Peringatan Keamanan

Temsirolimus has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m2. The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of temsirolimus greater than 25 mg.

Temsirolimus

DB06287

small molecule approved

Deskripsi

Temsirolimus is a derivative of sirolimus used in the treatment of renal cell carcinoma (RCC). It was developed by Wyeth Pharmaceuticals under the trade name Torisel. Temsirolimus was approved by the FDA in late May 2007 as well as the European Medicines Agency (EMEA) on November 2007.

Struktur Molekul 2D

Berat 1030.2871
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Temsirolimus exhibits a bi-exponential decline in whole blood concentrations and the mean half-lives of temsirolimus and sirolimus were 17.3 hr and 54.6 hr, respectively.
Volume Distribusi 172 L in whole blood of cancer patients; both temsirolimus and sirolimus are extensive distributed partitioned into formed blood elements
Klirens (Clearance) 16.2 L/h (22%)

Absorpsi

Infused intravenous over 30 - 60 minutes. Cmax is typically observed at the end of infusion

Metabolisme

Primarily metabolized by cytochrome P450 3A4 in the human liver. Sirolimus, an equally potent metabolite, is the primary metabolite in humans following IV infusion. Other metabolic pathways observed in in vitro temsirolimus metabolism studies include hydroxylation, reduction and demethylation.

Rute Eliminasi

Excreted predominantly in feces (76%), 4.6% of drug and metabolites recovered in urine. 17% of drug was not recovered by either route following a 14-day sample collection.

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of temsirolimus, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of temsirolimus and may reduce its serum concentration.

Interaksi Obat

1397 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Temsirolimus.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Temsirolimus.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Temsirolimus.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Temsirolimus.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Temsirolimus.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Temsirolimus.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Temsirolimus.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Temsirolimus.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Temsirolimus.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Temsirolimus.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Temsirolimus.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Temsirolimus.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Temsirolimus.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Temsirolimus.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Temsirolimus.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Temsirolimus.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Temsirolimus.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Temsirolimus.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Temsirolimus.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Temsirolimus.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Temsirolimus.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Temsirolimus.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Temsirolimus.
Cladribine Temsirolimus may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Temsirolimus.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Temsirolimus.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Temsirolimus.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Temsirolimus.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Temsirolimus.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Temsirolimus.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Temsirolimus.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Temsirolimus.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Temsirolimus.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Temsirolimus.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Temsirolimus.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Temsirolimus.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Temsirolimus.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Temsirolimus.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Temsirolimus.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Temsirolimus.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Temsirolimus.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Temsirolimus.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Temsirolimus.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Temsirolimus.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Temsirolimus.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Temsirolimus.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Temsirolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Temsirolimus.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Temsirolimus.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Temsirolimus.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Temsirolimus.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Temsirolimus.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Temsirolimus.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Temsirolimus.
Thalidomide The metabolism of Temsirolimus can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Temsirolimus.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Temsirolimus.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Temsirolimus.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Temsirolimus.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Temsirolimus.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Temsirolimus.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Temsirolimus.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Temsirolimus.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Temsirolimus.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Temsirolimus.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Temsirolimus.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Temsirolimus.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Temsirolimus.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Temsirolimus.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Temsirolimus.
Belinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Temsirolimus.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Temsirolimus.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Temsirolimus.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Temsirolimus.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Temsirolimus.
Mepolizumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Temsirolimus is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Temsirolimus is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Temsirolimus is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Temsirolimus is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Temsirolimus is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Temsirolimus is combined with Teriflunomide.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Temsirolimus is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Temsirolimus is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Temsirolimus is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Temsirolimus is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Temsirolimus is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Temsirolimus is combined with Pirarubicin.
Peficitinib The risk or severity of adverse effects can be increased when Temsirolimus is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Temsirolimus is combined with Guselkumab.
Triptolide The risk or severity of adverse effects can be increased when Temsirolimus is combined with Triptolide.

Target Protein

Serine/threonine-protein kinase mTOR MTOR

Referensi & Sumber

Synthesis reference: Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee, "Process for preparation of temsirolimus." U.S. Patent US20100249415, issued September 30, 2010.
Artikel (PubMed)
  • PMID: 17913896
    Boni J, Leister C, Burns J, Cincotta M, Hug B, Moore L: Pharmacokinetic profile of temsirolimus with concomitant administration of cytochrome p450-inducing medications. J Clin Pharmacol. 2007 Nov;47(11):1430-9. Epub 2007 Oct 3.

Contoh Produk & Brand

Produk: 8 • International brands: 0
Produk
  • Gd-temsirolimus
    Solution • 25 mg / mL • Intravenous • Canada • Generic • Approved
  • Temsirolimus
    Injection, solution, concentrate; Kit • 25 mg/1mL • Intravenous • US • Generic • Approved
  • Temsirolimus
    Injection, solution, concentrate; Kit • 25 mg/1mL • Intravenous • US • Generic • Approved
  • Temsirolimus
    Injection, solution, concentrate; Kit • 25 mg/1mL • Intravenous • US • Generic • Approved
  • Temsirolimus
    Kit • 25 mg/1mL • Intravenous • US • Generic • Approved
  • Torisel
    Injection, solution, concentrate; Kit • 25 mg/1mL • Intravenous • US • Approved
  • Torisel
    Solution • 25 mg / mL • Intravenous • Canada • Approved
  • Torisel
    Injection, solution, concentrate • 30 mg • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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