A Two-Part Phase 2a Study in Patients With End-Stage Renal Disease Treated With Hemodialysis; Part A is an Open-Label Study Arm to Evaluate the Effect of Hemodialysis on the Pharmacokinetics of 100 mg RVX000222; and Part B is a Double-Blind, Randomized, Placebo-Controlled, Sequential Cross-Over Study Arm to Evaluate the Efficacy, Safety, and Pharmacokinetics of RVX000222

This is a multi-center, two-part study; Part A and Part B. Part A of the study is an open-label, single-dose pharmacokinetic (PK) evaluation of 100 mg RVX000222 on dialysis and non-dialysis days in eight (8) End Stage Renal Disease (ESRD) patients who receive hemodialysis as standard of care.
Part B of the study is a double-blind, placebo-controlled study in up to thirty six (36) ESRD patients receiving hemodialysis using a sequential cross-over design with RVX000222 at a daily oral dose of 100 mg b.i.d. (200 mg per day) or matching placebo in combination with SoC.
The primary objective of the study is to evaluate if treatment with RVX000222 in combination with standard of care (SoC) decreases plasma alkaline phosphatase in comparison to placebo and SoC.

开始日期2024-11-22

申办/合作机构

Resverlogix Corp.

NCT04915300 / Not yet recruiting临床2期IIT

Apabetalone for Pulmonary Arterial Hypertension: a Phase 2 Clinical Study

Throughout the past twenty years, numerous specific pharmacologic agents targeting the endothelial dysfunction associated with PAH have emerged. Short term placebo-controlled randomized trials assessing PAH-specific monotherapy with these molecules have reported improvements in pulmonary hemodynamics and exercise capacity. A recent meta-analysis also documented a reduction in short-term mortality of about ≈40% with such therapies. Several randomized clinical trials evaluating PAH-specific combination therapy have been conducted. Our recent meta-analysis showed that combination therapy was associated with a 35% risk reduction for the occurrence of clinical worsening compared to monotherapy. Nonetheless, the investigators also showed 17% of PAH patients receiving combination therapy still experienced clinical worsening over a median exposure of 16 weeks. Moreover, long-term survival on PAH-specific also therapy remains poor in the modern era, with a yearly mortality rate of 15 % in incident idiopathic PAH. The identification of innovative therapeutic targets and validation of these complementary therapeutic interventions are thus urgently needed in PAH.
The investigators and others (K. Stenmark, University of Colorado and H. Bogaard, VU University Medical Center, Amsterdam, personal communications), have published strong evidence that BRD4 plays a key role in the pathological phenotype in PAH accounting for disease progression and showed that BRD4 inhibition can reverse PAH in several animal models. Intriguingly, coronary artery disease (CAD) and metabolic syndrome are more prevalent in PAH compared with the global population, suggesting a link between these diseases. Interestingly, BRD4 is also a trigger for calcification and remodeling processes and regulates transcription of lipoprotein and inflammatory factors, all of which are important in PAH and CAD. Apabetalone, an orally available BRD4 inhibitor, is now in a clinical development stage with a good safety profile.
The overall objective of the study is to explore the efficacy and safety of apabetalone as an add-on therapy for adult PAH patients and to inform the conduct and the design of a Phase 3 trial.
The primary objective of the study is to assess the efficacy of apabetalone as evaluated by the change in PVR over a period of 24 weeks compared to placebo in adult subjects with PAH on stable background therapy.
Secondary objectives include changes at week 24 in 6MWD, plasma NT-proBNP concentration, WHO functional class, ESC/ERS risk stratification score, health-related quality of life and additional hemodynamic data from right heart.
Exploratory objectives are to evaluate the effects of apabetalone compared to placebo in adult subjects with PAH on mortality and clinically relevant morbidity events, and on circulating levels and transcription changes in whole blood markers of metabolism, vascular calcification, inflammation, DNA damage and leucocyte expression of BMPR2.

开始日期2023-10-01

申办/合作机构

Université Laval

[+2]

NCT03228940 / Withdrawn临床1/2期

An Open-Label Study to Assess the Safety and Effect on Key Biomarkers of Oral RVX000222 in Subjects With Fabry Disease

Fabry Disease (FD) is a rare X-linked lysosomal storage disorder (LSD) caused by mutations in the GLA gene which translates into decreased activity or lack of function of the enzyme alpha-galactosidase A (α-GAL A) and accumulation of the enzymes substrate, i.e., Gb3, throughout the body. Cardiovascular and renal complications are among the leading causes of death in FD patients. RVX000222 is a BET inhibitor which modulates the expression of a variety of genes and, due to its effects on pathways downstream of substrate accumulation and reduction of major cardiac events, holds promise as a potential add-on therapy to accompany enzyme replacement therapy (ERT) in FD patients.

开始日期2022-11-22

申办/合作机构

Resverlogix Corp.

100 项与 Apabetalone 相关的临床结果

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100 项与 Apabetalone 相关的转化医学

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100 项与 Apabetalone 相关的专利（医药）

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项与 Apabetalone 相关的文献（医药）

2023-12-31·Translational neuroscience

The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation

Article

作者: Wong, Norman C W ; Daze, Emily ; Fu, Li ; Rakai, Brooke D ; Gilham, Dean ; Rinker, Kristina D ; Tsujikawa, Laura M ; Sarsons, Chris D ; Studer, Deborah ; Wasiak, Sylwia ; Jahagirdar, Ravi ; Johansson, Jan O ; Stotz, Stephanie C ; Kulikowski, Ewelina ; Sweeney, Michael

Abstract:

Brain vascular inflammation is characterized by endothelial activation and immune cell recruitment to the blood vessel wall, potentially causing a breach in the blood – brain barrier, brain parenchyma inflammation, and a decline of cognitive function. The clinical-stage small molecule, apabetalone, reduces circulating vascular endothelial inflammation markers and improves cognitive scores in elderly patients by targeting epigenetic regulators of gene transcription, bromodomain and extraterminal proteins. However, the effect of apabetalone on cytokine-activated brain vascular endothelial cells (BMVECs) is unknown. Here, we show that apabetalone treatment of BMVECs reduces hallmarks of in vitro endothelial activation, including monocyte chemoattractant protein-1 (MCP-1) and RANTES chemokine secretion, cell surface expression of endothelial cell adhesion molecule VCAM-1, as well as endothelial capture of THP-1 monocytes in static and shear stress conditions. Apabetalone pretreatment of THP-1 downregulates cell surface expression of chemokine receptors CCR1, CCR2, and CCR5, and of the VCAM-1 cognate receptor, integrin α4. Consequently, apabetalone reduces THP-1 chemoattraction towards soluble CCR ligands MCP-1 and RANTES, and THP-1 adhesion to activated BMVECs. In a mouse model of brain inflammation, apabetalone counters lipopolysaccharide-induced transcription of endothelial and myeloid cell markers, consistent with decreased neuroendothelial inflammation. In conclusion, apabetalone decreases proinflammatory activation of brain endothelial cells and monocytes in vitro and in the mouse brain during systemic inflammation.

2023-12-01·Journal of clinical periodontology

Selective BET inhibitor RVX‐208 ameliorates periodontal inflammation and bone loss

Article

作者: Clayton, Nicholas ; Sahingur, Sinem Esra ; Giannobile, William V ; Lin, Zhao ; Wong, Andrew ; Carrico, Caroline K ; Kim, Jin Ha ; Boyan, Barbara D ; Asmussen, Niels ; Pellei, David ; Mokhtari, Sasan ; Alam, Sheikh ; Luong, Gary ; Sun, Mingxu ; Schwartz, Zvi

Abstract:

Aim:

To determine the effects of RVX‐208, a selective bromodomain and extra‐terminal domain (BET) inhibitor targeting bromodomain 2 (BD2), on periodontal inflammation and bone loss.

Materials and Methods:

Macrophage‐like cells (RAW264.7) and human gingival epithelial cells were challenged by Porphyromonas gingivalis (Pg) with or without RVX‐208. Inflammatory gene expression and cytokine production were measured by reverse transcription polymerase chain reaction and enzyme‐linked immunosorbent assay, respectively. RAW264.7 cells were induced to osteoclast differentiation. After RVX‐208 treatment, osteoclast differentiation was evaluated by histology, tartrate‐resistant‐acid‐phosphatase (TRAP) activity and the expression of osteoclast‐specific genes. The effect of RVX‐208 on osteoclast transcriptome was studied by RNA sequencing. Periodontitis was induced in rats by ligature and local RVX‐208 treatment was administered every other day. Alveolar bone loss was measured by micro‐computed tomography.

Results:

RVX‐208 inhibited inflammatory gene expression and cytokine production in Pg‐infected cells. Osteoclast differentiation was inhibited by RVX‐208, as evidenced by reduced osteoclast number, TRAP activity and osteoclast‐specific gene expression. RVX‐208 displayed a more selective and less profound suppressive impact on transcriptome compared with pan‐BET inhibitor, JQ1. RVX‐208 administration prevented the alveolar bone loss in vivo.

Conclusions:

RVX‐208 regulated both upstream (inflammatory cytokine production) and downstream (osteoclast differentiation) events that lead to periodontal tissue destruction, suggesting that it may be a promising ‘epi‐drug’ for the prevention of periodontitis.

2023-12-01·Antiviral therapy

RVX-208, an inducer of Apolipoprotein A-I, inhibits the particle production of hepatitis B virus through activation of cGAS-STING pathway

Article

作者: Cheng, Lin ; Liu, Dan ; Yuan, Kefei ; Wei, He ; Shu, Dan

Background:

Previously, we have demonstrated that Apolipoprotein A-I (ApoA-I) could inhibit the secretion of Hepatitis B virus (HBV), suggesting that stimulation of ApoA-I may block particle production. In the present study, we evaluated the anti-HBV effect of RVX-208, a small-molecule stimulator of ApoA-I gene expression.

Methods:

RVX-208 was used to treat HepG2.2.15 cell, a HepG2 derived cell line stably producing HBV virus. Real-time PCR was performed to examine the HBV DNA levels. Magnetic particles, which were coated with anti-HBS or anti-HBE antibody, were used to examine the HBsAg and HBeAg levels in the supernatant of cultured HepG2.2.15 cells in combination with the enzyme conjugates that were prepared with horseradish peroxidase labelled anti-HBS or anti-HBE antibody in a double antibody sandwich manner. RNA-seq, immunoblots and real-time PCR were used to analyze the functional mechanism of RVX-208.

Results:

RVX-208 could elevate the ApoA-I protein levels in HepG2.2.15 cells. In the meantime, RVX-208 significantly repressed HBV DNA, HBsAg and HBeAg levels in the supernatants of HepG2.2.15 cells. RNA-seq data revealed that RVX-208 treatment not only affected the cholesterol metabolism, which is closely related to ApoA-I, but also regulated signalling pathways that are associated with antiviral immune response. Moreover, mechanistic studies demonstrated that RVX-208 could activate cGAS-STING pathway and upregulate the transcription of a series of interferons, pro-inflammatory cytokines and chemokines with antiviral potential that are at the downstream of cGAS-STING pathway.

Conclusion:

Our study demonstrated that RVX-208, an inducer of ApoA-I, could suppress HBV particle production through activation of cGAS-STING pathway.

项与 Apabetalone 相关的新闻（医药）

2024-05-28

·BioSpace

Resverlogix Announces Updated Annual and Special Meeting of Shareholders

Calgary, Alberta--(News - May 28, 2024) - Resverlogix Corp. (TSX: RVX) ("Resverlogix" or the "Company") announced today that its Annual and Special Meeting of Shareholders (the "Meeting") will be held on Wednesday, July 31, 2024, commencing at approximately 1:00 pm (MT), as opposed to as previously scheduled for June 27, 2024. A Notice of Meeting and Management Information Circular, containing the matters to be considered at the Meeting, will be delivered to shareholders and filed on SEDAR+ at . Following the formal business of the Meeting, a corporate update presentation will be provided. About Resverlogix Founded in 2001, Resverlogix is a Calgary based late-stage biotechnology company, and a world leader in epigenetics, with the goal of developing first-in-class therapies for the benefit of patients with chronic disease. Resverlogix is developing a new class of epigenetic therapies designed to regulate the expression of disease-causing genes. We aim to improve patients' lives by restoring biological functions – altered by serious illnesses such as cardiovascular disease – back to a healthier state. The Company's clinical program is focused on evaluating the lead epigenetic candidate apabetalone for the treatment of cardiovascular disease, associated comorbidities, and post COVID-19 conditions. Resverlogix has partnered with EVERSANA™, the pioneer of next generation commercial services to the global life sciences industry, to support the rapid commercialization of apabetalone for cardiovascular disease, post COVID-19 conditions, and pulmonary arterial hypertension in Canada and the United States. Resverlogix common shares trade on the Toronto Stock Exchange (TSX: RVX). Follow us on: Twitter: @Resverlogix_RVX LinkedIn: Forward-Looking Statements: This news release may contain certain forward-looking information as defined under applicable Canadian securities legislation, that are not based on historical fact, including without limitation statements containing the words "believes", "anticipates", "plans", "intends", "will", "should", "expects", "continue", "estimate", "forecasts", and other similar expressions. In particular, this news release includes forward looking information related to the upcoming Annual and Special Meeting of Shareholders and the potential role of apabetalone in the treatment of patients with cardiovascular disease, post COVID-19 conditions, pulmonary arterial hypertension, associated comorbidities, and other chronic diseases. Our actual results, events or developments could be materially different from those expressed or implied by these forward-looking statements. We can give no assurance that any of the events or expectations will occur or be realized. By their nature, forward-looking statements are subject to numerous assumptions and risk factors including those discussed in our Annual Information Form and most recent MD&A which are incorporated herein by reference and are available through SEDAR+ at . The forward-looking statements contained in this news release are expressly qualified by this cautionary statement and are made as of the date hereof. The Company disclaims any intention and has no obligation or responsibility, except as required by law, to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. For further information please contact: Investor Relations Email: ir@resverlogix.com Phone: 403-254-9252 Or visit our website: To view the source version of this press release, please visit

2024-02-22

·BioSpace

Resverlogix Announces Change to Its Board of Directors.

Calgary, Alberta--(News - February 21, 2024) - Resverlogix Corp. (TSX: RVX) ("Resverlogix" or the "Company") today announced that Shawn Lu has stepped down from the Board of Directors, effective today. "We would like to thank Shawn for his contributions and wish him all the best," said Donald McCaffrey, Resverlogix's President and CEO. About Resverlogix Founded in 2001, Resverlogix is a Calgary based late-stage biotechnology company, and a world leader in epigenetics, with the goal of developing first-in-class therapies for the benefit of patients with chronic disease. Resverlogix is developing a new class of epigenetic therapies designed to regulate the expression of disease-causing genes. We aim to improve patients' lives by restoring biological functions - altered by serious illnesses such as cardiovascular disease - back to a healthier state. The Company's clinical program is focused on evaluating the lead epigenetic candidate apabetalone for the treatment of cardiovascular disease, associated comorbidities, and post COVID-19 conditions. Resverlogix has partnered with EVERSANA™, the pioneer of next generation commercial services to the global life sciences industry, to support the rapid commercialization of apabetalone for cardiovascular disease, post COVID-19 conditions, and pulmonary arterial hypertension in Canada and the United States. Resverlogix common shares trade on the Toronto Stock Exchange (TSX: RVX). Follow us on: Twitter: @Resverlogix_RVX LinkedIn: For further information please contact: Investor Relations Email: ir@resverlogix.com Phone: 403-254-9252 Or visit our website: This news release may contain certain forward-looking information as defined under applicable Canadian securities legislation, that are not based on historical fact, including without limitation statements containing the words "believes", "anticipates", "plans", "intends", "will", "should", "expects", "continue", "estimate", "forecasts", and other similar expressions. In particular, this news release includes forward looking information related to the potential role of apabetalone in the treatment of patients with cardiovascular disease, post COVID-19 conditions, pulmonary arterial hypertension, associated comorbidities, and other chronic diseases. Our actual results, events or developments could be materially different from those expressed or implied by these forward-looking statements. We can give no assurance that any of the events or expectations will occur or be realized. By their nature, forward-looking statements are subject to numerous assumptions and risk factors including those discussed in our Annual Information Form and most recent MD&A which are incorporated herein by reference and are available through SEDAR at . The forward-looking statements contained in this news release are expressly qualified by this cautionary statement and are made as of the date hereof. The Company disclaims any intention and has no obligation or responsibility, except as required by law, to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. To view the source version of this press release, please visit

高管变更

2024-02-06

·生物制药小编

“小分子“开发“大分子”靶标

近一个世纪，小分子药物一直是制药行业的中流砥柱。小分子药物被定义为低分子量（＜1000Da）的有机化合物，作为治疗药物具有一些明显的优势：大多数可以口服给药，并且可以穿过细胞膜到达细胞内靶标。还可以被设计成通过各种作用模式与生物靶点接触，它们的分布可以进一步定制，例如允许在有或没有大脑穿透的情况下进行全身暴露。随着Humira、Keytruda、Stelara等生物制剂不断刷新销售记录，制药公司在药物开发选择方向上越来越多地面临“小分子还是生物制剂”的选择。尽管生物制剂取得了显著的成就，但小分子药物仍然在行业中占据统治地位。随着技术的更新，小分子药物也在不断创造新的发展条件。下面小编将带大家一起对小分子药物进行一次全面的认识。小分子药物开发的优势和挑战小分子药物开发是目前药物研发领域的主流，其具有许多优势和挑战。优势：①首先，小分子药物具有较小的分子量和较简单的化学结构，这使得它们易于合成和修改，从而提高了药物开发的效率。②此外，小分子药物通常具有较好的口服生物利用度，可以通过口服给药途径进行治疗，提高患者的便利性和治疗依从性。挑战：①首先，小分子药物往往具有较短的半衰期，需要频繁的给药以维持治疗效果。②此外，小分子药物通常具有较高的代谢和排泄速率，容易被机体代谢和清除，从而限制了其在体内的持续作用时间。③此外，小分子药物的选择性和特异性较低，容易与其他分子发生非特异性相互作用，导致副作用的发生。尽管面临一些限制，小分子药物仍然是目前药物研发的主要方向，其在临床应用和市场上具有广泛的应用前景。开发大分子靶标的意义大分子靶标是指具有较大分子量的蛋白质或其他生物大分子，其特点和应用领域在药物开发中具有重要意义。大分子靶标通常具有复杂的结构和功能，与小分子靶标相比，其药物开发过程更加复杂和挑战性。首先，大分子靶标具有更高的特异性。由于其复杂的结构和功能，大分子靶标通常具有更高的特异性，能够更精确地与药物相互作用。这使得大分子靶标在疾病治疗中具有更好的选择性，能够减少对正常细胞的不良影响。其次，大分子靶标在药物开发中具有更广泛的应用领域。大分子靶标在多个疾病领域中发挥着重要作用，如癌症、免疫系统疾病、神经系统疾病等。通过针对大分子靶标的药物开发，可以实现对这些疾病的精准治疗，提高治疗效果和患者生活质量。此外，大分子靶标在临床应用中具有一定的挑战性。由于大分子药物的复杂性和制备难度，其临床应用往往面临一些挑战。例如，大分子药物的制备成本较高，需要更复杂的生产工艺和设备。此外，大分子药物在体内的稳定性和药代动力学也需要更多的研究和优化。小分子药物开发大分子靶标近期发表在C&EN上的一篇文章展望了小分子药物的前景。文章认为小分子药物的开发将迎来一个新的阶段，且在医药领域发挥重要作用。分子胶和PROTAC等新型小分子药物也正在不断向前发展以推动人类疾病治疗。此外，人工智能的应用也将直接推动小分子药物的设计和开发。图注：2013-2022年间FDA批准药物的对比。图片来源：C&EN目前CD33、CD30、HER2、CD22、CD79b、Nectin-4、BCMA、EGFR、CD19、TissueFactor和FRα等靶点已经是上市小分子药物的成熟靶点，在研靶点包括HER2、EGFR、CLDN18.2、TROP2、c-Met、CD19、PSMA、Muc1、BCMA和PDL1。目前在开发大分子靶标方面，有许多小分子正在被研究和开发：● 抗癌药物：包括靶向蛋白激酶的小分子抑制剂，如吉非替尼（Gefitinib）和厄洛替尼（Erlotinib）用于EGFR阳性非小细胞肺癌的治疗；以及靶向蛋白酶的小分子抑制剂，如伊马替尼（Imatinib）用于慢性髓性白血病的治疗。● 免疫调节药物：包括靶向免疫检查点的小分子抑制剂，如伊普替尼（Ipilimumab）和尼伦帕尼布（Nivolumab）用于恶性黑色素瘤的治疗。● 炎症性疾病药物：包括靶向炎症介质的小分子抑制剂，如阿帕替尼布（Apabetalone）用于治疗心血管疾病。● 病毒感染药物：包括靶向病毒复制过程的小分子抑制剂，如奥司他韦（Oseltamivir）用于流感病毒感染的治疗。● 神经系统疾病药物：包括靶向神经递质受体的小分子调节剂，如多巴胺受体激动剂用于帕金森病的治疗。共价抑制剂、蛋白质降解技术（如PROTAC）、分子胶、分子门、人工智能的发展为小分子药物设计和开发提供了更多的模式与方法，有望加速新药的推出并降低研发的成本。图注：海外临床在研PROTAC药物（资料来源：安信证券研究中心）图注：国内临床在研PROTAC药物（资料来源：安信证券研究中心）根据Mordor Intelligence的报告，小分子药物发现市场预计将在2023年达到523.5亿美元，并以年增长率8.76%增长，到2028年将达到796.7亿美元。一些公司如ICON Plc、Charles River Laboratories和Labcorp在该市场上扮演重要角色。根据X-MOL的报道，2022年药物销售业绩Top 10中，生物制剂占据了6个位置，小分子药物占据了4个位置。但是考虑到生物制剂的生产成本较高，总体来说，小分子的成绩或许更亮眼。根据在Medicine in Drug Discovery 上发表的一篇文章，小分子仍处于创新药物研发的范畴，在全球范围内销售的所有药物中，约 90% 是小分子，其RNA靶向活性、抑癌活性、抗病毒活性等逐步被发掘，此外在考虑成本以及受众群体再到新技术开发等方面，小分子仍然在治疗领域占据不可替代的地位。在 FDA 2017-2022 年批准的 293 个新化学实体（NCE）中，182 个是小分子。不论是从数量上还是从市场实际情况上来看，小分子药物依然占据医药市场的统治地位。未来发展方向和挑战小分子药物开发大分子靶标领域一直面临着许多挑战，但也有着广阔的发展前景。未来的发展方向将主要集中在以下几个方面：● 靶向多靶点治疗：随着对疾病机制的深入研究，我们发现许多疾病是由多个靶点的紊乱引起的。因此，未来的小分子药物开发将更加注重靶向多个靶点的治疗策略，以提高治疗效果。● 靶向特定亚型：许多疾病的发展与特定亚型的靶标有关。因此，未来的研究将更加注重发现和开发针对特定亚型的小分子药物，以实现个体化治疗。● 结构优化和药物设计：小分子药物的结构优化和药物设计是提高药物疗效和减少副作用的关键。未来的发展将更加注重利用计算机辅助药物设计和结构优化技术，以提高药物的选择性和亲和力。● 新技术的应用：随着科技的不断进步，新技术的应用将为小分子药物开发带来新的机遇。例如，基因编辑技术和纳米技术的应用将为小分子药物的靶向性和传递性提供更多可能性。然而，小分子药物开发在大分子靶标领域仍然面临着一些挑战：● 靶标的复杂性：大分子靶标通常具有复杂的结构和功能，这给小分子药物的开发带来了挑战。因此，研究人员需要深入了解靶标的结构和功能，以寻找合适的小分子药物。● 药物递送：大分子靶标通常位于细胞内或细胞膜上，而小分子药物需要通过细胞膜进入细胞内才能发挥作用。因此，药物的传递性是一个重要的挑战，需要寻找合适的传递载体或技术。● 药物耐受性和副作用：小分子药物的耐受性和副作用是开发过程中需要考虑的重要因素。研究人员需要寻找具有较低副作用和良好耐受性的小分子药物。● 临床试验的挑战：大分子靶标的临床试验通常需要更长的时间和更高的成本。因此，研究人员需要克服临床试验的挑战，以确保药物的安全性和有效性。总的来说，小分子药物开发大分子靶标领域面临着许多挑战，但也有着广阔的发展前景。通过针对多靶点治疗、靶向特定亚型、结构优化和药物设计以及新技术的应用，我们有望开发出更加有效和安全的小分子药物，为疾病治疗带来新的突破。然而，我们需要克服靶标的复杂性、药物传递性、药物耐受性和副作用以及临床试验的挑战，以实现小分子药物在大分子靶标领域的应用和推广。参考文章：1.A big future for small molecules: targeting the undruggable，AstraZeneca，August 2022， 2.Small Molecules，B. Lu, A. Atala, in In Situ Tissue Regeneration, 2016， 3.Visualizing molecular glues，Elizabeth Dougherty，Mar 27, 2020， 4.Makurvet, F. D. et. al. Biologics vs. small molecules: Drug costs and patient access. Med. Drug Discov., 2021, 9, 100075.5.ls this a golden age of small-molecule drug discovery? pubs.acs.org/doi/10.1021/cen-10136-cover6.Small molecules are sexy again’ : Gate Bioscience debuts with 560M and a new way to stop disease-causing proteins

100 项与 Apabetalone 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11131	-	-	DB12000

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
新型冠状病毒感染	临床3期	加拿大	Resverlogix Corp.	2022-01-14
冠心病	临床3期	阿根廷	Resverlogix Corp.	2015-11-01
冠心病	临床3期	澳大利亚	Resverlogix Corp.	2015-11-01
冠心病	临床3期	比利时	Resverlogix Corp.	2015-11-01
冠心病	临床3期	保加利亚	Resverlogix Corp.	2015-11-01
冠心病	临床3期	克罗地亚	Resverlogix Corp.	2015-11-01
冠心病	临床3期	德国	Resverlogix Corp.	2015-11-01
冠心病	临床3期	匈牙利	Resverlogix Corp.	2015-11-01
冠心病	临床3期	以色列	Resverlogix Corp.	2015-11-01
冠心病	临床3期	墨西哥	Resverlogix Corp.	2015-11-01

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临床结果

适应症

分期

评价

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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


NCT02586155 (BETonMACE, ERA2023)	临床3期	慢性肾病	-	Apabetalone 100 mg	範鹹鏇遞壓餘壓蓋淵鹽(遞製憲憲鹹廠醖襯廠鬱): HR = 0.5 (95% CI, 0.26 ~ 0.96), P-Value = 0.04	积极	2023-06-14
				Placebo
BETonMACE (ASN2021)	临床3期	-	-	Apabetalone 1-25 µ M	鹽選襯範糧餘鏇窪網齋(觸膚觸餘網艱糧淵鹽窪) = 遞鏇憲鏇夢壓齋鑰鬱蓋艱衊鏇壓糧範窪襯醖網 (範艱廠衊獵憲鹽簾遞窪 ) 更多	积极	2021-10-27
NCT03655704 (APPRoAcH-p, GlobeNewswire) 人工标引	临床1期	肺动脉高压	7	Apabetalone	蓋蓋選廠鹽鏇廠膚築積(醖壓糧製壓顧網鬱範簾) = improved 憲觸壓齋網積積窪醖廠 (構鏇觸簾夢鹹壓積艱艱 )	积极	2021-09-08
NCT02586155 (BETonMACE, CTgov)	临床3期	2型糖尿病 \| 冠心病	2,425	rosuvastatin+atorvastatin+Apabetalone (High-Intensity Statin Therapy+RVX000222)	襯積膚衊繭窪鹹願衊鬱(壓觸築齋鏇範鑰顧夢積) = 製觸製襯範鏇襯築廠襯顧淵顧繭醖鹽鑰構廠夢 (壓鹽願鑰簾觸網糧醖遞, 範繭淵窪蓋遞遞憲顧糧 ~ 憲糧範夢網壓鹹夢鏇築) 更多	-	2021-08-20
				Placebo+rosuvastatin+atorvastatin (High-Intensity Statin Therapy+Placebo)	襯積膚衊繭窪鹹願衊鬱(壓觸築齋鏇範鑰顧夢積) = 繭餘構壓鏇鹽壓積餘構顧淵顧繭醖鹽鑰構廠夢 (壓鹽願鑰簾觸網糧醖遞, 觸簾夢鑰構範齋顧觸憲 ~ 餘窪餘壓選淵範壓鑰鑰) 更多
BETonMACE2 (ERA2021)	临床3期	慢性肾病	-	APABETALONE	憲觸遞糧製繭觸網簾淵(餘淵製鏇築糧遞膚齋鹽) = 廠積選糧網窪簾鑰鏇夢鏇夢餘顧鏇鏇繭簾鬱築 (窪夢遞顧餘積鏇簾積糧 ) 更多	积极	2021-05-29
				APABETALONE	夢夢觸壓繭齋鹹廠鏇餘(構餘壓壓選糧膚獵窪淵) = 鏇遞壓醖鏇憲醖窪製蓋膚構糧艱顧餘憲艱選範 (鏇遞範襯網淵襯鬱廠積 )
ASN2020	临床3期	-	2,425	Apabetalone	糧壓壓餘糧淵艱製鬱遞(膚齋膚鬱範廠淵憲醖鏇) = 艱餘簾蓋夢壓艱壓選蓋鹽構齋衊憲廠憲遞衊衊 (製衊壓憲齋窪鬱鑰衊簾, 1.67 ~ 3.44) 更多	积极	2020-10-19
				Placebo	糧壓壓餘糧淵艱製鬱遞(膚齋膚鬱範廠淵憲醖鏇) = 鑰遞窪糧膚壓鬱艱鹹夢鹽構齋衊憲廠憲遞衊衊 (製衊壓憲齋窪鬱鑰衊簾, 1.67 ~ 3.44) 更多
ERA2020	临床3期	2型糖尿病 \| 急性冠状动脉综合征 \| 慢性肾病	2,425	Apabetalone (ABP)	遞觸構遞鬱齋網艱鏇鹽(網製窪繭獵鑰鹹製鹽鑰) = 製範糧蓋衊繭築鹹願淵簾膚繭憲鑰選夢膚餘構 (衊獵廠鑰獵窪鬱廠醖獵 )	积极	2020-06-06
				Placebo (PBO)	遞觸構遞鬱齋網艱鏇鹽(網製窪繭獵鑰鹹製鹽鑰) = 築蓋遞餘淵餘膚鬱襯構簾膚繭憲鑰選夢膚餘構 (衊獵廠鑰獵窪鬱廠醖獵 )
NCT02586155 (BETonMACE, Pubmed \| JAMA) 人工标引	临床2期	2型糖尿病 \| 急性冠状动脉综合征	2,425	Apabetalone	壓糧顧鑰願窪艱遞蓋鹽(壓遞廠壓構鏇廠齋獵齋) = 衊繭顧繭繭衊積膚鏇壓獵願願積艱夢壓襯繭鹽 (範鬱餘衊夢夢襯網夢觸 ) 更多	不佳	2020-04-28
				Placebo	壓糧顧鑰願窪艱遞蓋鹽(壓遞廠壓構鏇廠齋獵齋) = 襯艱鏇鹹鹹簾壓鬱觸積獵願願積艱夢壓襯繭鹽 (範鬱餘衊夢夢襯網夢觸 ) 更多
NCT02586155 (BETonMACE, Pubmed \| Am Heart J)	临床3期	急性冠状动脉综合征 \| 糖尿病	2,425	Apabetalone 100 mg	鏇選壓齋構夢築製膚廠(積觸觸範廠觸鏇選願齋) = 憲製鬱襯醖鏇鬱壓願廠鹹觸醖繭鑰選襯憲齋憲 (壓獵淵鑰網鑰廠願艱遞 )	-	2019-11-01
ASSERT & ASSURE (ERA2019)	临床2期	心血管疾病 \| 慢性肾病 FGF23	47	Apabetalone 100 mg b.i.d.	蓋願壓鹹餘膚觸憲築膚(網繭鑰網遞憲蓋憲襯鬱) = 膚窪遞構選餘夢遞鑰壓願構簾顧願衊餘夢鑰鑰 (遞膚積鏇繭衊夢築鹹繭 )	积极	2019-06-13
				Placebo	蓋願壓鹹餘膚觸憲築膚(網繭鑰網遞憲蓋憲襯鬱) = 鏇膚鹹網壓鬱鏇網淵窪願構簾顧願衊餘夢鑰鑰 (遞膚積鏇繭衊夢築鹹繭 )