ke ka lenaneo la ho khutlisa moriana. Bua le rakhemisi oa hau kapa ikopanye le lefapha la hau la litšila / la ho li nchafatsa ho ithuta ka mananeo a khutlisetsang sechaba sa heno. Bona file ea FDA's Disposal of Medicines Website bakeng sa tlhaiso-leseling e batsi haeba o sena mokhoa oa ho khutlisa.

Ke habohlokoa ho boloka meriana eohle e sa bonahaleng le ho fihlella ha bana ka lisebelisoa tse ngata (tse kang li-pilisi tsa beke le beke le tsa mahlaseli a mahlo, li-creams le li-inhalers) ha li hane le bana 'me bana ba banyenyane ba ka li bula habonolo. Ho sireletsa bana ba banyenyane hore ba se ke ba chefo, kamehla ba koale likotlolo tsa tšireletso 'me hang-hang ba behe meriana sebakeng se sireletsehileng - e leng holimo le ho tloha mahlong a bona le ho fihla.

Gefitinib

More Rearch: "Mmolai oa Kankere ea Lung" Gefitinib

Gefitinib ke pheko e reretsoeng kalafo e thibelang ts'ebetso ea tyrosine kinase ea epidermal growth factor receptor ka tlholisano ho thibela sebaka se tlamang sa ATP. Lithutong tsa pele ho nako gefitinib e bonts'itse tšebetso e matla mefuteng e mengata ea hlahala, ho kenyeletsoa mela e 'maloa ea lisele tsa mofetše oa matšoafo le xenografts Liphuputso tse peli tse kholo tsa Phase II (IDEAL 1 le IDEAL 2) ho mofets'e o seng o monyane oa lisele tsa matšoafo o tlalehile sekhahla sa karabelo se atamelang 20% ​​ho bakuli ba mola oa bobeli le ∼10% ho ba etsoang pele ka lipilisi tsa chemotherapy tse peli kapa ho feta. Pholoho e bohareng lithutong tsena tse peli e atametse likhoeli tse 6-8. Joaloka kalafo ea mohala oa pele, gefitinib e 'nile ea hlahlojoa e kopantsoe le mefuta e' meli e fapaneng ea chemotherapy lithutong tse peli tse kholo tse hlophisitsoeng (INTACT 1 le INTACT 2). Boithuto boo ka bobeli bo hlotsoe ho bonts'a ntlafatso ea pholoho ka kakaretso ea mokuli ea> bakuli ba 1000 thutong ka 'ngoe. Lintlha tse ling tsa pheletso (mohlala, nako ea tsoelo-pele le sekhahla sa karabelo) le tsona ha lia ntlafatsoa ka ho eketsoa ha gefitinib. Liphuputso tse ling li bonts'oa ho lekola karolo e ka bang teng ea gefitinib tlhokomelong ea bakuli ba fumaneng chemotherapy kapa chemoradiotherapy. Boithuto bo batlisisang gefitinib joalo ka monotherapy ea mohala oa pele le bona boa hlokahala.

Bongata ba bakuli ba nang le lisele tse nyane kankere ea matšoafo (NSCLC) qetellong e ba le lefu la metastatic kapa lefu le ke keng la sebelisoa liphekolo tsa lehae feela ebile e ka ba likhetho tsa kalafo ea sistimi. Le ha chemotherapy e ka ntlafatsa ho phela ho bakuli ba nang le mafu a tsoetseng pele, molemo ke likhoeli tse ∼2 feela ho feta tlhokomelo e molemohali ea ts'ehetso, mme hona ke litšenyehelo tsa litlamorao tse mpe. Ho batlana le mahlahana a macha ao bonyane a sebetsang joaloka chemotherapy empa a mamelleha hamolemo ho bohlokoa haholo. Baemeli ba 'maloa ba lipale ba sebetsang ka kotloloho khahlano le sepheo se khethiloeng se teng ka tsoaroa ke kankere lisele, joalo ka epidermal growth factor receptor (EGFR), li ntse li lekoa NSCLC e tsoetseng pele. Ho fihlela joale, haholo-holo bakuli ba NSCLC e tsoetseng pele ba se ba hlahlobiloe, empa ho na le lebaka le letle la ho fuputsa tse 'maloa tsa mahlahana ana maemong a pejana a lefu, moo a mang a mathata a liphatsa tsa lefutso a seng a ntse a le teng a seng a le teng.

EGFR e hlahisoa haholo ka lihlahala tse tiileng tse fapaneng, ho kenyeletsoa NSCLC. EGFR e hlahisoa haholo ho boholo ba (∼80%) lung squamous cell carcinomas, le hoo e batlang e le halofo ea matšoafo a adenocarcinomas le li-cell carcinomas tse kholo. Ts'ebetso ea EGFR ka lisele tsa mofets'e e bonts'itsoe ho khothaletsa lits'ebetso tse amehang ho ata ha lisele tsa hlahala, angiogenesis, tlhaselo le metastasis le ho thibela apoptosis. EGFR (erbB1 kapa HER1) ke setho sa lelapa la li-erbB receptor, le kenyeletsang erbB2 (HER2), erbB3 (HER3), le erbB4 (HER4). Ke transmembrane glycoprotein e entsoeng ka domain e tlamang ea ligand-extracellular, domain ea transmembrane, le domain-transducing domain e kenang ka har'a cell e nang le ts'ebetso ea tyrosine kinase. Kamora ho tlama ligand ea mmele e joalo ka kholo ea epidermal factor, EGFR e nyenyefala le monomer e mong oa EGFR kapa setho se seng sa lelapa la erbB. Sena se lebisa ho ts'ebetsong ha tyrosine kinase, autophosphorylation ea tyrosine, le ho qala ho tšoaea li-cascades tse qetellang li baka likarabo tse fapaneng tsa noka tse kang ho ata ha sele. Ho feta moo, polelo ea EGFR ka lihlahala e 'nile ea amahanngoa le karabelo e mpe ea kalafo, nts'etsopele ea ts'oaetso ea lithethefatsi ea cytotoxic, tsoelo-pele ea mafu le ho phela hampe. Mekhoa e meng ea ho eketseha ha lets'oao la EGFR e kanna ea ameha keketsehong ea lisele tsa kankere e kenyelletsa maemo a eketsehileng a li-extracellular ligand, heterodimerization ea EGFR le phetoho ea EGFR. Mofuta o tloaelehileng haholo oa EGFR e fetohileng ka har'a lihlahala ke EGFRvIII, e fumanoang ho fihlela ho 39% ea linyeoe tsa NSCLC. EGFRvIII e na le phetoho e tlositsoeng ho tloha ho amino acid 6 ho isa 273 sebakeng se tlamang sa lisele mme e bonts'a ts'ebetso ea tyrosine kinase e ikemetseng ka ntle ho sele e tlamang ea ligand.

AASraw ke moetsi oa litsebi oa Gefitinib.

Ka kopo tlanya mona bakeng sa tlhaiso-leseling e qotsitsoeng: Lethathamo la rona

 

Reference

[1] Rukazenkov Y, Speake G, Marshall G, et al. Epidermal growth factor receptor tyrosine kinase inhibitors: e ts'oanang empa e fapane? Lithethefatsi tsa Anticancer 2009; 20: 856-866.

[2] Woodburn JR Phallo ea li-epidermal factor factor le thibelo ea eona kalafong ea mofets'e. Pharmacol Ther 1999; 82: 241–250.

[3] Sehlopha se Kopaneng sa Kankere ea Lung ea Kankere. Chemotherapy ho mofets'e o seng o monyane oa kankere ea matšoafo: tlhahlobo ea meta e sebelisang lintlha tse ntlafalitsoeng ho bakuli ka bomong ba tsoang litekong tse 52 tsa liteko tsa bongaka. BMJ 1995; 311: 899-909.

[4] Douillard JY, Kim ES, Hirsh V, le al. Gefitinib (IRESSA) khahlanong le docetaxel ho bakuli ba nang le kankere ea matšoafo e seng e nyane ea lehae kapa ea metastatic e alafshoang pele ka chemotherapy e thehiloeng ho platinamo: thuto ea lotho ea phase III (INTEREST). J Thoracic Oncol 2007; 2: PRS-02 -

[5] Fukuoka M, Wu Y, Thongprasert S, et al. Biomarker e sekaseka ho tloha mokhatlong oa III, o hlophisitsoeng ka mokhoa o hlophisehileng, o bulehileng, oa pele oa thuto ea gefitinib (G) khahlanong le carboplatin / paclitaxel (C / P) ho bakuli ba khethiloeng ke lingaka (pts) ba nang le mofets'e o seng o monyane oa lisele tsa kankere ea matšoafo (NSCLC) ho Asia (IPASS). J Clin Oncol 2009; 27 Tlatsetso. 15: 8006–.

[6] Reck MA mohato o moholo oa kalafo ea motho ka mong ea mofets'e oa matšoafo le gefitinib: nyeoe ea IPASS le ho feta. Setsebi Rev Anticancer Ther 2010; 10: 955–965.

[7] Barker, AJ Studies e lebisang ho khethollo ea ZD1839 (IRESSA): e sebetsang ka molomo, e khethollang epidermal factor factor receptor tyrosine kinase inhibitor e lebisitsoeng kalafong ea mofets'e. Bioorg. Med. Khem. Lett. 11, 1911-1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): inhibitor e sebetsang ka molomo ea tšoaetso ea kholo ea tšoaetso e nang le monyetla oa kalafo ea mofets'e. Kankere Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Ho sa ts'oaroe marang-rang a tšoaeang ErbB. Tlhaho Mor. Cell Biol. 2, 127-137 (2001).

[10] Cersosimo, RJ Kankere ea matšoafo: tlhahlobo. Am. J. Bophelo Syst. Pharm. 59, 611-642 (2002).

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