IFNγ inhibitors(Interferon gamma inhibitors), IL-2 inhibitors(Interleukin-2 inhibitors), IRAK4 inhibitors(Interleukin-1 receptor-associated kinase 4 inhibitors)

+ [2]

Therapeutic Areas

Digestive System DisordersOther DiseasesNeoplasms+ [8]

Active Indication-

Inactive Indication

Barrett EsophagusCardiac transplant rejectionChemotherapy-induced damage+ [10]

Originator Organization

Genzyme Corp.

Active Organization-

Inactive Organization

Procter & Gamble Co.

Genzyme Corp.Synt:em SA

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Structure

Molecular FormulaC59H105N17O11

InChIKeySFGFYNXPJMOUHK-PKAFTLKUSA-N

CAS Registry287096-87-1

Gene Sequence

Sequence Code 14392555

100 Clinical Results associated with Delmitide

100 Translational Medicine associated with Delmitide

100 Patents (Medical) associated with Delmitide

Literatures (Medical) associated with Delmitide

01 Jul 2024·International Immunopharmacology

Oral administration of RDP58 ameliorated DSS-induced colitis in intestinal microbiota dependent manner

Article

Author: Chen, Gang ; Yan, Chao ; Cai, Huajing ; Zheng, Du ; Ke, Xinlong ; Chen, Yeru ; Sun, Jihong

BACKGROUNDAlthough the pathogenesis of inflammatory bowel disease (IBD), including ulcerative colitis (UC) and Crohn's disease (CD), has not been fully elucidated, accumulating researches suggest that intestinal microbiota imbalance contributes to the development of IBD in patients and animal models. RDP58, a peptide-based computer-assisted rational design, has been demonstrated to be effective in protecting against a wide range of autoimmune and inflammatory diseases. However, the underlying mechanism by which RDP58 protects against IBD mediated by intestinal microbiota has yet to be elucidated.METHODSThe colitis model was induced by continuously administering 2.5 % (wt/vol) dextran sodium sulfate (DSS) solution for 7 days. The manifestations of colon inflammation were assessed via daily weight changes, colon length, tumor necrosis factor-alpha (TNF-α) level, disease activity index (DAI) score, pathology score, and intestinal barrier permeability. Intestinal microbiota analysis was carried out by 16S-rRNA sequencing. Colonic short chain fatty acids (SCFAs) and regulatory T cells (Tregs) were also detected. To further confirm the protective effect of RDP58 on intestinal microbiota, broad-spectrum antibiotic cocktail (ABX) treatment and fecal microbial transplantation (FMT) experiment were performed.RESULTSOral administration of RDP58 ameliorated DSS-induced mice colitis by altering the diversity and composition of intestinal microbiota. Notably, RDP58 significantly upregulated SCFAs-producing microbiota, thereby promoting the generation of Tregs. ABX and FMT were performed to verify the above mechanism.CONCLUSIONSRDP58 ameliorated DSS-induced colitis through altering intestinal microbiota and enhancing SCFAs and Tregs production in intestinal microbiota dependent manner, potentially provide a novel therapy for IBD.

01 Jun 2013·Pharmacology & TherapeuticsQ1 · MEDICINE

Toll-like receptors as therapeutic targets for autoimmune connective tissue diseases

Q1 · MEDICINE

Review

Author: Yin, Hang ; Zhang, Fengchun ; Wang, Xiaohui ; Li, Jing

Autoimmune connective tissue diseases (ACTDs) are a family of consistent systemic autoimmune inflammatory disorders, including systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), systemic sclerosis (SSc) and Sjögren's syndrome (SS). IL-1R-like receptors (TLRs) are located on various cellular membranes and sense exogenous and endogenous danger-associated molecular patterns (DAMPs) and pathogen-associated molecular patterns (PAMPs), playing a critical role in innate immune responses. During the past decade, the investigation of TLRs in inflammatory autoimmune diseases has been fruitful. In this report, we review the significant biochemical, physiological and pathological studies of the key functions of TLRs in ACTDs. Several proteins in the TLR signaling pathways (e.g., IKK-2 and MyD88) have been identified as potential therapeutic targets for the treatment of ACTDs. Antibodies, oligodeoxyribonucleotides (ODNs) and small molecular inhibitors (SMIs) have been tested to modulate TLR signaling. Some drug-like SMIs of TLR signaling, such as RDP58, ST2825, ML120B and PHA-408, have demonstrated remarkable potential, with promising safety and efficacy profiles, which should warrant further clinical investigation. Nonetheless, one should bear in mind that all TLRs exert both protective and pathogenic functions; the function of TLR4 in inflammatory bowel disease represents such an example. Therefore, an important aspect of TLR modulator development involves the identification of a balance between the suppression of disease-inducing inflammation, while retaining the beneficiary host immune response.

01 Oct 2012·Transplant ImmunologyQ4 · MEDICINE

Prolonged survival time of allografts by the oral administration of RDP58 linked to the cholera toxin B subunit

Q4 · MEDICINE

Article

Author: Pingxian Wang ; Ya Xiao ; Xuesong Yu ; Bo Song ; Genfu Zhang ; Chibing Huang ; Mingqi Fang ; Jiayu Feng

Oral administration, which has been identified as a tool for boosting physiological immunoregulatory mechanisms in an antigen-specific manner, is a more convenient way than classical parenteral injection methods. RDP58 is derived from specific regions of class-I MHC molecules and is known to have immunomodulatory effects after intraperitoneal injection or intravenous administration. To determine whether the oral administration of RDP58 conjugated to the cholera toxin B subunit (CTB) can better induce peripheral tolerance than the use of traditional methods, we used various feeding regimens and methods of administration using equivalent doses of antigen during rat kidney transplantation. The results showed that RDP58-GC/CTB treatment increased the activity of Haem oxygenase-1 (HO-1) in vivo and significantly improved the survival and histopathology of allograft kidney tissue relative to the oral administration of RDP58 alone. These results suggest that the administration of RDP58 linked to CTB outweighs the benefits of oral administration of RDP58 alone for prolonging the survival time of kidney transplantation. This study supports the potential therapeutic use of oral administration of RDP58 linked to CTB as a platform molecule in the treatment of allograft rejection.

100 Deals associated with Delmitide

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Barrett Esophagus	Phase 2	US	-	-
Cardiac transplant rejection	Phase 2	US	-	-
Cardiac transplant rejection	Phase 2	FR	Synt:em SA	-
Colitis, Ulcerative	Phase 2	-	-	-
Colitis, Ulcerative	Phase 2	-	Genzyme Corp.	-
Crohn Disease	Phase 2	-	Genzyme Corp.	-
Crohn Disease	Phase 2	-	-	-
Crohn Disease	Phase 2	-	Procter & Gamble Co.	-
Diarrhea	Phase 2	US	-	-
Psoriasis	Phase 2	US	-	-

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