Aricept grows to make ₩70B ... Ebixa nears ₩15B

OBT Aricept Evess makes steady sales in the ₩6-9 billion range

Exelon·Reminyl PR makes ₩6.2B last year... whether it will exceed ₩10B this year focus of attention

Domestic launch for Aduhelm in preparation despite continued dispute over its FDA approval

Eisai Korea’s Aricept (donepezil hydrochloride) continued on its solid lead in the original Alzheimer’s treatment market, occupying nearly 70% of the KRW 100 billion market.

 

According to drug distribution performance data, Aricept’s made KRW 71 billion, 65.5 billion, 69.2 billion, and 70.3 billion in 2018, 2019, 2020, and 2021, respectively, virtually leading the market ever since its release.

 

Aricept Evess, an orally disintegrating tablet formulation with the same ingredient that was approved in 2008 has been showing sales in the KRW 6 billion to 9 billion range.

 

The runner-up in the market, Lundbeck Korea’s Ebixa (memantine hydrochloride), which had maintained blockbuster-worthy sales in the KRW 10 billion range for 3 consecutive years from 2018 to 2020, had seen halved sales last year, making KRW6.2 billion.

 

However, as the company had recorded KRW 7.7 billion in sales in 1H this year, the company is expected to gross sales around KRW14 billion this year.

 

In 2021, Novartis’s Exelon (rivastigmine tartrate) and Janssen’s Reminyl (galantamine hydrobromide) have made around KRW 6.2 billion each.

 

Exelon’s sales in 2018,2019,2020 were KRW 2.9 billion, 4.5 billion, and 5.3 billion, respectively, and Reminyl PR made KRW 4.3 billion, 5.4 billion, and 5.8 billion, respectively, during the same period.

 

Eisai Korea’s Aricept, which was the second dementia treatment to be approved by the US FDA in 1995, is a donepezil formulation that had improved the convenience of intake by allowing once daily intake before sleep.

 

Unlike acetylcholinesterase inhibitors that have the inconvenience of requiring an initial dose-escalation phase, where patients need to start with a very low dose and then increase the dose until the patients achieve the therapeutic dose, the initial dose for Aricept is 5mg, and can be increased to 10mg for maximum effect.

 

Aricept has the advantage as patients can maintain the treatment dose that it has better tolerability and does not cause liver damage.

 

Due to the specificity of the formulation and its mechanism of action, patients who had suffered from ulcers in the past need to frequently monitor gastrointestinal bleeding.

 

Novartis’s Exelon, which had been the third to be approved in the field in 2000, contains rivastigmine, Like Aricept, it works by blocking the enzyme that breaks down acetylcholine --acetylcholinesterase – which transmits excitement to the neuron synapse, a neuronal junction.

 

By blocking these enzymes, Exelon allows patients to recover cognitive function.

 

Exelon is effective in moderate-to-severe Alzheimer’s patients, but if symptoms such as nausea, vomiting, abdominal pain, weight loss, etc.

 

are observed during the course of administering the dose should be reduced.

 

The fact that this drug also does not show hepatotoxicity is evaluated as its greatest advantage.

 

Janssen’s Reminyl PR is the fourth Alzheimer’s treatment that was approved by the FDA in 2001.

 

Reminyl contains galantamine, a herbal ingredient derived from the bulbs of the daffodil, Narcissus pseudonarcissus.

 

Although it has a similar mechanism of action as Aricept or Exelon, it does not have the ability to stop or repair nerve cell damage that is indicated as the cause of Alzheimer's.

 

Therefore, the drug does not dramatically reverse the course of the disease but enables patients to defer progression in cognitive impairment damage or provide slight recovery.

 

At a memory test conducted in a clinical trial, the control group’s memory had deteriorated by 5 to 11 points, compared with the high-dose Reminyl group that maintained its initial score.

 

Also, patients with vascular dementia and mixed type dementia that took Reminyl were able to relatively preserve their memory, orientation, and language ability.

 

Lundbeck’s Namenda (Ebixa) which was approved in 2003 as a severe Alzheimer’s treatment is an antagonist to the NDMA receptors in the nerve cells.

 

It inhibits the overstimulation of NDMA receptors by excessive glutamate.

 

Unlike acetylcholinesterase inhibitor class treatments that are indicated for moderate-to-severe Alzheimer’s, Namenda showed significant inhibition in the deterioration of cognitive or physical function in severe patients in a clinical trial where patients were administered 20mg of Namenda for 28 weeks.

 

Also, the drug has been positively received for raising the level of treatment for dementia of the Alzheimer's type in a clinical trial in combination with Aricept.

 

In June 2021, despite the overwhelming negative opinions from advisors, Aduhelm (Aducanumab), which was developed by Biogen/Eisa received FDA approval.

 

Its launch in Korea is also in preparation.

 

The FDA said Aduhelm provides significant benefits to patients by reducing the build-up of accumulated amyloid beta plaques.

 

Its once-every-four-week method of administration had opened a new horizon in drug delivery, its cost of KRW 60 million per year remain a large burden for the patients.

 

The first FDA-approved drug for Alzheimer’s is tacrine, which was launched in 1933, but the use of the drug is restricted due to hepatotoxicity.

 

Other acetylcholinesterase inhibitors used for the treatment of Alzheimer's disease include donepezil, rivastigmine, and galantamine.

 

Patients should start with a relatively low dose and gradually increase the dose of Alzheimer’s treatment according to the principle of geriatric pharmacology in principle, and must take the drug while closely monitoring its effect and side effects.