Peringatan Keamanan

There is no known antidote for an overdose of docetaxel injection. In case of overdose, patients should be closely monitored in specialized units. Some of the anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis. After an overdose is discovered, patients should receive granulocyte colony-stimulating factor (G-CSF) as soon as possible. Other appropriate symptomatic measures should be taken as needed.L46466

In two reports of overdose, one patient received 150 mg/m2, and the other received 200 mg/m2 as 1-hour infusions. Both patients experienced severe neutropenia, mild asthenia, cutaneous reactions, and mild paresthesia, and recovered without incident.L46466 In rats, the oral LD50 of docetaxel is >2000 mg/kg. The intravenous LD50 in mice is 138 mg/kg.L46471

Docetaxel

DB01248

small molecule approved investigational

Deskripsi

Docetaxel is a clinically well established anti-mitotic chemotherapy medication used for the treatment of different types of cancer, including breast, ovarian, and non-small cell lung cancer. Docetaxel is a complex diterpenoid molecule and a semisynthetic analogue of paclitaxel.A259676,L46466 Docetaxel reversibly binds to microtubulin with high affinity in a 1:1 stoichiometric ratio, allowing it to prevent cell division and promote to cell death.A259676 Compared to paclitaxel, docetaxel is two times more potent as an inhibitor of microtubule depolymerization. Docetaxel binds to microtubules but does not interact with dimeric tubulin.A259671

The use of docetaxel may lead to udesired outcomes such as hepatic impairment, hematologic effects, enterocolitis and neutropenic colitis, hypersensitivity reactions, fluid retention, second primary malignancies, embryo-fetal toxicity, and tumor lysis syndrome.L46466 Docetaxel was approved by the FDA in 1996 and is available in solution for injection for intravenous or parenteral administration.A259676

Struktur Molekul 2D

Berat 807.8792
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) With plasma sampling up to 8 to 22 days after docetaxel infusion, the terminal elimination half-life was 116 hours.[L46466] Doses between 70 and 115 mg/m<sup>2</sup> with infusion times of 1 to 2 hours produce a triphasic elimination profile. The half-life of the alpha, beta, and gamma phases are 4 minutes, 36 minutes, and 11.1 hours, respectively.[L46476]
Volume Distribusi Docetaxel has a steady-state volume of distribution of 113 L. Its pharmacokinetic profile is consistent with a three-compartment pharmacokinetic model.[L46466,L46476]
Klirens (Clearance) After the administration of 20–115 mg/m<sup>2</sup> of intravenous docetaxel to cancer patients, the total body clearance was 21 L/h/m<sup>2</sup>.[L46476] In patients aged 1 to 20 years with solid tumors that received 55 mg/m<sup>2</sup> to 235 mg/m<sup>2</sup> of docetaxel in a 1-hour intravenous infusion every 3 weeks, clearance was 17.3 L/h/m<sup>2</sup>.[L46466]

Absorpsi

The pharmacokinetic profile of docetaxel is consistent with a three-compartment model. The initial rapid decline represents the distribution to the peripheral compartments, and the late (terminal) phase is partly due to a relatively slow efflux of docetaxel from the peripheral compartment. The area under the curve (AUC) was dose proportional at doses between 70 mg/m2 and 115 mg/m2 with infusion times of 1 to 2 hours.L46466,L46476 In a group of patients with solid tumors given 100 mg/m2 of docetaxel intravenously, the Cmax and AUC were 2.41 ?g/mL and 5.93 ?g?h/mL, respectively.A259646,A259656

Metabolisme

Docetaxel undergoes hepatic metabolism. In vitro drug interaction studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme.L46466,L46476 CYP3A5 also plays a role in the metabolism of this drug.A259646 In humans, docetaxel is metabolized by CYP3A4/5 into four metabolites: M1, M2, M3 and M4. Docetaxel undergoes hydroxylation of the synthetic isobutoxy side chain, forming metabolite M2. The oxidation of M2 forms an unstable aldehyde that is immediately cyclised into the stereoisomers M1 and M3. M4 is then formed by the oxidation of M1/M3.A259651

Rute Eliminasi

Docetaxel was eliminated in urine and feces following oxidative metabolism of the tert-butyl ester group, but fecal excretion was the main elimination route. Within 7 days, urinary and fecal excretion accounted for approximately 6% and 75% of the administered radioactivity, respectively. In the first 48 hours, approximately 80% of the radioactivity recovered was excreted in feces. One major and three minor metabolites were excreted at this point, with less than 8% as the unchanged drug.L46466,L46476

Farmakogenomik

1 Varian
ABCC2 (rs12762549)

Patients with this polymorphism in ABCC2 are at a higher risk of experiencing drug-induced leukopenia and drug-induced neutropenia when treated with docetaxel.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum levels of docetaxel.
  • 2. Exercise caution with St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of docetaxel.

Interaksi Obat

1096 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Docetaxel.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Docetaxel.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Docetaxel.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Docetaxel.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Docetaxel.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Docetaxel.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Docetaxel.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Docetaxel.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Docetaxel.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Docetaxel.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Docetaxel.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Docetaxel.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Docetaxel.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Docetaxel.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Docetaxel.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Docetaxel.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Docetaxel.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Docetaxel.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Docetaxel.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Docetaxel.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Docetaxel.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Docetaxel.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Docetaxel.
Cladribine Docetaxel may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Docetaxel.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Docetaxel.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Docetaxel.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Docetaxel.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Docetaxel.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Docetaxel.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Docetaxel.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Docetaxel.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Docetaxel.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Docetaxel.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Docetaxel.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Docetaxel.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Docetaxel.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Docetaxel.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Docetaxel.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Docetaxel.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Docetaxel.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Docetaxel.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Docetaxel.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Docetaxel.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Docetaxel.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Docetaxel.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Docetaxel.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Docetaxel.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Docetaxel.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Docetaxel.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Docetaxel.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Docetaxel.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Docetaxel.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Docetaxel.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Docetaxel.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Docetaxel.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Docetaxel.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Docetaxel.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Docetaxel.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Docetaxel.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Docetaxel.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Docetaxel.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Docetaxel.
Thalidomide The risk or severity of peripheral neuropathy can be increased when Thalidomide is combined with Docetaxel.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Docetaxel.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Docetaxel.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Docetaxel.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Docetaxel.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Docetaxel.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Docetaxel.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Docetaxel.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Docetaxel.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Docetaxel.
Eculizumab The risk or severity of adverse effects can be increased when Docetaxel is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Docetaxel is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Docetaxel is combined with Nelarabine.
Ciclesonide The risk or severity of adverse effects can be increased when Docetaxel is combined with Ciclesonide.
Stepronin The risk or severity of adverse effects can be increased when Docetaxel is combined with Stepronin.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Docetaxel is combined with Hydroxychloroquine.
Castanospermine The risk or severity of adverse effects can be increased when Docetaxel is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Docetaxel is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Docetaxel is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Docetaxel is combined with Brequinar.
Aldosterone The risk or severity of adverse effects can be increased when Docetaxel is combined with Aldosterone.
Pirfenidone The risk or severity of adverse effects can be increased when Docetaxel is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Docetaxel is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Docetaxel is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Docetaxel is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Docetaxel is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Docetaxel is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Docetaxel is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Docetaxel is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Docetaxel is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Docetaxel is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Docetaxel is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Docetaxel is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Docetaxel is combined with Belimumab.
Teriflunomide The risk or severity of liver damage can be increased when Docetaxel is combined with Teriflunomide.
Carfilzomib The risk or severity of adverse effects can be increased when Docetaxel is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Docetaxel is combined with Dimethyl fumarate.

Target Protein

Tubulin beta-1 chain TUBB1
Apoptosis regulator Bcl-2 BCL2
Nuclear receptor subfamily 1 group I member 2 NR1I2

Referensi & Sumber

Synthesis reference: Nicholas J. Sisti, Charles S. Swindell, "Method for docetaxel synthesis." U.S. Patent US5688977, issued September, 1991.
Artikel (PubMed)
  • PMID: 25728850
    Kenmotsu H, Tanigawara Y: Pharmacokinetics, dynamics and toxicity of docetaxel: Why the Japanese dose differs from the Western dose. Cancer Sci. 2015 May;106(5):497-504. doi: 10.1111/cas.12647. Epub 2015 Mar 25.
  • PMID: 23939959
    Hendrikx JJ, Dubbelman AC, Rosing H, Schinkel AH, Schellens JH, Beijnen JH: Quantification of docetaxel and its metabolites in human plasma by liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2013 Sep 15;27(17):1925-34. doi: 10.1002/rcm.6654.
  • PMID: 8094996
    Extra JM, Rousseau F, Bruno R, Clavel M, Le Bail N, Marty M: Phase I and pharmacokinetic study of Taxotere (RP 56976; NSC 628503) given as a short intravenous infusion. Cancer Res. 1993 Mar 1;53(5):1037-42.
  • PMID: 11685722
    Pienta KJ: Preclinical mechanisms of action of docetaxel and docetaxel combinations in prostate cancer. Semin Oncol. 2001 Aug;28(4 Suppl 15):3-7. doi: 10.1016/s0093-7754(01)90148-4.
  • PMID: 7670132
    Bissery MC, Nohynek G, Sanderink GJ, Lavelle F: Docetaxel (Taxotere): a review of preclinical and clinical experience. Part I: Preclinical experience. Anticancer Drugs. 1995 Jun;6(3):339-55, 363-8. doi: 10.1097/00001813-199506000-00001.
  • PMID: 31644206
    Authors unspecified: Docetaxel. .

Contoh Produk & Brand

Produk: 153 • International brands: 0
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