Ndi Zomwe Mukudziwa Zomwe Muyenera Kudziwa Musanagwiritse Ntchito Erlotinib - AASraw
AASraw imapanga ufa wa Cannabidiol (CBD) ndi Hemp Mafuta Ofunika ambiri!

Erlotinib

 

  1. Kodi Erlotinib ndi Chiyani?
  2. Kodi Erlotinib Amagwira Ntchito Motani?
  3. Kodi Erlotinib Amachiza Matenda Ati?
  4. Kodi Erlotinib Akugwiritsidwa Ntchito Motani M'chipatala?
  5. Mwa Odwala Omwe Kodi Erlotinib Amagwira Bwino Kwambiri?
  6. Kodi Kukaniza kwa Erlotinib N'kutani?
  7. Kodi Ndizoopsa Zotani Zomwe Zimakhudzana ndi Erlotinib?
  8. Ndi mankhwala ati kapena zowonjezera zomwe zimayenderana ndi Erlotinib?
  9. Chithandizo Chovomerezeka cha FDA Erlotinib
  10. Chidule

 

Kodi N'chiyani? Erlotinib

Erlotinib (CAS:183321-74-6ali m'gulu la mankhwala omwe amadziwika kuti tyrosine kinase inhibitors. Zimagwira ntchito poletsa ntchito ya puloteni yotchedwa epidermal grow factor receptor (EGFR). EGFR imapezeka pamwamba pa maselo ambiri a khansa komanso maselo abwinobwino. Imagwira ngati "tinyanga," yolandira zikwangwani kuchokera kuma cell ena ndi chilengedwe chomwe chimauza khungu kuti likule ndikugawana. EGFR imagwira gawo lofunikira pakukula ndikukula msanga komanso nthawi yaubwana ndipo imathandizira kukhalabe m'malo mwa akulu ndi owonongeka mwa akulu. Komabe, maselo ambiri a khansa ali ndi EGFR yambiri pamtunda, kapena EGFR yawo yasinthidwa ndi kusintha kwa DNA yomwe imanyamula mtundu wa protein. Zotsatira zake ndikuti zikwangwani zochokera ku EGFR ndizolimba kwambiri, zomwe zimapangitsa kukula kwamaselo ndi magawano, chizindikiro cha khansa.

 

Kodi Amachita Bwanji? Erlotinib Ntchito? 

Limagwirira a antitumor zochita za erlotinib sadziwika bwino. Erlotinib amaletsa phosphorylation yama cell ya tyrosine kinase yolumikizidwa ndi epidermal kukula factor receptor (EGFR). Makamaka a zopinga zokhudzana ndi ma tyrosine kinase receptors ena sanazindikiridwe bwino. EGFR imawonetsedwa pakhungu lamaselo abwinobwino ndi maselo a khansa.

 

Zomwe Matenda Amachita Erlotinib Kuchiza Kwambiri? 

(1) Matenda a khansa

Erlotinib yemwe ali ndi khansa ya m'mapapo yopanda zingwe yosakanika ikawonjezeredwa ku chemotherapy imathandizira kuti anthu azikhala ndi moyo wokwanira 19%, ndikupitilizabe kupitirira pang'onopang'ono (PFS) ndi 29%, poyerekeza ndi chemotherapy yokha. US Food and Drug Administration (FDA) idavomereza erotinib zochizira khansa yam'mapapo yam'mapapo kapena yaying'ono yam'mimba yomwe yalephera ngakhale mtundu umodzi wamankhwala am'mbuyomu.

Mu khansa ya m'mapapo, erlotinib yawonetsedwa kuti ndiyothandiza kwa odwala omwe alibe kapena opanda kusintha kwa EGFR, koma akuwoneka kuti ndiwothandiza kwa odwala omwe asintha EGFR. Kupulumuka konse, kupulumuka kopita patsogolo komanso kupulumuka kwa chaka chimodzi ndikofanana ndi mzere wachiwiri wachiwiri chithandizo (docetaxel kapena pemetrexed). Kuchuluka kwa mayankho kuli pafupifupi 50% kuposa chemotherapy yachiwiri yachiwiri. Odwala omwe samasuta, komanso osuta omwe kale amasuta, omwe ali ndi adenocarcinoma kapena ma subtypes ngati BAC atha kukhala ndi kusintha kwa EGFR, koma kusintha kumatha kuchitika mitundu yonse ya odwala . Kuyesa kwa kusintha kwa EGFR kwapangidwa ndi Genzyme.

 

(2) Khansara yapancreatic

Mu Novembala 2005, a FDA adavomereza erlotinib kuphatikiza ndi gemcitabine yothandizira khansa yapakhungu yotsogola, yosasunthika, kapena yamatenda.

AASraw ndiye katswiri wopanga Erlotinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

(3) Kukaniza chithandizo

Erlotinib womangidwa ku ErbB1 pamalingaliro a 2.6A; Mtundu wapadziko lapansi umawonetsa hydrophobicity. Pankhani ya erlotinib izi zimachitika miyezi 8-12 kuyambira pomwe mankhwala amayamba. Kuposa 50% ya kukana kumayambitsidwa ndi kusintha kwa thumba lolimbitsa la ATP la domain ya EGFR kinase yokhudzana ndi kusinthana ndi zotsalira zazing'ono za polar threonine ndi zotsalira zazikulu za methionine (T790M) .Pafupifupi 20% ya kukana mankhwala kumayambitsidwa hepatocyte grow factor receptor, yomwe imayendetsa kutsegulira kwa ERBB3 kwa PI3K.

 

Erlotinib

 

Bwanji Is Erlotinib Cmwachangu Used In The Cnthabwala?

Erlotinib adavomerezedwa koyamba ndi United States Food and Drug Administration (FDA) kuti igwiritsidwe ntchito kwa odwala omwe ali ndi khansa yaying'ono yaying'ono yamapapo yam'mapapo omwe adabwereranso pambuyo pa mtundu wina wamankhwala. Mu 2005, idavomerezedwa kuti igwiritsidwe ntchito limodzi ndi mankhwala ena, gemcitabine, ya khansa yayikulu ya kapamba. Mu 2010, kugwiritsiridwa ntchito kwake kudakulitsidwa ndikuphatikizira chithandizo chothandizira odwala omwe ali ndi khansa yaying'ono yaying'ono yamapapo yam'mapapo yomwe matenda awo anali okhazikika patatha nthawi zinayi zochiritsira ndi mankhwala a platinamu, monga cisplatin kapena carboplatin. Odwala omwe amatenga erlotinib nthawi zambiri amalekerera mankhwalawa bwino. Zotsatira zoyipa kwambiri ndikutuluka pakhungu ndi kutsegula m'mimba.

 

In Which Pati Is Erlotinib Most Ezakuthupi?

Kwa zaka XNUMX zapitazi, azachipatala adziwa zambiri ndi tyrosine kinase inhibitors, monga erlotinib, yomwe imaletsa EGFR. Zakhala zikuwonekeratu kuti mankhwalawa amagwira ntchito bwino kwa odwala omwe khansa ya m'mapapo imakhala ndi mtundu wina wamasinthidwe womwe umabweretsa protein yachilendo ya EGFR. Odwalawa nthawi zambiri amakhala ochokera ku Asia, azimayi, komanso osasuta fodya omwe ali ndi khansa yamapapo yotchedwa bronchoalveolar adenocarcinoma. Chifukwa chake, mu 2013, erlotinib adavomerezedwa kukhala chithandizo choyamba pagululi, ngati khansa yawo singathe kuchiritsidwa opaleshoni.

 

Chani Is Erlotinib Rthandizo?

Erlotinib ndiwothandiza kwambiri pagulu la odwala omwe asintha kusintha kwa EGFR. Komabe, ngakhale odwalawo pamapeto pake ayamba kuwonetsa kupitilira kwa khansa yawo atatha miyezi 12 ya mankhwala a erlotinib. Ichi ndi chifukwa chitukuko cha kukana mankhwala mu yotsalira maselo a khansa. Nthawi zambiri, kukana kumachitika chifukwa chakusintha kwachiwiri kwamapuloteni a EGFR omwe amaletsa erlotinib kuti asalumikizane ndi dera la tyrosine kinase. Njira zatsopano zothandizira odwalawa ndi monga tyrosine kinase inhibitor afatinib, yokha kapena yophatikiza ndi cetuximab (Erbitux), yomwe imaletsa EGFR ndi njira ina.

 

Kodi Ndizoopsa Zotani Zomwe Zimakhudzana ndi Erlotinib?

M'maphunziro, zovuta zoyipa kwambiri ndi Erlotinib zikagwiritsidwa ntchito ngati monotherapy ya khansa yam'mapapo zinali zotupa (zomwe zimakhudza 75% ya odwala), kutsekula m'mimba (54%), kusowa kwa njala ndi kutopa (52% iliyonse). Pakafukufuku wa Tarceva ogwiritsidwa ntchito limodzi ndi gemcitabine ya khansa ya kapamba, zovuta zoyipa kwambiri zinali kutopa (zomwe zimakhudza 73% ya odwala), zotupa (69%) ndi kutsegula m'mimba (48%). Kuti muwone mndandanda wonse wazotsatira ndi zoletsa za Erlotinib, onani kapepala kake.

 

amene Dmakalapeti kapena Smafilimu Iosachita Wit Erlotinib?

CYP3A4 ndi enzyme m'chiwindi yomwe imawonongeka ndipo imathandizira kuthana ndi erlotinib mthupi. Mankhwala omwe amaletsa CYP3A4 atha kubweretsa kuchuluka kwa erlotinib mthupi, ndipo kuchuluka kwake kumatha kubweretsa poizoni kuchokera ku erlotinib. Mankhwalawa amaphatikizapo atazanavir (Reyataz), clarithromycin (Biaxin), indinavir (Crixivan), itraconazole (Sporanox), ketoconazole (Nizoral), nefazodone (Serzone), nelfinavir (Viracept), ritonavir (Norvir), saquasevir (Invvase) telithromycin (Ketek), ndi voriconazole (VFEND). Odwala omwe amalandira mankhwalawa, pangafunike mlingo wocheperako wa erlotinib popewa poizoni.

Mankhwala ena amachulukitsa kuchotsedwa kwa erlotinib powonjezera ntchito ya michere ya CYP3A4. Izi zimachepetsa milingo ya erlotinib mthupi ndipo imatha kuchepetsa zotsatira zake. Zitsanzo za mankhwalawa ndi monga rifampicin (Rifadin), rifabutin (Mycobutin), rifapentine (Priftin), phenytoin (Dilantin), carbamazepine (Tegretol), phenobarbital ndi St. John's Wort. Mankhwalawa ayenera kupewedwa mwa odwala omwe atenga erlotinib, ngati zingatheke. Ngati mankhwala ena si njira ina, pamafunika kuchuluka kwa mankhwala a erlotinib. Kusuta ndudu kumachepetsanso kuchuluka kwa erlotinib m'magazi. Odwala amalangizidwa kuti asiye kusuta.

Mankhwala omwe amachepetsa kupanga asidi m'mimba amachepetsa kuyamwa kwa erlotinib. Chifukwa chake, ma proton pump inhibitors (ma PPI, mwachitsanzo, omeprazole [Prilosec, Zegerid]) sayenera kuperekedwa ndi erlotinib, ndipo erlotinib iyenera kuperekedwa maola 10 H2-receptor blockers (mwachitsanzo, ranitidine [Zantac]) kapena patadutsa maola awiri kutenga cholembera cha H2-receptor.

Kuwongolera ma antiacids kuyenera kulekanitsidwa ndi kuyang'anira erlotinib ndi maola angapo. Erlotinib adalumikizidwa ndi chiopsezo chowonjezeka chakutaya magazi, makamaka kwa odwala omwe akutenga warfarin (Coumadin). Odwala omwe akutenga warfarin ayenera kuyang'aniridwa bwino.

 

FDA Yavomerezedwa Erlotinib chithandizo

Pa Okutobala 18, 2016, US Food and Drug Administration idasintha chiwonetsero cha erlotinib (TARCEVA, Astellas Pharm Global Development Inc.) yothandizira khansa ya m'mapapo yaing'ono (Zamgululi) kuchepetsa kugwiritsa ntchito kwa odwala omwe zotupa zawo zimakhala ndi kusintha kwamtundu wa epidermal kukula factor receptor (EGFR).

Kusintha kolembako kumagwira ntchito kwa odwala omwe ali ndi NSCLC akulandila chithandizo chachiwiri kapena chachikulu. Zizindikirozi zidzangokhala kwa odwala omwe zotupa zawo zimachotsedwa ndi EGFR exon 19 kapena exon 21 L858R m'malo osintha monga amuonera ndi mayeso ovomerezeka a FDA. Chizindikiro cha mzere woyamba m'mbuyomu chinali chokhacho kwa odwala omwe ali ndi EGFR exon 19 kuchotsa kapena exon 21 m'malo osintha.

Chowonjezera choterechi chimachokera ku zotsatira za kuyesedwa kwa IUNO, kuyesayesa kosawoneka bwino, kosawoneka bwino, kolamulidwa ndi placebo, kuyesedwa kwa erlotinib komwe kumayendetsedwa ngati mankhwala osamalira odwala 643 omwe ali ndi NSCLC yotsogola omwe sanakumanepo ndi matenda kapena poyizoni wosavomerezeka munthawi zinayi za platinum yochokera ku chemotherapy yoyamba. Odwala omwe zotupa zawo zimakhudza kuyambitsa kusintha kwa EGFR (exon 19 deletions or exon 21 L858R mutations) sanatulukidwe pamlanduwu. Odwala adasinthidwa 1: 1 kuti alandire erlotinib kapena placebo pakamwa kamodzi tsiku lililonse (322 erlotinib, 321 placebo) mpaka matenda atha kapena poyizoni wosavomerezeka. Kutsatira kupitilira kwa chithandizo choyambirira, odwala anali oyenera kulowa gawo lotseguka. Makumi asanu ndi anayi mwa odwala omwe adasinthidwa kuti erlotinib adalowa nawo lotseguka ndipo adalandira chemotherapy, pomwe 77% ya odwala omwe adasinthidwa kupita ku placebo adalowa gawo lotseguka ndikulandila erlotinib.

Mapeto ake oyeserera anali kupulumuka kwathunthu. Zotsatira zikuwonetsa kuti kupulumuka pakutsata chithandizo ndi erlotinib sikunali bwinoko kuposa malobo omwe amathandizidwa posamalira odwala omwe ali ndi zotupa za NSCLC zosasunga masinthidwe oyambitsa EGFR. Palibe kusiyana pakukhala kopanda kupita patsogolo pakati pa mkono wa erlotinib ndi mkono wa placebo.

FDA sidzafuna zofunikira zotsatsa pambuyo pake kapena kupempha zomwe adzachite kutsatsa pambuyo pazotsatira za kuyesedwa kwa IUNO.

AASraw ndiye katswiri wopanga Erlotinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

Chidule

Erlotinib ndi mankhwala opangira mankhwala a khansa. Amavomerezedwa kuti athetse khansa ya m'mapapo yosakhala yaying'ono, khansa ya prostate yosasunthika, komanso khansa ya kapamba. Unikaninso zoyipa, kuchuluka kwa mankhwala, kulumikizana ndi mankhwala, machenjezo ndi zodzitetezera, komanso zidziwitso zachitetezo cha mimba zisanachitike ntchito Erlotinib.

 

Reference

[1] Thomas L. Petty, MD (2003). "Otsimikiza a Kuyankha kwa Chotupa ndi Kupulumuka Ndi Erlotinib mwa Odwala Omwe Ali ndi Khansa Yapakhungu Yochepa Kwambiri". Zolemba pa Clinical Oncology. 1 (17): 3-4.

[2] "FDA ivomereza kuyesedwa kwa Roche ngati CDx ya Tarceva pochizira odwala ena a NSCLC". GenomeWeb. Inabwezeretsanso 10 Januware 2020.

[3] Dudek AZ, Kmak KL, Koopmeiners J, ndi al. (2006). "Ziphuphu zakhungu ndi bronchoalveolar histology zimagwirizana ndi chithandizo chamankhwala kwa odwala omwe amathandizidwa ndi gefitinib ngati chithandizo cha khansa yamapapo yam'mapapo yam'mapapo yam'magazi" Khansa Yam'mapapo. 51 (1): 89–96.

[4] Jones HE, Goddard L, Gee JM, Hiscox S, Rubini M, Barrow D, Knowlden JM, Williams S, Wakeling AE, Nicholson RI: Insulin-like factor factor-I receptor signature ndikulimbana ndi gefitinib (ZD1839; Iressa) in maselo a khansa ya m'mawere ndi prostate. Khansa ya Endocr Relat. Disembala la 2004; 11 (4): 793-814.

[5] Kobayashi K, Hagiwara K (2013). "Epidermal growth factor receptor (EGFR) kusintha kwamankhwala ndi makonda pa khansa ya m'mapapo yopanda khungu (NSCLC)". Oncology Yoyenera. 8 (1): 27-33. onetsani: 10.1007 / s11523-013-0258-9. Mphatso ya PMC 3591525.

[6] Cohen, Martin H .; Johnson, John R .; Chen, Yeh-Fong; Sridhara, Rajeshwari; Pazdur, Richard (Ogasiti 2005). "Chidule cha kuvomerezeka kwa FDA: mapiritsi a erlotinib (Tarceva)". Oncologist. 10 (7): 461-466.

[7] Blum G, Gazit A, Levitzki A: Gawo lotsutsana ndi zoletsa za IGF-1 receptor kinase. Zamoyo. 2000 Dis 26; 39 (51): 15705-12.

[8] "Mankhwala a khansa: Khothi Lalikulu limalola Cipla kuchotsa apilo ku Roche". Nthawi Yachuma. 16 June 2017. Zasungidwa kuyambira pachiyambi pa 24 Disembala 2019. Zotulutsidwa 23 Disembala 2019.

[9] Delbaldo C, Faivre S, Raymond E: [Epidermal growth factor inhibitors]. Rev Med Interne. 2003 Jun; 24 (6): 372-83.

[10] Chen X, Ji ZL, Chen YZ: TTD: Database Yoyang'anira Zamankhwala. Nucleic Acids Res. 2002 Jan 1; 30 (1): 412-5.

[11] Filppula AM, Neuvonen PJ, Backman JT: Kuunika kwa vitro kwa zoletsa zomwe zimadalira nthawi pa CYP2C8 ndi ntchito ya CYP3A ndi mapuloteni kinase inhibitors khumi ndi anayi. Kutaya Mankhwala Osokoneza bongo. 2014 Jul; 42 (7): 1202-9. onetsani: 10.1124 / dmd.114.057695. Epub 2014 Apr 8.

0 Likes
126 Views

Mukhozanso ndimakonda

Comments atsekedwa.