Romidepsine

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

Romidepsine is a selective inhibitor of histone deacetylase, approved in the US in 2009 for the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated.

Romidepsine
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Romidepsine
Availability	Prescription only
Generic	Romidepsin
Romidepsin Other Names	Romidepsin, Romidepsina, Romidepsine, Romidepsinum
Related Drugs	bexarotene, methoxsalen, Targretin, vorinostat, Folotyn, belinostat, pralatrexate, Targretin Gel, Istodax
Type
Formula	C₂₄H₃₆N₄O₆S₂
Weight	Average: 540.69 Monoisotopic: 540.207627243
Protein binding	Highly protein bound in plasma (92%-94%)
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Romidepsine is a histone deacetylase (HDAC) inhibitor used to treat cutaneous and peripheral T-cell lymphoma.

For the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated.

Romidepsine is also used to associated treatment for these conditions: Refractory peripheral cutaneous T-cell lymphoma

How Romidepsine works

Romidepsine is a prodrug, where it becomes active once taken up into the cell. The active metabolite has a free thiol group, which interacts with zinc ions in the active site of class 1 and 2 HDAC enzymes, resulting in inhibition of its enzymatic activity. Certain tumors have over expressed HDACs and downregulated/mutated histone acetyltransferases. This imbalance of HDAC relative to histone acetyltransferase can lead to a decrease in regulatory genes, ensuing tumorigenesis. Inhibition of HDAC may restore normal gene expression in cancer cells and result in cell cycle arrest and apoptosis.

Toxicity

Risk factor D in pregnancy. It is not known if romidepsin is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, the manufacturer recommends a decision be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother. The majority of patients receiving romidepsin experience nausea, vomiting, and anorexia.

Food Interaction

Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of romidepsin.
Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce serum levels of romidepsin.