Roche's Potential Best-in-Class Breast Cancer Drug GDC-9545 Granted Clinical Trial Approval in China

China’s National Medical Products Administration (NMPA) Center for Drug Evaluation (CDE) has recently announced that Roche’s Class 1 novel drug, GDC-9545, has received implicit approval for clinical trials. The drug is intended for the treatment of estrogen receptor (ER)-positive, HER2-negative locally advanced or metastatic breast cancer. According to public information released earlier this year by Genentech, a member of the Roche Group, GDC-9545 is a selective estrogen receptor degrader (SERD) and a potential “best-in-class” novel therapy. It is currently undergoing Phase 3 clinical trials globally.

Screenshot source: CDE official website

GDC-9545 is a selective estrogen receptor degrader developed by Genentech. By binding to the estrogen receptor (ER), it prevents ER from activating the transcription of target genes and induces ER protein degradation, thereby more completely blocking ER-mediated signaling pathways.

According to public information, GDC-9545 is a potential “best-in-class” new drug administered orally. Studies have shown that this product has the following characteristics:

· The candidate drug exhibits higher and more potent activity and efficacy in vivo;

· Can completely block the estrogen receptor pathway;

· Demonstrates excellent pharmacokinetic (PK) data regarding efficacy at low doses in humans;

· Possesses a broad non-clinical safety margin.

The ClinicalTrials.gov website shows that five studies have been registered for GDC-9545. These include a Phase 3, randomized, double-blind, placebo-controlled, multicenter study designed to evaluate the efficacy and safety of GDC-9545 in combination with the CDK4/6 inhibitor palbociclib in patients with estrogen receptor-positive, HER2-negative locally advanced or metastatic breast cancer.

▲Introduction to GDC-9545 (Image source: Reference [2])

Breast cancer is the most common cancer among women worldwide. It is estimated that 90% of breast cancers are diagnosed at an early stage. The most common subtype is hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer, which accounts for 70% of all breast cancer cases. Approximately 30% of patients diagnosed with early-stage HR+, HER2- breast cancer remain at risk of cancer recurrence. If patients present with certain clinical and/or pathological features, such as lymph node involvement, larger tumor size, and higher histological grade, their risk of recurrence is significantly increased.

Currently, the standard treatment for patients with hormone receptor-positive (HR+) breast cancer is estrogen receptor inhibitors. However, existing inhibitors do not fully suppress estrogen receptor function, allowing some estrogen receptor-positive (ER+) tumor cells to continue proliferating. Therefore, there is an urgent need for new therapeutic options for these patients.

Source: Medical Observation

▽Follow [WuXi AppTecDe】WeChat Official Account