Romidepsin
- Atc Codes:L01XX39
- CAS Codes:128517-07-7
- PHARMGKB ID:128517-07-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Istodax.
Asia
Japan: Chromadax.
Drug combinations
Chemistry
Romidepsin: C~24~H~36~N~4~O~6~S~2~. Mw: 540.71. (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone. CAS-128517-07-7.
Pharmacologic Category
Other Antineoplastic Agents. Histone Deacetylase Inhibitor. (ATC-Code: L01XX39).
Mechanism of action
Romidepsin is a histone deacetylase (HDAC) inhibitor. HDACs catalyze the removal of acetyl groups from acetylated lysine residues in histones, resulting in the modulation of gene expression. HDACs also deacetylate non-histone proteins, such as transcription factors. In vitro, romidepsin causes the accumulation of acetylated histones, and induces cell cycle arrest and apoptosis of some cancer cell lines with IC~50~ values in the nanomolar range. The mechanism of the antineoplastic effect of romidepsin observed in nonclinical and clinical studies has not been fully characterized.
Therapeutic use
Treatment of cutaneous T-cell lymphoma (CTCL) in patients who have received at least one prior systemic therapy.
Pregnancy and lactiation implications
May cause fetal harm when administered to a pregnant woman. Not recommended during lactation.
Unlabeled use
Contraindications
None known to date.
Warnings and precautions
Risk of QT prolongation (ensure that potassium and magnesium are within the normal range before administration). Treatment with romidepsin has been associated with thrombocytopenia, leukopenia (neutropenia and lymphopenia), and anemia (monitor these hematological parameters during treatment and modify the dose as necessary). Electrocardiographic (ECG) changes have been observed. Based on its mechanism of action, may cause fetal harm when administered to a pregnant woman. May reduce the effectiveness of estrogen-containing contraceptives due to its binding to estrogen receptors.