GB-5001

Global pharmaceutical industries have been striving to conquer dementia, but the efficacy has been limited and there have been numerous reports of side effects, including fatalities due to cerebral edema. As a result, dementia remains one of the diseases that have yet to be fully conquered.

Aricept, an oral medication with donepezil hydrochloride as its active ingredient, is the most representative product of dementia treatments with established efficacy. Generally, the cognitive symptoms and signs of Alzheimer's disease are thought to be due to a deficiency in cholinergic neurotransmission, and donepezil reversibly inhibits the breakdown of acetylcholine, thereby improving cholinergic function and exhibiting therapeutic effects.

However, donepezil hydrochloride, the active ingredient in Aricept, has a disadvantage due to the characteristic of being a water-soluble drug and the low medication convenience of taking it every day before bedtime for patients suffering from dysphagia.

G2GBIO aims to develop GB-5001 as an Alzheimer's treatment with superiority in terms of patient medication convenience and efficacy lasting for more than 4 weeks after a single dose. It is currently undergoing Phase 1 clinical trials in Canada and aims to begin clinical trials in South Korea this year. In particular, the InnoLAMP technology allows for the manufacture of uniform microspheres, making scale-up production of 1 kg per batch achievable and working towards a goal of 10 kg production.

G2GBIO have developed GB-5001 that allows intramuscular and subcutaneous administration through a drastic improvement in drug concentration compared to competitors, reducing the injection amount per dose. We have effectively controlled the excessive initial release, which was a disadvantage in the early stages of development, and G2GBIO's differentiating factor is the ability to maintain sufficient therapeutic effects with a small amount of controlled release.

GB-5001A
GB-5001D

G2GBio has completed the formulation development of GB-5001A and GB-5001D and is preparing for a phase 1 clinical trial in Korea.

GB-5112

Rivastigmine is a drug used to treat mild to moderate Parkinson's and Alzheimer's disease. It works by inhibiting acetylcholinesterase and butyrylcholinesterase, enzymes that break down acetylcholine, an important neurotransmitter in the brain associated with memory. By preventing the breakdown of acetylcholine, Rivastigmine maintains normal acetylcholine neurotransmission and improves cognitive function. Currently, Rivastigmine therapies are available as oral tablets that need to be taken twice a day and patches that are applied once a day. However, the tablets can cause gastrointestinal side effects, and the patches can cause skin irritation. Therefore, there is a need to develop formulations that can overcome these limitations. To address this issue, G2GBIO has developed a formulation using InnoLAMP technology, which can sustain efficacy for four weeks with a single dose. G2GBIO is currently preparing for phase 1 clinical trials.

GB-6002

Opioid drugs, such as opiate analogues, are the most commonly used drugs for pain relief. However, due to the serious side effects of drug dependence and addiction caused by opioid drugs, it has been reported that about 700,000 people have died in the United States due to drug abuse over the past 20 years. Therefore, it is urgent to develop non-opioid analgesics that can replace opioid drugs with severe addiction and side effects.

Ropivacaine, one of the non-opioid analgesics, is a local anesthetic of the Amide group and has a very similar structure to Bupivacaine, but it is composed of 100% S-isomer, which has less cardiovascular and CNS toxicity, and has a wide safety margin of the drug. In addition, it can selectively block sensory nerves rather than motor nerves, making it the most suitable drug for post-operative pain management.

G2GBIO's GB-6002 is a continuous release injection using Ropivacaine, which is administered directly to the surgical site, which reduces systemic exposure to the drug and reduces side effects compared to conventional administration methods. It aims to relieve pain for more than three days with one injection, and drug development has been completed with a phase 1 clinical plan in Korea.

GB-7001

Type-2 Diabetes is a metabolic disorder caused by insulin insufficiency causing metabolic abnormality such as hyperglycemia and is a disease with a high risk of vascular complications due to hyperglycemia. When diabetes becomes chronic, it can lead to chronic complications such as macrovascular complications (angina, stroke), microvascular complications (retinopathy, nephropathy, neuropathy), and diabetic foot disease, which are more dangerous than hyperglycemia itself. Especially in the case of diabetes patients, the incidence of these diseases is much higher as patients often have additional risk factors such as abdominal obesity, platelet dysfunction, and insulin resistance, making them the main cause of death among diabetes patients.

In the global market for type-2 diabetes treatments over the past decade, new drugs such as GLP-1 analogues, DDP-4 inhibitors, and SGLT inhibitors have been emerging and achieving great success. Among them, the GLP-1 analogue series has particularly received a lot of attention as it has excellent drug efficacy and low side effects such as hypoglycemia.

G2GBIO's GB-7001 is a diabetes treatment that applies InnoLAMP technology to Semaglutide (GLP-1 analogue) and lasts for 4 weeks with a single administration, offering great advantages in terms of medication convenience compared to other GLP-1 analogues. GB-7001 has completed its formulation development and is currently undergoing pre-clinical trials in Korea.

GB-5313

GB-7101, GB-7103

Prostate cancer is one of the most common malignant tumors, accounting for about 20-30% of male cancer patients in the United States and Europe, and its incidence is increasing in Korea due to the westernization of dietary habits and an aging society. Treatment options for prostate cancer include surgical castration (orchidectomy), medical castration (estrogen therapy, LHRH agonists), and anti-androgen therapy. Orchidectomy has almost no surgical complications, but psychological shock due to surgical castration is a problem. Estrogen therapy is not used much these days due to cardiovascular and cerebrovascular side effects. On the other hand, physiologically active peptides such as LHRH analogues have fewer side effects and superior efficacy and are receiving attention as prostate cancer treatments. Despite the advantages of peptides over other treatments, their oral administration has the disadvantage of requiring long-term administration for several months to years as the absorption is low due to breakdown in the stomach and metabolism in the liver. To overcome these drawbacks, injection or nasal spray administration has been developed for peptide treatments, and G2GBIO has completed the development of a new dosage form using the InnoLAMP technology, which can maintain its effect for one to three months with a single administration. Preclinical studies in Korea are currently underway.

GB-6201, GB-6203

All male-pattern baldness treatments used in Korea are oral medications and consist of two types of drugs, finasteride and dutasteride. Among them, Propecia which uses finasteride and has received approval from the US Food and Drug Administration (FDA) is a representative product for hair loss treatment.

In the case of these oral hair loss treatments, there is an inconvenience in having to continuously take the medication at a designated time every day to maintain the hair loss treatment effect. Moreover, if the medication is not taken regularly, the efficacy of the drug may decrease, making it difficult for patients to achieve a satisfactory improvement effect.

To overcome these drawbacks, G2GBIO has developed a sustained-release injectable formulation that maintains the drug's efficacy for 1 month or 3 months after a single injection and is currently preparing for a clinical trial in Korea.

GH-001

만성 B형간염 치료 목표는 장기적으로 혹은 영구적으로 바이러스의 증식을 억제하고 혈청 아미노전이효소를 정상으로 유지시켜, 간경변증으로의 진행을 예방하고 간세포암의 발생을 억제하며 이를 통하여 사망률을 감소시키고 삶의 질을 향상시키는 데 있습니다.

뉴클리오사이드/뉴클리오타이드 (nucleoside/nucleotide) 유사체인 엔테카비르(Entecavir)의 경우, B형간염 바이러스 중합효소의 작용 지점에 직접 결합하여 바이러스의 복제를 막는 역할을 하는데, 이들은 대부분의 만성 B형간염 환자에게 효과를 보이며, 치료 동안의 바이러스 복제를 억제하는 능력이 매우 뛰어나고, 부작용 또한 적습니다.

하지만 이들 뉴클리오사이드/뉴클레오타이드 유사체의경우, 약물 치료 중단 시 곧바로 바이러스 복제가 시작되는데, 오직 약물치료 기간에만 이러한 치료 효과가 나타난다는 것이 이들의 가장 큰 단점입니다.

따라서 약효를 지속시켜 B형간염 치료 효과를 유지하기 위해서는 매일 일정한 시간에 지속적으로 복용을 해야 하는 문제가 존재하며, 최근에 사용중인 경구투여제의 경우 음식물과 함께 투약 시 약 18~20% 정도 흡수가 감소되기 때문에 공복 (식사 2시간 후 또는 최소 2시간 전) 투여가 권장되므로, 환자의 복약편의성 면에서 불편한 점이 있습니다. 또한 약물의 복약이 정상적으로 이루어지지 않아 나타날 수 있는 약제 내성 문제들도 있다.

그러므로 이를 해결하기 위한 방안으로 1회 투여로 장기간 약효 지속이 가능하며 복약 편의성을 보다 개선하기 위해 ㈜ 지투지바이오에서는 엔테카비르를 사용하여 생분해성 고분자에 봉입한 엔테카비르 서방형 주사제 연구를 수행 중이며 3개월 약효 지속가능한 제품을 목표로 개발을 수행중이며, 현재 전임상 전단계에 이르고 있으며, 현재 국내 대형 제약사와 함께 공동연구를 하고 있습니다.

GB-2001

GB-2006

As the trend of Pet Humanization spreads globally, various medical demands for companion animals are expanding, including postoperative pain relief drugs (Bupivacaine Liposome preparations).

So far, there has been only one product for postoperative pain relief drugs for animals in the global market. However, G2GBIO is developing an animal postoperative pain relief drug that uses Ropivacaine, a non-opioid analgesic similar to GB-6002, to relieve pain for more than three days. Unlike Bupivacaine, Ropivacaine has no cardiovascular toxicity, and it is expected to have a very high market potential upon completion of development.

Currently, G2GBIO is conducting clinical trials for GB-2006.