Goserelin Txhajyog ib qho hluavtaws gonadotropin- tso tawm cov tshuaj hormones (GnRH) agonist, txawv los ntawm nws lub peev xwm los tswj cov qib hormonal los ntawm kev txhawb nqa - tso tawm daim ntawv ntau npaum li cas rau lub sijhawm ntev - kho cov teebmeem. Kev tswj hwm subcutaneously, nws cov qauv tsim yog ib qho kev txhawb nqa - tso tawm cov tshuaj tso tawm uas ua rau cov tshuaj txuas ntxiv thiab ruaj khov tso tawm hauv lub cev tom qab txhaj tshuaj. Qhov no tshem tawm qhov hassle ntawm cov tshuaj niaj hnub thiab txhim kho kev ua raws li tus neeg mob. Thaum nkag mus rau hauv lub cev, cov tshuaj luv luv nkoos gonadotropin secretion, ua raws li inhibition ntawm hypothalamic-pituitary-gonadal axis los ntawm kev tawm tswv yim tsis zoo, uas maj mam txo cov qib testosterone hauv cov txiv neej lossis cov tshuaj estrogen hauv cov poj niam kom ua tiav cov txiaj ntsig kho mob. Qhov kev ua haujlwm tshwj xeeb no ua rau nws ua tus neeg sawv cev kho mob tseem ceeb rau cov tshuaj hormone{10}}nyob ntawm cov kab mob.
Peb Cov Khoom Muag Khoom
Goserelin COA
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| Certificate of Analysis | ||
| Compound npe | Goserelin | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 65807-02-5 | |
| Ntau | 15g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202512090051 | |
| MFG | Peb 9, 2025 | |
| EXP | Peb 8 Dec 2028 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.90% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500 ppm |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Tshuaj Formula | C59H84N18O14 | |
| Exact Mass | 1268.64 | |
| Molecular Luj | 1269.43 | |
| m/z | 1268.64(100.0%), 1269.64(63.8%), 1270.65(20.0%), 1269.64(6.6%), 1270.64(4.0%), 1271.65(3.3%), 1270.65(2.9%), 1271.65(1.8%), 1271.65(1.3%) | |
| Elemental Analysis | C,55.82; H,6.67; N,19.86; O,17.64 | |
Core Mechanism of Action
Cov kev kho mob tseem ceeb ntawm cov khoom yog nyob rau hauv lub zog thiab txhawb nqa inhibition ntawm androgen qib los ntawm cov lus qhia tsis zoo ntawm cov hypothalamic{0}}pituitary-gonadal axis, uas yog kev kho mob castration, uas hloov cov kev phais phais castration. Nws cov txheej txheem ua haujlwm nyob rau hauv ob theem: Hauv thawj theem, tom qab khi rau pituitary GnRH receptors, cov tshuaj luv luv txhawb kev tso tawm ntawm gonadotropins (luteinizing hormone thiab follicle-stimulating hormone), ua rau lub sijhawm nce siab hauv cov ntshav qib testosterone. Tom qab, los ntawm receptor downregulation, nws inhibits pituitary pituitary inhibition kawg. androgen synthesis thiab secretion, thiab txo cov ntshav testosterone rau qib castration-qhov no hauv paus inhibits proliferation thiab loj hlob ntawm prostate cancer hlwb.
Piv nrog rau kev phais castration, Goserelin muaj qhov zoo ntawm kev thim rov qab: qib hormonal tuaj yeem maj mam rov qab los tom qab tshem tawm cov tshuaj, tawm hauv chav rau kev kho mob hauv cov neeg mob uas xav tau kev xeeb tub lossis cov neeg uas muaj kab mob. Nws kuj zam kev raug mob ntawm kev phais thiab kev puas siab puas ntsws, txhim kho kev ua raws li kev kho mob. Cov txheej txheem tshwj xeeb no ua rau nws yog ib qho ntawm thawj - kab mob endocrine kho rau cov tshuaj hormone- mob qog noj ntshav prostate.
Theem -Cov ntawv thov kev kho mob tshwj xeeb
Metastatic Prostate Cancer: Ib Qhov Tseem Ceeb Ua Ntej -Line Palliative Therapy
Kev kho mob tsis muaj peev xwm ua tau rau cov neeg mob qog nqaij hlav cancer prostate nrog cov metastases nyob deb (xws li, pob txha lossis visceral metastases), thiab lub hom phiaj kho mob hloov mus rau kev tswj cov tsos mob, kab mob kev loj hlob qeeb thiab kev muaj sia nyob ntev. Raws li thawj - kab mob endocrine,Goserelin Txhajtuaj yeem siv ib leeg lossis ua ke nrog antiandrogens (xws li, bicalutamide) kom txo qis androgen sai thiab tswj cov qog nqaij hlav.
Cov kev tshawb fawb soj ntsuam tau pom tias ntev -Goserelin txoj kev kho mob rau cov mob qog nqaij hlav prostate metastatic tau txais txiaj ntsig zoo piv rau kev phais castration thiab txo cov qog nqaij hlav zoo- cov tsos mob xws li mob pob txha thiab hematuria.
Ob qhov kev sim tswj kev sim tau pom tau tias tus kab mob tswj hwm tus nqi thiab kev nce qib -kev muaj sia nyob dawb ntawm cov neeg mob hauv pab pawg kho Goserelin txuas ntxiv tsis yog- qis dua rau cov neeg nyob hauv pawg phais castration, thiab qhov yooj yim ntawm kev txhaj tshuaj tau ua rau ntev - kev kho mob ntau dua rau cov neeg mob.
Locally Advanced Prostate Cancer: Ib Qhov Tseem Ceeb Neoadjuvant thiab Adjuvant Therapy
Cov neeg mob uas muaj mob qog noj ntshav hauv zos (cT3-T4 theem) muaj cov tsos mob tsis zoo nrog kev phais lossis kev kho mob hluav taws xob ib leeg thiab muaj kev pheej hmoo siab rov tshwm sim thiab metastasis; Kev kho kom dav yog txoj hauv kev tam sim no, uas Goserelin ua lub luag haujlwm tseem ceeb hauv ob qho tib si neoadjuvant thiab adjuvant chaw.
Neoadjuvant kev kho mob:
Kev tswj hwm ua ntej kev kho hluav taws xob lossis kev phais, nws lub hom phiaj txo cov qog ntim, txo qis tus kab mob, thiab txhim kho qhov ua tiav ntawm kev kho mob. RTOG8610 txoj kev tshawb fawb pom tau tias pib kho Goserelin 2 lub hlis ua ntej kev kho hluav taws xob thiab txuas ntxiv nws thaum lub sij hawm siv hluav taws xob txo qis hauv zos qog nqaij hlav thiab muaj kev pheej hmoo ntawm radioresistance. Rau kev kho mob preoperative neoadjuvant, kev tswj hwm ntawm Goserelin ua ke nrog abiraterone acetate tau pom tias muaj txiaj ntsig zoo.
Adjuvant kev kho mob:
Rau cov neeg mob uas muaj kev pheej hmoo ntawm rov tshwm sim dua tom qab kev phais mob radical lossis kev kho hluav taws xob, Goserelin tuaj yeem tshem tawm cov qog hlwb ntxiv thiab txo tus nqi rov qab.
Siab -Risk Localized Prostate Cancer: Ib Txoj Cai Radiosensitizing Regimen hauv Kev Sib Txuas Nrog Kev Kho Mob
High-risk localized prostate cancer (e.g., PSA >20ng / mL, Gleason qhab nia Ntau dua lossis sib npaug rau 8) tsis muaj qhov cuam tshuam nyob deb tab sis muaj kev pheej hmoo rov muaj dua, thiab kev kho hluav taws xob ib leeg ua rau muaj txiaj ntsig tsawg. Cov txheej txheem kho mob pom zoo kom siv xov tooj cua ua ke nrog kev kho mob endocrine; raws li tus neeg sawv cev tseem ceeb,Goserelin Txhajtxhim kho radiosensitivity los ntawm hormonal inhibition thiab txhim kho cov txiaj ntsig kev kho mob.
Ib txoj kev tshawb nrhiav tau pib kho Goserelin nyob rau lub lim tiam dhau los ntawm kev siv xov tooj cua thiab txuas ntxiv mus txog thaum muaj kab mob, qhia tias tus kab mob - ciaj sia dawb thiab tag nrho cov ciaj sia nyob ntawm cov neeg mob hauv pab pawg kho mob ua ke tau zoo dua li cov hauv kev kho hluav taws xob - ib leeg, tsis muaj qhov tshwm sim ntawm qhov tshwm sim tsis zoo. Lub hauv paus txheej txheem yog tias androgen deprivation ntes prostate qog nqaij hlav qog nqaij hlav hauv theem G0 / G1, thaum lub sij hawm lawv muaj kev nkag siab ntau dua rau hluav taws xob; Nws kuj tseem txo cov qog angiogenesis kom ntxiv inhibit qog loj hlob.
Kev Tswj Xyuas Kev Nyab Xeeb
Common Adverse Reactions thiab Management
Cov tshuaj tau txais txiaj ntsig zoo- zam, thiab feem ntau cov kev tsis zoo tshwm sim yog kev kho tshuaj kho mob, mob me me, thiab feem ntau tsis tas yuav muaj kev cuam tshuam kev kho mob, kev daws teeb meem tom qab tshem tawm cov tshuaj. Cov kev phiv tshwm sim feem ntau muaj xws li kub hnyiab, hyperhidrosis, kev sib deev tsis ua haujlwm (tso erectile muaj nuj nqi, txo libido), thiab qhov chaw txhaj tshuaj hauv zos (mob, ecchymosis). Musculoskeletal phiv tej zaum yuav muaj xws li arthralgia thiab txo cov pob txha ntxhia pob txha; Cov teebmeem ntawm neurological qee zaus muaj xws li kev hloov mus ob peb vas thiab kev hnov mob neuropathy; thiab cov teebmeem ntawm cov hlab plawv tuaj yeem cuam tshuam nrog kev hloov ntshav siab.
Rautxo cov pob txha ntxhia pob txha: Kev kho ua ke nrog bisphosphonates tuaj yeem txo cov pob txha. Cov neeg mob uas muaj kev pheej hmoo siab (xws li, cov neeg uas muaj keeb kwm ntawm tsev neeg mob pob txha, ntev- haus luam yeeb lossis haus cawv) yuav tsum tau saib xyuas cov pob txha pob txha tsis tu ncua thiab kev cuam tshuam.
Rauqhov chaw txhaj tshuaj ecchymosis: Kev nyem tuaj yeem ua tiav los ntawm kev tshaj tawm - kev txhaj tshuaj compression, nrog rau kev ua kom tsis muaj zog.
Raukev sib deev tsis ua haujlwm: Kev kho cov tsos mob thiab kev tawm tswv yim txog kev puas siab puas ntsws tuaj yeem pab txo tus neeg mob lub nra hnyav.
Kev Ceeb Toom Thaum Ntxov thiab Kev Tiv Thaiv Mob hnyav
Tumor flare phenomenon
Kev nce qib ntawm testosterone tom qab thawj koob tshuaj yuav ua rau muaj qhov tshwm sim ntawm qog nqaij hlav ib ntus (xws li, mob pob txha hnyav, ureteral obstruction) hauv qee cov neeg mob, feem ntau tshwm sim hauv thawj 4 lub lis piam ntawm kev kho mob. Co-kev tswj hwm ntawm cyproterone acetate (300mg txhua hnub) los ntawm 3 hnub ua ntej mus rau 3 lub lis piam tom qab thawj koob tshuaj tuaj yeem tiv thaiv qhov tsis zoo ntawm testosterone nce. Yuav tsum tau saib xyuas ze, thiab kev kho tus qauv yuav tsum tau pib sai thaum muaj kev cuam tshuam los yog txha caj qaum.
Tsis tshua muaj tshwm sim tsis zoo
Tom qab- kev soj ntsuam kev lag luam tau txheeb xyuas qhov tsis tshua muaj tshwm sim ntawm pituitary apoplexy (tam sim no nrog mob taub hau, ntuav, pom kev txawv txav), feem ntau tshwm sim hauv 2 lub lis piam ntawm thawj koob tshuaj, uas yuav tsum tau kho mob ceev ceev tam sim. Tsis tshua muaj tshwm sim ntawm hypersensitivity tshwm sim (urticaria, anaphylaxis) thiab cov qog pituitary kuj tau tshaj tawm; Kev tshem tawm tshuaj thiab kev tswj cov tsos mob yuav tsum tau ua thaum tshwm sim.
Lwm yam kev pheej hmoo tswj
Rau cov neeg mob uas muaj kab mob plawv, cov txiaj ntsig thiab kev pheej hmoo ntawm kev kho mob yuav tsum raug soj ntsuam; Lub plawv dhia thiab ntshav siab yuav tsum tau saib xyuas thaum noj tshuaj, nrog ceev faj txog myocardial infarction thiab mob stroke. Cov neeg mob ntshav qab zib yuav tsum tau saib xyuas cov ntshav qabzib tsis tu ncua thiab glycated hemoglobin kom tsis txhob muaj glycemic tswj tsis zoo. Cov neeg mob uas muaj keeb kwm ntawm QT ncua ncua sij hawm yuav tsum tau ceev faj thaum sib txuas nrog QT- cov tshuaj ntev, thiab kev soj ntsuam electrocardiogram yog tsim nyog yog tias qhia.
Clinical Value thiab Application Prospects
Goserelin Txhajtau hloov kho thaj chaw ntawm kev kho mob endocrine rau kev mob qog noj ntshav prostate nrog nws qhov zoo ntawm qhov ntev - ua cov kev tso tawm tsis tu ncua, kev ua tau zoo, muaj kev nyab xeeb siab thiab siv tau yooj yim, tawm los ua cov tshuaj tseem ceeb thoob plaws hauv cov kab mob metastatic, hauv zos siab heev thiab siab - muaj feem cuam tshuam hauv zos prostate cancer. Nws tsis tsuas yog hloov qee cov txheej txheem phais castration los txo cov kev raug mob tab sis kuj tseem txhim kho cov txiaj ntsig kev kho mob, kev ua neej zoo thiab kev muaj sia nyob hauv cov neeg mob los ntawm kev sib xyaw ua ke (xws li, nrog abiraterone lossis radiotherapy).
Nrog rau kev txhim kho ntawm cov tshuaj precision, kev sib xyaw ua ke ntawm Goserelin tau ua kom zoo dua qub, thiab nws cov xwm txheej hauv kev kho neoadjuvant thiab tom qab- kev kho mob kuj nthuav dav. Nyob rau hauv lub neej yav tom ntej, kuaj noob-raws li tus kheej cov tswv yim noj tshuaj yuav ntxiv txhim kho qhov tseeb ntawm nws txoj kev kho mob thiab ua rau muaj txiaj ntsig ntau ntxiv rau cov neeg mob qog noj ntshav prostate.
Raws li Class B lub teb chaws cov tshuaj pov hwm kho mob, Goserelin tau nkag mus tau ntau dua, muab kev xaiv kev kho mob zoo rau cov neeg mob qog noj ntshav ntau.
Core Physicochemical Properties
Goserelin yog dawb los yog tawm -cov hmoov dawb, tsis muaj ntxhiab, me ntsis soluble hauv dej, me ntsis soluble hauv methanol, thiab yuav luag insoluble hauv ethanol. Qhov profile solubility no dictates nws formulation raws li ib tug sustained - tso implant es tsis yog ib tug aqueous txhaj. Nws muaj pKa tus nqi ntawm kwv yees li 7.8 thiab tsis muaj zog hauv lub cev pH (7.35-7.45), ua kom muaj kev ruaj khov nyob rau hauv cov kua dej subcutaneous interstitial rau qeeb tso tawm thiab nqus. Lub compound tsis muaj qhov tseem ceeb kho qhov muag thiab qhov chaw melting ntawm 195-200 degree, decomposing raws li cua sov; Yog li, kev tswj qhov kub thiab txias yog qhov yuav tsum tau ua thaum lub sijhawm tsim khoom thiab khaws cia kom tsis txhob muaj cov khoom xyaw nquag.
Stability thiab Dosage Form Compatibility
Goserelin yog rhiab heev rau lub teeb thiab av noo, nquag degradation thaum raug lub teeb muaj zog los yog high humidity; yog li ntawd, qhov txhaj tshuaj yog ntim rau hauv lub teeb -resistant thiab hermetically kaw ntim. Nws ruaj khov - tso tawm cog siv poly(lactic-co-glycolic acid) (PLGA) ua tus nqa khoom, thiab cov tshuaj sib raug zoo ntawm Goserelin thiab cov khoom nqa khoom ua rau muaj kev tso tshuaj txuas ntxiv thiab khov kho hauv lub cev rau 12 lub lis piam. Hauv vitro kev ntsuas kev ruaj ntseg tau pom tias cov tshuaj Goserelin nyoos muaj lub neej txee ntawm 2 xyoos hauv qhov chaw qhuav hauv qab 25 degree; Tom qab tau tsim los rau hauv kev cog qoob loo, nws muaj lub neej txee ntawm 18 lub hlis nyob rau hauv hermetic cia tej yam kev mob, ua tau raws li cov kev cai zoo rau kev siv tshuaj txhaj tshuaj.
FAQ
1.Yog goserelin yog tshuaj kho mob?
Koj tus kws kho mob, tus nais maum lossis tus kws muag tshuaj yuav tuaj yeem piav qhia seb koj txoj kev kho mob ua haujlwm li cas kom ntxaws ntxiv. Nws yog ib qho tseem ceeb kom nkag siab tias exemestane thiab goserelin yogtsis yog tshuaj chemotherapy tshuajthiab muaj kev sib txawv ntawm kev ua haujlwm. Lawv ua haujlwm los ntawm kev txo cov tshuaj hormones uas nres cov qog nqaij hlav cancer loj hlob thiab kis mus.
2.Dab tsi yog ib qho kev mob tshwm sim ntawm goserelin?
Zoladex (goserelin) - Kev Siv, Sab Nraud, thiab Ntau. Txheej txheem cej luam: Zoladex feem ntau yog siv los kho mob qog noj ntshav. Cov kev mob tshwm sim muaj xws li kub flashes, txo kev sib deev tsav, thiab teeb meem nrog erections. Zoladex yog ib qho cog uas muab tso rau hauv qab ntawm daim tawv nqaij los ntawm koj tus kws kho mob.
3.Koj txhaj tshuaj goserelin qhov twg?
Keeb kwm: Tus qauv kev saib xyuas rau cov tshuaj hormone receptor-zoo mob qog noj ntshav mis feem ntau cuam tshuam nrog kev siv sijhawm ntev ntawm kev ua haujlwm ntawm zes qe menyuam (OFS) kev kho mob, suav nrog goserelin. Cov chaw tsim khoom pom zoo qhia cov kws saib mob kom txhaj tshuaj goserelinsubcutaneously nyob rau hauv lub anterior plab phab ntsa, hauv qab ntawm txoj hlab ntaws.
4.Qhov kev kho goserelin ntev npaum li cas?
Lub sijhawm pom zoo ntawm kev kho yog6 hli. Siv: Rau kev tswj cov kab mob endometriosis, nrog rau qhov mob nyem thiab txo cov kab mob endometriotic.
Cim npe nrov: Tuam Tshoj goserelin txhaj tshuaj manufacturers, lwm tus neeg
