This article will be permanently flagged as inappropriate and made unaccessible to everyone. Are you certain this article is inappropriate? Excessive Violence Sexual Content Political / Social
Email Address:
Article Id: WHEBN0020845241 Reproduction Date:
InChI=1S/C21H23N3O2/c1-15-18(19-4-2-3-5-20(19)23-15)12-13-22-14-17-8-6-16(7-9-17)10-11-21(25)24-26/h2-11,22-23,26H,12-14H2,1H3,(H,24,25)/b11-10+ N Key:FPOHNWQLNRZRFC-ZHACJKMWSA-N N
Panobinostat (LBH-589, trade name Faridak) 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]
As of August 2012, it is being tested against Hodgkin's Lymphoma, cutaneous T cell lymphoma (CTCL)[3] and other types of malignant disease in Phase III clinical trials, against myelodysplastic syndromes, breast cancer and prostate cancer in Phase II trials, and against chronic myelomonocytic leukemia (CMML) in a Phase I trial.[4][5]
Panobinostat is currently being used in a Phase I/II clinical trial that aims at curing AIDS in patients on highly active antiretroviral therapy (HAART). In this technique, panobinostat is used to drive the HIV DNA out of the patient's DNA, in the expectation that the patient's immune system in combination with HAART will destroy it.[6][7] [8]
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 studied were all resistant to the effects of chemotherapy – as are many pancreatic tumors.[9]
Panobinostat has also been found to significantly increase in vitro the survival of motor neuron (SMN) protein levels in cells of patients suffering from spinal muscular atrophy.[10]
Panobinostat was able to selectively target triple negative breast cancer (TNBC) cells by inducing hyperacetylation and cell cycle arrest at the G2-M DNA damage checkpoint; partially reversing the morphological changes characteristic of breast cancer cells.[11]
Panobinostat, along with other HDAC inhibitors, is also being studied for potential to induce virus HIV-1 expression in latently infected cells and disrupt latency. These resting cells are not recognized by the immune system as harboring the virus and do not respond to antiretroviral drugs.[12]
Panobinostat inhibits multiple histone deacetylase enzymes, a mechanism leading to apoptosis of malignant cells via multiple pathways.[1]
: NEO
,
, ,
drug (//)
Diamond, Graphite, Solar system, Coal, /anolanthanide Chemistry
Oxygen, Argon, Hydrogen, Helium, Gold
Nitrogen, Hydrogen, Helium, Sulfur, Fluorine
Polymerase chain reaction, Primase, Replication fork, Topoisomerase, HolE
Ovarian cancer, Breast cancer, Lymphoma, Multiple myeloma, Gene expression
Lung cancer, Prostate cancer, Pancreatic cancer, Ovarian cancer, Breast cancer
Methylation, Cancer, Ovarian cancer, Chromatin, Transcription (genetics)
ATC code L, Leukemia, Cancer, Pharmacology, Metabolism
DNA replication, Ribonucleotide reductase inhibitor, Cell cycle, Alkylating antineoplastic agent, Chemotherapy