Idelalisib

Products

Idelalisib was approved in many countries in 2015 in film-coated tablet form (Zydelig).

Structure and properties

Idelalisib (C₂₂H₁₈FN₇O, M_r = 415.4 g/mol) exists as a white powder that is soluble in acidic environments.

Effects

Idelalisib (ATC L01XX47) has antiproliferative, selective cytotoxic, and antitumor properties. The effects are due to inhibition of phosphatidylinositol 3-kinase p110δ.

Indications

• B-cell chronic lymphocytic leukemia (B-CLL), in combination with rituximab.
• Recurrent follicular lymphoma.

Dosage

According to the professional information. The tablets are taken in the morning and evening, 12 hours apart and independently of meals.

Contraindications

• Hypersensitivity
• Acute hepatitis

For complete precautions, see the drug label.

Interactions

Idelalisib is biotransformed predominantly by aldehyde oxidase. To a lesser extent, CYP3A and UGT1A4 are also involved. Idelalisib and its major metabolite are substrates of P-glycoprotein and BCRP.

Adverse effects

The most common potential adverse effects include diarrhea, fever, fatigue, nausea, cough, pneumonia, abdominal pain, chills, and rash. Serious and life-threatening adverse reactions such as hepatotoxicity, severe diarrhea or colitis, pneumonitis, and intestinal perforation are possible.