Product Name

Ibrutinib

CAS Number

936563-96-1

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Product Name:
Ibrutinib
CAS Number:
936563-96-1
Indication:
Ibrutinib was approved by the FDA for the treatment of mantle cell lymphoma, and later in February 2014 for the treatment of chronic lymphocytic leukemia. Ibrutinib is also indicated for the treatment of patients with Waldenström’s Macroglobulinemia (WM).
Mode of Action:

Ibrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK). It forms a covalent bond with a cysteine residue in the active site of BTK, leading to its inhibition. BTK plays a role in signalling through the B-cell surface receptors which results in the activation of various pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Ibrutinib has been shown to inhibit malignant B cell proliferation and survival in vivo as well as substrate adhesion and cell migration.

Pharmacodynamics:

In patients with recurrent B-cell lymphoma > 90% occupancy of the BTK active site in peripheral blood mononuclear cells was observed up to 24 hours after ibrutinib doses of ≥ 2.5 mg/kg/day (≥ 175 mg/day for average weight of 70 kg).

Metabolism:

It is metabolized to several metabolites primarily by cytochrome P450, CYP3A, and to a minor extent by CYP2D6. The active metabolite, PCI-45227, is a dihydrodiol metabolite with inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib. The range of the mean metabolite to parent ratio for PCI-45227 at steady-state is 1 to 2.8.

ATC:
L01XE27
DrugBank:
DB09053
Formula:
C25-H24-N6-O2
Molecular Mass:
440.5046
Synonyms:
2-Propen-1-one, 1-((3R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo(3,4-d)pyrimidin-1-yl)-1-piperidinyl)-, CRA-032765, Ibrutinib, Pc-32765, PCI 32765, PCI32765, UNII-1X70OSD4VX
SMILES:
C=CC(=O)N1CCCC(C1)[n@]2c3c(c(n2)c4ccc(cc4)Oc5ccccc5)c(ncn3)N
InChi:
InChI=1S/C25H24N6O2/c1-2-21(32)30-14-6-7-18(15-30)31-25-22(24(26)27-16-28-25)23(29-31)17-10-12-20(13-11-17)33-19-8-4-3-5-9-19/h2-5,8-13,16,18H,1,6-7,14-15H2,(H2,26,27,28)
General Reference:
General Reference:

  1. Bagcchi S: Ibrutinib in pretreated Waldenstrom’s macroglobulinaemia. Lancet Oncol. 2015 May;16(5):e204. doi: 10.1016/S1470-2045(15)70185-3. Epub 2015 Apr 16. Pubmed
  2. Kim ES, Dhillon S: Ibrutinib: a review of its use in patients with mantle cell lymphoma or chronic lymphocytic leukaemia. Drugs. 2015 May;75(7):769-76. doi: 10.1007/s40265-015-0380-3. Pubmed
  3. Scheers E, Leclercq L, de Jong J, Bode N, Bockx M, Laenen A, Cuyckens F, Skee D, Murphy J, Sukbuntherng J, Mannens G: Absorption, metabolism, and excretion of oral 14C radiolabeled ibrutinib: an open-label, phase I, single-dose study in healthy men. Drug Metab Dispos. 2015 Feb;43(2):289-97. doi: 10.1124/dmd.114.060061. Epub 2014 Dec 8.

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