Our Key Active Ingredient: EF-API-001
EF-API-011
Key Active Ingredient
Two decades of relentless dedication materialized into a labor of love
■ Unleashing the Power of Traditional Chinese Medicine in Brain Cancer Treatment
The research and development team at Everfront Biotech has utilized a drug screening platform to identify the most promising active ingredients from traditional Chinese medicinal herbs and natural plants for the development of novel therapeutics targeting malignant glioblastoma. Analyzing over 50 traditional Chinese medicines and plants, we discovered that certain compounds possess the ability to inhibit telomerase activity, a crucial enzyme involved in the uncontrolled growth of cancer cells.
■Discovery and Therapeutic Potential of EF-API-001
During the development process, our team identified a small molecule known as EF-API-001, which is a key component found in traditional Chinese medicine. Through mouse experiments, it was discovered that injecting EF-API-001 into the brains of mice with glioblastoma significantly reduced tumor volume by approximately one-third after 16 days.
■Breakthrough in Treatment and Exploration of New Pathways
In a study conducted in 2016, the implantation of biodegradable polymer wafers (Cerebraca® Wafer) into mice enabled sustained release of high doses of EF-API-001 into the tumor site of recurrent glioblastoma. Compared to mice treated with traditional chemotherapy using Gliadel® Wafer, this novel treatment approach extended survival by 2.44 times and reduced the number of invasive cells found in the tumor. Additionally, our team is actively exploring the potential of EF-API-001 in treating various diseases such as amyotrophic lateral sclerosis (ALS), Alzheimer’s disease, and liver fibrosis.
Learn more: Cerebraca® Wafer
■The Mechanism of Action of EF-001
■Prospects and Challenges of Novel Treatment Methods
Research has revealed that administration of EF-API-001 can lead to a reduction in the expression of Axl protein, potentially opening up new avenues for treating glioblastoma.
Furthermore, our studies have identified the following mechanisms of cancer treatment associated with EF-API-001:
- Targeting Axl-1 receptor tyrosine kinase: Effectively inhibiting the growth and metastasis of brain tumor stem cells.
- Inhibiting PD-L1 immune checkpoint: Reducing the immunosuppressive nature of the tumor microenvironment, maintaining immune cell activity to kill tumor cells.
- Decreasing MGMT DNA repair enzyme: Overcoming resistance to Temozolomide (chemotherapy drug), allowing cancer cells to be killed by chemotherapy drugs once again.
■PIC/S GMP Production of EF-API-001
EF-API-001, a novel chemical entity (NCE), is being developed and produced by Everfront Biotech in compliance with PIC/S GMP standards. Everfront Biotech has established a scalable manufacturing process for EF-API-001. This compound has demonstrated good safety profiles in animal studies and Phase I clinical trials. Currently, it is undergoing human clinical trials in various formulations and therapeutic areas. We anticipate that these clinical trials will yield positive results swiftly, leading to the successful market launch of this medication.
Key Features:
- Low toxicity
- High purity
- Long shelf life
Multi-functional and Multi-target Therapeutic Opportunities
The Everfront team is actively delving into the biochemical characteristics of EF-API-001, exploring its mechanism of action (MOA), and uncovering potential applications beyond the treatment of brain cancer.
■Treating Pancreatic Cancer
Inhibiting the expression of DNA methyltransferase 1 (DNMT1), EF-009 Wafer demonstrates its efficacy in restraining pancreatic ductal adenocarcinoma (PDAC) cell growth and inducing cell cycle arrest at the G0/G1 phase, ultimately leading to apoptosis. Representing an innovative and challenging approach to pancreatic cancer treatment, EF-009 Wafer is an implantable dosage form designed for in situ therapy. This sustained-release drug delivery system provides continuous drug release at the tumor site for up to one month. It effectively suppresses cancer cell proliferation, modulates the tumor microenvironment, alleviates immune evasion, and enhances immune responses.
Learn more: EF-009 Wafer
■Treating Amyotrophic Lateral Sclerosis (ALS)
In animal studies, stimulation of mTOR signaling within SOD1G93A mutant cell lines has been shown to reduce the accumulation of LC3II and downstream autophagic effects, thereby extending the lifespan of SOD1G93A mice.
Learn more: HK-001 Soft capsules
■The Mechanism of Action of HK-001
■Treating Spinocerebellar Ataxia Type 3 (SCA3)
EF-API-001 modulates the early metabolic pathway of kynurenine, reducing the expression of tryptophan 2,3-dioxygenase (TDO2) and consequently lowering the downstream neurotoxic metabolite quinolinic acid (QA) generation. Furthermore, by controlling TDO2, EF-API-001 also reduces the levels of active calpain, a crucial enzyme involved in the degradation of mutant ATXN3 protein, thereby decreasing the generation of toxic fragments and associated neurotoxicity.
Learn more: TSCA-001
■Mechanism of Action for TSCA-001
■Treating Idiopathic Pulmonary Fibrosis (IPF)
In the promoter of type I collagen, there exists a specific binding site for SOX2. EF-API-001 can reduce the binding of SOX2 to the promoter of type I collagen, thereby inhibiting the expression and accumulation of type I collagen and preventing fibrosis formation both in vitro and in vivo.
Learn more: EF-011
■Mechanism of action of EF-011
■Treating Obesity
Brown adipose tissue (BAT) generates heat (non-shivering thermogenesis) to promote energy expenditure, as its mitochondrial content is higher than that of white adipose tissue (WAT). The primary function of BAT thermogenesis is to dissipate energy as heat to counteract obesity. In animal experiments with diet-induced obesity (DIO) mice, EF-API-001 has been found to prevent weight gain, improve serum parameters, increase energy expenditure, stimulate browning of white adipose tissue, reverse hepatic steatosis, and ameliorate metabolic conditions, thus demonstrating potential for treating obesity.
Partnering And Collaboration
EFB is looking for the opportunity to cooperate with international pharmaceutical companies or venture capitals.
Please mail us on efbiotech@efbiotech.com
