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Regorafenib

 

  1. Chii chinonzi Regorafenib?
  2. Nei Regorafenib Yakagamuchirwa neDFA?
  3. Regorafenib Inoshanda Sei?
  4. Chii chinonzi Regorafenib Main Inoshandiswa?
  5. Ndeapi mabhenefiti eReorafenib akaratidzirwa muZvidzidzo?
  6. Ndeapi Ngozi / Matambudziko anounzwa naRegorafenib May?
  7. Ini ndinochengeta sei uye / kana kukanda kunze Regorafenib?
  8. Ramangwana mafambiro eRegorafenib
  9. mhedziso

 

Chii Regorafenib?

Regorafenib (CAS: 755037-03-7), inotengeswa pasi pezita rezita Stivarga pakati pevamwe, ndeyemuromo yakawanda-kinase inhibitor yakagadzirirwa neBayer inotarisa angiogenic, stromal uye oncogenic receptor tyrosine kinase (RTK). Regorafenib inoratidza anti-angiogenic chiitiko nekuda kwayo mbiri yakatarisana VEGFR2-TIE2 tyrosine kinase inhibition. Kubva gore ra2009 yakadzidzwa senge ingangoita yekurapa sarudzo mumhando dzakasiyana dzemota.Paka gore ra2015 yaive iine mvumo mbiri dzeUS kumatenda epamberi.

 

Nei Regorafenib Approved ne FDA

The European Medicines Agency yakafunga kuti mabhenefiti aRegorafenib akakura kupfuura njodzi dzayo uye akakurudzira kuti igamuchirwe kuti ishandiswe muEU. Komiti yakaona kuti mukenza yakajeka. Mabhenefiti maererano nekuwedzera kurarama kwevarwere aive nemwero, asi akafunga kuti akakunda njodzi muvarwere vasina dzimwe nzira dzekurapa dzakasara. Zvisinei, zvichipiwa mhedzisiro, CHMP yakaona zvakakosha kuti utsvage nzira dzekuziva chero subgroups dzevarwere vanogona kupindura Stivarga.

Nezve GIST neHCC, Komiti yakaona kuti maonero haana kunaka kuvarwere vane chirwere chinonyanya kuwedzera kunyangwe kurapwa kwekutanga. Stivarga akange aratidzwa kunonoka kuwedzera kwechirwere muvarwere ava. Kune varwere vane HCC, izvi zvakatungamira mukuvandudzwa kwehurefu hwenguva varwere yavakagara. Iyo mhedzisiro mhedzisiro yeStivarga inogoneka.

 

Zvinoita Sei Regorafenib Basa? 

Regorafenib idiki mamorekuru inhibitor yeakawanda membrane-yakasungwa uye intracellular kinases inobatanidzwa mune zvakajairika maseru mashandiro uye mune pathologic maitiro senge oncogenesis, tumor angiogenesis, uye kugadziriswa kweiyo tumor microenvelo. In in vitro biochemical or cellular assays, regorafenib kana ayo makuru anoshanda emametabolites M-2 uye M-5 akatadzisa chiitiko cheRET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, uye Abl pazvikamu zve regorafenib zvakawanikwa mukiriniki. Mune in vivo modhi, regorafenib yakaratidza anti-angiogenic chiitiko mune gonzo bundu modhi, uye inhibition yekukura kwechirwere pamwe neanti-metastatic chiitiko mune akati wandei mbeva xenograft modhi kusanganisira zvimwe zvevanhu colorectal carcinoma.

AASraw ndiye nyanzvi yekugadzira Regorafenib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Chii Regorafenib Main Inoshandiswa?

Regorafenib imushonga wekenza une chinhu chinoshanda regorafenib powder. Inoshandiswa yega kurapa anotevera cancer.

Cancer Colorectal cancer (kenza yemuura uye rectum) yakapararira kune dzimwe nhengo dzemuviri;

Ast Gastrointestinal stromal tumor (GIST, gomarara remudumbu uye ura) iro rakapararira kana risingakwanise kuvhiyiwa;

③ Hepatocellular carcinoma (HCC, gomarara rechiropa).

Regorafenib inoshandiswa muvarwere vakatorapwa, kana vasingakwanise kupihwa, kumwe kurapa kuripo. Kune kenza yakajeka, izvi zvinosanganisira chemotherapy inoenderana nemishonga inonzi fluoropyrimidines uye kurapwa neimwe kenza mishonga inozivikanwa seye anti-VEGF uye anti-EGFR mishonga. Varwere vane GIST vaifanira kunge vakaedza kurapwa ne imatinib uye sunitinib uye varwere vane HCC vaifanira kunge vakaedza sorafenib vasati vatanga kurapwa naRegorafenib.

 

Regorafenib

 

Ndeapi mabhenefiti e Regorafenib zvakaratidzwa muStudies?

 Colorectal cancer

Mune ongororo huru inosanganisira varwere mazana manomwe nemakumi matanhatu vane metastatic colorectal cancer iyo yakanga yafambira mberi mushure mekurapa kwakajairika, Regorafenib akafananidzwa ne placebo (dummy kurapwa) uye chiyero chikuru chekubudirira kwaive kupona kwese (kureba kwenguva yakagara varwere). Vese varwere vakagashira rubatsiro rwekutsigira, kusanganisira mishonga yekurwadziwa uye kurapwa kwezvirwere. Chidzidzo ichi chakaratidza kuti Regorafenib yakavandudza kupona, nevarwere vakarapwa vanogara kwemwedzi 760 paavhareji, zvichienzaniswa nemwedzi mishanu kune avo vakapihwa placebo.

 

 GORA(Yakawedzera Gastrointestinal Stromal Tumors)

Mune kumwe kuongorora kukuru, Regorafenib akafananidzwa ne placebo mune varwere makumi maviri nevapfumbamwe vane GIST iyo yakanga yapararira kana kusashanda uye avo vakapiwawo rutsigiro rwakanyanya. Kuchengetwa kunotsigira kwaisanganisira kurapwa senge kurwadziwa kwekurwadziwa, mishonga inorwisa mabhakitiriya, uye kuwedzerwa ropa zvinobatsira murwere asi pasina kurapa kenza. Chidzidzo ichi chakaratidza kuti Regorafenib ine rubatsiro rwekutsigira yaishanda mukuwedzera urefu hwenguva iyo varwere vairarama pasina chirwere chavo chichiwedzera. Varwere vanorapwa naRegorafenib vakararama paavhareji kwemwedzi 4.8 pasina chirwere chavo kuchinyanya kuenzaniswa kana 0.9 mwedzi yevarwere vari kutora placebo uye nerutsigiro.

 

 HCC(Yakawedzera Hepatocellular Carcinoma)

Mune chidzidzo chikuru chinosanganisira varwere mazana mashanu nemakumi manomwe nenomwe vane HCC iyo yakanyanya kuwedzera mushure mekurapwa ne sorafenib, Regorafenib yakaenzaniswa ne placebo uye chiyero chikuru chekubudirira kwaive kupona kwese. Vose varwere vakagamuchirawo rubatsiro rwekutsigira. Chidzidzo ichi chakaratidza kuti Stivarga yakawedzera hurefu hwenguva iyo varwere vaigara zvachose, nevarwere vaibatwa naRegorafenib vachirarama kwemwedzi 10.6 paavhareji, zvichienzaniswa nemwedzi 7.8 yeavo vakapiwa placebo.

 

Ndezvipi Ngozi / Side effects zvinoita Regorafenib Unogona Kuunza?

Infection. Regorafenib inogona kukonzeresa njodzi yepamusoro yekutapukirwa kunyanya kweti yeurinary, mhuno, huro nemapapu. Regorafenib inogona kutungamira kune yakanyanya njodzi yehutachiona hutachiona hweiyo mucous membrane, ganda kana muviri. Udza mupi wako wezvehutano ipapo kana iwe ukawana fivha, kukosora kwakakomba pamwe kana pasina kuwedzera muhutsi (sputum) kugadzirwa, huro hwakanyanya, kupfupika kwekufema, kupisa kana kurwadziwa paunenge uchiita weti, kubuda kwechikadzi zvisina kujairika kana kutsamwa, kutsvuka, kuzvimba kana kurwadziwa chero nhengo yemuviri

Skubuda ropa zvakanyanya. Regorafenib inogona kukonzera kubuda ropa, izvo zvinogona kuve zvakakomba uye dzimwe nguva zvichitungamira kurufu. Udza mupi wako wezvehutano kana iwe uine chero zviratidzo zvekubuda ropa paunenge uchitora Regorafenib, inosanganisira: kurutsa ropa kana kana marutsi ako achitaridzika senge nzvimbo yekofi, pingi kana pini weti, tsvuku kana nhema (inoita kunge tara) zvigaro, kukosora ropa kana kuwanda kweropa, kubuda kumwedzi kunorema kupfuura zvakajairwa, kubuda ropa kwechikadzi zvisina kujairika, kubuda ropa mumhino kunoitika kazhinji, kupwanya, uye musoro wakareruka.

A kubvarura mudumbu mako kana mudumbu mudumbu (ura perforation). Regorafenib inogona kukonzera kuchema mudumbu mako kana mumatumbo madziro anogona kuve akakomba uye dzimwe nguva kutungamira kurufu. Bata wako mupi wezvehutano nekukurumidza kana iwe ukaona kurwadziwa kwakanyanya kana kuzvimba mudumbu rako nzvimbo (mudumbu), fivha, kutonhora, kusvotwa, kurutsa, kana kupera mvura.

A dambudziko reganda rinonzi ruoko-rutsoka ganda kuita uye rakakomba ganda mapundu. Maoko-tsoka tsoka ganda rinowanzoitika uye dzimwe nguva rinogona kunge rakakomba. Udza mupi wako wezvehutano ipapo kana iwe ukawana kutsvuka, kurwadziwa, mablisters, kubuda ropa, kana kuzvimba pamaoko emaoko ako nepasi petsoka dzako, kana kuputika kwakanyanya.

High kukwira kweropa. Ropa rako rinofanirwa kuongororwa vhiki rega rega kwemavhiki matanhatu ekutanga ekutanga Regorafenib. Ropa rako rinofanirwa kuongororwa nguva nenguva uye chero yakakwira BP inofanira kurapwa paunenge uchigamuchira Regorafenib. Udza mupi wako wezvehutano kana iwe uine kurwadziwa kwakanyanya kwemusoro, kureruka-musoro, kana shanduko mune chako chiratidzo.

Dkudzikamisa kuyerera kweropa kuenda kumoyo nekurwadziwa kwemoyo. Tora rubatsiro rwechimbichimbi kana uine kurwadziwa kwepfupa, uine mweya wekufema, unonzwa dzungu, kana kunzwa sekunge uchapfuura.

A mamiriro anonzi anodzoserwa kumashure poshure leukoencephalopathy syndrome (RPLS). Fonera wako mupi wezvehutano ipapo kana iwe uchinge wakakomba musoro, kubatwa, kuvhiringidzika, shanduko muchiono, kana matambudziko kufunga

Risk yemaronda ekuporesa matambudziko. Maronda anogona kusapora mushe panguva yekurapwa kweRegorafenib. Udza mupi wako wezvehutano kana iwe ukaronga kuita chero kuvhiyiwa usati watanga kana panguva yekurapwa naRegorafenib.

▪ Unofanirwa kurega kutora Regorafenib kweinenge vhiki mbiri usati wavhiyiwa.

▪ Mubatsiri wako wezvehutano anofanira kukuudza iwe paunotanga kutora Regorafenib zvakare mushure mekuvhiyiwa.

Mhedzisiro inowanzoitika neRegorafenib inosanganisira kurwadziwa kunosanganisira dumbu-nzvimbo (dumbu); kuneta, kushaya simba, kuneta; manyoka (kazhinji kana akasununguka ura); kuderera kwechido; hutachiona; izwi shanduko kana hoarseness; kuwedzera mune kumwe kuongorora kwechiropa; kupindwa nechando; kuzvimba, kurwadziwa, uye kutsvuka kwemukati mumuromo mako, pahuro, mudumbu, uye ura (mucositis); uye kuonda.

AASraw ndiye nyanzvi yekugadzira Regorafenib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Ini ndinochengeta sei uye / kana kukanda kunze Regorafenib?

♦ Chengeta mahwendefa mumudziyo wepakutanga mukamuri yekushisa. Chengeta chivharo chakanyatsovharwa. Usatora iyo antimoisture cube kana packet.

Away Rasa chero chikamu chisati chashandiswa mavhiki manomwe mushure mekuvhura bhodhoro.

♦ Chengeta munzvimbo yakaoma. Usachengete muimba yekugezera.

Chengetedza mishonga yese munzvimbo yakachengeteka. Chengetedza mishonga yose pasingasviki vana nezvipfuyo.

Ow Rasa zvinodhaka zvisina kushandiswa kana zvapera. Usadonhedze chimbuzi kana kudururira donhwe kunze kwekunge waudzwa kudaro. Tarisa nemufarisi wako kana uine mibvunzo nezve nzira yakanakisa yekurasa zvinodhaka. Panogona kunge paine zvirongwa zvekutora zvinodhaka munzvimbo yako.

 

Regorafenib

 

Future directions of Regorafenib

Makore mashanu mushure mekubvumidzwa, regorafenib inoramba iri mishonga ine mashoma ekurapwa kwekubata. Kutenderwa kushandiswa mukenza yakajeka, GIST uye HCC ndeye chete yemhando yepamusoro yechirwere. Yakasanganiswa nemutengo wakakwira, parizvino pane zvishoma zvekubatsira varwere. Zvakare, kuyedza kwakasiyana kuri kuitiswa kuitira kuti iitsanangure senzira nyowani yekurapa. Nhungamiro yemberi yechirwere ichi inosanganisira manejimendi yeosteosarcoma. Imwe yazvino placebo-inodzorwa, yakapofumadzwa bofu kutongwa muFrance yakaratidza kuwedzera kwekuenderera-kwemahara kupona nechinhu chevatatu muvarwere vane metastatic osteosarcoma iyo yakundikana mutsara wese wekurapa. Zvinomanikidza, idzi nyowani dhata dzinoratidza kubatsirwa pane yakakwira metastatic chirwere senzira yekupedzisira, zvakafanana nezvose zvazvino zvinogamuchirwa zvinoshandiswa.

Dzazvino dhata dzinoratidza zvinogona kuitika synergic maitiro pakati pe regorafenib uye immune checkpoint inhibitors, sezvakaratidzwa muREGONIVO kuyedza. (38% mukenza yemudumbu uye 44% mukenza yakajeka) uye inokanganisika mhedzisiro mhedzisiro muboka rakabatana. Iyi bhenefiti inokatyamadza inogona kunge iri yekudzikiswa kwemarara-inosanganisirwa macrophages ne regorafenib, ichiwedzera kusanzwisisika kwetumour kune nivolumab. Parizvino, iyo REGONIVO chikamu II kutongwa kuri kuitika uye inogona kukurumidza kutsigira iyi fungidziro. Pamusoro pezvo, chikamu chekupedzisira chechipiri chemakiriniki ekuyedzwa chakaratidza kuti regorafenib iri nani pane lomustine mune yepamusoro uye yakadzokororazve glioblastoma. Iyo REGOMA kuyedzwa, muItari, yakaratidza kuvandudzwa kwakakosha muhupenyu hwese (hazard ratio 36; 0.50% nguva yekuvimba 95-0.33; log-chinzvimbo p = 0.75) zvichienzaniswa neye lomustine kurapa.

Iwo REVERSE zvidzidzo zvakaitwa ne regorafenib uye cetuximab mukurapa kwe metastatic colorectal cancer. Mhedzisiro yakawanikwa pane kutevedzana kwekushandiswa kwemishonga yakadaro pakurapa gomarara iri inoratidza kuti iro rakarongeka raizove iro rekutanga manejimendi regorafenib ichiteverwa necetuximab, zvakasiyana neyakajairwa protocol parizvino. Mhedzisiro yacho yakaratidza kuvandudzwa kwekupona kwevarwere uye bhenefiti yacho yaitaridzika kunge ichitungamirwa zvakanyanya nebasa rakakura recetuximab pane regorafenib sekurapa kwechipiri.

Iyo INTEGRATE kutongwa kwe regorafenib monotherapy mukenza yemudumbu yakaratidza kuti uyu mushonga wakanyatsoshivirirwa uye kuti pakange pasina kukuvara muhupenyu hwevarwere zvichienzaniswa neavo vakagamuchira placebo uye kuti zvaisaratidzika kunge zvine mhedzisiro yakaipa pamipimo iyoyo kubva kune huturu. Mapurojekiti ekutsvagisa akasimbisa kuti hwaro hwekutanga hwemarwadzo, chishuwo, kuputirwa, uye kushanda kwemuviri zvakawanikwa zvichikosha kufungidzira kwekupona. Zvakare, kuyedzwa uku kwakaratidza kuti regorafenib yaive nebasa rakakura mukutanga kufambira mberi- kwemahara kupona kwekupedzisira. REDOS kutongwa kwakaitwa kubva 2015-2018 uye vanyori vakaratidza kuti dhosi-yekukwira nzira ye regorafenib ndeimwe nzira inogoneka kune yakajairwa regorafenib dosing zano re160 mg / zuva, kunyanya kune varwere vane metastatic colorectal cancer. Izvo zvakare zvakawanikwa kuti varwere vanorapwa nedosi kukwira vaine yakakwira frequency yekumashure-kufambira mberi kurapwa uye huwandu hwakareba kupona kwese.

Nezve kushivirira kwe regorafenib kana uchishandiswa kurapa colorectal cancer, dhata dhata inowanikwa pane shiviriro muvanhu vakuru vevarwere, uye danho rinofanirwa kuitwa tichifunga nezve kushomeka kwekupona kubatsirwa uye nehuturu chimiro. Tichifunga nezve ichi chinodhaka mukurapa kweCCC, mapurojekiti ekutsvagisa anosimbisa kuti kune chimiro chinogamuchirwa chekushivirira uye kuti regorafenib inopa bhenefiti yekupona. GIST kurapwa, vanyori vanoverengeka vanotaura kuti regorafenib inoregererwa zvakanaka pasina zvinotarisirwa zvisingatarisirwi.

Kuenderera mberi nekutsvaga kunodiwa kuti uone kuti ndevapi varwere vanogona kubatsirwa zvakanyanya kubva kune uyu mushonga. Kubva muna2019, miedzo iri kuenderera irikuedza kuti regorafenib inogona kuvandudza mhedzisiro mune dzakapfava materu sarcomas, senge osteogenic sarcoma, liposarcoma, Ewing sarcoma uye rhabdomyosarcoma.

 

mhedziso

Kunyangwe makore mashanu ekubvumidzwa uye achivimbisa pharmacodynamics, regorafenib yakaratidza yakaganhurirwa, asi yakaverengerwa kukosha, kubatsirwa kwemhando dzakasiyana dzemamota akasimba. Zvinyorwa zvakanyorwa zvine kenza yakajeka, GIST uye HCC. Yepamberi chikamu chechipiri miedzo yakaratidza kunatsiridza kwakanyanya mukupona kwekenza yemudumbu, glioblastoma uye osteosarcoma, iyo inogona kuratidza kuiswa mune ramangwana muzviratidzo zvakanyorwa.

Musanganiswa wekurapa ne immune checkpoint inhibitors yakaratidzirwa seinobatsira muchikamu chekutanga miedzo, uye yechikamu chechipiri cheyedzo chiri kuitwa. Parizvino, regorafenib iri kuongororwa kune mamwe kanzira futi. Mazhinji mhedzisiro mhedzisiro inogona kushandiswa seanomakisa emigumisiro iri nani nekurapwa. Pakati peavo, ruoko-tsoka tsoka uye hypothyroidism ndiyo inonyanya kuenderana nekuvandudza kupona. Muchidimbu, zvidzidzo zvakaratidza kuti regorafenib inogona kusimudzira zvakanyanya kupona nekushivirira kunogamuchirwa mune dzakasiyana mamota akasimba.

AASraw ndiye nyanzvi yekugadzira Regorafenib.

Ndokumbirawo ubaye pano kuti uwane ruzivo pasinaCont Cont us

 

Reference

[1] Krishnamoorthy SK, Relias V, Sebastian S, et al. Manejimendi e regorafenib-ane hukama huturu: ongororo. Ther Adv Gastroenterol. 2015; 8: 285-97.

[2] Thangaraju P, Singh H, Chakrabarti A. Regorafenib: inoverengeka tyrosine kinase inhibitor: kupfupikiswa kwekugona kwayo kwekurapa pakurapa metastatic colorectal carcinoma uye epamberi ematumbo stromal tumors. Indian J Kenza. 2015; 52: 257-60.

[3] Grünewald FS, Prota AE, Giese A, Ballmer-Hofer K. Structure-basa ongororo yeEGEGF receptor activation uye iro basa revanoona musimboti mune angiogenic siginecha. Biochim Biophys Acta Mapuroteni Proteomics. 2010; 1804: 567-80.

[4] Shinkai A, Ito M, Anazawa H, et al. Mepu yenzvimbo dzinosanganisirwa musangano wegandand uye kupatsanurwa padanho rekunze kweiyo kinase insert domain-ine receptor yevascular endothelial kukura chinhu. J Biol Chem. 1998; 273: 31283-8.

[5] Fuh G, Li B, Crowley C, uye al. Zvinodikanwa zvekusunga nekusayina kweiyo kinase domain receptor yevascular endothelial kukura chinhu. J Biol Chem. 1998; 273: 11197-204.

[6] Eriksson A, Cao R, Roy J, et al. Diki GTP-inosunga mapuroteni Rac ndeye muyananisi akakosha wevascular endothelial kukura chinhu-inosimudzira endothelial fenestrations uye vascular kukwana. Kutenderera. 2003; 107: 1532-8.

[7] Ascierto PA, Kirkwood JM, Grob JJ, et al. Basa re BRAF V600 shanduko mu melanoma. J Shandura Med. 2012; 10: 85.

[8] Emuss V, Garnett M, Mason C, Marais R. Kuchinja kweC-RAF hakuwanzoitika mukenza yemunhu nekuti C-RAF ine yakaderera basal kinase chiitiko ichienzaniswa neB-RAF. Cancer Res. 2005; 65: 9719-26.

[9] Bruix J, Qin S, Merle P, et al. Regorafenib yevarwere vane hepatocellular carcinoma avo vakafambira mberi pane sorafenib kurapwa (RESORCE): yakasarudzika, yakapofomara-bofu, inodzorwa ne placebo, chikamu chechitatu kutongwa. Lancet. 3; 2017: 389-56.

[10] Martin AJ, Gibbs E, Sjoquist K, et al. Hupenyu hwakanangana nehupenyu hwehupenyu hwakabatana neregorafenib kurapwa mune inoratidzira yepamusoro gastric adenocarcinoma. Gastric Kenza. 2018; 21: 473-80.

[11] Heo YA, Syed YY. Regorafenib: wongororo muhepatocellular carcinoma. Zvinodhaka. 2018; 78: 951-8.

[12] Yin X, Yin Y, Shen C, Chen H, Wang J, Cai Z, et al. Zviitiko zvakashata zvine njodzi zvine chekuita ne regorafenib mukurapa matumbo akasimba akasimba: meta-ongororo yemiedzo yakasarudzika. Onco Anonanga Ther. 2018; 11: 6405-14.

[13] Lombardi G, De Salvo GL, Brandes AA, et al. Regorafenib kana ichienzaniswa neLomustine mune varwere vane yakadzokororwa glioblastoma (REGOMA): multicentre, yakavhurika-label, yakasarudzika, inodzorwa, chikamu chechipiri kutongwa. Lancet Oncol. 2; 2019: 20-110.

[14] Bekaii-Saab T. Kunyatso tarisa regorafenib. Kliniki Adv Hematol Oncol. 2018; 16: 667-9.

[15] Yoshino K, Manaka D, Kudo R, et al. Metastatic colorectal cancer inopindura regorafenib kwemakore maviri: nyaya yenyaya. J Med Nyaya Rep. 2; 2017: 11.

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