Mepesuccinato De Omacetaxina
Mepesuccinato De Omacetaxina Uses, Dosage, Side Effects, Food Interaction and all others data.
Mepesuccinato De Omacetaxina (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. Mepesuccinato De Omacetaxina 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.
The pharmacodynamics of homoharringtonine is not fully understood. It is known that homoharringtonine is involvedwith protein synthesis inhibition and this leads to its antineoplastic activity.
| Trade Name | Mepesuccinato De Omacetaxina |
| Generic | Omacetaxine mepesuccinate |
| Omacetaxine mepesuccinate Other Names | Homoharringtonin, Homoharringtonine, mepesuccinato de omacetaxina, Omacetaxine mepesuccinate |
| Type | |
| Formula | C29H39NO9 |
| Weight | Average: 545.6213 Monoisotopic: 545.262481851 |
| Protein binding | Plasma protein binding is equal or less than 50%. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Mepesuccinato De Omacetaxina is a cephalotaxine used in the treatment of Chronic Myeloid Leukemia (CML) that is intolerant to or resistant to two or more tyrosine kinase inhibitors.
Used in patients who are intolerant and/or resistant to two or more tyrosine kinase inhibitors used to treat accelerated or chronic phase CML.
Mepesuccinato De Omacetaxina is also used to associated treatment for these conditions: Refractory, accelerated phase Chronic myeloid leukemia, Refractory, chronic phase Chronic myeloid leukemia
How Mepesuccinato De Omacetaxina works
Homoharringtonine inhibits protein synthesis by not directly binding to Bcr-Abl. It binds to the A-site cleft in the large ribosomal subunit, which affects chain elongation and prevents protein synthesis.
Toxicity
The most severe adverse effects after homoharringtonine administration are myelosuppression, bleeding, hyperglycemia, and fetal harm.
Food Interaction
No interactions found.Volume of Distribution
Homoharringtonine has a steady state Vd of 141 ± 93.4 L.
Elimination Route
Homoharringtonine absorption was not quantified, but maximum concentration is reached after about 30 mins.
Half Life
Homoharringtonine has a half life of about 6 hours after subcutaneous administration.
Clearance
Clearance for homoharringtonine was not quantified.
Elimination Route
The main route of elimination for homoharringtonine is still unknown, but renal elimination is less than 15%.
Innovators Monograph
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