A Biological Profile of a Nonsteroidal Antiandrogen, SCH 13521 (4'–Nitro–3'–Trifluoromethylisobutyranilide)1

Neri, R.; Florance, K; Koziol, Patricia; S, Van Cleave

doi:10.1210/endo-91-2-427

Cited by 330 publications

(107 citation statements)

References 0 publications

Supporting

Mentioning

104

Contrasting

Unclassified

Order By: Relevance

“…OHF and its precursor, flutamide, are non-steroidal AR antagonists which are highly specific for the AR (154,155). Flutamide is converted in vivo to the more potent OHF by hepatic hydroxylation (156).…”

Section: Effects Of the Anti-androgen Hydroxyflutamide (Ohf) On Bone mentioning

confidence: 99%

Androgen effects on bone metabolism: recent progress and controversies

Hofbauer

Khosla

1999

European Journal of Endocrinology

122

View full text Add to dashboard Cite

Androgens have beneficial effects on skeletal development and maintenance in women and men. The detection and functional characterization of androgen receptors in bone cells has implicated bone tissue as a potential target tissue for androgens. Gonadal and adrenal androgens directly regulate various aspects of osteoblastic lineage cells, including proliferation, differentiation, mineralization, and gene expression. These effects may differ depending on the stage of differentiation, the number of androgen receptors, and other inherent characteristics (species, site, cell biology) of the osteoblastic cell system. In addition, recent studies have suggested that some of the anabolic and anti-resorptive effects of androgens on bone may be mediated by regulation of autocrine and paracrine factors in the bone microenvironment, including transforming growth factor-b, insulin-like growth factors (and their binding proteins), and interleukin-6. This review summarizes the recent progress made in our knowledge of androgen receptor action, local androgen metabolism in bone, and direct and indirect effects of gonadal and adrenal androgens as well as androgen receptor antagonists on bone cells.

show abstract

Section: Effects Of the Anti-androgen Hydroxyflutamide (Ohf) On Bone mentioning

confidence: 99%

Androgen effects on bone metabolism: recent progress and controversies

Hofbauer

Khosla

1999

European Journal of Endocrinology

122

View full text Add to dashboard Cite

show abstract

“…Thereafter, it binds to androgen receptors in prostate cancer cells and exhibits antitumor effects by inhibiting androgen action. 8 However, since flutamide is metabolized in the liver, hepatopathy has previously been a side-effect. In Japan, it has been reported that eight patients died of severe liver dysfunction including fulminant hepatitis.…”

Section: Discussionmentioning

confidence: 99%

Clinical utility of ursodeoxycholic acid in preventing flutamide‐induced hepatopathy in patients with prostate cancer: A preliminary study

et al. 2002

View full text Add to dashboard Cite

Background: The present study was designed to ascertain retrospectively the validity of ursodeoxycholic acid (UDCA) in the treatment of prostate cancer in terms of prophylactic effects on the occurrence of flutamide-induced hepatopathy in a large number of patients surveyed in a multi-center cooperative study. Methods: One hundred and eighty-one patients (74.1 ± 4.9 years) with prostate cancer treated with flutamide with (n = 70) or without (n = 111) UDCA were retrospectively evaluated and the occurrence of hepatopathy was compared between these two patient groups. Results: Between patients treated with UDCA and those without it, no significant differences were noted in age, clinical stage, grade, duration of flutamide administration and serum prostate-specific antigen (PSA) levels before treatment. However, there were significant differences in the presence or absence of previous treatments and treatments used together with flutamide. The incidence of hepatopathy was 11.4% (8/70) in patients with UDCA and 32.4% (36/111) in those without it, showing a statistically significant difference (P < 0.05). The hepatopathy-free rate obtained by the Kaplan-Meier method was also significantly higher in patients with UDCA (88.4% 1 year following flutamide administration) than that in those without it (59.6%) (P < 0.005). Conclusion:These results suggest that UDCA has a prophylactic effect against flutamide-induced hepatopathy in patients with prostate cancer.

show abstract

“…Flutamide has been shown to have hormonal activity only on androgen-dependent sex structures. 37,38 Flutamide monotherapy was shown to reduce bone pain in 77% with minimal change in libido or sexual potency in patients with previously untreated advanced prostate cancer. 31 Other investigators 31,32,39 con®rmed the ef®cacy of¯utamide.…”

Section: Flutamidementioning

confidence: 99%

Combined androgen blockade for advanced prostatic carcinoma

Göktaş

Ziada

Crawford

1999

Prostate Cancer Prostatic Dis

View full text Add to dashboard Cite

Hormonal therapy has been mainstay of treatment for advanced forms of prostate cancer for over 50 y. The choice of hormonal therapy for carcinoma of the prostate depends not only on the desired progression-free and overall survival but also on the patient's quality of life, treatment costs and treatment toxicities. At the present time, several important questions have been raised over optimal treatment modalities for advanced prostate cancer. The optimal form of this therapy is still an enigma.

show abstract

A Biological Profile of a Nonsteroidal Antiandrogen, SCH 13521 (4'–Nitro–3'–Trifluoromethylisobutyranilide)1

Cited by 330 publications

References 0 publications

Androgen effects on bone metabolism: recent progress and controversies

Androgen effects on bone metabolism: recent progress and controversies

Clinical utility of ursodeoxycholic acid in preventing flutamide‐induced hepatopathy in patients with prostate cancer: A preliminary study

Combined androgen blockade for advanced prostatic carcinoma

Contact Info

Product

Resources

About