Mafunso a 6 About Afatinib on Anti-Caners (NSCLC) - AASraw
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Afatinib

 

  1. Kodi Afatinib ndi Chiyani?
  2. Pamene Timafunikira Afatinib?
  3. Kodi Afatinib imagwira ntchito bwanji?
  4. Kodi Afatinib Adavomerezedwa ndi FDA? Zedi
  5. Kodi Afatinib Imabweretsa Chiwopsezo / Zoyipa Ziti?
  6. Ndizofufuza Ziti Zina Zokhudza Afatinib?

 

Chani Is Afatinib?

Afatinib (CAS: 439081-18-2) ndi mankhwala omwe amadziwikanso kuti Giotrif. Amagwiritsidwa ntchito pochiza khansa ya m'mapapo yaing'ono (NSCLC) yomwe yayamba kufalikira kunja kwa mapapo kapena mbali zina za thupi. Itha kugwiritsidwanso ntchito kuthana ndi khansa zina ngati gawo la mayeso azachipatala.

Ndibwino kuti muwerenge izi ndi zambiri zokhudza khansa ya m'mapapo kapena mtundu wa khansa yomwe muli nayo. Dokotala wanu azikulankhulani za mankhwalawa komanso zotsatirapo zake musanavomere (kulandira) kulandira chithandizo. Mukamalandira chithandizo, mudzawona dokotala kapena namwino wa khansa. Izi ndi zomwe timatanthauza tikamanena za dokotala kapena namwino pazomwezi.

 

Pamene Tifunika Afatinib

Afatinib itha kugwiritsidwa ntchito pochiza khansa yaying'ono yamapapo yam'mapapo (NSCLC) yomwe ili ndi:

Read Kufalikira kumatenda oyandikana nawo (akumaloko)

Read Kufalikira ku ziwalo zina za thupi (zotsogola kapena zotumphukira).

Afatinib amangogwira ntchito ya khansa yomwe imakhala ndi puloteni yotchedwa epidermal grow factor receptor (EGFR). Kuyesedwa kumachitika pamaselo a khansa kuchokera ku biopsy kapena opaleshoni yam'mbuyomu kuti muwone kuchuluka kwa EGFR. Izi zimauza dokotala wanu ngati afatinib atha kukuchitirani ntchito.

 

Kodi Amachita Bwanji? Afatinib Ntchito?

Afatinib ndiwamphamvu komanso wosankha, wosasinthika wa ErbB. Afatinib imamangirira mozungulira ndikusinthasintha kosasunthika kwa ma homo ndi ma heterodimers opangidwa ndi mamembala amtundu wa ErbB EGFR (ErbB1), HER2 (ErbB2), ErbB3 ndi ErbB4.

Makamaka, afatinib imamangirira molumikizana ndi madera a kinase a EGFR (ErbB1), HER2 (ErbB2), ndi HER4 (ErbB4) ndipo amaletsanso tyrosine kinase autophosphorylation, zomwe zimapangitsa kuti ErbB asayinidwe. Zosintha zina ku EGFR, kuphatikiza kusintha kosagonjetseka komwe kumachitika mu kinase, kumatha kubweretsa kuchuluka kwa autophosphorylation ya cholandilira, zomwe zimapangitsa kuti pakhale kulandila kwa receptor, nthawi zina ngati kulibe kumangiriza kwa ligand, ndipo kumatha kuthandizira kuchuluka kwa ma cell ku NSCLC. Zosintha zosagonjetsedwa zimatanthauziridwa kuti ndizomwe zimachitika ku exon zomwe zimapanga dera la kinase la EGFR zomwe zimapangitsa kuti pakhale mphamvu yolandirira kulandira mphamvu komanso komwe kunenedweratu ndi 1) kuphulika kwa chotupa kuchipatala ndi mlingo woyenera wa afatinib ndi / kapena 2) choletsa kuchuluka kwa ma cell kapena EGFR tyrosine kinase phosphorylation pamlingo wa afatinib wokhazikika pamlingo woyenera malinga ndi njira zovomerezeka. Zomwe zimapezeka kwambiri pakusintha uku ndi exon 21 L858R m'malo ndi exon 19 kufufutidwa.

Kuphatikiza apo, afatinib idawonetsa kuletsa kwa autophosphorylation ndi / kapena mu vitro kuchuluka kwa ma cell omwe akuwonetsa EGFR yamtchire komanso mwa omwe akuwonetsa kusintha kwa EGFR exon 19 kuchotsa, exon 21 L858R masinthidwe, kapena zosintha zina zosavomerezeka, pakufika kwa atatinib odwala. Kuphatikiza apo, afatinib inaletsa mu vitro kuchuluka kwa mizere yama cell yopitilira muyeso HER2.

AASraw ndiye katswiri wopanga Afatinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

anali Afatinib Yavomerezedwa ndi FDA? Zedi

Kuvomerezeka kumapereka njira yachiwiri yothandizira odwala omwe ali ndi khungu lachiwiri laling'ono laling'ono khansa ya m'mapapo (NSCLC), yoyimira pafupifupi 20-30% yamilandu ya NSCLC

Kuvomerezeka kumachokera pazotsatira za kafukufuku wa LUX-Lung 8, zomwe zidawonetsa kusintha kwakukulu pakupulumuka komanso kupitilira pang'onopang'ono poyerekeza ndi Tarceva (erlotinib) mwa odwala omwe ali ndi squamous cell carcinoma ya m'mapapo

Afatinib wavomerezedwa kale m'maiko opitilira 60 kuti azithandizira odwala omwe ali ndi mitundu yosiyana ya NSCLC yosintha kwa EGFR

Afatinib

Chiopsezo Chotani/ Zotsatira zoyipa Kodi Afatinib Bweretsani? 

Zinthu zofunika kuzikumbukira pazotsatira zake za afatinib:

▪ Anthu ambiri sangaone zovuta zonse za afatinib zomwe zalembedwa.

▪ Zotsatira zoyipa za Afatinib nthawi zambiri zimadziwikiratu malinga ndi momwe zimayambira, kutalika kwake, komanso kuopsa kwake.

▪ Zotsatira zoyipa za Afatinib nthawi zambiri zimasinthidwa ndipo zimatha mankhwala akamaliza.

▪ Zotsatira zoyipa za Afatinib zitha kukhala zotheka. Pali zosankha zambiri zochepetsera kapena kupewa zovuta za afatinib.

 

Zotsatira zotsatirazi ndizofala (zomwe zimachitika kuposa 30%) kwa odwala omwe amamwa afatinib:

▪ Kutsekula m'mimba

▪ Kuphulika kwa ziphuphu (gulu la khungu lofanana ndi ziphuphu)

▪ Zilonda za pakamwa

▪ Paronychia (matenda a misomali)

▪ Pakamwa pouma

 

Izi ndizotsatira zoyipa zochepa (zomwe zimachitika mu 10-29%) kwa odwala omwe alandila afatinib:

▪ Kuchepetsa njala

▪ Kuyabwa

▪ Kuchepetsa thupi

▪ Mphuno imatuluka

▪ Cystitis (matenda a chikhodzodzo)

▪ Cheilitis (kutupa kwa milomo)

▪ Malungo

▪ Hypokalemia (potaziyamu wochepa)

▪ Conjunctivitis (diso la pinki)

▪ Rhinorrhea (mphuno yothamanga)

▪ Mavitamini okwera a chiwindi

Sizovuta zonse zomwe zalembedwa pamwambapa. Zina zomwe ndizosowa (zomwe zimachitika ochepera 10 peresenti ya odwala) sizidalembedwe apa. Nthawi zonse dziwitsani omwe akukuthandizani ngati mukukumana ndi zachilendo.

 

Zomwe Zina Zofufuza Zokhudza Afatinib?

 Kukula kwa Afatinib (BIBW 2992) mu khansa ya m'mapapo yosakhala yaying'ono

Afatinib (BIBW 2992), buku lochokera kwa aniline-quinazoline, losasinthika komanso mwaukadaulo likuwunikira zochitika zapakati pa kinase za onse omwe akuchita nawo banja la ErbB receptor. Zotsatira zamankhwala zikuwonetsa kuti afatinib imagwira bwino ntchito pamatenda am'mapapo am'mapapo, kuphatikiza omwe ali ndi kusintha kwa EGF receptor (EGFR) osagonjetsedwa ndi m'badwo woyamba wa EGFR inhibitors. Afatinib ikufufuzidwa mu pulogalamu ya LUX-Lung, yomwe idzawunika afatinib ngati mankhwala oyamba mwa odwala omwe ali ndi kusintha kwa ma EGFR (LUX-Lung 2, 3 ndi 6) komanso ngati wachiwiri kapena wachitatu wothandizira odwala omwe alimbana ndi gefitinib ndi / kapena erlotinib (LUX-Lung 1, 4 ndi 5). LUX-Lung 1 ndi 2 awonetsa, m'magulu awo, kuwonjezeka kwakukulu kwa kuchuluka kwa matenda a 58 ndi 86%, motsatana, komanso kutalikitsa kwakukulu kwa kupulumuka kopanda kupita patsogolo. Mayeso ena azachipatala a Phase III pano akupitiliza kuyesa afatinib kuphatikiza paclitaxel (LUX-Lung 5), ndikuyerekeza ndi cisplatin / pemetrexed (LUX-Lung 3) kapena cisplatin / gemcitabine (LUX-Lung 6).

AASraw ndiye katswiri wopanga Afatinib.

Chonde dinani apa kuti mumve zambiri: Ochezera ife

 

 Afatinib mu chordoma yakutsogolo komanso metastatic chordoma

Awa ndi mayeso a Phase 2 omwe amaphunzira za mphamvu ya mankhwala osokoneza bongo a khansa wotchedwa afatinib. Afatinib imalepheretsa mapuloteni a EGFR, omwe amakhulupirira kuti amatenga nawo gawo poyendetsa kukula kwa zotupa za chordoma. Kafukufukuyu adapangidwa makamaka kwa odwala chordoma azaka 18 kapena kupitilira apo omwe ali ndi zotupa zobwerezabwereza kapena metastatic. Ikusegulidwa ku Leiden University Medical Center (LUMC) ndi University College London Hospital (UCLH) ndipo idzatsegulidwa ku Istituto dei Nazionale Tumori (INT) ku Milan m'miyezi ikubwerayi. Ofufuzawo pa kafukufukuyu ndi Dr. Hans Gelderblom ku LUMC, Dr. Silvia Stacchiotti ku INT, ndi Dr. Sandra Strauss ku UCLH.

Epidermal Growth Factor Receptor (EGFR) ndi puloteni yomwe imapezeka pamwamba pamaselo ena mthupi lonse. Nthawi zambiri, EGFR imathandizira kuwongolera kukula kwa maselo ndipo imathandizira kuchiritsa kwa bala. Mu khansa ina, kuphatikiza ma chordomas ambiri, EGFR imayamba kugwira ntchito kwambiri, ndikupangitsa kuti ma cell a khansa achuluke.

Mankhwala omwe amaletsa EGFR otchedwa "EGFR inhibitors" amavomerezedwa kuti athetse mitundu ingapo ya khansa. Afatinib ndi EGFR inhibitor yomwe pakali pano imavomerezedwa kuti ithetse khansa ya m'mapapo yomwe siying'ono-yaying'ono ndipo ikuyesedwa mumitundu ina ya zotupa.

Ma EGFR inhibitors angapo awonetsedwa kuti amachepetsa kapena kuyimitsa kukula kwa ma chordoma cell ndi zotupa za chordoma mu mbewa. Mwa ma inhibitors onse a EGFR omwe adayesedwa, afatinib inali yothandiza kwambiri pamitundu yama mbewa ya chordoma. M'mitundu ina yama mbewa, imachedwetsa kukula kwa zotupazo, pomwe zina zidapangitsa kuti zotupazo zichepe kwambiri. Mlanduwu cholinga chake ndi kudziwa ngati afatinib ikhoza kuchepa kapena kuyimitsa kukula kwa zotupa za chordoma mwa odwala omwe ali ndi matenda obwerezabwereza kapena a metastatic.

 

Reference

[1] Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel Frühjahr 2013. (m'Chijeremani)

[2] Spreitzer H (13 Meyi 2008). "Neue Wirkstoffe - Tovok". Österreichische Apothekerzeitung (m'Chijeremani) (10/2008): 498.

[3] Li D, Ambrogio L, Shimamura T, Kubo S, Takahashi M, Chirieac LR, ndi al. (Ogasiti 2008). "BIBW2992, choletsa kusinthika kwa EGFR / HER2 choletsa kwambiri m'magulu am'mapapo am'mapapo". Oncogene. 27 (34): 4702–11. onetsani: 10.1038 / onc.2008.109. PMC 2748240. PMID 18408761 (Adasankhidwa)

[4] "Giotrif: EPAR-Zambiri Zazogulitsa" (PDF). European Medicines Agency. Boehringer Ingelheim Mayiko GmbH. 16 October 2013. Yotulutsidwa 28 Januware 2014.

[5] Kobayashi Y, Togashi Y, Yatabe Y, Mizuuchi H, Jangchul P, Kondo C, et al. (Disembala 2015). "EGFR Exon 18 Kusintha kwa Khansa Yam'mapapo: Olosera Zam'magazi Othandizira Kuwonjezeka kwa Afatinib kapena Neratinib Poyerekeza ndi TKIs Yoyamba kapena Yachitatu". Kafukufuku wa Khansa Yachipatala. 21 (23): 5305–13. onetsani: 10.1158 / 1078-0432.CCR-15-1046. PMID 26206867.

[6] Lin NU, Wopambana EP, Wheatley D, Carey LA, Houston S, Mendelson D, et al. (June 2012). "Kafukufuku wachiwiri wa afatinib (BIBW 2992), yemwe sangasinthe banja la ErbB, mwa odwala omwe ali ndi khansa ya m'mawere ya HER2 ikupita pambuyo pa trastuzumab". Kafukufuku wa Khansa ya m'mawere ndi Chithandizo. 133 (3): 1057-65. onetsani: 10.1007 / s10549-012-2003-y. MAFUNSO: PMC 3387495. PMID 22418700.

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