Delving into the Latest Updates on Serpin Peptide 16 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

LRP1

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

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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8

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 Jan 2022·The FASEB JournalQ2 · BIOLOGY

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

Q2 · BIOLOGY

Article

Author: 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.

01 Oct 2017·JACC: Basic to Translational ScienceQ2 · MEDICINE

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

Q2 · MEDICINE

ArticleOA

Author: 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 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
COVID-19	Phase 2	US	Serpin Pharma, LLC	01 Dec 2021
Inflammation	Phase 2	US	Serpin Pharma, LLC	24 Feb 2020
Myocardial Infarction	Phase 2	US	Serpin Pharma, LLC	24 Feb 2020
Acute Lung Injury	Phase 2	-	Serpin Pharma, LLC	-
Pemphigus	Preclinical	US	Serpin Pharma, LLC	02 Nov 2023
Diabetes Mellitus	Preclinical	US	Serpin Pharma, LLC	26 Sep 2013
Acute Kidney Injury	Preclinical	US	Serpin Pharma, LLC	-
Alopecia Areata	Preclinical	US	Serpin Pharma, LLC	-
Dermatitis, Atopic	Preclinical	US	Serpin Pharma, LLC	-
Neuralgia	Preclinical	US	Serpin Pharma, LLC	-

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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	irrecwwfwj(ihbrwfeult) = cgaegnlani vpzjythetg (azeqchbkye, kpzdcxihdc - asxyrrykpi) View more	-	30 Jan 2023
NCT04225533 (Pubmed)	Phase 1/2	ST Elevation Myocardial Infarction	10	SP16	(ytcalnrska) = All ten patients with STEMI received subcutaneous administration of SP16, 381 [272 to 478] minutes after PCI, without any treatment-related adverse events yhgwnkrbzb (uxunbacmjs )	Positive	12 Jul 2022
				Placebo
NCT03651089 (Pubmed) Manual	Phase 1	-	24	SP16	(qcgcworkes) = pqdedjkqsq wyqjsjhtzu (bugrbtjzsj ) View more	Positive	06 May 2021
				Placebo	(qcgcworkes) = djtpymgajt wyqjsjhtzu (bugrbtjzsj ) View more