Cikakken Gabatarwa akan "Ciwon Cutar Sankara" Gefitinib @media kawai allo da (-Webkit-min-na'urar-pixel-rabo: 1.5), kawai allo da (-mo-min-na'urar-pixel-rabo: 1.5), kawai allo da (-o-min-na'urar-pixel-pixel -ratio: 3/2), kawai allon da (min-na'urar-pixel-rabo: 1.5) {}
AASraw yana samar da NMN da NRC foda a cikin girma!

Gefitinib

  1. Bayanin Gefitinib
  2. Gefitinib Tsarin aikin
  3. Amfani da Gefitinib A Duniya
  4. Gurbin Gefitinib
  5. Ma'ajin Gefitinib
  6. Rearin Bincike: "Kashewar Ciwon Cutar Huhu" Gefitinib

 

Gefitinib Overview

Gefitinib shine mai hana kinase. Sunan sinadarin gefitinib shine 4-Quinazolinamine N- (3-chloro-4-fluorophenyl) -7-methoxy-6- [3- (4-morpholinyl) propoxy] .Gefitinib yana da tsarin kwayoyin C22H24ClFN4O3 , dangin kwayoyin dangi na dalton 446.9 kuma yana da farar launi mai launi. Gefitinib tushe ne na kyauta. Kwayar tana da pKas na 5.4 da 7.2. Gefitinib ana iya bayyana shi azaman mai saurin narkewa a pH 1, amma kusan ba za'a iya narkewa sama da pH 7 ba, tare da warwarewar yana raguwa sosai tsakanin pH 4 da pH 6. A cikin abubuwan da ba na ruwa ba, gefitinib yana da narkewa cikin yardar kaina a cikin acetic acid da dimethyl sulfoxide, mai narkewa a cikin pyridine, mai narkewa cikin tetrahydrofuran, da ɗan narkewa cikin methanol, ethanol (99.5%), ethyl acetate, propan-2-ol da acetonitrile.

Ana samun allunan Gefitinib azaman allunan da aka ruɓe da fim ɗin launin ruwan kasa, dauke da 250 MG na gefitinib foda, don maganganun baka. Abubuwan da basa aiki na asalin kwamfutar hannu na allunan IRESSA sune lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate da magnesium stearate. Rufin kwamfutar hannu ya ƙunshi hypromellose, polyethylene glycol 300, titanium dioxide, jan ferric oxide da rawaya ferric oxide.

 

Technical Information:

sunan Gefitinib
Formal Name N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
CAS Number 184475-35-2
nufin abu ɗaya ne ZD 1839
kwayoyin Formula C22H24JgFN4O3
Formula Weight 446.9
tsarki ≥98%
Halitta Kyakkyawan crystalline
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
Code InChi 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)
Maɓallin InChi XGALLCVXEZPNRQ-UHFFFAOYSA-N
Storage -20 ° C

 

Ana amfani da Gefitinib don magance ƙananan ƙwayoyin cuta na huhu wanda ya bazu zuwa wasu sassan jiki a cikin mutanen da ke da wasu nau'ikan ciwace-ciwace. Gefitinib yana cikin aji na magungunan da ake kira kinase inhibitors. Yana aiki ta hanyar toshe aikin wani abu wanda yake faruwa da shi wanda ake buƙata don taimakawa ciwon daji Kwayoyin suna ninka.

AASraw shine ƙwararren masanin masana'antar Gefitinib.

Da fatan za a danna nan don bayanin zance: Saduwa da mu

 

Gefitinib Tsarin aikin

Gefitinib shine mai hana mai karɓar haɓakar haɓakar epidermal factor (EGFR) tyrosine kinase wanda ke ɗaura ga adenosine triphosphate (ATP) -naganin haɗin enzyme. Ana nuna EGFR sau da yawa ana nuna shi fiye da kima a cikin wasu ƙwayoyin cututtukan mutum, kamar huhu da nono ciwon daji. Yawan nuna damuwa yana haifar da ingantaccen kunnawa na cascades na anti-apoptotic Ras siginar transcadction, wanda daga baya ya haifar da ƙarin rayuwa na ƙwayoyin ƙwayoyin cuta da yaduwar kwayar halitta. Gefitinib shine mai hana zaɓin farko na EGFR tyrosine kinase wanda kuma ake kira Her1 ko ErbB-1. Ta hanyar hana EGFR tyrosine kinase, ana kuma hana cascades na alamar zuwa ƙasa, wanda hakan ya haifar da hana yaduwar ƙwayoyin cuta.

 

Gefitinib Yi Amfani A Duniya

Gefitinib a yanzu ana kasuwanci a cikin sama da ƙasashe 64. An amince da sayar da Gefitinib kuma an tallata shi daga watan Yulin 2002 a Japan, wanda hakan ya sanya ta zama kasa ta farko da ta shigo da maganin.

The FDA ta amince gefitinib a cikin Mayu 2003 don ƙananan ƙwayar cutar huhu (NSCLC) .An yarda da shi azaman kulawa don kula da marasa lafiya tare da ci gaban gida ko NSCLC mai haɗari bayan gazawar duka magungunan platinum da docetaxel chemotherapies, azaman hanyar layin na uku.

A watan Yunin 2005 FDA ta janye amincewa don amfani da sababbin marasa lafiya saboda rashin hujja cewa ta tsawaita rayuwa.

A cikin Turai gefitinib an nuna shi tun daga 2009 a cikin NSCLC na ci gaba a cikin dukkan layukan magani don marasa lafiya da ke ɗaukar maye gurbin EGFR. An ba da wannan alamar bayan gefitinib da aka nuna a matsayin magani na farko don inganta ci gaban rayuwa ba tare da ci gaba ba tare da tsarin rubin biyun roba a cikin marasa lafiya masu ɗaukar irin wannan maye gurbi. IPASS shine farkon farkon gwaji huɗu na III don tabbatar da ƙimar gefitinib a cikin wannan haƙuri.

A mafi yawan sauran ƙasashe inda ake cinikin gefitinib a halin yanzu an yarda da shi ga marasa lafiya tare da NSCLC na ci gaba waɗanda suka karɓi aƙalla tsarin kula da cutar shan magani na baya. Koyaya, aikace-aikace don faɗaɗa lakabinsa azaman magani na layin farko a marasa lafiya dake ɗaukar maye gurbi na EGFR a halin yanzu ana aiwatar dasu bisa ga sabbin shaidun kimiyya. [Faɗar da ake bukata] Kamar yadda a watan Agusta 2012 New Zealand ta amince gefitinib a matsayin magani na farko don marasa lafiya tare da EGFR maye gurbi don ƙarancin ci gaban gida ko metastatic, wanda ba za a iya tantancewa ba NSCLC. An ba da kuɗin wannan a bainar jama'a don wa'adin watanni 4 na farko da sabuntawa idan babu ci gaba. A ranar 13 ga Yulin, 2015, FDA ta amince gefitinib a matsayin magani na farko na NSCLC.

Gefitinib

Tasirin Side of Gefitinib

Muhimmin abubuwa don tunawa game da tasirin gefitinib:

♦ Mafi yawan mutane basu dandana duk illolin da aka lissafa.

Effects Tasirin sakamako sau da yawa ana iya fa'idarsa dangane da farkonsu da tsawonsu.

Effects Illolin lalacewa kusan akasari ana juyawa kuma zasu tafi bayan an kammala jiyya.

Akwai zaɓuɓɓuka da yawa don taimakawa rage ko hana illa.

Babu wata dangantaka tsakanin kasancewar ko tsananin tasirin illa da tasirin maganin.

 

Abubuwa masu zuwa na yau da kullun sune (faruwa a cikin sama da 30%) ga marasa lafiya masu shan gefitinib:

Arrhea Gudawa

Reaction Skin dauki (kurji, kuraje)

AASraw shine ƙwararren masanin masana'antar Gefitinib.

Da fatan za a danna nan don bayanin zance: Saduwa da mu

 

Wadannan illolin sune cututtukan lalacewa marasa mahimmanci (wanda ke faruwa a kusan 10-29%) na marasa lafiya waɗanda ke karɓar gefitinib:

♦ Ciwan mara

♦ Amai

Yin ƙaiƙayi

Ite Rashin cin abinci

Ation Ciwon ido

 

Areananan lamura (game da 1%) na mummunan sakamako na cututtukan huhu na tsakiya (ciwon huhu, ko kumburin huhu ba tare da kamuwa da cuta ba). Lokacin da wannan tasirin ya faru, yakan kasance tare da wahalar numfashi tare da tari ko ƙananan zazzabi mai buƙatar asibiti. 1/3 na shari'o'in sun kai ga kisa. Idan farawan gajeren numfashi, tari da / ko zazzaɓi farat ɗaya yayin shan gefitinib, sanar da ƙwararren mai kula da lafiyar ku.

Hawan cikin gwajin aikin hanta (transaminase, bilirubin, da alkaline phosphatase) an lura da marasa lafiyar da aka yiwa maganin gefitinib. Wadannan tsawan ba su kasance tare da wasu alamun cututtukan hanta ba. Koyaya, ƙwararren masanin lafiyar ku na iya bincika gwajin jini don saka idanu aikin hanta lokaci-lokaci, yayin da kuke shan gefitinib.

Ba duk larurar illa bace aka lissafa a sama. Wasu waɗanda ba safai ba (waɗanda ke faruwa a ƙasa da 10% na marasa lafiya) ba a lissafa su a nan ba. Koyaya, koyaushe yakamata ku sanar da mai ba ku kiwon lafiya idan kun fuskanci wasu alamomi na al'ada.

 

Gefitinib Storage

A kiyaye gefitinib a cikin akwatin da ya shigo, a rufe sosai, kuma daga inda yara zasu isa. Ajiye shi a zafin jiki na ɗaki kuma nesa da yawan zafin rana da danshi (ba cikin gidan wanka ba).

Ya kamata a zubar gefitinib marasa amfani ta hanyoyi na musamman don tabbatar da cewa dabbobin gida, yara, da sauran mutane ba za su iya cinye su ba. Koyaya, bai kamata ku zubar da wannan gefitinib ɗin a bayan gida ba. Madadin haka, hanya mafi kyau don zubar gefitinib shine ta hanyar shirin dawo da magunguna. Yi magana da likitan ka ko ka tuntuɓi sashen shara / sake amfani da shara don sanin shirye-shiryen dawo da martabar ku a cikin al'ummarku. Duba Kasuwancin FDA na Yanar Gizo mai lafiya don ƙarin bayani idan ba ku da damar shirin karɓar kuɗi.

Yana da muhimmanci a kiyaye dukkan maganin da ba a gani da kuma isa ga yara kamar kwantena da yawa (irin su jariri da kullun mako daya da wadanda ke da idanu, creams, patches, and inhalers) ba su da yarinya kuma yara masu iya buɗe su sauƙi. Don kare yaran yara daga guba, kulle kullun lafiya kuma sanya wuri a cikin wuri mai aminci - wanda ke sama da tafi da kuma daga idanunsu kuma ya isa.

Gefitinib

Rearin Bincike: "Kashewar Ciwon Cutar Huhu" Gefitinib

Gefitinib wani sabon salo ne da aka tsara wanda yake hana aikin tyrosine kinase na mai karɓar haɓakar haɓakar epidermal ta hanyar toshe shafin haɗin ATP cikin gasa. A cikin karatu na yau da kullun gefitinib ya nuna aiki mai ƙarfi a cikin wasu nau'o'in ƙwayoyin cuta, ciki har da layukan ƙwayoyin sankara da huhu da yawa da kuma wasu abubuwa. Manyan manyan karatuttukan karatun II na II (IDEAL 1 da IDEAL 2) a cikin waɗanda ba a kula da ƙananan ƙwayoyin cuta na huhu sun ba da rahoton ƙimar mayar da martani da ke zuwa 20% a cikin marasa lafiya na layin na biyu da ∼10% a cikin waɗanda aka yi wa maganin hana shan magani biyu ko fiye. Rayuwa matsakaiciya a cikin waɗannan karatun biyu sun kusanci watanni 6-8. A matsayin hanyar layin farko, an kimanta gefitinib a haɗe tare da wasu nau'ikan tsarin kimoterapi guda biyu a cikin manyan karatun bazuwar guda biyu (INTACT 1 da INTACT 2). Dukkanin karatun biyu sun kasa nuna ci gaba a rayuwa kan adadin marasa lafiya> 1000 marasa lafiya a kowane binciken. Sauran abubuwan ƙarshen (misali, lokaci don ci gaba da ƙimar amsawa) suma ba a inganta su ba ta ƙarin gefitinib. Arearin karatu ana nuna su don tantance yuwuwar rawar gefitinib wajen kula da marasa lafiyar da suka karɓi cutar sankara ko chemoradiotherapy. Nazarin binciken gefitinib kamar yadda ake buƙatar monotherapy na farko.

Yawancin marasa lafiya da ƙananan ƙwayoyin cuta kwayar cutar huhu (NSCLC) daga ƙarshe ya haifar da cututtukan ƙwayar cuta ko cutar da ba za a iya yarda da ita ga hanyoyin kwantar da hankali na cikin gida kawai ba kuma suna da damar yin takara don hanyoyin kwantar da hankali. Kodayake jiyyar cutar sankara na iya inganta rayuwa a cikin marasa lafiya da cutar ta ci gaba, fa'idar kawai months2 ne kawai bisa mafi kyawun kulawa, kuma wannan yana cikin tsada mai tasiri. Neman sababbin wakilai waɗanda aƙalla suke aiki kamar maganin ƙwaƙwalwa amma an fi jurewa yana da mahimmancin gaske. Da yawa daga cikin wakilan wakili wadanda suke aiki musamman akan wadanda aka zaba wadanda aka gabatar ciwon daji sel, kamar mai karɓar haɓakar haɓakar epidermal (EGFR), ana gwada su a cikin NSCLC na ci gaba. Ya zuwa yanzu, akasarin marasa lafiya masu cutar NSCLC an tantance su, amma akwai kyakkyawar ma'ana don bincika da yawa daga cikin waɗannan wakilai a cikin cututtukan da suka gabata, inda wasu cututtukan ƙwayoyin cuta da aka yi niyya suka kasance.

EGFR an bayyana shi sosai a cikin nau'o'in ƙwayoyi masu ƙarfi, gami da NSCLC. EGFR an bayyana shi sosai a cikin mafi yawan (∼80%) ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin ƙwayoyin cuta, da kusan rabin rabin adenocarcinomas na huhu da kuma manyan ƙwayoyin-carcinomas. Kunna EGFR a cikin ƙwayoyin cutar kansa an nuna don inganta hanyoyin da ke tattare da haɓakar ƙwayar tumo, angiogenesis, mamayewa, da metastasis, da hana apoptosis. EGFR (erbB1 ko HER1) memba ne na gidan mai karɓar erbB, wanda ya haɗa da erbB2 (HER2), erbB3 (HER3), da erbB4 (HER4). Yana da glycoprotein mai yaduwa wanda aka hada shi da wani yanki mai hade da ligand, yankin transmembrane, da kuma siginar intracellular wanda ke haifar da aikin tyrosine kinase. Bayan ɗaura nauyin jijiyoyin jiki kamar su haɓakar haɓakar epidermal, EGFR ya daidaita tare da ko wani monomer EGFR ko wani memba na gidan erbB. Wannan yana haifar da kunnawa na tyrosine kinase, autophosphorylation na tyrosine, da ƙaddamar da sigar katako wanda hakan zai haifar da martani daban-daban kamar yaduwar kwayar halitta. Bugu da ƙari, bayanin EGFR a cikin ciwace-ciwacen ƙwayoyi yana da alaƙa da mummunan amsawa ga farfadowa, haɓaka haɓakar ƙwayoyin cytotoxic, ci gaban cuta, da rayuwa mara kyau. Sauran hanyoyin samar da siginar EGFR wanda zai iya shiga cikin yaduwar kwayar halitta ya hada da karuwar matakan ligandal da ke ciki, heterodimerization na EGFR, da maye gurbin EGFR. Mafi yawan nau'ikan nau'ikan maye gurbi na EGFR a cikin ciwace-ciwacen shine EGFRvIII, wanda aka samo shi har zuwa 39% na shari'o'in NSCLC. EGFRvIII yana ɗaukar maye gurbi daga amino acid 6 zuwa 273 a cikin yanki mai ɗaurewa kuma yana nuna babban aikin tyrosine kinase wanda yake zaman kansa ne daga ɗaurin haɗin liginal extracellular.

AASraw shine ƙwararren masanin masana'antar Gefitinib.

Da fatan za a danna nan don bayanin zance: Saduwa da mu

 

reference

[1] Rukazenkov Y, Magana G, Marshall G, et al. Epidermal girma factor receptor tyrosine kinase hanawa: kama amma daban-daban? Magungunan Anticancer 2009; 20: 856-866.

[2] Woodburn JR Mai karɓar haɓakar haɓakar epidermal da hanawarsa cikin maganin ciwon daji. Pharmacol Ther 1999; 82: 241-250.

[3] Laungiyar haɗin gwiwa na Lungiyoyin Ciwon Cellwayar ungasa. Chemotherapy a cikin ƙananan ƙwayar cutar huhu: wani zane-zane ta hanyar amfani da bayanan da aka sabunta kan marasa lafiya daga 52 gwaji na asibiti. BMJ 1995; 311: 899-909.

[4] Douillard JY, Kim ES, Hirsh V, et al. Gefitinib (IRESSA) tare da docetaxel a cikin marasa lafiya tare da ci gaba na cikin gida ko ƙananan ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta ta jiki: wani bazuwar, lakabi na lakabi na uku na binciken (INTEREST) J Thoracic Oncol 2007; 2: PRS-02–

[5] Fukuoka M, Wu Y, Thongprasert S, et al. Nazarin biomarker daga lokaci na III, bazuwar, lakabin buɗewa, binciken layin farko na gefitinib (G) akan carboplatin / paclitaxel (C / P) a cikin marasa lafiya da aka zaɓa (pts) tare da ci gaba ƙananan ƙananan ƙwayoyin huhu (NSCLC) a Asiya (IPASS). J Clin Oncol 2009; 27 Gudanarwa. 15: 8006–.

[6] Reck MA babban mataki zuwa ga keɓaɓɓen maganin kansar huhu tare da gefitinib: gwajin IPASS da ƙari. Gwani Rev Anticancer Ther 2010; 10: 955-965.

[7] Barker, Nazarin AJ wanda ke haifar da gano ZD1839 (IRESSA): mai aiki da baki, mai zaɓin haɓakaccen haɓakaccen haɓakaccen haɓakaccen mai karɓar maganin tyrosine kinase wanda aka yi niyya don maganin cutar kansa. Bioorg. Likita Chem. Lett. 11, 1911-1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): mai hana aiki mai magana da baki na haɓakar haɓakar epidermal tare da yiwuwar maganin kansar. Ciwon daji Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Rashin kwance cibiyar sadarwar sigina na ErbB. Yanayin Rev. Mol. Kwayar Biol. 2, 127-137 (2001).

[10] Cersosimo, RJ Ciwon huhu: wani bita. Am. J. Lafiya Syst. Pharm. 59, 611-642 (2002).

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