Pfizer's Investigational EZH2 Inhibitor PF-06821497 Receives Two Additional Clinical Approvals in China for Metastatic Castration-Resistant Prostate Cancer

Sep 13, 2024 15:48 CST Updated 15:48

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China's National Medical Products Administration (NMPA) Center for Drug Evaluation (CDE) website recently announced that Pfizer’s Class 1 new drug PF-06821497 tablets have received two implied clinical trial approvals. The indications are: proposed combination with enzalutamide for metastatic prostate cancer patients who have not previously received novel endocrine therapy or chemotherapy.Male patients with metastatic castration-resistant prostate cancerTreatment. Public information shows,PF-06821497 (mevrometostat) is an investigational EZH2 inhibitor.. According to Pfizer in March this yearOncology Innovation DayDuring theDisclosureBy 2030, its oncology R&D pipeline is expected to launch more than 8 blockbuster therapies, including this EZH2 inhibitor.

Screenshot source: CDEOfficial Website

EZH2 is a histone methyltransferase that controls the expression of various genes by catalyzing the methylation of histone H3 lysine 27 (H3K27), thereby regulating normal physiological functions of cells. The abnormal expression of EZH2 is associated with the progression and poor prognosis of various cancers, including prostate cancer, breast cancer, lung cancer, and hematological malignancies, among others. Existing studies have suggested,The overexpression of EZH2 can promote the occurrence and progression of cancer through various mechanisms of action, including silencing the expression of tumor suppressor genes, promoting the expression of genes involved in cell proliferation and survival, and so on.In addition, EZH2 has been shown to promote cancer metastasis by regulating the expression of genes involved in epithelial-mesenchymal transition, a process through which cancer cells acquire migratory and invasive properties.

Currently, EZH2 has become one of the leading targets in cancer treatment.MevrometostatIt is an EZH2-targeted inhibitor developed by Pfizer.It can block the abnormal gene expression driven by EZH2 overexpression in cancer cells, leading to reduced cancer cell proliferation, induction of cell death, andInhibitionCancer cell migration and invasion, ultimately achieving the goal of treating cancer.

According to the clinical data disclosed by Pfizer at the Innovation Day in Oncology held in March this year,mevrometostatAndXtandi (enzalutamide) Combination TherapyIn the phase 1 clinical trial targeting pretreated metastatic castration-resistant prostate cancer (mCRPC) patients, encouraging anticancer activity was demonstrated.Support the product's entry into Phase 3 clinical research. Among these, mevrometostat + enzalutamide for the treatment of mCRPC patients previously treated with abiraterone.The median radiographic progression-free survival (rPFS) was 17.1 months, showing significant benefit compared to historical data (rPFS of 4.8 months).; The rPFS for mCRPC patients previously treated with enzalutamide was 11.7 months. The most common TRAEs were diarrhea, anorexia, and anemia.

▲Clinical Trial Results of Mevrometostat (Image Source: Pfizer's Official Website)

Pfizer Plans to Launch Two Phase 3 Clinical Trials in the Second Half of 2024, Evaluating the Efficacy of Mevrometostat + Enzalutamide in mCRPC Patients Previously Treated with Abiraterone and in Treatment-Naïve mCRPC Patients, Respectively. According toClinicalTrialsAccording to the official website, Pfizer has launched one of its Phase III clinical trials in the United States this August.（MEVPRO-1 Study, for mCRPC patients who have previously received abiraterone acetate treatment.

In China,Mevrometostat has previously been approved for clinical use, intended to be combined with enzalutamide for the treatment of mCRPC patients who have previously received abiraterone acetate treatment. The approval of this new clinical study signifies new research and development progress in China.

Existing studies have shown that EZH2 inhibitors haveShowing potential to treat multiple types of cancer, including B-cell lymphoma, solid tumors, and certain other blood cancers.For example,TazemetostatAlreadyApproved for the treatment of certain types ofHematomaTumor. Meanwhile,Multiple EZH2 inhibitors are currently under development worldwide for the treatment of various types of tumors. It is hoped that these studies will proceed smoothly and benefit more patients as soon as possible.

References:

[1] Website of the Center for Drug Evaluation (CDE) under the National Medical Products Administration (NMPA) of China. Retrieved Feb 14, 2023, from https://www.cde.org.cn/main/xxgk/listpage/4b5255eb0a84820cef4ca3e8b6bbe20c

[2]Oncology Innovation Day. Retrieved March 1, 2024, from https://s28.q4cdn.com/781576035/files/doc_downloads/2024/02/29/Pfizer-Oncology-Innovation-Day-Presentation_FINAL.pdf

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