Peringatan Keamanan

The oral LD50 in rats is approximately 240-300 mg/kg.L41110

There is limited information regarding the overdose of olaparib.

Olaparib

DB09074

small molecule approved

Deskripsi

Olaparib is a selective and potent inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, PARP1 and PARP2.L41100, L40908, L43792 PARP inhibitors represent a novel class of anti-cancer therapy and they work by taking advantage of a defect in DNA repair in cancer cells with BRCA mutations and inducing cell death.A246015

Olaparib is used to treat a number of BRCA-associated tumours, including ovarian cancer, breast cancer, pancreatic cancer, and prostate cancer.L41100, L40908, L43792 It was first approved by the FDA and EU in December 2014,A246020 and by Health Canada in April 2016.L42820

Struktur Molekul 2D

Berat 434.4628
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following a single oral dose in patients with cancer, the mean terminal half-life was 6.10 hours.[A246025]
Volume Distribusi The mean (± standard deviation) apparent volume of distribution of olaparib is 158 ± 136 L following a single 300 mg dose.[L41100]
Klirens (Clearance) Following a single oral dose in patients with cancer, the mean apparent plasma clearance was 4.55 L/h.[A246025]

Absorpsi

Following oral administration, olaparib is rapidly absorbed.A35290 After administration of a single 300 mg dose of olaparib, the mean (CV%) Cmax was 5.4 ?g/mL (32%) and AUC was 39.2 ?g x h/mL (44%). The steady state Cmax and AUC following a dose of 300 mg twice daily was 7.6 ?g/mL (35%) and 49.2 ?g x h/mL (44%), respectively. Tmax is 1.5 hours. A high-fat and high-calorie meal may delay Tmax, but does not significantly alter the extent of olaparib absorption.L41100

Metabolisme

Olaparib is metabolized by cytochrome P450 (CYP) 3A4/5 in vitro. Following an oral dose of radiolabeled olaparib to female patients, unchanged olaparib accounted for 70% of the circulating radioactivity in plasma. Olaparib undergoes oxidation reactions as well as subsequent glucuronide or sulfate conjugation.L41100 In humans, olaparib can also undergo hydrolysis, hydroxylation, and dehydrogenation.A246000 While up to 37 metabolites of olaparib were detected in plasma, urine, and feces, the majority of metabolites represent less than 1% of the total administered dose and they have not been fully characterized. The major circulating metabolites are a ring-opened piperazin-3-ol moiety and two mono-oxygenated metabolites. The pharmacodynamic activity of the metabolites is unknown.L5089

Rute Eliminasi

Following a single dose of radiolabeled olaparib, 86% of the dosed radioactivity was recovered within a seven-day collection period, mostly in the form of metabolites. About 44% of the drug was excreted via the urine and 42% of the dose was excreted via the feces. Following an oral dose of radiolabeled olaparib to female patients, the unchanged drug accounted for 15% and 6% of the radioactivity in urine and feces, respectively.L41100

Interaksi Makanan

3 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of olaparib, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of olaparib and may reduce its serum concentration.
  • 3. Take with or without food. Food does not significantly alter the extent of olaparib absorption.

Interaksi Obat

1008 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Olaparib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Olaparib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Olaparib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Olaparib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Olaparib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Olaparib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Olaparib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Olaparib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Olaparib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Olaparib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Olaparib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Olaparib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Olaparib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Olaparib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Olaparib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Olaparib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Olaparib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Olaparib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Olaparib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Olaparib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Olaparib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Olaparib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Olaparib.
Cladribine Olaparib may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Olaparib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Olaparib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Olaparib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Olaparib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Olaparib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Olaparib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Olaparib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Olaparib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Olaparib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Olaparib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Olaparib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Olaparib.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Olaparib.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Olaparib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Olaparib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Olaparib.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Olaparib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Olaparib.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Olaparib.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Olaparib.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Olaparib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Olaparib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Olaparib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Olaparib.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Olaparib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Olaparib.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Olaparib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Olaparib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Olaparib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Olaparib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Olaparib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Olaparib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Olaparib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Olaparib.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Olaparib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Olaparib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Olaparib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Olaparib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Olaparib.
Thalidomide The metabolism of Olaparib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Olaparib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Olaparib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Olaparib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Olaparib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Olaparib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Olaparib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Olaparib.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Olaparib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Olaparib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Olaparib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Olaparib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Olaparib.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Olaparib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Olaparib.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Olaparib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Olaparib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Olaparib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Olaparib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Olaparib.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Olaparib.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Olaparib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Olaparib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Olaparib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Olaparib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Olaparib.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Olaparib.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Olaparib.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Olaparib.
Bendamustine The risk or severity of adverse effects can be increased when Bendamustine is combined with Olaparib.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Olaparib.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Olaparib.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Olaparib.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Olaparib.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Olaparib.
Carfilzomib The risk or severity of adverse effects can be increased when Carfilzomib is combined with Olaparib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Olaparib.

Target Protein

Poly [ADP-ribose] polymerase 1 PARP1
Poly [ADP-ribose] polymerase 2 PARP2
Protein mono-ADP-ribosyltransferase PARP3 PARP3
Aldo-keto reductase family 1 member C3 AKR1C3

Referensi & Sumber

Synthesis reference: Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S, Javaid H, Kerrigan F, Knights C, Lau A, Loh VM Jr, Matthews IT, Moore S, O'Connor MJ, Smith GC, Martin NM: 4-3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl-2H-phthalazin- 1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91. doi: 10.1021/jm8001263. Epub 2008 Sep 19. Pubmed(http://www.ncbi.nlm.nih.gov/pubmed/18800822)
Artikel (PubMed)
  • PMID: 26405320
    Solimando DA Jr, Waddell JA: Nivolumab and Olaparib. Hosp Pharm. 2015 May;50(5):356-66. doi: 10.1310/hpj5005-356.
  • PMID: 30069770
    Bochum S, Berger S, Martens UM: Olaparib. Recent Results Cancer Res. 2018;211:217-233. doi: 10.1007/978-3-319-91442-8_15.
  • PMID: 31499579
    Wang L, Wang M: In vitro metabolism of olaparib in liver microsomes by liquid chromatography/electrospray ionization high-resolution mass spectrometry. Rapid Commun Mass Spectrom. 2020 Feb 15;34(3):e8575. doi: 10.1002/rcm.8575.
  • PMID: 31625002
    Sachdev E, Tabatabai R, Roy V, Rimel BJ, Mita MM: PARP Inhibition in Cancer: An Update on Clinical Development. Target Oncol. 2019 Dec;14(6):657-679. doi: 10.1007/s11523-019-00680-2.
  • PMID: 25616434
    Deeks ED: Olaparib: first global approval. Drugs. 2015 Feb;75(2):231-40. doi: 10.1007/s40265-015-0345-6.
  • PMID: 23619942
    Chen Y, Zhang L, Hao Q: Olaparib: a promising PARP inhibitor in ovarian cancer therapy. Arch Gynecol Obstet. 2013 Aug;288(2):367-74. doi: 10.1007/s00404-013-2856-2. Epub 2013 Apr 26.

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