Drug name
Olanzapine Pamoate
Developer(s)
Cheplapharma
Drug information
Not provided
Olanzapine pamoate
ZypAdhera®, ZYPREXA® RELPREVV™.
Not provided
Olanzapine is a second generation antipsychotic used for the treatment of schizophrenia and bipolar disorder. Long-acting injectable olanzapine formulations utilise a crystalline salt comprised of olanzapine and pamoic acid that forms micron-sized crystals in aqueous suspension. After administration via deep intramuscular injection, olanzapine pamoate forms a depot that gradually dissolves over a time period of approximately four weeks, with an average half-life of 30 days. The distribution and absorption of olanzapine pamoate occurs quickly and it remains in systemic circulation for 6-8 months following the last injection. 93% of olanzapine pamoate is bound to α1-acid-glycoprotein and albumin. Smoking may reduce the effectiveness of olanzapine, as it is metabolised by the CYP1A2 enzyme.
Unknown
Unknown
Therapeutic area(s)
- Mental health
- Treatment
Administration route
Oral, Intramuscular
Associated long-acting platforms
Crystalline salt depot, Aqueous drug particle suspension
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
Not provided
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Associated technologies
Not provided
Comment & Information
Developer(s)
Cheplapharm Arzneimittel GmbH is a pharmaceutical company headquartered in Greifswald, Germany. In 2023, they acquired the worldwide commercial rights for Zyprexa® from Eli Lilly and Company. This portfolio included olanzapine formulations marketed under the brand names ZypAdhera® and ZYPREXA® RELPREVV™. These products are indicated for the treatment of schizophrenia and bipolar disorders.
Drug structure
Scale-up and manufacturing prospects
Compound is commercially manufactured.
Not provided
The manufacturing process includes media conditioning, compounding, particle size reduction, vial filling, lyophilisation, and terminal sterilisation to produce a sterile injectable formulation. Olanzapine particles are reduced to <600 nm (preferably <100 nm) using nano-milling, homogenisation, or precipitation. Spherical grinding media (beads ~0.01mm to 3 mm) made of polymeric resin, glass or Zirconium Silicate are used. Olanzapine is mixed with liquid to form a premix (5-60% concentration) and surface stabiliser is added. The pH of the liquid dispersion is maintained between 3.0 and 8.0.
Horiba LA 910 particle size analyser.
Excipients
Not provided
Not provided
Not provided
Delivery device(s)
No delivery device
There are either no relevant patents or these were not yet submitted to LAPaL
Publications
Samalin L, Garay R, Ameg A, Llorca PM. Olanzapine pamoate for the treatment of schizophrenia--a safety evaluation. Expert Opin Drug Saf. 2016;15(3):403-11. DOI: 10.1517/14740338.2016.1141893. Epub 2016 Feb 19. PMID: 26761429.
Introduction: Non-adherence to long-term treatment is a major issue for patients with schizophrenia and is associated with an increased risk of relapse. Long-acting injectable (LAI) antipsychotics can offer a useful option to improve adherence. Due to the type of sustained-release mechanism, olanzapine pamoate (OLAI) can differ in safety as compared with oral olanzapine. Recent safety data concerning olanzapine pamoate required an update of previous systematic reviews.
Areas covered: Safety data were found in US and EU clinical trial registries, and a literature search was undertaken using the databases PubMed and EMBASE to find all relevant published studies. Where appropriate, the number needed to harm and 95% confidence interval for categorical safety outcomes were calculated.
Expert opinion: The safety profile of OLAI was similar to the well-known safety profile of oral olanzapine, except for the risk of occurrence of post-injection delirium/sedation syndrome (PDSS). Olanzapine pamoate can be a choice for schizophrenic patients with a history of response to and acceptable tolerance of oral olanzapine, who have easy access to mental healthcare settings with emergency services for the treatment of PDSS. Long-term, prospective studies assessing the efficacy and safety of OLAI and head-to-head comparisons with other LAI and oral antipsychotics are needed.
Additional documents
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Useful links
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In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing