Lanreotide 120 mg txhajyog ib tug ntev-acting sustained-tso txhaj tshuaj raws li lub tswv yim nanotechnology, cais raws li ib tug somatostatin analog. Nws yog xa los ntawm lub syringe prefilled thiab yog tsim los rau lub sij hawm ntev kev tswj ntawm endocrine thiab neoplastic kab mob. Nws qhov kev txhaj tshuaj tshwj xeeb sawv cev rau qhov tseem ceeb ntawm qhov zoo dua li lwm hom tshuaj.Qhov kev txhaj tshuaj no siv cov dej-soluble formulation uas tsim cov kua-crystalline gel tov los ntawm saj zawg zog nanotubes, ua kom tiav ib tug dual nyhuv ntawm cov tshuaj sai sai tso tawm (Tmax=7.0 teev) thiab ntev-ntev sustained tso tawm (t1/{5} cov teebmeem) nrog rau ob peb hnub (t1/{5}). Raws li tsuas yog somatostatin analog (SSA) tau pom zoo thoob ntiaj teb rau kev tswj hwm tus kheej los ntawm kev txhaj tshuaj subcutaneous, nws cov khoom siv ua ntej yuav tsum tsis muaj kev kho dua tshiab; Kev npaj thiab txhaj tshuaj tsuas yog siv sijhawm 66 vib nas this, txo cov sijhawm tswj hwm zoo heev.
Peb Cov Khoom Muag Khoom
Lanreotide COA
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| Certificate of Analysis | ||
| Compound npe | Lanreotide | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 108736-35-2 | |
| Ntau | 55g | |
| 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% | 0.93% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.32% |
| 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 qho impurity | <0.8% | 0.21% |
| 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 | 416ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Tshuaj Formula | C54H69N11O10S2 | |
| Exact Mass | 1095.47 | |
| Molecular Luj | 1096.33 | |
| m/z | 1095.47(100.0%), 1096.47(58.4%), 1097.47(16.7%), 1097.46(9.0%), 1098.47(5.3%), 1096.46(4.1%), 1098.48(3.1%), 1097.47(2.4%), 1097.47(2.1%), 1096.47(1.6%), 1099.47(1.5%), 1098.47(1.2%) | |
| Elemental Analysis | C,59.16; H,6.34; N,14.05; O,14.59; S,5.85 | |
Daim ntawv thov hauv Acromegaly
Acromegaly yog ib hom kab mob endocrine thiab metabolic uas tshwm sim los ntawm kev tso tawm ntau dhau ntawm kev loj hlob hormone (GH) los ntawm lub caj pas pituitary, feem ntau yog los ntawm GH-secreting pituitary adenoma. Ntev dhau GH ua rau muaj kev loj hlob ntawm cov nqaij mos thiab cov pob txha, ua rau lub ntsej muag hloov pauv, loj dua tes thiab taw, thiab visceral hypertrophy. Nws kuj ua rau muaj kev pheej hmoo siab ntawm ntshav siab, ntshav qab zib mellitus, kab mob plawv, thiab lwm yam teeb meem, ua rau muaj kev cuam tshuam loj ntawm lub neej thiab kev ciaj sia.
Lub hom phiaj tseem ceeb ntawm kev kho mob yog los tswj GH thiab insulin-zoo li kev loj hlob yam tseem ceeb-1 (IGF-1), txo cov tsos mob, txo qis pituitary adenoma ntim, thiab txo qis tus nqi. Raws li SSA ua haujlwm ntev,Lanreotide 120 mg txhajmimics cov teebmeem physiological ntawm somatostatin, potently inhibits pituitary GH secretion, thiab exerts antiproliferative teebmeem ntawm pituitary adenoma hlwb. Nws yog lub hauv paus kev kho mob rau acromegaly, tshwj xeeb tshaj yog rau cov neeg mob uas muaj qhov tshwm sim tsis zoo ntawm kev phais, kab mob tsis tuaj yeem, lossis kev tsis haum rau kev phais lossis kev kho hluav taws xob.
Clinical Efficiency
Ntau cov kev tshawb fawb soj ntsuam tau lees paub tias Nws tswj cov qib tshuaj hormones zoo, txo cov tsos mob, thiab muaj txiaj ntsig zoo rau kev nyab xeeb mus ntev hauv acromegaly.
Hauv kev tshawb fawb 12-hli, cov neeg mob acromegaly kho nrog koob tshuaj 120 mg tau ua tiav GH tswj tus nqi (GH Tsawg dua lossis sib npaug li 2.5 ng / mL) ntawm 78% thiab IGF-1 normalization tus nqi ntawm 82%, ob qho tib si ntau dua li ntawm pawg qis. Ntawm cov neeg mob uas tsis muaj kev phais mob, kwv yees li 65% tau ua tiav qib GH thiab IGF-1 li qub tom qab 6 lub hlis ntawm kev kho mob ntawm qhov koob tshuaj no, nrog rau kev txhim kho acral o thiab hloov ntawm lub ntsej muag, thiab txo qis hauv kev mob taub hau, qaug zog, thiab lwm yam tsis xis nyob.
Cov ntaub ntawv mus sij hawm ntev qhia tau hais tias ib zaug-txhua-4-lub lim tiam kev tswj hwm tswj cov tshuaj hormones ruaj khov mus ntev. Pituitary adenoma ntim tau txo los ntawm 15% -30% hauv qee cov neeg mob, ua kom cov kab mob qeeb qeeb. Kev siv tshuaj yooj yim ua rau cov neeg mob ua raws li kev noj qab haus huv: piv nrog cov kev txhaj tshuaj luv luv, cov tshuaj tsis tau raug txo los ntawm ntau dua 60%, uas ua rau muaj kev tiv thaiv kab mob ntev ntev.
Tsis tas li ntawd, piv nrog cov tshuaj zoo sib xws octreotide microspheres, cov qauv no ua rau lub sijhawm npaj thiab txhaj tshuaj tsawg dua thiab muaj kev pheej hmoo tsawg dua ntawm koob clogging, ntxiv kev txhim kho kev kho mob yooj yim.
Kev nyab xeeb thiab ceev faj
Lanreotide 120 mg txhajmuaj qhov zoo tshaj plaws kev nyab xeeb profile hauv acromegaly. Feem ntau cov kev phiv tshwm sim yog me me mus rau nruab nrab, tshwm sim thaum ntxov ntawm kev kho mob, thiab txo qis nrog kev kho txuas ntxiv.
Cov kev phiv tshwm sim feem ntau yog qhov tshwm sim ntawm qhov chaw txhaj tshuaj (mob, liab, o, o, induration), tab sis qhov tshwm sim yog qis dua li cov tshuaj zoo sib xws, ntaus nqi los ntawm nanogel formulation thiab prefilled syringe tsim. Feem ntau cov tshuaj daws teeb meem tshwm sim tsis pub dhau 1-2 lub lis piam yam tsis muaj kev cuam tshuam.
Lwm yam kev phiv tshwm sim muaj xws li mob plab hnyuv (xws li plab, plab plab, raws plab) thiab endocrine cuam tshuam (cov ntshav qabzib hloov pauv, me ntsis hypothyroidism). Glucose fluctuations feem ntau yog me me thiab ntau zaus hauv cov neeg mob ntshav qab zib. Kev tshuaj xyuas ntshav qabzib raug pom zoo thaum pib kho thiab thaum hloov kho koob tshuaj, nrog rau cov tshuaj tiv thaiv kab mob ntshav qab zib titrated raws li. Rau cov neeg mob ntshav qab zib mellitus ntawm insulin, thawj koob tshuaj insulin yuav tsum raug txo los ntawm 25% thiab tom qab ntawd maj mam hloov.
Cov neeg mob tau txais cov tshuaj sib xyaw ua ke uas tuaj yeem ua rau bradycardia (piv txwv li, -blockers) yuav tsum tau saib xyuas kom zoo rau lub plawv dhia, nrog rau kev kho koob tshuaj raws li xav tau.
Tseem ceeb: Kev siv mus ntev yuav ua rau muaj kev pheej hmoo ntawm cholelithiasis. Kev saib xyuas lub gallbladder tsis tu ncua yog pom zoo. Yog hais tias muaj teeb meem ntawm lub gallstone, txiav tawm kev kho mob thiab muab kev kho mob.
Daim ntawv thov hauv Neuroendocrine hlav
Neuroendocrine qog (NETs) yog ib pawg neeg heterogeneous ntawm neoplasms los ntawm cov hlwb neuroendocrine, uas tuaj yeem tshwm sim thoob plaws hauv lub cev. Gastroenteropancreatic neuroendocrine qog (GEP-NETs) suav txog kwv yees li 70%. Cov qog no muaj qhov nyuaj, tsis muaj kev kho mob tshwj xeeb thiab tsis yooj yim rau kev kuaj mob, nrog lub sijhawm los kuaj mob txog li 5 xyoos. Kwv yees li 40% -50% ntawm cov neeg mob uas muaj cov kab mob metastasis nyob deb ntawm kev kuaj pom thawj zaug. 5-xyoos ciaj sia taus yog kwv yees li 54%, thiab tsuas yog 7.8% rau cov qog nqaij hlav qib siab, qhia tau tias muaj qhov tsis zoo.
Kev kho mob ntawm NETs yuav tsum muaj cov tswv yim sib txawv raws li qhov chaw ntawm qog nqaij hlav, theem, qib, thiab tus neeg mob tus mob. Cov hom phiaj tseem ceeb yog los tswj cov qog nqaij hlav, txo cov tsos mob tshwm sim los ntawm kev tso tawm cov tshuaj hormone ntau dhau, thiab ncua kev muaj sia nyob tsis muaj sia nyob (PFS) thiab kev ciaj sia tag nrho (OS).
Raws li kev ua haujlwm ntev SSA, nws muaj zog tiv thaiv kev loj hlob ntawm cov qog hlwb neuroendocrine thiab inhibits kev tso tawm ntawm ntau cov qog nqaij hlav los ntawm cov tshuaj hormones (xws li serotonin, gastrin). Nws yog thawj kab kev kho mob rau qib qis mus rau theem nrab GEP-NETs thiab carcinoid syndrome.
Clinical Efficiency
Nws pom tau tias muaj txiaj ntsig zoo hauv kev ua kom ntev PFS thiab txo cov tsos mob hauv cov qog neuroendocrine, nrog rau qhov zoo ntawm qee cov neeg ua haujlwm zoo sib xws.
Hauv kev sim tshuaj ntsuam xyuas randomized (RCT), cov neeg mob uas muaj qhov sib txawv ntawm GEP-NETs tau kho nrog 120 mg txhua 4 lub lis piam muaj qhov nruab nrab PFS ntawm 30.1 lub hlis, piv nrog 28.0 lub hlis rau octreotide microspheres (HR=0.9, 95% CI: 0.71lyion), ncua kev ua haujlwm – 1.2. Lwm qhov RCT qhia tau hais tias hauv cov neeg mob uas muaj qhov sib txawv zoo los yog muaj qhov sib txawv ntawm G1 / G2 GEP-NETs, 120 mg koob tau ua tiav PFS nruab nrab ntawm 32.8 lub hlis, ntau dua 18 lub hlis hauv pawg placebo. Pancreatic NET (pNET) pab pawg muaj qhov nruab nrab PFS ntawm 29.7 lub hlis.
Rau kev tswj cov tsos mob hauv carcinoid syndrome:
Mob raws plab: ua tiav lossis ib nrab teb tus nqi ntawm 76%
Flushing: teb tus nqi ntawm 73%
Kev siv cov tshuaj luv luv somatostatin analogues txo qis dua 60%.
Raws li kev kho mob tom qab phais, 120 mg ib zaug txhua 4 lub lis piam rau 1 xyoos txo qhov kev pheej hmoo rov qab ntawm GEP-NETs los ntawm 35%, nrog rau 5-xyoo OS ntawm 87.5%, ntau dua 65.6% hauv pawg octreotide.
Tsis tas li ntawd, qhov yooj yim ntawm kev txhaj tshuaj no txhawb kev kho mob ntev rau cov neeg mob qog nqaij hlav neuroendocrine. Raws li tsuas yog SSA pom zoo thoob ntiaj teb rau kev txhaj tshuaj subcutaneous tus kheej, 100% ntawm cov neeg mob nyiam kev tswj hwm tus kheej lossis tus neeg saib xyuas, thiab 97.8% ntawm cov kws saib xyuas neeg mob pom zoo cov khoom no. Nws cov koob-npaj, kev txhaj tshuaj sai sai txo qhov hnyav ntawm kev kho mob thiab txhim kho kev ua raws, ua kom muaj kev kho mob mus ntev.
Pharmacoeconomic tsom xam qhia tau hais tias, piv nrog ntev-acting octreotide, kev kho mob ntawm cov qog neuroendocrine nrog tus neeg sawv cev no ua rau muaj kev txuag nyiaj ntau xyoo, uas tau tsav los ntawm nws cov nqi zoo, lub sij hawm tswj xyuas luv dua, thiab qis dua kev pheej hmoo ntawm rab koob clogging.
Kev nyab xeeb thiab ceev faj
Kev ruaj ntseg profile ntawmLanreotide 120 mg txhajHauv cov qog nqaij hlav neuroendocrine feem ntau yog ua raws li hauv acromegaly. Feem ntau qhov tsis zoo tshwm sim yog me me mus rau nruab nrab thiab kev txwv tus kheej.
Feem ntau cov kev phiv tshwm sim tseem nyob rau hauv qhov chaw txhaj tshuaj (mob, liab, o, induration), nrog rau qhov tshwm sim ntawm 15% -20%, qis dua octreotide microspheres. Cov neeg mob feem ntau zam cov no yam tsis muaj kev cuam tshuam kev kho mob.
Cov kab mob hauv plab (xws li, ntuav, plab, raws plab) kuj tshwm sim, feem ntau tshwm sim hauv thawj 1-2 lub hlis thiab txhim kho nrog kev hloov kho. Cov mob hnyav tuaj yeem tswj tau cov tsos mob (antiemetics, antidiarrheals) yam tsis tau hloov koob tshuaj.
Vim tias cov neeg mob qog nqaij hlav neuroendocrine feem ntau muaj kev zom zaub mov tsis zoo, cov tshuaj noj tshuaj hauv plab hnyuv tuaj yeem txo cov hnyuv nqus ntawm cov tshuaj sib xyaw ua ke, suav nrog ciclosporin. Kev tswj hwm nrog ciclosporin tuaj yeem txo nws cov txheeb ze bioavailability; Yog li ntawd, kev soj ntsuam ntshav concentration thiab kev hloov koob tshuaj yog pom zoo.
Cov ntshav qabzib hloov pauv yuav tsum tau ua tib zoo saib xyuas, tshwj xeeb tshaj yog cov neeg mob ntshav qab zib. Intensified glucose monitoring thiab antidiabetic dose adjustment yog tsim nyog thaum kho.
Xyoo 1973, Dr. Guillemin thiab cov npoj yaig cais cov ntuj somatostatin los ntawm ovine hypothalamus. Qhov no endogenous polypeptide inhibits qhov tso tawm ntawm ntau cov tshuaj hormones, tshwj xeeb tshaj yog cov tshuaj hormones loj hlob, qhib txoj kev kho tshiab rau cov kab mob hormonal-hypersecretory xws li acromegaly. Guillemin tau txais txiaj ntsig Nobel nqi zog hauv Physiology lossis Tshuaj hauv xyoo 1977 rau txoj haujlwm no.
Txawm li cas los xij, ntuj somatostatin muaj cov kev txwv tseem ceeb: ib nrab-lub neej luv luv ntawm tsuas yog 2 feeb, ceev hauv vivo degradation, thiab yuav tsum tau txhaj tshuaj tas li, ua rau kev siv tshuaj kho mob tsis zoo. Kev tsim kho kom ruaj khov, ntev-ua yeeb yam somatostatin analogs tau dhau los ua kev tshawb fawb tseem ceeb.
Laboratory Breakthrough thiab Initial Optimization
Thaum ntxov xyoo 1980, tom qab kev sib txuas ua tiav ntawm octreotide- thawj zaug pom zoo somatostatin analog- pab pawg tshawb fawb ntawm Beaufour IPSEN (Fabkis) tau tsim ib qho kev pab cuam los tshawb pom cov tshiab somatostatin analogs.
Raws li 14-amino-acid qauv ntawm ntuj somatostatin, cov kws tshawb fawb tau khaws nws cov tshuaj pharmacologically cores, hloov labile amino acids, qhia txog stabilizing structural motifs, thiab optimized peptide conformation. Lanreotide (code BIM 23014) tau ua tiav tiav hauv chav kuaj.
Piv nrog rau ntuj somatostatin, nws pom tias:
Zoo heev ncua ib nrab-lub neej
High selective affinity rau somatostatin receptor subtype 2
Ntxiv khi rau subtypes 3 thiab 5
Ntau zog inhibition ntawm kev loj hlob hormone secretion
Nyob rau hauv 1998, nws yog thawj zaug launched nyob rau hauv Teb chaws Europe raws li ib tug microsphere sustained-tso formulation (Somatuline LA 30 mg), muab tshuaj subcutaneously txhua 7-14 hnub, feem ntau yog rau acromegaly. Qhov no ib nrab hais txog qhov tsis yooj yim ntawm ntuj somatostatin.
Hauv xyoo 2001, nws qhov kev ua yeeb yaj kiab ntev ntev tau pom zoo hauv Tebchaws Europe, txuas ntxiv kho cov sijhawm noj. Hauv xyoo 2007, US FDA tau pom zoo rau kev txhaj tshuaj ntev-tso tawm rau acromegaly, ua kom muaj qhov sib txawv ntawm kev kho mob hauv Asmeskas kev lag luam.
Tom qab ntawd, cov qauv tsim tau zoo tsis tu ncua siv cov tshuaj nanoscale xa cov thev naus laus zis los tsim cov khoom lag luam ntev uas yuav tsum tau txhaj tshuaj ib hlis xwb. Kev taw qhia ntawm cov koob txhaj tshuaj prefilled zoo heev txhim kho yooj yim ntawm kev tswj hwm.
Expansion of Indications thiab Global Adoption
Txij li thaum xyoo 2000s, kev tshawb fawb soj ntsuam tau nthuav dav cov lus qhia rau nws.
2003: Pom zoo hauv Tebchaws Europe rau kev tswj cov tsos mob ntawm carcinoid syndrome.
2015: Raws li CLARINET mus sib hais, FDA tau pom zoo nws rau GEP-NETs uas tsis tuaj yeem kho, ua rau PFS txuas ntxiv.
Hnub no,Lanreotide 120 mg txhajtau pom zoo nyob rau hauv ntau lub teb chaws thiab cheeb tsam rau cov kev qhia xws li acromegaly, gastroenteropancreatic neuroendocrine qog, thiab carcinoid syndrome. Nws lub sijhawm ntev, yooj yim, thiab kev nyab xeeb tau ua rau nws yog tus neeg sawv cev tseem ceeb ntawm somatostatin analogs, txuas ntxiv muab kev kho kom zoo dua qub rau cov neeg mob uas muaj kab mob.
FAQ
Nws siv rau dab tsi?
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Nws yog sivrau lub sij hawm ntev - kev kho mob ntawm acromegaly (kev loj hlob hormone tsis meej) nyob rau hauv cov neeg mob uas tsis tuaj yeem kho nrog kev phais lossis hluav taws xob. Cov tshuaj no ua haujlwm los ntawm kev txo qis cov tshuaj hormones uas lub cev tsim tawm.
Koj tuaj yeem nyob ntev npaum li cas?
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Yog tias koj muaj lanreotide los tswj kev loj hlob ntawm koj NET, koj txuas ntxiv qhov no rautsuav nws ua haujlwm, thiab cov kev mob tshwm sim tsis zoo heev.
Kev txhaj tshuaj lanreotide zoo li cas?
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Lanreotide feem ntau yog muab rau hauv pob tw los ntawm koj tus kws kho mob lossis kws kho mob. Yog tias koj tau txhaj tshuaj koj tus kheej,Kev txhaj tshuaj yuav tsum tau muab rau sab sauv, sab nraud ntawm koj tus ncej puab. Siv ib qhov chaw sib txawv txhua zaus txhaj tshuaj.
Dab tsi yog cov kev mob tshwm sim ntawm nws?
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Kev ua xua - cov tawv nqaij ua pob khaus, khaus, khaus khaus, o ntawm lub ntsej muag, daim di ncauj, tus nplaig, lossis caj pas. Teeb meem gallbladder- mob plab, xeev siab, ntuav, kub taub hau. Cov ntshav qab zib siab (hyperglycemia)- nqhis dej ntau ntxiv lossis tso zis ntau ntxiv, tsis muaj zog lossis qaug zog, pom qhov muag tsis pom.
Nws puas tuaj yeem ua rau poob phaus?
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Cov lus xaus: Hauv kev tshawb fawb yav tom ntej, peb tau pom tias cov koob tshuaj lanreotide qis (90 mg txhua 4 lub lis piam) txo cov siab ntim thiab cov tsos mob hauv cov neeg mob PCLD. Txawm li cas los xij, cov neeg mob tseem poob phaus thiab cov leeg nqaij. Cov teebmeem ntawm somatostatin analogues ntawm sarcopenia xav tau kev tshawb nrhiav.
Cim npe nrov: Lanreotide 120 mg txhaj tshuaj, Tuam Tshoj Lanreotide 120 mg txhaj tshuaj manufacturers, lwm tus neeg
