Pharmacokinetics and safety of imiquimod 5% cream in the treatment of molluscum contagiosum in children.
Imiquimod cream 5%, a toll-like receptor 7 agonist, induces alpha-interferon upon topical application, prompting off-label usage to treat children with molluscum contagiosum. We conducted an open-label study to measure serum drug concentration in children aged 2-12 years with extensive molluscum contagiosum (> or = 10% total body surface area). Dependent on extent of subject disease and weight, one to three packets (12.5 mg imiquimod per packet) were applied per dose, three times per week for 4 weeks. Serum imiquimod and metabolite concentrations were measured at pre dose and 2, 4, and 8 hours postdose 1 and dose 12. Thirty children were screened; 22 children (64% boys; 91% white; mean age 6.2 +/- 2.87 years; median involved body area treated 13.5%) were enrolled. Peak serum imiquimod concentrations following single and multiple dosing were low (< 10 ng/mL). Imiquimod concentrations increased 2- to 3.5-fold with multiple dosing. After single and multiple dosing, peak serum imiquimod (Pearson correlation r = 0.4989 and 0.7219, p < 0.05 both, respectively) and area under the serum concentration-time curve values (r = 0.4989 and 0.7219, p < 0.05 both, respectively) correlated with dose normalized for body weight (mg/kg). Systemic drug levels were low after single and multiple doses of imiquimod 5% cream in children.
Myhre
Paula E
PE
Department of Pharmacokinetics and Drug Metabolism, 3M Pharmaceuticals, 3M Center, Saint Paul, Minnesota, USA.
Levy
Moise L
ML
Eichenfield
Lawrence F
LF
Kolb
Vicki B
VB
Fielder
Sandra L
SL
Meng
Tze-Chiang
TC
D000287:Administration, Topical; D000367:Age Factors; D000634:Aminoquinolines / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D019540:Area Under Curve; D002648:Child; D002675:Child, Preschool; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D005260:Female; D005500:Follow-Up Studies; D006801:Humans; D000077271:Imiquimod; D007369:Interferon Inducers / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use; D008297:Male; D020714:Maximum Tolerated Dose; D008976:Molluscum Contagiosum / Q000175:diagnosis* / Q000188:drug therapy*; D011336:Probability; D018570:Risk Assessment; D012720:Severity of Illness Index; D012737:Sex Factors; D016037:Single-Blind Method; D016896:Treatment Outcome
D000634:Aminoquinolines; D007369:Interferon Inducers; D000077271:Imiquimod