Peringatan Keamanan

IC50 of 0.63 nM.

Everolimus

DB01590

small molecule approved

Deskripsi

Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein.

Struktur Molekul 2D

Berat 958.24
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) ~30 hours.
Volume Distribusi The blood-to-plasma ratio of everolimus is 17% to 73%.
Klirens (Clearance) Following a 3 mg radiolabeled dose of everolimus, 80% of the radioactivity was recovered from the feces, while 5% was excreted in the urine.

Absorpsi

In patients with advanced solid tumors, peak everolimus concentrations are reached 1 to 2 hours after administration of oral doses ranging from 5 mg to 70 mg. Following single doses, Cmax is dose-proportional between 5 mg and 10 mg. At doses of 20 mg and higher, the increase in Cmax is less than dose-proportional, however AUC shows dose-proportionality over the 5 mg to 70 mg dose range. Steady-state was achieved within 2 weeks following once-daily dosing. Dose Proportionality in Patients with SEGA (subependymal giant-cell astrocytomas) and TSC (tuberous sclerosis complex): In patients with SEGA and TSC, everolimus Cmin was approximately dose-proportional within the dose range from 1.35 mg/m2 to 14.4 mg/m2.

Metabolisme

Everolimus is a substrate of CYP3A4 and PgP (phosphoglycolate phosphatase). Three monohydroxylated metabolites, two hydrolytic ring-opened products, and a phosphatidylcholine conjugate of everolimus were the 6 primary metabolites detected in human blood. In vitro, everolimus competitively inhibited the metabolism of CYP3A4 and was a mixed inhibitor of the CYP2D6 substrate dextromethorphan.

Rute Eliminasi

After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was recovered from the feces and only a minor amount (5%) was excreted in urine.

Interaksi Makanan

5 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the metabolism of everolimus through the CYP3A4 pathway and, therefore, may increase serum levels of everolimus.
  • 2. Avoid St. John's Wort. Coadministration of St. John's Wort with everolimus may reduce serum levels of everolimus by inducing CYP3A4 and P-glycoprotein (PGP).
  • 3. Take at the same time every day.
  • 4. Take with a full glass of water.
  • 5. Take with or without food. Take consistently with regard to food as food may reduce the AUC and Cmax of everolimus.

Interaksi Obat

1373 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Everolimus.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Everolimus.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Everolimus.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Everolimus.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Everolimus.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Everolimus.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Everolimus.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Everolimus.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Everolimus.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Everolimus.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Everolimus.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Everolimus.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Everolimus.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Everolimus.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Everolimus.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Everolimus.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Everolimus.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Everolimus.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Everolimus.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Everolimus.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Everolimus.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Everolimus.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Everolimus.
Cladribine Everolimus may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Everolimus.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Everolimus.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Everolimus.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Everolimus.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Everolimus.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Everolimus.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Everolimus.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Everolimus.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Everolimus.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Everolimus.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Everolimus.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Everolimus.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Everolimus.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Everolimus.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Everolimus.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Everolimus.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Everolimus.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Everolimus.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Everolimus.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Everolimus.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Everolimus.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Everolimus.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Everolimus.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Everolimus.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Everolimus.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Everolimus.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Everolimus.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Everolimus.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Everolimus.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Everolimus.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Everolimus.
Thalidomide The metabolism of Everolimus can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Everolimus.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Everolimus.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Everolimus.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Everolimus.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Everolimus.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Everolimus.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Everolimus.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Everolimus.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Everolimus.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Everolimus.
Castanospermine The risk or severity of adverse effects can be increased when Everolimus is combined with Castanospermine.
Vorinostat The risk or severity of adverse effects can be increased when Everolimus is combined with Vorinostat.
2-Methoxyethanol The risk or severity of adverse effects can be increased when Everolimus is combined with 2-Methoxyethanol.
Brequinar The risk or severity of adverse effects can be increased when Everolimus is combined with Brequinar.
Pirfenidone The risk or severity of adverse effects can be increased when Everolimus is combined with Pirfenidone.
Belinostat The risk or severity of adverse effects can be increased when Everolimus is combined with Belinostat.
Interferon alfa The risk or severity of adverse effects can be increased when Everolimus is combined with Interferon alfa.
Glatiramer The risk or severity of adverse effects can be increased when Everolimus is combined with Glatiramer.
Briakinumab The risk or severity of adverse effects can be increased when Everolimus is combined with Briakinumab.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Everolimus is combined with Human interferon omega-1.
Mepolizumab The risk or severity of adverse effects can be increased when Everolimus is combined with Mepolizumab.
Abetimus The risk or severity of adverse effects can be increased when Everolimus is combined with Abetimus.
Belatacept The risk or severity of adverse effects can be increased when Everolimus is combined with Belatacept.
Pralatrexate The risk or severity of adverse effects can be increased when Everolimus is combined with Pralatrexate.
Wortmannin The risk or severity of adverse effects can be increased when Everolimus is combined with Wortmannin.
Eribulin The risk or severity of adverse effects can be increased when Everolimus is combined with Eribulin.
Belimumab The risk or severity of adverse effects can be increased when Everolimus is combined with Belimumab.
Teriflunomide The risk or severity of adverse effects can be increased when Everolimus is combined with Teriflunomide.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Everolimus is combined with Dimethyl fumarate.
Obinutuzumab The risk or severity of adverse effects can be increased when Everolimus is combined with Obinutuzumab.
Vedolizumab The risk or severity of adverse effects can be increased when Everolimus is combined with Vedolizumab.
Blinatumomab The risk or severity of adverse effects can be increased when Everolimus is combined with Blinatumomab.
Dinutuximab The risk or severity of adverse effects can be increased when Everolimus is combined with Dinutuximab.
Tixocortol The risk or severity of adverse effects can be increased when Everolimus is combined with Tixocortol.
Peginterferon beta-1a The risk or severity of adverse effects can be increased when Everolimus is combined with Peginterferon beta-1a.
Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Everolimus is combined with Antilymphocyte immunoglobulin (horse).
Tepoxalin The risk or severity of adverse effects can be increased when Everolimus is combined with Tepoxalin.
Ixekizumab The risk or severity of adverse effects can be increased when Everolimus is combined with Ixekizumab.
Ravulizumab The risk or severity of adverse effects can be increased when Everolimus is combined with Ravulizumab.
Pirarubicin The risk or severity of adverse effects can be increased when Everolimus is combined with Pirarubicin.
Peficitinib The risk or severity of adverse effects can be increased when Everolimus is combined with Peficitinib.
Brodalumab The risk or severity of adverse effects can be increased when Everolimus is combined with Brodalumab.
Sirukumab The risk or severity of adverse effects can be increased when Everolimus is combined with Sirukumab.
Guselkumab The risk or severity of adverse effects can be increased when Everolimus is combined with Guselkumab.

Target Protein

Serine/threonine-protein kinase mTOR MTOR

Referensi & Sumber

Synthesis reference: EMA Report(http://www.ema.europa.eu/docs/enGB/documentlibrary/EPAR-Publicassessmentreport/human/001038/WC500022817.pdf)
Artikel (PubMed)
  • PMID: 11384247
    Kuhn B, Jacobsen W, Christians U, Benet LZ, Kollman PA: Metabolism of sirolimus and its derivative everolimus by cytochrome P450 3A4: insights from docking, molecular dynamics, and quantum chemical calculations. J Med Chem. 2001 Jun 7;44(12):2027-34.
  • PMID: 21047224
    Krueger DA, Care MM, Holland K, Agricola K, Tudor C, Mangeshkar P, Wilson KA, Byars A, Sahmoud T, Franz DN: Everolimus for subependymal giant-cell astrocytomas in tuberous sclerosis. N Engl J Med. 2010 Nov 4;363(19):1801-11. doi: 10.1056/NEJMoa1001671.
  • PMID: 22899246
    den Burger JC, Wilhelm AJ, Chahbouni A, Vos RM, Sinjewel A, Swart EL: Analysis of cyclosporin A, tacrolimus, sirolimus, and everolimus in dried blood spot samples using liquid chromatography tandem mass spectrometry. Anal Bioanal Chem. 2012 Oct;404(6-7):1803-11. doi: 10.1007/s00216-012-6317-8. Epub 2012 Aug 17.
  • PMID: 23455452
    Pawaskar DK, Straubinger RM, Fetterly GJ, Hylander BH, Repasky EA, Ma WW, Jusko WJ: Synergistic interactions between sorafenib and everolimus in pancreatic cancer xenografts in mice. Cancer Chemother Pharmacol. 2013 May;71(5):1231-40. doi: 10.1007/s00280-013-2117-x. Epub 2013 Mar 3.

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