Delving into the Latest Updates on SR-0379 with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Target

Mechanism

Akt-1 inhibitors(Serine/threonine-protein kinase AKT inhibitors), Class I PI3K inhibitors(PI3-kinase class I inhibitors), mTOR inhibitors(Serine/threonine-protein kinase mTOR inhibitors)

Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication

Skin Ulcer

Inactive Indication

Pressure Ulcer

Originator Organization

FunPep Co., Ltd.

Active Organization

FunPep Co., Ltd.

Shionogi & Co., Ltd.

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC121H222N42O21S2

InChIKeyIVQFHGVEBLGBEL-RQEVABAPSA-N

CAS Registry1639363-19-1

Gene Sequence

Sequence Code 1495702

Author: Yokote, Koutaro ; Kiyohara, Eiji ; Yao, Xiang Jing ; Takemoto, Minoru ; Nakagami, Hironori ; Nakamura, Ayumi ; Ishikawa, Takahiro ; Rakugi, Hiromi ; Ebihara, Tamotsu ; Takami, Yoichi ; Nishikawa, Mitsunori ; Hayashi, Misa ; Yamamoto, Koichi ; Nakagawa, Yukinobu ; Hanaoka, Hideki ; Sugimoto, Ken ; Fujimoto, Taku ; Koshizaka, Masaya ; Takeya, Yasushi ; Terabe, Yuta ; Ando, Hiroshi

AimAn investigator‐initiated clinical study was carried out to evaluate the therapeutic potency of SR‐0379 for the treatment of leg ulcers in patients with Werner syndrome.MethodsA multicenter, open‐label study was carried out from September 2017 to February 2018. The inclusion criteria for leg ulcers were: (i) leg ulcers in patients with Werner syndrome, diabetes or critical limb ischemia/venous stasis; and (ii) a wound size of >1 cm and <6 cm in diameter. Four individuals with Werner syndrome and diabetic ulcers, respectively, were enrolled. SR‐0379 (0.1%) was sprayed on skin ulcers once per day for 4 weeks. Efficacy was evaluated by determining the rate of wound size reduction as a primary end‐point at 4 weeks after the first treatment compared with the pretreatment wound size. As secondary end‐points, the DESIGN‐R score index, the 50% wound size reduction ratio, time to wound closure and quantification of wound bacteria were also evaluated. The safety of SR‐0379 was evaluated during the study period.ResultsThe reduction rate of ulcer size treated with 0.1% SR‐0379 was 22.90% (mean) in the Werner syndrome ulcers group (n = 4) and 35.70% (mean) in the diabetic ulcers group (n = 4), respectively. The DESIGN‐R score decreased by 4.0 points in the Werner syndrome ulcers group and 4.3 points in the diabetic ulcers group. Two mild adverse events were reported in two patients, and causal relationships were denied in any events.ConclusionTreatment with SR‐0379 was safe, well‐tolerated, and effective for leg ulcers of both Werner syndrome and diabetes patients. Geriatr Gerontol Int 2019; 19: 1118–1123.

31 Oct 2017·BMB ReportsQ4 · BIOLOGY

The anti-microbial peptide SR-0379 stimulates human endothelial progenitor cell-mediated repair of peripheral artery diseases

Q4 · BIOLOGY

ArticleOA

Author: Park, Gyu Tae ; Kim, Seung-Chul ; Heo, Soon Chul ; Kwon, Yang Woo ; Yoon, Jung Won ; Lee, Tae Wook ; Jang, Il Ho ; Kim, Jae Ho

Ischemia is a serious disease, characterized by an inadequate blood supply to an organ or part of the body. In the present study, we evaluated the effects of the anti-microbial peptide SR-0379 on the stem cell-mediated therapy of ischemic diseases. The migratory and tube-forming abilities of human endothelial progenitor cells (EPCs) were enhanced by treatment with SR-0379 in vitro. Intramuscular administration of SR-0379 into a murine ischemic hindlimb significantly enhanced blood perfusion, decreased tissue necrosis, and increased the number of blood vessels in the ischemic muscle. Moreover, co-administration of SR-0379 with EPCs stimulated blood perfusion in an ischemic hindlimb more than intramuscular injection with either SR-0379 or EPCs alone. This enhanced blood perfusion was accompanied by a significant increase in the number of CD31- and α-SMApositive blood vessels in ischemic hindlimb. These results suggest that SR-0379 is a potential drug candidate for potentiating EPC-mediated therapy of ischemic diseases. [BMB Reports 2017; 50(10): 504-509].

PLoS ONEQ3 · CROSS-FIELD

Novel Anti-Microbial Peptide SR-0379 Accelerates Wound Healing via the PI3 Kinase/Akt/mTOR Pathway

Q3 · CROSS-FIELD

ArticleOA

Author: Saito, Yoshimi ; Tenma, Akiko ; Kaneda, Yasufumi ; Tomono, Kazunori ; Morishita, Ryuichi ; Nakagami, Hironori ; Kanamori, Toshihide ; Tomioka, Hideki ; Tamura, Nao ; Kaga, Toshihiro

We developed a novel cationic antimicrobial peptide, AG30/5C, which demonstrates angiogenic properties similar to those of LL-37 or PR39. However, improvement of its stability and cost efficacy are required for clinical application. Therefore, we examined the metabolites of AG30/5C, which provided the further optimized compound, SR-0379. SR-0379 enhanced the proliferation of human dermal fibroblast cells (NHDFs) via the PI3 kinase-Akt-mTOR pathway through integrin-mediated interactions. Furthermore SR-0379 promoted the tube formation of human umbilical vein endothelial cells (HUVECs) in co-culture with NHDFs. This compound also displays antimicrobial activities against a number of bacteria, including drug-resistant microbes and fungi. We evaluated the effect of SR-0379 in two different would-healing models in rats, the full-thickness defects under a diabetic condition and an acutely infected wound with full-thickness defects and inoculation with Staphylococcus aureus. Treatment with SR-0379 significantly accelerated wound healing when compared to fibroblast growth factor 2 (FGF2). The beneficial effects of SR-0379 on wound healing can be explained by enhanced angiogenesis, granulation tissue formation, proliferation of endothelial cells and fibroblasts and antimicrobial activity. These results indicate that SR-0379 may have the potential for drug development in wound repair, even under especially critical colonization conditions.

100 Deals associated with SR-0379

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Ulcer	Phase 3	JP	Shionogi & Co., Ltd.	30 Jan 2022
Skin Ulcer	Phase 3	JP	FunPep Co., Ltd.	30 Jan 2022
Pressure Ulcer	Discovery	JP	Shionogi & Co., Ltd.	27 Jun 2018