Abiraterone Acetate (CAS No.: 154229-}18-2) - Targeted Androgen Synthesis Inhibitor rau Advanced Prostate Cancer
Raws li tus kws tshaj lij ntawm cov kws kho mob - qib oncology cov khoom xyaw nquag, peb muab siab -Abiraterone Acetate purity uas ua raws li cov qauv tshuaj tshuaj thoob ntiaj teb (USP, EP, BP). Thawj -hauv- chav kawm qhov ncauj androgen synthesis inhibitor, nws yog lub hauv paus hauv kev kho mob ntawmmetastatic castration- mob qog nqaij hlav prostate (mCRPC)thiabmetastatic castration-sensitive prostate cancer (mCSPC)-ob theem ntawm kev mob qog noj ntshav prostate uas tau tsav los ntawm androgen signaling. Nws cov txheej txheem ntawm kev tsom mus rau androgen ntau lawm sab nraum cov qe ntshav (piv txwv li, hauv cov qog adrenal, cov qog nqaij hlav prostate) hais txog qhov xav tau tseem ceeb hauv cov neeg mob uas muaj tus kab mob hnyav txawm tias tus qauv hormonal kho.
Product Basic Information
| Yam khoom | Paub meej |
|---|---|
| Khoom npe | Abiraterone Acetate |
| CAS Nr. | 154229-18-2 |
| Synonyms | (3)-17-(3-Pyridinyl)androsta-5,16-dien-3-yl acetate; Zytiga® (lub npe hom rau kev lag luam formulations) |
| Molecular Formula | C₂₆H₃₃NO₂ |
| Molecular Luj | 391.54 |
| Qhov tshwm sim | Dawb rau tawm -dawb crystalline hmoov; Tsis hnov tsw |
| Specification | - Pharmaceutical Qib: Purity Ntau dua lossis sib npaug li 99.0% (HPLC); Assay (raws li abiraterone acetate) 98.0% -102.0%; Kev sib hloov kho qhov muag tshwj xeeb [ ]²⁰D +14℃rau +18℃(hauv chloroform); Poob ntawm ziab Tsawg dua lossis sib npaug li 0.5%; Cov hlau hnyav (Pb Tsawg dua lossis sib npaug ntawm 5ppm, Hg Tsawg dua lossis sib npaug rau 1ppm, Cd Tsawg dua lossis sib npaug li 1ppm); Cov kuab tshuaj seem (ethanol Tsawg dua lossis sib npaug rau 500ppm, acetone Tsawg dua lossis sib npaug rau 500ppm) |
| Melting Point | 110-114℃(nrog decomposition) |
| Solubility | Xyaum insoluble hauv dej (≈0.1 mg / L ntawm 25 degree); Soluble hauv ethanol (≈2 mg/mL), methanol (≈3 mg/mL), thiab chloroform (≈50 mg/mL); Sparingly soluble hauv ethyl acetate |
| Kev cia khoom | Khaws rau hauv qhov txias (2-8 degree), qhuav, lub teeb -cov thawv tiv thaiv; Sealed los tiv thaiv kev nqus dej noo, oxidation, thiab photodegradation; Lub neej txee: 36 lub hlis rau qib tshuaj (thaum khaws cia rau ib qho xwm txheej) |
Core Functions & Mechanism of Action
Prostate cancer kev loj hlob yog nyob ntawm androgens (txiv neej cov tshuaj hormones, piv txwv li, testosterone, dihydrotestosterone / DHT). Standard hormonal therapy (androgen deprivation therapy / ADT) txo cov qe ntshav ntawm androgen ntau lawm tab sis tsis thaiv androgen synthesis nyob rau hauv lwm cov ntaub so ntswg (adrenal qog, prostate qog hlwb) los yog los ntawm adrenal precursors (xws li, dehydroepiandrosterone / DHEA).
Abiraterone Acetate yog ibprodrug-nws tau hloov dua siab tshiab hauv lub cev mus rau nws daim ntawv nquag,tshuaj abiraterone, uas irreversibly inhibitscytochrome P450 17A1 (CYP17A1). CYP17A1 yog ib qho tseem ceeb enzyme hauv androgen synthesis uas catalyzes ob kauj ruam tseem ceeb:
17 -hydroxylation: Hloov pregnenolone/progesterone rau 17 -hydroxypregnenolone/17 -hydroxyprogesterone.
Kev ua haujlwm C17,20-lyase: Hloov cov 17 -hydroxy metabolites rau DHEA (tus thawj coj ntawm testosterone thiab DHT).
Los ntawm kev thaiv CYP17A1, abiraterone tshem tawm yuav luag txhua qhov chaw ntawm androgens (testicular, adrenal, thiab qog- tau los), inhibiting prostate cancer cell loj hlob thiab ciaj sia.
Kev Siv Tshuaj Kho Mob (Human Oncology)
Abiraterone Acetate tau pom zoo thoob ntiaj teb rau kev kho mob qog noj ntshav prostate, ib txwm siv ua ke nrogprednisone / prednisolone(ib corticosteroid) kom txo tau cov kev mob tshwm sim (piv txwv li, mineralocorticoid tshaj). Nws cov ntsiab lus tseem ceeb suav nrog:
1. Metastatic Castration-Resistant Prostate Cancer (mCRPC)
mCRPC yog mob qog noj ntshav prostate uas loj tuaj txawm tias ADT (castrate qib ntawm testosterone). Abiraterone Acetate yog siv nyob rau hauv ob qhov chaw:
Tom qab -kev kho mob mCRPC: Rau cov neeg mob uas tau txais docetaxel ua ntej (ib qho tshuaj khomob). Qhov ncauj koob tshuaj: 1000 mg ib hnub ib zaug (ntawm plab khoob) + prednisone 5 mg ob zaug ib hnub. Kev sim tshuaj (piv txwv li, COU-AA-301) tau pom tias muaj kev muaj sia nyob ntev (OS: 15.8 lub hlis vs. 11.2 hli nrog cov placebo) thiab ncua kev kis kab mob.
Ua ntej -kev kho mob mCRPC: Rau cov neeg mob uas tsis tau txais kev kho mob ua ntej. Qhov ncauj koob tshuaj: 1000 mg ib hnub ib zaug + prednisone 5 mg ob zaug ib hnub. Cov kev sim (piv txwv li, COU-AA-302) tau ua kom pom kev txhim kho OS (34.7 lub hlis vs{10}} hli nrog cov placebo) thiab txo qhov mob.
2. Metastatic Castration-Sensitive Prostate Cancer (mCSPC)
mCSPC yog mob qog noj ntshav prostate uas tau kis mus rau qhov chaw nyob deb (xws li cov pob txha, cov qog ntshav qog) tab sis tseem teb rau ADT. Abiraterone Acetate tau pom zoo siv ua ke nrog ADT thiab prednisone:
koob tshuaj qhov ncauj: 1000 mg ib hnub ib zaug + prednisone 5 mg ob zaug ib hnub + ADT (xws li, luteinizing hormone- tso cov tshuaj hormone agonists / antagonists). Cov kev sim (piv txwv li, LATITUDE, STAMPEDE) tau pom cov txiaj ntsig tseem ceeb ntawm OS (qhov nruab nrab OS tsis mus txog . 34.7 lub hlis nrog ADT ib leeg) thiab txo qis kev pheej hmoo ntawm kev kis kab mob lossis tuag los ntawm ~ 50%.
3. Lwm yam kev tshawb fawb siv
Kev tshawb nrhiav txuas ntxiv nthuav dav nws siv rau:
Tsis yog -metastatic castration- mob qog nqaij hlav prostate (nmCRPC).
Prostate cancer hauv cov neeg mob uas muaj kev hloov pauv BRCA (txhim kho DNA kho- cov qog tsis txaus).
Quality & Safety Assurance
Raws li cov tshuaj tshwj xeeb oncology nrog rau kev kho mob nruj heev, Abiraterone Acetate yuav tsum muaj kev tswj xyuas nruj kom ntseeg tau tias muaj txiaj ntsig, purity, thiab kev nyab xeeb:
1. Kev tsim khoom & Purity Control
Synthesis: Ua los ntawm ntau- kauj ruam chiral chemical synthesis (suav nrog steroid nucleus kev tsim kho thiab pyridine nplhaib txuas), nrog rau kev tswj nruj ntawm stereochemistry (kom ua kom muaj zog 3 -isomer). Purification ntawm kab chromatography thiab recrystallization tshem tawm impurities (xws li, diastereomers, hluavtaws byproducts) kom tsawg dua los yog sib npaug li 0.1%.
Ua raws li GMP: Ua nyob rau hauv Qib A/B cleanrooms (raws li ICH Q7 cov lus qhia) los tiv thaiv kab mob microbial thiab hla- kis nrog lwm yam tshuaj.
2. Critical Quality Attributes (CQAs)
| Cov khoom kuaj | Txoj kev | Kev lees txais |
|---|---|---|
| Purity & Assay | HPLC (C18 kem, 254 nm nrhiav pom) | Ntau dua lossis sib npaug rau 99.0% purity; 98.0% -102.0% kev xeem |
| Chiral Purity (3 -isomer) | Chiral HPLC (cellulose{0}}raws li kem) | Ntau dua lossis sib npaug li 99.5% (active isomer); Tsawg dua lossis sib npaug li 0.5% (tsis ua haujlwm 3 -isomer) |
| Yam khoom muaj feem | HPLC (gradient elution) | Ib qho impurity Tsawg dua lossis sib npaug li 0.2%; tag nrho impurities Tsawg dua lossis sib npaug li 0.5% |
| Hnyav Hlau | ICP-MS (Inductively Coupled Plasma-Mass Spectrometry) | Pb Tsawg dua lossis sib npaug rau 5ppm, Hg Tsawg dua lossis sib npaug rau 1ppm, Cd Tsawg dua lossis sib npaug rau 1ppm, Raws li Tsawg dua lossis sib npaug rau 1ppm |
| Residual Solvents | GC (headspace sampling) | Chav kawm 2 cov kuab tshuaj (ethanol, acetone) Tsawg dua lossis sib npaug li 500ppm; Class 1 cov kuab tshuaj (benzene, methanol) tsis kuaj |
| Dissolution Rate (Tablets) | USP Apparatus II (paddle method, 0.05M HCl + 0.5% sodium lauryl sulfate) | Ntau dua lossis sib npaug li 80% yaj hauv 60 feeb |
3. Kev txiav txim siab txog kev nyab xeeb
Cov teebmeem: Feem ntau cov kev mob tshwm sim muaj feem xyuam rau cov mineralocorticoid ntau dhau (vim yog CYP17A1 inhibition cuam tshuam rau cortisol synthesis) thiab muaj xws li kub siab, hypokalemia (tsis tshua muaj poov tshuaj), dej tuav, thiab edema. Cov no yog tswj nrog concurrent prednisone. Tsis tshua muaj tab sis muaj kev phiv loj muaj xws li hepatotoxicity (saib xyuas daim siab ua haujlwm kuaj / LFTs txhua hli), plawv arrhythmias, thiab adrenal insufficiency.
Contraindications: hypersensitivity rau abiraterone acetate los yog lwm yam excipients; Kev puas siab puas ntsws loj heev (Child-Pugh Class C); cev xeeb tub (kev pheej hmoo teratogenic- cov poj niam uas muaj hnub nyoog me nyuam yuav tsum tsis txhob kis tau).
Cov tshuaj sib cuam tshuam: Tsis txhob siv ib txhij nrog cov muaj zog CYP3A4 inducers (xws li, rifampin, phenytoin)-lawv txo cov qib abiraterone. Siv ceev faj nrog warfarin (ua rau muaj kev pheej hmoo los ntshav) thiab digoxin (ua rau muaj kev pheej hmoo ntawm hypokalemia- ntsig txog arrhythmia).
Kev koom tes & kev sib cuag
Peb muab cov kws kho mob -qib Abiraterone Acetate hauv cov ntim tshwj xeeb (amber iav vials nrog desiccants) kom muaj kev ruaj ntseg:
Ntim: 1g, 10g, 100g, lossis kev cai kom muaj nuj nqis (rau R&D lossis kev lag luam tsim khoom), kaw hauv qab nitrogen los tiv thaiv oxidation.
Kev pab txhawb nqa: Muab cov ncauj lus kom ntxaws COA (Certificate of Analysis), cov ntaub ntawv ruaj ntseg, thiab cov ntaub ntawv tswj hwm (DMF, CEP) los txhawb kev sau npe tshuaj hauv ntiaj teb kev lag luam (US, EU, APAC).
Yog tias koj yog cov chaw tsim tshuaj, lub tuam txhab oncology R&D, lossis cov koom haum tsim kev cog lus (CMO) tsom rau kev kho mob qog noj ntshav, thov hu rau peb kom paub meej kev koom tes:
Cov ntaub ntawv tiv tauj:
Email: sales@huarongpharma.com
Xov tooj/WhatsApp: +86 13751168070
Peb ua raws li cov hauv paus ntsiab lus ntawm "oncology- qib zoo, kev tswj hwm kev tswj hwm, thiab kev nyab xeeb ntawm tus neeg mob" thiab tos ntsoov yuav txhawb nqa kev txhim kho thiab kev noj qab haus huv ntawm lub neej-txuag kev kho mob qog noj ntshav prostate!
Hot TagsTom ntej: Abiraterone Acetate 154229-18-2, Prostate Cancer Drug, CYP17A1 Inhibitor, mCRPC Treatment, Oncology API, Pharmaceutical Grade Abiraterone, Tuam Tshoj Oncology Supplier
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