What is the clinical evidence from this study?

Population: Human African Trypanosomiasis. Intervention: SCYX-7158 vs. Untreated or Berenil. Primary outcome: Cure rate (aparasitemia for 180 days) in stage 2 CNS HAT mouse model.

What question did this study set out to answer?

The research aims to discover and develop an effective, safe, and orally available treatment for stage 2 human African trypanosomiasis.

June 28, 2011PLoS neglected tropical diseasesOpen Access

SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis

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Key result

SCYX-7158 administered orally at 25 mg/kg once daily for 7 days achieved a 100% cure rate in a mouse model of stage 2 Human African Trypanosomiasis.

Key Points

The research aims to discover and develop an effective, safe, and orally available treatment for stage 2 human African trypanosomiasis.
Integrated biological screening and medicinal chemistry were employed to optimize a new small-molecule compound.
In vitro and in vivo efficacy was assessed across various strains of Trypanosoma brucei in murine models.
Pharmacokinetic studies evaluated the absorption, distribution, metabolism, elimination, and toxicology of SCYX-7158.
SCYX-7158 is effective in vitro against T. b. rhodesiense and T. b. gambiense strains.
In rodent studies, it showed significant brain penetration with C(max) >10 µg/mL and AUC(0-24 hr) >100 µg*h/mL after a 25 mg/kg dose.
The compound is expected to progress to phase 1 clinical trials due to its promising safety and efficacy profiles.

Structured PICO

Population

Preclinical evaluation in murine models of acute and stage 2 Human African Trypanosomiasis, alongside pharmacokinetic studies in rodents and non-human primates.

Intervention

SCYX-7158 (orally active benzoxaborole)

Outcome

In vitro activity, in vivo efficacy in murine HAT models, and pharmacokinetic properties (bioavailability, clearance, half-life, brain exposure)surrogate

Main Result

Absolute Event Rate: 100% vs 0%

SCYX-7158 is a promising, orally bioavailable, and CNS-permeable preclinical candidate for the treatment of stage 2 Human African Trypanosomiasis.

Limitations

Mechanism of action is currently unknown
Preclinical animal study requiring further safety and human clinical trials

Discussion

No takes yet. Share an insight, caveat, or question.

Implication

Advances oral candidate for stage 2 HAT; leaves open safety and efficacy in clinical trials.

Cite This Study

Jacobs et al. (2011) studied Human African Trypanosomiasis. SCYX-7158 vs. Untreated or Berenil was evaluated on Cure rate (aparasitemia for 180 days) in stage 2 CNS HAT mouse model. SCYX-7158 administered orally at 25 mg/kg once daily for 7 days achieved a 100% cure rate in a mouse model of stage 2 Human African Trypanosomiasis.

synapsesocial.com/papers/6a3ee45874814fb57808d07f https://doi.org/10.1371/journal.pntd.0001151

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SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis

Key Points

Structured PICO

Main Result

Limitations

Discussion

Implication

Cite This Study

SCYX-7158, an Orally-Active Benzoxaborole for the Treatment of Stage 2 Human African Trypanosomiasis

Key Points

Structured PICO

Main Result

Limitations

Discussion

Implication

Cite This Study

Also Consider

Also Consider