Beleodaq

Beleodaq Uses, Dosage, Side Effects, Food Interaction and all others data.

Beleodaq 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 Beleodaq
Availability Prescription only
Generic Belinostat
Belinostat Other Names Belinostat
Related Drugs prednisone, methotrexate, dexamethasone, Revlimid, Imbruvica, Velcade, romidepsin, Folotyn, pralatrexate, Istodax
Weight 500mg,
Type Injection, Powder, Lyophilized, For Solution, Intravenous Powder For Injection
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
Beleodaq
Beleodaq

Uses

Beleodaq is a histone deacetylase (HDAC) inhibitor used for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL).

Beleodaq 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 .

Beleodaq is also used to associated treatment for these conditions: Relapsed Peripheral T-Cell Lymphoma, Refractory Peripheral T-cell Lymphoma Unspecified

How Beleodaq works

Beleodaq 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

Beleodaq 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.

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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