Pharmacodynamic imaging guides dosing of a selective estrogen receptor degrader

Clinical Cancer Research

Volumn 21, Issue 6, 2015, Pages 1340-1347

  Heidari, Pedram ^a   Deng, Francis ^a,b   Esfahani, Shadi A ^a   Leece, Alicia K ^a   Shoup, Timothy M ^a   Vasdev, Neil ^a   Mahmood, Umar ^a  

^a MASSACHUSETTS GENERAL HOSPITAL   (United States)

^b WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ESTROGEN RECEPTOR ALPHA; FLUORODEOXYGLUCOSE F 18; FULVESTRANT; KI 67 ANTIGEN; MESSENGER RNA; RADIOPHARMACEUTICAL AGENT; ANTINEOPLASTIC HORMONE AGONISTS AND ANTAGONISTS; ESTRADIOL; ESTROGEN RECEPTOR; ESTROGEN RECEPTOR ANTAGONIST;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BREAST CANCER; CANCER INHIBITION; CANCER MODEL; COMPUTER ASSISTED EMISSION TOMOGRAPHY; CONTROLLED STUDY; DEGRADATION KINETICS; DRUG MECHANISM; ENZYME LINKED IMMUNOSORBENT ASSAY; ESR1 GENE; EX VIVO STUDY; FEMALE; HISTOPATHOLOGY; HUMAN; HUMAN CELL; IMMUNOHISTOCHEMISTRY; MCF 7 CELL LINE; MOUSE; NONHUMAN; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL; PROCESS OPTIMIZATION; PROTEIN EXPRESSION; QUANTITATIVE ANALYSIS; RECEPTOR BLOCKING; TUMOR VOLUME; ANALOGS AND DERIVATIVES; ANIMAL; BREAST NEOPLASMS; DIAGNOSTIC IMAGING; DRUG SCREENING; MCF-7 CELL LINE; METABOLISM; NUDE MOUSE; POSITRON EMISSION TOMOGRAPHY; PROCEDURES; TUMOR CELL LINE;

ANIMALS; ANTINEOPLASTIC AGENTS, HORMONAL; BREAST NEOPLASMS; CELL LINE, TUMOR; ESTRADIOL; ESTROGEN RECEPTOR ANTAGONISTS; FEMALE; HUMANS; MCF-7 CELLS; MICE; MICE, NUDE; POSITRON-EMISSION TOMOGRAPHY; RECEPTORS, ESTROGEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84928011638     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-14-1178     Document Type: Article

References (39)

1. Dunnwald LK, Rossing MA, Li CI. Hormone receptor status, tumor characteristics, and prognosis: a prospective cohort of breast cancer patients. Breast Cancer Res 2007;9:R6.
2. Li CI, Daling JR, Malone KE. Incidence of invasive breast cancer by hormone receptor status from 1992 to 1998. J Clin Oncol 2003; 21:28-34.
3. Osborne CK, Yochmowitz MG, Knight WA III, McGuire WL. The value of estrogen and progesterone receptors in the treatment of breast cancer. Cancer 1980;46:2884-8.
4. Nicholson RI, Bouzubar N,Walker KJ,McClelland R, Dixon AR, Robertson JF, et al. Hormone sensitivity in breast cancer: influence of heterogeneity of oestrogen receptor expression and cell proliferation. Eur J Cancer 1991; 27:908-13.
5. Osborne CK. Heterogeneity in hormone receptor status in primary and metastatic breast cancer. Semin Oncol 1985;12:317-26.
6. Long X, Nephew KP. Fulvestrant (ICI 182,780)-dependent interacting proteins mediate immobilization and degradation of estrogen receptor-alpha. J Biol Chem 2006;281:9607-15.
7. Nawaz Z, Lonard DM, Dennis AP, Smith CL, O'Malley BW. Proteasome-dependent degradation of the human estrogen receptor. Proc Natl Acad Sci U S A 1999;96:1858-62.
8. Dauvois S, White R, Parker MG. The antiestrogen ICI 182780 disrupts estrogen receptor nucleocytoplasmic shuttling. J Cell Sci 1993;106: 1377-88.
9. Howell A, Robertson JF, Quaresma Albano J, Aschermannova A, Mauriac L, Kleeberg UR, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. J Clin Oncol 2002;20:3396-403.
10. Osborne CK, Pippen J, Jones SE, Parker LM, Ellis M, Come S, et al. Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial. J Clin Oncol 2002;20:3386-95.
11. Robertson JF, Llombart-Cussac A, Rolski J, Feltl D, Dewar J,Macpherson E, et al. Activity of fulvestrant 500 mg versus anastrozole 1 mg as first-line treatment for advanced breast cancer: results from the FIRST study. J Clin Oncol 2009;27:4530-5.
12. Robertson JF. Fulvestrant (Faslodex) - how to make a good drug better. Oncologist 2007;12:774-84.
13. DeFriend DJ, Howell A, Nicholson RI, Anderson E, DowsettM, Mansel RE, et al. Investigation of a new pure antiestrogen (ICI 182780) in women with primary breast cancer. Cancer Res 1994;54:408-14.
14. Robertson JF, Nicholson RI, Bundred NJ, Anderson E, Rayter Z, Dowsett M, et al. Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17betadiol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer. Cancer Res 2001;61:6739-46.
15. Ohno S, Rai Y, Iwata H, Yamamoto N, Yoshida M, Iwase H, et al. Three dose regimens of fulvestrant in postmenopausal Japanese women with advanced breast cancer: results from a double-blind, phase II comparative study (FINDER1). Ann Oncol 2010;21:2342-7.
16. Pritchard KI, Rolski J, Papai Z,Mauriac L, Cardoso F, Chang J, et al. Results of a phase II study comparing three dosing regimens of fulvestrant in postmenopausal women with advanced breast cancer (FINDER2). Breast Cancer Res Treat 2010;123:453-61.
17. Di Leo A, Jerusalem G, Petruzelka L, Torres R, Bondarenko IN, Khasanov R, et al. Results of the CONFIRM phase III trial comparing fulvestrant 250 mg with fulvestrant 500 mg in postmenopausal women with estrogen receptor-positive advanced breast cancer. J Clin Oncol 2010;28:4594-600.
18. Garnett SA, Martin M, Jerusalem G, Petruzelka L, Torres R, Bondarenko IN, et al. Comparing duration of response and duration of clinical benefit between fulvestrant treatment groups in the CONFIRM trial: application of new methodology. Breast Cancer Res Treat 2013;138:149-55.
19. Heidari P, Wehrenberg-Klee E, Habibollahi P, Yokell D, Kulke M, Mahmood U. Free somatostatin receptor fraction predicts the antiproliferative effect of octreotide in a neuroendocrine tumor model: implications for dose optimization. Cancer Res 2013;73:6865-73.
20. McGuire AH, Dehdashti F, Siegel BA, Lyss AP, Brodack JW,Mathias CJ, et al. Positron tomographic assessment of 16 alpha-[18F] fluoro-17 beta-estradiol uptake in metastatic breast carcinoma. J Nucl Med 1991;32:1526-31.
21. Mortimer JE, Dehdashti F, Siegel BA, Katzenellenbogen JA, Fracasso P, Welch MJ. Positron emission tomography with 2-[18F]Fluoro-2-deoxy-D-glucose and 16alpha-[18F]fluoro-17beta-estradiol in breast cancer: correlation with estrogen receptor status and response to systemic therapy. Clin Cancer Res 1996;2:933-9.
22. Sundararajan L, Linden HM, Link JM, Krohn KA, Mankoff DA. 18F-Fluoroestradiol. Semin Nucl Med 2007;37:470-6.
23. Dehdashti F, Mortimer JE, Siegel BA, Griffeth LK, Bonasera TJ, Fusselman MJ, et al. Positron tomographic assessment of estrogen receptors in breast cancer: comparison with FDG-PET and in vitro receptor assays. J Nucl Med 1995;36:1766-74.
24. Peterson LM, Mankoff DA, Lawton T, Yagle K, Schubert EK, Stekhova S, et al. Quantitative imaging of estrogen receptor expression in breast cancer with PET and 18F-fluoroestradiol. J Nucl Med 2008;49:367-74.
25. Peterson LM, Kurland BF, Schubert EK, Link JM, Gadi VK, Specht JM, et al. A phase 2 study of 16alpha-[F]-fluoro-17beta-estradiol positron emission tomography (FES-PET) as a marker of hormone sensitivity in metastatic breast cancer (MBC). Mol Imaging Biol 2014;16:431-40.
26. Currin E, Linden HM, Mankoff DA. Predicting breast cancer endocrine responsiveness using molecular imaging. Curr Breast Cancer Rep 2011; 3:205-11.
27. Linden HM, Stekhova SA, Link JM, Gralow JR, Livingston RB, Ellis GK, et al. Quantitative fluoroestradiol positron emission tomography imaging predicts response to endocrine treatment in breast cancer. J Clin Oncol 2006;24:2793-9.
28. Dehdashti F, Mortimer JE, Trinkaus K, Naughton MJ, Ellis M, Katzenellenbogen JA, et al. PET-based estradiol challenge as a predictive biomarker of response to endocrine therapy in women with estrogen-receptor-positive breast cancer. Breast Cancer Res Treat 2009;113:509-17.
29. Linden HM, Kurland BF, Peterson LM, Schubert EK, Gralow JR, Specht JM, et al. Fluoroestradiol positron emission tomography reveals differences in pharmacodynamics of aromatase inhibitors, tamoxifen, and fulvestrant in patients with metastatic breast cancer. Clin Cancer Res 2011;17:4799-805.
30. Lim JL, Zheng L, Berridge MS, Tewson TJ. The use of 3-methoxymethyl-16 beta, 17 beta-epiestriol-O-cyclic sulfone as the precursor in the synthesis of F-18 16 alpha-fluoroestradiol. Nucl Med Biol 1996;23:911-5.
31. Fowler AM, Chan SR, Sharp TL, Fettig NM, Zhou D, Dence CS, et al. Small-animal PET of steroid hormone receptors predicts tumor response to endocrine therapy using a preclinical model of breast cancer. J Nucl Med 2012;53:1119-26.
32. Kuter I, Gee JM, Hegg R, Singer CF, Badwe RA, Lowe ES, et al. Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized Phase II study. Breast Cancer Res Treat 2012;133:237-46.
33. van Kruchten M, de Vries EG, Brown M, de Vries EF, Glaudemans AW, Dierckx RA, et al. PET imaging of oestrogen receptors in patients with breast cancer. Lancet Oncol 2013;14:e465-75.
34. van Kruchten M, De Vries E, Brown M, Glaudemans AWJM, van Lanschot MC, Kema IP, et al. Residual estrogen receptor availability during fulvestrant 500 mg therapy in patients with metastatic breast cancer. ASCO Annual Meeting 2014;2014. p. 588.
35. Du X, Li XQ, Li L, Xu YY, Feng YM. The detection of ESR1/PGR/ERBB2 mRNA levels by RT-QPCR: a better approach for subtyping breast cancer and predicting prognosis. Breast Cancer Res Treat 2013;138:59-67.
36. Pentheroudakis G, Kotoula V, Eleftheraki AG, Tsolaki E, Wirtz RM, Kalogeras KT, et al. Prognostic significance of ESR1 gene amplification, mRNA/protein expression and functional profiles in high-risk early breast cancer: a translational study of the Hellenic Cooperative Oncology Group (HeCOG). PLoS One 2013;8:e70634.
37. Mankoff DA, Dehdashti F, Shields AF. Characterizing tumors using metabolic imaging: PET imaging of cellular proliferation and steroid receptors. Neoplasia 2000;2:71-88.
38. Brodie A, Jelovac D, Long BJ. Predictions from a preclinical model: studies of aromatase inhibitors and antiestrogens. Clin Cancer Res 2003;9:455S-459S.
39. Hoffmann J, Bohlmann R, Heinrich N, Hofmeister H, Kroll J, Kunzer H, et al. Characterization of new estrogen receptor destabilizing compounds: effects on estrogen-sensitive and tamoxifen-resistant breast cancer. J Natl Cancer Inst 2004;96:210-8.