Products
Ibrutinib is commercially available in capsule form (Imbruvica). It has been approved in many countries since 2014. Film-coated tablets were registered in 2019.
Structure and properties
Ibrutinib (C25H24N6O2, Mr = 440.5 g/mol) exists as a white substance that is practically insoluble in water.
Effects
Ibrutinib (ATC L01XE27) is a noncompetitive (irreversible) inhibitor of Bruton’s tyrosine kinase (BTK). This signaling molecule is involved in the pathogenesis of mantle cell lymphoma. Ibrutinib has a terminal half-life of approximately 15 hours.
Indications
- Mantle cell lymphoma (MCL)
- Chronic lymphocytic leukemia (CLL)
- Waldenström’s disease
Dosage
According to the professional information. The capsules or tablets are taken once a day always at the same time of day. Do not take with grapefruit juice.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Ibrutinib is metabolized by CYP3A and corresponding drug-drug interactions with CYP inhibitors and inducers are possible.
Adverse effects
The most common potential adverse effects include thrombocytopenia, diarrhea, neutropenia, anemia, fatigue, muscle pain, peripheral edema, upper respiratory tract infections, nausea, injury, taste disturbance, constipation, abdominal pain, dyspnea, rash, vomiting, and poor appetite.
