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The SARfaris: GPCR, Kinase, ADME

Friday, 15 November 2013

New Drug Approvals 2013 - Pt. XIX - Ibrutinib (ImbruvicaTM)

ATC Code:
Wikipedia: Ibrutinib

On November 13, 2013, the FDA approved Ibrutinib (ImbruvicaTM) for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy. MCL is a subtype of B-cell lymphoma and accounts for 6% of non-Hodgkin's lymphoma cases. In an open-label, multi-center, single-arm trial of 111 previously treated patients, Ibrutinib showed a 65.8% response rate.

Ibrutinib is an irreversible inhibitor of the Tyrosine-protein kinase BTK (Uniprot:Q06187; ChEMBL:CHEMBL5251; canSAR target synopsis) and is the first approved targeted BTK inhibitor. It forms a covalent bond with a cysteine residue via a Michael acceptor mechanism, in the BTK active site, leading to inhibition of BTK enzymatic activity

Ibrutinib (ChEMBL:CHEMBL1873475; canSAR drug synopsis; also known as CRA-032765 and PCI-32765) has the formula C25H24N6O2 and a molecular weight 440.50. It is absorbed after oral administration with a median Tmax of 1-2 hours. After administration of 560 mg dose, the observed AUC is 953 ± 705 ng⋅h/mL. The apparent volume of distribution at steady state (Vd,ss/F) is approximately 10000 L and the half-life is 4 to 6 hours.

ImbruvicaTM is produced by Pharmacyclics, Inc.

The full Prescribing Information is here

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