Enzalutamide (Xtandi)

Other Medications · Approved since 2012

US Off-label EU EMA Approved ES Hospital use off-label in CRC Oral 6 Clinical Trials
Androgen receptor (AR)

Description

Enzalutamide is an androgen receptor antagonist primarily approved for prostate cancer treatment that is being explored in colorectal cancer through tumor-agnostic approaches. In CRC, this medication is utilized in select cases where androgen receptor signaling may contribute to tumor growth, particularly in patients with specific molecular profiles including MET alterations or microsatellite instability-high (MSI-H) tumors. The drug represents a hormone-targeted approach to treating solid tumors that express androgen receptors, extending beyond its established prostate cancer indication.

Mechanism of Action

Enzalutamide blocks androgen receptor signaling by competitively inhibiting androgen binding, preventing nuclear translocation of the receptor complex, and impairing DNA binding. This triple mechanism of action disrupts androgen-dependent cellular processes that can drive tumor growth in cancers expressing functional androgen receptors.

Molecular Targets

Side Effects

Fatigue Hot flashes Hypertension Diarrhea Decreased appetite Weight loss Arthralgia Cognitive impairment

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

Clinical Trials

NCT07277270 Phase 1
Recruiting
A Study of GSK5764227 in Combination With Standard of Care (SoC) or Other Agents in Participants With Advanced Solid Tumors
United States, Australia, Spain
NCT07620574 Phase 3
Not yet recruiting
Long-Term Extension Study for Participants Previously Enrolled in an Exelixis-Sponsored Study
NCT05551117 Phase 2
Completed
A Study of Vobramitamab Duocarmazine in Participants With Metastatic Castration Resistant Prostate Cancer and Other Solid Tumors
United States, Australia, Belgium, France, Italy, Poland, South Korea, Spain, Un
NCT05057013 Phase 1
Active, not recruiting
A Phase I/IIa Trial of HMBD-001 in Advanced HER3 Positive Solid Tumours
United Kingdom
NCT03685591 Phase 1
Archived
PF-06952229 Treatment in Adult Patients With Advanced Solid Tumors
United States
NCT02740985 Phase 1
Archived
A Phase 1 Clinical Study of AZD4635 in Patients With Advanced Solid Malignancies
United States

Quick Info

Brand NameXtandi
CategoryOther Medications
US StatusOff-label
EU EMA StatusEMA Approved
ES Spain AccessHospital use off-label in CRC
AdministrationOral
Year Approved2012
Clinical Trials6
View Clinical Trials Back to Drug Glossary

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Medical Disclaimer

This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.