新型口服SERD TFX06：在氟维司群经治进展与脑转移的ER /HER2-晚期乳腺癌中展现卓越潜力
在近期举办的2025年美国圣安东尼奥乳腺癌研讨会（SABCS2025， 12月9号-12号）上，浙江扬厉医药(VyBio)自主研发的新一代口服SERD TFX06片Ⅰ/Ⅱ期临床研究（NCT05927779）公布了最新的数据。该研究结果显示，TFX06不仅在多线治疗后的ER+/HER2-晚期乳腺癌患者中表现出良好的安全性与系统性疗效，更在氟维司群经治进展人群以及脑转移患者中展现出令人鼓舞的治疗优势，为临床难治性乳腺癌患者提供了新的希望。
整体疗效确切，为末线患者提供持续的新的内分泌疗法获益
截至2025年07月28日，TFX06在150mg推荐剂量(RP2D)下纳入57例既往经过多线治疗的患者，并显示出明确的疗效：
· 所有患者的中位无进展生存期（mPFS）为5.5个月，6个月无进展生存率为43.1%；
· 在携带ESR1突变的患者中，mPFS延长至5.7个月，提示TFX06对现有内分泌疗法耐药患者具有治疗潜力。
这些数据表明，无论是否患者携带ESR1m，TFX06均能为多线治疗后的晚期乳腺癌患者提供具有临床意义的疾病控制和生存获益。
直面临床难点：氟维司群经治进展人群仍可获益
在晚期乳腺癌治疗中，既往接受过氟维司群治疗进展的患者往往面临后续治疗选择有限、疗效欠佳的困境。本项研究中，150mg推荐剂量组有56.1%的患者曾接受氟维司群治疗，61.4%的患者接受CDK4/6抑制剂治疗，其中超过三分之一（38.6%）更是经历过氟维司群联合CDK4/6抑制剂治疗后出现了疾病进展。TFX06在这一高度难治的人群中仍显示出明确的临床活性：
· 在21例既往接受氟维司群联合CDK4/6抑制剂治疗进展的患者中，临床获益率（CBR）达到42.9%；
· 在伴有ESR1突变的患者中，获益更为明显，CBR提升至55.6%，中位无进展生存期（mPFS）达5.6个月。
这提示TFX06对比同类口服SERD能够为氟维司群经治后进展的患者提供持续有效的疾病控制。
突破治疗壁垒：在脑转移患者中展现卓越颅内活性
ER-阳性/HER2-阴性乳腺癌脑转移是晚期乳腺癌治疗中的严峻挑战，传统内分泌药物疗效有限。TFX06在此方面取得了突破性进展：
· 在8例可评估的脑转移患者中，客观缓解率（ORR）高达37.5%，疾病控制率（DCR）为87.5%，临床获益率（CBR）达到75%；
· 患者的中位无进展生存期（mPFS）为7.6个月，显著优于整体研究人群；
· 影像学评估证实，部分患者的颅内靶病灶缩小超过70%，甚至达到完全缓解，证明了TFX06具有穿透血脑屏障、抑制颅内肿瘤生长的能力。同类口服SERD尚未有影像学证据报道。
安全性良好，保障治疗持续性
TFX06在临床应用中表现出良好的安全性和耐受性。最常见的不良反应为1-2级的血液指标异常，易于管理。胃肠道反应（如恶心、腹泻）以及心脏毒性（如窦性心动过缓）的发生率较低，无眼部不良反应（如闪光幻视）报道，为患者长期用药提供了重要的安全保障。
关于TFX06
TFX06是浙江扬厉医药自主研发的一款第三代口服选择性雌激素受体降解剂（SERD），属于新一代口服内分泌疗法，有效克服ESR1m突变带来现有内分泌疗法耐药的困境，旨在为ER-阳性/HER2-阴性乳腺癌患者提供更有效的更安全的创新疗法，而不影响患者的生活质量。目前，TFX06单药及联合CDK4/6抑制剂或依维莫司的临床研究正在积极推进中。
浙江扬厉医药(VyBio)致力于肿瘤及慢性病创新药物的研发，以满足未被满足的临床需求。TFX06在难治性乳腺癌患者、尤其是脑转移患者中展现的潜力，坚定了我们为全球患者带来更有效治疗选择的使命。
Chinese translation into English
NovelOralSERDTFX06:DemonstratesRemarkablePotentialin Prior Fulvestrant Treatment Progressed Patients With ER+/HER2- Advanced Breast Cancer And Patients with Brain Metastases
At the recently held 2025 San Antonio Breast Cancer Symposium (SABCS 2025), the latest data from the Phase Ⅰ/Ⅱ clinical trial (NCT05927779) of TFX06 tablets—a next-generation oral selective estrogen receptor degrader (SERD) independently developed by VyBio Therapeutics (Zhejiang Yangli Pharmaceutical Technology Co., Ltd.) —
was released. The results showed that TFX06 not only exhibited favorable safety and systemic efficacy in ER+/HER2- advanced breast cancer patients who had undergone multiple lines of prior treatment, but also demonstrated encouraging therapeutic advantages in prior fulvestrant
treatment progressed populations and patients with brain metastases, offering new hope for clinically refractory breast cancer patients.
Definite Overall Efficacy: Sustained Benefits for Heavily Pretreated Patients
As of July 28, 2025, 57 patients with extensive prior treatment history were enrolled in the TFX06 trial at the recommended dose of 150mg, showing clear efficacy:
The median progression-free survival (mPFS) for all patients was 5.5 months, with a 6-month progression-free survival rate of 43.1%;
In patients harboring ESR1 mutations, mPFS was extended to 5.7 months, indicating TFX06’s therapeutic potential in endocrine-resistant patients.
These data confirm that TFX06 can provide clinically meaningful disease control and survival benefits for advanced breast cancer patients after multiple lines of treatment, regardless of ESR1 mutation status.
AddressingClinicalChallenges:BenefitsRemainin Prior Fulvestrant Treatment Progressed Populations
In the treatment of advanced breast cancer, patients previously treated with fulvestrant often face limited subsequent treatment options and suboptimal efficacy. In this trial, 56.1% of patients in the 150mg recommended dose group had received prior fulvestrant treatment, and 61.4% had undergone CDK4/6 inhibitor therapy—among whom more than one-third (38.6%) experienced disease progression after fulvestrant combined with CDK4/6 inhibitor treatment. Despite this highly refractory population, TFX06 still showed distinct clinical activity:
In 21 patients with prior fulvestrant + CDK4/6 inhibitor treatment, the clinical benefit rate (CBR) reached 42.9%;
In patients with ESR1 mutations, the benefit was more pronounced, with CBR increasing to 55.6% and mPFS reaching 5.6 months.
This suggests that TFX06 can provide sustained and effective disease control for patients who progress after fulvestrant treatment.
Breaking Treatment Barriers: Outstanding Intracranial Activity in Patients with Brain Metastases
Brain metastasis is a severe challenge in advanced breast cancer treatment, with traditional endocrine therapies offering limited efficacy. TFX06 has achieved breakthrough progress in this area:
Among 8 evaluable patients with brain metastases, the objective response rate (ORR) was as high as 37.5%, the disease control rate (DCR) was 87.5%, and the clinical benefit rate (CBR) reached 75%;
The mPFS for these patients was 7.6 months, significantly superior to the overall study population;
Imaging assessments confirmed that intracranial target lesions in some patients shrank by more than 70%, and even achieved complete response, demonstrating TFX06’s ability to cross the blood-brain barrier and inhibit intracranial tumor growth. Among all oral SERDs reported, TFX06 is the first and only agent reporting clear MRI evidence of intracranial efficacy in breast cancer brain metastasis patients.
Favorable Safety Profile: Ensuring Treatment Continuity
TFX06 exhibited good safety and tolerability in clinical use. The most common adverse events were Grade 1-2 abnormalities in laboratory chemistry assessments, which are easily manageable. The incidence of gastrointestinal reactions (e.g., nausea, diarrhea)
and cardiac toxicity (e.g., sinus bradycardia) was low, no ocular toxicity reported, providing important safety assurance and good quality of life for long-term medication in patients.
About TFX06
TFX06 is a third-generation oral SERD independently developed by VyBio Therapeutics (Zhejiang Yangli Pharmaceutical Technology Co., Ltd.), aiming to provide better innovative medicine for ER-positive HER2-negative breast cancer patients. TFX06 is a new generation of endocrine therapy, demonstrated efficacy in patients with ESR1m who progressed from current endocrine therapies, such as letrozole, or fulvestrant, with/without combination with CDK4/6 inhibitors. Currently, clinical trials of TFX06 as monotherapy and in combination with CDK4/6 inhibitors or everolimus are actively underway.
About VyBio
VyBio Therapeutics (Zhejiang Yangli Pharmaceutical Technology Co., Ltd.) is committed to the research and development of innovative oncology and chronic disease medicine to meet unmet clinical needs for patients worldwide. The therapeutic potential demonstrated by TFX06 in refractory breast cancer patients, especially those with brain metastases, while maintaining good quality of life, reinforces our mission to bring safe and more effective treatment options to patients worldwide.
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浙江扬厉医药技术有限公司
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