Abiraterone (CAS No.: 154229-19-3) - Active Androgen Synthesis Inhibitor for Advanced Prostate Cancer Therapy
Raws li tus kws tshaj lij ntawm kev lag luam tshuaj -qib oncology active tshuaj cov khoom xyaw (APIs), peb muab siab -purityAbirateroneuas nruj me ntsis ua raws li kev cai thoob ntiaj teb pharmacopoeia (USP, EP, BP). Raws li cov nquag metabolite ntawm Abiraterone Acetate (ib qho tshuaj siv dav dav), qhov sib xyaw no ua haujlwm tseem ceeb hauv kev kho mob rau kev mob qog noj ntshav prostate. Nws tshwj xeeb thaiv cov khoom siv androgen sab nraum cov qog ntshav (xws li, hauv cov qog adrenal thiab cov qog nqaij hlav prostate), hais txog cov kev xav tau tsis zoo hauv cov neeg mob uas muaj tus kab mob loj hlob txawm tias tus qauv androgen deprivation therapy (ADT) thiab ua cov khoom siv tseem ceeb rau cov chaw tsim tshuaj oncology thoob ntiaj teb.
Product Basic Information
| Yam khoom | Paub meej |
|---|---|
| Khoom npe | Abiraterone |
| CAS Nr. | 154229-19-3 |
| Synonyms | (3)-17-(3-Pyridinyl)androsta-5,16-dien-3-ol; Active metabolite ntawm Abiraterone Acetate |
| Molecular Formula | C₂₄H₃₁NO |
| Molecular Luj | 349.51 |
| 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) 98.0%–102.0%; Kev hloov kho qhov muag tshwj xeeb [ ]²⁰D +15℃rau +19℃(hauv chloroform, c=1); Poob ntawm ziab Tsawg dua lossis sib npaug li 0.5%; Residue ntawm ignition Tsawg dua los yog sib npaug rau 0.1%; Cov hlau hnyav (Pb Tsawg dua lossis sib npaug li 5ppm, Hg Tsawg dua lossis sib npaug rau 1ppm, Cd Tsawg dua lossis sib npaug li 1ppm, Raws li Tsawg dua lossis sib npaug 1ppm); Cov kuab tshuaj seem (ethanol Tsawg dua lossis sib npaug li 500ppm, acetone Tsawg dua lossis sib npaug rau 500ppm, chloroform Tsawg dua lossis sib npaug li 60ppm) |
| Melting Point | 227-229℃(nrog me ntsis decomposition) |
| Boiling Point | 500.2℃ntawm 760 mmHg (theoretical) |
| Solubility | Xyaum insoluble hauv dej (≈0.05 mg / L ntawm 25 degree); Soluble hauv chloroform (≈60 mg/mL), methanol (≈5 mg/mL), ethanol (≈3 mg/mL); Sparingly soluble hauv ethyl acetate |
| Kev cia khoom | Khaws rau hauv qhov txias (2-8 degree), qhuav, lub teeb - tiv thaiv amber iav ntim; Muab ntim rau hauv nitrogen kom tsis txhob ya raws, oxidation, thiab photodegradation; Tsis txhob sib cuag nrog oxidizing agents, muaj zog acids, thiab muaj zog bases; Lub neej txee: 36 lub hlis rau qib tshuaj (thaum khaws cia rau ib qho xwm txheej) |
Core Mechanism & Therapeutic Tus Nqi
Kev loj hlob ntawm qog nqaij hlav cancer prostate yog nyob ntawm androgens (piv txwv li, testosterone, dihydrotestosterone / DHT). Thaum tus txheej txheem ADT txo qis cov qe ntshav thiab cov qog nqaij hlav, nws tsis tuaj yeem thaiv androgen synthesis hauv qog adrenal thiab prostate qog hlwb-cov "ntxiv-testicular" androgens tsav cov kab mob mus rau theem siab.
Abiraterone (daim ntawv nquag ntawm Abiraterone Acetate)exerts nws lub hom phiaj los tiv thaiv- mob qog noj ntshav los ntawm irreversibly inhibiting cytochrome P450 17A1 (CYP17A1)-ib qho tseem ceeb enzyme nyob rau hauv txoj kev androgen synthesis. CYP17A1 catalyzes ob qhov kev tshwm sim tseem ceeb:
- 17 -hydroxylation:Hloov ua lwm yam pregnenolone/progesterone (adrenal precursors) rau 17 -hydroxypregnenolone/17 -hydroxyprogesterone.
- Kev ua haujlwm C17,20-lyase:Hloov cov 17 -hydroxy metabolites mus rau dehydroepiandrosterone (DHEA)- thawj thawj ntawm testosterone thiab DHT.
Los ntawm kev thaiv cov CYP17A1, cov tshuaj tshem tawm yuav luag txhua qhov chaw ntawm androgens (testicular, adrenal, thiab qog- tau los), txo qis androgen ntau hauv lub cev thiab suppressing prostate cancer cell proliferation thiab ciaj sia taus.
Daim ntawv thov Scenario
Nws feem ntau yog siv los ua cov kws tshuaj API rau kev tsim cov tshuaj ntawm qhov ncauj oncology formulations (cov ntsiav tshuaj / tshuaj ntsiav) los kho mob qog noj ntshav siab. Nws daim ntawv thov kev kho mob (ntawm cov khoom tsim tawm) suav nrog:
1. Metastatic Castration-Resistant Prostate Cancer (mCRPC)
Rau cov neeg mob uas muaj mCRPC (prostate cancer uas loj hlob txawm tias castrate testosterone qib), cov khoom tsim (tswj raws li Abiraterone Acetate) yog ua ke nrog prednisone (ib corticosteroid) kom txo tau cov kev mob tshwm sim. Cov ntaub ntawv kho mob qhia tau tias nws txuas ntxiv kev ciaj sia tag nrho (OS) los ntawm 4-6 lub hlis thiab ncua kev kis kab mob piv rau cov placebo.
2. Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)
Nyob rau hauv siab -mHSPC (mob qog noj ntshav uas tau kis mus rau qhov chaw nyob deb tab sis tseem teb rau ADT), kev kho mob nrog prednisone ntxiv rau ADT txo qhov kev pheej hmoo ntawm kev kis kab mob lossis tuag los ntawm ~ 50% thiab txuas ntxiv OS (qhov nruab nrab OS tsis mus txog hauv kev sim vs. 34.7 hli nrog ADT ib leeg).
3.R&D & Kev Tsim Kho Kev Tsim Kho
Lub compound kuj tseem siv rau hauv preclinical thiab kho mob R & D rau:
- Optimizing tshuaj xa cov tshuab (xws li, txhim kho solubility los txhim kho qhov ncauj bioavailability).
- Txhim kho kev sib xyaw ua ke (xws li, nrog PARP inhibitors rau BRCA-mob qog nqaij hlav prostate).
- Tshawb nrhiav cov ntawv thov muaj peev xwm hauv lwm cov androgen{0}} cov kab mob uas tau tsav (xws li, qee hom mob qog noj ntshav mis).
Quality & Safety Assurance
Raws li qhov tshwj xeeb oncology API, Abiraterone yuav tsum muaj kev tswj xyuas nruj kom ntseeg tau tias muaj txiaj ntsig, purity, thiab ua raws li cov qauv kev cai thoob ntiaj teb:
1. Kev tsim khoom & Purity Control
Synthesis txheej txheem: Ua los ntawm ntau-qib chiral tshuaj synthesis (xws li steroid nucleus siv, pyridine nplhaib txuas, thiab hydroxyl pab pawg tiv thaiv / deprotection). Kev tswj hwm nruj ntawm stereochemistry ua kom muaj kev ua haujlwm 3 -isomer rau ntau dua lossis sib npaug rau 99.5% ntawm cov khoom kawg.
Kev huv huv: Purified los ntawm kem chromatography thiab recrystallization kom tshem tawm impurities (xws li, diastereomers, hluavtaws byproducts) - ib qho impurity Tsawg dua los yog sib npaug rau 0.2%, tag nrho impurities Tsawg dua lossis sib npaug li 0.5%.
Ua raws li GMP: Ua nyob rau hauv Qib A / B cleanrooms (raws li ICH Q7 cov lus qhia) nrog rau tag nrho traceability ntawm raw cov ntaub ntawv thiab cov txheej txheem ntau lawm; Kev tshuaj xyuas tsis tu ncua los ntawm thib peb - tog neeg tswj hwm (xws li FDA, EMA).
2. Cov Txheej Txheem Kev Ntsuas Zoo
| Cov khoom kuaj | Txoj kev | Kev lees txais |
|---|---|---|
| Purity & Assay | HPLC (C18 kem, 254 nm nrhiav pom) | Purity Ntau dua lossis sib npaug li 99.0%; Kev ntsuas 98.0% - 102.0% |
| Chiral Purity | Chiral HPLC (cellulose tris (3,5-dimethylphenylcarbamate) kem) | Active 3 -isomer Ntau dua lossis sib npaug rau 99.5%; Inactive 3 -isomer Tsawg dua lossis sib npaug li 0.5% |
| 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, FID ntes) | Chav kawm 2 cov kuab tshuaj tsawg dua lossis sib npaug ntawm 500ppm; Cov kuab tshuaj Class 1 tsis kuaj |
| Poob rau ziab | Gravimetric method (105℃rau 2 teev) | Tsawg dua los yog sib npaug li 0.5% |
| Kev txheeb xyuas | IR Spectroscopy & HPLC Retention Time | Sib tw siv tus qauv spectrum; Lub sijhawm khaws cia raws li tus qauv |
3. Kev ceeb toom kev nyab xeeb (rau cov khoom tsim)
Cov teebmeem: Thaum siv hauv kev kho mob (raws li ib feem ntawm cov tshuaj formulated), cov kev mob tshwm sim muaj xws li kub siab, hypokalemia (tsis tshua muaj poov tshuaj), dej tuav, thiab edema (tswj nrog prednisone concurrent). Tsis tshua muaj tab sis muaj kev pheej hmoo loj xws li hepatotoxicity (saib lub siab ua haujlwm txhua hli) thiab mob plawv arrhythmias.
Contraindications: Hypersensitivity rau Abiraterone los yog 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 raug API).
Cov tshuaj sib cuam tshuam: Tsis txhob siv ib txhij nrog cov muaj zog CYP3A4 inducers (xws li, rifampin, phenytoin) raws li lawv txo cov qib Abiraterone; siv ceev faj nrog warfarin (nce los ntshav txaus) thiab digoxin (nce arrhythmia txaus ntshai).
Kev koom tes & Kev Pabcuam
Peb muab cov kws tshuaj -qib Abiraterone hauv kev ntim khoom kom tau raws li cov kev xav tau ntawm cov tuam txhab tshuaj thiab R&D cov koom haum:
Ntim Cov Kev Xaiv: 1g, 10g, 100g, los yog 1kg amber iav vials (sau nrog Teflon-lined caps thiab desiccants) rau me me -batch R&D; 5kg, 25kg fiber ntau nruas (nrog txhuas ntawv ci liner) rau kev lag luam ntau lawm-tag nrho hauv kev tiv thaiv nitrogen.
Cov ntaub ntawv tswj hwm: Muab cov ntaub ntawv qhia ntxaws ntxaws, suav nrog Daim Ntawv Pov Thawj Kev Ntsuam Xyuas (COA), Cov Ntaub Ntawv Tshuaj Yeeb Tshuaj (DMF), Daim Ntawv Pov Thawj Zoo (CEP), thiab cov ntaub ntawv ruaj ntseg (nrawm, ntev- lub sijhawm) los txhawb kev sau npe tshuaj hauv EU, US, Tuam Tshoj, thiab lwm yam lag luam thoob ntiaj teb.
Tus nqi -Kev Pabcuam Ntxiv: Muab kev kho kom haum xeeb impurity profileing, solubility li kev pab tswv yim, thiab preclinical formulation kev pab txhawb nqa (xws li, rau lipid-raws li kev xa khoom) los txhim kho cov khoom tsim.
Tiv tauj peb
Yog tias koj yog cov chaw tsim tshuaj, lub tuam txhab oncology R&D, lossis cov koom haum tsim khoom cog lus (CMO) tsom rau kev kho mob qog noj ntshav prostate, peb zoo siab tos txais koj los koom tes nrog peb:
Cov ntaub ntawv tiv tauj:
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Chaw nyob: [Koj Chaw Nyob Chaw Nyob, xws li, No. XX, High-Tech Zone, Chengdu, Sichuan, Suav teb]
Peb ua raws li cov hauv paus ntsiab lus ntawm "oncology- qib zoo, kev tswj hwm, thiab cov neeg siv khoom-centricity" thiab tau cog lus los muab APIs txhim khu kev qha rau lub neej-txuag kev kho mob qog noj ntshav thoob ntiaj teb!
Cim npe nrov: Tuam Tshoj Abiraterone CAS 154229-19-3, Tuam Tshoj Abiraterone CAS 154229-19-3 manufacturers, lwm tus neeg
