Ixazomib

Products

Ixazomib was approved in capsule form in the United States in 2015, in the EU in 2016, and in many countries in 2017 (Ninlaro).

Structure and properties

Ixazomib is present in drugs in the form of the prodrug ixazomib citrate (C14H19BCl2N2O4, Mr = 361.0 g/mol) is present. In the body, it is hydrolyzed to the active ingredient ixazomib.

Effects

Ixazomib (ATC L01XX50) has antitumor and cytotoxic properties. It is a proteasome inhibitor that binds to the beta5 subunit of the 20S proteasome, leading to apoptosis of myeloma cells. Ixazomib has a long half-life of 9.5 days.

Indications

For the treatment of multiple myeloma. Ixazomib is used in combination with lenalidomide and dexamethasone in patients who have received prior therapy.

Dosage

The therapeutic regimen is outlined in the SmPC. The capsules are taken once a week in the therapeutic cycle, fasting once daily, at least one hour before or two hours after a meal. They should be administered on the same day of the week and at the same time of day.

Contraindications

For complete precautions, see the drug label.

Interactions

Ixazomib is a substrate of CYP450 isozymes and corresponding drug-drug interactions are possible.

Adverse effects

The most common potential adverse effects include diarrhea, constipation, thrombocytopenia, peripheral neuropathy, nausea, peripheral edema, vomiting, and back pain.