Delmitide

Delmitide (RDP58) is an orally active d-isomer decapeptide with potent anti-inflammatory activity. Delmitide inhibits production of TNF-α, IFN-γ, and interleukin (IL)-12, and up-regulates heme oxygenase 1 activity. Delmitide can be used for the research of ulcerative colitis[1][2].

Research Areas >> Cancer

Signaling Pathways >> Immunology/Inflammation >> IFNAR

Research Areas >> Infection

Research Areas >> Inflammation/Immunology

Delmitide (oral; 2.5, 5, 10 mg/kg; daily) significantly reduced CPT-11induced diarrhea, mucosal inflammation, and mortality in mice by suppressing the overproduction of proinflammatory cytokines TNF-a, IFN-y, and IL-12 in vivo[2]. Delmitide (oral; 2.5, 5, 10 mg/kg; daily) generates an enhanced tumor response and prolongation of time to relapse without concomitant Gl toxicity in mice[2]. Animal Model: BALB/c mice (female, 9-10-week)[2] Dosage: 2.5, 5, 10 mg/kg or 0.2 mL, 10 mg/kg Administration: Oral, daily Result: Reduced the incidence of diarrhea and attenuated CPT-11-associated GI toxicity and mortality in a dose-dependent manner. Had protective effect against chemotherapy-induced GI side-effects and reduced CPT-11-induced overexpression of TNF-α, IFN-γ, and IL-12 in vivo. Preserved the intestinal mucosa morphology by maintaining villus and crypt structure and inhibited TNF-α-mediated apoptosis in the crypt compartment, thereby protecting intestinal mucosa integrity in mice. Protected mice from CPT-11-induced GI toxicity and mortality and enhanced animal survival in tumor-bearing mice. Significantly reduced the incidence and overall tumor burden in a spontaneously metastatic model.

[1]. Arthur Kaser, et al. Novel therapeutic targets in the treatment of IBD. Kaser, Arthur; Tilg, Herbert (2008). Expert Opinion on Therapeutic Targets, 12(5), 553–563.

[2]. Jingsong Zhao, et al. Oral RDP58 allows CPT-11 dose intensification for enhanced tumor response by decreasing gastrointestinal toxicity. Clin Cancer Res. 2004 Apr 15;10(8):2851-9.