更新于：2024-11-01

RXFP1 x albumin

更新于：2024-11-01

基本信息

关联

项与 RXFP1 x albumin 相关的药物

Volenrelaxin

靶点

RXFP1 x albumin

作用机制

RXFP1激动剂 [+2]

在研机构

Eli Lilly & Co.

原研机构

Eli Lilly & Co.

在研适应症

慢性肾病 [+2]

非在研适应症-

最高研发阶段临床2期

首次获批国家/地区-

首次获批日期1800-01-20

项与 RXFP1 x albumin 相关的临床试验

NCT06598631 / Not yet recruiting临床2期

A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Efficacy and Safety of Volenrelaxin in Adults With Chronic Kidney Disease

The main purpose of this study is to investigate the efficacy and safety of Volenrelaxin in adults with Chronic Kidney Disease. The study will last about 12 weeks.

开始日期2024-10-01

申办/合作机构

Eli Lilly & Co.

NCT05592275 / Recruiting临床2期

A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Investigate the Efficacy and Safety of LY3540378 in Adults With Worsening Chronic Heart Failure With Preserved Ejection Fraction (HFpEF)

The main purpose of this study is to assess the efficacy and safety of LY3540378 in adults with worsening heart failure with preserved ejection fraction

开始日期2023-02-03

申办/合作机构

Eli Lilly & Co.

NCT04768855 / Completed临床1期

A Single and Multiple Ascending Dose Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of LY3540378 in Healthy Participants

The main purpose of this study is to evaluate the safety and tolerability of the study drug known as LY3540378 in healthy participants following single and multiple doses (Parts A and B) and multiple doses in Japanese (Part C) and Chinese (Part D) healthy participants. Blood tests will be performed to check how much LY3540378 gets into the bloodstream and how long it takes the body to eliminate it. This is a 4-part study and may last up to 70, 113, 113 and 113 days for each participant in Parts A, B, C, and D respectively.

开始日期2021-03-17

申办/合作机构

Eli Lilly & Co.

100 项与 RXFP1 x albumin 相关的临床结果

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100 项与 RXFP1 x albumin 相关的转化医学

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0 项与 RXFP1 x albumin 相关的专利（医药）

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项与 RXFP1 x albumin 相关的文献（医药）

2023-08-01·British Journal of Pharmacology

Development of a long‐acting relaxin analogue, LY3540378, for treatment of chronic heart failure

Article

作者: Paavola, Chad D. ; Bivi, Nicoletta ; Cottle, Steven R. ; Wang, Xiaojun ; Porter, Gina ; Lin, Joanne ; Beebe, Emily C. ; Nwosu, Sylvia O. ; Malherbe, Laurent ; Copeland, Victoria ; Schroeder, Richard L. ; Ferrante, Andrea ; Lee, Stacey L. ; Meyer, Catalina M. ; Coskun, Tamer ; Matkovich, Scot J. ; Heuer, Josef G. ; Zhang, Hong Y. ; Thompson, Tyran D. ; Verdino, Petra ; Abernathy, Matthew M. ; Grealish, Patrick F. ; Hansen, Ryan J. ; Hu, Charlie C. ; Siegel, Robert ; Porras, Leah L. ; Cooper, Fariba N. ; Carr, Molly C. ; Dey, Asim ; Balciunas, Aldona M.

AbstractBackground and PurposeChronic heart failure, a progressive disease with limited treatment options currently available, especially in heart failure with preserved ejection fraction (HFpEF), represents an unmet medical need as well as an economic burden. The development of a novel therapeutic to slow or reverse disease progression would be highly impactful to patients and society. Relaxin‐2 (relaxin) is a human hormone regulating cardiovascular, renal, and pulmonary adaptations during pregnancy. A short‐acting recombinant relaxin, Serelaxin, demonstrated short‐term heart failure symptom relief and biomarker improvement in acute heart failure trials. Here, we present the development of a long‐acting relaxin analogue to be tested in the treatment of chronic heart failure.Experimental ApproachLY3540378 is a long‐acting protein therapeutic composed of a human relaxin analogue and a serum albumin‐binding VHH domain.Key ResultsLY3540378 is a potent agonist of the relaxin family peptide receptor 1 (RXFP1) and maintains selectivity against RXFP2/3/4 comparable to native relaxin. The half‐life of LY3540378 in preclinical species is extended through high affinity binding of the albumin‐binding VHH domain to serum albumin. When tested in a single dose administration, LY3540378 elicited relaxin‐mediated pharmacodynamic responses, such as reduced serum osmolality and increased renal blood flow in rats. In an isoproterenol‐induced cardiac hypertrophy mouse model, treatment with LY3540378 significantly reduced cardiac hypertrophy and improved isovolumetric relaxation time. In a monkey cardiovascular safety study, there were no adverse observations from administration of LY3540378.Conclusion and ImplicationsLY3540378 demonstrated to be a suitable clinical development candidate, and is progressing in clinical trials.