Mizoribine

Description

Mizoribine is an orally active immunosuppressant isolated from Eupenicillium brefeldianum. It is reported to inhibit both cell-mediated and antibody mediated immune responses. Mizoribine is approved for use in the prevention of rejection of kidney transplants.

Description

Mizoribine is an imidazole nucleoside with immunosuppressive properties. It inhibits T cell proliferation in response to various mitogenic stimuli by 10-100% when used at concentrations ranging from 1 to 50 μg/mL. Mizoribine inhibits proliferation of stimulated T cells (IC₅₀ = 5 μg/ml), which can be reversed by guanosine. It also inhibits guanine nucleotide formation in T cells, reducing GTP pools by 40-60% when used at a concentration of 5 μg/ml. Mizoribine inhibits replication of hepatitis C virus (HCV) RNA in vitro (IC₅₀ = 100 μM). It suppresses glomerulosclerosis, urinary albumin excretion, interstitial fibrotic lesions, and macrophage infiltration into glomeruli and the interstitium in a rat model of type 2 diabetes when used at doses of 5 or 10 mg/kg. Mizoribine also reduces MCP-1, osteopontin (OPN), and TGF-β1 mRNA expression in the kidney in the same model. Formulations containing mizoribine have been used for the prevention of rejection after renal transplantation as well as in the treatment of lupus nephritis, rheumatoid arthritis, and primary nephritic syndrome.

Chemical properties

Crystalline Solid

Originator

Toyo Jozo (Japan)

The Uses of Mizoribine

Mizoribine has been used in topical treatment to evaluate its effect on ocular surface damage of dry eye in B6 mice subjected to desiccating stress (DS). It has also been used as an inosine monophosphate dehydrogenase (IMPDH) inhibitor to test its in vivo efficacy.

The Uses of Mizoribine

Nucleoside antibiotic with cytotoxic and immunosuppressive activity

What are the applications of Application

Mizoribine is an imidazole nucleoside immunosuppressant agent

What are the applications of Application

Mizoribine Hydrobromide is an immunosuppressant agent

Definition

ChEBI: Mizoribine is a member of imidazoles. It has a role as an anticoronaviral agent.

brand name

BREDININ

Biochem/physiol Actions

Mizoribine is an imidazole nucleoside possessing strong immunosuppressive properties. It selectively blocks T-cell proliferation response to mitogenic and allo-antigenic stimulation. Mizoribine blocks the movement of T cells from G to S phase. In addition, it significantly decreases the number of B cells at the S, G, and M phases. Mizoribine inhibits de novo synthesis of nucleotides by inhibition of inosine monophosphate dehydrogenase. The resulting nucleotide depletion inhibits DNA synthesis.(3)