Panobinostat lactate

Panobinostat lactate is a hydroxamic acid derivative and a histone deacetylase inhibitor (HDAC inhibitor) with potential antineoplastic activity. It is marketed by Novartis under the trade name Farydak.

Mechanism of Action

Panobinostat lactate inhibits the activity of histone deacetylase, an enzyme that removes acetyl groups from the histone proteins, leading to the condensation of the DNA helix, thereby preventing transcription. By inhibiting histone deacetylase, panobinostat lactate increases acetylation of histones, leading to a relaxed chromatin structure, which results in an increased rate of transcription. This may lead to a reduction in tumor cell proliferation and the induction of tumor cell apoptosis.

Clinical Use

Panobinostat lactate is used in the treatment of multiple myeloma, a type of blood cancer. It is used in combination with bortezomib and dexamethasone in patients who have received at least two prior regimens, including bortezomib and an immunomodulatory agent.

Side Effects

Common side effects of panobinostat lactate include fatigue, diarrhea, nausea, vomiting, and anemia. Serious side effects may include cardiac arrhythmias, electrolyte abnormalities, and bleeding.

Pharmacokinetics

Panobinostat lactate is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 2 hours. It is extensively metabolized in the liver, primarily by CYP3A4, and is excreted primarily in the feces.

See Also

• Histone deacetylase inhibitor
• Multiple myeloma
• Novartis