Sino Biopharmaceutical Co., Ltd · 小分子 · 小分子
eribulin mesilate 是一种小分子，由Sino Biopharmaceutical Co., Ltd研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)。
| 商品名 | Ailelin |
| 公司 | Sino Biopharmaceutical Co., Ltd |
| 药物类别 | 小分子 |
| 给药途径 | Injectable (Others) |
| 状态 | Approved |
eribulin mesilate 针对 1 个适应症，涉及 1 个治疗领域。
| 治疗领域 | 疾病/病症 | 分期 |
|---|---|---|
| Neoplasms benign, malignant and unspecified (incl cysts and polyps) | Breast cancer | ✓ Approved |
Ni Mengqian M, Zhou Lijia L, Zhang Lulu L, Su Yanhong Y et al.
Li Gaojin G, Zhong Delian D, Chen Jingjing J, Ju Jianjie J et al.
Extracorporeal membrane oxygenation (ECMO) and continuous renal replacement therapy (CRRT) require a balance between maintaining circuit patency and minimizing bleeding risk. Nafamostat mesilate (NM) is a short-acting anticoagulant with distinctive pharmacokinetic properties, including rapid metabolism and a short half-life, which may reduce prolonged systemic anticoagulant exposure. These characteristics make NM a potential alternative to conventional anticoagulation strategies, particularly for patients at high risk of bleeding. This study aimed to systematically evaluate the efficacy and safety of NM as an anticoagulant for ECMO/CRRT. PubMed, Embase, the Cochrane Library, China National Knowledge Infrastructure, and Wanfang Data were systematically searched for randomized controlled trials and cohort studies comparing NM with sodium citrate, unfractionated heparin (UFH), or no anticoagulation. A meta-analysis was conducted to evaluate filter lifespan, bleeding events, thromboembolic events, and 28-day/intensive care unit (ICU) mortality. Reporting characteristics and potential safety signals for the three anticoagulants were also compared using data from the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS). The meta-analysis included 17 studies involving 1,893 patients. Filter lifespan did not differ significantly between the NM and control groups (mean difference [MD] = 1.29 h; 95% confidence interval [CI], -1.09-3.66), whereas the risk of bleeding events was significantly lower in the NM group (odds ratio [OR] = 0.61; 95% CI, 0.43-0.86). Subgroup analyses showed that NM was associated with a significantly lower risk of bleeding than sodium citrate (OR = 0.53; 95% CI, 0.31-0.90) and no anticoagulation (OR = 0.41; 95% CI, 0.19-0.90); sensitivity analyses supported the robustness of this finding. The FAERS analysis included 24,238 reports, comprising 233 for NM, 1,612 for sodium citrate, and 22,393 for UFH, with distinct reporting profiles observed among the three anticoagulants. Representative signals for NM included disseminated intravascular coagulation (n = 17; ROR = 112.68, 95% CI: 69.69-182.19), gastrointestinal hemorrhage (n = 12; ROR = 15.44, 95% CI: 8.74-27.29), and decreased platelet count (n = 13; ROR = 7.52, 95% CI: 4.35-13.00). NM may reduce bleeding risk while maintaining a filter lifespan comparable to that achieved with other anticoagulation strategies, potentially providing an individualized anticoagulation option for patients at high risk of bleeding. In clinical practice, coagulation abnormalities, changes in platelet counts, and bleeding-related events should be closely monitored.
Kobayashi Megumi M, Miyamoto Ei E, Morimura Yuki Y, Ohsumi Yuki Y et al.
Myxofibrosarcoma is a malignant soft tissue tumor of fibroblastic origin, occurring mainly in the extremities but extremely rarely in the thoracic trunk. Myxofibrosarcoma typically appears as a slow-growing, painless mass but features a frequent local recurrence due to microscopic extension beyond visible margins. On MRI, the "tail sign"-which indicates subtle spread along the fascial plane-is known to be a potential risk factor for recurrence. The patient was a 73-year-old woman complaining of continuous right back pain. Chest CT showed a poorly contrast-enhanced mass involving the 5th and 6th right ribs, as well as a separate nodule. The biopsy confirmed a diagnosis of myxofibrosarcoma. The mass exhibited hypointensity on T1-weighted images and hyperintensity on T2-weighted images on MRI; on contrast-enhanced T1-weighted images and STIR images, a tail sign extending toward a small satellite nodule was observed. The patient underwent an extended resection involving the 5th through 7th ribs. A total of 61.2 Gy radiation was irradiated to the paravertebral region neighboring the tumor where the surgical margin was poor. A local recurrence was detected in the anterolateral region of the tumor resection site 5 months after surgery. The patient was treated with sequential chemotherapy using doxorubicin, eribulin, and pazopanib and is alive at 26 months after surgery without distant metastasis. The current case exemplifies the aggressive local behavior of thoracic myxofibrosarcoma, especially when a long tail sign appears.
Wang Congcong C, Xu Lulu L, Han Hao H, Sun Ping P et al.
Metastatic triple-negative breast cancer (mTNBC) is an aggressive malignancy with limited targeted therapeutic alternatives and dismal long-term prognosis. Sacituzumab govitecan (SG) is a Trop-2-directed antibody-drug conjugate (ADC) conjugated to the topoisomerase I inhibitor SN-38. SG has demonstrated robust anti-tumor activity across multiple clinical trials for mTNBC. We present a hypothesis-generating case report of a 50-year-old female patient with stage III triple-negative breast cancer (TNBC) who received curative-intent surgery followed by adjuvant multimodal therapy. Fourteen months after completing adjuvant treatment, the patient developed bone-only recurrence and received local bone radiotherapy plus first-line albumin-bound paclitaxel plus carboplatin chemotherapy, followed by capecitabine maintenance until 25 April 2023. Upon successive systemic disease progression, the patient sequentially received second-line toripalimab plus gemcitabine and third-line toripalimab plus eribulin through November 2023. Cervical lymph node biopsy confirmed metastatic TNBC with negative BRCA germline status and PD-L1 tumor proportion score (TPS) < 1%. Per international and domestic clinical guidelines, single-agent SG (10 mg/kg) was initiated as fourth-line therapy. During SG monotherapy, recurrent symptomatic malignant pleural effusion developed, and oral anlotinib 10 mg (days 1-14 every 21-day cycle) was added to the treatment regimen starting 18 July 2024. As of 4 February 2025, the patient completed 7 cycles of SG monotherapy and 9 cycles of sequential SG plus anlotinib combination treatment. Clinically, no recurrent pleural effusion was observed after anlotinib initiation; measurable pulmonary, hepatic, and cervical nodal metastases exhibited sustained shrinkage alongside declining serum tumor markers, yielding a 12-month progression-free survival (PFS). Grade 1-2 treatment-emergent adverse events included leukopenia, neutropenia, diarrhea, and fatigue, all manageable with supportive care. To our knowledge, this is the first descriptive case documenting sustained disease control following SG plus anlotinib combination in heavily pretreated mTNBC complicated by recurrent malignant pleural effusion. It should also be noted that although the timing of clinical symptom improvement coincided with the initiation of anlotinib, this single case cannot differentiate whether the clinical benefit observed derived from the potential synergistic effect of the two agents or the monotherapeutic effect of anlotinib alone. Without validation from phase II/III prospective clinical trials, this case only generates a preliminary hypothesis that SG combined with anlotinib may represent a potential salvage therapeutic strategy for heavily pretreated advanced TNBC patients complicated by refractory malignant pleural effusion or localized progression under single-agent SG. Further prospective clinical research is required to verify the synergistic activity of this regimen.
Nakamura Makiko M, Imamura Teruhiko T, Nakagaito Masaki M, Izumida Toshihide T et al.
Nafamostat mesilate (NM), a synthetic serine protease inhibitor, has been used as an anticoagulant in patients undergoing extracorporeal circulatory support who have bleeding or heparin-related adverse effects. The safety and efficacy of NM-based anticoagulation in patients receiving Impella support who develop bleeding or thrombocytopenia remain uncertain. Patients who underwent Impella placement without prior cardiopulmonary resuscitation between 2018 and 2026 at our institution were included. In January 2024, the anticoagulation strategy for patients with bleeding or thrombocytopenia was revised to incorporate NM alone or in combination with low-dose heparin, with selective use of a bicarbonate-based purge solution. Differences in 30-day mortality and survival to discharge between the early era (2018-2023) and the late era (2024-2026) were retrospectively evaluated. A total of 97 patients (median age 70 years; 64% male) were analyzed. The daily amount of transfused red blood cell products during Impella support was significantly lower in the late era (0.8 versus 1.8 units, p = 0.024). 30-day mortality was significantly lower, and survival to discharge was significantly higher in the late era (p < 0.05 for both). Multivariable logistic regression analysis showed that the late era was significantly associated with a higher likelihood of survival to discharge, with an odds ratio of 32.46 (95% confidence interval 4.28-756.14, p < 0.001). The late era, during which a revised anticoagulation strategy incorporating NM and selective use of a bicarbonate-based purge solution was implemented, was associated with lower daily red blood cell transfusion requirements and higher survival to discharge.
Feng Chaoyang C, Wu Chenglong C, Heng Xiaojie X, Wang Shouping S et al.
Maleimide-based conjugation, the predominant strategy in approved antibody-drug conjugates (ADCs), is susceptible to retro-Michael deconjugation, resulting in premature transfer of the linker-payload moiety to serum proteins rather than free payload release and reduced therapeutic index. Here, we report SuperHydra, a self-hydrolyzing maleimide linker that undergoes rapid post-conjugation ring-opening hydrolysis to irreversibly stabilize the thiosuccinimide linkage and suppress retro-Michael deconjugation. Incorporation of SuperHydra into the HER2-targeting ADC SMP-656, comprising the antibody Inetetamab and the microtubule inhibitor Eribulin, resulted in markedly enhanced plasma stability while preserving HER2 binding, internalization, Fc-mediated effector function, and bystander killing. SMP-656 exhibited potent antigen-dependent cytotoxicity, retained activity in DS-8201a-resistant tumor models, and achieved durable antitumor efficacy in multiple HER2-positive xenograft models. In cynomolgus monkeys, SMP-656 demonstrated favorable pharmacokinetic properties and an acceptable safety profile. Collectively, these findings establish SMP-656 as a promising HER2-targeting ADC, support its ongoing clinical evaluation in HER2-expressing solid tumors, and highlight the potential of the SuperHydra linker as a versatile platform for improving the stability and overall performance of maleimide-based ADCs.
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