Depot injections have been successfully introduced in certain markets and have illustrated the benefits of longer acting formulations. In 2003 the first atypical antipsychotic depot (2 week IM injection) was introduced to the schizophrenia market. The product showed very quickly the pharmacoeconomic benefits of a longer acting formulation by improving patient medication adherence and it quickly achieved blockbuster status. Since then, a few other atypical depot products have also been approved by the FDA. In spite the success of these products, they typically display certain limitations including:
- Technical limit of depot technologies to provide consistent blood levels for more than a few weeks.
- Safety issues since the drug cannot be withdraw if needed.
- Cumbersome dosing schedule during treatment initiation (or re-initiation when a dose is missed).
- Long washout period which complicates the process of switching treatments.
- Poor pharmacokinetic profile resulting in side effects at high plasma levels.
Our technologies overcome these barriers by extending the drug release to potentially as long as one year while maintaining zero order release pharmacokinetics. Furthermore, Delpor’s device allows for removal of the medication if needed (the device can be easily removed by any emergency room physician). Physicians and their patients have the flexibility to begin or interrupt the treatment at any time without having to worry about a complex dosing schedule during treatment initiation, or a long washout period after treatment interruption.
Comparison of DLP114 to Injectable Products
| Risperdal® Consta® | Invega® Sustenna® | Invega Trinza® | DLP-114 | |
|---|---|---|---|---|
| Duration | 2 Weeks | 4 Weeks | 3 Months | 6-12 Months |
| API | Risperidone | Paliperidone | Paliperidone | Risperidone |
| Reversibility | Not Reversible | Not Reversible | Not Reversible | Reversible |
| Initiation Dosing & Re-Initiation When Missing a Dose |
Oral Supplements For First 3 weeks | 2 Initiation Doses & Re-Initiation Needed If Dose is Missed* | Min 4 Months Sustenna® Initiation (6 doses) & Re-Initiation Needed If Dose is Missed** | No Initiation or Re-Initiation Required |
| Drug Accumulation/ Switching to Another Product | A few Weeks Washout | Several Weeks Washout | Several Months Washout*** | 1 Day Washout |
| PK | Peaks & Troughs | Peaks & Troughs | Peaks & Troughs | Smooth |
* Requires initiation doses on Days 1 & 8 before monthly injections begin, and Re-initiation if second initiation dose is missed or maintenance dose is missed by more than specified time interval (see Sustenna® label for details)
** Requires Re-initiation Regimen with 2 Sustenna® injections (Days 1 & 8) if Trinza® dose is missed by 1-6 months (i.e. 4-9 months since last injection); requires full Re-initiation Regimen with at least 6 Sustenna® injections if Trinza® dose is missed by over 6 months (i.e. >9 months since last injection). (see Trinza® label for details)
*** Requires 3 tier dose escalation schedule during ~6 months for switching to oral paliperidone. No data available for switching to another antipsychotic. Safety data involving concomitant use of Trinza® with other antipsychotics is limited. Paliperidone has been detected in plasma (7% of Cave) up to 18 months after a single-dose gluteal administration of 819 mg Trinza® (see Trinza® label for details)