Peringatan Keamanan

The oral LD50 is > 400 mg/kg in rats and 800 mg/kg in mice.L47730

The human experience of overdose with abiraterone is limited. Toxicity is related to the blockade of CYP17 activity. Blockade results in the accumulation of upstream mineralocorticoids like 11-deoxycorticosterone, leading to secondary hyperaldosteronism. Signs of hyperaldosteronism include fluid retention and hypokalemia.A257158 As there is no specific antidote for abiraterone overdose, overdosage should be managed with general supportive measures, including monitoring and assessment of cardiac and liver function.L40968, L40193

Abiraterone

DB05812

small molecule approved

Deskripsi

Abiraterone is a potent, irreversible, and selective inhibitor of 17 ?hydroxylase/C17,20-lyase (CYP17), an enzyme expressed in testicular, adrenal, and prostatic tumour tissues, to regulate androgen biosynthesis.A3811, A260880, L40968 Abiraterone was first approved by the FDA and EMA on April,A260880 July,L47745 and September 2011,A260880 respectively. It is used to treat metastatic castration-resistant prostate cancer and hormone-sensitive high-risk metastatic prostate cancer.L40968, L40193, L47740, L47745

As abiraterone has poor oral bioavailability and is susceptible to hydrolysis by esterases, abiraterone acetate was developed as an orally bioavailable prodrug with enhanced stability and absorption.A3811, A260835

Struktur Molekul 2D

Berat 349.509
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In patients with mCRPC, the mean (± SD) terminal half-life of abiraterone in plasma is 12 (± 5) hours.[L40968, L40193]
Volume Distribusi The mean (± SD) apparent steady-state volume of distribution is 19,669 (± 13,358) L.[L40968, L40193]
Klirens (Clearance) -

Absorpsi

Geometric mean (± SD) Cmax was 73 (± 44) ng/mL and AUC0-? was 373 (± 249) ng x hr/mL following a single dose of 500 mg abiraterone acetate in overnight-fasted healthy subjects. Dose proportionality was observed in single doses of abiraterone acetate ranging from 125 mg to 625 mg.L40968 A group of patients with mCRPC received a daily dose of 1,000 mg: at steady-state, the mean (± SD) Cmax was 226 (± 178) ng/mL and AUC was 993 (± 639) ng x hr/mL.L40193 Following oral administration of abiraterone acetate to patients with metastatic castration-resistant prostate cancer, the median Tmax was two hours. In vivo, abiraterone acetate is converted to abiraterone. In clinical studies of other abiraterone acetate formulations, abiraterone acetate plasma concentrations were below detectable levels (< 0.2 ng/mL) in > 99% of the analyzed samples.L40968 Systemic exposure to abiraterone is increased when abiraterone acetate is administered with food. Abiraterone Cmax was approximately 6.5-fold higher, and AUC0-? was 4.4-fold higher when a single dose of abiraterone acetate 500 mg was administered with a high-fat meal (56-60% fat, 900-1,000 calories) compared to overnight fasting in healthy subjects.L40968 Given the normal variation in the content and composition of meals, taking abiraterone with meals has the potential to result in increased and highly variable exposures.L40193

Metabolisme

The conversion of abiraterone acetate to abiraterone, the active metabolite, is likely to be mediated by esterases, although specific esterases have not been identified. In human plasma, the two main circulating metabolites are abiraterone sulfate, which is formed by CYP3A4 and SULT2A1, and N-oxide abiraterone sulfate, which is formed by SULT2A1. These metabolites each account for about 43% of abiraterone exposure and are pharmacologically inactive.A260885, L40968, L40193

Rute Eliminasi

Following oral administration of 14C-abiraterone acetate, approximately 88% of the radioactive dose is recovered in feces: the major compounds present in feces are unchanged abiraterone acetate and abiraterone, accounting for approximately 55% and 22% of the administered dose, respectively. Approximately 5% of the dose is recovered in urine.L40968, L40193

Interaksi Makanan

3 Data
  • 1. Exercise caution with St. John's Wort. This herb induces CYP3A4 and may increase the serum levels of abiraterone.
  • 2. Take on an empty stomach. Food increases Cmax and AUC. Take ZYTIGA , a product of abiraterone, at least 1 hour before or 2 hours after eating as food may increase exposure to abiraterone by 4-fold.
  • 3. Take with or without food. Food increases Cmax and AUC. YONSA, a product of abiraterone, can be taken with or without food.

Interaksi Obat

559 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Abiraterone.
Citalopram The metabolism of Citalopram can be decreased when combined with Abiraterone.
Clopidogrel The serum concentration of Clopidogrel can be increased when it is combined with Abiraterone.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Abiraterone.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Abiraterone.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Abiraterone.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Abiraterone.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Abiraterone.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Abiraterone.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Abiraterone.
Zolmitriptan The serum concentration of Zolmitriptan can be increased when it is combined with Abiraterone.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Abiraterone.
(S)-Warfarin The metabolism of (S)-Warfarin can be decreased when combined with Abiraterone.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Abiraterone.
Spironolactone The therapeutic efficacy of Abiraterone can be decreased when used in combination with Spironolactone.
Tamoxifen The metabolism of Tamoxifen can be decreased when combined with Abiraterone.
Mefenamic acid The serum concentration of Mefenamic acid can be increased when it is combined with Abiraterone.
Ondansetron The serum concentration of Ondansetron can be increased when it is combined with Abiraterone.
Azelastine The serum concentration of Azelastine can be increased when it is combined with Abiraterone.
Ethinylestradiol The serum concentration of Ethinylestradiol can be increased when it is combined with Abiraterone.
Fluvoxamine The serum concentration of Fluvoxamine can be increased when it is combined with Abiraterone.
Bortezomib The serum concentration of Bortezomib can be increased when it is combined with Abiraterone.
Betaxolol The serum concentration of Betaxolol can be increased when it is combined with Abiraterone.
Caffeine The serum concentration of Caffeine can be increased when it is combined with Abiraterone.
Anagrelide The serum concentration of Anagrelide can be increased when it is combined with Abiraterone.
Carmustine The serum concentration of Carmustine can be increased when it is combined with Abiraterone.
Theophylline The metabolism of Theophylline can be decreased when combined with Abiraterone.
Disopyramide The serum concentration of Disopyramide can be increased when it is combined with Abiraterone.
Lidocaine The serum concentration of Lidocaine can be increased when it is combined with Abiraterone.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Abiraterone.
Ropivacaine The serum concentration of Ropivacaine can be increased when it is combined with Abiraterone.
Acetaminophen The serum concentration of Acetaminophen can be increased when it is combined with Abiraterone.
Olanzapine The serum concentration of Olanzapine can be increased when it is combined with Abiraterone.
Chlorzoxazone The serum concentration of Chlorzoxazone can be increased when it is combined with Abiraterone.
Grepafloxacin The serum concentration of Grepafloxacin can be increased when it is combined with Abiraterone.
Mirtazapine The serum concentration of Mirtazapine can be increased when it is combined with Abiraterone.
Mexiletine The serum concentration of Mexiletine can be increased when it is combined with Abiraterone.
Tacrine The serum concentration of Tacrine can be increased when it is combined with Abiraterone.
Triamterene The serum concentration of Triamterene can be increased when it is combined with Abiraterone.
Sorafenib The serum concentration of Sorafenib can be increased when it is combined with Abiraterone.
Promazine The serum concentration of Promazine can be increased when it is combined with Abiraterone.
Zolpidem The serum concentration of Zolpidem can be increased when it is combined with Abiraterone.
Entecavir The serum concentration of Entecavir can be increased when it is combined with Abiraterone.
Imipramine The metabolism of Imipramine can be decreased when combined with Abiraterone.
Nabumetone The serum concentration of Nabumetone can be increased when it is combined with Abiraterone.
Quinine The serum concentration of Quinine can be increased when it is combined with Abiraterone.
Fluoxetine The serum concentration of Fluoxetine can be increased when it is combined with Abiraterone.
Chlorpromazine The serum concentration of Chlorpromazine can be increased when it is combined with Abiraterone.
Flutamide The serum concentration of Flutamide can be increased when it is combined with Abiraterone.
Albendazole The serum concentration of Albendazole can be increased when it is combined with Abiraterone.
Erlotinib The metabolism of Erlotinib can be decreased when combined with Abiraterone.
Mephenytoin The serum concentration of Mephenytoin can be increased when it is combined with Abiraterone.
Rofecoxib The serum concentration of Rofecoxib can be increased when it is combined with Abiraterone.
Fluorouracil The metabolism of Fluorouracil can be decreased when combined with Abiraterone.
Cinnarizine The serum concentration of Cinnarizine can be increased when it is combined with Abiraterone.
Propranolol The serum concentration of Propranolol can be increased when it is combined with Abiraterone.
Clonidine The metabolism of Clonidine can be decreased when combined with Abiraterone.
Diclofenac The serum concentration of Diclofenac can be increased when it is combined with Abiraterone.
Imatinib The serum concentration of Imatinib can be increased when it is combined with Abiraterone.
Guanabenz The serum concentration of Guanabenz can be increased when it is combined with Abiraterone.
Pemetrexed The serum concentration of Pemetrexed can be increased when it is combined with Abiraterone.
Verapamil The serum concentration of Verapamil can be increased when it is combined with Abiraterone.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Abiraterone.
Paroxetine The serum concentration of Paroxetine can be increased when it is combined with Abiraterone.
Thiabendazole The serum concentration of Thiabendazole can be increased when it is combined with Abiraterone.
Riluzole The serum concentration of Riluzole can be increased when it is combined with Abiraterone.
Zileuton The serum concentration of Zileuton can be increased when it is combined with Abiraterone.
Etoposide The serum concentration of Etoposide can be increased when it is combined with Abiraterone.
Estradiol The serum concentration of Estradiol can be increased when it is combined with Abiraterone.
Acyclovir The serum concentration of Acyclovir can be increased when it is combined with Abiraterone.
Naproxen The serum concentration of Naproxen can be increased when it is combined with Abiraterone.
Pentoxifylline The serum concentration of Pentoxifylline can be increased when it is combined with Abiraterone.
Trifluoperazine The serum concentration of Trifluoperazine can be increased when it is combined with Abiraterone.
Perphenazine The serum concentration of Perphenazine can be increased when it is combined with Abiraterone.
Dacarbazine The serum concentration of Dacarbazine can be increased when it is combined with Abiraterone.
Terbinafine The serum concentration of Terbinafine can be increased when it is combined with Abiraterone.
Ranitidine The serum concentration of Ranitidine can be increased when it is combined with Abiraterone.
Ethanol The serum concentration of Ethanol can be increased when it is combined with Abiraterone.
Cyclobenzaprine The serum concentration of Cyclobenzaprine can be increased when it is combined with Abiraterone.
Maprotiline The serum concentration of Maprotiline can be increased when it is combined with Abiraterone.
Alosetron The serum concentration of Alosetron can be increased when it is combined with Abiraterone.
Lomefloxacin The serum concentration of Lomefloxacin can be increased when it is combined with Abiraterone.
Azathioprine The serum concentration of Azathioprine can be increased when it is combined with Abiraterone.
Frovatriptan The serum concentration of Frovatriptan can be increased when it is combined with Abiraterone.
Levobupivacaine The serum concentration of Levobupivacaine can be increased when it is combined with Abiraterone.
Cinacalcet The serum concentration of Cinacalcet can be increased when it is combined with Abiraterone.
Selegiline The serum concentration of Selegiline can be increased when it is combined with Abiraterone.
Tocainide The serum concentration of Tocainide can be increased when it is combined with Abiraterone.
Praziquantel The serum concentration of Praziquantel can be increased when it is combined with Abiraterone.
Melatonin The serum concentration of Melatonin can be increased when it is combined with Abiraterone.
Primaquine The serum concentration of Primaquine can be increased when it is combined with Abiraterone.
Hesperetin The serum concentration of Hesperetin can be increased when it is combined with Abiraterone.
Leflunomide The serum concentration of Leflunomide can be increased when it is combined with Abiraterone.
Pimozide The metabolism of Pimozide can be decreased when combined with Abiraterone.
Nifedipine The serum concentration of Nifedipine can be increased when it is combined with Abiraterone.
Carvedilol The serum concentration of Carvedilol can be increased when it is combined with Abiraterone.
Doxepin The serum concentration of Doxepin can be increased when it is combined with Abiraterone.
Propafenone The serum concentration of Propafenone can be increased when it is combined with Abiraterone.
Domperidone The serum concentration of Domperidone can be increased when it is combined with Abiraterone.
Dexfenfluramine The serum concentration of Dexfenfluramine can be increased when it is combined with Abiraterone.

Target Protein

Steroid 17-alpha-hydroxylase/17,20 lyase CYP17A1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15150570
    O'Donnell A, Judson I, Dowsett M, Raynaud F, Dearnaley D, Mason M, Harland S, Robbins A, Halbert G, Nutley B, Jarman M: Hormonal impact of the 17alpha-hydroxylase/C(17,20)-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer. Br J Cancer. 2004 Jun 14;90(12):2317-25.
  • PMID: 23199349
    Ryan CJ, Cheng ML: Abiraterone acetate for the treatment of prostate cancer. Expert Opin Pharmacother. 2013 Jan;14(1):91-6. doi: 10.1517/14656566.2013.745852. Epub 2012 Nov 30.
  • PMID: 28131750
    Gill D, Gaston D, Bailey E, Hahn A, Gupta S, Batten J, Alex A, Boucher K, Stenehjem D, Agarwal N: Efficacy of Eplerenone in the Management of Mineralocorticoid Excess in Men With Metastatic Castration-resistant Prostate Cancer Treated With Abiraterone Without Prednisone. Clin Genitourin Cancer. 2017 Aug;15(4):e599-e602. doi: 10.1016/j.clgc.2016.12.008. Epub 2017 Jan 5.
  • PMID: 25592324
    Stappaerts J, Geboers S, Snoeys J, Brouwers J, Tack J, Annaert P, Augustijns P: Rapid conversion of the ester prodrug abiraterone acetate results in intestinal supersaturation and enhanced absorption of abiraterone: in vitro, rat in situ and human in vivo studies. Eur J Pharm Biopharm. 2015 Feb;90:1-7. doi: 10.1016/j.ejpb.2015.01.001. Epub 2015 Jan 12.
  • PMID: 12767280
    Haidar S, Ehmer PB, Barassin S, Batzl-Hartmann C, Hartmann RW: Effects of novel 17alpha-hydroxylase/C17, 20-lyase (P450 17, CYP 17) inhibitors on androgen biosynthesis in vitro and in vivo. J Steroid Biochem Mol Biol. 2003 Apr;84(5):555-62. doi: 10.1016/s0960-0760(03)00070-0.
  • PMID: 21761368
    Basu S, Tindall DJ: Androgen action in prostate cancer. Horm Cancer. 2010 Oct;1(5):223-8. doi: 10.1007/s12672-010-0044-4.
  • PMID: 29951171
    James A, Vincent B, Sivadas A, Pavithran K: A Study on the Clinical Outcome of Abiraterone Acetate in Castration Resistant Prostate Cancer Patients. Int J Hematol Oncol Stem Cell Res. 2018 Jan 1;12(1):4-7.
  • PMID: 23020788
    Acharya M, Gonzalez M, Mannens G, De Vries R, Lopez C, Griffin T, Tran N: A phase I, open-label, single-dose, mass balance study of 14C-labeled abiraterone acetate in healthy male subjects. Xenobiotica. 2013 Apr;43(4):379-89. doi: 10.3109/00498254.2012.721022. Epub 2012 Sep 28.

Contoh Produk & Brand

Produk: 113 • International brands: 0
Produk
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