Panobinostat
Wikipedia on Answers.com:
Top
Panobinostat
 |
|
|---|---|
| Systematic (IUPAC) name | |
| (2E)-N-hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 404950-80-7  |
| ATC code | L01XX42 |
| PubChem | CID 6918837 |
| UNII | 9647FM7Y3Z |
| Chemical data | |
| Formula | C21H23N3O2 |
| Mol. mass | 349.42622 g/mol |
| SMILES | eMolecules & PubChem |
 (what is this?) (verify) |
|
Panobinostat (LBH-589) is an experimental drug developed by Novartis for the treatment of various cancers. It is a hydroxamic acid[1] and acts as a non-selective histone deacetylase inhibitor (HDAC inhibitor).[2]
|
Contents
|
Clinical trials
As of December 2008[update], it is being tested against cutaneous T cell lymphoma (CTCL), chronic myelogenous leukemia, myelodysplastic syndromes, breast cancer, prostate cancer and other types of malignant disease in a number of Phase II and III clinical trials,[3][4] for example a Phase III study for CTCL.[5]
Preclinical studies
Panobinostat has been found to synergistically act with sirolimus to kill pancreatic cancer cells in the laboratory in a Mayo Clinic study. In the study, investigators found that this combination destroyed up to 65 percent of cultured pancreatic tumor cells. The finding is significant because the three cell lines studies were all resistant to the effects of chemotherapy – as are many pancreatic tumors.[6]
Panobinostat has also recently been found to significantly increase in vitro the survival of motor neuron (SMN) protein levels in cells of patients suffering from spinal muscular atrophy.[7]
Mechanism of action
Panobinostat inhibits multiple histone deacetylase enzymes, a mechanism leading to apoptosis of malignant cells via multiple pathways.[1]
References
- ^ a b Revill, P; Mealy, N; Serradell, N; Bolos, J; Rosa, E (2007). "Panobinostat". Drugs of the Future 32 (4): 315. doi:10.1358/dof.2007.032.04.1094476. ISSN 0377-8282. http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1094476&p_IsPs=N.
- ^ http://www.nature.com/nbt/journal/v28/n12/fig_tab/nbt.1724_T3.html
- ^ ClinicalTrials.gov: LBH-589
- ^ Prince, HM; M Bishton (2009). "Panobinostat (LBH589): a novel pan-deacetylase inhibitor with activity in T cell lymphoma". Hematology Meeting Reports (Parkville, Australia: Peter MacCallum Cancer Centre and University of Melbourne) 3 (1): 33–38. http://www.pagepress.org/journals/index.php/hmr/article/viewFile/526/606.
- ^ ClinicalTrials.gov NCT00425555 Study of Oral LBH589 in Adult Patients With Refractory Cutaneous T-Cell Lymphoma
- ^ Mayo Clinic Researchers Formulate Treatment Combination Lethal To Pancreatic Cancer Cells
- ^ Garbes, L; Riessland, M; Hölker, I; Heller, R; Hauke, J; Tränkle, Ch; Coras, R; Blümcke, I; Hahnen, E; Wirth, B (2009). "LBH589 induces up to 10-fold SMN protein levels by several independent mechanisms and is effective even in cells from SMA patients non-responsive to valproate". Human Molecular Genetics 18 (19): 3645–3658. doi:10.1093/hmg/ddp313. PMID 19584083. http://hmg.oxfordjournals.org/cgi/content/abstract/ddp313.
 |
This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it. |
This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
Post a question - any question - to the WikiAnswers community:
Copyrights:
Wikipedia on Answers.com
This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article Panobinostat.
Read more