A Phase 1 Randomized, Placebo-Controlled Study Evaluating the Safety, Tolerability, and Pharmacokinetics of Enteric-Coated Stabilized Sulforaphane (SFX-01) in Male Participants.
Level 2 - randomized trial
Phase 1 randomized, double-blind, placebo-controlled trial
PubMed 39520658 · doi:10.1007/s12325-024-03018-1
What was done
A randomized, double-blind, placebo-controlled, dose-escalation Phase 1 trial evaluated the safety, tolerability, and pharmacokinetics of an enteric-coated tablet formulation of SFX-01 (synthetic d,l-sulforaphane stabilized in an alpha-cyclodextrin complex). Healthy male participants were treated for 7 days with either placebo or SFX-01 at 300 mg once daily (46.2 mg sulforaphane), 300 mg twice daily, or 600 mg once daily (92.4 mg sulforaphane).
What was found
Treatment-emergent adverse events occurred in 94% of participants receiving SFX-01, consisting primarily of mild, treatment-related gastrointestinal symptoms. Peak blood concentrations (Cmax) of total thiol (sulforaphane plus metabolites) ranged between 0.43 and 2.12 µmol/L at 3 to 6 hours post-ingestion across cohorts. Cmax findings were inconclusive regarding dose-proportionality, and accumulation was minimal. Urinary excretion of sulforaphane and metabolites ranged from < 1% to 41% across doses.
Why it matters
SFX-01 provides a stable, orally bioavailable delivery format for sulforaphane, overcoming formulation instability barriers to enable clinical testing.
Limits
The abstract does not report the total participant count or specific adverse event rates in the placebo arm. The trial evaluated only healthy adult males over a short 7-day window, providing no data on long-term safety, female pharmacokinetics, or therapeutic efficacy.
Cited by
- supports A synthetic stabilized form of sulforaphane developed by a UK company produced adverse side effects in laboratory experiments.