@media only screen and (-Webkit-min-device-pixel-ratio: 1.5), only screen and (-moz-min-device-pixel-ratio: 1.5), only screen and (-o-min-device-pixel-ratio: 3/2), only screen and (min-device-pixel-ratio: 1.5) { }
Hana ʻo AASraw i nā pauka NMN a me NRC i ka nui!

ʻO Gefitinib

  1. ʻO Overview Gefitinib
  2. ʻO Gefitinib Mekanism o ka hana
  3. Hoʻohana ʻo Gefitinib i ka Honua
  4. Nā ʻaoʻao ʻaoʻao o Gefitinib
  5. Mālama pūnaewele Gefitinib
  6. ʻImi Hou: "Killer Cancer Lung" Gefitinib

 

ʻO Gefitinib Overview

ʻO Gefitinib kahi mea kāohi i ke kinase. , kahi hui mole moleka o 4 daltons a he pauka kala keʻokeʻo. He kumu manuahi ʻo Gefitinib. He pKas ka mole o 3 a me 4. Hiki ke wehewehe ʻia ʻo Gefitinib e like me ka hiki ke hoʻoheheʻe liʻiliʻi ʻia ma ka pH 7, akā hiki ʻole ke hoʻoheheʻe ʻia ma luna o ka PH 6, me ka hoʻoliʻiliʻi e hoʻoliʻiliʻi nui ana ma waena o ka pH 3 a me ka pH 4. i ka pyridine, hiki ke hoʻoheheʻe liʻiliʻi ʻia i ka tetrahydrofuran, a me ka hiki ke hoʻoheheʻe ʻia i ka methanol, ethanol (22%), ethyl acetate, propan-24-ol a me acetonitrile.

Loaʻa nā papa Gefitinib e like me nā papa i uhi ʻia me nā kiʻi ʻoniʻoni, me 250 mg o ʻO Gefitinib ka lehu, no ka hoʻoponopono waha. ʻO nā mea hana ʻole o ka huna papa o IRESSA papa he lactose monohidate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate a me ka magnesium stearate. Hoʻokomo ʻia ka uhi papa o hypromellose, polyethylene glycol 300, titanium dioxide, red ferric oxide a me yellow ferric oxide.

 

kōmike Information:

inoa ʻO Gefitinib
Kapa inoa N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
Kāleka CAS 184475-35-2
'O Synonyms ZD 1839
Ka Lā Molecular C22H24ClFN4O3
Kaumaha Kaumaha 446.9
Purity ≥98%
Hoʻoponoponoʻia He pōhakuʻeleʻele
Palekana 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)
Kauihi InChi XGALLCVXEZPNRQ-UHFFFAOYSA-N
pūnaewele -20 ° C

 

Hoʻohana ʻia ʻo Gefitinib e mālama i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi i pāhola ʻia i nā wahi ʻē aʻe o ke kino i ka poʻe me kekahi ʻano tumors. Aia ʻo Gefitinib i ka papa o nā lāʻau i kapa ʻia ʻo nā kinase inhibitors. Hana ia ma ka pale ʻana i ka hana o kekahi mea kūlohelohe e pono ai e kōkua Ka maʻi 'aʻai mahuahua nā hunaola.

ʻO AASraw ka mea hana ʻoihana o Gefitinib.

E ʻoluʻolu e kaomi ma aneʻi no ka ʻike ʻōlelo. Hana iā mākou

 

ʻO Gefitinib Ka hana hana

ʻO Gefitinib kahi mea kāohi o ka mea ulu epidermal factor receptor (EGFR) tyrosine kinase e hoʻopili ana i ka adenosine triphosphate (ATP) -e paʻa ana i ka pūnaewele. Hōʻike pinepine ʻia ʻo EGFR e hōʻike ākea ʻia i loko o kekahi mau hunaola kino kanaka, e like me ka akemāmā a me ka umauma ka maʻi kanesa. Alakaʻi ʻo Overexpression i ka hoʻonui ʻana i ka hoʻoulu ʻana o nā cascades transduction hōʻailona anti-apoptotic Ras, a laila hopena i ka hoʻonui ʻana i ke ola o nā hunaola maʻi ʻaʻai a me ka hoʻonui ʻia ʻana o ka cell. ʻO Gefitinib ka mea kāohi koho mua o ka EGFR tyrosine kinase i kapa ʻia ʻo Her1 a i ʻole ErbB-1. Ma ke kāpae ʻana i ka EGFR tyrosine kinase, ua kāohi ʻia hoʻi nā cascades hōʻailona o lalo, a laila ua hōʻemi ʻia ka hoʻonui ʻia ʻana o nā pūnaewele malignant.

 

ʻO Gefitinib E hoʻohana i ka Honua

Kūʻai ʻia ʻo Gefitinib ma nā ʻāina he 64. Ua ʻae ʻia a kūʻai ʻia ʻo Gefitinib mai Iulai 2002 i Iapana, a lilo ia i ʻāina mua i lawe mai i ka lāʻau.

ka Ua ʻae ʻo FDA i gefitinib i Mei 2003 no ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC). Ua ʻae ʻia e like me monotherapy no ka mālama ʻana i nā mea maʻi me ka NSCLC holomua a metastatic paha ma hope o ka holo pono ʻole ʻana o nā chemotherapies e pili ana i ka platinum a me nā docetaxel, ma ke ʻano he kolu o ka laina therapy.

I Iune 2005 ua haʻalele ka FDA i ka ʻae no ka hoʻohana ʻana i nā mea maʻi hou ma muli o ka nele o ka hōʻike e hoʻonui i ke ola.

Ma ʻEulopa ua hōʻike ʻia ʻo gefitinib mai ka 2009 i ka NSCLC holomua ma nā laina a pau o ka mālama ʻana no nā mea maʻi e ʻoki nei i nā hoʻololi EGFR. Ua hāʻawi ʻia kēia lepili ma hope o ka hōʻike ʻana o gefitinib ma ke ʻano he lālani mua e hoʻomaikaʻi i ke ola me ka manuahi o ka holomua vs. a me ke aupuni pāpālua o ka platinum i nā mea maʻi e kū nei i kēlā ʻano hoʻololi. ʻO IPASS ka mea mua o nā hoʻokolohua ʻehā pae III i hōʻoia i ke kiʻekiʻe gefitinib i kēia heluna hoʻomanawanui.

I ka hapanui o nā ʻāina ʻē aʻe kahi e kūʻai ʻia ai ʻo gefitinib i kēia manawa ua ʻae ʻia no nā mea maʻi me ka NSCLC kiʻekiʻe i loaʻa i hoʻokahi kaukani chemotherapy i hala. Eia nō naʻe, ʻo nā noi e hoʻonui i kona lepili ma ke ʻano he lālani mua i nā maʻi e mālama nei i nā hoʻololi EGFR i kēia manawa e hana ʻia ma muli o nā hōʻike ʻepekema hou loa. EGFR hoʻololi no ka naive kūloko a i ʻole metastatic, unresectable NSCLC. Hāʻawi kālā ākea ʻia kēia no kahi manawa 2012 mau mahina a me ka hoʻololi hou inā ʻaʻohe holomua. I Iulai 4, 13, ua ʻae ʻo FDA i ka gefitinib ma ke ʻano he lālani mua no NSCLC.

ʻO Gefitinib

Nā ʻaoʻao ʻaoʻao o ʻO Gefitinib

Nā mea nui e hoʻomanaʻo e pili ana i nā hopena ʻē aʻe o gefitinib:

♦ ʻAʻole ʻike ka hapa nui o ka poʻe i nā ʻaoʻao āpau i helu ʻia.

♦ Kuhi pinepine nā hopena ʻaoʻao ma nā ʻano o kā lākou hoʻomaka a me ka lōʻihi.

♦ ʻAneʻane hiki ke hoʻohuli i nā hopena ʻaoʻao a hele aku ma hope o ka pau ʻana o ka mālama ʻana.

♦ Nui a hewahewa nā koho e kōkua i ka hōʻemi a pale ʻana paha i nā hopena ʻaoʻao.

ʻAʻohe pilina ma waena o ke alo a me ke koʻikoʻi o nā hopena a me ka hopena o ka lāʻau.

 

ʻO nā hopena ʻē aʻe i maʻa mau (loaʻa i ʻoi aku ma mua o 30%) no nā mea maʻi e lawe ana i gefitinib:

♦ Diarrhea

♦ Ka hopena o ka ʻili (hū, huehue)

ʻO AASraw ka mea hana ʻoihana o Gefitinib.

E ʻoluʻolu e kaomi ma aneʻi no ka ʻike ʻōlelo. Hana iā mākou

 

ʻO kēia mau hopena ʻaoʻao nā hopena ʻē aʻe i ʻike pinepine ʻia (loaʻa ma kahi o 10-29%) o nā maʻi e loaʻa ana iā gefitinib:

♦ Nausea

♦ Ke noi nei

♦ Kāwili

♦ Makemake maikaʻi ʻole

♦ Hoʻonāukiuki maka

 

ʻO nā hihia kakaikahi (ma kahi o 1%) o kahi hopena koʻikoʻi o ka maʻi ākea interstitial (pneumonia, a i ʻole ka mumū o nā mumū me ka ʻole o ka maʻi. I ka hopena o kēia hopena, hele pinepine ʻia e ka hanu paʻakikī me ka pākeke a i ʻole ke kuni haʻahaʻa e koi ana i ka haukapila. ʻO 1/3 o nā hihia i alakaʻi i ka make. Inā piʻi koke ka manawa o ka hanu, kahe a me / a i ʻole ke kuni ke lawe ʻia ʻo gefitinib, e hoʻomaopopo i kāu ʻoihana mālama ola.

ʻO ke kiʻekiʻe i nā hoʻokolohua hana ate (transaminase, bilirubin, a me nā alkaline phosphatase) i mālama ʻia i nā mea maʻi i mālama ʻia me gefitinib. ʻAʻole hele pū ʻia kēia mau kiʻekiʻe e nā ʻōuli o ka hona ʻino. Eia nō naʻe, hiki i kāu ʻoihana mālama ola ke nānā i nā hoʻokolohua koko e nānā i kāu hana ate i kēlā me kēia manawa, ʻoiai ʻoe e lawe nei iā gefitinib.

ʻAʻole i helu ʻia nā hopena ʻaoʻao āpau ma luna. Kākaʻikahi kekahi mau mea (e hana ana ma lalo o 10% o nā maʻi) ʻaʻole i helu ʻia ma aneʻi. Eia nō naʻe, pono ʻoe e hoʻomaopopo mau i kāu mea mālama ola inā ʻike ʻoe i nā ʻōuli maʻamau.

 

Gefitinib pūnaewele

E mālama iā gefitinib i loko o ka pahu i komo ʻia i loko, pani paʻa loa ʻia, a ʻaʻole i hiki i nā kamaliʻi. E mālama iā ia i ka mahana wela o ka lumi a mamao aku mai ka wela a me ka momona (ʻaʻole i loko o ka lua.

Pono e hoʻolei ʻia nā gefitinib pono ʻole ma nā ala kūikawā e hōʻoia i hiki ʻole i nā holoholona, ​​nā keiki, a me nā kānaka ʻē aʻe ke hoʻopau iā lākou. Eia naʻe, ʻaʻole pono ʻoe e kaomi i kēia gefitinib i lalo i ka lua. Ma kahi o, ke ala ʻoi loa e hoʻolilo ai i kāu gefitinib ma o kahi papahana hoʻihoʻi lāʻau. E kamaʻilio me kāu kauka lāʻau a kāhea paha i kāu ʻōpala a me nā hana hoʻopōʻaiapuni kūloko e aʻo e pili ana i nā papahana hoʻihoʻi i kou kaiāulu. E ʻike i ka Ka hoʻolei palekana ʻana o kā FDA pūnaewele i ka pūnaewele no ka ʻike hou aku inā ʻaʻole ʻoe e komo i kahi papahana hoʻihoʻi.

He mea nui ka mālamaʻana i nā lāʻau a pau mai kaʻikeʻana a hiki i nā keiki e like me nā pahu (e like me nā pilina o ka pule hebedoma a me ka mea no nā maka o ka maka, ka'ōpū, nā pāpale, a me nā mea inu)ʻaʻole hiki ke kū'ē i ka'ōpiopio a hiki i nā keiki'ōpiopio ke wehe iā lākou. No ka paleʻana i nā keiki liʻiliʻi mai ka lāʻauʻawaʻawa, e hoʻopaʻa mau i nā piko palekana a kau koke i ka lāʻau i kahi wahi palekana - kahi eʻoi aku ana i waho a ma waho aku o ko lākou mau maka a hiki.

ʻO Gefitinib

ʻImi Hou: "Killer Cancer Lung" Gefitinib

ʻO Gefitinib kahi lāʻau i hoʻomākaukau ʻia e pale i ka hana tyrosine kinase o ka mea ulu ulu epidermal e ka hoʻokūkū hoʻokūkū ʻana i ka pūnaewele paʻa ATP. Ma nā noiʻi preclinical ua hōʻike ʻo gefitinib i ka hana mana i loko o nā ʻano tumere, e like me nā laina o nā pūnaeho maʻi ʻaʻai pūpū a me nā xenografts. ʻElua mau haʻawina nui randomized Phase II (IDEAL 1 a me IDEAL 2) i hōʻike ʻia i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi i hōʻike i kahi pane pane e hoʻokokoke ana i 20% i nā mea maʻi laina ʻelua a ∼10% i kēlā mau mea i hana ʻia me ʻelua a ʻoi paha regimens chemotherapy. ʻO ke ola waena ma kēia mau noiʻi ʻelua i hoʻokokoke i 6 mau mahina. Ma ke ʻano he laina laina mua, ua loiloi ʻia ʻo gefitinib i ka hoʻohui ʻia me nā regimens chemotherapy ʻelua i loko o ʻelua mau noiʻi randomized (INTACT 8 a me INTACT 1). ʻAʻole i hōʻike ʻia nā noiʻi ʻelua i kahi hoʻomaikaʻi ʻana i ke ola ʻana ma ka huina nui o nā mea hoʻomanawanui o> 2 mau maʻi i kēlā me kēia noi. ʻO nā kiko hope ʻē aʻe (e laʻa, ka manawa i ka holomua a me ka pane pane) ʻaʻole i hoʻomaikaʻi ʻia e ka hoʻohui ʻana o gefitinib. Hōʻike ʻia nā noiʻi hou e loiloi i ke kuleana o gefitinib i ka mālama ʻana i nā maʻi i loaʻa ka chemotherapy a i ʻole chemoradiotherapy. ʻImi ʻia nā noiʻi e noiʻi ana iā gefitinib ma ke ʻano he monotherapy laina mua.

ʻO ka hapa nui o nā mea maʻi me ka liʻiliʻi liʻiliʻi lung maʻi 'aʻai (NSCLC) i ka hopena e hoʻomōhala i ka maʻi metastatic a i ʻole ka maʻi ʻaʻole maikaʻi i nā lāʻau kūloko wale nō a he moho hiki no nā ʻōnaehana ʻōnaehana. ʻOiai ʻo chemotherapy hiki ke hoʻomaikaʻi i ke ola i nā mea maʻi me ka maʻi ʻoi loa, ʻo ka pōmaikaʻi he ∼2 mau mahina wale nō ma mua o ke kākoʻo kōkua maikaʻi loa, a ʻo kēia ke kumu kūʻai o nā hopena maikaʻi ʻole. ʻO ka ʻimi no nā ʻākena hou e like me ka chemotherapy akā ʻoi aku ka maikaʻi o ka ʻae ʻana. A helu o nā puke Agena e hana kikoʻī kūʻē i nā wae koho i kū ma Ka maʻi 'aʻai nā pūnaewele, e like me ka ʻepekema ulu ulu ʻepekema (EGFR), ke hoʻāʻo ʻia nei i ka NSCLC holomua. I kēia manawa, ua loiloi ʻia nā mea maʻi me ka NSCLC holomua, akā aia kahi kumu kūpono e nānā ai i kekahi o kēia mau ʻelele i nā hoʻonohonoho maʻi ma mua, kahi o kekahi o nā ʻōnaehana genetics i kuhi ʻia.

Hōʻike nui ʻia ʻo EGFR i nā tumors paʻa like ʻole, e like me NSCLC. Hōʻike nui ʻia ʻo EGFR i ka hapanui (∼80%) o nā cell caromasomas ʻōpala māmā, a me ka hapalua o nā adenocarcinomas pūnana āpau a me nā carcinomas nui pūnaewele. Ua hōʻike ʻia ka hoʻoulu ʻana o ka EGFR i nā hunaola maʻi ʻino e hoʻolaulaha i nā hana e pili ana i ka ulu ʻana o ka cell tumor, angiogenesis, invasion, a me metastasis, a me ka pāpā ʻana i ka apoptosis ʻO EGFR (erbB1 a i ʻole HER1) kahi lālā o ka ʻohana receptor erbB, a ʻo ia hoʻi ʻo erbB2 (HER2), erbB3 (HER3), a me erbB4 (HER4). He glycoprotein transmembrane ia i haku ʻia me kahi palena ligand-binding extracellular, kahi kikowaena transmembrane, a me kahi kikowaena-transducing kikowaena intracellular me ka hana tyrosine kinase. Ma hope o ka hoʻopaʻa ʻana i kahi ligand physiological e like me ka mea ulu epidermal, hoʻemi ka EGFR me kekahi monomer EGFR a i ʻole lālā ʻē aʻe o ka ʻohana erbB. Ke alakaʻi nei kēia i ka hoʻoulu ʻana o ka tyrosine kinase, ka autophosphorylation of tyrosine, a me ka hoʻomaka ʻana o nā cascades hōʻailona e hopena i nā pane i lalo e like me ka hoʻonui ʻana o ka cell. Eia kekahi, ua pili ka hōʻike ʻana o ka EGFR i nā tumors me kahi pane maikaʻi ʻole i ka hoʻōla, hoʻomohala ʻana i ke kūpaʻa lāʻau cytotoxic, ke piʻi nei o ka maʻi, a me ke ola maikaʻi ʻole. ʻO nā ʻano hana ʻē aʻe o ka hoʻonui ʻia ʻana o ka hōʻailona EGFR e pili ana i ka hoʻonui ʻia o ka cell tumor me ka hoʻonui ʻia o nā pae o ka ligand extracellular, ka heterodimerization o EGFR, a me ka hoʻololi EGFR. ʻO ke ʻano maʻamau o ka EGFR mutated i nā tumors ʻo EGFRvIII, i loaʻa a hiki i 39% o nā hihia NSCLC. Hāpai ʻo EGFRvIII i kahi mutation holoi ʻia mai nā amino acid 6 a 273 i loko o ke kāʻei paʻa extracellular a hōʻike i ka hana Constitive tyrosine kinase kūʻokoʻa i ka paʻa ligand extracellular.

ʻO AASraw ka mea hana ʻoihana o Gefitinib.

E ʻoluʻolu e kaomi ma aneʻi no ka ʻike ʻōlelo. Hana iā mākou

 

Reference

[1] Rukazenkov Y, Speake G, Marshall G, et al. ʻO nā mea ulu ulu Epidermal receptor tyrosine kinase nā mea kāohi: like akā ʻokoʻa? Nā lāʻau lapaʻau anticancer 2009; 20: 856-866.

[2] ʻO Woodburn JR ka ʻepekema ulu ulu epidermal a me kāna mea kāohi i ka maʻi maʻi maʻi maʻi. ʻO Pharmacol Ther 1999; 82: 241-250.

[3] Pūʻulu Hui PūʻIa Līkiʻi Puʻupuʻu liʻiliʻi liʻiliʻi. Chemotherapy i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi: kahi meta-analysis me ka hoʻohana ʻana i ka ʻikepili hou i kēlā me kēia mea maʻi mai 52 mau hoʻokolohua hoʻokolohua kaulike ʻia. BMJ 1995; 311: 899–909.

[4] ʻO Douillard JY, Kim ES, Hirsh V, et al. ʻO Gefitinib (IRESSA) me ka docetaxel i nā mea maʻi me ka maʻi kūpē liʻiliʻi liʻiliʻi kūloko a i ʻole metastatic i mālama mua ʻia me ka chemotherapy ma muli o ka platinum. ʻO J Thoracic Oncol 2007; 2: PRS-02–

[5] Fukuoka M, Wu Y, Thongprasert S, et al. Nānā ʻia ʻo Biomarker mai kahi pae III, i hoʻonohonoho ʻia, wehe-lepili, laina laina mua o gefitinib (G) me ka carboplatin / paclitaxel (C / P) i nā mea maʻi i koho ʻia (pts) me ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC) i ʻĀkia (IPASS). ʻO J Clin Oncol 2009; 27 Hōʻawi. 15: 8006–.

[6] ʻO Reck MA kahi hana nui i ka hoʻoponopono pilikino ʻana o ka maʻi ʻaʻai a me gefitinib: ka hoʻāʻo IPASS a ʻoi aku. ʻO Expert Rev Anticancer Ther 2010; 10: 955–965.

[7] ʻO Barker, AJ Haʻawina e alakaʻi ana i ka ʻike o ZD1839 (IRESSA): kahi waha wahaheʻe, mea koho epidermal ulu mea receptor tyrosine kinase mea hoʻopōkole i mālama ʻia i ka maʻi ʻaʻai. ʻO Bioorg. Med. Kemika Lett 11, 1911-1914 (2001).

[8] Wakeling, AE et al. ZD1839 (Iressa): kahi mea hoʻopuka waha waha o ka mea ulu epidermal e hōʻailona me ka hiki no ka maʻi maʻi maʻi maʻi. ʻO Res. 62, 5749-5754 (2002).

[9] Yarden, Y. & Sliwkowski, MX Wehe i ka pūnaewele hōʻailona ErbB. ʻAnoʻao Rev. Mol. Pūnaewele Biol. 2, 127–137 (2001).

[10] Cersosimo, RJ Lung cancer: he loiloi. ʻAm. J. Health Syst. Pāka lāʻau. 59, 611-642 (2002).

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