Development of a one-month extended-release subcutaneous donepezil injection... "World's first."

G2GBio Enters Domestic Clinical Trials... Enhanced Convenience with Alzheimer's Treatment Self-administration and Fewer Side Effects than Oral Form.

Clinical trials for a new injectable form of donepezil, which offers one month of effectiveness with a single injection, are scheduled to be conducted in South Korea. This new injectable form is noteworthy for its ability to be self-administered, unlike the traditional muscle injections that were previously developed.

The development of donepezil injectables is being pursued by some domestic companies, but the subcutaneous injection form is the world's first.

According to the Ministry of Food and Drug Safety on the 16th October 2023, G2GBio has received approval for the phase 1 clinical trial of 'GB-5001.'

GB-5001 is an innovative drug that transforms the existing once-daily oral medication for Alzheimer's disease, containing donepezil, into an injectable form. With its one-month effectiveness in a single administration, it enhances convenience for patients.

G2GBio will conduct clinical trials to evaluate the safety, pharmacokinetics, and tolerability of both the oral and injectable forms at Chungnam National University Hospital. Before conducting clinical trials in South Korea, G2GBio received approval for the phase 1 clinical trial of GB-5001 in Canada in 2021. The phase 1 trial currently underway in Canada is said to be in its final stages.

According to the company, the interim results of the phase 1 trial showed that the drug's concentration in the bloodstream was maintained at a certain level for over a month with no adverse reactions.

The phase 1 trial is currently in its final stages, with the completion of drug administration for all patients and ongoing result analysis. The company is placing great importance on the success of the clinical trial.

There are differences in the clinical trial design between the Canadian phase 1 trial and the upcoming South Korean trial. The Canadian trial involves a muscle injection form of donepezil, while the South Korean trial is developing the subcutaneous injection form.

Subcutaneous injection is considered the easiest method of administration among injection therapies, and it offers the advantage of patients being able to self-administer the injection without having to visit a hospital.

According to G2GBio, there is no other company worldwide currently developing a donepezil injectable in the subcutaneous form.

Donepezil is a key component that makes up 80% of the prescribed medications for dementia. Various forms have been developed, including immediate-release tablets, oral disintegrating tablets, oral solution, and transdermal patches. However, the most commonly prescribed form in the market remains the oral tablet, with other forms not being able to surpass it.

The major drawback of donepezil oral tablets is gastrointestinal side effects, leading to difficulties for some patients, including nausea and diarrhea. Additionally, dementia patients may find it challenging to take daily medication orally.

In contrast, an injectable form offers the advantage of one-month effectiveness with a single administration, providing convenience and potentially addressing the gastrointestinal side effects.

The development of a one-month extended-release injectable form of donepezil is considered to be technically challenging, and as of now, no company has successfully commercialized it.

If G2GBio succeeds in developing the self-administered donepezil injectable, it is expected to capture a significant portion of the market with its convenience as a selling point.

Furthermore, after completing the phase 1 trial in Canada, G2GBio is planning to conduct clinical trials in the United States.

The clinical trials in the United States, based on the results of the phase 1 trial, may involve discussions with the FDA for phase 3 trials or pivotal clinical trials. Phase 3 trials are resource-intensive and time-consuming, as they target dementia patients. Pivotal clinical trials, on the other hand, are conducted at the level of live experiments on healthy subjects, which relatively saves time and costs.

However, G2GBio recognizes that it may be challenging to conduct phase 3 trials or pivotal clinical trials independently, so they plan to seek technology export opportunities after completing the phase 1 trial.