Name: Dersimelagon (MT-7117) in Erythropoietic protoporphyria or X-linked protoporphyria: Pharmacokinetics
Published: 2026-09-21T21:42:40-04:00

Product information and disease description Product description Product information Pharmacology

Pharmacokinetics

5 evidence topics · 4 sources

Absorption and dose proportionality in the first-in-human study

“In this double-blind, placebo-controlled phase 1 study, the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple ascending oral doses of dersimelagon in healthy participants were evaluated.” (opens the source at this quote in a new tab)
“In the clinical trial, dersimelagon was rapidly absorbed following single oral doses, with exposure appearing to increase in a slightly more than dose-proportional manner, similar to that observed in rats following oral administration of dersimelagon.” (opens the source at this quote in a new tab)
“Following multiple doses, dersimelagon was rapidly absorbed (median Tmax ranging from 4 to 5 h postdose on days 1 and 14). Mean t1/2 ranged from 10.56 to 18.97 h on day 14, and the steady state of plasma concentration was generally reached by 5 days of multiple dosing.” (opens the source at this quote in a new tab)

Nonlinearity and effect of sex on exposure

“These studies showed that dersimelagon has a slightly nonlinear PK profile, with more than dose-proportional increases following single- or multiple-dose administration.” (opens the source at this quote in a new tab)
“Plasma concentrations were higher in females than in males and overall exposure was not significantly impacted by food intake.” (opens the source at this quote in a new tab)

Metabolism and route of excretion

“In humans, elimination of radioactivity in urine was negligible (excretion of radioactivity into the urine: 0.31% of dose), and the primary route of excretion was feces, with more than 90% of the radioactivity recovered through 5 days postdose.” (opens the source at this quote in a new tab)
“Findings from humans and animals suggest dersimelagon is extensively metabolized to the glucuronide in the liver, which is eliminated in bile, and hydrolyzed to unchanged dersimelagon in the gut.” (opens the source at this quote in a new tab)

Effect of food and of an acidic beverage on exposure

“No effect was observed on overall exposure (area under the plasma concentration versus time curve [AUC]) following consumption of a high-fat meal, and Cmax was higher (22%, 90% confidence interval [CI] 1.05-1.42) in a fed state compared with fasted conditions.” (opens the source at this quote in a new tab)
“In general, the consumption of an acidic beverage increased time to Cmax regardless of fed or fasted status and decreased overall exposure AUC and Cmax of dersimelagon.” (opens the source at this quote in a new tab)

Effect of age and race on exposure

“There were no observable effects of age or race on the PK profile of dersimelagon or its metabolite dersimelagon glucuronide.” (opens the source at this quote in a new tab)