Belinostat
Belinostat Uses, Dosage, Side Effects, Food Interaction and all others data.
Belinostat is a novel agent that inhibits the enzyme histone deacetylase (HDAC) with a sulfonamide-hydroxamide structure. It was developed as an orphan drug to target hematological malignancies and solid tumors by TopoTarget. The safety and efficacy of belinostat is currently being evaluated for use in combination with traditional front-line therapies for the treatment of PTCL. Intravenous administration of the agent is available as Beleodaq as monotherapy and the dosing regimen involves a 21-day cycle. It was US-approved in July 2014 as a therapeutic agent for relapsed or refractory peripheral T-cell lymphoma.
Beleodaq is a histone deacetylase (HDAC) inhibitor that exhibits pan-HDAC inhibition and potent growth inhibitory and pro-apoptotic activities in a variety of tumor cells, including PTCL cells, at nanomolar concentrations . None of the trials show any clinically relevant changes caused by Beleodaq on heart rate, PR duration or QRS duration as measures of autonomic state, atrio-ventricular conduction or depolarization; there were no cases of Torsades de Pointes.
| Trade Name | Belinostat |
| Availability | Prescription only |
| Generic | Belinostat |
| Belinostat Other Names | Belinostat |
| Related Drugs | prednisone, methotrexate, dexamethasone, Revlimid, Imbruvica, Velcade, romidepsin, Folotyn, pralatrexate, Istodax |
| Weight | 500mg, |
| Type | Intravenous Powder For Injection, Intravenous |
| Formula | C15H14N2O4S |
| Weight | Average: 318.35 Monoisotopic: 318.067428113 |
| Protein binding | 92.9% and 95.8% of belinostat is bound to protein. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Belinostat is a histone deacetylase (HDAC) inhibitor used for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL).
Belinostat is indicated for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) with manageable safety profile. It is a potential alternative therapy for patients who did not experience adequate response to first-line drugs for PTCL. It can be used in patients with baseline thrombocytopenia .
Belinostat is also used to associated treatment for these conditions: Relapsed Peripheral T-Cell Lymphoma, Refractory Peripheral T-cell Lymphoma Unspecified
How Belinostat works
Belinostat inhibits the activity of histone deacetylase (HDAC) thus prevents the removal of acetyl groups from the lysine residues of histones and some non-histone proteins. In vitro, belinostat caused the accumulation of acetylated histones and other proteins, increased the expression of tumor-suppressor genes. It ultimately induces cell cycle arrest, inhibition of angiogenesis and/or apoptosis of some transformed cells.
Toxicity
Belinostat is genotoxic according to Ames test and may impair male fertility. Weekly complete blood count should be monitored during treatment to adjust the dosage as intravenous infusion of belinostat is frequently associated with hematologic toxicity such as leukopenia and thrombocytopenia. Incidences of infections such as sepsis, hepatotoxicity, tumor lysis syndrome, gastrointestinal toxicity, and embryo-fetal toxicity may occur. No specific information is available on the treatment of overdosage of Beleodaq. There is no antidote for Beleodaq and it is not known if Beleodaq is dialyzable. If an overdose occurs, general supportive measures should be instituted as deemed necessary by the treating physician.
Food Interaction
No interactions found.Belinostat Disease Interaction
Major: tumor lysis syndromeModerate: hematologic toxicity, hepatic impairment, infections, renal impairment
Volume of Distribution
The volume of distribution is 409 ± 76.7 L.
Half Life
Displays a three-compartment pharmacokinetic property with elimination half life of 1.1 hours
Clearance
1240 mL/min
Elimination Route
Approximately 40% of the belinostat dose is excreted renally, primarily as metabolites and less than 2% of total dose recovered as unchanged parent drug.
Innovators Monograph
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