11,751
Views
13
CrossRef citations to date
0
Altmetric
Review

Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer

, , , , , , & show all
Pages 515-529 | Received 12 Aug 2021, Accepted 17 Sep 2021, Published online: 25 Oct 2021

References

  • Sharma R. Breast cancer incidence, mortality and mortality-to-incidence ratio (MIR) are associated with human development, 1990–2016: evidence from global burden of disease study 2016. Breast Cancer. 2019;26(4):428–445.
  • Sung H, Ferlay J, Siegel RL, et al. Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries. Ca Cancer J Clin. 2021;71(3):209–249.
  • Lüönd F, Tiede S, Christofori G. Breast cancer as an example of tumour heterogeneity and tumour cell plasticity during malignant progression. Br J Cancer. 2021;125(2):164–175.
  • Stravodimou A, Voutsadakis IA. The Future of ER+/HER2− metastatic breast cancer therapy: beyond PI3K Inhibitors. Anticancer Res. 2020;40(9):4829–4841.
  • Allison KH, Hammond MEH, Dowsett M, et al. Estrogen and progesterone receptor testing in breast cancer: ASCO/CAP guideline update. J Clin Oncol. 2020;38(12):1346–1366.
  • Harvey JM, Clark GM, Osborne CK, et al. Estrogen receptor status by immunohistochemistry is superior to the ligand-binding assay for predicting response to adjuvant endocrine therapy in breast cancer. J Clin Oncol. 1999;17(5):1474–1481.
  • Lumachi F, Santeufemia DA, Basso SM. Current medical treatment of estrogen receptor-positive breast cancer. World J Biol Chem. 2015;6(3):231–239.
  • Musgrove EA, Sutherland RL. Biological determinants of endocrine resistance in breast cancer. Nat Rev Cancer. 2009;9(9):631–643.
  • Patel HK, Bihani T. Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment. Pharmacol Ther. 2018;186:1–24.
  • National Comprehensive Cancer Network (NCCN). NCCN clinical practice guidelines in oncology (NCCN Guidelines®): breast cancer. Version 4. 2021 [cited 2021 May]. Available from: https://www.nccn.org/professionals/physician_gls/pdf/breast.pdf
  • Cardoso F, Kyriakides S, Ohno S, et al. Early breast cancer: ESMO clinical practice guidelines for diagnosis, treatment and follow-up. Ann Oncol. 2019;30(8):1194–1220.
  • Cardoso F, Paluch-Shimon S, Senkus E, et al. 5th ESO-ESMO international consensus guidelines for advanced breast cancer (ABC 5). Ann Oncol. 2020;31(12):1623–1649.
  • Cybulski C, Huzarski T, Byrski T, et al. Estrogen receptor status in CHEK2-positive breast cancers: implications for chemoprevention. Clin Genet. 2009;75(1):72–78.
  • Szostakowska M, Trębińska-Stryjewska A, Grzybowska EA, et al. Resistance to endocrine therapy in breast cancer: molecular mechanisms and future goals. Breast Cancer Res Treat. 2019;173(3):489–497.
  • Nardone A, De Angelis C, Trivedi MV, et al. The changing role of ER in endocrine resistance. Breast. 2015;24 Suppl 2(2):S60–66.
  • Robinson DR, Wu YM, Vats P, et al. Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat Genet. 2013;45(12):1446–1451.
  • Lei JT, Anurag M, Haricharan S, et al. Endocrine therapy resistance: new insights. Breast. 2019;Suppl 48(Suppl1):S26–S30.
  • Bahreini A, Li Z, Wang P, et al. Mutation site and context dependent effects of ESR1 mutation in genome-edited breast cancer cell models. BCR. 2017;19(1):60.
  • Jeselsohn R, Yelensky R, Buchwalter G, et al. Emergence of constitutively active estrogen receptor-α mutations in pretreated advanced estrogen receptor–positive breast cancer. Clin Cancer Res off J Am Assoc Cancer Res. 2014;20(7):1757–1767.
  • Hartmaier RJ, Trabucco SE, Priedigkeit N, et al. Recurrent hyperactive ESR1 fusion proteins in endocrine therapy-resistant breast cancer. Ann Oncol. 2018;29(4):872–880.
  • Lei JT, Shao J, Zhang J, et al. Functional annotation of ESR1 gene fusions in estrogen receptor-positive breast cancer. Cell Rep. 2018;24(6):1434–1444.e1437.
  • Turner NC, Swift C, Kilburn L, et al. ESR1 mutations and overall survival on fulvestrant versus exemestane in advanced hormone receptor-positive breast cancer: a combined analysis of the phase III SoFEA and EFECT trials. Clin Cancer Res off J Am Assoc Cancer Res. 2020;26(19):5172–5177.
  • De Santo I, McCartney A, Migliaccio I, et al. The emerging role of ESR1 mutations in luminal breast cancer as a prognostic and predictive biomarker of response to endocrine therapy. Cancers (Basel). 2019;11(12):1894.
  • Gottardis MM, Jordan VC. Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. Cancer Res. 1988;48(18):5183–5187.
  • Chang M. Tamoxifen resistance in breast cancer. Biomol Ther (Seoul). 2012;20(3):256–267.
  • Hanker AB, Sudhan DR, Arteaga CL. Overcoming endocrine resistance in breast cancer. Cancer Cell. 2020;37(4):496–513.
  • Razavi P, Chang MT, Xu G, et al. The genomic landscape of endocrine-resistant advanced breast cancers. Cancer Cell. 2018;34(3):427–438.e426.
  • Cancer Genome AN. Comprehensive molecular portraits of human breast tumours. Nature. 2012;490(7418):61–70.
  • Perez EA. Safety profiles of tamoxifen and the aromatase inhibitors in adjuvant therapy of hormone-responsive early breast cancer. Ann Oncol. 2007;18(Suppl 8):viii26–35.
  • Tseng OL, Spinelli JJ, Gotay CC, et al. Aromatase inhibitors are associated with a higher fracture risk than tamoxifen: a systematic review and meta-analysis. Ther Adv Musculoskelet Dis. 2018;10(4):71–90.
  • Schulz M, Klopp-Schulze L, Keilhack S, et al. Adherence to tamoxifen in breast cancer patients: what role does the pharmacist play in German primary care? Can Pharm J (Ott). 2019;152(1):28–34.
  • Moon Z, Moss-Morris R, Hunter MS, et al. Understanding tamoxifen adherence in women with breast cancer: a qualitative study. Br J Health Psychol. 2017;22(4):978–997.
  • Lin JH, Zhang SM, Manson JE. Predicting adherence to tamoxifen for breast cancer adjuvant therapy and prevention. Cancer Prev Res (Phila). 2011;4(9):1360–1365.
  • Murphy CC, Bartholomew LK, Carpentier MY, et al. Adherence to adjuvant hormonal therapy among breast cancer survivors in clinical practice: a systematic review. Breast Cancer Res Treat. 2012;134(2):459–478.
  • Partridge AH, Carey LA. Unmet needs in clinical research in breast cancer: where do we need to go? Clin Cancer Res off J Am Assoc Cancer Res. 2017;23(11):2611–2616.
  • Dodwell D, Wardley A, Johnston S. Postmenopausal advanced breast cancer: options for therapy after tamoxifen and aromatase inhibitors. Breast. 2006;15(5):584–594.
  • Howell A, Osborne CK, Morris C, et al. ICI 182,780 (Faslodex): development of a novel, “pure” antiestrogen. Cancer. 2000;89(4):817–825.
  • Bross PF, Cohen MH, Williams GA, et al. FDA drug approval summaries: fulvestrant. Oncologist. 2002;7(6):477–480.
  • Faslodex® (fulvestrant). Prescribing Information. AstraZeneca 2021 [cited 2021 Apr 7]. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/021344s044lbl.pdf
  • Faslodex® (fulvestrant). Summary of product characteristics. AstraZeneca 2020 [cited 2021 Apr 7]. Available from: https://www.ema.europa.eu/en/documents/product-information/faslodex-epar-product-information_en.pdf
  • Wakeling AE, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991;51(15):3867–3873.
  • Johnston SR. Endocrinology and hormone therapy in breast cancer: selective oestrogen receptor modulators and downregulators for breast cancer – have they lost their way? BCR. 2005;7(3):119–130.
  • Harrison M, Laight A, Clarke D, et al. Pharmacokinetics and metabolism of fulvestrant after oral, intravenous and intramuscular administration in healthy volunteers. 2003;5(1):Abstract564.EJC supplements: EJC: official journal of EORTC, European Organization for Research and Treatment of Cancer [et al]
  • Robertson JF, Harrison M. Fulvestrant: pharmacokinetics and pharmacology. Br J Cancer. 2004;Suppl 90(Suppl S1):S7–10.
  • Robertson JFR, Erikstein B, Osborne KC, et al. Pharmacokinetic profile of intramuscular fulvestrant in advanced breast cancer. Clin Pharmacokinet. 2004;43(8):529–538.
  • Robertson JF, Lindemann J, Garnett S, et al. A good drug made better: the fulvestrant dose-response story. Clin Breast Cancer. 2014;14(6):381–389.
  • Howell A, Robertson JF, Quaresma Albano J, 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(16):3396–3403.
  • Osborne CK, Pippen J, Jones SE, 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(16):3386–3395.
  • Howell A, Robertson JF, Abram P, et al. Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: a multinational, double-blind, randomized trial. J Clin Oncol. 2004;22(9):1605–1613.
  • Di Leo A, Jerusalem G, Petruzelka L, 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(30):4594–4600.
  • Robertson JFR, Bondarenko IM, Trishkina E, et al. Fulvestrant 500 mg versus anastrozole 1 mg for hormone receptor-positive advanced breast cancer (FALCON): an international, randomised, double-blind, phase 3 trial. Lancet. 2016;388(10063):2997–3005.
  • Gandell DL, Bienen EJ, Gudeman J. Mode of injection and treatment adherence: results of a survey characterizing the perspectives of health care providers and US women 18-45 years old. Patient Prefer Adherence. 2019;13:351–361.
  • Soliman E, Ranjan S, Xu T, et al. A narrative review of the success of intramuscular gluteal injections and its impact in psychiatry. Biodes Manuf. 2018;1(3):161–170.
  • Lai A, Kahraman M, Govek S, et al. Identification of GDC-0810 (ARN-810), an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts. J Med Chem. 2015;58(12):4888–4904.
  • Cheung KWK, Yoshida K, Cheeti S, et al. GDC-0810 pharmacokinetics and transporter-mediated drug interaction evaluation with an endogenous biomarker in the first-in-human, dose escalation study. Drug Metab Dispos. 2019;47(9):966–973.
  • Hou HH, Jia W, Liu L, et al. Effect of microenvironmental ph modulation on the dissolution rate and oral absorption of the salt of a weak acid – case study of GDC-0810. Pharm Res. 2018;35(2):37.
  • Cheeti S, Hou HH, Nelson E, et al. Application of a novel ‘make and test in parallel’ strategy to investigate the effect of formulation on the pharmacokinetics of GDC-0810 in healthy subjects. Pharm Res. 2018;35(12):233.
  • Joseph JD, Darimont B, Zhou W, et al. The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer. Elife. 2016;5:e15828.
  • Guan J, Zhou W, Hafner M, et al. Therapeutic ligands antagonize estrogen receptor function by impairing its mobility. Cell. 2019;178(4):949–963.e918.
  • Kahraman M, Govek SP, Nagasawa JY, et al. Maximizing ER-α degradation maximizes activity in a tamoxifen-resistant breast cancer model: identification of GDC-0927. ACS Med Chem Lett. 2018;10(1):50–55. including supplementary content
  • Liang J, Zbieg JR, Blake RA, et al., GDC-9545 (giredestrant): a potent and orally bioavailable selective estrogen receptor antagonist and degrader with an exceptional preclinical profile for ER+ breast cancer. J Med Chem. 64(16): 11841–11856. 2021.
  • Jhaveri K, Winer EP, Lim E, et al. A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-9545, in postmenopausal women with estrogen receptor-positive (ER+) HER2-negative (HER2–) metastatic breast cancer. Cancer Res. 2020;80(suppl 4):PD7-05. DOI: https://doi.org/10.1158/1538-7445.SABCS19-PD7-05
  • Metcalfe C, Ingalla E, Blake R, et al. GDC-9545: a novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes. Cancer Res. 2019;79(4Suppl):47.
  • Metcalfe C, Zhou W, Guan J, et al. GDC-9545: a pure antiestrogen clinical candidate that immobilizes the estrogen receptor and profoundly alters chromatin accessibility in vivo. Cancer Res. 2020;80(16Suppl):Abstract3406.
  • El-Ahmad Y, Tabart M, Halley F, et al. Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a potent and selective estrogen receptor degrader (SERD) for the treatment of estrogen-receptor-positive breast cancer. J Med Chem. 2020;63(2):512–528.
  • Shomali M, Cheng J, Sun F, et al. SAR439859, a Novel selective estrogen receptor degrader (SERD), demonstrates effective and broad antitumor activity in wild-type and mutant ER-positive breast cancer models. Mol Cancer Ther. 2021;20(2):250–262. including supplementary content
  • Campone M, Bardia A, Ulaner GA, et al. Dose-escalation study of SAR439859, an oral selective estrogen receptor degrader, in postmenopausal women with estrogen receptor-positive and human epidermal growth factor receptor 2-negative metastatic breast cancer. Cancer Res. 2020;80(4 Suppl):Abstract nr P5-11-02. DOI: https://doi.org/10.1158/1538-7445.SABCS19-P5-11-02
  • Chandarlapaty S, Linden HM, Neven P, et al. AMEERA-1: phase 1/2 study of amcenestrant (SAR439859), an oral selective estrogen receptor (ER) degrader (SERD), with palbociclib (palbo) in postmenopausal women with ER+/ human epidermal growth factor receptor 2-negative (HER2-) metastatic breast cancer (mBC). J Clin Oncol. 2021;39(15Suppl): 1058.
  • Campone M, Herold CI, Wang Q, et al. Phase II preoperative window study of SAR439859 versus letrozole in post-menopausal women with newly diagnosed estrogen receptor-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer. J Clin Oncol. 2020;38(15_suppl):1108.
  • Scott JS, Moss TA, Balazs A, et al. Discovery of AZD9833, a potent and orally bioavailable selective estrogen receptor degrader and antagonist. J Med Chem. 2020;63(23):14530–14559. including supplementary content
  • Scott JS, Moss T, Stokes S, et al. Discovery of AZD9833, an oral small molecule selective degrader of the estrogen receptor (SERD). Cancer Res. 2020;80(16Suppl):Abstract5674.
  • Bardia A, Kaklamani V, Wilks S, et al., Phase I study of elacestrant (RAD1901), a novel selective estrogen receptor degrader, in ER-positive, HER2-negative advanced breast cancer. J Clin Oncol. 39(12): 1360–1370. 2021.
  • Jager A, de Vries EGE, der Houven van Oordt CWM, et al., A phase 1b study evaluating the effect of elacestrant treatment on estrogen receptor availability and estradiol binding to the estrogen receptor in metastatic breast cancer lesions using 18F-FES PET/CT imaging. BCR. 22(1): 97. 2020.
  • Wardell SE, Nelson ER, Chao CA, et al. Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader. Endocr Relat Cancer. 2015;22(5):713–724.
  • Andreano KJ, Wardell SE, Baker JG, et al. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020;180(3):635–646. including supplementary content
  • Dees E, Aftimos P, van Oordt H, et al. Dose-escalation study of G1T48, an oral selective estrogen receptor degrader (SERD), in postmenopausal women with ER+/HER2- locally advanced or metastatic breast cancer (ABC). Ann Oncol. 2019;30:v121–v122. Abstract 340P and associated poster presentation
  • Aftimos P, Neven P, Pegram M, et al. Rintodestrant (G1T48), an oral selective estrogen receptor degrader in ER+/HER2- locally advanced or metastatic breast cancer: updated phase 1 results and dose selection. Cancer Res. 2021;81(4 Suppl):Abstract nr PS12-04. DOI: https://doi.org/10.1158/1538-7445.SABCS20-PS12-04
  • Beelen AP, Li C, Jarugula P, et al. Population pharmacokinetic and exposure-response modeling of the oral selective estrogen receptor degrader, rintodestrant (G1T48), in patients with ER+/HER2- advanced breast cancer. Cancer Res. 2021;81(4 Suppl):Abstract nr PS17-08. DOI: https://doi.org/10.1158/1538-7445.SABCS20-PS17-08
  • Liu L, Cheeti S, Yoshida K, et al. Effect of OATP1B1/1B3 inhibitor GDC-0810 on the pharmacokinetics of pravastatin and coproporphyrin I/III in healthy female subjects. J Clin Pharmacol. 2018;58(11):1427–1435.
  • Gangl ET, Markandu R, Sharma P, et al. Preclinical pharmacokinetic and metabolic characterization of the next generation oral SERD AZD9833. Cancer Res. 2020;80(16 Suppl):Abstract nr 1042. DOI: https://doi.org/10.1158/1538-7445.AM2020-1042
  • Garner F, Shomali M, Paquin D, et al. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. Anticancer Drugs. 2015;26(9):948–956.
  • Bihani T, Patel HK, Arlt H, et al. Elacestrant (RAD1901), a selective estrogen receptor degrader (SERD), has antitumor activity in multiple ER(+) breast cancer patient-derived xenograft models. Clin Cancer Res off J Am Assoc Cancer Res. 2017;23(16):4793–4804.
  • Patel HK, Tao N, Lee KM, et al. Elacestrant (RAD1901) exhibits anti-tumor activity in multiple ER+ breast cancer models resistant to CDK4/6 inhibitors. BCR. 2019;21(1):146.
  • Patel H, Tao N, Arlt H, et al. Anti-tumor activity of elacestrant (RAD1901) in models harboring ESR1 mutations resistant to standard of care therapies. Cancer Res. 2019;79(4 Suppl):Abstract nr P6-20-08. DOI: https://doi.org/10.1158/1538-7445.SABCS18-P6-20-08.
  • Wardell SE, Yllanes AP, Baker JG, et al. Effects of G1T48, a novel orally bioavailable selective estrogen receptor degrader (SERD), and the CDK4/6 inhibitor, G1T38, on tumor growth in animal models of endocrine resistant breast cancer. Cancer Res. 2017;77(13 Suppl):Abstract nr 5641. DOI: https://doi.org/10.1158/1538-7445.AM2017-5641
  • Wang Y, Ayres KL, Goldman DA, et al. (18) F-Fluoroestradiol PET/CT measurement of estrogen receptor suppression during a phase I trial of the novel estrogen receptor-targeted therapeutic GDC-0810: using an imaging biomarker to guide drug dosage in subsequent trials. Clin Cancer Res off J Am Assoc Cancer Res. 2017;23(12):3053–3060.
  • Dickler M, Villanueva R, Perez Fidalgo J, et al. A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-0927, in postmenopausal women with estrogen receptor positive (ER+) HER2-negative metastatic breast cancer (BC). Cancer Res 2018;78(4 Suppl):Abstract nr PD5-10. DOI: https://doi.org/10.1158/1538-7445.SABCS17-PD5-10
  • Jhaveri KL, Boni V, Sohn J, et al. Safety and activity of single-agent giredestrant (GDC-9545) from a phase Ia/b study in patients (pts) with estrogen receptor-positive (ER+), HER2-negative locally advanced/metastatic breast cancer (LA/mBC). J Clin Oncol. 2021;39(15_suppl):1017. Abstract 1017 and associated poster presentation.
  • van Kruchten M, de Vries EG, Glaudemans AW, et al. Measuring residual estrogen receptor availability during fulvestrant therapy in patients with metastatic breast cancer. Cancer Discov. 2015;5(1):72–81.
  • Moore HM, Boni V, Bellet M, et al. Evaluation of pharmacodynamic (PD) and biologic activity in a preoperative window-of-opportunity (WOO) study of giredestrant (GDC-9545) in postmenopausal patients (pts) with estrogen receptor-positive, HER2-negative (ER+/HER2–) operable breast cancer (BC). J Clin Oncol. 2021;39(15_suppl):577. Abstract 577 and associated poster presentation
  • Lim E, Jhaveri KL, Perez-Fidalgo JA, et al. A phase Ib study to evaluate the oral selective estrogen receptor degrader GDC-9545 alone or combined with palbociclib in metastatic ER-positive HER2-negative breast cancer. J Clin Oncol. 2020;38(15_suppl):1023. Abstract 1023 and associated poster presentation
  • Campone M, Bardia A, Ulaner GA, et al. Phase I/II study of SAR439859, an oral selective estrogen receptor degrader (SERD), in estrogen receptor-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-) metastatic breast cancer (mBC). J Clin Oncol. 2020;38(15_suppl):1070. Abstract 1070 and associated poster presentation.
  • Hamilton EP, Oliveira M, Banerji U, et al. A phase I dose escalation and expansion study of the next generation oral SERD AZD9833 in women with ER-positive, HER2-negative advanced breast cancer. J Clin Oncol. 2020;38(15_suppl):1024. Abstract 1024 and associated poster presentation.
  • Roncato R, Angelini J, Pani A, et al. CDK4/6 inhibitors in breast cancer treatment: potential interactions with drug, gene, and pathophysiological conditions. Int J Mol Sci. 2020;21(17):6350.
  • Baird R, Oliveira M, Gil EMC, et al. Updated data from SERENA-1: a phase 1 dose escalation and expansion study of the next generation oral SERD AZD9833 as a monotherapy and in combination with palbociclib, in women with ER-positive, HER2-negative advanced breast cancer. Cancer Res. 2021;81(4 Suppl):Abstract nr PS11-05. DOI: https://doi.org/10.1158/1538-7445.SABCS20-PS11-05
  • Clinicaltrials.gov. A comparative study of AZD9833 plus palbociclib versus anastrozole plus palbociclib in patients with ER-positive HER2 negative breast cancer who have not received any systemic treatment for advanced disease. (SERENA-4). 2021 [cited 2021 Jul]. Available from: https://clinicaltrials.gov/ct2/show/NCT04711252
  • Conlan MG, de Vries EFJ, Glaudemans A, et al. Pharmacokinetic and pharmacodynamic studies of elacestrant, a novel oral selective estrogen receptor degrader, in healthy post-menopausal women. Eur J Drug Metab Pharmacokinet. 2020;45(5):675–689.
  • Clinicaltrials.gov. Phase 3 trial of elacestrant vs. standard of care for the treatment of patients with ER+/HER2- advanced breast cancer (EMERALD) 2021 [cited 2021 Jul]. Available from: https://clinicaltrials.gov/ct2/show/NCT03778931
  • Aftimos P, Maglakelidze M, Glaudemans AW, et al. Pharmacodynamic analysis from a phase 1 study of rintodestrant (G1T48), an oral selective estrogen receptor degrader, in ER+/HER2- locally advanced or metastatic breast cancer. Cancer Res. 2021;81(4 Suppl):Abstract nr PD8-07. DOI: https://doi.org/10.1158/1538-7445.SABCS20-PD8-07
  • Maglakelidze M, Bulat I, Ryspayeva D, et al. Rintodestrant (G1T48), an oral selective estrogen receptor degrader, in combination with palbociclib for ER+/HER2– advanced breast cancer: phase 1 results. J Clin Oncol. 2021;39(15_suppl):1063. Abstract 1063 and associated poster presentation