{"doi":"10.1002/pros.2990120110","title":"Plasma levels of hydroxy‐flutamide in patients with prostatic cancer receiving the combined hormonal therapy: An LHRH agonist and flutamide","abstract":"<jats:title>Abstract</jats:title><jats:p>The present study describes a method for the measurement of the plasma levels of hydroxy‐flutamide (Flu‐OH), the biologically active and main circulating metabolite of flutamide. We have observed that two to four hours after oral administration of 250 mg of flutamide to healthy young men, as well as to patients with prostate cancer, the plasma concentration of Flu‐OH reaches a peak at approximately 1.7 μM. The plasma concentration of Flu‐OH measured at months 6, 12, and 18 of treatment shows a minimal basal level of 3.4 μM with a maximal increase at 6.8 to 8.5 μM at 2 to 4 hours. Since the serum levels of testosterone in these patients are approximately 1 nM, the levels of the active antiandrogen are at a 5000‐ to 10000‐fold excess. However, due to the low affinity of the antiandrogen for the androgen receptor, it is extremely important to maintain this concentration of the antiandrogen in plasma constant.</jats:p>","journal":"The Prostate","year":1988,"id":671439,"datarank":3.1775876518436874,"base_score":3.258096538021482,"endowment":3.258096538021482,"self_citation_contribution":0.4887144807032224,"citation_network_contribution":2.688873171140465,"self_endowment_contribution":0.4887144807032224,"citer_contribution":2.688873171140465,"corpus_percentile":null,"corpus_rank":null,"citation_count":25,"citer_count":24,"citers_with_citation_signal":23,"citers_with_endowment":23,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1754124,"name":"Marcelle Giasson","orcid":null,"position":1,"is_corresponding":false},{"id":1754125,"name":"Jean Couture","orcid":null,"position":2,"is_corresponding":false},{"id":1754126,"name":"André Dupont","orcid":null,"position":3,"is_corresponding":false},{"id":1754127,"name":"Leonello Cusan","orcid":null,"position":4,"is_corresponding":false},{"id":143912,"name":"Fernand Labrie","orcid":null,"position":5,"is_corresponding":false},{"id":1754122,"name":"Alain Bélanger","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Plasma levels of hydroxy‐flutamide in patients with prostatic cancer receiving the combined hormonal therapy: An LHRH agonist and flutamide","abstract":"<jats:title>Abstract</jats:title><jats:p>The present study describes a method for the measurement of the plasma levels of hydroxy‐flutamide (Flu‐OH), the biologically active and main circulating metabolite of flutamide. We have observed that two to four hours after oral administration of 250 mg of flutamide to healthy young men, as well as to patients with prostate cancer, the plasma concentration of Flu‐OH reaches a peak at approximately 1.7 μM. The plasma concentration of Flu‐OH measured at months 6, 12, and 18 of treatment shows a minimal basal level of 3.4 μM with a maximal increase at 6.8 to 8.5 μM at 2 to 4 hours. Since the serum levels of testosterone in these patients are approximately 1 nM, the levels of the active antiandrogen are at a 5000‐ to 10000‐fold excess. However, due to the low affinity of the antiandrogen for the androgen receptor, it is extremely important to maintain this concentration of the antiandrogen in plasma constant.</jats:p>","is_dataset_classified":null,"base_score":3.258096538021482,"endowment":3.258096538021482,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"3279409","pmcid":null,"openalex_id":"https://openalex.org/W2080966978","authors":[],"funders":[],"total_grants":0,"fwci":1.0165,"citation_percentile":0.78454867,"influential_citations":0,"citation_trend":[{"year":2013,"count":2},{"year":2014,"count":1},{"year":2020,"count":1}],"oa_status":"closed","license":"http://onlinelibrary.wiley.com/termsAndConditions#vor","oa_locations":[{"url":"https://api.wiley.com/onlinelibrary/tdm/v1/articles/10.1002%2Fpros.2990120110","host_type":"publisher"},{"url":"https://onlinelibrary.wiley.com/doi/pdf/10.1002/pros.2990120110","host_type":"publisher"},{"url":"https://doi.org/10.1002/pros.2990120110","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/3279409","host_type":"repository"}],"fields_of_study":["Hormonal and reproductive studies","Prostate Cancer Treatment and Research","Effects and risks of endocrine disrupting chemicals","Adult","Aged","Anilides","Antineoplastic Combined Chemotherapy Protocols","Flutamide","Gonadotropin-Releasing Hormone","Humans","Kinetics","Male","Middle Aged","Prostatic Neoplasms","Testosterone","Triptorelin Pamoate"],"mesh_terms":["Adult","Aged","Anilides","Antineoplastic Combined Chemotherapy Protocols","Flutamide","Humans","Kinetics","Gonadotropin-Releasing Hormone","Male","Middle Aged","Prostatic Neoplasms","Testosterone","Triptorelin Pamoate"],"keywords":["Flutamide","Antiandrogen","Endocrinology","Internal medicine","Prostate cancer","Testosterone (patch)","Medicine","Androgen receptor","Prostate","Agonist","Androgen","Metabolite","Hormone","Cancer","Receptor"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-16T02:44:33.046140Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}