Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm exemestane hmoov hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo siab exemestane hmoov rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Exemestane, tshuaj hu ua 6-methylenandrosta-1,4-diene-3,17-dione (CAS 107868-30-4), yog steroidal aromatase inhibitor (AI) nrog irreversible binding zog. Ua lag luam raws li cov npe lag luam nyiamAromasin, nws feem ntau yog siv los kho cov tshuaj hormone receptor-mob qog noj ntshav zoo hauv cov poj niam tom qab yug menyuam. Tshaj li oncology, exemestan lub cim tshwj xeeb ntawm kev ua haujlwm tau ua rau muaj kev txaus siab rau nws cov kev siv peev xwm hauv cov pob txha noj qab haus huv, lipid metabolism, thiab txawm tias yog cov cuab yeej tshawb fawb hauv endocrinology.
Mob qog noj ntshav mis yog qhov mob hnyav tshaj plaws ntawm cov poj niam thoob ntiaj teb, nrog HR + subtypes suav txog kwv yees li 70% ntawm cov neeg mob. Nyob rau hauv cov poj niam postmenopausal, estrogen ntau lawm hloov ntawm zes qe menyuam mus rau peripheral cov ntaub so ntswg, qhov twg androgens hloov mus rau estrogens ntawm aromatase enzyme. Aromatase inhibitors (AIs) zoo li exemestan tau hloov kho kev kho mob los ntawm kev tsom mus rau txoj hauv kev no, muab cov txiaj ntsig zoo thiab kev nyab xeeb piv rau cov kev kho qub xws li tamoxifen.
Cov ntaub ntawv khoom
Exemestane+. COA
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| Certificate of Analysis | ||
| Compound npe | Exemestane | |
| CAS Nr. | 107868-30-4 | |
| Ntau | 45kg ua | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 20250718012 | |
| MFG | Lub Rau Hli 22, 2025 | |
| EXP | Peb Hlis 22, 2028 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb rau tawm -dawb | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.13% |
| 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) | >98% | 99.20% |
| Ib leeg impurity | <0.8% | 0.18% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 30 |
| 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 | 300 ppm |
| Cia | -80 degree, 2 xyoos; -20 degree, 1 xyoo (Kev kaw cia, deb ntawm noo noo) | |
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| Shaanxi Chuzhan yog lub tuam txhab thev naus laus zis tshwj xeeb hauv kev tshawb fawb thiab kev tsim kho, tsim cov tshuaj thiab cov khoom siv kho kom haum, muab OEM / ODM tag nrho - cov kev daws teeb meem. Peb muab cov kev hloov pauv hloov pauv tag nrho - txheej txheem cov kev pabcuam customized, los ntawm cov qauv kev tshawb fawb thiab kev tsim kho mus rau kev xaiv cov khoom siv, txhua tus tuaj yeem hloov kho raws li cov neeg siv khoom xav tau. Txhawb nqa tag nrho- kev sib koom ua ke ntawm kev sib koom ua ke los ntawm me me- kev sim ntsuas me me, nruab nrab- ntsuas kev sim mus rau loj- nplai ntau lawm, nruab nrog pab pawg kws tshaj lij los muab cov txheej txheem kev ua kom zoo tshaj plaws, thiab tuaj yeem kho cov ntawv ntim raws li cov khoom xav tau ntawm cov neeg siv khoom. | ||
Chemical Properties thiab Formulation
Exemestane yog 17-oxo steroid nrog cov qauv molecular ntawm C₂₀H₂₄O₂ thiab molecular hnyav ntawm 296.403 g / mol. Tus qauv tsim, nws muaj cov methylene pawg ntawm 6-txoj hauj lwm ntawm androstane pob txha, uas txawv nws los ntawm lwm cov tshuaj steroidal. Lub compound yog dawb mus rau daj crystalline hmoov nrog ib tug melting point ntawm 155.13℃mus rau 191 degree, nyob ntawm seb qhov twg thiab purity. Nws yog xyaum insoluble nyob rau hauv dej tab sis soluble nyob rau hauv cov organic solvents xws li methanol, N, N-dimethylformamide, thiab chloroform, uas pab txhawb nws formulation rau hauv lub qhov ncauj ntsiav tshuaj los yog tsiav tshuaj.
Pharmaceutical -qib exemestan hmoov feem ntau yog khaws cia nyob rau hauv kev tswj xyuas kom muaj kev ruaj ntseg. Piv txwv li, nws raug nquahu kom khaws cov hmoov ntawm -20℃rau kev khaws cia ntev (txog 3 xyoos) lossis ntawm 4℃rau lub sijhawm luv (txog 2 xyoos). Thaum yaj hauv cov kuab tshuaj, exemestan nthuav tawm lub txee lub neej ntawm 6 lub hlis ntawm -80℃lossis 1 lub hlis ntawm -20 degree, qhia txog qhov tseem ceeb ntawm kev khaws cia kom zoo los tiv thaiv degradation.
Pharmacological Mechanism of Action
Aromatase yog lub luag haujlwm rau kev hloov pauv androgens (piv txwv li, androstenedione) rau hauv estrogens (piv txwv li, estradiol). Hauv cov poj niam postmenopausal, cov ntaub so ntswg peripheral (xws li, adipose, cov leeg) dhau los ua qhov tseem ceeb ntawm estrogen synthesis, tsav cov tshuaj hormones- nyob ntawm kev loj hlob ntawm qog nqaij hlav cancer mis. Exemestan inhibits aromatase los ntawm:
Irreversible Binding: Pab pawg 6-methylene hauv exemestan tsim cov ntawv cog lus nrog cov heme moiety ntawm aromatase, mus tas li inactivating enzyme.
Kev xaiv siab: Exemestan nthuav tawm tsawg kawg nkaus - cov teebmeem, nrog IC₅₀ qhov tseem ceeb ntawm 30 nM (tib neeg placental aromatase) thiab 40 nM (rat zes qe menyuam aromatase).
Kev Ua Haujlwm Androgenic: Tsis zoo li tsis yog -steroidal AIs, exemestan khaws cov khoom tsis muaj zog androgenic, uas tuaj yeem ua rau nws muaj txiaj ntsig zoo rau pob txha pob txha pob txha ntom ntom (BMD) thiab lipid profile.
Pharmacokinetics
Absorption: Qhov ncauj bioavailability yog kwv yees li 42%, nrog rau qhov siab tshaj plaws plasma concentrations (Cₘₐₓ) mus txog hauv 2-3 teev.
Distribution: It is highly protein-bound (>90%) rau albumin thiab alpha-1-acid glycoprotein.
Metabolism: Feem ntau metabolized los ntawm cytochrome P450 (CYP) enzymes, tshwj xeeb tshaj yog CYP3A4, nrog me me los ntawm CYP1A2 thiab CYP2C8.
Kev tshem tawm: Lub davhlau ya nyob twg ib nrab- lub neej yog 24 teev, nrog rau kev tso tawm ntawm cov zis (40%) thiab quav (40%).
Kev siv tshuaj kho mob
Exemestan yog FDA- pom zoo rau:
Adjuvant Therapy: Tom qab 2-3 xyoos ntawm tamoxifen nyob rau hauv cov poj niam postmenopausal nrog thaum ntxov- mob qog noj ntshav mis (raws li ib feem ntawm kev kho mob ua ntu zus).
Kab mob Advanced: Thib ob - kab kev kho mob rau mob qog noj ntshav mis metastatic tom qab kev loj hlob ntawm cov tsis yog -steroidal AIs.
Cov kev sim tshuaj tseem ceeb:
MA-17 Kev sim: Exemestan txo qhov kev pheej hmoo ntawm kev rov tshwm sim los ntawm 32% piv rau cov placebo thaum siv raws li kev kho mob txuas ntxiv tom qab tamoxifen.
Kev sim IES: Kev kho mob sib txuas nrog exemestan tom qab tamoxifen txhim kho kab mob-dawb ciaj sia taus (DFS) los ntawm 19% piv rau tamoxifen txuas ntxiv rau 5 xyoos.
SoFEA Kev sim: Hauv kev mob qog noj ntshav ntawm lub mis, exemestan tau qhia tias tsis yog -kev ua tsis zoo rau megestrol acetate, nrog rau kev nyab xeeb zoo dua.
Pob txha Health
Estrogen deficiency ua rau cov pob txha poob, ua rau muaj kev pheej hmoo ntawm pob txha hauv cov poj niam postmenopausal. Exemestan's androgenic zog tuaj yeem txo cov nyhuv no:
Hauv ovariectomized nas, exemestan (20-100 mg / kg / lub lis piam) nce lumbar BMD los ntawm 15% thiab txo cov ntshav pyridinoline (cov pob txha resorption marker) los ntawm 30%.
Ib txoj kev tshawb fawb me me qhia txog BMD ruaj khov hauv cov neeg mob qog noj ntshav thaum ntxov tau kho nrog exemestan rau 2 xyoos, sib piv nrog BMD poob pom nrog tsis yog -steroidal AIs.
Lipid Metabolism
Estrogen depletion feem ntau ua rau cov lipid profile, ua rau muaj kev pheej hmoo ntawm cov hlab plawv. Exemestan's androgenic kev ua haujlwm tuaj yeem cuam tshuam qhov no:
Hauv ovariectomized nas, exemestan txo tag nrho cov roj cholesterol los ntawm 25% thiab LDL-C los ntawm 30%.
Tib neeg cov ntaub ntawv raug txwv, tab sis ib theem II sim nyob rau hauv cov poj niam noj qab haus huv postmenopausal pom tsis muaj kev hloov pauv tseem ceeb hauv lipid tsis tau tom qab 12 lub lis piam ntawm exemestan (25 mg / hnub).
Lwm Yam Kev Siv Tau
Endometrial Cancer: Cov kev tshawb fawb hauv tsev kho mob qhia tias exemestan tuaj yeem cuam tshuam cov qog nqaij hlav endometrial cell proliferation ntawm estrogen receptor downregulation.
Polycystic Ovary Syndrome (PCOS): Exemestan lub peev xwm los txo cov androgen synthesis tuaj yeem muaj txiaj ntsig zoo rau cov poj niam nrog PCOS, txawm tias tsis muaj pov thawj ntawm kev kho mob.
Case Study
Tus neeg mob Profile
Ib tug poj niam muaj hnub nyoog 62-xyoo-laus postmenopausal nrog HR +/HER2- mob qog noj ntshav hauv lub mis metastatic tau nce ntxiv tom qab 4 xyoos ntawm kev siv tamoxifen. Nws tau hloov mus rau exemestan 25 mg / hnub tab sis tsim mob hnyav heev thiab qib 2 hypercholesterolemia ntawm 3 lub hlis.
Kev cuam tshuam
Txhawm rau txo qis AEs, pab pawg oncology tau koom tes nrog lub tsev muag tshuaj sib xyaw kom hloov kho exemestan ua cov gel transdermal (10% w / w hauv pluronic lecithin organogel). Cov gel tau siv txhua hnub rau sab hauv ncej puab, hla ua ntej - dhau ntawm cov metabolism thiab txo qis kev raug mob.
Cov txiaj ntsig
Kev ua tau zoo: Cov kab mob ruaj khov khaws cia rau 12 lub hlis (vs . 6 hli nrog qhov ncauj exemestan).
Kev nyab xeeb: Arthralgia daws tsis pub dhau 2 lub lis piam; Cov roj cholesterol normalized tom qab 4 lub lis piam.
Ua raws li: Tus neeg mob nyiam cov gel vim yooj yim ntawm kev siv thiab txo cov kev mob tshwm sim.
Cov ntaub ntawv no qhia txog lub peev xwm ntawm exemestan hmoov hauv cov tshuaj kho tus kheej, ua kom muaj cov qauv tsim nyog rau cov neeg mob uas tsis haum rau cov qauv kev kho qhov ncauj.
Kev nyab xeeb thiab kam rau ua
Common Adverse Effects:
Musculoskeletal: Arthralgia (30-50%), osteopenia (10-20%).
Vasomotor: Kub flashes (20-30%).
Mob plab: xeev siab (10-15%), qaug zog (10%).
Kev pheej hmoo loj:
Osteoporosis: Ntev- siv sijhawm ntev (Ntau dua lossis sib npaug li 5 xyoos) tuaj yeem ua rau muaj kev pheej hmoo ntawm pob txha, yuav tsum tau saib xyuas BMD.
Cov Txheej Txheem Kab Mob: Cov ntaub ntawv sib xyaw; Qee qhov kev tshawb fawb qhia tias muaj kev cuam tshuam nruab nrab, thaum lwm tus qhia txog kev pheej hmoo siab kub siab.
Cov tshuaj sib cuam tshuam: Nws yog metabolized los ntawm CYP3A4, yog li muaj zog inducers (xws li, rifampin) los yog inhibitors (xws li, ketoconazole) yuav hloov nws cov ntshav plasma.
Contraindications:
Cev xeeb tub: Teratogenic hauv cov tsiaj; contraindicated nyob rau hauv cov poj niam cev xeeb tub los yog pub niam mis.
Hypersensitivity: Cov neeg mob uas muaj keeb kwm ntawm exemestan-txog anaphylaxis yuav tsum tsis txhob siv.
Mob siab rau lub siab / raum tsis zoo: Kev kho koob tshuaj yuav tsum tau kho rau cov neeg mob uas muaj menyuam yaus -Pugh Class C cirrhosis lossis eGFR<30 mL/min.
Formulation Challenges thiab Innovations
Kev txwv ntawm Oral Tablets
Solubility: Exemestane yog dej tsis zoo -soluble (0.008 mg/mL ntawm 25 degree), txwv bioavailability.
Stability: Cov hmoov degrades nyob rau hauv lub teeb thiab av noo, yuav tsum nruj me ntsis cia tej yam kev mob (−20℃rau ntev - siv sij hawm).
Dosage Flexibility: Tsau 25 mg ntsiav tshuaj yuav tsis haum rau cov neeg mob uas yuav tsum tau hloov koob tshuaj (xws li cov neeg mob raum tsis zoo).
Compounding nrog Exemestane Powder
Exemestan hmoov yog invaluable nyob rau hauv compounding khw muag tshuaj rau kev npaj customized formulations:
Qhov ncauj Suspensions: Siv cosolvents (piv txwv li, DMSO, ethanol) los yog cyclodextrins los txhim kho solubility.
Transdermal Gels: Ib 10% w/w exemestan gel nyob rau hauv pluronic lecithin organogel (PLO) bypasses ua ntej - dhau metabolism, txo cov kab mob toxicity.
Subcutaneous Implants: Sustained - tso cov implants rau cov neeg mob nqos tsis tau tshuaj.
Case Study: Ib tug poj niam muaj hnub nyoog 62 xyoo uas muaj mob qog noj ntshav mis metastatic tau tsim mob hnyav heev ntawm qhov ncauj exemestan. Lub tsev muag tshuaj sib xyaw ua ke tau hloov kho nws ua cov gel transdermal, daws nws cov tsos mob thaum tswj hwm tus kab mob rau 12 lub hlis.
Kev Tshawb Fawb Kev Tshawb Fawb thiab Kev Qhia Txog Yav Tom Ntej
Combination Therapies
Nrog CDK4/6 Inhibitors: MONARCH-3 sim ntsuas exemestan ntxiv rau abemaciclib hauv HR +/HER2− metastatic mis mob cancer, qhia txog qhov nruab nrab PFS ntawm 28.2 lub hlis piv rau 14.8 lub hlis nrog exemestan ib leeg (HR=0.54, p < 0.001).
Nrog mTOR Inhibitors: Qhov kev sim BOLERO-2 tau pom tias exemestan ntxiv rau everolimus txhim kho PFS los ntawm 4 lub hlis piv rau exemestan monotherapy (7.4 vs. 3.2 hli, HR=0.43, p < 0.001).
Pob txha-Cov teebmeem tiv thaiv
Cov kev tshawb fawb ua ntej qhia tias exemestan qhov kev ua haujlwm tsis muaj zog androgenic tuaj yeem ua rau muaj kev sib txawv ntawm osteoblast, tiv thaiv estrogen deprivation- ua rau cov pob txha poob. Qhov kev xav no tau raug sim nyob rau hauv SWOG S1202 mus sib hais (NCT01596745), uas ntsuas exemestan qhov cuam tshuam rau BMD thaum ntxov-theem mob cancer mis.
Tshuaj kho tus kheej
Kev tshawb fawb Pharmacogenomic tau txheeb xyuas cov polymorphisms hauv CYP19A1 (aromatase gene) uas cuam tshuam rau kev ua tau zoo. Piv txwv li, rs4646 variant yog txuam nrog txhim kho DFS hauv exemestan- kho cov neeg mob, paving txoj kev rau genotype- coj kev kho.
Exemestan hmoov sawv cev rau lub hauv paus ntawm cov tshuaj hormone receptor-kev kho mob cancer mis zoo, muab kev sib xyaw ua ke ntawm kev ua tau zoo thiab kev ua haujlwm ntev. Nws irreversible aromatase inhibition, ua ke nrog cov txiaj ntsig zoo rau cov pob txha thiab lipid kev noj qab haus huv, tso nws ua tus neeg sawv cev ntau yam dhau ntawm oncology.
However, long-term safety concerns-particularly regarding bone density and cardiovascular risk-warrant ongoing surveillance. Raws li kev tshawb fawb txuas ntxiv mus unravel exemestane cov mechanisms thiab biomarkers, nws lub luag hauj lwm nyob rau hauv tus kheej cov tshuaj yog npaj los nthuav, solidifying nws qhov chaw nyob rau hauv lub kho mob armamentarium tiv thaiv estrogen- cov kab mob uas tau tsav.
Cov lus nug nquag
Dab tsi yog qhov tsaus ntuj ntawm exemestane?
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Feem ntau cov kev mob tshwm sim ntawm exemestane muaj xws likub flashes, mob pob qij txha, thiab qaug zog. Cov pob txha thinning, uas tsis tshua muaj tshwm sim, tuaj yeem tiv thaiv tau los ntawm kev noj tshuaj thiab noj cov khoom noj uas muaj calcium thiab vitamin D. Txawm tias tsis tshua muaj, muaj teeb meem loj hauv plawv ntsig txog exemestane tuaj yeem ua tau.
Puas yog exemestane suav tias yog kws khomob?
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Nws yog ib qho tseem ceeb kom nkag siab qhov ntawdExemestane tsis yog tshuaj khomob ib txwm sivthiab muaj kev sib txawv ntawm kev ua haujlwm. Nws ua haujlwm los ntawm kev txo cov tshuaj hormones uas nres cov qog nqaij hlav cancer loj hlob thiab kis mus.
Koj puas nce qhov hnyav nrog exemestane?
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Aromasin (exemestane) yog ib qho tshuaj kho mob uas siv los kho qee yam mob qog noj ntshav mis. Aromasin tuaj yeem ua rau muaj kev phiv xws li mob me mus rau qhov hnyav.Piv txwv xws li qhov hnyav ncethiab plaub hau poob.
Koj tuaj yeem nyob ntawm exemestane ntev npaum li cas?
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Lub sijhawm pom zoo uas exemestane raug coj mus rau yuav nyob ntawm koj tus kheej qhov xwm txheej. Cov neeg tau txais kev kho mob cancer mis thawj zaug feem ntau yuav siv exemestane rautsib mus rau kaum xyoo. Qee tus neeg pib noj cov tshuaj exemestane tom qab ob peb xyoos ntawm kev noj cov tshuaj hormone kho tamoxifen.
Dab tsi yog qhov zoo dua, anastrozole lossis exemestane?
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Cov tshuaj steroidal inhibitor exemestane yog ib nrab tsis-cross-resistant nrog nonsteroidal aromatase inhibitors thiab yog ib qho androgen me me thiabtuaj yeem ua pov thawj zoo tshaj rau anastrozole txog kev ua tau zoo thiab toxicity, tshwj xeeb nrog cov pob txha tsawg.
Cim npe nrov: exemestane hmoov, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom