Sugemalimab
(Synonyms: 舒格利单抗) 目录号 : GC65580
Sugemalimab 是一种完整的人全长抗程序性死亡配体 1 (PD-L1) 免疫球蛋白 G4 (IgG4) 单克隆抗体 (mAb)。Sugemalimab 显示出抗癌活性，可用于非小细胞肺癌的研究。
Cas No.:2256084-03-2
Sample solution is provided at 25 µL, 10mM.
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Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research[1].
Sugemalimab (CS1001) specifically binds to PD-L1, competitively blocks the binding of human PD-L1 with PD-1 and CD80, and effectively induces CD4+ T lymphocyte proliferation and enhances the production of interferon-γ and interleukin-2[2].Sugemalimab employs IgG4 isotype and lacks antibody-dependent cellular mediated cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC)[2].
Sugemalimab (CS1001) signifcantly inhibits tumor growth in the subcutaneous MC38-hPD-L1 murine colon carcinoma (murine MC38 cells expressing human PD-L1) in human PD-1 knock-in mouse model[2].Sugemalimab not only enhances the cytotoxic T cell/regulatory T cell ratio, but also significantly upregulates M1 macrophage and down-regulated MDSC (myeloid-derived suppressor cells) population in D-1/PD-L1 dual knock-in mice implanted with MC38-hPD-L1 tumor[2].
[1]. Dhillon S, et al. Sugemalimab: First Approval. Drugs. 2022 Apr;82(5):593-599.
[2]. Zhang J, et al. The preclinical characterization of CS1001, an anti-PD-L1 IgG4 monoclonal antibody and its activity beyond T cell regulation. Cancer Research, 2020, 80(16_Supplement): 3260-3260.
| Cas No. | 2256084-03-2 | SDF | Download SDF |
| 别名 | 舒格利单抗 | ||
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
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每只动物给药体积 | ul | |
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Sugemalimab versus placebo after concurrent or sequential chemoradiotherapy in patients with locally advanced, unresectable, stage III non-small-cell lung cancer in China (GEMSTONE-301): interim results of a randomised, double-blind, multicentre, phase 3 trial
Lancet Oncol 2022 Feb;23(2):209-219.PMID:35038429DOI:10.1016/S1470-2045(21)00630-6.
Background: A substantial proportion of patients with unresectable stage III non-small-cell lung cancer (NSCLC) cannot either tolerate or access concurrent chemoradiotherapy, so sequential chemoradiotherapy is commonly used. We assessed the efficacy and safety of Sugemalimab, an anti-PD-L1 antibody, in patients with stage III NSCLC whose disease had not progressed after concurrent or sequential chemoradiotherapy. Methods: GEMSTONE-301 is a randomised, double-blind, placebo-controlled, phase 3 trial in patients with locally advanced, unresectable, stage III NSCLC, done at 50 hospitals or academic research centres in China. Eligible patients were aged 18 years or older with an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1 who had not progressed after concurrent or sequential chemoradiotherapy. We randomly assigned patients (2:1, using an interactive voice-web response system) to receive Sugemalimab 1200 mg or matching placebo, intravenously every 3 weeks for up to 24 months. Stratification factors were ECOG performance status, previous chemoradiotherapy, and total radiotherapy dose. The investigators, trial coordination staff, patients, and study sponsor were masked to treatment allocation. The primary endpoint was progression-free survival as assessed by blinded independent central review (BICR) in the intention-to-treat population. Safety was assessed in all participants who received at least one dose of assigned study treatment. The study has completed enrolment and the results of a preplanned analysis of the primary endpoint are reported here. The trial is registered with ClinicalTrials.gov, NCT03728556. Findings: Between Aug 30, 2018 and Dec 30, 2020, we screened 564 patients of whom 381 were eligible. Study treatment was received by all patients randomly assigned to Sugemalimab (n=255) and to placebo (n=126). At data cutoff (March 8, 2021), median follow-up was 14·3 months (IQR 6·4-19·4) for patients in the Sugemalimab group and 13·7 months (7·1-18·4) for patients in the placebo group. Progression-free survival assessed by BICR was significantly longer with Sugemalimab than with placebo (median 9·0 months [95% CI 8·1-14·1] vs 5·8 months [95% CI 4·2-6·6]; stratified hazard ratio 0·64 [95% CI 0·48-0·85], p=0·0026). Grade 3 or 4 treatment-related adverse events occurred in 22 (9%) of 255 patients in the Sugemalimab group versus seven (6%) of 126 patients in the placebo group, the most common being pneumonitis or immune-mediated pneumonitis (seven [3%] of 255 patients in the Sugemalimab group vs one [<1%] of 126 in the placebo group). Treatment-related serious adverse events occurred in 38 (15%) patients in the Sugemalimab group and 12 (10%) in the placebo group. Treatment-related deaths were reported in four (2%) of 255 patients (pneumonia in two patients, pneumonia with immune-mediated pneumonitis in one patient, and acute hepatic failure in one patient) in the Sugemalimab group and none in the placebo group. Interpretation: Sugemalimab after definitive concurrent or sequential chemoradiotherapy could be an effective consolidation therapy for patients with stage III NSCLC whose disease has not progressed after sequential or concurrent chemoradiotherapy. Longer follow-up is needed to confirm this conclusion. Funding: CStone Pharmaceuticals and the National Key Research and Development Program of China. Translation: For the Chinese translation of the abstract see Supplementary Materials section.
Sugemalimab versus placebo, in combination with platinum-based chemotherapy, as first-line treatment of metastatic non-small-cell lung cancer (GEMSTONE-302): interim and final analyses of a double-blind, randomised, phase 3 clinical trial
Lancet Oncol 2022 Feb;23(2):220-233.PMID:35038432DOI:10.1016/S1470-2045(21)00650-1.
Background: PD-1 inhibitor plus chemotherapy had been shown to be an effective first-line treatment for patients with metastatic non-small-cell lung cancer (NSCLC). However, there was no robust evidence showing a PD-L1 inhibitor combined with chemotherapy benefited patients with squamous and non-squamous NSCLC. GEMSTONE-302 aimed to evaluate the efficacy and safety of a PD-L1 inhibitor, Sugemalimab, plus chemotherapy for patients with metastatic squamous or non-squamous NSCLC. Methods: This randomised, double-blind, phase 3 trial was done in 35 hospitals and academic research centres in China. Eligible patients were aged 18-75 years, had histologically or cytologically confirmed stage IV squamous or non-squamous NSCLC without known EGFR sensitising mutations, ALK, ROS1, or RET fusions, no previous systemic treatment for metastatic disease, and an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1. Patients were randomly assigned (2:1) to receive Sugemalimab (1200 mg, intravenously, every 3 weeks) plus platinum-based chemotherapy (carboplatin [area under the curve (AUC) 5 mg/mL per min, intravenously] and paclitaxel [175 mg/m2, intravenously] for squamous NSCLC, or carboplatin [AUC 5 mg/mL per min, intravenously] and pemetrexed [500 mg/m2, intravenously] for non-squamous NSCLC; Sugemalimab group) or placebo plus the same platinum-based chemotherapy regimens for squamous or non-squamous NSCLC as in the Sugemalimab group; placebo group) for up to four cycles, followed by maintenance therapy with Sugemalimab or placebo for squamous NSCLC, and intravenous Sugemalimab 500 mg/m2 or matching placebo plus pemetrexed for non-squamous NSCLC. Randomisation was done by an interactive voice-web-response system via permuted blocks (block size was a mixture of three and six with a random order within each stratum) and stratified by ECOG performance status, PD-L1 expression, and tumour pathology. The investigators, patients, and the sponsor were masked to treatment assignment. The primary endpoint was investigator-assessed progression-free survival in the intention-to-treat population. Safety was analysed in all patients who received at least one treatment dose. Results reported are from a prespecified interim analysis (ie, when the study met the primary endpoint) and an updated analysis (prespecified final analysis for progression-free survival) with a longer follow-up. This study is registered with ClinicalTrials.gov (NCT03789604), is closed to new participants, and follow-up is ongoing. Findings: Between Dec 13, 2018, and May 15, 2020, 846 patients were assessed for eligibility; 367 were ineligible, and the remaining 479 patients were randomly assigned to the Sugemalimab group (n=320) or placebo group (n=159). At the preplanned interim analysis (data cutoff June 8, 2020; median follow-up 8·6 months [IQR 6·1-11·4]), GEMSTONE-302 met its primary endpoint, with significantly longer progression-free survival in the Sugemalimab group compared with the placebo group (median 7·8 months [95% CI 6·9-9·0] vs 4·9 months [4·7-5·0]; stratified hazard ratio [HR] 0·50 [95% CI 0·39-0·64], p<0·0001]). At the final analysis (March 15, 2021) with a median follow-up of 17·8 months (IQR 15·1-20·9), the improvement in progression-free survival was maintained (median 9·0 months [95% CI 7·4-10·8] vs 4·9 months [4·8-5·1]; stratified HR 0·48 [95% CI 0·39-0·60], p<0·0001). The most common grade 3 or 4 any treatment-related adverse events were neutrophil count decreased (104 [33%] of 320 with Sugemalimab vs 52 [33%] of 159 with placebo), white blood cell count decreased (45 [14%] vs 27 [17%]), anaemia (43 [13%] vs 18 [11%]), platelet count decreased (33 [10%] vs 15 [9%]), and neutropenia (12 [4%] vs seven [4%]). Any treatment-related serious adverse events occurred in 73 (23%) patients in the Sugemalimab group and 31 (20%) patients in the placebo group. Any treatment-related deaths were reported in ten (3%) patients in the Sugemalimab group (pneumonia with respiratory failure in one patient; myelosuppression with septic shock in one patient; pneumonia in two patients; respiratory failure, abdominal pain, cardiac failure, and immune-mediated pneumonitis in one patient each; the other two deaths had an unspecified cause) and in two (1%) patients in the placebo group (pneumonia and multiple organ dysfunction syndrome). Interpretation: Sugemalimab plus chemotherapy showed a statistically significant and clinically meaningful progression-free survival improvement compared with placebo plus chemotherapy, in patients with previously untreated squamous and non-squamous metastatic NSCLC, regardless of PD-L1 expression, and could be a newfirst-line treatment option for both squamous and non-squamous metastatic NSCLC. Funding: CStone Pharmaceuticals. Translation: For the Chinese translation of the abstract see Supplementary Materials section.
Sugemalimab: First Approval
Drugs 2022 Apr;82(5):593-599.PMID:35298827DOI:10.1007/s40265-022-01693-4.
Sugemalimab (Cejemly® in China) is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb) that is being developed by CStone Pharmaceuticals for the treatment of advanced solid tumours and lymphoma. In December 2021, Sugemalimab was approved in China for the first-line treatment of epidermal growth factor receptor (EGFR) gene mutation and anaplastic lymphoma kinase (ALK) negative metastatic non-small cell lung cancer (NSCLC) administered in combination with pemetrexed and carboplatin for non-squamous NSCLC and in combination with paclitaxel and carboplatin for squamous NSCLC. Sugemalimab is under regulatory review as consolidation treatment in patients with stage III NSCLC in China. Clinical studies assessing Sugemalimab for the treatment of several other cancers, including liver cancer, gastric cancer, oesophageal cancer, Hodgkin lymphoma and extranodal natural killer/T cell lymphoma are underway in China, the US and Australia. This article summarizes the milestones in the development of Sugemalimab leading to this first approval for the first-line treatment of EGFR gene mutation and ALK-negative metastatic NSCLC.
Sugemalimab, a novel PD-L1 inhibitor for treatment of advanced or metastatic non-small cell lung cancer
Drugs Today (Barc) 2023 Mar;59(3):169-177.PMID:36847625DOI:10.1358/dot.2023.59.3.3507759.
Nearly two-thirds of patients with non-small cell lung cancer (NSCLC) have locally advanced or metastatic disease at the time of diagnosis, and many patients with early-stage disease will eventually experience metastatic recurrence. In the absence of a known driver alteration, treatment of metastatic NSCLC is limited to immunotherapy with or without cytotoxic chemotherapy. For most patients with locally advanced unresectable NSCLC, the standard of care involves concurrent chemoradiation followed by consolidative immunotherapy. Several immune checkpoint inhibitors have been developed and approved for NSCLC in both the metastatic and adjuvant settings. This review will discuss Sugemalimab, a novel programmed cell death 1 ligand 1 (PD-L1) inhibitor, for the treatment of advanced NSCLC.
Cost-effectiveness analysis of Sugemalimab vs. chemotherapy as first-line treatment of metastatic nonsquamous non-small cell lung cancer
Front Pharmacol 2022 Sep 12;13:996914.PMID:36172187DOI:10.3389/fphar.2022.996914.
Objective: Sugemalimab is approved in China as a first-line treatment in combination with chemotherapy for metastatic nonsquamous non-small cell lung cancer (NSCLC). This study aims to evaluate the cost-effectiveness of first-line additional Sugemalimab in combination with chemotherapy vs. chemotherapy from the perspective of the Chinese healthcare system. Materials and methods: A three-state Markov model was designed to evaluate the costs and quality-adjusted life years (QALYs) of first-line Sugemalimab combination with chemotherapy vs. chemotherapy over a 10-year period. Data on clinical outcomes were obtained from GEMSTONE-302 clinical trials. Costs and health utilities were collected from local databases and published literature. The uncertainty of the model parameters was explored through sensitivity analysis. Results: Compared to chemotherapy, Sugemalimab treatment for NSCLC resulted in an extra 0.50 QALYs at an additional cost of $73627.99, with an incremental cost-effectiveness ratio (ICER) of 148354.07/QALY at the willingness-to-pay (WTP) threshold of $37663.26/QALY. One-way sensitivity analysis indicated that the primary motivator in this model was the cost of Sugemalimab. However, none of the parameters significantly affected the model's results. Conclusion: Sugemalimab combination therapy is not economically advantageous for the first-line management of metastatic non-squamous NSCLC, according to the Chinese healthcare system.