Amcenestrant

Experimental drug for breast cancer treatment

{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (2S)-2-[[4-[2-(4-cyano-1H-pyrazol-1-yl)ethoxy]phenyl]sulfonyl]-3-(4-hydroxyphenyl)propanoic acid | image = Amcenestrant.svg | image2 = Amcenestrant.svg | width = 200 | alt = Chemical structure of Amcenestrant }}

Amcenestrant is an investigational drug being developed for the treatment of breast cancer. It is classified as a selective estrogen receptor degrader (SERD), which is a type of endocrine therapy that targets the estrogen receptor (ER) in hormone receptor-positive breast cancer.

Mechanism of Action

Amcenestrant works by binding to the estrogen receptor and inducing a conformational change that leads to the degradation of the receptor. This action reduces the number of estrogen receptors available in the cell, thereby inhibiting the growth of cancer cells that rely on estrogen signaling for proliferation. Unlike selective estrogen receptor modulators (SERMs), which block the receptor's activity, SERDs like amcenestrant lead to the receptor's destruction.

Development and Clinical Trials

Amcenestrant is being developed by Sanofi, a global biopharmaceutical company. It is currently undergoing clinical trials to evaluate its efficacy and safety in patients with hormone receptor-positive breast cancer. The drug is being tested both as a monotherapy and in combination with other treatments, such as CDK4/6 inhibitors and aromatase inhibitors.

Phase I Trials

The initial phase I trials focused on determining the safety, tolerability, and pharmacokinetics of amcenestrant in patients with advanced breast cancer. These studies helped establish the appropriate dosing regimen for subsequent trials.

Phase II and III Trials

In phase II trials, amcenestrant demonstrated promising activity in patients with hormone receptor-positive breast cancer, leading to further investigation in phase III trials. These later-stage trials aim to compare the efficacy of amcenestrant with existing standard-of-care treatments.

Potential Benefits

Amcenestrant offers several potential benefits over existing therapies. As a SERD, it may overcome resistance mechanisms associated with long-term use of SERMs and aromatase inhibitors. Additionally, its oral administration provides a convenient alternative to injectable SERDs like fulvestrant.

Challenges and Considerations

While amcenestrant shows promise, there are challenges in its development. The complexity of breast cancer biology means that not all patients may respond to SERD therapy. Identifying biomarkers that predict response to treatment is an ongoing area of research.

Related Pages

• Breast cancer
• Estrogen receptor
• Selective estrogen receptor degrader
• Endocrine therapy