Peringatan Keamanan

The most severe adverse effects after homoharringtonine administration are myelosuppression, bleeding, hyperglycemia, and fetal harm.

Omacetaxine mepesuccinate

DB04865

small molecule approved investigational

Deskripsi

Omacetaxine mepesuccinate (formerly known as HHT or Homoharringtonine), is a cephalotaxine ester and protein synthesis inhibitor with established clinical activity as a single agent in hematological malignancies. Omacetaxine mepesuccinate is synthesized from cephalotaxine, which is an extract from the leaves of the plant, Cephalotaxus species. In October 2005, omacetaxine mepesuccinate received Orphan Drug designation from the EMEA for the treatment of chronic myeloid leukemia (CML). Then in March 2006, it received Orphan Drug status from the FDA for the treatment of CML. In November 2006, omacetaxine mepesuccinate, for the treatment of CML, was granted Fast Track designation by the FDA. Most recently, in October 2012, omacetaxine mepesuccinate was marketed under the brand name Synribo and FDA approved for patients who are intolerant and/or resistant to two or more tyrosine kinase inhibitors used to treat accelerated or chronic phase CML.

Struktur Molekul 2D

Berat 545.6213
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Homoharringtonine has a half life of about 6 hours after subcutaneous administration.
Volume Distribusi Homoharringtonine has a steady state Vd of 141 ± 93.4 L.
Klirens (Clearance) Clearance for homoharringtonine was not quantified.

Absorpsi

Homoharringtonine absorption was not quantified, but maximum concentration is reached after about 30 mins.

Metabolisme

Homoharringtonine has undergoes little hepatic metabolism and is mostly metabolized to 4’-DMHHT by plasma esterase hydrolysis.

Rute Eliminasi

The main route of elimination for homoharringtonine is still unknown, but renal elimination is less than 15%.

Interaksi Obat

224 Data
Lepirudin The risk or severity of bleeding can be increased when Lepirudin is combined with Omacetaxine mepesuccinate.
Bivalirudin The risk or severity of bleeding can be increased when Bivalirudin is combined with Omacetaxine mepesuccinate.
Alteplase The risk or severity of bleeding can be increased when Alteplase is combined with Omacetaxine mepesuccinate.
Urokinase The risk or severity of bleeding can be increased when Urokinase is combined with Omacetaxine mepesuccinate.
Reteplase The risk or severity of bleeding can be increased when Reteplase is combined with Omacetaxine mepesuccinate.
Anistreplase The risk or severity of bleeding can be increased when Anistreplase is combined with Omacetaxine mepesuccinate.
Tenecteplase The risk or severity of bleeding can be increased when Tenecteplase is combined with Omacetaxine mepesuccinate.
Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Omacetaxine mepesuccinate.
Drotrecogin alfa The risk or severity of bleeding can be increased when Drotrecogin alfa is combined with Omacetaxine mepesuccinate.
Streptokinase The risk or severity of bleeding can be increased when Streptokinase is combined with Omacetaxine mepesuccinate.
Dicoumarol The risk or severity of bleeding can be increased when Dicoumarol is combined with Omacetaxine mepesuccinate.
Argatroban The risk or severity of bleeding can be increased when Argatroban is combined with Omacetaxine mepesuccinate.
Ardeparin The risk or severity of bleeding can be increased when Ardeparin is combined with Omacetaxine mepesuccinate.
Phenindione The risk or severity of bleeding can be increased when Phenindione is combined with Omacetaxine mepesuccinate.
Fondaparinux The risk or severity of bleeding can be increased when Fondaparinux is combined with Omacetaxine mepesuccinate.
Warfarin The risk or severity of bleeding can be increased when Warfarin is combined with Omacetaxine mepesuccinate.
Pentosan polysulfate The risk or severity of bleeding can be increased when Pentosan polysulfate is combined with Omacetaxine mepesuccinate.
Phenprocoumon The risk or severity of bleeding can be increased when Phenprocoumon is combined with Omacetaxine mepesuccinate.
Dipyridamole The risk or severity of bleeding can be increased when Dipyridamole is combined with Omacetaxine mepesuccinate.
Heparin The risk or severity of bleeding can be increased when Heparin is combined with Omacetaxine mepesuccinate.
Enoxaparin The risk or severity of bleeding can be increased when Enoxaparin is combined with Omacetaxine mepesuccinate.
Epoprostenol The risk or severity of bleeding can be increased when Epoprostenol is combined with Omacetaxine mepesuccinate.
Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Omacetaxine mepesuccinate.
4-hydroxycoumarin The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Omacetaxine mepesuccinate.
Coumarin The risk or severity of bleeding can be increased when Coumarin is combined with Omacetaxine mepesuccinate.
Ximelagatran The risk or severity of bleeding can be increased when Ximelagatran is combined with Omacetaxine mepesuccinate.
Desmoteplase The risk or severity of bleeding can be increased when Desmoteplase is combined with Omacetaxine mepesuccinate.
Defibrotide The risk or severity of bleeding can be increased when Defibrotide is combined with Omacetaxine mepesuccinate.
Ancrod The risk or severity of bleeding can be increased when Ancrod is combined with Omacetaxine mepesuccinate.
Beraprost The risk or severity of bleeding can be increased when Beraprost is combined with Omacetaxine mepesuccinate.
Prasugrel The risk or severity of bleeding can be increased when Prasugrel is combined with Omacetaxine mepesuccinate.
Rivaroxaban The risk or severity of bleeding can be increased when Rivaroxaban is combined with Omacetaxine mepesuccinate.
Sulodexide The risk or severity of bleeding can be increased when Sulodexide is combined with Omacetaxine mepesuccinate.
Semuloparin The risk or severity of bleeding can be increased when Semuloparin is combined with Omacetaxine mepesuccinate.
Idraparinux The risk or severity of bleeding can be increased when Idraparinux is combined with Omacetaxine mepesuccinate.
Cangrelor The risk or severity of bleeding can be increased when Cangrelor is combined with Omacetaxine mepesuccinate.
Astaxanthin The risk or severity of bleeding can be increased when Astaxanthin is combined with Omacetaxine mepesuccinate.
Apixaban The risk or severity of bleeding can be increased when Apixaban is combined with Omacetaxine mepesuccinate.
Otamixaban The risk or severity of bleeding can be increased when Otamixaban is combined with Omacetaxine mepesuccinate.
Amediplase The risk or severity of bleeding can be increased when Amediplase is combined with Omacetaxine mepesuccinate.
Dabigatran etexilate The risk or severity of bleeding can be increased when Dabigatran etexilate is combined with Omacetaxine mepesuccinate.
Danaparoid The risk or severity of bleeding can be increased when Danaparoid is combined with Omacetaxine mepesuccinate.
Dalteparin The risk or severity of bleeding can be increased when Dalteparin is combined with Omacetaxine mepesuccinate.
Tinzaparin The risk or severity of bleeding can be increased when Tinzaparin is combined with Omacetaxine mepesuccinate.
(R)-warfarin The risk or severity of bleeding can be increased when (R)-warfarin is combined with Omacetaxine mepesuccinate.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Ethyl biscoumacetate is combined with Omacetaxine mepesuccinate.
Nadroparin The risk or severity of bleeding can be increased when Nadroparin is combined with Omacetaxine mepesuccinate.
Triflusal The risk or severity of bleeding can be increased when Triflusal is combined with Omacetaxine mepesuccinate.
Ticagrelor The risk or severity of bleeding can be increased when Ticagrelor is combined with Omacetaxine mepesuccinate.
Ditazole The risk or severity of bleeding can be increased when Ditazole is combined with Omacetaxine mepesuccinate.
Vorapaxar The risk or severity of bleeding can be increased when Vorapaxar is combined with Omacetaxine mepesuccinate.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Omacetaxine mepesuccinate.
Sodium citrate The risk or severity of bleeding can be increased when Sodium citrate is combined with Omacetaxine mepesuccinate.
Dextran The risk or severity of bleeding can be increased when Dextran is combined with Omacetaxine mepesuccinate.
Bemiparin The risk or severity of bleeding can be increased when Bemiparin is combined with Omacetaxine mepesuccinate.
Parnaparin The risk or severity of bleeding can be increased when Parnaparin is combined with Omacetaxine mepesuccinate.
Desirudin The risk or severity of bleeding can be increased when Desirudin is combined with Omacetaxine mepesuccinate.
Antithrombin Alfa The risk or severity of bleeding can be increased when Antithrombin Alfa is combined with Omacetaxine mepesuccinate.
Protein C The risk or severity of bleeding can be increased when Protein C is combined with Omacetaxine mepesuccinate.
Antithrombin III human The risk or severity of bleeding can be increased when Antithrombin III human is combined with Omacetaxine mepesuccinate.
Letaxaban The risk or severity of bleeding can be increased when Letaxaban is combined with Omacetaxine mepesuccinate.
Darexaban The risk or severity of bleeding can be increased when Darexaban is combined with Omacetaxine mepesuccinate.
Betrixaban The risk or severity of bleeding can be increased when Betrixaban is combined with Omacetaxine mepesuccinate.
Nafamostat The risk or severity of bleeding can be increased when Nafamostat is combined with Omacetaxine mepesuccinate.
Monteplase The risk or severity of bleeding can be increased when Monteplase is combined with Omacetaxine mepesuccinate.
Gabexate The risk or severity of bleeding can be increased when Gabexate is combined with Omacetaxine mepesuccinate.
Fluindione The risk or severity of bleeding can be increased when Fluindione is combined with Omacetaxine mepesuccinate.
Protein S human The risk or severity of bleeding can be increased when Protein S human is combined with Omacetaxine mepesuccinate.
Brinase The risk or severity of bleeding can be increased when Brinase is combined with Omacetaxine mepesuccinate.
Clorindione The risk or severity of bleeding can be increased when Clorindione is combined with Omacetaxine mepesuccinate.
Diphenadione The risk or severity of bleeding can be increased when Diphenadione is combined with Omacetaxine mepesuccinate.
Tioclomarol The risk or severity of bleeding can be increased when Tioclomarol is combined with Omacetaxine mepesuccinate.
Melagatran The risk or severity of bleeding can be increased when Melagatran is combined with Omacetaxine mepesuccinate.
Saruplase The risk or severity of bleeding can be increased when Saruplase is combined with Omacetaxine mepesuccinate.
(S)-Warfarin The risk or severity of bleeding can be increased when (S)-Warfarin is combined with Omacetaxine mepesuccinate.
Tocopherylquinone The risk or severity of bleeding can be increased when Tocopherylquinone is combined with Omacetaxine mepesuccinate.
Dabigatran The risk or severity of bleeding can be increased when Dabigatran is combined with Omacetaxine mepesuccinate.
Troxerutin The risk or severity of bleeding can be increased when Troxerutin is combined with Omacetaxine mepesuccinate.
Edetic acid The risk or severity of bleeding can be increased when Edetic acid is combined with Omacetaxine mepesuccinate.
Reviparin The risk or severity of bleeding can be increased when Reviparin is combined with Omacetaxine mepesuccinate.
Dermatan sulfate The risk or severity of bleeding can be increased when Dermatan sulfate is combined with Omacetaxine mepesuccinate.
SR-123781A The risk or severity of bleeding can be increased when SR-123781A is combined with Omacetaxine mepesuccinate.
Icosapent The risk or severity of bleeding can be increased when Icosapent is combined with Omacetaxine mepesuccinate.
Indomethacin The risk or severity of bleeding can be increased when Indomethacin is combined with Omacetaxine mepesuccinate.
Nabumetone The risk or severity of bleeding can be increased when Nabumetone is combined with Omacetaxine mepesuccinate.
Ketorolac The risk or severity of bleeding can be increased when Ketorolac is combined with Omacetaxine mepesuccinate.
Tenoxicam The risk or severity of bleeding can be increased when Tenoxicam is combined with Omacetaxine mepesuccinate.
Celecoxib The risk or severity of bleeding can be increased when Celecoxib is combined with Omacetaxine mepesuccinate.
Tolmetin The risk or severity of bleeding can be increased when Tolmetin is combined with Omacetaxine mepesuccinate.
Rofecoxib The risk or severity of bleeding can be increased when Rofecoxib is combined with Omacetaxine mepesuccinate.
Piroxicam The risk or severity of bleeding can be increased when Piroxicam is combined with Omacetaxine mepesuccinate.
Fenoprofen The risk or severity of bleeding can be increased when Fenoprofen is combined with Omacetaxine mepesuccinate.
Valdecoxib The risk or severity of bleeding can be increased when Valdecoxib is combined with Omacetaxine mepesuccinate.
Diclofenac The risk or severity of bleeding can be increased when Diclofenac is combined with Omacetaxine mepesuccinate.
Sulindac The risk or severity of bleeding can be increased when Sulindac is combined with Omacetaxine mepesuccinate.
Flurbiprofen The risk or severity of bleeding can be increased when Flurbiprofen is combined with Omacetaxine mepesuccinate.
Etodolac The risk or severity of bleeding can be increased when Etodolac is combined with Omacetaxine mepesuccinate.
Mefenamic acid The risk or severity of bleeding can be increased when Mefenamic acid is combined with Omacetaxine mepesuccinate.
Naproxen The risk or severity of bleeding can be increased when Naproxen is combined with Omacetaxine mepesuccinate.
Sulfasalazine The risk or severity of bleeding can be increased when Sulfasalazine is combined with Omacetaxine mepesuccinate.

Target Protein

50S ribosomal protein L2 rpl2
Large ribosomal subunit protein uL3 RPL3

Referensi & Sumber

Synthesis reference: Yaguang Liu, "Process for producing harringtonine and homoharringtonine." U.S. Patent US4783454, issued June, 1980.
Artikel (PubMed)
  • PMID: 17613769
    Lou YJ, Qian WB, Jin J: Homoharringtonine induces apoptosis and growth arrest in human myeloma cells. Leuk Lymphoma. 2007 Jul;48(7):1400-6.
  • PMID: 17487741
    Jie H, Donghua H, Xingkui X, Liang G, Wenjun W, Xiaoyan H, Zhen C: Homoharringtonine-induced apoptosis of MDS cell line MUTZ-1 cells is mediated by the endoplasmic reticulum stress pathway. Leuk Lymphoma. 2007 May;48(5):964-77.

Contoh Produk & Brand

Produk: 1 • International brands: 2
Produk
  • Synribo
    Injection, powder, lyophilized, for solution • 3.5 mg/1mL • Subcutaneous • US • Approved
International Brands
  • Ceflatonin — ChemGenex Therapeutics
  • Myelostat

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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