Publications by authors named "Amanda M Mathis"
Article Synopsis
- Human African trypanosomiasis is a serious disease with limited treatment options, like pentamidine and its analogs, DB75 and DB820, which are effective against trypanosomes.
- Research indicates that these drugs accumulate in trypanosomes, particularly in the nucleus and acidocalcisomes, but their specific mechanisms of action remain unclear.
- This study found that even less potent compounds can accumulate to higher concentrations than more potent ones, suggesting that the degree of drug accumulation alone does not determine effectiveness in killing trypanosomes, and organelle-specific accumulation may not reliably predict drug activity.
The aromatic diamidine pentamidine has long been used to treat early-stage human African trypanosomiasis (HAT). Two analogs of pentamidine, DB75 and DB820, have been shown to be more potent and less toxic than pentamidine in murine models of trypanosomiasis. The diphenyl furan diamidine, DB75, is the active metabolite of the prodrug DB289, which is currently in phase III clinical trials as a new orally active candidate drug to treat first-stage HAT.
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