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依鲁替尼

印度依鲁替尼

【 药品别名 】 依鲁替尼 Ibrutinib Emlutini

【药品简介】 依鲁替尼是一种小分子BTK抑制剂,能够与BTK活性中心的半胱氨酸残基共价结合,从而抑制其活性。

【适应症状】 白血病、淋巴瘤:慢性淋巴细胞白血病或小淋巴细胞性淋巴瘤(CLL/SLL),以及带有17p缺失突变的CLL/SLL;用于治疗既往接受过治疗的套细胞淋巴瘤(MCL)

印度依鲁替尼(依鲁替尼 Ibrutinib Emlutini)价格,正品图片,治疗淋巴瘤药物, 购买依鲁替尼请到印度药房官方网站进行购买 【印度药房大全目录】

资料发布时间:2018-10-30 14:50:00 资料更新时间:2019-11-12 09:00:41

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【印度依鲁替尼(依鲁替尼 Ibrutinib Emlutini)说明书】

依鲁替尼作用机制:

依鲁替尼(Ibrutinib)是小分子BTK 抑制药,与BTK活性位点中的半胱氨酸残基形成共价键,从而抑制BTK酶的活性。研究显示,依鲁替尼具有抑制恶性B细胞增殖和体内的存活以及体外细胞迁移和底物的黏附作用。
 
依鲁替尼
 
依鲁替尼参考用法:

1. CLL/SLL:口服,420mg 每天一次(单药或与苯达莫司汀/美罗华联用);直至疾病进展或不可接受的毒性。

2. CLL/SLL(含17p缺失):口服,420mg 每天一次;直至疾病进展或不可接受的毒性

3. 套细胞淋巴瘤,经治:口服,560mg 每天一次,直至疾病进展或不可接受的毒性

4. Waldenström macroglobulinemia:口服,420mg 每天一次,直至疾病进展或不可接受的毒性
 
依鲁替尼常见副作用:

头痛、劳累、早饱、恶心呕吐、腹痛、腹泻、便秘、肌肉痛、关节痛等

临床试验中,在接受过治疗的CLL患者中,总反应率为58.3%,缓解持续时间为5.6-24.2月;套细胞淋巴瘤,总反应率位65.8%,缓解持续时间为17.5月

依鲁替尼英文说明书

Ibrutinib uses

Ibrutinib is used in the treatment of mantle-cell lymphoma and blood cancer (chronic lymphocytic leukemia). It is also used in chronic lymphocytic leukaemia who have received at least one prior therapy or with 17p deletion.

How ibrutinib works

Ibrutinib is a Bruton's tyrosine kinase inhibitor. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps to stop or slow the spread of cancer cells.

Common side effects of ibrutinib

Headache, Joint pain, Fever, Diarrhea, Vomiting, Stomatitis (Inflammation of the mouth), Nausea, Constipation, Low blood platelets, Decreased white blood cell count (neutrophils), Upper respiratory tract infection

Ibrutinib

生物活性

产品描述

Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

靶点活性

BLK,0.5 nM (cell free)

Bmx,0.8 nM (cell free)

BTK,0.5 nM (cell free)

CSK,2.3 nM (cell free)

FGR,2.3 nM (cell free)

BRK,3.3 nM (cell free)

实验溶液

2% DMSO+castor oil: 10 mg/mL

体外活性

In DOHH2, a cell line in which the BCR pathway can be activated by stimulation with anti-IgG, Ibrutinib (PCI-32765) inhibits autophosphorylation of Btk (IC50: 11 nM), phosphorylation of Btk's physiological substrate PLCγ (IC50: 29 nM), and phosphorylation of a further downstream kinase, ERK (IC50: 13 nM). Continuous exposure to 10 nM PCI-32765 for 18 h completely prevented up-regulation of the B-cell activation marker CD69. A 1-h pulse exposure to 10 nM PCI-32765 resulted in a similar level of CD69 inhibition in B cells [1]. PCI-32765 inhibited BCR-activated primary B cell proliferation (IC50: 8 nM). Following FcγR stimulation, PCI-32765 inhibited TNFα, IL-1β and IL-6 production in primary monocytes (IC50s: 2.6/0.5/3.9 nM). Following FcεRI stimulation of cultured human mast cells, PCI-32765 inhibited release of histamine, PGD(2), TNF-α, IL-8, and MCP-1 [2]. Treatment of CD40 or BCR activated CLL cells with PCI-32765 results in inhibition of BTK tyrosine phosphorylation and also effectively abrogates downstream survival pathways activated by this kinase including ERK1/2, PI3K, and NF-κB. In addition, PCI-32765 inhibits activation-induced proliferation of CLL cells in vitro and effectively blocks survival signals provided externally to CLL cells from the microenvironment [3].

体内活性

PCI-32765 (3.125, 12.5, or 50 mg/kg per day) markedly inhibited clinical arthritis scores. Partial and nearly complete elimination of clinical signs of the disease occurred after 9 to 11 d of treatment at dosages of 3.125 and 12.5 mg/kg per day, respectively. An oral single dose of PCI-32765 at 3.125 mg/kg per day resulted in partial Btk occupancy in splenocytes, and the maximally efficacious dose (12.5 mg/kg per day) was sufficient to fully occupy Btk for 12 h [1]. PCI-32765 dose-dependently and potently reversed arthritic inflammation in a therapeutic CIA model (ED50: 2.6 mg/kg/day). PCI-32765 also prevented clinical arthritis in CAIA models. In both models, infiltration of monocytes and macrophages into the synovium was completely inhibited [2].

激酶实验

In vitro kinase IC50s were measured using 33P filtration binding assay after 1 h incubation of kinase, 33P-ATP, inhibitor, and substrate [0.2 mg/mL poly(EY)(4:1]. Assays were performed at Reaction Biology [1].

细胞实验

CD20+ B and CD3+ T cells were purified by negative selection (RosetteSep, >90% purity) from buffy coat PBMCs and viably frozen in 10% DMSO. Cells were thawed at 37 °C and maintained in growth media (RPMI media containing 10% FCS). B cells were stimulated with goat anti-human IgM F(ab′)2 (10 μg/mL) and T cells were stimulated with anti-CD3/CD28 coated beads at a 1:1 bead/cell ratio. Cells were stained with PE-CD69 and analyzed by flow cytometry, gating on viable lymphocytes. PCI-32765 at concentrations lower than 10 μM did not decrease B- or T-cell viability during the course of the experiment, although PCI-32765 did block the modest survival benefit of anti-IgM stimulation in B cells. For washout experiments, cells were rinsed three times in 10 volumes of growth media, a protocol that was confirmed to completely wash away inhibition of BCR signaling by PCI-29732, a reversible Btk inhibitor [1].

细胞系: Chronic lymphocytic leukemia (CLL) cells

动物实验

ale DBA/1 mice were immunized with type II collagen plus Freund adjuvant and boosted 21 d later. On a rolling basis, as significant swelling appeared in at least one paw, mice were enrolled and randomized. PCI-32765 or dexamethasone (0.2 mg/kg) was administered orally once per day for 11 d. Arthritis scores (0–5) were assigned to the mice based on the degree and extent of paw swelling. Mouse anti-type II collagen antibody and total IgG levels were measured by ELISA. Female MRL/MpJ-Faslpr mice received PCI-32765 by oral gavage once per day from week 8 through week 20. Proteinuria was monitored weekly. At week 20, serum was collected and analyzed for BUN and mouse anti-dsDNA antibody levels. Kidney histology was scored according to established criteria (26). No drug-induced weight loss was observed at any of the dose levels tested. These studies were carried out at Boulder Biopath according to approved animal care protocols. Results are presented as the mean ± SEM. Statistical significance between groups were evaluated with repeated measures one-way ANOVA or one-way ANOVA using GraphPad Prism with Tukey or Bonferroni multicomparison posttest [1].

动物模型:MRL-Fas(lpr) lupus model and collagen-induced arthritis model.

化学信息

分子量

440.50

分子式

C25H24N6O2

CAS

936563-96-1

溶解度

DMSO: 82 mg/mL (186.2 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

  1 mg 5 mg 10 mg
1 mM 2.27 ml 11.351 ml 22.701 ml
5 mM 0.454 ml 2.27 ml 4.54 ml
10 mM 0.227 ml 1.135 ml 2.27 ml
50 mM 0.045 ml 0.227 ml 0.454 ml

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