Efavirenz directly modulates the oestrogen receptor and induces breast cancer cell growth

HIV Medicine

Volumn 11, Issue 9, 2010, Pages 603-607

  Sikora, M J ^a   Rae, J M ^b   Johnson, M D ^c   Desta, Z ^d  

^a UNIVERSITY OF MICHIGAN HEALTH SYSTEM   (United States)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

^c GEORGETOWN UNIVERSITY   (United States)

^d INDIANA UNIVERSITY   (United States)

Author keywords

Efavirenz; Gynaecomastia; Highly active antiretroviral therapy; Oestrogen receptor; Oestrogens

Indexed keywords

CRYSTAL VIOLET; EFAVIRENZ; ESTRADIOL; ESTROGEN RECEPTOR; FULVESTRANT;

ARTICLE; BINDING AFFINITY; BREAST CANCER; CANCER GROWTH; CELL GROWTH; CELL STRAIN MCF 7; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; DRUG RECEPTOR BINDING; GYNECOMASTIA; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; STAINING;

BENZOXAZINES; BREAST NEOPLASMS; CELL PROLIFERATION; CELLS, CULTURED; DOSE-RESPONSE RELATIONSHIP, DRUG; ESTRADIOL; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; FEMALE; GYNECOMASTIA; HUMANS; INHIBITORY CONCENTRATION 50; MALE; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 77956415880     PISSN: 14642662     EISSN: 14681293     Source Type: Journal    
DOI: 10.1111/j.1468-1293.2010.00831.x     Document Type: Article

References (21)

1. Palella FJ, Delaney KM, Moorman AC. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV outpatient study investigators. N Engl J Med 1998, 338:853-860.
2. Carr A, Cooper DA. Adverse effects of antiretroviral therapy. Lancet 2000, 356:1423-1430.
3. Hammer SM, Eron JJ, Reiss P. Antiretroviral treatment of adult HIV infection: 2008 recommendations of the International AIDS Society-USA panel. JAMA 2008, 300:555-570.
4. Marzolini C, Telenti A, Decosterd LA, Greub G, Biollaz J, Buclin T. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS 2001, 15:71-75.
5. Cespedes MS, Aberg JA. Neuropsychiatric complications of antiretroviral therapy. Drug Saf 2006, 29:865-874.
6. Caso JA, Prieto Jde M, Casas E, Sanz J. Gynecomastia without lipodystrophy syndrome in HIV-infected men treated with efavirenz. AIDS 2001, 15:1447-1448.
7. Mercie P, Viallard JF, Thiebaut R. Efavirenz-associated breast hypertrophy in HIV-infection patients. AIDS 2001, 15:126-129.
8. Rahim S, Ortiz O, Maslow M, Holzman R. A case-control study of gynecomastia in HIV-1-infected patients receiving HAART. AIDS Read 2004, 14:23-24. 29-32, 35-40
9. Manfredi R, Calza L, Chiodo F. Efavirenz versus nevirapine in current clinical practice: a prospective, open-label observational study. J Acquir Immune Defic Syndr 2004, 35:492-502.
10. Jover F, Cuadrado JM, Roig P, Rodriguez M, Andreu L, Merino J. Efavirenz-associated gynecomastia: report of five cases and review of the literature. Breast J 2004, 10:244-246.
11. Mira JA, Lozano F, Santos J. Gynaecomastia in HIV-infected men on highly active antiretroviral therapy: association with efavirenz and didanosine treatment. Antivir Ther 2004, 9:511-517.
12. Sikora MJ, Cordero KE, Larios JM, Johnson MD, Lippman ME, Rae JM. The androgen metabolite 5alpha-androstane-3beta,17beta-diol (3betaAdiol) induces breast cancer growth via estrogen receptor: implications for aromatase inhibitor resistance. Breast Cancer Res Treat 2009, 115:289-296.
13. Stahle L, Moberg L, Svensson JO, Sonnerborg A. Efavirenz plasma concentrations in HIV-infected patients: inter- and intraindividual variability and clinical effects. Ther Drug Monit 2004, 26:267-270.
14. Dobrzycka KM, Townson SM, Jiang S, Oesterreich S. Estrogen receptor corepressors - a role in human breast cancer? Endocr Relat Cancer 2003, 10:517-536.
15. Shiels MS, Cole SR, Kirk GD, Poole C. A meta-analysis of the incidence of non-AIDS cancers in HIV-infected individuals. J Acquir Immune Defic Syndr 2009, 52:611-622.
16. Kegg S, Lau R. Tamoxifen in antiretroviral-associated gynaecomastia. Int J STD AIDS 2002, 13:582-583.
17. Perdona S, Autorino R, De Placido S. Efficacy of tamoxifen and radiotherapy for prevention and treatment of gynaecomastia and breast pain caused by bicalutamide in prostate cancer: a randomised controlled trial. Lancet Oncol 2005, 6:295-300.
18. Fradet Y, Egerdie B, Andersen M. Tamoxifen as prophylaxis for prevention of gynaecomastia and breast pain associated with bicalutamide 150 mg monotherapy in patients with prostate cancer: a randomised, placebo-controlled, dose-response study. Eur Urol 2007, 52:106-114.
19. Johnson MD, Zuo H, Lee KH. Pharmacological characterization of 4-hydroxy-N-desmethyl tamoxifen, a novel active metabolite of tamoxifen. Breast Cancer Res Treat 2004, 85:151-159.
20. Rae JM, Johnson MD, Scheys JO, Cordero KE, Larios JM, Lippman ME. GREB 1 is a critical regulator of hormone dependent breast cancer growth. Breast Cancer Res Treat 2005, 92:141-149.
21. Rae JM, Lippman ME. Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitors. Breast Cancer Res Treat 2004, 83:99-107.