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DM-3411
- Development stage
- Unknown
- Lead developer
- Otsuka Pharmaceutical Development & Commercialization
- Modality
- Small Molecules
- Administration
- Not Administered Directly (metabolite Formed In Vivo From Oral Brexpiprazole)
01
Overview
DM-3411 is the major active metabolite of brexpiprazole, formed via cytochrome enzymes CYP2D6 and CYP3A4. It exhibits a pharmacodynamic profile similar to brexpiprazole but is less potent and has lower penetration to the central nervous system, resulting in negligible contribution to brexpiprazole’s clinical therapeutic effects[1][3]. Both brexpiprazole and DM-3411 bind extensively to serum proteins (99%), potentially affecting the free levels of concomitant serum protein-bound drugs[1]. DM-3411 represents 23.1%-47.7% of brexpiprazole exposure (AUC) in plasma, but its brain exposures are typically below clinically relevant detection limits[3].
- Brand names
- DM-3411DM3411DM 3411
- Other names
- DM-3411DM3411DM 3411
02
Targets
CYP3A4 (Cytochrome P450 3A4)SLC47A1 (Multidrug and toxin extrusion transporter 1)MATE2-K (Multidrug and toxin extrusion protein 2)OATP1B1 (Organic anion transporting polypeptide 1B1)OCT2 (Organic cation transporter 2)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR2A (Serotonin receptor 5-HT2A)
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