Tiragolumab
目录号 : GC68355Tiragolumab 是一种与 T 细胞免疫球蛋白和 ITIM 结构域 (TIGIT) 结合的免疫检查点抑制剂。Tiragolumab 单独或与 PD-L1 抑制剂 Atezolizumab 联合使用，可能对多种实体恶性肿瘤有效，尤其是非小细胞肺癌。
Cas No.:1918185-84-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Tiragolumab is an immune checkpoint inhibitor binding to T-cell immunoglobulin and ITIM domain (TIGIT). Tiragolumab, alone or in combination with the PD-L1 inhibitor Atezolizumab, may be effective against multiple solid malignancies-most notably non-small cell lung cancer[1][2].
[1]. Mohammed Sqalli Houssaini, et al. Advances in the management of non-small cell lung cancer (NSCLC): A new practice changing data from asco 2020 annual meeting. Cancer Treat Res Commun. 2020;25:100239.
[2]. Tiragolumab Impresses in Multiple Trials. Cancer Discov. 2020 Aug;10(8):1086-1087.
| Cas No. | 1918185-84-8 | SDF | Download SDF |
| 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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Tiragolumab plus atezolizumab versus placebo plus atezolizumab as a first-line treatment for PD-L1-selected non-small-cell lung cancer (CITYSCAPE): primary and follow-up analyses of a randomised, double-blind, phase 2 study
Lancet Oncol 2022 Jun;23(6):781-792.PMID:35576957DOI:10.1016/S1470-2045(22)00226-1.
Background: Targeted inhibition of the PD-L1-PD-1 pathway might be further amplified through combination of PD-1 or PD-L1 inhibitors with novel anti-TIGIT inhibitory immune checkpoint agents, such as Tiragolumab. In the CITYSCAPE trial, we aimed to assess the preliminary efficacy and safety of Tiragolumab plus atezolizumab (anti-PD-L1) therapy as first-line treatment for non-small-cell lung cancer (NSCLC). Methods: CITYSCAPE is a phase 2, randomised, double-blind, placebo-controlled trial. Patients with chemotherapy-naive, PD-L1-positive (defined as a tumour proportion score of ≥1% by 22C3 immunohistochemistry pharmDx assay; Dako, Agilent Technologies, Santa Clara, CA, USA) recurrent or metastatic NSCLC with measurable disease, Eastern Cooperative Oncology Group performance status of 0 or 1, and no EGFR or ALK alterations were enrolled from 41 clinics in Europe, Asia, and the USA. Patients were randomly assigned (1:1), via an interactive voice or web-based response system, to receive Tiragolumab (600 mg) plus atezolizumab (1200 mg) or placebo plus atezolizumab intravenously once every 3 weeks. Investigators and patients were masked to treatment assignment. The co-primary endpoints were investigator-assessed objective response rate and progression-free survival as per Response Evaluation Criteria in Solid Tumors version 1.1 in the intention-to-treat population, analysed after approximately 80 progression-free survival events had been observed in the primary population. Safety was assessed in all patients who received at least one dose of study drug. This trial is registered with ClinicalTrials.gov, NCT03563716, and is ongoing. Findings: Patients were enrolled between Aug 10, 2018, and March 20, 2019. At data cutoff for the primary analysis (June 30, 2019), 135 of 275 patients assessed for eligibility were randomly assigned to receive Tiragolumab plus atezolizumab (67 [50%]) or placebo plus atezolizumab (68 [50%]). In this primary analysis, after a median follow-up of 5·9 months (4·6-7·6, in the intention-to-treat population, 21 patients (31·3% [95% CI 19·5-43·2]) in the Tiragolumab plus atezolizumab group versus 11 patients (16·2% [6·7-25·7]) in the placebo plus atezolizumab group had an objective response (p=0·031). Median progression-free survival was 5·4 months (95% CI 4·2-not estimable) in the Tiragolumab plus atezolizumab group versus 3·6 months (2·7-4·4) in the placebo plus atezolizumab group (stratified hazard ratio 0·57 [95% CI 0·37-0·90], p=0·015). 14 (21%) patients receiving Tiragolumab plus atezolizumab and 12 (18%) patients receiving placebo plus atezolizumab had serious treatment-related adverse events. The most frequently reported grade 3 or worse treatment-related adverse event was lipase increase (in six [9%] patients in the Tiragolumab plus atezolizumab group vs two [3%] in the placebo plus atezolizumab group). Two treatment-related deaths (of pyrexia and infection) occurred in the Tiragolumab plus atezolizumab group. Interpretation: Tiragolumab plus atezolizumab showed a clinically meaningful improvement in objective response rate and progression-free survival compared with placebo plus atezolizumab in patients with chemotherapy-naive, PD-L1-positive, recurrent or metastatic NSCLC. Tiragolumab plus atezolizumab was well tolerated, with a safety profile generally similar to that of atezolizumab alone. These findings demonstrate that Tiragolumab plus atezolizumab is a promising immunotherapy combination for the treatment of previously untreated, locally advanced unresectable or metastatic NSCLC. Funding: F Hoffmann-La Roche and Genentech.
Tiragolumab Results Cast Shadow on TIGIT Pipeline
Cancer Discov 2022 Jul 6;12(7):1603-1604.PMID:35652612DOI:10.1158/2159-8290.CD-NB2022-0040.
Genentech's TIGIT-targeted antibody Tiragolumab missed its endpoints in two late-stage lung cancer trials, raising doubts about one of the most widely studied next-generation checkpoint targets in immuno-oncology. But numerical signs of benefit among certain patients with metastatic non-small cell lung cancer suggest that TIGIT blockade still has potential-if drug developers can successfully identify the best indications, drug combinations, or patient populations.
Tiragolumab (Anti-TIGIT) in SCLC: Skyscraper-02, a Towering Inferno
Lung Cancer (Auckl) 2023 Jan 5;14:1-9.PMID:36636263DOI:10.2147/LCTT.S379389.
Small cell lung cancer (SCLC) is characterized by rapid progression and poor prognosis. Although the phase II CITYSCAPE-02 trial found objective response rate (ORR) and progression-free survival (PFS) of non-small cell lung cancer (NSCLC) patients improved when Tiragolumab was added to atezolizumab and chemotherapy, the phase III SKYSCRAPER-02 failed to find PFS or OS benefit in patients with SCLC. Atezolizumab was the first immunotherapy to show survival benefit in extensive SCLC based on the phase III IMpower133 study. Given that immunotherapy has become the standard of care for SCLC patients, further research is needed into ways to augment the immune system to better treat these patients.
TIGIT/CD226 Axis Regulates Anti-Tumor Immunity
Pharmaceuticals (Basel) 2021 Feb 28;14(3):200.PMID:33670993DOI:10.3390/ph14030200.
Tumors escape immune surveillance by inducing various immunosuppressive pathways, including the activation of inhibitory receptors on tumor-infiltrating T cells. While monoclonal antibodies (mAbs) blocking programmed cell death 1 (PD-1), programmed death-ligand 1 (PD-L1), and cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) have been approved for multiple cancer indications, only a subset of patients benefit from immune checkpoint blockade therapies, highlighting the need for additional approaches. Therefore, the identification of new target molecules acting in distinct or complementary pathways in monotherapy or combination therapy with PD-1/PD-L1 blockade is gaining immense interest. T cell immunoreceptor with Ig and immunoreceptor tyrosine-based inhibitory motif (ITIM) domains (TIGIT) has received considerable attention in cancer immunotherapy. Recently, anti-TIGIT mAb (Tiragolumab) has demonstrated promising clinical efficacy in non-small cell lung cancer treatment when combined with an anti-PD-L1 drug (Tecentriq), leading to phase III trial initiation. TIGIT is expressed mainly on T and natural killer cells; it functions as an inhibitory checkpoint receptor, thereby limiting adaptive and innate immunity. CD226 competes for binding with the same ligands with TIGIT but delivers a positive stimulatory signal to the immune cells. This review discusses the recent discoveries regarding the roles of TIGIT and CD226 in immune cell function and their potential application in cancer immunotherapy.
Tiragolumab Impresses in Multiple Trials
Cancer Discov 2020 Aug;10(8):1086-1087.PMID:32576590DOI:10.1158/2159-8290.CD-NB2020-063.
The TIGIT inhibitor Tiragolumab, alone or in combination with the PD-L1 inhibitor atezolizumab, may be effective against solid cancers. In phase I and II trials, the agent achieved statistically significant results in multiple solid malignancies-most notably non-small cell lung cancer.