LB-102 · program
LB-102 (N-methylamisulpride) for Major depressive disorder
Indications for LB-102: Schizophrenia · Phase 3 Bipolar depression · Phase 2 Major depressive disorder · Unknown
Planned (not yet initiated) adjunctive MDD program. Per LB Pharmaceuticals' SEC 10-K (FY2025, filed Mar 2026): 'We are planning a Phase 2 trial that will evaluate LB-102 as an adjunctive therapy in MDD. We plan to initiate this trial in early 2027 and expect to report topline data in the first half of 2029.' Planned design: a two-arm, six-week, outpatient, multi-center, randomized, double-blind, placebo-controlled, fixed- and flexible-dose trial evaluating two doses of LB-102 (15 mg and 25 mg once daily) added to standard antidepressant therapy in approximately 380 patients with MDD who have an inadequate response after 1-2 prior antidepressant trials, at approximately 50 sites in the U.S. and Europe. Patients randomized 1:1 to LB-102 (pooled across dose) vs placebo on top of ongoing antidepressant therapy; primary endpoint MADRS-10 at Week 6; secondary endpoints CGI-I/CGI-S, anhedonia, function, cognition, and safety/tolerability. As of June 2026 no MDD trial is registered on ClinicalTrials.gov and enrollment has not begun, so phase is tracked as 'unknown' (planning stage) rather than phase_2.
Development timeline
- UpcomingLB Pharmaceuticals plans to initiate a Phase 2 adjunctive-MDD trial of LB-102 in early 2027, with topline data expected in 1H 2029.↗
Readouts
- 1H 2029AnticipatedTopline data
LB Pharmaceuticals plans to initiate a Phase 2 adjunctive-MDD trial of LB-102 in early 2027, with topline data expected in 1H 2029. ↗
Formulations
| Formulation | Route | Regimen | Pharmacokinetics |
|---|---|---|---|
| LB-102 long-acting injectablelong-acting injectable (LAI) Long-acting injectable formulation planned for global development (route/schedule not yet disclosed) | Subcutaneous depot (LAI) | — | — |
Mechanism of action
Selective antagonist of dopamine D2 and D3 receptors and serotonin 5-HT7 receptors. LB-102 retains high-affinity D2/D3 antagonism (Ki = 0.8 nM at each) and 5-HT7 antagonism (Ki = 31 nM); like its parent amisulpride it is a racemate with enantiomer-divergent polypharmacy (the S-enantiomer preferentially engages D2/D3, the R-enantiomer preferentially engages 5-HT7). N-methylation increases lipophilicity and passive membrane diffusion, giving better brain penetration than amisulpride and enabling once-daily oral dosing at 5-8 fold lower systemic exposure while still achieving the 60-80% striatal dopamine receptor occupancy associated with antipsychotic efficacy.
| Target | Action | Affinity |
|---|---|---|
| D2primaryDRD2 | Antagonist | Ki 0.8 nMⓘ |
| 5-HT7HTR7 | Antagonist | Ki 31 nMⓘ |
| D3DRD3 | Antagonist | Ki 0.8 nMⓘ |
← Full LB-102 compound page (identity, identifiers, all indications)
Sources
- Antipsychotic Efficacy and Safety of LB-102 in the Treatment of Adults With Acute Schizophrenia: A Randomized Clinical Trial (NOVA-1) — JAMA Psychiatry (PMC)
- LB Pharmaceuticals Announces Positive Topline Results from Phase 2 Trial of LB-102 in Schizophrenia — LB Pharmaceuticals (GlobeNewswire)
- LB Pharmaceuticals Inc. Form 10-K for fiscal year ended December 31, 2025 (Business: 'Phase 2 Trial of LB-102 in Adjunctive MDD', planned design and timeline) — U.S. Securities and Exchange Commission (EDGAR)