Panobinostat

Products

Panobinostat was approved in many countries in 2015 in capsule form (Farydak).

Structure and properties

Panobinostat (C21H23N3O2, Mr = 349.4 g/mol) is present in the drug as panobinostat lactate, a white to slightly yellow or brownish powder that is sparingly soluble in water. It is an indole, a hydroxamic acid, and a propenamide derivative.

Effects

Panobinostat (ATC L01XX42) has cytotoxic and antiproliferative properties. The effects are due to inhibition of histone deacetylases (HDACs), which catalyze the removal of acetyl groups from lysine residues on histones. This leads to accumulation of acetylated histones and eventual cell death (apoptosis). Panobinostat has a long half-life of 37 hours.

Indications

For treatment of multiple myeloma (not as first-line agent, combination therapy with bortezomib and dexamethasone).

Dosage

According to the SmPC. Capsules are taken every other day at the same time of day on a full stomach. Treatment is given in cycles of therapy.

Contraindications

For complete precautions, see the drug label.

Interactions

Panobinostat is a substrate of CYP3A with minor involvement of CYP2D6 and CYP2C19. It is glucuronidated by several UGT isozymes. Corresponding drug-drug interactions may occur.

Adverse effects

The most common potential adverse effects include diarrhea, fatigue, nausea, peripheral edema, poor appetite, fever, and vomiting.