mizoribine
Mizoribine is an immunosuppressive drug. The compound was first observed in Tokyo, Japan, in 1971. It was first isolated from the fungus Penicillium brefeldianum. Mizoribine is an imidazole nucleoside that has been used in renal transplantation, and in steroid-resistant nephrotic syndrome, IgA nephropathy, lupus, as well as for adults with rheumatoid arthritis, lupus nephritis and other rheumatic diseases. MZB exerts its activity through selective inhibition of inosine monophosphate dehydrogenase and guanosine monophosphate synthetase, resulting in the complete inhibition of guanine nucleotide synthesis without incorporation into nucleotides. It arrests DNA synthesis in the S phase of cellular division. Thus, MZB has less toxicity than azathioprine, another immunosuppressant used for some of the same diseases. — Wikipedia
Clinical trial activity
6 trials · 7 clinical orgs · 0 marketing orgs
Earliest trial started Nov 1, 2013 (NCT02005757)
Timeline
Indications
Approved for
Mechanism of action
- AICAR transformylaseINHIBITOR
ATIC inhibitor
Inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor
- GMP synthase [glutamine-hydrolyzing]INHIBITOR
GMP synthase [glutamine-hydrolyzing] inhibitor
Chemistry & pharmacology
SMILES
NC(=O)c1ncn([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c1O- Mol. weight
- 259.22 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaMizoribine ↗
- ChEMBLCHEMBL245019 ↗
Also known as
- beta-bredinin
- bredinin
- bredinin
- bredinin
- bredinin
- bredinin
- mizoribin
- mizoribine
- mizoribine
- mizoribine
- mizoribine
- mizoribine
- mizoribine
- mizoribine
- mizoribine
- mizoribine 5'-monophosphate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06114953 | Phase 4 | Jan 1, 2023 | Lee's Pharmaceutical, Sichuan University |
| NCT05293704 | Phase 4 | May 1, 2022 | Lee's Pharmaceutical |
| NCT02373202 | Phase 3 | Feb 1, 2015 | Regeneron, Sanofi |
| NCT02256150 | Phase 3 | Nov 1, 2014 | Asahi Kasei Pharma |
| NCT02257697 | Phase 3 | Nov 1, 2014 | Asahi Kasei Pharma |
| NCT02005757 | Phase 2 | Nov 1, 2013 | Chong Kun Dang Pharmaceutical, University of Ulsan |
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Asahi Kasei Pharma | For profit | 2 | 2 | 1 | 2014 |
| Lee's Pharmaceutical | For profit | 2 | 2 | 1 | 2022 |
| Chong Kun Dang Pharmaceutical | For profit | 1 | 1 | 1 | 2013 |
| Regeneron | For profit | 1 | 0 | 1 | 2015 |
| Sanofi | For profit | 1 | 1 | 1 | 2015 |
| Sichuan University | Academic/Hospital | 1 | 0 | 1 | 2023 |
| University of Ulsan | Academic/Hospital | 1 | 0 | 1 | 2013 |