flutamide

Overview

Flutamide is a first-generation nonsteroidal androgen receptor (AR) antagonist used historically in the treatment of prostate adenocarcinoma (PRAD). The AR H875Y point mutation, also known as T877A in some numbering schemes, has been characterized as a resistance mutation that allows flutamide to act as an AR agonist rather than antagonist.

Evidence in the corpus

• AR H875Y mutation associated with flutamide resistance detected via MSK-IMPACT in locoregional prostate cancer; illustrates that first-generation AR resistance mechanisms are detectable even in early-stage disease PMID:28825054.

Resistance mechanisms

• AR H875Y — point mutation in the AR ligand-binding domain; converts flutamide from antagonist to agonist, conferring drug resistance; identified by targeted sequencing in locoregional prostate cancer patients PMID:28825054.

Cancer types (linked)

• PRAD — prostate adenocarcinoma; primarily historical use in androgen-deprivation therapy combinations PMID:28825054.

Sources

• PMID:28825054 — Abida et al. 2017, MSK-IMPACT pan-prostate cancer genomic profiling (504 tumors, 451 patients); describes AR H875Y resistance to flutamide detected in locoregional tumors.

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