A Single Center, Phase I, Double-Blind, Placebo-Controlled Evaluation of the Safety, Tolerability, and Pharmacokinetics of Single Ascending Oral Doses of INV-101 in Healthy Male and Female Subjects

Single center, randomized, double-blinded, placebo-controlled, single ascending-dose study for the evaluation of the safety, tolerability, and PK following single oral doses of INV-101.

开始日期2020-09-08

申办/合作机构

Inversago Pharma, Inc.初创企业

100 项与 Zevaquenabant 相关的临床结果

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100 项与 Zevaquenabant 相关的转化医学

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100 项与 Zevaquenabant 相关的专利（医药）

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项与 Zevaquenabant 相关的文献（医药）

2023-12-01·BIOMEDICINE & PHARMACOTHERAPY

In vitro and in vivo pharmacokinetic characterization, chiral conversion and PBPK scaling towards human PK simulation of S-MRI-1867, a drug candidate for Hermansky-Pudlak syndrome pulmonary fibrosis.

Article

作者: Gaucher, Geneviève ; Padilha, Elias C ; Xu, Xin ; Yang, Mengbi ; Iyer, Malliga R ; Malicdan, May Christine V ; Shah, Pranav ; Zawatsky, Charles N ; Cinar, Resat ; Wang, Amy Q ; Duan, Jianmin ; Kunos, George ; Park, Joshua K ; Ravenelle, François

Hermansky-Pudlak syndrome (HPS) is a rare autosomal recessive disorder that affects lysosome-related organelles, often leading to fatal pulmonary fibrosis (PF). The search for a treatment for HPS pulmonary fibrosis (HPSPF) is ongoing. S-MRI-1867, a dual cannabinoid receptor 1 (CB₁R)/inducible nitric oxide synthase (iNOS) inhibitor, has shown great promise for the treatment of several fibrotic diseases, including HPSPF. In this study, we investigated the in vitro ADME characteristics of S-MRI-1867, as well as its pharmacokinetic (PK) properties in mice, rats, dogs, and monkeys. S-MRI-1867 showed low aqueous solubility (< 1 µg/mL), high plasma protein binding (>99%), and moderate to high metabolic stability. In its preclinical PK studies, S-MRI-1867 exhibited moderate to low plasma clearance (CL_p) and high steady-state volume of distribution (Vd_ss) across all species. Despite the low solubility and P-gp efflux, S-MRI-1867 showed great permeability and metabolic stability leading to a moderate bioavailability (21-60%) across mouse, rat, dog, and monkey. Since the R form of MRI-1867 is CB₁R-inactive, we investigated the potential conversion of S-MRI-1867 to R-MRI-1867 in mice and found that the chiral conversion was negligible. Furthermore, we developed and validated a PBPK model that adequately fits the PK profiles of S-MRI-1867 in mice, rats, dogs, and monkeys using various dosing regimens. We employed this PBPK model to simulate the human PK profiles of S-MRI-1867, enabling us to inform human dose selection and support the advancement of this promising drug candidate in the treatment of HPSPF.

2020-10-01·Diabetes1区 · 医学

A New Treatment Strategy for Diabetic Dyslipidemia?

1区 · 医学

Article

作者: Bornfeldt, Karin E. ; Kothari, Vishal

A review.The dual CB1R/iNOS inhibitor (S)-MRI-1867 reduces hepatic secretion of VLDL through inhibiting CB1R-mediated MTP expression and reduces PCSK9 expression and subsequently increases LDL receptor expression via iNOS inhibition.Hepatic overproduction of VLDL can contribute to diabetic dyslipidemia, defects in clearance of TRLs/RLPs and perhaps reduced HDL cholesterol levels are likely to be important in CVD risk.Large clin. trials would be needed to establish whether (S)-MRI-1867, or similar hybrid compounds, have beneficial effects on dyslipidemia, NAFLD, and incident CVD in patients with T2D.

2020-10-01·Diabetes1区 · 医学

Simultaneous Inhibition of Peripheral CB1R and iNOS Mitigates Obesity-Related Dyslipidemia Through Distinct Mechanisms

1区 · 医学

Article

作者: Passilly-Degrace, Patricia ; Leemput, Julia ; Jourdan, Tony ; Roger, Célia ; Cinar, Resat ; Muller, Tania ; Kunos, George ; Degrace, Pascal ; Demizieux, Laurent ; Vergès, Bruno ; Iyer, Malliga R. ; Buch, Chloé

Diabetic dyslipidemia, characterized by increased plasma triglycerides and decreased HDL cholesterol levels, is a major factor contributing to nonalcoholic steatohepatitis and cardiovascular risk in type 2 diabetes. Activation of the cannabinoid-1 receptor (CB1R) and activation of inducible nitric oxide synthase (iNOS) are associated with nonalcoholic steatohepatitis progression. Here, we tested whether dual-targeting inhibition of hepatic CB1R and iNOS improves diabetic dyslipidemia in mice with diet-induced obesity (DIO mice). DIO mice were treated for 14 days with (S)-MRI-1867, a peripherally restricted hybrid inhibitor of CB1R and iNOS. (R)-MRI-1867, the CB1R-inactive stereoisomer that retains iNOS inhibitory activity, and JD-5037, a peripherally restricted CB1R antagonist, were used to assess the relative contribution of the two targets to the effects of (S)-MRI-1867. (S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9). The decrease in VLDL secretion could be attributed to CB1R blockade, while the reduction of PCSK9 levels and the related increase in LDLR resulted from iNOS inhibition via an mTOR complex 1–dependent mechanism. In conclusion, this approach based on the concomitant inhibition of CB1R and iNOS represents a promising therapeutic strategy for the treatment of dyslipidemia.

项与 Zevaquenabant 相关的新闻（医药）

2023-08-11

·佰傲谷BioValley

诺和诺德再次扩大肥胖管线，10.75亿美元收购Inversago

8月10日，诺和诺德宣布已同意在达到某些开发和商业里程碑的情况下，以最高10.75 亿美元的现金收购Inversago。根据发布的公告，此次收购需在 2023 年底之前获得适用的监管部门批准和其他惯例条件，以及达到某些开发和商业里程碑。有消息透露，根据最近的行业交易，诺和诺德可能支付了一半以上的预付款。Inversago Pharma 是一家总部位于蒙特利尔的私营开发商，开发基于 CB1 受体的疗法，用于治疗肥胖、糖尿病和代谢紊乱相关并发症。Inversago 的收购包括该公司的主要开发资产 INV-202，一种口服 CB1 反向激动剂。INV-202 优先阻断外周组织（如脂肪组织、胃肠道、肾脏、肝脏、胰腺、肌肉和肺部）中的受体蛋白CB1，CB1在新陈代谢和食欲调节中发挥着重要作用。诺和诺德打算研究INV-202治疗肥胖症和肥胖症相关并发症的潜力，INV-202 在 1b 期试验中展示了优异疗效，目前正在进行糖尿病肾病 (DKD) 的 2 期试验。此外，还正在开发针对代谢和纤维化疾病的其他管道资产。除了进展最快的INV-202 外，Inversago 还有另外两项处于临床前阶段的资产：INV-300（考虑用于多种适应症）和 INV-101（治疗特发性肺纤维化）。Inversago 表示将继续专注于顺利完成正在进行和计划进行的试验，同时与诺和诺德密切合作。此次收购的完成预计将于2023年底前完成。本周好文推荐如需转载请联系佰傲谷并在醒目位置注明出处﹀ ·········点亮在看，传递信息♥

并购临床2期

2021-09-03

·BioSpace

Scopus BioPharma’s Subsidiary — Duet Therapeutics — to Present at the 14th Annual RNA Consortium MeetingAlan Horsager, Ph.D., President and Chief Executive Officer of Duet, to Present on Clinical Development of CpG-STAT3 Inhibitors

NEW YORK, Sept. 03, 2021 (GLOBE NEWSWIRE) -- Scopus BioPharma Inc. (Nasdaq: “SCPS”), a clinical-stage biopharmaceutical company developing transformational therapeutics for serious diseases with significant unmet medical need, today announced that Alan Horsager, Ph.D., President and Chief Executive Officer of Duet Therapeutics, will present at the 14th Annual RNA Consortium Meeting, to be held virtually on Friday, September 10, 2021. Duet Therapeutics is a wholly-owned subsidiary of Scopus. Dr. Horsager is also President — Immuno-Oncology of Scopus. Dr. Horsager’s presentation will be part of the Clinical Translation of Oligonucleotide Therapeutics session. Dr. Horsager will present on Clinical Development of CpG-STAT3 Inhibitors. Duet Therapeutics was recently launched by Scopus BioPharma to integrate the immunotherapy assets of Scopus and Olimmune, creating the Duet Platform. The Duet Platform is comprised of three distinctive complementary CpG-STAT3 inhibitors: • RNA silencing CpG-STAT3siRNA (“DUET-01”) • Antisense CpG-STAT3ASO (“DUET-02”) • DNA-binding inhibitor CpG-STAT3decoy (“DUET-03”) The Duet Platform enables and facilitates development of STAT3 inhibitors which are highly selective for a multitude of different solid tumors and hematological malignancies. Current and potential indications for the Duet Platform include: B-cell non-Hodgkin lymphoma, T-cell non-Hodgkin lymphoma, genitourinary (e.g., prostate, kidney and bladder) and head & neck cancers. Duet’s CpG-STAT3 inhibitors are also being evaluated as combination therapies with checkpoint inhibitors and CAR-Ts. About Scopus BioPharma Scopus BioPharma Inc., both directly and through subsidiaries, is a clinical-stage biopharmaceutical company developing transformational therapeutics for serious diseases with significant unmet medical need. The company’s lead drug candidate is a novel, targeted immuno-oncology RNA therapy for the treatment of multiple cancers. This drug candidate is highly distinctive, encompassing both RNA therapy and immunotherapy by synthetically linking siRNA to an oligonucleotide TLR9 agonist, creating the potential for targeted gene silencing with simultaneous TLR stimulation and immune activation in the tumor microenvironment. Additional STAT3-targeting immunotherapy drug candidates include bi-functional antisense and protein degradation therapies. In addition, the company is developing additional drug candidates that target the endocannabinoid system, including MRI-1867 for the treatment systemic sclerosis. The company also seeks to identify additional compelling technologies for potential acquisition, in-licensing and/or other similar transactions. Receive updates by following Scopus BioPharma on Twitter here. Forward-Looking Statements This press release may include forward-looking statements that involve risks and uncertainties. Forward-looking statements are statements that are not historical facts. Such forward-looking statements are subject to risks (including those set forth in the company’s Form 10-K for the fiscal year ended December 31, 2020, as amended, filed with the U.S. Securities and Exchange Commission (“SEC”)) and uncertainties which could cause actual results to differ from the forward-looking statements. The company expressly disclaims any obligations or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein to reflect any change in the company’s expectations with respect thereto or any change in events, conditions or circumstances on which any statement is based. Investors should realize that if our underlying assumptions for the projections contained herein prove inaccurate or that known or unknown risks or uncertainties materialize, actual results could vary materially from our expectations and projections. Further, there can be no assurance that the company will identify and/or consummate any transaction relating to any additional technologies. Contacts Rodd Leeds/David Waldman Crescendo Communications, LLC Tel: (212) 671-1020 Email: SCPS@crescendo-ir.com Hugh Burns/Delia Cannan/Nicholas Leasure Reevemark Tel: (212) 433-4600 Email: scopus@reevemark.com

合作寡核苷酸免疫疗法并购siRNA

2021-09-02

·BioSpace

Scopus BioPharma Launches Duet Therapeutics

Duet Therapeutics Integrates Immunotherapy Assets of Scopus and Olimmune, Acquired by Scopus in June 2021 Integration Creates Comprehensive, Industry-Leading Portfolio of Bi-Functional Cancer-Targeting Oligonucleotides NEW YORK, Sept. 02, 2021 (GLOBE NEWSWIRE) -- Scopus BioPharma Inc. (Nasdaq: “SCPS”), a clinical-stage biopharmaceutical company developing transformational therapeutics for serious diseases with significant unmet medical need, today announced the launch of Duet Therapeutics. Duet Therapeutics integrates the management and clinical development of the immunotherapy assets of Scopus and Olimmune, acquired by Scopus in June 2021. Duet is a wholly-owned subsidiary of Scopus. Joshua R. Lamstein, Chairman of Scopus, stated, “We are extremely excited to announce the launch of Duet Therapeutics. The integration of the immuno-oncology assets of Scopus and Olimmune creates a comprehensive, industry-leading portfolio of bi-functional cancer-targeting oligonucleotides. Our highly complementary IP-protected technologies all target STAT3 inhibition. We believe our oligonucleotide technologies are unique, highly differentiated and superior to other STAT3 inhibitors currently under development.” Alan Horsager, Ph.D., President and Chief Executive Officer of Duet and President — Immuno-Oncology for Scopus, stated, “Overseeing the integration and clinical development of Duet’s immuno-oncology platform is an extraordinary opportunity. It is a privilege to play a key role in integrating and developing Duet’s drug candidates. Based on the large body of scientific data, we firmly believe our oligonucleotide platform has enormous potential to address one of society’s most significant unmet medical needs — unprecedented treatments, and potentially cures, for many different types of cancer. I can think of no greater professional mission than creating new standards of care, improving patient outcomes and saving lives.” The Duet Platform is comprised of three complementary, underpinning technologies: • RNA silencing CpG-STAT3siRNA (“DUET-01”) • Antisense CpG-STAT3ASO (“DUET-02”) • Protein degradation CpG-STAT3decoy (“DUET-03”) Dr. Horsager added, “The unique mechanism-of-action of these synthetic oligos comes from simultaneously targeting two intracellular immune pathways, STAT3 and TLR9. The targeted inhibition of STAT3, a master immune checkpoint inhibitor, reawakens immune cells and allows for the full potential of TLR9-driven immune responses.” DUET-01 is in a Phase 1 clinical trial, as a monotherapy, for B-cell non-Hodgkin lymphoma. In 2022, Duet is targeting to INDs for DUET-02 in two separate indications: genitourinary and head & neck cancers. Duet is also evaluating combination therapies with checkpoint inhibitors. About Scopus BioPharma Scopus BioPharma Inc., both directly and through subsidiaries, is a clinical-stage biopharmaceutical company developing transformational therapeutics for serious diseases with significant unmet medical need. The company’s lead drug candidate is a novel, targeted immuno-oncology RNA therapy for the treatment of multiple cancers. This drug candidate is highly distinctive, encompassing both RNA therapy and immunotherapy by synthetically linking siRNA to an oligonucleotide TLR9 agonist, creating the potential for targeted gene silencing with simultaneous TLR stimulation and immune activation in the tumor microenvironment. Additional STAT3-targeting immunotherapy drug candidates include bi-functional antisense and protein degradation therapies. In addition, the company is developing additional drug candidates that target the endocannabinoid system, including MRI-1867 for the treatment systemic sclerosis. The company also seeks to identify additional compelling technologies for potential acquisition, in-licensing and/or other similar transactions. Receive updates by following Scopus BioPharma on Twitter here. Forward-Looking Statements This press release may include forward-looking statements that involve risks and uncertainties. Forward-looking statements are statements that are not historical facts. Such forward-looking statements are subject to risks (including those set forth in the company’s Form 10-K for the fiscal year ended December 31, 2020, as amended, filed with the U.S. Securities and Exchange Commission (“SEC”)) and uncertainties which could cause actual results to differ from the forward-looking statements. The company expressly disclaims any obligations or undertaking to release publicly any updates or revisions to any forward-looking statements contained herein to reflect any change in the company’s expectations with respect thereto or any change in events, conditions or circumstances on which any statement is based. Investors should realize that if our underlying assumptions for the projections contained herein prove inaccurate or that known or unknown risks or uncertainties materialize, actual results could vary materially from our expectations and projections. Further, there can be no assurance that the company will identify and/or consummate any transaction relating to any additional technologies. Contacts Rodd Leeds/David Waldman Crescendo Communications, LLC Tel: (212) 671-1020 Email: SCPS@crescendo-ir.com Hugh Burns/Delia Cannan/Nicholas Leasure Reevemark Tel: (212) 433-4600 Email: scopus@reevemark.com

寡核苷酸免疫疗法并购siRNA

100 项与 Zevaquenabant 相关的药物交易

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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
非酒精性脂肪性肝炎	临床1期	加拿大	Inversago Pharma, Inc.初创企业	2020-09-29
普拉德-威利综合症	临床1期	加拿大	Inversago Pharma, Inc.初创企业	2020-09-29
特发性肺纤维化	临床前	加拿大	Inversago Pharma, Inc.初创企业	2023-08-11
进行性肺纤维化	临床前	加拿大	Inversago Pharma, Inc.初创企业	2020-09-14
Hermanski-Pudlak综合征	临床前	加拿大	Inversago Pharma, Inc.初创企业	2020-09-07
系统性硬化相关的间质性肺病	临床前	加拿大	Inversago Pharma, Inc.初创企业	2020-09-07