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

作用方式

激动剂

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-

权益机构-

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/序列

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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64

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.

2024-02-01·Protection of Metals and Physical Chemistry of Surfaces

Quantum Chemical Modeling of Optical and Physicochemical Properties of Amphiphilic Spiropyranes

作者: Zaichenko, N. L. ; Selivantev, Yu. M. ; Lyubimov, A. V. ; Morozov, A. N. ; Raitman, O. A.

The time-dependent d. functional theory method was used for the first time to calculate electronic transitions of amphiphilic spiro compoundsIt is shown that it gives a fundamentally correct electron d. distribution, corresponding to the results obtained using the CASSCF method, and allows one to predict the nature of the electronic transition of the merocyanine form.For neg. photochromes, the possibility of the existence of conical intersections of the potential energy surfaces of the ground and excited electronic states has been discovered, which may be the reason for the slow photochromism of these compoundsThe fundamental possibility of using TD-DFT to predict the optical characteristics of long-chain spiropyrans is demonstrated, provided that scaling regressions are used.For the first time, linear regressions have been developed for such compounds, taking into account a set of phys. parameters of the solvent in explicit form.This made it possible to obtain a unified empirical correction that takes into account the solvatochromic effect.The results obtained can be used as a basis for developing a main concept that takes into account the effect of the solvent on the spectral properties of spiro compounds and for constructing a unified regression model covering various types of solvato- and photochromism.

2023-12-01·Bulletin of the Russian Academy of Sciences: Physics

Photoinduced Control of Phase State of Monolayers Based on Phospholipids and Spirocompounds

作者: Zaichenko, N. L. ; Lyubimov, A. B. ; Degtyareva, V. A. ; Morozov, A. N. ; Raitman, O. A.

The results of a study of the physicochem. and photomech. properties of mixed Langmuir monolayers based on palmitoyloleoylphosphatidylcholine (POPC), dipalmitoylphosphatidylcholine (DPPC) and amphiphilic spirocompounds are presented.For the first time mixed monolayers based on POPC, DPPC, spiropyran 1',3'-dihydro-1'-hexadecyl-3'3'-dimethyl-6-nitrospiro[2H-benzopyran-2,2'-(2H)indole] and spironaphtoxazine 3,3-dimethyl-1-hexadecyl-1,3-dihydrospiro[indoline-2,3'-naphtho[2,1-b][1,4]oxazine]-9'-ol were formed in various combinations and ratios, and their comparative study was carried out.It has been established that binary mixture of phospholipids and spiro compounds form stable monolayers in which phase transitions can be controlled by UV-light.It has been shown that irradiation of monomol. phosphatidylcholine films containing small amounts of photosensitive compounds (up to 10% by weight) makes it possible to turn them into a liquid-condensed state at pressures above 10 mN/m.The results obtained open broad prospects for using photochromic spirocompounds to control the permeability of biol. membranes using light stimuli.

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
急性肺损伤	临床2期	-	Serpin Pharma, LLC	-
嗜酸粒细胞性食管炎	临床前	美国	Serpin Pharma, LLC	2023-11-02
炎症	临床前	美国	Serpin Pharma, LLC	2020-02-24
心肌梗塞	临床前	美国	Serpin Pharma, LLC	2020-02-24
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	-
新型冠状病毒感染	药物发现	美国	Serpin Pharma, LLC	2021-12-01

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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


NCT04225533 (SPIRIT, CTgov)	临床1/2期	心肌梗塞 \| 炎症	10	SP16	構築鑰醖願壓簾淵壓繭(選廠範壓範繭網廠淵鏇) = 憲網糧獵齋鹽糧觸廠鏇廠鑰築艱鏇齋遞憲鹽襯 (願鹹築廠憲觸鬱淵構簾, 觸製齋鏇蓋鹽窪繭淵憲 ~ 構夢鹹構壓艱衊繭繭網) 更多	-	2023-01-30
NCT04225533 (Pubmed \| J Cardiovasc Pharmacol)	临床1/2期	ST段抬高心肌梗死	10	SP16	簾鏇顧襯鹹齋顧網蓋鹽(網鏇願繭襯鹹願製醖簾) = All ten patients with STEMI received subcutaneous administration of SP16, 381 [272 to 478] minutes after PCI, without any treatment-related adverse events 築簾簾觸鹽鑰製壓觸壓 (齋糧繭製製構糧構網願 )	积极	2022-07-12
				Placebo
NCT03651089 (Pubmed) 人工标引	临床1期	-	24	SP16	(網觸廠鹹艱齋餘壓醖鏇) = 窪夢鬱觸淵簾選鏇網糧餘繭襯糧廠觸鏇顧鏇築 (鏇糧鏇衊獵積願簾醖壓 ) 更多	积极	2021-05-06
				Placebo	(網觸廠鹹艱齋餘壓醖鏇) = 鏇膚遞簾範醖範願廠衊餘繭襯糧廠觸鏇顧鏇築 (鏇糧鏇衊獵積願簾醖壓 ) 更多