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Lapatinib powder ividiyo


I-apatinib powder Abalinganiswa basisiseko:

igama: ILapatinib powder
CAS: 231277-92-2
I-molecular Formula: C29H26ClFN4O4S
Isisindo somzimba: 581.05
Melt Point: 136-140 ° C
Isitoreji sokugcina: Ifriji
umbala: I-White okanye i-white powstalline powder


1.Tykerb eziphambili zePowder.

igama Tykerb
Iimeko 231277-92-2
I-Molecular Formula C29H26CIFN4O4S
Isisindo somzimba 581.05
umbala I-White okanye i-white powstalline powder
Amanye amagama lapatini


2.Yintoni Tykerb?

Amagama okurhweba iTykerb kunye neTyverb yinyango esetyenziswayo ngomlomo ngomhlaza wesifuba kunye nezinye izicubu ezinzima. Yimbini ye-tyrosine kinase inhibitor ephazamisa i-HER2 / neu kunye ne-epidermal yokukhula kwe-factor receptor (EGFR). Isetyenziswe ngonyango oludibeneyo kumhlaza webele weHER2-positive. Isetyenziselwa unyango lwezigulane ezinomdlavuza ophezulu okanye we-metastatic breast whose tumors are overxpress HER2 (ErbB2) .Amanye amazwe ase-US amkhathaza iTyker kunye neYurophu kunye neRashiya ebizwa ngokuba yiTyverb. NgoJanuwari 2010, uTykerb wamukelwa ngokukhawuleza kunyango lwabasetyhini be-postmenopausal nge-hormone receptor yesifo sengqondo somhlaza we-breastast Lapatinib inqanda iinkqubo ze-receptor zenzeke ngokubopha kwi-ATP- kwi-domain ye-EGFR / HER2 protein kinase, ukuthintela ukuzakhela i-self-phosphorylation kunye nokusebenza ngokulandelelana kwendlela yokubonisa, iTykerb (lapatinib) ngumhlaza womhlaza osetyenziswe kunye nenye ikhambi ebizwa ngokuba yi-capecitabine (Xeloda) ukunyanga uhlobo oluthile lomhlaza wesifuba oluphambili oluye lwasasazeka kwezinye iindawo zomzimba, kwaye kaninzi lunikezwa emva kweminye imishanguzo yomhlaza iye yazama ngaphandle kokunyanga impatho yeempawu


3.Kwenzeka njani Tykerb ukusebenza?

unyango lwe-Cancer unyango lujolise ngokutsha ekubulaleni ngokukhawuleza ukwahlula iiseli kuba enye yeengqambela zesifo somhlaza wentlungu kukuba bahlula ngokukhawuleza. umhlaza webele iiseli.Izintlobo ezahlukeneyo zonyango ezijoliswe kuzo, ezichazwe kwiindidi ezintathu ezibanzi. Ezinye iinkqubo ezijoliswe kuzo zijolise kumacandelo angaphakathi kunye nomsebenzi weselfini somhlaza wesifuba. Iipilisi ezijoliswe kuzo zisebenzisa i-molecule ezincinci ezingena kwiseli kwaye ziphazamise umsebenzi weeseli, zibangela ukuba zife. Kukho iintlobo ezininzi zonyango olujoliswe kuzo ezijolise kwiindawo zangaphakathi zeeseli. Ezinye iithagethi ezijoliswe kuzo zijoliswe kwii-receptors ezingaphandle kweseli. Iipilisi ezijoliswe kwizifunyenwe ziyakwaziwa njengama-antibodies e-monoclonal. I-Antiangiogenesis inhibitors ijolise kwimithambo yegazi eyenza i-oksijeni kwiiseli, ekugqibeleni ibangele iiselingi zilambile.IPertuzumab yintsholongwane ye-monoclonal ejolise kummandla weeseli ze-epidermal growth factor receptor 2 protein (HER2) kumgca wesifo somhlaza, ukuphazamisa i-HER2 ebangela ukufa komhlaza wesifo sebele. I-Pertuzumab ibopha kwindawo eyahlukileyo yeprotheni ye-HER2 kune-trastuzumab ukuze xa i-pertuzumab idibene ne-trastuzumab, ukukhutshwa okupheleleyo kwe-HER2 ukubonakalisa kwenzeka ngaphakathi kwe-HER2-positive cell cell cancer, i-HER2 receptors zisebenzisa iiprotheyini, ezibizwa ngokuba yi-kinases, iseli ukuba ikhule kwaye ihlule ngokungaqhelekanga. I-Kinase ilawula ukusetyenziswa kwamandla amangakanani amaseli ukuba akhule kwaye atyuke. Iiseli zomhlaza zesifuba ezithe gqithisa kakhulu i-HER2 ingaba nomsebenzi omkhulu we-kinase, ngoko iiseli zomhlaza zikhula kakhulu, ngokukhawuleza. I -ykerb isebenza ngokuphazamisana ne-HER2 ezinxulumene ne-cell phone ngaphakathi kweseli, ukunciphisa inani lamanqamu omhlaza webele wamandla kufuneka likhule liphindise . Ngokunciphisa inani lamandla, iTykerb inganciphisa okanye imise ukukhula komhlaza wesisu.


4.Uya kuba iTykerb isebenza kuwe?

Izivavanyo ezine ezahlukeneyo zingasetyenziselwa ukuba zibone ukuba umhlaza ngu-HER2-positive kwaye ukuba uya kuphendula iTykerb:

  • IHC (ImmunoHistoChemistry)

IHC yeyona ngokuqhelekileyo kusetyenziswa yovavanyo ukubona ukuba ithumba uye kakhulu kwi HER2 receptor protein phezu komhlaba umhlaza cells.The IHC uvavanyo inika amanqaku of 0 ukuya 3 + esibonisa imali HER2 receptor iiprothini ngamathumba. Ukuba amanqaku ithumba 0 ku 1 +, ibizwa ngokuba "HER2 negative." Ukuba amanqaku 2 + okanye 3 +, ibizwa ngokuba "HER2 kakuhle." Abafazi kunye IHC amanqaku ezintle ube ukuphendula kakuhle Tykerb. Isilwanyana asibhekanyanga sisebenza kakuhle kwiimvumi kunye nezikolo ze-IHC ze-0 okanye i-1 +.

  • I-FISH (i-Fluorescence In Situation Hybridation)

Uvavanyo lwe-FISH lujonge i-HER2 yesimo esingavamile. Olu vavanyo lulona luchanekileyo, kodwa lungaphantsi, lukwazi ukufumanisa ukuba isisu sebele sisenokuphendula kwiTykerb ..

Xa uvavanyo lwe-FISH, ufumana amanqaku enoba "othe tye" okanye "ongalunganga" (ezinye izibhedlele zibiza uvavanyo olubi "zero"). Ukuba umhlaza ungumthombo we-FISH, mhlawumbi uya kuphendula iTykerb.

Uvavanyo lwe-SpoT-Light HER2 uvavanyo lwe-CISH lubheka iigeri ze-HER2 kwisiqulatho sesisu somhlaza wesifuba. Uvavanyo Spot-Ukhanyiselo isebenzisa ibala eyenza izakhi HER2 / neu ukutshintsha color.With uvavanyo Spot-Ukhanyiselo, ufumana amanqaku nokuba "positive" okanye "ezimbi." Ukuba umhlaza liyavumelana Spot-Ukhanyiselo, cishe phendula kakuhle iTykerb.

  • Yazisa i-HER2 ye-ISH (kwi-Hybridisation Situation)

Ukwazisa uvavanyo lwe-HER2 Dual ISH isebenzisa ibala elikhethekileyo elenza i-HER2 proteins ishintshe umbala. Isalathisi sisetyenziselwa kwisampuli se-cancer yesifuba kwaye ibonwa phantsi kwe-microscope. Olu vavanyo lunikeza iziphumo ezichanekileyo kunokuba uvavanyo lweHC HER.Kukwazisa uvavanyo lweHER2 Dual ISH, ufumana amanqaku okuba "HER2 positive" okanye "HER2 negative".


5.Iyiphi intsebenziswano yezidakamizwa zikaTykerb?

I-Tykerb iqhutywe yi-enzyme yesibindi CYP3A4. Iziyobisi ezivimbela okanye zenza i CYP3A4 zingathintela uxinzelelo lweTykerb emzimbeni. Ama-inhibitors akwandisa amanqanaba egazi kaTykerb kunye nama-inducers anciphisa amanqanaba egazi. Ukulungiswa kwetayiti yeTykerb kufuneka kucatshangelwe kwizigulane ezifumana i-CYP3A4 inhibitors okanye inducitors ezinamandla. Le ilandelayo ke uluhlu olubanzi inhibitors kunye inducers.Inhibitors: ketoconazole, clarithromycin, atazanavir, nefazodone, nelfinavir (Viracept), telithromycin, kunye voriconazole.Inducers: dexamethasone, phenytoin, carbamazepine, rifampin, phenobarbital, kunye Wort St Johns.


6.ITykerb Side Effects

Common imiphumela iTykerb ziquka:

isicathulo, ukuhlanza, isisu esicasulayo, izilonda zomlomo, ukugqithisa, isikhumba esomileyo, intlungu okanye ubomvu kwiintendelezo zezandla zakho okanye iinyawo zeenyawo zakho, ukulahleka kweenwele, iingxaki zeminwe yakho okanye izikhonkwane, ufumane ukulala.Wathi uTykerb unikezwa ngeXeloda chemotherapy , usenokufumana nemiphumo emibi yechemotherapy. Ngokukodwa, i-Xeloda idibene ne-neuropathy, okanye ibomvu kunye nokubetha kwizandla nangeenyawo. Xa iTykerb inikezwa ngo-Femara, nawe unokuba nemiphumo emibi ye-Femara. Iziphumo eziqhelekileyo ze-Femara zincinci kunye nethambo kunye neentlungu ezihlangeneyo. I-Tykerb ayibonakali iyabangela iingxaki ezinzulu zentliziyo kunye nemiphunga ehambelana no-Herceptin. Ukuba ukhulelwe okanye ucinge ukuba unokukhulelwa, xela ugqirha wakho. Ayaziwa ukuba le nkunkuma idlula ubisi lwebele. Ngenxa yengozi yintsana, ukuncelisa xa kusetyenziswa le chiza akukhuthazwa.


7.Iziphi izilumkiso kunye nokuqapha kweTykerb?

  • I-Tykerb inokuchaphazela indlela intliziyo igxotha ngayo igazi. Qinisekisa isiqhekeza esivumelekileyo sesiqhekeza se-ventricular (LVEF) ngaphambi kokuba uqale iTykerb kwaye uqhubeke ubeka iliso ngexesha lokunyanga.
  • I-Tykerb ayikho nto ibangela ukubangelwa kwesibindi. Ukujonga umsebenzi wesibindi ngaphambi kokuba unyango kunye neveki ze-4-6 ngexesha lonyango.
  • ITykerb inokubangela isifo sohudo. Ukuba isifo sohudo sisenzeka, lawula ngamanxiza olwa-diarral and substitution.
  • I-Tykerb inokubangela iingxaki ezinkulu zamaphaphu. Yeka iTykerb ukuba izibonakaliso zezi zinto zenzeka.
  • I-Tykerb inokubangela ukunyamezeka kancinci kwesikhumba. Yeka iTykerb ukuba oko kwenzeka.


8.Iyiphi imilinganiselo yeTykerb?

  • I-Tykerb inikwe iipilisi ze-250 mg. Amacwecwe amahlanu athatyathwa kanye ngosuku ngalunye kwisisu esingenalutho kwiintsuku ze-21 kwimijikelezo yemihla ye-21. Musa ukuchoboza okanye ukuhlaziya iipilisi. Gcina kwiqondo lokushisa lokugcina kwaye ugcine isitya esivaliwe ngokuqinile. T Tykerb unikezwa ngeXeloda (capecitabine) 2000mg / m2 / ngomlomo olawulwa ngomlomo kwi-2 iisadi ezihlukeneyo, iiyure ze-12 ngaphandle kweentsuku zokuqala ze-14 nganye Umjikelezo wonyango lwe-21. I-Capecitabine kufuneka ithathwe ngokutya okanye imizuzu ye-30 emva kokutya.
  • Thatha la mayeza ngokuchanekileyo njengoko ugqirha ugqirha wakho. Landela izikhokelo kwiileyibrari yakho ngokuchanekileyo.
  • Umthamo ugqirha ugqirha unokuthi usekelwe kulo:
  • imeko ephathwayo
  • ezinye iimeko zonyango onayo
  • amanye amayeza owathathayo
  • indlela osabela ngayo kule nyilisi
  • ubunzima bakho, ubude bakho, ubudala bakho, ubulili bakho

Imilinganiselo ephakanyisiweyo ye-lapatinib yomhlaza wesifuba ophezulu okanye we-metastatic isifo se-1,250 mg (iipilisi ze-5) ezinikezwa ngomlomo kanye ngosuku ngemihla ye-1-21.I-dose ephakanyisiweyo ye-lapatinib ye-hormone-receptor-positive (HER2-positive) umdlavuza webele we-metastatic 1,500 mg (Iipilisi ze-6) zinikezwa ngomlomo xa zihamba rhoqo imihla ngemihla ngokudibanisa ne-letrozole.


9.Yintoni i indleko iTykerb?

Umyinge wexabiso lentengo: $ 30.10 nge-tablet ye-250 mg

Uxhasi lweSuku lwe-21 (umjikelezo we-1): $ 3,160.50


10.Iyiphi intsebenziswano yezidakamizwa zikaTykerb?

I-Tykerb iqhutywe yi-enzyme yesibindi CYP3A4. Iziyobisi ezivimbela okanye zenza i CYP3A4 zingathintela uxinzelelo lweTykerb emzimbeni. Ama-inhibitors akwandisa amanqanaba egazi kaTykerb kunye nama-inducers anciphisa amanqanaba egazi. Ulungelelaniso lweentambo zeTykerb kufuneka lucatshangelwe kwizigulane ezithe zaqina CYP3A4 inhibitors okanye inducers. Oku kulandelayo akulona uluhlu olubanzi lwee-inhibitors kunye nabangaphakathi.

Inhibitors: ketoconazole, clarithromycin, atazanavir, nefazodone, nelfinavir (iViracept), i-telithromycin kunye ne-voriconazole.

Ukukhupha: i-dexamethasone, i-phenytoin, i-carbamazepine, i-rifampin, i-phenobarbital kunye ne-St John's wort.


11.Withini xa ndidlula?

Ukuba u ukugqithisai-lapatinib, biza ugqirha wakho okanye isikhulu sokulawula utyhefu, okanye uye kwisibhedlele esiphumeleleyo esibhedlele esibhedlele kwangoko. Thatha amacwecwe e-lapatinib xa kunokwenzeka.


12.Ungafumana phi ulwazi oluninzi?

Khumbula, gcina lo kunye nawo onke amayeza ngaphandle kokufikelela kubantwana, ungaze wabelane ngamayeza akho nabanye, kwaye usebenzise le mayeza kuphela ngenjongo echaziweyo.
Yonke imizamo yenziwe ukuba kuqinisekiswe ukuba ulwazi olunikezwa ngu-AASraw up-to-date, kwaye luzalisekile, kodwa akukho siqinisekiso esenziwe kuloo nto. Ulwazi lweziyobisi oluqulethwe apha lungaba luncedo. Inkcazelo ye-AASraw ihlanganiswe ukuze isebenziswe ngabasebenzi bezempilo kunye nabathengi e-United States kwaye ngoko i-AASraw ayifuni ukuba isebenzise ngaphandle kwe-United States ifanelekile, ngaphandle kokuba iboniswe ngenye indlela. AASrawUlwazi lweziyobisi aluvumeli iziyobisi, ukuxilonga izigulane okanye ukucebisa unyango. Ulwazi lweziyobisi lwe-AASraw luyimithombo yolwazi eyenzelwe ukuncedisa abasebenzi bezempilo abanemvume ekunyamekeleni izigulane zabo kunye / nokuba bakhonze abathengi bebukela le nkonzo njengencediso, kwaye kungabi yinto ethatha indawo, ubuchule, ubuchule, ulwazi kunye nesigwebo sabasebenzi bezempilo. Ukungabikho kwesilumkiso kwisilwanyana esisinikiweyo okanye inkunkuma engekho nto kufuneka kuthethwe ukuba kuboniswe ukuba izilwanyana okanye iziyobisi zikhuselekile, zichanekile okanye zifanelekile naziphi na iziguli. I-AASraw ayicingi nayiphi na imbopheleleko nayiphi na into ebalulekileyo yokunakekelwa kwempilo elawulwa ngoncedo lwengcacisoAASraw inikezela. Ingcaciso equlethwe apha ayihloselwe ukugqithisa zonke izinto ezisetyenziswayo, izikhokelo, izilumkiso, izilumkiso, ukusebenzisana kwezidakamizwa, ukuphendulwa kwezidakamizwa, okanye iziphumo ezimbi. Ukuba unemibuzo malunga neziyobisi othabathayo, jonga ugqirha wakho, umongikazi okanye umkhompiki.


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