A Phase 1b/2 Study of GS-5829 in Combination With Fulvestrant or Exemestane in Subjects With Advanced Estrogen Receptor Positive, HER2 Negative-Breast Cancer

The primary objectives of the Phase 1b Dose Escalation part of this study are to characterize the safety and tolerability of GS-5829 in combination with exemestane or fulvestrant and to determine the maximum tolerated dose (MTD) or the recommended Phase 2 dose of GS-5829 in combination with fulvestrant in women with advanced estrogen receptor positive, HER2-negative (ER+/HER2-) breast cancer.
The primary objective of the Randomized Phase 2 Dose Expansion portion of this study is to evaluate the efficacy of GS-5829 in combination with fulvestrant compared to fulvestrant alone in women with advanced ER+/HER2- breast cancer.
This study was terminated early and the Phase 2 portion of the study was not conducted.

开始日期2017-01-10

申办/合作机构

Gilead Sciences, Inc.

NCT02607228

/ Terminated临床1/2期

A Phase 1b/2 Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of GS-5829 as a Single Agent and In Combination With Enzalutamide in Subjects With Metastatic Castrate-Resistant Prostate Cancer

This study consists of two phases: Dose Escalation (Phase 1b) and Dose Expansion (Phase 2)
The Dose Escalation phase will characterize the safety, tolerability, and determine the maximum tolerated dose (MTD) of alobresib as a single agent and in combination with enzalutamide, in participants with metastatic castrate-resistant prostate cancer (mCRPC).
The Dose Expansion phase will evaluate the following:
* In group 1, the efficacy of alobresib as a single agent in participants with mCRPC who have progressed while receiving enzalutamide (may have also received abiraterone)
* In group 2, the efficacy of alobresib combined with enzalutamide in participants with mCRPC who have progressed while receiving treatment with abiraterone (may not have previously received enzalutamide)
* In group 3, the efficacy of alobresib combined with enzalutamide in participants with mCRPC who have had prostate specific antigen (PSA) progression, but not radiographic progression, while receiving treatment with enzalutamide (participants may have also previously received abiraterone)

开始日期2015-12-08

申办/合作机构

Gilead Sciences, Inc.

NCT02392611

/ Completed临床1期

A Phase 1 Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Alobresib (Formerly GS-5829) as a Monotherapy in Subjects With Advanced Solid Tumors and Lymphomas and in Combination With Exemestane or Fulvestrant in Subjects With Estrogen Receptor Positive Breast Cancer

The primary objectives of this study are to characterize the safety and tolerability and determine the maximum tolerated dose (MTD) or recommended dose for phase 2 study (RDP2) of alobresib as a monotherapy in participants with advanced solid tumors and lymphomas, and in combination with exemestane or fulvestrant in participants with advanced estrogen receptor positive breast cancer.

开始日期2015-03-16

申办/合作机构

Gilead Sciences, Inc.

100 项与 Alobresib 相关的临床结果

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100 项与 Alobresib 相关的转化医学

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100 项与 Alobresib 相关的专利（医药）

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项与 Alobresib 相关的文献（医药）

2022-09-15·Clinical cancer research : an official journal of the American Association for Cancer Research

Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer

Article

作者: Xing, Guan ; Starodub, Alexander N. ; Aggarwal, Rahul ; Carducci, Michael A. ; Koh, Brian D. ; Armstrong, Andrew J.

Abstract:

Purpose::

A phase Ib study (1604) was conducted to evaluate the safety and efficacy of GS-5829, an oral bromodomain and extraterminal inhibitor, alone and in combination with enzalutamide in metastatic castration-resistant prostate cancer (mCRPC). A phase I study (1599) in solid tumors/lymphoma was also conducted.

Patients and Methods::

Men with confirmed mCRPC and disease progression despite abiraterone and/or enzalutamide treatment were enrolled in a 3 + 3 dose escalation paradigm starting at 2 mg daily with GS-5829 alone and in combination with 160 mg daily enzalutamide. The primary efficacy endpoint was nonprogression rate at week 24; secondary endpoints included prostate-specific antigen reduction from baseline, progression-free survival, and GS-5829 pharmacokinetics (PK). PK and safety were also evaluated in Study 1599.

Results::

Thirty-one men, with a median of five prior regimens, received at least 1 dose of study drug in Study 1604. Treatment-emergent adverse events (TEAE) were reported in 94% of patients; 16% discontinued for TEAEs. There were no dose-dependent increases in the AUCtau or Cmax after once-daily administration of GS-5829 2 to 9 mg, and biomarkers CCR2 inhibition and HEXIM1 induction were increased only at higher doses of monotherapy. A high degree of interpatient variability existed across all doses in PK and pharmacodynamic parameters. The proportion with nonprogression at week 24, estimated by Kaplan–Meier model, was 25% (95% confidence interval, 10–42) for all treated patients.

Conclusions::

GS-5829 was generally tolerated but demonstrated limited efficacy and lack of dose proportional increases in plasma concentrations in patients with mCRPC.

2020-06-01·Leukemia1区 · 医学

The BET inhibitor GS-5829 targets chronic lymphocytic leukemia cells and their supportive microenvironment

1区 · 医学

Article

作者: Wierda, William G ; Clarke, Astrid ; Jain, Nitin ; Sivina, Mariela ; Ten Hacken, Elisa ; Thompson, Philip A ; Burger, Jan A ; Bhalla, Kapil N ; Kim, Ekaterina ; Keating, Michael J ; Estrov, Zeev ; Ferrajoli, Alessandra

Despite major improvements in treatment outcome with novel targeted therapies, such as the Bruton tyrosine kinase (BTK) inhibitor ibrutinib, chronic lymphocytic leukemia (CLL) remains incurable in the majority of patients. Activation of PI3K, NF-κB, and/or MYC has been linked to residual disease and/or resistance in ibrutinib-treated patients. These pathways can be targeted by inhibitors of bromodomain and extra-terminal (BET) proteins. Here we report about the preclinical activity of GS-5829, a novel BET inhibitor, in CLL. GS-5829 inhibited CLL cell proliferation and induced leukemia cell apoptosis through deregulation of key signaling pathways, such as BLK, AKT, ERK1/2, and MYC. IκBα modulation indicates that GS-5829 also inhibited NF-κB signaling. GS-5829-induced apoptosis resulted from an imbalance between positive (BIM) and negative regulators (BCL-X_L) of the intrinsic apoptosis pathway. The antileukemia activity of GS-5829 increased synergistically in combinations with B-cell receptor signaling inhibitors, the BTK inhibitor ibrutinib, the PI3Kδ inhibitor idelalisib, and the SYK inhibitor entospletinib. In cocultures that mimic the lymph node microenvironment, GS-5829 inhibited signaling pathways within nurselike cells and their growth, indicating that BET inhibitors also can target the supportive CLL microenvironment. Collectively, these data provide a rationale for the clinical evaluation of BET inhibitors in CLL.

2018-10-01·Clinical cancer research : an official journal of the American Association for Cancer Research1区 · 医学

Inhibition of BET Bromodomain Proteins with GS-5829 and GS-626510 in Uterine Serous Carcinoma, a Biologically Aggressive Variant of Endometrial Cancer

1区 · 医学

Article

作者: Altwerger, Gary ; Hui, Pei ; Lopez, Salvatore ; Riccio, Francesco ; Yadav, Ghanshyam ; Manara, Paola ; Buza, Natalia ; Zammataro, Luca ; Azodi, Masoud ; Schlessinger, Joseph ; Menderes, Gulden ; Manzano, Aranzazu ; Bellone, Stefania ; Cocco, Emiliano ; Huang, Gloria S. ; Litkouhi, Babak ; Bonazzoli, Elena ; Silasi, Dan-Arin ; Bianchi, Anna ; Santin, Alessandro D. ; Wong, Serena ; Predolini, Federica ; Schwartz, Peter E. ; Han, Chanhee ; Pettinella, Francesca ; Ratner, Elena

Abstract:

Purpose: Uterine serous carcinoma (USC) is a rare and aggressive variant of endometrial cancer. Whole-exome sequencing (WES) studies have recently reported c-Myc gene amplification in a large number of USCs, suggesting c-Myc as a potential therapeutic target. We investigated the activity of novel BET bromodomain inhibitors (GS-5829 and GS-626510, Gilead Sciences Inc.) and JQ1 against primary USC cultures and USC xenografts.Experimental Design: We evaluated c-Myc expression by qRT-PCR in a total of 45 USCs including fresh-frozen tumor tissues and primary USC cell lines. We also performed IHC and Western blot experiments in 8 USC tumors. USC cultures were evaluated for sensitivity to GS-5829, GS-626510, and JQ1 in vitro using proliferation, viability, and apoptosis assays. Finally, the in vivo activity of GS-5829, GS-626510, and JQ1 was studied in USC-ARK1 and USC-ARK2 mouse xenografts.Results: Fresh-frozen USC and primary USC cell lines overexpressed c-Myc when compared with normal tissues (P = 0.0009 and 0.0083, respectively). High c-Myc expression was found in 7 of 8 of primary USC cell lines tested by qRT-PCR and 5 of 8 tested by IHC. In vitro experiments demonstrated high sensitivity of USC cell lines to the exposure to GS-5829, GS-626510, and JQ1 with BET inhibitors causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis). In comparative in vivo experiments, GS-5829 and/or GS-626510 were found more effective than JQ1 at the concentrations/doses used in decreasing tumor growth in both USC-ARK1 and USC-ARK2 mouse xenograft models.Conclusions: GS-5829 and GS-626510 may represent novel, highly effective therapeutics agents against recurrent/chemotherapy-resistant USC-overexpressing c-Myc. Clinical studies with GS-5829 in patients with USC harboring chemotherapy-resistant disease are warranted. Clin Cancer Res; 24(19); 4845–53. ©2018 AACR.

项与 Alobresib 相关的新闻（医药）

2023-09-11

·SYNAPSE

Latest Developments in the Research and Development of BET inhibitor

BET (Bromodomain and Extra-Terminal) proteins play a crucial role in the regulation of gene expression in the human body. These proteins are involved in the recognition and binding of acetylated lysine residues on histone proteins, which are responsible for controlling gene transcription. By binding to these acetylated lysine residues, BET proteins facilitate the recruitment of transcriptional machinery and other regulatory proteins to specific gene loci, thereby influencing gene expression. This makes BET proteins important regulators of various cellular processes, including cell growth, differentiation, and inflammation. Due to their involvement in gene regulation, BET proteins have emerged as potential therapeutic targets for various diseases, including cancer and inflammatory disorders. BET Competitive LandscapeAccording to the data provided by Patsnap Synapse-Global Drug Intelligence Database: the following figure shows that as of 8 Sep 2023, there are a total of 60 BET drugs worldwide, from 62 organizations, covering 64 indications, and conducting 83 clinical trials. 👇Please click on the picture link below for free registration or login directly if you have freemium accounts, you can browse the latest research progress on drugs , indications, organizations, clinical trials, clinical results, and drug patents related to this target. The current competitive landscape of target BET is characterized by the presence of multiple companies at different stages of development. MorphoSys AG is leading with drugs in Phase 3 and Phase 2. Bristol Myers Squibb Co., GSK Plc, Zenith Epigenetics Ltd., and other companies also have drugs in advanced stages of development. The indications for drugs under target BET cover a wide range of diseases, including various types of cancers. Small molecule drugs, AAV based gene therapy, PROTACs, and other drug types are being researched and developed for target BET. The development of target BET is progressing in countries such as the United States, Canada, European Union, Spain, United Kingdom, and China. China has shown progress in the development of drugs for target BET. The future development of target BET is expected to witness intense competition, especially in the small molecule drug category, as indicated by the presence of biosimilars. Further research and development by pharmaceutical companies and institutions will contribute to the advancement of treatments for diseases associated with target BET. BET Inhibitor in Phase III Clinical Trials: PelabresibPelabresib is a small molecule drug that falls under the category of biomedicine. It specifically targets BET proteins, which are involved in various cellular processes and have been implicated in the development and progression of several diseases. The drug is being developed by Constellation Pharmaceuticals, Inc., a pharmaceutical company specializing in the field of epigenetics. Pelabresib has shown potential therapeutic benefits in the treatment of various diseases, particularly those related to the hemic and lymphatic systems. It has demonstrated efficacy in the treatment of osteomyelofibrosis, a rare bone marrow disorder characterized by the replacement of bone marrow with fibrous tissue. The drug has also shown promise in the treatment of primary myelofibrosis, a chronic blood cancer that affects the bone marrow and leads to the formation of scar tissue. 👇Please click on the image below to directly access the latest data (R&D Status | Core Patent | Clinical Trial | Approval status in Global countries) of this drug. In addition to these indications, pelabresib has shown activity against acute myeloid leukemia, a type of cancer that affects the blood and bone marrow. It has also shown potential in the treatment of bone marrow neoplasms, which are abnormal growths or tumors that develop in the bone marrow. Furthermore, the drug has demonstrated efficacy in myelodysplastic syndromes, a group of disorders characterized by abnormal production of blood cells in the bone marrow. Currently, pelabresib has reached Phase 3 of clinical development. This phase involves large-scale clinical trials to evaluate the safety and efficacy of the drug in a larger patient population. The results from these trials will provide crucial data to support the potential approval and commercialization of pelabresib. In summary, pelabresib is a small molecule drug developed by Constellation Pharmaceuticals, Inc. It targets BET proteins and has shown potential therapeutic benefits in the treatment of various diseases, including osteomyelofibrosis, primary myelofibrosis, acute myeloid leukemia, bone marrow neoplasms, and myelodysplastic syndromes. The drug is currently in Phase 3 of clinical development, and further studies will determine its safety and efficacy for potential approval and commercialization. BET inhibitor entering clinical phase II: AlobresibAlobresib is a small molecule drug that falls under the category of biomedicine. It specifically targets BET, which stands for bromodomain and extra-terminal proteins. This drug has shown potential in treating various therapeutic areas including neoplasms, urogenital diseases, immune system diseases, and hemic and lymphatic diseases. 👇Please click on the image below to directly access the latest data (R&D Status | Core Patent | Clinical Trial | Approval status in Global countries) of this drug. In terms of active indications, Alobresib has demonstrated efficacy in the treatment of prostatic cancer and diffuse large B-cell lymphoma. These are both serious and potentially life-threatening conditions, making the development of effective treatments crucial. The originator organization of Alobresib is Gilead Sciences, Inc. Gilead Sciences is a renowned pharmaceutical company known for its contributions to the field of biomedicine. As the originator organization, Gilead Sciences is responsible for the initial discovery and development of Alobresib. Currently, Alobresib has reached Phase 2 of clinical development. Clinical trials are an essential part of drug development, as they help determine the safety and efficacy of a drug in a controlled setting. Phase 2 trials involve a larger number of participants and aim to further evaluate the drug's effectiveness and side effects. In summary, Alobresib is a small molecule drug that targets BET and shows promise in treating various therapeutic areas such as neoplasms, urogenital diseases, immune system diseases, and hemic and lymphatic diseases. It is actively being studied for its potential in treating prostatic cancer and diffuse large B-cell lymphoma. Gilead Sciences, Inc. is the originator organization behind the development of Alobresib. Currently, the drug has reached Phase 2 of clinical trials, indicating progress in its development and potential for future use in patients.

2023-02-22

·PATSNAP

创新征程火力全开的加科思

开年以来，加科思药业喜讯频频，先是Aurora A抑制剂JAB-2485在美国完成首例患者给药，随后加科思宣布世界卫生组织（WHO）选定“Glecirasib”为其自主研发的KRAS G12C抑制剂JAB-21822的国际非专利药品名称（INN），这样一个极具创新力的公司自然赢得了大家的关注，今天让我们一起来看看加科思的发展之路。 2015年7月，加科思（Jacobio）药业在北京成立，公司创始人是王印祥博士。王博士之前是贝达药业的总裁兼首席科学家，有三十多年的肿瘤研究经历，曾主导中国第一款靶向抗肿瘤药盐酸埃克替尼（Icotinib）的研发与上市，丰富的研究经历让王博士的“二次创业”一路高歌猛进，此次一同创业的伙伴还有曾今贝达药业的诸多伙伴，比如副总裁王晓洁、高级副总裁胡云雁、化学部主任龙伟博士和研发中心药理部主任王燕萍等人。纵观加科思药业的药物开发，其主要围绕六大肿瘤信号通路，包括KRAS信号通路、MYC信号通路、P53信号通路、RB信号通路、肿瘤代谢通路以及肿瘤免疫通路，这六大信号通路覆盖约70-80%的癌症类型。公司在研药物约40种，其中进入临床阶段的就有7款，包括KRAS G12C抑制剂JAB-21822、SHP2抑制剂JAB-3068和JAB-3312、BET（BRPF2）抑制剂JAB-8263、Aurora A抑制剂JAB-2485、CD73抑制剂JAB-BX102（抗体）和FGFR4拮抗剂JAB-6343。除此之外，加科思药业还在诸多前沿靶点上进行布局，如PARP7、P53Y220C、KRASG12D和KRASG12V等。如今，公司立志做核心项目全球前三的诺言正在逐步实现，全球第二个进入临床的同类产品SHP2抑制剂JAB-3312和JAB-3068，这也是加科思管线中进展最快的药物。全球第三个进入临床的同类产品Aurora A抑制剂JAB-2485，于今年年初在美国完成首例患者给药。除此之外，BET抑制剂JAB-8263和KRAS G12C抑制剂JAB-21822有望成为同类产品中的最佳。 SHP2抑制剂当前还未有获批上市的SHP2抑制剂，据不完全统计，临床在研的SHP2抑制剂共计28款，其中小分子药物23款，而进入临床阶段的有15款均为小分子药物，其中加科思药业的JAB-3312和JAB-3068、赛诺菲的RMC-4630和诺华制药的TNO-155进展最快，均已进入临床2期阶段，不出意外的话，未来全球首个获批上市的SHP2抑制剂应该就在这几家企业中产生，而加科思药业布局两款SHP2抑制剂，从概率上来说赢面更大，期待后续表现。现有研究表明，JAB-3312和JAB-3068可能对具有某些特定基因突变的非小细胞肺癌、头颈鳞癌、食管鳞癌、结直肠癌、胰腺癌的患者有效，以及患有第三类BRAF突变或NF1功能缺失突变实体瘤的患者或能从中获益。从2019年的全球肿瘤发病数据估算，全球120万晚期实体瘤者有望从SHP2抑制剂单药疗法中受益。此外，SHP2抑制剂已显示出与多种靶向疗法和免疫疗法有协同作用，如靶向KRAS、EGFR、PD-1、MEK等。 Aurora A抑制剂 RB（Retinoblastoma）是重要的抑癌基因，但在小细胞肺癌患者中RB基因的缺失是非常普遍的现象。其缺失导致肿瘤细胞的纺锤体组装检查点（SAC）蛋白功能持续激活，造成肿瘤细胞的有丝分裂过度活跃，促使肿瘤快速生长。最新研究表明，RB缺失的肿瘤对Aurora A抑制剂十分敏感，靶向Aurora A可在RB缺失的肿瘤中，通过合成致死（Synthetic Lethality）的原理有效干扰有丝分裂，杀死肿瘤。当前也还未有获批上市的Aurora A抑制剂，据不完全统计，当前在研的Aurora A抑制剂有31种，其中小分子化药28种，进入临床研究阶段的有14款，这些Aurora A抑制剂大多数为多靶点药物。研究表明，靶向Aurora B会导致许多副作用，因此开发选择性的Aurora A抑制剂有望改善这一现状，当前进入临床阶段的选择性Aurora A药物仅有4款，分别为武田制药的Alisertib、礼来制药的Erbumine（LY-3295668）、加科思的JAB-2485和苏州君境生物的WJ-05129。加科思药业的JAB-2485是高选择性极光激酶A（Aurora Kinase A，AURKA）抑制剂，它对极光激酶B的选择性为2000多倍。临床前数据表明，JAB-2485具有更好的有效性和安全性，有望使RB缺失的小细胞肺癌患者、AURKA高表达的肿瘤患者获益，故而作为新一代选择性Aurora A抑制剂，具有非凡的潜力。 BET抑制剂溴结构域和超末端结构域（BET）家族包含4个功能相似蛋白：BRD2、BRD3、BRD4和BRDT。BET通过控制癌基因如c-MYC的表达在肿瘤发生中发挥关键作用。BET蛋白可特异性识别赖氨酸乙酰化的组蛋白，从而调控基因转录，亦可通过对转录因子等非组蛋白的乙酰化修饰而广泛参与细胞周期、细胞分化、信号转导等过程。肿瘤细胞中BET的活性增加可导致促肿瘤蛋白MYC的高表达，进而促进肿瘤的生长。MYC作为转录因子，是一个经典的致癌基因，因其蛋白结构散乱而长期难以被直接靶向，而BET抑制剂的开发正好解决这一难题，同时选择性BET抑制剂的开发有望解决上一代同时靶向BD1和BD2结构域所带来的副作用，包括BD1选择性抑制剂、BD2选择性抑制剂和BRD4选择性抑制剂。据不完全统计，与JAB-8263同靶点（BRPF2）的在研BET抑制剂共计18款，其中进入临床的有10款，选择性靶向BRPF2的BET抑制剂9款，包括进入临床2期研究的Alobresib、BMS-986158、JAB-8263和ZEN-3694等。总体来看，BET抑制剂开发这条赛道已经拥挤了起来，好在加科思声称其自主研发的创新药JAB-8263是现有同类临床项目中活性最强的BET抑制剂，临床前研究显示，JAB-8263可在极低剂量下有效抑制多种肿瘤生长，包括血液肿瘤和实体瘤。加科思目前正在中国和美国开展多中心、开放性I/IIa期临床研究，我们期待后续的表现。 KRAS G12C抑制剂相较于其它靶点，当前KRAS G12C靶点药物的开发可谓是卷到极致，据不完全统计，当前在研的KRAS抑制剂高达158种，其中小分子化药89款，进入临床研究阶段的41款，其中两款KRAS G12C抑制剂获批上市，分别为安进制药的Sotorasib和Mirati Therapeutics的Adagrasib。其次进展最快的是诺华制药的JDQ-443和罗氏制药的GDC-6036，已达临床3期。然后是进入临床2期研究的KRAS G12C抑制剂，包括加科思的JAB-21822、益方生物的D-1553、劲方医药的GF-105（GFH925或IBI-351）、勤浩医药的GH-35等。 JAB-21822是加科思自主研发的KRAS G12C变构抑制剂，1期临床数据显示该药具有良好的疗效和安全性，有望成为同类最佳分子。截至2022年4月1日共入组72例晚期实体瘤患者。其中有疗效评估的KRAS G12C突变的非小细胞肺癌患者共32例，客观缓解率（ORR）为56.3%（18/32），疾病控制率（DCR）为90.6%（29/32）。根据已公布的数据可以看出，在同类产品中，KRAS G12C抑制剂JAB-21822的ORR和DCR具有竞争优势，有望在后续的竞争中分得一块蛋糕，但患者人数仍然较少，有待在进一步的实验中验证该结果。 JAB-21822不但能单药用于治疗带有KRAS G12C突变的非小细胞肺癌、胰腺癌、结直肠癌等实体瘤，而且与SHP2抑制剂JAB-3312（NCT05288205）、EGFR抑制剂西妥昔单抗（NCT05002270、NCT05194995）、PD-1单抗联合用药，有望实现更优疗效，以及克服继发性耐药。总结加科思药业依托其独有的诱导变构药物发现平台，针对六大肿瘤信号通路开发创新药物，在靶点布局和临床进展上争做全球领先，逐渐建立起自己的肿瘤治疗护城河，是一个创新力十足且前景光明的制药公司，希望加科思药业的在研药物早日获批，造福广大患者！参考来源： 1.《致力于“不可成药”靶点的加科思，能否超越埃克替尼的成就？》，丰硕创投，2021 2.加科思官网，2022 3.智慧芽新药情报库 4.《加科思厂子都建起来了，野心很大啊……》，腾讯网，2022 5.Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development，2021-3 6.《BET抑制剂的开发进展》，雪球网，2021-10 7.《全球第二款KRAS 抑制剂获批上市，adagrasib能否成功逆袭？》，医学界，2022-12 8.《D-1553治疗KRAS G12C突变的晚期或转移性实体瘤》，健康界，2022-12 9.《国产抗癌药JAB-21822向最难攻克的KRAS靶点宣战！》，健康界，2022-6 10.《获批突破性疗法！国产KRAS肺癌新药JAB-21822突围！》，健康界，2022-12 11.《2022 AACR | ORR达57%，KRAS G12C新药JDQ443初步结果首亮相！》，医脉通，2022-4 12.《非小细胞肺癌KRAS G12C抑制剂GDC-6036客观缓解率53%》，全球肿瘤医生，2022-8

突破性疗法临床研究小分子药物

2021-07-29

·GlobeNewswire

Kura Oncology Appoints Helen Collins, MD to Board of

SAN DIEGO, July 29, 2021 (GLOBE NEWSWIRE) -- Kura Oncology, Inc. (Nasdaq: KURA), a clinical-stage biopharmaceutical company committed to realizing the promise of precision medicines for the treatment of cancer, today announced the appointment of industry veteran Helen Collins, M.D., to its board of directors. Dr. Collins served as Chief Medical Officer at Five Prime Therapeutics, where she oversaw the development of bemarituzumab, a first-in-class anti-FGFR2b antibody for the treatment of patients with gastric cancer. “With a deep background in medical oncology/hematology and significant experience leading clinical development programs targeting cancers of high unmet need, Helen brings a valuable perspective to the board as we continue to advance our pipeline of precision medicines,” said Troy Wilson, Ph.D., J.D., President and Chief Executive Officer of Kura Oncology. “On behalf of Kura Oncology and our board of directors, we want to welcome her to the board and look forward to drawing upon her strategic and clinical acumen as we work to fulfill our mission of bringing new treatment options to patients.” Dr. Collins joins the Kura board of directors with more than 25 years of medical experience. Most recently, she served as Executive Vice President and Chief Medical Officer at Five Prime Therapeutics, where she was responsible for the strategy and execution of the company’s clinical development plans until its acquisition by Amgen in April 2021. Previously, Dr. Collins held positions of increasing responsibility at Gilead Sciences, most recently as Program and Clinical Lead for Gilead’s GS-5829 (BET inhibitor) and GS-4059 (BTK inhibitor) programs, and Amgen, most recently as Global Lead of Oncology Biosimilars. Prior to her career in the biopharma industry, Dr. Collins practiced as a medical oncologist/hematologist for 12 years. She earned her M.D. from Johns Hopkins University School of Medicine, completing her residency at Johns Hopkins Hospital and oncology fellowship at Stanford University School of Medicine, and her B.A. from Bryn Mawr College. “I’m pleased to join the Kura board of directors as the company continues to build on the strong foundation of its clinical and preclinical pipeline,” said Dr. Collins. “I am impressed by the preliminary data from the menin inhibitor program, KO-539, in acute myeloid leukemia, as well as the broad therapeutic potential of the tipifarnib program, and I look forward to contributing to their continued progress and success.” About Kura Oncology Kura Oncology is a clinical-stage biopharmaceutical company committed to realizing the promise of precision medicines for the treatment of cancer. The Company’s pipeline consists of small molecule drug candidates that target cancer signaling pathways. KO-539, a potent and selective menin inhibitor, is currently in a Phase 1/2 clinical trial (KOMET-001) and targeting patients with relapsed/refractory acute myeloid leukemia, including patients with NPM1 mutations. Tipifarnib, a potent, selective and orally bioavailable farnesyl transferase inhibitor, has received Breakthrough Therapy Designation for the treatment of patients with HRAS mutant head and neck squamous cell carcinoma (HNSCC) and is currently in a registration-directed study (AIM-HN) in patients with this devastating disease. In addition, Kura is pursuing the use of tipifarnib in combination with other oncology therapeutics to address larger genetic subsets, including patients who have HRAS and/or PIK3CA-dependent HNSCC. The Company is also developing a next-generation farnesyl transferase inhibitor, which is intended to target innovative biology and larger oncology indications through rational combinations. For additional information about Kura, please visit the Company’s website at . Forward-Looking Statements This news release contains certain forward-looking statements that involve risks and uncertainties that could cause actual results to be materially different from historical results or from any future results expressed or implied by such forward-looking statements. Such forward-looking statements include statements regarding, among other things, the efficacy, safety and therapeutic potential of Kura’s drug candidates, tipifarnib and KO-539, progress and expected timing of Kura’s drug development programs and clinical trials and submission of regulatory filings, the presentation of data from clinical trials, plans regarding regulatory filings and future clinical trials, the regulatory approval path for tipifarnib, the strength of Kura’s balance sheet and the adequacy of cash on hand. Factors that may cause actual results to differ materially include the risk that compounds that appeared promising in early research or clinical trials do not demonstrate safety and/or efficacy in later preclinical studies or clinical trials, the risk that Kura may not obtain approval to market its drug candidates, uncertainties associated with performing clinical trials, regulatory filings, applications and other interactions with regulatory bodies, the risks associated with reliance on third parties to successfully conduct clinical trials, the risks associated with reliance on outside financing to meet capital requirements, the risks associated with the COVID-19 global pandemic, and other risks associated with the process of discovering, developing and commercializing drugs that are safe and effective for use as human therapeutics, and in the endeavor of building a business around such drugs. You are urged to consider statements that include the words "may," "will," "would," "could," "should," "believes," "estimates," "projects," "promise," "potential," "expects," "plans," "anticipates," "intends," "continues," "designed," "goal," or the negative of those words or other comparable words to be uncertain and forward-looking. For a further list and description of the risks and uncertainties the Company faces, please refer to the Company's periodic and other filings with the Securities and Exchange Commission, which are available at . Such forward-looking statements are current only as of the date they are made, and Kura assumes no obligation to update any forward-looking statements, whether as a result of new information, future events or otherwise. Contacts Company:Pete De SpainVice President, Investor Relations &Corporate Communications(858) 500-8803pete@kuraoncology.com Investors:Robert H. UhlManaging DirectorWestwicke ICR(858) 356-5932robert.uhl@westwicke.com Media:Jason SparkManaging DirectorCanale Communications(619) 849-6005jason@canalecomm.com

抗体突破性疗法生物类似药First in Class小分子药物

100 项与 Alobresib 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14970

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
ER阳性/HER2阴性乳腺癌	临床2期	美国	Gilead Sciences, Inc.	2017-01-10
ER阳性/HER2阳性乳腺癌	临床2期	美国	Gilead Sciences, Inc.	2017-01-10
转移性去势抵抗性前列腺癌	临床2期	美国	Gilead Sciences, Inc.	2015-12-08
晚期恶性实体瘤	临床1期	美国	Gilead Sciences, Inc.	2015-03-16
ER阳性乳腺癌	临床1期	美国	Gilead Sciences, Inc.	2015-03-16
淋巴瘤	临床1期	美国	Gilead Sciences, Inc.	2015-03-16

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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


NCT02607228 (Pubmed) 人工标引	临床1期	转移性去势抵抗性前列腺癌	31	GS-5829	糧構憲壓顧齋構艱鬱積(蓋鹽製餘壓廠繭鑰築膚) = 壓觸醖築窪遞遞繭獵餘壓窪簾艱糧願鹽製遞積 (獵壓積鹽淵壓願觸夢糧, 10 ~ 42) 更多	不佳	2022-07-11
NCT02392611 (CTgov)	临床1期	晚期恶性实体瘤 \| ER阳性乳腺癌 \| 淋巴瘤	33	Alobresib (Monotherapy: Alobresib 0.6 mg)	膚鏇鹽遞蓋廠鏇鏇鹹廠 = 鏇壓壓齋窪憲膚鹽鹹窪壓繭壓獵夢膚蓋獵構築 (壓淵簾範憲廠窪鏇餘糧, 壓鹽鹹遞糧繭製憲衊範 ~ 衊廠範鹽築構顧觸簾觸) 更多	-	2020-12-29
				Alobresib (Monotherapy: Alobresib 1.4 mg)	膚鏇鹽遞蓋廠鏇鏇鹹廠 = 鏇網鑰選夢繭齋網襯遞壓繭壓獵夢膚蓋獵構築 (壓淵簾範憲廠窪鏇餘糧, 遞鹹鹽夢簾憲構蓋獵鏇 ~ 衊鬱醖壓構構鏇糧鏇襯) 更多
NCT02607228 (CTgov)	临床1/2期	去势抵抗性前列腺癌 \| 转移性去势抵抗性前列腺癌	31	Alobresib (Monotherapy: Alobresib 2 mg)	獵範觸觸艱鬱鬱網廠醖 = 鹽衊憲蓋鹹製窪顧鹹蓋蓋淵繭觸簾構鏇鬱餘鏇 (醖壓願壓積築醖獵積繭, 遞選襯選壓壓製艱築簾 ~ 築廠醖遞網鹽鹹願糧醖) 更多	-	2020-12-08
				Alobresib (Monotherapy: Alobresib 3 mg)	獵範觸觸艱鬱鬱網廠醖 = 範範鑰艱鹽獵遞鏇糧壓蓋淵繭觸簾構鏇鬱餘鏇 (醖壓願壓積築醖獵積繭, 鏇窪簾遞艱鏇獵鏇選鹹 ~ 獵構積淵簾廠窪廠願夢) 更多
NCT02983604 (CTgov)	临床1/2期	ER阳性/HER2阳性乳腺癌 \| ER阳性/HER2阴性乳腺癌	14	Exemestane+GS-5829 (GS-5829 4 mg + Exemestane)	網鏇窪築夢範範選蓋憲 = 糧遞鏇齋蓋膚醖憲糧鹹蓋憲鹹網網製糧夢廠鑰 (鏇範觸顧構網築艱願窪, 蓋築糧繭鹹淵窪襯夢簾 ~ 製窪願醖網鏇鹽襯鬱衊) 更多	-	2019-08-07
				Fulvestrant+GS-5829 (GS-5829 4 mg + Fulvestrant)	網鏇窪築夢範範選蓋憲 = 願繭鑰觸簾鹽鏇蓋壓鏇蓋憲鹹網網製糧夢廠鑰 (鏇範觸顧構網築艱願窪, 醖窪蓋淵鑰襯範構鑰膚 ~ 淵鏇築壓齋廠願醖鬱淵) 更多