Rapastinel: Dosing Protocols
Dosing guidelines, reconstitution, and administration information
๐TL;DR
- โข1 dosing protocols documented
- โขReconstitution instructions included
- โขStorage: Lyophilized powder stored at -20 degrees C. Reconstituted solutions used immediately in clinical trial settings.
Protocol Quick-Reference
Rapid-acting antidepressant (discontinued investigational)
Dosing
Amount
5-10 mg/kg IV
Frequency
Single dose (phase 2) or weekly (phase 3)
Duration
Single dose to repeated weekly dosing
Administration
Route
IVSchedule
Single dose or weekly IV infusion
Timing
Administered as IV infusion in clinical trial setting only. Effects onset within 2 hours and lasted up to 7 days from a single dose in phase 2.
Cycle
Duration
Single dose to weekly ongoing
Repeatable
Yes
โ๏ธ Suggested Bloodwork (3 tests)
CBC with differential
When: Baseline
Why: Baseline blood cell counts before IV administration
CMP (Comprehensive Metabolic Panel)
When: Baseline
Why: Liver and kidney function baseline
Mental health assessment (HDRS-17)
When: Baseline and post-dose
Why: Monitor antidepressant response
๐ก Key Considerations
- โClinical development was discontinued after phase 3 failure in March 2019
- โRequires intravenous infusion in a clinical setting; not suitable for self-administration
- โInverted U-shaped dose-response curve observed; 1 mg/kg and 30 mg/kg were not effective
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| Purpose | Dose | Frequency | Duration | Notes |
|---|---|---|---|---|
| Phase 2 Clinical Trial (Treatment-Resistant MDD) | Single IV dose of 1, 5, 10, or 30 mg/kg. The 5 and 10 mg/kg doses demonstrated significant antidepressant effects. | Single dose (phase 2); weekly IV infusion explored in phase 3 | Single dose in phase 2; repeated weekly dosing in phase 3 | Clinical development was discontinued after phase 3 failure in March 2019. These doses are from clinical trial protocols and are not approved for therapeutic use. |
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๐Reconstitution Instructions
In clinical trials, rapastinel was supplied as a lyophilized powder for IV reconstitution in sterile saline. Specific reconstitution volumes were not publicly disclosed. The compound is no longer in clinical development.
Recommended Injection Sites
- โIntravenous infusion (clinical trial setting only)
๐งStorage Requirements
Lyophilized powder stored at -20 degrees C. Reconstituted solutions used immediately in clinical trial settings.
Community Dosing Protocols
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Before You Begin
Review safety warnings and contraindications before starting any protocol.
Important Disclaimer#
Rapastinel is a discontinued investigational drug. Clinical development was halted after three phase 3 trials failed to meet primary endpoints in March 2019. It is not approved for any therapeutic use. The dosing information below is from published clinical trial data and is provided for informational purposes only.
Clinical Trial Dosing#
Phase 2 Proof-of-Concept Study (Preskorn et al., 2015)#
The key phase 2 study enrolled 116 subjects with MDD who had not responded to at least one antidepressant. Subjects received a single IV dose of rapastinel or placebo:
| Dose Group | Route | Result |
|---|---|---|
| 1 mg/kg | Single IV infusion | Not significantly different from placebo |
| 5 mg/kg | Single IV infusion | Significant reduction in HDRS-17 at days 1-7 |
| 10 mg/kg | Single IV infusion | Significant reduction in HDRS-17 at days 1-7 |
| 30 mg/kg | Single IV infusion | Not significantly different from placebo |
An inverted U-shaped dose-response was observed, with 5 and 10 mg/kg producing optimal effects. Onset of action was within 2 hours, with effects persisting approximately 7 days.
Phase 3 Trials (Failed)#
Phase 3 studies evaluated repeated weekly IV infusions of rapastinel as adjunctive therapy. All three studies failed to differentiate from placebo. Development was discontinued.
Route of Administration#
Rapastinel requires intravenous infusion due to poor oral bioavailability. This was a significant practical limitation for outpatient depression treatment.
Dosing Context#
Rapastinel belongs to the Neuropeptide category of research peptides. Dosing protocols for Rapastinel are derived from available clinical trial data. These protocols are provided for research reference only and do not constitute medical advice. Actual dosing decisions should be made by qualified healthcare providers based on individual patient factors.
Research Protocols#
The following dosing protocols have been documented in clinical research for Rapastinel:
Phase 2 Clinical Trial (Treatment-Resistant MDD)#
Dose: Single IV dose of 1, 5, 10, or 30 mg/kg. The 5 and 10 mg/kg doses demonstrated significant antidepressant effects.
Frequency: Single dose (phase 2); weekly IV infusion explored in phase 3
Duration: Single dose in phase 2; repeated weekly dosing in phase 3
Clinical development was discontinued after phase 3 failure in March 2019. These doses are from clinical trial protocols and are not approved for therapeutic use.
Reconstitution and Preparation#
In clinical trials, rapastinel was supplied as a lyophilized powder for IV reconstitution in sterile saline. Specific reconstitution volumes were not publicly disclosed. The compound is no longer in clinical development.
Injection Sites#
Recommended injection sites for Rapastinel include:
- Intravenous infusion (clinical trial setting only)
Site rotation is recommended to minimize local tissue reactions and ensure consistent absorption.
Storage Requirements#
Lyophilized powder stored at -20 degrees C. Reconstituted solutions used immediately in clinical trial settings.
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.