Romidepsina
Romidepsina Uses, Dosage, Side Effects, Food Interaction and all others data.
Romidepsina 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.
| Trade Name | Romidepsina |
| 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
Romidepsina 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.
Romidepsina is also used to associated treatment for these conditions: Refractory peripheral cutaneous T-cell lymphoma
How Romidepsina works
Romidepsina 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.
Romidepsina Disease Interaction
Moderate: hepatic impairment, infections, myelosuppression, QT prolongation, renal impairment
Volume of Distribution
44.5L
Elimination Route
Romidepsina exhibited linear pharmacokinetics at standard doses.
Half Life
Approximately 3 hours
Clearance
8.4L/h
Innovators Monograph
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