In Vivo Absorption, Metabolism, Excretion (AME) Clinical Study of [14C]Afuresertib in Healthy Chinese Male Adults - Human Mass Balance and Biotransformation Study of [14C]Afuresertib

This study adopts a single-center, single-dose, non-randomized, open-label design with a proposed enrollment of 6-10 healthy male subjects. After a single oral dose of approximately 125 mg/150 µCi [14C]Afuresertib tablets, blood, urine and fecal specimens are collected from each subject at defined time points/periods during the trial, and PK parameters, recovery, and excretion routes of [14C]Afuresertib in plasma are calculated by measuring the total radioactivity. The main metabolic and elimination pathways and characteristics of Afuresertib in human, as well as circulating metabolites with close to or higher than 10% of plasma total radioactivity exposure, are also identified by plasma, urine, and fecal radioactive metabolite profiles and major metabolite structure.

开始日期2022-08-06

申办/合作机构

来凯医药科技（上海）有限公司初创企业

CTR20221613

/ Completed临床1期

[14C]Afuresertib 在中国成年男性健康受试者体内吸收、代谢和排泄临床试验-[14C]Afuresertib 人体物质平衡及生物转化研究

主要研究目的：1. 定量分析男性健康受试者口服[14C]Afuresertib 后排泄物中的总放射性，获得人体放射性排泄率数据和主要排泄途径；2. 考察男性健康受试者单次口服[14C]Afuresertib 后全血和血浆中的分配情况和血浆中总放射性的药代动力学；3. 鉴定男性健康受试者口服[14C]Afuresertib 后人体内的主要代谢产物，确定主要生物转化途径和主要代谢产物（接近或高于10%总放射性AUC）；4. 采用已验证的HPLC-MS/MS 方法定量分析血浆中Afuresertib及其代谢产物（如适用）的浓度，获得血浆中Afuresertib 及其代谢产物（如适用）的药代动力学参数。次要研究目的：观察[14C] Afuresertib 单次给药后男性健康受试者的安全性

开始日期2022-08-01

申办/合作机构

缔脉生物医药科技（上海）有限公司初创企业

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100 项与 Afuresertib 相关的临床结果

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100 项与 Afuresertib 相关的转化医学

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100 项与 Afuresertib 相关的专利（医药）

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项与 Afuresertib 相关的文献（医药）

2025-04-01·SLAS Discovery

Combinatorial screen of targeted agents with the PI3K inhibitors inavolisib, alpelisib, duvelisib, and copanlisib in multi-cell type tumor spheroids

Article

作者: Said, Rabih ; Takebe, Naoko ; Moscow, Jeffrey A ; Dexheimer, Thomas S ; Coussens, Nathan P ; Teicher, Beverly A ; Davoudi, Zahra ; Doroshow, James H ; Silvers, Thomas ; Morris, Joel

Dysregulation of the phosphatidylinositol 3-kinase (PI3K) pathway is a key contributor to cancer, making PI3K inhibitors a promising approach for targeted therapy. The selectivity of available inhibitors varies across different PI3K isoforms. Alpelisib and inavolisib are selective for the α-isoform, while duvelisib targets the δ- and γ-isoforms, and copanlisib is a pan-PI3K inhibitor, active against all isoforms. This study investigated the activity of these four PI3K inhibitors in combination with other targeted agents using multi-cell type tumor spheroids composed of 60% malignant cells, 25% endothelial cells, and 15% mesenchymal stem cells. Twenty-nine tumor spheroid models were evaluated, including twenty-six patient-derived cancer cell lines from the NCI Patient-Derived Models Repository and three established cell lines from the NCI-60 human tumor cell line panel. Additive and/or synergistic effects were observed with alpelisib or inavolisib or copanlisib in combination with a RAS/MEK/ERK pathway inhibitor, either selumetinib (MEK), ravoxertinib (ERK 1/2), or tovorafenib (DAY101, RAF). Combinations of each of these three PI3K inhibitors with the KRAS mutation specific inhibitors MTRX1133 (KRAS G12D) or sotorasib (KRAS G12C) had selective activity in cell lines harboring the corresponding target. Lastly, combination effects were observed from vertical inhibition of the PI3K/AKT/mTOR pathway with a PI3K inhibitor in combination with either the mTORC1/2 inhibitor sapanisertib or an AKT inhibitor, ipatasertib or afuresertib.

2025-04-01·Molecular Diversity

An in silico approach to identify novel and potential Akt1 (protein kinase B-alpha) inhibitors as anticancer drugs

Article

作者: Kuchana, Vinutha ; Etikyala, Umadevi ; Dalimba, Udayakumar ; Reddyrajula, Rajkumar ; Vani, T ; Manga, Vijjulatha

Akt1 (protein kinase B) has become a major focus of attention due to its significant functionality in a variety of cellular processes and the inhibition of Akt1 could lead to a decrease in tumour growth effectively in cancer cells. In the present work, we discovered a set of novel Akt1 inhibitors by using multiple computational techniques, i.e. pharmacophore-based virtual screening, molecular docking, binding free energy calculations, and ADME properties. A five-point pharmacophore hypothesis was implemented and validated with AADRR38. The obtained R² and Q² values are in the acceptable region with the values of 0.90 and 0.64, respectively. The generated pharmacophore model was employed for virtual screening to find out the potential Akt1 inhibitors. Further, the selected hits were subjected to molecular docking, binding free energy analysis, and refined using ADME properties. Also, we designed a series of 6-methoxybenzo[b]oxazole analogues by comprising the structural characteristics of the hits acquired from the database. Molecules D1-D10 were found to have strong binding interactions and higher binding free energy values. In addition, Molecular dynamic simulation was performed to understand the conformational changes of protein-ligand complex.

2025-01-01·Nature Genetics

A multilineage screen identifies actionable synthetic lethal interactions in human cancers

Article

作者: Hager, Jeffrey H ; Mali, Prashant ; Mattson, Nicole M. ; White, Michael A ; Shen, John Paul ; Fong, Samson H ; Bergendahl, Sarah ; Bojorquez-Gomez, Ana ; Munson, Brenton P ; Licon, Katherine ; Kreisberg, Jason F. ; White, Michael A. ; Lee, John ; Munson, Brenton P. ; Kuenzi, Brent M. ; Ideker, Trey ; Hager, Jeffrey H. ; Kreisberg, Jason F ; Ford, Kyle ; Fong, Samson H. ; Mattson, Nicole M ; Sanchez, Kyle ; Kuenzi, Brent M

Cancers are driven by alterations in diverse genes, creating dependencies that can be therapeutically targeted. However, many genetic dependencies have proven inconsistent across tumors. Here we describe SCHEMATIC, a strategy to identify a core network of highly penetrant, actionable genetic interactions. First, fundamental cellular processes are perturbed by systematic combinatorial knockouts across tumor lineages, identifying 1,805 synthetic lethal interactions (95% unreported). Interactions are then analyzed by hierarchical pooling, revealing that half segregate reliably by tissue type or biomarker status (51%) and a substantial minority are penetrant across lineages (34%). Interactions converge on 49 multigene systems, including MAPK signaling and BAF transcriptional regulatory complexes, which become essential on disruption of polymerases. Some 266 interactions translate to robust biomarkers of drug sensitivity, including frequent genetic alterations in the KDM5C/6A histone demethylases, which sensitize to inhibition of TIPARP (PARP7). SCHEMATIC offers a context-aware, data-driven approach to match genetic alterations to targeted therapies.

项与 Afuresertib 相关的新闻（医药）

2025-03-03

·laekna.com

Laekna Announces IND Approval of LAE120 (a Novel USP1 Inhibitor) for Treatment of Advanced Solid Tumors by FDA

– A novel, allosteric and highly potent USP1 inhibitor, LAE120 exhibits robust tumor inhibitory activity across various xenograft models – Significantly accelerated the progress of drug discovery leveraging cutting-edge AI models – Another potential anti-tumor drug candidate, LAE118 (a mutant-selective PI3Kα inhibitor) also in IND-enabling studies March 3, 2025 — Laekna (2105.HK) announced that the U.S. Food and Drug Administration (FDA) has approved the IND for LAE120, an internally discovered USP1 inhibitor, for the treatment of advanced solid tumors. LAE120 is a novel, allosteric and highly potent USP1 inhibitor, displaying monotherapy potency and combination activity with PARP inhibitor in HRD (homologous recombination deficiency) cancers. It has a unique chemical structure differentiated from all the other disclosed USP1 inhibitors and is expected to induce a different conformational change in USP1. LAE120 shows robust tumor inhibitory activity across various xenograft models such as MDA-MB-436 and K562 as a single agent and exhibits synergistic effect in combination with PARP inhibitors. It also demonstrates good therapeutic windows in GLP long-term toxicology study. Laekna is actively exploring partnerships to accelerate the clinical development of LAE120. “Leveraging our deep know-how and extensive expertise in drug discovery, Laekna has developed a distinctive portfolio of innovative drug candidates through the close collaboration of our Med Chem, Biology and AIDD (AI-driven Drug Discovery) teams, continuously advancing preclinical drug candidates into clinical stage. Laekna has also significantly accelerated the progress of drug discovery by utilizing cutting-edge artificial intelligence tools”, said Dr. Justin Gu, Chief Scientific Officer of Laekna. "We look forward to bringing novel drugs to patients as swiftly as possible," he added. Advancing Diversified Pipelines Laekna is actively advancing preclinical drug candidates. In the fourth quarter of 2024, another internally discovered anti-tumor drug candidate, LAE118, a potentially best-in-class, mutant-selective PI3Kαinhibitor, has advanced to IND-enabling study. PI3Kα mutations are prevalent in patients with breast, colorectal, lung, endometrial, and numerous other cancers. However, the first-generation drugs targeting PI3Kα inhibit the wild-type and mutant PI3Kα with equal potency, which raises concerns of tolerability and therapeutic efficacy. As a novel allosteric inhibitor, LAE118 demonstrates excellent potency and selectivity towards various PI3Kα mutants. With superior anti-cancer efficacy and tolerability than other current PI3Kα inhibitors, LAE118 is potentially the best-in-class pan-mutant-selective PI3Kα inhibitor. Laekna has presented the preclinical characterization of LAE118 at the San Antonio Breast Cancer Symposium (SABCS) in December 2024. LAE118 is in IND-enabling studies and IND is expected to be filed in the fourth quarter of 2025. Strategic Partnerships to Accelerate Globalization " We will continue to advance and expand our product portfolio in the therapeutic areas where we have accumulated tremendous experience and extensive know-how.”, said Dr. Chris Lu, Chief Executive Officer of Laekna, “In November 2024, the Group has entered into a clinical collaboration agreement with Lilly (NYSE:LLY) to support and accelerate global clinical development of LAE102 for the treatment of obesity. We plan to pursue strategic partnerships with global leading pharmaceutical companies to accelerate clinical development and commercialization of our drug candidate assets. We keep advancing and expanding our pipeline and are committed to bringing life-changing medicines to more people around the world.” - End – About Laekna Stock Code: 2105.HK Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapeutics to patients with cancer, metabolic diseases and liver fibrosis patients around the world. As of June 30, 2024, Laekna has initiated seven clinical trials for LAE102, LAE002(afuresertib), LAE001 and LAE005 to address unmet medical needs in obesity and cancers. LAE102 is our internally discovered antibody against ActRIIA. It has been shown in the pre-clinical studies to increase lean mass and decrease fat mass. We’ve obtained IND approvals from the FDA and the CDE for LAE102 in obesity indication and are advancing the Phase I clinical trial in China. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass. Laekna team has accumulated tremendous experiences and deep know-how in this specific field and is developing more drug candidates (LAE103 and LAE123), in addition to LAE102, to maximize the value of targeting ActRII receptors. In the cancer area, Laekna has built a comprehensive portfolio of drug candidates, covering the treatment of breast cancer, prostate cancer, ovarian cancer and PD-1/ PD-L1 drug-resistant solid tumors. LAE002 (afuresertib) is a potent AKT inhibitor that inhibits all three AKT isoforms (AKT1, AKT2 and AKT3) as well as one of the only two AKT inhibitors in late-stage development for breast and prostate cancer globally. Laekna has commenced the Phase III clinical trial (AFFIRM-205) for LAE002 in patients with HR+/HER2- breast cancer. Laekna, Inc. (2105.HK) was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the “Hong Kong Stock Exchange”) on June 29, 2023. For more information, please visit: https://www.laekna.com/ or https://www.linkedin.com/company/74110713/ Forward-Looking Statements This press release may contain certain “forward-looking statements” which are not historical facts, but instead are predictions about future events based on Laekna’s current beliefs, assumptions and expectations, commonly identified by words such as "would", "may", "expects", "believes", "plans", "intends", "projects" and other terms with similar meaning. Although we believe that our predictions are reasonable, future events are inherently uncertain and our actual future results or performance may be materially different from what we expect. Accordingly, you are strongly cautioned that reliance on any forward-looking statements is subject to significant known and unknown risks and uncertainties. All forward-looking statements contained herein are qualified by reference to the cautionary statements set forth in this section. All information provided in this press release is as of the date of this press release and are based on assumptions that we believe to be reasonable as of this date, and we do not undertake any obligation to update any forward-looking statement, except as required under applicable law.

临床申请临床3期临床1期

2025-02-28

·ioncology

SGO 2025丨最重要的研究进展：科学全体会议的报告一览

点上方蓝字“ioncology”关注我们，然后点右上角“…”菜单，选择“设为星标” SGO 2025微专辑扫描二维码可查看更多内容第56届美国妇科肿瘤学年会（SGO 2025）将于2025年3月14-17日在西雅图举办。在肿瘤学学术会议中，“Scientific Plenary”（科学全体会议）通常是指会议中最核心、最具权威性的学术环节，其内容往往代表年度研究最高水平。本文汇总2025 SGO科学全体会议的研究内容，供读者参考。科学全体会议（Scientific Plenary）摘要ID：935279 英文标题：Pembrolizumab Plus Chemoradiotherapy for High-Risk Locally Advanced Cervical Cancer: Overall Survival and Progression-Free Survival 2 Results From the Randomized, Double-Blind, Phase III ENGOT-cx11/GOG-3047/KEYNOTE-A18 Study 中文标题：帕博利珠单抗联合放化疗治疗高风险局部晚期宫颈癌：随机、双盲、III期ENGOT-cx11/GOG-3047/KEYNOTE-A18研究的总生存（OS）和第二次无进展生存（PFS2）结果汇报人：Linda Duska丨弗吉尼亚大学医学院摘要ID：864114 英文标题：Cadonilimab plus lenvatinib in patients with advanced endometrial cancer: a multicenter, single-arm, phase II trial 中文标题：卡度尼利单抗+乐伐替尼治疗晚期子宫内膜癌患者：一项多中心、单组I期试验汇报人：蓝春燕丨中山大学附属肿瘤医院摘要ID：852136 英文标题：A Phase II study of induction PD-1 blockade (nivolumab) in patients with surgically completely resectable mismatch repair deficient endometrial cancer (NIVEC) 中文标题：针对可手术完全切除的错配修复缺陷型子宫内膜癌患者进行诱导PD-1阻断（纳武利尤单抗）治疗的II期研究汇报人：Lee Yong Jae丨延世大学医学院摘要ID：812874 英文标题：Sentinel Lymph Node Biopsy versus Pelvic Lymphadenectomy in Cervical Cancer: the PHENIX-I trial 中文标题：宫颈癌前哨淋巴结活检vs盆腔淋巴结清扫术：PHENIX-I试验汇报人：刘继红丨中山大学肿瘤防治中心摘要ID：922975 英文标题：Durvalumab plus carboplatin/paclitaxel followed by durvalumab with/without olaparib in endometrial cancer: biomarkers, histological heterogeneity, baseline circulating tumor DNA levels, and efficacy in the DUO-E mismatch repair proficient subpopulation 中文标题：度伐利尤单抗+卡铂/紫杉醇序贯度伐利尤单抗±奥拉帕利治疗子宫内膜癌：生物标志物、组织学异质性、基线循环肿瘤DNA水平以及DUO-E错配修复功能健全亚组的疗效汇报人：Kathleen Moore丨俄克拉荷马大学摘要ID：815965 英文标题：Randomized Phase III Trial of Adjuvant Radiation versus Chemo-radiation in Intermediate-Risk, Early-stage Cervical Carcinoma following Radical Hysterectomy and Lymphadenectomy (Results of NRG Oncology/GOG-263) 中文标题：对比辅助放疗vs化放疗用于接受根治性子宫切除术和淋巴结清扫术后的中危早期宫颈癌患者：随机III期NRG Oncology/GOG-263试验结果汇报人：Ryu Sang Young丨韩国癌症中心医院摘要ID：808923 英文标题：Patient-reported outcomes (PROs) on a Randomized Phase III Clinical Trial of Adjuvant Radiation (RT) versus Chemoradiation (RT+CIS) in Intermediate Risk, Stage I/IIA Cervical Cancer Treated with Initial Radical Hysterectomy and Pelvic Lympha 中文标题：对比辅助放疗vs放化疗用于初始根治性子宫切除术和盆腔淋巴结清扫术治疗后的中危I/IIA期宫颈癌患者：一项随机III期临床试验的患者报告结果(PRO) 汇报人：Alexandra Smick丨加利福尼亚大学洛杉矶分校（UCLA）摘要ID：811862 英文标题：Comparing community member and provider-perceived barriers to clinical trial enrollment in rural areas: how well do we know our patients? 中文标题：比较社区成员和医疗提供方认为的农村地区临床试验的入组障碍：我们对患者的了解程度如何？汇报人：Kaylee Underkofler丨弗吉尼亚大学摘要ID：812926 英文标题：Development of an Endometrial Cancer Test for Evaluating Abnormal Uterine Bleeding 中文标题：开发用于评估异常子宫出血的子宫内膜癌检测方法汇报人：Jamie Bakkum-Gamez丨梅奥诊所摘要ID：822422 英文标题：Utility of the CA125 KELIM in for predicting the benefit of from HIPEC in patients with advanced ovarian cancer: pooled analysis of individual data from KGOG3042 and KOV-HIPEC01 中文标题：使用CA125 KELIM预测晚期卵巢癌患者接受HIPEC治疗获益：KGOG3042和KOV-HIPEC01个体数据的汇总分析汇报人：Cho Hyun-Woong丨高丽大学教师医院摘要ID：843870 英文标题：An Open-Label Randomized Active-Controlled Phase II Clinical Study to Assess the Efficacy and Safety of Afuresertib Plus Paclitaxel Versus Paclitaxel in Patients with Platinum-Resistant Ovarian Cancer (GOG 3044) 中文标题：开放标签随机阳性对照II期临床研究（GOG 3044）：评估Afuresertib+紫杉醇vs紫杉醇治疗铂耐药卵巢癌患者的疗效和安全汇报人：Thomas Herzog丨辛辛那提大学癌症中心摘要ID：812768 英文标题：DB-1305/BNT325 (a novel TROP-2 ADC) in patients with ovarian cancer: Efficacy and safety data from a phase 1/2 study 中文标题：DB-1305/BNT325（新型TROP-2 ADC）在卵巢癌患者中的应用：I/II期研究的疗效和安全性数据汇报人：Maria Rubinstein丨纪念斯隆凯特琳癌症中心摘要ID：814654 英文标题：Cyclin E1 is a Predictive Biomarker of Azenosertib Benefit in Platinum-Resistant Ovarian Cancer (PROC): Outcomes from Part 1b of the DENALI Study (GOG-3066) 中文标题：细胞周期蛋白E1是Azenosertib治疗铂耐药卵巢癌获益的预测性生物标志物：DENALI研究（GOG-3066）Ib部分的结果汇报人：Fiona Simpkins丨宾夕法尼亚大学摘要ID：933087 英文标题：Safety and preliminary efficacy of puxitatug samrotecan (P-Sam, AZD8205) in patients (pts) with endometrial cancer (EC): a first-in-human Phase 1/2a study 中文标题：puxitatug samrotecan（P-Sam, AZD8205）治疗子宫内膜癌患者的安全性和初步疗效：一项首次人体I/IIa期研究汇报人：Stephanie Gaillard丨约翰霍普金斯大学西德尼·金梅尔癌症中心摘要ID：926320 英文标题：Early salpingectomy with delayed oophorectomy as alternative for risk-reducing salpingo-oophorectomy - the first 2000 participants in the ongoing international TUBA-WISP II study 中文标题：早期输卵管切除术和延迟卵巢切除术作为降低风险的输卵管卵巢切除术的替代方案：正在进行的国际II期TUBA-WISP研究的前2000名受试者汇报人：Tamar Gootzen丨拉德堡德医学中心摘要ID：927707 英文标题：Comparing Efficacy and Safety of Biweekly Single-Dose Actinomycin D versus Multiday Methotrexate Therapy in Low-Risk Gestational Trophoblastic Neoplasia: A Prospective Multicentre Randomized Trial 中文标题：比较每两周一次放线菌素D vs多日甲氨蝶呤治疗低风险妊娠滋养细胞肿瘤的疗效和安全性：一项前瞻性多中心随机试验汇报人：蒋芳丨北京协和医院摘要ID：938179 英文标题：Phase 2 study of letrozole, abemaciclib and metformin in estrogen receptor (ER) positive recurrent endometrial cancer (EC) 中文标题：来曲唑、阿贝西利和二甲双胍治疗雌激素受体（ER）阳性复发性子宫内膜癌的II期研究汇报人：Panagiotis Konstantinopoulos丨丹娜—法伯癌症研究所摘要ID：922978 英文标题：Efficacy and safety of luveltamab tazevibulin in patients with recurrent platinum-resistant ovarian cancer: results from the dose-optimization stage of the REFRalphaME-O1 (GOG-3086, ENGOT-79OV, and APGOT-OV9) phase 2/3 study 中文标题：Luveltamab tazevibulin治疗复发性铂耐药卵巢癌的疗效和安全性：II/III期REFRaME-O1（GOG-3086、ENGOT-79OV和APGOT-OV9）临床试验剂量优化阶段的结果汇报人：Lee Jung-Yun丨延世大学世福兰斯医院摘要ID：953906 英文标题：Chemotherapy with or without pembrolizumab followed by maintenance with olaparib or placebo for first-line treatment of advanced BRCA non-mutated epithelial ovarian cancer: Results from the randomized phase 3 ENGOT-OV43/GOG-30 中文标题：化疗±帕博利珠单抗序贯奥拉帕利或安慰剂维持治疗作为晚期BRCA非突变上皮性卵巢癌的一线治疗：随机III期ENGOT-OV43/GOG-30试验结果汇报人：Matthew Powell丨华盛顿大学医学院摘要ID：939696 英文标题：Final overall survival analysis among patients with FRalpha;-positive, platinum-resistant ovarian cancer (PROC) treated with mirvetuximab soravtansine (MIRV) vs. investigator's choice chemotherapy (ICC) in the Phase 3 MIRASOL (GOG 304) 中文标题：索米妥昔单抗(MIRV) vs 研究者选择的化疗治疗FRα阳性、铂耐药卵巢癌：III期MIRASOL（GOG 304）试验的最终OS分析汇报人：Toon Van Gorp丨鲁汶大学医院摘要ID：822484 英文标题：Phase 2 study of Maintenance of Niraparib rechallenge plus Bevacizumab in Patients with Platinum-Sensitive, Recurrent Ovarian Cancer Previously Treated with a PARP inhibitor (KGOG 3056/NIRVANA-R) 中文标题：PARP抑制剂经治的铂敏感复发性卵巢癌患者接受尼拉帕利再使用+贝伐珠单抗维持治疗的II期临床研究 (KGOG 3056/NIRVANA-R) 汇报人：Hyun-Woong Cho丨高丽大学九老医院摘要ID：938651 英文标题：Trends in Gynecologic Cancers across the United States from 2001-2019: Impact of Social Determinants of Health on Stage at Diagnosis 中文标题：2001-2019年美国妇科癌症趋势：“健康的社会决定因素”对诊断分期的影响汇报人：Michael Desjardins丨约翰霍普金斯大学彭博公共卫生学院摘要ID：812404 英文标题：Measuring Contemporary Symptoms in a Diverse Population of Endometrial Cancer Patients: Development and Initial Validation of a Brief Symptom Index from the PROMOTE Study 中文标题：评估不同子宫内膜癌患者群体的当前症状：PROMOTE研究中简明症状指数的开发和初步验证汇报人：Chelsea McKinney丨加州大学欧文分校摘要ID：842468 英文标题：Impact of treatment-emergent ocular events on health-related quality of life in patients with FRalpha;-positive platinum-resistant ovarian cancer treated with mirvetuximab soravtansine: results from the phase 3 MIRASOL study 中文标题：治疗中出现的眼部不良事件对接受索米妥昔单抗治疗的FRa阳性铂耐药卵巢癌患者健康相关生活质量的影响：来自III期MIRASOL研究的结果汇报人：Tashanna Myers丨贝斯特医疗中心摘要ID：808773 英文标题：Clinician Nudge to Gynecologic Oncology Referral at Suspected Ovarian Cancer Diagnosis: A Pilot Study 中文标题：临床医生推动疑似卵巢癌的患者向妇科肿瘤科转诊：一项试点研究汇报人：Anna Jo Smith丨宾夕法尼亚大学（来源：《肿瘤瞭望》编辑部）声明凡署名原创的文章版权属《肿瘤瞭望》所有，欢迎分享、转载。本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。

临床2期临床结果

2025-01-13

·求实药社

来凯医药LAE102肥胖症I期临床取得重大进展

2025年1月13日，来凯医药宣布，其自主研发的LAE102（ActRIIA单克隆抗体）针对超重/肥胖在中国开展的I期临床试验取得重大进展：单剂量递增研究（SAD研究）已成功完成。来凯医药董事长兼首席执行官吕向阳博士称“对于LAE102治疗肥胖症I期单剂量递增研究的全新临床数据，我们感到既兴奋又期待。SAD的积极数据证明，选择性激活素A受体抑制有望成为一种重要的创新疗法。” 此次SAD研究共招募了64名健康受试者，平均BMI23.2±2.2kg/m2，包括5个静脉给药队列和3个皮下给药队列。截至目前，LAE102的SAD研究数据显示了令人鼓舞的安全性和耐受性特征。未发生严重不良事件，也没有因不良事件而中止治疗到目前为止报告的所有治疗相关不良事件都被很好地耐受，其中大多数报告为轻度（1级）实验室检查异常，且没有出现任何临床症状或体征没有报告任何腹泻病例试验观察到明显的药物靶点结合和预期的药效动力学生物标志物变化，单次剂量的LAE102给药导致激活素A水平显著且持续增加，表明了强有力的靶点抑制。靶点抑制的持续时间与剂量水平相关。I期SAD详细研究结果将尽快在相关科学会议上进行展示。积极的SAD研究结果支持继续对LAE102针对肥胖症治疗的研究。公司计划在2025年第一季度启动I期MAD研究，并与礼来合作尽快启动美国一期研究。I期MAD研究是一项随机、双盲、安慰剂对照研究，旨在评估皮下给药的LAE102在60名超重/肥胖受试者中的安全性、耐受性、药代动力学和药效动力学。 LAE102是自主研发针对ActRIIA的单克隆抗体，ActRIIA是在肌肉再生和脂肪代谢中发挥重要作用的受体。在临床前模型中，LAE102已显示出增加肌肉并减少脂肪的效果。LAE102与GLP-1受体激动剂联用可进一步减少脂肪并显著降低GLP-1受体激动剂导致的肌肉流失，使LAE102成为一种高质量体重控制候选药物。2024年11月，来凯医药宣布与礼来在美国合作，加速LAE102的肥胖症治疗领域的临床研究。根据Insight数据库统计数据，截至目前，处于临床开发阶段的激活素信号通路抑制剂候选药物有7种，开发适应症包括肺动脉高压、肥胖、骨纤维化、骨质疏松等。来凯医药成立于2016年，是一家以科学为驱动、处于临床阶段的生物医药科技公司，致力于为全球肿瘤、代谢疾病及肝纤维化患者带来新型疗法。截至2024年6月30日，来凯医药围绕LAE102、LAE002(afuresertib)、LAE001及LAE005启动了七项临床试验，以解决肥胖症及肿瘤领域未被满足的医疗需求。 LAE102是来凯自主研发针对ActRIIA的单克隆抗体。临床前研究显示，可增加肌肉并减少脂肪。LAE102已获得中国和美国针对肥胖适应症的新药临床试验（IND）批准，I期临床研究正在全速推进。阻断Activin-ActRII通路可促进肌肉再生和减少脂肪。来凯团队在这一特定领域积累了丰富的经验及深厚的专业知识，并正在开发更多的候选药物（LAE103、LAE123等），以最大限度地发挥靶向ActRII受体的价值。在肿瘤领域，来凯已经建立全面的候选药物组合，覆盖乳腺癌、前列腺癌、卵巢癌及PD-1/PD-L1耐药实体瘤等。 LAE002(afuresertib)是一种AKT强效抑制剂，抑制所有三种AKT亚型（AKT1、AKT2及AKT3），也是全球两种处于晚期临床开发阶段的针对乳腺癌及前列腺癌的AKT抑制剂之一。目前来凯医药针对HR+/HER2-乳腺癌III期关键研究（AFFIRM-205）已全面启动。公司在研管线内容来源于网络，如有侵权，请联系删除。

临床结果

100 项与 Afuresertib 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10381	-	-	DB11648

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
HR阳性/HER2阴性乳腺癌	临床3期	中国	来凯医药	2022-02-18
HR阳性/HER2阴性乳腺癌	临床3期	美国	来凯医药	2022-02-18
慢性淋巴细胞白血病	临床2期	-	Novartis Pharma AG	-
慢性淋巴细胞白血病	临床2期	-	来凯医药科技（上海）有限公司初创企业	-
慢性淋巴细胞白血病	临床2期	-	GSK Plc	-
多发性骨髓瘤	临床2期	-	Novartis Pharma AG	-
慢性淋巴细胞白血病	临床1期	加拿大	-	-
卵巢癌	临床1期	俄罗斯	Novartis Oncology, Inc.	-
卵巢癌	临床1期	英国	Novartis Oncology, Inc.	-
卵巢癌	临床1期	澳大利亚	Novartis Oncology, Inc.	-

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05383482 (IGCS2024) 人工标引	临床1/2期	实体瘤 \| 子宫内膜癌 \| 宫颈癌	18	Afuresertib + Sintilimab + Nab-paclitaxel	(構蓋鏇糧鹽簾壓遞膚願) = 艱壓製壓製壓鑰顧鬱鹽鏇構範選齋鑰壓鹽築顧 (壓選遞積淵顧艱簾夢齋, 31.6 ~ 86.1) 更多	积极	2024-10-16
NCT04851613 (NEWS) 人工标引	临床1期	HR阳性/HER2阴性乳腺癌 \|	18	LAE002 (afuresertib) plus fulvestrant (PIK3CA/AKT1/PTEN alteration)	(窪齋艱壓積觸衊製壓壓) = 願蓋餘積鏇鏇顧遞艱遞膚廠醖憲獵繭餘鹹選壓 (鏇窪選鬱鬱醖鹹積鹹遞 ) 更多	积极	2024-09-19
NCT04851613 (ESMO2024) 人工标引	临床1期	HR阳性/HER2阴性乳腺癌 \| ... 更多	31	Afuresertib plus fulvestrant	(築鏇窪鏇願蓋鑰繭衊獵) = 鑰顧鬱艱鬱鑰積鏇積顧窪鹹齋齋鑰獵網製憲簾 (淵窪選艱窪憲窪鑰積鹽 ) 更多	积极	2024-09-16
NCT04851613 (ESMO2024) 人工标引	临床1期	HR阳性/HER2阴性乳腺癌 \| ... 更多	31	afuresertib (PIK3CA/AKT1/PTEN-altered subjects)	(築鏇窪鏇願蓋鑰繭衊獵) = 艱鏇遞糧鏇網簾艱蓋糧窪鹹齋齋鑰獵網製憲簾 (淵窪選艱窪憲窪鑰積鹽 ) 更多	积极	2024-09-16
NCT04374630 (PROFECTA II, Corporate Publications) 人工标引	临床2期	铂耐药性卵巢癌	150	Afuresertib+Paclitaxel	(餘夢築築夢憲餘獵艱築): HR = 0.744 (95% CI, 0.502 ~ 1.102) 未达到	不佳	2024-01-28
NCT04374630 (PROFECTA II, Corporate Publications) 人工标引	临床2期	铂耐药性卵巢癌	150	Paclitaxel	(餘夢築築夢憲餘獵艱築): HR = 0.744 (95% CI, 0.502 ~ 1.102) 未达到	不佳	2024-01-28
NCT04060394 (ESMO 12023 \| ESMO 22023) 人工标引	临床1/2期	转移性去势抵抗性前列腺癌	40	LAE001+prednisone+ afuresertib	(製廠鑰願選築窪蓋網蓋) = thrombocytopenia (7.5%), anaemia (5.0%), hyperglycaemia (5.0%), hyponatraemia (5.0%), and hypertension (5.0%). SAEs were reported in 9 patients (22.5%), 5 (12.5%) were assessed as related to study treatment 憲壓襯範蓋窪選鹽憲積 (廠鏇鹽遞遞艱範積襯衊 )	积极	2023-10-22
NCT04060394 (ESMO 12021 \| ESMO 22021) 人工标引	临床1期	转移性去势抵抗性前列腺癌	14	prednisone+afuresertib+LAE001	(獵築鹹範淵顧鑰襯憲繭) = RP2D was a skin rash 網夢築鏇願簾願鏇齋衊 (顧觸窪遞襯醖鹽膚鬱糧 ) 更多	积极	2021-09-16
NCT01531894 (CTgov)	临床2期	实体瘤 \| 血液肿瘤	11	GSK2110183 (afuresertib)	網蓋願遞築壓積壓網艱(簾憲鏇衊鹽糧獵壓醖積) = 遞壓夢壓憲衊遞餘遞顧遞窪製廠簾遞淵選製壓 (艱構遞襯簾積鬱範積範, 鹽積憲網膚鹹顧觸構衊 ~ 餘膚餘艱壓齋築顧鹽窪)	-	2019-07-09
NCT01653912 (Pubmed \| Clin Cancer Res)	临床1/2期	复发性铂耐药性卵巢癌	59	Afuresertib	(壓顧憲淵網範網蓋鹹夢) = 顧衊範積齋簾淵淵遞積顧築艱構廠淵艱觸糧鬱 (鬱選夢鑰齋築鏇鑰鏇衊, 15.9 ~ 52.4) 更多	-	2019-03-01
NCT01653912 (Pubmed \| Clin Cancer Res)	临床1/2期	复发性铂耐药性卵巢癌	59	Carboplatin and Paclitaxel	(壓顧憲淵網範網蓋鹹夢) = 壓廠齋鹹膚繭艱願壓顧顧築艱構廠淵艱觸糧鬱 (鬱選夢鑰齋築鏇鑰鏇衊, 31.3 ~ 72.2)	-	2019-03-01
NCT01653912 (CTgov)	临床1/2期	铂耐药性卵巢癌 \| 复发性铂耐药性卵巢癌	59	GSK2110183 (Phase 1 (Dose Escalation): GSK2110183)	醖遞糧顧齋網鬱築鏇蓋(衊觸壓蓋顧蓋窪構繭獵) = 獵構憲範選構願鬱壓廠淵網築壓範糧選壓觸膚 (廠齋淵鏇艱蓋憲襯鏇積, 築鬱築壓壓積鬱積範膚 ~ 顧鏇衊膚襯壓夢夢範製) 更多	-	2018-04-02
NCT01653912 (CTgov)	临床1/2期	铂耐药性卵巢癌 \| 复发性铂耐药性卵巢癌	59	GSK2110183 (Phase 2 (Treatment Group): GSK2110183)	(艱鑰鹽構願壓築襯蓋遞) = 選觸餘壓願膚網積餘鬱夢範廠網遞構齋鬱鑰衊 (壓構鑰選艱築築繭壓餘, 積淵網鬱齋築鹹鏇網衊 ~ 築築願廠鹹齋簾繭製蓋) 更多	-	2018-04-02
NCT01653912 (ASCO2016)	临床1/2期	复发性卵巢癌	59	Afuresertib + Paclitaxel + Carboplatin	構憲顧蓋觸醖鬱襯築積(糧鹽製遞鏇襯艱築鬱製) = G3/4 AEs included diarrhea (20%), fatigue (10%), rash (10%), vomiting (7%), and nausea (3%) 艱願餘餘築齋選遞簾鹹 (齋選齋選襯淵衊鹹範餘 )	积极	2016-05-20