*** Welcome to piglix ***

Ibrutinib

Ibrutinib
Ibrutinib.svg
Clinical data
Trade names Imbruvica
License data
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
administration
Oral (capsules)
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding 97.3%
Metabolism Hepatic (CYP3A & CYP2D6)
Biological half-life 4–6 hours
Excretion Feces (80%), urine (10%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.232.543
Chemical and physical data
Formula C25H24N6O2
Molar mass 440.4971
3D model (Jmol)

Ibrutinib (Imbruvica) is a small molecule drug that binds permanently to a protein, Bruton's tyrosine kinase (BTK), that is important in B cells; the drug is used to treat B cell cancers like mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenström's macroglobulinemia, a form of non-Hodgkin's lymphoma.

Ibrutinib was created by scientists at Celera Genomics as a tool compound for studying BTK function, then developed by Pharmacyclics up to Phase II, then partnered with Johnson & Johnson. Pharmacyclics was acquired by AbbVie in May 2015, and Abbvie projected global sales of US$1 billion in 2016 and $5 billion in 2020.

According to the Wall Street Journal in January 2016 ibrutinib, a specialty drug, cost US$116,600 to $155,400 a year wholesale in the United States. In spite of discounts and medical insurance, the prohibitive price causes some patients to not fill their prescriptions.

Ibrutinib is used to treat mantle cell lymphoma, chronic lymphocytic leukemia, and Waldenstrom's macroglobulinemia.

Very common (>10% frequency) adverse effects include pneumonia, upper respiratory tract infection, sinusitis, skin infection, low neutrophil count, low platelet counts, headache, bleeding, bruising, diarrhea, vomiting, inflammation of mouth and lips, nausea, constipation, rash, joint pain, muscle spasms, musculoskeletal pain, fever, and edema.


...
Wikipedia

...