Ro 13-3978

Ro 13-3978 is an orally active antischistosomal agent. Ro 13-3978 exhibits excellent in vivo antischistosomal activity against juvenile and adult Schistosoma mansoni infections. Ro 13-3978 shows no in vivo activity against E. caproni and F. hepatica. Ro 13-3978 blocks dihydrotestosterone-induced proliferation of androgen-dependent cells. Ro 13-3978 can be used in research related to schistosomiasis^[1][2]. In Vitro:Ro 13-3978 (100 μg/mL; 72 h) moderately reduces the motility of newly transformed S. mansoni schistosomula in vitro without causing tegument damage^[1].
Ro 13-3978 (0.12-90 μM; 70 h) shows no cytotoxicity against rat skeletal myoblast L6 cells at concentrations up to 90 μM after 70 h of incubation, with an IC₅₀ greater than 90 μM^[1].
Ro 13-3978 (25-100 μg/mL; 72 h) causes mild tegumentary changes in adult S. mansoni worms in vitro, including wrinkling in males and sloughing in a subset of females^[1]. In Vivo:Ro 13-3978 (12.5-200 mg/kg; p.o.; single dose) exhibits dose-dependent antischistosomal activity in NMRI mice, with an ED₅₀ of 14.6 mg/kg against adult S. mansoni and 138.9 mg/kg against juvenile S. mansoni following a single oral dose^[1].
Ro 13-3978 (100 mg/kg; p.o.; single dose) shows stage-specific antischistosomal activity in NMRI mice, with high efficacy (64.3-94.6% total WBR) against S. mansoni from day 22 post-infection onwards, no activity against 7-14 day-old worms, and moderate efficacy when administered pre-infection^[1].