Serpin Peptide 16(Serpin Peptide 16) - 药物靶点：LRP1_在研适应症：急性肺损伤，带状疱疹，嗜酸粒细胞性食管炎_专利_临床

概要

基本信息

药物类型

合成多肽

别名

靶点

LRP1

作用机制

LRP1激动剂(LDL receptor related protein 1 agonists)

治疗领域

呼吸系统疾病其他疾病免疫系统疾病+ [8]

在研适应症

急性肺损伤带状疱疹嗜酸粒细胞性食管炎+ [6]

非在研适应症

新型冠状病毒感染炎症心肌梗塞

原研机构

Serpin Pharma, LLC

在研机构

Serpin Pharma, LLC

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C34H48N2O3

InChIKeyUTKQYACBDGXDMC-UHFFFAOYSA-N

CAS号60168-17-4

关联

3

项与 Serpin Peptide 16 相关的临床试验

NCT05135624 / Terminated临床1期

SP16 as a Therapeutic for SARS-CoV-2 Induced ARDS

This randomized, double-blind, placebo-controlled, Phase 1b study evaluates the safety and tolerability, and effects on cytokine and acute phase reactants of SP16, an anti-inflammatory drug, in patients with pneumonia due to SARS-CoV-2 infection. The study will enroll up to 20 patients and each eligible patient will be randomized to receive either one of two doses of SP16 (6 mg or 12 mg) or placebo by subcutaneous injection.

开始日期2021-12-01

申办/合作机构

Serpin Pharma, LLC

[+1]

NCT04225533 / Completed临床1/2期

SP16 Inflammatory Response Inhibition Trial

This study will evaluate the potential benefit of blocking inflammation during a heart attack using an investigational anti-inflammatory medicine called SP16. The study will enroll 10 patients and all 10 patients will receive a standard dose of SP16.

开始日期2020-02-24

申办/合作机构

Serpin Pharma, LLC

[+1]

NCT03651089 / Completed临床1期

Safety, Tolerability and Pharmacokinetics of a Single Subcutaneous Administration of SP16-a SERPIN-like, Small Peptide Agonist of the Low Density Lipoprotein-like Receptor 1-in Healthy Individuals

This study is a randomized, double-blind, placebo-controlled Phase 1 Clinical Trial of 24 healthy individuals to test the safety, tolerability and pharmacokinetics of a single subcutaneous administration of Serpin Peptide 16 (SP16), a Serine Protease Inhibitor (Serpin)-like, small peptide agonist of the Low Density Lipoprotein Receptor-like Protein 1 (LRPP1) hypothesized to have anti-inflammatory activity.

开始日期2018-07-16

申办/合作机构

Serpin Pharma, LLC

[+2]

100 项与 Serpin Peptide 16 相关的临床结果

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100 项与 Serpin Peptide 16 相关的转化医学

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100 项与 Serpin Peptide 16 相关的专利（医药）

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8

项与 Serpin Peptide 16 相关的文献（医药）

2024-02-01·Bioorganic Chemistry

Synthesis, molecular docking and biological evaluation of 1,2,4-oxadiazole based novel non-steroidal derivatives against prostate cancer

Article

作者: Wadhwa, Pankaj ; Kumar, Shubham

Prostate cancer is one of the most prevalent cancers in men leading to second most death causing cancer in men. Despite the availability of multiple treatment still the prevalence is high for prostate cancer. Steroidal antagonists associated with poor bioavailability, side effects while non-steroidal antagonists show serious side effects like gynecomastia. Therefore, there is a need of potential candidate for the treatment of prostate cancer with better bioavailability, good therapeutic effect and minimal side effects. In the same context, we have designed the series, SP1-SP25 based 3-phenyl-5-styryl-1,2,4-oxadiazole as the core structure. We successfully synthesized all 25 molecules in this series and characterized them using ¹H, ¹³C NMR, and mass spectroscopy. Subsequently, we conducted MTT assays using PC-3 cells and observed that all the compounds exhibited a dose-dependent decrease in cell viability. Notably, compounds SP04, SP16, and SP19 demonstrated a significant decrease in cell viability and exhibited potent activity compared to the other synthesized molecules and standard drug bicalutamide. Among them, SP04 emerged as the one of the most potent compounds with an IC₅₀ value of 238.13 nM and an 89.99 % inhibition of PC-3 cells, compared to synthesized molecules and standard drug bicalutamide. Furthermore, we conducted ROS assays and androgen receptor inhibition assays using the potent compound SP04 and bicalutamide. The results indicated that SP04 increased ROS production and decreased androgen receptor expression dose-dependent manner. Additionally, we conducted a docking study to analyse the interaction patterns within the active site of the androgen receptor. ADMET analysis revealed that all the compounds exhibited favorable physicochemical properties and manageable toxicity profiles.

2022-01-01·The FASEB Journal2区 · 生物学

α1‐Antitrypsin derived SP16 peptide demonstrates efficacy in rodent models of acute and neuropathic pain

2区 · 生物学

Article

作者: Gelber, Cohava ; Van Enoo, Alicia ; Austin, Dana ; Campana, Wendy M. ; Wang, Zixuan ; Martellucci, Stefano

SP16 is an innovative peptide derived from the carboxyl-terminus of α1-Antitrypsin (AAT), corresponding to residues 364-380, and contains recognition sequences for the low-density lipoprotein receptor-related protein-1 (LRP1). LRP1 is an endocytic and cell-signaling receptor that regulates inflammation. Deletion of Lrp1 in Schwann cells increases neuropathic pain; however, the role of LRP1 activation in nociceptive and neuropathic pain regulation remains unknown. Herein, we show that SP16 is bioactive in sensory neurons in vitro. Neurite length and regenerative gene expression were increased by SP16. In PC12 cells, SP16 activated Akt and ERK1/2 cell-signaling in an LRP1-dependent manner. When formalin was injected into mouse hind paws, to model inflammatory pain, SP16 dose-dependently attenuated nociceptive pain behaviors in the early and late phases. In a second model of acute pain using capsaicin, SP16 significantly reduced paw licking in both male and female mice (p < .01) similarly to enzymatically inactive tissue plasminogen activator, a known LRP1 interactor. SP16 also prevented development of tactile allodynia after partial nerve ligation and this response was sustained for nine days (p < .01). Immunoblot analysis of the injured nerve revealed decreased CD11b (p < .01) and Toll-like receptor-4 (p < .005). In injured dorsal root ganglia SP16 reduced CD11b⁺ cells (p < .05) and GFAP (p < .005), indicating that inflammatory cell recruitment and satellite cell activation were inhibited. In conclusion, administration of SP16 blocked pain-related responses in three distinct pain models, suggesting efficacy against acute nociceptive, inflammatory, and neuropathic pain. SP16 also attenuated innate immunity in the PNS. These studies identify SP16 as a potentially effective treatment for pain.

2017-10-01·JACC: Basic to Translational Science2区 · 医学

Low-Density Lipoprotein Receptor–Related Protein-1 Is a Therapeutic Target in Acute Myocardial Infarction

2区 · 医学

ArticleOA

作者: Carbone, Salvatore ; Mezzaroma, Eleonora ; Gelber, Cohava ; Mauro, Adolfo G ; Mogelsvang, Soren ; Toldo, Stefano ; Abbate, Antonio ; Marchetti, Carlo ; Van Tassell, Benjamin W ; Austin, Dana

Low-density lipoprotein receptor-related protein-1 (LRP1) is a ubiquitous membrane receptor functioning as a scavenger and regulatory receptor, inducing anti-inflammatory and prosurvival signals. Based on the known structure-activity of the LRP1 receptor binding site, the authors synthesized a small peptide (SP16). SP16 induced a >50% reduction in infarct size (p < 0.001) and preservation of left ventricular systolic function (p < 0.001), and treatment with an LRP1 blocking antibody eliminated the protective effects of SP16. In conclusion, LRP1 activation with SP16 given within 30 min of reperfusion during experimental acute myocardial infarction leads to a cardioprotective signal reducing infarct size and preservation of cardiac systolic function.

100 项与 Serpin Peptide 16 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
新型冠状病毒感染	临床2期	美国	Serpin Pharma, LLC	2021-12-01
炎症	临床2期	美国	Serpin Pharma, LLC	2020-02-24
心肌梗塞	临床2期	美国	Serpin Pharma, LLC	2020-02-24
急性肺损伤	临床2期	-	Serpin Pharma, LLC	-
天疱疮	临床前	美国	Serpin Pharma, LLC	2023-11-02
糖尿病	临床前	美国	Serpin Pharma, LLC	2013-09-26
急性肾损伤	临床前	美国	Serpin Pharma, LLC	-
斑秃	临床前	美国	Serpin Pharma, LLC	-
特应性皮炎	临床前	美国	Serpin Pharma, LLC	-
神经痛	临床前	美国	Serpin Pharma, LLC	-

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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


NCT04225533 (SPIRIT, CTgov)	临床1/2期	心肌梗塞 \| 炎症	10	SP16	窪鬱繭鏇鑰艱鹹蓋鏇艱(繭觸艱醖網選齋選鏇蓋) = 鬱糧製膚網鹹鏇遞淵齋顧壓鹹簾獵鹽蓋壓選鑰 (憲糧願襯鑰獵鬱壓淵顧, 鏇餘鹽糧蓋願選壓積簾 ~ 鬱壓鏇醖窪鹹範鏇膚糧) 更多	-	2023-01-30
NCT04225533 (Pubmed)	临床1/2期	ST段抬高心肌梗死	10	SP16	(衊齋齋蓋範鏇鑰網築襯) = All ten patients with STEMI received subcutaneous administration of SP16, 381 [272 to 478] minutes after PCI, without any treatment-related adverse events 蓋齋築簾構遞醖顧鹹範 (鏇鹹獵膚膚觸廠窪顧廠 )	积极	2022-07-12
				Placebo
NCT03651089 (Pubmed) 人工标引	临床1期	-	24	SP16	(膚蓋鑰製夢衊鑰願醖蓋) = 鹹鑰構壓齋蓋製繭鏇衊簾築願膚製淵襯夢壓夢 (遞願鏇廠蓋窪鹽顧齋艱 ) 更多	积极	2021-05-06
				Placebo	(膚蓋鑰製夢衊鑰願醖蓋) = 鏇範遞夢構鏇獵鬱醖蓋簾築願膚製淵襯夢壓夢 (遞願鏇廠蓋窪鹽顧齋艱 ) 更多