Romidepsin
![Skeletal formula of (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-diisopropyl-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone](https://en.wikipedia.org/wiki/File:Romidepsin_structure_(2).svg) |
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| Clinical data | |
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| Trade names | Istodax |
| MedlinePlus | a610005 |
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| Routes of administration |
Intravenous infusion |
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| Pharmacokinetic data | |
| Bioavailability | Not applicable (IV only) |
| Protein binding | 92–94% |
| Metabolism | Hepatic (mostly CYP3A4-mediated) |
| Biological half-life | 3 hours |
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| Synonyms | FK228; FR901228; Istodax |
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| ECHA InfoCard | 100.211.884 |
| Chemical and physical data | |
| Formula | C24H36N4O6S2 |
| Molar mass | 540.695 g/mol |
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Romidepsin, also known as Istodax, is an anticancer agent used in cutaneous T-cell lymphoma (CTCL) and other peripheral T-cell lymphomas (PTCLs). Romidepsin is a natural product obtained from the bacterium Chromobacterium violaceum, and works by blocking enzymes known as histone deacetylases, thus inducing apoptosis. It is sometimes referred to as depsipeptide, after the class of molecules to which it belongs. Romidepsin is branded and owned by Gloucester Pharmaceuticals, now a part of Celgene.
Romidepsin was first reported in the scientific literature in 1994, by a team of researchers from Fujisawa Pharmaceutical Company (now Astellas Pharma) in Tsukuba, Japan, who isolated it in a culture of Chromobacterium violaceum from a soil sample obtained in Yamagata Prefecture. It was found to have little to no antibacterial activity, but was potently cytotoxic against several human cancer cell lines, with no effect on normal cells; studies on mice later found it to have antitumor activity in vivo as well.
The first total synthesis of romidepsin was accomplished by Harvard researchers and published in 1996. Its mechanism of action was elucidated in 1998, when researchers from Fujisawa and the University of Tokyo found it to be a histone deacetylase inhibitor with effects similar to those of trichostatin A.
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