Sulforaphane in a tablet?

A 2024 randomized placebo-controlled human study by the product manufacturer investigated enteric-coated sulforaphane:

“The safety, tolerability, and pharmacokinetics of an enteric-coated tablet formulation of SFX-01 were evaluated in a randomized, double-blind, placebo-controlled, dose-escalation study [300 mg once daily (46.2 mg sulforaphane (SFN)), 300 mg twice daily or 600 mg once daily (92.4 mg SFN)] over 7 days in healthy male participants. Treatment-emergent adverse events occurred in 94% of participants who received SFX-01 and were most commonly gastrointestinal events.

The observed peak blood concentration (Cmax) for the sum of SFN and metabolites (total thiol) across all treatment cohorts ranged from 0.43 to 2.12 µmol/L in 3–6 hours. Urinary excretion of SFN and individual metabolites ranged from < 1 to 41%, and the proportion excreted did not appear to be influenced by the dose.

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Pharmacokinetic analyses demonstrated that the behavior of SFX-01 enteric-coated tablets was in line with expectations (i.e., rapid absorption following a lag phase attributed to the enteric coating on the tablet formulation), and individual Cmax and AUC values for combined SFN and metabolites were within the range required for pharmacological activity based on in vitro data. Future studies in relevant patient populations/disease indications will look to evaluate pharmacodynamics and target engagement.”

https://link.springer.com/article/10.1007/s12325-024-03018-1 “A Phase 1 Randomized, Placebo-Controlled Study Evaluating the Safety, Tolerability, and Pharmacokinetics of Enteric-Coated Stabilized Sulforaphane (SFX-01) in Male Participants”


This study’s referenced a 2017 study for:

“The proportion excreted via the urine in this study (15–60%) broadly agreed with a 2017 report in which 10 patients were administered 200 µmol of SFN in a 1:1 alpha-cyclodextrin solution, and a mean excretion of 62.3% of the administered dose was measured.”

I’ve curated that 2017 study several times, such as in the second discussion topic of Microwave broccoli seeds to create sulforaphane.

I’m sure these researchers feel that they did a good job for their sponsor. But this current study didn’t address items that would advance science past the 2017 study done at a lower 35 mg dose. For example:

  1. Why did subject bioavailability vary from < 1 to 41% as measured by urinary excretion of sulforaphane and metabolites? The 62.3% average of the 2017 study was meaningless considering those subjects varied from 86.9% to 19.5% (> 400% higher).
  2. Why did subject peak blood concentration vary from 2.12 to 0.43 µmol/L (almost 500% higher)? These researchers knew that would happen as the 2017 study subjects varied from 2.032 to 0.359 μmol (over 500% higher).
  3. Why did almost all (94%) subjects have adverse reactions to the 46.2 to 92.4 mg sulforaphane doses? 60% of the 2017 study subjects also had adverse reactions to a lower 35 mg dose. In what normal situation would people want to take tablets that made them nauseous?

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