PharmaEngine, Inc. (TWO:4162) announces PEP08 Phase I clinical trial in solid tumors has been approved by Australia HREC (Human Research Ethics Committee) and acknowledged by Australia TGA (Therapeutic Goods Administration). (ClinicalTrials.gov Identifier: NCT06973863)

 

PEP08 is a second-generation PRMT5 inhibitor (protein arginine methyltransferase 5). PRMT5 has important functions in maintaining stable cell survival, including gene transcription, cell growth, DNA damage response, and immune regulation, so inhibiting the PRMT5 function can lead to tumor cell apoptosis. Compared with the first-generation PRMT5 inhibitors, PEP08 is more precise in inhibiting only tumor cells with the MTAP gene deletion and does not affect the growth of normal cells. This feature also allows PEP08 to achieve lower toxicity and improved safety compared to first-generation PRMT5 inhibitors.

 

MTAP gene deletion is observed in 10-15% of human cancers, including brain cancer, pancreatic cancer, non-small cell lung cancer, gastric cancer and bladder cancer, and are related to poor prognosis. Among them, brain cancer has the highest MTAP gene deletion rate of more than 40%, and pancreatic cancer and bladder cancer also have 20-25% of MTAP gene deletion. According to Globocan 2022 data, there are about 20 million new cancer patients worldwide, so it is estimated that 2-3 million cancer patients will have MTAP gene deletion.

 

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About PEP08

 

PEP08 is a second-generation PRMT5 inhibitor (protein arginine methyltransferase 5). PRMT5 has important functions in maintaining stable cell survival, including gene transcription, cell growth, DNA damage response, and immune regulation, so inhibiting the PRMT5 function can lead to tumor cell apoptosis. Compared with the first-generation PRMT5 inhibitors, PEP08 is more precise in inhibiting only tumor cells with the MTAP gene deletion and does not affect the growth of normal cells. This feature also allows PEP08 to achieve lower toxicity and improved safety compared to first-generation PRMT5 inhibitors.

 

Preclinical animal experiments have shown that PEP08 can significantly inhibit the growth of tumor cells with MTAP gene deletion. Pharmacokinetic data also shows that PEP08 can penetrate the blood-brain barrier to reach the brain and inhibit brain tumor growth, which has great potential for the future treatment of brain cancer.

 

Moreover, current research data shows that PEP08 has a better tumor cell inhibition effect than other competitors. Therefore, PEP08 has the most potential to become the best-in-class candidate drug for PRMT5 inhibitors currently under development for MTAP gene deletion tumors.

 

About PharmaEngine, Inc.

PharmaEngine, Inc., headquartered in Taipei, began operations in February 2003. PharmaEngine focuses on new drug development by adopting “Virtual Pharmaceutical Company Business Model”. PharmaEngine has one commercial product, ONIVYDE®, which is currently approved in most major markets including the U.S., Europe, and Asia in combination with fluorouracil and leucovorin for the treatment of adult patients with metastatic pancreatic adenocarcinoma after disease progression. PharmaEngine also conducts, collaborates or licenses-in new drug discovery and development projects. With extensive experience in drug development and project management, we continue to expand our pipeline and accelerate drug development and the subsequent commercialization of new medicines.

 

Media Contact: ChiHsing Chang, Spokesperson/Vice President (info@pharmaengine.com)