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Pafuramidine

Cat. No. M28972
Pafuramidine Structure
Synonym:

DB289

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Quality Control & Documentation
Biological Activity

Pafuramidine (DB289) is an orally active proagent of Furamidine. Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.

Chemical Information
Molecular Weight 364.4
Formula C20H20N4O3
CAS Number 186953-56-0
Form Solid
Solubility (25°C) DMSO 33.33 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gabriele Pohlig, et al. PLoS Negl Trop Dis. Efficacy and Safety of Pafuramidine versus Pentamidine Maleate for Treatment of First Stage Sleeping Sickness in a Randomized, Comparator-Controlled, International Phase 3 Clinical Trial

[2] Christian Burri, et al. PLoS Negl Trop Dis. Efficacy, Safety, and Dose of Pafuramidine, a New Oral Drug for Treatment of First Stage Sleeping Sickness, in a Phase 2a Clinical Study and Phase 2b Randomized Clinical Studies

[3] Myaing M Nyunt, et al. Am J Trop Med Hyg. Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites

[4] Donald Chen, et al. Expert Rev Anti Infect Ther. Pafuramidine for Pneumocystis jiroveci pneumonia in HIV-infected individuals

[5] Michael Zhuo Wang, et al. Drug Metab Dispos. Human enteric microsomal CYP4F enzymes O-demethylate the antiparasitic prodrug pafuramidine

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