Oveporexton: Dosing Protocols
Dosing guidelines, reconstitution, and administration information
๐TL;DR
- โข2 dosing protocols documented
- โขReconstitution instructions included
- โขStorage: Storage conditions for the commercial formulation have not been publicly disclosed. Research-grade material should be stored as powder at -20 degrees C. Clinical trial supplies are handled per protocol-specific instructions.
Protocol Quick-Reference
Narcolepsy type 1 (excessive daytime sleepiness and cataplexy)
Dosing
Amount
2 mg twice daily
Frequency
Twice daily
Duration
12 weeks (Phase 3)
Administration
Route
OralTiming
Taken as oral tablets twice daily (morning and evening); onset of clinical improvement observed within the first weeks of treatment
Cycle
Duration
Ongoing (chronic treatment)
Repeatable
Yes
โ๏ธ Suggested Bloodwork (3 tests)
Liver function tests (ALT, AST)
When: Baseline
Why: Baseline hepatic function (prior OX2R agonist had hepatotoxicity)
Urinalysis
When: Baseline
Why: Baseline assessment given urinary side effects
Liver function tests
When: 8 weeks
Why: Monitor hepatic safety during treatment
๐ก Key Considerations
- โInvestigational: NDA accepted with Priority Review; not yet FDA-approved
- โMost common adverse events are insomnia (43-48%), urinary urgency (30-33%), and urinary frequency (29-32%)
- โNot a peptide; small molecule OX2R-selective agonist that addresses root cause of narcolepsy type 1
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| Purpose | Dose | Frequency | Duration | Notes |
|---|---|---|---|---|
| Narcolepsy Type 1 (Phase 2b Trial: NEJM 2025) | Four dose groups were evaluated: 0.5 mg twice daily, 2 mg twice daily, 2 mg morning/5 mg evening once daily, and 7 mg once daily. All doses showed significant efficacy compared to placebo. The 2 mg twice daily dose produced the largest improvements. | Once daily or twice daily oral administration | 8 weeks (Phase 2b trial duration) | All dose groups demonstrated statistically significant improvements in MWT, ESS, and cataplexy. The 2 mg BID dose produced MWT improvement of 23.5 minutes (vs -1.2 min placebo) and ESS improvement of -13.8 points (vs -2.5 placebo). |
| Narcolepsy Type 1 (Phase 3 FirstLight and RadiantLight) | Two dose groups evaluated: 1 mg twice daily and 2 mg twice daily (with placebo comparator). Both doses met all primary and secondary endpoints. | Twice daily oral administration | 12 weeks (Phase 3 trial duration) | The majority of participants on the 2 mg BID dose achieved wakefulness within normative range (MWT 20 minutes or more) and approximately 85% achieved ESS scores of 10 or less, comparable to healthy individuals. Cataplexy reduced by more than 80%. |
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๐Reconstitution Instructions
Oveporexton is an oral small molecule administered as tablets. No reconstitution, mixing, or dilution is required. Tablets are taken by mouth with water.
๐งStorage Requirements
Storage conditions for the commercial formulation have not been publicly disclosed. Research-grade material should be stored as powder at -20 degrees C. Clinical trial supplies are handled per protocol-specific instructions.
Community Dosing Protocols
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Before You Begin
Review safety warnings and contraindications before starting any protocol.
Investigational Status#
Oveporexton (TAK-861) is an investigational drug that is not yet approved by any regulatory agency. All dosing information below is derived from published clinical trial data and is provided for informational purposes only. Oveporexton should only be used under the supervision of qualified investigators in the context of clinical trials.
Phase 2b Trial Dosing (NEJM 2025)#
The Phase 2b trial (Dauvilliers et al., NEJM 2025) evaluated four dosing regimens of oveporexton in 112 participants with narcolepsy type 1 over 8 weeks:
| Dose Group | Regimen | N | MWT Change (min) | ESS Change | P-value vs Placebo |
|---|---|---|---|---|---|
| 0.5 mg BID | Twice daily | 23 | +12.5 | -8.9 | P less than or equal to 0.001 |
| 2 mg BID | Twice daily | 21 | +23.5 | -13.8 | P less than or equal to 0.001 |
| 2/5 mg QD | Once daily (AM/PM) | 23 | +25.4 | -12.8 | P less than or equal to 0.001 |
| 7 mg QD | Once daily | 23 | +15.0 | -11.3 | P less than or equal to 0.001 |
| Placebo | -- | 22 | -1.2 | -2.5 | -- |
All four doses produced statistically significant improvements. The 2 mg BID and 2/5 mg QD regimens produced the largest MWT improvements, suggesting that divided dosing or higher total daily doses may optimize efficacy.
Phase 3 Trial Dosing (FirstLight and RadiantLight)#
FirstLight (TAK-861-3001)#
- Design: Randomized, double-blind, placebo-controlled
- Participants: 168 with narcolepsy type 1
- Dose groups: 1 mg BID, 2 mg BID, and placebo
- Duration: 12 weeks
- Countries: 19 countries
RadiantLight (TAK-861-3002)#
- Design: Randomized, double-blind, placebo-controlled
- Participants: 105 with narcolepsy type 1
- Dose groups: 2 mg BID and placebo
- Duration: 12 weeks
Both studies met all primary (MWT) and secondary (ESS, cataplexy) endpoints at both dose levels with P-values of less than 0.001.
Administration#
Oveporexton is administered orally as tablets. Based on clinical trial data:
- Route: Oral
- Timing: Twice daily (morning and evening) for the Phase 3 dosing regimen
- Food effect: Not publicly disclosed; clinical trial protocols specify administration conditions
- No injection required: Unlike many peptide therapeutics, oveporexton is a small molecule with oral bioavailability
Clinical Response Timeline#
Based on Phase 2b and Phase 3 data:
- Onset of effect: Clinical improvements observed within the first weeks of treatment
- Most common adverse events onset: Insomnia and urinary symptoms typically appeared within 1-2 days of treatment initiation
- Peak efficacy: Measured at week 8 (Phase 2b) and week 12 (Phase 3)
- Insomnia resolution: Most cases of treatment-emergent insomnia resolved within the first week
Long-Term Extension#
A long-term extension study is ongoing for participants who completed the Phase 2b trial, providing data on sustained efficacy and long-term safety. Interim analysis results have been presented but full publication is pending.
Related Reading#
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Medical Disclaimer
This website is for educational and informational purposes only. The information provided is not intended to diagnose, treat, cure, or prevent any disease. Always consult with a qualified healthcare professional before using any peptide or supplement.