About Long acting

Peptides are recognized for being highly selective, efficacious, relatively safe, and well tolerated but usually, it requires inject formulation rather than oral or other administrative routes. Also, its half-life is relatively short and injection frequency is usually limited as 1 or 2 times per day when it is used as a commercialized drug.

Therefore, the main themes in peptide drug development is sustained release of peptide drug or increase in vivo stability of peptide drug itself to make reduce injection frequency, because the injection frequency may influence to patient compliance and long term treatment efficacy. In addition, long-acting technologies may offer controlled drug-release profile during expecting period of time after each injection, less incidence of adverse events related with injection frequency, and overall cost savings during treatment periods.

Long acting technologies

Generally, current available long acting technologies are classified 2 groups as sustained release systems which can release drugs longer than one week and chemical modifications of peptide itself to increase stability as below.

Comparison of long acting technologies

All technologies have advantages and disadvantages in comparison with each other but the advantages of sustained release technologies would be no change of API which may be better to have 100% efficacy, easier to make longer acting form as monthly or beyond, and possible to bypass stability/safety study while chemical modification technologies has modified API which may not guarantee its own efficacy and requires full clinical trials as new drug in current regulations in global. Also, immediate systemic drug availability and rapid onset of action will be additional benefits of sustained release technologies.

Company Name Modification Technology Sustained Release Technology
API Modified Not modified
Maximum Duration
in common
1 - 4 weeks Up to 6 months
Requirement of
All preclinical & clinical studies are needed Partial preclinical & clinical studies are needed

Development status of long acting technology

Various drugs are investigated for sustained-release injectable for controlled drug delivery. These systems include small molecular drugs and protein/peptide drugs. Those examples are hormone therapy and protein therapeutics such as the analog of glucagon-like peptide-1(GLP-1)

With many groups are developing sustained release formulation as a new drug and generics, only drugs in limited therapeutic areas are available on the market. Antipsychotic drugs and hormones have been used for more than five decades in the field of schizophrenia and hormone replacement therapy. Since the first launching of microsphere formulation, Lupron Depot (Abbott, Abbott Park, IL) for the palliative treatment of advanced prostate cancer in 1989, several microsphere formulations and in situ-forming implants have been released on the US market. The therapeutic indications and drugs of commercialized products include: the palliative treatment of advanced prostate cancer (leuprolide acetate and triptorelin pamoate); the treatment of acromegaly (octreotide acetate and lanreotide acetate); the long-term treatment of growth failure (somatropin-rDNA origin); the treatment of schizophrenia (risperidone); and the treatment of alcohol dependence (naltrexone).