He aha ka ʻike āu e ʻike ai ma mua o ka hoʻohana ʻana iā Erlotinib - AASraw
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ʻO Erlotinib

 

  1. He aha ʻo Erlotinib?
  2. Pehea e hana ai ʻo Erlotinib?
  3. He aha nā maʻi e mālama pinepine ai ʻo Erlotinib?
  4. Pehea e hoʻohana ai ʻo Erlotinib i kēia manawa ma ke keʻena maʻi?
  5. I nā maʻi hea ka hopena ʻoi loa ʻo Erlotinib?
  6. He aha ke kūʻē ʻana ʻo Erlotinib?
  7. He aha nā pilikia i hui pū ʻia me Erlotinib?
  8. ʻO nā lāʻau a me nā mea hoʻohui paha e launa pū me Erlotinib?
  9. Ua ʻae ʻo FDA i ka lapaʻau ʻo Erlotinib
  10. hōʻuluʻulu manaʻo

 

He aha ʻO Erlotinib

Erlotinib (CAS:183321-74-6) pili i kahi papa o nā lāʻau i ʻike ʻia me nā mea kāohi ʻia ʻo tyrosine kinase. Hana ia ma ke kāpae ʻana i ka hana o kahi protein i kapa ʻia ka ʻepekema ulu ulu epidermal (EGFR). ʻIke ʻia ka EGFR ma ka ʻili o nā hunaola maʻi ʻaʻai e like me nā hunaola maʻamau. Mālama ʻia ia me he "antenna," ke loaʻa nei nā hōʻailona mai nā pūnaewele ʻē aʻe a me ke kaiapuni e haʻi i ka cell e ulu a māhele. He mea nui ka EGFR i ka ulu a me ka hoʻomohala prenatally a i ka wā kamaliʻi a kōkua i ka mālama ʻana i ka hoʻololi maʻamau o nā hunaola kahiko a ʻino hoʻi i nā mākua. Eia nō naʻe, nui nā pūnaewele maʻi ʻaʻai i loaʻa ka nui o ka nui o ka EGFR ma ko lākou ʻili, a i ʻole ua hoʻololi ʻia ko lākou EGFR e ka hoʻololi ʻana o ka DNA e hāpai ana i ka code genetika no ka protein. ʻO ka hopena ʻo ia nā hōʻailona e hele mai ana mai ka EGFR ikaika loa, e alakaʻi ana i ka ulu nui ʻana o ka cell a me ka mahele, kahi hiʻohiʻona o ka maʻi ʻaʻai.

 

Pehea ʻO Erlotinib Hana? 

ʻO ka hana o ka antitumor clinical hana o erlotinib ʻaʻole i hōʻike piha ʻia. Hoʻopili ʻo Erlotinib i ka phacorylac intracellular o ke kinase tyrosine e pili ana i ka epidermal ulu factor receptor (EGFR). Kekahi kikoʻī o ka pāpā ʻana e pili ana i nā recrect kinase tyrosine ʻē aʻe ʻaʻole i ʻike piha ʻia. Hōʻike ʻia ʻo EGFR ma ka ʻili o nā hunaola maʻamau a me nā hunaola maʻi ʻaʻai.

 

He aha nā maʻi e hana ai ʻO Erlotinib Mālama nui? 

(1) ʻO ka maʻi kano

ʻO Erlotinib i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi ʻole ke hoʻohui ʻia i ka chemotherapy e hoʻomaikaʻi i ke ola holoʻokoʻa e 19%, a hoʻomaikaʻi i ke ola manuahi holomua (PFS) e 29%, ke hoʻohālikelike ʻia i ka chemotherapy wale nō. Ua ʻae ʻo US Food and Drug Administration (FDA) erlotinib no ka hoʻomaʻamaʻa ʻana i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi kūloko a metastatic ʻole i kūleʻa i ka liʻiliʻi ma mua o hoʻokahi regimana chemotherapy.

I ka maʻi ʻaʻai māmā, ua hōʻike ʻia ka maikaʻi o erlotinib i nā mea maʻi me ka ʻole o nā hoʻololi EGFR, akā ʻoi aku ka maikaʻi o nā mea maʻi me nā hoʻololi EGFR. ʻO ke ola holoʻokoʻa, ke ola manuahi o ka holomua a me hoʻokahi makahiki ke ola e like me ka laina laina maʻamau. kaukaʻi (docetaxel a i ʻole pemetrexed). ʻO ka helu pane maʻamau e pili ana iā 50% ʻoi aku ka maikaʻi ma mua o ka chemotherapy laina ʻelua. ʻO nā maʻi ʻo ka poʻe puhipaka ʻole ʻole, a me nā mea puhipaka māmā mua, me adenocarcinoma a i ʻole subtypes e like me BAC e loaʻa ana i nā mutations EGFR, akā hiki ke hoʻololi i nā ʻano maʻi āpau. . Ua hoʻomohala ʻia kahi hōʻike no ka hoʻololi EGFR e Genzyme.

 

(2) ʻO ka kanesa Pancreatic

I Nowemapa 2005, ua ʻae ʻo FDA i ka erlotinib me ka gemcitabine no ka mālama ʻana i ka maʻi kūpale kūloko kūloko.

ʻO AASraw ka mea hana hana na Erlotinib.

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

 

(3) Ke kūpaʻa i ka lāʻau

Ua hoʻopaʻa ʻia ʻo Erlotinib iā ErbB1 ma ka hoʻonā 2.6A; Kākoʻo ke aniani i ka hydrophobicity. I ka hihia o erlotinib hiki pinepine kēia i nā 8-12 mau mahina mai ka hoʻomaka ʻana o ka lāʻau. Ma muli o 50% o ke kūʻē ʻana i hopena ʻia i ka ʻeke paʻa ATP o ka EGFR kinase domain e pili ana i ka hakahaka o kahi koena polar threonine me kahi koena nonpolar methionine (T790M). ʻelima receptor mea ulu ulu, ʻo ia ka mea e hoʻohuli iā ERBB20 i ka hoʻoulu ʻia ʻana o PI3K.

 

ʻO Erlotinib

 

Pehea Is Erlotinib Ci kēia manawa UIn The Clinic?

Ua ʻae mua ʻia ʻo Erlotinib e ka United States Food and Drug Administration (FDA) no ka hoʻohana ʻana i nā mea maʻi me ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi i hoʻi hou ma hope o hoʻokahi ʻano ʻano lāʻau. I ka 2005, ua ʻae ʻia no ka hoʻohana pū ʻana me kekahi lāʻau ʻē aʻe, gemcitabine, no ka maʻi ʻaʻai pancreatic holomua. I ka makahiki 2010, ua hoʻonui ʻia ka hoʻohana ʻana e komo pū me ka mālama mālama no nā mea maʻi me ka maʻi ʻaʻai liʻiliʻi liʻiliʻi ʻoi loa ka maʻi i kūpaʻa ma hope o ʻehā mau hanana o ka mālama ʻana me kahi lāʻau i hoʻokumu ʻia ma ka platinum, e like me cisplatin a i ʻole carboplatin. ʻO nā mea maʻi e lawe nei i ka erlotinib e hoʻomanawanui mau i ka lāʻau. ʻO nā hopena ʻaoʻao maʻamau ka hū o ka ʻili a me ka diarrhea.

 

In Wʻo ia Ppuʻuwai Is Erlotinib Mʻost Epili?

I loko o nā makahiki he XNUMX i hala iho nei, ua loaʻa i nā kauka he nui i ka ʻike me nā mea kālai lāʻau tyrosine kinase, e like me erlotinib, ālai i ka EGFR Ua lilo ka maopopo loa i ka hana pono ʻana o kēia mau lāʻau i nā mea maʻi nāna lung maʻi 'aʻai hali i kahi ʻano hoʻololi e hopena i kahi protein EGFR pono ʻole. ʻO kēia mau mea maʻi he poʻe kūloko lākou i ʻAsia, nā wahine, a ʻaʻole loa e puhipaka me kahi ʻano o ka maʻi ʻaʻa maʻi i kapa ʻia ʻo bronchoalveolar adenocarcinoma. No laila, i ka 2013, ʻae ʻia ʻo erlotinib e lilo i lapaʻau mua loa no kēia hui o nā mea maʻi, inā ʻaʻole hiki ke hōʻola ʻia ko lākou maʻi ʻaʻa.

 

Heaha Is Erlotinib Rʻākeʻe

He maikaʻi loa ʻo Erlotinib i ka subset o nā mea maʻi e hāpai ana i nā hoʻololi EGFR. Eia nō naʻe, e hoʻomaka kēia mau maʻi e hōʻike i ka holomua o kā lākou maʻi ʻaʻai ma hope o 12 mau mahina o ka erlotinib therapy. Loaʻa kēia i ka ulu ʻana o ke kūpaʻa i ka lāʻau i nā koena maʻi ʻaʻai. I nā manawa he nui, nā hopena kūʻē mai ka hoʻomohala ʻana o kahi hoʻololi ʻelua i ka protein EGFR e pale ai i ka erlotinib mai ka hoʻopili ʻana i ka domain kinase tyrosine. ʻO nā ala hou i ka mālama ʻana i kēia mau maʻi e komo pū me kahi mea hoʻomākino hou i kūkulu ʻia ʻo tyrosine kinase afatinib, hoʻokahi a i ʻole hui pū ʻia me cetuximab (Erbitux), kahi e kāpae i ka EGFR e kahi ʻano ʻokoʻa.

 

He aha nā pilikia i hui pū ʻia me Erlotinib?

I nā noiʻi ʻana, ʻo nā hopena maʻa mau me Erlotinib ke hoʻohana ʻia ma ke ʻano he monotherapy no ka maʻi ʻaʻa maʻi ʻo ka huhū (e pili ana i 75% o nā mea maʻi), ka maʻi palahēhē (54%), ka nele o ka makemake a me ka luhi (52% pākahi). I ke aʻo ʻana o Tarceva i hoʻohana ʻia me ka gemcitabine no ka maʻi ʻaʻai pancreatic, ʻo ka hopena maʻamau ka luhi (e pili ana i 73% o nā mea maʻi), ʻōwili (69%) a me ka palahī (48%). No ka papa inoa piha o nā hopena a me nā kapu me Erlotinib, e ʻike i ka pepa leaflet.

 

ka mea Dkapeta a Snā mea hoʻonui Ipāʻani With Erlotinib?

ʻO CYP3A4 kahi enzyme i ke akepaʻa e haki a kōkua i ka hoʻopau ʻana i ka erlotinib mai ke kino. ʻO nā lāʻau lapaʻau e kāohi iā CYP3A4 hiki ke hopena i nā pae kiʻekiʻe o erlotinib i ke kino, a ʻo nā pae kiʻekiʻe ke hopena i ka hopena mai ka erlotinib. ʻO ia mau lāʻau e pili ana i ka atazanavir (Reyataz), clarithromycin (Biaxin), indinavir (Crixivan), itraconazole (Sporanox), ketoconazole (Nizoral), nefazodone (Serzone), nelfinavir (Viracept), ritonavir (Norvir), saquinavir (Invasv) telithromycin (Ketek), a me voriconazole (VFEND). I nā mea maʻi e loaʻa ana i kēia mau lāʻau, pono ʻia kahi mahele haʻahaʻa o erlotinib e pale ai i ka mea ʻino.

Hoʻonui kekahi mau lāʻau i ka hoʻopau ʻia ʻana o erlotinib e ka hoʻonui ʻana i ka hana o nā CYP3A4 enzyme. Hoʻoemi kēia i nā kiʻekiʻe o erlotinib i ke kino a hoʻemi paha i ka hopena. ʻO nā laʻana o ia ʻano lāʻau e like me rifampicin (Rifadin), rifabutin (Mycobutin), rifapentine (Priftin), phenytoin (Dilantin), carbamazepine (Tegretol), phenobarbital a me St. John's Wort. Pono e hōʻalo i kēia mau lāʻau i nā mea maʻi e lawe ana i erlotinib, inā hiki. Inā ʻaʻole koho nā lāʻau ʻē aʻe, koi ʻia nā lāʻau ʻoi loa o erlotinib. ʻO ka uahi paka ʻana kekahi e hoʻoliʻiliʻi i ka nui o erlotinib i ke koko. Kūkā ʻia nā mea maʻi e haʻalele i ka puhipaka.

ʻO nā lāʻau e hoʻemi ana i ka hana o ka waikawa i loko o ka ʻōpū e hoʻoliʻiliʻi i ka lawe ʻana o erlotinib. No laila, protet pump pump (PPI's, ʻo kahi laʻana, omeprazole [Prilosec, Zegerid]) ʻaʻole pono e lawelawe ʻia me erlotinib, a pono e lawelawe ʻia ʻo erlotinib i 10 mau hola ma mua o ka H2-receptor blockers (e laʻa me Ranitidine [Zantac]) ke lawe nei i ka H2-receptor blocker.

Pono e hoʻokaʻawale i ka lawelawe ʻana i nā antacids mai ka lawelawe ʻana o erlotinib e kekahi mau hola. Ua pili ʻo Erlotinib me ka nui o ka makaʻu o ke kahe ʻana, ʻo ia hoʻi i nā mea maʻi e lawe ana i ka warfarin (Coumadin). Pono e nānā pono ʻia nā mea maʻi e lawe ana iā warfarin.

 

Ua'āponoʻiaʻo FDA ʻO Erlotinib lapaʻau

Ma ʻOkakopa 18, 2016, ua hoʻololi ka US Food and Drug Administration i ka hōʻailona no erlotinib (TARCEVA, Astellas Pharm Global Development Inc.) no ka mālama ʻana i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi liʻiliʻi (NSCLC) e kaupalena i ka hoʻohana ʻana i nā mea maʻi i loaʻa i nā tumors i kikoʻī i ka ulu ʻana o ka meaola (EGFR).

Pili ka hoʻololi lepili i nā mea maʻi me ka NSCLC e mālama nei a i ʻole ka mālama ʻana i ka laina ʻelua a ʻoi paha. E kaupalena ʻia kēia mau hōʻailona i kēlā mau maʻi i loaʻa i ko lākou tumors iā EGFR exon 19 kāpae a i ʻole exon 21 L858R mea hoʻololi e like me ka mea i ʻike ʻia e kahi hōʻike i ʻāpono ʻia e ka FDA. Ua kaupalena ʻia ka hōʻailona laina mua i nā mea maʻi me ka EGFR exon 19 hoʻopau a i ʻole exon 21 hoʻololi hoʻololi.

Hoʻokumu ʻia kēia waihona lepili i nā hopena o ka hoʻāʻo IUNO, kahi randomized, double-blind, placebo-control, hoʻokolokolo ʻia o erlotinib i lawelawe ʻia ma ke ʻano he mālama mālama i nā maʻi he 643 me ka NSCLC holomua i ʻike ʻole i ka holomua o ka maʻi a i ʻole ke ʻino kūpono ʻole i nā wā ʻehā o laina chemotherapy laina ma muli o ka platinum. ʻO nā mea maʻi i kū nā pūpū i ka hoʻoulu ʻana i nā mutations EGFR (exon 19 Delete a exon 21 L858R mutations) i kāpae ʻia mai kēia hoʻokolokolo ʻana. Hoʻohui ʻia nā mea maʻi ma 1: 1 e loaʻa iā erlotinib a i ʻole placebo waha i hoʻokahi manawa i kēlā me kēia lā (322 erlotinib, 321 placebo) a hiki i ka holomua ʻana o ka maʻi a i ʻole ka ʻawahia ʻae ʻole ʻia. Ma hope o ka holomua ʻana ma ka lāʻau lapaʻau mua, ua hiki i nā mea maʻi ke komo i kahi pae hāmama. He kanalima pākēneka o nā mea maʻi i randomized i erlotinib i komo i ka wehe-label phase a loaʻa chemotherapy, ʻoiai ʻo 77% o nā mea maʻi i randomized i placebo i komo i ka open-label phase a loaʻa erlotinib.

ʻO ka hopena mua o ka hoʻokolokolo ke ola holoʻokoʻa. Ua hōʻike ʻia nā hopena i ke ola ʻana ma hope o ka mālama ʻana me erlotinib ʻaʻole i ʻoi aku ka maikaʻi ma mua o ka placebo i lawelawe ʻia ma ke ʻano he mālama i nā mea maʻi me nā tumors NSCLC metastatic ʻaʻole e mālama i nā hoʻololi o ka EGFR. ʻAʻohe ʻokoʻa i ke ola manuahi o ka holomua ma waena o ka lima erlotinib a me ka lima placebo i ʻike ʻia.

ʻAʻole e koi ʻo FDA i nā koi ma hope o ke kūʻai aku ʻana a noi i nā hoʻokō kia hope e pili ana i nā hopena o ka hoʻokolokolo IUNO.

ʻO AASraw ka mea hana hana na Erlotinib.

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

 

hōʻuluʻulu manaʻo

ʻO Erlotinib kahi lāʻau synthetic i kuhikuhi ʻia no ka mālama ʻana i ka maʻi ʻaʻai. Ua ʻae ʻia e mālama i ka maʻi ʻaʻai liʻiliʻi liʻiliʻi ʻole, ka maʻi ʻaʻai prostate metastatic holomua i mua, a no ka maʻi ʻaʻai pancreatic. Loiloi i nā hopena ʻaoʻao, nā mahele lāʻau, nā launa lāʻau, nā ʻōlelo aʻoaʻo a me nā mālama, a me ka ʻike palekana o ka hāpai ma mua o hoʻohana ʻO Erlotinib.

 

Reference

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[2] "Ua ʻae ʻo FDA iā Roche Test ma ke ʻano he CDx no Tarceva no ka mālama ʻana i kekahi mau maʻi NSCLC". ʻO GenomeWeb. Ua kiʻi ʻia 10 Ianuali 2020.

[3] Dudek AZ, Kmak KL, Koopmeiners J, et al. (2006). "Hoʻopili ka wīwī o ka ʻili a me ka bronchoalveolar histology me ka pōmaikaʻi olakino i nā mea maʻi i mālama ʻia me gefitinib ma ke ʻano he lāʻau hoʻomākino no ka maʻi maʻi ʻāpā liʻiliʻi ʻole liʻiliʻi liʻiliʻi". Kanesa Maʻi Lung. 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: Insulintor like factor factor-I receptor signaling and loaʻa resist to gefitinib (ZD1839; Iressa) in umauma kanaka a me ka prostate maʻi 'aʻai keena. Ka maʻi ʻaʻai Endocr Relat. 2004 Dec; 11 (4): 793-814.

[5] Kobayashi K, Hagiwara K (2013). "ʻO ka ulu ʻana o ka Epidermal factor receptor (EGFR) a me ka hoʻomaʻamaʻa pilikino ʻana i ka maʻi ʻaʻaʻa nonsmall cell lung (NSCLC)". Oncology i māka ʻia. 8 (1): 27–33. hana: 10.1007 / s11523-013-0258-9. PMC 3591525. PMID 23361373.

[6] Cohen, Martin H. Johnson, John R.; Chen, Yeh-Fong; Sridhara, Rajeshwari; Pazdur, Richard (ʻAukake 2005). "Hōʻuluʻulu ʻae ʻae lāʻau FDA: erlotinib (Tarceva) papa". ʻO Oncologist. 10 (7): 461–466.

[7] Blum G, Gazit A, Levitzki A: Substrate hoʻokūkū hoʻokūkū o ka IGF-1 receptor kinase. ʻO Biokimia 2000 Dec 26; 39 (51): 15705-12.

[8] "Ka lāʻau lapaʻau maʻi ʻaʻai: ʻAe ka ʻaha kiʻekiʻe iā Cipla e kāpae i ka hoʻopiʻi kūʻē iā Roche". ʻO ka wā hoʻokele waiwai. 16 Iune 2017. Archive from the original on 24 December 2019. Ua kiʻi ʻia 23 December 2019.

[9] Delbaldo C, Faivre S, Raymond E: [Nā mea kūpaka ulu ulu Epidermal]. ʻO Rev Med Interne. 2003 Jun; 24 (6): 372-83.

[10] Chen X, Ji ZL, Chen YZ: TTD: Pūnaewele Hōʻailona Therapeutic. ʻO Nucleic Acids Res. 2002 Ian 1; 30 (1): 412-5.

[11] Filppula AM, Neuvonen PJ, Backman JT: Nānā in vitro o nā hopena kaohi manawa hilinaʻi i ka hana CYP2C8 a me CYP3A e nā mea hanaola kinase ʻumikūmāhā. ʻO ka hoʻolei Metab lāʻau lāʻau. 2014 Jul; 42 (7): 1202-9. hana: 10.1124 / dmd.114.057695. Epub 2014 Apr 8.

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