Ascletis Announces Investment Escalation in R&D of Cancer Lipid Metabolism and Oral Checkpoint Inhibitors

On March 29, 2021 Ascletis Pharma Inc. (HKEX: 1672) reported that the board of directors (the "Board") of the Company has resolved to deploy more resources and investment in the R&D of cancer lipid metabolism and oral checkpoint inhibitors, our pipeline of which is shown below (Press release, Ascletis, MAR 29, 2021, View Source [SID1234577295]):

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The Board believes that the Company has made significant efforts and progress over the last few years through in-licensing and in-house R&D in the areas of cancer lipid metabolism and oral PD-L1 small molecule inhibitors, which has laid a solid foundation for the future development in our oncology pipeline.

The positive results were demonstrated from the investigator sponsored Phase II trial of ASC40(TVB-2640) in combination with bevacizumab in patients with first relapse of high-grade astrocytoma, which was completed in the United States (ClinicalTrials.gov Identifier: NCT03032484). The Company plans to initiate a pivotal randomized, double-blind, placebo-controlled Phase II trial of ASC40 (TVB-2640) in combination with bevacizumab in China for the same patient population (first relapse of high-grade astrocytoma) as in the United States.

The data from the investigator sponsored Phase II trial were presented at European Society for Medical Oncology 2020 and have shown that the overall response rate (ORR) for ASC40 (TVB-2640) plus bevacizumab was 65% including the complete response (CR) of 20% and partial response (PR) of 45%. Furthermore, the data indicate that the progression-free survival at six months (PFS6) observed for ASC40 (TVB-2640) plus bevacizumab was 47%, representing a statistically significant improvement in PFS6 over historical bevacizumab monotherapy (BELOB16%, P=0.01). ASC40 (TVB-2640) in combination with bevacizumab was safe and well tolerated in such patient population.

Lipid metabolism has been reported to play a critical role in various cancers. Fatty acid synthase (FASN) is one of the most important proteins which regulate lipid metabolism. Many solid and hematopoietic tumors overexpress FASN, including glioblastoma (GBM, Grade IV astrocytoma), non-small cell lung, breast, ovarian, prostate, colon, pancreatic cancers, and non-Hodgkin lymphoma.

In addition to FASN inhibitors in combination of bevacizumab, an anti-angiogenesis drug, in-house data and external research papers indicate that FASN inhibitors have potential to treat multiple tumors in combination with signal transduction inhibitors and immunotherapies. Therefore, the Company is considering additional clinical trials for (1) ASC40 in combination with chemotherapies for high-grade astrocytoma immediately followed by the surgery and radiation therapy; (2) ASC40 in combination with other therapies for various solid tumors. As a next generation oral FASN inhibitor, ASC60 has potential to be combined with other therapies for various solid tumors.

In addition to cancer lipid metabolism drug candidates targeting FASN, the Company’s oral PD-L1 small molecule inhibitors discovered in-house have shown favorable anti-tumor activities in animal model compared to a marketed anti-PD-L1 antibody. The Company believes that oral PD-L1 small molecule inhibitors are next generation checkpoint inhibitors as cancer immune therapies and have potential to be combined with oral FASN small molecule inhibitors.

"We are excited about our oncology pipeline since it has strong competitive edges in the crowded oncology space," said Dr. Jinzi J. Wu, Founder, Chairman and CEO of Ascletis. "The recent breakthrough from the Phase II trial in patients with first relapse of high-grade astrocytoma indicates that oral FASN inhibitors can play a significant role in the treatment of multiple solid tumors. Furthermore, we are now seeking collaborations with other pharmaceutical companies to develop various combination regimens with FASN inhibitors."