Daiichi Sankyo's EZH1/2 Inhibitor Valemetostat Receives Two IND Approvals in China for First-Line NSCLC Combination Therapy with Pembrolizumab

Sep 11, 2024 14:30 CST Updated 14:30

Daiichi-Sankyo

Pharmaceutical R&D Developer

▎Edited by the WuXi AppTec content team

On September 10, the Center for Drug Evaluation of the National Medical Products Administration of China(CDE) Official WebsitePublic Notice: DS-3201b Tablets, submitted by Daiichi Sankyo, have been approved.Approval for 2 clinical trials, indications areIn combination with pembrolizumab for the first-line treatment of advanced or metastatic non-small cell lung cancer (NSCLC) expressing PD-L1 (TPS≥50%) without driver genomic alterations.。

Public information shows,DS-3201b Tablets (valemetostat) isAEZH1/2 Dual Inhibitor，In September 2022 inJapanApproved for marketing, isThe world's first to receive regulatory approvalEZH1/2Inhibitor.

Screenshot source: CDE official website

Public information shows,DS-3201bIt is a "first-in-class" dual inhibitor of histone lysine methyltransferase (EZH) 1/2, used to treat various hematologic malignancies and solid tumors, including non-Hodgkin lymphoma (NHL). The product wasSeptember 2022InJapanApproved for Marketing(Product name isEzharmia），Used to treat recurrent or refractory adult T-cell leukemia/lymphoma (ATL), a subtype of NHL.

Currently, Daiichi Sankyo is also exploringvThe Therapeutic Potential of Alemetostat in More Cancer Types. Especially in combination therapy,vThe progress of alemetostat that has drawn more attention includes:AssociatedCombineCTLA-4Targeted AntibodyIpilimumab TreatmentClinical studies on metastatic prostate cancer, urothelial cancer, and renal cell carcinoma; combinationYiIrinotecan TreatmentResearch on Recurrent Small Cell Lung Cancer;AssociatedHER2-targeted ADC drugsDS-8201 in the Treatment of HER2 Low-Expression/Negative Advanced Breast CancerResearch, etc.

This timevThe two clinical trials approved for alemetostat in China areCompared with the PD-1 star drug PembrolizumabCombined Therapy, aiming to explore the potential of first-line treatment for advanced or metastatic non-small cell lung cancer (NSCLC) with tumor expression of PD-L1 (TPS≥50%) and no driver genomic alterations.

It is worth mentioning that,EZH1/2 is one of the frontier targets in epigenetics.The study points out that EZH1/2 is associated with the suppression of tumor suppressor gene expression and the promotion of tumor growth.EZH1/2, as part of the Polycomb protein complex, can assist in regulating and maintaining the expression of hematopoietic stem cell genes through histone methylation.These two proteins are often overexpressed in hematological malignancies, including T-cell lymphoma, and mutations in them are commonly seen in relapsed tumors.

VAlemetostat isThe world's first to receive regulatory approval for cancer treatmentEZH1/2Inhibitors, Global TargetMore R&D pipelines for EZH1/2 are advancing.。In China, forThe new drug R&D pipeline for the EZH2 target already has several candidates in clinical development, fromHutchmed, Hengrui Medicine, Haihe Biopharma, Xennovate Pharma, etc.。

CurrentEpigenetic regulators are an emerging class of cancer treatment targets, and many epigenetic therapies are currently in clinical trials.Under development. In addition to EZH2, more epigenetic targets such as histone deacetylase (HDAC), DNA methyltransferase (DNMT), and histone-binding protein BET have also shown therapeutic potential in cancer treatment.

References:

[1] Official website of the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) of China. Retrieved Sep 10, 2024, from https://www.cde.org.cn/main/xxgk/listpage/9f9c74c73e0f8f56a8bfbc646055026d

[2] EZHARMIA® Approved in Japan as First Dual EZH1 and EZH2 Inhibitor Therapy for Patients with Adult T-Cell Leukemia/Lymphoma. Retrieved September 27, 2022 from https://www.daiichisankyo.com/files/news/pressrelease/pdf/202209/20220926_E.pdf

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