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AASraw inogadzira NMN neNRC powders muhuwandu!

Gefitinib

  1. Gefitinib Ongororo
  2. Gefitinib Maitiro ekuita
  3. Gefitinib Shandisa MuNyika
  4. Side Migumisiro yeGefitinib
  5. Gefitinib Kuchengetedza
  6. More Rearch: "Lung Cancer Muurayi" Gefitinib

 

Gefitinib tsananguro

Iyo kemikari zita re gefitinib iri 4-Quinazolinamine N- (3-chloro-4-fluorophenyl) -7-methoxy-6- [3- (4-morpholinyl) propoxy]. Gefitinib ine molecular fomula C22H24ClFN4O3. , iri hama mamorekuru mashoma e446.9 dalton uye iri chena-chena poda. Gefitinib inzvimbo yemahara. Morekuru rine pKas ye5.4 uye 7.2. Gefitinib inogona kutsanangurwa seyakanyungudika zvishoma paPH 1, asi haina kunyungudika pamusoro pH 7, nekunyungudika kuri kudzikira zvakanyanya pakati pH 4 uye pH 6.Mune isina-aqueous solvents, gefitinib inosununguka zvakasununguka mune glacial acetic acid uye dimethyl sulfoxide, yakasviba mu pyridine, zvishoma zvinogadziriswa mu tetrahydrofuran, uye zvishoma kusungunuka mu methanol, ethanol (99.5%), ethyl acetate, propan-2-ol uye acetonitrile.

Mahwendefa eGefitinib anowanikwa semapiritsi akasviba-akaputirwa nefirimu, ane 250 mg ye gefitinib powder, yekutungamira kwemuromo. Izvo zvisingaite zvigadzirwa zvehwendefa piritsi re IRESSA mahwendefa anonzi lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate uye magnesium stearate. Iyo piritsi yekunamatira inoumbwa ne hypromellose, polyethylene glycol 300, titanium dioxide, tsvuku ferric oxide uye yero ferric oxide.

 

Technical Information:

zita Gefitinib
Zita rakanyorwa N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
CAS Number 184475-35-2
Synonyms ZD 1839
Molecular Formula C22H24ClFN4O3
Formula Weight 446.9
Purity ≥98%
Formulation A crystalline yakasimba
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
InChi 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)
InChi Kiyi XGALLCVXEZPNRQ-UHFFFAOYSA-N
chengetedzo -20 ° C

 

Gefitinib inoshandiswa kurapa isiri-diki kenza yemapapu kenza iyo yakapararira kune zvimwe zvikamu zvemuviri mune vanhu vane mamwe marudzi emamota. Gefitinib iri mukirasi yemishonga inonzi kinase inhibitors. Izvo zvinoshanda nekudzivirira chiito chechimwe chinhu chinowanzoitika chinogona kudikanwa kubatsira kenza masero anowanda.

AASraw ndiye nyanzvi yekugadzira Gefitinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Gefitinib Mechanism of action

Gefitinib is inhibitor yeiyo epidermal kukura factor receptor (EGFR) tyrosine kinase inosunga kune adenosine triphosphate (ATP) - inosunga saiti yeiyo enzyme. EGFR inowanzo kuratidzwa kuve yakanyanyisa kuratidzwa mune mamwe maseru evanhu ecarcinoma, senge mapapu uye zamu kenza masero. Kunyanyisa kuwedzera kunotungamira mukusimudzira mashandisiro eanopokana-apoptotic Ras chiratidzo kutapurirana macashure, zvichizoguma nekuwedzera kupona kwemaseru ekenza uye kusadzora kuwanda kwesero. Gefitinib ndiyo yekutanga inosarudza inhibitor yeEGFR tyrosine kinase iyo inonziwo Her1 kana ErbB-1. Nekudzivirira EGFR tyrosine kinase, iyo yekudzika yekuisa chiratidzo macascades aka dzivirirwawo, zvichikonzera kudzivirirwa kwakaipisisa kwemasero kuwanda.

 

Gefitinib Shandisa Munyika

Gefitinib parizvino iri kutengeswa munyika dzinopfuura makumi matanhatu nematanhatu. Gefitinib yakagamuchirwa uye yakatengeswa kubva muna Chikunguru 64 kuJapan, ichiita nyika yekutanga kupinza mushonga.

The FDA yakatenderwa gefitinib muna Chivabvu 2003 yekenza isiri-diki yemukenza yemapapu (NSCLC) Yakagamuchirwa semonotherapy kurapwa kwevarwere vane yemuno yepamusoro kana metastatic NSCLC mushure mekundikana kweplatinum-based uye docetaxel chemotherapies, seyechitatu-mutsetse kurapwa.

MunaJune 2005 iyo FDA yakabvisa mvumo yekushandisa muvarwere vatsva nekuda kwekushayikwa kweuchapupu hwekuti yakawedzera hupenyu.

MuEurope gefitinib inoratidzirwa kubvira 2009 mune yepamusoro NSCLC mumitsara yese yekurapa kwevarwere vanochengeta shanduko yeEGFR. Chikwata ichi chakapihwa mushure mekuratidzwa kwegefitinib semutsara wekutanga kurapwa kunatsiridza kufambira mberi-kwemahara kurarama pamwe neplatinamu huviri hutongi muvarwere vanochengeta shanduko dzakadai. IPASS yave iri yekutanga yechina yechikamu chechitatu miedzo kuve yakasimbisa gefitinib ukuru mune iyi varwere varwere.

Mune mazhinji eimwe nyika uko gefitinib iri kutengeswa parizvino inogamuchirwa kune varwere vane advanced NSCLC avo vakagamuchira kanenge kamwe kamberi chemotherapy hurumende. Zvisinei, mafomu ekuwedzera zita rayo sechirapa chekutanga mune varwere vanochengeta shanduko yeEGFR parizvino irikuitwa zvichibva pauchapupu hwazvino hwesainzi. EGFR shanduko yevasina ruzivo munharaunda yemhando yepamusoro kana metastatic, isingagadzirisike NSCLC. Izvi zvakabhadharwa pachena kune yekutanga mwedzi-mina temu uye kuvandudzwa kana pasina kufambira mberi.Pana Chikunguru 2012, 4, iyo FDA yakabvumidza gefitinib semutsara wekutanga kurapwa kweNSCLC.

Gefitinib

Side Migumisiro ye Gefitinib

Zvinhu zvakakosha zvekurangarira nezve mhedzisiro ye gefitinib:

♦ Vanhu vazhinji havawani ese emhedzisiro akanyorwa.

♦ Mhedzisiro inowanzo fungidzirwa maererano nekutanga kwavo uye nguva.

♦ Mhedzisiro inowanzo kuve inodzoserwa uye inozopera mushure mekurapwa kwapera.

Pane mikana yakawanda yekubatsira kudzikisira kana kudzivirira mhedzisiro.

Is Hapana hukama pakati pekuvapo kana kuomarara kwemhedzisiro uye kugona kwemushonga.

 

Iyi inotevera mhedzisiro yakajairika (inoitika mune yakakura kupfuura 30%) yevarwere vanotora gefitinib:

♦ Manyoka

Reaction Kugadzirwa kweganda (mapundu, acne)

AASraw ndiye nyanzvi yekugadzira Gefitinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Iyi mhedzisiro haina kujairika mhedzisiro (inoitika mune ingangoita 10-29%) yevarwere vanowana gefitinib:

Ause Nausea

♦ Kusvipa

Ching Itching

Kusadya zvakanaka

Kushatirwa kwemaziso

 

Kazhinji kesi (inenge 1%) yechakakomba divi mhedzisiro yechirwere chemapapu chemukati (pneumonia, kana kuzvimba kwemapapu pasina hutachiona). Kana iri divi mhedzisiro rikaitika, raiwanzoperekedzwa nekufema kunetseka nekukosora kana fivhiri yepasi-inoda inoda kuiswa muchipatara. 1/3 yemakesi anga atungamira kurufu. Kana kamwe kamwe kwekutanga kwekufema kwekufema, kukosora uye / kana fever kunoitika uchitora gefitinib, zivisa nyanzvi yako yehutano.

Kukwidziridzwa kwechiropa basa bvunzo (transaminase, bilirubin, uye alkaline phosphatase) yakaonekwa kune varwere vanorapwa negefitinib. Aya kukwidziridzwa aisaperekedzwa nezviratidzo zvehuturu hwechiropa. Nekudaro, wako wehutano wezvehutano anogona kutarisa bvunzo dzeropa kuti utarise chiropa chako chinoshanda nguva nenguva, paunenge uchitora gefitinib.

Haasi ese mhedzisiro akanyorwa pamusoro. Zvimwe izvo zvisingawanzoitika (zvinoitika mune isingasviki gumi muzana yevarwere) hazvina kunyorwa pano. Nekudaro, iwe unofanirwa kugara uchizivisa mupi wako wezvehutano kana iwe uchinge uchinge uchinge uchinge uchinge uchinge uchinge uchinge uchinge uchinge uchiona zviratidzo

 

Gefitinib chengetedzo

Chengeta gefitinib mumudziyo iyo yakauya mukati, yakasungwa yakavharwa, uye isingasvike kune vana. Zvichengetedze pane tembiricha yemukati uye kure nekupisa kwakanyanya uye hunyoro (kwete muchimbuzi).

Isina kudiwa gefitinib inofanirwa kuraswa nenzira dzakakosha kuona kuti zvipfuyo, vana, uye nevamwe vanhu havagone kuzvidya. Nekudaro, iwe haufanire kuburitsa iyi gefitinib pasi pechimbuzi. Panzvimbo iyoyo, nzira yakanakisa yekurasa yako gefitinib iri kuburikidza neyekurapa-kudzosera chirongwa. Taura nachiremba wako kana kuti taura nedhipatimendi rako remarara / rekudzokorora kuti udzidze nezve zvirongwa zvekudzosa munharaunda yako. Ona iyo FDA's Zvakachengeteka Kubviswa kweMishonga webhusaiti kuti uwane rumwe ruzivo kana iwe usina mukana wekutora kudzoka chirongwa.

Zvakakosha kuchengetedza mishonga yose isingaoneki uye kusvika kune vana semiti yakawanda (yakadai sepiritsi yevhiki nevhiki uye yeavo madonhe emeso, makemikari, makanda, uye inhalers) haisi vana vasingagoneki uye vana vaduku vanogona kuvhura nyore nyore. Kuchengetedza vana vaduku kubva muchetura, nguva dzose chengetedza kuchengetedzwa kwekuchengetedza uye pakarepo ita mishonga munzvimbo yakachengeteka - imwe yakasimuka uye kure uye isati yavaona uye inosvika.

Gefitinib

More Rearch: "Lung Cancer Muurayi" Gefitinib

Gefitinib inyaya yakanangwa kurapwa iyo inotitisa iyo tyrosine kinase chiitiko cheiyo epidermal yekukura factor receptor nekukwikwidza kuvhara iyo ATP inosunga saiti. Mune prelinical zvidzidzo gefitinib yakaratidza chiitiko chakasimba mune akati wandei mamota mamodheru, kusanganisira akati wandei kenza yemapapu maseru mitsara uye xenografts. Zvidzidzo zviviri zvakakura zveChitatu II (IDEAL 1 uye IDEAL 2) mune yakafungidzirwa isiri-diki kenza yemapapu yemapapu yakashuma chiyero chekupindura chinosvika makumi maviri muzana mune yechipiri-varwere varwere uye ∼20% mune avo vanofungidzirwa nemaviri kana anopfuura emakemikari marimeni. Kupona kwepakati mune izvi zviviri zvidzidzo kwakasvika pamwedzi 10-6. Sekutanga-mutsara wekurapa, gefitinib yakaongororwa pamwe chete nemaviri akasiyana chemotherapy regimens mune mbiri huru dzakasarudzika zvidzidzo (INTACT 8 uye INTACT 1). Zvese zvidzidzo zvakatadza kuratidza kuvandudzwa kwekupona pane yakazara murwere yakawedzera ye> 2 varwere mune yega yega kudzidza. Mamwe maperero ekupedzisira (semuenzaniso, nguva yekufambira mberi uye yekupindura mwero) zvakare haina kuvandudzwa nekuwedzera kwegefitinib. Zvimwe zvidzidzo zvinoratidzwa kuti zviongorore zvinogona kuita gefitinib mukuchengetedza kwevarwere vakagamuchira chemotherapy kana chemoradiotherapy. Zvidzidzo zvichiongorora gefitinib seyekutanga-mutsara monotherapy zvakare inodikanwa.

Ruzhinji rwevarwere vane isina-diki sero kenza yemapapu (NSCLC) inozopedzisira yaita chirwere chemastastatic kana chirwere chisingagone kurapwa kwese chete uye vanogona kukwikwidza kurapa kwehurongwa. Kunyangwe chemotherapy ichigona kuvandudza kupona kwevarwere vane chirwere chemberi, mukana wacho unongova ∼2 mwedzi pamusoro pekuchengetwa kwakanyanya, uye izvi zviri pamutengo wemhedzisiro. Kutsvaga kwevamiririri vatsva ayo angangoita senge chemotherapy asi zvirinani kubvumidzwa ndiko kwakanyanya kukosha. Huwandu hwevanoverengeka vamiririri vanoita zvakanangana nekusarudza zvinangwa zviripo kenza masero, senge epidermal kukura factor receptor (EGFR), ari kuyedzwa mune yepamusoro NSCLC. Parizvino, kunyanya varwere vane advanced NSCLC vakaongororwa, asi pane chikonzero chakanaka chekuongorora akati wandei eava vamiririri muzvirongwa zvekutanga zvechirwere, uko zvimwe zvezvakanangana nemagene zvisizvo zviripo.

EGFR inonyanya kuratidzwa mumhando dzakasiyana dzemamota akasimba, kusanganisira NSCLC. EGFR inonyatsoratidzwa mune mazhinji (∼80%) mapapu squamous cell carcinomas, uye ingangoita hafu yemapapu adenocarcinomas uye makuru-maseru carcinomas. Kushanda kweEGFR mumasero emukenza kwakaratidzirwa kusimudzira maitiro anobatanidzwa mune bundu sero kuwanda, angiogenesis, kupinda, uye metastasis, uye kudzivirira apoptosis. EGFR (erbB1 kana HER1) inhengo yemhuri yeerbB yekugamuchira, iyo inosanganisirawo erbB2 (HER2), erbB3 (HER3), uye erbB4 (HER4). Iyo transmembrane glycoprotein inoumbwa nedhiraina-rinosunga dura-rinosunga dura, dura rekuturikidzana, uye chinzvimbo chemukati chesaina-chinodhinda dhizaini ine tyrosine kinase chiitiko. Mushure mekusunga kweiyo yemuviri ligand senge epidermal yekukura chinhu, iyo EGFR inoyerera nechero imwe EGFR monomer kana imwe nhengo yemhuri yeerbB. Izvi zvinotungamira mukumisikidzwa kwe tyrosine kinase, autophosphorylation ye tyrosine, uye kutanga kwekusaina macascades ayo anozopedzisira aunza mhinduro dzakasiyana siyana dzakadzika senge kuwanda kwesero. Uyezve, kutaura kweEGFR mumamota kwave kuchisanganiswa nemhinduro isina kunaka kurapa, kusimudzira kwecytotoxic drug kuramba, kufambira mberi kwezvirwere, uye kurarama kwakashata. Dzimwe nzira dzekuwedzera EGFR chiratidzo chinogona kuve chakabatanidzwa mune bundu sero kuwanda kunosanganisira kuwedzera mazinga e extracellular ligand, heterodimerization yeEGFR, uye EGFR mutation. Iyo yakajairika fomu yekuchinja mutsi EGFR mumamota iEGFRvIII, iyo inowanikwa inosvika makumi matatu nepfumbamwe muzana yeNSCLC kesi. EGFRvIII inotakura deletion mutation kubva kuamino acids 39 kusvika 6 mune yekuwedzera maseru inosunga domain uye inoratidzira inogadzira tyrosine kinase chiitiko icho chakazvimiririra kune yekunze maselular ligand inosunga.

AASraw ndiye nyanzvi yekugadzira Gefitinib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Reference

[1] Rukazenkov Y, Taura G, Marshall G, et al. Epidermal kukura chinhu receptor tyrosine kinase inhibitors: zvakafanana asi zvakasiyana? Anticancer Zvinodhaka 2009; 20: 856-866.

[2] Woodburn JR Iyo epidermal yekukura factor receptor uye yayo inhibition mune cancer cancer. Pharmacol Ther 1999; 82: 241–250.

[3] Isiri-diki Cell Lung Cancer Inobatana Boka. Chemotherapy mune isiri-diki kenza yemapapu kenza: meta-ongororo ichishandisa yakagadziriswa dhata pane mumwe murwere kubva makumi mashanu nemaviri emakiriniki ekuedzwa. BMJ 52; 1995: 311-899.

[4] Douillard JY, Kim ES, Hirsh V, et al. Gefitinib (IRESSA) maringe nedetaetaxel mune varwere vane kenza yemunzvimbo yepamusoro kana metastatic isina-diki kenza yemapapu inotarisirwa kurapwa neplatinamu-yakavakirwa chemotherapy: yakasarudzika, yakavhurika-yekushambadzira chikamu chechitatu kudzidza (INTEREST). J Thoracic Oncol 2007; 2: PRS-02–

[5] Fukuoka M, Wu Y, Thongprasert S, et al. Biomarker inoongorora kubva muchikamu chechitatu, chakasarudzika, chakavhurika-chita, yekutanga-mutsara kudzidza kwe gefitinib (G) maringe ne carboplatin / paclitaxel (C / P) mune varwere vakasarudzwa kiriniki (pts) vane epamberi isiri-diki kenza yemapapu kenza (NSCLC) mu Asia (IPASS). J Clin Oncol 2009; 27 Suppl. 15: 8006–.

[6] Reck MA yakakosha nhanho kune yakasarudzika kurapwa kwekenza yemapapu negefitinib: iyo IPASS kuyedzwa uye kupfuura. Nyanzvi Rev Anticancer Ther 2010; 10: 955-965.

[7] Barker, AJ Zvidzidzo zvinotungamira mukuzivikanwa kweZD1839 (IRESSA): inoshanda nemuromo, inosarudzika epidermal kukura chinhu receptor tyrosine kinase inhibitor yakanangana nekurapa kenza. Bioorg. Med. Chem. Lett. 11, 1911-1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): muromo unoshanda inhibitor wepidermal kukura chinhu chinoratidzira nekwaniso yekenza kurapwa. Cancer Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Kubvisa iyo ErbB yekuratidzira network. Zvisikwa Rev. Mol. Cell Biol. 2, 127-137 (2001).

[10] Cersosimo, RJ Kenza yemapapu: ongororo. Ndiri. J. Hutano Syst. Pharm. 59, 611-642 (2002).

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