NCT04094519

A Study to Evaluate the Effect of Multiple Doses of Enzalutamide on the Pharmacokinetics of Substrates of P-glycoprotein (Digoxin) and Breast Cancer Resistant Protein (Rosuvastatin) in Male Subjects With Prostate Cancer

Completed Phase 1 Last updated 20 November 2024

What this trial tests

Phase 1 trial testing enzalutamide in Prostate Cancer in 24 participants. Completed in 27 December 2020.

Timeline

27 January 2020

Primary endpoint
27 December 2020

27 December 2020

Quick facts

Lead sponsor	Astellas Pharma Global Development, Inc.
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	na
Design	single group
Masking	none
Primary purpose	treatment
Enrollment	24
Start date	27 January 2020
Primary completion	27 December 2020
Estimated completion	27 December 2020
Sites	1 location across Moldova

Drugs / interventions tested

• enzalutamide (enzalutamide) — full drug profile →
• enzalutamide Placebo
• digoxin (digoxin) — full drug profile →
• rosuvastatin (rosuvastatin) — full drug profile →

Conditions studied

• Prostate Cancer — all drugs for Prostate Cancer →

Sponsor

Astellas Pharma Global Development, Inc. — full company profile →

Who can join

18 and older, male only, with Prostate Cancer. Patients with the condition only — healthy volunteers not accepted.

Sponsor's own description

The primary purpose of this study is to determine the effect of multiple once daily administrations of enzalutamide on the pharmacokinetics of a single dose of digoxin (P-glycoprotein (P-gp) substrate) and rosuvastatin (breast cancer resistant protein (BCRP) substrate) in participants with prostate cancer.

This study will also evaluate the safety and tolerability of multiple once daily administrations of enzalutamide alone and in combination with a single dose of digoxin (P-gp substrate) and rosuvastatin (BCRP substrate) in participants with prostate cancer, as well, assess the pharmacokinetics of enzalutamide and its active metabolite.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

1. The updated landscape of tumor microenvironment and drug repurposing.
   Jin MZ, Jin WL. · · 2020 · cited 900× · PMID 32843638 · DOI 10.1038/s41392-020-00280-x
2. Multidrug Resistance of Cancer Cells and the Vital Role of P-Glycoprotein.
   Karthika C, Sureshkumar R, Zehravi M, Akter R, et al · · 2022 · cited 75× · PMID 35743927 · DOI 10.3390/life12060897
3. Na⁺/K⁺-ATPase Revisited: On Its Mechanism of Action, Role in Cancer, and Activity Modulation.
   Bejček J, Spiwok V, Kmoníčková E, Rimpelová S. · · 2021 · cited 67× · PMID 33800655 · DOI 10.3390/molecules26071905
4. Metabolic changes during prostate cancer development and progression.
   Beier AK, Puhr M, Stope MB, Thomas C, et al · · 2023 · cited 50× · PMID 36151426 · DOI 10.1007/s00432-022-04371-w
5. Effect of enzalutamide on PK of P-gp and BCRP substrates in cancer patients: CYP450 induction may not always predict overall effect on transporters.
   Poondru S, Ghicavii V, Khosravan R, Manchandani P, et al · · 2022 · cited 9× · PMID 35118821 · DOI 10.1111/cts.13229
6. Path to Clonal Theranostics in Luminal Breast Cancers.
   Hajjaji N, Aboulouard S, Cardon T, Bertin D, et al · · 2021 · cited 7× · PMID 35096604 · DOI 10.3389/fonc.2021.802177
7. Cardiac glycosides: Looking beyond heart failure and atrial fibrillation.
   Omole JG, Udom GJ, Aturamu A, Agbana RD, et al · · 2025 · cited 4× · PMID 40324829 · DOI 10.4103/ijp.ijp_934_24
8. Revisiting the role of metabolic reprogramming as a contributor to prostate cancer disease progression.
   Ding H, Meng Q, Zhou J, Chen L, et al · · 2025 · PMID 41276494 · DOI 10.1097/cm9.0000000000003844