Belinostat

Action and Spectrum

Histone deacetylase (HDAC) is inhibited by belinostat, which stops acetyl groups from being removed from the lysine residues of histones and certain non-histone proteins. 

Belinostat induced the buildup of acetylated histones and other proteins in vitro and raised the expression of genes that limit tumor growth. 

At a nanomolar dosage, the histone deacetylase (HDAC) inhibitor beleodaq has strong growth inhibitory and pro-apoptotic effects in PTCL cells as well as pan-HDAC inhibition across a range of tumor types. 

Drug Interaction

Adverse Reaction

Frequency defined

>10%

Fatigue (37%)

Nausea (42%)

Pyrexia (35%)

Vomiting (29%)

Anemia (32%)

Constipation (23%)

Dyspnea (22%)

Diarrhea (23%)

Rash (20%)

Cough (19%)

Peripheral edema (20%)

Black Box Warning

None

Contraindication / Caution

Contraindication: 

None 

Caution: 

Hematologic toxicity 

Infections 

Hepatotoxicity 

Tumor lysis syndrome 

Pregnancy / Lactation

Pregnancy consideration: N/A

Lactation: N/A

Pregnancy category:

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women.
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women.
• Category N: There is no data available for the drug under this category.

Pharmacology

Beleodaq did not cause any clinically significant changes in heart rate, PR or QRS duration, which are indicators of autonomic status, atrioventricular conduction, or depolarization, and there were no instances of Torsades de Pointes in any of the trials. 

The acetyl groups that are present in the lysine residues of histones and certain nonhistone proteins are removed by HDACs.  

Adminstartion

For administration, attach the infusion bag holding the medication solution to an infusion set equipped with a 0.22 micron in-line filter. 

Infuse through intravenous route over 30 minutes. 

Stir the contents of the vial until the final solution is free of any visible particles. 

Infusion site pain or other symptoms linked to the infusion may cause the infusion period to be extended to 45 minutes. 

Patient Information Leaflet

Patient information leaflet

Generic Name: belinostat

Why do we use belinostat?

belinostat is a medication that belongs to a class of drugs known as histone deacetylase (HDAC) inhibitors. It is used to treat a type of cancer known as peripheral T-cell lymphoma (PTCL) in patients who have not responded to other treatments or who have relapsed after treatment.

PTCL is a rare and aggressive form of non-Hodgkin lymphoma that develops in mature T-cells, a type of white blood cell. belinostat works by blocking the action of certain enzymes in cancer cells, which leads to cell death and slows down the growth and spread of cancer cells.