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Gefitinib

  1. Guudmarka Gefitinib
  2. Farsamaynta Gefitinib
  3. Isticmaalka Gefitinib Adduunyada
  4. Waxyeelada Gefitinib
  5. Kaydinta Gefitinib
  6. Rearch More: "Dilaa Kansarka Sambabka" Gefitinib

 

Gefitinib Guudmarka

Gefitinib waa kinase inhibitor.Magaca kiimikada ee gefitinib waa 4-Quinazolinamine N- (3-chloro-4-fluorophenyl) -7-methoxy-6- [3- (4-morpholinyl) propoxy] .Gefitinib wuxuu leeyahay qaacidada molikuyuulka ee C22H24ClFN4O3 , cufnaanta molikaliska ee 446.9 dalton waana budo midab cad leh. Gefitinib waa saldhig bilaash ah. Molikuyuulku wuxuu leeyahay pKas oo ah 5.4 iyo 7.2. Gefitinib waxaa lagu qeexi karaa inuu si tartiib tartiib ah ugu milmi karo pH 1, laakiin ficil ahaan laguma milmi karo korka pH 7, iyadoo milanka uu aad hoos ugu dhacayo inta udhaxeysa pH 4 iyo pH 6. Waxyaabaha dareeraha ah ee aan biyaha kujirin, gefitinib wuxuu si xur ah ugu milmi karaa aaladda acid-ka ee glacial iyo dimethyl sulfoxide, waa la milmi karaa in pyridine, si tartiib tartiib ah loogu milmi karo tetrahydrofuran, waxyarna lagu milmi karo methanol, ethanol (99.5%), ethyl acetate, propan-2-ol iyo acetonitrile.

Kiniiniyada 'Gefitinib' ayaa loo heli karaa inay yihiin kiniinno filim bunni leh, oo ay ku jiraan 250 mg oo ah gefitinib budo, maamulka afka. Maaddooyinka aan firfircooneyn ee aasaasiga kiniinka kiniinnada IRESSA waa lactose monohydrate, microcrystalline cellulose, sodium croscarmellose, povidone, sodium lauryl sulfate iyo magnesium stearate. Dahaarka kiniinka wuxuu ka kooban yahay hypromellose, polyetylen glycol 300, titanium dioxide, cas ferric oxide iyo yellow ferric oxide.

 

Information Technical:

magaca Gefitinib
Magaca rasmiga ah N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
CAS Number 184475-35-2
Isku mid ahaanshaha ZD 1839
Formula kelli C22H24ClFN4O3
Miisaanka Nooca 446.9
xagiisayna ≥98%
Dejinta A adag crystalline
milmi DMF: 20 mg / ml
DMSO: 20 mg / ml
DMSO: PBS (pH7.2) (1: 1): 0.5 mg / ml
Ethanol: 0.3 mg / ml
dhoola COC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4
Xeerka 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)
Keydka InChi XGALLCVXEZPNRQ-UHFFFAOYSA-N
kaydinta -20 ° C

 

Gefitinib waxaa loo isticmaalaa in lagu daaweeyo kansarka sanbabada ee unugyada yar oo ku faaftay qaybaha kale ee jirka dadka qaba noocyo burooyin ah. Gefitinib wuxuu kujiraa nooc daawooyin ah oo loo yaqaan kinase inhibitors. Waxay ku shaqeysaa iyada oo la xakameynayo ficil ka mid ah walax dabiici ah oo dabiici ah oo loo baahan karo si loo caawiyo kansarka unugyadu way tarmayaan.

AASraw waa soo saaraha xirfadlaha ah ee Gefitinib.

Fadlan halkan guji si aad u hesho macluumaadka xigashada: bannaanNala soo xiriir

 

Gefitinib Farsamaynta ficilka

Gefitinib waa kahortaga xajiyaha cuncunka epidermal factor receptor (EGFR) tyrosine kinase oo kuxiran goobta adenosine triphosphate (ATP) ee xarigga u ah enzyme. EGFR badanaa waxaa lagu muujiyaa in lagu badbadiyey unugyada kansarka qaarkood, sida sanbabada iyo naaska unugyada kansarka. Cadaadiska xad-dhaafka ahi wuxuu keenaa firfircoonaan firfircoon oo ka-hortagga apopatotic-ka ee calaamadaha 'Ras-transduction cascades', ka dib taasoo keentay sii noolaanshaha unugyada kansarka iyo kordhinta unugyada. Gefitinib waa kahortaga koowaad ee xulashada EGFR tyrosine kinase kaas oo sidoo kale loo yaqaan Her1 ama ErbB-1. Adoo xakameynaya EGFR tyrosine kinase, cascades-ka hooseeya ee isha ayaa sidoo kale la xakameynayaa, taasoo dhalisay kororka unugyada halista ah.

 

Gefitinib Ku Isticmaal Adduunyada

Gefitinib hadda waxaa laga iibiyaa in kabadan 64 dal. Gefitinib waxaa laga ansixiyay oo laga suuq geeyay bishii Julaay 2002 Japan, taasoo ka dhigtay dalkii ugu horeeyay ee daroogada soo galiya.

The FDA ayaa ansixisay gefitinib Bishii Meey 2003 si loogu daweeyo kansarka sanbabada ee aan yareyn (NSCLC) .Waxaa loo ogolaaday daaweynta monotherapy ee daaweynta bukaanada qaba heer sare ama heer sare ah NSCLC ka dib markii ay ku guuldareysteen labadaba daawada 'platinum' iyo 'docetaxel chemotherapies', oo ah daaweynta sadarka saddexaad.

Bishii Juun 2005 FDA waxay ka noqotay oggolaanshaha isticmaalka bukaannada cusub sababo la xiriira caddayn la'aan inay sii dheereysey nolosha.

Yurub agteeda gefitinib waxaa lagu muujiyey tan iyo 2009 in NSCLC horumarsan dhammaan khadadka daaweynta ee loogu talagalay bukaanada ku jira isbedelada EGFR. Calaamaddan waxaa la siiyay ka dib markii gefitinib loo muujiyey daaweynta ugu horreysa si loo hagaajiyo badbaadada ka-hor-imaad la'aanta ah iyo nidaamka laba-laabma ee bukaan-socodka ee bukaanada ku jira is-beddelka noocaas ah. IPASS wuxuu ahaa kii ugu horreeyay ee afarta waji III ee tijaabooyinka ah ee lagu xaqiijiyay gefitinib sarreynta bukaankaan bukaanka ah.

Inta badan dalalka kale ee gefitinib hadda lagu suuq geeyo waxaa loo oggol yahay bukaanada qaba NSCLC horumarsan oo helay ugu yaraan hal nidaam dawladeed oo hore. Si kastaba ha noqotee, codsiyada lagu balaarinayo calaamadeeda inay tahay daaweynta ugu horeysa ee bukaanada heysta isbedelada EGFR ayaa hada lagu gudajiraa iyadoo lagu saleynayo cadeyntii ugu dambeysay ee cilmiyaysan. [Xigasho] Bishii Ogosto 2012 New Zealand waxay ogolaatay gefitinib oo ah daaweynta ugu horeysa ee bukaanka qaba Isbeddelka EGFR ee caqli-galnimada maxalliga ah ama heer sare ah, oo aan la aqbali karin NSCLC. Tan waxaa si guud loo maal galiyaa mudo 4 bilood ah oo bilaw ah iyo cusbooneysiin haddii aan wax horumar ah la samaynin. Bishii Luulyo 13, 2015, FDA waxay ogolaatay gefitinib oo ah daweynta koowaad ee NSCLC.

Gefitinib

Waxyeelada Gefitinib

Waxyaabaha muhiimka ah ee laga xasuusto waxyeelada gefitinib:

Dadka badankood ma dareemaan dhammaan dhibaatooyinka soo raaca ee taxan.

Effects Dhibaatooyinka soo raaca badanaa waa la saadaalin karaa marka loo eego bilowgooda iyo muddadooda.

Effects Dhibaatooyinka soo raaca badanaa waa la beddeli karaa waxayna bixi doonaan ka dib marka daaweyntu dhammaato.

Waxaa jira fursado badan oo kaa caawinaya yareynta ama ka hortagga dhibaatooyinka soo raaca.

No Ma jiro xiriir u dhexeeya joogitaanka ama darnaanta dhibaatooyinka soo raaca iyo waxtarka daawada.

 

Waxyeellooyinka soo socdaa waa wax caadi ah (oo ku dhaca in ka badan 30%) bukaanada qaata gefitinib:

Arrhea Shuban

Reaction Dareen-celinta maqaarka (finan, finan)

AASraw waa soo saaraha xirfadlaha ah ee Gefitinib.

Fadlan halkan guji si aad u hesho macluumaadka xigashada: bannaanNala soo xiriir

 

Dhibaatooyinkan soo noqnoqda waa waxyeellooyin aan caadi ahayn (oo ku dhaca qiyaastii 10-29%) bukaannada qaata gefitinib:

Lallabbo

♦ Matag

♦ Cuncun

Appet Cunto xumo

Ation Indho cuncun

 

Xaalado dhif ah (qiyaastii 1%) oo saameyn daran oo daran ah oo ku dhaca isirka sanbabada dhexdooda (oof wareenka, ama caabuq ku dhaca sambabaha cudur la'aan). Markii waxyeelladan ay dhacday, waxaa badanaa la socday neefsashada oo adkaata qufac ama qandho heer-hoose ah oo u baahan isbitaal dhigid. 1/3 kiisaska waxay keeneen dhimasho. Haddii neefsigu kugu soo boodo, qufac iyo / ama qandho dhacdo inta aad qaadanaysid gefitinib, u sheeg xirfadlahaaga daryeelka caafimaadka.

Sare u qaadista tijaabooyinka shaqada beerka (transaminase, bilirubin, iyo alkaline phosphatase) ayaa lagu arkay bukaanada lagu daweeyay gefitinib. Meelahan sare ayaan la socon wax calaamado ah sumowga beerka. Si kastaba ha noqotee, xirfadlahaaga daryeelka caafimaadka ayaa laga yaabaa inuu hubiyo baaritaanka dhiigga si uu ula socdo shaqada beerkaaga xilliyada qaarkood, intaad qaadanayso gefitinib.

Dhibaatooyinka oo dhan kuma qorna kor. Qaar dhif iyo naadir ah (oo ku dhaca wax ka yar 10% bukaannada) halkan laguma qorin. Si kastaba ha noqotee, waa inaad marwalba ogeysiisaa bixiyahaaga daryeelka caafimaadka haddii aad isku aragto astaamo aan caadi ahayn.

 

Gefitinib kaydinta

Ku ilaali gefitinib weelka ay soo gashay, si adag u xir, oo ka fog carruurta. Ku keydi heerkulka qolka oo ka fog kuleylka iyo qoyaanka badan (ha ku jirin musqusha).

Gefitinib aan loo baahnayn waa in lagu tuuraa siyaabo gaar ah si loo hubiyo in xayawaanka, carruurta, iyo dadka kaleba aysan cuni karin. Si kastaba ha noqotee, waa inaadan ku shubin gefitinibkan musqusha. Taabadalkeed, habka ugufiican ee loo tuuro gefitinib-kaaga waa iyada oo loo maro barnaamijka dib-u-celinta daawada. La hadal farmashiistahaaga ama la xiriir waaxda qashinka / dib u warshadaynta si aad wax uga ogaato barnaamijyada dib-u-celinta ee bulshadaada. Eeg Qashin-qaadashada Amni ee FDA boggeeda internetka wixii macluumaad dheeraad ah haddii aadan marin u lahayn barnaamijka dib-u-celinta.

Waxaa muhiim ah in daawada oo dhan la ilaaliyo oo ay gaaraan carruurta oo ay weheliyaan weelal badan (sida mashiinka kiniinka ee toddobaadlaha ah iyo kuwa dhibcaha kiniiniga, kiriimyada, dhejisyada, iyo neefsashada) ma aha ilmo u adkaysta caruurta yar yarna si fudud ayey u furi karaan. Si carruurta yar yar looga ilaaliyo sunta, marwalba xir albaabyada amniga iyo isla markaaba daawada meel nabadgelyo leh - waa mid kor u kaca oo ka baxsan aragtidooda iyo gaadho.

Gefitinib

Rearch More: "Dilaa Kansarka Sambabka" Gefitinib

Gefitinib waa daaweyn ugub ah oo lagu bartilmaameedsado oo xakameynaya waxqabadka tyrosine kinase ee soo-saaraha kobaca epidermal iyadoo si tartan ah looga xannibayo goobta qabashada ATP. Daraasado ku-meel-gaadh ah oo gefitinib ah ayaa muujiyay firfircoonaan xoog leh oo dhowr moodel buro ah, oo ay ku jiraan dhowr khadadka kansarka sambabka iyo xenografts. Laba daraasadood oo waaweyn oo la kala soocay oo wejiga II ah (IDEAL 1 iyo IDEAL 2) oo lagu daweeyey kansarka sanbabada ee unugyada aan yareyn ayaa lagu soo warramey heerka jawaabta ee ku soo dhowaanaya 20% bukaannada safka labaad ah iyo ∼10% kuwa lagu daaweynayo laba ama in ka badan oo ah daaweynta kemotherabi. Badbaadada dhexdhexaadka ah ee labadan daraasadood waxay soo dhawaatay 6-8 bilood. Daaweynta-safka koowaad, gefitinib waxaa lagu qiimeeyay isku darka laba nidaam oo daaweyn kimikal oo kaladuwan laba daraasadood oo waaweyn oo kala sooc ah (INTACT 1 iyo INTACT 2). Labada daraasadoodba waxay ku fashilmeen inay muujiyaan hagaajinta badbaadada wadarta guud ee bukaan socodka ee> bukaanada 1000 daraasad kasta. Qodobbada kale ee dhammaadka (tusaale, waqtiga horumarka iyo heerka jawaabcelinta) sidoo kale laguma sii wanaajin ku darista gefitinib. Daraasado dheeri ah ayaa lagu muujiyey si loo qiimeeyo doorka suurtagalka ah ee gefitinib ee dayactirka bukaannada helay daaweynta kiimoteraabiga ama kiimikada. Daraasado baaritaan ku sameeya gefitinib maadaama daaweynta koowaad ee monotherapy sidoo kale loo baahan yahay.

Inta badan bukaanada qaba unugyada aan yareyn kansarka sanbabada (NSCLC) ugu dambayntii waxay ku dhacdaa cudur metastatic ah ama cudur aan ku habboonayn daaweynta deegaanka oo keliya waana musharraxiinta suurtagalka u ah daaweynta nidaamka. In kasta oo daaweynta kiimikada ay wanaajin karto badbaadada bukaanka qaba cudurrada horumarsan, haddana faa'iidada ayaa ah ∼2 bilood oo keliya daryeelka ugu fiican ee taageerada, tanina waxay ku kacaysaa kharashka waxyeelo weyn. Raadinta wakiilo cusub oo ugu yaraan u firfircoon sida daaweynta kiimikada laakiin u dulqaadashada fiican ayaa ah muhiimadda ugu weyn. Tiro ka mid ah wakiilo cusub oo si gaar ah uga hortaga bartilmaameedyada la xushay ee taagan kansarka unugyada, sida soo-dhaweynta epidermal factor reseptor (EGFR), waxaa lagu tijaabiyaa NSCLC horumarsan. Illaa iyo hadda, ugu horreyntii bukaanada qaba NSCLC heer sare ah ayaa la qiimeeyay, laakiin waxaa jira caqli gal wanaagsan oo lagu baaro dhowr ka mid ah wakiilladaan goobaha cudurka hore, halkaas oo qaar ka mid ah cilladaha hidde-ahaaneed ee la bartilmaameedsaday ay horeyba u joogeen.

EGFR waxaa si heer sare ah loogu muujiyey burooyin kala duwan oo adag, oo ay ku jiraan NSCLC. EGFR waxaa si aad ah loogu muujiyey inta badan (∼80%) kansarka unugyada sanbabada, iyo ku dhowaad kalabar dhamaan adenocarcinomas sambabaha iyo unugyada waaweyn ee kansarka. Dhaqdhaqaaqa EGFR ee unugyada kansarka ayaa lagu muujiyey inuu dhiirrigelinayo geeddi-socodka ku lug leh sii kordhiska unugyada burooyinka, angiogenesis, duulaanka, iyo metastasis, iyo in la joojiyo apoptosis. EGFR (erbB1 ama HER1) waa xubin ka mid ah qoysaska soo dhaweynta erbB, oo ay ku jiraan erbB2 (HER2), erbB3 (HER3), iyo erbB4 (HER4). Waa transmembrane glycoprotein oo ka kooban shey dheeri ah oo isku xidha isku xidhka 'ligand-binding domain', 'transmembrane domain', iyo istiraatiijiyad istiraatiijiyad isbadal ku samaysa oo leh waxqabadka tyrosine kinase. Ka dib markii la xiro lafdhabarta jirka sida sheyga koritaanka epidermal, EGFR waxay hoos u dhigeysaa monomer kale EGFR ama xubin kale oo ka tirsan qoyska erbB. Tani waxay horseed u noqotaa firfircoonida tyrosine kinase, autophosphorylation of tyrosine, iyo bilaabista calaamadaha cascades taas oo ugu dambeyntii keenta jawaabo kala duwan oo ka hooseeya sida kordhinta unugyada. Intaa waxaa sii dheer, muujinta EGFR ee burooyinka ayaa lala xiriiriyay jawaab celin liidata oo ku saabsan daaweynta, horumarinta caabbinta daroogada cytotoxic, horumarka cudurka, iyo badbaadada liidata. Farsamooyinka kale ee kordhinta calaamadaha EGFR ee laga yaabo inay ku lug yeeshaan faafitaanka unugyada burooyinka waxaa ka mid ah heerarka sii kordhaya ee ligand ka baxsan, heterodimerization of EGFR, iyo EGFR mutation. Nooca ugu caansan ee isbeddelay EGFR ee burooyinka waa EGFRvIII, oo laga helo illaa 39% kiisaska NSCLC. EGFRvIII wuxuu xambaarsan yahay isbeddelka tirtirka amino acids 6 illaa 273 ee qaybta ka baxsan isku xidhka wuxuuna muujiyaa waxqabadka tyrosine kinase oo ka madax bannaan isku xidhka 'extracellular ligand bind'.

AASraw waa soo saaraha xirfadlaha ah ee Gefitinib.

Fadlan halkan guji si aad u hesho macluumaadka xigashada: bannaanNala soo xiriir

 

Tixraaca

[1] Rukazenkov Y, Speake G, Marshall G, iyo al. Cuncunka koritaanka Epidermal ee ka hortagayaasha tyrosine kinase inhibitors: isku mid laakiin way ka duwan yihiin? Dawooyinka Anticancer-ka 2009; 20: 856-866.

[2] Woodburn JR Daaweynta lafdhabarta cuncunka epidermal iyo kahortaga daaweynta kansarka. Farmashiil Ther 1999; 82: 241-250.

[3] Kooxda Iskaashatada Kansarka Sambabka ee aan-yareyn. Chemotherapy ee kansarka sanbabada ee unugyada aan yareyn: falanqeyn maadadeed iyada oo la adeegsanayo xogta la cusbooneysiiyay ee bukaanka shaqsiyeed ee laga helay 52 tijaabooyin caafimaad oo la kala soocay. BMJ 1995; 311: 899–909.

[4] Douillard JY, Kim ES, Hirsh V, et al. Gefitinib (IRESSA) iyo docetaxel ee bukaanka qaba kansarka sanbabada ee unugyada unugyada aan horumarsanayn ama metastatic ah ee horay loogu daweeyay daaweynta kiimikada ee ku saleysan platinum: daraasad weji III ah oo furan, sumad furan. J Thoracic Oncol 2007; 2: PRS-02–

[5] Fukuoka M, Wu Y, Thongprasert S, iyo al. Falanqaynta Biomarker ee wajiga III, kala soocida, calaamadda furan, daraasadda koowaad ee gefitinib (G) oo ka soo horjeeda karboplatin / paclitaxel (C / P) ee bukaan socod eegtada la xushay (pts) oo leh kansarka sanbabada unugyada aan yareyn (NSCLC) ee Aasiya (IPASS). J Clin Oncol 2009; 27 Qalabka. 15: 8006–.

[6] Tixgeli MA tallaabada ugu weyn ee loo qaado daaweynta shakhsi ahaaneed ee kansarka sanbabada oo leh gefitinib: tijaabada IPASS iyo wixii ka dambeeya. Khabiir Rev Anticancer Ther 2010; 10: 955-965.

[7] Barker, Daraasadaha AJ ee horseedaya aqoonsiga ZD1839 (IRESSA): firfircoon hadal ahaan, xulasho koritaanka epidermal factor receptor tyrosine kinase inhibitor loogu talagalay daaweynta kansarka. Bioorg. Med. Chem. Lett. 11, 1911–1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): kahortag firfircoon oo afka ah oo ka soo baxda cunsurka koritaanka epidermal ee tilmaamaya suurtagalnimada daaweynta kansarka. Kansarka Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Unangling the ErbB network signaling. Dabeecadda Rev. Mol. Qalabka Biol. 2, 127-137 (2001).

[10] Cersosimo, RJ Kansarka sambabka: dib u eegis. Am. J. Caafimaadka Syst. Farmashiye. 59, 611-642 (2002).

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