Peringatan Keamanan

Rat (ipr) LD50=32530 µg/kg. Symptoms of overdose include bone marrow suppression, peripheral neurotoxicity, and mucositis. Overdoses in pediatric patients may be associated with acute ethanol toxicity.

Paclitaxel

DB01229

small molecule approved vet_approved

Deskripsi

Paclitaxel is a chemotherapeutic agent marketed under the brand name Taxol among others. Used as a treatment for various cancers, paclitaxel is a mitotic inhibitor that was first isolated in 1971 from the bark of the Pacific yew tree which contains endophytic fungi that synthesize paclitaxel. It is available as an intravenous solution for injection and the newer formulation contains albumin-bound paclitaxel marketed under the brand name Abraxane.

Struktur Molekul 2D

Berat 853.9061
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) When a 24 hour infusion of 135 mg/m^2 is given to ovarian cancer patients, the elimination half=life is 52.7 hours.
Volume Distribusi * 227 to 688 L/m^2 [apparent volume of distribution at steady-state, 24 hour infusion]
Klirens (Clearance) * 21.7 L/h/m2 [Dose 135 mg/m2, infusion duration 24 h] * 23.8 L/h/m2 [Dose 175 mg/m2, infusion duration 24 h] * 7 L/h/m2 [Dose 135 mg/m2, infusion duration 3 h] * 12.2 L/h/m2 [Dose 175 mg/m2, infusion duration 3 h]

Absorpsi

When a 24 hour infusion of 135 mg/m^2 is given to ovarian cancer patients, the maximum plasma concentration (Cmax) is 195 ng/mL, while the AUC is 6300 ng•h/mL.

Metabolisme

Hepatic. In vitro studies with human liver microsomes and tissue slices showed that paclitaxel was metabolized primarily to 6a-hydrox-ypaclitaxel by the cytochrome P450 isozyme CYP2C8; and to two minor metabolites, 3’-p-hydroxypaclitaxel and 6a, 3’-p-dihydroxypaclitaxel, by CYP3A4.

Rute Eliminasi

In 5 patients administered a 225 or 250 mg/m2 dose of radiolabeled paclitaxel as a 3-hour infusion, a mean of 71% of the radioactivity was excreted in the feces in 120 hours, and 14% was recovered in the urine.

Interaksi Makanan

3 Data
  • 1. Avoid echinacea. Co-administration may decrease the effectiveness of immunosuppressants, and echinacea may induce CYP3A4 increasing paclitaxel metabolism.
  • 2. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of paclitaxel.
  • 3. Exercise caution with St. John's Wort. This herb induces the CYP3A4 metabolism of paclitaxel and may reduce its serum concentration.

Interaksi Obat

1528 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Paclitaxel.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Paclitaxel.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Paclitaxel.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Paclitaxel.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Paclitaxel.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Paclitaxel.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Paclitaxel.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Paclitaxel.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Paclitaxel.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Paclitaxel.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Paclitaxel.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Paclitaxel.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Paclitaxel.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Paclitaxel.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Paclitaxel.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Paclitaxel.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Paclitaxel.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Paclitaxel.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Paclitaxel.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Paclitaxel.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Paclitaxel.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Paclitaxel.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Paclitaxel.
Cladribine Paclitaxel may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Paclitaxel.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Paclitaxel.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Paclitaxel.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Paclitaxel.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Paclitaxel.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Paclitaxel.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Paclitaxel.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Paclitaxel.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Paclitaxel.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Paclitaxel.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Paclitaxel.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Paclitaxel.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Paclitaxel.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Paclitaxel.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Paclitaxel.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Paclitaxel.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Paclitaxel.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Paclitaxel.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Paclitaxel.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Paclitaxel.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Paclitaxel.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Paclitaxel.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Paclitaxel.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Paclitaxel.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Paclitaxel.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Paclitaxel.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Paclitaxel.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Paclitaxel.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Paclitaxel.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Paclitaxel.
Thalidomide The risk or severity of peripheral neuropathy can be increased when Thalidomide is combined with Paclitaxel.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Paclitaxel.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Paclitaxel.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Paclitaxel.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Paclitaxel.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Paclitaxel.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Paclitaxel.
Eculizumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Eculizumab.
Decitabine The risk or severity of adverse effects can be increased when Paclitaxel is combined with Decitabine.
Nelarabine The risk or severity of adverse effects can be increased when Paclitaxel is combined with Nelarabine.
Stepronin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Stepronin.
Castanospermine The risk or severity of adverse effects can be increased when Paclitaxel is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Paclitaxel is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Paclitaxel is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Paclitaxel is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Paclitaxel is combined with Pirfenidone.
Interferon alfa The risk or severity of adverse effects can be increased when Paclitaxel is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Paclitaxel is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Paclitaxel is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Paclitaxel is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Paclitaxel is combined with Belatacept.
Bendamustine The risk or severity of adverse effects can be increased when Paclitaxel is combined with Bendamustine.
Pralatrexate The risk or severity of adverse effects can be increased when Paclitaxel is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Belimumab.
Carfilzomib The risk or severity of adverse effects can be increased when Paclitaxel is combined with Carfilzomib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Paclitaxel is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Paclitaxel is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Paclitaxel is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Paclitaxel is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Pirarubicin.
Voclosporin The risk or severity of adverse effects can be increased when Paclitaxel is combined with Voclosporin.
Peficitinib The risk or severity of adverse effects can be increased when Paclitaxel is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Paclitaxel is combined with Guselkumab.

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: Hendricus B. A. de Bont, Ruben G. G. Leenders, Johan W. Scheeren, Hidde J. Haisma, Dick de Vos, "Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy." U.S. Patent US5760072, issued September, 1989.
Artikel (PubMed)
  • PMID: 7850785
    Wall ME, Wani MC: Camptothecin and taxol: discovery to clinic--thirteenth Bruce F. Cain Memorial Award Lecture. Cancer Res. 1995 Feb 15;55(4):753-60.
  • PMID: 5553076
    Wani MC, Taylor HL, Wall ME, Coggon P, McPhail AT: Plant antitumor agents. VI. The isolation and structure of taxol, a novel antileukemic and antitumor agent from Taxus brevifolia. J Am Chem Soc. 1971 May 5;93(9):2325-7.
  • PMID: 688258
    Fuchs DA, Johnson RK: Cytologic evidence that taxol, an antineoplastic agent from Taxus brevifolia, acts as a mitotic spindle poison. Cancer Treat Rep. 1978 Aug;62(8):1219-22.
  • PMID: 7603142
    Saville MW, Lietzau J, Pluda JM, Feuerstein I, Odom J, Wilson WH, Humphrey RW, Feigal E, Steinberg SM, Broder S, et al.: Treatment of HIV-associated Kaposi's sarcoma with paclitaxel. Lancet. 1995 Jul 1;346(8966):26-8.
  • PMID: 15139776
    Authors unspecified: ABI 007. Drugs R D. 2004;5(3):155-9.
  • PMID: 20217610
    Gaitanis A, Staal S: Liposomal doxorubicin and nab-paclitaxel: nanoparticle cancer chemotherapy in current clinical use. Methods Mol Biol. 2010;624:385-92. doi: 10.1007/978-1-60761-609-2_26.

Contoh Produk & Brand

Produk: 96 • International brands: 2
Produk
  • Abraxane
    Injection, powder, lyophilized, for suspension • 100 mg/20mL • Intravenous • US • Approved
  • Abraxane
    Injection, powder, for suspension • 5 mg/ml • Intravenous • EU • Approved
  • Abraxane
    Injection, powder, for suspension • 5 mg/ml • Intravenous • EU • Approved
  • Abraxane for Injectable Suspension
    Powder, for suspension • 100 mg / vial • Intravenous • Canada • Approved
  • Aj-paclitaxel
    Solution • 6 mg / mL • Intravenous • Canada • Generic • Approved
  • Apealea
    Injection, powder, for solution • 60 mg • Intravenous • EU
  • Apo-paclitaxel Injectable
    Solution • 6 mg / mL • Intravenous • Canada • Generic • Approved
  • Naveruclif
    - • 5 mg/ml • Intravenous • EU • Approved
Menampilkan 8 dari 96 produk.
International Brands
  • NanoPac
  • Paxceed

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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