Giredestrant

Selective estrogen receptor degrader

Giredestrant
[[File: Chemical structure of Giredestrant |frameless|220px|alt=|]]
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number	2411274-68-3
PubChem	137460970
DrugBank
ChemSpider	64835292
KEGG

Giredestrant is a selective estrogen receptor degrader (SERD) that is being investigated for the treatment of hormone receptor-positive breast cancer. It is designed to bind to the estrogen receptor and induce its degradation, thereby inhibiting the growth of estrogen-dependent tumors.

Mechanism of Action

Giredestrant functions by targeting the estrogen receptor (ER), a nuclear hormone receptor that is activated by the hormone estrogen. In hormone receptor-positive breast cancer, the growth of cancer cells is often driven by estrogen signaling through the ER. Giredestrant binds to the ER and promotes its degradation, reducing the receptor's ability to mediate estrogen signaling. This action helps to inhibit the proliferation of cancer cells that rely on estrogen for growth.

Clinical Development

Giredestrant is currently undergoing clinical trials to evaluate its efficacy and safety in patients with hormone receptor-positive breast cancer. These trials aim to determine the optimal dosing regimen and to assess the drug's effectiveness in comparison to existing therapies such as tamoxifen and aromatase inhibitors.

Pharmacokinetics

The pharmacokinetic profile of giredestrant includes its absorption, distribution, metabolism, and excretion. Giredestrant is administered orally, and its bioavailability is influenced by factors such as food intake and patient-specific variables. The drug is metabolized primarily in the liver, and its metabolites are excreted via the urine and feces.

Potential Benefits

Giredestrant offers potential benefits over traditional therapies by providing a novel mechanism of action that directly targets and degrades the estrogen receptor. This could lead to improved outcomes for patients with hormone receptor-positive breast cancer, particularly those who have developed resistance to other forms of endocrine therapy.

Side Effects

As with any therapeutic agent, giredestrant may cause side effects. Commonly reported side effects in clinical trials include nausea, fatigue, and hot flashes. The safety profile of giredestrant continues to be evaluated in ongoing studies.

Related Pages

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