First‐In‐Human Study of Mirogabalin ( BM2216 ) Sustained‐Release Tablets: Safety, Tolerability, Pharmacokinetics, Food Effect and Dose Proportionality With Comparison to Mirogabalin Besylate in Healthy Participants
Authors' conclusion
BM2216 SR was safe and shows linear PK (5.5-3 mg single dose).
Study context
- Population
- Healthy adults aged 18–45 yearsParts 1–3: 18, 32, 16
- Comparison
- BM2216 sustained-release (SR) tablets vs mirogabalin besylate tablets; fed vs fasted; single doses 5.5–33 mg
- Outcome
- PK of BM2216 SR tablets
Methodological detailssingle-centre, randomised, open-label, crossover, three parts, 72 h washout between crossover periods, PK parameters by non-compartmental analysis
- Single-centre
- Randomised
- Open-label
- Crossover
- Three parts
- 72 h washout between crossover periods
- PK parameters by non-compartmental analysis
Main finding
As reported in the abstract
Tmax median, single postprandial doses
3.00-5.02 h
Further findings
Multiple-dose PK (16.5 mg QD, 4 days)
- Tmax,ss median
- 5.996 h
- t1/2,ss mean
- 3.8075 h
- RAC,Cmax (no accumulation)
- 0.9965
- RAC,AUC (no accumulation)
- 1.0150
Food effect (high-fat meal)
- T1/2 extended by
- 3.5 h
- Cmax increased by
- 16%
- Tmax delayed by
- 3 h
- AUC raised by
- 30%
Safety
Adverse events
- Dizziness
- 15.6%
- Increased bile acids
- 12.5%
- Vertigo
- 12.5%
- Serious adverse events (AEs)
- 0
- Dizziness in both the 16.5 and 33 mg dose groups; vertigo only in the 33 mg group
Original publication
First‐In‐Human Study of Mirogabalin ( BM2216 ) Sustained‐Release Tablets: Safety, Tolerability, Pharmacokinetics, Food Effect and Dose Proportionality With Comparison to Mirogabalin Besylate in Healthy Participants. Diabetes Obes Metab. Published 1 September 2026. doi:10.
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