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Gefitinib

  1. Chidule cha Gefitinib
  2. Njira ya Gefitinib yogwirira ntchito
  3. Ntchito ya Gefitinib Padziko Lapansi
  4. Zotsatira zoyipa za Gefitinib
  5. Kusungirako kwa Gefitinib
  6. Zowonjezeranso: "Wakupha Khansa Yam'mapapo" Gefitinib

 

Gefitinib mwachidule

Dzina la mankhwala a gefitinib ndi 4-Quinazolinamine N- (3-chloro-4-fluorophenyl) -7-methoxy-6- [3- (4-morpholinyl) propoxy]. Gefitinib ili ndi molekyulu ya C22H24ClFN4O3 , maselo ochepa a ma 446.9 dalton ndipo ndi ufa wonyezimira. Gefitinib ndi maziko aulere. Molekyu ili ndi pKas ya 5.4 ndi 7.2. Gefitinib imatha kufotokozedwa ngati yosungunuka pang'ono pa pH 1, koma imakhala yosasungunuka pamwamba pa pH 7, ndi kusungunuka kumachepa kwambiri pakati pa pH 4 ndi pH 6.M'magulu osungunulira amadzi, gefitinib imasungunuka momasuka mu glacial acetic acid ndi dimethyl sulfoxide, yosungunuka mu pyridine, osungunuka pang'ono mu tetrahydrofuran, komanso osungunuka pang'ono mu methanol, ethanol (99.5%), ethyl acetate, propan-2-ol ndi acetonitrile.

Mapiritsi a Gefitinib amapezeka ngati mapiritsi okutidwa ndi bulauni, okhala ndi 250 mg ya alireza ufa, poyang'anira pakamwa. Zosakaniza zopanda piritsi la mapiritsi a IRESSA ndi lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulphate ndi magnesium stearate. Chovala cha piritsi chimapangidwa ndi hypromellose, polyethylene glycol 300, titaniyamu dioxide, red ferric oxide ndi yellow ferric oxide.

 

Information luso:

dzina Gefitinib
Dzina lokhazikika N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Nambala ya CAS 184475-35-2
Mafananidwe ZD 1839
Molecular Formula Zogwirizana
Kulemera kwa Fomu 446.9
Chiyeretso ≥98%
Kupanga Kristalline olimba
Kutupa DMF: 20 mg / ml
DMSO: 20 mg / ml
DMSO: PBS (pH7.2) (1: 1): 0.5 mg / ml
Mowa: 0.3 mg / ml
SMILES COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
ChiChi Chi 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)
InChi Key XGALLCVXEZPNRQ-UHFFFAOYSA-N
yosungirako -20 ° C

 

Gefitinib imagwiritsidwa ntchito pochiza khansa ya m'mapapo yomwe siying'ono yomwe yafalikira mbali zina za thupi mwa anthu omwe ali ndi zotupa zina. Gefitinib ali mgulu la mankhwala otchedwa kinase inhibitors. Zimagwira ntchito poletsa kuchitapo kanthu mwachilengedwe komwe kumafunikira kuthandizira khansa maselo amachulukana.

AASraw ndiye katswiri wopanga Gefitinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

Gefitinib Njira yogwirira ntchito

Gefitinib ndi choletsa cha epidermal grow factor receptor (EGFR) tyrosine kinase chomwe chimamangiriza ku adenosine triphosphate (ATP) -binding site ya enzyme. EGFR nthawi zambiri imawonetsedwa kuti imakhudzidwa kwambiri ndi maselo ena a carcinoma, monga m'mapapo ndi m'mawere maselo a khansa. Kufotokozera mopitirira muyeso kumayambitsa kukonzanso kwa ma anti-apoptotic Ras sign transcction, zomwe zimapangitsa kuti maselo a khansa apulumuke komanso kuchuluka kwama cell osalamulirika. Gefitinib ndiye woyamba kusankha inhibitor wa EGFR tyrosine kinase yemwe amatchedwanso Her1 kapena ErbB-1. Mwa kuletsa EGFR tyrosine kinase, ma kasinidwe otsika otsika nawonso amaletsedweratu, zomwe zimapangitsa kufalikira kwa maselo owopsa.

 

Gefitinib Gwiritsani Ntchito Padziko Lonse Lapansi

Gefitinib ikugulitsidwa m'maiko opitilira 64. Gefitinib adavomerezedwa ndikugulitsidwa kuyambira Julayi 2002 ku Japan, ndikupanga kukhala dziko loyamba kulowetsa mankhwalawa.

The FDA idavomereza gefitinib mu Meyi 2003 chifukwa cha khansa yaying'ono yamapapo yam'mapapo (NSCLC). Idavomerezedwa ngati monotherapy yothandizira odwala omwe ali ndi NSCLC yakomweko kapena metastatic atalephera kugwiritsa ntchito platinamu komanso docetaxel chemotherapies, ngati njira yachitatu.

Mu June 2005 a FDA adachotsa chilolezo choti agwiritse ntchito odwala atsopano chifukwa chosowa umboni woti watalikitsa moyo.

Ku Europe gefitinib imawonetsedwa kuyambira 2009 mu NSCLC yapamwamba munjira zonse zamankhwala odwala akusintha masinthidwe a EGFR. Chizindikirocho chinaperekedwa pambuyo poti gefitinib yawonetsa ngati njira yoyamba yothandizira kuti pakhale kupulumuka kopanda kupita patsogolo motsutsana ndi boma la platinamu mwa odwala omwe akusintha. IPASS yakhala yoyamba pamayeso anayi a gawo lachitatu kutsimikizira kupambana kwa gefitinib mwa anthu odwalawa.

M'mayiko ena ambiri komwe gefitinib imagulitsidwa pano ndivomerezedwa kwa odwala omwe ali ndi NSCLC yapamwamba omwe adalandirapo kamodzi kamodzi ka chemotherapy. Komabe, ofunsira kukulitsa chizindikiro chake ngati chithandizo chotsatira mwa odwala omwe akusunga kusintha kwa EGFR pakadali pano akukonzekera kutengera umboni waposachedwa wasayansi. [Onaninso] Monga mu Ogasiti 2012 New Zealand idavomereza gefitinib ngati chithandizo choyamba cha odwala omwe ali ndi Kusintha kwa EGFR kwa NSCLC yopanda nzeru yakomweko kapena metastatic, yosasinthika. Izi zimalipilidwa pagulu pamwezi woyamba wa 4 miyezi ndikukhazikitsanso ngati palibe kupita patsogolo.Pa Julayi 13, 2015, a FDA adavomereza gefitinib ngati mankhwala oyamba a NSCLC.

Gefitinib

Zotsatira zoyipa za Gefitinib

Zinthu zofunika kuzikumbukira pazotsatira za gefitinib:

People Anthu ambiri samakumana ndi zovuta zonse zomwe zalembedwa.

Effects Zotsatira zoyipa nthawi zambiri zimadziwikiratu malinga ndi momwe zimayambira komanso kutalika kwake.

Effects Zotsatira zoyipa nthawi zambiri zimasinthidwa ndipo zimatha mankhwala akamaliza.

Are Pali njira zambiri zothandizira kuchepetsa kapena kupewa zovuta zoyipa.

Relationship Palibe mgwirizano pakati pa kupezeka kapena kuopsa kwa zotsatirapo zake ndi mphamvu ya mankhwala.

 

Zotsatira zotsatirazi ndizofala (zomwe zimachitika kuposa 30%) kwa odwala omwe amatenga gefitinib:

♦ Kutsekula m'mimba

Reaction Khungu limachita (zidzolo, ziphuphu)

AASraw ndiye katswiri wopanga Gefitinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

Zotsatirazi ndizotsatira zoyipa zochepa (zomwe zimachitika pafupifupi 10-29%) ya odwala omwe alandila gefitinib:

Ause kunyansidwa

♦ Kusanza

Ching Kuyabwa

♦ Kulakalaka kudya

Kukhumudwa kwa diso

 

Kawirikawiri (pafupifupi 1%) ya zotsatira zoyipa zamatenda am'mapapo (chibayo, kapena kutupa kwa mapapo popanda matenda). Izi zikachitika, nthawi zambiri zimaphatikizana ndi kupuma movutikira ndi chifuwa kapena malungo otsika kwambiri omwe amafunikira kuchipatala. 1/3 mwa milanduyo idabweretsa imfa. Ngati mwadzidzidzi mpweya wochepa, chifuwa ndi / kapena malungo zimachitika mukamamwa gefitinib, dziwitsani akatswiri azachipatala.

Kukwera kwa kuyesa kwa chiwindi (transaminase, bilirubin, ndi alkaline phosphatase) kwawonetsedwa mwa odwala omwe ali ndi gefitinib. Kukwera kumeneku sikunapite limodzi ndi zizindikilo zilizonse za chiwindi cha chiwindi. Komabe, wothandizira zaumoyo wanu angawunike mayeso a magazi kuti muwone momwe chiwindi chanu chimagwirira ntchito nthawi ndi nthawi, pomwe mukumwa gefitinib.

Sizovuta zonse zomwe zalembedwa pamwambapa. Zina zomwe ndizosowa (zomwe zimachitika ochepera 10% ya odwala) sizidalembedwe apa. Komabe, nthawi zonse muyenera kudziwitsa omwe akukuthandizani ngati mukukumana ndi zachilendo.

 

Galireza yosungirako

Sungani gefitinib mu chidebe chomwe chidalowa, chatsekedwa mwamphamvu, komanso chosafikira ana. Sungani pa firiji komanso kutali ndi kutentha ndi kutentha kwambiri (osati kubafa).

Ma gefitinib osafunikira ayenera kutayidwa munjira zapadera zowonetsetsa kuti ziweto, ana, ndi anthu ena sangathe kuwadya. Komabe, simuyenera kutsuka gefitinib iyi mchimbudzi. M'malo mwake, njira yabwino yotayira gefitinib yanu ndi pulogalamu yobwezera mankhwala. Lankhulani ndi wamankhwala wanu kapena lemberani dipatimenti yakunyumba / yobwezeretsanso kwanuko kuti muphunzire zamapulogalamu obwezeretsanso mdera lanu. Onani fayilo ya Kutaya Kwachangu kwa Mankhwala a FDA kuti mumve zambiri ngati mulibe pulogalamu yobwezera.

Ndikofunika kuti mankhwala onse asamaoneke komanso kuti ana azikhala ndi zida zambiri (monga mapiritsi apakati pa mlungu ndi madontho, maso, mavitamini, ndi inhalers) sagonjetsedwa ndi ana ndipo akhoza kuwatsegula mosavuta. Pofuna kuteteza ana aang'ono ku poizoni, nthawi zonse mutseka makapu a chitetezo ndipo nthawi yomweyo perekani mankhwalawa pamalo otetezeka - omwe ali pamwamba ndi kutali ndi osawona ndi kufika.

Gefitinib

Zowonjezeranso: "Wakupha Khansa Yam'mapapo" Gefitinib

Gefitinib ndi buku lothandizira lomwe limalepheretsa tyrosine kinase zochitika za epidermal kukula factor receptor poletsa mpikisano kutchinga tsamba la ATP. M'maphunziro oyeserera gefitinib yawonetsa zochitika zazikulu pamitundu ingapo ya zotupa, kuphatikiza mizere ingapo yama cell am'magazi am'mapapo ndi xenografts. Maphunziro awiri akuluakulu a Phase II (IDEAL 1 ndi IDEAL 2) omwe ali ndi khansa ya m'mapapo yomwe sinatchulidwepo akuti kuchuluka kwa mayankho kumayandikira 20% mwa odwala achiwiri komanso ∼10% mwa omwe amadzipangira mankhwala a chemotherapy awiri kapena kupitilira apo. Kupulumuka kwapakatikati m'maphunziro awiriwa kunayandikira miyezi 6-8. Monga mankhwala oyamba, gefitinib adayesedwa kuphatikiza mitundu iwiri ya chemotherapy m'maphunziro akulu akulu awiri (INTACT 1 ndi INTACT 2). Kafukufuku onsewa adalephera kuwonetsa kusintha kwakupulumuka kwa wodwala okwanira> odwala 1000 paphunziro lililonse. Madera ena omaliza (mwachitsanzo, nthawi yopita patsogolo ndi kuchuluka kwa mayankho) sanasinthidwe ndikuwonjezera kwa gefitinib. Kafukufuku wowonjezerapo akuwonetsedwa kuti awone momwe ntchito ya gefitinib ingathere posamalira odwala omwe adalandira chemotherapy kapena chemoradiotherapy. Kafukufuku wofufuza za gefitinib ngati monotherapy yoyamba amafunikanso.

Odwala ambiri omwe ali ndi khungu laling'ono khansa ya m'mapapo (NSCLC) pamapeto pake imadwala matenda am'mimba kapena matenda omwe sangakhale othandiza kuzithandizo zanyumba zokha ndipo ndiomwe angafune chithandizo chamankhwala. Ngakhale chemotherapy imathandizira kupulumuka kwa odwala omwe ali ndi matenda otsogola, mwayiwo ndi miyezi ∼2 yokha kuposa chisamaliro chothandiza kwambiri, ndipo izi zimawononga zotsatira zoyipa. Kufufuza kwa othandizira atsopano omwe ali ngati chemotherapy koma olekerera bwino ndikofunikira kwambiri. Othandizira angapo omwe amachita motsutsana ndi zosankha zomwe zikupezeka pano khansa maselo, monga epidermal growth factor receptor (EGFR), akuyesedwa ku NSCLC yapamwamba. Pakadali pano, makamaka odwala omwe ali ndi NSCLC otsogola ayesedwa, koma pali chifukwa chabwino chofufuzira ambiri mwa othandizirawa m'matenda am'mbuyomu, pomwe zina mwazovuta zomwe zilipo kale zilipo.

EGFR imafotokozedwa bwino pamatumba olimba osiyanasiyana, kuphatikiza NSCLC. EGFR imafotokozedwa bwino kwambiri (∼80%) yamapapu squamous cell carcinomas, ndipo pafupifupi theka la mapapo adenocarcinomas ndi ma cell-cell carcinomas. Kukhazikitsidwa kwa EGFR m'maselo a khansa kwawonetsedwa kuti ikulimbikitsa njira zomwe zimakhudzana ndi kuchuluka kwa chotupa cha cell, angiogenesis, kuwukira, ndi metastasis, ndikuletsa apoptosis. EGFR (erbB1 kapena HER1) ndi membala wa banja la erbB receptor, lomwe limaphatikizaponso erbB2 (HER2), erbB3 (HER3), ndi erbB4 (HER4). Ndi transmembrane glycoprotein yopangidwa ndi gawo lakunja la ma cell a ligand, cholumikizira ma transmembrane, ndi gawo loyendetsa ma cell opatsirana ndi tyrosine kinase. Pambuyo pomanga thupi lanyama monga epidermal kukula factor, EGFR imachepa ndi monomer wina wa EGFR kapena membala wina wabanja la erbB. Izi zimabweretsa kuyambitsa kwa tyrosine kinase, autophosphorylation ya tyrosine, ndikuyambitsa kuwonetsa ma cascades omwe pamapeto pake amabweretsa mayankho osiyanasiyana kutsika monga kuchuluka kwa ma cell. Kuphatikiza apo, kufotokozera kwa EGFR m'matumbo kumalumikizidwa ndi yankho loipa pamankhwala, chitukuko cha mankhwala osokoneza bongo a cytotoxic, kupitilira kwa matenda, komanso kupulumuka koyenera. Njira zina zowonjezera kuwonjezeka kwa EGFR zomwe zingakhudzidwe ndi kuchuluka kwa chotupa cha cell zimaphatikizapo kuchuluka kwa ma extracellular ligand, heterodimerization of EGFR, ndi EGFR mutation. Mitundu yofala kwambiri ya EGFR yosinthika m'matumba ndi EGFRvIII, yomwe imapezeka mpaka 39% yamilandu ya NSCLC. EGFRvIII imanyamula kusintha kwa amino acid 6 mpaka 273 mdera lomwe limamangiriza ma cell ndikuwonetsa zochitika za tyrosine kinase zomwe sizimayimira pakumangirira kwapadera kwama cell.

AASraw ndiye katswiri wopanga Gefitinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

Reference

[1] Rukazenkov Y, Yankhulani G, Marshall G, et al. Epidermal grow factor receptor tyrosine kinase inhibitors: ofanana koma osiyana? Mankhwala Osokoneza Bongo 2009; 20: 856-866.

[2] Woodburn JR Epidermal kukula factor receptor ndi kuletsa kwake kuchiza khansa. Pharmacol Ther 1999; 82: 241-250.

[3] Gulu Lothandizirana ndi Khansa Yam'mapapo Yaying'ono. Chemotherapy mu khansa yaying'ono yamapapo yam'mapapo: kusanthula meta pogwiritsa ntchito zomwe zasinthidwa kwa wodwala aliyense wazama 52 mayesero azachipatala. BMJ 1995; 311: 899-909.

[4] Douillard JY, Kim ES, Hirsh V, ndi al. Gefitinib (IRESSA) motsutsana ndi docetaxel mwa odwala omwe ali ndi khansa yam'mapapo yam'mapapo kapena yaying'ono yam'mapapo yomwe amathandizidwapo ndi chemotherapy yochokera ku platinamu: kafukufuku wodziwika bwino wa gawo lachitatu (INTEREST). J Wopweteka Oncol 2007; 2: PRS-02 -

[5] Fukuoka M, Wu Y, Thongprasert S, ndi al. Biomarker imawunika kuchokera gawo lachitatu, lotseguka, lotseguka, kafukufuku woyamba wa gefitinib (G) motsutsana ndi carboplatin / paclitaxel (C / P) mwa odwala omwe asankhidwa kuchipatala (pts) omwe ali ndi khansa yaying'ono yaying'ono yamapapo (NSCLC) mu Asia (IPASS). J Clin Oncol 2009; 27 Wothandizira. 15: 8006–.

[6] Reck MA njira yayikulu yothandizira payekhapayekha khansa ya m'mapapo ndi gefitinib: kuyesa kwa IPASS ndi kupitirira. Katswiri Rev Anticancer Ther 2010; 10: 955-965.

[7] Barker, AJ Kafukufuku wopangitsa kudziwika kwa ZD1839 (IRESSA): yogwira pakamwa, yosankha epidermal kukula factor receptor tyrosine kinase inhibitor yolimbana ndi khansa. Zolemba. Med. Chem. Lett. 11, 1911-1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): choletsa pakamwa kuwonetsa kukula kwa khungu komwe kukuwonetsa kuthekera kwa chithandizo cha khansa. Khansa Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Kusokoneza makina owonetsera a ErbB. Wachilengedwe Rev. Cell Biol. 2, 127-137 (2001).

[10] Cersosimo, RJ Khansa ya m'mapapo: kubwereza. Ndine. J. Zaumoyo. Mankhwala. 59, 611-642 (2002).

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