Name: Dersimelagon (MT-7117) in Erythropoietic protoporphyria or X-linked protoporphyria: Effects of Dersimelagon on other drugs
Published: 2026-09-21T21:42:40-04:00

Product information and disease description Product description Product information Drug/Drug, drug/disease interactions

Effects of Dersimelagon on other drugs

2 evidence topics · 2 sources

Clinical drug interaction study with probe substrates

“Relatively potent in vitro inhibition of CYP2C9, CYP3A, UGT1A1, BCRP, P‐gp, and OATPs by dersimelagon was observed.” (opens the source at this quote in a new tab)
“Midazolam (CYP3A substrate), digoxin (P‐gp), pravastatin (OATP), and simvastatin (CYP3A) did not show any clinically relevant DDI effects when co‐administered with dersimelagon.” (opens the source at this quote in a new tab)
“Dersimelagon 300 mg did not elicit major DDIs involving CYP/UGT enzymes and drug transporters; however, dersimelagon may have potential for clinically relevant DDIs with drugs that are substrates for BCRP, such as atorvastatin and rosuvastatin, and caution should be exercised when co‐administering 300‐mg dersimelagon with these statin drugs.” (opens the source at this quote in a new tab)

Predicted statin exposure at the clinical doses

“In vitro studies showed that dersimelagon is a weak, reversible, competitive and time‐dependent inhibitor of cytochrome P450 3A4 (CYP3A4), as well as a potential inhibitor of efflux and uptake transporter proteins, such as P‐glycoprotein (P‐gp), breast cancer resistance protein (BCRP), organic anion transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3), organic anion transporters 1 (OAT1) and 3 (OAT3), and multidrug and toxin extrusion 1” (opens the source at this quote in a new tab)
“The systemic exposure of atorvastatin based on the maximum plasma concentration and area under the plasma concentration–time curve was predicted to increase 1.21‐fold and 1.25‐fold, respectively, if coadministered with dersimelagon 100 mg, and 1.42‐fold and 1.45‐fold with dersimelagon 200 mg.” (opens the source at this quote in a new tab)
“Overall, PBPK modelling results indicate that the simulated changes in plasma exposure of atorvastatin and rosuvastatin following coadministration with dersimelagon 100 or 200 mg are not clinically significant, but caution and appropriate clinical monitoring should be recommended.” (opens the source at this quote in a new tab)