Peringatan Keamanan

The reported oral TDLo in a human woman is 1.68 mg/kg given intermittently over the course of 12 weeks.L8887 Knowledge of the signs and symptoms of anastrozole overdose is incomplete as there are no documented descriptions of a patient receiving more than 60mg,L8872 a dose which was administered to a healthy male volunteer and was well-tolerated.L8863,L8869 There is no antidote for anastrozole and treatment should be supportive and symptomatic, including close monitoring of patient vital signs. As anastrozole exhibits relatively low protein binding, dialysis may be helpful and should be considered in select cases.L8863,L8869

Anastrozole

DB01217

small molecule approved investigational

Deskripsi

Anastrozole is a non-steroidal aromatase inhibitor (AI), similar to letrozole, used to decrease circulating estrogen levels in the treatment of postmenopausal women with estrogen-responsive breast cancer.L8863 Anastrozole is also related to exemestane, a steroidal AI, but its non-steroidal nature provides stark advantages including a lack of steroid-associated adverse effects such as weight gain and acne.A186865 Aromatase inhibitors, including anastrozole, have become endocrine drugs of choice in the treatment of postmenopausal breast cancer due to a more favourable efficacy and adverse effect profile as compared to earlier estrogen receptor modulators such as tamoxifen.A186877,A186955

Anastrozole was first approved for use in the United States in 1995.L8863

Struktur Molekul 2D

Berat 293.3663
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of anastrozole is approximately 50 hours.[L8863,L8869,A186877]
Volume Distribusi The volume of distribution of anastrozole into brain tissue in mice is 3.19 mL/g. Distribution into the CNS is limited due to the activity of P-gp efflux pumps at the blood brain barrier, of which anastrozole is a substrate.[A186859]
Klirens (Clearance) Anastrozole's clearance is mainly via hepatic metabolism and can therefore be altered in patients with hepatic impairment - patients with stable hepatic cirrhosis exhibit an apparent oral clearance approximately 30% lower compared with patients with normal liver function.[L8863,L8869] Conversely, renal impairment has a negligible effect on total drug clearance as the renal route is a relatively minor clearance pathway for anastrozole. In volunteers with severe renal impairment, renal clearance was reduced by 50% while total clearance was only reduced by approximately 10%.[L8863,L8869]

Absorpsi

Anastrozole is rapidly absorbed and Tmax is typically reached within 2 hours of dosing under fasted conditions.A186877,L8869 Coadministration with food reduces the rate but not the overall extent of absorption - mean Cmax decreased by 16% and the median Tmax was extended to 5 hours when anastrozole was administered 30 minutes after ingestion of food,L8863 though this relatively minor alteration in absorption kinetics is not expected to result in clinically significant effects.L8866

Metabolisme

Anastrozole is primarily metabolized in the liver via oxidation and glucuronidation to a number of inactive metabolites, including hydroxyanastrozole (both free and glucuronidated) and anastrozole glucuronide.A184457,L8863,L8869 Oxidation to hydroxyanastrozole is catalyzed predominantly by CYP3A4 (as well as CYP3A5 and CYP2C8, to a lesser extent) and the direct glucuronidation of anastrozole appears to be catalyzed mainly by UGT1A4.A184457 Anastrozole may also undergo N-dealkylation to form triazole and 3,5-Bis-(2-methylpropiononitrile)-benzoic acid.A184457 Labels for anastrozole state the main metabolite found in plasma following administration is triazole,L8863,L8869 but a recent pharmacokinetic study was unable to detect any products of N-dealkylation in vitro.A184457

Rute Eliminasi

Hepatic metabolism accounts for approximately 85% of anastrozole elimination.L8863 Approximately 10% of the administered dosage is eliminated unchanged in the urine.L8869,L8872

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food reduces the rate, but not the overall extent, of absorption.

Interaksi Obat

332 Data
Mifepristone The serum concentration of Anastrozole can be increased when it is combined with Mifepristone.
Tamoxifen The serum concentration of Anastrozole can be decreased when it is combined with Tamoxifen.
Methadone The serum concentration of Methadone can be increased when it is combined with Anastrozole.
Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Anastrozole.
Deslanoside Deslanoside may decrease the cardiotoxic activities of Anastrozole.
Ouabain Ouabain may decrease the cardiotoxic activities of Anastrozole.
Oleandrin Oleandrin may decrease the cardiotoxic activities of Anastrozole.
Cymarin Cymarin may decrease the cardiotoxic activities of Anastrozole.
Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Anastrozole.
Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Anastrozole.
Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Anastrozole.
Gitoformate Gitoformate may decrease the cardiotoxic activities of Anastrozole.
Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Anastrozole.
Peruvoside Peruvoside may decrease the cardiotoxic activities of Anastrozole.
Digoxin Digoxin may decrease the cardiotoxic activities of Anastrozole.
Digitoxin Digitoxin may decrease the cardiotoxic activities of Anastrozole.
Secobarbital The metabolism of Anastrozole can be increased when combined with Secobarbital.
Rifampin The metabolism of Anastrozole can be increased when combined with Rifampicin.
Bexarotene The metabolism of Anastrozole can be decreased when combined with Bexarotene.
Levothyroxine The metabolism of Anastrozole can be decreased when combined with Levothyroxine.
Loratadine The metabolism of Anastrozole can be decreased when combined with Loratadine.
Medroxyprogesterone acetate The metabolism of Anastrozole can be decreased when combined with Medroxyprogesterone acetate.
Nicardipine The metabolism of Anastrozole can be decreased when combined with Nicardipine.
Efavirenz The metabolism of Anastrozole can be decreased when combined with Efavirenz.
Ketoconazole The metabolism of Anastrozole can be decreased when combined with Ketoconazole.
Oxybutynin The metabolism of Anastrozole can be decreased when combined with Oxybutynin.
Topiroxostat The metabolism of Anastrozole can be decreased when combined with Topiroxostat.
Abiraterone The metabolism of Anastrozole can be decreased when combined with Abiraterone.
Teriflunomide The metabolism of Anastrozole can be decreased when combined with Teriflunomide.
Diltiazem The metabolism of Anastrozole can be decreased when combined with Diltiazem.
Quinine The metabolism of Anastrozole can be decreased when combined with Quinine.
Saquinavir The metabolism of Anastrozole can be decreased when combined with Saquinavir.
Genistein The metabolism of Anastrozole can be decreased when combined with Genistein.
Trimethoprim The metabolism of Anastrozole can be decreased when combined with Trimethoprim.
Candesartan cilexetil The metabolism of Anastrozole can be decreased when combined with Candesartan cilexetil.
Felodipine The metabolism of Anastrozole can be decreased when combined with Felodipine.
Clopidogrel The metabolism of Anastrozole can be decreased when combined with Clopidogrel.
Ritonavir The metabolism of Anastrozole can be decreased when combined with Ritonavir.
Fluticasone propionate The metabolism of Anastrozole can be decreased when combined with Fluticasone propionate.
Salmeterol The metabolism of Anastrozole can be decreased when combined with Salmeterol.
Gemfibrozil The metabolism of Anastrozole can be decreased when combined with Gemfibrozil.
Fluticasone The metabolism of Anastrozole can be decreased when combined with Fluticasone.
Mometasone furoate The metabolism of Anastrozole can be decreased when combined with Mometasone furoate.
Peginterferon alfa-2a The risk or severity of cardiotoxicity can be increased when Peginterferon alfa-2a is combined with Anastrozole.
Trastuzumab The risk or severity of cardiotoxicity can be increased when Trastuzumab is combined with Anastrozole.
Bevacizumab The risk or severity of cardiotoxicity can be increased when Bevacizumab is combined with Anastrozole.
Bortezomib The risk or severity of cardiotoxicity can be increased when Bortezomib is combined with Anastrozole.
Cladribine The risk or severity of cardiotoxicity can be increased when Cladribine is combined with Anastrozole.
Carmustine The risk or severity of cardiotoxicity can be increased when Carmustine is combined with Anastrozole.
Amsacrine The risk or severity of cardiotoxicity can be increased when Amsacrine is combined with Anastrozole.
Bleomycin The risk or severity of cardiotoxicity can be increased when Bleomycin is combined with Anastrozole.
Mitomycin The risk or severity of cardiotoxicity can be increased when Mitomycin is combined with Anastrozole.
Vindesine The risk or severity of cardiotoxicity can be increased when Vindesine is combined with Anastrozole.
Vinorelbine The risk or severity of cardiotoxicity can be increased when Vinorelbine is combined with Anastrozole.
Teniposide The risk or severity of cardiotoxicity can be increased when Teniposide is combined with Anastrozole.
Epirubicin The risk or severity of cardiotoxicity can be increased when Epirubicin is combined with Anastrozole.
Cisplatin The risk or severity of cardiotoxicity can be increased when Cisplatin is combined with Anastrozole.
Cyclophosphamide The risk or severity of cardiotoxicity can be increased when Cyclophosphamide is combined with Anastrozole.
Vincristine The risk or severity of cardiotoxicity can be increased when Vincristine is combined with Anastrozole.
Pentostatin The risk or severity of cardiotoxicity can be increased when Pentostatin is combined with Anastrozole.
Methotrexate The risk or severity of cardiotoxicity can be increased when Methotrexate is combined with Anastrozole.
Vinblastine The risk or severity of cardiotoxicity can be increased when Vinblastine is combined with Anastrozole.
Imatinib The risk or severity of cardiotoxicity can be increased when Imatinib is combined with Anastrozole.
Daunorubicin The risk or severity of cardiotoxicity can be increased when Daunorubicin is combined with Anastrozole.
Tretinoin The risk or severity of cardiotoxicity can be increased when Tretinoin is combined with Anastrozole.
Etoposide The risk or severity of cardiotoxicity can be increased when Etoposide is combined with Anastrozole.
Mechlorethamine The risk or severity of cardiotoxicity can be increased when Mechlorethamine is combined with Anastrozole.
Doxorubicin The risk or severity of cardiotoxicity can be increased when Doxorubicin is combined with Anastrozole.
Thalidomide The risk or severity of cardiotoxicity can be increased when Thalidomide is combined with Anastrozole.
Fludarabine The risk or severity of cardiotoxicity can be increased when Fludarabine is combined with Anastrozole.
Capecitabine The risk or severity of cardiotoxicity can be increased when Capecitabine is combined with Anastrozole.
Arsenic trioxide The risk or severity of cardiotoxicity can be increased when Arsenic trioxide is combined with Anastrozole.
Idarubicin The risk or severity of cardiotoxicity can be increased when Idarubicin is combined with Anastrozole.
Ifosfamide The risk or severity of cardiotoxicity can be increased when Ifosfamide is combined with Anastrozole.
Mitoxantrone The risk or severity of cardiotoxicity can be increased when Mitoxantrone is combined with Anastrozole.
Docetaxel The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Docetaxel.
Aldoxorubicin The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Aldoxorubicin.
Paclitaxel trevatide The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Paclitaxel trevatide.
Paclitaxel poliglumex The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Paclitaxel poliglumex.
Busulfan The risk or severity of cardiotoxicity can be increased when Busulfan is combined with Anastrozole.
Pertuzumab The risk or severity of cardiotoxicity can be increased when Anastrozole is combined with Pertuzumab.
Cabozantinib The metabolism of Anastrozole can be decreased when combined with Cabozantinib.
Rofecoxib The metabolism of Anastrozole can be decreased when combined with Rofecoxib.
Pyrimethamine The metabolism of Anastrozole can be decreased when combined with Pyrimethamine.
Ticlopidine The metabolism of Anastrozole can be decreased when combined with Ticlopidine.
Ketoprofen The metabolism of Anastrozole can be decreased when combined with Ketoprofen.
Cimetidine The metabolism of Anastrozole can be decreased when combined with Cimetidine.
Quinidine The metabolism of Anastrozole can be decreased when combined with Quinidine.
Fenofibrate The metabolism of Anastrozole can be decreased when combined with Fenofibrate.
Atazanavir The metabolism of Anastrozole can be decreased when combined with Atazanavir.
Tegaserod The metabolism of Anastrozole can be decreased when combined with Tegaserod.
Candesartan The metabolism of Anastrozole can be decreased when combined with Candesartan.
Triclabendazole The metabolism of Anastrozole can be decreased when combined with Triclabendazole.
Bezafibrate The metabolism of Anastrozole can be decreased when combined with Bezafibrate.
Cerivastatin The metabolism of Anastrozole can be decreased when combined with Cerivastatin.
Raloxifene The metabolism of Anastrozole can be decreased when combined with Raloxifene.
Nilutamide The metabolism of Anastrozole can be decreased when combined with Nilutamide.
Deferasirox The metabolism of Anastrozole can be decreased when combined with Deferasirox.
Nilvadipine The metabolism of Anastrozole can be decreased when combined with Nilvadipine.
Sulfaphenazole The metabolism of Anastrozole can be decreased when combined with Sulfaphenazole.

Target Protein

Aromatase CYP19A1

Referensi & Sumber

Synthesis reference: Anil Khile, Narendra Joshi, Shekhar Bhirud, "Process for the preparation of anastrozole and intermediates thereof." U.S. Patent US20060189670, issued August 24, 2006.
Artikel (PubMed)
  • PMID: 21175441
    Kamdem LK, Liu Y, Stearns V, Kadlubar SA, Ramirez J, Jeter S, Shahverdi K, Ward BA, Ogburn E, Ratain MJ, Flockhart DA, Desta Z: In vitro and in vivo oxidative metabolism and glucuronidation of anastrozole. Br J Clin Pharmacol. 2010 Dec;70(6):854-69. doi: 10.1111/j.1365-2125.2010.03791.x.
  • PMID: 23712697
    Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y: Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system. J Pharm Sci. 2013 Sep;102(9):3309-19. doi: 10.1002/jps.23600. Epub 2013 May 27.
  • PMID: 27747906
    Gervasini G, Jara C, Olier C, Romero N, Martinez R, Carrillo JA: Polymorphisms in ABCB1 and CYP19A1 genes affect anastrozole plasma concentrations and clinical outcomes in postmenopausal breast cancer patients. Br J Clin Pharmacol. 2017 Mar;83(3):562-571. doi: 10.1111/bcp.13130. Epub 2016 Oct 18.
  • PMID: 12404296
    Buzdar AU, Robertson JF, Eiermann W, Nabholtz JM: An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. 2002 Nov 1;95(9):2006-16. doi: 10.1002/cncr.10908.
  • PMID: 28614542
    Barros-Oliveira MDC, Costa-Silva DR, Andrade DB, Borges US, Tavares CB, Borges RS, Silva JM, Silva BBD: Use of anastrozole in the chemoprevention and treatment of breast cancer: A literature review. Rev Assoc Med Bras (1992). 2017 Apr;63(4):371-378. doi: 10.1590/1806-9282.63.04.371.
  • PMID: 9152599
    Grimm SW, Dyroff MC: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos. 1997 May;25(5):598-602.
  • PMID: 20923259
    Kelly CM, Buzdar AU: Anastrozole. Expert Opin Drug Saf. 2010 Nov;9(6):995-1003. doi: 10.1517/14740338.2010.515977.
  • PMID: 21087898
    Cuzick J, Sestak I, Baum M, Buzdar A, Howell A, Dowsett M, Forbes JF: Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial. Lancet Oncol. 2010 Dec;11(12):1135-41. doi: 10.1016/S1470-2045(10)70257-6. Epub 2010 Nov 17.
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Contoh Produk & Brand

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International Brands
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