Delving into the Latest Updates on Serpin Peptide 16 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

LRP1

Action

agonists

Mechanism

LRP1 agonists(LDL receptor related protein 1 agonists)

Therapeutic Areas

Respiratory DiseasesOther DiseasesImmune System Diseases+ [8]

Active Indication

Acute Lung InjuryHerpes ZosterEosinophilic Esophagitis+ [6]

Inactive Indication

COVID-19InflammationMyocardial Infarction

Originator Organization

Serpin Pharma, LLC

Active Organization

Serpin Pharma, LLC

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC34H48N2O3

InChIKeyUTKQYACBDGXDMC-UHFFFAOYSA-N

CAS Registry60168-17-4

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.

Start Date01 Dec 2021

Sponsor / Collaborator

Serpin Pharma, LLC

[+1]

NCT04225533

/ CompletedPhase 1/2

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.

Start Date24 Feb 2020

Sponsor / Collaborator

Serpin Pharma, LLC

[+1]

NCT03651089

/ CompletedPhase 1

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.

Start Date16 Jul 2018

Sponsor / Collaborator

Serpin Pharma, LLC

[+2]

100 Clinical Results associated with Serpin Peptide 16

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100 Translational Medicine associated with Serpin Peptide 16

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100 Patents (Medical) associated with Serpin Peptide 16

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64

Literatures (Medical) associated with Serpin Peptide 16

01 Feb 2024·Bioorganic Chemistry

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

Article

Author: 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.

01 Feb 2024·Protection of Metals and Physical Chemistry of Surfaces

Quantum Chemical Modeling of Optical and Physicochemical Properties of Amphiphilic Spiropyranes

Author: 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.

01 Dec 2023·Bulletin of the Russian Academy of Sciences: Physics

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

Author: 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 Deals associated with Serpin Peptide 16

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Phase 2	United States	Serpin Pharma, LLC	24 Feb 2020
Myocardial Infarction	Phase 2	United States	Serpin Pharma, LLC	24 Feb 2020
Acute Lung Injury	Phase 2	-	Serpin Pharma, LLC	-
Pemphigus	Preclinical	United States	Serpin Pharma, LLC	02 Nov 2023
Diabetes Mellitus	Preclinical	United States	Serpin Pharma, LLC	26 Sep 2013
Acute Kidney Injury	Preclinical	United States	Serpin Pharma, LLC	-
Alopecia Areata	Preclinical	United States	Serpin Pharma, LLC	-
Dermatitis, Atopic	Preclinical	United States	Serpin Pharma, LLC	-
Neuralgia	Preclinical	United States	Serpin Pharma, LLC	-
COVID-19	Discovery	United States	Serpin Pharma, LLC	01 Dec 2021

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04225533 (SPIRIT, CTgov)	Phase 1/2	Myocardial Infarction \| Inflammation	10	SP16	rpzkzkhywc(bjssbgrzlo) = zwkoocupkj yjfmfpvfym (fflzfihuqy, acfviohnqi - ivqxxbpwet) View more	-	30 Jan 2023
NCT04225533 (Pubmed \| J Cardiovasc Pharmacol)	Phase 1/2	ST Elevation Myocardial Infarction	10	SP16	uqpjbcgzqb(thsjwqcwqt) = All ten patients with STEMI received subcutaneous administration of SP16, 381 [272 to 478] minutes after PCI, without any treatment-related adverse events wftkauwplg (znmcvldnww )	Positive	12 Jul 2022
				Placebo
NCT03651089 (Pubmed) Manual	Phase 1	-	24	SP16	(fuitjokyty) = uvxizgofzr pglwohfkdw (gjgmorfoua ) View more	Positive	06 May 2021
				Placebo	(fuitjokyty) = xzrtzguiui pglwohfkdw (gjgmorfoua ) View more

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Biosimilar

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