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PubChem
| Name: | Flutamide |
|---|---|
| PubChem Compound ID: | 10802904 |
| Description: | An antiandrogen with about the same potency as cyproterone in rodent and canine species. |
| Molecular formula: | C11H11F3N2O3 |
| Molecular weight: | 283.255 g/mol |
DrugBank
Identification
| Name: | Flutamide |
|---|---|
| Name (isomeric): | DB00499 |
| Drug Type: | small molecule |
| Description: | An antiandrogen with about the same potency as cyproterone in rodent and canine species. |
| Synonyms: |
FTA; Flutamide USP25
|
| Brand: | Eulexin, Niftholide, Cebatrol, Niftolide |
| Category: | Androgen Antagonists, Antineoplastic Agents, Hormonal |
| CAS number: | 13311-84-7 |
Pharmacology
| Indication: | For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate |
|---|---|
| Pharmacology: |
Flutamide is a nonsteroidal antiandrogen. In animal studies, flutamide demonstrates potent antiandrogenic effects. It exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues or both. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that countera...
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| Mechanism of Action: | Flutamide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Flutamide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen. |
| Absorption: | Rapidly and completely absorbed. |
| Protein binding: | 94-96% |
| Biotransformation: | Flutamide is rapidly and extensively metabolized, with flutamide comprising only 2.5% of plasma radioactivity 1 hour after administration. |
| Route of elimination: | Flutamide and its metabolites are excreted mainly in the urine with only 4.2% of a single dose excreted in the feces over 72 hours. |
| Half Life: | The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours. |
| Toxicity: | In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia. |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
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Targets
Enzymes
