fulvestrant (Faslodex)

Other Medications · Approved since 2002

US Off-label EU EMA Approved ES Funded by SNS off-label in CRC Intramuscular 4 Clinical Trials
Estrogen receptor alpha

Description

Fulvestrant is a selective estrogen receptor degrader (SERD) that is FDA-approved for estrogen receptor-positive breast cancer but is being explored in colorectal cancer patients with HER2 alterations. In CRC, fulvestrant appears in clinical trials as combination therapy alongside HER2-targeted agents like tucatinib and trastuzumab for tumors harboring HER2 mutations or amplifications. This represents an off-label application exploring potential hormone pathway interactions in HER2-positive colorectal tumors.

Mechanism of Action

Fulvestrant binds to estrogen receptors with high affinity and promotes their degradation, effectively eliminating estrogen receptor signaling. Unlike selective estrogen receptor modulators, fulvestrant acts as a pure antagonist with no agonist activity, leading to complete blockade of estrogen-mediated cellular proliferation.

Molecular Targets

Side Effects

Injection site reactions Hot flashes Nausea Fatigue Headache Back pain Vomiting Constipation

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT07540572 Phase 1
Recruiting
A Study to Investigate the Safety, Pharmacokinetics, and Preliminary Efficacy of IDE574 Therapy in Adult Participants With Advanced Solid Tumors
United States
NCT07318805 Phase 1
Recruiting
A Study to Learn About the Study Medicine Called PF-08032562 in People With Advanced or Metastatic Solid Tumors
United States
NCT06625775 Phase 1
Recruiting
Open-Label Study of BBO-10203 in Subjects With Advanced Solid Tumors
United States, Australia, France, Spain
NCT04579380 Phase 2
Active, not recruiting
Basket Study of Tucatinib and Trastuzumab in Solid Tumors With HER2 Alterations
United States, Belgium, Germany, Italy, Japan, South Korea, Spain, United Kingdo