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Lucatumumab Sale

(Synonyms: HCD122) 目录号 : GC66382

Lucatumumab (HCD122) 是一种全人抗 CD40 拮抗剂单克隆抗体,可阻断 CD40/ CD40L 介导的信号通路。Lucatumumab 可有效介导抗体依赖性细胞介导的细胞毒性 (ADCC) 和肿瘤细胞清除,可用于顽固性淋巴瘤、慢性淋巴细胞白血病 (CLL) 和多发性骨髓瘤研究。

Lucatumumab Chemical Structure

Cas No.:903512-50-5

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产品描述

Lucatumumab (HCD122) is a fully human anti-CD40 antagonist monoclonal antibody, which blocks CD40/CD40L-mediated signaling. Lucatumumab efficiently mediates antibody-dependent cell-mediated cytotoxicity (ADCC) and clearance of tumor cells, can be used for refractory lymphomas, CLL and multiple myeloma research[1][2].

Lucatumumab (0.001-10 μg/mL; 4 h; 37 ℃) inhibit B-cell chronic lymphocytic leukemia (B-CLL) growth by ADCC-mediated cell lysis, with the average maximal lysis of B-CLL cells of 49%[1].
Lucatumumab (0.1-10 μg/mL; 3 d) inhibits CD40L-induced signaling and viability of B-CLL cells[1].
Lucatumumab (10 μg/mL; 24 h) inhibits cytokine secretion by B-CLL cells[1].

Cell Viability Assay[1]

Cell Line: B-cell chronic lymphocytic leukemia (B-CLL)
Concentration: 0.001 to 10 μg/mL
Incubation Time: 72 hours; 37 ℃
Result: Inhibited B-CLL growth with an ED50 of 14 pM and a average maximal lysis of B-CLL cells of 49%.

Chemical Properties

Cas No. 903512-50-5 SDF Download SDF
别名 HCD122
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Research Update

Phase I study of the anti-CD40 humanized monoclonal antibody Lucatumumab (HCD122) in relapsed chronic lymphocytic leukemia

Leuk Lymphoma 2012 Nov;53(11):2136-42.PMID:22475052DOI:10.3109/10428194.2012.681655.

Lucatumumab is a fully humanized anti-CD40 antibody that blocks interaction of CD40L with CD40 and also mediates antibody-dependent cell-mediated cytotoxicity (ADCC). We evaluated Lucatumumab in a phase I clinical trial in chronic lymphocytic leukemia (CLL). Twenty-six patients with relapsed CLL were enrolled on five different dose cohorts administered weekly for 4 weeks. The maximally tolerated dose (MTD) of Lucatumumab was 3.0 mg/kg. Four patients at doses of 4.5 mg/kg and 6.0 mg/kg experienced grade 3 or 4 asymptomatic elevated amylase and lipase levels. Of the 26 patients enrolled, 17 patients had stable disease (mean duration of 76 days, range 29-504 days) and one patient had a nodular partial response for 230 days. Saturation of CD40 receptor on CLL cells was uniform at all doses post-treatment but also persisted at trough time points in the 3.0 mg/kg or greater cohorts. At the MTD, the median half-life of Lucatumumab was 50 h following the first infusion, and 124 h following the fourth infusion. In summary, Lucatumumab had acceptable tolerability, pharmacokinetics that supported chronic dosing and pharmacodynamic target antagonism at doses of 3.0 mg/kg, but demonstrated minimal single-agent activity. Future efforts with Lucatumumab in CLL should focus on combination-based therapy.

Anti-CD40-mediated cancer immunotherapy: an update of recent and ongoing clinical trials

Immunopharmacol Immunotoxicol 2014 Apr;36(2):96-104.PMID:24555495DOI:10.3109/08923973.2014.890626.

The costimulatory molecule CD40 is a member of the tumor necrosis factor (TNF) receptor superfamily and is expressed on various antigen presenting cells (APCs) as well as some tumor cells. The binding to the natural ligand CD40L, which is expressed on T helper cells, leads to APC activation and thus enhancement of immune responses. Treatment with anti-CD40 monoclonal antibodies has been exploited in several cancer immunotherapy studies in mice and led to the development of anti-CD40 antibodies for clinical use. Here, Dacetuzumab and Lucatumumab are in the most advanced stage and are being tested as treatment for malignancies such as chronic lymphatic leukemia (CLL), Multiple Myeloma (MM), and non-Hodgkin's lymphoma (NHL). The promising results from these early clinical trials have encouraged clinical drug development in order to investigate the effect of CD40 mAbs in combination with other cancer immunotherapies, in particular interleukin (IL)-2. An in-depth analysis of this immunotherapy is provided elsewhere. In the present review, we provide an update of the most recent clinical trials with anti-CD40 antibodies. We present and discuss recent and ongoing clinical trials in this field, including clinical studies which combine anti-CD40 treatment with other cancer-treatments, such as Rituximab and Tremelimumab.

A phase 1 study of Lucatumumab, a fully human anti-CD40 antagonist monoclonal antibody administered intravenously to patients with relapsed or refractory multiple myeloma

Br J Haematol 2012 Oct;159(1):58-66.PMID:22861192DOI:10.1111/j.1365-2141.2012.09251.x.

In this open-label, multicentre, phase 1 study a fully human anti-CD40 antagonist monoclonal antibody, Lucatumumab, was evaluated in patients with relapsed/refractory multiple myeloma (MM). The primary objective was to determine the maximum tolerated dose (MTD) based on dose-limiting toxicities (DLTs). Secondary objectives included safety, pharmacokinetics, pharmacodynamics and antimyeloma activity. Twenty-eight patients, enrolled using a standard '3 + 3' dose escalation, received one or two (n = 3) cycles of Lucatumumab 1·0, 3·0, 4·5 or 6·0 mg/kg once weekly for 4 weeks. Common lucatumumab-related adverse events were reversible, mild-to-moderate infusion reactions. Severe adverse events were anaemia, chills, hypercalcaemia and pyrexia (7% each). DLTs included grade 4 thrombocytopenia, grade 3 increased alanine aminotransferase and grade 4 increased lipase (n = 1 each). The MTD was 4·5 mg/kg. At doses ≥3·0 mg/kg, sustained receptor occupancy (≥87%), observed throughout weekly infusions up to 5 weeks after the last infusion, correlated with an estimated half-life of 4-19 d. Twelve patients (43%) had stable disease, and one patient (4%) maintained a partial response for ≥8 months. These findings indicate that single-agent Lucatumumab was well tolerated up to 4·5 mg/kg with modest clinical activity in relapsed/refractory MM, warranting further study as a combination therapy.

Phase IA/II, multicentre, open-label study of the CD40 antagonistic monoclonal antibody Lucatumumab in adult patients with advanced non-Hodgkin or Hodgkin lymphoma

Br J Haematol 2014 Jan;164(2):258-65.PMID:24219359DOI:10.1111/bjh.12630.

Despite advancements in the treatment of non-Hodgkin lymphoma (NHL) and Hodgkin lymphoma (HL), patients continue to relapse and thus a need for new targeted therapies remains. The CD40 receptor is highly expressed on neoplastic B cells and activation leads to enhanced proliferation and survival. Lucatumumab (HCD122) is a fully human antagonistic CD40 monoclonal antibody. A phase IA/II study was designed to determine the maximum tolerated dose (MTD) and activity of Lucatumumab in patients with relapsed/refractory lymphoma. Determination of the MTD was the primary objective of the phase IA dose escalation portion and clinical response was the primary objective of the phase II dose expansion portion. Patients received escalating doses of Lucatumumab administered intravenously once weekly for 4 weeks of an 8-week cycle. MTD was determined at 4 mg/kg of Lucatumumab. A total of 111 patients with NHL (n = 74) and HL (n = 37) were enrolled. Responses were observed across various lymphoma subtypes. The overall response rate by computed tomography among patients with follicular lymphoma (FL) and marginal zone lymphoma of mucosa-associated lymphatic tissue (MZL/MALT) was 33·3% and 42·9%, respectively. Lucatumumab demonstrates modest activity in relapsed/refractory patients with advanced lymphoma, suggesting that targeting of CD40 warrants further investigation.

Emerging antibodies for the treatment of multiple myeloma

Expert Opin Emerg Drugs 2016 Jun;21(2):225-37.PMID:27195659DOI:10.1080/14728214.2016.1186644.

Introduction: Monoclonal antibodies mark the beginning of a new era in the context of multiple myeloma (MM) treatment. Numerous antibodies have been tested or are currently in development for patients with MM, in order to improve tolerability and quality of life. Areas covered: This manuscript reviews emerging antibodies for the treatment of MM i.e. elotuzumab, daratumumab, MOR03087, isatuximab, bevacizumab, cetuximab, siltuximab, tocilizumab, elsilimomab, azintrel, rituximab, tositumomab, milatuzumab, Lucatumumab, dacetuzumab, figitumumab, dalotuzumab, AVE1642, tabalumab, pembrolizumab, pidilizumab, nivolumab. Expert opinion: Amongst these antibodies, elotuzumab which targets SLAMF-7 and daratumumab which targets CD38, have been recently approved by FDA for patients with relapsed/refractory MM. Both agents are well tolerated. Multiple clinical trials incorporating these monoclonal antibodies in MM treatment are currently ongoing. Of special interest are the anticipated results of phase III clinical trials with elotuzumab [NCT0189164; NCT01335399; NCT02495922] and daratumumab [NCT02252172; NCT02195479] in newly diagnosed MM patients. Moreover, of great interest are the awaited data on pembrolizumabin combination with pomalidomide and dexamethasone in refractory/relapsed MM patients [NCT02576977] and in combination with lenalidomide and dexamethasone in newly diagnosed MM patients. It seems that the incorporation of monoclonal antibodies will change the landscape of myeloma therapy in the near future.