Dupilumab
(Synonyms: 度匹鲁单抗,REGN-668; SAR-231893) 目录号 : GC60798
Dupilumab (anti-IL-4Rα) (Dupixent, REGN-668, SAR-231893) is a fully human anti–interleukin-4 receptor α monoclonal antibody that inhibits both interleukin-4 (IL-4) and interleukin-13 (IL-13) signaling through blockade of the shared IL-4α subunit.
Cas No.:1190264-60-8
Sample solution is provided at 25 µL, 10mM.
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Dupilumab (anti-IL-4Rα) (Dupixent, REGN-668, SAR-231893) is a fully human anti–interleukin-4 receptor α monoclonal antibody that inhibits both interleukin-4 (IL-4) and interleukin-13 (IL-13) signaling through blockade of the shared IL-4α subunit.
[1] Mario Castro, et al. N Engl J Med . 2018 Jun 28;378(26):2486-2496. [2] Melinda J Gooderham, et al. J Am Acad Dermatol . 2018 Mar;78(3 Suppl 1):S28-S36.
| Cas No. | 1190264-60-8 | SDF | |
| 别名 | 度匹鲁单抗,REGN-668; SAR-231893 | ||
| Canonical SMILES | [Dupilumab] | ||
| 分子式 | 分子量 | ||
| 溶解度 | 储存条件 | Store at -20°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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Dupilumab Efficacy and Safety in Moderate-to-Severe Uncontrolled Asthma
N Engl J Med 2018 Jun 28;378(26):2486-2496.PMID:29782217DOI:10.1056/NEJMoa1804092.
Background: Dupilumab is a fully human anti-interleukin-4 receptor α monoclonal antibody that blocks both interleukin-4 and interleukin-13 signaling. We assessed its efficacy and safety in patients with uncontrolled asthma. Methods: We randomly assigned 1902 patients 12 years of age or older with uncontrolled asthma in a 2:2:1:1 ratio to receive add-on subcutaneous Dupilumab at a dose of 200 or 300 mg every 2 weeks or matched-volume placebos for 52 weeks. The primary end points were the annualized rate of severe asthma exacerbations and the absolute change from baseline to week 12 in the forced expiratory volume in 1 second (FEV1) before bronchodilator use in the overall trial population. Secondary end points included the exacerbation rate and FEV1 in patients with a blood eosinophil count of 300 or more per cubic millimeter. Asthma control and Dupilumab safety were also assessed. Results: The annualized rate of severe asthma exacerbations was 0.46 (95% confidence interval [CI], 0.39 to 0.53) among patients assigned to 200 mg of Dupilumab every 2 weeks and 0.87 (95% CI, 0.72 to 1.05) among those assigned to a matched placebo, for a 47.7% lower rate with Dupilumab than with placebo (P<0.001); similar results were seen with the Dupilumab dose of 300 mg every 2 weeks. At week 12, the FEV1 had increased by 0.32 liters in patients assigned to the lower dose of Dupilumab (difference vs. matched placebo, 0.14 liters; P<0.001); similar results were seen with the higher dose. Among patients with a blood eosinophil count of 300 or more per cubic millimeter, the annualized rate of severe asthma exacerbations was 0.37 (95% CI, 0.29 to 0.48) among those receiving lower-dose Dupilumab and 1.08 (95% CI, 0.85 to 1.38) among those receiving a matched placebo (65.8% lower rate with Dupilumab than with placebo; 95% CI, 52.0 to 75.6); similar results were observed with the higher dose. Blood eosinophilia occurred after the start of the intervention in 52 patients (4.1%) who received Dupilumab as compared with 4 patients (0.6%) who received placebo. Conclusions: In this trial, patients who received Dupilumab had significantly lower rates of severe asthma exacerbation than those who received placebo, as well as better lung function and asthma control. Greater benefits were seen in patients with higher baseline levels of eosinophils. Hypereosinophilia was observed in some patients. (Funded by Sanofi and Regeneron Pharmaceuticals; LIBERTY ASTHMA QUEST ClinicalTrials.gov number, NCT02414854 .).
Dupilumab for treatment of atopic dermatitis
Expert Rev Clin Pharmacol 2018 May;11(5):467-474.PMID:29557246DOI:10.1080/17512433.2018.1449642.
Dupilumab is a new treatment option for patients with moderate-to-severe atopic dermatitis. It blocks IL-4/IL13-signaling and thereby inhibits receptor signaling downstream the JAK-STAT-pathway. Three of the main disease mechanisms of atopic dermatitis are affected by blocking this pathway; the decrease of skin barrier function, the class switch to IgE and the TH2-differentiation. Areas Covered: Dupilumab showed promising results in clinical trials of phase I-III. Clinical outcome parameters such as SCORAD, EASI, IGA and BSA improved with Dupilumab. A positive effect on patient-reported outcomes like DLQI or pruritus-rating-scales was also demonstrated. The safety profile of Dupilumab is superior to conventional immunosuppressive drugs, such as cyclosporine or methotrexate. Injection-site reactions and conjunctivitis were the most relevant side-effects. Skin infections were less frequently observed compared to placebo. Data on the use of Dupilumab during pregnancy or in children are not published to date. Expert Commentary: Dupilumab was approved by the FDA in April 2017 for the treatment of adult patients with moderate-to-severe atopic dermatitis whose disease is not adequately controlled with topical prescription therapies or when those therapies are not advisable.
Management of inadequate response and adverse effects to Dupilumab in atopic dermatitis
J Am Acad Dermatol 2022 Mar;86(3):628-636.PMID:34126094DOI:10.1016/j.jaad.2021.06.017.
Atopic dermatitis (AD) is a chronic inflammatory skin disease characterized by pruritus, skin pain, and sleep disturbances. Currently, Dupilumab is the only systemic therapy and biologic medication approved by the United States Food and Drug Administration for moderate-to-severe AD in adults and children. There is a sparsity of literature available on determining treatment failure with Dupilumab and the next steps health care providers can take to treat AD. Individual goals and quality of life and not just body surface area should be considered when defining treatment failure. Possible confounding dermatoses also should be ruled out. Early identification of dupilumab-induced adverse events is important. For most patients, Dupilumab can be continued while treatment for the adverse event is initiated. Adjusting the frequency of Dupilumab dosing also may be considered in some circumstances. Adjuvant therapies, such as methotrexate, azathioprine, mycophenolate mofetil, cyclosporine, or phototherapy can be added but the safety and efficacy of these combination treatments are not known at this time.
Dupilumab: A Review of Present Indications and Off-Label Uses
J Investig Allergol Clin Immunol 2022 Apr 19;32(2):97-115.PMID:33661102DOI:10.18176/jiaci.0682.
Recent advances in our understanding of T2 inflammation have revealed more diseases in which T2 inflammation is involved. Dupilumab is a recently developed monoclonal antibody that blocks signaling of IL-4 and IL-13, both of which are crucial cytokines in the T2 response. New possible indications are increasingly explored and include skin diseases, such as prurigo nodularis, nummular eczema, allergic contact dermatitis, chronic hand eczema, spontaneous chronic urticaria, bullous pemphigoid, alopecia areata, and Netherton syndrome, as well as respiratory diseases, such as allergic bronchopulmonary aspergillosis, chronic eosinophilic pneumonia, and allergic rhinitis. In addition, eosinophilic gastrointestinal disorders, particularly eosinophilic esophagitis, and food allergy, are also research fields of interest. Here, we review published data and clinical trials examining the use of Dupilumab in these disorders.
Dupilumab treatment in adults with moderate-to-severe atopic dermatitis
N Engl J Med 2014 Jul 10;371(2):130-9.PMID:25006719DOI:10.1056/NEJMoa1314768.
Background: Dupilumab, a fully human monoclonal antibody that blocks interleukin-4 and interleukin-13, has shown efficacy in patients with asthma and elevated eosinophil levels. The blockade by Dupilumab of these key drivers of type 2 helper T-cell (Th2)-mediated inflammation could help in the treatment of related diseases, including atopic dermatitis. Methods: We performed randomized, double-blind, placebo-controlled trials involving adults who had moderate-to-severe atopic dermatitis despite treatment with topical glucocorticoids and calcineurin inhibitors. Dupilumab was evaluated as monotherapy in two 4-week trials and in one 12-week trial and in combination with topical glucocorticoids in another 4-week study. End points included the Eczema Area and Severity Index (EASI) score, the investigator's global assessment score, pruritus, safety assessments, serum biomarker levels, and disease transcriptome. Results: In the 4-week monotherapy studies, Dupilumab resulted in rapid and dose-dependent improvements in clinical indexes, biomarker levels, and the transcriptome. The results of the 12-week study of Dupilumab monotherapy reproduced and extended the 4-week findings: 85% of patients in the Dupilumab group, as compared with 35% of those in the placebo group, had a 50% reduction in the EASI score (EASI-50, with higher scores in the EASI indicating greater severity of eczema) (P<0.001); 40% of patients in the Dupilumab group, as compared with 7% in the placebo group, had a score of 0 to 1 (indicating clearing or near-clearing of skin lesions) on the investigator's global assessment (P<0.001); and pruritus scores decreased (indicating a reduction in itch) by 55.7% in the Dupilumab group versus 15.1% in the placebo group (P<0.001). In the combination study, 100% of the patients in the Dupilumab group, as compared with 50% of those who received topical glucocorticoids with placebo injection, met the criterion for EASI-50 (P=0.002), despite the fact that patients who received Dupilumab plus glucocorticoids used less than half the amount of topical glucocorticoids used by those who received placebo plus the topical medication (P=0.16). Adverse events, such as skin infection, occurred more frequently with placebo; nasopharyngitis and headache were the most frequent adverse events with Dupilumab. Conclusions: Patients treated with Dupilumab had marked and rapid improvement in all the evaluated measures of atopic dermatitis disease activity. Side-effect profiles were not dose-limiting. (Funded by Regeneron Pharmaceuticals and Sanofi; ClinicalTrials.gov numbers, NCT01259323, NCT01385657, NCT01639040, and NCT01548404.).