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Avelumab (Anti-Human PD-L1, Human Antibody; MSB 0010718C; MSB0010718C; trade name Bavencio) is a fully human IgG1 anti-PD-L1 monoclonal antibody with potential antibody-dependent cell-mediated cytotoxicity. It is developed by Merck KGaA and Pfize as a pharmaceutical drug for use in immunotherapy, originally for the treatment of non-small-cell lung carcinoma (NSCLC). Avelumab targets the protein programmed death-ligand 1 (PD-L1). It has received orphan drug designation by the European Medicines Agency (EMA) for the treatment of gastric cancer in January 2017. The US Food and Drug Administration (FDA) approved it in March 2017 for Merkel-cell carcinoma, an aggressive type of skin cancer. The EMA approved it in September 2017 for the same indication
| ln Vitro |
Avelumab is a monoclonal antibody that is entirely human IgG1 anti-PD-L1 and has the ability to cause cell-mediated cytotoxicity that is dependent on the antibody. Avelumab causes NK-cell lysis in JHC7 cells to increase 3.1-fold (P=0.01) in comparison to the isotype control. The following cell lines show that Avelumab significantly increases NK-cell lysis in response to IFN-γ treatment: JHC7 (7.56-fold; P=0.001), UM-Chor1 (7.34-fold; P<0.001), U-CH2 (2.6 fold; P=0.008), and MUG-Chor1 (8.38-fold; P=0.0016). Avelumab efficiently and to the same extent boosts the non-cancer stem cell (CSC) and CSC subpopulations' antibody-dependent cell-mediated cytotoxicity (ADCC)[1]. The results further show that, in comparison to the isotype control in CEFT-stimulated peripheral blood mononuclear cells (PBMCs), the addition of Avelumab enhances the frequency of antigen-specific multifunctional CD8+ T cells by more than five times[2].
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| ln Vivo |
Tumor growth in the animals treated with Avelumab has clearly slowed down, as demonstrated by measurements of individual tumors. The average tumor volume of the Avelumab-treated animals decreases significantly (P<0.01) by day 36 after tumor implantation. A significant (P<0.05) increase in % survival is observed in the mice treated with Avelumab due to a long-lasting reduction in the formation of MB49 tumors. Eight of the ten mice treated with avelumab for bladder cancers showed full tumor remission, as shown by histology. Nevertheless, avelumab therapy is significantly less successful in reducing the burden of bladder tumors in animals lacking either CD4 or CD8 cells, with tumor breakthrough happening more frequently in mice without CD4 T cells[3].
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| References |
[1]. Fujii R, et al. Enhanced killing of chordoma cells by antibody-dependent cell-mediated cytotoxicity employing the novel anti-PD-L1 antibody avelumab. Oncotarget. 2016 Jun 7;7(23):33498-511.
[2]. Grenga I, et al. A fully human IgG1 anti-PD-L1 MAb in an in vitro assay enhances antigen-specific T-cell responses. Clin Transl Immunology. 2016 May 20;5(5):e83. [3]. Vandeveer AJ, et al. Systemic Immunotherapy of Non-Muscle Invasive Mouse Bladder Cancer with Avelumab, an Anti-PD-L1 Immune Checkpoint Inhibitor. Cancer Immunol Res. 2016 May;4(5):452-62 |
| Molecular Weight |
0
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| CAS # |
1537032-82-8
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| SMILES |
[Avelumab]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| Cell Assay |
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To examine the relationship between a cancer stem cell (CSC) subpopulation and antibody-dependent cell-mediated cytotoxicity (ADCC) activity,UM-Chor1 cellsare left untreated or treated with 50 ng/mL of IFN-γ for 24 h. Cells are then plated as targets at 50,000 cells/well in 6-well round-bottom culture plates and incubated with2 μg/mL of Avelumabat room temperaturefor 30 min. NK cells are added at 2500,000 cells/well at an effector-to-target (E:T) ratio of 50:1. After 4 h, tumor cells are harvested and stained with antibodies for flow cytometry[1]. |
| Animal Administration |
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Female C57BL/6 miceare used in this study. Subcutaneous tumor injections are carried out by inoculating C57BL/6 mice with 1×105MB49 parental cells on the right shaved flank. Tumor growth is measured with calipers and 8 days post-inoculation mice are assigned to treatment groups. Tumor-bearing mice are treated withAvelumab(400 µg per 100 µL) and injected i.p.three times,3 days apart. Since Avelumab is a human IgG1, three injections have to be compressed within a7 to 9 daywindow (i.e., days 9, 12, and 15 post-tumor inoculation) to avoid the onset of neutralizing mouse anti-human Ig[3]. |
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