Imetelstat

DB14909

small molecule approved investigational

Deskripsi

Imetelstat is a first-in-class 18-amino acid oligonucleotide that directly and competitively inhibits human telomerase.A263973 It is used to treat anemia in patients with myelodysplastic syndromes (MDS), a group of hematologic disorders characterized by ineffective hematopoiesis, peripheral cytopenia, abnormal marrow cell morphology and a risk for transformation to acute myeloid leukemia.A187838 Standard therapy for anemia in patients with MDS involves the use of erythropoiesis-stimulating agents (e.g. erythropoietin), but primary resistance to these agents is frequent - the median response duration is 18 to 24 months, with most responders (70%) relapsing due to loss of sensitivity of erythroid progenitors to ESAs.A187838

Imetelstat received FDA approval in June 2024 for use in certain patients with MDS who have transfusion-dependent anemia and are unable to use ESAs.L50883,L50888

Struktur Molekul 2D

Berat 4610.18
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The geometric mean apparent plasma half-life of imetelstat is approximately 4.9 hours when given at the approved recommended dosage.[L50883]
Volume Distribusi The geometric mean volume of distribution of imetelstat following a single intravenous dose of 7.1 mg/kg administered over 2 hours in patients with myelodysplastic syndromes is approximately 14.1 liters.[L50883]
Klirens (Clearance) -

Absorpsi

Imetelstat is effectively 100% bioavailable given its intravenous administration. The geometric mean maximum plasma concentration (Cmax) is 18.3 µM and the AUC from 0 to 28 days (AUC0-28 is 114.2 h*µM.L50883 It does not accumulate between treatment cycles.

Metabolisme

Imetelstat is likely metabolized by non-specific nucleases to smaller nucleotides.L50883

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

106 Data
Darbepoetin alfa The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Imetelstat.
Erythropoietin The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Imetelstat.
Peginesatide The risk or severity of Thrombosis can be increased when Peginesatide is combined with Imetelstat.
Methoxy polyethylene glycol-epoetin beta The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Imetelstat.
Lidocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Lidocaine.
Ropivacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Ropivacaine.
Bupivacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Bupivacaine.
Cinchocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Cinchocaine.
Dyclonine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Dyclonine.
Procaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Procaine.
Prilocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Prilocaine.
Proparacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Proparacaine.
Meloxicam The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Meloxicam.
Oxybuprocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Oxybuprocaine.
Cocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Cocaine.
Mepivacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Mepivacaine.
Levobupivacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Levobupivacaine.
Diphenhydramine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Diphenhydramine.
Benzocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Benzocaine.
Chloroprocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Chloroprocaine.
Phenol The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Phenol.
Tetrodotoxin The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Tetrodotoxin.
Ambroxol The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Ambroxol.
Benzyl alcohol The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Benzyl alcohol.
Capsaicin The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Capsaicin.
Etidocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Etidocaine.
Articaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Articaine.
Tetracaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Tetracaine.
Propoxycaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Propoxycaine.
Pramocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Pramocaine.
Butamben The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Butamben.
Butacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Butacaine.
Oxetacaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Oxetacaine.
Ethyl chloride The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Ethyl chloride.
Butanilicaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Butanilicaine.
Metabutethamine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Metabutethamine.
Quinisocaine The risk or severity of methemoglobinemia can be increased when Imetelstat is combined with Quinisocaine.
Etrasimod The risk or severity of immunosuppression can be increased when Imetelstat is combined with Etrasimod.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Imetelstat.
Pravastatin The serum concentration of Pravastatin can be increased when it is combined with Imetelstat.
Valsartan The serum concentration of Valsartan can be increased when it is combined with Imetelstat.
Erythromycin The serum concentration of Erythromycin can be increased when it is combined with Imetelstat.
Torasemide The serum concentration of Torasemide can be increased when it is combined with Imetelstat.
Mesalazine The serum concentration of Mesalazine can be increased when it is combined with Imetelstat.
Liothyronine The serum concentration of Liothyronine can be increased when it is combined with Imetelstat.
Conjugated estrogens The serum concentration of Conjugated estrogens can be increased when it is combined with Imetelstat.
Digoxin The serum concentration of Digoxin can be increased when it is combined with Imetelstat.
Cerivastatin The serum concentration of Cerivastatin can be increased when it is combined with Imetelstat.
Raloxifene The serum concentration of Raloxifene can be increased when it is combined with Imetelstat.
Caspofungin The serum concentration of Caspofungin can be increased when it is combined with Imetelstat.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Imetelstat.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Imetelstat.
Enalapril The serum concentration of Enalapril can be increased when it is combined with Imetelstat.
Simvastatin The serum concentration of Simvastatin can be increased when it is combined with Imetelstat.
Sumatriptan The serum concentration of Sumatriptan can be increased when it is combined with Imetelstat.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be increased when it is combined with Imetelstat.
Penicillamine The serum concentration of Penicillamine can be increased when it is combined with Imetelstat.
Repaglinide The serum concentration of Repaglinide can be increased when it is combined with Imetelstat.
Dinoprostone The serum concentration of Dinoprostone can be increased when it is combined with Imetelstat.
Fexofenadine The serum concentration of Fexofenadine can be increased when it is combined with Imetelstat.
Ezetimibe The serum concentration of Ezetimibe can be increased when it is combined with Imetelstat.
Benzylpenicillin The serum concentration of Benzylpenicillin can be increased when it is combined with Imetelstat.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Imetelstat.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Imetelstat.
Fluvastatin The serum concentration of Fluvastatin can be increased when it is combined with Imetelstat.
Rosuvastatin The serum concentration of Rosuvastatin can be increased when it is combined with Imetelstat.
Liotrix The serum concentration of Liotrix can be increased when it is combined with Imetelstat.
Cholic Acid The serum concentration of Cholic Acid can be increased when it is combined with Imetelstat.
Taurocholic acid The serum concentration of Taurocholic acid can be increased when it is combined with Imetelstat.
Atrasentan The serum concentration of Atrasentan can be increased when it is combined with Imetelstat.
Simeprevir The serum concentration of Simeprevir can be increased when it is combined with Imetelstat.
Ambrisentan The serum concentration of Ambrisentan can be increased when it is combined with Imetelstat.
Axitinib The serum concentration of Axitinib can be increased when it is combined with Imetelstat.
Gimatecan The serum concentration of Gimatecan can be increased when it is combined with Imetelstat.
Temocapril The serum concentration of Temocapril can be increased when it is combined with Imetelstat.
Cholecystokinin The serum concentration of Cholecystokinin can be increased when it is combined with Imetelstat.
Gadoxetic acid The serum concentration of Gadoxetic acid can be increased when it is combined with Imetelstat.
Technetium Tc-99m mebrofenin The serum concentration of Technetium Tc-99m mebrofenin can be increased when it is combined with Imetelstat.
Fimasartan The serum concentration of Fimasartan can be increased when it is combined with Imetelstat.
Paritaprevir The serum concentration of Paritaprevir can be increased when it is combined with Imetelstat.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Imetelstat.
Selexipag The serum concentration of Selexipag can be increased when it is combined with Imetelstat.
Grazoprevir The serum concentration of Grazoprevir can be increased when it is combined with Imetelstat.
Asunaprevir The serum concentration of Asunaprevir can be increased when it is combined with Imetelstat.
Tezacaftor The serum concentration of Tezacaftor can be increased when it is combined with Imetelstat.
Momelotinib The serum concentration of Momelotinib can be increased when it is combined with Imetelstat.
Revefenacin Imetelstat may decrease the excretion rate of Revefenacin which could result in a higher serum level.
Elagolix The serum concentration of Elagolix can be increased when it is combined with Imetelstat.
Voxilaprevir The serum concentration of Voxilaprevir can be increased when it is combined with Imetelstat.
Letermovir The serum concentration of Letermovir can be increased when it is combined with Imetelstat.
Brincidofovir The serum concentration of Brincidofovir can be increased when it is combined with Imetelstat.
Resmetirom The serum concentration of Resmetirom can be increased when it is combined with Imetelstat.
Levosalbutamol The serum concentration of Levosalbutamol can be increased when it is combined with Imetelstat.
Glecaprevir The serum concentration of Glecaprevir can be increased when it is combined with Imetelstat.
Belantamab mafodotin The serum concentration of Belantamab mafodotin can be increased when it is combined with Imetelstat.
Atogepant The serum concentration of Atogepant can be increased when it is combined with Imetelstat.
Testosterone The serum concentration of Testosterone can be increased when it is combined with Imetelstat.
Paclitaxel The serum concentration of Paclitaxel can be increased when it is combined with Imetelstat.
Docetaxel The serum concentration of Docetaxel can be increased when it is combined with Imetelstat.
Sincalide The serum concentration of Sincalide can be increased when it is combined with Imetelstat.

Target Protein

Telomerase reverse transcriptase TERT
Human telomerase RNA component

Referensi & Sumber

Artikel (PubMed)
  • PMID: 37504319
    Lucero J, Al-Harbi S, Yee KWL: Management of Patients with Lower-Risk Myelodysplastic Neoplasms (MDS). Curr Oncol. 2023 Jun 27;30(7):6177-6196. doi: 10.3390/curroncol30070459.
  • PMID: 31394818
    Kubasch AS, Platzbecker U: Setting Fire to ESA and EMA Resistance: New Targeted Treatment Options in Lower Risk Myelodysplastic Syndromes. Int J Mol Sci. 2019 Aug 7;20(16). pii: ijms20163853. doi: 10.3390/ijms20163853.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Rytelo
    Injection, powder, lyophilized, for solution • 47 mg/1 • Intravenous • US • Approved
  • Rytelo
    Injection, powder, lyophilized, for solution • 188 mg/1 • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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