Background
The in vivo plasma concentration of penicillin needed to prevent Streptococcus pyogenes pharyngitis, recurrent acute rheumatic fever, and rheumatic heart disease is not known. We used a human challenge model to fill this knowledge gap.
Methods
In this randomised, double-blinded, placebo-controlled, human challenge trial, healthy adult volunteers were randomly assigned to target steady-state penicillin plasma concentrations (0, 3, 6, 9, 12, or 20 ng/mL). Participants and site staff were blinded to treatment allocation and outcomes. Individualised 5-day continuous intravenous infusions of penicillin were commenced 12 hours prior to pharyngeal application of an emm75 S. pyogenes inoculum (MIC=12 ng/mL). The primary endpoint was clinical pharyngitis.
Findings
Sixty participants were randomised, with 57 included in the analysis. The pharyngitis endpoint was met in 8/14 of the placebo group, followed by 4/9, 4/9, 0/8, 0/8, and 0/9 in each of the groups assigned 3, 6, 9, 12, and 20 ng/mL, respectively. No severe (grade 3) or serious adverse events occurred. Using Bayesian concentration-response modelling, the minimum steady-state plasma concentration of penicillin where 90% of participants would avoid clinical pharyngitis was 8.1 ng/mL (95% credible interval 6.1-10.9 ng/mL). The penicillin concentration where 90% of participants avoid an elevation in CRP of >20mg/L was 7.6 ng/mL (95% credible interval 5.8-10.3 ng/mL).
Interpretation
When steady state penicillin concentrations are greater than 9 ng/mL, few people will develop experimental emm75 S. pyogenes pharyngitis. These data will inform efforts to improve long-acting penicillin preparations and dosage regimens to prevent recurrent rheumatic fever and rheumatic heart disease.