Chemical Property of Panobinostat
Chemical Property:
- Appearance/Colour:Yellow solid
- Melting Point:114-117?C
- Refractive Index:1.682
- PKA:8.71±0.23(Predicted)
- PSA：77.15000
- Density:1.241 g/cm3
- LogP:4.10900
- Storage Temp.:-20°C Freezer, Under Inert Atmosphere
- Solubility.:Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 5 mg/ml with warming).
- XLogP3:3
- Hydrogen Bond Donor Count:4
- Hydrogen Bond Acceptor Count:3
- Rotatable Bond Count:7
- Exact Mass:349.17902698
- Heavy Atom Count:26
- Complexity:474
- Purity/Quality:
-
99%, *data from raw suppliers
Panobinostat *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- Statements:
22-36/37/38-20
- Safety Statements:
24/25
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Antineoplastic Agents
- Canonical SMILES:CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=O)NO
- Isomeric SMILES:CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)/C=C/C(=O)NO
- Recent ClinicalTrials:Panobinostat/Bortezomib/Dexamethasone in Relapsed or Relapsed-and-refractory Multiple Myeloma
- Recent EU Clinical Trials:Efficacy of daratumumab (Dara) retreatment using a histone deacetylase-inhibitor (HDACi: panobinostat) as a Dara-longevity-inducing, epigenetic agent in combination with bortezomib-dexamethasone as a quadruplet in relapsed / refractory multiple myeloma (RRMM) patients
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Description
Panobinostat is a potent inhibitor of all histone deacetylases (HDACs), with Ki values ranging from 0.6 to 31 nM for HDAC1-11. Through this action, it leads to acetylation of a range of cellular proteins, resulting in cell cycle arrest and apoptosis in cancer cells. It has potential applications in several different forms of cancer as well as in spinal muscular atrophy and HIV therapy.
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Uses
The novel labelled histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells.
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Clinical Use
Histone deacetylase (HDAC) inhibitor:
Treatment of relapsed and/or refractory multiple
myeloma
-
Drug interactions
Potentially hazardous interactions with other drugs
Analgesics: avoid with dextromethorphan possibly
increased risk of ventricular arrhythmias with
methadone - avoid.
Anti-arrhythmics: increased risk of ventricular
arrhythmias with amiodarone and possibly
disopyramide - avoid.
Antibacterials: increased risk of ventricular
arrhythmias with clarithromycin and moxifloxacin -
avoid; avoid with rifampicin.
Antidepressants: avoid with St John’s wort.
Antiepileptics: avoid with carbamazepine,
fosphenytoin, phenobarbital, phenytoin and
primidone.
Antifungals: concentration increased by ketoconazole
and possibly posaconazole and voriconazole - reduce
panobinostat dose; concentration possibly increased
by itraconazole - avoid.
Antimalarials: possibly increased risk of ventricular
arrhythmias with chloroquine - avoid.
Antipsychotics: avoid with pimozide.
Antivirals: concentration possibly increased
by ritonavir and saquinavir - reduce dose of
panobinostat.
Beta-blockers: possibly increased risk of ventricular
arrhythmias with sotalol - avoid.
Grapefruit juice: avoid concomitant use.
5HT3
antagonists: possibly increased risk of
ventricular arrhythmias with granisetron and
ondansetron - avoid with granisetron.
