Chemistry:Tolevamer
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| Clinical data | |
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| Trade names | Tolevamer |
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| Bioavailability | None |
| Metabolism | None |
| Excretion | Faeces (100%) |
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| Chemical and physical data | |
| Formula | [C8H7SO3−] n |
Tolevamer is a medication developed to combat Clostridium difficile associated diarrhea.[1] It is a potassium sodium polystyrene sulfonate. It was never marketed.
Mechanism of action
Tolevamer was designed to bind the enterotoxins of Clostridium difficile. Since it has no antibiotic properties, it does not harm the gut flora. Early studies used the sodium salt, but it was soon replaced with the potassium sodium salt to prevent hypokalaemia, which is often associated with diarrhea.[2][3]
History
Termination of development
In early 2008, a noninferiority study versus vancomycin or metronidazole for Clostridium difficile associated diarrhea (CDAD) found that about half of the patients in the tolevamer group did not complete the treatment, versus 25% in the vancomycin and 29% in the metronidazole groups. CDAD recurrence in patients reaching clinical success was reduced significantly by tolevamer (6% recurrence rate), vancomycin (18%) and metronidazole (19%). However, the good result of tolevamer is partly due to the high drop-out rate in this group. Since tolevamer did not reach its primary endpoint in this study, its development was halted.[4]
References
- ↑ "Tolevamer, an anionic polymer, neutralizes toxins produced by the BI/027 strains of Clostridium difficile". Antimicrobial Agents and Chemotherapy 52 (6): 2190–5. June 2008. doi:10.1128/AAC.00041-08. PMID 18391047.
- ↑ "Neue Wirkstoffe - Tolevamer" (in German). Österreichische Apothekerzeitung (20/2007): 955. September 24, 2007.
- ↑ "Tolevamer Potassium Sodium". Drugs of the Future 32 (6): 501–505. 2007. doi:10.1358/dof.2007.032.06.1108513.
- ↑ "Tolevamer Less Effective Than Standard Therapies for C difficile–Associated Diarrhea". Medscape.com. 24 April 2008. http://www.medscape.com/viewarticle/573449.
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