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Product name: Ibrutinib /CAS: 936563-96-1

Appearance White powder
Purity (gc area %) ≥ 98.5%
Density 1.34
H NMR Conforms to structure
Bruton tyrosine kinase (BTK) inhibitor Ibrutinib is a kind of Bruton tyrosine kinase (BTK) inhibitor, it could be used for the treatment of chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). MCL and CLL are belonged to the B-cell non-Hodgkin’s lymphoma, which is difficult to cure and easy to recurrent. Common chemical immunotherapy does not have the targeting, often occurs 3 or 4 adverse reactions. Ibrutinib and B lymphocytes could target with BTK which is necessary for formation, differentiation, and transmission of information, inhibit BTK activity irreversibly, and inhibit tumor cell proliferation and survival effectively. Ibrutinib could be rapidly absorbed after oral administration, during 1 ~ 2h reach maximum blood concentration, adverse reactions belong to one or two, therefore, Ibrutinib will become a new choice of treatment of CLL and MCL.
Food and Drug Administration (FDA) of USA has speed up approval of Pharmacyclics Corporation and Johnson & Johnson’s Imbruvica (generic name: Ibrutinib) came to market to the cure a kind of rarely aggressive leukemia – mantle cell lymphoma (MCL) in 13th November, 2013. Ibrutinib is a new kind of oral Bruton tyrosine kinase (BTK) inhibitor, it was awarded by FDA be a breakthrough drugs in February of 2013, and approved the MCL and CLL treatments in 13th November, 2013 and 12th February, 2014 respectively. It could covalently bound selectively with cysteine residues (Cys-481) in active site of Btk target protein, irreversible inhibit BTK, thereby effectively prevent tumor cells from migrating from B cell to lymphoid tissue where adapt for tumor growth. Information was collated by Xiaonan editor of Chemicalbook.
Chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) Chronic lymphocytic leukemia (CLL) is a kind of chronic hematological malignancies that because mature lymphocytes cannot apoptosis normally, but the clonal proliferation in lymphoid tissues.CLL has some hereditary, it is a common form and belonged to non-Hodgkin’s lymphoma (NHL) of B cells. Mantle cell lymphoma (MCL) is a rare B-cell NHL, 5% ~ 10% accounting for all the NHL, it has refractory and aggressive of malignant lymphoma. MCL is difficult to diagnose, approximately 85% patients are diagnosed at stage Ⅲ ~ Ⅳ, and easy to relapse,which is the lowest long-term survival of lymphoma subtypes. Clinical manifestations are including High fever, fatigue, spleen and lymph nodes, infiltration of the gastrointestinal tract, and nervous system involvement.
At present, first-line treatment for CLL is FCR program, which is combining fludarabine (F), cyclophosphamide (C), and rituximab (R). This program had positive effect, but the survival was 38% Current first-line treatment for CLL is FCR program that of the three joint regimen, the program has some effect, but the rate of progression-free survival was 38%, it happened 3 or 4 adverse reactions sometimes. MCL often used anthracycline or high-dose cytarabine-containing drugs, but mostly conventional chemotherapy is not sensitive. Though there are many drugs for the treatment, survival was not significantly longer ; Although the program is also used in combination with chemotherapy drugs and monoclonal antibody therapy MCL, high toxicity has made the infection rate is about 14%, 3 to 4 adverse reaction rates as high as 87%. Therefore, coming up with more viable treatment programs and safe drugs are need to be introduced efficiently.
Research and development process Ibrutinib was developed by American Celera Genentech (Celera Genomics)
that was well known because it was the first one drawn “human genome”.
Pan Zhengying (now Beijing University Shenzhen Graduate School
Distinguished Fellow) as the first author of this research and published
the process of Ibrutinib in 2007 (ChemMedChem 2 (1): 58-61). But Celera
had transferred the development rights to Pharmacyclics Company of
California due to funding and resources.
Although Pharmacyclics Company was in a very difficult stage, only $
0.64 for the stock, facing delisting and bankruptcy in that time,
company’s management has managed to raise funds, spent only $ 2 million
to down payment, 100 million shares and future sales royalty and
milestone payment of royalties more to get Ibrutinib.
In 2011, Johnson & Johnson subsidiary Janssen pay $ 150 million
upfront payment in order to get the right to cooperate with
Pharmacyclics. Once the new drugs in clinical trials and approved to
listing, Pharmacyclics company will get $ 975 million in total revenue,
and they will share the sales.When the deal was announced, Pharmacyclics
stock is only $ 12. Market value was only several hundred million
dollars. However, the stock is already $ 123, $ 9.05 billion value now.
Signaling pathway of B cell antigen receptor (BCR) is a key driver of tumor growth and spread. BTK as an indispensable participant for BCR signal peptide, it is very important for formation, differentiation, messaging and survival of B lymphocyte. BTK is an identifiable signal peptide molecules of BCR channel. When the signal peptide molecules across the B lymphocyte surface receptors, required channel is activated for transportation, chemotaxis and adhesion, which provide a convenience to be B-cell malignancies.
Ibrutinib is a small molecule can selectively and covalently bound to a cysteine residue (Cys-481) BTK active site, and irreversibly inhibit BTK activity, thereby inhibiting BCR activated signaling pathway, which could effectively prevent the tumor from B cells to lymphoid tissues where suitable for tumor growth, to reduce B cell proliferation and induce apoptosis of malignant cells, which play a role in the treatment of CLL and MCL. Non-clinical studies have shown that Ibrutinib can inhibit malignant B lymphocyte proliferation and survival.
Metabolism and Elimination Ibrutinib primarily metabolized by the cytochrome P450 (CYP3A and a small part of the CYP2D6) and produce a variety of metabolites after metabolism. The metabolite (PCI-45227) is a kind of dihydrodiol substance which is an activity of inhibiting BTK.Compared with Ibrutinib, PCI-45227 has much stronger inhibition on BTK, which is about 15 times stronger. At steady state, the average rate of metabolism of PCI-45227 is around 1 ~ 2.8.
Apparent clearance (CL / F) of Ibrutinibis is approximately 1 000 L / h, the half-life (t1 / 2) is 4 ~ 6 h. Ibrutinib mainly be metabolites in the body, excrete with the feces. To healthy subjects by oral radioactive 14C-labeled Ibrutinib, found that nearly 90% of the radiation were eliminated in 168 h, most (about 80%) of them were excreted with the feces, and nearly 10% were excreted in the urine, about 1 % be prototypes were excreted with the feces.
Elimination of Ibrutinib will not make a difference in age (37 to 84 years) and gender, but systemic exposure of patients with moderate hepatic injury will be 6 times higher than in healthy subjects.

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