POZ™ polymer LAI

Sponsor(s)

No sponsor indicated

Partnerships

Enable Injections, Inc. https://enableinjections.com/

Type of technology

Polymer-based particles, Monoclonal antibodies and antibody drug conjugates

Administration route

Subcutaneous

Development state and regulatory approval

apomorphine

Not provided

Under clinical investigation

Description

The POZ platform technology is based on poly(2-oxazoline), a water-soluble, low-viscosity polymer designed to enable the sustained delivery of drugs with narrow therapeutic indices. Although initially developed for small-molecule applications, the platform is adaptable to a broad range of substrates, including proteins, lipid nanoparticles, and antibody–drug conjugates (ADCs). The release kinetics of the API can be modulated through deliberate structural modifications of the POZ polymer, allowing fine control over drug release rates. This results in a near-liner PK profile of the API.

Technology highlight

1) Non-immunogenic 2) Simple one pot synthesis of the POZ polymer 3) Higher API loading capacity 4) Customizable PK profiling by modulating the polymer characteristics

Technology main components

POZ is connected to API via pendant groups and a degradable linker. Components of POZ drug conjugate includes: 1) Poly 2-oxazoline (POZ) polymer backbone 2) API (small molecules, proteins and peptides) 3) Linker (eg: 3‑propionate, carboxylate ester, carbonate ester, carbamate, amid, disulfide, peptides) 4) Pendant groups (eg: R, X) - i) hydrophobic pendant group ii) hydrophilic pendant group 5) Solvents / vehicles (Water, saline, oils) 6) Solid carriers (Gum acacia, gelatin, starch paste, talc, keratin, colloidal silica, urea 7) Functional excipients (formulation aids)- Stabilizers, Thickening agents, Lubricating agents, Flavoring agents

Information on the raw materials sourcing, availability and anticipated price

Not available

Delivery device(s)

Not provided

API desired features

Water-soluble molecules

Water-insoluble molecules

Small molecules

API list includes, but is not limited to, a therapeutic agent (such as but not limited to a drug), a diagnostic agent, and an organic small molecule. Further API can be hydrophobic in nature. Typically, a hydrophilic APIs with one or more oxygen, nitrogen, sulfur, and/or phosphorous atoms and/or one or more polar covalent bonds can also be encorporated into POZ conjugated complex. Compounds such as apomorphine, buprenorphine, rotigotine, dexanabinol, cannabidiol, tetrahydrocannabinol, cannabigerol, and other dopamine agonists are the first choice for POZ technology.

Additional solubility data

Not provided

Additional stability data

Not provided

API loading: Maximum drug quantity to be loaded

75-90 wt%

API co-administration

1 single API :

LogP

Min: 0.5 Max: 8

Scale-up prospects

The main synthesis and development of the proprietary POZ polymers occur at their Huntsville, Alabama laboratory, United States of America.

Tentative equipment list for manufacturing

1. Standard organic synthesis reactors (flasks/reactors) 2. Magnetic/overhead stirrers 3. Temperature-controlled reaction baths 4. Dropping funnels / dosing pumps 5. pH adjustment setup (pH meter)

Manufacturing

1. POZ polymer synthesis: Initiator (e.g., HOTf or alkyl initiator); organic solvent (e.g., chlorobenzene) ~80 °C 2. Introduction of functional (pendant) groups 3. Polymer termination 4. Drug–linker synthesis 5. Conjugation (key step): Click chemistry (Cu(I)-catalyzed azide–alkyne cycloaddition) 6. Purification

Specific analytical instrument required for characterization of formulation

1. GPC (Gel permeation chromatography) → MW, PDI 2. ¹H NMR (Nuclear Magnetic Chromatography) → drug loading, structure 3. HPLC/LC-MS (High Permeation Liquid Chromatography - Mass Spectrometry)

SER-214 Ia

Identifier

NCT02579473

Link

https://clinicaltrials.gov/study/NCT02579473

Phase

Phase I

Status

Unknown status

Sponsor

Serina Therapeutics

More details

SER-214 is a poly (2-ethyl-2oxazoline)(POZ) polymer conjugate of rotigotine, a potent dopamine agonist that has high affinity for the subclass of dopamine receptors in the brain that mediate dopamine signaling. SER-214 will be administered subcutaneously once a week via a standard 1 mL insulin syringe to determine the safety, tolerability and pharmacokinetic (PK) profile of released rotigotine and POZ-conjugate. Subjects in this study are eligible if they have early, stable or untreated Parkinson's disease and are still experiencing motor fluctuations.

Purpose

A Study of Weekly Subcutaneous Injections of SER-214 in Subjects With Parkinson's Disease (PD), to Determine the Safety, Tolerability and Pharmacokinetic (PK) Profile of SER-214

Interventions

Intervention 1

Countries

Sites / Institutions

Not provided

Trials dates

Anticipated Start Date
Not provided

Actual Start Date
2016-01-01

Anticipated Date of Last Follow-up
2023-04-10

Estimated Primary Completion Date
2023-12-31

Estimated Completion Date
2023-12-31

Actual Primary Completion Date
Not provided

Actual Completion Date
Not provided

Studied populations

Age Cohort

• Adults
• Older Adults

Genders

• All

Accepts pregnant individuals
Unspecified

Accepts lactating individuals
Unspecified

Accepts healthy individuals
No

Comments about the studied populations

Inclusion Criteria: 1. Female or male subjects 40-80 years of age inclusive 2. A diagnosis of idiopathic Parkinson's disease (PD) consistent with UK brain bank criteria 3. De novo PD patients and those on a stable regimen of anti-Parkinson's drugs for at least 4weeks prior to screening including anticholingerics, amantadine, MAO-B inhibitors, COMT inhibitors or levodopa, but not dopamine agonists 4. Free of clinically significant motor complications as determined by the investigator 5. Ability to complete up to four weeks of dosing once per week with two weeks of terminal "wash-out" PK 6. Ability to return to the clinic for blood sampling, clinical and laboratory assessment on scheduled days, based upon cohort 7. Mini Mental State Exam (MMSE) \> 26 8. Women of child-bearing potential (WOC

Health status

Not provided

Study type

Interventional (clinical trial)

Enrollment

20

Allocation

Not provided

Intervention model

Parallel Assignment

Intervention model description

Not provided

Masking

Open label

Masking description

Not provided

Frequency of administration

Studied LA-formulation(s)

Studied route(s) of administration

Use case

Treatment

Key resources

Proprietary excipients used

Not provided

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

Not provided

Residual solvents used

Not provided

Other features of the technology

• Biodegradable

Release properties

API release occurs via slow hydrolysis of the POZ–drug linker. The release rate is governed by: (i) polymer conformation, where a compact structure reduces water/enzyme access and prolongs t½, while a loose structure accelerates release; (ii) polymer molecular weight, with >20 kDa increasing steric shielding and t½, and <20 kDa enabling faster hydrolysis; and (iii) linker structure, where steric and electronic properties modulate hydrolytic stability and thus drug release kinetics.

Injectability

Yes. POZ platform can be adminstered through subcutaneous and intramuscular routes

Safety

No safety data has been reported yet.

Stability

The stability of the POZ polymer in the human plasma is approximately 55 hours (more exposed systems) upto 87 hours (more shielded systems).

Storage conditions and cold-chain related features

No stability and storage studies have been conducted yet.

Therapeutic area(s)

Use case(s)

Use of technology

Description

Polyoxazoline-lipid conjugates and lipid nanoparticles and pharmaceutical compositions including same

Brief description

POZ - lipid conjugates and lipid nanoparticles ( LNPs ) including POZ - lipid conjugates used to facilitate delivery of an encapsulated payload . LNPs including POZ - lipid conjugates and a nucleic acid payload such as , but not limited to, mRNA or modified mRNA are disclosed . Such LNPs have no immunogenicity or reduced immunogenicity as compared to a coorresponding LNP containing a PEG-lipid. pared to a corresponding LNP containing a PEG - lipid

Representative patent

US20220249695A1

Category

Composition

Patent holder

Serina Therapeutics Inc

Exclusivity

Not provided

Expiration date

May 23, 2042

Status

Active

Description

Subcutaneous delivery of poly(oxazoline) polymer conjugates

Brief description

The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a hydrolyzable moiety

Representative patent

US11224595B2

Category

Composition

Patent holder

Serina Therapeutics Inc

Exclusivity

Not provided

Expiration date

June 18, 2032

Status

Active

Publications

There are no publication

Additional documents

No documents were uploaded

Useful links

There are no additional links

	Collaborate for development Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology Not provided
	Share technical information for match-making assessment Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit Not provided
	Work with MPP to expand access in LMICs 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 Not provided