Olanzapine Pamoate

Drug information

Drug's link(s)

Not provided

Generic name

Olanzapine pamoate

Brand names

ZypAdhera®, ZYPREXA® RELPREVV™.

Compound type

Small molecule

Drug class/category

Not provided

Summary

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.

Approval status

Unknown

Regulatory authorities

Unknown

Therapeutic area(s)

Mental Health Disorders (incl. schizophrenia, bipolar disorders, Schiz. Aff. Dis.)

Use case(s)

Treatment

Administration route

Oral, Intramuscular

Associated long-acting platforms

Crystalline salt depot, Aqueous drug particle suspension

Use of drug

Ease of administration

Administered by a nurse
Administered by a specialty health worker

Frequency of administration

Not provided

User acceptance

Not provided

Dosage

Available dose and strength

Not provided

Maximum dose

Not provided

Recommended dosing regimen

Not provided

Additional comments

Not provided

Dosage link(s)

Not provided

Associated compounds, formulations and regimens

Not provided

Associated technologies

Not provided

Additional information

Not provided

Developer(s)

Originator

Germany

CheplaPharm

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

Scale-up prospects

Compound is commercially manufactured.

Tentative equipment list for manufacturing

Not provided

Manufacturing

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.

Specific analytical instrument required for characterization of formulation

Horiba LA 910 particle size analyser.

Excipients & delivery device(s)

Proprietary excipients used

Not provided

Novel excipients or existing excipients at a concentration above Inactive Ingredient Database (IID) for the specified route of administration

Not provided

Residual solvents used

Not provided

Delivery device(s)

No delivery device

Safety, Efficacy and Evidence Summary

Safety

Not provided

Efficacy

Not provided

Evidence Summary

Not provided

References and relevant studies

Not provided

Description

Olanzapine pamoate salts and formulations

Brief description

The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.

Representative patent

WO2000018408